alogliptin: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
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. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 11450633 |
| CHEMBL ID | 376359 |
| CHEBI ID | 72323 |
| SCHEMBL ID | 121028 |
| MeSH ID | M0511100 |
| Synonym |
|---|
| 850649-61-5 |
| 2-({6-[(3r)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2h)-yl}methyl)benzonitrile |
| alogliptin |
| 2-({6-[(3r)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl}methyl)benzonitrile |
| bdbm16285 |
| CHEMBL376359 |
| chebi:72323 , |
| alogliptina |
| alogliptinum |
| alogliptine |
| syr322 |
| alogliptin [inn] |
| hsdb 8203 |
| jhc049lo86 , |
| 2-((6-((3r)-3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2h)-yl)methyl) benzonitrile |
| unii-jhc049lo86 |
| alogliptin [mi] |
| alogliptin [vandf] |
| alogliptin [who-dd] |
| S2868 |
| S5365 |
| gtpl6319 |
| vipidia |
| DB06203 |
| CS-1617 |
| HY-A0023A |
| SCHEMBL121028 |
| (r)-2-((6-(3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2h)-yl)methyl)benzonitrile |
| 2-{6-[3(r)-amino-piperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydro-2h-pyrimidin-1-ylmethyl}-benzonitrile |
| ZSBOMTDTBDDKMP-OAHLLOKOSA-N |
| DTXSID90234130 , |
| AKOS025149226 |
| AC-26300 |
| 2-[[6-[(3r)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile |
| mfcd09833196 |
| SW219186-1 |
| Q4734170 |
| alogliptin pound syr-322 pound(c) |
| AS-19582 |
| AMY22119 |
| BRD-K83003151-057-02-4 |
| CCG-267915 |
| CCG-267914 |
| NCGC00386215-05 |
| EX-A5446 |
| 2-[[6-[(3r)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2h)-pyrimidinyl]methyl]benzonitrile; (r)-2-[6-[3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-ylmethyl]benzonitrile; 2-[[6-[(3r)-3-amino-1-piperidinyl]-3,4-dihydr |
| 1347001-80-2 |
| dtxcid90156621 |
| benzonitrile, 2-((6-((3r)-3-amino-1-piperidinyl)-3,4-dihydro-3-methyl-2,4-dioxo-1(2h)-pyrimidinyl)methyl)- |
| 2-((6-((3r)-3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2h)-yl)methyl)benzonitrile |
| a10bh04 |
| alogliptin tartrate |
| EN300-6482025 |
Alogliptin (ALG) is a FDA-approved oral anti-hyperglycemic drug. It inhibits dipeptidyl peptidase-4. The drug may have effective anticancer properties against many types of malignancies.
Alogliptin has a low risk of hypoglycemia, and serious adverse events are uncommon. It has a moderate degree of absorption, estimated to exceed 75%.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Alogliptin has a moderate degree of absorption, estimated to exceed 75%, and its absorption is not affected by food." | ( Alogliptin: A new dipeptidyl peptidase-4 inhibitor for the management of type 2 diabetes mellitus. Erowele, G; Ndefo, UA; Okoli, O, 2014) | 2.57 |
| "Alogliptin has a low risk of hypoglycemia, and serious adverse events are uncommon." | ( Pioglitazone and alogliptin combination therapy in type 2 diabetes: a pathophysiologically sound treatment. Cersosimo, E; DeFronzo, RA; Triplitt, C, 2010) | 1.42 |
| "Alogliptin has been developed by Takeda under the brand name "Nesina"." | ( Novel serine protease dipeptidyl peptidase IV inhibitor: alogliptin. Agrawal, R; Bahare, RS; Dikshit, SN; Ganguly, S; Jain, P, 2012) | 1.35 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Alogliptin did not increase the risk of either first or recurrent CV events when compared with placebo in patients with T2DM and recent acute coronary syndrome." | ( Total cardiovascular events analysis of the EXAMINE trial in patients with type 2 diabetes and recent acute coronary syndrome. Bergenstal, RM; Cannon, CP; Cavender, MA; Cushman, WC; Heller, S; Liu, Y; Massaro, JM; Mehta, CR; White, WB; Zannad, F, 2018) | 1.2 |
Alogliptin treatment alleviated LPS-induced cognitive impairment as assessed by Morris water maze and novel object recognition tests. Treatment recovered the reduction in occludin and ZO-1 induced by OGD/R.
Alogliptin alone or in combination with other antidiabetic agents has shown a significant reduction in HbA1c while remaining safe and tolerable. The percentage of subjects who experienced all adverse events including hypoglycemia were comparable to those with placebo.
Study was conducted to evaluate the pharmacokinetic (PK) drug-drug interactions of alogliptin with pioglitazone or glyburide. To determine the rate of DPP-4 inhibition induced by these inhibitors, pharmacokinetics and pharmacodynamic parameters were used.
The aim of the study was to assess the efficacy and tolerability of alogliptin combined with pioglitazone in metformin-treated type 2 diabetic patients.
Alogliptin is a selective, orally bioavailable inhibitor of dipeptidyl peptidase-4 (DPP-4) It is used in the management of type 2 diabetes mellitus.
Alogliptin does not require any dosage adjustment when coadministered with ketoconazole, fluconazole,. gemfibrozil, warfarin, metformin, glyburide, and pioglitazone. The objective of this model-based meta-analysis was to describe the time course of HbA1c response after dosing with alogliptins.
| Role | Description |
|---|---|
| EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor | An EC 3.4.14.* (dipeptidyl- and tripeptidyl-peptidases) inhibitor that specifically inhibits dipeptidyl peptidase-4 (EC 3.4.14.5). |
| hypoglycemic agent | A drug which lowers the blood glucose level. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| nitrile | A compound having the structure RC#N; thus a C-substituted derivative of hydrocyanic acid, HC#N. In systematic nomenclature, the suffix nitrile denotes the triply bound #N atom, not the carbon atom attached to it. |
| piperidines | |
| pyrimidines | Any compound having a pyrimidine as part of its structure. |
| primary amino compound | A compound formally derived from ammonia by replacing one hydrogen atom by an organyl group. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 1.7740 | 10.0000 | AID566681 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 46.6667 | 0.0001 | 1.7536 | 10.0000 | AID1305313; AID566685; AID771378 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 (µMol) | 55.0000 | 0.0000 | 2.0151 | 10.0000 | AID1305313; AID566684 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 2.8005 | 10.0000 | AID566682 |
| Dipeptidyl peptidase 4 | Homo sapiens (human) | IC50 (µMol) | 5.2694 | 0.0001 | 0.4444 | 10.0000 | AID1189029; AID1305311; AID1373610; AID1444855; AID1570155; AID1614273; AID1631905; AID1706156; AID1781443; AID1797489; AID1801383; AID1917944; AID429379; AID566627; AID567004; AID659746; AID749996; AID771382 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 2.3983 | 10.0000 | AID566683 |
| Prolyl endopeptidase FAP | Homo sapiens (human) | IC50 (µMol) | 556.6667 | 0.0120 | 1.1589 | 5.8300 | AID1305312; AID1663821; AID688691 |
| Dipeptidyl peptidase 8 | Homo sapiens (human) | IC50 (µMol) | 66.6758 | 0.0019 | 2.6532 | 10.0000 | AID1189030; AID1305314; AID1570156; AID1614274; AID1706157; AID1781442; AID1797489; AID566628; AID567005; AID659747; AID688693 |
| Dipeptidyl peptidase 9 | Homo sapiens (human) | IC50 (µMol) | 66.6778 | 0.0001 | 1.4207 | 10.0000 | AID1189031; AID1305315; AID1570157; AID1614275; AID1706159; AID1781440; AID567006; AID659748; AID688690 |
| Dipeptidyl peptidase 2 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0002 | 0.9316 | 6.6000 | AID1305313; AID688688 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Dipeptidyl peptidase 4 | Homo sapiens (human) | Kd | 0.0155 | 0.0000 | 0.0080 | 0.0285 | AID1631907; AID1631913 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | Activity | 30.0000 | 0.0110 | 4.7055 | 9.4000 | AID567007 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1781445 | Inhibition of human recombinant DPP4 at 200 nM using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by fluorescence based microplate reader assay relative to control | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Identification and structure-activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
| AID1570178 | Anti-diabetic activity in 8 hrs-fasted C57BL/6 db/db mouse assessed as reduction in blood glucose AUC (0 to 120 mins) at 10 mg/kg, po pretreated for 60 mins followed by glucose challenge and measured after 120 mins post glucose challenge by OGTT relative | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study. |
| AID1614271 | Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells at 200 nM using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay relative to control | 2019 | Bioorganic & medicinal chemistry, 02-15, Volume: 27, Issue:4 | Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors. |
| AID1781444 | Inhibition of human recombinant DPP4 at 40 nM using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by fluorescence based microplate reader assay relative to control | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Identification and structure-activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
| AID567005 | Inhibition of DPP8 after 20 mins by fluorescence assay | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes. |
| AID688690 | Inhibition of DPP9 | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID1305312 | Inhibition of FAP (unknown origin) preincubated for 20 mins followed by Nle-Pro-AMC addition measured for 40 mins by continuous fluorescence assay | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1706184 | Anti-Hyperglycemic activity in high fat diet-fed/streptozotocin-induced type 2 diabetic mellitus C57BL/6 mouse model assessed as reduction in blood glucose level at 10 mg/kg/day for 14 days and measured on day 5 | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors. |
| AID771370 | In vivo inhibition of DPP-4 in ICR mouse assessed as cleavage rate of Gly-Pro-AMC in plasma at 3 mg/kg, po measured at 4.5 hrs by fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization. |
| AID429379 | Inhibition of human DPP4 by fluorimetry | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors. |
| AID771364 | In vivo inhibition of DPP-4 in ICR mouse assessed as cleavage rate of Gly-Pro-AMC in plasma at 1 mg/kg, po measured at 24 hrs by fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization. |
| AID688685 | Selectivity ratio of IC50 for FAPalpha to IC50 for human DPP4 | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID1570185 | Anti-diabetic activity in db/db mouse assessed as reduction in blood glucose AUC (0 to 120 mins) at 10 mg/kg, po dosed once daily for 3 weeks following 12 hrs fasting and glucose challenge measured up to 120 mins relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study. |
| AID566630 | Half life in human liver microsomes by LC/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID771382 | Inhibition of human DPP-4 using Gly-pro-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization. |
| AID1305330 | Antidiabetic activity in C57BL/6N mouse assessed as reduction in blood glucose AUC at 3 mg/kg, po administered for 60 mins followed by dextrose challenge by OGTT | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID771368 | In vivo inhibition of DPP-4 in ICR mouse assessed as cleavage rate of Gly-Pro-AMC in plasma at 3 mg/kg, po measured at 24 hrs by fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization. |
| AID1706174 | Anti-Hyperglycemic activity in high fat diet-fed/streptozotocin-induced type 2 diabetic mellitus C57BL/6 mouse model assessed as blood glucose level at 10 mg/kg, ip administered 30 mins prior to glucose challenge and measured after 2 hrs by IPGTT (Rvb = 1 | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors. |
| AID566627 | Inhibition of human DPP4 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID688687 | Selectivity ratio of IC50 for DPP8 to IC50 for human DPP4 | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID1706171 | Anti-Hyperglycemic activity in high fat diet-fed/streptozotocin-induced type 2 diabetic mellitus C57BL/6 mouse model assessed as blood glucose level at 10 mg/kg, ip administered 30 mins prior to glucose challenge and measured after 0.5 hrs by IPGTT (Rvb = | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors. |
| AID566629 | Half life in rat liver microsomes by LC/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID771371 | In vivo inhibition of DPP-4 in ICR mouse assessed as cleavage rate of Gly-Pro-AMC in plasma at 3 mg/kg, po measured at 0.5 hrs by fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization. |
| AID1486868 | Antidiabetic activity in HFD-fed C57BL/6J mouse assessed as increase in insulin secretion at 30 mg/kg, po pretreated for 1 hr followed by glucose challenge by OGTT | |||
| AID1631913 | Binding affinity to human recombinant DPP4 (39 to 766 residues) at 5 uM by isothermal titration calorimetry | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1781458 | Hypoglycemic activity in ICR mouse assessed as reduction in glucose secretion at 10 mg/kg, po via gavage administered as single dose pretreated with compound followed by glucose challenge measured after 120 mins relative to control | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Identification and structure-activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
| AID566686 | Inhibition of human ERG up to 30 uM | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID659753 | Reduction of glucose excursions in C57Bl/6j lean mouse at 3 mg/kg, po measured after 45 mins by oral glucose tolerance test | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization. |
| AID1570174 | Anti-diabetic activity in Sprague-Dawley rat assessed as redcution in DPP4 inhibition in plasma at 10 mg/kg, po via gavage administered as single dose measured up to 12 hrs post dose by fluorometric assay relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study. |
| AID749996 | Inhibition of DPP4 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Synthetic approaches to the 2011 new drugs. |
| AID771378 | Inhibition of CYP3A (unknown origin) | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization. |
| AID1570156 | Inhibition of DPP8 (unknown origin) using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition measured at 60 secs interval for 20 mins by fluorometic method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study. |
| AID1444855 | Inhibition of human recombinant DPP4 using Gly-Pro-7-amido-4-methyl-coumarin as substrate incubated for 15 mins by fluorescence assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Synthetic Approaches to the New Drugs Approved During 2015. |
| AID659747 | Inhibition of DPP8 | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization. |
| AID688693 | Inhibition of DPP8 | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID566687 | Toxicity in rat by GLP toxicology study | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID567006 | Inhibition of DPP9 after 20 mins by fluorescence assay | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes. |
| AID1305313 | Inhibition of QPP (unknown origin) preincubated for 30 mins followed by Nle-Pro-AMC addition measured for 50 mins by continuous fluorescence assay | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1305311 | Inhibition of human DPP4 preincubated for 30 mins followed by Gly-Pro-AMC addition measured for 50 mins by continuous fluorescence assay | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1305314 | Inhibition of recombinant DPP8 (unknown origin) preincubated for 20 mins followed by Ala-Pro-AFC addition measured for 40 mins by continuous fluorescence assay | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1706156 | Inhibition of DPP4 in human Caco-2 cells using AP-AFC as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured after 10 mins by fluorescence based analysis | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors. |
| AID1570157 | Inhibition of DPP9 (unknown origin) using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition measured at 60 secs interval for 20 mins by fluorometic method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study. |
| AID1570177 | Anti-diabetic activity in 12 hrs-fasted ICR mouse assessed as reduction in blood glucose AUC (0 to 120 mins)at 10 mg/kg, po pretreated for 60 mins followed by glucose challenge and measured after 120 mins post glucose challenge by OGTT relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study. |
| AID771369 | In vivo inhibition of DPP-4 in ICR mouse assessed as cleavage rate of Gly-Pro-AMC in plasma at 3 mg/kg, po measured at 7 hrs by fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization. |
| AID1189029 | Inhibition of human recombinant DPP4 pre-incubated with compound for 15 mins before substrate addition by luminescence assay | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes. |
| AID614455 | Inhibition of DPP4 in human plasma assessed as formation of 7-amino-4-methylcoumarin from glycyl-L-proline 4-methylcoumaryl-7-amide by fluorescence assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | 2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivatio |
| AID688686 | Selectivity ratio of IC50 for DPP9 to IC50 for human DPP4 | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID1305315 | Inhibition of DPP9 (unknown origin) preincubated for 20 mins followed by Gly-Pro-AMC addition measured for 50 mins by continuous fluorescence assay | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1781443 | Inhibition of human recombinant DPP4 using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by fluorescence based microplate reader assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Identification and structure-activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
| AID659746 | Inhibition of human DPP4 after 10 mins | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization. |
| AID688691 | Inhibition of FAPalpha | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID566685 | Inhibition of CYP3A4 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID1486867 | Antidiabetic activity in HFD-fed C57BL/6J mouse assessed as decrease in blood glucose level at 30 mg/kg, po pretreated for 1 hr followed by glucose challenge by OGTT | |||
| AID1706157 | Inhibition of DPP8 (unknown origin) | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors. |
| AID1781460 | Hypoglycemic activity in overnight fasted C57BL/6 db/db mouse reduction in blood glucose AUC (0 to 120 mins) at 10 mg/kg, po pretreated with compound for 30 mins followed by oral glucose challenge and measured up to 120 mins by glucometer relative to cont | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Identification and structure-activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
| AID1614273 | Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay | 2019 | Bioorganic & medicinal chemistry, 02-15, Volume: 27, Issue:4 | Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors. |
| AID1706160 | Selectivity index, ratio of IC50 for inhibition of DPP9 (unknown origin) to IC50 for inhibition of DPP4 in human Caco-2 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors. |
| AID566628 | Inhibition of human DPP8 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID567004 | Inhibition of DPP4 after 20 mins by fluorescence assay | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes. |
| AID688689 | Inhibition of DPP4 in human plasma using Gly-Pro-AMC as substrate by fluorimetric analysis | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID1189030 | Inhibition of human recombinant DPP8 pre-incubated with compound for 15 mins before substrate addition by luminescence assay | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes. |
| AID1706158 | Selectivity index, ratio of IC50 for inhibition of DPP8 (unknown origin) to IC50 for inhibition of DPP4 in human Caco-2 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors. |
| AID1781457 | In vivo inhibition of DPP4 in Sprague-Dawley rat plasma at 10 mg/kg, po via gavage using Gly-Pro-AMC as substrate measured after 24 hrs relative to control | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Identification and structure-activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
| AID1614274 | Inhibition of recombinant full-length human N-terminal GST-tagged DPP8 expressed in Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay | 2019 | Bioorganic & medicinal chemistry, 02-15, Volume: 27, Issue:4 | Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors. |
| AID1570155 | Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition measured at 60 secs interval for 20 mins by fluorometic method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study. |
| AID1614279 | Hypoglycemic activity in Kunming mouse assessed as decrease in blood glucose AUC (0 to 120 mins) at 10 mg/kg, po administered as single dose treated for 30 mins prior to glucose load by OGTT relative to control | 2019 | Bioorganic & medicinal chemistry, 02-15, Volume: 27, Issue:4 | Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors. |
| AID1631910 | Binding affinity to human recombinant DPP4 (39 to 766 residues) assessed as residence time on target by surface plasmon resonance analysis | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1614275 | Inhibition of recombinant full-length human N-terminal GST-tagged DPP9 expressed in Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay | 2019 | Bioorganic & medicinal chemistry, 02-15, Volume: 27, Issue:4 | Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors. |
| AID1706159 | Inhibition of DPP9 (unknown origin) | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors. |
| AID1917944 | Inhibition of human DPP4 using Gly-Pro-AMC as substrate incubated for 30 mins by continuous fluorescent assay | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Proline based rationally designed peptide esters against dipeptidyl peptidase-4: Highly potent anti-diabetic agents. |
| AID1706173 | Anti-Hyperglycemic activity in high fat diet-fed/streptozotocin-induced type 2 diabetic mellitus C57BL/6 mouse model assessed as blood glucose level at 10 mg/kg, ip administered 30 mins prior to glucose challenge and measured after 1.5 hrs by IPGTT (Rvb = | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors. |
| AID1781442 | Inhibition of human recombinant DPP8 using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by fluorescence based microplate reader assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Identification and structure-activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
| AID566681 | Inhibition of CYP1A2 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID771367 | In vivo inhibition of DPP-4 in ICR mouse assessed as cleavage rate of Gly-Pro-AMC in plasma at 1 mg/kg, po measured at 0.5 hrs by fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization. |
| AID771377 | Half life in Sprague-Dawley rat at 25 mg/kg, po | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization. |
| AID1395907 | Elimination half life in human | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
| AID1663821 | Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | A cell-based fluorescent assay for FAP inhibitor discovery. |
| AID1781466 | Antidiabetic activity in C57BL/6 db/db mouse assessed as reduction in blood glucose AUC (0 to 120 mins) at 10 mg/kg, po administered once daily for 4 weeks followed by 12 hrs fasting and subsequent glucose challenge and measured up to 120 mins by glucomet | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Identification and structure-activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
| AID286709 | Inhibition of hERG up to 30 uM | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. |
| AID566684 | Inhibition of CYP2D6 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID1486869 | Antidiabetic activity in HFD-fed C57BL/6J mouse assessed as decrease in blood glucose AUC at 30 mg/kg, po pretreated for 1 hr followed by glucose challenge after 1 hr of compound dosing measured up to 120 mins post glucose challenge by OGTT | |||
| AID1631905 | Inhibition of human recombinant DPP4 (39 to 766 residues) using Ala-Pro-AFC as substrate incubated for 1 hr by fluorescence assay | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1781440 | Inhibition of human recombinant DPP9 using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by fluorescence based microplate reader assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Identification and structure-activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
| AID1706172 | Anti-Hyperglycemic activity in high fat diet-fed/streptozotocin-induced type 2 diabetic mellitus C57BL/6 mouse model assessed as blood glucose level at 10 mg/kg, ip administered 30 mins prior to glucose challenge and measured after 1 hrs by IPGTT (Rvb = 1 | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors. |
| AID566683 | Inhibition of CYP2C19 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID1189031 | Inhibition of human recombinant DPP9 pre-incubated with compound for 15 mins before substrate addition by luminescence assay | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes. |
| AID1631908 | Binding affinity to human recombinant DPP4 (39 to 766 residues) assessed as association rate constant by surface plasmon resonance analysis | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID771366 | In vivo inhibition of DPP-4 in ICR mouse assessed as cleavage rate of Gly-Pro-AMC in plasma at 1 mg/kg, po measured at 4.5 hrs by fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization. |
| AID1706181 | Anti-Hyperglycemic activity in high fat diet-fed/streptozotocin-induced type 2 diabetic mellitus C57BL/6 mouse model assessed as reduction in AUC(0 to 120 mins) of blood glucose level at 10 mg/kg, ip administered 30 mins prior to glucose challenge and mea | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors. |
| AID1127773 | Inhibition of plasma DPP4 (unknown origin) after 24 hrs | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Dipeptidyl peptidase IV and its inhibitors: therapeutics for type 2 diabetes and what else? |
| AID1373610 | Inhibition of human DPP4 using A-P-7-amido-4-trifluoromethylcoumarin as substrate pretreated for 10 mins followed by substrate addition measured after 10 mins | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 | Surrogating and redirection of pyrazolo[1,5-a]pyrimidin-7(4H)-one core, a novel class of potent and selective DPP-4 inhibitors. |
| AID1706183 | Anti-Hyperglycemic activity in high fat diet-fed/streptozotocin-induced type 2 diabetic mellitus C57BL/6 mouse model assessed as reduction in blood glucose level at 10 mg/kg/day for 14 days and measured on day 14 | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors. |
| AID659748 | Inhibition of DPP9 | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization. |
| AID688688 | Inhibition of human DPP2 using Lys-Ala-AMC as substrate by fluorimetric analysis | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID1614272 | Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells at 40 nM using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay relative to control | 2019 | Bioorganic & medicinal chemistry, 02-15, Volume: 27, Issue:4 | Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors. |
| AID286707 | Improvement in glucose tolerance in Wistar fatty rat | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. |
| AID614482 | Ratio of Kinact/Ki for CYP3A4 in human liver microsomes | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | 2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivatio |
| AID1631907 | Binding affinity to human recombinant DPP4 (39 to 766 residues) by surface plasmon resonance analysis | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID286708 | Increase in plasma insulin level in Wistar fatty rat | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. |
| AID567007 | Inhibition of human ERG expressed in HEK293 cells after 3 hrs by nonradioactive rubidium efflux assay | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes. |
| AID1614285 | Hypoglycemic activity in Kunming mouse assessed as decrease in blood glucose AUC (0 to 120 mins) at 3 mg/kg, po administered as single dose treated for 30 mins prior to glucose load by OGTT relative to control | 2019 | Bioorganic & medicinal chemistry, 02-15, Volume: 27, Issue:4 | Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors. |
| AID1631909 | Binding affinity to human recombinant DPP4 (39 to 766 residues) assessed as dissociation rate constant by surface plasmon resonance analysis | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID566688 | Toxicity in dog by GLP toxicology study | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID566682 | Inhibition of CYP2C9 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID771365 | In vivo inhibition of DPP-4 in ICR mouse assessed as cleavage rate of Gly-Pro-AMC in plasma at 1 mg/kg, po measured at 7 hrs by fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization. |
| AID1797489 | DPP Inhibition Assay from Article 10.1021/jm070104l: \\Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV.\\ | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. |
| AID1801383 | In vitro Assay for Inhibition of DPP-4 from Article 10.1111/cbdd.12560: \\Design, Synthesis and Biological Evaluation of Imidazo[1,2-a]pyridine Derivatives as Novel DPP-4 Inhibitors.\\ | 2015 | Chemical biology & drug design, Oct, Volume: 86, Issue:4 | Design, Synthesis and Biological Evaluation of Imidazo[1,2-a]pyridine Derivatives as Novel DPP-4 Inhibitors. |
| AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| AID1345443 | Human dipeptidyl peptidase 4 (S9: Prolyl oligopeptidase) | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 20 (6.83) | 29.6817 |
| 2010's | 228 (77.82) | 24.3611 |
| 2020's | 45 (15.36) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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.
| This Compound (79.27) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 80 (26.49%) | 5.53% |
| Reviews | 62 (20.53%) | 6.00% |
| Case Studies | 6 (1.99%) | 4.05% |
| Observational | 7 (2.32%) | 0.25% |
| Other | 147 (48.68%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| To Evaluate the Effect of Nesinaact on Non-alcoholic Steatohepatitis Through MRI and Liver Fibroscan in Patients With Type 2 Diabetes: A Prospective, Open-Label, Single-Arm, Single-Center Clinical Study [NCT03950505] | Phase 4 | 60 participants (Anticipated) | Interventional | 2020-05-29 | Recruiting | ||
| A Randomized, Open, Single-dose, Crossover-design, Phase I Study to Evaluate Bioequivalence After Co-administration of ALO 25 mg and MET XR 1,000 mg or Administration of CT-L01 25/1,000 mg in Healthy Volunteers [NCT05363384] | Phase 1 | 48 participants (Actual) | Interventional | 2022-06-11 | Completed | ||
| 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) | Observational | 2012-10-31 | Not yet recruiting | |||
| A Long-Term, Open-Label Extension Study to Investigate the Long-Term Safety of SYR-322 When Used in Combination With Thiazolidine in Subjects With Type 2 Diabetes in Japan [NCT01318122] | Phase 2/Phase 3 | 336 participants (Actual) | Interventional | 2008-05-31 | Completed | ||
| A Phase 2/3, Double-Blind, Randomized, Placebo-Controlled, Parallel-Group, Multicenter Study to Determine the Efficacy and Safety of SYR-322 When Used in Combination With Sulfonylurea in Subjects With Type 2 Diabetes in Japan [NCT01318083] | Phase 2/Phase 3 | 312 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
| Post Marketing Surveillance Protocol for Nesina® Tablet [Monotherapy or Combination Therapy in Type 2 Diabetic Patients] [NCT04980040] | 3,623 participants (Actual) | Observational | 2014-04-19 | Completed | |||
| A Multi-center, Randomized, Double-blind, Placebo/Positive Parallel Phase III Clinical Trial to Evaluate the Efficacy and Safety of SAL067 in Type 2 Diabetes Patients Who Cannot Effectively Control Blood Glucose Through Diet and Exercise [NCT05782192] | Phase 3 | 458 participants (Actual) | Interventional | 2019-06-13 | Completed | ||
| A Phase 2/3, Double-Blind, Randomized, Placebo-Controlled, Parallel-Group, Multicenter Study to Determine the Efficacy and Safety of SYR-322 When Used in Combination With Metformin in Subjects With Type 2 Diabetes in Japan [NCT01318109] | Phase 2/Phase 3 | 288 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
| A Prospective, Non-Interventional Study of the Use of Alogliptin and Alogliptin Fixed-Dose Combinations With Pioglitazone and With Metformin in Standard Clinical Practice [NCT02989649] | 593 participants (Actual) | Observational | 2016-12-22 | Terminated(stopped due to Business Decision; No Safety Or Efficacy Concerns) | |||
| A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Alogliptin Compared With Placebo in Pediatric Subjects With Type 2 Diabetes Mellitus [NCT02856113] | Phase 3 | 152 participants (Actual) | Interventional | 2016-10-14 | Completed | ||
| Long-term Use of Alogliptin/Pioglitazone Combination Tablets in Patients With Type 2 Diabetes Mellitus [NCT01990300] | 3,281 participants (Actual) | Observational | 2011-11-28 | Completed | |||
| A Long-term, Open-label Extension Study to Investigate the Long-term Safety of Alogliptin When Used in Combination With Sulfonylurea or Metformin in Subjects With Type 2 Diabetes in Japan [NCT01318135] | Phase 2/Phase 3 | 576 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
| Local, Multicentre, Observational, Non-Interventional Prospective Study of Alogliptin Benzoate in Patients With Diabetes Mellitus Type 2 [NCT02756832] | 1,409 participants (Actual) | Observational | 2016-09-20 | Completed | |||
| Comparison of Glimepiride, Alogliptin and Alogliptin+Pioglitazone Combination in Poorly Controlled Type 2 Diabetic Patients [NCT04470310] | Phase 4 | 99 participants (Actual) | Interventional | 2015-12-31 | Active, not recruiting | ||
| A Randomized, Open, Single-dose, Crossover-design, Phase I Study to Evaluate Bioequivalence After Co-administration of ALO 12.5 mg and MET XR 500 mg or Administration of CT-L01 12.5/500 mg in Healthy Volunteers [NCT05363592] | Phase 1 | 48 participants (Actual) | Interventional | 2022-06-25 | Completed | ||
| A Phase 2/3, Double-Blind, Randomized, Placebo-Controlled, Parallel-Group, Multicenter Study to Determine the Efficacy and Safety of SYR-322 When Used in Combination With Thiazolidine in Subjects With Type 2 Diabetes in Japan [NCT01318070] | Phase 2/Phase 3 | 339 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
| Multicenter Trial on Effects of Alogliptin on Pancreatic Beta Cell Function [NCT01303055] | 80 participants (Anticipated) | Interventional | 2011-02-28 | Recruiting | |||
| A Randomized, Open-Label, Single-Dose, 4-Period Crossover Study to Determine the Bioequivalence of Alogliptin (25 mg) and Pioglitazone (15 and 30 mg) When Administered as Individual Tablets and as Fixed-Dose Combination Tablets to Healthy Russian Subjects [NCT03501277] | Phase 1 | 72 participants (Actual) | Interventional | 2018-05-26 | Completed | ||
| A Phase 2/3, Double-blind, Randomized, Placebo-controlled, Parallel-group, Multicenter Study to Determine the Efficacy and Safety of SYR-322 When Used in Combination With α-glucosidase Inhibitor in Subjects With Type 2 Diabetes in Japan [NCT01263483] | Phase 2/Phase 3 | 230 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
| A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate Cardiovascular Outcomes Following Treatment With Alogliptin in Addition to Standard of Care in Subjects With Type 2 Diabetes and Acute Coronary Syndrome [NCT00968708] | Phase 3 | 5,380 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
| A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Determine the Efficacy and Safety of Alogliptin Plus Metformin, Alogliptin Alone, or Metformin Alone in Subjects With Type 2 Diabetes [NCT01023581] | Phase 3 | 784 participants (Actual) | Interventional | 2009-11-30 | Completed | ||
| A Long-Term, Open-Label Extension Study to Investigate the Long-Term Safety of SYR110322 (SYR-322) in Subjects With Type 2 Diabetes [NCT00306384] | Phase 3 | 3,323 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
| A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Determine the Efficacy and Safety of SYR110322 (SYR-322) When Used in Combination With Pioglitazone in Subjects With Type 2 Diabetes Mellitus [NCT00286494] | Phase 3 | 493 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
| [NCT02798172] | 81 participants (Actual) | Interventional | 2014-05-31 | Completed | |||
| An Exploratory Study to Evaluate the Effects of Trelagliptin and Alogliptin by CGM on Glucose Variability for One Week in Patients With Type 2 Diabetes Mellitus [NCT02771093] | Phase 4 | 27 participants (Actual) | Interventional | 2016-09-08 | Completed | ||
| A Phase 1b, Randomized, Double-Blind, Active Comparator (Open-Label Exenatide) Controlled Study to Evaluate the Effect of Roflumilast Plus Alogliptin on Postprandial Active GLP-1 Level and 24-hour Glucose Level in Subjects With Type 2 Diabetes Who Are Ina [NCT01664624] | Phase 1 | 40 participants (Actual) | Interventional | 2012-07-31 | Completed | ||
| A Multicenter, Double-Blind Study to Determine the Efficacy and Safety of SYR-322 Plus Pioglitazone HCl (Actos®), SYR-322 Alone or Pioglitazone HCl Alone in Subjects With Type 2 Diabetes [NCT00395512] | Phase 3 | 655 participants (Actual) | Interventional | 2006-11-30 | Completed | ||
| Efficacy and Safety of Alogliptin vs. Acarbose in Chinese T2DM Patients With High CV Risk or CHD Treated With Aspirin and Inadequately Controlled With Metformin Monotherapy or Drug Naive: A Multicenter, Randomized, Open Label, Prospective Study [NCT03794336] | Phase 4 | 1,293 participants (Actual) | Interventional | 2019-06-29 | Completed | ||
| Treatment Preference for Weekly DPP-4 Inhibitors Versus Daily DPP-4 Inhibitors in Patients With Type 2 Diabetes Mellitus [NCT03231709] | Phase 4 | 60 participants (Actual) | Interventional | 2017-08-18 | Completed | ||
| A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Determine the Efficacy and Safety of SYR110322 (SYR-322) When Used in Combination With a Sulfonylurea in Subjects With Type 2 Diabetes [NCT00286468] | Phase 3 | 500 participants (Actual) | Interventional | 2006-04-30 | Completed | ||
| A Multicenter, Randomized, Double-Blind, Placebo-Controlled Comparison Study to Determine the Efficacy and Safety of SYR110322 in Patients With Type 2 Diabetes, Who Are Either Receiving No Current Treatment or Currently Treated With Diet and Exercise, Sul [NCT00755846] | Phase 2 | 265 participants (Actual) | Interventional | 2005-03-31 | Completed | ||
| A Phase 2, Double-Blind Randomized, Placebo-Controlled, Parallel Group, Multicenter Study to Evaluate Treatment With SYR-619 in Subjects With Type 2 Diabetes [NCT00763347] | Phase 2 | 82 participants (Actual) | Interventional | 2006-11-30 | Terminated(stopped due to Voluntarily terminated based on preliminary non-clinical findings.) | ||
| A Long-Term, Open-Label Study to Investigate the Long-Term Safety of SYR-322 When Used in Combination With Rapid-Acting Insulin Secretagogues in Subjects With Type 2 Diabetes in Japan [NCT01456130] | Phase 3 | 67 participants (Actual) | Interventional | 2011-11-30 | Completed | ||
| Comparison of Type 2 Diabetes Pharmacotherapy Regimens Using Targeted Learning [NCT05073692] | 270,000 participants (Anticipated) | Observational | 2021-07-01 | Recruiting | |||
| A Multicenter, Randomized, Double-Blind Study to Determine the Efficacy and Safety of the Addition of SYR-322 25 mg Versus Dose Titration From 30 mg to 45 mg of Pioglitazone HCl (ACTOS®) in Subjects With Type 2 Diabetes Mellitus Who Have Inadequate Contro [NCT00432276] | Phase 3 | 803 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
| A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Determine the Efficacy and Safety of SYR110322 (SYR-322) Compared With Placebo in Subjects With Type 2 Diabetes [NCT00286455] | Phase 3 | 329 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
| A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Determine the Efficacy and Safety of SYR110322 (SYR-322) When Used in Combination With Metformin in Subjects With Type 2 Diabetes [NCT00286442] | Phase 3 | 527 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
| A Phase 2, Double-blind, Randomized, Placebo-controlled, Parallel-group, Multicenter Study to Determine the Efficacy and Safety of SYR-322 in Subjects With Type 2 Diabetes in Japan [NCT01263470] | Phase 2 | 480 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
| A Randomized, Open-label, Crossover Study to Determine the Effect of Food on the Pharmacokinetics of Single Oral Dose Administration of a Fixed-Dose Combination of SYR-322 and Metformin Hydrochloride in Healthy Adult Male Subjects [NCT02276274] | Phase 3 | 12 participants (Actual) | Interventional | 2014-06-30 | Completed | ||
| Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study Comparing SYR-322 Alone and Combination SYR-322 With Pioglitazone Versus Placebo on Postprandial Lipids in Subjects With Type 2 Diabetes [NCT00655863] | Phase 3 | 71 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
| A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Determine the Efficacy and Safety of the Combination of SYR-322 (SYR110322) and Pioglitazone HCl (ACTOS®), in Subjects With Type 2 Diabetes [NCT00328627] | Phase 3 | 1,554 participants (Actual) | Interventional | 2006-05-31 | Completed | ||
| A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Determine the Efficacy and Safety of SYR110322 (SYR-322) When Used in Combination With Insulin in Subjects With Type 2 Diabetes [NCT00286429] | Phase 3 | 390 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
| A Multicenter, Randomized, Double-Blind, Active-Controlled Study to Evaluate the Durability of the Efficacy and Safety of Alogliptin Compared to Glipizide When Used in Combination With Metformin in Subjects With Type 2 Diabetes [NCT00856284] | Phase 3 | 2,639 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
| An Extension Study of Protocol ALO-IIT(PEAK Study) to Examine the Long-term Efficacy and Safety of Metformin + Alogliptin + Pioglitazone Triple Combination Therapy in the Korean Type 2 Diabetes Patients [NCT02763007] | Phase 4 | 41 participants (Actual) | Interventional | 2016-05-18 | Terminated(stopped due to difficulty in recruiting patients) | ||
| A Comparative, Randomized, Open-Label, Multi-Center, Single Dose Pharmacokinetic, Pharmacodynamic and Safety Study of Alogliptin (12.5 mg and 25 mg) Between Children, Adolescents, and Adults With Type 2 (Non-Insulin Dependent) Diabetes Mellitus [NCT00957268] | Phase 1 | 46 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
| A Phase 3 Study to Investigate the Efficacy and Safety of SYR-322 When Used in Combination With Insulin Preparation in Subjects With Type 2 Diabetes in Japan [NCT01521962] | Phase 3 | 67 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
| An International, Multicenter, Randomized, Double-blind, Placebo-controlled, Phase 3 Study to Determine the Efficacy and Safety of SYR-322 When Used in Subjects With Type 2 Diabetes [NCT01289119] | Phase 3 | 506 participants (Actual) | Interventional | 2010-12-31 | Completed | ||
| A Long-term, Open-label Extension Study to Investigate the Long-term Safety of SYR-322 in Subjects With Type 2 Diabetes in Japan. [NCT01263496] | Phase 2 | 438 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
| A Phase 1, Randomized, Double-Blind, Placebo-Controlled, Single and Multiple-Dose Study of the Pharmacokinetics and Pharmacodynamics of Alogliptin 12.5 mg, 25 mg and 50 mg in Healthy Korean Subjects [NCT01391663] | Phase 1 | 48 participants (Actual) | Interventional | 2011-07-31 | Completed | ||
| A Long-term, Open-label Extension Study to Investigate the Long-term Safety of SYR-322 When Used in Combination With α-glucosidase Inhibitor in Subjects With Type 2 Diabetes in Japan [NCT01263509] | Phase 2/Phase 3 | 179 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
| 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 3 | 106 participants (Actual) | Interventional | 2010-10-21 | Completed | ||
| "Alogliptin (Nesina) Tablets Specified Drug-use Survey Type 2 Diabetes Mellitus: Combination Therapy With Hypoglycemic Drug (Insulin Preparation or Rapid-acting Insulin Secretagogues, Etc)" [NCT02221284] | 964 participants (Actual) | Observational | 2014-06-30 | Completed | |||
| Comparative Effectiveness and Safety of Four Second Line Pharmacological Strategies in Type 2 Diabetes Study [NCT05220917] | 781,430 participants (Anticipated) | Observational | 2021-08-01 | Active, not recruiting | |||
| Comparison of Anti-inflammatory Status Linked to Atherosclerosis Formation/Progression Among Diabetes Mellitus Type 2 Patients Under Combined Pharmacological Therapy [NCT04392557] | Phase 4 | 36 participants (Anticipated) | Interventional | 2020-07-01 | Recruiting | ||
| A Multicenter, Randomized, Double-Blind Study to Evaluate the Efficacy and Safety of Alogliptin Compared to Glipizide in Elderly Subjects With Type 2 Diabetes [NCT00707993] | Phase 3 | 441 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| [NCT01632007] | Phase 3 | 245 participants (Anticipated) | Interventional | 2012-05-01 | Completed | ||
| "Nesina Tablets Special Drug Use Surveillance Type 2 Diabetes Mellitus: Combination Therapy With Thiazolidinediones" [NCT01945242] | 1,374 participants (Actual) | Observational | 2011-03-31 | Completed | |||
| An Open-Label, Single-dose, Randomized, Crossover Study to Determine the Bioavailability and Bioequivalence of Alogliptin 12.5 mg and Metformin 1000 mg When Administered as Individual Tablets and as a Fixed-Dose Combination Tablet Vipdomet (Alogliptin FDC [NCT02508168] | Phase 1 | 24 participants (Actual) | Interventional | 2016-04-30 | Completed | ||
| Prospective, Multi-center, Open-label, Phase IV Study to Evaluate the Safety and Efficacy of Alogliptin as Monotherapy or Add on Therapy in Indian Patients With Type 2 Diabetes Mellitus [NCT03042325] | Phase 4 | 0 participants (Actual) | Interventional | 2017-07-30 | Withdrawn(stopped due to Business decision, no safety or efficacy concerns) | ||
| "Alogliptin Tablets Special Drug Use Surveillance Type 2 Diabetes Mellitus: Monotherapy/Combination Therapy With α-GI" [NCT01945216] | 3,317 participants (Actual) | Observational | 2010-07-08 | Completed | |||
| A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Determine the Efficacy and Safety of Alogliptin and Metformin Fixed Dose Combination, Alogliptin Alone, or Metformin Alone in Subjects With Type 2 Diabetes Mellitus [NCT01890122] | Phase 3 | 647 participants (Actual) | Interventional | 2013-09-30 | Completed | ||
| A Multicenter, Randomized, Open-label, Two-arm, Phase 4 Study to Evaluate the Effect of Add-on Pioglitazone or Dapagliflozin in Subjects With Type 2 Diabetes Mellitus Inadequately Controlled by Dipeptidyl Peptidase-4 Inhibitor and Metformin Therapy [NCT03499704] | Phase 4 | 133 participants (Actual) | Interventional | 2020-02-11 | Active, not recruiting | ||
| A Phase 3 Multicenter, Randomized, Double-blind, Parallel-group, Comparative Study When Metformin Hydrochloride 500 mg is Added on to SYR-322 25 mg in Type 2 Diabetic Patients [NCT02068443] | Phase 3 | 374 participants (Actual) | Interventional | 2014-02-28 | Completed | ||
| Alogliptin (Nesina) Tablets Special Drug Use Surveillance: Mild Type 2 Diabetes Mellitus [NCT01964963] | 19,192 participants (Actual) | Observational | 2011-08-03 | Completed | |||
| "Specified Drug-Use Survey of Alogliptin and Metformin Hydrochloride Combination Tablets Survey on Long-term Use in Type 2 Diabetes Mellitus Patients With Renal or Hepatic Impairment or Advanced Age" [NCT03555565] | 1,026 participants (Actual) | Observational | 2017-02-28 | Completed | |||
| Multicenter, Randomized, Double Blind, Three-arm Parallel Group Study to Evaluate Efficacy and Safety of Alogliptin and Pioglitazone Combination Therapy on Glucose Control in Type 2 Diabetes Subjects Who Have Inadequate Control With Metformin Monotherapy [NCT02231021] | Phase 4 | 216 participants (Actual) | Interventional | 2014-09-30 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||
The change between Body Weight measured at week 8 and Body Weight measured at baseline. (NCT00286429)
Timeframe: Baseline and Week 8.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | 0.39 |
| Alogliptin 12.5 mg QD | 0.10 |
| Alogliptin 25 mg QD | 0.18 |
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 8 and Glycosylated Hemoglobin collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 8.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.27 |
| Alogliptin 12.5 mg QD | -0.76 |
| Alogliptin 25 mg QD | -0.84 |
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 4 and Glycosylated Hemoglobin collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 4.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.26 |
| Alogliptin 12.5 mg QD | -0.47 |
| Alogliptin 25 mg QD | -0.58 |
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 20 and Glycosylated Hemoglobin collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 20.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.17 |
| Alogliptin 12.5 mg QD | -0.76 |
| Alogliptin 25 mg QD | -0.74 |
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 16 and Glycosylated Hemoglobin collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 16.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.22 |
| Alogliptin 12.5 mg QD | -0.80 |
| Alogliptin 25 mg QD | -0.76 |
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 12 and Glycosylated Hemoglobin collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 12.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.27 |
| Alogliptin 12.5 mg QD | -0.84 |
| Alogliptin 25 mg QD | -0.81 |
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 26 or final visit and glycosylated hemoglobin collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 26.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.13 |
| Alogliptin 12.5 mg QD | -0.63 |
| Alogliptin 25 mg QD | -0.71 |
The change between the value of fasting plasma glucose collected at week 8 and fasting plasma glucose collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 8.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 5.4 |
| Alogliptin 12.5 mg QD | -13.5 |
| Alogliptin 25 mg QD | -14.1 |
The change between the value of fasting plasma glucose collected at week 4 and fasting plasma glucose collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 4.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 5.3 |
| Alogliptin 12.5 mg QD | -5.0 |
| Alogliptin 25 mg QD | -12.1 |
The change between the value of fasting plasma glucose collected at week 26 or final visit and fasting plasma glucose collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 26.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 5.8 |
| Alogliptin 12.5 mg QD | 2.3 |
| Alogliptin 25 mg QD | -11.7 |
The change between the value of fasting plasma glucose collected at week 20 and fasting plasma glucose collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 20.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 8.6 |
| Alogliptin 12.5 mg QD | -4.2 |
| Alogliptin 25 mg QD | -11.3 |
The change between the value of fasting plasma glucose collected at week 2 and fasting plasma glucose collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 2.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 1.0 |
| Alogliptin 12.5 mg QD | -3.1 |
| Alogliptin 25 mg QD | -11.4 |
The change between the value of fasting plasma glucose collected at week 16 and fasting plasma glucose collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 16.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 4.6 |
| Alogliptin 12.5 mg QD | -5.3 |
| Alogliptin 25 mg QD | -6.3 |
The change between the value of fasting plasma glucose collected at week 12 and fasting plasma glucose collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -1.4 |
| Alogliptin 12.5 mg QD | -5.2 |
| Alogliptin 25 mg QD | -2.9 |
The change between the value of fasting plasma glucose collected at final visit or week 1 and fasting plasma glucose collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 1.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 6.3 |
| Alogliptin 12.5 mg QD | -5.0 |
| Alogliptin 25 mg QD | -9.9 |
The change between the value of C-peptide collected at week 8 and C-peptide collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 8.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.024 |
| Alogliptin 12.5 mg QD | 0.178 |
| Alogliptin 25 mg QD | 0.348 |
The change between the value of C-peptide collected at week 4 and C-peptide collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 4.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.023 |
| Alogliptin 12.5 mg QD | 0.132 |
| Alogliptin 25 mg QD | 0.453 |
The change between the value of C-peptide collected at week 26 or final visit and C-peptide collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 26.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.083 |
| Alogliptin 12.5 mg QD | 0.199 |
| Alogliptin 25 mg QD | 0.042 |
The change between the value of C-peptide collected at week 20 and C-peptide collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 20.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | 0.239 |
| Alogliptin 12.5 mg QD | 0.318 |
| Alogliptin 25 mg QD | 0.281 |
The change between the value of C-peptide collected at week 16 and C-peptide collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 16.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | 0.241 |
| Alogliptin 12.5 mg QD | 0.319 |
| Alogliptin 25 mg QD | 0.396 |
The change between Body Weight measured at week 26 or final visit and Body Weight measured at baseline. (NCT00286429)
Timeframe: Baseline and Week 26.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | 0.63 |
| Alogliptin 12.5 mg QD | 0.68 |
| Alogliptin 25 mg QD | 0.60 |
The change between Body Weight measured at week 12 and Body Weight measured at baseline. (NCT00286429)
Timeframe: Baseline and Week 12.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | 0.50 |
| Alogliptin 12.5 mg QD | 0.44 |
| Alogliptin 25 mg QD | 0.31 |
The number of participants with a fasting plasma glucose value greater than or equal to 200 mg per dL during the 26 week study. (NCT00286429)
Timeframe: 26 Weeks.
