Compounds > sitagliptin phosphate
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sitagliptin phosphate

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Description

Sitagliptin Phosphate: A pyrazine-derived DIPEPTIDYL-PEPTIDASE IV INHIBITOR and HYPOGLYCEMIC AGENT that increases the levels of the INCRETIN hormones GLUCAGON-LIKE PEPTIDE-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). It is used in the treatment of TYPE 2 DIABETES. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11591741
CHEMBL ID1201174
SCHEMBL ID1039535
MeSH IDM0498840

Synonyms (66)

Synonym
AC-1939
mk-0431
tesavel
glactiv
ono-5435
januvia
mk-431
januvia (tn)
sitagliptin phosphate (usan)
D06645
sitagliptin phosphate monohydrate
654671-77-9
sitagliptin phosphate hydrate (jp17)
mk0431 ,
sitagliptin monophosphate monohydrate
sitagliptin phosphate
CHEMBL1201174
sitagliptin phosphate hydrate
sitagliptin monophosphate anhydrous
S4002
unii-ts63ew8x6f
sitagliptin phosphate [usan]
1,2,4-triazolo(4,3-a)pyrazine, 7-((3r)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl)-5,6,7,8- tetrahydro-3-(trifluoromethyl)-, phosphate (1:1) monohydrate
ts63ew8x6f ,
7-((3r)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl)-3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4- triazolo(4,3-a)pyrazine monophosphate monohydrate
sitagliptin phosphate [usp monograph]
sitagliptin phosphate [vandf]
steglujan component sitagliptin phosphate
sitagliptin phosphate [orange book]
sitagliptin phosphate component of janumet
sitagliptin phosphate component of stelujan
sitagliptin phosphate hydrate [jan]
stelujan component sitagliptin phosphate
sitagliptin phosphate component of steglujan
sitagliptin phosphate monohydrate [ep monograph]
1,2,4-triazolo(4,3-a)pyrazine, 7-((3r)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl)-5,6,7,8-tetrahydro-3-(trifluoromethyl), phosphate (1:1) monohydrate
7-[(3r)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyrazine monophosphate monohydrate
janumet component sitagliptin phosphate
sitagliptin monophosphate monohydrate [mi]
sitagliptin phosphate [mart.]
sitagliptin phosphate monohydrate [who-dd]
sitagliptin phosphate [usp-rs]
sitagliptin phosphate [jan]
AKOS015895530
SCHEMBL1039535
CCG-213562
(2r)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8h)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine dihydrogenphosphate monohydrate
(2r)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-alpha]pyrazin-7(8h)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine dihydrogenphosphate monohydrate
CS-3683
(r)-3-amino-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8h)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one phosphate hydrate
sitagliptin monohydrate
sitagliptin (phosphate monohydrate)
HY-13749B
mfcd10001393
(r)-3-amino-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8h)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one phosphate hydra
(3r)-3-amino-1-[3-(trifluoromethyl)-6,8-dihydro-5h-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;phosphoric acid;hydrate
DTXSID50904746
(r)-3-amino-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8h)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one phosphate monohydrate.
654671-77-9 (phosphate hydrate)
AS-18643
7-[(3r)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine phosphate (1:1) monohydrate
AMY1793
1,2,4-triazolo[4,3-a]pyrazine,7-[(3r)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-, phosphate (1:1), monohydrate
Q27290248
sitagpliptin monohydrate
BS164409

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The incidence of hypoglycaemia and gastrointestinal adverse experiences was not significantly different between sitagliptin and placebo."( Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy in patients with type 2 diabetes mellitus.
Caria, C; Hanefeld, M; Khatami, H; Raz, I; Williams-Herman, D; Xu, L, 2006)		0.33
" There was no increased risk of hypoglycemia or gastrointestinal adverse experiences with sitagliptin compared with placebo."( Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin added to ongoing metformin therapy in patients with type 2 diabetes inadequately controlled with metformin alone.
Charbonnel, B; Karasik, A; Liu, J; Meininger, G; Wu, M, 2006)		0.33
" 47%) and drug-related adverse experiences (AEs) (15 vs."( Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, in patients with type 2 diabetes mellitus inadequately controlled on glimepiride alone or on glimepiride and metformin.
Fanurik, D; Hermansen, K; Khatami, H; Kipnes, M; Luo, E; Stein, P, 2007)		0.34
" Careful postmarketing surveillance for adverse effects, especially among the DPP4 inhibitors, and continued evaluation in longer-term studies and in clinical practice are required to determine the role of this new class among current pharmacotherapies for type 2 diabetes."( Efficacy and safety of incretin therapy in type 2 diabetes: systematic review and meta-analysis.
Amori, RE; Lau, J; Pittas, AG, 2007)		0.34
" Clinical and laboratory adverse experiences were similar between treatments, with no reported hypoglycemia adverse events with sitagliptin."( Efficacy and safety of sitagliptin monotherapy in Japanese patients with type 2 diabetes.
Ahmed, T; Davies, MJ; Fujimoto, G; Hirayama, Y; Kakikawa, T; Kato, N; Nonaka, K; Okuyama, K; Sato, A; Stein, PP; Suzuki, H, 2008)		0.35
" Compared with placebo, sitagliptin had a neutral effect on body weight and did not significantly increase the risk of hypoglycemia or gastrointestinal adverse events."( Efficacy and safety of sitagliptin added to ongoing metformin therapy in patients with type 2 diabetes.
Alba, M; Amatruda, JM; Chen, Y; Hussain, S; Kaufman, KD; Langdon, RB; Raz, I; Stein, PP; Wu, M, 2008)		0.35
" Both active treatments were generally well tolerated, with no increased risk of hypoglycaemia or gastrointestinal adverse events compared with placebo."( Efficacy and safety of sitagliptin when added to ongoing metformin therapy in patients with type 2 diabetes.
Davies, MJ; Engel, SS; Loeys, T; Scott, R, 2008)		0.35
" The overall incidence of adverse experiences was generally similar between groups."( Safety and efficacy of sitagliptin in patients with type 2 diabetes and chronic renal insufficiency.
Amatruda, JM; Arjona Ferreira, JC; Chan, JC; Davies, MJ; Gonzalez, E; Kaufman, KD; Scott, R; Sheng, D; Stein, PP; Williams-Herman, D, 2008)		0.35
" Clinical adverse events (AEs) were reported in 23."( Efficacy and safety of sitagliptin in the treatment of patients with type 2 diabetes in China, India, and Korea.
Amatruda, JM; Kaufman, KD; Langdon, RB; Mohan, V; Noble, L; Son, HY; Stein, PP; Xu, L; Yang, W, 2009)		0.35
" The incidence of gastrointestinal adverse experiences with the co-administration of sitagliptin and metformin was similar to that observed with metformin alone."( Efficacy and safety of initial combination therapy with sitagliptin and metformin in patients with type 2 diabetes: a 54-week study.
Amatruda, JM; Davies, MJ; Goldstein, BJ; Johnson, J; Kaufman, KD; Luo, E; Teng, R; Williams-Herman, D, 2009)		0.35
" DPP-4 inhibitors are safe and tolerable with no increased risk of adverse events compared to placebo and have a low risk of hypoglycaemia."( Clinical results of treating type 2 diabetic patients with sitagliptin, vildagliptin or saxagliptin--diabetes control and potential adverse events.
Ahrén, B, 2009)		0.35
"During the first 6 weeks of follow-up, only two major adverse cardiac events occurred (one de novo stenosis and one instent-restenosis) in the first 36 patients."( Safety and efficacy of SITAgliptin plus GRanulocyte-colony-stimulating factor in patients suffering from Acute Myocardial Infarction (SITAGRAMI-Trial)--rationale, design and first interim analysis.
Brenner, C; Engelmann, MG; Franz, WM; Henschel, V; Huber, B; Mansmann, U; Reiser, M; Steinbeck, G; Theiss, HD; Wintersperger, B; Zaruba, MM, 2010)		0.36
"Our data demonstrate that the combined application of Sitagliptin and G-CSF seems to be safe on the short term and feasible after acute myocardial infarction and may represent a new therapeutic option in future."( Safety and efficacy of SITAgliptin plus GRanulocyte-colony-stimulating factor in patients suffering from Acute Myocardial Infarction (SITAGRAMI-Trial)--rationale, design and first interim analysis.
Brenner, C; Engelmann, MG; Franz, WM; Henschel, V; Huber, B; Mansmann, U; Reiser, M; Steinbeck, G; Theiss, HD; Wintersperger, B; Zaruba, MM, 2010)		0.36
" The incidence of gastrointestinal-related adverse experiences was substantially lower with sitagliptin (11."( Efficacy and safety of monotherapy of sitagliptin compared with metformin in patients with type 2 diabetes.
Aschner, P; Goldstein, BJ; Guo, H; Katzeff, HL; Kaufman, KD; Sunga, S; Williams-Herman, D, 2010)		0.36
" Although both treatments were generally well tolerated, a lower incidence of gastrointestinal-related adverse experiences was observed with sitagliptin."( Efficacy and safety of monotherapy of sitagliptin compared with metformin in patients with type 2 diabetes.
Aschner, P; Goldstein, BJ; Guo, H; Katzeff, HL; Kaufman, KD; Sunga, S; Williams-Herman, D, 2010)		0.36
" The incidences of gastrointestinal adverse experiences were generally lower in the sitagliptin group and similar between the metformin monotherapy and combination groups."( Efficacy and safety of sitagliptin and metformin as initial combination therapy and as monotherapy over 2 years in patients with type 2 diabetes.
Amatruda, JM; Goldstein, BJ; Golm, G; Johnson, J; Kaufman, KD; Teng, R; Williams-Herman, D, 2010)		0.36
" The most frequent adverse events with exenatide and sitagliptin were nausea (n=38, 24%, and n=16, 10%, respectively) and diarrhoea (n=29, 18%, and n=16, 10%, respectively); upper-respiratory-tract infection (n=17, 10%) and peripheral oedema (n=13, 8%) were the most frequent events with pioglitazone."( Efficacy and safety of exenatide once weekly versus sitagliptin or pioglitazone as an adjunct to metformin for treatment of type 2 diabetes (DURATION-2): a randomised trial.
Bergenstal, RM; Macconell, L; Malloy, J; Malone, J; Porter, LE; Walsh, B; Wilhelm, K; Wysham, C; Yan, P, 2010)		0.36
" After 12 weeks, the incidences of clinical adverse experiences (AEs), drug-related AEs and gastrointestinal AEs in the sitagliptin group (48."( Efficacy and safety of sitagliptin monotherapy compared with voglibose in Japanese patients with type 2 diabetes: a randomized, double-blind trial.
Amatruda, JM; Arjona Ferreira, JC; Iwamoto, Y; Kadowaki, T; Nishii, M; Nonaka, K; Tajima, N; Taniguchi, T, 2010)		0.36
" Both treatments were generally well tolerated; incidence and types of adverse events were comparable between groups."( Efficacy and safety of saxagliptin in combination with metformin compared with sitagliptin in combination with metformin in adult patients with type 2 diabetes mellitus.
Charpentier, G; Gause-Nilsson, I; Hellqvist, A; Ostgren, CJ; Scheen, AJ, 2010)		0.36
" Safety endpoints included adverse events (AEs) and hypoglycaemia."( Efficacy and safety of insulin detemir once daily in combination with sitagliptin and metformin: the TRANSITION randomized controlled trial.
Hollander, P; Liutkus, JF; Raslova, K; Råstam, J; Skjøth, TV, 2011)		0.37
" Exenatide once-weekly was generally well tolerated and adverse events were predominantly mild or moderate in intensity."( DURATION-2: efficacy and safety of switching from maximum daily sitagliptin or pioglitazone to once-weekly exenatide.
Bergenstal, R; Malloy, J; Malone, J; Taylor, K; Walsh, B; Wysham, C; Yan, P, 2011)		0.37
" They provide lesser effect on PPG, similar reduction in body weight, and result in a potentially favorable adverse event profile compared with exenatide twice daily."( Efficacy and safety of long-acting glucagon-like peptide-1 receptor agonists compared with exenatide twice daily and sitagliptin in type 2 diabetes mellitus: a systematic review and meta-analysis.
Hurren, KM; Pinelli, NR, 2011)		0.37
" A numerically higher incidence of gastrointestinal adverse events and a significantly lower incidence of oedema were observed with SITA/MET vs."( Efficacy and safety of sitagliptin and the fixed-dose combination of sitagliptin and metformin vs. pioglitazone in drug-naïve patients with type 2 diabetes.
Engel, SS; Goldstein, BJ; Kaufman, KD; Lee, MA; Pérez-Monteverde, A; Seck, T; Sisk, CM; Williams-Herman, DE; Xu, L, 2011)		0.37
" Common adverse events were as follows: EQW, nausea (11."( Efficacy and safety of exenatide once weekly versus metformin, pioglitazone, and sitagliptin used as monotherapy in drug-naive patients with type 2 diabetes (DURATION-4): a 26-week double-blind study.
Boardman, MK; Chan, M; Cuddihy, RM; González, JG; Hanefeld, M; Kumar, A; Russell-Jones, D; Wolka, AM, 2012)		0.38
"The combination therapy with sitagliptin and low dosage sulphonylureas was safe and effective for glycaemic control."( Sitagliptin add-on to low dosage sulphonylureas: efficacy and safety of combination therapy on glycaemic control and insulin secretion capacity in type 2 diabetes.
Aono, M; Fukushima, T; Harashima, SI; Inagaki, N; Koizumi, T; Murata, Y; Ogura, M; Seike, M; Tanaka, D; Wang, Y, 2012)		0.38
" Changes in body weight and the rates of adverse events overall, hypoglycemia, and gastrointestinal adverse events were similar in the sitagliptin and placebo groups during the 54-week study."( Efficacy and safety of sitagliptin added to ongoing metformin and rosiglitazone combination therapy in a randomized placebo-controlled 54-week trial in patients with type 2 diabetes.
Amatruda, JM; Aschner, P; Chen, Y; Dobs, AS; Duran, L; Ferreira, JC; Goldstein, BJ; Golm, GT; Hill, JS; Horton, ES; Kaufman, KD; Langdon, RB; Umpierrez, GE; Williams-Herman, DE, 2013)		0.39
" The incidences of reported adverse events were generally similar between the treatment groups."( Efficacy and safety of sitagliptin added to ongoing metformin and pioglitazone combination therapy in a randomized, placebo-controlled, 26-week trial in patients with type 2 diabetes.
Fonseca, V; Goldstein, BJ; Golm, GT; Johnson-Levonas, AO; Kaufman, KD; Morgan, JD; Shentu, Y; Staels, B; Steinberg, H, )		0.13
" There was a lower incidence of symptomatic hypoglycemia adverse events (AEs) with sitagliptin versus glipizide (6."( Efficacy and safety of sitagliptin versus glipizide in patients with type 2 diabetes and moderate-to-severe chronic renal insufficiency.
Arjona Ferreira, JC; Barzilai, N; Goldstein, BJ; Golm, GT; Guo, H; Kaufman, KD; Marre, M; Sisk, CM, 2013)		0.39
" Patient-level data were used in this analysis of major adverse cardiovascular events (MACE) including ischaemic events and cardiovascular deaths."( Cardiovascular safety of sitagliptin in patients with type 2 diabetes mellitus: a pooled analysis.
Davies, MJ; Engel, SS; Goldstein, BJ; Golm, GT; Kaufman, KD; Shapiro, D, 2013)		0.39
" There was no increased risk of adverse effects with this dose of gemigliptin compared with sitagliptin 100 mg qd."( Efficacy and safety of the dipeptidyl peptidase-4 inhibitor gemigliptin compared with sitagliptin added to ongoing metformin therapy in patients with type 2 diabetes inadequately controlled with metformin alone.
Chung, CH; Jang, HC; Kim, JA; Kim, SW; Lee, WY; Min, KW; Nam-Goong, IS; Rhee, EJ; Shivane, VK; Sosale, AR, 2013)		0.39
" The most common adverse event was hypoglycemia, and the most common adverse event responsible for discontinuation was constipation."( Long-term efficacy and safety of sitagliptin in the treatment of Japanese Type 2 diabetes (ASSET-K1) to a target of HbA1c <7%.
Kanamori, A; Kubota, A; Maeda, H; Matsuba, I; Tanaka, Y; Terauchi, Y, 2013)		0.39
" The reduction of prescribed sulfonylurea dose in DPP-4 patients following the safety alert coincided with a decrease of adverse event reports."( Effects of a sitagliptin safety alert on prescription behaviour for oral antihyperglycaemic drugs: a propensity score-matched cohort study of prescription receipt data in Japan.
Kimura, H; Masuda, S; Sato, D; Sato, Y, 2013)		0.39
" Overall adverse events (AEs) were similar in both groups."( Efficacy and safety of adding pioglitazone or sitagliptin to patients with type 2 diabetes insufficiently controlled with metformin and a sulfonylurea.
Chen, WC; Chien, KL; Leung, CH; Liu, SC; Wang, CH, )		0.13
"Results of this pilot indicate that treatment with sitagliptin alone or in combination with basal insulin is safe and effective for the management of hyperglycemia in general medicine and surgery patients with T2D."( Safety and efficacy of sitagliptin therapy for the inpatient management of general medicine and surgery patients with type 2 diabetes: a pilot, randomized, controlled study.
Farrokhi, F; Gianchandani, R; Jacobs, S; Lathkar-Pradhan, S; Newton, C; Pasquel, F; Peng, L; Reyes, D; Smiley, D; Umpierrez, GE; Wesorick, DH, 2013)		0.39
" Combination therapy was generally well tolerated; adverse events (AEs) of hypoglycaemia were reported with similar incidence (7."( Efficacy and safety of initial combination treatment with sitagliptin and pioglitazone--a factorial study.
Chou, MZ; Fonseca, VA; Goldstein, BJ; Golm, GT; Henry, RR; Kaufman, KD; Langdon, RB; Staels, B; Steinberg, H; Teng, R, 2014)		0.4
" Safety endpoints included hypoglycemia and any adverse events."( Efficacy and safety of sitagliptin as add-on therapy on glycemic control and blood glucose fluctuation in Japanese type 2 diabetes subjects ongoing with multiple daily insulin injections therapy.
Araki, E; Furukawa, N; Goto, R; Ichimori, S; Iwashita, S; Kawashima, J; Kondo, T; Maeda, T; Matsumura, T; Matsuo, T; Matsuo, Y; Motoshima, H; Nishida, K; Sekigami, T; Shimoda, S, 2013)		0.39
" Adverse events (AEs) were recorded throughout the study."( Efficacy and safety of canagliflozin compared with placebo and sitagliptin in patients with type 2 diabetes on background metformin monotherapy: a randomised trial.
Canovatchel, W; Davidson, J; Januszewicz, A; Lavalle-González, FJ; Meininger, G; Qiu, R; Tong, C, 2013)		0.39
" Adverse events (AEs) were recorded throughout the study."( Long-term efficacy and safety of canagliflozin monotherapy in patients with type 2 diabetes inadequately controlled with diet and exercise: findings from the 52-week CANTATA-M study.
Alba, M; Canovatchel, W; Cefalu, WT; Edwards, R; Jodar, E; Kim, KA; Meininger, G; Stenlöf, K; Tong, C, 2014)		0.4
" Adverse events (AEs) were reported in 63."( Long-term safety and efficacy of empagliflozin, sitagliptin, and metformin: an active-controlled, parallel-group, randomized, 78-week open-label extension study in patients with type 2 diabetes.
Berk, A; Broedl, UC; Ferrannini, E; Hach, T; Hantel, S; Pinnetti, S; Woerle, HJ, 2013)		0.39
" There are limited available oral drugs to treat hyperglycaemia in this population owing to reduced renal function, potential interactions with immunosuppressive drugs and adverse effects such as hypoglycaemic events that may increase the cardiovascular risk."( Short-term efficacy and safety of sitagliptin treatment in long-term stable renal recipients with new-onset diabetes after transplantation.
Åsberg, A; Hartmann, A; Jenssen, T; Strøm Halden, TA; Vik, K, 2014)		0.4
" No serious adverse events were observed."( Short-term efficacy and safety of sitagliptin treatment in long-term stable renal recipients with new-onset diabetes after transplantation.
Åsberg, A; Hartmann, A; Jenssen, T; Strøm Halden, TA; Vik, K, 2014)		0.4
" The short-term treatment was well tolerated, and sitagliptin seems safe in this population."( Short-term efficacy and safety of sitagliptin treatment in long-term stable renal recipients with new-onset diabetes after transplantation.
Åsberg, A; Hartmann, A; Jenssen, T; Strøm Halden, TA; Vik, K, 2014)		0.4
"In each study, investigators reported serious and non-serious adverse events that occurred during the study, and serious adverse events occurring within 14 days following the last dose of study drug."( Safety of sitagliptin in elderly patients with type 2 diabetes: a pooled analysis of 25 clinical studies.
Davies, MJ; Engel, SS; Goldstein, BJ; Golm, GT; Kaufman, KD; Round, EM, 2014)		0.4
"Summary measures of adverse events overall were similar between the sitagliptin and non-exposed (active comparator or placebo) groups, except for higher incidences of deaths and drug-related adverse events in the non-exposed group."( Safety of sitagliptin in elderly patients with type 2 diabetes: a pooled analysis of 25 clinical studies.
Davies, MJ; Engel, SS; Goldstein, BJ; Golm, GT; Kaufman, KD; Round, EM, 2014)		0.4
" Overall adverse event (AE) incidence over 52 weeks was 69."( Efficacy and safety of canagliflozin over 52 weeks in patients with type 2 diabetes on background metformin and pioglitazone.
Forst, T; Goldenberg, R; Guthrie, R; Meininger, G; Stein, P; Vijapurkar, U; Yee, J, 2014)		0.4
" So, Sitagliptin in combination with CSII therapy can be a new safe and effective therapy in patients with newly diagnosed type 2diabetes."( Safety and efficacy of sitagliptin in combination with transient continuous subcutaneous insulin infusion (CSII) therapy in patients with newly diagnosed type 2 diabetes.
Dong, S; Jia, J; Mao, C; Qian, W; Tang, B; Wang, D; Yang, L; Ye, J; Yu, S; Yuan, G; Zhang, C; Zhou, L; Zhu, T, 2014)		0.4
" Imeglimin was generally well tolerated, with a safety profile comparable to placebo and no related treatment-emergent adverse events."( The efficacy and safety of imeglimin as add-on therapy in patients with type 2 diabetes inadequately controlled with sitagliptin monotherapy.
Bailey, CJ; Diamant, M; Fouqueray, P; Inzucchi, SE; Lebovitz, HE; Pirags, V; Schernthaner, G, 2014)		0.4
"This review considers the pharmacokinetic profile, adverse effects and drug interactions of DPP-4 inhibitors."( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected].
Athyros, VG; Elisaf, MS; Filippatos, TD, 2014)		0.4
" However, DPP-4 inhibitors have certain differences in their pharmacokinetic properties that may be associated with different clinical effects and adverse event profiles."( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected].
Athyros, VG; Elisaf, MS; Filippatos, TD, 2014)		0.4
" Rates of serious adverse events in the albiglutide group were similar to comparison groups."( HARMONY 3: 104-week randomized, double-blind, placebo- and active-controlled trial assessing the efficacy and safety of albiglutide compared with placebo, sitagliptin, and glimepiride in patients with type 2 diabetes taking metformin.
Ahrén, B; Cirkel, DT; Feinglos, MN; Johnson, SL; Perry, C; Stewart, M; Yang, F, 2014)		0.4
"Sitagliptin for the treatment of NAFLD with type2 DM was safe and showed similar antidiabetic effects as reported for type 2 DM, suggesting that tight glycemic control would contribute to the improvement of NAFLD based from the findings of correlation between the changes of HbA1c and transaminases."( Efficacy and safety of sitagliptin for the treatment of nonalcoholic fatty liver disease with type 2 diabetes mellitus.
Aikata, H; Chayama, K; Fujino, H; Fukuhara, T; Hiramatsu, A; Honda, Y; Hyogo, H; Imamura, M; Kan, H; Kawakami, Y; Kawaoka, T; Miyaki, D; Naeshiro, N; Ochi, H; Tsuge, M, )		0.13
" Results of safety assessments were similar between groups, and most adverse events (AEs) were mild or moderate."( Efficacy and safety of the once-weekly GLP-1 receptor agonist albiglutide versus sitagliptin in patients with type 2 diabetes and renal impairment: a randomized phase III study.
Carr, MC; Handelsman, Y; Jones-Leone, A; Leiter, LA; Scott, R; Stewart, M; Yang, F, 2014)		0.4
"7% of patients (9/328) withdrew because of adverse events (AEs); the frequency of AEs was evenly distributed across groups."( Dose-ranging efficacy and safety study of ertugliflozin, a sodium-glucose co-transporter 2 inhibitor, in patients with type 2 diabetes on a background of metformin.
Amin, NB; Jain, SM; Lee, DS; Nucci, G; Rusnak, JM; Wang, X, 2015)		0.42
" Parameters assessed included the hemoglobin A1c (HbA1c), body weight, serum creatinine, and adverse events."( Two-year assessment of the efficacy and safety of sitagliptin in elderly patients with type 2 diabetes: Post hoc analysis of the ASSET-K study.
Amamiya, H; Aoyagi, S; Honda, S; Hoshino, K; Iemitsu, K; Ishikawa, M; Ito, S; Jin, Y; Kanamori, A; Kaneshige, H; Kaneshiro, M; Kawata, T; Kubota, A; Machimura, H; Maeda, H; Matoba, K; Matsuba, I; Minagawa, F; Minami, N; Miyairi, Y; Mokubo, A; Motomiya, T; Naka, Y; Obana, M; Sasai, N; Takai, M; Takeda, H; Takuma, T; Tanaka, Y; Terauchi, Y; Umezawa, S; Waseda, M, 2015)		0.42
"Comparison of glycemic control parameters, laboratory values, and adverse events revealed significant improvement of HbA1c, casual postprandial plasma glucose, and fasting plasma glucose in each age group with no change in body weight."( Two-year assessment of the efficacy and safety of sitagliptin in elderly patients with type 2 diabetes: Post hoc analysis of the ASSET-K study.
Amamiya, H; Aoyagi, S; Honda, S; Hoshino, K; Iemitsu, K; Ishikawa, M; Ito, S; Jin, Y; Kanamori, A; Kaneshige, H; Kaneshiro, M; Kawata, T; Kubota, A; Machimura, H; Maeda, H; Matoba, K; Matsuba, I; Minagawa, F; Minami, N; Miyairi, Y; Mokubo, A; Motomiya, T; Naka, Y; Obana, M; Sasai, N; Takai, M; Takeda, H; Takuma, T; Tanaka, Y; Terauchi, Y; Umezawa, S; Waseda, M, 2015)		0.42
" Safety was assessed based on adverse event (AE) reports."( Efficacy and safety of canagliflozin in patients with type 2 diabetes mellitus from Latin America.
Alba, M; Cerdas, S; Chacon, Mdel P; Eliaschewitz, FG; Lavalle-González, FJ; Tong, C, 2016)		0.43
" At Week 24, the incidence of adverse events (AEs) was numerically greater with sitagliptin than placebo, primarily because of a higher incidence of hypoglycemia."( A randomized clinical trial evaluating the safety and efficacy of sitagliptin added to the combination of sulfonylurea and metformin in patients with type 2 diabetes mellitus and inadequate glycemic control.
Engel, SS; Gantz, I; Goldstein, BJ; Golm, GT; Kaufman, KD; Moses, RG; O'neill, EA; Round, E; Shentu, Y, 2016)		0.43
" Adverse events (AEs) were reported in 76."( Safety, tolerability and effects on cardiometabolic risk factors of empagliflozin monotherapy in drug-naïve patients with type 2 diabetes: a double-blind extension of a Phase III randomized controlled trial.
Broedl, UC; Christiansen, AV; Kim, G; Merker, L; Roden, M; Roux, F; Salsali, A; Stella, P; Woerle, HJ, 2015)		0.42
" Patients in the placebo group had a similar risk for a major adverse cardiac event within 12 months of follow-up as compared to patients under GS."( Sitagliptin plus granulocyte colony-stimulating factor in patients suffering from acute myocardial infarction: A double-blind, randomized placebo-controlled trial of efficacy and safety (SITAGRAMI trial).
Adrion, C; Becker, A; Brenner, C; Franz, WM; Grabmaier, U; Hoffmann, E; Leber, A; Mansmann, U; Sohn, HY; Steinbeck, G; Theisen, D; Theiss, HD; von Ziegler, F, 2016)		0.43
" This meta-analysis revealed the use of dulaglutide as a monotherapy or an add-on to OAM and lispro appeared to be effective and safe for adults with T2DM."( Efficacy and safety of dulaglutide in patients with type 2 diabetes: a meta-analysis and systematic review.
Tong, N; Zhang, L; Zhang, M; Zhang, Y, 2016)		0.43
" The rate of adverse events was 86."( Clinical study of repaglinide efficacy and safety in type 2 diabetes mellitus patients with blood glucose levels inadequately controlled by sitagliptin.
Hanafusa, T; Hotta, N; Ioriya, K; Kageyama, S; Kaku, K; Kawamori, R, 2016)		0.43
"We tested the possible association between dipeptidyl peptidase-4 inhibitors (DPP-4-I) use and heart failure (HF) occurrence by assessing the publicly available US-FDA Adverse Event Reporting System (FAERS)."( Dipeptidyl peptidase-4 inhibitors and heart failure: Analysis of spontaneous reports submitted to the FDA Adverse Event Reporting System.
Antonazzo, IC; De Ponti, F; Koci, A; Marchesini, G; Poluzzi, E; Raschi, E, 2016)		0.43
"6 mmol/l (≥100 mg/dl); and no volume depletion-related adverse events (AEs) within 2 weeks before dose increase."( Efficacy and safety of titrated canagliflozin in patients with type 2 diabetes mellitus inadequately controlled on metformin and sitagliptin.
Aggarwal, N; Alba, M; Cao, A; Fung, A; Pfeifer, M; Rodbard, HW; Seufert, J, 2016)		0.43
" The incidences of gastrointestinal adverse events were generally higher in high-dose metformin groups than in the placebo group."( Randomized clinical trial of the safety and efficacy of sitagliptin and metformin co-administered to Chinese patients with type 2 diabetes mellitus.
Engel, SS; Golm, GT; Han, P; Ji, L; Jou, YM; Kaufman, KD; Liu, J; O'Neill, EA; Shankar, RR; Wang, X; Zheng, S, 2016)		0.43
" Safety assessments comprised weight gain from baseline and the incidence of adverse events (AEs)."( Efficacy and safety of sitagliptin/metformin fixed-dose combination compared with glimepiride in patients with type 2 diabetes: A multicenter randomized double-blind study.
Chung, SC; Kim, IJ; Kim, SS; Kim, YI; Lee, KJ; Lee, SJ; Lee, YS; Park, JH, 2017)		0.46
" The addition of sitagliptin was generally well tolerated, with a comparable incidence of adverse events and drug-related adverse events in both treatment groups."( Randomized trial assessing the safety and efficacy of sitagliptin in Chinese patients with type 2 diabetes mellitus inadequately controlled on sulfonylurea alone or combined with metformin.
Ba, J; Engel, SS; Han, P; Hanson, ME; Mo, Z; Pan, C; Shankar, RR; Wu, F; Xu, L; Yuan, G, 2017)		0.46
" A higher incidence of serious adverse events was observed in the sitagliptin group (5."( A randomized clinical trial of the safety and efficacy of sitagliptin in patients with type 2 diabetes mellitus inadequately controlled by acarbose alone.
Engel, SS; Fujita, KP; Kaufman, KD; Liu, X; Ma, J; Ning, G; O'Neill, EA; Shankar, RR; Wang, W; Wu, F; Xu, L; Zheng, S, 2017)		0.46
"71]), rates of acute pancreatitis and pancreatic cancer, or serious adverse events."( Assessing the Safety of Sitagliptin in Older Participants in the Trial Evaluating Cardiovascular Outcomes with Sitagliptin (TECOS).
Bethel, MA; Engel, SS; Green, JB; Holman, RR; Huang, Z; Josse, RG; Kaufman, KD; McGuire, DK; Peterson, ED; Standl, E; Suryawanshi, S; Van de Werf, F, 2017)		0.46
" In general, both treatments were well tolerated, with incidences and types of adverse events comparable between the two groups."( Efficacy and safety of adding evogliptin versus sitagliptin for metformin-treated patients with type 2 diabetes: A 24-week randomized, controlled trial with open label extension.
Chung, CH; Han, KA; Hong, SM; Hwang, DM; Lee, CB; Mok, JO; Park, CY; Park, KS; Park, SW; Yoon, KH, 2017)		0.46
" There were no notable differences in adverse events and the incidence of symptomatic hypoglycaemia was low and similar in the groups."( Randomized clinical trial comparing the efficacy and safety of treatment with the once-weekly dipeptidyl peptidase-4 (DPP-4) inhibitor omarigliptin or the once-daily DPP-4 inhibitor sitagliptin in patients with type 2 diabetes inadequately controlled on m
Andryuk, PJ; Engel, SS; Gantz, I; Goldenberg, R; Kaufman, KD; Lai, E; O'Neill, EA; Suryawanshi, S; Wang, YN, 2017)		0.46
" The most common adverse events with exenatide QWS-AI were gastrointestinal events and injection-site reactions."( Efficacy and safety of autoinjected exenatide once-weekly suspension versus sitagliptin or placebo with metformin in patients with type 2 diabetes: The DURATION-NEO-2 randomized clinical study.
Gadde, KM; Hardy, E; Iqbal, N; Öhman, P; Vetter, ML, 2017)		0.46
" The incidences of adverse events (AEs) were 29."( Efficacy and safety of metformin and sitagliptin based triple antihyperglycemic therapy (STRATEGY): a multicenter, randomized, controlled, non-inferiority clinical trial.
Bi, Y; Engel, SS; Ji, L; Ji, Q; Jia, W; Lu, J; Mao, A; Mu, Y; Ran, X; Weng, J; Xu, W; Yang, W; Yao, B; Zeng, L; Zhao, B; Zhao, J; Zhou, Z; Zhu, D, 2017)		0.46
" Safety endpoints were adverse events including hypoglycaemia."( Efficacy and safety of sitagliptin as compared with glimepiride in Japanese patients with type 2 diabetes mellitus aged ≥ 60 years (START-J trial).
Ishida, H; Kitaoka, M; Ohsugi, M; Satoh, J; Seino, Y; Shihara, N; Terauchi, Y; Yabe, D; Yamada, Y, 2017)		0.46
" Incidences of serious adverse events, malignancy, bone fracture, severe hypoglycaemia and most categories of diabetes complications were higher in the CKD cohort compared with those without CKD."( Safety of sitagliptin in patients with type 2 diabetes and chronic kidney disease: outcomes from TECOS.
Cornel, JH; Engel, SS; Holman, RR; Jakuboniene, N; Josse, RG; Peterson, ED; Riefflin, A; Stevens, SR; Suryawanshi, S; Tankova, T; Wainstein, J, 2017)		0.46
"Participants in TECOS with CKD had higher incidences of serious adverse events and diabetes complications than those without CKD."( Safety of sitagliptin in patients with type 2 diabetes and chronic kidney disease: outcomes from TECOS.
Cornel, JH; Engel, SS; Holman, RR; Jakuboniene, N; Josse, RG; Peterson, ED; Riefflin, A; Stevens, SR; Suryawanshi, S; Tankova, T; Wainstein, J, 2017)		0.46
" Over the 24-week double-blind period, there were no clinically meaningful differences in the incidence rates of adverse events among the treatment groups."( A randomized, placebo- and sitagliptin-controlled trial of the safety and efficacy of omarigliptin, a once-weekly dipeptidyl peptidase-4 inhibitor, in Japanese patients with type 2 diabetes.
Engel, SS; Gantz, I; Ito, Y; Kaufman, KD; Lai, E; O'Neill, EA; Okamoto, T; Okuyama, K, 2017)		0.46
" The primary endpoint was number of treatment-emergent adverse events (TEAEs) after 30 weeks."( Safety and efficacy of semaglutide once weekly vs sitagliptin once daily, both as monotherapy in Japanese people with type 2 diabetes.
Abe, N; Kaneko, S; Nishida, T; Osonoi, T; Seino, Y; Terauchi, Y; Yabe, D; Zacho, J, 2018)		0.48
"0 mg groups were attributable to adverse events (AEs)."( Safety and efficacy of semaglutide once weekly vs sitagliptin once daily, both as monotherapy in Japanese people with type 2 diabetes.
Abe, N; Kaneko, S; Nishida, T; Osonoi, T; Seino, Y; Terauchi, Y; Yabe, D; Zacho, J, 2018)		0.48
" Meanwhile, the adverse reactions such as gastrointestinal problems were common in the liraglutide treatment group."( Efficacy and safety of liraglutide versus sitagliptin both in combination with metformin in patients with type 2 diabetes: A systematic review and meta-analysis.
Jiang, D; Li, M; Wang, Y; Yang, Y; Ying, M; Zhao, R, 2017)		0.46
" There were no adverse events to be related to the drugs."( The renoprotective effect and safety of a DPP-4 inhibitor, sitagliptin, at a small dose in type 2 diabetic patients with a renal dysfunction when changed from other DPP-4 inhibitors: REAL trial.
Hasegawa, H; Kaneko, K; Kanozawa, K; Katayama, S; Kono, R; Nakamura, S; Noguchi, Y; Ogawa, T; Sato, S; Sugahara, S; Yamamoto, H, 2018)		0.48
" A Liver Safety Evaluation Committee consisting of hepatologists blinded to treatment assignments evaluated hepatic adverse events (AEs) and serious AEs (SAEs) for causal relationship to study drug."( Liver Safety of Fasiglifam (TAK-875) in Patients with Type 2 Diabetes: Review of the Global Clinical Trial Experience.
Marcinak, JF; Munsaka, MS; Ohira, T; Smith, N; Watkins, PB, 2018)		0.48
" There were no significant treatment-emergent adverse events leading to discontinuation during the study."( Efficacy and safety of the G protein-coupled receptor 119 agonist DS-8500a in Japanese type 2 diabetes mellitus patients with inadequate glycemic control on sitagliptin: A phase 2 randomized placebo-controlled study.
Nakatsuka, Y; Shiosakai, K; Taguchi, T; Terauchi, Y; Washio, T; Watada, H; Yamada, Y, 2018)		0.48
" As such, we assessed disproportionate reporting of major adverse cardiac events (MACE) among reports for DPP-4i submitted to the FDA Adverse Event Reporting System (FAERS) from 2006 to 2015."( Cardiovascular safety signals with dipeptidyl peptidase-4 inhibitors: A disproportionality analysis among high-risk patients.
Alexander, GC; Baksh, SN; McAdams-DeMarco, M; Segal, JB, 2018)		0.48
"3 million adverse event reports, 13."( Cardiovascular safety signals with dipeptidyl peptidase-4 inhibitors: A disproportionality analysis among high-risk patients.
Alexander, GC; Baksh, SN; McAdams-DeMarco, M; Segal, JB, 2018)		0.48
" Adverse event rates were similar between groups (ipragliflozin: 51."( Efficacy and safety of ipragliflozin as an add-on therapy to sitagliptin and metformin in Korean patients with inadequately controlled type 2 diabetes mellitus: A randomized controlled trial.
Baik, S; Cha, BS; Chon, S; Chung, CH; Han, KA; Jung, CH; Kim, DS; Lee, IK; Lee, KW; Lee, MK; Lim, S; Park, KS; Park, S; Sakatani, T; Yoon, KH, 2018)		0.48
"The proposed HbA1c-based hospital discharge algorithm using a combination of sitagliptin-metformin was safe and significantly improved glycemic control after hospital discharge in general medicine and surgery patients with T2D."( THE EFFICACY AND SAFETY OF CO-ADMINISTRATION OF SITAGLIPTIN WITH METFORMIN IN PATIENTS WITH TYPE 2 DIABETES AT HOSPITAL DISCHARGE.
Anzola, I; Dungan, KM; Gianchandani, RY; Gomez, P; Hodish, I; Iyengar, J; Lathkar-Pradhan, S; Pasquel, FJ; Rubin, DJ; Umpierrez, GE; Vellanki, P; Wang, H, 2018)		0.48
" Adverse events were generally similar between the treatment groups."( Efficacy and safety of sitagliptin added to treatment of patients with type 2 diabetes inadequately controlled with premixed insulin.
Chen, G; Engel, SS; Lin, J; Liu, S; O'Neill, EA; Shankar, RR; Tu, Y; Yu, M; Zhang, R; Zhang, Y, 2019)		0.51
" Adverse events overall and changes from baseline in body weight were similar between the two treatment groups."( Double-blind, randomized clinical trial comparing the efficacy and safety of continuing or discontinuing the dipeptidyl peptidase-4 inhibitor sitagliptin when initiating insulin glargine therapy in patients with type 2 diabetes: The CompoSIT-I Study.
Darmiento, C; Duran-García, S; Engel, SS; Gantz, I; Golm, GT; Kaufman, KD; Lam, RLH; O'Neill, EA; Roussel, R; Shah, S; Shankar, RR; Zhang, Y, 2019)		0.51
"Cisplatin has been extensively used as a chemotherapeutic agent since around 40 years, though its usage is limited due to severe adverse effects like neurotoxicity that might be because of oxidative stress."( Neuroprotective influence of sitagliptin against cisplatin-induced neurotoxicity, biochemical and behavioral alterations in Wistar rats.
Li, Y; Mishra, A; Sah, SK; Singh, Y; Zheng, M, 2019)		0.51
" DAPA plus SAXA was generally well tolerated and the incidence of adverse events was similar in both treatment arms."( Sustained 52-week efficacy and safety of triple therapy with dapagliflozin plus saxagliptin versus dual therapy with sitagliptin added to metformin in patients with uncontrolled type 2 diabetes.
Del Prato, S; Garcia-Sanchez, R; Handelsman, Y; Iqbal, N; Johnsson, E; Kurlyandskaya, R; Mathieu, C; Rosenstock, J, 2019)		0.51
" In comparison to systemic application, metformin displayed the most adverse effects in vitro in nearly all analyses, interestingly at serum equivalent concentrations."( Side effects of frequently used oral antidiabetics on wound healing in vitro.
Bachmann, HS; Besser, M; Koester, V; Severing, AL; Stuermer, EK; Terberger, N, 2019)		0.51
" There were no notable differences between groups with regard to adverse events overall, hypoglycaemia events, changes in body weight or other safety variables."( Double-blind, randomized clinical trial assessing the efficacy and safety of early initiation of sitagliptin during metformin uptitration in the treatment of patients with type 2 diabetes: The CompoSIT-M study.
Amorin, G; Crutchlow, MF; Engel, SS; Frias, JP; Iredale, C; Kaufman, KD; Lam, RLH; Makimura, H; Ntabadde, C; O'Neill, EA; Zimmer, Z, 2019)		0.51
" Both gliptins were well-tolerated with no difference in the number of adverse events."( A ProspectIve, OpeN-Label, Randomized Study Comparing EffIcacy and Safety of Teneligliptin VErsus Sitagliptin in Indian Patients with Inadequately Controlled Type 2 Diabetes Mellitus: INSITES Study.
Kasthuri, S; Mohan, V; Poongothai, S; Ramu, M, 2019)		0.51
" Both gliptins were found to be safe and well-tolerated in Indian patients with T2DM."( A ProspectIve, OpeN-Label, Randomized Study Comparing EffIcacy and Safety of Teneligliptin VErsus Sitagliptin in Indian Patients with Inadequately Controlled Type 2 Diabetes Mellitus: INSITES Study.
Kasthuri, S; Mohan, V; Poongothai, S; Ramu, M, 2019)		0.51
" The existing side effect prediction methods mainly focus on the chemical and biological properties of drugs."( Prediction of Side Effects Using Comprehensive Similarity Measures.
Kim, MH; Lee, T; Seo, S; Yoon, Y, 2020)		0.56
" The efficacy end-point was change in glycated hemoglobin (HbA1c) in each stage, and the safety end-point was adverse events with a focus on hypoglycemia."( Efficacy and safety of metformin and sitagliptin-based dual and triple therapy in elderly Chinese patients with type 2 diabetes: Subgroup analysis of STRATEGY study.
Chen, G; Engel, SS; Ji, Q; Liu, S; Liu, X; Wang, L; Weng, J; Xing, Y; Xu, W; Yao, B; Zeng, L; Zhang, R; Zhang, Y, 2020)		0.56
" Although sitagliptin is safe and well tolerated in NAFLD patients, it exerts no beneficial effects on liver transaminase and liver fat content in these patients."( Effects and Safety of Sitagliptin in Non-Alcoholic Fatty Liver Disease: A Systematic Review and Meta-Analysis.
Cai, T; Dong, J; Gao, P; Guo, C; Liao, L; Yao, J; Zhang, Y; Zhao, J, 2020)		0.56
" In Trial 843, the incidences of adverse events (AEs) overall and prespecified AEs of clinical interest (symptomatic hypoglycaemia, urinary tract infection, genital infection, hypovolaemia, and polyuria/pollakiuria) were similar between groups."( Efficacy and safety of ipragliflozin in Japanese patients with type 2 diabetes and inadequate glycaemic control on sitagliptin.
Engel, SS; Kadowaki, T; Kaku, K; Kaufman, KD; O'Neill, EA; Okamoto, T; Sato, A; Seino, Y; Shirakawa, M, 2021)		0.62
" Patients on metformin or sitagliptin were contacted by telephone for recording of possible adverse events and to support continuation of treatment at 2 weeks, 6 weeks and 3 months after inclusion."( Safety, feasibility and efficacy of metformin and sitagliptin in patients with a TIA or minor ischaemic stroke and impaired glucose tolerance.
Brouwers, PJAM; den Hertog, H; Dippel, DWJ; Koudstaal, P; Lingsma, H; Mulder, LJMM; Osei, E; Zandbergen, A, 2021)		0.62
" There were no notable between-group differences in the adverse event profiles through Week 54."( A randomized clinical trial of the efficacy and safety of sitagliptin as initial oral therapy in youth with type 2 diabetes.
Deeb, A; Engel, SS; Garcia, R; Golm, GT; Jalaludin, MY; Kaufman, KD; Lam, RLH; Newfield, RS; Rosario, CA; Saha, CK; Samoilova, Y; Scherer, LW; Shankar, RR; Shehadeh, N; Zeitler, P; Zhang, Y; Zilli, M, 2022)		0.72
" The outcome measures included parameters of glycemic control, β-cell function, body mass index and adverse events."( Efficacy and safety of sitagliptin and insulin for latent autoimmune diabetes in adults: A systematic review and meta-analysis.
Cai, Y; Lian, Y; Lin, T; Liu, C; Liu, M; Tang, L, 2022)		0.72
" The adverse events were comparable to placebo; however, gastrointestinal adverse events were highly recorded in tirzepatide, oral and SC semaglutide groups."( Semaglutide for the treatment of type 2 Diabetes Mellitus: A systematic review and network meta-analysis of safety and efficacy outcomes.
Abdel-Aziz, W; Aladwan, H; Ali, AS; Elkady, S; Elmegeed, AA; Elshahawy, IM; Elshanbary, AA; Gbreel, MI; Hamdallah, A; Hasabo, EA; Helmy, SK; Nourelden, AZ; Rabie, S; Ragab, KM; Sayed, AK; Zaazouee, MS, 2022)		0.72
" We obtained data from the US Food and Drug Administration Adverse Event Reporting System and performed a disproportionality analysis, using the reporting odds ratio (ROR) and information component (IC) for signal detection in patients aged ≥ 40 years, stratified by age group and sex."( Pharmacovigilance study of the association between dipeptidyl peptidase-4 inhibitors and angioedema using the FDA Adverse Event Reporting System (FAERS).
Hori, Y; Ohyama, K; Shindo, J; Takahashi, T; Takeuchi, H, 2022)		0.72
" There were no significant differences between treatments in the incidence of adverse events, except that liraglutide+metformin had significant adverse effect such as abdominal pain."( Comparative efficacy and safety of glucose-lowering drugs in children and adolescents with type 2 diabetes: A systematic review and network meta-analysis.
Feng, Y; Ge, Y; He, Y; Hou, L; Huo, M; Ji, Y; Li, H; Liu, X; Liu, Y; Luo, Q; Qian, F; Wang, J; Wei, Y; Wu, S; Wu, Y; Xue, F; Yu, Y, 2022)		0.72
" With a vague consensus, the advantageous and non-inferior effects of evogliptin relative to other DPP-4i drugs were recently demonstrated on hemoglobin A1c (HbA1c) levels and overall adverse events in T2DM patients."( The efficacy and safety of evogliptin for type 2 diabetes mellitus: A systematic review and meta-analysis.
Pan, W; Peng, L; Tang, Q, 2022)		0.72
" Data about HbA1c levels and the adverse events of T2DM patients were collected and analyzed."( The efficacy and safety of evogliptin for type 2 diabetes mellitus: A systematic review and meta-analysis.
Pan, W; Peng, L; Tang, Q, 2022)		0.72
"The study provides preliminary evidence regarding the similarity in the efficacy of evogliptin compared to other DPP-4i drugs, including sitagliptin and linagliptin, for managing HbA1c levels and adverse events."( The efficacy and safety of evogliptin for type 2 diabetes mellitus: A systematic review and meta-analysis.
Pan, W; Peng, L; Tang, Q, 2022)		0.72
" Sodium glucose co-transporter -2 inhibitors (SGLT2i) are considered safe with a low risk of hypoglycemia."( Efficacy and safety of combination of empagliflozin and metformin with combination of sitagliptin and metformin during Ramadan: an observational study.
Aamir, AH; Ahmed, I; Asghar, A; Ghaffar, T; Ishtiaq, O; Khan, S; Kumar, S; Masood, F; Raja, UY; Randhawa, FA; Raza, A; Rehman, T; Sherin, A; Wahab, MU, 2022)		0.72
"SGLT-2 inhibitors combined with metformin for patients with diabetes during Ramadan fasting is as effective, safe and well tolerated as DPP4 combined with metformin."( Efficacy and safety of combination of empagliflozin and metformin with combination of sitagliptin and metformin during Ramadan: an observational study.
Aamir, AH; Ahmed, I; Asghar, A; Ghaffar, T; Ishtiaq, O; Khan, S; Kumar, S; Masood, F; Raja, UY; Randhawa, FA; Raza, A; Rehman, T; Sherin, A; Wahab, MU, 2022)		0.72
" There were no differences in the incidence of adverse effects, except for cystatin C elevation and platelet count reduction in sitagliptin group."( Efficacy and safety of sitagliptin treatment in older adults with moderately controlled type 2 diabetes: the STREAM study.
Harada, T; Nagao, M; Oikawa, S; Sakuma, I; Sasaki, J; Sugihara, H; Tanimura-Inagaki, K, 2023)		0.91
" We examined the adverse events that occurred during the administration of a DPP-4 inhibitor in patients with diabetes using FDA Adverse Event Reporting System (FAERS) data."( Comparison of Adverse Events Occurred During Administration of Dipeptidyl Peptidase-4 Inhibitor in Patients with Diabetes Using FDA Adverse Event Reporting System.
Ogura, T; Shiraishi, C, 2023)		0.91
"000 of all occurrences of adverse events, these results may be used for drug selection when the patient has adverse events that need to be avoided."( Comparison of Adverse Events Occurred During Administration of Dipeptidyl Peptidase-4 Inhibitor in Patients with Diabetes Using FDA Adverse Event Reporting System.
Ogura, T; Shiraishi, C, 2023)		0.91
" However, CYP cerebral neurotoxicity is a worrisome side effect for clinicians and patients."( Antidiabetic drug sitagliptin blocks cyclophosphamide cerebral neurotoxicity by activating Nrf2 and suppressing redox cycle imbalance, inflammatory iNOS/NO/NF-κB response and caspase-3/Bax activation in rats.
Asogwa, NT; Ezea, SC; Famurewa, AC, 2023)		0.91
" Regarding secondary outcomes, there was an elevated risk of total adverse events and premature treatment discontinuation with Semaglutide."( Comparative efficacy and safety profile of once-weekly Semaglutide versus once-daily Sitagliptin as an add-on to metformin in patients with type 2 diabetes: a systematic review and meta-analysis.
Ahmed, M; Butt, TS; Ganesan, S; Khatri, M; Kumar, S; Madhurita, F; Nageeta, F; Patel, T; Sohail, R; Varrassi, G; Zafar, M; Zafar, W; Zaman, MU, 2023)		0.91

Pharmacokinetics

ExcerptReferenceRelevance
"Sitagliptin was well absorbed (approximately 80% excreted unchanged in the urine) with an apparent terminal half-life ranging from 8 to 14 hours."( Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses.
Bergman, A; Davies, MJ; De Smet, M; Gottesdiener, KM; Herman, GA; Hilliard, D; Musson, D; Ramael, S; Snyder, K; Stevens, C; Tanaka, W; Tanen, M; Van Dyck, K; Wagner, JA; Wang, AQ; Winchell, G; Yi, B; Zeng, W, 2005)		0.33
" Sitagliptin possesses pharmacokinetic and pharmacodynamic characteristics that support a once-daily dosing regimen."( Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses.
Bergman, A; Davies, MJ; De Smet, M; Gottesdiener, KM; Herman, GA; Hilliard, D; Musson, D; Ramael, S; Snyder, K; Stevens, C; Tanaka, W; Tanen, M; Van Dyck, K; Wagner, JA; Wang, AQ; Winchell, G; Yi, B; Zeng, W, 2005)		0.33
"The aim of this study was to assess the pharmacokinetic and pharmacodynamic (PK/PD) properties and tolerability of multiple oral once-daily or twice-daily doses of sitagliptin."( Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: a double-blind, randomized, placebo-controlled study in healthy male volunteers.
Bergman, AJ; Chen, L; Davies, MJ; De Smet, M; Herman, GA; Hilliard, D; Laethem, M; Ramael, S; Snyder, K; Stevens, C; Tanaka, W; Tanen, M; Wagner, JA; Wang, AQ; Winchell, G; Yi, B; Zeng, W; Zhou, Y, 2006)		0.33
" This multicenter, randomized, double-blind, placebo-controlled study examined the pharmacokinetic and pharmacodynamic effects of sitagliptin in obese subjects."( Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects.
Bergman, A; Blum, R; Chen, L; Dilzer, S; Herman, GA; Hilliard, D; Lasseter, K; Liu, F; Meehan, AG; Snyder, K; Stevens, C; Tanaka, W; Tanen, M; Wagner, JA; Wang, AQ; Zeng, W, 2006)		0.33
"As part of the clinical development of sitagliptin, a dipeptidyl peptidase-4 inhibitor, for the treatment of type 2 diabetes, the potential for pharmacokinetic interactions with other antihyperglycemic agents used in managing patients with type 2 diabetes are being carefully evaluated."( Tolerability and pharmacokinetics of metformin and the dipeptidyl peptidase-4 inhibitor sitagliptin when co-administered in patients with type 2 diabetes.
Bergman, A; Herman, GA; Kipnes, M; Yi, B, 2006)		0.33
" Following dosing on Day 7 of each treatment period, these pharmacokinetic parameters were determined for plasma sitagliptin and metformin: area under the plasma concentrations-time curve over the dosing interval (AUC(0-12h)), maximum observed plasma concentrations (C(max)), and time of occurrence of maximum observed plasma concentrations (T(max))."( Tolerability and pharmacokinetics of metformin and the dipeptidyl peptidase-4 inhibitor sitagliptin when co-administered in patients with type 2 diabetes.
Bergman, A; Herman, GA; Kipnes, M; Yi, B, 2006)		0.33
"The mean AUC(0-infinity) and Cmax for sitagliptin were numerically, but not significantly (p>0."( Effect of moderate hepatic insufficiency on the pharmacokinetics of sitagliptin.
Bergman, AJ; Davies, MJ; Dilzer, SC; Herman, GA; Lasseter, KC; Luo, WL; Migoya, EM; Stevens, CH; Wagner, JA, 2009)		0.35
" PK/pharmacodynamics characteristics, that is, sufficiently prolonged half-life and sustained DPP-4 enzyme inactivation, generally allow one single oral administration per day for the management of T2DM; the only exception is vildagliptin for which a twice-daily administration is recommended because of a shorter half-life."( Pharmacokinetics of dipeptidylpeptidase-4 inhibitors.
Scheen, AJ, 2010)		0.36
"An extensive literature search was performed to analyze the potential pharmacokinetic (PK) and pharmacodynamic (PD) interactions between metformin (first-line drug for the management of type 2 diabetes) and sitagliptin (first commercialized DPP IV inhibitor)."( Pharmacokinetic and pharmacodynamic evaluation of sitagliptin plus metformin.
Scheen, AJ, 2010)		0.36
" The current studies assessed the potential for pharmacokinetic (PK) interaction between dapagliflozin and pioglitazone, metformin, glimepiride or sitagliptin in healthy subjects following single-dose administration."( Lack of pharmacokinetic interaction between dapagliflozin, a novel sodium-glucose transporter 2 inhibitor, and metformin, pioglitazone, glimepiride or sitagliptin in healthy subjects.
Boulton, DW; Griffen, SC; Kasichayanula, S; LaCreta, FP; Li, T; Liu, X; Pfister, M; Shyu, WC; Zhang, W, 2011)		0.37
" The present aim was to evaluate pharmacokinetic (PK), pharmacodynamic (PD) and safety characteristics of sitagliptin following single doses in healthy, young Japanese males."( Evaluation of pharmacokinetic parameters and dipeptidyl peptidase-4 inhibition following single doses of sitagliptin in healthy, young Japanese males.
Bergman, AJ; Chen, L; Davies, MJ; Gottesdiener, KM; Herman, GA; Langdon, RB; Larson, PJ; Mistry, GC; Ruckle, JL; Snyder, K; Wagner, JA; Wang, AQ; Yi, B; Zeng, W, 2011)		0.37
" The mean apparent terminal half-life for plasma sitagliptin was 9-14h, with the half-life slightly decreasing as the dose increased."( Evaluation of pharmacokinetic parameters and dipeptidyl peptidase-4 inhibition following single doses of sitagliptin in healthy, young Japanese males.
Bergman, AJ; Chen, L; Davies, MJ; Gottesdiener, KM; Herman, GA; Langdon, RB; Larson, PJ; Mistry, GC; Ruckle, JL; Snyder, K; Wagner, JA; Wang, AQ; Yi, B; Zeng, W, 2011)		0.37
" The interindividual differences in the pharmacokinetic parameters of sitagliptin were found to be within acceptable limits (coefficient of variation <20%)."( Pharmacokinetic drug interaction between gemfibrozil and sitagliptin in healthy Indian male volunteers.
B, S; Dubala, A; K P, A; K, E; Kucherlapati, VS; M, D; Meda, VS; P R, AV, 2012)		0.38
" The developed assay was successfully applied to a pharmacokinetic study in human volunteers."( Simultaneous determination of sitagliptin and simvastatin in human plasma by LC-MS/MS and its application to a human pharmacokinetic study.
Burugula, L; Kandhagatla, R; Lodagala, DS; Makula, A; Mullangi, R; Pilli, NR, 2013)		0.39
" Saliva and plasma samples were collected for 3-5 half-life values of sitagliptin, cinacalcet, metformin, montelukast, tolterodine, hydrochlorothiazide (HCT), lornoxicam, azithromycin, diacerhein, rosuvastatin, cloxacillin, losartan and tamsulosin after oral dosing."( Saliva versus plasma pharmacokinetics: theory and application of a salivary excretion classification system.
Arafat, T; Idkaidek, N, 2012)		0.38
"The objectives of this study were to determine if ABCB1 polymorphisms are associated with interindividual variability in sitagliptin pharmacokinetics and if atorvastatin alters the pharmacokinetic disposition of sitagliptin in healthy volunteers."( Effect of ABCB1 polymorphisms and atorvastatin on sitagliptin pharmacokinetics in healthy volunteers.
Aquilante, CL; Kosmiski, LA; Predhomme, JA; Sidhom, MS; Wempe, MF, 2013)		0.39
" A 24-h pharmacokinetic study followed each sitagliptin dose, and the study phases were separated by a 14-day washout period."( Effect of ABCB1 polymorphisms and atorvastatin on sitagliptin pharmacokinetics in healthy volunteers.
Aquilante, CL; Kosmiski, LA; Predhomme, JA; Sidhom, MS; Wempe, MF, 2013)		0.39
"Sitagliptin pharmacokinetic parameters did not differ significantly between ABCB1 CGC/CGC, CGC/TTT, and TTT/TTT diplotype groups during the monotherapy phase."( Effect of ABCB1 polymorphisms and atorvastatin on sitagliptin pharmacokinetics in healthy volunteers.
Aquilante, CL; Kosmiski, LA; Predhomme, JA; Sidhom, MS; Wempe, MF, 2013)		0.39
" Colesevelam (3750mg once daily) was dosed throughout the pharmacokinetic sampling period."( Lack of effect of colesevelam HCl on the single-dose pharmacokinetics of aspirin, atenolol, enalapril, phenytoin, rosiglitazone, and sitagliptin.
He, L; Lee, J; Mendell-Harary, J; Tao, B; Walker, J; Wickremasingha, P; Wight, D, 2014)		0.4
"For all six test drugs, 90% CIs for geometric least-squares mean ratios of AUC and Cmax for the measured analytes were within specified limits, indicating no interaction between the test drug and colesevelam."( Lack of effect of colesevelam HCl on the single-dose pharmacokinetics of aspirin, atenolol, enalapril, phenytoin, rosiglitazone, and sitagliptin.
He, L; Lee, J; Mendell-Harary, J; Tao, B; Walker, J; Wickremasingha, P; Wight, D, 2014)		0.4
" Although the phenytoin study indicated no pharmacokinetic interaction, phenytoin should continue to be taken ≥4h before colesevelam in accordance with current prescribing information."( Lack of effect of colesevelam HCl on the single-dose pharmacokinetics of aspirin, atenolol, enalapril, phenytoin, rosiglitazone, and sitagliptin.
He, L; Lee, J; Mendell-Harary, J; Tao, B; Walker, J; Wickremasingha, P; Wight, D, 2014)		0.4
"This review considers the pharmacokinetic profile, adverse effects and drug interactions of DPP-4 inhibitors."( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected].
Athyros, VG; Elisaf, MS; Filippatos, TD, 2014)		0.4
" However, DPP-4 inhibitors have certain differences in their pharmacokinetic properties that may be associated with different clinical effects and adverse event profiles."( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected].
Athyros, VG; Elisaf, MS; Filippatos, TD, 2014)		0.4
"The availability of intravenous and oral pharmacokinetic data in animals enabled the allometry scaling of 6 DPP-IV inhibitors."( Retrospective and Prospective Human Intravenous and Oral Pharmacokinetic Projection of Dipeptidyl peptidase-IV Inhibitors Using Simple Allometric Principles - Case Studies of ABT-279, ABT-341, Alogliptin, Carmegliptin, Sitagliptin and Vildagliptin.
Bhamidipati, RK; Gilibili, RR; Mullangi, R; Srinivas, NR, 2015)		0.42
" This clinical pharmacology study was designed to investigate the potential glucose-lowering effect or pharmacodynamic (PD), pharmacokinetic (PK), and safety/tolerability interactions between piragliatin and glyburide in T2D patients already taking glyburide but not adequately controlled."( Pharmacokinetic and Pharmacodynamic Drug Interaction Study of Piragliatin, a Glucokinase Activator, and Glyburide, a Sulfonylurea, in Type 2 Diabetic Patients.
Georgy, A; Liang, Z; Zhai, S; Zhi, J, 2016)		0.43
"To develop a population pharmacodynamic (PPD) model describing the time course for the hemoglobin A1c (HbA1c)-lowering effects of adding treatment of DPP-4 inhibitors and to assess the efficacy of combination therapy in type 2 diabetes mellitus patients based on electronic medical records."( Population pharmacodynamic analysis of hemoglobin A1c-lowering effects by adding treatment of DPP-4 inhibitors (sitagliptin) in type 2 diabetes mellitus patients based on electronic medical records.
Ezaki, M; Fukae, M; Hirakawa, M; Hirota, T; Ieiri, I; Kakara, M; Matsubayashi, S; Nomura, H, )		0.13
"Preclinical pharmacokinetic studies are an essential part of modern drug development."( Using miniature MS system with automatic blood sampler for preclinical pharmacokinetics study.
Bateman, KP; Helmy, R; Liu, Y; Ouyang, Z; Pu, F; Zhang, W, 2017)		0.46
" The miniature MS system was used to obtain drug concentrations, which were subsequently used to calculate the pharmacokinetic parameters."( Using miniature MS system with automatic blood sampler for preclinical pharmacokinetics study.
Bateman, KP; Helmy, R; Liu, Y; Ouyang, Z; Pu, F; Zhang, W, 2017)		0.46
" Pharmacokinetic parameters were determined from blood and urine; levels of all compounds were evaluated using liquid chromatography with tandem mass spectrometry."( Imeglimin Does Not Induce Clinically Relevant Pharmacokinetic Interactions When Combined with Either Metformin or Sitagliptin in Healthy Subjects.
Bolze, S; Fouqueray, P; Perrimond-Dauchy, S, 2020)		0.56
" The objective of this study was to investigate a possible pharmacokinetic interaction between lobeglitazone and sitagliptin after multiple oral administrations in healthy Korean men."( An Assessment of Pharmacokinetic Interaction Between Lobeglitazone and Sitagliptin After Multiple Oral Administrations in Healthy Men.
Kim, MG; Moon, SJ; Yu, KS, 2020)		0.56
"Nineteen men from study 1 and 17 from study 2 completed the pharmacokinetic sampling and were included in the analyses."( An Assessment of Pharmacokinetic Interaction Between Lobeglitazone and Sitagliptin After Multiple Oral Administrations in Healthy Men.
Kim, MG; Moon, SJ; Yu, KS, 2020)		0.56
" This method has been successfully applied to the pharmacokinetic study of sitagliptin after single intravenous administration in rats."( High-throughput bioanalysis of sitagliptin in plasma using direct analysis in real time mass spectrometry and its application in the pharmacokinetic study thereof.
Gu, J; Liu, Y; Meng, X; Shan, Y; Sun, D; Zhang, L; Zhang, Y, 2022)		0.72
"The pharmacokinetic profiling of active compounds is necessary for drug development and application."( Comparison of biomarker and chromatographic analytical approaches to pharmacokinetic study of sitagliptin.
Faustova, NM; Karlina, MV; Kosman, VM; Makarov, VG; Makarova, MN, 2022)		0.72
" Blood samples were collected and analysed for pharmacokinetic and pharmacodynamic properties."( A double-blind, randomized, placebo and positive-controlled study in healthy volunteers to evaluate pharmacokinetic and pharmacodynamic properties of multiple oral doses of cetagliptin.
Chen, J; Ding, J; Lu, J; Shao, F; Tang, D; Tian, X; Wang, L; Wang, T; Xie, D; Xie, L; Yu, Q; Zhou, C; Zhou, S, 2022)		0.72
" The pharmacokinetic profiles of STG and IRB were successfully applied on simultaneous oral administration to rats."( The simultaneous quantification of Sitagliptin and Irbesartan in rat plasma using the validated LC-MS/MS method is applied to a pharmacokinetic study.
Alanazi, AM; Ali Khan, A; Divya Bhargavi, P; Lolla, S; Shiva Gubbiyappa, K; Sugunan, S; Vijay Nayak, B, 2023)		0.91

Compound-Compound Interactions

ExcerptReferenceRelevance
"Patients with type 2 diabetes mellitus (T2DM) are generally treated with many pharmacological compounds and are exposed to a high risk of drug-drug interactions."( Dipeptidylpeptidase-4 inhibitors (gliptins): focus on drug-drug interactions.
Scheen, AJ, 2010)		0.36
"Dipeptidyl peptidase-4 inhibitors improve glycaemic control in patients with type 2 diabetes mellitus when used as monotherapy or in combination with other anti-diabetic drugs (metformin, sulphonylurea, or thiazolidinedione)."( Efficacy and safety of saxagliptin in combination with metformin compared with sitagliptin in combination with metformin in adult patients with type 2 diabetes mellitus.
Charpentier, G; Gause-Nilsson, I; Hellqvist, A; Ostgren, CJ; Scheen, AJ, 2010)		0.36
"The aim of this trial was to evaluate the efficacy and safety of the combination of once-daily insulin detemir (IDet) and sitagliptin (SITA) versus SITA ± sulphonylurea (SU), both in combination with metformin (MET) in insulin-naive subjects."( Efficacy and safety of insulin detemir once daily in combination with sitagliptin and metformin: the TRANSITION randomized controlled trial.
Hollander, P; Liutkus, JF; Raslova, K; Råstam, J; Skjøth, TV, 2011)		0.37
"The combination of once-daily IDet with SITA showed a clinically and significantly better improvement in glycaemic control than SITA in combination with or without SUs."( Efficacy and safety of insulin detemir once daily in combination with sitagliptin and metformin: the TRANSITION randomized controlled trial.
Hollander, P; Liutkus, JF; Raslova, K; Råstam, J; Skjøth, TV, 2011)		0.37
"This randomized, open-label, crossover study investigated potential drug-drug interactions between the sodium glucose cotransporter-2 (SGLT-2) inhibitor empagliflozin and the dipeptidyl peptidase-4 (DPP-4) inhibitor sitagliptin."( Pharmacokinetics of empagliflozin, a sodium glucose cotransporter-2 (SGLT-2) inhibitor, coadministered with sitagliptin in healthy volunteers.
Brand, T; Macha, S; Mattheus, M; Pinnetti, S; Woerle, HJ, 2012)		0.38
"Sitagliptin was used as monotherapy or in combination with metformin, thiazolidinedione or sulfonylurea."( Safety and efficacy of sitagliptin in combination with transient continuous subcutaneous insulin infusion (CSII) therapy in patients with newly diagnosed type 2 diabetes.
Dong, S; Jia, J; Mao, C; Qian, W; Tang, B; Wang, D; Yang, L; Ye, J; Yu, S; Yuan, G; Zhang, C; Zhou, L; Zhu, T, 2014)		0.4
"We investigated the possibilities of drug-drug interactions between luseogliflozin, a sodium-glucose co-transporter-2 inhibitor, and oral antidiabetic drugs (OADs) in healthy Japanese males."( Absence of Drug-Drug Interactions Between Luseogliflozin, a Sodium-Glucose Co-transporter-2 Inhibitor, and Various Oral Antidiabetic Drugs in Healthy Japanese Males.
Fukatsu, A; Sakai, S; Samukawa, Y; Sasaki, T; Seino, Y; Ubukata, M, 2015)		0.42
" From October 2013 to July 2014, a total of 166 T2DM outpatients who attended the Shanghai Changhai Hospital and the Yijishan Hospital of Wannan Medical College were randomly assigned into an experimental sitagliptin/metformin combined with low caloric diet group (n = 115) and an insulin glargine combined with metformin control group (n = 51)."( Sitagliptin/Metformin Versus Insulin Glargine Combined With Metformin in Obese Subjects With Newly Diagnosed Type 2 Diabetes.
Cao, J; Ji, M; Xia, L; Zou, D, 2016)		0.43
" However, sitagliptin was observed to have no effect when administered alone or in combination with the other three drugs."( Drug combinations in diabetic neuropathic pain: an experimental validation.
Mehta, AK; Tripathi, CD; Yadav, AM, 2016)		0.43
" Sitagliptin, a selective once-daily oral dipeptidyl peptidase-4 inhibitor, has been shown to improve glycemic control as monotherapy and in combination with other antihyperglycemic agents, including sulfonylureas and metformin."( Randomized trial assessing the safety and efficacy of sitagliptin in Chinese patients with type 2 diabetes mellitus inadequately controlled on sulfonylurea alone or combined with metformin.
Ba, J; Engel, SS; Han, P; Hanson, ME; Mo, Z; Pan, C; Shankar, RR; Wu, F; Xu, L; Yuan, G, 2017)		0.46
"Sitagliptin or voglibose combined with SAP can improve glucose control and protect islet function for patients with newly diagnosed T2DM."( [Comparison of therapeutic effects between sitagliptin and voglibose both combined with sensor-augmented insulin pump in newly diagnosed type 2 diabetes].
Bai, R; Du, JL; Liu, D; Shi, CH; Wang, H; Wang, L; Wang, YB; Yang, Y; Zhang, XY, 2016)		0.43
"We compared the individual effects of mitiglinide and glibenclamide administered in combination with the dipeptidyl peptidase-IV (DPP-IV) inhibitor sitagliptin on plasma DPP-IV activity and blood glucose levels in rats with streptozotocin-nicotinamide-induced type 2 diabetes (STZ-NA rats)."( Comparison of the Effects of Mitiglinide and Glibenclamide Administered in Combination with the Dipeptidyl Peptidase-IV Inhibitor Sitagliptin in Rats with Streptozotocin-Nicotinamide-Induced Type 2 Diabetes.
Akahane, K; Inoue, T; Kiguchi, S; Kobayashi, M; Ojima, K; Takeda, H; Tatemichi, S; Yokoyama, A, 2017)		0.46
"The aim of this systematic review was to evaluate the efficacy and safety of liraglutide versus sitagliptin both in combination with metformin in patients with type 2 diabetes and provide reference basis for rational use of clinical drugs."( Efficacy and safety of liraglutide versus sitagliptin both in combination with metformin in patients with type 2 diabetes: A systematic review and meta-analysis.
Jiang, D; Li, M; Wang, Y; Yang, Y; Ying, M; Zhao, R, 2017)		0.46
" Only randomized controlled trials (RCTs) of liraglutide versus sitagliptin both in combination with metformin up to 31 August 2016 were included."( Efficacy and safety of liraglutide versus sitagliptin both in combination with metformin in patients with type 2 diabetes: A systematic review and meta-analysis.
Jiang, D; Li, M; Wang, Y; Yang, Y; Ying, M; Zhao, R, 2017)		0.46
" Compound 4d, a novel TGR5 agonist, in combination with Sitagliptin, a DPP-4 inhibitor, has demonstrated an adequate GLP-1 secretion and glucose lowering effect in animal models, suggesting a potential clinical option in treatment of type-2 diabetes."( Evaluation of novel TGR5 agonist in combination with Sitagliptin for possible treatment of type 2 diabetes.
Agarwal, S; Bhayani, H; Deshmukh, P; Giri, P; Giri, S; Jain, M; Kulkarni, N; Kumar, J; Sasane, S; Soman, S, 2018)		0.48
"To analyze the efficacy and safety of replacing sitagliptin with canagliflozin in patients with type 2 diabetes (T2D) and poor metabolic control despite treatment with sitagliptin in combination with metformin and/or gliclazide."( Efficacy and safety of replacing sitagliptin with canagliflozin in real-world patients with type 2 diabetes uncontrolled with sitagliptin combined with metformin and/or gliclazide: The SITA-CANA Switch Study.
Garcia de Lucas, MD; Gómez Huelgas, R; Olalla Sierra, J; Pérez Belmonte, LM; Suárez Tembra, M, 2018)		0.48
"5%) treated with sitagliptin in combination with metformin and/or gliclazide, sitagliptin (and gliclazide if appropriate) were replaced by canagliflozin."( Efficacy and safety of replacing sitagliptin with canagliflozin in real-world patients with type 2 diabetes uncontrolled with sitagliptin combined with metformin and/or gliclazide: The SITA-CANA Switch Study.
Garcia de Lucas, MD; Gómez Huelgas, R; Olalla Sierra, J; Pérez Belmonte, LM; Suárez Tembra, M, 2018)		0.48
"In patients with T2D poorly controlled with sitagliptin, whether alone or in combination with metformin and/or gliclazide, replacing it with canagliflozin may be a simple yet effective intensification strategy."( Efficacy and safety of replacing sitagliptin with canagliflozin in real-world patients with type 2 diabetes uncontrolled with sitagliptin combined with metformin and/or gliclazide: The SITA-CANA Switch Study.
Garcia de Lucas, MD; Gómez Huelgas, R; Olalla Sierra, J; Pérez Belmonte, LM; Suárez Tembra, M, 2018)		0.48
"There were no adverse effects on bone or muscle when sitagliptin was used in combination with either ipragliflozin or metformin."( Effects of ipragliflozin versus metformin in combination with sitagliptin on bone and muscle in Japanese patients with type 2 diabetes mellitus: Subanalysis of a prospective, randomized, controlled study (PRIME-V study).
Baba, Y; Hashimoto, N; Hattori, A; Horikoshi, T; Ide, K; Ide, S; Ishibashi, R; Ishikawa, K; Ishikawa, T; Kitamoto, T; Kobayashi, A; Kobayashi, K; Koshizaka, M; Maezawa, Y; Nagashima, K; Nakamura, S; Newby, LK; Ogino, J; Ohara, E; Onishi, S; Sakamoto, K; Sato, Y; Shimada, F; Shimofusa, R; Shoji, M; Takahashi, S; Takemoto, M; Tokuyama, H; Uchida, D; Yamaga, M; Yokoh, H; Yokote, K, 2021)		0.62
" Further, the impact of metformin alone or in combination with dipeptidyl peptidase-4 inhibitors on cognition, depression, and QoL of T2DM patients was also compared with newly diagnosed T2DM patients."( Metformin alone and in combination with sitagliptin induces depression and impairs quality of life in type 2 diabetes mellitus patients: An observational study.
Athar, M; Garg, A; Khan, MA; Kohli, S; Parveen, R; Vohora, D, 2023)		0.91
" The subjects were equally divided into four groups: healthy controls, newly diagnosed T2DM patients, and T2DM patients taking either metformin alone or in combination with sitagliptin."( Metformin alone and in combination with sitagliptin induces depression and impairs quality of life in type 2 diabetes mellitus patients: An observational study.
Athar, M; Garg, A; Khan, MA; Kohli, S; Parveen, R; Vohora, D, 2023)		0.91
"05), and in combination with sitagliptin (p < 0."( Metformin alone and in combination with sitagliptin induces depression and impairs quality of life in type 2 diabetes mellitus patients: An observational study.
Athar, M; Garg, A; Khan, MA; Kohli, S; Parveen, R; Vohora, D, 2023)		0.91
" We present a case of severe thrombocytopenia in a 70-year-old NSCLC patient caused by osimertinib combined with sitagliptin."( Successful osimertinib rechallenge after severe thrombocytopenia caused by osimertinib combined with sitagliptin: a case report.
Chen, S; He, L; Huang, M; Tan, X; Zhang, X, 2023)		0.91

Bioavailability

ExcerptReferenceRelevance
" (2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine (1) is a potent, orally active DPP-IV inhibitor (IC(50) = 18 nM) with excellent selectivity over other proline-selective peptidases, oral bioavailability in preclinical species, and in vivo efficacy in animal models."( (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Beconi, M; Eiermann, GJ; Fisher, MH; He, H; Hickey, GJ; Kim, D; Kowalchick, JE; Leiting, B; Lyons, K; Marsilio, F; McCann, ME; Patel, RA; Patel, SB; Petrov, A; Roy, RS; Scapin, G; Thornberry, NA; Wang, L; Weber, AE; Wu, JK; Wyvratt, MJ; Zhang, BB; Zhu, L, 2005)		0.33
"Sitagliptin was well absorbed (approximately 80% excreted unchanged in the urine) with an apparent terminal half-life ranging from 8 to 14 hours."( Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses.
Bergman, A; Davies, MJ; De Smet, M; Gottesdiener, KM; Herman, GA; Hilliard, D; Musson, D; Ramael, S; Snyder, K; Stevens, C; Tanaka, W; Tanen, M; Van Dyck, K; Wagner, JA; Wang, AQ; Winchell, G; Yi, B; Zeng, W, 2005)		0.33
" The absolute oral bioavailability was high, and the pharmacokinetics were fairly dose-proportional."( Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs.
Beconi, MG; Ciccotto, S; Elmore, CS; Hora, DF; Kochansky, CJ; Liu, DQ; Reed, JR; Stearns, RA; Teffera, Y; Vincent, SH; Xia, YQ; Xu, S, 2007)		0.34
"The purpose of this study was to determine the absolute bioavailability of sitagliptin, an orally active, potent and highly selective dipeptidyl peptidase-4 inhibitor recently approved in the United States for the treatment of type 2 diabetes."( Absolute bioavailability of sitagliptin, an oral dipeptidyl peptidase-4 inhibitor, in healthy volunteers.
Bergman, A; Chen, L; Dilzer, S; Ebel, D; Herman, G; Krishna, R; Lasseter, K; Liu, F; Stone, J; Wagner, J; Wang, A; Zeng, W, 2007)		0.34
" All together gliptins have a good oral bioavailability which is not significantly influenced by food intake."( Pharmacokinetics of dipeptidylpeptidase-4 inhibitors.
Scheen, AJ, 2010)		0.36
"Although the bioavailability of sitagliptin was increased by 54% when co-administered with gemfibrozil, this interaction may not have any clinical significance as sitagliptin has a wide therapeutic index."( Pharmacokinetic drug interaction between gemfibrozil and sitagliptin in healthy Indian male volunteers.
B, S; Dubala, A; K P, A; K, E; Kucherlapati, VS; M, D; Meda, VS; P R, AV, 2012)		0.38
" Ertugliflozin demonstrated roughly 100% bioavailability following a single dose of 15 mg."( Ertugliflozin for the treatment of type 2 diabetes.
Kuhad, A; Razdan, K; Sharma, R, 2019)		0.51
" The solubility and permeability characteristics of sitagliptin were reviewed according to the BCS, along with dissolution, therapeutic index, therapeutic applications, pharmacokinetics, pharmacodynamic characteristics, reports of bioequivalence (BE) / bioavailability problems, data on interactions between the drug and excipients and other data germane to the subject."( Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Sitagliptin Phosphate Monohydrate.
Abdallah, DB; Abrahamsson, B; Bakheit, AA; Charoo, NA; Cristofoletti, R; Dressman, J; Haque, KU; Hassan, HA; Langguth, P; Mehta, M; Parr, A; Polli, JE; Shah, VP; Tajiri, T, 2022)		0.96
" The imeglimine molecule is well absorbed (Tmax-4), and the half-life is 5-6 hours, is largely excreted through the kidneys, and also has no clinically significant interactions with either metformin or sitagliptin."( [Imeglimin: features of the mechanism of action and potential benefits].
Arapieva, AM; Bobrik, AG; Bobrik, DV; Khamitova, AD; Kuznetsov, KO; Mahmutova, EI; Nagaev, IR; Saetova, AA, 2022)		0.72

Dosage Studied

This monograph assesses whether methods based on the Biopharmaceutics Classification System (BCS) could be used to assess the bioequivalence of oral dosage forms. Metformin hydrochloride (MTF), sitagliptin phosphate (SIT), simvastatin (SIM) and ezetimibe (EZB) were simultaneously determined with a simple reversed-phase LC method.

ExcerptRelevanceReference
" Sitagliptin possesses pharmacokinetic and pharmacodynamic characteristics that support a once-daily dosing regimen."( Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses.
Bergman, A; Davies, MJ; De Smet, M; Gottesdiener, KM; Herman, GA; Hilliard, D; Musson, D; Ramael, S; Snyder, K; Stevens, C; Tanaka, W; Tanen, M; Van Dyck, K; Wagner, JA; Wang, AQ; Winchell, G; Yi, B; Zeng, W, 2005)		0.33
" Multiple dosing of sitagliptin exhibited a PK/PD profile consistent with that of a QD regimen and was well tolerated."( Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: a double-blind, randomized, placebo-controlled study in healthy male volunteers.
Bergman, AJ; Chen, L; Davies, MJ; De Smet, M; Herman, GA; Hilliard, D; Laethem, M; Ramael, S; Snyder, K; Stevens, C; Tanaka, W; Tanen, M; Wagner, JA; Wang, AQ; Winchell, G; Yi, B; Zeng, W; Zhou, Y, 2006)		0.33
" Following dosing on Day 7 of each treatment period, these pharmacokinetic parameters were determined for plasma sitagliptin and metformin: area under the plasma concentrations-time curve over the dosing interval (AUC(0-12h)), maximum observed plasma concentrations (C(max)), and time of occurrence of maximum observed plasma concentrations (T(max))."( Tolerability and pharmacokinetics of metformin and the dipeptidyl peptidase-4 inhibitor sitagliptin when co-administered in patients with type 2 diabetes.
Bergman, A; Herman, GA; Kipnes, M; Yi, B, 2006)		0.33
" Additionally, the glycemic response to sitagliptin 100 mg daily was evaluated as a once-daily (100 mg once-daily) or twice-daily (50 mg twice-daily) dosing regimen."( Once-daily sitagliptin, a dipeptidyl peptidase-4 inhibitor, for the treatment of patients with type 2 diabetes.
Hanefeld, M; Herman, GA; Mickel, C; Sanchez, M; Stein, PP; Wu, M, 2007)		0.34
" The sitagliptin dosage recommended by the manufacturer is 100 mg once daily as monotherapy or in combination with metformin or a thiazolidinedione."( Sitagliptin: a novel agent for the management of type 2 diabetes mellitus.
Nogid, A; Pham, DQ; Plakogiannis, R, 2008)		0.35
" As it had been 10 months since her last dosage adjustment of diltiazem, it was unlikely that the statin-induced rhabdomyolysis was precipitated by diltiazem."( Rhabdomyolysis caused by a potential sitagliptin-lovastatin interaction.
DiGregorio, RV; Pasikhova, Y, 2009)		0.35
" These results support a once-daily dosing regimen in Japanese patients with T2DM."( Effects of once-daily sitagliptin on 24-h glucose control following 4 weeks of treatment in Japanese patients with type 2 diabetes mellitus.
Amatruda, JM; Fukao, Y; Johnson-Levonas, AO; Nonaka, K; Okuyama, K; Tsubouchi, H, 2009)		0.35
" Plasma DPP-4 activity was assessed at trough, 24 h following dosing on day 7; percent DPP-4 inhibition was corrected for sample assay dilution."( Sitagliptin 100 mg daily effect on DPP-4 inhibition and compound-specific glycemic improvement.
Alba, M; Goldstein, BJ; Guan, Y; Herman, G; Kaufman, KD; Larson, P; Sachs, JR; Sheng, D; Thornberry, N; Williams-Herman, D, 2009)		0.35
"Across sitagliptin doses in this study, the similarity of the 24-h WMG concentrations and the similarity of the corrected DPP-4 inhibition values support prior findings that the maximal glucose-lowering efficacy of sitagliptin is achieved with once-daily dosing of 100 mg."( Sitagliptin 100 mg daily effect on DPP-4 inhibition and compound-specific glycemic improvement.
Alba, M; Goldstein, BJ; Guan, Y; Herman, G; Kaufman, KD; Larson, P; Sachs, JR; Sheng, D; Thornberry, N; Williams-Herman, D, 2009)		0.35
"Sitagliptin is recommended for initial and maintenance dosing at 100 mg daily."( Drug use evaluation of sitagliptin dosing by pharmacist versus nonpharmacist clinicians in an internal medicine department of a private physician-owned multispecialty clinic.
Cross, LB; Gentry, C; Gross, B; McFarland, MS; Patel, UP; Tunney, J, 2009)		0.35
"To determine the prevalence of the potentially inappropriate initial dosing of sitagliptin based on estimated glomerular filtration rate (GFR) at baseline for pharmacist versus nonpharmacist prescribers in an internal medicine department of a private physician-owned multispecialty clinic that included a pharmacist-managed diabetes program."( Drug use evaluation of sitagliptin dosing by pharmacist versus nonpharmacist clinicians in an internal medicine department of a private physician-owned multispecialty clinic.
Cross, LB; Gentry, C; Gross, B; McFarland, MS; Patel, UP; Tunney, J, 2009)		0.35
" For patients prescribed sitagliptin between October 17, 2006, and June 5, 2008, the variables of interest were (a) the initial sitagliptin dose; (b) the GFR, calculated for each patient using the 4-point Modification of Dosing in Renal Disease (MDRD) formula at the time of initiation of sitagliptin; and (c) whether the clinician initiating the dose was a pharmacist or nonpharmacist (i."( Drug use evaluation of sitagliptin dosing by pharmacist versus nonpharmacist clinicians in an internal medicine department of a private physician-owned multispecialty clinic.
Cross, LB; Gentry, C; Gross, B; McFarland, MS; Patel, UP; Tunney, J, 2009)		0.35
" Potentially inappropriate dosing occurred in 1 of 158 patients (0."( Drug use evaluation of sitagliptin dosing by pharmacist versus nonpharmacist clinicians in an internal medicine department of a private physician-owned multispecialty clinic.
Cross, LB; Gentry, C; Gross, B; McFarland, MS; Patel, UP; Tunney, J, 2009)		0.35
"Potentially inappropriate initial dosing of sitagliptin based on assessment of renal function was more likely to occur with nonpharmacist prescribers than with a pharmacist prescriber."( Drug use evaluation of sitagliptin dosing by pharmacist versus nonpharmacist clinicians in an internal medicine department of a private physician-owned multispecialty clinic.
Cross, LB; Gentry, C; Gross, B; McFarland, MS; Patel, UP; Tunney, J, 2009)		0.35
" Pharmacokinetics (AUC for R(+) and S(-) warfarin) and pharmacodynamics (INR of R(+) or S(-) warfarin) were not meaningfully altered following coadministration of multiple-dose sitagliptin and single-dose warfarin, indicating that no dosage adjustment for warfarin is necessary when coadministered with sitagliptin."( Multiple doses of sitagliptin, a selective DPP-4 inhibitor, do not meaningfully alter pharmacokinetics and pharmacodynamics of warfarin.
Herman, GA; Johnson-Levonas, AO; Liu, Q; Maes, A; Wagner, JA; Wright, DH, 2009)		0.35
" A baseline blood sample was drawn before oral dosing with a 100-mg tablet of sitagliptin."( Preprandial single oral dose of sitagliptin does not affect circulating ghrelin and gastrin levels in normal subjects.
Hsu, CH; Huang, CL; Huang, KC; Su, HY; Weng, SF, 2010)		0.36
" Ingestion of a traditional Japanese breakfast prior to dosing had only a minor effect on PK parameters."( Evaluation of pharmacokinetic parameters and dipeptidyl peptidase-4 inhibition following single doses of sitagliptin in healthy, young Japanese males.
Bergman, AJ; Chen, L; Davies, MJ; Gottesdiener, KM; Herman, GA; Langdon, RB; Larson, PJ; Mistry, GC; Ruckle, JL; Snyder, K; Wagner, JA; Wang, AQ; Yi, B; Zeng, W, 2011)		0.37
"The PK and PD findings from this study are consistent with once daily dosing of sitagliptin in Japanese patients with type 2 diabetes."( Evaluation of pharmacokinetic parameters and dipeptidyl peptidase-4 inhibition following single doses of sitagliptin in healthy, young Japanese males.
Bergman, AJ; Chen, L; Davies, MJ; Gottesdiener, KM; Herman, GA; Langdon, RB; Larson, PJ; Mistry, GC; Ruckle, JL; Snyder, K; Wagner, JA; Wang, AQ; Yi, B; Zeng, W, 2011)		0.37
" The method was subsequently used to determine the oral pharmacokinetics of metformin and sitagliptin after dosing to male mice."( Simultaneous quantitation of metformin and sitagliptin from mouse and human dried blood spots using laser diode thermal desorption tandem mass spectrometry.
Denn, M; Gallagher, RT; Peter, RM; Swales, JG, 2011)		0.37
"Assessment of kidney function is necessary to determine appropriate dosing regimens."( Evaluation of Modification of Diet in Renal Disease Study and Cockcroft-Gault equations for sitagliptin dosing.
Hudson, JQ; Markley, BM; McFarland, MS; Zhang, P, )		0.13
" Clinical implications are the potential for excessive dosing of sitagliptin and other agents with similar dose stratification by eCLCr in individuals with kidney dysfunction."( Evaluation of Modification of Diet in Renal Disease Study and Cockcroft-Gault equations for sitagliptin dosing.
Hudson, JQ; Markley, BM; McFarland, MS; Zhang, P, )		0.13
" The objective of this model-based meta-analysis was to describe the time course of HbA1c response after dosing with alogliptin (ALOG), saxagliptin (SAXA), sitagliptin (SITA), or vildagliptin (VILD)."( Quantitative model of the relationship between dipeptidyl peptidase-4 (DPP-4) inhibition and response: meta-analysis of alogliptin, saxagliptin, sitagliptin, and vildagliptin efficacy results.
Barbee, T; Correa, I; Fredrickson, J; Gibbs, JP; Gibbs, MA; Lin, SL; Smith, B, 2012)		0.38
" Multiple dosing of JNJ-38431055 increased post-meal total glucagon-like peptide 1 and gastric insulinotropic peptide concentrations compared to baseline."( Effects of JNJ-38431055, a novel GPR119 receptor agonist, in randomized, double-blind, placebo-controlled studies in subjects with type 2 diabetes.
Gambale, JJ; Katz, LB; Rothenberg, PL; Sarich, TC; Stein, PP; Vaccaro, N; Vanapalli, SR; Xi, L, 2012)		0.38
"Case records of 50 overweight or obese patients with DM who successfully decreased dosage or discontinued diabetes medications after losing weight via attendance at two University-based, outpatient weight management centers were analyzed."( Intentional weight loss and dose reductions of anti-diabetic medications--a retrospective cohort study.
Boddu, ND; Cheskin, LJ; Kahan, S; Kumar, AA; Palamaner Subash Shantha, G; Samson, RJ, 2012)		0.38
"To assess the 54-week efficacy of initial combination therapy with sitagliptin and pioglitazone, compared with pioglitazone monotherapy, and to assess safety in these groups during the 30 weeks after the dosage of pioglitazone was increased from 30 to 45 mg/day, in drug-naÏve patients with type 2 diabetes mellitus and inadequate glycaemic control [haemoglobin A1c (HbA1c) 8-12%]."( Efficacy and safety of initial combination therapy with sitagliptin and pioglitazone in patients with type 2 diabetes: a 54-week study.
Goldstein, BJ; Golm, GT; Kaufman, KD; Lee, M; O'Neill, EA; Steinberg, H; Teng, R; Yoon, KH, 2012)		0.38
"To assess the efficacy and safety of combination therapy with sitagliptin and low dosage sulphonylureas on glycaemic control and insulin secretion capacity in Japanese type 2 diabetes."( Sitagliptin add-on to low dosage sulphonylureas: efficacy and safety of combination therapy on glycaemic control and insulin secretion capacity in type 2 diabetes.
Aono, M; Fukushima, T; Harashima, SI; Inagaki, N; Koizumi, T; Murata, Y; Ogura, M; Seike, M; Tanaka, D; Wang, Y, 2012)		0.38
" The dosage of sitagliptin was increased from 50 mg to 69."( Sitagliptin add-on to low dosage sulphonylureas: efficacy and safety of combination therapy on glycaemic control and insulin secretion capacity in type 2 diabetes.
Aono, M; Fukushima, T; Harashima, SI; Inagaki, N; Koizumi, T; Murata, Y; Ogura, M; Seike, M; Tanaka, D; Wang, Y, 2012)		0.38
"The combination therapy with sitagliptin and low dosage sulphonylureas was safe and effective for glycaemic control."( Sitagliptin add-on to low dosage sulphonylureas: efficacy and safety of combination therapy on glycaemic control and insulin secretion capacity in type 2 diabetes.
Aono, M; Fukushima, T; Harashima, SI; Inagaki, N; Koizumi, T; Murata, Y; Ogura, M; Seike, M; Tanaka, D; Wang, Y, 2012)		0.38
" Primary endpoints were the area under the curve from the time of dosing to infinity (AUC(inf)) and the maximum observed plasma concentration (C(max)) of each drug."( No pharmacokinetic interaction between ipragliflozin and sitagliptin, pioglitazone, or glimepiride in healthy subjects.
Kadokura, T; Keirns, J; Krauwinkel, WJ; Smulders, RA; van Dijk, J; Veltkamp, SA; Zhang, W, 2012)		0.38
" Sitagliptin 100 mg daily was substituted, and glipizide was later added and its dosage adjusted over the next several months."( Combination exenatide-sitagliptin therapy used with glipizide in a patient with type 2 diabetes mellitus.
Edgerton, LP; Elmore, LK; Patel, MB; Whalin, LM, 2012)		0.38
"7 years) were studied on two occasions following 2 days dosing with sitagliptin (100 mg/day) or placebo."( The effects of sitagliptin on gastric emptying in healthy humans - a randomised, controlled study.
Deacon, CF; Horowitz, M; Jones, KL; Nauck, M; Rayner, CK; Stevens, JE, 2012)		0.38
"Coadministration of sitagliptin with empagliflozin did not have a clinically relevant effect on the area under the concentration-time curve of the analyte in plasma at steady state over a uniform dosing interval τ (AUC(τ,ss)) (geometric mean ratio [GMR] 110."( Pharmacokinetics of empagliflozin, a sodium glucose cotransporter-2 (SGLT-2) inhibitor, coadministered with sitagliptin in healthy volunteers.
Brand, T; Macha, S; Mattheus, M; Pinnetti, S; Woerle, HJ, 2012)		0.38
" Optimizing sitagliptin dosing to achieve more sustained DPP-4 inhibition may further improve outcome."( In vivo DPP-4 inhibition to enhance engraftment of single-unit cord blood transplants in adults with hematological malignancies.
Abonour, R; Broxmeyer, HE; Cornetta, K; Farag, SS; Jones, DR; Messina-Graham, S; Robertson, MJ; Schwartz, J; Secrest, A; Srivastava, S; Strother, RM; Wood, L, 2013)		0.39
"01), and the insulin dosage was reduced from 27."( Add-on therapy with the DPP-4 inhibitor sitagliptin improves glycemic control in insulin-treated Japanese patients with type 2 diabetes mellitus.
Ida, K; Ikeda, H; Katsuno, T; Miyagawa, J; Namba, M, 2013)		0.39
" The model was used to drive Monte Carlo simulations to probe the various dosage schedules and the attendant DPP4 response."( Modelling the sitagliptin effect on dipeptidyl peptidase-4 activity in adults with haematological malignancies after umbilical cord blood haematopoietic cell transplantation.
Bies, RR; Broxmeyer, HE; Chitnis, SD; Farag, SS; Messina-Graham, S; Strother, RM; Vélez de Mendizábal, N, 2014)		0.4
" Simulations showed that twice daily or three times daily dosage schedules were superior to a once daily schedule for maximal DPP4 inhibition at the lowest sitagliptin exposure."( Modelling the sitagliptin effect on dipeptidyl peptidase-4 activity in adults with haematological malignancies after umbilical cord blood haematopoietic cell transplantation.
Bies, RR; Broxmeyer, HE; Chitnis, SD; Farag, SS; Messina-Graham, S; Strother, RM; Vélez de Mendizábal, N, 2014)		0.4
"This study provides the first pharmacokinetic-pharmacodynamic model of sitagliptin in the context of HCT, and provides a valuable tool for exploration of optimal dosing regimens, which are critical for improving the time to engraftment in patients after UCB HCT."( Modelling the sitagliptin effect on dipeptidyl peptidase-4 activity in adults with haematological malignancies after umbilical cord blood haematopoietic cell transplantation.
Bies, RR; Broxmeyer, HE; Chitnis, SD; Farag, SS; Messina-Graham, S; Strother, RM; Vélez de Mendizábal, N, 2014)		0.4
" Almost 5 years after its launch in Belgium, the present review summarizes the most recent data regarding the clinical efficacy of this antidiabetic agent, the controversy about its safety profile, its use at lower dosage in case of moderate to severe renal insufficiency, the various indications that have been successively accepted and reimbursed, and, finally, the perspectives offered by a large ongoing cardiovascular outcome trial (TECOS)."( [Sitagliptin in the treatment of type 2 diabetes: insights five years after commercialisation].
Scheen, AJ; Van Gaal, LF, 2013)		0.39
" The proportional dosing alternative of 100 mg every 96 h would result in a TED."( Time of effect duration and administration interval for sitagliptin in patients with kidney failure.
Czock, D; Hartmann, B; Keller, F, 2014)		0.4
" Following 3 months of oral dosing with vehicle, or sitagliptin at doses 3- to 19-fold above the clinically therapeutic plasma concentration, which increased active plasma glucagon-like peptide-1 levels up to approximately 3-fold, or following 3 months of oral dosing with metformin, a non-incretin-based reference T2DM treatment, the pancreas of male ZDF rats was evaluated using qualitative and quantitative histopathology techniques."( Characterization of the exocrine pancreas in the male Zucker diabetic fatty rat model of type 2 diabetes mellitus following 3 months of treatment with sitagliptin.
Cunningham, C; Dey, M; Forest, T; Frederick, C; Holder, D; Prahalada, S; Smith, A; Yao, X, 2014)		0.4
" Sitagliptin increased active GLP-1, but caused a profound suppression of total PYY, GLP-1, and GIP when dosed alone or with GSK263."( Gut hormone pharmacology of a novel GPR119 agonist (GSK1292263), metformin, and sitagliptin in type 2 diabetes mellitus: results from two randomized studies.
Apseloff, G; Atiee, G; Bush, MA; Collins, DA; Corsino, L; Feldman, PL; Gillmor, D; McMullen, SL; Morrow, L; Nunez, DJ, 2014)		0.4
" Colesevelam (3750mg once daily) was dosed throughout the pharmacokinetic sampling period."( Lack of effect of colesevelam HCl on the single-dose pharmacokinetics of aspirin, atenolol, enalapril, phenytoin, rosiglitazone, and sitagliptin.
He, L; Lee, J; Mendell-Harary, J; Tao, B; Walker, J; Wickremasingha, P; Wight, D, 2014)		0.4
" Combination of Sitagliptin with food protein-derived peptides may help in reducing drug dosage and possible associated side-effects."( Utilisation of the isobole methodology to study dietary peptide-drug and peptide-peptide interactive effects on dipeptidyl peptidase IV (DPP-IV) inhibition.
FitzGerald, RJ; Nongonierma, AB, 2015)		0.42
" It is an attractive option because it is dosed once-weekly, provides A1C lowering similar to liraglutide, weight reduction similar to exenatide, and has an adverse effect profile similar to exenatide and liraglutide."( Dulaglutide: the newest GLP-1 receptor agonist for the management of type 2 diabetes.
Thompson, AM; Trujillo, JM, 2015)		0.42
" Compared with sitagliptin 100 mg, canagliflozin 300 mg demonstrated superior diabetes-related quality measure attainment, including glycemic, BP, and weight-related quality measures; there was no difference in LDL-C quality measure attainment between either dosage of canagliflozin and the 100-mg dosage of sitagliptin."( Diabetes-related quality measure attainment: canagliflozin versus sitagliptin based on a pooled analysis of 2 clinical trials.
Bailey, RA; Blonde, L; Meininger, GE; Rupnow, MF; Vijapurkar, U, 2014)		0.4
" Subjects who met the inclusion criteria were added on sitagliptin and started on sitagliptin/metformin combination at the dosage of 50 mg/1000 mg twice daily."( Effect of sitagliptin on epicardial fat thickness in subjects with type 2 diabetes and obesity: a pilot study.
Balladares, N; Contreras, M; D'Marco, L; Iacobellis, G; Lima-Martínez, MM; Paoli, M; Rodney, M, 2016)		0.43
"Trelagliptin (SYR-472), a novel dipeptidyl peptidase-4 inhibitor, shows sustained efficacy by once-weekly dosing in type 2 diabetes patients."( Trelagliptin (SYR-472, Zafatek), Novel Once-Weekly Treatment for Type 2 Diabetes, Inhibits Dipeptidyl Peptidase-4 (DPP-4) via a Non-Covalent Mechanism.
Grimshaw, CE; Jennings, A; Kamran, R; Kinugawa, Y; Kosaka, T; Koumura, E; Nishigaki, N; Sano, H; Shi, L; Takeuchi, K; Tani, A; Ueno, H, 2016)		0.43
" This prescribing could have been due to the complexity of different dosing requirements, or a lack of awareness of the need for dose adjustment of most DPP-4 inhibitors in patients with renal impairment."( Demographic and Clinical Characteristics of Patients With Type 2 Diabetes Mellitus Initiating Dipeptidyl Peptidase 4 Inhibitors: A Retrospective Study of UK General Practice.
Bingham-Gardiner, P; Bolodeoku, J; Hassan, SW; Lee, S; Scowcroft, A; Spencer, W; Tebboth, A, 2016)		0.43
" Endothelial function and plasma markers of endothelial activation (intercellular adhesion molecule 1 (ICAM-1) and vascular cell adhesion molecule 1 (VCAM-1)) were measured prior to and 2 hours following acute dosing of sitagliptin or placebo, as well as following 8 weeks of intervention with each pill."( Impact of DPP-4 inhibition on acute and chronic endothelial function in humans with type 2 diabetes on background metformin therapy.
Branum, A; Malik, M; Puppala, VK; Signorelli, K; Suboc, TM; Tanner, MJ; Tyagi, S; Wang, J; Widlansky, ME; Ying, R, 2017)		0.46
" Metformin hydrochloride (MTF), sitagliptin phosphate (SIT), simvastatin (SIM) and ezetimibe (EZB) were simultaneously determined with a simple reversed-phase LC method in which a SIT-SIM binary mixture, present in a dosage form brand, was considered central for its development."( A Versatile Liquid Chromatographic Method for the Simultaneous Determination of Metformin, Sitagliptin, Simvastatin, and Ezetimibe in Different Dosage Forms.
El-Zaher, AA; Elkady, EF; Elwy, HM; Saleh, MAEM, 2018)		0.76
"To estimate the proportion of patients with moderate to severe chronic kidney disease (CKD) whose initial dipeptidyl-peptidase-4 inhibitor (DPP4-i) dosage was concordant with prescribing information (label) recommendations in the United States."( Concordance with prescribing information dosage recommendations for dipeptidyl-peptidase-4 inhibitors among type 2 diabetes mellitus patients with moderate to severe chronic kidney disease.
Bauer, E; Huang, H; Lang, K; Shetty, S, 2018)		0.48
"9% for saxagliptin and 0% for linagliptin [which does not require dosage adjustment])."( Concordance with prescribing information dosage recommendations for dipeptidyl-peptidase-4 inhibitors among type 2 diabetes mellitus patients with moderate to severe chronic kidney disease.
Bauer, E; Huang, H; Lang, K; Shetty, S, 2018)		0.48
"More than a third of DPP4-i patients with CKD stage 3b or higher were prescribed doses not concordant with DPP4-i label dosage recommendations."( Concordance with prescribing information dosage recommendations for dipeptidyl-peptidase-4 inhibitors among type 2 diabetes mellitus patients with moderate to severe chronic kidney disease.
Bauer, E; Huang, H; Lang, K; Shetty, S, 2018)		0.48
" Twenty-four hours after oral dosing particularly in vivo inhibition of renal-specific DPP-4 activity was more sustained in Sprague Dawley rats after exposure to linagliptin than it was after sitagliptin."( Differences in kidney-specific DPP-4 inhibition by linagliptin and sitagliptin.
Amann, K; Daniel, C; Klein, T; Luippold, G; Mark, M, 2018)		0.48
"SGLT2 inhibitors canagliflozin and dapagliflozin resulted in a weight and A1c-independent reduction of ALT levels compared to incretin agents, with a dose-response observed at higher baseline ALT levels."( SGLT2 inhibitors and incretin agents: Associations with alanine aminotransferase activity in type 2 diabetes.
Aronson, R; Bajaj, HS; Bhullar, L; Brown, RE; Kalra, S; Sohi, N, 2018)		0.48
" Semaglutide was initiated at 3 mg/d and escalated every 4 weeks, first to 7 mg/d then to 14 mg/d, until the randomized dosage was achieved."( Effect of Additional Oral Semaglutide vs Sitagliptin on Glycated Hemoglobin in Adults With Type 2 Diabetes Uncontrolled With Metformin Alone or With Sulfonylurea: The PIONEER 3 Randomized Clinical Trial.
Allison, D; Birkenfeld, AL; Blicher, TM; Davies, M; Deenadayalan, S; Jacobsen, JB; Rosenstock, J; Serusclat, P; Violante, R; Watada, H, 2019)		0.51
"6 hours) than presently available gliflozins, which translates into single daily dosing and dose reduction allowing for patient compliance."( Ertugliflozin for the treatment of type 2 diabetes.
Kuhad, A; Razdan, K; Sharma, R, 2019)		0.51
"Recently, 2 dipeptidyl peptidase-4 (DPP-4) inhibitors, sitagliptin and saxagliptin, adjusted dosing specification from creatinine clearance to glomerular filtration rate, more typically reported in routine laboratory tests."( DPP-4 Inhibitor Dose Selection According to Manufacturer Specifications: A Contemporary Experience From UK General Practice.
Busse, M; Gollop, ND; Marcus, MW; Spanopoulos, D; Tebboth, A; Webb, J, 2019)		0.51
"The development of oral solid dosage forms, such as tablets that contain a high dose of drug(s), requires polymers and other additives to be incorporated at low levels as possible, to keep the final tablet weight low, and, correspondingly, the dosage form size small enough to be acceptable from a patient perspective."( Metformin Hydrochloride and Sitagliptin Phosphate Fixed-Dose Combination Product Prepared Using Melt Granulation Continuous Processing Technology.
Almajaan, A; Andrews, GP; Gilvary, GC; Healy, AM; Jones, DS; Kelleher, JF; Li, S; Loys, ZS; Madi, AM; Tian, YW, 2019)		0.81
" Serial blood samples were collected up to 48 h after dosing on the fifth day."( An Assessment of Pharmacokinetic Interaction Between Lobeglitazone and Sitagliptin After Multiple Oral Administrations in Healthy Men.
Kim, MG; Moon, SJ; Yu, KS, 2020)		0.56
" This study deals with an oral combined dosage form design for two anti-diabetic drugs, sitagliptin and dapagliflozin using self-nanoemulsifying drug delivery systems (SNEDDS)."( Development and optimization of sitagliptin and dapagliflozin loaded oral self-nanoemulsifying formulation against type 2 diabetes mellitus.
Ahmad, A; Alanazi, FK; Aldughaim, MS; Alqahtani, A; Alqahtani, AS; Kazi, M; Noman, OM, 2021)		0.62
" Literature data and in-house experiments were applied in this monograph to assess whether methods based on the Biopharmaceutics Classification System (BCS) could be used to assess the bioequivalence of solid immediate-release (IR) oral dosage forms containing sitagliptin phosphate monohydrate, as an alternative to a pharmacokinetic study in human volunteers."( Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Sitagliptin Phosphate Monohydrate.
Abdallah, DB; Abrahamsson, B; Bakheit, AA; Charoo, NA; Cristofoletti, R; Dressman, J; Haque, KU; Hassan, HA; Langguth, P; Mehta, M; Parr, A; Polli, JE; Shah, VP; Tajiri, T, 2022)		1.14
" Patients with swallowing problems who use feeding tubes and are unable to take oral solid dosage forms may benefit from this research."( Stability of extemporaneously prepared sitagliptin phosphate solution.
Abu Salah, T; Abu Zaaror, Y; Ghanem, M; Jaradat, N; Kaddumi, A; Omari, L; Siaj, S; Zaid, AN, 2022)		0.99
" This study aims to explore reliable approaches to alleviate diarrhea by focusing on two strategies: adjusting the dosing regimen of afatinib itself and implementing combination therapy."( Medication adjustment of afatinib and combination therapy with sitagliptin for alleviating afatinib-induced diarrhea in rats.
Cheng, Z; Hu, A; Liu, Y; Wang, L; Wang, Y; Xu, L; Yang, Y; Zhang, L, 2023)		0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1724391Suppression of glucose tolerance in Wistar Kyoto N-STZ-1.5 rat model of streptozotocin-induced diabetes at 10 mg/kg, po followed by glucose challenge2020Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
Design and Identification of a GPR40 Full Agonist (
AID1724390Stimulation of insulin secretion in Wistar Kyoto N-STZ-1.5 rat model of streptozotocin-induced diabetes at 10 mg/kg, po followed by glucose challenge by ELISA2020Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
Design and Identification of a GPR40 Full Agonist (
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,656)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's188 (11.35)29.6817
2010's1133 (68.42)24.3611
2020's335 (20.23)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 71.50