| Intervention | participants (Number) |
|---|---|
| Placebo | 105 |
| Alogliptin 12.5 mg QD | 99 |
| Alogliptin 25 mg QD | 86 |
The change between Body Weight measured at week 20 and Body Weight measured at baseline. (NCT00286429)
Timeframe: Baseline and Week 20.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | 0.73 |
| Alogliptin 12.5 mg QD | 0.55 |
| Alogliptin 25 mg QD | 0.45 |
The change between the value of C-peptide collected at week 12 and C-peptide collected at baseline. (NCT00286429)
Timeframe: Baseline and Week 12.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | 0.207 |
| Alogliptin 12.5 mg QD | 0.333 |
| Alogliptin 25 mg QD | 0.390 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 2.0% during the 26 week study. (NCT00286429)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 0 |
| Alogliptin 12.5 mg QD | 11 |
| Alogliptin 25 mg QD | 11 |
The number of participants requiring rescue for failing to achieve pre-specified glycemic targets during the 26 week study. (NCT00286429)
Timeframe: 26 Weeks.
| Intervention | participants (Number) |
|---|---|
| Placebo | 52 |
| Alogliptin 12.5 mg QD | 27 |
| Alogliptin 25 mg QD | 25 |
The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 6.5% during the 26 week study. (NCT00286429)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 0 |
| Alogliptin 12.5 mg QD | 3 |
| Alogliptin 25 mg QD | 3 |
The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 7.0% during the 26 week study. (NCT00286429)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 1 |
| Alogliptin 12.5 mg QD | 11 |
| Alogliptin 25 mg QD | 10 |
The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 7.5% during the 26 week study. (NCT00286429)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 5 |
| Alogliptin 12.5 mg QD | 22 |
| Alogliptin 25 mg QD | 33 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 0.5% during the 26 week study. (NCT00286429)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 40 |
| Alogliptin 12.5 mg QD | 70 |
| Alogliptin 25 mg QD | 70 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 1.0% during the 26 week study. (NCT00286429)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 17 |
| Alogliptin 12.5 mg QD | 41 |
| Alogliptin 25 mg QD | 47 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 1.5% during the 26 week study. (NCT00286429)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 6 |
| Alogliptin 12.5 mg QD | 22 |
| Alogliptin 25 mg QD | 23 |
The change between the value of insulin collected at week 16 and insulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 16.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | 1.27 |
| Alogliptin 25 mg QD | 1.53 |
| Placebo | 0.64 |
The change between the value of insulin collected at week 12 and insulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 12.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | 1.6 |
| Alogliptin 25 mg QD | 0.46 |
| Placebo | 1.92 |
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 8 and Glycosylated Hemoglobin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 8.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.59 |
| Alogliptin 25 mg QD | -0.59 |
| Placebo | -0.21 |
The number of participants with a fasting plasma glucose value greater than or equal to 200 mg per dL during the 26 week study. (NCT00286442)
Timeframe: 26 Weeks.
| Intervention | participants (Number) |
|---|---|
| Alogliptin 12.5 mg QD | 61 |
| Alogliptin 25 mg QD | 65 |
| Placebo | 53 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 2.0% during the 26 week study. (NCT00286442)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Alogliptin 12.5 mg QD | 7 |
| Alogliptin 25 mg QD | 5 |
| Placebo | 4 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 1.5% during the 26 week study. (NCT00286442)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Alogliptin 12.5 mg QD | 20 |
| Alogliptin 25 mg QD | 24 |
| Placebo | 6 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 1.0% during the 26 week study. (NCT00286442)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Alogliptin 12.5 mg QD | 61 |
| Alogliptin 25 mg QD | 62 |
| Placebo | 9 |
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 4 and Glycosylated Hemoglobin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 4.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.36 |
| Alogliptin 25 mg QD | -0.40 |
| Placebo | -0.10 |
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 20 and Glycosylated Hemoglobin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 20.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.63 |
| Alogliptin 25 mg QD | -0.63 |
| Placebo | -0.12 |
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 16 and Glycosylated Hemoglobin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 16.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.66 |
| Alogliptin 25 mg QD | -0.64 |
| Placebo | -0.13 |
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 12 and Glycosylated Hemoglobin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 12.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.66 |
| Alogliptin 25 mg QD | -0.66 |
| Placebo | -0.16 |
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 26 or final visit and glycosylated hemoglobin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 26.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.61 |
| Alogliptin 25 mg QD | -0.59 |
| Placebo | -0.10 |
The change between the value of fasting proinsulin collected at week 26 or final visit and fasting proinsulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 26.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -2.1 |
| Alogliptin 25 mg QD | -1.6 |
| Placebo | -3.2 |
The change between the value of fasting proinsulin collected at week 8 and fasting proinsulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 8.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -2.9 |
| Alogliptin 25 mg QD | -5.0 |
| Placebo | -0.4 |
The change between the value of fasting proinsulin collected at week 4 and fasting proinsulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 4.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -1.9 |
| Alogliptin 25 mg QD | -5.0 |
| Placebo | -0.5 |
The change between the ratio value of proinsulin and insulin collected at week 8 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 8.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.055 |
| Alogliptin 25 mg QD | -0.046 |
| Placebo | -0.009 |
The change between Body Weight measured at week 12 and Body Weight measured at baseline. (NCT00286442)
Timeframe: Baseline and Week 12.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.28 |
| Alogliptin 25 mg QD | -0.64 |
| Placebo | -0.57 |
The change between Body Weight measured at week 20 and Body Weight measured at baseline. (NCT00286442)
Timeframe: Baseline and Week 20.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.38 |
| Alogliptin 25 mg QD | -0.58 |
| Placebo | -0.40 |
The change between Body Weight measured at week 26 or final visit and Body Weight measured at baseline. (NCT00286442)
Timeframe: Baseline and Week 26.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.39 |
| Alogliptin 25 mg QD | -0.67 |
| Placebo | -0.39 |
The change between Body Weight measured at week 8 and Body Weight measured at baseline. (NCT00286442)
Timeframe: Baseline and Week 8.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.30 |
| Alogliptin 25 mg QD | -0.53 |
| Placebo | -0.12 |
The change between the value of C-peptide collected at week 12 and C-peptide collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 12.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | 0.154 |
| Alogliptin 25 mg QD | 0.246 |
| Placebo | -0.033 |
The change between the value of C-peptide collected at week 16 and C-peptide collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 16.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | 0.138 |
| Alogliptin 25 mg QD | 0.250 |
| Placebo | -0.018 |
The change between the value of C-peptide collected at week 20 and C-peptide collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 20.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | 0.007 |
| Alogliptin 25 mg QD | 0.054 |
| Placebo | -0.137 |
The change between the value of C-peptide collected at week 26 or final visit and C-peptide collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 26.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.083 |
| Alogliptin 25 mg QD | -0.214 |
| Placebo | -0.476 |
The change between the value of C-peptide collected at week 4 and C-peptide collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 4.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | 0.222 |
| Alogliptin 25 mg QD | 0.190 |
| Placebo | -0.114 |
The change between the value of C-peptide collected at week 8 and C-peptide collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 8.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | 0.215 |
| Alogliptin 25 mg QD | 0.238 |
| Placebo | 0.127 |
The change between the value of fasting plasma glucose collected at final visit or week 1 and fasting plasma glucose collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 1.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -14.3 |
| Alogliptin 25 mg QD | -12.5 |
| Placebo | -0.6 |
The change between the value of fasting plasma glucose collected at week 12 and fasting plasma glucose collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -16.9 |
| Alogliptin 25 mg QD | -16.8 |
| Placebo | 0.3 |
The change between the value of fasting plasma glucose collected at week 16 and fasting plasma glucose collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 16.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -17.8 |
| Alogliptin 25 mg QD | -15.4 |
| Placebo | 1.3 |
The change between the ratio value of proinsulin and insulin collected at week 4 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 4.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.045 |
| Alogliptin 25 mg QD | -0.056 |
| Placebo | -0.008 |
The change between the ratio value of proinsulin and insulin collected at week 26 or final visit and the ratio value of proinsulin and insulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 26.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.049 |
| Alogliptin 25 mg QD | 0.000 |
| Placebo | 0.004 |
The change between the value of fasting plasma glucose collected at week 20 and fasting plasma glucose collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 20.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -18.1 |
| Alogliptin 25 mg QD | -15.6 |
| Placebo | -0.1 |
The change between the value of fasting plasma glucose collected at week 26 or final visit and fasting plasma glucose collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 26.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -18.7 |
| Alogliptin 25 mg QD | -17.4 |
| Placebo | 0.0 |
The change between the value of fasting plasma glucose collected at week 4 and fasting plasma glucose collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 4.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -18.4 |
| Alogliptin 25 mg QD | -18.1 |
| Placebo | -0.6 |
The change between the value of fasting plasma glucose collected at week 8 and fasting plasma glucose collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 8.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -19.6 |
| Alogliptin 25 mg QD | -17.2 |
| Placebo | 0.4 |
The change between the value of fasting proinsulin collected at week 12 and fasting proinsulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 12.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -2.6 |
| Alogliptin 25 mg QD | -2.7 |
| Placebo | -1.3 |
The change between the value of fasting proinsulin collected at week 16 and fasting proinsulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 16.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -1.4 |
| Alogliptin 25 mg QD | -2.7 |
| Placebo | -0.5 |
The change between the value of fasting proinsulin collected at week 20 and fasting proinsulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 20.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -4.2 |
| Alogliptin 25 mg QD | -1.1 |
| Placebo | -2.0 |
The number of participants requiring rescue for failing to achieve pre-specified glycemic targets during the 26 week study. (NCT00286442)
Timeframe: 26 Weeks.
| Intervention | participants (Number) |
|---|---|
| Alogliptin 12.5 mg QD | 19 |
| Alogliptin 25 mg QD | 17 |
| Placebo | 25 |
The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 6.5% during the 26 week study. (NCT00286442)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Alogliptin 12.5 mg QD | 42 |
| Alogliptin 25 mg QD | 36 |
| Placebo | 4 |
The change between the value of fasting plasma glucose collected at week 2 and fasting plasma glucose collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 2.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -17.4 |
| Alogliptin 25 mg QD | -17.6 |
| Placebo | -0.7 |
The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 7.5% during the 26 week study. (NCT00286442)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Alogliptin 12.5 mg QD | 153 |
| Alogliptin 25 mg QD | 137 |
| Placebo | 47 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 0.5% during the 26 week study. (NCT00286442)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Alogliptin 12.5 mg QD | 123 |
| Alogliptin 25 mg QD | 122 |
| Placebo | 28 |
The change between the ratio value of proinsulin and insulin collected at week 20 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 20.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.53 |
| Alogliptin 25 mg QD | -0.011 |
| Placebo | -0.007 |
The change between the ratio value of proinsulin and insulin collected at week 16 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 16.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.051 |
| Alogliptin 25 mg QD | -0.043 |
| Placebo | 0.001 |
The change between the ratio value of proinsulin and insulin collected at week 12 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 12.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | -0.044 |
| Alogliptin 25 mg QD | -0.042 |
| Placebo | -0.005 |
The change between the value of insulin collected at week 8 and insulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 8.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | 2.50 |
| Alogliptin 25 mg QD | 0.18 |
| Placebo | 2.68 |
The change between the value of insulin collected at week 4 and insulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 4.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | 1.11 |
| Alogliptin 25 mg QD | 0.52 |
| Placebo | -1.07 |
The change between the value of insulin collected at week 26 and insulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 26.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | 0.63 |
| Alogliptin 25 mg QD | -0.01 |
| Placebo | -2.23 |
The change between the value of insulin collected at week 20 and insulin collected at baseline. (NCT00286442)
Timeframe: Baseline and Week 20.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Alogliptin 12.5 mg QD | 0.91 |
| Alogliptin 25 mg QD | 0.86 |
| Placebo | -0.21 |
The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 7.0% during the 26 week study. (NCT00286442)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Alogliptin 12.5 mg QD | 110 |
| Alogliptin 25 mg QD | 92 |
| Placebo | 19 |
The change between the ratio value of proinsulin and insulin collected at week 16 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 16.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo QD | 0.001 |
| Alogliptin 12.5 mg QD | -0.044 |
| Alogliptin 25 mg QD | -0.039 |
The change between the ratio value of proinsulin and insulin collected at week 12 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 12.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo QD | 0.025 |
| Alogliptin 12.5 mg QD | -0.043 |
| Alogliptin 25 mg QD | -0.047 |
The change between the value of insulin collected at week 8 and insulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 8.
| Intervention | ϻIU/mL (Least Squares Mean) |
|---|---|
| Placebo QD | -0.35 |
| Alogliptin 12.5 mg QD | 1.18 |
| Alogliptin 25 mg QD | 0.94 |
The change between the value of insulin collected at week 4 and insulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 4.
| Intervention | ϻIU/mL (Least Squares Mean) |
|---|---|
| Placebo QD | 0.87 |
| Alogliptin 12.5 mg QD | 0.14 |
| Alogliptin 25 mg QD | -1.27 |
The change between the value of insulin collected at week 20 and insulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 20.
| Intervention | ϻIU/mL (Least Squares Mean) |
|---|---|
| Placebo QD | -1.32 |
| Alogliptin 12.5 mg QD | -0.32 |
| Alogliptin 25 mg QD | -1.12 |
The change between the value of insulin collected at week 16 and insulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 16.
| Intervention | ϻIU/mL (Least Squares Mean) |
|---|---|
| Placebo QD | -0.41 |
| Alogliptin 12.5 mg QD | 0.55 |
| Alogliptin 25 mg QD | -1.46 |
The change between the value of insulin collected at week 12 and insulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 12.
| Intervention | ϻIU/mL (Least Squares Mean) |
|---|---|
| Placebo QD | -1.66 |
| Alogliptin 12.5 mg QD | 0.94 |
| Alogliptin 25 mg QD | -1.60 |
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 8 and Glycosylated Hemoglobin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 8.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo QD | -0.13 |
| Alogliptin 12.5 mg QD | -0.53 |
| Alogliptin 25 mg QD | -0.64 |
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 4 and Glycosylated Hemoglobin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 4.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo QD | -0.11 |
| Alogliptin 12.5 mg QD | -0.37 |
| Alogliptin 25 mg QD | -0.45 |
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 20 and Glycosylated Hemoglobin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 20.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo QD | -0.12 |
| Alogliptin 12.5 mg QD | -0.58 |
| Alogliptin 25 mg QD | -0.61 |
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 16 and Glycosylated Hemoglobin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 16.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo QD | -0.12 |
| Alogliptin 12.5 mg QD | -0.59 |
| Alogliptin 25 mg QD | -0.65 |
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 12 and Glycosylated Hemoglobin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 12.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo QD | -0.13 |
| Alogliptin 12.5 mg QD | -0.57 |
| Alogliptin 25 mg QD | -0.66 |
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 26 or final visit and glycosylated hemoglobin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo QD | -0.02 |
| Alogliptin 12.5 mg QD | -0.56 |
| Alogliptin 25 mg QD | -0.59 |
The change between the value of glucagon collected at week 8 and glucagon collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 8.
| Intervention | pg/mL (Mean) |
|---|---|
| Placebo QD | -1.2 |
| Alogliptin 12.5 mg QD | -0.9 |
| Alogliptin 25 mg QD | -0.2 |
The change between the value of glucagon collected at week 4 and glucagon collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 4.
| Intervention | pg/mL (Mean) |
|---|---|
| Placebo QD | 2.1 |
| Alogliptin 12.5 mg QD | 3.6 |
| Alogliptin 25 mg QD | 1.8 |
The change between the value of glucagon collected at week 26 or final visit and glucagon collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | pg/mL (Mean) |
|---|---|
| Placebo QD | 5.2 |
| Alogliptin 12.5 mg QD | 4.2 |
| Alogliptin 25 mg QD | 2.4 |
The change between the value of glucagon collected at week 20 and glucagon collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 20.
| Intervention | pg/mL (Mean) |
|---|---|
| Placebo QD | 1.6 |
| Alogliptin 12.5 mg QD | 3.3 |
| Alogliptin 25 mg QD | 3.5 |
The change between the value of glucagon collected at week 16 and glucagon collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 16.
| Intervention | pg/mL (Mean) |
|---|---|
| Placebo QD | 2.4 |
| Alogliptin 12.5 mg QD | 3.3 |
| Alogliptin 25 mg QD | 3.4 |
The change between the value of glucagon collected at week 12 and glucagon collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 12.
| Intervention | pg/mL (Mean) |
|---|---|
| Placebo QD | -1.2 |
| Alogliptin 12.5 mg QD | 0.8 |
| Alogliptin 25 mg QD | 2.8 |
The change between the value of fasting proinsulin collected at week 8 and fasting proinsulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 8.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo QD | -3.9 |
| Alogliptin 12.5 mg QD | -3.1 |
| Alogliptin 25 mg QD | -1.4 |
The change between the value of C-peptide collected at week 20 and C-peptide collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 20.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo QD | -0.194 |
| Alogliptin 12.5 mg QD | -0.264 |
| Alogliptin 25 mg QD | -0.231 |
The change between the value of fasting proinsulin collected at week 4 and fasting proinsulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 4.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo QD | 2.9 |
| Alogliptin 12.5 mg QD | -4.7 |
| Alogliptin 25 mg QD | -10.4 |
The change between the value of fasting proinsulin collected at week 26 or final visit and fasting proinsulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo QD | -2.1 |
| Alogliptin 12.5 mg QD | -6.1 |
| Alogliptin 25 mg QD | -7.4 |
The change between the value of fasting proinsulin collected at week 20 and fasting proinsulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 20.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo QD | -0.8 |
| Alogliptin 12.5 mg QD | -6.0 |
| Alogliptin 25 mg QD | -6.3 |
The change between the value of fasting proinsulin collected at week 16 and fasting proinsulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 16.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo QD | -0.6 |
| Alogliptin 12.5 mg QD | -4.5 |
| Alogliptin 25 mg QD | -6.6 |
The change between the value of fasting proinsulin collected at week 12 and fasting proinsulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 12.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo QD | -2.8 |
| Alogliptin 12.5 mg QD | -3.2 |
| Alogliptin 25 mg QD | -8.5 |
The change between the value of fasting plasma glucose collected at week 8 and fasting plasma glucose collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 8.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | 2.5 |
| Alogliptin 12.5 mg QD | -14.3 |
| Alogliptin 25 mg QD | -19.8 |
The change between the value of fasting plasma glucose collected at week 4 and fasting plasma glucose collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 4.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | 2.8 |
| Alogliptin 12.5 mg QD | -15.6 |
| Alogliptin 25 mg QD | -21.6 |
The change between the value of fasting plasma glucose collected at week 26 or final visit and fasting plasma glucose collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | 11.3 |
| Alogliptin 12.5 mg QD | -10.3 |
| Alogliptin 25 mg QD | -16.4 |
The change between the value of fasting plasma glucose collected at week 20 and fasting plasma glucose collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 20.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | 7.0 |
| Alogliptin 12.5 mg QD | -12.3 |
| Alogliptin 25 mg QD | -17.3 |
The change between the value of fasting plasma glucose collected at week 2 and fasting plasma glucose collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 2.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | 3.8 |
| Alogliptin 12.5 mg QD | -14.6 |
| Alogliptin 25 mg QD | -17.6 |
The change between the value of fasting plasma glucose collected at week 16 and fasting plasma glucose collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 16.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | 5.2 |
| Alogliptin 12.5 mg QD | -14.6 |
| Alogliptin 25 mg QD | -18.2 |
The change between the value of fasting plasma glucose collected at week 12 and fasting plasma glucose collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | 1.2 |
| Alogliptin 12.5 mg QD | -15.3 |
| Alogliptin 25 mg QD | -20.0 |
The change between the value of fasting plasma glucose collected at final visit or week 1 and fasting plasma glucose collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 1.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | 4.6 |
| Alogliptin 12.5 mg QD | -8.6 |
| Alogliptin 25 mg QD | -14.0 |
The change between the value of C-peptide collected at week 4 and C-peptide collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 4.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo QD | 0.242 |
| Alogliptin 12.5 mg QD | 0.026 |
| Alogliptin 25 mg QD | 0.088 |
The change between the value of C-peptide collected at week 26 or final visit and C-peptide collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo QD | -0.282 |
| Alogliptin 12.5 mg QD | -0.360 |
| Alogliptin 25 mg QD | -0.279 |
The change between the value of C-peptide collected at week 16 and C-peptide collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 16.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo QD | -0.030 |
| Alogliptin 12.5 mg QD | -0.060 |
| Alogliptin 25 mg QD | -0.127 |
The change between the value of C-peptide collected at week 12 and C-peptide collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 12.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo QD | -0.104 |
| Alogliptin 12.5 mg QD | 0.064 |
| Alogliptin 25 mg QD | -0.091 |
The change between Body Weight measured at week 8 and Body Weight measured at baseline. (NCT00286455)
Timeframe: Baseline and Week 8.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo QD | -0.36 |
| Alogliptin 12.5 mg QD | 0.01 |
| Alogliptin 25 mg QD | -0.03 |
The change between Body Weight measured at week 26 or final visit and Body Weight measured at baseline. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo QD | 0.18 |
| Alogliptin 12.5 mg QD | -0.09 |
| Alogliptin 25 mg QD | -0.22 |
The change between Body Weight measured at week 20 and Body Weight measured at baseline. (NCT00286455)
Timeframe: Baseline and Week 20.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo QD | -0.17 |
| Alogliptin 12.5 mg QD | -0.18 |
| Alogliptin 25 mg QD | -0.17 |
The change between Body Weight measured at week 12 and Body Weight measured at baseline. (NCT00286455)
Timeframe: Baseline and Week 12.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo QD | -0.25 |
| Alogliptin 12.5 mg QD | -0.37 |
| Alogliptin 25 mg QD | 0.05 |
The change between the value of C-peptide collected at week 8 and C-peptide collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 8.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo QD | -0.014 |
| Alogliptin 12.5 mg QD | 0.070 |
| Alogliptin 25 mg QD | 0.269 |
The number of participants with a fasting plasma glucose value greater than or equal to 200 mg per dL at any measurement time point during the 26 week study. (NCT00286455)
Timeframe: 26 Weeks.
| Intervention | participants (Number) |
|---|---|
| Placebo QD | 30 |
| Alogliptin 12.5 mg QD | 44 |
| Alogliptin 25 mg QD | 33 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 2.0% during the 26 week study. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo QD | 1 |
| Alogliptin 12.5 mg QD | 3 |
| Alogliptin 25 mg QD | 6 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 1.5% during the 26 week study. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo QD | 3 |
| Alogliptin 12.5 mg QD | 11 |
| Alogliptin 25 mg QD | 16 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 1.0% during the 26 week study. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo QD | 7 |
| Alogliptin 12.5 mg QD | 38 |
| Alogliptin 25 mg QD | 39 |
The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 7.5% during the 26 week study. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo QD | 25 |
| Alogliptin 12.5 mg QD | 81 |
| Alogliptin 25 mg QD | 88 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 0.5% during the 26 week study. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo QD | 19 |
| Alogliptin 12.5 mg QD | 67 |
| Alogliptin 25 mg QD | 72 |
The change between the value of insulin collected at week 26 and insulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | ϻIU/mL (Least Squares Mean) |
|---|---|
| Placebo QD | -1.17 |
| Alogliptin 12.5 mg QD | -0.92 |
| Alogliptin 25 mg QD | -1.08 |
The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 7.0% during the 26 week study. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo QD | 15 |
| Alogliptin 12.5 mg QD | 63 |
| Alogliptin 25 mg QD | 58 |
The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 6.5% during the 26 week study. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo QD | 7 |
| Alogliptin 12.5 mg QD | 23 |
| Alogliptin 25 mg QD | 27 |
The number of participants requiring rescue for failing to achieve pre-specified glycemic targets during the 26 week study. (NCT00286455)
Timeframe: 26 Weeks.
| Intervention | participants (Number) |
|---|---|
| Placebo QD | 19 |
| Alogliptin 12.5 mg QD | 13 |
| Alogliptin 25 mg QD | 10 |
The change between the ratio value of proinsulin and insulin collected at week 8 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 8.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo QD | 0.014 |
| Alogliptin 12.5 mg QD | -0.054 |
| Alogliptin 25 mg QD | -0.038 |
The change between the ratio value of proinsulin and insulin collected at week 4 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 4.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo QD | 0.008 |
| Alogliptin 12.5 mg QD | -0.043 |
| Alogliptin 25 mg QD | -0.063 |
The change between the ratio value of proinsulin and insulin collected at week 26 or final visit and the ratio value of proinsulin and insulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 26.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo QD | 0.046 |
| Alogliptin 12.5 mg QD | -0.040 |
| Alogliptin 25 mg QD | -0.038 |
The change between the ratio value of proinsulin and insulin collected at week 20 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286455)
Timeframe: Baseline and Week 20.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo QD | 0.119 |
| Alogliptin 12.5 mg QD | -0.043 |
| Alogliptin 25 mg QD | -0.040 |
The change between the value of fasting proinsulin collected at week 16 and fasting proinsulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 16.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -1.8 |
| Alogliptin 12.5 mg QD | -1.5 |
| Alogliptin 25 mg QD | -1.1 |
The change between the value of fasting proinsulin collected at week 12 and fasting proinsulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 12.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -0.5 |
| Alogliptin 12.5 mg QD | -0.7 |
| Alogliptin 25 mg QD | -0.7 |
The change between the value of fasting plasma glucose collected at week 8 and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 8.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -3.2 |
| Alogliptin 12.5 mg QD | -19.9 |
| Alogliptin 25 mg QD | -18.6 |
The change between the value of fasting plasma glucose collected at week 4 and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 4.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -3.7 |
| Alogliptin 12.5 mg QD | -14.6 |
| Alogliptin 25 mg QD | -21.1 |
The change between the value of fasting plasma glucose collected at week 26 or final visit and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 26.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 2.2 |
| Alogliptin 12.5 mg QD | -4.7 |
| Alogliptin 25 mg QD | -8.4 |
The change between the value of fasting plasma glucose collected at week 20 and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 20.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -0.4 |
| Alogliptin 12.5 mg QD | -9.3 |
| Alogliptin 25 mg QD | -13.6 |
The change between the value of fasting plasma glucose collected at week 2 and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 2.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -1.8 |
| Alogliptin 12.5 mg QD | -16.7 |
| Alogliptin 25 mg QD | -21.8 |
The change between the value of fasting plasma glucose collected at week 16 and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 16.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -7.1 |
| Alogliptin 12.5 mg QD | -9.0 |
| Alogliptin 25 mg QD | -13.0 |
The change between the value of fasting plasma glucose collected at week 12 and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -3.4 |
| Alogliptin 12.5 mg QD | -13.5 |
| Alogliptin 25 mg QD | -15.0 |
The change between the value of fasting plasma glucose collected at final visit or week 1 and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 1.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 0.3 |
| Alogliptin 12.5 mg QD | -11.8 |
| Alogliptin 25 mg QD | -19.0 |
The change between the value of C-peptide collected at week 8 and C-peptide collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 8.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.176 |
| Alogliptin 12.5 mg QD | 0.092 |
| Alogliptin 25 mg QD | 0.173 |
The change between the value of C-peptide collected at week 4 and C-peptide collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 4.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.041 |
| Alogliptin 12.5 mg QD | 0.122 |
| Alogliptin 25 mg QD | 0.136 |
The change between the value of insulin collected at week 12 and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 12.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.02 |
| Alogliptin 12.5 mg QD | 1.33 |
| Alogliptin 25 mg QD | 1.00 |
The change between the value of insulin collected at week 16 and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 16.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Placebo | -1.21 |
| Alogliptin 12.5 mg QD | 1.74 |
| Alogliptin 25 mg QD | 0.51 |
The change between the value of insulin collected at week 20 and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 20.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.07 |
| Alogliptin 12.5 mg QD | 1.18 |
| Alogliptin 25 mg QD | 0.93 |
The change between the value of insulin collected at week 26 and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 26.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Placebo | -1.89 |
| Alogliptin 12.5 mg QD | -0.85 |
| Alogliptin 25 mg QD | 0.14 |
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 8 and Glycosylated Hemoglobin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 8.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -0.18 |
| Alogliptin 12.5 mg QD | -0.57 |
| Alogliptin 25 mg QD | -0.65 |
The change between the ratio value of proinsulin and insulin collected at week 12 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 12.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | -0.002 |
| Alogliptin 12.5 mg QD | -0.030 |
| Alogliptin 25 mg QD | -0.040 |
The change between Body Weight measured at week 12 and Body Weight measured at baseline. (NCT00286468)
Timeframe: Baseline and Week 12.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | -0.12 |
| Alogliptin 12.5 mg QD | 0.58 |
| Alogliptin 25 mg QD | 0.40 |
The change between Body Weight measured at week 20 and Body Weight measured at baseline. (NCT00286468)
Timeframe: Baseline and Week 20.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | -0.30 |
| Alogliptin 12.5 mg QD | 0.79 |
| Alogliptin 25 mg QD | 0.61 |
The change between Body Weight measured at week 26 or final visit and Body Weight measured at baseline. (NCT00286468)
Timeframe: Baseline and Week 26.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | -0.20 |
| Alogliptin 12.5 mg QD | 0.60 |
| Alogliptin 25 mg QD | 0.68 |
The change between Body Weight measured at week 8 and Body Weight measured at baseline. (NCT00286468)
Timeframe: Baseline and Week 8.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | -0.27 |
| Alogliptin 12.5 mg QD | 0.47 |
| Alogliptin 25 mg QD | 0.33 |
The change between the value of C-peptide collected at week 12 and C-peptide collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 12.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.020 |
| Alogliptin 12.5 mg QD | 0.162 |
| Alogliptin 25 mg QD | 0.206 |
The change between the value of insulin collected at week 4 and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 4.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.62 |
| Alogliptin 12.5 mg QD | 0.64 |
| Alogliptin 25 mg QD | 0.89 |
The change between the value of C-peptide collected at week 16 and C-peptide collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 16.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.007 |
| Alogliptin 12.5 mg QD | 0.222 |
| Alogliptin 25 mg QD | 0.153 |
The change between the value of C-peptide collected at week 20 and C-peptide collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 20.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.016 |
| Alogliptin 12.5 mg QD | -0.001 |
| Alogliptin 25 mg QD | 0.122 |
The change between the ratio value of proinsulin and insulin collected at week 26 or final visit and the ratio value of proinsulin and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 26.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | -0.008 |
| Alogliptin 12.5 mg QD | -0.034 |
| Alogliptin 25 mg QD | -0.034 |
The change between the value of C-peptide collected at week 26 or final visit and C-peptide collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 26.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.215 |
| Alogliptin 12.5 mg QD | -0.140 |
| Alogliptin 25 mg QD | -0.153 |
The change between the ratio value of proinsulin and insulin collected at week 16 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 16.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | 0.003 |
| Alogliptin 12.5 mg QD | -0.037 |
| Alogliptin 25 mg QD | -0.041 |
The change between the ratio value of proinsulin and insulin collected at week 20 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 20.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | -0.005 |
| Alogliptin 12.5 mg QD | -0.035 |
| Alogliptin 25 mg QD | -0.036 |
The change between the ratio value of proinsulin and insulin collected at week 4 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 4.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | -0.008 |
| Alogliptin 12.5 mg QD | -0.064 |
| Alogliptin 25 mg QD | -0.043 |
The change between the ratio value of proinsulin and insulin collected at week 8 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 8.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | -0.009 |
| Alogliptin 12.5 mg QD | -0.052 |
| Alogliptin 25 mg QD | -0.045 |
The number of participants requiring rescue for failing to achieve pre-specified glycemic targets during the 26 week study. (NCT00286468)
Timeframe: 26 Weeks.
| Intervention | participants (Number) |
|---|---|
| Placebo | 28 |
| Alogliptin 12.5 mg QD | 30 |
| Alogliptin 25 mg QD | 31 |
The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 6.5% during the 26 week study. (NCT00286468)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 7 |
| Alogliptin 12.5 mg QD | 19 |
| Alogliptin 25 mg QD | 28 |
The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 7.0% during the 26 week study. (NCT00286468)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 18 |
| Alogliptin 12.5 mg QD | 60 |
| Alogliptin 25 mg QD | 69 |
The change between the value of insulin collected at week 8 and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 8.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.81 |
| Alogliptin 12.5 mg QD | -0.62 |
| Alogliptin 25 mg QD | 0.38 |
The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 7.5% during the 26 week study. (NCT00286468)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 33 |
| Alogliptin 12.5 mg QD | 94 |
| Alogliptin 25 mg QD | 112 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 0.5% during the 26 week study. (NCT00286468)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 26 |
| Alogliptin 12.5 mg QD | 96 |
| Alogliptin 25 mg QD | 100 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 1.0% during the 26 week study. (NCT00286468)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 13 |
| Alogliptin 12.5 mg QD | 38 |
| Alogliptin 25 mg QD | 59 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 1.5% during the 26 week study. (NCT00286468)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 7 |
| Alogliptin 12.5 mg QD | 13 |
| Alogliptin 25 mg QD | 24 |
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 4 and Glycosylated Hemoglobin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 4.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -0.18 |
| Alogliptin 12.5 mg QD | -0.40 |
| Alogliptin 25 mg QD | -0.46 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 2.0% during the 26 week study. (NCT00286468)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 4 |
| Alogliptin 12.5 mg QD | 5 |
| Alogliptin 25 mg QD | 12 |
The number of participants with a fasting plasma glucose value greater than or equal to 200 mg per dL during the 26 week study. (NCT00286468)
Timeframe: 26 Weeks.
| Intervention | participants (Number) |
|---|---|
| Placebo | 53 |
| Alogliptin 12.5 mg QD | 94 |
| Alogliptin 25 mg QD | 79 |
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 20 and Glycosylated Hemoglobin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 20.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -0.08 |
| Alogliptin 12.5 mg QD | -0.43 |
| Alogliptin 25 mg QD | -0.60 |
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 16 and Glycosylated Hemoglobin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 16.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -0.16 |
| Alogliptin 12.5 mg QD | -0.53 |
| Alogliptin 25 mg QD | -0.66 |
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 12 and Glycosylated Hemoglobin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -0.17 |
| Alogliptin 12.5 mg QD | -0.58 |
| Alogliptin 25 mg QD | -0.69 |
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 26 or final visit and glycosylated hemoglobin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 26.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 0.01 |
| Alogliptin 12.5 mg QD | -0.38 |
| Alogliptin 25 mg QD | -0.52 |
The change between the value of fasting proinsulin collected at week 8 and fasting proinsulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 8.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -4.2 |
| Alogliptin 12.5 mg QD | -4.5 |
| Alogliptin 25 mg QD | -0.9 |
The change between the value of fasting proinsulin collected at week 4 and fasting proinsulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 4.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -3.0 |
| Alogliptin 12.5 mg QD | -2.6 |
| Alogliptin 25 mg QD | 0.7 |
The change between the value of fasting proinsulin collected at week 26 or final visit and fasting proinsulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 26.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -2.0 |
| Alogliptin 12.5 mg QD | -3.9 |
| Alogliptin 25 mg QD | -2.1 |
The change between the value of fasting proinsulin collected at week 20 and fasting proinsulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 20.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -2.5 |
| Alogliptin 12.5 mg QD | -2.1 |
| Alogliptin 25 mg QD | 0.0 |
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 12 and Glycosylated Hemoglobin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 12.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.23 |
| Alogliptin 12.5 mg QD | -0.70 |
| Alogliptin 25 mg QD | -0.82 |
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 16 and Glycosylated Hemoglobin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 16.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.26 |
| Alogliptin 12.5 mg QD | -0.70 |
| Alogliptin 25 mg QD | -0.84 |
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 20 and Glycosylated Hemoglobin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 20.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.27 |
| Alogliptin 12.5 mg QD | -0.68 |
| Alogliptin 25 mg QD | -0.82 |
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 4 and Glycosylated Hemoglobin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 4.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.14 |
| Alogliptin 12.5 mg QD | -0.40 |
| Alogliptin 25 mg QD | -0.45 |
The change between the value of fasting plasma glucose collected at week 4 and fasting plasma glucose collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 4.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -3.1 |
| Alogliptin 12.5 mg QD | -23.7 |
| Alogliptin 25 mg QD | -26.0 |
The change between the value of insulin collected at week 12 and insulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 12.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Placebo | 0.00 |
| Alogliptin 12.5 mg QD | 0.43 |
| Alogliptin 25 mg QD | -0.58 |
The change between the value of insulin collected at week 16 and insulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 16.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.85 |
| Alogliptin 12.5 mg QD | -0.10 |
| Alogliptin 25 mg QD | -0.16 |
The change between Body Weight measured at week 12 and Body Weight measured at baseline. (NCT00286494)
Timeframe: Baseline and Week 12.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | 0.60 |
| Alogliptin 12.5 mg QD | 0.74 |
| Alogliptin 25 mg QD | 0.64 |
The change between Body Weight measured at week 20 and Body Weight measured at baseline. (NCT00286494)
Timeframe: Baseline and Week 20.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | 0.94 |
| Alogliptin 12.5 mg QD | 1.14 |
| Alogliptin 25 mg QD | 0.93 |
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 8 and Glycosylated Hemoglobin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 8.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.18 |
| Alogliptin 12.5 mg QD | -0.60 |
| Alogliptin 25 mg QD | -0.73 |
The change between Body Weight measured at week 26 or final visit and Body Weight measured at baseline. (NCT00286494)
Timeframe: Baseline and Week 26.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | 1.04 |
| Alogliptin 12.5 mg QD | 1.46 |
| Alogliptin 25 mg QD | 1.09 |
The change between Body Weight measured at week 8 and Body Weight measured at baseline. (NCT00286494)
Timeframe: Baseline and Week 8.
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | 0.36 |
| Alogliptin 12.5 mg QD | 0.46 |
| Alogliptin 25 mg QD | 0.39 |
The change between the value of C-peptide collected at week 12 and C-peptide collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 12.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.017 |
| Alogliptin 12.5 mg QD | -0.085 |
| Alogliptin 25 mg QD | -0.067 |
The change between the value of C-peptide collected at week 16 and C-peptide collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 16.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.290 |
| Alogliptin 12.5 mg QD | -0.071 |
| Alogliptin 25 mg QD | -0.052 |
The change between the value of C-peptide collected at week 20 and C-peptide collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 20.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.255 |
| Alogliptin 12.5 mg QD | -0.228 |
| Alogliptin 25 mg QD | -0.123 |
The change between the value of C-peptide collected at week 26 or final visit and C-peptide collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 26.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.356 |
| Alogliptin 12.5 mg QD | -0.233 |
| Alogliptin 25 mg QD | -0.133 |
The change between the value of C-peptide collected at week 4 and C-peptide collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 4.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.144 |
| Alogliptin 12.5 mg QD | -0.156 |
| Alogliptin 25 mg QD | -0.088 |
The change between the value of C-peptide collected at week 8 and C-peptide collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 8.
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.111 |
| Alogliptin 12.5 mg QD | -0.117 |
| Alogliptin 25 mg QD | 0.023 |
The change between the value of fasting plasma glucose collected at final visit or week 1 and fasting plasma glucose collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 1.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -2.7 |
| Alogliptin 12.5 mg QD | -14.2 |
| Alogliptin 25 mg QD | -18.2 |
The change between the value of fasting plasma glucose collected at week 12 and fasting plasma glucose collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -9.9 |
| Alogliptin 12.5 mg QD | -20.4 |
| Alogliptin 25 mg QD | -26.2 |
The change between the value of fasting plasma glucose collected at week 16 and fasting plasma glucose collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 16.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -8.3 |
| Alogliptin 12.5 mg QD | -18.3 |
| Alogliptin 25 mg QD | -22.8 |
The change between the value of fasting plasma glucose collected at week 2 and fasting plasma glucose collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 2.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -1.8 |
| Alogliptin 12.5 mg QD | -21.0 |
| Alogliptin 25 mg QD | -21.2 |
The change between the value of fasting plasma glucose collected at week 20 and fasting plasma glucose collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 20.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -6.4 |
| Alogliptin 12.5 mg QD | -21.9 |
| Alogliptin 25 mg QD | -21.6 |
The number of participants with a fasting plasma glucose value greater than or equal to 200 mg per dL during the 26 week study. (NCT00286494)
Timeframe: 26 Weeks.
| Intervention | participants (Number) |
|---|---|
| Placebo | 43 |
| Alogliptin 12.5 mg QD | 49 |
| Alogliptin 25 mg QD | 43 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 2.0% during the 26 week study. (NCT00286494)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 3 |
| Alogliptin 12.5 mg QD | 12 |
| Alogliptin 25 mg QD | 14 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 1.5% during the 26 week study. (NCT00286494)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 5 |
| Alogliptin 12.5 mg QD | 32 |
| Alogliptin 25 mg QD | 37 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 1.0% during the 26 week study. (NCT00286494)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 12 |
| Alogliptin 12.5 mg QD | 64 |
| Alogliptin 25 mg QD | 73 |
The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 0.5% during the 26 week study. (NCT00286494)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 26 |
| Alogliptin 12.5 mg QD | 118 |
| Alogliptin 25 mg QD | 128 |
The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 7.5% during the 26 week study. (NCT00286494)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 47 |
| Alogliptin 12.5 mg QD | 127 |
| Alogliptin 25 mg QD | 141 |
The number of participants with a value for the percentage of glycosylated hemoglobin less (the percentage of hemoglobin that is bound to glucose) than or equal to 7.0% during the 26 week study. (NCT00286494)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 33 |
| Alogliptin 12.5 mg QD | 87 |
| Alogliptin 25 mg QD | 98 |
The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 6.5% during the 26 week study. (NCT00286494)
Timeframe: Baseline and Week 26.
| Intervention | participants (Number) |
|---|---|
| Placebo | 5 |
| Alogliptin 12.5 mg QD | 34 |
| Alogliptin 25 mg QD | 41 |
The number of participants requiring rescue for failing to achieve pre-specified glycemic targets during the 26 week study. (NCT00286494)
Timeframe: 26 Weeks.
| Intervention | participants (Number) |
|---|---|
| Placebo | 12 |
| Alogliptin 12.5 mg QD | 19 |
| Alogliptin 25 mg QD | 18 |
The change between the ratio value of proinsulin and insulin collected at week 8 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 8.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | -0.006 |
| Alogliptin 12.5 mg QD | -0.055 |
| Alogliptin 25 mg QD | -0.057 |
The change between the ratio value of proinsulin and insulin collected at week 4 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 4.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | 0.006 |
| Alogliptin 12.5 mg QD | -0.051 |
| Alogliptin 25 mg QD | -0.053 |
The change between the ratio value of proinsulin and insulin collected at week 26 or final visit and the ratio value of proinsulin and insulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 26.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | 0.015 |
| Alogliptin 12.5 mg QD | -0.035 |
| Alogliptin 25 mg QD | -0.022 |
The change between the ratio value of proinsulin and insulin collected at week 20 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 20.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | 0.012 |
| Alogliptin 12.5 mg QD | -0.047 |
| Alogliptin 25 mg QD | -0.040 |
The change between the ratio value of proinsulin and insulin collected at week 16 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 16.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | -0.015 |
| Alogliptin 12.5 mg QD | -0.042 |
| Alogliptin 25 mg QD | -0.045 |
The change between the ratio value of proinsulin and insulin collected at week 12 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 12.