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index71.50 (24.57)
Research Supply Index7.69 (2.92)
Research Growth Index5.16 (4.65)
Search Engine Demand Index125.98 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (71.50)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials471 (27.46%)5.53%
Reviews217 (12.65%)6.00%
Case Studies86 (5.01%)4.05%
Observational32 (1.87%)0.25%
Other909 (53.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (463)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Multicenter, Randomized, Double-Blind Study to Evaluate the Safety and Efficacy of the Initial Therapy With Coadministration of Sitagliptin and Pioglitazone in Patients With Type 2 Diabetes Mellitus [NCT00397631]Phase 3520 participants (Actual)Interventional2006-12-19Completed
DPP-4 Inhibition With Sitagliptin and the Risk for Hypoglycaemia in the Fasting State in Subjects With Type 2 Diabetes Treated to Fasting Plasma Glucose Targets With Insulin Glargine and Metformin [NCT03359590]Phase 220 participants (Actual)Interventional2018-03-21Completed
A Randomized, Open-label, Fed, Single Dose, Crossover Study to Compare the Pharmacokinetic Characteristics of GLH1SM Extended Release Tablets in Healthy Volunteers [NCT03927170]Phase 125 participants (Actual)Interventional2019-05-02Completed
A Multicenter, Randomized, Double-Blind Study to Evaluate the Safety and Efficacy of the Addition of MK0431 to Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Pioglitazone Therapy [NCT00086502]Phase 3353 participants (Actual)Interventional2004-06-30Completed
The Effects of the DPPIV Inhibitor Sitagliptin in Cystic Fibrosis-related Diabetes [NCT01257464]Phase 23 participants (Actual)Interventional2010-09-30Terminated(stopped due to Lack of recruitment)
A Multicenter, Randomized, Parallel-Group, Double-Blind, Placebo Controlled Phase 2 Dose Finding Study Comparing the Safety, Tolerance, and Efficacy of Various Doses of SK-0403 Versus Placebo and Sitagliptin 100 mg in Patients Not Well-Controlled on Metfo [NCT01169090]Phase 2620 participants (Anticipated)Interventional2010-07-31Completed
Prescription Patterns, Resource Utilization & Costs - Add-on Therapy With Anti Dipeptidyl Peptidase-IVs vs Rosiglitazone [NCT01332370]5,391 participants (Actual)Observational2009-12-31Completed
The Efficacy and Safety of Ursodeoxycholic Acid (UDCA) Added to the Dipeptidyl Peptidase-4 Inhibitor, Sitagliptin in People With Type 2 Diabetes and Chronic Liver Diseases [NCT01337440]Phase 420 participants (Anticipated)Interventional2010-04-30Recruiting
"Is Beta Cell Rest by Insulin Treatment Beneficial Compared to State-of-the Art Enhancers of Insulin Secretion in Preserving Beta Cell Function in Subjects With Latent Autoimmune Diabetes of the Adult (LADA)?" [NCT01140438]64 participants (Actual)Interventional2009-03-31Completed
The Effect of Neprilysin on Plasma Concentrations of Glucagon-Like Peptide-1 in Patients With Type 2 Diabetes [NCT03893526]Phase 412 participants (Actual)Interventional2019-01-25Completed
Impact of Sitagliptin on Cardiovascular Exercise Performance in Type 2 Diabetes [NCT01951339]36 participants (Actual)Interventional2013-10-31Completed
Sitagliptin for the Treatment of Non-alcoholic Steatohepatitis in Patients With Type 2 Diabetes. [NCT01260246]12 participants (Actual)Interventional2010-12-31Terminated(stopped due to Slow recruitment)
Re-examination Study for General Drug Use to Assess the Safety and Efficacy Profile of JANUMET in Usual Practice [NCT01065766]4,065 participants (Actual)Observational2009-03-31Completed
A 12-Week, Phase 2, Randomized, Double-Blind, Placebo Controlled, Dose-Ranging, Parallel Group Study To Evaluate The Efficacy And Safety Of Once Daily Pf-04991532 And Sitagliptin In Adult Patients With Type 2 Diabetes Mellitus Inadequately Controlled On M [NCT01336738]Phase 2266 participants (Actual)Interventional2011-06-30Completed
Chinese PLA General Hospital Hainan Branch [NCT03602638]Phase 4300 participants (Anticipated)Interventional2018-10-01Not yet recruiting
Efficacy and Safety of Oral Semaglutide Using a Flexible Dose Adjustment Based on Clinical Evaluation Versus Sitagliptin in Subjects With Type 2 Diabetes Mellitus [NCT02849080]Phase 3504 participants (Actual)Interventional2016-09-20Completed
Effect of DPP-IV Inhibitors on Occurence of Cancers and the Mechanism Using AGE and RAGE in Patients With Type 2 Diabetes [NCT01588587]500 participants (Anticipated)Observational2012-10-31Not yet recruiting
A Single Center, Randomized, Double-blind Controlled Trial of Sitagliptin Versus Placebo to Reduce the Incidence and Severity of New-onset Diabetes After Kidney Transplant [NCT01928199]Phase 461 participants (Actual)Interventional2013-09-30Completed
Open-labelled, Randomized, Active-controlled, Parallel-arm, Single-center Study on Effect of Sitagliptin on T2DM Patients on Treatment With Metformin and Insulin [NCT01341717]Phase 4440 participants (Actual)Interventional2012-02-29Completed
Incretin-based Drugs and the Risk of Heart Failure: A Multi-center Network Observational Study [NCT02456428]1,499,650 participants (Actual)Observational2014-03-31Completed
Changes in Bone Turnover With Increased Incretin Hormone Exposure (UAB Diabetes Research and Training Center Pilot and Feasibility Study) [NCT01374568]Phase 46 participants (Actual)Interventional2010-07-31Terminated(stopped due to Study closed by sponsor. Funding ended.)
Does Glycated Hemoglobin Variability in Type 2 Diabetes Differ Depending on the Diabetes Treatment Threshold Used in the Qatari Population: Implication on Diabetes Complication Risk? [NCT02879409]150 participants (Anticipated)Interventional2016-11-30Active, not recruiting
Therapeutic Efficacy and Safety of Sitagliptin, Dapagliflozin and Lobeglitazone in Patients With Type 2 Diabetes Mellitus Inadequately Controlled on Glimepiride and Metformin. [NCT02338921]Phase 478 participants (Actual)Interventional2015-01-31Completed
Comparison of Three DPP-4 Inhibitors on 24 Hour Blood Glucose, Incretin Hormones and Islet Function in Patients With Type 2 Diabetes [NCT02089438]Phase 424 participants (Actual)Interventional2014-05-31Completed
Postprandial Secretion of of Incretin Hormones and Incretin Effect in Patients With Maturity-onset Diabetes of the Young (MODY) [NCT01342939]31 participants (Actual)Observational2011-01-31Completed
A Retrospective Database Assessment of Clinical Effectiveness in Type 2 Diabetes Patients Treated With Liraglutide From Primary Care Centers in Sweden [NCT02077946]1,059 participants (Actual)Observational2014-02-10Completed
A Phase III, Multicenter, Randomized, Double-Blind, Placebo-Controlled Clinical Trial to Study the Safety and Efficacy of the Addition of Sitagliptin During Metformin Up-titration Compared With Metformin Up-titration Alone in Subjects With Type 2 Diabetes [NCT02791490]Phase 3458 participants (Actual)Interventional2016-06-16Completed
Metformin and Sitagliptin Therapy for Adult Patients With Type 2 Diabetes Admitted to the General Medical Unit [NCT02250794]Phase 40 participants (Actual)Interventional2014-10-31Withdrawn(stopped due to No subjects enrolled.)
A Multicenter, Two Part, Randomized, Parallel Group, Placebo and Sitagliptin Controlled Study to Evaluate the Safety and Efficacy of GSK256073 Administered Once or Twice Daily for 12 Weeks in Subjects With Type 2 Diabetes Mellitus Who Are Being Treated Wi [NCT01376323]Phase 292 participants (Actual)Interventional2011-07-13Completed
A 12-week, Phase 2, Randomized, Double-blind, Placebo Controlled, Dose-ranging, Parallel Group Study to Evaluate the Efficacy and Safety of Twice Daily Pf-04991532 and Once Daily Sitagliptin in Adult Patients With Type 2 Diabetes Mellitus Inadequately Con [NCT01338870]Phase 2301 participants (Actual)Interventional2011-06-30Completed
Study on Polymorphism of DPP-4 and GLP-1R Genes in Chinese Population and Its Empirical Study on Treatment of Diabetes [NCT03108521]Phase 4119 participants (Actual)Interventional2016-04-21Completed
Prospective, Randomized, Open-label Study With Blinded Endpoint (PROBE Design) to Compare the 72 hr Glycemic Profiles Obtained by Continuous Subcutaneous Glucose Monitoring (CSGM) in Type 2 Diabetic Patients at Baseline With Metformin Monotherapy and Afte [NCT01193296]Phase 436 participants (Actual)Interventional2010-06-30Completed
Efficacy of Combination Therapy With Sitagliptin and Beidougen Capsule in Chinese Patients With Type 2 Diabetes [NCT05667220]Phase 420 participants (Anticipated)Interventional2022-12-01Recruiting
Approaches To Therapy Escalation In T2D: A Cluster Randomized Control Trial (ATTACC) [NCT03813316]Phase 40 participants (Actual)Interventional2019-05-01Withdrawn(stopped due to Lack of funding availability to complete project)
A Pilot Study to Evaluate the Clinical and Biological Tolerance of Sitagliptin With Pegylated Interferon alfa2a Plus Ribavirin Combination Therapy in Chronic Hepatitis C Patients [NCT01567540]Phase 13 participants (Actual)Interventional2013-03-31Terminated(stopped due to New treatments available, which prevents additional recruitment.)
A Multicenter, Randomized, Double Blind, Placebo-Controlled Study to Evaluate the Safety and Efficacy of the Addition of MK0431 to Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Glimepiride Alone or in Combination With Metf [NCT00106704]Phase 3441 participants (Actual)Interventional2005-03-31Completed
A Multicenter, Double-Blind, Randomized Study to Evaluate the Safety and Efficacy of the Addition of MK0431 Compared With Sulfonylurea Therapy in Patients With Type 2 Diabetes With Inadequate Glycemic Control on Metformin Monotherapy [NCT00094770]Phase 31,172 participants (Actual)Interventional2004-09-30Completed
A Multicenter, Randomized, Double-Blind Factorial Study of the Co-Administration of MK0431 and Metformin in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control [NCT00103857]Phase 31,208 participants (Actual)Interventional2005-03-17Completed
The Effects of Neprilysin on Glucagon-like Peptide-1 [NCT03717688]Phase 419 participants (Actual)Interventional2018-05-17Completed
Effects of Sitagliptin on Postprandial Glycaemia, Incretin Hormones and Blood Pressure in Type 2 Diabetes - Relationship to Gastric Emptying [NCT02324010]Phase 214 participants (Actual)Interventional2015-07-31Completed
The Use of Incretin-based Drugs and the Risk of Acute Pancreatitis in Patients With Type 2 Diabetes [NCT02476760]1,417,914 participants (Actual)Observational2014-03-31Completed
Plasma and Endothelial Activity of Dipeptidyl Peptidase 4 During Different Doses of Sitagliptin [NCT02192853]Phase 420 participants (Actual)Interventional2013-05-31Completed
A Randomized, Placebo-Controlled Study to Evaluate the Safety, Efficacy and Mechanism of Action of MK0431/Sitagliptin in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control [NCT00704132]Phase 157 participants (Actual)Interventional2007-02-14Completed
Pilot Project Evaluation of the DPP-4 Inhibitor Sitagliptin in the Treatment of Non-Alcoholic Fatty Liver Disease Using MRI [NCT02263677]Phase 40 participants (Actual)Interventional2014-03-31Withdrawn(stopped due to Technical difficulties have caused this study to be terminated)
Phase 2, Randomized, Double-Blind, Placebo and Active-Comparator Controlled Study to Evaluate the Efficacy, Safety, Tolerability, and Pharmacokinetics of MBX-2982 Administered Daily for 4 Weeks as Monotherapy in Patients With Type 2 Diabetes [NCT01035879]Phase 2100 participants (Actual)Interventional2009-12-31Completed
A Phase III, Multicenter, Double-Blind, Randomized Study to Evaluate the Safety and Efficacy of the Addition of Sitagliptin Compared With the Addition of Glimepiride in Patients With Type 2 Diabetes Mellitus With Inadequate Glycemic Control on Metformin [NCT00701090]Phase 31,035 participants (Actual)Interventional2008-05-31Completed
Effects of Colesevelam HCl, Avandia® (Rosiglitazone Maleate), or JanuviaTM (Sitagliptin) on Glycemic Parameters and Lipid Profiles in Subjects With Type 2 Diabetes Mellitus Inadequately Controlled on Metformin Monotherapy [NCT00484419]Phase 3169 participants (Actual)Interventional2007-05-31Completed
Dynamic Responsiveness of Insulin Secretory Parameters to Sitagliptin and Glimeperide Administration in Subjects With Type 2 Diabetes Mellitus: An Open Label Study [NCT02443922]100 participants (Anticipated)Interventional2015-06-30Not yet recruiting
Preventive Effects of Sitagliptin on Endothelial Dysfunction Induced by Forearm Ischemia-Reperfusion Injury Model [NCT02406950]Phase 310 participants (Anticipated)Interventional2015-02-28Recruiting
A 24-Week, Multicenter, Randomized, Double-blind, Parallel Group, Placebo-controlled Study to Investigate the Effects of Saxagliptin and Sitagliptin in Patients With Type 2 Diabetes Mellitus and Heart Failure [NCT02917031]Phase 4348 participants (Actual)Interventional2017-01-10Completed
DPP-4 Inhibitors in Patients With Type 2 Diabetes and Acute Myocardial Infarction:Effects on Platelet Function [NCT02377388]Phase 374 participants (Actual)Interventional2017-02-07Completed
A Phase 1b, Double-Blind, Placebo-Controlled, Multiple Ascending Dose (MAD) Study to Evaluate the Safety, Tolerability, PK and PD of DA-1241 in Healthy Male Subjects and Subjects With T2DM [NCT03646721]Phase 1108 participants (Actual)Interventional2018-08-29Completed
The Safety and Tolerance of Sitagliptin Combined With Gemcitabine and Albumin-bound Paclitaxel in Subjects With Locally Advanced and Metastatic Pancreatic Adenocarcinoma: an Open, One-Armed, Single-Center, Phase Ⅱ Study. [NCT05947825]Phase 230 participants (Anticipated)Interventional2023-07-30Not yet recruiting
The Empagliflozin vs. DPP-4 Inhibitors and GLP-1 Receptor Agonists Cost of Care Study: a German Claims Data Analysis [NCT04295005]24,500 participants (Actual)Observational2020-11-16Completed
Effect of Dapagliflozin vs Sitagliptin on Liver Fat Accumulation and Body Composition in Patients With Diabetes Mellitus and Liver Transplantation: a Randomized Controlled Trial [NCT05042505]100 participants (Anticipated)Interventional2022-01-01Recruiting
[NCT00860288]Phase 2/Phase 31,988 participants (Actual)Interventional2009-02-28Completed
A Multicenter, Randomized, Double-dummy, Placebo and Active-controlled Study to Assess the Safety, Tolerability and Effect of Taspoglutide on Glycemic Control Compared to Sitagliptin and Placebo in Patients With Type II Diabetes Mellitus Inadequately Cont [NCT00754988]Phase 3666 participants (Actual)Interventional2008-10-31Completed
A Phase III, Multicenter, Randomized, Double-Blind, Double-Dummy, Active-Comparator, Placebo-Controlled Clinical Trial of DBPR108 Tablets for Type 2 Diabetes Mellitus [NCT04161430]Phase 3766 participants (Actual)Interventional2020-01-02Completed
The Effect of Sitagliptin on Brown Adipose Tissue and Whole-body Metabolism in Overweight Pre-diabetic Men [NCT02294084]Phase 430 participants (Actual)Interventional2014-03-31Completed
A Randomized, Prospective, Parallel Design Study to Compare the Effectiveness of Sitagliptin Versus Glimepiride on Endothelial Dysfunction During an Oral Glucose Loading in Drug Naive Patients With Type 2 Diabetes. [NCT02301806]Phase 430 participants (Anticipated)Interventional2015-01-31Recruiting
Comparative Study of Incretin System in Three Ethnic Groups With Abnormal Glucose Tolerance [NCT03659461]174 participants (Actual)Interventional2017-10-01Completed
A Phase 2, Randomized, Placebo-Controlled, Factorial, Double-Blind, Double-Dummy, Parallel-Group, Multicenter Study to Determine the Efficacy and Safety of 25 mg and 50 mg of TAK-875 in Combination With Sitagliptin 100 mg in Subjects With Type 2 Diabetes [NCT01414920]Phase 2368 participants (Actual)Interventional2011-08-31Completed
A Phase 2, Double-Blind, Randomized, Placebo-Controlled, Parallel-Group, Multicenter Study to Evaluate Treatment With SYR-472 in Subjects With Type 2 Diabetes [NCT00760344]Phase 2386 participants (Actual)Interventional2007-03-31Completed
A Phase III, Multicenter, Randomized, Placebo-Controlled, Parallel-Group, Double-Blind Trial to Assess the Safety and Efficacy of Addition of Sitagliptin in Japanese Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Ipragliflo [NCT02577016]Phase 3141 participants (Actual)Interventional2015-11-05Completed
Efficacy of Liraglutide vs. Sitagliptin vs. Insulin Glargine Per Day on Liver Fat When Combined With Metformin in T2DM Subjects With Non-alcoholic Fatty-liver Disease [NCT02147925]Phase 475 participants (Actual)Interventional2014-08-31Completed
A Phase 1, Open Label, Randomized, Crossover, Drug Interaction Study of the Pharmacokinetics of ASP1941 and Sitagliptin After Separate and Concomitant Administration to Healthy Adult Subjects [NCT01104532]Phase 164 participants (Actual)Interventional2010-02-28Completed
The GLP-1 Agonist Semaglutide for the Treatment of Metabolic Disease in Liver Transplant Recipients: A Phase IV, Randomized Trial [NCT05195944]Phase 4140 participants (Anticipated)Interventional2022-10-26Enrolling by invitation
Relative Bioavailability of Both BI 10773 and Sitagliptin After Co-administration Compared to Multiple Oral Doses of BI 10773 (50 mg q.d.) Alone and Sitagliptin (100 mg q.d.) Alone in Healthy Male Volunteers (an Open-label, Randomised, Crossover, Clinical [NCT02172196]Phase 116 participants (Actual)Interventional2009-05-31Completed
Therapeutic Efficacy of Triple Combination of Metformin, DPP4 Inhibitor and Thiazolidinedione in Drug-naïve Korean Type 2 Diabetic Patients [NCT02188186]Phase 4200 participants (Actual)Interventional2014-07-31Completed
A Multicenter, Randomized, Double-Blind Study of MK0431 in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control [NCT00094757]Phase 3521 participants (Actual)Interventional2004-10-06Completed
Metabolism-independent Vascular Effects of the Dipetidylpeptidase-4-inhibitor Sitagliptin in Patients With Type 2 Diabetes Mellitus [NCT01096277]Phase 470 participants (Anticipated)Interventional2010-10-31Not yet recruiting
A Study to Assess the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of LEZ763 Following Single and Multiple Ascending Doses in Healthy Subjects and Patients With Type 2 Diabetes [NCT01619332]Phase 1/Phase 2220 participants (Actual)Interventional2012-03-31Completed
Comparison Between Sitagliptin Add-on Therapy and Insulin Dose Increase Therapy for Uncontrolled Type 2 Diabetes on Insulin Therapy [NCT01100125]Phase 4140 participants (Actual)Interventional2010-04-30Completed
Effects of Treatment With Metformin and/or Sitagliptin on Beta-cell Function and Insulin Resistance in Women With Previous Gestational Diabetes [NCT01336322]Phase 240 participants (Actual)Interventional2011-05-31Completed
A Phase 3, Randomized, Double-Blind, Active-Controlled Study to Evaluate the Effects of Bexagliflozin Versus Sitagliptin in Subjects With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control by Metformin [NCT03115112]Phase 3386 participants (Actual)Interventional2017-10-12Completed
Treatment of Hypoglycemia Following Gastric Bypass Surgery [NCT02527993]Phase 411 participants (Actual)Interventional2015-10-31Completed
Cardiovascular Effects of GLP-1 Receptor Activation [NCT03101930]Phase 4329 participants (Actual)Interventional2017-05-01Completed
A Randomized, Open-label, Fasting, Single Dose, Crossover Study to Compare the Pharmacokinetic Characteristics of GLH1SM Extended Release Tablets in Healthy Volunteers [NCT03851341]Phase 130 participants (Actual)Interventional2019-01-02Completed
The Blood Glucose-lowering Effect of Glucose-dependent Insulinotropic Polypeptide [NCT03845179]12 participants (Actual)Interventional2019-05-29Completed
Comparison Between GLP 1 Analogues and DPP 4 Inhibitors in Type 1 Diabetes Mellitus [NCT01235819]Phase 420 participants (Actual)Interventional2010-11-30Completed
Canagliflozin Continuous Glucose Monitoring (CANA CGM) Trial: A Pilot Randomized, Double-Blind, Controlled, Crossover Study on the Effects of the SGLT-2 Inhibitor Canagliflozin (vs. the DPP-4 Inhibitor Sitagliptin) on Glucose Variability in Mexican Patien [NCT03267576]Phase 464 participants (Actual)Interventional2017-10-27Completed
Efficacy and Safety of Semaglutide Once-weekly Versus Sitagliptin Once-daily as add-on to Metformin in Subjects With Type 2 Diabetes. A 30-week Randomised, Double-blind, Double-dummy, Active-controlled, Parallel-group, Multi-centre and Multi-national Tria [NCT03061214]Phase 3868 participants (Actual)Interventional2017-08-28Completed
Protective Effects of Sitagliptin on β Cell Function in Patients With Adult-onset Latent Autoimmune Diabetes (LADA) [NCT01159847]Phase 1/Phase 230 participants (Actual)Interventional2010-01-31Completed
A Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multicenter Study to Evaluate the Efficacy, Safety, and Tolerability of Canagliflozin as Monotherapy in the Treatment of Subjects With Type 2 Diabetes Mellitus Inadequately Controlled With Di [NCT01081834]Phase 3678 participants (Actual)Interventional2010-03-31Completed
Efficacy and Safety of Sitagliptin and Glargine Compared to a Basal-plus Insulin Regimen in Hospitalized Patients With Type 2 Diabetes [NCT05579119]Phase 476 participants (Actual)Interventional2022-07-06Completed
Effects of Sitagliptin On Markers of Bone Turnover in Patients With Type 2 Diabetes [NCT00732121]Phase 420 participants (Anticipated)Interventional2008-08-31Active, not recruiting
TriMaster: Randomised Double-Blind Crossover Study of a DPP4 Inhibitor, SGLT2 Inhibitor and Thiazolidinedione as Third Line Therapy in Patients With Type 2 Diabetes Who Have Suboptimal Glycaemic Control on Dual Therapy With Metformin and a Sulphonylurea [NCT02653209]Phase 4525 participants (Actual)Interventional2016-11-01Completed
The Use of Dipeptidyl Peptidase-4 Inhibitor Influences the Absorption of Intestine in Short Bowel Syndrome [NCT02653131]Phase 48 participants (Actual)Interventional2016-01-31Terminated(stopped due to too many side-effects)
Superiority Study of Insulin Glargine Over Sitagliptin in Insulin-naïve Patients With Type 2 Diabetes Treated With Metformin and Not Adequately Controlled [NCT00751114]Phase 4515 participants (Actual)Interventional2008-11-30Completed
Effect of Sitagliptin on Clinical, Metabolic and Hormonal Parameters in Polycystic Ovarian Syndrome Patients [NCT05972928]Phase 2/Phase 380 participants (Anticipated)Interventional2023-07-30Not yet recruiting
Involvement of Dipeptidyl Peptidase-4 and Sodium-glucose Co-transporter-2 in Extrapancreatic Glucagon Secretion [NCT04061473]20 participants (Actual)Interventional2019-04-02Completed
A 4-week, Randomized, Double Blind, Double Dummy, Placebo Controlled, Parallel Group Study Comparing the Influence of BI 1356 (5 mg) and Sitagliptin (100 mg) Administered Orally Once Daily on Various Biomarkers in Type 2 Diabetic Patients [NCT00716092]Phase 2121 participants (Actual)Interventional2008-07-31Completed
Sitagliptin Versus Sulphonylurea Based Treatments in Muslim Patients With Type 2 Diabetes During Ramadan [NCT00766441]Phase 422 participants (Actual)Interventional2008-08-31Terminated(stopped due to inadequate recruitment)
A Randomized, Double-blind, Double-dummy, 2-arm Parallel-group, Multicenter 24-week Study Comparing the Efficacy and Safety of AVE0010 to Sitagliptin as add-on to Metformin in Obese Type 2 Diabetic Patients Younger Than 50 and Not Adequately Controlled Wi [NCT00976937]Phase 3319 participants (Actual)Interventional2009-08-31Completed
A Phase II Trial of Inhibition of CD26 Peptidase Using Sitagliptin to Enhance Engraftment After Umbilical Cord Blood Transplantation for Adults With Hematological Malignancies [NCT00862719]Phase 229 participants (Actual)Interventional2009-03-31Completed
Novel Therapy Combining Regenerative Stimuli Immunomodulation to Preserve Beta Cell Function in New Onset Type 1 Diabetes [NCT00837759]Phase 27 participants (Actual)Interventional2009-02-28Terminated(stopped due to Changes to study personnel.)
A Randomized, Open-label, Multiple Dosing, 2-way Crossover Study to Evaluate the Effect of Lobeglitazoneon Pharmacokinetics of Sitagliptin in Healthy Male Volunteers [NCT02827890]Phase 120 participants (Actual)Interventional2016-04-30Completed
A Phase III, Randomized, Placebo-Controlled, Double-Blind Clinical Trial and Subsequent Open-Label, Extension Clinical Trial to Study the Efficacy and Safety of Addition of MK-0431/ONO-5435 in Japansese Patients With Type 2 Diabetes Mellitus Who Have Inad [NCT00854035]Phase 3266 participants (Actual)Interventional2009-02-28Completed
SD in Subjects With T2DM [NCT00871507]Phase 125 participants (Actual)Interventional2009-04-30Completed
Phase III Study of Chiglitazar in Patients With Type 2 Diabetes Mellitus and Insufficient Glycemic Control Despite Diet and Exercise -- A Multicenter, Randomized, Double-Blind, and Sitagliptin-Controlled Trial [NCT02173457]Phase 3740 participants (Actual)Interventional2014-09-30Completed
Sitagliptin Efficacy and Safety for Prevention of Acute Graft Versus Host Disease in Patients Receiving Alternative Donor Allogeneic Hematopoietic Stem Cell Transplantation [NCT05149365]Phase 3190 participants (Anticipated)Interventional2021-12-22Recruiting
Double-blinded, Randomized, Controlled Paired Trial Comparing Sitagliptin to Placebo in Closed Loop. [NCT02328040]Phase 117 participants (Actual)Interventional2014-09-30Completed
A Phase III, Randomized, Double-blind, Clinical Trial to Study the Efficacy and Safety of MK-0431D (a Fixed-dose Combination [FDC] of Sitagliptin and Simvastatin) for the Treatment of Patients With Type 2 Diabetes Mellitus (T2DM) With Inadequate Glycemic [NCT01678820]Phase 3299 participants (Actual)Interventional2012-10-10Terminated(stopped due to Merck terminated the study for business reasons in November 2013.)
Mechanism(s) Underlying Hypotensive Response to ARB/NEP Inhibition - Aim 1 [NCT03738878]Phase 432 participants (Anticipated)Interventional2018-11-15Active, not recruiting
Sitagliptin for the Prevention and Treatment of Stress Hyperglycemia in Non-Diabetic Patients Undergoing Cardiac Surgery [NCT02443402]Phase 468 participants (Actual)Interventional2016-01-31Completed
The Combination of Sitagliptin and Danazol as the Treatment of Steroid-resistant/Relapse Immune Thrombocytopenia: A Randomized, Controlled, Multicenter, Open-label Trial [NCT05353673]Phase 2120 participants (Anticipated)Interventional2021-06-01Recruiting
Effects of Exercise and Inhibition of Dipeptidyl Peptidase-4 on Insulin Secretion in Subjects With Type 1 Diabetes [NCT02127047]Phase 224 participants (Actual)Interventional2013-11-30Completed
Single Dose Crossover Comparative Bioavailability Study of Metformin/Sitagliptin 850 mg/50 mg Film-coated Tablets in Healthy Male and Female Volunteers. [NCT05549570]Phase 126 participants (Actual)Interventional2017-10-22Completed
Polypill Versus Metformin in New Onset Type 2 Diabetes: a Low Dose Triple Therapy Polypill Versus Metformin for Glycaemic Control in Newly Diagnosed Type 2 Diabetes [NCT05833958]Phase 2334 participants (Anticipated)Interventional2024-01-31Not yet recruiting
A Multicenter, Open, Randomized, 24 Weeks Study to Evaluate the Superiority of Glimepiride Over Sitagliptin for the Treatment of naïve Patients With Type 2 Diabetes Mellitus [NCT00957060]Phase 4400 participants (Actual)Interventional2009-07-31Completed
The Effect of Sitagliptin Treatment on Glucose Metabolism and Endothelial Function in Renal Transplant Recipients - JANUVIA-08 [NCT00740363]Phase 425 participants (Actual)Interventional2008-09-30Completed
A Pilot Trial of Adding Oral Hypoglycemic Therapy to Insulin Treatment in Monogenic Variant Carriers of the Joslin 50-Year Medalist Study [NCT04409795]Phase 2/Phase 321 participants (Anticipated)Interventional2021-08-26Enrolling by invitation
Influence of Improving Glycaemic Control on Glucagon-Like-Peptide-1 Response to an Oral Glucose Load. Comparison of Sulphonylurea With DPP-4 Inhibition. [NCT00747383]74 participants (Actual)Interventional2008-09-30Completed
Effects of 4-week Sitagliptin Therapy on Endothelial Progenitor Cells in Type 2 Diabetic Patients. A Non-randomized Controlled Open-label Pilot Trial. [NCT00968006]Phase 440 participants (Actual)Interventional2009-10-31Completed
Predictive Parameters for Therapeutic Efficacy of Initial Combination Therapy With Sitagliptin and Metformin in Type 2 Diabetic Patients [NCT00969566]Phase 4150 participants (Actual)Interventional2009-01-31Completed
A Multicenter, Randomized, Double-Blind Study to Evaluate the Safety and Efficacy of the Addition of MK0431 to Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Metformin Therapy [NCT00086515]Phase 3701 participants (Actual)Interventional2004-06-30Completed
A Randomised, Open, Phase I Study in Patients With Type 2 Diabetes Mellitus Treated With Metformin to Evaluate the Effect of AZD1656 on the Pharmacokinetics of Sitagliptin and Vice Versa [NCT01095991]Phase 112 participants (Anticipated)Interventional2010-03-31Completed
A Randomized, Open-label, Multiple Dosing, 2-way Crossover Study to Evaluate the Effect of Sitagliptin on Pharmacokinetics of Lobeglitazone in Healthy Male Volunteers [NCT02824874]Phase 120 participants (Actual)Interventional2016-04-30Completed
Feed-Back Suppression of Meal-Induced GLP-1 Secretion Mediated Through Elevations in Intact GLP-1 Caused by Dipeptidyl Peptidase 4 (DPP-4) Inhibition: A Randomized, Prospective Comparison of Sitagliptin and Vildagliptin Treatment [NCT02749032]Phase 124 participants (Actual)Interventional2011-11-30Completed
Single Centre in Vivo Cocktail Phenotyping Study on OATP1B1, OCT1/2, MATE1/2K, OAT1/3, and P-gp Drug Transporters in Healthy Volunteers [NCT02743260]Phase 424 participants (Actual)Interventional2016-04-30Completed
An Open-Label, Randomized, Two-Period Crossover Definitive Bioequivalence Study With the Final Marketed Image (FMI) Sitagliptin/Metformin Fixed-Dose Combination (FDC) Tablet and Co-Administration of the Sitagliptin and Metformin Individual Tablets After C [NCT00929201]Phase 161 participants (Actual)Interventional2008-01-31Completed
A Prospective, Multi-center, Randomized, Controlled Study to Evaluate the Effect of DiPeptidyl-Peptidase 4 Inhibitor on Vascular Healing After Biodegradable Polymer Based Sirolimus Eluting Stent Implantation in Diabetic Patients: OCT Study (DIAMOND-OCT) [NCT02802644]Phase 466 participants (Anticipated)Interventional2016-06-30Recruiting
Pilot Study of Safety and Efficacy of Combined Use of Dipeptidyl-peptidase Inhibitor (Sitagliptin) and Proton Pump Inhibitor (Pantoprazole) to Prevent Beta-cell Apoptosis and Promote Islet Regeneration in Islet Transplant Recipients With Early Graft Dysfu [NCT00768651]Phase 28 participants (Actual)Interventional2008-10-31Completed
A Multicenter, Randomized, Double-Blind, Double-Dummy, Active Controlled Clinical Trial for the Validation of Optimum Dose and Preliminary Evaluation of Efficacy and Safety of Evogliptin in Patients With Type 2 Diabetes Mellitus [NCT02689362]Phase 2146 participants (Actual)Interventional2017-08-08Completed
An Open-Label, Single- & Multiple-Dose Study to Investigate the Pharmacokinetics of Sitagliptin 100 mg in Healthy Chinese Adult Subjects [NCT00642798]Phase 116 participants (Actual)Interventional2008-03-31Completed
The Effect of Sitagliptin on Postprandial Glycemia and Endothelial Function in Chinese Subjects With Impaired Glucose Tolerance [NCT00961363]Phase 260 participants (Anticipated)Interventional2009-12-31Recruiting
A 2-Part Trial: a Randomized 6-day Repeat-dose, Parallel-group Study in Subjects With T2DM to Assess the Safety and Tolerability of GSK1614235 Compared to Placebo and Sitagliptin; and a Randomized Single-dose, Food Effect Study in Healthy Volunteers to As [NCT00976261]Phase 172 participants (Actual)Interventional2009-10-17Completed
Acute Effect of a GLP-1-Analogue (Exenatide) and of a DPP-4-Inhibitor (Sitagliptin) in Subjects With Type 2 Diabetes Treated With Insulin Glargine Once Daily [NCT00971659]Phase 148 participants (Actual)Interventional2008-01-31Completed
Sitagliptin Prophylaxis for Glucocorticoid-Induced Impairment of Glucose Metabolism and Beta-Cell Dysfunction in Males With the Metabolic Syndrome X: A Randomized, Placebo-controlled, Double-blind Intervention Study With a 2x2 Factorial Design [NCT00721552]82 participants (Actual)Interventional2008-10-31Completed
"Effect of Dipeptidyl Peptidase IV Inhibitors on Glycemia, Insulin, Glucagon, C Peptide, Glp 1 and Lipids After Isocaloric Meals With Different Nutritional Composition in Patients With Type 2 Diabetes näive of Treatment" [NCT00881543]45 participants (Actual)Interventional2009-06-30Completed
A Multicenter, Randomized, Double-Blind Study to Evaluate the Efficacy and Safety of Sitagliptin Versus Glipizide in Patients With Type 2 Diabetes Mellitus and Chronic Renal Insufficiency Who Have Inadequate Glycemic Control [NCT00509262]Phase 3426 participants (Actual)Interventional2007-10-09Completed
A Phase III, Multicenter, Randomized, Double-Blind Clinical Trial to Study the Safety and Efficacy of the Addition of Sitagliptin (MK0431) to Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Insulin Therapy (Alone or In Combi [NCT00395343]Phase 3641 participants (Actual)Interventional2006-12-11Completed
A Phase 1b, Multicenter, Double-Blind, Randomized, Placebo-Controlled, Crossover Clinical Trial of Sitagliptin 100 mg and Sitagliptin 200 mg in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Diet and Exercise [NCT00541229]Phase 1103 participants (Actual)Interventional2007-08-24Completed
A Multicenter, Double-Blind, Placebo and Active Controlled, Randomized Study to Evaluate the Safety and Efficacy of the Addition of Sitagliptin 100 mg Once Daily in Patients With Type 2 Diabetes With Inadequate Glycemic Control on Metformin Monotherapy [NCT00541775]Phase 3273 participants (Actual)Interventional2006-06-30Completed
A Comparison of Adding Exenatide With Switching to Exenatide in Patients With Type 2 Diabetes Experiencing Inadequate Glycemic Control With Sitagliptin Plus Metformin [NCT00870194]Phase 4255 participants (Actual)Interventional2009-03-31Completed
Combination Therapy of Insulin Glargine and Sitagliptin in Patients With Type 2 Diabetes Not Adequately Controlled by a Previous Treatment With Metformin and Either Insulin Glargine or Sitagliptin [NCT00851903]Phase 3112 participants (Actual)Interventional2009-06-30Completed
A Pilot Study to Evaluate the Safety of a 3 Weeks Sitagliptin Treatment in HCC Patients Undergoing Liver Resection [NCT02650427]Phase 114 participants (Actual)Interventional2016-02-29Completed
A 24 Week, Multicenter, Open-label Study to Evaluate the Efficacy and Safety of Adding Sitagliptin 100 mg Once Daily in Patients With T2DM Who Have Inadequate Glycemic Control on Metformin Therapy [NCT00833027]Phase 4608 participants (Actual)Interventional2008-03-01Completed
Short and Long Term Effects of a Dypeptidil-peptidase-4 Versus Bedtime NPH Insulin as add-on Therapy in Patients With Type 2 Diabetes [NCT02607410]Phase 440 participants (Actual)Interventional2010-01-31Completed
A Phase II, Randomized, Parallel Group Safety, Efficacy, and Pharmacokinetics Study of BI 10773 (1 mg, 5 mg, 10 mg, 25 mg, and 50 mg) Administered Orally Once Daily Over 12 Weeks Compared Double Blind to Placebo With an Additional Open-label Sitagliptin A [NCT00749190]Phase 2495 participants (Actual)Interventional2008-08-31Completed
A Single-Dose Study to Assess the Pharmacokinetics, Safety, and Tolerability of Sitagliptin in Adolescents [NCT00730275]Phase 135 participants (Actual)Interventional2008-07-18Completed
Study of the Effects of Glutamine on Glycemia, Glucagon-like Peptide-1 (GLP-1) and Insulin Secretion in Man [NCT00673894]22 participants (Actual)Interventional2008-04-30Completed
Quantification of the DPP-4 Inhibition-mediated Enhancement of the Activity of the Entero-insular Axis [NCT00683735]Phase 2/Phase 320 participants (Actual)Interventional2009-02-28Completed
Effect of Detemir and Sitagliptin on Blood Glucose Control in Subjects With Type 2 Diabetes Mellitus [NCT00789191]Phase 3222 participants (Actual)Interventional2008-11-30Completed
A Phase 2/3, Placebo-Controlled, Efficacy and Safety Study of Once-Weekly, Subcutaneous LY2189265 Compared to Sitagliptin in Patients With Type 2 Diabetes Mellitus on Metformin [NCT00734474]Phase 2/Phase 31,202 participants (Actual)Interventional2008-08-31Completed
Comparison of the Effect of Exenatide vs. Sitagliptin on 24-hour Average Glucose in Patients With Type 2 Diabetes on Metformin or a Thiazolidinedione [NCT00729326]Phase 483 participants (Actual)Interventional2008-08-31Completed
TECOS: A Randomized, Placebo Controlled Clinical Trial to Evaluate Cardiovascular Outcomes After Treatment With Sitagliptin in Patients With Type 2 Diabetes Mellitus and Inadequate Glycemic Control [NCT00790205]Phase 314,671 participants (Actual)Interventional2008-12-10Completed
Effects of Sitagliptin on Arterial Vasoreactivity and Proatherogenic Mediators in Obesity [NCT02576288]Phase 221 participants (Actual)Interventional2016-01-31Completed
Accelerated Wound Healing in Diabetic Ulcers by Sitagliptin [NCT02675335]Phase 30 participants (Actual)Interventional2016-03-31Withdrawn
Effect of Sitagliptin on Progression of Coronary Intermediate Lesion in Patients With Coronary Heart Disease Complicated With Type 2 Diabetes [NCT02655757]Phase 4120 participants (Actual)Interventional2015-12-31Completed
A Randomized Clinical Trial to Evaluate Glucose-Dependent Insulinotropic Effects of a Single Dose of a DPP-4 Inhibitor in Lean Healthy Males [NCT00888238]Phase 112 participants (Actual)Interventional2009-05-12Completed
A Phase III, Multicenter, Double-Blind, Randomized, Placebo-Controlled Clinical Trial in China to Study the Safety and Efficacy of Co-administration of Sitagliptin and Metformin in Patients With Type 2 Diabetes Mellitus [NCT01076088]Phase 3744 participants (Actual)Interventional2010-11-15Completed
Roux-en-Y Gastric Bypass for BMI 27-32 Type 2 Diabetes vs Best Medical Treatment [NCT02041234]Phase 440 participants (Anticipated)Interventional2014-02-28Completed
A Phase III, Randomized, Placebo-controlled, Double-blind Clinical Trial and Subsequent Open-label, Extension Clinical Trial to Study the Efficacy and Safety of Addition of Sitagliptin in Japanese Patients With Type 2 Diabetes Mellitus Who Have Inadequate [NCT00837577]Phase 3133 participants (Actual)Interventional2009-02-05Completed
Treatment of Wolfram Syndrome Type 2 With the Chelator Deferiprone, and Incretin Based Therapy [NCT02882477]Phase 2/Phase 320 participants (Anticipated)Interventional2016-12-31Not yet recruiting
Phase IV Study Evaluating the Effect of Sitagliptin (Januvia™) on Beta-cell Function in Patients With Acute Myocardial Infarction or Unstable Angina Pectoris and Newly Detected Impaired Glucose Tolerance or Type 2 Diabetes. [NCT00627744]Phase 485 participants (Actual)Interventional2008-05-31Completed
A Randomized, Double-Blind, Active-Controlled, Parallel-Group, Multicenter Study to Determine the Efficacy and Safety of Albiglutide as Compared With Sitagliptin in Subjects With Type 2 Diabetes Mellitus With Renal Impairment [NCT01098539]Phase 3507 participants (Actual)Interventional2010-05-31Completed
Sitagliptin in Combination Oral Agent Therapy for Type 2 Diabetes [NCT00686634]Phase 4108 participants (Actual)Interventional2008-01-31Completed
Combination Therapy With Sitagliptin (DPP 4 Inhibitor) and Lansoprazole (PPI) Inhibitor) to Restore Pancreatic Beta Cell Function in Recent-Onset Type 1 Diabetes [NCT01155284]Phase 270 participants (Actual)Interventional2010-08-31Completed
A Randomized, Double-Blind, Placebo and Active-Controlled, Parallel-Group, Multicenter Study to Determine the Efficacy and Safety of Albiglutide When Used in Combination With Metformin Compared With Metformin Plus Sitagliptin, Metformin Plus Glimepiride, [NCT00838903]Phase 31,049 participants (Actual)Interventional2009-02-28Completed
An Open-Label, Randomized Naturalistic Study to Evaluate the Incidence of Hypoglycemia Comparing Sitagliptin With Sulfonylurea Treatment in Patients With Type 2 Diabetes During Ramadan Fasting [NCT01131182]Phase 41,147 participants (Actual)Interventional2010-06-13Completed
A Preliminary Clinical Study on the Effects of Oral Hypoglycemic Agents on the Stress Hyperglycemic Ratio in Type 2 Diabetes Patients in the Absence of Serious Illness [NCT05822674]80 participants (Actual)Observational2022-01-01Completed
Evaluation of the Effect of Sitagliptin on Gut Microbiota in Patients With Newly Diagnosed Type 2 Diabetes [NCT02900417]9 participants (Anticipated)Interventional2016-09-30Not yet recruiting
Safety and Efficacy of Exenatide Once Weekly Injection Versus Metformin, Dipeptidyl Peptidase-4 Inhibitor, or Thiazolidinedione as Monotherapy in Drug-Naive Patients With Type 2 Diabetes [NCT00676338]Phase 3820 participants (Actual)Interventional2008-11-30Completed
Phase I/II Trial of High-Dose Post-Transplant Cyclophosphamide, Bortezomib, and Sitagliptin for the Prevention of Graft-versus-Host Disease Following Allogeneic Hematopoietic Stem Cell Transplantation [NCT05895201]Phase 1/Phase 272 participants (Anticipated)Interventional2023-09-30Not yet recruiting
A Randomized, Double-blind, Placebo Controlled Study of the Effectiveness of Chronic Incretin-based Therapy on Insulin Secretion in Cystic Fibrosis [NCT01879228]26 participants (Actual)Interventional2013-06-30Completed
Cross-over Study to Assess the Difference in Fasting Plasma Glucose (FPG) Between Vildagliptin (Galvus®/Eucreas®) and Sitagliptin (Januvia®/Janumet®) After Two Weeks [NCT01398592]Phase 4187 participants (Actual)Interventional2011-06-30Completed
A Prospective, Randomized, Parallel-group, Adaptive Design Phase IIb/III, Multicenter Study, to Assess the Efficacy of Polychemotherapy for Inducing Remission of Newly Diagnosed Type 2 Diabetes. [NCT04271189]Phase 2/Phase 3180 participants (Anticipated)Interventional2020-09-01Active, not recruiting
A 3-Part, Open-Label, Randomized, 2-Period Crossover Study to Demonstrate the Definitive Bioequivalence After Administration of the FMI Sitagliptin/Metformin 50/500 mg, 50/850 mg and 50/1000 mg FDC Tablet and Co-administration of Corresponding Doses of Si [NCT00961480]Phase 124 participants (Actual)Interventional2007-10-31Completed
A Randomized, Placebo-Controlled, Double-Blind, Double-Dummy, Four-Period Crossover Study to Assess the Effects of Concomitant Administration of MK0431 and Metformin Alone and in Combination on Post-Meal Incretin Hormone Concentrations in Healthy Adult Su [NCT00975052]Phase 116 participants (Actual)Interventional2006-01-31Completed
Multicenter, Open, Pragmatic, Randomized Trial Comparing the Efficacy of 3 Different Lifestyle Interventions After Addition of Sitagliptin to Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Metformin Therapy [NCT00545584]Phase 31,512 participants (Actual)Interventional2007-04-01Completed
A Phase III Randomized, Active-Comparator (Pioglitazone) Controlled Clinical Trial to Study the Efficacy and Safety of the MK0431A (A Fixed-Dose Combination Tablet of Sitagliptin and Metformin) in Patients With Type 2 Diabetes Mellitus [NCT00532935]Phase 3517 participants (Actual)Interventional2008-01-26Completed
Pilot Study Assessing Glucose Effects of Sitagliptin (Januvia) in Adult Patients With Type 1 Diabetes [NCT00978796]Phase 420 participants (Anticipated)Interventional2009-09-30Completed
A Randomized, Double-Blind, Placebo-Controlled, 3-Arm, Parallel-Group, Multicenter Study to Evaluate the Efficacy, Safety, and Tolerability of Canagliflozin in the Treatment of Subjects With Type 2 Diabetes Mellitus With Inadequate Glycemic Control on Met [NCT01106690]Phase 3344 participants (Actual)Interventional2010-06-30Completed
A Phase III Randomized, Active-Comparator (Pioglitazone) Controlled Clinical Trial to Study the Efficacy and Safety of Sitagliptin and MK0431A (A Fixed-Dose Combination Tablet of Sitagliptin and Metformin) in Patients With Type 2 Diabetes Mellitus [NCT00541450]Phase 3492 participants (Actual)Interventional2008-01-15Completed
The Effect of Sitagliptin on Hypertension, Arterial Stiffness, Oxidative Stress and Inflammation [NCT00696982]60 participants (Anticipated)Interventional2008-06-30Recruiting
The Comparative Study of Dipeptidyl Peptidase-IV Inhibitor and Sulfonylurea on the Effect of Improving Glucose Variability and Oxidative Stress in Type 2 Diabetic Patients With Inadequate Glycemic Control on Metformin [NCT00699322]Phase 436 participants (Anticipated)Interventional2008-06-30Recruiting
Open-label, Non Placebo-Controlled Study To Verify the Effect of Sitagliptin In Adult Patients With Type 2 Diabetes and Inadequate Glycemic Control [NCT00832624]Phase 410 participants (Actual)Interventional2008-11-26Terminated(stopped due to Business Reasons)
[NCT00939939]Phase 43 participants (Actual)Interventional2010-03-31Terminated(stopped due to Recruitment failure)
A Phase III Randomized, Placebo-Controlled Clinical Trial to Study the Safety and Efficacy of the Addition of Sitagliptin (MK0431) in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Combination Therapy With Metformin and a P [NCT00350779]Phase 3262 participants (Actual)Interventional2006-06-12Completed
Assessment of the Effects of a DPP-4 Inhibitor (Sitagliptin) Januvia on Immune Function in Healthy Individuals [NCT00813228]Phase 176 participants (Actual)Interventional2009-01-06Completed
A Multicenter, Randomized, Double-Blind Study of the Co-Administration of Sitagliptin and Pioglitazone in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control [NCT00722371]Phase 31,615 participants (Actual)Interventional2008-09-05Completed
Phase II Study on Sitagliptin -Assessment of Glucose-lowering Effects [NCT00758069]Phase 280 participants (Actual)Interventional2005-07-03Completed
Efficacy of Metformin Versus Sitagliptin on Benign Thyroid Nodules Size in Type 2 Diabetes: a 2-years Prospective Multicentric Study [NCT04298684]Phase 490 participants (Anticipated)Interventional2021-01-01Not yet recruiting
A Phase 3, Randomized, Double-Blind, Active-Controlled, Multi-Center Extension Study to Evaluate Safety and Efficacy of Dutogliptin in Subjects With Type 2 Diabetes Mellitus on a Background Medication of Metformin [NCT00998686]Phase 3650 participants (Anticipated)Interventional2009-11-30Terminated
A Randomized, Double-Blind, Placebo- and Sitagliptin-Controlled, Multi-Center Study to Evaluate Safety and Efficacy of Dutogliptin in Type 2 Diabetes Mellitus Subjects With Moderate and Severe Renal Impairment Including Subjects on Hemodialysis [NCT00958269]Phase 3360 participants (Anticipated)Interventional2009-08-31Terminated(stopped due to Technical/operational issues)
A Phase IIa, Dose-finding, Double-blind, Placebo-controlled, Double-dummy, Randomized, Eightfold Cross-over Study to Investigate the Glucose Lowering Effects of Dextromethorphan Alone or in Combination With Sitagliptin in Subjects With Type 2 Diabetes Mel [NCT01936025]Phase 234 participants (Actual)Interventional2013-10-31Completed
An Open-label, Randomized Two-Part, Two-Period Crossover Study to Demonstrate the Definitive Bioequivalence After Administration of Final Market Image (FMI) Sitagliptin /Metformin 50/500 mg and 50/1000 mg Fixed Dose Combination (FDC) and Concomitant Admin [NCT00961857]Phase 148 participants (Actual)Interventional2005-12-01Completed
Impact of Liraglutide on Cardiac Function and Structure in Young Adults With Type 2 Diabetes: an Open-label, Randomised Active-comparator Trial [NCT02043054]Phase 390 participants (Actual)Interventional2013-12-16Completed
Pharmacokinetic Drug Interaction Study of Dapagliflozin and Glimepiride or Sitagliptin in Healthy Subjects [NCT00842556]Phase 118 participants (Actual)Interventional2009-03-31Completed
A Randomized Controlled Trial to Determine if Sitagliptin Will Enhance Islet Graft Function When Given for 1 Year Following Transplantation [NCT00853944]Phase 312 participants (Anticipated)Interventional2009-07-31Terminated(stopped due to Sponsor withdrew funding du to lack of enrollment. Lack of enrollment was due to decrease in number of islet transplant procedures)
18-wk, International, Multi-centre, Randomized, Parallel-group, Double-Blind, Active-Controlled Phase IIIb Study to Evaluate the Efficacy and Safety of Saxagliptin in Combination With Metformin in Comparison With Sitagliptin in Combination With Metformin [NCT00666458]Phase 3822 participants (Actual)Interventional2008-04-30Completed
A Phase I Double-Blind, Randomized, Placebo-Controlled Clinical Trial to Study the Safety, Efficacy, and Mechanism of Action of Sitagliptin and Pioglitazone in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Diet and Exercis [NCT00511108]Phase 1211 participants (Actual)Interventional2007-07-11Completed
Multiple-dose, Dose Escalation Study to Investigate the Pharmacokinetics/Pharmacodynamics of Sitagliptin in Healthy Male Volunteers [NCT00960453]Phase 112 participants (Anticipated)Interventional2008-12-31Completed
Vagal Mechanisms Mediating the Effects of Glucagon-Like Peptide 1 (GLP-1) on the Endocrine Pancreas - the Entero-endocrine Axis. [NCT02940184]24 participants (Anticipated)Interventional2016-06-30Recruiting
Phase III Study on the Effect of Sitagliptin on Maximal Beta Cell Stimulation [NCT00425490]Phase 330 participants (Anticipated)Interventional2007-01-31Completed
A Randomized, Double-Blind, Placebo-Controlled, Double-Dummy, Parallel Group, Multicenter, Dose-Ranging Study in Subjects With Type 2 Diabetes Mellitus to Evaluate the Efficacy, Safety, and Tolerability of Orally Administered SGLT2 Inhibitor JNJ-28431754 [NCT00642278]Phase 2451 participants (Actual)Interventional2008-04-30Completed
Does the DPP4 Inhibitor Sitagliptin Have a Role in Preventing Type 2 Diabetes- A Randomised Controlled Study. [NCT01038648]Phase 30 participants (Actual)Interventional2011-12-31Withdrawn
A Multicenter, Double-Blind, Randomized Study to Evaluate the Safety and Efficacy of Sitagliptin Compared With Metformin in Patients With Type 2 Diabetes Mellitus With Inadequate Glycemic Control [NCT00449930]Phase 31,050 participants (Actual)Interventional2007-03-01Completed
MK0431 (Sitagliptin) Phase III Clinical Study -Pioglitazone add-on Study for Patients With Type 2 Diabetes Mellitus [NCT00372060]Phase 3134 participants (Actual)Interventional2006-08-21Completed
Sitagliptin (MK0431) Phase III Double-blind Comparative Study - Type 2 Diabetes Mellitus - [NCT00411554]Phase 3319 participants (Actual)Interventional2007-01-31Completed
Sitagliptin (MK0431) Late Phase II Double-Blind Dose-Response Study - Type 2 Diabetes Mellitus [NCT00127192]Phase 2363 participants (Actual)Interventional2005-07-31Completed
Sitagliptin Study in Patients With Type 2 Diabetes Mellitus and Chronic Renal Insufficiency [NCT00095056]Phase 391 participants (Actual)Interventional2004-10-31Completed
Sitagliptin Combo Study [NCT01054118]Phase 118 participants (Actual)Interventional2009-12-31Completed
Re-examination Study for General Drug Use to Assess the Safety and Efficacy Profile of Januvia in Usual Practice [NCT01062048]3,483 participants (Actual)Observational2008-10-31Completed
A Randomized, Double-Blind, Active-Comparator Controlled, Clinical Trial to Study the Efficacy and Safety of MK0431A for the Treatment of Patients With Type 2 Diabetes Mellitus (T2DM) [NCT00482729]Phase 31,246 participants (Actual)Interventional2007-06-19Completed
A Multicenter, Double-Blind, Randomized Study to Evaluate the Safety and Efficacy of the Addition of Sitagliptin to Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Metformin Therapy [NCT00337610]Phase 3190 participants (Actual)Interventional2006-06-30Completed
A Multicenter, Double-Blind, Randomized, Parallel Group Study to Evaluate the Safety and Efficacy of Sitagliptin in Elderly Patients With Type 2 Diabetes Mellitus [NCT00305604]Phase 3206 participants (Actual)Interventional2006-03-08Completed
A Multicenter, Double-Blind, Randomized, Placebo-Controlled Study of MK0431 in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control [NCT00289848]Phase 3530 participants (Actual)Interventional2006-03-31Completed
A Lifestyle Intervention Study Investigating the Role of Interleukin-6 in the Beneficial Effect of Exercise on Beta-cell Function in Obese People and Patients With Type 2 Diabetes [NCT01073826]56 participants (Actual)Interventional2010-02-28Completed
A Randomized, Multicenter, Open-Label, Parallel-Group, 28 Days Phase IV Study Comparing The Postprandial Plasma Glucose Profile of Lixisenatide With That of Sitagliptin Add-On to Insulin Glargine in Type 2 Diabetes Mellitus [NCT02200991]Phase 4136 participants (Actual)Interventional2014-08-31Completed
Effect of a Single Dose of the DPP-4 Inhibitor on Islet Function After Igestion of a Standardized Mixed Meal in Subjects With Type 2 Diabetes [NCT01901861]12 participants (Actual)Interventional2013-07-31Completed
A Phase III, Multicenter, Double-blind, Active-Controlled, 52 Week Extension Study to Evaluate the Safety and Efficacy of Dutogliptin in Patients With Type 2 Diabetes Mellitus Receiving Background Treatment With Glimepiride Alone or in Combination With Me [NCT01089790]Phase 3141 participants (Actual)Interventional2010-03-31Terminated
A Multicenter Randomized, Double-blind, Placebo and Positive Controlled ,Parallel Group ,Phase II Study to Access the Efficacy and Safety of SP2086 Treated Type 2 Diabetes Patients [NCT01969357]Phase 2200 participants (Actual)Interventional2011-06-30Completed
A Phase IIIb Randomised, Double-blind, Active-controlled, Parallel Group, Efficacy and Safety Study of Once Daily Oral Administration of Empagliflozin 25 mg Compared to Sitagliptin 100 mg During 52 Weeks in Type 2 Diabetes Mellitus Patients Who Are Treatm [NCT01984606]Phase 30 participants (Actual)Interventional2015-01-31Withdrawn
A Phase III Double-blind, Extension, Placebo-controlled Parallel Group Safety and Efficacy Trial of BI 10773 (10 and 25mg Once Daily) and Sitagliptin (100mg Once Daily) Given for Minimum 76 Weeks (Incl. 24 Weeks of Preceding Trial) as Monotherapy or With [NCT01289990]Phase 32,705 participants (Actual)Interventional2011-02-28Completed
The Effect of Dipeptidyl Peptidase-4 Inhibition on GLP-1 Induced Insulin Secretion and Glucose Turnover During Mild Stable Hyperglycemia in Young and Old Normal Volunteers [NCT00947011]Phase 212 participants (Actual)Interventional2009-03-31Terminated(stopped due to PI left JHU)
Comparing the Therapeutic Effect of Sitagliptin/Metformin and Metformin on Biochemical Factors and Expression of GDF-9 and BMP-15 Genes in Patients With Classic PCOS Undergoing Intra-cytoplasmic Sperm Injection (ICSI) [NCT04268563]Phase 1/Phase 280 participants (Anticipated)Interventional2020-01-10Recruiting
Perioperative Sitagliptin Medication for Reduction of the Inflammatory Response Associated With Cardiopulmonary Bypass and Postoperative Glucose Control in Diabetic Patients Undergoing Elective Cardiac Surgery - a Pilot Study [NCT05725798]20 participants (Actual)Observational2022-02-01Completed
A Phase III Randomised, Double-blind, Placebo-controlled Parallel Group Efficacy and Safety Study of BI 10773 and Sitagliptin Administered Orally Over 24 Weeks, in Drug naïve Patients With Type 2 Diabetes Mellitus and Insufficient Glycaemic Control Despit [NCT01177813]Phase 3986 participants (Actual)Interventional2010-07-31Completed
Efficacy of Adding Sitagliptin or Pioglitazone to Patients With Type 2 Diabetes Insufficiently Controlled With Metformin and Sulfonylurea [NCT01195090]Phase 4120 participants (Actual)Interventional2009-10-31Completed
A Phase III, Multicenter, Randomized, Placebo-Controlled, Double-Blind Clinical Trial to Evaluate the Safety and Efficacy of the Addition of Sitagliptin in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Diet/Exercise Therap [NCT01177384]Phase 3380 participants (Actual)Interventional2011-01-25Completed
A Multicenter, Multinational, Randomized, Active-controlled, Parallel Group, Double-blind, Phase III Trial to Evaluate the Efficacy and Safety of LC15-0444 Compared With Sitagliptin Added to Ongoing Metformin Therapy in Patients With Type 2 Diabetes Inade [NCT01602003]Phase 3425 participants (Actual)Interventional2009-12-31Completed
An Open-Label, Randomized Naturalistic Study to Evaluate the Incidence of Hypoglycemia Comparing Sitagliptin With Sulfonylurea Treatment in Patients With Type 2 Diabetes During Ramadan Fasting [NCT01340768]Phase 3870 participants (Actual)Interventional2010-06-22Completed
A Randomized, Double-Blind, Placebo and Active-Controlled, 4-Arm, Parallel Group, Multicenter Study to Evaluate the Efficacy, Safety, and Tolerability of Canagliflozin in the Treatment of Subjects With Type 2 Diabetes Mellitus With Inadequate Glycemic Con [NCT01106677]Phase 31,284 participants (Actual)Interventional2010-05-31Completed
A Phase III, Multicenter, Double-Blind, Placebo-Controlled, Randomized Study to Evaluate the Safety and Efficacy of the Addition of Sitagliptin 100 mg Once Daily in Patients With Type 2 Diabetes With Inadequate Glycemic Control on Metformin Monotherapy [NCT00813995]Phase 3395 participants (Actual)Interventional2008-12-09Completed
A Randomized Controlled Pilot Study Assessing the Effect of Sitagliptin on the Preservation of Beta-Cell Function in Patients With Type 2 Diabetes [NCT00420511]Phase 221 participants (Actual)Interventional2007-01-31Completed
A Randomized, Controlled Trial Comparing the Effect of Exenatide, Sitagliptin or Glimepiride on Functional ß -Cell Mass in Patients With Impaired Fasting Glucose or Early Type 2 Diabetes [NCT00775684]47 participants (Actual)Interventional2008-10-31Completed
Comparative Study of DPP-4 Inhibitors and SGLT-2 Inhibitors in Egyptian Diabetic Patients [NCT05359341]175 participants (Actual)Interventional2020-09-20Completed
Monitoring Parameters Beyond Glycemic Control: Impact of Sitagliptin on Quality of Life in Type 2 Diabetes Patients [NCT05167513]Phase 4188 participants (Actual)Interventional2021-01-01Completed
A Phase 2, Randomized, Double-blind, Dose Finding Study of DS-8500a in Japanese Patients With Type 2 Diabetes Mellitus [NCT02628392]368 participants (Actual)Interventional2015-11-30Completed
A Phase III, Multicenter, Double-Blind, Randomized, Active-Controlled Study to Evaluate the Safety and Efficacy of Sitagliptin Compared With Glimepiride in Elderly Patients With Type 2 Diabetes Mellitus With Inadequate Glycemic Control [NCT01189890]Phase 3480 participants (Actual)Interventional2010-08-16Completed
Efficacy and Safety Comparison of Sitagliptin and Glimepiride in Elderly Japanese Patients With Type 2 Diabetes [NCT01183104]305 participants (Actual)Interventional2010-08-31Completed
A 30-Week Extension to: A Multicenter, Randomized, Double-Blind Study to Evaluate the Safety and Efficacy of the Initial Therapy With Coadministration of Sitagliptin and Pioglitazone in Patients With Type 2 Diabetes Mellitus [NCT01028391]Phase 3317 participants (Actual)Interventional2007-09-01Completed
Response of Gut Microbiota in Type 2 Diabetes to Hypoglycemic Agents [NCT04287387]Phase 4180 participants (Anticipated)Interventional2020-03-02Not yet recruiting
A Study in Type II Diabetic Subjects of Single and Multiple Doses of Orally Administered GSK1292263 to Investigate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of the Compound Alone and When Co-administered With Sitagliptin or Metformin [NCT01119846]Phase 2100 participants (Actual)Interventional2009-06-05Completed
A Randomized, 2-period, 2-treatment, Single-dose, Crossover Study to Assess the Bioequivalence of the Fixed Dose Combination (FDC) of Dapagliflozin 10 mg and Sitagliptin 100 mg, and Dapagliflozin 10 mg and Sitagliptin 100 mg Administered as Individual Tab [NCT05266404]Phase 146 participants (Actual)Interventional2022-03-21Completed
The Effects of Co-administration of Colesevelam and Sitagliptin on Glucose Metabolism in Patients With Type 2 Diabetes [NCT01092663]61 participants (Actual)Interventional2010-03-31Completed
A Phase III Randomized, Placebo-Controlled Clinical Trial to Study the Safety and Efficacy of the Addition of Sitagliptin (MK-0431) in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Combination Therapy With Metformin and Pi [NCT00885352]Phase 3313 participants (Actual)Interventional2009-04-15Completed
A Phase III, Randomized, Clinical Trial to Evaluate the Safety and Efficacy of the Addition of Sitagliptin in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on a Sulfonylurea in Combination With Metformin [NCT01076075]Phase 3427 participants (Actual)Interventional2010-06-03Completed
A 78 Week Open Label Extension to Trials Assessing the Safety and Efficacy of BI 10773 as Monotherapy or in Combination With Metformin in Type 2 Diabetic Patients [NCT00881530]Phase 2660 participants (Actual)Interventional2009-03-31Completed
A Randomized, Double-blind, Placebo-controlled Study to Determine Whether Chronic Treatment of Cystic Fibrosis Subjects With Impaired Glucose Tolerance Using Sitagliptin (Januvia) Prevents the Development of Diabetes [NCT00967798]Phase 333 participants (Actual)Interventional2010-05-31Terminated(stopped due to Could not achieve target enrollment)
A Randomized, Double-Blind, Active-Controlled, Multicenter Study to Evaluate the Efficacy, Safety, and Tolerability of Canagliflozin Versus Sitagliptin in the Treatment of Subjects With Type 2 Diabetes Mellitus With Inadequate Glycemic Control on Metformi [NCT01137812]Phase 3756 participants (Actual)Interventional2010-07-31Completed
Effects of Sitagliptin in Individuals With Genetically Decreased DPP4 [NCT04323189]Phase 420 participants (Anticipated)Interventional2020-08-26Recruiting
Pharmacodynamics After Concomitant Administration With Mitiglinide and Sitagliptin Compared to Mitiglinide, Sitagliptin Single Administration in Patients With Type 2 Diabetes [NCT01422590]Phase 126 participants (Actual)Interventional2010-05-31Completed
The Effect of Glimepiride Compared With Sitagliptin as an add-on Therapy to Metformin in Severe Insulin Deficiency Diabetes [NCT05386186]Phase 4192 participants (Anticipated)Interventional2022-01-01Recruiting
A Multicenter, Randomized Double-Blind Study to Evaluate the Efficacy and Safety of Sitagliptin Versus Glipizide in Participants With Type 2 Diabetes Mellitus and End-Stage Renal Disease Who Are on Dialysis and Who Have Inadequate Glycemic Control [NCT00509236]Phase 3129 participants (Actual)Interventional2007-10-19Completed
An Open-Label, Single Dose Study to Investigate the Influence of Hepatic Insufficiency on the Pharmacokinetics of MK0431 [NCT00696826]Phase 120 participants (Actual)Interventional2004-04-30Completed
A 24-week,Multi-centre,Int.,Double-blind,Rand.,Parallel-group,Plac.-Controlled,Phase III Study With a 78-week Ext.Per. to Evaluate the Effect of Dapagliflozin in Combination With Metformin on Body Weight in Subjects With Type2 Diabetes Mellitus Who Have I [NCT00855166]Phase 3182 participants (Actual)Interventional2009-02-28Completed
Sitagliptin Reduces Left Ventricular Mass in Normotensive Type 2 Diabetic Patients With Coronary Artery Disease [NCT01863147]Phase 466 participants (Actual)Interventional2013-07-31Completed
A Randomized, Double-Blind, Placebo-Controlled With Active Comparator, 12-Week Study of DS-8500a in Subjects With Type 2 Diabetes Mellitus on Metformin [NCT02647320]Phase 2298 participants (Actual)Interventional2016-01-31Completed
A Randomized, Double-Blind, Parallel-Group, Multicenter Study to Compare the Glycemic Effects, Safety, and Tolerability of Exenatide Long-Acting Release(Once Weekly) to Those of Sitagliptin and a Thiazolidinedione in Subjects With Type 2 Diabetes Mellitus [NCT00637273]Phase 3514 participants (Actual)Interventional2008-01-31Completed
A Phase 1, Open-label, Randomized, Three-period, Crossover Study to Evaluate Pharmacokinetic Interaction Between Bexagliflozin Tablets and Metformin, Glimepiride, or Sitagliptin in Healthy Subjects [NCT02956044]Phase 154 participants (Actual)Interventional2016-11-30Completed
A Multicenter, Randomized, Open-label Study to Assess the Efficacy and Safety of Sitagliptin Added to the Regimen of Patients With T2 DM With Inadequate Glycemic Control on Metformin [NCT00875394]Phase 368 participants (Actual)Interventional2007-02-01Completed
Treatment of Dysglycemia Using Sitagliptin in Adolescents With Cystic Fibrosis. [NCT01721382]Phase 16 participants (Actual)Interventional2012-11-30Completed
Sitagliptin in the Elderly [NCT00451113]Phase 212 participants (Actual)Interventional2006-11-30Completed
Sitagliptin Treatment in Patients With Type 2 Diabetes Mellitus After Kidney Transplant [NCT00466518]16 participants (Actual)Interventional2007-04-30Completed
A Multicenter, Double-Blind, Randomized, Placebo- and Active-Controlled Dose-Range Finding Study of MK0431 in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control [NCT00482079]Phase 2743 participants (Actual)Interventional2003-05-13Completed
Effects of Sitagliptin on Gastric Emptying in Healthy Subjects [NCT00501657]Phase 115 participants (Actual)Interventional2007-07-31Completed
A Randomized, Double-Blind, Crossover Study to Compare the Effects of Exenatide and Sitagliptin on Postprandial Glucose in Subjects With Type 2 Diabetes Mellitus [NCT00477581]Phase 4102 participants (Actual)Interventional2007-05-31Completed
A Phase III, Multicenter, Randomized, Open-label Clinical Trial Comparing the Efficacy and Safety of a Sitagliptin-Based Treatment Paradigm to a Liraglutide-Based Treatment Paradigm in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Co [NCT01296412]Phase 3653 participants (Actual)Interventional2011-03-11Completed
Effectiveness and Tolerability of Novel, Initial Triple Combination Therapy With Xigduo (Dapagliflozin Plus Metformin) and Saxagliptin vs. Conventional Stepwise add-on Therapy in Drug-naïve Patients With Type 2 Diabetes [NCT02946632]Phase 3104 participants (Anticipated)Interventional2016-12-31Not yet recruiting
[NCT02941445]Phase 424 participants (Actual)Interventional2015-10-31Completed
The Effect of Januvia (Sitagliptin) on Oxidative Stress in Obese Type 2 Diabetic Subjects [NCT00659711]22 participants (Actual)Interventional2008-03-31Completed
Contribution of Substance P to Blood Pressure Regulation in the Setting of Dipeptidyl Peptidase IV (DPP4) and Angiotensin-Converting Enzyme (ACE) Inhibition [NCT02130687]106 participants (Actual)Interventional2014-06-30Completed
Effect of Apple Cider Vinegar in Type 2 Diabetic Patients With Poor Glycemic Control: a Randomized Controlled Design [NCT03593135]126 participants (Actual)Interventional2017-07-15Completed
Randomized, Double-Blind, Placebo-Controlled Study Evaluating the Efficacy of Januvia (Sitagliptin) in Healing Chronic Diabetic Foot Ulcers [NCT02015910]Phase 41 participants (Actual)Interventional2014-01-31Terminated(stopped due to Terminated by the sponsor due to slow enrollment)
MK-0431/ONO-5435 Phase III Clinical Study - Metformin Add-On Study for Patients With Type 2 Diabetes Mellitus [NCT00363948]Phase 3188 participants (Actual)Interventional2006-08-31Completed
Effects of Oral Hypoglycemic Agents Combined With Short-term CSII on Glycemic Control in Newly-diagnosed Type 2 Diabetic Patients [NCT01471808]Phase 4336 participants (Anticipated)Interventional2011-10-31Enrolling by invitation
An Open- Label, 2 Part Study to Investigate the Pharmacokinetics, Safety, and Tolerability of MK0431(Sitagliptin Phosphate) in Patients With Varying Degrees of Renal Insufficiency [NCT00418366]Phase 124 participants (Actual)Interventional2003-01-31Completed
The Role of Phosphodiesterase Inhibitors in Incretin Secretion [NCT02363335]Phase 129 participants (Actual)Interventional2015-02-13Completed
A Phase 1 Clinical Trial to Compare and Evaluate Safety and Pharmacokinetic Characteristics After Administration of SID1903 (Fixed-dose Combination of Dapagliflozin and Sitagliptin) or Loose Combination in Healthy Adult Volunteers [NCT05236998]Phase 145 participants (Actual)Interventional2021-11-03Completed
A Multicenter, Double-Blind, Randomized, Placebo-Controlled Dose-Ranging Finding Study of Once-Daily Dosing of Sitaglipin (MK-0431) in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control [NCT00481663]Phase 2555 participants (Actual)Interventional2003-08-19Completed
A Study to Assess the Effects of Co-Administration of Sitagliptin and Metformin on Incretin Hormone Concentrations [NCT00830076]Phase 118 participants (Actual)Interventional2008-12-02Completed
A Bioequivalence Study With Two Tablet Strengths of the Final Market Image (FMI) Sitagliptin/Metformin Fixed Dose Combination (FDC) Tablet [NCT01093794]Phase 128 participants (Actual)Interventional2010-04-30Completed
The Role of P-glycoprotein in Sitagliptin Clinical Pharmacology [NCT01112670]Phase 433 participants (Actual)Interventional2009-11-30Completed
A Phase III Clinical Trial to Investigate the Efficacy and Safety of Evogliptin When Added to Ongoing Metformin Monotherapy in Patients With Type 2 Diabetes [NCT02949193]Phase 3222 participants (Actual)Interventional2013-05-31Completed
A Randomized, Placebo-Controlled, 4-period, Crossover Study to Assess the Impact of MK-0431 (Sitagliptin) on Incretin Effect and the Role of Specific Incretin Hormones in Patients With Type 2 Diabetes Mellitus [NCT00551590]Phase 124 participants (Actual)Interventional2007-12-31Completed
A Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel, Phase 2a Clinical Trial to Evaluate the Efficacy and Safety of DA-1241 in Subjects With Presumed Non-alcoholic Steatohepatitis (NASH) [NCT06054815]Phase 287 participants (Anticipated)Interventional2023-09-14Recruiting
A Study in Type 2 Diabetic Subjects on Stable Metformin Therapy to Investigate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Co-administering Single and Multiple Oral Doses of GSK1292263 [NCT01128621]Phase 266 participants (Actual)Interventional2009-11-23Completed
Phase III Study of ASP1941 - Open-label, Non-comparative Study to Assess the Long-term Safety, Tolerability and Efficacy of ASP1941 in Combination With a Dipeptidyl Peptidase-4 Inhibitor in Japanese Patients With Type 2 Diabetes Mellitus Who Have Inadequa [NCT01242228]Phase 3106 participants (Actual)Interventional2010-10-21Completed
MK-0431/ONO-5435 Phase III Clinical Trial-Rapid-acting Insulin Secretagogue Add-on Study in Patients With Type 2 Diabetes [NCT01517321]Phase 30 participants InterventionalCompleted
A Multicenter, Randomized, Double-blind, Double Dummy, Active-controlled, Therapeutic Confirmatory Trial(Phase 3) to Evaluate the Efficacy and Safety of CWP-0403 Compared With Sitagliptin Added to Ongoing Metformin Therapy in Patients With Type 2 DM Insuf [NCT01529541]Phase 3200 participants (Anticipated)Interventional2011-05-31Completed
Effect of DPP-IV Inhibitor on Glycemic Control and Autonomic Neuropathy in Adult Patients With Diabetes Mellitus [NCT01545024]60 participants (Anticipated)Observational2011-09-30Recruiting
Treatment With Sitagliptin Phosphate in Patients With Reactive Hypoglycemia Secondary to Dysinsulinism. A Controlled, Randomized, Double-blind, Clinical Trial [NCT00847080]Phase 420 participants (Actual)Interventional2008-12-31Completed
A Randomized Study to Evaluate the Metabolic Responses of Adding Dapagliflozin Versus Sitagliptin to Chinese Patients With Type 2 Diabetes Inadequately Controlled With Insulin Therapy (DISTINCTION Study) [NCT03959501]Phase 460 participants (Actual)Interventional2017-08-16Completed
Pharmacogenetics of Ace Inhibitor-Associated Angioedema:Aim 1 [NCT01413542]44 participants (Actual)Interventional2011-11-30Completed
Replication of the DAPA-CKD (Chronic Kidney Disease) Trial in Healthcare Claims Data [NCT04882813]87,727 participants (Actual)Observational2020-12-13Completed
Effectiveness of Sitagliptin for the Treatment of Newly Diagnosed Type 2 Diabetes [NCT04495881]Phase 450 participants (Anticipated)Interventional2020-01-01Recruiting
Study of Sulphonylurea Synergy With DPP4 Inhibitors [NCT04192292]30 participants (Actual)Interventional2019-10-08Completed
A Phase 1, Open-Label, Sequential, Multiple-Dose, Drug-Drug Interaction Study of Dorzagliatin and Sitagliptin in Subjects With Type 2 Diabetes Mellitus [NCT03790839]Phase 115 participants (Actual)Interventional2019-01-31Completed
Comparative Effectiveness and Safety of Four Second Line Pharmacological Strategies in Type 2 Diabetes Study [NCT05220917]781,430 participants (Anticipated)Observational2021-08-01Active, not recruiting
Sitagliptin Versus Placebo in the Treatment of Non-alcoholic Fatty Liver Disease [NCT01963845]Phase 250 participants (Actual)Interventional2014-01-31Completed
Response To Oral Agents in Diabetes (ROAD)- Pilot Study [NCT00780715]Phase 429 participants (Actual)Interventional2008-12-31Completed
The Use of Incretin-based Drugs and the Risk of Pancreatic Cancer in Patients With Type 2 Diabetes [NCT02475499]886,172 participants (Actual)Observational2014-03-31Completed
Mechanisms of Glucose Lowering Effects of Sitagliptin and Metformin Alone and in Combination in Patients With Type 2 Diabetes Mellitus [NCT00820573]Phase 416 participants (Actual)Interventional2009-10-31Completed
Exploring the Incretin Effect in People With IFG [NCT00795275]26 participants (Actual)Interventional2008-01-31Completed
MK-0431/ONO-5435 Phase III Clinical Study - Long-term Treatment Study for Patients With Type 2 Diabetes Mellitus [NCT00363844]Phase 3209 participants (Actual)Interventional2006-08-31Completed
[NCT01610154]Phase 485 participants (Actual)Interventional2012-10-31Completed
Antidiabetic Effects of Adding a DPP-4 Inhibitor (Sitagliptin) to Pre-Existing Treatment With an Incretin Mimetic (Liraglutide) in Patients With Type 2 Diabetes Treated With Metformin [NCT01937598]Phase 316 participants (Actual)Interventional2013-08-31Completed
EFFECTS OF SITAGLIPTIN THERAPY ON THE KINETICS OF MARKERS OF LOW-GRADE INFLAMMATION AND CELL ADHESION MOLECULES IN PATIENTS WITH TYPE 2 DIABETES [NCT02536248]Phase 320 participants (Actual)Interventional2015-08-01Completed
The Effect of Sitagliptin, a Dipeptidyl Peptidase-4 Inhibitor, on Glycemic Control and Inappropriate Glucagon Secretion in Non-obese Japanese Patients With Type 2 Diabetes. [NCT01642108]40 participants (Anticipated)Interventional2012-07-31Recruiting
A 12-Week, Phase 2, Randomized, Double-Blinded, Placebo-Controlled, Dose-Ranging, Parallel Group Study to Evaluate the Safety, Tolerability and Efficacy Of Once Daily PF-04971729 And Sitagliptin On Glycemic Control And Body Weight In Adult Patients With T [NCT01059825]Phase 2375 participants (Actual)Interventional2010-02-24Completed
A Comparison of Four Hypoglycaemic Regimens During Ramadan Fasting in Type 2 Diabetic Patients and the Effect of Add-On Acarbose on Glycaemic Excursions During Ramadan Fasting [NCT01624116]161 participants (Actual)Interventional2011-08-31Completed
"An Open-label, Randomized, Four-way Cross-over, Single Dose Study to Compare the Different Effect of DPP-4 Inhibitors and Sulfonylurea on the Beta Cell Function by Using Biphase-Hyperglycemic Clamp" [NCT01660386]Phase 412 participants (Anticipated)Interventional2012-07-31Recruiting
Effect of Sitagliptin on the Blood Pressure Response to ACE Inhibition in the Metabolic Syndrome [NCT00666848]Phase 424 participants (Actual)Interventional2008-03-31Completed
An Open-label, Randomized, Parallel Design Trial to Compare the Efficacy of a Sitagliptin-based Metabolic Intervention Versus Standard Diabetes Therapy in Inducing Remission of Type 2 Diabetes [NCT02623998]Phase 3102 participants (Actual)Interventional2016-07-09Completed
Effect of Sitagliptin on Glycemic Control, Post-prandial Glucagon, and Inflammation in Type 1 Diabetics [NCT01741103]0 participants (Actual)Interventional2011-06-30Withdrawn(stopped due to Study funding was for 1 year to a fellow who graduated in early stages of enrollment. While 6 patients were enrolled, many patients didn't finish the study and therefore little data was collected and no results will be entered.)
A Multicenter, Randomized, Double-Blind Comparative Study of Efficacy，Tolerance and Safety Between Sitagliptin ,Vildagliptin and Saxagliptin After 12-week Monotherapy in Drug-naive Adult Patients With Type 2 Diabetes Mellitus [NCT01703637]300 participants (Anticipated)Interventional2012-10-31Recruiting
ß-Cell Function and Glycemic Control of Basal Insulin, Metformin or Sitagliptin in Newly Diagnosed Type 2 Diabetic Patients With Moderate Hyperglycemia [NCT01717911]Phase 4160 participants (Anticipated)Interventional2010-09-30Recruiting
A Pilot Study to Assess the Glucose Lowering Effect of Metformin and Sitagliptin in Adolescents With Type 1 Diabetes Mellitus [NCT01718093]Phase 421 participants (Actual)Interventional2012-10-31Completed
A Phase IV, Randomized, Double-blind, Placebo-controlled, Parallel-group Trial to Assess the Effect of 12-week Treatment With the Glucagon-like Peptide-1 Receptor Agonist (GLP-1RA) Liraglutide or Dipeptidyl Peptidase-4 Inhibitor (DPP-4i) Sitagliptin on th [NCT01744236]Phase 470 participants (Actual)Interventional2013-04-30Completed
Glucose Variability With DPP-4 Inhibition [NCT01751321]50 participants (Anticipated)Interventional2013-05-31Not yet recruiting
Differences in Endothelial Function Amongst Sitagliptin and Liraglutide Users: A Randomized, Open-label, Parallel-group and Active Controlled Trial [NCT01785043]Phase 413 participants (Actual)Interventional2013-03-31Completed
A Multi-center, Randomized, Double-blind, Parallel-group Dose-finding Study to Evaluate Change in HbA1c After 12 Weeks Monotherapy With 7 Doses of LIK066 Compared With Placebo or Sitagliptin in Patients With Type 2 Diabetes [NCT01824264]Phase 20 participants (Actual)Interventional2015-11-30Withdrawn
MASTERMIND - Understanding Individual Variation in Treatment Response in Type 2 [NCT01847144]Phase 4143 participants (Actual)Interventional2013-04-30Completed
MK-0431/ONO-5435 Phase III Clinical Study - Glimepiride add-on Study for Patients With Type 2 Diabetes Mellitus [NCT00363519]Phase 3195 participants (Actual)Interventional2006-08-31Completed
A Double-Blind, Randomized, Placebo Controlled Intervention Study to Assess the Impact of Sitagliptin 100 mg/Day for 1 Year on Insulin Independence Following Pancreatectomy and Autoislet Transplantation [NCT01186562]Phase 483 participants (Actual)Interventional2010-08-31Completed
Sitagliptin Phosphate/Metformin HCl (JANUMET®) Post Marketing Surveillance Protocol [NCT01357148]143 participants (Actual)Observational2009-03-31Terminated(stopped due to Completion of MK-0431A-235 was rendered unnecessary, as the local oversight authority accepted in its stead the results of another study [MK-0431-234].)
Contribution of Neuropeptide Y (NPY) to Vasoconstriction and Sympathetic Activation in the Setting of Dipeptidyl Peptidase IV (DPP4) Inhibition [NCT02639637]Phase 418 participants (Actual)Interventional2015-12-31Completed
Glycemia Reduction Approaches in Diabetes: A Comparative Effectiveness Study [NCT01794143]Phase 35,047 participants (Actual)Interventional2013-05-31Completed
MK0431 Early Phase II Double-blind Study - Type 2 Diabetes Mellitus [NCT00371007]Phase 2126 participants Interventional2004-06-01Completed
Efficacy of Ipragliflozin Compared With Sitagliptin in Uncontrolled Type 2 Diabetes With Sulfonylurea and Metformin [NCT03076112]Phase 3170 participants (Actual)Interventional2017-04-25Completed
Effects of DPP-4 Inhibitor Therapy on Renal Sodium Handling and Renal Hemodynamics in Type 2 Diabetes Patients. The INDORSE Study: Inhibition of Dipeptidyl Peptidase IV: Outcomes on Renal Sodium Excretion [NCT02406443]Phase 436 participants (Actual)Interventional2015-03-31Completed
A Phase III, Multicenter, Randomized, Double-Blind, Placebo-Controlled Clinical Trial to Study the Safety and Insulin-Sparing Efficacy of the Addition of Sitagliptin in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Insulin [NCT01462266]Phase 3660 participants (Actual)Interventional2012-01-13Completed
A Phase 3, Randomized, Active Comparator, Double-Blind, Multi-Center Study to Compare the Efficacy, Safety and Tolerability of ITCA 650 to Sitagliptin as Add-on Therapy to Metformin in Patients With Type 2 Diabetes [NCT01455870]Phase 3535 participants (Actual)Interventional2013-05-31Completed
A Phase 1, Open-label, 3-period, 3-treatment, Single Dose Crossover Study to Evaluate the Pharmacodynamic Effects of LX4211 When Administered Concurrently With JANUVIA® (Sitagliptin) in Subjects With Type 2 Diabetes Mellitus [NCT01441232]Phase 118 participants (Actual)Interventional2011-10-31Completed
Replication of the GRADE Diabetes Trial in Healthcare Claims Data [NCT05099198]6,403 participants (Actual)Observational2018-09-01Completed
Replication of the TECOS Diabetes Trial in Healthcare Claims [NCT03936062]349,476 participants (Actual)Observational2017-09-22Completed
A Multicenter, Randomized, Double Blind Study to Compare the Efficacy and Safety of Sitagliptin/Metformin Fixed-Dose Combination (Janumet®) Compared to Glimepiride in Patients With Type 2 Diabetes Mellitus [NCT00993187]Phase 4292 participants (Actual)Interventional2010-05-04Completed
A Blinded Randomized Controlled Pilot Immunologic and Virologic Safety Trial of an FDA-approved DPPIV-inhibitor in HIV+ Men and Women [NCT01093651]Phase 2/Phase 320 participants (Actual)Interventional2010-06-30Completed
Sitagliptin for the Prevention and Treatment of Hyperglycemia in Patients With Type 2 Diabetes Undergoing Cardiac Surgery [NCT02556918]Phase 4202 participants (Actual)Interventional2016-01-31Completed
DPP-4 Inhibition and Thiazolidinedione for Diabetes Mellitus Prevention (DInT DM Study) [NCT01006018]3 participants (Actual)Interventional2011-07-31Terminated(stopped due to Unanticipated delays due to sterilization/stabilization testing of GLP-1.)
Randomized Controlled Study of Dipeptidyl Peptidase-4 (DPP4) Inhibitor (Sitagliptin) Therapy in the Inpatient Management of Patients With Type 2 Diabetes [NCT01378117]Phase 490 participants (Actual)Interventional2011-08-31Completed
Sitagliptin for the Treatment of Grade 3-4 and Refractory Acute Graft-versus-host Disease [NCT04448587]Phase 210 participants (Anticipated)Interventional2020-10-01Recruiting
Effects of 6 Weeks Treatment With a Dipeptidyl Peptidase 4 Inhibitor on Counterregulatory and Incretin Hormones During Acute Hypoglycaemia in Patients With Type 1 Diabetes: a Randomized Double Blind Placebo-controlled Cross-over Study [NCT01272583]16 participants (Actual)Interventional2011-03-31Completed
Observational Study of the Treatment and Follow-up of Patients With Type II Diabetes Receiving Bitherapy With or Without Sitagliptin (Januvia®/Xelevia®). [NCT01357135]3,453 participants (Actual)Observational2009-07-15Completed
An Open-label Study to Assess the Safety and Tolerability of JANUVIA (Sitagliptin) in 30 Patients With Type 2 Diabetes With Inadequate Glycemic Control on Metformin Monotherapy [NCT01034111]Phase 330 participants (Actual)Interventional2010-03-01Completed
Effects of Sitagliptin in Relatives of Patients With Type 1 Diabetes Mellitus, at High Risk of Developing the Disease [NCT05219409]Phase 2/Phase 370 participants (Anticipated)Interventional2023-07-31Not yet recruiting
Mechanisms Underlying Predictors of Success From Obesity Surgery [NCT02697253]Phase 20 participants (Actual)Interventional2016-01-31Withdrawn
A Randomized, Double-blind, Placebo-controlled, Crossover Study to Evaluate the Effects of Sitagliptin on the Kinetics of Triglyceride-rich Lipoproteins Apolipoprotein B48 and Apolipoprotein B100 in Patients With Type 2 Diabetes [NCT01334229]Phase 322 participants (Actual)Interventional2011-04-30Completed
Bioequivalence of Sitagliptin Phosphate/Metformin Hydrochloride Tablets in Healthy Chinese Subjects: A Single-dose and Two-period Crossover Study [NCT04877106]Phase 148 participants (Actual)Interventional2018-04-07Completed
Effects on Glycemic Variability and Glyco-metabolic Control of Metformin, Pioglitazone and Sitagliptin in Type 2 Diabetic Patients [NCT01895569]Phase 464 participants (Anticipated)Interventional2013-06-30Recruiting
A Multicenter, Randomized, Active-controlled, Parallel Group, Open-label, Exploratory Study to Evaluate the Efficacy on Glucose Variability(MAGE, Glucose SD) and Safety of Initial Combination Therapy of Gemigliptin 50mg q.d., Versus Sitagliptin 100mg q.d. [NCT01890629]Phase 469 participants (Actual)Interventional2013-05-31Completed
Safety and Efficacy of Sitagliptin Plus Granulocyte-colony Stimulating Factor in Patients Suffering From Acute Myocardial Infarction [NCT00650143]Phase 2/Phase 3174 participants (Actual)Interventional2008-03-31Completed
Effect of Sitagliptin on Short-Term Metabolic Dysregulation of Oral Glucocorticoid Therapy [NCT01488279]10 participants (Actual)Interventional2012-09-30Completed
Mechanism of Reduced Response to DPP-4 Inhibitor in Patients With Type 2 Diabetes Mellitus [NCT01449747]Phase 424 participants (Actual)Interventional2011-12-31Completed
A Multicenter, Randomized, Double Blind, Placebo-controlled Study to Evaluate the Efficacy of Acarbose Added on Top of Metformin and Sitagliptin Combination Treatment in Type 2 Diabetes Mellitus Patients [NCT01490918]Phase 4165 participants (Actual)Interventional2012-04-30Completed
The Effect of Sitagliptin on Glucagon Counterregulation and Incretin Hormones During Mild Hypoglycemia in Elderly Patients With Metformin-treated Type 2 Diabetes [NCT02256189]Phase 428 participants (Actual)Interventional2015-04-30Completed
A Phase III, Multicenter, Randomized, Placebo-Controlled, Parallel-Group, Double-Blind Trial to Assess the Safety and Efficacy of Addition of Ipragliflozin in Japanese Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Sitaglip [NCT02577003]Phase 3143 participants (Actual)Interventional2015-11-09Completed
A Phase III, Randomized, Double-Blind, Multicenter Study to Evaluate the Efficacy and Safety of the Combination of Ertugliflozin (MK-8835/PF-04971729) With Sitagliptin Compared With Ertugliflozin Alone and Sitagliptin Alone, in the Treatment of Subjects W [NCT02099110]Phase 31,233 participants (Actual)Interventional2014-04-22Completed
Efficacy and Long-term Safety of Oral Semaglutide Versus Sitagliptin in Subjects With Type 2 Diabetes [NCT02607865]Phase 31,864 participants (Actual)Interventional2016-02-15Completed
A Multi-center, Active Controlled, Randomized, Double-blinded, Parallel, Phase IV Study to Evaluate the Effect of Improving Glycemic Variability of Anagliptin Compared With Sitagliptin in Patients With Type 2 Diabetes Mellitus [NCT04810507]Phase 489 participants (Actual)Interventional2018-11-09Completed
Investigating the Protective Effect of Newer Antidiabetic Drugs on Cognitive Decline in Diabetic Patients [NCT05347459]100 participants (Anticipated)Observational2022-03-02Recruiting
The Effect of Sitagliptin Treatment in COVID-19 Positive Diabetic Patients [NCT04365517]Phase 3170 participants (Anticipated)Interventional2021-12-29Not yet recruiting
A Randomized Active-Control Double-Blinded Study to Evaluate the Treatment of Diabetes in Patients With Systolic Heart Failure [NCT02920918]Phase 436 participants (Actual)Interventional2016-10-31Completed
Study of the Effect of Sitagliptin on the Hormonal Responses to Macronutrient Ingestion in Healthy Volunteers [NCT00885638]Phase 412 participants (Actual)Interventional2009-08-31Completed
A Randomized, Double-blind, Parallel-group, Placebo-controlled Study to Assess Efficacy, Safety and Tolerability of Sitagliptin Phosphate 100 mg as Treatment for Recurrent, Persistent or Newly Diagnosed Type 2 Diabetes After Gastric Bypass [NCT01512797]37 participants (Actual)Interventional2012-07-31Completed
A Phase IIa, Multicenter, Double-Blind, Randomized, Active Comparator-Controlled Clinical Trial to Study the Efficacy and Safety of MK0893 in Combination With Sitagliptin or in Combination With Metformin in Patients With Type 2 Diabetes Mellitus Who Have [NCT00631488]Phase 2146 participants (Actual)Interventional2008-02-29Completed
Ketosis-Prone Diabetes in African Americans: Predictive Markers, Underlying Mechanisms, and Treatment Outcomes: The Effects of Metformin vs. Sitagliptin on Beta-Cell Preservation in Obese Subjects With Ketosis-Prone Type 2 Diabetes Mellitus [NCT01099618]Phase 448 participants (Actual)Interventional2010-03-31Completed
A Phase III, Multicenter, Randomized, Double-Blind, Placebo-Controlled Clinical Trial in China to Study the Safety and Efficacy of the Addition of Sitagliptin in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Insulin Therap [NCT01590797]Phase 3467 participants (Actual)Interventional2012-07-10Completed
Sitagliptin (JANUVIA®) Post Marketing Surveillance Protocol [NCT01354990]2,974 participants (Actual)Observational2009-02-28Completed
A 26-week International, Multicenter, Randomized, Double-Blind, Active Controlled, Parallel Group, Phase 3bTrial With a Blinded 26-week Long -Term Extension Period to Evaluate the Efficacy and Safety of Saxagliptin Co-administered With Dapagliflozin in Co [NCT02284893]Phase 3461 participants (Actual)Interventional2014-09-09Completed
Efficacy, Durability, Safety, and Tolerability of Sitagliptin vs. Pioglitazone as add-on Treatments in Patients With Type 2 Diabetes Uncontrolled on the Full-dose Metformin Plus Sulfonylurea: a 52-week, Randomized, Open-label, Parallel-group, Phase 3 Clin [NCT03125694]Phase 3250 participants (Actual)Interventional2015-02-01Completed
Randomized Double Blind Parallel Design Study Comparing Risk of Nocturnal Hypoglycemia and Critical Arrhythmia With Sitagliptin Versus Glimepiride in Patients With Type 2 Diabetes Insufficiently Controlled With Metformin Monotherapy [NCT02373865]Phase 44 participants (Actual)Interventional2015-09-30Terminated(stopped due to Premature termination due to insufficient patient recruitement..)
A Phase 1b, Randomized, Double-blind, Active Comparator Controlled, 3-period, Cross-over Study To Characterize The Pharmacodynamics And Tolerability Of Two Dosing Regimens Of Pf-04937319 In Adults With Type 2 Diabetes Mellitus Inadequately Controlled On M [NCT01933672]Phase 133 participants (Actual)Interventional2013-10-31Completed
A Randomized, Double-Blinded, Placebo-Controlled Trial of a Dipeptidyl Peptidase-4 Inhibitor (Sitagliptin, Januvia) for Reducing Inflammation and Immune Activation in HIV-Infected Men and Women: A Multicenter Trial of the AIDS Clinical Trials Group (ACTG) [NCT02513771]Phase 290 participants (Actual)Interventional2015-09-30Completed
Clinical Effect of Dipeptidyl Peptidase-4 (DPP-4) Inhibitors in Urinary Albumin to Creatinine Ratio in Patients With Overt Kidney Disease [NCT02048904]Phase 4142 participants (Actual)Interventional2014-01-31Terminated(stopped due to Original Principal Investigator left institution. No data analyzed.)
A Phase III, Multicenter, Randomized, Double-Blind, Active-Comparator-Controlled Clinical Trial to Study the Safety and Efficacy of the Addition of Ertugliflozin (MK-8835/PF-04971729) Compared With the Addition of Glimepiride in Subjects With Type 2 Diabe [NCT01999218]Phase 31,326 participants (Actual)Interventional2013-12-16Completed
Efficacy and Safety of Semaglutide Once-weekly Versus Sitagliptin Once-daily as add-on to Metformin and/or TZD in Subjects With Type 2 Diabetes (SUSTAIN™ 2 - vs. DPP-4 Inhibitor) [NCT01930188]Phase 31,231 participants (Actual)Interventional2013-12-02Completed
Dietary Impacts on Glucose-lowering Effects of Sitagliptin in Type 2 Diabetes: a Multicenter, Randomized, Prospective, Open-label, Clinical Trial [NCT02312063]Phase 448 participants (Actual)Interventional2015-02-28Completed
Prevention of Stress Hyperglycemia With the Use of DPP-4 Inhibitors in Non-diabetic Patients Undergoing Non-cardiac Surgery, a Pilot Study [NCT02741687]Phase 480 participants (Actual)Interventional2016-06-30Completed
The Efficacy and Safety of Liraglutide Compared to Sitagliptin, Both in Combination With Metformin in Chinese Subjects With Type 2 Diabetes.(LIRA-DPP-4 CHINA™) [NCT02008682]Phase 4368 participants (Actual)Interventional2013-12-31Completed
Comparative, Randomized, Single Dose, Two-way Crossover Bioequivalence Study to Determine the Bioequivalence of Metformin HCl From Gleptomet 50/1000 mg F.C.Tablets (EVA Pharma for Pharmaceuticals & Medical Appliances, Egypt) and Janumet 50/1000 mg F.C.Tab [NCT05798715]Phase 130 participants (Actual)Interventional2022-11-29Completed
The Role of Incretins in the Pathogenesis of Fasting and Postprandial Glucose Metabolism in People With Impaired Fasting Glucose [NCT00364377]Phase 422 participants (Actual)Interventional2006-08-31Completed
Effect of Anagliptin and Sitagliptin on Low-density Lipoprotein Cholesterol in Patients With Type 2 Diabetes and Cardiovascular Risk Factors: Randomized Controlled Trial [NCT02330406]Phase 4353 participants (Actual)Interventional2015-04-30Completed
Phase 3, Double Blinded, Placebo Controlled Study of the Effects of 12 Weeks DPP-IV Inhibitor Treatment on Secretion and Action of the Incretin Hormones in Patients With Type 2 Diabetes [NCT00411411]Phase 349 participants (Actual)Interventional2007-02-28Completed
A Phase III Randomized Clinical Trial to Study the Efficacy and Safety of the Co-administration of Sitagliptin and Atorvastatin in Patients With Type 2 Diabetes Mellitus With Inadequate Glycemic Control on Metformin Monotherapy [NCT01477853]Phase 3166 participants (Actual)Interventional2011-10-24Terminated(stopped due to The study was terminated early by the Sponsor for business reasons.)
A Phase 2, Randomized, Double-blinded, Placebo-controlled, Dose-ranging, Parallel Group Study To Evaluate Safety And Efficacy Of Pf-04937319 And Sitagliptin On Glycemic Control In Adult Patients With Type 2 Diabetes Mellitus Inadequately Controlled On Met [NCT01475461]Phase 2345 participants (Actual)Interventional2011-11-30Completed
Multicentric Cross-over Trial to Assess the Glycemic Profiles on 8 Weeks of Vildagliptin and Sitagliptin Treatment, Each, in Type-2 Diabetic Patients With a Pre-existing Cardiovascular Disease Pre-treated With Insulin, Using a PROBE-design [NCT01686932]Phase 451 participants (Actual)Interventional2012-11-30Completed
Efficacy and Safety of Lobeglitazone Versus Sitagliptin in Inadequately Controlled by Metformin Alone Type 2 Diabetes Mellitus Patients With Metabolic Syndrome: 24-week, Multi-center, Randomized, Double-blind, Phase 4 Study [NCT02480465]Phase 4248 participants (Anticipated)Interventional2015-01-31Recruiting
Empagliflozin Versus Sitagliptin Therapy for Improvement of Myocardial Perfusion Reserve in Diabetic Patients With Coronary Artery disease_ELITE Trial [NCT03208465]Phase 4100 participants (Actual)Interventional2017-08-07Completed
The Effect of Liraglutide Compared to Sitagliptin, Both in Combination With Metformin in Subjects With Type 2 Diabetes. A 26-week, Randomised, Open-label, Active Comparator, Three-armed, Parallel-group, Multi-centre, Multinational Trial With a 52-week Ext [NCT00700817]Phase 3665 participants (Actual)Interventional2008-06-30Completed
Single Dose Crossover Comparative Bioavailability Study of Sitagliptin/Metformin 50 mg/1000 mg Film-coated Tablets in Healthy Male and Female Volunteers / Fed State [NCT05549583]Phase 126 participants (Actual)Interventional2018-04-15Completed
Exploring Effective and Safety Therapies Which Protect Islet β Cell on Newly Diagnosed Type 2 Diabetes Patients With High Glucose Toxicity [NCT03180281]135 participants (Anticipated)Interventional2017-07-01Not yet recruiting
A Phase III, Multicenter, Open-label Long-term Treatment Trial to Assess the Safety and Efficacy of Addition of Ipragliflozin in Japanese Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Sitagliptin Monotherapy in Addition to [NCT02564211]Phase 377 participants (Actual)Interventional2015-10-26Completed
Effect of DPP-4I and Related Treatment on Non-alcoholic Fatty Liver Disease [NCT05480007]68 participants (Actual)Interventional2011-01-30Completed
Role of Alpha-cell GLP-1 in the Beta-cell Response to DPP-4 Inhibition [NCT02683187]Phase 140 participants (Actual)Interventional2017-03-01Completed
A Phase III, Multicenter, Randomized, Double-Blind, Active-Comparator Controlled Clinical Trial to Study the Safety and Efficacy of the Addition of Sitagliptin Compared With the Addition of Dapagliflozin in Subjects With Type 2 Diabetes Mellitus and Mild [NCT02532855]Phase 3614 participants (Actual)Interventional2015-10-20Completed
An Open-label, Randomized,Three-way Cross-over, Single Dose Study to Explore the Effect of DPP-4 Inhibitors on β-cell Function by Using the Two-step Hyperglycemic Clamp [NCT02386943]Phase 412 participants (Anticipated)Interventional2013-12-31Recruiting
The Effect of Dipeptidyl Peptidase 4 Inhibition on Growth Hormone Secretion in Women With Polycystic Ovarian Syndrome [NCT02122380]Phase 423 participants (Actual)Interventional2016-02-29Completed
A Phase 1 Clinical Trial to Compare and Evaluate the Safety and Pharmacokinetic Characteristics After Administration of Fixed-dose Combination of DW6012 and Loose-combination of Each Component in Healthy Adult Volunteers [NCT05403281]Phase 141 participants (Actual)Interventional2021-11-05Completed
A Safety, Tolerability, Pharmacokinetic, and Pharmacodynamic Study of LY3325656 After Single Dose in Healthy Subjects and Patients With Type 2 Diabetes [NCT03115099]Phase 180 participants (Actual)Interventional2017-05-31Completed
Phase II Trial of Inhibition of Dipeptidyl Peptidase (DPP)-4 With Sitagliptin for the Prevention of Acute Graft Versus-Host Disease Following Allogeneic Hematopoietic Stem Cell Transplantation [NCT02683525]Phase 237 participants (Actual)Interventional2016-02-03Completed
A 28-Day Multiple Dose Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of K-757 in Healthy Overweight/Obese Volunteers [NCT05900531]Phase 160 participants (Actual)Interventional2022-09-21Completed
Dipeptidyl Peptidase-4 Inhibition and Narrow-band Ultraviolet-B Light in Psoriasis (DINUP): A Randomised Clinical Trial [NCT02347501]Phase 2118 participants (Actual)Interventional2013-11-30Completed
Influence of Gut Hormones on Food Intake After Roux-en-Y Gastric Bypass Surgery [NCT02336659]12 participants (Actual)Interventional2014-04-30Completed
A Double Blind, Randomized, Placebo Controlled Study to Determine the Physiological Effectiveness of Januvia for Reducing Inflammation and Increasing EPC Number in HIV Infected Men and Women With Insulin Resistance and Central Adiposity. [NCT01552694]Phase 338 participants (Actual)Interventional2012-10-31Completed
A Multicenter, Randomized, Double-Blind, Placebo- and Active-Controlled, Phase 3 Study to Evaluate the Efficacy and Safety of TAK-875 25 mg and 50 mg Compared to Placebo and Sitagliptin 100 mg When Used in Combination With Metformin in Subjects With Type [NCT01549964]Phase 3916 participants (Actual)Interventional2012-04-30Terminated(stopped due to Due to concerns about potential liver safety (See Detailed Description))
A Randomized, Double-Blind, Placebo-Controlled, Crossover Study To Evaluate The Effects of Sitagliptin on Postprandial Plasma Lipoprotein Concentrations in Men With Type 2 Diabetes [NCT00660075]Phase 336 participants (Actual)Interventional2008-02-29Completed
Sitagliptin (®Januvia) Regulation of Intestinal and Hepatic Lipoprotein Particle and Hepatic Glucose Production in Humans [NCT01600703]Phase 2/Phase 321 participants (Actual)Interventional2012-07-31Completed
An Open-Label, Randomized, 2-Period, Single-Dose, Balanced, Crossover Study in Healthy Subjects to Establish the Bioequivalence of Tablet Formulations Containing the Anhydrous and Monohydrate (FMI) Forms of MK0431 [NCT00944450]Phase 112 participants (Actual)Interventional2004-08-31Completed
A Phase 3, Multicenter, Randomized, Double-Blind, Active-Controlled, 24-Week Study to Evaluate the Efficacy and Safety of Daily Oral TAK-875 50 mg Compared With Sitagliptin 100 mg When Used in Combination With Metformin in Subjects With Type 2 Diabetes [NCT01834274]Phase 396 participants (Actual)Interventional2013-06-30Terminated(stopped due to Due to potential concerns about liver safety (See Detailed Description))
A Phase III, Multicenter, Randomized, Double-Blind, Placebo-Controlled Clinical Trial in China to Study the Safety and Efficacy of the Addition of Sitagliptin in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Sulfonylurea T [NCT01590771]Phase 3498 participants (Actual)Interventional2012-07-09Completed
A Multi-Center, Adaptive Phase 2, Randomized, Double-Blind, Placebo- and Active-Controlled (Sitagliptin), Parallel Group Study to Evaluate the Safety and Efficacy of TTP399 Following 6 Months Administration in Subjects With Type 2 Diabetes Mellitus on A S [NCT02405260]Phase 2190 participants (Actual)Interventional2015-03-31Completed
A Phase II, Randomized, Placebo-Controlled, Parallel-group, Double-Blind, Dose Response Finding Clinical Trial to Study the Efficacy and Safety of MK-0431/ONO-5435 in Japanese Subjects With Impaired Glucose Tolerance Who Have Inadequate Glycemic Control o [NCT01405911]Phase 2242 participants (Actual)Interventional2011-08-16Completed
China Multi-regional Clinical Trial: Efficacy and Safety of Oral Semaglutide Versus Sitagliptin in Subjects With Type 2 Diabetes Mellitus Treated With Metformin [NCT04017832]Phase 31,441 participants (Actual)Interventional2019-07-29Completed
Effect of Sitagliptin on Insulin Resistance and Myocardial Metabolism in Heart Failure [NCT00657280]Early Phase 116 participants (Actual)Interventional2008-04-30Completed
A Phase III, Multicenter, Randomized, Placebo- and Sitagliptin-controlled, Parallel-group, Double-blinded Study and Subsequent Open-label, Extension Study to Assess the Safety and Efficacy of MK-3102 in Japanese Patients With Type 2 Diabetes Mellitis Who [NCT01703221]Phase 3414 participants (Actual)Interventional2012-10-24Completed
The Effect of Dipeptidyl Peptidase IV Inhibition on Growth Hormone-Mediated Vasodilation [NCT01701973]Phase 444 participants (Actual)Interventional2013-01-31Completed
Study to Assess the Efficacy and Safety of Sitagliptin in Recently Diagnosed, Naive Type 2 Diabetics With Inadequate Glycemic Control on Diet and Exercise [NCT00832390]Phase 429 participants (Actual)Interventional2007-02-14Completed
A Multicenter, Randomized, Active-Controlled, Open-label Clinical Trial to Evaluate the Safety and Efficacy of Glimepiride, Gliclazide, Repaglinide or Acarbose as a Third OAHA on Top of Sitagliptin+Metformin Combination Therapy in Chinese Patients With Ty [NCT01709305]Phase 45,570 participants (Actual)Interventional2012-11-08Completed
A Trial Comparing Efficacy and Safety of NN1250 With Sitagliptin in Insulin Naive Subjects With Type 2 Diabetes (BEGIN™ : EARLY) [NCT01046110]Phase 3458 participants (Actual)Interventional2010-01-31Completed
An Open-label Study to Assess the Safety and Tolerability of MK-0431D for the Treatment of Patients With Type 2 Diabetes Mellitus (T2DM) With Inadequate Glycemic Control on Metformin Monotherapy [NCT01702298]Phase 342 participants (Actual)Interventional2012-12-07Completed
An Oral Single-dose, Randomized, Balanced, Open-label, Two-sequence, Two-treatment, Two-period, Crossover Bioequivalence Study of Sitagliptin Hydrochloride / Metformin Hydrochloride Extended-release Film Coated Tablets 100 mg /1000 mg (FDC) of Galenicum H [NCT06124573]Phase 148 participants (Actual)Interventional2022-11-07Completed
An Oral Single-dose, Randomized, Balanced, Open-label, Two-sequence, Two-treatment, Two-period, Crossover Bioequivalence Study of Sitagliptin Hydrochloride / Metformin Hydrochloride Extended-release Film Coated Tablets 100 mg /1000 mg (FDC) of Galenicum H [NCT06124560]Phase 158 participants (Actual)Interventional2022-10-28Completed
An Oral Single-dose, Randomized, Balanced, Open-label, Two-sequence, Two-treatment, Two-period, Crossover Bioequivalence Study of Sitagliptin Hydrochloride / Metformin Hydrochloride Extended Release Film Coated Tablets 50 mg / 500 mg (FDC) of Galenicum He [NCT06124547]Phase 148 participants (Actual)Interventional2023-01-16Completed
An Oral Single-dose, Randomized, Balanced, Open-label, Two-sequence, Two-treatment, Two-period, Crossover Bioequivalence Study of Sitagliptin Hydrochloride / Metformin Hydrochloride Extended-release Film Coated Tablets 50 mg / 500 mg (FDC) of Galenicum He [NCT06124495]Phase 158 participants (Actual)Interventional2023-01-13Completed
A Multicenter, Randomized, Double-Blind Study to Evaluate the Safety and Efficacy of MK0431 Monotherapy in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control [NCT00087516]Phase 3741 participants (Actual)Interventional2004-06-30Completed
Safety and Efficacy of Sitagliptin, Vildagliptin, and Metformin in Recently Diagnosed Drug-naïve Patients With Type 2 Diabetes [NCT04916093]Phase 460 participants (Actual)Interventional2019-12-20Completed
Comparison of the FGM Profiles in Patients of Type 2 Diabetes Treated With Sitagliptin and Acarbose [NCT05035849]60 participants (Actual)Interventional2020-01-30Completed
An Open Label Randomized Control Trial to Compare the Safety and Efficacy of Dapagliflozin Plus Metformin Versus Sitagliptin Plus Metformin for Treatment of Diabetes in Patients With Compensated and Stable Decompensated Cirrhosis [NCT06147518]240 participants (Anticipated)Interventional2023-12-20Not yet recruiting
Prospective, Randomized, Double Blind, Parallel Group, Two Arm, Comparative, Multicenter, Clinical Study to Compare Efficacy and Safety of Oral CPL-2009-0031 140 mg of Cadila Pharmaceutical Limited, India Against Innovator Sitagliptin 100 mg in Patients W [NCT04801199]Phase 3355 participants (Actual)Interventional2020-01-26Completed
Use of Sitagliptin for Stress Hyperglycemia or Mild Diabetes Following Cardiac Surgery [NCT01970462]Phase 48 participants (Actual)Interventional2014-01-31Terminated(stopped due to Recruitment)
Study to Evaluate the Effect of LY2189265 on Sitagliptin Pharmacokinetics in Patients With Type 2 Diabetes Mellitus [NCT01408888]Phase 129 participants (Actual)Interventional2011-08-31Completed
Effect of Canagliflozin on Cardiac Microcirculation Function in Patients With Type 2 Diabetes Mellitus Complicated With Cardiovascular Risk Factors [NCT05367063]Phase 470 participants (Anticipated)Interventional2022-01-05Recruiting
Sitagliptin Dose Determination Study in Type 1 Diabetes [NCT01530178]Phase 48 participants (Actual)Interventional2011-11-30Completed
A Randomized, Placebo-Controlled Double-Blind Trial Using Sitagliptin as a Treatment to Prevent New Onset Diabetes After Kidney Transplantation: A Pilot Study [NCT00936663]Phase 43 participants (Actual)Interventional2009-07-06Terminated(stopped due to lack of funding)
A Pooled Analysis of the Safety and Efficacy of MK-0431A and MK-0431A XR in Pediatric Patients With Type 2 Diabetes Mellitus With Inadequate Glycemic Control on Metformin Therapy (Alone or in Combination With Insulin) [NCT01760447]Phase 3223 participants (Actual)Interventional2011-12-07Completed
A Phase 3, Randomized, Active Comparator, Double-Blind, Multi-Center Study to Compare the Efficacy, Safety and Tolerability of ITCA 650 to Sitagliptin as Add-on Therapy to Metformin in Patients With Type 2 Diabetes [NCT01455909]Phase 30 participants (Actual)Interventional2013-02-28Withdrawn
A Study to Assess and Compare the Pharmacokinetic and Pharmacodynamic Profiles for Sitagliptin, Saxagliptin and Vildagliptin in Patients With Type 2 Diabetes Mellitus [NCT01582308]Phase 122 participants (Actual)Interventional2012-06-21Completed
A Study to Assess the Pharmacokinetics and the Ability for Pediatric Patients With Type 2 Diabetes to Swallow MK-0431A XR Tablets [NCT01557504]Phase 125 participants (Actual)Interventional2012-07-18Completed
A 24 Week Randomised, Open Label, 3 Parallel-group Comparison of Once and Twice Daily Biphasic Insulin Aspart (BIAsp) 30 Plus Sitagliptin and Twice Daily BIAsp 30, All in Combination With Metformin in Insulin naïve Type 2 Diabetic Subjects Inadequately Co [NCT01519674]Phase 4582 participants (Actual)Interventional2012-06-30Completed
[NCT00901979]Phase 2693 participants (Actual)Interventional2009-04-30Completed
A 28-week Extension to a 24-week Multicenter, Randomized, Double-blind, Active-controlled Clinical Trial to Evaluate the Safety and Tolerability of Vildagliptin (50 mg qd) Versus Sitagliptin (25 mg qd) in Patients With Type 2 Diabetes and Severe Renal Ins [NCT00770081]Phase 375 participants (Actual)Interventional2008-09-30Completed
A Multi-center, Randomized, Double-blind, Active-controlled Clinical Trial to Evaluate the Safety and Tolerability of 24 Weeks Treatment With Vildagliptin (50 mg qd) Versus Sitagliptin (25 mg qd) in Patients With Type 2 Diabetes and Severe Renal Insuffici [NCT00616811]Phase 3148 participants (Actual)Interventional2008-01-31Completed
A Phase III, Multicenter, Randomized, Double-Blind, Placebo-Controlled Clinical Trial to Study the Efficacy and Safety of the Continuation of Sitagliptin Compared With the Withdrawal of Sitagliptin During Initiation and Titration of Insulin Glargine (LANT [NCT02738879]Phase 3746 participants (Actual)Interventional2016-05-09Completed
Dipeptidyl Peptidase-4 (DPP-4) Inhibitor Sitagliptin Improved Beta Cell Function and Prevented a Conversion Rate to Impaired Glucose Tolerance IGT and Type 2 Diabetes T2D in Metformin Intolerant Obese Women With Polycystic Ovary Syndrome PCOS [NCT03122041]Phase 430 participants (Actual)Interventional2016-08-31Completed
The Impact of Sitagliptin as an Add on Therapy With Closed Loop Control in Adolescents With Type 1 Diabetes Mellitus and Diabetic Nephropathy [NCT06115460]Phase 346 participants (Actual)Interventional2022-03-01Completed
A Phase III, Multicenter, Double-Blind, Randomized, Placebo-Controlled Clinical Trial to Evaluate the Safety and Efficacy of Sitagliptin in Pediatric Patients With Type 2 Diabetes Mellitus With Inadequate Glycemic Control [NCT01485614]Phase 3200 participants (Actual)Interventional2012-02-10Completed
Retrospective and Multicenter Study of Real-world Evidence With SGLT2i (Dapagliflozin) and DPP4i (Sitagliptin) in Type 2 Diabetes Patients in Spain [NCT04149067]1,080 participants (Actual)Observational2017-06-05Completed
A Phase III, Randomized, Placebo and Active-Controlled, Double-Blind Clinical Trial to Study the Efficacy and Safety of the Addition of Metformin in Japanese Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Diet/Exercise Ther [NCT01545388]Phase 3337 participants (Actual)Interventional2012-02-23Completed
An Individualized treatMent aPproach for oldER patIents: A Randomized, Controlled stUdy in Type 2 Diabetes Mellitus (IMPERIUM) [NCT02072096]Phase 4192 participants (Actual)Interventional2014-02-28Terminated(stopped due to The trial was terminated per protocol because of lack of feasibility.)
A Randomized, Placebo Controlled, Repeat Dose, Double Blind (Sponsor Unblind) Study Investigating Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of GSK2330672 Administered With Metformin to Type 2 Diabetes Patients [NCT02202161]Phase 270 participants (Actual)Interventional2014-08-27Completed
A Randomized, Crossover Design Study of Acute and Chronic Effects of Sitagliptin on Endothelial Function in Humans With Type 2 Diabetes on Background Metformin [NCT01859793]Phase 438 participants (Actual)Interventional2013-06-30Completed
A Randomized Pilot Study Evaluating Combination Dipeptidyl Peptidase-4 Inhibitor Sitagliptin Plus Metformin Compared to Metformin Monotherapy and Placebo on Metabolic Abnormalities in Women With a Recent History of GDM [NCT01856907]Phase 436 participants (Actual)Interventional2013-09-28Completed
A Multi-center, Randomized, Open-label, Phase IV Study to Investigate the Management of Pasireotide-induced Hyperglycemia With Incretin Based Therapy or Insulin in Adult Patients With Cushing's Disease or Acromegaly [NCT02060383]Phase 4249 participants (Actual)Interventional2014-05-23Completed
A Phase 2, Double-Blind, Placebo-Controlled Trial to Evaluate the Safety and Efficacy of LY2409021 Compared to Sitagliptin in Subjects With Type 2 Diabetes Mellitus [NCT02111096]Phase 2174 participants (Actual)Interventional2014-04-30Terminated(stopped due to The overall benefit-risk profile did not support continued development of LY2409021 for type 2 diabetes.)
A Phase III, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Clinical Trial to Evaluate the Safety and Efficacy of Ertugliflozin (MK-8835/PF-04971729) in the Treatment of Subjects With Type 2 Diabetes Mellitus Who Have Inadequate [NCT02036515]Phase 3464 participants (Actual)Interventional2014-03-12Completed
Randomized Controlled Trial on the Safety and Efficacy of Sitagliptin Therapy for the Inpatient Management of General Medicine and Surgery Patients With Type 2 Diabetes [NCT01845831]Phase 4292 participants (Actual)Interventional2013-08-31Completed
A Phase III, Multicenter, Double-Blind, Randomized Study to Evaluate the Safety and Efficacy of the Addition of MK-3102 Compared With the Addition of Sitagliptin in Subjects With Type 2 Diabetes Mellitus With Inadequate Glycemic Control on Metformin [NCT01841697]Phase 3642 participants (Actual)Interventional2013-06-13Completed
Dipeptidyl Peptidase-4 Inhibition in Psoriasis Patients With Diabetes (DIP): A Randomized Clinical Trial. [NCT01991197]Phase 220 participants (Actual)Interventional2014-04-30Completed
A Placebo- and Active-controlled, Randomised, Double-blind, Dose-escalation Phase I Study of IDG-16177 for the Evaluation of Its Safety and Pharmacokinetics With the Exploration on Its Pharmacodynamics and Efficacy [NCT04982705]Phase 194 participants (Anticipated)Interventional2021-07-07Recruiting
A Randomized, Double-blind, Active Control, Parallel Group, Exploratory Phase IV Study to Compare the Effects of Tenelia® or Januvia® on Glucose Variability in add-on to Metformin in Patients With Inadequately Controlled Type2 Diabetes Mellitus in Metform [NCT02512523]Phase 440 participants (Anticipated)Interventional2015-08-31Recruiting
Degradation of the Anorexic Hormone Peptide YY [NCT02493959]Early Phase 18 participants (Actual)Interventional2014-05-31Completed
Pilot Project Evaluation of the DPP-4 Inhibition With Sitagliptin on Calcium and Bone Metabolism in Patients With Type 2 Diabetes Mellitus [NCT02444364]Early Phase 10 participants (Actual)Interventional2015-05-31Withdrawn(stopped due to Funding withdrawn; no participants enrolled.)
A Phase IV, Open Label, Randomized Trial on the Effect of Metformin Plus Lantus Insulin, Pioglitazone, or DPP4 Inhibitor on Fatty Liver in Patients With Type II Diabetes [NCT02365233]Phase 45 participants (Actual)Interventional2013-05-01Terminated(stopped due to IRB withheld the data due to inadequate supporting documentation)
A Phase III, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multicenter Clinical Trial to Evaluate the Efficacy and Safety of the Initial Combination of Ertugliflozin (MK-8835/PF-04971729) With Sitagliptin in the Treatment of Subjects With [NCT02226003]Phase 3291 participants (Actual)Interventional2014-09-23Completed
Efficacy and Safety of Switching From Sitagliptin to Liraglutide in Subjects With Type 2 Diabetes Not Achieving Adequate Glycaemic Control on Sitagliptin and Metformin [NCT01907854]Phase 4407 participants (Actual)Interventional2013-12-02Completed
A Randomized, Long-Term, Open-Label, 3-Arm, Multicenter Study to Compare the Glycemic Effects, Safety, and Tolerability of Exenatide Once Weekly Suspension to Sitagliptin and Placebo in Subjects With Type 2 Diabetes Mellitus [NCT01652729]Phase 3365 participants (Actual)Interventional2013-02-28Completed
Safety and Efficacy of Semaglutide Once Weekly Versus Sitagliptin Once Daily, Both as Monotherapy in Japanese Subjects With Type 2 Diabetes [NCT02254291]Phase 3308 participants (Actual)Interventional2014-10-02Completed
A Randomized, Open-label, Comparative Clinical Trial to Study the Efficacy of Sitagliptin and Glibenclamide in a Short Term Treatment on the Daily Glucose Variability Using Continuous Glucose Monitoring (CGM) in Japanese Patients With Type 2 Diabetes Mell [NCT02318693]Phase 453 participants (Actual)Interventional2015-02-04Completed
A Multicenter Phase II Trial of Inhibition of CD26 Peptidase Using Sitagliptin to Enhance Engraftment After Umbilical Cord Blood Transplantation for Adults With Hematological Malignancies [NCT01720264]Phase 215 participants (Actual)Interventional2012-11-02Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00086502 (2) [back to overview]Change From Baseline in FPG (Fasting Plasma Glucose) at Week 24
NCT00086502 (2) [back to overview]Change From Baseline in HbA1c (Hemoglobin A1C) at Week 24
NCT00086515 (3) [back to overview]Change From Baseline in Hemoglobin A1C (A1C) at Week 24
NCT00086515 (3) [back to overview]Change From Baseline in 2-hour Post-meal Glucose (PMG) at Week 24
NCT00086515 (3) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24
NCT00087516 (6) [back to overview]Change From Baseline in A1C at Week 24
NCT00087516 (6) [back to overview]Change From Baseline in A1C at Week 104
NCT00087516 (6) [back to overview]Change From Baseline in FPG at Week 104
NCT00087516 (6) [back to overview]Change From Baseline in FPG at Week 24
NCT00087516 (6) [back to overview]Change From Baseline in 2-hour Post-meal Glucose (2-hr PMG) at Week 24
NCT00087516 (6) [back to overview]Change From Baseline in 2-hr PMG at Week 104
NCT00094757 (4) [back to overview]Change From Baseline in FPG at Week 18
NCT00094757 (4) [back to overview]Change From Baseline in A1C at Week 18
NCT00094757 (4) [back to overview]Change From Baseline in A1C at Week 54
NCT00094757 (4) [back to overview]Change From Baseline in FPG at Week 54
NCT00094770 (12) [back to overview]Number of Participants With Laboratory Adverse Experiences (LAEs) at Week 104
NCT00094770 (12) [back to overview]Number of Participants With Drug-related CAEs at Week 104
NCT00094770 (12) [back to overview]Number of Participants With Clinical Adverse Experiences (CAEs) at Week 104
NCT00094770 (12) [back to overview]Change From Baseline in HbA1c at Week 104
NCT00094770 (12) [back to overview]Hypoglycemic Events at Week 104
NCT00094770 (12) [back to overview]Number of Participants With Drug-related LAEs at Week 104
NCT00094770 (12) [back to overview]Change From Baseline in HbA1c at Week 52
NCT00094770 (12) [back to overview]Change From Baseline in Body Weight at Week 52
NCT00094770 (12) [back to overview]Change From Baseline in Body Weight at Week 104
NCT00094770 (12) [back to overview]Hypoglycemic Events at Week 52
NCT00094770 (12) [back to overview]Number of Participants With Serious LAEs at Week 104
NCT00094770 (12) [back to overview]Number of Participants With Serious CAEs at Week 104
NCT00095056 (2) [back to overview]Safety and Tolerability of Sitagliptin After 12 Weeks of Treatment
NCT00095056 (2) [back to overview]Safety and Tolerability of Sitagliptin Over 54 Weeks
NCT00103857 (9) [back to overview]Change From Baseline in HbA1c (Hemoglobin A1C) at Week 24
NCT00103857 (9) [back to overview]Change From Baseline in FPG (Fasting Plasma Glucose) at Week 24
NCT00103857 (9) [back to overview]Change From Baseline in 2-Hour PMG (Post-Meal Glucose) at Week 24
NCT00103857 (9) [back to overview]Change From Baseline in 2-Hour PMG (Post-Meal Glucose) at Week 104
NCT00103857 (9) [back to overview]Change From Baseline in 2-Hour PMG (Post-Meal Glucose) at Week 54
NCT00103857 (9) [back to overview]Change From Baseline in FPG (Fasting Plasma Glucose) at Week 104
NCT00103857 (9) [back to overview]Change From Baseline in HbA1c (Hemoglobin A1C) at Week 104
NCT00103857 (9) [back to overview]Change From Baseline in FPG (Fasting Plasma Glucose) at Week 54
NCT00103857 (9) [back to overview]Change From Baseline in HbA1c (Hemoglobin A1C) at Week 54
NCT00106704 (2) [back to overview]Change From Baseline in A1C at Week 24
NCT00106704 (2) [back to overview]Change From Baseline in FPG at Week 24
NCT00127192 (3) [back to overview]Change From Baseline in Fasting Plasma Glucose at Week 12
NCT00127192 (3) [back to overview]Change From Baseline in Glycosylated Albumin at Week 12
NCT00127192 (3) [back to overview]Change From Baseline in HbA1c at Week 12
NCT00289848 (3) [back to overview]Change From Baseline in 2-hr Post-Meal Glucose (PMG) at Week 18
NCT00289848 (3) [back to overview]Change From Baseline in Hemoglobin A1c (HbA1c) at Week 18
NCT00289848 (3) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 18
NCT00305604 (4) [back to overview]Rapidity of Onset of Action as Determined by Home Glucose Monitoring After 1 Week
NCT00305604 (4) [back to overview]Change From Baseline in HbA1c (Hemoglobin A1c) at Week 24
NCT00305604 (4) [back to overview]Change From Baseline in FPG (Fasting Plasma Glucose) at Week 24
NCT00305604 (4) [back to overview]Change From Baseline in 2-hour PPG (Post-prandial Glucose) at Week 24
NCT00337610 (4) [back to overview]Change From Baseline in 2 Hr-PMG at Week 18
NCT00337610 (4) [back to overview]Change From Baseline in FPG at Week 18
NCT00337610 (4) [back to overview]Change From Baseline in A1C at Week 30
NCT00337610 (4) [back to overview]Change From Baseline in A1C at Week 18
NCT00350779 (6) [back to overview]Change From Baseline in 2-hour PMG (Post-meal Glucose) at Week 18
NCT00350779 (6) [back to overview]Change From Baseline in 2-hour PMG (Post-meal Glucose) at Week 54
NCT00350779 (6) [back to overview]Change From Baseline in FPG (Fasting Plasma Glucose) at Week 18
NCT00350779 (6) [back to overview]Change From Baseline in FPG (Fasting Plasma Glucose) at Week 54
NCT00350779 (6) [back to overview]Change From Baseline in HbA1c (Hemoglobin A1C) at Week 54
NCT00350779 (6) [back to overview]Change From Baseline in HbA1c (Hemoglobin A1C) at Week 18
NCT00364377 (1) [back to overview]Lowering of Fasting Glucose
NCT00372060 (4) [back to overview]Change From Baseline in 2 Hour Postprandial Glucose at Week 12
NCT00372060 (4) [back to overview]Change From Baseline in Fasting Plasma Glucose at Week 12
NCT00372060 (4) [back to overview]Change From Baseline in Hemoglobin A1c (HbA1c ) at Week 12
NCT00372060 (4) [back to overview]Change From Baseline in Hemoglobin A1c (HbA1c ) at Week 52
NCT00395343 (7) [back to overview]Percent of Patients With A1C < 7.0% at Week 24
NCT00395343 (7) [back to overview]Percent of Patients With A1C < 6.5% at Week 24
NCT00395343 (7) [back to overview]Change From Baseline in A1C at Week 24
NCT00395343 (7) [back to overview]Change From Baseline in A1C at Week 24
NCT00395343 (7) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24
NCT00395343 (7) [back to overview]Change From Baseline in 2-hour Post-meal Glucose (PMG) at Week 24
NCT00395343 (7) [back to overview]Percent Change From Baseline in Index of Static Beta-Cell Sensitivity to Glucose at Week 24
NCT00397631 (3) [back to overview]Change From Baseline in HbA1c (Hemoglobin A1C) at Week 24
NCT00397631 (3) [back to overview]Change From Baseline in FPG (Fasting Plasma Glucose) at Week 24
NCT00397631 (3) [back to overview]Change From Baseline in 2-hour PPG (Post-prandial Glucose) at Week 24
NCT00411411 (2) [back to overview]Restoration of the Insulinotropic Effect of GIP
NCT00411411 (2) [back to overview]the Relative Increase in Meal-induced Total GLP-1 Secretion
NCT00411554 (3) [back to overview]Change From Baseline in Fasting Plasma Glucose at Week 12
NCT00411554 (3) [back to overview]Change From Baseline in 2 Hour Postprandial Glucose at Week 12
NCT00411554 (3) [back to overview]Change From Baseline in HbA1c at Week 12
NCT00420511 (3) [back to overview]Fasting Blood Glucose at 48 Weeks
NCT00420511 (3) [back to overview]Insulinogenic Index Divided by HOMA-IR at 48 Weeks
NCT00420511 (3) [back to overview]Preservation of Beta-cell Function Measured by Area-under-the-curve (C-peptide/Glucose)/HOMA-IR
NCT00449930 (5) [back to overview]Number of Patients Who Reported 1 or More Episodes of the Adverse Experience of Diarrhea
NCT00449930 (5) [back to overview]Number of Patients Who Reported 1 or More Episodes of the Adverse Experience of Nausea
NCT00449930 (5) [back to overview]Number of Patients Who Reported 1 or More Episodes of the Adverse Experience of Vomiting
NCT00449930 (5) [back to overview]Number of Patients Who Reported 1 or More Episodes of the Adverse Experience of Abdominal Pain
NCT00449930 (5) [back to overview]Change From Baseline in Hemoglobin A1c (HbA1c) at Week 24
NCT00482729 (5) [back to overview]Change From Baseline in A1C at Week 44
NCT00482729 (5) [back to overview]Number of Patients With A1C < 7.0% at Week 44
NCT00482729 (5) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 18
NCT00482729 (5) [back to overview]Change From Baseline in Hemoglobin A1c (A1C) at Week 18
NCT00482729 (5) [back to overview]Number of Patients With A1C < 7.0% at Week 18
NCT00484419 (18) [back to overview]Change in Fasting Plasma Glucose (FPG) From Week 0(Baseline) to Week 8 Least Squares Mean
NCT00484419 (18) [back to overview]Change in Fasting Insulin From Week 0(Baseline) to Week 16 Least Squares Mean
NCT00484419 (18) [back to overview]Change in Fasting Insulin From Week 0(Baseline) to Week 8 Least Squares Mean
NCT00484419 (18) [back to overview]Change in FPG From Week 0(Baseline) to Week 16 Least Squares Mean
NCT00484419 (18) [back to overview]Change in Low-Density Lipoprotein-C(LDL-C) From Week 0(Baseline) to Week 16 Least Squares Mean
NCT00484419 (18) [back to overview]Change in Post-prandial Glucose From Week 0(Baseline) to Week 16 Least Squares Mean
NCT00484419 (18) [back to overview]Mean Change in Fasting Insulin From Week 0(Baseline) to Week 16
NCT00484419 (18) [back to overview]Mean Change in Fasting Insulin From Week 0(Baseline) to Week 8
NCT00484419 (18) [back to overview]Mean Change in FPG From Week 0(Baseline) to Week 16
NCT00484419 (18) [back to overview]Mean Change in FPG From Week 0(Baseline) to Week 8
NCT00484419 (18) [back to overview]Mean Change in LDL-C From Week 0(Baseline) to Week 16
NCT00484419 (18) [back to overview]Mean Change in Post-prandial Glucose From Week 0(Baseline) to Week 16
NCT00484419 (18) [back to overview]Mean Change in Post-prandial Insulin From Week 0(Baseline) to Week 16
NCT00484419 (18) [back to overview]Mean Percentage of Change in Glycosylated Hemoglobin (HbA1c) From Week 0(Baseline) to Week 16 Endpoint Least Squares Mean
NCT00484419 (18) [back to overview]Mean Percentage of Change in HbA1c From Week 0(Baseline) to Week 16 Endpoint
NCT00484419 (18) [back to overview]Mean Percentage of Change in HbA1c From Week 0(Baseline) to Week 8
NCT00484419 (18) [back to overview]Mean Percentage of Change in LDL-C Levels From Week 0(Baseline) to Week 16
NCT00484419 (18) [back to overview]Mean Percentage of Change in LDL-C Levels From Week 0(Baseline) to Week 16 (Least Squares Mean)
NCT00509236 (5) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG)
NCT00509236 (5) [back to overview]Change From Baseline in Hemoglobin A1c After Sitagliptin Treatment
NCT00509236 (5) [back to overview]Change From Baseline in Hemoglobin A1c for Sitagliptin Versus Glipizide Treatment
NCT00509236 (5) [back to overview]Number of Participants With Clinical Adverse Events
NCT00509236 (5) [back to overview]Number of Participants With Symptomatic Hypoglycemic Adverse Events
NCT00509262 (4) [back to overview]Percentage of Participants With Hypoglycemic Events
NCT00509262 (4) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 54
NCT00509262 (4) [back to overview]Change From Baseline in Body Weight at Week 54
NCT00509262 (4) [back to overview]Change From Baseline in Hemoglobin A1c (A1C) Levels at Week 54
NCT00511108 (3) [back to overview]Change From Baseline in Glucagon 3-hour Total Area Under the Curve (AUC) After 12 Weeks of Treatment
NCT00511108 (3) [back to overview]Change From Baseline in Glucose 5-hour Total AUC After 12 Weeks of Treatment
NCT00511108 (3) [back to overview]Percent Change From Baseline in Index of Static Beta-cell Sensitivity to Glucose After 12 Weeks of Treatment
NCT00532935 (5) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 1
NCT00532935 (5) [back to overview]Change From Baseline in A1C at Week 32
NCT00532935 (5) [back to overview]Change From Baseline in FPG at Week 32
NCT00532935 (5) [back to overview]Change From Baseline in 2-hour Post-Meal Glucose (PMG) at Week 32
NCT00532935 (5) [back to overview]Percent of Participants With A1C <7.0% at Week 32
NCT00541229 (1) [back to overview]24-hour Weighted Mean Glucose (WMG)
NCT00541450 (6) [back to overview]Change in Fasting Plasma Glucose (FPG) in Participants Treated With Sitagliptin or Pioglitazone at 12 Weeks
NCT00541450 (6) [back to overview]Change in Fasting Plasma Glucose (FPG) in the Sita/Met FDC or Pioglitazone Groups at 40 Weeks
NCT00541450 (6) [back to overview]Change in Hemoglobin A1c (A1C) in Participants Treated With Sitagliptin or Pioglitazone at 12 Weeks
NCT00541450 (6) [back to overview]Change in Hemoglobin A1c (A1C) in the Sita/Met Fixed-Dose Combination (FDC) or Pioglitazone Groups at 40 Weeks
NCT00541450 (6) [back to overview]Change in 2-hour Postprandial Glucose (PMG) in the Sita/Met FDC or Pioglitazone Groups at 40 Weeks
NCT00541450 (6) [back to overview]Change in 2-hour Postprandial Glucose (PMG) in Participants Treated With Sitagliptin or Pioglitazone at 12 Weeks
NCT00541775 (3) [back to overview]2-hour Post-meal Glucose (PMG) at Week 18
NCT00541775 (3) [back to overview]Hemoglobin A1C (A1C) at Week 18
NCT00541775 (3) [back to overview]Fasting Plasma Glucose (FPG) at Week 18
NCT00545584 (2) [back to overview]Fasting Plasma Glucose (FPG) Measurement
NCT00545584 (2) [back to overview]Hemoglobin A1c Measurement
NCT00631488 (5) [back to overview]Change From Baseline (BL) to Week 4 in 24-hour Weighted Mean Glucose (WMG) Levels
NCT00631488 (5) [back to overview]Change From BL to Week 4 in 2-hr Glucose Area Under The Curve (AUC)
NCT00631488 (5) [back to overview]Change From BL to Week 4 in Fasting Plasma Glucose (FPG)
NCT00631488 (5) [back to overview]Change From BL to Week 4 in the 2-Hour Total GLP-1 Total AUC
NCT00631488 (5) [back to overview]Change From BL to Week 4 in the 2-Hour Active GLP-1 Total AUC
NCT00637273 (12) [back to overview]Ratio of Fasting Triglycerides at Week 26 to Baseline
NCT00637273 (12) [back to overview]Assessment on Event Rate of Treatment-emergent Hypoglycemic Events
NCT00637273 (12) [back to overview]Change in Fasting Plasma Glucose From Baseline to Week 26
NCT00637273 (12) [back to overview]Change in Diastolic Blood Pressure From Baseline to Week 26
NCT00637273 (12) [back to overview]Change in Fasting Total Cholesterol From Baseline to Week 26
NCT00637273 (12) [back to overview]Change in HbA1c From Baseline to Week 26
NCT00637273 (12) [back to overview]Change in Systolic Blood Pressure From Baseline to Week 26
NCT00637273 (12) [back to overview]Change in Body Weight From Baseline to Week 26
NCT00637273 (12) [back to overview]Change in Fasting High-density Lipoprotein (HDL) From Baseline to Week 26
NCT00637273 (12) [back to overview]Percentage of Subjects Achieving HbA1c Target of <=6.0% at Week 26
NCT00637273 (12) [back to overview]Percentage of Subjects Achieving HbA1c Target of <=6.5% at Week 26
NCT00637273 (12) [back to overview]Percentage of Subjects Achieving HbA1c Target of <7% at Week 26
NCT00642278 (6) [back to overview]Absolute Change in Body Weight From Baseline to Week 12
NCT00642278 (6) [back to overview]Change in Overnight Urine Glucose/Creatinine Ratio From Baseline to Week 12
NCT00642278 (6) [back to overview]Percent Change in Body Weight From Baseline to Week 12
NCT00642278 (6) [back to overview]Percentage of Patients With Symptoms of Hypoglycemia
NCT00642278 (6) [back to overview]Change in Fasting Plasma Glucose (FPG) From Baseline to Week 12
NCT00642278 (6) [back to overview]Change in HbA1c From Baseline to Week 12
NCT00657280 (1) [back to overview]Determine the Effects of Sitagliptin on Myocardial Glucose Uptake Measured by Myocardial PET Scan
NCT00659711 (2) [back to overview]Change in Oxidative Stress From Baseline to 12 Weeks
NCT00659711 (2) [back to overview]Change in Reactive Oxygen Species (ROS) Generation by MNC, Protein and mRNA Expression of p47phox Subunit of NADPH Oxidase, in MNC's of Obese Type 2 Diabetic Patients
NCT00660075 (1) [back to overview]Measurement of the Area Under the Curve of Plasma Triglycerides (TG) Levels During Postprandial Period (Time 0,2,4,6,8 Hours)
NCT00666458 (4) [back to overview]Hemoglobin A1c (HbA1c) Change From Baseline to Week 18
NCT00666458 (4) [back to overview]Fasting Plasma Glucose Change From Baseline to Week 18 (mmol/L)
NCT00666458 (4) [back to overview]Fasting Plasma Glucose Change From Baseline to Week 18 (mg/dL)
NCT00666458 (4) [back to overview]Proportion of Patients Achieving Therapeutic Glycaemic Response Defined as HbA1c <= 6.5% at Week 18
NCT00666848 (2) [back to overview]Change in MAP During Sitagliptin
NCT00666848 (2) [back to overview]Change in MAP During Placebo
NCT00673894 (2) [back to overview]Fructosamine
NCT00673894 (2) [back to overview]Postprandial Glucose Area Under the Curve (AUC)
NCT00676338 (11) [back to overview]Assessment on Event Rate of Treatment-emergent Major Hypoglycemic Events
NCT00676338 (11) [back to overview]Assessment on Event Rate of Treatment-Emergent Minor Hypoglycemic Events
NCT00676338 (11) [back to overview]Change in Body Weight From Baseline to Week 26
NCT00676338 (11) [back to overview]Change in Diastolic Blood Pressure From Baseline to Week 26.
NCT00676338 (11) [back to overview]Change in Fasting High-Density Lipoprotein (HDL) From Baseline to Week 26
NCT00676338 (11) [back to overview]Percentage of Patients Achieving HbA1c <=7% at Week 26
NCT00676338 (11) [back to overview]Change in Systolic Blood Pressure From Baseline to Week 26.
NCT00676338 (11) [back to overview]Change in HbA1c From Baseline to Week 26
NCT00676338 (11) [back to overview]Change in Fasting Total Cholesterol (TC) From Baseline to Week 26
NCT00676338 (11) [back to overview]Change in Fasting Serum Glucose (FSG) From Baseline to Week 26
NCT00676338 (11) [back to overview]Ratio of Fasting Triglycerides at Week 26 to Baseline
NCT00686634 (4) [back to overview]Number of Subjects Maintaining Hemoglobin A1c 7.5% or Less by 1 Year
NCT00686634 (4) [back to overview]Number of Subjects With Hemoglobin A1c 7.5% or Less at 4 Months
NCT00686634 (4) [back to overview]Number of Adverse Events
NCT00686634 (4) [back to overview]Hemoglobin A1c (HbA1c) Change From Baseline
NCT00700817 (75) [back to overview]Percentage of Subjects Achieving Treatment Target of HbA1c < 7.0% at Week 78
NCT00700817 (75) [back to overview]Mean Change From Baseline in Tumour Necrosis Factor Alpha (TNF-alpha) at Week 26.
NCT00700817 (75) [back to overview]Mean Change From Baseline in Triglycerides (TG) at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Triglycerides (TG) at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in Total Cholesterol at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Fasting Plasma Glucose (FPG) at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in Diastolic Blood Pressure (DBP) at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Fasting Plasma Glucose (FPG) at Week 78
NCT00700817 (75) [back to overview]Mean Change From Baseline in Free Fatty Acids (FFA) at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in Free Fatty Acids (FFA) at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Glycosylated Haemoglobin A1c (HbA1c) at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in Glycosylated Haemoglobin A1c (HbA1c) at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Glycosylated Haemoglobin A1c (HbA1c) at Week 78
NCT00700817 (75) [back to overview]Mean Change From Baseline in Total Cholesterol at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in High-density Lipoprotein-cholesterol (HDL-C) at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in High-density Lipoprotein-cholesterol (HDL-C) at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Highly Sensitive C-reactive Protein (hsCRP) at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in Interleukin-6 (IL-6) at Week 26.
NCT00700817 (75) [back to overview]Mean Change From Baseline in Low-density Lipoprotein-cholesterol (LDL-C) at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in Low-density Lipoprotein-cholesterol (LDL-C) at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in N-terminal Pro B-type Natriuretic Peptide (NT-proBNP) at Week 26.
NCT00700817 (75) [back to overview]Mean Change From Baseline in Overall Treatment Satisfaction (OTS) at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in Overall Treatment Satisfaction (OTS) at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Diastolic Blood Pressure (DBP) at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in Body Weight at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Body Weight at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in Beta-cell Function at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Beta-cell Function at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in Apolipoprotein B at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Plasminogen Activator Inhibitor-1 (PAI-1) at Week 26.
NCT00700817 (75) [back to overview]Mean Change From Baseline in Pulse at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in Pulse at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Apolipoprotein B at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in Systolic Blood Pressure (SBP) at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in Systolic Blood Pressure (SBP) at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Adiponectin at Week 26.
NCT00700817 (75) [back to overview]Hypoglyceamic Episodes, Weeks 0-78
NCT00700817 (75) [back to overview]Hypoglyceamic Episodes, Weeks 0-52
NCT00700817 (75) [back to overview]Hypoglyceamic Episodes, Weeks 0-26
NCT00700817 (75) [back to overview]Hypoglycaemic Episodes (Excluding Outlier Subject), Weeks 0-78
NCT00700817 (75) [back to overview]Hypoglycaemic Episodes (Excluding Outlier Subject), Weeks 0-52
NCT00700817 (75) [back to overview]Hypoglycaemic Episodes (Excluding Outlier Subject), Weeks 0-26
NCT00700817 (75) [back to overview]Hypoglycaamic Episodes, Weeks 52-78
NCT00700817 (75) [back to overview]Percentage of Subjects Achieving Treatment Target of HbA1c =< 6.5% at Week 78
NCT00700817 (75) [back to overview]Percentage of Subjects Achieving Treatment Target of HbA1c =< 6.5% at Week 78
NCT00700817 (75) [back to overview]Percentage of Subjects Achieving Treatment Target of HbA1c =< 6.5% at Week 52
NCT00700817 (75) [back to overview]Percentage of Subjects Achieving Treatment Target of HbA1c =< 6.5% at Week 26
NCT00700817 (75) [back to overview]Percentage of Subjects Achieving Treatment Target of HbA1c < 7.0% at Week 78
NCT00700817 (75) [back to overview]Mean Change in Low-density Lipoprotein-cholesterol (LDL-C) From Week 52 to Week 78
NCT00700817 (75) [back to overview]Percentage of Subjects Achieving Treatment Target of HbA1c < 7.0% at Week 52
NCT00700817 (75) [back to overview]Percentage of Subjects Achieving Treatment Target of HbA1c < 7.0% at Week 26
NCT00700817 (75) [back to overview]Mean Change From Baseline in Fasting Plasma Glucose (FPG) at Week 52
NCT00700817 (75) [back to overview]Mean Change in Waist to Hip Ratio From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in Waist Circumference From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in Very Low-density Lipoprotein-cholesterol (VLDL-C) at Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in Triglycerides (TG) From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in Total Cholesterol From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in Systolic Blood Pressure (SBP) From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in Pulse From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in Overall Treatment Satisfaction (OTS) From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in High-density Lipoprotein-cholesterol (HDL-C) From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in Glycosylated Haemoglobin A1c (HbA1c) From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in Free Fatty Acids (FFA) From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in Fasting Plasma Glucose (FPG) From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in Diastolic Blood Pressure (DBP) From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in Body Weight From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in Beta-cell Function From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change in Apolipoprotein B From Week 52 to Week 78
NCT00700817 (75) [back to overview]Mean Change From Baseline in Waist to Hip Ratio at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Waist to Hip Ratio at Week 26.
NCT00700817 (75) [back to overview]Mean Change From Baseline in Waist Circumference at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Waist Circumference at Week 26.
NCT00700817 (75) [back to overview]Mean Change From Baseline in Von Willebrand Factor (vWf) at Week 26.
NCT00700817 (75) [back to overview]Mean Change From Baseline in Very Low-density Lipoprotein-cholesterol (VLDL-C) at Week 52
NCT00700817 (75) [back to overview]Mean Change From Baseline in Very Low-density Lipoprotein-cholesterol (VLDL-C) at Week 26
NCT00701090 (6) [back to overview]Change From Baseline in HbA1c at Week 30
NCT00701090 (6) [back to overview]Change From Baseline in FPG (Fasting Plasma Glucose) at Week 30
NCT00701090 (6) [back to overview]Change From Baseline in Body Weight at Week 30
NCT00701090 (6) [back to overview]Percent of Patients With at Least One Hypoglycemia Episode of Any Type at Week 30
NCT00701090 (6) [back to overview]Percent of Patients With A1C <7.0% at Week 30
NCT00701090 (6) [back to overview]Percent of Patients With A1C <6.5% at Week 30
NCT00704132 (1) [back to overview]Change From Baseline in Glucose 5-Hour Incremental AUC at Week 6
NCT00716092 (8) [back to overview]Weighted Mean Glucose (WMG) Change From Baseline at Day 28
NCT00716092 (8) [back to overview]Fasting Plasma Glucose (FPG) Change From Baseline at Day 28
NCT00716092 (8) [back to overview]Exploratory Sensitivity Analysis of the WMG Change From Baseline at Day 28
NCT00716092 (8) [back to overview]Exploratory Sensitivity Analysis of Plasma Glucose AUEC (0-3h) Change From Baseline at Day 28
NCT00716092 (8) [back to overview]Exploratory Sensitivity Analysis of GLP-1 AUEC (0-2h) Change From Baseline at Day 28
NCT00716092 (8) [back to overview]Plasma Glucose Area Under Effect Curve (AUEC) (0-3h) Change From Baseline at Day 28
NCT00716092 (8) [back to overview]Exploratory Sensitivity Analysis of FPG Change From Baseline at Day 28
NCT00716092 (8) [back to overview]GLP-1 (Glucagon Like Peptide 1) AUEC (0-2h) (Area Under Effect Curve) Change From Baseline at Day 28
NCT00722371 (6) [back to overview]Change From Baseline in 2-Hour PMG at Week 54
NCT00722371 (6) [back to overview]Change From Baseline in 2-Hour Post-meal Glucose (PMG) at Week 24
NCT00722371 (6) [back to overview]Change From Baseline in A1C at Week 54
NCT00722371 (6) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24
NCT00722371 (6) [back to overview]Change From Baseline in FPG at Week 54
NCT00722371 (6) [back to overview]Change From Baseline in Hemoglobin A1C (A1C) at Week 24
NCT00729326 (19) [back to overview]Percentage of Patients Experiencing Hypoglycemia (Overall)
NCT00729326 (19) [back to overview]Percentage of Patients Experiencing Hypoglycemia (Week 4 to Week 8)
NCT00729326 (19) [back to overview]Change in Postprandial Insulin AUC After the Morning Meal
NCT00729326 (19) [back to overview]Change in Postprandial Glucagon AUC Excursion After the Morning Meal
NCT00729326 (19) [back to overview]Change in Postprandial Glucagon Area Under the Concentration-time Curve (AUC) After the Morning Meal
NCT00729326 (19) [back to overview]Change in Postprandial C-peptide AUC Excursion After the Morning Meal
NCT00729326 (19) [back to overview]Change in Postprandial C-peptide AUC After the Morning Meal
NCT00729326 (19) [back to overview]Change in Postprandial Active GLP-1 AUC Excursion After the Monrning Meal
NCT00729326 (19) [back to overview]Change in Postprandial Active GLP-1 AUC After the Morning Meal
NCT00729326 (19) [back to overview]Change in Postprandial Insulin AUC Excursion After the Morning Meal
NCT00729326 (19) [back to overview]Change in Postprandial Triglyceride AUC After the Morning Meal
NCT00729326 (19) [back to overview]Change in Postprandial Triglyceride AUC Excursion After the Morning Meal
NCT00729326 (19) [back to overview]Change in Time-averaged Glucose During a 24 Hour Period
NCT00729326 (19) [back to overview]Change in Two-hour Postprandial Glucose After the Morning Meal
NCT00729326 (19) [back to overview]Episodes of Hypoglycemia (Baseline to Week 4)
NCT00729326 (19) [back to overview]Episodes of Hypoglycemia (Overall)
NCT00729326 (19) [back to overview]Episodes of Hypoglycemia (Week 4 to Week 8)
NCT00729326 (19) [back to overview]Percentage of Patients Experiencing Hypoglycemia (Baseline to Week 4)
NCT00729326 (19) [back to overview]Change in Fasting Blood Glucose After the Morning Meal
NCT00730275 (6) [back to overview]Number of Participants Who Experienced at Least One Adverse Event
NCT00730275 (6) [back to overview]Time of Occurence of Maximum Concentration (Tmax) Following a Single Dose of Sitagliptin
NCT00730275 (6) [back to overview]Plasma Dipeptidyl Peptidase-4 (DPP-4) Activity Following a Single Dose of Sitagliptin or Placebo
NCT00730275 (6) [back to overview]Maximum Concentration (Cmax) Following a Single Dose of Sitagliptin
NCT00730275 (6) [back to overview]Apparent Terminal Half-life (Apparent t1/2) Following a Single Dose of Sitagliptin
NCT00730275 (6) [back to overview]Area Under the Concentration-time Curve (AUC) From Time 0 to Infinity Following a Single Dose of Sitagliptin
NCT00734474 (33) [back to overview]Waist Circumference Change From Baseline
NCT00734474 (33) [back to overview]Participant-reported Outcomes, Impact of Weight on Quality of Life-Lite (IWQoL-Lite)
NCT00734474 (33) [back to overview]Antibodies to LY2189265
NCT00734474 (33) [back to overview]Change From Baseline in Body Weight at Dose Decision Point
NCT00734474 (33) [back to overview]Change From Baseline in Glycosylated Hemoglobin (HbA1c) at the Dose Decision Point
NCT00734474 (33) [back to overview]Change From Baseline in Pulse Rate at Dose Decision Point
NCT00734474 (33) [back to overview]Number of Participants With Adjudicated Pancreatitis at 104 Weeks
NCT00734474 (33) [back to overview]Number of Participants With Treatment-emergent Adverse Events at 104 Weeks
NCT00734474 (33) [back to overview]Number of Participants With Treatment-emergent Adverse Events at 52 Weeks
NCT00734474 (33) [back to overview]Glycosylated Hemoglobin (HbA1c) Change From Baseline
NCT00734474 (33) [back to overview]Number of Participants With Treatment-emergent Adverse Events at 26 Weeks
NCT00734474 (33) [back to overview]Pharmacokinetics of LY2189265: Area Under the Concentration-Time Curve
NCT00734474 (33) [back to overview]Beta Cell Function and Insulin Sensitivity (HOMA2)
NCT00734474 (33) [back to overview]Body Weight Change From Baseline
NCT00734474 (33) [back to overview]Change From Baseline in Blood Pressure
NCT00734474 (33) [back to overview]Change From Baseline in Electrocardiogram (ECG) Parameters, Fridericia-corrected QT (QTcF) and PR Interval
NCT00734474 (33) [back to overview]Change From Baseline in Pulse Rate
NCT00734474 (33) [back to overview]Durability of Change From Baseline Body Weight
NCT00734474 (33) [back to overview]Durability of Change From Baseline in Glycosylated Hemoglobin (HbA1c)
NCT00734474 (33) [back to overview]Fasting Blood Glucose Change From Baseline
NCT00734474 (33) [back to overview]Fasting Insulin Change From Baseline
NCT00734474 (33) [back to overview]Glycosylated Hemoglobin (HbA1c) Change From Baseline
NCT00734474 (33) [back to overview]Incidence of Hypoglycemic Episodes
NCT00734474 (33) [back to overview]Number of Participants With Treatment-emergent Abnormal Laboratory Tests at 104 Weeks
NCT00734474 (33) [back to overview]Number of Participants With Treatment-emergent Abnormal Laboratory Tests at 26 Weeks
NCT00734474 (33) [back to overview]Number of Participants With Adjudicated Cardiovascular Events at 104 Weeks
NCT00734474 (33) [back to overview]Change From Baseline in Blood Pressure at Dose Decision Point
NCT00734474 (33) [back to overview]Number of Participants With Treatment-emergent Abnormal Laboratory Tests at 52 Weeks
NCT00734474 (33) [back to overview]Number of Participants With Treatment-emergent Abnormal Lipid Tests
NCT00734474 (33) [back to overview]Participant-reported Outcomes, EQ-5D
NCT00734474 (33) [back to overview]Percentage of Participants Who Achieve Glycosylated Hemoglobin (HbA1c) <7% or ≤6.5%
NCT00734474 (33) [back to overview]Rate of Hypoglycemic Episodes
NCT00734474 (33) [back to overview]Resource Utilization
NCT00749190 (10) [back to overview]Change in Homeostasis Model Assessment Index for Insulin Resistance (HOMA-IR)
NCT00749190 (10) [back to overview]Change From Baseline in HbA1c After 12 Weeks of Treatment
NCT00749190 (10) [back to overview]Proportion of Patients Who Achieve an HbA1c Lowering of at Least 0.5% After 12 Weeks of Treatment
NCT00749190 (10) [back to overview]Change in Homeostasis Model Assessment Index for Beta Cell Function (HOMA-%B)
NCT00749190 (10) [back to overview]Change From Baseline to Week 12 in Fasting Plasma Insulin (FPI)
NCT00749190 (10) [back to overview]Proportion of Patients Who Achieve an HbA1c ≤7.0% After 12 Weeks of Treatment
NCT00749190 (10) [back to overview]Change of HbA1c From Baseline Over Time
NCT00749190 (10) [back to overview]Change of Body Weight After 12 Weeks of Treatment
NCT00749190 (10) [back to overview]Change of FPG From Baseline After 12 Weeks of Treatment
NCT00749190 (10) [back to overview]Trough Concentrations of Empagliflozin in Plasma
NCT00751114 (10) [back to overview]Insulin Dose in the Insulin Glargine Group
NCT00751114 (10) [back to overview]Lipid Profile: Change From Baseline to Study Endpoint
NCT00751114 (10) [back to overview]HbA1c Response Rate: Percentage of Patients Who Reach the Target of HbA1c < 6.5% at Study Endpoint
NCT00751114 (10) [back to overview]HbA1c Response Rate: Percentage of Patients Who Reach the Target of HbA1c < 7% at Study Endpoint
NCT00751114 (10) [back to overview]Change in Body Weight From Baseline to Study Endpoint
NCT00751114 (10) [back to overview]HbA1c: Change From Baseline to Study Endpoint
NCT00751114 (10) [back to overview]Number of Patients With at Least One Episode of Severe Symptomatic Hypoglycemia
NCT00751114 (10) [back to overview]Number of Patients With at Least One Episode of Symptomatic Hypoglycemia
NCT00751114 (10) [back to overview]Self-monitored Fasting Plasma Glucose (SMFPG) Mean : Change From Baseline to Study Endpoint
NCT00751114 (10) [back to overview]7-point Plasma Glucose Profile: Change From Baseline to Study Endpoint
NCT00758069 (2) [back to overview]Change From Baseline in 24-hour Weighted Mean Plasma Glucose
NCT00758069 (2) [back to overview]Change From Baseline in Plasma Glucose
NCT00768651 (2) [back to overview]The Primary Endpoint Will be Insulin Independence After 6 Months of Therapy.
NCT00768651 (2) [back to overview]Insulin Independence After the 3 Month Washout Period
NCT00775684 (5) [back to overview]Change in Acute Insulin Response to Arginine. (AIRarg)
NCT00775684 (5) [back to overview]Effect on Functional Beta-cell Mass as Determined by Change in ß-cell Secretory Capacity at 6 Months (pg/mL)
NCT00775684 (5) [back to overview]Effect on Functional Beta-cell Mass as Determined by Change in ß-cell Secretory Capacity at 6 Months (μU/ml)
NCT00775684 (5) [back to overview]Insulin Sensitivity at Baseline and 6 Months
NCT00775684 (5) [back to overview]PG 50 (the Plasma Glucose Level at Which Half-maximal Insulin Secretion is Achieved During the Glucose-potentiated Arginine Test) at Baseline and 6 Months
NCT00780715 (1) [back to overview]HbA1c Change
NCT00789191 (12) [back to overview]Number of Subjects Achieving HbA1c Less Than or Equal to 6.5%
NCT00789191 (12) [back to overview]Change in BMI (Body Mass Index)
NCT00789191 (12) [back to overview]Change in Body Weight
NCT00789191 (12) [back to overview]FPG (Fasting Plasma Glucose)
NCT00789191 (12) [back to overview]HbA1c (Glycosylated Haemoglobin A1c)
NCT00789191 (12) [back to overview]Hypoglycemic Episodes
NCT00789191 (12) [back to overview]Hypoglycemic Episodes: Day Time
NCT00789191 (12) [back to overview]Hypoglycemic Episodes: Night Time
NCT00789191 (12) [back to overview]Number of Subjects Achieving HbA1c Less Than or Equal to 6.5% Without Symptomatic Hypoglycaemia
NCT00789191 (12) [back to overview]Number of Subjects Achieving HbA1c Less Than or Equal to 7.0%
NCT00789191 (12) [back to overview]Number of Subjects Achieving HbA1c Less Than or Equal to 7.0% Without Symptomatic Hypoglycaemia
NCT00789191 (12) [back to overview]Self-measured 9-point Plasma Glucose Profile
NCT00790205 (18) [back to overview]Percentage of Participants With First Confirmed CV Event of MACE (Intent to Treat Population)
NCT00790205 (18) [back to overview]Percentage of Participants With First Confirmed CV Event of MACE (Per Protocol Population)
NCT00790205 (18) [back to overview]Percentage of Participants With First Confirmed CV Event of Major Adverse Cardiovascular Event (MACE) Plus (Intent to Treat Population)
NCT00790205 (18) [back to overview]Percentage of Participants With Initiation of Co-interventional Agent (Intent to Treat Population)
NCT00790205 (18) [back to overview]Percentage of Participants With Initiation of Co-interventional Agent (Per Protocol Population)
NCT00790205 (18) [back to overview]Change From Baseline in HbA1c Over Time (Intent to Treat Population)
NCT00790205 (18) [back to overview]Change From Baseline in HbA1c Over Time (Per Protocol Population)
NCT00790205 (18) [back to overview]Change From Baseline in Renal Function Over Time (Intent to Treat Population)
NCT00790205 (18) [back to overview]Change From Baseline in Renal Function Over Time (Per Protocol Population)
NCT00790205 (18) [back to overview]Change From Baseline in Urine Albumin:Creatinine Ratio Over Time (Intent to Treat Population)
NCT00790205 (18) [back to overview]Change From Baseline in Urine Albumin:Creatinine Ratio Over Time (Per Protocol Population)
NCT00790205 (18) [back to overview]Percent Incidence of All-cause Mortality (Intent to Treat Population)
NCT00790205 (18) [back to overview]Percent Incidence of All-cause Mortality (Per Protocol Population)
NCT00790205 (18) [back to overview]Percent Incidence of CHF Requiring Hospitalization (Intent to Treat Population)
NCT00790205 (18) [back to overview]Percent Incidence of Congestive Heart Failure (CHF) Requiring Hospitalization (Per Protocol Population)
NCT00790205 (18) [back to overview]Percentage of Participants Who Initiated Chronic Insulin Therapy (Intent to Treat Population)
NCT00790205 (18) [back to overview]Percentage of Participants Who Initiated Chronic Insulin Therapy (Per Protocol Population)
NCT00790205 (18) [back to overview]Percentage of Participants With First Confirmed Cardiovascular (CV) Event of Major Adverse Cardiovascular Event (MACE) Plus (Per Protocol Population)
NCT00795275 (8) [back to overview]Change in Endogenous Glucose Production
NCT00795275 (8) [back to overview]Change in Insulin Secretion
NCT00795275 (8) [back to overview]Baseline and Change in Hormones, Substrates and Insulin Action: C-peptide
NCT00795275 (8) [back to overview]Baseline and Change in Hormones, Substrates and Insulin Action: FFA
NCT00795275 (8) [back to overview]Baseline and Change in Hormones, Substrates and Insulin Action: GLP-1
NCT00795275 (8) [back to overview]Baseline and Change in Hormones, Substrates and Insulin Action: Glucagon
NCT00795275 (8) [back to overview]Baseline and Change in Hormones, Substrates and Insulin Action: Glycerol
NCT00795275 (8) [back to overview]Baseline and Change in Hormones, Substrates and Insulin Action: Lactate
NCT00813995 (5) [back to overview]Change From Baseline in Hemoglobin A1c (A1C) at Week 24 for Participants on Metformin 1700 mg/Day
NCT00813995 (5) [back to overview]Change From Baseline in Hemoglobin A1c (A1C) at Week 24 for Participants on Metformin 1000 mg/Day
NCT00813995 (5) [back to overview]Change From Baseline in Hemoglobin A1c (A1C) at Week 24
NCT00813995 (5) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24
NCT00813995 (5) [back to overview]Change From Baseline in 2-hour Post-meal Glucose (PMG) at Week 24
NCT00820573 (4) [back to overview]Objective: Comparisons of the Effects of Co-administration of Sitagliptin and Metformin Alone or in Combination Versus Placebo on Baseline Endogenous Glucose Production (EGP).
NCT00820573 (4) [back to overview]Changes in Plasma Glucose Post-MTT After Each Six Weeks of Therapy Compared to Baseline
NCT00820573 (4) [back to overview]Fasting Plasma Glucose 6 Weeks After Therapy
NCT00820573 (4) [back to overview]Average of Plasma Glucose During Mixed Meal Tolerance Test (MTT) Compared to Baseline Plasma Glucose to Post Therapy (6-weeks).
NCT00830076 (3) [back to overview]Incremental Post-prandial 4-hour Weighted Mean Active Glucagon-like Peptide-1 (GLP-1) Plasma Concentrations
NCT00830076 (3) [back to overview]β-cell Sensitivity
NCT00830076 (3) [back to overview]Incremental Post-prandial 4-hour Weighted Mean Plasma Glucose Concentrations
NCT00832390 (1) [back to overview]Change From Baseline in A1C at Week 24
NCT00833027 (2) [back to overview]Change From Baseline in HbA1c at Week 12
NCT00833027 (2) [back to overview]Change From Baseline in HbA1c at Week 24
NCT00837577 (3) [back to overview]Change From Baseline in 2-hour Postprandial Glucose at Week 12
NCT00837577 (3) [back to overview]Change From Baseline in Hemoglobin A1c (HbA1c) at Week 12
NCT00837577 (3) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 12
NCT00837759 (6) [back to overview]Change in Insulin Dose
NCT00837759 (6) [back to overview]Change in C-peptide
NCT00837759 (6) [back to overview]Change in Anti-IA2 Titer
NCT00837759 (6) [back to overview]Change in Anti-GAD Autoantibody Titers
NCT00837759 (6) [back to overview]Glycemia Control (Change in HbA1c Level)
NCT00837759 (6) [back to overview]Change in ZnT8 Autoantibody Titer
NCT00838903 (9) [back to overview]Time to Hyperglycemia Rescue
NCT00838903 (9) [back to overview]Number of Participants Who Achieved Clinically Meaningful HbA1c Response Levels of <6.5%, <7%, and <7.5% at Week 104
NCT00838903 (9) [back to overview]Number of Participants Who Achieved Clinically Meaningful HbA1c Response Levels of <6.5%, <7%, and <7.5% at Week 156
NCT00838903 (9) [back to overview]Change From Baseline (BL) in Glycosylated Hemoglobin (HbA1c) at Week 104
NCT00838903 (9) [back to overview]Change From Baseline in Body Weight at Week 104
NCT00838903 (9) [back to overview]Change From Baseline in Body Weight at Week 156
NCT00838903 (9) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 104
NCT00838903 (9) [back to overview]Change From Baseline in FPG at Week 156
NCT00838903 (9) [back to overview]Change From Baseline in HbA1c at Week 156
NCT00851903 (7) [back to overview]HbA1c: Change From Baseline to Study Endpoint
NCT00851903 (7) [back to overview]HbA1c Response Rate: Percentage of Patients Achieving Glycosylated Haemoglobin A1c (HbA1c) < 7% at Study Endpoint (End of Treatment Period)
NCT00851903 (7) [back to overview]Number of Patients With at Least One Episode of Symptomatic Hypoglycemia
NCT00851903 (7) [back to overview]Change in Body Weight From Baseline to Study Endpoint
NCT00851903 (7) [back to overview]Self-Monitored Fasting Plasma Glucose (SMFPG) Mean : Change From Baseline to Study Endpoint
NCT00851903 (7) [back to overview]7-point Plasma Glucose Profile: Change From Baseline to Study Endpoint
NCT00851903 (7) [back to overview]Insulin Dose
NCT00855166 (7) [back to overview]Adjusted Percent Change in Bone Mineral Density (BMD) at Total Hip
NCT00855166 (7) [back to overview]Proportion of Participants With Body Weight Decrease ≥5%
NCT00855166 (7) [back to overview]Adjusted Mean Change in Waist Circumference
NCT00855166 (7) [back to overview]Adjusted Percent Change in Bone Mineral Density (BMD) at Lumbar Spine (L1-4)
NCT00855166 (7) [back to overview]Adjusted Mean Change in Body Fat Mass
NCT00855166 (7) [back to overview]Adjusted Mean Change in Total Body Weight
NCT00855166 (7) [back to overview]Adjusted Percent Change in Bone Mineral Density (BMD) at Femoral Neck
NCT00862719 (4) [back to overview]Treatment Related Adverse Events Grade 3 or Higher for Non-hematological Toxicity
NCT00862719 (4) [back to overview]Time to Platelet Engraftment
NCT00862719 (4) [back to overview]Cumulative Incidence of Patients With Engraftment by Day +30 Following Transplant
NCT00862719 (4) [back to overview]Time to Neutrophil Engraftment
NCT00870194 (17) [back to overview]Change in Triglycerides (mmol/L)
NCT00870194 (17) [back to overview]Change in Total Cholesterol (mmol/L)
NCT00870194 (17) [back to overview]Change in LDL (mmol/L)
NCT00870194 (17) [back to overview]Change in HDL (mmol/L)
NCT00870194 (17) [back to overview]Change in FSG (mmol/L)
NCT00870194 (17) [back to overview]Change in Body Weight (kg)
NCT00870194 (17) [back to overview]Percentage of Patients Achieving HbA1c <=6.5%
NCT00870194 (17) [back to overview]Percentage of Patients Achieving HbA1c <=7.0%
NCT00870194 (17) [back to overview]Percentage of Patients Achieving HbA1c <7.0%
NCT00870194 (17) [back to overview]SMBG (mmol/L)
NCT00870194 (17) [back to overview]Waist-to-Hip Ratio
NCT00870194 (17) [back to overview]Incidence of Nocturnal Hypoglycemia (Overall)
NCT00870194 (17) [back to overview]Incidence of Hypoglycemia (Overall)
NCT00870194 (17) [back to overview]Change in Waist Circumference (cm)
NCT00870194 (17) [back to overview]Incidence of Confirmed Hypoglycemia(Overall)
NCT00870194 (17) [back to overview]Change in HbA1c (Percent)
NCT00870194 (17) [back to overview]Incidence of Severe Hypoglycemia(Overall)
NCT00881530 (8) [back to overview]Change From Baseline in HbA1c Over Time
NCT00881530 (8) [back to overview]Clinical Relevant Abnormalities for Physical Examination, Vital Signs, ECG and Laboratory Measurements
NCT00881530 (8) [back to overview]Occurence of a Treat-to-target Response (HbA1c < 7.0%)
NCT00881530 (8) [back to overview]Occurrence of a Relative Efficacy Response
NCT00881530 (8) [back to overview]Change From Baseline to Week 78 in Lipid Parameters
NCT00881530 (8) [back to overview]Hypoglycaemic Events
NCT00881530 (8) [back to overview]Occurrence of a Treat-to-target Response (HbA1c < 6.5%)
NCT00881530 (8) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) Over Time
NCT00885352 (3) [back to overview]Change From Baseline in 2-Hour Post-Meal Glucose (PMG) at Week 26
NCT00885352 (3) [back to overview]Change From Baseline in Hemoglobin A1c (A1C) at Week 26
NCT00885352 (3) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 26
NCT00885638 (2) [back to overview]Glucagon-like Peptide-1 Secretion After Meal Ingestion
NCT00885638 (2) [back to overview]Insulin Secretion After Ingestion of Meal
NCT00888238 (2) [back to overview]Glucose Infusion Rate (GIR) During 190 - 340 Minutes Post-dose
NCT00888238 (2) [back to overview]Insulin Secretion Rate (ISR) During 190 - 340 Minutes Post-dose
NCT00929201 (2) [back to overview]Plasma Area Under the Curve (AUC(0 to Infinity)) for Metformin
NCT00929201 (2) [back to overview]Peak Plasma Concentration (Cmax) of Metformin
NCT00936663 (8) [back to overview]AUC for Glucose
NCT00936663 (8) [back to overview]Hypoglycemia
NCT00936663 (8) [back to overview]HbA1c
NCT00936663 (8) [back to overview]eGFR
NCT00936663 (8) [back to overview]AUC for Proinsulin
NCT00936663 (8) [back to overview]Fasting Blood Glucose
NCT00936663 (8) [back to overview]AUC for Insulin
NCT00936663 (8) [back to overview]AUC for C Peptide
NCT00944450 (2) [back to overview]Area Under the Curve (AUC(0 to Infinity)) Following Single Dose Administration of the Anhydrous and Monohydrate Forms of MK0431 (Sitagliptin)
NCT00944450 (2) [back to overview]Peak Plasma Concentration (Cmax) Following Single Dose Administration of the Anhydrous and Monohydrate Forms of MK0431 (Sitagliptin)
NCT00967798 (2) [back to overview]Change in Percent Predicted FEV1
NCT00967798 (2) [back to overview]Number of Participants With Conversion to Cystic Fibrosis Related Diabetes
NCT00976937 (18) [back to overview]Absolute Change From Baseline in HbA1c at Week 24
NCT00976937 (18) [back to overview]Change From Baseline in Glucose Excursion at Week 24
NCT00976937 (18) [back to overview]Percentage of Patients With Glycosylated Hemoglobin (HbA1c) Level Less Than 7% and at Least 5% Weight Loss From Baseline at Week 24
NCT00976937 (18) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24
NCT00976937 (18) [back to overview]Change From Baseline in Beta Cell Function Assessed by Homeostasis Model Assessment-Beta (HOMA-beta) at Week 24
NCT00976937 (18) [back to overview]Change From Baseline in Body Weight at Week 24
NCT00976937 (18) [back to overview]Number of Patients With Symptomatic Hypoglycemia and Severe Symptomatic Hypoglycemia
NCT00976937 (18) [back to overview]Change From Baseline in Fasting Glucagon and 2-hour Postprandial Glucagon at Week 24
NCT00976937 (18) [back to overview]Percentage of Patients With at Least 5% Weight Loss From Baseline at Week 24
NCT00976937 (18) [back to overview]Change From Baseline in Fasting Proinsulin-to-insulin Ratio and 2-hour Postprandial Proinsulin-to-insulin Ratio at Week 24
NCT00976937 (18) [back to overview]Change From Baseline in Fasting Proinsulin and 2-hour Postprandial Proinsulin at Week 24
NCT00976937 (18) [back to overview]Change From Baseline in Fasting Plasma Insulin (FPI) and 2-hour Postprandial Plasma Insulin (PPI) at Week 24
NCT00976937 (18) [back to overview]Change From Baseline in Fasting C-peptide and 2-hour Postprandial C-peptide at Week 24
NCT00976937 (18) [back to overview]Percentage of Patients With Glycosylated Hemoglobin (HbA1c) Level Less Than or Equal to 6.5% at Week 24
NCT00976937 (18) [back to overview]Percentage of Patients With Glycosylated Hemoglobin (HbA1c) Level Less Than 7% at Week 24
NCT00976937 (18) [back to overview]Change From Baseline in 2-hour Postprandial Plasma Glucose (PPG) at Week 24
NCT00976937 (18) [back to overview]Percentage of Patients Requiring Rescue Therapy During 24-Week Period
NCT00976937 (18) [back to overview]Change From Baseline in Insulin Resistance Assessed by Homeostasis Model Assessment- Insulin Resistance (HOMA-IR) at Week 24
NCT00993187 (7) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 30
NCT00993187 (7) [back to overview]Change From Baseline in Body Weight at Week 30
NCT00993187 (7) [back to overview]Percentage of Participants With HbA1C < 7.0% at Week 30
NCT00993187 (7) [back to overview]Percentage of Participants With One or More Episodes of Hypoglycemia
NCT00993187 (7) [back to overview]Number of Participants Who Discontinued Study Drug Due to an Adverse Event
NCT00993187 (7) [back to overview]Number of Participants Who Experienced at Least One Adverse Event (AE)
NCT00993187 (7) [back to overview]Change From Baseline in Hemoglobin A1C (HbA1C) at Week 30
NCT01028391 (2) [back to overview]Change From Baseline (i.e., Week 0 of the 24-week Base Study) in Fasting Plasma Glucose (FPG) at Week 54
NCT01028391 (2) [back to overview]Change From Baseline (i.e., Week 0 of the 24-week Base Study) in Hemoglobin A1c (HbA1c) at Week 54
NCT01034111 (2) [back to overview]Safety and Tolerability of Sitagliptin After 4 Weeks of Treatment
NCT01034111 (2) [back to overview]Change From Baseline in Fasting Plasma Glucose at Week 4
NCT01046110 (2) [back to overview]Change in Fasting Plasma Glucose (FPG)
NCT01046110 (2) [back to overview]Change in Glycosylated Haemoglobin (HbA1c)
NCT01059825 (29) [back to overview]Change From Baseline in Systolic Blood Pressure at Week 4
NCT01059825 (29) [back to overview]Change From Baseline in Systolic Blood Pressure at Week 2
NCT01059825 (29) [back to overview]Change From Baseline in Systolic Blood Pressure at Week 12
NCT01059825 (29) [back to overview]Change From Baseline in HbA1c at Week 8
NCT01059825 (29) [back to overview]Change From Baseline in HbA1c at Week 4
NCT01059825 (29) [back to overview]Change From Baseline in HbA1C at Week 2
NCT01059825 (29) [back to overview]Change From Baseline in HbA1c at Week 12
NCT01059825 (29) [back to overview]Baseline Body Weight
NCT01059825 (29) [back to overview]Percentage of Participants Achieving HbA1c <7% at Week 12
NCT01059825 (29) [back to overview]Baseline Hemoglobin A1c (HbA1c)
NCT01059825 (29) [back to overview]Percentage of Participants Achieving HbA1C <6.5% at Week 12
NCT01059825 (29) [back to overview]Change From Baseline in Fasting Plasma Glucose at Week 2
NCT01059825 (29) [back to overview]Change From Baseline in Fasting Plasma Glucose at Week 8
NCT01059825 (29) [back to overview]Change From Baseline in Fasting Plasma Glucose at Week 4
NCT01059825 (29) [back to overview]Change From Baseline in Fasting Plasma Glucose at Week 12
NCT01059825 (29) [back to overview]Change From Baseline in Diastolic Blood Pressure at Week 8
NCT01059825 (29) [back to overview]Change From Baseline in Diastolic Blood Pressure at Week 4
NCT01059825 (29) [back to overview]Change From Baseline in Diastolic Blood Pressure at Week 2
NCT01059825 (29) [back to overview]Change From Baseline in Diastolic Blood Pressure at Week 12
NCT01059825 (29) [back to overview]Percent Change From Baseline in Body Weight at Week 8
NCT01059825 (29) [back to overview]Baseline Systolic Blood Pressure
NCT01059825 (29) [back to overview]Baseline Fasting Plasma Glucose
NCT01059825 (29) [back to overview]Baseline Diastolic Blood Pressure
NCT01059825 (29) [back to overview]Percent Change From Baseline in Body Weight at Week 4
NCT01059825 (29) [back to overview]Percent Change From Baseline in Body Weight at Week 2
NCT01059825 (29) [back to overview]Percent Change From Baseline in Body Weight at Week 12
NCT01059825 (29) [back to overview]Number of Participants Who Experienced an Advere Event (AE)
NCT01059825 (29) [back to overview]Number of Participants Who Discontinued Study Medication Due to an AE
NCT01059825 (29) [back to overview]Change From Baseline in Systolic Blood Pressure at Week 8
NCT01065766 (9) [back to overview]Percentage of Participants With an Overall Efficacy Evaluation by the Investigator of Improved, Stable, or Worse at Week 24
NCT01065766 (9) [back to overview]Percentage of Participants With an Overall Efficacy Evaluation by the Investigator of Improved, Stable, or Worse at Week 12
NCT01065766 (9) [back to overview]Percentage of Participants With Any Adverse Experience
NCT01065766 (9) [back to overview]Change From Baseline to Treatment in Hemoglobin HbA1c (A1C) at Week 12
NCT01065766 (9) [back to overview]Change From Baseline to Treatment in HbA1c at Week 24
NCT01065766 (9) [back to overview]Change From Baseline to Treatment in FPG at Week 24
NCT01065766 (9) [back to overview]Change From Baseline to Treatment in Fasting Plasma Glucose (FPG) at Week 12
NCT01065766 (9) [back to overview]Change From Baseline in 2hr-PPG at Week 24
NCT01065766 (9) [back to overview]Change From Baseline in 2-hour Post Prandial Glucose (2hr-PPG) at Week 12
NCT01076075 (5) [back to overview]Change From Baseline in Hemoglobin A1C (%) at Week 24
NCT01076075 (5) [back to overview]Number of Participants Discontinuing Study Drug Due to An Adverse Event
NCT01076075 (5) [back to overview]Number of Participants With One or More Adverse Events (AEs) - Week 0 to Week 54
NCT01076075 (5) [back to overview]Change From Baseline in 2-hour Post-Meal Glucose at Week 24
NCT01076075 (5) [back to overview]Change From Baseline in Fasting Plasma Glucose at Week 24
NCT01076088 (3) [back to overview]Change From Baseline in Hemoglobin A1C (A1C) at Week 24
NCT01076088 (3) [back to overview]Change From Baseline in 2-hour Post Meal Glucose (2-h PMG) at Week 24
NCT01076088 (3) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24
NCT01081834 (16) [back to overview]Change in HbA1c From Baseline to Week 26 (Main Study)
NCT01081834 (16) [back to overview]Percentage of Patients With HbA1c <7% at Week 26 (High Glycemic Substudy)
NCT01081834 (16) [back to overview]Percent Change in High-density Lipoprotein Cholesterol (HDL-C) From Baseline to Week 26 (Main Study)
NCT01081834 (16) [back to overview]Change in Fasting Plasma Glucose (FPG) From Baseline to Week 26 (High Glycemic Substudy)
NCT01081834 (16) [back to overview]Change in 2-hour Post-prandial Glucose From Baseline to Week 26 (Main Study)
NCT01081834 (16) [back to overview]Change in 2-hour Post-prandial Glucose From Baseline to Week 26 (High Glycemic Substudy)
NCT01081834 (16) [back to overview]Percent Change in High-density Lipoprotein Cholesterol (HDL-C) From Baseline to Week 26 (High Glycemic Substudy)
NCT01081834 (16) [back to overview]Percentage of Patients With HbA1c <7% at Week 26 (Main Study)
NCT01081834 (16) [back to overview]Percent Change in Triglycerides From Baseline to Week 26 (Main Study)
NCT01081834 (16) [back to overview]Percent Change in Triglycerides From Baseline to Week 26 (High Glycemic Substudy)
NCT01081834 (16) [back to overview]Change in Fasting Plasma Glucose (FPG) From Baseline to Week 26 (Main Study)
NCT01081834 (16) [back to overview]Change in HbA1c From Baseline to Week 26 (High Glycemic Substudy)
NCT01081834 (16) [back to overview]Change in Systolic Blood Pressure (SBP) From Baseline to Week 26 (High Glycemic Substudy)
NCT01081834 (16) [back to overview]Change in Systolic Blood Pressure (SBP) From Baseline to Week 26 (Main Study)
NCT01081834 (16) [back to overview]Percent Change in Body Weight From Baseline to Week 26 (High Glycemic Substudy)
NCT01081834 (16) [back to overview]Percent Change in Body Weight From Baseline to Week 26 (Main Study)
NCT01092663 (21) [back to overview]Postprandial Total GIP (AUC)
NCT01092663 (21) [back to overview]Fasting Gluconeogenesis
NCT01092663 (21) [back to overview]Fasting Endogenous Glucose Production
NCT01092663 (21) [back to overview]Fasting Active Plasma Glucagon Like-Peptide 1 (GLP-1)
NCT01092663 (21) [back to overview]Appearance Rate of Oral Glucose
NCT01092663 (21) [back to overview]Postprandial Rate of Total Glucose Disposal Area Under the Curve (AUC)
NCT01092663 (21) [back to overview]Postprandial Insulin (AUC)
NCT01092663 (21) [back to overview]Postprandial Glucose (AUC)
NCT01092663 (21) [back to overview]Postprandial Glucagon (AUC)
NCT01092663 (21) [back to overview]Postprandial Endogenous Glucose Production
NCT01092663 (21) [back to overview]Postprandial C-peptide (AUC)
NCT01092663 (21) [back to overview]Postprandial Active GLP-1 (AUC)
NCT01092663 (21) [back to overview]Hemoglobin A1C
NCT01092663 (21) [back to overview]Fasting Plasma Total Glucose-dependent Insulinotropic Peptide (GIP)
NCT01092663 (21) [back to overview]Fasting Plasma Glucose Clearance
NCT01092663 (21) [back to overview]Fasting Plasma Glucose
NCT01092663 (21) [back to overview]Fasting Plasma C-peptide
NCT01092663 (21) [back to overview]Fasting Plamsa Glucagon
NCT01092663 (21) [back to overview]Fasting Insulin
NCT01092663 (21) [back to overview]Whole-body Glycolytic Disposal of Oral Glucose
NCT01092663 (21) [back to overview]Fasting Glycogenolysis
NCT01093651 (7) [back to overview]Self-reported Symptoms
NCT01093651 (7) [back to overview]SDF1α; Serum Biomarkers of Immune Activation
NCT01093651 (7) [back to overview]RANTES; Serum Biomarkers of Immune Activation
NCT01093651 (7) [back to overview]Oral Glucose Tolerance
NCT01093651 (7) [back to overview]CD4+ T-cell Count
NCT01093651 (7) [back to overview]Plasma HIV Viremia (Viral Load)
NCT01093651 (7) [back to overview]Soluble TNFR2; Serum Biomarkers of Immune Activation
NCT01093794 (2) [back to overview]Area Under the Curve (AUC(0-t)) for Sitagliptin
NCT01093794 (2) [back to overview]Cmax for Sitagliptin and Metformin
NCT01098539 (16) [back to overview]Number of Participants With the Indicated Time to Hyperglycemic Rescue Through Week 52
NCT01098539 (16) [back to overview]Plasma Concentrations (Conc.) of Albiglutide at Week 8 and Week 16
NCT01098539 (16) [back to overview]Change From Baseline in Body Weight Through Week 52: OC
NCT01098539 (16) [back to overview]Mean Change From Baseline in Fasting Plasma Glucose (FPG) at Weeks 1, 2, 3, 4, 8, 12, 16, 20, 26, 36, 48, and Week 52: OC
NCT01098539 (16) [back to overview]Mean Change From Baseline in FPG at Weeks 4, 8, 12, 16, 20, and 26: LOCF
NCT01098539 (16) [back to overview]Mean Change From Baseline in HbA1c at Weeks 4, 8, 12, 16, 20, 26, 36, 48, and Week 52: Observed Cases
NCT01098539 (16) [back to overview]Mean Change From Baseline in HbA1c at Weeks 4, 8, 12, 16, and 20: LOCF
NCT01098539 (16) [back to overview]Number of Participants Who Achieved a Clinically Meaningful HbA1c Response Level of <6.5% and <7.0% at Week 52: OC
NCT01098539 (16) [back to overview]Number of Participants Who Achieved a Clinically Meaningful Improvement in the HbA1c Response Level of >=1.0%, >=1.5%, and >=2.0% at Week 26: LOCF
NCT01098539 (16) [back to overview]Number of Participants Who Achieved a Clinically Meaningful Improvement in the HbA1c Response Level of >=1.0%, >=1.5%, and >=2.0% at Week 52: OC
NCT01098539 (16) [back to overview]Number of Participants Who Achieved Clinically Meaningful HbA1c Response Levels of <6.5% and <7.0% at Week 26: LOCF
NCT01098539 (16) [back to overview]Change From Baseline in Body Weight at Week 26: LOCF
NCT01098539 (16) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 26
NCT01098539 (16) [back to overview]Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 26
NCT01098539 (16) [back to overview]Time to Hyperglycemic Rescue Through Week 52
NCT01098539 (16) [back to overview]Change From Baseline in Body Weight Through Week 26: LOCF
NCT01099618 (1) [back to overview]Length of Remission
NCT01106677 (14) [back to overview]Percent Change in Body Weight From Baseline to Week 26
NCT01106677 (14) [back to overview]Percent Change in High-density Lipoprotein Cholesterol (HDL-C) From Baseline to Week 52
NCT01106677 (14) [back to overview]Percent Change in High-density Lipoprotein Cholesterol (HDL-C) From Baseline to Week 26
NCT01106677 (14) [back to overview]Percent Change in Body Weight From Baseline to Week 52
NCT01106677 (14) [back to overview]Change in 2-hour Post-prandial Glucose From Baseline to Week 26
NCT01106677 (14) [back to overview]Percent Change in Triglycerides From Baseline to Week 26
NCT01106677 (14) [back to overview]Change in Systolic Blood Pressure (SBP) From Baseline to Week 52
NCT01106677 (14) [back to overview]Change in Systolic Blood Pressure (SBP) From Baseline to Week 26
NCT01106677 (14) [back to overview]Change in HbA1c From Baseline to Week 52
NCT01106677 (14) [back to overview]Change in HbA1c From Baseline to Week 26
NCT01106677 (14) [back to overview]Change in Fasting Plasma Glucose (FPG) From Baseline to Week 52
NCT01106677 (14) [back to overview]Change in Fasting Plasma Glucose (FPG) From Baseline to Week 26
NCT01106677 (14) [back to overview]Percentage of Patients With HbA1c <7% at Week 26
NCT01106677 (14) [back to overview]Percent Change in Triglycerides From Baseline to Week 52
NCT01106690 (8) [back to overview]Percent Change in Body Weight From Baseline to Week 26
NCT01106690 (8) [back to overview]Percent Change in High-density Lipoprotein Cholesterol (HDL-C) From Baseline to Week 26
NCT01106690 (8) [back to overview]Percent Change in Triglycerides From Baseline to Week 26
NCT01106690 (8) [back to overview]Percentage of Patients With HbA1c <7% at Week 26
NCT01106690 (8) [back to overview]Change in Homeostasis Model Assessment (HOMA2-%B) From Baseline to Week 26
NCT01106690 (8) [back to overview]Change in Fasting Plasma Glucose (FPG) From Baseline to Week 26
NCT01106690 (8) [back to overview]Change in HbA1c From Baseline to Week 26
NCT01106690 (8) [back to overview]Change in Systolic Blood Pressure (SBP) From Baseline to Week 26
NCT01112670 (11) [back to overview]Relative Change in Sitagliptin Renal Clearance (CLr)
NCT01112670 (11) [back to overview]Atorvastatin Area Under the Plasma Concentration Time Curve (AUC) Over the Dosing Interval (0-24 Hours)
NCT01112670 (11) [back to overview]Atorvastatin Maximum Plasma Concentration (Cmax)
NCT01112670 (11) [back to overview]Relative Change in Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity
NCT01112670 (11) [back to overview]Sitagliptin Monotherapy: Sitagliptin Maximum Plasma Concentration (Cmax)
NCT01112670 (11) [back to overview]Sitagliptin Monotherapy: Sitagliptin Renal Clearance (CLr)
NCT01112670 (11) [back to overview]Sitagliptin + Atorvastatin: Sitagliptin Maximum Plasma Concentration (Cmax)
NCT01112670 (11) [back to overview]Sitagliptin + Atorvastatin: Sitagliptin Renal Clearance (CLr)
NCT01112670 (11) [back to overview]Sitagliptin Monotherapy: Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity
NCT01112670 (11) [back to overview]Sitagliptin + Atorvastatin: Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity
NCT01112670 (11) [back to overview]Relative Change in Sitagliptin Maximum Plasma Concentration (Cmax)
NCT01119846 (46) [back to overview]Part B: Number of Participants With AEs and SAEs
NCT01119846 (46) [back to overview]Part B: Summary of AUC0-t and AUC0-24
NCT01119846 (46) [back to overview]Part B: Summary of Change From Baseline in Fasted Glucagon, GLP-1, C-peptide, Total GIP, Total PYY and Insulin
NCT01119846 (46) [back to overview]Part B: Summary of T-max and T-lag
NCT01119846 (46) [back to overview]Part C: Number of Participants With Abnormal Clinical Chemistry Parameters of PCI
NCT01119846 (46) [back to overview]Part C: Summary of T-half and Tmax of GSK1292263 and Sitagliptin When Co-administered
NCT01119846 (46) [back to overview]Part C: Summary of T-max and T-lag
NCT01119846 (46) [back to overview]Part C: Summary of Change From Baseline in Fasted Insulin
NCT01119846 (46) [back to overview]Part C: Summary of Change From Baseline in Fasted Glucose
NCT01119846 (46) [back to overview]Part C: Summary of AUC0-24, AUC0-t of GSK1292263 and Sitagliptin When Co-administered
NCT01119846 (46) [back to overview]Part C: Summary of AUC0-10, AUC0-12 and AUC0-24
NCT01119846 (46) [back to overview]Part C: Summary of Accumulation Ratio (Ro)
NCT01119846 (46) [back to overview]Part C: Relationships Between GSK1292263 Drug Exposures and Insulin Sensitivity
NCT01119846 (46) [back to overview]Part C: Number of Participants With AEs and SAEs
NCT01119846 (46) [back to overview]Part C: Number of Participants With Abnormal Vital Signs of PCI
NCT01119846 (46) [back to overview]Part C: Number of Participants With Abnormal Hematology Parameters of PCI
NCT01119846 (46) [back to overview]Part C: Summary of Plasma Cmax
NCT01119846 (46) [back to overview]Part A: Summary of the AUC 0-13, AUC 0-24, Incremental AUC (iAUC) 0-13 and iAUC 0-24 of Glucose
NCT01119846 (46) [back to overview]Part A: Summary of the OGTT AUC (0-2) and iAUC(0-2)- C-peptide, Total GIP, GLP-1 (Active and Total), Glucagon and Total PYY and AUC 0-3 and iAUC 0-3 of Insulin
NCT01119846 (46) [back to overview]Part A: Summary of the OGTT AUC (0-3) and iAUC(0-3)-Glucose
NCT01119846 (46) [back to overview]Part A: Summary of the OGTT Derived Parameters: Glucose/Insulin and Insulin/Glucose Ratio
NCT01119846 (46) [back to overview]Part A: Summary of Time to Maximum Concentration (T-max) and Lag Time Before Observation of Drug Concentration in Sampled Matrix (T-lag)
NCT01119846 (46) [back to overview]Part A: Summary of Maximum Plasma Concentration (Cmax)
NCT01119846 (46) [back to overview]Part A: Number of Participants With Abnormal Electrocardiogram (ECG) Findings
NCT01119846 (46) [back to overview]Part A: Number of Participants With Abnormal Hematology Parameters of Potential Clinical Importance (PCI)
NCT01119846 (46) [back to overview]Part A: Number of Participants With Abnormal Vital Signs of PCI
NCT01119846 (46) [back to overview]Part A: Relationships Between GSK1292263 Drug Exposures and Insulin Sensitivity
NCT01119846 (46) [back to overview]Part A: Summary of Change From Baseline in Fasted Glucose
NCT01119846 (46) [back to overview]Part A: Summary of the OGTT Derived Parameters: Disposition Index
NCT01119846 (46) [back to overview]Part A: Summary of the OGTT Derived Parameters: Insulin Glucose Index
NCT01119846 (46) [back to overview]Part A: Summary of the OGTT Derived Parameters: Insulin Sensitivity Index
NCT01119846 (46) [back to overview]Part B: Number of Participants With Abnormal Clinical Chemistry Parameters of PCI
NCT01119846 (46) [back to overview]Part B: Number of Participants With Abnormal Hematology Parameters of PCI
NCT01119846 (46) [back to overview]Part B: Number of Participants With Abnormal Vital Signs of PCI
NCT01119846 (46) [back to overview]Part B: Number of Participants With Significant ECG Abnormalities
NCT01119846 (46) [back to overview]Part B: Summary of Change From Baseline in Fasted Glucose
NCT01119846 (46) [back to overview]Part B: Summary of Plasma Cmax
NCT01119846 (46) [back to overview]Part C: Number of Participants With Significant ECG Abnormalities
NCT01119846 (46) [back to overview]Part C: Summary of Cmax of GSK1292263 and Sitagliptin When Co-administered
NCT01119846 (46) [back to overview]Part C: Summary of Time Invariance Ratio (Rs) of AUC0-10 for BID Dose of GSK1292263
NCT01119846 (46) [back to overview]Part C: Summary of Time Invariance Ratio (Rs) of AUC0-24 for Once Daily Dose of GSK1292263
NCT01119846 (46) [back to overview]Part C: Summary of Time Invariance Ratio (Rs) of Cmax
NCT01119846 (46) [back to overview]Part A: Number of Participants With Abnormal Clinical Chemistry Parameters of PCI
NCT01119846 (46) [back to overview]Part A: Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT01119846 (46) [back to overview]Part A: Summary of Area Under the Concentration-time Curve From Time Zero (Pre-dose) to Last Time of Quantifiable Concentration (AUC0-t) and Area Under the Concentration-time Curve From Zero (Pre-dose) to 24 Hours (AUC0-24)
NCT01119846 (46) [back to overview]Part A: Summary of the AUC 0-12 and iAUC 0-12 of Glucagon, Glucagon-like Peptide (GLP; Active and Total)-1, C-peptide, Total Glucose-dependent Insulinotropic Peptide (GIP) and Total Peptide Tyrosine-tyrosine (PYY) and AUC 0-13 and iAUC 0-13 of Insulin
NCT01128621 (33) [back to overview]Mean Value of Urine Albumin (Part B)
NCT01128621 (33) [back to overview]Lag Time Before Observation of Drug Concentrations in Sampled Matrix (Tlag) and Time of Occurrence of Cmax (Tmax) Following a Single Dose of GSK1292263 (Part A)
NCT01128621 (33) [back to overview]Mean Accumulation Ratio by AUC (0-10), AUC (0-24) and Cmax for GSK1292263 (Part B)
NCT01128621 (33) [back to overview]Mean Value of Urine pH (Part A)
NCT01128621 (33) [back to overview]Mean Value of Urine pH (Part B)
NCT01128621 (33) [back to overview]Mean Value of Urine Specific Gravity (Part A)
NCT01128621 (33) [back to overview]Mean Value of Urine Specific Gravity (Part B)
NCT01128621 (33) [back to overview]Number of Participants With Abnormal Clinical Chemistry Values of PCI (Part B)
NCT01128621 (33) [back to overview]Number of Participants With Abnormal Electrocardiogram (ECG) Findings (Part A)
NCT01128621 (33) [back to overview]Change From Baseline in Mean Fasted Glucose Value (Part B)
NCT01128621 (33) [back to overview]Number of Participants With Abnormal Electrocardiogram (ECG) Findings (Part B)
NCT01128621 (33) [back to overview]Number of Participants With Abnormal Hematology Values of PCI (Part B)
NCT01128621 (33) [back to overview]Number of Participants With Abnormal Urinalysis Data Values (Part B)
NCT01128621 (33) [back to overview]Number of Participants With Abnormal Urinalysis Data Values by Dipstick Method (Part A)
NCT01128621 (33) [back to overview]Number of Participants With Abnormal Vital Signs of PCI (Part A)
NCT01128621 (33) [back to overview]Number of Participants With Abnormal Vital Signs of PCI (Part B)
NCT01128621 (33) [back to overview]Number of Participants With Any AEs and Serious Adverse Events SAEs (Part B)
NCT01128621 (33) [back to overview]Tmax and Tlag Following Repeat Dose of GSK1292263 (Part B)
NCT01128621 (33) [back to overview]Number of Participants With Any Adverse Events (AEs) and Serious Adverse Events (SAEs) (Part A)
NCT01128621 (33) [back to overview]Change From Baseline in Mean Fasted Insulin Value (Part B)
NCT01128621 (33) [back to overview]Change From Baseline in Weighted Mean for Glucose Value (Part B)
NCT01128621 (33) [back to overview]AUC From Time Zero (Pre-dose) to 10 Hours [AUC (0-10)] and AUC (0-24) Following Repeat Dose of GSK1292263 (Part B)
NCT01128621 (33) [back to overview]Area Under the Concentration-time Curve From Zero (Pre-dose) to 24 Hours [AUC (0-24)] and AUC From Time Zero (Pre-dose) to Last Time of Quantifiable Concentration (AUC [0-last)] Following a Single Dose of GSK1292263 (Part A)
NCT01128621 (33) [back to overview]Number of Participants With Abnormal Hematology Values of Potential Clinical Importance (PCI) (Part A)
NCT01128621 (33) [back to overview]Mean Value of Urine Albumin at Follow up (Part A)
NCT01128621 (33) [back to overview]Maximum Observed Concentration (Cmax) Following a Single Dose of GSK1292263 (Part A)
NCT01128621 (33) [back to overview]Change From Baseline in Mean Fasted Insulin Value (Part A)
NCT01128621 (33) [back to overview]Change From Baseline in Mean Fasted Glucose Value (Part A)
NCT01128621 (33) [back to overview]Change From Baseline in Weighted Mean for Insulin Value (Part B)
NCT01128621 (33) [back to overview]Mean Post Meal Glucose Value (Part B)
NCT01128621 (33) [back to overview]Cmax Following Repeat Dose of GSK1292263 (Part B)
NCT01128621 (33) [back to overview]Number of Participants With Abnormal Clinical Chemistry Values of PCI (Part A)
NCT01128621 (33) [back to overview]Mean Post Meal Insulin Value (Part B)
NCT01131182 (2) [back to overview]Proportion of Participants With at Least One Symptomatic or Asymptomatic Hypoglycemic Event
NCT01131182 (2) [back to overview]Proportion of Participants With at Least One Symptomatic Hypoglycemic Event
NCT01137812 (7) [back to overview]Percent Change in High-density Lipoprotein Cholesterol (HDL-C) From Baseline to Week 52
NCT01137812 (7) [back to overview]Percentage of Patients With HbA1c <7% at Week 52
NCT01137812 (7) [back to overview]Percent Change in Triglycerides From Baseline to Week 52
NCT01137812 (7) [back to overview]Percent Change in Body Weight From Baseline to Week 52
NCT01137812 (7) [back to overview]Change in Fasting Plasma Glucose (FPG) From Baseline to Week 52
NCT01137812 (7) [back to overview]Change in HbA1c From Baseline to Week 52
NCT01137812 (7) [back to overview]Change in Systolic Blood Pressure (SBP) From Baseline to Week 52
NCT01155284 (2) [back to overview]2 Hour C-peptide AUC in Response to MMTT
NCT01155284 (2) [back to overview]2 Hour C-peptide AUC in Response to MMTT
NCT01177384 (4) [back to overview]Number of Participants Who Experienced at Least One Adverse Event
NCT01177384 (4) [back to overview]Number of Participants Who Discontinued Study Drug Due to an Adverse Event
NCT01177384 (4) [back to overview]Change From Baseline in Hemoglobin A1c (A1C) at Week 24
NCT01177384 (4) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24
NCT01177813 (4) [back to overview]Confirmed Hypoglycaemic Adverse Events
NCT01177813 (4) [back to overview]Change From Baseline to Week 24 in Body Weight
NCT01177813 (4) [back to overview]Change From Baseline to Week 24 in Systolic and Diastolic Blood Pressure (SBP and DBP)
NCT01177813 (4) [back to overview]Change From Baseline in Glycosylated Haemoglobin (HbA1c) After 24 Weeks
NCT01183104 (6) [back to overview]Number of Participants With Hypoglycaemia
NCT01183104 (6) [back to overview]Change From Baseline in Body Weight at 52 W
NCT01183104 (6) [back to overview]Change From Baseline in HbA1c at 52 W
NCT01183104 (6) [back to overview]Change From Baseline in HOMA-β at 52 W
NCT01183104 (6) [back to overview]Change From Baseline in Insulin/Proinsulin Ratio at 52 W
NCT01183104 (6) [back to overview]The Number of Participants Achieving HbA1c < 6.9 %
NCT01186562 (6) [back to overview]Insulin Independence
NCT01186562 (6) [back to overview]Insulin Independence
NCT01186562 (6) [back to overview]AUC C-peptide
NCT01186562 (6) [back to overview]Area Under the Curve (AUC) C-peptide (ng/dL*Min)
NCT01186562 (6) [back to overview]Acute C-peptide Response (ACR) to Glucose
NCT01186562 (6) [back to overview]Acute C-peptide Response (ACR) to Glucose
NCT01189890 (8) [back to overview]Number of Participants Discontinuing Study Treatment Due to An AE
NCT01189890 (8) [back to overview]Percentage of Participants With HbA1c <7.0% at Week 30
NCT01189890 (8) [back to overview]Percentage of Participants With HbA1c <6.5% at Week 30
NCT01189890 (8) [back to overview]Number of Participants With an Adverse Event of Symptomatic Hypoglycemia Up to Week 30
NCT01189890 (8) [back to overview]Number of Participants Experiencing An Adverse Event (AE)
NCT01189890 (8) [back to overview]Least Squares (LS) Mean Change From Baseline in Hemoglobin A1c (HbA1c) at Week 30
NCT01189890 (8) [back to overview]LS Mean Change From Baseline in Fasting Plasma Glucose (FPG) at Week 30
NCT01189890 (8) [back to overview]LS Mean Change From Baseline in Participant Body Weight at Week 30
NCT01195090 (27) [back to overview]Percentages of Patients With Nasopharyngitis
NCT01195090 (27) [back to overview]Percentages of Patients With Severe Hypoglycemia
NCT01195090 (27) [back to overview]The Percentages of Patient Achieving an A1C <7%
NCT01195090 (27) [back to overview]Percentages of Patients With Total Adverse Events (AE)
NCT01195090 (27) [back to overview]Baseline A1C
NCT01195090 (27) [back to overview]Baseline Alanine-aminotransferase (ALT)
NCT01195090 (27) [back to overview]Baseline Body Weight
NCT01195090 (27) [back to overview]Baseline Fasting Plasma Glucose
NCT01195090 (27) [back to overview]Baseline High Sensitive C-reactive Protein
NCT01195090 (27) [back to overview]Baseline High-density Lipoprotein Cholesterol (HDL-C)
NCT01195090 (27) [back to overview]Baseline Homoeostasis Model Assessment of Insulin Resistance (HOMA-IR)
NCT01195090 (27) [back to overview]Baseline Low-density Lipoprotein Cholesterol (LDL-C)
NCT01195090 (27) [back to overview]Baseline Total Cholesterol
NCT01195090 (27) [back to overview]Baseline Triglyceride (TG)
NCT01195090 (27) [back to overview]Body Weight Change
NCT01195090 (27) [back to overview]Change in Fasting High-density Lipoprotein Cholesterol(HDL-C)
NCT01195090 (27) [back to overview]Change in Fasting Low-density Lipoprotein Cholesterol (LDL-C)
NCT01195090 (27) [back to overview]Change in Fasting Plasma Alanine-aminotransferase (ALT)
NCT01195090 (27) [back to overview]Change in Fasting Total-cholesterol
NCT01195090 (27) [back to overview]Change in Fasting Triglycerides(TG)
NCT01195090 (27) [back to overview]Changes in Fasting Plasma Glucose
NCT01195090 (27) [back to overview]Changes in High Sensitive C-reactive Protein
NCT01195090 (27) [back to overview]Changes in Homoeostasis Model Assessment of Insulin Resistance (HOMA-IR)
NCT01195090 (27) [back to overview]Mean Change in Glycosylated Hemoglobin (A1C)
NCT01195090 (27) [back to overview]Percentages of Patients With Edema
NCT01195090 (27) [back to overview]Percentages of Patients With Gastrointestinal Adverse Events
NCT01195090 (27) [back to overview]Percentages of Patients With Mild to Moderate Hypoglycemia
NCT01272583 (8) [back to overview]Symptomatic Hormone Responses to Acute Hypoglycaemia.
NCT01272583 (8) [back to overview]Intact and Total Glucagon Like Peptide-1 (GLP-1), Intact and Total Gastric Inhibitory Peptide (GIP) Response to Acute Hypoglycaemia
NCT01272583 (8) [back to overview]Norepinephrine Response to Acute Hypoglycaemia
NCT01272583 (8) [back to overview]Glucagon Response to Acute Hypoglycaemia
NCT01272583 (8) [back to overview]Glucagon Response to Acute Hypoglycaemia
NCT01272583 (8) [back to overview]Growth Hormone Response to Acute Hypoglycaemia
NCT01272583 (8) [back to overview]Epinephrine Response to Acute Hypoglycaemia
NCT01272583 (8) [back to overview]Cortisol Response to Acute Hypoglycaemia
NCT01289990 (13) [back to overview]Body Weight (kg) Change From Baseline After 76 Weeks of Treatment
NCT01289990 (13) [back to overview]Changes From Baseline in Glycosylated Haemoglobin (HbA1c) (%) After 52 Weeks of Treatment
NCT01289990 (13) [back to overview]Changes From Baseline in HbA1c (%) After 76 Weeks of Treatment
NCT01289990 (13) [back to overview]Body Weight (kg) Change From Baseline After 52 Weeks of Treatment
NCT01289990 (13) [back to overview]Diastolic Blood Pressure: Change From Baseline After 52 Weeks of Treatment
NCT01289990 (13) [back to overview]HbA1c (%) Changes From Baseline After 76 Weeks of Treatment
NCT01289990 (13) [back to overview]Waist Circumference (cm) Change From Baseline After 76 Weeks of Treatment
NCT01289990 (13) [back to overview]Waist Circumference (cm) Change From Baseline After 52 Weeks of Treatment
NCT01289990 (13) [back to overview]Systolic Blood Pressure: Change From Baseline After 76 Weeks of Treatment
NCT01289990 (13) [back to overview]Systolic Blood Pressure: Change From Baseline After 52 Weeks of Treatment
NCT01289990 (13) [back to overview]Diastolic Blood Pressure: Change From Baseline After 76 Weeks of Treatment
NCT01289990 (13) [back to overview]Fasting Plasma Glucose Change From Baseline After 52 Weeks of Treatment
NCT01289990 (13) [back to overview]Fasting Plasma Glucose Change From Baseline After 76 Weeks of Treatment
NCT01296412 (4) [back to overview]Percentage of Participants Reaching A1C Goal of <6.5%
NCT01296412 (4) [back to overview]Change From Baseline in Hemoglobin A1c (A1C)
NCT01296412 (4) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG)
NCT01296412 (4) [back to overview]Percentage of Participants Reaching A1C Goal of <7.0%
NCT01334229 (6) [back to overview]Measurement of Apolipoprotein B48 and Apolipoprotein B100 Pool Sizes With Stable Isotope During Postprandial Period
NCT01334229 (6) [back to overview]Measurement of Apolipoprotein B48 and Apolipoprotein B100 Production Rates With Stable Isotope During Postprandial Period
NCT01334229 (6) [back to overview]Measurement of Glucagon-like Peptide-1 by ELISA
NCT01334229 (6) [back to overview]Measurement of Glucose
NCT01334229 (6) [back to overview]Measurement of Insulin
NCT01334229 (6) [back to overview]Measurement of Apolipoprotein B48 and Apolipoprotein B100 Fractional Catabolic Rates With Stable Isotope During Postprandial Period
NCT01336738 (7) [back to overview]Change From Baseline in Body Weight at Week 1, 2, 4, 8 and 12
NCT01336738 (7) [back to overview]Percentage of Participants With Greater Than or Equal to (>=) 1% or >= 2% Body Weight Loss From Baseline
NCT01336738 (7) [back to overview]Percentage of Participants Achieving Less Than (<) 6.5% or <7% Glycosylated Hemoglobin (HbA1c) Levels
NCT01336738 (7) [back to overview]Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 12
NCT01336738 (7) [back to overview]Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 1, 2, 4 and 8
NCT01336738 (7) [back to overview]Change From Baseline in Fasting Plasma Glucose at Week 1, 2, 4, 8 and 12
NCT01336738 (7) [back to overview]Percentage of Participants With Greater Than or Equal to (>=) 1% or >= 2% Body Weight Gain From Baseline
NCT01338870 (7) [back to overview]Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 1, 2, 4 and 8
NCT01338870 (7) [back to overview]Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 12
NCT01338870 (7) [back to overview]Percentage of Participants Achieving Less Than (<) 6.5% or <7% Glycosylated Hemoglobin (HbA1c) Levels
NCT01338870 (7) [back to overview]Percentage of Participants With Greater Than or Equal to (>=) 1% or >= 2% Gain in Body Weight From Baseline
NCT01338870 (7) [back to overview]Percentage of Participants With Greater Than or Equal to (>=) 1% or >= 2% Loss in Body Weight From Baseline
NCT01338870 (7) [back to overview]Change From Baseline in Fasting Plasma Glucose at Week 1, 2, 4, 8 and 12
NCT01338870 (7) [back to overview]Change From Baseline in Body Weight at Week 1, 2, 4, 8 and 12
NCT01340768 (2) [back to overview]Percentage of Participants With at Least One Symptomatic Hypoglycemic Event
NCT01340768 (2) [back to overview]Percentage of Participants With at Least One Symptomatic or Asymptomatic Hypoglycemic Event
NCT01354990 (4) [back to overview]Number of Participants With an Adverse Event
NCT01354990 (4) [back to overview]Number of Participants With Concomitant Conditions
NCT01354990 (4) [back to overview]Number of Participants With Concomitant Therapies
NCT01354990 (4) [back to overview]Age of Participants Prescribed Sitagliptin
NCT01357135 (2) [back to overview]Percentage of Participants With Strict Changes in Initial Dual Therapy
NCT01357135 (2) [back to overview]Median Duration (in Months) of Initial Dual Therapy
NCT01357148 (4) [back to overview]Age of Participants Prescribed Sitagliptin Phosphate/Metformin HCl
NCT01357148 (4) [back to overview]Number of Participants Taking Concomitant Medications
NCT01357148 (4) [back to overview]Number of Participants With an Adverse Event
NCT01357148 (4) [back to overview]Number of Participants With Concomitant Conditions
NCT01374568 (2) [back to overview]Bone Turnover in Subjects Treated With Sitagliptin When Compared to Those Treated With Placebo
NCT01374568 (2) [back to overview]Bone Turnover in Subjects Treated With Sitagliptin When Compared to Those Treated With Placebo.
NCT01376323 (14) [back to overview]Number of Participants With Clinical Chemistry Abnormalities of Potential Clinical Importance (PCI)
NCT01376323 (14) [back to overview]Number of Participants With HbA1c < 7.0% and < 6.5%
NCT01376323 (14) [back to overview]Number of Participants With Hematology Abnormalities of Potential Clinical Importance (PCI)
NCT01376323 (14) [back to overview]Summary of Homeostatic Model Assessment (HOMA) Index Calculated From Change From Baseline in Fasting Insulin and Fasting Glucose at Week 12
NCT01376323 (14) [back to overview]Number of Participants With Abnormal Electrocardiograms (ECGs) Findings
NCT01376323 (14) [back to overview]Change From Baseline in Fasting Plasma Glucose at Week 12
NCT01376323 (14) [back to overview]Change From Baseline in 12 Hour Non-esterified Fatty Acids (NEFA) and Glucose Weighted Mean Concentration Value at Day 2 and at Week 6
NCT01376323 (14) [back to overview]Change From Baseline in Fasting Insulin at Week 12
NCT01376323 (14) [back to overview]Change From Baseline in Fructosamine at Week 6 and Week 12
NCT01376323 (14) [back to overview]Change From Baseline in Glycated Hemoglobin (HbA1c) at Week 12
NCT01376323 (14) [back to overview]Change From Baseline in Heart Rate
NCT01376323 (14) [back to overview]Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
NCT01376323 (14) [back to overview]Number of Participants With Abnormal Urinalysis: Glucose, Protein, Blood and Ketones by Dipstick
NCT01376323 (14) [back to overview]Number of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)
NCT01378117 (9) [back to overview]Number of Subjects With Acute Renal Failure Among the Three Randomized Groups During Hospitalization
NCT01378117 (9) [back to overview]Mean Blood Glucose Levels Among the Three Groups at the Time of Hospitalization to 1st Day After Therapy
NCT01378117 (9) [back to overview]Percent of Blood Glucose Readings Within Target Range Between 70 and 140 mg/dL Among the Three Groups After 24 Hrs of Randomized Treatment
NCT01378117 (9) [back to overview]Number of Patients With Severe Hypoglycemic Episodes Among the 3 Treatment Groups
NCT01378117 (9) [back to overview]Number of Patients With Hypoglycemic Events Among the Treatment Groups
NCT01378117 (9) [back to overview]Number of Patients With a Mean Daily BG > 240 mg/dL After the 1st Day of Treatment Among the Treatment Groups
NCT01378117 (9) [back to overview]Mean Total Daily Dose of Insulin in Units/Day Given During Hospitalization Among the Three Groups
NCT01378117 (9) [back to overview]Number of Deaths Among the Subjects in Different Groups
NCT01378117 (9) [back to overview]Mean Length of Stay in Days in the Hospital Among Different Groups
NCT01405911 (4) [back to overview]Percent Change From Baseline in Glucose Total Area Under the Concentration Curve 0 to 2 Hours (AUC 0-2 Hrs) for Meal Tolerance Test (MTT) at Week 8
NCT01405911 (4) [back to overview]Percent Change From Baseline in Glucose Total Area Under the Concentration Curve 0 to 2 Hours (AUC 0-2 Hrs) for 75-gram Oral Glucose Tolerance Test (OGTT) at Week 7
NCT01405911 (4) [back to overview]Percentage of Participants Who Experienced One or More Adverse Events (AEs)
NCT01405911 (4) [back to overview]Percentage of Participants Who Discontinued Treatment Due to an Adverse Event (AE)
NCT01408888 (6) [back to overview]Pharmacokinetics: Maximum Observed Drug Concentration (Cmax) of Sitagliptin
NCT01408888 (6) [back to overview]Pharmacokinetics: Time of Maximum Observed Drug Concentration (Tmax) of LY2189265
NCT01408888 (6) [back to overview]Pharmacokinetics: Time of Maximum Observed Drug Concentration (Tmax) of Sitagliptin
NCT01408888 (6) [back to overview]Pharmacokinetics: Maximum Observed Drug Concentration (Cmax) of LY2189265
NCT01408888 (6) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve (AUC) of Sitagliptin
NCT01408888 (6) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve (AUC) of LY2189265
NCT01413542 (5) [back to overview]The Effect of Enalaprilat (ACE Inhibition), Sitagliptin (DPP4 Inhibition), or the Combination on the Vasodilator Response (Forearm Blood Flow) to Substance P (SP) and Bradykinin (Group 1) or Glucagon Like Peptide-1 and Brain Naturetic Peptide (Group 2).
NCT01413542 (5) [back to overview]Assess Effect of ACE and/or DPP4 Inhibition on Heart Rate Response to Substance P (SP)
NCT01413542 (5) [back to overview]Assess Tissue Type Plasminogen Activator (tPA) Release
NCT01413542 (5) [back to overview]Effect of Treatment (ACE or DPP4 Inhibition, or Combined) on Norepinephrine (NE) Release (Arterial Venous Gradient) in Response to Substance P (SP)
NCT01413542 (5) [back to overview]Effect of Treatment (DPP4 Inhibition vs. Placebo) on Venous GLP-1 Levels in Response to Arterial GLP-1 Infusion
NCT01449747 (5) [back to overview]Differences of DPP-4 Activity After Sitagliptin Treatment Between Responder and Non-responder Groups
NCT01449747 (5) [back to overview]Change in AUC of Active GLP-1, Total GLP-1 and Total GIP Between Before and After Sitagliptin Treatment
NCT01449747 (5) [back to overview]Plasma Concentration of Total Glucose-dependent Insulinotropic Polypeptide (GIP) Before and After Sitagliptin Treatment
NCT01449747 (5) [back to overview]Plasma Concentration of Active Glucagon-like Peptide 1 (GLP-1) Before and After Sitagliptin Treatment
NCT01449747 (5) [back to overview]Plasma Concentration of Total GLP-1 Before and After Sitagliptin Treatment
NCT01462266 (5) [back to overview]Change From Baseline in Daily Insulin Dose at Week 24
NCT01462266 (5) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24
NCT01462266 (5) [back to overview]Change From Baseline in Hemoglobin A1c (A1C) at Week 24
NCT01462266 (5) [back to overview]Percent of Participants Achieving Fasting Glucose Target at Any Time During the Study
NCT01462266 (5) [back to overview]Time to Achieve the Fasting Glucose Target
NCT01475461 (11) [back to overview]Number of Hypoglycemic Events (HAE) Episodes Per Participant
NCT01475461 (11) [back to overview]Number of Participants With Increase/Decrease From Baseline Vital Signs Data
NCT01475461 (11) [back to overview]Percentage of Participants With at Least 1 Hypoglycemic Events (HAE) Episode
NCT01475461 (11) [back to overview]Change From Baseline in Body Weight at Week 2, 4, 8, 12 and 14
NCT01475461 (11) [back to overview]Percentage of Participants Achieving Less Than 6.5 Percent and Less Than 7 Percent Glycosylated Hemoglobin (HbA1c) Levels at Week 12
NCT01475461 (11) [back to overview]Change From Baseline in Fasting Plasma Glucose at Week 1, 2, 4, 8, 12 and 14
NCT01475461 (11) [back to overview]Number of Participants With Abnormal Laboratory Values
NCT01475461 (11) [back to overview]Change From Baseline in Glycosylated Hemoglobin (HbA1C) at Week 12
NCT01475461 (11) [back to overview]Change From Baseline in Glycosylated Hemoglobin (HbA1C) at Week 2, 4 and 8
NCT01475461 (11) [back to overview]Number of Participants With Increase From Baseline Electrocardiogram (ECG)Data
NCT01475461 (11) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs)
NCT01477853 (11) [back to overview]Percent Change From Baseline in Very Low-density Lipoprotein Cholesterol (VLDL-C) at Week 16
NCT01477853 (11) [back to overview]Percent Change From Baseline in High Density Lipoprotein Cholesterol (HDL-C) at Week 16
NCT01477853 (11) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 16
NCT01477853 (11) [back to overview]Change From Baseline in Hemoglobin A1C (A1C) at Week 16
NCT01477853 (11) [back to overview]Number of Participants Who Discontinued Study Drug Due to an Adverse Event
NCT01477853 (11) [back to overview]Percent Change From Baseline in Apolipoprotein B (Apo B) at Week 16
NCT01477853 (11) [back to overview]Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C) at Week 16
NCT01477853 (11) [back to overview]Percent Change From Baseline in Non-high Density Lipoprotein Cholesterol (Non-HDL-C) at Week 16
NCT01477853 (11) [back to overview]Percent Change From Baseline in Total Cholesterol at Week 16
NCT01477853 (11) [back to overview]Percent Change From Baseline in Triglycerides at Week 16
NCT01477853 (11) [back to overview]Number of Participants Who Experienced at Least One Adverse Event
NCT01485614 (92) [back to overview]Skeletal Maturation at Week 20 - Females
NCT01485614 (92) [back to overview]Skeletal Maturation at Week 20 - Males
NCT01485614 (92) [back to overview]Skeletal Maturation at Week 54 - Females
NCT01485614 (92) [back to overview]Skeletal Maturation at Week 54 - Males
NCT01485614 (92) [back to overview]Participants With Worsening in Dental Status at Week 20
NCT01485614 (92) [back to overview]Participants With Worsening in Dental Status at Week 54
NCT01485614 (92) [back to overview]Change From Baseline in C-peptide 3-Hour AUC at Week 54
NCT01485614 (92) [back to overview]Change From Baseline in C-peptide 3-Hour AUC at Week 20
NCT01485614 (92) [back to overview]Change From Baseline in Bone-Specific Alkaline Phosphatase at Week 54 - Males
NCT01485614 (92) [back to overview]Change From Baseline in Bone-Specific Alkaline Phosphatase at Week 54 - Females
NCT01485614 (92) [back to overview]Change From Baseline in Bone-Specific Alkaline Phosphatase at Week 20 - Males
NCT01485614 (92) [back to overview]Percentage of Participants Initiating Glycemic Rescue Therapy by Week 54
NCT01485614 (92) [back to overview]Change From Baseline in Bone-Specific Alkaline Phosphatase at Week 20 - Females
NCT01485614 (92) [back to overview]Change From Baseline in Body Mass Index (BMI) at Week 20
NCT01485614 (92) [back to overview]Change From Baseline in A1C at Week 54
NCT01485614 (92) [back to overview]Change From Baseline In A1C at Week 20 (Analysis of Selected Arms: Sitagliptin and Placebo (Pooled))
NCT01485614 (92) [back to overview]Change From Baseline in 2-Hour Post-meal Glucose (PMG) at Week 20
NCT01485614 (92) [back to overview]Change From Baseline in 2-hour PMG at Week 54
NCT01485614 (92) [back to overview]Change From Baseline in 2-Hour Incremental PMG at Week 54
NCT01485614 (92) [back to overview]Change From Baseline in 2-hour Incremental PMG at Week 20
NCT01485614 (92) [back to overview]Baseline Glycated Hemoglobin (A1C) for the Placebo (Pooled) Arm
NCT01485614 (92) [back to overview]Baseline Fasting Plasma Glucose (FPG) for the Placebo (Pooled) Arm
NCT01485614 (92) [back to overview]Change From Baseline in Insulin 3-Hour AUC/ Glucose 3-Hour AUC Ratio at Week 20
NCT01485614 (92) [back to overview]Change From Baseline in Insulin 3-Hour AUC/Glucose 3-Hour AUC Ratio at Week 54
NCT01485614 (92) [back to overview]Change From Baseline in Insulin at Week 20 for Participants Not on Background Insulin
NCT01485614 (92) [back to overview]Change From Baseline in Insulin at Week 54 For Participants Not on Background Insulin
NCT01485614 (92) [back to overview]Change From Baseline in Insulin Excursion 3-Hour AUC at Week 20
NCT01485614 (92) [back to overview]Change From Baseline in Insulin Excursion 3-Hour AUC at Week 54
NCT01485614 (92) [back to overview]Change From Baseline in Insulin Excursion 3-Hour AUC/Glucose Excursion 3-Hour AUC Ratio at Week 20
NCT01485614 (92) [back to overview]Change From Baseline in Insulin Excursion 3-Hour AUC/Glucose Excursion 3-Hour AUC Ratio at Week 54
NCT01485614 (92) [back to overview]Change From Baseline in Proinsulin at Week 20 For Participants Not on Background Insulin
NCT01485614 (92) [back to overview]Change From Baseline in Homeostatic Model Assessment of Insulin Resistance (HOMA-IR) at Week 20 For Participants Not on Background Insulin
NCT01485614 (92) [back to overview]Change From Baseline in Proinsulin at Week 54 For Participants Not on Background Insulin
NCT01485614 (92) [back to overview]Change From Baseline in Proinsulin/Insulin Ratio at Week 20 for Participants Not on Background Insulin
NCT01485614 (92) [back to overview]Change From Baseline in Proinsulin/Insulin Ratio at Week 54 For Participants Not on Background Insulin
NCT01485614 (92) [back to overview]Change From Baseline in Tanner Stage for Pubic Hair at Week 20 - Females
NCT01485614 (92) [back to overview]Change From Baseline in Tanner Stage for Pubic Hair at Week 20 - Males
NCT01485614 (92) [back to overview]Change From Baseline in Tanner Stage for Pubic Hair at Week 54 - Females
NCT01485614 (92) [back to overview]Change From Baseline in Tanner Stage for Pubic Hair at Week 54 - Males
NCT01485614 (92) [back to overview]Change From Baseline in Tanner Staging for Breasts at Week 20 - Females
NCT01485614 (92) [back to overview]Change From Baseline in Tanner Staging for Breasts at Week 54 - Females
NCT01485614 (92) [back to overview]Change From Baseline in Tanner Staging for Genitalia at Week 20 - Males
NCT01485614 (92) [back to overview]Change From Baseline in Tanner Staging for Genitalia at Week 54 - Males
NCT01485614 (92) [back to overview]Change From Baseline in u-NTx/Creatinine Ratio at Week 54 - Females
NCT01485614 (92) [back to overview]Change From Baseline in u-NTx/Creatinine Ratio at Week 54 - Males
NCT01485614 (92) [back to overview]Change From Baseline in Urine N-terminal Cross-linking Telopeptide of Bone Collagen [u-NTx]/Creatinine Ratio at Week 20 - Females
NCT01485614 (92) [back to overview]Change From Baseline u-NTx/Creatinine Ratio at Week 20 - Males
NCT01485614 (92) [back to overview]Growth Velocity at Week 20 - Females
NCT01485614 (92) [back to overview]Growth Velocity at Week 20 - Males
NCT01485614 (92) [back to overview]Growth Velocity at Week 54 - Females
NCT01485614 (92) [back to overview]Growth Velocity at Week 54 - Males
NCT01485614 (92) [back to overview]Change From Baseline in Insulin 3-Hour AUC at Week 54
NCT01485614 (92) [back to overview]Change From Baseline in Insulin 3-hour AUC at Week 20
NCT01485614 (92) [back to overview]Change From Baseline in Homeostatic Model Assessment of β-cell Function (HOMA-β) at Week 20 For Participants Not on Background Insulin
NCT01485614 (92) [back to overview]Change From Baseline in HOMA-β at Week 54 For Participants Not on Background Insulin
NCT01485614 (92) [back to overview]Change From Baseline in HOMA-IR at Week 54 For Participants Not on Background Insulin
NCT01485614 (92) [back to overview]Change From Baseline in Hemoglobin A1C (A1C) at Week 20
NCT01485614 (92) [back to overview]Change From Baseline in Glucose Excursion 3-Hour AUC at Week 54
NCT01485614 (92) [back to overview]Change From Baseline in Glucose Excursion 3-Hour AUC at Week 20
NCT01485614 (92) [back to overview]Change From Baseline in Glucose 3-Hour Total Area Under the Curve (AUC) at Week 20
NCT01485614 (92) [back to overview]Mean Percent Change of Peripheral Blood Mononuclear Cells Expressing CD26 From Baseline at Week 20
NCT01485614 (92) [back to overview]Mean Percent Change of Peripheral Blood Mononuclear Cells Expressing CD26 From Baseline at Week 54
NCT01485614 (92) [back to overview]Number of Participants Who Discontinued Study Drug Due to an Adverse Event During Weeks 0-54
NCT01485614 (92) [back to overview]Number of Participants Who Experienced ≥1 Adverse Event During Weeks 0-56
NCT01485614 (92) [back to overview]Percent Change From Baseline in IGF-1 at Week 20 - Males
NCT01485614 (92) [back to overview]Percent Change From Baseline in IGF-1 at Week 54 - Males
NCT01485614 (92) [back to overview]Percent Change From Baseline in IGF-1 at Week 54 - Females
NCT01485614 (92) [back to overview]Percent Change From Baseline in IGF-BP3 at Week 20 - Males
NCT01485614 (92) [back to overview]Percent Change From Baseline in IGF-BP3 at Week 54 - Females
NCT01485614 (92) [back to overview]Percent Change From Baseline in IGF-BP3 at Week 54 - Males
NCT01485614 (92) [back to overview]Percent Change From Baseline in Insulin-like Growth Factor Binding Protein 3 (IGF-BP3) at Week 20 - Females
NCT01485614 (92) [back to overview]Percent Change From Baseline in Insulin-like Growth Factor-1 (IGF-1) at Week 20 - Females
NCT01485614 (92) [back to overview]Percentage of Participants Initiating Glycemic Rescue Therapy by Week 20
NCT01485614 (92) [back to overview]Change From Baseline in BMI at Week 54
NCT01485614 (92) [back to overview]Percentage of Participants Who Discontinued Study Drug Due to an Adverse Event During Weeks 0-54 (Analysis of Selected Arms: Sitagliptin and Placebo/Metformin)
NCT01485614 (92) [back to overview]Percentage of Participants Who Experienced ≥1 Adverse Event During Weeks 0-56 (Analysis of Selected Arms: Sitagliptin and Placebo/Metformin)
NCT01485614 (92) [back to overview]Percentage of Participants With A1C at Goal (<6.5%) at Week 20
NCT01485614 (92) [back to overview]Percentage of Participants With A1C at Goal (<6.5%) at Week 20 (Analysis of Selected Arms: Sitagliptin and Placebo (Pooled))
NCT01485614 (92) [back to overview]Change From Baseline in FPG at Week 20 (Analysis of Selected Arms: Sitagliptin and Placebo (Pooled))
NCT01485614 (92) [back to overview]Change From Baseline in Glucose 3-Hour AUC at Week 54
NCT01485614 (92) [back to overview]Change From Baseline in FPG at Week 54
NCT01485614 (92) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 20
NCT01485614 (92) [back to overview]Change From Baseline in Calcitonin at Week 54 - Males
NCT01485614 (92) [back to overview]Change From Baseline in Calcitonin at Week 54 - Females
NCT01485614 (92) [back to overview]Percentage of Participants With A1C at Goal (<6.5%) at Week 54
NCT01485614 (92) [back to overview]Percentage of Participants With A1C at Goal (<7.0%) at Week 20
NCT01485614 (92) [back to overview]Percentage of Participants With A1C at Goal (<7.0%) at Week 20 (Analysis of Selected Arms: Sitagliptin and Placebo (Pooled))
NCT01485614 (92) [back to overview]Percentage of Participants With A1C at Goal (<7.0%) at Week 54
NCT01485614 (92) [back to overview]Change From Baseline in Calcitonin at Week 20 - Males
NCT01485614 (92) [back to overview]Change From Baseline in Calcitonin at Week 20 - Females
NCT01485614 (92) [back to overview]Change From Baseline in C-Peptide Excursion 3-Hour AUC at Week 54
NCT01485614 (92) [back to overview]Change From Baseline in C-peptide Excursion 3-Hour AUC at Week 20
NCT01488279 (3) [back to overview]Insulin Sensitivity
NCT01488279 (3) [back to overview]Change in Glucose Response
NCT01488279 (3) [back to overview]Change in Insulin Secretion (AIRg or Acute Insulinogenic Response to Glucose)
NCT01490918 (11) [back to overview]The Change of Glycated Hemoglogin(HbA1c) From Baseline to 16 Weeks of Treatment
NCT01490918 (11) [back to overview]The Change of HbA1c From Baseline to 24 Weeks of Treatment
NCT01490918 (11) [back to overview]The Change of PPG2hr From Baseline to 24 Weeks of Treatment
NCT01490918 (11) [back to overview]Changes in MAGE of Glucose During CGMS Between 2 Group(Group 1 vs Group 2),
NCT01490918 (11) [back to overview]Changes in Mean Glucose During CGMS Between 3 Group
NCT01490918 (11) [back to overview]Changes in Variation of Glucose During CGMS Between 3 Group
NCT01490918 (11) [back to overview]Change in Active GLP-1 at 0 Minute During Mixed Meal Test Between 2 Groups (Group 1, group2)
NCT01490918 (11) [back to overview]Change in Active GLP-1 at 120 Minute During Mixed Meal Test Between 2 Groups (Group 1, group2)
NCT01490918 (11) [back to overview]Changes in Glucagon During Meal Tolerance Test Between 2 Group(Group 1 vs Group 2),
NCT01490918 (11) [back to overview]Changes in Glucose During Meal Tolerance Test Between 2 Group(Group 1 vs Group 2),
NCT01490918 (11) [back to overview]Changes in Insulin During Mixed Meal Tolerance Test Between 2 Group(Group 1 vs Group 2),
NCT01512797 (5) [back to overview]Active GLP-1
NCT01512797 (5) [back to overview]Change in Area Under the Curve (AUC) Glucose Levels After Mixed Meal Test
NCT01512797 (5) [back to overview]Change in Postprandial Glucose Levels After Mixed Meal Test
NCT01512797 (5) [back to overview]Effect of Sitagliptin vs Placebo on Satiety in Patients With Type 2 Diabetes After Gastric Bypass Surgery
NCT01512797 (5) [back to overview]Occurrence of Side Effects In Relation to Sitagliptin
NCT01519674 (11) [back to overview]Prandial Plasma Glucose (PPG) Increments at Lunch.
NCT01519674 (11) [back to overview]Prandial Plasma Glucose (PPG) Increments at Dinner.
NCT01519674 (11) [back to overview]Prandial Plasma Glucose (PPG) Increments at Breakfast
NCT01519674 (11) [back to overview]Change From Baseline in Patient Reported Outcome by Use of the Treatment Related Impact Measure - Diabetes.
NCT01519674 (11) [back to overview]Adverse Events (AEs)
NCT01519674 (11) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG)
NCT01519674 (11) [back to overview]Change From Baseline in HbA1c (Glycosylated Haemoglobin)
NCT01519674 (11) [back to overview]Number of Treatment Emergent Hypoglycaemic Episodes (Nocturnal and Day-time) Classified Both According to the American Diabetes Association (ADA) Definition and to an Additional Definition for Minor Episodes.
NCT01519674 (11) [back to overview]Responder for HbA1c, Proportion of Subjects Achieving Pre-defined HbA1c Targets (HbA1c ≤ 6.5%)
NCT01519674 (11) [back to overview]Responder for HbA1c, Proportion of Subjects Achieving Pre-defined HbA1c Targets (HbA1c < 7.0%)
NCT01519674 (11) [back to overview]Prandial Plasma Glucose (PPG) Overall Mean Increment.
NCT01530178 (1) [back to overview]Better Targeted Blood Glucose Levels
NCT01545388 (4) [back to overview]Percentage of Participants Who Experienced at Least One Adverse Event
NCT01545388 (4) [back to overview]Number of Participants Who Discontinued Study Drug Due to an Adverse Event
NCT01545388 (4) [back to overview]Change From Baseline to Week 24 in Hemoglobin A1c (HbA1c)
NCT01545388 (4) [back to overview]Change From Baseline to Week 24 in Fasting Plasma Glucose (FPG)
NCT01549964 (3) [back to overview]Change From Baseline in Glycosylated Hemoglobin (HbA1c)
NCT01549964 (3) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG)
NCT01549964 (3) [back to overview]Incidence of HbA1c <7%
NCT01552694 (5) [back to overview]Inflammatory Biomarker 3: Serum D-dimer Concentration
NCT01552694 (5) [back to overview]Inflammatory Biomarker 2: Plasma IL-6 Concentration
NCT01552694 (5) [back to overview]Inflammatory Biomarker 1: Plasma hsCRP Concentration
NCT01552694 (5) [back to overview]Percent Change in Blood Endothelial Progenitor Cells
NCT01552694 (5) [back to overview]Fold Change in Adipose Inflammation Marker CCL2 (MCP-1) mRNA Expression
NCT01557504 (15) [back to overview]AUC 0-24 of Metformin Following Single Administration of Sitagliptin/Metformin XR
NCT01557504 (15) [back to overview]AUC 0-24 of Sitagliptin Following Single Administration of Sitagliptin/Metformin XR
NCT01557504 (15) [back to overview]Cmax of Metformin Following Single Dose Administration of Sitagliptin/Metformin XR
NCT01557504 (15) [back to overview]Cmax of Sitagliptin Following Single Dose Administration of Sitagliptin/Metformin XR
NCT01557504 (15) [back to overview]Number of Participants Who Experienced an Abnormal Vital Sign Value
NCT01557504 (15) [back to overview]Number of Participants Who Successfully Swallowed Study Medication (Med) on Day 2
NCT01557504 (15) [back to overview]Number of Participants Who Successfully Swallowed Study Med on Day 9
NCT01557504 (15) [back to overview]Number of Participants Who Successfully Swallowed Study Med on Day 6
NCT01557504 (15) [back to overview]Number of Participants Who Successfully Swallowed Study Med on Day 4
NCT01557504 (15) [back to overview]Tmax of Sitagliptin and Metformin Following Single Dose Administration of Sitagliptin/Metformin XR
NCT01557504 (15) [back to overview]Number of Participants Who Experienced an Adverse Event (AE)
NCT01557504 (15) [back to overview]Number of Participants Who Discontinued Study Drug Due to an AE
NCT01557504 (15) [back to overview]Apparent Terminal Half Life (t1/2) of Sitagliptin Following Single Dose Administration of Sitagliptin/Metformin XR
NCT01557504 (15) [back to overview]Area Under the Curve 0 to Infinity (AUC 0-∞) of Sitagliptin Following Single Administration of Sitagliptin/Metformin XR
NCT01557504 (15) [back to overview]Area Under the Curve 0 to Last (AUC 0-last) of Sitagliptin Following Single Administration of Sitagliptin/Metformin XR
NCT01582308 (5) [back to overview]Percent Inhibition of Dipeptidyl Peptidase IV (DPP-4) Activity at Trough
NCT01582308 (5) [back to overview]Pharmacokinetic Analysis: Area Under the Curve 0-12 Hours (AUC 0-12hr) for Vildagliptin 50 mg BID
NCT01582308 (5) [back to overview]Pharmacokinetic Analysis: Area Under the Curve 0-24 Hours (AUC 0-24hr)
NCT01582308 (5) [back to overview]Pharmacokinetic Analysis: Peak Plasma Drug Concentration (Cmax)
NCT01582308 (5) [back to overview]Pharmacokinetic Analysis: Time to the Peak Plasma Drug Concentration (Tmax)
NCT01590771 (11) [back to overview]Number of Participants Who Experienced an Adverse Event
NCT01590771 (11) [back to overview]Number of Participants Who Discontinued Study Drug Due to an Adverse Event
NCT01590771 (11) [back to overview]Change From Baseline in FPG Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea Alone or in Combination With Metformin
NCT01590771 (11) [back to overview]Change From Baseline in FPG Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea Alone
NCT01590771 (11) [back to overview]Change From Baseline in 2-hr PMG Levels at Week 24 in Participants Receiving Sitagliptin and a Sulfonylurea in Combination With Metformin
NCT01590771 (11) [back to overview]Change From Baseline in 2-hr PMG Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea Alone
NCT01590771 (11) [back to overview]Change From Baseline in A1C Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea Alone
NCT01590771 (11) [back to overview]Change From Baseline in A1C Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea Alone or in Combination With Metformin
NCT01590771 (11) [back to overview]Change From Baseline in A1C Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea in Combination With Metformin
NCT01590771 (11) [back to overview]Change From Baseline in 2-hr PMG Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea Alone or in Combination With Metformin
NCT01590771 (11) [back to overview]Change From Baseline in FPG Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea in Combination With Metformin
NCT01590797 (5) [back to overview]Number of Participants With One or More Adverse Events
NCT01590797 (5) [back to overview]Number of Participants Discontinuing Study Medication Due to an AE
NCT01590797 (5) [back to overview]Change From Baseline in Hemoglobin A1C (HbA1C) Levels at Week 24 in Participants Receiving Insulin Alone or in Combination With Metformin
NCT01590797 (5) [back to overview]Change From Baseline in HbA1C Levels at Week 24 in Participants Receiving Insulin in Combination With Metformin
NCT01590797 (5) [back to overview]Change From Baseline in 2-Hour Post Meal Glucose Levels at Week 24 in Participants Receiving Insulin Alone or in Combination With Metformin
NCT01600703 (2) [back to overview]Apolipoprotein B100 Production Rate After Acute Oral Administration of 100mg Sitagliptin (Compared to Placebo)
NCT01600703 (2) [back to overview]Apolipoprotein B48 Production Rate After Acute Oral Administration of 100mg Sitagliptin (Compared to Placebo)
NCT01610154 (9) [back to overview]Change From Baseline in Insulin Sensitivity in Patients With Different BMI
NCT01610154 (9) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG)
NCT01610154 (9) [back to overview]Change From Baseline in Hemoglobin A1c (HbA1c)
NCT01610154 (9) [back to overview]Change From Baseline in Insulin Sensitivity
NCT01610154 (9) [back to overview]Change From Baseline in Pancreatic α Cell Function
NCT01610154 (9) [back to overview]Change From Baseline in Pancreatic α Cell Function in Patients With Different BMI
NCT01610154 (9) [back to overview]Change From Baseline in Pancreatic β Cell Function
NCT01610154 (9) [back to overview]Change From Baseline in Pancreatic β Cell Function in Patients With Different BMI
NCT01610154 (9) [back to overview]Change From Baseline in Postprandial Plasma Glucose (PPG)
NCT01652729 (5) [back to overview]Percentage of Subjects Achieving HbA1c <7% at Week 28
NCT01652729 (5) [back to overview]Change in HbA1c (Glycosylated Hemoglobin) From Baseline to Week 28
NCT01652729 (5) [back to overview]Change in Fasting Plasma Glucose Concentrations From Baseline to Week 28
NCT01652729 (5) [back to overview]Change in Body Weight (kg) From Baseline to Week 28
NCT01652729 (5) [back to overview]Change in 2-hour Postprandial Glucose Concentrations From Baseline to Week 16 (Visit 8)
NCT01678820 (13) [back to overview]Percent Change From Baseline in Total Cholesterol (TC) at Week 16
NCT01678820 (13) [back to overview]Number of Participants Who Experienced at Least One Adverse Event (AE)
NCT01678820 (13) [back to overview]Number of Participants Who Discontinued Study Drug Due to an Adverse Event
NCT01678820 (13) [back to overview]Change From Baseline in A1C at Week 16 (Sitagliptin/Simvastatin FDC vs. Simvastatin)
NCT01678820 (13) [back to overview]Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) at Week 16
NCT01678820 (13) [back to overview]Percent Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C) at Week 16
NCT01678820 (13) [back to overview]Percent Change From Baseline in Apolipoprotein B (Apo B) at Week 16
NCT01678820 (13) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 16
NCT01678820 (13) [back to overview]Change From Baseline in Hemoglobin A1C (A1C) at Week 16 (Sitagliptin/Simvastatin FDC vs. Sitagliptin)
NCT01678820 (13) [back to overview]Percentage of Participants With A1C Level <7% at Week 16
NCT01678820 (13) [back to overview]Percent Change From Baseline in Non-high Density Lipoprotein Cholesterol (Non-HDL-C) at Week 16
NCT01678820 (13) [back to overview]Percent Change From Baseline in Very Low-density Lipoprotein Cholesterol (VLDL-C) at Week 16
NCT01678820 (13) [back to overview]Percent Change From Baseline in Triglycerides (TG) at Week 16
NCT01686932 (11) [back to overview]Percentage Change From Baseline of Pro-insulin/C-peptide Ratios After 8 Weeks of Treatment Period 1 & Period 2
NCT01686932 (11) [back to overview]Change From Baseline of Inflammatory Biomarkers Interleukin 6 (IL-6) After 8 Weeks of Treatment in Period 1 & Period 2
NCT01686932 (11) [back to overview]Change From Baseline of Inflammatory Biomarkers High Sensitivity C-reactive Protein (hsCRP) After 8 Weeks of Treatment in Period 1 & Period 2
NCT01686932 (11) [back to overview]Number of Participants With ECG Abnormalities Depending on Hypoglycemic Events After 8 Weeks of Treatment Period 1 & Period 2
NCT01686932 (11) [back to overview]Number of Occurrence of Pre-defined ECG Findings During 4 Days of Continuous ECG Monitoring at Baseline and in the 8th Week of Periods 1 and 2
NCT01686932 (11) [back to overview]Number of Hypoglycemic Events During Vildagliptin Treatment Compared to Sitagliptin Treatment.
NCT01686932 (11) [back to overview]Number of Severe Hypoglycemic Events During Vildagliptin Treatment Compared to Sitagliptin Treatment After 8 Weeks of Treatment in Period 1 and Period 2
NCT01686932 (11) [back to overview]Mean Duration of Hypoglycemic Events (Min.) Measured With Continuous Glucose Monitoring (CGM) Over 4 Days After 8 Weeks of Treatment for Period 1 & Period 2
NCT01686932 (11) [back to overview]Mean Amplitudes of Hypoglycemic Events (mmol/L) Measured With Continuous Glucose Monitoring (CGM) Over 4 Days After 8 Weeks of Treatment for Period 1 & Period 2
NCT01686932 (11) [back to overview]Hypoglycemic Profile of Vildagliptin Compared to Sitagliptin Over 4 Days After 8 Weeks of Treatment in Period 1 & 2
NCT01686932 (11) [back to overview]Glucose Fluctuations During the Day Under Vildagliptin Treatment Compared to Sitagliptin Treatment on Day 2 After 8 Weeks of Treatment Period 1 & Period 2
NCT01701973 (8) [back to overview]Aim 1: Percent Change From Baseline in Forearm Blood Flow
NCT01701973 (8) [back to overview]Aim 2: Venous Blood Sampling for Tissue Plasminogen Activator (TPA) Activity Levels
NCT01701973 (8) [back to overview]Aim 2: Percent Change From Baseline in Forearm Vascular Resistance
NCT01701973 (8) [back to overview]Aim 2: Percent Change From Baseline in Forearm Blood Flow
NCT01701973 (8) [back to overview]Aim 2: Measurement of Growth Hormone (GH) Levels
NCT01701973 (8) [back to overview]Aim 1: Venous Blood Sampling for Tissue Plasminogen Activator (TPA) Activity Levels
NCT01701973 (8) [back to overview]Aim 1: Percent Change From Baseline in Forearm Vascular Resistance
NCT01701973 (8) [back to overview]Aim 1: Stimulated Peak Growth Hormone Level
NCT01702298 (8) [back to overview]Change From Baseline in Total Cholesterol (TC)
NCT01702298 (8) [back to overview]Change From Baseline in Non-high Density Lipoprotein Cholesterol (Non-HDL-C)
NCT01702298 (8) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG)
NCT01702298 (8) [back to overview]Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C)
NCT01702298 (8) [back to overview]Change From Baseline in Triglycerides (TG)
NCT01702298 (8) [back to overview]Percentage of Participants Who Experienced at Least One Adverse Event
NCT01702298 (8) [back to overview]Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C)
NCT01702298 (8) [back to overview]Number of Participants Who Discontinued Study Drug Due to an Adverse Event
NCT01703221 (7) [back to overview]Percentage of Participants Who Discontinued From the Study Due to an Adverse Event During Phase A
NCT01703221 (7) [back to overview]Percentage of Participants Who Experienced at Least One Adverse Event During the Overall Study
NCT01703221 (7) [back to overview]Percentage of Participants Who Experienced at Least One Adverse Event During Phase A
NCT01703221 (7) [back to overview]Percentage of Participants Who Discontinued From the Study Due to an Adverse Event During the Overall Study
NCT01703221 (7) [back to overview]Change From Baseline for 2-hour Post Meal Glucose (PMG) at Week 24
NCT01703221 (7) [back to overview]Change From Baseline for Fasting Plasma Glucose (FPG) at Week 24
NCT01703221 (7) [back to overview]Change From Baseline for Hemoglobin A1c (HbA1c) at Week 24
NCT01709305 (7) [back to overview]Percentage of Participants With a Gastrointestinal (GI) AE of Nausea (Phase 2)
NCT01709305 (7) [back to overview]Percentage of Participants With a GI AE of Abdominal Pain (Phase 2)
NCT01709305 (7) [back to overview]Percentage of Participants With a GI AE of Diarrhea (Phase 2)
NCT01709305 (7) [back to overview]Percentage of Participants With a GI AE of Vomiting (Phase 2)
NCT01709305 (7) [back to overview]Percentage of Participants With Hypoglycemia Events (Phase 2)
NCT01709305 (7) [back to overview]Change From Phase 2 Baseline to Week 44 in Participant Body Weight (Phase 2)
NCT01709305 (7) [back to overview]Change From Phase 2 Baseline to Week 44 in Hemoglobin A1c (HbA1c) Levels (Phase 2)
NCT01720264 (4) [back to overview]The Percent of Subjects Engrafting by Day +30 After Transplantation
NCT01720264 (4) [back to overview]Time to Neutrophil Engraftment
NCT01720264 (4) [back to overview]Time to Platelet Engraftment
NCT01720264 (4) [back to overview]Number of Subjects With Treatment Related Adverse Events Grade 3 and 4 Non-hematological Toxicities
NCT01760447 (15) [back to overview]Percentage of Participants With A1C at Goal (<6.5%) at Week 54
NCT01760447 (15) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 20
NCT01760447 (15) [back to overview]Change From Baseline in A1C at Week 54
NCT01760447 (15) [back to overview]Percentage of Participants With A1C at Goal (<7.0%) at Week 54
NCT01760447 (15) [back to overview]Number of Participants Who Experienced ≥1 Adverse Event During Weeks 0-20
NCT01760447 (15) [back to overview]Baseline A1C
NCT01760447 (15) [back to overview]Percentage of Participants With A1C at Goal (<7.0%) at Week 20
NCT01760447 (15) [back to overview]Percentage of Participants With A1C at Goal (<6.5%) at Week 20
NCT01760447 (15) [back to overview]Percentage of Participants Initiating Insulin Glargine During Weeks 20-54
NCT01760447 (15) [back to overview]Percentage of Participants Initiating Glycemic Rescue Therapy by Week 20
NCT01760447 (15) [back to overview]Number of Participants Who Experienced ≥1 Adverse Event During Weeks 0-56
NCT01760447 (15) [back to overview]Change From Baseline in A1C at Week 20
NCT01760447 (15) [back to overview]Number of Participants Who Discontinued Study Drug Due to Experiencing an Adverse Event During Weeks 0-54
NCT01760447 (15) [back to overview]Number of Participants Who Discontinued Study Drug Due to Experiencing an Adverse Event During Weeks 0-20
NCT01760447 (15) [back to overview]Change From Baseline in FPG at Week 54
NCT01834274 (2) [back to overview]Change From Baseline in Glycosylated Hemoglobin (HbA1c)
NCT01834274 (2) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG)
NCT01841697 (6) [back to overview]Percentage of Participants Who Discontinued Study Drug Due to an Adverse Event
NCT01841697 (6) [back to overview]Percentage of Participants Achieving an A1C Goal <7.0% After 24 Weeks of Treatment
NCT01841697 (6) [back to overview]Percentage of Participants Who Experienced at Least One Adverse Event
NCT01841697 (6) [back to overview]Change From Baseline in A1C at Week 24
NCT01841697 (6) [back to overview]Change From Baseline in FPG at Week 24
NCT01841697 (6) [back to overview]Percentage of Participants Achieving an A1C Goal <6.5% After 24 Weeks of Treatment
NCT01845831 (11) [back to overview]Acute Renal Failure Rate
NCT01845831 (11) [back to overview]Length of Hospital Stay
NCT01845831 (11) [back to overview]Mean Blood Glucose Concentration After First Day of Treatment
NCT01845831 (11) [back to overview]Mean Percentage of Blood Glucose Readings Between 3.9 - 10.0 mmol/L
NCT01845831 (11) [back to overview]Mean Percentage of Blood Glucose Readings Between 3.9 - 7.8 mmol/L
NCT01845831 (11) [back to overview]Hospital Mortality Rate
NCT01845831 (11) [back to overview]Mean Percentage of Blood Glucose Readings Greater Than 13.3 mmol/L
NCT01845831 (11) [back to overview]Mean Percentage of Blood Glucose Readings Between 5.6 - 7.8 mmol/L
NCT01845831 (11) [back to overview]Change in HbA1C
NCT01845831 (11) [back to overview]Number of Participants With a Hypoglycemic Event
NCT01845831 (11) [back to overview]Total Daily Insulin Dose
NCT01856907 (11) [back to overview]Triglyceride/HDL-Cholesterol Ratio
NCT01856907 (11) [back to overview]Waist Circumference
NCT01856907 (11) [back to overview]Waist-to-Height Ratio
NCT01856907 (11) [back to overview]Oral Disposition Index
NCT01856907 (11) [back to overview]Normalization of Glucose Levels
NCT01856907 (11) [back to overview]Mean Blood Glucose Level From the Oral Glucose Tolerance Test (OGTT)
NCT01856907 (11) [back to overview]Matsuda Index of Insulin Sensitivity
NCT01856907 (11) [back to overview]Liver Enzymes as Safety Measure
NCT01856907 (11) [back to overview]Fasting Insulin Resistance
NCT01856907 (11) [back to overview]Fasting Blood Glucose
NCT01856907 (11) [back to overview]Body Mass Index
NCT01859793 (3) [back to overview]Brachial Artery Flow Mediated Dilation
NCT01859793 (3) [back to overview]Circulating Inflammatory Markers VCAM-1
NCT01859793 (3) [back to overview]Circulating Inflammatory Marker ICAM-1
NCT01879228 (1) [back to overview]Change in Second-phase Insulin Response Derived From the Glucose-potentiated Arginine Test as a Measure of β-cell Sensitivity to Glucose at Baseline and at 6 Months
NCT01907854 (7) [back to overview]Change in Fasting Blood Lipids
NCT01907854 (7) [back to overview]Number of Treatment Emergent Adverse Events (TEAEs)
NCT01907854 (7) [back to overview]Subjects Who Achieve HbA1c Below 7.0% (53 mmol/Mol) (American Diabetes Association Target) (y/n)
NCT01907854 (7) [back to overview]Change in Systolic Blood Pressure and Diastolic Blood Pressure
NCT01907854 (7) [back to overview]Change in HbA1c (Glycosylated Haemoglobin)
NCT01907854 (7) [back to overview]Change in Fasting Plasma Glucose
NCT01907854 (7) [back to overview]Change in Body Weight
NCT01928199 (5) [back to overview]Hemoglobin A1c, 6 Month
NCT01928199 (5) [back to overview]Normal 2-hour Oral Glucose Tolerance Test-derived Blood Sugar
NCT01928199 (5) [back to overview]6 Month OGTT Result (Completion of Washout From Study Drug)
NCT01928199 (5) [back to overview]2-hour Oral Glucose Tolerance Test-derived Blood Sugar
NCT01928199 (5) [back to overview]Hemoglobin A1c, 3 Month
NCT01930188 (6) [back to overview]Change in HbA1c (Glycosylated Haemoglobin) From Baseline
NCT01930188 (6) [back to overview]Change in Patient Reported Outcome (PRO) Questionnaire Diabetes Treatment Satisfaction Questionnaire Status (DTSQs) From Baseline
NCT01930188 (6) [back to overview]Change in Systolic and Diastolic Blood Pressure From Baseline
NCT01930188 (6) [back to overview]Subjects Who Achieved HbA1c Below or Equal to 6.5% (48 mmol/Mol) American Association of Clinical Endocrinologists (AACE) Target (Yes/no)
NCT01930188 (6) [back to overview]Change in Fasting Plasma Glucose (FPG) From Baseline
NCT01930188 (6) [back to overview]Change in Body Weight From Baseline
NCT01933672 (15) [back to overview]Plasma PF-04937319 Time for Cmax (Tmax) on Day 14
NCT01933672 (15) [back to overview]Plasma PF-04937319 Lowest Observed Concentration During the 24-hour Period (Cmin) on Day 14
NCT01933672 (15) [back to overview]Plasma PF-04937319 Highest Observed Concentration (Cmax) on Day 14
NCT01933672 (15) [back to overview]Plasma PF-04937319 Average Concentration Over the 24-hour Period (Cav) on Day 14
NCT01933672 (15) [back to overview]Plasma PF-04937319 Apparent Clearance (CL/F) on Day 14
NCT01933672 (15) [back to overview]Change From Baseline in Weighted Mean Daily Glucose (WMDG) at Day 14
NCT01933672 (15) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Day 14
NCT01933672 (15) [back to overview]Change From Baseline in Body Weight (kg)
NCT01933672 (15) [back to overview]Number of Participants With Post-baseline Electrocardiograms (ECGs) Data Met Criteria of Potential Clinical Concern
NCT01933672 (15) [back to overview]Plasma PF-04937319 Area Under the Concentration Time Curve From Time 0 to 24 Hours (AUC24) of PF-04937319 at Day 14
NCT01933672 (15) [back to overview]Number of Participants With Vital Signs Data Met Criteria of Potential Clinical Concern
NCT01933672 (15) [back to overview]Change From Baseline in Pre-meal Insulin on Day 14
NCT01933672 (15) [back to overview]Incidence of All Causality Treatment-Emergent Adverse Event by Preferred Term (Frequency Rate >5%)
NCT01933672 (15) [back to overview]Frequency of Laboratory Test Abnormalities Reported in Any Treatment Group
NCT01933672 (15) [back to overview]Change From Baseline in Pre-meal C-Peptide on Day 14
NCT01937598 (9) [back to overview]AUC C-peptide
NCT01937598 (9) [back to overview]AUC Active GLP-1
NCT01937598 (9) [back to overview]AUC Active GIP
NCT01937598 (9) [back to overview]AUC Total GIP
NCT01937598 (9) [back to overview]AUC Plasma Glucose
NCT01937598 (9) [back to overview]AUC Insulin
NCT01937598 (9) [back to overview]AUC Glucagon
NCT01937598 (9) [back to overview]Incremental Area Under the Plasma Glucose (BG) Concentration-time Profile (AUC)
NCT01937598 (9) [back to overview]AUC Total GLP-1
NCT01951339 (8) [back to overview]Change in Oxygen Uptake Kinetics (VO2 Kinetics)
NCT01951339 (8) [back to overview]Changes From Baseline in 31P Measurement: Free Pi Time Constant
NCT01951339 (8) [back to overview]Changes From Baseline in 31P Measurement: Adenosine Triphosphate (ATP) Peaks
NCT01951339 (8) [back to overview]Changes From Baseline in 31P Measurement: Adenosine Diphosphate (ADP) Time Constant
NCT01951339 (8) [back to overview]Peak Oxygen Consumption (VO2peak).
NCT01951339 (8) [back to overview]Changes From Baseline in Echocardiographic Measures (Stroke Volume)
NCT01951339 (8) [back to overview]Changes From Baseline in 31P Measurement: Phosphocreatine Time Constant
NCT01951339 (8) [back to overview]Changes From Baseline in 31P Measurement: pH
NCT01963845 (5) [back to overview]Percentage Change in Liver Fat Relative to Baseline Assessed by MRI-PDFF
NCT01963845 (5) [back to overview]ALT, Alanine Aminotransferase
NCT01963845 (5) [back to overview]AST, Aspartate Aminotransferase
NCT01963845 (5) [back to overview]HOMA-IR, Homeostatic Model Assessment of Insulin Resistance
NCT01963845 (5) [back to overview]LDL, Low-density Lipoprotein
NCT01991197 (16) [back to overview]The Change in the Psoriasis Area and Severity Index (PASI) From Baseline to 16 Weeks in Psoriasis Patients With Type 2 Diabetes Treated With Sitagliptin Compared to Patients Treated With Gliclazide.
NCT01991197 (16) [back to overview]The Change in PASI From Baseline to 32 Weeks in Psoriasis Patients With Type 2 Diabetes Treated With Sitagliptin Compared to Patients Treated With Gliclazide.
NCT01991197 (16) [back to overview]The Change in Levels of Total Cholesterol From Baseline to 16 Weeks in the Sitagliptin and Gliclazide Arms.
NCT01991197 (16) [back to overview]The Change in Levels of Systolic Blood Pressure From Baseline to 16 Weeks in the Sitagliptin and Gliclazide Arms.
NCT01991197 (16) [back to overview]The Change in Levels of Serum Glucose From Baseline to 16 Weeks in the Sitagliptin and Gliclazide Arms.
NCT01991197 (16) [back to overview]The Change in Levels of High Sensitivity C-reactive Protein From Baseline to 16 Weeks in the Sitagliptin and Gliclazide Arms.
NCT01991197 (16) [back to overview]The Effect of Treatment With Sitagliptin and With Gliclazide From Baseline to 16 Weeks on the Change in Dipeptidyl Peptidase-4 Levels in the Skin (in a Sub-group of Participants Willing to Undergo Skin Biopsies).
NCT01991197 (16) [back to overview]The Effects of Treatment With Sitagliptin and Treatment With Gliclazide on Other Efficacy Endpoints.
NCT01991197 (16) [back to overview]The Change in Quality of Life Scores From Baseline to 16 Weeks in the Sitagliptin and Gliclazide Arms.
NCT01991197 (16) [back to overview]The Number of Patricipants in the Sitagliptin and Gliclazide Arms With Adverse Events at 32 Weeks.
NCT01991197 (16) [back to overview]The Effects of Treatment With Sitagliptin and Treatment With Gliclazide on the Serum Cytokine Tumour Necrosis Factor Alpha.
NCT01991197 (16) [back to overview]The Effects of Treatment With Sitagliptin and Treatment With Gliclazide on the Change in Serum Leptin From Baseline to 16 Weeks.
NCT01991197 (16) [back to overview]The Effects of Treatment With Sitagliptin and Treatment With Gliclazide From Baseline to 16 Weeks on Serum Levels Interleukin-23.
NCT01991197 (16) [back to overview]The Effects of Treatment With Sitagliptin and Treatment With Gliclazide From Baseline to 16 Weeks on Serum Levels Interleukin-17.
NCT01991197 (16) [back to overview]The Effect of Treatment With Sitagliptin and With Gliclazide From Baseline to 16 Weeks on the Change in Interleukin-17 Levels in the Skin (in a Sub-group of Participants Willing to Undergo Skin Biopsies).
NCT01991197 (16) [back to overview]The Change in Weight From Baseline to 16 Weeks in the Sitagliptin and Gliclazide Arms.
NCT01999218 (6) [back to overview]Percentage of Participants With an Adverse Event of Symptomatic Hypoglycemia Up to Week 52: Excluding Rescue Approach
NCT01999218 (6) [back to overview]Percentage of Participants Experiencing An Adverse Event (AE) Up to Week 106
NCT01999218 (6) [back to overview]Percentage of Participants Discontinuing Study Treatment Due to an AE Up to Week 104
NCT01999218 (6) [back to overview]Change From Baseline in Sitting Systolic Blood Pressure (SBP) at Week 52 Excluding Rescue Approach
NCT01999218 (6) [back to overview]Change From Baseline in Body Weight at Week 52 Excluding Rescue Approach
NCT01999218 (6) [back to overview]Change From Baseline in Hemoglobin A1C (A1C) at Week 52: Excluding Rescue Approach
NCT02008682 (6) [back to overview]Number of Confirmed Hypoglycaemic Episodes
NCT02008682 (6) [back to overview]Change From Baseline in Glycosylated Haemoglobin (HbA1c)
NCT02008682 (6) [back to overview]Change From Baseline in 7-point Self-measured Plasma Glucose Profile
NCT02008682 (6) [back to overview]Change From Baseline in Fasting Plasma Glucose
NCT02008682 (6) [back to overview]Subjects Who Achieve (Yes/no) HbA1c Below or Equal to 6.5 % (American Association of Clinical Endocrinologists Target)
NCT02008682 (6) [back to overview]Subjects Who Achieve (Yes/no) HbA1c Below 7.0 % (American Diabetes Association Target)
NCT02036515 (24) [back to overview]Baseline Homeostasis Model Assessment of β-cell Function (HOMA-%β) Value
NCT02036515 (24) [back to overview]Change From Baseline in Body Weight at Week 26
NCT02036515 (24) [back to overview]Time to Initiation of Glycemic Rescue by Week 52
NCT02036515 (24) [back to overview]Time to Initiation of Glycemic Rescue by Week 26
NCT02036515 (24) [back to overview]Change From Baseline in Sitting Systolic Blood Pressure at Week 52
NCT02036515 (24) [back to overview]Change From Baseline in Sitting Systolic Blood Pressure at Week 26
NCT02036515 (24) [back to overview]Change From Baseline in Sitting Diastolic Blood Pressure at Week 52
NCT02036515 (24) [back to overview]Change From Baseline in Sitting Diastolic Blood Pressure at Week 26
NCT02036515 (24) [back to overview]Percentage of Participants With an A1C <7% (53 mmol/Mol) at Week 52
NCT02036515 (24) [back to overview]Change From Baseline in Body Weight at Week 52
NCT02036515 (24) [back to overview]Baseline EQ-5D 3-level Version (EQ-5D-3L) Questionnaire Score
NCT02036515 (24) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 26
NCT02036515 (24) [back to overview]Change From Baseline in EQ-5D-3L Questionnaire Score at Week 26
NCT02036515 (24) [back to overview]Change From Baseline in EQ-5D-3L Score at Week 52
NCT02036515 (24) [back to overview]Percentage of Participants With an A1C <7% (53 mmol/Mol) at Week 26
NCT02036515 (24) [back to overview]Percentage of Participants Receiving Glycemic Rescue Medication by Week 52
NCT02036515 (24) [back to overview]Percentage of Participants Receiving Glycemic Rescue Medication by Week 26
NCT02036515 (24) [back to overview]Percentage of Participants Experiencing An Adverse Event (AE)
NCT02036515 (24) [back to overview]Percentage of Participants Discontinuing Study Treatment Due to an AE
NCT02036515 (24) [back to overview]Change From Baseline in HOMA-%β at Week 52
NCT02036515 (24) [back to overview]Change From Baseline in HOMA-%β at Week 26
NCT02036515 (24) [back to overview]Change From Baseline in Hemoglobin A1C at Week 52
NCT02036515 (24) [back to overview]Change From Baseline in Hemoglobin A1C at Week 26
NCT02036515 (24) [back to overview]Change From Baseline in FPG at Week 52
NCT02060383 (7) [back to overview]Absolute Change in FPG From Baseline to End of Core Phase
NCT02060383 (7) [back to overview]Change in HbA1c From Randomization to Approximately 16 Weeks
NCT02060383 (7) [back to overview]Change in HbA1c From Randomization (R) Over Time Per Randomized Arm
NCT02060383 (7) [back to overview]Change in FPG (Fasting Plasma Glucose) From Randomization Until End of Core Phase
NCT02060383 (7) [back to overview]Absolute Change in HbA1c From Baseline to End of Core Phase
NCT02060383 (7) [back to overview]Percentage of Participants With ≤ 0.3% HbA1c Increase to End of Core Phase
NCT02060383 (7) [back to overview]Percentage of Participants in the Incretin-based Arm Who Required Anti-diabetic Rescue Therapy With Insulin
NCT02072096 (6) [back to overview]Change From Baseline of Estimated Glomerular Filtration Rate (eGFR)
NCT02072096 (6) [back to overview]Change From Baseline in Body Mass Index (BMI)
NCT02072096 (6) [back to overview]Change From Baseline of Urinary Albumin to Creatinine Ratio
NCT02072096 (6) [back to overview]Percentage of Participants Achieving and Maintaining Individualized Glycated Hemoglobin A1c (HbA1c) Targets Without Clinically Significant Hypoglycemia
NCT02072096 (6) [back to overview]Number of Participants With Total Hypoglycemia and Other Categories of Hypoglycemia
NCT02072096 (6) [back to overview]Percentage of Participants Requiring Alternative Treatment Due to Glycemic Failure of First Line Injectable Therapy
NCT02099110 (8) [back to overview]Change From Baseline in Body Weight at Week 26: Excluding Rescue Approach
NCT02099110 (8) [back to overview]Change From Baseline in Sitting Systolic Blood Pressure at Week 26: Excluding Rescue Approach
NCT02099110 (8) [back to overview]Change From Baseline in Static Beta-Cell Sensitivity to Glucose Index at Week 26; Excluding Rescue Approach
NCT02099110 (8) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 26 - Excluding Rescue Approach
NCT02099110 (8) [back to overview]Percentage of Participants Who Experienced an Adverse Event (AE): Including Rescue Approach
NCT02099110 (8) [back to overview]Percentage of Participants Who Discontinued Study Treatment Due to an AE: Including Rescue Approach
NCT02099110 (8) [back to overview]Change From Baseline in A1C at Week 26: Excluding Rescue Approach
NCT02099110 (8) [back to overview]Percentage of Participants Achieving a Hemoglobin A1C of <7% (<53 mmol/Mol) (Raw Proportions): Excluding Rescue Approach
NCT02111096 (15) [back to overview]Rate of Hypoglycemic Events Adjusted Per 30 Days
NCT02111096 (15) [back to overview]Population Pharmacokinetics: Apparent Volume of Distribution of LY2409021
NCT02111096 (15) [back to overview]Population Pharmacokinetics: Apparent Clearance of LY2409021
NCT02111096 (15) [back to overview]Number of Participants With Hypoglycemic Events
NCT02111096 (15) [back to overview]Number of Participants With Hepatobiliary Adverse Events of Special Interest (AESI)
NCT02111096 (15) [back to overview]Change From Baseline to 6 Months in Pulse Rate
NCT02111096 (15) [back to overview]Change From Baseline to 6 Months in Fasting Blood Glucagon
NCT02111096 (15) [back to overview]Change From Baseline to 6 Months in Hemoglobin A1c (HbA1c)
NCT02111096 (15) [back to overview]Change From Baseline to 6 Months in Fasting Plasma Glucose
NCT02111096 (15) [back to overview]Change From Baseline to 6 Months in Hepatic Fat Fraction
NCT02111096 (15) [back to overview]Change From Baseline to 6 Months in Body Weight
NCT02111096 (15) [back to overview]Change From Baseline to 6 Months in Alanine Aminotransferase Levels
NCT02111096 (15) [back to overview]Change From Baseline to 6 Months in Fasting Lipids Levels
NCT02111096 (15) [back to overview]Change From Baseline to 6 Months in 7-Point Self-Monitoring of Blood Glucose (SMBG)
NCT02111096 (15) [back to overview]Change From Baseline to 6 Months in Blood Pressure
NCT02122380 (5) [back to overview]Visceral Adipose Tissue
NCT02122380 (5) [back to overview]Vascular Function (Endothelium-dependent Vasodilation)
NCT02122380 (5) [back to overview]Early Insulin Secretion During Oral Glucose Tolerance Test
NCT02122380 (5) [back to overview]Area Under the Curve (AUC) for Blood Glucoses During 75 Gram Oral Glucose Tolerance Test
NCT02122380 (5) [back to overview]Mean Overnight Growth Hormone Levels
NCT02130687 (12) [back to overview]Heart Rate
NCT02130687 (12) [back to overview]Norepinephrine (NE) Concentrations
NCT02130687 (12) [back to overview]Neuropeptide Y
NCT02130687 (12) [back to overview]Dipeptidyl Peptidase IV (DPP4) Activity
NCT02130687 (12) [back to overview]Heart Rate
NCT02130687 (12) [back to overview]Insulin
NCT02130687 (12) [back to overview]Mean Arterial Blood Pressure
NCT02130687 (12) [back to overview]Mean Arterial Blood Pressure
NCT02130687 (12) [back to overview]24hr Urinary Testing for Sodium
NCT02130687 (12) [back to overview]Low Frequency Variability of Blood Pressure Activity
NCT02130687 (12) [back to overview]Angiotensin Converting Enzyme (ACE) Activity
NCT02130687 (12) [back to overview]Glucose
NCT02202161 (27) [back to overview]Number of Events With the Rating on Quality of Stools as Rated Using the BSFS Across Days 1 to 14
NCT02202161 (27) [back to overview]Number of Participants With Abnormal Hematology With Potential Clinical Concern (PCI)
NCT02202161 (27) [back to overview]Number of Bowel Movements (Stool Frequency) as Rated Using the Bristol Stool Form Scale (BSFS) Across Days 1 to 14
NCT02202161 (27) [back to overview]Number of Participants With Fecal Occult Blood Monitoring for Symptomatic or Visible Gastrointestinal Bleeding or Asymptomatic Occult Bleeding
NCT02202161 (27) [back to overview]PK Parameters for Metformin Steady State PK Parameters When Co-dosed With GSK2330672, Sitagliptin or Placebo-maximum Observed Concentration (Cmax)
NCT02202161 (27) [back to overview]Summary of Urinalysis Data-mean Specific Gravity
NCT02202161 (27) [back to overview]Summary of Urinalysis Data-mean pH
NCT02202161 (27) [back to overview]Sitagliptin Steady State PK Parameters When Co-dosed With Metformin-Tmax Following the First and Second Sitagliptin Doses
NCT02202161 (27) [back to overview]Sitagliptin Steady State PK Parameters When Co-dosed With Metformin-Cmax Following the First and Second Sitagliptin Doses
NCT02202161 (27) [back to overview]Ratio to Baseline in Fasting Low-density Cholesterol (LDL) Cholesterol, High-density Cholesterol (HDL) Cholesterol, Total Cholesterol, Non-HDL Cholesterol and Triglycerides
NCT02202161 (27) [back to overview]Ratio to Baseline in Fasting Apolipoprotein B
NCT02202161 (27) [back to overview]Number of Participants With Incidence and Nature of Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT02202161 (27) [back to overview]Number of Participants With Gastrointestinal Tolerability Assessments as Rated Using the Gastrointestinal Symptom Rating Scale (GSRS; With Worsening Symptoms >=2 Levels)
NCT02202161 (27) [back to overview]Number of Participants With Abnormal Urinalysis Data
NCT02202161 (27) [back to overview]Number of Participants With Abnormal Electrocardiogram (ECG) Findings Any Time Post-Baseline
NCT02202161 (27) [back to overview]Number of Participants With Abnormal Clinical Chemistry With PCI
NCT02202161 (27) [back to overview]Number of Events With the Rating on Quality of Stools as Rated Using the BSFS Across Days 1 to 14
NCT02202161 (27) [back to overview]Number of Events With the Rating on Quality of Stools as Rated Using the BSFS Across Days 1 to 14
NCT02202161 (27) [back to overview]Number of Events With the Rating on Quality of Stools as Rated Using the BSFS Across Days 1 to 14
NCT02202161 (27) [back to overview]Number of Events With the Rating on Quality of Stools as Rated Using the BSFS Across Days 1 to 14
NCT02202161 (27) [back to overview]Change From Baseline in Vital Signs Assessments-temperature
NCT02202161 (27) [back to overview]Change From Baseline in Vital Signs Assessments-systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
NCT02202161 (27) [back to overview]Change From Baseline in Vital Signs Assessments-heart Rate
NCT02202161 (27) [back to overview]Change From Baseline in Derived Plasma Glucose Parameter Over a 24-hour Period-fasting and Weighted Mean Glucose Area Under Curve (AUC[0-24 Hour])
NCT02202161 (27) [back to overview]Sitagliptin Steady State PK Parameters When Co-dosed With Metformin-AUC(0-10)
NCT02202161 (27) [back to overview]PK Parameters for Metformin Steady State PK Parameters When Co-dosed With GSK2330672, Sitagliptin or Placebo-time of Occurrence of Cmax (Tmax)
NCT02202161 (27) [back to overview]PK Parameters for Metformin Steady State PK Parameters When Co-dosed With GSK2330672, Sitagliptin or Placebo-area Under the Concentration-time Curve Over the Dosing Interval of 10 Hours (AUC[0-10])
NCT02226003 (9) [back to overview]Change From Baseline in 2-hour Post-Meal Glucose (PMG) at Week 26 - Full Analysis Set Excluding Rescue Approach
NCT02226003 (9) [back to overview]Change From Baseline in Body Weight at Week 26 - Full Analysis Set Excluding Rescue Approach
NCT02226003 (9) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 26 - Full Analysis Set Excluding Rescue Approach
NCT02226003 (9) [back to overview]Change From Baseline in Hemoglobin A1C (HbA1C) at Week 26 - Full Analysis Set (FAS Population Excluding Rescue Approach
NCT02226003 (9) [back to overview]Percentage of Participants Who Discontinued Study Medication Due to an AE - All Participants as Treated Excluding Rescue Approach
NCT02226003 (9) [back to overview]Change From Baseline in Sitting Systolic Blood Pressure at Week 26 - Full Analysis Set Excluding Rescue Approach
NCT02226003 (9) [back to overview]Change From Baseline in Sitting Diastolic Blood Pressure at Week 26 - Full Analysis Set Excluding Rescue Approach
NCT02226003 (9) [back to overview]Percentage of Participants With HbA1C <7% (<53 mmol/Mol) at Week 26
NCT02226003 (9) [back to overview]Percentage of Participants Who Experienced an Adverse Event (AE) - All Participants as Treated Excluding Rescue Approach
NCT02254291 (3) [back to overview]Number of Treatment Emergent Adverse Events (TEAEs)
NCT02254291 (3) [back to overview]Number of Severe or Blood Glucose (BG) Confirmed Symptomatic Hypoglycaemic Episodes
NCT02254291 (3) [back to overview]Change in Glycosylated Haemoglobin A1c (HbA1c)
NCT02256189 (1) [back to overview]Glucagon Counterregulation to Hypoglycemia
NCT02284893 (4) [back to overview]Percent of Subjects Achieving a Therapeutic Glycemic Response, Defined as HbA1c < 7.0%
NCT02284893 (4) [back to overview]Mean Change in Total Body Weight
NCT02284893 (4) [back to overview]Mean Change in HbA1c
NCT02284893 (4) [back to overview]Mean Change in Fasting Plasma Glucose (FPG)
NCT02312063 (2) [back to overview]Correlation of Plasma Levels of EPA and DHA With HbA1c Reduction
NCT02312063 (2) [back to overview]Correlation of Estimated Seafood Intake With HbA1c Reduction
NCT02318693 (5) [back to overview]Change From Baseline in Percentage of Hypoglycemic Values (Glucose Sensor Readings: < 70, <60, <50 mg/dL)
NCT02318693 (5) [back to overview]Change From Baseline in Maximum Incremental Postprandial Glucose Levels in Each Meal
NCT02318693 (5) [back to overview]Change From Baseline in the Standard Deviation of Blood Glucose Levels
NCT02318693 (5) [back to overview]Change From Baseline in Mean Amplitude of Glycemic Excursions (MAGE) at Day 13
NCT02318693 (5) [back to overview]Change From Baseline in 24-hour Mean Glucose Level
NCT02328040 (2) [back to overview]Blood Glucose Measures in Subjects Treated With Sitagliptin, Compared to the Placebo
NCT02328040 (2) [back to overview]Measure of Glucagon Concentration in Subjects Treated With Sitagliptin, Compared to Placebo
NCT02406443 (7) [back to overview]Change in Glomerular Filtration Rate (GFR)
NCT02406443 (7) [back to overview]Change From Baseline in SDF-1alpha^1-67 (Intact) Measured by Immunoaffinity and Tandem Mass Spectrometry
NCT02406443 (7) [back to overview]Change From Baseline in SDF-1alpha^3-67 (Truncated) Measured by Tandem Mass Spectrometry With Antibody-based Affinity Enrichment
NCT02406443 (7) [back to overview]Change in Fractional Excretion of Lithium (FELi)
NCT02406443 (7) [back to overview]Change in Systolic Blood Pressure (SBP), Non-invasive Cardiac Output Monitoring
NCT02406443 (7) [back to overview]Percent Change in Fractional Excretion of Sodium (FENA)
NCT02406443 (7) [back to overview]Change in Effective Renal Plasma Flow (ERPF)
NCT02443402 (28) [back to overview]Number of Participants With Blood Glucose Less Than 40 mg/dl
NCT02443402 (28) [back to overview]Number of Participants Re-admitted to the Hospital Not Due to Wound Infections
NCT02443402 (28) [back to overview]Number of Participants Re-admitted to the Hospital Due to Wound Infections
NCT02443402 (28) [back to overview]Need for Continuous Intravenous Insulin (CII) for Treatment of Hyperglycemia
NCT02443402 (28) [back to overview]Mean Units Subcutaneous (SQ) Insulin Required
NCT02443402 (28) [back to overview]Mean Blood Glucose (BG) Concentration After Transition From Intensive Care Unit (ICU)
NCT02443402 (28) [back to overview]Total Insulin Therapy in the Intensive Care Unit (ICU)
NCT02443402 (28) [back to overview]Number of Subjects With Persistent Hyperglycemia
NCT02443402 (28) [back to overview]Number of Subjects Requiring the Use of Inotropes for Greater Than 24 Hours
NCT02443402 (28) [back to overview]Mean Daily Intensive Care Unit (ICU) Blood Glucose (BG) Concentration
NCT02443402 (28) [back to overview]Mean Amount of Insulin Therapy in the Intensive Care Unit (ICU)
NCT02443402 (28) [back to overview]Length of Stay: Intensive Care Unit (ICU)
NCT02443402 (28) [back to overview]Length of Hospital Stay After Study Randomization
NCT02443402 (28) [back to overview]Intensive Care Unit (ICU) Mortality Rate
NCT02443402 (28) [back to overview]Number of Subjects Requiring Re-intubation Within 24 Hours
NCT02443402 (28) [back to overview]Number of Subject Requiring Surgical Re-Intervention
NCT02443402 (28) [back to overview]Number of Participants With Stress Hyperglycemic Events in the Intensive Care Unit (ICU)
NCT02443402 (28) [back to overview]Number of Participants With Severe Hyperglycemic Events During Continuous Insulin Infusion (CII)
NCT02443402 (28) [back to overview]Number of Participants With Infections Not Requiring Hospital Re-admission
NCT02443402 (28) [back to overview]Number of Subjects Requiring Re-intubation
NCT02443402 (28) [back to overview]Number of Participants With Hypoglycemia During Intensive Care Unit (ICU) Stay
NCT02443402 (28) [back to overview]Number of Participants With Hypoglycemia After Transition From Intensive Care Unit (ICU)
NCT02443402 (28) [back to overview]Number of Participants With Hyperglycemia After Transition From Intensive Care Unit (ICU)
NCT02443402 (28) [back to overview]Duration of Continuous Intravenous Insulin (CII)
NCT02443402 (28) [back to overview]Hospital Complication Rate
NCT02443402 (28) [back to overview]Number of Participants With Emergency Room (ER) Visits
NCT02443402 (28) [back to overview]Hospital Mortality Rate
NCT02443402 (28) [back to overview]Number of Participants With Cerebrovascular Events
NCT02513771 (16) [back to overview]Change in %CD14+/CD16- (Classical Monocytes)
NCT02513771 (16) [back to overview]Change in %CD14dim/CD16++ (Non-classical Monocytes)
NCT02513771 (16) [back to overview]Change in CD4+ T-cell Activation
NCT02513771 (16) [back to overview]Change in sCD14 From Baseline to Week 15/16
NCT02513771 (16) [back to overview]Number of Participants With Grade ≥2 Adverse Events Related to Study Drug
NCT02513771 (16) [back to overview]Change in CD4+/CD8+ T-cell Ratio
NCT02513771 (16) [back to overview]Change in CD8+ T-cell Activation
NCT02513771 (16) [back to overview]Change in sCD14 From Week 15/16 to Week 20
NCT02513771 (16) [back to overview]Change in hsCRP
NCT02513771 (16) [back to overview]Change in IL-6
NCT02513771 (16) [back to overview]Change in IP-10
NCT02513771 (16) [back to overview]Change in sCD163
NCT02513771 (16) [back to overview]Change in sCD26
NCT02513771 (16) [back to overview]Change in sTNF-r1
NCT02513771 (16) [back to overview]Change in sTNF-r2
NCT02513771 (16) [back to overview]Change in %CD14+/CD16+ (Intermediate Monocytes)
NCT02532855 (10) [back to overview]Percentage of Participants Who Experienced One or More Adverse Events
NCT02532855 (10) [back to overview]Percentage of Participants With A1C <7% (53 mmol/Mol) at Week 24
NCT02532855 (10) [back to overview]Percentage of Participants Who Discontinued Study Drug Due to an AE
NCT02532855 (10) [back to overview]Change From Baseline in 2-hr Postprandial Glucose (PPG) at Week 24
NCT02532855 (10) [back to overview]Change From Baseline in A1C at Week 24
NCT02532855 (10) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24
NCT02532855 (10) [back to overview]Change From Baseline in Glucagon Area Under the Curve (AUC0-120 Minutes) at Week 24
NCT02532855 (10) [back to overview]Change From Baseline in Incremental 2-hour (2-hr) Postprandial Glucose Excursion (PPGE) at Week 24
NCT02532855 (10) [back to overview]Change From Baseline in Insulin AUC0-120 Minutes at Week 24
NCT02532855 (10) [back to overview]Change From Baseline in Postprandial Insulin AUC0-120 Minutes to Glucagon AUC0-120 Minutes Ratio at Week 24
NCT02536248 (1) [back to overview]Measurement of Serum Amyloid A Production Rate With Stable Isotope During Postprandial Period
NCT02556918 (26) [back to overview]Duration of Intubation
NCT02556918 (26) [back to overview]Length of Intensive Care Unit (ICU) Stay
NCT02556918 (26) [back to overview]Total IV Insulin in ICU
NCT02556918 (26) [back to overview]Mean Insulin Dose Per Day During Intensive Care Unit (ICU) Recovery
NCT02556918 (26) [back to overview]Mean Post-operative Blood Glucose (BG) Concentration
NCT02556918 (26) [back to overview]Median Number of Days of Subcutaneous (SC) Insulin After Discontinuation of Continuous Intravenous Insulin Infusion (CII)
NCT02556918 (26) [back to overview]Number of Cerebrovascular Events
NCT02556918 (26) [back to overview]Number of Intensive Care Unit (ICU) Readmission
NCT02556918 (26) [back to overview]Number of Patients Requiring Continuous Intravenous Insulin Infusion (CII)
NCT02556918 (26) [back to overview]Number of Patients Requiring Subcutaneous (SQ) Insulin After Discontinuation of Continuous Intravenous Insulin Infusion (CII)
NCT02556918 (26) [back to overview]Number of Subjects With Hyperglycemia (Blood Glucose Greater Than or Equal to 300 mg/dL) in Non-ICU
NCT02556918 (26) [back to overview]Total Length of Hospital Stay
NCT02556918 (26) [back to overview]Amount of Subcutaneous (SC) Insulin in Intensive Care Unit (ICU) 48 Hours
NCT02556918 (26) [back to overview]Mean Blood Glucose (BG) Concentration in the Intensive Care Unit (ICU)
NCT02556918 (26) [back to overview]Number of Patients With Hyperglycemia in the Intensive Care Unit (ICU)
NCT02556918 (26) [back to overview]Number of Patients With Hypoglycemic Events in Intensive Care Unit (ICU)
NCT02556918 (26) [back to overview]Number of Patients With Hypoglycemic Events in Non-intensive Care Unit (ICU)
NCT02556918 (26) [back to overview]Number of Patients With Persistent Hyperglycemia
NCT02556918 (26) [back to overview]Number of Patients With Severe Hypoglycemic Events in Intensive Care Unit (ICU)
NCT02556918 (26) [back to overview]Number of Patients With Severe Hypoglycemic Events in Non-intensive Care Unit (ICU)
NCT02556918 (26) [back to overview]Number of Subjects Readmitted to the Hospital
NCT02556918 (26) [back to overview]Number of Subjects Returning to the ER Within 30 Days
NCT02556918 (26) [back to overview]Amount of Subcutaneous (SC) Insulin Taken in Intensive Care Unit (ICU)
NCT02556918 (26) [back to overview]Composite of Perioperative Complications
NCT02556918 (26) [back to overview]Duration of Continuous Intravenous Insulin Infusion (CII)
NCT02556918 (26) [back to overview]Number of Subjects With Hyperglycemia in Intensive Care Unit (ICU)
NCT02564211 (3) [back to overview]Change From Baseline in HbA1c
NCT02564211 (3) [back to overview]Percentage of Participants Who Experienced at Least 1 Adverse Event (AE)
NCT02564211 (3) [back to overview]Percentage of Participants Who Had Study Drug Discontinued Due to an AE
NCT02577003 (7) [back to overview]Percentage of Participants Who Discontinued Study Drug Due to an AE
NCT02577003 (7) [back to overview]Change From Baseline in 2-hr PMG at Week 24
NCT02577003 (7) [back to overview]Change From Baseline in Body Weight at Week 24
NCT02577003 (7) [back to overview]Change From Baseline in Glucose Total AUC0-2hr After Meal at Week 24
NCT02577003 (7) [back to overview]Change From Baseline in HbA1c at Week 24
NCT02577003 (7) [back to overview]Percentage of Participants Who Experienced at Least One Adverse Event (AE)
NCT02577003 (7) [back to overview]Change From Baseline in FPG at Week 24
NCT02577016 (6) [back to overview]Percentage of Participants Who Experienced at Least One Adverse Event (AE)
NCT02577016 (6) [back to overview]Change From Baseline in 2-hr PMG at Week 24
NCT02577016 (6) [back to overview]Change From Baseline in FPG at Week 24
NCT02577016 (6) [back to overview]Change From Baseline in Glucose Total Area Under the Plasma Concentration Curve From Hour 0 to Hour 2 (AUC0-2hr) After Meal at Week 24
NCT02577016 (6) [back to overview]Change From Baseline in HbA1c at Week 24
NCT02577016 (6) [back to overview]Percentage of Participants Who Discontinued Study Drug Due to an AE
NCT02607865 (45) [back to overview]Time to Rescue Medication
NCT02607865 (45) [back to overview]Change in SMPG - Mean 7-point Profile
NCT02607865 (45) [back to overview]Change in FPG
NCT02607865 (45) [back to overview]Change in Free Fatty Acids (Ratio to Baseline)
NCT02607865 (45) [back to overview]Change in HbA1c: Week 26
NCT02607865 (45) [back to overview]Change in HbA1c: Weeks 52 and 78
NCT02607865 (45) [back to overview]Change in HDL Cholesterol (Ratio to Baseline)
NCT02607865 (45) [back to overview]Participants With Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes
NCT02607865 (45) [back to overview]Change in LDL Cholesterol (Ratio to Baseline)
NCT02607865 (45) [back to overview]Change in Lipase (Ratio to Baseline)
NCT02607865 (45) [back to overview]Change in Pulse Rate
NCT02607865 (45) [back to overview]Change in SBP and DBP
NCT02607865 (45) [back to overview]Change in SF-36v2 (Acute Version) Health Survey: Scores From the 8 Domains, the Physical Component Summary (PCS) and the Mental Component Summary (MCS)
NCT02607865 (45) [back to overview]Change in SMPG - Mean Postprandial Increment Over All Meals
NCT02607865 (45) [back to overview]Change in Total Cholesterol (Ratio to Baseline)
NCT02607865 (45) [back to overview]Change in IWQoL-Lite-CT: Total Score and Scores From the 4 Domains
NCT02607865 (45) [back to overview]Change in Triglycerides (Ratio to Baseline)
NCT02607865 (45) [back to overview]Participants Who Achieve HbA1c <7.0 % (53 mmol/Mol) Without Hypoglycaemia (Severe or BG Confirmed Symptomatic Hypoglycaemia) and no Weight Gain (Yes/no)
NCT02607865 (45) [back to overview]Change in Physical Examination
NCT02607865 (45) [back to overview]Number of TEAEs During Exposure to Trial Product
NCT02607865 (45) [back to overview]Number of Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes
NCT02607865 (45) [back to overview]Occurrence of Anti-semaglutide Binding Antibodies (Yes/no)
NCT02607865 (45) [back to overview]Occurrence of Anti-semaglutide Binding Antibodies Cross Reacting With Native GLP-1 (Yes/no)
NCT02607865 (45) [back to overview]Occurrence of Anti-semaglutide Neutralising Antibodies (Yes/no)
NCT02607865 (45) [back to overview]Occurrence of Anti-semaglutide Neutralising Antibodies Cross Reacting With Native GLP-1 (Yes/no)
NCT02607865 (45) [back to overview]Change in Eye Examination Category
NCT02607865 (45) [back to overview]Anti-semaglutide Binding Antibody Levels
NCT02607865 (45) [back to overview]Anti-semaglutide Binding Antibody Levels
NCT02607865 (45) [back to overview]Anti-semaglutide Binding Antibody Levels
NCT02607865 (45) [back to overview]Change in Amylase (Ratio to Baseline)
NCT02607865 (45) [back to overview]Change in BMI
NCT02607865 (45) [back to overview]Change in Body Weight (%)
NCT02607865 (45) [back to overview]Change in Body Weight (kg): Weeks 52 and 78
NCT02607865 (45) [back to overview]Change in Body Weight: Week 26
NCT02607865 (45) [back to overview]Change in CoEQ: Scores From the 4 Domains and the 19 Items
NCT02607865 (45) [back to overview]Participants Who Achieve Weight Loss ≥5% (Yes/no)
NCT02607865 (45) [back to overview]Participants Who Achieve Weight Loss ≥10% (Yes/no)
NCT02607865 (45) [back to overview]Participants Who Achieve HbA1c Reduction ≥1% (10.9 mmol/Mol) and Weight Loss ≥3% (Yes/no)
NCT02607865 (45) [back to overview]Participants Who Achieve HbA1c ≤6.5% (48 mmol/Mol) AACE Target (Yes/no)
NCT02607865 (45) [back to overview]Participants Who Achieve HbA1c <7.0% (53 mmol/Mol) ADA Target (Yes/no)
NCT02607865 (45) [back to overview]Time to Additional Anti-diabetic Medication
NCT02607865 (45) [back to overview]Semaglutide Plasma Concentration in a Subset of the Participants for Population PK Analyses
NCT02607865 (45) [back to overview]Change in VLDL Cholesterol (Ratio to Baseline)
NCT02607865 (45) [back to overview]Change in Waist Circumference
NCT02607865 (45) [back to overview]Change in ECG Evaluation
NCT02623998 (6) [back to overview]Percent Change in Weight
NCT02623998 (6) [back to overview]Number of Participants With Severe Hypoglycemic Episodes
NCT02623998 (6) [back to overview]Number of Participants Achieving Drug-free Diabetes Remission
NCT02623998 (6) [back to overview]Change in Waist Circumference
NCT02623998 (6) [back to overview]Number of Participants With Drug-free Normal Glucose Tolerance
NCT02623998 (6) [back to overview]Number of Participants With Hyperglycemia Relapse in the Experimental Group Compared to the Control Group
NCT02639637 (13) [back to overview]Arterial tPA
NCT02639637 (13) [back to overview]Mean Arterial Pressure
NCT02639637 (13) [back to overview]Low Frequency Variability of Blood Pressure Activity
NCT02639637 (13) [back to overview]Insulin
NCT02639637 (13) [back to overview]Heart Rate
NCT02639637 (13) [back to overview]Glucose
NCT02639637 (13) [back to overview]Forearm Blood Flow
NCT02639637 (13) [back to overview]DPP4 Activity
NCT02639637 (13) [back to overview]Venous Norepinephrine
NCT02639637 (13) [back to overview]Arterial Norepinephrine
NCT02639637 (13) [back to overview]ACE Activity
NCT02639637 (13) [back to overview]Venous tPA
NCT02639637 (13) [back to overview]NPY Metabolites
NCT02647320 (15) [back to overview]Change From Baseline in Non-HDL-C at Week 12
NCT02647320 (15) [back to overview]Change From Baseline in Area-Under-the Curve 0-3 Hours (AUC0-3h) of Plasma Glucose (PG) in Response to the Mixed Meal Tolerance Test (MMTT) at Week 4
NCT02647320 (15) [back to overview]Change From Baseline in Total Cholesterol (TC) at Week 12
NCT02647320 (15) [back to overview]Change From Baseline in Cmax of PG in Response to MMTT at Week 12
NCT02647320 (15) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 12
NCT02647320 (15) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 2
NCT02647320 (15) [back to overview]Change From Baseline in Triglycerides at Week 12
NCT02647320 (15) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 4
NCT02647320 (15) [back to overview]Change From Baseline in AUC0-3h of PG in Response to the MMTT at Week 12
NCT02647320 (15) [back to overview]Count of Participants With HbA1c Less Than 7.0% at Week 12
NCT02647320 (15) [back to overview]Change From Baseline in Glycated Hemoglobin (HbA1c) at Week 12
NCT02647320 (15) [back to overview]Change From Baseline in HDL-C at Week 12
NCT02647320 (15) [back to overview]Change From Baseline in LDL-C at Week 12
NCT02647320 (15) [back to overview]Change From Baseline in Maximum Concentration (Cmax) of PG in Response to MMTT at Week 4
NCT02647320 (15) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 8
NCT02683187 (1) [back to overview]Arginine-stimulated Insulin Secretion With and Without GLP-1 Blockade
NCT02683525 (11) [back to overview]Percentage of Patients With Grade III-IV Acute GvHD at Day +100
NCT02683525 (11) [back to overview]Percentage of Patients With Grade II-IV Acute GvHD by Day +100 Following Transplant
NCT02683525 (11) [back to overview]Number of Unique Patients With Infections by Day +100
NCT02683525 (11) [back to overview]Percentage of Patients With Relapse of the Primary Hematological Malignancy at 1 Year
NCT02683525 (11) [back to overview]Percentage of Patients With Grade II-IV Acute GvHD at Day +100
NCT02683525 (11) [back to overview]Percentage of Patients With Non-relapse Mortality (NRM) at +1 Year
NCT02683525 (11) [back to overview]Number of Patients With Treatment Related Adverse Events Grade 3 or Higher for Non-hematological Toxicity
NCT02683525 (11) [back to overview]Percentage of Patients Diagnosed With Chronic GvHD at 1 Year
NCT02683525 (11) [back to overview]Percentage of Patients Surviving at +1 Year
NCT02683525 (11) [back to overview]Median Time to Engraftment of Neutrophils
NCT02683525 (11) [back to overview]Median Time to Engraftment of Platelets
NCT02738879 (15) [back to overview]Event Rate of Documented Hypoglycemia With Blood Glucose ≤70 mg/dL (≤3.9 mmol/L)
NCT02738879 (15) [back to overview]Event Rate of Documented Symptomatic Hypoglycemia With Blood Glucose <56 mg/dL (≤3.1 mmol/L)
NCT02738879 (15) [back to overview]Event Rate of Documented Symptomatic Hypoglycemia With Blood Glucose ≤70 mg/dL (≤3.9 mmol/L)
NCT02738879 (15) [back to overview]Percentage of Participants Who Experienced One or More Adverse Events (AEs)
NCT02738879 (15) [back to overview]Percentage of Participants With A1C Goal <7.0% (<53 mmol/Mol) at Week 30
NCT02738879 (15) [back to overview]Percentage of Participants With Documented Hypoglycemia With Blood Glucose <56 mg/dL (≤3.1 mmol/L)
NCT02738879 (15) [back to overview]Percentage of Participants With Documented Hypoglycemia With Blood Glucose ≤70 mg/dL (≤3.9 mmol/L)
NCT02738879 (15) [back to overview]Percentage of Participants With Documented Symptomatic Hypoglycemia With Blood Glucose <56 mg/dL (≤3.1 mmol/L)
NCT02738879 (15) [back to overview]Percentage of Participants With Events of Documented Symptomatic Hypoglycemia With Blood Glucose ≤70 mg/dL (≤3.9 mmol/L)
NCT02738879 (15) [back to overview]Percentage of Participants With A1C Goal <7.0% (<53 mmol/Mol at Week 30 and No Documented Hypoglycemia With Blood Glucose ≤70 mg/dL (≤3.9 mmol/L) up to Week 30
NCT02738879 (15) [back to overview]Change From Baseline in A1C at Week 30
NCT02738879 (15) [back to overview]Percentage of Participants Who Discontinued Study Drug Due to an AE
NCT02738879 (15) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 30
NCT02738879 (15) [back to overview]Change From Baseline in Total Daily Insulin Dose (Units) at Week 30
NCT02738879 (15) [back to overview]Event Rate of Documented Hypoglycemia With Blood Glucose <56 mg/dL (≤3.1 mmol/L)
NCT02741687 (10) [back to overview]Total Daily Dose of Insulin for Patients Requiring Supplemental Insulin
NCT02741687 (10) [back to overview]Number of Participants Experiencing Complications
NCT02741687 (10) [back to overview]Number of Days in the ICU
NCT02741687 (10) [back to overview]Number of Participants Experiencing Stress Hyperglycemia
NCT02741687 (10) [back to overview]Number of Participants With Hospital Readmissions After Discharge
NCT02741687 (10) [back to overview]Number of Participants With Hypoglycemic Events
NCT02741687 (10) [back to overview]Number of Patients Requiring Supplemental, Subcutaneous Insulin
NCT02741687 (10) [back to overview]Number of Participants With Emergency Room Visits After Discharge
NCT02741687 (10) [back to overview]Length of Hospital Stay
NCT02741687 (10) [back to overview]Number of Patients Transferred to the ICU Immediately After Surgery or During Hospitalization
NCT02791490 (7) [back to overview]Percentage of Participants With Hemoglobin A1C ≥8.5% at Baseline That Attained A1C Goal of <7% at Week 20
NCT02791490 (7) [back to overview]Percentage of Participants With Hemoglobin A1C <7% at Week 20
NCT02791490 (7) [back to overview]Percentage of Participants Who Experienced at Least One Adverse Event (AE)
NCT02791490 (7) [back to overview]Percentage of Participants Receiving Glycemic Rescue Therapy
NCT02791490 (7) [back to overview]Change From Baseline in Hemoglobin A1C at Week 20
NCT02791490 (7) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 20
NCT02791490 (7) [back to overview]Percentage of Participants Who Discontinued Study Drug Due to an Adverse Event
NCT02849080 (60) [back to overview]Change in Body Weight (%)- Sustainability
NCT02849080 (60) [back to overview]Change in Body Weight (%)- Switch
NCT02849080 (60) [back to overview]Change in Body Weight (kg)- Sustainability
NCT02849080 (60) [back to overview]Change in Body Weight- Switch
NCT02849080 (60) [back to overview]Change in FPG
NCT02849080 (60) [back to overview]Change in FPG- Sustainability
NCT02849080 (60) [back to overview]Change in FPG- Switch
NCT02849080 (60) [back to overview]Change in Waist Circumference- Sustainability
NCT02849080 (60) [back to overview]Change in HbA1c
NCT02849080 (60) [back to overview]Change in HbA1c- Sustainability
NCT02849080 (60) [back to overview]Change in HbA1c- Switch
NCT02849080 (60) [back to overview]Change in LDL Cholesterol (Ratio to Baseline)
NCT02849080 (60) [back to overview]Change in Lipase (Ratio to Baseline)
NCT02849080 (60) [back to overview]Change in Lipase (Ratio to Baseline)- Sustainability
NCT02849080 (60) [back to overview]Change in Lipase (Ratio to Baseline)- Switch
NCT02849080 (60) [back to overview]Change in Pulse Rate
NCT02849080 (60) [back to overview]Change in HDL Cholesterol (Ratio to Baseline)
NCT02849080 (60) [back to overview]Time to Rescue Medication
NCT02849080 (60) [back to overview]Time to Additional Anti-diabetic Medication- Switch
NCT02849080 (60) [back to overview]Time to Additional Anti-diabetic Medication
NCT02849080 (60) [back to overview]Paticipants With Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes (Yes/no)- Switch
NCT02849080 (60) [back to overview]Paticipants With Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes (Yes/no)- Sustainability
NCT02849080 (60) [back to overview]Paticipants With Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes (Yes/no)
NCT02849080 (60) [back to overview]Participants Who Achieve HbA1c <7.0% (53 mmol/Mol) ADA Target and no Need for Rescue Medication (Yes/no)- Switch
NCT02849080 (60) [back to overview]Number of Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes)- Sustainability
NCT02849080 (60) [back to overview]Number of Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes- Switch
NCT02849080 (60) [back to overview]Number of Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes
NCT02849080 (60) [back to overview]Number of TEAEs During Exposure to Trial Product- Switch
NCT02849080 (60) [back to overview]Number of TEAEs During Exposure to Trial Product- Sustainability
NCT02849080 (60) [back to overview]Number of TEAEs During Exposure to Trial Product
NCT02849080 (60) [back to overview]Change in Waist Circumference- Switch
NCT02849080 (60) [back to overview]Change in Amylase (Ratio to Baseline)
NCT02849080 (60) [back to overview]Change in Waist Circumference
NCT02849080 (60) [back to overview]Change in Triglycerides (Ratio to Baseline)
NCT02849080 (60) [back to overview]Change in Total Cholesterol (Ratio to Baseline)
NCT02849080 (60) [back to overview]Change in Pulse Rate- Switch
NCT02849080 (60) [back to overview]Change in Pulse Rate- Sustainability
NCT02849080 (60) [back to overview]Time to Rescue Medication- Switch
NCT02849080 (60) [back to overview]Change in Amylase (Ratio to Baseline)- Sustainability
NCT02849080 (60) [back to overview]Change in Amylase (Ratio to Baseline)- Switch
NCT02849080 (60) [back to overview]Change in BMI
NCT02849080 (60) [back to overview]Change in BMI- Sustainability
NCT02849080 (60) [back to overview]Participants Who Achieve HbA1c <7.0% (53 mmol/Mol) ADA Target (Yes/no)
NCT02849080 (60) [back to overview]Participants Who Achieve Weight Loss ≥5% (Yes/no)
NCT02849080 (60) [back to overview]Change in BMI- Switch
NCT02849080 (60) [back to overview]Change in Body Weight (%)
NCT02849080 (60) [back to overview]Participants Who Achieve Weight Loss ≥10% (Yes/no)
NCT02849080 (60) [back to overview]Participants Who Achieve HbA1c Reduction ≥1% (10.9 mmol/Mol) and Weight Loss ≥3% (Yes/no)
NCT02849080 (60) [back to overview]Participants Who Achieve HbA1c ≤6.5% (48 mmol/Mol) AACE Target (Yes/no)
NCT02849080 (60) [back to overview]Participants Who Achieve HbA1c <7.0 % (53 mmol/Mol) Without Hypoglycaemia (Severe or BG Confirmed Symptomatic Hypoglycaemia) and no Weight Gain (Yes/no)
NCT02849080 (60) [back to overview]Change in SF-36v2 (Acute Version) Health Survey: Scores From the 8 Domains, the Physical Component Summary (PCS) and the Mental Component Summary (MCS)- Switch
NCT02849080 (60) [back to overview]Change in SF-36v2 (Acute Version) Health Survey: Scores From the 8 Domains, the Physical Component Summary (PCS) and the Mental Component Summary (MCS)- Sustainability
NCT02849080 (60) [back to overview]Change in SF-36v2 (Acute Version) Health Survey: Scores From the 8 Domains, the Physical Component Summary (PCS) and the Mental Component Summary (MCS)
NCT02849080 (60) [back to overview]Change in DTSQ- Switch
NCT02849080 (60) [back to overview]Change in DTSQ- Sustainability
NCT02849080 (60) [back to overview]Change in DTSQ
NCT02849080 (60) [back to overview]Change in Body Weight
NCT02849080 (60) [back to overview]Change in Blood Pressure (Systolic and Diastolic Blood Pressure)- Switch
NCT02849080 (60) [back to overview]Change in Blood Pressure (Systolic and Diastolic Blood Pressure)- Sustainability
NCT02849080 (60) [back to overview]Change in Blood Pressure (Systolic and Diastolic Blood Pressure)
NCT02917031 (6) [back to overview]Change From Baseline in Left Ventricular Ejection Fraction (LVEF) Measured by MRI at 24 Weeks.
NCT02917031 (6) [back to overview]Number of Participants With Adverse Events
NCT02917031 (6) [back to overview]Change From Baseline in NT-proBNP After 24 Weeks of Treatment
NCT02917031 (6) [back to overview]Change From Baseline in Left Ventricular Mass (LVM) Measured by MRI at 24 Weeks.
NCT02917031 (6) [back to overview]Change From Baseline in Left Ventricular End Systolic Volume (LVESV) Index, Measured by MRI at 24 Weeks.
NCT02917031 (6) [back to overview]Change From Baseline in Left Ventricular End Diastolic Volume (LVEDV) Index Measured by Magnetic Resonance Imaging (MRI) at 24 Weeks
NCT02920918 (2) [back to overview]Change From Baseline Aerobic Exercise Capacity at 12 Weeks
NCT02920918 (2) [back to overview]Change From Baseline Ventilatory Efficiency at 12 Weeks
NCT02956044 (30) [back to overview]Cmax (Maximum Observed Plasma Concentration)
NCT02956044 (30) [back to overview]Urinary Glucose Excretion up to 0-72 hr
NCT02956044 (30) [back to overview]Urinary Glucose Excretion up to 0-72 hr
NCT02956044 (30) [back to overview]Tmax (Time of Maximum Observed Plasma Concentration)
NCT02956044 (30) [back to overview]Tmax (Time of Maximum Observed Plasma Concentration)
NCT02956044 (30) [back to overview]Tmax (Time of Maximum Observed Plasma Concentration)
NCT02956044 (30) [back to overview]AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)
NCT02956044 (30) [back to overview]Cmax (Maximum Observed Plasma Concentration)
NCT02956044 (30) [back to overview]Cmax (Maximum Observed Plasma Concentration)
NCT02956044 (30) [back to overview]T1/2 (Apparent Terminal Elimination Half-life)
NCT02956044 (30) [back to overview]Cmax (Maximum Observed Plasma Concentration)
NCT02956044 (30) [back to overview]Cmax (Maximum Observed Plasma Concentration)
NCT02956044 (30) [back to overview]Tmax (Time of Maximum Observed Plasma Concentration)
NCT02956044 (30) [back to overview]Tmax (Time of Maximum Observed Plasma Concentration)
NCT02956044 (30) [back to overview]Tmax (Time of Maximum Observed Plasma Concentration)
NCT02956044 (30) [back to overview]Tmax (Time of Maximum Observed Plasma Concentration)
NCT02956044 (30) [back to overview]AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)
NCT02956044 (30) [back to overview]AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)
NCT02956044 (30) [back to overview]AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)
NCT02956044 (30) [back to overview]T1/2 (Apparent Terminal Elimination Half-life)
NCT02956044 (30) [back to overview]AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)
NCT02956044 (30) [back to overview]T1/2 (Apparent Terminal Elimination Half-life)
NCT02956044 (30) [back to overview]AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)
NCT02956044 (30) [back to overview]AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)
NCT02956044 (30) [back to overview]T1/2 (Apparent Terminal Elimination Half-life)
NCT02956044 (30) [back to overview]T1/2 (Apparent Terminal Elimination Half-life)
NCT02956044 (30) [back to overview]T1/2 (Apparent Terminal Elimination Half-life)
NCT02956044 (30) [back to overview]T1/2 (Apparent Terminal Elimination Half-life)
NCT02956044 (30) [back to overview]Cmax (Maximum Observed Plasma Concentration)
NCT02956044 (30) [back to overview]Cmax (Maximum Observed Plasma Concentration)
NCT03061214 (74) [back to overview]Change in Fasting Total Cholesterol - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Calcitonin - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Clinical Evaluation: Pulse
NCT03061214 (74) [back to overview]Change in Fasting Glucagon - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Fasting HDL Cholesterol - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Fasting HOMA-B (Beta-cell Function) - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Fasting HOMA-IR (Insulin Resistence) - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Fasting Insulin - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Fasting LDL Cholesterol - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Fasting Plasma Glucose (FPG)
NCT03061214 (74) [back to overview]Change in Fasting Proinsulin - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Fasting Proinsulin/Insulin Ratio - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Fasting Triglycerides - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Fasting VLDL Cholesterol - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Free Fatty Acids - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Haematological Parameter: Haematocrit - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Haematological Parameter: Haemoglobin - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Hematological Parameter (Differential Cell Count of Leukocytes): Basophils - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Hematological Parameter (Differential Cell Count of Leukocytes): Eosinophils - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Hematological Parameter (Differential Cell Count of Leukocytes): Lymphocytes - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Hematological Parameter (Differential Cell Count of Leukocytes): Monocytes - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Hematological Parameter (Differential Cell Count of Leukocytes): Neutrophils - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Hematological Parameter: Erythrocytes - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Hematological Parameter: Leukocytes - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Hematological Parameter: Thrombocytes - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in High-sensitivity CRP - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Self-measured Plasma Glucose (SMPG) - Mean 7-point Profile
NCT03061214 (74) [back to overview]Change in Self-measured Plasma Glucose (SMPG) - Mean Postprandial Increment Over All Meals
NCT03061214 (74) [back to overview]Change in Urinalysis Parameter - UACR-ratio to Baseline
NCT03061214 (74) [back to overview]Change in Waist Circumference
NCT03061214 (74) [back to overview]Number of Treatment Emergent Severe or Blood Glucose (BG) Confirmed Symptomatic Hypoglycaemic Episodes
NCT03061214 (74) [back to overview]Total Number of Treatment Emergent Adverse Events
NCT03061214 (74) [back to overview]Anti-semaglutide Antibody Levels
NCT03061214 (74) [back to overview]Change in Blood Pressure (Systolic and Diastolic Blood Pressure)
NCT03061214 (74) [back to overview]Change in HbA1c
NCT03061214 (74) [back to overview]Change in Patient Reported Outcome Questionnaire: DTSQs Score
NCT03061214 (74) [back to overview]Change in Patient Reported Outcome Questionnaire: SF-36v2™ Score
NCT03061214 (74) [back to overview]Occurence of Anti-semaglutide Antibodies Cross Reacting With Endogenous GLP-1 (Yes/no)
NCT03061214 (74) [back to overview]Occurence of Cross Reacting Antibodies With in Vitro Neutralising Effect to Endogenous GLP-1 (Yes/no)
NCT03061214 (74) [back to overview]Percentage of Participants That Achieved (Yes/no): Body Weight Loss ≥10%
NCT03061214 (74) [back to overview]Percentage of Participants That Achieved (Yes/no): Body Weight Loss ≥5%
NCT03061214 (74) [back to overview]Percentage of Participants That Achieved (Yes/no): HbA1c <7.0% (53 mmol/Mol) Without Severe or Blood Glucose (BG)-Confirmed Symptomatic Hypoglycaemia and no Weight Gain
NCT03061214 (74) [back to overview]Percentage of Participants Who Achieved HbA1c <7.0% (53 mmol/Mol), ADA Target, (Yes/no)
NCT03061214 (74) [back to overview]Percentage of Participants Who Achieved HbA1c ≤6.5% (48 mmol/Mol), AACE Target, (Yes/no)
NCT03061214 (74) [back to overview]Change in Clinical Evaluation: ECG
NCT03061214 (74) [back to overview]Change in Clinical Evaluation: Eye Examinations
NCT03061214 (74) [back to overview]Change in Physical Examination
NCT03061214 (74) [back to overview]Change in Urinalysis Parameter: Erythrocytes
NCT03061214 (74) [back to overview]Change in Urinalysis Parameter: Glucose
NCT03061214 (74) [back to overview]Change in Urinalysis Parameter: Ketones
NCT03061214 (74) [back to overview]Change in Urinalysis Parameter: pH
NCT03061214 (74) [back to overview]Change in Urinalysis Parameter: Protein
NCT03061214 (74) [back to overview]Occurence of Anti-semaglutide Antibodies (Yes/no)
NCT03061214 (74) [back to overview]Occurence of Anti-semaglutide Antibodies With In-vitro Neutralising Effect (Yes/no)
NCT03061214 (74) [back to overview]Change in Fasting C-peptide - Ratio to Baseline
NCT03061214 (74) [back to overview]Participants With Severe or Blood Glucose (BG) Confirmed Symptomatic Hypoglycaemic Episodes
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Alanine Aminotransferase - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Aspartate Aminotransferase - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Amylase - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Alkaline Phosphatase - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Albumin - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Calcium (Corrected)- Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Creatine Kinase - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Creatinine - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Estimated Glomerular Filtration Rate (eGFR) - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Lipase - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Potassium - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Sodium - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Total Bilirubin - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Total Calcium - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Total Protein- Ratio to Baseline
NCT03061214 (74) [back to overview]Change in Biochemistry Parameter: Urea - Ratio to Baseline
NCT03061214 (74) [back to overview]Change in BMI
NCT03061214 (74) [back to overview]Change in Body Weight
NCT03101930 (8) [back to overview]Fasting Insulin
NCT03101930 (8) [back to overview]Change in Plasminogen Activator Inhibitor-1
NCT03101930 (8) [back to overview]Change in Flow-mediated Dilation
NCT03101930 (8) [back to overview]Blood Pressure
NCT03101930 (8) [back to overview]Change in Weight
NCT03101930 (8) [back to overview]Heart Rate
NCT03101930 (8) [back to overview]Fasting Glucose
NCT03101930 (8) [back to overview]Urine Albumin-to-creatinine Ratio
NCT03108521 (5) [back to overview]Change in C-peptide
NCT03108521 (5) [back to overview]Glycosylated Hemoglobin A1c (HbA1c)
NCT03108521 (5) [back to overview]Change in Insulin
NCT03108521 (5) [back to overview]Types of Gene Polymorphism
NCT03108521 (5) [back to overview]Change in Blood Glucose
NCT03115112 (4) [back to overview]Change in SBP in Subjects From Baseline at Week 24
NCT03115112 (4) [back to overview]Change in HbA1c From Baseline to Week 24
NCT03115112 (4) [back to overview]Change in FPG From Baseline at Week 24
NCT03115112 (4) [back to overview]Change in Body Weight in Subjects With Baseline BMI ≥ 25 kg/m2 at Week 24
NCT03267576 (15) [back to overview]Percent Change From Baseline in Time During 24 Hours With Glucose 70 to 139 mg/dL
NCT03267576 (15) [back to overview]Change From Baseline in Time Spent With Glucose Level 70 to 139 mg/dL
NCT03267576 (15) [back to overview]Percent Change From Baseline in Time During 24 Hours With Glucose Level > 180 mg/dL
NCT03267576 (15) [back to overview]Change From Baseline in Time Spent With Glucose Level > 180 mg/dL
NCT03267576 (15) [back to overview]Change From Baseline in Time Spent With Glucose Level > 140 mg/dL
NCT03267576 (15) [back to overview]Change From Baseline in Time Spent With Glucose Level < 70 mg/dL
NCT03267576 (15) [back to overview]Percent Change From Baseline in Time During 24 Hours With Glucose Greater Than (>) 140 mg/dL
NCT03267576 (15) [back to overview]Change From Baseline in Mean 24-hour Glucose Profile
NCT03267576 (15) [back to overview]Change From Baseline in Glycemic Standard Deviation (SD) for 24-hour Glucose Profile
NCT03267576 (15) [back to overview]Change From Baseline in Fasting Plasma Glucose Levels
NCT03267576 (15) [back to overview]Change From Baseline in 2-hour Post-prandial Glucose (PPG) Levels
NCT03267576 (15) [back to overview]Change From Baseline in Glycemic Coefficient of Variation (CV) in Treatment Period 2
NCT03267576 (15) [back to overview]Change From Baseline in Glycemic Coefficient of Variation (CV) in Treatment Period 1
NCT03267576 (15) [back to overview]Change From Baseline in Percentage of 2 Consecutive Glucose Readings With < 70 mg/dL
NCT03267576 (15) [back to overview]Percent Change From Baseline in Time During 24 Hours With Glucose Level Less Than (<) 70 mg/dL
NCT03359590 (1) [back to overview]The Frequency of Hypoglycaemic Episodes With Sitagliptin vs Placebo Treatment.
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Fasting Lipid Profile: Low-density Lipoprotein (LDL) Cholesterol (Ratio to Baseline)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Fasting Lipid Profile: Total Cholesterol (Ratio to Baseline)
NCT04017832 (36) [back to overview]Time to Rescue Medication
NCT04017832 (36) [back to overview]Percentage Change From Baseline to Week 26 in Body Weight
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Electrocardiogram (ECG) Category
NCT04017832 (36) [back to overview]Number of Participants With Treatment-emergent Severe or Blood Glucose Confirmed Symptomatic Hypoglycaemic Episodes During Exposure to Trial Product
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Short Form-36 Version 2 (SF-36v2) (Acute Version) Health Survey
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Haematology Parameters: Basophils, Eosinophils, Lymphocytes, Monocytes, and Neutrophils
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Glycated Haemoglobin (HbA1c) (%)
NCT04017832 (36) [back to overview]Number of Treatment-emergent Adverse Events During Exposure to Trial Product
NCT04017832 (36) [back to overview]Physical Examination Category
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Waist Circumference
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Biochemistry Parameter: Calcium (Total) (Ratio to Baseline)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Biochemistry Parameter: Potassium (Ratio to Baseline)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Eye Examination Category
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Vital Signs: Pulse Rate
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Vital Signs: Diastolic Blood Pressure
NCT04017832 (36) [back to overview]Number of Treatment-emergent Severe or Blood Glucose Confirmed Symptomatic Hypoglycaemic Episodes During Exposure to Trial Product
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in 7 Point SMPG Profile: Mean Postprandial Increment (Over All Meals)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Biochemistry Parameter: Albumin (Ratio to Baseline)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Haematology Parameter: Thrombocytes (Ratio to Baseline)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Haematology Parameter: Leucocytes (Ratio to Baseline)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Haematology Parameter: Haemoglobin (Ratio to Baseline)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Haematology Parameter: Haematocrit (Ratio to Baseline)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Fasting Plasma Glucose (FPG)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Fasting Lipid Profile: Very-low-density Lipoprotein (VLDL) Cholesterol (Ratio to Baseline)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Fasting Lipid Profile: Triglycerides (Ratio to Baseline)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Self-measured Plasma Glucose (SMPG) Profile: Mean 7-point Profile
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Biochemistry Parameter: Urea (Ratio to Baseline)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Vital Signs: Systolic Blood Pressure
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Body Mass Index (BMI)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Body Weight (Kilogram [kg])
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Calcitonin (Ratio to Baseline)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Fasting Lipid Profile: Free Fatty Acids (Ratio to Baseline)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Fasting Lipid Profile: High-density Lipoprotein (HDL) Cholesterol (Ratio to Baseline)
NCT04017832 (36) [back to overview]Change From Baseline to Week 26 in Biochemistry Parameter: Sodium (Ratio to Baseline)

Change From Baseline in FPG (Fasting Plasma Glucose) at Week 24

Change from baseline at Week 24 is defined as Week 24 minus Week 0. (NCT00086502)
Timeframe: Baseline and week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-16.7
Placebo1.0

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Change From Baseline in HbA1c (Hemoglobin A1C) at Week 24

HbA1c is measured as a percent. Thus, this change from baseline reflects the Week 24 HbA1c percent minus the Week 0 HbA1c percent. (NCT00086502)
Timeframe: Baseline and week 24

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg-0.85
Placebo-0.15

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Change From Baseline in Hemoglobin A1C (A1C) at Week 24

"A1C is measured as a percent. Thus, this change from~baseline reflects the Week 24 A1C percent minus the Week 0 A1C percent." (NCT00086515)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg-0.67
Placebo / Glipizide 5 mg-0.02

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Change From Baseline in 2-hour Post-meal Glucose (PMG) at Week 24

Change from baseline at Week 24 is defined as PMG at Week 24 minus PMG at Week 0. (NCT00086515)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-62.0
Placebo / Glipizide 5 mg-11.4

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24

"Change from baseline at Week 24 is defined as FPG at~Week 24 minus FPG at Week 0." (NCT00086515)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-16.9
Placebo / Glipizide 5 mg8.5

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Change From Baseline in A1C at Week 24

A1C is measured as a percent. Thus, this change from baseline reflects the Week 24 A1C percent minus the Week 0 A1C percent. (NCT00087516)
Timeframe: Weeks 0-24

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg-0.61
Sitagliptin 200 mg-0.76
Placebo0.18

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Change From Baseline in A1C at Week 104

A1C is measured as a percent. Thus, this change from baseline reflects the Week 104 A1C percent minus the Week 0 A1C percent. (NCT00087516)
Timeframe: Weeks 0-104

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg/100 mg-0.27
Sitagliptin 200 mg/200 mg-0.40
Placebo/ Sitagliptin 100 mg-0.32
Placebo/Sitagliptin 200 mg-0.34

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Change From Baseline in FPG at Week 104

Change from baseline at Week 104 is defined as Week 104 FPG minus Week 0 FPG. (NCT00087516)
Timeframe: Weeks 0-104

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg/100 mg-1.8
Sitagliptin 200 mg/200 mg-5.7
Placebo/Sitagliptin 100 mg-4.1
Placebo/Sitagliptin 200 mg-4.1

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Change From Baseline in FPG at Week 24

Change from baseline at Week 24 is defined as Week 24 FPG minus Week 0 FPG. (NCT00087516)
Timeframe: Weeks 0-24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-12.4
Sitagliptin 200 mg-16.6
Placebo4.7

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Change From Baseline in 2-hour Post-meal Glucose (2-hr PMG) at Week 24

Change from baseline at Week 24 is defined as Week 24 2-hr PMG minus Week 0 2-hr PMG. (NCT00087516)
Timeframe: Weeks 0-24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-48.9
Sitagliptin 200 mg-56.3
Placebo-2.2

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Change From Baseline in 2-hr PMG at Week 104

Change from baseline at Week 104 is defined as Week 104 2-hr PMG minus Week 0 2-hr PMG. (NCT00087516)
Timeframe: Weeks 0-104

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg/100 mg-30.5
Sitagliptin 200 mg/200 mg-41.5
Placebo/Sitagliptin 100 mg-38.3
Placebo/Sitagliptin 200 mg-35.5

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Change From Baseline in FPG at Week 18

The change from baseline reflects the Week 18 Fasting Plasma Glucose (FPG) minus the Week 0 FPG. (NCT00094757)
Timeframe: Weeks 0-18

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-12.7
Sitagliptin 200 mg-9.9
Placebo/Pioglitazone7.0

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Change From Baseline in A1C at Week 18

Hemoglobin A1C (A1C) is measured as percent. Thus this change from baseline reflects the Week 18 A1C percent minus the Week 0 A1C percent. (NCT00094757)
Timeframe: Weeks 0-18

Interventionpercent (Least Squares Mean)
Sitagliptin 100 mg-0.48
Sitagliptin 200 mg-0.36
Placebo/Pioglitazone0.12

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Change From Baseline in A1C at Week 54

A1C is measured as percent. Thus this change from baseline reflects the Week 54 A1C percent minus the Week 0 A1C percent. (NCT00094757)
Timeframe: Weeks 0-54

Interventionpercent (Least Squares Mean)
Sitagliptin 100 mg-0.28
Sitagliptin 200 mg-0.19
Placebo/Pioglitazone-0.87

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Change From Baseline in FPG at Week 54

The change from baseline reflects the Week 54 FPG minus the Week 0 FPG. (NCT00094757)
Timeframe: Weeks 0-54

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-5.5
Sitagliptin 200 mg-0.7
Placebo/Pioglitazone-28.0

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Number of Participants With Laboratory Adverse Experiences (LAEs) at Week 104

A laboratory adverse experience (LAE) is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the SPONSOR'S product, whether or not considered related to the use of the product. (NCT00094770)
Timeframe: Baseline to Week 104

,
InterventionParticipants (Number)
With LAEsWithout LAEs
Glipizide74510
Sitagliptin 100 mg85503

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Number of Participants With Clinical Adverse Experiences (CAEs) at Week 104

An adverse experience (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR'S product, whether or not considered related to the use of the product. (NCT00094770)
Timeframe: Baseline to Week 104

,
InterventionParticipants (Number)
With CAESWithout CAES
Glipizide480104
Sitagliptin 100 mg452136

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Change From Baseline in HbA1c at Week 104

HbA1c is measured as percent. Thus, this change from baseline reflects the Week 104 HbA1c percent minus the Week 0 HbA1c percent. (NCT00094770)
Timeframe: Baseline and Week 104

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg-0.54
Glipizide-0.51

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Hypoglycemic Events at Week 104

Number of participants who reported 1 or more episodes of the adverse experience of hypoglycemia. (NCT00094770)
Timeframe: Baseline to Week 104

,
InterventionParticipants (Number)
Participants with one or more Hypoglycemic AEsTotal number of Hypoglycemic episodesParticipants with no Hypoglycemic AEs
Glipizide199805385
Sitagliptin 100 mg3157557

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Change From Baseline in HbA1c at Week 52

HbA1c is measured as percent. Thus, this change from baseline reflects the Week 52 HbA1c percent minus the Week 0 HbA1c percent. (NCT00094770)
Timeframe: Baseline and Week 52

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg-0.67
Glipizide-0.67

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Change From Baseline in Body Weight at Week 52

Change from baseline at Week 52 is defined as Week 52 minus Week 0. (NCT00094770)
Timeframe: Baseline and Week 52

InterventionKilograms (Least Squares Mean)
Sitagliptin 100 mg-1.5
Glipizide1.1

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Change From Baseline in Body Weight at Week 104

Change from baseline at Week 104 is defined as Week 104 minus Week 0. (NCT00094770)
Timeframe: Baseline and Week 104

InterventionKilograms (Least Squares Mean)
Sitagliptin 100 mg-1.6
Glipizide0.7

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Hypoglycemic Events at Week 52

Number of participants who reported 1 or more episodes of the adverse experience (AEs) of hypoglycemia. (NCT00094770)
Timeframe: Baseline to Week 52

,
InterventionParticipants (Number)
Participants with one or more Hypoglycemic AEsTotal number of Hypoglycemic episodesParticipants with no Hypoglycemic AEs
Glipizide187657397
Sitagliptin 100 mg2950559

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Number of Participants With Serious LAEs at Week 104

Serious LAEs are any LAEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose. (NCT00094770)
Timeframe: Baseline to Week 104

,
InterventionParticipants (Number)
With serious LAEsWithout serious LAEs
Glipizide0584
Sitagliptin 100 mg0588

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Number of Participants With Serious CAEs at Week 104

Serious CAEs are any AEs occurring at any dose that; Results in death; or Is life threatening; or Results in a persistent or significant disability/incapacity; or Results in or prolongs an existing inpatient hospitalization; or Is a congenital anomaly/birth defect; or Is a cancer; or Is an overdose. (NCT00094770)
Timeframe: Baseline to Week 104

,
InterventionParticipants (Number)
With serious CAEsWithout serious CAEs
Glipizide73511
Sitagliptin 100 mg64524

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Safety and Tolerability of Sitagliptin After 12 Weeks of Treatment

Safety and tolerability were measured in terms of the number of patients with clinical adverse experiences (CAEs), serious CAEs, drug-related CAEs, laboratory adverse experiences (LAEs), serious LAEs, and drug-related LAEs. Drug-relationship was assessed by the study investigator according to his/her best clinical judgment. (NCT00095056)
Timeframe: Week 0 through Week 12

,
InterventionParticipants (Number)
With CAEsWith drug-related CAEsWith serious CAEsWith LAEsWith drug-related LAEsWith serious LAEs
Placebo1611500
Sitagliptin4189910

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Safety and Tolerability of Sitagliptin Over 54 Weeks

Safety and tolerability were measured in terms of the number of patients with clinical adverse experiences (CAEs), serious CAEs, drug-related CAEs, laboratory adverse experiences (LAEs), serious LAEs, and drug-related LAEs. Drug-relationship was assessed by the study investigator according to his/her best clinical judgment. (NCT00095056)
Timeframe: Week 0 through Week 54

,
InterventionParticipants (Number)
With CAEsWith drug-related CAEsWith serious CAEsWith LAEsWith drug-related LAEsWith serious LAEs
Placebo22510800
Sitagliptin508201520

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Change From Baseline in HbA1c (Hemoglobin A1C) at Week 24

HbA1c is measured as a percent. This change from baseline reflects the Week 24 HbA1c percent minus the Week 0 HbA1c percent. (NCT00103857)
Timeframe: Week 24

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg q.d.-0.66
Metformin 500 mg b.i.d.-0.82
Metformin 1000 mg b.i.d.-1.13
Sitagliptin 50 mg b.i.d. + Metformin 500 mg b.i.d.-1.40
Sitagliptin 50 mg b.i.d + Metformin 1000 mg b.i.d.-1.90
Placebo/Metformin 1000 mg b.i.d.0.17

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Change From Baseline in FPG (Fasting Plasma Glucose) at Week 24

Change from baseline at Week 24 is defined as Week 24 minus Week 0. (NCT00103857)
Timeframe: Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg q.d.-17.5
Metformin 500 mg b.i.d.-27.3
Metformin 1000 mg b.i.d.-29.3
Sitagliptin 50 mg b.i.d. + Metformin 500 mg b.i.d.-47.1
Sitagliptin 50 mg b.i.d + Metformin 1000 mg b.i.d.-63.9
Placebo/Metformin 1000 mg b.i.d.5.8

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Change From Baseline in 2-Hour PMG (Post-Meal Glucose) at Week 24

Change from baseline at Week 24 is defined as Week 24 minus Week 0. (NCT00103857)
Timeframe: Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg q.d.-51.9
Metformin 500 mg b.i.d.-53.4
Metformin 1000 mg b.i.d.-78.0
Sitagliptin 50 mg b.i.d. + Metformin 500 mg b.i.d.-92.5
Sitagliptin 50 mg b.i.d + Metformin 1000 mg b.i.d.-116.6
Placebo/Metformin 1000 mg b.i.d.0.3

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Change From Baseline in 2-Hour PMG (Post-Meal Glucose) at Week 104

Change from baseline at Week 104 is defined as Week 104 minus Week 0. (NCT00103857)
Timeframe: Week 104

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg q.d.-74.1
Metformin 500 mg b.i.d.-72.7
Metformin 1000 mg b.i.d.-86.7
Sitagliptin 50 mg b.i.d. + Metformin 500 mg b.i.d.-96.2
Sitagliptin 50 mg b.i.d + Metformin 1000 mg b.i.d.-110.0
Placebo/Metformin 1000 mg b.i.d.-93.3

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Change From Baseline in 2-Hour PMG (Post-Meal Glucose) at Week 54

Change from baseline at Week 54 is defined as Week 54 minus Week 0. (NCT00103857)
Timeframe: Week 54

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg q.d.-45.9
Metformin 500 mg b.i.d.-58.6
Metformin 1000 mg b.i.d.-76.3
Sitagliptin 50 mg b.i.d. + Metformin 500 mg b.i.d.-89.6
Sitagliptin 50 mg b.i.d + Metformin 1000 mg b.i.d.-107.9
Placebo/Metformin 1000 mg b.i.d.-80.9

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Change From Baseline in FPG (Fasting Plasma Glucose) at Week 104

Change from baseline at Week 104 is defined as Week 104 minus Week 0. (NCT00103857)
Timeframe: Week 104

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg q.d.-26.8
Metformin 500 mg b.i.d.-41.4
Metformin 1000 mg b.i.d.-43.2
Sitagliptin 50 mg b.i.d. + Metformin 500 mg b.i.d.-47.5
Sitagliptin 50 mg b.i.d + Metformin 1000 mg b.i.d.-57.3
Placebo/Metformin 1000 mg b.i.d.-45.2

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Change From Baseline in HbA1c (Hemoglobin A1C) at Week 104

HbA1c is measured as a percent. This change from baseline reflects the Week 104 HbA1c percent minus the Week 0 HbA1c percent. (NCT00103857)
Timeframe: Week 104

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg q.d.-1.15
Metformin 500 mg b.i.d.-1.06
Metformin 1000 mg b.i.d.-1.34
Sitagliptin 50 mg b.i.d. + Metformin 500 mg b.i.d.-1.39
Sitagliptin 50 mg b.i.d + Metformin 1000 mg b.i.d.-1.66
Placebo/Metformin 1000 mg b.i.d.-1.39

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Change From Baseline in FPG (Fasting Plasma Glucose) at Week 54

Change from baseline at Week 54 is defined as Week 54 minus Week 0. (NCT00103857)
Timeframe: Week 54

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg q.d.-16.0
Metformin 500 mg b.i.d.-29.0
Metformin 1000 mg b.i.d.-39.6
Sitagliptin 50 mg b.i.d. + Metformin 500 mg b.i.d.-42.5
Sitagliptin 50 mg b.i.d + Metformin 1000 mg b.i.d.-55.6
Placebo/Metformin 1000 mg b.i.d.-43.9

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Change From Baseline in HbA1c (Hemoglobin A1C) at Week 54

HbA1c is measured as a percent. This change from baseline reflects the Week 54 HbA1c percent minus the Week 0 HbA1c percent. (NCT00103857)
Timeframe: Week 54

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg q.d.-0.82
Metformin 500 mg b.i.d.-1.01
Metformin 1000 mg b.i.d.-1.34
Sitagliptin 50 mg b.i.d. + Metformin 500 mg b.i.d.-1.41
Sitagliptin 50 mg b.i.d + Metformin 1000 mg b.i.d.-1.80
Placebo/Metformin 1000 mg b.i.d.-1.10

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Change From Baseline in A1C at Week 24

Hemoglobin A1C (A1C) is measured as percent. Thus this change from baseline reflects the Week 24 A1C percent minus the Week 0 A1C percent. (NCT00106704)
Timeframe: Baseline and 24 Weeks

InterventionPercent (Least Squares Mean)
Sitagliptin-0.45
Placebo/ Pioglitazone0.28

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Change From Baseline in FPG at Week 24

The change from baseline is the Week 24 Fasting Plasma Glucose (FPG) minus the Week 0 FPG. (NCT00106704)
Timeframe: Baseline and 24 Weeks

Interventionmg/dL (Least Squares Mean)
Sitagliptin-4.4
Placebo/ Pioglitazone15.7

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Change From Baseline in Fasting Plasma Glucose at Week 12

Change from baseline at Week 12 is defined as Week 12 minus Week 0. (NCT00127192)
Timeframe: Baseline and Week 12

Interventionmg/dL (Least Squares Mean)
Sitagliptin 25 mg QD-9.6
Sitagliptin 50 mg QD-11.4
Sitagliptin 100 mg QD-14.6
Sitagliptin 200 mg QD-16.9
Placebo6.3

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Change From Baseline in Glycosylated Albumin at Week 12

Change from baseline at Week 12 is defined as Week 12 minus Week 0. (NCT00127192)
Timeframe: Baseline and Week 12

InterventionPercent (Least Squares Mean)
Sitagliptin 25 mg QD-1.9
Sitagliptin 50 mg QD-2.6
Sitagliptin 100 mg QD-2.6
Sitagliptin 200 mg QD-2.9
Placebo0.7

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Change From Baseline in HbA1c at Week 12

HbA1c is measured as a percent. Thus, this change from baseline reflects the Week 12 HbA1c percent minus the Week 0 HbA1c percent. (NCT00127192)
Timeframe: Baseline and Week 12

InterventionPercent (Least Squares Mean)
Sitagliptin 25 mg QD-0.41
Sitagliptin 50 mg QD-0.71
Sitagliptin 100 mg QD-0.69
Sitagliptin 200 mg QD-0.76
Placebo0.28

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Change From Baseline in 2-hr Post-Meal Glucose (PMG) at Week 18

Change from baseline at Week 18 is defined as Week 18 minus Week 0. (NCT00289848)
Timeframe: Baseline and Week 18

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-63.8
Placebo-7.2

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Change From Baseline in Hemoglobin A1c (HbA1c) at Week 18

A1C was measured as a percent. Thus, this change from baseline reflects the Week 18 A1C percent minus the Week 0 A1C percent. (NCT00289848)
Timeframe: Baseline and Week 18

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg-0.71
Placebo0.31

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 18

Change from baseline at Week 18 is defined as Week 18 FPG minus Week 0 FPG. (NCT00289848)
Timeframe: Baseline and Week 18

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-25.8
Placebo5.2

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Rapidity of Onset of Action as Determined by Home Glucose Monitoring After 1 Week

Fingerstick glucose measurements were taken at 4 times (pre- and 2 hours post-breakfast and dinner) at each of Days -2, 3, and 7. The average of the 4 values was computed for each day. This outcome reflects the Day 7 average minus the Day -2 average. (NCT00305604)
Timeframe: Week 1

Interventionmg/dL (Least Squares Mean)
Sitagliptin-25.7
Placebo-2.1

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Change From Baseline in HbA1c (Hemoglobin A1c) at Week 24

Change from baseline at Week 24 is defined as Week 24 minus Week 0. (NCT00305604)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Sitagliptin-0.47
Placebo0.23

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Change From Baseline in FPG (Fasting Plasma Glucose) at Week 24

Change from baseline at Week 24 is defined as Week 24 minus Week 0. (NCT00305604)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-16.2
Placebo10.6

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Change From Baseline in 2-hour PPG (Post-prandial Glucose) at Week 24

Change from baseline at Week 24 is defined as Week 24 minus Week 0. (NCT00305604)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-52.1
Placebo8.9

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Change From Baseline in 2 Hr-PMG at Week 18

Change from baseline at Week 18 is defined as Week 18 minus Week 0. (NCT00337610)
Timeframe: Baseline and Week 18

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-67.6
Placebo-13.5

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Change From Baseline in FPG at Week 18

Change from baseline at Week 18 is defined as Week 18 FPG minus Week 0 FPG. (NCT00337610)
Timeframe: Baseline and Week 18

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-32.0
Placebo-6.5

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Change From Baseline in A1C at Week 30

A1C was measured as a percent. Thus, this change from baseline reflects the Week 30 A1C percent minus the Week 0 A1C percent. (NCT00337610)
Timeframe: Baseline and Week 30

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg-0.98
Placebo0.04

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Change From Baseline in A1C at Week 18

A1C was measured as a percent. Thus, this change from baseline reflects the Week 18 A1C percent minus the Week 0 A1C percent. (NCT00337610)
Timeframe: Baseline and Week 18

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg-1.00
Placebo0.02

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Change From Baseline in 2-hour PMG (Post-meal Glucose) at Week 18

Change from baseline at Week 18 is defined as Week 18 minus Week 0 (NCT00350779)
Timeframe: Baseline and Week 18

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-59.9
Placebo-22.0

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Change From Baseline in 2-hour PMG (Post-meal Glucose) at Week 54

Change from baseline at Week 54 is defined as Week 54 minus Week 0. (NCT00350779)
Timeframe: Baseline and Week 54

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-50.7
Placebo-16.6

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Change From Baseline in FPG (Fasting Plasma Glucose) at Week 18

Change from baseline at Week 18 is defined as Week 18 minus Week 0 (NCT00350779)
Timeframe: Baseline and 18 Weeks

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-30.7
Placebo-11.7

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Change From Baseline in FPG (Fasting Plasma Glucose) at Week 54

Change from baseline at Week 54 is defined as Week 54 minus Week 0 (NCT00350779)
Timeframe: Baseline and Week 54

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-28.0
Placebo-10.7

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Change From Baseline in HbA1c (Hemoglobin A1C) at Week 54

HbA1c is measured as a percent. Thus, this change from baseline reflects the Week 54 HbA1c percent minus the Week 0 HbA1c percent. (NCT00350779)
Timeframe: Baseline and Week 54

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg-1.05
Placebo-0.28

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Change From Baseline in HbA1c (Hemoglobin A1C) at Week 18

HbA1c is measured as a percent. Thus, this change from baseline reflects the Week 18 HbA1c percent minus the Week 0 HbA1c percent. (NCT00350779)
Timeframe: Baseline and 18 Weeks

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg-1.03
Placebo-0.31

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Lowering of Fasting Glucose

fasting glucose taken as the mean of blood glucose measured at -30, -20, -10 and 0 minutes prior to each inpatient meal study (NCT00364377)
Timeframe: 8 weeks

Interventionmmol/l (Mean)
Sitagliptin5.78
Placebo5.83

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Change From Baseline in 2 Hour Postprandial Glucose at Week 12

Change from baseline measurement, where the baseline measurement was obtained at randomization (0 week) before receiving study medication. (NCT00372060)
Timeframe: 12 weeks

Interventionmg/dL (Least Squares Mean)
Sitagliptin / Sitagliptin-42.7
Placebo / Sitagliptin6.4

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Change From Baseline in Fasting Plasma Glucose at Week 12

Change from baseline measurement, where the baseline measurement was obtained at randomization (0 week) before receiving study medication. (NCT00372060)
Timeframe: 12 Weeks

Interventionmg/dL (Least Squares Mean)
Sitagliptin / Sitagliptin-12.2
Placebo / Sitagliptin4.4

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Change From Baseline in Hemoglobin A1c (HbA1c ) at Week 12

Change from the baseline measurement, where the baseline measurement was obtained at randomization (0 week) before receiving study medication. (NCT00372060)
Timeframe: 12 Weeks

InterventionPercent (Least Squares Mean)
Sitagliptin / Sitagliptin-0.4
Placebo / Sitagliptin0.4

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Change From Baseline in Hemoglobin A1c (HbA1c ) at Week 52

Change from the last value before receiving sitagliptin therapy: Week 0 for Sitagliptin/Sitagliptin group and Week 12 for the Placebo/Sitagliptin group. (NCT00372060)
Timeframe: Week 52 (reflecting change from Week 0) for Sitagliptin/Sitagliptin group; Weeks 52 (reflecting change from Week 12) for Placebo/Sitagliptin group.

InterventionPercent (Mean)
Sitagliptin / Sitagliptin-0.6
Placebo / Sitagliptin-0.9

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Percent of Patients With A1C < 7.0% at Week 24

(NCT00395343)
Timeframe: 24 Weeks

InterventionPercent (Number)
Sitagliptin 100 mg q.d.12.8
Placebo5.1

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Percent of Patients With A1C < 6.5% at Week 24

(NCT00395343)
Timeframe: Week 24

InterventionPercent (Number)
Sitagliptin 100 mg q.d.2.3
Placebo1.9

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Change From Baseline in A1C at Week 24

"A1C in subset of patients on long-acting or intermediate-acting insulin.~A1C is measured as a percent. Thus, this change from baseline reflects the Week 24 A1C percent minus the Week 0 A1C percent." (NCT00395343)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg q.d.-0.61
Placebo-0.04

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Change From Baseline in A1C at Week 24

A1C is measured as a percent. Thus, this change from baseline reflects the Week 24 A1C percent minus the Week 0 A1C percent. (NCT00395343)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg q.d.-0.59
Placebo-0.03

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24

Change from baseline at Week 24 is defined as Week 24 minus Week 0. (NCT00395343)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg q.d.-18.5
Placebo-3.5

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Change From Baseline in 2-hour Post-meal Glucose (PMG) at Week 24

Change from baseline at Week 24 is defined as Week 24 minus Week 0. (NCT00395343)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg q.d.-30.9
Placebo5.2

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Percent Change From Baseline in Index of Static Beta-Cell Sensitivity to Glucose at Week 24

Static sensitivity is a measure of the effect of glucose on beta-cell secretion and is the ratio between the insulin secretion rate and glucose concentration above the threshold level at steady state. (See Breda and Cobelli, Annals of Biomedical Engineering 29, 692-700 (2001) for more details.) (NCT00395343)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg q.d.28.4
Placebo-8.1

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Change From Baseline in HbA1c (Hemoglobin A1C) at Week 24

HbA1c is measured as a percent. Thus, this change from baseline reflects the Week 24 HbA1c percent minus the Week 0 HbA1c percent. (NCT00397631)
Timeframe: Baseline and 24 weeks

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg q.d. + Pioglitazone 30 mg q.d.-2.38
Pioglitazone 30 mg q.d.-1.49

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Change From Baseline in FPG (Fasting Plasma Glucose) at Week 24

Change from baseline at Week 24 is defined as Week 24 minus Week 0. (NCT00397631)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg q.d. + Pioglitazone 30 mg q.d.-63.0
Pioglitazone 30 mg q.d.-40.2

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Change From Baseline in 2-hour PPG (Post-prandial Glucose) at Week 24

Change from baseline at Week 24 is defined as Week 24 minus Week 0. (NCT00397631)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg q.d. + Pioglitazone 30 mg q.d.-113.6
Pioglitazone 30 mg q.d.-68.9

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Restoration of the Insulinotropic Effect of GIP

Restoration of the insulinotropic effect of GIP measured as the relative increase in GIP induced amplification of the late phase insulin secretion (AUC) response to glucose. Patients will be followed for 12 weeks with examinations after 1 and after 12 weeks of treatment. (NCT00411411)
Timeframe: 12 weeks

,
InterventionpM x 120 min (Mean)
After 1 weekAfter 12 weeks
Januvia21.330.0
Placebo17.819.7

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the Relative Increase in Meal-induced Total GLP-1 Secretion

Patients will be followed for 12 weeks with three meal test examinations; before treatment, after 1 week of treatment and after 12 weeks of treatment. Primary outcome is AUC GLP-1 (pM x 120 as stated). (NCT00411411)
Timeframe: 12 weeks

InterventionpM x 120 min (Mean)
Placebo2591
Januvia3959

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Change From Baseline in Fasting Plasma Glucose at Week 12

Change from baseline at Week 12 is defined as fasting plasma glucose at Week 12 minus fasting plasma glucose at Week 0. (NCT00411554)
Timeframe: Baseline and Week 12

Interventionmg/dL (Least Squares Mean)
Sitagliptin 50 mg QD-19.6
Voglibose 0.2 mg TID-8.9

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Change From Baseline in 2 Hour Postprandial Glucose at Week 12

Change from baseline at Week 12 is defined as 2-hour postprandial glucose Week 12 minus 2-hour postprandial glucose Week 0. (NCT00411554)
Timeframe: Baseline and Week 12

Interventionmg/dL (Least Squares Mean)
Sitagliptin 50 mg QD-51.0
Voglibose 0.2 mg TID-32.2

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Change From Baseline in HbA1c at Week 12

HbA1c is measured as a percent. Thus, this change from baseline reflects the Week 12 HbA1c percent minus the Week 0 HbA1c percent. (NCT00411554)
Timeframe: Baseline and Week 12

InterventionPercent (Least Squares Mean)
Sitagliptin 50 mg QD-0.70
Voglibose 0.2 mg TID-0.30

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Fasting Blood Glucose at 48 Weeks

(NCT00420511)
Timeframe: 48 weeks

Interventionmmol/l (Median)
Sitagliptin6.9
Placebo6.7

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Insulinogenic Index Divided by HOMA-IR at 48 Weeks

Insulinogenic index was calculated as the incremental change in insulin from 0 to 30 minutes divided by the incremental change in glucose over the same period of time. Insulinogenic index divided by HOMA-IR provides an additional measure of beta-cell function. A higher value indicates better beta-cell function (NCT00420511)
Timeframe: 48 weeks

Interventionindex of beta-cell function (Median)
Sitagliptin3.9
Placebo1.8

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Preservation of Beta-cell Function Measured by Area-under-the-curve (C-peptide/Glucose)/HOMA-IR

Area-under-the-C-peptide-curve (AUCCpep) and area-under-the-glucose-curve (AUCgluc) from 0 to 240 minutes during meal tests were calculated using the trapezoidal rule. Insulin resistance was assessed using the Homeostasis Model Assessment of Insulin Resistance (HOMA-IR). Beta-cell function was assessed using the ratio of total AUCCpep to AUCgluc divided by HOMA-IR (AUCCpep/gluc/HOMA-IR), a measure of insulin secretion in the context of ambient insulin sensitivity, analogous to the disposition index and adaptation index. Higher AUCCpep/gluc/HOMA-IR is indicative of better beta-cell function. (NCT00420511)
Timeframe: 48 weeks

Interventionindex of beta-cell function (Median)
Sitagliptin80.4
Placebo71.2

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Number of Patients Who Reported 1 or More Episodes of the Adverse Experience of Diarrhea

(NCT00449930)
Timeframe: Baseline to Week 24

,
InterventionParticipants (Number)
Patients Who Reported DiarrheaPatients Who Did Not Report Diarrhea
Metformin57465
Sitagliptin 100 mg19509

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Number of Patients Who Reported 1 or More Episodes of the Adverse Experience of Nausea

(NCT00449930)
Timeframe: Baseline to Week 24

,
InterventionParticipants (Number)
Patients Who Reported NauseaPatients Who Did Not Report Nausea
Metformin16506
Sitagliptin 100 mg6522

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Number of Patients Who Reported 1 or More Episodes of the Adverse Experience of Vomiting

(NCT00449930)
Timeframe: Baseline to Week 24

,
InterventionParticipants (Number)
Patients Who Reported VomitingPatients Who Did Not Report Vomiting
Metformin7515
Sitagliptin 100 mg2526

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Number of Patients Who Reported 1 or More Episodes of the Adverse Experience of Abdominal Pain

(NCT00449930)
Timeframe: Baseline to Week 24

,
InterventionParticipants (Number)
Patients Who Reported Abdominal PainPatients Who Did Not Report Abdominal Pain
Metformin20502
Sitagliptin 100 mg11517

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Change From Baseline in Hemoglobin A1c (HbA1c) at Week 24

HbA1c is measured as a percent. Thus, this change from baseline reflects the Week 24 HbA1c percent minus the Week 0 HbA1c percent. (NCT00449930)
Timeframe: Baseline and 24 weeks

InterventionPercent (Least Squares Mean)
Sitagliptin 100 mg-0.43
Metformin-0.57

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Change From Baseline in A1C at Week 44

A1C is measured as percent. Thus, this change from baseline reflects the Week 44 A1C percent minus the Week 0 A1C percent. (NCT00482729)
Timeframe: Baseline and Week 44

InterventionPercent (Least Squares Mean)
Sita/Met FDC-2.25
Metformin-1.77

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Number of Patients With A1C < 7.0% at Week 44

(NCT00482729)
Timeframe: Week 44

,
InterventionParticipants (Number)
Patients with A1C <7.0% at Week 44Patients with A1C ≥7.0% at Week 44
Metformin173396
Sita/Met FDC258302

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 18

FPG is measured as mg/dL. Thus, this change from baseline reflects the Week 18 FPG mg/dL minus the Week 0 FPG mg/dL. (NCT00482729)
Timeframe: Baseline and Week 18

Interventionmg/dL (Least Squares Mean)
Sita/Met FDC-69.4
Metformin-53.7

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Change From Baseline in Hemoglobin A1c (A1C) at Week 18

A1C is measured as percent. Thus, this change from baseline reflects the Week 18 A1C percent minus the Week 0 A1C percent. (NCT00482729)
Timeframe: Baseline and Week 18

InterventionPercent (Least Squares Mean)
Sita/Met FDC-2.37
Metformin-1.76

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Number of Patients With A1C < 7.0% at Week 18

(NCT00482729)
Timeframe: Week 18

,
InterventionParticipants (Number)
Patients with A1C <7.0% at Week 18Patients with A1C ≥7.0% at Week 18
Metformin193371
Sita/Met FDC275284

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Change in Fasting Plasma Glucose (FPG) From Week 0(Baseline) to Week 8 Least Squares Mean

change in FPG from Week 0(baseline) to week 8 least squares mean and 95% confidence interval change = week 8 - week 0. (NCT00484419)
Timeframe: 8 weeks change = week 8- week 0.

Interventionmg/dL (Least Squares Mean)
Colesevelam-15.6
Rosiglitazone-28.9
Sitagliptin-17.4

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Change in Fasting Insulin From Week 0(Baseline) to Week 16 Least Squares Mean

change in fasting insulin from Week 0(baseline) to week 16 least squares mean and 95% confidence interval change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

InterventionuIU/mL (Least Squares Mean)
Colesevelam-0.320
Rosiglitazone-1.482
Sitagliptin0.092

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Change in Fasting Insulin From Week 0(Baseline) to Week 8 Least Squares Mean

change in fasting insulin from Week 0(baseline) to week 8 least squares mean and 95% confidence interval change = week 8 - week 0. (NCT00484419)
Timeframe: 8 weeks change = week 8- week 0.

InterventionuIU/mL (Least Squares Mean)
Colesevelam0.075
Rosiglitazone-2.156
Sitagliptin4.002

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Change in FPG From Week 0(Baseline) to Week 16 Least Squares Mean

change in FPG from Week 0(baseline) to week 16 least squares mean and 95% confidence interval change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Interventionmg/dL (Least Squares Mean)
Colesevelam-17.3
Rosiglitazone-31.4
Sitagliptin-24.4

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Change in Low-Density Lipoprotein-C(LDL-C) From Week 0(Baseline) to Week 16 Least Squares Mean

change in LDL-C from Week 0(baseline) to week 16 least squares mean with 95% confidence intervals change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Interventionmg/dL (Least Squares Mean)
Colesevelam-19.5
Rosiglitazone4.9
Sitagliptin6.2

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Change in Post-prandial Glucose From Week 0(Baseline) to Week 16 Least Squares Mean

change in post-prandial glucose from Week 0(baseline) to week 16 least squares mean with 95% confidence intervals change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Interventionmg/dL (Least Squares Mean)
Colesevelam-17.7
Rosiglitazone-53.6
Sitagliptin-43.6

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Mean Change in Fasting Insulin From Week 0(Baseline) to Week 16

mean change in fasting insulin from Week 0(baseline) to week 16 with standard deviation change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

InterventionuIU/mL (Mean)
Colesevelam-0.212
Rosiglitazone-1.910
Sitagliptin-0.419

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Mean Change in Fasting Insulin From Week 0(Baseline) to Week 8

mean change in fasting insulin from Week 0(baseline) to week 8 with standard deviation change = week 8 - week 0. (NCT00484419)
Timeframe: 8 weeks change = week 8- week 0.

InterventionuIU/mL (Mean)
Colesevelam0.107
Rosiglitazone-2.213
Sitagliptin4.028

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Mean Change in FPG From Week 0(Baseline) to Week 16

change in FPG from Week 0(baseline) to week 16 mean and standard deviation change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Interventionmg/dL (Mean)
Colesevelam-15.8
Rosiglitazone-34.0
Sitagliptin-23.1

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Mean Change in FPG From Week 0(Baseline) to Week 8

mean change in FPG from Week 0(baseline) to Week 8 with standard deviation change = week 8 - week 0. (NCT00484419)
Timeframe: 8 weeks change = week 8- week 0.

Interventionmg/dL (Mean)
Colesevelam-12.5
Rosiglitazone-30.8
Sitagliptin-18.6

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Mean Change in LDL-C From Week 0(Baseline) to Week 16

mean change in LDL-C from Week 0(baseline) to week 16 with standard deviation change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Interventionmg/dL (Mean)
Colesevelam-19.7
Rosiglitazone5.5
Sitagliptin5.7

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Mean Change in Post-prandial Glucose From Week 0(Baseline) to Week 16

mean change in post-prandial glucose from Week 0(baseline) to week 16 with standard deviation change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Interventionmg/dL (Mean)
Colesevelam-20.1
Rosiglitazone-54.0
Sitagliptin-40.9

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Mean Change in Post-prandial Insulin From Week 0(Baseline) to Week 16

mean change in post-prandial insulin from Week 0(baseline) to week 16 with standard deviation change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Interventionmg/dL (Mean)
Colesevelam3.898
Rosiglitazone1.962
Sitagliptin4.832

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Mean Percentage of Change in Glycosylated Hemoglobin (HbA1c) From Week 0(Baseline) to Week 16 Endpoint Least Squares Mean

Change in HbA1c from Week 0(baseline)to Week 16 endpoint least squares mean with 95% confidence intervals, change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention% change in HbA1c (Least Squares Mean)
Colesevelam-0.27
Rosiglitazone-0.58
Sitagliptin-0.38

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Mean Percentage of Change in HbA1c From Week 0(Baseline) to Week 16 Endpoint

Change in HbA1c from Week 0(baseline) to Week 16 endpoint mean with standard deviation change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention% change HbA1c (Mean)
Colesevelam-0.31
Rosiglitazone-0.65
Sitagliptin-0.56

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Mean Percentage of Change in HbA1c From Week 0(Baseline) to Week 8

change in HbA1c from Week 0(baseline) to week 8 mean and standard deviation change = week 8 - week 0. (NCT00484419)
Timeframe: 8 weeks change = week 8- week 0.

Intervention% change in HbA1c (Mean)
Colesevelam-0.31
Rosiglitazone-0.19
Sitagliptin-0.48

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Mean Percentage of Change in LDL-C Levels From Week 0(Baseline) to Week 16

mean percent change in LDL-C levels from Week 0(baseline) to Week 16 mean with standard deviation change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention% change in LDL-C (Mean)
Colesevelam-16.40
Rosiglitazone7.41
Sitagliptin7.61

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Mean Percentage of Change in LDL-C Levels From Week 0(Baseline) to Week 16 (Least Squares Mean)

percent change in LDL-C levels from Week 0(baseline) to Week 16 (least squares mean with 95% confidence interval) (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention% change in LDL-C (Least Squares Mean)
Colesevelam-16.24
Rosiglitazone6.92
Sitagliptin7.98

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Change From Baseline in Fasting Plasma Glucose (FPG)

Change from baseline in mean Fasting Plasma Glucose after treatment with sitagliptin versus glipizide for 54 weeks. (NCT00509236)
Timeframe: Baseline / Week 54

,
Interventionmg/dL (Mean)
BaselineWeek 54Change from Baseline to Week 54
Glipizide 2.5 mg - 20 mg167.0134.0-33.0
Sitagliptin 25 mg160.3135.8-24.5

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Change From Baseline in Hemoglobin A1c After Sitagliptin Treatment

Change from baseline in mean hemoglobin A1c after treatment with sitagliptin for 54 weeks. Hemoglobin A1c is the percent of hemoglobin that is glycated. Results for the glipizide arm are not reported in this table because the primary outcome measure is for the sitagliptin arm only. (NCT00509236)
Timeframe: Baseline / Week 54

InterventionPercent hemoglobin A1c (Mean)
BaselineWeek 54Change from Baseline at Week 54
Sitagliptin 25 mg7.897.15-0.74

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Change From Baseline in Hemoglobin A1c for Sitagliptin Versus Glipizide Treatment

Change from baseline in least square means hemoglobin A1c after treatment with sitagliptin versus glipizide for 54 weeks. Hemoglobin A1c is the percent of hemoglobin that is glycated. (NCT00509236)
Timeframe: Baseline / Week 54

InterventionPercent hemoglobin A1c (Least Squares Mean)
Sitagliptin 25 mg-0.72
Glipizide 2.5 mg - 20 mg-0.87

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Number of Participants With Clinical Adverse Events

Reported experiences assessed by investigators as adverse events, excluding data after initiation of glycemic rescue therapy. (NCT00509236)
Timeframe: 54 Week Treatment Period + 28 days

InterventionParticipants (Number)
Sitagliptin 25 mg53
Glipizide 2.5 mg - 20 mg52

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Number of Participants With Symptomatic Hypoglycemic Adverse Events

A symptomatic hypoglycemic adverse event is an episode with clinical symptoms attributed to hypoglycemia, without regard to fingerstick glucose level. (NCT00509236)
Timeframe: 54 Week Treatment Period + 28 days

InterventionParticipants (Number)
Sitagliptin 25 mg4
Glipizide 2.5 mg - 20 mg7

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Percentage of Participants With Hypoglycemic Events

Percentage of participants with at least one symptomatic hypoglycemic adverse event, excluding data after initiation of glycemic rescue therapy. (NCT00509262)
Timeframe: Baseline up to 28 days following the last dose of study therapy

Interventionpercentage of participants (Number)
Sitagliptin6.2
Glipizide17.0

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 54

(NCT00509262)
Timeframe: Baseline to Week 54

,
Interventionmg/dL (Mean)
BaselineChange from Baseline at Week 54
Glipizide143.9-20.2
Sitagliptin148.6-16.7

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Change From Baseline in Body Weight at Week 54

(NCT00509262)
Timeframe: Baseline to Week 54

Interventionkg (Least Squares Mean)
Sitagliptin-0.6
Glipizide1.2

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Change From Baseline in Hemoglobin A1c (A1C) Levels at Week 54

A1C represents percentage of glycosylated hemoglobin. (NCT00509262)
Timeframe: Baseline to Week 54

,
InterventionPercent of glycosylated hemoglobin (Mean)
BaselineChange from Baseline at Week 54
Glipizide7.79-0.62
Sitagliptin7.76-0.70

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Change From Baseline in Glucagon 3-hour Total Area Under the Curve (AUC) After 12 Weeks of Treatment

Glucagon concentration was measured at 9 points during an Meal Tolerance Test (MTT), at times -10, 0, 10, 20, 30, 60, 90, 120, and 180 minutes. Total AUC was calculated over 3 hours including all sample points starting from 0 minutes using the trapezoid method. The change from baseline reflects Week 12 total AUC minus the Week 0 total AUC. (NCT00511108)
Timeframe: Baseline and 12 weeks

Interventionpg*hr/mL (Least Squares Mean)
Sitagliptin 100 mg-17.2
Pioglitazone 30 mg-4.9
Sitagliptin 100 mg + Pioglitazone 30 mg-29.8
Placebo12.5

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Change From Baseline in Glucose 5-hour Total AUC After 12 Weeks of Treatment

Glucose concentration was measured at 11 points during an Meal Tolerance Test (MTT), at times -10, 0, 10, 20, 30, 60, 90, 120, 180, 240, 300 minutes. Total AUC was calculated over 5 hours including all sample points starting from 0 minutes using the trapezoid method. The change from baseline reflects Week 12 total AUC minus the Week 0 total AUC. (NCT00511108)
Timeframe: Baseline and 12 weeks

Interventionmg*hr/dL (Least Squares Mean)
Sitagliptin 100 mg-209.8
Pioglitazone 30 mg-245.6
Sitagliptin 100 mg + Pioglitazone 30 mg-389.2
Placebo18.6

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Percent Change From Baseline in Index of Static Beta-cell Sensitivity to Glucose After 12 Weeks of Treatment

"Static sensitivity is a measure of the effect of glucose on beta cell secretion and is the ratio between the insulin secretion rate and glucose concentration above the threshold level at steady state.~Percent change from baseline was calculated as the difference between index of static sensitivities at Week 12 and at baseline with respect to the index of static sensitivity at baseline times 100." (NCT00511108)
Timeframe: Baseline and 12 weeks

InterventionPercent Change (Least Squares Mean)
Sitagliptin 100 mg71.5
Pioglitazone 30 mg27.0
Sitagliptin 100 mg + Pioglitazone 30 mg125.2
Placebo-2.3

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 1

Change from baseline reflects the Week 1 FPG minus the baseline FPG. At Week 1, the dose was 50/500 mg b.i.d. for Sita/Met FDC and 30 mg q.d. for pioglitazone (NCT00532935)
Timeframe: Baseline and Week 1

Interventionmg/dL (Least Squares Mean)
Sitagliptin/Metformin Fixed-Dose Combination-40.5
Pioglitazone-13.0

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Change From Baseline in A1C at Week 32

A1C is measured as a percent. Thus this change from baseline reflects the Week 32 A1C percent minus the baseline A1C percent (NCT00532935)
Timeframe: Baseline and Week 32

InterventionPercent of glycosylated hemoglobin (A1C) (Least Squares Mean)
Sitagliptin/Metformin Fixed-Dose Combination-1.86
Pioglitazone-1.39

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Change From Baseline in FPG at Week 32

Change from baseline reflects the Week 32 FPG minus the baseline FPG (NCT00532935)
Timeframe: Baseline and Week 32

Interventionmg/dL (Least Squares Mean)
Sitagliptin/Metformin Fixed-Dose Combination-56.0
Pioglitazone-44.0

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Change From Baseline in 2-hour Post-Meal Glucose (PMG) at Week 32

Change from baseline reflects the Week 32 2-hour PMG minus the baseline 2-hour PMG (NCT00532935)
Timeframe: Baseline and Week 32

Interventionmg/dL (Least Squares Mean)
Sitagliptin/Metformin Fixed-Dose Combination-102.2
Pioglitazone-82.0

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Percent of Participants With A1C <7.0% at Week 32

(NCT00532935)
Timeframe: Week 32

InterventionPercent Participants (Number)
Sitagliptin/Metformin Fixed-Dose Combination57.3
Pioglitazone43.5

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24-hour Weighted Mean Glucose (WMG)

The 24-hour WMG was calculated as the area under the 24-hour glucose curve (AUC(0-24 hr)) divided by 24 using linear trapezoidal method. (NCT00541229)
Timeframe: Day 7 of Treatment Period I. Due to a carry-over effect that was observed between treatment periods, efficacy results are presented from Treatment Period I only.

Interventionmg/dL (Least Squares Mean)
Sitagliptin 200mg169.1
Sitagliptin 100mg159.0
Placebo200.9

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Change in Fasting Plasma Glucose (FPG) in Participants Treated With Sitagliptin or Pioglitazone at 12 Weeks

The change in FPG compared to baseline was measured for the participants treated with sitagliptin or pioglitazone at Week 12. Sitagliptin was the only intervention administered to the Sita/Met FDC group during this phase. To calculate Least Squares, the ANCOVA model included a term for treatment and the baseline value as a covariate. (NCT00541450)
Timeframe: Baseline to 12 weeks

Interventionmg/dL (Least Squares Mean)
Sitagliptin (Phase A)-26.6
Pioglitazone (Phase A)-28.0

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Change in Fasting Plasma Glucose (FPG) in the Sita/Met FDC or Pioglitazone Groups at 40 Weeks

The change in FPG compared to baseline was measured for the Sita/Met FDC and the pioglitazone groups at Week 40. (NCT00541450)
Timeframe: Baseline and 40 weeks

Interventionmg/dL (Least Squares Mean)
Sita/Met FDC-45.8
Pioglitazone-37.6

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Change in Hemoglobin A1c (A1C) in Participants Treated With Sitagliptin or Pioglitazone at 12 Weeks

The change in A1C compared to baseline was measured for the participants treated with sitagliptin or pioglitazone at Week 12. Sitagliptin was the only intervention administered to the Sita/Met FDC group during this phase. A1c represents percentage of glycosylated hemoglobin. (NCT00541450)
Timeframe: Baseline to 12 weeks

Interventionpercentage of glycosylated hemoglobin (Least Squares Mean)
Sitagliptin (Phase A)-1.03
Pioglitazone (Phase A)-0.87

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Change in Hemoglobin A1c (A1C) in the Sita/Met Fixed-Dose Combination (FDC) or Pioglitazone Groups at 40 Weeks

The change in A1C, compared to baseline for the Sita/Met FDC and the pioglitazone groups at Week 40. A1C represents percentage of glycosylated hemoglobin. (NCT00541450)
Timeframe: Baseline to 40 weeks

Interventionpercentage of glycosylated hemoglobin (Least Squares Mean)
Sita/Met FDC-1.75
Pioglitazone-1.38

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Change in 2-hour Postprandial Glucose (PMG) in the Sita/Met FDC or Pioglitazone Groups at 40 Weeks

The change in PMG compared to baseline was measured using the Meal Tolerance Test (MTT) for the Sita/Met FDC and the pioglitazone groups at Week 40. (NCT00541450)
Timeframe: Baseline and 40 weeks

Interventionmg/dL (Least Squares Mean)
Sita/Met FDC-90.3
Pioglitazone-69.1

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Change in 2-hour Postprandial Glucose (PMG) in Participants Treated With Sitagliptin or Pioglitazone at 12 Weeks

The change in PMG compared to baseline was measured using the Meal Tolerance Test (MTT) for the participants treated with Sitagliptin or Pioglitazone at Week 12. Sitagliptin was the only intervention administered to the Sita/Met FDC group during this phase. To calculate Least Squares, the ANCOVA model included a term for treatment and the baseline value as a covariate. (NCT00541450)
Timeframe: Baseline to 12 weeks

Interventionmg/dL (Least Squares Mean)
Sitagliptin (Phase A)-52.8
Pioglitazone (Phase A)-50.1

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2-hour Post-meal Glucose (PMG) at Week 18

The change from baseline is the Week 18 PMG minus the Week 0 PMG. (NCT00541775)
Timeframe: Baseline and 18 Weeks

Interventionmg/dL (Least Squares Mean)
Sitagliptin-35.4
Rosiglitazone-51.3
Placebo-4.9

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Hemoglobin A1C (A1C) at Week 18

"A1C is measured as percent. Thus, this change from baseline reflects the Week 18 A1C percent minus the Week 0 A1C percent.~The study hypothesis comparison was between sitagliptin versus placebo." (NCT00541775)
Timeframe: Baseline and 18 Weeks

InterventionPercent of glycosylated hemoglobin (A1C) (Least Squares Mean)
Sitagliptin-0.73
Rosiglitazone-0.79
Placebo-0.22

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Fasting Plasma Glucose (FPG) at Week 18

The change from baseline is the Week 18 FPG minus the Week 0 FPG. (NCT00541775)
Timeframe: Baseline and 18 Weeks

Interventionmg/dL (Least Squares Mean)
Sitagliptin-11.7
Rosiglitazone-24.5
Placebo6.1

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Fasting Plasma Glucose (FPG) Measurement

Generally FPG values of ~5.0-7.2 mmol/L would be considered goal (American Diabetes Association). (NCT00545584)
Timeframe: Baseline and Week 24

,,
Interventionmmol/L glucose (Mean)
Baseline (n=350, 350, 252, respectively)Week 24 (n=310, 303, and 224, respectively)
Sitagliptin With Diet Advice9.008.32
Sitagliptin With Diet and Physical Activity Advice8.918.47
Sitagliptin With Standard of Care8.878.21

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Hemoglobin A1c Measurement

Hemoglobin A1c (HbA1c) is a measure of glycated hemoglobin in the blood. HbA1c greater than 6.5% was considered inadequately controlled. (NCT00545584)
Timeframe: Baseline and Week 24

,,
Interventionpercent HbA1c (Mean)
Baseline (n=360, 358, and 265, respectively)Week 24 (n=362, 358, and 265, respectively)
Sitagliptin With Diet Advice7.507.42
Sitagliptin With Diet and Physical Activity Advice7.497.40
Sitagliptin With Standard of Care7.377.33

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Change From Baseline (BL) to Week 4 in 24-hour Weighted Mean Glucose (WMG) Levels

(NCT00631488)
Timeframe: BL, 4 weeks (end of double-blind treatment period)

Interventionmg/dL (Least Squares Mean)
MK-0893 + Sitagliptin-85.7
MK-0893 + Metformin-117.4
Sitagliptin + Metformin-99.6

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Change From BL to Week 4 in 2-hr Glucose Area Under The Curve (AUC)

(NCT00631488)
Timeframe: BL, 4 weeks (end of double-blind treatment period)

Interventionmg.h/dL (Least Squares Mean)
MK-0893 + Sitagliptin-187.7
MK-0893 + Metformin-254.9
Sitagliptin + Metformin-210.3

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Change From BL to Week 4 in Fasting Plasma Glucose (FPG)

(NCT00631488)
Timeframe: BL, 4 weeks (end of double-blind treatment period)

Interventionmg/dL (Least Squares Mean)
MK-0893 + Sitagliptin-73.7
MK-0893 + Metformin-101.9
Sitagliptin + Metformin-82.8

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Change From BL to Week 4 in the 2-Hour Total GLP-1 Total AUC

Glucagon-Like Peptide-1 (GLP-1) is an incretin hormone that acts as a potent insulin secretegogue in response to nutrient ingestion and stimulates glucose disposition. The total AUC of Total GLP-1 levels was calculated from blood sample data measured after the morning meal. (NCT00631488)
Timeframe: BL, 4 weeks (end of double-blind treatment period)

Interventionpmol*h/L (Least Squares Mean)
MK-0893 + Sitagliptin7.4
MK-0893 + Metformin16.4
Sitagliptin + Metformin3.2

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Change From BL to Week 4 in the 2-Hour Active GLP-1 Total AUC

GLP-1 is cleaved from proglucagon to form the active peptide GLP-1. The active form promotes suppression of glucagon secretion. The total AUC of Active GLP-1 levels was calculated from blood sample data measured after the morning meal. (NCT00631488)
Timeframe: BL, 4 weeks (end of double-blind treatment period)

Interventionpmole*h/L (Least Squares Mean)
MK-0893 + Sitagliptin11.0
MK-0893 + Metformin6.3
Sitagliptin + Metformin17.6

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Ratio of Fasting Triglycerides at Week 26 to Baseline

Ratio of triglycerides (measured in mg/dL) at Week 26 to baseline (Day 1). Log (Postbaseline Triglycerides) - log (Baseline Triglycerides); change from baseline to endpoint is presented as ratio of endpoint to baseline. (NCT00637273)
Timeframe: Day 1, Week 26

Interventionratio (Least Squares Mean)
Exenatide Once Weekly0.95
Sitagliptin0.95
Pioglitazone0.84

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Assessment on Event Rate of Treatment-emergent Hypoglycemic Events

Major hypoglycemia: events that, in the judgment of the investigator or physician, resulted in loss of consciousness, seizure, coma, or other change in mental status consistent with neuroglycopenia, in which symptoms resolved after administration of intramuscular glucagon or intravenous glucose, required third-party assistance, and was accompanied by a blood glucose concentration < 54 mg/dL prior to treatment. Minor hypoglycemia: symptoms consistent with hypoglycemia and blood glucose concentration < 54 mg/dL prior to treatment and not classified as major hypoglycemia. (NCT00637273)
Timeframe: Day 1 to Week 26

,,
Interventionrate per subject-year (Mean)
Treatment-Emergent Major HypoglycemiaTreatment-Emergent Minor Hypoglycemia
Exenatide Once Weekly0.000.03
Pioglitazone0.000.01
Sitagliptin0.000.12

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Change in Fasting Plasma Glucose From Baseline to Week 26

Change in fasting plasma glucose from baseline (Day 1) to Week 26. (NCT00637273)
Timeframe: Day 1, Week 26

Interventionmg/dL (Least Squares Mean)
Exenatide Once Weekly-31.8
Sitagliptin-16.3
Pioglitazone-27.3

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Change in Diastolic Blood Pressure From Baseline to Week 26

Change in diastolic blood pressure from baseline (Day 1) to Week 26. (NCT00637273)
Timeframe: Day 1, Week 26

InterventionmmHg (Least Squares Mean)
Exenatide Once Weekly-1.4
Sitagliptin-0.4
Pioglitazone-2.5

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Change in Fasting Total Cholesterol From Baseline to Week 26

Change in fasting total cholesterol from baseline (Day 1) to Week 26. (NCT00637273)
Timeframe: Day 1, Week 26

Interventionmg/dL (Least Squares Mean)
Exenatide Once Weekly-0.6
Sitagliptin3.1
Pioglitazone6.2

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Change in HbA1c From Baseline to Week 26

Absolute change in HbA1c from baseline (Day 1) to Week 26 [Week 26 - Baseline]. (NCT00637273)
Timeframe: Day 1, Week 26

Interventionpercentage of total hemoglobin (Least Squares Mean)
Exenatide Once Weekly-1.55
Sitagliptin-0.92
Pioglitazone-1.23

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Change in Systolic Blood Pressure From Baseline to Week 26

Change in systolic blood pressure from baseline (Day 1) to Week 26. (NCT00637273)
Timeframe: Day 1, Week 26

InterventionmmHg (Least Squares Mean)
Exenatide Once Weekly-3.6
Sitagliptin0.2
Pioglitazone-1.6

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Change in Body Weight From Baseline to Week 26

Change in body weight from baseline (Day 1) to Week 26. (NCT00637273)
Timeframe: Day 1, Week 26

Interventionkg (Least Squares Mean)
Exenatide Once Weekly-2.31
Sitagliptin-0.77
Pioglitazone2.79

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Change in Fasting High-density Lipoprotein (HDL) From Baseline to Week 26

Change in fasting HDL from baseline (Day 1) to Week 26. (NCT00637273)
Timeframe: Day 1, Week 26

Interventionmg/dL (Least Squares Mean)
Exenatide Once Weekly2.0
Sitagliptin2.0
Pioglitazone6.2

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Percentage of Subjects Achieving HbA1c Target of <=6.0% at Week 26

Percentages of subjects achieving HbA1c target values of <=6.0% at Week 26. (NCT00637273)
Timeframe: Week 26

Interventionpercentage of subjects (Number)
Exenatide Once Weekly13.8
Sitagliptin9.0
Pioglitazone4.8

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Percentage of Subjects Achieving HbA1c Target of <=6.5% at Week 26

Percentages of subjects achieving HbA1c target values of <=6.5% at Week 26. (NCT00637273)
Timeframe: Week 26

Interventionpercentage of subjects (Number)
Exenatide Once Weekly38.8
Sitagliptin15.7
Pioglitazone26.7

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Percentage of Subjects Achieving HbA1c Target of <7% at Week 26

Percentages of subjects achieving HbA1c target values of <7% at Week 26. (NCT00637273)
Timeframe: Week 26

Interventionpercentage of subjects (Number)
Exenatide Once Weekly58.8
Sitagliptin30.7
Pioglitazone43.6

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Absolute Change in Body Weight From Baseline to Week 12

The table below shows the mean absolute change in body weight from Baseline to Week 12 for each treatment group. (NCT00642278)
Timeframe: Day 1 (Baseline) and Week 12

Interventionkg (Mean)
Placebo-0.78
Canagliflozin 50 mg Daily-1.96
Canagliflozin 100 mg Daily-2.25
Canagliflozin 200 mg Daily-2.32
Canagliflozin 300 mg Daily-2.88
Canagliflozin 300 mg Twice Daily-2.87
Sitagliptin 100 mg Daily-0.43

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Change in Overnight Urine Glucose/Creatinine Ratio From Baseline to Week 12

The table below shows the mean change in overnight urine glucose/creatinine ratio from Baseline to Week 12 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin or sitagliptin group minus placebo) in the least-squares mean change. (NCT00642278)
Timeframe: Day 1 (Baseline) and Week 12

Interventionmg/mg (Mean)
Placebo1.9
Canagliflozin 50 mg Daily35.4
Canagliflozin 100 mg Daily51.5
Canagliflozin 200 mg Daily50.5
Canagliflozin 300 mg Daily49.4
Canagliflozin 300 mg Twice Daily61.6
Sitagliptin 100 mg Daily-1.9

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Percent Change in Body Weight From Baseline to Week 12

The table below shows the mean percent change in body weight from Baseline to Week 12 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin or sitagliptin group minus placebo) in the least-squares mean change. (NCT00642278)
Timeframe: Day 1 (Baseline) and Week 12

InterventionPercent change (Mean)
Placebo-1.1
Canagliflozin 50 mg Daily-2.3
Canagliflozin 100 mg Daily-2.6
Canagliflozin 200 mg Daily-2.7
Canagliflozin 300 mg Daily-3.4
Canagliflozin 300 mg Twice Daily-3.4
Sitagliptin 100 mg Daily-0.6

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Percentage of Patients With Symptoms of Hypoglycemia

The table below shows the percentage of patients who experienced symptomatic hypoglycemic events between Baseline and Week 12. (NCT00642278)
Timeframe: Up to Week 12

InterventionPercentage of patients (Number)
Placebo2
Canagliflozin 50 mg Daily0
Canagliflozin 100 mg Daily2
Canagliflozin 200 mg Daily6
Canagliflozin 300 mg Daily0
Canagliflozin 300 mg Twice Daily3
Sitagliptin 100 mg Daily5

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Change in Fasting Plasma Glucose (FPG) From Baseline to Week 12

The table below shows the mean change in FPG from Baseline to Week 12 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin or sitagliptin group minus placebo) in the least-squares mean change. (NCT00642278)
Timeframe: Day 1 (Baseline) and Week 12

Interventionmmol/L (Mean)
Placebo0.2
Canagliflozin 50 mg Daily-0.9
Canagliflozin 100 mg Daily-1.4
Canagliflozin 200 mg Daily-1.5
Canagliflozin 300 mg Daily-1.4
Canagliflozin 300 mg Twice Daily-1.3
Sitagliptin 100 mg Daily-0.7

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Change in HbA1c From Baseline to Week 12

The table below shows the mean change in HbA1c from Baseline to Week 12 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin or sitagliptin group minus placebo) in the least-squares mean change. (NCT00642278)
Timeframe: Day 1 (Baseline) and Week 12

InterventionPercent (Mean)
Placebo-0.22
Canagliflozin 50 mg Daily-0.79
Canagliflozin 100 mg Daily-0.76
Canagliflozin 200 mg Daily-0.70
Canagliflozin 300 mg Daily-0.92
Canagliflozin 300 mg Twice Daily-0.95
Sitagliptin 100 mg Daily-0.74

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Determine the Effects of Sitagliptin on Myocardial Glucose Uptake Measured by Myocardial PET Scan

This study will investigate the effects of sitagliptin, a medicine commonly used to treat type 2 diabetes, on the utilization of glucose by the heart in patients with heart failure which is not due to heart attacks. We hope to determine whether improving the heart's ability to use glucose in the blood may help improve the function of the heart as well. If so, this may suggest that even people who do not have frank diabetes but who do have heart failure may benefit from using this medication. Baseline glucose uptake scans will be compared with the scans on sitagliptin thirty days after baseline (NCT00657280)
Timeframe: 30 days

InterventionSUV (Mean)
Baseline30 days
Sitagliptin3.44.1

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Change in Oxidative Stress From Baseline to 12 Weeks

"To investigate that therapy with sitagliptin orally daily (100 mg) for 12 weeks decreases oxidized lipids (9-hydroxyoctadecadienoicacid (9-HODE) and 13-HODE) in plasma and F2-isoprostane in urine of obese type 2 diabetic patients~Outcome measures given are calculated from the baseline - 12 weeks." (NCT00659711)
Timeframe: value at 12 weeks minus value at baseline

InterventionmM (Mean)
Januvia 100mg-0.13
Placebo-0.06

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Change in Reactive Oxygen Species (ROS) Generation by MNC, Protein and mRNA Expression of p47phox Subunit of NADPH Oxidase, in MNC's of Obese Type 2 Diabetic Patients

(NCT00659711)
Timeframe: 12 weeks

,
InterventionPercent change (Mean)
TNF-alphaTLR-4TLR-2JNK-1IKK-betaCCR-2
Januvia 100mg-39-23-35-19-17-24
Placebo1283496

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Measurement of the Area Under the Curve of Plasma Triglycerides (TG) Levels During Postprandial Period (Time 0,2,4,6,8 Hours)

(NCT00660075)
Timeframe: At the end of the two 6-week interventions

Interventionmmol*h/L (Mean)
Placebo30.0
Sitagliptin 100 mg/d27.1

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Hemoglobin A1c (HbA1c) Change From Baseline to Week 18

Adjusted mean change from baseline in HbA1c achieved with saxagliptin added on to metformin versus sitagliptin added on to metformin at Week 18 (Per Protocol Analysis Set). HbA1c is a continuous measure, the change from baseline for each participant is calculated as the Week 18 value minus the baseline value. (NCT00666458)
Timeframe: Baseline, Week 18

,
InterventionPercent (Mean)
BaselineWeek 18Adjusted Change from Baseline
Saxa + Met7.687.16-0.52
Sita + Met7.697.07-0.62

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Fasting Plasma Glucose Change From Baseline to Week 18 (mmol/L)

Adjusted mean change from baseline in Fasting Plasma Glucose achieved with saxagliptin added on to metformin versus sitagliptin added on to metformin at Week 18 (Full Analysis Set). Fasting Plasma Glucose is a continuous measure, the change from baseline for each participant is calculated as the Week 18 (LOCF) value minus the baseline value. (NCT00666458)
Timeframe: Baseline, Week 18 (Last Observation Carried Forward)

,
Interventionmmol/L (Mean)
BaselineWeek 18Adjusted Change from Baseline
Saxa + Met8.868.27-0.60
Sita + Met8.897.99-0.90

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Fasting Plasma Glucose Change From Baseline to Week 18 (mg/dL)

Adjusted mean change from baseline in Fasting Plasma Glucose achieved with saxagliptin added on to metformin versus sitagliptin added on to metformin at Week 18 (Full Analysis Set). Fasting Plasma Glucose is a continuous measure, the change from baseline for each participant is calculated as the Week 18 (LOCF) value minus the baseline value. (NCT00666458)
Timeframe: Baseline, Week 18 (Last Observation Carried Forward)

,
Interventionmg/dL (Mean)
BaselineWeek 18Adjusted Change from Baseline
Saxa + Met159.67149.04-10.75
Sita + Met160.22143.94-16.16

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Proportion of Patients Achieving Therapeutic Glycaemic Response Defined as HbA1c <= 6.5% at Week 18

Proportion of Patients Achieving Therapeutic Glycaemic Response Defined as HbA1c <= 6.5% at Week 18 (Full Analysis Set) (NCT00666458)
Timeframe: Week 18 (Last Observation Carried Forward)

InterventionPercentage of Participants (Number)
Saxa + Met26.3
Sita + Met29.1

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Change in MAP During Sitagliptin

Mean change in mean arterial pressure in response to placebo or enalapril in the presence of 5 days of sitagliptin 100mg/day (NCT00666848)
Timeframe: just prior to drug administration and 8 hours following treatment

InterventionmmHg (Mean)
2 (Enalapril 5mg)-5.7
1 (Placebo)-2.3
3 (Enalapril 10mg)-0.9

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Change in MAP During Placebo

The change in mean arterial pressure (MAP) in response to placebo or enalapril after pretreatment with 5 days of placebo (NCT00666848)
Timeframe: just prior to drug administration and 8 hours after drug administration

InterventionmmHg (Mean)
2 (Enalapril 5mg)-0.9
1 (Placebo)2.7
3 (Enalapril 10mg)-7.9

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Fructosamine

The blood concentration of the glycemic control marker fructosamine (NCT00673894)
Timeframe: 4 weeks

Interventionmicro mol per litre (Mean)
Glutamine+Sitagliptin244
Glutamine+Placebo240

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Postprandial Glucose Area Under the Curve (AUC)

The area under the curve (AUC) of the postprandial glucose following a meal challenge (NCT00673894)
Timeframe: 0 to 180 minutes

Interventionmmol/L*t (Mean)
Glutamine+Sitagliptin1341
Glutamine+Placebo1463

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Assessment on Event Rate of Treatment-emergent Major Hypoglycemic Events

Major hypoglycemia is defined as any event that has symptoms consistent with hypoglycemia resulting in loss of consciousness or seizure that shows prompt recovery in response to administration of glucagon or glucose, or documented hypoglycemia (blood glucose <3.0 mmol/L [54 mg/dL]) requiring the assistance of another person because of severe impairment in consciousness or behavior (whether or not symptoms of hypoglycemia are detected by the patient). Mean event rate = total number of events for all subjects in a treatment regimen / the total number of subject years of exposure for all subjects in that treatment. Standard error = square root of (total number of events / (subject years of exposure)**2). (NCT00676338)
Timeframe: Baseline to Week 26

Interventionevents per subject-year (Mean)
Exenatide Once Weekly0.00
Metformin0.00
Pioglitazone0.00
Sitagliptin0.00

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Assessment on Event Rate of Treatment-Emergent Minor Hypoglycemic Events

Minor hypoglycemia is defined as a sign or symptom associated with hypoglycemia that is either self-treated by the patient or resolves on its own AND has a concurrent finger stick blood glucose <3.0 mmol/L (54 mg/dL) and not classified as major hypoglycemia. Mean event rate = total number of events for all subjects in a treatment regimen / the total number of subject years of exposure for all subjects in that treatment. Standard error = square root of (total number of events / (subject years of exposure)**2). (NCT00676338)
Timeframe: Baseline to Week 26

Interventionevents per subject-year (Mean)
Exenatide Once Weekly0.05
Metformin0.00
Pioglitazone0.00
Sitagliptin0.00

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Change in Body Weight From Baseline to Week 26

Change in Body Weight from baseline to Week 26. (NCT00676338)
Timeframe: Baseline, Week 26

Interventionkg (Least Squares Mean)
Exenatide Once Weekly-2.04
Metformin-2.00
Pioglitazone1.52
Sitagliptin-0.76

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Change in Diastolic Blood Pressure From Baseline to Week 26.

Change in Diastolic Blood Pressure from baseline to Week 26. (NCT00676338)
Timeframe: Baseline, Week 26

InterventionmmHg (Least Squares Mean)
Exenatide Once Weekly-0.50
Metformin-0.86
Pioglitazone-2.50
Sitagliptin-0.45

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Change in Fasting High-Density Lipoprotein (HDL) From Baseline to Week 26

Change in Fasting HDL from baseline to Week 26. (NCT00676338)
Timeframe: Baseline, Week 26

Interventionmmol/L (Least Squares Mean)
Exenatide Once Weekly0.01
Metformin0.07
Pioglitazone0.17
Sitagliptin0.04

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Percentage of Patients Achieving HbA1c <=7% at Week 26

Percentage of patients achieving HbA1c <=7% at Week 26 (for patients with baseline HbA1c >7%). (NCT00676338)
Timeframe: Baseline, Week 26

Interventionpercentage of patients (Number)
Exenatide Once Weekly64.2
Metformin57.3
Pioglitazone63.3
Sitagliptin45.5

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Change in Systolic Blood Pressure From Baseline to Week 26.

Change in Systolic Blood Pressure from baseline to Week 26. (NCT00676338)
Timeframe: Baseline, Week 26

InterventionmmHg (Least Squares Mean)
Exenatide Once Weekly-1.25
Metformin0.14
Pioglitazone-1.74
Sitagliptin-1.81

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Change in HbA1c From Baseline to Week 26

Change in HbA1c from baseline to Week 26. (NCT00676338)
Timeframe: Baseline, Week 26

Interventionpercentage of total hemoglobin (Least Squares Mean)
Exenatide Once Weekly-1.53
Metformin-1.48
Pioglitazone-1.63
Sitagliptin-1.15

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Change in Fasting Total Cholesterol (TC) From Baseline to Week 26

Change in Fasting TC from baseline to Week 26. (NCT00676338)
Timeframe: Baseline, Week 26

Interventionmmol/L (Least Squares Mean)
Exenatide Once Weekly-0.24
Metformin-0.22
Pioglitazone0.09
Sitagliptin-0.01

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Change in Fasting Serum Glucose (FSG) From Baseline to Week 26

Change in FSG from baseline to Week 26. (NCT00676338)
Timeframe: Baseline, Week 26

Interventionmmol/L (Least Squares Mean)
Exenatide Once Weekly-2.25
Metformin-1.98
Pioglitazone-2.57
Sitagliptin-1.13

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Ratio of Fasting Triglycerides at Week 26 to Baseline

Ratio of Fasting Triglycerides (measured in mmol/L) at Week 26 to baseline. Log(Post-baseline Triglycerides) - log(Baseline Triglycerides); change from baseline to Week 26 is presented as ratio of endpoint to baseline. (NCT00676338)
Timeframe: Baseline, Week 26

Interventionratio (Least Squares Mean)
Exenatide Once Weekly0.98
Metformin0.96
Pioglitazone0.85
Sitagliptin0.94

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Number of Subjects Maintaining Hemoglobin A1c 7.5% or Less by 1 Year

(NCT00686634)
Timeframe: 1 year

Interventionparticipants (Number)
Sitagliptin26

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Number of Subjects With Hemoglobin A1c 7.5% or Less at 4 Months

(NCT00686634)
Timeframe: 4 months

Interventionparticipants (Number)
Sitagliptin47

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Number of Adverse Events

(NCT00686634)
Timeframe: 1 year

InterventionAdverse event (Number)
HypoglycemiaOther adverse events
Sitagliptin33

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Hemoglobin A1c (HbA1c) Change From Baseline

(NCT00686634)
Timeframe: Baseline, 4 months

Interventionpercentage (Mean)
Sitagliptin-1.3

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Percentage of Subjects Achieving Treatment Target of HbA1c < 7.0% at Week 78

Calculated as an estimate of the percentage of subjects achieving treatment target of HbA1c < 7.0% at Week 78. Based on the extension 2 FAS. (NCT00700817)
Timeframe: Week 0, Week 78

Interventionpercentage of subjects (Number)
Sita -> Sita -> Lira 1.2 mg49
Sita -> Sita -> Lira 1.8 mg50

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Mean Change From Baseline in Tumour Necrosis Factor Alpha (TNF-alpha) at Week 26.

Calculated as an estimate of the mean change from baseline in Tumour Necrosis Factor Alpha (TNF-alpha) at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionpg/mL (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.55
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.74
Sita -> Sita-0.53

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Mean Change From Baseline in Triglycerides (TG) at Week 52

Calculated as an estimate of the change from baseline in triglycerides (TG) at Week 52. (NCT00700817)
Timeframe: Week 0, Week 52

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.10
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.32
Sita -> Sita-0.23

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Mean Change From Baseline in Triglycerides (TG) at Week 26

Calculated as an estimate of the change from baseline in triglycerides (TG) at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.19
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.43
Sita -> Sita-0.40

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Mean Change From Baseline in Total Cholesterol at Week 52

Calculated as an estimate of the mean change from baseline in total cholesterol at Week 52. (NCT00700817)
Timeframe: Week 0, Week 52

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.01
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.09
Sita -> Sita0.03

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Mean Change From Baseline in Fasting Plasma Glucose (FPG) at Week 26

Calculated as an estimate of the mean change from baseline in fasting plasma glucose (FPG) at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-1.87
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-2.14
Sita -> Sita-0.83

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Mean Change From Baseline in Diastolic Blood Pressure (DBP) at Week 52

Calculated as an estimate of the mean change from baseline in diastolic blood pressure (DBP) at Week 52. (NCT00700817)
Timeframe: Week 0, Week 52

InterventionmmHg (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.53
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.87
Sita -> Sita-1.47

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Mean Change From Baseline in Fasting Plasma Glucose (FPG) at Week 78

Calculated as an estimate of the mean change in fasting plasma glucose (FPG) from baseline to Week 78. (NCT00700817)
Timeframe: Week 0, Week 78

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-1.30
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-1.65

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Mean Change From Baseline in Free Fatty Acids (FFA) at Week 26

Calculated as an estimate of the change from baseline in free fatty acids (FFA) at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.03
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.07
Sita -> Sita-0.05

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Mean Change From Baseline in Free Fatty Acids (FFA) at Week 52

Calculated as an estimate of the change from baseline in free fatty acids (FFA) at Week 52. (NCT00700817)
Timeframe: Week 0, Week 52

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.07
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.10
Sita -> Sita-0.06

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Mean Change From Baseline in Glycosylated Haemoglobin A1c (HbA1c) at Week 26

Calculated as an estimate of the mean change from baseline in glycosylated haemoglobin A1c (HbA1c) at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

InterventionPercentage point of total HbA1c (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-1.24
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-1.5
Sita -> Sita-0.9

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Mean Change From Baseline in Glycosylated Haemoglobin A1c (HbA1c) at Week 52

Calculated as an estimate of the mean change from baseline in glycosylated haemoglobin A1c (HbA1c) at Week 52. (NCT00700817)
Timeframe: Week 0, Week 52

InterventionPercentage point of total HbA1c (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-1.29
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-1.51
Sita -> Sita-0.88

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Mean Change From Baseline in Glycosylated Haemoglobin A1c (HbA1c) at Week 78

Calculated as an estimate of the mean change from baseline in glycosylated haemoglobin A1c (HbA1c) at Week 78. (NCT00700817)
Timeframe: Week 0, Week 78

InterventionPercentage point of total HbA1c (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.94
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-1.28

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Mean Change From Baseline in Total Cholesterol at Week 26

Calculated as an estimate of the mean change from baseline in total cholesterol at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.03
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.17
Sita -> Sita-0.02

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Mean Change From Baseline in High-density Lipoprotein-cholesterol (HDL-C) at Week 26

Calculated as an estimate of the mean change from baseline in high-density lipoprotein-cholesterol (HDL-C) at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg0.00
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg0.00
Sita -> Sita0.00

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Mean Change From Baseline in High-density Lipoprotein-cholesterol (HDL-C) at Week 52

Calculated as an estimate of the mean change from baseline in high-density lipoprotein-cholesterol (HDL-C) at Week 52. (NCT00700817)
Timeframe: Week 0, Week 52

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg0.01
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg0.02
Sita -> Sita0.01

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Mean Change From Baseline in Highly Sensitive C-reactive Protein (hsCRP) at Week 26

Calculated as an estimate of the mean change from baseline in highly sensitive C-reactive protein (hsCRP) at week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionmg/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-1.02
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.99
Sita -> Sita-0.66

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Mean Change From Baseline in Interleukin-6 (IL-6) at Week 26.

Calculated as an estimate of the mean change from baseline in interleukin-6 (IL-6) at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionpg/mL (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-1.70
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg1.71
Sita -> Sita0.91

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Mean Change From Baseline in Low-density Lipoprotein-cholesterol (LDL-C) at Week 26

Calculated as an estimate of the mean change in low-density lipoprotein-cholesterol (LDL-C) at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg0.08
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg0.05
Sita -> Sita0.13

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Mean Change From Baseline in Low-density Lipoprotein-cholesterol (LDL-C) at Week 52

Calculated as an estimate of the mean change in low-density lipoprotein-cholesterol (LDL-C) at Week 52. (NCT00700817)
Timeframe: Week 0, Week 52

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg0.09
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg0.09
Sita -> Sita0.17

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Mean Change From Baseline in N-terminal Pro B-type Natriuretic Peptide (NT-proBNP) at Week 26.

Calculated as an estimate of the mean change from baseline in N-terminal pro B-type Natriuretic Peptide (NT-proBNP) at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionpmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg5.19
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg3.74
Sita -> Sita3.71

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Mean Change From Baseline in Overall Treatment Satisfaction (OTS) at Week 26

The Overall Treatment Satisfaction is a sum of 6 items from the Diabetes Treatment Satisfaction Questionnaire, which is a self-assessment of treatment satisfaction. The scale of each sub-item goes from 0 (lowest satisfaction) to 6 (highest satisfaction) and the overall scale of OTS therefore goes from 0 to 36. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionscores on a scale (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg3.51
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg4.35
Sita -> Sita2.96

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Mean Change From Baseline in Overall Treatment Satisfaction (OTS) at Week 52

The Overall Treatment Satisfaction is a sum of 6 items from the Diabetes Treatment Satisfaction Questionnaire, which is a self-assessment of treatment satisfaction. The scale of each sub-item goes from 0 (lowest satisfaction) to 6 (highest satisfaction) and the overall scale of OTS therefore goes from 0 to 36. (NCT00700817)
Timeframe: Week 0, Week 52

Interventionscores on a scale (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg3.32
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg4.31
Sita -> Sita2.96

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Mean Change From Baseline in Diastolic Blood Pressure (DBP) at Week 26

Calculated as an estimate of the mean change from baseline in diastolic blood pressure (DBP) at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

InterventionmmHg (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.71
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg0.07
Sita -> Sita-1.78

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Mean Change From Baseline in Body Weight at Week 52

Calculated as an estimate of the mean change from baseline in body weight at Week 52. (NCT00700817)
Timeframe: Week 0, Week 52

Interventionkg (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-2.78
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-3.68
Sita -> Sita-1.16

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Mean Change From Baseline in Body Weight at Week 26

Calculated as an estimate of the mean change from baseline in body weight at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionkg (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-2.86
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-3.38
Sita -> Sita-0.96

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Mean Change From Baseline in Beta-cell Function at Week 52

"Calculated as an estimate of the mean change from baseline in beta-cell function at Week 52.~Derived from fasting plasma glucose (FPG) and fasting insulin using the homeostatic model assessment (HOMA) method with the assumption that normal-weight subjects aged under 35 years have a 100% beta-cell function (HOMA-B)." (NCT00700817)
Timeframe: Week 0, Week 52

Interventionpercentage point (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg22.58
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg25.76
Sita -> Sita3.98

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Mean Change From Baseline in Beta-cell Function at Week 26

"Calculated as an estimate of the mean change from baseline in beta-cell function at Week 26.~Derived from fasting plasma glucose (FPG) and fasting insulin using the homeostatic model assessment (HOMA) method with the assumption that normal-weight subjects aged under 35 years have a 100% beta-cell function (HOMA-B)." (NCT00700817)
Timeframe: Week 0, Week 26

Interventionpercentage point (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg27.23
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg28.70
Sita -> Sita4.18

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Mean Change From Baseline in Apolipoprotein B at Week 52

Calculated as an estimate of the change from baseline in apolipoprotein B (ApoB) at Week 52. (NCT00700817)
Timeframe: Week 0, Week 52

Interventiong/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.03
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.03
Sita -> Sita-0.03

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Mean Change From Baseline in Plasminogen Activator Inhibitor-1 (PAI-1) at Week 26.

Calculated as an estimate of the mean change from baseline in plasminogen activator inhibitor-1 (PAI-1) at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

InterventionU/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-833
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-561
Sita -> Sita586

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Mean Change From Baseline in Pulse at Week 26

Calculated as an estimate of the mean change from baseline in pulse at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionbeats/minute (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg2.32
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg3.94
Sita -> Sita-0.64

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Mean Change From Baseline in Pulse at Week 52

Calculated as an estimate of the mean change from baseline in pulse at Week 52. (NCT00700817)
Timeframe: Week 0, Week 52

InterventionmmHg (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg1.72
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg3.09
Sita -> Sita0.09

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Mean Change From Baseline in Apolipoprotein B at Week 26

Calculated as an estimate of the change from baseline in apolipoprotein B (ApoB) at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventiong/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.06
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.07
Sita -> Sita-0.05

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Mean Change From Baseline in Systolic Blood Pressure (SBP) at Week 26

Calculated as an estimate of the mean change from baseline in Systolic Blood Pressure (SBP) at Week 26 (NCT00700817)
Timeframe: Week 0, Week 26

InterventionmmHg (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.55
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.72
Sita -> Sita-0.94

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Mean Change From Baseline in Systolic Blood Pressure (SBP) at Week 52

Calculated as an estimate of the mean change from baseline in systolic blood pressure (SBP) at Week 52. (NCT00700817)
Timeframe: Week 0, Week 52

InterventionmmHg (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.37
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-2.55
Sita -> Sita-1.03

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Mean Change From Baseline in Adiponectin at Week 26.

Calculated as an estimate of the mean change from baseline in Adiponectin at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionmcg/mL (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg1.69
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg1.51
Sita -> Sita1.35

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Hypoglyceamic Episodes, Weeks 0-78

Number of hypoglycaemic episodes from Week 0 to Week 78, defined as major, minor, or symptoms only. Major if unable to treat her/himself. Minor if able to treat her/himself and plasma glucose below 3.1 mmol/L. Symptoms only if able to treat her/himself and no plasma glucose measurement or plasma glucose higher than or equal to 3.1 mmol/L. (NCT00700817)
Timeframe: Weeks 0-78

,,
Interventionepisodes (Number)
MajorMinorSymptoms onlyUnclassified
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg236180
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg056401
Sita -> Sita034130

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Hypoglyceamic Episodes, Weeks 0-52

Number of hypoglycaemic episodes from Week 0 to Week 52, defined as major, minor, or symptoms only. Major if unable to treat her/himself. Minor if able to treat her/himself and plasma glucose below 3.1 mmol/L. Symptoms only if able to treat her/himself and no plasma glucose measurement or plasma glucose higher than or equal to 3.1 mmol/L. (NCT00700817)
Timeframe: Weeks 0-52

,,
Interventionepisodes (Number)
MajorMinorSymptoms onlyUnclassified
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg124140
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg051291
Sita -> Sita025120

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Hypoglyceamic Episodes, Weeks 0-26

Number of hypoglycaemic episodes from Week 0 to Week 26, defined as major, minor, or symptoms only. Major if unable to treat her/himself. Minor if able to treat her/himself and plasma glucose below 3.1 mmol/L. Symptoms only if able to treat her/himself and no plasma glucose measurement or plasma glucose higher than or equal to 3.1 mmol/L. (NCT00700817)
Timeframe: Weeks 0-26

,,
Interventionepisodes (Number)
MajorMinorSymptoms onlyUnclassified
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg117120
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg037151
Sita -> Sita011100

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Hypoglycaemic Episodes (Excluding Outlier Subject), Weeks 0-78

Number of hypoglycaemic episodes from Week 0 to Week 78, defined as major, minor, or symptoms only. Major if unable to treat her/himself. Minor if able to treat her/himself and plasma glucose below 3.1 mmol/L. Symptoms only if able to treat her/himself and no plasma glucose measurement or plasma glucose higher than or equal to 3.1 mmol/L. (NCT00700817)
Timeframe: Weeks 0-78

,,
Interventionepisodes (Number)
MajorMinorSymptoms onlyUnclassified
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg236180
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg033401
Sita -> Sita034130

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Hypoglycaemic Episodes (Excluding Outlier Subject), Weeks 0-52

Number of hypoglycaemic episodes from Week 0 to Week 52, defined as major, minor, or symptoms only. Major if unable to treat her/himself. Minor if able to treat her/himself and plasma glucose below 3.1 mmol/L. Symptoms only if able to treat her/himself and no plasma glucose measurement or plasma glucose higher than or equal to 3.1 mmol/L. (NCT00700817)
Timeframe: Weeks 0-52

,,
Interventionepisodes (Number)
MajorMinorSymptoms onlyUnclassified
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg124140
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg028291
Sita -> Sita025120

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Hypoglycaemic Episodes (Excluding Outlier Subject), Weeks 0-26

Number of hypoglycaemic episodes from Week 0 to Week 26, defined as major, minor, or symptoms only. Major if unable to treat her/himself. Minor if able to treat her/himself and plasma glucose below 3.1 mmol/L. Symptoms only if able to treat her/himself and no plasma glucose measurement or plasma glucose higher than or equal to 3.1 mmol/L. (NCT00700817)
Timeframe: Weeks 0-26

,,
Interventionepisodes (Number)
MajorMinorSymptoms onlyUnclassified
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg117120
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg016151
Sita -> Sita011100

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Hypoglycaamic Episodes, Weeks 52-78

Number of hypoglycaemic episodes from Week 52 to Week 78, defined as major, minor, or symptoms only. Major if unable to treat her/himself. Minor if able to treat her/himself and plasma glucose below 3.1 mmol/L. Symptoms only if able to treat her/himself and no plasma glucose measurement or plasma glucose higher than or equal to 3.1 mmol/L. (NCT00700817)
Timeframe: Week 52-78

,,,
Interventionepisodes (Number)
MajorMinorSymptoms onlyUnclassified
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg11230
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg05110
Sita -> Sita -> Lira 1.2 mg0310
Sita -> Sita -> Lira 1.8 mg0600

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Percentage of Subjects Achieving Treatment Target of HbA1c =< 6.5% at Week 78

Calculated as an estimate of the percentage of subjects achieving treatment target of HbA1c =< 6.5% at Week 78. Based on the FAS. (NCT00700817)
Timeframe: Week 0, Week 78

Interventionpercentage of subjects (Number)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg12
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg27

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Percentage of Subjects Achieving Treatment Target of HbA1c =< 6.5% at Week 78

Calculated as an estimate of the percentage of subjects achieving treatment target of HbA1c =< 6.5% at Week 78. Based on the extension 2 FAS. (NCT00700817)
Timeframe: Week 0, Week 78

Interventionpercentage of subjects (Number)
Sita -> Sita -> Lira 1.2 mg29
Sita -> Sita -> Lira 1.8 mg25

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Percentage of Subjects Achieving Treatment Target of HbA1c =< 6.5% at Week 52

Calculated as an estimate of the percentage of subjects achieving treatment target of HbA1c =< 6.5% at Week 52 (NCT00700817)
Timeframe: Week 0, Week 52

Interventionpercentage of subjects (Number)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg24
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg40
Sita -> Sita17

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Percentage of Subjects Achieving Treatment Target of HbA1c =< 6.5% at Week 26

Calculated as the percentage of subjects achieving treatment target of HbA1c =< 6.5% at Week 26 (NCT00700817)
Timeframe: Week 0, Week 26

Interventionpercentage of subjects (Number)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg23
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg36
Sita -> Sita12

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Percentage of Subjects Achieving Treatment Target of HbA1c < 7.0% at Week 78

Calculated as an estimate of the percentage of subjects achieving treatment target of HbA1c < 7.0% at Week 78. Based on the FAS. (NCT00700817)
Timeframe: Week 0, Week 78

Interventionpercentage of subjects (Number)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg35
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg51

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Mean Change in Low-density Lipoprotein-cholesterol (LDL-C) From Week 52 to Week 78

Mean change in low-density lipoprotein-cholesterol (LDL-C) from week 52 to Week 78. (NCT00700817)
Timeframe: Week 52, Week 78

Interventionmmol/L (Mean)
Sita -> Sita -> Lira 1.2 mg-0.22
Sita -> Sita -> Lira 1.8 mg-0.25

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Percentage of Subjects Achieving Treatment Target of HbA1c < 7.0% at Week 52

Calculated as an estimate of the percentage of subjects achieving treatment target of HbA1c < 7.0% at Week 52 (NCT00700817)
Timeframe: Week 0, Week 52

Interventionpercentage of subjects (Number)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg50
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg63
Sita -> Sita27

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Percentage of Subjects Achieving Treatment Target of HbA1c < 7.0% at Week 26

Calculated as the percentage of subjects achieving treatment target of HbA1c < 7.0% at Week 26 (NCT00700817)
Timeframe: Week 0, Week 26

Interventionpercentage of subjects (Number)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg43
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg55
Sita -> Sita22

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Mean Change From Baseline in Fasting Plasma Glucose (FPG) at Week 52

Calculated as an estimate of the mean change from baseline in fasting plasma glucose (FPG) at Week 52. (NCT00700817)
Timeframe: Week 0, Week 52

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-1.71
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-2.04
Sita -> Sita-0.59

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Mean Change in Waist to Hip Ratio From Week 52 to Week 78

Mean change in Waist to Hip Ratio from Week 52 to Week 78. The measure is assessed as the circumference of the waist divided by the circumference of the hip. (NCT00700817)
Timeframe: Week 52, Week 78

Interventioncm/cm (Mean)
Sita -> Sita -> Lira 1.2 mg-0.01
Sita -> Sita -> Lira 1.8 mg-0.00

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Mean Change in Waist Circumference From Week 52 to Week 78

Mean change in Waist Circumference from Week 52 to Week 78. (NCT00700817)
Timeframe: Week 52, Week 78

Interventionkg (Mean)
Sita -> Sita -> Lira 1.2 mg-1.33
Sita -> Sita -> Lira 1.8 mg-2.05

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Mean Change in Very Low-density Lipoprotein-cholesterol (VLDL-C) at Week 52 to Week 78

Mean change in very low-density lipoprotein-cholesterol (VLDL-C) from Week 52 to Week 78. (NCT00700817)
Timeframe: Week 52, Week 78

Interventionmmol/L (Mean)
Sita -> Sita -> Lira 1.2 mg0.03
Sita -> Sita -> Lira 1.8 mg0.02

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Mean Change in Triglycerides (TG) From Week 52 to Week 78

Mean change in triglycerides (TG) from Week 52 to Week 78. (NCT00700817)
Timeframe: Week 52, Week 78

Interventionmmol/L (Mean)
Sita -> Sita -> Lira 1.2 mg-0.20
Sita -> Sita -> Lira 1.8 mg-0.26

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Mean Change in Total Cholesterol From Week 52 to Week 78

Mean change in total cholesterol from Week 52 to Week 78 (NCT00700817)
Timeframe: Week 52, Week 78

Interventionmmol/L (Mean)
Sita -> Sita -> Lira 1.2 mg-0.16
Sita -> Sita -> Lira 1.8 mg-0.24

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Mean Change in Systolic Blood Pressure (SBP) From Week 52 to Week 78

Mean change in systolic blood pressure (SBP) from Week 52 to Week 78. (NCT00700817)
Timeframe: Week 52, Week 78

InterventionmmHg (Mean)
Sita -> Sita -> Lira 1.2 mg-2.12
Sita -> Sita -> Lira 1.8 mg0.35

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Mean Change in Pulse From Week 52 to Week 78

Mean change in pulse from Week 52 to Week 78. (NCT00700817)
Timeframe: Week 52, Week 78

Interventionbeats/minute (Mean)
Sita -> Sita -> Lira 1.2 mg0.90
Sita -> Sita -> Lira 1.8 mg2.19

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Mean Change in Overall Treatment Satisfaction (OTS) From Week 52 to Week 78

The Overall Treatment Satisfaction is a sum of 6 items from the Diabetes Treatment Satisfaction Questionnaire, which is a self-assessment of treatment satisfaction. The scale of each sub-item goes from 0 (lowest satisfaction) to 6 (highest satisfaction) and the overall scale of OTS therefore goes from 0 to 36. (NCT00700817)
Timeframe: Week 52, Week 78

Interventionscores on a scale (Mean)
Sita -> Sita -> Lira 1.2 mg1.48
Sita -> Sita -> Lira 1.8 mg0.98

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Mean Change in High-density Lipoprotein-cholesterol (HDL-C) From Week 52 to Week 78

Mean change in high-density lipoprotein-cholesterol (HDL-C) from Week 52 to Week 78. (NCT00700817)
Timeframe: Week 52, Week 78

Interventionmmol/L (Mean)
Sita -> Sita -> Lira 1.2 mg0.02
Sita -> Sita -> Lira 1.8 mg-0.01

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Mean Change in Glycosylated Haemoglobin A1c (HbA1c) From Week 52 to Week 78

Mean Change in Glycosylated Haemoglobin A1c (HbA1c) from Week 52 to Week 78 (NCT00700817)
Timeframe: Week 52, Week 78

InterventionPercentage point of total HbA1c (Mean)
Sita -> Sita -> Lira 1.2 mg-0.24
Sita -> Sita -> Lira 1.8 mg-0.45

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Mean Change in Free Fatty Acids (FFA) From Week 52 to Week 78

Mean change in free fatty acids (FFA) from Week 52 to Week 78. (NCT00700817)
Timeframe: Week 52, Week 78

Interventionmmol/L (Mean)
Sita -> Sita -> Lira 1.2 mg0.02
Sita -> Sita -> Lira 1.8 mg-0.01

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Mean Change in Fasting Plasma Glucose (FPG) From Week 52 to Week 78

Mean change in fasting plasma glucose (FPG) Week 52 to Week 78. (NCT00700817)
Timeframe: Week 52, Week 78

Interventionmmol/L (Mean)
Sita -> Sita -> Lira 1.2 mg-0.84
Sita -> Sita -> Lira 1.8 mg-1.42

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Mean Change in Diastolic Blood Pressure (DBP) From Week 52 to Week 78

Mean change in diastolic blood pressure (DBP) from Week 52 to Week 78. (NCT00700817)
Timeframe: Week 52, Week 78

InterventionmmHg (Mean)
Sita -> Sita -> Lira 1.2 mg-0.60
Sita -> Sita -> Lira 1.8 mg0.03

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Mean Change in Body Weight From Week 52 to Week 78

Mean change in body weight from Week 52 to Week 78. (NCT00700817)
Timeframe: Week 52, Week 78

Interventionkg (Mean)
Sita -> Sita -> Lira 1.2 mg-1.64
Sita -> Sita -> Lira 1.8 mg-2.48

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Mean Change in Beta-cell Function From Week 52 to Week 78

Mean change in beta-cell function from Week 52 to Week 78. Derived from fasting plasma glucose (FPG) and fasting insulin using the homeostatic model assessment (HOMA) method with the assumption that normal-weight subjects aged under 35 years have a 100% beta-cell function (HOMA-B). (NCT00700817)
Timeframe: Week 52, Week 78

Interventionpercentage point (Mean)
Sita -> Sita -> Lira 1.2 mg13.31
Sita -> Sita -> Lira 1.8 mg23.09

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Mean Change in Apolipoprotein B From Week 52 to Week 78

Mean change in apolipoprotein B (ApoB) from Week 52 to Week 78. (NCT00700817)
Timeframe: Week 52, Week 78

Interventionmmol/L (Mean)
Sita -> Sita -> Lira 1.2 mg0.23
Sita -> Sita -> Lira 1.8 mg0.17

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Mean Change From Baseline in Waist to Hip Ratio at Week 52

Calculated as an estimate of the mean change from baseline in Waist to Hip Ratio at Week 52. The measure is assessed as the circumference of the waist divided by the circumference of the hip. (NCT00700817)
Timeframe: Week 0, Week 52

Interventioncm/cm (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.00
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.01
Sita -> Sita-0.00

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Mean Change From Baseline in Waist to Hip Ratio at Week 26.

Calculated as an estimate of the mean change from baseline in Waist to Hip Ratio at Week 26. The measure is assessed as the circumference of the waist divided by the circumference of the hip. (NCT00700817)
Timeframe: Week 0, Week 26

Interventioncm/cm (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.01
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.01
Sita -> Sita-0.00

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Mean Change From Baseline in Waist Circumference at Week 52

Calculated as an estimate of the mean change from baseline in Waist Circumference at Week 52. (NCT00700817)
Timeframe: Week 0, Week 52

Interventionparticipants (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-2.36
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-3.02
Sita -> Sita-1.23

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Mean Change From Baseline in Waist Circumference at Week 26.

Calculated as an estimate of the mean change from baseline in Waist Circumference at Week 26 (NCT00700817)
Timeframe: Week 0, Week 26

Interventioncm (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-2.69
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-2.63
Sita -> Sita-1.12

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Mean Change From Baseline in Von Willebrand Factor (vWf) at Week 26.

Calculated as an estimate of the mean change from baseline in von Willebrand Factor (vWf) at Week 26. vWf is a blood glycoprotein involved in haemostasis. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionpercentage point (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-1.73
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-4.34
Sita -> Sita-1.8

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Mean Change From Baseline in Very Low-density Lipoprotein-cholesterol (VLDL-C) at Week 52

Calculated as an estimate of the change from baseline in very low-density lipoprotein-cholesterol (VLDL-C) at Week 52. (NCT00700817)
Timeframe: Week 0, Week 52

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.11
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.19
Sita -> Sita-0.15

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Mean Change From Baseline in Very Low-density Lipoprotein-cholesterol (VLDL-C) at Week 26

Calculated as an estimate of the change from baseline in very low-density lipoprotein-cholesterol (VLDL-C) at Week 26. (NCT00700817)
Timeframe: Week 0, Week 26

Interventionmmol/L (Least Squares Mean)
Lira 1.2 mg -> Lira 1.2 mg -> Lira 1.2 mg-0.11
Lira 1.8 mg -> Lira 1.8 mg -> Lira 1.8 mg-0.20
Sita -> Sita-0.15

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Change From Baseline in HbA1c at Week 30

Patient-level HbA1c is measured as a percent. Thus, this change from baseline reflects the Week 30 HbA1c percent minus the Week 0 HbA1c percent. (NCT00701090)
Timeframe: Week 0 to Week 30

InterventionPercent (Least Squares Mean)
Sitagliptin-0.47
Glimepiride-0.54

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Change From Baseline in FPG (Fasting Plasma Glucose) at Week 30

Change from baseline at Week 30 was defined as Week 30 minus Week 0. (NCT00701090)
Timeframe: Week 0 to Week 30

Interventionmg/dL (Least Squares Mean)
Sitagliptin-14.6
Glimepiride-17.5

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Change From Baseline in Body Weight at Week 30

Change from baseline at Week 30 was defined as Week 30 minus Week 0. (NCT00701090)
Timeframe: Week 0 to Week 30

InterventionKilograms (Least Squares Mean)
Sitagliptin-0.8
Glimepiride1.2

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Percent of Patients With at Least One Hypoglycemia Episode of Any Type at Week 30

(NCT00701090)
Timeframe: Week 0 to Week 30

InterventionPercentage of Participants (Number)
Sitagliptin7.0
Glimepiride22.0

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Percent of Patients With A1C <7.0% at Week 30

(NCT00701090)
Timeframe: Week 30

InterventionPercentage of Participants (Number)
Sitagliptin52.4
Glimepiride59.6

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Percent of Patients With A1C <6.5% at Week 30

(NCT00701090)
Timeframe: Week 30

InterventionPercentage of Participants (Number)
Sitagliptin21.2
Glimepiride27.5

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Change From Baseline in Glucose 5-Hour Incremental AUC at Week 6

Participants underwent the 5-hour meal test prior to randomization (baseline) and was repeated at the conclusion of the 6-week double-blind study period. The change from baseline in Glucose 5-Hour Incremental AUC at Week 6 is computed as the difference between the Week 6 measurement and the baseline measurement. (NCT00704132)
Timeframe: Baseline and Week 6

Interventionmg*hr/dL (Least Squares Mean)
Sitagliptin-83.9
Placebo27.0

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Weighted Mean Glucose (WMG) Change From Baseline at Day 28

The change from baseline reflects the day 28 WMG value minus the baseline WMG value. Means are treatment adjusted for baseline HbA1c, previous anti-diabetic medication, and baseline WMG. (NCT00716092)
Timeframe: Baseline and day 28

Interventionmg/dL (Mean)
Placebo0.1
BI1356-19.8
Sitagliptin-26.1

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Fasting Plasma Glucose (FPG) Change From Baseline at Day 28

The change from baseline reflects the day 28 FPG value minus the baseline FPG value. Means are treatment adjusted for baseline HbA1c, previous anti-diabetic medication and baseline FPG. (NCT00716092)
Timeframe: Baseline and day 28

Interventionmg/dL (Mean)
Placebo-0.1
BI1356-10.9
Sitagliptin-15.6

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Exploratory Sensitivity Analysis of the WMG Change From Baseline at Day 28

The change from baseline reflects the day 28 WMG value minus the baseline WMG value. Means are treatment adjusted for baseline HbA1c, previous anti-diabetic medication and baseline WMG. (NCT00716092)
Timeframe: Baseline and day 28

Interventionmg/dL (Mean)
Placebo-0.2
BI1356-20.1
Sitagliptin-26.1

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Exploratory Sensitivity Analysis of Plasma Glucose AUEC (0-3h) Change From Baseline at Day 28

The change from baseline reflects the day 28 FPG value minus the baseline FPG value. Means are treatment adjusted for baseline HbA1c, previous anti-diabetic medication and baseline FPG. (NCT00716092)
Timeframe: Baseline and day 28

Interventionmg*h/dL (Mean)
Placebo9.8
BI1356-96.4
Sitagliptin-119.1

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Exploratory Sensitivity Analysis of GLP-1 AUEC (0-2h) Change From Baseline at Day 28

The change from baseline reflects the day 28 GLP-1 AUEC (0-2h) value minus the baseline GLP-1 AUEC (0-2h) value. Means are treatment adjusted for baseline HbA1c, previous anti-diabetic medication and baseline GLP-1. (NCT00716092)
Timeframe: Baseline and day 28

Interventionpmol*h/L (Mean)
Placebo-0.1
BI135618.1
Sitagliptin15.3

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Plasma Glucose Area Under Effect Curve (AUEC) (0-3h) Change From Baseline at Day 28

The change from baseline reflects the day 28 Glucose AUEC (0-3h) value minus the baseline Glucose AUEC (0-3h) value. Means are treatment adjusted for baseline HbA1c, previous anti-diabetic medication and baseline plasma glucose AUEC (0-3h). (NCT00716092)
Timeframe: Baseline and day 28

Interventionmg*h/dL (Mean)
Placebo8.1
BI1356-98.4
Sitagliptin-119.1

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Exploratory Sensitivity Analysis of FPG Change From Baseline at Day 28

The change from baseline reflects the day 28 FPG value minus the baseline FPG value. Means are treatment adjusted for baseline HbA1c, previous anti-diabetic medication and baseline FPG. (NCT00716092)
Timeframe: Baseline and day 28

Interventionmg/dL (Mean)
Placebo0.4
BI1356-10.3
Sitagliptin-15.6

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GLP-1 (Glucagon Like Peptide 1) AUEC (0-2h) (Area Under Effect Curve) Change From Baseline at Day 28

The change from baseline reflects the day 28 GLP-1 AUEC (0-2h) value minus the baseline GLP-1 AUEC (0-2h) value. Means are treatment adjusted for baseline HbA1c, previous anti-diabetic medication and baseline GLP-1. (NCT00716092)
Timeframe: Baseline and day 28

Interventionpmol*h/L (Mean)
Placebo0.4
BI135618.5
Sitagliptin15.3

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Change From Baseline in 2-Hour PMG at Week 54

PMG was measured using the Meal Tolerance Test (MTT). (NCT00722371)
Timeframe: Baseline and Week 54

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-37.0
Pioglitazone 15 mg-26.7
Pioglitazone 30 mg-46.8
Pioglitazone 45 mg-58.2
Sitagliptin 100 mg/ Pioglitazone 15 mg-64.7
Sitagliptin 100 mg/ Pioglitazone 30 mg-69.7
Sitagliptin 100 mg/ Pioglitazone 45 mg-88.2

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Change From Baseline in 2-Hour Post-meal Glucose (PMG) at Week 24

PMG was measured using the Meal Tolerance Test (MTT). (NCT00722371)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-51.1
Pioglitazone 15 mg-30.6
Pioglitazone 30 mg-52.5
Pioglitazone 45 mg-66.6
Sitagliptin 100 mg/ Pioglitazone 15 mg-69.2
Sitagliptin 100 mg/ Pioglitazone 30 mg-85.5
Sitagliptin 100 mg/ Pioglitazone 45 mg-93.8

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Change From Baseline in A1C at Week 54

A1C represents the percentage of glycosylated hemoglobin. (NCT00722371)
Timeframe: Baseline and Week 54

InterventionPercent of glycosylated hemoglobin (Least Squares Mean)
Sitagliptin 100 mg-0.93
Pioglitazone 15 mg-0.74
Pioglitazone 30 mg-1.16
Pioglitazone 45 mg-1.23
Sitagliptin 100 mg/ Pioglitazone 15 mg-1.45
Sitagliptin 100 mg/ Pioglitazone 30 mg-1.49
Sitagliptin 100 mg/ Pioglitazone 45 mg-1.78

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24

(NCT00722371)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-24.3
Pioglitazone 15 mg-19.5
Pioglitazone 30 mg-29.9
Pioglitazone 45 mg-37.4
Sitagliptin 100 mg/ Pioglitazone 15 mg-41.0
Sitagliptin 100 mg/ Pioglitazone 30 mg-46.9
Sitagliptin 100 mg/ Pioglitazone 45 mg-52.0

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Change From Baseline in FPG at Week 54

(NCT00722371)
Timeframe: Baseline and Week 54

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg-13.1
Pioglitazone 15 mg-10.5
Pioglitazone 30 mg-24.0
Pioglitazone 45 mg-33.3
Sitagliptin 100 mg/ Pioglitazone 15 mg-33.9
Sitagliptin 100 mg/ Pioglitazone 30 mg-37.1
Sitagliptin 100 mg/ Pioglitazone 45 mg-47.8

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Change From Baseline in Hemoglobin A1C (A1C) at Week 24

A1C represents the percentage of glycosylated hemoglobin. (NCT00722371)
Timeframe: Baseline and Week 24

InterventionPercentage of glycosylated hemoglobin (Least Squares Mean)
Sitagliptin 100 mg-1.09
Pioglitazone 15 mg-0.88
Pioglitazone 30 mg-1.21
Pioglitazone 45 mg-1.20
Sitagliptin 100 mg/ Pioglitazone 15 mg-1.53
Sitagliptin 100 mg/ Pioglitazone 30 mg-1.63
Sitagliptin 100 mg/ Pioglitazone 45 mg-1.81

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Percentage of Patients Experiencing Hypoglycemia (Overall)

Percentage of patients experiencing minor hypoglycemia with a confirmed glucose <54mg/dL (NCT00729326)
Timeframe: 4 weeks and 8 weeks

InterventionPercentage of patients (Number)
Exenatide4.3
Sitagliptin1.4

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Percentage of Patients Experiencing Hypoglycemia (Week 4 to Week 8)

Percentage of patients experiencing minor hypoglycemia with a confirmed glucose <54mg/dL (NCT00729326)
Timeframe: 8 weeks

InterventionPercentage of patients (Number)
Exenatide5.7
Sitagliptin0.0

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Change in Postprandial Insulin AUC After the Morning Meal

Change in postprandial insulin AUC after the morning meal (t=0 to 4 hours) (i.e., postprandial insulin AUC after the morning meal at baseline minus postprandial insulin AUC after the morning meal at endpoint) (NCT00729326)
Timeframe: baseline and 8 Weeks

Interventionpmol*hours/L (Least Squares Mean)
Exenatide-396.12
Sitagliptin-8.79

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Change in Postprandial Glucagon AUC Excursion After the Morning Meal

Change in postprandial glucagon AUC excursion after the morning meal (t=0 to 4 hours) (i.e., glucagon AUC excursion for 4 hours following the morning meal at baseline minus glucagon AUC excursion for 4 hours following the morning meal at endpoint) (NCT00729326)
Timeframe: baseline and 8 Weeks

Interventionpmol*hours/L (Least Squares Mean)
Exenatide-30.94
Sitagliptin-14.93

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Change in Postprandial Glucagon Area Under the Concentration-time Curve (AUC) After the Morning Meal

Change in Postprandial Glucagon AUC after the morning meal (t=0 to 4 hours) (i.e., Glucagon AUC over the first 4 hours following the morning meal at baseline minus glucagon AUC over the first 4 hours following the morning meal at endpoint) (NCT00729326)
Timeframe: baseline and 8 Weeks

Interventionpmol*hours/L (Least Squares Mean)
Exenatide-29.60
Sitagliptin-16.91

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Change in Postprandial C-peptide AUC Excursion After the Morning Meal

Change in Postprandial C-peptide AUC excursion after the morning meal (t=0 to 4 hours) (i.e., postprandial C-peptide AUC excursion after the morning meal at baseline minus postprandial C-peptide AUC excursion after the morning meal at endpoint) (NCT00729326)
Timeframe: baseline and 8 Weeks

Interventionnmol*hours/L (Least Squares Mean)
Exenatide-2.83
Sitagliptin0.14

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Change in Postprandial C-peptide AUC After the Morning Meal

Change in postprandial C-peptide AUC after the morning meal (t=0 to 4 hours) (i.e., postprandial C-peptide AUC after the morning meal at baseline minus postprandial C-peptide AUC after the morning meal at endpoint) (NCT00729326)
Timeframe: baseline and 8 Weeks

Interventionnmol*hours/L (Least Squares Mean)
Exenatide-1.78
Sitagliptin0.25

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Change in Postprandial Active GLP-1 AUC Excursion After the Monrning Meal

Change in Postprandial active GLP-1 AUC excursion after the morning meal (t=0 to 4 hours) (i.e., postprandial active GLP-1 AUC excursion after the morning meal at baseline minus postprandial active GLP-1 AUC excursion after the morning meals at endpoint) (NCT00729326)
Timeframe: baseline and 8 Weeks

Interventionpmol*hours/L (Least Squares Mean)
Exenatide-14.04
Sitagliptin23.53

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Change in Postprandial Active GLP-1 AUC After the Morning Meal

Change in Postprandial active GLP-1 AUC after the morning meal (t=0 to 4 hours) (i.e., postprandial active GLP-1 AUC after the morning meal at baseline minus postprandial active GLP-1 AUC after the morning meal at endpoint) (NCT00729326)
Timeframe: baseline and 8 Weeks

Interventionpmol*hours/L (Least Squares Mean)
Exenatide-14.28
Sitagliptin47.37

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Change in Postprandial Insulin AUC Excursion After the Morning Meal

Change in Postprandial insulin AUC excursion after the morning meal (t=0 to 4 hours) (i.e., postprandial insulin AUC excursion after the morning meal at baseline minus postprandial insulin AUC excursion after the morning meal at endpoint) (NCT00729326)
Timeframe: baseline and 8 Weeks

Interventionpmol*hours/L (Least Squares Mean)
Exenatide-525.01
Sitagliptin-34.83

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Change in Postprandial Triglyceride AUC After the Morning Meal

Change in postprandial triglyceride AUC after the morning meal (t=0 to 4 hours) (i.e., postprandial triglyceride AUC after the morning meal at baseline minus postprandial triglyceride AUC after the morning meal at endpoint) (NCT00729326)
Timeframe: baseline and 8 Weeks

Interventionmg*hours/dL (Least Squares Mean)
Exenatide0.83
Sitagliptin0.87

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Change in Postprandial Triglyceride AUC Excursion After the Morning Meal

Change in postprandial triglyceride AUC excursion after the morning meal (t=0 to 4 hours) (i.e., postprandial triglyceride AUC excursion after the morning meal at baseline minus postprandial triglyceride AUC excursion after the morning meal at endpoint) (NCT00729326)
Timeframe: baseline and 8 Weeks

Interventionmg*hours/dL (Least Squares Mean)
Exenatide-108.16
Sitagliptin-41.39

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Change in Time-averaged Glucose During a 24 Hour Period

Change in time-averaged glucose during a 24-hour period from baseline to endpoint (i.e., time-averaged glucose over 24 hours at endpoint minus time-averaged glucose over 24 hours at baseline). (NCT00729326)
Timeframe: baseline and 8 Weeks

Interventionmg/dL (Least Squares Mean)
Exenatide-41.65
Sitagliptin-29.56

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Change in Two-hour Postprandial Glucose After the Morning Meal

Change in 2 hour post-prandial glucose after the morning meal from baseline to endpoint (i.e., glucose level 2 hours after the morning meal at baseline minus glucose level 2 hours after the morning meal at endpoint) (NCT00729326)
Timeframe: baseline and 8 Weeks

Interventionmg/dL (Least Squares Mean)
Exenatide-108.35
Sitagliptin-44.43

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Episodes of Hypoglycemia (Baseline to Week 4)

Number of episodes of hypoglycemia experienced during the first 4 weeks of the study (NCT00729326)
Timeframe: 4 weeks

Interventionepisodes of hypoglycemia (Number)
Exenatide1
Sitagliptin1

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Episodes of Hypoglycemia (Overall)

Number of episodes of hypoglycemia experienced overall during the study (NCT00729326)
Timeframe: 4 weeks and 8 weeks

Interventionepisodes of hypoglycemia (Number)
Exenatide3
Sitagliptin1

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Episodes of Hypoglycemia (Week 4 to Week 8)

Number of episodes of hypoglycemia experienced between week 4 and week 8 of the study (NCT00729326)
Timeframe: 8 weeks

Interventionepisodes of hypoglycemia (Number)
Exenatide2
Sitagliptin0

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Percentage of Patients Experiencing Hypoglycemia (Baseline to Week 4)

Percentage of patients experiencing minor hypoglycemia with a confirmed glucose <54mg/dL (NCT00729326)
Timeframe: 4 Weeks

InterventionPercentage of patients (Number)
Exenatide2.9
Sitagliptin2.7

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Change in Fasting Blood Glucose After the Morning Meal

Change in fasting blood glucose after the morning meal from baseline to endpoint (i.e., fasting blood glucose after the morning meal at baseline minus fasting blood glucose after the morning meal at endpoint) (NCT00729326)
Timeframe: baseline and 8 Weeks

Interventionmg/dL (Least Squares Mean)
Exenatide-28.93
Sitagliptin-28.22

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Number of Participants Who Experienced at Least One Adverse Event

(NCT00730275)
Timeframe: Pre-study through 10 to 14 days following administration of study drug

Interventionparticipants (Number)
Sitagliptin 50 mg3
Sitagliptin 100 mg1
Sitagliptin 200 mg1
Placebo2

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Time of Occurence of Maximum Concentration (Tmax) Following a Single Dose of Sitagliptin

Serum samples were used to determine the Tmax for sitagliptin. The placebo group is not included in the table below; this outcome measure only evaluated the sitagliptin groups. (NCT00730275)
Timeframe: Pre-dose through 72 hours post-dose

Interventionhours (Median)
Sitagliptin 50 mg3.0
Sitagliptin 100 mg3.0
Sitagliptin 200 mg2.5

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Plasma Dipeptidyl Peptidase-4 (DPP-4) Activity Following a Single Dose of Sitagliptin or Placebo

"Plasma DPP-4 activity was analyzed using the 24-hour weighted average inhibition (WAI) and percent inhibition at 24 hours post-dose.~WAI was defined as the AUC of inhibition divided by the length of the post-dose time interval. Positive values of WAI represent a decrease in DPP-4 activity." (NCT00730275)
Timeframe: Pre-dose through 24 hours post-dose

,,,
InterventionPercent inhibition (Least Squares Mean)
24-hour WAI of DPP-4 activityDDP-4 activity at 24 hours post-dose
Placebo6.763.57
Sitagliptin 100 mg80.5362.78
Sitagliptin 200 mg87.9675.76
Sitagliptin 50 mg73.9853.98

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Maximum Concentration (Cmax) Following a Single Dose of Sitagliptin

Serum samples were used to determine the Cmax for sitagliptin. The placebo group is not included in the table below; this outcome measure only evaluated the sitagliptin groups. (NCT00730275)
Timeframe: Pre-dose through 72 hours post-dose

InterventionnM (Geometric Mean)
Sitagliptin 50 mg366
Sitagliptin 100 mg666
Sitagliptin 200 mg1876

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Apparent Terminal Half-life (Apparent t1/2) Following a Single Dose of Sitagliptin

Serum samples were used to determine the apparent t1/2 for sitagliptin. The placebo group is not included in the table below; this outcome measure only evaluated the sitagliptin groups. (NCT00730275)
Timeframe: Pre-dose through 72 hours post-dose

Interventionhours (Mean)
Sitagliptin 50 mg12.1
Sitagliptin 100 mg11.2
Sitagliptin 200 mg11.7

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Area Under the Concentration-time Curve (AUC) From Time 0 to Infinity Following a Single Dose of Sitagliptin

Serum samples were used to determine the AUC from time 0 to infinity for sitagliptin. The placebo group is not included in the table below; this outcome measure only evaluated the sitagliptin groups. (NCT00730275)
Timeframe: Pre-dose through 72 hours post-dose

InterventionnM*hour (Geometric Mean)
Sitagliptin 50 mg3438
Sitagliptin 100 mg5869
Sitagliptin 200 mg12965

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Waist Circumference Change From Baseline

Least squares (LS) means of change from baseline were calculated using a mixed-effects model for repeated measures (MMRM) with treatment, country, visit, and treatment-by-visit interaction as fixed effects and baseline as a covariate. (NCT00734474)
Timeframe: Baseline, 26, 52, and 104 weeks

,,,
Interventioncentimeters (cm) (Least Squares Mean)
26 Weeks (n=266, 273, 277, 138)52 Weeks (n=238, 250, 247)104 Weeks (n=192, 189, 188)
0.75 mg LY2189265-1.78-2.05-1.75
1.5 mg LY2189265-2.89-2.91-2.57
Placebo/Sitagliptin (Baseline Through 26 Weeks)-1.20NANA
Sitagliptin-1.45-1.45-1.20

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Participant-reported Outcomes, Impact of Weight on Quality of Life-Lite (IWQoL-Lite)

"The Impact of Weight on Quality of Life-Lite (IWQoL-Lite questionnaire) is an obesity-specific, 31-item questionnaire designed to measure the impact of weight on participants' quality of life. Items are scored on a 5-point numeric rating scale where 5 = always true and 1 = never true. Items are summed into 6 scales (physical function [11 items], self-esteem [7 items], sexual life [4 items], public distress [5 items], work [4 items], and total score [31 items]) based on the average for the valid responses on that scale multiplied by the number of items on that scale (rounded to the nearest whole integer). Higher scores indicate lower levels of functioning (negative effects). Scores are linearly transformed to a 0 to 100 scale." (NCT00734474)
Timeframe: Baseline, 52 weeks, and 104 weeks

,,
Interventionunits on a scale (Mean)
Total Score, Baseline (n=285, 284, 300)Total Score, 52 Weeks (n=237, 252, 247)Total Score, 104 Weeks (n=190, 190, 185)
0.75 mg LY218926582.5586.3187.47
1.5 mg LY218926583.4186.9288.08
Sitagliptin83.9786.2586.93

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Antibodies to LY2189265

The number of participants with postbaseline detection of treatment-emergent antidrug LY2189265 antibodies (ADA) is summarized. (NCT00734474)
Timeframe: Baseline through 104 weeks

Interventionparticipants (Number)
LY21892659

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Change From Baseline in Body Weight at Dose Decision Point

Change from baseline in body weight was 1 of the 4 measures included in the clinical utility index (CUI) used to evaluate the dose decision. The maximum duration of exposure to LY2189265, Sitagliptin, or Placebo (across all treatment arms) at the decision point was 27.4 weeks. (NCT00734474)
Timeframe: Baseline up to 27.4 weeks

Interventionkilograms (kg) (Mean)
3.0 mg LY2189265-3.32
2.0 mg LY2189265-2.15
1.5 mg LY2189265-2.12
1.0 mg LY2189265-2.23
0.75 mg LY2189265-1.17
0.5 mg LY2189265-1.53
0.25 mg LY2189265-0.85
Sitagliptin-0.43
Placebo/Sitagliptin (Baseline Through 26 Weeks)-0.56

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Change From Baseline in Glycosylated Hemoglobin (HbA1c) at the Dose Decision Point

Change from baseline in HbA1c was 1 of the 4 measures included in the clinical utility index (CUI) used to evaluate the dose decision. The maximum duration of exposure to LY2189265, Sitagliptin, or Placebo (across all treatment arms) at the decision point was 27.4 weeks. (NCT00734474)
Timeframe: Baseline up to 27.4 weeks

Interventionpercentage of HbA1c (Mean)
3.0 mg LY2189265-1.09
2.0 mg LY2189265-1.25
1.5 mg LY2189265-1.49
1.0 mg LY2189265-0.98
0.75 mg LY2189265-1.02
0.5 mg LY2189265-0.94
0.25 mg LY2189265-0.70
Sitagliptin-0.76
Placebo/Sitagliptin (Baseline Through 26 Weeks)-0.06

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Change From Baseline in Pulse Rate at Dose Decision Point

Sitting pulse rate was measured at the time that the dose decision was made (dose decision point). Change from baseline in pulse rate was 1 of the 4 measures included in the clinical utility index (CUI) used to evaluate the dose decision. The maximum duration of exposure to LY2189265, Sitagliptin, or Placebo (across all treatment arms) at the decision point was 27.4 weeks. (NCT00734474)
Timeframe: Baseline up to 27.4 weeks

Interventionbeats per minute (bpm) (Mean)
3.0 mg LY21892656.63
2.0 mg LY21892653.43
1.5 mg LY21892652.39
1.0 mg LY21892653.34
0.75 mg LY2189265-1.63
0.5 mg LY21892651.91
0.25 mg LY21892651.05
Sitagliptin-0.16
Placebo/Sitagliptin (Baseline Through 26 Weeks)1.81

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Number of Participants With Adjudicated Pancreatitis at 104 Weeks

The number of participants with pancreatitis confirmed by adjudication is summarized cumulatively. A summary of serious and other non-serious adverse events regardless of causality is located in the Reported Adverse Events module. (NCT00734474)
Timeframe: Baseline through 104 weeks

Interventionparticipants (Number)
3.0 mg LY21892650
2.0 mg LY21892650
1.5 mg LY21892650
1.0 mg LY21892650
0.75 mg LY21892650
0.5 mg LY21892650
0.25 mg LY21892650
Sitagliptin2
Placebo/Sitagliptin (Baseline Through 26 Weeks)0
Placebo/Sitagliptin (26 Weeks Through 104 Weeks)1

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Number of Participants With Treatment-emergent Adverse Events at 104 Weeks

A treatment-emergent adverse event (TEAE) was defined as an event that first occurs or worsens (increases in severity) after baseline regardless of causality or severity. The number of participants with 1 or more TEAEs is summarized cumulatively. A summary of serious and other non-serious adverse events regardless of causality is located in the Reported Adverse Events module. (NCT00734474)
Timeframe: Baseline through 104 weeks

Interventionparticipants (Number)
1.5 mg LY2189265259
0.75 mg LY2189265255
Sitagliptin242

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Number of Participants With Treatment-emergent Adverse Events at 52 Weeks

A treatment-emergent adverse event (TEAE) was defined as an event that first occurs or worsens (increases in severity) after baseline regardless of causality or severity. The number of participants with 1 or more TEAEs is summarized cumulatively. A summary of serious and other non-serious adverse events regardless of causality is located in the Reported Adverse Events module. (NCT00734474)
Timeframe: Baseline through 52 weeks

Interventionparticipants (Number)
3.0 mg LY21892659
2.0 mg LY218926520
1.5 mg LY2189265233
1.0 mg LY21892658
0.75 mg LY2189265231
0.5 mg LY218926515
0.25 mg LY218926510
Sitagliptin219

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Glycosylated Hemoglobin (HbA1c) Change From Baseline

Least squares (LS) means were calculated using analysis of covariance (ANCOVA) and last observation carried forward (LOCF) imputation with country and treatment as fixed effects and baseline HbA1c as a covariate. (NCT00734474)
Timeframe: Baseline, 52 weeks

Interventionpercentage of HbA1c (Least Squares Mean)
1.5 mg LY2189265-1.10
0.75 mg LY2189265-0.87
Sitagliptin-0.39

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Number of Participants With Treatment-emergent Adverse Events at 26 Weeks

A treatment-emergent adverse event (TEAE) was defined as an event that first occurs or worsens (increases in severity) after baseline regardless of causality or severity. The number of participants with 1 or more TEAEs is summarized cumulatively. A summary of serious and other non-serious adverse events regardless of causality is located in the Reported Adverse Events module. (NCT00734474)
Timeframe: Baseline through 26 weeks

Interventionparticipants (Number)
1.5 mg LY2189265208
0.75 mg LY2189265204
Sitagliptin185
Placebo/Sitagliptin (Baseline Through 26 Weeks)111

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Pharmacokinetics of LY2189265: Area Under the Concentration-Time Curve

Pharmacokinetic (PK) parameter estimates from LY2189265 concentration data were obtained using a 2-compartment population PK model with first order absorption. Area under the plasma-concentration curve from 0 to 168 hours, steady state (AUC0-168h, ss) of LY2189265 is summarized. (NCT00734474)
Timeframe: Baseline through 52 weeks

Interventionnanograms times hours per milliliter (Mean)
1.5 mg LY218926513378
0.75 mg LY21892657246

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Beta Cell Function and Insulin Sensitivity (HOMA2)

The homeostatic model assessment (HOMA) is a method used to quantify insulin resistance and beta (β)-cell function. HOMA2-%B is a computer model that uses fasting plasma insulin and glucose concentrations to estimate steady state beta cell function (%B) as a percentage of a normal reference population (normal young adults). HOMA2-%S is a computer model that uses fasting plasma insulin and glucose concentrations to estimate insulin sensitivity (%S), as percentages of a normal reference population (normal young adults). The normal reference population for both HOMA2-%B and HOMA2-%S were set at 100%. Least squares (LS) means of change from baseline of C-peptide based HOMA2-%B and HOMA2-%S were calculated using a mixed-effects model for repeated measures (MMRM) with treatment, country, visit, and treatment-by-visit interaction as fixed effects and baseline as a covariate. (NCT00734474)
Timeframe: Baseline, 26, 52, and 104 weeks

,,,
InterventionHOMA2-% (Least Squares Mean)
HOMA2-%B, 26 Weeks (n=206, 226, 206, 84)HOMA2-%B, 52 Weeks (n=188, 198, 180)HOMA2-%B, 104 Weeks (n=148, 154, 134)HOMA2-%S, 26 Weeks (n=206, 226, 206, 84)HOMA2-%S, 52 Weeks (n=188, 198, 180)HOMA2-%S, 104 Weeks (n=148, 154, 134)
0.75 mg LY218926526.9822.3019.110.782.28-0.12
1.5 mg LY218926532.2833.5730.895.754.693.82
Placebo/Sitagliptin (Baseline Through 26 Weeks)1.60NANA9.82NANA
Sitagliptin10.816.661.472.294.255.61

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Body Weight Change From Baseline

Least squares (LS) means of change from baseline body weight were calculated using analysis of covariance (ANCOVA) and last observation carried forward (LOCF) imputation with country and treatment as fixed effects and baseline as a covariate. (NCT00734474)
Timeframe: Baseline, 26, 52, and 104 weeks

,,,
Interventionkilograms (kg) (Least Squares Mean)
26 Weeks52 Weeks104 Weeks
0.75 mg LY2189265-2.63-2.60-2.39
1.5 mg LY2189265-3.18-3.03-2.88
Placebo/Sitagliptin (Baseline Through 26 Weeks)-1.47NANA
Sitagliptin-1.46-1.53-1.75

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Change From Baseline in Blood Pressure

Sitting and standing systolic blood pressure (SBP) and diastolic blood pressure (DBP) were measured. Least squares (LS) means of change from baseline were calculated using a mixed-effects model for repeated measures (MMRM) with treatment, country, visit, and treatment-by-visit interaction as fixed effects and baseline as a covariate. (NCT00734474)
Timeframe: Baseline, 26 weeks, 104 weeks

,,,
Interventionmillimeters of mercury (mmHg) (Least Squares Mean)
Sitting SBP, 26 Weeks (n=271, 278, 283, 138)Sitting SBP, 104 Weeks (n=197, 192, 191)Sitting DBP, 26 Weeks (n=271, 278, 283, 138)Sitting DBP, 104 Weeks (n=197, 192, 191)Standing SBP, 26 Weeks (n=271, 277, 281, 138)Standing SBP, 104 Weeks (n=197, 192, 191)Standing DBP, 26 Weeks (n=271, 277, 281, 138)Standing DBP, 104 Weeks (n=197, 192, 191)
0.75 mg LY2189265-1.401.28-0.201.40-1.720.170.030.36
1.5 mg LY2189265-1.73-0.07-0.430.38-1.53-1.30-0.11-0.23
Placebo/Sitagliptin (Baseline Through 26 Weeks)1.12NA0.68NA0.26NA-0.52NA
Sitagliptin-1.940.02-1.06-0.36-2.54-1.20-1.36-0.67

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Change From Baseline in Electrocardiogram (ECG) Parameters, Fridericia-corrected QT (QTcF) and PR Interval

The QT interval is a measure of the time between the start of the Q wave and the end of the T wave and was calculated from electrocardiogram (ECG) data using Fridericia's formula: QTc = QT/RR^0.33. Corrected QT (QTc) is the QT interval corrected for heart rate and RR, which is the interval between two R waves. PR is the interval between the P wave and the QRS complex. Least Squares (LS) means of change from baseline were calculated using a mixed-effects model for repeated measures (MMRM) with treatment, country, visit, and treatment-by-visit interaction as fixed effects and baseline as a covariate. (NCT00734474)
Timeframe: Baseline, 26 weeks, 104 weeks

,,,
Interventionmilliseconds (msec) (Least Squares Mean)
PR Interval, 26 Weeks (n=256, 261, 268, 132)PR Interval, 104 Weeks (n=168, 170, 167)QTcF Interval, 26 Weeks (n=258, 262, 268, 132)QTcF Interval, 104 Weeks (n=169, 170, 168)
0.75 mg LY21892651.603.06-2.44-2.49
1.5 mg LY21892652.944.59-3.86-2.71
Placebo/Sitagliptin (Baseline Through 26 Weeks)2.24NA1.76NA
Sitagliptin0.423.19-1.31-0.02

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Change From Baseline in Pulse Rate

Sitting and standing pulse rate were measured. Least squares (LS) means of change from baseline were calculated using a mixed-effects model for repeated measures (MMRM) with treatment, country, visit, and treatment-by-visit interaction as fixed effects and baseline as covariate. (NCT00734474)
Timeframe: Baseline, 26 weeks, 104 weeks

,,,
Interventionbeats per minute (bpm) (Least Squares Mean)
Sitting, 26 Weeks (n=271, 278, 283, 138)Sitting, 104 Weeks (n=197, 192, 191)Standing, 26 Weeks (n=271, 277, 281, 138)Standing, 104 Weeks (n=197, 192, 191)
0.75 mg LY21892651.902.772.002.50
1.5 mg LY21892652.572.283.242.26
Placebo/Sitagliptin (Baseline Through 26 Weeks)-0.22NA-0.17NA
Sitagliptin-0.11-0.78-0.24-1.06

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Durability of Change From Baseline Body Weight

Durability of effect on body weight was assessed by comparing the differences in mean change from baseline in body weight at 1 time point versus an earlier time point. Least squares (LS) means of change from baseline body weight data were calculated using a mixed-effects model for repeated measures (MMRM) analysis with treatment, country, visit, and treatment-by-visit interaction as fixed effects and baseline as a covariate. (NCT00734474)
Timeframe: Baseline, 13, 26, 52, and 104 weeks

,,,
Interventionkilograms (kg) (Least Squares Mean)
26 Weeks Versus 13 Weeks (n=271, 278, 282, 138)52 Weeks Versus 26 Weeks (n=246, 255, 253)104 Weeks Versus 26 Weeks (n=197, 192, 191)
0.75 mg LY2189265-0.570.060.32
1.5 mg LY2189265-0.530.170.42
Placebo/Sitagliptin (Baseline Through 26 Weeks)-0.37NANA
Sitagliptin-0.42-0.04-0.39

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Durability of Change From Baseline in Glycosylated Hemoglobin (HbA1c)

Durability of effect on HbA1c was assessed by comparing the differences in mean change from baseline in HbA1c at 1 time point versus an earlier time point. Least squares (LS) means of change from baseline HbA1c data were calculated using a mixed-effects model for repeated measures (MMRM) analysis with treatment, country, visit, and treatment-by-visit interaction as fixed effects and baseline as a covariate. (NCT00734474)
Timeframe: Baseline, 13, 26, 52, and 104 weeks

,,,
Interventionpercentage of HbA1c (Least Squares Mean)
26 Weeks Versus 13 Weeks (n=269, 269, 276, 136)52 Weeks Versus 26 Weeks (n=245, 254, 250)104 Weeks Versus 52 Weeks (n=194, 191, 190)
0.75 mg LY21892650.020.160.16
1.5 mg LY2189265-0.030.140.13
Placebo/Sitagliptin (Baseline Through 26 Weeks)-0.14NANA
Sitagliptin0.000.240.09

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Fasting Blood Glucose Change From Baseline

Least squares (LS) means of change from baseline were calculated using mixed-effects model for repeated measures (MMRM) with treatment, country, visit, and treatment-by-visit interaction as fixed effects and baseline as a covariate. (NCT00734474)
Timeframe: Baseline, 26, 52, and 104 weeks

,,,
Interventionmillimoles per liter (mmol/L) (Least Squares Mean)
26 Weeks (n=265, 271, 276, 135)52 Weeks (n=239, 247, 244)104 Weeks (n=190, 187, 181)
0.75 mg LY2189265-1.97-1.63-1.39
1.5 mg LY2189265-2.38-2.38-1.99
Placebo/Sitagliptin (Baseline Through 26 Weeks)-0.49NANA
Sitagliptin-0.97-0.90-0.47

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Fasting Insulin Change From Baseline

Least squares (LS) means of change from baseline fasting insulin data were calculated using a mixed-effects model for repeated measures (MMRM) analysis with treatment, country, visit, and treatment-by-visit interaction as fixed effects and baseline as a covariate. (NCT00734474)
Timeframe: Baseline, 26, 52, and 104 weeks

,,,
Interventionpicomoles per liter (pmol/L) (Least Squares Mean)
26 Weeks (n=238, 249, 230, 115)52 Weeks (n=207, 218, 200)104 Weeks (n=187, 200, 183)
0.75 mg LY218926510.1512.9521.56
1.5 mg LY218926511.5910.5711.36
Placebo/Sitagliptin (Baseline Through 26 Weeks)-6.92NANA
Sitagliptin8.484.180.29

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Glycosylated Hemoglobin (HbA1c) Change From Baseline

Least squares (LS) means were calculated using analysis of covariance (ANCOVA) and last observation carried forward (LOCF) imputation with country and treatment as fixed effects and baseline HbA1c as a covariate. (NCT00734474)
Timeframe: Baseline, 26 weeks, 104 weeks

,,,
Interventionpercentage of HbA1c (Least Squares Mean)
26 Weeks104 Weeks
0.75 mg LY2189265-1.01-0.71
1.5 mg LY2189265-1.22-0.99
Placebo/Sitagliptin (Baseline Through 26 Weeks)0.03NA
Sitagliptin-0.61-0.32

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Incidence of Hypoglycemic Episodes

Hypoglycemic episodes (HE) were classified as severe (defined as episodes requiring assistance from another person to actively administer resuscitative actions), documented symptomatic (defined as any time a participant feels that he/she is experiencing symptoms and/or signs associated with hypoglycemia and has a plasma glucose level of ≤3.9 millimoles per liter [mmol/L]), asymptomatic (defined as episodes not accompanied by typical symptoms of hypoglycemia but with a measured plasma glucose of ≤3.9 mmol/L), nocturnal (defined as any episode that occurred between bedtime and waking), or probable symptomatic (defined as episodes during which symptoms of hypoglycemia were not accompanied by a plasma glucose determination). The number of participants with self-reported hypoglycemic events is summarized cumulatively. (NCT00734474)
Timeframe: Baseline through 26 and 104 weeks

,,,
Interventionparticipants (Number)
Severe HE, 26 WeeksSevere HE, 104 WeeksDocumented Symptomatic HE, 26 WeeksDocumented Symptomatic HE, 104 WeeksAsymptomatic HE, 26 WeeksAsymptomatic HE, 104 WeeksNocturnal HE, 26 WeeksNocturnal HE, 104 WeeksProbable HE, 26 WeeksProbable HE, 104 Weeks
0.75 mg LY2189265008195951302
1.5 mg LY21892650017335971456
Placebo/Sitagliptin (Baseline Through 26 Weeks)0NA2NA0NA0NA0NA
Sitagliptin0010180321026

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Number of Participants With Treatment-emergent Abnormal Laboratory Tests at 104 Weeks

The number of participants with treatment-emergent abnormal laboratory results (defined as abnormalities that first occur after baseline) was summarized cumulatively for alkaline phosphatase, alanine aminotransferase or serum glutamic pyruvic transaminase (ALT/SGPT), amylase (pancreatic and total), aspartate aminotransferase or serum glutamic oxaloacetic transaminase (AST/SGOT), basophils, bilirubin (direct and total), calcitonin, chloride, creatine phosphokinase (CPK), creatinine, creatinine clearance, eosinophils, erythrocytes, gamma glutamyltransferase (GGT), hematocrit, hemoglobin, leukocytes, lipase, lymphocytes, mean cell hemoglobin concentration (MCHC), mean cell volume (MCV), monocytes, neutrophils, platelets, potassium, sodium, urea nitrogen, and urine microalbumin-to-creatinine ratio (UMCR). (NCT00734474)
Timeframe: Baseline through 104 weeks

,,
Interventionparticipants (Number)
Alkaline Phosphate, High (n=276, 258, 281)ALT/SGPT, High (n=232, 237, 244)Amylase Pancreatic, High (n=283, 277, 295)Amylase Total, High (n=266, 265, 277)AST/SGOT, High (n=273, 269, 284)Basophils, High (n=276, 268, 288)Basophils, Low (n=277, 268, 288)Bilirubin Direct, High (n=295, 291, 307)Bilirubin Total, High (n=295, 290, 305)Calcitonin, High (n=233, 239, 235)Chloride, High (n=299, 293, 310)Chloride, Low (n=299, 293, 308)CPK, High (n=273, 262, 276)Creatinine, High (n=294, 285, 303)Creatinine Clearance, High (n=164, 186, 180)Creatinine Clearance, Low (n=292, 278, 303)Eosinophils, High (n=265, 265, 284)Eosinophils, Low (n=277, 268, 288)Erythrocyte Count, High (n=283, 276, 292)Erythrocyte Count, Low (n=278, 272, 285)GGT, High (n=234, 240, 245)Hematocrit, High (n=280, 274, 290)Hematocrit, Low (n=262, 251, 269)Hemoglobin, High (n=282, 275, 294)Hemoglobin, Low (n=265, 253, 269)Leukocyte Count, High (n=277, 270, 292)Leukocyte Count, Low (n=277, 267, 284)Lipase, High (n=255, 248, 269)Lymphocytes, High (n=257, 262, 279)Lymphocytes, Low (n=273, 266, 281)MCHC, High (n=281, 274, 291)MCHC, Low (n=280, 272, 290)MCV, High (n=267, 256, 273)MCV, Low (n=270, 261, 286)Monocytes, High (n=274, 267, 284)Monocytes, Low (n=271, 264, 283)Neutrophils, High (n=272, 263, 286)Neutrophils, Low (n=271, 260, 280)Platelet Count, High (n=273, 268, 287)Platelet Count, Low (n=270, 260, 275)Potassium, High (n=297, 291, 307)Potassium, Low (n=298, 293, 308)Sodium, High (n=291, 291, 307)Sodium, Low (n=298, 292, 305)Urea Nitrogen, High (n=287, 282, 305)UMCR, High (n=223, 212, 239)
0.75 mg LY2189265113778552700183224116322522021424624328971322090425311412637981012927
1.5 mg LY2189265132981442110235035211262412031816330430139142195053993101510281481051738
Sitagliptin20396143361036413549342014011945329225814126211205254111713103885652930

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Number of Participants With Treatment-emergent Abnormal Laboratory Tests at 26 Weeks

The number of participants with treatment-emergent abnormal laboratory results (defined as abnormalities that first occur after baseline) was summarized cumulatively for alkaline phosphatase, alanine aminotransferase or serum glutamic pyruvic transaminase (ALT/SGPT), amylase (pancreatic and total), aspartate aminotransferase or serum glutamic oxaloacetic transaminase (AST/SGOT), basophils, bilirubin (direct and total), calcitonin, chloride, creatine phosphokinase (CPK), creatinine, creatinine clearance, eosinophils, erythrocytes, gamma glutamyltransferase (GGT), hematocrit, hemoglobin, leukocytes, lipase, lymphocytes, mean cell hemoglobin concentration (MCHC), mean cell volume (MCV), monocytes, neutrophils, platelets, potassium, sodium, urea nitrogen, and urine microalbumin-to-creatinine ratio (UMCR). (NCT00734474)
Timeframe: Baseline through 26 weeks

,,,
Interventionparticipants (Number)
Alkaline Phosphatase (n=276, 258, 281, 162)ALT/SGPT (n=232, 237, 244, 128)Amylase Pancreatic, High (n=283, 277, 295, 160)Amylase Total (n=266, 265, 277, 143)AST/SGOT (n=273, 269, 284, 148)Basophils, High (n=268, 259, 278, 163)Basophils, Low (n=269, 259, 278, 163)Bilirubin Direct, High (n=295, 291, 307, 171)Bilirubin Total, High (n=295, 290, 305, 168)Calcitonin, High (n=226, 233, 230, 113)Chloride, High (n=299, 293, 310, 174)Chloride, Low (n=299, 293, 308, 174)CPK, High (n=273, 262, 276, 156Creatinine, High (n=294, 285, 303, 172)Creatinine Clearance, High (n=164, 186, 180, 107)Creatinine Clearance, Low (n=292, 278,303,168)Eosinophils, High (n=258, 256, 275, 157)Eosinophils, Low (n=269, 259, 278, 163)Erythrocyte Count, High (n=279, 272, 287, 164)Erythrocyte Count, Low (n=274, 268, 280, 161)GGT, High (n=234, 240, 245, 144)Hematocrit, High (n=273, 265, 279, 161)Hematocrit, Low (n=256, 242, 259, 157)Hemoglobin, High (n=278, 271, 289, 164)Hemoglobin, Low (n=262, 249, 265, 162)Leukocyte Count, High (n=272, 265, 286, 165)Leukocyte Count, Low (n=272, 262, 280, 165)Lipase, High (n=255, 248, 269, 147)Lymphocytes, High (n=249, 253, 269, 161)Lymphocytes, Low (n=265, 258, 273, 159)MCHC, High (n=274, 265, 280, 163)MCHC, Low (n=273, 263, 279, 163)MCV, High (n=261, 248, 263, 156)MCV, Low (n=264, 252, 275, 162)Monocytes, High (n=266, 258, 274, 163)Monocytes, Low (n=265, 255, 274, 158)Neutrophils, High (n=264, 255, 276, 161)Neutrophils, Low (n=263, 251, 271, 162)Platelet Count, High (n=265, 260, 281, 160)Platelet Count, Low (n=262, 252, 269, 154)Potassium, High (n=297, 291, 307, 172)Potassium, Low (n=298, 293, 308, 169)Sodium, High (n=291, 291, 307, 170)Sodium, Low (n=298, 292, 305, 174)Urea Nitrogen, High (n=287, 282, 305, 169)UMCR, High (n=217, 204, 232, 130)
0.75 mg LY21892653245533120014212201028171101711110116639293021220551032641179
1.5 mg LY21892659185433141012101297171140112911311332109530019316420274321118
Placebo/Sitagliptin (Baseline Through 26 Weeks)3818137002100175256200310252301373200501101103414155
Sitagliptin12254227181014201305261260072316151497640014238321653441313

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Number of Participants With Adjudicated Cardiovascular Events at 104 Weeks

Data on any new cardiovascular (CV) event was prospectively collected using a CV event electronic case report form. At prespecified visits, participants were asked about any new CV event. Deaths and nonfatal cardiovascular adverse events (AEs) were adjudicated by a committee of physicians with cardiology expertise external to the Sponsor. The nonfatal cardiovascular AEs to be adjudicated include myocardial infarction, hospitalization for unstable angina, hospitalization for heart failure, coronary interventions (such as coronary artery bypass graft or percutaneous coronary intervention), and cerebrovascular events including cerebrovascular accident (stroke) and transient ischemic attack. The number of participants with adjudicated CV events is summarized cumulatively. A summary of serious and other non-serious adverse events regardless of causality is located in the Reported Adverse Events module. (NCT00734474)
Timeframe: Baseline through 104 weeks

,,,,,,,,,
Interventionparticipants (Number)
Participants With Any CV EventParticipants With a Fatal CV EventParticipants With a Non-fatal CV Event
0.25 mg LY2189265000
0.5 mg LY2189265000
0.75 mg LY2189265404
1.0 mg LY2189265000
1.5 mg LY2189265616
2.0 mg LY2189265000
3.0 mg LY2189265000
Placebo/Sitagliptin (26 Weeks Through 104 Weeks)312
Placebo/Sitagliptin (Baseline Through 26 Weeks)000
Sitagliptin514

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Change From Baseline in Blood Pressure at Dose Decision Point

Sitting systolic blood pressure (SBP) and diastolic blood pressure (DBP) were measured at the dose decision point. Change from baseline in DBP was 1 of the 4 measures included in the clinical utility index (CUI) used to evaluate the dose decision. The maximum duration of exposure to LY2189265, Sitagliptin, or Placebo (across all treatment arms) at the time of the decision point was 27.4 weeks. (NCT00734474)
Timeframe: Baseline up to 27.4 weeks

,,,,,,,,
Interventionmillimeters of mercury (mmHg) (Mean)
Sitting SBPSitting DBP
0.25 mg LY21892651.671.28
0.5 mg LY21892650.40-0.75
0.75 mg LY2189265-6.21-3.18
1.0 mg LY2189265-2.00-0.08
1.5 mg LY2189265-4.77-1.20
2.0 mg LY2189265-4.63-1.17
3.0 mg LY2189265-8.85-1.21
Placebo/Sitagliptin (Baseline Through 26 Weeks)-0.61-0.22
Sitagliptin-2.16-1.11

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Number of Participants With Treatment-emergent Abnormal Laboratory Tests at 52 Weeks

The number of participants with treatment-emergent abnormal laboratory results (defined as abnormalities that first occur after baseline) was summarized cumulatively for alkaline phosphatase, alanine aminotransferase or serum glutamic pyruvic transaminase (ALT/SGPT), amylase (pancreatic and total), aspartate aminotransferase or serum glutamic oxaloacetic transaminase (AST/SGOT), basophils, bilirubin (direct and total), calcitonin, chloride, creatine phosphokinase (CPK), creatinine, creatinine clearance, eosinophils, erythrocytes, gamma glutamyltransferase (GGT), hematocrit, hemoglobin, leukocytes, lipase, lymphocytes, mean cell hemoglobin concentration (MCHC), mean cell volume (MCV), monocytes, neutrophils, platelets, potassium, sodium, urea nitrogen, and urine microalbumin-to-creatinine ratio (UMCR) . (NCT00734474)
Timeframe: Baseline through 52 weeks

,,
Interventionparticipants (Number)
Alkaline Phosphatase, High (n=276, 258, 281)ALT/SGPT, High (n=232, 237, 244)Amylase Pancreatic, High (n=283, 277, 295)Amylase Total, High (n=266, 265, 277)AST/SGOT, High (n=273, 269, 284)Basophils, High (n=276, 268, 287)Basophils, Low (n=277, 268, 287)Bilirubin Direct, High (n=295, 291, 307)Bilirubin Total, High (n=295, 290, 305)Calcitonin, High (n=233, 239, 235)Chloride, High (n=299, 293, 310)Chloride, Low (n=299, 293, 308)CPK, High (n=273, 262, 276)Creatinine, High (n=294, 285, 303)Creatinine Clearance, High (n=164, 186, 180)Creatinine Clearance, Low (n=292, 278, 303)Eosinophils, High (n=265, 265, 283)Eosinophils, Low (n=277, 268, 287)Erythrocyte Count, High (n=283, 276, 292)Erythrocyte Count, Low (n=278, 272, 285)GGT, High (n=234, 240, 245)Hematocrit, High (n=280, 274, 290)Hematocrit, Low (n=262, 251, 269)Hemoglobin, High (n=282, 275, 294)Hemoglobin, Low (n=265, 253, 269)Leukocyte Count, High (n=277, 270, 292)Leukocyte Count, Low (n=277, 267, 284)Lipase, High (n=255, 248, 269)Lymphocytes, High (n=257, 262, 278)Lymphocytes, Low (n=273, 266, 280)MCHC, High (n=281, 274, 291)MCHC, Low (n=280, 272, 290)MCV, High (n=267, 256, 273)MCV, Low (n=270, 261, 286)Monocytes, High (n=274, 267, 283)Monocytes, Low (n=271, 264, 282)Neutrophils, High (n=272, 263, 285)Neutrophils, Low (n=271, 260, 279)Platelet Count, High (n=272, 267, 287)Platelet Count, Low (n=269, 259, 275)Potassium, High (n=297, 291, 307)Potassium, Low (n=298, 293, 308)Sodium, High (n=291, 291, 307)Sodium, Low (n=298, 292, 305)Urea Nitrogen, High (n=287, 282, 305)UMCR, High (n=223, 212, 238)
0.75 mg LY21892656277042190016212281030201401914213119631111540318209722557811921
1.5 mg LY2189265102567381510124013892318110315103213217512412402253188604106531433
Sitagliptin1628553625102520243629151001113421111139110111103194515762855442118

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Number of Participants With Treatment-emergent Abnormal Lipid Tests

The number of participants with treatment-emergent abnormal lipid test (cholesterol, high density lipoprotein cholesterol [HDL-C], low density lipoprotein cholesterol [LDL-C], and triglycerides [TG]) results (defined as lipid test abnormalities that first occurred after baseline) is summarized cumulatively. (NCT00734474)
Timeframe: Baseline through 26 and 104 weeks

,,,
Interventionparticipants (Number)
Cholesterol, High, 26 Weeks (n=144, 158, 139, 58)Cholesterol, High, 104 Weeks (n=151, 164, 146)HDL-C, High, 26 Weeks (n=197, 201, 189, 78)HDL-C, Low, 26 Weeks (n=127, 137, 129, 52)HDL-C, High, 104 Weeks (n=206, 212, 199)HDL-C, Low, 104 Weeks (n=134, 143, 138)LDL-C, High, 26 Weeks (n=155, 163, 150, 61)LDL-C, High, 104 Weeks (n=163, 170, 157)TG, High, 26 Weeks (n=163, 174, 156, 64)TG, High, 104 Weeks (n=170, 183, 166)
0.75 mg LY2189265212901312011231322
1.5 mg LY21892651634192131531613
Placebo/Sitagliptin (Baseline Through 26 Weeks)8NA01NANA7NA2NA
Sitagliptin20340821319291015

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Participant-reported Outcomes, EQ-5D

The EQ-5D questionnaire is a generic, multidimensional, health-related, quality-of-life instrument. It consists of 2 parts. The first part allows participants to rate their health state in 5 health domains: mobility, self-care, usual activities, pain/discomfort, and mood using a three level scale of 1-3 (no problem, some problems, and major problems). These combinations of attributes were converted into a weighted health-state Index Score according to the United Kingdom (UK) population-based algorithm. The possible values for the Index Score ranged from -0.59 (severe problems in all 5 dimensions) to 1.0 (no problem in any dimension). The second part of the questionnaire consists of a 100-millimeter visual analog scale (VAS) on which the participants rated their perceived health state on that day from 0 (worst imaginable health state) to 100 (best imaginable health state). (NCT00734474)
Timeframe: Baseline, 52 weeks, and 104 weeks

,,
Interventionunits on a scale (Mean)
EQ-5D, UK, Baseline (n=285, 281, 300)EQ-5D, UK, 52 Weeks (n=237, 250, 244)EQ-5D, UK, 104 Weeks (n=189, 190, 185)VAS, Baseline (n=285, 284, 301)VAS, 52 Weeks (n=238, 251, 245)VAS, 104 Weeks (n=189, 190, 185)
0.75 mg LY21892650.820.840.8675.3578.2278.52
1.5 mg LY21892650.800.830.8475.5778.9379.66
Sitagliptin0.840.850.8676.8578.7981.34

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Percentage of Participants Who Achieve Glycosylated Hemoglobin (HbA1c) <7% or ≤6.5%

The percentage of participants achieving HbA1c levels <7.0% and ≤6.5% was analyzed using a logistic regression model and last observation carried forward (LOCF) imputation with baseline, country, and treatment as factors included in the model. (NCT00734474)
Timeframe: Baseline, 26, 52, and 104 weeks

,,,
Interventionpercentage of participants (Number)
<7.0% at 26 Weeks<7.0% at 52 Weeks<7.0% at 104 Weeks≤6.5% at 26 Weeks≤6.5% at 52 Weeks≤6.5% at 104 Weeks
0.75 mg LY218926555.248.844.831.029.024.2
1.5 mg LY218926560.957.654.346.741.739.1
Placebo/Sitagliptin (Baseline Through 26 Weeks)21.0NANA12.5NANA
Sitagliptin37.833.031.121.819.214.1

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Rate of Hypoglycemic Episodes

Hypoglycemic episodes (HE) were classified as severe (defined as episodes requiring assistance from another person to actively administer resuscitative actions), documented symptomatic (defined as any time a participant feels that he/she is experiencing symptoms and/or signs associated with hypoglycemia and has a plasma glucose level of ≤3.9 millimoles per liter [mmol/L]), asymptomatic (defined as episodes not accompanied by typical symptoms of hypoglycemia but with a measured plasma glucose of ≤3.9 mmol/L), nocturnal (defined as any episode that occurred between bedtime and waking), or probable symptomatic (defined as episodes during which symptoms of hypoglycemia were not accompanied by a plasma glucose determination). The 1-year adjusted rate of HE is summarized cumulatively. (NCT00734474)
Timeframe: Baseline through 26 and 104 weeks

,,,
Interventionepisodes per participant per year (Mean)
Severe HE, 26 WeeksSevere HE, 104 WeeksDocumented Symptomatic HE, 26 WeeksDocumented Symptomatic HE, 104 WeeksAsymptomatic HE, 26 WeeksAsymptomatic HE, 104 WeeksNocturnal HE, 26 WeeksNocturnal HE, 104 WeeksProbable Symptomatic HE, 26 WeeksProbable Symptomatic HE, 104 Weeks
0.75 mg LY21892650.00.00.10.20.10.00.10.00.00.0
1.5 mg LY21892650.00.00.30.20.10.10.10.10.00.0
Placebo/Sitagliptin (Baseline Through 26 Weeks)0.0NA0.1NA0.0NA0.0NA0.0NA
Sitagliptin0.00.00.10.20.00.00.00.10.00.0

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Resource Utilization

The number of visits to the emergency room (ER) is summarized cumulatively. (NCT00734474)
Timeframe: Baseline through 52 and 104 weeks

,,
Interventionevents (Number)
52 Weeks104 Weeks
0.75 mg LY2189265NANA
1.5 mg LY2189265NANA
SitagliptinNANA

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Change in Homeostasis Model Assessment Index for Insulin Resistance (HOMA-IR)

HOMA-IR (to assess insulin resistance) is defined as (FPI x FPG)/22.5. Results based on ANCOVA. (NCT00749190)
Timeframe: Baseline and 12 weeks

InterventionmU/L x mmol/L (Mean)
Placebo0.23
Empagliflozin 1 mg-0.11
Empagliflozin 5 mg-0.60
Empagliflozin 10 mg-1.04
Empagliflozin 25 mg-0.52
Empagliflozin 50 mg-1.10
Sitagliptin OL0.48

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Change From Baseline in HbA1c After 12 Weeks of Treatment

"Change from baseline in HbA1c after 12 weeks of treatment.~In the measured values adjusted means are displayed. For means for the placebo and empagliflozin arms are from the model excluding the sitagliptin open label (OL) arm. The mean for the sitagliptin OL arm is from the model with just this treatment group and the placebo group." (NCT00749190)
Timeframe: Baseline and 12 weeks

Interventionpercentage of HbA1c (Mean)
Placebo0.15
Empagliflozin 1 mg-0.09
Empagliflozin 5 mg-0.23
Empagliflozin 10 mg-0.56
Empagliflozin 25 mg-0.55
Empagliflozin 50 mg-0.49
Sitagliptin OL-0.45

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Proportion of Patients Who Achieve an HbA1c Lowering of at Least 0.5% After 12 Weeks of Treatment

Results for HbA1c categories at week 12 (Proportion of patients with HbA1c lowered at least 0.5%) based on logistic regression (NCT00749190)
Timeframe: Baseline and 12 weeks

Interventionpercentage of participants (Number)
Placebo21.1
Empagliflozin 1 mg31.0
Empagliflozin 5 mg40.8
Empagliflozin 10 mg60.6
Empagliflozin 25 mg60.0
Empagliflozin 50 mg48.6
Sitagliptin OL53.5

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Change in Homeostasis Model Assessment Index for Beta Cell Function (HOMA-%B)

HOMA-%B (to assess insulin beta cell function) is defined as (20 x FPI)/(FPG-3.5), FPG in mg/dl. Results are based on ANCOVA. (NCT00749190)
Timeframe: Baseline and 12 weeks

InterventionmU / mmol (Mean)
Placebo0.30
Empagliflozin 1 mg0.08
Empagliflozin 5 mg0.36
Empagliflozin 10 mg1.55
Empagliflozin 25 mg6.68
Empagliflozin 50 mg4.01
Sitagliptin OL12.38

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Change From Baseline to Week 12 in Fasting Plasma Insulin (FPI)

Results for change of FPI from baseline at week 12 based on ANCOVA (NCT00749190)
Timeframe: Baseline and 12 weeks

InterventionmU/L (Mean)
Placebo0.43
Empagliflozin 1 mg0.09
Empagliflozin 5 mg-0.84
Empagliflozin 10 mg-1.77
Empagliflozin 25 mg-0.11
Empagliflozin 50 mg-1.52
Sitagliptin OL1.84

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Proportion of Patients Who Achieve an HbA1c ≤7.0% After 12 Weeks of Treatment

Results for HbA1c categories at week 12 (Proportion of patients with HbA1c less than equal to 7%) based on logistic regression (NCT00749190)
Timeframe: Baseline and 12 weeks

Interventionpercentage of participants (Number)
Placebo15.5
Empagliflozin 1 mg23.9
Empagliflozin 5 mg21.1
Empagliflozin 10 mg38.0
Empagliflozin 25 mg37.1
Empagliflozin 50 mg35.7
Sitagliptin OL33.8

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Change of HbA1c From Baseline Over Time

Change of HbA1c from baseline over time. Results presented stem from a repeated measures analysis. (NCT00749190)
Timeframe: Baseline and weeks 4, 8 and 12

,,,,,,
Interventionpercentage of HbA1c (Mean)
Week 4Week 8Week 12
Empagliflozin 1 mg-0.12-0.14-0.08
Empagliflozin 10 mg-0.32-0.57-0.57
Empagliflozin 25 mg-0.31-0.52-0.59
Empagliflozin 5 mg-0.16-0.30-0.27
Empagliflozin 50 mg-0.36-0.53-0.50
Placebo0.020.050.12
Sitagliptin OL-0.26-0.40-0.45

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Change of Body Weight After 12 Weeks of Treatment

Results for change of body weight after 12 weeks of treatment based on ANCOVA. (NCT00749190)
Timeframe: Baseline and 12 weeks

Interventionkg (Mean)
Placebo-1.16
Empagliflozin 1 mg-1.55
Empagliflozin 5 mg-2.28
Empagliflozin 10 mg-2.74
Empagliflozin 25 mg-2.56
Empagliflozin 50 mg-2.85
Sitagliptin OL-0.84

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Change of FPG From Baseline After 12 Weeks of Treatment

"Change of Fasting Plasma Glucose (FPG) from baseline after 12 weeks of treatment. Results presented stem from a repeated measures analysis.~In the measured values adjusted means are displayed. For means for the placebo and empagliflozin arms are from the model excluding the sitagliptin open label (OL) arm. The mean for the sitagliptin OL arm is from the model with just this treatment group and the placebo group." (NCT00749190)
Timeframe: Baseline and 12 weeks

Interventionmg/dL (Mean)
Placebo4.75
Empagliflozin 1 mg-1.70
Empagliflozin 5 mg-15.84
Empagliflozin 10 mg-22.14
Empagliflozin 25 mg-26.83
Empagliflozin 50 mg-27.91
Sitagliptin OL-12.92

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Trough Concentrations of Empagliflozin in Plasma

(Pre-dose) trough concentrations of Empagliflozin in plasma, within 30 minutes of dosing. (NCT00749190)
Timeframe: Days 28, 56 and 84

,,,,
Interventionnmol/L (Geometric Mean)
Day 28 (N=58, 65, 62, 58, 63)Day 56 (N=56, 64, 64, 61, 61)Day 84 (N=53, 61, 59, 57, 57)
Empagliflozin 1 mg3.192.932.87
Empagliflozin 10 mg27.323.023.4
Empagliflozin 25 mg92.575.471.0
Empagliflozin 5 mg13.111.511.2
Empagliflozin 50 mg119119112

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Insulin Dose in the Insulin Glargine Group

Daily dose at the face-to-face visits. (NCT00751114)
Timeframe: visit 4 (week 2), visit 8 (week 6), visit 11 (week 12), visit 12 (week 16), visit 14 (week 24), first dose received defined as first available value, study endpoint defined as last available value

Interventionunit per kg body weight (Mean)
First dose received N=236Visit 4 (week 2) N=230Visit 8 (week 6) N=222Visit 11 (week 12) N=219Visit 12 (week 16) N=214Visit 14 (week 24) N=220Study endpoint N=237
Insulin Glargine0.190.270.380.450.480.500.49

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Lipid Profile: Change From Baseline to Study Endpoint

(NCT00751114)
Timeframe: baseline (week 0), study endpoint: visit 14 (week 24) or visit 11 (week 12) if value not available at visit 14

,
Interventionmg/dL (Least Squares Mean)
Change in Total CholesterolChange in LDL CholesterolChange in HDL CholesterolChange in Triglycerides
Insulin Glargine-7.94-3.680.13-34.07
Sitagliptin-1.54-0.190.570.31

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HbA1c Response Rate: Percentage of Patients Who Reach the Target of HbA1c < 6.5% at Study Endpoint

(NCT00751114)
Timeframe: study endpoint: visit 14 (week 24) or visit 11 (week 12) if value not available at visit 14

Interventionpercentage of participants (Number)
Insulin Glargine40.2
Sitagliptin16.9

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HbA1c Response Rate: Percentage of Patients Who Reach the Target of HbA1c < 7% at Study Endpoint

(NCT00751114)
Timeframe: study endpoint: visit 14 (week 24) or visit 11 (week 12) if value not available at visit 14

Interventionpercentage of participants (Number)
Insulin Glargine67.9
Sitagliptin41.9

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Change in Body Weight From Baseline to Study Endpoint

(NCT00751114)
Timeframe: baseline (week 0), study endpoint: visit 14 (week 24) or visit 12 (week 16) or visit 11 (week 12) or visit 8 (week 6) depending on last available value

Interventionkg (Least Squares Mean)
Insulin Glargine0.44
Sitagliptin-1.08

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HbA1c: Change From Baseline to Study Endpoint

Change in HbA1c from baseline to study endpoint defined as the last available HbA1c value measured during the 24-week treatment period. (NCT00751114)
Timeframe: baseline (week 0), study endpoint: visit 14 (week 24) or visit 11 (week 12) if value not available at visit 14

Interventionpercent (Least Squares Mean)
Insulin Glargine-1.72
Sitagliptin-1.13

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Number of Patients With at Least One Episode of Severe Symptomatic Hypoglycemia

Severe symptomatic hypoglycemia was defined as an event with clinical symptoms which required assistance of another person and with either a Plasma Glucose level < 36 mg/dL (2 mmol/L) or with a prompt recovery after oral carbohydrate, intravenous glucose, or glucagon administration (NCT00751114)
Timeframe: During the treatment phase (24 weeks) plus 7 days after last dose

Interventionparticipants (Number)
Insulin Glargine3
Sitagliptin1

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Number of Patients With at Least One Episode of Symptomatic Hypoglycemia

Symptomatic hypoglycemia was defined as an event with clinical symptoms that were considered to result from hypoglycemia confirmed or not by a plasma glucose measurement <= 70mg/dL [3.9 mmol/L] (NCT00751114)
Timeframe: During the treatment phase (24 weeks) plus 7 days after last dose

Interventionparticipants (Number)
Insulin Glargine108
Sitagliptin35

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Self-monitored Fasting Plasma Glucose (SMFPG) Mean : Change From Baseline to Study Endpoint

"SMFPG mean = mean of the fasting plasma glucose values recorded on the 6 consecutive days before the visit (at least 3 values needed).~Study endpoint was defined as the last available SMFPG mean value collected on-treatment.~Change= study endpoint - baseline" (NCT00751114)
Timeframe: baseline (week 0), study endpoint: visit 14 (week 24) or visit 12 (week 16) or visit 11 (week 12) or visit 8 (week 6) depending on last available value

Interventionmg/dL (Least Squares Mean)
Insulin Glargine-60.52
Sitagliptin-19.35

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7-point Plasma Glucose Profile: Change From Baseline to Study Endpoint

"7-point plasma glucose recorded before and after breakfast, before and after lunch, before and after dinner and at bedtime.~Change = study endpoint - baseline." (NCT00751114)
Timeframe: baseline (week 0), study endpoint: visit 14 (week 24) or visit 11 (week 12) if value not available at visit 14

,
Interventionmg/dL (Least Squares Mean)
Before breakfast (N ig = 203 & N s = 226)After breakfast (N ig = 202 & N s = 220)Before lunch (N ig = 201 & N s = 223)After lunch (N ig = 202 & N s = 226)Before dinner (N ig = 199 & N s = 223)After dinner (N ig = 196 & N s = 220)At bedtime (N ig = 177 & N s = 210)
Insulin Glargine-59.90-66.25-48.00-45.54-40.68-45.88-45.58
Sitagliptin-20.39-36.41-19.82-26.10-25.07-33.78-31.16

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Change From Baseline in 24-hour Weighted Mean Plasma Glucose

Change from baseline at Week 4 is defined as 24-hour weighted mean glucose (24hr-WMG) at Week 4 minus 24hr-WMG at Week 0. (NCT00758069)
Timeframe: Baseline and Week 4

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg QD-34.9
Sitagliptin 50 mg BID-28.6
Placebo-9.0

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Change From Baseline in Plasma Glucose

Change from baseline at Week 4 is defined as fasting plasma glucose at Week 4 minus fasting plasma glucose at Week 0. (NCT00758069)
Timeframe: Baseline and Week 4

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg QD-22.3
Sitagliptin 50 mg BID-16.0
Placebo-3.1

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The Primary Endpoint Will be Insulin Independence After 6 Months of Therapy.

Insulin independence was defined as no insulin use for at least one week, HbA1c < 6.0%, fasting plasma glucose < 7.0 mmol/l, fasting or stimulated c-peptide ≥ 0.5 ng/ml. In addition capillary blood glucose levels could not be >7.8 mmol/l (fasting) or > 10 mmol/l (post-prandial) on more than three occasions in the preceding week. Mean daily insulin use was calculated from the three days prior to study visits. Blinded continuous glucose monitoring (CGM) was performed using the iPro device and Carelink software (Medtronic, Mississauga, ON, CA). (NCT00768651)
Timeframe: 6 months

Interventionproportion of participants (Number)
One Arm: Sitagliptin + Pantoprazole0.25

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Insulin Independence After the 3 Month Washout Period

Insulin independence was defined as no insulin use for at least one week, HbA1c < 6.0%, fasting plasma glucose < 7.0 mmol/l, fasting or stimulated c-peptide ≥ 0.5 ng/ml. In addition capillary blood glucose levels could not be >7.8 mmol/l (fasting) or > 10 mmol/l (post-prandial) on more than three occasions in the preceding week. Mean daily insulin use was calculated from the three days prior to study visits. Blinded continuous glucose monitoring (CGM) was performed using the iPro device and Carelink software (Medtronic, Mississauga, ON, CA). (NCT00768651)
Timeframe: After the 3 month washout period

Intervention% of insulin indipendent participants (Number)
One Arm: Sitagliptin + Pantoprazole0

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Change in Acute Insulin Response to Arginine. (AIRarg)

The changes in B-cell insulin secretion, Acute Insulin Response to arginine (AIRarg) after 6 months were compared to baseline AIRarg for each group. Listed below are AIRarg at baseline and 6 months for each group. (NCT00775684)
Timeframe: Baseline and 6 months

,,
InterventionuU/mL (Mean)
Acute Insulin Response (AIRarg) BaselineAcute Insulin Response (AIRarg) 6 Months
AIRarg Exenatide5252
AIRarg Glimepiride4442
AIRarg Sitagliptin3534

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Effect on Functional Beta-cell Mass as Determined by Change in ß-cell Secretory Capacity at 6 Months (pg/mL)

AGRmin is performed during the 340mg/dl glucose clamp allows for estimation of the minimum alpha-cell glucagon secretion. Changes from baseline to 6 months of AGRmin were compared across groups. (NCT00775684)
Timeframe: Baseline and 6 months

,,
Interventionpg/mL (Mean)
Acute Glucose Response (AGRmin) BaselineAcute Glucose Response (AGRmin) 6 Months
Exenatide5152
Glimepiride3759
Sitagliptin5559

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Effect on Functional Beta-cell Mass as Determined by Change in ß-cell Secretory Capacity at 6 Months (μU/ml)

The acute insulin response to arginine (AIRarg) performed during the 340mg/dl glucose clamp allows for estimation of the the beta-cell secretory capacity (AIRmax) or functional beta-cell mass. Changes from baseline to 6 months of AIRmax were compared across groups (NCT00775684)
Timeframe: Baseline and 6 months

,,
InterventionμU/ml (Mean)
Acute Insulin Response (AIRmax)BaselineAcute Insulin Response (AIRmax) 6 Months
Exenatide214188.5
Glimepiride133202.5
Sitagliptin149158.3

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Insulin Sensitivity at Baseline and 6 Months

Insulin sensitivity (M/I) was determined by dividing the mean glucose infusion rate required during the 230 mg/dL glucose clamp (M) by the mean prestimulus insulin level (I) between 40 and 45 min of the glucose infusion The mean difference after 6 months in insulin sensitivity (M/I) were compared (NCT00775684)
Timeframe: Baseline and 6 months

,,
Intervention((mg/kg) /min) /uU/mL (Mean)
M/I BaselineM/I 6 Months
M/I Exenatide0.30.3
M/I Glimepiride0.30.3
M/I Sitagliptin0.30.3

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PG 50 (the Plasma Glucose Level at Which Half-maximal Insulin Secretion is Achieved During the Glucose-potentiated Arginine Test) at Baseline and 6 Months

Between ∼60 and 250 mg/dL, the magnitude of AIRarg is a linear function of the plasma glucose level, so the difference in AIRarg at fasting and 230 mg/dL glucose levels divided by the difference in plasma glucose (ΔAIRarg/ΔPG) gives the glucose-potentiation slope (GPS) (8,24-26). Using the y-intercept (b) from the line created by these two points, the plasma glucose level at which half-maximal insulin secretion is achieved (PG50) is derived from solving the equation 1/2 (AIRmax) = (GPS · PG50) + b, and provides a measure of β-cell sensitivity to glucose The mean difference after 6 months in PG 50 were compared. Listed below are the PG50 values at baseline and 6 months. (NCT00775684)
Timeframe: Baseline and 6 months

,,
Interventionmg/dL (Mean)
PG50 BaselinePG50 6 Months
P50 Exenatide175190
P50 Glimepiride168182
P50 Sitagliptin226209

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HbA1c Change

Units are absolute difference in %HbA1c (HbA1c being the percentage of glycated Haemoglobin, reflecting glucose exposure over the last 3 months) (NCT00780715)
Timeframe: 6 months

Interventionabsolute change in %HbA1c (Mean)
Gliclazide MR-0.42
Sitagliptin-0.58
Pioglitazone-1.04
Metformin-1.59

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Number of Subjects Achieving HbA1c Less Than or Equal to 6.5%

(NCT00789191)
Timeframe: Week 26

,
InterventionSubjects (Number)
Target achievedTarget not achieved
Comb2083
Sita1195

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Change in BMI (Body Mass Index)

(NCT00789191)
Timeframe: Week 0, Week 26

Interventionkg/m^2 (Mean)
Comb-0.30
Sita-0.58

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Change in Body Weight

(NCT00789191)
Timeframe: Week 0, Week 26

Interventionkg (Mean)
Comb-0.81
Sita-1.66

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FPG (Fasting Plasma Glucose)

(NCT00789191)
Timeframe: Week 26

Interventionmmol/L (Mean)
Comb6.08
Sita8.52

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HbA1c (Glycosylated Haemoglobin A1c)

(NCT00789191)
Timeframe: Week 26

InterventionPercent (%) glycosylated haemoglobin (Mean)
Comb7.08
Sita7.64

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Hypoglycemic Episodes

Overall: All episodes. Minor: Symptomatic, with PG < 3.1 mmol/L. Symptoms only: Symptomatic with PG ≥ 3.1 mmol/L (NCT00789191)
Timeframe: Weeks 0-26

,
Interventionepisodes (Number)
OverallMinorSymptoms OnlyUnclassified
Comb1000
Sita1000

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Hypoglycemic Episodes: Day Time

Day time: Episodes between 6 pm and 11 am. Overall: All episodes. Minor: Symptomatic, with PG < 3.1 mmol/L. Symptoms only: Symptomatic with PG ≥ 3.1 mmol/L (NCT00789191)
Timeframe: Weeks 0-26

,
Interventionepisodes (Number)
OverallMinorSymptoms OnlyUnclassified
Comb1000
Sita1000

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Hypoglycemic Episodes: Night Time

Night time: Episodes between 11 am and 6 pm. Overall: All episodes. Minor: Symptomatic, with PG < 3.1 mmol/L. Symptoms only: Symptomatic with PG ≥ 3.1 mmol/L (NCT00789191)
Timeframe: Weeks 0-26

,
Interventionepisodes (Number)
OverallMinorSymptoms OnlyUnclassified
Comb0000
Sita0000

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Number of Subjects Achieving HbA1c Less Than or Equal to 6.5% Without Symptomatic Hypoglycaemia

Symptomatic hypoglycaemia is biochemically confirmed hypoglycaemia or major hypoglycaemia (NCT00789191)
Timeframe: Week 26

,
InterventionSubjects (Number)
Target achievedTarget not achieved
Comb1588
Sita898

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Number of Subjects Achieving HbA1c Less Than or Equal to 7.0%

(NCT00789191)
Timeframe: Week 26

,
InterventionSubjects (Number)
Target achievedTarget not achieved
Comb4657
Sita2581

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Number of Subjects Achieving HbA1c Less Than or Equal to 7.0% Without Symptomatic Hypoglycaemia

Symptomatic hypoglycaemia is biochemically confirmed hypoglycaemia or major hypoglycaemia (NCT00789191)
Timeframe: Week 26

,
InterventionSubjects (Number)
Target achievedTarget not achieved
Comb3766
Sita2185

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Self-measured 9-point Plasma Glucose Profile

(NCT00789191)
Timeframe: Week 26

,
Interventionmmol/L (Mean)
Before breakfast120 minutes after start of breakfastBefore Lunch120 minutes after start of lunchBefore dinner120 minutes after start of dinnerBedtimeAt 03:00 A.M.Before breakfast the following day
Comb6.168.826.998.697.859.308.386.856.07
Sita8.1710.508.019.998.6110.209.428.027.87

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Percentage of Participants With First Confirmed CV Event of MACE (Intent to Treat Population)

CV composite endpoint of MACE which includes CV-related death, nonfatal MI, or nonfatal stroke. (NCT00790205)
Timeframe: Up to 5 years

InterventionPercentage of participants (Number)
Sitagliptin10.2
Placebo10.2

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Percentage of Participants With First Confirmed CV Event of MACE (Per Protocol Population)

CV composite endpoint of MACE which includes CV-related death, nonfatal MI, or nonfatal stroke. (NCT00790205)
Timeframe: Up to 5 years

InterventionPercentage of participants (Number)
Sitagliptin8.4
Placebo8.3

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Percentage of Participants With First Confirmed CV Event of Major Adverse Cardiovascular Event (MACE) Plus (Intent to Treat Population)

Primary composite CV endpoint of MACE plus which includes CV-related death, nonfatal MI, nonfatal stroke, or unstable angina requiring hospitalization. (NCT00790205)
Timeframe: Up to 5 years

InterventionPercentage of participants (Number)
Sitagliptin11.4
Placebo11.6

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Percentage of Participants With Initiation of Co-interventional Agent (Intent to Treat Population)

In participants not receiving insulin at baseline, time to addition of first co-interventional agent (i.e., next oral AHA or chronic insulin, where chronic insulin therapy is defined as a continuous period of insulin use of more than 3 months.) (NCT00790205)
Timeframe: Up to 5 years

InterventionPercentage of participants (Number)
Sitagliptin21.7
Placebo27.9

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Percentage of Participants With Initiation of Co-interventional Agent (Per Protocol Population)

In participants not receiving insulin at baseline, time to addition of first co-interventional agent (i.e., next oral antihyperglycemic agent [AHA] or chronic insulin, where chronic insulin therapy is defined as a continuous period of insulin use of more than 3 months.) (NCT00790205)
Timeframe: Up to 5 years

InterventionPercentage of participants (Number)
Sitagliptin18.9
Placebo24.5

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Change From Baseline in HbA1c Over Time (Intent to Treat Population)

HbA1c is a measure of the percentage of glycated hemoglobin in the blood. Estimated mean difference between sitagliptin and placebo controlling for baseline HbA1c and region. (NCT00790205)
Timeframe: Baseline and up to 4 years

,
InterventionPercentage of HbA1c (Mean)
Month 4: Sitagliptin, n= 6772; Placebo, n= 6738Month 8: Sitagliptin, n= 6478; Placebo, n= 6414Month 12: Sitagliptin, n= 6448; Placebo, n= 6384Month 24: Sitagliptin, n= 6105; Placebo, n= 5975Month 36: Sitagliptin, n= 3521; Placebo, n= 3439Month 48: Sitagliptin, n= 1432; Placebo, n= 1383Month 60: Sitagliptin, n= 123; Placebo, n= 128
Placebo0.10.10.10.10.10.10.0
Sitagliptin-0.3-0.2-0.2-0.1-0.10.00.0

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Change From Baseline in HbA1c Over Time (Per Protocol Population)

HbA1c is a measure of the percentage of glycated hemoglobin in the blood. Estimated mean difference between sitagliptin and placebo controlling for baseline HbA1c and region. (NCT00790205)
Timeframe: Baseline and up to 4 years

,
InterventionPercentage of HbA1c (Mean)
Month 4; Sitagliptin, n=6632, Placebo, n=6588Month 8; Sitagliptin, n=6294, Placebo, n=6197Month 12; Sitagliptin, n=6217, Placebo, n=6092Month 24; Sitagliptin, n=5668, Placebo, n=5475Month 36; Sitagliptin, n=3227, Placebo, n=3083Month 48; Sitagliptin, n=1271, Placebo, n=1224Month 60; Sitagliptin, n=106, Placebo, n=108
Placebo0.10.10.10.20.10.10.0
Sitagliptin-0.3-0.3-0.2-0.1-0.10.0-0.1

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Change From Baseline in Renal Function Over Time (Intent to Treat Population)

Change in renal function based on eGFR using the MDRD method. (NCT00790205)
Timeframe: Baseline and up to 5 years

,
InterventionmL/min/1.73 m^2 (Mean)
Month 4; Sitagliptin, n=3949; Placebo, n=3977Month 8; Sitagliptin, n=3687; Placebo, n=3648Month 12; Sitagliptin, n=5082; Placebo, n=5015Month 24; Sitagliptin, n=5157; Placebo, n=5071Month 36; Sitagliptin, n=3037; Placebo, n=2942Month 48; Sitagliptin, n=1237; Placebo, n=1210Month 60; Sitagliptin, n=93; Placebo, n=106
Placebo-0.8-0.9-0.5-1.7-1.6-2.8-5.7
Sitagliptin-1.8-2.4-1.8-3.2-3.8-4.0-4.2

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Change From Baseline in Renal Function Over Time (Per Protocol Population)

Change in renal function based on estimated glomerular filtration rate [eGFR] using the Modification of Diet in Renal Disease [MDRD] method. (NCT00790205)
Timeframe: Baseline and up to 5 years

,
InterventionmL/min/1.73 m^2 (Mean)
Month 4; Sitagliptin, n= 3859; Placebo, n= 3864Month 8; Sitagliptin, n= 3562; Placebo, n= 3501Month 12; Sitagliptin, n=4912, Placebo, n=4778Month 24; Sitagliptin, n=4782, Placebo, n=4637Month 36; Sitagliptin, n=2776, Placebo, n=2614Month 48; Sitagliptin, n=1096, Placebo, n=1056Month 60; Sitagliptin, n=79, Placebo, n=88
Placebo-0.8-0.9-0.5-1.7-1.6-2.8-6.4
Sitagliptin-1.9-2.5-1.8-3.1-3.7-3.7-3.5

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Change From Baseline in Urine Albumin:Creatinine Ratio Over Time (Intent to Treat Population)

Change from baseline reflects the difference between the urine albumin:creatinine ratio reported time point and baseline value. (NCT00790205)
Timeframe: Baseline and up to 5 years

,
Interventiong/mol Creatinine (Mean)
Month 4; n=677, n=713Month 8; n=658, n=624Month 12; n=1167, n=1115Month 24; n=1011, n=964Month 36; n=537, n=553Month 48; n=265, n=256Month 60; n=14, n=18
Placebo-1.40.51.23.13.91.66.4
Sitagliptin-2.12.11.30.52.61.9-2.5

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Change From Baseline in Urine Albumin:Creatinine Ratio Over Time (Per Protocol Population)

Change from baseline reflects the difference between the urine albumin:creatinine ratio reported time point and baseline value. (NCT00790205)
Timeframe: Baseline and up to 5 years

,
Interventiong/mol Creatinine (Mean)
Month 4; Sitagliptin, n=664; Placebo, n=688Month 8; Sitagliptin, n=635; Placebo, n=597Month 12; Sitagliptin, n=1126; Placebo, n=1059Month 24; Sitagliptin, n=930; Placebo, n=892Month 36; Sitagliptin, n=488; Placebo, n=513Month 48; Sitagliptin, n=238; Placebo, n=233Month 60; Sitagliptin, n=13; Placebo, n=17
Placebo-1.40.21.23.24.01.54.8
Sitagliptin-2.21.70.80.72.51.3-2.7

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Percent Incidence of All-cause Mortality (Intent to Treat Population)

Percent incidence of all-cause mortality is reported as the percentage of participants who died due to any cause. (NCT00790205)
Timeframe: Up to 5 years

InterventionPercentage of participants (Number)
Sitagliptin7.5
Placebo7.3

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Percent Incidence of All-cause Mortality (Per Protocol Population)

Percent incidence of all-cause mortality is reported as the percentage of participants who died due to any cause. (NCT00790205)
Timeframe: Up to 5 years

InterventionPercentage of participants (Number)
Sitagliptin4.7
Placebo4.3

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Percent Incidence of CHF Requiring Hospitalization (Intent to Treat Population)

Percent incidence of CHF requiring hospitalization was reported as the percentage of participants who were admitted to the hospital for CHF. (NCT00790205)
Timeframe: Up to 5 years

InterventionPercentage of participants (Number)
Sitagliptin3.1
Placebo3.1

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Percent Incidence of Congestive Heart Failure (CHF) Requiring Hospitalization (Per Protocol Population)

Percent incidence of CHF requiring hospitalization was reported as the percentage of participants who were admitted to the hospital for CHF. (NCT00790205)
Timeframe: Up to 5 years

InterventionPercentage of participants (Number)
Sitagliptin2.8
Placebo2.8

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Percentage of Participants Who Initiated Chronic Insulin Therapy (Intent to Treat Population)

Chronic insulin therapy is defined as a continuous period of insulin use of more than 3 months. (NCT00790205)
Timeframe: Up to 5 years

InterventionPercentage of participants (Number)
Sitagliptin9.7
Placebo13.2

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Percentage of Participants Who Initiated Chronic Insulin Therapy (Per Protocol Population)

Chronic insulin therapy is defined as a continuous period of insulin use of more than 3 months. (NCT00790205)
Timeframe: Up to 5 years

InterventionPercentage of participants (Number)
Sitagliptin8.6
Placebo11.9

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Percentage of Participants With First Confirmed Cardiovascular (CV) Event of Major Adverse Cardiovascular Event (MACE) Plus (Per Protocol Population)

Primary composite CV endpoint of MACE plus which includes CV-related death, nonfatal MI, nonfatal stroke, or unstable angina requiring hospitalization. (NCT00790205)
Timeframe: Up to 5 years

InterventionPercentage of participants (Number)
Sitagliptin9.6
Placebo9.6

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Change in Endogenous Glucose Production

(NCT00795275)
Timeframe: Baseline and 28 days

,
Interventionmg/kg/min (Mean)
BaselineDay 28
People With Impaired Fasting Glucose1.471.44
People With Normal Glucose Tolerance1.461.37

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Change in Insulin Secretion

(NCT00795275)
Timeframe: Baseline and 28 days

,
Interventionpmol/l (Mean)
Baseline28 Days
Impaired Fasting Glucose10475
Normal Glucose Tolerance9771

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Baseline and Change in Hormones, Substrates and Insulin Action: C-peptide

(NCT00795275)
Timeframe: Baseline and 28 days

,
Interventionnmol/l (Mean)
BaselineDay 28
Impaired Fasting Glucose0.80.9
Normal Glucose Tolerance0.70.7

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Baseline and Change in Hormones, Substrates and Insulin Action: FFA

(NCT00795275)
Timeframe: Baseline and 28 days

,
Interventionumol/l (Mean)
BaselineDay 28
Impaired Fasting Glucose604631
Normal Glucose Tolerance610547

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Baseline and Change in Hormones, Substrates and Insulin Action: GLP-1

(NCT00795275)
Timeframe: Baseline and 28 days

,
Interventionpmol/l (Mean)
BaselineDay 28
Impaired Fasting Glucose7.58.3
Normal Glucose Tolerance3.45.4

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Baseline and Change in Hormones, Substrates and Insulin Action: Glucagon

(NCT00795275)
Timeframe: Baseline and 28 days

,
Interventionng/l (Mean)
BaselineDay 28
Impaired Fasting Glucose6261
Normal Glucose Tolerance6366

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Baseline and Change in Hormones, Substrates and Insulin Action: Glycerol

(NCT00795275)
Timeframe: Baseline and 28 days

,
Interventionumol/l (Mean)
BaselineDay 28
Impaired Fasting Glucose9193
Normal Glucose Tolerance8585

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Baseline and Change in Hormones, Substrates and Insulin Action: Lactate

(NCT00795275)
Timeframe: Baseline and 28 days

,
Interventionmmol/l (Mean)
BaselineDay 28
Impaired Fasting Glucose0.40.4
Normal Glucose Tolerance0.30.4

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Change From Baseline in Hemoglobin A1c (A1C) at Week 24 for Participants on Metformin 1700 mg/Day

A1C is measured as percent. Thus, this change from baseline reflects the Week 24 A1C percent minus the Week 0 A1C percent. (NCT00813995)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Sitagliptin-1.14
Placebo-0.21

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Change From Baseline in Hemoglobin A1c (A1C) at Week 24 for Participants on Metformin 1000 mg/Day

A1C is measured as percent. Thus, this change from baseline reflects the Week 24 A1C percent minus the Week 0 A1C percent. (NCT00813995)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Sitagliptin-0.84
Placebo-0.01

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Change From Baseline in Hemoglobin A1c (A1C) at Week 24

A1C is measured as percent. Thus, this change from baseline reflects the Week 24 A1C percent minus the Week 0 A1C percent. (NCT00813995)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Sitagliptin-1.02
Placebo-0.14

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24

Change from baseline at Week 24 is defined as Week 24 minus Week 0. (NCT00813995)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-20.3
Placebo0.5

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Change From Baseline in 2-hour Post-meal Glucose (PMG) at Week 24

Change from baseline at Week 24 is defined as Week 24 minus Week 0. (NCT00813995)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-43.4
Placebo-10.0

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Objective: Comparisons of the Effects of Co-administration of Sitagliptin and Metformin Alone or in Combination Versus Placebo on Baseline Endogenous Glucose Production (EGP).