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | 0.017 |
| Alogliptin 12.5 mg QD | -0.029 |
| Alogliptin 25 mg QD | -0.040 |
The change between the value of insulin collected at week 8 and insulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 8.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.17 |
| Alogliptin 12.5 mg QD | -0.82 |
| Alogliptin 25 mg QD | 0.21 |
The change between the value of insulin collected at week 4 and insulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 4.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.09 |
| Alogliptin 12.5 mg QD | -1.08 |
| Alogliptin 25 mg QD | -0.97 |
The change between the value of insulin collected at week 26 and insulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 26.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.81 |
| Alogliptin 12.5 mg QD | -0.19 |
| Alogliptin 25 mg QD | 0.00 |
The change between the value of insulin collected at week 20 and insulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 20.
| Intervention | mcIU/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.19 |
| Alogliptin 12.5 mg QD | -0.40 |
| Alogliptin 25 mg QD | -0.33 |
The change between the value of fasting plasma glucose collected at week 26 or final visit and fasting plasma glucose collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 26.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -5.7 |
| Alogliptin 12.5 mg QD | -19.7 |
| Alogliptin 25 mg QD | -19.9 |
The change between the value of fasting plasma glucose collected at week 8 and fasting plasma glucose collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 8.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -6.1 |
| Alogliptin 12.5 mg QD | -22.6 |
| Alogliptin 25 mg QD | -27.1 |
The change between the value of fasting proinsulin collected at week 12 and fasting proinsulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 12.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | 0.6 |
| Alogliptin 12.5 mg QD | -3.6 |
| Alogliptin 25 mg QD | -3.8 |
The change between the value of fasting proinsulin collected at week 16 and fasting proinsulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 16.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -3.1 |
| Alogliptin 12.5 mg QD | -3.5 |
| Alogliptin 25 mg QD | -3.1 |
The change between the value of fasting proinsulin collected at week 20 and fasting proinsulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 20.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -0.9 |
| Alogliptin 12.5 mg QD | -6.2 |
| Alogliptin 25 mg QD | -3.9 |
The change between the value of fasting proinsulin collected at week 26 or final visit and fasting proinsulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 26.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -1.0 |
| Alogliptin 12.5 mg QD | -5.1 |
| Alogliptin 25 mg QD | -1.7 |
The change between the value of fasting proinsulin collected at week 8 and fasting proinsulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 8.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -2.3 |
| Alogliptin 12.5 mg QD | -6.5 |
| Alogliptin 25 mg QD | -3.7 |
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 26 or final visit and glycosylated hemoglobin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 26.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.19 |
| Alogliptin 12.5 mg QD | -0.66 |
| Alogliptin 25 mg QD | -0.80 |
The change between the value of fasting proinsulin collected at week 4 and fasting proinsulin collected at baseline. (NCT00286494)
Timeframe: Baseline and Week 4.
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -0.7 |
| Alogliptin 12.5 mg QD | -7.0 |
| Alogliptin 25 mg QD | -5.6 |
"Marked Hyperglycemia is defined as fasting plasma glucose greater than or equal to 200 mg/dL (≥11.10 mmol/L).~The Month 42 to Month 45 interval includes all marked hyperglycemic episodes occurring on or after Day 1247 (a 203-day visit window)." (NCT00306384)
Timeframe: Randomization up to 4 years.
| Intervention | percentage of participants (Number) | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Day 1 to | Week 2 to | Week 4 to | Week 8 to | Week 12 to | Month 6 to | Month 9 to | Month 12 to | Month 15 to | Month 18 to | Month 21 to | Month 24 to | Month 27 to | Month 30 to | Month 33 to | Month 36 to | Month 39 to | Month 42 to Month 45 (n=889, 921, 261) | Overall (n= 1389, 1392, 518) | | |
| Alogliptin 12.5 mg | 9.1 | 11.5 | 9.2 | 11.5 | 12.0 | 12.8 | 11.4 | 13.1 | 12.7 | 11.7 | 11.2 | 11.6 | 12.6 | 11.6 | 11.5 | 13.2 | 13.7 | 25.5 | 49.7 |
| Alogliptin 25 mg | 8.0 | 10.2 | 11.0 | 10.8 | 11.6 | 10.7 | 12.9 | 13.0 | 13.8 | 11.6 | 11.5 | 12.3 | 11.8 | 11.7 | 12.3 | 12.5 | 13.1 | 23.9 | 50.7 |
| Rescued: Alogliptin 25 mg | 55.5 | 45.9 | 46.1 | 41.0 | 39.4 | 36.8 | 32.5 | 29.3 | 27.8 | 26.8 | 26.3 | 24.9 | 24.7 | 19.7 | 23.5 | 21.0 | 19.5 | 39.1 | 87.6 |
The change from Baseline in glycosylated hemoglobin (HbA1c; the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) during the study. Endpoint was defined as the last postbaseline observation collected within 7 days after the last dose of open-label study drug. (NCT00306384)
Timeframe: Baseline and Month 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42 and 45.
| Intervention | percent glycosylated hemoglobin (Mean) | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (n=1362, 1359, 501) | Week 12 change from Baseline (n=1290, 1286, 463) | Month 6 change from Baseline (n= 1236, 1252, 433) | Month 9 change from Baseline (n=1217, 1231, 413) | Month 12 change from Baseline (1175, 1182, 388) | Month 15 change from Baseline (n=1119, 1133, 374) | Month 18 change from Baseline (n=1111, 1095, 350) | Month 21 change from Baseline (n=1061, 1071, 338) | Month 24 change from Baseline (n=1027, 1039, 320) | Month 27 change from Baseline (n=991, 1002, 300) | Month 30 change from Baseline (n=944, 955, 281) | Month 33 change from Baseline (n=923, 941, 276) | Month 36 change from Baseline (n=882, 931, 274) | Month 39 change from Baseline (n=886, 913, 259) | Month 42 change from Baseline (n=854, 891, 252) | Month 45 change from Baseline (n=866, 902, 253) | Endpoint change from Baseline (n=1362, 1359, 501) | |
| Alogliptin 12.5 mg | 7.21 | 0.18 | 0.31 | 0.34 | 0.41 | 0.47 | 0.50 | 0.52 | 0.53 | 0.58 | 0.57 | 0.55 | 0.54 | 0.56 | 0.59 | 0.61 | 1.63 |
| Alogliptin 25 mg | 7.22 | 0.14 | 0.26 | 0.33 | 0.41 | 0.48 | 0.50 | 0.51 | 0.58 | 0.58 | 0.57 | 0.57 | 0.55 | 0.56 | 0.54 | 0.56 | 0.61 |
| Rescued: Alogliptin 25 mg | 9.30 | -0.52 | -0.73 | -0.78 | -0.78 | -0.75 | -0.70 | -0.75 | -0.69 | -0.71 | -0.78 | -0.73 | -0.80 | -0.73 | -0.78 | -0.70 | -0.42 |
"Proinsulin is a precursor to insulin, and was measured as an indicator of pancreatic function. The change from Baseline in fasting proinsulin to the last post-baseline observation, collected within 7 days after the last dose of open-label study drug.~Note: A transcription error occurred in the reporting of 1 proinsulin value for a patient in the alogliptin 25 mg completed group, for whom a partial patient ID number was mistakenly entered as an end-of-treatment proinsulin level." (NCT00306384)
Timeframe: Baseline and Year 4
| Intervention | pmol/L (Mean) | |
|---|---|---|
| Baseline | Change from Baseline | |
| Alogliptin 12.5 mg | 26.1 | 4.1 |
| Alogliptin 25 mg | 25.4 | 39.7 |
| Rescued: Alogliptin 25 mg | 40.2 | -3.3 |
The change from Baseline in fasting insulin at the last post-baseline observation, collected within 7 days after the last dose of open-label study drug. (NCT00306384)
Timeframe: Baseline and Year 4
| Intervention | μIU/mL (Mean) | |
|---|---|---|
| Baseline | Change from Baseline | |
| Alogliptin 12.5 mg | 15.19 | 2.45 |
| Alogliptin 25 mg | 15.50 | 2.13 |
| Rescued: Alogliptin 25 mg | 18.64 | 5.62 |
The change from Baseline in fasting plasma glucose (FPG) at the last post-baseline observation, collected within 7 days after the last dose of open-label study drug. (NCT00306384)
Timeframe: Baseline and Year 4
| Intervention | mg/dL (Mean) | |
|---|---|---|
| Baseline | Change from Baseline | |
| Alogliptin 12.5 mg | 144.4 | 14.8 |
| Alogliptin 25 mg | 142.6 | 14.9 |
| Rescued: Alogliptin 25 mg | 215.3 | -26.4 |
C-peptide is a byproduct created when the hormone insulin is produced and is measured by a blood test. Change from Baseline to the last post-baseline observation, collected within 7 days after the last dose of open-label study drug. (NCT00306384)
Timeframe: Baseline and Year 4
| Intervention | ng/mL (Mean) | |
|---|---|---|
| Baseline | Change from Baseline | |
| Alogliptin 12.5 mg | 3.406 | -0.471 |
| Alogliptin 25 mg | 3.323 | -0.439 |
| Rescued: Alogliptin 25 mg | 3.572 | -0.641 |
Change from Baseline in body weight to the last post-baseline observation collected within 7 days after the last dose of open-label study drug. (NCT00306384)
Timeframe: Baseline and Year 4
| Intervention | kg (Mean) | |
|---|---|---|
| Baseline | Change from Baseline | |
| Alogliptin 12.5 mg | 86.12 | -0.64 |
| Alogliptin 25 mg | 86.61 | -0.61 |
| Rescued: Alogliptin 25 mg | 88.62 | 0.25 |
"Clinical response was defined based on the absolute value of HbA1c meeting one of two clinical targets at any post-baseline visit:~HbA1c ≤6.5%;~HbA1c ≤7.0%." (NCT00306384)
Timeframe: Weeks 2, 4, 8, 12, every 3 months up to 4 years, and 1 Day after final dose.
| Intervention | percentage of participants (Number) | |
|---|---|---|
| HbA1c ≤6.5% | HbA1c ≤7.0% | |
| Alogliptin 12.5 mg | 34.8 | 64.1 |
| Alogliptin 25 mg | 34.1 | 65.5 |
| Rescued: Alogliptin 25 mg | 11.0 | 27.1 |
Safety was assessed by physical examinations, clinical laboratory parameters, electrocardiogram (ECG) readings, vital sign measurements, oral temperature, and hypoglycemic events. Changes in laboratory values or ECG parameters were considered to be adverse events if they were judged to be clinically significant. A TEAE was any event that started on or after the first dose of open-label study drug and within 14 days after the last dose. (NCT00306384)
Timeframe: 4 years
| Intervention | percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Any treatment emergent adverse event (TEAE) | Study drug-related TEAE | TEAE leading to discontinuation | Treatment emergent serious AE | Study drug-related serious AE | Treatment-emergent deaths | |
| Alogliptin 12.5 mg | 87.2 | 25.6 | 7.0 | 16.7 | 2.6 | 1.4 |
| Alogliptin 25 mg | 87.1 | 22.7 | 6.1 | 16.3 | 2.1 | 1.0 |
| Rescued: Alogliptin 25 mg | 84.6 | 24.9 | 7.6 | 15.7 | 1.9 | 0.9 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline triglycerides as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 3.7 |
| Alogliptin 12.5 + Placebo | -1.1 |
| Alogliptin 25 + Placebo | -15.2 |
| Placebo + Pioglitazone 15 | -29.5 |
| Alogliptin 12.5 + Pioglitazone 15 | -37.7 |
| Alogliptin 25 + Pioglitazone 15 | -38.5 |
| Placebo + Pioglitazone 30 | -27.0 |
| Alogliptin 12.5 + Pioglitazone 30 | -37.3 |
| Alogliptin 25 + Pioglitazone 30 | -33.5 |
| Placebo + Pioglitazone 45 | -32.4 |
| Alogliptin 12.5 + Pioglitazone 45 | -49.3 |
| Alogliptin 25 + Pioglitazone 45 | -50.1 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline total cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 4.4 |
| Alogliptin 12.5 + Placebo | 2.2 |
| Alogliptin 25 + Placebo | 0.9 |
| Placebo + Pioglitazone 15 | 5.8 |
| Alogliptin 12.5 + Pioglitazone 15 | 4.3 |
| Alogliptin 25 + Pioglitazone 15 | 3.5 |
| Placebo + Pioglitazone 30 | 8.8 |
| Alogliptin 12.5 + Pioglitazone 30 | 2.8 |
| Alogliptin 25 + Pioglitazone 30 | 3.2 |
| Placebo + Pioglitazone 45 | 9.5 |
| Alogliptin 12.5 + Pioglitazone 45 | 6.0 |
| Alogliptin 25 + Pioglitazone 45 | 5.1 |
"The ratio of proinsulin to insulin was calculated as proinsulin (pmol/L) / insulin (μIU/mL).~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline proinsulin/insulin ratio as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | -0.007 |
| Alogliptin 12.5 + Placebo | -0.001 |
| Alogliptin 25 + Placebo | -0.064 |
| Placebo + Pioglitazone 15 | -0.038 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.071 |
| Alogliptin 25 + Pioglitazone 15 | -0.063 |
| Placebo + Pioglitazone 30 | -0.030 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.081 |
| Alogliptin 25 + Pioglitazone 30 | -0.072 |
| Placebo + Pioglitazone 45 | -0.014 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.109 |
| Alogliptin 25 + Pioglitazone 45 | -0.092 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline PAI-1 as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -3.00 |
| Alogliptin 12.5 + Placebo | 0.57 |
| Alogliptin 25 + Placebo | -3.29 |
| Placebo + Pioglitazone 15 | -5.43 |
| Alogliptin 12.5 + Pioglitazone 15 | -4.75 |
| Alogliptin 25 + Pioglitazone 15 | -9.62 |
| Placebo + Pioglitazone 30 | -5.24 |
| Alogliptin 12.5 + Pioglitazone 30 | 1.89 |
| Alogliptin 25 + Pioglitazone 30 | -6.66 |
| Placebo + Pioglitazone 45 | -3.02 |
| Alogliptin 12.5 + Pioglitazone 45 | -5.22 |
| Alogliptin 25 + Pioglitazone 45 | -11.48 |
"NMR lipid fractionation was used to assess the change from Baseline in total triglyceride levels at Week 26.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR total triglycerides as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 12.4 |
| Alogliptin 12.5 + Placebo | 7.3 |
| Alogliptin 25 + Placebo | -6.8 |
| Placebo + Pioglitazone 15 | -18.9 |
| Alogliptin 12.5 + Pioglitazone 15 | -20.4 |
| Alogliptin 25 + Pioglitazone 15 | -23.1 |
| Placebo + Pioglitazone 30 | -6.9 |
| Alogliptin 12.5 + Pioglitazone 30 | -23.5 |
| Alogliptin 25 + Pioglitazone 30 | -19.7 |
| Placebo + Pioglitazone 45 | -8.6 |
| Alogliptin 12.5 + Pioglitazone 45 | -32.1 |
| Alogliptin 25 + Pioglitazone 45 | -25.8 |
"The change from Baseline in mean VLDL particle size was assessed by NMR lipid fractionation.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline mean VLDL particle size as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | nm (Least Squares Mean) |
|---|---|
| Placebo | 0.26 |
| Alogliptin 12.5 + Placebo | 0.52 |
| Alogliptin 25 + Placebo | 0.35 |
| Placebo + Pioglitazone 15 | -2.99 |
| Alogliptin 12.5 + Pioglitazone 15 | -2.66 |
| Alogliptin 25 + Pioglitazone 15 | -2.36 |
| Placebo + Pioglitazone 30 | -2.88 |
| Alogliptin 12.5 + Pioglitazone 30 | -3.69 |
| Alogliptin 25 + Pioglitazone 30 | -3.30 |
| Placebo + Pioglitazone 45 | -1.60 |
| Alogliptin 12.5 + Pioglitazone 45 | -4.65 |
| Alogliptin 25 + Pioglitazone 45 | -4.12 |
"The change from Baseline in mean LDL particle size was assessed by NMR lipid fractionation.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline mean LDL particle size as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | nm (Least Squares Mean) |
|---|---|
| Placebo | -0.06 |
| Alogliptin 12.5 + Placebo | -0.01 |
| Alogliptin 25 + Placebo | 0.07 |
| Placebo + Pioglitazone 15 | 0.26 |
| Alogliptin 12.5 + Pioglitazone 15 | 0.38 |
| Alogliptin 25 + Pioglitazone 15 | 0.41 |
| Placebo + Pioglitazone 30 | 0.38 |
| Alogliptin 12.5 + Pioglitazone 30 | 0.48 |
| Alogliptin 25 + Pioglitazone 30 | 0.57 |
| Placebo + Pioglitazone 45 | 0.59 |
| Alogliptin 12.5 + Pioglitazone 45 | 0.55 |
| Alogliptin 25 + Pioglitazone 45 | 0.63 |
The change from Baseline in mean HDL particle size was assessed by NMR lipid fractionation. Least squares means are from are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline mean HDL particle size as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | nm (Least Squares Mean) |
|---|---|
| Placebo | 0.03 |
| Alogliptin 12.5 + Placebo | 0.00 |
| Alogliptin 25 + Placebo | 0.07 |
| Placebo + Pioglitazone 15 | 0.06 |
| Alogliptin 12.5 + Pioglitazone 15 | 0.06 |
| Alogliptin 25 + Pioglitazone 15 | 0.11 |
| Placebo + Pioglitazone 30 | 0.10 |
| Alogliptin 12.5 + Pioglitazone 30 | 0.15 |
| Alogliptin 25 + Pioglitazone 30 | 0.20 |
| Placebo + Pioglitazone 45 | 0.19 |
| Alogliptin 12.5 + Pioglitazone 45 | 0.16 |
| Alogliptin 25 + Pioglitazone 45 | 0.19 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline LDL cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 3.6 |
| Alogliptin 12.5 + Placebo | 2.8 |
| Alogliptin 25 + Placebo | 3.6 |
| Placebo + Pioglitazone 15 | 7.9 |
| Alogliptin 12.5 + Pioglitazone 15 | 3.7 |
| Alogliptin 25 + Pioglitazone 15 | 6.1 |
| Placebo + Pioglitazone 30 | 6.2 |
| Alogliptin 12.5 + Pioglitazone 30 | 2.9 |
| Alogliptin 25 + Pioglitazone 30 | 3.0 |
| Placebo + Pioglitazone 45 | 8.1 |
| Alogliptin 12.5 + Pioglitazone 45 | 9.1 |
| Alogliptin 25 + Pioglitazone 45 | 7.7 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline insulin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | µIU/mL (Least Squares Mean) |
|---|---|
| Placebo | 6.78 |
| Alogliptin 12.5 + Placebo | 1.33 |
| Alogliptin 25 + Placebo | 1.43 |
| Placebo + Pioglitazone 15 | -0.78 |
| Alogliptin 12.5 + Pioglitazone 15 | -3.05 |
| Alogliptin 25 + Pioglitazone 15 | -0.76 |
| Placebo + Pioglitazone 30 | -2.56 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.76 |
| Alogliptin 25 + Pioglitazone 30 | -1.42 |
| Placebo + Pioglitazone 45 | -1.88 |
| Alogliptin 12.5 + Pioglitazone 45 | -2.33 |
| Alogliptin 25 + Pioglitazone 45 | -2.79 |
"The change from Baseline in levels of IDL particles was assessed by NMR lipid fractionation.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR IDL particles as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | nmol/L (Least Squares Mean) |
|---|---|
| Placebo | 5.1 |
| Alogliptin 12.5 + Placebo | -7.3 |
| Alogliptin 25 + Placebo | -3.2 |
| Placebo + Pioglitazone 15 | 5.2 |
| Alogliptin 12.5 + Pioglitazone 15 | -2.4 |
| Alogliptin 25 + Pioglitazone 15 | 0.0 |
| Placebo + Pioglitazone 30 | 3.0 |
| Alogliptin 12.5 + Pioglitazone 30 | -5.0 |
| Alogliptin 25 + Pioglitazone 30 | -5.5 |
| Placebo + Pioglitazone 45 | 0.1 |
| Alogliptin 12.5 + Pioglitazone 45 | -5.0 |
| Alogliptin 25 + Pioglitazone 45 | 1.0 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline hsCRP as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | mg/L (Least Squares Mean) |
|---|---|
| Placebo | -0.0550 |
| Alogliptin 12.5 + Placebo | -0.6606 |
| Alogliptin 25 + Placebo | 0.2618 |
| Placebo + Pioglitazone 15 | 0.2375 |
| Alogliptin 12.5 + Pioglitazone 15 | -1.2490 |
| Alogliptin 25 + Pioglitazone 15 | -0.9438 |
| Placebo + Pioglitazone 30 | -1.0480 |
| Alogliptin 12.5 + Pioglitazone 30 | -1.1725 |
| Alogliptin 25 + Pioglitazone 30 | 0.1697 |
| Placebo + Pioglitazone 45 | -1.8562 |
| Alogliptin 12.5 + Pioglitazone 45 | -2.8933 |
| Alogliptin 25 + Pioglitazone 45 | -2.2191 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HDL cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 0.5 |
| Alogliptin 12.5 + Placebo | 0.6 |
| Alogliptin 25 + Placebo | 1.3 |
| Placebo + Pioglitazone 15 | 3.8 |
| Alogliptin 12.5 + Pioglitazone 15 | 4.2 |
| Alogliptin 25 + Pioglitazone 15 | 4.1 |
| Placebo + Pioglitazone 30 | 5.5 |
| Alogliptin 12.5 + Pioglitazone 30 | 6.0 |
| Alogliptin 25 + Pioglitazone 30 | 5.0 |
| Placebo + Pioglitazone 45 | 6.1 |
| Alogliptin 12.5 + Pioglitazone 45 | 6.2 |
| Alogliptin 25 + Pioglitazone 45 | 6.0 |
The change from Baseline to Week 26 in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound). (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | percentage of glycosylated hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.13 |
| Alogliptin 12.5 + Placebo | -0.64 |
| Alogliptin 25 + Placebo | -0.90 |
| Placebo + Pioglitazone 15 | -0.75 |
| Alogliptin 12.5 + Pioglitazone 15 | -1.34 |
| Alogliptin 25 + Pioglitazone 15 | -1.27 |
| Placebo + Pioglitazone 30 | -0.92 |
| Alogliptin 12.5 + Pioglitazone 30 | -1.39 |
| Alogliptin 25 + Pioglitazone 30 | -1.39 |
| Placebo + Pioglitazone 45 | -1.00 |
| Alogliptin 12.5 + Pioglitazone 45 | -1.55 |
| Alogliptin 25 + Pioglitazone 45 | -1.60 |
"The change from Baseline to Week 26 in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound).~The primary analysis compared the groupings (combinations of individual treatment groups) of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone (Pioglitazone Alone)." (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | percentage of glycosylated hemoglobin (Least Squares Mean) |
|---|---|
| Pioglitazone Alone | -0.89 |
| Alogliptin 12.5 + Pioglitazone | -1.43 |
| Alogliptin 25 + Pioglitazone | -1.42 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline free fatty acid as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | mmol/L (Least Squares Mean) |
|---|---|
| Placebo | -0.0387 |
| Alogliptin 12.5 + Placebo | -0.0427 |
| Alogliptin 25 + Placebo | -0.0386 |
| Placebo + Pioglitazone 15 | -0.0561 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.0752 |
| Alogliptin 25 + Pioglitazone 15 | -0.0972 |
| Placebo + Pioglitazone 30 | -0.0737 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.0956 |
| Alogliptin 25 + Pioglitazone 30 | -0.1232 |
| Placebo + Pioglitazone 45 | -0.0730 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.1125 |
| Alogliptin 25 + Pioglitazone 45 | -0.1228 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline proinsulin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | 1.2 |
| Alogliptin 12.5 + Placebo | 0.7 |
| Alogliptin 25 + Placebo | -3.3 |
| Placebo + Pioglitazone 15 | -3.5 |
| Alogliptin 12.5 + Pioglitazone 15 | -10.9 |
| Alogliptin 25 + Pioglitazone 15 | -7.2 |
| Placebo + Pioglitazone 30 | -8.4 |
| Alogliptin 12.5 + Pioglitazone 30 | -8.9 |
| Alogliptin 25 + Pioglitazone 30 | -8.8 |
| Placebo + Pioglitazone 45 | -4.1 |
| Alogliptin 12.5 + Pioglitazone 45 | -12.1 |
| Alogliptin 25 + Pioglitazone 45 | -12.6 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline fasting plasma glucose as covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 6.5 |
| Alogliptin 12.5 + Placebo | -13.2 |
| Alogliptin 25 + Placebo | -18.6 |
| Placebo + Pioglitazone 15 | -23.6 |
| Alogliptin 12.5 + Pioglitazone 15 | -42.0 |
| Alogliptin 25 + Pioglitazone 15 | -38.0 |
| Placebo + Pioglitazone 30 | -28.8 |
| Alogliptin 12.5 + Pioglitazone 30 | -42.2 |
| Alogliptin 25 + Pioglitazone 30 | -41.7 |
| Placebo + Pioglitazone 45 | -32.4 |
| Alogliptin 12.5 + Pioglitazone 45 | -51.3 |
| Alogliptin 25 + Pioglitazone 45 | -52.7 |
"The Homeostasis Model Assessment of insulin resistance (HOMA IR) measures insulin resistance based on fasting glucose and insulin measurements:~HOMA IR = fasting plasma insulin (µIU/mL) * fasting plasma glucose (mmol/L) / 22.5.~A higher number indicates a greater degree of insulin resistance. Least Squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and HOMA-IR as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | insulin resistance (Least Squares Mean) |
|---|---|
| Placebo | 0.464 |
| Alogliptin 12.5 + Placebo | 0.311 |
| Alogliptin 25 + Placebo | -0.179 |
| Placebo + Pioglitazone 15 | -0.864 |
| Alogliptin 12.5 + Pioglitazone 15 | -2.300 |
| Alogliptin 25 + Pioglitazone 15 | -0.223 |
| Placebo + Pioglitazone 30 | -2.061 |
| Alogliptin 12.5 + Pioglitazone 30 | -1.871 |
| Alogliptin 25 + Pioglitazone 30 | -2.056 |
| Placebo + Pioglitazone 45 | -1.789 |
| Alogliptin 12.5 + Pioglitazone 45 | -2.456 |
| Alogliptin 25 + Pioglitazone 45 | -2.854 |
"The Homeostasis Model Assessment (HOMA) estimates steady state beta cell function (%B) as a percentage of a normal reference population.~HOMA %B = 20 * insulin (µIU/mL) / fasting plasma glucose (mmol/L) - 3.5. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HOMA beta cell function as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | percentage beta cell function (Least Squares Mean) |
|---|---|
| Placebo | -0.924 |
| Alogliptin 12.5 + Placebo | 11.812 |
| Alogliptin 25 + Placebo | 17.814 |
| Placebo + Pioglitazone 15 | 2.770 |
| Alogliptin 12.5 + Pioglitazone 15 | 10.977 |
| Alogliptin 25 + Pioglitazone 15 | 19.320 |
| Placebo + Pioglitazone 30 | 8.983 |
| Alogliptin 12.5 + Pioglitazone 30 | 22.474 |
| Alogliptin 25 + Pioglitazone 30 | 23.475 |
| Placebo + Pioglitazone 45 | 3.427 |
| Alogliptin 12.5 + Pioglitazone 45 | 21.068 |
| Alogliptin 25 + Pioglitazone 45 | 23.752 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline C-peptide as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.011 |
| Alogliptin 12.5 + Placebo | 0.000 |
| Alogliptin 25 + Placebo | 0.059 |
| Placebo + Pioglitazone 15 | -0.239 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.380 |
| Alogliptin 25 + Pioglitazone 15 | -0.204 |
| Placebo + Pioglitazone 30 | -0.353 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.235 |
| Alogliptin 25 + Pioglitazone 30 | -0.300 |
| Placebo + Pioglitazone 45 | -0.429 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.421 |
| Alogliptin 25 + Pioglitazone 45 | -0.474 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline weight as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | -0.66 |
| Alogliptin 12.5 + Placebo | -0.02 |
| Alogliptin 25 + Placebo | -0.67 |
| Placebo + Pioglitazone 15 | 0.94 |
| Alogliptin 12.5 + Pioglitazone 15 | 1.25 |
| Alogliptin 25 + Pioglitazone 15 | 1.27 |
| Placebo + Pioglitazone 30 | 1.88 |
| Alogliptin 12.5 + Pioglitazone 30 | 1.89 |
| Alogliptin 25 + Pioglitazone 30 | 2.10 |
| Placebo + Pioglitazone 45 | 1.65 |
| Alogliptin 12.5 + Pioglitazone 45 | 2.30 |
| Alogliptin 25 + Pioglitazone 45 | 2.25 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein C-III as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 0.4 |
| Alogliptin 12.5 + Placebo | 0.5 |
| Alogliptin 25 + Placebo | -0.7 |
| Placebo + Pioglitazone 15 | -0.4 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.6 |
| Alogliptin 25 + Pioglitazone 15 | -0.7 |
| Placebo + Pioglitazone 30 | 0.2 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.4 |
| Alogliptin 25 + Pioglitazone 30 | -0.6 |
| Placebo + Pioglitazone 45 | 0.0 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.7 |
| Alogliptin 25 + Pioglitazone 45 | -0.5 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein B as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 0.6 |
| Alogliptin 12.5 + Placebo | -0.6 |
| Alogliptin 25 + Placebo | -3.7 |
| Placebo + Pioglitazone 15 | -1.5 |
| Alogliptin 12.5 + Pioglitazone 15 | -6.0 |
| Alogliptin 25 + Pioglitazone 15 | -4.8 |
| Placebo + Pioglitazone 30 | -3.2 |
| Alogliptin 12.5 + Pioglitazone 30 | -7.2 |
| Alogliptin 25 + Pioglitazone 30 | -8.8 |
| Placebo + Pioglitazone 45 | -3.6 |
| Alogliptin 12.5 + Pioglitazone 45 | -6.1 |
| Alogliptin 25 + Pioglitazone 45 | -5.5 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein A2 as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 0.1 |
| Alogliptin 12.5 + Placebo | 0.2 |
| Alogliptin 25 + Placebo | 0.4 |
| Placebo + Pioglitazone 15 | 1.9 |
| Alogliptin 12.5 + Pioglitazone 15 | 1.2 |
| Alogliptin 25 + Pioglitazone 15 | 1.0 |
| Placebo + Pioglitazone 30 | 2.7 |
| Alogliptin 12.5 + Pioglitazone 30 | 2.1 |
| Alogliptin 25 + Pioglitazone 30 | 1.6 |
| Placebo + Pioglitazone 45 | 2.8 |
| Alogliptin 12.5 + Pioglitazone 45 | 3.1 |
| Alogliptin 25 + Pioglitazone 45 | 2.7 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein A1 as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -4.9 |
| Alogliptin 12.5 + Placebo | -3.0 |
| Alogliptin 25 + Placebo | -4.2 |
| Placebo + Pioglitazone 15 | -3.3 |
| Alogliptin 12.5 + Pioglitazone 15 | -3.5 |
| Alogliptin 25 + Pioglitazone 15 | -2.9 |
| Placebo + Pioglitazone 30 | -0.2 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.1 |
| Alogliptin 25 + Pioglitazone 30 | -3.2 |
| Placebo + Pioglitazone 45 | -1.4 |
| Alogliptin 12.5 + Pioglitazone 45 | -1.0 |
| Alogliptin 25 + Pioglitazone 45 | -2.2 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline adiponectin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | μg/mL (Least Squares Mean) |
|---|---|
| Placebo | 0.43 |
| Alogliptin 12.5 + Placebo | 0.48 |
| Alogliptin 25 + Placebo | 0.26 |
| Placebo + Pioglitazone 15 | 3.30 |
| Alogliptin 12.5 + Pioglitazone 15 | 4.80 |
| Alogliptin 25 + Pioglitazone 15 | 2.93 |
| Placebo + Pioglitazone 30 | 5.90 |
| Alogliptin 12.5 + Pioglitazone 30 | 6.30 |
| Alogliptin 25 + Pioglitazone 30 | 6.87 |
| Placebo + Pioglitazone 45 | 8.75 |
| Alogliptin 12.5 + Pioglitazone 45 | 8.18 |
| Alogliptin 25 + Pioglitazone 45 | 9.59 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline triglycerides as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 20
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 5.7 |
| Alogliptin 12.5 + Placebo | -7.0 |
| Alogliptin 25 + Placebo | -23.7 |
| Placebo + Pioglitazone 15 | -18.0 |
| Alogliptin 12.5 + Pioglitazone 15 | -41.2 |
| Alogliptin 25 + Pioglitazone 15 | -34.6 |
| Placebo + Pioglitazone 30 | -37.5 |
| Alogliptin 12.5 + Pioglitazone 30 | -43.1 |
| Alogliptin 25 + Pioglitazone 30 | -42.4 |
| Placebo + Pioglitazone 45 | -49.3 |
| Alogliptin 12.5 + Pioglitazone 45 | -46.4 |
| Alogliptin 25 + Pioglitazone 45 | -51.2 |
"The ratio of proinsulin to insulin was calculated as proinsulin (pmol/L) / insulin (μIU/mL).~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline proinsulin/insulin ratio as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 20
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | -0.007 |
| Alogliptin 12.5 + Placebo | -0.014 |
| Alogliptin 25 + Placebo | -0.046 |
| Placebo + Pioglitazone 15 | -0.039 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.081 |
| Alogliptin 25 + Pioglitazone 15 | -0.065 |
| Placebo + Pioglitazone 30 | -0.042 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.085 |
| Alogliptin 25 + Pioglitazone 30 | -0.077 |
| Placebo + Pioglitazone 45 | -0.020 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.099 |
| Alogliptin 25 + Pioglitazone 45 | -0.092 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline LDL cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 20
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 6.9 |
| Alogliptin 12.5 + Placebo | 2.9 |
| Alogliptin 25 + Placebo | 1.9 |
| Placebo + Pioglitazone 15 | 7.7 |
| Alogliptin 12.5 + Pioglitazone 15 | 4.3 |
| Alogliptin 25 + Pioglitazone 15 | 3.0 |
| Placebo + Pioglitazone 30 | 6.6 |
| Alogliptin 12.5 + Pioglitazone 30 | 2.3 |
| Alogliptin 25 + Pioglitazone 30 | 4.1 |
| Placebo + Pioglitazone 45 | 6.3 |
| Alogliptin 12.5 + Pioglitazone 45 | 6.1 |
| Alogliptin 25 + Pioglitazone 45 | 1.9 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline insulin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 20
| Intervention | µIU/mL (Least Squares Mean) |
|---|---|
| Placebo | 0.18 |
| Alogliptin 12.5 + Placebo | 2.03 |
| Alogliptin 25 + Placebo | 0.76 |
| Placebo + Pioglitazone 15 | -0.66 |
| Alogliptin 12.5 + Pioglitazone 15 | -2.35 |
| Alogliptin 25 + Pioglitazone 15 | -0.90 |
| Placebo + Pioglitazone 30 | -3.29 |
| Alogliptin 12.5 + Pioglitazone 30 | -2.20 |
| Alogliptin 25 + Pioglitazone 30 | -2.29 |
| Placebo + Pioglitazone 45 | -3.12 |
| Alogliptin 12.5 + Pioglitazone 45 | -1.16 |
| Alogliptin 25 + Pioglitazone 45 | -3.01 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HDL cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 20
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 0.6 |
| Alogliptin 12.5 + Placebo | 0.9 |
| Alogliptin 25 + Placebo | 0.5 |
| Placebo + Pioglitazone 15 | 3.8 |
| Alogliptin 12.5 + Pioglitazone 15 | 4.3 |
| Alogliptin 25 + Pioglitazone 15 | 3.9 |
| Placebo + Pioglitazone 30 | 5.9 |
| Alogliptin 12.5 + Pioglitazone 30 | 5.7 |
| Alogliptin 25 + Pioglitazone 30 | 5.3 |
| Placebo + Pioglitazone 45 | 5.9 |
| Alogliptin 12.5 + Pioglitazone 45 | 7.1 |
| Alogliptin 25 + Pioglitazone 45 | 6.5 |
"The change from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) at week 20.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HbA1c as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 20
| Intervention | percentage of glycosylated hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.24 |
| Alogliptin 12.5 + Placebo | -0.75 |
| Alogliptin 25 + Placebo | -0.99 |
| Placebo + Pioglitazone 15 | -0.75 |
| Alogliptin 12.5 + Pioglitazone 15 | -1.39 |
| Alogliptin 25 + Pioglitazone 15 | -1.37 |
| Placebo + Pioglitazone 30 | -0.90 |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -1.43 |
| Alogliptin 25 + Pioglitazone 30 | -1.49 |
| Placebo + Pioglitazone 45 mg | -1.10 |
| Alogliptin 12.5 + Pioglitazone 45 | -1.57 |
| Alogliptin 25 + Pioglitazone 45 | -1.66 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline proinsulin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 20
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -0.9 |
| Alogliptin 12.5 + Placebo | 1.5 |
| Alogliptin 25 + Placebo | -3.0 |
| Placebo + Pioglitazone 15 | -3.4 |
| Alogliptin 12.5 + Pioglitazone 15 | -11.2 |
| Alogliptin 25 + Pioglitazone 15 | -8.7 |
| Placebo + Pioglitazone 30 | -9.3 |
| Alogliptin 12.5 + Pioglitazone 30 | -10.0 |
| Alogliptin 25 + Pioglitazone 30 | -10.7 |
| Placebo + Pioglitazone 45 | -7.1 |
| Alogliptin 12.5 + Pioglitazone 45 | -10.2 |
| Alogliptin 25 + Pioglitazone 45 | -12.5 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline fasting plasma glucose as covariates. (NCT00328627)
Timeframe: Baseline and Week 20
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 6.7 |
| Alogliptin 12.5 + Placebo | -8.7 |
| Alogliptin 25 + Placebo | -23.5 |
| Placebo + Pioglitazone 15 | -22.4 |
| Alogliptin 12.5 + Pioglitazone 15 | -43.0 |
| Alogliptin 25 + Pioglitazone 15 | -39.3 |
| Placebo + Pioglitazone 30 | -26.3 |
| Alogliptin 12.5 + Pioglitazone 30 | -41.1 |
| Alogliptin 25 + Pioglitazone 30 | -43.1 |
| Placebo + Pioglitazone 45 | -35.7 |
| Alogliptin 12.5 + Pioglitazone 45 | -46.8 |