Baseline endogenous glucose production prior to a mixed meal tolerance test (placebo) and following 6 weeks of either sitagliptin, metformin or sitagliptin plus metformin combination therapy in all 16 participants (NCT00820573)
Timeframe: 6 weeks

Interventionmg/kg.min (Mean)
Placebo2.0
Metformin1.8
Sitagliptin1.7
Sitagliptin Plus Metformin1.5

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Changes in Plasma Glucose Post-MTT After Each Six Weeks of Therapy Compared to Baseline

The absolute values of mean plasma glucose post-meal (360 minutes)were determined after each specific 6 week treatment and these absolute values after each specific sequence therapy were compared amongst all groups. (NCT00820573)
Timeframe: 360 min

Interventionmg/dl (Mean)
Placebo205
Metformin191
Sitagliptin195
Sitagliptin+Metformin161

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Fasting Plasma Glucose 6 Weeks After Therapy

Basal pasma glucose was determined with the glucose oxidase method after each specific 6 week treatment. The absolute values obtained of basal plasma glucose at the end of each 6-week therapeutic period in each sequence study group (both basal and post-meal) were compared amongst all groups. (NCT00820573)
Timeframe: 6 weeks

Interventionmg/dl (Mean)
Placebo160
Metformin145
Sitagliptin150
Sitagliptin Plus Metformin120

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Average of Plasma Glucose During Mixed Meal Tolerance Test (MTT) Compared to Baseline Plasma Glucose to Post Therapy (6-weeks).

The degree of suppression of baseline endogenous glucose production was measured in absolute values and as a percent of basal values at the end of each 6-week therapeutic period. The absolute values obtained in each sequence study group (both basal and post-meal) were compared amongst all groups. (NCT00820573)
Timeframe: 6 weeks

Interventionmg/kg.min (Mean)
Placebo1.8
Metformin1.6
Sitagliptin1.7
Sitagliptin + Metformin1.5

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Incremental Post-prandial 4-hour Weighted Mean Active Glucagon-like Peptide-1 (GLP-1) Plasma Concentrations

Meal was given 2 hours postdose. Blood samples for determination of active GLP-1 concentration were collected (4 hours postmeal) on Day 2 in each treatment period. (NCT00830076)
Timeframe: 6 hours postdose (4 hours postmeal) on Day 2

Interventionpicomolar (Least Squares Mean)
Sitagliptin + placebo metforminMetformin + placebo sitagliptinSitagliptin + metforminPlacebo sitagliptin + placebo metformin
All Participants6.004.097.221.55

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β-cell Sensitivity

"β-cell sensitivity was defined as the incremental post-prandial~4-hour area under the curve (AUC) for insulin secretion rate (ISR) normalized by the incremental post-prandial 4-hour plasma glucose AUC." (NCT00830076)
Timeframe: 6 hour post-dose (4 hour postmeal) on Day 2

Intervention(ng/min)/(mg/dL)*10^ -3 (Least Squares Mean)
Sitagliptin + placebo metformin, n=17Metformin + placebo sitagliptin, n=17Sitagliptin + metformin, n=18Placebo sitagliptin + placebo metformin, n=18
All Participants19.5025.7126.3915.44

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Incremental Post-prandial 4-hour Weighted Mean Plasma Glucose Concentrations

Meal was given 2 hours postdose. Blood samples for determination of glucose concentration were collected (4 hours postmeal) on Day 2 in each treatment period. (NCT00830076)
Timeframe: 6 hours postdose (4 hours postmeal) on Day 2

Interventionmg/dL (Least Squares Mean)
Sitagliptin + placebo metforminMetformin + placebo sitagliptinSitagliptin + metforminPlacebo sitagliptin + placebo metformin
All Participants42.3029.3320.0251.02

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Change From Baseline in A1C at Week 24

"Week 24 A1C minus baseline (Week 0) A1C. The unit for A1C is percent. Thus, this measure represents a difference of percent values." (NCT00832390)
Timeframe: Baseline and 24 Weeks

InterventionPercent Difference (Mean)
Sitagliptin 100 mg q.d. (Once Daily)-0.2
Sitagliptin 100 mg q.d. (Once Daily) and Metformin-1.0
Standard Care Regimen0.0

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Change From Baseline in HbA1c at Week 12

HbA1c is measured as percent. Thus, this change from baseline reflects the Week 12 HbA1c percent minus the Week 0 HbA1c percent (NCT00833027)
Timeframe: Baseline and Week 12

InterventionPercent (Mean)
Sitagliptin 100mg-0.6

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Change From Baseline in HbA1c at Week 24

HbA1c is measured as percent. Thus, this change from baseline reflects the Week 24 HbA1c percent minus the Week 0 HbA1c percent (NCT00833027)
Timeframe: Baseline and Week 24

InterventionPercent (Mean)
Sitagliptin 100mg-0.6

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Change From Baseline in 2-hour Postprandial Glucose at Week 12

Change from baseline measurement, where the baseline measurement was obtained at randomization (Week 0) before receiving study medication. (NCT00837577)
Timeframe: Baseline and Week 12

Interventionmg/dL (Least Squares Mean)
Sitagliptin/Sitagliptin-55.3
Placebo/Sitagliptin-4.0

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Change From Baseline in Hemoglobin A1c (HbA1c) at Week 12

Change from baseline measurement, where the baseline measurement was obtained at randomization (Week 0) before receiving study medication. This study used Japan Diabetes Society (JDS)-certified HbA1c values, the standard at the time when the study was conducted (HbA1c [National Glycohemoglobin Standardization Program; NGSP] = HbA1c (JDS-HbA1c [%]) + 0.4%). (NCT00837577)
Timeframe: Baseline and Week 12

InterventionPercentage of glycosylated hemoglobin (Least Squares Mean)
Sitagliptin/Sitagliptin-0.76
Placebo/Sitagliptin0.16

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 12

Change from baseline measurement, where the baseline measurement was obtained at randomization (Week 0) before receiving study medication. (NCT00837577)
Timeframe: Baseline and Week 12

Interventionmg/dL (Least Squares Mean)
Sitagliptin/Sitagliptin-22.6
Placebo/Sitagliptin-0.1

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Change in Insulin Dose

(NCT00837759)
Timeframe: 6 months following the protocol subject's randomization/treatment initiation

InterventionU/kg/day (Mean)
T1D Group0.02

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Change in C-peptide

(NCT00837759)
Timeframe: 6 months following the protocol subject's randomization/treatment initiation

Interventionng/mL (Mean)
T1D Group0.51

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Change in Anti-IA2 Titer

(NCT00837759)
Timeframe: 6 months following the protocol subject's randomization/treatment initiation

InterventionTiters (Mean)
T1D Group-29212

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Change in Anti-GAD Autoantibody Titers

(NCT00837759)
Timeframe: 6 months following the protocol subject's randomization/treatment initiation

InterventionTiters (Mean)
T1D Group119278

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Glycemia Control (Change in HbA1c Level)

(NCT00837759)
Timeframe: 6 months following the protocol subject's randomization/treatment initiation

InterventionPercentage (Mean)
T1D Group-1.17

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Change in ZnT8 Autoantibody Titer

(NCT00837759)
Timeframe: 6 months following the protocol subject's randomization/treatment initiation

InterventionTiters (Mean)
T1D Group-0.11

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Time to Hyperglycemia Rescue

Participants who experienced persistent hyperglycemia (high blood glucose) could have qualified for hyperglycemia rescue.The conditions for hyperglycemic rescue were as follows: FPG >=280 milligrams/deciliter (mg/dL) between >=Week 2 and =250 mg/dL between >=Week 4 and =8.5% and a <=0.5% reduction from Baseline between >=Week 12 and =8.5% between >=Week 24 and =8.0% between >= Week 48 and NCT00838903)
Timeframe: From the start of study medication until the end of the treatment (up to Week 156)

InterventionWeeks (Median)
Placebo Plus Metformin67.71
Sitagliptin 100 mg Plus MetforminNA
Glimepiride 2 mg Plus MetforminNA
Albiglutide 30 mg Plus MetforminNA

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Number of Participants Who Achieved Clinically Meaningful HbA1c Response Levels of <6.5%, <7%, and <7.5% at Week 104

The number of participants who achieved the HbA1c treatment goal (i.e., HbA1c response levels of <6.5%, <7%, and <7.5% at Week 52) were assessed. (NCT00838903)
Timeframe: Week 104

,,,
InterventionParticipants (Number)
HbA1c <6.5%HbA1c <7.0%HbA1c <7.5%
Albiglutide 30 mg Plus Metformin50113172
Glimepiride 2 mg Plus Metformin4094147
Placebo Plus Metformin71527
Sitagliptin 100 mg Plus Metformin4594132

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Number of Participants Who Achieved Clinically Meaningful HbA1c Response Levels of <6.5%, <7%, and <7.5% at Week 156

The number of participants who achieved the HbA1c treatment goal (i.e., HbA1c response levels of <6.5%, <7%, and <7.5% at Week 156) were assessed. (NCT00838903)
Timeframe: Week 156

,,,
InterventionParticipants (Number)
HbA1c <6.5%HbA1c <7.0%HbA1c <7.5%
Albiglutide 30 mg Plus Metformin316990
Glimepiride 2 mg Plus Metformin154469
Placebo Plus Metformin4713
Sitagliptin 100 mg Plus Metformin234469

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Change From Baseline (BL) in Glycosylated Hemoglobin (HbA1c) at Week 104

HbA1c is a form of hemoglobin that is measured primarily to identify the average plasma glucose concentration over a 2- to 3-month period. The BL HbA1c value is defined as the last non-missing value before the start of treatment. Change from BL was calculated as the value at Week 104 minus the value at BL. Based on analysis of covariance (ANCOVA): change = treatment + BL HbA1c + prior myocardial infarction history + age category + region. Difference of least squares means (albiglutide - placebo, albiglutide - sitagliptin, albiglutide - glimepiride) is from the ANCOVA model. The last observation carried forward (LOCF) method was used to impute missing post-Baseline HbA1c values; the last non-missing post-BL on-treatment measurement was used to impute the missing measurement. HbA1c values obtained after hyperglycemic rescue were treated as missing and were replaced with pre-rescue values. (NCT00838903)
Timeframe: Baseline and Week 104

InterventionPercentage of HbA1c in the blood (Least Squares Mean)
Placebo Plus Metformin0.27
Sitagliptin 100 mg Plus Metformin-0.28
Glimepiride 2 mg Plus Metformin-0.36
Albiglutide 30 mg Plus Metformin-0.63

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Change From Baseline in Body Weight at Week 104

The Baseline value is the last non-missing value before the start of treatment. Change from Baseline was calculated as the post-Baseline weight minus the Baseline weight. The LOCF method was used to impute missing post-Baseline weight values. Weight values obtained after hyperglycemia rescue were treated as missing and replaced with prerescue values. Based on ANCOVA: change = treatment + Baseline weight + Baseline HbA1c category + prior myocardial infarction history + age category + region. (NCT00838903)
Timeframe: Baseline and Week 104

InterventionKilograms (Least Squares Mean)
Placebo Plus Metformin-1.00
Sitagliptin 100 mg Plus Metformin-0.86
Glimepiride 2 mg Plus Metformin1.17
Albiglutide 30 mg Plus Metformin-1.21

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Change From Baseline in Body Weight at Week 156

The Baseline value is the last non-missing value before the start of treatment. Change from Baseline was calculated as the post-Baseline weight minus the Baseline weight. This analysis used observed body weight values excluding those obtained after hyperglycemia rescue; no missing data imputation was performed. (NCT00838903)
Timeframe: Baseline and Week 156

InterventionKilograms (Mean)
Placebo Plus Metformin-3.61
Sitagliptin 100 mg Plus Metformin-2.05
Glimepiride 2 mg Plus Metformin0.98
Albiglutide 30 mg Plus Metformin-2.31

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 104

The FPG test measures blood sugar levels after the participant has not eaten (fasted) for 12 to 14 hours. The Baseline FPG value is the last non-missing value before the start of treatment. The LOCF method was used to impute missing post-Baseline FPG values. FPG values obtained after hyperglycemia rescue were treated as missing and replaced with pre-rescue values. Change from Baseline was calculated as the post-Baseline value minus the Baseline value. Based on ANCOVA: change = treatment + Baseline FPG + Baseline HbA1c category + prior myocardial infarction history + age category + region. (NCT00838903)
Timeframe: Baseline and Week 104

InterventionMillimoles per liter (mmol/L) (Least Squares Mean)
Placebo Plus Metformin0.55
Sitagliptin 100 mg Plus Metformin-0.12
Glimepiride 2 mg Plus Metformin-0.41
Albiglutide 30 mg Plus Metformin-0.98

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Change From Baseline in FPG at Week 156

The FPG test measures blood sugar levels after the participant has not eaten (fasted) for 12 to 14 hours. The Baseline FPG value is the last non-missing value before the start of treatment. Change from Baseline was calculated as the post-Baseline value minus the Baseline value. This analysis used observed FPG values excluding those obtained after hyperglycemia rescue; no missing data imputation was performed. (NCT00838903)
Timeframe: Baseline and Week 156

InterventionMillimoles per liter (mmol/L) (Mean)
Placebo Plus Metformin-0.11
Sitagliptin 100 mg Plus Metformin-0.50
Glimepiride 2 mg Plus Metformin-0.71
Albiglutide 30 mg Plus Metformin-1.30

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Change From Baseline in HbA1c at Week 156

HbA1c is a form of hemoglobin that is measured primarily to identify the average plasma glucose concentration over a 2- to 3-month period. Baseline HbA1c value is defined as the last non-missing value before the start of treatment. Change from Baseline was calculated as the post-Baseline value minus the Baseline value. This analysis used observed HbA1c values, excluding those obtained after hyperglycemia rescue; no missing data imputation was performed . (NCT00838903)
Timeframe: Baseline and Week 156

InterventionPercentage of HbA1c in the blood (Mean)
Placebo Plus Metformin-0.46
Sitagliptin 100 mg Plus Metformin-0.56
Glimepiride 2 mg Plus Metformin-0.59
Albiglutide 30 mg Plus Metformin-0.88

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HbA1c: Change From Baseline to Study Endpoint

Change = study endpoint - baseline (NCT00851903)
Timeframe: baseline, study endpoint: week 12 or earlier in case of premature discontinuation

Interventionpercent (Mean)
Combination Insulin Glargine and Sitagliptin-0.80

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HbA1c Response Rate: Percentage of Patients Achieving Glycosylated Haemoglobin A1c (HbA1c) < 7% at Study Endpoint (End of Treatment Period)

(NCT00851903)
Timeframe: study endpoint: week 12 or earlier in case of premature discontinuation

Interventionpercentage of participants (Number)
Combination Insulin Glargine and Sitagliptin51.9

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Number of Patients With at Least One Episode of Symptomatic Hypoglycemia

Symptomatic hypoglycemia was defined as an event with clinical symptoms that were considered to result from hypoglycemia confirmed or not by a plasma glucose measurement <= 70mg/dL [3.9 mmol/L] (NCT00851903)
Timeframe: During the treatment period (12 weeks) plus 7 days after last dose

Interventionparticipants (Number)
Combination Insulin Glargine and Sitagliptin40

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Change in Body Weight From Baseline to Study Endpoint

Change = study endpoint - baseline (NCT00851903)
Timeframe: baseline, study endpoint: week 12 or week 8 or week 4 depending on last available value

Interventionkg (Mean)
Combination Insulin Glargine and Sitagliptin1.15

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Self-Monitored Fasting Plasma Glucose (SMFPG) Mean : Change From Baseline to Study Endpoint

"SMFPG mean = mean of the fasting plasma glucose values recorded on the 6 consecutive days before the visit (at least 3 values needed).~Change = study endpoint - baseline." (NCT00851903)
Timeframe: baseline, study endpoint: week 12 or week 8 if value not available at week 12

Interventionmg/dL (Mean)
Combination Insulin Glargine and Sitagliptin-35.43

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7-point Plasma Glucose Profile: Change From Baseline to Study Endpoint

"7-point plasma glucose recorded before and after breakfast, before and after lunch, before and after dinner and at bedtime.~Change = study endpoint - baseline." (NCT00851903)
Timeframe: baseline, study endpoint: week 12 or week 8 if value not available at week 12

Interventionmg/dL (Mean)
Before breakfast (N=104)After breakfast (N=103)Before lunch (N=104)After lunch (N=104)Before dinner (N=103)After dinner (N=100)At bedtime (N=93)
Combination Insulin Glargine and Sitagliptin-34.2-34.1-26.6-26.5-25.1-24.9-35.2

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Insulin Dose

Daily dose at the face-to-face visits (NCT00851903)
Timeframe: baseline, week 4, week 8, week 12

Interventionunit per kg body weight (Mean)
BaselineWeek 4 N=110Week 8 N=110Week 12
Combination Insulin Glargine and Sitagliptin0.280.370.420.46

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Adjusted Percent Change in Bone Mineral Density (BMD) at Total Hip

To assess the effect of dapagliflozin 10 mg daily in combination with metformin compared to placebo in combination with metformin after 102 weeks of double-blind treatment on Bone Mineral Density at total hip as measured by Dual Energy X-ray Absorptiometry. (NCT00855166)
Timeframe: Baseline to Week 102

InterventionPercent (Least Squares Mean)
Placebo Plus Metformin-0.37
Dapagliflozin Plus Metformin-0.82

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Proportion of Participants With Body Weight Decrease ≥5%

To assess the effect of dapagliflozin 10 mg daily in combination with metformin compared to placebo in combination with metformin after 24 weeks of double-blind treatment on body weight decrease ≥5%. Least Squares Mean represents the percent of participants adjusted for body weight baseline value. (NCT00855166)
Timeframe: Baseline to Week 24

InterventionPercentage of participants (Least Squares Mean)
Placebo Plus Metformin4.3
Dapagliflozin Plus Metformin30.6

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Adjusted Mean Change in Waist Circumference

To assess the effect of dapagliflozin 10 mg daily in combination with metformin compared to placebo in combination with metformin after 24 weeks of double-blind treatment on waist circumference. (NCT00855166)
Timeframe: Baseline to Week 24

Interventioncm (Least Squares Mean)
Placebo Plus Metformin-0.99
Dapagliflozin Plus Metformin-2.51

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Adjusted Percent Change in Bone Mineral Density (BMD) at Lumbar Spine (L1-4)

To assess the effect of dapagliflozin 10 mg daily in combination with metformin compared to placebo in combination with metformin after 102 weeks of double-blind treatment on Bone Mineral Density at lumbar spine (L1-4) as measured by Dual Energy X-ray Absorptiometry. (NCT00855166)
Timeframe: Baseline to Week 102

InterventionPercent (Least Squares Mean)
Placebo Plus Metformin0.47
Dapagliflozin Plus Metformin0.69

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Adjusted Mean Change in Body Fat Mass

To assess the effect of dapagliflozin 10 mg daily in combination with metformin compared to placebo in combination with metformin after 24 weeks of double-blind treatment on total body fat mass measured by dual energy X-ray absorptiometry. (NCT00855166)
Timeframe: Baseline to Week 24

Interventionkg (Least Squares Mean)
Placebo Plus Metformin-0.74
Dapagliflozin Plus Metformin-2.22

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Adjusted Mean Change in Total Body Weight

To evaluate the effect of dapagliflozin 10 mg daily in combination with metformin compared to placebo in combination with metformin on total body weight after 24 weeks of oral administration of double-blind treatment. (NCT00855166)
Timeframe: Baseline to Week 24

Interventionkg (Least Squares Mean)
Placebo Plus Metformin-0.88
Dapagliflozin Plus Metformin-2.96

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Adjusted Percent Change in Bone Mineral Density (BMD) at Femoral Neck

To assess the effect of dapagliflozin 10 mg daily in combination with metformin compared to placebo in combination with metformin after 102 weeks of double-blind treatment on Bone Mineral Density at femoral neck as measured by Dual Energy X-ray Absorptiometry. (NCT00855166)
Timeframe: Baseline to Week 102

InterventionPercent (Least Squares Mean)
Placebo Plus Metformin0.09
Dapagliflozin Plus Metformin-0.85

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Time to Platelet Engraftment

Time to platelet engraftment will be analyzed by the Kaplan-Meier method. The time to engraftment of platelets is defined as the time from day 0 to the first of seven consecutive days after transplantation during which the platelet count is at least 20 x109/l without transfusion support. Only patients who achieved engraftment of platelets will be included in the analysis. The median and 95% confidence intervals will be provided. (NCT00862719)
Timeframe: Transplant (Day 0) up to 1 year

Interventiondays (Median)
Red Cell-Depleted (RCD) - 600 mg Sitagliptin/24 Hrs77
Red Cell-Replete, Plasma-Depleted (PD) - 600 mg Sitagliptin/2491
600 mg Sitagliptin/12 HrsNA
600 mg Sitagliptin/8 HrsNA

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Cumulative Incidence of Patients With Engraftment by Day +30 Following Transplant

Evaluate the efficacy of CD26/DPP-IV inhibition in increasing the cumulative incidence of adult patients with hematological malignancies engrafting by day +30 following transplantation of UCB by 30 percent. The cumulative incidence of patients achieving this will be reported. The value of the estimate will be from bootstrapping 1000 samples with replacement of the data and the 95% confidence interval will be calculated using the percentile method. (NCT00862719)
Timeframe: Transplant (Day 0) through Day +30

Interventionpercentage of participants (Number)
Red Cell-Depleted (RCD) - 600 mg Sitagliptin/24 Hrs88

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Time to Neutrophil Engraftment

Time to neutrophil engraftment will be analyzed by the Kaplan-Meier method. The time to engraftment of neutrophils is defined as the time from day 0 to the date of the first of three consecutive days after transplantation during which the absolute neutrophils count (ANC) is at least 0.5 x109/l. Patients who did not have neutrophil engraftment before death will be censored at the date of death. The median and 95% confidence intervals will be provided. For the RCD group, all patients engrafted before day +30, except one patient who died at day 28 before engraftment. For the PD group, all patients engrafted before day +100, except one patient who died on day +103 before engraftment. For the 600 mg sitagliptin/12 hours group, two patients engrafted before day +100, and the other two patients died before day +100 before engraftment. The one patient on 600 mg sitagliptin/8 hours died on day +14 before engraftment. (NCT00862719)
Timeframe: Transplant (Day 0) up to 1 year

Interventiondays (Median)
Red Cell-Depleted (RCD) - 600 mg Sitagliptin/24 Hrs21
Red Cell-Replete, Plasma-Depleted (PD) - 600 mg Sitagliptin/2435
600 mg Sitagliptin/12 Hrs51
600 mg Sitagliptin/8 Hrs14

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Change in Triglycerides (mmol/L)

Change in triglycerides from baseline to endpoint (Week 20) (NCT00870194)
Timeframe: Baseline to 20 Weeks

Interventionmmol/L (Least Squares Mean)
Exenatide + Placebo0.17
Exenatide + Sitagliptin-0.07

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Change in Total Cholesterol (mmol/L)

Change in total cholesterol from baseline to endpoint (Week 20) (NCT00870194)
Timeframe: Baseline to 20 Weeks

Interventionmmol/L (Least Squares Mean)
Exenatide + Placebo0.09
Exenatide + Sitagliptin0.08

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Change in LDL (mmol/L)

Change in low-density lipoprotein (LDL) cholesterol from baseline to endpoint (Week 20) (NCT00870194)
Timeframe: Baseline to 20 Weeks

Interventionmmol/L (Least Squares Mean)
Exenatide + Placebo0.06
Exenatide + Sitagliptin0.10

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Change in HDL (mmol/L)

Change in high-density lipoprotein (HDL) cholesterol from baseline to endpoint (Week 20) (NCT00870194)
Timeframe: Baseline to 20 Weeks

Interventionmmol/L (Least Squares Mean)
Exenatide + Placebo-0.03
Exenatide + Sitagliptin-0.01

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Change in FSG (mmol/L)

Change in fasting serum glucose (FSG) from baseline to endpoint (Week 20) (NCT00870194)
Timeframe: Baseline to 20 Weeks

Interventionmmol/L (Least Squares Mean)
Exenatide + Placebo0.06
Exenatide + Sitagliptin-0.55

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Change in Body Weight (kg)

Change in body weight from baseline to endpoint (Week 20) (NCT00870194)
Timeframe: Baseline to 20 Weeks

Interventionkg (Least Squares Mean)
Exenatide + Placebo-2.58
Exenatide + Sitagliptin-2.20

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Percentage of Patients Achieving HbA1c <=6.5%

Percentage of patients whose baseline HbA1c was > 6.5% achieving HbA1c <=6.5% at endpoint (Week 20) (NCT00870194)
Timeframe: Baseline to 20 Weeks

InterventionPercentage (Number)
Exenatide + Placebo16.5
Exenatide + Sitagliptin20.7

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Percentage of Patients Achieving HbA1c <=7.0%

Percentage of patients whose baseline HbA1c was > 7.0% achieving HbA1c <=7.0% at endpoint (Week 20) (NCT00870194)
Timeframe: Baseline to 20 Weeks

InterventionPercentage (Number)
Exenatide + Placebo29.5
Exenatide + Sitagliptin44.3

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Percentage of Patients Achieving HbA1c <7.0%

Percentage of patients whose baseline HbA1c was >=7.0% achieving HbA1c <7.0% at endpoint (Week 20) (NCT00870194)
Timeframe: Baseline to 20 Weeks

InterventionPercentage (Number)
Exenatide + Placebo26.6
Exenatide + Sitagliptin41.7

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SMBG (mmol/L)

7 point Self Monitored Blood Glucose Profiles - daily mean value (Week 20) (NCT00870194)
Timeframe: Baseline to 20 Weeks

Interventionmmol/L (Least Squares Mean)
Exenatide + Placebo8.57
Exenatide + Sitagliptin8.16

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Waist-to-Hip Ratio

Change in waist-to-hip ratio from baseline to endpoint (Week20) (NCT00870194)
Timeframe: Baseline to 20 Weeks

InterventionRatio (Least Squares Mean)
Exenatide + Placebo-0.01
Exenatide + Sitagliptin-0.00

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Incidence of Nocturnal Hypoglycemia (Overall)

Incidence of nocturnal hypoglycemia experienced overall during the study (NCT00870194)
Timeframe: Baseline to 20 Weeks

InterventionParticipants (Number)
Exenatide + Placebo0
Exenatide + Sitagliptin3

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Incidence of Hypoglycemia (Overall)

Incidence of hypoglycemic episodes experienced overall during the study (NCT00870194)
Timeframe: Baseline to 20 Weeks

InterventionParticipants (Number)
Exenatide + Placebo5
Exenatide + Sitagliptin10

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Change in Waist Circumference (cm)

Change in waist circumference from baseline to endpoint (Week 20) (NCT00870194)
Timeframe: Baseline to 20 Weeks

Interventioncm (Least Squares Mean)
Exenatide + Placebo-3.25
Exenatide + Sitagliptin-2.36

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Incidence of Confirmed Hypoglycemia(Overall)

Incidence of confirmed hypoglycemia experienced overall during the study (NCT00870194)
Timeframe: Baseline to 20 Weeks

InterventionParticipants (Number)
Exenatide + Placebo1
Exenatide + Sitagliptin2

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Change in HbA1c (Percent)

Change in HbA1c from baseline to endpoint (Week 20); difference of base percent values [X% - Y%] (NCT00870194)
Timeframe: Baseline to 20 Weeks

InterventionPercent HbA1c (Least Squares Mean)
Exenatide + Placebo-0.38
Exenatide + Sitagliptin-0.68

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Incidence of Severe Hypoglycemia(Overall)

Incidence of severe hypoglycemia experienced overall during the study (NCT00870194)
Timeframe: Baseline to 20 Weeks

InterventionParticipants (Number)
Exenatide + Placebo1
Exenatide + Sitagliptin0

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Change From Baseline in HbA1c Over Time

Baseline source: before first intake of active treatment (preceding trial or Open label extension) (NCT00881530)
Timeframe: Weeks 1, 6, 18, 30, 42, 54, 66 and 78

,,,,,
Interventionpercentage of HbA1c (Mean)
Week 6 (N=104, 108, 55, 162, 163, 54)Week 18 (N=93, 105, 53, 149, 157, 48)Week 30 (N=93, 99, 50, 140, 151, 45)Week 42 (N=85, 93, 46, 132, 140, 44)Week 54 (N=78, 85, 44, 128, 136, 41)Week 66 (N=80, 87, 43, 120, 127, 39)Week 78 (N=72, 84, 42, 115, 121, 38)
Empagliflozin 10 mg-0.40-0.58-0.47-0.59-0.66-0.55-0.50
Empagliflozin 10 mg + Metformin-0.36-0.51-0.58-0.65-0.62-0.59-0.56
Empagliflozin 25 mg-0.57-0.72-0.61-0.74-0.71-0.71-0.55
Empagliflozin 25 mg + Metformin-0.55-0.70-0.76-0.79-0.75-0.73-0.71
Metformin-1.03-0.92-0.95-1.10-1.13-1.04-0.80
Sitaglipin + Metformin-0.75-0.79-0.68-0.51-0.79-0.78-0.66

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Clinical Relevant Abnormalities for Physical Examination, Vital Signs, ECG and Laboratory Measurements

Clinical Relevant Abnormalities for Physical Examination, Vital Signs, ECG and Laboratory Measurements. New abnormal findings or worsening of baseline conditions were reported as treatment related Adverse Events. (NCT00881530)
Timeframe: 78 weeks plus 1 week of follow-up

,,,,,
Interventionpercentage of participants (Number)
Alanine aminotransferase increasedAspartate aminotransferase increasedGamma-glutamyltransferase increasedBlood alkaline phosphatase increasedBlood creatine phosphokinase increasedGranulocyte count decreasedHepatic enzyme increasedBlood creatinine increasedCreatinine renal clearance decreasedWeight decreasedSick sinus syndromeTachycardia
Empagliflozin 10 mg0.91.90.90.90.90.90.00.90.00.00.90.9
Empagliflozin 10 mg + Metformin0.60.00.00.00.00.00.60.00.60.00.00.6
Empagliflozin 25 mg0.90.00.00.00.00.00.90.90.00.90.01.8
Empagliflozin 25 mg + Metformin0.60.61.20.00.00.00.00.60.00.60.00.6
Metformin3.61.81.80.00.00.00.00.00.00.00.00.0
Sitaglipin + Metformin1.80.00.00.00.00.00.00.00.00.00.00.0

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Occurence of a Treat-to-target Response (HbA1c < 7.0%)

Occurence of a treat-to-target response, defined as HbA1c < 7.0% over time (NCT00881530)
Timeframe: Weeks 1, 6, 18, 30, 42, 54, 66 and 78

,,,,,
Interventionpercentage of participants (Number)
Week 6 (N=104, 108, 55, 162, 163, 54)Week 18 (N=93, 105, 53, 149, 157, 48)Week 30 (N=93, 99, 50, 140, 151, 45)Week 42 (N=85, 93, 46, 132, 140, 44)Week 54 (N=78, 85, 44, 128, 136, 41)Week 66 (N=80, 87, 43, 120, 127, 39)Week 78 (N=72, 84, 42, 115, 121, 38)
Empagliflozin 10 mg26.933.334.441.243.631.331.9
Empagliflozin 10 mg + Metformin24.131.528.639.435.935.827.0
Empagliflozin 25 mg25.033.329.340.932.939.132.1
Empagliflozin 25 mg + Metformin25.237.645.747.147.848.044.6
Metformin45.545.342.052.256.844.231.0
Sitaglipin + Metformin35.235.428.925.029.338.536.8

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Occurrence of a Relative Efficacy Response

Occurrence of a Relative Efficacy Response (HbA1c Lowered by at least >=0.5% over time) (NCT00881530)
Timeframe: Weeks 1, 6, 18, 30, 42, 54, 66 and 78

,,,,,
Interventionpercentage of participants (Number)
Week 6 (N=104, 108, 55, 162, 163, 54)Week 18 (N=93, 105, 53, 149, 157, 48)Week 30 (N=93, 99, 50, 140, 151, 45)Week 42 (N=85, 93, 46, 132, 140, 44)Week 54 (N=78, 85, 44, 128, 136, 41)Week 66 (N=80, 87, 43, 120, 127, 39)Week 78 (N=72, 84, 42, 115, 121, 38)
Empagliflozin 10 mg42.351.650.558.862.853.850.0
Empagliflozin 10 mg + Metformin41.453.755.062.159.455.056.5
Empagliflozin 25 mg50.961.955.660.258.856.350.0
Empagliflozin 25 mg + Metformin56.461.863.666.465.464.664.5
Metformin80.077.478.082.681.876.766.7
Sitaglipin + Metformin63.066.768.954.558.566.760.5

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Change From Baseline to Week 78 in Lipid Parameters

Change from baseline to week 78 in lipid parameters (Total cholesterol, High-density lipoprotein (HDL), Low-density lipoprotein (LDL) and Triglyceride) (NCT00881530)
Timeframe: Weeks 1 and 78

,,,,,
Interventionmmol/L (Mean)
Total CholesterolHDLLDL (N=102, 108, 52, 161, 159, 55)Triglyceride
Empagliflozin 10 mg-0.130.08-0.02-0.5
Empagliflozin 10 mg + Metformin0.190.060.130.1
Empagliflozin 25 mg0.090.070.05-0.0
Empagliflozin 25 mg + Metformin0.130.070.07-0.1
Metformin-0.240.06-0.13-0.5
Sitaglipin + Metformin-0.050.030.00-0.2

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Hypoglycaemic Events

"Investigator defined Hypoglycaemic events. For documentation of hypoglycemic events, the following criteria were taken into consideration:~Asymptomatic hypoglycemia: the event was not accompanied by typical symptoms of hypoglycemia but with a measured plasma glucose of ≤70 mg/dL (≤3.9 mmol/L)~Documented symptomatic hypoglycemia with glucose of ≥54 mg/dL and ≤70 mg/dL (≥3.0 mmol/L and ≤3.9 mmol/L)~Documented symptomatic hypoglycemia with glucose of <54 mg/dL (<3.0 mmol/L): the event was accompanied by typical symptoms of hypoglycemia but in no need for external assistance~Severe hypoglycemic episode: the event required the assistance of another person to actively administer carbohydrate, glucagon, or other resuscitative actions" (NCT00881530)
Timeframe: 78 weeks plus 1 week of follow-up

Interventionpercentage of participants (Number)
Empagliflozin 10 mg0.9
Empagliflozin 25 mg1.8
Metformin7.1
Empagliflozin 10 mg + Metformin2.4
Empagliflozin 25 mg + Metformin3.6
Sitaglipin + Metformin5.4

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Occurrence of a Treat-to-target Response (HbA1c < 6.5%)

Occurrence of a Treat-to-target Response, defined as HbA1c < 6.5% over time (NCT00881530)
Timeframe: Weeks 1, 6, 18, 30, 42, 54, 66 and 78

,,,,,
Interventionpercentage of participants (Number)
Week 6 (N=104, 108, 55, 162, 163, 54)Week 18 (N=93, 105, 53, 149, 157, 48)Week 30 (N=93, 99, 50, 140, 151, 45)Week 42 (N=85, 93, 46, 132, 140, 44)Week 54 (N=78, 85, 44, 128, 136, 41)Week 66 (N=80, 87, 43, 120, 127, 39)Week 78 (N=72, 84, 42, 115, 121, 38)
Empagliflozin 10 mg3.811.88.611.811.510.06.9
Empagliflozin 10 mg + Metformin6.24.78.610.610.98.310.4
Empagliflozin 25 mg11.112.410.110.85.911.58.3
Empagliflozin 25 mg + Metformin6.75.110.621.415.412.613.2
Metformin16.413.214.021.718.214.09.5
Sitaglipin + Metformin11.112.54.49.19.815.418.4

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Change From Baseline in Fasting Plasma Glucose (FPG) Over Time

Baseline source: before first intake of active treatment (preceding trial or Open label extension) (NCT00881530)
Timeframe: Weeks 1, 6, 18, 30, 42, 54, 66 and 78

,,,,,
Interventionmg/dL (Mean)
Week 6 (N=102, 108, 55, 156, 160, 53)Week 18 (N=94, 103, 51, 144, 153, 45)Week 30 (N=92, 101, 51, 133, 147, 43)Week 42 (N=85, 93, 46, 126, 140, 42)Week 54 (N=80, 88, 44, 124, 134, 39)Week 66 (N=80, 86, 43, 116, 125, 38)Week 78 (N=72, 84, 43, 112, 121, 36)
Empagliflozin 10 mg-30.6-35.5-32.3-35.8-32.1-28.0-27.9
Empagliflozin 10 mg + Metformin-25.7-30.6-29.9-30.8-28.2-21.7-24.7
Empagliflozin 25 mg-35.8-33.7-35.0-31.3-31.0-28.6-25.4
Empagliflozin 25 mg + Metformin-36.7-37.6-37.9-36.8-36.8-29.6-31.9
Metformin-29.9-30.4-28.5-31.0-31.8-26.4-22.9
Sitaglipin + Metformin-32.6-16.7-25.6-18.5-29.4-32.5-25.7

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Change From Baseline in 2-Hour Post-Meal Glucose (PMG) at Week 26

Change from baseline reflects the Week 26 value minus the baseline value. (NCT00885352)
Timeframe: Baseline and Week 26

Interventionmg/dL (Least Squares Mean)
Sitagliptin-54.4
Placebo-14.7

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Change From Baseline in Hemoglobin A1c (A1C) at Week 26

Change from baseline reflects the Week 26 value minus the baseline value. A1C represents the percentage of glycosylated hemoglobin. (NCT00885352)
Timeframe: Baseline and Week 26

InterventionPercent of glycosylated hemoglobin (Least Squares Mean)
Sitagliptin-1.15
Placebo-0.40

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 26

Change from baseline reflects the Week 26 value minus the baseline value. (NCT00885352)
Timeframe: Baseline and Week 26

Interventionmg/dL (Least Squares Mean)
Sitagliptin-20.3
Placebo-2.8

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Glucagon-like Peptide-1 Secretion After Meal Ingestion

Plasma GLP-1 levels will be measured during 300 min after meal ingestion for estimation of GLP-1 secretion (NCT00885638)
Timeframe: 300 min

Interventionnmol/l/min (Mean)
Placebo0.82
Sitagliptin1.24

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Insulin Secretion After Ingestion of Meal

Plasma insulin levels will be measured during 300 min after meal ingestion to estimation of insulin secretion (NCT00885638)
Timeframe: 300 min

Interventionmol/l/min (Mean)
Placebo29.6
Sitagliptin24.7

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Glucose Infusion Rate (GIR) During 190 - 340 Minutes Post-dose

Glucose Infusion Rate required to maintain the target glucose level of 160 milligrams / deciliter (mg/dL) ; GIR was normalized to subject's body weight (kg). (NCT00888238)
Timeframe: 190 minutes to 340 minutes

Interventionmg / kg / min (Least Squares Mean)
Sitagliptin 100 mg15.0
Placebo13.7

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Insulin Secretion Rate (ISR) During 190 - 340 Minutes Post-dose

ISR was estimated by the deconvolution of peripheral C-peptide concentrations using a 2-compartment model that utilizes population C-peptide kinetic parameters. (NCT00888238)
Timeframe: 190 minutes to 340 minutes

Interventionng/min (Least Squares Mean)
Sitagliptin 100 mg9.73
Placebo8.03

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Plasma Area Under the Curve (AUC(0 to Infinity)) for Metformin

Serum samples were used to determine the AUC from time 0 to infinity for metformin. (NCT00929201)
Timeframe: Predose and 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 16, 24, 32, 48, and 72 hours postdose

Interventionμg * hr/mL (Least Squares Mean)
Sita + Met7.65
Sita/Met FDC7.45

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Peak Plasma Concentration (Cmax) of Metformin

Serum samples were used to determine the maximum concentration for metformin. (NCT00929201)
Timeframe: Predose and 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 16, 24, 32, 48, and 72 hours postdose

Interventionng/mL (Least Squares Mean)
Sita + Met929
Sita/Met FDC887

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AUC for Glucose

Area Under the Curve for glucose after OGTT (NCT00936663)
Timeframe: 1 year

Interventionmg*hr/dl (Mean)
Sitagliptin 100 mg Daily277.5
Placebo336.5

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Hypoglycemia

Number of episodes of hypoglycemia (blood glucose less than 70 mg/dl) (NCT00936663)
Timeframe: 1 year

Interventionepisodes (Mean)
Sitagliptin 100 mg Daily0
Placebo0

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HbA1c

HbA1c at 1 year (NCT00936663)
Timeframe: 1 year

Interventionpercentage of glycated haemoglobin (Mean)
Sitagliptin 100 mg Daily6.1
Placebo5.8

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eGFR

estimated glomerular filtration rate (eGFR) at 1 year (NCT00936663)
Timeframe: 1 year

InterventionmL/min/1.73 m² (Mean)
Sitagliptin 100 mg Daily52
Placebo41.5

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AUC for Proinsulin

Area Under the Curve for Proinsulin after OGTT (NCT00936663)
Timeframe: 1 year

Interventionpmol*hr/L (Mean)
Sitagliptin 100 mg Daily62.6
Placebo44.83

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Fasting Blood Glucose

Fasting blood glucose levels at 1 year (NCT00936663)
Timeframe: 1 year

Interventionmg/dl (Mean)
Sitagliptin 100 mg Daily107
Placebo102.5

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AUC for Insulin

Area Under the Curve for insulin after OGTT (NCT00936663)
Timeframe: 1 year

Interventionmciu*hr/ml (Mean)
Sitagliptin 100 mg Daily72.5
Placebo85.75

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AUC for C Peptide

Area Under the Curve for C peptide after OGTT (NCT00936663)
Timeframe: 1 year

Interventionng*hr/ml (Mean)
Sitagliptin 100 mg Daily19.5
Placebo23.28

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Area Under the Curve (AUC(0 to Infinity)) Following Single Dose Administration of the Anhydrous and Monohydrate Forms of MK0431 (Sitagliptin)

Area Under the Plasma Concentration-Time Curve and peak concentration of the Anhydrous and Monohydrate Forms of MK0431 (Sitagliptin) (NCT00944450)
Timeframe: Through 72 Hours Following the Administration of the Medication

Interventionμmol*hr/L (Geometric Mean)
100 mg MK0431 Anhydrous8.38
100 mg MK0431 Monohydrate8.78

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Peak Plasma Concentration (Cmax) Following Single Dose Administration of the Anhydrous and Monohydrate Forms of MK0431 (Sitagliptin)

Peak Plasma concentration (Cmax) for the Anhydrous and Monohydrate Forms of MK0431 (Sitagliptin) (NCT00944450)
Timeframe: Through 72 Hours Following the Administration of the Medication

Interventionμmol/L (Geometric Mean)
100 mg MK0431 Anhydrous799
100 mg MK0431 Monohydrate856

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Change in Percent Predicted FEV1

The decline of lung function was assessed with forced expiratory volume (FEV1), which measures how much air is exhaled during one second of a forced exhale. Change is described as the difference in FEV1 at baseline subtracted from FEV1 at the end of treatment study visit. A protocol change during the study reduced the treatment time from 24 months to 12 months. The end of treatment study visit for participants in the early part of the study occurred at 24 months, while the end of treatment visit was a 12 months for participants enrolling later. Negative values indicate a decline in lung function over the course of the study. (NCT00967798)
Timeframe: Baseline, end of treatment (Month 12 or Month 24)

Interventionpercent predicted (Mean)
Sitagliptin-9.7
Placebo-8.5

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Absolute Change From Baseline in HbA1c at Week 24

Absolute change = HbA1c value at Week 24 minus HbA1c value at baseline. The on-treatment period for this efficacy variable is the time from the first dose of study drug up to 3 days after the last dose of study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Baseline, Week 24

Interventionpercentage of hemoglobin (Least Squares Mean)
Lixisenatide-0.66
Sitagliptin-0.72

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Change From Baseline in Glucose Excursion at Week 24

Glucose excursion = 2-hour PPG minus plasma glucose 30 minutes prior to the standardized meal test, before study drug administration. Change was calculated by subtracting baseline value from Week 24 value. The on-treatment period for this efficacy variable is the time from the first dose of study drug up to the last dosing day of the study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Baseline, Week 24

Interventionmmol/L (Least Squares Mean)
Lixisenatide-2.55
Sitagliptin-0.42

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Percentage of Patients With Glycosylated Hemoglobin (HbA1c) Level Less Than 7% and at Least 5% Weight Loss From Baseline at Week 24

Percentage of patients who met both criteria (HbA1c <7% at Week 24 and at least 5% weight loss from baseline at Week 24) is reported. The on-treatment period for this efficacy variable is the time from the first dose of study drug up to 3 days after the last dose of study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Week 24

Interventionpercentage of participants (Number)
Lixisenatide12.0
Sitagliptin7.5

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24

Change was calculated by subtracting baseline value from Week 24 value. The on-treatment period for this efficacy variable is the time from the first dose of study drug up to 1 day after the last dose of study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Baseline, Week 24

Interventionmmol/L (Least Squares Mean)
Lixisenatide-0.45
Sitagliptin-0.69

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Change From Baseline in Beta Cell Function Assessed by Homeostasis Model Assessment-Beta (HOMA-beta) at Week 24

HOMA-beta was derived from FPG and FPI as: (20*FPI [micro units/milliliter]) divided by (FPG [mmol/L] minus 3.5). Change was calculated for HOMA-beta by subtracting the baseline value from Week 24 value. The on-treatment period for this efficacy variable is the time from the first dose of study drug up to the last dosing day of study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Baseline, Week 24

Interventionpercentage of normal beta cells function (Least Squares Mean)
Lixisenatide17.66
Sitagliptin17.79

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Change From Baseline in Body Weight at Week 24

Change was calculated by subtracting baseline value from Week 24 value. The on-treatment period for this efficacy variable is the time from the first dose of study drug up to 3 days after the last dose of study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Baseline, Week 24

Interventionkilogram (Least Squares Mean)
Lixisenatide-2.51
Sitagliptin-1.17

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Number of Patients With Symptomatic Hypoglycemia and Severe Symptomatic Hypoglycemia

Symptomatic hypoglycemia was an event with clinical symptoms that were considered to result from a hypoglycemic episode with an accompanying plasma glucose less than 60 mg/dL (3.3 mmol/L) or associated with prompt recovery after oral carbohydrate, intravenous glucose, or glucagon administration if no plasma glucose measurement was available. Severe symptomatic hypoglycemia was symptomatic hypoglycemia event in which the patient required the assistance of another person and was associated with either a plasma glucose level below 36 mg/dL (2.0 mmol/L) or prompt recovery after oral carbohydrate, intravenous glucose, or glucagon administration, if no plasma glucose measurement was available. (NCT00976937)
Timeframe: First dose of study drug up to 3 days after the last dose administration

,
Interventionparticipants (Number)
Symptomatic hypoglycemiaSevere symptomatic hypoglycemia
Lixisenatide10
Sitagliptin30

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Change From Baseline in Fasting Glucagon and 2-hour Postprandial Glucagon at Week 24

Change was calculated for fasting glucagon and 2-hour postprandial glucagon by subtracting the baseline value from Week 24 value. The on-treatment period for this efficacy variable is the time from the first dose of study drug up to the last dosing day of study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Baseline, Week 24

,
Interventionng/L (Least Squares Mean)
Fasting Glucagon (n=124, 138)2-hour postprandial Glucagon (n=124, 134)
Lixisenatide1.89-8.16
Sitagliptin3.52-4.38

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Percentage of Patients With at Least 5% Weight Loss From Baseline at Week 24

The on-treatment period for this efficacy variable is the time from the first dose of study drug up to 3 days after the last dose of study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Baseline, Week 24

Interventionpercentage of participants (Number)
Lixisenatide18.4
Sitagliptin11.9

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Change From Baseline in Fasting Proinsulin-to-insulin Ratio and 2-hour Postprandial Proinsulin-to-insulin Ratio at Week 24

Change was calculated by subtracting baseline value from Week 24 value. The on-treatment period for this efficacy variable is the time from the first dose of study drug up to the last dosing day of the study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Baseline, Week 24

,
Interventionratio (Least Squares Mean)
Fasting Proinsulin-to-insulin ratio (n=119, 133)2-hour PP Proinsulin-to-insulin ratio (n=123, 130)
Lixisenatide-0.08-0.01
Sitagliptin-0.17-0.05

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Change From Baseline in Fasting Proinsulin and 2-hour Postprandial Proinsulin at Week 24

Change was calculated for fasting proinsulin and 2-hour postprandial proinsulin by subtracting the baseline value from Week 24 value. The on-treatment period for this efficacy variable is the time from the first dose of the study drug up to the last dosing day of study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Baseline, Week 24

,
Interventionpmol/L (Least Squares Mean)
Fasting Proinsulin (n=125, 140)2-hour postprandial Proinsulin (n=125, 139)
Lixisenatide-2.180.28
Sitagliptin-4.84-3.95

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Change From Baseline in Fasting Plasma Insulin (FPI) and 2-hour Postprandial Plasma Insulin (PPI) at Week 24

Change was calculated for fasting plasma insulin and 2-hour post prandial plasma insulin by subtracting the baseline value from Week 24 value. The on-treatment period for this efficacy variable is the time from the first dose of study drug up to the last dosing day of the study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Baseline, Week 24

,
Interventionpmol/L (Least Squares Mean)
FPI (n=119, 133)2-hour PPI (n=123, 130)
Lixisenatide-1.70-57.81
Sitagliptin-0.88-2.85

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Change From Baseline in Fasting C-peptide and 2-hour Postprandial C-peptide at Week 24

Change was calculated for fasting C-peptide and 2-hour postprandial C-peptide by subtracting the baseline value from Week 24 value. The on-treatment period for this efficacy variable is the time from the first dose of study drug up to the last dosing day of study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Baseline, Week 24

,
Interventionnmol/L (Least Squares Mean)
Fasting C-peptide (n= 123,139)2-hour postprandial C-peptide (n=125, 139)
Lixisenatide-0.02-0.15
Sitagliptin-0.020.08

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Percentage of Patients With Glycosylated Hemoglobin (HbA1c) Level Less Than or Equal to 6.5% at Week 24

The on-treatment period for this efficacy variable is the time from the first dose of study drug up to 3 days after the last dose of study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Week 24

Interventionpercentage of participants (Number)
Lixisenatide24.0
Sitagliptin26.3

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Percentage of Patients With Glycosylated Hemoglobin (HbA1c) Level Less Than 7% at Week 24

The on-treatment period for this efficacy variable is the time from the first dose of study drug up to 3 days after the last dose of study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Week 24

Interventionpercentage of participants (Number)
Lixisenatide40.7
Sitagliptin40.0

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Change From Baseline in 2-hour Postprandial Plasma Glucose (PPG) at Week 24

The 2-hour PPG test measured blood glucose 2 hours after eating a standardized meal. Change was calculated by subtracting baseline value from Week 24 value. The on-treatment period for this efficacy variable is the time from the first dose of study drug up to the last dosing day of the study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Baseline, Week 24

Interventionmmol/L (Least Squares Mean)
Lixisenatide-3.35
Sitagliptin-1.44

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Percentage of Patients Requiring Rescue Therapy During 24-Week Period

Routine fasting self-measured plasma glucose (SMPG) and central laboratory FPG (and HbA1c after week 12) values were used to determine the requirement of rescue medication. If fasting SMPG value exceeded the specified limit for 3 consecutive days, the central laboratory FPG (and HbA1c after week 12) were performed. Threshold values - from baseline to Week 8: fasting SMPG/FPG >270 milligram/deciliter (mg/dL) (15.0 mmol/L), from Week 8 to Week 12: fasting SMPG/FPG >240 mg/dL (13.3 mmol/L), and from Week 12 to Week 24: fasting SMPG/FPG >200 mg/dL (11.1 mmol/L) or HbA1c >8.5%. (NCT00976937)
Timeframe: Baseline up to Week 24

Interventionpercentage of participants (Number)
Lixisenatide9.5
Sitagliptin6.8

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Change From Baseline in Insulin Resistance Assessed by Homeostasis Model Assessment- Insulin Resistance (HOMA-IR) at Week 24

HOMA-IR was derived from FPG and FPI as: (FPI [micro units per milliliter]*FPG [mmol/L]) divided by 22.5. Change was calculated for HOMA-IR by subtracting the baseline value from Week 24 value. The on-treatment period for this efficacy variable is the time from the first dose of study drug up to the last dosing day of study drug or up to the introduction of rescue therapy, whichever is the earliest. (NCT00976937)
Timeframe: Baseline, Week 24

InterventionmU * mmol/L^2 (Least Squares Mean)
Lixisenatide-0.52
Sitagliptin-0.57

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 30

Blood glucose was measured on a fasting basis (collected after an 8- to 10-hour fast). FPG is expressed as mg/dL. Blood was drawn at predose on Day 1 and after 30 weeks of treatment to determine change in plasma glucose levels (i.e., FPG at Week 30 minus FPG at baseline). (NCT00993187)
Timeframe: Baseline and Week 30

Interventionmg/dL (Least Squares Mean)
Sitagliptin/Metformin-47.0
Glimepiride-23.5

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Change From Baseline in Body Weight at Week 30

Change in body weight following 30 weeks of therapy (i.e., body weight at Week 30 minus body weight at baseline) (NCT00993187)
Timeframe: Baseline and Week 30

Interventionkg (Least Squares Mean)
Sitagliptin/Metformin-0.83
Glimepiride0.90

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Percentage of Participants With HbA1C < 7.0% at Week 30

HbA1C is blood marker used to report average blood glucose levels over a prolonged periods of time and is reported as a percentage (%). (NCT00993187)
Timeframe: Week 30

InterventionPercentage of Participants (Number)
Sitagliptin/Metformin81.2
Glimepiride40.1

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Percentage of Participants With One or More Episodes of Hypoglycemia

Symptomatic episodes assessed as likely to be due to hypoglycemia were reported by investigators as adverse experiences of hypoglycemia. Adverse experiences of hypoglycemia were based on all reports of hypoglycemia; a concurrent glucose measurement was not required. (NCT00993187)
Timeframe: Up to Week 30

InterventionPercentage of participants (Number)
Sitagliptin/Metformin5.5
Glimepiride20.1

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Number of Participants Who Discontinued Study Drug Due to an Adverse Event

An AE is any unfavorable and unintended change in the structure, function or chemistry of the body temporally associated with study drug administration whether or not considered related to the use of the product. (NCT00993187)
Timeframe: Up to 30 weeks

InterventionParticipants (Number)
Sitagliptin/Metformin8
Glimepiride8

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Number of Participants Who Experienced at Least One Adverse Event (AE)

An adverse event (AE) is any unfavorable and unintended change in the structure, function or chemistry of the body temporally associated with study drug administration whether or not considered related to the use of the product. (NCT00993187)
Timeframe: Up to 32 weeks

InterventionParticipants (Number)
Sitagliptin/Metformin88
Glimepiride101

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Change From Baseline in Hemoglobin A1C (HbA1C) at Week 30

HbA1C is blood marker used to report average blood glucose levels over a prolonged periods of time and is reported as a percentage (%). Change in A1C following 30 weeks of therapy (i.e., A1C at Week 30 minus A1C at baseline). (NCT00993187)
Timeframe: Baseline and Week 30

InterventionPercent of total hemoglobin (Least Squares Mean)
Sitagliptin/Metformin-1.5
Glimepiride-0.7

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Change From Baseline (i.e., Week 0 of the 24-week Base Study) in Fasting Plasma Glucose (FPG) at Week 54

Change from baseline at Week 54 is defined as Week 54 minus Week 0. (NCT01028391)
Timeframe: Baseline and Week 54

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg q.d. + Pioglitazone 45 mg q.d.-61.3
Pioglitazone 45 mg q.d.-52.8

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Change From Baseline (i.e., Week 0 of the 24-week Base Study) in Hemoglobin A1c (HbA1c) at Week 54

HbA1c is measured as percent. Thus this change from baseline reflects the Week 54 HbA1c percent minus the Week 0 HbA1c percent. (NCT01028391)
Timeframe: Baseline and 54 Weeks

InterventionPercent HbA1c (Least Squares Mean)
Sitagliptin 100 mg q.d. + Pioglitazone 45 mg q.d.-2.37
Pioglitazone 45 mg q.d.-1.86

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Safety and Tolerability of Sitagliptin After 4 Weeks of Treatment

Safety & tolerability were measured in terms of the # of participants with >=1 adverse event (AE), >=1 drug-related AE, >=1 serious AE (SAE), or discontinued treatment due to an AE. SAEs included events occurring after initiation of glycemic rescue therapy. AE is defined as any unfavorable/unintended change in structure, function, or chemistry of the body temporally associated with the use of SPONSOR's product. SAE is defined as any AE that results in death, is life-threatening, an overdose, causes or prolongs in-patient hospitalization, or considered medically significant by the investigator. (NCT01034111)
Timeframe: 4 weeks

InterventionParticipants (Number)
At least one adverse eventAt least one drug-related adverse eventAt least one serious adverse eventDiscontinued treatment due to an adverse event
Sitagliptin5500

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Change From Baseline in Fasting Plasma Glucose at Week 4

Calculated as the mean change from baseline in fasting plasma glucose at Week 4. (NCT01034111)
Timeframe: Baseline and Week 4

Interventionmmol/L (Mean)
Sitagliptin1.6

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Change in Fasting Plasma Glucose (FPG)

Change from baseline in FPG after 26 weeks of treatment (NCT01046110)
Timeframe: Week 0, Week 26

Interventionmmol/L (Mean)
IDeg OD-3.22
DPP-IV Inhibitor-1.39

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Change in Glycosylated Haemoglobin (HbA1c)

Change from baseline in HbA1c after 26 weeks of treatment (NCT01046110)
Timeframe: Week 0, Week 26

Interventionpercentage of glycosylated haemoglobin (Mean)
IDeg OD-1.56
DPP-IV Inhibitor-1.22

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Change From Baseline in Systolic Blood Pressure at Week 4

Sitting blood pressure was measured in triplicate and the average of the measurements taken at a single assessment time was analyzed. The change from baseline is the Week 4 systolic blood pressure minus the Week 0 systolic blood pressure (LOCF). (NCT01059825)
Timeframe: Baseline and Week 4

InterventionmmHg (Least Squares Mean)
Placebo-2.57
Ertugliflozin 1 mg-3.94
Ertugliflozin 5 mg-5.15
Ertugliflozin 10 mg-5.43
Ertugliflozin 25 mg-3.33
Sitagliptin 100 mg-3.32

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Change From Baseline in Systolic Blood Pressure at Week 2

Sitting blood pressure was measured in triplicate and the average of the measurements taken at a single assessment time was analyzed. The change from baseline is the Week 2 systolic blood pressure minus the Week 0 systolic blood pressure (LOCF). (NCT01059825)
Timeframe: Baseline and Week 2

InterventionmmHg (Least Squares Mean)
Placebo-1.93
Ertugliflozin 1 mg-2.30
Ertugliflozin 5 mg-4.73
Ertugliflozin 10 mg-2.28
Ertugliflozin 25 mg-5.39
Sitagliptin 100 mg-0.91

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Change From Baseline in Systolic Blood Pressure at Week 12

Sitting blood pressure was measured in triplicate and the average of the measurements taken at a single assessment time was analyzed. The change from baseline is the Week 12 systolic blood pressure minus the Week 0 systolic blood pressure (LOCF). (NCT01059825)
Timeframe: Baseline and Week 12

InterventionmmHg (Least Squares Mean)
Placebo-0.55
Ertugliflozin 1 mg-2.69
Ertugliflozin 5 mg-4.03
Ertugliflozin 10 mg-3.43
Ertugliflozin 25 mg-3.93
Sitagliptin 100 mg-1.09

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Change From Baseline in HbA1c at Week 8

HbA1c is measured as percent. The change from baseline is the Week 8 HbA1c percent minus the Week 0 HbA1c percent (LOCF). (NCT01059825)
Timeframe: Baseline and Week 8

InterventionPercent (Least Squares Mean)
Placebo-0.10
Ertugliflozin 1 mg-0.57
Ertugliflozin 5 mg-0.76
Ertugliflozin 10 mg-0.73
Ertugliflozin 25 mg-0.75
Sitagliptin 100 mg-0.77

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Change From Baseline in HbA1c at Week 4

HbA1c is measured as percent. The change from baseline is the Week 4 HbA1c percent minus the Week 0 HbA1c percent (LOCF). (NCT01059825)
Timeframe: Baseline and Week 4

InterventionPercent (Least Squares Mean)
Placebo-0.04
Ertugliflozin 1 mg-0.40
Ertugliflozin 5 mg-0.49
Ertugliflozin 10 mg-0.48
Ertugliflozin 25 mg-0.40
Sitagliptin 100 mg-0.48

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Change From Baseline in HbA1C at Week 2

HbA1c is measured as percent. The change from baseline is the Week 2 HbA1c percent minus the Week 0 HbA1c percent (LOCF). (NCT01059825)
Timeframe: Baseline and Week 2

InterventionPercent (Least Squares Mean)
Placebo0.00
Ertugliflozin 1 mg-0.14
Ertugliflozin 5 mg-0.29
Ertugliflozin 10 mg-0.22
Ertugliflozin 25 mg-0.17
Sitagliptin 100 mg-0.26

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Change From Baseline in HbA1c at Week 12

HbA1c is measured as percent. The change from baseline is the Week 12 HbA1c percent minus the Week 0 HbA1c percent (last observation carried forward [LOCF]). (NCT01059825)
Timeframe: Baseline and Week 12

InterventionPercent (Least Squares Mean)
Placebo-0.11
Ertugliflozin 1 mg-0.56
Ertugliflozin 5 mg-0.80
Ertugliflozin 10 mg-0.73
Ertugliflozin 25 mg-0.83
Sitagliptin 100 mg-0.87

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Baseline Body Weight

(NCT01059825)
Timeframe: Baseline

Interventionkg (Mean)
Placebo83.78
Ertugliflozin 1 mg83.44
Ertugliflozin 5 mg85.74
Ertugliflozin 10 mg82.28
Ertugliflozin 25 mg81.81
Sitagliptin 100 mg85.52

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Percentage of Participants Achieving HbA1c <7% at Week 12

Laboratory measurements were performed after an overnight fast ≥8 hours in duration. (NCT01059825)
Timeframe: Week 12

InterventionPercentage of participants (Number)
Placebo15.6
Ertugliflozin 1 mg44.0
Ertugliflozin 5 mg42.9
Ertugliflozin 10 mg38.6
Ertugliflozin 25 mg36.2
Sitagliptin 100 mg43.1

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Baseline Hemoglobin A1c (HbA1c)

HbA1c is measured as percent. (NCT01059825)
Timeframe: Baseline

InterventionPercent (Mean)
Placebo8.08
Ertugliflozin 1 mg8.01
Ertugliflozin 5 mg7.88
Ertugliflozin 10 mg8.13
Ertugliflozin 25 mg8.30
Sitagliptin 100 mg8.24

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Percentage of Participants Achieving HbA1C <6.5% at Week 12

Laboratory measurements were performed after an overnight fast ≥8 hours in duration. (NCT01059825)
Timeframe: Week 12

InterventionPercentage of participants (Number)
Placebo6.7
Ertugliflozin 1 mg12.0
Ertugliflozin 5 mg20.4
Ertugliflozin 10 mg13.6
Ertugliflozin 25 mg14.9
Sitagliptin 100 mg25.5

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Change From Baseline in Fasting Plasma Glucose at Week 2

The change from baseline is the Week 2 FPG minus the Week 0 FPG (LOCF). Laboratory measurements were performed after an overnight fast ≥8 hours in duration. (NCT01059825)
Timeframe: Baseline and Week 2

Interventionmg/dL (Least Squares Mean)
Placebo5.89
Ertugliflozin 1 mg-15.07
Ertugliflozin 5 mg-15.68
Ertugliflozin 10 mg-26.65
Ertugliflozin 25 mg-16.44
Sitagliptin 100 mg-14.69

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Change From Baseline in Fasting Plasma Glucose at Week 8

The change from baseline is the Week 8 FPG minus the Week 0 FPG (LOCF). Laboratory measurements were performed after an overnight fast ≥8 hours in duration. (NCT01059825)
Timeframe: Baseline and Week 8

Interventionmg/dL (Least Squares Mean)
Placebo3.82
Ertugliflozin 1 mg-18.25
Ertugliflozin 5 mg-24.69
Ertugliflozin 10 mg-31.59
Ertugliflozin 25 mg-30.99
Sitagliptin 100 mg-18.93

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Change From Baseline in Fasting Plasma Glucose at Week 4

The change from baseline is the Week 4 FPG minus the Week 0 FPG (LOCF). Laboratory measurements were performed after an overnight fast ≥8 hours in duration. (NCT01059825)
Timeframe: Baseline and Week 4

Interventionmg/dL (Least Squares Mean)
Placebo5.17
Ertugliflozin 1 mg-16.91
Ertugliflozin 5 mg-22.77
Ertugliflozin 10 mg-27.95
Ertugliflozin 25 mg-26.62
Sitagliptin 100 mg-18.00

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Change From Baseline in Fasting Plasma Glucose at Week 12

The change from baseline is the Week 12 FPG minus the Week 0 fasting plasma glucose (LOCF). Laboratory measurements were performed after an overnight fast ≥8 hours in duration. (NCT01059825)
Timeframe: Baseline and Week 12

Interventionmg/dL (Least Squares Mean)
Placebo2.76
Ertugliflozin 1 mg-18.23
Ertugliflozin 5 mg-23.06
Ertugliflozin 10 mg-31.47
Ertugliflozin 25 mg-29.26
Sitagliptin 100 mg-17.29

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Change From Baseline in Diastolic Blood Pressure at Week 8

Sitting blood pressure was measured in triplicate and the average of the measurements taken at a single assessment time was analyzed. The change from baseline is the Week 8 diastolic blood pressure minus the Week 0 diastolic blood pressure (LOCF). (NCT01059825)
Timeframe: Baseline and Week 8

InterventionmmHg (Least Squares Mean)
Placebo0.80
Ertugliflozin 1 mg-1.40
Ertugliflozin 5 mg-0.69
Ertugliflozin 10 mg-2.23
Ertugliflozin 25 mg-1.20
Sitagliptin 100 mg0.32

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Change From Baseline in Diastolic Blood Pressure at Week 4

Sitting blood pressure was measured in triplicate and the average of the measurements taken at a single assessment time was analyzed. The change from baseline is the Week 4 diastolic blood pressure minus the Week 0 diastolic blood pressure (LOCF). (NCT01059825)
Timeframe: Baseline and Week 4

InterventionmmHg (Least Squares Mean)
Placebo-0.80
Ertugliflozin 1 mg-2.47
Ertugliflozin 5 mg-3.08
Ertugliflozin 10 mg-2.81
Ertugliflozin 25 mg-2.10
Sitagliptin 100 mg-0.51

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Change From Baseline in Diastolic Blood Pressure at Week 2

Sitting blood pressure was measured in triplicate and the average of the measurements taken at a single assessment time was analyzed. The change from baseline is the Week 2 diastolic blood pressure minus the Week 0 diastolic blood pressure (LOCF). (NCT01059825)
Timeframe: Baseline and Week 2

InterventionmmHg (Least Squares Mean)
Placebo-0.57
Ertugliflozin 1 mg-1.25
Ertugliflozin 5 mg-1.26
Ertugliflozin 10 mg-1.97
Ertugliflozin 25 mg-3.01
Sitagliptin 100 mg0.92

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Change From Baseline in Diastolic Blood Pressure at Week 12

Sitting blood pressure was measured in triplicate and the average of the measurements taken at a single assessment time was analyzed. The change from baseline is the Week 12 diastolic blood pressure minus the Week 0 diastolic blood pressure (LOCF). (NCT01059825)
Timeframe: Baseline and Week 12

InterventionmmHg (Least Squares Mean)
Placebo0.81
Ertugliflozin 1 mg-1.12
Ertugliflozin 5 mg-1.01
Ertugliflozin 10 mg-3.18
Ertugliflozin 25 mg-1.83
Sitagliptin 100 mg1.68

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Percent Change From Baseline in Body Weight at Week 8

The percent change from baseline is the ([Week 8 body weight minus the Week 0 body weight] divided by the Week 0 body weight) X 100 (LOCF). (NCT01059825)
Timeframe: Baseline and Week 8

InterventionPercent change (Least Squares Mean)
Placebo-0.62
Ertugliflozin 1 mg-1.65
Ertugliflozin 5 mg-2.18
Ertugliflozin 10 mg-2.30
Ertugliflozin 25 mg-2.40
Sitagliptin 100 mg-0.38

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Baseline Systolic Blood Pressure

Sitting blood pressure was measured in triplicate and the average of the measurements taken at a single assessment time was analyzed. (NCT01059825)
Timeframe: Baseline

InterventionmmHg (Mean)
Placebo126.7
Ertugliflozin 1 mg126.5
Ertugliflozin 5 mg127.9
Ertugliflozin 10 mg125.8
Ertugliflozin 25 mg124.9
Sitagliptin 100 mg126.6

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Baseline Fasting Plasma Glucose

Laboratory measurements were performed after an overnight fast ≥8 hours in duration. (NCT01059825)
Timeframe: Baseline

Interventionmg/dL (Mean)
Placebo165.3
Ertugliflozin 1 mg162.5
Ertugliflozin 5 mg156.5
Ertugliflozin 10 mg163.3
Ertugliflozin 25 mg171.3
Sitagliptin 100 mg166.2

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Baseline Diastolic Blood Pressure

Sitting blood pressure was measured in triplicate and the average of the measurements taken at a single assessment time was analyzed. (NCT01059825)
Timeframe: Baseline

InterventionmmHg (Mean)
Placebo79.14
Ertugliflozin 1 mg78.95
Ertugliflozin 5 mg78.19
Ertugliflozin 10 mg78.45
Ertugliflozin 25 mg78.61
Sitagliptin 100 mg79.15

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Percent Change From Baseline in Body Weight at Week 4

The percent change from baseline is the ([Week 4 body weight minus the Week 0 body weight] divided by the Week 0 body weight) X 100 (LOCF). (NCT01059825)
Timeframe: Baseline and Week 4

InterventionPercent change (Least Squares Mean)
Placebo-0.44
Ertugliflozin 1 mg-1.20
Ertugliflozin 5 mg-1.76
Ertugliflozin 10 mg-1.68
Ertugliflozin 25 mg-1.52
Sitagliptin 100 mg0.01

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Percent Change From Baseline in Body Weight at Week 2

The percent change from baseline is the ([Week 2 body weight minus the Week 0 body weight] divided by the Week 0 body weight) X 100 (LOCF). (NCT01059825)
Timeframe: Baseline and Week 2

InterventionPercent change (Least Squares Mean)
Placebo-0.24
Ertugliflozin 1 mg-0.65
Ertugliflozin 5 mg-1.36
Ertugliflozin 10 mg-1.14
Ertugliflozin 25 mg-1.11
Sitagliptin 100 mg0.21

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Percent Change From Baseline in Body Weight at Week 12

The percent change from baseline is the ([Week 12 body weight minus the Week 0 body weight] divided by the Week 0 body weight) X 100 (LOCF). (NCT01059825)
Timeframe: Baseline and Week 12

InterventionPercent change (Least Squares Mean)
Placebo-0.75
Ertugliflozin 1 mg-1.90
Ertugliflozin 5 mg-2.50
Ertugliflozin 10 mg-2.90
Ertugliflozin 25 mg-2.66
Sitagliptin 100 mg-0.30

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Number of Participants Who Experienced an Advere Event (AE)

An adverse event is defines as any untoward medical occurrence in a clinical investigation participant administered a product or medical device; the event need not necessarily have a causal relationship with the treatment or usage. Below table includes all data collected since the first dose of sponsor-provided metformin. (NCT01059825)
Timeframe: Up to 98 days

InterventionParticipants (Number)
Placebo29
Ertugliflozin 1 mg31
Ertugliflozin 5 mg30
Ertugliflozin 10 mg29
Ertugliflozin 25 mg28
Sitagliptin 100 mg30
Metformin Run-in82

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Number of Participants Who Discontinued Study Medication Due to an AE

An adverse event is defines as any untoward medical occurrence in a clinical investigation participant administered a product or medical device; the event need not necessarily have a causal relationship with the treatment or usage. Below table includes all data collected since the first dose of sponsor-provided metformin and excludes a temporary discontinuation of study medication. (NCT01059825)
Timeframe: Up to 84 days

InterventionParticipants (Number)
Placebo1
Ertugliflozin 1 mg1
Ertugliflozin 5 mg3
Ertugliflozin 10 mg2
Ertugliflozin 25 mg1
Sitagliptin 100 mg1
Metformin Run-in3

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Change From Baseline in Systolic Blood Pressure at Week 8

Sitting blood pressure was measured in triplicate and the average of the measurements taken at a single assessment time was analyzed. The change from baseline is the Week 8 systolic blood pressure minus the Week 0 systolic blood pressure (LOCF). (NCT01059825)
Timeframe: Baseline and Week 8

InterventionmmHg (Least Squares Mean)
Placebo-0.44
Ertugliflozin 1 mg-1.53
Ertugliflozin 5 mg-2.85
Ertugliflozin 10 mg-3.04
Ertugliflozin 25 mg-3.30
Sitagliptin 100 mg-2.43

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Percentage of Participants With an Overall Efficacy Evaluation by the Investigator of Improved, Stable, or Worse at Week 24

"Overall efficacy analysis was conducted on participants who have used study drug for more than 24 weeks and whose improvement of the disease has been assessed by Principal investigator. The investigator's global assessment of disease improvement was classified as either: Improved, Stable and Worse in a Medical History/Physical Examination form." (NCT01065766)
Timeframe: At Week 24

InterventionPercentage of participants (Number)
ImprovedStableWorse
All Participants Included in the Safety Evaluation76.3815.887.75

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Percentage of Participants With an Overall Efficacy Evaluation by the Investigator of Improved, Stable, or Worse at Week 12

"Overall efficacy analysis was conducted on participants who have used study drug for more than 12 weeks and whose improvement of the disease has been assessed by Principal investigator. The investigator's global assessment of disease improvement was classified as either: Improved, Stable and Worse in a Medical History/Physical Examination form." (NCT01065766)
Timeframe: At Week 12

InterventionPercentage of participants (Number)
ImprovedStableWorse
All Participants Included in the Safety Evaluation78.6816.384.94

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Percentage of Participants With Any Adverse Experience

An adverse event (AE) is any unfavorable and unintended change in the structure, function or chemistry of the body temporally associated with study drug administration whether or not considered related to the use of the product. (NCT01065766)
Timeframe: Up to 26 weeks

InterventionPercentage of participants (Number)
All Participants Included in the Safety Evaluation3.74

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Change From Baseline to Treatment in Hemoglobin HbA1c (A1C) at Week 12

HbA1C is found when high blood levels of glucose combines with hemoglobin to form glycated hemoglobin. The average amount of glucose in blood over a prolonged periods of time can be determined by measuring a hemoglobin A1c level which is reported as a percentage (%). The change from baseline reflects the Week 12 A1C minus Week 0 A1C. (NCT01065766)
Timeframe: Baseline and Week 12

InterventionPercentage of glycosylated hemoglobin (Mean)
All Participants Included in the Safety Evaluation-0.93

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Change From Baseline to Treatment in HbA1c at Week 24

HbA1C is blood marker used to report average blood glucose levels over a prolonged periods of time and is reported as a percentage (%). Therefore, this change from baseline reflects the Week 24 A1C minus Week 0 A1C. (NCT01065766)
Timeframe: Baseline and Week 24

InterventionPercentage of glycosylated hemoglobin (Mean)
All Participants Included in the Safety Evaluation-1.08

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Change From Baseline to Treatment in FPG at Week 24

Blood glucose was measured on a fasting basis (collected after an 8- to 10-hour fast). FPG is expressed as mg/dL. Therefore, this change from baseline reflects the Week 24 FPG minus Week 0 FPG. (NCT01065766)
Timeframe: Baseline and Week 24

Interventionmg/dL (Mean)
All Participants Included in the Safety Evaluation-32.40

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Change From Baseline to Treatment in Fasting Plasma Glucose (FPG) at Week 12

Blood glucose was measured on a fasting basis (collected after an 8- to 10-hour fast). FPG is expressed as mg/dL. Therefore, this change from baseline reflects the Week 12 FPG minus Week 0 FPG. (NCT01065766)
Timeframe: Baseline and Week 12

Interventionmg/dL (Mean)
All Participants Included in the Safety Evaluation-28.21

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Change From Baseline in 2hr-PPG at Week 24

Blood glucose was measured 2 hours after a meal (2hr-PPG). 2hr-PPG is expressed as mg/dL. Therefore, this change from baseline reflects the Week 24 2hr-PPG minus Week 0 2hr-PPG. (NCT01065766)
Timeframe: Baseline and Week 24

Interventionmg/dL (Mean)
All Participants Included in the Safety Evaluation-62.13

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Change From Baseline in 2-hour Post Prandial Glucose (2hr-PPG) at Week 12

Blood glucose was measured 2 hours after a meal (2hr-PPG). 2hr-PPG is expressed as mg/dL. Therefore, this change from baseline reflects the Week 12 2hr-PPG minus Week 0 2hr-PPG. (NCT01065766)
Timeframe: Baseline and Week 12

Interventionmg/dL (Mean)
All Participants Included in the Safety Evaluation-58.02

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Change From Baseline in Hemoglobin A1C (%) at Week 24

Change from baseline reflects the Week 24 value minus the baseline value. A1C represents the percentage of glycosylated hemoglobin. (NCT01076075)
Timeframe: Baseline and Week 24

InterventionPercentage of glycosylated hemoglobin (Least Squares Mean)
Sitagliptin-0.84
Placebo/Pioglitazone-0.16

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Number of Participants Discontinuing Study Drug Due to An Adverse Event

(NCT01076075)
Timeframe: Week 0 to Week 54

Interventionparticipants (Number)
Sitagliptin3
Placebo/Pioglitazone9

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Number of Participants With One or More Adverse Events (AEs) - Week 0 to Week 54

(NCT01076075)
Timeframe: Week 0 to Week 54

Interventionparticipants (Number)
Sitagliptin120
Placebo/Pioglitazone122

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Change From Baseline in 2-hour Post-Meal Glucose at Week 24

Change from baseline reflects the Week 24 value minus the baseline value. Two-hour post-meal glucose was measured following a standard meal. (NCT01076075)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-36.8
Placebo/Pioglitazone-3.3

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Change From Baseline in Fasting Plasma Glucose at Week 24

Change from baseline reflects the Week 24 value minus the baseline value. (NCT01076075)
Timeframe: Baseline to Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-13.2
Placebo/Pioglitazone5.3

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Change From Baseline in Hemoglobin A1C (A1C) at Week 24

A1C is measured as percent. Thus, this change from baseline reflects the Week 24 A1C percent minus the Week 0 A1C percent. (NCT01076088)
Timeframe: Baseline and Week 24

InterventionPercent of glycosylated hemoglobin (Least Squares Mean)
Sitagliptin 50 mg + Metformin 500 mg-1.67
Sitagliptin 50 mg + Metformin 850 mg-1.83
Metformin 500 mg-1.29
Metformin 850 mg-1.56
Sitagliptin 100 mg-0.99
Placebo-0.59

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Change From Baseline in 2-hour Post Meal Glucose (2-h PMG) at Week 24

Change from baseline in 2-h PMG at Week 24 is defined as Week 24 2-h PMG minus Week 0 2-h PMG. (NCT01076088)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 50 mg + Metformin 500 mg-97.05
Sitagliptin 50 mg + Metformin 850 mg-109.46
Metformin 500 mg-65.67
Metformin 850-90.93
Sitagliptin 100 mg-48.11
Placebo-21.88

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24

Change from baseline in FPG at Week 24 is defined as Week 24 FPG minus Week 0 FPG. (NCT01076088)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin 50 mg + Metformin 500 mg-39.38
Sitagliptin 50 mg + Metformin 850 mg-47.74
Metformin 500 mg-33.66
Metformin 850-39.63
Sitagliptin 100 mg-21.86
Placebo-11.93

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Change in HbA1c From Baseline to Week 26 (Main Study)

The table below shows the least-squares (LS) mean change in HbA1c from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the LS mean change. (NCT01081834)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent (Least Squares Mean)
Placebo0.14
Canagliflozin 100 mg-0.77
Canagliflozin 300 mg-1.03

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Percentage of Patients With HbA1c <7% at Week 26 (High Glycemic Substudy)

The table below shows the percentage of patients with HbA1c <7% at Week 26 for each treatment group in patients randomized to the High Glycemic Substudy. (NCT01081834)
Timeframe: Week 26

InterventionPercentage of patients (Number)
Canagliflozin 100 mg17.4
Canagliflozin 300 mg11.6

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Percent Change in High-density Lipoprotein Cholesterol (HDL-C) From Baseline to Week 26 (Main Study)

The table below shows the least-squares (LS) mean percent change in HDL-C from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the LS mean percent change. (NCT01081834)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent change (Least Squares Mean)
Placebo4.4
Canagliflozin 100 mg11.2
Canagliflozin 300 mg10.5

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Change in Fasting Plasma Glucose (FPG) From Baseline to Week 26 (High Glycemic Substudy)

The table below shows the least-squares (LS) mean change in FPG from Baseline to Week 26 for each treatment group in patients randomized to the High Glycemic Substudy. (NCT01081834)
Timeframe: Day 1 (Baseline) and Week 26

Interventionmg/dL (Least Squares Mean)
Canagliflozin 100 mg-81.7
Canagliflozin 300 mg-86.3

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Change in 2-hour Post-prandial Glucose From Baseline to Week 26 (Main Study)

The table below shows the least-squares (LS) mean change in 2-hour post-prandial glucose from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the LS mean change. (NCT01081834)
Timeframe: Day 1 (Baseline) and Week 26

Interventionmg/dL (Least Squares Mean)
Placebo5.19
Canagliflozin 100 mg-42.9
Canagliflozin 300 mg-58.8

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Change in 2-hour Post-prandial Glucose From Baseline to Week 26 (High Glycemic Substudy)

The table below shows the least-squares (LS) mean change in 2-hour post-prandial glucose from Baseline to Week 26 for each treatment group in patients randomized to the High Glycemic Substudy. (NCT01081834)
Timeframe: Day 1 (Baseline) and Week 26

Interventionmg/dL (Least Squares Mean)
Canagliflozin 100 mg-118
Canagliflozin 300 mg-126

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Percent Change in High-density Lipoprotein Cholesterol (HDL-C) From Baseline to Week 26 (High Glycemic Substudy)

The table below shows the least-squares mean percent change in HDL-C from Baseline to Week 26 for each treatment group in patients randomized to the High Glycemic Substudy. (NCT01081834)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent change (Least Squares Mean)
Canagliflozin 100 mg2.4
Canagliflozin 300 mg10.8

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Percentage of Patients With HbA1c <7% at Week 26 (Main Study)

The table below shows the percentage of patients with HbA1c <7% at Week 26. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the percentage. (NCT01081834)
Timeframe: Week 26

InterventionPercentage of patients (Number)
Placebo20.6
Canagliflozin 100 mg44.5
Canagliflozin 300 mg62.4

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Percent Change in Triglycerides From Baseline to Week 26 (Main Study)

The table below shows the least-squares (LS) mean percent change in triglycerides from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the LS mean percent change. (NCT01081834)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent change (Least Squares Mean)
Placebo7.8
Canagliflozin 100 mg2.5
Canagliflozin 300 mg-2.4

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Percent Change in Triglycerides From Baseline to Week 26 (High Glycemic Substudy)

The table below shows the least-squares mean percent change in triglycerides from Baseline to Week 26 for each treatment group in patients randomized to the High Glycemic Substudy. (NCT01081834)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent change (Least Squares Mean)
Canagliflozin 100 mg-0.6
Canagliflozin 300 mg-12.7

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Change in Fasting Plasma Glucose (FPG) From Baseline to Week 26 (Main Study)

The table below shows the least-squares (LS) mean change in FPG from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the LS mean change. (NCT01081834)
Timeframe: Day 1 (Baseline) and Week 26

Interventionmg/dL (Least Squares Mean)
Placebo8.33
Canagliflozin 100 mg-27.2
Canagliflozin 300 mg-35.0

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Change in HbA1c From Baseline to Week 26 (High Glycemic Substudy)

The table below shows the least-squares (LS) mean change in HbA1c from Baseline to Week 26 for each treatment group in patients randomized to the High Glycemic Substudy. (NCT01081834)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent (Least Squares Mean)
Canagliflozin 100 mg-2.13
Canagliflozin 300 mg-2.56

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Change in Systolic Blood Pressure (SBP) From Baseline to Week 26 (High Glycemic Substudy)

The table below shows the least-squares (LS) mean change in SBP from Baseline to Week 26 for each treatment group in patients randomized to the High Glycemic Substudy. (NCT01081834)
Timeframe: Day 1 (Baseline) and Week 26

InterventionmmHg (Least Squares Mean)
Canagliflozin 100 mg-4.47
Canagliflozin 300 mg-4.97

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Change in Systolic Blood Pressure (SBP) From Baseline to Week 26 (Main Study)

The table below shows the least-squares (LS) mean change in SBP from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the LS mean change. (NCT01081834)
Timeframe: Day 1 (Baseline) and Week 26

InterventionmmHg (Least Squares Mean)
Placebo0.38
Canagliflozin 100 mg-3.34
Canagliflozin 300 mg-5.04

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Percent Change in Body Weight From Baseline to Week 26 (High Glycemic Substudy)

The table below shows the least-squares (LS) mean percent change in body weight from Baseline to Week 26 for each treatment group in patients randomized to the High Glycemic Substudy. (NCT01081834)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent change (Least Squares Mean)
Canagliflozin 100 mg-3.0
Canagliflozin 300 mg-3.8

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Percent Change in Body Weight From Baseline to Week 26 (Main Study)

The table below shows the least-squares (LS) mean percent change in body weight from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the LS mean percent change. (NCT01081834)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent change (Least Squares Mean)
Placebo-0.6
Canagliflozin 100 mg-2.8
Canagliflozin 300 mg-3.9

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Postprandial Total GIP (AUC)

To evaluate the effects of treatment on postprandial total GIP (AUC) (NCT01092663)
Timeframe: Baseline and 12 weeks

Interventionpmol/l x min (Mean)
Colesevelam-2
Colesevelam Plus Sitagliptin-5

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Fasting Gluconeogenesis

Change from baseline in fasting gluconeogenesis after 12 weeks of colesevelam alone or colesevelam plus sitagliptin treatment (NCT01092663)
Timeframe: baseline and 12 weeks

Interventionumol per kilogram (kg) FFM per min (Mean)
Colesevelam0.2
Colesevelam Plus Sitagliptin-0.3

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Fasting Endogenous Glucose Production

Change from baseline in fasting endogenous glucose production after 12 weeks of colesevelam alone or colesevelam plus sitagliptin treatment (NCT01092663)
Timeframe: baseline and 12 weeks

Interventionmicromoles (umol) per kg FFM per min (Mean)
Colesevelam1.0
Colesevelam Plus Sitagliptin1.0

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Fasting Active Plasma Glucagon Like-Peptide 1 (GLP-1)

To evaluate the effect of treatments on plasma GLP-1 concentrations. (NCT01092663)
Timeframe: Baseline and 12 weeks

Interventionpmol/L (Mean)
Colesevelam2.4
Colesevelam Plus Sitagliptin2.8

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Appearance Rate of Oral Glucose

Change from baseline in appearance rate of oral glucose after 12 weeks of colesevelam alone or colesevelam plus sitagliptin treatments (NCT01092663)
Timeframe: baseline and 12 weeks

Interventionumol per kg per min (Mean)
Colesevelam118
Colesevelam Plus Sitagliptin-244

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Postprandial Rate of Total Glucose Disposal Area Under the Curve (AUC)

"Change from baseline in postprandial rate of total glucose disposal (AUC) after 12 weeks of colesevelam alone or colesevelam plus sitagliptin treatments~AUC was calculated by the trapezoid method using all results measured between 0 and 300 min during the meal tolerance test." (NCT01092663)
Timeframe: baseline and 12 weeks

Interventionumol per kg per min (Mean)
Colesevelam-10
Colesevelam Plus Sitagliptin-256

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Postprandial Insulin (AUC)

To evaluate the effect of treatments on postprandial insulin (AUC) (NCT01092663)
Timeframe: Baseline and 12 weeks

Interventionpmol/l x min (Mean)
Colesevelam-13
Colesevelam Plus Sitagliptin40

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Postprandial Glucose (AUC)

Comparison between baseline and 12 weeks values of postrandial glucose (AUC). (NCT01092663)
Timeframe: Baseline and 12 weeks

Interventionmillimoles (mmol)/l x min (Mean)
Colesevelam-1.1
Colesevelam Plus Sitagliptin-1.5

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Postprandial Glucagon (AUC)

To evaluate the effects of treatment on postprandial glucagon (AUC) (NCT01092663)
Timeframe: Baseline and 12 weeks

Interventionpicograms (pg)/milliter (ml) x min (Mean)
Colesevelam-7
Colesevelam Plus Sitagliptin-4.7

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Postprandial Endogenous Glucose Production

"Change from baseline in postprandial endogenous glucose production after 12 weeks of colesevelam alone or colesevelam plus sitagliptin treatments~Mean value was calculated using all results measured between 10 and 300 min post meal." (NCT01092663)
Timeframe: baseline and 12 weeks

Interventionumol per kg per min (Mean)
Colesevelam-0.1
Colesevelam Plus Sitagliptin-0.2

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Postprandial C-peptide (AUC)

To evaluate the effect of treatments on postprandial C-peptide (AUC) (NCT01092663)
Timeframe: Baseline and 12 weeks

Interventionpmol/l x min (Mean)
Colesevelam30
Colesevelam Plus Sitagliptin193

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Postprandial Active GLP-1 (AUC)

To evaluate the effects of treatments on postprandial active GLP-1 (AUC) (NCT01092663)
Timeframe: Baseline and 12 weeks

Interventionpmol/l x min (Mean)
Colesevelam1.8
Colesevelam Plus Sitagliptin6.6

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Hemoglobin A1C

Change from baseline in hemoglobin A1C after 12 weeks of colesevelam or colesevelam plus sitagliptin treatments (NCT01092663)
Timeframe: Baseline and 12 weeks

Interventionpercentage (Mean)
Colesevelam0.3
Colesevelam Plus Sitagliptin-0.1

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Fasting Plasma Total Glucose-dependent Insulinotropic Peptide (GIP)

To evaluate the effect of treatments on plasma Glucose-dependent Insulinotropic Peptide (GIP) concentrations. (NCT01092663)
Timeframe: Baseline and 12 weeks

Interventionpmol/L (Mean)
Colesevelam1.8
Colesevelam Plus Sitagliptin-1.3

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Fasting Plasma Glucose Clearance

Change from baseline in fasting plasma glucose clearance after 12 weeks of colesevelam alone or colesevelam plus sitagliptin treatments. (NCT01092663)
Timeframe: baseline and 12 weeks

Interventionml per kg FFM per minute (min) (Mean)
Colesevelam0.30
Colesevelam Plus Sitagliptin0.27

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Fasting Plasma Glucose

Change from baseline in fasting plasma glucose concentrations after 12 weeks of colesevelam or colesevelam plus sitagliptin treatments. (NCT01092663)
Timeframe: Baseline and 12 weeks

Interventionmillimoles (mmol)/Liter (L) (Mean)
Colesevelam-0.8
Colesevelam Plus Sitagliptin-0.6

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Fasting Plasma C-peptide

To evaluate the effect of treatments on plamsa C-peptide concentrations. (NCT01092663)
Timeframe: Baseline and 12 weeks

Interventionpicomoles (pmol)/Liter (L) (Mean)
Colesevelam26
Colesevelam Plus Sitagliptin103

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Fasting Plamsa Glucagon

To evaluate the effect of treatments on plasma glucagon concentrations. (NCT01092663)
Timeframe: Baseline and 12 weeks

Interventionpicograms (pg)/milliliter (ml) (Mean)
Colesevelam1
Colesevelam Plus Sitagliptin0

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Fasting Insulin

To evaluate the effect of treatments on fasting insulin concentrations (NCT01092663)
Timeframe: Baseline and 12 weeks

Interventionpmol/L (Mean)
Colesevelam6
Colesevelam Plus Sitagliptin12

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Whole-body Glycolytic Disposal of Oral Glucose

Change in baseline in whole-body glycolytic disposal of oral glucose after 12 weeks of colesevelam alone or colesevelam plus glucose treatments (NCT01092663)
Timeframe: baseline and 12 weeks

InterventionPercent of Load (Mean)
Colesevelam4
Colesevelam Plus Sitagliptin2

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Fasting Glycogenolysis

Change from baseline in fasting glycogenolysis after 12 weeks of colesevelam alone or colesevelam plus sitagliptin treatment (NCT01092663)
Timeframe: baseline and 12 weeks

Interventionumol per kg Fat-Free Mass (FFM) per min (Mean)
Colesevelam0.8
Colesevelam Plus Sitagliptin1.7

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Self-reported Symptoms

Cumulative number of self-reported symptoms based on the Division of AIDS Grading Scale for the Severity of Adult Adverse Events (0-4 scale where 0 is no new symptoms, 4 is serious adverse event or toxicity) (NCT01093651)
Timeframe: Monthly for 4 months

,
Interventiontotal number of self reported symptoms (Number)
Hypoglycemia symptomsGI symptomsUpper respiratory symptomsGeneralized fatigueHeadacheOther (e.g., rash, muscle pain, mood change)
DPPIV Inhibition335245
Placebo1810556

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SDF1α; Serum Biomarkers of Immune Activation

serum stromal cell-derived factor-1α concentration (NCT01093651)
Timeframe: Baseline, week 8, week 16

,
Interventionpg/mL (Mean)
Baselineweek 8week 16
DPPIV Inhibition237812081277
Placebo232723132309

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RANTES; Serum Biomarkers of Immune Activation

serum Regulated on Activation, Normal T cell Expressed and Secreted concentration (NCT01093651)
Timeframe: Baseline, week 8, week 16

,
Interventionng/mL (Mean)
Baselineweek 8week 16
DPPIV Inhibition64.468.562.8
Placebo80.885.374.9

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Oral Glucose Tolerance

Area under the 75-gr oral glucose tolerance curve (AUCg) based on plasma glucose values measured at 0, 30, 60, 90, and 120 mins post-glucose challenge. (NCT01093651)
Timeframe: Baseline, week 8, week 16

,
Interventionmg*min/mL (Mean)
Baseline AUCgWeek 8 AUCgWeek 16 AUCg
DPPIV Inhibition145.6133.6142.5
Placebo142.5158.0157.5

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CD4+ T-cell Count

(NCT01093651)
Timeframe: Monthly for 4 months

,
Interventioncells/µL (Mean)
BaselineWeek 4Week 8Week 12Week 16
DPPIV Inhibition648750656706636
Placebo602689696686681

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Plasma HIV Viremia (Viral Load)

Percentage of participants with plasma HIV RNA copy number less than 48 copies/mL (NCT01093651)
Timeframe: Monthly for 6 months

,
Interventionpercentage of participants below 48 c/mL (Number)
BaselineWeek 4Week 8Week 12Week 16Week 24
DPPIV Inhibition100100100100100100
Placebo100100100100100100

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Soluble TNFR2; Serum Biomarkers of Immune Activation

serum soluble tumor necrosis factor receptor-2 concentration (NCT01093651)
Timeframe: Baseline, week 8, week 16

,
Interventionpg/mL (Mean)
Baselineweek 8week 16
DPPIV Inhibition243626172388
Placebo222022182279

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Area Under the Curve (AUC(0-t)) for Sitagliptin

AUC (0-t) is the area under the curve for the plot showing plasma concentration against time from time zero to the time of the last quantifiable concentration for sitagliptin 50 mg, metformin 500 mg and metformin 850 mg. (NCT01093794)
Timeframe: baseline through 72 hours postdose

,,,
Interventionhr*ng/mL (Mean)
sitagliptin 50 mgmetformin 500 mgmetformin 850 mg
Sit 50 mg + Met 500 mg15708350NA
Sit 50 mg + Met 850 mg1520NA11800
SitMet 50mg/500mg FDC15908750NA
SitMet 50mg/850mg FDC1600NA13100

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Cmax for Sitagliptin and Metformin

Cmax is the peak serum concentration of a therapeutic drug after administration; and is used to determine the rate and extent of drug absorption. Cmax is reported for sitagliptin 50 mg, metformin 500 mg and metformin 850 mg. (NCT01093794)
Timeframe: baseline through 72 hours postdose

,,,
Interventionng/mL (Mean)
sitagliptin 50 mgMetformin 500 mgMetformin 850 mg
Sit 50 mg + Met 500 mg1891210NA
Sit 50 mg + Met 850 mg187NA1790
SitMet 50mg/500mg FDC1821310NA
SitMet 50mg/850mg FDC194NA1970

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Number of Participants With the Indicated Time to Hyperglycemic Rescue Through Week 52

Hyperglycemic rescue was defined as meeting one of the following criteria, confirmed by a second sample drawn within 7 days and analyzed by the central laboratory: for the Week 2 to Week 4 visit, a single FPG value >=280 milligrams per deciliter (mg/dL); for the >Week 4 and =250 mg/dL and previous titration for >=4 weeks; for the >=Week 12 and =8.5% and a <=0.5% reduction from Baseline and previous titration for >=4 weeks; for the >=Week 26 and =8.5% and previous titration for >=4 weeks; for the >=Week 48 and =8.0% and previous titration for >=4 weeks. Time to hyperglycemia rescue is the time between the date of first dose and the date of hyperglycemia rescue plus 1 day, or the time between the date of first dose and the date of last visit during active treatment period plus 1 day for participants not requiring rescue. (NCT01098539)
Timeframe: Week 2 to Week 52

,
InterventionParticipants (Number)
Week 2Week 4Week 8Week 12Week 16Week 20Week 26Week 36Week 48Week 52
Albiglutide 30 mg00125915253344
Sitagliptin 100 mg223561429475368

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Plasma Concentrations (Conc.) of Albiglutide at Week 8 and Week 16

Sparse population pharmacokinetic (PK) data were collected for population PK and PK/pharmacodynamic (PD) analyses. Participants (par.) who received albiglutide were initiated on a 30 mg weekly dosing regimen. Beginning at Week 4, uptitration of albiglutide was allowed based on glycemic parameters. As such, albiglutide plasma conc. achieved at each sampling time represent a mixed population of par. who received either 30 mg or 50 mg weekly for various durations. The PK and PK/PD of albiglutide were characterized using a population modeling approach. Mean albiglutide plasma conc. observed at Weeks 8 and 16 are presented. Par. came to the clinic at Weeks 8 and 16 without taking albiglutide/matching placebo. The pre-dose PK sample was taken immediately prior to dosing. The Week 8 post-dose sample was taken between Weeks 8 and 10, >=2 days after a dose of medication. The Week 16 post-dose PK sample was taken any time between Weeks 16 and 20, >=2 days after the previous dose of albiglutide. (NCT01098539)
Timeframe: Week 8 Pre-dose (immediately prior to dose), Week 8 Post-dose (at least 2 days after a dose of medication), Week 16 Pre-dose (immediately prior to dose), and Week 16 Post-dose (at least 2 days after previous dose of albiglutide)

Interventionnanograms per milliliter (ng/mL) (Mean)
Week 8, Pre-dose, n=223Week 8, Post-dose, n=220Week 16, Pre-dose, n=215Week 16, Post-dose, n=205
Albiglutide 30 mg3005.803452.622994.153583.06

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Change From Baseline in Body Weight Through Week 52: OC

Change from Baseline was calculated as the post-Baseline weight minus the Baseline weight. The Baseline weight value is defined as the last non-missing value prior to treatment. This analysis used observed weight values excluding those obtained after hyperglycemia rescue; no missing data imputation was performed. (NCT01098539)
Timeframe: Baseline; Week 1, Week 2 , Week 3, Week 4, Week 8, Week 12, Week 16, Week 20, Week 26, Week 36, Week 48, and Week 52

,
InterventionKilograms (Mean)
Week 1, n=225, 225Week 2, n=232, 227Week 3, n=236, 224Week 4, n=235, 230Week 8, n=226, 214Week 12, n=228, 219Week 16, n=223, 210Week 20, n=211, 198Week 26, n=202, 178Week 36, n=190, 155Week 48, n=172, 140Week 52, n=157, 119
Albiglutide 30 mg-0.17-0.21-0.24-0.31-0.61-0.45-0.68-0.76-0.87-0.92-0.93-0.82
Sitagliptin 100 mg0.12-0.010.030.100.050.160.070.09-0.040.010.070.31

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Mean Change From Baseline in Fasting Plasma Glucose (FPG) at Weeks 1, 2, 3, 4, 8, 12, 16, 20, 26, 36, 48, and Week 52: OC

The FPG test measures blood sugar levels after the participant has not eaten (fasted) for 12 to 14 hours. The Baseline FPG value is defined as the last non-missing value prior to treatment. Change from Baseline in FBG was calculated as the post-Baseline value minus the Baseline value. The OC method (no imputation of missing data) was used. If a participant had missing observation(s) immediately after Baseline, the Baseline observation was not carried forward and was left as missing. Participants were analyzed in a particular treatment week if they had received at least one dose in that treatment week. (NCT01098539)
Timeframe: Baseline; Weeks 1, 2, 3, 4, 8, 12, 16, 20, 26, 36, 48, Week 52

,
InterventionMillimoles per liter (mmol/L) (Mean)
Week 1, n=219, 217Week 2, n=226, 223Week 3, n=230, 219Week 4, n=231, 226Week 8, n=221, 210Week 12, n=224, 216Week 16, n=214, 204Week 20, n=207, 191Week 26, n=200, 177Week 36, n=186, 149Week 48, n=165, 140Week 52, n=149, 114
Albiglutide 30 mg-0.82-1.28-1.25-1.55-1.24-1.46-1.41-1.51-1.54-1.42-1.08-1.06
Sitagliptin 100 mg-0.93-0.66-0.88-0.76-0.74-0.88-0.55-1.00-0.58-0.92-0.58-0.96

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Mean Change From Baseline in FPG at Weeks 4, 8, 12, 16, 20, and 26: LOCF

The FPG test measures blood sugar levels after the participant has not eaten (fasted) for 12 to 14 hours. The Baseline FPG value is the last non-missing value before the start of treatment. Change from Baseline in FBG was calculated as the post-Baseline value minus the Baseline value. The LOCF method was used to impute missing data, in which the last non-missing post-Baseline on-treatment measurement was used to impute the missing measurement. If a participant had missing observation(s) immediately after Baseline, the Baseline observation was not carried forward and was left as missing. Participants were analyzed in a particular treatment week if they had received at least one dose in that treatment week. (NCT01098539)
Timeframe: Baseline; Weeks 4, 8, 12, 16, 20, and 26

,
InterventionMillimoles per liter (mmol/L) (Mean)
Week 4, n=244, 240Week 8, n=244, 240Week 12, n=244, 240Week 16, n=244, 240Week 20, n=244, 240
Albiglutide 30 mg-1.47-1.19-1.35-1.34-1.37
Sitagliptin 100 mg-0.84-0.82-0.81-0.49-0.62

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Mean Change From Baseline in HbA1c at Weeks 4, 8, 12, 16, 20, 26, 36, 48, and Week 52: Observed Cases

HbA1c is a form of hemoglobin that is measured primarily to identify the average plasma glucose concentration over a 2- to 3-month period. The Baseline HbA1c value is defined as the last non-missing value before the start of treatment. Change from Baseline in HbA1c was calculated as the post-Baseline value minus the Baseline value. The Observed Cases (OC) method (no imputation of missing data) was used. If a participant had missing observation(s) immediately after Baseline, the Baseline observation was not carried forward and was left as missing. Participants were analyzed in a particular treatment week if they had received at least one dose in that treatment week. (NCT01098539)
Timeframe: Baseline; Weeks 4, 8, 12, 16, 20, 26, 36, 48, and 52

,
InterventionPercentage of HbA1c in the blood (Mean)
Week 4, n=233, 228Week 8, n=222, 213Week 12, n=224, 216Week 16, n=218, 209Week 20, n=207, 196Week 26, n=202, 178Week 36, n=192, 155Week 48, n=172, 139Week 52, n=157, 118
Albiglutide 30 mg-0.43-0.63-0.71-0.75-0.86-0.93-1.01-1.01-1.04
Sitagliptin 100 mg-0.37-0.56-0.62-0.63-0.71-0.80-0.82-0.89-1.03

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Mean Change From Baseline in HbA1c at Weeks 4, 8, 12, 16, and 20: LOCF

HbA1c is a form of hemoglobin that is measured primarily to identify the average plasma glucose concentration over a 2- to 3-month period. The Baseline HbA1c value is defined as the last non-missing value before the start of treatment. Change from Baseline in HbA1c was calculated as the post-Baseline value minus the Baseline value. The LOCF method was used to impute missing data, in which the last non-missing post-Baseline on-treatment measurement was used to impute the missing measurement. If a participant had missing observation(s) immediately after Baseline, the Baseline observation was not carried forward and was left as missing. Participants were analyzed in a particular treatment week if they had received at least one dose in that treatment week. (NCT01098539)
Timeframe: Baseline; Weeks 4, 8, 12, 16, and 20

,
InterventionPercentage of HbA1c in the blood (Mean)
Week 4, n=237, 234Week 8, n=242, 236Week 12, n=242, 236Week 16, n=242, 236Week 20, n=242, 236
Albiglutide 30 mg-0.43-0.60-0.69-0.75-0.79
Sitagliptin 100 mg-0.37-0.52-0.56-0.56-0.54

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Number of Participants Who Achieved a Clinically Meaningful HbA1c Response Level of <6.5% and <7.0% at Week 52: OC

The number of participants who acheieved the HbA1c treatment goal (i.e., number of participants who achieved HbA1c <7% and <6.5% at Week 26) was assessed. The OC method (no imputation of missing data) was used. If a participant had missing observation(s) immediately after Baseline, the Baseline observation was not carried forward and was left as missing. (NCT01098539)
Timeframe: Week 52

,
InterventionParticipants (Number)
HbA1c <6.5%HbA1c <7.0%
Albiglutide 30 mg4498
Sitagliptin 100 mg2761

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Number of Participants Who Achieved a Clinically Meaningful Improvement in the HbA1c Response Level of >=1.0%, >=1.5%, and >=2.0% at Week 26: LOCF

The number of participants who a clinically meaningful improvement from Baseline in the HbA1c response level of >=1.0%, >=1.5%, and >=2.0% at Week 26 were assessed. The LOCF method was used to impute missing data, in which the last non-missing post-Baseline on-treatment measurement was used to impute the missing measurement. If a participant had missing observation(s) immediately after Baseline, the Baseline observation was not carried forward and was left as missing. (NCT01098539)
Timeframe: Week 26

,
InterventionParticipants (Number)
HbA1c >=1.0%HbA1c >=1.5%HbA1c >=2.0%
Albiglutide 30 mg1024926
Sitagliptin 100 mg773817

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Number of Participants Who Achieved a Clinically Meaningful Improvement in the HbA1c Response Level of >=1.0%, >=1.5%, and >=2.0% at Week 52: OC

The number of participants who a clinically meaningful improvement from Baseline in the HbA1c response level of >=1.0%, >=1.5%, and >=2.0% at Week 52 assessed. The OC method (no imputation of missing data) was used. If a participant had missing observation(s) immediately after Baseline, the Baseline observation was not carried forward and was left as missing. (NCT01098539)
Timeframe: Week 52

,
InterventionParticipants (Number)
HbA1c >=1.0%HbA1c >=1.5%HbA1c >=2.0%
Albiglutide 30 mg794320
Sitagliptin 100 mg653015

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Number of Participants Who Achieved Clinically Meaningful HbA1c Response Levels of <6.5% and <7.0% at Week 26: LOCF

The number of participants who acheieved the HbA1c treatment goal (i.e., the number of participants who achieved HbA1c <7% and <6.5% at Week 26) was assessed. The LOCF method was used to impute missing data, in which the last non-missing post-Baseline on-treatment measurement was used to impute the missing measurement. If a participant had missing observation(s) immediately after Baseline, the Baseline observation was not carried forward and was left as missing. (NCT01098539)
Timeframe: Week 26

,
InterventionParticipants (Number)
HbA1c <6.5%HbA1c <7.0%
Albiglutide 30 mg37103
Sitagliptin 100 mg2972

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Change From Baseline in Body Weight at Week 26: LOCF

Change from Baseline was calculated as the post-Baseline weight minus the Baseline weight. The Baseline weight value is defined as the last non-missing value prior to treatment. This analysis used the LOCF method for missing post-Baseline weight values. Weight values obtained after hyperglycemia rescue werre treated as missing and were replaced with pre-rescue values. Based on ANCOVA: Change = treatment + Baseline weight + renal impairment + prior myocardial infarction history + age category + region. (NCT01098539)
Timeframe: Baseline; Week 26

InterventionKilograms (Least Squares Mean)
Albiglutide 30 mg-0.79
Sitagliptin 100 mg-0.19

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 26

The FPG test measures blood sugar levels after the participant has not eaten (fasted) for 12 to 14 hours. The Baseline FPG value is define as the last non-missing value before the start of treatment. Change from Baseline in FBG was calculated as the post-Baseline value minus the Baseline value. The LOCF method was used to impute missing data, in which the last non-missing post-Baseline on-treatment measurement was used to impute the missing measurement. If a participant had missing observation(s) immediately after Baseline, the Baseline observation was not carried forward and was left as missing. Participants were analyzed in a particular treatment week if they had received at least one dose in that treatment week. Based on ANCOVA: Change = treatment + Baseline FPG + renal impairment + prior myocardial infarction history + age category + region. (NCT01098539)
Timeframe: Baseline; Week 26

InterventionMillimoles per liter (mmol/L) (Least Squares Mean)
Albiglutide 30 mg-1.42
Sitagliptin 100 mg-0.22

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Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 26

HbA1c is a form of hemoglobin that is measured primarily to identify the average plasma glucose concentration over a 2- to 3-month period. The Baseline HbA1c value is defined as the last non-missing value before the start of treatment. Change from Baseline in HbA1c was calculated as the value at Week 26 minus the value at Baseline. The analysis was performed using an Analysis of Covariance (ANCOVA) model with treatment group, region, history of prior myocardial infarction (yes versus no), and age category (<65 years versus >=65 years) as factors and Baseline HbA1c as a continuous covariate. The last observation carried forward (LOCF) method was used to impute missing data, in which the last non-missing post-Baseline on-treatment measurement was used to impute the missing measurement. If a participant had missing observation(s) immediately after Baseline, the Baseline observation was not carried forward and was left as missing. (NCT01098539)
Timeframe: Baseline; Week 26

InterventionPercentage of HbA1c in the blood (Least Squares Mean)
Albiglutide 30 mg-0.83
Sitagliptin 100 mg-0.52

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Time to Hyperglycemic Rescue Through Week 52

Hyperglycemic rescue was defined as meeting one of the following criteria, confirmed by a second sample drawn within 7 days and analyzed by the central laboratory: for the Week 2 to Week 4 visit, a single FPG value >=280 milligrams per deciliter (mg/dL); for the >Week 4 and =250 mg/dL and previous titration for >=4 weeks; for the >=Week 12 and =8.5% and a <=0.5% reduction from Baseline and previous titration for >=4 weeks; for the >=Week 26 and =8.5% and previous titration for >=4 weeks; for the >=Week 48 and =8.0% and previous titration for >=4 weeks. Time to hyperglycemia rescue is the time between the date of first dose and the date of hyperglycemia rescue plus 1 day, or the time between the date of first dose and the date of last visit during active treatment period plus 1 day for participants not requiring rescue. This time is divided by 7 to express the result in weeks. (NCT01098539)
Timeframe: Week 2 to Week 52

InterventionWeeks (Median)
Albiglutide 30 mgNA
Sitagliptin 100 mgNA

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Change From Baseline in Body Weight Through Week 26: LOCF

Change from Baseline was calculated as the post-Baseline weight minus the Baseline weight. The Baseline weight value is defined as the last non-missing value prior to treatment. This analysis used the LOCF method for missing post-Baseline weight values. Weight values obtained after hyperglycemia rescue werre treated as missing and were replaced with pre-rescue values. (NCT01098539)
Timeframe: Baseline; Week 1, Week 2 , Week 3, Week 4, Week 8, Week 12, Week 16, Week 20, and Week 26

,
InterventionKilograms (Mean)
Week 1, n=225, 225Week 2, n=241, 238Week 3, n=244, 240Week 4, n=244, 240Week 8, n=244, 240Week 12, n=244, 240Week 16, n=244, 240Week 20, n=244, 240
Albiglutide 30 mg-0.17-0.21-0.25-0.33-0.58-0.47-0.63-0.69
Sitagliptin 100 mg0.12-0.020.010.090.020.03-0.08-0.07

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Length of Remission

For those patients that are able to discontinue insulin therapy at or <12 weeks, how long were they able to well controlled with an A1c <7% on the agent that they were randomized to. (NCT01099618)
Timeframe: 3 years

Interventiondays (Median)
Metformin472
Sitagliptin589
Placebo111

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Percent Change in Body Weight From Baseline to Week 26

The table below shows the least-squares (LS) mean percent change in body weight from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin or sitagliptin group minus placebo) in the LS mean percent change. (NCT01106677)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent change (Least Squares Mean)
Placebo/Sitagliptin-1.2
Canagliflozin 100 mg-3.7
Canagliflozin 300 mg-4.2
Sitagliptin 100 mg-1.2

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Percent Change in High-density Lipoprotein Cholesterol (HDL-C) From Baseline to Week 52

The table below shows the least-squares (LS) mean percent change in HDL-C from Baseline to Week 52 for each active treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus sitagliptin) in the LS mean percent change. (NCT01106677)
Timeframe: Day 1 (Baseline) and Week 52

InterventionPercent change (Least Squares Mean)
Canagliflozin 100 mg11.2
Canagliflozin 300 mg13.3
Sitagliptin 100 mg6.0

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Percent Change in High-density Lipoprotein Cholesterol (HDL-C) From Baseline to Week 26

The table below shows the least-squares (LS) mean percent change in HDL-C from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin or sitagliptin group minus placebo) in the LS mean percent change. (NCT01106677)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent change (Least Squares Mean)
Placebo/Sitagliptin3.7
Canagliflozin 100 mg10.4
Canagliflozin 300 mg12.1
Sitagliptin 100 mg5.0

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Percent Change in Body Weight From Baseline to Week 52

The table below shows the least-squares (LS) mean percent change in body weight from Baseline to Week 52 for each active treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus sitagliptin) in the LS mean percent change. (NCT01106677)
Timeframe: Day 1 (Baseline) and Week 52

InterventionPercent change (Least Squares Mean)
Canagliflozin 100 mg-3.8
Canagliflozin 300 mg-4.2
Sitagliptin 100 mg-1.3

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Change in 2-hour Post-prandial Glucose From Baseline to Week 26

The table below shows the least-squares (LS) mean change in 2-hour post-prandial glucose from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin or sitagliptin group minus placebo) in the LS mean change. (NCT01106677)
Timeframe: Day 1 (Baseline) and Week 26

Interventionmg/dL (Least Squares Mean)
Placebo/Sitagliptin-9.79
Canagliflozin 100 mg-47.9
Canagliflozin 300 mg-57.1
Sitagliptin 100 mg-49.3

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Percent Change in Triglycerides From Baseline to Week 26

The table below shows the least-squares (LS) mean percent change in triglycerides from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin or sitagliptin group minus placebo) in the LS mean percent change. (NCT01106677)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent change (Least Squares Mean)
Placebo/Sitagliptin3.2
Canagliflozin 100 mg1.6
Canagliflozin 300 mg-1.4
Sitagliptin 100 mg1.0

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Change in Systolic Blood Pressure (SBP) From Baseline to Week 52

The table below shows the least-squares (LS) mean change in SBP from Baseline to Week 52 for each active treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus sitagliptin) in the LS mean change. (NCT01106677)
Timeframe: Day 1 (Baseline) and Week 52

InterventionmmHg (Least Squares Mean)
Canagliflozin 100 mg-3.53
Canagliflozin 300 mg-4.65
Sitagliptin 100 mg-0.66

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Change in Systolic Blood Pressure (SBP) From Baseline to Week 26

The table below shows the least-squares (LS) mean change in SBP from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin or sitagliptin group minus placebo) in the LS mean change. (NCT01106677)
Timeframe: Day 1 (Baseline) and Week 26

InterventionmmHg (Least Squares Mean)
Placebo/Sitagliptin1.52
Canagliflozin 100 mg-3.84
Canagliflozin 300 mg-5.06
Sitagliptin 100 mg-1.83

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Change in HbA1c From Baseline to Week 52

The table below shows the least-squares (LS) mean change in HbA1c from Baseline to Week 52 for each active treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus sitagliptin) in the LS mean change. (NCT01106677)
Timeframe: Day 1 (Baseline) and Week 52

InterventionPercent (Least Squares Mean)
Canagliflozin 100 mg-0.73
Canagliflozin 300 mg-0.88
Sitagliptin 100 mg-0.73

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Change in HbA1c From Baseline to Week 26

The table below shows the least-squares (LS) mean change in HbA1c from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin or sitagliptin group minus placebo) in the LS mean change. (NCT01106677)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent (Least Squares Mean)
Placebo/Sitagliptin-0.17
Canagliflozin 100 mg-0.79
Canagliflozin 300 mg-0.94
Sitagliptin 100 mg-0.82

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Change in Fasting Plasma Glucose (FPG) From Baseline to Week 52

The table below shows the least-squares (LS) mean change in FPG from Baseline to Week 52 for each active treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus sitagliptin) in the LS mean change. (NCT01106677)
Timeframe: Day 1 (Baseline) and Week 52

Interventionmg/dL (Least Squares Mean)
Canagliflozin 100 mg-26.2
Canagliflozin 300 mg-35.2
Sitagliptin 100 mg-17.7

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Change in Fasting Plasma Glucose (FPG) From Baseline to Week 26

The table below shows the least-squares (LS) mean change in FPG from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin or sitagliptin group minus placebo) in the LS mean change. (NCT01106677)
Timeframe: Day 1 (Baseline) and Week 26

Interventionmg/dL (Least Squares Mean)
Placebo/Sitagliptin2.47
Canagliflozin 100 mg-27.3
Canagliflozin 300 mg-37.8
Sitagliptin 100 mg-20.2

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Percentage of Patients With HbA1c <7% at Week 26

The table below shows the percentage of patients with HbA1c <7% at Week 26 in each treatment group. The statistical analyses show the treatment differences between each canagliflozin or sitagliptin group and placebo. (NCT01106677)
Timeframe: Week 26

InterventionPercentage of patients (Number)
Placebo/Sitagliptin29.8
Canagliflozin 100 mg45.5
Canagliflozin 300 mg57.8
Sitagliptin 100 mg54.5

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Percent Change in Triglycerides From Baseline to Week 52

The table below shows the least-squares (LS) mean percent change in triglycerides from Baseline to Week 52 for each active treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus sitagliptin) in the LS mean percent change. (NCT01106677)
Timeframe: Day 1 (Baseline) and Week 52

InterventionPercent change (Least Squares Mean)
Canagliflozin 100 mg1.9
Canagliflozin 300 mg2.7
Sitagliptin 100 mg-0.4

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Percent Change in Body Weight From Baseline to Week 26

The table below shows the least-squares (LS) mean percent change in body weight from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the LS mean percent change. (NCT01106690)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent change (Least Squares Mean)
Placebo/Sitagliptin-0.1
Canagliflozin 100 mg-2.8
Canagliflozin 300 mg-3.8

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Percent Change in High-density Lipoprotein Cholesterol (HDL-C) From Baseline to Week 26

The table below shows the least-squares (LS) mean percent change in HDL-C from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the LS mean percent change. (NCT01106690)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent change (Least Squares Mean)
Placebo/Sitagliptin2.4
Canagliflozin 100 mg7.2
Canagliflozin 300 mg8.9

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Percent Change in Triglycerides From Baseline to Week 26

The table below shows the least-squares (LS) mean percent change in triglycerides from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the LS mean percent change. (NCT01106690)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent change (Least Squares Mean)
Placebo/Sitagliptin15.2
Canagliflozin 100 mg3.2
Canagliflozin 300 mg-1.7

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Percentage of Patients With HbA1c <7% at Week 26

The table below shows the percentage of patients with HbA1c<7% at Week 26 in each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the percentage. (NCT01106690)
Timeframe: Week 26

InterventionPercentage of patients (Number)
Placebo/Sitagliptin32.5
Canagliflozin 100 mg46.9
Canagliflozin 300 mg64.3

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Change in Homeostasis Model Assessment (HOMA2-%B) From Baseline to Week 26

HOMA2-%B is a measure of beta cell function (the cells in the pancreas that produce and store insulin). The table below shows the least-squares (LS) mean change in HOMA2-%B from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the LS mean change. (NCT01106690)
Timeframe: Day 1 (Baseline) and Week 26

InterventionHOMA2-%B (Least Squares Mean)
Placebo/Sitagliptin0.91
Canagliflozin 100 mg15.19
Canagliflozin 300 mg18.14

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Change in Fasting Plasma Glucose (FPG) From Baseline to Week 26

The table below shows the least-squares (LS) mean change in FPG from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the LS mean change. (NCT01106690)
Timeframe: Day 1 (Baseline) and Week 26

Interventionmg/dL (Least Squares Mean)
Placebo/Sitagliptin2.54
Canagliflozin 100 mg-26.8
Canagliflozin 300 mg-33.2

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Change in HbA1c From Baseline to Week 26

The table below shows the least-squares (LS) mean change in HbA1c from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the LS mean change. (NCT01106690)
Timeframe: Day 1 (Baseline) and Week 26

InterventionPercent (Least Squares Mean)
Placebo/Sitagliptin-0.26
Canagliflozin 100 mg-0.89
Canagliflozin 300 mg-1.03

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Change in Systolic Blood Pressure (SBP) From Baseline to Week 26

The table below shows the least-squares (LS) mean change in SBP from Baseline to Week 26 for each treatment group. The statistical analyses show the treatment differences (ie, each canagliflozin group minus placebo) in the LS mean change. (NCT01106690)
Timeframe: Day 1 (Baseline) and Week 26

InterventionmmHg (Least Squares Mean)
Placebo/Sitagliptin-1.24
Canagliflozin 100 mg-5.30
Canagliflozin 300 mg-4.70

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Relative Change in Sitagliptin Renal Clearance (CLr)

CLr of sitagliptin when administered with atorvastatin divided by CLr of sitagliptin when administered alone (NCT01112670)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours

Interventionratio (Mean)
ABCB1 Group 11.22
ABCB1 Group 20.99
ABCB1 Group 31.0

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Atorvastatin Area Under the Plasma Concentration Time Curve (AUC) Over the Dosing Interval (0-24 Hours)

(NCT01112670)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

Interventionng*h/ml (Mean)
ABCB1 Group 144.4
ABCB1 Group 235.4
ABCB1 Group 349.0

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Atorvastatin Maximum Plasma Concentration (Cmax)

(NCT01112670)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

Interventionng/ml (Mean)
ABCB1 Group 18.6
ABCB1 Group 27.5
ABCB1 Group 310.6

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Relative Change in Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity

AUC of sitagliptin when administered with atorvastatin divided by AUC of sitagliptin when administered alone (NCT01112670)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

Interventionratio (Mean)
ABCB1 Group 10.96
ABCB1 Group 20.98
ABCB1 Group 30.97

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Sitagliptin Monotherapy: Sitagliptin Maximum Plasma Concentration (Cmax)

(NCT01112670)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

Interventionng/ml (Mean)
ABCB1 Group 1454
ABCB1 Group 2438
ABCB1 Group 3394

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Sitagliptin Monotherapy: Sitagliptin Renal Clearance (CLr)

(NCT01112670)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

Interventionml/min (Mean)
ABCB1 Group 1254
ABCB1 Group 2232
ABCB1 Group 3359

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Sitagliptin + Atorvastatin: Sitagliptin Maximum Plasma Concentration (Cmax)

(NCT01112670)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

Interventionng/ml (Mean)
ABCB1 Group 1428
ABCB1 Group 2420
ABCB1 Group 3370

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Sitagliptin + Atorvastatin: Sitagliptin Renal Clearance (CLr)

(NCT01112670)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

Interventionml/min (Mean)
ABCB1 Group 1280
ABCB1 Group 2226
ABCB1 Group 3339

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Sitagliptin Monotherapy: Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity

(NCT01112670)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

Interventionng*hr/ml (Mean)
ABCB1 Group 13638
ABCB1 Group 23502
ABCB1 Group 33129

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Sitagliptin + Atorvastatin: Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity

(NCT01112670)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

Interventionng*h/ml (Mean)
ABCB1 Group 13501
ABCB1 Group 23430
ABCB1 Group 33117

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Relative Change in Sitagliptin Maximum Plasma Concentration (Cmax)

Cmax of sitagliptin when administered with atorvastatin divided by Cmax of sitagliptin when administered alone (NCT01112670)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

Interventionratio (Mean)
ABCB1 Group 10.96
ABCB1 Group 21.0
ABCB1 Group 30.93

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Part B: Number of Participants With AEs and SAEs

An AE was defined as any untoward MO in a participant temporally associated with the use of a MP, whether or not considered related to the MP and can therefore be any unfavourable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with its use. The SAE was any untoward MO that, at any dose, results in death, life threatening, persistent or significant disability/incapacity, results in or prolongs inpatient hospitalization, congenital abnormality or birth defect, that may not be immediately life-threatening or result in death or hospitalization but may jeopardize the participant or may require medical or surgical intervention to prevent one of the other outcomes listed in this definition. (NCT01119846)
Timeframe: Up to Week 7

,
InterventionParticipants (Count of Participants)
Any AEAny SAE
Part B: GSK1292263 800 mg Fasted Condition Orally00
Part B: GSK1292263 800 mg Fed Condition Orally10

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Part B: Summary of AUC0-t and AUC0-24

The AUC 0-24 and AUC 0-t determined using the linear trapezoidal rule for increasing concentrations and the logarithmic trapezoidal rule for decreasing concentrations. Blood samples for the determination of PK was collected at on Day 1 of each period: immediately pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 13 and 24 hours. (NCT01119846)
Timeframe: Pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 13 and 24 hours on Day 1 of each treatment period

,
InterventionNanograms×hour per mL (Geometric Mean)
AUC 0-24AUC 0-t
Part B: GSK1292263 800 mg Fasted Condition Orally3370.433370.43
Part B: GSK1292263 800 mg Fed Condition Orally12639.8412659.88

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Part B: Summary of Change From Baseline in Fasted Glucagon, GLP-1, C-peptide, Total GIP, Total PYY and Insulin

Blood samples for the determination of glucose and other PD markers were collected at pre-dose on Day 1 of each dosing period. For breakfast, lunch and evening meal in Part B, samples were collected just after the meal and at the following times after starting each meal: 0.5, 1 and 2 hours. Samples were also collected in Part B at 24 hours post-dose. When this results in multiple samples at the same time point, only one sample was collected. Change from Baseline was calculated by subtracting Baseline value from post-Baseline value. (NCT01119846)
Timeframe: Baseline (Day 1 pre-dose) and Day 1 (24 hours)

,
InterventionPico moles per Liter (Geometric Mean)
C-PEPTIDEGIP TOTALGLP-1 ACTIVEGLP-1 TOTALGLUCAGONINSULINPYY TOTAL
Part B: GSK1292263 800 mg Fasted Condition Orally13.442.230.000.560.9431.183.05
Part B: GSK1292263 800 mg Fed Condition Orally55.835.400.000.482.027.194.55

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Part B: Summary of T-max and T-lag

The time at which Cmax was observed was determined directly from the raw concentration-time data. The lag time before observation of drug concentrations in sample matrix determined as the time of the sample preceding the first quantifiable concentration. Blood samples for the determination of PK was collected at on Day 1 of each period: immediately pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 13 and 24 hours. (NCT01119846)
Timeframe: Pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 13 and 24 hours on Day 1 of each treatment period

,
InterventionHour (Median)
T-maxT-lag
Part B: GSK1292263 800 mg Fasted Condition Orally2.000.00
Part B: GSK1292263 800 mg Fed Condition Orally4.980.00

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Part C: Number of Participants With Abnormal Clinical Chemistry Parameters of PCI

Clinical chemistry parameters included BUN, potassium, AST, total and direct bilirubin, creatinine, chloride, ALT, uric acid, glucose fasting, GGT, albumin, sodium, magnesium, phosphorus inorganic, calcium, total CO2, ALP, triglycerides, total cholesterol, LDL cholesterol, free fatty acid (NEFA), HDL cholesterol and total protein. It was assessed on Screening, Day -2 (can be non-fasting) and prior to breakfast (early in the morning, fasting) on Days 1, 7 and 14, and on Day 15 prior to checkout, (=24 hours post-dose) of each treatment period and Follow-up (7 to 10 days after final discharge). Only those parameters for which at least one value of PCI was reported are summarized. Null data is not presented. (NCT01119846)
Timeframe: Up to Week 7

,,,,,
InterventionParticipants (Count of Participants)
Phosphorus inorganic, LowCO2, HighGlucose, HighCO2, LowPotassium, LowALT, HighAlbumin, LowCalcium, LowSodium, Low
Part C: GSK1292263 150 mg BID001000001
Part C: GSK1292263 300 mg BID004000000
Part C: GSK1292263 50 mg BID015000110
Part C: GSK1292263 600 mg Once Daily004000000
Part C: Placebo113111000
Part C: Sitagliptin 100 mg013000000

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Part C: Summary of T-half and Tmax of GSK1292263 and Sitagliptin When Co-administered

The time at which Cmax was observed was determined directly from the raw concentration-time data. The lag time before observation of drug concentrations in sample matrix determined as the time of the sample preceding the first quantifiable concentration. When GSK1292263 was dosed once daily, blood samples were collected on Days 1, 13 and 14 immediately pre-dose (time 0) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-dose. When GSK1292263 was dosed BID, blood samples were collected on Days 1, 13 and 14, at immediately pre-morning dose, 1,2, 4, 6, 8, 10, 11, 12, 14, 16, 18 and 24 hours post-morning dose. For once daily and BID dosing regimens on Day 7, blood samples were collected at pre-dose (= post-breakfast), 1, 2, 4 (= pre-lunch), 6, 10 (= immediately post-dinner) and 12 hours. When planned PK sampling results in multiple samples at the same time point, only one sample was collected. (NCT01119846)
Timeframe: Days 1, 7, 13 and 14

,,,,,
InterventionHour (Median)
T-half, Day 14T-max, Day 14
Part C: GSK1292263 150 mg BID7.242.00
Part C: GSK1292263 300 mg BID7.382.00
Part C: GSK1292263 50 mg BID7.602.00
Part C: GSK1292263 600 mg Once Daily7.222.00
Part C: Placebo7.852.00
Part C: Sitagliptin 100 mg7.892.00

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Part C: Summary of T-max and T-lag

The time at which Cmax was observed was determined directly from the raw concentration-time data. The lag time before observation of drug concentrations in sample matrix determined as the time of the sample preceding the first quantifiable concentration. When GSK1292263 was dosed once daily, blood samples were collected on Days 1, 13 and 14 immediately pre-dose (time 0) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-dose. When GSK1292263 was dosed BID, blood samples were collected on Days 1, 13 and 14, at immediately pre-morning dose, 1,2, 4, 6, 8, 10, 11, 12, 14, 16, 18 and 24 hours post-morning dose. For once daily and BID dosing regimens on Day 7, blood samples were collected at pre-dose (= post-breakfast), 1, 2, 4 (= pre-lunch), 6, 10 (=immediately post-dinner) and 12 hours. When planned PK sampling results in multiple samples at the same time point, only one sample was collected. (NCT01119846)
Timeframe: Days 1, 7, 13 and 14

,,,
InterventionHour (Median)
T-lag, Day 1T-max, Day 1T-max, Day 7T-max, Day 13T-max, Day 14
Part C: GSK1292263 150 mg BID0.0012.003.973.983.98
Part C: GSK1292263 300 mg BID0.0012.003.973.973.98
Part C: GSK1292263 50 mg BID0.004.003.973.974.01
Part C: GSK1292263 600 mg Once Daily0.503.974.03.973.98

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Part C: Summary of Change From Baseline in Fasted Insulin

Blood samples were collected fasting pre-breakfast and pre-morning dose (PD time 0) on Days -1, 13 and 14 and then at 10, 20, 30, 60, 90, 120, 180 min after eating the standardized breakfast meal tolerance test. For lunch (4 hour post-morning dose) samples were collected just before the meal and after starting each meal: 0.5, 1, 1.5, 2 and 3 hours. For the evening meal (10 hour post-morning dose), BID dosing groups followed the sequence of sampling, food and dosing as for breakfast (PD sample immediately before meal, eat and then dose), then 0.5, 1, 1.5, 2 and 3 hours post-dinner. A sample was also collected 24 hours post-dose. When this results in multiple samples at the same time point, only one sample was collected. Change from Baseline was calculated by subtracting Baseline value minus post-Baseline value. The point estimates and corresponding 95% CI for treatment ratios were calculated for treatment comparisons versus placebo. (NCT01119846)
Timeframe: Baseline (Day 1 pre-dose) and Day -1, 13 and 14

,,,,,
InterventionMillimoles per Liter (Geometric Mean)
Day 7, 1 HourDay 7, 2 HoursDay 7, 4 HoursDay 7, 6 HoursDay 7, 10 HoursDay 7, 12 HoursDay 14, 24 Hours
Part C: GSK1292263 150 mg BID117.1594.1820.1088.7055.2895.161.51
Part C: GSK1292263 300 mg BID151.56143.7527.32136.1555.4098.263.54
Part C: GSK1292263 50 mg BID158.9192.1735.05103.5268.08107.5212.45
Part C: GSK1292263 600 mg Once Daily129.4487.3021.93131.0866.90114.9311.03
Part C: Placebo216.95160.5719.41142.1064.04138.427.87
Part C: Sitagliptin 100 mg162.83163.4630.25130.8839.35123.653.26

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Part C: Summary of Change From Baseline in Fasted Glucose

Blood samples were collected fasting pre-breakfast and pre-morning dose (PD time 0) on Days -1, 13 and 14 and then at 10, 20, 30, 60, 90, 120, 180 min after eating the standardized breakfast meal tolerance test. For lunch (4 hour post-morning dose) samples were collected just before the meal and after starting each meal: 0.5, 1, 1.5, 2 and 3 hours. For the evening meal (10 hour post-morning dose), BID dosing groups followed the sequence of sampling, food and dosing as for breakfast (PD sample immediately before meal, eat and then dose), then 0.5, 1, 1.5, 2 and 3 hours post-dinner. A sample was also collected 24 hours post-dose. When this results in multiple samples at the same time point, only one sample was collected. Change from Baseline was calculated by subtracting Baseline value minus post-Baseline value. The point estimates and corresponding 95% CI for treatment ratios were calculated for treatment comparisons versus placebo. (NCT01119846)
Timeframe: Baseline (Day 1 pre-dose) and Day -1, 13 and 14.

,,,,,
InterventionMillimoles per Liter (Geometric Mean)
Day 7, 1 HourDay 7, 2 HoursDay 7, 4 HoursDay 7, 6 HoursDay 7, 10 HoursDay 7, 12 HoursDay 14, 24 Hours
Part C: GSK1292263 150 mg BID4.933.651.113.721.912.421.09
Part C: GSK1292263 300 mg BID7.395.001.136.163.184.411.34
Part C: GSK1292263 50 mg BID4.604.711.854.982.073.661.26
Part C: GSK1292263 600 mg Once Daily5.173.612.054.153.133.531.21
Part C: Placebo5.512.590.953.932.063.771.52
Part C: Sitagliptin 100 mg4.093.172.133.705.173.332.08

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Part C: Summary of AUC0-24, AUC0-t of GSK1292263 and Sitagliptin When Co-administered

The AUC0-10, AUC0-12 and AUC0-24 determined using the linear trapezoidal rule for increasing concentrations and the logarithmic trapezoidal rule for decreasing concentrations. When GSK1292263 was dosed once daily, blood samples were collected on Days 1, 13 and 14 immediately pre-dose (time 0) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-dose. When GSK1292263 was dosed BID, blood samples were collected on Days 1, 13 and 14, at immediately pre-morning dose, 1,2, 4, 6, 8, 10, 11, 12, 14, 16, 18 and 24 hours post-morning dose. For once daily and BID dosing regimens on Day 7, blood samples were collected at pre-dose (= post- breakfast), 1, 2, 4 (= pre lunch), 6, 10 (= immediately post-dinner) and 12 hours. When planned PK sampling results in multiple samples at the same time point, only one sample was collected. (NCT01119846)
Timeframe: Days 1, 7, 13 and 14

,,,,,
InterventionNanograms×hour per mL (Geometric Mean)
AUC 0-24, Day 14AUC 0-t, Day 14
Part C: GSK1292263 150 mg BID2585.152585.10
Part C: GSK1292263 300 mg BID3338.493338.27
Part C: GSK1292263 50 mg BID2701.812701.79
Part C: GSK1292263 600 mg Once Daily3012.703012.70
Part C: Placebo2437.102436.88
Part C: Sitagliptin 100 mg3027.993027.81

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Part C: Summary of AUC0-10, AUC0-12 and AUC0-24

The AUC0-10, AUC0-12 and AUC0-24 determined using the linear trapezoidal rule for increasing concentrations and the logarithmic trapezoidal rule for decreasing concentrations. When GSK1292263 was dosed once daily, blood samples were collected on Days 1, 13 and 14 immediately pre-dose (time 0) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-dose. When GSK1292263 was dosed BID, blood samples were collected on Days 1, 13 and 14, at immediately pre-morning dose, 1,2, 4, 6, 8, 10, 11, 12, 14, 16, 18 and 24 hours post-morning dose. For QD and BID dosing regimens on Day 7, blood samples were collected at pre-dose (=post- breakfast), 1, 2, 4 (=pre lunch), 6, 10 (=immediately post-dinner) and 12 hours. When planned PK sampling results in multiple samples at the same time point, only one sample was collected. (NCT01119846)
Timeframe: Days 1, 7, 13 and 14

,,,
InterventionRatio (Geometric Mean)
AUC 0-10, Day 1AUC 0-10, Day 13AUC 0-10, Day 14AUC 0-12, Day 7AUC 0-24, Day 1AUC 0-24, Day 13AUC 0-24, Day 14
Part C: GSK1292263 150 mg BID1868.875869.825723.556413.056439.5614463.5014356.75
Part C: GSK1292263 300 mg BID3076.527332.267451.139965.1411078.9718682.3419134.61
Part C: GSK1292263 50 mg BID1127.453167.193179.513559.593552.467776.268026.26
Part C: GSK1292263 600 mg Once Daily4003.805348.215470.576268.957153.169388.9310166.83

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Part C: Summary of Accumulation Ratio (Ro)

Ro was derived as follows: Ro = Day 13 (AUC0-24)/Day 1 (AUC0-24) for once daily dosing; Ro = Day 13 AM (AUC0-10)/Day 1 AM (AUC0-10) for BID dosing and Ro = Day 13 (AUC0-24)/Day 1 (AUC0-24) for BID dosing. When GSK1292263 was dosed once daily, blood samples were collected on Days 1, 13 and 14 immediately pre-dose (time 0) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-dose. When GSK1292263 was dosed BID, blood samples were collected on Days 1, 13 and 14, at immediately pre-morning dose, 1,2, 4, 6, 8, 10, 11, 12, 14, 16, 18 and 24 hours post-morning dose. For once daily and BID dosing regimens on Day 7, blood samples were collected at pre-dose (= post-breakfast), 1, 2, 4 (= pre-lunch), 6, 10 (=immediately post-dinner) and 12 hours. When planned PK sampling results in multiple samples at the same time point, only one sample was collected. Data presented for Day 13 and Day 14. (NCT01119846)
Timeframe: Days 1, 7, 13 and 14

,,,
InterventionRatio (Geometric Mean)
Day 13Day 14
Part C: GSK1292263 150 mg BID2.172.15
Part C: GSK1292263 300 mg BID1.721.77
Part C: GSK1292263 50 mg BID2.222.29
Part C: GSK1292263 600 mg Once Daily1.291.39

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Part C: Relationships Between GSK1292263 Drug Exposures and Insulin Sensitivity

"Blood samples for the determination of insulin were collected fasting pre-breakfast and then pre-morning dose (PD time 0) on Days -1, 13 and 14, and then at 10, 20, 30, 60, 90, 120, 180 min after eating the standardized breakfast meal tolerance test. For lunch (approximately 4 hour post-morning dose) samples were collected just before the meal and at the following times after starting each meal: 0.5, 1, 1.5, 2 and 3 hours. For the evening meal (approximately 10 hour post-morning dose), BID dosing groups followed the sequence of sampling, food and dosing as for breakfast (PD sample immediately before meal, eat and then dose), then 0.5, 1, 1.5, 2 and 3 hours post-dinner. A sample was also collected 24 hours post-dose.~When this results in multiple samples at the same time point, only one sample was collected (example: 24 hours post first-dose = pre-dose [time 0] for the second dose)." (NCT01119846)
Timeframe: Day -1, 13 and 14

,,,,,
InterventionmL/min×1/µIU×10^4 (Geometric Mean)
Day -1Day 13Day 14
Part C: GSK1292263 150 mg BID9.88.69.0
Part C: GSK1292263 300 mg BID9.28.77.3
Part C: GSK1292263 50 mg BID6.45.65.7
Part C: GSK1292263 600 mg Once Daily8.07.28.0
Part C: Placebo6.66.66.8
Part C: Sitagliptin 100 mg7.07.45.7

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Part C: Number of Participants With AEs and SAEs

An AE was defined as any untoward MO in a participant temporally associated with the use of a MP, whether or not considered related to the MP and can therefore be any unfavourable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with its use. The SAE was any untoward MO that, at any dose, results in death, life threatening, persistent or significant disability/incapacity, results in or prolongs inpatient hospitalization, congenital abnormality or birth defect, that may not be immediately life-threatening or result in death or hospitalization but may jeopardize the participant or may require medical or surgical intervention to prevent one of the other outcomes listed in this definition. (NCT01119846)
Timeframe: Up to Week 7

,,,,,
InterventionParticipants (Count of Participants)
Any AEAny SAE
Part C: GSK1292263 150 mg BID50
Part C: GSK1292263 300 mg BID10
Part C: GSK1292263 50 mg BID40
Part C: GSK1292263 600 mg Once Daily40
Part C: Placebo40
Part C: Sitagliptin 100 mg20

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Part C: Number of Participants With Abnormal Vital Signs of PCI

SBP, DBP and pulse rate measurements were recorded at each time point, assessment was performed after resting in a supine or semi-supine position for at least 10 minutes. Participants with abnormal clinically significant vital signs findings is presented. It was assessed on Screening, on Days -1 to 14 in a fasting state early in the morning (prior to morning dosing on days 1-14) and at Follow-up. On Days 1, 7, 13 and 14, it was also taken at 1, 3, 6, 9, 12 and 24 hours after the morning dose each treatment period and Follow-up (7 to 10 days after final discharge). (NCT01119846)
Timeframe: Up to Week 7

,,,,,
InterventionParticipants (Count of Participants)
SBP, LowSBP, HighPulse rate, High
Part C: GSK1292263 150 mg BID000
Part C: GSK1292263 300 mg BID010
Part C: GSK1292263 50 mg BID000
Part C: GSK1292263 600 mg Once Daily101
Part C: Placebo020
Part C: Sitagliptin 100 mg000

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Part C: Number of Participants With Abnormal Hematology Parameters of PCI

Hematology parameters included platelet count, RBC count, MCV, total neutrophils, WBC absolute, MCH, lymphocytes, MCHC, monocytes, hemoglobin, eosinophils, hematocrit, reticulocytes and basophils. It was assessed on Screening, Day -2 (can be non-fasting) and prior to breakfast (early in the morning, fasting) on Days 1, 7 and 14, and on Day 15 prior to checkout, (=24 hours post-dose) of each treatment period and Follow-up (7 to 10 days after final discharge). Only those parameters for which at least one value of PCI was reported are summarized. Null data is not presented. (NCT01119846)
Timeframe: Up to Week 7

,,,,,
InterventionParticipants (Count of Participants)
Hematocrit, HighHemoglobin, HighTotal neutrophils, Low
Part C: GSK1292263 150 mg BID000
Part C: GSK1292263 300 mg BID000
Part C: GSK1292263 50 mg BID000
Part C: GSK1292263 600 mg Once Daily122
Part C: Placebo000
Part C: Sitagliptin 100 mg021

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Part C: Summary of Plasma Cmax

The first occurrence of the maximum observed plasma concentration determined directly from the raw concentration-time data. When GSK1292263 was dosed once daily, blood samples were collected on Days 1, 13 and 14 immediately pre-dose (time 0) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-dose. When GSK1292263 was dosed BID, blood samples were collected on Days 1, 13 and 14, at immediately pre-morning dose, 1,2, 4, 6, 8, 10, 11, 12, 14, 16, 18 and 24 hours post-morning dose. For once daily and BID dosing regimens on Day 7, blood samples were collected at pre-dose (= post-breakfast), 1, 2, 4 (= pre-lunch), 6, 10 (=immediately post-dinner) and 12 hours. When planned PK sampling results in multiple samples at the same time point, only one sample was collected. (NCT01119846)
Timeframe: Days 1, 7, 13 and 14

,,,
InterventionNanograms per millimeter (Geometric Least Squares Mean)
Day 1Day 7Day 13Day 14
Part C: GSK1292263 150 mg BID364.73715.01732.05715.71
Part C: GSK1292263 300 mg BID584.321149.32969.19950.52
Part C: GSK1292263 50 mg BID219.36410.98433.12438.36
Part C: GSK1292263 600 mg Once Daily721.18813.03831.23772.89

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Part A: Summary of the AUC 0-13, AUC 0-24, Incremental AUC (iAUC) 0-13 and iAUC 0-24 of Glucose

Blood samples for the determination of glucose were collected at pre-dose on Day 1 of each dosing period and immediately prior to and at 10, 20, 30, 60, 90, 120, 180 min after administration of the 75 grams glucose drink. For lunch and evening meal in Part A, samples were collected just before the meal and at the following times after starting each meal: 0.5, 1, 1.5 (except breakfast in Part B), 2 and 3 hours. When this results in multiple samples at the same time point, only one sample was collected. The point estimates and corresponding 95% CI for treatment ratios were calculated for treatment comparisons versus placebo. (NCT01119846)
Timeframe: Up to Day 1 (24 hours)

,,,,
InterventionMillimoles per Liter (Geometric Mean)
AUC 0-13AUC 0-24iAUC 0-13iAUC 0-24
Part A: GSK1292263 150 mg9.159.031.481.44
Part A: GSK1292263 25 mg9.449.171.351.04
Part A: GSK1292263 800 mg8.648.671.780.90
Part A: Placebo9.428.722.111.18
Part A: Sitagliptin 100 mg9.238.951.480.53

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Part A: Summary of the OGTT AUC (0-2) and iAUC(0-2)- C-peptide, Total GIP, GLP-1 (Active and Total), Glucagon and Total PYY and AUC 0-3 and iAUC 0-3 of Insulin

Blood samples for the determination of glucose and other PD markers were collected at pre-dose on Day 1 of each dosing period and immediately prior to and at 10, 20, 30, 60, 90, 120, 180 min after administration of the 75 grams glucose drink. When this results in multiple samples at the same time point, only one sample was collected. The point estimates and corresponding 95% CI for treatment ratios were calculated for treatment comparisons versus placebo. (NCT01119846)
Timeframe: Up to Day 1 (24 hours)

,,,,
InterventionPico moles per Liter (Geometric Mean)
C-peptide, AUC 0-2C-peptide, iAUC 0-2GIP total, AUC 0-2GIP total, iAUC 0-2GLP-1 active, AUC 0-2GLP-1 active, iAUC 0-2GLP-1 total, AUC 0-2GLP-1 total, iAUC 0-2Glucagon, AUC 0-2Glucagon, iAUC 0-2Insulin, AUC 0-3Insulin, iAUC 0-3PYY total, AUC 0-2PYY total, iAUC 0-2
Part A: GSK1292263 150 mg1357.81620.9534.8229.272.180.185.022.406.080.62235.88161.0522.456.81
Part A: GSK1292263 25 mg1352.32676.2437.8631.502.12NA4.511.664.770.24230.91156.3219.304.66
Part A: GSK1292263 800 mg1387.78695.3142.2533.512.140.185.592.384.490.73254.61179.9323.425.59
Part A: Placebo1207.17563.7529.7325.302.120.034.452.653.600.56204.77146.0316.765.89
Part A: Sitagliptin 100 mg1287.66692.1126.5721.794.732.472.971.263.850.39213.17150.3313.931.25

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Part A: Summary of the OGTT AUC (0-3) and iAUC(0-3)-Glucose

Blood samples for the determination of glucose were collected at pre-dose on Day 1 of each dosing period and immediately prior to and at 10, 20, 30, 60, 90, 120, 180 min after administration of the 75 grams glucose drink. When this results in multiple samples at the same time point, only one sample was collected. The point estimates and corresponding 95% CI for treatment ratios were calculated for treatment comparisons versus placebo. (NCT01119846)
Timeframe: Up to Day 1 (24 hours)

,,,,
InterventionMillimoles per Liter (Geometric Mean)
AUC 0-3iAUC 0-3
Part A: GSK1292263 150 mg12.124.78
Part A: GSK1292263 25 mg12.795.17
Part A: GSK1292263 800 mg11.264.25
Part A: Placebo12.825.55
Part A: Sitagliptin 100 mg11.974.43

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Part A: Summary of the OGTT Derived Parameters: Glucose/Insulin and Insulin/Glucose Ratio

Blood samples for the determination of glucose and other PD markers were collected at pre-dose on Day 1 of each dosing period and immediately prior to and at 10, 20, 30, 60, 90, 120, 180 min after administration of the 75 grams glucose drink. When this results in multiple samples at the same time point, only one sample was collected. It was calculated as insulin/glucose ratio was calculated as insulin AUC(0-3]/glucose AUC(0-3) during OGTT, while glucose/insulin ratio was calculated as glucose AUC(0-3)/insulin AUC(0-3) during OGTT. The point estimates and corresponding 95% CI for treatment ratios were calculated for treatment comparisons versus placebo. (NCT01119846)
Timeframe: Up to Day 1 (24 hours)

,,,,
InterventionRatio (Geometric Mean)
G/I ratioI/G ratio
Part A: GSK1292263 150 mg0.0519.46
Part A: GSK1292263 25 mg0.0618.05
Part A: GSK1292263 800 mg0.0422.61
Part A: Placebo0.0615.98
Part A: Sitagliptin 100 mg0.0617.80

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Part A: Summary of Time to Maximum Concentration (T-max) and Lag Time Before Observation of Drug Concentration in Sampled Matrix (T-lag)

The time at which Cmax was observed was determined directly from the raw concentration-time data. The lag time before observation of drug concentrations in sample matrix determined as the time of the sample preceding the first quantifiable concentration. Blood samples for the determination of PK was collected on Day 1 of each period: immediately pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 14 and 24 hours. (NCT01119846)
Timeframe: Pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 14 and 24 hours on Day 1 of each treatment period

,,
InterventionHour (Median)
T-lagT-max
Part A: GSK1292263 150 mg0.003.00
Part A: GSK1292263 25 mg0.504.99
Part A: GSK1292263 800 mg0.003.00

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Part A: Summary of Maximum Plasma Concentration (Cmax)

The first occurrence of the maximum observed plasma concentration determined directly from the raw concentration-time data. Blood samples for the determination of PKs was collected at on Day 1 of each period: immediately pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 14 and 24 hours. (NCT01119846)
Timeframe: Pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 14 and 24 hours on Day 1 of each treatment period

InterventionNanograms per milliliters (Geometric Mean)
Part A: GSK1292263 25 mg52.04
Part A: GSK1292263 150 mg165.62
Part A: GSK1292263 800 mg379.79

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Part A: Number of Participants With Abnormal Electrocardiogram (ECG) Findings

Twelve-lead ECGs was obtained in a supine position at each time point during the study using an ECG machine that automatically measured PR, QRS, QT and QTc intervals (QT duration corrected for heart rate by Bazett's formula [QTcB] and Fridericia's formula [QTcF]). Participants with abnormal clinically significant ECG findings is presented. It was assessed on Screening, Day 1 at pre-dose, 1, 2, 3, 4, 6, 10, 16, 24 hours and Follow-up (7 to 10 days after final discharge). (NCT01119846)
Timeframe: Up to Week 10

InterventionParticipants (Count of Participants)
Part A: Placebo0
Part A: GSK1292263 25 mg0
Part A: GSK1292263 150 mg0
Part A: GSK1292263 800 mg0
Part A: Sitagliptin 100 mg0

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Part A: Number of Participants With Abnormal Hematology Parameters of Potential Clinical Importance (PCI)

Hematology parameters included platelet count, red blood cell (RBC) count, mean corpuscular volume (MCV), total neutrophils, white blood cell count (WBC; absolute), mean corpuscular hemoglobin (MCH), lymphocytes, mean corpuscular hemoglobin concentration (MCHC), monocytes, hemoglobin, eosinophils, hematocrit, reticulocytes and basophils. It was assessed on Screening, Day -1, Day 2 (of each treatment period) and Follow-up (7 to 10 days after final discharge). Only those parameters (hemoglobin, high) for which at least one value of PCI was reported are summarized. Null data is not presented. (NCT01119846)
Timeframe: Up to Week 10

InterventionParticipants (Count of Participants)
Part A: Placebo0
Part A: GSK1292263 25 mg0
Part A: GSK1292263 150 mg1
Part A: GSK1292263 800 mg0
Part A: Sitagliptin 100 mg1

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Part A: Number of Participants With Abnormal Vital Signs of PCI

Systolic blood pressure (SBP), diastolic blood pressure (DBP) and pulse rate measurements were recorded at each time point, assessment was performed after resting in a supine or semi-supine position for at least 10 minutes. Participants with abnormal clinically significant vital signs findings is presented. It was assessed on Screening, Day -1, 1, 2 (pre-dose, 1, 3, 4, 6, 10, 16 and 24 hours of each treatment period) and Follow-up (7 to10 days after final discharge). (NCT01119846)
Timeframe: Up to Week 10.

InterventionParticipants (Count of Participants)
Part A: Placebo0
Part A: GSK1292263 25 mg0
Part A: GSK1292263 150 mg0
Part A: GSK1292263 800 mg0
Part A: Sitagliptin 100 mg0

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Part A: Relationships Between GSK1292263 Drug Exposures and Insulin Sensitivity

Blood samples for the determination of insulin were collected at pre-dose on Day 1 of each dosing period and immediately prior to and at 10, 20, 30, 60, 90, 120, 180 min after administration of the 75 grams glucose drink. For lunch and evening meal in Part A, samples were collected just before the meal and at the following times after starting each meal: 0.5, 1, 1.5 (except breakfast in Part B), 2 and 3 hours. When this results in multiple samples at the same time point, only one sample was collected. The unit of measure is mL/min×1/micro international unit×10^4 (mL/min×1/µIU×10^4). (NCT01119846)
Timeframe: Day 1 of each treatment period

InterventionmL/min×1/µIU×10^4 (Geometric Mean)
Part A: Placebo1.4
Part A: GSK1292263 25 mg2.1
Part A: GSK1292263 150 mg2.3
Part A: GSK1292263 800 mg2.8
Part A: Sitagliptin 100 mg2.7

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Part A: Summary of Change From Baseline in Fasted Glucose

Blood samples for the determination of glucose were collected at pre-dose on Day 1 of each dosing period and immediately prior to and at 10, 20, 30, 60, 90, 120, 180 min after administration of the 75 grams glucose drink. For lunch and evening meal in Part A, samples were collected just before the meal and at the following times after starting each meal: 0.5, 1, 1.5 (except breakfast in Part B), 2 and 3 hours. When this results in multiple samples at the same time point, only one sample was collected. Change from Baseline was calculated by subtracting Baseline value from post-Baseline value. The point estimates and corresponding 95% CI for treatment ratios were calculated for treatment comparisons versus placebo. (NCT01119846)
Timeframe: Baseline (Day 1 pre-dose) and Day 1 (24 hours)

InterventionMillimoles per Liter (Geometric Mean)
Part A: Placebo0.52
Part A: GSK1292263 25 mg1.49
Part A: GSK1292263 150 mg0.53
Part A: GSK1292263 800 mg0.87
Part A: Sitagliptin 100 mg0.58

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Part A: Summary of the OGTT Derived Parameters: Disposition Index

Blood samples for the determination of glucose and other PD markers were collected at pre-dose on Day 1 of each dosing period and immediately prior to and at 10, 20, 30, 60, 90, 120, 180 min after administration of the 75 grams glucose drink. When this results in multiple samples at the same time point, only one sample was collected. It was calculated by multiplying insulin glucose index with insulin sensitivity index. The point estimates and corresponding 95% CI for treatment ratios were calculated for treatment comparisons versus placebo. (NCT01119846)
Timeframe: Up to Day 1 (24 hours)

Intervention[(µIU/mL)/(mg/deciliter [dL])]^2 (Geometric Mean)
Part A: Placebo0.87
Part A: GSK1292263 25 mg0.76
Part A: GSK1292263 150 mg1.07
Part A: GSK1292263 800 mg0.94
Part A: Sitagliptin 100 mg0.86

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Part A: Summary of the OGTT Derived Parameters: Insulin Glucose Index

Blood samples for the determination of glucose and other PD markers were collected at pre-dose on Day 1 of each dosing period and immediately prior to and at 10, 20, 30, 60, 90, 120, 180 min after administration of the 75 grams glucose drink. When this results in multiple samples at the same time point, only one sample was collected. It was calculated as insulin (30 min) - insulin (0 min)/glucose (30 min) - glucose (0 min). It was calculated as insulin (30 min) - insulin (0 min)/glucose (30 min) - glucose (0 min). The point estimates and corresponding 95% CI for treatment ratios were calculated for treatment comparisons versus placebo. (NCT01119846)
Timeframe: Up to Day 1 (24 hours)

InterventionµIU/mL/mg/dL (Geometric Mean)
Part A: Placebo0.23
Part A: GSK1292263 25 mg0.22
Part A: GSK1292263 150 mg0.28
Part A: GSK1292263 800 mg0.26
Part A: Sitagliptin 100 mg0.21

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Part A: Summary of the OGTT Derived Parameters: Insulin Sensitivity Index

Blood samples for the determination of glucose and other PD markers were collected at pre-dose on Day 1 of each dosing period and immediately prior to and at 10, 20, 30, 60, 90, 120, 180 min after administration of the 75 grams glucose drink. When this results in multiple samples at the same time point, only one sample was collected. It was calculated as 10,000/square root ([mean plasma insulin × mean plasma glucose during OGTT or meal challenge] × [fasting plasma glucose × fasting plasma insulin]). The point estimates and corresponding 95% CI for treatment ratios were calculated for treatment comparisons versus placebo. (NCT01119846)
Timeframe: Up to Day 1 (24 hours)

Intervention1/(mg/dL)×1/(µIU/mL) (Geometric Mean)
Part A: Placebo3.95
Part A: GSK1292263 25 mg3.47
Part A: GSK1292263 150 mg3.87
Part A: GSK1292263 800 mg3.60
Part A: Sitagliptin 100 mg4.01

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Part B: Number of Participants With Abnormal Clinical Chemistry Parameters of PCI

Clinical chemistry parameters included BUN, potassium, AST, total and direct bilirubin, creatinine, chloride, ALT, uric acid, glucose fasting, GGT, albumin, sodium, magnesium, phosphorus inorganic, calcium, total CO2, ALP, triglycerides, total cholesterol, LDL cholesterol, free fatty acid (NEFA), HDL cholesterol and total protein. It was assessed on Screening, Day -1, 2 (of each treatment period) and Follow-up (7 to 10 days after final discharge). Only those parameters (Glucose, High) for which at least one value of PCI was reported are summarized. Null data is not presented. (NCT01119846)
Timeframe: Up to Week 7

InterventionParticipants (Count of Participants)
Part B: GSK1292263 800 mg Fasted Condition Orally1
Part B: GSK1292263 800 mg Fed Condition Orally1

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Part B: Number of Participants With Abnormal Hematology Parameters of PCI

Hematology parameters included platelet count, RBC count, MCV, total neutrophils, WBC absolute, MCH, lymphocytes, MCHC, monocytes, hemoglobin, eosinophils, hematocrit, reticulocytes and basophils. It was assessed on Screening, Day -1, 2 (of each treatment period) and Follow-up (7 to 10 days after final discharge). Only those parameters for which at least one value of PCI was reported are summarized. Null data is not presented. (NCT01119846)
Timeframe: Up to Week 7

InterventionParticipants (Count of Participants)
Part B: GSK1292263 800 mg Fasted Condition Orally0
Part B: GSK1292263 800 mg Fed Condition Orally0

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Part B: Number of Participants With Abnormal Vital Signs of PCI

SBP, DBP and pulse rate measurements were recorded at each time point, assessment was performed after resting in a supine or semi-supine position for at least 10 min. Participants with abnormal clinically significant vital signs findings is presented. It was assessed on Screening, Day -1, 1, 2 (pre-dose, 1, 3, 4, 6, 10, 16 and 24 hours of each treatment period) and Follow-up (7 -10 days after final discharge). (NCT01119846)
Timeframe: Up to Week 7

InterventionParticipants (Count of Participants)
Part B: GSK1292263 800 mg Fasted Condition Orally0
Part B: GSK1292263 800 mg Fed Condition Orally0

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Part B: Number of Participants With Significant ECG Abnormalities

Twelve-lead ECGs was obtained in a supine position at each time point during the study using an ECG machine that automatically measured PR, QRS, QT and QTc intervals (QTcB and QTcF). Participants with abnormal clinically significant ECG findings is presented. It was assessed on Screening, Day 1 at pre-dose, 1, 2, 3, 4, 6, 10, 16, 24 hours and Follow-up (7 -10 days after final discharge). (NCT01119846)
Timeframe: Up to Week 7

InterventionParticipants (Count of Participants)
Part B: GSK1292263 800 mg Fasted Condition Orally0
Part B: GSK1292263 800 mg Fed Condition Orally0

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Part B: Summary of Change From Baseline in Fasted Glucose

Blood samples for the determination of glucose were collected at pre-dose on Day 1 of each dosing period and immediately prior to and at 10, 20, 30, 60, 90, 120, 180 min after administration of the 75 grams glucose drink. For lunch and evening meal in Part A, samples were collected just before the meal and at the following times after starting each meal: 0.5, 1, 1.5 (except breakfast in Part B), 2 and 3 hours. When this results in multiple samples at the same time point, only one sample was collected. Change from Baseline was calculated by subtracting Baseline value from post-Baseline value. (NCT01119846)
Timeframe: Baseline (Day 1 pre-dose) and Day 1 (24 hours)

InterventionMillimoles per Liter (Geometric Mean)
Part B: GSK1292263 800 mg Fasted Condition Orally0.40
Part B: GSK1292263 800 mg Fed Condition Orally1.95

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Part B: Summary of Plasma Cmax

The first occurrence of the maximum observed plasma concentration determined directly from the raw concentration-time data. Blood samples for the determination of PK was collected at on Day 1 of each period: immediately pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 13 and 24 hours. (NCT01119846)
Timeframe: Pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 13 and 24 hours on Day 1 of each treatment period.

InterventionNanograms per mL (Geometric Mean)
Part B: GSK1292263 800 mg Fasted Condition Orally339.52
Part B: GSK1292263 800 mg Fed Condition Orally944.21

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Part C: Number of Participants With Significant ECG Abnormalities

Twelve-lead ECGs was obtained in a supine position at each time point during the study using an ECG machine that automatically measured PR, QRS, QT and QTc intervals (QTcB and QTcF). Participants with abnormal clinically significant ECG findings is presented. It was assessed on Screening, on Day -1, 1, 7, 13 and 14 pre-breakfast dose (fasting) and at 1, 3, 6, 9, 12 and 24 hours of each treatment period and Follow-up (7 to 10 days after final discharge). (NCT01119846)
Timeframe: Up to Week 7

InterventionParticipants (Count of Participants)
Part C: GSK1292263 50 mg BID0
Part C: GSK1292263 150 mg BID0
Part C: GSK1292263 300 mg BID0
Part C: GSK1292263 600 mg Once Daily0
Part C: Placebo0
Part C: Sitagliptin 100 mg0

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Part C: Summary of Cmax of GSK1292263 and Sitagliptin When Co-administered

The first occurrence of the maximum observed plasma concentration determined directly from the raw concentration-time data. When GSK1292263 was dosed once daily, blood samples were collected on Days 1, 13 and 14 immediately pre-dose (time 0) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-dose. When GSK1292263 was dosed BID, blood samples were collected on Days 1, 13 and 14, at immediately pre-morning dose, 1,2, 4, 6, 8, 10, 11, 12, 14, 16, 18 and 24 hours post-morning dose. For once daily and BID dosing regimens on Day 7, blood samples were collected at pre-dose (= post-breakfast), 1, 2, 4 (= pre-lunch), 6, 10 (= immediately post-dinner) and 12 hours. When planned PK sampling results in multiple samples at the same time point, only one sample was collected. (NCT01119846)
Timeframe: Days 1, 7, 13 and 14

InterventionNanograms per mL (Geometric Mean)
Part C: GSK1292263 50 mg BID301.89
Part C: GSK1292263 150 mg BID284.59
Part C: GSK1292263 300 mg BID458.24
Part C: GSK1292263 600 mg Once Daily378.12
Part C: Placebo307.45
Part C: Sitagliptin 100 mg360.91

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Part C: Summary of Time Invariance Ratio (Rs) of AUC0-10 for BID Dose of GSK1292263

The AUC0-10 determined using the linear trapezoidal rule for increasing concentrations and the logarithmic trapezoidal rule for decreasing concentrations. When GSK1292263 was dosed once daily, blood samples were collected on Days 1, 13 and 14 immediately pre-dose (time 0) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-dose. When GSK1292263 was dosed BID, blood samples were collected on Days 1, 13 and 14, at immediately pre-morning dose, 1,2, 4, 6, 8, 10, 11, 12, 14, 16, 18 and 24 hours post-morning dose. For once daily and BID dosing regimens on Day 7, blood samples were collected at pre-dose (=post-breakfast), 1, 2, 4 (=pre lunch), 6, 10 (=immediately post-dinner) and 12 hours. When planned PK sampling results in multiple samples at the same time point, only one sample was collected. (NCT01119846)
Timeframe: Days 1, 7, 13 and 14

InterventionRatio (Geometric Mean)
Part C: GSK1292263 50 mg BID2.8174
Part C: GSK1292263 150 mg BID3.0033
Part C: GSK1292263 300 mg BID2.4218

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Part C: Summary of Time Invariance Ratio (Rs) of AUC0-24 for Once Daily Dose of GSK1292263

The AUC0-24 determined using the linear trapezoidal rule for increasing concentrations and the logarithmic trapezoidal rule for decreasing concentrations. When GSK1292263 was dosed once daily, blood samples were collected on Days 1, 13 and 14 immediately pre-dose (time 0) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-dose. When GSK1292263 was dosed BID, blood samples were collected on Days 1, 13 and 14, at immediately pre-morning dose, 1,2, 4, 6, 8, 10, 11, 12, 14, 16, 18 and 24 hours post-morning dose. For once daily and BID dosing regimens on Day 7, blood samples were collected at pre-dose (=post-breakfast), 1, 2, 4 (=pre lunch), 6, 10 (=immediately post-dinner) and 12 hours. When planned PK sampling results in multiple samples at the same time point, only one sample was collected. (NCT01119846)
Timeframe: Days 1, 7, 13 and 14

InterventionRatio (Geometric Mean)
Part C: GSK1292263 600 mg Once Daily1.2871

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Part C: Summary of Time Invariance Ratio (Rs) of Cmax

The first occurrence of the maximum observed plasma concentration determined directly from the raw concentration-time data. When GSK1292263 was dosed once daily, blood samples were collected on Days 1, 13 and 14 immediately pre-dose (time 0) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-dose. When GSK1292263 was dosed BID, blood samples were collected on Days 1, 13 and 14, at immediately pre-morning dose, 1,2, 4, 6, 8, 10, 11, 12, 14, 16, 18 and 24 hours post-morning dose. For once daily and BID dosing regimens on Day 7, blood samples were collected at pre-dose (=post-breakfast), 1, 2, 4 (=pre lunch), 6, 10 (=immediately post-dinner) and 12 hours. When planned PK sampling results in multiple samples at the same time point, only one sample was collected. Cmax for one participant from 50 BID x 14 day was not analyzed due to positive definite G Matrix. (NCT01119846)
Timeframe: Days 1, 7, 13 and 14

InterventionRatio (Geometric Least Squares Mean)
Part C: GSK1292263 150 mg BID1.9186
Part C: GSK1292263 300 mg BID1.6755
Part C: GSK1292263 600 mg Once Daily1.1703

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Part A: Number of Participants With Abnormal Clinical Chemistry Parameters of PCI

Clinical chemistry parameters included blood urea nitrogen (BUN), potassium, aspartate aminotransferase (AST), total and direct bilirubin, creatinine, chloride, alanine aminotransferase (ALT), uric acid, glucose fasting, gamma glutamyltransferase (GGT), albumin, sodium, magnesium, phosphorus inorganic, calcium, total carbon dioxide (CO2), alkaline phosphatase (ALP), triglycerides, total cholesterol, low-density lipoprotein (LDL) cholesterol, free fatty acid (non-esterified fatty acids; [NEFA]), high-density lipoprotein (HDL) cholesterol and total protein. It was assessed on Screening, Day -1, Day 2 (of each treatment period) and Follow-up (7 to 10 days after final discharge). Only those parameters for which at least one value of PCI was reported are summarized. Null data is not presented. (NCT01119846)
Timeframe: Up to Week 10

,,,,
InterventionParticipants (Count of Participants)
Glucose, HighCO2, LowMagnesium, High
Part A: GSK1292263 150 mg000
Part A: GSK1292263 25 mg110
Part A: GSK1292263 800 mg000
Part A: Placebo000
Part A: Sitagliptin 100 mg001

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Part A: Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

An AE was defined as any untoward medical occurrence (MO) in a participant temporally associated with the use of a medicinal product (MP), whether or not considered related to the MP and can therefore be any unfavourable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with its use. The SAE was any untoward MO that, at any dose, results in death, life threatening, persistent or significant disability/incapacity, results in or prolongs inpatient hospitalization, congenital abnormality or birth defect, that may not be immediately life-threatening or result in death or hospitalization but may jeopardize the participant or may require medical or surgical intervention to prevent one of the other outcomes listed in this definition. (NCT01119846)
Timeframe: Up to Week 10

,,,,
InterventionParticipants (Count of Participants)
Any AEAny SAE
Part A: GSK1292263 150 mg20
Part A: GSK1292263 25 mg20
Part A: GSK1292263 800 mg40
Part A: Placebo20
Part A: Sitagliptin 100 mg20

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Part A: Summary of Area Under the Concentration-time Curve From Time Zero (Pre-dose) to Last Time of Quantifiable Concentration (AUC0-t) and Area Under the Concentration-time Curve From Zero (Pre-dose) to 24 Hours (AUC0-24)

The AUC 0-24 and AUC 0-t determined using the linear trapezoidal rule for increasing concentrations and the logarithmic trapezoidal rule for decreasing concentrations. Blood samples for the determination of PK was collected at on Day 1 of each period: immediately pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 14 and 24 hours. (NCT01119846)
Timeframe: Pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 14 and 24 hours on Day 1 of each treatment period

,,
InterventionNanograms×hour per milliliters (Geometric Mean)
AUC 0-24AUC 0-t
Part A: GSK1292263 150 mg1684.861685.44
Part A: GSK1292263 25 mg524.30526.88
Part A: GSK1292263 800 mg3985.723979.35

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Part A: Summary of the AUC 0-12 and iAUC 0-12 of Glucagon, Glucagon-like Peptide (GLP; Active and Total)-1, C-peptide, Total Glucose-dependent Insulinotropic Peptide (GIP) and Total Peptide Tyrosine-tyrosine (PYY) and AUC 0-13 and iAUC 0-13 of Insulin

Blood samples for the determination of glucose and other PD markers were collected at pre-dose on Day 1 of each dosing period and immediately prior to and at 10, 20, 30, 60, 90, 120, 180 min after administration of the 75 grams glucose drink. For lunch and evening meal in Part A, samples were collected just before the meal and at the following times after starting each meal: 0.5, 1, 1.5 (except breakfast in Part B), 2 and 3 hours. When this results in multiple samples at the same time point, only one sample was collected. The point estimates and corresponding 95% CI for treatment ratios were calculated for treatment comparisons versus placebo. (NCT01119846)
Timeframe: Up to Day 1 (24 hours)

,,,,
InterventionPico moles per Liter (Geometric Mean)
C-peptide, AUC 0-12C-peptide, iAUC 0-12GIP total, AUC 0-12GIP total, iAUC 0-12GLP-1 active, AUC 0-12GLP-1 active, iAUC 0-12GLP-1 total, AUC 0-12GLP-1 total, iAUC 0-12Glucagon, AUC 0-12Glucagon, iAUC 0-12Insulin, AUC 0-13Insulin, iAUC 0-13PYY total, AUC 0-12PYY total, iAUC 0-12
Part A: GSK1292263 150 mg1523.99821.4644.0738.522.260.126.133.6410.622.60277.10207.0230.4615.56
Part A: GSK1292263 25 mg1518.81874.4144.9138.772.120.065.833.349.552.81272.04199.4229.7215.04
Part A: GSK1292263 800 mg1513.90846.3451.2142.152.200.077.444.339.341.97280.90208.1935.3817.74
Part A: Placebo1533.54920.6239.9935.362.140.055.663.358.113.77267.68211.9523.0410.34
Part A: Sitagliptin 100 mg1418.12836.9832.7628.035.353.054.042.367.441.86210.66151.5317.673.79

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Mean Value of Urine Albumin (Part B)

Urine samples were collected at screening, on Day -2, and on Days 1, 7, 15 and at follow-up. Urine albumin was assessed using quantitative analysis. (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 15) in Part B

,,,,
Interventionmg/L (Mean)
Day 1, pre-breakfastDay 7, pre-breakfastDay 14, 24 hoursFollow up
GSK1292263 300 mg8.724.511.417.6
GSK1292263 600 mg15.724.011.029.5
GSK1292263 75 mg17.719.528.326.1
Placebo15.38.07.854.0
Sitagliptin 50 mg6.67.310.411.2

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Lag Time Before Observation of Drug Concentrations in Sampled Matrix (Tlag) and Time of Occurrence of Cmax (Tmax) Following a Single Dose of GSK1292263 (Part A)

Blood samples for the determination of PK were collected on Day 1 Immediately pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 13, 24 and 48 hours post-dose. PK samples for 2 participants were not analyzed. The PK parameters were calculated by standard non-compartmental analysis. Tmax was determined directly from the raw concentration-time data. Tlag was determined as the time of the sample preceding the first quantifiable concentration, on Day 1 only. (NCT01128621)
Timeframe: On Day 1 Immediately pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 13, 24 and 48 hours post-dose.

Interventionhour (Median)
TlagTmax
Part A0.0005.00

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Mean Accumulation Ratio by AUC (0-10), AUC (0-24) and Cmax for GSK1292263 (Part B)

Accumulation ratio (Ro) was derived as: Ro = Day 14 morning AUC(0-10)/Day 1 morning AUC(0-10) (for BID regimens only). Ro = Day 14 AUC(0-24)/Day 1 AUC(0-24) (for both BID and once daily regimens). Accumulation ratio (RCmax)= Day 14 Cmax/Day 1 Cmax. RCmax was not computed for each dosing period (morning and evening). (NCT01128621)
Timeframe: On Days 1 and 14, at immediately pre-morning dose, 1, 2, 4, 6, 8, 10, 11, 12, 14, 16, 18, 24 and 48 hours post-morning dose.

,,
InterventionRatio (Mean)
AUC (0-10)AUC (0-24)Cmax
GSK1292263 300 mg1.92301.55281.3137
GSK1292263 600 mgNA1.37301.1077
GSK1292263 75 mg2.73802.06191.6438

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Mean Value of Urine pH (Part A)

Urine samples were collected at screening, Day -1, at 24hr post- dose (Day 2), and at follow-up. Urinalysis parameters included urine pH assessed using dipstick analysis. pH is calculated on a scale of 0 to 14, such that, the lower the number, more acidic the urine and higher the number, more alkaline the urine with 7 being neutral. (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 2) in Part A

InterventionpH (Mean)
Day 1, 24 hoursFollow up
Part A6.175.92

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Mean Value of Urine pH (Part B)

Urine samples were collected at screening, on Day -2, and on Days 1, 7, 15 and at follow-up. Urinalysis parameters included urine pH assessed using dipstick analysis. pH is calculated on a scale of 0 to 14, such that, the lower the number, more acidic the urine and higher the number, more alkaline the urine with 7 being neutral. (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 15) in Part B

,,,,
InterventionpH (Mean)
Day 1, pre-breakfastDay 7, pre-breakfastDay 14, 24 hoursFollow up
GSK1292263 300 mg6.046.006.175.96
GSK1292263 600 mg6.036.076.076.08
GSK1292263 75 mg6.045.856.045.88
Placebo6.046.115.966.15
Sitagliptin 50 mg5.926.046.085.88

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Mean Value of Urine Specific Gravity (Part A)

Urine samples were collected at screening, Day -1, at 24hr post- dose (Day 2), and at follow-up. Urinalysis parameter include urine specific gravity. Urinary specific gravity is a measure of the concentration of solutes in the urine . It measures the ratio of urine density compared with water density and provides information on the kidney's ability to concentrate urine . (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 2) in Part A

InterventionRatio (Mean)
Day 1, 24 hoursFollow up
Arm A1.01501.0210

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Mean Value of Urine Specific Gravity (Part B)

Urine samples were collected at screening, on Day -2, and on Days 1, 7, 15 and at follow-up. Urinalysis parameter include urine specific gravity. Urinary specific gravity is a measure of the concentration of solutes in the urine . It measures the ratio of urine density compared with water density and provides information on the kidney's ability to concentrate urine . (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 15) in Part B

,,,,
InterventionRatio (Mean)
Day 1, pre-breakfastDay 7, pre-breakfastDay 14, 24 hoursFollow up
GSK1292263 300 mg1.01251.01501.01431.0185
GSK1292263 600 mg1.01321.01251.01271.0172
GSK1292263 75 mg1.01441.01771.01611.0163
Placebo1.01271.01441.01701.0200
Sitagliptin 50 mg1.01351.01411.01381.0165

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Number of Participants With Abnormal Clinical Chemistry Values of PCI (Part B)

Blood samples for chemistry assessments were collected at screening, on Day -2 (non-fasting), and prior to breakfast (early in the morning, fasting) on Days 1, 7, and on Day 15 prior to checkout, (=24hrs post-dose), and at follow-up. Clinical chemistry parameters: Aspartate amino transferase (unit: international unit per liter [IU/L]) and Total bilirubin (unit: micromoles per liter (µmol/L) were assessed for abnormal values of PCI. For aspartate aminotransferase the PCI range was >=2 x ULN (high). For total bilirubin the PCI range was >=1.5 x ULN (high). (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 15) in Part B

,,,,
InterventionParticipants (Count of Participants)
Aspartate aminotransferase, highTotal bilirubin, high
GSK1292263 300 mg00
GSK1292263 600 mg10
GSK1292263 75 mg00
Placebo00
Sitagliptin 50 mg01

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Number of Participants With Abnormal Electrocardiogram (ECG) Findings (Part A)

ECGs were taken at Screening, pre-breakfast on Day -1, on Day 1 (pre-breakfast, 1 hour, 2, 3, 4, 6, 8, 13, 24hours post-dose), and at follow-up. Assessments were made in triplicate on Day 1 at the pre-breakfast time point, and single assessments were made at all other times. ECGs were taken in supine position. The data has been presented as abnormal- not clinically significant (NCS) and abnormal-clinically significant (CS). (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 2) in Part A

InterventionParticipants (Count of Participants)
Day 1, pre-breakfast 1, abnormal-NCSDay 1, pre-breakfast 2, abnormal-NCSDay 1, pre-breakfast 3, abnormal-NCSDay 1, 1 hour, abnormal-NCSDay 1, 2 hour, abnormal-NCSDay 1, 3 hour, abnormal-NCSDay 1, 4 hour, abnormal-NCSDay 1, 6 hour, abnormal-NCSDay 1, 8 hour, abnormal-NCSDay 1, 13 hour, abnormal-NCSDay 1, 24 hour, abnormal-NCS
Part A32213321312

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Change From Baseline in Mean Fasted Glucose Value (Part B)

Baseline was considered to be Day -1 pre-breakfast value. The change from Baseline was calculated by subtracting the Baseline values from the individual post-randomization values. If either the Baseline or post-randomization value was missing, the change from Baseline is set to missing as well. If measurements were taken in triplicate, then the mean of the triplicate measurements was used as the Baseline. (NCT01128621)
Timeframe: Baseline and at pre-breakfast on Days -1 and 14, and then at 0.5, 1, 1.5, 2 and 3 hours post dose.

,,,,
Interventionmmol/L (Mean)
Day 7, pre-breakfastDay 14, pre-breakfastDay 14, 24 hours
GSK1292263 300 mg-0.28-0.810.66
GSK1292263 600 mg0.21-0.110.68
GSK1292263 75 mg-0.74-1.57-0.57
Placebo-0.53-0.74-0.01
Sitagliptin 50 mg-1.75-1.83-1.06

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Number of Participants With Abnormal Electrocardiogram (ECG) Findings (Part B)

ECGs were taken at Screening, pre-breakfast on Day -1 and at Follow-up. On Days 1, 7 and 14 ECGs were taken pre-breakfast (fasting) and at 1, 2, 4, 6, 8, 12 and 24hours post-dose. Triplicate ECGs were taken at the pre-breakfast time point, and single assessments were taken at all other times. ECGs were taken in supine position. The data has been presented as abnormal- not clinically significant (NCS) and abnormal-clinically significant (CS). (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 15) in Part B

,,,,
InterventionParticipants (Count of Participants)
Day 1, pre-breakfast 1, abnormal-NCSDay 1, pre-breakfast 2, abnormal-NCSDay 1, pre-breakfast 3, abnormal-NCSDay 1, 1 hour, abnormal-NCSDay 1, 1 hour, abnormal-CSDay 1, 2 hour, abnormal-NCSDay 1, 4 hour, abnormal-NCSDay 1, 6 hour, abnormal-NCSDay 1, 8 hour, abnormal-NCSDay 1, 12 hour, abnormal-NCSDay 1, 24 hour, abnormal-NCSDay 7, pre-breakfast 1, abnormal-NCSDay 7, pre-breakfast 2, abnormal-NCSDay 7, pre-breakfast 3, abnormal-NCSDay 7, 1 hour, abnormal-NCSDay 7, 2 hour, abnormal-NCSDay 7, 4 hour, abnormal-NCSDay 7, 6 hour, abnormal-NCSDay 7, 8 hour, abnormal-NCSDay 7, 12 hour, abnormal-NCSDay 7, 24 hour, abnormal-NCSDay 14, pre-breakfast 1, abnormal-NCSDay 14, pre-breakfast 2, abnormal-NCSDay 14, pre-breakfast 3, abnormal-NCSDay 14, 1 hour, abnormal-NCSDay 14, 2 hour, abnormal-NCSDay 14, 4 hour, abnormal-NCSDay 14, 6 hour, abnormal-NCSDay 14, 8 hour, abnormal-NCSDay 14, 12 hour, abnormal-NCSDay 14, 24 hour, abnormal-NCSFollow up-NCS
GSK1292263 300 mg45540344433443554343445454340552
GSK1292263 600 mg32260444433332233222333323321333
GSK1292263 75 mg22211122432233132342312132221212
Placebo21110112113121000012111111001111
Sitagliptin 50 mg34430223334323434533444422311233

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Number of Participants With Abnormal Hematology Values of PCI (Part B)

Blood samples for hematology assessments were collected at screening, on Day -2 (non-fasting), and prior to breakfast (early in the morning, fasting) on Days 1, 7, and on Day 15 prior to checkout, (=24hrs post-dose), and at follow-up. Hematology parameters: Hematocrit (unit: ratio) and hemoglobin (unit: grams per liter [g/L]), were assessed for abnormal values of PCI. The PCI range for hematocrit was: >0.075 decrease from Baseline (low), >1.02 x upper limit normal (ULN) (high-male), >1.17 x ULN (high-female). The PCI range for hemoglobin was: >25 decrease from Baseline (low), >1.03 x ULN (high-male), >1.13 x ULN (high-female). Data has been presented for the number of participants with hematology data values high from the PCI range in a consolidated format. (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 15) in Part B

,,,,
InterventionParticipants (Count of Participants)
Hematocrit, highHemoglobin, high
GSK1292263 300 mg01
GSK1292263 600 mg11
GSK1292263 75 mg11
Placebo00
Sitagliptin 50mg01

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Number of Participants With Abnormal Urinalysis Data Values (Part B)

Urinalysis parameters: Urine occult blood, Urine glucose, Urine ketones, Urine protein, White blood cells were assessed for abnormal findings by dipstick analysis. The abnormal findings were presented as trace, 1+, 2+ and 3+. Trace indicates lowest concentration of the mentioned parameters in urine and 3+ indicates highest concentration. Concentration of 3+ indicates worse outcome. (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 15) in Part B

,,,,
InterventionParticipants (Count of Participants)
Urine occult blood, Day 1, pre-breakfast, 3+Urine occult blood, Day 1, pre-breakfast, traceUrine occult blood, Day 7, pre-breakfast, traceUrine occult blood, Day 14, 24 hours, traceUrine occult blood, follow up, traceUrine glucose, Day 1, pre-breakfast, 1+Urine glucose, Day 1, pre-breakfast, 2+Urine glucose, Day 1, pre-breakfast, 3+Urine glucose, Day 1, pre-breakfast, traceUrine glucose, Day 7, pre-breakfast, 1+Urine glucose, Day 7, pre-breakfast, 2+Urine glucose, Day 7, pre-breakfast, traceUrine glucose, Day 14, 24 hours, 3+Urine glucose, Day 14, 24 hours, traceUrine glucose, follow up, 1+Urine glucose, follow up, 2+Urine glucose, follow up, 3+Urine glucose, follow up, traceUrine ketones, Day 1, pre-breakfast, traceUrine ketones, Day 7, pre-breakfast, traceUrine ketones, Day 14, 24 hours, traceUrine ketones, follow up, 1+Urine ketones, follow up, traceUrine protein, Day 1, pre-breakfast, traceUrine protein, Day 7, pre-breakfast, 1+Urine protein, Day 7, pre-breakfast, traceUrine protein, Day 14, 24 hours, traceUrine protein, follow up, 1+Urine protein, follow up, 2+Urine protein, follow up, traceWhite blood cells, Day 1, pre-breakfast, 1+White blood cells, Day 1, pre-breakfast, traceWhite blood cells, Day 7, pre-breakfast, 1+White blood cells, Day 7, pre-breakfast, traceWhite blood cells, Day 14, 24 hours, 1+White blood cells, Day 14, 24 hours, traceWhite blood cells, follow up, 1+White blood cells, follow up, 2+White blood cells, follow up, trace
GSK1292263 300 mg001000010002111041012110013014211200001
GSK1292263 600 mg000210011010110022120042111004010001000
GSK1292263 75 mg021220002000010202101002022103110111100
Placebo011201110101000112000000010113220105012
Sitagliptin 50 mg100000001000000001000001000001010111000

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Number of Participants With Abnormal Urinalysis Data Values by Dipstick Method (Part A)

Urinalysis parameters: Urine occult blood, Urine Glucose, Urine ketones and Urine protein were assessed for abnormal findings by dipstick analysis. The abnormalities were presented as trace, 1+, 2+ and 3+. Trace indicates lowest concentration of the mentioned parameters in urine and 3+ indicates highest concentration. Concentration of 3+ indicates worse outcome. (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 2) in Part A

InterventionParticipants (Count of Participants)
Urine occult blood, Day 1, 24 hours, traceUrine occult blood, follow up, traceUrine glucose, Day 1, 24 hours, 3+Urine glucose, follow up, 3+Urine glucose, follow up, traceUrine ketones, follow up, traceUrine protein, Day 1, 24 hours, traceUrine protein, follow up, trace
Part A11112212

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Number of Participants With Abnormal Vital Signs of PCI (Part A)

Assessment of vital signs (including systolic, diastolic blood pressure and heart rate) was performed at one time point at Screening, at follow-up and pre-breakfast on Day -1. On Day 1, they were taken at pre-breakfast, 1 hour, 3, 4, 6, 10, 16 and 24 hours post-dose. Assessments were made in triplicate at the pre-breakfast time point, and single assessments were made at all other times. Assessments were performed after resting in a supine or semi-supine position for at least 10 minutes. PCI value of systolic blood pressure: <85 and >160 millimeter of mercury (mmHg). PCI value of diastolic blood pressure: <45 and >100 mmHg. PCI value of heart rate: <40 and >110 beats per minute. (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 2) in Part A

InterventionParticipants (Count of Participants)
Blood pressure (systolic and diastolic)Heart rate, high
Part A01

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Number of Participants With Abnormal Vital Signs of PCI (Part B)

Assessment of vital signs (including systolic and diastolic blood pressure and heart rate) was performed at Screening, pre-breakfast on Days -1 to 14 in a fasting state early in the morning (prior to morning dosing on Days 1-14), and at Follow-up. On Days 1, 7 and 14, they were taken at 1, 3, 6, 9, 12 and 24 hours after the morning dose. At each time point, assessment was performed after resting in a supine or semi-supine position for at least 10 minutes. (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 15) in Part B

,,,,
InterventionParticipants (Count of Participants)
Systolic blood pressure, highHeart rate
GSK1292263 300 mg10
GSK1292263 600 mg00
GSK1292263 75 mg00
Placebo00
Sitagliptin 50 mg00

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Number of Participants With Any AEs and Serious Adverse Events SAEs (Part B)

An AE is defined as any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, is a congenital anomaly/birth defect, may jeopardize the participant or require medical or surgical intervention to prevent one of the other outcomes listed in the definition above, or is an event of possible drug-induced liver injury. (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 15) in Part B

,,,,
InterventionParticipants (Count of Participants)
Any AEAny SAE
GSK1292263 300 mg30
GSK1292263 600 mg40
GSK1292263 75 mg30
Placebo20
Sitagliptin 50 mg50

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Tmax and Tlag Following Repeat Dose of GSK1292263 (Part B)

Serial blood samples for the determination of the PK of GSK1292263 were collected on Days 1, 7 and 14. Blood samples for PK were collected on Days 1 and 14, at immediately pre-morning dose, 1, 2, 4, 6, 8, 10, 11, 12, 14, 16, 18, 24 and 48 hours post-morning dose. On Day 7, blood samples for PK were collected at pre-dose (post-breakfast), 1, 2, 4 (pre-lunch), 6 and 10 (immediately post-dinner, pre-dose for BID regimen). When planned PK sampling resulted in multiple samples at the same time point, only one sample was collected. The PK parameters were calculated by standard non-compartmental analysis. Tmax was determined directly from the raw concentration-time data. Tlag was determined as the time of the sample preceding the first quantifiable concentration, on Day 1 only. (NCT01128621)
Timeframe: On Days 1 and 14, at immediately pre-morning dose, 1, 2, 4, 6, 8, 10, 11, 12, 14, 16, 18, 24 and 48 hours post-morning dose. On Day 7, at pre-dose (post-breakfast), 1, 2, 4 (pre-lunch), 6 and 10 (immediately post-dinner, pre-dose for BID regimen).

,,
Interventionhour (Median)
Tlag, Day1Tmax, Day 1Tmax, Day 7Tmax, Day 14
GSK1292263 300 mg0.00014.004.0013.00
GSK1292263 600 mg0.0004.04.004.0
GSK1292263 75 mg0.00014.004.004.00

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Number of Participants With Any Adverse Events (AEs) and Serious Adverse Events (SAEs) (Part A)

An AE is defined as any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, is a congenital anomaly/birth defect, may jeopardize the participant or require medical or surgical intervention to prevent one of the other outcomes listed in the definition above, or is an event of possible drug-induced liver injury. (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 2) in Part A

InterventionParticipants (Count of Participants)
Any AEAny SAE
Part A00

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Change From Baseline in Mean Fasted Insulin Value (Part B)

Baseline was considered to be Day -1 pre-breakfast value. The change from Baseline was calculated by subtracting the Baseline values from the individual post-randomization values. If either the Baseline or post-randomization value was missing, the change from Baseline is set to missing as well. If measurements were taken in triplicate, then the mean of the triplicate measurements was used as the Baseline. (NCT01128621)
Timeframe: Baseline and at pre-breakfast on Days -1 and 14, and then at 0.5, 1, 1.5, 2 and 3 hours post dose.

,,,,
Interventionpmol/L (Mean)
Day 7, pre-breakfastDay 14, pre-breakfastDay 14, 24 hours
GSK1292263 300 mg-26.34-13.48-12.54
GSK1292263 600 mg-22.99-33.26-17.52
GSK1292263 75 mg-1.846.224.97
Placebo-2.744.8423.25
Sitagliptin 50 mg2.074.4327.47

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Change From Baseline in Weighted Mean for Glucose Value (Part B)

Baseline was considered to be Day -1 pre-breakfast value. The change from Baseline was calculated by subtracting the Baseline values from the individual post-randomization values. If either the Baseline or post-randomization value was missing, the change from Baseline is set to missing as well. If measurements were taken in triplicate, then the mean of the triplicate measurements was used as the Baseline. Weighted mean were assessed for (0-12) and (0-24). AUC with respect to that time interval was calculated using the linear trapezoidal rule. The weighted mean was determined by dividing the AUC by the observed length of the collection interval (time of last assessment - time of first assessment in hours). In order for the AUC to be calculated, the first and last time points and at least one additional assessment falling between the two must be non-missing. (NCT01128621)
Timeframe: Baseline and at pre-breakfast on Days -1 and 14, and then at 0.5, 1, 1.5, 2 and 3 hours post dose.

,,,,
Interventionmmol/L (Mean)
Weighted mean (0-12), Day 7Weighted mean (0-12), Day 14Weighted mean (0-24), Day 14
GSK1292263 300 mg0.5550.1230.321
GSK1292263 600 mg1.1030.6560.837
GSK1292263 75 mg-0.432-0.539-0.555
Placebo0.064-0.235-0.414
Sitagliptin 50 mg-0.862-1.039-1.025

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AUC From Time Zero (Pre-dose) to 10 Hours [AUC (0-10)] and AUC (0-24) Following Repeat Dose of GSK1292263 (Part B)

Serial blood samples for the determination of the PK of GSK1292263 were collected on Days 1, 7 and 14. Blood samples for PK were collected on Days 1 and 14, at immediately pre-morning dose, 1, 2, 4, 6, 8, 10, 11, 12, 14, 16, 18, 24 and 48 hours post-morning dose. On Day 7, blood samples for PK were collected at pre-dose (post-breakfast), 1, 2, 4 (pre-lunch), 6 and 10 (immediately post-dinner, pre-dose for BID regimen). When planned PK sampling resulted in multiple samples at the same time point, only one sample was collected. The PK parameters were calculated by standard non-compartmental analysis. AUC (0-10) and AUC (0-24) were determined using the linear trapezoidal rule for increasing concentrations and the logarithmic trapezoidal rule for decreasing concentrations. (NCT01128621)
Timeframe: On Days 1 and 14, at immediately pre-morning dose, 1, 2, 4, 6, 8, 10, 11, 12, 14, 16, 18, 24 and 48 hours post-morning dose. On Day 7, at pre-dose (post-breakfast), 1, 2, 4 (pre-lunch), 6 and 10 (immediately post-dinner, pre-dose for BID regimen).

,,
Interventionng*hr/mL (Geometric Mean)
AUC (0-10), Day 1AUC (0-10), Day 7AUC (0-10), Day 14AUC (0-24), Day 1AUC (0-24), Day 14
GSK1292263 300 mg3149.946472.686057.419968.8815479.48
GSK1292263 600 mgNA5205.86NA6791.909391.30
GSK1292263 75 mg1143.352930.473130.503775.767785.24

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Area Under the Concentration-time Curve From Zero (Pre-dose) to 24 Hours [AUC (0-24)] and AUC From Time Zero (Pre-dose) to Last Time of Quantifiable Concentration (AUC [0-last)] Following a Single Dose of GSK1292263 (Part A)

Blood samples for the determination of pharmacokinetics (PK) were collected on Day 1 Immediately pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 13, 24 and 48 hours post-dose. PK samples for 2 participants were not analyzed. The PK parameters were calculated by standard non-compartmental analysis. AUC (0-last) and AUC (0-24) were determined using the linear trapezoidal rule for increasing concentrations and the logarithmic trapezoidal rule for decreasing concentrations. (NCT01128621)
Timeframe: On Day 1 Immediately pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 13, 24 and 48 hours post-dose.

Interventionnanograms hour per milliliter (ng*hr/mL) (Geometric Mean)
AUC (0-24)AUC (0-last)
Part A7046.2510099.35

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Number of Participants With Abnormal Hematology Values of Potential Clinical Importance (PCI) (Part A)

Blood samples for hematology assessments were collected at screening, fasting (Day -1), at 24hr post- dose (morning of Day 2), and at follow-up. Hematology parameter: Total Neutrophil count was assessed for abnormal value of PCI. The range of PCI value was: <0.83 x lower limit normal (LLN) with unit x10^9 per liter (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 2) in Part A

InterventionParticipants (Count of Participants)
Part A1

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Mean Value of Urine Albumin at Follow up (Part A)

Urine samples were collected at screening, Day -1, at 24hr post- dose (Day 2), and at follow-up. Urine albumin was assessed using quantitative analysis. (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 2) in Part A

Interventionmilligrams per liter (mg/L) (Mean)
Arm A6.0

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Maximum Observed Concentration (Cmax) Following a Single Dose of GSK1292263 (Part A)

Blood samples for the determination of PK were collected on Day 1 Immediately pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 13, 24 and 48 hours post-dose. PK samples for participants were not analyzed. The PK parameters were calculated by standard non-compartmental analysis. Cmax was determined directly from the raw concentration-time data. (NCT01128621)
Timeframe: On Day 1 Immediately pre-dose (time 0) and at 0.5, 1, 2, 3, 4, 6, 8, 13, 24 and 48 hours post-dose.

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
Part A582.619

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Change From Baseline in Mean Fasted Insulin Value (Part A)

Baseline was considered to be Day 1 pre-breakfast. The change from Baseline was calculated by subtracting the Baseline values from the individual post-randomization values. If either the Baseline or post-randomization value was missing, the change from Baseline is set to missing as well. If measurements were taken in triplicate, then the mean of the triplicate measurements was used as the Baseline. (NCT01128621)
Timeframe: Baseline and at pre-breakfast on Day 1 and 24 hours post-dose.

Interventionpicomoles per liter (pmol/L) (Geometric Mean)
Part A3.45

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Change From Baseline in Mean Fasted Glucose Value (Part A)

Baseline was considered to be Day 1 pre-breakfast. The change from Baseline was calculated by subtracting the Baseline values from the individual post-randomization values. If either the Baseline or post-randomization value was missing, the change from Baseline is set to missing as well. If measurements were taken in triplicate, then the mean of the triplicate measurements was used as the Baseline. (NCT01128621)
Timeframe: Baseline and at pre-breakfast on Day 1 and 24 h post-dose.

Interventionmillimoles per liter (mmol/L) (Geometric Mean)
Part A0.17

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Change From Baseline in Weighted Mean for Insulin Value (Part B)

Baseline was considered to be Day -1 pre-breakfast value. The change from Baseline was calculated by subtracting the Baseline values from the individual post-randomization values. If either the Baseline or post-randomization value was missing, the change from Baseline is set to missing as well. If measurements were taken in triplicate, then the mean of the triplicate measurements was used as the Baseline. AUC with respect to that time interval was calculated using the linear trapezoidal rule. The weighted mean was determined by dividing the AUC by the observed length of the collection interval (time of last assessment - time of first assessment in hours). In order for the AUC to be calculated, the first and last time points and at least one additional assessment falling between the two must be non-missing. (NCT01128621)
Timeframe: Baseline and at pre-breakfast on Days -1 and 14, and then at 0.5, 1, 1.5, 2 and 3 hours post dose.

,,,,
Interventionpmol/L (Mean)
Weighted mean (0-12), Day 7Weighted mean (0-12), Day 14Weighted mean (0-24), Day 14
GSK1292263 300 mg-47.290-42.657-35.220
GSK1292263 600 mg-36.334-33.753-31.067
GSK1292263 75 mg-19.2416.6724.626
Placebo6.14621.75122.127
Sitagliptin 50 mg5.97917.32818.848

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Mean Post Meal Glucose Value (Part B)

Blood samples were collected on Days -1 and 14, post-breakfast at 0.5, 1, 1.5, 2 and 3 hours post dose. For lunch (approximately 4 hours post morning dose) samples were collected at the following times after starting each meal: 0.5, 1, 1.5, 2 and 3 hours. For the evening meal (approximately 10 hours post morning dose), samples were taken at 0.5, 1, 1.5, 2 and 3 hours post dinner. (NCT01128621)
Timeframe: At pre-breakfast on Days -1 and 14, and then at 0.5, 1, 1.5, 2 and 3 hours post dose.

,,,,
Interventionmmol/L (Mean)
Day -1, post-breakfast, 0.5 hourDay -1, post-breakfast, 1 hourDay -1, post-breakfast, 1.5 hourDay -1, post-breakfast, 2 hourDay -1, post-breakfast, 3 hourDay -1, post-lunch, 0.5 hourDay -1, post-lunch, 1 hourDay -1, post-lunch, 1.5 hourDay -1, post-lunch, 2 hourDay -1, post-lunch, 3 hourDay -1, post-dinner, 0.5 hourDay -1, post-dinner, 1 hourDay -1, post-dinner, 1.5 hourDay -1, post-dinner, 2 hourDay -1, post-dinner, 3 hourDay 14, post-breakfast, 0.5 hourDay 14, post-breakfast, 1 hourDay 14, post-breakfast, 1.5 hourDay 14, post-breakfast, 2 hourDay 14, post-breakfast, 3 hourDay 14, post-lunch, 0.5 hourDay 14, post-lunch, 1 hourDay 14, post-lunch, 1.5 hourDay 14, post-lunch, 2 hourDay 14, post-lunch, 3 hourDay 14, post-dinner, 0.5 hourDay 14, post-dinner, 1 hourDay 14, post-dinner, 1.5 hourDay 14, post-dinner, 2 hourDay 14, post-dinner, 3 hour
GSK1292263 300 mg14.6814.4812.9411.508.688.5610.7111.6411.7511.258.7811.0010.9910.8110.3414.9614.2312.9610.938.2010.0711.9612.3312.0910.579.3712.2113.0112.0710.69
GSK1292263 600 mg13.0413.4312.0210.678.468.5810.1210.4510.1110.378.9210.7710.9410.9810.4813.8314.3213.0711.118.738.7010.4211.1210.8710.4410.4112.5613.0312.6011.75
GSK1292263 75 mg13.5113.4212.1210.558.488.9011.1911.1710.8210.059.1911.2710.9710.7610.4113.1313.3211.589.986.968.7310.5910.8010.519.717.9911.2011.8111.279.78
Placebo13.7513.6212.5610.717.787.4610.3111.0711.3111.059.2811.1511.4511.6711.5814.1614.0212.6911.157.567.439.6110.3810.8310.518.1711.0711.6511.4210.43
Sitagliptin 50 mg13.6013.1211.399.757.737.9310.3610.6910.729.928.3910.2710.5210.189.6612.2612.0310.559.106.697.778.388.838.848.907.299.4310.4110.078.80

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Cmax Following Repeat Dose of GSK1292263 (Part B)

Serial blood samples for the determination of the PK of GSK1292263 were collected on Days 1, 7 and 14. Blood samples for PK were collected on Days 1 and 14, at immediately pre-morning dose, 1, 2, 4, 6, 8, 10, 11, 12, 14, 16, 18, 24 and 48 hours post-morning dose. On Day 7, blood samples for PK were collected at pre-dose (post-breakfast), 1, 2, 4 (pre-lunch), 6 and 10 (immediately post-dinner, pre-dose for BID regimen). When planned PK sampling resulted in multiple samples at the same time point, only one sample was collected. The PK parameters were calculated by standard non-compartmental analysis. Cmax was determined directly from the raw concentration-time data. (NCT01128621)
Timeframe: On Days 1 and 14, at immediately pre-morning dose, 1, 2, 4, 6, 8, 10, 11, 12, 14, 16, 18, 24 and 48 hours post-morning dose. On Day 7, at pre-dose (post-breakfast), 1, 2, 4 (pre-lunch), 6 and 10 (immediately post-dinner, pre-dose for BID regimen).

,,
Interventionng/mL (Geometric Mean)
Day 1Day 7Day 14
GSK1292263 300 mg686.845872.843902.325
GSK1292263 600 mg610.586738.918664.505
GSK1292263 75 mg278.451416.441457.716

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Number of Participants With Abnormal Clinical Chemistry Values of PCI (Part A)

"Blood samples for chemistry assessments were collected at screening, fasting (Day -1), at 24hr post- dose (morning of Day 2), and at follow-up.~Clinical chemistry parameter: Glucose (unit: millimoles per liter [mmol/L]) was assessed for abnormal high value of PCI. The normal range was 3.6 to 5.5 mmol/L" (NCT01128621)
Timeframe: Up to 10 days after discharge (Day 2) in Part A

InterventionParticipants (Count of Participants)
Part A1

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Mean Post Meal Insulin Value (Part B)

Blood samples were collected on Days -1 and 14, post-breakfast at 0.5, 1, 1.5, 2 and 3 hours post dose. For lunch (approximately 4 hours post morning dose) samples were collected at the following times after starting each meal: 0.5, 1, 1.5, 2 and 3 hours. For the evening meal (approximately 10 hours post morning dose), samples were taken at 0.5, 1, 1.5, 2 and 3 hours post dinner. (NCT01128621)
Timeframe: At pre-breakfast on Days -1 and 14, and then at 0.5, 1, 1.5, 2 and 3 hours post dose.

,,,,
Interventionpmol/L (Mean)
Day -1, post-breakfast, 0.5 hourDay -1, post-breakfast, 1 hourDay -1, post-breakfast, 1.5 hourDay -1, post-breakfast, 2 hourDay -1, post-breakfast, 3 hourDay -1, post-lunch, 0.5 hourDay -1, post-lunch, 1 hourDay -1, post-lunch, 1.5 hourDay -1, post-lunch, 2 hourDay -1, post-lunch, 3 hourDay -1, post-dinner, 0.5 hourDay -1, post-dinner, 1 hourDay -1, post-dinner, 1.5 hourDay -1, post-dinner, 2 hourDay -1, post-dinner, 3 hourDay 14, post-breakfast, 0.5 hourDay 14, post-breakfast, 1 hourDay 14, post-breakfast, 1.5 hourDay 14, post-breakfast, 2 hourDay 14, post-breakfast, 3 hourDay 14, post-lunch, 0.5 hourDay 14, post-lunch, 1 hourDay 14, post-lunch, 1.5 hourDay 14, post-lunch, 2 hourDay 14, post-lunch, 3 hourDay 14, post-dinner, 0.5 hourDay 14, post-dinner, 1 hourDay 14, post-dinner, 1.5 hourDay 14, post-dinner, 2 hourDay 14, post-dinner, 3 hour
GSK1292263 300 mg270.35296.05318.38258.69162.58147.60186.02212.29218.67207.00150.10226.22206.80206.16172.36241.13297.58272.63229.72122.31126.26172.43179.44177.88137.6775.85141.59163.94168.71134.98
GSK1292263 600 mg264.15338.58351.10304.66180.43187.22246.08289.19295.21270.43207.99274.72275.17266.34225.12259.89348.37409.93333.39188.31169.17190.65223.72227.81195.64137.16191.90215.57223.18191.01
GSK1292263 75 mg185.34258.37246.76221.27114.67115.21193.65208.37196.74171.15131.50205.59183.16205.06164.28240.43280.93299.22234.65110.81129.25169.74194.93214.66181.4398.57178.38210.90220.97167.22
Placebo201.81222.44251.01233.85131.95135.17193.80188.57235.41191.74132.04199.54195.55209.64176.48258.61304.23297.57283.85161.67153.65201.54229.56237.34219.3199.41204.76204.67237.14200.85
Sitagliptin 50 mg219.24251.79237.46196.53106.98109.63180.49173.21202.47167.37104.16149.94171.08171.94155.62268.74354.57300.33246.53117.21155.68164.53184.69188.61172.2292.78156.48179.94187.66175.02

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Proportion of Participants With at Least One Symptomatic or Asymptomatic Hypoglycemic Event

Hypoglycemic event was based on the participant's self-report and/or finger-stick blood glucose level. Symptomatic hypoglycemic symptoms included faintness, headache, confusion, anxiety, sweating, tremor, palpitation, nausea, pallor, dizziness, hunger, and sudden behavioral change. (NCT01131182)
Timeframe: 30 days: first day of Ramadan (August 11) to last day of Ramadan (September 10)

InterventionProportion of participants (Number)
Sitagliptin0.08
Sulfonylurea0.18

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Proportion of Participants With at Least One Symptomatic Hypoglycemic Event

Symptomatic hypoglycemic event was determined based on the participant's self-reported symptoms including faintness, headache, confusion, anxiety, sweating, tremor, palpitation, nausea, pallor, dizziness, hunger, and sudden behavioral change. (NCT01131182)
Timeframe: 30 days: first day of Ramadan (August 11) to last day of Ramadan (September 10)

Interventionproportion of participants (Number)
Sitagliptin0.07
Sulfonylurea0.13

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Percent Change in High-density Lipoprotein Cholesterol (HDL-C) From Baseline to Week 52

The table below shows the mean percent change in HDL-C from Baseline to Week 52 for each treatment group. The statistical analysis shows the treatment difference (ie, between canagliflozin and sitagliptin) in the LS mean change. (NCT01137812)
Timeframe: Day 1 (Baseline) and Week 52

InterventionPercent change (Least Squares Mean)
Canagliflozin 300 mg7.6
Sitagliptin 100 mg0.6

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Percentage of Patients With HbA1c <7% at Week 52

The table below shows the percentage of patients with HbA1c <7% at Week 52 in each treatment group. The statistical analysis shows the treatment difference (ie, between canagliflozin and sitagliptin) in the percentage. (NCT01137812)
Timeframe: Week 52

InterventionPercentage of patients (Number)
Canagliflozin 300 mg47.6
Sitagliptin 100 mg35.3

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Percent Change in Triglycerides From Baseline to Week 52

The table below shows the mean percent change in triglycerides from Baseline to Week 52 for each treatment group. The statistical analysis shows the treatment difference (ie, between canagliflozin and sitagliptin) in the LS mean change. (NCT01137812)
Timeframe: Day 1 (Baseline) and Week 52

InterventionPercent change (Least Squares Mean)
Canagliflozin 300 mg9.6
Sitagliptin 100 mg11.9

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Percent Change in Body Weight From Baseline to Week 52

The table below shows the least-squares (LS) mean percent change in body weight from Baseline to Week 52 for each treatment group. The statistical analysis shows the treatment difference (ie, between canagliflozin and sitagliptin) in the LS mean percent change. (NCT01137812)
Timeframe: Day 1 (Baseline) and Week 52

InterventionPercent change (Least Squares Mean)
Canagliflozin 300 mg-2.5
Sitagliptin 100 mg0.3

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Change in Fasting Plasma Glucose (FPG) From Baseline to Week 52

The table below shows the least-squares (LS) mean change in FPG from Baseline to Week 52 for each treatment group. The statistical analysis shows the treatment difference (ie, between canagliflozin and sitagliptin) in the LS mean change. (NCT01137812)
Timeframe: Day 1 (Baseline) and Week 52

Interventionmg/dL (Least Squares Mean)
Canagliflozin 300 mg-29.9
Sitagliptin 100 mg-5.85

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Change in HbA1c From Baseline to Week 52

The table below shows the least-squares (LS) mean change in HbA1c from Baseline to Week 52 for each treatment group. The statistical analysis shows the treatment difference (ie, between canagliflozin and sitagliptin) in the LS mean change. (NCT01137812)
Timeframe: Day 1 (Baseline) and Week 52

InterventionPercent (Least Squares Mean)
Canagliflozin 300 mg-1.03
Sitagliptin 100 mg-0.66

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Change in Systolic Blood Pressure (SBP) From Baseline to Week 52

The table below shows the least-squares (LS) mean change in SBP from Baseline to Week 52 for each treatment group. The statistical analysis shows the treatment difference (ie, between canagliflozin and sitagliptin) in the LS mean change. (NCT01137812)
Timeframe: Day 1 (Baseline) and Week 52

InterventionmmHg (Least Squares Mean)
Canagliflozin 300 mg-5.06
Sitagliptin 100 mg0.85

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2 Hour C-peptide AUC in Response to MMTT

Blood samples for C-peptide were collected at baseline (pre-meal) and 15, 30, 60, 90, and 120 minutes post-meal. (NCT01155284)
Timeframe: Month 6

Interventionpmol/L (Median)
Sitagliptin and Lansoprazole485
Placebo675

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2 Hour C-peptide AUC in Response to MMTT

Blood samples for C-peptide were collected at baseline (pre-meal) and 15, 30, 60, 90 and 120 minutes post-meal. (NCT01155284)
Timeframe: Month 12

Interventionpmol/L (Median)
Sitagliptin and Lansoprazole358
Placebo495

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Number of Participants Who Experienced at Least One Adverse Event

(NCT01177384)
Timeframe: Up to Week 24 + 14 Day Post-Study Follow-up

InterventionParticipants (Number)
Sitagliptin62
Placebo58

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Number of Participants Who Discontinued Study Drug Due to an Adverse Event

(NCT01177384)
Timeframe: Up to 24 Weeks

InterventionParticipants (Number)
Sitagliptin5
Placebo2

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Change From Baseline in Hemoglobin A1c (A1C) at Week 24

A1C is measured as a percent. Thus, this change from baseline reflects the Week 24 A1C percent minus the Week 0 A1C percent. Efficacy analyses treated data as missing after the initiation of rescue therapy. (NCT01177384)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Sitagliptin-0.76
Placebo-0.14

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24

Change from baseline at Week 24 is defined as Week 24 FPG minus Week 0 FPG. Efficacy analyses treated data as missing after the initiation of rescue therapy. (NCT01177384)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-17.9
Placebo-3.5

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Confirmed Hypoglycaemic Adverse Events

"Confirmed hypoglycaemic events refer to all hypoglycaemic events, that had a glucose value <= 70 ml/dL or where assistance was required.~Symptomatic hypoglycaemic events were to be reported as adverse events. Patients can be counted in more than one category." (NCT01177813)
Timeframe: From first drug intake until 7 days after last medication intake, up to 219 days

,,,,
Interventionpercentage of participants (Number)
Symptomatic hypoglycaemic adverse eventsAsymptomatic hypoglycaemic adverse events
Empagliflozin 25 mg0.40
Empagliflozin 25 mg OL00
Empagliflozin10 mg0.40
Placebo0.40
Sitagliptin 100 mg0.40

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Change From Baseline to Week 24 in Body Weight

"The term baseline refers to the last observation before the start of randomised trial treatment (or of open-label treatment for the open-label arm).~In this endpoint, the measured values show unadjusted values, whereas the statistical analyses show adjusted values. Statistics for open-label group are descriptive." (NCT01177813)
Timeframe: Baseline and day 169

Interventionkg (Mean)
Placebo-0.33
Empagliflozin10 mg-2.26
Empagliflozin 25 mg-2.48
Sitagliptin 100 mg0.17
Empagliflozin 25 mg OL-1.93

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Change From Baseline to Week 24 in Systolic and Diastolic Blood Pressure (SBP and DBP)

"The term baseline refers to the last observation before the start of randomised trial treatment (or of open-label treatment for the open-label arm).~In this endpoint, the measured values show unadjusted values, whereas the statistical analyses show adjusted values. Statistics for open-label group are descriptive.~For blood pressure, data following changes in antihypertensive therapy is censored, in the same way that data following initiation of rescue medication is censored." (NCT01177813)
Timeframe: Baseline and week 24

,,,,
InterventionmmHg (Mean)
Systolic blood pressureDiastolic blood pressure
Empagliflozin 25 mg-3.2-1.7
Empagliflozin 25 mg OL-3.8-1.5
Empagliflozin10 mg-3.5-1.1
Placebo0.0-0.4
Sitagliptin 100 mg0.20.4

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Change From Baseline in Glycosylated Haemoglobin (HbA1c) After 24 Weeks

"The term baseline refers to the last observation before the start of randomised trial treatment (or of open-label treatment for the open-label arm).~In this endpoint, the measured values show unadjusted values, whereas the statistical analyses show adjusted values. Statistics for open-label group are descriptive." (NCT01177813)
Timeframe: Baseline and day 169

Interventionpercent of HbA1c (Mean)
Placebo0.06
Empagliflozin10 mg-0.66
Empagliflozin 25 mg-0.77
Sitagliptin 100 mg-0.65
Empagliflozin 25 mg OL-3.10

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Number of Participants With Hypoglycaemia

(NCT01183104)
Timeframe: From baseline to 52 W

InterventionParticipants (Count of Participants)
Sitagliptin7
Glimepiride23

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Change From Baseline in Body Weight at 52 W

(NCT01183104)
Timeframe: Baseline and 52 W

Interventionkg (Mean)
Sitagliptin-0.367
Glimepiride0.309

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Change From Baseline in HbA1c at 52 W

(NCT01183104)
Timeframe: Baseline and 52 W

Interventionpercent (Least Squares Mean)
Sitagliptin-0.66
Glimepiride-0.77

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Change From Baseline in HOMA-β at 52 W

β cell function is measured by the Homeostatic Model Assessment(HOMA-β). HOMA β = [20 x fasting insulin (μU/mL)] / [fasting plasma glucose (mmol/L) - 3.5] (NCT01183104)
Timeframe: Baseline and 52 W

Interventionpercent (Mean)
Sitagliptin10.2
Glimepiride23.7

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Change From Baseline in Insulin/Proinsulin Ratio at 52 W

(NCT01183104)
Timeframe: Baseline and 52 W

Interventionratio (Mean)
Sitagliptin-0.049
Glimepiride-0.002

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The Number of Participants Achieving HbA1c < 6.9 %

(NCT01183104)
Timeframe: 52 W

InterventionParticipants (Count of Participants)
Sitagliptin89
Glimepiride86

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Insulin Independence

percentage of patients insulin independent (NCT01186562)
Timeframe: 18 months

Interventionpercentage of participants (Number)
Sitagliptin36
Placebo44

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Insulin Independence

percentage of patients insulin independent (NCT01186562)
Timeframe: 12 months

Interventionpercentage of participants (Number)
Sitagliptin42
Placebo45

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AUC C-peptide

AUC C-peptide (ng/dL*min) from mixed meal tolerance test (measured times 0 to 2 hours after Boost HP) (NCT01186562)
Timeframe: 18 months

Interventionmin*ng/dL (Mean)
Sitagliptin274
Placebo235

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Area Under the Curve (AUC) C-peptide (ng/dL*Min)

AUC C-peptide obtained from a mixed meal test (measured time 0 to 2 hours after Boost HP) (NCT01186562)
Timeframe: 12 months

Interventionng*min/dL (Mean)
Sitagliptin273
Placebo273

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Acute C-peptide Response (ACR) to Glucose

Derived from intravenous gluocose tolerance testing (0 to 10 minute measures after dextrose bolus) (NCT01186562)
Timeframe: 12 months

Interventionmin*ng/dL (Mean)
Sitagliptin9.9
Placebo7.2

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Acute C-peptide Response (ACR) to Glucose

Derived from intravenous glucose tolerance test (0 to 10 minute measures after IV dextrose bolus) (NCT01186562)
Timeframe: 18 months

Interventionmin*ng/dL (Mean)
Sitagliptin6.9
Placebo6.0

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Number of Participants Discontinuing Study Treatment Due to An AE

"An AE was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the~study treatment, whether or not considered related to the use of the treatment administered." (NCT01189890)
Timeframe: Up to Week 30

InterventionParticipants (Number)
Sitagliptin3
Glimepiride4

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Percentage of Participants With HbA1c <7.0% at Week 30

Participant whole blood samples were collected at Week 30 to determine the number of participants achieving HbA1c <7.0% at Week 30. HbA1c is a measure of the percentage of glycated hemoglobin in the blood and provides an indication of participant blood glucose control in the 2 to 3 months prior to the evaluation. (NCT01189890)
Timeframe: Week 30

InterventionPercentage of Participants (Number)
Sitagliptin33.5
Glimepiride46.6

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Percentage of Participants With HbA1c <6.5% at Week 30

Participant whole blood samples were collected at Week 30 to determine the number of participants achieving HbA1c <6.5% at Week 30. Hemoglobin A1c is a measure of the percentage of glycated hemoglobin in the blood and provides an indication of participant blood glucose control in the 2 to 3 months prior to the evaluation. (NCT01189890)
Timeframe: Week 30

InterventionPercentage of Participants (Number)
Sitagliptin9.1
Glimepiride20.9

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Number of Participants With an Adverse Event of Symptomatic Hypoglycemia Up to Week 30

Symptomatic hypoglycemia was defined as an episode with clinical symptoms attributed to hypoglycemia, without regard to glucose level. Participants were instructed to complete the Hypoglycemia Assessment Log (HAL) for any symptomatic episodes he or she believed represent hypoglycemia. If a fingerstick glucose was obtained before or shortly (i.e., within a few minutes) after treating, the value was recorded in the HAL. In addition, participants were instructed to record in the HAL any fingerstick glucose values ≤70 mg/dL (≤3.9 mmol/L) regardless of the presence of clinical symptoms. (NCT01189890)
Timeframe: Up to Week 30

InterventionParticipants (Number)
Sitagliptin2
Glimepiride11

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Number of Participants Experiencing An Adverse Event (AE)

"An AE was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the~study treatment, whether or not considered related to the use of the treatment administered." (NCT01189890)
Timeframe: Up to Week 30

InterventionParticipants (Number)
Sitagliptin118
Glimepiride115

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Least Squares (LS) Mean Change From Baseline in Hemoglobin A1c (HbA1c) at Week 30

Participant whole blood samples were collected at baseline and Week 30 to determine the LS mean HbA1c change from baseline. HbA1c is a measure of the percentage of glycated hemoglobin in the blood and provides an indication of participant blood glucose control in the 2 to 3 months prior to the evaluation. (NCT01189890)
Timeframe: Baseline and Week 30

InterventionPercentage of HbA1c (Least Squares Mean)
Sitagliptin-0.32
Glimepiride-0.51

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LS Mean Change From Baseline in Fasting Plasma Glucose (FPG) at Week 30

Plasma samples were collected from participants after an overnight fast at baseline and Week 30 to determine the mean change from baseline in participant FPG. (NCT01189890)
Timeframe: Baseline and Week 30

Interventionmg/dL (Least Squares Mean)
Sitagliptin-14.5
Glimepiride-21.2

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LS Mean Change From Baseline in Participant Body Weight at Week 30

Participants were only permitted to wear a drape gown and undergarments (no street clothes, no shoes or socks) for this evaluation. Body weight was measured after voiding (to the nearest 0.1 kg) and measurements were collected until 2 consecutive measurements did not differ by more than 0.2 kg from each other. Body weight measurements were evaluated using a standardized, calibrated digital scale and was reported in kilograms (kg) at baseline and Week 30. (NCT01189890)
Timeframe: Baseline and Week 30

Interventionkg (Least Squares Mean)
Sitagliptin0.4
Glimepiride1.1

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Percentages of Patients With Nasopharyngitis

Proportion of Nasopharyngitis after treatment (NCT01195090)
Timeframe: 24 weeks

Interventionpercentage (Number)
Sitagliptin20.0
Pioglitazone18.6

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Percentages of Patients With Severe Hypoglycemia

Proportion of severe hypoglycemia after treatment (NCT01195090)
Timeframe: 24 weeks

Interventionpercentage (Number)
Sitagliptin0
Pioglitazone0

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The Percentages of Patient Achieving an A1C <7%

The percentages of patient achieving an A1C <7% at endpoint (NCT01195090)
Timeframe: 24 weeks

Interventionpercentage (Number)
Sitagliptin28.3
Pioglitazone28.8

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Percentages of Patients With Total Adverse Events (AE)

percentages of total adverse events (NCT01195090)
Timeframe: 24 weeks

Interventionpercentage (Number)
Sitagliptin43.1
Pioglitazone51.7

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Baseline A1C

baseline A1C (NCT01195090)
Timeframe: Baseline

Interventionpercentage of Hb (Mean)
Sitagliptin8.27
Pioglitazone8.54

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Baseline Alanine-aminotransferase (ALT)

Baseline alanine-aminotransferase (NCT01195090)
Timeframe: Baseline

InterventionIU/L (Mean)
Sitagliptin34.2
Pioglitazone28.5

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Baseline Body Weight

Baseline body weight (NCT01195090)
Timeframe: Baseline

Interventionkg (Mean)
Sitagliptin69.4
Pioglitazone65.4

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Baseline Fasting Plasma Glucose

Baseline fasting plasma glucose (NCT01195090)
Timeframe: baseline

Interventionmg/dl (Mean)
Sitagliptin177
Pioglitazone182

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Baseline High Sensitive C-reactive Protein

Baseline high sensitive C-reactive Protein (NCT01195090)
Timeframe: baseline

Interventionmg/dl (Mean)
Sitagliptin0.38
Pioglitazone0.42

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Baseline High-density Lipoprotein Cholesterol (HDL-C)

Baseline HDL-C (NCT01195090)
Timeframe: Baseline

Interventionmg/dl (Mean)
Sitagliptin42
Pioglitazone43

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Baseline Homoeostasis Model Assessment of Insulin Resistance (HOMA-IR)

Baseline HOMA-IR (NCT01195090)
Timeframe: Baseline HOMA-IR

InterventionHOMA-IR score (Mean)
Sitagliptin5.6
Pioglitazone4.8

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Baseline Low-density Lipoprotein Cholesterol (LDL-C)

Baseline LDL-C (NCT01195090)
Timeframe: Baseline

Interventionmg/dl (Mean)
Sitagliptin102
Pioglitazone111

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Baseline Total Cholesterol

Baseline Total cholesterol (NCT01195090)
Timeframe: Baseline

Interventionmg/dl (Mean)
Sitagliptin174
Pioglitazone194

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Baseline Triglyceride (TG)

Baseline TG (NCT01195090)
Timeframe: Baseline

Interventionmg/dl (Mean)
Sitagliptin137
Pioglitazone164

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Body Weight Change

body weight change from baseline to 24 weeks (NCT01195090)
Timeframe: 24 weeks

Interventionkg (Least Squares Mean)
Sitagliptin-0.26
Pioglitazone1.34

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Change in Fasting High-density Lipoprotein Cholesterol(HDL-C)

HDL-C change from baseline to 24 weeks (NCT01195090)
Timeframe: 24 weeks

Interventionmg/dl (Least Squares Mean)
Sitagliptin1.3
Pioglitazone6.3

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Change in Fasting Low-density Lipoprotein Cholesterol (LDL-C)

LDL-C change from baseline to 24 weeks (NCT01195090)
Timeframe: 24 weeks

Interventionmg/dl (Least Squares Mean)
Sitagliptin-1.2
Pioglitazone6.6

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Change in Fasting Plasma Alanine-aminotransferase (ALT)

ALT change from baseline to 24 weeks (NCT01195090)
Timeframe: 24 weeks

InterventionIU/L (Least Squares Mean)
Sitagliptin-0.0
Pioglitazone-4.5

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Change in Fasting Total-cholesterol

Total-cholesterol change from baseline to 24 weeks (NCT01195090)
Timeframe: 24 weeks

Interventionmg/dl (Least Squares Mean)
Sitagliptin0.6
Pioglitazone9.9

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Change in Fasting Triglycerides(TG)

TG change from baseline to 24 weeks (NCT01195090)
Timeframe: 24 weeks

Interventionmg/dl (Least Squares Mean)
Sitagliptin6.3
Pioglitazone-23.9

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Changes in Fasting Plasma Glucose

fasting serum sugar change from baseline to 24 weeks (NCT01195090)
Timeframe: 24 weeks

Interventionmg/dl (Least Squares Mean)
Sitagliptin-23
Pioglitazone-36

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Changes in High Sensitive C-reactive Protein

fasting high sensitive serum C-reactive protein change from baseline to 24 weeks (NCT01195090)
Timeframe: 24 weeks

Interventionmg/dl (Least Squares Mean)
Sitagliptin-0.07
Pioglitazone-0.19

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Changes in Homoeostasis Model Assessment of Insulin Resistance (HOMA-IR)

HOMA-IR change from baseline to 24 weeks (NCT01195090)
Timeframe: 24 weeks

InterventionHOMA-IR score (Least Squares Mean)
Sitagliptin-0.00
Pioglitazone-1.56

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Mean Change in Glycosylated Hemoglobin (A1C)

A1C change from baseline to 24 weeks (NCT01195090)
Timeframe: 24 weeks

Interventionpercentage of Hb (Least Squares Mean)
Sitagliptin-0.71
Pioglitazone-0.94

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Percentages of Patients With Edema

proportion of edema after treatment (NCT01195090)
Timeframe: 24 weeks

Interventionpercentage (Number)
Sitagliptin0
Pioglitazone27.1

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Percentages of Patients With Gastrointestinal Adverse Events

Proportion of Gastrointestinal adverse events after treatment (NCT01195090)
Timeframe: 24 weeks

Interventionpercentge (Number)
Sitagliptin20.0
Pioglitazone6.8

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Percentages of Patients With Mild to Moderate Hypoglycemia

Incidence of mild to moderate hypoglycemia after treatment (NCT01195090)
Timeframe: 24 weeks

Interventionpercentage (Number)
Sitagliptin10
Pioglitazone8.5

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Symptomatic Hormone Responses to Acute Hypoglycaemia.

The symptomatic responses to hypoglycaemia were assessed using a standard validated symptom questionnaire adapted for experimental hypoglycaemia (McCrimmon et al (2003) Diabet.Med. 20: 507-509). A 7-point Likert scale (1=symptom absent; 7=symptom experienced with great intensity) was used to score presence and intensity of autonomic and neuroglycopenic symptoms of hypoglycaemia. Symptom scores were obtained during the initialisation phase, at occurrence of autonomic reaction and again 30 minutes later. For analyses the scale was considered as a continuous variable. (NCT01272583)
Timeframe: Change from baseline symptomatic response at hypoglycaemia and 30 minutes after hypoglycaemia

,,
Interventionunits on a scale (Median)
Autonomic symptoms scoreNeurologic symptoms score
Baseline1.72.1
Placebo1.52.1
Sitagliptin Treatment1.32.4

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Intact and Total Glucagon Like Peptide-1 (GLP-1), Intact and Total Gastric Inhibitory Peptide (GIP) Response to Acute Hypoglycaemia

Area under the curve (AUC) from onset of the autonomic response to hypoglycaemia to 40 minutes after onset of the autonomic response. AUC values were calculated by the trapezoid method. (NCT01272583)
Timeframe: 0, 10, 20, 40 minutes

,,
Interventionpmol*minutes/L (Median)
GLP-1 intactGLP-1 totalGIP intactGIP total
Baseline2.000562.2455.0302.5
Placebo4.500552.5452.5342.5
Sitagliptin Treatment43.50555.0490.0285.0

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Norepinephrine Response to Acute Hypoglycaemia

Area under the curve (AUC) from onset of the autonomic response to hypoglycaemia to 40 minutes after onset of the autonomic response. AUC values were calculated by the trapezoid method. (NCT01272583)
Timeframe: 0, 10, 20, 40 minutes

Interventionnmol*minutes/L (Median)
Baseline70.0
Sitagliptin Treatment62.5
Placebo62.3

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Glucagon Response to Acute Hypoglycaemia

Change in glucagon concentration from the initialisation phase to 40 minutes after occurrence of the autonomic reaction to hypoglycaemia (NCT01272583)
Timeframe: Change from initialisation phase to 40 minutes after onset of hypoglycaemia

Interventionpmol/L (Median)
Baseline1.33
Sitagliptin Treatment1.0
Placebo1.33

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Glucagon Response to Acute Hypoglycaemia

Area under the curve (AUC) from onset of the autonomic response to hypoglycaemia to 40 minutes after onset of the autonomic response. AUC values were calculated by the trapezoid method. (NCT01272583)
Timeframe: 0, 10, 20 and 40 minutes

Interventionpmol*minutes/L (Median)
Baseline120
Sitagliptin Treatment125
Placebo120

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Growth Hormone Response to Acute Hypoglycaemia

Area under the curve (AUC) from onset of the autonomic response to hypoglycaemia to 40 minutes after onset of the autonomic response. AUC values were calculated by the trapezoid method. (NCT01272583)
Timeframe: 0, 10, 20, 40 minutes

InterventionmU*minutes/L (Median)
Baseline1299
Sitagliptin Treatment261.5
Placebo1406

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Epinephrine Response to Acute Hypoglycaemia

Area under the curve (AUC) from onset of the autonomic response to hypoglycaemia to 40 minutes after onset of the autonomic response. AUC values were calculated by the trapezoid method. (NCT01272583)
Timeframe: 0, 10, 20, 40 minutes

Interventionnmol*minutes/L (Median)
Baseline36.1
Sitagliptin Treatment32.6
Placebo58.7

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Cortisol Response to Acute Hypoglycaemia

Area under the curve (AUC) from onset of the autonomic response to hypoglycaemia to 40 minutes after onset of the autonomic response. AUC values were calculated by the trapezoid method. (NCT01272583)
Timeframe: 0, 10, 20, 40 minutes

InterventionmU*minutes/L (Median)
Baseline14480
Sitagliptin Treatment13190
Placebo14800

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Body Weight (kg) Change From Baseline After 76 Weeks of Treatment

Body Weight (kg) - Change From Baseline After 76 Weeks of Treatment (NCT01289990)
Timeframe: Baseline and 76 weeks

Interventionkg (Least Squares Mean)
BI 10773 Low (Drug Naive)-2.24
BI 10773 High (Drug Naive)-2.45
Placebo (Drug Naive)-0.43
Sitagliptin 100mg (Drug Naive)0.10
BI 10773 Low (Pioglitazone)-1.47
BI 10773 High (Pioglitazone)-1.21
Placebo (Pioglitazone)0.50
BI 10773 Low (Metformin)-2.39
BI 10773 High (Metformin)-2.65
Placebo (Metformin)-0.46
BI 10773 Low (Metformin+Sulfonylurea)-2.44
BI 10773 High (Metformin+Sulfonylurea)-2.28
Placebo (Metformin+Sulfonylurea)-0.63

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Changes From Baseline in Glycosylated Haemoglobin (HbA1c) (%) After 52 Weeks of Treatment

Change from baseline in HbA1c after 52 weeks (NCT01289990)
Timeframe: Baseline and 52 weeks

Intervention% of HbA1c (Least Squares Mean)
BI 10773 Low (Drug Naive)-0.70
BI 10773 High (Drug Naive)-0.82
Placebo (Drug Naive)0.09
Sitagliptin 100mg (Drug Naive)-0.58
BI 10773 Low (Pioglitazone)-0.63
BI 10773 High (Pioglitazone)-0.71
Placebo (Pioglitazone)-0.03
BI 10773 Low (Metformin)-0.69
BI 10773 High (Metformin)-0.76
Placebo (Metformin)-0.07
BI 10773 Low (Metformin+Sulfonylurea)-0.78
BI 10773 High (Metformin+Sulfonylurea)-0.74
Placebo (Metformin+Sulfonylurea)-0.04

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Changes From Baseline in HbA1c (%) After 76 Weeks of Treatment

Change from baseline in HbA1c after 76 weeks (NCT01289990)
Timeframe: Baseline and 76 weeks

Intervention% of HbA1c (Least Squares Mean)
BI 10773 Low (Drug Naive)-0.65
BI 10773 High (Drug Naive)-0.76
Placebo (Drug Naive)0.13
Sitagliptin 100mg (Drug Naive)-0.53
BI 10773 Low (Pioglitazone)-0.61
BI 10773 High (Pioglitazone)-0.70
Placebo (Pioglitazone)-0.01
BI 10773 Low (Metformin)-0.62
BI 10773 High (Metformin)-0.74
Placebo (Metformin)-0.01
BI 10773 Low (Metformin+Sulfonylurea)-0.74
BI 10773 High (Metformin+Sulfonylurea)-0.72
Placebo (Metformin+Sulfonylurea)-0.03

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Body Weight (kg) Change From Baseline After 52 Weeks of Treatment

Body Weight (kg) - Change From Baseline After 52 Weeks of Treatment (NCT01289990)
Timeframe: Baseline and 52 weeks

Interventionkg (Least Squares Mean)
BI 10773 Low (Drug Naive)-2.70
BI 10773 High (Drug Naive)-2.61
Placebo (Drug Naive)-0.48
Sitagliptin 100mg (Drug Naive)0.14
BI 10773 Low (Pioglitazone)-1.50
BI 10773 High (Pioglitazone)-1.40
Placebo (Pioglitazone)0.59
BI 10773 Low (Metformin)-2.27
BI 10773 High (Metformin)-2.84
Placebo (Metformin)-0.54
BI 10773 Low (Metformin+Sulfonylurea)-2.28
BI 10773 High (Metformin+Sulfonylurea)-2.32
Placebo (Metformin+Sulfonylurea)-0.31

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Diastolic Blood Pressure: Change From Baseline After 52 Weeks of Treatment

Diastolic blood pressure - change from baseline after 52 weeks of treatment (NCT01289990)
Timeframe: Baseline and 52 weeks

InterventionmmHg (Least Squares Mean)
BI 10773 Low (Drug Naive)-1.3
BI 10773 High (Drug Naive)-1.9
Placebo (Drug Naive)-0.2
Sitagliptin 100mg (Drug Naive)-0.3
BI 10773 Low (Pioglitazone)-1.6
BI 10773 High (Pioglitazone)-2.2
Placebo (Pioglitazone)0.4
BI 10773 Low (Metformin)-2.2
BI 10773 High (Metformin)-2.1
Placebo (Metformin)-0.4
BI 10773 Low (Metformin+Sulfonylurea)-1.7
BI 10773 High (Metformin+Sulfonylurea)-1.6
Placebo (Metformin+Sulfonylurea)-1.0

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HbA1c (%) Changes From Baseline After 76 Weeks of Treatment

Change from baseline in HbA1c (%) after 76 weeks using MMRM approach (NCT01289990)
Timeframe: Baseline and 76 weeks

Intervention% of HbA1c (Least Squares Mean)
BI 10773 Low (Drug Naive)-0.70
BI 10773 High (Drug Naive)-0.77
Placebo (Drug Naive)0.13
Sitagliptin 100mg (Drug Naive)-0.48
BI 10773 Low (Pioglitazone)-0.67
BI 10773 High (Pioglitazone)-0.77
Placebo (Pioglitazone)-0.05
BI 10773 Low (Metformin)-0.60
BI 10773 High (Metformin)-0.76
Placebo (Metformin)0.07
BI 10773 Low (Metformin+Sulfonylurea)-0.75
BI 10773 High (Metformin+Sulfonylurea)-0.75
Placebo (Metformin+Sulfonylurea)0.06

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Waist Circumference (cm) Change From Baseline After 76 Weeks of Treatment

Waist circumference (cm) - change from baseline after 76 weeks of treatment (NCT01289990)
Timeframe: Baseline and 76 weeks

Interventioncm (Least Squares Mean)
BI 10773 Low (Drug Naive)-1.5
BI 10773 High (Drug Naive)-1.6
Placebo (Drug Naive)0.1
Sitagliptin 100mg (Drug Naive)0.5
BI 10773 Low (Pioglitazone)-1.4
BI 10773 High (Pioglitazone)-0.9
Placebo (Pioglitazone)0.0
BI 10773 Low (Metformin)-1.8
BI 10773 High (Metformin)-1.3
Placebo (Metformin)-0.2
BI 10773 Low (Metformin+Sulfonylurea)-1.6
BI 10773 High (Metformin+Sulfonylurea)-1.4
Placebo (Metformin+Sulfonylurea)-0.3

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Waist Circumference (cm) Change From Baseline After 52 Weeks of Treatment

Waist circumference (cm) - change from baseline after 52 weeks of treatment (NCT01289990)
Timeframe: Baseline and 52 weeks

Interventioncm (Least Squares Mean)
BI 10773 Low (Drug Naive)-2.0
BI 10773 High (Drug Naive)-1.7
Placebo (Drug Naive)0.1
Sitagliptin 100mg (Drug Naive)0.4
BI 10773 Low (Pioglitazone)-1.5
BI 10773 High (Pioglitazone)-1.1
Placebo (Pioglitazone)-0.1
BI 10773 Low (Metformin)-1.5
BI 10773 High (Metformin)-2.0
Placebo (Metformin)-0.4
BI 10773 Low (Metformin+Sulfonylurea)-1.5
BI 10773 High (Metformin+Sulfonylurea)-1.5
Placebo (Metformin+Sulfonylurea)-0.2

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Systolic Blood Pressure: Change From Baseline After 76 Weeks of Treatment

Systolic blood pressure - change from baseline after 76 weeks of treatment (NCT01289990)
Timeframe: Baseline and 76 weeks

InterventionmmHg (Least Squares Mean)
BI 10773 Low (Drug Naive)-4.1
BI 10773 High (Drug Naive)-4.2
Placebo (Drug Naive)-0.7
Sitagliptin 100mg (Drug Naive)-0.3
BI 10773 Low (Pioglitazone)-1.7
BI 10773 High (Pioglitazone)-3.4
Placebo (Pioglitazone)0.3
BI 10773 Low (Metformin)-5.2
BI 10773 High (Metformin)-4.5
Placebo (Metformin)-0.8
BI 10773 Low (Metformin+Sulfonylurea)-3.8
BI 10773 High (Metformin+Sulfonylurea)-3.7
Placebo (Metformin+Sulfonylurea)-1.6

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Systolic Blood Pressure: Change From Baseline After 52 Weeks of Treatment

Systolic blood pressure - change from baseline after 52 weeks of treatment (NCT01289990)
Timeframe: Baseline and 52 weeks

InterventionmmHg (Least Squares Mean)
BI 10773 Low (Drug Naive)-4.9
BI 10773 High (Drug Naive)-4.5
Placebo (Drug Naive)-1.6
Sitagliptin 100mg (Drug Naive)-0.2
BI 10773 Low (Pioglitazone)-1.8
BI 10773 High (Pioglitazone)-3.3
Placebo (Pioglitazone)0.6
BI 10773 Low (Metformin)-3.6
BI 10773 High (Metformin)-5.2
Placebo (Metformin)-0.7
BI 10773 Low (Metformin+Sulfonylurea)-3.1
BI 10773 High (Metformin+Sulfonylurea)-2.7
Placebo (Metformin+Sulfonylurea)-0.2

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Diastolic Blood Pressure: Change From Baseline After 76 Weeks of Treatment

Diastolic blood pressure - change from baseline after 76 weeks of treatment (NCT01289990)
Timeframe: Baseline and 76 weeks

InterventionmmHg (Least Squares Mean)
BI 10773 Low (Drug Naive)-1.6
BI 10773 High (Drug Naive)-1.6
Placebo (Drug Naive)-0.6
Sitagliptin 100mg (Drug Naive)-0.1
BI 10773 Low (Pioglitazone)-1.3
BI 10773 High (Pioglitazone)-2.0
Placebo (Pioglitazone)0.2
BI 10773 Low (Metformin)-2.5
BI 10773 High (Metformin)-1.9
Placebo (Metformin)-0.5
BI 10773 Low (Metformin+Sulfonylurea)-2.6
BI 10773 High (Metformin+Sulfonylurea)-2.3
Placebo (Metformin+Sulfonylurea)-1.4

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Fasting Plasma Glucose Change From Baseline After 52 Weeks of Treatment

Fasting plasma glucose - change from baseline after 52 weeks of treatment (NCT01289990)
Timeframe: Baseline and 52 weeks

Interventionmg/dL (Least Squares Mean)
BI 10773 Low (Drug Naive)-18.9
BI 10773 High (Drug Naive)-23.9
Placebo (Drug Naive)13.3
Sitagliptin 100mg (Drug Naive)-3.9
BI 10773 Low (Pioglitazone)-16.7
BI 10773 High (Pioglitazone)-20.7
Placebo (Pioglitazone)10.3
BI 10773 Low (Metformin)-16.7
BI 10773 High (Metformin)-19.7
Placebo (Metformin)7.6
BI 10773 Low (Metformin+Sulfonylurea)-18.4
BI 10773 High (Metformin+Sulfonylurea)-19.3
Placebo (Metformin+Sulfonylurea)9.4

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Fasting Plasma Glucose Change From Baseline After 76 Weeks of Treatment

Fasting plasma glucose - change from baseline after 76 weeks of treatment (NCT01289990)
Timeframe: Baseline and 76 weeks

Interventionmg/dL (Least Squares Mean)
BI 10773 Low (Drug Naive)-17.2
BI 10773 High (Drug Naive)-20.4
Placebo (Drug Naive)14.4
Sitagliptin 100mg (Drug Naive)-1.8
BI 10773 Low (Pioglitazone)-13.9
BI 10773 High (Pioglitazone)-18.0
Placebo (Pioglitazone)9.4
BI 10773 Low (Metformin)-14.5
BI 10773 High (Metformin)-20.9
Placebo (Metformin)10.5
BI 10773 Low (Metformin+Sulfonylurea)-19.5
BI 10773 High (Metformin+Sulfonylurea)-20.4
Placebo (Metformin+Sulfonylurea)11.4

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Percentage of Participants Reaching A1C Goal of <6.5%

(NCT01296412)
Timeframe: Week 26

Interventionpercentage of participants (Number)
Sitagliptin +/- Glimepiride33.8
Liraglutide38.3

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Change From Baseline in Hemoglobin A1c (A1C)

A1C is measured as percent. Thus, this change from baseline reflects the Week 26 A1C percent minus the Week 0 A1C percent. (NCT01296412)
Timeframe: Baseline and Week 26

Interventionpercent (Least Squares Mean)
Sitagliptin +/- Glimepiride-1.32
Liraglutide-1.42

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Change From Baseline in Fasting Plasma Glucose (FPG)

Change from baseline at Week 26 is defined as Week 26 minus Week 0. (NCT01296412)
Timeframe: Baseline and Week 26

Interventionmg/dL (Least Squares Mean)
Sitagliptin +/- Glimepiride-33.7
Liraglutide-39.6

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Percentage of Participants Reaching A1C Goal of <7.0%

(NCT01296412)
Timeframe: Week 26

Interventionpercentage of participants (Number)
Sitagliptin +/- Glimepiride62.8
Liraglutide72.3

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Measurement of Apolipoprotein B48 and Apolipoprotein B100 Pool Sizes With Stable Isotope During Postprandial Period

(NCT01334229)
Timeframe: 6 weeks

,
Interventionmg (Mean)
apolipoprotein B48 pool sizeapolipoprotein B100 pool size
Placebo48.5537.8
Sitagliptin38.4488.0

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Measurement of Apolipoprotein B48 and Apolipoprotein B100 Production Rates With Stable Isotope During Postprandial Period

(NCT01334229)
Timeframe: 6 weeks

,
Interventionmg/kg/day (Mean)
apolipoprotein B48 production rateapolipoprotein B100 production rate
Placebo2.530.3
Sitagliptin2.127.5

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Measurement of Glucagon-like Peptide-1 by ELISA

(NCT01334229)
Timeframe: 6 weeks

Interventionpmol/L (Mean)
Sitagliptin5.6
Placebo3.1

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Measurement of Glucose

(NCT01334229)
Timeframe: 6 weeks

Interventionmmol/L (Mean)
Sitagliptin7.7
Placebo8.9

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Measurement of Insulin

(NCT01334229)
Timeframe: 6 weeks

Interventionpmol/L (Mean)
Sitagliptin161.1
Placebo179.5

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Measurement of Apolipoprotein B48 and Apolipoprotein B100 Fractional Catabolic Rates With Stable Isotope During Postprandial Period

(NCT01334229)
Timeframe: 6 weeks

,
Interventionpools/day (Mean)
apolipoprotein B48 fractional catabolic rateapolipoprotein B100 fractional catabolic rate
Placebo6.35.9
Sitagliptin6.25.9

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Change From Baseline in Body Weight at Week 1, 2, 4, 8 and 12

Overweight or obesity increases the risk for developing diabetes. The treatment of diabetes has been the recommendation to lose weight. As weight loss progresses and is maintained, an improvement of glycemia may be evidenced by a reduction in HbA1c. (NCT01336738)
Timeframe: Baseline, Week 1, 2, 4, 8, 12

,,,,
Interventionkilogram (kg) (Mean)
Baseline (n=52, 53, 52, 54, 53)Change at Week 1 (n=50, 51, 49, 51, 51)Change at Week 2 (n=50, 52, 51, 50, 48)Change at Week 4 (n=49, 49, 49, 50, 46)Change at Week 8 (n=46, 44, 45, 48, 45)Change at Week 12 (n=45, 44, 45, 48, 43)
PF-04991532 150 mg92.57-0.10-0.12-0.18-0.27-0.91
PF-04991532 450 mg88.91-0.31-0.33-0.72-0.66-0.82
PF-04991532 750 mg86.08-0.34-0.38-0.34-0.45-0.90
Placebo87.43-0.33-0.37-0.52-0.60-0.95
Sitagliptin 100 mg87.480.14-0.000.15-0.21-0.22

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Percentage of Participants With Greater Than or Equal to (>=) 1% or >= 2% Body Weight Loss From Baseline

The treatment of diabetes has been the recommendation to lose weight. As weight loss progresses and is maintained, an improvement of glycemia may be evidenced by a reduction in HbA1c. Participants with >= 1% or >= 2% body weight loss from baseline signifies an improvement of glycemia. (NCT01336738)
Timeframe: Week 12

,,,,
Interventionpercentage of participants (Number)
>= 1%>= 2%
PF-04991532 150 mg55.5626.67
PF-04991532 450 mg47.7334.09
PF-04991532 750 mg46.6731.11
Placebo41.8634.88
Sitagliptin 100 mg29.1718.75

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Percentage of Participants Achieving Less Than (<) 6.5% or <7% Glycosylated Hemoglobin (HbA1c) Levels

HbA1c is a form of hemoglobin which is measured primarily to identify the average plasma glucose concentration over prolonged periods of time. The normal range for the HbA1c test is between 4% and 5.6%. HbA1c levels between 5.7% and 6.4% indicate increased risk of diabetes and levels of 6.5% or higher indicate diabetes. (NCT01336738)
Timeframe: Week 12

,,,,
Interventionpercentage of participants (Number)
< 6.5%< 7%
PF-04991532 150 mg4.513.6
PF-04991532 450 mg9.136.4
PF-04991532 750 mg23.360.5
Placebo11.616.3
Sitagliptin 100 mg14.639.6

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Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 12

HbA1c is a form of hemoglobin which is measured primarily to identify the average plasma glucose concentration over prolonged periods of time. The normal range for the HbA1c test is between 4 percent (%) and 5.6%. HbA1c levels between 5.7% and 6.4% indicate increased risk of diabetes and levels of 6.5% or higher indicate diabetes. (NCT01336738)
Timeframe: Baseline, Week 12

,,,,
Interventionpercentage of hemoglobin (Mean)
Baseline (n=52, 53, 52, 54, 53)Change at Week 12 (n=44, 44, 43, 48, 43)
PF-04991532 150 mg8.34-0.17
PF-04991532 450 mg8.19-0.57
PF-04991532 750 mg7.96-0.70
Placebo8.55-0.21
Sitagliptin 100 mg7.97-0.78

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Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 1, 2, 4 and 8

HbA1c is a form of hemoglobin which is measured primarily to identify the average plasma glucose concentration over prolonged periods of time. The normal range for the HbA1c test is between 4% and 5.6%. HbA1c levels between 5.7% and 6.4% indicate increased risk of diabetes and levels of 6.5% or higher indicate diabetes. (NCT01336738)
Timeframe: Baseline, Week 1, 2, 4, 8

,,,,
Interventionpercentage of hemoglobin (Mean)
Change at Week 1 (n=50, 51, 49, 49, 48)Change at Week 2 (n=50, 52, 49, 49, 47)Change at Week 4 (n=48, 49, 48, 50, 46)Change at Week 8 (n=45, 44, 45, 47, 45)
PF-04991532 150 mg-0.04-0.04-0.22-0.21
PF-04991532 450 mg-0.03-0.14-0.34-0.50
PF-04991532 750 mg-0.13-0.18-0.40-0.66
Placebo-0.02-0.07-0.16-0.22
Sitagliptin 100 mg-0.07-0.23-0.42-0.71

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Change From Baseline in Fasting Plasma Glucose at Week 1, 2, 4, 8 and 12

(NCT01336738)
Timeframe: Baseline, Week 1, 2, 4, 8, 12

,,,,
Interventionmilligram/deciliter (mg/dL) (Mean)
Baseline (n=52, 53, 52, 54, 53)Change at Week 1 (n=50, 51, 49, 49, 51)Change at Week 2 (n=50, 51, 51, 50, 47)Change at Week 4 (n=49, 49, 49, 50, 45)Change at Week 8 (n=46, 44, 44, 47, 45)Change at Week 12 (n=45, 44, 44, 48, 43)
PF-04991532 150 mg172.680.87-4.481.133.690.08
PF-04991532 450 mg169.161.634.13-5.14-1.495.87
PF-04991532 750 mg159.11-1.55-5.26-6.682.956.86
Placebo183.61-4.21-3.72-4.282.18-0.03
Sitagliptin 100 mg158.38-13.72-15.70-21.86-14.05-17.64

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Percentage of Participants With Greater Than or Equal to (>=) 1% or >= 2% Body Weight Gain From Baseline

Overweight or obesity increases the risk for developing diabetes. Participants with >= 1% or >= 2% body weight gain from baseline signifies a higher risk of diabetes. (NCT01336738)
Timeframe: Week 12

,,,,
Interventionpercentage of participants (Number)
>= 1%>= 2%
PF-04991532 150 mg17.786.67
PF-04991532 450 mg18.1811.36
PF-04991532 750 mg15.5611.11
Placebo23.266.98
Sitagliptin 100 mg29.1714.58

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Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 1, 2, 4 and 8

HbA1c is a form of hemoglobin which is measured primarily to identify the average plasma glucose concentration over prolonged periods of time. The normal range for the HbA1c test is between 4% and 5.6%. HbA1c levels between 5.7% and 6.4% indicate increased risk of diabetes and levels of 6.5% or higher indicate diabetes. (NCT01338870)
Timeframe: Baseline, Week 1, 2, 4, 8

,,,,,
Interventionpercentage of hemoglobin (Mean)
Change at Week 1 (n= 48, 47, 47, 46, 46, 47)Change at Week 2 (n= 45, 44, 45, 45, 47, 48)Change at Week 4 (n= 46, 42, 44, 45, 48, 49)Change at Week 8 (n= 43, 40, 41, 42, 45, 45)
PF-04991532 150 mg-0.06-0.06-0.32-0.42
PF-04991532 25 mg-0.01-0.10-0.15-0.14
PF-04991532 300 mg-0.02-0.17-0.37-0.58
PF-04991532 75 mg-0.07-0.08-0.26-0.40
Placebo0.03-0.02-0.14-0.26
Sitagliptin 100 mg-0.14-0.21-0.40-0.54

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Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 12

HbA1c is a form of hemoglobin which is measured primarily to identify the average plasma glucose concentration over prolonged periods of time. The normal range for the HbA1c test is between 4 percent (%) and 5.6%. HbA1c levels between 5.7% and 6.4% indicate increased risk of diabetes and levels of 6.5% or higher indicate diabetes. (NCT01338870)
Timeframe: Baseline, Week 12

,,,,,
Interventionpercentage of hemoglobin (Mean)
Baseline (n= 50, 49, 50, 50, 52, 50)Change at Week 12 (n= 42, 37, 39, 40, 46, 44)
PF-04991532 150 mg7.93-0.36
PF-04991532 25 mg7.90-0.15
PF-04991532 300 mg8.01-0.79
PF-04991532 75 mg7.86-0.51
Placebo8.11-0.30
Sitagliptin 100 mg8.05-0.65

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Percentage of Participants Achieving Less Than (<) 6.5% or <7% Glycosylated Hemoglobin (HbA1c) Levels

HbA1c is a form of hemoglobin which is measured primarily to identify the average plasma glucose concentration over prolonged periods of time. The normal range for the HbA1c test is between 4% and 5.6%. HbA1c levels between 5.7% and 6.4% indicate increased risk of diabetes, and levels of 6.5% or higher indicate diabetes. (NCT01338870)
Timeframe: Week 12

,,,,,
Interventionpercentage of participants (Number)
< 6.5%< 7%
PF-04991532 150 mg17.535.0
PF-04991532 25 mg8.129.7
PF-04991532 300 mg17.443.5
PF-04991532 75 mg15.438.5
Placebo11.923.8
Sitagliptin 100 mg15.936.4

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Percentage of Participants With Greater Than or Equal to (>=) 1% or >= 2% Gain in Body Weight From Baseline

Overweight or obesity increases the risk for developing diabetes. Participants with >= 1% or >= 2% gain in body weight from baseline signifies a higher risk of diabetes. (NCT01338870)
Timeframe: Week 12

,,,,,
Interventionpercentage of participants (Number)
>= 1%>= 2%
PF-04991532 150 mg21.957.32
PF-04991532 25 mg27.032.70
PF-04991532 300 mg15.226.52
PF-04991532 75 mg38.4615.38
Placebo23.812.38
Sitagliptin 100 mg31.8215.91

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Percentage of Participants With Greater Than or Equal to (>=) 1% or >= 2% Loss in Body Weight From Baseline

The treatment of diabetes has been the recommendation to lose weight. As weight loss progresses and is maintained, an improvement of glycemia may be evidenced by a reduction in HbA1c. Participants with >= 1% or >= 2% loss in body weight from baseline signifies an improvement of glycemia. (NCT01338870)
Timeframe: Week 12

,,,,,
Interventionpercentage of participants (Number)
>= 1%>= 2%
PF-04991532 150 mg48.7826.83
PF-04991532 25 mg35.1427.03
PF-04991532 300 mg41.3030.43
PF-04991532 75 mg30.7717.95
Placebo38.1023.81
Sitagliptin 100 mg40.9129.55

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Change From Baseline in Fasting Plasma Glucose at Week 1, 2, 4, 8 and 12

(NCT01338870)
Timeframe: Baseline, Week 1, 2, 4, 8, 12

,,,,,
Interventionmilligram/deciliter (mg/dL) (Mean)
Baseline (n= 50, 49, 50, 50 ,52, 50)Change at Week 1 (n= 48, 47, 47, 46, 46, 45)Change at Week 2 (n= 44, 44, 45, 45, 47, 48)Change at Week 4 (n= 46, 42, 44, 45, 48, 49)Change at Week 8 (n= 43, 40, 41, 42, 46, 45)Change at Week 12 (n= 42, 37, 38, 40, 46, 44)
PF-04991532 150 mg163.38-3.75-1.683.614.436.20
PF-04991532 25 mg167.71-0.701.056.089.428.06
PF-04991532 300 mg168.87-15.35-16.68-19.84-14.24-16.80
PF-04991532 75 mg161.43-3.29-3.84-6.56-4.98-6.55
Placebo168.413.69-1.312.005.633.41
Sitagliptin 100 mg170.42-18.59-20.13-18.90-17.84-16.07

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Change From Baseline in Body Weight at Week 1, 2, 4, 8 and 12

Overweight or obesity increases the risk for developing diabetes. The treatment of diabetes has been the recommendation to lose weight. As weight loss progresses and is maintained, an improvement of glycemia may be evidenced by a reduction in HbA1c. (NCT01338870)
Timeframe: Baseline, Week 1, 2, 4, 8, 12

,,,,,
Interventionkilogram (kg) (Mean)
Baseline (n= 50, 49, 50, 50, 52, 50)Change at Week 1 (n= 48, 47, 47, 46, 47, 47)Change at Week 2 (n= 45, 44, 45, 45, 47, 48)Change at Week 4 (n= 46, 42, 44, 45, 48, 49)Change at Week 8 (n= 43, 40, 41, 42, 46, 45)Change at Week 12 (n= 42, 37, 39, 41, 46, 44)
PF-04991532 150 mg85.44-0.20-0.25-0.27-0.64-0.83
PF-04991532 25 mg87.24-0.20-0.49-0.55-0.57-0.71
PF-04991532 300 mg91.61-0.20-0.03-0.58-0.67-0.75
PF-04991532 75 mg85.690.140.070.20-0.04-0.15
Placebo89.690.010.31-0.10-0.21-0.30
Sitagliptin 100 mg91.00-0.33-0.32-0.30-0.61-0.83

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Percentage of Participants With at Least One Symptomatic Hypoglycemic Event

Symptomatic hypoglycemic events were based on the participants own self-reported symptoms (for example, but not limited to the following: faintness, headache, confusion, anxiety, sweating, tremor, palpitations, nausea, pallor, dizziness, hunger, sudden behavioral change). (NCT01340768)
Timeframe: Up to 30 days (Day 1 through last day of Ramadan)

Interventionpercentage of participants (Number)
Sitagliptin3.8
Sulfonylurea Therapy7.3

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Percentage of Participants With at Least One Symptomatic or Asymptomatic Hypoglycemic Event

Symptomatic hypoglycemic events were based on the participants own self-reported symptoms (for example but not limited to the following: faintness, headache, confusion, anxiety, sweating, tremor, palpitations, nausea, pallor, dizziness, hunger, sudden behavioral change). Asymptomatic hypoglycemic events were based on self-monitored finger-stick blood glucose level. (NCT01340768)
Timeframe: Up to 30 days (Day 1 through last day of Ramadan)

Interventionpercentage of participants (Number)
Sitagliptin4.8
Sulfonylurea Therapy9.6

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Number of Participants With an Adverse Event

(NCT01354990)
Timeframe: Up to approximately 28 months

Interventionparticipants (Number)
Sitagliptin Phosphate (JANUVIA®)25

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Number of Participants With Concomitant Conditions

(NCT01354990)
Timeframe: Up to approximately 28 months

Interventionparticipants (Number)
Sitagliptin Phosphate (JANUVIA®)752

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Number of Participants With Concomitant Therapies

(NCT01354990)
Timeframe: Up to approximately 28 months

Interventionparticipants (Number)
Sitagliptin Phosphate (JANUVIA®)1878

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Age of Participants Prescribed Sitagliptin

(NCT01354990)
Timeframe: Up to approximately 28 months

Interventionyears (Mean)
Sitagliptin Phosphate (JANUVIA®)55

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Percentage of Participants With Strict Changes in Initial Dual Therapy

Strict changes in dual therapy were defined as withdrawal of an agent, replacement of one agent by another, or the addition of a third agent. Changes in dose level were not considered strict changes. (NCT01357135)
Timeframe: Up to 3 years

InterventionPercentage of Participants (Number)
Metformin + Sitagliptin33.1
Metformin + Sulfonylurea46.5

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Median Duration (in Months) of Initial Dual Therapy

The treatment maintenance duration corresponds to the treatment maintenance and persistence duration for dual therapy combining the same agents. Withdrawal of an agent, replacement of one agent by another or addition of a third agent is perceived as a change in treatment and, hence, the end of the treatment maintenance duration for dual therapy. (NCT01357135)
Timeframe: Up to 3 years

Interventionmonths (Median)
Metformin + Sitagliptin43.2
Metformin + Sulfonylurea20.2

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Age of Participants Prescribed Sitagliptin Phosphate/Metformin HCl

(NCT01357148)
Timeframe: Up to approximately 28 months

Interventionyears (Mean)
Sitagliptin Phosphate/Metformin HCl51

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Number of Participants Taking Concomitant Medications

(NCT01357148)
Timeframe: Up to approximately 28 months

Interventionparticipants (Number)
Sitagliptin Phosphate/Metformin HCl86

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Number of Participants With an Adverse Event

(NCT01357148)
Timeframe: Up to approximately 28 months

Interventionparticipants (Number)
Sitagliptin Phosphate/Metformin HCl6

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Number of Participants With Concomitant Conditions

(NCT01357148)
Timeframe: Up to approximately 28 months

Interventionparticipants (Number)
Sitagliptin Phosphate/Metformin HCl100

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Bone Turnover in Subjects Treated With Sitagliptin When Compared to Those Treated With Placebo

Bone turnover assessed using change in bone-specific alkaline phosphatase (BAP) over 8 weeks of treatment. (NCT01374568)
Timeframe: 8 WEEKS

Interventionmg/L (Mean)
Sitagliptin0.05
Placebo0

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Bone Turnover in Subjects Treated With Sitagliptin When Compared to Those Treated With Placebo.

Bone turnover assessed using change in TRACP5b over 8 weeks of treatment. (NCT01374568)
Timeframe: 8 weeks

InterventionU/L (Mean)
Sitagliptin-0.25
Placebo0.30

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Number of Participants With Clinical Chemistry Abnormalities of Potential Clinical Importance (PCI)

Clinical chemistry parameters included blood urea nitrogen (BUN), potassium, aspartate aminotransferase (AST), total bilirubin, direct bilirubin, creatinine, chloride, alanine aminotransferase (ALT), uric acid, fasting glucose, total carbon dioxide, gamma glutamyltransferase (GGT), albumin, sodium, calcium, alkaline phosphatase (ALP), total protein, creatine phosphokinase (CPK) and fasting lipid panel including total cholesterol, triglycerides, high density lipoprotein (HDL) cholesterol and low density lipoprotein (LDL) cholesterol. It was assessed on Baseline (pre-dose Day 1), Week 3 and 12. Data for parameters with high and low of PCI is provided. (NCT01376323)
Timeframe: Up to Week 12

,,,,
InterventionParticipants (Count of Participants)
Potassium, highPotassium, lowAlbumin, lowCreatine kinase, highCreatinine, highTotal bilirubin, high
GSK256073 10 mg Once Daily100100
GSK256073 25 mg BID000001
GSK256073 5 mg BID000100
GSK256073 50 mg Once Daily100000
Placebo (Pooled)112210

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Number of Participants With HbA1c < 7.0% and < 6.5%

Data has been presented for number of participants with their corresponding percentages with HbA1c <7.0% and <6.5%. (NCT01376323)
Timeframe: Up to Week 12

,,,,
InterventionParticipants (Count of Participants)
<7%<6.5%
GSK256073 10 mg Once Daily20
GSK256073 25 mg BID31
GSK256073 5 mg BID30
GSK256073 50 mg Once Daily114
Placebo (Pooled)42

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Number of Participants With Hematology Abnormalities of Potential Clinical Importance (PCI)

Hematology parameters included platelet, red blood cell (RBC) count, mean corpuscular volume (MCV), neutrophils, white blood cell (WBC) count (absolute), mean corpuscular hemoglobin (MCH), lymphocytes, reticulocyte count, mean corpuscular hemoglobin concentration (MCHC), monocytes, hemoglobin, eosinophils, hematocrit and basophils. It was assessed on Baseline (pre-dose Day 1) and 12. Data for parameters with high and low of PCI is provided. (NCT01376323)
Timeframe: Up to Week 12

,,,,
InterventionParticipants (Count of Participants)
Total neutrophils, lowPlatelet count, lowLymphocytes, lowWBC, low
GSK256073 10 mg Once Daily0000
GSK256073 25 mg BID1021
GSK256073 5 mg BID0100
GSK256073 50 mg Once Daily0100
Placebo (Pooled)3100

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Summary of Homeostatic Model Assessment (HOMA) Index Calculated From Change From Baseline in Fasting Insulin and Fasting Glucose at Week 12

Mean of triplicate measurements at pre-dose time point was considered for the summary. HOMA was calculated by multiplying insulin concentration with glucose concentration divided by 22.5. Change from Baseline for insulin and glucose was calculated by subtracting the Baseline values from the corresponding post-treatment values. Baseline was defined as mean of Day 1 pre-dose visit. Statistics is provided for least square mean. It was assessed on Day 1 (pre-dose), 2 (pre-dose), Week 6 (pre-dose) and Week 12. (NCT01376323)
Timeframe: Baseline (Day 1) and up to Week 12

,,,,
InterventionIndex (Mean)
Day 2Week 6Week 12
GSK256073 10 mg Once Daily0.3-0.3-0.3
GSK256073 25 mg BID-0.2-0.41.5
GSK256073 5 mg BID1.1-1.40.0
GSK256073 50 mg Once Daily-0.2-0.7-0.1
Placebo (Pooled)0.2-0.6-0.0

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Number of Participants With Abnormal Electrocardiograms (ECGs) Findings

Single 12-lead ECGs were obtained at each time point during the study using an ECG machine that automatically calculated the heart rate and measured PR, QRS, QT, and QTc intervals. It was assessed at Baseline (pre-dose Day 1), Day 2, Week 3, Week 6 and 12. Participants with normal, abnormal not clinically significant and abnormal clinically significant ECG were presented. (NCT01376323)
Timeframe: Up to Week 20

InterventionParticipants (Count of Participants)
Day 172552205Day 172552208Day 172552209Day 172552206Day 172552207Day 272552205Day 272552208Day 272552209Day 272552206Day 272552207Week 372552208Week 372552209Week 372552207Week 372552205Week 372552206Week 672552207Week 672552208Week 672552209Week 672552205Week 672552206Week 1272552205Week 1272552208Week 1272552209Week 1272552206Week 1272552207
normalabnormal not clinically significantabnormal clinically significant
Placebo (Pooled)12
GSK256073 25 mg BID18
GSK256073 50 mg Once Daily12
Placebo (Pooled)8
GSK256073 5 mg BID4
GSK256073 10 mg Once Daily6
GSK256073 25 mg BID1
GSK256073 50 mg Once Daily6
GSK256073 25 mg BID0
GSK256073 50 mg Once Daily0
Placebo (Pooled)14
Placebo (Pooled)6
GSK256073 10 mg Once Daily5
Placebo (Pooled)17
GSK256073 25 mg BID16
GSK256073 50 mg Once Daily13
GSK256073 25 mg BID2
GSK256073 50 mg Once Daily4
Placebo (Pooled)16
GSK256073 5 mg BID14
GSK256073 10 mg Once Daily14
Placebo (Pooled)3
GSK256073 5 mg BID3
GSK256073 25 mg BID4
Placebo (Pooled)0
GSK256073 5 mg BID0
Placebo (Pooled)10
GSK256073 10 mg Once Daily13
GSK256073 25 mg BID12
GSK256073 50 mg Once Daily14
GSK256073 10 mg Once Daily3
GSK256073 25 mg BID3
GSK256073 50 mg Once Daily3
GSK256073 10 mg Once Daily0

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Change From Baseline in Fasting Plasma Glucose at Week 12

Mean of triplicate measurements at pre-dose time point were considered for the summary. Change from Baseline was calculated by subtracting the Baseline values from the corresponding post-treatment values. Baseline was defined as mean of Day 1 pre-dose visit. Statistics is provided for least square mean at Week 12. It was assessed on Day 1 (pre-dose), 2 (pre-dose), Week 6 (pre-dose) and Week 12. (NCT01376323)
Timeframe: Baseline (Day 1) and up to Week 12

,,,,
InterventionMillimoles per liter (Mean)
Day 2Week 6Week 12
GSK256073 10 mg Once Daily0.04-1.06-0.71
GSK256073 25 mg BID0.04-0.62-0.44
GSK256073 5 mg BID-0.05-0.82-0.85
GSK256073 50 mg Once Daily-0.34-0.91-0.83
Placebo (Pooled)0.09-0.25-0.64

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Change From Baseline in 12 Hour Non-esterified Fatty Acids (NEFA) and Glucose Weighted Mean Concentration Value at Day 2 and at Week 6

Change from Baseline was calculated by subtracting the Baseline values from the corresponding post-treatment values. Baseline was defined as weighted mean value at Day 1 visit. Statistics is provided for least square mean at Week 6. It was assessed on Baseline (Day 1), Day 2 and Week 6. (NCT01376323)
Timeframe: Baseline (Day 1) and up to Week 6

,,,,
InterventionMillimoles per liter (Mean)
Glucose, Day 2Glucose, Week 6NEFA, Day 2NEFA, Week 6
GSK256073 10 mg qd0.036-0.502-0.1326-0.0423
GSK256073 25 mg Bid-0.517-0.647-0.1926-0.0293
GSK256073 5 mg Bid-0.502-0.786-0.1307-0.0342
GSK256073 50 mg qd-0.076-0.544-0.1503-0.1032
Placebo (Pooled)0.4620.009-0.0152-0.0457

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Change From Baseline in Fasting Insulin at Week 12

Mean of triplicate measurements at pre-dose time point were considered for the summary. Change from Baseline was calculated by subtracting the Baseline values from the corresponding post-treatment values. Baseline was defined as mean of Day 1 pre-dose visit. Statistics is provided for least square mean at Week 12. It was assessed on Day 1 (pre-dose), 2 (pre-dose), Week 6 (pre-dose) and Week 12. (NCT01376323)
Timeframe: Baseline (Day 1) and up to Week 12

,,,,
InterventionPicomoles per liter (Mean)
Day 2Week 6Week 12
GSK256073 10 mg qd6.62.9-2.0
GSK256073 25 mg BID-2.8-6.033.4
GSK256073 5 mg BID19.1-9.114.7
GSK256073 50 mg qd0.22.64.7
Placebo (Pooled)-1.1-3.927.3

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Change From Baseline in Fructosamine at Week 6 and Week 12

Change from Baseline was calculated by subtracting the Baseline values from the corresponding post-treatment values. Baseline was defined as mean of Day -1 visit. Statistics is provided for least square mean. It was assessed on Baseline (Day -1), Day 41 and Week 12. (NCT01376323)
Timeframe: Baseline (Day -1) and Week 12

,,,,
InterventionMicromoles per liter (Mean)
Day 41Week 12
GSK256073 10 mg Once Daily-21.2-30.7
GSK256073 25 mg BID-26.3-25.4
GSK256073 5 mg BID-18.8-16.4
GSK256073 50 mg Once Daily-21.1-36.1
Placebo (Pooled)-14.9-22.3

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Change From Baseline in Glycated Hemoglobin (HbA1c) at Week 12

Blood samples for analysis of HbA1c were collected at Baseline (Day -1), Day 41, Week 9 and Week 12. Change from Baseline was calculated by subtracting the Baseline values from the corresponding post-treatment values. Baseline was defined as Day -1 visit. Statistics is provided for least square mean at Week 12. (NCT01376323)
Timeframe: Baseline (Day -1) and up to Week 12

,,,,
InterventionPercentage of Glycosylated Hemoglobin (Mean)
Day 41Week 9Week 12
GSK256073 10 mg Once Daily-0.37-0.48-0.46
GSK256073 25 mg BID-0.42-0.56-0.56
GSK256073 5 mg BID-0.18-0.24-0.14
GSK256073 50 mg Once Daily-0.44-0.59-0.64
Placebo (Pooled)-0.34-0.44-0.36

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Change From Baseline in Heart Rate

Mean of triplicate measurements at each time point was considered for the summary. Baseline was defined as pre-dose of Day 1 visit. Change from Baseline was calculated by subtracting the Baseline values from the corresponding post-treatment values. It was assessed on Baseline (pre-dose Day 1), Day 1 (12 hours), Day 2, Week 3, 6, 9 and 12. (NCT01376323)
Timeframe: Baseline (pre-dose Day 1) and up to Week 12

,,,,
InterventionBeats per minute (Mean)
Day 1,12 hoursDay 2, pre-doseDay 2, 12 hoursWeek 3Day 6, pre-doseDay 6, 12 hoursWeek 9Week 12
GSK256073 10mg Once Daily1.12.64.63.10.53.34.94.1
GSK256073 25mg BID1.30.93.80.13.16.64.43.9
GSK256073 50mg Once Daily0.71.31.51.2-1.2-3.83.2-0.5
GSK256073 5mg BID-1.01.21.91.2-1.62.23.61.1
Placebo (Pooled)2.51.23.33.2-0.92.91.72.8

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Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)

Mean of triplicate measurements at each time point was considered for the summary. Baseline was defined as pre-dose of Day 1 visit. Change from Baseline was calculated by subtracting the Baseline values from the corresponding post-treatment values. It was assessed on Baseline, Day 1 (12 hours), Day 2 (pre-dose and 12 hours), Week 3, 6 (pre-dose and 12 hours), 9 and 12. (NCT01376323)
Timeframe: Baseline (pre-dose Day 1) and up to Week 12

,,,,
InterventionMillimeters of mercury (Mean)
SBP, Day 1,12 hoursSBP, Day 2, pre-doseSBP, Day 2, 12 hoursSBP, Week 3SBP, Day 6, pre-doseSBP, Day 6, 12 hoursSBP, Week 9SBP, Week 12DBP, Day 1,12 hoursDBP, Day 2, pre-doseDBP, Day 2, 12 hoursDBP, Week 3DBP, Day 6, pre-doseDBP, Day 6, 12 hoursDBP, Week 9DBP, Week 12
GSK256073 10mg Once Daily4.9-7.71.10.5-3.41.0-1.6-0.32.0-2.11.4-0.1-0.41.00.10.7
GSK256073 25mg BID3.0-1.71.7-1.7-5.32.7-2.02.8-0.5-1.70.8-0.5-2.00.6-0.90.9
GSK256073 50mg Once Daily1.9-4.7-1.8-1.1-5.81.6-3.80.43.2-0.22.01.0-1.41.5-1.20.3
GSK256073 5mg BID0.9-6.5-3.8-3.9-7.7-2.5-9.1-6.40.6-2.1-0.60.3-4.7-1.7-2.8-3.4
Placebo (Pooled)3.4-0.80.73.7-0.16.64.02.31.4-1.20.82.21.32.93.30.1

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Number of Participants With Abnormal Urinalysis: Glucose, Protein, Blood and Ketones by Dipstick

Urinalysis parameters included glucose, protein, blood and ketones by dipstick. It was assessed on Baseline (Day -1) and 12. Urine glucose was measured as grams per deciliter (G/dL). (NCT01376323)
Timeframe: Up to Week 12

,,,,
InterventionParticipants (Count of Participants)
Urine glucose, Day -1, NegativeUrine glucose, Day -1, TraceUrine glucose, Day -1, Trace or 1/10 g/dLUrine glucose, Day -1, 1+ or 1/4 g/dLUrine glucose, Day -1, 2+ or 1/2 g/dLUrine glucose, Day -1, 3+ or 1 g/dLUrine glucose, Day 41, NegativeUrine glucose, Day 41, TraceUrine glucose, Day 41, Trace or 1/10 g/dLUrine glucose, Day 41, 1+ or 1/4 g/dLUrine glucose, Day 41, 2+ or 1/2 g/dLUrine glucose, Day 41, 3+ or 1 g/dLUrine glucose, Week 12, NegativeUrine glucose, Week 12, TraceUrine glucose, Week 12, Trace or 1/10 g/dLUrine glucose, Week 12, 1+ or 1/4 g/dLUrine glucose, Week 12, 2+ or 1/2 g/dLUrine glucose, Week 12, 3+ or 1 g/dLUrine ketones, Day -1, NegativeUrine ketones, Day -1, TraceUrine ketones, Day -1, 1+Urine ketones, Day 41, NegativeUrine ketones, Day 41, TraceUrine ketones, Day 41, 1+ or 1/4Urine ketones, Day 41, 2+Urine ketones, Week 12, NegativeUrine ketones, Week 12, TraceUrine ketones, Week 12, 1+ or 1/4Urine occult blood, Day -1, NegativeUrine occult blood, Day -1, TraceUrine occult blood, Day -1, 1+Urine occult blood, Day 41, NegativeUrine occult blood, Day 41, TraceUrine occult blood, Week 12, NegativeUrine occult blood, Week 12, TraceUrine occult blood, Week 12, 1+Urine protein, Day -1, NegativeUrine protein, Day -1, TraceUrine protein, Day -1, 1+Urine protein, Day -1, 2+Urine protein, Day -1, 3+Urine protein, Day 41, NegativeUrine protein, Day 41, TraceUrine protein, Day 41, 1+Urine protein, Day 41, 2+Urine protein, Week 12, NegativeUrine protein, Week 12, TraceUrine protein, Week 12, 1+Urine protein, Week 12, 2+Urine protein, Week 12, 3+
GSK256073 10 mg Once Daily14022101301200130001119001321015001630151150012421013111140100
GSK256073 25 mg BID102330112011128113011810142101211170215212111422011501193101
GSK256073 5 mg BID11041111203002130210117011510114301701152150213221012311122210
GSK256073 50 mg Once Daily14012011302101150000117101430012311800170160014400014300142000
Placebo (Pooled)13012031311103130121118101810017101810190170118001017110152100

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Number of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)

An AE is defined as any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, is a congenital anomaly/birth defect, may jeopardize the participant or require medical or surgical intervention to prevent one of the other outcomes listed in the definition above, or is an event of possible drug-induced liver injury. (NCT01376323)
Timeframe: Up to Week 12

,,,,
InterventionParticipants (Count of Participants)
Any AEAny SAE
GSK256073 10 mg Once Daily120
GSK256073 25 mg BID112
GSK256073 5 mg BID120
GSK256073 50 mg Once Daily100
Placebo (Pooled)111

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Number of Subjects With Acute Renal Failure Among the Three Randomized Groups During Hospitalization

Acute renal failure is defined as a clinical diagnosis of acute renal failure with documented new-onset abnormal renal function (serum creatinine > 2.2 mg/dL or an increment > 0.5 mg/dL from baseline). The total daily dose of insulin and sitagliptin will be adjusted as per serum creatinine concentration. The total daily insulin dose will be reduced to 0.3 unit/kg in patients with creatinine >1.7 mg/dl. The dose of sitagliptin will be reduced to 50 mg/day in patients with creatinine clearance between 30-50 ml/min (approximate serum creatinine levels >1.7 and ≤3.0 mg/dl for men and >1.5 and ≤2.5 mg/dl for women). (NCT01378117)
Timeframe: during hospitalization, up to 10 days

InterventionParticipants (Count of Participants)
Sitagliptin + SSI Prn0
Sitagliptin and Glargine + SSI0
Glargine and Lispro + SSI0

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Mean Blood Glucose Levels Among the Three Groups at the Time of Hospitalization to 1st Day After Therapy

The primary outcome of the study is to determine differences in glycemic control as measured by mean BG concentration between sitagliptin once daily and basal bolus therapy with glargine once daily plus supplemental lispro insulin in hospitalized patients with type 2 diabetes mellitus, at the time of admission to the blood glucose levels 24hrs after the therapy (NCT01378117)
Timeframe: Admission and after 1st day of therapy

,,
Interventionmg/dl (Mean)
At time of admissionAfter 1st day of therapy
Glargine and Lispro + SSI225158.3
Sitagliptin + SSI Prn209168.4
Sitagliptin and Glargine + SSI203154.2

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Percent of Blood Glucose Readings Within Target Range Between 70 and 140 mg/dL Among the Three Groups After 24 Hrs of Randomized Treatment

The blood glucose within target range is defined as the levels between 70 mg/dL and 140 mg/dL. BG was measured before each meal and at bedtime (or every 6 h if a patient was not eating) using a point-of-care glucose meter (ACCUCHECK; Roche, Indianapolis, IN). In addition, BG was measured at any time if a patient experienced symptoms of hypoglycemia or if requested by the treating physician. the percentage of the readings are calculated and compared (NCT01378117)
Timeframe: during hospitalization, up to 10 days

Interventionpercentage of blood glucose readings (Mean)
Sitagliptin + SSI Prn36
Sitagliptin and Glargine + SSI43
Glargine and Lispro + SSI43

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Number of Patients With Severe Hypoglycemic Episodes Among the 3 Treatment Groups

severe hypoglycemic episodes are defined as blood glucose levels <40 mg/dl. The number of patients with these events during the 5 days of hospitalization are recorded and compared. BG was measured before each meal and at bedtime (or every 6 h if a patient was not eating) using a point-of-care glucose meter. (NCT01378117)
Timeframe: during hospitalization,up to 5 days

InterventionParticipants (Count of Participants)
Sitagliptin + SSI Prn0
Sitagliptin and Glargine + SSI0
Glargine and Lispro + SSI0

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Number of Patients With Hypoglycemic Events Among the Treatment Groups

Hypoglycemia is defined as blood glucose (BG) reading <70 mg/dl. The number of hypoglycemia events during hospitalization are recorded and compared among the different groups. BG was measured before each meal and at bedtime (or every 6 h if a patient was not eating) using a point-of-care glucose meter (NCT01378117)
Timeframe: during hospitalization,up to 10 days

InterventionParticipants (Count of Participants)
Sitagliptin + SSI Prn1
Sitagliptin and Glargine + SSI2
Glargine and Lispro + SSI2

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Number of Patients With a Mean Daily BG > 240 mg/dL After the 1st Day of Treatment Among the Treatment Groups

Mean daily blood glucose levels are measured to assess the treatment Failures. For study purpose Treatment failure was defined as having three or more consecutive Blood Glucose (BG) readings > 240 mg/dL or a mean daily BG >240 mg/dL after the 1st day of treatment. Number of patients with a mean daily BG > 240 mg/dL after the 1st day of treatment are recorded and compared among the treatment groups. BG was measured before each meal and at bedtime (or every 6 h if a patient was not eating) using a point-of-care glucose meter. (NCT01378117)
Timeframe: during hospitalization,up to 10 days

InterventionParticipants (Count of Participants)
Sitagliptin + SSI Prn3
Sitagliptin and Glargine + SSI1
Glargine and Lispro + SSI2

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Mean Total Daily Dose of Insulin in Units/Day Given During Hospitalization Among the Three Groups

The total insulin includes total glargine insulin (units/day) and total lispro insulin (units/day) given to subjects for maintaining blood glucose levels during hospitalization in different groups. The goal of therapy was to maintain a fasting and premeal glucose concentration between 100 and 140 mg/dL. The doses of insulin were adjusted daily according to protocol. The mean amount is calculated among the different groups and compared. (NCT01378117)
Timeframe: during hospitalization, up to 10 days

Interventionunits/day (Mean)
Sitagliptin + SSI Prn11.5
Sitagliptin and Glargine + SSI28.2
Glargine and Lispro + SSI39.8

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Number of Deaths Among the Subjects in Different Groups

Mortality is defined as death occurring during admission among the participants. The number of deaths in each assigned group is calculated. (NCT01378117)
Timeframe: during hospitalization, up to 10 days

InterventionParticipants (Count of Participants)
Sitagliptin + SSI Prn0
Sitagliptin and Glargine + SSI0
Glargine and Lispro + SSI0

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Mean Length of Stay in Days in the Hospital Among Different Groups

The duration of stay in days in the hospital between the three groups is calculated and mean number of days is measured. (NCT01378117)
Timeframe: during hospitalization, up to 10 days

Interventiondays (Mean)
Sitagliptin + SSI Prn6.3
Sitagliptin and Glargine + SSI6.9
Glargine and Lispro + SSI6.3

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Percent Change From Baseline in Glucose Total Area Under the Concentration Curve 0 to 2 Hours (AUC 0-2 Hrs) for Meal Tolerance Test (MTT) at Week 8

Glucose total AUC 0-2 hours for MTT was measured at Baseline (Week 0) and at Week 8. After fasting for ≥10 hours, blood samples for glucose measurement were drawn at 0 minutes (at standard meal loading), 30 minutes, 60 minutes, 90 minutes, and 120 minutes. At Week 8, participants received study drug or placebo 30 minutes prior to consuming a standard meal. (NCT01405911)
Timeframe: Baseline (Week 0) and Week 8

InterventionPercent change (Least Squares Mean)
Placebo-2.42
Sitagliptin 25 mg-9.52
Sitagliptin 50 mg-11.49

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Percent Change From Baseline in Glucose Total Area Under the Concentration Curve 0 to 2 Hours (AUC 0-2 Hrs) for 75-gram Oral Glucose Tolerance Test (OGTT) at Week 7

Glucose total AUC 0-2 hours for 75 g OGTT was measured at Baseline (Week -1) and at Week 7. After fasting for ≥10 hours, blood samples for glucose measurement were drawn at 0 minutes (at 75 g glucose loading), 30 minutes, 60 minutes, 90 minutes, and 120 minutes. At Week 7, participants received study drug or placebo 30 minutes prior to loading 75 g glucose solution. (NCT01405911)
Timeframe: Baseline (Week -1) and Week 7

InterventionPercent change (Least Squares Mean)
Placebo-3.68
Sitagliptin 25 mg-21.38
Sitagliptin 50 mg-20.09

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Percentage of Participants Who Experienced One or More Adverse Events (AEs)

An AE is any untoward medical occurrence in a study participant administered a pharmaceutical product that does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product, whether or not related to the medicinal product. (NCT01405911)
Timeframe: Up to 10 weeks

InterventionPercentage of participants (Number)
Placebo30.9
Sitagliptin 25 mg34.1
Sitagliptin 50 mg41.0

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Percentage of Participants Who Discontinued Treatment Due to an Adverse Event (AE)

An AE is any untoward medical occurrence in a study participant administered a pharmaceutical product that does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product, whether or not related to the medicinal product. (NCT01405911)
Timeframe: Up to 8 weeks

InterventionPercentage of participants (Number)
Placebo0.0
Sitagliptin 25 mg0.0
Sitagliptin 50 mg0.0

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Pharmacokinetics: Maximum Observed Drug Concentration (Cmax) of Sitagliptin

(NCT01408888)
Timeframe: Predose and up to 24 hours postdose on Day 4, Day 6, and Day 13 of Treatment 2

Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
100 mg Sitagliptin (Day 4)417
100 mg Sitagliptin + 1.5 mg LY2189265 (Day 6)374
100 mg Sitagliptin + 1.5 mg LY2189265 (Day 13)318

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Pharmacokinetics: Time of Maximum Observed Drug Concentration (Tmax) of LY2189265

(NCT01408888)
Timeframe: Predose and up to 168 hours postdose on Day 1 of Treatment 1 and on Day 5 and Day 12 of Treatment 2

Interventionhours (Median)
1.5 mg LY2189265 (Day 1)72.0
100 mg Sitagliptin + 1.5 mg LY2189265 (Day 5)72.0
100 mg Sitagliptin + 1.5 mg LY2189265 (Day 12)59.8

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Pharmacokinetics: Time of Maximum Observed Drug Concentration (Tmax) of Sitagliptin

(NCT01408888)
Timeframe: Predose and up to 24 hours post dose on Day 4, Day 6, and Day 13 of Treatment 2

Interventionhours (Median)
100 mg Sitagliptin (Day 4)1.00
100 mg Sitagliptin + 1.5 mg LY2189265 (Day 6)2.00
100 mg Sitagliptin + 1.5 mg LY2189265 (Day 13)2.00

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Pharmacokinetics: Maximum Observed Drug Concentration (Cmax) of LY2189265

(NCT01408888)
Timeframe: Predose and up to 168 hours postdose on Day 1 of Treatment 1 and on Day 5 and Day 12 of Treatment 2

Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
1.5 mg LY2189265 (Day 1)52.9
100 mg Sitagliptin + 1.5 mg LY2189265 (Day 5)68.1
100 mg Sitagliptin + 1.5 mg LY2189265 (Day 12)101

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Pharmacokinetics: Area Under the Concentration Versus Time Curve (AUC) of Sitagliptin

Area under the sitagliptin pharmacokinetic (PK) concentration versus time curve (AUC [0-tau]) during one dosing interval (24 hours) is summarized. (NCT01408888)
Timeframe: Predose and up to 24 hours postdose on Day 4, Day 6, and Day 13 of Treatment 2

Interventionnanograms times hour/milliliter(ng*h/mL) (Geometric Mean)
100 mg Sitagliptin (Day 4)3210
100 mg Sitagliptin + 1.5 mg LY2189265 (Day 6)3240
100 mg Sitagliptin + 1.5 mg LY2189265 (Day 13)2970

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Pharmacokinetics: Area Under the Concentration Versus Time Curve (AUC) of LY2189265

Area under the LY2189265 pharmacokinetic (PK) concentration versus time curve (AUC [0-tau]) during one dosing interval (168 hours) is summarized. (NCT01408888)
Timeframe: Predose and up to 168 hours postdose on Day 1 of Treatment 1 and on Day 5 and Day 12 of Treatment 2

Interventionnanograms times hour/milliliter(ng*h/mL) (Geometric Mean)
1.5 mg LY2189265 (Day 1)6590
100 mg Sitagliptin + 1.5 mg LY2189265 (Day 5)8890
100 mg Sitagliptin + 1.5 mg LY2189265 (Day 12)13900

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The Effect of Enalaprilat (ACE Inhibition), Sitagliptin (DPP4 Inhibition), or the Combination on the Vasodilator Response (Forearm Blood Flow) to Substance P (SP) and Bradykinin (Group 1) or Glucagon Like Peptide-1 and Brain Naturetic Peptide (Group 2).

Forearm blood flow (FBF) was measured by strain gauge plethysmography at the completion of each dose of intra-arterial peptide. A dose response curve was therefore constructed for each vasoactive peptide substrate. The effect of sitagliptin (DPP4 inhibition) vs. placebo and enalaprilat (ACE inhibition) vs. vehicle on the forearm blood flow response to each peptide could then be determined. (NCT01413542)
Timeframe: 60 minutes post-placebo or sitagliptin (DPP4 inhibition) and over last 2 minutes of each 5 min infusion per peptide dose (30 min washout between peptides); sequence repeated with enalaprilat (ACE inhibition) or vehicle

,
Interventionestimate of difference(ml/min/100ml FBF) (Mean)
Effect ACE inhibition on FBF response to Peptide 1Effect DPP4 inhibition on FBF Response to Peptide1Effect ACE/DPP4 inhibit on FBF response Peptide 1Effect DPP4/ACEinhib vs. ACEinhib (FBF to Pep1)Effect DPP4/ACEinhib vs. DPP4inhib (FBF to Pep1)Effect ACE inhibition on FBF response to Peptide 2Effect DPP4 inhibition on FBF response to Peptide2Effect ACE/DPP4 inhibition on Peptide 2 FBFEffect DPP4/ACEinhib vs. ACEinhib (FBF to Pep2)Effect DPP4/ACEinhib vs. DPP4inhib (FBF to Pep2)
Group 16.50.25.9-0.65.70.80.10.6-0.30.4
Group 2NA-5.0NANANANA-3.2NANANA

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Assess Effect of ACE and/or DPP4 Inhibition on Heart Rate Response to Substance P (SP)

(NCT01413542)
Timeframe: Heart rate was measured every 5 minutes throughout the study day (and thus during each dose of peptide infusion)

Interventionbeats per minute (Mean)
Change in Pulse after SP during PlaceboChange in Pulse after SP w/ACE inhibitionChange in Pulse after SP w/DPP4inhibitionPulse change after SP w/ACE+DPP4inhibition
Group 1-1.82.550.454.55

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Assess Tissue Type Plasminogen Activator (tPA) Release

Following measurement of FBF, samples will be obtained to determine the effect of ACE inhibition and/or DPP4 inhibition on tPA release in response to bradykinin and substance P (SP) (group 1) (NCT01413542)
Timeframe: Blood for analysis of tPA release was obtained 60 minutes after sitagliptin (DPP4 inhibition) vs. placebo and after each assessment of FBF (see primary outcome measure)

,
Interventionestimate of difference (ng/min/100mL) (Number)
Effect ACE inhibition on bradykinin tPA releaseEffect of DPP4 inhibition on bradykinintPA releaseEffect of ACE/DPP4 inhibitio on bradykinin tPAeffect ace/dpp4 vs. aceinhibi on bradykinin tpaeffect ace/dpp4 vs. dpp4inhib on bradykinin tpaEffect of ACE inhibition on SP tPA releaseEffect of DPP4 inhibition on SP tPAEffect of ACE+DPP4 inhibition on SP tPAeffect ace/dpp4 vs. aceinhibi on SP tpaeffect ace/dpp4 vs. dpp4inhibi on SP tpa
Group 1 (Females)145.512.9132.1-13.4119.343.9-29.03.8-40.132.8
Group 1 (Males)118.61.690.9-27.889.3-15.3-25.80.816.126.6

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Effect of Treatment (ACE or DPP4 Inhibition, or Combined) on Norepinephrine (NE) Release (Arterial Venous Gradient) in Response to Substance P (SP)

(NCT01413542)
Timeframe: Blood for analysis of norepinephrine (NE) release was obtained 60 minutes after sitagliptin (DPP4 inhibition) vs. placebo and after each assessment of FBF (see primary outcome measure)

Interventionpg/mL (Mean)
Change NE AV Gradient with SP after placeboChange NE AV Gradient with SP after ACEinhibitionChange NE AV Gradient with SP after DPP4inhibitionChange NE AV with SP after ACE+DPPinhibition
Group 1-43.18-52.18-37.2723.45

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Effect of Treatment (DPP4 Inhibition vs. Placebo) on Venous GLP-1 Levels in Response to Arterial GLP-1 Infusion

(NCT01413542)
Timeframe: Blood for analysis of GLP-1 levels was obtained one hour after sitagliptin (DPP4 inhibition) vs. placebo administration and after each dose of GLP-1

Interventionpmol/L (Mean)
Venous GLP-1 levels 1 hour after placeboVenous GLP-1 Levels after Max Dose GLP-1 (Placebo)Venous GLP-1 levels 1 hour after DPP4 inhibitionVenous GLP-1 levels Max Dose GLP-1 (DPP4inhibiton)
Group 25.1315.445.3930.63

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Differences of DPP-4 Activity After Sitagliptin Treatment Between Responder and Non-responder Groups

The DPP-4 activity was measured at baseline and 0, 15, 30, 45 and 60 min during the meal tolerance test. Second measurement of DPP-4 activity was measured with MTT after taking sitagliptin 100 mg 1 hour before the test. Plasma DPP-4 activity during meal tolerance test is expressed as percentage activity relative to baseline. DPP-4 activity % was calculated using the following formula : (DPP-4 activity at time t / Baseline DPP-4 activity) × 100. (NCT01449747)
Timeframe: 0, 15, 30, 45, 60 min post-dose

,
Interventionpercentage of DPP4 activity (Mean)
baselineSitagliptin 0 minSitagliptin 15 minSitagliptin 30 minSitagliptin 45 minSitagliptin 60 min
Non-responder10067.267.367.759.658.5
Responder10040.539.238.733.544.3

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Change in AUC of Active GLP-1, Total GLP-1 and Total GIP Between Before and After Sitagliptin Treatment

Plasma concentrations of active GLP-1, total GLP-1 and total GIP were measured at 0, 15, 30, 45, 60, 90, 120 and 180 min during the meal tolerance test. Second measurements were measured with MTT after taking sitagliptin 100 mg 1 hour before the test. Comparisons were made using Area under the curve (AUC) values and incremental area under the curve (ΔAUC) of active GLP-1, total GLP-1 and total GIP before and after the addition of sitagliptin. (NCT01449747)
Timeframe: 0, 15, 30, 45, 60, 90, 120, 180 min pre and post-dose

,
Interventionpmol*min/L (Mean)
baseline AUC active GLP-1baseline AUC total GLP-1baseline AUC total GIPpost-dose AUC active GLP-1post-dose AUC total GLP-1post-dose AUC total GIPΔAUC active GLP-1ΔAUC total GLP-1ΔAUC total GIP
Non-responder2181.75766.510216.73898.54794.58784.61716.8-972.0-1432.1
Responder1578.23680.27575.63535.13373.65929.41956.8-306.7-1646.2

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Plasma Concentration of Total Glucose-dependent Insulinotropic Polypeptide (GIP) Before and After Sitagliptin Treatment

Plasma concentrations of total GIP were measured at 0, 15, 30, 45, 60, 90, 120 and 180 min during the meal tolerance test. Second measurement of total GIP were measured with MTT after taking sitagliptin 100 mg 1 hour before the test. (NCT01449747)
Timeframe: 0, 15, 30, 45, 60, 90, 120, 180 min pre and post-dose

,
Interventionpmol/L (Mean)
baseline 0 minbaseline 15 minbaseline 30 minbaseline 45 minbaseline 60 minbaseline 90 minbaseline 120 minbaseline 180 minpost-dose 0 minpost-dose 15 minpost-dose 30 minpost-dose 45 minpost-dose 60 minpost-dose 90 minpost-dose 120 minpost-dose 180 min
Non-responder13.842.3109.6109.683.066.361.739.910.534.290.877.661.544.243.832.8
Responder12.340.360.254.152.044.739.030.010.326.333.138.537.738.235.024.7

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Plasma Concentration of Active Glucagon-like Peptide 1 (GLP-1) Before and After Sitagliptin Treatment

Plasma concentrations of active GLP-1 were measured at 0, 15, 30, 45, 60, 90, 120 and 180 min during the meal tolerance test (MTT). Second measurement of active GLP-1 were measured with MTT after taking sitagliptin 100 mg 1 hour before the test. (NCT01449747)
Timeframe: 0, 15, 30, 45, 60, 90, 120, 180 min pre and post-dose

,
Interventionpmol/L (Mean)
baseline 0 minbaseline 15 minbaseline 30 minbaseline 45 minbaseline 60 minbaseline 90 minbaseline 120 minbaseline 180 minpost-dose 0 minpost-dose 15 minpost-dose 30 minpost-dose 45 minpost-dose 60 minpost-dose 90 minpost-dose 120 minpost-dose 180 min
Non-responder7.010.615.714.713.710.611.312.613.624.028.422.421.719.322.020.5
Responder6.114.114.39.38.47.67.47.110.526.034.327.122.816.516.413.5

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Plasma Concentration of Total GLP-1 Before and After Sitagliptin Treatment

Plasma concentrations of total GLP-1 were measured at 0, 15, 30, 45, 60, 90, 120 and 180 min during the meal tolerance test. Second measurement of total GLP-1 were measured with MTT after taking sitagliptin 100 mg 1 hour before the test. (NCT01449747)
Timeframe: 0, 15, 30, 45, 60, 90, 120, 180 min pre and post-dose

,
Interventionpmol/L (Mean)
baseline 0 minbaseline 15 minbaseline 30 minbaseline 45 minbaseline 60 minbaseline 90 minbaseline 120 minbaseline 180 minpost-dose 0 minpost-dose 15 minpost-dose 30 minpost-dose 45 minpost-dose 60 minpost-dose 90 minpost-dose 120 minpost-dose 180 min
Non-responder25.630.536.230.931.831.831.334.523.028.426.329.226.526.226.726.0
Responder15.620.422.425.521.719.219.919.316.420.620.618.918.618.118.718.2

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Change From Baseline in Daily Insulin Dose at Week 24

Change in daily insulin dose following 24 weeks of therapy (i.e., daily insulin dose at Week 24 minus daily insulin dose at baseline) (NCT01462266)
Timeframe: Baseline and Week 24

InterventionInternational Units (IU) (Least Squares Mean)
Sitagliptin19.0
Placebo23.8

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24

Change in FPG (before breakfast) following 24 weeks of therapy (i.e., FPG at Week 24 minus FPG at baseline) (NCT01462266)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-55.5
Placebo-44.8

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Change From Baseline in Hemoglobin A1c (A1C) at Week 24

A1C is measured as the percentage of glycosylated hemoglobin. Change in A1C following 24 weeks of therapy (i.e., A1C at Week 24 minus A1C at baseline) (NCT01462266)
Timeframe: Baseline and Week 24

InterventionPercent of total hemoglobin (Least Squares Mean)
Sitagliptin-1.31
Placebo-0.87

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Percent of Participants Achieving Fasting Glucose Target at Any Time During the Study

The fasting glucose target was defined as 3 consecutive days with a fingerstick glucose of 72 to 100 mg/dL (4.0 - 5.6 mmol/L). (NCT01462266)
Timeframe: Up to 24 weeks

InterventionPercentage of participants (Number)
Sitagliptin77.4
Placebo74.1

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Time to Achieve the Fasting Glucose Target

Fasting glucose target 3 consecutive days with a fingerstick glucose of 72 to 100 mg/dL (4.0 - 5.6 mmol/L). This analysis was the Kaplan-Meier estimated 50th percentile of time (days) to first attainment of target. (NCT01462266)
Timeframe: Up to 24 weeks

InterventionDays to first attainment of target (Median)
Sitagliptin78
Placebo90

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Number of Hypoglycemic Events (HAE) Episodes Per Participant

A hypoglycemic event (HAE) was identified by characteristic symptoms or blood glucose levels. Median number of events per participant was reported (NCT01475461)
Timeframe: Baseline (Day 1) up to Week 14

Interventionevents per participant (Median)
Metformin 500 mg0
Placebo0
PF-04937319 3 mg0
PF-04937319 20 mg0
PF-04937319 50 mg0
PF-04937319 100 mg0
Sitagliptin 100 mg0

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Number of Participants With Increase/Decrease From Baseline Vital Signs Data

Participants who met the criteria for increase or decrease in vital signs data were reported. Criteria for increase or decrease from baseline vital signs data: sitting systolic blood pressure (BP) of >=30 millimeter of mercury (mmHg); sitting diastolic BP of >=20 mmHg and pulse rate was based on investigator's discretion. (NCT01475461)
Timeframe: Baseline (Day 1) up to Week 14

,,,,,
Interventionparticipants (Number)
Increase in systolic BP (>=30 mmHg)Increase in diastolic BP (>=20 mmHg)Decrease in systolic BP (>=30 mmHg)Decrease in diastolic BP (>=20 mmHg)
PF-04937319 100 mg3423
PF-04937319 20 mg2016
PF-04937319 3 mg2421
PF-04937319 50 mg1111
Placebo1112
Sitagliptin2211

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Percentage of Participants With at Least 1 Hypoglycemic Events (HAE) Episode

A hypoglycemic event (HAE) was identified by characteristic symptoms or blood glucose levels. HAE is defined as 1 of the given definitions: Characteristic symptoms of HAE with no home glucose monitoring performed where clinical picture included prompt resolution with food intake, subcutaneous glucagon, or intravenous glucose; or characteristic symptoms of HAE with home glucose monitoring measurement =< 70 milligram per deciliter (mg/dL) using ACCU-CHEK plasma-referenced home glucometers or =<74 mg/dL using International Federation of Clinical Chemistry (IFCC) referenced ACCU-CHEK or central laboratory glucometers; or any laboratory glucose value, meeting the following criterion with or without accompanying symptoms: =<49 mg/dL using ACCU-CHEK plasma-referenced home glucometers or =<53 mg/dL using IFCC referenced ACCU-CHEK or central laboratory glucometers. (NCT01475461)
Timeframe: Baseline (Day 1) up to Week 14

Interventionpercentage of participants (Number)
Metformin 500 mg0
Placebo0
PF-04937319 3 mg0
PF-04937319 20 mg1
PF-04937319 50 mg0
PF-04937319 100 mg2
Sitagliptin 100 mg1

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Change From Baseline in Body Weight at Week 2, 4, 8, 12 and 14

(NCT01475461)
Timeframe: Baseline (Day 1), Week 2, 4, 8 , 12 , 14

,,,,,
Interventionkilogram (kg) (Mean)
Baseline (n=55, 55, 50, 56, 54, 55)Change at Week 2 (n=54, 55, 49, 56, 53, 55)Change at Week 4 (n=51, 55, 49, 55, 53, 53)Change at Week 8 (n=49, 53, 45, 52, 50, 52)Change at Week 12 (n=47, 52, 45, 52, 50, 53)Change at Week 14 (n=44, 52, 44, 52, 50, 53)
PF-04937319 100 mg91.239-0.053-0.374-0.475-0.623-0.916
PF-04937319 20 mg88.371-0.052-0.192-0.510-0.455-0.613
PF-04937319 3 mg87.8650.4350.214-0.003-0.1420.011
PF-04937319 50 mg88.066-0.283-0.203-0.270-0.352-0.492
Placebo86.446-0.239-0.704-0.823-0.804-0.588
Sitagliptin 100 mg87.025-0.384-0.353-0.702-0.917-1.172

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Percentage of Participants Achieving Less Than 6.5 Percent and Less Than 7 Percent Glycosylated Hemoglobin (HbA1c) Levels at Week 12

HbA1c is a form of hemoglobin which is measured primarily to identify the average glycemic control over prolonged periods of time. The normal range for the HbA1c test, was identified as <6.5 percent by the study-specific central laboratory used and data are presented in categories of <6.5 percent and <7 percent. (NCT01475461)
Timeframe: Week 12

,,,,,
Interventionpercentage of participants (Number)
<6.5 percent<7 percent
PF-04937319 100 mg17.639.2
PF-04937319 20 mg19.142.6
PF-04937319 3 mg9.426.4
PF-04937319 50 mg15.430.8
Placebo12.522.9
Sitagliptin32.156.6

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Change From Baseline in Fasting Plasma Glucose at Week 1, 2, 4, 8, 12 and 14

(NCT01475461)
Timeframe: Baseline (Day 1), Week 1, 2, 4, 8, 12, 14

,,,,,
Interventionmilligram per deciliter (mg/dL) (Mean)
Baseline (n=56, 56, 52, 56, 55, 55)Change at Week 2 (n=54, 56, 50, 56, 54, 55)Change at Week 4 (n=52, 56, 51, 55, 54, 53)Change at Week 8 (n=50, 54, 47, 52, 51, 52)Change at Week 12 (n=48, 53, 47, 52, 51, 53)Change at Week 14 (n=45, 53, 46, 52, 51, 53)
PF-04937319 100 mg164.8-10.8-9.6-6.53.510.2
PF-04937319 20 mg155.1-3.2-0.2-2.5-3.8-3.1
PF-04937319 3 mg159.80.7-0.30.7-2.5-3.5
PF-04937319 50 mg166.1-6.8-8.3-15.2-10.8-1.0
Placebo168.3-5.2-1.8-3.1-7.5-5.9
Sitagliptin160.7-13.6-19.3-15.4-12.9-2.6

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Number of Participants With Abnormal Laboratory Values

Hemoglobin,hematocrit,red blood cells(RBC) count:less than [<]0.8*lower limit of normal[LLN],platelets:<0.5*LLN/greater than [>]1.75*upper limit of normal [ULN],white blood cells(WBC):<0.6*LLN or >1.5*ULN,lymphocytes,total neutrophils:<0.8*LLN or >1.2*ULN, basophils,eosinophil,monocytes:>1.2*ULN;aspartate aminotransferase,alanine aminotransferase, alkaline phosphatase:>0.3*ULN,total protein,albumin:<0.8*LLN or >1.2*ULN;total bilirubin,direct bilirubin,indirect bilirubin:>1.5*ULN;triglycerides,cholesterol:>1.3*ULN, HDL:<0.8*LLN, LDL:>1.2*ULN,blood urea nitrogen,creatinine:>1.3*ULN,uric acid:>1.2*ULN;sodium: <0.95*LLN or >1.05*ULN,potassium,chloride,calcium,bicarbonate:<0.9*LLN or >1.1*ULN;creatine kinase:>2.0*ULN;glucose:<0.6*LLN or >1.5*ULN,urine WBC and RBC:>= 20/High Power Field [HPF]),urine epithelial cells (>=1 HPF),urine bacteria >20 high-powered field;qualitative urine glucose,urine blood to Hgb ratio (>=1);urine(protein,nitrite,mucus,leukocyte >=1 in urine dipstick test). (NCT01475461)
Timeframe: Baseline (Day 1) up to Week 14

Interventionparticipants (Number)
Placebo46
PF-04937319 3 mg49
PF-04937319 20 mg45
PF-04937319 50 mg46
PF-04937319 100 mg53
Sitagliptin 100 mg43

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Change From Baseline in Glycosylated Hemoglobin (HbA1C) at Week 12

HbA1c is a form of hemoglobin which is measured primarily to identify the average glycemic control over prolonged periods of time. The normal range for the HbA1c test, was identified as less than (<) 6.5 percent (%) by the study-specific central laboratory used. Change from baseline in percentage of HbA1c in participants were reported. (NCT01475461)
Timeframe: Baseline (Day 1), Week 12

,,,,,
Interventionpercentage of hemoglobin (Mean)
Baseline (n=50,55,48,55,53,53)Change at Week 12 (n=46,52,45,52,50,53)
PF-04937319 100 mg8.31-0.80
PF-04937319 20 mg7.80-0.53
PF-04937319 3 mg8.00-0.33
PF-04937319 50 mg8.15-0.59
Placebo8.01-0.42
Sitagliptin7.89-0.79

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Change From Baseline in Glycosylated Hemoglobin (HbA1C) at Week 2, 4 and 8

HbA1c is a form of hemoglobin which is measured primarily to identify the average glycemic control over prolonged periods of time. The normal range for the HbA1c test, was identified as <6.5 percent by the study-specific central laboratory used. Change from baseline in percentage of HbA1c in participants were reported. (NCT01475461)
Timeframe: Baseline(Day 1), Week 2, 4, 8

,,,,,
Interventionpercentage of hemoglobin (Mean)
Change at Week 4 (n= 50, 55, 48, 55, 53, 53)Change at Week 8 (n=48, 53, 45, 52, 50, 51)
PF-04937319 100 mg-0.50-0.86
PF-04937319 20 mg-0.32-0.46
PF-04937319 3 mg-0.24-0.32
PF-04937319 50 mg-0.35-0.50
Placebo-0.20-0.36
Sitagliptin-0.52-0.77

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Number of Participants With Increase From Baseline Electrocardiogram (ECG)Data

Criteria for increase from baseline data: PR interval (percent change of greater than or equal to [>=] 25/50% [if baseline>200 then percent change of >25% counts; if baseline <=200 then percent change of >50% counts]; QRS complex (percent change of >=50%); QT Fridericia's correction (QTcF) interval (change of >=30 to <60 millisecond [msec], and change of >=60 msec). (NCT01475461)
Timeframe: Baseline (Day 1) up to Week 14

,,,,,
Interventionparticipants (Number)
PR interval: Percent change of >=25/50%QRS interval: Percent change of >=50%QTcF interval: Change of >=30 to <60 msecQTcF interval: Change of >=60 msec
PF-04937319 100 mg1132
PF-04937319 20 mg0130
PF-04937319 3 mg1150
PF-04937319 50 mg0131
Placebo0071
Sitagliptin2170

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Number of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs)

An AE was any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent are events between first dose of study drug and up to 14 days after last dose that were absent before treatment or that worsened relative to pretreatment state. AEs included both serious and non-serious adverse events. (NCT01475461)
Timeframe: Baseline (Day 1) up to 14 days after last dose (up to 101 days)

,,,,,,
Interventionparticipants (Number)
AEsSAEs
Metformin 500 mg370
PF-04937319 100 mg241
PF-04937319 20 mg191
PF-04937319 3 mg190
PF-04937319 50 mg160
Placebo191
Sitagliptin 100 mg180

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Percent Change From Baseline in Very Low-density Lipoprotein Cholesterol (VLDL-C) at Week 16

Percent change from baseline was calculated as the Week 16 value minus the Week 0 value, divided by the Week 0 value ×100%. (NCT01477853)
Timeframe: Baseline and Week 16

InterventionPercent change (Mean)
Sitagliptin/Sitagliptin + Atorvastatin-15.5
Atorvastatin/Atorvastatin + Glimepiride-28.6
Sitagliptin + Atorvastatin/Sitagliptin + Atorvastatin-10.4

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Percent Change From Baseline in High Density Lipoprotein Cholesterol (HDL-C) at Week 16

Percent change from baseline was calculated as the Week 16 value minus the Week 0 value, divided by the Week 0 value ×100%. (NCT01477853)
Timeframe: Baseline and Week 16

InterventionPercent change (Mean)
Sitagliptin/Sitagliptin + Atorvastatin-0.3
Atorvastatin/Atorvastatin + Glimepiride-5.8
Sitagliptin + Atorvastatin/Sitagliptin + Atorvastatin1.5

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 16

Change from baseline reflects the Week 16 value minus the Week 0 value. (NCT01477853)
Timeframe: Baseline and Week 16

Interventionmg/dL (Mean)
Sitagliptin/Sitagliptin + Atorvastatin-15.7
Atorvastatin/Atorvastatin + Glimepiride22.7
Sitagliptin + Atorvastatin/Sitagliptin + Atorvastatin-26.0

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Change From Baseline in Hemoglobin A1C (A1C) at Week 16

A1C is measured as percent. Thus, this change from baseline reflects the Week 16 A1C percent minus the Week 0 A1C percent. (NCT01477853)
Timeframe: Baseline and Week 16

InterventionPercent (Mean)
Sitagliptin/Sitagliptin + Atorvastatin-1.17
Atorvastatin/Atorvastatin + Glimepiride0.04
Sitagliptin + Atorvastatin/Sitagliptin + Atorvastatin-1.01

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Number of Participants Who Discontinued Study Drug Due to an Adverse Event

An adverse event is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the investigational product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which is temporally associated with the use of the investigational product, is also an adverse event. Data presented exclude data following the initiation of glycemic rescue therapy. (NCT01477853)
Timeframe: Up to 54 weeks

InterventionParticipants (Number)
Sitagliptin/Sitagliptin + Atorvastatin1
Atorvastatin/Atorvastatin + Glimepiride2
Sitagliptin + Atorvastatin/Sitagliptin + Atorvastatin2

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Percent Change From Baseline in Apolipoprotein B (Apo B) at Week 16

Percent change from baseline was calculated as the Week 16 value minus the Week 0 value, divided by the Week 0 value ×100%. (NCT01477853)
Timeframe: Baseline and Week 16

InterventionPercent change (Mean)
Sitagliptin/Sitagliptin + Atorvastatin-4.8
Atorvastatin/Atorvastatin + Glimepiride-32.9
Sitagliptin + Atorvastatin/Sitagliptin + Atorvastatin-29.0

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Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C) at Week 16

Percent change from baseline was calculated as the Week 16 value minus the Week 0 value, divided by the Week 0 value ×100%. (NCT01477853)
Timeframe: Baseline and Week 16

InterventionPercent change (Mean)
Sitagliptin/Sitagliptin + Atorvastatin4.9
Atorvastatin/Atorvastatin + Glimepiride-35.7
Sitagliptin + Atorvastatin/Sitagliptin + Atorvastatin-38.7

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Percent Change From Baseline in Non-high Density Lipoprotein Cholesterol (Non-HDL-C) at Week 16

Percent change from baseline was calculated as the Week 16 value minus the Week 0 value, divided by the Week 0 value ×100%. (NCT01477853)
Timeframe: Baseline and Week 16

InterventionPercent change (Mean)
Sitagliptin/Sitagliptin + Atorvastatin-1.0
Atorvastatin/Atorvastatin + Glimepiride-34.4
Sitagliptin + Atorvastatin/Sitagliptin + Atorvastatin-34.6

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Percent Change From Baseline in Total Cholesterol at Week 16

Percent change from baseline was calculated as the Week 16 value minus the Week 0 value, divided by the Week 0 value ×100%. (NCT01477853)
Timeframe: Baseline and Week 16

InterventionPercent change (Mean)
Sitagliptin/Sitagliptin + Atorvastatin-1.7
Atorvastatin/Atorvastatin + Glimepiride-28.3
Sitagliptin + Atorvastatin/Sitagliptin + Atorvastatin-25.7

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Percent Change From Baseline in Triglycerides at Week 16

Percent change from baseline was calculated as the Week 16 value minus the Week 0 value, divided by the Week 0 value ×100%. (NCT01477853)
Timeframe: Baseline and Week 16

InterventionPercent change (Mean)
Sitagliptin/Sitagliptin + Atorvastatin-9.9
Atorvastatin/Atorvastatin + Glimepiride-28.7
Sitagliptin + Atorvastatin/Sitagliptin + Atorvastatin-10.5

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Number of Participants Who Experienced at Least One Adverse Event

An adverse event is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the investigational product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which is temporally associated with the use of the investigational product, is also an adverse event. Data presented exclude data following the initiation of glycemic rescue therapy. (NCT01477853)
Timeframe: Up to 56 weeks (including 2-week follow-up)

InterventionParticipants (Number)
Sitagliptin/Sitagliptin + Atorvastatin10
Atorvastatin/Atorvastatin + Glimepiride13
Sitagliptin + Atorvastatin/Sitagliptin + Atorvastatin13

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Skeletal Maturation at Week 20 - Females

Skeletal Maturation = (Change from Baseline in bone age)/(Change from Baseline in chronologic age). Bone age was determined from an X-ray of left hand and wrist. (NCT01485614)
Timeframe: Week 20

InterventionRatio (Mean)
Sitagliptin0.6
Placebo/Metformin0.4
Metformin1.7
Placebo/Sitagliptin-0.8

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Skeletal Maturation at Week 20 - Males

Skeletal Maturation = (Change from Baseline in bone age)/(Change from Baseline in chronologic age). Bone age was determined from X-ray of left hand and wrist. (NCT01485614)
Timeframe: Week 20

InterventionRatio (Mean)
Sitagliptin1.6
Placebo/Metformin1.2
Metformin0.4
Placebo/Sitagliptin2.4

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Skeletal Maturation at Week 54 - Females

Skeletal Maturation = (Change from Baseline in bone age)/(Change from Baseline in chronologic age). Bone age was determined from X-ray of left hand and wrist. All participants in the Placebo/Sitagliptin arm were missing baseline or Week 54 measurements. (NCT01485614)
Timeframe: Week 54

InterventionRatio (Mean)
Sitagliptin1.3
Placebo/Metformin1.0
Metformin1.3

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Skeletal Maturation at Week 54 - Males

Skeletal Maturation = (Change from Baseline in bone age)/(Change from Baseline in chronologic age). Bone age was determined from X-ray of left hand and wrist. All participants in the Metformin and Placebo/Sitagliptin arms were missing baseline or Week 54 measurements. (NCT01485614)
Timeframe: Week 54

InterventionRatio (Mean)
Sitagliptin1.3
Placebo/Metformin1.3

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Participants With Worsening in Dental Status at Week 20

Participants were evaluated with a visual oral exam; a subset had dental photographs. Teeth worsening was defined as worsening of tooth fracture, tooth discoloration, or enamel defect as determined by an independent reviewer. Worsening in these categories was a change in dental defect assessments made by comparing Week 20 dental assessments versus baseline dental assessments. (NCT01485614)
Timeframe: Week 20

,,,
InterventionParticipants (Count of Participants)
1. With ≥1 tooth with worsening in any category2. With ≥1 tooth with worsening fracture3. With ≥1 tooth with worsening discoloration4. With ≥1 tooth with worsening enamel defect
Metformin1001
Placebo/Metformin255234
Placebo/Sitagliptin0000
Sitagliptin325297

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Participants With Worsening in Dental Status at Week 54

Participants were evaluated with a visual oral exam; a subset had dental photographs. Teeth worsening was defined as worsening of tooth fracture, tooth discoloration, or enamel defect as determined by an independent reviewer. Worsening in these categories was a change in dental defect assessments made by comparing Week 54 dental assessments versus baseline dental assessments. (NCT01485614)
Timeframe: Week 54

,,,
InterventionParticipants (Count of Participants)
1. With ≥1 tooth with worsening in any category2. With ≥1 tooth with worsening fracture3. With ≥1 tooth with worsening discoloration4. With ≥1 with worsening enamel defect
Metformin2121
Placebo/Metformin50154813
Placebo/Sitagliptin0000
Sitagliptin49134513

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Change From Baseline in C-peptide 3-Hour AUC at Week 54

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. This change from baseline was Week 54 C-peptide 3-hour AUC minus the Week 0 C-peptide 3-hour AUC. (NCT01485614)
Timeframe: Baseline and Week 54 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

Interventionng*hr/ml (Mean)
Sitagliptin-0.1
Placebo/Metformin-6.1
Metformin1.7
Placebo/Sitagliptin-8.9

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Change From Baseline in C-peptide 3-Hour AUC at Week 20

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. This change from baseline was Week 20 C-peptide 3-hour AUC minus the Week 0 C-peptide 3-hour AUC. (NCT01485614)
Timeframe: Baseline and Week 20 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

Interventionng*hr/mL (Mean)
Sitagliptin-1.8
Placebo/Metformin-0.1
Metformin5.9
Placebo/Sitagliptin-6.4

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Change From Baseline in Bone-Specific Alkaline Phosphatase at Week 54 - Males

Bone-specific alkaline phosphatase is a biochemical marker of bone turnover. This change from baseline was Week 54 bone-specific alkaline phosphatase minus the Week 0 bone-specific alkaline phosphatase. (NCT01485614)
Timeframe: Baseline and Week 54

Interventionμg/L (Mean)
Sitagliptin-16.2
Placebo/Metformin-15.0
Metformin-1.3
Placebo/Sitagliptin-15.3

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Change From Baseline in Bone-Specific Alkaline Phosphatase at Week 54 - Females

Bone-specific alkaline phosphatase is a biochemical marker of bone turnover. This change from baseline was Week 54 bone-specific alkaline phosphatase minus the Week 0 bone-specific alkaline phosphatase. (NCT01485614)
Timeframe: Baseline and Week 54

Interventionμg/L (Mean)
Sitagliptin-20.0
Placebo/Metformin-13.5
Metformin-14.9
Placebo/Sitagliptin-6.9

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Change From Baseline in Bone-Specific Alkaline Phosphatase at Week 20 - Males

Bone-specific alkaline phosphatase is a biochemical marker of bone turnover. This change from baseline was Week 20 bone-specific alkaline phosphatase minus the Week 0 bone-specific alkaline phosphatase. (NCT01485614)
Timeframe: Baseline and Week 20

Interventionμg/L (Mean)
Sitagliptin-2.2
Placebo/Metformin0.1
Metformin-7.1
Placebo/Sitagliptin4.7

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Percentage of Participants Initiating Glycemic Rescue Therapy by Week 54

The percentage of participants who initiated glycemic rescue therapy prior to Week 54 was reported. (NCT01485614)
Timeframe: Up to Week 54

InterventionPercentage of participants (Number)
Sitagliptin35.8
Placebo/Metformin28.9
Metformin11.1
Placebo/Sitagliptin80.0

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Change From Baseline in Bone-Specific Alkaline Phosphatase at Week 20 - Females

Bone-specific alkaline phosphatase is a biochemical marker of bone turnover. This change from baseline was Week 20 bone-specific alkaline phosphatase minus the Week 0 bone-specific alkaline phosphatase. (NCT01485614)
Timeframe: Baseline and Week 20

Interventionμg/L (Mean)
Sitagliptin-6.0
Placebo/Metformin-4.2
Metformin-9.7
Placebo/Sitagliptin10.7

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Change From Baseline in Body Mass Index (BMI) at Week 20

This change from baseline was Week 20 BMI minus the Week 0 BMI. (NCT01485614)
Timeframe: Baseline and Week 20

Interventionkg/m^2 (Mean)
Sitagliptin0.0
Placebo/Metformin-0.7
Metformin-0.8
Placebo/Sitagliptin-1.7

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Change From Baseline in A1C at Week 54

A1C is a blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. This change from baseline reflects the Week 54 A1C minus the Week 0 A1C. (NCT01485614)
Timeframe: Baseline and Week 54

InterventionPercentage (Mean)
Sitagliptin-0.19
Placebo/Metformin-0.90
Metformin-0.70
Placebo/Sitagliptin-0.50

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Change From Baseline In A1C at Week 20 (Analysis of Selected Arms: Sitagliptin and Placebo (Pooled))

Glycated hemoglobin (A1C) is a blood marker used to report average blood glucose levels over time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. Mean change from baseline was estimated as the Week 20 A1C minus the Week 0 A1C from a longitudinal data analysis (LDA) model. The placebo arm in this comparison is a pooling of the Placebo/Metformin and Placebo/Sitagliptin arms. The Statistical Analysis Plan (SAP) did not specify for the Metformin arm to be included in statistical comparisons, so results for this arm are provided separately. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionPercentage (Least Squares Mean)
Sitagliptin-0.01
Placebo (Pooled)0.18

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Change From Baseline in 2-Hour Post-meal Glucose (PMG) at Week 20

PMG endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. This change from baseline was Week 20 2-hour PMG minus the Week 0 2-hour PMG. (NCT01485614)
Timeframe: Baseline and Week 20

Interventionmg/dL (Mean)
Sitagliptin-2.9
Placebo/Metformin2.1
Metformin-6.8
Placebo/Sitagliptin63.5

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Change From Baseline in 2-hour PMG at Week 54

PMG endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. This change from baseline was Week 54 2-hour PMG minus the Week 0 2-hour PMG. (NCT01485614)
Timeframe: Baseline and Week 54

Interventionmg/dL (Mean)
Sitagliptin-1.7
Placebo/Metformin-16.8
Metformin-39.7
Placebo/Sitagliptin-28.0

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Change From Baseline in 2-Hour Incremental PMG at Week 54

2-Hour incremental PMG = Glucose at 120 minutes - glucose at 0 minutes. PMG endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. This change from baseline was Week 54 2-hour incremental PMG minus the Week 0 2-hour incremental PMG. (NCT01485614)
Timeframe: Baseline and Week 54

Interventionmg/dL (Mean)
Sitagliptin-0.6
Placebo/Metformin-26.6
Metformin-31.3
Placebo/Sitagliptin-32.0

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Change From Baseline in 2-hour Incremental PMG at Week 20

2-Hour incremental PMG = Glucose at 120 minutes - glucose at 0 minutes. PMG endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. This change from baseline was Week 20 2-hour incremental PMG minus the Week 0 2-hour incremental PMG. (NCT01485614)
Timeframe: Baseline and Week 20

Interventionmg/dL (Mean)
Sitagliptin1.5
Placebo/Metformin0.7
Metformin0.8
Placebo/Sitagliptin12.5

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Baseline Glycated Hemoglobin (A1C) for the Placebo (Pooled) Arm

A1C is a blood marker used to report average blood glucose levels over prolonged periods of time. A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. The Placebo (pooled) arm was a pooling of the Placebo/Metformin and Placebo/Sitagliptin arms for analysis purposes. (NCT01485614)
Timeframe: Baseline

InterventionPercentage (Mean)
Placebo (Pooled)7.58

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Baseline Fasting Plasma Glucose (FPG) for the Placebo (Pooled) Arm

Blood glucose was measured on a fasting basis. The Placebo (pooled) arm was a pooling of the Placebo/Metformin and Placebo/Sitagliptin arms for analysis purposes. (NCT01485614)
Timeframe: Baseline

Interventionmg/dL (Mean)
Placebo (Pooled)138.8

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Change From Baseline in Insulin 3-Hour AUC/ Glucose 3-Hour AUC Ratio at Week 20

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. This change from baseline was Week 20 insulin total AUC/glucose total AUC ratio minus the Week 0 insulin total AUC/glucose total AUC ratio. (NCT01485614)
Timeframe: Baseline and Week 20 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

Intervention[µIU*hr/mL]/[mg*hr/dL] (Mean)
Sitagliptin0.0
Placebo/Metformin-0.1
Metformin0.2
Placebo/Sitagliptin-0.2

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Change From Baseline in Insulin 3-Hour AUC/Glucose 3-Hour AUC Ratio at Week 54

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. This change from baseline was Week 54 insulin 3-hour AUC/glucose 3-hour AUC ratio minus the Week 0 insulin 3-hour AUC/glucose 3-hour AUC ratio. (NCT01485614)
Timeframe: Baseline and Week 54 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

Intervention[μIU*hr/mL]/[mg*hr/dL] (Mean)
Sitagliptin-0.1
Placebo/Metformin-0.6
Metformin-0.0
Placebo/Sitagliptin-0.3

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Change From Baseline in Insulin at Week 20 for Participants Not on Background Insulin

This change from baseline reflects the Week 20 insulin minus the Week 0 insulin. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionmIU/L (Mean)
Sitagliptin1.59
Placebo/Metformin-3.91
Metformin-7.25
Placebo/Sitagliptin-1.23

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Change From Baseline in Insulin at Week 54 For Participants Not on Background Insulin

This change from baseline reflects the Week 54 insulin minus the Week 0 insulin. (NCT01485614)
Timeframe: Baseline and Week 54

InterventionmIU/L (Mean)
Sitagliptin-9.65
Placebo/Metformin-6.64
Metformin-20.50
Placebo/Sitagliptin-9.95

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Change From Baseline in Insulin Excursion 3-Hour AUC at Week 20

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. Excursion AUC = Incremental AUC above the level at the start of the meal. AUC below the level at the start of the meal did not contribute to the Excursion AUC. This change from baseline was Week 20 insulin Excursion 3-hour AUC minus the Week 0 insulin Excursion 3-hour AUC. (NCT01485614)
Timeframe: Baseline and Week 20 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

InterventionµIU*hr/mL (Mean)
Sitagliptin-12.4
Placebo/Metformin-19.4
Metformin87.5
Placebo/Sitagliptin-82.8

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Change From Baseline in Insulin Excursion 3-Hour AUC at Week 54

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. Excursion AUC = Incremental AUC above the level at the start of the meal. AUC below the level at the start of the meal did not contribute to the Excursion AUC. This change from baseline was Week 54 insulin Excursion 3-hour AUC minus the Week 0 insulin Excursion 3-hour AUC. (NCT01485614)
Timeframe: Baseline and Week 54 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

InterventionµIU*hr/mL (Mean)
Sitagliptin-103.8
Placebo/Metformin-198.5
Metformin-40.2
Placebo/Sitagliptin-116.6

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Change From Baseline in Insulin Excursion 3-Hour AUC/Glucose Excursion 3-Hour AUC Ratio at Week 20

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. Excursion AUC = Incremental AUC above the level at the start of the meal. AUC below the level at the start of the meal did not contribute to the Excursion AUC. This change from baseline was Week 20 insulin Excursion 3-hour AUC/glucose Excursion 3-hour AUC ratio minus the Week 0 insulin Excursion 3-hour AUC/glucose Excursion 3-hour AUC ratio. (NCT01485614)
Timeframe: Baseline and Week 20 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

Intervention[μIU*hr/mL]/[mg*hr/dL] (Mean)
Sitagliptin2.2
Placebo/Metformin7.2
Metformin-2.5
Placebo/Sitagliptin1.4

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Change From Baseline in Insulin Excursion 3-Hour AUC/Glucose Excursion 3-Hour AUC Ratio at Week 54

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. Excursion AUC = Incremental AUC above the level at the start of the meal. AUC below the level at the start of the meal did not contribute to the Excursion AUC. This change from baseline was Week 54 insulin Excursion 3-hour AUC/glucose Excursion 3-hour AUC ratio minus the Week 0 insulin Excursion 3-hour AUC/glucose Excursion 3-hour AUC ratio. (NCT01485614)
Timeframe: Baseline and Week 54 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

Intervention[µIU*hr/mL]/[mg*hr/dL] (Mean)
Sitagliptin4.1
Placebo/Metformin3.7
Metformin-2.7
Placebo/Sitagliptin1.4

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Change From Baseline in Proinsulin at Week 20 For Participants Not on Background Insulin

This change from baseline reflects the Week 20 proinsulin minus the Week 0 proinsulin. (NCT01485614)
Timeframe: Baseline and Week 20

Interventionpmol/L (Mean)
Sitagliptin0.91
Placebo/Metformin-10.88
Metformin12.57
Placebo/Sitagliptin-1.33

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Change From Baseline in Homeostatic Model Assessment of Insulin Resistance (HOMA-IR) at Week 20 For Participants Not on Background Insulin

HOMA-IR = fasting insulin (in mcIU/mL) × FPG (in mg/dL) / (22.5×18). This change from baseline was Week 20 HOMA-IR minus the Week 0 HOMA-IR. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionIndex of insulin resistance (Mean)
Sitagliptin-0.50
Placebo/Metformin-0.86
Metformin-4.46
Placebo/Sitagliptin2.58

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Change From Baseline in Proinsulin at Week 54 For Participants Not on Background Insulin

This change from baseline reflects the Week 54 proinsulin minus the Week 0 proinsulin. (NCT01485614)
Timeframe: Baseline and Week 54

Interventionpmol/L (Mean)
Sitagliptin-10.62
Placebo/Metformin-16.13
Metformin-23.30
Placebo/Sitagliptin-0.50

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Change From Baseline in Proinsulin/Insulin Ratio at Week 20 for Participants Not on Background Insulin

Change from baseline was the Week 20 proinsulin/insulin ratio minus the Week 0 proinsulin/insulin ratio. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionRatio (Mean)
Sitagliptin0.02
Placebo/Metformin0.02
Metformin-0.03
Placebo/Sitagliptin-0.19

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Change From Baseline in Proinsulin/Insulin Ratio at Week 54 For Participants Not on Background Insulin

The change from baseline was Week 54 proinsulin/insulin ratio minus the Week 0 proinsulin/insulin ratio. (NCT01485614)
Timeframe: Baseline and Week 54

InterventionRatio (Mean)
Sitagliptin0.02
Placebo/Metformin-0.03
Metformin-0.01
Placebo/Sitagliptin0.02

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Change From Baseline in Tanner Stage for Pubic Hair at Week 20 - Females

Participant's stage of sexual maturation was assessed using the Tanner staging measure for determining pubertal development in female participants. Tanner staging includes an assessment of pubic hair development (females). Tanner stage (pubic hair) is a score of range 1 to 5 where 1=no development and 5=adult pubic hair. This change from baseline was Week 20 Tanner Staging for Pubic Hair minus the Week 0 Tanner Staging for Pubic Hair. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionScore on a scale (Mean)
Sitagliptin0.1
Placebo/Metformin0.1
Metformin0.2
Placebo/Sitagliptin0.0

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Change From Baseline in Tanner Stage for Pubic Hair at Week 20 - Males

Participant's stage of sexual maturation was assessed using the Tanner staging measure for determining pubertal development in male participants. Tanner staging includes an assessment of pubic hair development (males). Tanner stage (pubic hair) is a score of range 1 to 5 where 1=no development and 5=adult pubic hair. This change from baseline was Week 20 Tanner Staging for Pubic Hair minus the Week 0 Tanner Staging for Pubic Hair. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionScore on a scale (Mean)
Sitagliptin0.3
Placebo/Metformin0.2
Metformin0.0
Placebo/Sitagliptin0.5

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Change From Baseline in Tanner Stage for Pubic Hair at Week 54 - Females

Participant's stage of sexual maturation was assessed using the Tanner staging measure for determining pubertal development in female participants. Tanner staging includes an assessment of pubic hair development (females). Tanner stage (pubic hair) is a score of range 1 to 5 where 1=no development and 5=adult pubic hair. This change from baseline was Week 54 Tanner Staging for Pubic Hair minus the Week 0 Tanner Staging for Pubic Hair. (NCT01485614)
Timeframe: Baseline and Week 54

InterventionScore on a scale (Mean)
Sitagliptin0.5
Placebo/Metformin0.3
Metformin0.8
Placebo/Sitagliptin0.3

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Change From Baseline in Tanner Stage for Pubic Hair at Week 54 - Males

Participant's stage of sexual maturation was assessed using the Tanner staging measure for determining pubertal development in male participants. Tanner staging includes an assessment of pubic hair development (males). Tanner stage (pubic hair) is a score of range 1 to 5 where 1=no development and 5=adult pubic hair. This change from baseline was Week 54 Tanner Staging for Pubic Hair minus the Week 0 Tanner Staging for Pubic Hair. (NCT01485614)
Timeframe: Baseline and Week 54

InterventionScore on a scale (Mean)
Sitagliptin0.5
Placebo/Metformin0.6
Placebo/Sitagliptin0.5

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Change From Baseline in Tanner Staging for Breasts at Week 20 - Females

Participant's stage of sexual maturation was assessed using the Tanner staging measure for determining pubertal development in female participants. Tanner staging includes an assessment of breast development (females). Tanner stage (breast) is a score of range 1 to 5 where 1=no development and 5=adult breast. This change from baseline was Week 20 Tanner Staging for Breasts minus the Week 0 Tanner Staging for Breasts. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionScore on a Scale (Mean)
Sitagliptin0.2
Placebo/Metformin0.1
Metformin0.2
Placebo/Sitagliptin0.3

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Change From Baseline in Tanner Staging for Breasts at Week 54 - Females

Participant's stage of sexual maturation was assessed using the Tanner staging measure for determining pubertal development in female participants. Tanner staging includes an assessment of breast development (females). Tanner stage (breast) is a score of range 1 to 5 where 1=no development and 5=adult breast. This change from baseline was Week 54 Tanner Staging for Breasts minus the Week 0 Tanner Staging for Breasts. (NCT01485614)
Timeframe: Baseline and Week 54

InterventionScore on a Scale (Mean)
Sitagliptin0.5
Placebo/Metformin0.4
Metformin0.5
Placebo/Sitagliptin0.7

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Change From Baseline in Tanner Staging for Genitalia at Week 20 - Males

Participant's stage of sexual maturation was assessed using the Tanner staging measure for determining pubertal development in male participants. Tanner staging includes an assessment of genital development (males) with a score of range 1 to 5 where 1=no development and 5=adult genitals. This change from baseline was Week 20 Tanner Staging for Genitalia minus the Week 0 Tanner Staging for Genitalia. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionScore on a scale (Mean)
Sitagliptin0.3
Placebo/Metformin0.2
Metformin0.0
Placebo/Sitagliptin0.5

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Change From Baseline in Tanner Staging for Genitalia at Week 54 - Males

Participant's stage of sexual maturation was assessed using the Tanner staging measure for determining pubertal development in male participants. Tanner staging includes an assessment of genital development (males) with a score of range 1 to 5 where 1=no development and 5=adult genitals. This change from baseline was Week 54 Tanner Staging for Genitalia minus the Week 0 Tanner Staging for Genitalia. All participants in the Metformin arm were missing baseline or Week 54 measurements. (NCT01485614)
Timeframe: Baseline and Week 54

InterventionScore on a scale (Mean)
Sitagliptin0.5
Placebo/Metformin0.6
Placebo/Sitagliptin0.6

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Change From Baseline in u-NTx/Creatinine Ratio at Week 54 - Females

Urine N-terminal cross-linking telopeptide of bone collagen [u-NTx]/creatinine ratio is a biochemical marker of bone turnover/resorption. Bone Collagen Equivalents (NCT01485614)
Timeframe: Baseline and Week 54

Interventionnmol(BCE)/mmol(creatinine) (Mean)
Sitagliptin-88.4
Placebo/Metformin-61.2
Metformin-80.3
Placebo/Sitagliptin-17.0

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Change From Baseline in u-NTx/Creatinine Ratio at Week 54 - Males

Urine N-terminal cross-linking telopeptide of bone collagen [u-NTx]/creatinine ratio is a biochemical marker of bone turnover/resorption. All participants in the Metformin arm were missing baseline or Week 54 measurements. BCE = Bone Collagen Equivalents (NCT01485614)
Timeframe: Baseline and Week 54

Interventionnmol(BCE)/mmol(creatinine) (Mean)
Sitagliptin-78.2
Placebo/Metformin-102.4
Placebo/Sitagliptin-30.0

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Change From Baseline in Urine N-terminal Cross-linking Telopeptide of Bone Collagen [u-NTx]/Creatinine Ratio at Week 20 - Females

Urine N-terminal cross-linking telopeptide of bone collagen [u-NTx]/creatinine ratio is a biochemical marker of bone turnover/resorption. BCE = Bone Collagen Equivalents (NCT01485614)
Timeframe: Baseline and Week 20

Interventionnmol(BCE)/mmol(creatinine) (Mean)
Sitagliptin-28.7
Placebo/Metformin-41.2
Metformin-98.0
Placebo/Sitagliptin12.7

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Change From Baseline u-NTx/Creatinine Ratio at Week 20 - Males

Urine N-terminal cross-linking telopeptide of bone collagen [u-NTx]/creatinine ratio is a biochemical marker of bone turnover/resorption. BCE = Bone Collagen Equivalents (NCT01485614)
Timeframe: Baseline and Week 20

Interventionnmol(BCE)/mmol(creatinine) (Mean)
Sitagliptin-30.9
Placebo/Metformin-69.8
Metformin62.0
Placebo/Sitagliptin-29.0

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Growth Velocity at Week 20 - Females

Growth Velocity (cm/year) = (Change from Baseline in height)/(Change from Baseline in chronologic age). (NCT01485614)
Timeframe: Week 20

Interventioncm/year (Mean)
Sitagliptin3.2
Placebo/Metformin1.9
Metformin5.0
Placebo/Sitagliptin0.6

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Growth Velocity at Week 20 - Males

Growth Velocity (cm/year) = (Change from Baseline in height)/(Change from Baseline in chronologic age). (NCT01485614)
Timeframe: Week 20

Interventioncm/year (Mean)
Sitagliptin2.6
Placebo/Metformin3.6
Metformin-1.0
Placebo/Sitagliptin1.7

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Growth Velocity at Week 54 - Females

Growth Velocity (cm/year) = (Change from Baseline in height)/(Change from Baseline in chronologic age). (NCT01485614)
Timeframe: Week 54

Interventioncm/year (Mean)
Sitagliptin2.1
Placebo/Metformin1.2
Metformin2.4
Placebo/Sitagliptin0.7

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Growth Velocity at Week 54 - Males

Growth Velocity (cm/year) = (Change from Baseline in height)/(Change from Baseline in chronologic age). (NCT01485614)
Timeframe: Week 54

Interventioncm/year (Mean)
Sitagliptin2.5
Placebo/Metformin2.8
Metformin1.7
Placebo/Sitagliptin2.8

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Change From Baseline in Insulin 3-Hour AUC at Week 54

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. This change from baseline was Week 54 insulin 3-hour AUC minus the Week 0 insulin 3-hour AUC. (NCT01485614)
Timeframe: Baseline and Week 54 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

InterventionµIU*hr/mL (Mean)
Sitagliptin-43.2
Placebo/Metformin-253.9
Metformin-37.8
Placebo/Sitagliptin-184.4

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Change From Baseline in Insulin 3-hour AUC at Week 20

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. This change from baseline was Week 20 insulin 3-hour AUC minus the Week 0 insulin 3-hour AUC. (NCT01485614)
Timeframe: Baseline and Week 20 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

InterventionµIU*hr/mL (Mean)
Sitagliptin-14.5
Placebo/Metformin-32.8
Metformin141.7
Placebo/Sitagliptin-145.6

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Change From Baseline in Homeostatic Model Assessment of β-cell Function (HOMA-β) at Week 20 For Participants Not on Background Insulin

HOMA-β = 20 × fasting insulin (in mcIU/mL) ÷ {[FPG (in mg/dL)/18] - 3.5}. The change from baseline was Week 20 HOMA-β minus the Week 0 HOMA-β. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionPercentage of Beta Cell Function (Mean)
Sitagliptin15.72
Placebo/Metformin-53.23
Metformin-1757.50
Placebo/Sitagliptin-64.78

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Change From Baseline in HOMA-β at Week 54 For Participants Not on Background Insulin

HOMA-β = 20 × fasting insulin (in mcIU/mL) ÷ {[FPG (in mg/dL)/18] - 3.5}. This change from baseline was Week 54 HOMA-β minus the Week 0 HOMA-β. (NCT01485614)
Timeframe: Baseline and Week 54

InterventionPercentage of Beta Cell Function (Mean)
Sitagliptin-41.15
Placebo/Metformin-63.88
Metformin-1860.69
Placebo/Sitagliptin-121.48

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Change From Baseline in HOMA-IR at Week 54 For Participants Not on Background Insulin

HOMA-IR = fasting insulin (in mcIU/mL) × FPG (in mg/dL) / (22.5×18). This change from baseline was Week 54 HOMA-IR minus the Week 0 HOMA-IR. (NCT01485614)
Timeframe: Baseline and Week 54

InterventionIndex of insulin resistance (Mean)
Sitagliptin-6.13
Placebo/Metformin-1.30
Metformin-15.18
Placebo/Sitagliptin-2.21

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Change From Baseline in Hemoglobin A1C (A1C) at Week 20

Glycated hemoglobin (A1C) is a blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. Change from baseline was estimated as the Week 20 A1C minus the Week 0 A1C. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionPercentage (Mean)
Sitagliptin-0.13
Placebo/Metformin-0.02
Metformin-1.03
Placebo/Sitagliptin0.57

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Change From Baseline in Glucose Excursion 3-Hour AUC at Week 54

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. Excursion AUC = Incremental AUC above the level at the start of the meal. AUC below the level at the start of the meal did not contribute to the Excursion AUC. This change from baseline was Week 54 glucose Excursion 3-hour AUC minus the Week 0 glucose Excursion 3-hour AUC. (NCT01485614)
Timeframe: Baseline and Week 54 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

Interventionmg*hr/dL (Mean)
Sitagliptin-30.7
Placebo/Metformin-50.1
Metformin-49.0
Placebo/Sitagliptin-74.0

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Change From Baseline in Glucose Excursion 3-Hour AUC at Week 20

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. Excursion AUC = Incremental AUC above the level at the start of the meal. AUC below the level at the start of the meal did not contribute to the Excursion AUC. This change from baseline was Week 20 glucose Excursion 3-hour AUC minus the Week 0 glucose Excursion 3-hour AUC. (NCT01485614)
Timeframe: Baseline and Week 20 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

Interventionmg*hr/dL (Mean)
Sitagliptin-43.5
Placebo/Metformin10.8
Metformin39.8
Placebo/Sitagliptin46.2

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Change From Baseline in Glucose 3-Hour Total Area Under the Curve (AUC) at Week 20

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. This change from baseline was Week 20 glucose 3-hour AUC minus the Week 0 glucose 3-hour AUC. (NCT01485614)
Timeframe: Baseline and Week 20 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

Interventionmg*hr/dL (Mean)
Sitagliptin-49.3
Placebo/Metformin2.0
Metformin18.6
Placebo/Sitagliptin191.0

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Mean Percent Change of Peripheral Blood Mononuclear Cells Expressing CD26 From Baseline at Week 20

The percent change from baseline in CD26 = ([CD26 value at Week 20] - [baseline CD26 value]) ÷ baseline CD26 value × 100. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionPercent Change (Mean)
Sitagliptin4.06
Placebo/Metformin-1.78
Metformin4.89
Placebo/Sitagliptin14.57

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Mean Percent Change of Peripheral Blood Mononuclear Cells Expressing CD26 From Baseline at Week 54

The percent change from baseline in CD26 = ([CD26 value at Week 54] - [baseline CD26 value]) ÷ baseline CD26 value × 100. (NCT01485614)
Timeframe: Baseline and Week 54

InterventionPercent Change (Mean)
Sitagliptin4.74
Placebo/Metformin4.27
Metformin12.63
Placebo/Sitagliptin-5.30

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Number of Participants Who Discontinued Study Drug Due to an Adverse Event During Weeks 0-54

The number of participants who discontinued from study drug due to an adverse event during Weeks 0-54 was reported. An adverse event is defined as any untoward medical occurrence in a person administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT01485614)
Timeframe: Up to Week 54

InterventionParticipants (Count of Participants)
Sitagliptin5
Placebo/Metformin1
Metformin0
Placebo/Sitagliptin0

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Number of Participants Who Experienced ≥1 Adverse Event During Weeks 0-56

The number of participants experiencing ≥1 adverse event during Weeks 0-56 was reported. An adverse event is defined as any untoward medical occurrence in a person administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT01485614)
Timeframe: Up to Week 56

InterventionParticipants (Count of Participants)
Sitagliptin73
Placebo/Metformin67
Metformin7
Placebo/Sitagliptin4

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Percent Change From Baseline in IGF-1 at Week 20 - Males

IGF-1 is a biochemical marker of growth hormone action and growth. The percent change from baseline in IGF-1 = ([IGF-1 value at Week 20] - [baseline IGF-1 value]) ÷ [baseline IGF-1 value] × 100. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionPercent Change (Mean)
Sitagliptin-2.7
Placebo/Metformin9.3
Metformin7.6
Placebo/Sitagliptin5.3

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Percent Change From Baseline in IGF-1 at Week 54 - Males

IGF-1 is a biochemical marker of growth hormone action and growth. The percent change from baseline in IGF-1 = ([IGF-1 value at Week 54] - [baseline IGF-1 value]) ÷ [baseline IGF-1 value] × 100. (NCT01485614)
Timeframe: Baseline and Week 54

InterventionPercent Change (Mean)
Sitagliptin-4.9
Placebo/Metformin29.6
Metformin18.8
Placebo/Sitagliptin-6.8

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Percent Change From Baseline in IGF-1 at Week 54 - Females

IGF-1 is a biochemical marker of growth hormone action and growth. The percent change from baseline in IGF-1 = ([IGF-1 value at Week 54] - [baseline IGF-1 value]) ÷ [baseline IGF-1 value] × 100. (NCT01485614)
Timeframe: Baseline and Week 54

InterventionPercent Change (Mean)
Sitagliptin-1.5
Placebo/Metformin7.2
Metformin-11.9
Placebo/Sitagliptin-13.5

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Percent Change From Baseline in IGF-BP3 at Week 20 - Males

IGF-BP3 is a biochemical marker of growth hormone action and growth. The percent change from baseline in IGF-BP3 = ([IGF-BP3 value at Week 20] - [baseline IGF-BP3 value]) ÷ [baseline IGF-BP3 value] × 100. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionPercent Change (Mean)
Sitagliptin5.6
Placebo/Metformin10.2
Metformin3.3
Placebo/Sitagliptin14.2

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Percent Change From Baseline in IGF-BP3 at Week 54 - Females

IGF-BP3 is a biochemical marker of growth hormone action and growth. The percent change from baseline in IGF-BP3 = ([IGF-BP3 value at Week 54] - [baseline IGF-BP3 value]) ÷ [baseline IGF-BP3 value] × 100. (NCT01485614)
Timeframe: Baseline and Week 54

InterventionPercent Change (Mean)
Sitagliptin2.0
Placebo/Metformin4.5
Metformin11.4
Placebo/Sitagliptin-13.4

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Percent Change From Baseline in IGF-BP3 at Week 54 - Males

IGF-BP3 is a biochemical marker of growth hormone action and growth. The percent change from baseline in IGF-BP3 = ([IGF-BP3 value at Week 54] - [baseline IGF-BP3 value]) ÷ [baseline IGF-BP3 value] × 100. (NCT01485614)
Timeframe: Baseline and Week 54

InterventionPercent Change (Mean)
Sitagliptin5.4
Placebo/Metformin18.2
Metformin-2.9
Placebo/Sitagliptin22.5

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Percent Change From Baseline in Insulin-like Growth Factor Binding Protein 3 (IGF-BP3) at Week 20 - Females

IGF-BP3 is a biochemical marker of growth hormone action and growth. The percent change from baseline in IGF-BP3 = ([IGF-BP3 value at Week 20] - [baseline IGF-BP3 value]) ÷ [baseline IGF-BP3 value] × 100. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionPercent Change (Mean)
Sitagliptin3.5
Placebo/Metformin3.8
Metformin8.4
Placebo/Sitagliptin-0.7

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Percent Change From Baseline in Insulin-like Growth Factor-1 (IGF-1) at Week 20 - Females

IGF-1 is a biochemical marker of growth hormone action and growth. The percent change from baseline in IGF-1 = ([IGF-1 value at Week 20] - [baseline IGF-1 value]) ÷ [baseline IGF-1 value] × 100. (NCT01485614)
Timeframe: Baseline and Week 20

InterventionPercent Change (Mean)
Sitagliptin0.5
Placebo/Metformin11.0
Metformin-3.2
Placebo/Sitagliptin41.4

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Percentage of Participants Initiating Glycemic Rescue Therapy by Week 20

The percentage of participants who initiated glycemic rescue therapy prior to Week 20 was reported. (NCT01485614)
Timeframe: Up to Week 20

InterventionPercentage of participants (Number)
Sitagliptin5.3
Placebo/Metformin11.1
Metformin0.0
Placebo/Sitagliptin40.0

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Change From Baseline in BMI at Week 54

This change from baseline was Week 54 BMI minus the Week 0 BMI. (NCT01485614)
Timeframe: Baseline and Week 54

Interventionkg/m^2 (Mean)
Sitagliptin-0.4
Placebo/Metformin-1.0
Metformin-0.6
Placebo/Sitagliptin-0.3

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Percentage of Participants Who Discontinued Study Drug Due to an Adverse Event During Weeks 0-54 (Analysis of Selected Arms: Sitagliptin and Placebo/Metformin)

The percentage of participants who discontinued from study drug due to an adverse event during Weeks 0-54 was reported. An adverse event is any untoward medical occurrence in a person administered a pharmaceutical product and does not have to have a causal relationship with this treatment. The SAP did not specify for the Metformin arm to be included in statistical comparisons, so results for this arm are provided separately. (NCT01485614)
Timeframe: Up to Week 54

InterventionPercentage of participants (Number)
Sitagliptin5.3
Placebo/Metformin1.1

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Percentage of Participants Who Experienced ≥1 Adverse Event During Weeks 0-56 (Analysis of Selected Arms: Sitagliptin and Placebo/Metformin)

The number of participants experiencing ≥1 adverse event during Weeks 0-56 was reported. An adverse event is any untoward medical occurrence in a person administered a pharmaceutical product and does not have to have a causal relationship with this treatment. The SAP did not specify for the Metformin arm to be included in statistical comparisons, so results for this arm are provided separately. (NCT01485614)
Timeframe: Up to Week 56

InterventionPercentage of participants (Number)
Sitagliptin76.8
Placebo/Metformin74.4

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Percentage of Participants With A1C at Goal (<6.5%) at Week 20

The percentage of participants with A1C at goal (<6.5%) at Week 20 was presented. All numbers shown in each individual treatment arm are based on the observed values (Missing = Not at Goal). (NCT01485614)
Timeframe: Week 20

InterventionPercentage of participants (Number)
Sitagliptin30.5
Placebo/Metformin23.3
Metformin66.7
Placebo/Sitagliptin20.0

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Percentage of Participants With A1C at Goal (<6.5%) at Week 20 (Analysis of Selected Arms: Sitagliptin and Placebo (Pooled))

The percentage of participants with A1C at goal (<6.5%) at Week 20 was presented. The analysis table includes the observed values for each treatment arm (Missing = Not at Goal) and the estimated treatment difference (Missing = Multiple Imputation). The current outcome measure focused on comparing results from participants randomized to sitagliptin or placebo. The Placebo arm in this comparison was a pooling of the Placebo/Metformin and Placebo/Sitagliptin arms. The SAP did not specify for the Metformin arm to be included in statistical comparisons, so results for this arm are provided separately. (NCT01485614)
Timeframe: Week 20

InterventionPercentage of Participants (Number)
Sitagliptin30.5
Placebo (Pooled)23.2

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Change From Baseline in FPG at Week 20 (Analysis of Selected Arms: Sitagliptin and Placebo (Pooled))

Blood glucose was measured on a fasting basis. Change in plasma glucose levels was FPG at Week 20 minus FPG at baseline and was estimated from a longitudinal data analysis model. The current outcome measure focused on results from participants randomized to sitagliptin or placebo. The Week 20 treatment comparison of Sitagliptin vs Placebo included all participants treated with Sitagliptin or Placebo. The Placebo arm in this comparison was a pooling of the Placebo/Metformin and Placebo/Sitagliptin arms. The SAP did not specify for the Metformin arm to be included in statistical comparisons, so results for this arm are provided separately. (NCT01485614)
Timeframe: Baseline and Week 20

Interventionmg/dL (Least Squares Mean)
Sitagliptin7.2
Placebo (Pooled)5.7

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Change From Baseline in Glucose 3-Hour AUC at Week 54

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. This change from baseline was Week 54 glucose 3-hour AUC minus the Week 0 glucose 3-hour AUC. (NCT01485614)
Timeframe: Baseline and Week 54 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

Interventionmg*hr/dL (Mean)
Sitagliptin-21.1
Placebo/Metformin-36.0
Metformin-73.1
Placebo/Sitagliptin-63.3

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Change From Baseline in FPG at Week 54

Blood glucose was measured on a fasting basis. Change in plasma glucose levels was FPG at Week 54 minus FPG at baseline. (NCT01485614)
Timeframe: Baseline and Week 54

Interventionmg/dL (Mean)
Sitagliptin-3.03
Placebo/Metformin-4.52
Metformin-29.92
Placebo/Sitagliptin3.00

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 20

Blood glucose was measured on a fasting basis. Change in plasma glucose levels was FPG at Week 20 minus FPG at baseline. (NCT01485614)
Timeframe: Baseline and Week 20

Interventionmg/dL (Mean)
Sitagliptin9.98
Placebo/Metformin7.59
Metformin-19.88
Placebo/Sitagliptin57.67

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Change From Baseline in Calcitonin at Week 54 - Males

Calcitonin, along with parathyroid hormone, is a hormone that regulates calcium and bone metabolism. This change from baseline was Week 54 calcitonin minus the Week 0 calcitonin. (NCT01485614)
Timeframe: Baseline and Week 54

Interventionng/L (Mean)
Sitagliptin0.1
Placebo/Metformin-0.3
Metformin0.0
Placebo/Sitagliptin1.4

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Change From Baseline in Calcitonin at Week 54 - Females

Calcitonin, along with parathyroid hormone, is a hormone that regulates calcium and bone metabolism. This change from baseline was Week 54 calcitonin minus the Week 0 calcitonin. (NCT01485614)
Timeframe: Baseline and Week 54

Interventionng/L (Mean)
Sitagliptin-1.0
Placebo/Metformin-1.9
Metformin0.0
Placebo/Sitagliptin0.3

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Percentage of Participants With A1C at Goal (<6.5%) at Week 54

The percentage of participants with A1C at goal (<6.5%) at Week 54 was presented. All numbers shown in each individual treatment arm are based on the observed values (Missing = Not at Goal). (NCT01485614)
Timeframe: Week 54

InterventionPercentage of participants (Number)
Sitagliptin20.0
Placebo/Metformin35.6
Metformin22.2
Placebo/Sitagliptin20.0

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Percentage of Participants With A1C at Goal (<7.0%) at Week 20

The percentage of participants with A1C at goal (<7.0%) at Week 20 was presented. All numbers shown in each individual treatment arm are based on the observed values (Missing = Not at Goal). (NCT01485614)
Timeframe: Week 20

InterventionPercentage of Participants (Number)
Sitagliptin49.5
Placebo/Metformin37.8
Metformin77.8
Placebo/Sitagliptin20.0

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Percentage of Participants With A1C at Goal (<7.0%) at Week 20 (Analysis of Selected Arms: Sitagliptin and Placebo (Pooled))

The percentage of participants with A1C at goal (<7.0%) at Week 20 was presented. The analysis table includes the observed values for each treatment arm (Missing = Not at Goal) and the estimated treatment difference (Missing = Multiple Imputation). The current outcome measure focused on comparing results from participants randomized to sitagliptin or placebo. The Placebo arm in this comparison was a pooling of the Placebo/Metformin and Placebo/Sitagliptin arms. The SAP did not specify for the Metformin arm to be included in statistical comparisons, so results for this arm are provided separately. (NCT01485614)
Timeframe: Week 20

InterventionPercentage of participants (Number)
Sitagliptin49.5
Placebo (Pooled)36.8

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Percentage of Participants With A1C at Goal (<7.0%) at Week 54

The percentage of participants with A1C at goal (<7.0%) at Week 54 was presented. All numbers shown in each individual treatment arm are based on the observed values (Missing = Not at Goal). (NCT01485614)
Timeframe: Week 54

InterventionPercentage of participants (Number)
Sitagliptin28.4
Placebo/Metformin40.0
Metformin33.3
Placebo/Sitagliptin20.0

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Change From Baseline in Calcitonin at Week 20 - Males

Calcitonin, along with parathyroid hormone, is a hormone that regulates calcium and bone metabolism. This change from baseline was Week 20 calcitonin minus the Week 0 calcitonin. (NCT01485614)
Timeframe: Baseline and Week 20

Interventionng/L (Mean)
Sitagliptin0.2
Placebo/Metformin-0.2
Metformin-1.6
Placebo/Sitagliptin0.5

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Change From Baseline in Calcitonin at Week 20 - Females

Calcitonin, along with parathyroid hormone, is a hormone that regulates calcium and bone metabolism. This change from baseline was Week 20 calcitonin minus the Week 0 calcitonin. (NCT01485614)
Timeframe: Baseline and Week 20

Interventionng/L (Mean)
Sitagliptin-0.1
Placebo/Metformin-2.0
Metformin0.0
Placebo/Sitagliptin0.0

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Change From Baseline in C-Peptide Excursion 3-Hour AUC at Week 54

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. Excursion AUC = Incremental AUC above the level at the start of the meal. AUC below the level at the start of the meal did not contribute to the Excursion AUC. This change from baseline was Week 54 C-peptide Excursion 3-hour AUC minus the Week 0 C-peptide Excursion 3-hour AUC. (NCT01485614)
Timeframe: Baseline and Week 54 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

Interventionng*hr/ml (Mean)
Sitagliptin-1.8
Placebo/Metformin-5.2
Metformin0.9
Placebo/Sitagliptin-5.9

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Change From Baseline in C-peptide Excursion 3-Hour AUC at Week 20

AUC endpoints were derived via the trapezoidal rule using 9-point Meal Tolerance Test (MTT) measurements. Excursion AUC = Incremental AUC above the level at the start of the meal. AUC below the level at the start of the meal did not contribute to the Excursion AUC. This change from baseline was Week 20 C-peptide Excursion 3-hour AUC minus the Week 0 C-peptide Excursion 3-hour AUC. (NCT01485614)
Timeframe: Baseline and Week 20 (-10 min. before ingesting the meal, 0 min. prior to the meal, 10, 20, 30, 60, 90, 120, 180 minutes after ingesting the meal)

Interventionng*hr/ml (Mean)
Sitagliptin-1.1
Placebo/Metformin-0.4
Metformin4.1
Placebo/Sitagliptin-4.8

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Insulin Sensitivity

Insulin Sensitivity measured at the end of each treatment period. The primary outcome variable was the difference in the disposition index (DI) determined as the product of the acute insulin response to glucose (AIRg) x the insulin sensitivity index (SI) in subjects during IVGTT on the 8th day (after 7 days) of on dex + placebo, then a after a washout of approximately 4 weeks, participants crossed over to dex + sitagliptin 100 mg x 7 days. Subjects were randomized to order of medication. The primary analyses will be an ANCOVA, including baseline responses as a covariate. (NCT01488279)
Timeframe: Measured on day #8 (after 8 days of sitagliptin or placebo) followed by a 4 week washout then measured again on day #8 (after 8 days of crossover treatment).

Interventionratio without units (Mean)
Sitagliptin1835.4
Placebo1846.0

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Change in Glucose Response

Change in glucose response during the MTT. This was the Si (insulin sensitivity). We sought to determine whether there was an improvement in the glucose response after a meal on the DPP4i compared to placebo in the face of steroid (dexamethasone). (NCT01488279)
Timeframe: measured on day #9 (after 7 days of study drug and 1 day of IVGTT) of sitagliptin during MTT, then after 4 week washout, measured again on day #9 (after 7 days of study drug + 1 day of IVGTT) of dex + placebo during MTT

Interventionresponse x 10000 / minute / microUnit/ml (Least Squares Mean)
Sitagliptin4.219
Placebo4.228

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Change in Insulin Secretion (AIRg or Acute Insulinogenic Response to Glucose)

We measured the change in insulin secretion (AIRg or acute insulinogenic response to glucose) during the MTT and compared the insulin secretion on the DPP4 inhibitor (sitagliptin) compared to placebo. We had expected the AIRg to be greater with DPP4i compared to placebo. (NCT01488279)
Timeframe: measured twice: on day #8 (after 7 days of study drug and 1 day of IVGTT) of sitagliptin during MTT, then after 4 week washout, measured again on day #8 (after 7 days of study drug + 1 day of IVGTT) of dex + placebo during MTT

Interventionpmol/l (Least Squares Mean)
Sitagliptin519.6
Placebo558.6

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The Change of Glycated Hemoglogin(HbA1c) From Baseline to 16 Weeks of Treatment

The change of glycated hemoglogin(HbA1c) from baseline to 16 weeks of treatment between Placebo + Metformin+Sitagliptin and Metformin + Sitagliptin + Acarbose group (NCT01490918)
Timeframe: baseline, 16 weeks

Intervention% of HbA1c (Mean)
Placebo+Metformin+Sitagliptin-0.09
Sitagliptin+Metformin+Acarbose-0.44
Placebo+Sitagliptin+Acarbose0.84

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The Change of HbA1c From Baseline to 24 Weeks of Treatment

The change of glycated hemoglogin(HbA1c) from baseline to 24 weeks of treatment between 3 groups (NCT01490918)
Timeframe: baseline, 24 weeks

Intervention% of HbA1c (Mean)
Placebo+Metformin+Sitagliptin-0.34
Sitagliptin+Metformin+Acarbose-0.47
Placebo+Sitagliptin+Acarbose0.23

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The Change of PPG2hr From Baseline to 24 Weeks of Treatment

The change of PPG2hr (post prandia blood glucose 2hr from baseline to 24 weeks of treatment between 3 groups (NCT01490918)
Timeframe: baseline, 24 weeks

Interventionmmol/L (Mean)
Placebo+Metformin+Sitagliptin-1.73
Sitagliptin+Metformin+Acarbose-1.76
Placebo+Sitagliptin+Acarbose0.06

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Changes in MAGE of Glucose During CGMS Between 2 Group(Group 1 vs Group 2),

Change of mean amplitude of glycemic excursion of CGMS(continuous glucose monitoring system) data at 16 week from baseline between 2 groups (placebo+metformin + sitagliptin vs acarbose + metformin + sitagliptin) (NCT01490918)
Timeframe: Visit 2(baseline) and Visit 5(16W)

Interventionmg/dL (Mean)
Placebo+Metformin+Sitagliptin-8.79
Sitagliptin+Metformin+Acarbose-18.5
Placebo + Acarbose + Sitagliptin2.72

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Changes in Mean Glucose During CGMS Between 3 Group

Change of mean glucose of CGMS(continuous glucose monitoring system) data at 16 week from baseline between 3 groups (NCT01490918)
Timeframe: Visit 2(baseline) and Visit 5(16W)

Interventionmmol/L (Mean)
Placebo+Metformin+Sitagliptin-0.91
Sitagliptin+Metformin+Acarbose-1.16
Placebo + Sitagliptin + Acarbose3.22

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Changes in Variation of Glucose During CGMS Between 3 Group

Change of standard deviation of CGMS(continuous glucose monitoring system) data at 16 week from baseline between 3 groups (placebo+metformin + sitagliptin vs acarbose + metformin + sitagliptin vs placebo + acarbose + sitagliptin) (NCT01490918)
Timeframe: Visit 2(baseline) and Visit 5(16W)

Interventionmmol/L (Mean)
Placebo+Metformin+Sitagliptin-0.33
Sitagliptin+Metformin+Acarbose-0.65
Placebo + Acarbose + Sitagliptin0.03

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Change in Active GLP-1 at 0 Minute During Mixed Meal Test Between 2 Groups (Group 1, group2)

Change of active GLP-1 at 0 minute during mixed meal test at 16 week from baseline between 2 groups(group1, group2) (NCT01490918)
Timeframe: baseline, 16 week

Interventionpg/ml (Mean)
Placebo+Metformin+Sitagliptin-8.55
Sitagliptin+Metformin+Acarbose-9.33

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Change in Active GLP-1 at 120 Minute During Mixed Meal Test Between 2 Groups (Group 1, group2)

Change of active GLP-1 at 120 minute during mixed meal test at 16 week from baseline between 2 groups(group1, group2) (NCT01490918)
Timeframe: baseline, 16 week

Interventionpg/ml (Mean)
Placebo+Metformin+Sitagliptin-32.92
Sitagliptin+Metformin+Acarbose-23.36

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Changes in Glucagon During Meal Tolerance Test Between 2 Group(Group 1 vs Group 2),

Change of AUC(area under the curve) of glucagon at 16 week from baseline between 2 groups (placebo+metformin + sitagliptin vs acarbose + metformin + sitagliptin) (NCT01490918)
Timeframe: Visit 2(baseline) and Visit 5(16W)

Interventionmin pg/mL (Mean)
Placebo+Metformin+Sitagliptin-79.22
Sitagliptin+Metformin+Acarbose-1411.79

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Changes in Glucose During Meal Tolerance Test Between 2 Group(Group 1 vs Group 2),

Change of AUC(area under the curve) of glucose at 16 week from baseline between 2 groups (placebo+metformin + sitagliptin vs acarbose + metformin + sitagliptin) (NCT01490918)
Timeframe: Visit 2(baseline) and Visit 5(16W)

Interventionmg min/dL (Mean)
Placebo+Metformin+Sitagliptin28.85
Sitagliptin+Metformin+Acarbose-743.08

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Changes in Insulin During Mixed Meal Tolerance Test Between 2 Group(Group 1 vs Group 2),

Change of AUC(area under the curve) of insulin at 16 week from baseline between 2 groups (placebo+metformin + sitagliptin vs acarbose + metformin + sitagliptin) (NCT01490918)
Timeframe: Visit 2(baseline) and Visit 5(16W)

Interventionpg min/mL (Mean)
Placebo+Metformin+Sitagliptin647.65
Sitagliptin+Metformin+Acarbose221.42

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Active GLP-1

Active GLP-1 (Fasting and during a Mixed Meal Test). The Change in Fasting Active GLP-1 refers to the change in fasting active GLP-1 from pre-intervention time point to post-intervention time point. The Change in Peak Active GLP-1 refers to the change in the peak active GLP-1 level from the pre-intervention time point to post-intervention time point. (NCT01512797)
Timeframe: Pre-Intervention and Post-Intervention

,
Interventionpmol/L (Mean)
Change in Fasting Active GLP-1Change in Peak Active GLP-1
Placebo-0.222.97
Sitagliptin Phosphate1.4522.08

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Change in Area Under the Curve (AUC) Glucose Levels After Mixed Meal Test

Glucose levels were measured in study participants while fasting and periodically over 3 hours after drinking a 200 kcal mixed meal test, before and after intervention (Sitagliptin or Placebo). AUC was measured by trapezoidal method. (NCT01512797)
Timeframe: Baseline and ~4 weeks

,
Interventionmmol/L/min (Mean)
Pre-Intervention Glucose AUCPost-Intervention Glucose AUC
Placebo7.967.75
Sitagliptin Phosphate8.317.67

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Change in Postprandial Glucose Levels After Mixed Meal Test

Glucose levels were measured in study participants while fasting and periodically over 3 hours after drinking a 200 kcal mixed meal test, before and after intervention (Sitagliptin or Placebo). (NCT01512797)
Timeframe: Baseline and ~4 weeks

,
Interventionmmol/L (Mean)
Pre-Intervention Fasting GlucosePost-Intervention Fasting GlucosePre-Intervention 120 minute glucosePost-Intervention 120 minute glucosePre-Intervention Average Glucose during MMTPost-Intervention Average Glucose during MMT
Placebo6.526.397.016.978.127.86
Sitagliptin Phosphate7.106.447.516.798.557.84

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Effect of Sitagliptin vs Placebo on Satiety in Patients With Type 2 Diabetes After Gastric Bypass Surgery

"Satiety levels were measured in study participants while they were fasting and periodically over a three hour period after drinking a 200 kcal meal drink, before and after intervention via a Visual Analog Scale. Participants were asked to mark on a 0 to 150 millimeter scale their response to the following question: How full do you feel right now? with lower scores indicating not full at all and higher scores indicating extremely full." (NCT01512797)
Timeframe: Baseline and ~4 weeks

,
Interventionmm (Mean)
Pre-Intervention fasting satiety levelPost-Intervention fasting satiety levelPre-Intervention 180 minute glucosePost-Intervention 180 minute glucose
Placebo49.0658.5050.50103.75
Sitagliptin Phosphate51.9422.3837.8143.69

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Occurrence of Side Effects In Relation to Sitagliptin

Side effects to Sitagliptin or Placebo were measured in study participants via Sigstad score questionnaire, while fasting and periodically during a 3 hour period after drinking a 200 kcal meal drink, before and after intervention. The Sigstad scoring system is based on the participants report of the occurrence of 16 symptoms suggestive of the dumping syndrome. Each symptom is given a different score. For example, desire to sit down (+4), breathlessness (+3), dizziness (+2), nausea (+1), vomiting (-4) etc.The scale can range from -5 to 34. Scores greater than or equal to 7, after glucose intake, are considered diagnostic of dumping syndrome. (NCT01512797)
Timeframe: 6 weeks

,
Interventionunits on Sigstad scale (Mean)
Pre-Intervention Average Sigstad ScorePost-Intervention Average Sigstad Score
Placebo5.584.40
Sitagliptin Phosphate2.152.24

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Prandial Plasma Glucose (PPG) Increments at Lunch.

Estimated mean post prandial increments at lunch after 24 weeks of treatment. (NCT01519674)
Timeframe: After 24 weeks of treatment

Interventionmmol/L (Least Squares Mean)
BID + Met3.05
BID + Sita + Met2.19
OD + Sita + Met2.52

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Prandial Plasma Glucose (PPG) Increments at Dinner.

Estimated mean post prandial increments at dinner after 24 weeks of treatment. (NCT01519674)
Timeframe: After 24 weeks of treatment

Interventionmmol/L (Least Squares Mean)
BID + Met0.89
BID + Sita + Met1.01
OD + Sita + Met0.17

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Prandial Plasma Glucose (PPG) Increments at Breakfast

Estimated mean post prandial increments at breakfast after 24 weeks of treatment. (NCT01519674)
Timeframe: After 24 weeks of treatment

Interventionmmol/L (Least Squares Mean)
BID + Met2.01
BID + Sita + Met1.73
OD + Sita + Met2.89

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Change From Baseline in Patient Reported Outcome by Use of the Treatment Related Impact Measure - Diabetes.

Estimated mean change from baseline in Treatment Related Impact Measure - Diabetes (TRIM-D) 'total score' to end of trial. The score measured treatment satisfaction. The scores were transformed to a 0-100 scale with higher scores indicating greater satisfaction. (NCT01519674)
Timeframe: Week 0 to Week 24

Interventionscores (Least Squares Mean)
BID + Met6.22
BID + Sita + Met5.93
OD + Sita + Met6.20

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Adverse Events (AEs)

Rate of AEs per 100 years of patient exposure. An adverse event was defined as treatment emergent if the event had onset date on or after the first day of exposure to randomised treatment and no later than the last day of randomised treatment. (NCT01519674)
Timeframe: Week 0 to Week 24

,,
InterventionEvents/100 years of patient exposure (Number)
All treatment emergent adverse eventsSerious adverse eventsSevere adverse eventsModerate adverse eventsMild adverse eventsFatal adverse events
BID + Met262.28.46.071.0185.20
BID + Sita + Met209.95.810.574.6124.80
OD + Sita + Met281.210.57.079.7194.50

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Change From Baseline in Fasting Plasma Glucose (FPG)

Estimated mean change from baseline in fasting plasma glucose (FPG) (NCT01519674)
Timeframe: Week 0 to Week 24

Interventionmmol/L (Least Squares Mean)
BID + Met-1.90
BID + Sita + Met-2.03
OD + Sita + Met-1.96

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Change From Baseline in HbA1c (Glycosylated Haemoglobin)

Estimated mean change from baseline in HbA1c after 24 weeks of treatment. (NCT01519674)
Timeframe: Week 0 to Week 24

Interventionpercentage of glycosylated haemoglobin (Least Squares Mean)
BID + Met-1.27
BID + Sita + Met-1.51
OD + Sita + Met-1.15

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Number of Treatment Emergent Hypoglycaemic Episodes (Nocturnal and Day-time) Classified Both According to the American Diabetes Association (ADA) Definition and to an Additional Definition for Minor Episodes.

Number of treatment emergent hypoglycaemic episodes. Treatment emergent hypoglycaemic episode: if the onset of the episode was on or after the first day of exposure to randomised treatment and no later than the last day of randomised treatment. Nocturnal: Time of onset between 00:01 and 05:59 a.m. (both included). Additional minor hypoglycaemic episode: symptomatic or asymptomatic hypoglycaemia with blood glucose (BG) values < 2.8 mmol/L (50 mg/dL) or plasma glucose (PG) < 3.1 mmol/L (56 mg/dL), and which was handled by the subject him/herself. (NCT01519674)
Timeframe: Week 0 to Week 24

,,
Interventionepisodes (Number)
Diurnal (ADA)Nocturnal (ADA)Diurnal (additional minor)Nocturnal (additional minor)
BID + Met5156816321
BID + Sita + Met4405411214
OD + Sita + Met249637123

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Responder for HbA1c, Proportion of Subjects Achieving Pre-defined HbA1c Targets (HbA1c ≤ 6.5%)

Proportion of subjects achieving HbA1c equal to or below 6.5% after 24 weeks of treatment. (NCT01519674)
Timeframe: After 24 weeks of treatment

Interventionpercentage (%) of subjects (Number)
BID + Met30.6
BID + Sita + Met40.7
OD + Sita + Met25.1

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Responder for HbA1c, Proportion of Subjects Achieving Pre-defined HbA1c Targets (HbA1c < 7.0%)

Proportion of subjects achieving HbA1c below 7.0% after 24 weeks of treatment (NCT01519674)
Timeframe: After 24 weeks of treatment

Interventionpercentage (%) of subjects (Number)
BID + Met49.7
BID + Sita + Met59.8
OD + Sita + Met46.5

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Prandial Plasma Glucose (PPG) Overall Mean Increment.

Estimated overall mean post prandial increment after 24 weeks of treatment. (NCT01519674)
Timeframe: After 24 weeks of treatment

Interventionmmol/L (Least Squares Mean)
BID + Met1.97
BID + Sita + Met1.66
OD + Sita + Met1.88

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Better Targeted Blood Glucose Levels

The current trial is designed to detect a significant difference in the mean glucose levels in the treatment group (NCT01530178)
Timeframe: 1 Year

Interventionmg/dl (Mean)
Sitagliptin 25 mg184.1
Sitagliptin 50 mg179.4
Sitagliptin 100 mg153.6
Placebo181.5

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Percentage of Participants Who Experienced at Least One Adverse Event

(NCT01545388)
Timeframe: Up to 26 weeks

InterventionPercentage of participants (Number)
Metformin 500 mg q.d.65.9
Metformin 250 mg b.i.d.67.7
Placebo60.6

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Number of Participants Who Discontinued Study Drug Due to an Adverse Event

(NCT01545388)
Timeframe: Up to 24 weeks

InterventionParticipants (Number)
Metformin 500 mg q.d.2
Metformin 250 mg b.i.d.3
Placebo1

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Change From Baseline to Week 24 in Hemoglobin A1c (HbA1c)

Based on a constrained longitudinal data analysis (cLDA) model with terms for treatment, other prior antihyperglycemic agent (AHA) therapy status other than sitagliptin (yes/no), study drug regimen (just before meal/after meal), sitagliptin dosage (50 mg/100 mg), time and the interaction of time by treatment, time by other prior AHA therapy status, time by study drug regimen, time by sitagliptin dosage and study drug regimen by sitagliptin dosage, with a constraint that the mean baseline is the same for all treatment groups. (NCT01545388)
Timeframe: Baseline and Week 24

InterventionPercent of glycosylated hemoglobin (Least Squares Mean)
Metformin 500 mg q.d.-0.434
Metformin 250 mg b.i.d.-0.587
Placebo0.091

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Change From Baseline to Week 24 in Fasting Plasma Glucose (FPG)

Based on a cLDA model with terms for treatment, other prior AHA therapy status other than sitagliptin (yes/no), study drug regimen (just before meal/after meal), sitagliptin dosage (50 mg/100 mg), time and the interaction of time by treatment, time by other prior AHA therapy status, time by study drug regimen, time by sitagliptin dosage and study drug regimen by sitagliptin dosage, with a constraint that the mean baseline is the same for all treatment groups. (NCT01545388)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Metformin 500 mg q.d.-9.02
Metformin 250 mg b.i.d.-11.27
Placebo7.32

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Change From Baseline in Glycosylated Hemoglobin (HbA1c)

The change in the value of glycosylated hemoglobin (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) collected at Week 24 relative to Baseline. A Mixed Model Repeated Measures (MMRM) model was used for analysis with treatment, country, schedule, visit and visit by treatment interaction as fixed factors and with Baseline value and Baseline value by visit interaction as covariates with an unstructured covariance structure. (NCT01549964)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Placebo-0.19
Sitagliptin 100 mg-1.07
Fasiglifam 25 mg-0.75
Fasiglifam 50 mg-1.01

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Change From Baseline in Fasting Plasma Glucose (FPG)

The change between FPG collected at week 24 relative to Baseline. A MMRM model was used for analysis with treatment, country, schedule, visit and visit by treatment interaction as fixed factors and with Baseline value and Baseline value by visit interaction as covariates with an unstructured covariance structure. (NCT01549964)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Placebo-1.6
Sitagliptin 100 mg-21.7
Fasiglifam 25 mg-26.9
Fasiglifam 50 mg-32.9

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Incidence of HbA1c <7%

Incidence (percentage) of participants with glycosylated hemoglobin (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) less than 7% at Week 24. (NCT01549964)
Timeframe: 24 Weeks

Interventionpercentage of participants (Number)
Placebo14.9
Sitagliptin 100 mg42.8
Fasiglifam 25 mg24.3
Fasiglifam 50 mg37.0

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Inflammatory Biomarker 3: Serum D-dimer Concentration

There are 3 levels of the primary outcome measure, hsCRP, IL-6, and D-dimer (NCT01552694)
Timeframe: 2 months

,
Interventionµg FEU/mL (Mean)
BaselineWeek 8
Placebo0.280.31
Sitagliptin0.320.33

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Inflammatory Biomarker 2: Plasma IL-6 Concentration

There are 3 levels of the primary outcome measure; hsCRP, IL-6, and D-dimer concentrations measured at baseline and week 8 (NCT01552694)
Timeframe: 2 months

,
Interventionpg/mL (Mean)
BaselineWeek 8
Placebo2.612.65
Sitagliptin1.361.30

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Inflammatory Biomarker 1: Plasma hsCRP Concentration

Fasting serum and plasma samples obtained at baseline and week 8 are batched for ELISA analysis (end of sudy) of hsCRP, IL-6 and D-dimer concentrations. (NCT01552694)
Timeframe: 2 months

,
Interventionmg/L (Mean)
BaselineWeek 8
Placebo5.47.4
Sitagliptin3.42.9

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Percent Change in Blood Endothelial Progenitor Cells

Monocytes (PBMC) are isolated from 20 mL blood. CD34+/VEGFR2+/KDR+ monocytes represent cell markers for endothelial progenitor cells (EPC). CD34+/VEGFR2+/KDR+ monocytes are counted (flow cytometry) and expressed as a percentage of PBMC number. Percent change between population averages from baseline to 2 months for the EPC/PBMC ratio is calculated and reported as the outcome measure. (NCT01552694)
Timeframe: Baseline to 2 months

InterventionPercent change (Number)
Sitagliptin0.3
Placebo-0.2

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Fold Change in Adipose Inflammation Marker CCL2 (MCP-1) mRNA Expression

Adipose tissue from obese, insulin resistant subjects is characterized by increased macrophage infiltration and overexpression of inflammatory cytokines/chemokines. In adipose samples, mRNA expression for the macrophage inflammation marker CCL2 (MCP-1) was quantified. Fold change between population averages from baseline to 2 months for adipose macrophage CCL2 (MCP-1) mRNA expression is the outcome measure. (NCT01552694)
Timeframe: Baseline to 2 months

Interventionfold change (Number)
Sitagliptin-2.5
Placebo-0.4

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AUC 0-24 of Metformin Following Single Administration of Sitagliptin/Metformin XR

In this study, metformin products were withheld 24 hours prior to sitagliptin/metformin XR administration and were permitted to re-initiate 24 hours post study drug administration. Due different units of measure for sitagliptin and metformin, sitagliptin data are presented in another endpoint. (NCT01557504)
Timeframe: Pre-dose, and 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, and 24 hours post-dose

Interventionng*hr/mL (Geometric Mean)
Metformin14200

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AUC 0-24 of Sitagliptin Following Single Administration of Sitagliptin/Metformin XR

Due different units of measure for sitagliptin and metformin, metformin data are presented in another endpoint. (NCT01557504)
Timeframe: Pre-dose, and 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, and 24 hours post-dose

InterventionnM*hr (Geometric Mean)
Sitagliptin5310

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Cmax of Metformin Following Single Dose Administration of Sitagliptin/Metformin XR

In this study, metformin products were withheld 24 hours prior to sitagliptin/metformin XR administration and were permitted to re-initiate 24 hours post study drug administration. Due different units of measure for sitagliptin and metformin, sitagliptin data are presented in another endpoint. (NCT01557504)
Timeframe: Pre-dose, and 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, and 72 hours post-dose

Interventionng/mL (Geometric Mean)
Metformin1490

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Cmax of Sitagliptin Following Single Dose Administration of Sitagliptin/Metformin XR

Due different units of measure for sitagliptin and metformin, metformin data are presented in another endpoint. (NCT01557504)
Timeframe: Pre-dose, and 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, and 72 hours post-dose

InterventionnM (Geometric Mean)
Sitagliptin757

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Number of Participants Who Experienced an Abnormal Vital Sign Value

Vital sign measurements included blood pressure, heart rate, respiratory rate, and oral temperature. (NCT01557504)
Timeframe: Up to 23 days (including approximately 10 to 14 days after the last dose of study drug)

InterventionParticipants (Number)
Sitagliptin0
Placebo0

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Number of Participants Who Successfully Swallowed Study Medication (Med) on Day 2

The Swallowing Ability Questionnaire was completed on Day 2 after the participant received two matching placebo tablets (excluding marking) following consumption of a low- to moderate-fat meal in pediatric participants aged 10 to 17 years. The questionnaire consisted of five parts: could only swallow study med with help, easy to start swallowing study med, easy to swallow study med, felt like study med got stuck in throat, and had to swallow study med more than once. The number of participants who strongly agreed or agreed in each of the five parts is reported. (NCT01557504)
Timeframe: Day 2

InterventionParticipants (Number)
Strongly Agreed: Could Only Swallow Med With HelpAgreed: Could Only Swallow Med With HelpStrongly Agreed: Easy to Start Swallowing MedAgreed: Easy to Start Swallowing MedStrongly Agreed: Easy to Swallow MedAgreed: Easy to Swallow MedStrongly Agreed: Felt Like Med Got Stuck in ThroatAgreed: Felt Like Med Got Stuck in ThroatStrongly Agreed: Had to Swallow Med More Than OnceAgreed: Had to Swallow Med More Than Once
All Treated Participants67101213100423

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Number of Participants Who Successfully Swallowed Study Med on Day 9

The Swallowing Ability Questionnaire was completed on Day 9 after the participant received two matching placebo tablets (excluding marking) following consumption of a low- to moderate-fat meal in pediatric participants aged 10 to 17 years. The questionnaire consisted of five parts: could only swallow study med with help, easy to start swallowing study med, easy to swallow study med, felt like study med got stuck in throat, and had to swallow study med more than once. The number of participants who strongly agreed or agreed in each of the five parts is reported. (NCT01557504)
Timeframe: Day 9

InterventionParticipants (Number)
Strongly Agreed: Could Only Swallow Med With HelpAgreed: Could Only Swallow Med With HelpStrongly Agreed: Easy to Start Swallowing MedAgreed: Easy to Start Swallowing MedStrongly Agreed: Easy to Swallow MedAgreed: Easy to Swallow MedStrongly Agreed: Felt Like Med Got Stuck in ThroatAgreed: Felt Like Med Got Stuck in ThroatStrongly Agreed: Had to Swallow Med More Than OnceAgreed: Had to Swallow Med More Than Once
All Treated Participants9591312111125

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Number of Participants Who Successfully Swallowed Study Med on Day 6

The Swallowing Ability Questionnaire was completed on Day 6 after the participant received two matching placebo tablets (excluding marking) following consumption of a low- to moderate-fat meal in pediatric participants aged 10 to 17 years. The questionnaire consisted of five parts: could only swallow study med with help, easy to start swallowing study med, easy to swallow study med, felt like study med got stuck in throat, and had to swallow study med more than once. The number of participants who strongly agreed or agreed in each of the five parts is reported. (NCT01557504)
Timeframe: Day 6

InterventionParticipants (Number)
Strongly Agreed: Could Only Swallow Med With HelpAgreed: Could Only Swallow Med With HelpStrongly Agreed: Easy to Start Swallowing MedAgreed: Easy to Start Swallowing MedStrongly Agreed: Easy to Swallow MedAgreed: Easy to Swallow MedStrongly Agreed: Felt Like Med Got Stuck in ThroatAgreed: Felt Like Med Got Stuck in ThroatStrongly Agreed: Had to Swallow Med More Than OnceAgreed: Had to Swallow Med More Than Once
All Treated Participants57101111120325

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Number of Participants Who Successfully Swallowed Study Med on Day 4

The Swallowing Ability Questionnaire was completed on Day 4 after the participant received two matching placebo tablets (excluding marking) following consumption of a low- to moderate-fat meal in pediatric participants aged 10 to 17 years. The questionnaire consisted of five parts: could only swallow study med with help, easy to start swallowing study med, easy to swallow study med, felt like study med got stuck in throat, and had to swallow study med more than once. The number of participants who strongly agreed or agreed in each of the five parts is reported. (NCT01557504)
Timeframe: Day 4

InterventionParticipants (Number)
Strongly Agreed: Could Only Swallow Med With HelpAgreed: Could Only Swallow Med With HelpStrongly Agreed: Easy to Start Swallowing MedAgreed: Easy to Start Swallowing MedStrongly Agreed: Easy to Swallow MedAgreed: Easy to Swallow MedStrongly Agreed: Felt Like Med Got Stuck in ThroatAgreed: Felt Like Med Got Stuck in ThroatStrongly Agreed: Had to Swallow Med More Than OnceAgreed: Had to Swallow Med More Than Once
All Treated Participants668148150405

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Tmax of Sitagliptin and Metformin Following Single Dose Administration of Sitagliptin/Metformin XR

In this study, metformin products were withheld 24 hours prior to sitagliptin/metformin XR administration and were permitted to re-initiate 24 hours post study drug administration. (NCT01557504)
Timeframe: Pre-dose, and 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, and 72 hours post-dose

InterventionHour (Median)
Sitagliptin1.52
Metformin5.00

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Number of Participants Who Experienced an Adverse Event (AE)

An AE was defined as any untoward medical occurrence in the form of signs, symptoms, abnormal laboratory findings, or diseases that emerges or worsens relative to baseline during a clinical study with an Investigational Medicinal Product (IMP), regardless of causal relationship and even if no IMP has been administered. (NCT01557504)
Timeframe: Up to 23 days (including approximately 10 to 14 days after the last dose of study drug)

InterventionParticipants (Number)
Sitagliptin5
Placebo5

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Number of Participants Who Discontinued Study Drug Due to an AE

An AE was defined as any untoward medical occurrence in the form of signs, symptoms, abnormal laboratory findings, or diseases that emerges or worsens relative to baseline during a clinical study with an IMP, regardless of causal relationship and even if no IMP has been administered. (NCT01557504)
Timeframe: Up to 9 days

InterventionParticipants (Number)
Sitagliptin0
Placebo0

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Apparent Terminal Half Life (t1/2) of Sitagliptin Following Single Dose Administration of Sitagliptin/Metformin XR

In this study, metformin products were withheld 24 hours prior to sitagliptin/metformin XR administration and were permitted to re-initiate 24 hours post study drug administration. Owing to resumption of therapeutic metformin administration 24 hours after sitagliptin/metformin XR administration for all participants, metformin pharmacokinetic analyses were restricted to Cmax, Tmax and AUC0-24hr. Therefore, metformin arm is not included in this endpoint. (NCT01557504)
Timeframe: Pre-dose, and 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, and 72 hours post-dose

InterventionHour (Geometric Mean)
Sitagliptin10.0

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Area Under the Curve 0 to Infinity (AUC 0-∞) of Sitagliptin Following Single Administration of Sitagliptin/Metformin XR

In this study, metformin products were withheld 24 hours prior to sitagliptin/metformin XR administration and were permitted to re-initiate 24 hours post study drug administration. Owing to resumption of therapeutic metformin administration 24 hours after sitagliptin/metformin XR administration for all participants, metformin pharmacokinetic analyses were restricted to Cmax, Tmax and AUC0-24hr. Therefore, metformin arm is not included in this endpoint. (NCT01557504)
Timeframe: Pre-dose, and 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, and 72 hours post-dose

InterventionnM*hr (Geometric Mean)
Sitagliptin6020

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Area Under the Curve 0 to Last (AUC 0-last) of Sitagliptin Following Single Administration of Sitagliptin/Metformin XR

In this study, metformin products were withheld 24 hours (hrs) prior to sitagliptin/metformin XR administration and were permitted to re-initiate 24 hrs post study drug administration. Owing to resumption of therapeutic metformin administration 24 hrs after sitagliptin/metformin XR administration for all participants, metformin pharmacokinetic analyses were restricted to maximum plasma concentration (Cmax), time to maximum plasma concentration (Tmax) and area under the curve 0 to 24 hrs (AUC0-24hr). Therefore, metformin arm is not included in this endpoint. (NCT01557504)
Timeframe: Pre-dose, and 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, and 72 hours post-dose

InterventionnM*hr/mL (Geometric Mean)
Sitagliptin5940

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Percent Inhibition of Dipeptidyl Peptidase IV (DPP-4) Activity at Trough

Percent inhibition of DPP-4 activity at 24 hours after the Day 5 morning dose (i.e., at trough) was determined by analysis of blood samples collected from the study participants. (NCT01582308)
Timeframe: 24 hours following the final morning dose on Day 5

InterventionPercent inhibition (Least Squares Mean)
Sitagliptin 100 mg91.73
Saxagliptin 5 mg73.50
Vildagliptin 50 mg28.88
Vildagliptin 50 mg BID90.63
Placebo3.49

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Pharmacokinetic Analysis: Area Under the Curve 0-12 Hours (AUC 0-12hr) for Vildagliptin 50 mg BID

AUC 0-12hr is the area under the plasma drug concentration-time curve calculated for the 12 hour interval after the Day 5 morning dose for the vildagliptin 50 mg BID dose only. (NCT01582308)
Timeframe: Predose (0 hours) and 0.5, 1, 2, 4, 8 and 12 hours after the morning dose on Day 5

InterventionnM*hr (Geometric Mean)
Vildagliptin 50 mg BID3720

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Pharmacokinetic Analysis: Area Under the Curve 0-24 Hours (AUC 0-24hr)

AUC 0-24hr is the area under the plasma drug concentration-time curve calculated for the 24 hour interval after the Day 5 morning dose. (NCT01582308)
Timeframe: Predose (0 Hours) and 0.5, 1, 2, 4, 8, 12, 13 (vildagliptin 50 mg BID only), 14 (vildagliptin 50 mg BID only), 16, 20 and 24 hours after the morning dose on Day 5

InterventionnM*hr (Geometric Mean)
Sitagliptin 100 mg7070
Saxagliptin 5 mg370
Vildagliptin 50 mg3100
Vildagliptin 50 mg BID6600

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Pharmacokinetic Analysis: Peak Plasma Drug Concentration (Cmax)

Measurement of the peak plasma drug concentration following the Day 5 morning dose. (NCT01582308)
Timeframe: Predose (0 hours) and 0.5, 1, 2, 4, 8, 12, 13 (vildagliptin 50 mg BID only), 14 (vildagliptin 50 mg BID only), 16, 20, 24, 36, 48 and 96 hours after the morning dose on Day 5

InterventionnM (Geometric Mean)
Sitagliptin 100 mg724
Saxagliptin 5 mg88.8
Vildagliptin 50 mg586
Vildagliptin 50 mg BID759

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Pharmacokinetic Analysis: Time to the Peak Plasma Drug Concentration (Tmax)

Measurement of the time to the peak plasma drug concentration following the Day 5 morning dose. (NCT01582308)
Timeframe: Predose (0 hours) and 0.5, 1, 2, 4, 8, 12, 13 (vildagliptin 50 mg BID only), 14 (vildagliptin 50 mg BID only), 16, 20, 24, 36, 48 and 96 hours after the morning dose on Day 5

Interventionhr (Median)
Sitagliptin 100 mg4
Saxagliptin 5 mg1
Vildagliptin 50 mg1
Vildagliptin 50 mg BID1

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Number of Participants Who Experienced an Adverse Event

An adverse event is any untoward medical occurrence in a participant administered study drug which does not necessarily have a causal relationship with the treatment. Adverse events may include the onset of new illness and the exacerbation of pre-existing conditions. (NCT01590771)
Timeframe: Up to 26 weeks

InterventionParticipants (Number)
Sitagliptin106
Placebo98

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Number of Participants Who Discontinued Study Drug Due to an Adverse Event

An adverse event is any untoward medical occurrence in a participant administered study drug which does not necessarily have a causal relationship with the treatment. Adverse events may include the onset of new illness and the exacerbation of pre-existing conditions. (NCT01590771)
Timeframe: Up to 24 weeks

InterventionParticipants (Number)
Sitagliptin3
Placebo7

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Change From Baseline in FPG Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea Alone or in Combination With Metformin

This change from baseline reflects the FPG level at Week 24 minus the FPG level at Week 0. (NCT01590771)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-24.4
Placebo-7.7

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Change From Baseline in FPG Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea Alone

This change from baseline reflects the FPG level at Week 24 minus the FPG level at Week 0. (NCT01590771)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-26.3
Placebo-9.3

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Change From Baseline in 2-hr PMG Levels at Week 24 in Participants Receiving Sitagliptin and a Sulfonylurea in Combination With Metformin

This change from baseline reflects the 2-hr PMG level at Week 24 minus the 2-hr PMG level at Week 0. (NCT01590771)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-33.4
Placebo-6.2

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Change From Baseline in 2-hr PMG Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea Alone

This change from baseline reflects the 2-hr PMG level at Week 24 minus the 2-hr PMG level at Week 0. (NCT01590771)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-49.5
Placebo-11.9

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Change From Baseline in A1C Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea Alone

A1C was measured as a percent. This change from baseline reflects the A1C percent at Week 24 minus the A1C percent at Week 0. (NCT01590771)
Timeframe: Baseline and Week 24

InterventionPercent of glycosylated hemoglobin (A1C) (Least Squares Mean)
Sitagliptin-0.85
Placebo-0.05

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Change From Baseline in A1C Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea Alone or in Combination With Metformin

A1C was measured as a percent. This change from baseline reflects the A1C percent at Week 24 minus the A1C percent at Week 0. (NCT01590771)
Timeframe: Baseline and Week 24

InterventionPercent of glycosylated hemoglobin (A1C) (Least Squares Mean)
Sitagliptin-0.88
Placebo-0.27

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Change From Baseline in A1C Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea in Combination With Metformin

A1C was measured as a percent. This change from baseline reflects the A1C percent at Week 24 minus the A1C percent at Week 0. (NCT01590771)
Timeframe: Baseline and Week 24

InterventionPercent of glycosylated hemoglobin (A1C) (Least Squares Mean)
Sitagliptin-0.86
Placebo-0.45

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Change From Baseline in 2-hr PMG Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea Alone or in Combination With Metformin

This change from baseline reflects the 2-hr PMG level at Week 24 minus the 2-hr PMG level at Week 0. (NCT01590771)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-40.7
Placebo-7.7

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Change From Baseline in FPG Levels at Week 24 in Participants Receiving Sitagliptin and Sulfonylurea in Combination With Metformin

This change from baseline reflects the FPG level at Week 24 minus the FPG level at Week 0. (NCT01590771)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-22.2
Placebo-5.7

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Number of Participants With One or More Adverse Events

An adverse event (AE) is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure, that occurs during the course of the study. (NCT01590797)
Timeframe: Up to Week 26

InterventionParticipants (Number)
Sitagliptin126
Placebo116

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Number of Participants Discontinuing Study Medication Due to an AE

An AE is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure, that occurs during the course of the study. (NCT01590797)
Timeframe: Up to Week 24

InterventionParticipants (Number)
Sitagliptin4
Placebo2

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Change From Baseline in Hemoglobin A1C (HbA1C) Levels at Week 24 in Participants Receiving Insulin Alone or in Combination With Metformin

(NCT01590797)
Timeframe: Baseline and Week 24

InterventionA1C % (Least Squares Mean)
Sitagliptin-0.67
Placebo-0.32

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Change From Baseline in HbA1C Levels at Week 24 in Participants Receiving Insulin in Combination With Metformin

(NCT01590797)
Timeframe: Baseline and Week 24

InterventionA1C % (Least Squares Mean)
Sitagliptin-0.72
Placebo-0.34

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Change From Baseline in 2-Hour Post Meal Glucose Levels at Week 24 in Participants Receiving Insulin Alone or in Combination With Metformin

(NCT01590797)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-47.9
Placebo-21.3

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Apolipoprotein B100 Production Rate After Acute Oral Administration of 100mg Sitagliptin (Compared to Placebo)

Apolipoprotein B100 turnover was measured in a 10-hour kinetic study with in vivo tracer techniques and mathematical modeling to calculate production rates. Studies were performed under conditions of a pancreatic clamp and a steady state fed state in volunteers receiving single oral dose of either 100mg sitagliptin or matching placebo. (NCT01600703)
Timeframe: 10 hours

Interventionmg/kg/day (Mean)
Placebo17.6
Sitagliptin20.4

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Apolipoprotein B48 Production Rate After Acute Oral Administration of 100mg Sitagliptin (Compared to Placebo)

Apolipoprotein B48 turnover was measured in a 10-hour kinetic study with in vivo tracer techniques and mathematical modeling to calculate production rates. Studies were performed under conditions of a pancreatic clamp and a steady state fed state in volunteers receiving single oral dose of either 100mg sitagliptin or matching placebo. (NCT01600703)
Timeframe: 10 hours

Interventionug/kg/day (Mean)
Placebo122.9
Sitagliptin60.6

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Change From Baseline in Insulin Sensitivity in Patients With Different BMI

The insulin sensitivity was detected by evaluating the glucose infusion rate (GIR) with euglycemic hyperinsulinemic clamp test. (NCT01610154)
Timeframe: Baseline to 12 weeks

Interventionmg/kg/min (Median)
Non-obese Group0.42
Obese Group0.72

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Change From Baseline in Fasting Plasma Glucose (FPG)

(NCT01610154)
Timeframe: Baseline to 12 weeks

Interventionmmol/L (Mean)
Sitagliptin-1.99

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Change From Baseline in Hemoglobin A1c (HbA1c)

(NCT01610154)
Timeframe: Baseline to 12 weeks

Interventionpercentage (Mean)
Sitagliptin-1.08

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Change From Baseline in Insulin Sensitivity

The insulin sensitivity was detected by evaluating the glucose infusion rate (GIR) with euglycemic hyperinsulinemic clamp test. (NCT01610154)
Timeframe: Baseline to 12 weeks

Interventionmg/kg/min (Median)
Sitagliptin0.64

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Change From Baseline in Pancreatic α Cell Function

The glucagon-AUC was adopted to show pancreatic α cell function. (NCT01610154)
Timeframe: Baseline to 12 weeks

Interventionmin∙pg/ml (Mean)
Sitagliptin-27.8

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Change From Baseline in Pancreatic α Cell Function in Patients With Different BMI

The glucagon-AUC was adopted to show pancreatic α cell function. (NCT01610154)
Timeframe: Baseline to 12 weeks

Interventionmin∙pg/ml (Mean)
Non-obese Group13.6
Obese Group-54.0

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Change From Baseline in Pancreatic β Cell Function

The early phase insulin response (△I30/△G30) was adopted to determine β cell function. (NCT01610154)
Timeframe: Baseline to 12 weeks

Interventionμu/ml/mmol (Median)
Sitagliptin2.53

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Change From Baseline in Pancreatic β Cell Function in Patients With Different BMI

The early phase insulin response (△I30/△G30) was adopted to determine β cell function. (NCT01610154)
Timeframe: Baseline to 12 weeks

Interventionμu/ml/mmol (Median)
Non-obese Group2.30
Obese Group2.85

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Change From Baseline in Postprandial Plasma Glucose (PPG)

(NCT01610154)
Timeframe: Baseline to 12 weeks

Interventionmmol/L (Mean)
Sitagliptin-4.69

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Percentage of Subjects Achieving HbA1c <7% at Week 28

Percentage of subjects achieving HbA1c target values of < 7.0% at Week 28/Study Termination. (NCT01652729)
Timeframe: Baseline to Week 28

,,
Interventionpercentage of subjects (Number)
Baseline YesBaseline NoWeek 28 YesWeek 28 No
Active Comparator: Sitagliptin1.698.432.068.0
Experimental: Exenatide3.396.743.156.9
Placebo Comparator: Placebo3.396.724.675.4

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Change in HbA1c (Glycosylated Hemoglobin) From Baseline to Week 28

Absolute change in HbA1c from baseline (Day 1, Visit 3) to Week 28/Study Termination (Visit 11). Hypothesis testing on the primary endpoint followed a serial gated procedure with all tests carried out at a 2-sided significance level of 0.05 to protect the family-wise error rate. These tests were conducted sequentially, and are presented in the statistical analysis section below in the order in which they were performed; each test was the gatekeeper of later tests. (NCT01652729)
Timeframe: Baseline to Week 28

Interventionpercentage of total hemoglobin (Least Squares Mean)
Experimental: Exenatide-1.13
Active Comparator: Sitagliptin-0.75
Placebo Comparator: Placebo-0.40

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Change in Fasting Plasma Glucose Concentrations From Baseline to Week 28

The change in fasting plasma glucose concentrations from baseline (Day 1) to Week 28/Study Termination. (NCT01652729)
Timeframe: Baseline to Week 28

Interventionmg/dL (Least Squares Mean)
Experimental: Exenatide-21.3
Active Comparator: Sitagliptin-11.3
Placebo Comparator: Placebo9.6

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Change in Body Weight (kg) From Baseline to Week 28

The change in body weight (kg) from baseline (Day 1) to Week 28/Study Termination. (NCT01652729)
Timeframe: Baseline to Week 28

Interventionkg (Least Squares Mean)
Experimental: Exenatide-1.12
Active Comparator: Sitagliptin-1.19
Placebo Comparator: Placebo0.15

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Change in 2-hour Postprandial Glucose Concentrations From Baseline to Week 16 (Visit 8)

The change in 2-hour postprandial plasma glucose from baseline (Day 1) to Visit 8 (Week 16) was analyzed using a general linear model including treatment, and baseline HbA1c stratum (< 9% or ≥ 9%) as fixed factors, and the baseline 2-hour postprandial plasma glucose concentrations as a covariate. (NCT01652729)
Timeframe: Baseline to Week 16

Interventionmg/dL (Least Squares Mean)
Experimental: Exenatide-59.57
Active Comparator: Sitagliptin-23.61
Placebo Comparator: Placebo-38.68

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Percent Change From Baseline in Total Cholesterol (TC) at Week 16

Percent change from baseline was calculated as the Week 16 value minus the Week 0 value, divided by the Week 0 value ×100%. (NCT01678820)
Timeframe: Baseline and Week 16

InterventionPercent change (Least Squares Mean)
Sitagliptin/Simvastatin FDC-18.4
Sitagliptin-0.4
Simvastatin-18.4

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Number of Participants Who Experienced at Least One Adverse Event (AE)

Excludes data after rescue therapy. Adverse event is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the Sponsor's product, whether or not considered related to the use of the product. (NCT01678820)
Timeframe: Up to 16 weeks for non-serious AEs, up to 18 weeks for serious AEs

InterventionParticipants (Number)
Sitagliptin/Simvastatin FDC13
Sitagliptin13
Simvastatin17

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Number of Participants Who Discontinued Study Drug Due to an Adverse Event

Excludes data after rescue therapy. Adverse event is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the Sponsor's product, whether or not considered related to the use of the product. (NCT01678820)
Timeframe: Up to 16 weeks

InterventionParticipants (Number)
Sitagliptin/Simvastatin FDC2
Sitagliptin1
Simvastatin2

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Change From Baseline in A1C at Week 16 (Sitagliptin/Simvastatin FDC vs. Simvastatin)

A1C is measured as percent. Thus, this change from baseline reflects the Week 16 A1C percent minus the Week 0 A1C percent. This primary outcome measure only includes results for sitagliptin/simvastatin FDC vs. simvastatin. Results for sitagliptin are presented above under primary outcome measures. (NCT01678820)
Timeframe: Baseline and Week 16

InterventionPercent (Least Squares Mean)
Sitagliptin/Simvastatin FDC-0.41
Simvastatin0.21

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Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) at Week 16

Percent change from baseline was calculated as the Week 16 value minus the Week 0 value, divided by the Week 0 value ×100%. (NCT01678820)
Timeframe: Baseline and Week 16

InterventionPercent change (Least Squares Mean)
Sitagliptin/Simvastatin FDC-21.6
Sitagliptin4.0
Simvastatin-26.9

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Percent Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C) at Week 16

Percent change from baseline was calculated as the Week 16 value minus the Week 0 value, divided by the Week 0 value ×100%. (NCT01678820)
Timeframe: Baseline and Week 16

InterventionPercent change (Least Squares Mean)
Sitagliptin/Simvastatin FDC2.5
Sitagliptin2.0
Simvastatin2.1

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Percent Change From Baseline in Apolipoprotein B (Apo B) at Week 16

Percent change from baseline was calculated as the Week 16 value minus the Week 0 value, divided by the Week 0 value ×100%. (NCT01678820)
Timeframe: Baseline and Week 16

InterventionPercent change (Least Squares Mean)
Sitagliptin/Simvastatin FDC-16.9
Sitagliptin3.3
Simvastatin-19.8

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 16

Change from baseline reflects the Week 16 value minus the Week 0 value. (NCT01678820)
Timeframe: Baseline and Week 16

Interventionmg/dL (Least Squares Mean)
Sitagliptin/Simvastatin FDC-7.9
Sitagliptin-9.6
Simvastatin21.3

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Change From Baseline in Hemoglobin A1C (A1C) at Week 16 (Sitagliptin/Simvastatin FDC vs. Sitagliptin)

A1C is measured as percent. Thus, this change from baseline reflects the Week 16 A1C percent minus the Week 0 A1C percent. This primary outcome measure only includes results for sitagliptin/simvastatin FDC vs. sitagliptin. Results for simvastatin are presented below under secondary outcome measures. (NCT01678820)
Timeframe: Baseline and Week 16

InterventionPercent (Least Squares Mean)
Sitagliptin/Simvastatin FDC-0.41
Sitagliptin-0.59

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Percentage of Participants With A1C Level <7% at Week 16

Percentage of participants achieving glycemic goal (A1C <7%) after 16 weeks of treatment. Data as observed. (NCT01678820)
Timeframe: Week 16

InterventionPercentage of participants (Number)
Sitagliptin/Simvastatin FDC29.9
Sitagliptin29.6
Simvastatin17.6

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Percent Change From Baseline in Non-high Density Lipoprotein Cholesterol (Non-HDL-C) at Week 16

Percent change from baseline was calculated as the Week 16 value minus the Week 0 value, divided by the Week 0 value ×100%. (NCT01678820)
Timeframe: Baseline and Week 16

InterventionPercent change (Least Squares Mean)
Sitagliptin/Simvastatin FDC-23.9
Sitagliptin0.6
Simvastatin-24.2

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Percent Change From Baseline in Very Low-density Lipoprotein Cholesterol (VLDL-C) at Week 16

Percent change from baseline was calculated as the Week 16 value minus the Week 0 value, divided by the Week 0 value ×100%. (NCT01678820)
Timeframe: Baseline and Week 16

InterventionPercent change (Least Squares Mean)
Sitagliptin/Simvastatin FDC-17.5
Sitagliptin12.9
Simvastatin-2.2

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Percent Change From Baseline in Triglycerides (TG) at Week 16

Percent change from baseline was calculated as the Week 16 value minus the Week 0 value, divided by the Week 0 value ×100%. (NCT01678820)
Timeframe: Baseline and Week 16

InterventionPercent change (Mean)
Sitagliptin/Simvastatin FDC-20.4
Sitagliptin-4.9
Simvastatin-10.1

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Percentage Change From Baseline of Pro-insulin/C-peptide Ratios After 8 Weeks of Treatment Period 1 & Period 2

Percentage Change from baseline of pro-insulin/C-peptide ratios after 8 weeks of treatment Period 1 & Period 2 Higher pro-insulin / C-peptide ratios (expressing disproportional hyperproinsulinemia) may be associated with increasing beta cell dysfunction and more inefficient pro-insulin processing (NCT01686932)
Timeframe: Baseline, after 8 weeks Period 1 & Period 2

InterventionPercentage Change (Mean)
Vitagliptin-0.34
Sitagliptin-0.31

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Change From Baseline of Inflammatory Biomarkers Interleukin 6 (IL-6) After 8 Weeks of Treatment in Period 1 & Period 2

The inflammatory biomarkers IL-6 was assessed at baseline and after 8 weeks of treatment Period 1 & Period 2 (NCT01686932)
Timeframe: Baseline, after 8 weeks Period 1 & Period 2

Interventionpg/L (Mean)
Vitagliptin0.40
Sitagliptin0.08

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Change From Baseline of Inflammatory Biomarkers High Sensitivity C-reactive Protein (hsCRP) After 8 Weeks of Treatment in Period 1 & Period 2

The inflammatory biomarkers hsCRP was assessed at baseline and after 8 weeks of treatment Period 1 & Period 2 (NCT01686932)
Timeframe: Baseline, after 8 weeks Period 1 & Period 2

Interventionmg/L (Mean)
Vitagliptin0.79
Sitagliptin0.60

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Number of Participants With ECG Abnormalities Depending on Hypoglycemic Events After 8 Weeks of Treatment Period 1 & Period 2

ECG abnormalities are defined as either: • Occurrence of >30 ventricular extrasystoles (VES) per hour or • Occurrence of ≥2 consecutive VES (Couplets) or • Occurrence of ≥3 consecutive VES (Triplets) or • QT-time corrected for heart rate (QTc) >440 ms. after 8 weeks of treatment Period 1 & Period 2 (NCT01686932)
Timeframe: after 8 weeks of treatment Period 1 & Period 2

,
Interventionparticipants (Number)
Patients with hypoglycemia (n=21,17)Patients without hypoglycemia (n=28,32)
Sitagliptin1024
Vitagliptin1419

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Number of Occurrence of Pre-defined ECG Findings During 4 Days of Continuous ECG Monitoring at Baseline and in the 8th Week of Periods 1 and 2

Number of Occurrence of pre-defined ECG findings during 4 days of continuous ECG monitoring at baseline and in the 8th week of Periods 1 and 2. ECG data were continuously recorded and analyzed over a period of 4 days simultaneously with continuous glucose monitoring. It assessed number of any Vertical Electric(al) Sounding (VES), number of 2 consecutive VES [couplets], and number of >3 consecutive VES [salves] (NCT01686932)
Timeframe: after 8 weeks Period 1 & Period 2

,
Interventionnumber of occurrence (Mean)
# any VES Per.1 n=23, 25# any VES Per.2 n=25, 23# couplets VES Per.1 n=23, 25# couplets VES Per.2 n=25, 23# salves VES Per.1 n=23, 25# salves VES Per.2 n=25, 23
Sitagliptin2786.71060.2115.02.415.80.9
Vitagliptin879.74389.912.86.71.00.8

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Number of Hypoglycemic Events During Vildagliptin Treatment Compared to Sitagliptin Treatment.