| Alogliptin 25 + Pioglitazone 45 | -52.4 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline C-peptide as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 20
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.046 |
| Alogliptin 12.5 + Placebo | 0.114 |
| Alogliptin 25 + Placebo | 0.019 |
| Placebo + Pioglitazone 15 | -0.193 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.377 |
| Alogliptin 25 + Pioglitazone 15 | -0.184 |
| Placebo + Pioglitazone 30 | -0.380 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.343 |
| Alogliptin 25 + Pioglitazone 30 | -0.266 |
| Placebo + Pioglitazone 45 | -0.506 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.329 |
| Alogliptin 25 + Pioglitazone 45 | -0.430 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline weight as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 20
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | -0.55 |
| Alogliptin 12.5 + Placebo | -0.08 |
| Alogliptin 25 + Placebo | -0.48 |
| Placebo + Pioglitazone 15 | 0.76 |
| Alogliptin 12.5 + Pioglitazone 15 | 0.96 |
| Alogliptin 25 + Pioglitazone 15 | 0.85 |
| Placebo + Pioglitazone 30 | 1.51 |
| Alogliptin 12.5 + Pioglitazone 30 | 1.45 |
| Alogliptin 25 + Pioglitazone 30 | 1.76 |
| Placebo + Pioglitazone 45 | 1.35 |
| Alogliptin 12.5 + Pioglitazone 45 | 1.93 |
| Alogliptin 25 + Pioglitazone 45 | 1.76 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline fasting plasma glucose as covariates. (NCT00328627)
Timeframe: Baseline and Week 2
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 4.8 |
| Alogliptin 12.5 + Placebo | -21.9 |
| Alogliptin 25 + Placebo | -18.9 |
| Placebo + Pioglitazone 15 | -10.4 |
| Alogliptin 12.5 + Pioglitazone 15 | -30.1 |
| Alogliptin 25 + Pioglitazone 15 | -31.7 |
| Placebo + Pioglitazone 30 | -4.3 |
| Alogliptin 12.5 + Pioglitazone 30 | -30.0 |
| Alogliptin 25 + Pioglitazone 30 | -31.3 |
| Placebo + Pioglitazone 45 | -19.3 |
| Alogliptin 12.5 + Pioglitazone 45 | -30.8 |
| Alogliptin 25 + Pioglitazone 45 | -31.7 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline triglycerides as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 16
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 10.6 |
| Alogliptin 12.5 + Placebo | -7.5 |
| Alogliptin 25 + Placebo | -26.8 |
| Placebo + Pioglitazone 15 | -10.5 |
| Alogliptin 12.5 + Pioglitazone 15 | -53.0 |
| Alogliptin 25 + Pioglitazone 15 | -33.8 |
| Placebo + Pioglitazone 30 | -28.2 |
| Alogliptin 12.5 + Pioglitazone 30 | -44.2 |
| Alogliptin 25 + Pioglitazone 30 | -45.9 |
| Placebo + Pioglitazone 45 | -49.4 |
| Alogliptin 12.5 + Pioglitazone 45 | -50.7 |
| Alogliptin 25 + Pioglitazone 45 | -59.1 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline total cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 16
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 5.0 |
| Alogliptin 12.5 + Placebo | -0.5 |
| Alogliptin 25 + Placebo | -2.9 |
| Placebo + Pioglitazone 15 | 7.2 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.4 |
| Alogliptin 25 + Pioglitazone 15 | 3.2 |
| Placebo + Pioglitazone 30 | 10.0 |
| Alogliptin 12.5 + Pioglitazone 30 | 0.9 |
| Alogliptin 25 + Pioglitazone 30 | -1.2 |
| Placebo + Pioglitazone 45 | 2.3 |
| Alogliptin 12.5 + Pioglitazone 45 | 2.9 |
| Alogliptin 25 + Pioglitazone 45 | -1.8 |
"The ratio of proinsulin to insulin was calculated as proinsulin (pmol/L) / insulin (μIU/mL).~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline proinsulin/insulin ratio as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 16
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | -0.026 |
| Alogliptin 12.5 + Placebo | -0.036 |
| Alogliptin 25 + Placebo | -0.046 |
| Placebo + Pioglitazone 15 | -0.035 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.078 |
| Alogliptin 25 + Pioglitazone 15 | -0.066 |
| Placebo + Pioglitazone 30 | -0.035 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.094 |
| Alogliptin 25 + Pioglitazone 30 | -0.061 |
| Placebo + Pioglitazone 45 | -0.030 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.102 |
| Alogliptin 25 + Pioglitazone 45 | -0.104 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline LDL cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 16
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 4.2 |
| Alogliptin 12.5 + Placebo | 1.3 |
| Alogliptin 25 + Placebo | 0.9 |
| Placebo + Pioglitazone 15 | 7.1 |
| Alogliptin 12.5 + Pioglitazone 15 | 2.9 |
| Alogliptin 25 + Pioglitazone 15 | 4.6 |
| Placebo + Pioglitazone 30 | 7.1 |
| Alogliptin 12.5 + Pioglitazone 30 | 2.1 |
| Alogliptin 25 + Pioglitazone 30 | 0.8 |
| Placebo + Pioglitazone 45 | 4.1 |
| Alogliptin 12.5 + Pioglitazone 45 | 4.9 |
| Alogliptin 25 + Pioglitazone 45 | 1.8 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline insulin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 16
| Intervention | µIU/mL (Least Squares Mean) |
|---|---|
| Placebo | 0.34 |
| Alogliptin 12.5 + Placebo | 1.22 |
| Alogliptin 25 + Placebo | 1.83 |
| Placebo + Pioglitazone 15 | -0.63 |
| Alogliptin 12.5 + Pioglitazone 15 | -2.28 |
| Alogliptin 25 + Pioglitazone 15 | -1.11 |
| Placebo + Pioglitazone 30 | -3.46 |
| Alogliptin 12.5 + Pioglitazone 30 | -2.50 |
| Alogliptin 25 + Pioglitazone 30 | -2.82 |
| Placebo + Pioglitazone 45 | -2.48 |
| Alogliptin 12.5 + Pioglitazone 45 | -3.00 |
| Alogliptin 25 + Pioglitazone 45 | -3.52 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HDL cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 16
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -0.3 |
| Alogliptin 12.5 + Placebo | 0.4 |
| Alogliptin 25 + Placebo | 0.7 |
| Placebo + Pioglitazone 15 | 3.9 |
| Alogliptin 12.5 + Pioglitazone 15 | 4.2 |
| Alogliptin 25 + Pioglitazone 15 | 4.0 |
| Placebo + Pioglitazone 30 | 5.7 |
| Alogliptin 12.5 + Pioglitazone 30 | 5.5 |
| Alogliptin 25 + Pioglitazone 30 | 4.3 |
| Placebo + Pioglitazone 45 | 5.9 |
| Alogliptin 12.5 + Pioglitazone 45 | 6.1 |
| Alogliptin 25 + Pioglitazone 45 | 6.7 |
The change from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) at week 16. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HbA1c as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 16
| Intervention | percentage of glycosylated hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.27 |
| Alogliptin 12.5 + Placebo | -0.82 |
| Alogliptin 25 + Placebo | -1.03 |
| Placebo + Pioglitazone 15 | -0.74 |
| Alogliptin 12.5 + Pioglitazone 15 | -1.36 |
| Alogliptin 25 + Pioglitazone 15 | -1.36 |
| Placebo + Pioglitazone 30 | -0.91 |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -1.42 |
| Alogliptin 25 + Pioglitazone 30 | -1.45 |
| Placebo + Pioglitazone 45 mg | -1.12 |
| Alogliptin 12.5 + Pioglitazone 45 | -1.53 |
| Alogliptin 25 + Pioglitazone 45 | -1.66 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline proinsulin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 16
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -3.0 |
| Alogliptin 12.5 + Placebo | 0.0 |
| Alogliptin 25 + Placebo | -2.3 |
| Placebo + Pioglitazone 15 | -3.7 |
| Alogliptin 12.5 + Pioglitazone 15 | -11.0 |
| Alogliptin 25 + Pioglitazone 15 | -8.4 |
| Placebo + Pioglitazone 30 | -10.0 |
| Alogliptin 12.5 + Pioglitazone 30 | -12.6 |
| Alogliptin 25 + Pioglitazone 30 | -11.2 |
| Placebo + Pioglitazone 45 | -8.0 |
| Alogliptin 12.5 + Pioglitazone 45 | -13.0 |
| Alogliptin 25 + Pioglitazone 45 | -14.4 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline C-peptide as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 16
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.076 |
| Alogliptin 12.5 + Placebo | 0.032 |
| Alogliptin 25 + Placebo | 0.101 |
| Placebo + Pioglitazone 15 | -0.242 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.282 |
| Alogliptin 25 + Pioglitazone 15 | -0.184 |
| Placebo + Pioglitazone 30 | -0.410 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.318 |
| Alogliptin 25 + Pioglitazone 30 | -0.306 |
| Placebo + Pioglitazone 45 | -0.404 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.431 |
| Alogliptin 25 + Pioglitazone 45 | -0.510 |
The change from Baseline in VLDL/chylomicron triglyceride levels was assessed by NMR lipid fractionation. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR VLDL/chylomicron triglycerides as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 19.9 |
| Alogliptin 12.5 + Placebo | -3.5 |
| Alogliptin 25 + Placebo | -6.4 |
| Placebo + Pioglitazone 15 | -14.2 |
| Alogliptin 12.5 + Pioglitazone 15 | -21.1 |
| Alogliptin 25 + Pioglitazone 15 | -26.5 |
| Placebo + Pioglitazone 30 | -19.1 |
| Alogliptin 12.5 + Pioglitazone 30 | -29.5 |
| Alogliptin 25 + Pioglitazone 30 | -30.1 |
| Placebo + Pioglitazone 45 | -28.4 |
| Alogliptin 12.5 + Pioglitazone 45 | -35.5 |
| Alogliptin 25 + Pioglitazone 45 | -34.8 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline triglycerides as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 18.9 |
| Alogliptin 12.5 + Placebo | -4.3 |
| Alogliptin 25 + Placebo | -18.1 |
| Placebo + Pioglitazone 15 | -24.1 |
| Alogliptin 12.5 + Pioglitazone 15 | -37.4 |
| Alogliptin 25 + Pioglitazone 15 | -44.0 |
| Placebo + Pioglitazone 30 | -37.4 |
| Alogliptin 12.5 + Pioglitazone 30 | -47.9 |
| Alogliptin 25 + Pioglitazone 30 | -46.8 |
| Placebo + Pioglitazone 45 | -42.1 |
| Alogliptin 12.5 + Pioglitazone 45 | -57.1 |
| Alogliptin 25 + Pioglitazone 45 | -57.4 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline total cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 7.8 |
| Alogliptin 12.5 + Placebo | 0.4 |
| Alogliptin 25 + Placebo | 0.1 |
| Placebo + Pioglitazone 15 | 8.7 |
| Alogliptin 12.5 + Pioglitazone 15 | 1.9 |
| Alogliptin 25 + Pioglitazone 15 | -0.2 |
| Placebo + Pioglitazone 30 | 7.3 |
| Alogliptin 12.5 + Pioglitazone 30 | 0.3 |
| Alogliptin 25 + Pioglitazone 30 | -1.0 |
| Placebo + Pioglitazone 45 | 3.7 |
| Alogliptin 12.5 + Pioglitazone 45 | 1.7 |
| Alogliptin 25 + Pioglitazone 45 | -3.9 |
"The ratio of proinsulin to insulin was calculated as proinsulin (pmol/L) / insulin (μIU/mL).~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline proinsulin/insulin ratio as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | -0.006 |
| Alogliptin 12.5 + Placebo | -0.024 |
| Alogliptin 25 + Placebo | -0.041 |
| Placebo + Pioglitazone 15 | -0.041 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.073 |
| Alogliptin 25 + Pioglitazone 15 | -0.056 |
| Placebo + Pioglitazone 30 | -0.063 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.072 |
| Alogliptin 25 + Pioglitazone 30 | -0.088 |
| Placebo + Pioglitazone 45 | -0.021 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.112 |
| Alogliptin 25 + Pioglitazone 45 | -0.101 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline PAI-1 as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -4.55 |
| Alogliptin 12.5 + Placebo | 3.54 |
| Alogliptin 25 + Placebo | -1.80 |
| Placebo + Pioglitazone 15 | -5.32 |
| Alogliptin 12.5 + Pioglitazone 15 | -6.28 |
| Alogliptin 25 + Pioglitazone 15 | -10.94 |
| Placebo + Pioglitazone 30 | -8.53 |
| Alogliptin 12.5 + Pioglitazone 30 | -10.47 |
| Alogliptin 25 + Pioglitazone 30 | -1.71 |
| Placebo + Pioglitazone 45 | 1.85 |
| Alogliptin 12.5 + Pioglitazone 45 | -9.13 |
| Alogliptin 25 + Pioglitazone 45 | -12.63 |
"NMR lipid fractionation was used to assess the change from Baseline in total triglyceride levels at Week 12.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR total triglycerides as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 20.6 |
| Alogliptin 12.5 + Placebo | -4.9 |
| Alogliptin 25 + Placebo | -7.8 |
| Placebo + Pioglitazone 15 | -12.9 |
| Alogliptin 12.5 + Pioglitazone 15 | -21.8 |
| Alogliptin 25 + Pioglitazone 15 | -27.2 |
| Placebo + Pioglitazone 30 | -18.3 |
| Alogliptin 12.5 + Pioglitazone 30 | -29.8 |
| Alogliptin 25 + Pioglitazone 30 | -31.6 |
| Placebo + Pioglitazone 45 | -27.9 |
| Alogliptin 12.5 + Pioglitazone 45 | -35.1 |
| Alogliptin 25 + Pioglitazone 45 | -36.0 |
"The change from Baseline in mean VLDL particle size was assessed by NMR lipid fractionation.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline mean VLDL particle size as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | nm (Least Squares Mean) |
|---|---|
| Placebo | 0.65 |
| Alogliptin 12.5 + Placebo | 0.12 |
| Alogliptin 25 + Placebo | -0.18 |
| Placebo + Pioglitazone 15 | -2.81 |
| Alogliptin 12.5 + Pioglitazone 15 | -2.10 |
| Alogliptin 25 + Pioglitazone 15 | -2.56 |
| Placebo + Pioglitazone 30 | -3.16 |
| Alogliptin 12.5 + Pioglitazone 30 | -2.88 |
| Alogliptin 25 + Pioglitazone 30 | -2.49 |
| Placebo + Pioglitazone 45 | -2.37 |
| Alogliptin 12.5 + Pioglitazone 45 | -4.00 |
| Alogliptin 25 + Pioglitazone 45 | -4.03 |
"The change from Baseline in mean LDL particle size was assessed by NMR lipid fractionation.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline mean LDL particle size as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | nm (Least Squares Mean) |
|---|---|
| Placebo | -0.05 |
| Alogliptin 12.5 + Placebo | 0.13 |
| Alogliptin 25 + Placebo | 0.06 |
| Placebo + Pioglitazone 15 | 0.25 |
| Alogliptin 12.5 + Pioglitazone 15 | 0.43 |
| Alogliptin 25 + Pioglitazone 15 | 0.49 |
| Placebo + Pioglitazone 30 | 0.44 |
| Alogliptin 12.5 + Pioglitazone 30 | 0.61 |
| Alogliptin 25 + Pioglitazone 30 | 0.61 |
| Placebo + Pioglitazone 45 | 0.58 |
| Alogliptin 12.5 + Pioglitazone 45 | 0.68 |
| Alogliptin 25 + Pioglitazone 45 | 0.73 |
The change from Baseline in mean HDL particle size was assessed by NMR lipid fractionation. Least squares means are from are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline mean HDL particle size as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | nm (Least Squares Mean) |
|---|---|
| Placebo | 0.00 |
| Alogliptin 12.5 + Placebo | 0.00 |
| Alogliptin 25 + Placebo | 0.00 |
| Placebo + Pioglitazone 15 | 0.06 |
| Alogliptin 12.5 + Pioglitazone 15 | 0.07 |
| Alogliptin 25 + Pioglitazone 15 | 0.09 |
| Placebo + Pioglitazone 30 | 0.10 |
| Alogliptin 12.5 + Pioglitazone 30 | 0.15 |
| Alogliptin 25 + Pioglitazone 30 | 0.17 |
| Placebo + Pioglitazone 45 | 0.18 |
| Alogliptin 12.5 + Pioglitazone 45 | 0.17 |
| Alogliptin 25 + Pioglitazone 45 | 0.21 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline LDL cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 6.5 |
| Alogliptin 12.5 + Placebo | 1.9 |
| Alogliptin 25 + Placebo | 3.7 |
| Placebo + Pioglitazone 15 | 8.9 |
| Alogliptin 12.5 + Pioglitazone 15 | 3.3 |
| Alogliptin 25 + Pioglitazone 15 | 3.8 |
| Placebo + Pioglitazone 30 | 6.1 |
| Alogliptin 12.5 + Pioglitazone 30 | 1.9 |
| Alogliptin 25 + Pioglitazone 30 | 0.9 |
| Placebo + Pioglitazone 45 | 5.7 |
| Alogliptin 12.5 + Pioglitazone 45 | 4.9 |
| Alogliptin 25 + Pioglitazone 45 | -0.3 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline insulin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | µIU/mL (Least Squares Mean) |
|---|---|
| Placebo | 0.06 |
| Alogliptin 12.5 + Placebo | 1.79 |
| Alogliptin 25 + Placebo | 1.93 |
| Placebo + Pioglitazone 15 | -1.29 |
| Alogliptin 12.5 + Pioglitazone 15 | -1.47 |
| Alogliptin 25 + Pioglitazone 15 | -2.01 |
| Placebo + Pioglitazone 30 | -3.61 |
| Alogliptin 12.5 + Pioglitazone 30 | -1.36 |
| Alogliptin 25 + Pioglitazone 30 | -2.83 |
| Placebo + Pioglitazone 45 | -2.95 |
| Alogliptin 12.5 + Pioglitazone 45 | -2.35 |
| Alogliptin 25 + Pioglitazone 45 | -3.01 |
"The change from Baseline in levels of IDL particles was assessed by NMR lipid fractionation.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR IDL particles as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | nmol/L (Least Squares Mean) |
|---|---|
| Placebo | 1.6 |
| Alogliptin 12.5 + Placebo | -11.1 |
| Alogliptin 25 + Placebo | -6.0 |
| Placebo + Pioglitazone 15 | 5.1 |
| Alogliptin 12.5 + Pioglitazone 15 | -6.0 |
| Alogliptin 25 + Pioglitazone 15 | -2.3 |
| Placebo + Pioglitazone 30 | -2.2 |
| Alogliptin 12.5 + Pioglitazone 30 | -6.3 |
| Alogliptin 25 + Pioglitazone 30 | -8.1 |
| Placebo + Pioglitazone 45 | -1.5 |
| Alogliptin 12.5 + Pioglitazone 45 | 0.7 |
| Alogliptin 25 + Pioglitazone 45 | -6.5 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline hsCRP as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | mg/L (Least Squares Mean) |
|---|---|
| Placebo | -1.1053 |
| Alogliptin 12.5 + Placebo | -1.0730 |
| Alogliptin 25 + Placebo | 0.3516 |
| Placebo + Pioglitazone 15 | -0.9166 |
| Alogliptin 12.5 + Pioglitazone 15 | -2.2362 |
| Alogliptin 25 + Pioglitazone 15 | -2.4217 |
| Placebo + Pioglitazone 30 | -2.7023 |
| Alogliptin 12.5 + Pioglitazone 30 | -2.2143 |
| Alogliptin 25 + Pioglitazone 30 | -1.0006 |
| Placebo + Pioglitazone 45 | -2.4212 |
| Alogliptin 12.5 + Pioglitazone 45 | -2.9032 |
| Alogliptin 25 + Pioglitazone 45 | -2.2978 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HDL cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -0.2 |
| Alogliptin 12.5 + Placebo | 0.0 |
| Alogliptin 25 + Placebo | 0.3 |
| Placebo + Pioglitazone 15 | 3.8 |
| Alogliptin 12.5 + Pioglitazone 15 | 3.7 |
| Alogliptin 25 + Pioglitazone 15 | 3.7 |
| Placebo + Pioglitazone 30 | 6.3 |
| Alogliptin 12.5 + Pioglitazone 30 | 5.8 |
| Alogliptin 25 + Pioglitazone 30 | 5.3 |
| Placebo + Pioglitazone 45 | 6.1 |
| Alogliptin 12.5 + Pioglitazone 45 | 6.3 |
| Alogliptin 25 + Pioglitazone 45 | 6.4 |
"The change from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) at week 12.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HbA1c as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | percentage of glycosylated hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.28 |
| Alogliptin 12.5 + Placebo | -0.84 |
| Alogliptin 25 + Placebo | -0.92 |
| Placebo + Pioglitazone 15 | -0.65 |
| Alogliptin 12.5 + Pioglitazone 15 | -1.24 |
| Alogliptin 25 + Pioglitazone 15 | -1.26 |
| Placebo + Pioglitazone 30 | -0.77 |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -1.29 |
| Alogliptin 25 + Pioglitazone 30 | -1.33 |
| Placebo + Pioglitazone 45 mg | -1.02 |
| Alogliptin 12.5 + Pioglitazone 45 | -1.34 |
| Alogliptin 25 + Pioglitazone 45 | -1.53 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline free fatty acid as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | mmol/L (Least Squares Mean) |
|---|---|
| Placebo | 0.0067 |
| Alogliptin 12.5 + Placebo | -0.0149 |
| Alogliptin 25 + Placebo | -0.0769 |
| Placebo + Pioglitazone 15 | -0.0879 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.1305 |
| Alogliptin 25 + Pioglitazone 15 | -0.1291 |
| Placebo + Pioglitazone 30 | -0.0395 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.1167 |
| Alogliptin 25 + Pioglitazone 30 | -0.1126 |
| Placebo + Pioglitazone 45 | -0.0848 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.1447 |
| Alogliptin 25 + Pioglitazone 45 | -0.1401 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline proinsulin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -1.0 |
| Alogliptin 12.5 + Placebo | -0.7 |
| Alogliptin 25 + Placebo | -2.3 |
| Placebo + Pioglitazone 15 | -5.3 |
| Alogliptin 12.5 + Pioglitazone 15 | -10.1 |
| Alogliptin 25 + Pioglitazone 15 | -8.8 |
| Placebo + Pioglitazone 30 | -11.2 |
| Alogliptin 12.5 + Pioglitazone 30 | -12.1 |
| Alogliptin 25 + Pioglitazone 30 | -12.7 |
| Placebo + Pioglitazone 45 | -8.1 |
| Alogliptin 12.5 + Pioglitazone 45 | -12.7 |
| Alogliptin 25 + Pioglitazone 45 | -13.2 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline fasting plasma glucose as covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 3.4 |
| Alogliptin 12.5 + Placebo | -19.3 |
| Alogliptin 25 + Placebo | -23.3 |
| Placebo + Pioglitazone 15 | -23.0 |
| Alogliptin 12.5 + Pioglitazone 15 | -42.9 |
| Alogliptin 25 + Pioglitazone 15 | -42.5 |
| Placebo + Pioglitazone 30 | -26.6 |
| Alogliptin 12.5 + Pioglitazone 30 | -42.8 |
| Alogliptin 25 + Pioglitazone 30 | -49.0 |
| Placebo + Pioglitazone 45 | -41.3 |
| Alogliptin 12.5 + Pioglitazone 45 | -49.2 |
| Alogliptin 25 + Pioglitazone 45 | -51.4 |
"The Homeostasis Model Assessment of insulin resistance (HOMA IR) measures insulin resistance based on fasting glucose and insulin measurements:~HOMA IR = fasting plasma insulin (µIU/mL) * fasting plasma glucose (mmol/L) / 22.5.~A higher number indicates a greater degree of insulin resistance. Least Squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and HOMA-IR as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | insulin resistance (Least Squares Mean) |
|---|---|
| Placebo | 0.337 |
| Alogliptin 12.5 + Placebo | 0.063 |
| Alogliptin 25 + Placebo | 0.041 |
| Placebo + Pioglitazone 15 | -1.012 |
| Alogliptin 12.5 + Pioglitazone 15 | -1.819 |
| Alogliptin 25 + Pioglitazone 15 | -2.305 |
| Placebo + Pioglitazone 30 | -2.278 |
| Alogliptin 12.5 + Pioglitazone 30 | -1.457 |
| Alogliptin 25 + Pioglitazone 30 | -2.665 |
| Placebo + Pioglitazone 45 | -2.202 |
| Alogliptin 12.5 + Pioglitazone 45 | -2.615 |
| Alogliptin 25 + Pioglitazone 45 | -2.742 |
"The Homeostasis Model Assessment (HOMA) estimates steady state beta cell function (%B) as a percentage of a normal reference population.~HOMA %B = 20 * insulin (µIU/mL) / fasting plasma glucose (mmol/L) - 3.5. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HOMA beta cell function as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | percentage beta cell function (Least Squares Mean) |
|---|---|
| Placebo | -3.027 |
| Alogliptin 12.5 + Placebo | 16.304 |
| Alogliptin 25 + Placebo | 22.996 |
| Placebo + Pioglitazone 15 | 2.565 |
| Alogliptin 12.5 + Pioglitazone 15 | 30.346 |
| Alogliptin 25 + Pioglitazone 15 | 19.887 |
| Placebo + Pioglitazone 30 | 1.118 |
| Alogliptin 12.5 + Pioglitazone 30 | 21.045 |
| Alogliptin 25 + Pioglitazone 30 | 19.935 |
| Placebo + Pioglitazone 45 | 4.023 |
| Alogliptin 12.5 + Pioglitazone 45 | 19.938 |
| Alogliptin 25 + Pioglitazone 45 | 18.541 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline C-peptide as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.055 |
| Alogliptin 12.5 + Placebo | 0.083 |
| Alogliptin 25 + Placebo | 0.140 |
| Placebo + Pioglitazone 15 | 0.116 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.155 |
| Alogliptin 25 + Pioglitazone 15 | -0.215 |
| Placebo + Pioglitazone 30 | -0.439 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.212 |
| Alogliptin 25 + Pioglitazone 30 | -0.326 |
| Placebo + Pioglitazone 45 | -0.483 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.381 |
| Alogliptin 25 + Pioglitazone 45 | -0.464 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline weight as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | -0.46 |
| Alogliptin 12.5 + Placebo | -0.14 |
| Alogliptin 25 + Placebo | -0.56 |
| Placebo + Pioglitazone 15 | 0.39 |
| Alogliptin 12.5 + Pioglitazone 15 | 0.22 |
| Alogliptin 25 + Pioglitazone 15 | 0.39 |
| Placebo + Pioglitazone 30 | 0.75 |
| Alogliptin 12.5 + Pioglitazone 30 | 0.60 |
| Alogliptin 25 + Pioglitazone 30 | 0.98 |
| Placebo + Pioglitazone 45 | 0.55 |
| Alogliptin 12.5 + Pioglitazone 45 | 0.88 |
| Alogliptin 25 + Pioglitazone 45 | 1.08 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline fasting plasma glucose as covariates. (NCT00328627)
Timeframe: Baseline and Week 16
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 1.4 |
| Alogliptin 12.5 + Placebo | -16.2 |
| Alogliptin 25 + Placebo | -22.6 |
| Placebo + Pioglitazone 15 | -21.2 |
| Alogliptin 12.5 + Pioglitazone 15 | -41.6 |
| Alogliptin 25 + Pioglitazone 15 | -39.1 |
| Placebo + Pioglitazone 30 | -26.3 |
| Alogliptin 12.5 + Pioglitazone 30 | -41.5 |
| Alogliptin 25 + Pioglitazone 30 | -43.4 |
| Placebo + Pioglitazone 45 | -36.3 |
| Alogliptin 12.5 + Pioglitazone 45 | -47.9 |
| Alogliptin 25 + Pioglitazone 45 | -53.8 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein C-III as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 0.7 |
| Alogliptin 12.5 + Placebo | -0.4 |
| Alogliptin 25 + Placebo | -0.7 |
| Placebo + Pioglitazone 15 | -0.3 |
| Alogliptin 12.5 + Pioglitazone 15 | -1.0 |
| Alogliptin 25 + Pioglitazone 15 | -1.4 |
| Placebo + Pioglitazone 30 | -0.3 |
| Alogliptin 12.5 + Pioglitazone 30 | -1.0 |
| Alogliptin 25 + Pioglitazone 30 | -1.3 |
| Placebo + Pioglitazone 45 | -1.1 |
| Alogliptin 12.5 + Pioglitazone 45 | -1.4 |
| Alogliptin 25 + Pioglitazone 45 | -1.2 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein B as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 5.0 |
| Alogliptin 12.5 + Placebo | -2.3 |
| Alogliptin 25 + Placebo | -3.6 |
| Placebo + Pioglitazone 15 | -0.3 |
| Alogliptin 12.5 + Pioglitazone 15 | -7.2 |
| Alogliptin 25 + Pioglitazone 15 | -6.1 |
| Placebo + Pioglitazone 30 | -2.1 |
| Alogliptin 12.5 + Pioglitazone 30 | -8.4 |
| Alogliptin 25 + Pioglitazone 30 | -12.2 |
| Placebo + Pioglitazone 45 | -6.6 |
| Alogliptin 12.5 + Pioglitazone 45 | -8.0 |
| Alogliptin 25 + Pioglitazone 45 | -11.7 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein A2 as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 0.4 |
| Alogliptin 12.5 + Placebo | 0.1 |
| Alogliptin 25 + Placebo | 0.4 |
| Placebo + Pioglitazone 15 | 2.4 |
| Alogliptin 12.5 + Pioglitazone 15 | 1.4 |
| Alogliptin 25 + Pioglitazone 15 | 1.9 |
| Placebo + Pioglitazone 30 | 3.7 |
| Alogliptin 12.5 + Pioglitazone 30 | 2.5 |
| Alogliptin 25 + Pioglitazone 30 | 1.8 |
| Placebo + Pioglitazone 45 | 3.0 |
| Alogliptin 12.5 + Pioglitazone 45 | 3.7 |
| Alogliptin 25 + Pioglitazone 45 | 3.2 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein A1 as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -1.9 |
| Alogliptin 12.5 + Placebo | -4.4 |
| Alogliptin 25 + Placebo | -3.0 |
| Placebo + Pioglitazone 15 | 0.8 |
| Alogliptin 12.5 + Pioglitazone 15 | -1.3 |
| Alogliptin 25 + Pioglitazone 15 | 1.7 |
| Placebo + Pioglitazone 30 | 3.5 |
| Alogliptin 12.5 + Pioglitazone 30 | 0.7 |
| Alogliptin 25 + Pioglitazone 30 | 0.4 |
| Placebo + Pioglitazone 45 | -0.1 |
| Alogliptin 12.5 + Pioglitazone 45 | 1.1 |
| Alogliptin 25 + Pioglitazone 45 | -1.2 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline adiponectin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | μg/mL (Least Squares Mean) |
|---|---|
| Placebo | 0.02 |
| Alogliptin 12.5 + Placebo | 0.44 |
| Alogliptin 25 + Placebo | 0.22 |
| Placebo + Pioglitazone 15 | 3.54 |
| Alogliptin 12.5 + Pioglitazone 15 | 3.78 |
| Alogliptin 25 + Pioglitazone 15 | 2.91 |
| Placebo + Pioglitazone 30 | 6.07 |
| Alogliptin 12.5 + Pioglitazone 30 | 6.31 |
| Alogliptin 25 + Pioglitazone 30 | 7.13 |
| Placebo + Pioglitazone 45 | 8.47 |
| Alogliptin 12.5 + Pioglitazone 45 | 9.42 |
| Alogliptin 25 + Pioglitazone 45 | 9.46 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline fasting plasma glucose as covariates. (NCT00328627)
Timeframe: Baseline and Week 1
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 1.8 |
| Alogliptin 12.5 + Placebo | -14.5 |
| Alogliptin 25 + Placebo | -18.6 |
| Placebo + Pioglitazone 15 | -6.1 |
| Alogliptin 12.5 + Pioglitazone 15 | -21.3 |
| Alogliptin 25 + Pioglitazone 15 | -20.9 |
| Placebo + Pioglitazone 30 | 0.4 |
| Alogliptin 12.5 + Pioglitazone 30 | -23.2 |
| Alogliptin 25 + Pioglitazone 30 | -23.2 |
| Placebo + Pioglitazone 45 | -6.7 |
| Alogliptin 12.5 + Pioglitazone 45 | -23.2 |
| Alogliptin 25 + Pioglitazone 45 | -25.0 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline total cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 20
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 6.7 |
| Alogliptin 12.5 + Placebo | 1.8 |
| Alogliptin 25 + Placebo | -1.9 |
| Placebo + Pioglitazone 15 | 6.3 |
| Alogliptin 12.5 + Pioglitazone 15 | 4.0 |
| Alogliptin 25 + Pioglitazone 15 | 1.4 |
| Placebo + Pioglitazone 30 | 7.0 |
| Alogliptin 12.5 + Pioglitazone 30 | 1.1 |
| Alogliptin 25 + Pioglitazone 30 | 3.4 |
| Placebo + Pioglitazone 45 | 4.6 |
| Alogliptin 12.5 + Pioglitazone 45 | 4.0 |
| Alogliptin 25 + Pioglitazone 45 | -0.3 |
"The change from Baseline in levels of total, large, medium and small HDL particles was assessed by NMR fractionation at Weeks 12 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR HDL particles as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | μMOL/L (Least Squares Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Total Particles - Week 12 (n=332, 345, 343) | Total Particles - Week 26 (n=348, 359, 357) | Large Particles - Week 12 (n=332, 345, 343) | Large Particles - Week 26 (n=348, 359, 357) | Medium Particles - Week 12 (n=332, 345, 343) | Medium Particles - Week 26 (n=348, 359, 357) | Small Particles - Week 12 (n=332, 345, 343) | Small Particles - Week 26 (n=348, 359, 357) | |
| Alogliptin 12.5 + Pioglitazone | 0.58 | 1.18 | 0.78 | 0.90 | 1.16 | 1.10 | -1.39 | -0.85 |
| Alogliptin 25 + Pioglitazone | 0.43 | 0.78 | 0.89 | 1.01 | 1.63 | 1.46 | -2.12 | -1.73 |
| Pioglitazone Alone | 0.86 | 0.62 | 0.89 | 0.81 | 1.38 | 1.34 | -1.35 | -1.45 |
"The change from Baseline to Weeks 4, 8, 12, 16 and 20 in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound).~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an analysis of covariance (ANCOVA) model with treatment and geographic region as class variables, and baseline metformin dose and HbA1c as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 4, 8, 12, 16 and 20.
| Intervention | percentage of glycosylated hemoglobin (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Week 4 (n=345, 359, 346) | Week 8 (n=376, 385, 377) | Week 12 (n=376, 385, 377) | Week 16 (n=376, 385, 377) | Week 20 (n=376, 385, 377) | |
| Alogliptin 12.5 + Pioglitazone | -0.57 | -1.06 | -1.29 | -1.44 | -1.46 |
| Alogliptin 25 + Pioglitazone | -0.61 | -1.09 | -1.38 | -1.49 | -1.51 |
| Pioglitazone Alone | -0.32 | -0.61 | -0.81 | -0.92 | -0.92 |
Change from Baseline in free fatty acids (FFA) was assessed at Weeks 12 and 26. This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline free fatty acid as continuous covariates. (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | mmol/L (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=339, 356, 352) | Week 26 (n=353, 368, 363) | |
| Alogliptin 12.5 + Pioglitazone | -0.1306 | -0.0945 |
| Alogliptin 25 + Pioglitazone | -0.1273 | -0.1144 |
| Pioglitazone Alone | -0.0707 | -0.0676 |
"Proinsulin is a precursor to insulin, and was measured as an indicator of pancreatic function. The change from Baseline in fasting proinsulin was assessed at Weeks 4, 8, 12, 16, 20 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and proinsulin as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | pmol/L (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=328, 319, 327) | Week 8 (n=357, 347, 358) | Week 12 (n=357, 347, 358) | Week 16 (n=358, 348, 358) | Week 20 (n=358, 349, 359) | Week 26 (n=358, 349, 359) | |
| Alogliptin 12.5 + Pioglitazone | -10.3 | -11.3 | -11.6 | -12.2 | -10.4 | -10.6 |
| Alogliptin 25 + Pioglitazone | -10.1 | -11.3 | -11.6 | -11.3 | -10.7 | -9.5 |
| Pioglitazone Alone | -6.2 | -7.2 | -8.2 | -7.2 | -6.6 | -5.3 |
"The change from Baseline in fasting plasma glucose was assessed at weeks 1, 2, 4, 8, 12, 16, 20 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline fasting plasma glucose as covariates." (NCT00328627)
Timeframe: Baseline and Weeks 1, 2, 4, 8, 12, 16, 20 and 26.
| Intervention | mg/dL (Least Squares Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 1 (n=358, 355, 354) | Week 2 (n=379, 383, 381) | Week 4 (n=381, 386, 383) | Week 8 (n=381, 386, 383) | Week 12 (n=381, 386, 383) | Week 16 (n=381, 386, 383) | Week 20 (n=381, 386, 383) | Week 26 (n=381, 386, 383) | |
| Alogliptin 12.5 + Pioglitazone | -22.6 | -30.3 | -36.8 | -42.3 | -45.0 | -43.7 | -43.6 | -45.2 |
| Alogliptin 25 + Pioglitazone | -23.1 | -31.6 | -39.8 | -45.2 | -47.6 | -45.4 | -45.0 | -44.2 |
| Pioglitazone Alone | -4.1 | -11.3 | -19.9 | -27.3 | -30.3 | -27.9 | -28.1 | -28.3 |
"HOMA IR measures insulin resistance based on fasting glucose and insulin measurements:~HOMA IR = fasting plasma insulin (µIU/mL) * fasting plasma glucose (mmol/L) / 22.5.~A higher number indicates a greater insulin resistance. This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone.~Least Squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and HOMA-IR as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | insulin resistance (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=347, 344, 351) | Week 26 (n=348, 346, 352) | |
| Alogliptin 12.5 + Pioglitazone | -1.966 | -2.209 |
| Alogliptin 25 + Pioglitazone | -2.572 | -1.711 |
| Pioglitazone Alone | -1.832 | -1.571 |
"C-peptide is a byproduct created when the hormone insulin is produced and is measured by a blood test. Change from Baseline was assessed at Weeks 4, 8, 12, 16, 20 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline C-peptide as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | ng/mL (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=335, 335, 336) | Week 8 (n=367, 366, 371) | Week 12 (n=367, 369, 374) | Week 16 (n=369, 374, 374) | Week 20 (n=369, 375, 375) | Week 26 (n=371, 378, 375) | |
| Alogliptin 12.5 + Pioglitazone | -0.255 | -0.327 | -0.249 | -0.343 | -0.350 | -0.346 |
| Alogliptin 25 + Pioglitazone | -0.282 | -0.311 | -0.334 | -0.333 | -0.293 | -0.326 |
| Pioglitazone Alone | -0.292 | -0.356 | -0.268 | -0.352 | -0.360 | -0.341 |
Change from Baseline in body weight was assessed at Weeks 8, 12, 20 and 26. This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline weight as continuous covariates. (NCT00328627)
Timeframe: Baseline and Weeks 8, 12, 20 and 26.