Hypoglycemic events are defined as blood glucose values <70 mg/dL measured by a self-monitored blood glucose (SMBG) or continuous glucose monitoring (CGM) measurement regardless of any symptoms suggestive of low blood glucose. (NCT01686932)
Timeframe: after 8 weeks period 1 and Period 2

,
Interventionnumber of hypoglycemic events (Number)
continuous glucose monitoring (CGM)self-monitored blood glucose (SMBG)
Sitagliptin3713
Vitagliptin6929

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Number of Severe Hypoglycemic Events During Vildagliptin Treatment Compared to Sitagliptin Treatment After 8 Weeks of Treatment in Period 1 and Period 2

Severe hypoglycemic events are defined as any episode requiring the assistance of another party or measured plasma glucose levels of <40 mg /dL. Assessed by self-monitored blood glucose (SMBG)After 8 weeks of treatment in Period 1 and Period 2 (NCT01686932)
Timeframe: after 8 weeks Period 1 & Period 2

Interventionsevere hypoglycemic events (Number)
Vitagliptin1
Sitagliptin1

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Mean Duration of Hypoglycemic Events (Min.) Measured With Continuous Glucose Monitoring (CGM) Over 4 Days After 8 Weeks of Treatment for Period 1 & Period 2

the mean duration of hypoglycemic events is detected by continuous glucose monitoring (CGM)measurement. (NCT01686932)
Timeframe: after 8 weeks for Period 1 & Period 2

Interventionminutes (Mean)
Vitagliptin29.1
Sitagliptin28.0

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Mean Amplitudes of Hypoglycemic Events (mmol/L) Measured With Continuous Glucose Monitoring (CGM) Over 4 Days After 8 Weeks of Treatment for Period 1 & Period 2

To evaluate by CGM measurement the grade of severity of hypoglycemia measured as the mean amplitude over 4 days after 8 weeks of treatment in Period 1 & Period 2 (NCT01686932)
Timeframe: after 8 weeks Period 1 & Period 2

Interventionmmol/L (Mean)
Vitagliptin0.2
Sitagliptin0.2

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Hypoglycemic Profile of Vildagliptin Compared to Sitagliptin Over 4 Days After 8 Weeks of Treatment in Period 1 & 2

The hypoglycemic profile is defined as the area under the curve glucose-time profile obtained by continuous glucose monitoring Interstitial glucose values below 3.9 mmol/L (averaged over 5 minutes) were considered relevant for the estimation of the interstitial glucose AUC in the hypoglycemic range These AUC<3.9mmol/L/5min. values were summed up over 4 days (unit: mmol/L/4d) or over 24 hours at measurement Days 2, 3, 4, and 5 (unit: mmol/L/24h). Lower values for AUC reflect less intense hypoglycemia. (NCT01686932)
Timeframe: baseline and 0-24 hours post-dose on Days 2 to 5

Interventionmmol/L/4d (Mean)
Vitagliptin11.2
Sitagliptin5.3

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Glucose Fluctuations During the Day Under Vildagliptin Treatment Compared to Sitagliptin Treatment on Day 2 After 8 Weeks of Treatment Period 1 & Period 2

Glucose fluctuations are assessed by the mean amplitude of glycemic excursions (MAGE) and standard deviations (SD) (Service et al., 1970). on day 2 after 8 weeks of treatment Period 1 & Period 2 (NCT01686932)
Timeframe: Day 2 after 8 weeks of treatment Period 1 & Period 2

Interventionmmol/L (Mean)
Vitagliptin4.7
Sitagliptin4.6

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Aim 1: Percent Change From Baseline in Forearm Blood Flow

Forearm blood flow was determined by strain gauge plethysmography. The percent change from baseline was determined at each timepoint. (NCT01701973)
Timeframe: Percent change from baseline in forearm blood flow at 30 minutes, 60 minutes, 90 minutes, 120 minutes, 150 minutes, 180 minutes.

,,,
Interventionpercent change from baseline (Mean)
30 minutes60 minutes90 minutes120 minutes150 minutes180 minutes
Aim 1: Placebo, Female Participants1.64584.910111.728510.308119.735530.0924
Aim 1: Placebo, Male Participants9.25970.678913.53589.937915.094426.1772
Aim 1: Sitagliptin, Male Participants-.0238-2.88691.521220.118521.601116.8489
Aim 1: Sitagliptin,Female Participants0.48355.341615.919223.224839.926940.6354

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Aim 2: Venous Blood Sampling for Tissue Plasminogen Activator (TPA) Activity Levels

Subjects undergo two study days separated by a washout period. On one study day they received sitagliptin plus pegvisomant and on another sitagliptin plus placebo, in a randomized double-blind fashion. Tissue plasminogen activator activity (tPA) was assessed at each visit. (NCT01701973)
Timeframe: baseline and every 30 minutes until 180 minutes

,
InterventionIU/ml (Mean)
Baseline prior to Arginine30 minutes45 minutes60 minutes90 minutes120 minutes150 minutes180 minutes
Aim 2: Sitagliptin and Pegvisomant, Female Participants0.100.150.170.140.160.160.200.23
Aim 2: Sitagliptin and Placebo, Females in Pegvisomant Group0.240.260.330.270.260.280.310.35

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Aim 2: Percent Change From Baseline in Forearm Vascular Resistance

Subjects undergo two study days separated by a washout period. On one study day they will receive sitagliptin plus another study drug and on another sitagliptin plus placebo, in a randomized double-blind fashion. Forearm blood flow was assessed at each visit every 30 minutes for 3 hours. This was divided into mean arterial pressure to determine forearm vascular resistance. (NCT01701973)
Timeframe: Percent change from baseline in forearm vascular resistance at 30 minutes, 60 minutes, 90 minutes, 120 minutes, 150 minutes, 180 minutes

,,,,,,,,,
Interventionpercent change from baseline (Mean)
30 minutes60 minutes90 minutes120 minutes150 minutes180 minutes
Aim 2: Sitagliptin & Placebo,Females in Pegvisomant Group-3.75-10.973.79-14.57-14.25-17.97
Aim 2: Sitagliptin and Exendin 9-39, Female Participants5.3014.461.76-22.37-20.92-22.58
Aim 2: Sitagliptin and Exendin 9-39, Male Participant0.57-11.80-14.02-16.20-32.30-34.69
Aim 2: Sitagliptin and LNMMA, Female Participants-8.678.77-4.890.99-13.25-10.25
Aim 2: Sitagliptin and LNMMA, Male Participants-9.87-9.75-23.34-24.81-20.62-22.56
Aim 2: Sitagliptin and Pegvisomant, Female Participants-20.00-4.05-25.28-32.39-30.12-25.00
Aim 2: Sitagliptin and Placebo, Females in Exendin 9-39 Group4.53-4.264.82-13.16-8.49-16.76
Aim 2: Sitagliptin and Placebo, Females in LNMMA Group8.9851.8239.2421.9842.275.28
Aim 2: Sitagliptin and Placebo, Male in Exendin 9-39 Group27.776.7322.4526.68-1.321.69
Aim 2: Sitagliptin and Placebo, Males in LNMMA Group-14.60-2.42-16.75-28.34-32.11-19.52

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Aim 2: Percent Change From Baseline in Forearm Blood Flow

Subjects undergo two study days separated by a washout period. On one study day they received sitagliptin plus another study drug and on another sitagliptin plus placebo, in a randomized double-blind fashion. Forearm blood flow was assessed at each visit. (NCT01701973)
Timeframe: Percent change from baseline in forearm blood flow at 30 minutes, 60 minutes, 90 minutes, 120 minutes, 150 minutes, 180 minutes.

,,,,,,,,,
Interventionpercent change from baseline (Mean)
30 minutes60 minutes90 minutes120 minutes150 minutes180 minutes
Aim 2: Sitagliptin & Placebo, Females in Pegvisomant Group0.3916.1016.6741.9726.8743.51
Aim 2: Sitagliptin and Exendin 9-39, Female Participants-7.33-10.542.2331.1029.4830.76
Aim 2: Sitagliptin and Exendin 9-39, Male Participant-7.599.375.3616.5245.9854.91
Aim 2: Sitagliptin and LNMMA, Female Participants-0.71-3.643.244.2216.0914.80
Aim 2: Sitagliptin and LNMMA, Male Participants5.177.0525.6932.9226.2729.24
Aim 2: Sitagliptin and Pegvisomant, Female Participants15.646.5836.9654.1059.0851.21
Aim 2: Sitagliptin and Placebo, Females in Exendin 9-39 Group-0.986.952.0822.2415.5927.11
Aim 2: Sitagliptin and Placebo, Females in LNMMA Group-9.34-17.06-6.359.8011.2617.12
Aim 2: Sitagliptin and Placebo, Male in Exendin 9-39 Group-22.67-13.00-18.33-22.001.33-1.67
Aim 2: Sitagliptin and Placebo, Males in LNMMA Group14.784.5620.3256.2671.5165.31

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Aim 2: Measurement of Growth Hormone (GH) Levels

Subjects undergo two study days separated by a washout period. On one study day they received sitagliptin plus pegvisomant and on another sitagliptin plus placebo, in a randomized double-blind fashion. Growth hormone secretion following arginine stimulation was assessed at each visit. Growth hormone levels were determined using an assay that is not subject to interference by pegvisomant. (NCT01701973)
Timeframe: baseline and every 30 minutes until 180 minutes

,
Interventionng/mL (Mean)
30 minutes60 minutes90 minutes120 minutes150 minutes180 minutes
Aim 2: Sitagliptin and Pegvisomant, Female Participants4.277.0011.536.174.091.77
Aim 2: Sitagliptin and Placebo, Females in Pegvisomant Group2.995.926.054.061.831.57

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Aim 1: Venous Blood Sampling for Tissue Plasminogen Activator (TPA) Activity Levels

In Aim 1 subjects underwent two study days separated by a washout period. On one study day they received study drug and on another placebo, in a randomized double-blind fashion. Venous blood samples were obtained at each visit. (NCT01701973)
Timeframe: baseline and every 30 minutes for 180 minutes

,,,
InterventionIU/ml (Mean)
Baseline prior to Arginine30 minutes45 minutes60 minutes90 minutes120 minutes150 minutes180 minutes
Aim 1: Placebo, Female Participants0.280.320.350.320.350.350.410.50
Aim 1: Placebo, Male Participants0.220.250.320.340.270.280.370.45
Aim 1: Sitagliptin, Male Participants0.440.280.400.370.340.380.420.51
Aim 1: Sitagliptin,Female Participants0.300.400.430.400.390.400.440.55

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Aim 1: Percent Change From Baseline in Forearm Vascular Resistance

Forearm blood flow was determined by strain gauge plethysmography. Forearm vascular resistance was then calculated by dividing this into mean arterial pressure. The percent change from baseline was determined at each timepoint. (NCT01701973)
Timeframe: Percent change from baseline in forearm vascular resistance at 30 minutes, 60 minutes, 90 minutes, 120 minutes, 150 minutes, 180 minutes

,,,
Interventionpercentage change from baseline (Mean)
30 minutes60 minutes90 minutes120 minutes150 minutes180 minutes
Aim 1: Placebo, Female Participants-5.3498-1.0195-1.6694-5.0763-11.8335-16.5358
Aim 1: Placebo, Male Participants-11.22354.6875-3.8029-2.7449-7.1590-15.0591
Aim 1: Sitagliptin, Male Participants1.49296.73551.0144-10.3674-9.7129-11.9609
Aim 1: Sitagliptin,Female Participants-5.0677-5.1365-10.1867-12.5192-24.1962-22.4043

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Aim 1: Stimulated Peak Growth Hormone Level

Subjects underwent two study days separated by a washout period. On one study day they will receive sitagliptin and on another placebo, in a randomized double-blind fashion. Growth hormone secretion was stimulated using arginine (30 grams i.v. over 30 minutes) on each study day. Growth hormone levels were assessed during a 3 hour period following arginine stimulation. (NCT01701973)
Timeframe: Growth Hormone Level at 30 minutes (i.e. at completion of arginine infusion), 45 minutes, 60 minutes, 90 minutes, 120 minutes, 150 minutes, 180 minutes

,,,
Interventionng/ml (Mean)
30 minutes45 minutes60 minutes90 minutes120 minutes150 minutes180 minutes
Aim 1: Placebo, Female Participants3.16.67.06.44.22.41.3
Aim 1: Placebo, Male Participants2.03.93.32.10.91.81.0
Aim 1: Sitagliptin, Male Participants1.93.43.01.11.52.21.0
Aim 1: Sitagliptin,Female Participants5.29.59.45.02.71.80.9

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Change From Baseline in Total Cholesterol (TC)

Change from baseline in TC was measured as a percent change from baseline at Week 6 based on LDA model including percent change from baseline as response variable and term time. (NCT01702298)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Sitagliptin 100 mg/Simvastatin 40 mg FDC-33.7

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Change From Baseline in Non-high Density Lipoprotein Cholesterol (Non-HDL-C)

Change from baseline in non-HDL-C was measured as a percent change from baseline at Week 6 based on LDA model including percent change from baseline as response variable and term time. (NCT01702298)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Sitagliptin 100 mg/Simvastatin 40 mg FDC-43.1

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Change From Baseline in Fasting Plasma Glucose (FPG)

Change from baseline in FPG at Week 6 based on longitudinal data analysis (LDA) model including both baseline and post-baseline measurements as response variable and term time. (NCT01702298)
Timeframe: Baseline and Week 6

Interventionmg/dL (Least Squares Mean)
Sitagliptin 100 mg/Simvastatin 40 mg FDC-27.6

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Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C)

Change from baseline in HDL-C was measured as a percent change from baseline at Week 6 based on LDA model including percent change from baseline as response variable and term time. (NCT01702298)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Sitagliptin 100 mg/Simvastatin 40 mg FDC1.3

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Change From Baseline in Triglycerides (TG)

Change from baseline in TG was measured as a percent change from baseline at Week 6 (median and distribution free 95% confidence interval). (NCT01702298)
Timeframe: Baseline and Week 6

InterventionPercent change (Median)
Sitagliptin 100 mg/Simvastatin 40 mg FDC-31.8

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Percentage of Participants Who Experienced at Least One Adverse Event

An adverse event is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the Sponsor's product, whether or not considered related to the use of the product. (NCT01702298)
Timeframe: Up to 8 weeks (including 14 days after final dose of study drug)

InterventionPercentage of participants (Number)
Sitagliptin 100 mg/Simvastatin 40 mg FDC9.5

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Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C)

Change from baseline in LDL-C was measured as a percent change from baseline at Week 6 based on LDA model including percent change from baseline as response variable and term time. (NCT01702298)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Sitagliptin 100 mg/Simvastatin 40 mg FDC-46.5

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Number of Participants Who Discontinued Study Drug Due to an Adverse Event

Participants who were discontinued from study drug due to an adverse event during the 6 weeks of treatment. (NCT01702298)
Timeframe: Up to 6 weeks

InterventionParticipants (Number)
Sitagliptin 100 mg/Simvastatin 40 mg FDC0

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Percentage of Participants Who Discontinued From the Study Due to an Adverse Event During Phase A

An AE is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure, that occurs during the course of the study. (NCT01703221)
Timeframe: Up to 24 weeks

InterventionPercentage of participants (Number)
Omarigliptin (Phase A)0.6
Sitagliptin (Phase A)1.2
Placebo (Phase A)0

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Percentage of Participants Who Experienced at Least One Adverse Event During the Overall Study

An AE is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure, that occurs during the course of the study. These results represent the accrual of events over different treatment intervals: 52 weeks, omarigliptin (Phase A+B) defined as the double-blind period and open label extension period versus 28 weeks for the Sitagliptin (Phase A)→Omarigliptin (Phase B) and placebo (Phase A)→Omarigliptin (Phase B) group defined as the open-label extension period only. (NCT01703221)
Timeframe: Up to 52 weeks

InterventionPercentage of Participants (Number)
Omarigliptin (Phase A+B)69.9
Omarigliptin (Phase B)-S47.2
Omarigliptin (Phase B)-P56.3

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Percentage of Participants Who Experienced at Least One Adverse Event During Phase A

An adverse event (AE) is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure, that occurs during the course of the study. (NCT01703221)
Timeframe: Up to 24 weeks

InterventionPercentage of participants (Number)
Omarigliptin (Phase A)50.0
Sitagliptin (Phase A)49.4
Placebo (Phase A)65.9

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Percentage of Participants Who Discontinued From the Study Due to an Adverse Event During the Overall Study

An AE is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure, that occurs during the course of the study. These results represent the accrual of events over different treatment intervals: 52 weeks, omarigliptin (Phase A+B) defined as the double-blind period and open label extension period versus 28 weeks for the Sitagliptin (Phase A)→Omarigliptin (Phase B) and placebo (Phase A)→Omarigliptin (Phase B) group defined as the open-label extension period only. (NCT01703221)
Timeframe: Up to 52 weeks

InterventionPercentage of participants (Number)
Omarigliptin (Phase A+B)2.4
Omarigliptin (Phase B)-S1.2
Omarigliptin (Phase B)-P1.3

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Change From Baseline for 2-hour Post Meal Glucose (PMG) at Week 24

Change from baseline at Week 24 is defined as PMG at Week 24 minus PMG at Week 0. (NCT01703221)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Omarigliptin (Phase A)-42.38
Sitagliptin (Phase A)-45.24
Placebo (Phase A)-5.48

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Change From Baseline for Fasting Plasma Glucose (FPG) at Week 24

Blood glucose was measured on a fasting basis. FPG is expressed as mg/dL. Blood was drawn at predose on Day 1 and after 24 weeks of treatment to determine change in plasma glucose levels (i.e., FPG at Week 24 minus FPG at baseline). (NCT01703221)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Omarigliptin (Phase A)-18.52
Sitagliptin (Phase A)-20.75
Placebo (Phase A)-6.23

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Change From Baseline for Hemoglobin A1c (HbA1c) at Week 24

HbA1C is blood marker used to report average blood glucose levels over prolonged periods of time and is reported as a percentage (%). Change in A1C following 24 weeks of therapy (i.e., A1C at Week 24 minus A1C at baseline). (NCT01703221)
Timeframe: Baseline and Week 24

InterventionPercent HbA1c (Least Squares Mean)
Omarigliptin (Phase A)-0.66
Sitagliptin (Phase A)-0.65
Placebo (Phase A)0.13

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Percentage of Participants With a Gastrointestinal (GI) AE of Nausea (Phase 2)

"The percentage of participants with a GI AE of nausea was reported." (NCT01709305)
Timeframe: From Week 20 through Week 44

InterventionPercentage of Participants (Number)
Phase 2: Metformin + Sitagliptin + Glimepiride0
Phase 2: Metformin + Sitagliptin + Repaglinide0
Phase 2: Metformin + Sitagliptin + Acarbose0.4
Phase 2: Metformin + Sitagliptin + Gliclazide0.2

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Percentage of Participants With a GI AE of Abdominal Pain (Phase 2)

"The percentage of participants with a GI AE of abdominal pain was reported." (NCT01709305)
Timeframe: From Week 20 through Week 44

InterventionPercentage of Participants (Number)
Phase 2: Metformin + Sitagliptin + Glimepiride0
Phase 2: Metformin + Sitagliptin + Repaglinide0
Phase 2: Metformin + Sitagliptin + Acarbose0.4
Phase 2: Metformin + Sitagliptin + Gliclazide0.2

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Percentage of Participants With a GI AE of Diarrhea (Phase 2)

"The percentage of participants with a GI AE of diarrhea was reported." (NCT01709305)
Timeframe: From Week 20 through Week 44

InterventionPercentage of Participants (Number)
Phase 2: Metformin + Sitagliptin + Glimepiride0.5
Phase 2: Metformin + Sitagliptin + Repaglinide0.4
Phase 2: Metformin + Sitagliptin + Acarbose0.4
Phase 2: Metformin + Sitagliptin + Gliclazide0.9

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Percentage of Participants With a GI AE of Vomiting (Phase 2)

"The percentage of participants with a GI AE of vomiting was reported." (NCT01709305)
Timeframe: From Week 20 through Week 44

InterventionPercentage of Participants (Number)
Phase 2: Metformin + Sitagliptin + Glimepiride0.2
Phase 2: Metformin + Sitagliptin + Repaglinide0
Phase 2: Metformin + Sitagliptin + Acarbose0.2
Phase 2: Metformin + Sitagliptin + Gliclazide0.2

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Percentage of Participants With Hypoglycemia Events (Phase 2)

Hypoglycemia events represent epidsodes symptomatic of hypoglycemia (e.g., weakness, dizziness, shakiness, increased sweating, palpitations, or confusion) and/or finger stick glucose values of ≤70 mg/dL (3.9 mmol/L). The percentage of participants with hypoglycemia events was reported. (NCT01709305)
Timeframe: From Week 20 through Week 44

InterventionPercentage of Participants (Number)
Phase 2: Metformin + Sitagliptin + Glimepiride8.9
Phase 2: Metformin + Sitagliptin + Repaglinide6.1
Phase 2: Metformin + Sitagliptin + Acarbose0.5
Phase 2: Metformin + Sitagliptin + Gliclazide3.6

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Change From Phase 2 Baseline to Week 44 in Participant Body Weight (Phase 2)

Change from baseline in body weight in Phase 2 was reported. Change from baseline reflects the Week 44 body weight minus baseline body weight. Baseline is defined as Visit 6/Week 20. If this measurement was unavailable, the Week 16 value was used. (NCT01709305)
Timeframe: Phase 2 Baseline (Week 20), Week 44

Interventionkg (Mean)
Phase 2: Metformin + Sitagliptin + Glimepiride0.4
Phase 2: Metformin + Sitagliptin + Repaglinide0.2
Phase 2: Metformin + Sitagliptin + Acarbose-0.9
Phase 2: Metformin + Sitagliptin + Gliclazide0.2

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Change From Phase 2 Baseline to Week 44 in Hemoglobin A1c (HbA1c) Levels (Phase 2)

HbA1c is blood marker used to report average blood glucose levels over prolonged periods of time and is reported as a percentage (%). Change from baseline reflects the Week 44 A1C minus baseline A1C. Baseline is defined as Visit 6/Week 20. If this measurement was unavailable, the Week 16 value was used. Change from baseline was based on the constrained longitudinal data analysis (cLDA) model including all available measurements from baseline through the last visit. The terms in the cLDA model include treatment, time in weeks (categorical), regions, and treatment-by-time interaction. (NCT01709305)
Timeframe: Phase 2 Baseline (Week 20) and Week 44

InterventionPercent (Least Squares Mean)
Phase 2: Metformin + Sitagliptin + Glimepiride-0.65
Phase 2: Metformin + Sitagliptin + Repaglinide-0.62
Phase 2: Metformin + Sitagliptin + Acarbose-0.46
Phase 2: Metformin + Sitagliptin + Gliclazide-0.69

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The Percent of Subjects Engrafting by Day +30 After Transplantation

Percent of patients and the 95% Binomial Confidence interval who were able to achieve neutrophils engraftment (defined as the date of the first of three consecutive ANC values obtained on different days after transplantation during which the absolute neutrophils count (ANC) is at least 0.5 x109/l) by 30 days following transplant. (NCT01720264)
Timeframe: Day 0 to Day +30 post transplant

Interventionpercentage of participants (Number)
Sitagliptin100

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Time to Neutrophil Engraftment

Time to neutrophil engraftment will be analyzed by the Kaplan-Meier method. The time to engraftment of neutrophils is defined as the time from day 0 to the date of the first of three consecutive days after transplantation during which the absolute neutrophils count (ANC) is at least 0.5 x109/l. Patients surviving at least 14 days after transplant will be evaluable for this endpoint. Patients who did not have neutrophil engraftment before death will be censored at the date of death. The median and 95% confidence intervals will be provided. (NCT01720264)
Timeframe: Transplant (Day 0) up to 1 year

Interventiondays (Median)
Sitagliptin19

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Time to Platelet Engraftment

Time to platelet engraftment will be analyzed by the Kaplan-Meier method. The time to engraftment of platelets is defined as the time from day 0 to the first of three consecutive Complete Blood Counts (CBCs) obtained on different days after transplantation during which the platelet count is at least 20 x109/l. The CBCs obtained should be at least seven days after the most recent platelet transfusion. Only patients who achieved engraftment of platelets will be included in the analysis. The median and 95% confidence intervals will be provided. (NCT01720264)
Timeframe: Transplant (Day 0) up to 1 year

Interventiondays (Median)
Sitagliptin52

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Percentage of Participants With A1C at Goal (<6.5%) at Week 54

Glycated hemoglobin (A1C) is a blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. Percentage of participants with A1C at goal (<6.5%) at Week 54 was presented. (NCT01760447)
Timeframe: Week 54

InterventionPercentage of participants (Number)
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled18.6
Metformin and Metformin XR Pooled19.5

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 20

Blood glucose was measured on a fasting basis. Mean change from baseline at Week 20 was estimated from a longitudinal data analysis model. (NCT01760447)
Timeframe: Baseline and Week 20

Interventionmg/dL (Least Squares Mean)
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled-2.5
Metformin and Metformin XR Pooled8.3

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Change From Baseline in A1C at Week 54

A1C is a blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. Mean change from baseline at Week 54 was estimated from a longitudinal data analysis model. (NCT01760447)
Timeframe: Baseline and Week 54

InterventionPercentage of glycated hemoglobin (Least Squares Mean)
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled0.35
Metformin and Metformin XR Pooled0.73

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Percentage of Participants With A1C at Goal (<7.0%) at Week 54

Glycated hemoglobin (A1C) is a blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. Percentage of participants with A1C at goal (<7.0%) at Week 54 was presented. (NCT01760447)
Timeframe: Week 54

InterventionPercentage of participants (Number)
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled31.4
Metformin and Metformin XR Pooled27.3

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Number of Participants Who Experienced ≥1 Adverse Event During Weeks 0-20

The number of participants experiencing ≥1 adverse event during Weeks 0-20 was reported. An adverse event is defined as any untoward medical occurrence in a person administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT01760447)
Timeframe: Up to Week 20

InterventionParticipants (Count of Participants)
Sitagliptin/Metformin42
Metformin46
Sitagliptin/Metformin XR29
Metformin XR30
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled71
Metformin and Metformin XR Pooled76

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Baseline A1C

Glycated hemoglobin (A1C) is a blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. (NCT01760447)
Timeframe: Baseline

InterventionPercentage of glycated hemoglobin (Mean)
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled7.96
Metformin and Metformin XR Pooled8.06

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Percentage of Participants With A1C at Goal (<7.0%) at Week 20

Glycated hemoglobin (A1C) is a blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. Percentage of participants with A1C at goal (<7.0%) at Week 20 was presented. (NCT01760447)
Timeframe: Week 20

InterventionPercentage of participants (Number)
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled43.0
Metformin and Metformin XR Pooled31.0

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Percentage of Participants With A1C at Goal (<6.5%) at Week 20

Glycated hemoglobin (A1C) is a blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. Percentage of participants with A1C at goal (<6.5%) at Week 20 was presented. (NCT01760447)
Timeframe: Week 20

InterventionPercentage of participants (Number)
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled29.0
Metformin and Metformin XR Pooled20.4

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Percentage of Participants Initiating Insulin Glargine During Weeks 20-54

Percentage of participants who initiated insulin glargine therapy from Weeks 20 through 54 was reported. (NCT01760447)
Timeframe: Week 20 up to Week 54

InterventionPercentage of participants (Number)
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled22.7
Metformin and Metformin XR Pooled26.6

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Percentage of Participants Initiating Glycemic Rescue Therapy by Week 20

Percentage of participants who initiated glycemic rescue therapy prior to Week 20 was reported. (NCT01760447)
Timeframe: Up to Week 20

InterventionPercentage of participants (Number)
Sitagliptin/Metformin3.2
Metformin19.4
Sitagliptin/Metformin XR4.4
Metformin XR13.7
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled3.7
Metformin and Metformin XR Pooled16.8

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Number of Participants Who Experienced ≥1 Adverse Event During Weeks 0-56

The number of participants experiencing ≥1 adverse event during Weeks 0-56 were reported. An adverse event is defined as any untoward medical occurrence in a person administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT01760447)
Timeframe: Up to approximately Week 56

InterventionParticipants (Count of Participants)
Sitagliptin/Metformin26
Metformin27
Sitagliptin/Metformin XR36
Metformin XR39
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled62
Metformin and Metformin XR Pooled66

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Change From Baseline in A1C at Week 20

Glycated hemoglobin (A1C) is a blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. Mean change from baseline at Week 20 was estimated from a longitudinal data analysis model. (NCT01760447)
Timeframe: Baseline and Week 20

InterventionPercentage of glycated hemoglobin (Least Squares Mean)
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled-0.58
Metformin and Metformin XR Pooled-0.09

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Number of Participants Who Discontinued Study Drug Due to Experiencing an Adverse Event During Weeks 0-54

The number of participants who discontinued from study drug due to an adverse event during Weeks 0-54 was reported. An adverse event is defined as any untoward medical occurrence in a person administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT01760447)
Timeframe: Up to Week 54

InterventionParticipants (Count of Participants)
Sitagliptin/Metformin1
Metformin1
Sitagliptin/Metformin XR1
Metformin XR3
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled2
Metformin and Metformin XR Pooled4

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Number of Participants Who Discontinued Study Drug Due to Experiencing an Adverse Event During Weeks 0-20

The number of participants who discontinued from study drug due to an adverse event during Weeks 0-20 was reported. An adverse event is defined as any untoward medical occurrence in a person administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT01760447)
Timeframe: Up to Week 20

InterventionParticipants (Count of Participants)
Sitagliptin/Metformin1
Metformin2
Sitagliptin/Metformin XR2
Metformin XR2
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled3
Metformin and Metformin XR Pooled4

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Change From Baseline in FPG at Week 54

Blood glucose was measured on a fasting basis. Mean change from baseline at Week 54 was estimated from a longitudinal data analysis model. (NCT01760447)
Timeframe: Baseline and Week 54

Interventionmg/dL (Least Squares Mean)
Sitagliptin/Metformin and Sitagliptin/Metformin XR Pooled16.8
Metformin and Metformin XR Pooled16.9

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Change From Baseline in Glycosylated Hemoglobin (HbA1c)

The change in the value of glycosylated hemoglobin (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) collected at week 24 or final visit relative to Baseline. A negative change from Baseline indicated improvement. (NCT01834274)
Timeframe: Baseline and Week 24

InterventionPercent (Mean)
Fasiglifam 50 mg-0.63
Sitagliptin 100 mg-0.43

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Change From Baseline in Fasting Plasma Glucose (FPG)

The change between FPG collected at week 24 or final visit relative to Baseline. A negative change from Baseline indicated improvement. (NCT01834274)
Timeframe: Baseline and Week 24

Interventionmmol/L (Mean)
Fasiglifam 50 mg-0.22
Sitagliptin 100 mg1.54

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Percentage of Participants Who Discontinued Study Drug Due to an Adverse Event

An adverse event is defined as any unfavourable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product or protocol-specified procedure, whether or not considered related to the medicinal product or protocol-specified procedure. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition that is temporally associated with the use of the Sponsor's product, is also an adverse event. Data presented below excludes data after initiation of glycemic rescue therapy. (NCT01841697)
Timeframe: Up to 24 weeks

InterventionPercentage of participants (Number)
Omarigliptin 25 mg Once Weekly0.9
Sitagliptin 100 mg Once Daily2.2

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Percentage of Participants Achieving an A1C Goal <7.0% After 24 Weeks of Treatment

Participant whole blood samples were collected at Week 24 to determine the number of participants achieving A1C <7.0% at Week 24. (NCT01841697)
Timeframe: Week 24

InterventionPercentage of participants (Number)
Omarigliptin 25 mg Once Weekly50.9
Sitagliptin 100 mg Once Daily49.1

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Percentage of Participants Who Experienced at Least One Adverse Event

An adverse event is defined as any unfavourable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product or protocol-specified procedure, whether or not considered related to the medicinal product or protocol-specified procedure. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition that is temporally associated with the use of the Sponsor's product, is also an adverse event. Data presented below excludes data after initiation of glycemic rescue therapy. (NCT01841697)
Timeframe: Up to 27 weeks (including 3-week follow-up)

InterventionPercentage of participants (Number)
Omarigliptin 25 mg Once Weekly36.3
Sitagliptin 100 mg Once Daily40.6

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Change From Baseline in A1C at Week 24

A1C is a measure of the percentage of glycated hemoglobin in the blood. Participant whole blood samples were collected at baseline and Week 24 to determine the least squares mean A1C change from baseline. (NCT01841697)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Omarigliptin 25 mg Once Weekly-0.47
Sitagliptin 100 mg Once Daily-0.43

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Change From Baseline in FPG at Week 24

Participant whole blood samples were collected after an overnight fast at baseline and Week 24 to determine the least squares mean change from baseline in participant FPG. (NCT01841697)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Omarigliptin 25 mg Once Weekly-13.7
Sitagliptin 100 mg Once Daily-9.5

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Percentage of Participants Achieving an A1C Goal <6.5% After 24 Weeks of Treatment

Participant whole blood samples were collected at Week 24 to determine the percentage of participants achieving A1C <6.5% at Week 24. (NCT01841697)
Timeframe: Week 24

InterventionPercentage of participants (Number)
Omarigliptin 25 mg Once Weekly27.0
Sitagliptin 100 mg Once Daily22.8

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Acute Renal Failure Rate

Acute renal failure is defined as a clinical diagnosis of acute renal failure with documented new-onset abnormal renal function (increment > 0.5 mg/dL from baseline). (NCT01845831)
Timeframe: Duration of Hospitalization (Up to 10 Days)

Interventionparticipants (Number)
Sitagliptin + Glargine (Hospital)7
Basal Bolus (Hospital)6

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Length of Hospital Stay

Length of hospital stay in days. (NCT01845831)
Timeframe: Duration of Hospitalization (Up to 10 Days)

Interventiondays (Median)
Sitagliptin + Glargine (Hospital)4.0
Basal Bolus (Hospital)4.0

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Mean Blood Glucose Concentration After First Day of Treatment

The average blood glucose (BG) concentration after the first day of treatment (NCT01845831)
Timeframe: Duration of Hospitalization (Up to 10 Days)

Interventionmmol/L (Mean)
Sitagliptin + Glargine (Hospital)9.5
Basal Bolus (Hospital)9.4

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Mean Percentage of Blood Glucose Readings Between 3.9 - 10.0 mmol/L

Differences in glycemic control as measured by mean daily blood glucose (BG) concentration between sitagliptin once daily and basal bolus therapy with glargine once daily plus supplemental lispro insulin in hospitalized patients with T2D. (NCT01845831)
Timeframe: Duration of Hospitalization (Up to 10 Days)

Interventionpercentage of blood glucose readings (Mean)
Sitagliptin + Glargine (Hospital)57.0
Basal Bolus (Hospital)59.6

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Mean Percentage of Blood Glucose Readings Between 3.9 - 7.8 mmol/L

Differences in glycemic control as measured by mean daily blood glucose (BG) concentration between sitagliptin once daily and basal bolus therapy with glargine once daily plus supplemental lispro insulin in hospitalized patients with T2D. (NCT01845831)
Timeframe: Duration of Hospitalization (Up to 10 Days)

Interventionpercentage of blood glucose readings (Mean)
Sitagliptin + Glargine (Hospital)30.7
Basal Bolus (Hospital)29.7

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Hospital Mortality Rate

Mortality is defined as death occurring during admission. (NCT01845831)
Timeframe: Duration of Hospitalization (Up to 10 Days)

Interventionparticipants (Number)
Sitagliptin + Glargine (Hospital)0
Basal Bolus (Hospital)0

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Mean Percentage of Blood Glucose Readings Greater Than 13.3 mmol/L

Differences in glycemic control as measured by mean daily blood glucose (BG) concentration between sitagliptin once daily and basal bolus therapy with glargine once daily plus supplemental lispro insulin in hospitalized patients with T2D. (NCT01845831)
Timeframe: Duration of Hospitalization (Up to 10 Days)

Interventionpercentage of blood glucose readings (Mean)
Sitagliptin + Glargine (Hospital)14.8
Basal Bolus (Hospital)16.7

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Mean Percentage of Blood Glucose Readings Between 5.6 - 7.8 mmol/L

Differences in glycemic control as measured by mean daily blood glucose (BG) concentration between sitagliptin once daily and basal bolus therapy with glargine once daily plus supplemental lispro insulin in hospitalized patients with T2D. (NCT01845831)
Timeframe: Duration of Hospitalization (Up to 10 Days)

Interventionpercentage of blood glucose readings (Mean)
Sitagliptin + Glargine (Hospital)23.3
Basal Bolus (Hospital)23.5

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Change in HbA1C

The mean HbA1C measured at 3 months and 6 months post hospitalization. HbA1C is an indicator of diabetes control; below 6.0% is normal, 6.0% to 6.4% indicates prediabetes, and 6.5% or over indicates diabetes. (NCT01845831)
Timeframe: Post Hospital Discharge Month 3, Month 6

,,
Interventionpercent (Mean)
BaselineMonth 3Month 6
Metformin and Sitagliptin6.36.36.2
Metformin and Sitagliptin + Glargine 50%8.07.37.3
Metformin and Sitagliptin + Glargine 80%11.38.08.0

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Number of Participants With a Hypoglycemic Event

The number of participants who had a hypoglycemic event during hospitalization. (NCT01845831)
Timeframe: Duration of Hospitalization (Up to 10 Days)

,
InterventionParticipants (Count of Participants)
Blood Glucose <3.9 mmol/LBlood Glucose <2.2 mmol/L
Basal Bolus (Hospital)170
Sitagliptin + Glargine (Hospital)130

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Total Daily Insulin Dose

Daily insulin requirement (units per day). (NCT01845831)
Timeframe: Duration of Hospitalization (Up to 10 Days)

Interventionunits per day (Mean)
Sitagliptin + Glargine (Hospital)24.1
Basal Bolus (Hospital)34.0

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Triglyceride/HDL-Cholesterol Ratio

The ratio of triglyceride to HDL cholesterol is used as an indirect measure of insulin resistance (NCT01856907)
Timeframe: 16 weeks

InterventionRatio (Mean)
Sitagliptin-Metformin3.3
Placebo Pill4.5
Metformin2.7

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Waist Circumference

Measure of central fat (NCT01856907)
Timeframe: 16 weeks

Interventioncentimeters (Mean)
Sitagliptin-Metformin90
Placebo Pill93
Metformin93

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Waist-to-Height Ratio

Measure of central obesity adjusted for stature (NCT01856907)
Timeframe: 16 weeks

InterventionRatio (Mean)
Sitagliptin-Metformin.54
Placebo Pill.57
Metformin.58

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Oral Disposition Index

Measure of pancreatic beta cell compensatory action known as IS-SI (NCT01856907)
Timeframe: 16 weeks

Interventionindex (Mean)
Sitagliptin-Metformin427
Placebo Pill194
Metformin170

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Normalization of Glucose Levels

Normalization of glucose in patients with abnormal glucose levels is defined as a fasting glucose level of <100 mg/dL and a 2-hour glucose level following a 75 gram oral glucose load of <140 mg/dL (NCT01856907)
Timeframe: 16 weeks

InterventionParticipants (Count of Participants)
Sitagliptin-Metformin9
Placebo Pill2
Metformin4

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Mean Blood Glucose Level From the Oral Glucose Tolerance Test (OGTT)

The mean blood glucose is calculated by averaging the 4 blood glucose levels measure during a 75 gm oral glucose tolerance test . This involves summing the glucose levels measured at baseline, and 1/2 hour,1 hour and 2 hours after the glucose load and dividing by 4.. (NCT01856907)
Timeframe: 16 weeks

Interventionmg/dL (Mean)
Sitagliptin-Metformin113
Placebo Pill132
Metformin143

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Matsuda Index of Insulin Sensitivity

Composite insulin sensitivity index calculated from from glucose and insulin levels obtained during the OGTT (NCT01856907)
Timeframe: 16 weeks

Interventionindex (Mean)
Sitagliptin-Metformin6.2
Placebo Pill5.0
Metformin5.2

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Liver Enzymes as Safety Measure

Number of patients with no clinically significant changes in liver enzymes-measure of liver enzymes was a study safety endpoint (NCT01856907)
Timeframe: 16 weeks

InterventionParticipants (Count of Participants)
Sitagliptin-Metformin0
Placebo Pill0
Metformin0

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Fasting Insulin Resistance

Insulin resistance calculated from fasting glucose and insulin levels known as HOMA-IR (NCT01856907)
Timeframe: 16 weeks

Interventionindex (Mean)
Sitagliptin-Metformin2.4
Placebo Pill4.7
Metformin2.6

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Fasting Blood Glucose

Blood glucose in the fasting state (NCT01856907)
Timeframe: 16 weeks

Interventionmg/dL (Mean)
Sitagliptin-Metformin96
Placebo Pill101
Metformin93

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Body Mass Index

Measure of body weight corrected by height (NCT01856907)
Timeframe: 16 weeks

Interventionkg/meters^2 (Mean)
Sitagliptin-Metformin32.6
Placebo Pill33.5
Metformin33.6

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Brachial Artery Flow Mediated Dilation

A measurement of endothelial function in humans (NCT01859793)
Timeframe: Change before and after a single dose (2 hours post) and 8 weeks after daily dosing

,
Intervention%FMD (Mean)
Prior To Intervention2 hours post acute doseFollowing 8 weeks of therapy
Matching Placebo5.25.66.0
Sitagliptin5.66.35.8

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Circulating Inflammatory Markers VCAM-1

(NCT01859793)
Timeframe: Change before and after acute dose (2 hours) and 8 weeks after daily dosing of medication

,
Interventionmg/mL (Mean)
Pre-Intervention2 hours post acute dosepost 8 weeks of therapy
Matching Placebo584575620
Sitagliptin608574620

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Circulating Inflammatory Marker ICAM-1

(NCT01859793)
Timeframe: Change before and after acute dose (2 hours) and 8 weeks after daily dosing of medication

,
Interventionmg/mL (Mean)
Pre-Intervention2 hours post acute dosepost 8 weeks of therapy
Matching Placebo226216228
Sitagliptin223211232

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Change in Second-phase Insulin Response Derived From the Glucose-potentiated Arginine Test as a Measure of β-cell Sensitivity to Glucose at Baseline and at 6 Months

The key endpoint of interest will be the change in second phase insulin response derived from the Glucose-Potentiated Arginine (GPA) test. The GPA test will measure insulin, which will be a measure of pancreatic endocrine function in response to the injection of arginine. Arginine is a naturally occurring amino acid (substance) in the body. It will be given in the veins to make the pancreas secrete insulin. After the first injection of arginine, a glucose infusion will be started in order to raise the level of sugar in the blood to 230 mg/dl. Once the level is achieved, arginine will be injected again and blood samples are measured. After a 2 hour break, the glucose infusion will be started to achieve a blood sugar of 340 mg/dl and the arginine injection will be repeated. Comparison of responses at baseline and after 6 months of incretin-based therapy (Sitagliptin) or placebo will be performed using statistical methods. (NCT01879228)
Timeframe: Baseline and 6 months

,
InterventionInsulin230 µU/mL (Median)
Baseline6 Months
Placebo0.0550.053
Sitagliptin0.110.085

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Change in Fasting Blood Lipids

Ratio to baseline in fasting blood lipids (total cholesterol, low density lipoprotein [LDL], very low density lipoprotein [VLDL], high density lipoprotein [HDL], triglycerides, and free fatty acids) were analysed after 26 weeks treatment. Missing values were imputed using MMRM. Here we are presenting ratio to baseline data. (NCT01907854)
Timeframe: From baseline to week 26

,
Interventionratio (Mean)
Total cholesterolLDL cholesterolVLDL cholesterolHDL cholesterolTriglyceridesFree Fatty acids
Liraglutide1.0111.0491.0621.0041.0891.086
Sitagliptin1.0451.1211.0750.9971.0991.104

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Number of Treatment Emergent Adverse Events (TEAEs)

A treatment emergent adverse event (TEAE) was defined as an event that had an onset date (or increase in severity) on or after the first day of exposure to randomised treatment and no later than seven days after the last day of randomised treatment. The number of TEAEs was recorded during 26 weeks of treatment plus one week follow-up period. (NCT01907854)
Timeframe: During 26 weeks of treatment plus one week follow-up period.

Interventionnumber of events (Number)
Liraglutide455
Sitagliptin318

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Subjects Who Achieve HbA1c Below 7.0% (53 mmol/Mol) (American Diabetes Association Target) (y/n)

Number of subjects who achieve HbA1c <7.0% were analysed after 26 weeks of treatment. Missing values were imputed using MMRM. (NCT01907854)
Timeframe: After 26 weeks of treatment

,
Interventionpercentage (%) (Number)
YesNo
Liraglutide50.649.4
Sitagliptin26.973.1

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Change in Systolic Blood Pressure and Diastolic Blood Pressure

Change from baseline in systolic and diastolic blood pressure were analysed after 26 weeks of treatment. Missing values were imputed using MMRM. (NCT01907854)
Timeframe: From baseline to week 26

,
InterventionmmHg (Mean)
Systolic Blood PressureDiastolic Blood Pressure
Liraglutide-3.6-0.23
Sitagliptin-2.57-0.81

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Change in HbA1c (Glycosylated Haemoglobin)

Change from baseline in HbA1c was analysed after 26 weeks of treatment. Analysis population set: full analysis set (FAS); all randomised subjects receiving at least one dose of any of the trial products. Missing values were imputed using mixed model for repeated measurements (MMRM). (NCT01907854)
Timeframe: From baseline to week 26

Interventionpercentage of glycosylated haemoglobin (Mean)
Liraglutide-1.146
Sitagliptin-0.529

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Change in Fasting Plasma Glucose

Change from baseline in fasting plasma glucose was analysed after 26 weeks of treatment. Missing values were imputed using MMRM. (NCT01907854)
Timeframe: From baseline to week 26

Interventionnmol/L (Mean)
Liraglutide-1.967
Sitagliptin-0.588

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Change in Body Weight

Change from baseline in body weight was analysed after 26 weeks of treatment. Analysis population set: FAS: all randomised subjects receiving at least one dose of any of the trial products. Missing values were imputed using MMRM. (NCT01907854)
Timeframe: From baseline to week 26

Interventionkg (Mean)
Liraglutide-3.32
Sitagliptin-1.80

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Hemoglobin A1c, 6 Month

This is the result of hemoglobin A1c measured 3 months after stopping study drug/placebo, tested at the 6 month study time point (NCT01928199)
Timeframe: 6 months

Interventionpercentage of glycosylated hemoglobin (Mean)
Sitagliptin5.91
Placebo5.79

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Normal 2-hour Oral Glucose Tolerance Test-derived Blood Sugar

Number of subjects who have normal 2-hour oral glucose tolerance test-derived blood sugar will be measured at 3 months (NCT01928199)
Timeframe: 3 months

InterventionParticipants (Count of Participants)
Sitagliptin16
Placebo10

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6 Month OGTT Result (Completion of Washout From Study Drug)

We tested another OGTT at 6 months into study, after a 3 month washout from the study drug. Study drug was discontinued after the 3 month OGTT was completed. (NCT01928199)
Timeframe: 6 months

Interventionmg/dL (Mean)
Sitagliptin174.38
Placebo171.86

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2-hour Oral Glucose Tolerance Test-derived Blood Sugar

Change in 2-hour OGTT-derived blood sugar will be measured at three months and again at six months. These are 3 month OGTT results (NCT01928199)
Timeframe: 3 months

Interventionmg/dL (Mean)
Sitagliptin141.00
Placebo165.22

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Hemoglobin A1c, 3 Month

Measurement of Hemoglobin A1c at 3 months of being on study drug/placebo (NCT01928199)
Timeframe: 3 months

Interventionpercentage of glycosylated hemoglobin (Mean)
Sitagliptin5.52
Placebo5.78

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Change in HbA1c (Glycosylated Haemoglobin) From Baseline

Change in HbA1c from baseline until week 56.Full analysis set (FAS=1225) included all randomised subjects who had received at least one dose of randomised semaglutide or sitagliptin. (NCT01930188)
Timeframe: Week 0, week 56

Interventionpercentage of glycosylated haemoglobin (Least Squares Mean)
Semaglutide 0.5 mg + Sitagliptin Placebo-1.32
Semaglutide 1.0 mg + Sitagliptin Placebo-1.61
Sitagliptin + Semaglutide Placebo-0.55

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Change in Patient Reported Outcome (PRO) Questionnaire Diabetes Treatment Satisfaction Questionnaire Status (DTSQs) From Baseline

Full analysis set (FAS=1225) included all randomised subjects who had received at least one dose of semaglutide or sitagliptin. The DTSQs questionnaire was used to assess subjects' treatment satisfaction. This questionnaire contained 8 components and evaluates the diabetes treatment (including insulin, tablets and/or diet) in terms of convenience, flexibility and general feelings towards the treatment. The result presented is the 'Treatment Satisfaction' summary score, which is the sum of 6 of the 8 items of the DTSQs questionnaire. Response options range from 6 (best case) to 0 (worst case). Total scores for treatment satisfaction range from 0-36. Higher scores indicate higher satisfaction. (NCT01930188)
Timeframe: Week 0, week 56

InterventionUnits on a scale (Least Squares Mean)
Semaglutide 0.5 mg + Sitagliptin Placebo5.28
Semaglutide 1.0 mg + Sitagliptin Placebo5.91
Sitagliptin + Semaglutide Placebo4.45

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Change in Systolic and Diastolic Blood Pressure From Baseline

Change in systolic and diastolic blood pressure from baseline to week 56. Full analysis set (FAS=1225) included all randomised subjects who had received at least one dose of semaglutide or sitagliptin (NCT01930188)
Timeframe: Week 0, week 56

,,
InterventionmmHg (Least Squares Mean)
Systolic blood pressureDiastolic blood pressure
Semaglutide 0.5 mg + Sitagliptin Placebo-5.07-2.01
Semaglutide 1.0 mg + Sitagliptin Placebo-5.61-1.91
Sitagliptin + Semaglutide Placebo-2.29-1.11

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Subjects Who Achieved HbA1c Below or Equal to 6.5% (48 mmol/Mol) American Association of Clinical Endocrinologists (AACE) Target (Yes/no)

Subjects who achieved HbA1c ≤6.5% (48 mmol/mol) American Association of Clinical Endocrinologists (AACE) target (yes/no) after week 56 weeks of treatment. (NCT01930188)
Timeframe: After 56 weeks treatment

,,
InterventionSubjects (Number)
YesNo
Semaglutide 0.5 mg + Sitagliptin Placebo215194
Semaglutide 1.0 mg + Sitagliptin Placebo270139
Sitagliptin + Semaglutide Placebo83324

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Change in Fasting Plasma Glucose (FPG) From Baseline

Change in fasting plasma glucose from baseline to week 56. Full analysis set (FAS=1225) included all randomised subjects who had received at least one dose of semaglutide or sitagliptin. (NCT01930188)
Timeframe: Week 0, week 56

Interventionmg/dL (Least Squares Mean)
Semaglutide 0.5 mg + Sitagliptin Placebo-37.38
Semaglutide 1.0 mg + Sitagliptin Placebo-46.72
Sitagliptin + Semaglutide Placebo-19.85

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Change in Body Weight From Baseline

Change in body weight from baseline to week 56. Full analysis set (FAS=1225) included all randomised subjects who had received at least one dose of semaglutide or sitagliptin. (NCT01930188)
Timeframe: Week 0, week 56

Interventionkilograms (Least Squares Mean)
Semaglutide 0.5 mg + Sitagliptin Placebo-4.28
Semaglutide 1.0 mg + Sitagliptin Placebo-6.13
Sitagliptin + Semaglutide Placebo-1.93

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Plasma PF-04937319 Time for Cmax (Tmax) on Day 14

Tmax was time of maximum concentration. The PK parameters were summarized descriptively by treatment as appropriate. (NCT01933672)
Timeframe: Predose, 1.5, 3, 5, 6.5, 8, 11, 12.5, and 14 hours on Days 0 and 14; and predose on Days 7 and 15.

Interventionhour (Median)
PF-04937319 Split-Dose (150+100 mg)6.50
PF-04937319 Once-Daily (300 mg)5.00

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Plasma PF-04937319 Lowest Observed Concentration During the 24-hour Period (Cmin) on Day 14

Cmin lowest observed concentration during the 24-hour period. The PK parameters were summarized descriptively by treatment as appropriate. (NCT01933672)
Timeframe: Predose, 1.5, 3, 5, 6.5, 8, 11, 12.5, and 14 hours on Days 0 and 14; and predose on Days 7 and 15.

Interventionng/mL (Geometric Mean)
PF-04937319 Split-Dose (150+100 mg)101.9
PF-04937319 Once-Daily (300 mg)131.0

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Plasma PF-04937319 Highest Observed Concentration (Cmax) on Day 14

Cmax was highest observed concentration. The PK parameters were summarized descriptively by treatment as appropriate. (NCT01933672)
Timeframe: Predose, 1.5, 3, 5, 6.5, 8, 11, 12.5, and 14 hours on Days 0 and 14; and predose on Days 7 and 15.

Interventionng/mL (Geometric Mean)
PF-04937319 Split-Dose (150+100 mg)776.6
PF-04937319 Once-Daily (300 mg)980.5

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Plasma PF-04937319 Average Concentration Over the 24-hour Period (Cav) on Day 14

Cav was average concentration over the 24-hour period. The PK parameters were summarized descriptively by treatment as appropriate. (NCT01933672)
Timeframe: Predose, 1.5, 3, 5, 6.5, 8, 11, 12.5, and 14 hours on Days 0 and 14; and predose on Days 7 and 15.

Interventionng/mL (Geometric Mean)
PF-04937319 Split-Dose (150+100 mg)446.1
PF-04937319 Once-Daily (300 mg)492.0

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Plasma PF-04937319 Apparent Clearance (CL/F) on Day 14

The PK parameters were summarized descriptively by treatment as appropriate. Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Clearance was estimated from population PK modeling. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood. (NCT01933672)
Timeframe: Predose, 1.5, 3, 5, 6.5, 8, 11, 12.5, and 14 hours on Days 0 and 14; and predose on Days 7 and 15.

InterventionmL/min (Geometric Mean)
PF-04937319 Split-Dose (150+100 mg)389.2
PF-04937319 Once-Daily (300 mg)423.3

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Change From Baseline in Weighted Mean Daily Glucose (WMDG) at Day 14

Plasma glucose concentration was determined predose (Hour 0) and at 1.5, 3, 5, 6.5, 8, 11, 12.5, 14, 16, 20, and 24 hours postdose on Days 0 (baseline) and 14. WMDG was calculated as the area under the curve (AUC) of the 12-point plasma glucose concentration-time profile divided by 24 hours. (NCT01933672)
Timeframe: Prior to morning dose (Hour 0) and at 1.5, 3, 5, 6.5, 8, 11, 12.5, 14, 16, 20, and 24 hours post morning dose on Days 0 (baseline) and Day 14

Interventionmilligram/deciliter (mg/dL) (Least Squares Mean)
PF-04937319 Split-Dose (150+100 mg)-31.24
PF-04937319 Once-Daily (300 mg)-31.33
Sitagliptin 100 mg-19.24

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Change From Baseline in Fasting Plasma Glucose (FPG) at Day 14

"Blood samples for measurement of glucose to permit derivation of pre-meal collections at the pre-specified nominal timepoints of each period: predose (ie, time 0), 1.5, 3, 5, 6.5, 8, 11, 12.5, 14, 16 and 20 hours on Day 0 (baseline) and Day 14; and predose on Days 1 and 15." (NCT01933672)
Timeframe: Day 14

Interventionmg/dL (Least Squares Mean)
PF-04937319 Split-Dose (150+100 mg)-21.92
PF-04937319 Once-Daily (300 mg)-20.70
Sitagliptin 100 mg-16.51

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Change From Baseline in Body Weight (kg)

(NCT01933672)
Timeframe: Day 1 up to Day 14

Interventionkg (Mean)
PF-04937319 Split-Dose (150+100 mg)0.50
PF-04937319 Once-Daily (300 mg)0.30
Sitagliptin 100 mg0.05

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Number of Participants With Post-baseline Electrocardiograms (ECGs) Data Met Criteria of Potential Clinical Concern

ECG criteria of potential clinical concern were 1), PR interval: >=300 milliseconds (msec); >=25% increase when baseline >200 msec; or increase >=50% when baseline <=200 msec; 2), QRS interval: >=140 msec; >=50% increase from baseline; 3), QTc interval using Fridericia's formula (QTcF interval): absolute value >=450 - <480 msec, >=480-<500 msec, >500 msec; absolute change 30 - <60, >=60 msec. (NCT01933672)
Timeframe: Day 1 up to Day 14

,,
Interventionparticipants (Number)
PR interval >=300 msec, n=31,30,29QRS interval >=140 msec, n=31,30,29QTcF interval 450-480 msec, n=31,30,29QTcF interval 480-500 msec, n=31,30,29QTcF interval >=500 msec, n=31,30,29PR interval increase >=25%/50%, n=31,30,29QRS interval increase >=50%, n=31,30,29QTcF increase 30-60 msec, n=31,30,29QTcF increase >=60 msec, n=31,30,29
PF-04937319 Once-Daily (300 mg)001000000
PF-04937319 Split-Dose (150+100 mg)002000000
Sitagliptin 100 mg001000000

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Plasma PF-04937319 Area Under the Concentration Time Curve From Time 0 to 24 Hours (AUC24) of PF-04937319 at Day 14

The PK parameters were summarized descriptively by treatment as appropriate. Two (2) PK parameters specified in the protocol and SAP were not reported: AUClast was not reported since it was the same as AUC24 in this study, and apparent volume of distribution (Vz/F) was not reported since the log-linear terminal phase of the concentration-time profiles was not consistently well characterized in the 24-hour sampling period. (NCT01933672)
Timeframe: Predose, 1.5, 3, 5, 6.5, 8, 11, 12.5, and 14 hours on Days 0 and 14; and predose on Days 7 and 15.

Interventionng•hr/mL (Geometric Mean)
PF-04937319 Split-Dose (150+100 mg)10710
PF-04937319 Once-Daily (300 mg)11810

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Number of Participants With Vital Signs Data Met Criteria of Potential Clinical Concern

Vital signs included blood pressure (BP; supine, sitting and standing) and pulse rate. Vital signs criteria of potential clinical concern were 1), BP: sitting systolic BP (SBP) greater than or equal to (>=) 30 millimeters of mercury (mm Hg) change from baseline, sitting SBP =<20 mmHg change from baseline, supine/sitting/standing SBP less than (<) 90 mm Hg; sitting diastolic BP (DBP) >=20 mm Hg change from baseline, sitting SBP =<20 mmHg change from baseline, supine/sitting/standing DBP <50 mm Hg; 2), pulse rate (supine): <40 or greater than (>) 120 beats per minute (bpm). (NCT01933672)
Timeframe: Day 1 up to Day 14

,,
Interventionparticipants (Number)
Sitting SBP <90 mm HgSitting DBP <50 mm HgSitting Pulse Rate <40 bpmSitting Pulse Rate >120 bpmIncrease:sitting SBP≥30 mm HgIncrease:sitting DBP≥20 mm HgDecrease:sitting SBP≥30 mm HgDecrease:sitting DBP≥30 mm Hg
PF-04937319 Once-Daily (300 mg)00001120
PF-04937319 Split-Dose (150+100 mg)00001020
Sitagliptin 100 mg01002022

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Change From Baseline in Pre-meal Insulin on Day 14

Blood samples for measurement of glucose to permit derivation of pre-meal collections of blood samples for insulin at 0, 5 and 11 hours on Day 0 (baseline) and Day 14. (NCT01933672)
Timeframe: Day 14

,,
Interventionmicro international unit/milliliter (Least Squares Mean)
Pre-breakfast (n=31,30,26)Pre-lunch (n=30,27,25)Pre-dinner (n=30,28,24)
PF-04937319 Once-Daily (300 mg)0.464.075.06
PF-04937319 Split-Dose (150+100 mg)0.161.69-0.70
Sitagliptin 100 mg1.60-0.013.42

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Incidence of All Causality Treatment-Emergent Adverse Event by Preferred Term (Frequency Rate >5%)

(NCT01933672)
Timeframe: Day 1 up to Day 14

,,,
Interventionparticipants (Number)
Participants evaluable for AEsParticipants with AEs having a frequency rate >5%Participants with hypoglycaemiaParticipants with HeadacheParticipants with Back painParticipants with DiarrhoeaParticipants with Musculoskeletal painParticipants with Pain in extremityParticipants with Cough
Metformin Run-in4332001000
PF-04937319 Once-Daily (300 mg)301914412220
PF-04937319 Split-Dose (150+100 mg)311611420111
Sitagliptin 100 mg30124422112

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Frequency of Laboratory Test Abnormalities Reported in Any Treatment Group

The total number of participants with laboratory test abnormalities (without regard to baseline abnormality) was assessed. (NCT01933672)
Timeframe: Day 1 up to Day 14

,,
Interventionparticipants (Number)
Total neutrophils (abs) (10^3/mm^3) <0.8 × LLNEosinophils (abs) (10^3/mm^3) >1.2 × ULNTriglycerides (mg/dL) >1.3 × ULNPhosphate (mg/dL)<0.8 × LLNGlucose (mg/dL)>1.5 × ULNCreatine kinase (U/L) >2.0 × ULNUrine glucose (qual) ≥1Urine nitrite ≥1Urine leukocyte esterase ≥1Urine WBC (/HPF) ≥20
PF-04937319 Once-Daily (300 mg)00001214311
PF-04937319 Split-Dose (150+100 mg)10211618211
Sitagliptin 100 mg01201405121

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Change From Baseline in Pre-meal C-Peptide on Day 14

Blood samples for measurement of glucose to permit derivation of pre-meal collections of blood samples for C-peptide at the pre-specified nominal timepoints at predose, 5 and 11 hours on Day 0 (baseline) and Day 14. (NCT01933672)
Timeframe: Day 14

,,
Interventionnanograms/milliliter (ng/mL) (Least Squares Mean)
Pre-breakfast change from baselinePre-lunch change from baselinePre-dinner change from baseline
PF-04937319 Once-Daily (300 mg)0.060.700.30
PF-04937319 Split-Dose (150+100 mg)-0.060.200.36
Sitagliptin 100 mg0.300.060.32

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AUC C-peptide

(NCT01937598)
Timeframe: Approximately 6 weeks (range 9 - 60 days / 8.5 weeks)

Interventionnmol/l*min (Mean)
Sitagliptin171.5
Placebo159.2

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AUC Active GLP-1

(NCT01937598)
Timeframe: Approximately 6 weeks (range 9 - 60 days / 8.5 weeks)

Interventionpmol/l*min (Mean)
Sitagliptin607.9
Placebo418.4

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AUC Active GIP

(NCT01937598)
Timeframe: Approximately 6 weeks (range 9 - 60 days / 8.5 weeks)

Interventionpmol/l*min (Mean)
Sitagliptin6270
Placebo3496

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AUC Total GIP

(NCT01937598)
Timeframe: Approximately 6 weeks (range 9 - 60 days / 8.5 weeks)

Interventionpmol/l*min (Mean)
Sitagliptin6242
Placebo7523

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AUC Plasma Glucose

Incremental AUC from 0 to 300 min (NCT01937598)
Timeframe: Approximately 6 weeks (range 9 - 60 days / 8.5 weeks)

Interventionmmol/l*min (Mean)
Sitagliptin315.4
Placebo308.7

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AUC Insulin

(NCT01937598)
Timeframe: Approximately 6 weeks (range 9 - 60 days / 8.5 weeks)

Interventionnmol/l*min (Mean)
Sitagliptin45.8
Placebo42.6

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AUC Glucagon

(NCT01937598)
Timeframe: Approximately 6 weeks (range 9 - 60 days / 8.5 weeks)

Interventionpmol/l*min (Mean)
Sitagliptin6933
Placebo7004

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Incremental Area Under the Plasma Glucose (BG) Concentration-time Profile (AUC)

Incremental area under the plasma glucose (BG) concentration-time profile (AUC) immediately before to 300 min after a mixed meal test. In addition, the time course of BG values will be analysed with an ANCOVA model for repeated measurements with placebo baseline values as covariate. Time points to create the curce were 0, 15, 30, 45, 60, 90, 120, 150, 180, 240 and 300 minutes post mixed meal test. (NCT01937598)
Timeframe: 0 to 300 min post mixed meal test

Intervention[mg*min/dL] (Mean)
Sitagliptin5678
Placebo5557

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AUC Total GLP-1

(NCT01937598)
Timeframe: Approximately 6 weeks (range 9 - 60 days / 8.5 weeks)

Interventionpmol/l*min (Mean)
Sitagliptin748
Placebo1143

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Change in Oxygen Uptake Kinetics (VO2 Kinetics)

Oxygen uptake kinetics will be tested on a stationary bike before and after 3 months of study medication. VO2 kinetics is reported as the time constant associated with the change in oxygen update from rest to steady state. (NCT01951339)
Timeframe: Pre-intervention (Baseline) and post-intervention (3 months)

,
Interventionseconds (Mean)
Pre-interventionPost-intervention
Glimepiride Plus Placebo54.254.6
Sitagliptin Plus Placebo56.267.5

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Changes From Baseline in 31P Measurement: Free Pi Time Constant

Potential change in muscle mitochondrial function will be assessed after three months of study medication treatment. Data are represented as the change in Pi through the scan. (NCT01951339)
Timeframe: Pre-intervention (Baseline) and post-intervention (3 months)

,
Interventionseconds (Mean)
Pre-interventionPost-intervention
Glimepiride Plus Placebo28.5426.15
Sitagliptin Plus Placebo29.7327.94

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Changes From Baseline in 31P Measurement: Adenosine Triphosphate (ATP) Peaks

Potential change in muscle mitochondrial function will be assessed after three months of study medication treatment (NCT01951339)
Timeframe: Pre-intervention (Baseline) and post-intervention (3 months)

,
InterventionmM (Mean)
Pre-interventionPost-intervention
Glimepiride Plus Placebo7.938.02
Sitagliptin Plus Placebo8.1912.66

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Changes From Baseline in 31P Measurement: Adenosine Diphosphate (ADP) Time Constant

Potential change in muscle mitochondrial function will be assessed after three months of study medication treatment (NCT01951339)
Timeframe: Pre-intervention (Baseline) and post-intervention (3 months)

,
Interventionseconds (Mean)
Pre-interventionPost-intervention
Glimepiride Plus Placebo24.521.2
Sitagliptin Plus Placebo28.019.4

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Peak Oxygen Consumption (VO2peak).

Subjects' peak oxygen consumption will be tested on a stationary bike before and after 3 months of study medication. (NCT01951339)
Timeframe: Pre-intervention (Baseline) and post-intervention (3 months)

,
Interventionml/min (Mean)
Pre-interventionPost-intervention
Glimepiride Plus Placebo19531881
Sitagliptin Plus Placebo18931849

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Changes From Baseline in Echocardiographic Measures (Stroke Volume)

Potential change in cardiac function will be assessed by echocardiography before and after 3 months of study medication (NCT01951339)
Timeframe: Pre-intervention (Baseline) and post-intervention (3 months)

,
InterventionmL/beat (Mean)
Pre-interventionPost-intervention
Glimepiride Plus Placebo72.777.8
Sitagliptin Plus Placebo58.264.6

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Changes From Baseline in 31P Measurement: Phosphocreatine Time Constant

Potential change in muscle mitochondrial function will be assessed after three months of study medication treatment (NCT01951339)
Timeframe: Pre-intervention (Baseline) and post-intervention (3 months)

,
Interventionseconds (Mean)
Pre-interventionPost-intervention
Glimepiride Plus Placebo30.929.6
Sitagliptin Plus Placebo34.126.6

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Changes From Baseline in 31P Measurement: pH

Potential change in muscle mitochondrial function will be assessed after three months of study medication treatment (NCT01951339)
Timeframe: Pre-intervention (Baseline) and post-intervention (3 months)

,
InterventionpH (Mean)
Pre-interventionPost-intervention
Glimepiride Plus Placebo6.886.89
Sitagliptin Plus Placebo6.886.85

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Percentage Change in Liver Fat Relative to Baseline Assessed by MRI-PDFF

Participants liver fat was measured at baseline and 24 weeks. This is the percentage change in liver fat assessed by MRI-PDFF and stratified by treatment group. (NCT01963845)
Timeframe: Baseline and 24 weeks

Interventionpercentage change in liver fat (Mean)
Placebo13.9
Active Drug8.4

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ALT, Alanine Aminotransferase

ALT, measured in IU/L at baseline and 24 weeks (NCT01963845)
Timeframe: Baseline and 24 weeks

,
InterventionIU/L (Median)
Baseline24 weeks
Active Drug43.034.0
Placebo40.028.5

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AST, Aspartate Aminotransferase

AST, measured in IU/L at baseline and 24 weeks (NCT01963845)
Timeframe: Baseline and 24 weeks

,
InterventionIU/L (Median)
Baseline24 weeks
Active Drug28.027.0
Placebo28.523.5

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HOMA-IR, Homeostatic Model Assessment of Insulin Resistance

HOMA-IR, calculated as [(glucose (mg/dL) X insulin (mg/dL)) / 405 ] at baseline and 24 weeks (NCT01963845)
Timeframe: Baseline and 24 weeks

,
InterventionHOMA-IR score (Median)
Baseline24 weeks
Active Drug5.96.8
Placebo5.44.9

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LDL, Low-density Lipoprotein

LDL, measured in mg/dL at baseline and 24 weeks (NCT01963845)
Timeframe: Baseline and 24 weeks

,
Interventionmg/dL (Median)
Baseline24 weeks
Active Drug100.098.0
Placebo99.0101.0

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The Change in the Psoriasis Area and Severity Index (PASI) From Baseline to 16 Weeks in Psoriasis Patients With Type 2 Diabetes Treated With Sitagliptin Compared to Patients Treated With Gliclazide.

Psoriasis area and severity index (0-72), higher scores worse outcome (NCT01991197)
Timeframe: 16 weeks

Interventionscore on a scale (Median)
Sitagliptin9.5
Gliclazide9.4

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The Change in PASI From Baseline to 32 Weeks in Psoriasis Patients With Type 2 Diabetes Treated With Sitagliptin Compared to Patients Treated With Gliclazide.

Psoriasis area and severity index 0-72, higher score worse outcome (NCT01991197)
Timeframe: baseline and 32 weeks

Interventionscore on a scale (Median)
Sitagliptin3
Gliclazide1.8

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The Change in Levels of Total Cholesterol From Baseline to 16 Weeks in the Sitagliptin and Gliclazide Arms.

The change in total cholesterol from baseline to 16 weeks (NCT01991197)
Timeframe: 16 weeks

Interventionmmol/L (Median)
Sitagliptin0.1
Gliclazide-0.1

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The Change in Levels of Systolic Blood Pressure From Baseline to 16 Weeks in the Sitagliptin and Gliclazide Arms.

The change in systolic blood pressure from baseline to 16 weeks measured in kg (NCT01991197)
Timeframe: 16 weeks

InterventionmmHg (Median)
Sitagliptin4
Gliclazide-9

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The Change in Levels of Serum Glucose From Baseline to 16 Weeks in the Sitagliptin and Gliclazide Arms.

The change in glucose from baseline to 16 weeks (NCT01991197)
Timeframe: 16 weeks

Interventionmmol/L (Median)
Sitagliptin-0.2
Gliclazide-0.1

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The Change in Levels of High Sensitivity C-reactive Protein From Baseline to 16 Weeks in the Sitagliptin and Gliclazide Arms.

High sensitivity C-reactive protein (range 0 - no maximum) (NCT01991197)
Timeframe: 16 weeks

Interventionµg/ml (Median)
Sitagliptin0
Gliclazide8.4

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The Effect of Treatment With Sitagliptin and With Gliclazide From Baseline to 16 Weeks on the Change in Dipeptidyl Peptidase-4 Levels in the Skin (in a Sub-group of Participants Willing to Undergo Skin Biopsies).

Dipeptidyl peptidase-4 levels levels in skin (0-no maximum) (NCT01991197)
Timeframe: 16 weeks

InterventiondCt (Median)
Gliclazide-1.12
Sitagliptin0

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The Effects of Treatment With Sitagliptin and Treatment With Gliclazide on Other Efficacy Endpoints.

"Secondary outcomes:~d. number or participants who acheived a greater than 50% reduction in PASI from baseline (PASI-50); e. number of participants who achieved PASI-75 and PASI-90." (NCT01991197)
Timeframe: 16 weeks

,
InterventionParticipants (Count of Participants)
PASI 50PASI 75PASI 90
Gliclazide100
Sitagliptin100

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The Change in Quality of Life Scores From Baseline to 16 Weeks in the Sitagliptin and Gliclazide Arms.

"Dermatology life quality index (a skin related quality of life measure) (0-10), higher score worse outcome EQ-5D Euroqol 5 item quality of life index comprising 5 dimensions mobility, self-care, usual activities, pain, anxiety. An index can be derived from these 5 dimensions by conversion with a table of scores. The maximum score of 1 indicates the best health state and minimum score indicating the worst health outcome -0.594.~HADS Hospital anxiety and depression scale 0-16 for anxiety and 0-16 for depression, higher score worse outcome HAQ-8 Stanford 8 item disability scale. Scoring is from 0 (without any difficulty) to 3 (unable to do). The 8 scores from the 8 sections are summed and divided by 8. The result is the disability index (range 0-3 with 25 possible values). A" (NCT01991197)
Timeframe: 16 weeks

,
Interventionscore on a scale (Median)
DLQIHAQ-8HADS AnxietyHADS DepressionEQ-5D
Gliclazide-1.00.000-0.2
Sitagliptin0.00.0-100

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The Number of Patricipants in the Sitagliptin and Gliclazide Arms With Adverse Events at 32 Weeks.

"Dosage: Sitagliptin: 100mg daily, or 50mg daily for participants with moderate kidney disease Gliclazide: 80-320 mg daily.~Secondary outcomes: the number participants with adverse events." (NCT01991197)
Timeframe: 32 weeks

InterventionParticipants (Count of Participants)
Sitagliptin6
Gliclazide10

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The Effects of Treatment With Sitagliptin and Treatment With Gliclazide on the Serum Cytokine Tumour Necrosis Factor Alpha.

"Secondary outcomes:~The change in serum concentrations of the cytokines tumour necrosis factor alpha (TNFα) Range: 0-no maximum" (NCT01991197)
Timeframe: 16 weeks

Interventionpg/ml (Median)
Sitagliptin0
Gliclazide0

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The Effects of Treatment With Sitagliptin and Treatment With Gliclazide on the Change in Serum Leptin From Baseline to 16 Weeks.

"Secondary outcomes:~The change in serum concentrations of the adipokine leptin Range: 0-no maximum" (NCT01991197)
Timeframe: 16 weeks

Interventionpg/ml (Median)
Sitagliptin-0.07
Gliclazide0.43

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The Effects of Treatment With Sitagliptin and Treatment With Gliclazide From Baseline to 16 Weeks on Serum Levels Interleukin-23.

"Secondary outcomes:~The change in serum concentrations of the cytokine interleukin-23 (IL-23) Range: 0-no maximum" (NCT01991197)
Timeframe: 16 weeks

Interventionpg/ml (Median)
Sitagliptin0
Gliclazide0

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The Effects of Treatment With Sitagliptin and Treatment With Gliclazide From Baseline to 16 Weeks on Serum Levels Interleukin-17.

"Secondary outcomes:~The change in serum concentrations of the cytokine interleukin-17 (IL-17) Range: 0-no maximum" (NCT01991197)
Timeframe: 16 weeks

Interventionpg/ml (Median)
Sitagliptin0
Gliclazide0

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The Effect of Treatment With Sitagliptin and With Gliclazide From Baseline to 16 Weeks on the Change in Interleukin-17 Levels in the Skin (in a Sub-group of Participants Willing to Undergo Skin Biopsies).

Interleukin 17 levels in skin (0-no maximum) (NCT01991197)
Timeframe: 16 weeks

InterventiondCt (Median)
Sitagliptin3.41
Gliclazide2.09

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The Change in Weight From Baseline to 16 Weeks in the Sitagliptin and Gliclazide Arms.

The change in weight from baseline to 16 weeks measured in kg (NCT01991197)
Timeframe: 16 weeks

Interventionkg (Median)
Sitagliptin-0.5
Gliclazide-0.6

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Percentage of Participants With an Adverse Event of Symptomatic Hypoglycemia Up to Week 52: Excluding Rescue Approach

Symptomatic hypoglycemia was an event with clinical symptoms reported by the investigator as hypoglycemia (biochemical documentation not required). Participants who met glycemic rescue criteria received open-label sitagliptin glycemic rescue medication. (NCT01999218)
Timeframe: Up to Week 52

InterventionPercentage of Participants (Number)
Ertugliflozin 5 mg3.1
Ertugliflozin 15 mg5.2
Glimepiride19.2

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Percentage of Participants Experiencing An Adverse Event (AE) Up to Week 106

An AE is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure, that occurs during the course of the study. (NCT01999218)
Timeframe: Up to Week 106

InterventionPercentage of Participants (Number)
Ertugliflozin 5 mg70.1
Ertugliflozin 15 mg71.3
Glimepiride69.7

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Percentage of Participants Discontinuing Study Treatment Due to an AE Up to Week 104

An AE is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure, that occurs during the course of the study. (NCT01999218)
Timeframe: Up to Week 104

InterventionPercentage of Participants (Number)
Ertugliflozin 5 mg6.5
Ertugliflozin 15 mg8.0
Glimepiride5.1

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Change From Baseline in Sitting Systolic Blood Pressure (SBP) at Week 52 Excluding Rescue Approach

This change from baseline reflects the Week 52 SBP minus the Week 0 SBP. Participants who met glycemic rescue criteria received open-label sitagliptin glycemic rescue medication. (NCT01999218)
Timeframe: Baseline and Week 52

InterventionmmHg (Least Squares Mean)
Ertugliflozin 5 mg-2.25
Ertugliflozin 15 mg-3.81
Glimepiride0.95

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Change From Baseline in Body Weight at Week 52 Excluding Rescue Approach

This change from baseline reflects the Week 52 body weight minus the Week 0 body weight. Participants who met glycemic rescue criteria received open-label sitagliptin glycemic rescue medication. (NCT01999218)
Timeframe: Baseline and Week 52

InterventionKilograms (Least Squares Mean)
Ertugliflozin 5 mg-2.96
Ertugliflozin 15 mg-3.38
Glimepiride0.91

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Change From Baseline in Hemoglobin A1C (A1C) at Week 52: Excluding Rescue Approach

A1C is blood marker used to report average blood glucose levels over prolonged periods of time and is reported as a percentage (%). A1C represents the percentage of glycated hemoglobin. This change from baseline reflects the Week 52 A1C minus the Week 0 A1C. A negative number indicates a reduction in A1C level. Participants who met glycemic rescue criteria received open-label sitagliptin glycemic rescue medication. The primary study objective was the MK-8835 15 mg vs. glimepiride comparison; the MK-8835 5mg vs glimerpiride comparison was a secondary study objective. (NCT01999218)
Timeframe: Baseline and Week 52

InterventionPercent (Least Squares Mean)
Ertugliflozin 5 mg-0.56
Ertugliflozin 15 mg-0.64
Glimepiride-0.74

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Number of Confirmed Hypoglycaemic Episodes

confirmed hypoglycaemic episode defined as severe (unable to treat her/himself) or biochemically confirmed by a plasma glucose < 3.1 mmol/L (NCT02008682)
Timeframe: Weeks 0-26

Interventionepisodes (Number)
Liraglutide2
Sitagliptin1

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Change From Baseline in Glycosylated Haemoglobin (HbA1c)

Mean change from baseline in glycosylated haemoglobin A1c (HbA1c) at Week 26. (NCT02008682)
Timeframe: Week 0, week 26

InterventionPercent (%) glycosylated haemoglobin (Mean)
Liraglutide-1.666
Sitagliptin-0.969

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Change From Baseline in 7-point Self-measured Plasma Glucose Profile

Mean change from baseline in mean of 7-point self-measured plasma glucose at week 26. The 7-point self-measured plasma glucose levels were measured before and after (120 minutes after the start of the meal) the three main meals (breakfast, lunch and dinner), and at bed time. (NCT02008682)
Timeframe: Week 0, week 26

Interventionmmol/L (Mean)
Liraglutide-2.25
Sitagliptin-1.36

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Change From Baseline in Fasting Plasma Glucose

Mean change from baseline in fasting plasma glucose (FPG) at Week 26. (NCT02008682)
Timeframe: Week 0, week 26

Interventionmmol/L (Mean)
Liraglutide-2.347
Sitagliptin-1.205

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Subjects Who Achieve (Yes/no) HbA1c Below or Equal to 6.5 % (American Association of Clinical Endocrinologists Target)

Calculated as the percentage of subjects achieving treatment target of HbA1c <= 6.5% at Week 26 (NCT02008682)
Timeframe: After 26 weeks of treatment

Interventionpercentage of subjects (Number)
Liraglutide61.7
Sitagliptin26.3

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Subjects Who Achieve (Yes/no) HbA1c Below 7.0 % (American Diabetes Association Target)

Calculated as the percentage of subjects achieving treatment target of HbA1c < 7.0% at Week 26 (NCT02008682)
Timeframe: After 26 weeks of treatment

Interventionpercentage of subjects (Number)
Liraglutide76.5
Sitagliptin52.6

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Baseline Homeostasis Model Assessment of β-cell Function (HOMA-%β) Value

HOMA-%β is a well-accepted means of assessing fasting β-cell function, and is calculated using measured C-peptide and glucose levels and is measured as a percentage of a normal reference population. HOMA-%β = [20 x fasting insulin (μU/mL)] / [fasting plasma glucose (mmol/L) - 3.5] (NCT02036515)
Timeframe: Baseline

InterventionPercentage (Mean)
Ertugliflozin 5 mg47.99
Ertugliflozin 15 mg48.54
Placebo48.04

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Change From Baseline in Body Weight at Week 26

The change from baseline is the Week 26 body weight minus the Week 0 body weight. Data presented exclude data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Baseline and Week 26

Interventionkg (Least Squares Mean)
Ertugliflozin 5 mg-3.35
Ertugliflozin 15 mg-3.04
Placebo-1.32

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Time to Initiation of Glycemic Rescue by Week 52

Glycemic rescue medication was initiated for participants who met progressively more stringent glycemic rescue criteria. Rescue medication included glimepiride (or insulin glargine if glimepiride was not considered appropriate for the participant). Data presented are the minimum and maximum times to the initiation of rescue therapy in days. (NCT02036515)
Timeframe: Up to week 52

,,
InterventionDays (Number)
Minimum time to initiation of glycemic rescueMaximum time to initiation of glycemic rescue
Ertugliflozin 15 mg43299
Ertugliflozin 5 mg135295
Placebo26327

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Time to Initiation of Glycemic Rescue by Week 26

Glycemic rescue medication was initiated for participants who met progressively more stringent glycemic rescue criteria. Rescue medication included glimepiride (or insulin glargine if glimepiride was not considered appropriate for the participant). Data presented are the minimum and maximum times to the initiation of rescue therapy in days. Below data include data from 1 participant in the Placebo arm who continued Phase A treatment for an additional 30 days. (NCT02036515)
Timeframe: Up to Week 26 (plus 30 days for 1 placebo participant)

,,
InterventionDays (Number)
Minimum time to initiation of glycemic rescueMaximum time to initiation of glycemic rescue
Ertugliflozin 15 mg43147
Ertugliflozin 5 mg135141
Placebo26212

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Change From Baseline in Sitting Systolic Blood Pressure at Week 52

The change from baseline is the Week 52 systolic blood pressure minus the Week 0 systolic blood pressure. Sitting blood pressure was measured in triplicate. Data presented exclude data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Baseline and Week 52

,,
InterventionmmHg (Least Squares Mean)
BaselineChange from baseline
Ertugliflozin 15 mg130.92-4.09
Ertugliflozin 5 mg130.92-4.16
Placebo130.920.83

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Change From Baseline in Sitting Systolic Blood Pressure at Week 26

The change from baseline is the Week 26 systolic blood pressure minus the Week 0 systolic blood pressure. Sitting blood pressure was measured in triplicate. Data presented exclude data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Baseline and Week 26

,,
InterventionmmHg (Least Squares Mean)
BaselineChange from baseline
Ertugliflozin 15 mg130.87-4.82
Ertugliflozin 5 mg130.87-3.81
Placebo130.87-0.88

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Change From Baseline in Sitting Diastolic Blood Pressure at Week 52

The change from baseline is the Week 52 diastolic blood pressure minus the Week 0 diastolic blood pressure. Sitting blood pressure was measured in triplicate. Data presented exclude data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Baseline and Week 52

,,
InterventionmmHg (Least Squares Mean)
BaselineChange from baseline
Ertugliflozin 15 mg78.44-1.38
Ertugliflozin 5 mg78.44-1.52
Placebo78.44-0.53

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Change From Baseline in Sitting Diastolic Blood Pressure at Week 26

The change from baseline is the Week 26 diastolic blood pressure minus the Week 0 diastolic blood pressure. Sitting blood pressure was measured in triplicate. Data presented exclude data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Baseline and Week 26

,,
InterventionmmHg (Least Squares Mean)
BaselineChange from baseline
Ertugliflozin 15 mg78.42-1.81
Ertugliflozin 5 mg78.42-1.68
Placebo78.42-0.43

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Percentage of Participants With an A1C <7% (53 mmol/Mol) at Week 52

A1C is measured as percent. Laboratory measurements were performed after an overnight fast ≥10 hours in duration. Data presented exclude data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Week 52

InterventionPercentage of participants (Number)
Ertugliflozin 5 mg33.3
Ertugliflozin 15 mg32.7
Placebo13.7

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Change From Baseline in Body Weight at Week 52

The change from baseline is the Week 52 body weight minus the Week 0 body weight. Data presented exclude data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Baseline and Week 52

Interventionkg (Least Squares Mean)
Ertugliflozin 5 mg-3.46
Ertugliflozin 15 mg-2.83
Placebo-0.95

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Baseline EQ-5D 3-level Version (EQ-5D-3L) Questionnaire Score

"The EQ-5D-3L is a health profile questionnaire that assesses quality of life along 5 dimensions. Participants rate 5 aspects of health (mobility, self-care, usual activities, pain/discomfort, and anxiety/depression) by choosing from 3 answering options (1=no problems; 2=some problems; 3=extreme problems). The summed score ranges from 1-15 with 3 corresponding to no problems and 15 corresponding to severe problems in the 5 dimensions. EQ-5D-3L also includes an EQ visual analogue score (VAS) that ranges between 100 (best imaginable health) and 0 (worst imaginable health). Total index EQ-5D-3L summary score is weighted with a range of -0.594 (worst) to 1.0 (best)." (NCT02036515)
Timeframe: Baseline

InterventionScore on a scale (Mean)
Ertugliflozin 5 mg0.88
Ertugliflozin 15 mg0.89
Placebo0.90

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 26

The change from baseline is the Week 26 FPG minus the Week 0 FPG. Laboratory measurements were performed after an overnight fast ≥10 hours in duration. Data presented exclude data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Baseline and Week 26

Interventionmg/dL (Least Squares Mean)
Ertugliflozin 5 mg-26.91
Ertugliflozin 15 mg-33.04
Placebo-1.76

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Change From Baseline in EQ-5D-3L Questionnaire Score at Week 26

"The EQ-5D-3L is a health profile questionnaire that assesses quality of life along 5 dimensions. Participants rate 5 aspects of health (mobility, self-care, usual activities, pain/discomfort, and anxiety/depression) by choosing from 3 answering options (1=no problems; 2=some problems; 3=extreme problems). The summed score ranges from 3-15 with 3 corresponding to no problems and 15 corresponding to severe problems in the 5 dimensions. EQ-5D-3L also includes an EQ VAS that ranges between 100 (best imaginable health) and 0 (worst imaginable health). Decrease from baseline in EQ-5D-3L signifies improvement. Total index EQ-5D-3L summary score is weighted with a range of -0.594 (worst) to 1.0 (best). Data presented exclude data following the initiation of rescue therapy." (NCT02036515)
Timeframe: Baseline and Week 26

InterventionScore on a scale (Least Squares Mean)
Ertugliflozin 5 mg0.00
Ertugliflozin 15 mg0.02
Placebo0.01

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Change From Baseline in EQ-5D-3L Score at Week 52

"The EQ-5D-3L is a health profile questionnaire that assesses quality of life along 5 dimensions. Participants rate 5 aspects of health (mobility, self-care, usual activities, pain/discomfort, and anxiety/depression) by choosing from 3 answering options (1=no problems; 2=some problems; 3=extreme problems). The summed score ranges from 3-15 with 3 corresponding to no problems and 15 corresponding to severe problems in the 5 dimensions. EQ-5D-3L also includes an EQ VAS that ranges between 100 (best imaginable health) and 0 (worst imaginable health). Decrease from baseline in EQ-5D-3L signifies improvement. Total index EQ-5D-3L summary score is weighted with a range of -0.594 (worst) to 1.0 (best). Data presented exclude data following the initiation of rescue therapy." (NCT02036515)
Timeframe: Baseline and Week 52

InterventionScore on a scale (Least Squares Mean)
Ertugliflozin 5 mg0.03
Ertugliflozin 15 mg-0.00
Placebo0.02

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Percentage of Participants With an A1C <7% (53 mmol/Mol) at Week 26

A1C is measured as percent. Laboratory measurements were performed after an overnight fast ≥10 hours in duration. Data presented exclude data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Week 26

InterventionPercentage of participants (Number)
Ertugliflozin 5 mg32.1
Ertugliflozin 15 mg39.9
Placebo17.0

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Percentage of Participants Receiving Glycemic Rescue Medication by Week 52

Glycemic rescue medication was initiated for participants who met progressively more stringent glycemic rescue criteria. Rescue medication included glimepiride (or insulin glargine if glimepiride was not considered appropriate for the participant). (NCT02036515)
Timeframe: Week 52

InterventionPercentage of participants (Number)
Ertugliflozin 5 mg12.8
Ertugliflozin 15 mg13.7
Placebo41.8

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Percentage of Participants Receiving Glycemic Rescue Medication by Week 26

Glycemic rescue medication was initiated for participants who met progressively more stringent glycemic rescue criteria. Rescue medication included glimepiride (or insulin glargine if glimepiride was not considered appropriate for the participant). (NCT02036515)
Timeframe: Week 26

InterventionPercentage of participants (Number)
Ertugliflozin 5 mg1.3
Ertugliflozin 15 mg2.0
Placebo16.3

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Percentage of Participants Experiencing An Adverse Event (AE)

An adverse event is defined as any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product, and which does not necessarily have to have a causal relationship with this treatment. Data presented include data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Up to Week 54

InterventionPercentage of participants (Number)
Ertugliflozin 5 mg57.7
Ertugliflozin 15 mg60.1
Placebo63.4

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Percentage of Participants Discontinuing Study Treatment Due to an AE

An adverse event is defined as any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product, and which does not necessarily have to have a causal relationship with this treatment. Data presented include data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Up to Week 52

InterventionPercentage of participants (Number)
Ertugliflozin 5 mg4.5
Ertugliflozin 15 mg3.9
Placebo3.9

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Change From Baseline in HOMA-%β at Week 52

HOMA-%β is a well-accepted means of assessing fasting β-cell function, and is calculated using measured C-peptide and glucose levels and is measured as a percentage of a normal reference population. HOMA-%β = [20 x fasting insulin (μU/mL)] / [fasting plasma glucose (mmol/L) - 3.5]. Data presented exclude data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Baseline and Week 52

InterventionPercentage (Least Squares Mean)
Ertugliflozin 5 mg10.85
Ertugliflozin 15 mg10.93
Placebo-1.93

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Change From Baseline in HOMA-%β at Week 26

HOMA-%β is a well-accepted means of assessing fasting β-cell function, and is calculated using measured C-peptide and glucose levels and is measured as a percentage of a normal reference population. HOMA-%β = [20 x fasting insulin (μU/mL)] / [fasting plasma glucose (mmol/L) - 3.5]. Data presented exclude data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Baseline and Week 26

InterventionPercentage (Least Squares Mean)
Ertugliflozin 5 mg13.28
Ertugliflozin 15 mg12.43
Placebo0.52

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Change From Baseline in Hemoglobin A1C at Week 52

A1C is measured as percent. Thus this change from baseline reflects the Week 52 A1C percent minus the Week 0 A1C percent. Laboratory measurements were performed after an overnight fast ≥10 hours in duration. Data presented exclude data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Baseline and Week 52

InterventionPercent (Least Squares Mean)
Ertugliflozin 5 mg-0.75
Ertugliflozin 15 mg-0.81
Placebo0.02

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Change From Baseline in Hemoglobin A1C at Week 26

A1C is measured as percent. Thus this change from baseline reflects the Week 26 A1C percent minus the Week 0 A1C percent. Laboratory measurements were performed after an overnight fast ≥10 hours in duration. Data presented exclude data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Baseline and Week 26

InterventionPercent (Least Squares Mean)
Ertugliflozin 5 mg-0.78
Ertugliflozin 15 mg-0.86
Placebo-0.09

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Change From Baseline in FPG at Week 52

The change from baseline is the Week 52 FPG minus the Week 0 FPG. Laboratory measurements were performed after an overnight fast ≥10 hours in duration. Data presented exclude data following the initiation of rescue therapy. (NCT02036515)
Timeframe: Baseline and Week 52

Interventionmg/dL (Least Squares Mean)
Ertugliflozin 5 mg-25.57
Ertugliflozin 15 mg-26.38
Placebo3.19

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Absolute Change in FPG From Baseline to End of Core Phase

Absolute change in FPG from baseline to end of core phase in the incretin based therapy arm and the insulin arm. (NCT02060383)
Timeframe: Baseline, Up to 32 weeks (end of Core Phase)

,,,,
Interventionmg/dL (Mean)
Baseline: All PatientsChange at EOP: All PatientsBaseline: Cushing'sChange at EOP: Cushing'sBaseline: AcromegalyChange at EOP: Acromegaly
Baseline Insulin (BL) (Non-randomized Group)157.79.8147.221.3162.54.6
Incretin Based Therapy (Randomized Group)111.122.2117.913.4107.926.5
Insulin (Randomized Group)111.822.5106.336.4114.216.7
No OAD (Non-randomized Group)92.216.385.511.793.417.0
Oral Antidiabetic Drugs (OAD) (Non-randomized Group)97.222.993.315.898.825.8

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Change in HbA1c From Randomization to Approximately 16 Weeks

Absolute change in HbA1c from randomization to end of core phase (16 weeks) in incretin based therapy arm and insulin arm, and mean difference of change in HbA1c between the two treatment groups based on an ANOVA model using treatment (Incretin, Insulin) and the two randomization stratification factors (Disease: Cushing's disease vs Acromegaly; Baseline glycemic status: HbA1c <7% vs HbA1c ≥ 7%) as fixed effects. For Participants who discontinued the study or required rescue treatment before the time of assessing the primary endpoint, the last HbA1c assessment collected 8 weeks (56 days) after randomization (and prior to or on the date of start of rescue treatment) was carried forward. If the participant discontinued the study or used rescue treatment within 8 weeks after randomization, it was considered missing. (NCT02060383)
Timeframe: Randomization, 16 weeks

,
InterventionHba1c percentage (Mean)
All PatientsCushing's DiseaseAcromegaly
Incretin Based Therapy (Randomized Group)-0.120.33-0.25
Insulin (Randomized Group)0.260.450.19

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Change in HbA1c From Randomization (R) Over Time Per Randomized Arm

Absolute change in HbA1c overtime from randomization (i.e. start of randomized antidiabetic treatment) to end of core phase per randomized arm (NCT02060383)
Timeframe: Randomization (R), Week (W) 4 post R, W 8 post R, W 16 post R, end of Core phase (up to week 16 post R)

,
InterventionHbA1c percentage (Mean)
RandomizationChange at RW4 D29Change at RW8 D57Change at RW12 D85Change at RW16 D113End of Core Phase
Incretin Based Therapy (Randomized Group)7.10.50.30.20.00.0
Insulin (Randomized Group)7.10.50.50.40.30.3

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Change in FPG (Fasting Plasma Glucose) From Randomization Until End of Core Phase

Absolute change in fasting glucose overtime from randomization (i.e. start of randomized antidiabetic treatment) to end of core phase per randomized arm (NCT02060383)
Timeframe: Randomization, R(randomization) Week 2, R-Week 4, R-Week 6, R-Week 8, R-Week 10, R-Week 12, R-Week 14, R-Week 16, end of Core phase

,
Interventionmg/dL (Mean)
RandomizationChange at RW2 D15Change at RW4 D29Change at RW6 D43Change at RW8 D57Change at RW10 D71Change at RW12 D85Change at RW14 D99Change at RW16 D113End of Core Phase
Incretin Based Therapy (Randomized Group)172.24.6-15.0-17.7-25.7-28.8-33.4-35.1-38.8-40.1
Insulin (Randomized Group)167.9-31.1-28.3-37.5-38.3-36.9-41.1-35.6-33.4-36.0

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Absolute Change in HbA1c From Baseline to End of Core Phase

Absolute change in HbA1c from baseline to end of core phase in the incretin based therapy arm and the insulin arm (NCT02060383)
Timeframe: Baseline, up to 32 weeks (end of Core phase)

,,,,
InterventionHbA1c percentage (Mean)
Baseline: All PatientsChange at EOP: All PatientsBaseline: Cushing'sChange at EOP: Cushing'sBaseline: AcromegalyChange at EOP: Acromegaly
Baseline Insulin (BL) (Non-randomized Group)7.71.36.91.48.01.2
Incretin Based Therapy (Randomized Group)6.30.86.61.36.10.6
Insulin (Randomized Group)6.31.16.51.76.30.8
No OAD (Non-randomized Group)5.40.45.50.55.40.4
Oral Antidiabetic Drugs (OAD) (Non-randomized Group)5.70.85.90.95.60.7

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Percentage of Participants With ≤ 0.3% HbA1c Increase to End of Core Phase

Percentage of participants with ≤ 0.3% HbA1c increase in the incretin based therapy arm and the insulin arm. (NCT02060383)
Timeframe: Randomization, up to 16 weeks

InterventionPercentage of participants (Number)
Incretin Based Therapy (Randomized Group)73.7
Insulin (Randomized Group)65.1

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Percentage of Participants in the Incretin-based Arm Who Required Anti-diabetic Rescue Therapy With Insulin

The percentage of participants who received anti-diabetic rescue therapy in incretin based therapy is summarized. (NCT02060383)
Timeframe: Randomization to up to 16 weeks

InterventionPercentage of participants (Number)
Incretin Based Therapy (Randomized Group)31.6

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Change From Baseline of Estimated Glomerular Filtration Rate (eGFR)

The eGFR is used in addition to the Urinary Albumin to Creatinine Ratio to measure the incidence and progression of diabetic kidney disease. (NCT02072096)
Timeframe: Baseline, Week 72

Interventionmilliliter per minute/1.73 square meter (Mean)
Strategy A (Glucose-Dependent)-5.00
Strategy B (Reference)-5.88

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Change From Baseline in Body Mass Index (BMI)

(NCT02072096)
Timeframe: Baseline, Week 72

Interventionkilogram per square meter (kg/m^2) (Mean)
Strategy A (Glucose-Dependent)-0.47
Strategy B (Reference)0.20

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Change From Baseline of Urinary Albumin to Creatinine Ratio

The Urinary Albumin to Creatinine Ratio is used in addition to Estimated Glomerular Filtration Rate (eGFR) to measure the incidence and progression of diabetic kidney disease. (NCT02072096)
Timeframe: Baseline, Week 72

Interventionmilligram per millimole (mg/mmol) (Mean)
Strategy A (Glucose-Dependent)1.85
Strategy B (Reference)1.85

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Percentage of Participants Achieving and Maintaining Individualized Glycated Hemoglobin A1c (HbA1c) Targets Without Clinically Significant Hypoglycemia

Failed to reach and maintain HbA1c target, without clinically significant hypoglycemia, is defined as having 2 consecutive HbA1c > upper limit of HbA1c target over 12 weeks starting from Week 24 for participants with HbA1c data beyond Week 24, or Week 24 HbA1c > upper limit of HbA1c target for participants without HbA1c data beyond Week 24. Clinically significant hypoglycemia is defined as any severe hypoglycemia or repeated hypoglycemia interrupting participants activities or sleep and associated with blood glucose ≤3.9 millimole per liter (mmol/L), or repeated asymptomatic hypoglycemia associated with blood glucose <3.0 mmol/L. Success is defined as lacking of failure. (NCT02072096)
Timeframe: Baseline to last participant visit (up to 72 weeks)

Interventionpercentage of participants (Number)
Strategy A (Glucose-Dependent)64.5
Strategy B (Reference)54.9

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Number of Participants With Total Hypoglycemia and Other Categories of Hypoglycemia

(NCT02072096)
Timeframe: Baseline to last participant visit (up to 72 weeks)

,
InterventionParticipants (Number)
Total HypoglycemiaSevere HypoglycemiaClinically Significant HypoglycemiaSymptomatic HypoglycemiaAsymptomatic HypoglycemiaProbable Symptomatic HypoglycemiaUnspecified HypoglycemiaRelative HypoglycemiaNocturnal Hypoglycemia
Strategy A (Glucose-Dependent)1000580214
Strategy B (Reference)5001343077610

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Percentage of Participants Requiring Alternative Treatment Due to Glycemic Failure of First Line Injectable Therapy

(NCT02072096)
Timeframe: Baseline to last participant visit (up to 72 weeks)

Interventionpercentage of participants (Number)
Strategy A (Glucose-Dependent)21
Strategy B (Reference)13

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Change From Baseline in Body Weight at Week 26: Excluding Rescue Approach

This change from baseline reflects the Week 26 body weight minus the Week 0 body weight. Excluding recue approach data analysis excluded all data following the initiation of rescue therapy at any time point, in order to avoid the confounding influence of the rescue therapy. (NCT02099110)
Timeframe: Baseline and Week 26

InterventionKilograms (Least Squares Mean)
Ertugliflozin 5 mg-2.69
Ertugliflozin 15 mg-3.74
Sitagliptin 100 mg-0.67
Ertugliflozin 5 mg + Sitagliptin 100 mg-2.52
Ertugliflozin 15 mg + Sitagliptin 100 mg-2.94

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Change From Baseline in Sitting Systolic Blood Pressure at Week 26: Excluding Rescue Approach

This change from baseline reflects the Week 26 systolic blood pressure minus the Week 0 systolic blood pressure. Excluding recue approach data analysis excluded all data following the initiation of rescue therapy at any time point, in order to avoid the confounding influence of the rescue therapy. (NCT02099110)
Timeframe: Baseline and Week 26

Interventionmm Hg (Least Squares Mean)
Ertugliflozin 5 mg-3.89
Ertugliflozin 15 mg-3.69
Sitagliptin 100 mg-0.66
Ertugliflozin 5 mg + Sitagliptin 100 mg-3.42
Ertugliflozin 15 mg + Sitagliptin 100 mg-3.67

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Change From Baseline in Static Beta-Cell Sensitivity to Glucose Index at Week 26; Excluding Rescue Approach

Static beta-cell sensitivity to glucose index (SBCSGI) estimates the ratio of insulin secretion (expressed in pmol/min) related to above-basal glucose concentration (expressed in mmol/L * L) following a meal. Blood samples were collected before and after a standard meal and glucose, insulin, and C-peptide levels were analyzed. The C-peptides minimal model was used to estimate the insulin secretion rate (ISR). Analysis included both non-model-based [including insulinogenic index with C-peptide, glucose area under the curve (AUC)/insulin AUC] and model-based [beta cell function and insulin secretion rate at 9 mM glucose] testing. Analysis was performed with non-linear least squares using the Software Architecture Analysis Method (SAAM) II software. SBCSGI was expressed in units of 10^-9 min^-1. Excluding rescue approach data analysis excluded all data following the initiation of rescue therapy at any time point, in order to avoid the confounding influence of the rescue therapy. (NCT02099110)
Timeframe: 30 min. before and 0, 15, 30, 60, 90, 120, and 180 minutes following the start of the standard meal at Baseline and Week 26

InterventionSBCSGI (10^-9min^-1) (Least Squares Mean)
Ertugliflozin 5 mg8.62
Ertugliflozin 15 mg9.71
Sitagliptin 100 mg21.11
Ertugliflozin 5 mg + Sitagliptin 100 mg16.24
Ertugliflozin 15 mg + Sitagliptin 100 mg11.51

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 26 - Excluding Rescue Approach

Blood glucose was measured on a fasting basis after at least a 10-hour fast. This change from baseline reflects the Week 26 FPG minus the Week 0 FPG. Excluding recue approach data analysis excluded all data following the initiation of rescue therapy at any time point, in order to avoid the confounding influence of the rescue therapy. (NCT02099110)
Timeframe: Baseline and Week 26

Interventionmg/dL (Least Squares Mean)
Ertugliflozin 5 mg-35.73
Ertugliflozin 15 mg-36.91
Sitagliptin 100 mg-25.56
Ertugliflozin 5 mg + Sitagliptin 100 mg-43.96
Ertugliflozin 15 mg + Sitagliptin 100 mg-48.70

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Percentage of Participants Who Experienced an Adverse Event (AE): Including Rescue Approach

An AE is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure, that occurs during the course of the study. Including rescue approach data analysis included data following the initiation of rescue therapy. (NCT02099110)
Timeframe: Up to 54 weeks

InterventionPercentage of participants (Number)
Ertugliflozin 5 mg62.0
Ertugliflozin 15 mg57.7
Sitagliptin 100 mg57.5
Ertugliflozin 5 mg + Sitagliptin 100 mg58.8
Ertugliflozin 15 mg + Sitagliptin 100 mg55.7

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Percentage of Participants Who Discontinued Study Treatment Due to an AE: Including Rescue Approach

An AE is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure, that occurs during the course of the study. Including rescue approach data analysis included data following the initiation of rescue therapy. (NCT02099110)
Timeframe: Up to 52 weeks

InterventionPercentage of participants (Number)
Ertugliflozin 5 mg3.2
Ertugliflozin 15 mg3.2
Sitagliptin 100 mg2.8
Ertugliflozin 5 mg + Sitagliptin 100 mg3.3
Ertugliflozin 15 mg + Sitagliptin 100 mg3.7

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Change From Baseline in A1C at Week 26: Excluding Rescue Approach

A1C is blood marker used to report average blood glucose levels over prolonged periods of time and is reported as a percentage (%). This change from baseline reflects the Week 26 A1C minus the Week 0 A1C. Excluding recue approach data analysis excluded all data following the initiation of rescue therapy at any time point, in order to avoid the confounding influence of the rescue therapy. (NCT02099110)
Timeframe: Baseline and Week 26

InterventionPercentage (Least Squares Mean)
Ertugliflozin 5 mg-1.02
Ertugliflozin 15 mg-1.08
Sitagliptin 100 mg-1.05
Ertugliflozin 5 mg + Sitagliptin 100 mg-1.49
Ertugliflozin 15 mg + Sitagliptin 100 mg-1.52

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Percentage of Participants Achieving a Hemoglobin A1C of <7% (<53 mmol/Mol) (Raw Proportions): Excluding Rescue Approach

A1C is blood marker used to report average blood glucose levels over a prolonged periods of time and is reported as a percentage (%). Excluding recue approach data analysis excluded all data following the initiation of rescue therapy at any time point, in order to avoid the confounding influence of the rescue therapy. (NCT02099110)
Timeframe: Week 26

InterventionPercentage of participants (Number)
Ertugliflozin 5 mg26.4
Ertugliflozin 15 mg31.9
Sitagliptin 100 mg32.8
Ertugliflozin 5 mg + Sitagliptin 100 mg52.3
Ertugliflozin 15 mg + Sitagliptin 100 mg49.2

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Rate of Hypoglycemic Events Adjusted Per 30 Days

Documented symptomatic hypoglycemia, an event during which typical symptoms of hypoglycemia are accompanied by a measured plasma glucose concentration <=70 mg/dL (<=39 mmol/L),is presented. Rate: (30 days) is calculated as: (number of episodes during the time period divided by the number of days during the time period) multiplied by 30. (NCT02111096)
Timeframe: Baseline through 6 months

Interventionnumber of episodes per day (Number)
LY24090210.27
Sitagliptin0.19
Placebo0.12

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Population Pharmacokinetics: Apparent Volume of Distribution of LY2409021

(NCT02111096)
Timeframe: Day 1 Month 1, 3, 6, 9, predose, 1 hour postdose,

InterventionLiters (L) (Number)
LY240902131.9

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Population Pharmacokinetics: Apparent Clearance of LY2409021

Reported as a Population Estimate with % Standard Errors of Estimation (SEE), 5th-95th confidence interval. (NCT02111096)
Timeframe: Day 1 Month 1, 3, 6, 9, predose, 1 hour postdose,

InterventionLiters per hour (L/h) (Number)
LY24090210.526

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Number of Participants With Hypoglycemic Events

Documented symptomatic hypoglycemia, an event during which typical symptoms of hypoglycemia are accompanied by a measured plasma glucose concentration <=70 mg/dL (<=39 mmol/L), is presented. The number of subjects with an event are subjects who had at least one episode of documented symptomatic hypoglycemia during the time period. (NCT02111096)
Timeframe: Baseline through 6 months

InterventionParticipants (Count of Participants)
LY240902120
Sitagliptin40
Placebo68

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Number of Participants With Hepatobiliary Adverse Events of Special Interest (AESI)

Number of participants with ALT or AST greater than 3 times the upper limit of normal at a post-baseline visit. A summary of other non-serious AEs, and all SAE's, regardless of causality, is located in the Reported Adverse Events section. (NCT02111096)
Timeframe: Baseline, 6 months

InterventionParticipants (Count of Participants)
LY24090210
Sitagliptin1
Placebo1

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Change From Baseline to 6 Months in Pulse Rate

Seated pulse rate was measured in triplicate throughout the study. At each visit, all available pulse measurements for a subject were averaged to provide the pulse for that visit. Least Squares (LS) means were calculated using mixed model repeated measures (MMRM) adjusting for treatment, country, baseline HbA1c stratum (<=8.0%, >8.0%), visit, baseline score, and treatment-by-visit. (NCT02111096)
Timeframe: Baseline, 6 months

Interventionbeats per minutes (bpm) (Least Squares Mean)
LY24090211.5
Sitagliptin3.5
Placebo1.2

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Change From Baseline to 6 Months in Fasting Blood Glucagon

Glucagon values assessed by a central laboratory. Least Squares (LS) means were calculated using mixed model repeated measures (MMRM) adjusting for treatment, country, baseline HbA1c stratum (<=8.0%, >8.0%), visit, baseline score, and treatment-by-visit. (NCT02111096)
Timeframe: Baseline, 6 months

Interventionpicomol per liter (pmol/L) (Least Squares Mean)
LY240902144.06
Sitagliptin3.38
Placebo5.05

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Change From Baseline to 6 Months in Hemoglobin A1c (HbA1c)

HbA1c is a form of hemoglobin that is measured primarily to identify the average plasma glucose concentration over prolonged periods of time. Least Squares (LS) means were calculated using mixed model repeated measures (MMRM) adjusting for treatment, country, visit, baseline score, and treatment-by-visit. (NCT02111096)
Timeframe: Baseline, 6 months

Interventionpercent of HbA1c (Least Squares Mean)
LY2409021-0.63
Sitagliptin-0.42
Placebo0.14

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Change From Baseline to 6 Months in Fasting Plasma Glucose

Least Squares (LS) means were calculated using mixed model repeated measures (MMRM) adjusting for treatment, country, baseline HbA1c stratum (<=8.0%, >8.0%), visit, baseline score, and treatment-by-visit. (NCT02111096)
Timeframe: Baseline, 6 months

Interventionmilligram per decililiter (mg/dL) (Least Squares Mean)
LY2409021-20.5
Sitagliptin-9.4
Placebo6.6

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Change From Baseline to 6 Months in Hepatic Fat Fraction

The hepatic fat fraction (HFF) was calculated by a core imaging laboratory from noncontrast magnetic resonance imaging (MRI) of the liver. Least Squares (LS) means were calculated using mixed model repeated measures (MMRM) adjusting for treatment, country, baseline HbA1c stratum (<=8.0%, >8.0%), visit, baseline score, and treatment-by-visit. (NCT02111096)
Timeframe: Baseline, 6 months

Interventionpercentage (Least Squares Mean)
LY24090213.65
Sitagliptin-0.07
Placebo-0.79

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Change From Baseline to 6 Months in Body Weight

Least Squares (LS) means were calculated using mixed model repeated measures (MMRM) adjusting for treatment, country, baseline HbA1c stratum (<=8.0%, >8.0%), visit, baseline score, and treatment-by-visit. (NCT02111096)
Timeframe: Baseline, 6 months

Interventionkilograms (kg) (Least Squares Mean)
LY24090210.37
Sitagliptin-0.08
Placebo-0.05

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Change From Baseline to 6 Months in Alanine Aminotransferase Levels

Alanine aminotransferase (ALT) assessed by a central laboratory. Least Squares (LS) means were calculated using mixed model repeated measures (MMRM) adjusting for treatment, country, baseline HbA1c stratum (<=8.0%, >8.0%), visit, baseline score, and treatment-by-visit. (NCT02111096)
Timeframe: Baseline, 6 months

Interventionmicrogram per Liter (µ/L) (Least Squares Mean)
LY24090219.4
Sitagliptin2.6
Placebo-1.3

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Change From Baseline to 6 Months in Fasting Lipids Levels

Lipid values (cholesterol, HDL cholesterol, LDL cholesterol, and triglycerides) assessed by a central laboratory. Least Squares (LS) means were calculated using mixed model repeated measures (MMRM) adjusting for treatment, country, baseline HbA1c stratum (<=8.0%, >8.0%), visit, baseline score, and treatment-by-visit. (NCT02111096)
Timeframe: Baseline, 6 months

,,
Interventionmillimol per liter (mmol/L) (Least Squares Mean)
CholesterolHDL CholesterolTriglyceridesLDL cholesterol
LY24090210.4680.0460.3750.244
Placebo0.130-0.0210.0990.019
Sitagliptin0.0060.0320.078-0.075

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Change From Baseline to 6 Months in 7-Point Self-Monitoring of Blood Glucose (SMBG)

7-point profile consists of pre-meal and 2-hour postprandial SMBG measurements for the morning, midday, and evening meals in 1 day and at 3 AM (nocturnal blood glucose measurement). Pre-meal measurements were taken before the subject began eating the meal. Participants recorded their glucose measurements in their study diaries. (NCT02111096)
Timeframe: Baseline, 6 months

,,
Interventionmg/dL (Mean)
Morning Pre-MealMid-day Pre MealMorning 2 Hour (Hr) Post MealMidday 2 hr Post MealEvening Pre MealEvening 2 hr Post MealThree AM
LY2409021-29.4-28.43-38.8-24.22-24.58-28.36-22.78
Placebo-4.31-9.30-18.28-10.49-14.13-9.500.88
Sitagliptin-8.13-30.58-30.76-25.20-16.78-21.12-20.12

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Change From Baseline to 6 Months in Blood Pressure

Seated systolic blood pressure (SBP) and seated diastolic blood pressure (DBP) were measured in triplicate throughout the study. At each visit, all available blood pressure measurements for a subject were averaged to provide the blood pressure for that visit. Least Squares (LS) means were calculated using mixed model repeated measures (MMRM) adjusting for treatment, country, baseline HbA1c stratum (<=8.0%, >8.0%), visit, baseline score, and treatment-by-visit. (NCT02111096)
Timeframe: Baseline, 6 months

,,
Interventionmillimeters of mercury (mm/Hg) (Least Squares Mean)
Systolic Blood PressureDiastolic Blood Pressure
LY24090216.12.9
Placebo1.81.5
Sitagliptin1.10.3

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Visceral Adipose Tissue

During the inpatient visit of each treatment (placebo and sitagliptin), visceral adipose tissue was determined by a certified densitometrist using dual-energy x-ray absorptiometry with enCore software (v. 13.6) (NCT02122380)
Timeframe: At completion of 30 days of placebo treatment and at completion of 30 days of sitagliptin treatment.

Interventiongrams (Mean)
Placebo1141.9
Sitagliptin1055.1

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Vascular Function (Endothelium-dependent Vasodilation)

Endothelium-dependent vasodilation was evaluated by measuring the diameter of the brachial artery under basal (i.e. rest) condition and during reactive hyperemia. The percentage change in diameter (i.e. endothelium-dependent vasodilation) was calculated as percent change=[(peak diameter-baseline diameter)/baseline diameter]*100. Endothelium-dependent vasodilation was determined twice during the study: at completion of 30 days of placebo treatment and at completion of 30 days of sitagliptin treatment. (NCT02122380)
Timeframe: Vascular function was determined by measuring brachial artery diameter at rest and during reactive hyperemia and calculating percent change. This was determined after 30 days of placebo treatment and after 30 days of sitagliptin treatment.

Interventionpercent change (Mean)
Placebo13.63
Sitagliptin13.00

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Early Insulin Secretion During Oral Glucose Tolerance Test

Oral glucose tolerance testing was performed with 75 grams of glucose solution. Baseline venous blood samples of insulin were obtained prior to ingestion of oral glucose solution (time 0). Insulin levels were then obtained through a peripheral IV line every 15 minutes for 270 minutes after glucose solution is swallowed. Early insulin secretion was determined by calculating area under the curve using data (i.e. insulin levels) obtained at baseline (time 0), 15 minutes and 30 minutes. (NCT02122380)
Timeframe: During Outpatient Visit (after 2 weeks of therapy) during placebo and sitagliptin treatment periods. Insulin levels were obtained at time 0, 15 and 30 minutes following 75 gram glucose ingestion.

InterventionmicroU*minutes/mL (Mean)
Placebo1522.1
Sitagliptin1871.3

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Area Under the Curve (AUC) for Blood Glucoses During 75 Gram Oral Glucose Tolerance Test

Oral glucose tolerance testing was performed with 75 grams of glucose solution. Baseline blood glucose was obtained prior to ingestion of oral glucose solution (time 0). Blood glucose levels were then obtained through a peripheral IV line every 15 minutes from timepoint 0 until 120 minutes to calculate the area under the curve. (NCT02122380)
Timeframe: During Outpatient Visit (after 2 weeks of therapy) during placebo and sitagliptin treatment periods. Every 15 minutes from time 0 to 120 minutes after oral glucose ingestion.

Interventionmg*minutes/dL (Mean)
Placebo15353.8
Sitagliptin13877.5

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Mean Overnight Growth Hormone Levels

Growth hormone levels were determined every 10 minutes from 8 PM until 8 AM during the inpatient visit on the last day of each treatment. A mean of the GH levels was calculated for each participant, and then the value from each participant was averaged across all participants. (NCT02122380)
Timeframe: At completion of 30 days of placebo treatment and at completion of 30 days of sitagliptin treatment; every 10 minutes from 8 PM until 8 AM.

Interventionng/mL (Mean)
Placebo0.85
Sitagliptin0.84

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Heart Rate

The average of measurements made every five minutes prior to (time 0) and for four four hours after ingestion of a mixed meal (NCT02130687)
Timeframe: Value provided is the average of measurements made every five minutes prior to (time 0) and for four four hours after ingestion of a mixed meal.

Interventionbpm (Mean)
Amlodipine Plus Placebo/Placebo71.8
Amlodipine Plus Sitagliptin/Placebo70.3
Amlodipine Plus Sitagliptin/Aprepitant71.7
Ramipril Plus Placebo/Placebo69.9
Ramipril Plus Sitagliptin/Placebo73.3
Ramipril Plus Sitagliptin/Aprepitant72.0
Valsartan Plus Placebo/Placebo70.3
Valsartan Plus Sitagliptin/Placebo71.9
Valsartan Plus Sitagliptin/Aprepitant71.9

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Norepinephrine (NE) Concentrations

The primary analyses will focus on blood pressure, heart rate, and norepinephrine (NE) concentrations during ramipril versus ramipril+sitagliptin, and during ramipril+sitagliptin versus ramipril+sitagliptin+aprepitant. We will make similar comparisons within the valsartan- and placebo-treated groups. In addition, we will compare blood pressure and heart rate parameters among the ramipril-treated, valsartan-treated, and placebo-treated groups during comparable concurrent treatment. (NCT02130687)
Timeframe: 4.5 hours on the 7th day of each intervention (placebo, sitagliptin, or sitagliptin+aprepitant)

Interventionpg/mL (Mean)
Amlodipine Plus Placebo/Placebo741.65
Amlodipine Plus Sitagliptin/Placebo730.88
Amlodipine Plus Sitagliptin/Aprepitant610.65
Ramipril Plus Placebo/Placebo470.69
Ramipril Plus Sitagliptin/Placebo627.55
Ramipril Plus Sitagliptin/Aprepitant649.39
Valsartan Plus Placebo/Placebo874.22
Valsartan Plus Sitagliptin/Placebo986.31
Valsartan Plus Sitagliptin/Aprepitant1013.54

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Neuropeptide Y

Measurement of Neuropeptide Y (NPY) concentrations (NCT02130687)
Timeframe: Neuropeptide Y concentration prior to ingestion of the mixed meal.

InterventionpM (Mean)
Amlodipine Plus Placebo/Placebo0.35
Amlodipine Plus Sitagliptin/Placebo0.52
Amlodipine Plus Sitagliptin/Aprepitant0.51
Ramipril Plus Placebo/Placebo0.32
Ramipril Plus Sitagliptin/Placebo0.54
Ramipril Plus Sitagliptin/Aprepitant0.52
Valsartan Plus Placebo/Placebo0.27
Valsartan Plus Sitagliptin/Placebo0.50
Valsartan Plus Sitagliptin/Aprepitant0.47

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Dipeptidyl Peptidase IV (DPP4) Activity

Measure of DPP4 inhibitor administration. (NCT02130687)
Timeframe: for 4.5 hours on the 7th day of each intervention (placebo, sitagliptin, sitagliptin+aprepitant)

Interventionnmol/mL/min (Mean)
Amlodipine Plus Placebo/Placebo20.27
Amlodipine Plus Sitagliptin/Placebo7.34
Amlodipine Plus Sitagliptin/Aprepitant6.96
Ramipril Plus Placebo/Placebo20.61
Ramipril Plus Sitagliptin/Placebo8.78
Ramipril Plus Sitagliptin/Aprepitant7.71
Valsartan Plus Placebo/Placebo19.4
Valsartan Plus Sitagliptin/Placebo7.83
Valsartan Plus Sitagliptin/Aprepitant6.70

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Heart Rate

The primary analyses will focus on blood pressure, heart rate, and norepinephrine (NE) concentrations during ramipril versus ramipril+sitagliptin, and during ramipril+sitagliptin versus ramipril+sitagliptin+aprepitant. We will make similar comparisons within the valsartan- and placebo-treated groups. In addition, we will compare blood pressure and heart rate parameters among the ramipril-treated, valsartan-treated, and placebo-treated groups during comparable concurrent treatment. (NCT02130687)
Timeframe: 4.5 hours on the 7th day of each intervention (placebo, sitagliptin, or sitagliptin+aprepitant)

Interventionbeats per minute (Mean)
Amlodipine Plus Placebo/Placebo69.59
Amlodipine Plus Sitagliptin/Placebo70.43
Amlodipine Plus Sitagliptin/Aprepitant69.41
Ramipril Plus Placebo/Placebo66.58
Ramipril Plus Sitagliptin/Placebo66.30
Ramipril Plus Sitagliptin/Aprepitant66.15
Valsartan Plus Placebo/Placebo66.19
Valsartan Plus Sitagliptin/Placebo65.86
Valsartan Plus Sitagliptin/Aprepitant65.10

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Insulin

Measure of insulin resistance. (NCT02130687)
Timeframe: fasting insulin measured at 3 hours on the 7th day of each intervention (placebo, sitagliptin, sitatliptin+aprepitant)

InterventionmicroU/mL (Mean)
Amlodipine Plus Placebo/Placebo20.7
Amlodipine Plus Sitagliptin/Placebo20.72
Amlodipine Plus Sitagliptin/Aprepitant20.22
Ramipril Plus Placebo/Placebo26.15
Ramipril Plus Sitagliptin/Placebo22.59
Ramipril Plus Sitagliptin/Aprepitant26.02
Valsartan Plus Placebo/Placebo21.39
Valsartan Plus Sitagliptin/Placebo19.92
Valsartan Plus Sitagliptin/Aprepitant16.83

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Mean Arterial Blood Pressure

The primary analyses will focus on mean arterial blood pressure, heart rate, and norepinephrine (NE) concentrations during ramipril versus ramipril+sitagliptin, and during ramipril+sitagliptin versus ramipril+sitagliptin+aprepitant. We will make similar comparisons within the valsartan- and placebo-treated groups. In addition, we will compare blood pressure and heart rate parameters among the ramipril-treated, valsartan-treated, and placebo-treated groups during comparable concurrent treatment. (NCT02130687)
Timeframe: 4.5 hours on the 7th day of each intervention (placebo, sitagliptin, or sitagliptin+aprepitant)

InterventionmmHg (Mean)
Amlodipine Plus Placebo/Placebo94.42
Amlodipine Plus Sitagliptin/Placebo93.41
Amlodipine Plus Sitagliptin/Aprepitant91.54
Ramipril Plus Placebo/Placebo90.21
Ramipril Plus Sitagliptin/Placebo89.88
Ramipril Plus Sitagliptin/Aprepitant86.95
Valsartan Plus Placebo/Placebo94.54
Valsartan Plus Sitagliptin/Placebo93.71
Valsartan Plus Sitagliptin/Aprepitant93.98

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Mean Arterial Blood Pressure

Average of measurements made every five minutes beginning just prior to (time 0) and for four hours after the ingestion of a mixed meal (NCT02130687)
Timeframe: Value provided is the AVERAGE of measurements made every five minutes prior to (time 0) and for four four hours after ingestion of a mixed meal.

InterventionmmHg (Mean)
Amlodipine Plus Placebo/Placebo96.0
Amlodipine Plus Sitagliptin/Placebo93.6
Amlodipine Plus Sitagliptin/Aprepitant92.9
Ramipril Plus Placebo/Placebo94.2
Ramipril Plus Sitagliptin/Placebo92.6
Ramipril Plus Sitagliptin/Aprepitant91.0
Valsartan Plus Placebo/Placebo94.2
Valsartan Plus Sitagliptin/Placebo96.1
Valsartan Plus Sitagliptin/Aprepitant94.5

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24hr Urinary Testing for Sodium

Subjects will collect 24hr urine sample and bring with to the study day for analysis (NCT02130687)
Timeframe: Urine was collected for sodium for 24 hrs prior to each of the study days listed below. Study days occurred after each 7-day treatment arm (placebo/placebo, sitagliptin/placebo, or sitagliptin/aprepitant) within 3 anti-hypertensive groups.

InterventionmEq (Mean)
Amlodipine Plus Placebo/Placebo147.66
Amlodipine Plus Sitagliptin/Placebo146.90
Amlodipine Plus Sitagliptin/Aprepitant154.42
Ramipril Plus Placebo/Placebo177.70
Ramipril Plus Sitagliptin/Placebo162.05
Ramipril Plus Sitagliptin/Aprepitant142.95
Valsartan Plus Placebo/Placebo158.77
Valsartan Plus Sitagliptin/Placebo138.65
Valsartan Plus Sitagliptin/Aprepitant160.92

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Low Frequency Variability of Blood Pressure Activity

Low frequency variability of systolic blood pressure will be measured using spectral analysis. (NCT02130687)
Timeframe: for 5 minutes on the 7th day of each intervention (placebo, sitagliptin, sitagliptin+aprepitant)

InterventionmmHg2 (Mean)
Amlodipine Plus Placebo/Placebo5.14
Amlodipine Plus Sitagliptin/Placebo7.32
Amlodipine Plus Sitagliptin/Aprepitant7.07
Ramipril Plus Placebo/Placebo8.78
Ramipril Plus Sitagliptin/Placebo7.27
Ramipril Plus Sitagliptin/Aprepitant12.18
Valsartan Plus Placebo/Placebo8.51
Valsartan Plus Sitagliptin/Placebo7.81
Valsartan Plus Sitagliptin/Aprepitant8.58

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Angiotensin Converting Enzyme (ACE) Activity

This is a measure of activity of the angiotensin-converting enzyme (ACE). The assay is a kinetic assay (Labcore) that measures the rate of cleavage of an added ACE substrate over time and the results are reported in Units, which represent the rate of increase in fluorescent metabolite over 30 minutes under standard conditions at 37C. (NCT02130687)
Timeframe: for 4.5 hours on the 7th day of each intervention (placebo, sitagliptin, sitagliptin+aprepitant)

InterventionUnits (Mean)
Amlodipine Plus Placebo/Placebo37.00
Amlodipine Plus Sitagliptin/Placebo40.15
Amlodipine Plus Sitagliptin/Aprepitant35.78
Ramipril Plus Placebo/Placebo15.44
Ramipril Plus Sitagliptin/Placebo14.69
Ramipril Plus Sitagliptin/Aprepitant13.46
Valsartan Plus Placebo/Placebo37.21
Valsartan Plus Sitagliptin/Placebo36.68
Valsartan Plus Sitagliptin/Aprepitant36.89

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Glucose

measure of effectiveness of DPP4 inhibitor (NCT02130687)
Timeframe: fasting at 3 hours on the 7th day of each intervention (placebo, sitagliptin, sitagliptin+aprepitant)

Interventionmg/dL (Mean)
Amlodipine Plus Placebo/Placebo123.78
Amlodipine Plus Sitagliptin/Placebo112.51
Amlodipine Plus Sitagliptin/Aprepitant109.08
Ramipril Plus Placebo/Placebo118.04
Ramipril Plus Sitagliptin/Placebo107.55
Ramipril Plus Sitagliptin/Aprepitant107.66
Valsartan Plus Placebo/Placebo112.01
Valsartan Plus Sitagliptin/Placebo103.69
Valsartan Plus Sitagliptin/Aprepitant99.75

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Number of Events With the Rating on Quality of Stools as Rated Using the BSFS Across Days 1 to 14

The site staff classified participant's stools and record the date and time of occurrence after any bowel movement that occurs while participants were in residence in the clinic. BSFS is scale between type 1-7, it measured the shape of the stool, type 1: separate hard lumps, like nuts; type 2: sausage shaped but lumpy; type 3: like a sausage or snake but with cracks on its surface; type 4: like a sausage or snake, smooth and soft; type 5: soft blobs with clear cut edges; type 6: fluffy pieces with ragged edges, a mushy stool and type 7: watery, no solid pieces. Participants were discharged after they have had at least one bowel movement after the Day 14 dosing and after the investigator/designee had reviewed the Day 15 end of study questions. (NCT02202161)
Timeframe: Up to Day 15 (administered after every in-house bowel movement)

,,
InterventionEvents (Number)
BSFS scale rating, 1 event : EventsBSFS scale rating, 2 events : EventsBSFS scale rating, 3 events : EventsBSFS scale rating, 4 events : EventsBSFS scale rating, 5 events : EventsBSFS scale rating, 6 events : EventsBSFS scale rating, 7 events : Events
GSK2330672 30 mg BID111192618186
Placebo262856305916
Sitagliptin 50 mg BID2103641267010

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Number of Participants With Abnormal Hematology With Potential Clinical Concern (PCI)

Hematology parameters included platelet, red blood cell (RBC) count, mean corpuscular volume (MCV), neutrophils, white blood cell (WBC) count (absolute), mean corpuscular hemoglobin (MCH), lymphocytes, mean corpuscular hemoglobin concentration (MCHC), monocytes, hemoglobin, eosinophils, hematocrit and basophils. It was assessed on Baseline (pre-dose Day -1), Day 7 and 15. Data for parameters with above and below the PCI is provided. (NCT02202161)
Timeframe: Up to Day 15

InterventionParticipants (Count of Participants)
Placebo0
GSK2330672 10 mg BID0
GSK2330672 20 mg BID0
GSK2330672 30 mg BID0
GSK2330672 60 mg BID0
GSK2330672 90 mg BID1
Sitagliptin 50 mg BID0

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Number of Bowel Movements (Stool Frequency) as Rated Using the Bristol Stool Form Scale (BSFS) Across Days 1 to 14

The site staff classified participant's stools and record the date and time of occurrence after any bowel movement that occurs while participants were in residence in the clinic. BSFS is scale between type 1-7, it measured the shape of the stool, type 1: separate hard lumps, like nuts; type 2: sausage shaped but lumpy; type 3: like a sausage or snake but with cracks on its surface; type 4: like a sausage or snake, smooth and soft; type 5: soft blobs with clear cut edges; type 6: fluffy pieces with ragged edges, a mushy stool and type 7: watery, no solid pieces. Participants were discharged after they have had at least one bowel movement after the Day 14 dosing and after the investigator/designee had reviewed the Day 15 end of study questions. (NCT02202161)
Timeframe: Up to Day 15 (administered after every in-house bowel movement)

InterventionCount of bowel movements (Mean)
Placebo15.2
GSK2330672 10 mg BID28.2
GSK2330672 20 mg BID38.4
GSK2330672 30 mg BID35.0
GSK2330672 60 mg BID37.3
GSK2330672 90 mg BID35.9
Sitagliptin 50 mg BID15.0

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Number of Participants With Fecal Occult Blood Monitoring for Symptomatic or Visible Gastrointestinal Bleeding or Asymptomatic Occult Bleeding

Testing cards were provided to participants for assessments. Participants with abnormal not clinically significant and abnormal clinically significant is presented. The Day -1 sample was obtained any time starting Day -2 and prior to GSK2330672 dosing on Day 1. The Day 14 sample was collected any time after dosing on Day 14 and prior to discharge on Day 15. (NCT02202161)
Timeframe: Up to Day 15

,,,,,,,
InterventionParticipants (Count of Participants)
Abnormal not clinically significantAbnormal clinically significant
GSK2330672 10 mg BID10
GSK2330672 20 mg BID10
GSK2330672 30 mg BID00
GSK2330672 60 mg BID00
GSK2330672 90 mg BID11
Placebo00
Run-in Only02
Sitagliptin 50 mg BID10

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PK Parameters for Metformin Steady State PK Parameters When Co-dosed With GSK2330672, Sitagliptin or Placebo-maximum Observed Concentration (Cmax)

The first occurrence of the maximum observed plasma concentration determined directly from the raw concentration-time data. Statistics for geometric least square mean provided. (NCT02202161)
Timeframe: Fasting pre-dose (within 15 minutes of dose), 30 minutes, 1, 1.5, 2, 3, 4 (pre-lunch), 5.5, 8, 10 hours (pre-dinner) on Day 14

InterventionNanograms per milliliter (ng/mL) (Geometric Least Squares Mean)
Placebo1102.2
GSK2330672 10 mg BID1289.3
GSK2330672 20 mg BID1219.9
GSK2330672 30 mg BID1160.0
GSK2330672 60 mg BID1378.8
GSK2330672 90 mg BID1376.6
Sitagliptin 50 mg BID1223.5

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Summary of Urinalysis Data-mean Specific Gravity

Data for mean specific gravity is provided. Specific gravity is a measure of the amount of material dissolved in the urine. Specific gravity is the ratio of the density (mass of a unit volume) of a substance to the density (mass of the same unit volume) of a reference substance. Normal urine has a specific gravity between 1.010 and 1.020. (NCT02202161)
Timeframe: Baseline (pre-dose Day -1), Day 7 and 15

,,,,,,
InterventionRatio (Mean)
Day -1Day 7Day 15
GSK2330672 10 mg BID1.01821.02081.0193
GSK2330672 20 mg BID1.01281.01841.0158
GSK2330672 30 mg BID1.01901.01911.0132
GSK2330672 60 mg BID1.01721.01941.0121
GSK2330672 90 mg BID1.01891.02081.0160
Placebo1.01931.01961.0188
Sitagliptin 50 mg BID1.01481.01601.0140

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Summary of Urinalysis Data-mean pH

Urine pH is an acid-base measurement. pH is measured on a numeric scale ranging from 0 to 14; values on the scale refer to the degree of alkalinity or acidity. A pH of 7 is neutral. A pH less than 7 is acidic, and a pH greater than 7 is basic. Normal urine has a slightly acid pH (5.0 - 6.0). (NCT02202161)
Timeframe: Baseline (pre-dose Day -1), Day 7 and 15

,,,,,,
InterventionUnit on a scale (Mean)
Day -1Day 7Day 15
GSK2330672 10 mg BID6.005.905.88
GSK2330672 20 mg BID6.106.006.00
GSK2330672 30 mg BID6.115.896.00
GSK2330672 60 mg BID5.835.615.72
GSK2330672 90 mg BID5.955.956.06
Placebo5.735.835.88
Sitagliptin 50 mg BID5.855.695.88

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Sitagliptin Steady State PK Parameters When Co-dosed With Metformin-Tmax Following the First and Second Sitagliptin Doses

The time at which Cmax was observed by determining directly from the raw concentration-time data following the first and second dose of sitagliptin on Day 14 (Tmax1 and Tmax2). If data permits, Tmax2 was defined as the time of Cmax following the second dose of sitagliptin. (NCT02202161)
Timeframe: Fasting pre-dose (within 15 minutes of dose), 1, 2, 3, 4 (pre-lunch), 10 (pre-dinner), 13 and 14 hours (bed time) on Day 14

InterventionHour (Median)
Tmax 1Tmax 2
Sitagliptin 50 mg BID2.0003.050

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Sitagliptin Steady State PK Parameters When Co-dosed With Metformin-Cmax Following the First and Second Sitagliptin Doses

The first occurrence of the maximum observed plasma concentration determined directly from the raw concentration-time data following the first and second dose of sitagliptin on Day 14 (Cmax1 and Cmax2). (NCT02202161)
Timeframe: Fasting pre-dose (within 15 minutes of dose), 1, 2, 3, 4 (pre-lunch), 10 (pre-dinner), 13 and 14 hours (bed time) on Day 14

InterventionNg/mL (Geometric Mean)
Cmax 1Cmax 2
Sitagliptin 50 mg BID238.2188.5

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Ratio to Baseline in Fasting Low-density Cholesterol (LDL) Cholesterol, High-density Cholesterol (HDL) Cholesterol, Total Cholesterol, Non-HDL Cholesterol and Triglycerides

Data for fasting low-density cholesterol (LDL) cholesterol, high-density cholesterol (HDL) cholesterol, total cholesterol, non-HDL cholesterol and triglycerides is presented. Participants withdrawing early were excluded. Results were based on an ANCOVA model: Log(post-Baseline) - Log(Baseline) = Log(Baseline) + treatment + concomitant use of lipid lowering drugs. (NCT02202161)
Timeframe: Baseline (pre-dose Day -1) and Day 7, 14

,,,,,,
InterventionRatio (Geometric Mean)
Cholesterol, Day 7Cholesterol, Day 14HDL cholesterol, Day 7HDL cholesterol, Day 14LDL cholesterol, Day 7LDL cholesterol, Day 14Non-HDL Cholesterol, Day 7Non-HDL Cholesterol, Day 14Triglycerides, Day 7Triglycerides, Day 14
GSK2330672 10 mg BID0.990.981.081.110.890.800.960.941.071.21
GSK2330672 20 mg BID0.840.811.051.020.770.690.780.740.930.96
GSK2330672 30 mg BID0.840.830.970.970.730.720.800.781.111.07
GSK2330672 60 mg BID0.740.750.950.960.580.600.650.670.981.00
GSK2330672 90 mg BID0.800.751.091.010.710.670.730.680.931.00
Placebo0.950.951.000.990.970.940.930.940.850.85
Sitagliptin 50 mg BID0.970.920.970.971.000.920.980.900.790.74

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Ratio to Baseline in Fasting Apolipoprotein B

Data for fasting apolipoprotein B is presented. Participants withdrawing early were excluded. Results were based on an ANCOVA model: Log(post-Baseline) - Log(Baseline) = Log(Baseline) + treatment + concomitant use of lipid lowering drugs. (NCT02202161)
Timeframe: Baseline (pre-dose Day -1) and Day 7, 14

,,,,,,
InterventionRatio (Geometric Mean)
Day 7Day 14
GSK2330672 10 mg BID0.950.85
GSK2330672 20 mg BID0.780.75
GSK2330672 30 mg BID0.810.78
GSK2330672 60 mg BID0.690.67
GSK2330672 90 mg BID0.760.69
Placebo0.970.93
Sitagliptin 50 mg BID0.960.88

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Number of Participants With Incidence and Nature of Adverse Events (AEs) and Serious Adverse Events (SAEs)

An AE was defined as any untoward medical occurrence (MO) in a participant temporally associated with the use of a medicinal product (MP), whether or not considered related to the MP and can therefore be any unfavourable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with its use. The SAE was any untoward MO that, at any dose, results in death, life threatening, persistent or significant disability/incapacity, results in or prolongs inpatient hospitalization, congenital abnormality or birth defect, that may not be immediately life-threatening or result in death or hospitalization but may jeopardize the participant or may require medical or surgical intervention to prevent one of the other outcomes listed in this definition and alanine aminotransferase (ALT) >= 3× upper limit of normal (ULN) and total bilirubin >=2 × ULN (>35% direct) or ALT >=3 × ULN and international normalized ratio >1.5. (NCT02202161)
Timeframe: Up to 14 days (treatment period)

,,,,,,
InterventionParticipants (Count of Participants)
Any AEAny SAE
GSK2330672 10 mg BID41
GSK2330672 20 mg BID50
GSK2330672 30 mg BID50
GSK2330672 60 mg BID80
GSK2330672 90 mg BID80
Placebo90
Sitagliptin 50 mg BID80

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Number of Participants With Gastrointestinal Tolerability Assessments as Rated Using the Gastrointestinal Symptom Rating Scale (GSRS; With Worsening Symptoms >=2 Levels)

GSRS is a rating scale consisting of 15 items. Each item was scored from 1: no discomfort at all, 2: minor discomfort, 3: mild discomfort, 4: moderate discomfort, 5: moderately severe discomfort, 6: severe discomfort, 7: very severe discomfort. The overall GSRS score is the mean of these 15 items, varying from 1 to 7; a score of 1 indicates that no symptoms are present, and a score of 7 indicates the worst possible degree of all symptoms. A higher score relative to Baseline indicates worsening of severity. There were 5 defined syndrome scores and 1 overall score that was derived by computing the mean of the scores for specific subsets of questions as indicated below: abdominal pain (1, 4, 5); reflux syndrome (2, 3); diarrhea syndrome (11, 12, 14); indigestion syndrome (6, 7, 8, 9); constipation syndrome (10, 13, 15) and overall GSRS (1-15). The data is presented for participants with worsening of symptoms in >=2 levels. (NCT02202161)
Timeframe: Day 7 and 14

,,,,,,
InterventionParticipants (Count of Participants)
Pain/discomfort in upper abdomen, Day 7Heartburn, Day 7Acid reflux, Day 7Hunger pains, Day 7Nausea, Day 7Rumbling, Day 7Bloated, Day 7Burping, Day 7Passing gas or flatus, Day 7Constipation, Day 7Diarrhea, Day 7Loose stools, Day 7Hard stools, Day 7Urgent need to have bowel movement, Day 7Sensatn not complete empty bowels, Day 7Abdominal pain, Day 7Reflux syndrome, Day 7Indigestion syndrome, Day 7Constipation syndrome, Day 7Diarrhea syndrome, Day 7Overall GSRS, Day 7Pain/discomfort in upper abdomen, Day 14Heartburn, Day 14Acid reflux, Day 14Hunger pains, Day 14Nausea, Day 14Rumbling, Day 14Bloated, Day 14Burping, Day 14Passing gas or flatus, Day 14Constipation, Day 14Diarrhea, Day 14Loose stools, Day 14Hard stools, Day 14Urgent need to have bowel movement, Day 14Sensation not complete empty bowels, Day 14Abdominal pain, Day 14Reflux syndrome, Day 14Indigestion syndrome, Day 14Constipation syndrome, Day 14Diarrhea syndrome, Day 14Overall GSRS, Day 14
GSK2330672 10 mg BID000000001000000000000101001111101010001000
GSK2330672 20 mg BID211102111323022111021221212212143243111231
GSK2330672 30 mg BID200000101434012000030100201102032022001021
GSK2330672 60 mg BID000101000343023000020100000000023033000010
GSK2330672 90 mg BID011102322043122012021101202322253132012232
Placebo000011211101010001000111001210011010010000
Sitagliptin 50 mg BID0000100000000000000001000000000000000000000

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Number of Participants With Abnormal Urinalysis Data

Urinalysis included urine occult blood: trace to 3+, glucose: negative to 3+, protein: negative to 2+ and ketones: trace to negative by dipstick and microscopic examination included cast, cellular cast, granular cast, hyaline cast (none seen to 1) and RBC: 0-2, 3-10, 11-30, >30, WBC: none seen, 0-5, 1, 2, 4, <5, 6-10, 11-30, 19, >30). The plus sign increases with a higher level of occult blood, glucose, ketones, proteins, RBC, WBC in the urine: 1+: slightly positive, 2+: positive, 3+: high positive. Participants were categorized as none seen or 1 based on the absence or presence, respectively, of cast, cellular cast, granular cast and hyaline cast. Higher value indicates higher abnormality. (NCT02202161)
Timeframe: Baseline (pre-dose Day -1), Day 7 and 15

,,,,,,
InterventionParticipants (Count of Participants)
Urine Occult Blood, Day -1, TraceUrine Occult Blood, Day -1, smallUrine Occult Blood, Day-1, 3+Urine Occult Blood, Day 7, TraceUrine Occult Blood, Day 7, Trace intactUrine Occult Blood, Day 7, smallUrine Occult Blood, Day 7, 1+Urine Occult Blood, Day 15, TraceUrine Occult Blood, Day 15, smallUrine Occult Blood, Day 15, 2+Urine Microscopy-Casts, Day 7, none seenUrine Microscopy-Cellular Casts, Day -1, none seenUrine Microscopy-Cellular Casts, Day 7, none seenUrine Microscopy-Cellular Casts, Day 15, none seenUrine Microscopy-Granular Casts, Day -1, none seenUrine Microscopy-Granular Casts, Day 7, none seenUrine Microscopy-Granular Casts, Day 15, none seenUrine Glucose, Day -1, TraceUrine Glucose, Day -1, 1+Urine Glucose, Day -1, 2+Urine Glucose, Day -1, 3+Urine Glucose, Day 7, TraceUrine Glucose, Day 7, 1+Urine Microscopy-Hyaline Casts, Day -1, none seenUrine Microscopy-Hyaline Casts, Day 7, None seenUrine Microscopy-Hyaline Casts, Day 7, 1Urine Microscopy-Hyaline Casts, Day 15, none seenUrine Ketones, Day 7, TraceUrine Protein, Day -1, 1+Urine Protein, Day 7, 2+Urine Protein, Day 15, TraceUrine Protein, Day 15, 1+Urine Microscopy-RBC, Day -1, none seenUrine Microscopy-RBC, Day -1, 0-2Urine Microscopy-RBC, Day -1, 3-10Urine Microscopy-RBC, Day -1, 11-30Urine Microscopy-RBC, Day 7, none seenUrine Microscopy-RBC, Day 7, 0-2Urine Microscopy-RBC, Day 15, none seenUrine Microscopy-RBC, Day 7, 3-10Urine Microscopy-WBC, Day -1, none seenUrine Microscopy-WBC, Day -1, 0-5Urine Microscopy-WBC, Day -1, 1Urine Microscopy-WBC, Day -1, 4Urine Microscopy-WBC, Day -1, 6-10Urine Microscopy-WBC, Day -1, 11-30Urine Microscopy-WBC, Day -1, >30Urine Microscopy-WBC, Day 7, 0-5Urine Microscopy-WBC, Day 7, 1Urine Microscopy-WBC, Day 7, <5Urine Microscopy-WBC, Day 7, 11-30Urine Microscopy-WBC, Day 7, 19Urine Microscopy-WBC, Day 7, >30Urine Microscopy-WBC, Day 15, 0-5Urine Microscopy-WBC, Day 15, 1Urine Microscopy-WBC, Day 15, 2Urine Microscopy-WBC, Day 15, 4Urine Microscopy-WBC, Day 15, 11-30Urine Microscopy-WBC, Day 15, >30
GSK2330672 10 mg BID10110000000000000000000000000000001110002000000100000000000
GSK2330672 20 mg BID00010000000000000100001000010000001001000000100100000100000
GSK2330672 30 mg BID00000000000000000130020000001101100000101000000000000100000
GSK2330672 60 mg BID01000100100122122101110111200000000000000010000020000001100
GSK2330672 90 mg BID00000000000000000200010000000010000001000000000000100000000
Placebo00000000010000000100001000000010210010002100000100000100000
Sitagliptin 50 mg BID10011011001111111000211110100000111020111001011001111010011

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Number of Participants With Abnormal Electrocardiogram (ECG) Findings Any Time Post-Baseline

Single 12-lead ECGs was obtained at each time point during the study using an ECG machine that automatically calculates the heart rate and measures PR, QRS, QT, and QTc intervals. It was assessed on Baseline (pre-dose Day -1), Day 7 and 15. Participants with normal, abnormal not clinically significant and abnormal clinically significant ECG is presented. (NCT02202161)
Timeframe: Up to Day 15

,,,,,,
InterventionParticipants (Count of Participants)
NormalAbnormal not clinically significantAbnormal clinically significant
GSK2330672 10 mg BID401
GSK2330672 20 mg BID410
GSK2330672 30 mg BID810
GSK2330672 60 mg BID630
GSK2330672 90 mg BID640
Placebo940
Sitagliptin 50 mg BID940

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Number of Participants With Abnormal Clinical Chemistry With PCI

Clinical chemistry parameters included blood urea nitrogen (BUN), potassium, aspartate aminotransferase (AST), total bilirubin, direct bilirubin, creatinine, chloride, alanine aminotransferase (ALT), uric acid, fasting glucose, total carbon dioxide, gamma glutamyltransferase (GGT), albumin, sodium, calcium, alkaline phosphatase (ALP), total protein, total carbon dioxide and triglycerides. It was assessed on Baseline (pre-dose Day -1), Day 7 and 15. Data for parameters with above and below the PCI is provided. The normal range (NR) and PCI definition for abnormal parameters are: ALT (NR: 0-44, 0-32, 2-33; PCI: >=2×upper limit of normal [ULN]); AST (NR: 0-40; PCI: >=2× ULN) and total bilirubin (NR: 0.00-20.52; PCI: >=1.5× ULN). (NCT02202161)
Timeframe: Up to Day 15

,,,,,,
InterventionParticipants (Count of Participants)
ALT, highAST, highTotal Bilirubin, hgh
GSK2330672 10 mg BID000
GSK2330672 20 mg BID200
GSK2330672 30 mg BID200
GSK2330672 60 mg BID211
GSK2330672 90 mg BID100
Placebo100
Sitagliptin 50 mg BID100

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Number of Events With the Rating on Quality of Stools as Rated Using the BSFS Across Days 1 to 14

The site staff classified participant's stools and record the date and time of occurrence after any bowel movement that occurs while participants were in residence in the clinic. BSFS is scale between type 1-7, it measured the shape of the stool, type 1: separate hard lumps, like nuts; type 2: sausage shaped but lumpy; type 3: like a sausage or snake but with cracks on its surface; type 4: like a sausage or snake, smooth and soft; type 5: soft blobs with clear cut edges; type 6: fluffy pieces with ragged edges, a mushy stool and type 7: watery, no solid pieces. Participants were discharged after they have had at least one bowel movement after the Day 14 dosing and after the investigator/designee had reviewed the Day 15 end of study questions. (NCT02202161)
Timeframe: Up to Day 15 (administered after every in-house bowel movement)

InterventionEvents (Number)
BSFS scale rating, 2 events : EventsBSFS scale rating, 3 events : EventsBSFS scale rating, 4 events : EventsBSFS scale rating, 5 events : EventsBSFS scale rating, 6 events : EventsBSFS scale rating, 7 events : Events
GSK2330672 20 mg BID2418811347

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Number of Events With the Rating on Quality of Stools as Rated Using the BSFS Across Days 1 to 14

The site staff classified participant's stools and record the date and time of occurrence after any bowel movement that occurs while participants were in residence in the clinic. BSFS is scale between type 1-7, it measured the shape of the stool, type 1: separate hard lumps, like nuts; type 2: sausage shaped but lumpy; type 3: like a sausage or snake but with cracks on its surface; type 4: like a sausage or snake, smooth and soft; type 5: soft blobs with clear cut edges; type 6: fluffy pieces with ragged edges, a mushy stool and type 7: watery, no solid pieces. Participants were discharged after they have had at least one bowel movement after the Day 14 dosing and after the investigator/designee had reviewed the Day 15 end of study questions. (NCT02202161)
Timeframe: Up to Day 15 (administered after every in-house bowel movement)

InterventionEvents (Number)
BSFS scale rating, 1 event : EventsBSFS scale rating, 3 events : EventsBSFS scale rating, 4 events : EventsBSFS scale rating, 5 events : EventsBSFS scale rating, 6 events : EventsBSFS scale rating, 7 events : Events
GSK2330672 90 mg BID15243020198

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Number of Events With the Rating on Quality of Stools as Rated Using the BSFS Across Days 1 to 14

The site staff classified participant's stools and record the date and time of occurrence after any bowel movement that occurs while participants were in residence in the clinic. BSFS is scale between type 1-7, it measured the shape of the stool, type 1: separate hard lumps, like nuts; type 2: sausage shaped but lumpy; type 3: like a sausage or snake but with cracks on its surface; type 4: like a sausage or snake, smooth and soft; type 5: soft blobs with clear cut edges; type 6: fluffy pieces with ragged edges, a mushy stool and type 7: watery, no solid pieces. Participants were discharged after they have had at least one bowel movement after the Day 14 dosing and after the investigator/designee had reviewed the Day 15 end of study questions. (NCT02202161)
Timeframe: Up to Day 15 (administered after every in-house bowel movement)

InterventionEvents (Number)
BSFS scale rating, 3 events : EventsBSFS scale rating, 4 events : EventsBSFS scale rating, 5 events : EventsBSFS scale rating, 6 events : EventsBSFS scale rating, 7 events : Events
GSK2330672 60 mg BID621925050

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Number of Events With the Rating on Quality of Stools as Rated Using the BSFS Across Days 1 to 14

The site staff classified participant's stools and record the date and time of occurrence after any bowel movement that occurs while participants were in residence in the clinic. BSFS is scale between type 1-7, it measured the shape of the stool, type 1: separate hard lumps, like nuts; type 2: sausage shaped but lumpy; type 3: like a sausage or snake but with cracks on its surface; type 4: like a sausage or snake, smooth and soft; type 5: soft blobs with clear cut edges; type 6: fluffy pieces with ragged edges, a mushy stool and type 7: watery, no solid pieces. Participants were discharged after they have had at least one bowel movement after the Day 14 dosing and after the investigator/designee had reviewed the Day 15 end of study questions. (NCT02202161)
Timeframe: Up to Day 15 (administered after every in-house bowel movement)

InterventionEvents (Number)
BSFS scale rating, 4 events : EventsBSFS scale rating, 5 events : EventsBSFS scale rating, 6 events : EventsBSFS scale rating, 7 events : Events
GSK2330672 10 mg BID728151

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Change From Baseline in Vital Signs Assessments-temperature

The change from Baseline was calculated by subtracting the Baseline values from the individual post-Baseline values. Baseline was defined as pre-dose Day -1 value. (NCT02202161)
Timeframe: Baseline (pre-dose Day -1) and, Day 7, 15

,,,,,,
InterventionDegree Celsius (Mean)
Day 7Day 15
GSK2330672 10 mg BID-0.2800.025
GSK2330672 20 mg BID0.040-0.040
GSK2330672 30 mg BID0.033-0.111
GSK2330672 60 mg BID0.0330.056
GSK2330672 90 mg BID0.010-0.178
Placebo-0.133-0.208
Sitagliptin 50 mg BID0.0150.062

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Change From Baseline in Vital Signs Assessments-systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)

The change from Baseline was calculated by subtracting the Baseline values from the individual post-Baseline values. Baseline was defined as pre-dose Day -1 value. (NCT02202161)
Timeframe: Baseline (pre-dose Day -1) and Day 7, 15

,,,,,,
InterventionMillimeters of mercury (Mean)
DBP, Day 7DBP, Day 15SBP, Day 7SBP, Day 15
GSK2330672 10 mg BID-1.600-2.750-4.000-4.500
GSK2330672 20 mg BID-6.6001.800-15.6000.600
GSK2330672 30 mg BID-1.556-1.3332.222-5.111
GSK2330672 60 mg BID-4.111-1.6671.222-1.000
GSK2330672 90 mg BID-2.700-2.667-4.300-2.111
Placebo-0.0830.7502.2502.167
Sitagliptin 50 mg BID-2.462-0.769-5.462-4.385

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Change From Baseline in Vital Signs Assessments-heart Rate

The change from Baseline was calculated by subtracting the Baseline values from the individual post-Baseline values. Baseline was defined as pre-dose Day -1 value. (NCT02202161)
Timeframe: Baseline (pre-dose Day -1) and Day 7, 15

,,,,,,
InterventionBeats per minute (Mean)
Day 7Day 15
GSK2330672 10 mg BID9.2000.250
GSK2330672 20 mg BID4.4009.200
GSK2330672 30 mg BID0.556-0.444
GSK2330672 60 mg BID4.6674.889
GSK2330672 90 mg BID1.4000.000
Placebo-0.5000.083
Sitagliptin 50 mg BID-0.7691.846

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Change From Baseline in Derived Plasma Glucose Parameter Over a 24-hour Period-fasting and Weighted Mean Glucose Area Under Curve (AUC[0-24 Hour])

The change from Baseline was calculated by subtracting the Baseline values from the individual post-Baseline values. Baseline was defined as pre-dose Day -1 value. It was assessed on Baseline, Day 7 and 14. Data for fasting and weighted mean (WM) AUC(0-24 hour) glucose is provided. Statistics for least square mean is provided and participants withdrawing early were excluded. Results were based on an analysis of covariance (ANCOVA) model: change from Baseline = Baseline + treatment. (NCT02202161)
Timeframe: Baseline (Day -1) and Day 14 (Fasting Pre-dose [within 15 minutes of dose], 30 minutes, 1, 1.5, 2, 4 [pre-lunch], 5.5, 10 [pre-dinner], 11.5, 14 [bed time] and 24 hours) and Day 7 (30 minutes, 2, 4 [pre-lunch], 5.5, 10 [pre-dinner], 11.5, and 24 hours)

,,,,,,
InterventionMg/deciliter (Mean)
Fasting, Day 7Fasting, Day 14WM AUC(0-24 hour), Day 7WM AUC(0-24 hour), Day 14
GSK2330672 10 mg BID-8.25-22.75-12.14-22.44
GSK2330672 20 mg BID-1.40-16.20-7.01-17.80
GSK2330672 30 mg BID-38.56-48.67-25.33-37.48
GSK2330672 60 mg BID-34.38-36.13-21.47-32.22
GSK2330672 90 mg BID-24.78-40.22-14.84-45.54
Placebo-6.58-10.003.91-9.94
Sitagliptin 50 mg BID-24.54-38.38-26.63-35.85

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Sitagliptin Steady State PK Parameters When Co-dosed With Metformin-AUC(0-10)

The AUC(0-10) following the first dose and prior to the second dose of sitagliptin was determined using the linear trapezoidal rule for increasing concentrations and the logarithmic trapezoidal rule for decreasing concentrations. (NCT02202161)
Timeframe: Fasting pre-dose (within 15 minutes of dose), 1, 2, 3, 4 (pre-lunch), 10 (pre-dinner) on Day 14

InterventionHour×ng/mL (Geometric Mean)
Sitagliptin 50 mg BID1473.5

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PK Parameters for Metformin Steady State PK Parameters When Co-dosed With GSK2330672, Sitagliptin or Placebo-time of Occurrence of Cmax (Tmax)

The time at which Cmax observed was determined directly from the raw concentration-time data. (NCT02202161)
Timeframe: Fasting pre-dose (within 15 minutes of dose), 30 minutes, 1, 1.5, 2, 3, 4 (pre-lunch), 5.5, 8, 10 hours (pre-dinner) on Day 14

InterventionHour (Median)
Placebo1.510
GSK2330672 10 mg BID1.000
GSK2330672 20 mg BID1.000
GSK2330672 30 mg BID1.050
GSK2330672 60 mg BID1.750
GSK2330672 90 mg BID1.500
Sitagliptin 50 mg BID2.050

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PK Parameters for Metformin Steady State PK Parameters When Co-dosed With GSK2330672, Sitagliptin or Placebo-area Under the Concentration-time Curve Over the Dosing Interval of 10 Hours (AUC[0-10])

PK population. Only those participants available at the specified time points were analyzed. (NCT02202161)
Timeframe: Fasting pre-dose (within 15 minutes of dose), 30 minutes, 1, 1.5, 2, 3, 4 (pre-lunch), 5.5, 8, 10 hours (pre-dinner) on Day 14

InterventionHour×ng/mL (Geometric Mean)
Placebo6805.8
GSK2330672 10 mg BID5982.0
GSK2330672 20 mg BID7066.2
GSK2330672 30 mg BID7066.5
GSK2330672 60 mg BID8090.5
GSK2330672 90 mg BID8375.3
Sitagliptin 50 mg BID8425.4

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Change From Baseline in 2-hour Post-Meal Glucose (PMG) at Week 26 - Full Analysis Set Excluding Rescue Approach

Change from baseline at Week 26 is defined as 2-hour PMG at Week 26 minus 2-hour PMG at Week 0. Two-hour post-meal glucose was measured following a standard meal. Excluding rescue approach excludes all data following the initiation of rescue, in order to avoid the confounding influence of the rescue therapy with open-label glimepiride. (NCT02226003)
Timeframe: Baseline and Week 26

Interventionmilligrams/deciliter (Least Squares Mean)
Ertugliflozin 5 mg + Sitagliptin 100 mg-82.80
Ertugliflozin 15 mg + Sitagliptin 100 mg-90.03
Placebo-20.38

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Change From Baseline in Body Weight at Week 26 - Full Analysis Set Excluding Rescue Approach

Body weight was measured using a standardized, digital scale at each of the pre-defined nominal time points. Weight was taken in duplicate throughout the trial at approximately the same time of day, after voiding (i.e., forced void) and while wearing only a gown and underwear. Excluding rescue approach excludes all data following the initiation of rescue, in order to avoid the confounding influence of the rescue therapy with open-label glimepiride. (NCT02226003)
Timeframe: Baseline and Week 26

InterventionKilograms (Least Squares Mean)
Ertugliflozin 5 mg + Sitagliptin 100 mg-2.94
Ertugliflozin 15 mg + Sitagliptin 100 mg-3.04
Placebo-0.94

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 26 - Full Analysis Set Excluding Rescue Approach

Blood glucose was measured after a ≥10 hour fast. Blood was drawn at predose on Day 1 and after 26 weeks of treatment to determine change in plasma glucose levels (i.e., FPG at Week 26 minus FPG at baseline). Excluding rescue approach excludes all data following the initiation of rescue, in order to avoid the confounding influence of the rescue therapy with open-label glimepiride. (NCT02226003)
Timeframe: Baseline and Week 26

Interventionmilligrams/deciliter (Least Squares Mean)
Ertugliflozin 5 mg + Sitagliptin 100 mg-48.25
Ertugliflozin 15 mg + Sitagliptin 100 mg-55.36
Placebo-9.30

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Change From Baseline in Hemoglobin A1C (HbA1C) at Week 26 - Full Analysis Set (FAS Population Excluding Rescue Approach

HbA1C is blood marker used to report average blood glucose levels over prolonged periods of time and is reported as a percentage (%). HbA1C represents the percentage of glycated hemoglobin. A negative number indicates a reduction in HbA1C level. Excluding rescue approach excludes all data following the initiation of rescue, in order to avoid the confounding influence of the rescue therapy with open-label glimepiride. (NCT02226003)
Timeframe: Baseline and Week 26

InterventionPercentage (Least Squares Mean)
Ertugliflozin 5 mg + Sitagliptin 100 mg-1.60
Ertugliflozin 15 mg + Sitagliptin 100 mg-1.68
Placebo-0.44

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Percentage of Participants Who Discontinued Study Medication Due to an AE - All Participants as Treated Excluding Rescue Approach

An AE is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure, that occurs during the course of the study. Excluding rescue approach excludes all data following the initiation of rescue, in order to avoid the confounding influence of the rescue therapy with open-label glimepiride. (NCT02226003)
Timeframe: Up to Week 26

InterventionPercentage of Participants (Number)
Ertugliflozin 5 mg + Sitagliptin 100 mg2.0
Ertugliflozin 15 mg + Sitagliptin 100 mg2.1
Placebo2.1

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Change From Baseline in Sitting Systolic Blood Pressure at Week 26 - Full Analysis Set Excluding Rescue Approach

Blood pressure measurements were taken after at least 5 minutes of rest. Three measurements were taken approximately 2 minutes apart with the triplicate set recorded. Excluding rescue approach excludes all data following the initiation of rescue, in order to avoid the confounding influence of the rescue therapy with open-label glimepiride. (NCT02226003)
Timeframe: Baseline and Week 26

Interventionmillimeters of mercury (Least Squares Mean)
Ertugliflozin 5 mg + Sitagliptin 100 mg-2.04
Ertugliflozin 15 mg + Sitagliptin 100 mg-3.98
Placebo2.41

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Change From Baseline in Sitting Diastolic Blood Pressure at Week 26 - Full Analysis Set Excluding Rescue Approach

Blood pressure measurements were taken after at least 5 minutes of rest. Three measurements were taken approximately 2 minutes apart with the triplicate set recorded. Excluding rescue approach excludes all data following the initiation of rescue, in order to avoid the confounding influence of the rescue therapy with open-label glimepiride. (NCT02226003)
Timeframe: Baseline and Week 26

Interventionmillimeters of mercury (Least Squares Mean)
Ertugliflozin 5 mg + Sitagliptin 100 mg-0.44
Ertugliflozin 15 mg + Sitagliptin 100 mg-0.97
Placebo1.21

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Percentage of Participants With HbA1C <7% (<53 mmol/Mol) at Week 26

HbA1C is blood marker used to report average blood glucose levels over prolonged periods of time and is reported as a percentage (%). HbA1c represents the percentage of glycated hemoglobin. (NCT02226003)
Timeframe: Week 26

InterventionPercentage of participants (Number)
Ertugliflozin 5 mg + Sitagliptin 100 mg35.7
Ertugliflozin 15 mg + Sitagliptin 100 mg31.3
Placebo8.3

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Percentage of Participants Who Experienced an Adverse Event (AE) - All Participants as Treated Excluding Rescue Approach

An adverse event (AE) is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure, that occurs during the course of the study. Excluding rescue approach excludes all data following the initiation of rescue, in order to avoid the confounding influence of the rescue therapy with open-label glimepiride. (NCT02226003)
Timeframe: Up to Week 28

InterventionPercentage of Participants (Number)
Ertugliflozin 5 mg + Sitagliptin 100 mg44.9
Ertugliflozin 15 mg + Sitagliptin 100 mg44.8
Placebo42.3

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Number of Treatment Emergent Adverse Events (TEAEs)

An adverse events (AEs) was defined as any unfavourable and unintended sign (including an abnormal laboratory finding), symptom or disease temporally associated with the use of a product, whether or not considered related to the product. All AEs mentioned here are treatment emergent adverse events (TEAE) defined as an event that had onset date (or increase in severity) on or after the first day of exposure to randomised treatment (week 0-30 treatment period) and no later than the follow-up visit during the on-treatment observation period (date of last dose + 42 days). (NCT02254291)
Timeframe: Weeks 0-30

InterventionNumber of events (Number)
Semaglutide 0.5 mg228
Semaglutide 1.0 mg197
Sitagliptin186

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Number of Severe or Blood Glucose (BG) Confirmed Symptomatic Hypoglycaemic Episodes

Severe or blood glucose (BG) confirmed symptomatic hypoglycaemic episodes were defined as episodes that were severe and/or BG confirmed by a plasma glucose value of <56 mg/dL (3.1 mmol/L), with symptoms consistent with hypoglycaemia. Severe hypoglycaemia was an episode requiring assistance of another person to actively administer carbohydrate, glucagon, or take other corrective actions. The episodes mentioned here are treatment emergent hypoglycaemic episodes and defined as an event that had onset date (or increase in severity) on or after the first day of exposure to randomised treatment (week 0-30 treatment period) and no later than the follow-up visit during the on-treatment observation period (date of last dose + 42 days). (NCT02254291)
Timeframe: Weeks 0-30

InterventionNumber of episodes (Number)
Semaglutide 0.5 mg0
Semaglutide 1.0 mg1
Sitagliptin0

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Change in Glycosylated Haemoglobin A1c (HbA1c)

"Mean changes in HbA1c values from baseline after 30 weeks of treatment. Changes in HbA1c were analysed using a mixed model for repeated measurements (MMRM) with treatment and pre-trial treatment at screening as fixed factors and baseline value as covariate. The data were analysed for the on-treatment without rescue medication observation period which includes observations noted at or after the date of first dose of randomised treatment and not after the last dose of the trial product (+ a 7-day visit window) or initiation of rescue medication." (NCT02254291)
Timeframe: Week 0 and week 30

InterventionPercentage of glycosylated haemoglobin (Least Squares Mean)
Semaglutide 0.5 mg-1.87
Semaglutide 1.0 mg-2.18
Sitagliptin-0.74

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Glucagon Counterregulation to Hypoglycemia

Change in plasma glucagon to insulin-induced hypoglycemia after four weeks of treatment with sitagliptin and placebo (NCT02256189)
Timeframe: Four weeks treatment

Interventionpmol/l (Mean)
Sitagliptin16.0
Placebo16.5

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Percent of Subjects Achieving a Therapeutic Glycemic Response, Defined as HbA1c < 7.0%

(NCT02284893)
Timeframe: week 26

InterventionPercentage of subjects (Number)
Saxagliptin + Dapagliflozin + Metformin Group37.3
SITA + MET25.1

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Mean Change in Total Body Weight

(NCT02284893)
Timeframe: Baseline (randomization) to Week 26

Interventionkg (Mean)
Saxagliptin + Dapagliflozin + Metformin Group-1.86
SITA + MET-0.51

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Mean Change in HbA1c

(NCT02284893)
Timeframe: Baseline (randomization) to Week 26

Interventionpercentage (%) (Least Squares Mean)
Saxagliptin + Dapagliflozin + Metformin Group-1.41
SITA + MET-1.07

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Mean Change in Fasting Plasma Glucose (FPG)

(NCT02284893)
Timeframe: Baseline (randomization) to Week 26

Interventionmg/dl (Mean)
Saxagliptin + Dapagliflozin + Metformin Group-31.9
SITA + MET-11.0

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Correlation of Plasma Levels of EPA and DHA With HbA1c Reduction

Pearson's correlation coefficient of HbA1c reduction with plasma levels of EPA and DHA at baseline (NCT02312063)
Timeframe: 0-16 weeks

,
Interventionpearson's correlation coefficient (Number)
r (EPA and delta HbA1c)r (DHA and delta HbA1c)
Glimepiride0.0670.093
Sitagliptin-0.414-0.319

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Correlation of Estimated Seafood Intake With HbA1c Reduction

Pearson's correlation coefficient of HbA1c reduction with estimated seafood intake (NCT02312063)
Timeframe: 0-16 weeks

Interventionpearson's correlation coefficient (Number)
Sitagliptin-0.042
Glimepiride0.215

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Change From Baseline in Percentage of Hypoglycemic Values (Glucose Sensor Readings: < 70, <60, <50 mg/dL)

Hypoglycemia, defined as low blood glucose, is a common side effect of medications used to treat diabetes mellitus type 2. The percentage of hypoglycemic corrected CGM readings (sensor glucose <70, <60, <50 mg/dL) over a 24-hour period were determined at baseline and Day 13. CGM values were corrected using a participant-administered finger-stick test for blood glucose. LS mean values were derived from a constrained longitudinal analysis model. A negative (-) change from baseline to Day 13 indicates improvement in occurrence of hypoglycemia. (NCT02318693)
Timeframe: Baseline (Day -2) and Day 13

,
InterventionPercent change (Least Squares Mean)
<70 mg/dL<60 mg/dL<50 mg/dL
Glibenclamide 2.50 mg TDD0.80.2-0.3
Sitagliptin 50 mg-0.3-0.4-0.3

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Change From Baseline in Maximum Incremental Postprandial Glucose Levels in Each Meal

The peak postprandial glucose level during the 3 hours post meal minus the preprandial glucose level 1 hour before meal was determined for corrected CGM values at Baseline and Day 13 for breakfast, lunch, and dinner. Meals were standardized with respect to total calories, and protein, fat, and carbohydrate composition as well as timing of administration. CGM values were corrected using a participant-administered finger-stick test for blood glucose. LS mean values were derived from a constrained longitudinal analysis model. A negative (-) change from baseline to Day 13 indicates better control of postprandial glucose. (NCT02318693)
Timeframe: Baseline (Day -2) and Day 13

,
Interventionmg/dL (Least Squares Mean)
BreakfastLunchDinner
Glibenclamide 2.50 mg TDD-12.01.2-14.1
Sitagliptin 50 mg-24.8-13.2-9.0

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Change From Baseline in the Standard Deviation of Blood Glucose Levels

SD is a popular metric for assessment of postprandial glucose swings. The SD of all glycemic excursions over 24 hours (i.e., total of 288 glucose values over 24 hours) was determined for Baseline and Day 13. Original values were obtained using CGM and corrected for blood glucose values obtained via participant-administered finger-stick. LS mean values were derived from a constrained longitudinal analysis model. A negative (-) change from Baseline to Day 13 indicates improvement of the assessed outcome. (NCT02318693)
Timeframe: Baseline (Day -2) and Day 13

Interventionmg/dL (Least Squares Mean)
Sitagliptin 50 mg-10.2
Glibenclamide 2.50 mg TDD-4.2

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Change From Baseline in Mean Amplitude of Glycemic Excursions (MAGE) at Day 13

MAGE is a popular metric for assessment of major (e.g., postprandial) glucose swings. MAGE is calculated as the average of differences between consecutive glucose peaks and nadirs greater than 1 standard deviation (SD) of 24-hour mean glucose. In this assessment, glucose levels were determined using continuous glucose monitoring (CGM) over 24 hours at Baseline and Day 13; CGM values were further corrected for blood glucose values obtained via participant-administered finger-stick. Least squares (LS) means values were derived from a constrained longitudinal analysis model. A negative (-) change from Baseline to Day 13 indicates improvement of the assessed outcome. (NCT02318693)
Timeframe: Baseline (Day -2) and Day 13

Interventionmg/dL (Least Squares Mean)
Sitagliptin 50 mg-18.5
Glibenclamide 2.50 mg TDD-9.7

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Change From Baseline in 24-hour Mean Glucose Level

The mean glucose level over 24-hours at Baseline and Day 13 was determined using CGM values corrected for participant-administered finger-stick values. LS mean values were derived from a constrained longitudinal analysis model. A negative (-) change from Baseline to Day 13 indicates improvement of the assessed outcome. (NCT02318693)
Timeframe: Baseline (Day -2) and Day 13

Interventionmg/dL (Least Squares Mean)
Sitagliptin 50 mg-19.1
Glibenclamide 2.50 mg TDD-34.8

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Blood Glucose Measures in Subjects Treated With Sitagliptin, Compared to the Placebo

Better targeted blood glucose levels in the CL setting in the treatment arm, Sitagliptin, compared to placebo (insulin monotherapy) (NCT02328040)
Timeframe: 18 Months

Interventionmg/dl (Mean)
Placebo/Insulin149.7
Sitagliptin/Insulin155.9

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Measure of Glucagon Concentration in Subjects Treated With Sitagliptin, Compared to Placebo

Serum glucagon concentrations were measured in the CL setting in the treatment arm, sitagliptin, compared to the placebo (Insulin monotherapy) (NCT02328040)
Timeframe: 18 months

InterventionPmol/L (Mean)
Placebo/Insulin6.04
Sitagliptin/Insulin5.66

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Change in Glomerular Filtration Rate (GFR)

Measured GFR (Inulin Clearance) at 3Hrs post study-drug after 1 month compared to Measured GFR at 3Hrs post-study drug after 1 dose, sitagliptin vs. placebo (NCT02406443)
Timeframe: 3 Hrs post-administration after 1 month and after 1 dose

Interventionml per min per 1.73 m2 (Mean)
Experimental Arm3.9
Placebo Arm-1.8

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Change From Baseline in SDF-1alpha^1-67 (Intact) Measured by Immunoaffinity and Tandem Mass Spectrometry

Plasma concentration of SDF-1alpha^1-67 (intact) measured by quantitative mass spectrometry methods after antibody-based affinity enrichment, sitagliptin vs. placebo (NCT02406443)
Timeframe: 3 Hr vs. baseline after 1 dose

Interventionng per mL (Mean)
Experimental Arm0.5
Placebo Arm0

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Change From Baseline in SDF-1alpha^3-67 (Truncated) Measured by Tandem Mass Spectrometry With Antibody-based Affinity Enrichment

Plasma concentration of SDF-1alpha^3-67 (intact) measured by quantitative mass spectrometry methods after antibody-based affinity enrichment, sitagliptin vs. placebo (NCT02406443)
Timeframe: 3Hrs vs baseline after 1 dose

Interventionng per mL (Mean)
Experimental Arm-2.0
Placebo Arm0.4

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Change in Fractional Excretion of Lithium (FELi)

FELi at 3 Hr post-study drug administration after 1 month compared to FELI at 3hrs post-study drug administration after 1 dose, sitagliptin vs. placebo (NCT02406443)
Timeframe: 3 Hrs post-administration after 1 month and after 1 dose

Interventionpercentage of change (Mean)
Experimental Arm29
Placebo Arm7

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Change in Systolic Blood Pressure (SBP), Non-invasive Cardiac Output Monitoring

SBP by Non-Invasive cardiac output monitoring at 3Hrs post- study drug administration after 1 month compared to SBP by Non-invasive cardiac output monitoring at 3Hrs after 1 dose, sitagliptin vs placebo (NCT02406443)
Timeframe: 3 Hrs post-administration after 1 month and after 1 dose

InterventionmmHg (Mean)
Experimental Arm5.7
Placebo Arm0.0

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Percent Change in Fractional Excretion of Sodium (FENA)

FENA at 3Hrs post-study drug administration after 1 month compared to FENA at 3Hrs post-study drug administration after 1 dose expressed as percent change, sitagliptin vs. placebo (NCT02406443)
Timeframe: 3 Hrs post-administration after 1 month and after 1 dose

Interventionpercentage of change (Mean)
Experimental Arm41
Placebo Arm-5.0

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Change in Effective Renal Plasma Flow (ERPF)

ERPF (para-aminohippurate clearance) 3Hrs post-study drug administration after 1 month compared to ERPF at 3Hhrs post-study drug administration after 1 dose, sitagliptin vs placebo (NCT02406443)
Timeframe: 3 Hrs post-administration after 1 month and after 1 dose

Interventionml per min per 1.73 m2 (Mean)
Experimental Arm31.1
Placebo Arm-24.7

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Number of Participants With Blood Glucose Less Than 40 mg/dl

Number of participants with blood glucose (BG) <40 throughout the duration of hospitalization. (NCT02443402)
Timeframe: Duration of Hospitalization (Up to 30 Days)

InterventionParticipants (Count of Participants)
Sitagliptin0
Placebo0

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Number of Participants Re-admitted to the Hospital Not Due to Wound Infections

Number of subjects readmitted to the hospital within 30 days for all causes excluding wound infection. (NCT02443402)
Timeframe: Post-Hospital Discharge (Up to 30 Days)

InterventionParticipants (Count of Participants)
Sitagliptin3
Placebo0

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Number of Participants Re-admitted to the Hospital Due to Wound Infections

Number of subjects readmitted to the hospital within 30 days due to wound infection. (NCT02443402)
Timeframe: Post-Hospital Discharge (Up to 30 Days)

InterventionParticipants (Count of Participants)
Sitagliptin1
Placebo1

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Need for Continuous Intravenous Insulin (CII) for Treatment of Hyperglycemia

Number of subjects with hyperglycemia (BG >180 mg/dL) who require CII in the ICU. (NCT02443402)
Timeframe: Post-Surgery (Up to 4 Days)

InterventionParticipants (Count of Participants)
Sitagliptin7
Placebo7

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Mean Units Subcutaneous (SQ) Insulin Required

Mean number of supplemental insulin units (lispro or aspart) administered after receiving insulin glargine (SQ insulin). (NCT02443402)
Timeframe: Post-Surgery (Up to 10 Days)

Interventionunits (Mean)
Sitagliptin2.4
Placebo2.4

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Mean Blood Glucose (BG) Concentration After Transition From Intensive Care Unit (ICU)

The blood glucose levels will be assessed throughout the day using a glucose meter after transition form the ICU. The normal BG range for someone with diabetes is 80-130 mg/dL. (NCT02443402)
Timeframe: Post-Surgery (Up to 4 Days)

Interventionmg/dl (Mean)
Sitagliptin123
Placebo124

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Total Insulin Therapy in the Intensive Care Unit (ICU)

Total amount of insulin glargine insulin (units) administered in the ICU per day. (NCT02443402)
Timeframe: Post-Surgery (Up to 4 Days)

Interventionunits per day (Mean)
Sitagliptin0
Placebo0

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Number of Subjects With Persistent Hyperglycemia

Number of subjects with persistent hyperglycemia (2 consecutive fasting and/or premeal BG > 180 mg/dL, or with average daily BG >180 mg/dl) who require insulin glargine (rescue therapy) after discontinuation of continuous intravenous insulin (CII) (NCT02443402)
Timeframe: Post-Surgery (Up to 10 Days)

InterventionParticipants (Count of Participants)
Sitagliptin7
Placebo6

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Number of Subjects Requiring the Use of Inotropes for Greater Than 24 Hours

The number of subjects requiring the use of inotropes for >24 hours post CABG. (NCT02443402)
Timeframe: Post-Surgery (Up to 2 Days)

InterventionParticipants (Count of Participants)
Sitagliptin11
Placebo7

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Mean Daily Intensive Care Unit (ICU) Blood Glucose (BG) Concentration

The blood glucose levels will be assessed throughout the day using a glucose meter. An average will be calculated. The normal BG range for someone with diabetes is 80-130 mg/dL. (NCT02443402)
Timeframe: Post-Surgery (Up to 4 Days)

Interventionmg/dL (Mean)
Sitagliptin137
Placebo138

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Mean Amount of Insulin Therapy in the Intensive Care Unit (ICU)

The mean number of insulin infusions given per day (unit/day) while subjects are in the ICU. The more insulin given, the more hyperglycemic events experienced. (NCT02443402)
Timeframe: Post-Surgery (Up to 4 Days)

Interventionunits per day (Mean)
Sitagliptin37
Placebo83

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Length of Stay: Intensive Care Unit (ICU)

Number of days in the ICU after coronary artery bypass graft surgery (CABG). (NCT02443402)
Timeframe: Post-Surgery (Up to 4 Days)

Interventiondays (Mean)
Sitagliptin2
Placebo2

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Length of Hospital Stay After Study Randomization

Number of days in the hospital after a participant is randomized to a study intervention. (NCT02443402)
Timeframe: Post-Randomization (Up to 9 days)

Interventiondays (Mean)
Sitagliptin6.0
Placebo6.5

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Intensive Care Unit (ICU) Mortality Rate

The total number of subject deaths during ICU stay will be recorded. (NCT02443402)
Timeframe: Post-Surgery (Up to 4 Days)

InterventionParticipants (Count of Participants)
Sitagliptin0
Placebo0

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Number of Subjects Requiring Re-intubation Within 24 Hours

The number of subjects requiring re-intubation with 24 after CABG. (NCT02443402)
Timeframe: Post-Surgery (Up to 24 Hours)

InterventionParticipants (Count of Participants)
Sitagliptin2
Placebo1

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Number of Subject Requiring Surgical Re-Intervention

The number of subjects that require surgical re-intervention due to mediastinal exploration and post-operative hemorrhage. (NCT02443402)
Timeframe: Post-Surgery (Up to 10 Days)

InterventionParticipants (Count of Participants)
Sitagliptin1
Placebo2

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Number of Participants With Stress Hyperglycemic Events in the Intensive Care Unit (ICU)

Number of participants who developed stress hyperglycemia (BG >180 mg/dl) during coronary artery bypass grafting (CABG) or after CABG requiring continuous IV insulin infusion (CII) while in the ICU. (NCT02443402)
Timeframe: Post-Surgery (Up to 4 Days)

InterventionParticipants (Count of Participants)
Sitagliptin22
Placebo25

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Number of Participants With Severe Hyperglycemic Events During Continuous Insulin Infusion (CII)

Number of participants with two consecutive blood glucose concentrations >180 mg/dL in ICU during CII. (NCT02443402)
Timeframe: Post-Surgery (Up to 4 Days)

InterventionParticipants (Count of Participants)
Sitagliptin7
Placebo6

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Number of Participants With Infections Not Requiring Hospital Re-admission

Number of subjects with infections not requiring hospital re-admission within 30 days after hospital discharge. (NCT02443402)
Timeframe: Post-Hospital Discharge (Up to 30 Days)

InterventionParticipants (Count of Participants)
Sitagliptin0
Placebo1

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Number of Subjects Requiring Re-intubation

The number of subjects requiring re-intubation after CABG. (NCT02443402)
Timeframe: Post-Surgery (Up to 2 Days)

InterventionParticipants (Count of Participants)
Sitagliptin1
Placebo2

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Number of Participants With Hypoglycemia During Intensive Care Unit (ICU) Stay

Number of participants with blood glucose (BG) <70 during ICU stay. (NCT02443402)
Timeframe: Post-Surgery (Up to 4 Days)

InterventionParticipants (Count of Participants)
Sitagliptin2
Placebo1

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Number of Participants With Hypoglycemia After Transition From Intensive Care Unit (ICU)

Number of participants with blood glucose (BG) <70 after transition from ICU. (NCT02443402)
Timeframe: Post-Surgery (Up to 4 Days)

InterventionParticipants (Count of Participants)
Sitagliptin1
Placebo0

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Number of Participants With Hyperglycemia After Transition From Intensive Care Unit (ICU)

Number of participants with blood glucose (BG) >180 after transition from ICU. (NCT02443402)
Timeframe: Post-Surgery (Up to 10 Days)

InterventionParticipants (Count of Participants)
Sitagliptin8
Placebo8

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Duration of Continuous Intravenous Insulin (CII)

Mean number of hours on continuous intravenous insulin (CII) after ICU discharge. (NCT02443402)
Timeframe: Post-Intensive Care Unit (ICU) Discharge (Up to 4 Days)

Interventionhours (Mean)
Sitagliptin12
Placebo17

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Hospital Complication Rate

The total number of all complications experienced during hospitalization. Participants may experience more than one complication during hospitalization and these will be included in the hospital complication rate. (NCT02443402)
Timeframe: Duration of Hospitalization (Up to 30 days)

Interventionnumber of complications (Number)
Sitagliptin47
Placebo57

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Number of Participants With Emergency Room (ER) Visits

Number of subjects returning to the ER up to 30 days (all-cause) after hospital discharge. (NCT02443402)
Timeframe: Post-Hospital Discharge (Up to 30 Days)

InterventionParticipants (Count of Participants)
Sitagliptin2
Placebo1

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Hospital Mortality Rate

The total number of subject deaths during hospital stay will be recorded. (NCT02443402)
Timeframe: Post-Surgery (Up to 10 Days)

InterventionParticipants (Count of Participants)
Sitagliptin0
Placebo0

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Number of Participants With Cerebrovascular Events

Number of participants that experienced permanent stroke and reversible ischemic neurologic deficit events. (NCT02443402)
Timeframe: Post-Hospital Discharge (Up to 10 Days)

InterventionParticipants (Count of Participants)
Sitagliptin2
Placebo1

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Change in %CD14+/CD16- (Classical Monocytes)

"CD14+/CD16- is the percentage of cells that expressed CD14 and low CD16 in total monocytes (also known as classical monocytes).~This endpoint is measuring the change from week 0 to week 15 (week 15 - week 0) and change from week 15 to week 20 (week 20 - week 15).~Data for cellular markers are not available as of November 2017. The study team prioritized completion of the soluble markers (including the primary outcome measure), which are reported herein, over the completion of the cellular markers. Results will be entered once the data is complete and analyzed." (NCT02513771)
Timeframe: Week 0, week 15, week 20

,
Interventionpercentage of cells (Median)
change from baseline to week 15change from week 15 to week 20
Placebo Arm-0.80-1.00
Sitagliptin Arm-2.300.40

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Change in %CD14dim/CD16++ (Non-classical Monocytes)

"%CD14dim/CD16++ is the percentage of cells that expressed low levels of CD14dim and high levels of CD16++ in total monocytes (also known as non-classical monocytes).~This endpoint is measuring the change from week 0 to week 15 (week 15 - week 0) and change from week 15 to week 20 (week 20 - week 15).~Data for cellular markers are not available as of December 2017. These data are based on immunology assays which were tested in batch to minimize variability. Due to batch testing, shipment of samples for testing could not begin until after the study follow-up completion, which was 1 month after the primary complete date. Please note that these secondary outcomes were not included in the primary analyses. There are many outcomes in this study and the immunology lab had to give priority to the assays planned to be included in the primary manuscript. Results will be entered once the data is complete and analyzed." (NCT02513771)
Timeframe: Week 0, week 15, week 20

,
Interventionpercentage of cells (Median)
change from baseline to week 15change from week 15 to week 20
Placebo Arm-0.030.12
Sitagliptin Arm0.31-0.37

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Change in CD4+ T-cell Activation

"Level of CD4+ T-cell activation was determined by measuring the percentage of cells that expressed both the activation marker CD38+ and Human leukocyte antigen (HLA)-DR+.~The endpoint is measuring the change from week 0 to week 15 (week 15 - week 0) and change from week 15 to week 20 (week 20 - week 15).~Data for cellular markers are not available as of December 2017. These data are based on immunology assays which were tested in batch to minimize variability. Due to batch testing, shipment of samples for testing could not begin until after the study follow-up completion, which was 1 month after the primary complete date. Please note that these secondary outcomes were not included in the primary analyses. There are many outcomes in this study and the immunology lab had to give priority to the assays planned to be included in the primary manuscript. Results will be entered once the data is complete and analyzed." (NCT02513771)
Timeframe: Week 0, week 15, week 20

,
Interventionpercentage of cells (Median)
change from baseline to week 15change from week 15 to week 20
Placebo Arm0.080.06
Sitagliptin Arm0.120.07

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Change in sCD14 From Baseline to Week 15/16

"sCD14 (soluble cluster of differentiation 14) is a biomarker of gut microbial translocation and monocyte/macrophage activation.~The outcome measures are changes in log10 transformed sCD14 from baseline to week 15/16 (week 15/16 - baseline) Levels measured at pre-entry and entry were averaged for baseline, levels measured at week 15 and week 16 were averaged for week 15/16." (NCT02513771)
Timeframe: Pre-entry, Week 0, Week 15, Week 16

Interventionlog10 pg/mL (Median)
Sitagliptin Arm-0.03
Placebo Arm-0.03

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Change in CD4+/CD8+ T-cell Ratio

CD4+/CD8+ T-cell ratio change from week 0 to week 15 (week 15 - week 0). Note that CD4 and CD8 were not evaluated at week 20 in this study. (NCT02513771)
Timeframe: Week 0 and week 15

Interventionratio (Median)
Sitagliptin Arm0.00
Placebo Arm0.02

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Change in CD8+ T-cell Activation

"Level of CD8+ T-cell activation was determined by measuring the percentage of cells that expressed both the activation marker CD38+ and Human leukocyte antigen (HLA)-DR+.~The endpoint is measuring the change from week 0 to week 15 (week 15 - week 0) and change from week 15 to week 20 (week 20 - week 15).~Data for cellular markers are not available as of December 2017. These data are based on immunology assays which were tested in batch to minimize variability. Due to batch testing, shipment of samples for testing could not begin until after the study follow-up completion, which was 1 month after the primary complete date. Please note that these secondary outcomes were not included in the primary analyses. There are many outcomes in this study and the immunology lab had to give priority to the assays planned to be included in the primary manuscript. Results will be entered once the data is complete and analyzed." (NCT02513771)
Timeframe: Week 0, week 15, week 20

,
Interventionpercentage of cells (Median)
change from baseline to week 15change from week 15 to week 20
Placebo Arm-0.27-0.29
Sitagliptin Arm0.030.11

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Change in sCD14 From Week 15/16 to Week 20

"sCD14 (soluble cluster of differentiation 14) is a biomarker of gut microbial translocation and monocyte/macrophage activation.~The outcome measures are changes in log10 transformed sCD14 from week 15/16 to week 20 (week 20 - week 15/16).~Levels measured at week 15 and week 16 were averaged for week 15/16." (NCT02513771)
Timeframe: Week 15, week 16, week 20

Interventionlog10 pg/mL (Median)
Sitagliptin Arm0.04
Placebo Arm0.02

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Change in hsCRP

hsCRP (high-sensitivity C-reactive protein) is a biomarker of inflammation. Change in log10 transformed hsCRP from Week 0 to week 15 (week 15 - week 0), and from week 15 to week 20 (week 20 - week 15). (NCT02513771)
Timeframe: Week 0, week 15, week 20

,
Interventionlog10 ng/mL (Median)
Change from week 0 to week 15Change from week 15 to week 20
Placebo Arm-0.05-0.01
Sitagliptin Arm-0.08-0.02

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Change in IL-6

IL-6 (Interleukin-6) is a biomarker of systemic inflammation. Change in log10 transformed IL-6 from Week 0 to week 15 (week 15 - week 0), and from week 15 to week 20 (week 20 - week 15). (NCT02513771)
Timeframe: Week 0, week 15, week 20

,
Interventionlog10 pg/mL (Median)
Change from week 0 to week 15Change from week 15 to week 20
Placebo Arm0.000.01
Sitagliptin Arm0.00-0.06

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Change in IP-10

"IP-10 (also known as CXCL10) is a biomarker implicated in cardiovascular disease.~Change in log10 transformed IP-10 from Week 0 to week 15 (week 15 - week 0), and from week 15 to week 20 (week 20 - week 15)." (NCT02513771)
Timeframe: Week 0, week 15, week 20

,
Interventionlog10 pg/mL (Median)
Change from week 0 to week 15Change from week 15 to week 20
Placebo Arm-0.010.02
Sitagliptin Arm-0.310.23

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Change in sCD163

"sCD163 (soluble CD 163) is a marker of macrophage activation and arterial inflammation.~Change in log10 transformed sCD163 from Week 0 to week 15 (week 15 - week 0), and from week 15 to week 20 (week 20 - week 15)." (NCT02513771)
Timeframe: Week 0, week 15, week 20

,
Interventionlog10 ng/mL (Median)
Change from week 0 to week 15Change from week 15 to week 20
Placebo Arm-0.020.00
Sitagliptin Arm-0.030.01

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Change in sCD26

"sCD26 (soluble cluster of differentiation 26) is an enzyme that metabolizes DPP-4 (dipeptidyl peptidase-4), an enzyme that is inhibited by sitagliptin.~Change in log10 transformed sCD26 from Week 0 to week 15 (week 15 - week 0), and from week 15 to week 20 (week 20 - week 15)." (NCT02513771)
Timeframe: Week 0, week 15, week 20

,
Interventionlog10 ng/mL (Median)
Change from week 0 to week 15Change from week 15 to week 20
Placebo Arm-0.160.04
Sitagliptin Arm-0.160.08

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Change in sTNF-r1

"sTNF-r1 (soluble tumour necrosis alpha receptor 1) is a biomarker of inflammation.~Change in log10 transformed sTNF-r1 from Week 0 to week 15 (week 15 - week 0), and from week 15 to week 20 (week 20 - week 15)." (NCT02513771)
Timeframe: Week 0, week 15, week 20

,
Interventionlog10 pg/mL (Median)
Change from week 0 to week 15Change from week 15 to week 20
Placebo Arm-0.04-0.01
Sitagliptin Arm-0.010.00

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Change in sTNF-r2

"sTNF-r2 (soluble tumour necrosis alpha receptor 2) is a biomarker of inflammation.~Change in log10 transformed sTNF-r2 from Week 0 to week 15 (week 15 - week 0), and from week 15 to week 20 (week 20 - week 15)." (NCT02513771)
Timeframe: Week 0, week 15, week 20

,
Interventionlog10 pg/mL (Median)
Change from week 0 to week 15Change from week 15 to week 20
Placebo Arm-0.060.05
Sitagliptin Arm-0.050.06

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Change in %CD14+/CD16+ (Intermediate Monocytes)

"%CD14+/CD16+ is the percentage of cells that expressed both CD14 and CD16 in total monocytes (also known as intermediate monocytes).~This endpoint is measuring the change from week 0 to week 15 (week 15 - week 0) and change from week 15 to week 20 (week 20 - week 15).~Data for cellular markers are not available as of December 2017. These data are based on immunology assays which were tested in batch to minimize variability. Due to batch testing, shipment of samples for testing could not begin until after the study follow-up completion, which was 1 month after the primary complete date. Please note that these secondary outcomes were not included in the primary analyses. There are many outcomes in this study and the immunology lab had to give priority to the assays planned to be included in the primary manuscript. Results will be entered once the data is complete and analyzed." (NCT02513771)
Timeframe: Week 0, week 15, week 20

,
Interventionpercentage of cells (Median)
change from baseline to week 15change from week 15 to week 20
Placebo Arm-0.12-0.19
Sitagliptin Arm0.87-0.65

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Percentage of Participants Who Experienced One or More Adverse Events

An adverse event (AE) is any untoward medical occurrence in a patient or clinical investigation participant administered a pharmaceutical product. The AE does not have to have a causal relationship with this treatment. The AE can include any unfavourable and unintended sign, symptom, or disease or any worsening (change in frequency and/or intensity) of a preexisting condition that is temporally associated with the use of the pharmaceutical product. (NCT02532855)
Timeframe: Up to 26 weeks

InterventionPercentage of participants (Number)
Sitagliptin48.9
Dapagliflozin51.6

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Percentage of Participants With A1C <7% (53 mmol/Mol) at Week 24

A1C is blood marker used to report average blood glucose levels over prolonged periods of time and is reported as a percentage (%). Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. (NCT02532855)
Timeframe: Week 24

InterventionPercentage of Participants (Number)
Sitagliptin42.6
Dapagliflozin27.0

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Percentage of Participants Who Discontinued Study Drug Due to an AE

An adverse event (AE) is any untoward medical occurrence in a patient or clinical investigation participant administered a pharmaceutical product. The AE does not have to have a causal relationship with this treatment. The AE can include any unfavourable and unintended sign, symptom, or disease or any worsening (change in frequency and/or intensity) of a preexisting condition that is temporally associated with the use of the pharmaceutical product. (NCT02532855)
Timeframe: Up to 24 weeks

InterventionPercentage of participants (Number)
Sitagliptin3.3
Dapagliflozin3.3

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Change From Baseline in 2-hr Postprandial Glucose (PPG) at Week 24

The 2hr PPG is the change from baseline in mean post prandial glucose (change from baseline PPG = Week 24 mean T-120 glucose minus Baseline mean T-120 glucose) and shows each drugs impact on PPG. The 2-point MMTT measured values at T-0 and T-120 while the 3-point MMTT measured values at T-0, T-60, and T-120: although only a subset of the study had the 3-point MMTT performed, all participants had a T-0 and T-120 time point. A negative (-) change from baseline to Week 24 indicates better control of postprandial glucose. (NCT02532855)
Timeframe: Immediately before and 120 minutes after the standard meal at Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-40.4
Dapagliflozin-37.0

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Change From Baseline in A1C at Week 24

A1C is blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. Thus, this change from baseline reflects the Week 24 A1C minus the Week 0 A1C. (NCT02532855)
Timeframe: Baseline and Week 24

InterventionPercent A1C (Least Squares Mean)
Sitagliptin-0.51
Dapagliflozin-0.36

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24

Blood glucose was measured on a fasting basis. Blood was drawn at predose on Day 1 and after 24 weeks of treatment to determine change in plasma glucose levels (i.e., FPG at Week 24 minus FPG at Week 0). (NCT02532855)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-16.5
Dapagliflozin-20.1

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Change From Baseline in Glucagon Area Under the Curve (AUC0-120 Minutes) at Week 24

AUC endpoints were analyzed for participants who underwent the 3-point MMTT. Blood samples were drawn immediately prior to (T=0 minutes) and 60 and 120 minutes after the administration of the standard meal. The AUC curve was generated with the 3 time points. If any time point for a given participant was missing, the AUC was not included. Change in Postprandial Glucagon AUC after the morning meal (t=0 to 120 minutes) was calculated from the glucagon AUC over the first 120 minutes following the morning meal at baseline minus glucagon AUC over the first 120 minutes following the morning meal at Week 24. A negative (-) change from baseline to Week 24 indicates better control of postprandial glucose. (NCT02532855)
Timeframe: Immediately before and 60 and 120 minutes after the standard meal at Baseline and Week 24

Interventionpmol.hr/L (Least Squares Mean)
Sitagliptin-4.2
Dapagliflozin0.2

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Change From Baseline in Incremental 2-hour (2-hr) Postprandial Glucose Excursion (PPGE) at Week 24

The 2hr PPGE is the change from baseline in the mean incremental change in post meal glucose defined as T-120 minus T-0 for each participant: change from baseline PPGE = Week 24 mean (T-120 minus T-0) minus Baseline mean (T-120 minus T-0). The 2-point MMTT measured values at T-0 and T-120 while the 3-point MMTT measured values at T-0, T-60, and T-120: although only a subset of the study had the 3-point MMTT performed, all participants had a T-0 and T-120 time point. A negative (-) change from baseline to Week 24 indicates better control of postprandial glucose. (NCT02532855)
Timeframe: Immediately before and 120 minutes after the standard meal at Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin-24.2
Dapagliflozin-18.5

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Change From Baseline in Insulin AUC0-120 Minutes at Week 24

AUC endpoints were analyzed for participants who underwent the 3-point MMTT. Blood samples were drawn immediately prior to (T=0 minutes) and 60 and 120 minutes after the administration of the standard meal. The AUC curve was generated with the 3 time points. If any time point for a given participant was missing, the AUC was not included. Change in Postprandial Insulin AUC after the morning meal (t=0 to 120 minutes) was calculated from insulin AUC over the first 120 minutes following the morning meal at baseline minus insulin AUC over the first 120 minutes following the morning meal at Week 24. A negative (-) change from baseline to Week 24 indicates better control of postprandial glucose. (NCT02532855)
Timeframe: Immediately before and 60 and 120 minutes after the standard meal at Baseline and Week 24

InterventionmIU.hr/L (Least Squares Mean)
Sitagliptin-23.4
Dapagliflozin-28.2

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Change From Baseline in Postprandial Insulin AUC0-120 Minutes to Glucagon AUC0-120 Minutes Ratio at Week 24

AUC endpoints were analyzed for participants who underwent the 3-point MMTT. Blood samples were drawn immediately prior to (T=0 minutes) and 60 and 120 minutes after the administration of the standard meal. The AUC curve was generated with the 3 time points. If any time point for a given participant was missing, the AUC was not included. The endpoint was calculated from the ratio of (insulin AUC / glucagon AUC) over the first 120 minutes following the morning meal at baseline minus AUC over the first 120 minutes following the morning meal at Week 24. A negative (-) change from baseline to Week 24 indicates better control of postprandial glucose. (NCT02532855)
Timeframe: Immediately before and 60 and 120 minutes after the standard meal at Baseline and Week 24

InterventionRatio (Least Squares Mean)
Sitagliptin-0.6
Dapagliflozin-1.2

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Measurement of Serum Amyloid A Production Rate With Stable Isotope During Postprandial Period

(NCT02536248)
Timeframe: 6 weeks

Interventionmg/kg/day (Mean)
Sitagliptin0.039
Placebo0.049

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Duration of Intubation

Duration that patients required to be intubated (NCT02556918)
Timeframe: 10 days (average time of discharge from the hospital)

Interventiondays (Mean)
Sitagliptin0.5
Placebo0.7

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Length of Intensive Care Unit (ICU) Stay

Total number of days spent in intensive care unit (ICU) (NCT02556918)
Timeframe: 2 days (average time of discharge from ICU)

Interventiondays (Median)
Sitagliptin2.0
Placebo2.2

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Total IV Insulin in ICU

Total IV insulin in ICU during recovery period. (NCT02556918)
Timeframe: 2 days (average time of discharge from ICU)

Interventionunits (Mean)
Sitagliptin100.43
Placebo95.68

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Mean Insulin Dose Per Day During Intensive Care Unit (ICU) Recovery

Mean insulin infusion dose per day of ICU patients during recovery period. (NCT02556918)
Timeframe: 2 days (average time of discharge from ICU)

Interventionunit/day (Mean)
Sitagliptin45.9
Placebo46.4

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Mean Post-operative Blood Glucose (BG) Concentration

Mean post-operative blood glucose (BG) concentration during recovery period. (NCT02556918)
Timeframe: 10 days (average time of discharge from the hospital)

Interventionmmol/L (Mean)
Sitagliptin154.2
Placebo156.5

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Median Number of Days of Subcutaneous (SC) Insulin After Discontinuation of Continuous Intravenous Insulin Infusion (CII)

Median number of days patients requiring SC insulin after discontinuation of CII (NCT02556918)
Timeframe: Up to 14 days (time of discharge from the hospital)

Interventiondays (Median)
Sitagliptin4
Placebo4

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Number of Cerebrovascular Events

Number of cerebrovascular events including permanent stroke and reversible ischemic neurologic deficit (NCT02556918)
Timeframe: 10 days (average time of discharge from the hospital)

Interventionevents (Number)
Sitagliptin5
Placebo7

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Number of Intensive Care Unit (ICU) Readmission

Number of re-admissions to intensive care unit during the same hospital course. (NCT02556918)
Timeframe: 10 days (average time of discharge from the hospital)

Interventionreadmissions (Number)
Sitagliptin14
Placebo7

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Number of Patients Requiring Continuous Intravenous Insulin Infusion (CII)

Number of patients requiring CII to achieve a blood glucose level (BG) target between 150-200 mg/dl (NCT02556918)
Timeframe: 2 days (average time of discharge from ICU)

InterventionParticipants (Count of Participants)
Sitagliptin86
Placebo85

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Number of Patients Requiring Subcutaneous (SQ) Insulin After Discontinuation of Continuous Intravenous Insulin Infusion (CII)

Number of patients requiring subcutaneous (SQ) insulin after discontinuation of continuous intravenous insulin infusion (CII) (NCT02556918)
Timeframe: 10 days (average time of discharge from the hospital)

InterventionParticipants (Count of Participants)
Sitagliptin74
Placebo78

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Number of Subjects With Hyperglycemia (Blood Glucose Greater Than or Equal to 300 mg/dL) in Non-ICU

Number of subjects with hyperglycemia (blood glucose greater than or equal to 300 mg/dL) in non-ICU recovery period. (NCT02556918)
Timeframe: 10 days (average time of discharge from the hospital)

InterventionParticipants (Count of Participants)
Sitagliptin20
Placebo12

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Total Length of Hospital Stay

Total number of days spent in hospital (NCT02556918)
Timeframe: 10 days (average time of discharge from the hospital)

Interventiondays (Median)
Sitagliptin9
Placebo7

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Amount of Subcutaneous (SC) Insulin in Intensive Care Unit (ICU) 48 Hours

Amount of subcutaneous (SC) insulin in intensive care unit (ICU) 48 hours during recovery period. (NCT02556918)
Timeframe: 48 hours during recovery period

Interventionunits (Mean)
Sitagliptin0.48
Placebo1.5

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Mean Blood Glucose (BG) Concentration in the Intensive Care Unit (ICU)

Mean blood glucose (BG) concentration of ICU patients during recovery period. (NCT02556918)
Timeframe: 2 days (average time of discharge from ICU)

Interventionmmol/L (Mean)
Sitagliptin148.7
Placebo149.8

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Number of Patients With Hyperglycemia in the Intensive Care Unit (ICU)

Number of patients with blood glucose (BG) levels greater than 180 mg/dl (NCT02556918)
Timeframe: 2 days (average time of discharge from ICU)

InterventionParticipants (Count of Participants)
Sitagliptin76
Placebo68

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Number of Patients With Hypoglycemic Events in Intensive Care Unit (ICU)

Number of patients with events (blood glucose less than 70 mg/dL) in patients in intensive care unit (ICU). (NCT02556918)
Timeframe: 2 days (average time of discharge from ICU)

InterventionParticipants (Count of Participants)
Sitagliptin8
Placebo6

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Number of Patients With Hypoglycemic Events in Non-intensive Care Unit (ICU)

Number of Patients With hypoglycemic events (blood glucose less than 70 mg/dL) in patients in non-intensive care unit (ICU). (NCT02556918)
Timeframe: 10 days (average time of discharge from the hospital)

InterventionParticipants (Count of Participants)
Sitagliptin8
Placebo8

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Number of Patients With Persistent Hyperglycemia

Number of patients with two consecutive fasting and/or pre-meal blood glucose (BG) greater than 180 mg/dl, or with average daily BG greater than 80 mg/dl who require rescue therapy with subcutaneous (SC) insulin after discontinuation of continuous intravenous insulin infusion (CII). (NCT02556918)
Timeframe: 10 days (average time of discharge from the hospital)

InterventionParticipants (Count of Participants)
Sitagliptin58
Placebo59

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Number of Patients With Severe Hypoglycemic Events in Intensive Care Unit (ICU)

Number of Patients With severe hypoglycemia (blood glucose less than 40 mg/dL) in patients in intensive care unit (ICU). (NCT02556918)
Timeframe: 2 days (average time of discharge from ICU)

InterventionParticipants (Count of Participants)
Sitagliptin0
Placebo0

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Number of Patients With Severe Hypoglycemic Events in Non-intensive Care Unit (ICU)

Number of Patients With hypoglycemic events (blood glucose less than 40 mg/dL) in patients in non-intensive care unit (ICU). (NCT02556918)
Timeframe: 10 days (average time of discharge from the hospital)

InterventionParticipants (Count of Participants)
Sitagliptin0
Placebo0

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Number of Subjects Readmitted to the Hospital

Number of subjects readmitted to the hospital within 30 days (all-cause). (NCT02556918)
Timeframe: 30 days

InterventionParticipants (Count of Participants)
Sitagliptin10
Placebo12

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Number of Subjects Returning to the ER Within 30 Days

Number of subjects returning to the ER within 30 days (all-cause). (NCT02556918)
Timeframe: 30 days

InterventionParticipants (Count of Participants)
Sitagliptin61
Placebo57

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Amount of Subcutaneous (SC) Insulin Taken in Intensive Care Unit (ICU)

Total amount of SC insulin taken by ICU patients during recovery period. (NCT02556918)
Timeframe: 2 days (average time of discharge from ICU)

Interventionunits (Mean)
Sitagliptin1.0
Placebo2.2

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Composite of Perioperative Complications

Number of perioperative complications including hospital mortality, infection,acute renal failure, and acute mycordial infarction. (NCT02556918)
Timeframe: 10 days (average time of discharge from the hospital)

Interventionevents (Number)
Sitagliptin63
Placebo42

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Duration of Continuous Intravenous Insulin Infusion (CII)

Total hours of continuous intravenous insulin infusion (CII) (NCT02556918)
Timeframe: Up to 48 hours (average time of discharge from ICU)

Interventionhours (Mean)
Sitagliptin27.7
Placebo27.7

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Number of Subjects With Hyperglycemia in Intensive Care Unit (ICU)

Number of subjects with hyperglycemia (blood glucose greater than or equal to 300 mg/dL) in ICU recovery period. (NCT02556918)
Timeframe: 2 days (average time of discharge from ICU)

InterventionParticipants (Count of Participants)
Sitagliptin5
Placebo3

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Change From Baseline in HbA1c

Participants had HbA1c levels determined at baseline and at Week 52. HbA1c is reported as a percentage. A negative number reflects a decrease in percentage. (NCT02564211)
Timeframe: Baseline and Week 52

InterventionPercent (Mean)
Ipragliflozin-0.80

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Percentage of Participants Who Experienced at Least 1 Adverse Event (AE)

An AE was any unfavorable or unintended sign, symptom, or disease, and a causal relationship to the relevant investigational product is not considered. An AE could therefore be any unfavorable and unintended sign, including results from laboratory assessments, physical examination, electrocardiograms, and vital sign assessments. The percentage of participants that had AE was recorded. (NCT02564211)
Timeframe: Up to 54 weeks

InterventionPercentage of participants (Number)
Ipragliflozin77.9

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Percentage of Participants Who Had Study Drug Discontinued Due to an AE

The percentage of participants who had study treatment stopped due to an AE regardless if they completed study. (NCT02564211)
Timeframe: Up to 52 weeks

InterventionPercentage of Participants (Number)
Ipragliflozin5.2

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Percentage of Participants Who Discontinued Study Drug Due to an AE

An adverse event is defined as any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT02577003)
Timeframe: Up to 24 weeks

InterventionPercentage of participants (Number)
Ipragliflozin + Sitagliptin2.7
Placebo + Sitagliptin5.7

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Change From Baseline in 2-hr PMG at Week 24

Change from baseline in 2-hr PMG at Week 24 is defined as Week 24 2-hr PMG minus Week 0 2-hr PMG. Statistical analysis based on a cLDA model with terms for treatment, time, prior use of AHAs, the interactions of treatment by time, time by prior use of AHAs, treatment by time by prior use of AHAs, and baseline eGFR value with the constraint that the mean baseline 2-hr PMG is the same for both treatment groups. (NCT02577003)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Ipragliflozin + Sitagliptin-52.4
Placebo + Sitagliptin-3.8

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Change From Baseline in Body Weight at Week 24

Change from baseline in body weight at Week 24 is defined as Week 24 body weight minus Week 0 body weight. Statistical analysis based on a cLDA model with terms for treatment, time, prior use of AHAs, the interactions of treatment by time, time by prior use of AHAs and treatment by time by prior use of AHAs, and baseline eGFR value with the constraint that the mean baseline body weight is the same for both treatment groups. (NCT02577003)
Timeframe: Baseline and Week 24

Interventionkg (Least Squares Mean)
Ipragliflozin + Sitagliptin-2.4
Placebo + Sitagliptin-0.6

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Change From Baseline in Glucose Total AUC0-2hr After Meal at Week 24

Change from baseline in glucose total AUC0-2hr after meal at Week 24 is defined as Week 24 glucose total AUC0-2hr after a meal minus Week 0 glucose total AUC0-2hr after a meal. Statistical analysis based on a cLDA model with terms for treatment, time, prior use of AHAs, the interactions of treatment by time, time by prior use of AHAs and treatment by time by prior use of AHAs, and baseline eGFR value with the constraint that the mean baseline glucose total AUC0-2hr after meal is the same for both treatment groups. (NCT02577003)
Timeframe: Baseline and Week 24 (just before the loading meal [0 min], 30 min, 60 min and 120 min)

Interventionmg･hr/dL (Least Squares Mean)
Ipragliflozin + Sitagliptin-86.9
Placebo + Sitagliptin-2.3

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Change From Baseline in HbA1c at Week 24

HbA1c is measured as percent. Thus, this change from baseline reflects the Week 24 HbA1c percent minus the Week 0 HbA1c percent. Statistical analysis based on a constrained longitudinal data analysis (cLDA) model with terms for treatment, time, prior use of AHAs, the interactions of treatment by time, time by prior use of AHAs, treatment by time by prior use of AHAs, and baseline eGFR value with the constraint that the mean baseline HbA1c is the same for both treatment groups. (NCT02577003)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Ipragliflozin + Sitagliptin-0.84
Placebo + Sitagliptin-0.07

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Percentage of Participants Who Experienced at Least One Adverse Event (AE)

An adverse event is defined as any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT02577003)
Timeframe: Up to 26 weeks

InterventionPercentage of participants (Number)
Ipragliflozin + Sitagliptin50.7
Placebo + Sitagliptin65.7

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Change From Baseline in FPG at Week 24

Change from baseline in FPG at Week 24 is defined as Week 24 FPG minus Week 0 FPG. Statistical analysis based on a cLDA model with terms for treatment, time, prior use of AHAs, the interactions of treatment by time, time by prior use of AHAs, treatment by time by prior use of AHAs, and baseline eGFR value with the constraint that the mean baseline FPG is the same for both treatment groups. (NCT02577003)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Ipragliflozin + Sitagliptin-30.3
Placebo + Sitagliptin-2.1

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Percentage of Participants Who Experienced at Least One Adverse Event (AE)

An adverse event is defined as any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT02577016)
Timeframe: Up to 26 weeks

InterventionPercentage of participants (Number)
Sitagliptin + Ipragliflozin54.3
Placebo + Ipragliflozin63.4

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Change From Baseline in 2-hr PMG at Week 24

Change from baseline in 2-hr PMG at Week 24 is defined as Week 24 2-hr PMG minus Week 0 2-hr PMG. Statistical analysis based on a cLDA model with terms for treatment, time, prior use of AHAs, the interactions of treatment by time, time by prior use of AHAs, and treatment by time by prior use of AHAs with the constraint that the mean baseline 2-hr PMG is the same for both treatment groups. (NCT02577016)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin + Ipragliflozin-39.0
Placebo + Ipragliflozin3.4

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Change From Baseline in FPG at Week 24

Change from baseline in FPG at Week 24 is defined as Week 24 FPG minus Week 0 FPG. Statistical analysis based on a cLDA model with terms for treatment, time, prior use of AHAs, the interactions of treatment by time, time by prior use of AHAs, and treatment by time by prior use of AHAs with the constraint that the mean baseline FPG is the same for both treatment groups. (NCT02577016)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Sitagliptin + Ipragliflozin-11.8
Placebo + Ipragliflozin-0.6

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Change From Baseline in Glucose Total Area Under the Plasma Concentration Curve From Hour 0 to Hour 2 (AUC0-2hr) After Meal at Week 24

Change from Baseline in Glucose Total AUC0-2hr after Meal at Week 24 is defined as Week 24 Glucose Total AUC0-2hr after a meal minus Week 0 Glucose Total AUC0-2hr after a meal. Statistical analysis based on a cLDA model with terms for treatment, time, prior use of AHAs, the interactions of treatment by time, time by prior use of AHAs, and treatment by time by prior use of AHAs with the constraint that the mean baseline glucose total AUC0-2hr after meal is the same for both treatment groups. (NCT02577016)
Timeframe: Baseline and Week 24 (just before loading meal [0 min], 30 min, 60 min and 120 min)

Interventionmg･hr/dL (Least Squares Mean)
Sitagliptin + Ipragliflozin-65.7
Placebo + Ipragliflozin1.3

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Change From Baseline in HbA1c at Week 24

HbA1c is measured as percent. Thus, this change from baseline reflects the Week 24 HbA1c percent minus the Week 0 HbA1c percent. Statistical analysis based on a constrained longitudinal data analysis (cLDA) model with terms for treatment, time, prior use of AHAs, the interactions of treatment by time, time by prior use of AHAs, and treatment by time by prior use of AHAs with the constraint that the mean baseline is the same for both treatment groups. (NCT02577016)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Sitagliptin + Ipragliflozin-0.69
Placebo + Ipragliflozin0.14

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Percentage of Participants Who Discontinued Study Drug Due to an AE

An adverse event is defined as any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT02577016)
Timeframe: Up to 24 weeks

InterventionPercentage of participants (Number)
Sitagliptin + Ipragliflozin2.9
Placebo + Ipragliflozin0.0

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Time to Rescue Medication

Presented results are the number of participants who had taken rescue medication anytime during the periods, from week 0 to week 26, week 0 to week 52 and week 0 to week 78. Rescue medication was defined as any new anti-diabetic medication used as add-on to trial product and used for more than 21 days with the initiation at or after randomisation (week 0) and before last day on trial product, and/or intensification of anti-diabetic medication (a more than 20% increase in dose relative to baseline) for more than 21 days with the intensification at or after randomisation and before last day on trial product. Results are based on the data from the on-treatment without rescue medication observation period, which was the time period when a participant was on treatment with trial product, excluding any period after initiation of rescue medication and/or premature trial product discontinuation. (NCT02607865)
Timeframe: Weeks 0-78

,,,
InterventionParticipants (Count of Participants)
Week 0 to week 26Week 0 to week 52Week 0 to week 78
Oral Semaglutide 14 mg53147
Oral Semaglutide 3 mg25121160
Oral Semaglutide 7 mg1173103
Sitagliptin 100 mg1394129

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Change in SMPG - Mean 7-point Profile

Change from baseline (week 0) in mean 7-point self-measured plasma glucose (SMPG) profile. SMPG was recorded at the following 7 time points: before breakfast, 90 minutes after start of breakfast, before lunch, 90 minutes after start of lunch, before dinner, 90 minutes after dinner and at bedtime. Mean 7-point profile was defined as the area under the profile, calculated using the trapezoidal method, divided by the measurement time. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
Interventionmmol/L (Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg-1.7-1.8-1.7
Oral Semaglutide 3 mg-1.1-1.3-1.3
Oral Semaglutide 7 mg-1.5-1.5-1.5
Sitagliptin 100 mg-1.2-1.4-1.3

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Change in FPG

Change from baseline (week 0) in fasting plasma glucose (FPG) was evaluated at weeks 26, 52 and 78. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
Interventionmmol/L (Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg-1.67-1.75-1.65
Oral Semaglutide 3 mg-0.83-0.98-1.07
Oral Semaglutide 7 mg-1.17-1.28-1.11
Sitagliptin 100 mg-0.90-1.03-0.91

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Change in Free Fatty Acids (Ratio to Baseline)

Change from baseline (week 0) in free fatty acids (FFA) (mmol/L) at weeks 26, 52 and 78 is presented as ratio to baseline. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. Because of an issue with the handling of the blood samples for FFA, all FFA data were considered invalid for this trial; thus, no conclusion with regards to FFA levels can be made based on the data presented here. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionRatio of FFA (Geometric Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg0.880.960.88
Oral Semaglutide 3 mg0.961.030.92
Oral Semaglutide 7 mg0.911.000.87
Sitagliptin 100 mg0.900.980.87

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Change in HbA1c: Week 26

Change from baseline (week 0) in glycosylated haemoglobin (HbA1c) was evaluated at week 26. The endpoint was evaluated based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. The endpoint was also evaluated based on the data from the on-treatment without rescue medication observation period, which was the time period when a participant was on treatment with trial product, excluding any period after initiation of rescue medication and/or premature trial product discontinuation. (NCT02607865)
Timeframe: Week 0, week 26

,,,
InterventionPercentage of HbA1c (Mean)
In-trialOn-treatment without rescue medication
Oral Semaglutide 14 mg-1.3-1.4
Oral Semaglutide 3 mg-0.6-0.6
Oral Semaglutide 7 mg-1.1-1.2
Sitagliptin 100 mg-0.8-0.8

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Change in HbA1c: Weeks 52 and 78

Change from baseline (week 0) in HbA1c was evaluated at weeks 52 and 78. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 52, week 78

,,,
InterventionPercentage of HbA1c (Mean)
Week 52Week 78
Oral Semaglutide 14 mg-1.2-1.1
Oral Semaglutide 3 mg-0.6-0.6
Oral Semaglutide 7 mg-1.0-0.9
Sitagliptin 100 mg-0.7-0.7

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Change in HDL Cholesterol (Ratio to Baseline)

Change from baseline (week 0) in high-density lipoprotein (HDL) cholesterol (mmol/L) at weeks 26, 52 and 78 is presented as ratio to baseline. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionRatio of HDL cholesterol (Geometric Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg0.981.011.00
Oral Semaglutide 3 mg0.970.990.97
Oral Semaglutide 7 mg0.991.010.99
Sitagliptin 100 mg0.990.990.99

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Participants With Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes

Treatment emergent severe or BG confirmed symptomatic hypoglycaemic episodes were recorded from week 0 to week 83 (78-week treatment period plus the 5-week follow-up period). Hypoglycaemic episodes with onset during the on-treatment observation period were considered treatment-emergent. On-treatment observation period was defined as the time period when a subject was on treatment with trial product, including any period after initiation of rescue medication. Severe hypoglycaemia was defined as an episode requiring assistance of another person to actively administer carbohydrate or glucagon, or take other corrective actions. BG-confirmed symptomatic hypoglycaemia: Confirmed by a glucose value <3.1 mmol/L (56 mg/dL) with symptoms consistent with hypoglycaemia. (NCT02607865)
Timeframe: Weeks 0-83

InterventionParticipants (Count of Participants)
Oral Semaglutide 3 mg23
Oral Semaglutide 7 mg24
Oral Semaglutide 14 mg36
Sitagliptin 100 mg39

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Change in LDL Cholesterol (Ratio to Baseline)

Change from baseline (week 0) in low-density lipoprotein (LDL) cholesterol (mmol/L) at weeks 26, 52 and 78 is presented as ratio to baseline. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionRatio of LDL cholesterol (Geometric Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg0.980.991.00
Oral Semaglutide 3 mg1.021.021.03
Oral Semaglutide 7 mg0.980.991.00
Sitagliptin 100 mg1.021.031.03

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Change in Lipase (Ratio to Baseline)

Change from baseline (week 0) in lipase (U/L) at weeks 26, 52 and 78 is presented as ratio to baseline. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionRatio (Geometric Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg1.261.251.18
Oral Semaglutide 3 mg1.071.061.04
Oral Semaglutide 7 mg1.131.151.14
Sitagliptin 100 mg1.141.151.10

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Change in Pulse Rate

Change from baseline (week 0) in pulse rate was evaluated at weeks 26, 52 and 78. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionBeats/minute (Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg322
Oral Semaglutide 3 mg101
Oral Semaglutide 7 mg221
Sitagliptin 100 mg0-00

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Change in SBP and DBP

Change from baseline (week 0) in systolic blood pressure (SBP) and diastolic blood pressure (DBP) was evaluated at weeks 26, 52 and 78. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionmmHg (Mean)
SBP: Week 26SBP: Week 52SBP: Week 78DBP: Week 26DBP: Week 52DBP: Week 78
Oral Semaglutide 14 mg-3-3-3-1-1-1
Oral Semaglutide 3 mg-2-2-2-1-2-1
Oral Semaglutide 7 mg-2-4-3-0-1-1
Sitagliptin 100 mg-2-10-0-1-1

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Change in SF-36v2 (Acute Version) Health Survey: Scores From the 8 Domains, the Physical Component Summary (PCS) and the Mental Component Summary (MCS)

SF-36 is a 36-item patient-reported survey of patient health that measures the participant's overall health-related quality of life (HRQoL). SF-36v2™ (acute version) questionnaire measured eight domains of functional health and well-being as well as two component summary scores (physical component summary (PCS) and mental component summary (MCS)). The 0-100 scale scores (where higher scores indicated a better HRQoL) from the SF-36 were converted to norm-based scores to enable a direct interpretation in relation to the distribution of the scores in the 2009 U.S. general population. In the metric of norm-based scores, 50 and 10 corresponds to the mean and standard deviation respectively of the 2009 U.S. general population. Change from baseline (week 0) in the domain scores and component summary (PCS and MCS) scores were evaluated at weeks 26, 52 and 78. A positive change score indicates an improvement since baseline. Results are based on the data from the in-trial observation period. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionScore on a scale (Mean)
1) Physical functioning (week 26)1) Physical functioning (week 52)1) Physical functioning (week 78)2) Role-Physical (week 26)2) Role-Physical (week 52)2) Role-Physical (week 78)3) Bodily pain (week 26)3) Bodily pain (week 52)3) Bodily pain (week 78)4) General health (week 26)4) General health (week 52)4) General health (week 78)5) Vitality (week 26)5) Vitality (week 52)5) Vitality (week 78)6) Social functioning (week 26)6) Social functioning (week 52)6) Social functioning (week 78)7) Role emotional (week 26)7) Role emotional (week 52)7) Role emotional (week 78)8) Mental health (week 26)8) Mental health (week 52)8) Mental health (week 78)Physical component summary (week 26)Physical component summary (week 52)Physical component summary (week 78)Mental component summary (week 26)Mental component summary (week 52)Mental component summary (week 78)
Oral Semaglutide 14 mg0.630.360.54-0.13-0.82-0.330.22-0.640.741.191.031.210.880.580.710.31-0.83-0.27-0.37-0.86-0.300.240.050.280.630.090.670.08-0.37-0.07
Oral Semaglutide 3 mg0.370.290.060.42-0.050.280.560.160.481.171.061.020.590.451.050.11-0.25-0.380.840.150.320.330.450.190.560.310.460.480.230.27
Oral Semaglutide 7 mg1.120.640.940.76-0.06-0.01-0.11-0.650.321.671.201.211.110.790.850.15-0.370.190.67-0.450.230.240.420.290.980.360.710.34-0.000.23
Sitagliptin 100 mg0.460.060.090.38-0.690.440.440.670.541.420.951.321.030.191.070.09-0.680.570.15-0.63-0.240.610.230.300.690.310.700.41-0.310.30

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Change in SMPG - Mean Postprandial Increment Over All Meals

Change from baseline (week 0) in the average of the post-prandial increments over all meals was evaluated at weeks 26, 52 and 78. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
Interventionmmol/L (Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg-0.6-0.7-0.6
Oral Semaglutide 3 mg-0.4-0.4-0.4
Oral Semaglutide 7 mg-0.4-0.4-0.4
Sitagliptin 100 mg-0.6-0.4-0.6

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Change in Total Cholesterol (Ratio to Baseline)

Change from baseline (week 0) in total cholesterol (mmol/L) at weeks 26, 52 and 78 is presented as ratio to baseline. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionRatio of total cholesterol (Geometric Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg0.970.980.99
Oral Semaglutide 3 mg1.001.001.00
Oral Semaglutide 7 mg0.980.990.99
Sitagliptin 100 mg1.001.011.00

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Change in IWQoL-Lite-CT: Total Score and Scores From the 4 Domains

The Impact of Weight on Quality of Life Clinical Trials Version (IWQOL-Lite-CT) is designed to assess the impact of changes in weight on patients' quality of life within the context of clinical trials. The items of the IWQOL-Lite-CT pertain to physical functioning (physical, physical function and pain/discomfort) and psychosocial domains and all items employ a 5-point graded response scale (never, rarely, sometimes, usually, always; or not at all true, a little true, moderately true, mostly true, completely true). All IWQOL-Lite-CT composite scores range from 0 to 100, with higher scores reflecting better levels of functioning. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionScore on a scale (Mean)
1) Physical (week 26)1) Physical (week 52)1) Physical (week 78)2) Physical function (week 26)2) Physical function (week 52)2) Physical function (week 78)3) Pain/discomfort (week 26)3) Pain/discomfort (week 52)3) Pain/discomfort (week 78)4) Psychosocial (week 26)4) Psychosocial (week 52)4) Psychosocial (week 78)IWQOL-Lite-CT Total (week 26)IWQOL-Lite-CT Total (week 52)IWQOL-Lite-CT Total (week 78)
Oral Semaglutide 14 mg2.873.183.863.203.193.762.033.154.072.983.973.732.953.643.77
Oral Semaglutide 3 mg3.251.842.713.522.282.552.510.763.062.693.123.832.882.673.45
Oral Semaglutide 7 mg2.383.033.552.783.244.041.372.522.354.305.195.363.624.434.73
Sitagliptin 100 mg1.971.492.861.701.222.542.662.123.632.102.533.292.052.173.16

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Change in Triglycerides (Ratio to Baseline)

Change from baseline (week 0) in triglycerides (mmol/L) at weeks 26, 52 and 78 is presented as ratio to baseline. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionRatio of triglycerides (Geometric Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg0.920.930.92
Oral Semaglutide 3 mg0.991.000.95
Oral Semaglutide 7 mg0.960.970.94
Sitagliptin 100 mg0.970.980.93

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Participants Who Achieve HbA1c <7.0 % (53 mmol/Mol) Without Hypoglycaemia (Severe or BG Confirmed Symptomatic Hypoglycaemia) and no Weight Gain (Yes/no)

Participants who achieved HbA1c less than 7.0 % without severe or blood glucose (BG) confirmed symptomatic hypoglycaemia and without weight gain (yes/no) at weeks 26, 52 and 78 are presented. Severe hypoglycaemia was defined as an episode requiring assistance of another person to actively administer carbohydrate or glucagon, or take other corrective actions. BG-confirmed symptomatic hypoglycaemia was defined as an episode with plasma glucose value <3.1 mmol/L with symptoms consistent with hypoglycaemia. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 26, week 52, week 78

InterventionParticipants (Count of Participants)
Week 2671931141Week 2671931138Week 2671931139Week 2671931140Week 5271931138Week 5271931141Week 5271931139Week 5271931140Week 7871931140Week 7871931141Week 7871931138Week 7871931139
YesNo
Oral Semaglutide 7 mg155
Oral Semaglutide 14 mg208
Sitagliptin 100 mg90
Oral Semaglutide 3 mg348
Oral Semaglutide 7 mg283
Oral Semaglutide 14 mg228
Sitagliptin 100 mg356
Oral Semaglutide 3 mg87
Oral Semaglutide 7 mg134
Oral Semaglutide 14 mg195
Sitagliptin 100 mg87
Oral Semaglutide 3 mg340
Oral Semaglutide 7 mg297
Oral Semaglutide 14 mg239
Sitagliptin 100 mg349
Oral Semaglutide 3 mg85
Oral Semaglutide 7 mg136
Oral Semaglutide 14 mg151
Sitagliptin 100 mg84
Oral Semaglutide 3 mg336
Oral Semaglutide 7 mg288
Oral Semaglutide 14 mg274
Sitagliptin 100 mg355

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Change in Physical Examination

Participants with physical examination findings, normal, abnormal NCS and abnormal CS at baseline (weeks -2), weeks 52 and 78 are presented. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. Results are presented for the following examinations: 1) Cardiovascular system; 2) Central and peripheral nervous system; 3) Gastrointestinal system, incl. mouth; 4) General appearance; 5) Head, ears, eyes, nose, throat, neck; 6) Lymph node palpation; 7) Musculoskeletal system; 8) Respiratory system; 9) Skin; 10) Thyroid gland. (NCT02607865)
Timeframe: Week -2, week 52, week 78

InterventionParticipants (Count of Participants)
1) Cardiovascular system (week -2)719311381) Cardiovascular system (week -2)719311391) Cardiovascular system (week -2)719311401) Cardiovascular system (week -2)719311411) Cardiovascular system (week 52)719311381) Cardiovascular system (week 52)719311391) Cardiovascular system (week 52)719311401) Cardiovascular system (week 52)719311411) Cardiovascular system (week 78)719311381) Cardiovascular system (week 78)719311391) Cardiovascular system (week 78)719311401) Cardiovascular system (week 78)719311412) Central and peripheral nervous system (week -2)719311382) Central and peripheral nervous system (week -2)719311392) Central and peripheral nervous system (week -2)719311402) Central and peripheral nervous system (week -2)719311412) Central and peripheral nervous system (week 52)719311382) Central and peripheral nervous system (week 52)719311392) Central and peripheral nervous system (week 52)719311402) Central and peripheral nervous system (week 52)719311412) Central and peripheral nervous system (week 78)719311382) Central and peripheral nervous system (week 78)719311392) Central and peripheral nervous system (week 78)719311402) Central and peripheral nervous system (week 78)719311413) Gastrointestinal system, incl. mouth (week -2)719311383) Gastrointestinal system, incl. mouth (week -2)719311393) Gastrointestinal system, incl. mouth (week -2)719311403) Gastrointestinal system, incl. mouth (week -2)719311413) Gastrointestinal system, incl. mouth (week 52)719311393) Gastrointestinal system, incl. mouth (week 52)719311413) Gastrointestinal system, incl. mouth (week 52)719311383) Gastrointestinal system, incl. mouth (week 52)719311403) Gastrointestinal system, incl. mouth (week 78)719311393) Gastrointestinal system, incl. mouth (week 78)719311413) Gastrointestinal system, incl. mouth (week 78)719311383) Gastrointestinal system, incl. mouth (week 78)719311404) General appearance (week -2)719311414) General appearance (week -2)719311384) General appearance (week -2)719311394) General appearance (week -2)719311404) General appearance (week 52)719311384) General appearance (week 52)719311394) General appearance (week 52)719311404) General appearance (week 52)719311414) General appearance (week 78)719311384) General appearance (week 78)719311394) General appearance (week 78)719311404) General appearance (week 78)719311415) Head, ears, eyes, nose, throat, neck (week -2)719311385) Head, ears, eyes, nose, throat, neck (week -2)719311395) Head, ears, eyes, nose, throat, neck (week -2)719311405) Head, ears, eyes, nose, throat, neck (week -2)719311415) Head, ears, eyes, nose, throat, neck (week 52)719311385) Head, ears, eyes, nose, throat, neck (week 52)719311395) Head, ears, eyes, nose, throat, neck (week 52)719311405) Head, ears, eyes, nose, throat, neck (week 52)719311415) Head, ears, eyes, nose, throat, neck (week 78)719311385) Head, ears, eyes, nose, throat, neck (week 78)719311395) Head, ears, eyes, nose, throat, neck (week 78)719311405) Head, ears, eyes, nose, throat, neck (week 78)719311416) Lymph node palpation (week -2)719311416) Lymph node palpation (week -2)719311386) Lymph node palpation (week -2)719311396) Lymph node palpation (week -2)719311406) Lymph node palpation (week 52)719311416) Lymph node palpation (week 52)719311386) Lymph node palpation (week 52)719311396) Lymph node palpation (week 52)719311406) Lymph node palpation (week 78)719311416) Lymph node palpation (week 78)719311386) Lymph node palpation (week 78)719311396) Lymph node palpation (week 78)719311407) Musculoskeletal system (week -2)719311387) Musculoskeletal system (week -2)719311397) Musculoskeletal system (week -2)719311407) Musculoskeletal system (week -2)719311417) Musculoskeletal system (week 52)719311387) Musculoskeletal system (week 52)719311397) Musculoskeletal system (week 52)719311407) Musculoskeletal system (week 52)719311417) Musculoskeletal system (week 78)719311397) Musculoskeletal system (week 78)719311407) Musculoskeletal system (week 78)719311417) Musculoskeletal system (week 78)719311388) Respiratory system (week -2)719311408) Respiratory system (week -2)719311418) Respiratory system (week -2)719311388) Respiratory system (week -2)719311398) Respiratory system (week 52)719311408) Respiratory system (week 52)719311418) Respiratory system (week 52)719311388) Respiratory system (week 52)719311398) Respiratory system (week 78)719311388) Respiratory system (week 78)719311398) Respiratory system (week 78)719311408) Respiratory system (week 78)719311419) Skin (week -2)719311389) Skin (week -2)719311399) Skin (week -2)719311409) Skin (week -2)719311419) Skin (week 52)719311409) Skin (week 52)719311419) Skin (week 52)719311389) Skin (week 52)719311399) Skin (week 78)719311389) Skin (week 78)719311399) Skin (week 78)719311409) Skin (week 78)7193114110) Thyroid gland (week -2)7193113810) Thyroid gland (week -2)7193113910) Thyroid gland (week -2)7193114010) Thyroid gland (week -2)7193114110) Thyroid gland (week 52)7193113810) Thyroid gland (week 52)7193113910) Thyroid gland (week 52)7193114010) Thyroid gland (week 52)7193114110) Thyroid gland (week 78)7193113910) Thyroid gland (week 78)7193114110) Thyroid gland (week 78)7193113810) Thyroid gland (week 78)71931140
Abnormal NCSAbnormal CSNormal
Oral Semaglutide 3 mg431
Oral Semaglutide 7 mg425
Oral Semaglutide 14 mg432
Sitagliptin 100 mg424
Oral Semaglutide 3 mg30
Oral Semaglutide 7 mg38
Oral Semaglutide 14 mg30
Oral Semaglutide 3 mg5
Oral Semaglutide 14 mg3
Oral Semaglutide 3 mg398
Oral Semaglutide 7 mg396
Oral Semaglutide 14 mg404
Sitagliptin 100 mg399
Oral Semaglutide 3 mg24
Oral Semaglutide 7 mg36
Oral Semaglutide 14 mg28
Sitagliptin 100 mg37
Oral Semaglutide 3 mg395
Oral Semaglutide 7 mg386
Oral Semaglutide 14 mg402
Oral Semaglutide 7 mg33
Oral Semaglutide 14 mg24
Oral Semaglutide 14 mg2
Oral Semaglutide 3 mg410
Oral Semaglutide 7 mg415
Oral Semaglutide 14 mg407
Sitagliptin 100 mg409
Oral Semaglutide 3 mg44
Oral Semaglutide 7 mg42
Oral Semaglutide 14 mg49
Sitagliptin 100 mg43
Oral Semaglutide 3 mg12
Oral Semaglutide 7 mg6
Sitagliptin 100 mg14
Oral Semaglutide 3 mg376
Oral Semaglutide 7 mg382
Oral Semaglutide 14 mg388
Sitagliptin 100 mg385
Oral Semaglutide 7 mg45
Oral Semaglutide 14 mg38
Sitagliptin 100 mg42
Oral Semaglutide 3 mg7
Oral Semaglutide 14 mg9
Oral Semaglutide 3 mg377
Oral Semaglutide 7 mg376
Oral Semaglutide 14 mg384
Oral Semaglutide 3 mg43
Oral Semaglutide 7 mg43
Oral Semaglutide 14 mg37
Oral Semaglutide 3 mg4
Oral Semaglutide 7 mg4
Sitagliptin 100 mg5
Oral Semaglutide 3 mg419
Oral Semaglutide 7 mg421
Oral Semaglutide 14 mg420
Sitagliptin 100 mg421
Oral Semaglutide 3 mg45
Oral Semaglutide 7 mg39
Oral Semaglutide 14 mg45
Sitagliptin 100 mg45
Oral Semaglutide 14 mg0
Oral Semaglutide 3 mg386
Oral Semaglutide 7 mg402
Oral Semaglutide 14 mg397
Sitagliptin 100 mg394
Oral Semaglutide 3 mg39
Oral Semaglutide 7 mg28
Oral Semaglutide 14 mg36
Sitagliptin 100 mg40
Oral Semaglutide 7 mg3
Sitagliptin 100 mg2
Oral Semaglutide 7 mg387
Oral Semaglutide 14 mg393
Sitagliptin 100 mg408
Oral Semaglutide 3 mg26
Oral Semaglutide 7 mg31
Oral Semaglutide 14 mg35
Sitagliptin 100 mg31
Oral Semaglutide 3 mg0
Oral Semaglutide 7 mg5
Oral Semaglutide 3 mg407
Oral Semaglutide 7 mg405
Oral Semaglutide 14 mg412
Sitagliptin 100 mg405
Sitagliptin 100 mg46
Oral Semaglutide 3 mg16
Oral Semaglutide 7 mg14
Oral Semaglutide 14 mg15
Sitagliptin 100 mg15
Oral Semaglutide 3 mg381
Oral Semaglutide 7 mg384
Oral Semaglutide 14 mg390
Oral Semaglutide 3 mg37
Oral Semaglutide 7 mg37
Oral Semaglutide 14 mg33
Sitagliptin 100 mg39
Oral Semaglutide 3 mg8
Oral Semaglutide 14 mg12
Oral Semaglutide 3 mg379
Oral Semaglutide 7 mg373
Oral Semaglutide 7 mg40
Oral Semaglutide 7 mg10
Oral Semaglutide 3 mg441
Oral Semaglutide 7 mg440
Oral Semaglutide 14 mg435
Sitagliptin 100 mg444
Oral Semaglutide 3 mg25
Oral Semaglutide 7 mg24
Oral Semaglutide 14 mg27
Sitagliptin 100 mg21
Oral Semaglutide 7 mg0
Oral Semaglutide 7 mg411
Sitagliptin 100 mg410
Oral Semaglutide 7 mg21
Sitagliptin 100 mg26
Oral Semaglutide 3 mg3
Oral Semaglutide 7 mg1
Oral Semaglutide 14 mg4
Oral Semaglutide 3 mg400
Oral Semaglutide 14 mg399
Sitagliptin 100 mg415
Oral Semaglutide 3 mg22
Oral Semaglutide 7 mg17
Sitagliptin 100 mg25
Oral Semaglutide 14 mg1
Oral Semaglutide 3 mg466
Oral Semaglutide 7 mg462
Oral Semaglutide 14 mg463
Sitagliptin 100 mg464
Oral Semaglutide 3 mg425
Oral Semaglutide 7 mg432
Oral Semaglutide 14 mg434
Sitagliptin 100 mg436
Oral Semaglutide 3 mg421
Oral Semaglutide 7 mg423
Sitagliptin 100 mg441
Oral Semaglutide 7 mg435
Oral Semaglutide 14 mg440
Sitagliptin 100 mg430
Oral Semaglutide 14 mg23
Sitagliptin 100 mg32
Oral Semaglutide 3 mg6
Sitagliptin 100 mg4
Oral Semaglutide 3 mg383
Oral Semaglutide 7 mg400
Oral Semaglutide 14 mg408
Sitagliptin 100 mg403
Oral Semaglutide 3 mg388
Oral Semaglutide 7 mg389
Sitagliptin 100 mg413
Oral Semaglutide 3 mg33
Sitagliptin 100 mg23
Oral Semaglutide 3 mg458
Oral Semaglutide 7 mg451
Oral Semaglutide 14 mg462
Sitagliptin 100 mg456
Oral Semaglutide 7 mg9
Sitagliptin 100 mg10
Sitagliptin 100 mg0
Oral Semaglutide 3 mg418
Oral Semaglutide 7 mg427
Oral Semaglutide 14 mg431
Sitagliptin 100 mg429
Sitagliptin 100 mg6
Oral Semaglutide 7 mg2
Sitagliptin 100 mg1
Oral Semaglutide 7 mg418
Oral Semaglutide 14 mg427
Sitagliptin 100 mg434
Oral Semaglutide 3 mg394
Oral Semaglutide 14 mg394
Sitagliptin 100 mg402
Oral Semaglutide 3 mg66
Oral Semaglutide 7 mg56
Oral Semaglutide 14 mg61
Sitagliptin 100 mg58
Oral Semaglutide 7 mg8
Oral Semaglutide 14 mg10
Oral Semaglutide 3 mg372
Oral Semaglutide 7 mg383
Oral Semaglutide 14 mg383
Sitagliptin 100 mg375
Oral Semaglutide 3 mg52
Oral Semaglutide 7 mg44
Oral Semaglutide 14 mg44
Sitagliptin 100 mg51
Oral Semaglutide 3 mg361
Oral Semaglutide 7 mg370
Oral Semaglutide 14 mg382
Sitagliptin 100 mg393
Oral Semaglutide 3 mg55
Sitagliptin 100 mg41
Sitagliptin 100 mg7
Oral Semaglutide 3 mg451
Oral Semaglutide 7 mg452
Oral Semaglutide 14 mg451
Sitagliptin 100 mg454
Oral Semaglutide 3 mg13
Oral Semaglutide 7 mg11
Oral Semaglutide 14 mg11
Sitagliptin 100 mg12
Oral Semaglutide 3 mg1
Oral Semaglutide 3 mg413
Oral Semaglutide 14 mg425
Sitagliptin 100 mg427
Oral Semaglutide 3 mg11
Oral Semaglutide 14 mg7
Sitagliptin 100 mg8
Oral Semaglutide 3 mg2
Oral Semaglutide 3 mg411
Oral Semaglutide 14 mg418
Sitagliptin 100 mg433
Oral Semaglutide 7 mg12
Oral Semaglutide 14 mg8

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Number of TEAEs During Exposure to Trial Product

Treatment emergent adverse events (TEAEs) were recorded from week 0 to week 83 (78-week treatment period plus the 5-week follow-up period). Adverse events (AEs) with onset during the on-treatment observation period were considered treatment-emergent. On-treatment observation period: Time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02607865)
Timeframe: Weeks 0-83

InterventionEvents (Number)
Oral Semaglutide 3 mg1774
Oral Semaglutide 7 mg1686
Oral Semaglutide 14 mg1824
Sitagliptin 100 mg1852

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Number of Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes

Treatment emergent severe or BG confirmed symptomatic hypoglycaemic episodes were recorded during weeks 0-83 (78-week treatment period plus the 5-week follow-up period). Hypoglycaemic episodes with onset during the on-treatment observation period were considered treatment-emergent. On-treatment observation period was defined as the time period when a subject was on treatment with trial product, including any period after initiation of rescue medication. Severe hypoglycaemia was defined as an episode requiring assistance of another person to actively administer carbohydrate or glucagon, or take other corrective actions. BG-confirmed symptomatic hypoglycaemia: Confirmed by a glucose value <3.1 mmol/L (56 mg/dL) with symptoms consistent with hypoglycaemia. (NCT02607865)
Timeframe: Weeks 0-83

InterventionEpisodes (Number)
Oral Semaglutide 3 mg56
Oral Semaglutide 7 mg42
Oral Semaglutide 14 mg60
Sitagliptin 100 mg76

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Occurrence of Anti-semaglutide Binding Antibodies (Yes/no)

This outcome measure is only applicable for the oral semaglutide treatment arms (3 mg, 7 mg and 14 mg). Number of participants who measured with anti-semaglutide binding antibodies anytime during post-baseline visits (weeks 0-83) are presented. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Weeks 0-83

InterventionParticipants (Count of Participants)
Oral Semaglutide 3 mg1
Oral Semaglutide 7 mg2
Oral Semaglutide 14 mg3

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Occurrence of Anti-semaglutide Binding Antibodies Cross Reacting With Native GLP-1 (Yes/no)

This outcome measure is only applicable for the oral semaglutide treatment arms (3 mg, 7 mg and 14 mg). Number of participants who measured with anti-semaglutide binding antibodies cross reacting with native glucagon-like peptide-1 (GLP-1) anytime during post-baseline visits (weeks 0-83) are presented. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Weeks 0-83

InterventionParticipants (Count of Participants)
Oral Semaglutide 3 mg0
Oral Semaglutide 7 mg1
Oral Semaglutide 14 mg1

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Occurrence of Anti-semaglutide Neutralising Antibodies (Yes/no)

This outcome measure is only applicable for the oral semaglutide treatment arms (3 mg, 7 mg and 14 mg). Number of participants who measured with anti-semaglutide neutralising antibodies anytime during post-baseline visits (weeks 0-83) are presented. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Weeks 0-83

InterventionParticipants (Count of Participants)
Oral Semaglutide 3 mg0
Oral Semaglutide 7 mg0
Oral Semaglutide 14 mg0

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Occurrence of Anti-semaglutide Neutralising Antibodies Cross Reacting With Native GLP-1 (Yes/no)

This outcome measure is only applicable for the oral semaglutide treatment arms (3 mg, 7 mg and 14 mg). Number of participants who measured with anti-semaglutide neutralising antibodies cross reacting with native GLP-1 anytime during post-baseline visits (weeks 0-83) are presented. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Weeks 0-83

InterventionParticipants (Count of Participants)
Oral Semaglutide 3 mg0
Oral Semaglutide 7 mg0
Oral Semaglutide 14 mg0

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Change in Eye Examination Category

Participants with eye examination (fundoscopy) findings, normal, abnormal NCS and abnormal CS at baseline (week -2), week 52 and week 78 are presented. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week -2, week 52, week 78

InterventionParticipants (Count of Participants)
Left eye (week -2)71931138Left eye (week -2)71931139Left eye (week -2)71931140Left eye (week -2)71931141Left eye (week 52)71931138Left eye (week 52)71931139Left eye (week 52)71931140Left eye (week 52)71931141Left eye (week 78)71931138Left eye (week 78)71931140Left eye (week 78)71931139Left eye (week 78)71931141Right eye (week -2)71931138Right eye (week -2)71931139Right eye (week -2)71931140Right eye (week -2)71931141Right eye (week 52)71931138Right eye (week 52)71931139Right eye (week 52)71931140Right eye (week 52)71931141Right eye (week 78)71931138Right eye (week 78)71931139Right eye (week 78)71931140Right eye (week 78)71931141
Abnormal CSNormalAbnormal NCS
Oral Semaglutide 3 mg302
Oral Semaglutide 7 mg299
Oral Semaglutide 14 mg305
Oral Semaglutide 3 mg130
Oral Semaglutide 7 mg138
Oral Semaglutide 14 mg129
Sitagliptin 100 mg137
Oral Semaglutide 3 mg27
Oral Semaglutide 7 mg18
Sitagliptin 100 mg29
Oral Semaglutide 3 mg249
Oral Semaglutide 7 mg253
Oral Semaglutide 14 mg270
Sitagliptin 100 mg252
Oral Semaglutide 3 mg119
Oral Semaglutide 7 mg113
Oral Semaglutide 14 mg101
Sitagliptin 100 mg126
Oral Semaglutide 3 mg25
Oral Semaglutide 7 mg22
Oral Semaglutide 14 mg20
Oral Semaglutide 3 mg261
Oral Semaglutide 14 mg273
Sitagliptin 100 mg287
Oral Semaglutide 3 mg135
Oral Semaglutide 7 mg141
Oral Semaglutide 14 mg130
Sitagliptin 100 mg113
Oral Semaglutide 3 mg21
Oral Semaglutide 7 mg19
Sitagliptin 100 mg31
Oral Semaglutide 3 mg309
Oral Semaglutide 7 mg298
Oral Semaglutide 14 mg308
Sitagliptin 100 mg297
Oral Semaglutide 3 mg126
Oral Semaglutide 7 mg139
Oral Semaglutide 14 mg126
Sitagliptin 100 mg138
Oral Semaglutide 7 mg17
Oral Semaglutide 14 mg23
Sitagliptin 100 mg28
Oral Semaglutide 3 mg247
Oral Semaglutide 7 mg256
Oral Semaglutide 14 mg271
Sitagliptin 100 mg255
Oral Semaglutide 3 mg122
Oral Semaglutide 7 mg112
Oral Semaglutide 14 mg103
Sitagliptin 100 mg123
Oral Semaglutide 3 mg24
Oral Semaglutide 7 mg20
Oral Semaglutide 14 mg17
Sitagliptin 100 mg27
Oral Semaglutide 3 mg258
Oral Semaglutide 7 mg255
Oral Semaglutide 14 mg275
Sitagliptin 100 mg279
Oral Semaglutide 3 mg136
Oral Semaglutide 7 mg146
Oral Semaglutide 14 mg128
Sitagliptin 100 mg122
Oral Semaglutide 3 mg23
Oral Semaglutide 7 mg14
Sitagliptin 100 mg30

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Anti-semaglutide Binding Antibody Levels

This outcome measure is only applicable for the oral semaglutide treatment arms (3 mg, 7 mg and 14 mg). It is based on the data from participants who were measured with anti-semaglutide antibodies anytime during post-baseline visits (weeks 0-83). Results are presented as percentage of bound radioactivity-labelled semaglutide /total added radioactivity-labelled semaglutide (%B/T). Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Weeks 0-83

Intervention%B/T (Mean)
Week 8
Oral Semaglutide 3 mg1.93

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Anti-semaglutide Binding Antibody Levels

This outcome measure is only applicable for the oral semaglutide treatment arms (3 mg, 7 mg and 14 mg). It is based on the data from participants who were measured with anti-semaglutide antibodies anytime during post-baseline visits (weeks 0-83). Results are presented as percentage of bound radioactivity-labelled semaglutide /total added radioactivity-labelled semaglutide (%B/T). Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Weeks 0-83

Intervention%B/T (Mean)
Week 14Week 26
Oral Semaglutide 7 mg3.282.39

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Anti-semaglutide Binding Antibody Levels

This outcome measure is only applicable for the oral semaglutide treatment arms (3 mg, 7 mg and 14 mg). It is based on the data from participants who were measured with anti-semaglutide antibodies anytime during post-baseline visits (weeks 0-83). Results are presented as percentage of bound radioactivity-labelled semaglutide /total added radioactivity-labelled semaglutide (%B/T). Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Weeks 0-83

Intervention%B/T (Mean)
Week 4Week 26Week 38
Oral Semaglutide 14 mg9.822.052.24

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Change in Amylase (Ratio to Baseline)

Change from baseline (week 0) in amylase (units/litre (U/L)) at weeks 26, 52 and 78 is presented as ratio to baseline. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionRatio (Geometric Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg1.141.111.09
Oral Semaglutide 3 mg1.031.031.02
Oral Semaglutide 7 mg1.071.091.09
Sitagliptin 100 mg1.081.081.08

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Change in BMI

Change from baseline (week 0) in body mass index (BMI) was evaluated at weeks 26, 52 and 78. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionKg/m^2 (Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg-1.1-1.2-1.1
Oral Semaglutide 3 mg-0.4-0.6-0.7
Oral Semaglutide 7 mg-0.8-0.9-1.0
Sitagliptin 100 mg-0.2-0.3-0.4

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Change in Body Weight (%)

Relative change from baseline (week 0) in body weight (kg) was evaluated at weeks 26, 52 and 78. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionPercentage change (Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg-3.44-3.83-3.47
Oral Semaglutide 3 mg-1.23-1.65-1.87
Oral Semaglutide 7 mg-2.36-2.63-2.92
Sitagliptin 100 mg-0.64-0.76-0.99

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Change in Body Weight (kg): Weeks 52 and 78

Change from baseline (week 0) in body weight was evaluated at weeks 52 and 78. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 52, week 78

,,,
InterventionKg (Mean)
Week 52Week 78
Oral Semaglutide 14 mg-3.5-3.2
Oral Semaglutide 3 mg-1.6-1.8
Oral Semaglutide 7 mg-2.5-2.8
Sitagliptin 100 mg-0.7-1.0

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Change in Body Weight: Week 26

Change from baseline (week 0) in body weight was evaluated at week 26. The endpoint was evaluated based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. The endpoint was also evaluated based on the data from the on-treatment without rescue medication observation period, which was the time period when a participant was on treatment with trial product, excluding any period after initiation of rescue medication and/or premature trial product discontinuation. (NCT02607865)
Timeframe: Week 0, week 26

,,,
InterventionKg (Mean)
In-trialon-treatment without rescue medication
Oral Semaglutide 14 mg-3.1-3.2
Oral Semaglutide 3 mg-1.2-1.2
Oral Semaglutide 7 mg-2.2-2.2
Sitagliptin 100 mg-0.6-0.6

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Change in CoEQ: Scores From the 4 Domains and the 19 Items

Change from baseline (week 0) in Control of Eating Questionnaire (CoEQ) was evaluated at weeks (wk) 26, 52 and 78. The CoEQ comprised 19 items to assess the intensity and type of food cravings, as well as subjective sensation of appetite and mood, with the 4 domains: 'craving control' (items 9-12, 19), 'positive mood' (items 5-8), 'craving for savoury' (items 4, 16-18) and 'craving for sweet' (items 3, 13-15). The 19 items were scored on an 11-point graded response scale ranging from 10 to 0, with items relating to each of the 4 domains being averaged to create a final score. A low score in the domains 'craving for sweet and 'craving for savoury' represents a low level of craving; whereas a high score in the domains 'craving control' and 'positive mood' represents good control and a good mood, respectively. Results are based on the data from the in-trial observation period. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionScore on a scale (Mean)
1) Feeling of hunger (wk 26)1) Feeling of hunger (wk 52)1) Feeling of hunger (wk 78)2) Feeling of fullness (wk 26)2) Feeling of fullness (wk 52)2) Feeling of fullness (wk 78)3) Desire to eat sweet foods (wk 26)3) Desire to eat sweet foods (wk 52)3) Desire to eat sweet foods (wk 78)4) Desire to eat savoury foods (wk 26)4) Desire to eat savoury foods (wk 52)4) Desire to eat savoury foods (wk 78)5) Feeling of happiness (wk 26)5) Feeling of happiness (wk 52)5) Feeling of happiness (wk 78)6) Feeling of anxiousness (wk 26)6) Feeling of anxiousness (wk 52)6) Feeling of anxiousness (wk 78)7) Feeling of alertness (wk 26)7) Feeling of alertness (wk 52)7) Feeling of alertness (wk 78)8) Feeling of contentment (wk 26)8) Feeling of contentment (wk 52)8) Feeling of contentment (wk 78)9) Food cravings during last 7 days (wk 26)9) Food cravings during last 7 days (wk 52)9) Food cravings during last 7 days (wk 78)10) Strength of food cravings (wk 26)10) Strength of food cravings (wk 52)10) Strength of food cravings (wk 78)11) Difficulty to resist food cravings (wk 26)11) Difficulty to resist food cravings (wk 52)11) Difficulty to resist food cravings (wk 78)12) Eating in response to food cravings (wk 26)12) Eating in response to food cravings (wk 52)12) Eating in response to food cravings (wk 78)13) Cravings for chocolate (wk 26)13) Cravings for chocolate (wk 52)13) Cravings for chocolate (wk 78)14) Cravings for other sweet foods (wk 26)14) Cravings for other sweet foods (wk 52)14) Cravings for other sweet foods (wk 78)15) Cravings for fruit or fruit juice (wk 26)15) Cravings for fruit or fruit juice (wk 52)15) Cravings for fruit or fruit juice (wk 78)16) Cravings for dairy foods (wk 26)16) Cravings for dairy foods (wk 52)16) Cravings for dairy foods (wk 78)17) Cravings for starchy foods (wk 26)17) Cravings for starchy foods (wk 52)17) Cravings for starchy foods (wk 78)18) Cravings for savoury foods (wk 26)18) Cravings for savoury foods (wk 52)18) Cravings for savoury foods (wk 78)19) Difficulty to control eating in general(wk 26)19) Difficulty to control eating in general(wk 52)19) Difficulty to control eating in general(wk 78)Craving control: items 9-12, 19 (wk 26)Craving control: items 9-12, 19 (wk 52)Craving control: items 9-12, 19 (wk 78)Positive mood: items 5-8 (wk 26)Positive mood: items 5-8 (wk 52)Positive mood: items 5-8 (wk 78)Craving for savoury: items 4, 16-18 (wk 26)Craving for savoury: items 4, 16-18 (wk 52)Craving for savoury: items 4, 16-18 (wk 78)Craving for sweet: items 3, 13-15 (wk 26)Craving for sweet: items 3, 13-15 (wk 52)Craving for sweet: items 3, 13-15 (wk 78)
Oral Semaglutide 14 mg-0.54-0.35-0.360.150.220.09-0.47-0.31-0.45-0.30-0.44-0.390.040.090.040.20-0.06-0.12-0.06-0.050.040.180.130.17-0.37-0.25-0.38-0.25-0.21-0.32-0.46-0.42-0.24-0.17-0.25-0.17-0.140.060.06-0.36-0.31-0.40-0.09-0.22-0.02-0.37-0.41-0.45-0.49-0.62-0.61-0.49-0.56-0.48-0.49-0.56-0.540.350.340.33-0.010.050.09-0.41-0.51-0.48-0.26-0.19-0.20
Oral Semaglutide 3 mg-0.41-0.28-0.31-0.08-0.02-0.03-0.41-0.31-0.38-0.27-0.27-0.390.010.09-0.050.02-0.050.050.110.010.100.050.04-0.04-0.59-0.40-0.47-0.50-0.23-0.20-0.460.00-0.04-0.40-0.04-0.02-0.27-0.28-0.08-0.33-0.33-0.20-0.20-0.40-0.14-0.23-0.42-0.30-0.42-0.54-0.44-0.41-0.41-0.27-0.47-0.32-0.400.490.200.220.040.04-0.01-0.33-0.41-0.35-0.30-0.33-0.20
Oral Semaglutide 7 mg-0.37-0.23-0.22-0.08-0.07-0.09-0.54-0.31-0.42-0.16-0.21-0.390.030.04-0.08-0.18-0.160.120.03-0.14-0.040.040.08-0.03-0.41-0.30-0.28-0.33-0.14-0.28-0.38-0.23-0.32-0.15-0.110.01-0.030.030.00-0.31-0.34-0.14-0.03-0.01-0.11-0.20-0.30-0.20-0.24-0.35-0.32-0.16-0.20-0.16-0.69-0.59-0.590.390.270.290.070.03-0.07-0.19-0.27-0.26-0.23-0.15-0.16
Sitagliptin 100 mg-0.18-0.25-0.220.150.270.26-0.33-0.45-0.49-0.35-0.33-0.420.130.140.02-0.210.17-0.010.05-0.05-0.010.180.200.17-0.46-0.21-0.33-0.35-0.30-0.38-0.17-0.26-0.22-0.27-0.17-0.25-0.150.030.06-0.33-0.09-0.22-0.07-0.08-0.33-0.270.04-0.20-0.42-0.28-0.36-0.40-0.37-0.34-0.51-0.51-0.510.350.290.340.150.030.05-0.36-0.24-0.33-0.22-0.15-0.24

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Participants Who Achieve Weight Loss ≥5% (Yes/no)

Participants who achieved weight loss more than or equal to 5% of their baseline body weight (yes/no) at weeks 26, 52 and 78 are presented. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 26, week 52, week 78

InterventionParticipants (Count of Participants)
Week 2671931138Week 2671931139Week 2671931140Week 2671931141Week 5271931138Week 5271931139Week 5271931141Week 5271931140Week 7871931138Week 7871931139Week 7871931140Week 7871931141
YesNo
Oral Semaglutide 3 mg53
Oral Semaglutide 7 mg81
Oral Semaglutide 14 mg131
Sitagliptin 100 mg45
Oral Semaglutide 3 mg385
Oral Semaglutide 7 mg359
Oral Semaglutide 14 mg308
Sitagliptin 100 mg402
Oral Semaglutide 3 mg66
Oral Semaglutide 7 mg118
Oral Semaglutide 14 mg147
Sitagliptin 100 mg50
Oral Semaglutide 3 mg362
Oral Semaglutide 7 mg315
Oral Semaglutide 14 mg288
Sitagliptin 100 mg387
Oral Semaglutide 3 mg83
Oral Semaglutide 7 mg115
Oral Semaglutide 14 mg139
Sitagliptin 100 mg59
Oral Semaglutide 3 mg342
Oral Semaglutide 7 mg310
Oral Semaglutide 14 mg289
Sitagliptin 100 mg384

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Participants Who Achieve Weight Loss ≥10% (Yes/no)

Participants who achieved weight loss more than or equal to 10% of their baseline body weight (yes/no) at weeks 26, 52 and 78 are presented. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 26, week 52, week 78

InterventionParticipants (Count of Participants)
Week 2671931141Week 2671931138Week 2671931139Week 2671931140Week 5271931139Week 5271931138Week 5271931140Week 5271931141Week 7871931138Week 7871931139Week 7871931140Week 7871931141
YesNo
Oral Semaglutide 3 mg5
Oral Semaglutide 7 mg23
Oral Semaglutide 14 mg29
Sitagliptin 100 mg8
Oral Semaglutide 3 mg433
Oral Semaglutide 7 mg417
Oral Semaglutide 14 mg410
Sitagliptin 100 mg439
Oral Semaglutide 3 mg13
Oral Semaglutide 7 mg31
Oral Semaglutide 14 mg48
Sitagliptin 100 mg11
Oral Semaglutide 3 mg415
Oral Semaglutide 7 mg402
Oral Semaglutide 14 mg387
Oral Semaglutide 3 mg12
Oral Semaglutide 7 mg43
Oral Semaglutide 14 mg46
Sitagliptin 100 mg17
Oral Semaglutide 3 mg413
Oral Semaglutide 7 mg382
Oral Semaglutide 14 mg382
Sitagliptin 100 mg426

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Participants Who Achieve HbA1c Reduction ≥1% (10.9 mmol/Mol) and Weight Loss ≥3% (Yes/no)

Participants who achieved HbA1c reduction more than or equal to 1% of their baseline HbA1c and weight loss of more than or equal to 3% of their baseline body weight (yes/no) at weeks 26, 52 and 78 are presented. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 26, week 52, week 78

InterventionParticipants (Count of Participants)
Week 2671931140Week 2671931141Week 2671931138Week 2671931139Week 5271931138Week 5271931139Week 5271931140Week 5271931141Week 7871931138Week 7871931139Week 7871931140Week 7871931141
YesNo
Oral Semaglutide 3 mg55
Oral Semaglutide 7 mg117
Oral Semaglutide 14 mg166
Sitagliptin 100 mg43
Oral Semaglutide 3 mg380
Oral Semaglutide 7 mg321
Sitagliptin 100 mg403
Oral Semaglutide 3 mg73
Oral Semaglutide 7 mg106
Oral Semaglutide 14 mg164
Sitagliptin 100 mg51
Oral Semaglutide 3 mg354
Oral Semaglutide 7 mg325
Oral Semaglutide 14 mg270
Sitagliptin 100 mg385
Oral Semaglutide 3 mg76
Oral Semaglutide 7 mg113
Oral Semaglutide 14 mg149
Sitagliptin 100 mg60
Oral Semaglutide 3 mg345
Oral Semaglutide 7 mg311
Oral Semaglutide 14 mg276
Sitagliptin 100 mg379

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Participants Who Achieve HbA1c ≤6.5% (48 mmol/Mol) AACE Target (Yes/no)

Participants who achieved HbA1c less than or equal to 6.5% (American Association of Clinical Endocrinologists (AACE) target) (yes/no) at weeks 26, 52 and 78 are presented. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 26, week 52, week 78

InterventionParticipants (Count of Participants)
Week 2671931138Week 2671931140Week 2671931139Week 2671931141Week 5271931138Week 5271931139Week 5271931141Week 5271931140Week 7871931138Week 7871931139Week 7871931140Week 7871931141
YesNo
Oral Semaglutide 3 mg55
Oral Semaglutide 7 mg116
Oral Semaglutide 14 mg161
Sitagliptin 100 mg61
Oral Semaglutide 3 mg380
Oral Semaglutide 7 mg322
Oral Semaglutide 14 mg275
Sitagliptin 100 mg385
Oral Semaglutide 7 mg99
Oral Semaglutide 14 mg146
Sitagliptin 100 mg59
Oral Semaglutide 3 mg372
Oral Semaglutide 7 mg332
Oral Semaglutide 14 mg288
Sitagliptin 100 mg377
Oral Semaglutide 3 mg49
Oral Semaglutide 7 mg100
Oral Semaglutide 14 mg129
Sitagliptin 100 mg60
Oral Semaglutide 7 mg324
Oral Semaglutide 14 mg296
Sitagliptin 100 mg379

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Participants Who Achieve HbA1c <7.0% (53 mmol/Mol) ADA Target (Yes/no)

Participants who achieved HbA1c <7.0% (American Diabetes Association (ADA) target) (yes/no), was evaluated at weeks 26, 52 and 78. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 26, week 52, week 78

InterventionParticipants (Count of Participants)
Week 2671931138Week 2671931139Week 2671931140Week 2671931141Week 5271931138Week 5271931139Week 5271931140Week 5271931141Week 7871931138Week 7871931139Week 7871931140Week 7871931141
YesNo
Oral Semaglutide 3 mg116
Oral Semaglutide 7 mg192
Oral Semaglutide 14 mg246
Sitagliptin 100 mg144
Oral Semaglutide 3 mg319
Oral Semaglutide 7 mg246
Oral Semaglutide 14 mg190
Sitagliptin 100 mg302
Oral Semaglutide 3 mg113
Oral Semaglutide 7 mg168
Oral Semaglutide 14 mg238
Sitagliptin 100 mg138
Oral Semaglutide 3 mg314
Oral Semaglutide 7 mg263
Oral Semaglutide 14 mg196
Sitagliptin 100 mg298
Oral Semaglutide 7 mg165
Oral Semaglutide 14 mg191
Sitagliptin 100 mg129
Oral Semaglutide 3 mg308
Oral Semaglutide 7 mg259
Oral Semaglutide 14 mg234
Sitagliptin 100 mg310

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Time to Additional Anti-diabetic Medication

Presented results are the number of participants who had taken additional anti-diabetic medication anytime during the periods, from week 0 to week 26, week 0 to week 52 and week 0 to week 78. Additional anti-diabetic medication was defined as any new anti-diabetic medication used for more than 21 days with the initiation at or after randomisation (week 0) and before (planned) end-of-treatment (week 78), and/or intensification of anti-diabetic medication (a more than 20% increase in dose relative to baseline) for more than 21 days with the intensification at or after randomisation and before (planned) end-of-treatment. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Weeks 0-78

,,,
InterventionParticipants (Count of Participants)
Week 0 to week 26Week 0 to week 52Week 0 to week 78
Oral Semaglutide 14 mg155175
Oral Semaglutide 3 mg33137179
Oral Semaglutide 7 mg2086119
Sitagliptin 100 mg20111148

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Semaglutide Plasma Concentration in a Subset of the Participants for Population PK Analyses

This outcome measure is only applicable for the oral semaglutide treatment arms (3 mg, 7 mg and 14 mg). Semaglutide plasma concentrations for participants in the pharmacokinetic (PK) subpopulation are presented. The PK subpopulation consisted of participants from sites in Germany, Japan and the United States receiving oral semaglutide (3 mg, 7 mg or 14 mg). Results are based on the data from the on-treatment observation period and follow-up period. The on-treatment observation period was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02607865)
Timeframe: Weeks 0-83

,,
Interventionnmol/L (Geometric Mean)
Week 0Week 4Week 8Week 14Week 26Week 38Week 52Week 78Week 83
Oral Semaglutide 14 mg0.41.64.29.48.68.68.28.90.4
Oral Semaglutide 3 mg0.41.51.51.41.31.41.41.30.4
Oral Semaglutide 7 mg0.41.54.14.03.73.53.53.50.4

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Change in VLDL Cholesterol (Ratio to Baseline)

Change from baseline (week 0) in very-low-density lipoprotein (VLDL) cholesterol (mmol/L) at weeks 26, 52 and 78 is presented as ratio to baseline. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionRatio of VLDL cholesterol (Geometric Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg0.910.930.91
Oral Semaglutide 3 mg0.991.000.95
Oral Semaglutide 7 mg0.960.980.94
Sitagliptin 100 mg0.970.980.94

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Change in Waist Circumference

Change from baseline (week 0) in waist circumference was evaluated at weeks 26, 52 and 78. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
Interventioncm (Mean)
Week 26Week 52Week 78
Oral Semaglutide 14 mg-2.3-2.6-2.4
Oral Semaglutide 3 mg-0.7-1.3-1.2
Oral Semaglutide 7 mg-1.8-2.3-2.4
Sitagliptin 100 mg-0.6-0.5-0.7

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Change in ECG Evaluation

Change from baseline (week 0) in electrocardiogram (ECG) was evaluated at weeks 26, 52 and 78. Change from baseline results are presented as shift in findings (normal, abnormal and not clinically significant (NCS) and abnormal and clinically significant (CS)) from week 0 to week 26, 52 and 78. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02607865)
Timeframe: Week 0, week 26, week 52, week 78

,,,
InterventionParticipants (Count of Participants)
Normal (week 0) to normal (week 26)Normal (week 0) to abnormal NCS (week 26)Normal (week 0) to abnormal CS (week 26)Abnormal (week 0) NCS to normal (week 26)Abnormal (week 0) NCS to abnormal NCS (week 26)Abnormal (week 0) NCS to abnormal CS (week 26)Abnormal (week 0) CS to normal (week 26)Abnormal (week 0) CS to abnormal NCS (week 26)Abnormal (week 0) CS to abnormal CS (week 26)Normal (week 0) to normal (week 52)Normal (week 0) to abnormal NCS (week 52)Normal (week 0) to abnormal CS (week 52)Abnormal (week 0) NCS to normal (week 52)Abnormal (week 0) NCS to abnormal NCS (week 52)Abnormal (week 0) NCS to abnormal CS (week 52)Abnormal (week 0) CS to normal (week 52)Abnormal (week 0) CS to abnormal NCS (week 52)Abnormal (week 0) CS to abnormal CS (week 52)Normal (week 0) to normal (week 78)Normal (week 0) to abnormal NCS (week 78)Normal (week 0) to abnormal CS (week 78)Abnormal (week 0) NCS to normal (week 78)Abnormal (week 0) NCS to abnormal NCS (week 78)Abnormal (week 0) NCS to abnormal CS (week 78)Abnormal (week 0) CS to normal (week 78)Abnormal (week 0) CS to abnormal NCS (week 78)Abnormal (week 0) CS to abnormal CS (week 78)
Oral Semaglutide 14 mg230240421331036219331561180207219311511143135
Oral Semaglutide 3 mg211384411324134196471401314134196413391315044
Oral Semaglutide 7 mg214425441281122218370491231131201432451251321
Sitagliptin 100 mg204414401433324204404481282126208401471332324

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Percent Change in Weight

(NCT02623998)
Timeframe: Baseline and 12 weeks after randomization

Intervention% change (Mean)
Intervention-2.1
Standard Care-1.4

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Number of Participants With Severe Hypoglycemic Episodes

(NCT02623998)
Timeframe: 64 weeks of follow-up

InterventionParticipants (Count of Participants)
Intervention0
Standard Care0

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Number of Participants Achieving Drug-free Diabetes Remission

Diabetes remission is defined as absence of hyperglycemia relapse (NCT02623998)
Timeframe: 24 weeks after randomization

InterventionParticipants (Count of Participants)
Intervention8
Standard Care4

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Change in Waist Circumference

(NCT02623998)
Timeframe: Baseline and 12 weeks after randomization

Interventioncm (Mean)
Intervention-2.3
Standard Care-1.8

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Number of Participants With Drug-free Normal Glucose Tolerance

Normal glucose tolerance is defined as a FPG<6.1 mmol/L and a 2-hour plasma glucose <7.8 mmol/L on a 75 g oral glucose tolerance test (NCT02623998)
Timeframe: 24 weeks after randomization

InterventionParticipants (Count of Participants)
Intervention3
Standard Care1

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Number of Participants With Hyperglycemia Relapse in the Experimental Group Compared to the Control Group

"Hyperglycemia relapse for primary outcome was defined as any one of:~Capillary glucose >10 mmol/L on >/=50% of readings over 1 week;~HbA1C >/=6.5%;~use of diabetes drugs;~fasting plasma glucose >/= 7.0 mmol/L;~2-hour postprandial plasma glucose >/=11.1 mmol/L on an oral glucose tolerance test." (NCT02623998)
Timeframe: 64 weeks of follow-up

InterventionParticipants (Count of Participants)
Intervention41
Standard Care48

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Arterial tPA

Measured using an ELISA. (NCT02639637)
Timeframe: Measured at baseline (time 0) of each study day prior to the infusion of neuropeptide Y. Study days were separated by five weeks, a four-week washout and one-week treatment period.

Interventionng/mL (Mean)
Sitagliptin (Diabetics and Controls)0.047
Placebo (Diabetics and Controls)0.115

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Mean Arterial Pressure

(NCT02639637)
Timeframe: Measured at baseline (time 0) of each study day prior to the infusion of neuropeptide Y. Study days were separated by five weeks, a four-week washout and one-week treatment period.

Interventionmm Hg (Mean)
Sitagliptin (Diabetics and Controls)79.3
Placebo (Diabetics and Controls)81.4
Sitagliptin and Valsartan (Controls Only)75.4
Placebo and Valsartan (Controls Only)74.0

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Low Frequency Variability of Blood Pressure Activity

Measured using the VITAL-GARD 450c monitor Ivy Biomedical Systems, Branford, CT, USA) (NCT02639637)
Timeframe: Measured at baseline (time 0) of each study day prior to the infusion of neuropeptide Y. Study days were separated by five weeks, a four-week washout and one-week treatment period.

Interventionmm Hg2 (Mean)
Sitagliptin (Diabetics and Controls)5.16
Placebo (Diabetics and Controls)5.60
Sitagliptin and Valsartan (Controls Only)6.05
Placebo and Valsartan (Controls Only)4.27

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Insulin

Plasma insulin measured by radioimmunoassay. (NCT02639637)
Timeframe: Measured at baseline (time 0) of each study day prior to the infusion of neuropeptide Y. Study days 1 and 2 were separated by five weeks, a four-week washout and one-week treatment period.

InterventionmicroU/mL (Mean)
Sitagliptin (Diabetics and Controls)16.2
Placebo (Diabetics and Controls)19.6

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Heart Rate

(NCT02639637)
Timeframe: Measured at baseline (time 0) of each study day prior to the infusion of neuropeptide Y. Study days were separated by five weeks, a four-week washout and one-week treatment period.

Interventionbeats per minute (Mean)
Sitagliptin (Diabetics and Controls)67.4
Placebo (Diabetics and Controls)66.0
Sitagliptin and Valsartan (Controls Only)59.8
Placebo and Valsartan (Controls Only)60.2

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Glucose

Glucose was measured by the glucose oxidase method using a YSI glucose analyzer (NCT02639637)
Timeframe: Measured at baseline (time 0) of each study day prior to the infusion of neuropeptide Y. Study days were separated by five weeks, a four-week washout and one-week treatment period.

Interventionmg/dL (Mean)
Sitagliptin (Diabetics and Controls)94.3
Placebo (Diabetics and Controls)100.3
Sitagliptin and Valsartan (Controls Only)85.7
Placebo and Valsartan (Controls Only)88.3

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Forearm Blood Flow

Forearm blood flow measured by strain gauge plethysmography in response to 1.0 nmol/min neuropeptide Y, the highest dose that all received. (NCT02639637)
Timeframe: FBF measured after 5 min of the 1 nmol/min dose of neuropeptide Y on study days 1 and 2. Study days 1 and two were separated by five weeks.

InterventionmL/min/100 mL (Mean)
Sitagliptin and Enalaprilat (Diabetics and Controls)1.72
Placebo and Enalaprilat (Diabetics and Controls)2.29
Sitagliptin and Valsartan (Controls Only)1.17
Placebo and Valsartan (Controls Only)1.63

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DPP4 Activity

DPP4 activity was measured by detection of cleavage of a colorimetric substrate. (NCT02639637)
Timeframe: Measured at baseline (time 0) of each study day prior to the infusion of neuropeptide Y. Study days were separated by five weeks, a four-week washout and one-week treatment period.

Interventionnmol/ml/min (Mean)
Sitagliptin (Diabetics and Controls)10.97
Placebo (Diabetics and Controls)21.22
Sitagliptin and Valsartan (Controls Only)17.46
Placebo and Valsartan (Controls Only)32.55

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Venous Norepinephrine

Venous norepinephrine concentration measured by high-performance liquid chromatography (NCT02639637)
Timeframe: Measured at baseline (time 0) prior to the infusion of neuropeptide Y on each study day. Study days 1 and 2 were separated by five weeks.

Interventionpg/mL (Mean)
Sitagliptin + Enalaprilat (Diabetics and Controls)250.6
Placebo + Enalaprilat (Diabetics and Controls)178.3
Sitagliptin and Valsartan (Controls Only)192.6
Placebo and Valsartan (Controls Only)173.1

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Arterial Norepinephrine

Arterial norepinephrine concentration measured by high-performance liquid chromatography. (NCT02639637)
Timeframe: Measured at baseline (time 0) prior to the infusion of neuropeptide Y on each study day. Study days 1 and 2 were separated by five weeks.

Interventionpg/mL (Mean)
Sitagliptin + Enalaprilat (Diabetics and Controls)211.8
Placebo + Enalaprilat (Diabetics and Controls)174.7
Sitagliptin and Valsartan (Controls Only)151.8
Placebo and Valsartan (Controls Only)125.5

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ACE Activity

ACE activity was measured using a commercially available assay (Olympus AU400/AU600, Alpco Diagnotics, Salem, NH.) The lower level of detection was 15 U/L and values below the level of detection were reported at half the level of detection. (NCT02639637)
Timeframe: Measured at baseline (time 0) of each study day prior to the infusion of neuropeptide Y. Study days were separated by five weeks, a four-week washout and one-week treatment period.

InterventionU/L (Mean)
Sitagliptin + Enalaprilat (Diabetics and Controls)7.5
Placebo + Enalaprilat (Diabetics and Controls)7.5

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Venous tPA

Measured using an ELISA. This was measured in a few subjects. After it was determined that there was no change in net t-PA release it was not measured in the remainder. (NCT02639637)
Timeframe: Measured at baseline (time 0) of each study day prior to the infusion of neuropeptide Y. Study days were separated by five weeks, a four-week washout and one-week treatment period.

Interventionng/mL (Mean)
Sitagliptin (Diabetics and Controls)0.030
Placebo (Diabetics and Controls)0.110

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NPY Metabolites

"NPY (3-36) concentration measured by micro ultra-hgih pressure liquid chromatography tandem mass spectrometry.~NPY (3-36) is the degradation product of NPY by dipeptidyl peptidase 4. It was measured only in the diabetics studied." (NCT02639637)
Timeframe: Measured after 5 min infusion of the 1.0 nmol/min dose of neuropeptide Y on study days 1 and 2. Study days 1 and 2 were separated by five weeks.

Interventionpmol/L (Mean)
Sitagliptin (Diabetics)749
Placebo (Diabetics)1206

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Change From Baseline in Non-HDL-C at Week 12

"Non-HDL-C is the measure of bad cholesterol in the blood, including triglycerides and LDL-C, so a negative change means improvement. The equation for Non-HDL-C = LDL-C + (triglycerides/5)." (NCT02647320)
Timeframe: Baseline, Week 12

InterventionPercent change in Non-HDL-C (Mean)
DS-8500a 25mg-8.9
DS-8500a 50 mg-2.5
DS-8500a 75 mg-2.9
Sitagliptin 100 mg-4.7
Placebo-2.5

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Change From Baseline in Area-Under-the Curve 0-3 Hours (AUC0-3h) of Plasma Glucose (PG) in Response to the Mixed Meal Tolerance Test (MMTT) at Week 4

"The MMTT requires a participant to drink a mixed meal, such as Boost or Ensure, that contains protein, carbohydrates, and fat. The goal of the test is to find out how much insulin the pancreas makes in response to food by measuring the level of glucose in the blood. The lower the level of glucose in the blood during the first three hours after the test (AUC0-3h), the more insulin the body has made in response to the test. This would mean a negative change shows improvement." (NCT02647320)
Timeframe: Baseline, Week 4

Intervention(mg/dL)*hr (Mean)
DS-8500a 25mg-4.32
DS-8500a 50 mg1.36
DS-8500a 75 mg-6.32
Sitagliptin 100 mg-41.61
Placebo-3.97

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Change From Baseline in Total Cholesterol (TC) at Week 12

"Total cholesterol is a measure of the total amount of cholesterol in the blood, including low-density lipoprotein cholesterol (LDL-C) - the bad cholesterol, high-density lipoprotein cholesterol (HDL-C) - the good cholesterol, and triglycerides. The equation to calculate total cholesterol is: LDL + HDL + (triglycerides/5) = total cholesterol." (NCT02647320)
Timeframe: Baseline, Week 12

Interventionpercent change in TC (Mean)
DS-8500a 25mg-5.6
DS-8500a 50 mg-1.7
DS-8500a 75 mg-1.8
Sitagliptin 100 mg-3.6
Placebo-1.7

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Change From Baseline in Cmax of PG in Response to MMTT at Week 12

Cmax measures the highest amount of glucose in the blood, so a negative change means improvement. (NCT02647320)
Timeframe: Baseline, Week 12

Interventionmg/dL (Mean)
DS-8500a 25mg-5.93
DS-8500a 50 mg-1.10
DS-8500a 75 mg-4.43
Sitagliptin 100 mg-28.29
Placebo1.11

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 12

Normal fasting plasma glucose -- or blood sugar -- is between 70 and 100 milligrams per deciliter (mg/dL) for people who do not have diabetes. People with Type 2 diabetes typically have FPG that is too high, so a negative change from baseline means improvement. (NCT02647320)
Timeframe: Baseline, Week 12

Interventionmg/dL (Mean)
DS-8500a 25mg0.0
DS-8500a 50 mg-9.1
DS-8500a 75 mg-5.8
Sitagliptin 100 mg-5.7
Placebo8.1

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 2

Normal fasting plasma glucose -- or blood sugar -- is between 70 and 100 milligrams per deciliter (mg/dL) for people who do not have diabetes. People with Type 2 diabetes typically have FPG that is too high, so a negative change from baseline means improvement. (NCT02647320)
Timeframe: Baseline, Week 2

Interventionmg/dL (Mean)
DS-8500a 25mg4.3
DS-8500a 50 mg-8.1
DS-8500a 75 mg0.0
Sitagliptin 100 mg-16.2
Placebo10.7

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Change From Baseline in Triglycerides at Week 12

Triglycerides are a type of fat found in the blood. The body uses them for energy. Some triglycerides are needed for good health. But high triglycerides might raise the risk of heart disease. Since Type 2 diabetics tend to have high triglycerides, a negative change means improvement. (NCT02647320)
Timeframe: Baseline, Week 12

Interventionpercent change in triglycerides (Mean)
DS-8500a 25mg-12.4
DS-8500a 50 mg-1.9
DS-8500a 75 mg-5.8
Sitagliptin 100 mg-7.0
Placebo-3.0

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 4

Normal fasting plasma glucose -- or blood sugar -- is between 70 and 100 milligrams per deciliter (mg/dL) for people who do not have diabetes. People with Type 2 diabetes typically have FPG that is too high, so a negative change from baseline means improvement. (NCT02647320)
Timeframe: Baseline, Week 4

Interventionmg/dL (Mean)
DS-8500a 25mg0.04
DS-8500a 50 mg-12.7
DS-8500a 75 mg-5.9
Sitagliptin 100 mg-11.1
Placebo2.4

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Change From Baseline in AUC0-3h of PG in Response to the MMTT at Week 12

"The MMTT requires a participant to drink a mixed meal, such as Boost or Ensure, that contains protein, carbohydrates, and fat. The goal of the test is to find out how much insulin the pancreas makes in response to food by measuring the level of glucose in the blood. The lower the level of glucose in the blood during the first three hours after the test (AUC0-3h), the more insulin the body has made in response to the test. This would mean a negative change shows improvement." (NCT02647320)
Timeframe: Baseline, Week 12

Intervention(mg/dL)*hr (Mean)
DS-8500a 25mg-18.77
DS-8500a 50 mg13.81
DS-8500a 75 mg-5.51
Sitagliptin 100 mg-53.40
Placebo-24.16

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Count of Participants With HbA1c Less Than 7.0% at Week 12

HbA1C less than 7% is the success goal for many Type 2 diabetics. (NCT02647320)
Timeframe: Week 12

InterventionParticipants (Count of Participants)
DS-8500a 25mg6
DS-8500a 50 mg8
DS-8500a 75 mg15
Sitagliptin 100 mg28
Placebo10

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Change From Baseline in Glycated Hemoglobin (HbA1c) at Week 12

Glycated hemoglobin is a form of hemoglobin that is measured primarily to identify the three-month average glucose concentration in the blood. Target HbA1c for Type 2 diabetics was less than 7% at the time of this trial. Negative scores show improvement from baseline. (NCT02647320)
Timeframe: Baseline, Week 12

Interventionpercent of HbA1c (Mean)
DS-8500a 25mg-0.24
DS-8500a 50 mg-0.16
DS-8500a 75 mg-0.35
Sitagliptin 100 mg-0.66
Placebo-0.23

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Change From Baseline in HDL-C at Week 12

"HDL-C is known as the good cholesterol, so a higher score (positive change) means improvement." (NCT02647320)
Timeframe: Baseline, Week 12

Interventionpercent change in HCL-C (Mean)
DS-8500a 25mg3.0
DS-8500a 50 mg1.1
DS-8500a 75 mg2.2
Sitagliptin 100 mg1.1
Placebo1.2

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Change From Baseline in LDL-C at Week 12

"LDL-C is known as the bad cholesterol, so a lower score (negative change) means improvement." (NCT02647320)
Timeframe: Baseline, Week 12

Interventionpercent change in LDL-C (Mean)
DS-8500a 25mg-6.7
DS-8500a 50 mg2.8
DS-8500a 75 mg-0.1
Sitagliptin 100 mg-2.4
Placebo0.9

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Change From Baseline in Maximum Concentration (Cmax) of PG in Response to MMTT at Week 4

Cmax measures the highest amount of glucose in the blood, so a negative change means improvement. (NCT02647320)
Timeframe: Baseline, Week 4

Interventionmg/dL (Mean)
DS-8500a 25mg-1.92
DS-8500a 50 mg-7.35
DS-8500a 75 mg-3.47
Sitagliptin 100 mg-28.44
Placebo-0.35

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 8

Normal fasting plasma glucose -- or blood sugar -- is between 70 and 100 milligrams per deciliter (mg/dL) for people who do not have diabetes. People with Type 2 diabetes typically have FPG that is too high, so a negative change from baseline means improvement. (NCT02647320)
Timeframe: Baseline, Week 8

Interventionmg/dL (Mean)
DS-8500a 25mg2.3
DS-8500a 50 mg-5.9
DS-8500a 75 mg-7.1
Sitagliptin 100 mg-16.6
Placebo-1.0

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Arginine-stimulated Insulin Secretion With and Without GLP-1 Blockade

The investigators will use the mean increment of insulin secretion rate above baseline in the 30 minutes after Arginine stimulation to integrate insulin secretion, the primary outcome measure, and 2-way ANOVA with and without Sitagliptin and Ex-9/saline at the two factors. (NCT02683187)
Timeframe: 30 minutes

,,,
Interventionpmol/L (Mean)
With GLP-1 BlockadeWithout GLP-1 Blockade
Non-Sitagliptin and Ex-9/Saline (Diabetics)251.2249.2
Non-Sitagliptin and Ex-9/Saline (Non-diabetics)280371.4
Sitagliptin and Ex-9/Saline (Diabetics)243.4319.4
Sitagliptin and Ex-9/Saline (Non-diabetics)320.1318.7

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Percentage of Patients With Grade III-IV Acute GvHD at Day +100

Kaplan-Meier methods will be used to conduct a competing risk analysis. Time until grade III-IV acute GvHD will be calculated from transplant until grade III-IV acute GvHD or death from GvHD. Patients who relapsed or died from causes other than GvHD will be considered a competing risk and calculated from time of transplant until relapse or death. Otherwise, patients will be censored and calculated from transplant until the last known alive date. The cumulative incidence percentage of grade II-IV acute GvHD at day +100 was calculated along with a 95% confidence interval. (NCT02683525)
Timeframe: 100 days from transplant

Interventionpercentage of participants (Number)
Sitagliptin2.7

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Percentage of Patients With Grade II-IV Acute GvHD by Day +100 Following Transplant

Percent of patients and the 95% Confidence interval who did not have Grade II-IV Acute GvHD by 100 days following transplant. Since the study completed the two-phase design, proper inference was used to generate the confidence interval (Koyama and Chen). Only patients who were on the study for at least 100 days post transplant were included in the analysis. (NCT02683525)
Timeframe: up to 100 days

Interventionpercentage of participants (Number)
Sitagliptin94.4

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Number of Unique Patients With Infections by Day +100

Number of unique patients who had each type of infection (i.e., viral, bacterial, fungal, etc.) during the 100 days post transplant. A patient could have more than one type of infection. (NCT02683525)
Timeframe: 100 days from transplant

InterventionParticipants (Count of Participants)
BacterialGram Positive BacteriaOther BacteriaFungalViralCMV
Sitagliptin5111111

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Percentage of Patients With Relapse of the Primary Hematological Malignancy at 1 Year

Kaplan-Meier methods will be used to conduct a competing risk analysis. Time until relapse will be calculated from transplant until relapse or death from relapse. Patients who died from causes other than relapse will be considered a competing risk and calculated from time of transplant until death. Otherwise, patients will be censored and calculated from transplant until the last known alive date. The cumulative incidence percentage of relapse at day +365 was calculated along with a 95% confidence interval. (NCT02683525)
Timeframe: 1 year from transplant

Interventionpercentage of participants (Number)
Sitagliptin25.6

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Percentage of Patients With Grade II-IV Acute GvHD at Day +100

Kaplan-Meier methods will be used to conduct a competing risk analysis. Time until grade II-IV acute GvHD will be calculated from transplant until grade II-IV acute GvHD or death from GvHD. Patients who relapsed or died from causes other than GvHD will be considered a competing risk and calculated from time of transplant until relapse or death. Otherwise, patients will be censored and calculated from transplant until the last known alive date. The cumulative incidence percentage of grade II-IV acute GvHD at day +100 was calculated along with a 95% confidence interval. (NCT02683525)
Timeframe: 100 days from transplant

Interventionpercentage of participants (Number)
Sitagliptin5.5

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Percentage of Patients With Non-relapse Mortality (NRM) at +1 Year

Kaplan-Meier methods will be used to conduct a competing risk analysis. Time until non-relapse death will be calculated from transplant until death. Patients who died from relapse will be considered a competing risk and calculated from time of transplant until death. Otherwise, patients will be censored and calculated from transplant until the last known alive date. The cumulative incidence percentage of non-relapse mortality at day +365 was calculated along with a 95% confidence interval. (NCT02683525)
Timeframe: 1 year from transplant

Interventionpercentage of participants (Number)
Sitagliptin0

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Percentage of Patients Diagnosed With Chronic GvHD at 1 Year

Patients surviving at least 100 days will be evaluable for chronic GvHD. The cumulative incidence of chronic GvHD (total, and mild, moderate, severe) will be described using deaths from causes other than chronic GvHD considered as a competing risk. Kaplan-Meier methods will be used to conduct a competing risk analysis. Time until chronic GvHD will be calculated from transplant until chronic GvHD or death from GvHD. Patients who relapsed or died from causes other than GvHD will be considered a competing risk and calculated from time of transplant until relapse or death. Otherwise, patients will be censored and calculated from transplant until the last known alive date. The cumulative incidence percentage at 1 year will calculated along with a 95% confidence interval. (NCT02683525)
Timeframe: 1 year from transplant

Interventionpercentage of participants (Number)
Sitagliptin37.4

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Percentage of Patients Surviving at +1 Year

Duration of time from the start of treatment to time of death due to any causes. Patients who do not die will be censored on their last known alive date. Kaplan-Meier methods will be used and the median and 95% confidence intervals will be calculated. The cumulative incidence percentage of survival at day +365 was calculated along with a 95% confidence interval. (NCT02683525)
Timeframe: 1 year from transplant

Interventionpercentage of participants (Number)
Sitagliptin94.3

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Median Time to Engraftment of Neutrophils

Time to neutrophil engraftment will be analyzed by the Kaplan-Meier method. The time to engraftment of neutrophils is defined as the time from day 0 to the date of the first of three consecutive days after transplantation during which the absolute neutrophils count (ANC) is at least 0.5 x109/l. Patients who did not have neutrophil engraftment before death will be censored at the date of death. The median and 95% confidence intervals were calculated. (NCT02683525)
Timeframe: up to 1 month

Interventiondays (Median)
Sitagliptin13

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Median Time to Engraftment of Platelets

Time to platelet engraftment will be analyzed by the Kaplan-Meier method. The time to engraftment of platelets is defined as the time from day 0 to the first of seven consecutive Complete Blood Counts (CBCs) obtained on different days after transplantation during which the platelet count is at least 20 x109/l. The CBCs obtained should be at least seven days after the most recent platelet transfusion. The median and 95% confidence intervals were calculated. (NCT02683525)
Timeframe: up to 4 months

Interventiondays (Median)
Sitagliptin15

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Event Rate of Documented Hypoglycemia With Blood Glucose ≤70 mg/dL (≤3.9 mmol/L)

Documented hypoglycemia is defined by a measured (e.g., by fingerstick) plasma glucose concentration ≤70 mg/dL (≤3.9 mmol/L). The event rate was the total number of events divided by follow-up time (participant-years), including multiple events from the same participant. (NCT02738879)
Timeframe: Up to 30 weeks

InterventionEvents/Participant-Years (Number)
Sitagliptin5.05
Placebo6.21

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Event Rate of Documented Symptomatic Hypoglycemia With Blood Glucose <56 mg/dL (≤3.1 mmol/L)

Documented symptomatic hypoglycemia is defined as an event during which typical symptoms of hypoglycemia are accompanied by a measured (e.g., by fingerstick) plasma glucose concentration <56 mg/dL (≤3.1 mmol/L). The event rate was the total number of events divided by follow-up time (participant-years), including multiple events from the same participant. (NCT02738879)
Timeframe: Up to 30 weeks

InterventionEvents/Participant-Years (Number)
Sitagliptin0.17
Placebo0.22

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Event Rate of Documented Symptomatic Hypoglycemia With Blood Glucose ≤70 mg/dL (≤3.9 mmol/L)

Documented symptomatic hypoglycemia is defined as an event during which typical symptoms of hypoglycemia are accompanied by a measured (e.g., by fingerstick) plasma glucose concentration ≤70 mg/dL (≤3.9 mmol/L). The event rate was the total number of events divided by follow-up time (participant-years), including multiple events from the same participant. (NCT02738879)
Timeframe: Up to 30 weeks

InterventionEvents/Participant-Years (Number)
Sitagliptin1.55
Placebo2.12

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Percentage of Participants Who Experienced One or More Adverse Events (AEs)

An AE is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure, that occurs during the course of the study. (NCT02738879)
Timeframe: Up to 32 weeks

InterventionPercentage of participants (Number)
Sitagliptin57.9
Placebo60.0

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Percentage of Participants With A1C Goal <7.0% (<53 mmol/Mol) at Week 30

A1C is blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. (NCT02738879)
Timeframe: Week 30

InterventionPercentage of participants (Number)
Sitagliptin54.2
Placebo35.4

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Percentage of Participants With Documented Hypoglycemia With Blood Glucose <56 mg/dL (≤3.1 mmol/L)

Documented hypoglycemia is defined by a measured (e.g., by fingerstick) plasma glucose concentration <56 mg/dL (≤3.1 mmol/L). (NCT02738879)
Timeframe: Up to 30 weeks

InterventionPercentage of participants (Number)
Sitagliptin12.4
Placebo13.6

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Percentage of Participants With Documented Hypoglycemia With Blood Glucose ≤70 mg/dL (≤3.9 mmol/L)

Documented hypoglycemia is defined by a measured (e.g., by fingerstick) plasma glucose concentration ≤70 mg/dL (≤3.9 mmol/L). (NCT02738879)
Timeframe: Up to 30 weeks

InterventionPercentage of participants (Number)
Sitagliptin66.8
Placebo68.0

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Percentage of Participants With Documented Symptomatic Hypoglycemia With Blood Glucose <56 mg/dL (≤3.1 mmol/L)

Documented symptomatic hypoglycemia is defined as an event during which typical symptoms of hypoglycemia are accompanied by a measured (e.g., by fingerstick) plasma glucose concentration <56 mg/dL (≤3.1 mmol/L). (NCT02738879)
Timeframe: Up to 30 weeks

InterventionPercentage of participants (Number)
Sitagliptin7.6
Placebo8.3

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Percentage of Participants With Events of Documented Symptomatic Hypoglycemia With Blood Glucose ≤70 mg/dL (≤3.9 mmol/L)

Documented symptomatic hypoglycemia is defined as an event during which typical symptoms of hypoglycemia are accompanied by a measured (e.g., by fingerstick) plasma glucose concentration ≤70 mg/dL (≤3.9 mmol/L). The incidence (number of participants with ≥1 event divided by number of participants) of documented symptomatic hypoglycemia was determined. (NCT02738879)
Timeframe: Up to 30 weeks

InterventionPercentage of participants (Number)
Sitagliptin33.5
Placebo37.7

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Percentage of Participants With A1C Goal <7.0% (<53 mmol/Mol at Week 30 and No Documented Hypoglycemia With Blood Glucose ≤70 mg/dL (≤3.9 mmol/L) up to Week 30

A1C is blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. (NCT02738879)
Timeframe: Week 30

InterventionPercentage of participants (Number)
Sitagliptin15.3
Placebo10.0

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Change From Baseline in A1C at Week 30

A1C is blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. Thus, this change from baseline reflects the Week 30 A1C minus the Week 0 A1C. (NCT02738879)
Timeframe: Baseline and Week 30

InterventionPercent A1C (Least Squares Mean)
Sitagliptin-1.88
Placebo-1.42

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Percentage of Participants Who Discontinued Study Drug Due to an AE

An AE is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure, that occurs during the course of the study. (NCT02738879)
Timeframe: Up to 30 weeks

InterventionPercentage of participants (Number)
Sitagliptin1.3
Placebo1.6

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 30

Blood glucose was measured on a fasting basis. Blood was drawn at predose on Day 1 and after 30 weeks of treatment to determine change in plasma glucose levels (i.e., FPG at Week 30 minus FPG at Week 0). (NCT02738879)
Timeframe: Baseline and Week 30

Interventionmg/dL (Least Squares Mean)
Sitagliptin-84.8
Placebo-78.3

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Change From Baseline in Total Daily Insulin Dose (Units) at Week 30

Change from baseline reflects the Week 30 total daily insulin dose minus the Week 0 total daily insulin dose. The Week 0 total daily insulin dose was 0, by definition, because insulin was not administered at baseline. (NCT02738879)
Timeframe: Baseline and Week 30

InterventionInsulin Units (Least Squares Mean)
Sitagliptin53.2
Placebo61.3

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Event Rate of Documented Hypoglycemia With Blood Glucose <56 mg/dL (≤3.1 mmol/L)

Documented hypoglycemia is defined by a measured (e.g., by fingerstick) plasma glucose concentration <56 mg/dL (≤3.1 mmol/L). The event rate was the total number of events divided by follow-up time (participant-years), including multiple events from the same participant. (NCT02738879)
Timeframe: Up to 30 weeks

InterventionEvents/Participant-Years (Number)
Sitagliptin0.30
Placebo0.36

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Total Daily Dose of Insulin for Patients Requiring Supplemental Insulin

Total daily dose of insulin for patients requiring supplemental insulin during surgery and recovery in participants receiving sitagliptin and those receiving the placebo (NCT02741687)
Timeframe: Up to time of discharge from hospital, an average of 10 days

Interventioninternational units of insulin (Number)
Sitagliptin5

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Number of Participants Experiencing Complications

The number of subjects who experience complications including: wound infection, respiratory failure, pneumonia, acute kidney injury with a rise in creatinine by 38 micromoles/Liter from baseline, major adverse cardiac events, bacterial septic infection, and death. Participants will be followed for 30 days following hospital discharge and all complications will be documented. (NCT02741687)
Timeframe: Up to 40 days (average time of discharge from the hospital plus 30 days)

,
InterventionParticipants (Count of Participants)
Wound infectionRespiratory failurePneumoniaAcute kidney injuryCardiac eventBacterial septic infection
Placebo000100
Sitagliptin000100

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Number of Days in the ICU

The number of days a participant spent in the ICU following surgery, when transfer to the ICU was required. (NCT02741687)
Timeframe: Up to time of discharge from hospital, an average of 10 days

Interventiondays (Median)
Placebo2.0
Sitagliptin1.5

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Number of Participants Experiencing Stress Hyperglycemia

The number of participants with at least one episode of stress hyperglycemia. Stress hyperglycemia is defined as a blood glucose > 180 mg/dL. (NCT02741687)
Timeframe: Up to time of discharge from hospital, an average of 10 days

InterventionParticipants (Count of Participants)
Placebo7
Sitagliptin5

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Number of Participants With Hospital Readmissions After Discharge

Readmissions to the study hospital occurring within 30 days of hospital discharge were documented. There were no follow up phone calls or appointments with participants so any hospital readmissions to hospitals other than the one where the surgery occurred are not known. (NCT02741687)
Timeframe: Up to 40 days (average time of discharge from the hospital plus 30 days)

InterventionParticipants (Count of Participants)
Placebo0
Sitagliptin1

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Number of Participants With Hypoglycemic Events

Number of participants experiencing at least one episode of mild hypoglycemia (blood glucose < 70 mg/dL) or clinically significant hypoglycemia (blood glucose < 54 mg/dL) (NCT02741687)
Timeframe: Up to time of discharge from hospital, an average of 10 days

,
InterventionParticipants (Count of Participants)
Mild hypoglycemiaClinically significant hypoglycemia
Placebo20
Sitagliptin50

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Number of Patients Requiring Supplemental, Subcutaneous Insulin

Number of patients requiring subcutaneous insulin, either sliding scale insulin or basal insulin (NCT02741687)
Timeframe: Up to time of discharge from hospital, an average of 10 days

InterventionParticipants (Count of Participants)
Placebo0
Sitagliptin1

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Number of Participants With Emergency Room Visits After Discharge

Emergency room visits to the study hospital occurring within 30 days of hospital discharge were documented. There were no follow up phone calls or appointments with participants so any emergency room visits to hospitals other than the one where the surgery occurred are not known. (NCT02741687)
Timeframe: Up to 40 days (average time of discharge from the hospital plus 30 days)

InterventionParticipants (Count of Participants)
Placebo0
Sitagliptin0

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Length of Hospital Stay

Total length of hospital stay (NCT02741687)
Timeframe: Up to time of discharge from hospital, an average of 10 days

Interventiondays (Median)
Placebo9
Sitagliptin11

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Number of Patients Transferred to the ICU Immediately After Surgery or During Hospitalization

The number of patients who were transferred to the ICU immediately following surgery or anytime while hospitalized after surgery. (NCT02741687)
Timeframe: Up to time of discharge from hospital, an average of 10 days

InterventionParticipants (Count of Participants)
Placebo1
Sitagliptin2

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Percentage of Participants With Hemoglobin A1C ≥8.5% at Baseline That Attained A1C Goal of <7% at Week 20

Hemoglobin A1C is a blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. (NCT02791490)
Timeframe: Baseline and Week 20

InterventionPercentage of participants (Number)
Sitagliptin15.6
Placebo5.7

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Percentage of Participants With Hemoglobin A1C <7% at Week 20

Hemoglobin A1C is a blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. (NCT02791490)
Timeframe: Week 20

InterventionPercentage of participants (Number)
Sitagliptin28.8
Placebo16.6

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Percentage of Participants Who Experienced at Least One Adverse Event (AE)

An adverse event (AE) is any untoward medical occurrence in a study participant administered a pharmaceutical product that does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product, whether or not related to the medicinal product. (NCT02791490)
Timeframe: Up to 22 weeks

InterventionPercentage of participants (Number)
Sitagliptin44.1
Placebo45.9

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Percentage of Participants Receiving Glycemic Rescue Therapy

Participants who met pre-specified criteria for glycemic rescue received appropriate rescue therapy. The choice of anti-hyperglycemic rescue agent, dose, and regimen was directed by the investigator, as clinically appropriate. (NCT02791490)
Timeframe: Up to 20 weeks

InterventionPercentage of participants (Number)
Sitagliptin1.3
Placebo3.1

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Change From Baseline in Hemoglobin A1C at Week 20

Hemoglobin A1C is a blood marker used to report average blood glucose levels over prolonged periods of time. Percentage A1C is the ratio of glycated hemoglobin to total hemoglobin x 100. The change from baseline represents the Week 20 A1C value minus the Week 0 (baseline) A1C value. (NCT02791490)
Timeframe: Baseline and Week 20

InterventionA1C (%) (Least Squares Mean)
Sitagliptin-1.10
Placebo-0.69

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 20

Plasma glucose was measured on a fasting basis and is expressed as mg/dL. Blood was drawn predose on Day 1 and after 20 weeks of treatment to determine change in FPG levels. The change from baseline represents the Week 20 FPG value minus the Week 0 (baseline) FPG value. (NCT02791490)
Timeframe: Baseline and Week 20

Interventionmg/dL (Least Squares Mean)
Sitagliptin-29.3
Placebo-16.9

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Percentage of Participants Who Discontinued Study Drug Due to an Adverse Event

An adverse event (AE) is any untoward medical occurrence in a study participant administered a pharmaceutical product that does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product, whether or not related to the medicinal product. (NCT02791490)
Timeframe: Up to 20 weeks

InterventionPercentage of participants (Number)
Sitagliptin0.9
Placebo0.0

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Change in Body Weight (%)- Sustainability

Relative change from baseline (week 0) in body weight (kg) was evaluated at week 104. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, week 104

InterventionPercentage change (Mean)
Oral Semaglutide Flex- Sustainability-4.03

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Change in Body Weight (%)- Switch

Relative change from week 52 in body weight (kg) was evaluated at week 104. Results are based on the data from the in-trial observation period, which was the time period from when a participant was re-randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 52, week 104

InterventionPercentage change (Mean)
Oral Semaglutide Flex- Switch-3.12
Sitagliptin 100 mg- Switch-0.70

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Change in Body Weight (kg)- Sustainability

Change from baseline (week 0) in body weight was evaluated at week 104. The endpoint was evaluated based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, week 104

InterventionKg (Mean)
Oral Semaglutide Flex- Sustainability-3.7

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Change in Body Weight- Switch

Change from week 52 in body weight was evaluated at week 104. Results are based on the data from the in-trial observation period, which was the time period from when a participant was re-randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 52, week 104

InterventionKg (Mean)
Oral Semaglutide Flex- Switch-2.6
Sitagliptin 100 mg- Switch-0.9

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Change in FPG

Change from baseline (week 0) in fasting plasma glucose (FPG) was evaluated at week 52. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, week 52

InterventionMillimoles per liter (mmol/L) (Mean)
Oral Semaglutide Flex- Main Phase-2.41
Sitagliptin 100 mg- Main Phase-1.39

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Change in FPG- Sustainability

Change from baseline (week 0) in fasting plasma glucose (FPG) was evaluated at week 104. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, week 104

InterventionMillimoles per liter (mmol/L) (Mean)
Oral Semaglutide Flex- Sustainability-39.4

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Change in FPG- Switch

Change from week 52 in fasting plasma glucose (FPG) was evaluated at week 104. Results are based on the data from the in-trial observation period, which was the time period from when a participant was re-randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 52, week 104

InterventionMillimoles per liter (mmol/L) (Mean)
Oral Semaglutide Flex- Switch-0.35
Sitagliptin 100 mg- Switch0.02

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Change in Waist Circumference- Sustainability

Change from baseline (week 0) in waist circumference was evaluated at week 104. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, week 104

Interventioncm (Mean)
Oral Semaglutide Flex- Sustainability-2.5

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Change in HbA1c

Change from baseline (week 0) in HbA1c was evaluated at week 52. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, week 52

InterventionPercentage of HbA1c (Mean)
Oral Semaglutide Flex- Main Phase-1.3
Sitagliptin 100 mg- Main Phase-0.8

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Change in HbA1c- Sustainability

Change from baseline (week 0) in HbA1c was evaluated at week 104. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, week 104

InterventionPercentage of HbA1c (Mean)
Oral Semaglutide Flex- Sustainability-1.3

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Change in HbA1c- Switch

Change from week 52 in HbA1c was evaluated at week 104. Results are based on the data from the in-trial observation period, which was the time period from when a participant was re-randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 52, week 104

InterventionPercentage of HbA1c (Mean)
Oral Semaglutide Flex- Switch-0.2
Sitagliptin 100 mg- Switch0.0

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Change in LDL Cholesterol (Ratio to Baseline)

Change from baseline (week 0) in low-density lipoprotein (LDL) cholesterol (mmol/L) at week 52 is presented as ratio to baseline. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, week 52

InterventionRatio of LDL cholesterol (Geometric Mean)
Oral Semaglutide Flex- Main Phase0.97
Sitagliptin 100 mg- Main Phase1.03

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Change in Lipase (Ratio to Baseline)

Change from baseline (week 0) in lipase (U/L) to week 52 is presented as ratio to baseline. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 0, Week 52

InterventionRatio of lipase (Geometric Mean)
Oral Semaglutide Flex- Main Phase1.24
Sitagliptin 100 mg- Main Phase1.13

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Change in Lipase (Ratio to Baseline)- Sustainability

Change from baseline (week 0) in lipase (U/L) to week 104 is presented as ratio to baseline. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 0, Week 104

InterventionRatio of lipase (Geometric Mean)
Oral Semaglutide Flex- Sustainability1.18

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Change in Lipase (Ratio to Baseline)- Switch

Change from week 52 in lipase (U/L) to week 104 is presented as ratio to baseline. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 52, Week 104

InterventionRatio of lipase (Geometric Mean)
Oral Semaglutide Flex- Switch1.13
Sitagliptin 100 mg- Switch0.92

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Change in Pulse Rate

Change from baseline (week 0) in pulse rate was evaluated at week 52. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 0, week 52

InterventionBeats per minute (Mean)
Oral Semaglutide Flex- Main Phase3
Sitagliptin 100 mg- Main Phase0

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Change in HDL Cholesterol (Ratio to Baseline)

Change from baseline (week 0) in high-density lipoprotein (HDL) cholesterol (mmol/L) at weeks 26, 52 and 78 is presented as ratio to baseline. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, week 52

InterventionRatio of HDL cholesterol (Geometric Mean)
Oral Semaglutide Flex- Main Phase1.00
Sitagliptin 100 mg- Main Phase1.02

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Time to Rescue Medication

Presented results are the number of participants who had taken rescue medication anytime during the periods, from week 0 to week 52. Rescue medication was defined as any new anti-diabetic medication used as add-on to trial product and used for more than 21 days with the initiation at or after randomisation (week 0) and before last day on trial product, and/or intensification of anti-diabetic medication (a more than 20% increase in dose relative to baseline) for more than 21 days with the intensification at or after randomisation and before last day on trial product. Results are based on the data from the on-treatment without rescue medication observation period, which was the time period when a participant was on treatment with trial product, excluding any period after initiation of rescue medication and/or premature trial product discontinuation. (NCT02849080)
Timeframe: Weeks 0-52

InterventionParticipants (Count of Participants)
Oral Semaglutide Flex- Main Phase8
Sitagliptin 100 mg- Main Phase40

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Time to Additional Anti-diabetic Medication- Switch

Presented results are the number of participants who had taken additional anti-diabetic medication anytime during the period from week 53 to week 104. Additional anti-diabetic medication was defined as any new anti-diabetic medication used for more than 21 days with the initiation at or after re-randomisation (week 52) and before (planned) end-of-treatment (week 104), and/or intensification of anti-diabetic medication (a more than 20% increase in dose relative to baseline) for more than 21 days with the intensification at or after randomisation and before (planned) end-of-treatment. Results are based on the data from the in-trial observation period, which was the time period from when a participant was re-randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Weeks 53-104

InterventionParticipants (Count of Participants)
Oral Semaglutide Flex- Switch15
Sitagliptin 100 mg- Switch26

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Time to Additional Anti-diabetic Medication

Presented results are the number of participants who had taken additional anti-diabetic medication anytime during the period from week 0 to week 52. Additional anti-diabetic medication was defined as any new anti-diabetic medication used for more than 21 days with the initiation at or after randomisation (week 0) and before (planned) end-of-treatment (week 52), and/or intensification of anti-diabetic medication (a more than 20% increase in dose relative to baseline) for more than 21 days with the intensification at or after randomisation and before (planned) end-of-treatment. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Weeks 0-52

InterventionParticipants (Count of Participants)
Oral Semaglutide Flex- Main Phase22
Sitagliptin 100 mg- Main Phase47

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Paticipants With Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes (Yes/no)- Switch

Number of participants with treatment-emergent severe or BG confirmed symptomatic hypoglycaemic episodes were recorded during weeks 53 to 109. Hypoglycaemic episodes with onset during the on-treatment observation period were considered treatment-emergent. On-treatment observation period was defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. Severe hypoglycaemia was defined as an episode requiring assistance of another person to actively administer carbohydrate or glucagon, or take other corrective actions. BG-confirmed symptomatic hypoglycaemia: Confirmed by a glucose value <3.1 mmol/L (56 mg/dL) with symptoms consistent with hypoglycaemia. (NCT02849080)
Timeframe: Week 53-109

InterventionParticipants (Count of Participants)
Oral Semaglutide Flex- Switch2
Sitagliptin 100 mg- Switch4

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Paticipants With Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes (Yes/no)- Sustainability

Number of participants with treatment-emergent severe or BG confirmed symptomatic hypoglycaemic episodes were recorded during weeks 0-109 ((104-week treatment period for participants who continued in the extension phase or 52-week treatment period for participants who did not continue in the extension phase) plus the 5-week follow-up period). Hypoglycaemic episodes with onset during the on-treatment observation period were considered treatment-emergent. On-treatment observation period was defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. Severe hypoglycaemia was defined as an episode requiring assistance of another person to actively administer carbohydrate or glucagon, or take other corrective actions. BG-confirmed symptomatic hypoglycaemia: Confirmed by a glucose value <3.1 mmol/L (56 mg/dL) with symptoms consistent with hypoglycaemia. (NCT02849080)
Timeframe: Week 0-109

InterventionParticipants (Count of Participants)
Oral Semaglutide Flex- Sustainability18

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Paticipants With Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes (Yes/no)

Treatment emergent severe or BG confirmed symptomatic hypoglycaemic episodes were recorded during weeks 0-57 (52-week treatment period for participants who continued in the extension phase; 52-week treatment period plus the 5-week follow-up period for participants who did not continue in the extension phase). Hypoglycaemic episodes with onset during the on-treatment observation period were considered treatment-emergent. On-treatment observation period was defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. Severe hypoglycaemia was defined as an episode requiring assistance of another person to actively administer carbohydrate or glucagon, or take other corrective actions. BG-confirmed symptomatic hypoglycaemia: Confirmed by a glucose value <3.1 mmol/L (56 mg/dL) with symptoms consistent with hypoglycaemia. (NCT02849080)
Timeframe: Week 0-57

InterventionParticipants (Count of Participants)
Oral Semaglutide Flex- Main Phase14
Sitagliptin 100 mg- Main Phase14

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Participants Who Achieve HbA1c <7.0% (53 mmol/Mol) ADA Target and no Need for Rescue Medication (Yes/no)- Switch

Participants who achieved HbA1c <7.0% (American Diabetes Association (ADA) target) and no need for rescue medication (yes/no), was evaluated at week 104. Results are based on the data from the on-treatment without rescue medication observation period, which was the time period when a participant was on treatment with trial product, excluding any period after initiation of rescue medication and/or premature trial product discontinuation. (NCT02849080)
Timeframe: Week 104 (i.e., after 52 weeks of treatment in the extension phase)

InterventionParticipants (Count of Participants)
Oral Semaglutide Flex- Switch41
Sitagliptin 100 mg- Switch23

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Number of Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes)- Sustainability

Treatment emergent severe or BG confirmed symptomatic hypoglycaemic episodes were recorded during weeks 0-109 ((104-week treatment period for participants who continued in the extension phase or 52-week treatment period for participants who did not continue in the extension phase) plus the 5-week follow-up period). Hypoglycaemic episodes with onset during the on-treatment observation period were considered treatment-emergent. On-treatment observation period was defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. Severe hypoglycaemia was defined as an episode requiring assistance of another person to actively administer carbohydrate or glucagon, or take other corrective actions. BG-confirmed symptomatic hypoglycaemia: Confirmed by a glucose value <3.1 mmol/L (56 mg/dL) with symptoms consistent with hypoglycaemia. (NCT02849080)
Timeframe: Week 0-109

InterventionEpisodes (Number)
Oral Semaglutide Flex- Sustainability45

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Number of Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes- Switch

Treatment emergent severe or BG confirmed symptomatic hypoglycaemic episodes were recorded during weeks 53 to 109. Hypoglycaemic episodes with onset during the on-treatment observation period were considered treatment-emergent. On-treatment observation period was defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. Severe hypoglycaemia was defined as an episode requiring assistance of another person to actively administer carbohydrate or glucagon, or take other corrective actions. BG-confirmed symptomatic hypoglycaemia: Confirmed by a glucose value <3.1 mmol/L (56 mg/dL) with symptoms consistent with hypoglycaemia. (NCT02849080)
Timeframe: Week 53-109

InterventionEpisodes (Number)
Oral Semaglutide Flex- Switch2
Sitagliptin 100 mg- Switch12

[back to top]

Number of Treatment-emergent Severe or BG-confirmed Symptomatic Hypoglycaemic Episodes

Treatment emergent severe or BG confirmed symptomatic hypoglycaemic episodes were recorded during weeks 0-57 (52-week treatment period for participants who continued in the extension phase; 52-week treatment period plus the 5-week follow-up period for participants who did not continue in the extension phase). Hypoglycaemic episodes with onset during the on-treatment observation period were considered treatment-emergent. On-treatment observation period was defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. Severe hypoglycaemia was defined as an episode requiring assistance of another person to actively administer carbohydrate or glucagon, or take other corrective actions. BG-confirmed symptomatic hypoglycaemia: Confirmed by a glucose value <3.1 mmol/L (56 mg/dL) with symptoms consistent with hypoglycaemia. (NCT02849080)
Timeframe: Week 0-57

InterventionEpisodes (Number)
Oral Semaglutide Flex- Main Phase34
Sitagliptin 100 mg- Main Phase22

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Number of TEAEs During Exposure to Trial Product- Switch

Treatment emergent adverse events (TEAEs) were recorded from week 53 to week 109. Adverse events (AEs) with onset during the on-treatment observation period were considered treatment-emergent. On-treatment observation period: Time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 53-109

InterventionEvents (Number)
Oral Semaglutide Flex- Switch267
Sitagliptin 100 mg- Switch225

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Number of TEAEs During Exposure to Trial Product- Sustainability

Treatment emergent adverse events (TEAEs) were recorded from week 0 to week 109 ((104-week treatment period for participants who continued in the extension phase or 52-week treatment period for participants who did not continue in the extension phase) plus the 5-week follow-up period). Adverse events (AEs) with onset during the on-treatment observation period were considered treatment-emergent. On-treatment observation period: Time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 0-109

InterventionEvents (Number)
Oral Semaglutide Flex- Sustainability1157

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Number of TEAEs During Exposure to Trial Product

Treatment emergent adverse events (TEAEs) were recorded from week 0 to week 57 (52-week treatment period for participants who continued in the extension phase; 52-week treatment period plus the 5-week follow-up period for participants who did not continue in the extension phase). Adverse events (AEs) with onset during the on-treatment observation period were considered treatment-emergent. On-treatment observation period: Time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 0-57

InterventionEvents (Number)
Oral Semaglutide Flex- Main Phase768
Sitagliptin 100 mg- Main Phase519

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Change in Waist Circumference- Switch

Change from week 52 in waist circumference was evaluated at week 104. Results are based on the data from the in-trial observation period, which was the time period from when a participant was re-randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 52, week 104

InterventionCentimeters (cm) (Mean)
Oral Semaglutide Flex- Switch-1.8
Sitagliptin 100 mg- Switch-0.9

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Change in Amylase (Ratio to Baseline)

Change from baseline (week 0) in biochemical parameter- amylase (units per liter [U/L]) to week 52 is presented as ratio to baseline. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 0, Week 52

InterventionRatio of amylase (Geometric Mean)
Oral Semaglutide Flex- Main Phase1.14
Sitagliptin 100 mg- Main Phase1.08

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Change in Waist Circumference

Change from baseline (week 0) in waist circumference was evaluated at week 52. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, week 52

InterventionCentimeters (cm) (Mean)
Oral Semaglutide Flex- Main Phase-2.6
Sitagliptin 100 mg- Main Phase-0.7

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Change in Triglycerides (Ratio to Baseline)

Change from baseline (week 0) in triglycerides (mmol/L) at week 52 is presented as ratio to baseline. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, week 52

InterventionRatio of triglycerides (Geometric Mean)
Oral Semaglutide Flex- Main Phase0.89
Sitagliptin 100 mg- Main Phase0.91

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Change in Total Cholesterol (Ratio to Baseline)

Change from baseline (week 0) in total cholesterol (mmol/L) at week 52 is presented as ratio to baseline. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, Week 52

InterventionRatio of total cholesterol (Geometric Mean)
Oral Semaglutide Flex- Main Phase0.96
Sitagliptin 100 mg- Main Phase1.01

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Change in Pulse Rate- Switch

Change from week 52 in pulse rate was evaluated at week 104. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 52, week 104

InterventionBeats per minute (Mean)
Oral Semaglutide Flex- Switch1
Sitagliptin 100 mg- Switch-0

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Change in Pulse Rate- Sustainability

Change from baseline (week 0) in pulse rate was evaluated at week 104. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 0, week 104

InterventionBeats per minute (Mean)
Oral Semaglutide Flex- Sustainability2

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Time to Rescue Medication- Switch

Presented results are the number of participants who had taken rescue medication anytime during the periods, from week 53 to week 104. Rescue medication was defined as any new anti-diabetic medication used as add-on to trial product and used for more than 21 days with the initiation at or after re-randomisation (week 52) and before last day on trial product, and/or intensification of anti-diabetic medication (a more than 20% increase in dose relative to baseline) for more than 21 days with the intensification at or after randomisation and before last day on trial product. Results are based on the data from the on-treatment without rescue medication observation period, which was the time period when a participant was on treatment with trial product, excluding any period after initiation of rescue medication and/or premature trial product discontinuation. (NCT02849080)
Timeframe: Weeks 53-104

InterventionParticipants (Count of Participants)
Oral Semaglutide Flex- Switch9
Sitagliptin 100 mg- Switch23

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Change in Amylase (Ratio to Baseline)- Sustainability

Change from baseline (week 0) in biochemical parameter- amylase (units per liter [U/L]) to week 104 is presented as ratio to baseline. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 0, week 104

InterventionRatio of amylase (Geometric Mean)
Oral Semaglutide Flex- Sustainability1.13

[back to top]

Change in Amylase (Ratio to Baseline)- Switch

Change from week 52 in biochemical parameter- amylase (U/L) to week 104 is presented as ratio to baseline. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 52, Week 104

InterventionRatio of amylase (Geometric Mean)
Oral Semaglutide Flex- Switch1.09
Sitagliptin 100 mg- Switch1.00

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Change in BMI

Change from baseline (week 0) in body mass index (BMI) was evaluated at week 52. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, Week 52

InterventionKilograms per square meter (kg/m^2) (Mean)
Oral Semaglutide Flex- Main Phase-1.0
Sitagliptin 100 mg- Main Phase-0.3

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Change in BMI- Sustainability

Change from baseline (week 0) in body mass index (BMI) was evaluated at week 104. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, Week 104

Interventionkg/m^2 (Mean)
Oral Semaglutide Flex- Sustainability-1.3

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Participants Who Achieve HbA1c <7.0% (53 mmol/Mol) ADA Target (Yes/no)

Participants who achieved HbA1c <7.0% (American Diabetes Association (ADA) target) (yes/no), was evaluated at week 52. The endpoint was evaluated based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. The endpoint was also evaluated based on the data from the on-treatment without rescue medication observation period, which was the time period when a participant was on treatment with trial product, excluding any period after initiation of rescue medication and/or premature trial product discontinuation. (NCT02849080)
Timeframe: Week 52

InterventionParticipants (Count of Participants)
In-trial72499292In-trial72499293On-treatment without rescue medication72499292On-treatment without rescue medication72499293
YesNo
Oral Semaglutide Flex- Main Phase134
Sitagliptin 100 mg- Main Phase60
Oral Semaglutide Flex- Main Phase96
Sitagliptin 100 mg- Main Phase178
Oral Semaglutide Flex- Main Phase123
Sitagliptin 100 mg- Main Phase52
Oral Semaglutide Flex- Main Phase73
Sitagliptin 100 mg- Main Phase132

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Participants Who Achieve Weight Loss ≥5% (Yes/no)

Participants who achieved weight loss more than or equal to 5% of their baseline body weight (yes/no) at weeks 52 is presented. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 52

,
InterventionParticipants (Count of Participants)
YesNo
Oral Semaglutide Flex- Main Phase63170
Sitagliptin 100 mg- Main Phase29210

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Change in BMI- Switch

Change from week 52 in body mass index (BMI) was evaluated at week 104. Results are based on the data from the in-trial observation period, which was the time period from when a participant was re-randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 52, Week 104

Interventionkg/m^2 (Mean)
Oral Semaglutide Flex- Switch-0.9
Sitagliptin 100 mg- Switch-0.3

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Change in Body Weight (%)

Relative change from baseline (week 0) in body weight (kg) was evaluated at week 52. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 0, week 52

InterventionPercentage change (Mean)
Oral Semaglutide Flex- Main Phase-2.99
Sitagliptin 100 mg- Main Phase-0.76

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Participants Who Achieve Weight Loss ≥10% (Yes/no)

Participants who achieved weight loss more than or equal to 10% of their baseline body weight (yes/no) at week 52 is presented. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 52

,
InterventionParticipants (Count of Participants)
YesNo
Oral Semaglutide Flex- Main Phase15218
Sitagliptin 100 mg- Main Phase5234

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Participants Who Achieve HbA1c Reduction ≥1% (10.9 mmol/Mol) and Weight Loss ≥3% (Yes/no)

Participants who achieved HbA1c reduction more than or equal to 1% of their baseline HbA1c and weight loss of more than or equal to 3% of their baseline body weight (yes/no) at week 52 is presented. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 52

,
InterventionParticipants (Count of Participants)
YesNo
Oral Semaglutide Flex- Main Phase80150
Sitagliptin 100 mg- Main Phase25213

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Participants Who Achieve HbA1c ≤6.5% (48 mmol/Mol) AACE Target (Yes/no)

Participants who achieved HbA1c less than or equal to 6.5% (American Association of Clinical Endocrinologists (AACE) target) (yes/no) at week 52 is presented. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 52

,
InterventionParticipants (Count of Participants)
YesNo
Oral Semaglutide Flex- Main Phase76154
Sitagliptin 100 mg- Main Phase29209

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Participants Who Achieve HbA1c <7.0 % (53 mmol/Mol) Without Hypoglycaemia (Severe or BG Confirmed Symptomatic Hypoglycaemia) and no Weight Gain (Yes/no)

Participants who achieved HbA1c less than 7.0 % without severe or blood glucose (BG) confirmed symptomatic hypoglycaemia and without weight gain (yes/no) at week 52 is presented. Severe hypoglycaemia was defined as an episode requiring assistance of another person to actively administer carbohydrate or glucagon, or take other corrective actions. BG-confirmed symptomatic hypoglycaemia was defined as an episode with plasma glucose value <3.1 mmol/L with symptoms consistent with hypoglycaemia. Results are based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. (NCT02849080)
Timeframe: Week 52

,
InterventionParticipants (Count of Participants)
YesNo
Oral Semaglutide Flex- Main Phase104126
Sitagliptin 100 mg- Main Phase35203

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Change in SF-36v2 (Acute Version) Health Survey: Scores From the 8 Domains, the Physical Component Summary (PCS) and the Mental Component Summary (MCS)- Switch

SF-36 is a 36-item patient-reported survey of patient health that measures the participant's overall health-related quality of life (HRQoL). SF-36v2™ (acute version) questionnaire measured eight domains of functional health and well-being as well as two component summary scores (physical component summary (PCS) and mental component summary (MCS)). The 0-100 scale scores (where higher scores indicated a better HRQoL) from the SF-36 were converted to norm-based scores to enable a direct interpretation in relation to the distribution of the scores in the 2009 U.S. general population. In the metric of norm-based scores, 50 and 10 corresponds to the mean and standard deviation respectively of the 2009 U.S. general population. Change from week 52 in the domain scores and component summary (PCS and MCS) scores were evaluated at week 104. A positive change score indicates an improvement since week 52. Results are based on the data from the in-trial observation period. (NCT02849080)
Timeframe: Week 52, week 104

,
InterventionScore on a scale (Mean)
Physical functioningRole physicalBodily painGeneral healthVitalitySocial functioningRole emotionalMental healthPCSMCS
Oral Semaglutide Flex- Switch1.141.37-0.180.69-0.180.211.720.370.660.52
Sitagliptin 100 mg- Switch-0.97-0.22-0.300.53-0.150.10-0.390.20-0.430.19

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Change in SF-36v2 (Acute Version) Health Survey: Scores From the 8 Domains, the Physical Component Summary (PCS) and the Mental Component Summary (MCS)- Sustainability

Short form (SF)-36 is a 36-item patient-reported survey of patient health that measures the participant's overall health-related quality of life (HRQoL). SF-36v2™ (acute version) questionnaire measured eight domains of functional health and well-being as well as two component summary scores (physical component summary (PCS) and mental component summary (MCS)). The 0-100 scale scores (where higher scores indicated a better HRQoL) from the SF-36 were converted to norm-based scores to enable a direct interpretation in relation to the distribution of the scores in the 2009 U.S. general population. In the metric of norm-based scores, 50 and 10 corresponds to the mean and standard deviation respectively of the 2009 U.S. general population. Change from baseline (week 0) in the domain scores and component summary (PCS and MCS) scores were evaluated at week 104. A positive change score indicates an improvement since baseline. Results are based on the data from the in-trial observation period. (NCT02849080)
Timeframe: Week 0, week 104

InterventionScore on a scale (Mean)
Physical functioningRole physicalBodily painGeneral healthVitalitySocial functioningRole emotionalMental healthPCSMCS
Oral Semaglutide Flex- Sustainability1.440.221.071.980.97-0.11-0.041.051.330.20

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Change in SF-36v2 (Acute Version) Health Survey: Scores From the 8 Domains, the Physical Component Summary (PCS) and the Mental Component Summary (MCS)

SF-36 is a 36-item patient-reported survey of patient health that measures the participant's overall health-related quality of life (HRQoL). SF-36v2™ (acute version) questionnaire measured eight domains of functional health and well-being as well as two component summary scores (physical component summary (PCS) and mental component summary (MCS)). The 0-100 scale scores (where higher scores indicated a better HRQoL) from the SF-36 were converted to norm-based scores to enable a direct interpretation in relation to the distribution of the scores in the 2009 U.S. general population. In the metric of norm-based scores, 50 and 10 corresponds to the mean and standard deviation respectively of the 2009 U.S. general population. Change from baseline (week 0) in the domain scores and component summary (PCS and MCS) scores were evaluated at week 52. A positive change score indicates an improvement since baseline. Results are based on the data from the in-trial observation period. (NCT02849080)
Timeframe: Week 0, week 52

,
InterventionScore on a scale (Mean)
Physical functioningRole physicalBodily painGeneral healthVitalitySocial functioningRole emotionalMental healthPCSMCS
Oral Semaglutide Flex- Main Phase1.540.401.091.831.070.38-0.911.211.510.01
Sitagliptin 100 mg- Main Phase-0.030.131.201.620.510.41-0.540.860.740.26

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Change in DTSQ- Switch

"Change from week 52 in diabetes treatment satisfaction questionnaire - status (DTSQs) was evaluated at week 104. The DTSQs items are scored on a 7-point graded response scale ranging from 6 to 0. Higher scores indicate higher levels of treatment satisfaction for DTSQs items 1, 4 -8. For items 2 and 3 a higher score indicates a higher patient perceived experience of high blood sugars and low blood sugars, respectively. Thus, lower scores indicate a perception of blood glucose levels being none of the time unacceptably high (item 2) or low (item 3). The domain score of total treatment satisfaction (total treatment satisfaction score) was computed by adding the six items scores 1, 4-8. The score ranges 0-36. A higher treatment satisfaction score indicates a higher level of treatment satisfaction. Results are based on the data from the in-trial observation period." (NCT02849080)
Timeframe: Week 52, week 104

,
InterventionScore on a scale (Mean)
1) Satisfaction with treatment2) Feeling of unacceptably high blood sugars3) Feeling of unacceptably low blood sugars4) Convenience of treatment5) Flexibility of current treatment6) Satisfaction with understanding of diabetes7) Recommending treatment to others8) Satisfaction to continue with present treatmentTotal treatment satisfaction score
Oral Semaglutide Flex- Switch0.06-0.320.020.130.010.020.04-0.050.20
Sitagliptin 100 mg- Switch-0.240.090.230.130.060.04-0.050.00-0.06

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Change in DTSQ- Sustainability

"Change from week 0 in diabetes treatment satisfaction questionnaire - status (DTSQs) was evaluated at week 104. The DTSQs items are scored on a 7-point graded response scale ranging from 6 to 0. Higher scores indicate higher levels of treatment satisfaction for DTSQs items 1, 4 -8. For items 2 and 3 a higher score indicates a higher patient perceived experience of high blood sugars and low blood sugars, respectively. Thus, lower scores indicate a perception of blood glucose levels being none of the time unacceptably high (item 2) or low (item 3). The domain score of total treatment satisfaction (total treatment satisfaction score) was computed by adding the six items scores 1, 4-8. The score ranges 0-36. A higher treatment satisfaction score indicates a higher level of treatment satisfaction. Results are based on the data from the in-trial observation period." (NCT02849080)
Timeframe: Week 0, week 104

InterventionScore on a scale (Mean)
1) Satisfaction with treatment2) Feeling of unacceptably high blood sugars3) Feeling of unacceptably low blood sugars4) Convenience of treatment5) Flexibility of current treatment6) Satisfaction with understanding of diabetes7) Recommending treatment to others8) Satisfaction to continue with present treatmentTotal treatment satisfaction score
Oral Semaglutide Flex- Sustainability1.19-1.46-0.140.880.860.840.941.115.81

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Change in DTSQ

"Change from baseline (week 0) in diabetes treatment satisfaction questionnaire - status (DTSQs) was evaluated at week 52. The DTSQs items are scored on a 7-point graded response scale ranging from 6 to 0. Higher scores indicate higher levels of treatment satisfaction for DTSQs items 1, 4 -8. For items 2 and 3 a higher score indicates a higher patient perceived experience of high blood sugars and low blood sugars, respectively. Thus, lower scores indicate a perception of blood glucose levels being none of the time unacceptably high (item 2) or low (item 3). The domain score of total treatment satisfaction (total treatment satisfaction score) was computed by adding the six items scores 1, 4-8. The score ranges 0-36. A higher treatment satisfaction score indicates a higher level of treatment satisfaction. Results are based on the data from the in-trial observation period." (NCT02849080)
Timeframe: Week 0, Week 52

,
InterventionScore on a scale (Mean)
1) Satisfaction with treatment2) Feeling of unacceptably high blood sugars3) Feeling of unacceptably low blood sugars4) Convenience of treatment5) Flexibility of current treatment6) Satisfaction with understanding of diabetes7) Recommending treatment to others8) Satisfaction to continue with present treatmentTotal treatment satisfaction score
Oral Semaglutide Flex- Main Phase1.09-1.58-0.150.820.800.770.881.035.39
Sitagliptin 100 mg- Main Phase0.92-1.14-0.240.590.680.770.790.954.70

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Change in Body Weight

Change from baseline (week 0) in body weight was evaluated at week 52. The endpoint was evaluated based on the data from the in-trial observation period, which was the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication and/or premature discontinuation of trial product. The endpoint was also evaluated based on the data from the on-treatment without rescue medication observation period, which was the time period when a participant was on treatment with trial product, excluding any period after initiation of rescue medication and/or premature trial product discontinuation. (NCT02849080)
Timeframe: Week 0, week 52

,
InterventionKilogram (Kg) (Mean)
In-trialOn-treatment without rescue medication
Oral Semaglutide Flex- Main Phase-2.7-2.9
Sitagliptin 100 mg- Main Phase-0.7-0.9

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Change in Blood Pressure (Systolic and Diastolic Blood Pressure)- Switch

Change from week 52 in systolic blood pressure (SBP) and diastolic blood pressure (DBP) was evaluated at week 104. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 52, week 104

,
InterventionMillimeters of mercury (mmHg) (Mean)
Systolic blood pressureDiastolic blood pressure
Oral Semaglutide Flex- Switch-3-1
Sitagliptin 100 mg- Switch2-0

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Change in Blood Pressure (Systolic and Diastolic Blood Pressure)- Sustainability

Change from baseline (week 0) in systolic blood pressure (SBP) and diastolic blood pressure (DBP) was evaluated at week 104. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 0, week 104

InterventionMillimeters of mercury (mmHg) (Mean)
Systolic blood pressureDiastolic blood pressure
Oral Semaglutide Flex- Sustainability-3-1

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Change in Blood Pressure (Systolic and Diastolic Blood Pressure)

Change from baseline (week 0) in systolic blood pressure (SBP) and diastolic blood pressure (DBP) was evaluated at week 52. Results are based on the data from the on-treatment observation period which was the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT02849080)
Timeframe: Week 0, week 52

,
InterventionMillimeters of mercury (mmHg) (Mean)
Systolic blood pressureDiastolic blood pressure
Oral Semaglutide Flex- Main Phase-3-0
Sitagliptin 100 mg- Main Phase-2-1

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Change From Baseline in Left Ventricular Ejection Fraction (LVEF) Measured by MRI at 24 Weeks.

Evaluation the effects of saxagliptin compared to placebo on left ventricular end systolic volume (LVESV) index, left ventricular ejection fraction (LVEF), and left ventricular mass (LVM) after 24 weeks in patients with T2DM and HF. (NCT02917031)
Timeframe: Baseline to week 24

InterventionPercentage (Mean)
Saxagliptin0.533
Placebo0.298

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Number of Participants With Adverse Events

Assessment of safety and tolerability of saxagliptin and sitagliptin treatment in patients with T2DM and HF (NCT02917031)
Timeframe: From screening (Days -28 to -1) until Week 28 (follow-up visit)

,,
InterventionParticipants (Count of Participants)
Any AEAny severe AEAny treatment related AEAny AE with outcome DeathAny SAEAny treatment related SAEAny SAE leading to discontinuation of study treatmentAny AE leading to discontinuation of study treatmentAny Adverse event of special interest
Placebo5814042904716
Saxagliptin539321701512
Sitagliptin5113431900315

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Change From Baseline in NT-proBNP After 24 Weeks of Treatment

Evaluation of the effects of saxagliptin compared to placebo on N-terminal prohormone of brain natriuretic peptide (NT-proBNP) after 24 weeks of treatment. (NCT02917031)
Timeframe: Baseline to Week 28 (End of Study visit [EoS])

Interventionpg/mL (Mean)
Saxagliptin-277.525
Placebo-61.895

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Change From Baseline in Left Ventricular Mass (LVM) Measured by MRI at 24 Weeks.

Evaluation of the effects of saxagliptin compared to placebo on left ventricular mass (LVM) after 24 weeks in patients with T2DM and HF. (NCT02917031)
Timeframe: At 24 week

InterventionGram (Mean)
Saxagliptin-4.211
Placebo-0.758

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Change From Baseline in Left Ventricular End Systolic Volume (LVESV) Index, Measured by MRI at 24 Weeks.

Evaluation of the effects of saxagliptin compared to placebo on left ventricular end systolic volume (LVESV) index, after 24 weeks in patients with T2DM and HF. (NCT02917031)
Timeframe: Baseline to week 24

InterventionmL/m2 (Mean)
Saxagliptin-2.555
Placebo-0.839

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Change From Baseline in Left Ventricular End Diastolic Volume (LVEDV) Index Measured by Magnetic Resonance Imaging (MRI) at 24 Weeks

MRI was performed to evaluate LVEDV at baseline and Visit 10 (Week 24). Evaluated to exclude an increase in left ventricular end diastolic volume (LVEDV) index of greater than 10% of the overall baseline value (noninferiority margin) in patients with T2DM and HF treated with saxagliptin for 24 weeks, compared to placebo. Baseline is last assessment on or before the date of first dose. (NCT02917031)
Timeframe: Baseline to 24 weeks

InterventionmL/m^2 (Mean)
Saxagliptin-3.395
Placebo-0.716

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Change From Baseline Aerobic Exercise Capacity at 12 Weeks

Peak oxygen consumption (VO2) measured by maximal cardiopulmonary exercise test (NCT02920918)
Timeframe: baseline and 12 weeks

InterventionmL/kg/min (Mean)
Canagliflozin0.67
Sitagliptin-0.53

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Change From Baseline Ventilatory Efficiency at 12 Weeks

Minute ventilation (VE) relative to CO2 production (VCO2) slope measured by cardiopulmonary exercise test (NCT02920918)
Timeframe: baseline and 12 weeks

InterventionUnitless (Mean)
Canagliflozin-0.3
Sitagliptin-0.3

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Cmax (Maximum Observed Plasma Concentration)

Whole venous blood samples of 5 mL were be collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. Pharmacokinetic (PK) blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. Cmax was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionng/mL (Geometric Mean)
Bexagliflozin PK parametersGlimepiride PK parameters
Group 2: Bexagliflozin + Glimepiride143.767.1

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Urinary Glucose Excretion up to 0-72 hr

Pre-dose urine samples were collected from -12 to 0 h for baseline measurement. Subjects was instructed to empty their bladder prior to dosing. Post-dose urine was collected in 4 batches for Groups 1 and 2 at 0 to 12 h, 12 to 24 h, 24 o 36 h, and 36 to 48 h collections. Post-dose urine was collected in batches for Group 3 at 0 to 12 h, 12 to 24 h, 24 to 36 h, 36 to 48 h, 48 to 60 h and 60 to 72 h. (NCT02956044)
Timeframe: up to 0-72 hr

,,
Interventiong (Mean)
0 - 12 hours12 - 24 hours24 - 36 hours36 - 48 hours48 - 60 hours60 - 72 hours
Group 3: Bexagliflozin + Sitagliptin23.9422.8524.1510.1711.502.70
Group 3: Bexagliflozin Alone29.0124.3822.319.8311.322.67
Group 3: Sitagliptin Alone0.030.040.170.030.050.02

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Urinary Glucose Excretion up to 0-72 hr

Pre-dose urine samples were collected from -12 to 0 h for baseline measurement. Subjects was instructed to empty their bladder prior to dosing. Post-dose urine was collected in 4 batches for Groups 1 and 2 at 0 to 12 h, 12 to 24 h, 24 o 36 h, and 36 to 48 h collections. Post-dose urine was collected in batches for Group 3 at 0 to 12 h, 12 to 24 h, 24 to 36 h, 36 to 48 h, 48 to 60 h and 60 to 72 h. (NCT02956044)
Timeframe: up to 0-72 hr

,,,,,
Interventiong (Mean)
0 - 12 hours12 - 24 hours24 - 36 hours36 - 48 hours
Group 1: Bexagliflozin + Metformin26.2622.5719.505.53
Group 1: Bexagliflozin Alone31.5717.3223.948.91
Group 1: Metformin Alone0.020.040.040.02
Group 2: Bexagliflozin + Glimepiride31.0222.5928.469.34
Group 2: Bexagliflozin Alone36.9926.8529.7911.03
Group 2: Glimepiride Alone1.260.040.200.03

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Tmax (Time of Maximum Observed Plasma Concentration)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. Tmax was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionhours (Median)
Metformin PK parametersGlimepiride PK parameters
Group 2: Glimepiride Alone05.5

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Tmax (Time of Maximum Observed Plasma Concentration)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. Tmax was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionhours (Median)
Bexagliflozin PK parametersSitagliptin PK parameters
Group 3: Bexagliflozin + Sitagliptin4.02.5

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Tmax (Time of Maximum Observed Plasma Concentration)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. Tmax was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionhours (Median)
Bexagliflozin PK parametersMetformin PK parameters
Group 1: Bexagliflozin + Metformin3.02.0

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AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. AUC0-inf was estimated for each subject. (NCT02956044)
Timeframe: Up to 72 hours

,,
Interventionh*ng/mL (Geometric Mean)
Bexagliflozin PK parameters
Group 1: Bexagliflozin Alone1154.4
Group 2: Bexagliflozin Alone1204.9
Group 3: Bexagliflozin Alone1011.8

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Cmax (Maximum Observed Plasma Concentration)

Whole venous blood samples of 5 mL were be collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. Pharmacokinetic (PK) blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. Cmax was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionng/mL (Geometric Mean)
Sitagliptin PK parameters
Group 3: Sitagliptin Alone356.6

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Cmax (Maximum Observed Plasma Concentration)

Whole venous blood samples of 5 mL were be collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. Pharmacokinetic (PK) blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. Cmax was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionng/mL (Geometric Mean)
Metformin PK parameters
Group 1: Metformin Alone2067.6

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T1/2 (Apparent Terminal Elimination Half-life)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. T1/2 was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionhours (Geometric Mean)
Bexagliflozin PK parametersSitagliptin PK parameters
Group 3: Bexagliflozin + Sitagliptin13.314.8

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Cmax (Maximum Observed Plasma Concentration)

Whole venous blood samples of 5 mL were be collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. Pharmacokinetic (PK) blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. Cmax was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionng/mL (Geometric Mean)
Glimepiride PK parameters
Group 2: Glimepiride Alone59.9

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Cmax (Maximum Observed Plasma Concentration)

Whole venous blood samples of 5 mL were be collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. Pharmacokinetic (PK) blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. Cmax was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

,,
Interventionng/mL (Geometric Mean)
Bexagliflozin PK parameters
Group 1: Bexagliflozin Alone124.6
Group 2: Bexagliflozin Alone158.6
Group 3: Bexagliflozin Alone117.1

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Tmax (Time of Maximum Observed Plasma Concentration)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. Tmax was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionhours (Median)
Bexagliflozin PK parametersGlimepiride PK parameters
Group 2: Bexagliflozin + Glimepiride6.07.0

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Tmax (Time of Maximum Observed Plasma Concentration)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. Tmax was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionhours (Median)
Sitagliptin PK parameters
Group 3: Sitagliptin Alone2.5

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Tmax (Time of Maximum Observed Plasma Concentration)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. Tmax was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionhours (Median)
Metformin PK parameters
Group 1: Metformin Alone2.5

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Tmax (Time of Maximum Observed Plasma Concentration)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. Tmax was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

,,
Interventionhours (Median)
Bexagliflozin PK parameters
Group 1: Bexagliflozin Alone4.0
Group 2: Bexagliflozin Alone8.0
Group 3: Bexagliflozin Alone3.0

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AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. AUC0-inf was estimated for each subject. (NCT02956044)
Timeframe: Up to 72 hours

Interventionh*ng/mL (Geometric Mean)
Bexagliflozin PK parametersSitagliptin PK parameters
Group 3: Bexagliflozin + Sitagliptin1158.13692.8

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AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. AUC0-inf was estimated for each subject. (NCT02956044)
Timeframe: Up to 72 hours

Interventionh*ng/mL (Geometric Mean)
Bexagliflozin PK parametersMetformin PK parameters
Group 1: Bexagliflozin + Metformin1008.613784.6

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AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. AUC0-inf was estimated for each subject. (NCT02956044)
Timeframe: Up to 72 hours

Interventionh*ng/mL (Geometric Mean)
Bexagliflozin PK parametersGlimepiride PK parameters
Group 2: Bexagliflozin + Glimepiride1162.2633.0

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T1/2 (Apparent Terminal Elimination Half-life)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. T1/2 was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionhours (Geometric Mean)
Bexagliflozin PK parametersMetformin PK parameters
Group 1: Bexagliflozin + Metformin7.810.2

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AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. AUC0-inf was estimated for each subject. (NCT02956044)
Timeframe: Up to 72 hours

Interventionh*ng/mL (Geometric Mean)
Sitagliptin PK parameters
Group 3: Sitagliptin Alone3579.6

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T1/2 (Apparent Terminal Elimination Half-life)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. T1/2 was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionhours (Geometric Mean)
Glimepiride PK parameters
Group 2: Glimepiride Alone7.8

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AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. AUC0-inf was estimated for each subject. (NCT02956044)
Timeframe: Up to 72 hours

Interventionh*ng/mL (Geometric Mean)
Metformin PK parameters
Group 1: Metformin Alone13351.9

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AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. AUC0-inf was estimated for each subject. (NCT02956044)
Timeframe: Up to 72 hours

Interventionh*ng/mL (Geometric Mean)
Glimepiride PK parameters
Group 2: Glimepiride Alone496.1

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T1/2 (Apparent Terminal Elimination Half-life)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. T1/2 was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionhours (Geometric Mean)
Bexagliflozin PK parametersGlimepiride PK parameters
Group 2: Bexagliflozin + Glimepiride7.86.6

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T1/2 (Apparent Terminal Elimination Half-life)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. T1/2 was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionhours (Geometric Mean)
Sitagliptin PK parameters
Group 3: Sitagliptin Alone14.3

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T1/2 (Apparent Terminal Elimination Half-life)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. T1/2 was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionhours (Geometric Mean)
Metformin PK parameters
Group 1: Metformin Alone9.0

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T1/2 (Apparent Terminal Elimination Half-life)

Whole venous blood samples of 5 mL were collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. PK blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. T1/2 was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

,,
Interventionhours (Geometric Mean)
Bexagliflozin PK parameters
Group 1: Bexagliflozin Alone10.3
Group 2: Bexagliflozin Alone8.0
Group 3: Bexagliflozin Alone12.6

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Cmax (Maximum Observed Plasma Concentration)

Whole venous blood samples of 5 mL were be collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. Pharmacokinetic (PK) blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. Cmax was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionng/mL (Geometric Mean)
Bexagliflozin PK parametersSitagliptin PK parameters
Group 3: Bexagliflozin + Sitagliptin148.3351.2

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Cmax (Maximum Observed Plasma Concentration)

Whole venous blood samples of 5 mL were be collected from a peripheral vein in each period at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h post-dose for Group 1 and 2. Pharmacokinetic (PK) blood samples were collected at pre-dose and at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose for Group 3. Plasma was obtained from centrifugation, frozen and analyzed. Cmax was obtained directly from experimental observations. (NCT02956044)
Timeframe: Up to 72 hours

Interventionng/mL (Geometric Mean)
Bexagliflozin PK parametersMetformin PK parameters
Group 1: Bexagliflozin + Metformin135.51965.2

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Change in Fasting Total Cholesterol - Ratio to Baseline

Change in fasting total cholesterol from baseline (week 0) to week 30 is presented as ratio to baseline. Fasting total cholesterol was measured in mmol/L. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of fasting total cholesterol (Geometric Mean)
Semaglutide 0.5 mg0.95
Semaglutide 1.0 mg0.95
Sitagliptin1.00

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Change in Calcitonin - Ratio to Baseline

Change in calcitonin from baseline (week -2) to week 30 is presented as ratio to baseline. Calcitonin was measured in nanogram per liter (ng/L). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week -2, week 30

InterventionRatio of calcitonin (Geometric Mean)
Semaglutide 0.5 mg0.96
Semaglutide 1.0 mg1.00
Sitagliptin0.96

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Change in Clinical Evaluation: Pulse

Change in pulse from baseline (week 0) to week 30 is presented. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionBeats per minute (beats/min) (Mean)
Semaglutide 0.5 mg3.7
Semaglutide 1.0 mg3.7
Sitagliptin0.2

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Change in Fasting Glucagon - Ratio to Baseline

Change in fasting glucagon from baseline (week 0) to week 30 is presented as ratio to baseline. Fasting glucagon was measured in picogram per mililiter (pg/mL). Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of fasting glucagon (Geometric Mean)
Semaglutide 0.5 mg0.89
Semaglutide 1.0 mg0.89
Sitagliptin0.93

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Change in Fasting HDL Cholesterol - Ratio to Baseline

Change in fasting high density lipoprotein (HDL) from baseline (week 0) to week 30 is presented as ratio to baseline. Fasting HDL was measured in mmol/L. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of fasting HDL cholesterol (Geometric Mean)
Semaglutide 0.5 mg1.00
Semaglutide 1.0 mg1.02
Sitagliptin1.01

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Change in Fasting HOMA-B (Beta-cell Function) - Ratio to Baseline

Change in fasting HOMA-B (homeostasis model assessment beta-cell function) from baseline (week 0) to week 30 is presented as ratio to baseline. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of fasting HOMA-B (Geometric Mean)
Semaglutide 0.5 mg1.81
Semaglutide 1.0 mg1.95
Sitagliptin1.25

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Change in Fasting HOMA-IR (Insulin Resistence) - Ratio to Baseline

Change in fasting HOMA-IR (homeostasis model assessment insulin resistence) from baseline (week 0) to week 30 is presented as ratio to baseline. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of fasting HOMA-IR (Geometric Mean)
Semaglutide 0.5 mg0.81
Semaglutide 1.0 mg0.74
Sitagliptin0.90

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Change in Fasting Insulin - Ratio to Baseline

Change in fasting insulin from baseline (week 0) to week 30 is presented as ratio to baseline. Fasting insulin was measured in picomoles per liter (pmol/L). Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of fasting insulin (Geometric Mean)
Semaglutide 0.5 mg1.06
Semaglutide 1.0 mg1.03
Sitagliptin1.01

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Change in Fasting LDL Cholesterol - Ratio to Baseline

Change in fasting low density lipoprotein (LDL) from baseline (week 0) to week 30 is presented as ratio to baseline. Fasting LDL was measured in mmol/L. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of fasting LDL cholesterol (Geometric Mean)
Semaglutide 0.5 mg0.97
Semaglutide 1.0 mg0.99
Sitagliptin1.01

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Change in Fasting Plasma Glucose (FPG)

Change from baseline (week 0) to week 30 in FPG was evaluated. Results are based on the 'on-treatment without rescue medication' observation period which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionMillimoles per liter (mmol/L) (Mean)
Semaglutide 0.5 mg-2.18
Semaglutide 1.0 mg-2.62
Sitagliptin-1.0

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Change in Fasting Proinsulin - Ratio to Baseline

Change in fasting proinsulin from baseline (week 0) to week 30 is presented as ratio to baseline. Fasting proinsulin was measured in picomole per liter (pmol/L). Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of fasting proinsulin (Geometric Mean)
Semaglutide 0.5 mg0.68
Semaglutide 1.0 mg0.59
Sitagliptin0.81

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Change in Fasting Proinsulin/Insulin Ratio - Ratio to Baseline

Change in fasting proinsulin/insulin ratio from baseline (week 0) to week 30 is presented as ratio to baseline. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of fasting proinsulin/insulin (Geometric Mean)
Semaglutide 0.5 mg0.63
Semaglutide 1.0 mg0.57
Sitagliptin0.80

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Change in Fasting Triglycerides - Ratio to Baseline

Change in fasting triglycerides from baseline (week 0) to week 30 is presented as ratio to baseline. Triglycerides was measured in mmol/L. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of fasting triglycerides (Geometric Mean)
Semaglutide 0.5 mg0.86
Semaglutide 1.0 mg0.81
Sitagliptin0.93

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Change in Fasting VLDL Cholesterol - Ratio to Baseline

Change in fasting very low density lipoprotein (VLDL) from baseline (week 0) to week 30 is presented as ratio to baseline. Fasting VLDL was measured in mmol/L. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of fasting VLDL cholesterol (Geometric Mean)
Semaglutide 0.5 mg0.86
Semaglutide 1.0 mg0.82
Sitagliptin0.93

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Change in Free Fatty Acids - Ratio to Baseline

Change in free fatty acids from baseline (week 0) to week 30 is presented as ratio to baseline. Free fatty acids was measured in mmol/L. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of free fatty acids (Geometric Mean)
Semaglutide 0.5 mg0.78
Semaglutide 1.0 mg0.78
Sitagliptin0.87

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Change in Haematological Parameter: Haematocrit - Ratio to Baseline

Change in haematocrit from baseline (week 0) to week 30 is presented as ratio to baseline. Haematocrit was measured in percentage. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of haematocrit (Geometric Mean)
Semaglutide 0.5 mg1.00
Semaglutide 1.0 mg1.00
Sitagliptin1.00

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Change in Haematological Parameter: Haemoglobin - Ratio to Baseline

Change in haemoglobin from baseline (week 0) to week 30 is presented as ratio to baseline. Haemoglobin was measured in mmol/L. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of haemoglobin (Geometric Mean)
Semaglutide 0.5 mg1.00
Semaglutide 1.0 mg1.00
Sitagliptin1.00

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Change in Hematological Parameter (Differential Cell Count of Leukocytes): Basophils - Ratio to Baseline

Change in basophils from baseline (week 0) to week 30 is presented as ratio to baseline. Basophils were measured in percentage. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of basophils (Geometric Mean)
Semaglutide 0.5 mg0.91
Semaglutide 1.0 mg0.80
Sitagliptin0.83

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Change in Hematological Parameter (Differential Cell Count of Leukocytes): Eosinophils - Ratio to Baseline

Change in eosinophils from baseline (week 0) to week 30 is presented as ratio to baseline. Eosinophils were measured in percentage. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of eosinophils (Geometric Mean)
Semaglutide 0.5 mg0.98
Semaglutide 1.0 mg1.04
Sitagliptin1.00

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Change in Hematological Parameter (Differential Cell Count of Leukocytes): Lymphocytes - Ratio to Baseline

Change in lymphocytes from baseline (week 0) to week 30 is presented as ratio to baseline. Lymphocytes were measured in percentage. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of lymphocytes (Geometric Mean)
Semaglutide 0.5 mg1.01
Semaglutide 1.0 mg0.98
Sitagliptin0.97

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Change in Hematological Parameter (Differential Cell Count of Leukocytes): Monocytes - Ratio to Baseline

Change in monocytes from baseline (week 0) to week 30 is presented as ratio to baseline. Monocytes were measured in percentage. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of monocytes (Geometric Mean)
Semaglutide 0.5 mg0.96
Semaglutide 1.0 mg0.98
Sitagliptin1.04

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Change in Hematological Parameter (Differential Cell Count of Leukocytes): Neutrophils - Ratio to Baseline

Change in neutrophils from baseline (week 0) to week 30 is presented as ratio to baseline. Neutrophils were measured in percentage. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of neutrophils (Geometric Mean)
Semaglutide 0.5 mg1.01
Semaglutide 1.0 mg1.02
Sitagliptin1.02

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Change in Hematological Parameter: Erythrocytes - Ratio to Baseline

Change in erythrocytes from baseline (week 0) to week 30 is presented as ratio to baseline. Erythrocytes were measured in 10^12 cells per liter. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of erythrocytes (Geometric Mean)
Semaglutide 0.5 mg0.99
Semaglutide 1.0 mg0.99
Sitagliptin0.99

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Change in Hematological Parameter: Leukocytes - Ratio to Baseline

Change in leukocytes from baseline (week 0) to week 30 is presented as ratio to baseline. Leukocytes were measured in 10^9 cells per liter. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of leukocytes (Geometric Mean)
Semaglutide 0.5 mg1.03
Semaglutide 1.0 mg1.01
Sitagliptin1.08

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Change in Hematological Parameter: Thrombocytes - Ratio to Baseline

Change in thrombocytes from baseline (week 0) to week 30 is presented as ratio to baseline. Thrombocytes was measured in 10^9 cells per liter. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of thrombocytes (Geometric Mean)
Semaglutide 0.5 mg1.01
Semaglutide 1.0 mg1.01
Sitagliptin0.99

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Change in High-sensitivity CRP - Ratio to Baseline

Change in high-sensitivity C-reactive protein (CRP) from baseline (week 0) to week 30 is presented as ratio to baseline. High-sensitivity CRP was measured in mg/L. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of high-sensitivity CRP (Geometric Mean)
Semaglutide 0.5 mg0.73
Semaglutide 1.0 mg0.64
Sitagliptin0.96

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Change in Self-measured Plasma Glucose (SMPG) - Mean 7-point Profile

Change from baseline (week 0) to week 30 in SMPG mean 7-point profile was evaluated. SMPG was recorded at the following 7 time points: before breakfast, 90 minutes after start of breakfast, before lunch, 90 minutes after start of lunch, before dinner, 90 minutes after dinner and at bedtime. Mean 7-point profile was defined as the area under the profile, calculated using the trapezoidal method, divided by the measurement time. Results are based on the 'on-treatment without rescue medication' observation period which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionMillimoles per liter (mmol/L) (Mean)
Semaglutide 0.5 mg-2.5
Semaglutide 1.0 mg-3.3
Sitagliptin-1.6

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Change in Self-measured Plasma Glucose (SMPG) - Mean Postprandial Increment Over All Meals

Change from baseline (week 0) to week 30 in SMPG mean postprandial increment over all meals was evaluated. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionMillimoles per liter (mmol/L) (Mean)
Semaglutide 0.5 mg-1.0
Semaglutide 1.0 mg-1.2
Sitagliptin-0.7

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Change in Urinalysis Parameter - UACR-ratio to Baseline

Change in urin albumin to creatinine ratio (UACR) from baseline (week 0) to week 30 is presented as ratio to baseline. UACR was measured in milligram/millimole (mg/mmol). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of UACR (Geometric Mean)
Semaglutide 0.5 mg0.77
Semaglutide 1.0 mg0.69
Sitagliptin0.89

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Change in Waist Circumference

Change in waist circumference from baseline (week 0) to week 30 was measured. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionCentimeter (cm) (Mean)
Semaglutide 0.5 mg-2.7
Semaglutide 1.0 mg-4.0
Sitagliptin-0.7

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Number of Treatment Emergent Severe or Blood Glucose (BG) Confirmed Symptomatic Hypoglycaemic Episodes

Hypoglycaemic episodes are defined as treatment-emergent if the onset of the episode occurs within the on-treatment observation period. Severe or BG-confirmed symptomatic hypoglycaemia is an episode that is severe according to the American Diabetes Association classification or blood glucose-confirmed by a plasma glucose value <3.1 mmol/L (56 mg/dL) with symptoms consistent with hypoglycaemia. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0 to week 30

InterventionEpisodes (Number)
Semaglutide 0.5 mg3
Semaglutide 1.0 mg7
Sitagliptin5

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Total Number of Treatment Emergent Adverse Events

A treatment emergent adverse event (TEAE) is defined as an adverse event with onset in the on-treatment observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0 to week 30

InterventionEvents (Number)
Semaglutide 0.5 mg729
Semaglutide 1.0 mg788
Sitagliptin596

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Anti-semaglutide Antibody Levels

This outcome measure is only applicable for the semaglutide arms. Anti-semaglutide antibody level at week 30 and week 35 are presented. Antibody levels were measured in percentage of bound radioactivity-labelled semaglutide/total added radioactivity-labelled semaglutide (%B/T; B =Bound, T = Total). Evaluation was based on 'in trial' observation period, which is the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication or premature treatment discontinuation. (NCT03061214)
Timeframe: week 30, week 35

Intervention%B/T (Mean)
At week 30At week 35
Semaglutide 1.0 mg2.83.3

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Change in Blood Pressure (Systolic and Diastolic Blood Pressure)

Change from baseline (week 0) to week 30 in systolic blood pressure and diastolic blood pressure were evaluated. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

,,
InterventionMillimeters of mercury (mmHg) (Mean)
Systolic blood pressureDiastolic blood pressure
Semaglutide 0.5 mg-3.4-0.7
Semaglutide 1.0 mg-6.5-1.5
Sitagliptin-0.9-0.8

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Change in HbA1c

Change from baseline (week 0) to week 30 in glycosylated haemoglobin (HbA1c) was evaluated. Results are based on the 'on-treatment without rescue medication' observation period and 'in trial' observation period. 'On-treatment without rescue medication' observation period: started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. 'In-trial' observation period: started when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication or premature treatment discontinuation. (NCT03061214)
Timeframe: Week 0, week 30

,,
InterventionPercentage of glycosylated haemoglobin (Mean)
On-treatment without rescue medication obs. periodIn-trial observation period
Semaglutide 0.5 mg-1.5-1.5
Semaglutide 1.0 mg-1.8-1.7
Sitagliptin-1.0-0.9

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Change in Patient Reported Outcome Questionnaire: DTSQs Score

"Change from baseline (week 0) in Diabetes Treatment Satisfaction Questionnaire (DTSQs) was evaluated at week 30. The DTSQs items are scored on a 7-point graded response scale ranging from 6 to 0. Higher scores indicate higher levels of treatment satisfaction for DTSQs items 3 -8. For items 1 and 2 a higher score indicates a higher patient perceived experience of high blood sugars and low blood sugars, respectively. Thus, lower scores indicate a perception of blood glucose levels being none of the time unacceptably high (item 1) or low (item 2). The domain score of total treatment satisfaction (total treatment satisfaction score) was computed by adding the six items scores 3-8. The score ranges 0-36. A higher treatment satisfaction score indicates a higher level of treatment satisfaction. Results are based on the 'on-treatment without rescue medication' observation period." (NCT03061214)
Timeframe: Week 0, week 30

,,
InterventionScore on a scale (Mean)
1) Feeling of unacceptably high blood sugars2) Feeling of unacceptably low blood sugars3) Satisfaction with treatment4) Convenience of treatment5) Flexibility of current treatment6) Satisfaction with understanding of diabetes7) Recommending treatment to others8) Satisfaction to continue with present treatmentTotal Diabetic Treatment Satisfaction score
Semaglutide 0.5 mg-1.4-0.11.10.70.70.90.90.74.9
Semaglutide 1.0 mg-1.6-0.31.30.70.80.80.90.75.1
Sitagliptin-1.0-0.10.70.50.40.70.70.63.7

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Change in Patient Reported Outcome Questionnaire: SF-36v2™ Score

Short Form (SF)-36 is a 36-item patient-reported survey that measures patient's overall health-related quality of life (HRQoL). SF-36v2™ (acute version) questionnaire measured 8 domains of functional health & well-being and 2 component summary scores (physical component summary-PCS and mental component summary-MCS). The 0-100 scale scores (where higher scores indicated a better HRQoL) from the SF-36 were converted to norm-based scores to enable a direct interpretation in relation to the distribution of the scores in the 2009 U.S. general population. In the metric of norm-based scores, 50 and 10 corresponds to the mean and standard deviation respectively of the 2009 U.S. general population. Change from baseline (week 0) in the domain scores and component summary (PCS and MCS) scores were evaluated at weeks 30. A positive change score indicates an improvement since baseline. Results are based on the data from the 'on-treatment without rescue medication' observation period. (NCT03061214)
Timeframe: Week 0, week 30

,,
InterventionScore on a scale (Mean)
Physical component summary (PCS)Physical functioningRole-physicalBodily painGeneral healthMental component summary (MCS)Social functioningRole-emotionalVitalityMental health
Semaglutide 0.5 mg1.30.61.40.63.31.21.31.31.20.9
Semaglutide 1.0 mg1.10.90.20.42.90.5-0.40.91.40.4
Sitagliptin0.0-0.3-0.00.02.21.50.81.01.11.1

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Occurence of Anti-semaglutide Antibodies Cross Reacting With Endogenous GLP-1 (Yes/no)

This outcome measure is only applicable for the semaglutide arms. Development of anti-semaglutide antibodies cross reacting with endogenous glucagon-like peptide-1 (GLP-1) was evaluated in participants. The number of participants who were positive/ negative for anti-semaglutide antibodies cross reacting with endogenous GLP-1 are presented. Evaluation was based on in-trial observation period, which is the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication or premature treatment discontinuation. (NCT03061214)
Timeframe: Week 35

,
InterventionParticipants (Count of Participants)
Yes (positive for antibody)No (negative for antibody)
Semaglutide 0.5 mg0262
Semaglutide 1.0 mg1263

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Occurence of Cross Reacting Antibodies With in Vitro Neutralising Effect to Endogenous GLP-1 (Yes/no)

This outcome measure is only applicable for the semaglutide arms. Development of cross reacting antibodies with in-vitro neutralising effect to endogenous glucagon-like peptide-1 (GLP-1) was evaluated in participants. The number of participants who were positive/ negative for anti-semaglutide antibodies with in vitro neutralising effect to endogenous GLP-1 are presented. Evaluation was based on in-trial observation period, which is the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication or premature treatment discontinuation. (NCT03061214)
Timeframe: Week 35

,
InterventionParticipants (Count of Participants)
Yes (positive for antibody)No (negative for antibody)
Semaglutide 0.5 mg0262
Semaglutide 1.0 mg0264

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Percentage of Participants That Achieved (Yes/no): Body Weight Loss ≥10%

Percentage of participants losing ≥10% of baseline body weight (yes/no) is presented. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 30

,,
InterventionPercentage of participants (Number)
YesNo
Semaglutide 0.5 mg9.790.3
Semaglutide 1.0 mg17.282.8
Sitagliptin0.499.6

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Percentage of Participants That Achieved (Yes/no): Body Weight Loss ≥5%

Percentage of participants losing ≥5% of baseline body weight (yes/no) is presented. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 30

,,
InterventionPercentage of participants (Number)
YesNo
Semaglutide 0.5 mg36.663.4
Semaglutide 1.0 mg52.747.3
Sitagliptin5.994.1

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Percentage of Participants That Achieved (Yes/no): HbA1c <7.0% (53 mmol/Mol) Without Severe or Blood Glucose (BG)-Confirmed Symptomatic Hypoglycaemia and no Weight Gain

Severe or blood glucose (BG)-confirmed symptomatic hypoglycaemia is an episode that is severe according to the American Diabetes Association classification or blood glucose-confirmed by a plasma glucose value <3.1 mmol/L (56 milligrams per deciliter [mg/dL]) with symptoms consistent with hypoglycaemia. Percentage of participants who achieved HbA1c below 7.0% (53 mmol/mol) without severe or blood glucose confirmed symptomatic hypoglycaemia episodes and no weight gain (yes/no) is presented. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 30

,,
InterventionPercentage of participants (Number)
YesNo
Semaglutide 0.5 mg66.034.0
Semaglutide 1.0 mg76.923.1
Sitagliptin33.766.3

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Percentage of Participants Who Achieved HbA1c <7.0% (53 mmol/Mol), ADA Target, (Yes/no)

Percentage of participants who achieved HbA1c < 7.0% (53 millimoles per mole [mmol/mol]), American Diabetes Association (ADA) target (yes/no) is presented. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 30

,,
InterventionPercentage of participants (Number)
YesNo
Semaglutide 0.5 mg74.525.5
Semaglutide 1.0 mg84.016.0
Sitagliptin49.650.4

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Percentage of Participants Who Achieved HbA1c ≤6.5% (48 mmol/Mol), AACE Target, (Yes/no)

Percentage of participants who achieved HbA1c ≤6.5% (48 millimoles per mole [mmol/mol]), American Association of Clinical Endocrinologists (AACE) target (yes/no) is presented. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 30

,,
InterventionPercentage of participants (Number)
YesNo
Semaglutide 0.5 mg60.439.6
Semaglutide 1.0 mg70.629.4
Sitagliptin31.668.4

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Change in Clinical Evaluation: ECG

The electrocardiogram (ECG) was assessed by the investigator and categorised as normal, abnormal not clinically significant (NCS) or abnormal clinically significant (CS). Number of participants in each ECG category at baseline and week 30 are presented. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionParticipants (Count of Participants)
At week 072522679At week 072522680At week 072522681At week 3072522679At week 3072522681At week 3072522680
Abnormal, CSNormalAbnormal, NCS
Semaglutide 0.5 mg191
Semaglutide 1.0 mg196
Sitagliptin185
Semaglutide 0.5 mg72
Semaglutide 1.0 mg68
Sitagliptin76
Semaglutide 0.5 mg23
Semaglutide 1.0 mg26
Sitagliptin29
Semaglutide 0.5 mg162
Semaglutide 1.0 mg172
Sitagliptin167
Semaglutide 0.5 mg81
Semaglutide 1.0 mg74
Sitagliptin85
Semaglutide 0.5 mg19
Semaglutide 1.0 mg18
Sitagliptin26

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Change in Clinical Evaluation: Eye Examinations

Eye examination was performed by the investigator and the results of the examination were interpreted for each eye (left/right) are categorised as normal, abnormal not clinically significant (NCS) or abnormal clinically significant (CS). Number of participants in each category at baseline (week 0) and at week 30 are presented. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionParticipants (Count of Participants)
At week 0, Left eye72522680At week 0, Left eye72522681At week 0, Left eye72522679At week 30, Left eye72522680At week 30, Left eye72522681At week 30, Left eye72522679At week 0, Right eye72522680At week 0, Right eye72522681At week 0, Right eye72522679At week 52, Right eye72522681At week 52, Right eye72522679At week 52, Right eye72522680
Abnormal, NCSAbnormal, CSNormal
Semaglutide 0.5 mg202
Semaglutide 1.0 mg222
Sitagliptin202
Semaglutide 0.5 mg40
Semaglutide 1.0 mg32
Sitagliptin47
Semaglutide 0.5 mg44
Semaglutide 1.0 mg36
Sitagliptin41
Semaglutide 0.5 mg162
Semaglutide 1.0 mg184
Sitagliptin174
Semaglutide 0.5 mg26
Semaglutide 1.0 mg18
Sitagliptin32
Semaglutide 0.5 mg42
Semaglutide 0.5 mg210
Sitagliptin201
Semaglutide 0.5 mg37
Semaglutide 1.0 mg31
Semaglutide 0.5 mg39
Semaglutide 1.0 mg37
Sitagliptin42
Semaglutide 0.5 mg161
Semaglutide 1.0 mg180
Sitagliptin172
Semaglutide 0.5 mg27
Semaglutide 1.0 mg19
Sitagliptin31
Semaglutide 1.0 mg34
Sitagliptin43

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Change in Physical Examination

Physical examination parameters are categorised as general appearance; nervous system (central and peripheral); cardiovascular system; gastrointestinal system; skin; respiratory system; lymph node palpation; thyroid gland; left foot; right foot; left leg and right leg. The number of participants assessed as normal, abnormal not clinically significant (NCS) and abnormal clinically significant (CS) at baseline (week -2) and week 30 are presented. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week -2, week 30

InterventionParticipants (Count of Participants)
At week -2, General Appearance72522680At week -2, General Appearance72522681At week -2, General Appearance72522679At week 30, General Appearance72522679At week 30, General Appearance72522680At week 30, General Appearance72522681At week -2, Nervous System72522679At week -2, Nervous System72522681At week -2, Nervous System72522680At week 30, Nervous System72522681At week 30, Nervous System72522679At week 30, Nervous System72522680At week -2, Cardiovascular System72522680At week -2, Cardiovascular System72522681At week -2, Cardiovascular System72522679At week 30, Cardiovascular System72522680At week 30, Cardiovascular System72522681At week 30, Cardiovascular System72522679At week -2, Gastrointestinal System72522681At week -2, Gastrointestinal System72522679At week -2, Gastrointestinal System72522680At week 30, Gastrointestinal System72522679At week 30, Gastrointestinal System72522680At week 30, Gastrointestinal System72522681At week -2, Musculoskeletal System72522681At week -2, Musculoskeletal System72522679At week -2, Musculoskeletal System72522680At week 30, Musculoskeletal System72522681At week 30, Musculoskeletal System72522679At week 30, Musculoskeletal System72522680At week -2, Skin72522680At week -2, Skin72522681At week -2, Skin72522679At week 30, Skin72522681At week 30, Skin72522679At week 30, Skin72522680At week -2, Head,Ears,Eyes,Nose, Throat, Neck72522681At week -2, Head,Ears,Eyes,Nose, Throat, Neck72522679At week -2, Head,Ears,Eyes,Nose, Throat, Neck72522680At week 30, Head,Ears,Eyes,Nose, Throat, Neck72522680At week 30, Head,Ears,Eyes,Nose, Throat, Neck72522681At week 30, Head,Ears,Eyes,Nose, Throat, Neck72522679At week -2, Respiratory System72522679At week -2, Respiratory System72522680At week -2, Respiratory System72522681At week 30, Respiratory System72522679At week 30, Respiratory System72522680At week 30, Respiratory System72522681At week -2, Lymph Node Palpation72522679At week -2, Lymph Node Palpation72522680At week -2, Lymph Node Palpation72522681At week 30, Lymph Node Palpation72522679At week 30, Lymph Node Palpation72522680At week 30, Lymph Node Palpation72522681At week -2, Thyroid Gland72522681At week -2, Thyroid Gland72522679At week -2, Thyroid Gland72522680At week 30, Thyroid Gland72522679At week 30, Thyroid Gland72522680At week 30, Thyroid Gland72522681
NormalAbnormal, NCSAbnormal, CS
Semaglutide 0.5 mg282
Semaglutide 1.0 mg283
Sitagliptin281
Semaglutide 0.5 mg3
Semaglutide 1.0 mg7
Sitagliptin8
Sitagliptin1
Semaglutide 0.5 mg252
Sitagliptin270
Sitagliptin5
Semaglutide 0.5 mg277
Semaglutide 1.0 mg287
Sitagliptin279
Sitagliptin3
Semaglutide 0.5 mg247
Sitagliptin268
Semaglutide 0.5 mg4
Semaglutide 0.5 mg276
Semaglutide 1.0 mg281
Sitagliptin278
Semaglutide 1.0 mg6
Sitagliptin10
Semaglutide 1.0 mg3
Sitagliptin2
Semaglutide 0.5 mg245
Semaglutide 1.0 mg246
Sitagliptin265
Semaglutide 0.5 mg8
Semaglutide 1.0 mg4
Semaglutide 1.0 mg285
Sitagliptin280
Semaglutide 1.0 mg5
Semaglutide 1.0 mg0
Sitagliptin0
Semaglutide 0.5 mg251
Semaglutide 1.0 mg250
Sitagliptin264
Sitagliptin11
Semaglutide 0.5 mg281
Sitagliptin282
Semaglutide 1.0 mg247
Semaglutide 1.0 mg252
Sitagliptin254
Semaglutide 0.5 mg28
Semaglutide 1.0 mg37
Sitagliptin29
Semaglutide 0.5 mg6
Semaglutide 0.5 mg226
Semaglutide 1.0 mg217
Sitagliptin240
Semaglutide 0.5 mg25
Semaglutide 1.0 mg33
Sitagliptin31
Semaglutide 0.5 mg5
Semaglutide 0.5 mg273
Sitagliptin277
Semaglutide 0.5 mg12
Sitagliptin7
Semaglutide 1.0 mg2
Sitagliptin6
Semaglutide 1.0 mg244
Sitagliptin263
Semaglutide 0.5 mg9
Semaglutide 0.5 mg287
Semaglutide 1.0 mg288
Sitagliptin287
Semaglutide 0.5 mg0
Sitagliptin274
Semaglutide 0.5 mg284
Semaglutide 1.0 mg284
Sitagliptin285
Sitagliptin4
Semaglutide 1.0 mg1
Semaglutide 0.5 mg255
Sitagliptin271
Semaglutide 0.5 mg280
Sitagliptin9
Semaglutide 0.5 mg253
Semaglutide 1.0 mg249
Semaglutide 0.5 mg2
Semaglutide 0.5 mg1

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Change in Urinalysis Parameter: Erythrocytes

Erythrocytes in urine was assessed by the investigator and categorised as negative, trace, small, moderate, large. Number of participants in each category at baseline (week 0) and week 30 are presented. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionParticipants (Count of Participants)
At week 072522680At week 072522679At week 072522681At week 3072522679At week 3072522680At week 3072522681
ModerateLargeNegativeTraceSmall
Semaglutide 0.5 mg251
Semaglutide 1.0 mg250
Sitagliptin253
Semaglutide 0.5 mg25
Semaglutide 1.0 mg20
Sitagliptin19
Semaglutide 0.5 mg5
Semaglutide 0.5 mg1
Semaglutide 1.0 mg3
Semaglutide 0.5 mg4
Semaglutide 1.0 mg8
Sitagliptin3
Semaglutide 0.5 mg258
Semaglutide 1.0 mg259
Sitagliptin252
Semaglutide 0.5 mg18
Semaglutide 1.0 mg13
Sitagliptin22
Semaglutide 1.0 mg5
Sitagliptin9
Semaglutide 0.5 mg2
Sitagliptin1
Semaglutide 1.0 mg6

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Change in Urinalysis Parameter: Glucose

Glucose in urine was assessed by the investigator and categorised as negative, [100-249], [250-499], [500-999] and >= 1000. Number of participants in each category at baseline (week 0) and week 30 are presented. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionParticipants (Count of Participants)
At week 072522679At week 072522681At week 072522680At week 3072522679At week 3072522680At week 3072522681
500-999Negative100-249250-499>= 1000
Semaglutide 0.5 mg189
Semaglutide 1.0 mg187
Sitagliptin176
Semaglutide 0.5 mg28
Semaglutide 1.0 mg27
Sitagliptin42
Semaglutide 0.5 mg12
Semaglutide 1.0 mg20
Sitagliptin25
Semaglutide 0.5 mg20
Semaglutide 1.0 mg25
Sitagliptin21
Semaglutide 0.5 mg37
Semaglutide 1.0 mg30
Sitagliptin23
Semaglutide 0.5 mg244
Semaglutide 1.0 mg258
Sitagliptin233
Semaglutide 0.5 mg7
Semaglutide 1.0 mg15
Semaglutide 0.5 mg10
Semaglutide 1.0 mg5
Sitagliptin5
Semaglutide 0.5 mg11
Semaglutide 1.0 mg4
Sitagliptin12
Semaglutide 0.5 mg14
Semaglutide 1.0 mg7
Sitagliptin14

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Change in Urinalysis Parameter: Ketones

Ketones in urine was assessed by the investigator and categorised as negative, trace, 15-39, 40-79, Approximately 80, >= 80. Number of participants in each category at baseline (week 0) and week 30 are presented. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionParticipants (Count of Participants)
At week 072522681At week 072522679At week 072522680At week 3072522681At week 3072522679At week 3072522680
NegativeTrace15-3940- 79Approximately 80>=80
Semaglutide 0.5 mg267
Semaglutide 1.0 mg268
Sitagliptin274
Semaglutide 0.5 mg11
Semaglutide 1.0 mg17
Sitagliptin9
Semaglutide 0.5 mg8
Sitagliptin3
Semaglutide 1.0 mg1
Sitagliptin0
Sitagliptin1
Semaglutide 0.5 mg268
Semaglutide 1.0 mg274
Semaglutide 0.5 mg12
Semaglutide 1.0 mg12
Sitagliptin11
Semaglutide 0.5 mg6
Semaglutide 1.0 mg3
Semaglutide 0.5 mg0
Semaglutide 1.0 mg0

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Change in Urinalysis Parameter: pH

pH in urine was assessed by the investigator and categorised as 5, 5.5, 6, 6.5, 7, 7.5, 8, 8.5, 9, >=9. Number of participants in each category at baseline (week 0) and week 30 are presented. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionParticipants (Count of Participants)
At week 072522679At week 072522680At week 072522681At week 3072522681At week 3072522680At week 3072522679
66.577.588.5>= 955.5
Semaglutide 0.5 mg17
Semaglutide 1.0 mg15
Sitagliptin14
Semaglutide 0.5 mg220
Semaglutide 1.0 mg214
Sitagliptin222
Semaglutide 0.5 mg31
Sitagliptin33
Semaglutide 0.5 mg13
Semaglutide 1.0 mg14
Sitagliptin15
Semaglutide 0.5 mg3
Semaglutide 1.0 mg4
Semaglutide 1.0 mg2
Semaglutide 1.0 mg0
Sitagliptin1
Sitagliptin0
Semaglutide 0.5 mg16
Semaglutide 1.0 mg21
Sitagliptin30
Semaglutide 0.5 mg209
Semaglutide 1.0 mg194
Sitagliptin201
Semaglutide 0.5 mg33
Semaglutide 1.0 mg40
Sitagliptin24
Semaglutide 0.5 mg24
Semaglutide 1.0 mg30
Sitagliptin22
Semaglutide 0.5 mg2
Semaglutide 1.0 mg3
Semaglutide 1.0 mg1
Sitagliptin5
Semaglutide 0.5 mg1
Semaglutide 0.5 mg0

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Change in Urinalysis Parameter: Protein

Protein in urine was assessed by the investigator and categorised as negative, trace, 30-99, 100-299, Approximately 300, >=300. Number of participants in each category at baseline (week 0) and week 30 are presented. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionParticipants (Count of Participants)
At week 072522679At week 072522681At week 072522680At week 3072522679At week 3072522680At week 3072522681
100-299Approximately 300>=300NegativeTrace30-99
Semaglutide 0.5 mg231
Semaglutide 1.0 mg233
Sitagliptin235
Semaglutide 0.5 mg31
Semaglutide 1.0 mg32
Sitagliptin30
Semaglutide 0.5 mg17
Semaglutide 1.0 mg18
Sitagliptin15
Semaglutide 0.5 mg6
Semaglutide 1.0 mg4
Sitagliptin6
Semaglutide 1.0 mg0
Sitagliptin0
Semaglutide 0.5 mg1
Semaglutide 1.0 mg2
Sitagliptin1
Semaglutide 0.5 mg247
Semaglutide 1.0 mg248
Sitagliptin239
Semaglutide 0.5 mg22
Semaglutide 1.0 mg28
Sitagliptin24
Semaglutide 0.5 mg13
Semaglutide 1.0 mg9
Sitagliptin12
Semaglutide 0.5 mg4
Sitagliptin11
Semaglutide 0.5 mg0

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Occurence of Anti-semaglutide Antibodies (Yes/no)

This outcome measure is only applicable for the semaglutide arms. Development of anti-semaglutide antibodies was evaluated in participants during the study. The number of participants who were positive/ negative for anti-semaglutide antibodies were presented. Evaluation was based on 'in trial' observation period, which is the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication or premature treatment discontinuation. (NCT03061214)
Timeframe: Week 0, week 16, week 30, week 35

InterventionParticipants (Count of Participants)
At week 072522679At week 072522680At week 1672522679At week 1672522680At week 3072522679At week 3072522680At week 3572522680At week 3572522679
Yes (positive for antibody)No (negative for antibody)
Semaglutide 0.5 mg0
Semaglutide 1.0 mg1
Semaglutide 0.5 mg285
Semaglutide 1.0 mg288
Semaglutide 0.5 mg1
Semaglutide 1.0 mg0
Semaglutide 0.5 mg284
Semaglutide 1.0 mg290
Semaglutide 1.0 mg2
Semaglutide 0.5 mg257
Semaglutide 1.0 mg3
Semaglutide 0.5 mg262
Semaglutide 1.0 mg261

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Occurence of Anti-semaglutide Antibodies With In-vitro Neutralising Effect (Yes/no)

This outcome measure is only applicable for the semaglutide arms. Development of anti-semaglutide antibodies with in-vitro neutralising effect was evaluated in participants during the study. The number of participants who were positive/ negative for anti-semaglutide antibodies with in vitro neutralising effect are presented. Evaluation was based on in-trial observation period, which is the time period from when a participant was randomised until the final scheduled visit, including any period after initiation of rescue medication or premature treatment discontinuation. (NCT03061214)
Timeframe: Week 0, week 16, week 30, week 35

InterventionParticipants (Count of Participants)
At week 072522679At week 072522680At week 1672522679At week 1672522680At week 3072522680At week 3072522679At week 3572522679At week 3572522680
Yes (positive for antibody)No (negative for antibody)
Semaglutide 0.5 mg0
Semaglutide 1.0 mg0
Semaglutide 0.5 mg285
Semaglutide 1.0 mg289
Semaglutide 1.0 mg290
Semaglutide 0.5 mg257
Semaglutide 1.0 mg263
Semaglutide 0.5 mg262
Semaglutide 1.0 mg264

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Change in Fasting C-peptide - Ratio to Baseline

Change in fasting C-peptide from baseline (week 0) to week 30 is presented as ratio to baseline. C-peptide was measured in nanomoles per liter (nmol/L). Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of fasting C-peptide (Geometric Mean)
Semaglutide 0.5 mg1.08
Semaglutide 1.0 mg1.05
Sitagliptin1.0

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Participants With Severe or Blood Glucose (BG) Confirmed Symptomatic Hypoglycaemic Episodes

Number of participants with treatment emergent severe or blood glucose-confirmed symptomatic hypoglycaemic episodes. Hypoglycaemic episodes defined as treatment-emergent if the onset of the episode occurs within the on-treatment observation period. Severe or BG-confirmed symptomatic hypoglycaemia is an episode that is severe according to the American Diabetes Association classification or blood glucose-confirmed by a plasma glucose value <3.1 mmol/L (56 mg/dL) with symptoms consistent with hypoglycaemia. Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0 to week 30

InterventionParticipants (Count of Participants)
Semaglutide 0.5 mg2
Semaglutide 1.0 mg6
Sitagliptin4

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Change in Biochemistry Parameter: Alanine Aminotransferase - Ratio to Baseline

Change in alanine aminotransferase from baseline (week 0) to week 30 is presented as ratio to baseline. Alanine aminotransferase was measured in units per liter (U/L). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of alanine aminotransferase (Geometric Mean)
Semaglutide 0.5 mg0.86
Semaglutide 1.0 mg0.83
Sitagliptin0.95

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Change in Biochemistry Parameter: Aspartate Aminotransferase - Ratio to Baseline

Change in aspartate aminotransferase from baseline (week 0) to week 30 is presented as ratio to baseline. Aspartate aminotransferase was measured in units per liter (U/L). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of aspartate aminotransferase (Geometric Mean)
Semaglutide 0.5 mg0.92
Semaglutide 1.0 mg0.88
Sitagliptin0.99

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Change in Biochemistry Parameter: Amylase - Ratio to Baseline

Change in amylase from baseline (week 0) to week 30 is presented as ratio to baseline. Amylase was measured in units per liter (U/L). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of amylase (Geometric Mean)
Semaglutide 0.5 mg1.17
Semaglutide 1.0 mg1.19
Sitagliptin1.10

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Change in Biochemistry Parameter: Alkaline Phosphatase - Ratio to Baseline

Change in alkaline phosphatase from baseline (week 0) to week 30 is presented as ratio to baseline. Alkaline phosphatase was measured in units per liter (U/L). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of alkaline phosphatase (Geometric Mean)
Semaglutide 0.5 mg0.92
Semaglutide 1.0 mg0.91
Sitagliptin0.92

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Change in Biochemistry Parameter: Albumin - Ratio to Baseline

Change in albumin from baseline (week 0) to week 30 is presented as ratio to baseline. Albumin was measured in grams per deciliter (g/dL). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of albumin (Geometric Mean)
Semaglutide 0.5 mg1.02
Semaglutide 1.0 mg1.02
Sitagliptin1.01

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Change in Biochemistry Parameter: Calcium (Corrected)- Ratio to Baseline

Change in calcium (corrected) from baseline (week 0) to week 30 is presented as ratio to baseline. Calcium was measured in millimoles per litre (mmol/L). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of calcium (Geometric Mean)
Semaglutide 0.5 mg1.01
Semaglutide 1.0 mg1.01
Sitagliptin1.01

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Change in Biochemistry Parameter: Creatine Kinase - Ratio to Baseline

Change in creatine kinase from baseline (week 0) to week 30 is presented as ratio to baseline. Creatine kinase was measured in units per liter (U/L). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of creatine kinase (Geometric Mean)
Semaglutide 0.5 mg1.02
Semaglutide 1.0 mg0.96
Sitagliptin1.07

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Change in Biochemistry Parameter: Creatinine - Ratio to Baseline

Change in creatinine from baseline (week -2) to week 30 is presented as ratio to baseline. Creatinine was measured in micromoles per lier (umol/L). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week -2, week 30

InterventionRatio of creatinine (Geometric Mean)
Semaglutide 0.5 mg1.08
Semaglutide 1.0 mg1.07
Sitagliptin1.05

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Change in Biochemistry Parameter: Estimated Glomerular Filtration Rate (eGFR) - Ratio to Baseline

Change in estimated glomerular filtration rate (eGFR) from baseline (week 0) to week 30 is presented as ratio to baseline. Glomerular filtration rate was measured in milliliter/minute/specific surface area (mL/min/SSA). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of eGFR (Geometric Mean)
Semaglutide 0.5 mg0.92
Semaglutide 1.0 mg0.92
Sitagliptin0.94

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Change in Biochemistry Parameter: Lipase - Ratio to Baseline

Change in lipase from baseline (week 0) to week 30 is presented as ratio to baseline. Lipase was measured in units per liter (U/L). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of lipase (Geometric Mean)
Semaglutide 0.5 mg1.33
Semaglutide 1.0 mg1.42
Sitagliptin1.24

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Change in Biochemistry Parameter: Potassium - Ratio to Baseline

Change in potassium from baseline (week 0) to week 30 is presented as ratio to baseline. Potassium was measured in millimoles per liter (mmol/L). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of potassium (Geometric Mean)
Semaglutide 0.5 mg1.01
Semaglutide 1.0 mg1.00
Sitagliptin1.00

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Change in Biochemistry Parameter: Sodium - Ratio to Baseline

Change in sodium from baseline (week 0) to week 30 is presented as ratio to baseline. Sodium was measured in millimoles per litre (mmol/L). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of sodium (Geometric Mean)
Semaglutide 0.5 mg1.01
Semaglutide 1.0 mg1.00
Sitagliptin1.00

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Change in Biochemistry Parameter: Total Bilirubin - Ratio to Baseline

Change in total bilirubin from baseline (week 0) to week 30 is presented as ratio to baseline. Total bilirubin was measured in micromoles per liter (umol/L). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of total bilirubin (Geometric Mean)
Semaglutide 0.5 mg0.93
Semaglutide 1.0 mg0.93
Sitagliptin0.93

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Change in Biochemistry Parameter: Total Calcium - Ratio to Baseline

Change in total calcium from baseline (week 0) to week 30 is presented as ratio to baseline. Calcium was measured in millimoles per litre (mmol/L). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of total calcium (Geometric Mean)
Semaglutide 0.5 mg1.02
Semaglutide 1.0 mg1.01
Sitagliptin1.01

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Change in Biochemistry Parameter: Total Protein- Ratio to Baseline

Change in Total protein from baseline (week 0) to week 30 is presented as ratio to baseline. Total Protein was measured in grams per deciliter (g/dL). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of total protein (Geometric Mean)
Semaglutide 0.5 mg1.01
Semaglutide 1.0 mg1.00
Sitagliptin1.01

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Change in Biochemistry Parameter: Urea - Ratio to Baseline

Change in urea from baseline (week 0) to week 30 is presented as ratio to baseline. Urea was measured in millimoles per liter (mmol/L). Results are based on the 'on-treatment' observation period. On-treatment observation period is defined as the time period when a participant was on treatment with trial product, including any period after initiation of rescue medication. (NCT03061214)
Timeframe: Week 0, week 30

InterventionRatio of urea (Geometric Mean)
Semaglutide 0.5 mg1.01
Semaglutide 1.0 mg1.02
Sitagliptin1.01

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Change in BMI

Change in body mass index (BMI) from baseline (week 0) to week 30 was measured. Results are based on the 'on-treatment without rescue medication' observation period, which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionKilogram per square meter (kg/m^2) (Mean)
Semaglutide 0.5 mg-1.1
Semaglutide 1.0 mg-1.6
Sitagliptin-0.1

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Change in Body Weight

Change from baseline (week 0) to week 30 in body weight was evaluated. Results are based on the 'on-treatment without rescue medication' observation period which started at the date of first dose to either the day of last dose plus 7 days or first initiation of rescue medication, whichever came first. (NCT03061214)
Timeframe: Week 0, week 30

InterventionKilogram (kg) (Mean)
Semaglutide 0.5 mg-3.0
Semaglutide 1.0 mg-4.2
Sitagliptin-0.4

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Fasting Insulin

Plasma insulin collected after overnight fast (NCT03101930)
Timeframe: Baseline, and after 2 weeks and 14 weeks of treatment

,,
InterventionuU/mL (Mean)
Baseline2 weeks14 weeks
Hypocaloric Diet26.719.720.3
Liraglutide22.718.320.3
Sitagliptin23.329.426.0

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Change in Plasminogen Activator Inhibitor-1

Plasma plasminogen activator inhibitor-1 antigen (NCT03101930)
Timeframe: Baseline to 2 and 14 weeks

,,
Interventionunits/mL (Mean)
Baseline to 2 weeksBaseline to 14 weeks
Hypocaloric Diet1.1-3.6
Liraglutide-2.4-3.7
Sitagliptin-1.31.3

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Change in Flow-mediated Dilation

Brachial artery diameter is measured under basal conditions and during reactive hyperemia (Flow Mediated Dilation as %) (NCT03101930)
Timeframe: Baseline to 2 and 14 weeks

,,
InterventionPercentage (Mean)
Baseline to 2 weeks (Placebo infusion)Baseline to 2 weeks (Exendin infusion)Baseline to 14 weeks (Placebo infusion)Baseline to 14 weeks (Exendin infusion)
Hypocaloric Diet1.241.431.010.42
Liraglutide0.710.481.431.73
Sitagliptin2.060.131.591.42

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Blood Pressure

The mean of three systolic blood pressure measurements one minute apart using a oscillometric recording device with patient in supine position (NCT03101930)
Timeframe: Baseline, and after 2 weeks and 14 weeks of treatment

,,
InterventionmmHg (Mean)
Baseline2 weeks14 weeks
Hypocaloric Diet127.7121.7119.7
Liraglutide124.1122.9122.2
Sitagliptin120.2117.5118.2

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Change in Weight

Weight measured in light clothing without shoes (NCT03101930)
Timeframe: Change from baseline to 14 weeks

Interventionkg (Mean)
Liraglutide-2.72
Sitagliptin-0.71
Hypocaloric Diet-4.95

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Heart Rate

The mean of three measurements with the patient in the supine position (NCT03101930)
Timeframe: Baseline, and after 2 weeks and 14 weeks of treatment

,,
InterventionBeats per minute (Mean)
Baseline2 weeks14 weeks
Hypocaloric Diet63.863.261.7
Liraglutide64.968.968.9
Sitagliptin67.266.265.9

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Fasting Glucose

Blood glucose collected after overnight fast (NCT03101930)
Timeframe: Baseline, and after 2 weeks and 14 weeks of treatment

,,
Interventionmg/dl (Mean)
Baseline2 weeks14 weeks
Hypocaloric Diet94.592.491.2
Liraglutide95.384.2685.2
Sitagliptin97.693.996.6

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Urine Albumin-to-creatinine Ratio

Ratio of urine albumin to creatinine in a spot urine collected after overnight rest (NCT03101930)
Timeframe: Baseline to 13 weeks

,,
Interventionmg/g (Mean)
Baseline13 Weeks
Hypocaloric Diet6.310.1
Liraglutide12.010.5
Sitagliptin7.99.2

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Change in C-peptide

"Fasting C-peptide, the postprandial 2-hour C-peptide were measured at baseline and at study end points, and the difference between baseline and study end points were compared.The changes in fasting C-peptide, the postprandial 2-hour C-peptide were compared among patients with different genotypes at baseline and at study end points.Participants in Non-T2DM Group were not taking Sitagliptin, so their C-peptide were not measured." (NCT03108521)
Timeframe: Basline and 12 weeks later. Fasting and 2h after take 75g glucose orally.

Interventionng/ml (Mean)
ΔFasting C peptideΔ2h C peptide
Sitagliptin Group0.031.11

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Glycosylated Hemoglobin A1c (HbA1c)

non-T2D subjects only tested HbA1c at baseline. Of the 71 patients who completed the study, 69 collected HbA1c at both baseline and study endpoint, and 2 subjects did not carry out HbA1c measurement for personal reasons. (NCT03108521)
Timeframe: 12 weeks later

Interventionpercentage of (Mean)
Sitagliptin Group6.78

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Change in Insulin

"Fasting insulin, the postprandial 0.5-hour,2-hour,3-hour insulin were measured at baseline and at study end points, and the difference between baseline and study end points were compared.The changes in fasting insulin, the postprandial 0.5-hour,2-hour,3-hour insulin were compared among patients with different genotypes at baseline and at study end points.Participants in Non-T2DM Group were not taking Sitagliptin, so their insulin were not measured." (NCT03108521)
Timeframe: Basline and 12 weeks later. Fasting and 0.5h, 2h,3h after take 75g glucose orally.