| Intervention | kg (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 8 (n=361, 372, 367) | Week 12 (n=368, 374, 373) | Week 20 (n=368, 374, 373) | Week 26 (n=368, 374, 373) | |
| Alogliptin 12.5 + Pioglitazone | 0.34 | 0.57 | 1.45 | 1.81 |
| Alogliptin 25 + Pioglitazone | 0.63 | 0.82 | 1.46 | 1.87 |
| Pioglitazone Alone | 0.45 | 0.56 | 1.21 | 1.49 |
Change from Baseline in apolipoprotein C-III was assessed at Weeks 12 and 26. This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein C-III as continuous covariates. (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26
| Intervention | mg/dL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=337, 352, 345) | Week 26 (n=353, 366, 355) | |
| Alogliptin 12.5 + Pioglitazone | -1.2 | -0.6 |
| Alogliptin 25 + Pioglitazone | -1.3 | -0.6 |
| Pioglitazone Alone | -0.6 | -0.1 |
Change from Baseline in Apolipoprotein B was assessed at Weeks 12 and 26. This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein B as continuous covariates. (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26
| Intervention | mg/dL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=338, 354, 346) | Week 26 (n=354, 367, 356) | |
| Alogliptin 12.5 + Pioglitazone | -7.9 | -6.4 |
| Alogliptin 25 + Pioglitazone | -10.0 | -6.4 |
| Pioglitazone Alone | -3.0 | -2.8 |
Change from Baseline in Apolipoprotein A2 was assessed at Weeks 12 and 26. This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein A2 as continuous covariates. (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26
| Intervention | mg/dL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=339, 354, 345) | Week 26 (n=354, 367, 355) | |
| Alogliptin 12.5 + Pioglitazone | 2.5 | 2.1 |
| Alogliptin 25 + Pioglitazone | 2.3 | 1.8 |
| Pioglitazone Alone | 3.1 | 2.4 |
Change from Baseline in Apolipoprotein A1 was assessed at Weeks 12 and 26. This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein A1 as continuous covariates. (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | mg/dL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=339, 354, 346) | Week 26 (n=354, 367, 356) | |
| Alogliptin 12.5 + Pioglitazone | 0.2 | -1.5 |
| Alogliptin 25 + Pioglitazone | 0.3 | -2.8 |
| Pioglitazone Alone | 1.4 | -1.6 |
Change from Baseline in adiponectin was assessed at Weeks 12 and 26. This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline adiponectin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | μg/mL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=339, 357, 348) | Week 26 (n=356, 369, 361) | |
| Alogliptin 12.5 + Pioglitazone | 6.51 | 6.43 |
| Alogliptin 25 + Pioglitazone | 6.51 | 6.46 |
| Pioglitazone Alone | 6.03 | 5.98 |
"Marked hyperglycemia is defined as fasting plasma glucose greater than or equal to 200 mg/dL (11.10 mmol/L).~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone." (NCT00328627)
Timeframe: From Week 1 to Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Pioglitazone Alone | 39.4 |
| Alogliptin 12.5 + Pioglitazone | 24.6 |
| Alogliptin 25 + Pioglitazone | 22.1 |
Marked hyperglycemia is defined as fasting plasma glucose greater than or equal to 200 mg/dL (11.10 mmol/L). (NCT00328627)
Timeframe: From Week 1 to Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 60.5 |
| Alogliptin 12.5 + Placebo | 42.6 |
| Alogliptin 25 + Placebo | 39.7 |
| Placebo + Pioglitazone 15 | 37.8 |
| Alogliptin 12.5 + Pioglitazone 15 | 27.1 |
| Alogliptin 25 + Pioglitazone 15 | 22.3 |
| Placebo + Pioglitazone 30 | 39.2 |
| Alogliptin 12.5 + Pioglitazone 30 | 26.4 |
| Alogliptin 25 + Pioglitazone 30 | 23.6 |
| Placebo + Pioglitazone 45 | 41.1 |
| Alogliptin 12.5 + Pioglitazone 45 | 20.3 |
| Alogliptin 25 + Pioglitazone 45 | 20.5 |
Clinical response at Week 26 was assessed by the percentage of participants with HbA1c less than or equal to 7%. (NCT00328627)
Timeframe: Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 6.2 |
| Alogliptin 12.5 + Placebo | 22.7 |
| Alogliptin 25 + Placebo | 27.1 |
| Placebo + Pioglitazone 15 | 25.6 |
| Alogliptin 12.5 + Pioglitazone 15 | 49.2 |
| Alogliptin 25 + Pioglitazone 15 | 54.6 |
| Placebo + Pioglitazone 30 | 29.5 |
| Alogliptin 12.5 + Pioglitazone 30 | 53.1 |
| Alogliptin 25 + Pioglitazone 30 | 53.1 |
| Placebo + Pioglitazone 45 | 36.4 |
| Alogliptin 12.5 + Pioglitazone 45 | 61.5 |
| Alogliptin 25 + Pioglitazone 45 | 60.0 |
"Clinical response at Week 26 was assessed by the percentage of participants with HbA1c less than or equal to 7.5%.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone." (NCT00328627)
Timeframe: Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Pioglitazone Alone | 54.8 |
| Alogliptin 12.5 + Pioglitazone | 77.4 |
| Alogliptin 25 + Pioglitazone | 74.1 |
Clinical response at Week 26 was assessed by the percentage of participants with HbA1c less than or equal to 7.5%. (NCT00328627)
Timeframe: Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 24.8 |
| Alogliptin 12.5 + Placebo | 38.3 |
| Alogliptin 25 + Placebo | 55.0 |
| Placebo + Pioglitazone 15 | 51.9 |
| Alogliptin 12.5 + Pioglitazone 15 | 77.7 |
| Alogliptin 25 + Pioglitazone 15 | 71.5 |
| Placebo + Pioglitazone 30 | 55.8 |
| Alogliptin 12.5 + Pioglitazone 30 | 73.8 |
| Alogliptin 25 + Pioglitazone 30 | 72.3 |
| Placebo + Pioglitazone 45 | 56.6 |
| Alogliptin 12.5 + Pioglitazone 45 | 80.8 |
| Alogliptin 25 + Pioglitazone 45 | 78.5 |
"Clinical response at Week 26 was assessed by the percentage of participants with HbA1c less than or equal to 7%.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone." (NCT00328627)
Timeframe: Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Pioglitazone Alone | 30.5 |
| Alogliptin 12.5 + Pioglitazone | 54.6 |
| Alogliptin 25 + Pioglitazone | 55.9 |
"Clinical response at Week 26 was assessed by the percentage of participants with HbA1c less than or equal to 6.5%.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone." (NCT00328627)
Timeframe: Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Pioglitazone Alone | 12.4 |
| Alogliptin 12.5 + Pioglitazone | 27.9 |
| Alogliptin 25 + Pioglitazone | 29.2 |
"Change from Baseline in high-density lipoprotein cholesterol (HDL-C) was assessed at Weeks 4, 8, 12, 16, 20 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HDL cholesterol as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | mg/dL (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=345, 353, 348) | Week 8 (n=374, 380, 376) | Week 12 (n=374, 380, 376) | Week 16 (n=374, 380, 376) | Week 20 (n=374, 380, 376) | Week 26 (n=374, 380, 376) | |
| Alogliptin 12.5 + Pioglitazone | 2.7 | 4.1 | 5.3 | 5.2 | 5.7 | 5.5 |
| Alogliptin 25 + Pioglitazone | 3.4 | 4.6 | 5.1 | 5.0 | 5.2 | 5.0 |
| Pioglitazone Alone | 3.0 | 4.0 | 5.4 | 5.2 | 5.2 | 5.1 |
"Change from Baseline in high-sensitivity C-Reactive Protein (hsCRP) was assessed at Weeks 12 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline hsCRP as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | mg/L (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=346, 356, 355) | Week 26 (n=359, 369, 363) | |
| Alogliptin 12.5 + Pioglitazone | -2.4653 | -1.7716 |
| Alogliptin 25 + Pioglitazone | -1.9208 | -0.9977 |
| Pioglitazone Alone | -2.0274 | -0.8889 |
"The homeostatic model assessment estimates steady state beta cell function as a percentage of a normal reference population (%B).~HOMA %B = 20 * insulin (µIU/mL) / fasting plasma glucose (mmol/L) - 3.5.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HOMA beta cell function as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26
| Intervention | percentage beta cell function (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=347, 344, 350) | Week 26 (n=348, 346, 351) | |
| Alogliptin 12.5 + Pioglitazone | 23.799 | 18.173 |
| Alogliptin 25 + Pioglitazone | 19.477 | 22.182 |
| Pioglitazone Alone | 2.591 | 5.060 |
The change from Baseline in fasting insulin was assessed at Weeks 4, 8, 12, 16, 20 and 26. This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline insulin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | µIU/mL (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=325, 318, 326) | Week 8 (n=355, 346, 356) | Week 12 (n=355, 347, 356) | Week 16 (n=356, 348, 356) | Week 20 (n=356, 349, 357) | Week 26 (n=356, 349, 357) | |
| Alogliptin 12.5 + Pioglitazone | -2.11 | -2.44 | -1.73 | -2.60 | -1.91 | -2.05 |
| Alogliptin 25 + Pioglitazone | -2.19 | -2.36 | -2.62 | -2.48 | -2.06 | -1.66 |
| Pioglitazone Alone | -2.29 | -2.35 | -2.62 | -2.19 | -2.35 | -1.74 |
"The change from Baseline in levels of IDL particles was assessed by NMR lipid fractionation at Weeks 12 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR IDL particles as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26
| Intervention | nmol/L (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=332, 345, 343) | Week 26 (n=348, 359, 357) | |
| Alogliptin 12.5 + Pioglitazone | -3.9 | -4.2 |
| Alogliptin 25 + Pioglitazone | -5.7 | -1.5 |
| Pioglitazone Alone | 0.4 | 2.8 |
"The change from Baseline in levels of total, large, medium-small, total small and very small LDL particles was assessed by NMR fractionation at Weeks 12 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR LDL particles as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26
| Intervention | nmol/L (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Total Particles - Week 12 (n=332, 345, 343) | Total Particles - Week 26 (n=348, 359, 357) | Large Particles - Week 12 (n=332, 345, 343) | Large Particles - Week 26 (n=348, 359, 357) | Medium-Small Particles - Week 12 (n=332, 345, 343) | Medium-Small Particles - Week 26 (n=348, 359, 357) | Total Small Particles - Week 12 (n=332, 345, 343) | Total Small Particles - Week 26 (n=348, 359, 357) | Very Small Particles - Week 12 (n=332, 345, 343) | Very Small Particles - Week 26 (n=348, 359, 357) | |
| Alogliptin 12.5 + Pioglitazone | -180.5 | -146.2 | 111.6 | 93.9 | -55.3 | -44.9 | -287.5 | -235.0 | -232.3 | -190.3 |
| Alogliptin 25 + Pioglitazone | -236.8 | -182.9 | 102.3 | 106.1 | -60.1 | -49.6 | -331.4 | -285.9 | -271.3 | -236.2 |
| Pioglitazone Alone | -104.1 | -78.2 | 85.5 | 95.8 | -36.6 | -34.3 | -191.4 | -178.1 | -154.6 | -143.6 |
"Change from Baseline in low-density lipoprotein cholesterol (LDL-C) was assessed at Weeks 4, 8, 12, 16, 20 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline LDL cholesterol as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | mg/dL (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=330, 336, 338) | Week 8 (n=365, 365, 365) | Week 12 (n=365, 367, 366) | Week 16 (n=365, 368, 366) | Week 20 (n=365, 368, 366) | Week 26 (n=365, 368, 366) | |
| Alogliptin 12.5 + Pioglitazone | -0.5 | 1.3 | 3.3 | 3.3 | 4.2 | 5.2 |
| Alogliptin 25 + Pioglitazone | -1.9 | 0.1 | 1.5 | 2.4 | 3.0 | 5.6 |
| Pioglitazone Alone | 3.1 | 5.9 | 6.9 | 6.1 | 6.9 | 7.4 |
"The change from Baseline in mean HDL particle size was assessed by NMR lipid fractionation at Weeks 12 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline mean HDL particle size as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26
| Intervention | nm (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=332, 345, 343) | Week 26 (n=348, 359, 357) | |
| Alogliptin 12.5 + Pioglitazone | 0.13 | 0.12 |
| Alogliptin 25 + Pioglitazone | 0.16 | 0.17 |
| Pioglitazone Alone | 0.11 | 0.11 |
"The change from Baseline in mean LDL particle size was assessed by NMR lipid fractionation at Weeks 12 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline mean LDL particle size as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26
| Intervention | nm (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=332, 345, 343) | Week 26 (n=348, 359, 357) | |
| Alogliptin 12.5 + Pioglitazone | 0.58 | 0.47 |
| Alogliptin 25 + Pioglitazone | 0.61 | 0.54 |
| Pioglitazone Alone | 0.43 | 0.41 |
"The change from Baseline in mean VLDL particle size was assessed by NMR lipid fractionation at Weeks 12 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline mean VLDL particle size as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26
| Intervention | nm (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=332, 344, 343) | Week 26 (n=348, 358, 357) | |
| Alogliptin 12.5 + Pioglitazone | -2.98 | -3.67 |
| Alogliptin 25 + Pioglitazone | -3.02 | -3.26 |
| Pioglitazone Alone | -2.77 | -2.49 |
"Nuclear Magnetic Resonance (NMR) lipid fractionation was used to assess the change from Baseline in total triglyceride levels at Weeks 12 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR total triglycerides as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | mg/dL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=332, 345, 343) | Week 26 (n=348, 359, 357) | |
| Alogliptin 12.5 + Pioglitazone | -28.8 | -25.4 |
| Alogliptin 25 + Pioglitazone | -31.5 | -22.9 |
| Pioglitazone Alone | -19.6 | -11.5 |
"Change from Baseline in plasminogen activator inhibitor-1 (PAI-1) was assessed at Weeks 12 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline PAI-1 as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | ng/mL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=311, 333, 328) | Week 26 (n=341, 354, 348) | |
| Alogliptin 12.5 + Pioglitazone | -8.76 | -2.69 |
| Alogliptin 25 + Pioglitazone | -8.57 | -9.25 |
| Pioglitazone Alone | -4.14 | -4.56 |
"The ratio of proinsulin to insulin was calculated as proinsulin (pmol/L) / insulin (μIU/mL) at weeks 4, 8, 12, 16, 20 and 26 relative to the Baseline value.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline proinsulin/insulin ratio as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | ratio (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=325, 315, 326) | Week 8 (n=355, 344, 356) | Week 12 (n=355, 345, 356) | Week 16 (n=356, 346, 356) | Week 20 (n=356, 347, 357) | Week 26 (n=356, 347, 357) | |
| Alogliptin 12.5 + Pioglitazone | -0.078 | -0.079 | -0.086 | -0.091 | -0.088 | -0.087 |
| Alogliptin 25 + Pioglitazone | -0.057 | -0.081 | -0.082 | -0.077 | -0.078 | -0.076 |
| Pioglitazone Alone | -0.021 | -0.019 | -0.042 | -0.033 | -0.034 | -0.027 |
Change from Baseline in total cholesterol was assessed at Weeks 4, 8, 12, 16, 20 and 26. This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline total cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | mg/dL (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=345, 354, 348) | Week 8 (n=374, 380, 376) | Week 12 (n=374, 380, 376) | Week 16 (n=374, 380, 376) | Week 20 (n=374, 380, 376) | Week 26 (n=374, 380, 376) | |
| Alogliptin 12.5 + Pioglitazone | -4.3 | -1.8 | 1.3 | 1.2 | 3.0 | 4.4 |
| Alogliptin 25 + Pioglitazone | -6.5 | -3.3 | -1.7 | 0.1 | 1.5 | 3.9 |
| Pioglitazone Alone | 1.6 | 4.8 | 6.6 | 6.5 | 5.9 | 8.0 |
Change from Baseline in triglycerides was assessed at Weeks 4, 8, 12, 16, 20 and 26. This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline triglycerides as continuous covariates. (NCT00328627)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | mg/dL (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=345, 354, 348) | Week 8 (n=374, 380, 376) | Week 12 (n=374, 380, 376) | Week 16 (n=374, 380, 376) | Week 20 (n=374, 380, 376) | Week 26 (n=374, 380, 376) | |
| Alogliptin 12.5 + Pioglitazone | -38.9 | -44.4 | -47.5 | -49.3 | -43.6 | -41.4 |
| Alogliptin 25 + Pioglitazone | -48.0 | -47.9 | -49.4 | -46.3 | -42.7 | -40.7 |
| Pioglitazone Alone | -31.5 | -34.7 | -34.5 | -29.4 | -34.9 | -29.6 |
"The change from Baseline in levels of total VLDL/chylomicron particles and large VLDL/chylomicron particles was assessed by NMR lipid fractionation at Weeks 12 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR VLDL/chylomicron particles as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26
| Intervention | nmol/L (Least Squares Mean) | |||
|---|---|---|---|---|
| Total Particles - Week 12 (n=332, 345, 343) | Total Particles - Week 26 (n=348, 359, 357) | Large Particles - Week 12 (n=332, 345, 343) | Large Particles - Week 26 (n=348, 359, 357) | |
| Alogliptin 12.5 + Pioglitazone | -6.40 | -1.87 | -2.20 | -2.25 |
| Alogliptin 25 + Pioglitazone | -7.26 | -1.31 | -2.17 | -1.98 |
| Pioglitazone Alone | -1.85 | -1.05 | -1.61 | -1.05 |
"The change from Baseline in levels of VLDL/chylomicron triglycerides was assessed by NMR lipid fractionation at Weeks 12 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR VLDL/chylomicron triglycerides as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26
| Intervention | mg/dL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=332, 345, 343) | Week 26 (n=348, 359, 357) | |
| Alogliptin 12.5 + Pioglitazone | -28.5 | -25.4 |
| Alogliptin 25 + Pioglitazone | -30.3 | -23.0 |
| Pioglitazone Alone | -20.4 | -13.0 |
"The change from Baseline in levels of medium VLDL particles and small VLDL particles was assessed by NMR fractionation at Weeks 12 and 26.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR VLDL particles as continuous covariates." (NCT00328627)
Timeframe: Baseline and Weeks 12 and 26
| Intervention | nmol/L (Least Squares Mean) | |||
|---|---|---|---|---|
| Medium Particles - Week 12 (n=332, 345, 343) | Medium Particles - Week 26 (n=348, 359, 357) | Small Particles - Week 12 (n=332, 345, 343) | Small Particles - Week 26 (n=348, 359, 357) | |
| Alogliptin 12.5 + Pioglitazone | -5.36 | -3.02 | 1.33 | 3.55 |
| Alogliptin 25 + Pioglitazone | -7.30 | -4.88 | 1.91 | 5.22 |
| Pioglitazone Alone | -4.44 | -2.28 | 4.16 | 2.30 |
"The change from Baseline in levels of total, large, medium and small HDL particles was assessed by NMR lipid fractionation.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR HDL particles as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | μmol/L (Least Squares Mean) | |||
|---|---|---|---|---|
| Total Particles | Large Particles | Medium Particles | Small Particles | |
| Alogliptin 12.5 + Pioglitazone 15 | 0.37 | 0.24 | 1.15 | -1.09 |
| Alogliptin 12.5 + Pioglitazone 30 | 0.75 | 0.95 | 0.97 | -1.18 |
| Alogliptin 12.5 + Pioglitazone 45 | 0.63 | 1.17 | 1.30 | -1.84 |
| Alogliptin 12.5 + Placebo | -0.06 | -0.29 | -0.24 | 0.43 |
| Alogliptin 25 + Pioglitazone 15 | 0.55 | 0.50 | 0.65 | -0.63 |
| Alogliptin 25 + Pioglitazone 30 | 0.15 | 1.12 | 1.89 | -2.82 |
| Alogliptin 25 + Pioglitazone 45 | 0.60 | 1.06 | 2.31 | -2.84 |
| Alogliptin 25 + Placebo | 0.16 | -0.10 | -0.01 | 0.27 |
| Placebo | -0.08 | -0.21 | 0.17 | -0.07 |
| Placebo + Pioglitazone 15 | 0.90 | 0.53 | 0.81 | -0.25 |
| Placebo + Pioglitazone 30 | 1.29 | 1.09 | 1.21 | -0.92 |
| Placebo + Pioglitazone 45 | 0.40 | 1.06 | 2.06 | -2.82 |
"The change from Baseline in levels of total, large, medium-small, total small and very small LDL particles was assessed by NMR lipid fractionation.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR LDL particles as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | nmol/L (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Total Particles | Large Particles | Medium-Small Particles | Total Small Particles | Very Small Particles | |
| Alogliptin 12.5 + Pioglitazone 15 | -143.5 | 73.8 | -41.1 | -211.0 | -170.3 |
| Alogliptin 12.5 + Pioglitazone 30 | -195.8 | 126.2 | -58.2 | -313.7 | -255.7 |
| Alogliptin 12.5 + Pioglitazone 45 | -202.2 | 135.2 | -66.8 | -337.9 | -271.0 |
| Alogliptin 12.5 + Placebo | -39.1 | 21.1 | -7.7 | -52.0 | -44.1 |
| Alogliptin 25 + Pioglitazone 15 | -175.6 | 85.7 | -48.0 | -256.3 | -207.6 |
| Alogliptin 25 + Pioglitazone 30 | -248.8 | 105.7 | -64.1 | -345.4 | -281.5 |
| Alogliptin 25 + Pioglitazone 45 | -285.8 | 116.1 | -68.2 | -392.7 | -325.0 |
| Alogliptin 25 + Placebo | -69.9 | -8.0 | -5.1 | -56.5 | -51.9 |
| Placebo | 52.0 | 4.7 | 9.4 | 45.1 | 36.4 |
| Placebo + Pioglitazone 15 | -48.8 | 56.2 | -20.3 | -109.9 | -89.2 |
| Placebo + Pioglitazone 30 | -96.2 | 83.9 | -34.4 | -184.1 | -149.8 |
| Placebo + Pioglitazone 45 | -167.0 | 116.9 | -55.4 | -280.4 | -225.0 |
"The change from Baseline in levels of total VLDL/chylomicron particles and large VLDL/chylomicron particles was assessed by NMR lipid fractionation.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR VLDL/chylomicron particles as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | nmol/L (Least Squares Mean) | |
|---|---|---|
| Total Particles | Large Particles | |
| Alogliptin 12.5 + Pioglitazone 15 | -3.46 | -1.63 |
| Alogliptin 12.5 + Pioglitazone 30 | -7.82 | -2.19 |
| Alogliptin 12.5 + Pioglitazone 45 | -7.99 | -2.81 |
| Alogliptin 12.5 + Placebo | -1.59 | -0.42 |
| Alogliptin 25 + Pioglitazone 15 | -5.57 | -1.81 |
| Alogliptin 25 + Pioglitazone 30 | -6.54 | -2.29 |
| Alogliptin 25 + Pioglitazone 45 | -9.76 | -2.45 |
| Alogliptin 25 + Placebo | -5.32 | -0.27 |
| Placebo | 5.82 | 1.12 |
| Placebo + Pioglitazone 15 | 2.52 | -1.20 |
| Placebo + Pioglitazone 30 | 0.45 | -1.69 |
| Placebo + Pioglitazone 45 | -8.58 | -1.97 |
"The change from Baseline in levels of medium VLDL particles and small VLDL particles was assessed by NMR lipid fractionation.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR VLDL particles as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 12
| Intervention | nmol/L (Least Squares Mean) | |
|---|---|---|
| Medium Particles | Small Particles | |
| Alogliptin 12.5 + Pioglitazone 15 | -3.16 | 1.16 |
| Alogliptin 12.5 + Pioglitazone 30 | -6.70 | 1.15 |
| Alogliptin 12.5 + Pioglitazone 45 | -6.38 | 1.80 |
| Alogliptin 12.5 + Placebo | -1.13 | 0.39 |
| Alogliptin 25 + Pioglitazone 15 | -6.51 | 2.60 |
| Alogliptin 25 + Pioglitazone 30 | -7.05 | 2.51 |
| Alogliptin 25 + Pioglitazone 45 | -8.50 | 0.73 |
| Alogliptin 25 + Placebo | -2.88 | -2.30 |
| Placebo | 2.13 | 2.76 |
| Placebo + Pioglitazone 15 | -2.25 | 5.99 |
| Placebo + Pioglitazone 30 | -2.59 | 4.39 |
| Placebo + Pioglitazone 45 | -8.64 | 2.22 |
"The change from Baseline in levels of total, large, medium and small HDL particles was assessed by NMR lipid fractionation.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR HDL particles as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | μmol/L (Least Squares Mean) | |||
|---|---|---|---|---|
| Total Particles | Large Particles | Medium Particles | Small Particles | |
| Alogliptin 12.5 + Pioglitazone 15 | 0.77 | 0.55 | 0.86 | -0.68 |
| Alogliptin 12.5 + Pioglitazone 30 | 1.15 | 1.13 | 1.47 | -1.47 |
| Alogliptin 12.5 + Pioglitazone 45 | 1.61 | 1.02 | 0.96 | -0.40 |
| Alogliptin 12.5 + Placebo | 0.43 | -0.16 | 0.16 | 0.41 |
| Alogliptin 25 + Pioglitazone 15 | 1.31 | 0.75 | 0.67 | -0.17 |
| Alogliptin 25 + Pioglitazone 30 | 0.26 | 1.34 | 1.69 | -2.77 |
| Alogliptin 25 + Pioglitazone 45 | 0.77 | 0.95 | 2.01 | -2.24 |
| Alogliptin 25 + Placebo | 1.03 | 0.39 | 0.54 | 0.10 |
| Placebo | 0.18 | 0.02 | 0.13 | 0.00 |
| Placebo + Pioglitazone 15 | 0.37 | 0.53 | 0.81 | -0.78 |
| Placebo + Pioglitazone 30 | 0.67 | 0.64 | 1.48 | -1.35 |
| Placebo + Pioglitazone 45 | 0.83 | 1.26 | 1.71 | -2.21 |
"The change from Baseline in levels of total, large, medium-small, total small and very small LDL particles was assessed by NMR lipid fractionation.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR LDL particles as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | nmol/L (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Total Particles | Large Particles | Medium-Small Particles | Total Small Particles | Very Small Particles | |
| Alogliptin 12.5 + Pioglitazone 15 | -115.1 | 63.2 | -29.9 | -175.1 | -145.7 |
| Alogliptin 12.5 + Pioglitazone 30 | -158.9 | 96.6 | -47.4 | -248.7 | -201.6 |
| Alogliptin 12.5 + Pioglitazone 45 | -164.6 | 121.9 | -57.6 | -281.1 | -223.6 |
| Alogliptin 12.5 + Placebo | -14.5 | -12.3 | 0.0 | 2.2 | 2.5 |
| Alogliptin 25 + Pioglitazone 15 | -119.4 | 93.1 | -36.2 | -211.5 | -174.5 |
| Alogliptin 25 + Pioglitazone 30 | -209.4 | 102.7 | -55.0 | -304.9 | -250.0 |
| Alogliptin 25 + Pioglitazone 45 | -219.9 | 122.7 | -57.8 | -341.3 | -283.9 |
| Alogliptin 25 + Placebo | -30.8 | 15.3 | -6.9 | -42.9 | -36.6 |
| Placebo | 15.0 | -23.8 | 9.1 | 32.4 | 24.0 |
| Placebo + Pioglitazone 15 | -46.3 | 70.5 | -25.8 | -122.5 | -96.3 |
| Placebo + Pioglitazone 30 | -68.6 | 79.3 | -30.0 | -154.9 | -124.9 |
| Placebo + Pioglitazone 45 | -119.7 | 137.7 | -47.1 | -256.9 | -209.6 |
"The change from Baseline in levels of total VLDL/chylomicron particles and large VLDL/chylomicron particles was assessed by NMR lipid fractionation.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR VLDL/chylomicron particles as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | nmol/L (Least Squares Mean) | |
|---|---|---|
| Total Particles | Large Particles | |
| Alogliptin 12.5 + Pioglitazone 15 | -3.31 | -1.71 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.59 | -2.24 |
| Alogliptin 12.5 + Pioglitazone 45 | -1.70 | -2.80 |
| Alogliptin 12.5 + Placebo | 0.59 | 0.94 |
| Alogliptin 25 + Pioglitazone 15 | -5.15 | -1.80 |
| Alogliptin 25 + Pioglitazone 30 | -0.35 | -1.79 |
| Alogliptin 25 + Pioglitazone 45 | 1.56 | -2.36 |
| Alogliptin 25 + Placebo | -5.79 | -0.14 |
| Placebo | 2.80 | 1.31 |
| Placebo + Pioglitazone 15 | -2.99 | -1.56 |
| Placebo + Pioglitazone 30 | 3.68 | -0.90 |
| Placebo + Pioglitazone 45 | -3.83 | -0.67 |
"The change from Baseline in levels of medium VLDL particles and small VLDL particles was assessed by NMR lipid fractionation.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR VLDL particles as continuous covariates" (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | nmol/L (Least Squares Mean) | |
|---|---|---|
| Medium Particles | Small Particles | |
| Alogliptin 12.5 + Pioglitazone 15 | -1.78 | -0.19 |
| Alogliptin 12.5 + Pioglitazone 30 | -2.17 | 4.07 |
| Alogliptin 12.5 + Pioglitazone 45 | -5.09 | 6.77 |
| Alogliptin 12.5 + Placebo | 0.85 | -0.87 |
| Alogliptin 25 + Pioglitazone 15 | -5.42 | 1.90 |
| Alogliptin 25 + Pioglitazone 30 | -4.38 | 5.45 |
| Alogliptin 25 + Pioglitazone 45 | -4.83 | 8.33 |
| Alogliptin 25 + Placebo | -2.94 | -2.91 |
| Placebo | 1.54 | 0.26 |
| Placebo + Pioglitazone 15 | -4.43 | 2.83 |
| Placebo + Pioglitazone 30 | 0.28 | 4.16 |
| Placebo + Pioglitazone 45 | -2.70 | -0.08 |
Clinical response at Week 26 was assessed by the percentage of participants with HbA1c less than or equal to 6.5%. (NCT00328627)
Timeframe: Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 0.8 |
| Alogliptin 12.5 + Placebo | 8.6 |
| Alogliptin 25 + Placebo | 12.4 |
| Placebo + Pioglitazone 15 | 6.2 |
| Alogliptin 12.5 + Pioglitazone 15 | 21.5 |
| Alogliptin 25 + Pioglitazone 15 | 24.6 |
| Placebo + Pioglitazone 30 | 11.6 |
| Alogliptin 12.5 + Pioglitazone 30 | 30.0 |
| Alogliptin 25 + Pioglitazone 30 | 30.0 |
| Placebo + Pioglitazone 45 | 19.4 |
| Alogliptin 12.5 + Pioglitazone 45 | 32.3 |
| Alogliptin 25 + Pioglitazone 45 | 33.1 |
Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 2%. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 1.6 |
| Alogliptin 12.5 + Placebo | 7.8 |
| Alogliptin 25 + Placebo | 11.6 |
| Placebo + Pioglitazone 15 | 7.0 |
| Alogliptin 12.5 + Pioglitazone 15 | 23.1 |
| Alogliptin 25 + Pioglitazone 15 | 21.5 |
| Placebo + Pioglitazone 30 | 9.3 |
| Alogliptin 12.5 + Pioglitazone 30 | 22.3 |
| Alogliptin 25 + Pioglitazone 30 | 26.2 |
| Placebo + Pioglitazone 45 | 17.1 |
| Alogliptin 12.5 + Pioglitazone 45 | 30.8 |
| Alogliptin 25 + Pioglitazone 45 | 35.4 |
"Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 2.0%.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone." (NCT00328627)
Timeframe: Baseline and Week 26.
| Intervention | percentage of participants (Number) |
|---|---|
| Pioglitazone Alone | 11.1 |
| Alogliptin 12.5 + Pioglitazone | 25.4 |
| Alogliptin 25 + Pioglitazone | 27.7 |
"Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 1%.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone." (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Pioglitazone Alone | 45.7 |
| Alogliptin 12.5 + Pioglitazone | 71.8 |
| Alogliptin 25 + Pioglitazone | 69.5 |
Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 1%. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 16.3 |
| Alogliptin 12.5 + Placebo | 33.6 |
| Alogliptin 25 + Placebo | 47.3 |
| Placebo + Pioglitazone 15 | 36.4 |
| Alogliptin 12.5 + Pioglitazone 15 | 69.2 |
| Alogliptin 25 + Pioglitazone 15 | 66.9 |
| Placebo + Pioglitazone 30 | 46.5 |
| Alogliptin 12.5 + Pioglitazone 30 | 73.1 |
| Alogliptin 25 + Pioglitazone 30 | 69.2 |
| Placebo + Pioglitazone 45 | 54.3 |
| Alogliptin 12.5 + Pioglitazone 45 | 73.1 |
| Alogliptin 25 + Pioglitazone 45 | 72.3 |
"Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 1.5%.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone." (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Pioglitazone Alone | 27.6 |
| Alogliptin 12.5 + Pioglitazone | 45.9 |
| Alogliptin 25 + Pioglitazone | 50.3 |
Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 1.5%. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 5.4 |
| Alogliptin 12.5 + Placebo | 15.6 |
| Alogliptin 25 + Placebo | 28.7 |
| Placebo + Pioglitazone 15 | 21.7 |
| Alogliptin 12.5 + Pioglitazone 15 | 41.5 |
| Alogliptin 25 + Pioglitazone 15 | 46.2 |
| Placebo + Pioglitazone 30 | 27.1 |
| Alogliptin 12.5 + Pioglitazone 30 | 45.4 |
| Alogliptin 25 + Pioglitazone 30 | 46.2 |
| Placebo + Pioglitazone 45 | 34.1 |
| Alogliptin 12.5 + Pioglitazone 45 | 50.8 |
| Alogliptin 25 + Pioglitazone 45 | 58.5 |
"Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 0.5%.~This analysis compared the groupings of participants who received the combination of pioglitazone with each dose of alogliptin with the grouping of participants who received pioglitazone alone." (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Pioglitazone Alone | 67.2 |
| Alogliptin 12.5 + Pioglitazone | 85.6 |
| Alogliptin 25 + Pioglitazone | 83.3 |
Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 0.5%. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 31.8 |
| Alogliptin 12.5 + Placebo | 57.8 |
| Alogliptin 25 + Placebo | 66.7 |
| Placebo + Pioglitazone 15 | 61.2 |
| Alogliptin 12.5 + Pioglitazone 15 | 86.2 |
| Alogliptin 25 + Pioglitazone 15 | 79.2 |
| Placebo + Pioglitazone 30 | 68.2 |
| Alogliptin 12.5 + Pioglitazone 30 | 86.9 |
| Alogliptin 25 + Pioglitazone 30 | 83.8 |
| Placebo + Pioglitazone 45 | 72.1 |
| Alogliptin 12.5 + Pioglitazone 45 | 83.8 |
| Alogliptin 25 + Pioglitazone 45 | 86.9 |
"Rescue was defined as meeting 1 of the following criteria, confirmed by a 2nd sample drawn within 5 days of the first and analyzed by the central laboratory:~After the Week 1 Visit but prior to the Week 4 Visit: a single fasting plasma glucose ≥300 mg/dL;~From the Week 4 Visit but prior to the Week 8 Visit: a single fasting plasma glucose ≥275 mg/dL;~From the Week 8 Visit but prior to the Week 12 Visit: a single fasting plasma glucose ≥250 mg/dL;~From the Week 12 Visit through the End-of-Treatment Visit: HbA1c ≥8.5% and ≤0.5% reduction in HbA1c as compared with Baseline HbA1c." (NCT00328627)
Timeframe: From Week 1 to Week 26.
| Intervention | percentage of participants (Number) |
|---|---|
| Pioglitazone Alone | 11.4 |
| Alogliptin 12.5 + Pioglitazone | 3.9 |
| Alogliptin 25 + Pioglitazone | 3.4 |
"Rescue was defined as meeting 1 of the following criteria, confirmed by a 2nd sample drawn within 5 days of the first and analyzed by the central laboratory:~After the Week 1 Visit but prior to the Week 4 Visit: a single fasting plasma glucose ≥300 mg/dL;~From the Week 4 Visit but prior to the Week 8 Visit: a single fasting plasma glucose ≥275 mg/dL;~From the Week 8 Visit but prior to the Week 12 Visit: a single fasting plasma glucose ≥250 mg/dL;~From the Week 12 Visit through the End-of-Treatment Visit: HbA1c ≥8.5% and ≤0.5% reduction in HbA1c as compared with Baseline HbA1c." (NCT00328627)
Timeframe: From Week 1 to Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 32.8 |
| Alogliptin 12.5 + Placebo | 14.5 |
| Alogliptin 25 + Placebo | 12.8 |
| Placebo + Pioglitazone 15 | 10.2 |
| Alogliptin 12.5 + Pioglitazone 15 | 4.7 |
| Alogliptin 25 + Pioglitazone 15 | 3.9 |
| Placebo + Pioglitazone 30 | 15.4 |
| Alogliptin 12.5 + Pioglitazone 30 | 4.8 |
| Alogliptin 25 + Pioglitazone 30 | 4.9 |
| Placebo + Pioglitazone 45 | 8.7 |
| Alogliptin 12.5 + Pioglitazone 45 | 2.4 |
| Alogliptin 25 + Pioglitazone 45 | 1.6 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline triglycerides as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 8
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 26.3 |
| Alogliptin 12.5 + Placebo | -16.4 |
| Alogliptin 25 + Placebo | -23.0 |
| Placebo + Pioglitazone 15 | -20.5 |
| Alogliptin 12.5 + Pioglitazone 15 | -30.1 |
| Alogliptin 25 + Pioglitazone 15 | -46.4 |
| Placebo + Pioglitazone 30 | -30.3 |
| Alogliptin 12.5 + Pioglitazone 30 | -43.1 |
| Alogliptin 25 + Pioglitazone 30 | -44.5 |
| Placebo + Pioglitazone 45 | -53.1 |
| Alogliptin 12.5 + Pioglitazone 45 | -60.1 |
| Alogliptin 25 + Pioglitazone 45 | -52.7 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline total cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 8
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 10.9 |
| Alogliptin 12.5 + Placebo | -1.4 |
| Alogliptin 25 + Placebo | -0.3 |
| Placebo + Pioglitazone 15 | 7.3 |
| Alogliptin 12.5 + Pioglitazone 15 | -2.3 |
| Alogliptin 25 + Pioglitazone 15 | -4.1 |
| Placebo + Pioglitazone 30 | 6.6 |
| Alogliptin 12.5 + Pioglitazone 30 | 0.1 |
| Alogliptin 25 + Pioglitazone 30 | 0.3 |
| Placebo + Pioglitazone 45 | 0.3 |
| Alogliptin 12.5 + Pioglitazone 45 | -3.1 |
| Alogliptin 25 + Pioglitazone 45 | -6.2 |
"The ratio of proinsulin to insulin was calculated as proinsulin (pmol/L) / insulin (μIU/mL).~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline proinsulin/insulin ratio as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 8
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | 0.005 |
| Alogliptin 12.5 + Placebo | -0.025 |
| Alogliptin 25 + Placebo | -0.045 |
| Placebo + Pioglitazone 15 | -0.007 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.086 |
| Alogliptin 25 + Pioglitazone 15 | -0.077 |
| Placebo + Pioglitazone 30 | -0.036 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.054 |
| Alogliptin 25 + Pioglitazone 30 | -0.072 |
| Placebo + Pioglitazone 45 | -0.013 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.098 |
| Alogliptin 25 + Pioglitazone 45 | -0.093 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline LDL cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 8
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 9.4 |
| Alogliptin 12.5 + Placebo | 2.1 |
| Alogliptin 25 + Placebo | 3.4 |
| Placebo + Pioglitazone 15 | 7.3 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.4 |
| Alogliptin 25 + Pioglitazone 15 | 1.0 |
| Placebo + Pioglitazone 30 | 5.4 |
| Alogliptin 12.5 + Pioglitazone 30 | 2.4 |
| Alogliptin 25 + Pioglitazone 30 | 2.7 |
| Placebo + Pioglitazone 45 | 4.8 |
| Alogliptin 12.5 + Pioglitazone 45 | 2.0 |
| Alogliptin 25 + Pioglitazone 45 | -3.2 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline insulin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 8
| Intervention | µIU/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.46 |
| Alogliptin 12.5 + Placebo | 1.80 |
| Alogliptin 25 + Placebo | 1.69 |
| Placebo + Pioglitazone 15 | -1.47 |
| Alogliptin 12.5 + Pioglitazone 15 | -2.21 |
| Alogliptin 25 + Pioglitazone 15 | -2.78 |
| Placebo + Pioglitazone 30 | -2.74 |
| Alogliptin 12.5 + Pioglitazone 30 | -3.15 |
| Alogliptin 25 + Pioglitazone 30 | -1.20 |
| Placebo + Pioglitazone 45 | -2.83 |
| Alogliptin 12.5 + Pioglitazone 45 | -1.96 |
| Alogliptin 25 + Pioglitazone 45 | -3.09 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HDL cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 8
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -0.5 |
| Alogliptin 12.5 + Placebo | -0.1 |
| Alogliptin 25 + Placebo | 0.6 |
| Placebo + Pioglitazone 15 | 2.8 |
| Alogliptin 12.5 + Pioglitazone 15 | 2.3 |
| Alogliptin 25 + Pioglitazone 15 | 2.9 |
| Placebo + Pioglitazone 30 | 4.8 |
| Alogliptin 12.5 + Pioglitazone 30 | 4.2 |
| Alogliptin 25 + Pioglitazone 30 | 4.6 |
| Placebo + Pioglitazone 45 | 4.5 |
| Alogliptin 12.5 + Pioglitazone 45 | 5.7 |
| Alogliptin 25 + Pioglitazone 45 | 6.3 |
The change from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) at week 8. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HbA1c as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 8
| Intervention | percentage of glycosylated hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.30 |
| Alogliptin 12.5 + Placebo | -0.75 |
| Alogliptin 25 + Placebo | -0.80 |
| Placebo + Pioglitazone 15 | -0.50 |
| Alogliptin 12.5 + Pioglitazone 15 | -1.01 |
| Alogliptin 25 + Pioglitazone 15 | -1.04 |
| Placebo + Pioglitazone 30 | -0.57 |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -1.05 |
| Alogliptin 25 + Pioglitazone 30 | -1.02 |
| Placebo + Pioglitazone 45 mg | -0.76 |
| Alogliptin 12.5 + Pioglitazone 45 | -1.11 |
| Alogliptin 25 + Pioglitazone 45 | -1.20 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline proinsulin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 8
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | 0.7 |
| Alogliptin 12.5 + Placebo | 0.2 |
| Alogliptin 25 + Placebo | -2.6 |
| Placebo + Pioglitazone 15 | -3.8 |
| Alogliptin 12.5 + Pioglitazone 15 | -11.1 |
| Alogliptin 25 + Pioglitazone 15 | -10.7 |
| Placebo + Pioglitazone 30 | -8.8 |
| Alogliptin 12.5 + Pioglitazone 30 | -11.8 |
| Alogliptin 25 + Pioglitazone 30 | -9.4 |
| Placebo + Pioglitazone 45 | -9.0 |
| Alogliptin 12.5 + Pioglitazone 45 | -11.0 |
| Alogliptin 25 + Pioglitazone 45 | -13.8 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline fasting plasma glucose as covariates. (NCT00328627)
Timeframe: Baseline and Week 8
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 5.7 |
| Alogliptin 12.5 + Placebo | -19.5 |
| Alogliptin 25 + Placebo | -19.3 |
| Placebo + Pioglitazone 15 | -22.2 |
| Alogliptin 12.5 + Pioglitazone 15 | -42.3 |
| Alogliptin 25 + Pioglitazone 15 | -39.3 |
| Placebo + Pioglitazone 30 | -24.0 |
| Alogliptin 12.5 + Pioglitazone 30 | -40.5 |
| Alogliptin 25 + Pioglitazone 30 | -44.1 |
| Placebo + Pioglitazone 45 | -35.6 |
| Alogliptin 12.5 + Pioglitazone 45 | -44.0 |
| Alogliptin 25 + Pioglitazone 45 | -52.3 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline C-peptide as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 8
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | -0.044 |
| Alogliptin 12.5 + Placebo | 0.114 |
| Alogliptin 25 + Placebo | 0.108 |
| Placebo + Pioglitazone 15 | -0.221 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.315 |
| Alogliptin 25 + Pioglitazone 15 | -0.261 |
| Placebo + Pioglitazone 30 | -0.380 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.365 |
| Alogliptin 25 + Pioglitazone 30 | -0.207 |
| Placebo + Pioglitazone 45 | -0.467 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.300 |
| Alogliptin 25 + Pioglitazone 45 | -0.464 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline weight as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 8
| Intervention | kg (Least Squares Mean) |
|---|---|
| Placebo | -0.13 |
| Alogliptin 12.5 + Placebo | -0.05 |
| Alogliptin 25 + Placebo | -0.45 |
| Placebo + Pioglitazone 15 | 0.32 |
| Alogliptin 12.5 + Pioglitazone 15 | 0.09 |
| Alogliptin 25 + Pioglitazone 15 | 0.22 |
| Placebo + Pioglitazone 30 | 0.57 |
| Alogliptin 12.5 + Pioglitazone 30 | 0.49 |
| Alogliptin 25 + Pioglitazone 30 | 0.74 |
| Placebo + Pioglitazone 45 | 0.46 |
| Alogliptin 12.5 + Pioglitazone 45 | 0.43 |
| Alogliptin 25 + Pioglitazone 45 | 0.93 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline triglycerides as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 4
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -2.4 |
| Alogliptin 12.5 + Placebo | -2.2 |
| Alogliptin 25 + Placebo | -25.0 |
| Placebo + Pioglitazone 15 | -21.5 |
| Alogliptin 12.5 + Pioglitazone 15 | -35.8 |
| Alogliptin 25 + Pioglitazone 15 | -51.1 |
| Placebo + Pioglitazone 30 | -26.7 |
| Alogliptin 12.5 + Pioglitazone 30 | -42.2 |
| Alogliptin 25 + Pioglitazone 30 | -44.4 |
| Placebo + Pioglitazone 45 | -47.1 |
| Alogliptin 12.5 + Pioglitazone 45 | -39.2 |
| Alogliptin 25 + Pioglitazone 45 | -49.1 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline total cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 4
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 1.3 |
| Alogliptin 12.5 + Placebo | -3.8 |
| Alogliptin 25 + Placebo | -3.7 |
| Placebo + Pioglitazone 15 | 2.1 |
| Alogliptin 12.5 + Pioglitazone 15 | -2.3 |
| Alogliptin 25 + Pioglitazone 15 | -10.2 |
| Placebo + Pioglitazone 30 | 3.7 |
| Alogliptin 12.5 + Pioglitazone 30 | -7.2 |
| Alogliptin 25 + Pioglitazone 30 | -2.7 |
| Placebo + Pioglitazone 45 | -1.2 |
| Alogliptin 12.5 + Pioglitazone 45 | -3.6 |
| Alogliptin 25 + Pioglitazone 45 | -6.7 |
"The ratio of proinsulin to insulin was calculated as proinsulin (pmol/L) / insulin (μIU/mL).~Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline proinsulin/insulin ratio as continuous covariates." (NCT00328627)
Timeframe: Baseline and Week 4
| Intervention | ratio (Least Squares Mean) |
|---|---|
| Placebo | -0.015 |
| Alogliptin 12.5 + Placebo | -0.039 |
| Alogliptin 25 + Placebo | -0.058 |
| Placebo + Pioglitazone 15 | -0.029 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.054 |
| Alogliptin 25 + Pioglitazone 15 | -0.054 |
| Placebo + Pioglitazone 30 | -0.023 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.068 |
| Alogliptin 25 + Pioglitazone 30 | -0.045 |
| Placebo + Pioglitazone 45 | -0.009 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.111 |
| Alogliptin 25 + Pioglitazone 45 | -0.072 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline LDL cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 4
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 2.1 |
| Alogliptin 12.5 + Placebo | -2.4 |
| Alogliptin 25 + Placebo | 1.4 |
| Placebo + Pioglitazone 15 | 2.6 |
| Alogliptin 12.5 + Pioglitazone 15 | 1.6 |
| Alogliptin 25 + Pioglitazone 15 | -2.7 |
| Placebo + Pioglitazone 30 | 3.2 |
| Alogliptin 12.5 + Pioglitazone 30 | -2.8 |
| Alogliptin 25 + Pioglitazone 30 | 0.4 |
| Placebo + Pioglitazone 45 | 3.4 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.3 |
| Alogliptin 25 + Pioglitazone 45 | -3.4 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline insulin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 4
| Intervention | µIU/mL (Least Squares Mean) |
|---|---|
| Placebo | 1.06 |
| Alogliptin 12.5 + Placebo | -0.33 |
| Alogliptin 25 + Placebo | 2.31 |
| Placebo + Pioglitazone 15 | -1.68 |
| Alogliptin 12.5 + Pioglitazone 15 | -3.03 |
| Alogliptin 25 + Pioglitazone 15 | -1.86 |
| Placebo + Pioglitazone 30 | -2.43 |
| Alogliptin 12.5 + Pioglitazone 30 | -1.45 |
| Alogliptin 25 + Pioglitazone 30 | -2.05 |
| Placebo + Pioglitazone 45 | -2.76 |
| Alogliptin 12.5 + Pioglitazone 45 | -1.85 |
| Alogliptin 25 + Pioglitazone 45 | -2.65 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HDL cholesterol as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 4
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | -0.4 |
| Alogliptin 12.5 + Placebo | -0.6 |
| Alogliptin 25 + Placebo | -0.5 |
| Placebo + Pioglitazone 15 | 2.5 |
| Alogliptin 12.5 + Pioglitazone 15 | 1.6 |
| Alogliptin 25 + Pioglitazone 15 | 1.6 |
| Placebo + Pioglitazone 30 | 3.2 |
| Alogliptin 12.5 + Pioglitazone 30 | 2.3 |
| Alogliptin 25 + Pioglitazone 30 | 3.5 |
| Placebo + Pioglitazone 45 | 3.3 |
| Alogliptin 12.5 + Pioglitazone 45 | 4.2 |
| Alogliptin 25 + Pioglitazone 45 | 5.1 |
The change from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) at week 4. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline HbA1c as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 4
| Intervention | percentage of glycosylated hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.22 |
| Alogliptin 12.5 + Placebo | -0.46 |
| Alogliptin 25 + Placebo | -0.51 |
| Placebo + Pioglitazone 15 | -0.32 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.53 |
| Alogliptin 25 + Pioglitazone 15 | -0.61 |
| Placebo + Pioglitazone 30 | -0.24 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.60 |
| Alogliptin 25 + Pioglitazone 30 | -0.60 |
| Placebo + Pioglitazone 45 | -0.40 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.58 |
| Alogliptin 25 + Pioglitazone 45 | -0.63 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline proinsulin as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 4
| Intervention | pmol/L (Least Squares Mean) |
|---|---|
| Placebo | -0.1 |
| Alogliptin 12.5 + Placebo | -4.7 |
| Alogliptin 25 + Placebo | -2.3 |
| Placebo + Pioglitazone 15 | -4.8 |
| Alogliptin 12.5 + Pioglitazone 15 | -9.9 |
| Alogliptin 25 + Pioglitazone 15 | -8.9 |
| Placebo + Pioglitazone 30 | -6.7 |
| Alogliptin 12.5 + Pioglitazone 30 | -9.6 |
| Alogliptin 25 + Pioglitazone 30 | -9.5 |
| Placebo + Pioglitazone 45 | -7.2 |
| Alogliptin 12.5 + Pioglitazone 45 | -11.3 |
| Alogliptin 25 + Pioglitazone 45 | -11.7 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline fasting plasma glucose as covariates. (NCT00328627)
Timeframe: Baseline and Week 4
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 3.8 |
| Alogliptin 12.5 + Placebo | -20.4 |
| Alogliptin 25 + Placebo | -22.8 |
| Placebo + Pioglitazone 15 | -20.2 |
| Alogliptin 12.5 + Pioglitazone 15 | -35.3 |
| Alogliptin 25 + Pioglitazone 15 | -37.3 |
| Placebo + Pioglitazone 30 | -13.4 |
| Alogliptin 12.5 + Pioglitazone 30 | -37.4 |
| Alogliptin 25 + Pioglitazone 30 | -36.0 |
| Placebo + Pioglitazone 45 | -26.1 |
| Alogliptin 12.5 + Pioglitazone 45 | -37.8 |
| Alogliptin 25 + Pioglitazone 45 | -46.2 |
Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline C-peptide as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 4
| Intervention | ng/mL (Least Squares Mean) |
|---|---|
| Placebo | 0.002 |
| Alogliptin 12.5 + Placebo | -0.032 |
| Alogliptin 25 + Placebo | 0.076 |
| Placebo + Pioglitazone 15 | -0.246 |
| Alogliptin 12.5 + Pioglitazone 15 | -0.248 |
| Alogliptin 25 + Pioglitazone 15 | -0.238 |
| Placebo + Pioglitazone 30 | -0.232 |
| Alogliptin 12.5 + Pioglitazone 30 | -0.259 |
| Alogliptin 25 + Pioglitazone 30 | -0.268 |
| Placebo + Pioglitazone 45 | -0.393 |
| Alogliptin 12.5 + Pioglitazone 45 | -0.252 |
| Alogliptin 25 + Pioglitazone 45 | -0.337 |
The change from Baseline in VLDL/chylomicron triglyceride levels was assessed by NMR lipid fractionation. Least squares means are from an ANCOVA model with treatment and geographic region as class variables, and baseline metformin dose and baseline NMR VLDL/chylomicron triglycerides as continuous covariates. (NCT00328627)
Timeframe: Baseline and Week 26
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo | 11.9 |
| Alogliptin 12.5 + Placebo | 8.3 |
| Alogliptin 25 + Placebo | -7.0 |
| Placebo + Pioglitazone 15 | -20.4 |
| Alogliptin 12.5 + Pioglitazone 15 | -20.4 |
| Alogliptin 25 + Pioglitazone 15 | -23.8 |
| Placebo + Pioglitazone 30 | -8.2 |
| Alogliptin 12.5 + Pioglitazone 30 | -23.5 |
| Alogliptin 25 + Pioglitazone 30 | -18.9 |
| Placebo + Pioglitazone 45 | -10.4 |
| Alogliptin 12.5 + Pioglitazone 45 | -32.3 |
| Alogliptin 25 + Pioglitazone 45 | -26.2 |
The change from Baseline in fasting plasma glucose was assessed at weeks 1, 2, 4, 8, 12, 16, 20 and 26. Least Squares Means were from an ANCOVA model with treatment and geographic region as class variables and baseline plasma glucose as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 1, 2, 4, 8, 12, 16, 20 and 26.