InterventionμU/ml (Mean)
ΔFasting insulinΔ0.5h insulinΔ2h insulinΔ3h insulin
Sitagliptin Group0.664.008.432.99

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Types of Gene Polymorphism

24 SNPs genetic points of DPP-4, GLP-1 and GLP-1R. (NCT03108521)
Timeframe: Baseline

,
Interventionpercentage of Allele frequency (Number)
rs7565794rs10166311rs2300757rs2302873rs2284872rs7608798rs2111850rs16822665
Non-T2DM Group29.224.325.025.025.024.32525.0
Sitagliptin Group40.040.539.242.442.444.240.542.5

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Change in Blood Glucose

"Fasting Blood glucose, the postprandial 0.5-hour,2-hour,3-hour blood glucose were measured at baseline and at study end points, and the difference between baseline and study end points were compared.Participants in Non-T2DM Group were not taking Sitagliptin, so their blood glucose were not measured." (NCT03108521)
Timeframe: Basline and 12 weeks later. Fasting, 0.5h, 2h,3h after take 75g glucose orally.

Interventionmmol/l (Mean)
ΔFasting blood glucoseΔ0.5h GlucoseΔ2h GlucoseΔ3h Glucose
Sitagliptin Group-1.60-2.18-3.49-3.45

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Change in SBP in Subjects From Baseline at Week 24

To evaluate the treatment effect of bexagliflozin vs. sitagliptin on the change in systolic blood pressure (SBP) in subjects at week 24 (NCT03115112)
Timeframe: Baseline to week 24

Interventionmm Hg (Least Squares Mean)
Bexagliflozin-4.23
Sitagliptin-1.90

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Change in HbA1c From Baseline to Week 24

The primary efficacy objective is to demonstrate that bexagliflozin is non-inferior to sitagliptin by evaluating the treatment effect on hemoglobin A1c (HbA1c) reduction at week 24 in subjects whose type 2 diabetes mellitus (T2DM) is inadequately controlled by metformin. (NCT03115112)
Timeframe: Baseline to week 24

Interventionpercentage of HbA1c (Least Squares Mean)
Bexagliflozin-0.74
Sitagliptin-0.82

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Change in FPG From Baseline at Week 24

To evaluate the treatment effect of bexagliflozin vs. sitagliptin on the change in fasting plasma glucose (FPG) at week 24 (NCT03115112)
Timeframe: Baseline to week 24

Interventionmmol/L (Least Squares Mean)
Bexagliflozin-1.82
Sitagliptin-1.45

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Change in Body Weight in Subjects With Baseline BMI ≥ 25 kg/m2 at Week 24

To evaluate the treatment effect of bexagliflozin vs. sitagliptin on the change in body weight in subjects with baseline body mass index (BMI) ≥ 25 kg/m2 at week 24 (NCT03115112)
Timeframe: Baseline to week 24

Interventionkg (Least Squares Mean)
Bexagliflozin-3.35
Sitagliptin-0.81

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Percent Change From Baseline in Time During 24 Hours With Glucose 70 to 139 mg/dL

Percent change from baseline in time during 24 hours with glucose levels 70 to 139 mg/dL was determined over a 6-day period (in order to obtain a continuous 72-hour reading) at baseline and at the end of each active treatment. The participants were analyzed according to treatment received in treatment period 1 and treatment period 2 as per the sequence reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 1 (Days 22 to 27) and End of Treatment Period 2 (Days 66 to 71)

,
InterventionPercent Change (Mean)
Treatment Period 1Treatment Period 2
Treatment Sequence AB0.1570.192
Treatment Sequence BA0.1910.182

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Change From Baseline in Time Spent With Glucose Level 70 to 139 mg/dL

Time spent with the glucose level 70 to 139 mg/dL was determined over a 6-day period (in order to obtain a continuous 72-hour reading) at baseline and at the end of each active treatment. The participants were analyzed according to treatment received in treatment period 1 and treatment period 2 as per the sequence reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 1 (Days 22 to 27) and End of Treatment Period 2 (Days 66 to 71)

,
InterventionMinutes (Mean)
Treatment Period 1Treatment Period 2
Treatment Sequence AB226.64277.00
Treatment Sequence BA275.64261.57

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Percent Change From Baseline in Time During 24 Hours With Glucose Level > 180 mg/dL

Percent change from baseline in time during 24 hours within the glucose levels >180 mg/dL was determined over a 6-day period (in order to obtain a continuous 72-hour reading) at baseline and at the end of each active treatment. The participants were analyzed according to treatment received in treatment period 1 as per the sequence reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 1 (Days 22 to 27) and End of Treatment Period 2 (Days 66 to 71)

,
InterventionPercent Change (Mean)
Treatment Period 1Treatment Period 2
Treatment Sequence AB-0.235-0.246
Treatment Sequence BA-0.212-0.251

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Change From Baseline in Time Spent With Glucose Level > 180 mg/dL

Time spent with the glucose level > 180 mg/dL was determined over a 6-day period (in order to obtain a continuous 72-hour reading) at baseline and at the end of each active treatment. The participants were analyzed according to treatment received in treatment period 1 as per the sequence reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 1 (Days 22 to 27) and End of Treatment Period 2 (Days 66 to 71)

,
InterventionMinutes (Mean)
Treatment Period 1Treatment Period 2
Treatment Sequence AB-338.36-354.63
Treatment Sequence BA-305.69-361.65

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Change From Baseline in Time Spent With Glucose Level > 140 mg/dL

Time spent with the glucose level > 140 mg/dL was determined over a 6-day period (in order to obtain a continuous 72-hour reading) at baseline and at the end of each active treatment. The participants were analyzed according to treatment received in treatment period 1 and treatment period 2 as per the sequence reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 1 (Days 22 to 27) and End of Treatment Period 2 (Days 66 to 71)

,
InterventionMinutes (Mean)
Treatment Period 1Treatment Period 2
Treatment Sequence AB-231.98-308.68
Treatment Sequence BA-310.41318.23

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Change From Baseline in Time Spent With Glucose Level < 70 mg/dL

Time spent with the glucose level < 70 mg/dL was determined over a 6-day period (in order to obtain a continuous 72-hour reading) at baseline and at the end of each active treatment. The participants were analyzed according to treatment received in treatment period 1 and treatment period 2 as per the sequence reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 1 (Days 22 to 27) and End of Treatment Period 2 (Days 66 to 71)

,
InterventionMinutes (Mean)
Treatment Period 1Treatment Period 2
Treatment Sequence ABNANA
Treatment Sequence BANANA

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Percent Change From Baseline in Time During 24 Hours With Glucose Greater Than (>) 140 mg/dL

Percent change from baseline in time during 24 hours within the glucose levels >140 mg/dL was determined over a 6-day period (in order to obtain a continuous 72-hour reading) at baseline and at the end of each active treatment. The participants were analyzed according to treatment received in treatment period 1 and treatment period 2 as per the sequence reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 1 (Days 22 to 27) and End of Treatment Period 2 (Days 66 to 71)

,
InterventionPercent Change (Mean)
Treatment Period 1Treatment Period 2
Treatment Sequence AB-0.161-214
Treatment Sequence BA-0.216-0.221

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Change From Baseline in Mean 24-hour Glucose Profile

Mean 24-hour glucose profiles as measured by CGM was determined over a 6-day period (in order to obtain a continuous 72-hour reading) at baseline and at the end of each active treatment. The participants were analyzed according to treatment received in treatment period 1 and treatment period 2 as per the sequence reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 1 (Days 22 to 27) and End of Treatment Period 2 (Days 66 to 71)

,
Interventionmg/dL (Mean)
Treatment Period 1Treatment Period 2
Treatment Sequence AB-34.81-31.27
Treatment Sequence BA-39.56-41.74

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Change From Baseline in Glycemic Standard Deviation (SD) for 24-hour Glucose Profile

Glycemic standard deviation for 24-hour glucose profile (glycemic variability), as measured by CGM was determined over a 6-day period (in order to obtain a continuous 72-hour reading) at baseline and at the end of each active treatment. The participants who received the study drug in the treatment period 1 and 2 as per the sequence were reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 1 (Days 22 to 27) and End of Treatment Period 2 (Days 66 to 71)

,
Interventionmg/dL (Mean)
Treatment Period 1Treatment Period 2
Treatment Sequence AB-7.64-8.53
Treatment Sequence BA-8.40-7.13

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Change From Baseline in Fasting Plasma Glucose Levels

Fasting plasma glucose levels were determined over a 6-day period (in order to obtain a continuous 72-hour reading) at baseline and at the end of each active treatment. The participants were analyzed according to treatment received in treatment period 1 and treatment period 2 as per the sequence reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 1 (Days 22 to 27) and End of Treatment Period 2 (Days 66 to 71)

,
Interventionmg/dL (Mean)
Treatment Period 1Treatment Period 2
Treatment Sequence AB-32.04-27.69
Treatment Sequence BA-34.48-45.51

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Change From Baseline in 2-hour Post-prandial Glucose (PPG) Levels

2-hour post-prandial glucose levels were determined over a 6-day period (in order to obtain a continuous 72-hour reading) at baseline and at the end of each active treatment. The participants were analyzed according to treatment received in treatment period 1 and treatment period 2 as per the sequence reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 1 (Days 22 to 27) and End of Treatment Period 2 (Days 66 to 71)

,
Interventionmg/dL (Mean)
Treatment Period 1Treatment Period 2
Treatment Sequence AB-47.03-41.12
Treatment Sequence BA-43.36-44.03

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Change From Baseline in Glycemic Coefficient of Variation (CV) in Treatment Period 2

Continuous blood glucose monitoring was done in participants using CGM determined over a 6-day period (in order to obtain a continuous 72-hour reading) at baseline and after each active treatment. Glucose coefficient of variation was calculated based on CGM data dividing the standard deviation of blood glucose values by the mean of the corresponding glucose readings. The participants were analyzed according to treatment received in treatment period 2 as per the sequence reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 2 (Days 66 to 71)

InterventionPercentage of CV (Mean)
Treatment Sequence AB-1.26
Treatment Sequence BA0.77

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Change From Baseline in Glycemic Coefficient of Variation (CV) in Treatment Period 1

Continuous blood glucose monitoring was done in participants using continuous glucose monitoring (CGM) determined over a 6-day period (in order to obtain a continuous 72-hour reading) at baseline and after each active treatment. Glucose coefficient of variation (CV) was calculated based on CGM data dividing the standard deviation of blood glucose values by the mean of the corresponding glucose readings. The participants were analyzed according to treatment received in treatment period 2 as per the sequence reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 1 (Days 22 to 27)

InterventionPercentage of CV (Mean)
Treatment Sequence AB-0.69
Treatment Sequence BA0.24

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Change From Baseline in Percentage of 2 Consecutive Glucose Readings With < 70 mg/dL

The percentage of 2 consecutive glucose readings with < 70 mg/dL were reported. The participants were analyzed according to treatment received in treatment period 1 and treatment period 2 as per the sequence reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 1 (Days 22 to 27) and End of Treatment Period 2 (Days 66 to 71)

,
InterventionPercentage of readings (Mean)
Treatment Period 1Treatment Period 2
Treatment Sequence ABNANA
Treatment Sequence BANANA

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Percent Change From Baseline in Time During 24 Hours With Glucose Level Less Than (<) 70 mg/dL

Percent change from baseline in time during 24 hours within the glucose levels < 70 mg/dL was determined over a 6-day period (in order to obtain a continuous 72-hour reading) at baseline and at the end of each active treatment. The participants were analyzed according to treatment received in treatment period 1 and treatment period 2 as per the sequence reported in this outcome measure. (NCT03267576)
Timeframe: Baseline up to End of Treatment Period 1 (Days 22 to 27) and End of Treatment Period 2 (Days 66 to 71)

,
InterventionPercent Change (Mean)
Treatment Period 1Treatment Period 2
Treatment Sequence ABNANA
Treatment Sequence BANANA

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The Frequency of Hypoglycaemic Episodes With Sitagliptin vs Placebo Treatment.

The purpose of the trial was to test the influence of DPP-4 inhibition on the risk to develop hypoglycaemia. Chemical hypoglycaemic episodes (characterised by a plasma glucose nadir ≤70 mg/dL) occurring during the in-house periods of the subjects were compared. (NCT03359590)
Timeframe: during the two in-house periods (54 hs each) after treatment with sitagliptin or placebo for up to 24 weeks

InterventionHypoglycaemic episodes (Mean)
Sitagliptin Arm5.35
Placebo Arm5.72

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Change From Baseline to Week 26 in Fasting Lipid Profile: Low-density Lipoprotein (LDL) Cholesterol (Ratio to Baseline)

Change from baseline in LDL cholesterol (measured in mmol/L) at week 26 is presented as ratio to baseline. The outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization up to the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of LDL cholesterol (Geometric Mean)
Oral Semaglutide 3 mg1.02
Oral Semaglutide 7 mg0.98
Oral Semaglutide 14 mg0.98
Sitagliptin 100 mg1.01

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Change From Baseline to Week 26 in Fasting Lipid Profile: Total Cholesterol (Ratio to Baseline)

Change from baseline in total cholesterol (measured in mmol/L) at week 26 is presented as ratio to baseline. The outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization up to the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of total cholesterol (Geometric Mean)
Oral Semaglutide 3 mg1.00
Oral Semaglutide 7 mg0.96
Oral Semaglutide 14 mg0.96
Sitagliptin 100 mg0.99

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Time to Rescue Medication

Time to rescue medication is presented as the number of participants who had taken rescue medication anytime from baseline to week 31. 'Rescue medication': use of new anti-diabetic medication as add-on to trial product and used for more than 21 days with the initiation at or after randomisation and before last day on trial product, and/or intensification of anti-diabetic medication (a more than 20% increase in dose relative to baseline) for more than 21 days with the intensification at or after randomisation and before last day on trial product. The outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization and the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 31

InterventionParticipants (Count of Participants)
Oral Semaglutide 3 mg5
Oral Semaglutide 7 mg6
Oral Semaglutide 14 mg6
Sitagliptin 100 mg7

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Percentage Change From Baseline to Week 26 in Body Weight

Percentage change from baseline to week 26 in body weight is presented. The outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization and the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

InterventionPercentage change (Mean)
Oral Semaglutide 3 mg-2
Oral Semaglutide 7 mg-4
Oral Semaglutide 14 mg-5
Sitagliptin 100 mg-1

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Change From Baseline to Week 26 in Electrocardiogram (ECG) Category

Change from baseline in ECG category at week 26 is presented. Change from baseline results are presented as shift in findings categorized as: normal, abnormal and not clinically significant (NCS), and abnormal and clinically significant (CS). The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

,,,
InterventionParticipants (Count of Participants)
Normal (Baseline) to normal (week 26)Normal (Baseline) to abnormal NCS (week 26)Normal (Baseline) to abnormal CS (week 26)Abnormal NCS (Baseline) to normal (week 26)Abnormal NCS (Baseline) to abnormal NCS (week 26)Abnormal NCS (Baseline) to abnormal CS (week 26)Abnormal CS (Baseline) to normal (week 26)Abnormal CS (Baseline) to abnormal NCS (week 26)Abnormal CS (Baseline) to abnormal CS (week 26)
Oral Semaglutide 14 mg1652910264057417
Oral Semaglutide 3 mg174218265638527
Oral Semaglutide 7 mg1633032761313325
Sitagliptin 100 mg175175436426923

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Number of Participants With Treatment-emergent Severe or Blood Glucose Confirmed Symptomatic Hypoglycaemic Episodes During Exposure to Trial Product

Number of participants with treatment-emergent severe or blood glucose (BG) confirmed symptomatic hypoglycaemic episodes during exposure to trial product is presented. Severe: requiring assistance from another person for recovery. 'BG-confirmed': hypoglycaemic episode with a plasma glucose value < 3.1 mmol/L (56 mg/dL); The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 31

InterventionParticipants (Count of Participants)
Oral Semaglutide 3 mg2
Oral Semaglutide 7 mg2
Oral Semaglutide 14 mg2
Sitagliptin 100 mg1

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Change From Baseline to Week 26 in Short Form-36 Version 2 (SF-36v2) (Acute Version) Health Survey

SF-36 v2.0 is a 36-item, patient-reported survey of patient health. SF-36 measures the participant's overall Health Related Quality of Life on 8 domains (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role emotional and mental health) and two component summary scores (physical component summary and mental component summary). Range of score for domains and component summary scores : 1-100 (Higher scores indicated a better health state). A positive change score indicates an improvement since baseline. Outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization up to end date which was first date of any of following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

,,,
InterventionScore on a scale (Mean)
Physical FunctionRole PhysicalBodily PainGeneral HealthVitalitySocial FunctionRole EmotionalMental HealthPhysical ComponentMental Component
Oral Semaglutide 14 mg0.930.280.511.951.210.170.230.700.980.44
Oral Semaglutide 3 mg0.20-0.47-0.061.470.440.490.060.510.150.50
Oral Semaglutide 7 mg0.48-0.41-0.371.040.84-0.36-0.660.330.29-0.07
Sitagliptin 100 mg0.310.240.220.950.330.100.03-0.70.69-0.39

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Change From Baseline to Week 26 in Haematology Parameters: Basophils, Eosinophils, Lymphocytes, Monocytes, and Neutrophils

Change from baseline in hematology parameters such as basophils, eosinophils, lymphocytes, monocytes, and neutrophils were reported. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

,,,
Intervention10^9 cells per liter (Mean)
BasophilsEosinophilsLymphocytesMonocytesNeutrophils
Oral Semaglutide 14 mg0.00-0.010.000.010.10
Oral Semaglutide 3 mg0.010.00-0.030.010.03
Oral Semaglutide 7 mg0.010.000.010.010.13
Sitagliptin 100 mg0.00-0.000.000.020.31

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Change From Baseline to Week 26 in Glycated Haemoglobin (HbA1c) (%)

Change in HbA1c from baseline to week 26 in percentage (%) point of HbA1c is presented. The outcome data was evaluated based on the on-treatment without rescue medication observation period and in-trial observation period. On-treatment without rescue medication observation period: from date of first dose of trial product following randomization and the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. In-trial observation period: the time period where participants were considered to be in the trial, regardless of discontinuation of trial product or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

,,,
InterventionPercentage point of HbA1C (Mean)
On-treatment observation periodIn-trial observation period
Oral Semaglutide 14 mg-1.6-1.5
Oral Semaglutide 3 mg-0.8-0.8
Oral Semaglutide 7 mg-1.3-1.3
Sitagliptin 100 mg-0.7-0.7

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Number of Treatment-emergent Adverse Events During Exposure to Trial Product

An adverse event (AE) was defined as any unfavourable and unintended sign (including an abnormal laboratory finding), symptom or disease temporally associated with the use of a product, whether or not considered related to the product. AEs with onset during the on-treatment period correspond to treatment-emergent AEs (TEAEs). The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 31

InterventionEvents (Number)
Oral Semaglutide 3 mg635
Oral Semaglutide 7 mg741
Oral Semaglutide 14 mg793
Sitagliptin 100 mg643

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Physical Examination Category

The physical examination values for different body systems at baseline and week 26 are presented. The investigator interpreted the results and categorised them as: normal, abnormal NCS or abnormal CS. The physical examination are presented for the following body systems: cardiovascular system; central and peripheral nervous system; gastrointestinal system, including mouth; general appearance; head, ears, eyes, nose, throat, neck; lymph node palpation; musculoskeletal system; respiratory system; skin; and thyroid gland. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: Baseline and week 26

,,,
InterventionParticipants (Count of Participants)
Cardiovascular system - Normal (Baseline)Cardiovascular system - abnormal NCS (Baseline)Cardiovascular system - Abnormal CS (Baseline)Cardiovascular system -Normal (Week 26)Cardiovascular system - Abnormal NCS (Week 26)Cardiovascular system - Abnormal CS (Week 26)Central and Peripheral Nervous System - Normal (Baseline)Central and Peripheral Nervous System - Abnormal NCS (Baseline)Central and Peripheral Nervous System - Abnormal CS (Baseline)Central and Peripheral Nervous System - Normal (Week 26)Central and Peripheral Nervous System - Abnormal NCS (Week 26)Central and Peripheral Nervous System - Abnormal CS (Week 26)Gastrointestinal System incl. Mouth - Normal (Baseline)Gastrointestinal System incl. Mouth - Abnormal NCS (Baseline)Gastrointestinal System incl. Mouth - Abnormal CS (Baseline)Gastrointestinal System incl. Mouth - Normal (Week 26)Gastrointestinal System incl. Mouth - Abnormal NCS (Week 26)Gastrointestinal System incl. Mouth - Abnormal CS (Week 26)General Appearance - Normal (Baseline)General Appearance - Abnormal NCS (Baseline)General Appearance - Abnormal CS (Baseline)General Appearance - Normal (Week 26)General Appearance - Abnormal NCS (Week 26)General Appearance - Abnormal CS (Week 26)Head, Ears, Eyes, Nose, Throat, Neck - Normal (Baseline)Head, Ears, Eyes, Nose, Throat, Neck - Abnormal NCS (Baseline)Head, Ears, Eyes, Nose, Throat, Neck - Abnormal CS (Baseline)Head, Ears, Eyes, Nose, Throat, Neck - Normal (Week 26)Head, Ears, Eyes, Nose, Throat, Neck - Abnormal NCS (Week 26)Head, Ears, Eyes, Nose, Throat, Neck - Abnormal CS (Week 26)Lymph Node Palpation - Normal (Baseline)Lymph Node Palpation - Abnormal NCS (Baseline)Lymph Node Palpation - Abnormal CS (Baseline)Lymph Node Palpation - Normal (Week 26)Lymph Node Palpation - Abnormal NCS (Week 26)Lymph Node Palpation - Abnormal CS (Week 26)Musculoskeletal System - Normal (Baseline)Musculoskeletal System - Abnormal NCS (Baseline)Musculoskeletal System - Abnormal CS (Baseline)Musculoskeletal System - Normal (Week 26)Musculoskeletal System - Abnormal NCS (Week 26)Musculoskeletal System - Abnormal CS (Week 26)Respiratory System - Normal (Baseline)Respiratory System -Abnormal NCS (Baseline)Respiratory System - Abnormal CS (Baseline)Respiratory System - Normal (Week 26)Respiratory System - Abnormal NCS (Week 26)Respiratory System - Abnormal CS (Week 26)Skin - Normal (Baseline)Skin - Abnormal NCS (Baseline)Skin - Abnormal CS (Baseline)Skin - Normal (Week 26)Skin - Abnormal NCS (Week 26)Skin - Abnormal CS (Week 26)Thyroid Gland - Normal (Baseline)Thyroid Gland - Abnormal NCS (Baseline)Thyroid Gland - Abnormal CS (Baseline)Thyroid Gland - Normal (Week 26)Thyroid Gland - Abnormal NCS (Week 26)Thyroid Gland - Abnormal CS (Week 26)
Oral Semaglutide 14 mg3556030131358303022135371300413282112280196351542974235731304103517330122359113050029654112564273581230401
Oral Semaglutide 3 mg35452319533552432222350101314120329257300216348943223236100325103441343146635533324202827182606073564132232
Oral Semaglutide 7 mg353413222235152321323431413151013252762952743498031951353503233034585319433553032510282651126352113514331943
Sitagliptin 100 mg356203392035710339203461113291023282283132173446533045357103410035242335333571034100277651626760143504433722

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Change From Baseline to Week 26 in Waist Circumference

Change from baseline in waist circumference is presented. The outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization and the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

InterventionCentimeter (Mean)
Oral Semaglutide 3 mg-1.6
Oral Semaglutide 7 mg-2.7
Oral Semaglutide 14 mg-3.7
Sitagliptin 100 mg-0.8

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Change From Baseline to Week 26 in Biochemistry Parameter: Calcium (Total) (Ratio to Baseline)

Change from baseline in calcium (total) (measured in mmol/L) at week 26 is presented as ratio to baseline. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of calcium (Geometric Mean)
Oral Semaglutide 3 mg0.98
Oral Semaglutide 7 mg0.98
Oral Semaglutide 14 mg0.99
Sitagliptin 100 mg0.98

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Change From Baseline to Week 26 in Biochemistry Parameter: Potassium (Ratio to Baseline)

Change from baseline in potassium (measured in mmol/L) at week 26 is presented as ratio to baseline. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of potassium (Geometric Mean)
Oral Semaglutide 3 mg1.00
Oral Semaglutide 7 mg1.00
Oral Semaglutide 14 mg1.00
Sitagliptin 100 mg1.01

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Change From Baseline to Week 26 in Eye Examination Category

The eye examination category at baseline and week 26 are presented. The investigator interpreted the results and categorised them as: normal, abnormal NCS or abnormal CS. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

,,,
InterventionParticipants (Count of Participants)
Left Eye Ophthalmoscopy - Normal (Baseline)Left Eye Ophthalmoscopy - Abnormal NCS (Baseline)Left Eye Ophthalmoscopy - Abnormal CS (Baseline)Left Eye Ophthalmoscopy - Normal (Week 26)Left Eye Ophthalmoscopy -Abnormal NCS (Week 26)Left Eye Ophthalmoscopy - Abnormal CS (Week 26)Right Eye Ophthalmoscopy - Normal (Baseline)Right Eye Ophthalmoscopy - Abnormal NCS (Baseline)Right Eye Ophthalmoscopy - Abnormal CS (Baseline)Right Eye Ophthalmoscopy - Normal (Week 26)Right Eye Ophthalmoscopy - Abnormal NCS (Week 26)Right Eye Ophthalmoscopy - Abnormal CS (Week 26)
Oral Semaglutide 14 mg2546146217503425756482204536
Oral Semaglutide 3 mg2456056221495524064572234953
Oral Semaglutide 7 mg2405167226445323454692184955
Sitagliptin 100 mg2485258240395624053652334359

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Change From Baseline to Week 26 in Vital Signs: Pulse Rate

Change from baseline in pulse rate is presented. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

InterventionBeats per minute (beats/min) (Mean)
Oral Semaglutide 3 mg78
Oral Semaglutide 7 mg78
Oral Semaglutide 14 mg78
Sitagliptin 100 mg78

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Change From Baseline to Week 26 in Vital Signs: Diastolic Blood Pressure

Change from baseline in diastolic blood pressure is presented. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

InterventionMillimeter of mercury (mmHg) (Mean)
Oral Semaglutide 3 mg83
Oral Semaglutide 7 mg84
Oral Semaglutide 14 mg83
Sitagliptin 100 mg83

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Number of Treatment-emergent Severe or Blood Glucose Confirmed Symptomatic Hypoglycaemic Episodes During Exposure to Trial Product

Number of treatment-emergent severe or blood glucose (BG) confirmed symptomatic hypoglycaemic episodes during exposure to trial product is presented. Severe: requiring assistance from another person for recovery. 'BG-confirmed': hypoglycaemic episode with a plasma glucose value < 3.1 mmol/L (56 mg/dL); The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 31

InterventionEpisodes (Number)
Oral Semaglutide 3 mg2
Oral Semaglutide 7 mg2
Oral Semaglutide 14 mg2
Sitagliptin 100 mg1

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Change From Baseline to Week 26 in 7 Point SMPG Profile: Mean Postprandial Increment (Over All Meals)

Change from baseline in 7-point SMPG: Mean postprandial increment (over all meals) at week 26 is presented. The outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization and the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

Interventionmmol/L (Mean)
Oral Semaglutide 3 mg-0.4
Oral Semaglutide 7 mg-0.9
Oral Semaglutide 14 mg-1.0
Sitagliptin 100 mg-0.6

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Change From Baseline to Week 26 in Biochemistry Parameter: Albumin (Ratio to Baseline)

Change from baseline in Albumin (measured in grams per deciliter [g/dL]) at week 26 is presented as ratio to baseline. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of albumin (Geometric Mean)
Oral Semaglutide 3 mg0.99
Oral Semaglutide 7 mg0.99
Oral Semaglutide 14 mg0.99
Sitagliptin 100 mg0.99

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Change From Baseline to Week 26 in Haematology Parameter: Thrombocytes (Ratio to Baseline)

Change from baseline in thrombocytes at week 26 is reported as ratio to baseline. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of thrombocytes (Geometric Mean)
Oral Semaglutide 3 mg0.99
Oral Semaglutide 7 mg0.99
Oral Semaglutide 14 mg0.99
Sitagliptin 100 mg0.97

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Change From Baseline to Week 26 in Haematology Parameter: Leucocytes (Ratio to Baseline)

Change from baseline in Leucocytes at week 26 is reported as ratio to baseline. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of leucocytes (Geometric Mean)
Oral Semaglutide 3 mg1.01
Oral Semaglutide 7 mg1.02
Oral Semaglutide 14 mg1.01
Sitagliptin 100 mg1.04

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Change From Baseline to Week 26 in Haematology Parameter: Haemoglobin (Ratio to Baseline)

Change from baseline in Haemoglobin at week 26 is reported as ratio to baseline. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of haemoglobin (Geometric Mean)
Oral Semaglutide 3 mg1.00
Oral Semaglutide 7 mg1.00
Oral Semaglutide 14 mg1.00
Sitagliptin 100 mg1.00

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Change From Baseline to Week 26 in Haematology Parameter: Haematocrit (Ratio to Baseline)

Change from baseline in Haematocrit at week 26 is reported as ratio to baseline. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of haematocrit (Geometric Mean)
Oral Semaglutide 3 mg1.01
Oral Semaglutide 7 mg1.00
Oral Semaglutide 14 mg1.00
Sitagliptin 100 mg1.00

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Change From Baseline to Week 26 in Fasting Plasma Glucose (FPG)

Change in fasting plasma glucose (FPG) from baseline to week 26 in millimole per liter (mmol/l) is presented. The outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization and the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

Interventionmmol/l (Mean)
Oral Semaglutide 3 mg-1.03
Oral Semaglutide 7 mg-1.79
Oral Semaglutide 14 mg-2.00
Sitagliptin 100 mg-0.52

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Change From Baseline to Week 26 in Fasting Lipid Profile: Very-low-density Lipoprotein (VLDL) Cholesterol (Ratio to Baseline)

Change from baseline in VLDL cholesterol (measured in mmol/L) at week 26 is presented as ratio to baseline. The outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization up to the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of VLDL cholesterol (Mean)
Oral Semaglutide 3 mg1.05
Oral Semaglutide 7 mg0.94
Oral Semaglutide 14 mg0.94
Sitagliptin 100 mg0.98

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Change From Baseline to Week 26 in Fasting Lipid Profile: Triglycerides (Ratio to Baseline)

Change from baseline in triglycerides (measured in mmol/L) at week 26 is presented as ratio to baseline. The outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization up to the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of triglycerides (Geometric Mean)
Oral Semaglutide 3 mg0.96
Oral Semaglutide 7 mg0.86
Oral Semaglutide 14 mg0.86
Sitagliptin 100 mg0.91

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Change From Baseline to Week 26 in Self-measured Plasma Glucose (SMPG) Profile: Mean 7-point Profile

Change from baseline in mean 7-point SMPG profile at week 26 is presented. SMPG was recorded at the following 7 time points: before breakfast, 90 minutes after start of breakfast, before lunch, 90 minutes after start of lunch, before dinner, 90 minutes after dinner and at bedtime. The outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization and the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

Interventionmmol/L (Mean)
Oral Semaglutide 3 mg-1.5
Oral Semaglutide 7 mg-2.3
Oral Semaglutide 14 mg-2.6
Sitagliptin 100 mg-1.2

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Change From Baseline to Week 26 in Biochemistry Parameter: Urea (Ratio to Baseline)

Change from baseline in urea (measured in mmol/L) at week 26 is presented as ratio to baseline. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of urea (Geometric Mean)
Oral Semaglutide 3 mg1.00
Oral Semaglutide 7 mg0.99
Oral Semaglutide 14 mg0.98
Sitagliptin 100 mg1.03

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Change From Baseline to Week 26 in Vital Signs: Systolic Blood Pressure

Change from baseline in systolic blood pressure is presented. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

InterventionMillimeter of mercury (mmHg) (Mean)
Oral Semaglutide 3 mg131
Oral Semaglutide 7 mg132
Oral Semaglutide 14 mg130
Sitagliptin 100 mg130

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Change From Baseline to Week 26 in Body Mass Index (BMI)

Change from baseline in BMI is presented. The outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization and the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

InterventionKilogram per square meter (kg/m^2) (Mean)
Oral Semaglutide 3 mg-0.5
Oral Semaglutide 7 mg-1.1
Oral Semaglutide 14 mg-1.4
Sitagliptin 100 mg-0.2

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Change From Baseline to Week 26 in Body Weight (Kilogram [kg])

Change in body weight from baseline to week 26 in kg is presented. The outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization and the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

InterventionKilogram (Mean)
Oral Semaglutide 3 mg-1.4
Oral Semaglutide 7 mg-2.9
Oral Semaglutide 14 mg-3.8
Sitagliptin 100 mg-0.5

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Change From Baseline to Week 26 in Calcitonin (Ratio to Baseline)

Change from baseline in calcitonin (measured in picograms per milliliter [pg/ml]) at week 26 is presented as ratio to baseline. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of calcitonin (Geometric Mean)
Oral Semaglutide 3 mg1.00
Oral Semaglutide 7 mg1.05
Oral Semaglutide 14 mg1.02
Sitagliptin 100 mg1.01

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Change From Baseline to Week 26 in Fasting Lipid Profile: Free Fatty Acids (Ratio to Baseline)

Change from baseline in free fatty acids (measured in mmol/L) at week 26 is presented as ratio to baseline. The outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization up to the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of free fatty acids (Geometric Mean)
Oral Semaglutide 3 mg0.95
Oral Semaglutide 7 mg0.89
Oral Semaglutide 14 mg0.87
Sitagliptin 100 mg0.96

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Change From Baseline to Week 26 in Fasting Lipid Profile: High-density Lipoprotein (HDL) Cholesterol (Ratio to Baseline)

Change from baseline in HDL Cholesterol (measured in mmol/L) at week 26 is presented as ratio to baseline. The outcome data was evaluated based on the on-treatment without rescue medication observation period: from date of first dose of trial product following randomization up to the end date which was the first date of any of the following: the last dose of trial product plus 3 days or initiation of rescue medication. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of HDL cholesterol (Geometric Mean)
Oral Semaglutide 3 mg1.02
Oral Semaglutide 7 mg1.01
Oral Semaglutide 14 mg1.00
Sitagliptin 100 mg1.00

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Change From Baseline to Week 26 in Biochemistry Parameter: Sodium (Ratio to Baseline)

Change from baseline in sodium (measured in mmol/L) at week 26 is presented as ratio to baseline. The outcome data was evaluated based on the on-treatment observation period: from date of first dose of trial product following randomization up to the first date of any of the following: follow-up visit, premature follow-up visit, last date on trial product plus 38 days or the end of the in-trial observation period. (NCT04017832)
Timeframe: From baseline to week 26

InterventionRatio of sodium (Geometric Mean)
Oral Semaglutide 3 mg1.00
Oral Semaglutide 7 mg1.00
Oral Semaglutide 14 mg1.00
Sitagliptin 100 mg1.00

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SubstanceRelationship StrengthStudiesTrialsClassesRoles
gamma-aminobutyric acid
gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.		4.2440amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid		human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
adenine
[no description available]		2.21106-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
carbamates
[no description available]		7.3262amino-acid anion
carnitine
[no description available]		2.4110amino-acid betainehuman metabolite;
mouse metabolite
n(g),n(g')-dimethyl-l-arginine
N,N-dimethylarginine: asymmetric dimethylarginine; do not confuse with N,N'-dimethylarginine		2.610alpha-amino acid
3,4-dihydroxyphenylacetic acid
3,4-Dihydroxyphenylacetic Acid: A deaminated metabolite of LEVODOPA.. (3,4-dihydroxyphenyl)acetic acid : A dihydroxyphenylacetic acid having the two hydroxy substituents located at the 3- and 4-positions. It is a metabolite of dopamine.. dihydroxyphenylacetic acid : A dihydroxy monocarboxylic acid consisting of phenylacetic acid having two phenolic hydroxy substituents.		2.1510catechols;
dihydroxyphenylacetic acid		human metabolite
lactic acid
Lactic Acid: A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed). 2-hydroxypropanoic acid : A 2-hydroxy monocarboxylic acid that is propanoic acid in which one of the alpha-hydrogens is replaced by a hydroxy group.		3.16102-hydroxy monocarboxylic acidalgal metabolite;
Daphnia magna metabolite
glycine
[no description available]		3.1310alpha-amino acid;
amino acid zwitterion;
proteinogenic amino acid;
serine family amino acid		EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor;
fundamental metabolite;
hepatoprotective agent;
micronutrient;
neurotransmitter;
NMDA receptor agonist;
nutraceutical
glycerol
Moon: The natural satellite of the planet Earth. It includes the lunar cycles or phases, the lunar month, lunar landscapes, geography, and soil.		2.1310alditol;
triol		algal metabolite;
detergent;
Escherichia coli metabolite;
geroprotector;
human metabolite;
mouse metabolite;
osmolyte;
Saccharomyces cerevisiae metabolite;
solvent
histamine
[no description available]		2.610aralkylamino compound;
imidazoles		human metabolite;
mouse metabolite;
neurotransmitter
imidazole
imidazole: RN given refers to parent cpd. 1H-imidazole : An imidazole tautomer which has the migrating hydrogen at position 1.		2.1710imidazole
thioctic acid
Thioctic Acid: An octanoic acid bridged with two sulfurs so that it is sometimes also called a pentanoic acid in some naming schemes. It is biosynthesized by cleavage of LINOLEIC ACID and is a coenzyme of oxoglutarate dehydrogenase (KETOGLUTARATE DEHYDROGENASE COMPLEX). It is used in DIETARY SUPPLEMENTS.		2.1310dithiolanes;
heterocyclic fatty acid;
thia fatty acid		fundamental metabolite;
geroprotector
methanol
Methanol: A colorless, flammable liquid used in the manufacture of FORMALDEHYDE and ACETIC ACID, in chemical synthesis, antifreeze, and as a solvent. Ingestion of methanol is toxic and may cause blindness.. primary alcohol : A primary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has either three hydrogen atoms attached to it or only one other carbon atom and two hydrogen atoms attached to it.. methanol : The primary alcohol that is the simplest aliphatic alcohol, comprising a methyl and an alcohol group.		2.1310alkyl alcohol;
one-carbon compound;
primary alcohol;
volatile organic compound		amphiprotic solvent;
Escherichia coli metabolite;
fuel;
human metabolite;
mouse metabolite;
Mycoplasma genitalium metabolite
inositol
Inositol: An isomer of glucose that has traditionally been considered to be a B vitamin although it has an uncertain status as a vitamin and a deficiency syndrome has not been identified in man. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1379) Inositol phospholipids are important in signal transduction.. inositol : Any cyclohexane-1,2,3,4,5,6-hexol.. 1D-chiro-inositol : Belonging to the inositol family of compounds, D-chiro-inositol (DCI) is an isomer of glucose. It is an important secondary messenger in insulin signal transduction.. muco-inositol : An inositol that is cyclohexane-1,2,3,4,5,6-hexol having a (1R,2R,3r,4R,5S,6r)-configuration.		8.331210cyclitol;
hexol
melatonin
[no description available]		2.920acetamides;
tryptamines		anticonvulsant;
central nervous system depressant;
geroprotector;
hormone;
human metabolite;
immunological adjuvant;
mouse metabolite;
radical scavenger
niacinamide
nicotinamide : A pyridinecarboxamide that is pyridine in which the hydrogen at position 3 is replaced by a carboxamide group.		4.2850pyridine alkaloid;
pyridinecarboxamide;
vitamin B3		anti-inflammatory agent;
antioxidant;
cofactor;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
Escherichia coli metabolite;
geroprotector;
human urinary metabolite;
metabolite;
mouse metabolite;
neuroprotective agent;
Saccharomyces cerevisiae metabolite;
Sir2 inhibitor
niacin
Niacin: A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.. vitamin B3 : Any member of a group of vitamers that belong to the chemical structural class called pyridines that exhibit biological activity against vitamin B3 deficiency. Vitamin B3 deficiency causes a condition known as pellagra whose symptoms include depression, dermatitis and diarrhea. The vitamers include nicotinic acid and nicotinamide (and their ionized and salt forms).. nicotinic acid : A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group.		2.4110pyridine alkaloid;
pyridinemonocarboxylic acid;
vitamin B3		antidote;
antilipemic drug;
EC 3.5.1.19 (nicotinamidase) inhibitor;
Escherichia coli metabolite;
human urinary metabolite;
metabolite;
mouse metabolite;
plant metabolite;
vasodilator agent
palmitic acid
Palmitic Acid: A common saturated fatty acid found in fats and waxes including olive oil, palm oil, and body lipids.. hexadecanoic acid : A straight-chain, sixteen-carbon, saturated long-chain fatty acid.		2.5820long-chain fatty acid;
straight-chain saturated fatty acid		algal metabolite;
Daphnia magna metabolite;
EC 1.1.1.189 (prostaglandin-E2 9-reductase) inhibitor;
plant metabolite
picolinic acid
picolinic acid: iron-chelating agent that inhibits DNA synthesis; may interfere with iron-dependent production of stable free organic radical which is essential for ribonucleotide reductase formation of deoxyribonucleotides; RN given refers to parent cpd; structure in Merck Index, 9th ed, #7206. picolinic acid : A pyridinemonocarboxylic acid in which the carboxy group is located at position 2. It is an intermediate in the metabolism of tryptophan.		3.4611pyridinemonocarboxylic acidhuman metabolite;
MALDI matrix material
pyridoxal phosphate
Pyridoxal Phosphate: This is the active form of VITAMIN B 6 serving as a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, aminolevulinic acid. During transamination of amino acids, pyridoxal phosphate is transiently converted into pyridoxamine phosphate (PYRIDOXAMINE).. pyridoxal 5'-phosphate : The monophosphate ester obtained by condensation of phosphoric acid with the primary hydroxy group of pyridoxal.		2.2110methylpyridines;
monohydroxypyridine;
pyridinecarbaldehyde;
vitamin B6 phosphate		coenzyme;
cofactor;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
sarcosine
cocobetaine: N-alkyl-betaine; cause of shampoo dermatitis		2.1110N-alkylglycine zwitterion;
N-alkylglycine;
N-methyl-amino acid;
N-methylglycines		Escherichia coli metabolite;
glycine receptor agonist;
glycine transporter 1 inhibitor;
human metabolite;
mouse metabolite
uracil
2,4-dihydroxypyrimidine: a urinary biomarker for bipolar disorder		13.15484pyrimidine nucleobase;
pyrimidone		allergen;
Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
prodrug;
Saccharomyces cerevisiae metabolite
urea
pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.		2.1710isourea;
monocarboxylic acid amide;
one-carbon compound		Daphnia magna metabolite;
Escherichia coli metabolite;
fertilizer;
flour treatment agent;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
1,2-dimethylhydrazine
1,2-Dimethylhydrazine: A DNA alkylating agent that has been shown to be a potent carcinogen and is widely used to induce colon tumors in experimental animals.. 1,2-dimethylhydrazine : A member of the class of hydrazines that is hydrazine in which one of the hydrogens attached to each nitrogen is replaced by a methyl group. A powerful DNA alkylating agent and carcinogen, it is used to induce colon cancer in laboratory rats and mice.		2.4820hydrazinesalkylating agent;
carcinogenic agent
1-anilino-8-naphthalenesulfonate
1-anilino-8-naphthalenesulfonate: RN given refers to parent cpd. 8-anilinonaphthalene-1-sulfonic acid : A naphthalenesulfonic acid that is naphthalene-1-sulfonic acid substituted by a phenylamino group at position 8.		3.5820aminonaphthalene;
naphthalenesulfonic acid		fluorescent probe
phenytoin
[no description available]		2.110imidazolidine-2,4-dioneanticonvulsant;
drug allergen;
sodium channel blocker;
teratogenic agent
5-hydroxydecanoate
5-hydroxydecanoic acid: Potassium Channel Blocker; RN refers to parent cpd		2.1710medium-chain fatty acid
hydroxyindoleacetic acid
(5-hydroxyindol-3-yl)acetic acid : A member of the class of indole-3-acetic acids that is indole-3-acetic acid substituted by a hydroxy group at C-5.		2.1510indole-3-acetic acidsdrug metabolite;
human metabolite;
mouse metabolite
amiodarone
Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.. amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias.		2.05101-benzofurans;
aromatic ketone;
organoiodine compound;
tertiary amino compound		cardiovascular drug
amitriptyline
Amitriptyline: Tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines.. amitriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(dimethylamino)propylidene group at position 5.		2.1310carbotricyclic compound;
tertiary amine		adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
tropomyosin-related kinase B receptor agonist;
xenobiotic
amoxapine
Amoxapine: The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both; it also blocks dopamine receptors. Amoxapine is used for the treatment of depression.. amoxapine : A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position.		2.0610dibenzooxazepineadrenergic uptake inhibitor;
antidepressant;
dopaminergic antagonist;
geroprotector;
serotonin uptake inhibitor
aspirin
Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity.		6.3842benzoic acids;
phenyl acetates;
salicylates		anticoagulant;
antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
EC 1.1.1.188 (prostaglandin-F synthase) inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
plant activator;
platelet aggregation inhibitor;
prostaglandin antagonist;
teratogenic agent
atenolol
Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.		2.110ethanolamines;
monocarboxylic acid amide;
propanolamine		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
sympatholytic agent;
xenobiotic
azathioprine
Azathioprine: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed). azathioprine : A thiopurine that is 6-mercaptopurine in which the mercapto hydrogen is replaced by a 1-methyl-4-nitroimidazol-5-yl group. It is a prodrug for mercaptopurine and is used as an immunosuppressant, prescribed for the treatment of inflammatory conditions and after organ transplantation and also for treatment of Crohn's didease and MS.		3.1710aryl sulfide;
C-nitro compound;
imidazoles;
thiopurine		antimetabolite;
antineoplastic agent;
carcinogenic agent;
DNA synthesis inhibitor;
hepatotoxic agent;
immunosuppressive agent;
prodrug
bisindolylmaleimide i
bisindolylmaleimide I: a bis(indolyl)maleimide		2.1110
verapamil
Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.		3.5911aromatic ether;
nitrile;
polyether;
tertiary amino compound
celecoxib
[no description available]		2.4110organofluorine compound;
pyrazoles;
sulfonamide;
toluenes		cyclooxygenase 2 inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
citalopram
Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group.		2.31102-benzofurans;
cyclic ether;
nitrile;
organofluorine compound;
tertiary amino compound
clonidine
Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group.		2.7220clonidine;
imidazoline
fenofibrate
Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE		3.1910aromatic ether;
chlorobenzophenone;
isopropyl ester;
monochlorobenzenes		antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
fexofenadine
fexofenadine: a second generation antihistamine; metabolite of the antihistaminic drug terfenadine; structure in first source; RN refers to HCl. fexofenadine : A piperidine-based anti-histamine compound.		2.2110piperidines;
tertiary amine		anti-allergic agent;
H1-receptor antagonist
fluconazole
Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis.		3.1710conazole antifungal drug;
difluorobenzene;
tertiary alcohol;
triazole antifungal drug		environmental contaminant;
P450 inhibitor;
xenobiotic
furosemide
Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.		2.1110chlorobenzoic acid;
furans;
sulfonamide		environmental contaminant;
loop diuretic;
xenobiotic
gemfibrozil
[no description available]		3.4611aromatic etherantilipemic drug
gentamicin
Gentamicins: A complex of closely related aminoglycosides obtained from MICROMONOSPORA purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit PROTEIN BIOSYNTHESIS.		2.8630
gliclazide
Gliclazide: An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion.		7.24101N-sulfonylureahypoglycemic agent;
insulin secretagogue;
radical scavenger
glimepiride
glimepiride: structure given in first source		16.596348sulfonamide
glipizide
Glipizide: An oral hypoglycemic agent which is rapidly absorbed and completely metabolized.. glipizide : An N-sulfonylurea that is glyburide in which the (5-chloro-2-methoxybenzoyl group is replaced by a (5-methylpyrazin-2-yl)carbonyl group. An oral hypoglycemic agent, it is used in the treatment of type 2 diabetes mellitus.		9.68157aromatic amide;
monocarboxylic acid amide;
N-sulfonylurea;
pyrazines		EC 2.7.1.33 (pantothenate kinase) inhibitor;
hypoglycemic agent;
insulin secretagogue
glyburide
Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.		8.88166monochlorobenzenes;
N-sulfonylurea		anti-arrhythmia drug;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor;
hypoglycemic agent
hydrochlorothiazide
Hydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.. hydrochlorothiazide : A benzothiadiazine that is 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted by a chloro group at position 6 and a sulfonamide at 7. It is diuretic used for the treatment of hypertension and congestive heart failure.		2.0710benzothiadiazine;
organochlorine compound;
sulfonamide		antihypertensive agent;
diuretic;
environmental contaminant;
xenobiotic
hydroxychloroquine
Hydroxychloroquine: A chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p970). hydroxychloroquine : An aminoquinoline that is chloroquine in which one of the N-ethyl groups is hydroxylated at position 2. An antimalarial with properties similar to chloroquine that acts against erythrocytic forms of malarial parasites, it is mainly used as the sulfate salt for the treatment of lupus erythematosus, rheumatoid arthritis, and light-sensitive skin eruptions.		2.610aminoquinoline;
organochlorine compound;
primary alcohol;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
dermatologic drug
avapro
Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.		2.5420azaspiro compound;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
isoproterenol
Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.		2.9130catechols;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
sympathomimetic agent
staurosporine aglycone
staurosporine aglycone: metabolite from culture broth of Nocardiopsis sp.; a neurotrophin antag; inhibits BDNF TrkB receptor		2.1710
lansoprazole
Lansoprazole: A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers.		6.1232benzimidazoles;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
losartan
Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position		2.4820biphenylyltetrazole;
imidazoles		angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
metformin
Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1.		23.5395202guanidinesenvironmental contaminant;
geroprotector;
hypoglycemic agent;
xenobiotic
nitroglycerin
Nitroglycerin: A volatile vasodilator which relieves ANGINA PECTORIS by stimulating GUANYLATE CYCLASE and lowering cytosolic calcium. It is also sometimes used for TOCOLYSIS and explosives.. nitroglycerol : A nitrate ester that is glycerol in which nitro group(s) replace the hydrogen(s) attached to one or more of the hydroxy groups.. nitroglycerin : A nitroglycerol that is glycerol in which the hydrogen atoms of all three hydroxy groups are replaced by nitro groups. It acts as a prodrug, releasing nitric oxide to open blood vessels and so alleviate heart pain.		3.4611nitroglycerolexplosive;
muscle relaxant;
nitric oxide donor;
prodrug;
tocolytic agent;
vasodilator agent;
xenobiotic
omeprazole
Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.		2.4110aromatic ether;
benzimidazoles;
pyridines;
sulfoxide
o-phthalaldehyde
o-Phthalaldehyde: A reagent that forms fluorescent conjugation products with primary amines. It is used for the detection of many biogenic amines, peptides, and proteins in nanogram quantities in body fluids.. phthalaldehyde : A dialdehyde in which two formyl groups are attached to adjacent carbon centres on a benzene ring.		2.5820benzaldehydes;
dialdehyde		epitope
pioglitazone
Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.		18.58135aromatic ether;
pyridines;
thiazolidinediones		antidepressant;
cardioprotective agent;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hypoglycemic agent;
insulin-sensitizing drug;
PPARgamma agonist;
xenobiotic
piperazine
[no description available]		2.0410azacycloalkane;
piperazines;
saturated organic heteromonocyclic parent		anthelminthic drug
sotalol
Sotalol: An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.. sotalol : A sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is substituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias.		2.3110ethanolamines;
secondary alcohol;
secondary amino compound;
sulfonamide		anti-arrhythmia drug;
beta-adrenergic antagonist;
environmental contaminant;
xenobiotic
vorinostat
Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).		2.2510dicarboxylic acid diamide;
hydroxamic acid		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
temozolomide
[no description available]		2.610imidazotetrazine;
monocarboxylic acid amide;
triazene derivative		alkylating agent;
antineoplastic agent;
prodrug
terfenadine
Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.		2.2110diarylmethane
2,4-thiazolidinedione
thiazolidine-2,4-dione: structure in first source. 1,3-thiazolidine-2,4-dione : A thiazolidenedione carrying oxo substituents at positions 2 and 4.		4.2850thiazolidenedione
trigonelline
trigonelline: in hydra among other organisms; RN given refers to hydroxide inner salt; structure. N-methylnicotinic acid : A pyridinium ion consisting of nicotinic acid having a methyl substituent on the pyridine nitrogen.. N-methylnicotinate : An iminium betaine that is the conjugate base of N-methylnicotinic acid, arising from deprotonation of the carboxy group.		2.1510alkaloid;
iminium betaine		food component;
human urinary metabolite;
plant metabolite
prednisolone
Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone.		4.41111beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
drug metabolite;
environmental contaminant;
immunosuppressive agent;
xenobiotic
sorbitol
D-glucitol : The D-enantiomer of glucitol (also known as D-sorbitol).		4.522glucitolcathartic;
Escherichia coli metabolite;
food humectant;
human metabolite;
laxative;
metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite;
sweetening agent
thymidine
[no description available]		3.5620pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
metabolite;
mouse metabolite
benzimidazole
1H-benzimidazole : The 1H-tautomer of benzimidazole.		2.0510benzimidazole;
polycyclic heteroarene
aldosterone
[no description available]		4.361111beta-hydroxy steroid;
18-oxo steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid hormone;
mineralocorticoid;
primary alpha-hydroxy ketone;
steroid aldehyde		human metabolite;
mouse metabolite
prednisone
Prednisone: A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.. prednisone : A synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid.		2.071011-oxo steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
immunosuppressive agent;
prodrug
pentylenetetrazole
Pentylenetetrazole: A pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GAMMA-AMINOBUTYRIC ACID antagonist. Pentylenetetrazole has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility.. pentetrazol : An organic heterobicyclic compound that is 1H-tetrazole in which the hydrogens at positions 1 and 5 are replaced by a pentane-1,5-diyl group. A central and respiratory stimulant, it was formerly used for the treatment of cough and other respiratory tract disorders, cardiovascular disorders including hypotension, and pruritis.		2.6120organic heterobicyclic compound;
organonitrogen heterocyclic compound
diethylnitrosamine
Diethylnitrosamine: A nitrosamine derivative with alkylating, carcinogenic, and mutagenic properties.. N-nitrosodiethylamine : A nitrosamine that is N-ethylethanamine substituted by a nitroso group at the N-atom.		2.1710nitrosaminecarcinogenic agent;
hepatotoxic agent;
mutagen
biguanides
Biguanides: Derivatives of biguanide (the structure formula HN(C(NH)NH2)2) that are primarily used as oral HYPOGLYCEMIC AGENTS for the treatment of DIABETES MELLITUS, TYPE 2 and PREDIABETES.. biguanides : A class of oral hypoglycemic drugs used for diabetes mellitus or prediabetes treatment. They have a structure based on the 2-carbamimidoylguanidine skeleton.		5.6570guanidines
serine
Serine: A non-essential amino acid occurring in natural form as the L-isomer. It is synthesized from GLYCINE or THREONINE. It is involved in the biosynthesis of PURINES; PYRIMIDINES; and other amino acids.. serine : An alpha-amino acid that is alanine substituted at position 3 by a hydroxy group.		2.0810L-alpha-amino acid;
proteinogenic amino acid;
serine family amino acid;
serine zwitterion;
serine		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
glutamine
Glutamine: A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.. L-glutamine : An optically active form of glutamine having L-configuration.. glutamine : An alpha-amino acid that consists of butyric acid bearing an amino substituent at position 2 and a carbamoyl substituent at position 4.		6.3342amino acid zwitterion;
glutamine family amino acid;
glutamine;
L-alpha-amino acid;
polar amino acid zwitterion;
proteinogenic amino acid		EC 1.14.13.39 (nitric oxide synthase) inhibitor;
Escherichia coli metabolite;
human metabolite;
metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
sucrose
Saccharum: A plant genus of the family POACEAE widely cultivated in the tropics for the sweet cane that is processed into sugar.		2.7830glycosyl glycosidealgal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
osmolyte;
Saccharomyces cerevisiae metabolite;
sweetening agent
ethinyl estradiol
Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration.		3.451117-hydroxy steroid;
3-hydroxy steroid;
terminal acetylenic compound		xenoestrogen
apomorphine
Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.		3.5620aporphine alkaloidalpha-adrenergic drug;
antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
emetic;
serotonergic drug
phenylephrine
Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.. phenylephrine : A member of the class of the class of phenylethanolamines that is (1R)-2-(methylamino)-1-phenylethan-1-ol carrying an additional hydroxy substituent at position 3 on the phenyl ring.		2.2110phenols;
phenylethanolamines;
secondary amino compound		alpha-adrenergic agonist;
cardiotonic drug;
mydriatic agent;
nasal decongestant;
protective agent;
sympathomimetic agent;
vasoconstrictor agent
levodopa
Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease		2.2110amino acid zwitterion;
dopa;
L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		allelochemical;
antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
hapten;
human metabolite;
mouse metabolite;
neurotoxin;
plant growth retardant;
plant metabolite;
prodrug
tyrosine
Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.		10.5651amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine		EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
cloxacillin
Cloxacillin: A semi-synthetic antibiotic that is a chlorinated derivative of OXACILLIN.. cloxacillin : A semisynthetic penicillin antibiotic carrying a 3-(2-chlorophenyl)-5-methylisoxazole-4-carboxamido group at position 6.		2.0710penicillin allergen;
penicillin;
semisynthetic derivative		antibacterial agent;
antibacterial drug
methionine
Methionine: A sulfur-containing essential L-amino acid that is important in many body functions.. methionine : A sulfur-containing amino acid that is butyric acid bearing an amino substituent at position 2 and a methylthio substituent at position 4.		2.930aspartate family amino acid;
L-alpha-amino acid;
methionine zwitterion;
methionine;
proteinogenic amino acid		antidote to paracetamol poisoning;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical
phenylalanine
Phenylalanine: An essential aromatic amino acid that is a precursor of MELANIN; DOPAMINE; noradrenalin (NOREPINEPHRINE), and THYROXINE.. L-phenylalanine : The L-enantiomer of phenylalanine.. phenylalanine : An aromatic amino acid that is alanine in which one of the methyl hydrogens is substituted by a phenyl group.		5.4841amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
phenylalanine;
proteinogenic amino acid		algal metabolite;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
Escherichia coli metabolite;
human xenobiotic metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
norethindrone
Norethindrone: A synthetic progestational hormone with actions similar to those of PROGESTERONE but functioning as a more potent inhibitor of ovulation. It has weak estrogenic and androgenic properties. The hormone has been used in treating amenorrhea, functional uterine bleeding, endometriosis, and for CONTRACEPTION.. norethisterone : A 17beta-hydroxy steroid that is testosterone in which the hydrogen at position 17 is replaced by an ethynyl group and in which the methyl group attached to position 10 is replaced by hydrogen.		3.451117beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
terminal acetylenic compound;
tertiary alcohol		progestin;
synthetic oral contraceptive
cytarabine
[no description available]		2.1710beta-D-arabinoside;
monosaccharide derivative;
pyrimidine nucleoside		antimetabolite;
antineoplastic agent;
antiviral agent;
immunosuppressive agent
valine
Valine: A branched-chain essential amino acid that has stimulant activity. It promotes muscle growth and tissue repair. It is a precursor in the penicillin biosynthetic pathway.. valine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isopropyl group.. L-valine : The L-enantiomer of valine.		2.2110L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid;
valine		algal metabolite;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
isoleucine
Isoleucine: An essential branched-chain aliphatic amino acid found in many proteins. It is an isomer of LEUCINE. It is important in hemoglobin synthesis and regulation of blood sugar and energy levels.. isoleucine : A 2-amino-3-methylpentanoic acid having either (2R,3R)- or (2S,3S)-configuration.. L-isoleucine : The L-enantiomer of isoleucine.		2.0510aspartate family amino acid;
isoleucine;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
arginine
Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group.		4.1650arginine;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		biomarker;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical
tetraethoxysilane
[no description available]		2.610
rotenone
Derris: A plant genus of the family FABACEAE. The root is a source of rotenoids (ROTENONE) and flavonoids. Some species of Pongamia have been reclassified to this genus and some to MILLETTIA. Some species of Deguelia have been reclassified to this genus.. rotenoid : Members of the class of tetrahydrochromenochromene that consists of a cis-fused tetrahydrochromeno[3,4-b]chromene skeleton and its substituted derivatives. The term was originally restricted to natural products, but is now also used to describe semi-synthetic and fully synthetic compounds.		2.5820organic heteropentacyclic compound;
rotenones		antineoplastic agent;
metabolite;
mitochondrial NADH:ubiquinone reductase inhibitor;
phytogenic insecticide;
piscicide;
toxin
quinoxalines
quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.		3.1410mancude organic heterobicyclic parent;
naphthyridine;
ortho-fused heteroarene
tolonium chloride
Tolonium Chloride: A phenothiazine that has been used as a hemostatic, a biological stain, and a dye for wool and silk. Tolonium chloride has also been used as a diagnostic aid for oral and gastric neoplasms and in the identification of the parathyroid gland in thyroid surgery.. tolonium chloride : An organic chloride salt having 3-amino-7-(dimethylamino)-2-methylphenothiazin-5-ium (tolonium) as the counterion. It is a blue nuclear counterstain that can be used to demonstrate Nissl substance and is also useful for staining mast cell granules, both in metachromatic and orthochromatic techniques.		2.610
allyl bromide
[no description available]		2.1110
allylamine
Allylamine: Possesses an unusual and selective cytotoxicity for VASCULAR SMOOTH MUSCLE cells in dogs and rats. Useful for experiments dealing with arterial injury, myocardial fibrosis or cardiac decompensation.		2.7730alkylamine
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		5.541pyrrole;
secondary amine
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		14.53026mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
phenformin
Phenformin: A biguanide hypoglycemic agent with actions and uses similar to those of METFORMIN. Although it is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal, it is still available in some countries. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). phenformin : A member of the class of biguanides that is biguanide in which one of the terminal nitrogen atoms is substituted by a 2-phenylethyl group. It was used as an anti-diabetic drug but was later withdrawn from the market due to potential risk of lactic acidosis.		2.610biguanidesantineoplastic agent;
geroprotector;
hypoglycemic agent
meglumine
Meglumine: 1-Deoxy-1-(methylamino)-D-glucitol. A derivative of sorbitol in which the hydroxyl group in position 1 is replaced by a methylamino group. Often used in conjunction with iodinated organic compounds as contrast medium.. N-methylglucamine : A hexosamine that is D-glucitol in which the hydroxy group at position 1 is substituted by the nitrogen of a methylamino group. A crystalline base, it is used in preparing salts of certain acids for use as diagnostic radiopaque media, while its antimonate is used as an antiprotozoal in the treatment of leishmaniasis.		3.1810hexosamine;
secondary amino compound
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		8.32170azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
indazoles
Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.		3.2110indazole
benzoxazoles
1,3-benzoxazole : A benzoxazole in which the benzene ring is fused to a 1,3-oxazole ring across positions 4 and 5.. benzoxazole : Compounds based on a fused 1,2- or 1,3-oxazole and benzene bicyclic ring skeleton.		2.13101,3-benzoxazoles;
mancude organic heterobicyclic parent
adamantane
Adamantane: A tricyclo bridged hydrocarbon.		19.7418817adamantanes;
polycyclic alkane
isoxazoles
Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.		2.0410isoxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
oxazoles
Oxazoles: Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.. 1,3-oxazole : A five-membered monocyclic heteroarene that is an analogue of cyclopentadiene with O in place of CH2 at position 1 and N in place of CH at position 3.. oxazole : An azole based on a five-membered heterocyclic aromatic skeleton containing one N and one O atom.		3.13101,3-oxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
pyrazines
Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.		26.25809279diazine;
pyrazines		Daphnia magna metabolite
monocrotaline
Monocrotaline: A pyrrolizidine alkaloid and a toxic plant constituent that poisons livestock and humans through the ingestion of contaminated grains and other foods. The alkaloid causes pulmonary artery hypertension, right ventricular hypertrophy, and pathological changes in the pulmonary vasculature. Significant attenuation of the cardiopulmonary changes are noted after oral magnesium treatment.		2.5820pyrrolizidine alkaloid
fluorobenzenes
Fluorobenzenes: Derivatives of BENZENE that contain FLUORINE.. monofluorobenzene : The simplest member of the class of monofluorobenzenes that is benzene carrying a single fluoro substituent.. fluorobenzenes : Any fluoroarene that is a benzene or a substituted benzene carrying at least one fluoro group.		3.5820monofluorobenzenesNMR chemical shift reference compound
limestone
Calcium Carbonate: Carbonic acid calcium salt (CaCO3). An odorless, tasteless powder or crystal that occurs in nature. It is used therapeutically as a phosphate buffer in hemodialysis patients and as a calcium supplement.. calcium carbonate : A calcium salt with formula CCaO3.		2.610calcium salt;
carbonate salt;
inorganic calcium salt;
one-carbon compound		antacid;
fertilizer;
food colouring;
food firming agent
chenodeoxycholic acid
Chenodeoxycholic Acid: A bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.. chenodeoxycholic acid : A dihydroxy-5beta-cholanic acid that is (5beta)-cholan-24-oic acid substituted by hydroxy groups at positions 3 and 7 respectively.. chenodeoxycholate : Conjugate base of chenodeoxycholic acid; major species at pH 7.3.		4.4311bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
phenylpropanolamine
Phenylpropanolamine: A sympathomimetic that acts mainly by causing release of NOREPINEPHRINE but also has direct agonist activity at some adrenergic receptors. It is most commonly used as a nasal vasoconstrictor and an appetite depressant.. phenylpropanolamine : An amphetamine in which the parent 1-phenylpropan-2-amine skeleton is substituted at position 1 with an hydroxy group. A decongestant and appetite suppressant, it is commonly used in prescription and over-the-counter cough and cold preparations.. (-)-norephedrine : An amphetamine that is propylbenzene substituted by a hydroxy group at position 1 and by an amino group at position 2 (the 1R,2S-stereoisomer). It is a plant alkaloid.		2.0710amphetamines;
phenethylamine alkaloid		plant metabolite
thiazolidines
Thiazolidines: Reduced (protonated) form of THIAZOLES. They can be oxidized to THIAZOLIDINEDIONES.		7.33113thiazolidine
malondialdehyde
Malondialdehyde: The dialdehyde of malonic acid.. malonaldehyde : A dialdehyde that is propane substituted by two oxo groups at the terminal carbon atoms respectively. A biomarker of oxidative damage to lipids caused by smoking, it exists in vivo mainly in the enol form.		5.1291dialdehydebiomarker
2-hydroxybutyric acid
2-hydroxybutyric acid: RN given refers to cpd without isomeric designation. hydroxybutyric acid : Any compound comprising a butyric acid core carrying at least one hydroxy substituent.. 2-hydroxybutyric acid : A hydroxybutyric acid having a single hydroxyl group located at position 2; urinary secretion of 2-hydroxybutyric acid is increased with alcohol ingestion or vigorous physical exercise and is associated with lactic acidosis and ketoacidosis in humans and diabetes in animals.		3.48112-hydroxy monocarboxylic acid;
hydroxybutyric acid		algal metabolite;
human metabolite
vinyl bromide
vinyl bromide: structure		2.1110bromoalkene;
monohaloethene
acetylcysteine
N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine.		2.0810acetylcysteine;
L-cysteine derivative;
N-acetyl-L-amino acid		antidote to paracetamol poisoning;
antiinfective agent;
antioxidant;
antiviral drug;
ferroptosis inhibitor;
geroprotector;
human metabolite;
mucolytic;
radical scavenger;
vulnerary
2-piperidone
2-piperidone: structure given in first source. piperidin-2-one : A delta-lactam that is piperidine which is substituted by an oxo group at position 2.		6.6153delta-lactam;
piperidones		EC 1.2.1.88 (L-glutamate gamma-semialdehyde dehydrogenase) inhibitor
d-alpha tocopherol
Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.. tocopherol : A collective name for a group of closely related lipids that contain a chroman-6-ol nucleus substituted at position 2 by a methyl group and by a saturated hydrocarbon chain consisting of three isoprenoid units. They are designated as alpha-, beta-, gamma-, and delta-tocopherol depending on the number and position of additional methyl substituents on the aromatic ring. Tocopherols occur in vegetable oils and vegetable oil products, almost exclusively with R,R,R configuration. Tocotrienols differ from tocopherols only in having three double bonds in the hydrocarbon chain.. vitamin E : Any member of a group of fat-soluble chromanols that exhibit biological activity against vitamin E deficiency. The vitamers in this class consists of a chroman-6-ol core which is substituted at position 2 by a methyl group and (also at position 2) either a saturated or a triply-unsaturated hydrocarbon chain consisting of three isoprenoid units. The major function of vitamin E is to act as a natural antioxidant by scavenging free radicals and molecular oxygen.. (R,R,R)-alpha-tocopherol : An alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils.		2.2110alpha-tocopherolalgal metabolite;
antiatherogenic agent;
anticoagulant;
antioxidant;
antiviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunomodulator;
micronutrient;
nutraceutical;
plant metabolite
s,n,n'-tripropylthiocarbamate
Reward: An object or a situation that can serve to reinforce a response, to satisfy a motive, or to afford pleasure.. vernolate : A monounsaturated fatty acid anion that is the conjugate base of vernolic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.		2.1510tertiary amine
ruthenium
Ruthenium: A hard, brittle, grayish-white rare earth metal with an atomic symbol Ru, atomic number 44, and atomic weight 101.07. It is used as a catalyst and hardener for PLATINUM and PALLADIUM.		2.4720iron group element atom;
platinum group metal atom
titanium
Titanium: A dark-gray, metallic element of widespread distribution but occurring in small amounts with atomic number, 22, atomic weight, 47.867 and symbol, Ti; specific gravity, 4.5; used for fixation of fractures.		2.2510titanium group element atom
cadmium
Cadmium: An element with atomic symbol Cd, atomic number 48, and atomic weight 112.41. It is a metal and ingestion will lead to CADMIUM POISONING.. elemental cadmium : An element in the zinc group of the periodic table with atomic number 48, atomic mass 112, M.P. 321degreeC, and B.P. 765degreeC). An odourless, tasteless, and highly poisonous soft, ductile, lustrous metal with electropositive properties. It has eight stable isotopes: (106)Cd, (108)Cd,(110)Cd, (111)Cd, (112)Cd, (113)Cd, (114)Cd and (116)Cd, with (112)Cd and (114)Cd being the most common.		2.3110cadmium molecular entity;
zinc group element atom
chromium
Chromium: A trace element that plays a role in glucose metabolism. It has the atomic symbol Cr, atomic number 24, and atomic weight 52. According to the Fourth Annual Report on Carcinogens (NTP85-002,1985), chromium and some of its compounds have been listed as known carcinogens.. chromium ion : An chromium atom having a net electric charge.. chromium atom : A chromium group element atom that has atomic number 24.		3.9321chromium group element atom;
metal allergen		micronutrient
europium
Europium: An element of the rare earth family of metals. It has the atomic symbol Eu, atomic number 63, and atomic weight 152. Europium is used in the form of its salts as coatings for cathode ray tubes and in the form of its organic derivatives as shift reagents in NMR spectroscopy.		2.4110f-block element atom;
lanthanoid atom
gold
Gold: A yellow metallic element with the atomic symbol Au, atomic number 79, and atomic weight 197. It is used in jewelry, goldplating of other metals, as currency, and in dental restoration. Many of its clinical applications, such as ANTIRHEUMATIC AGENTS, are in the form of its salts.		2.2510copper group element atom;
elemental gold
tricalcium phosphate
tricalcium phosphate: a form of tricalcium phosphate used as bioceramic bone replacement material; see also records for alpha-tricalcium phosphate, beta-tricalcium phosphate, calcium phosphate; apatitic tricalcium phosphate Ca9(HPO4)(PO4)5(OH) is the calcium orthophosphate leading to beta tricalcium phosphate Ca3(PO4)2 (b-TCP). calcium phosphate : A calcium salt composed of calcium and phosphate/diphosphate ions; present in milk and used for the mineralisation of calcified tissues.		2.4110calcium phosphate
fluorine
Fluorine: A nonmetallic, diatomic gas that is a trace element and member of the halogen family. It is used in dentistry as fluoride (FLUORIDES) to prevent dental caries.		2.830diatomic fluorine;
gas molecular entity		NMR chemical shift reference compound
glycerol 1-stearate
glycerol 1-stearate: isolated from the young fronds of the bracken fern Pteridium aquilinum; structure in first source. rac-1-monostearoylglycerol : A rac-1-monoacylglycerol composed of equal amounts of 3-stearoyl-sn-glycerol and 1-stearoyl-sn-glycerol.. 1-monostearoylglycerol : A 1-monoglyceride that has stearoyl as the acyl group.		2.03101-acylglycerol 18:0;
rac-1-monoacylglycerol		algal metabolite;
Caenorhabditis elegans metabolite
ozone
Ozone: The unstable triatomic form of oxygen, O3. It is a powerful oxidant that is produced for various chemical and industrial uses. Its production is also catalyzed in the ATMOSPHERE by ULTRAVIOLET RAY irradiation of oxygen or other ozone precursors such as VOLATILE ORGANIC COMPOUNDS and NITROGEN OXIDES. About 90% of the ozone in the atmosphere exists in the stratosphere (STRATOSPHERIC OZONE).. ozone : An elemental molecule with formula O3. An explosive, pale blue gas (b.p. -112degreeC) that has a characteristic, pungent odour, it is continuously produced in the upper atmosphere by the action of solar ultraviolet radiation on atmospheric oxygen. It is an antimicrobial agent used in the production of bottled water, as well as in the treatment of meat, poultry and other foodstuffs.		2.2510elemental molecule;
gas molecular entity;
reactive oxygen species;
triatomic oxygen		antiseptic drug;
disinfectant;
electrophilic reagent;
greenhouse gas;
mutagen;
oxidising agent;
tracer
trolamine salicylate
Arthritis: Acute or chronic inflammation of JOINTS.		3.730
diacerein
diacerein: chelates with bivalent metals; a quinone which possesses redox properties; metabolized to active rhein; proposed mechanisms include inhibiting IL1 and metalloproteinases; called a slow acting symptomatic drug in osteoarthritis; no effect of cyclooxygenase;		2.0710anthraquinone
tetradecanoylphorbol acetate
Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.		2.110acetate ester;
diester;
phorbol ester;
tertiary alpha-hydroxy ketone;
tetradecanoate ester		antineoplastic agent;
apoptosis inducer;
carcinogenic agent;
mitogen;
plant metabolite;
protein kinase C agonist;
reactive oxygen species generator
fluorides
[no description available]		2.1110halide anion;
monoatomic fluorine
1-deoxynojirimycin
1-deoxy-nojirimycin: structure in first source. duvoglustat : An optically active form of 2-(hydroxymethyl)piperidine-3,4,5-triol having 2R,3R,4R,5S-configuration.		6.91982-(hydroxymethyl)piperidine-3,4,5-triol;
piperidine alkaloid		anti-HIV agent;
anti-obesity agent;
bacterial metabolite;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
hepatoprotective agent;
hypoglycemic agent;
plant metabolite
daunorubicin
Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola.		2.1110aminoglycoside antibiotic;
anthracycline;
p-quinones;
tetracenequinones		antineoplastic agent;
bacterial metabolite
phenyl acetate
phenyl acetate: The ester formed between phenol and acetic acid. Don't confuse with phenylacetic acid derivatives listed under PHENYLACETATES.. phenyl acetate : An acetate ester obtained by the formal condensation of phenol with acetic acid.		2.4920benzenes;
phenyl acetates
ursodeoxycholic acid
Ursodeoxycholic Acid: An epimer of chenodeoxycholic acid. It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic.. ursodeoxycholic acid : A bile acid found in the bile of bears (Ursidae) as a conjugate with taurine. Used therapeutically, it prevents the synthesis and absorption of cholesterol and can lead to the dissolution of gallstones.. ursodeoxycholate : A bile acid anion that is the conjugate base of ursodeoxycholic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.		4.4311bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
amoxicillin
Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group.		2.1310penicillin allergen;
penicillin		antibacterial drug
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		2.2510taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
substance p
[no description available]		5.3522peptideneurokinin-1 receptor agonist;
neurotransmitter;
vasodilator agent
diltiazem
Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.. diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension.		2.31105-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetateantihypertensive agent;
calcium channel blocker;
vasodilator agent
ng-nitroarginine methyl ester
NG-Nitroarginine Methyl Ester: A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension.		2.5520alpha-amino acid ester;
L-arginine derivative;
methyl ester;
N-nitro compound		EC 1.14.13.39 (nitric oxide synthase) inhibitor
decamethrin
decamethrin: pyrethroid insecticide; RN given refers to cpd without isomeric designation; structure		2.2110aromatic ether;
cyclopropanecarboxylate ester;
nitrile;
organobromine compound		agrochemical;
antifeedant;
calcium channel agonist;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
pyrethroid ester insecticide
meglitinide
meglitinide: structure given in first source & in Negwer, 5th ed, #6436		2.110
indacrinone
indacrinone: polyvalent saluretic; RN given refers to parent cpd without isomeric designation; structure		3.1410
captopril
Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug.		2.2110alkanethiol;
L-proline derivative;
N-acylpyrrolidine;
pyrrolidinemonocarboxylic acid		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
colforsin
Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.		2.110acetate ester;
cyclic ketone;
labdane diterpenoid;
organic heterotricyclic compound;
tertiary alpha-hydroxy ketone;
triol		adenylate cyclase agonist;
anti-HIV agent;
antihypertensive agent;
plant metabolite;
platelet aggregation inhibitor;
protein kinase A agonist
lovastatin
Lovastatin: A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.. lovastatin : A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom).		2.0510delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring)		anticholesteremic drug;
antineoplastic agent;
Aspergillus metabolite;
prodrug
simvastatin
Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.		7.44112delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
statin (semi-synthetic)		EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
ferroptosis inducer;
geroprotector;
prodrug
ranolazine
Ranolazine: An acetanilide and piperazine derivative that functions as a SODIUM CHANNEL BLOCKER and prevents the release of enzymes during MYOCARDIAL ISCHEMIA. It is used in the treatment of ANGINA PECTORIS.. N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide : An aromatic amide obtained by formal condensation of the carboxy group of 2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetic acid with the amino group of 2,6-dimethylaniline.. ranolazine : A racemate comprising equal amounts of (R)- and (S)-ranolazine. Used for treatment of chronic angina.		3.1410aromatic amide;
monocarboxylic acid amide;
monomethoxybenzene;
N-alkylpiperazine;
secondary alcohol
n 0437, (-)-isomer
rotigotine: Antiparkinson Agent and dopamine receptor agonist; structure given in first source; RN given refers to cpd without isomeric designation		2.0410tetralins
clopidogrel
Clopidogrel: A ticlopidine analog and platelet purinergic P2Y receptor antagonist that inhibits adenosine diphosphate-mediated PLATELET AGGREGATION. It is used to prevent THROMBOEMBOLISM in patients with ARTERIAL OCCLUSIVE DISEASES; MYOCARDIAL INFARCTION; STROKE; or ATRIAL FIBRILLATION.. clopidogrel : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group, the methylene hydrogen of which is replaced by a methoxycarbonyl group (the S enantiomer). A P2Y12 receptor antagonist, it is used to inhibit blood clots and prevent heart attacks.		4.5111methyl ester;
monochlorobenzenes;
thienopyridine		anticoagulant;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
atorvastatin
[no description available]		5.4941aromatic amide;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrroles;
statin (synthetic)		environmental contaminant;
xenobiotic
duloxetine hydrochloride
Duloxetine Hydrochloride: A thiophene derivative and selective NEUROTRANSMITTER UPTAKE INHIBITOR for SEROTONIN and NORADRENALINE (SNRI). It is an ANTIDEPRESSIVE AGENT and ANXIOLYTIC, and is also used for the treatment of pain in patients with DIABETES MELLITUS and FIBROMYALGIA.. (S)-duloxetine hydrochloride : A duloxetine hydrochloride in which the duloxetine moiety has S configuration.		2.1310duloxetine hydrochlorideantidepressant
valsartan
Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.		7.1844biphenylyltetrazole;
monocarboxylic acid amide;
monocarboxylic acid		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
adenosine
quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit		3.6120adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
caloreen
caloreen: glucose polymer with average length of five glucose units for dietary energy supplement. dextrin : Glucans produced by the hydrolysis of starch or glycogen. They are mixtures of polymers of D-glucose units linked by alpha(1->4) or alpha(1->6) glycosidic bonds.		2.3110
glucose, (beta-d)-isomer
beta-D-glucose : D-Glucopyranose with beta configuration at the anomeric centre.. (1->4)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->4) linkages.. (1->3)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->3) linkages.		17.557344D-glucopyranoseepitope;
mouse metabolite
fenofibric acid
fenofibric acid: RN given refers to parent cpd without isomeric designation; structure. fenofibric acid : A monocarboxylic acid that is 2-methylpropanoic acid substituted by a 4-(4-chlorobenzoyl)phenoxy group at position 2. It is a metabolite of the drug fenofibrate.		3.1910aromatic ketone;
chlorobenzophenone;
monocarboxylic acid		drug metabolite;
marine xenobiotic metabolite
1,5-anhydroglucitol
1,5-anhydroglucitol: structure. 1,5-anhydro-D-glucitol : An anhydro sugar of D-glucitol.		5.2943anhydro sugarhuman metabolite
betulinic acid
[no description available]		2.1110hydroxy monocarboxylic acid;
pentacyclic triterpenoid		anti-HIV agent;
anti-inflammatory agent;
antimalarial;
antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
plant metabolite
plerixafor
plerixafor: a bicyclam derivate, highly potent & selective inhibitor of HIV-1 & HIV-2. plerixafor : An azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma.		2.1510azacycloalkane;
azamacrocycle;
benzenes;
crown amine;
secondary amino compound;
tertiary amino compound		anti-HIV agent;
antineoplastic agent;
C-X-C chemokine receptor type 4 antagonist;
immunological adjuvant
repaglinide
[no description available]		7.3262piperidines
telmisartan
Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.		2.4620benzimidazoles;
biphenyls;
carboxybiphenyl		angiotensin receptor antagonist;
antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
environmental contaminant;
xenobiotic
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		26.258072791,2,3-triazole
fluorodeoxyglucose f18
Fluorodeoxyglucose F18: The compound is given by intravenous injection to do POSITRON-EMISSION TOMOGRAPHY for the assessment of cerebral and myocardial glucose metabolism in various physiological or pathological states including stroke and myocardial ischemia. It is also employed for the detection of malignant tumors including those of the brain, liver, and thyroid gland. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1162)		2.5202-deoxy-2-((18)F)fluoro-D-glucose;
2-deoxy-2-fluoro-aldehydo-D-glucose
tyrosyltyrosine
tyrosyltyrosine: RN given refers to all-(L)-isomer. tyrosyltyrosine : A dipeptide comprising tyrosine with a tyrosyl residue attached to the alpha-nitrogen.. Tyr-Tyr : Tyrosyltyrosine in which each tyrosine residue has L-configuration.		2.1710tyrosyltyrosineMycoplasma genitalium metabolite
4-o-methyl-12-o-tetradecanoylphorbol 13-acetate
[no description available]		2.110
rosiglitazone
[no description available]		11.08147aminopyridine;
thiazolidinediones		EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug
nicotine
(S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum.		2.15103-(1-methylpyrrolidin-2-yl)pyridineanxiolytic drug;
biomarker;
immunomodulator;
mitogen;
neurotoxin;
nicotinic acetylcholine receptor agonist;
peripheral nervous system drug;
phytogenic insecticide;
plant metabolite;
psychotropic drug;
teratogenic agent;
xenobiotic
diprotin a
[no description available]		3.3660peptide
histidinoalanine
histidinoalanine: cross-linking amino acid in calcified tissue collagen; RN given refers to (L)-isomer		2.0610dipeptide zwitterion;
dipeptide		metabolite
2-amino-4-phenylbutyric acid
2-amino-4-phenylbutanoic acid: structure in first source		2.1110
cobalt
Cobalt: A trace element that is a component of vitamin B12. It has the atomic symbol Co, atomic number 27, and atomic weight 58.93. It is used in nuclear weapons, alloys, and pigments. Deficiency in animals leads to anemia; its excess in humans can lead to erythrocytosis.. cobalt(1+) : A monovalent inorganic cation obtained from cobalt.. cobalt atom : A cobalt group element atom that has atomic number 27.		2.1110cobalt group element atom;
metal allergen		micronutrient
p-methoxy-n-methylphenethylamine
p-Methoxy-N-methylphenethylamine: A potent mast cell degranulator. It is involved in histamine release.. N,O-dimethyltyramine : A secondary amino compound that is tyramine in which the hydrogen of the phenolic hydroxy group has been replaced by a methyl group.		2.0610aromatic ether;
secondary amino compound		metabolite
carbidopa, levodopa drug combination
[no description available]		2.2110
u 73122
1-(6-((3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione: structure given in first source. U-73122 : An aza-steroid that is 3-O-methyl-17beta-estradiol in which the 17beta-hydroxy group is replaced by a 6-(maleimid-1-yl)hexylamino group. An inibitor of phospholipase C.		2.1110aromatic ether;
aza-steroid;
maleimides		EC 3.1.4.11 (phosphoinositide phospholipase C) inhibitor
sr141716
[no description available]		3.1310amidopiperidine;
carbohydrazide;
dichlorobenzene;
monochlorobenzenes;
pyrazoles		anti-obesity agent;
appetite depressant;
CB1 receptor antagonist
deoxypyridinoline
deoxypyridinoline: structure given in first source		3.511
perindopril
Perindopril: An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure.. perindopril : An alpha-amino acid ester that is the ethyl ester of N-{(2S)-1-[(2S,3aS,7aS)-2-carboxyoctahydro-1H-indol-1-yl]-1-oxopropan-2-yl}-L-norvaline		2.0710alpha-amino acid ester;
dicarboxylic acid monoester;
ethyl ester;
organic heterobicyclic compound		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
fingolimod hydrochloride
Fingolimod Hydrochloride: A sphingosine-derivative and IMMUNOSUPPRESSIVE AGENT that blocks the migration and homing of LYMPHOCYTES to the CENTRAL NERVOUS SYSTEM through its action on SPHINGOSINE 1-PHOSPHATE RECEPTORS. It is used in the treatment of MULTIPLE SCLEROSIS.. fingolimod hydrochloride : The hydrochloride salt of 2-amino-2-[2-(4-octylphenyl) ethyl]-1,3-propanediol (fingolimod).		3.2110hydrochlorideimmunosuppressive agent;
prodrug;
sphingosine-1-phosphate receptor agonist
kt 5823
KT 5823: indolocarbazole; activates human neutrophils & fails to inhibit cGMP-dependent protein kinase phosphorylation of vimentin. KT 5823 : An organic heterooctacyclic compound that is 1H,1'H-2,2'-biindole in which the nitrogens have undergone formal oxidative coupling to positions 2 and 5 of methyl (3R)-3-methoxy-2-methyltetrahydrofuran-3-carboxylate (the 2S,3R,5R product), and in which the 3 and 3' positions of the biindole moiety have also undergone formal oxidative coupling to positions 3 and 4 of 1-methyl-1,5-dihydro-2H-pyrrol-2-one.		2.1710gamma-lactam;
hemiaminal;
indolocarbazole;
methyl ester;
organic heterooctacyclic compound		EC 2.7.11.12 (cGMP-dependent protein kinase) inhibitor
deoxyglucose
Deoxyglucose: 2-Deoxy-D-arabino-hexose. An antimetabolite of glucose with antiviral activity.. deoxyglucose : A deoxyhexose comprising glucose having at least one hydroxy group replaced by hydrogen.		5.2943
mitiglinide
mitiglinide: a rapid and short-acting hypoglycemic agent; acts on sulfonylurea receptor closing KATP channels; considered one of the glinides-an imprecise grouping; structure given in first source		7.3576benzenes;
monocarboxylic acid
peroxynitrous acid
Peroxynitrous Acid: A potent oxidant synthesized by the cell during its normal metabolism. Peroxynitrite is formed from the reaction of two free radicals, NITRIC OXIDE and the superoxide anion (SUPEROXIDES).		2.1710nitrogen oxoacid
imatinib mesylate
imatinib methanesulfonate : A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours.		2.1510methanesulfonate saltanticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
angiotensin ii, des-phe(8)-
Ile(5)-angiotensin II (1-7) : An angiotensin compound consisting of the linear heptapeptide sequence L-Asp-L-Arg-L-Val-L-Tyr-L-Ile-L-His-L-Pro.		3.1210amino acid zwitterion;
angiotensin		vasodilator agent
glycyl-arginyl-glycyl-aspartyl-serine
glycyl-arginyl-glycyl-aspartyl-serine: synthetic peptide from fibronectins; inhibits experimental metastasis of murine melanoma cells		2.2510
n,n-dimethylarginine
N,N-dimethylarginine: asymmetric dimethylarginine; do not confuse with N,N'-dimethylarginine. N(omega),N(omega)-dimethyl-L-arginine : A L-arginine derivative having two methyl groups both attached to the primary amino moiety of the guanidino group.		2.610dimethylarginine;
guanidines;
L-arginine derivative;
non-proteinogenic L-alpha-amino acid		EC 1.14.13.39 (nitric oxide synthase) inhibitor
methotrexate
[no description available]		2.6620dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
tamsulosin
[no description available]		2.07105-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamidealpha-adrenergic antagonist;
antineoplastic agent
flustramine b
flustramine B: from Flustra foliacea L.; exhibits muscle relaxant activity both in vivo & in vitro; structure given in first source		3.1410
abiraterone
[no description available]		2.17103beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
pyridines		antineoplastic agent;
EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor
n(4)-octadecyl-1-arabinofuranosylcytosine
[no description available]		2.1710
xylose
xylopyranose: structure in first source		4.3911D-xylose
proline
Proline: A non-essential amino acid that is synthesized from GLUTAMIC ACID. It is an essential component of COLLAGEN and is important for proper functioning of joints and tendons.. proline : An alpha-amino acid that is pyrrolidine bearing a carboxy substituent at position 2.		2.8230amino acid zwitterion;
glutamine family amino acid;
L-alpha-amino acid;
proline;
proteinogenic amino acid		algal metabolite;
compatible osmolytes;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
escitalopram
Escitalopram: S-enantiomer of CITALOPRAM. Belongs to a class of drugs known as SELECTIVE SEROTONIN REUPTAKE INHIBITORS, used to treat depression and generalized anxiety disorder.. escitalopram : A 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile that has S-configuration at the chiral centre. It is the active enantiomer of citalopram.		2.41101-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrileantidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
ezetimibe
Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer).		4.9221azetidines;
beta-lactam;
organofluorine compound		anticholesteremic drug;
antilipemic drug;
antimetabolite
moxifloxacin
Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.		3.4311aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug
as 3201
ranirestat: an aldose reductase inhibitor; AS-3201 and SX-3202 are the (R-(-))- and (S-(+))-isomers, respectively; structure in first source		3.1410
cinacalcet
cinacalcet : A secondary amino compound that is (1R)-1-(naphthalen-1-yl)ethanamine in which one of the hydrogens attached to the nitrogen is substituted by a 3-[3-(trifluoromethyl)phenyl]propyl group.		2.0710(trifluoromethyl)benzenes;
naphthalenes;
secondary amino compound		calcimimetic;
P450 inhibitor
telbivudine
[no description available]		3.1410pyrimidine 2'-deoxyribonucleosideantiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
varenicline
Varenicline: A benzazepine derivative that functions as an ALPHA4-BETA2 NICOTINIC RECEPTOR partial agonist. It is used for SMOKING CESSATION.. varenicline : An organic heterotetracyclic compound that acts as a partial agonist for nicotinic cholinergic receptors and is used (in the form of its tartate salt) as an aid to giving up smoking.		3.1410
lysylproline
lysylproline: third & fourth amino acid in substance P sequence. Lys-Pro : A dipeptide formed from L-lysine and L-proline residues.		2.4110dipeptidemetabolite
angiotensin ii
Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).		4.4270amino acid zwitterion;
angiotensin II		human metabolite
campesterol
campesterol: RN refers to (3beta,24R)-isomer; structure		4.51113beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
C28-steroid;
phytosterols		mouse metabolite
gvs 111
[no description available]		2.520
aflatoxin b1
Aflatoxin B1: A potent hepatotoxic and hepatocarcinogenic mycotoxin produced by the Aspergillus flavus group of fungi. It is also mutagenic, teratogenic, and causes immunosuppression in animals. It is found as a contaminant in peanuts, cottonseed meal, corn, and other grains. The mycotoxin requires epoxidation to aflatoxin B1 2,3-oxide for activation. Microsomal monooxygenases biotransform the toxin to the less toxic metabolites aflatoxin M1 and Q1.. aflatoxin B1 : An aflatoxin having a tetrahydrocyclopenta[c]furo[3',2':4,5]furo[2,3-h]chromene skeleton with oxygen functionality at positions 1, 4 and 11.		2.2510aflatoxin;
aromatic ether;
aromatic ketone		carcinogenic agent;
human metabolite
muraglitazar
muraglitazar: has glucose- and lipid-lowering activities; structure in first source; molecule composed of benzyloxazole-phenoxy-oxybenzylglycine-phenoxyl having structural analogy to PHENOXYBENZAMINE		3.13101,3-oxazoles
lapatinib
[no description available]		2.4110furans;
organochlorine compound;
organofluorine compound;
quinazolines		antineoplastic agent;
tyrosine kinase inhibitor
dabigatran
Dabigatran: A THROMBIN inhibitor which acts by binding and blocking thrombogenic activity and the prevention of thrombus formation. It is used to reduce the risk of stroke and systemic EMBOLISM in patients with nonvalvular atrial fibrillation.. dabigatran : An aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-carbamimidoylphenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amoino group of N-pyridin-2-yl-beta-alanine. The active metabolite of the prodrug dabigatran etexilate, it acts as an anticoagulant which is used for the prevention of stroke and systemic embolism.		2.1710aromatic amide;
benzimidazoles;
beta-alanine derivative;
carboxamidine;
pyridines		anticoagulant;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
EC 3.4.21.5 (thrombin) inhibitor
cholic acid
Cholic Acid: A major primary bile acid produced in the liver and usually conjugated with glycine or taurine. It facilitates fat absorption and cholesterol excretion.. cholic acid : A bile acid that is 5beta-cholan-24-oic acid bearing three alpha-hydroxy substituents at position 3, 7 and 12.		4.431112alpha-hydroxy steroid;
3alpha-hydroxy steroid;
7alpha-hydroxy steroid;
bile acid;
C24-steroid;
trihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
deoxycholic acid
Deoxycholic Acid: A bile acid formed by bacterial action from cholate. It is usually conjugated with glycine or taurine. Deoxycholic acid acts as a detergent to solubilize fats for intestinal absorption, is reabsorbed itself, and is used as a choleretic and detergent.. deoxycholic acid : A bile acid that is 5beta-cholan-24-oic acid substituted by hydroxy groups at positions 3 and 12 respectively.		4.4311bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human blood serum metabolite
3-nitrotyrosine
3-nitrotyrosine: RN given refers to parent cpd without isomeric designation. 3-nitrotyrosine : A nitrotyrosine comprising tyrosine having a nitro group at the 3-position on the phenyl ring.		3.91212-nitrophenols;
C-nitro compound;
nitrotyrosine;
non-proteinogenic alpha-amino acid
benzofurans
Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.		7.3955
o-(chloroacetylcarbamoyl)fumagillol
O-(Chloroacetylcarbamoyl)fumagillol: Semisynthetic analog of fumagillin (a cyclohexane-sesquiterpene antibiotic isolated from ASPERGILLUS FUMIGATUS) that inhibits angiogenesis.. O-(chloroacetylcarbamoyl)fumagillol : A carbamate ester that is fumagillol in which the hydroxy group has been converted to the corresponding N-(chloroacetyl)carbamate derivative.		2.3110carbamate ester;
organochlorine compound;
semisynthetic derivative;
sesquiterpenoid;
spiro-epoxide		angiogenesis inhibitor;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
methionine aminopeptidase 2 inhibitor;
retinoic acid receptor alpha antagonist
glycogen
glycogen : A polydisperse, highly branched glucan composed of chains of D-glucopyranose residues in alpha(1->4) glycosidic linkage, joined together by alpha(1->6) glycosidic linkages. A small number of alpha(1->3) glycosidic linkages and some cumulative alpha(1->6) links also may occur. The branches in glycogen typically contain 8 to 12 glucose residues.		2.1710
bradykinin
[no description available]		5.0831oligopeptidehuman blood serum metabolite;
vasodilator agent
miglitol
[no description available]		6.9198piperidines
n-formylmethionine leucyl-phenylalanine
N-Formylmethionine Leucyl-Phenylalanine: A formylated tripeptide originally isolated from bacterial filtrates that is positively chemotactic to polymorphonuclear leucocytes, and causes them to release lysosomal enzymes and become metabolically activated.. N-formyl-L-methionyl-L-leucyl-L-phenylalanine : A tripeptide composed of L-Met, L-Leu and L-Phe in a linear sequence with a formyl group at the amino terminus. It acts as a potent inducer of leucocyte chemotaxis and macrophage activator as well as a ligand for the FPR receptor.		2.1710tripeptide
ao 128
AO 128: alpha-glucosidase inhibitor; structure given in first source		8.331210organic molecular entity
arachidonic acid
icosa-5,8,11,14-tetraenoic acid : Any icosatetraenoic acid with the double bonds at positions 5, 8, 11 and 14.. arachidonate : A long-chain fatty acid anion resulting from the removal of a proton from the carboxy group of arachidonic acid.		2.0610icosa-5,8,11,14-tetraenoic acid;
long-chain fatty acid;
omega-6 fatty acid		Daphnia galeata metabolite;
EC 3.1.1.1 (carboxylesterase) inhibitor;
human metabolite;
mouse metabolite
resveratrol
trans-resveratrol : A resveratrol in which the double bond has E configuration.		2.1710resveratrolantioxidant;
phytoalexin;
plant metabolite;
quorum sensing inhibitor;
radical scavenger
tacrolimus
Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.		4.6211macrolide lactambacterial metabolite;
immunosuppressive agent
zithromax
Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections.		2.0710macrolide antibioticantibacterial drug;
environmental contaminant;
xenobiotic
epothilone a
Epothilones: A group of 16-member MACROLIDES which stabilize MICROTUBULES in a manner similar to PACLITAXEL. They were originally found in the myxobacterium Sorangium cellulosum, now renamed to Polyangium (MYXOCOCCALES).		2.1310epothilone;
epoxide		antineoplastic agent;
metabolite;
microtubule-stabilising agent;
tubulin modulator
h 89
N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide: structure given in first source. N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A member of the class of isoquinolines that is the sulfonamide obtained by formal condensation of the sulfo group of isoquinoline-5-sulfonic acid with the primary amino group of N(1)-[3-(4-bromophenyl)prop-2-en-1-yl]ethane-1,2-diamine. It is a protein kinase A inhibitor.. (E)-N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide in which the double bond adopts a trans-configuration.		2.2110N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide
dactinomycin
Dactinomycin: A compound composed of a two CYCLIC PEPTIDES attached to a phenoxazine that is derived from STREPTOMYCES parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015)		2.1310actinomycinmutagen
gamma-sitosterol
clionasterol : A member of the class of phytosterols that is poriferast-5-ene carrying a beta-hydroxy substituent at position 3.		4.51113beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
phytosterols		marine metabolite;
plant metabolite
bromochloroacetic acid
Keratins: A class of fibrous proteins or scleroproteins that represents the principal constituent of EPIDERMIS; HAIR; NAILS; horny tissues, and the organic matrix of tooth ENAMEL. Two major conformational groups have been characterized, alpha-keratin, whose peptide backbone forms a coiled-coil alpha helical structure consisting of TYPE I KERATIN and a TYPE II KERATIN, and beta-keratin, whose backbone forms a zigzag or pleated sheet structure. alpha-Keratins have been classified into at least 20 subtypes. In addition multiple isoforms of subtypes have been found which may be due to GENE DUPLICATION.. bromochloroacetic acid : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by bromine while a second is replaced by chlorine. A low-melting (27.5-31.5degreeC), hygroscopic crystalline solid, it can be formed during the disinfection (by chlorination) of water that contains bromide ions and organic matter, so can occur in drinking water as a byproduct of the disinfection process.		2.1102-bromocarboxylic acid;
monocarboxylic acid;
organochlorine compound
glycosides
[no description available]		4.3911
stilbenes
Stilbenes: Organic compounds that contain 1,2-diphenylethylene as a functional group.. trans-stilbene : The trans-isomer of stilbene.		2.5920stilbene
curcumin
Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.. curcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa.		2.2110aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol		anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger
capsaicin
ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief. capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers.		4.7921capsaicinoidnon-narcotic analgesic;
TRPV1 agonist;
voltage-gated sodium channel blocker
D-fructopyranose
[no description available]		3.4360cyclic hemiketal;
D-fructose;
fructopyranose		sweetening agent
thioacetamide
Thioacetamide: A crystalline compound used as a laboratory reagent in place of HYDROGEN SULFIDE. It is a potent hepatocarcinogen.. thioacetamide : A thiocarboxamide consiting of acetamide having the oxygen replaced by sulfur.		2.2110thiocarboxamidehepatotoxic agent
digoxin
Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small.		3.1410cardenolide glycoside;
steroid saponin		anti-arrhythmia drug;
cardiotonic drug;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
epitope
glycylproline
Gly-Pro : A dipeptide consisting of L-proline having a glycyl residue attached to its alpha-amino group.		2.4110dipeptide zwitterion;
dipeptide		metabolite
orlistat
Orlistat: A lactone derivative of LEUCINE that acts as a pancreatic lipase inhibitor to limit the absorption of dietary fat; it is used in the management of obesity.. orlistat : A carboxylic ester resulting from the formal condensation of the carboxy group of N-formyl-L-leucine with the hydroxy group of (3S,4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]oxetan-2-one. A pancreatic lipase inhibitor, it is used as an anti-obesity drug.		2.0510beta-lactone;
carboxylic ester;
formamides;
L-leucine derivative		anti-obesity agent;
bacterial metabolite;
EC 2.3.1.85 (fatty acid synthase) inhibitor;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor
4-(3-3,4-p-menthadien-(1,8)-yl)olivetol
4-(3-3,4-p-menthadien-(1,8)-yl)olivetol: has vasodilating activity		2.610
dasatinib
N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).		2.25101,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
cytellin
cytellin: a phytosterol preparation of mainly B-sitosterol, that was marketed by Eli Lilly to lower cholesterol 1957 to 1982		4.5111
phosphothreonine
Phosphothreonine: The phosphoric acid ester of threonine. Used as an identifier in the analysis of peptides, proteins, and enzymes.. O-phospho-L-threonine : A L-threonine derivative phosphorylated at the side-chain hydroxy function.		2.2510L-threonine derivative;
non-proteinogenic L-alpha-amino acid;
O-phosphoamino acid		Escherichia coli metabolite
ovalbumin
Ovalbumin: An albumin obtained from the white of eggs. It is a member of the serpin superfamily.		3.0340
sodium dodecyl sulfate
Sodium Dodecyl Sulfate: An anionic surfactant, usually a mixture of sodium alkyl sulfates, mainly the lauryl; lowers surface tension of aqueous solutions; used as fat emulsifier, wetting agent, detergent in cosmetics, pharmaceuticals and toothpastes; also as research tool in protein biochemistry.. sodium dodecyl sulfate : An organic sodium salt that is the sodium salt of dodecyl hydrogen sulfate.		2.3110organic sodium saltdetergent;
protein denaturant
crocin
crocin: a free radical scavenger		2.2110
quercetin
[no description available]		3.17407-hydroxyflavonol;
pentahydroxyflavone		antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger
linoleic acid
Linoleic Acid: A doubly unsaturated fatty acid, occurring widely in plant glycosides. It is an essential fatty acid in mammalian nutrition and is used in the biosynthesis of prostaglandins and cell membranes. (From Stedman, 26th ed). linoleic acid : An octadecadienoic acid in which the two double bonds are at positions 9 and 12 and have Z (cis) stereochemistry.		2.0610octadecadienoic acid;
omega-6 fatty acid		algal metabolite;
Daphnia galeata metabolite;
plant metabolite
vitamin k semiquinone radical
vitamin K semiquinone radical: found in active preparations of vitamin K-dependent carboxylase. vitamin K : Any member of a group of fat-soluble 2-methyl-1,4-napthoquinones that exhibit biological activity against vitamin K deficiency. Vitamin K is required for the synthesis of prothrombin and certain other blood coagulation factors.		4.5111
cholecalciferol
Cholecalciferol: Derivative of 7-dehydroxycholesterol formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. It differs from ERGOCALCIFEROL in having a single bond between C22 and C23 and lacking a methyl group at C24.. calciol : A hydroxy seco-steroid that is (5Z,7E)-9,10-secocholesta-5,7,10(19)-triene in which the pro-S hydrogen at position 3 has been replaced by a hydroxy group. It is the inactive form of vitamin D3, being hydroxylated in the liver to calcidiol (25-hydroxyvitamin D3), which is then further hydroxylated in the kidney to give calcitriol (1,25-dihydroxyvitamin D3), the active hormone.		3.3750D3 vitamins;
hydroxy seco-steroid;
seco-cholestane;
secondary alcohol;
steroid hormone		geroprotector;
human metabolite
rutin
Hydroxyethylrutoside: Monohydroxyethyl derivative of rutin. Peripheral circulation stimulant used in treatment of venous disorders.		2.3110disaccharide derivative;
quercetin O-glucoside;
rutinoside;
tetrahydroxyflavone		antioxidant;
metabolite
montelukast
montelukast: a leukotriene D4 receptor antagonist		2.0710aliphatic sulfide;
monocarboxylic acid;
quinolines		anti-arrhythmia drug;
anti-asthmatic drug;
leukotriene antagonist
mangiferin
shamimin: isolated from the leaves of Bombax ceiba; structure in first source		2.0710C-glycosyl compound;
xanthones		anti-inflammatory agent;
antioxidant;
hypoglycemic agent;
plant metabolite
coenzyme q10
coenzyme Q10: Ubiquinone ring with a chain of 10 isoprene units; redox equilibrium with ubiqunol serving in mitochondrial inner membrane to transfer electrons; presence during reconstitution of acetylcholine receptor into phospholipid vesicles yields vesicles active in catalyzing carbamylcholine-sensitive Na+ flux; coenzyme Q10 depletion has been noted with use of statins. coenzyme Q10 : A ubiquinone having a side chain of 10 isoprenoid units. In the naturally occurring isomer, all isoprenyl double bonds are in the E- configuration.		2.1510ubiquinonesantioxidant;
ferroptosis inhibitor;
human metabolite
4-hydroxy-2-nonenal
4-hydroxy-2-nonenal: cytotoxic product from peroxidation of liver microsomal lipids; RN given refers to cpd without isomeric designation. 4-hydroxynon-2-enal : An enal consisting of non-2-ene having an oxo group at the 1-position and a hydroxy group at the 4-position.. 4-hydroxynonenal : A monounsaturated fatty aldehyde that is nonanal that has undergone dehydrogenation to introduce a double bond at any position in the aliphatic chain and in which a hydrogen at position 4 has been replaced by a hydroxy group.		2.31104-hydroxynon-2-enal;
4-hydroxynonenal
sirolimus
Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.		4.6211antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
3-(2,4-dimethoxybenzylidene)anabaseine
3-(2,4-dimethoxybenzylidene)anabaseine: an alpha7nAChR nicotinic receptor agonist		2.4110dimethoxybenzene
bibp 3226
BIBP 3226: a selective non-peptide neuropeptide Y Y1 receptor antagonist; structure given in first source; BIBP-3435 is the S-enantiomer		2.0710
nateglinide
Nateglinide: A phenylalanine and cyclohexane derivative that acts as a hypoglycemic agent by stimulating the release of insulin from the pancreas. It is used in the treatment of TYPE 2 DIABETES.. nateglinide : An N-acyl-D-phenylalanine resulting from the formal condensation of the amino group of D-phenylalanine with the carboxy group of trans-4-isopropylcyclohexanecarboxylic acid. An orally-administered, rapidly-absorbed, short-acting insulinotropic agent, it is used for the treatment of type 2 diabetes mellitus.		5.2531phenylalanine derivative
su 11248
[no description available]		2.3110monocarboxylic acid amide;
pyrroles		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist
dextromethorphan
Dextromethorphan: Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity.. dextromethorphan : A 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough.		4.43116-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthreneantitussive;
environmental contaminant;
neurotoxin;
NMDA receptor antagonist;
oneirogen;
prodrug;
xenobiotic
lisinopril
Lisinopril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure.		2.110dipeptideEC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
ramipril
Ramipril: A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.. ramipril : A dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.. quark : Quarks comprise one of two classes of the fundamental particles. Quarks possess fractional electric charges and are not observed in free state. The word "quark" first appears in James Joyce's Finnegans Wake and has been chosen by Murray Gell-Mann as a name for fundamental building blocks of particles.		3.811azabicycloalkane;
cyclopentapyrrole;
dicarboxylic acid monoester;
dipeptide;
ethyl ester		bradykinin receptor B2 agonist;
cardioprotective agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
matrix metalloproteinase inhibitor;
prodrug
minfiensine
minfiensine: structure in first source		3.1410
enalapril
Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration).		5.341dicarboxylic acid monoester;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
geroprotector;
prodrug
fumarates
Fumarates: Compounds based on fumaric acid.. fumarate(2-) : A C4-dicarboxylate that is the E-isomer of but-2-enedioate(2-)		4.0940butenedioate;
C4-dicarboxylate		human metabolite;
metabolite;
Saccharomyces cerevisiae metabolite
enalaprilat anhydrous
Enalaprilat: The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.. enalaprilat dihydrate : The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection.. enalaprilat (anhydrous) : Enalapril in which the ethyl ester group has been hydrolysed to the corresponding carboxylic acid. Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor and is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is given by intravenous injection, usually as the dihydrate.		4.411dicarboxylic acid;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
pregabalin
Pregabalin: A gamma-aminobutyric acid (GABA) derivative that functions as a CALCIUM CHANNEL BLOCKER and is used as an ANTICONVULSANT as well as an ANTI-ANXIETY AGENT. It is also used as an ANALGESIC in the treatment of NEUROPATHIC PAIN and FIBROMYALGIA.. pregabalin : A gamma-amino acid that is gamma-aminobutyric acid (GABA) carrying an isobutyl substitutent at the beta-position (the S-enantiomer). Binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues.		3.9130gamma-amino acidanticonvulsant;
calcium channel blocker
aliskiren
aliskiren: orally active nonpeptidic renin inhibitor. aliskiren : A monomethoxybenzene compound having a 3-methoxypropoxy group at the 2-position and a multi-substituted branched alkyl substituent at the 4-position.		4.0940monocarboxylic acid amide;
monomethoxybenzene		antihypertensive agent
selenium
Selenium: An element with the atomic symbol Se, atomic number 34, and atomic weight 78.97. It is an essential micronutrient for mammals and other animals but is toxic in large amounts. Selenium protects intracellular structures against oxidative damage. It is an essential component of GLUTATHIONE PEROXIDASE.		2.3110chalcogen;
nonmetal atom		micronutrient
oxalates
Oxalates: Derivatives of OXALIC ACID. Included under this heading are a broad variety of acid forms, salts, esters, and amides that are derived from the ethanedioic acid structure.		2.4110
axitinib
[no description available]		3.2110aryl sulfide;
benzamides;
indazoles;
pyridines		antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist
sq-23377
Ionomycin: A divalent calcium ionophore that is widely used as a tool to investigate the role of intracellular calcium in cellular processes.. ionomycin : A very long-chain fatty acid that is docosa-10,16-dienoic acid which is substituted by methyl groups at positions 4, 6, 8, 12, 14, 18 and 20, by hydroxy groups at positions 11, 19 and 21, and by a (2',5-dimethyloctahydro-2,2'-bifuran-5-yl)ethanol group at position 21. An ionophore produced by Streptomyces conglobatus, it is used in research to raise the intracellular level of Ca(2+) and as a research tool to understand Ca(2+) transport across biological membranes.		2.0710cyclic ether;
enol;
polyunsaturated fatty acid;
very long-chain fatty acid		calcium ionophore;
metabolite
vildagliptin
[no description available]		19.0514714amino acid amide
sacubitril
[no description available]		6.1522biphenyls
lobeglitazone
lobeglitazone: putative antidiabetic agent for type 2 diabetes; structure in first source		8.3563aromatic ether
paliperidone palmitate
Paliperidone Palmitate: A benzisoxazole derivative and active metabolite of RISPERIDONE that functions as a DOPAMINE D2 RECEPTOR ANTAGONIST and SEROTONIN 5-HT2 RECEPTOR ANTAGONIST. It is an ANTIPSYCHOTIC AGENT used in the treatment of SCHIZOPHRENIA.. 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-2-methyl-4-oxo-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-9-yl hexadecanoate : A fatty acid ester obtained by the formal condensation of the carboxy group of hexadecanoic acid with the hydroxy group of 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one.. paliperidone palmitate : A racemate comprising equimolar amounts of (R)- and (S)-paliperidone palmitate. A long-acting injectable formulation of paliperidone (the major active metabolite of risperidone) that is used for treatment of schizophrenia.		2.04101,2-benzoxazoles;
fatty acid ester;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine
mocetinostat
mocetinostat: undergoing phase II clinical trials for treatment of cancer. mocetinostat : A benzamide obtained by formal condensation of the carboxy group of 4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzoic acid with one of the amino groups of benzene-1,2-diamine. It is an orally active and isotype-selective HDAC inhibitor which exhibits antitumour activity (IC50 = 0.15, 0.29, 1.66 and 0.59 muM for HDAC1, HDAC2, HDAC3 and HDAC11).		2.0610aminopyrimidine;
benzamides;
pyridines;
secondary amino compound;
secondary carboxamide;
substituted aniline		antineoplastic agent;
apoptosis inducer;
autophagy inducer;
cardioprotective agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
hepatotoxic agent
ticagrelor
Ticagrelor: An adenosine triphosphate analogue and reversible P2Y12 PURINORECEPTOR antagonist that inhibits ADP-mediated PLATELET AGGREGATION. It is used for the prevention of THROMBOEMBOLISM by patients with ACUTE CORONARY SYNDROME or a history of MYOCARDIAL INFARCTION.. ticagrelor : A triazolopyrimidine that is an adenosine isostere; the cyclopentane ring is similar to ribose and the nitrogen-rich [1,2,3]triazolo[4,5-d]pyrimidine moiety resembles the nucleobase adenine. A platelet aggregation inhibitor which is used for prevention of thromboembolic events in patients with acute coronary syndrome.		3.2110aryl sulfide;
hydroxyether;
organofluorine compound;
secondary amino compound;
triazolopyrimidines		P2Y12 receptor antagonist;
platelet aggregation inhibitor
lipid a
Lipid A: Lipid A is the biologically active component of lipopolysaccharides. It shows strong endotoxic activity and exhibits immunogenic properties.. lipid A : The glycolipid moiety of bacterial lipopolysaccharide (R can be either hydrogen or a fatty acyl group).		6.7533dodecanoate ester;
lipid A;
tetradecanoate ester		Escherichia coli metabolite
dapagliflozin
[no description available]		12.862414aromatic ether;
C-glycosyl compound;
monochlorobenzenes		hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor
tofacitinib
tofacitinib : A pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely active rheumatoid arthritis.		2.2510N-acylpiperidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound		antirheumatic drug;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
pasireotide
pasireotide : A six-membered homodetic cyclic peptide composed from L-phenylglycyl, D-tryptophyl, L-lysyl, O-benzyl-L-tyrosyl, L-phenylalanyl and modified L-hydroxyproline residues joined in sequence. A somatostatin analogue with pharmacologic properties mimicking those of the natural hormone somatostatin; used (as its diaspartate salt) for treatment of Cushing's disease.		3.9221homodetic cyclic peptide;
peptide hormone		antineoplastic agent
linagliptin
Linagliptin: A purine and quinazoline derivative that functions as an INCRETIN and DIPEPTIDYL-PEPTIDASE IV INHIBTOR. It is used as a HYPOGLYCEMIC AGENT in the treatment of TYPE II DIABETES MELLITUS.. linagliptin : A xanthine that is 7H-xanthine bearing (4-methylquinazolin-2-yl)methyl, methyl, but-2-yn-1-yl and 3-aminopiperidin-1-yl substituents at positions 1, 3, 7 and 8 respectively (the R-enantiomer). Used for treatment of type II diabetes.		10.45540aminopiperidine;
quinazolines		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
hypoglycemic agent
bibw 2992
[no description available]		2.610aromatic ether;
enamide;
furans;
monochlorobenzenes;
organofluorine compound;
quinazolines;
secondary carboxamide;
tertiary amino compound		antineoplastic agent;
tyrosine kinase inhibitor
7-aminoactinomycin d
7-aminoactinomycin D: staining reagent used in flow cytometry		2.1310
piragliatin
piragliatin: glucokinase activator		3.5111
ipragliflozin
[no description available]		9.591211glycoside
oxadiazoles
Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.		7.1754
uamc00039
UAMC00039: dipeptidyl peptidase II inhibitor; structure in first source		2.0510
alogliptin
alogliptin: structure in first source. alogliptin : A piperidine that is 3-methyl-2,4-dioxo-3,4-dihydropyrimidine carrying additional 2-cyanobenzyl and 3-aminopiperidin-1-yl groups at positions 1 and 2 respectively (the R-enantiomer). Used in the form of its benzoate salt for treatment of type 2 diabetes.		13.17494nitrile;
piperidines;
primary amino compound;
pyrimidines		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
hypoglycemic agent
psn 632408
PSN 632408: a GPR119 agonist; structure in first source		2.0810
losartan potassium
Erythropoietin: Glycoprotein hormone, secreted chiefly by the KIDNEY in the adult and the LIVER in the FETUS, that acts on erythroid stem cells of the BONE MARROW to stimulate proliferation and differentiation.		3.1910
empagliflozin
[no description available]		13.37339aromatic ether;
C-glycosyl compound;
monochlorobenzenes;
tetrahydrofuryl ether		hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor
lc15-0444
LC15-0444: Dipeptidyl Peptidase IV Inhibitors; orally active small molecule for the treatment of type II diabetes		6.4443organonitrogen compound;
organooxygen compound
pituitrin
Pituitrin: A substance or extract from the neurohypophysis (PITUITARY GLAND, POSTERIOR).		3.5111
phytosterols
Phytosterols: A class of organic compounds known as sterols or STEROIDS derived from plants.. phytosterols : Sterols similar to cholesterol which occur in plants and vary only in carbon side chains and/or presence or absence of a double bond.		4.5111
mdv 3100
[no description available]		2.1710(trifluoromethyl)benzenes;
benzamides;
imidazolidinone;
monofluorobenzenes;
nitrile;
thiocarbonyl compound		androgen antagonist;
antineoplastic agent
trelagliptin
trelagliptin: a dipeptidyl peptidase IV inhibitor		3.6820benzenes;
nitrile
cytochrome c-t
Cytochromes c: Cytochromes of the c type that are found in eukaryotic MITOCHONDRIA. They serve as redox intermediates that accept electrons from MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX III and transfer them to MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX IV.		2.1110
atrial natriuretic factor
Atrial Natriuretic Factor: A potent natriuretic and vasodilatory peptide or mixture of different-sized low molecular weight PEPTIDES derived from a common precursor and secreted mainly by the HEART ATRIUM. All these peptides share a sequence of about 20 AMINO ACIDS.		2.110polypeptide
xenin 25
xenin 25: 25 amino acid peptide having 6 C-terminal amino acids in common with amphibian xenopsin; amino acid sequence given in first source		2.6920
glucagon-like peptide 1 (7-36)amide
glucagon-like peptide 1 (7-36)amide: potent stimulator of insulin released in perfused mammalian pancreas		5.0831
gastrins
Gastrins: A family of gastrointestinal peptide hormones that excite the secretion of GASTRIC JUICE. They may also occur in the central nervous system where they are presumed to be neurotransmitters.		3.4411
glucagon
Glucagon: A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. Glucagon is secreted by PANCREATIC ALPHA CELLS and plays an important role in regulation of BLOOD GLUCOSE concentration, ketone metabolism, and several other biochemical and physiological processes. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1511). glucagon : A 29-amino acid peptide hormone consisting of His, Ser, Gln, Gly, Thr, Phe, Thr, Ser, Asp, Tyr, Ser, Lys, Tyr, Leu, Asp, Ser, Arg, Arg, Ala, Gln, Asp, Phe, Val, Gln, Trp, Leu, Met, Asn and Thr residues joined in sequence.		14.564722peptide hormone
neuropeptide y
Neuropeptide Y: A 36-amino acid peptide present in many organs and in many sympathetic noradrenergic neurons. It has vasoconstrictor and natriuretic activity and regulates local blood flow, glandular secretion, and smooth muscle activity. The peptide also stimulates feeding and drinking behavior and influences secretion of pituitary hormones.		4.7561
glucagon-like peptide 1 (7-36)
[no description available]		2.2510
liraglutide
[no description available]		19.2513731lipopeptide;
polypeptide		glucagon-like peptide-1 receptor agonist;
neuroprotective agent
glucagon-like peptide 1
Glucagon-Like Peptide 1: A peptide of 36 or 37 amino acids that is derived from PROGLUCAGON and mainly produced by the INTESTINAL L CELLS. GLP-1(1-37 or 1-36) is further N-terminally truncated resulting in GLP-1(7-37) or GLP-1-(7-36) which can be amidated. These GLP-1 peptides are known to enhance glucose-dependent INSULIN release, suppress GLUCAGON release and gastric emptying, lower BLOOD GLUCOSE, and reduce food intake.		22.3230186
insulin glulisine
insulin glulisine: provides greater beta-cell protective action		3.4811
insulin detemir
Insulin Detemir: A recombinant long-acting insulin and hypoglycemic agent in which a MYRISTIC ACID is conjugated to a LYSINE at position B29. It is used to manage BLOOD GLUCOSE levels in patients with DIABETES MELLITUS.		6.6943
diapep 277
DiaPep 277: a 24-mer laboratory-made peptide derived from Hsp60(437-460)		3.1710
alx-0600
ALX-0600: glucagon-like peptide 2 (GLP-2) analog. teduglutide : A 33-membered polypeptide consisting of His, Gly, Asp, Gly, Ser, Phe, Ser, Asp, Glu, Met, Asn, Thr, Ile, Leu, Asp, Asn, Leu, Ala, Ala, Arg, Asp, Phe, Ile, Asn, Trp, Leu, Ile, Gln, Thr, Lys, Ile, Thr and Asp residues joined in sequence. A glucagon-like peptide-2 receptor agonist used for the treatment of short-bowel syndrome.		2.0710polypeptideantioxidant;
glucagon-like peptide-2 receptor agonist;
metabolite;
protective agent
incretins
Incretins: Peptides which stimulate INSULIN release from the PANCREATIC BETA CELLS following oral nutrient ingestion, or postprandially.		17.9312424
c-peptide
C-Peptide: The middle segment of proinsulin that is between the N-terminal B-chain and the C-terminal A-chain. It is a pancreatic peptide of about 31 residues, depending on the species. Upon proteolytic cleavage of proinsulin, equimolar INSULIN and C-peptide are released. C-peptide immunoassay has been used to assess pancreatic beta cell function in diabetic patients with circulating insulin antibodies or exogenous insulin. Half-life of C-peptide is 30 min, almost 8 times that of insulin.		13.263322
natriuretic peptide, c-type
Natriuretic Peptide, C-Type: A PEPTIDE of 22 amino acids, derived mainly from cells of VASCULAR ENDOTHELIUM. It is also found in the BRAIN, major endocrine glands, and other tissues. It shares structural homology with ATRIAL NATRIURETIC FACTOR. It has vasorelaxant activity thus is important in the regulation of vascular tone and blood flow. Several high molecular weight forms containing the 22 amino acids have been identified.		4.7211
exendin (9-39)
exendin (9-39): a peptide from the venom of the lizard Heloderma suspectum; inhibits glucagon-like peptide-1 (GLP-1) induced cAMP production; its structure is related to exendin-4		3.8921
endothelin-1
Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)		2.1310
ubiquinone
Ubiquinone: A lipid-soluble benzoquinone which is involved in ELECTRON TRANSPORT in mitochondrial preparations. The compound occurs in the majority of aerobic organisms, from bacteria to higher plants and animals.		2.1510
chitosan
[no description available]		2.7220
raltegravir potassium
Raltegravir Potassium: A pyrrolidinone derivative and HIV INTEGRASE INHIBITOR that is used in combination with other ANTI-HIV AGENTS for the treatment of HIV INFECTION.		2.1710
gdc 0449
HhAntag691: inhibits the hedgehog pathway and ABC transporters; has antineoplastic activity		3.2110benzamides;
monochlorobenzenes;
pyridines;
sulfone		antineoplastic agent;
Hedgehog signaling pathway inhibitor;
SMO receptor antagonist;
teratogenic agent
canagliflozin
canagliflozin hydrate : A hydrate that is the hemihydrate form of canagliflozin. Used for treatment of type II diabetes via inhibition of sodium-glucose transport protein subtype 2.		15.884927C-glycosyl compound;
organofluorine compound;
thiophenes		hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor
imeglimin
imeglimin: a tetrahydrotriazine-containing oral antidiabetic		6.3452
insulin, isophane
Insulin, Isophane: An intermediate-acting INSULIN preparation with onset time of 2 hours and duration of 24 hours. It is produced by crystallizing ZINC-insulin-PROTAMINES at neutral pH 7. Thus it is called neutral protamine Hagedorn for inventor Hans Christian Hagedorn.		4.8621
sitagliptin phosphate, metformin hydrochloride drug combination
Sitagliptin Phosphate, Metformin Hydrochloride Drug Combination: A pharmaceutical preparation of sitagliptin phosphate and metformin hydrochloride that is used in the treatment of TYPE 2 DIABETES.		6.5751
tak-875
[no description available]		4.8232biphenyls
quetiapine fumarate
Quetiapine Fumarate: A dibenzothiazepine and ANTIPSYCHOTIC AGENT that targets the SEROTONIN 5-HT2 RECEPTOR; HISTAMINE H1 RECEPTOR, adrenergic alpha1 and alpha2 receptors, as well as the DOPAMINE D1 RECEPTOR and DOPAMINE D2 RECEPTOR. It is used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER and DEPRESSIVE DISORDER.		2.0510fumarate salt
cardiovascular agents
Cardiovascular Agents: Agents that affect the rate or intensity of cardiac contraction, blood vessel diameter, or blood volume.		521
neurotensin
neurotensin, Tyr(11)-: RN given refers to parent cpd & (D)-isomer; RN for cpd without isomeric designation not avail 5/91		2.6920peptide hormonehuman metabolite;
mitogen;
neurotransmitter;
vulnerary
incb-018424
[no description available]		2.610nitrile;
pyrazoles;
pyrrolopyrimidine		antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
tolterodine tartrate
Tolterodine Tartrate: An ANTIMUSCARINIC AGENT selective for the MUSCARINIC RECEPTORS of the BLADDER that is used in the treatment of URINARY INCONTINENCE and URINARY URGE INCONTINENCE.		2.0710tartrate salt
glycolipids
[no description available]		2.2510
piperidines
Piperidines: A family of hexahydropyridines.		14.11586
interleukin-8
Interleukin-8: A member of the CXC chemokine family that plays a role in the regulation of the acute inflammatory response. It is secreted by variety of cell types and induces CHEMOTAXIS of NEUTROPHILS and other inflammatory cells.		3.4811
anagliptin
anagliptin: anagliptin hydrochloride salt is the active compound		9.74116amino acid amide
pf 04971729
ertugliflozin: structure in first source		10.96117diarylmethane
sofosbuvir
Sofosbuvir: A uridine monophosphate analog inhibitor of HEPATITIS C VIRUS (HCV) polymerase NS5B that is used as an ANTIVIRAL AGENT in the treatment of CHRONIC HEPATITIS C.. sofosbuvir : A nucleotide conjugate that is used in combination with ledipasvir (under the trade name Harvoni) for the treatment of chronic hepatitis C genotype 1 infection.		3.2110isopropyl ester;
L-alanyl ester;
nucleotide conjugate;
organofluorine compound;
phosphoramidate ester		antiviral drug;
hepatitis C protease inhibitor;
prodrug
exenatide
Exenatide: A synthetic form of exendin-4, a 39-amino acid peptide isolated from the venom of the Gila monster lizard (Heloderma suspectum). Exenatide increases CYCLIC AMP levels in pancreatic acinar cells and acts as a GLUCAGON-LIKE PEPTIDE-1 RECEPTOR (GLP-1) agonist and incretin mimetic, enhancing insulin secretion in response to increased glucose levels; it also suppresses inappropriate glucagon secretion and slows gastric emptying. It is used an anti-diabetic and anti-obesity agent.		19.9717035
pf-04937319
N,N-dimethyl-5-((2-methyl-6-((5-methylpyrazin-2-yl)carbamoyl)benzofuran-4-yl)oxy)pyrimidine-2-carboxamide: a glucokinase activator; structure in first source		6.533
natriuretic peptide, brain
Natriuretic Peptide, Brain: A PEPTIDE that is secreted by the BRAIN and the HEART ATRIA, stored mainly in cardiac ventricular MYOCARDIUM. It can cause NATRIURESIS; DIURESIS; VASODILATION; and inhibits secretion of RENIN and ALDOSTERONE. It improves heart function. It contains 32 AMINO ACIDS.		7.3183polypeptide
piroxicam
[no description available]		2.0710benzothiazine;
monocarboxylic acid amide;
pyridines		analgesic;
antirheumatic drug;
cyclooxygenase 1 inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
warfarin
Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.		3.4311benzenes;
hydroxycoumarin;
methyl ketone
lornoxicam
lornoxicam : A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 6-chloro-4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain, primarily resulting from inflammatory diseases of the joints, osteoarthritis, surgery, sciatica and other inflammations.		2.0710heteroaryl hydroxy compound;
monocarboxylic acid amide;
organochlorine compound;
pyridines;
thienothiazine		antipyretic;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
epidermal growth factor
Epidermal Growth Factor: A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.		2.1110
transforming growth factor beta
Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.		5.761
semaglutide
[no description available]		13.52412lipopeptide;
polypeptide		anti-obesity agent;
appetite depressant;
glucagon-like peptide-1 receptor agonist;
hypoglycemic agent;
neuroprotective agent
am 1638
[no description available]		2.2510
(1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl)methyl methanesulfonate
(1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl)methyl methanesulfonate: a GPR119 agonist		5.8322
pyrethrins
[no description available]		2.2110
chiglitazar
chiglitazar: structure in first source		6.7633
osimertinib
osimertinib: an EGFR tyrosine kinase inhibitor. osimertinib : A member of the class of aminopyrimidines that is 4-(1-methylindol-3-yl)pyrimidin-2-amine in which one of the amino hydrogens is replaced by a 2-methoxy-4-[2-(dimethylamino)ethyl](methyl)amino-5-acrylamidophenyl group. Used (as the mesylate salt) for treatment of EGFR T790M mutation positive non-small cell lung cancer.		2.610acrylamides;
aminopyrimidine;
biaryl;
indoles;
monomethoxybenzene;
secondary amino compound;
secondary carboxamide;
substituted aniline;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist
glutaminase
[no description available]		3.1410
cyclin d1
Cyclin D1: Protein encoded by the bcl-1 gene which plays a critical role in regulating the cell cycle. Overexpression of cyclin D1 is the result of bcl-1 rearrangement, a t(11;14) translocation, and is implicated in various neoplasms.		2.1110
caseins
Caseins: A mixture of related phosphoproteins occurring in milk and cheese. The group is characterized as one of the most nutritive milk proteins, containing all of the common amino acids and rich in the essential ones.		2.3110
peptide yy
peptide YY (3-36): amino acid sequence given in first source		2.0710
glucagon-like peptide 2
Glucagon-Like Peptide 2: A 33-amino acid peptide derived from the C-terminal of PROGLUCAGON and mainly produced by the INTESTINAL L CELLS. It stimulates intestinal mucosal growth and decreased apoptosis of ENTEROCYTES. GLP-2 enhances gastrointestinal function and plays an important role in nutrient homeostasis.		4.1631
angiotensin i
Angiotensin I: A decapeptide that is cleaved from precursor angiotensinogen by RENIN. Angiotensin I has limited biological activity. It is converted to angiotensin II, a potent vasoconstrictor, after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME.. angiotensin I : A ten amino acid peptide formed by renin cleavage of angiotensinogen. Angiotensin I has no direct biological function except that high levels can stimulate catecholamine production. It is metabolized to its biologically active byproduct angiotensin II, a potent vasoconstrictor, by angiotensin converting enzyme (ACE) through cleavage of the two terminal amino acids.. angiotensin I dizwitterion : A peptide zwitterion that is the dizwitterionic form of angiotensin I having both carboxy groups deprotonated and the aspartyl amino group and arginine side-chain protonated. It is the major species at pH 7.3.		3.1210angiotensin;
peptide zwitterion		human metabolite;
neurotransmitter agent
nephrin
nephrin: gene nephrin is mutated in congenital nephrotic syndrome; amino acid sequence in first source; GenBank F19541; RefSeq NM_019459 (mouse), NM_004646 (human), NM_022628 (rat)		2.610
vitamin b 12
Vitamin B 12: A cobalt-containing coordination compound produced by intestinal micro-organisms and found also in soil and water. Higher plants do not concentrate vitamin B 12 from the soil and so are a poor source of the substance as compared with animal tissues. INTRINSIC FACTOR is important for the assimilation of vitamin B 12.		2.3110
insulin glargine
Insulin Glargine: A recombinant LONG ACTING INSULIN and HYPOGLYCEMIC AGENT that is used to manage BLOOD GLUCOSE in patients with DIABETES MELLITUS.		18.37637
insulin degludec
[no description available]		4.8121
oxyntomodulin
Glucagon-Like Peptides: Peptides derived from proglucagon which is also the precursor of pancreatic GLUCAGON. Despite expression of proglucagon in multiple tissues, the major production site of glucagon-like peptides (GLPs) is the INTESTINAL L CELLS. GLPs include glucagon-like peptide 1, glucagon-like peptide 2, and the various truncated forms.		15.163717
cyclosporine
Cyclosporine: A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).		4.9421
peptide yy
Peptide YY: A 36-amino acid peptide produced by the L cells of the distal small intestine and colon. Peptide YY inhibits gastric and pancreatic secretion.. peptide YY : A 36-membered human gut polypeptide consisting of Tyr, Pro, Ile, Lys, Pro, Glu, Ala, Pro, Gly, Glu, Asp, Ala, Ser, Pro, Glu, Glu, Leu, Asn, Arg, Tyr, Tyr, Ala, Ser, Leu, Arg, His, Tyr, Leu, Asn, Leu, Val, Thr, Arg, Gln, Arg and Tyr-NH2 residues joined in sequence.		6.8753
orabase
Orabase: used in therapy of oral mucosal ulcers		2.4110
exendin 3
exendin 3: from the gila monster lizard (Heloderma horridum); amino acid sequence given in first source		2.2110
exudates
Malaysia: A parliamentary democracy with a constitutional monarch in southeast Asia, consisting of 11 states (West Malaysia) on the Malay Peninsula and two states (East Malaysia) on the island of BORNEO. It is also called the Federation of Malaysia. Its capital is Kuala Lumpur. Before 1963 it was the Union of Malaya. It reorganized in 1948 as the Federation of Malaya, becoming independent from British Malaya in 1957 and becoming Malaysia in 1963 as a federation of Malaya, Sabah, Sarawak, and Singapore (which seceded in 1965). The form Malay- probably derives from the Tamil malay, mountain, with reference to its geography. (From Webster's New Geographical Dictionary, 1988, p715 & Room, Brewer's Dictionary of Names, 1992, p329)		4.3711
cyclic gmp
Cyclic GMP: Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed). 3',5'-cyclic GMP : A 3',5'-cyclic purine nucleotide in which the purine nucleobase is specified as guanidine.		2.53203',5'-cyclic purine nucleotide;
guanyl ribonucleotide		Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
deoxyguanosine
[no description available]		3.4811purine 2'-deoxyribonucleoside;
purines 2'-deoxy-D-ribonucleoside		Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
guanine
[no description available]		2.06102-aminopurines;
oxopurine;
purine nucleobase		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
guanosine
ribonucleoside : Any nucleoside where the sugar component is D-ribose.		3.711guanosines;
purines D-ribonucleoside		fundamental metabolite
clozapine
Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.		2.0510benzodiazepine;
N-arylpiperazine;
N-methylpiperazine;
organochlorine compound		adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
GABA antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
xenobiotic
allopurinol
Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.. allopurinol : A bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring.		2.0610nucleobase analogue;
organic heterobicyclic compound		antimetabolite;
EC 1.17.3.2 (xanthine oxidase) inhibitor;
gout suppressant;
radical scavenger
8-hydroxyguanosine
8-hydroxyguanosine: immunostimulant for B lymphocytes; structure given in first source		3.711purine nucleoside
aprepitant
Aprepitant: A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING.. aprepitant : A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors.		3.811(trifluoromethyl)benzenes;
cyclic acetal;
morpholines;
triazoles		antidepressant;
antiemetic;
neurokinin-1 receptor antagonist;
peripheral nervous system drug;
substance P receptor antagonist
8-hydroxyguanine
7,8-dihydro-8-oxoguanine: was substituted for guanine at G(8), G(9), G(14), or G(15) in the human telomeric oligonucleotide 5'-d[AGGGTTAG(8)G(9)GTT AG(14)G(15)GTTAGGGTGT]-3'. 7,8-dihydro-8-oxoguanine : An oxopurine that is guanine in which the hydrogen at position 8 is replaced by an oxo group and in which the nitrogens at positions 7 and 9 each bear a hydrogen.		2.0610oxopurine
8-hydroxy-2'-deoxyguanosine
8-Hydroxy-2'-Deoxyguanosine: Common oxidized form of deoxyguanosine in which C-8 position of guanine base has a carbonyl group.. 8-hydroxy-2'-deoxyguanosine : Guanosine substituted at the purine 8-position by a hydroxy group. It is used as a biomarker of oxidative DNA damage.		4.5122guanosinesbiomarker
carbidopa
Carbidopa: An inhibitor of DOPA DECARBOXYLASE that prevents conversion of LEVODOPA to dopamine. It is used in PARKINSON DISEASE to reduce peripheral adverse effects of LEVODOPA. It has no anti-parkinson activity by itself.. carbidopa : The hydrate of 3-(3,4-dihydroxyphenyl)propanoic acid in which the hydrogens alpha- to the carboxyl group are substituted by hydrazinyl and methyl groups (S-configuration). Carbidopa is a dopa decarboxylase inhibitor, so prevents conversion of levodopa to dopamine. It has no antiparkinson activity by itself, but is used in the management of Parkinson's disease to reduce peripheral adverse effects of levodopa.		2.2110
concanavalin a
Concanavalin A: A MANNOSE/GLUCOSE binding lectin isolated from the jack bean (Canavalia ensiformis). It is a potent mitogen used to stimulate cell proliferation in lymphocytes, primarily T-lymphocyte, cultures.		2.3110
leptin
Leptin: A 16-kDa peptide hormone secreted from WHITE ADIPOCYTES. Leptin serves as a feedback signal from fat cells to the CENTRAL NERVOUS SYSTEM in regulation of food intake, energy balance, and fat storage.		4.0221
pyrimidinones
Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O.		3.1410
ConditionIndicatedRelationship StrengthStudiesTrials
Alloxan Diabetes
[description not available]		07.6850
Diabetes Mellitus
A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.		115.48559
Diabetes Mellitus, Adult-Onset
[description not available]		029.811,585743
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		131.811,585743
Vascular Calcification
Deposition of calcium into the blood vessel structures. Excessive calcification of the vessels are associated with ATHEROSCLEROTIC PLAQUES formation particularly after MYOCARDIAL INFARCTION (see MONCKEBERG MEDIAL CALCIFIC SCLEROSIS) and chronic kidney diseases which in turn increase VASCULAR STIFFNESS.		02.3110
Impaired Glucose Tolerance
[description not available]		010.941811
Apoplexy
[description not available]		011.171510
Acute Ischemic Stroke
[description not available]		03.711
Cerebral Ischemia
[description not available]		04.2331
Anterior Circulation Transient Ischemic Attack
[description not available]		04.5322
Ischemic Stroke
Stroke due to BRAIN ISCHEMIA resulting in interruption or reduction of blood flow to a part of the brain. When obstruction is due to a BLOOD CLOT formed within in a cerebral blood vessel it is a thrombotic stroke. When obstruction is formed elsewhere and moved to block a cerebral blood vessel (see CEREBRAL EMBOLISM) it is referred to as embolic stroke. Wake-up stroke refers to ischemic stroke occurring during sleep while cryptogenic stroke refers to ischemic stroke of unknown origin.		03.711
Brain Ischemia
Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.		04.2331
Ischemic Attack, Transient
Brief reversible episodes of focal, nonconvulsive ischemic dysfunction of the brain having a duration of less than 24 hours, and usually less than one hour, caused by transient thrombotic or embolic blood vessel occlusion or stenosis. Events may be classified by arterial distribution, temporal pattern, or etiology (e.g., embolic vs. thrombotic). (From Adams et al., Principles of Neurology, 6th ed, pp814-6)		04.5322
Glucose Intolerance
A pathological state in which BLOOD GLUCOSE level is less than approximately 140 mg/100 ml of PLASMA at fasting, and above approximately 200 mg/100 ml plasma at 30-, 60-, or 90-minute during a GLUCOSE TOLERANCE TEST. This condition is seen frequently in DIABETES MELLITUS, but also occurs with other diseases and MALNUTRITION.		010.941811
Stroke
A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)		113.171510
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		021.64230151
Lung Injury, Acute
[description not available]		02.3110
Innate Inflammatory Response
[description not available]		013.275310
Acute Edematous Pancreatitis
[description not available]		08.94331
Acute Disease
Disease having a short and relatively severe course.		08.12191
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		013.275310
Pancreatitis
INFLAMMATION of the PANCREAS. Pancreatitis is classified as acute unless there are computed tomographic or endoscopic retrograde cholangiopancreatographic findings of CHRONIC PANCREATITIS (International Symposium on Acute Pancreatitis, Atlanta, 1992). The two most common forms of acute pancreatitis are ALCOHOLIC PANCREATITIS and gallstone pancreatitis.		08.94331
Acute Lung Injury
A condition of lung damage that is characterized by bilateral pulmonary infiltrates (PULMONARY EDEMA) rich in NEUTROPHILS, and in the absence of clinical HEART FAILURE. This can represent a spectrum of pulmonary lesions, endothelial and epithelial, due to numerous factors (physical, chemical, or biological).		02.3110
2019 Novel Coronavirus Disease
[description not available]		05.51110
Cicatrization
The formation of fibrous tissue in the place of normal tissue during the process of WOUND HEALING. It includes scar tissue formation occurring in healing internal organs as well as in the skin after surface injuries.		02.7220
Cicatrix
The fibrous tissue that replaces normal tissue during the process of WOUND HEALING.		02.7220
Brain Vascular Disorders
[description not available]		02.4110
Cardiac Failure
[description not available]		016.436330
Cardiovascular Stroke
[description not available]		012.543515
Cerebrovascular Disorders
A spectrum of pathological conditions of impaired blood flow in the brain. They can involve vessels (ARTERIES or VEINS) in the CEREBRUM, the CEREBELLUM, and the BRAIN STEM. Major categories include INTRACRANIAL ARTERIOVENOUS MALFORMATIONS; BRAIN ISCHEMIA; CEREBRAL HEMORRHAGE; and others.		02.4110
Heart Failure
A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.		016.436330
Myocardial Infarction
NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).		114.543515
Diabetic Glomerulosclerosis
[description not available]		010.19326
Diabetic Nephropathies
KIDNEY injuries associated with diabetes mellitus and affecting KIDNEY GLOMERULUS; ARTERIOLES; KIDNEY TUBULES; and the interstitium. Clinical signs include persistent PROTEINURIA, from microalbuminuria progressing to ALBUMINURIA of greater than 300 mg/24 h, leading to reduced GLOMERULAR FILTRATION RATE and END-STAGE RENAL DISEASE.		010.19326
Insulin Sensitivity
[description not available]		014.947025
Insulin Resistance
Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.		014.947025
Disease Exacerbation
[description not available]		010.38226
Endometrioma
An enlarged area of ENDOMETRIOSIS that resembles a tumor. It is usually found in the OVARY. When it is filled with old blood, it is known as a chocolate cyst.		02.4110
Endometriosis
A condition in which functional endometrial tissue is present outside the UTERUS. It is often confined to the PELVIS involving the OVARY, the ligaments, cul-de-sac, and the uterovesical peritoneum.		02.4110
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		09.47761
Polycystic Ovarian Syndrome
[description not available]		08.4993
Polycystic Ovary Syndrome
A complex disorder characterized by infertility, HIRSUTISM; OBESITY; and various menstrual disturbances such as OLIGOMENORRHEA; AMENORRHEA; ANOVULATION. Polycystic ovary syndrome is usually associated with bilateral enlarged ovaries studded with atretic follicles, not with cysts. The term, polycystic ovary, is misleading.		08.4993
Maternal Obesity
[description not available]		02.4110
Diseases, Metabolic
[description not available]		02.4110
Metabolic Diseases
Generic term for diseases caused by an abnormal metabolic process. It can be congenital due to inherited enzyme abnormality (METABOLISM, INBORN ERRORS) or acquired due to disease of an endocrine organ or failure of a metabolically important organ such as the liver. (Stedman, 26th ed)		02.4110
Obesity
A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).		013.35515
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		06.4753
Fatty Liver, Nonalcoholic
[description not available]		010.35317
Cirrhosis, Liver
[description not available]		03.4360
Liver Cirrhosis
Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.		03.4360
Non-alcoholic Fatty Liver Disease
Fatty liver finding without excessive ALCOHOL CONSUMPTION.		010.35317
Acute Onset Vascular Dementia
[description not available]		02.4110
Dementia, Vascular
An imprecise term referring to dementia associated with CEREBROVASCULAR DISORDERS, including CEREBRAL INFARCTION (single or multiple), and conditions associated with chronic BRAIN ISCHEMIA. Diffuse, cortical, and subcortical subtypes have been described. (From Gerontol Geriatr 1998 Feb;31(1):36-44)		02.4110
Graft-Versus-Host Disease
[description not available]		06.4771
Graft vs Host Disease
The clinical entity characterized by anorexia, diarrhea, loss of hair, leukopenia, thrombocytopenia, growth retardation, and eventual death brought about by the GRAFT VS HOST REACTION.		06.4771
Cardiac Diseases
[description not available]		011.471816
Heart Diseases
Pathological conditions involving the HEART including its structural and functional abnormalities.		011.471816
Diabetes Mellitus Type 1.5
[description not available]		09.74106
Latent Autoimmune Diabetes in Adults
Autoimmune diabetes in adults with slowly progressive PANCREATIC BETA CELL failure and the presence of circulating autoantibodies to PANCREATIC ISLETS cell antigens.		09.74106
Cardiometabolic Syndrome
A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components not only include metabolic dysfunctions of METABOLIC SYNDROME but also HYPERTENSION, and ABDOMINAL OBESITY.		08.41165
Metabolic Syndrome
A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components of metabolic syndrome include ABDOMINAL OBESITY; atherogenic DYSLIPIDEMIA; HYPERTENSION; HYPERGLYCEMIA; INSULIN RESISTANCE; a proinflammatory state; and a prothrombotic (THROMBOSIS) state.		08.41165
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		017.957750
Cirrhosis
[description not available]		05.11140
Elevated Cholesterol
[description not available]		05.7561
Fibrosis
Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.		05.11140
Hypercholesterolemia
A condition with abnormally high levels of CHOLESTEROL in the blood. It is defined as a cholesterol value exceeding the 95th percentile for the population.		05.7561
Necrosis
The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.		02.8630
Injuries, Radiation
[description not available]		02.4110
Anoxemia
[description not available]		03.4320
Injury, Myocardial Reperfusion
[description not available]		03.0640
Hypoxia
Sub-optimal OXYGEN levels in the ambient air of living organisms.		03.4320
Acute Confusional Senile Dementia
[description not available]		04.5780
Alzheimer Disease
A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)		04.5780
Angioneurotic Edema
[description not available]		03.3660
Angioedema
Swelling involving the deep DERMIS, subcutaneous, or submucosal tissues, representing localized EDEMA. Angioedema often occurs in the face, lips, tongue, and larynx.		03.3660
Pemphigoid
[description not available]		05.62140
Pemphigoid, Bullous
A chronic and relatively benign subepidermal blistering disease usually of the elderly and without histopathologic acantholysis.		05.62140
Rheumatoid Arthritis
[description not available]		02.8630
Arthritis, Rheumatoid
A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.		02.8630
Malignant Melanoma
[description not available]		02.4110
Melanoma
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)		02.4110
Injuries, Multiple
[description not available]		02.610
Complications of Diabetes Mellitus
[description not available]		08.81222
Dyslipidemia
[description not available]		09.78115
Asymmetric Diabetic Proximal Motor Neuropathy
[description not available]		07.4952
Blood Pressure, High
[description not available]		09.75216
Albuminuria
The presence of albumin in the urine, an indicator of KIDNEY DISEASES.		013.043229
Diabetic Neuropathies
Peripheral, autonomic, and cranial nerve disorders that are associated with DIABETES MELLITUS. These conditions usually result from diabetic microvascular injury involving small blood vessels that supply nerves (VASA NERVORUM). Relatively common conditions which may be associated with diabetic neuropathy include third nerve palsy (see OCULOMOTOR NERVE DISEASES); MONONEUROPATHY; mononeuropathy multiplex; diabetic amyotrophy; a painful POLYNEUROPATHY; autonomic neuropathy; and thoracoabdominal neuropathy. (From Adams et al., Principles of Neurology, 6th ed, p1325)		07.4952
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		09.75216
Dyslipidemias
Abnormalities in the serum levels of LIPIDS, including overproduction or deficiency. Abnormal serum lipid profiles may include high total CHOLESTEROL, high TRIGLYCERIDES, low HIGH DENSITY LIPOPROTEIN CHOLESTEROL, and elevated LOW DENSITY LIPOPROTEIN CHOLESTEROL.		09.78115
Fasting Hypoglycemia
HYPOGLYCEMIA expressed in the postabsorptive state, after prolonged FASTING, or an overnight fast.		024.22290101
Hypoglycemia
A syndrome of abnormally low BLOOD GLUCOSE level. Clinical hypoglycemia has diverse etiologies. Severe hypoglycemia eventually lead to glucose deprivation of the CENTRAL NERVOUS SYSTEM resulting in HUNGER; SWEATING; PARESTHESIA; impaired mental function; SEIZURES; COMA; and even DEATH.		024.22290101
Atherogenesis
[description not available]		011.733118
Chronic Kidney Diseases
[description not available]		010.55174
Atherosclerosis
A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.		011.733118
Renal Insufficiency, Chronic
Conditions in which the KIDNEYS perform below the normal level for more than three months. Chronic kidney insufficiency is classified by five stages according to the decline in GLOMERULAR FILTRATION RATE and the degree of kidney damage (as measured by the level of PROTEINURIA). The most severe form is the end-stage renal disease (CHRONIC KIDNEY FAILURE). (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002)		010.55174
Prediabetes
[description not available]		05.1642
Weight Reduction
[description not available]		019.88135118
Prediabetic State
The time period before the development of symptomatic diabetes. For example, certain risk factors can be observed in subjects who subsequently develop INSULIN RESISTANCE as in type 2 diabetes (DIABETES MELLITUS, TYPE 2).		05.1642
Weight Loss
Decrease in existing BODY WEIGHT.		019.88135118
Autoimmune Diabetes
[description not available]		021.4218115
Diabetes Mellitus, Type 1
A subtype of DIABETES MELLITUS that is characterized by INSULIN deficiency. It is manifested by the sudden onset of severe HYPERGLYCEMIA, rapid progression to DIABETIC KETOACIDOSIS, and DEATH unless treated with insulin. The disease may occur at any age, but is most common in childhood or adolescence.		021.4218115
Adverse Drug Event
[description not available]		04.9271
Drug-Related Side Effects and Adverse Reactions
Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.		04.9271
Depression
Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders.		05.2491
Diabetic Retinopathy
Disease of the RETINA as a complication of DIABETES MELLITUS. It is characterized by the progressive microvascular complications, such as ANEURYSM, interretinal EDEMA, and intraocular PATHOLOGIC NEOVASCULARIZATION.		04.970
Allergic Rhinitis
[description not available]		02.610
Rhinitis, Allergic
An inflammation of the NASAL MUCOSA triggered by ALLERGENS.		02.610
Carcinoma, Non-Small Cell Lung
[description not available]		03.0120
Cancer of Lung
[description not available]		03.1130
Thrombopenia
[description not available]		02.610
Carcinoma, Non-Small-Cell Lung
A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.		03.0120
Lung Neoplasms
Tumors or cancer of the LUNG.		03.1130
Thrombocytopenia
A subnormal level of BLOOD PLATELETS.		02.610
Liver Steatosis
[description not available]		06.84122
Fatty Liver
Lipid infiltration of the hepatic parenchymal cells resulting in a yellow-colored liver. The abnormal lipid accumulation is usually in the form of TRIGLYCERIDES, either as a single large droplet or multiple small droplets. Fatty liver is caused by an imbalance in the metabolism of FATTY ACIDS.		06.84122
Benign Neoplasms, Brain
[description not available]		02.610
Astrocytoma, Grade IV
[description not available]		02.610
Glial Cell Tumors
[description not available]		02.610
Brain Neoplasms
Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.		02.610
Glioblastoma
A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.		02.610
Glioma
Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)		02.610
Kidney Failure
A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.		07.0392
Renal Insufficiency
Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.		19.0392
Kidney Diseases
Pathological processes of the KIDNEY or its component tissues.		07.08103
Diastolic Heart Failure
[description not available]		02.610
Heart Failure, Diastolic
Heart failure caused by abnormal myocardial relaxation during DIASTOLE leading to defective cardiac filling.		02.610
Idiopathic Parkinson Disease
[description not available]		03.5720
Parkinson Disease
A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)		03.5720
Heart Disease, Ischemic
[description not available]		05.6661
Myocardial Ischemia
A disorder of cardiac function caused by insufficient blood flow to the muscle tissue of the heart. The decreased blood flow may be due to narrowing of the coronary arteries (CORONARY ARTERY DISEASE), to obstruction by a thrombus (CORONARY THROMBOSIS), or less commonly, to diffuse narrowing of arterioles and other small vessels within the heart. Severe interruption of the blood supply to the myocardial tissue may result in necrosis of cardiac muscle (MYOCARDIAL INFARCTION).		05.6661
Breast Cancer
[description not available]		03.0640
Breast Neoplasms
Tumors or cancer of the human BREAST.		03.0640
Hyperglycemia, Postprandial
Abnormally high BLOOD GLUCOSE level after a meal.		018.5411076
Hyperglycemia
Abnormally high BLOOD GLUCOSE level.		018.5411076
Encephalopathy, Traumatic
[description not available]		02.7620
Brain Injuries, Traumatic
A form of acquired brain injury which occurs when a sudden trauma causes damage to the brain.		02.7620
Diarrhea
An increased liquidity or decreased consistency of FECES, such as running stool. Fecal consistency is related to the ratio of water-holding capacity of insoluble solids to total water, rather than the amount of water present. Diarrhea is not hyperdefecation or increased fecal weight.		08.8264
Injury, Ischemia-Reperfusion
[description not available]		04.99130
Reperfusion Injury
Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.		04.99130
Left Ventricular Dysfunction
[description not available]		07.1873
Ventricular Dysfunction, Left
A condition in which the LEFT VENTRICLE of the heart was functionally impaired. This condition usually leads to HEART FAILURE; MYOCARDIAL INFARCTION; and other cardiovascular complications. Diagnosis is made by measuring the diminished ejection fraction and a depressed level of motility of the left ventricular wall.		07.1873
Angina at Rest
[description not available]		08.1855
Auricular Fibrillation
[description not available]		08.2255
Angina, Unstable
Precordial pain at rest, which may precede a MYOCARDIAL INFARCTION.		08.1855
Atrial Fibrillation
Abnormal cardiac rhythm that is characterized by rapid, uncoordinated firing of electrical impulses in the upper chambers of the heart (HEART ATRIA). In such case, blood cannot be effectively pumped into the lower chambers of the heart (HEART VENTRICLES). It is caused by abnormal impulse generation.		08.2255
Abnormality, Torsion
[description not available]		02.2510
Testicular Diseases
Pathological processes of the TESTIS.		02.6920
Cancer of Pancreas
[description not available]		07.491
Pancreatic Neoplasms
Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).		07.491
Blood Clot
[description not available]		02.2510
Thrombosis
Formation and development of a thrombus or blood clot in the blood vessel.		02.2510
Experimental Hepatoma
[description not available]		02.6120
Benign Neoplasms
[description not available]		04.1530
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		04.1530
Nasopharyngitis
Inflammation of the NASOPHARYNX, usually including its mucosa, related lymphoid structure, and glands.		02.2510
Cough
A sudden, audible expulsion of air from the lungs through a partially closed glottis, preceded by inhalation. It is a protective response that serves to clear the trachea, bronchi, and/or lungs of irritants and secretions, or to prevent aspiration of foreign materials into the lungs.		02.2510
Airflow Obstruction, Chronic
[description not available]		02.2510
Pulmonary Disease, Chronic Obstructive
A disease of chronic diffuse irreversible airflow obstruction. Subcategories of COPD include CHRONIC BRONCHITIS and PULMONARY EMPHYSEMA.		02.2510
Cancer of Stomach
[description not available]		02.2510
Stomach Neoplasms
Tumors or cancer of the STOMACH.		02.2510
Arteriosclerosis, Coronary
[description not available]		09.83155
Coronary Artery Disease
Pathological processes of CORONARY ARTERIES that may derive from a congenital abnormality, atherosclerotic, or non-atherosclerotic cause.		09.83155
Health Care Associated Infection
[description not available]		02.2510
Infections, Serratia
[description not available]		02.2510
Cross Infection
Any infection which a patient contracts in a health-care institution.		02.2510
Cryptogenic Fibrosing Alveolitis
[description not available]		02.2510
Idiopathic Pulmonary Fibrosis
A common interstitial lung disease of unknown etiology, usually occurring between 50-70 years of age. Clinically, it is characterized by an insidious onset of breathlessness with exertion and a nonproductive cough, leading to progressive DYSPNEA. Pathological features show scant interstitial inflammation, patchy collagen fibrosis, prominent fibroblast proliferation foci, and microscopic honeycomb change.		02.2510
Anemia
A reduction in the number of circulating ERYTHROCYTES or in the quantity of HEMOGLOBIN.		03.6411
Infections, Coronavirus
[description not available]		03.3650
Pneumonia, Viral
Inflammation of the lung parenchyma that is caused by a viral infection.		03.3650
Coronavirus Infections
Virus diseases caused by the CORONAVIRUS genus. Some specifics include transmissible enteritis of turkeys (ENTERITIS, TRANSMISSIBLE, OF TURKEYS); FELINE INFECTIOUS PERITONITIS; and transmissible gastroenteritis of swine (GASTROENTERITIS, TRANSMISSIBLE, OF SWINE).		03.3650
Injuries, Spinal Cord
[description not available]		02.2510
Spinal Cord Injuries
Penetrating and non-penetrating injuries to the spinal cord resulting from traumatic external forces (e.g., WOUNDS, GUNSHOT; WHIPLASH INJURIES; etc.).		02.2510
Vascular Diseases
Pathological processes involving any of the BLOOD VESSELS in the cardiac or peripheral circulation. They include diseases of ARTERIES; VEINS; and rest of the vasculature system in the body.		02.3110
Cognition Disorders
Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment.		05.4370
Absence Seizure
[description not available]		02.6120
Seizures
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.		02.6120
Deficiency, IgG
[description not available]		02.2510
Mononeuritis
[description not available]		02.6920
Mononeuropathies
Disease or trauma involving a single peripheral nerve in isolation, or out of proportion to evidence of diffuse peripheral nerve dysfunction. Mononeuropathy multiplex refers to a condition characterized by multiple isolated nerve injuries. Mononeuropathies may result from a wide variety of causes, including ISCHEMIA; traumatic injury; compression; CONNECTIVE TISSUE DISEASES; CUMULATIVE TRAUMA DISORDERS; and other conditions.		02.6920
Hematologic Malignancies
[description not available]		05.1231
Hematologic Neoplasms
Neoplasms located in the blood and blood-forming tissue (the bone marrow and lymphatic tissue). The commonest forms are the various types of LEUKEMIA, of LYMPHOMA, and of the progressive, life-threatening forms of the MYELODYSPLASTIC SYNDROMES.		05.1231
Adjuvant Arthritis
[description not available]		02.2510
Complication, Postoperative
[description not available]		018.691451
Postoperative Complications
Pathologic processes that affect patients after a surgical procedure. They may or may not be related to the disease for which the surgery was done, and they may or may not be direct results of the surgery.		018.691451
Carcinoma, Ehrlich Tumor
A transplantable, poorly differentiated malignant tumor which appeared originally as a spontaneous breast carcinoma in a mouse. It grows in both solid and ascitic forms.		02.3110
Alopecia Circumscripta
[description not available]		02.3110
Alopecia Areata
Loss of scalp and body hair involving microscopically inflammatory patchy areas.		02.3110
Cancer of Ovary
[description not available]		02.2510
Invasiveness, Neoplasm
[description not available]		02.9130
Ovarian Neoplasms
Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.		02.2510
Choline Deficiency
A condition produced by a deficiency of CHOLINE in animals. Choline is known as a lipotropic agent because it has been shown to promote the transport of excess fat from the liver under certain conditions in laboratory animals. Combined deficiency of choline (included in the B vitamin complex) and all other methyl group donors causes liver cirrhosis in some animals. Unlike compounds normally considered as vitamins, choline does not serve as a cofactor in enzymatic reactions. (From Saunders Dictionary & Encyclopedia of Laboratory Medicine and Technology, 1984)		02.5720
Proteinuria
The presence of proteins in the urine, an indicator of KIDNEY DISEASES.		03.2250
Recrudescence
[description not available]		05.2331
Acute Lymphoid Leukemia
[description not available]		04.6211
Granulocytic Leukemia
[description not available]		04.6211
Dysmyelopoietic Syndromes
[description not available]		04.6211
Leukemia, Myeloid
Form of leukemia characterized by an uncontrolled proliferation of the myeloid lineage and their precursors (MYELOID PROGENITOR CELLS) in the bone marrow and other sites.		04.6211
Myelodysplastic Syndromes
Clonal hematopoietic stem cell disorders characterized by dysplasia in one or more hematopoietic cell lineages. They predominantly affect patients over 60, are considered preleukemic conditions, and have high probability of transformation into ACUTE MYELOID LEUKEMIA.		04.6211
Precursor Cell Lymphoblastic Leukemia-Lymphoma
A neoplasm characterized by abnormalities of the lymphoid cell precursors leading to excessive lymphoblasts in the marrow and other organs. It is the most common cancer in children and accounts for the vast majority of all childhood leukemias.		04.6211
Adenocarcinoma, Basal Cell
[description not available]		02.5920
Metastase
[description not available]		02.5920
Colorectal Cancer
[description not available]		02.5920
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		02.5920
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		02.5920
Colorectal Neoplasms
Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.		02.5920
Anasarca
[description not available]		06.451
Plica Syndrome
[description not available]		02.3110
Edema
Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.		06.451
Synovitis
Inflammation of the SYNOVIAL MEMBRANE.		02.3110
Antibody Deficiency Syndrome
[description not available]		02.3110
Immunologic Deficiency Syndromes
Syndromes in which there is a deficiency or defect in the mechanisms of immunity, either cellular or humoral.		02.3110
Cystic Fibrosis of Pancreas
[description not available]		05.3131
Cystic Fibrosis
An autosomal recessive genetic disease of the EXOCRINE GLANDS. It is caused by mutations in the gene encoding the CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR expressed in several organs including the LUNG, the PANCREAS, the BILIARY SYSTEM, and the SWEAT GLANDS. Cystic fibrosis is characterized by epithelial secretory dysfunction associated with ductal obstruction resulting in AIRWAY OBSTRUCTION; chronic RESPIRATORY INFECTIONS; PANCREATIC INSUFFICIENCY; maldigestion; salt depletion; and HEAT PROSTRATION.		05.3131
Palmoplantaris Pustulosis
[description not available]		07.5772
Psoriasis
A common genetically determined, chronic, inflammatory skin disease characterized by rounded erythematous, dry, scaling patches. The lesions have a predilection for nails, scalp, genitalia, extensor surfaces, and the lumbosacral region. Accelerated epidermopoiesis is considered to be the fundamental pathologic feature in psoriasis.		07.5772
Muscular Weakness
[description not available]		02.3110
Muscle Disorders
[description not available]		02.3110
Symptom Cluster
[description not available]		02.3110
Muscular Diseases
Acquired, familial, and congenital disorders of SKELETAL MUSCLE and SMOOTH MUSCLE.		02.3110
Syndrome
A characteristic symptom complex.		02.3110
Muscle Weakness
A vague complaint of debility, fatigue, or exhaustion attributable to weakness of various muscles. The weakness can be characterized as subacute or chronic, often progressive, and is a manifestation of many muscle and neuromuscular diseases. (From Wyngaarden et al., Cecil Textbook of Medicine, 19th ed, p2251)		02.3110
Adenocarcinoma Of Kidney
[description not available]		02.6320
Cancer of Kidney
[description not available]		02.6320
Carcinoma, Renal Cell
A heterogeneous group of sporadic or hereditary carcinoma derived from cells of the KIDNEYS. There are several subtypes including the clear cells, the papillary, the chromophobe, the collecting duct, the spindle cells (sarcomatoid), or mixed cell-type carcinoma.		02.6320
Kidney Neoplasms
Tumors or cancers of the KIDNEY.		02.6320
Aura
[description not available]		02.6320
Epilepsy
A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)		02.6320
Short Bowel Syndrome
A malabsorption syndrome resulting from extensive operative resection of the SMALL INTESTINE, the absorptive region of the GASTROINTESTINAL TRACT.		02.3110
Systolic Heart Failure
[description not available]		03.711
Heart Failure, Systolic
Heart failure caused by abnormal myocardial contraction during SYSTOLE leading to defective cardiac emptying.		03.711
Arrhythmia
[description not available]		02.8630
Cardiac Arrest, Sudden
[description not available]		02.4110
Arrhythmias, Cardiac
Any disturbances of the normal rhythmic beating of the heart or MYOCARDIAL CONTRACTION. Cardiac arrhythmias can be classified by the abnormalities in HEART RATE, disorders of electrical impulse generation, or impulse conduction.		02.8630
Death, Sudden, Cardiac
Unexpected rapid natural death due to cardiovascular collapse within one hour of initial symptoms. It is usually caused by the worsening of existing heart diseases. The sudden onset of symptoms, such as CHEST PAIN and CARDIAC ARRHYTHMIAS, particularly VENTRICULAR TACHYCARDIA, can lead to the loss of consciousness and cardiac arrest followed by biological death. (from Braunwald's Heart Disease: A Textbook of Cardiovascular Medicine, 7th ed., 2005)		02.4110
Overweight
A status with BODY WEIGHT that is above certain standards. In the scale of BODY MASS INDEX, overweight is defined as having a BMI of 25.0-29.9 kg/m2. Overweight may or may not be due to increases in body fat (ADIPOSE TISSUE), hence overweight does not equal over fat.		09.66106
Abdominal Aortic Aneurysm
[description not available]		03.5120
Aortic Aneurysm, Abdominal
An abnormal balloon- or sac-like dilatation in the wall of the ABDOMINAL AORTA which gives rise to the visceral, the parietal, and the terminal (iliac) branches below the aortic hiatus at the diaphragm.		03.5120
Pancreatic Insufficiency
[description not available]		04.6211
Exocrine Pancreatic Insufficiency
A malabsorption condition resulting from greater than 10% reduction in the secretion of pancreatic digestive enzymes (LIPASE; PROTEASES; and AMYLASE) by the EXOCRINE PANCREAS into the DUODENUM. This condition is often associated with CYSTIC FIBROSIS and with chronic PANCREATITIS.		04.6211
Cruveilhier-Baumgarten Syndrome
Liver cirrhosis with intrahepatic portal obstruction, HYPERTENSION, and patent UMBILICAL VEINS.		02.3110
Hypertension, Portal
Abnormal increase of resistance to blood flow within the hepatic PORTAL SYSTEM, frequently seen in LIVER CIRRHOSIS and conditions with obstruction of the PORTAL VEIN.		02.3110
Acute Liver Injury, Drug-Induced
[description not available]		04.6451
Cirrhoses, Experimental Liver
[description not available]		02.5720
Chemical and Drug Induced Liver Injury
A spectrum of clinical liver diseases ranging from mild biochemical abnormalities to ACUTE LIVER FAILURE, caused by drugs, drug metabolites, herbal and dietary supplements and chemicals from the environment.		04.6451
Acromegaly Due To Pituitary Adenoma
[description not available]		02.1510
Adenoma, Basal Cell
[description not available]		03.7130
Acidosis, Diabetic
[description not available]		04.8521
Adenoma
A benign epithelial tumor with a glandular organization.		03.7130
Diabetic Ketoacidosis
A life-threatening complication of diabetes mellitus, primarily of TYPE 1 DIABETES MELLITUS with severe INSULIN deficiency and extreme HYPERGLYCEMIA. It is characterized by KETOSIS; DEHYDRATION; and depressed consciousness leading to COMA.		04.8521
Convulsions, Febrile
[description not available]		02.8330
Seizures, Febrile
Seizures that occur during a febrile episode. It is a common condition, affecting 2-5% of children aged 3 months to five years. An autosomal dominant pattern of inheritance has been identified in some families. The majority are simple febrile seizures (generally defined as generalized onset, single seizures with a duration of less than 30 minutes). Complex febrile seizures are characterized by focal onset, duration greater than 30 minutes, and/or more than one seizure in a 24 hour period. The likelihood of developing epilepsy (i.e., a nonfebrile seizure disorder) following simple febrile seizures is low. Complex febrile seizures are associated with a moderately increased incidence of epilepsy. (From Menkes, Textbook of Child Neurology, 5th ed, p784)		02.8330
Diabetic Cardiomyopathies
Diabetes complications in which VENTRICULAR REMODELING in the absence of CORONARY ATHEROSCLEROSIS and hypertension results in cardiac dysfunctions, typically LEFT VENTRICULAR DYSFUNCTION. The changes also result in myocardial hypertrophy, myocardial necrosis and fibrosis, and collagen deposition due to impaired glucose tolerance.		07.54103
Autoimmune Disease
[description not available]		02.5220
Autoimmune Diseases
Disorders that are characterized by the production of antibodies that react with host tissues or immune effector cells that are autoreactive to endogenous peptides.		02.5220
Familial Nonmedullary Thyroid Cancer
[description not available]		02.1510
Carcinoma, Anaplastic
[description not available]		03.0540
Carcinoma, Papillary
A malignant neoplasm characterized by the formation of numerous, irregular, finger-like projections of fibrous stroma that is covered with a surface layer of neoplastic epithelial cells. (Stedman, 25th ed)		02.1510
Cancer of the Thyroid
[description not available]		03.1950
Carcinoma
A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for cancer.		03.0540
Thyroid Neoplasms
Tumors or cancer of the THYROID GLAND.		03.1950
Cardiac Remodeling, Ventricular
[description not available]		06.2871
Acute Kidney Failure
[description not available]		03.4770
Rhabdomyolysis
Necrosis or disintegration of skeletal muscle often followed by myoglobinuria.		03.1650
Acute Kidney Injury
Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions.		03.4770
Colonic Inertia
Symptom characterized by the passage of stool once a week or less.		04.4811
Constipation
Infrequent or difficult evacuation of FECES. These symptoms are associated with a variety of causes, including low DIETARY FIBER intake, emotional or nervous disturbances, systemic and structural disorders, drug-induced aggravation, and infections.		04.4811
Nausea
An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.		014.223230
Ischemia
A hypoperfusion of the BLOOD through an organ or tissue caused by a PATHOLOGIC CONSTRICTION or obstruction of its BLOOD VESSELS, or an absence of BLOOD CIRCULATION.		03.0340
Cardiomyopathies, Primary
[description not available]		03.0240
Cardiomyopathies
A group of diseases in which the dominant feature is the involvement of the CARDIAC MUSCLE itself. Cardiomyopathies are classified according to their predominant pathophysiological features (DILATED CARDIOMYOPATHY; HYPERTROPHIC CARDIOMYOPATHY; RESTRICTIVE CARDIOMYOPATHY) or their etiological/pathological factors (CARDIOMYOPATHY, ALCOHOLIC; ENDOCARDIAL FIBROELASTOSIS).		03.0240
Hepatocellular Carcinoma
[description not available]		03.0840
Cancer of Liver
[description not available]		03.2550
Carcinoma, Hepatocellular
A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.		03.0840
Liver Neoplasms
Tumors or cancer of the LIVER.		03.2550
Pemphigus Foliaceus
[description not available]		02.5920
Pemphigus
Group of chronic blistering diseases characterized histologically by ACANTHOLYSIS and blister formation within the EPIDERMIS.		02.5920
Experimental Neoplasms
[description not available]		02.8530
Abnormalities, Autosome
[description not available]		02.5220
Atheroma
[description not available]		05.3643
Arterial Diseases, Carotid
[description not available]		05.5453
Carotid Artery Diseases
Pathological conditions involving the CAROTID ARTERIES, including the common, internal, and external carotid arteries. ATHEROSCLEROSIS and TRAUMA are relatively frequent causes of carotid artery pathology.		05.5453
Diabetic Angiopathies
VASCULAR DISEASES that are associated with DIABETES MELLITUS.		010.29147
Diabetes Mellitus, Gestational
[description not available]		04.5122
Diabetes, Gestational
Diabetes mellitus induced by PREGNANCY but resolved at the end of pregnancy. It does not include previously diagnosed diabetics who become pregnant (PREGNANCY IN DIABETICS). Gestational diabetes usually develops in late pregnancy when insulin antagonistic hormones peaks leading to INSULIN RESISTANCE; GLUCOSE INTOLERANCE; and HYPERGLYCEMIA.		04.5122
Emesis
[description not available]		013.72725
Colicky Pain
[description not available]		04.8221
Vomiting
The forcible expulsion of the contents of the STOMACH through the MOUTH.		013.72725
Abdominal Pain
Sensation of discomfort, distress, or agony in the abdominal region.		04.8221
Aging
The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.		06.7942
Central Retinal Edema, Cystoid
[description not available]		04.3720
Macular Edema
Fluid accumulation in the outer layer of the MACULA LUTEA that results from intraocular or systemic insults. It may develop in a diffuse pattern where the macula appears thickened or it may acquire the characteristic petaloid appearance referred to as cystoid macular edema. Although macular edema may be associated with various underlying conditions, it is most commonly seen following intraocular surgery, venous occlusive disease, DIABETIC RETINOPATHY, and posterior segment inflammatory disease. (From Survey of Ophthalmology 2004; 49(5) 470-90)		04.3720
Active Hyperemia
[description not available]		02.1710
Hyperemia
The presence of an increased amount of blood in a body part or an organ leading to congestion or engorgement of blood vessels. Hyperemia can be due to increase of blood flow into the area (active or arterial), or due to obstruction of outflow of blood from the area (passive or venous).		02.1710
Autosomal Dominant Juvenile Parkinson Disease
[description not available]		02.5920
Age-Related Memory Disorders
[description not available]		03.0340
Memory Disorders
Disturbances in registering an impression, in the retention of an acquired impression, or in the recall of an impression. Memory impairments are associated with DEMENTIA; CRANIOCEREBRAL TRAUMA; ENCEPHALITIS; ALCOHOLISM (see also ALCOHOL AMNESTIC DISORDER); SCHIZOPHRENIA; and other conditions.		03.0340
Parkinsonian Disorders
A group of disorders which feature impaired motor control characterized by bradykinesia, MUSCLE RIGIDITY; TREMOR; and postural instability. Parkinsonian diseases are generally divided into primary parkinsonism (see PARKINSON DISEASE), secondary parkinsonism (see PARKINSON DISEASE, SECONDARY) and inherited forms. These conditions are associated with dysfunction of dopaminergic or closely related motor integration neuronal pathways in the BASAL GANGLIA.		02.5920
Pulmonary Arterial Remodeling
[description not available]		02.1710
Pulmonary Hypertension
[description not available]		02.5920
Hypertension, Pulmonary
Increased VASCULAR RESISTANCE in the PULMONARY CIRCULATION, usually secondary to HEART DISEASES or LUNG DISEASES.		02.5920
Aggression
Behavior which may be manifested by destructive and attacking action which is verbal or physical, by covert attitudes of hostility or by obstructionism.		02.5420
Anxiety
Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.		02.8330
Injuries
Used with anatomic headings, animals, and sports for wounds and injuries. Excludes cell damage, for which pathology is used.		02.1710
Wounds and Injuries
Damage inflicted on the body as the direct or indirect result of an external force, with or without disruption of structural continuity.		02.1710
Acute Respiratory Distress Syndrome
[description not available]		03.0910
Respiratory Distress Syndrome
A syndrome characterized by progressive life-threatening RESPIRATORY INSUFFICIENCY in the absence of known LUNG DISEASES, usually following a systemic insult such as surgery or major TRAUMA.		03.0910
Intestinal Diseases
Pathological processes in any segment of the INTESTINE from DUODENUM to RECTUM.		02.1710
Pancreatic Diseases
Pathological processes of the PANCREAS.		02.2110
Androgen-Independent Prostatic Cancer
[description not available]		02.1710
Local Neoplasm Recurrence
[description not available]		02.1710
Prostatic Neoplasms, Castration-Resistant
Tumors or cancer of the PROSTATE which can grow in the presence of low or residual amount of androgen hormones such as TESTOSTERONE.		02.1710
Encephalopathy, Toxic
[description not available]		02.2110
Angiogenesis, Pathologic
[description not available]		02.2110
HIV Coinfection
[description not available]		06.8233
HIV
Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.		04.5111
HIV Infections
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).		06.8233
Dyskinesia, Medication-Induced
[description not available]		02.2110
Dyskinesia, Drug-Induced
Abnormal movements, including HYPERKINESIS; HYPOKINESIA; TREMOR; and DYSTONIA, associated with the use of certain medications or drugs. Muscles of the face, trunk, neck, and extremities are most commonly affected. Tardive dyskinesia refers to abnormal hyperkinetic movements of the muscles of the face, tongue, and neck associated with the use of neuroleptic agents (see ANTIPSYCHOTIC AGENTS). (Adams et al., Principles of Neurology, 6th ed, p1199)		02.2110
Affective Disorders
[description not available]		02.1310
Mood Disorders
Those disorders that have a disturbance in mood as their predominant feature.		02.1310
Dermatitis Medicamentosa
[description not available]		05.871
Absence Status
[description not available]		02.2110
Status Epilepticus
A prolonged seizure or seizures repeated frequently enough to prevent recovery between episodes occurring over a period of 20-30 minutes. The most common subtype is generalized tonic-clonic status epilepticus, a potentially fatal condition associated with neuronal injury and respiratory and metabolic dysfunction. Nonconvulsive forms include petit mal status and complex partial status, which may manifest as behavioral disturbances. Simple partial status epilepticus consists of persistent motor, sensory, or autonomic seizures that do not impair cognition (see also EPILEPSIA PARTIALIS CONTINUA). Subclinical status epilepticus generally refers to seizures occurring in an unresponsive or comatose individual in the absence of overt signs of seizure activity. (From N Engl J Med 1998 Apr 2;338(14):970-6; Neurologia 1997 Dec;12 Suppl 6:25-30)		02.2110
Hospital-Acquired Condition
[description not available]		02.5420
Coagulation, Disseminated Intravascular
[description not available]		02.2110
Disseminated Intravascular Coagulation
A disorder characterized by procoagulant substances entering the general circulation causing a systemic thrombotic process. The activation of the clotting mechanism may arise from any of a number of disorders. A majority of the patients manifest skin lesions, sometimes leading to PURPURA FULMINANS.		02.2110
Actinic Reticuloid Syndrome
[description not available]		02.5220
Morbid Obesity
[description not available]		03.5911
Obesity, Morbid
The condition of weighing two, three, or more times the ideal weight, so called because it is associated with many serious and life-threatening disorders. In the BODY MASS INDEX, morbid obesity is defined as having a BMI greater than 40.0 kg/m2.		03.5911
Nerve Degeneration
Loss of functional activity and trophic degeneration of nerve axons and their terminal arborizations following the destruction of their cells of origin or interruption of their continuity with these cells. The pathology is characteristic of neurodegenerative diseases. Often the process of nerve degeneration is studied in research on neuroanatomical localization and correlation of the neurophysiology of neural pathways.		02.2110
Abnormalities, Cardiovascular
[description not available]		03.1210
Cardiovascular Abnormalities
Congenital, inherited, or acquired anomalies of the CARDIOVASCULAR SYSTEM, including the HEART and BLOOD VESSELS.		03.1210
Nervous System Disorders
[description not available]		02.2110
Nervous System Diseases
Diseases of the central and peripheral nervous system. This includes disorders of the brain, spinal cord, cranial nerves, peripheral nerves, nerve roots, autonomic nervous system, neuromuscular junction, and muscle.		02.2110
Sclerosis, Systemic
[description not available]		03.1710
Scleroderma, Systemic
A chronic multi-system disorder of CONNECTIVE TISSUE. It is characterized by SCLEROSIS in the SKIN, the LUNGS, the HEART, the GASTROINTESTINAL TRACT, the KIDNEYS, and the MUSCULOSKELETAL SYSTEM. Other important features include diseased small BLOOD VESSELS and AUTOANTIBODIES. The disorder is named for its most prominent feature (hard skin), and classified into subsets by the extent of skin thickening: LIMITED SCLERODERMA and DIFFUSE SCLERODERMA.		03.1710
Polyarthritis
[description not available]		03.730
Arthritis
Acute or chronic inflammation of JOINTS.		03.730
Psychoses
[description not available]		02.0810
Psychotic Disorders
Disorders in which there is a loss of ego boundaries or a gross impairment in reality testing with delusions or prominent hallucinations. (From DSM-IV, 1994)		02.0810
Hyperplasia
An increase in the number of cells in a tissue or organ without tumor formation. It differs from HYPERTROPHY, which is an increase in bulk without an increase in the number of cells.		03.420
Neuroendocrine Tumors
Tumors whose cells possess secretory granules and originate from the neuroectoderm, i.e., the cells of the ectoblast or epiblast that program the neuroendocrine system. Common properties across most neuroendocrine tumors include ectopic hormone production (often via APUD CELLS), the presence of tumor-associated antigens, and isozyme composition.		03.4220
Acute Coronary Syndrome
An episode of MYOCARDIAL ISCHEMIA that generally lasts longer than a transient anginal episode that ultimately may lead to MYOCARDIAL INFARCTION.		05.9364
Hypermelanosis
[description not available]		02.0810
Nelson Syndrome
A syndrome characterized by HYPERPIGMENTATION, enlarging pituitary mass, visual defects secondary to compression of the OPTIC CHIASM, and elevated serum ACTH. It is caused by the expansion of an underlying ACTH-SECRETING PITUITARY ADENOMA that grows in the absence of feedback inhibition by adrenal CORTICOSTEROIDS, usually after ADRENALECTOMY.		02.0810
Central Nervous System Cysts
Congenital or acquired cysts of the brain, spinal cord, or meninges which may remain stable in size or undergo progressive enlargement.		02.0810
Hyperpigmentation
Excessive pigmentation of the skin, usually as a result of increased epidermal or dermal melanin pigmentation, hypermelanosis. Hyperpigmentation can be localized or generalized. The condition may arise from exposure to light, chemicals or other substances, or from a primary metabolic imbalance.		02.0810
Carcinogenesis
The origin, production or development of cancer through genotypic and phenotypic changes which upset the normal balance between cell proliferation and cell death. Carcinogenesis generally requires a constellation of steps, which may occur quickly or over a period of many years.		02.5120
Cancer of Colon
[description not available]		02.4820
Colonic Neoplasms
Tumors or cancer of the COLON.		02.4820
Chronic Kidney Failure
[description not available]		07.2883
Kidney Failure, Chronic
The end-stage of CHRONIC RENAL INSUFFICIENCY. It is characterized by the severe irreversible kidney damage (as measured by the level of PROTEINURIA) and the reduction in GLOMERULAR FILTRATION RATE to less than 15 ml per min (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002). These patients generally require HEMODIALYSIS or KIDNEY TRANSPLANTATION.		07.2883
Amyloid Deposits
[description not available]		02.0810
Chromosome-Defective Micronuclei
[description not available]		02.0810
Adult Premature Aging Syndrome
[description not available]		02.4820
Edema, Pulmonary
[description not available]		02.0810
Pulmonary Edema
Excessive accumulation of extravascular fluid in the lung, an indication of a serious underlying disease or disorder. Pulmonary edema prevents efficient PULMONARY GAS EXCHANGE in the PULMONARY ALVEOLI, and can be life-threatening.		02.0810
Urinary Tract Infections
Inflammatory responses of the epithelium of the URINARY TRACT to microbial invasions. They are often bacterial infections with associated BACTERIURIA and PYURIA.		011.791919
ANS (Autonomic Nervous System) Diseases
[description not available]		03.9210
Hypertension, Renal
Persistent high BLOOD PRESSURE due to KIDNEY DISEASES, such as those involving the renal parenchyma, the renal vasculature, or tumors that secrete RENIN.		02.4620
Nephritis
Inflammation of any part of the KIDNEY.		02.0810
Cardiac Hypertrophy
Enlargement of the HEART due to chamber HYPERTROPHY, an increase in wall thickness without an increase in the number of cells (MYOCYTES, CARDIAC). It is the result of increase in myocyte size, mitochondrial and myofibrillar mass, as well as changes in extracellular matrix.		02.0810
Cardiomegaly
Enlargement of the HEART, usually indicated by a cardiothoracic ratio above 0.50. Heart enlargement may involve the right, the left, or both HEART VENTRICLES or HEART ATRIA. Cardiomegaly is a nonspecific symptom seen in patients with chronic systolic heart failure (HEART FAILURE) or several forms of CARDIOMYOPATHIES.		02.0810
Weight Gain
Increase in BODY WEIGHT over existing weight.		010.56105
Tendinitis
Inflammation of TENDONS. It is characterized by the degeneration of tendons accompanied by an inflammatory repair response, fibroblastic proliferation, and formation of granulation tissue. Tendinitis is not a clinical diagnosis and can be confirmed only by histopathological findings.		02.110
Tendinopathy
Clinical syndrome describing overuse tendon injuries characterized by a combination of PAIN, diffuse or localized swelling, and impaired performance.		02.110
Candida Infection
[description not available]		03.4811
Female Genital Diseases
[description not available]		05.3722
Genital Diseases, Male
Pathological processes involving the male reproductive tract (GENITALIA, MALE).		05.3722
Candidiasis
Infection with a fungus of the genus CANDIDA. It is usually a superficial infection of the moist areas of the body and is generally caused by CANDIDA ALBICANS. (Dorland, 27th ed)		03.4811
Genital Diseases, Female
Pathological processes involving the female reproductive tract (GENITALIA, FEMALE).		05.3722
Atrophy
Decrease in the size of a cell, tissue, organ, or multiple organs, associated with a variety of pathological conditions such as abnormal cellular changes, ischemia, malnutrition, or hormonal changes.		02.110
Low Bone Density
[description not available]		03.511
Bone Loss, Perimenopausal
[description not available]		03.511
Bone Diseases, Metabolic
Diseases that affect the METABOLIC PROCESSES of BONE TISSUE.		03.511
Osteoporosis, Postmenopausal
Metabolic disorder associated with fractures of the femoral neck, vertebrae, and distal forearm. It occurs commonly in women within 15-20 years after menopause, and is caused by factors associated with menopause including estrogen deficiency.		03.511
Amino Acid Metabolism Disorders, Inborn
[description not available]		02.110
Delayed Hypersensitivity
[description not available]		03.0110
Bone Loss, Osteoclastic
[description not available]		02.4920
Psoriasis Arthropathica
[description not available]		02.110
Arthritis, Psoriatic
A type of inflammatory arthritis associated with PSORIASIS, often involving the axial joints and the peripheral terminal interphalangeal joints. It is characterized by the presence of HLA-B27-associated SPONDYLARTHROPATHY, and the absence of rheumatoid factor.		02.110
Arterial Obstructive Diseases
[description not available]		02.110
Arterial Occlusive Diseases
Pathological processes which result in the partial or complete obstruction of ARTERIES. They are characterized by greatly reduced or absence of blood flow through these vessels. They are also known as arterial insufficiency.		02.110
Cognitive Decline
[description not available]		02.1110
Cognitive Dysfunction
Diminished or impaired mental and/or intellectual function.		02.1110
Endotoxemia
A condition characterized by the presence of ENDOTOXINS in the blood. On lysis, the outer cell wall of gram-negative bacteria enters the systemic circulation and initiates a pathophysiologic cascade of pro-inflammatory mediators.		02.1110
Fungal Diseases
[description not available]		05.3922
Mycoses
Diseases caused by FUNGI.		05.3922
Colitis
Inflammation of the COLON section of the large intestine (INTESTINE, LARGE), usually with symptoms such as DIARRHEA (often with blood and mucus), ABDOMINAL PAIN, and FEVER.		02.1110
Hypertrophy
General increase in bulk of a part or organ due to CELL ENLARGEMENT and accumulation of FLUIDS AND SECRETIONS, not due to tumor formation, nor to an increase in the number of cells (HYPERPLASIA).		02.1110
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		05.8781
Pericementitis
[description not available]		02.1110
Alveolar Bone Atrophy
[description not available]		02.1110
Periodontitis
Inflammation and loss of connective tissues supporting or surrounding the teeth. This may involve any part of the PERIODONTIUM. Periodontitis is currently classified by disease progression (CHRONIC PERIODONTITIS; AGGRESSIVE PERIODONTITIS) instead of age of onset. (From 1999 International Workshop for a Classification of Periodontal Diseases and Conditions, American Academy of Periodontology)		02.1110
Coronary Heart Disease
[description not available]		02.1110
Coronary Disease
An imbalance between myocardial functional requirements and the capacity of the CORONARY VESSELS to supply sufficient blood flow. It is a form of MYOCARDIAL ISCHEMIA (insufficient blood supply to the heart muscle) caused by a decreased capacity of the coronary vessels.		02.1110
Cancer of Cervix
[description not available]		02.1110
Uterine Cervical Neoplasms
Tumors or cancer of the UTERINE CERVIX.		02.1110
Cell Transformation, Neoplastic
Cell changes manifested by escape from control mechanisms, increased growth potential, alterations in the cell surface, karyotypic abnormalities, morphological and biochemical deviations from the norm, and other attributes conferring the ability to invade, metastasize, and kill.		02.1110
Age-Related Osteoporosis
[description not available]		02.1110
Osteoporosis
Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis.		02.1110
Chronic Illness
[description not available]		03.7130
Airway Remodeling
The structural changes in the number, mass, size and/or composition of the airway tissues.		02.1110
Asthma, Bronchial
[description not available]		02.4920
Asthma
A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).		02.4920
Chronic Disease
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).		03.7130
Respiratory Tract Diseases
Diseases involving the RESPIRATORY SYSTEM.		02.1110
Carcinoma, Ductal, Pancreatic
[description not available]		02.1310
Carcinoma, Pancreatic Ductal
Carcinoma that arises from the PANCREATIC DUCTS. It accounts for the majority of cancers derived from the PANCREAS.		02.1310
Alcoholic Intoxication
An acute brain syndrome which results from the excessive ingestion of ETHANOL or ALCOHOLIC BEVERAGES.		02.1310
Osteoporotic Fractures
Breaks in bones resulting from low bone mass and microarchitectural deterioration characteristic of OSTEOPOROSIS.		03.9321
Day Blindness
[description not available]		03.0410
Anorexia
The lack or loss of APPETITE accompanied by an aversion to food and the inability to eat. It is the defining characteristic of the disorder ANOREXIA NERVOSA.		04.4311
Allergy, Drug
[description not available]		0340
Drug Hypersensitivity
Immunologically mediated adverse reactions to medicinal substances used legally or illegally.		0340
Arteriosclerosis
Thickening and loss of elasticity of the walls of ARTERIES of all sizes. There are many forms classified by the types of lesions and arteries involved, such as ATHEROSCLEROSIS with fatty lesions in the ARTERIAL INTIMA of medium and large muscular arteries.		02.520
Chronic Hepatitis C
[description not available]		03.8721
Hepatitis C, Chronic
INFLAMMATION of the LIVER in humans that is caused by HEPATITIS C VIRUS lasting six months or more. Chronic hepatitis C can lead to LIVER CIRRHOSIS.		03.8721
Hypovolemic
[description not available]		03.5111
Genital Tract Infections
[description not available]		03.5111
Hypovolemia
An abnormally low volume of blood circulating through the body. It may result in hypovolemic shock (see SHOCK).		03.5111
Indigestion
[description not available]		04.4511
Infection
[description not available]		04.8121
Dyspepsia
Impaired digestion, especially after eating.		04.4511
Infections
Invasion of the host organism by microorganisms or their toxins or by parasites that can cause pathological conditions or diseases.		04.8121
Cat Diseases
Diseases of the domestic cat (Felis catus or F. domesticus). This term does not include diseases of the so-called big cats such as CHEETAHS; LIONS; tigers, cougars, panthers, leopards, and other Felidae for which the heading CARNIVORA is used.		02.1310
Nerve Pain
[description not available]		02.1310
Neuralgia
Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.		02.1310
Genetic Predisposition
[description not available]		02.520
Interstitial Nephritis
[description not available]		02.1310
Nephritis, Interstitial
Inflammation of the interstitial tissue of the kidney. This term is generally used for primary inflammation of KIDNEY TUBULES and/or surrounding interstitium. For primary inflammation of glomerular interstitium, see GLOMERULONEPHRITIS. Infiltration of the inflammatory cells into the interstitial compartment results in EDEMA, increased spaces between the tubules, and tubular renal dysfunction.		02.1310
Chronic Pancreatitis
[description not available]		02.1310
Carcinoma, Intraepithelial
[description not available]		02.1310
Cystadenoma
A benign neoplasm derived from glandular epithelium, in which cystic accumulations of retained secretions are formed. In some instances, considerable portions of the neoplasm, or even the entire mass, may be cystic. (Stedman, 25th ed)		02.1310
Carcinoma in Situ
A lesion with cytological characteristics associated with invasive carcinoma but the tumor cells are confined to the epithelium of origin, without invasion of the basement membrane.		02.1310
Pancreatitis, Chronic
INFLAMMATION of the PANCREAS that is characterized by recurring or persistent ABDOMINAL PAIN with or without STEATORRHEA or DIABETES MELLITUS. It is characterized by the irregular destruction of the pancreatic parenchyma which may be focal, segmental, or diffuse.		02.1310
Compensatory Hyperinsulinemia
A GLUCOSE-induced HYPERINSULINEMIA, a marker of insulin-resistant state. It is a mechanism to compensate for reduced sensitivity to insulin.		04.1431
Hyperinsulinism
A syndrome with excessively high INSULIN levels in the BLOOD. It may cause HYPOGLYCEMIA. Etiology of hyperinsulinism varies, including hypersecretion of a beta cell tumor (INSULINOMA); autoantibodies against insulin (INSULIN ANTIBODIES); defective insulin receptor (INSULIN RESISTANCE); or overuse of exogenous insulin or HYPOGLYCEMIC AGENTS.		04.1431
Bone Fractures
[description not available]		03.5311
Intertrochanteric Fractures
[description not available]		03.5311
Hip Fractures
Fractures of the FEMUR HEAD; the FEMUR NECK; (FEMORAL NECK FRACTURES); the trochanters; or the inter- or subtrochanteric region. Excludes fractures of the acetabulum and fractures of the femoral shaft below the subtrochanteric region (FEMORAL FRACTURES).		03.5311
Fractures, Bone
Breaks in bones.		03.5311
Adenoma, beta-Cell
[description not available]		03.0610
Insulinoma
A benign tumor of the PANCREATIC BETA CELLS. Insulinoma secretes excess INSULIN resulting in HYPOGLYCEMIA.		03.0610
Cancer of Prostate
[description not available]		02.1510
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		02.1510
Alopecia Cicatrisata
[description not available]		02.1510
Alopecia
Absence of hair from areas where it is normally present.		02.1510
Lichen Ruber Planus
[description not available]		02.1510
Lichen Planus
An inflammatory, pruritic disease of the skin and mucous membranes, which can be either generalized or localized. It is characterized by distinctive purplish, flat-topped papules having a predilection for the trunk and flexor surfaces. The lesions may be discrete or coalesce to form plaques. Histologically, there is a saw-tooth pattern of epidermal hyperplasia and vacuolar alteration of the basal layer of the epidermis along with an intense upper dermal inflammatory infiltrate composed predominantly of T-cells. Etiology is unknown.		07.1510
Lactic Acidosis
[description not available]		02.1310
Acidosis, Lactic
Acidosis caused by accumulation of lactic acid more rapidly than it can be metabolized. It may occur spontaneously or in association with diseases such as DIABETES MELLITUS; LEUKEMIA; or LIVER FAILURE.		02.1310
Drug Overdose
Accidental or deliberate use of a medication or street drug in excess of normal dosage.		03.4220
Amentia
[description not available]		02.1310
Hypotension, Postural
[description not available]		02.1310
Dementia
An acquired organic mental disorder with loss of intellectual abilities of sufficient severity to interfere with social or occupational functioning. The dysfunction is multifaceted and involves memory, behavior, personality, judgment, attention, spatial relations, language, abstract thought, and other executive functions. The intellectual decline is usually progressive, and initially spares the level of consciousness.		02.1310
Hypotension, Orthostatic
A significant drop in BLOOD PRESSURE after assuming a standing position. Orthostatic hypotension is a finding, and defined as a 20-mm Hg decrease in systolic pressure or a 10-mm Hg decrease in diastolic pressure 3 minutes after the person has risen from supine to standing. Symptoms generally include DIZZINESS, blurred vision, and SYNCOPE.		02.1310
Erythrophagocytic Lymphohistiocytosis, Familial
[description not available]		02.1510
Lymphohistiocytosis, Hemophagocytic
A group of related disorders characterized by LYMPHOCYTOSIS; HISTIOCYTOSIS; and hemophagocytosis. The two major forms are familial and reactive.		02.1510
Cancer of Endometrium
[description not available]		02.1510
Endometrial Neoplasms
Tumors or cancer of ENDOMETRIUM, the mucous lining of the UTERUS. These neoplasms can be benign or malignant. Their classification and grading are based on the various cell types and the percent of undifferentiated cells.		02.1510
Acute Myelogenous Leukemia
[description not available]		02.0510
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		02.0510
Hepatitis B Virus Infection
[description not available]		02.9610
MS (Multiple Sclerosis)
[description not available]		02.9610
Hepatitis B
INFLAMMATION of the LIVER in humans caused by a member of the ORTHOHEPADNAVIRUS genus, HEPATITIS B VIRUS. It is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact.		02.9610
Multiple Sclerosis
An autoimmune disorder mainly affecting young adults and characterized by destruction of myelin in the central nervous system. Pathologic findings include multiple sharply demarcated areas of demyelination throughout the white matter of the central nervous system. Clinical manifestations include visual loss, extra-ocular movement disorders, paresthesias, loss of sensation, weakness, dysarthria, spasticity, ataxia, and bladder dysfunction. The usual pattern is one of recurrent attacks followed by partial recovery (see MULTIPLE SCLEROSIS, RELAPSING-REMITTING), but acute fulminating and chronic progressive forms (see MULTIPLE SCLEROSIS, CHRONIC PROGRESSIVE) also occur. (Adams et al., Principles of Neurology, 6th ed, p903)		02.9610
Smoking Cessation
Discontinuing the habit of SMOKING.		02.9610
Hepatic Insufficiency
Conditions in which the LIVER functions fall below the normal ranges. Severe hepatic insufficiency may cause LIVER FAILURE or DEATH. Treatment may include LIVER TRANSPLANTATION.		04.3511
Leukemia, Lymphoblastic, Acute, T Cell
[description not available]		02.0510
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
A leukemia/lymphoma found predominately in children and young adults and characterized LYMPHADENOPATHY and THYMUS GLAND involvement. It most frequently presents as a lymphoma, but a leukemic progression in the bone marrow is common.		02.0510
Hibernation, Myocardial
[description not available]		02.9710
Hyperlipemia
[description not available]		02.0510
Hyperlipidemias
Conditions with excess LIPIDS in the blood.		14.0510
Left Ventricular Hypertrophy
[description not available]		02.0510
Hypertrophy, Left Ventricular
Enlargement of the LEFT VENTRICLE of the heart. This increase in ventricular mass is attributed to sustained abnormal pressure or volume loads and is a contributor to cardiovascular morbidity and mortality.		02.0510
Leukocytopenia
[description not available]		02.0610
Leukopenia
A decrease in the number of LEUKOCYTES in a blood sample below the normal range (LEUKOCYTE COUNT less than 4000).		02.0610
Ache
[description not available]		03.4511
Erythema
Redness of the skin produced by congestion of the capillaries. This condition may result from a variety of disease processes.		03.4511
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		03.4511
Anaphylactic Reaction
[description not available]		02.0610
Allergic Reaction
[description not available]		02.0610
Anaphylaxis
An acute hypersensitivity reaction due to exposure to a previously encountered ANTIGEN. The reaction may include rapidly progressing URTICARIA, respiratory distress, vascular collapse, systemic SHOCK, and death.		02.0610
Hypersensitivity
Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen.		02.0610
Icterus
[description not available]		02.0610
Jaundice
A clinical manifestation of HYPERBILIRUBINEMIA, characterized by the yellowish staining of the SKIN; MUCOUS MEMBRANE; and SCLERA. Clinical jaundice usually is a sign of LIVER dysfunction.		02.0610
Carcinoma, Epidermoid
[description not available]		02.0710
Papilloma, Squamous Cell
[description not available]		02.0710
Cancer of Skin
[description not available]		02.0710
Carcinoma, Squamous Cell
A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)		02.0710
Papilloma
A circumscribed benign epithelial tumor projecting from the surrounding surface; more precisely, a benign epithelial neoplasm consisting of villous or arborescent outgrowths of fibrovascular stroma covered by neoplastic cells. (Stedman, 25th ed)		02.0710
Skin Neoplasms
Tumors or cancer of the SKIN.		02.0710
Itching
[description not available]		02.0710
Pruritus
An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.		02.0710
Uremia
A clinical syndrome associated with the retention of renal waste products or uremic toxins in the blood. It is usually the result of RENAL INSUFFICIENCY. Most uremic toxins are end products of protein or nitrogen CATABOLISM, such as UREA or CREATININE. Severe uremia can lead to multiple organ dysfunctions with a constellation of symptoms.		02.0610
Diathesis
[description not available]		02.0710
Bladder Cancer
[description not available]		02.0710
Urinary Bladder Neoplasms
Tumors or cancer of the URINARY BLADDER.		02.0710
Carcinoma, Medullary
A carcinoma composed mainly of epithelial elements with little or no stroma. Medullary carcinomas of the breast constitute 5%-7% of all mammary carcinomas; medullary carcinomas of the thyroid comprise 3%-10% of all thyroid malignancies. (From Dorland, 27th ed; DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, p1141; Segen, Dictionary of Modern Medicine, 1992)		02.0710
Depression, Endogenous
[description not available]		02.9910
Depressive Disorder
An affective disorder manifested by either a dysphoric mood or loss of interest or pleasure in usual activities. The mood disturbance is prominent and relatively persistent.		02.9910
Carotid Arteriopathies, Traumatic
[description not available]		02.0710
Coronary Restenosis
Recurrent narrowing or constriction of a coronary artery following surgical procedures performed to alleviate a prior obstruction.		02.0710
Bacteriuria
The presence of bacteria in the urine which is normally bacteria-free. These bacteria are from the URINARY TRACT and are not contaminants of the surrounding tissues. Bacteriuria can be symptomatic or asymptomatic. Significant bacteriuria is an indicator of urinary tract infection.		04.3711
Glycosuria
The appearance of an abnormally large amount of GLUCOSE in the urine, such as more than 500 mg/day in adults. It can be due to HYPERGLYCEMIA or genetic defects in renal reabsorption (RENAL GLYCOSURIA).		04.3711
Candidiasis, Genital
[description not available]		04.3711
Candidiasis, Vulvovaginal
Infection of the VULVA and VAGINA with a fungus of the genus CANDIDA.		04.3711
Aberrant Crypt Foci
Clusters of colonic crypts that appear different from the surrounding mucosa when visualized after staining. They are of interest as putative precursors to colorectal adenomas and potential biomarkers for colorectal carcinoma.		02.0710
Hypertriglyceridemia
A condition of elevated levels of TRIGLYCERIDES in the blood.		02.0710
Cardiomyopathy, Congestive
[description not available]		02.0710
Cardiomyopathy, Dilated
A form of CARDIAC MUSCLE disease that is characterized by ventricular dilation, VENTRICULAR DYSFUNCTION, and HEART FAILURE. Risk factors include SMOKING; ALCOHOL DRINKING; HYPERTENSION; INFECTION; PREGNANCY; and mutations in the LMNA gene encoding LAMIN TYPE A, a NUCLEAR LAMINA protein.		02.0710
Laryngeal Diseases
Pathological processes involving any part of the LARYNX which coordinates many functions such as voice production, breathing, swallowing, and coughing.		02.0710
Eosinophilia, Tropical
[description not available]		02.0710
Exanthem
[description not available]		02.0710
Eosinophilia
Abnormal increase of EOSINOPHILS in the blood, tissues or organs.		02.0710
Exanthema
Diseases in which skin eruptions or rashes are a prominent manifestation. Classically, six such diseases were described with similar rashes; they were numbered in the order in which they were reported. Only the fourth (Duke's disease), fifth (ERYTHEMA INFECTIOSUM), and sixth (EXANTHEMA SUBITUM) numeric designations survive as occasional synonyms in current terminology.		02.0710
AIDS Seroconversion
[description not available]		04.3911
Peripheral Arterial Diseases
[description not available]		02.4920
Peripheral Arterial Disease
Lack of perfusion in the EXTREMITIES resulting from atherosclerosis. It is characterized by INTERMITTENT CLAUDICATION, and an ANKLE BRACHIAL INDEX of 0.9 or less.		02.4920
Catarrh
Inflammation of a mucous membrane with increased flow of mucous in humans or animals. Catarrh is used mostly in a historical context.		04.3211
Eye Disorders
[description not available]		04.3211
Bilateral Headache
[description not available]		04.3211
Common Cold
A catarrhal disorder of the upper respiratory tract, which may be viral or a mixed infection. It generally involves a runny nose, nasal congestion, and sneezing.		04.3211
Eye Diseases
Diseases affecting the eye.		04.3211
Headache
The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS.		04.3211
Diseases, Peripheral Vascular
[description not available]		02.0310
Peripheral Vascular Diseases
Pathological processes involving any one of the BLOOD VESSELS in the vasculature outside the HEART.		02.0310
Age-Related Macular Degeneration
[description not available]		02.0410
Macular Degeneration
Degenerative changes in the RETINA usually of older adults which results in a loss of vision in the center of the visual field (the MACULA LUTEA) because of damage to the retina. It occurs in dry and wet forms.		02.0410