| Intervention | mg/dL (Least Squares Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 1 (n=148, 146, 152, 151) | Week 2 (n=161, 156, 162, 159) | Week 4 (n=162, 157, 162, 161) | Week 8 (n=162, 157, 162, 162) | Week 12 (n=162, 157, 162, 162) | Week 16 (n=162, 157, 162, 162) | Week 20 (n=162, 157, 162, 162) | Week 26 (n=162, 157, 162, 162) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -23.3 | -30.9 | -39.7 | -48.4 | -49.3 | -46.6 | -47.5 | -48.5 |
| Alogliptin 25 mg | -14.6 | -16.7 | -26.7 | -29.0 | -29.5 | -26.9 | -28.3 | -25.8 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -26.6 | -33.5 | -41.4 | -50.4 | -51.9 | -52.7 | -54.0 | -50.2 |
| Pioglitazone 30 mg | -7.3 | -14.2 | -31.9 | -38.0 | -42.4 | -40.6 | -42.0 | -37.3 |
"The Homeostasis Model Assessment of insulin resistance (HOMA IR) measures insulin resistance based on fasting glucose and insulin measurements:~HOMA IR = fasting plasma insulin (µIU/mL) * fasting plasma glucose (mmol/L) / 22.5~A higher number indicates a greater degree of insulin resistance. The change from Baseline in HOMA IR was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline HOMA IR as a covariate." (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | insulin resistance (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=139, 132, 137, 143) | Week 26 (n=145, 134, 144, 148) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -3.877 | -3.508 |
| Alogliptin 25 mg | -0.814 | -1.353 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -2.905 | -3.646 |
| Pioglitazone 30 mg | -3.479 | -3.350 |
Change from Baseline in high-sensitivity C-Reactive Protein (hsCRP) was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline hsCRP as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | mg/L (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=147, 134, 138, 146) | Week 26 (n=153, 135, 144, 149) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -2.2771 | -1.9796 |
| Alogliptin 25 mg | -0.4497 | -0.1851 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -1.5346 | -1.9763 |
| Pioglitazone 30 mg | -1.7446 | -1.0391 |
C-peptide is a byproduct created when the hormone insulin is produced and is measured by a blood test. Change from Baseline was assessed at Weeks 4, 8, 12, 16, 20 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline C-peptide as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | ng/mL (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=142, 141, 141, 146) | Week 8 (n=158, 150, 153, 156) | Week 12 (n=158, 150, 154, 156) | Week 16 (n=158, 150, 154, 156) | Week 20 (n=158, 150, 154, 156) | Week 26 (n=158, 150, 154, 156) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -0.452 | -0.547 | -0.536 | -0.353 | -0.374 | -0.444 |
| Alogliptin 25 mg | 0.057 | 0.034 | -0.040 | 0.037 | -0.097 | -0.068 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -0.593 | -0.620 | -0.534 | -0.424 | -0.556 | -0.541 |
| Pioglitazone 30 mg | -0.551 | -0.606 | -0.612 | -0.604 | -0.623 | -0.577 |
Change from Baseline in body weight was assessed at Weeks 8, 12, 20 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and Baseline weight as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 8, 12, 20 and 26.
| Intervention | kg (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 8 (n=155, 146, 152, 151) | Week 12 (n=159, 147, 155, 154) | Week 20 (n=159, 147, 155, 154) | Week 26 (n=159, 147, 155, 154) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 0.70 | 1.22 | 1.86 | 2.51 |
| Alogliptin 25 mg | -0.34 | -0.78 | -0.47 | -0.29 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 0.82 | 1.35 | 2.36 | 3.14 |
| Pioglitazone 30 mg | 0.58 | 0.96 | 1.56 | 2.19 |
Change from Baseline in apolipoprotein C-III was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline apolipoprotein C-III as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | mg/dL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=140, 138, 138, 144) | Week 26 (n=149, 139, 147, 146) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -0.3 | -0.4 |
| Alogliptin 25 mg | -0.5 | -0.4 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -0.8 | -0.3 |
| Pioglitazone 30 mg | -0.3 | -0.2 |
Change from Baseline in apolipoprotein B was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline apolipoprotein B as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | mg/dL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=140, 138, 137, 143) | Week 26 (n=149, 139, 146, 146) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -5.9 | -6.4 |
| Alogliptin 25 mg | -4.0 | -2.5 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -9.8 | -7.9 |
| Pioglitazone 30 mg | -5.0 | -3.7 |
Change from Baseline in apolipoprotein A2 was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline apolipoprotein A2 as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | mg/dL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=140, 138, 137, 144) | Week 26 (n=149, 139, 146, 146) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 3.2 | 2.6 |
| Alogliptin 25 mg | -0.1 | -0.3 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 2.8 | 2.5 |
| Pioglitazone 30 mg | 3.4 | 2.9 |
Change from Baseline in Apolipoprotein A1 was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and Baseline apolipoprotein A1 as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | mg/dL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=140, 138, 137, 144) | Week 26 (n=149, 139, 146, 146) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 1.7 | 1.6 |
| Alogliptin 25 mg | -1.6 | -4.5 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 1.0 | 0.8 |
| Pioglitazone 30 mg | 2.3 | 1.2 |
Change from Baseline in adiponectin was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline adiponectin as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | μg/mL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=148, 137, 141, 147) | Week 26 (n=154, 137, 147, 149) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 7.50 | 7.16 |
| Alogliptin 25 mg | -0.28 | -0.09 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 8.10 | 6.85 |
| Pioglitazone 30 mg | 6.35 | 6.90 |
Clinical response at Week 26 was assessed by the percentage of participants with HbA1c ≤ 7.5%. (NCT00395512)
Timeframe: Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin 25 mg | 44.5 |
| Pioglitazone 30 mg | 55.8 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 72.0 |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 72.4 |
Clinical response at Week 26 was assessed by the percentage of participants with HbA1c ≤ 7%. (NCT00395512)
Timeframe: Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin 25 mg | 24.4 |
| Pioglitazone 30 mg | 33.7 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 62.8 |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 53.4 |
Clinical response at Week 26 was assessed by the percentage of participants with HbA1c ≤6.5%. (NCT00395512)
Timeframe: Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin 25 mg | 11.6 |
| Pioglitazone 30 mg | 16.6 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 27.4 |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 26.4 |
Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of ≥ 2.0%. (NCT00395512)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin 25 mg | 17.7 |
| Pioglitazone 30 mg | 19.6 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 34.1 |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 33.1 |
Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of ≥ 1.5%. (NCT00395512)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin 25 mg | 29.3 |
| Pioglitazone 30 mg | 33.1 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 57.3 |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 50.9 |
"The Homeostasis Model Assessment (HOMA) estimates steady state beta cell function (%B) as a percentage of a normal reference population.~HOMA %B = 20 * insulin (µIU/mL) / fasting plasma glucose (mmol/L) - 3.5~The change from Baseline in the homeostasis model assessment of beta cell function was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline HOMA beta cell function as a covariate." (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | percentage beta cell function (Least Squares Mean) | |
|---|---|---|
| Week 12 (n= 139, 132, 137, 143) | Week 26 (n=145, 134, 144, 148) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 22.134 | 24.887 |
| Alogliptin 25 mg | 15.133 | 10.472 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 30.266 | 39.153 |
| Pioglitazone 30 mg | 17.328 | 17.500 |
Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of ≥ 0.5%. (NCT00395512)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin 25 mg | 66.5 |
| Pioglitazone 30 mg | 70.6 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 89.6 |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 85.3 |
The change from Baseline to Week 26 in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound). (NCT00395512)
Timeframe: Baseline and Week 26
| Intervention | percentage of glycosylated hemoglobin (Least Squares Mean) |
|---|---|
| Alogliptin 25 mg | -0.96 |
| Pioglitazone 30 mg | -1.15 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -1.71 |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -1.56 |
The change from Baseline in fasting insulin was assessed at Weeks 4, 8, 12, 16, 20 and 26. Least Squares Means were from an ANCOVA model with treatment and geographic region as class variables and baseline insulin as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | μIU/mL (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=135, 133, 133, 145) | Week 8 (n=150, 142, 147, 155) | Week 12 (n=150, 142, 148, 155) | Week 16 (n=150, 142, 148, 155) | Week 20 (n=150, 142, 148, 155) | Week 26 (n=150, 142, 148, 155) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -4.27 | -4.86 | -4.65 | -2.73 | -3.06 | -3.72 |
| Alogliptin 25 mg | 0.43 | 0.93 | 0.29 | 0.26 | -1.02 | -0.47 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -4.67 | -4.75 | -2.98 | -3.65 | -4.61 | -3.86 |
| Pioglitazone 30 mg | -4.74 | -4.41 | -4.08 | -4.49 | -4.56 | -4.06 |
"The change from Baseline in levels of IDL particles was assessed by NMR fractionation at Weeks 12 and 26.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline IDL particles as a covariate." (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | nmol/L (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=139, 132, 132, 141) | Week 26 (n=147, 133, 141, 147) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -4.0 | -5.8 |
| Alogliptin 25 mg | -2.9 | 0.5 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -2.9 | -1.0 |
| Pioglitazone 30 mg | -1.0 | 2.1 |
Change from Baseline in high-density lipoprotein cholesterol (HDL-C) was assessed at Weeks 4, 8, 12, 16, 20 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline HDL cholesterol as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | mg/dL (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=146, 144, 142, 149) | Week 8 (n=160, 151, 154, 158) | Week 12 (n=160, 151, 155, 158) | Week 16 (n=160, 151, 155, 158) | Week 20 (n=160, 151, 155, 158) | Week 26 (n=160, 151, 155, 158) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 3.0 | 4.8 | 6.5 | 5.9 | 5.6 | 6.2 |
| Alogliptin 25 mg | -0.2 | 0.5 | 0.9 | 0.9 | 0.5 | 0.8 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 3.8 | 5.0 | 6.4 | 6.0 | 5.6 | 6.2 |
| Pioglitazone 30 mg | 3.0 | 4.7 | 6.0 | 5.2 | 4.7 | 5.7 |
"The change from Baseline in levels of total, large, medium-small, total small and very small LDL particles was assessed by NMR fractionation at Weeks 12 and 26.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline LDL particles as a covariate." (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | nmol/L (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Total Particles - Week 12 (n=139, 132, 132, 141) | Total Particles - Week 26 (n=147, 133, 141, 147) | Large Particles - Week 12 (n=139, 132, 132, 141) | Large Particles - Week 26 (n=147, 133, 141, 147) | Medium-Small - Week 12 (n=139, 132, 132, 141) | Medium-Small - Week 26 (n=147, 133, 141, 147) | Total Small - Week 12 (n=139, 132, 132, 141) | Total Small - Week 26 (n=147, 133, 141, 147) | Very Small - Week 12 (n=139, 132, 132, 141) | Very Small - Week 26 (n=147, 133, 141, 147) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -181.8 | -177.1 | 142.1 | 155.5 | -65.8 | -66.6 | -320.0 | -327.4 | -254.2 | -260.8 |
| Alogliptin 25 mg | -11.9 | 60.9 | 15.3 | 2.6 | -6.2 | 9.9 | -27.8 | 54.5 | -20.9 | 45.1 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -207.0 | -169.9 | 129.4 | 146.6 | -65.8 | -63.0 | -331.2 | -313.8 | -265.7 | -250.9 |
| Pioglitazone 30 mg | -104.1 | -75.6 | 98.8 | 120.4 | -41.4 | -40.1 | -200.3 | -195.8 | -159.2 | -156.0 |
Change from Baseline in low-density lipoprotein cholesterol (LDL-C) was assessed at Weeks 4, 8, 12, 16, 20 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline LDL cholesterol as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | mg/dL (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=137, 130, 135, 142) | Week 8 (n=152, 139, 147, 153) | Week 12 (n=154, 140, 148, 154) | Week 16 (n=154, 140, 148, 154) | Week 20 (n=154, 140, 148, 154) | Week 26 (n=154, 140, 148, 154) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -2.8 | 1.3 | 3.9 | 4.6 | 0.5 | 3.8 |
| Alogliptin 25 mg | -3.5 | -0.5 | 0.8 | 1.8 | 0.9 | 2.0 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 2.2 | 2.6 | 1.4 | 5.3 | 2.1 | 4.6 |
| Pioglitazone 30 mg | 2.8 | 7.6 | 5.8 | 6.6 | 7.4 | 8.1 |
Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of ≥ 1%. (NCT00395512)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin 25 mg | 43.3 |
| Pioglitazone 30 mg | 54.6 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 75.6 |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 68.1 |
Change from Baseline in mean HDL particle size was assessed by NMR lipid fractionation at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline mean HDL particle size as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | nm (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=139, 132, 132, 141) | Week 26 (n=147, 133, 141, 147) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 0.15 | 0.14 |
| Alogliptin 25 mg | -0.02 | -0.03 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 0.17 | 0.15 |
| Pioglitazone 30 mg | 0.09 | 0.08 |
Change from Baseline in mean LDL particle size was assessed by NMR lipid fractionation at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline mean LDL particle size as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | nm (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=139, 132, 132, 141) | Week 26 (n=147, 133, 141, 147) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 0.58 | 0.61 |
| Alogliptin 25 mg | 0.09 | -0.02 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 0.63 | 0.65 |
| Pioglitazone 30 mg | 0.44 | 0.44 |
Change from Baseline in mean VLDL particle size was assessed by NMR lipid fractionation at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline mean VLDL particle size as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | nm (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=139, 132, 132, 141) | Week 26 (n=147, 133, 141, 147) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -2.85 | -2.80 |
| Alogliptin 25 mg | -0.97 | 0.30 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -2.92 | -4.21 |
| Pioglitazone 30 mg | -3.97 | -3.71 |
Nuclear Magnetic Resonance (NMR) lipid fractionation was used to assess the change from Baseline in total triglyceride levels at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline NMR total triglycerides as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | mg/dL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=139, 132, 132, 141) | Week 26 (n=147, 133, 141, 147) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -23.7 | -22.6 |
| Alogliptin 25 mg | -14.9 | -7.6 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -39.7 | -28.8 |
| Pioglitazone 30 mg | -25.0 | -20.2 |
Change from Baseline in plasminogen activator inhibitor-1 was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline plasminogen activator inhibitor-1 as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | ng/mL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=136, 127, 131, 133) | Week 26 (n=145, 129, 142, 137) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -11.87 | -8.38 |
| Alogliptin 25 mg | -1.58 | 1.71 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -9.63 | -7.14 |
| Pioglitazone 30 mg | -4.23 | -5.45 |
Marked Hyperglycemia is defined as fasting plasma glucose greater than or equal to 200 mg/dL. Study week windows are defined to place hyperglycemia into visit categories. (NCT00395512)
Timeframe: Weeks 1, 2, 4, 8, 12, 16, 20 and 26.
| Intervention | percentage of participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Week 1 to < Week 4 (n=162, 157, 162, 161) | Week 4 to < Week 8 (n=153, 147, 148, 147) | Week 8 to < Week 12 (n=151, 146, 152, 146) | Week 12 to < Week 16 (n=153, 141, 148, 139) | Week 16 to < Week 20 (n=142, 135, 144, 131) | Week 20 to Week 26 (n=130, 132, 143, 128) | Overall (n=162, 157, 162, 162) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 28.6 | 14.3 | 8.2 | 7.9 | 6.9 | 6.3 | 30.9 |
| Alogliptin 25 mg | 31.5 | 19.0 | 15.2 | 16.3 | 16.2 | 17.7 | 44.4 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 18.5 | 10.8 | 7.2 | 8.1 | 2.8 | 10.5 | 25.3 |
| Pioglitazone 30 mg | 31.8 | 15.0 | 11.6 | 9.2 | 14.8 | 11.4 | 38.2 |
"Rescue was defined as meeting 1 of the following criteria, confirmed by a 2nd sample drawn within 5 days after the first sample and analyzed by the central laboratory:~After more than 4 weeks of treatment but prior to the Week 8 Visit: a single fasting plasma glucose ≥310 mg/dL (≥17.5 mmol/L);~From the Week 8 Visit but prior to the Week 12 Visit: a single fasting plasma glucose ≥275 mg/dL (≥15.27 mmol/L);~From the Week 12 Visit through the End-of-Treatment Visit: HbA1c ≥8.5% and ≤0.5% reduction in HbA1c as compared with the Baseline HbA1c." (NCT00395512)
Timeframe: Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Week 4 to < Week 8 (n=160, 156, 161, 160) | Week 8 to < Week 12 (n=158, 151, 157, 153) | Week 12 to < Week 16 (n=156, 145, 153, 144) | Week 16 to < Week 20 (n=150, 138, 149, 134) | Week 20 to Week 26 (n=132, 133, 146, 130) | Overall (n=160, 156, 161, 160) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 0.6 | 0 | 2.1 | 1.5 | 0 | 3.8 |
| Alogliptin 25 mg | 0 | 1.3 | 2.6 | 7.3 | 0.8 | 11.3 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 0 | 0 | 1.3 | 0 | 1.4 | 2.5 |
| Pioglitazone 30 mg | 0 | 0 | 3.4 | 2.2 | 1.5 | 6.4 |
The ratio of proinsulin to insulin was calculated as proinsulin (pmol/L) / insulin (μIU/mL) at weeks 4, 8, 12, 16, 20 and 26 relative to the Baseline value. Least squares means were from an ANCOVA model with treatment and geographic region as class variables and Baseline proinsulin/insulin ratio as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | ratio (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=135, 133, 133, 145) | Week 8 (n=149, 142, 146, 155) | Week 12 (n=149, 142, 147, 155) | Week 16 (n=149, 142, 147, 155) | Week 20 (n=149, 142, 147, 155) | Week 26 (n=149, 142, 147, 155) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -0.056 | -0.102 | -0.095 | -0.090 | -0.119 | -0.102 |
| Alogliptin 25 mg | -0.073 | -0.041 | -0.062 | -0.049 | -0.057 | -0.051 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -0.080 | -0.094 | -0.123 | -0.115 | -0.124 | -0.107 |
| Pioglitazone 30 mg | -0.047 | -0.085 | -0.098 | -0.081 | -0.076 | -0.076 |
Change from Baseline in total cholesterol level was assessed at Weeks 4, 8, 12, 16, 20 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline total cholesterol as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | mg/dL (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=146, 144, 142, 149) | Week 8 (n=160, 151, 154, 158) | Week 12 (n=160, 151, 155, 158) | Week 16 (n=160, 151, 155, 158) | Week 20 (n=160, 151, 155, 158) | Week 26 (n=160, 151, 155, 158) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -5.3 | -1.2 | 4.4 | 4.7 | -0.6 | 4.0 |
| Alogliptin 25 mg | -8.5 | -5.4 | -4.0 | -4.3 | -2.9 | -0.5 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -0.4 | -0.3 | -0.6 | 3.8 | -0.3 | 3.7 |
| Pioglitazone 30 mg | 0.9 | 7.2 | 4.9 | 4.6 | 4.5 | 6.5 |
Change from Baseline in triglycerides was assessed at Weeks 4, 8, 12, 16, 20 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline triglycerides as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | mg/dL (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=146, 144, 142, 149) | Week 8 (n=160, 151, 154, 158) | Week 12 (n=160, 151, 155, 158) | Week 16 (n=160, 151, 155, 158) | Week 20 (n=160, 151, 155, 158) | Week 26 (n=160, 151, 155, 158) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -32.1 | -51.9 | -45.4 | -43.9 | -46.5 | -43.1 |
| Alogliptin 25 mg | -28.2 | -34.8 | -36.4 | -44.5 | -29.9 | -24.7 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -51.7 | -61.6 | -64.3 | -54.6 | -59.3 | -56.2 |
| Pioglitazone 30 mg | -43.2 | -38.2 | -47.9 | -48.3 | -46.6 | -46.6 |
"The change from Baseline in levels of total VLDL/chylomicron particles and large VLDL/chylomicron particles was assessed by NMR lipid fractionation at Weeks 12 and 26.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline VLDL/chylomicron particles as a covariate." (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | nmol/L (Least Squares Mean) | |||
|---|---|---|---|---|
| Total Particles - Week 12 (n=139, 132, 132, 141) | Total Particles - Week 26 (n=147, 133, 141, 147) | Large Particles - Week 12 (n=139, 132, 132, 141) | Large Particles - Week 26 (n=147, 133, 141, 147) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -2.67 | -1.17 | -2.06 | -2.11 |
| Alogliptin 25 mg | -6.59 | -4.97 | -0.94 | -0.18 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -9.63 | -0.73 | -2.63 | -2.37 |
| Pioglitazone 30 mg | 0.70 | 4.94 | -1.83 | -1.96 |
"The change from Baseline in levels of VLDL/chylomicron triglycerides was assessed by NMR lipid fractionation at Weeks 12 and 26.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline VLDL/chylomicron triglycerides as a covariate." (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | mg/dL (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=139, 132, 132, 141) | Week 26 (n=147, 133, 141, 147) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -24.2 | -23.3 |
| Alogliptin 25 mg | -14.4 | -8.2 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -39.5 | -29.7 |
| Pioglitazone 30 mg | -25.6 | -22.0 |
"The change from Baseline in levels of medium VLDL particles and small VLDL particles was assessed by NMR fractionation at Weeks 12 and 26.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline VLDL particles as a covariate." (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | nmol/L (Least Squares Mean) | |||
|---|---|---|---|---|
| Medium Particles - Week 12 (n=139, 132, 132, 141) | Medium Particles - Week 26 (n=147, 133, 141, 147) | Small Particles - Week 12 (n=139, 132, 132, 141) | Small Particles - Week 26 (n=147, 133, 141, 147) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -4.69 | -3.58 | 3.71 | 4.36 |
| Alogliptin 25 mg | -3.20 | -0.23 | -1.74 | -4.11 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -8.52 | -3.76 | 1.18 | 5.22 |
| Pioglitazone 30 mg | -2.30 | -0.39 | 4.77 | 7.16 |
Proinsulin is a precursor to insulin, and was measured as an indicator of pancreatic function. The change from Baseline in fasting proinsulin was assessed at Weeks 4, 8, 12, 16, 20 and 26. Least Squares Means were from an ANCOVA model with treatment and geographic region as class variables and baseline proinsulin as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26.
| Intervention | pmol/L (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=136, 134, 135, 145) | Week 8 (n=150, 143, 146, 155) | Week 12 (n=150, 143, 147, 155) | Week 16 (n=150, 143, 147, 155) | Week 20 (n=150, 143, 147, 155) | Week 26 (n=150, 143, 147, 155) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -12.3 | -17.7 | -16.7 | -13.1 | -15.5 | -15.1 |
| Alogliptin 25 mg | -4.9 | -3.7 | -5.9 | -3.4 | -8.1 | -4.8 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -16.0 | -18.2 | -18.6 | -16.0 | -19.8 | -18.3 |
| Pioglitazone 30 mg | -12.1 | -14.9 | -16.0 | -16.3 | -16.1 | -13.2 |
Change from Baseline in free fatty acids (FFA) was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline free fatty acid as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | mmol/L (Least Squares Mean) | |
|---|---|---|
| Week 12 (n=148, 136, 140, 147) | Week 26 (n=154, 136, 147, 150) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -0.0805 | -0.1013 |
| Alogliptin 25 mg | -0.0404 | -0.0429 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -0.1061 | -0.0881 |
| Pioglitazone 30 mg | -0.0990 | -0.0680 |
The change from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) at 4 week intervals during the study. Least Squares Means were from an Analysis of Covariance (ANCOVA) model with treatment and geographic region as class variables and baseline HbA1c as a covariate. (NCT00395512)
Timeframe: Baseline and Weeks 4, 8, 12, 16 and 20.
| Intervention | percentage of glycosylated hemoglobin (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Week 4 (n=145, 146, 144, 150) | Week 8 (n=160, 153, 158, 158) | Week 12 (n=160, 153, 158, 158) | Week 16 (n=160, 153, 158, 158) | Week 20 (n=160, 153, 158, 158) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | -0.51 | -1.03 | -1.34 | -1.43 | -1.54 |
| Alogliptin 25 mg | -0.55 | -0.84 | -0.98 | -1.01 | -1.00 |
| Alogliptin 25 mg + Pioglitazone 30 mg | -0.62 | -1.19 | -1.57 | -1.67 | -1.72 |
| Pioglitazone 30 mg | -0.30 | -0.72 | -1.04 | -1.17 | -1.20 |
"The change from Baseline in levels of total, large, medium and small HDL particles was assessed by NMR fractionation at Weeks 12 and 26.~Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline HDL particles as a covariate." (NCT00395512)
Timeframe: Baseline and Weeks 12 and 26.
| Intervention | µmol/L (Least Squares Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Total Particles - Week 12 (n=139, 132, 132, 141) | Total Particles - Week 26 (n=147, 133, 141, 147) | Large Particles - Week 12 (n=139, 132, 132, 141) | Large Particles - Week 26 (n=147, 133, 141, 147) | Medium Particles - Week 12 (n=139, 132, 132, 141) | Medium Particles - Week 26 (n=147, 133, 141, 147) | Small Particles - Week 12 (n=139, 132, 132, 141) | Small Particles - Week 26 (n=147, 133, 141, 147) | |
| Alogliptin 12.5 mg + Pioglitazone 30 mg | 0.54 | 1.03 | 1.31 | 1.31 | 1.61 | 1.30 | -2.42 | -1.63 |
| Alogliptin 25 mg | 0.18 | 0.81 | 0.07 | -0.06 | -0.26 | -0.26 | 0.50 | 1.24 |
| Alogliptin 25 mg + Pioglitazone 30 mg | 0.11 | 1.01 | 0.98 | 1.24 | 1.60 | 1.19 | -2.65 | -1.58 |
| Pioglitazone 30 mg | 0.92 | 1.67 | 0.99 | 1.14 | 0.72 | 0.95 | -0.68 | -0.28 |
"Rescue was defined as meeting 1 of the following criteria, confirmed by a 2nd sample drawn within 7 days after the first sample and analyzed by the central laboratory:~After more than 2 weeks of treatment but prior to the Week 4 Visit: A single fasting plasma glucose (FPG) ≥275 mg/dL;~From the Week 4 Visit but prior to the Week 8 Visit: A single FPG ≥250 mg/dL;~From the Week 8 Visit but prior to the Week 12 Visit: A single FPG ≥225 mg/dL;~From the Week 12 Visit through the End-of-Treatment Visit: HbA1c ≥8.5% AND ≤0.5% reduction in HbA1c as compared with the baseline HbA1c." (NCT00432276)
Timeframe: Baseline to Week 52
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 10.9 |
| Pioglitazone 45 mg + Metformin | 21.7 |
Marked Hyperglycemia is defined as fasting plasma glucose greater than or equal to 200 mg/dL (11.10 mmol/L). (NCT00432276)
Timeframe: Baseline to Week 52
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 27.3 |
| Pioglitazone 45 mg + Metformin | 36.1 |
Change from Baseline in adiponectin was assessed at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline adiponectin as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | μg/mL (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=355, 361) | Week 26 (n=366, 371) | Week 42 (n=367, 371) | Week 52 (n=367, 371) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 1.15 | 1.17 | -0.41 | -0.70 |
| Pioglitazone 45 mg + Metformin | 2.97 | 4.19 | 3.04 | 2.21 |
Change from Baseline in Apolipoprotein A1 was assessed at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein A1 as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | mg/dL (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=348, 355) | Week 26 (n=359, 363) | Week 42 (n=360, 363) | Week 52 (n=360, 363) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 0.5 | 0.1 | -2.1 | -4.5 |
| Pioglitazone 45 mg + Metformin | 0.0 | -0.9 | -2.2 | -4.4 |
Change from Baseline in Apolipoprotein A2 was assessed at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein A2 as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | mg/dL (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=348, 355) | Week 26 (n=359, 363) | Week 42 (n=360, 363) | Week 52 (n=360, 363) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -0.4 | 0.4 | 0.8 | 0.3 |
| Pioglitazone 45 mg + Metformin | 0.6 | 0.7 | 1.1 | 1.0 |
Change from Baseline in Apolipoprotein B was assessed at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein B as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | mg/dL (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 [N=348, 355] | Week 26 [N=359, 363] | Week 42 [N=360, 363] | Week 52 [N=360, 363] | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -3.1 | -0.6 | -0.4 | -1.2 |
| Pioglitazone 45 mg + Metformin | 0.1 | 1.1 | 1.8 | 1.7 |
Change from Baseline in Apolipoprotein C-III was assessed at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline apolipoprotein C-III as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | mg/dL (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=352, 361) | Week 26 (n=365, 369) | Week 42 (n=366, 369) | Week 52 (n=366, 369) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -0.6 | -0.1 | -0.3 | -0.5 |
| Pioglitazone 45 mg + Metformin | 0.1 | 0.2 | 0.2 | 0.0 |
Change from Baseline in body weight was assessed at Weeks 4, 8, 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline body weight as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 4, 8, 12, 26, 42 and 52.
| Intervention | kg (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=354, 344) | Week 8 (n=394, 394 | Week 12 (n=395, 394) | Week 26 (n=395, 394) | Week 42 (n=395, 394) | Week 52 (n=395, 394) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 0.18 | 0.31 | 0.35 | 0.73 | 1.09 | 1.10 |
| Pioglitazone 45 mg + Metformin | 0.32 | 0.51 | 0.64 | 0.97 | 1.52 | 1.60 |
C-peptide is a byproduct created when the hormone insulin is produced and is measured by a blood test. Change from Baseline was assessed at Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline fasting C-peptide as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52.
| Intervention | ng/mL (Least Squares Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Week 4 (n=349, 333) | Week 8 (n=393, 389) | Week 12 (n=394, 390) | Week 16 (n=395, 390) | Week 20 (n=395, 390) | Week 26 (n=395, 390) | Week 34 (n=395, 390) | Week 42 (n=395, 390) | Week 52 (n=395, 390) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 0.110 | 0.074 | 0.070 | 0.064 | 0.104 | 0.102 | 0.118 | 0.140 | 0.182 |
| Pioglitazone 45 mg + Metformin | -0.033 | -0.038 | 0.030 | 0.010 | -0.001 | -0.013 | 0.003 | 0.037 | 0.108 |
"The Homeostasis Model Assessment (HOMA) estimates steady state beta cell function (%B) as a percentage of a normal reference population.~HOMA %B = 20 * insulin (µIU/mL) / fasting plasma glucose (mmol/L) - 3.5~The change from Baseline in the homeostasis model assessment of beta cell function was assessed at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline HOMA beta cell function as covariates." (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | percentage beta cell function (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=380, 377) | Week 26 (n=381, 377) | Week 42 (n=381, 377) | Week 52 (n=381, 377) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 14.770 | 30.012 | 15.397 | 15.020 |
| Pioglitazone 45 mg + Metformin | 4.580 | 3.242 | 2.400 | 2.057 |
"The Homeostasis Model Assessment of insulin resistance (HOMA IR) measures insulin resistance based on fasting glucose and insulin measurements:~HOMA IR = fasting plasma insulin (µIU/mL) * fasting plasma glucose (mmol/L) / 22.5~A higher number indicates a greater degree of insulin resistance. The change from Baseline in HOMA IR was assessed at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline HOMA insulin resistance as covariates." (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | insulin resistance (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=380, 378) | Week 26 (n=381, 378) | Week 42 (n=381, 378) | Week 52 (n=381, 378) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 0.007 | 0.336 | 0.200 | 0.353 |
| Pioglitazone 45 mg + Metformin | 0.350 | 0.312 | 0.431 | 0.541 |
The change from Baseline in fasting insulin was assessed at Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52. Least Squares Means were from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline fasting insulin as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52.
| Intervention | μIU/mL (Least Squares Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Week 4 (n=344, 328) | Week 8 (n=382, 378) | Week 12 (n=382, 378) | Week 16 (n=383, 378) | Week 20 (n=383, 378) | Week 26 (n=383, 378) | Week 34 (n=383, 378) | Week 42 (n=383, 378) | Week 52 (n=383, 378) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 0.53 | 0.72 | 1.21 | 1.19 | 1.60 | 1.94 | 1.41 | 1.79 | 1.91 |
| Pioglitazone 45 mg + Metformin | -0.54 | 0.05 | 1.22 | 0.56 | 0.38 | 0.88 | 0.83 | 1.10 | 1.18 |
The change from Baseline in fasting plasma glucose (FPG) was assessed at Weeks 2, 4, 8, 12, 16, 20, 26, 34, 42 and 52. Least Squares Means were from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline FPG as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16, 20, 26, 34, 42 and 52.
| Intervention | mg/dL (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Week 2 (n=360, 345) | Week 4 (n=397, 394) | Week 8 (n=399, 396) | Week 12 (n=399, 396) | Week 16 (n=399, 396) | Week 20 (n=399, 396) | Week 26 (n=399, 396) | Week 34 (n=399, 396) | Week 42 (n=399, 396) | Week 52 (n=399, 396) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -15.5 | -17.7 | -19.1 | -19.6 | -18.0 | -16.4 | -17.1 | -13.6 | -15.9 | -14.6 |
| Pioglitazone 45 mg + Metformin | -0.5 | -1.4 | -5.7 | -4.8 | -4.5 | -5.8 | -4.9 | -6.2 | -4.9 | -3.7 |
Proinsulin is a precursor to insulin, and was measured as an indicator of pancreatic function. The change from Baseline in fasting proinsulin was assessed at Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52. Least Squares Means were from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline fasting proinsulin as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52.
| Intervention | pmol/L (Least Squares Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Week 4 (n=342, 325) | Week 8 (n=380, 376) | Week 12 (n=380, 376) | Week 16 (n=381, 376) | Week 20 (n=381, 376) | Week 26 (n=381, 376) | Week 34 (n=381, 376) | Week 42 (n=381, 376) | Week 52 (n=381, 376) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -2.0 | -2.3 | -1.3 | -0.2 | -0.5 | 0.6 | 0.9 | -0.1 | -0.5 |
| Pioglitazone 45 mg + Metformin | -0.8 | -0.5 | 1.6 | 0.6 | 0.3 | 0.7 | 0.3 | 1.1 | 1.2 |
Clinical response at Weeks 26 and 52 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 1.5%. (NCT00432276)
Timeframe: Weeks 26 and 52.
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Week 26 | Week 52 | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 18.6 | 17.1 |
| Pioglitazone 45 mg + Metformin | 7.5 | 8.0 |
Change from Baseline in free fatty acids was assessed at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline free fatty acids as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42, and 52.
| Intervention | mmol/L (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=355, 360) | Week 26 (n=366, 368) | Week 42 (n=367, 368) | Week 52 (n=367, 368) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -0.0526 | -0.0364 | -0.0243 | -0.0294 |
| Pioglitazone 45 mg + Metformin | -0.0332 | -0.0162 | -0.0222 | 0.0019 |
Clinical response at Weeks 26 and 52 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 2.0%. (NCT00432276)
Timeframe: Weeks 26 and 52.
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Week 26 | Week 52 | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 8.2 | 7.9 |
| Pioglitazone 45 mg + Metformin | 3.0 | 3.3 |
Clinical response at Weeks 26 and 52 was assessed by the percentage of participants with HbA1c less than or equal to 6.5%. (NCT00432276)
Timeframe: Weeks 26 and 52.
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Week 26 | Week 52 | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 13.9 | 8.7 |
| Pioglitazone 45 mg + Metformin | 7.8 | 4.3 |
Clinical response at Weeks 26 and 52 was assessed by the percentage of participants with HbA1c less than or equal to 7%. (NCT00432276)
Timeframe: Weeks 26 and 52.
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Week 26 | Week 52 | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 39.1 | 33.2 |
| Pioglitazone 45 mg + Metformin | 25.8 | 21.3 |
Clinical response at Weeks 26 and 52 was assessed by the percentage of participants with HbA1c less than or equal to 7.5%. (NCT00432276)
Timeframe: Weeks 26 and 52.
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Week 26 | Week 52 | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 64.9 | 59.9 |
| Pioglitazone 45 mg + Metformin | 47.1 | 44.1 |
"The change from Baseline in levels of VLDL/chylomicron triglycerides was assessed by NMR lipid fractionation at Weeks 12, 26, 42 and 52.~Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline VLDL/chylomicron triglycerides as covariates." (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | mg/dL (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=357, 361) | Week 26 (n=367, 368) | Week 42 (n=367, 369) | Week 52 (n=367, 369) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -7.6 | -1.3 | -5.4 | -6.1 |
| Pioglitazone 45 mg + Metformin | -0.2 | 0.2 | 0.2 | -1.5 |
"The change from Baseline in levels of total VLDL/chylomicron particles and large VLDL/chylomicron particles was assessed by NMR lipid fractionation at Weeks 12, 26, 42 and 52.~Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline VLDL/chylomicron particles as covariates." (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | nmol/L (Least Squares Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Total Particles - Week 12 (n=357, 361) | Total Particles - Week 26 (n=367, 368) | Total Particles - Week 42 (n=367, 369) | Total Particles - Week 52 (n=367, 369) | Large Particles - Week 12 (n=357, 361) | Large Particles - Week 26 (n=367, 368) | Large Particles - Week 42 (n=367, 369) | Large Particles - Week 52 (n=367, 369) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -0.59 | 1.27 | -1.35 | -1.20 | -0.83 | -0.39 | -0.72 | -0.66 |
| Pioglitazone 45 mg + Metformin | 2.39 | 3.09 | 1.64 | 3.03 | -0.27 | -0.32 | -0.38 | -0.46 |
Change from Baseline in triglycerides was assessed at Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline triglycerides as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52.
| Intervention | mg/dL (Least Squares Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Week 4 (n=397, 393) | Week 8 (n=399, 395) | Week 12 (n=399, 395) | Week 16 (n=399, 395) | Week 20 (n=399, 395) | Week 26 (n=399, 395) | Week 34 (n=399, 395) | Week 42 (n=399, 395) | Week 52 (n=399, 395) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -16.4 | -17.9 | -16.1 | -16.3 | -12.7 | -11.9 | -7.4 | -14.6 | -16.4 |
| Pioglitazone 45 mg + Metformin | -12.2 | -12.3 | -4.5 | -9.4 | -8.5 | -6.3 | -8.1 | -7.0 | -7.8 |
Change from Baseline in total cholesterol was assessed at Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline total cholesterol as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52.
| Intervention | mg/dL (Least Squares Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Week 4 (n=397, 393) | Week 8 (n=399, 395) | Week 12 (n=399, 395) | Week 16 (n=399, 395) | Week 20 (n=399, 395) | Week 26 (n=399, 395) | Week 34 (n=399, 395) | Week 42 (n=399, 395) | Week 52 (n=399, 395) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -5.2 | -4.0 | -3.6 | -4.3 | -3.9 | -2.1 | -3.5 | -3.8 | -4.4 |
| Pioglitazone 45 mg + Metformin | -1.9 | 0.3 | 1.1 | -0.4 | -0.5 | 1.0 | -0.7 | 0.0 | -0.1 |
The ratio of proinsulin to insulin was calculated as proinsulin (pmol/L) / insulin (μIU/mL) at weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52 relative to the Baseline value. Least squares means were from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline fasting proinsulin/insulin ratio as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52.
| Intervention | ratio (Least Squares Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Week 4 (n=341, 325) | Week 8 (n=380, 375) | Week 12 (n=380, 375) | Week 16 (n=381, 375) | Week 20 (n=381, 375) | Week 26 (n=381, 375) | Week 34 (n=381, 375) | Week 42 (n=381, 375) | Week 52 (n=381, 375) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -0.046 | -0.049 | -0.053 | -0.044 | -0.037 | -0.036 | -0.038 | -0.047 | -0.048 |
| Pioglitazone 45 mg + Metformin | -0.005 | -0.001 | 0.004 | 0.002 | -0.004 | -0.015 | -0.004 | -0.010 | -0.007 |
Change from Baseline in plasminogen activator inhibitor-1 (PAI-1) was assessed at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline PAI-1 as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | ng/ml (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=322, 330) | Week 26 (n=342, 343) | Week 42 (n=346, 344) | Week 52 (n=346, 344) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -3.23 | -2.83 | -2.08 | -2.92 |
| Pioglitazone 45 mg + Metformin | -3.59 | -3.63 | -4.89 | -4.70 |
Change from Baseline in mean VLDL particle size was assessed by NMR lipid fractionation at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline mean VLDL particle size as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | nm (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=355, 361) | Week 26 (n=365, 368) | Week 42 (n=365, 369) | Week 52 (n=365, 369) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -0.67 | 0.11 | 0.44 | -0.12 |
| Pioglitazone 45 mg + Metformin | -0.79 | -0.87 | -0.79 | -1.04 |
Change from Baseline in mean LDL particle size was assessed by NMR lipid fractionation at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline mean LDL particle size as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | nm (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=357, 361) | Week 26 (n=367, 368) | Week 42 (n=367, 369) | Week 52 (n=367, 369) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 0.05 | 0.03 | -0.02 | -0.04 |
| Pioglitazone 45 mg + Metformin | 0.06 | 0.07 | 0.05 | 0.03 |
Change from Baseline in mean HDL particle size was assessed by NMR lipid fractionation at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline mean HDL particle size as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | nm (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=357, 361) | Week 26 (n=367, 368) | Week 42 (n=367, 369) | Week 52 (n=367, 369) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 0.04 | 0.04 | 0.02 | 0.03 |
| Pioglitazone 45 mg + Metformin | 0.05 | 0.07 | 0.07 | 0.08 |
Change from Baseline in low-density lipoprotein cholesterol (LDL-C) was assessed at Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline LDL cholesterol as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52.
| Intervention | mg/dL (Least Squares Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Week 4 (n=388, 383) | Week 8 (n=390, 386) | Week 12 (n=390, 386) | Week 16 (n=390, 386) | Week 20 (n=390, 386) | Week 26 (n=390, 386) | Week 34 (n=390, 386) | Week 42 (n=390, 386) | Week 52 (n=390, 386) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -2.4 | -0.6 | -1.2 | -1.7 | -2.0 | -0.6 | -1.9 | -1.6 | -1.9 |
| Pioglitazone 45 mg + Metformin | 0.0 | 2.1 | 1.4 | -0.1 | 0.1 | 1.6 | 1.2 | 0.7 | 1.0 |
The change from Baseline in levels of total, large, medium-small, total small and very small LDL particles was assessed by NMR fractionation at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline LDL particles as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | nmol/L (Least Squares Mean) | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Total Particles - Week 12 (n=357, 361) | Total Particles - Week 26 (n=367, 368) | Total Particles - Week 42 (n=367, 369) | Total Particles - Week 52 (n=367, 369) | Large Particles - Week 12 (n=357, 361) | Large Particles - Week 26 (n=367, 368) | Large Particles - Week 42 (n=367, 369) | Large Particles - Week 52 (n=367, 369) | Medium-small Particles - Week 12 (n=357, 361) | Medium-small Particles - Week 26 (n=367, 368) | Medium-small Particles - Week 42 (n=367, 369) | Medium-small Particles - Week 52 (n=367, 369) | Total Small Particles - Week 12 (n=357, 361) | Total Small Particles - Week 26 (n=367, 368) | Total Small Particles - Week 42 (n=367, 369) | Total Small Particles - Week 52 (n=367, 369) | Very Small Particles - Week 12 (n=357, 361) | Very Small Particles - Week 26 (n=367, 368) | Very Small Particles - Week 42 (n=367, 369) | Very Small Particles - Week 52 (n=367, 369) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -46.9 | -14.0 | -11.7 | -13.0 | -4.4 | 1.1 | -20.8 | -19.2 | -7.0 | -0.7 | 4.1 | 2.4 | -37.6 | -10.9 | 15.0 | 10.9 | -30.6 | -10.1 | 11.0 | 8.6 |
| Pioglitazone 45 mg + Metformin | -22.3 | -8.2 | -10.7 | -2.7 | -5.0 | 8.8 | 0.0 | -2.4 | -0.3 | -0.7 | 1.8 | 1.2 | -20.8 | -18.2 | -13.0 | -3.5 | -20.6 | -17.5 | -14.9 | -4.8 |
The change from Baseline in levels of IDL particles was assessed by NMR lipid fractionation at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline IDL particles as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | nmol/L (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=357, 361) | Week 26 (n=367, 368) | Week 42 (n=367, 369) | Week 52 (n=367, 369) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -4.9 | -4.1 | -5.6 | -4.5 |
| Pioglitazone 45 mg + Metformin | 3.2 | 1.0 | 2.0 | 3.2 |
Change from Baseline in high-sensitivity C-Reactive Protein (hsCRP) was assessed at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline hsCRP as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | mg/L (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=357, 366) | Week 26 (n=366, 373) | Week 42 (n=367, 373) | Week 52 (n=367, 373) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 0.2989 | -0.0632 | 0.7251 | 0.5875 |
| Pioglitazone 45 mg + Metformin | 0.7049 | 0.9706 | 0.6443 | 1.4085 |
Change from Baseline in high-density lipoprotein cholesterol (HDL-C) was assessed at Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline HDL cholesterol as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20, 26, 34, 42 and 52.
| Intervention | mg/dL (Least Squares Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Week 4 (n=397, 392) | Week 8 (n=399, 395) | Week 12 (n=399, 395) | Week 16 (n=399, 395) | Week 20 (n=399, 395) | Week 26 (n=399, 395) | Week 34 (n=399, 395) | Week 42 (n=399, 395) | Week 52 (n=395, 395) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -0.7 | -0.8 | -0.2 | -0.5 | -0.2 | 0.0 | -0.6 | -0.3 | -0.3 |
| Pioglitazone 45 mg + Metformin | 0.4 | 0.6 | 1.1 | 0.9 | 0.7 | 0.6 | 0.3 | 0.6 | 0.3 |
The change from Baseline in levels of total, large, medium and small HDL particles was assessed by NMR fractionation at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline HDL particles as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | μmol/L (Least Squares Mean) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Total Particles - Week 12 (n=357, 361) | Total Particles - Week 26 (n=367, 368) | Total Particles - Week 42 (n=367, 369) | Total Particles - Week 52 (n=367, 369) | Large Particles - Week 12 (n=357, 361) | Large Particles - Week 26 (n=367, 368) | Large Particles - Week 42 (n=367, 369) | Large Particles - Week 52 (n=367, 369) | Medium Particles - Week 12 (n=357, 361) | Medium Particles - Week 26 (n=367, 368) | Medium Particles - Week 42 (n=367, 369) | Medium Particles - Week 52 (n=367, 369) | Small Particles - Week 12 (n=357, 361) | Small Particles - Week 26 (n=367, 368) | Small Particles - Week 42 (n=367, 369) | Small Particles - Week 52 (n=367, 369) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -0.18 | 0.37 | 0.09 | 0.38 | 0.08 | 0.19 | 0.06 | 0.19 | 0.10 | 0.71 | 0.57 | 0.66 | -0.38 | -0.53 | -0.54 | -0.47 |
| Pioglitazone 45 mg + Metformin | -0.14 | 0.03 | -0.11 | 0.02 | 0.35 | 0.53 | 0.51 | 0.57 | 0.43 | 0.90 | 0.70 | 0.96 | -0.92 | -1.39 | -1.31 | -1.49 |
The change from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) during the study. Least Squares Means were from an Analysis of Covariance (ANCOVA) model with treatment, study schedule, and geographic region as class variables, and baseline metformin dose and baseline HbA1c as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20, 34 and 42.
| Intervention | percentage of glycosylated hemoglobin (Least Squares Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Change from Baseline at Week 4 (n=276, 277) | Change from Baseline at Week 8 (n=303, 306) | Change from Baseline at Week 12 (n=303, 306) | Change from Baseline at Week 16 (n=303, 306) | Change from Baseline at Week 20 (n=303, 306) | Change from Baseline at Week 34 (n=303, 306) | Change from Baseline at Week 42 (n=303, 306) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -0.42 | -0.71 | -0.85 | -0.91 | -0.91 | -0.82 | -0.80 |
| Pioglitazone 45 mg + Metformin | -0.15 | -0.27 | -0.35 | -0.43 | -0.45 | -0.37 | -0.36 |
The change from Baseline to Week 26 and Week 52 in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound). (NCT00432276)
Timeframe: Baseline and Weeks 26 and 52.
| Intervention | percentage of glycosylated hemoglobin (Least Squares Mean) | |
|---|---|---|
| Change from Baseline at Week 26 | Change from Baseline at Week 52 | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -0.89 | -0.70 |
| Pioglitazone 45 mg + Metformin | -0.42 | -0.29 |
Nuclear Magnetic Resonance (NMR) lipid fractionation was used to assess the change from Baseline in total triglyceride levels at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline NMR triglycerides as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | mg/dL (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=357, 361) | Week 26 (n=367, 368) | Week 42 (n=367, 369) | Week 52 (n=367, 369) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -8.7 | -1.7 | -6.4 | -6.9 |
| Pioglitazone 45 mg + Metformin | 0.2 | 0.8 | 0.7 | -0.7 |
The change from Baseline in levels of medium VLDL particles and small VLDL particles was assessed by NMR fractionation at Weeks 12, 26, 42 and 52. Least squares means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and baseline metformin dose and baseline VLDL particles as covariates. (NCT00432276)
Timeframe: Baseline and Weeks 12, 26, 42 and 52.
| Intervention | nmol/L (Least Squares Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Medium Particles - Week 12 (n=357, 361) | Medium Particles - Week 26 (n=367, 368) | Medium Particles - Week 42 (n=367, 369) | Medium Particles - Week 52 (n=367, 369) | Small Particles - Week 12 (n=357, 361) | Small Particles - Week 26 (n=367, 368) | Small Particles - Week 42 (n=367, 369) | Small Particles - Week 52 (n=367, 369) | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | -0.09 | 1.30 | 1.03 | 0.26 | -0.04 | 0.07 | -1.86 | -1.02 |
| Pioglitazone 45 mg + Metformin | 1.74 | 2.23 | 2.43 | 2.12 | 1.30 | 1.47 | -0.21 | 1.58 |
Clinical response at Weeks 26 and 52 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 0.5%. (NCT00432276)
Timeframe: Weeks 26 and 52.
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Week 26 | Week 52 | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 72.0 | 60.9 |
| Pioglitazone 45 mg + Metformin | 42.1 | 37.6 |
Clinical response at Weeks 26 and 52 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 1.0%. (NCT00432276)
Timeframe: Weeks 26 and 52.
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Week 26 | Week 52 | |
| Alogliptin 25 mg + Pioglitazone 30 mg + Metformin | 42.3 | 35.6 |
| Pioglitazone 45 mg + Metformin | 20.3 | 17.3 |
The change in postprandial C-peptide collected at each week indicated relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 4 and Week 16.
| Intervention | ng/mL (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Week 4: 1 hour postprandial (n=24; n=21; n=19) | Week 4: 2 hours postprandial (n=24; n=21; n=19) | Week 4: 3 hours postprandial (n=24; n=21; n=19) | Week 4: 4 hours postprandial (n=24; n=21; n=19) | Week 4: 8 hours postprandial (n=23; n=20; n=19) | Week 16: 1 hour postprandial (n=24; n=25; n=21) | Week 16: 2 hours postprandial (n=24; n=25; n=21) | Week 16: 3 hours postprandial (n=24; n=25; n=21) | Week 16: 4 hours postprandial (n=24; n=25; n=21) | Week 16: 8 hours postprandial (n=24; n=24; n=21) | |
| Alogliptin 25 mg QD | -0.300 | -0.011 | 0.116 | 0.393 | 0.421 | -1.021 | -1.006 | -0.712 | -0.068 | 0.588 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -1.199 | -1.379 | -1.230 | -1.173 | -0.911 | -0.646 | -1.055 | -1.269 | -1.515 | -0.761 |
| Placebo QD | -0.106 | 0.311 | 0.376 | 0.256 | -0.063 | -0.176 | -0.011 | 0.492 | 0.496 | 0.151 |
The change in postprandial (after eating a meal) incremental area under the plasma concentration-time curve from 0 to 8 hours (AUC (0-8h)) postdose at week 16 relative to baseline. (NCT00655863)
Timeframe: Baseline and Week 16.
| Intervention | mg.h/dL (Least Squares Mean) |
|---|---|
| Placebo QD | -39.728 |
| Alogliptin 25 mg QD | -346.957 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -293.439 |
The change in postprandial incremental area under the plasma concentration-time curve from 0 to 8 hours (AUC(0-8h)) postdose at week 4 relative to baseline. (NCT00655863)
Timeframe: Baseline and Week 4.
| Intervention | mg.h/dL (Least Squares Mean) |
|---|---|
| Placebo QD | -16.291 |
| Alogliptin 25 mg QD | -288.490 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -279.116 |
The change in adiponectin collected at each week indicated relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 4 and Week 16.
| Intervention | µg/mL (Least Squares Mean) | |
|---|---|---|
| Week 4: 5 minutes prior to meal (n=24;n=21; n=19) | Week 16: 5 minutes prior to meal (n=24;n=25;n=21) | |
| Alogliptin 25 mg QD | 0.000 | 0.000 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | 0.006 | 0.007 |
| Placebo QD | 0.001 | 0.000 |
The change in ICAM collected at each week indicated relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 4 and Week 16.
| Intervention | ng/mL (Least Squares Mean) | |
|---|---|---|
| Week 4: 5 minutes prior to meal (n=24;n=21; n=19) | Week 16: 5 minutes prior to meal (n=24; n=25;n=21) | |
| Alogliptin 25 mg QD | -0.294 | -4.140 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -23.810 | -16.556 |
| Placebo QD | -1.154 | -2.495 |
Postprandial changes over time at each week indicated relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 4 and Week 16.
| Intervention | pg/mL (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Week 4: 1 hour postprandial (n=24; n=21; n=19) | Week 4: 2 hours postprandial (n=24; n=21; n=19) | Week 4: 3 hours postprandial (n=24; n=21; n=19) | Week 4: 4 hours postprandial (n=24; n=20; n=18) | Week 4: 8 hours postprandial (n=22; n=20; n=19) | Week 16: 1 hour postprandial (n=24; n=25; n=21) | Week 16: 2 hours postprandial (n=24; n=25; n=21) | Week 16: 3 hours postprandial (n=24; n=25; n=21) | Week 16: 4 hours postprandial (n=24; n=24; n=21) | Week 16: 8 hours postprandial (n=24; n=25; n=21) | |
| Alogliptin 25 mg QD | -14.639 | -17.015 | -13.200 | -4.679 | -3.789 | -16.955 | -20.949 | -13.602 | -8.577 | -5.818 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -17.704 | -22.081 | -15.987 | -8.860 | -5.150 | -17.462 | -20.662 | 10.84 | -10.326 | -9.332 |
| Placebo QD | 7.222 | 1.730 | 6.637 | 2.021 | 1.081 | 3.318 | -1.047 | 4.842 | 2.801 | 3.917 |
The change in postprandial proinsulin collected at each week indicated relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 4 and Week 16.
| Intervention | pmol/L (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Week 4: 1 hour postprandial (n=24; n=21; n=19) | Week 4: 2 hours postprandial (n=24; n=21; n=19) | Week 4: 3 hours postprandial (n=24; n=21; n=19) | Week 4: 4 hours postprandial (n=24; n=21; n=19) | Week 4: 8 hours postprandial (n=23; n=21; n=19) | Week 16: 1 hour postprandial (n=24; n=25; n=21) | Week 16: 2 hours postprandial (n=24; n=25; n=21) | Week 16: 3 hours postprandial (n=24; n=25; n=21) | Week 16: 4 hours postprandial (n=24; n=25; n=21) | Week 16: 8 hours postprandial (n=24; n=25; n=21) | |
| Alogliptin 25 mg QD | -13.024 | -12.568 | -12.987 | -6.848 | -5.561 | -22.812 | -29.930 | -27.768 | -21.862 | -6.898 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -41.192 | -56.478 | -59.573 | -52.649 | -35.159 | -30.658 | -45.487 | -50.058 | -48.757 | -28.776 |
| Placebo QD | -4.555 | -0.208 | -6.735 | -6.496 | -5.082 | 2.081 | 3.336 | 5.863 | 8.671 | 6.935 |
Postprandial incremental area under the curve changes for very-low-density lipoprotein (VLDL) Apo B-48, VLDL Apo B 100, VLDL2 Apo B-48, VLDL2 Apo B 100, chylomicron Apo B-48, chylomicron Apo B 100, and intermediate density lipoprotein (IDL) Apo B-48, IDL Apo B 100, and triglyceride-rich remnant (TRR) lipoproteins from 0 to 8 hours postdose at week 4 and week 16 relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 4 and Week 16.
| Intervention | mg.h/dL (Least Squares Mean) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| VLDL apo B-48 Week 4 (n=19; n=12; n=15) | VLDL apo B-48 Week 16 (n=19; n=16; n=16) | VLDL apo B 100 Week 4 (n=19; n=12; n=15) | VLDL apo B 100 Week 16 (n=19; n=16; n=16) | VLDL2 apo B-48 Week 4 (n=19; n=12; n=15) | VLDL2 apo B-48 Week 16 (n=19; n=16; n=16) | VLDL2 apo B 100 Week 4 (n=19; n=12; n=15) | VLDL2 apo B 100 Week 16 (n=19; n=16; n=16) | Chylomicron apo B-48 Week 4 (n=19; n=12; n=14) | Chylomicron apo B-48 Week 16 (n=19; n=16; n=16) | Chylomicron apo B 100 Week 4(n=19; n=12; n=14) | Chylomicron apo B 100 Week 16 (n=19; n=16; n=16) | IDL apo B-48 Week 4 (n=18; n=10; n=13) | IDL apo B-48 Week 16 (n=18; n=14; n=14) | IDL apo B 100 Week 4 (n=18; n=10; n=13) | IDL apo B 100 Week 16 (n=18; n=14; n=14) | TRR lipoproteins Week 4 (n=24; n=21; n=19) | TRR lipoproteins Week 16 (n=24; n=25; n=21) | |
| Alogliptin 25 mg QD | -0.491 | -0.654 | -2.670 | -6.967 | -0.101 | -0.175 | 0.507 | -2.049 | -0.097 | -0.113 | -0.417 | -0.419 | -0.247 | -0.188 | -2.029 | -2.876 | -1.071 | -12.719 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -0.312 | -0.266 | -2.977 | -3.265 | -0.022 | 0.002 | -0.781 | -1.793 | -0.071 | -0.084 | -0.389 | -0.409 | -0.223 | 0.021 | -2.769 | 0.073 | -5.673 | -7.853 |
| Placebo QD | -0.020 | -0.055 | 0.568 | -0.453 | -0.075 | -0.079 | 0.464 | -1.155 | -0.051 | -0.051 | -0.123 | -0.120 | 0.002 | 0.151 | 0.952 | 4.181 | 16.147 | 2.818 |
The change in hs-CRP collected at each week indicated relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 4 and Week 16.
| Intervention | mg/L (Least Squares Mean) | |
|---|---|---|
| Week 4: 5 minutes prior to meal (n=24; n=21; n=19) | Week 16: 5 minutes prior to meal (n=24; n=25;n=21) | |
| Alogliptin 25 mg QD | 0.631 | -0.402 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | 0.155 | -0.402 |
| Placebo QD | -1.514 | 4.338 |
The change in VCAM collected at each week indicated relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 4 and Week 16.
| Intervention | ng/mL (Least Squares Mean) | |
|---|---|---|
| Week 4: 5 minutes prior to meal (n=24;n=21; n=19) | Week 16: 5 minutes prior to meal (n=24;n=25;n=21) | |
| Alogliptin 25 mg QD | 2.392 | -1.441 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | 4.849 | 13.665 |
| Placebo QD | -37.351 | 5.067 |
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 each week indicated relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 8 and Week 16.
| Intervention | percentage of glycosylated hemoglobin (Least Squares Mean) | |
|---|---|---|
| Week 8: fasting (n=23; n=24; n=20) | Week 16: 5 minutes prior to meal (n=24;n=25; n=21) | |
| Alogliptin 25 mg QD | -0.55 | -0.39 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -1.01 | -0.95 |
| Placebo QD | -0.12 | 0.38 |
The change in postprandial incremental area under the plasma concentration-time curve for very-low-density lipoprotein (VLDL) cholesterol, VLDL triglycerides, VLDL2 cholesterol, VLDL2 triglycerides, chylomicron cholesterol, chylomicron triglycerides, intermediate-density lipoprotein (IDL) cholesterol, and IDL triglycerides from 0 to 8 hours postdose at week 4 and week 16 relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 4 and Week 16.
| Intervention | mg.h/dL (Least Squares Mean) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| VLDL triglycerides Week 4 (n=23; n=21; n=19) | VLDL triglycerides Week 16 (n=23; n=25; n=21) | VLDL cholesterol Week 4 (n=23; n=21; n=19) | VLDL cholesterol Week 16 (n=23; n=25; n=21) | VLDL 2 triglycerides Week 4 (n=23; n=20; n=19) | VLDL 2 triglycerides Week 16 (n=23; n=25; n=21) | VLDL 2 cholesterol Week 4 (n=23; n=20; n=19) | VLDL 2 cholesterol Week 16 (n=23; n=25; n=21) | Chylomicron triglycerides Week 4 (n=23; n=21; n=1 | Chylomicron triglycerides Week 16(n=23;n=25; n=21) | Chylomicron cholesterol Week 4 (n=23; n=21; n=19) | Chylomicron cholesterol Week 16 (n=23; n=25; n=21) | IDL triglycerides Week 4 (n=22; n=18; n=17) | IDL triglycerides Week 16 (n=22; n=23; n=19) | IDL cholesterol Week 4 (n=22; n=18; n=17) | IDL cholesterol Week 16 (n=22; n=23; n=19) | |
| Alogliptin 25 mg QD | -119.009 | -130.459 | -14.760 | -16.365 | -17.960 | -18.986 | -0.709 | -1.445 | -115.093 | -136.626 | -4.474 | -5.566 | -6.771 | -4.045 | -0.808 | 0.249 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -98.758 | -85.709 | -10.760 | -8.747 | -8.687 | -23.061 | -1.073 | -1.232 | -108.036 | -129.991 | -3.628 | -4.289 | -4.410 | -4.533 | 0.195 | 0.609 |
| Placebo QD | -9.488 | 25.194 | -6.914 | -4.561 | -5.221 | -24.280 | -2.396 | -2.190 | 0.617 | -18.577 | -0.091 | -1.431 | 14.667 | -0.313 | 1.473 | 0.171 |
Postprandial changes over time at each week indicated relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 4 and Week 16.
| Intervention | uIU/mL (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Week 4: 1 hour postprandial (n=24; n=21; n=18) | Week 4: 2 hours postprandial (n=24; n=21; n=19) | Week 4: 3 hours postprandial (n=24; n=21; n=19) | Week 4: 4 hours postprandial (n=24; n=21; n=19) | Week 4: 8 hours postprandial (n=23; n=21; n=19) | Week 16: 1 hour postprandial (n=24; n=25; n=21) | Week 16: 2 hours postprandial (n=24; n=25; n=21) | Week 16: 3 hours postprandial (n=24; n=25; n=21) | Week 16: 4 hours postprandial (n=24; n=25; n=21) | Week 16: 8 hours postprandial (n=24; n=25; n=21) | |
| Alogliptin 25 mg QD | -5.867 | 3.161 | 0.652 | 5.092 | 2.685 | -14.368 | -9.528 | -9.848 | -4.753 | 3.163 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -18.287 | -28.700 | -18.842 | -12.891 | -6.000 | -12.162 | -24.777 | -23.025 | -19.329 | -6.107 |
| Placebo QD | -5.047 | 1.405 | 0.637 | 2.999 | -1.174 | -8.896 | -9.258 | 4.447 | 8.405 | 0.495 |
Postprandial changes over time at each week indicated relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 4 and Week 16.
| Intervention | mg/dL (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Week 4: 1 hour postprandial (n=24; n=21; n=19) | Week 4: 2 hours postprandial (n=23; n=21; n=19) | Week 4: 3 hours postprandial (n=24; n=21; n=18) | Week 4: 4 hours postprandial (n=24; n=21; n=19) | Week 4: 8 hours postprandial (n=22; n=21; n=19) | Week 16: 1 hour postprandial (n=24; n=25; n=21) | Week 16: 2 hours postprandial (n=23; n=25; n=21) | Week 16: 3 hours postprandial (n=24; n=25; n=20) | Week 16: 4 hours postprandial (n=24; n=25; n=21) | Week 16: 8 hours postprandial (n=24; n=25; n=21) | |
| Alogliptin 25 mg QD | -35.065 | -24.721 | -19.367 | -13.907 | -6.077 | -36.189 | -29.745 | -16.996 | -12.517 | -5.737 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -65.905 | -67.718 | -54.345 | -48.643 | -27.856 | -58.168 | -61.899 | -51.891 | -41.943 | -19.381 |
| Placebo QD | -5.957 | -4.049 | 3.200 | 2.930 | 0.046 | 11.867 | 17.324 | 18.379 | 10.849 | 3.266 |
Postprandial changes over time at each week indicated relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 4 and Week 16.
| Intervention | pmol/L (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Week 4: 1 hour postprandial (n=20; n=17; n=15) | Week 4: 2 hours postprandial (n=21; n=17; n=16) | Week 4: 3 hours postprandial (n=21; n=17; n=16) | Week 4: 4 hours postprandial (n=21; n=17; n=16) | Week 4: 8 hours postprandial (n=19; n=16; n=16) | Week 16: 1 hour postprandial (n=21 ; n=20; n=16) | Week 16: 2 hours postprandial (n=21; n=21; n=17) | Week 16: 3 hours postprandial (n=21; n=21; n=17) | Week 16: 4 hours postprandial (n=21; n=21; n=17) | Week 16: 8 hours postprandial (n=21; n=21; n=17) | |
| Alogliptin 25 mg QD | -5.48 | -2.93 | -2.08 | 2.86 | -0.38 | -4.10 | -3.75 | -2.25 | -1.88 | 0.03 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -4.88 | -6.41 | -3.61 | -0.84 | -0.72 | -3.63 | -3.75 | -3.17 | -1.83 | -1.48 |
| Placebo QD | 0.52 | 0.92 | 1.20 | 1.76 | -1.01 | -0.28 | -3.59 | -1.08 | -0.64 | -1.36 |
The change in fasting plasma glucose collected at each week indicated relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 4, Week 8 and Week 16.
| Intervention | mg/dL (Least Squares Mean) | ||
|---|---|---|---|
| Week 4 (n=24; n=20; n=19) | Week 8 (n=24; n=25; n=21) | Week 16 (n=24; n=25; n=21) | |
| Alogliptin 25 mg QD | -20.669 | -16.293 | -17.052 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -38.826 | -38.242 | -38.481 |
| Placebo QD | -4.141 | 4.864 | 11.869 |
Pulse wave tonometry performed before the meal and 2 hours postmeal using one recording consisting of 15 to 20 sequentially recorded radial artery waveforms collected at each assessment. (NCT00655863)
Timeframe: Baseline and Week 16.
| Intervention | mmHg (Least Squares Mean) | |
|---|---|---|
| Week 16: pre-meal (n=23;n=23;n=20) | Week 16: 2 hours postmeal (n=24;n=24;n=20) | |
| Alogliptin 25 mg QD | -4.7 | 0.1 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -4.2 | -1.3 |
| Placebo QD | -3.6 | -1.6 |
The change in e-Selectin collected at each week indicated relative to baseline. (NCT00655863)
Timeframe: Baseline, Week 4 and Week 16.
| Intervention | ng/mL (Least Squares Mean) | |
|---|---|---|
| Week 4: 5 minutes prior to meal (n=24;n=21; n=19) | Week 16: 5 minutes prior to meal (n=24; n=25;n=21) | |
| Alogliptin 25 mg QD | 0.116 | -1.671 |
| Alogliptin 25 mg QD + Pioglitazone 30 mg QD | -6.437 | -4.056 |
| Placebo QD | 1.041 | 1.488 |
The number of participants with a fasting plasma glucose value ≥ to 200 mg per dL during the 52 week study. (NCT00707993)
Timeframe: On Occurrence (up to 52 weeks).
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
Baseline to | Week 4 to | Week 8 to | Week 12 to | Week 16 to | Week 20 to | Week 26 to | Week 34 to | Week 42 to Week 52 | Overall | | |
| Alogliptin 25 mg QD | 30 | 11 | 12 | 11 | 5 | 2 | 3 | 2 | 9 | 50 |
| Glipizide 5 mg QD | 17 | 5 | 8 | 8 | 4 | 3 | 8 | 4 | 6 | 37 |
The percentage of participants with a value for the percentage of glycosylated hemoglobin (HbA1c; the percentage of hemoglobin that is bound to glucose) less than or equal to 6.5 and 7.0% during the 52 week study. (NCT00707993)
Timeframe: Baseline and Week 52.
| Intervention | percentage of participants (Number) | |
|---|---|---|
| HbA1c ≤6.5% | HbA1c ≤7.0% | |
| Alogliptin 25 mg QD | 22.3 | 48.8 |
| Glipizide 5 mg QD | 18.2 | 45.3 |
Percentage of participants with at least one hypoglycemic episode during 52 week study. (NCT00707993)
Timeframe: On occurrence (up to 52 weeks).
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin 25 mg QD | 5.4 |
| Glipizide 5 mg QD | 26.0 |
The change in the percentage of glycosylated hemoglobin (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) collected at week 52 or final visit and glycosylated hemoglobin collected at baseline. (NCT00707993)
Timeframe: Baseline and Week 52.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Alogliptin 25 mg QD | -0.14 |
| Glipizide 5 mg QD | -0.09 |
The change between the value of insulin collected at each week indicated including final visit relative to baseline. (NCT00707993)
Timeframe: Baseline, Week 12, Week 26, Week 42 and Week 52.
| Intervention | mcIU/mL (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=207; n=188) | Week 26 (n=210; n=194) | Week 42 (n=210; n=194) | Week 52 (n=210; n=194) | |
| Alogliptin 25 mg QD | -2.36 | -0.41 | -0.58 | -1.72 |
| Glipizide 5 mg QD | 0.84 | 3.03 | 1.53 | 3.15 |
The change in postprandial (after eating a meal) glucose levels at week 52 relative to baseline. Standard 2-hour postprandial glucose (PPG) tests performed following an overnight fast and evaluated right before and after a 120-minute (2-hour) timeframe relative to ingestion of a standard oral glucose drink. (NCT00707993)
Timeframe: Baseline and Week 52.
| Intervention | mg/dL (Least Squares Mean) | |
|---|---|---|
| Week 52 PPG level (n=109; n=93) | Week 52 PPG excursion (n=109; n=93) | |
| Alogliptin 25 mg QD | -5.80 | 1.82 |
| Glipizide 5 mg QD | 6.30 | 7.17 |
The change in body weight measured at each week indicated including final visit from baseline. (NCT00707993)
Timeframe: Baseline, Week 8, Week 12, Week 26, Week 42 and Week 52.
| Intervention | kg (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Week 8 (n=213; n=200) | Week 12 (n=215; n=203) | Week 26 (n=215; n=204) | Week 42 (n=215; n=204) | Week 52 (n=215; n=204) | |
| Alogliptin 25 mg QD | -0.42 | -0.52 | -0.68 | -0.72 | -0.62 |
| Glipizide 5 mg QD | 0.55 | 0.42 | 0.66 | 0.57 | 0.60 |
The change in the value of fasting plasma glucose collected at each week indicated including final visit relative to baseline. (NCT00707993)
Timeframe: Baseline, Week 2, Week 4, Week 8, Week 12, Week 16, Week 20, Week 26, Week 34, Week 42 and Week 52.
| Intervention | mg/dL (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Week 2 (n=196; n=199) | Week 4 (n=217; n=213) | Week 8 (n=217; n=214) | Week 12 (n=217; n=214) | Week 16 (n=217; n=214) | Week 20 (n=217; n=214) | Week 26 (n=217; n=214) | Week 34 (n=217; n=214) | Week 42 (n=217; n=214) | Week 52 (n=217; n=214) | |
| Alogliptin 25 mg QD | -3.8 | -7.7 | -8.9 | -10.2 | -7.9 | -9.8 | -7.9 | -5.4 | -3.6 | -2.4 |
| Glipizide 5 mg QD | -5.0 | -7.6 | -8.7 | -9.9 | -11.4 | -8.7 | -6.2 | -5.7 | -7.4 | -4.2 |
The change between the value of fasting proinsulin collected at each week indicated including final visit relative to baseline. (NCT00707993)
Timeframe: Baseline, Week 12, Week 26, Week 42 and Week 52.
| Intervention | pmol/L (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=207; n=186) | Week 26 (n=211; n=194) | Week 42 (n=211; n=194) | Week 52 (n=211; n=194) | |
| Alogliptin 25 mg QD | -6.0 | -4.6 | -4.6 | -4.9 |
| Glipizide 5 mg QD | 1.0 | 3.0 | 3.1 | 3.0 |
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 each week indicated including final visit relative to baseline. (NCT00707993)
Timeframe: Baseline, Week 4, Week 8, Week 12, Week 16, Week 20, Week 26, Week 34 and Week 42.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 4 (n=175; n=148) | Week 8 (n=180; n=161) | Week 12 (n=180; n=162) | Week 16 (n=180; n=162) | Week 20 (n=180; n=162) | Week 26 (n=180; n=162) | Week 34 (n=180; n=162) | Week 42 (n=180; n=162) | |
| Alogliptin 25 mg QD | -0.14 | -0.27 | -0.34 | -0.31 | -0.31 | -0.28 | -0.21 | -0.17 |
| Glipizide 5 mg QD | -0.11 | -0.23 | -0.25 | -0.32 | -0.27 | -0.25 | -0.21 | -0.17 |
The change between the high sensitivity C-reactive protein value collected at each week indicated including final visit from baseline. (NCT00707993)
Timeframe: Baseline, Week 12, Week 26, Week 42 and Week 52.
| Intervention | mg/L (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=209; n=192) | Week 26 (n=212; n=198) | Week 42 (n=212; n=198) | Week 52 (n=212; n=198) | |
| Alogliptin 25 mg QD | 0.45 | -0.02 | 0.33 | 0.01 |
| Glipizide 5 mg QD | 0.10 | 0.47 | 0.53 | 0.21 |
The change between the ratio value of proinsulin and insulin collected at each week indicated including final visit relative to baseline. (NCT00707993)
Timeframe: Baseline, Week 12, Week 26, Week 42 and Week 52.
| Intervention | ratio (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=206; n=185) | Week 26 (n=210; n=193) | Week 42 (n=210; n=193) | Week 52 (n=210; n=193) | |
| Alogliptin 25 mg QD | -0.288 | -0.253 | -0.289 | -0.155 |
| Glipizide 5 mg QD | 0.053 | 0.562 | 0.183 | -0.057 |
The change in high-density lipoprotein cholesterol measured at each week indicated including final visit from baseline. (NCT00707993)
Timeframe: Baseline, Week 8, Week 12, Week 26, Week 42 and Week 52.
| Intervention | mg/dL (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Week 8 (n=206; n=193) | Week 12 (n=212; n=201) | Week 26 (n=212; n=201) | Week 42 (n=212; n=201) | Week 52 (n=212; n=201) | |
| Alogliptin 25 mg QD | -0.1 | 0.4 | 1.7 | 1.4 | 0.8 |
| Glipizide 5 mg QD | 1.2 | 0.5 | 0.2 | 0.1 | 0.3 |
The change in low-density lipoprotein cholesterol measured at each week indicated including final visit from baseline. (NCT00707993)
Timeframe: Baseline, Week 8, Week 12, Week 26, Week 42 and Week 52.
| Intervention | mg/dL (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Week 8 (n=200; n=185) | Week 12 (n=208; n=195) | Week 26 (n=208; n=196) | Week 42 (n=208; n=197) | Week 52 (n=209; n=197) | |
| Alogliptin 25 mg QD | -3.2 | -2.0 | 3.1 | 1.2 | 0.9 |
| Glipizide 5 mg QD | -2.8 | -2.4 | -1.1 | -0.8 | -1.4 |
The change in total cholesterol measured at each week indicated including final visit from baseline. (NCT00707993)
Timeframe: Baseline, Week 8, Week 12, Week 26, Week 42 and Week 52.
| Intervention | mg/dL (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Week 8 (n=208; n=195) | Week 12 (n=213; n=201) | Week 26 (n=213; n=201) | Week 42 (n=213; n=201) | Week 52 (n=213; n=201) | |
| Alogliptin 25 mg QD | -5.6 | -4.2 | 1.6 | 0.2 | -0.8 |
| Glipizide 5 mg QD | -1.6 | -0.7 | 0.1 | 0.1 | -0.5 |
The change in triglycerides measured at each week indicated including final visit from baseline. (NCT00707993)
Timeframe: Baseline, Week 8, Week 12, Week 26, Week 42 and Week 52.
| Intervention | mg/dL (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Week 8 (n=208; n=195) | Week 12 (n=213; n=201) | Week 26 (n=213; n=201) | Week 42 (n=213; n=201) | Week 52 (n=213; n=201) | |
| Alogliptin 25 mg QD | -12.8 | -15.5 | -16.3 | -12.6 | -13.2 |
| Glipizide 5 mg QD | 2.7 | 7.5 | 3.9 | 5.5 | 1.9 |
The change between homeostasis model assessment of beta cell function collected at each week indicated including final visit relative to baseline. Homeostasis model assessment of beta cell function measures beta cell function, calculated by a constant (20) times insulin, divided by fasting plasma glucose minus a constant (3.5). (NCT00707993)
Timeframe: Baseline, Week 12, Week 26, Week 42 and Week 52.
| Intervention | percent score of beta cell function (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 12 (n=203; n=184) | Week 26 (n=207; n=193) | Week 42 (n=207; n=193) | Week 52 (n=207; n=193) | |
| Alogliptin 25 mg QD | -6.104 | -0.136 | -5.571 | -9.755 |
| Glipizide 5 mg QD | 30.081 | 31.669 | 16.004 | 35.281 |
The percentage of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 0.5, 1.0, 1.5 and 2.0% during the 52 week study. (NCT00707993)
Timeframe: Baseline and Week 52.
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Decrease from Baseline in HbA1c ≥0.5% | Decrease from Baseline in HbA1c ≥1.0% | Decrease from Baseline in HbA1c ≥1.5% | Decrease from Baseline in HbA1c ≥2.0% | |
| Alogliptin 25 mg QD | 32.1 | 12.6 | 5.1 | 2.8 |
| Glipizide 5 mg QD | 29.0 | 10.3 | 2.3 | 1.4 |
The number of participants requiring rescue for failing to achieve pre-specified glycemic targets during the 52 week study. (NCT00707993)
Timeframe: On Occurrence (up to 52 weeks).
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
Week 2 to | Week 4 to | Week 8 to | Week 12 to | Week 16 to | Week 20 to | Week 26 to | Week 34 to | Week 42 to Week 52 | Overall | | |
| Alogliptin 25 mg QD | 1 | 2 | 1 | 14 | 6 | 5 | 10 | 6 | 10 | 50 |
| Glipizide 5 mg QD | 0 | 1 | 0 | 14 | 9 | 8 | 2 | 7 | 6 | 37 |
The change between the value of fasting fructosamine collected at day 85 or final visit and fasting fructosamine collected at baseline. (NCT00755846)
Timeframe: Baseline and Day 85.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | 7.7 |
| Alogliptin 6.25 mg QD | 0.2 |
| Alogliptin 12.5 mg QD | -9.8 |
| Alogliptin 25 mg QD | -16.4 |
| Alogliptin 50 mg QD | -12.4 |
| Alogliptin 100 mg QD | -4.8 |
The change between the value of fasting plasma glucose collected at day 85 or final visit and fasting plasma glucose collected at baseline. (NCT00755846)
Timeframe: Baseline and Day 85.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | 8.5 |
| Alogliptin 6.25 mg QD | -7.8 |
| Alogliptin 12.5 mg QD | -5.1 |
| Alogliptin 25 mg QD | -27.0 |
| Alogliptin 50 mg QD | -16.1 |
| Alogliptin 100 mg QD | -20.9 |
The change between the value of fasting fructosamine collected at day 43 and fasting fructosamine collected at baseline. (NCT00755846)
Timeframe: Baseline and Day 43.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | 7.6 |
| Alogliptin 6.25 mg QD | -4.2 |
| Alogliptin 12.5 mg QD | -13.1 |
| Alogliptin 25 mg QD | -14.5 |
| Alogliptin 50 mg QD | -16.3 |
| Alogliptin 100 mg QD | -11.7 |
The change between the value of fasting plasma glucose collected at day 43 and fasting plasma glucose collected at baseline. (NCT00755846)
Timeframe: Baseline and Day 43
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | 4.9 |
| Alogliptin 6.25 mg QD | -7.3 |
| Alogliptin 12.5 mg QD | -11.5 |
| Alogliptin 25 mg QD | -24.5 |
| Alogliptin 50 mg QD | -17.9 |
| Alogliptin 100 mg QD | -25.6 |
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 day 85 or final visit and glycosylated hemoglobin collected at baseline. (NCT00755846)
Timeframe: Baseline and Day 85.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo QD | -0.01 |
| Alogliptin 6.25 mg QD | -0.19 |
| Alogliptin 12.5 mg QD | -0.54 |
| Alogliptin 25 mg QD | -0.56 |
| Alogliptin 50 mg QD | -0.44 |
| Alogliptin 100 mg QD | -0.51 |
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 day 43 and glycosylated hemoglobin collected at baseline. (NCT00755846)
Timeframe: Baseline and Day 43.
| Intervention | percentage of Glycosylated Hemoglobin (Least Squares Mean) |
|---|---|
| Placebo QD | 0.02 |
| Alogliptin 6.25 mg QD | -0.12 |
| Alogliptin 12.5 mg QD | -0.35 |
| Alogliptin 25 mg QD | -0.36 |
| Alogliptin 50 mg QD | -0.32 |
| Alogliptin 100 mg QD | -0.31 |
The change between high-density lipoprotein cholesterol collected at day 43 and high-density lipoprotein cholesterol collected at baseline. (NCT00755846)
Timeframe: Baseline and Day 43.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | -1.4 |
| Alogliptin 6.25 mg QD | -0.6 |
| Alogliptin 12.5 mg QD | -2.0 |
| Alogliptin 25 mg QD | -2.4 |
| Alogliptin 50 mg QD | -2.8 |
| Alogliptin 100 mg QD | -1.1 |
The change between high-density lipoprotein cholesterol collected at day 85 or final visit and high-density lipoprotein cholesterol collected at baseline. (NCT00755846)
Timeframe: Baseline and Day 85.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | -1.9 |
| Alogliptin 6.25 mg QD | -0.7 |
| Alogliptin 12.5 mg QD | -2.3 |
| Alogliptin 25 mg QD | -2.5 |
| Alogliptin 50 mg QD | -2.0 |
| Alogliptin 100 mg QD | 0.4 |
The change between low-density lipoprotein cholesterol collected at day 43 and low-density lipoprotein cholesterol collected at baseline. (NCT00755846)
Timeframe: Baseline and Day 43.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | -8.9 |
| Alogliptin 6.25 mg QD | -3.8 |
| Alogliptin 12.5 mg QD | -6.4 |
| Alogliptin 25 mg QD | -1.5 |
| Alogliptin 50 mg QD | -9.9 |
| Alogliptin 100 mg QD | 0.8 |
The change between low-density lipoprotein cholesterol collected at day 85 or final visit and low-density lipoprotein cholesterol collected at baseline. (NCT00755846)
Timeframe: Baseline and Day 85.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | -13.6 |
| Alogliptin 6.25 mg QD | -2.6 |
| Alogliptin 12.5 mg QD | -2.7 |
| Alogliptin 25 mg QD | -0.6 |
| Alogliptin 50 mg QD | -5.0 |
| Alogliptin 100 mg QD | 4.0 |
The change between the value of cholesterol collected at day 43 and cholesterol collected at baseline. (NCT00755846)
Timeframe: Baseline and Day 43
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | -11.1 |
| Alogliptin 6.25 mg QD | -9.7 |
| Alogliptin 12.5 mg QD | -9.6 |
| Alogliptin 25 mg QD | -9.8 |
| Alogliptin 50 mg QD | -12.0 |
| Alogliptin 100 mg QD | -4.7 |
The change between the value of cholesterol collected at day 85 or final visit and cholesterol collected at baseline. (NCT00755846)
Timeframe: Baseline and Day 85.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | -15.1 |
| Alogliptin 6.25 mg QD | -9.0 |
| Alogliptin 12.5 mg QD | -4.8 |
| Alogliptin 25 mg QD | -8.7 |
| Alogliptin 50 mg QD | -7.7 |
| Alogliptin 100 mg QD | -0.4 |
The change between triglycerides collected at day 43 and triglycerides collected at baseline. (NCT00755846)
Timeframe: Baseline and Day 43.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | -18.7 |
| Alogliptin 6.25 mg QD | -28.0 |
| Alogliptin 12.5 mg QD | -10.1 |
| Alogliptin 25 mg QD | -27.7 |
| Alogliptin 50 mg QD | -7.2 |
| Alogliptin 100 mg QD | -31.5 |
The change between triglycerides collected at day 85 or final visit and triglycerides collected at baseline. (NCT00755846)
Timeframe: Baseline and Day 85.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Placebo QD | -13.9 |
| Alogliptin 6.25 mg QD | -26.4 |
| Alogliptin 12.5 mg QD | 9.2 |
| Alogliptin 25 mg QD | -32.9 |
| Alogliptin 50 mg QD | -14.4 |
| Alogliptin 100 mg QD | -24.9 |
The incidence of marked hyperglycemia occurring in participants with a fasting plasma glucose value greater than or equal to 200 mg per dL during study. Overall mean obtained by weighting the hyperglycemia percent incidence values at each time point by number of days in between visits. Mean percent incidence of marked hyperglycemia at each time point is the percent of self-monitored blood glucose measurements greater than or equal to 200 mg per dL, calculated per participant and then averaged across population. (NCT00755846)
Timeframe: 85 Days.
| Intervention | percent incidence (Mean) |
|---|---|
| Placebo QD | 54.0 |
| Alogliptin 6.25 mg QD | 34.7 |
| Alogliptin 12.5 mg QD | 25.8 |
| Alogliptin 25 mg QD | 28.1 |
| Alogliptin 50 mg QD | 30.4 |
| Alogliptin 100 mg QD | 30.6 |
The change from Baseline to Week 104 in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound). The least squares (LS) means are from an analysis of covariance (ANCOVA) model with treatment, study schedule, and geographic region as class variables, and Baseline metformin dose and Baseline HbA1c as covariates. (NCT00856284)
Timeframe: Baseline and Week 104
| Intervention | percentage glycosylated hemoglobin (Least Squares Mean) |
|---|---|
| Metformin + Alogliptin 12.5 mg | -0.68 |
| Metformin + Alogliptin 25 mg | -0.72 |
| Metformin + Glipizide | -0.59 |
The change from Baseline to Week 52 in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound). The least squares (LS) means are from an analysis of covariance (ANCOVA) model with treatment, study schedule, and geographic region as class variables, and Baseline metformin dose and Baseline HbA1c as covariates. (NCT00856284)
Timeframe: Baseline and Week 52
| Intervention | percentage glycosylated hemoglobin (Least Squares Mean) |
|---|---|
| Metformin + Alogliptin 12.5 mg | -0.81 |
| Metformin + Alogliptin 25 mg | -0.76 |
| Metformin + Glipizide | -0.73 |
LS Means are from an ANCOVA model with treatment, study schedule and geographic region as class variables, and Baseline weight and Baseline metformin dose as covariates. (NCT00856284)
Timeframe: Baseline and Weeks 12, 26, 39, 52, 65, 78, 91, and 104.
| Intervention | kg (Least Squares Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 12 | Week 26 | Week 39 | Week 52 | Week 65 | Week 78 | Week 91 | Week 104 | |
| Metformin + Alogliptin 12.5 mg | -0.51 | -0.65 | -0.60 | -0.63 | -0.70 | -0.78 | -0.67 | -0.68 |
| Metformin + Alogliptin 25 mg | -0.53 | -0.71 | -0.86 | -0.90 | -0.92 | -0.94 | -0.88 | -0.89 |
| Metformin + Glipizide | 0.71 | 0.86 | 0.97 | 0.89 | 0.87 | 0.88 | 0.89 | 0.95 |
The change from Baseline in fasting plasma glucose (FPG) was assessed at Weeks 2, 4, 8, 12, 16, 20, 26, 39, 52, 65, 78, 91, and 104. LS means are from an ANCOVA model with treatment, study schedule, and geographic region as class variables, and Baseline FPG and Baseline metformin dose as covariates. (NCT00856284)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16, 20, 26, 39, 52, 65, 78, 91, and 104.
| Intervention | mg/dL (Least Squares Mean) | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 2 (n=781, 803, 777) | Week 4 (n=863, 865, 855) | Week 8 (n=867, 867, 859) | Week 12 (n=867, 867, 859) | Week 16 (n=867, 867, 859) | Week 20 (n=867, 867, 859) | Week 26 (n=867, 867, 859) | Week 39 (n=867, 867, 859) | Week 52 (n=867, 867, 859) | Week 65 (n=867, 867, 859) | Week 78 (n=867, 867, 859) | Week 91 (n=867, 867, 859) | Week 104 (n=867, 867, 859) | |
| Metformin + Alogliptin 12.5 mg | -10.2 | -10.6 | -9.2 | -10.7 | -8.6 | -7.6 | -7.5 | -6.9 | -5.0 | -3.4 | -2.8 | -0.9 | -0.9 |
| Metformin + Alogliptin 25 mg | -11.4 | -11.6 | -11.6 | -11.2 | -9.9 | -10.1 | -10.1 | -8.4 | -7.0 | -5.9 | -5.1 | -3.4 | -3.2 |
| Metformin + Glipizide | -7.7 | -10.2 | -9.3 | -9.4 | -7.1 | -5.5 | -4.3 | -0.6 | 0.9 | 1.4 | 5.1 | 4.9 | 5.4 |
The change from Baseline over time in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound). LS means are from an ANCOVA model with treatment, study schedule, and geographic region as class variables, and Baseline metformin dose and Baseline HbA1c as covariates. (NCT00856284)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20, 26, 39, 65, 78, and 91.
| Intervention | percentage of glycosylated hemoglobin (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Week 4 (n=341, 354, 318) | Week 8 (n=370, 382, 336) | Week 12 (n=371, 382, 336) | Week 16 (n=371, 382, 336) | Week 20 (n=371, 382, 336) | Week 26 (n=371, 382, 336) | Week 39 (n=371, 382, 336) | Week 65 (n=371, 382, 336) | Week 78 (n=371, 382, 336) | Week 91 (n=371, 382, 336) | |
| Metformin + Alogliptin 12.5 mg | -0.37 | -0.56 | -0.69 | -0.74 | -0.76 | -0.80 | -0.81 | -0.81 | -0.82 | -0.76 |
| Metformin + Alogliptin 25 mg | -0.40 | -0.60 | -0.71 | -0.76 | -0.78 | -0.79 | -0.81 | -0.83 | -0.80 | -0.77 |
| Metformin + Glipizide | -0.41 | -0.66 | -0.78 | -0.78 | -0.79 | -0.80 | -0.74 | -0.76 | -0.73 | -0.68 |
The percentage of participants with HbA1c less than or equal to 6.5% at Weeks 26, 52, 78, and 104. Participants who did not complete the scheduled Week 104 visit were assessed based on their response at the time of discontinuation. (NCT00856284)
Timeframe: Weeks 26, 52, 78, and 104.
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Week 26 | Week 52 | Week 78 | Week 104 | |
| Metformin + Alogliptin 12.5 mg | 25.6 | 24.5 | 24.2 | 23.5 |
| Metformin + Alogliptin 25 mg | 26.2 | 24.8 | 26.4 | 24.1 |
| Metformin + Glipizide | 24.8 | 20.8 | 21.8 | 19.0 |
Percentage of participants with HbA1c ≤ 7.0% at Weeks 26, 52, 78, and 104. Participants who did not complete the scheduled Week 104 visit were assessed based on their response at the time of discontinuation. (NCT00856284)
Timeframe: Weeks 26, 52, 78, and 104.
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Week 26 | Week 52 | Week 78 | Week 104 | |
| Metformin + Alogliptin 12.5 mg | 56.4 | 51.7 | 48.8 | 45.6 |
| Metformin + Alogliptin 25 mg | 59.2 | 55.5 | 52.4 | 48.5 |
| Metformin + Glipizide | 56.1 | 47.4 | 46.6 | 42.8 |
The observed effect at 24 hours post-dose (E24) of baseline-corrected glucagon-like peptide-1 was determined from the concentration-time curve. Baseline-corrected glucagon-like peptide-1 concentrations were calculated as the post-dose concentration at each post-dose time point minus the baseline (pre-dose) concentration. (NCT00957268)
Timeframe: 1 hour pre-dose and 2, 4, 8, 12, and 24 hours post-dose
| Intervention | pmol/L (Mean) |
|---|---|
| Alogliptin 12.5 mg (Age 10 to < 14 Years) | 2.500 |
| Alogliptin 25 mg (Age 10 to < 14 Years) | 4.575 |
| Alogliptin 12.5 mg (Age 14 to < 18 Years) | 4.214 |
| Alogliptin 25 mg (Age 14 to < 18 Years) | 4.329 |
| Alogliptin 25 mg (Age 18 to 65 Years) | 5.419 |
The time to reach the maximum observed effect of dipeptidyl peptidase-4 (DPP-4) inhibition was determined from the inhibition-time curve. (NCT00957268)
Timeframe: 1 hour pre-dose and 2, 4, 8, 12, and 24 hours post-dose
| Intervention | hr (Median) |
|---|---|
| Alogliptin 12.5 mg (Age 10 to < 14 Years) | 4.050 |
| Alogliptin 25 mg (Age 10 to < 14 Years) | 2.080 |
| Alogliptin 12.5 mg (Age 14 to < 18 Years) | 4.000 |
| Alogliptin 25 mg (Age 14 to < 18 Years) | 4.000 |
| Alogliptin 25 mg (Age 18 to 65 Years) | 2.000 |
The time to reach the maximum observed effect of baseline-corrected glucagon-like peptide-1 was determined from the concentration-time curve. Baseline-corrected glucagon-like peptide-1 concentrations were calculated as the post-dose concentration at each post-dose time point minus the baseline (pre-dose) concentration. (NCT00957268)
Timeframe: 1 hour pre-dose and 2, 4, 8, 12, and 24 hours post-dose
| Intervention | hr (Median) |
|---|---|
| Alogliptin 12.5 mg (Age 10 to < 14 Years) | 8.170 |
| Alogliptin 25 mg (Age 10 to < 14 Years) | 11.985 |
| Alogliptin 12.5 mg (Age 14 to < 18 Years) | 11.920 |
| Alogliptin 25 mg (Age 14 to < 18 Years) | 8.020 |
| Alogliptin 25 mg (Age 18 to 65 Years) | 12.000 |
The maximum observed effect (Emax) of dipeptidyl peptidase-4 (DPP-4) inhibition was determined from the inhibition-time curve. (NCT00957268)
Timeframe: 1 hour pre-dose and 2, 4, 8, 12, and 24 hours post-dose
| Intervention | Percentage inhibition (Mean) |
|---|---|
| Alogliptin 12.5 mg (Age 10 to < 14 Years) | 83.660 |
| Alogliptin 25 mg (Age 10 to < 14 Years) | 89.300 |
| Alogliptin 12.5 mg (Age 14 to < 18 Years) | 81.643 |
| Alogliptin 25 mg (Age 14 to < 18 Years) | 90.429 |
| Alogliptin 25 mg (Age 18 to 65 Years) | 92.650 |
The area under the plasma effect-time curve from time 0 to 24 hours post-dose (AUEC[0-24]) of dipeptidyl peptidase-4 (DPP-4) inhibition was determined from the inhibition-time curve. (NCT00957268)
Timeframe: 1 hour pre-dose and 2, 4, 8, 12, and 24 hours post-dose
| Intervention | Percentage inhibition•hr (Mean) |
|---|---|
| Alogliptin 12.5 mg (Age 10 to < 14 Years) | 1569.633 |
| Alogliptin 25 mg (Age 10 to < 14 Years) | 1698.852 |
| Alogliptin 12.5 mg (Age 14 to < 18 Years) | 1557.788 |
| Alogliptin 25 mg (Age 14 to < 18 Years) | 1854.391 |
| Alogliptin 25 mg (Age 18 to 65 Years) | 1890.012 |
The area under the plasma effect-time curve from time 0 to 24 hours post-dose (AUEC[0-24]) of baseline-corrected glucagon-like peptide-1 was determined from the concentration-time curve. Baseline-corrected glucagon-like peptide-1 concentrations were calculated as the post-dose concentration at each post-dose time point minus the baseline (pre-dose) concentration. (NCT00957268)
Timeframe: 1 hour pre-dose and 2, 4, 8, 12, and 24 hours post-dose
| Intervention | pmol•hr/L (Mean) |
|---|---|
| Alogliptin 12.5 mg (Age 10 to < 14 Years) | 117.842 |
| Alogliptin 25 mg (Age 10 to < 14 Years) | 120.055 |
| Alogliptin 12.5 mg (Age 14 to < 18 Years) | 168.099 |
| Alogliptin 25 mg (Age 14 to < 18 Years) | 122.948 |
| Alogliptin 25 mg (Age 18 to 65 Years) | 278.669 |
AUC(0-inf) is measure of area under the curve over the dosing interval (tau) (AUC(0-tau]), where tau is the length of the dosing interval in this study). (NCT00957268)
Timeframe: 1 hour pre-dose and 1, 2, 4, 8, 12, 16, 24, 48, and 72 hours post-dose
| Intervention | ng•hr/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg (Age 10 to < 14 Years) | 789.29 |
| Alogliptin 25 mg (Age 10 to < 14 Years) | 1221.98 |
| Alogliptin 12.5 mg (Age 14 to < 18 Years) | 688.63 |
| Alogliptin 25 mg (Age 14 to < 18 Years) | 1318.41 |
| Alogliptin 25 mg (Age 18 to 65 Years) | 1704.02 |
Maximum observed plasma concentration (Cmax) is the peak plasma concentration of a drug after administration, obtained directly from the plasma concentration-time curve. (NCT00957268)
Timeframe: 1 hour pre-dose and 1, 2, 4, 8, 12, 16, 24, 48, and 72 hours post-dose
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg (Age 10 to < 14 Years) | 57.82 |
| Alogliptin 25 mg (Age 10 to < 14 Years) | 101.38 |
| Alogliptin 12.5 mg (Age 14 to < 18 Years) | 44.24 |
| Alogliptin 25 mg (Age 14 to < 18 Years) | 96.74 |
| Alogliptin 25 mg (Age 18 to 65 Years) | 136.50 |
The maximum observed effect (Emax) of baseline-corrected glucagon-like peptide-1 was determined from the concentration-time curve. Baseline-corrected glucagon-like peptide-1 concentrations were calculated as the post-dose concentration at each post-dose time point minus the baseline (pre-dose) concentration. (NCT00957268)
Timeframe: 1 hour pre-dose and 2, 4, 8, 12, and 24 hours post-dose
| Intervention | pmol/L (Mean) |
|---|---|
| Alogliptin 12.5 mg (Age 10 to < 14 Years) | 11.700 |
| Alogliptin 25 mg (Age 10 to < 14 Years) | 7.475 |
| Alogliptin 12.5 mg (Age 14 to < 18 Years) | 16.500 |
| Alogliptin 25 mg (Age 14 to < 18 Years) | 9.129 |
| Alogliptin 25 mg (Age 18 to 65 Years) | 23.843 |
The observed effect at 24 hours post-dose (E24) of dipeptidyl peptidase-4 (DPP-4) inhibition was determined from the inhibition-time curve. (NCT00957268)
Timeframe: 1 hour pre-dose and 2, 4, 8, 12, and 24 hours post-dose
| Intervention | Percentage inhibition (Mean) |
|---|---|
| Alogliptin 12.5 mg (Age 10 to < 14 Years) | 52.000 |
| Alogliptin 25 mg (Age 10 to < 14 Years) | 57.375 |
| Alogliptin 12.5 mg (Age 14 to < 18 Years) | 55.400 |
| Alogliptin 25 mg (Age 14 to < 18 Years) | 70.400 |
| Alogliptin 25 mg (Age 18 to 65 Years) | 72.843 |
Tmax: Time to reach the maximum plasma concentration (Cmax), equal to time (hours) to Cmax. (NCT00957268)
Timeframe: 1 hour pre-dose and 1, 2, 4, 8, 12, 16, 24, 48, and 72 hours post-dose
| Intervention | hr (Mean) |
|---|---|
| Alogliptin 12.5 mg (Age 10 to < 14 Years) | 3.24 |
| Alogliptin 25 mg (Age 10 to < 14 Years) | 2.04 |
| Alogliptin 12.5 mg (Age 14 to < 18 Years) | 5.58 |
| Alogliptin 25 mg (Age 14 to < 18 Years) | 2.86 |
| Alogliptin 25 mg (Age 18 to 65 Years) | 2.09 |
Secondary MACE composite consisted of cardiovascular death, nonfatal myocardial infarction, nonfatal stroke, or urgent revascularization due to unstable angina; these events were adjudicated by an independent cardiovascular endpoint committee. (NCT00968708)
Timeframe: From randomization until the adjudication cut-of date of May 31 2013 (maximum time on study was 41 months).
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 13.4 |
| Alogliptin | 12.7 |
Primary Major Adverse Cardiac Events were defined as a composite of cardiovascular death, nonfatal myocardial infarction and nonfatal stroke; these events were adjudicated by an independent cardiovascular endpoints committee. (NCT00968708)
Timeframe: From randomization until the adjudication cut-off date of May 31 2013 (maximum time on study was 41 months).
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 11.8 |
| Alogliptin | 11.3 |
The change from Baseline to Week 26 in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound). (NCT01023581)
Timeframe: Baseline and Week 26.
| Intervention | percentage glycosylated hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | 0.15 |
| Alogliptin 25 QD | -0.52 |
| Alogliptin 12.5 BID | -0.56 |
| Metformin 500 BID | -0.65 |
| Metformin 1000 BID | -1.11 |
| Alogliptin 12.5 BID + Metformin 500 BID | -1.22 |
| Alogliptin 12.5 BID + Metformin 1000 BID | -1.55 |
"The change from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) was assessed at Weeks 4, 8, 12, 16 and 20.~Least squares means are from an analysis of covariance (ANCOVA) model with treatment and geographic region as fixed effects, and baseline HbA1c as a covariate." (NCT01023581)
Timeframe: Baseline and Weeks 4, 8, 12, 16, and 20.
| Intervention | percentage glycosylated hemoglobin (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Week 4 (n=95, 97, 89, 94, 102, 94, 101) | Week 8 (n=102, 104, 104, 103, 108, 102, 111) | Week 12 (n=102, 104, 104, 103, 108, 102, 111) | Week 16 (n=102, 104, 104, 103, 108, 102, 111) | Week 20 (n=102, 104, 104, 103, 108, 102, 111) | |
| Alogliptin 12.5 BID | -0.42 | -0.58 | -0.62 | -0.63 | -0.59 |
| Alogliptin 12.5 BID + Metformin 1000 BID | -0.75 | -1.17 | -1.40 | -1.50 | -1.54 |
| Alogliptin 12.5 BID + Metformin 500 BID | -0.70 | -1.08 | -1.22 | -1.26 | -1.25 |
| Alogliptin 25 QD | -0.34 | -0.51 | -0.53 | -0.58 | -0.57 |
| Metformin 1000 BID | -0.58 | -0.86 | -1.02 | -1.09 | -1.14 |
| Metformin 500 BID | -0.37 | -0.59 | -0.68 | -0.72 | -0.68 |
| Placebo | 0.09 | 0.08 | 0.12 | 0.13 | 0.12 |
The change from Baseline in fasting plasma glucose was assessed at Weeks 1, 2, 4, 8, 12, 16, 20 and 26. Least Squares Means were from an ANCOVA model with treatment and geographic region as fixed effects, and baseline fasting plasma glucose as a covariate. (NCT01023581)
Timeframe: Baseline and Weeks 1, 2, 4, 8, 12, 16, 20 and 26.
| Intervention | mg/dL (Least Squares Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 1 (n=102, 103, 94, 95, 104, 101, 109) | Week 2 (n=105, 112, 105, 102, 108, 106, 111) | Week 4 (n=105, 112, 106, 106, 110, 106, 111) | Week 8 (n=105, 112, 106, 106, 110, 106, 112) | Week 12 (n=105, 112, 106, 106, 110, 106, 112) | Week 16 (n=105, 112, 106, 106, 110, 106, 112) | Week 20 (n=105, 112, 106, 106, 110, 106, 112) | Week 26 (n=105, 112, 106, 106, 110, 106, 112) | |
| Alogliptin 12.5 BID | -11.9 | -11.6 | -16.6 | -12.1 | -14.7 | -14.7 | -12.3 | -9.7 |
| Alogliptin 12.5 BID + Metformin 1000 BID | -36.3 | -43.6 | -44.1 | -43.8 | -44.7 | -47.7 | -44.6 | -45.9 |
| Alogliptin 12.5 BID + Metformin 500 BID | -32.7 | -34.5 | -37.6 | -32.9 | -31.6 | -35.9 | -33.8 | -31.7 |
| Alogliptin 25 QD | -3.9 | -7.4 | -11.5 | -10.9 | -9.7 | -7.1 | -9.2 | -6.1 |
| Metformin 1000 BID | -23.1 | -22.2 | -29.0 | -30.7 | -30.7 | -33.5 | -35.1 | -31.9 |
| Metformin 500 BID | -12.6 | -14.5 | -16.9 | -11.8 | -14.0 | -13.3 | -10.9 | -11.5 |
| Placebo | 5.7 | 4.6 | 7.2 | 7.1 | 11.6 | 10.1 | 8.7 | 12.4 |
The change between the value of insulin collected at week 12 or final visit and insulin collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263470)
Timeframe: Baseline and Week 12
| Intervention | μU·hr/mL (Mean) |
|---|---|
| Placebo | -3.60 |
| Alogliptin 6.25 mg QD | -0.74 |
| Alogliptin 12.5 mg QD | 1.86 |
| Alogliptin 25 mg QD | 4.12 |
| Alogliptin 50 mg QD | -1.04 |
| Voglibose 0.2 mg TID | -15.40 |
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 8 and glycosylated hemoglobin collected at baseline. (NCT01263470)
Timeframe: Baseline and Week 8.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Placebo | 0.00 |
| Alogliptin 6.25 mg QD | -0.50 |
| Alogliptin 12.5 mg QD | -0.61 |
| Alogliptin 25 mg QD | -0.66 |
| Alogliptin 50 mg QD | -0.69 |
| Voglibose 0.2 mg TID | -0.17 |
The change between the value of C-peptide collected at week 12 or final visit and C-peptide collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263470)
Timeframe: Baseline and Week 12.
| Intervention | ng·hr/mL (Mean) |
|---|---|
| Placebo | 0.01 |
| Alogliptin 6.25 mg QD | 0.54 |
| Alogliptin 12.5 mg QD | 0.77 |
| Alogliptin 25 mg QD | 1.01 |
| Alogliptin 50 mg QD | 0.97 |
| Voglibose 0.2 mg TID | -0.39 |
The change between the value of blood glucose collected at week 12 or final visit and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01263470)
Timeframe: Baseline and Week 12.
| Intervention | mg·hr/dL (Mean) |
|---|---|
| Placebo | 5.6 |
| Alogliptin 6.25 mg QD | -52.7 |
| Alogliptin 12.5 mg QD | -55.0 |
| Alogliptin 25 mg QD | -73.1 |
| Alogliptin 50 mg QD | -81.8 |
| Voglibose 0.2 mg TID | -50.0 |
The change between the value of blood glucose collected at week 12 or final visit and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01263470)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Placebo | -4.2 |
| Alogliptin 6.25 mg QD | -28.1 |
| Alogliptin 12.5 mg QD | -27.6 |
| Alogliptin 25 mg QD | -44.8 |
| Alogliptin 50 mg QD | -47.0 |
| Voglibose 0.2 mg TID | -22.7 |
The change between the value of fasting C-peptide collected at week 12 or final visit and fasting C-peptide collected at baseline. (NCT01263470)
Timeframe: Baseline and Week 12.
| Intervention | ng/mL (Mean) |
|---|---|
| Placebo | -0.00 |
| Alogliptin 6.25 mg QD | 0.04 |
| Alogliptin 12.5 mg QD | 0.17 |
| Alogliptin 25 mg QD | 0.25 |
| Alogliptin 50 mg QD | 0.18 |
| Voglibose 0.2 mg TID | -0.02 |
The change between the value of fasting C-peptide collected at week 2 and fasting C-peptide collected at baseline. (NCT01263470)
Timeframe: Baseline and Week 2.
| Intervention | ng/mL (Mean) |
|---|---|
| Placebo | 0.04 |
| Alogliptin 6.25 mg QD | -0.11 |
| Alogliptin 12.5 mg QD | 0.17 |
| Alogliptin 25 mg QD | 0.18 |
| Alogliptin 50 mg QD | 0.04 |
| Voglibose 0.2 mg TID | -0.11 |
The change between the value of fasting C-peptide collected at week 4 and fasting C-peptide collected at baseline. (NCT01263470)
Timeframe: Baseline and Week 4.
| Intervention | ng/mL (Mean) |
|---|---|
| Placebo | 0.01 |
| Alogliptin 6.25 mg QD | -0.04 |
| Alogliptin 12.5 mg QD | 0.02 |
| Alogliptin 25 mg QD | 0.16 |
| Alogliptin 50 mg QD | 0.05 |
| Voglibose 0.2 mg TID | -0.16 |
The change between the value of fasting C-peptide collected at week 8 and fasting C-peptide collected at baseline. (NCT01263470)
Timeframe: Baseline and Week 8.
| Intervention | ng/mL (Mean) |
|---|---|
| Placebo | 0.17 |
| Alogliptin 6.25 mg QD | 0.05 |
| Alogliptin 12.5 mg QD | 0.07 |
| Alogliptin 25 mg QD | 0.24 |
| Alogliptin 50 mg QD | 0.05 |
| Voglibose 0.2 mg TID | -0.05 |
The change between the value of fasting plasma glucose collected at week 12 or final visit and fasting plasma glucose collected at baseline. (NCT01263470)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Placebo | 5.6 |
| Alogliptin 6.25 mg QD | -9.3 |
| Alogliptin 12.5 mg QD | -14.6 |
| Alogliptin 25 mg QD | -17.5 |
| Alogliptin 50 mg QD | -22.6 |
| Voglibose 0.2 mg TID | -3.0 |
The change between the value of fasting plasma glucose collected at week 2 and fasting plasma glucose collected at baseline. (NCT01263470)
Timeframe: Baseline and Week 2
| Intervention | mg/dL (Mean) |
|---|---|
| Placebo | 1.8 |
| Alogliptin 6.25 mg QD | -13.8 |
| Alogliptin 12.5 mg QD | -15.9 |
| Alogliptin 25 mg QD | -14.3 |
| Alogliptin 50 mg QD | -21.7 |
| Voglibose 0.2 mg TID | -8.0 |
The change between the value of fasting plasma glucose collected at week 4 and fasting plasma glucose collected at baseline. (NCT01263470)
Timeframe: Baseline and Week 4.
| Intervention | mg/dL (Mean) |
|---|---|
| Placebo | 8.4 |
| Alogliptin 6.25 mg QD | -16.0 |
| Alogliptin 12.5 mg QD | -20.9 |
| Alogliptin 25 mg QD | -19.0 |
| Alogliptin 50 mg QD | -23.3 |
| Voglibose 0.2 mg TID | -7.2 |
The change between the value of fasting plasma glucose collected at week 8 and fasting plasma glucose collected at baseline. (NCT01263470)
Timeframe: Baseline and Week 8.
| Intervention | mg/dL (Mean) |
|---|---|
| Placebo | 5.7 |
| Alogliptin 6.25 mg QD | -12.0 |
| Alogliptin 12.5 mg QD | -18.5 |
| Alogliptin 25 mg QD | -18.6 |
| Alogliptin 50 mg QD | -22.6 |
| Voglibose 0.2 mg TID | -3.5 |
The change between the value of glucagons collected at week 12 or final visit and glucagons collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263470)
Timeframe: Baseline and Week 12
| Intervention | pg·hr/mL (Mean) |
|---|---|
| Placebo | -15.8 |
| Alogliptin 6.25 mg QD | -11.5 |
| Alogliptin 12.5 mg QD | -4.5 |
| Alogliptin 25 mg QD | -12.6 |
| Alogliptin 50 mg QD | -19.5 |
| Voglibose 0.2 mg TID | -16.3 |
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 12 or final visit and glycosylated hemoglobin collected at baseline. (NCT01263470)
Timeframe: Baseline and Week 12.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Placebo | 0.06 |
| Alogliptin 6.25 mg QD | -0.51 |
| Alogliptin 12.5 mg QD | -0.70 |
| Alogliptin 25 mg QD | -0.76 |
| Alogliptin 50 mg QD | -0.82 |
| Voglibose 0.2 mg TID | -0.16 |
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 2 and glycosylated hemoglobin collected at baseline. (NCT01263470)
Timeframe: Baseline and Week 2.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Placebo | 0.00 |
| Alogliptin 6.25 mg QD | -0.16 |
| Alogliptin 12.5 mg QD | -0.17 |
| Alogliptin 25 mg QD | -0.16 |
| Alogliptin 50 mg QD | -0.15 |
| Voglibose 0.2 mg TID | -0.10 |
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 4 and glycosylated hemoglobin collected at baseline. (NCT01263470)
Timeframe: Baseline and Week 4.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Placebo | -0.01 |
| Alogliptin 6.25 mg QD | -0.34 |
| Alogliptin 12.5 mg QD | -0.38 |
| Alogliptin 25 mg QD | -0.35 |
| Alogliptin 50 mg QD | -0.40 |
| Voglibose 0.2 mg TID | -0.16 |
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 2 and glycosylated hemoglobin collected at baseline. (NCT01263483)
Timeframe: Baseline and Week 2.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Voglibose 0.2 mg TID | -0.01 |
| Alogliptin 12.5 mg QD | -0.19 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.21 |
The change between the value of fasting C-peptide collected at week 8 and fasting C-peptide collected at baseline. (NCT01263483)
Timeframe: Baseline and Week 8.
| Intervention | ng/mL (Mean) |
|---|---|
| Voglibose 0.2 mg TID | 0.07 |
| Alogliptin 12.5 mg QD | 0.03 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.01 |
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 4 and glycosylated hemoglobin collected at baseline. (NCT01263483)
Timeframe: Baseline and Week 4.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Voglibose 0.2 mg TID | -0.02 |
| Alogliptin 12.5 mg QD | -0.44 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.43 |
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 8 and glycosylated hemoglobin collected at baseline. (NCT01263483)
Timeframe: Baseline and Week 8.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Voglibose 0.2 mg TID | -0.01 |
| Alogliptin 12.5 mg QD | -0.74 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.75 |
The change between the value of insulin collected at week 12 or final visit and insulin collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01263483)
Timeframe: Baseline and Week 12
| Intervention | μU·hr/mL (Mean) |
|---|---|
| Voglibose 0.2 mg TID | -2.47 |
| Alogliptin 12.5 mg QD | 4.62 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 1.50 |
The change between the value of blood glucose collected at week 12 or final visit and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01263483)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Voglibose 0.2 mg TID | 72.4 |
| Alogliptin 12.5 mg QD | 40.9 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 38.7 |
The change between the value of blood glucose collected at week 12 or final visit and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01263483)
Timeframe: Baseline and Week 12.
| Intervention | mg·hr/dL (Mean) |
|---|---|
| Voglibose 0.2 mg TID | -4.3 |
| Alogliptin 12.5 mg QD | -74.7 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -76.8 |
The change between the value of C-peptide collected at week 12 or final visit and C-peptide collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01263483)
Timeframe: Baseline and Week 12.
| Intervention | ng·hr/mL (Mean) |
|---|---|
| Voglibose 0.2 mg TID | 0.14 |
| Alogliptin 12.5 mg QD | 0.69 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.57 |
The change between the value of fasting C-peptide collected at week 12 or final visit and fasting C-peptide collected at baseline. (NCT01263483)
Timeframe: Baseline and Week 12.
| Intervention | ng/mL (Mean) |
|---|---|
| Voglibose 0.2 mg TID | 0.02 |
| Alogliptin 12.5 mg QD | 0.06 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.10 |
The change between the value of fasting C-peptide collected at week 2 and fasting C-peptide collected at baseline. (NCT01263483)
Timeframe: Baseline and Week 2.
| Intervention | ng/mL (Mean) |
|---|---|
| Voglibose 0.2 mg TID | 0.03 |
| Alogliptin 12.5 mg QD | -0.07 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.01 |
The change between the value of fasting C-peptide collected at week 4 and fasting C-peptide collected at baseline. (NCT01263483)
Timeframe: Baseline and Week 4.
| Intervention | ng/mL (Mean) |
|---|---|
| Voglibose 0.2 mg TID | 0.05 |
| Alogliptin 12.5 mg QD | 0.06 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.01 |
The change between the value of fasting plasma glucose collected at week 12 or final visit and fasting plasma glucose collected at baseline. (NCT01263483)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Voglibose 0.2 mg TID | -5.6 |
| Alogliptin 12.5 mg QD | -19.1 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -18.5 |
The change between the value of fasting plasma glucose collected at week 2 and fasting plasma glucose collected at baseline. (NCT01263483)
Timeframe: Baseline and Week 2
| Intervention | mg/dL (Mean) |
|---|---|
| Voglibose 0.2 mg TID | -3.5 |
| Alogliptin 12.5 mg QD | -15.5 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -18.8 |
The change between the value of fasting plasma glucose collected at week 4 and fasting plasma glucose collected at baseline. (NCT01263483)
Timeframe: Baseline and Week 4.
| Intervention | mg/dL (Mean) |
|---|---|
| Voglibose 0.2 mg TID | -0.6 |
| Alogliptin 12.5 mg QD | -16.2 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -22.6 |
The change between the value of fasting plasma glucose collected at week 8 and fasting plasma glucose collected at baseline. (NCT01263483)
Timeframe: Baseline and Week 8.
| Intervention | mg/dL (Mean) |
|---|---|
| Voglibose 0.2 mg TID | -2.5 |
| Alogliptin 12.5 mg QD | -20.8 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -21.9 |
The change between the value of glucagons collected at week 12 or final visit and glucagons collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01263483)
Timeframe: Baseline and Week 12
| Intervention | pg·hr/mL (Mean) |
|---|---|
| Voglibose 0.2 mg TID | -0.4 |
| Alogliptin 12.5 mg QD | -19.2 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -20.5 |
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 12 or final visit and glycosylated hemoglobin collected at baseline. (NCT01263483)
Timeframe: Baseline and Week 12.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Voglibose 0.2 mg TID | 0.04 |
| Alogliptin 12.5 mg QD | -0.96 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.91 |
The change between the value of fasting C-peptide collected at week 36 and fasting C-peptide collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 36.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 0.12 |
| Alogliptin 12.5 mg QD | 0.33 |
| Alogliptin 25 mg QD | 0.20 |
| Alogliptin 50 mg QD | 0.42 |
| Voglibose 0.2 mg TID | 0.09 |
The change between the value of fasting C-peptide collected at week 40 and fasting C-peptide collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 40.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.14 |
| Alogliptin 12.5 mg QD | 0.48 |
| Alogliptin 25 mg QD | 0.27 |
| Alogliptin 50 mg QD | 0.44 |
| Voglibose 0.2 mg TID | 0.13 |
The change between the value of fasting C-peptide collected at week 44 and fasting C-peptide collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 44.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 0.22 |
| Alogliptin 12.5 mg QD | 0.52 |
| Alogliptin 25 mg QD | 0.59 |
| Alogliptin 50 mg QD | 0.20 |
| Voglibose 0.2 mg TID | -0.06 |
The change between the value of fasting C-peptide collected at week 48 and fasting C-peptide collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 48.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.40 |
| Alogliptin 12.5 mg QD | 0.54 |
| Alogliptin 25 mg QD | 0.04 |
| Alogliptin 50 mg QD | 0.15 |
| Voglibose 0.2 mg TID | -0.10 |
The change between the value of fasting C-peptide collected at week 52 and fasting C-peptide collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 52.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.25 |
| Alogliptin 12.5 mg QD | 0.73 |
| Alogliptin 25 mg QD | 0.10 |
| Alogliptin 50 mg QD | 0.30 |
| Voglibose 0.2 mg TID | 0.70 |
The change between the value of fasting plasma glucose collected at week 52 or final visit and fasting plasma glucose collected at baseline. (NCT01263496)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -10.4 |
| Alogliptin 12.5 mg QD | -15.5 |
| Alogliptin 25 mg QD | -17.1 |
| Alogliptin 50 mg QD | -27.6 |
| Voglibose 0.2 mg TID | -8.8 |
The change between the value of fasting plasma glucose collected at week 12 and fasting plasma glucose collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 12
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -12.1 |
| Alogliptin 12.5 mg QD | -15.3 |
| Alogliptin 25 mg QD | -17.0 |
| Alogliptin 50 mg QD | -23.0 |
| Voglibose 0.2 mg TID | -3.6 |
The change between the value of fasting plasma glucose collected at week 16 and fasting plasma glucose collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 16.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -10.8 |
| Alogliptin 12.5 mg QD | -15.8 |
| Alogliptin 25 mg QD | -17.0 |
| Alogliptin 50 mg QD | -18.8 |
| Voglibose 0.2 mg TID | -6.4 |
The change between the value of fasting plasma glucose collected at week 20 and fasting plasma glucose collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 20.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -11.5 |
| Alogliptin 12.5 mg QD | -15.3 |
| Alogliptin 25 mg QD | -13.8 |
| Alogliptin 50 mg QD | -20.1 |
| Voglibose 0.2 mg TID | -4.6 |
The change between the value of fasting plasma glucose collected at week 24 and fasting plasma glucose collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 24.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -10.6 |
| Alogliptin 12.5 mg QD | -11.7 |
| Alogliptin 25 mg QD | -13.8 |
| Alogliptin 50 mg QD | -20.2 |
| Voglibose 0.2 mg TID | -8.3 |
The change between the value of fasting plasma glucose collected at week 28 and fasting plasma glucose collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 28.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -9.6 |
| Alogliptin 12.5 mg QD | -13.4 |
| Alogliptin 25 mg QD | -14.1 |
| Alogliptin 50 mg QD | -19.9 |
| Voglibose 0.2 mg TID | -7.2 |
The change between the value of fasting plasma glucose collected at week 32 and fasting plasma glucose collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 32.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -14.5 |
| Alogliptin 12.5 mg QD | -12.9 |
| Alogliptin 25 mg QD | -14.9 |
| Alogliptin 50 mg QD | -20.3 |
| Voglibose 0.2 mg TID | -9.1 |
The change between the value of fasting plasma glucose collected at week 36 and fasting plasma glucose collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 36.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -10.7 |
| Alogliptin 12.5 mg QD | -14.3 |
| Alogliptin 25 mg QD | -16.9 |
| Alogliptin 50 mg QD | -20.9 |
| Voglibose 0.2 mg TID | -8.4 |
The change between the value of fasting plasma glucose collected at week 40 and fasting plasma glucose collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 40.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -13.5 |
| Alogliptin 12.5 mg QD | -14.8 |
| Alogliptin 25 mg QD | -15.7 |
| Alogliptin 50 mg QD | -23.2 |
| Voglibose 0.2 mg TID | -13.8 |
The change between the value of fasting plasma glucose collected at week 44 and fasting plasma glucose collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 44.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -16.7 |
| Alogliptin 12.5 mg QD | -18.7 |
| Alogliptin 25 mg QD | -19.0 |
| Alogliptin 50 mg QD | -24.7 |
| Voglibose 0.2 mg TID | -15.0 |
The change between the value of fasting plasma glucose collected at week 48 and fasting plasma glucose collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 48.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -16.0 |
| Alogliptin 12.5 mg QD | -20.8 |
| Alogliptin 25 mg QD | -22.8 |
| Alogliptin 50 mg QD | -25.4 |
| Voglibose 0.2 mg TID | -13.5 |
The change between the value of fasting plasma glucose collected at week 52 and fasting plasma glucose collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 52.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -13.7 |
| Alogliptin 12.5 mg QD | -19.5 |
| Alogliptin 25 mg QD | -21.4 |
| Alogliptin 50 mg QD | -26.0 |
| Voglibose 0.2 mg TID | -12.5 |
The change between the value of glucagons collected at week 52 or final visit and glucagons collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | pg·hr/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -9.8 |
| Alogliptin 12.5 mg QD | -9.0 |
| Alogliptin 25 mg QD | -10.3 |
| Alogliptin 50 mg QD | -14.6 |
| Voglibose 0.2 mg TID | -13.9 |
The change between the value of glucagons collected at week 12 and glucagons collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 12
| Intervention | pg·hr/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -9.5 |
| Alogliptin 12.5 mg QD | -4.4 |
| Alogliptin 25 mg QD | -6.6 |
| Alogliptin 50 mg QD | -15.5 |
| Voglibose 0.2 mg TID | -16.3 |
The change between the value of glucagons collected at week 24 and glucagons collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 24.
| Intervention | pg·hr/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -1.7 |
| Alogliptin 12.5 mg QD | 3.0 |
| Alogliptin 25 mg QD | 0.9 |
| Alogliptin 50 mg QD | -0.8 |
| Voglibose 0.2 mg TID | -7.6 |
The change between the value of C-peptide collected at week 52 and C-peptide collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 52.
| Intervention | ng·hr/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 1.91 |
| Alogliptin 12.5 mg QD | 3.44 |
| Alogliptin 25 mg QD | 2.37 |
| Alogliptin 50 mg QD | 3.14 |
| Voglibose 0.2 mg TID | 1.86 |
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 52 or final visit and glycosylated hemoglobin collected at baseline. (NCT01263496)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.40 |
| Alogliptin 12.5 mg QD | -0.47 |
| Alogliptin 25 mg QD | -0.63 |
| Alogliptin 50 mg QD | -0.86 |
| Voglibose 0.2 mg TID | -0.22 |
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 12 and glycosylated hemoglobin collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 12.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.55 |
| Alogliptin 12.5 mg QD | -0.70 |
| Alogliptin 25 mg QD | -0.74 |
| Alogliptin 50 mg QD | -0.86 |
| Voglibose 0.2 mg TID | -0.15 |
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 16 and glycosylated hemoglobin collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 16.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.57 |
| Alogliptin 12.5 mg QD | -0.75 |
| Alogliptin 25 mg QD | -0.77 |
| Alogliptin 50 mg QD | -0.90 |
| Voglibose 0.2 mg TID | -0.25 |
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 20 and glycosylated hemoglobin collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 20.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.56 |
| Alogliptin 12.5 mg QD | -0.69 |
| Alogliptin 25 mg QD | -0.70 |
| Alogliptin 50 mg QD | -0.88 |
| Voglibose 0.2 mg TID | -0.30 |
The change between the value of fasting C-peptide collected at week 12 and fasting C-peptide collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 12.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.02 |
| Alogliptin 12.5 mg QD | 0.19 |
| Alogliptin 25 mg QD | 0.19 |
| Alogliptin 50 mg QD | 0.25 |
| Voglibose 0.2 mg TID | -0.04 |
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 28 and glycosylated hemoglobin collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 28.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.39 |
| Alogliptin 12.5 mg QD | -0.56 |
| Alogliptin 25 mg QD | -0.67 |
| Alogliptin 50 mg QD | -0.78 |
| Voglibose 0.2 mg TID | -0.32 |
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 32 and glycosylated hemoglobin collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 32.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.35 |
| Alogliptin 12.5 mg QD | -0.56 |
| Alogliptin 25 mg QD | -0.61 |
| Alogliptin 50 mg QD | -0.76 |
| Voglibose 0.2 mg TID | -0.27 |
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 36 and glycosylated hemoglobin collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 36.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.33 |
| Alogliptin 12.5 mg QD | -0.52 |
| Alogliptin 25 mg QD | -0.66 |
| Alogliptin 50 mg QD | -0.77 |
| Voglibose 0.2 mg TID | -0.28 |
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 40 and glycosylated hemoglobin collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 40.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.33 |
| Alogliptin 12.5 mg QD | -0.48 |
| Alogliptin 25 mg QD | -0.66 |
| Alogliptin 50 mg QD | -0.77 |
| Voglibose 0.2 mg TID | -0.28 |
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 44 and glycosylated hemoglobin collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 44.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.29 |
| Alogliptin 12.5 mg QD | -0.59 |
| Alogliptin 25 mg QD | -0.71 |
| Alogliptin 50 mg QD | -0.79 |
| Voglibose 0.2 mg TID | -0.35 |
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 48 and glycosylated hemoglobin collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 48.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.43 |
| Alogliptin 12.5 mg QD | -0.66 |
| Alogliptin 25 mg QD | -0.76 |
| Alogliptin 50 mg QD | -0.83 |
| Voglibose 0.2 mg TID | -0.40 |
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 52 and glycosylated hemoglobin collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 52.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.49 |
| Alogliptin 12.5 mg QD | -0.65 |
| Alogliptin 25 mg QD | -0.74 |
| Alogliptin 50 mg QD | -0.85 |
| Voglibose 0.2 mg TID | -0.37 |
The change between the value of insulin collected at week 52 or final visit and insulin collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | μU·hr/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -6.93 |
| Alogliptin 12.5 mg QD | -1.67 |
| Alogliptin 25 mg QD | 0.43 |
| Alogliptin 50 mg QD | -1.56 |
| Voglibose 0.2 mg TID | -14.65 |
The change between the value of insulin collected at week 12 and insulin collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 12
| Intervention | μU·hr/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 0.49 |
| Alogliptin 12.5 mg QD | 2.63 |
| Alogliptin 25 mg QD | 4.44 |
| Alogliptin 50 mg QD | -0.03 |
| Voglibose 0.2 mg TID | -15.40 |
The change between the value of insulin collected at week 24 and insulin collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 24.
| Intervention | μU·hr/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -1.89 |
| Alogliptin 12.5 mg QD | 4.50 |
| Alogliptin 25 mg QD | 2.85 |
| Alogliptin 50 mg QD | -0.98 |
| Voglibose 0.2 mg TID | -16.21 |
The change between the value of insulin collected at week 52 and insulin collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 52.
| Intervention | μU·hr/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -7.62 |
| Alogliptin 12.5 mg QD | -1.71 |
| Alogliptin 25 mg QD | -0.44 |
| Alogliptin 50 mg QD | -2.30 |
| Voglibose 0.2 mg TID | -15.66 |
A treatment-emergent adverse event (TEAE) is defined as an adverse event with an onset that occurs after receiving study drug and within 30 days after receiving the last dose of study drug. A TEAE may also be a pre-treatment adverse event or a concurrent medical condition diagnosed prior to the date of first dose of study drug, which increases in intensity after the start of dosing. Adverse events data with onset occurring more than 30 days after last dose of study drug (AE start date - last dose date >30) will be listed, but not included in the summary tables below. (NCT01263496)
Timeframe: 52 Weeks.
| Intervention | participants (Number) | ||
|---|---|---|---|
| Serious Adverse Event | Serious Adverse Event Related to Study Drug | Other Adverse Events (Incidence ≥3%) | |
| Alogliptin 12.5 mg QD | 5 | 2 | 81 |
| Alogliptin 25 mg QD | 8 | 2 | 81 |
| Alogliptin 50 mg QD | 5 | 2 | 88 |
| Alogliptin 6.25 mg QD | 1 | 1 | 78 |
| Voglibose 0.2 mg TID | 4 | 0 | 74 |
The change between the value of blood glucose collected at week 24 and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 24.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 64.3 |
| Alogliptin 12.5 mg QD | 55.5 |
| Alogliptin 25 mg QD | 55.5 |
| Alogliptin 50 mg QD | 55.9 |
| Voglibose 0.2 mg TID | 56.6 |
The change between the value of blood glucose collected at week 52 and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 52.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 65.7 |
| Alogliptin 12.5 mg QD | 62.6 |
| Alogliptin 25 mg QD | 58.3 |
| Alogliptin 50 mg QD | 51.8 |
| Voglibose 0.2 mg TID | 61.0 |
The change between the value of blood glucose collected at week 52 or final visit and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | mg·hr/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -53.5 |
| Alogliptin 12.5 mg QD | -55.1 |
| Alogliptin 25 mg QD | -67.6 |
| Alogliptin 50 mg QD | -91.3 |
| Voglibose 0.2 mg TID | -56.4 |
The change between the value of blood glucose collected at week 12 and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 12.
| Intervention | mg·hr/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -57.0 |
| Alogliptin 12.5 mg QD | -55.4 |
| Alogliptin 25 mg QD | -67.8 |
| Alogliptin 50 mg QD | -80.5 |
| Voglibose 0.2 mg TID | -50.0 |
The change between the value of blood glucose collected at week 24 and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 24.
| Intervention | mg·hr/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -43.9 |
| Alogliptin 12.5 mg QD | -52.5 |
| Alogliptin 25 mg QD | -69.8 |
| Alogliptin 50 mg QD | -75.1 |
| Voglibose 0.2 mg TID | -62.4 |
The change between the value of blood glucose collected at week 52 and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 52.
| Intervention | mg·hr/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -59.5 |
| Alogliptin 12.5 mg QD | -62.0 |
| Alogliptin 25 mg QD | -69.0 |
| Alogliptin 50 mg QD | -88.7 |
| Voglibose 0.2 mg TID | -65.4 |
The change between the value of C-peptide collected at week 52 or final visit and C-peptide collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | ng·hr/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 0.99 |
| Alogliptin 12.5 mg QD | 1.45 |
| Alogliptin 25 mg QD | 1.14 |
| Alogliptin 50 mg QD | 1.41 |
| Voglibose 0.2 mg TID | 0.15 |
The change between the value of C-peptide collected at week 12 and C-peptide collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 12.
| Intervention | ng·hr/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 0.56 |
| Alogliptin 12.5 mg QD | 0.97 |
| Alogliptin 25 mg QD | 0.96 |
| Alogliptin 50 mg QD | 0.99 |
| Voglibose 0.2 mg TID | -0.39 |
The change between the value of C-peptide collected at week 24 and C-peptide collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 24.
| Intervention | ng·hr/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 0.93 |
| Alogliptin 12.5 mg QD | 1.35 |
| Alogliptin 25 mg QD | 1.14 |
| Alogliptin 50 mg QD | 1.38 |
| Voglibose 0.2 mg TID | -0.10 |
The change between the value of glucagons collected at week 52 and glucagons collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 52.
| Intervention | pg·hr/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -10.7 |
| Alogliptin 12.5 mg QD | -11.3 |
| Alogliptin 25 mg QD | -14.5 |
| Alogliptin 50 mg QD | -12.5 |
| Voglibose 0.2 mg TID | -13.8 |
The change between the value of fasting C-peptide collected at week 52 or final visit and fasting C-peptide collected at baseline. (NCT01263496)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 0.34 |
| Alogliptin 12.5 mg QD | 0.44 |
| Alogliptin 25 mg QD | 0.32 |
| Alogliptin 50 mg QD | 0.48 |
| Voglibose 0.2 mg TID | 0.18 |
The change between the value of fasting C-peptide collected at week 16 and fasting C-peptide collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 16.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 0.08 |
| Alogliptin 12.5 mg QD | 0.22 |
| Alogliptin 25 mg QD | 0.33 |
| Alogliptin 50 mg QD | 0.46 |
| Voglibose 0.2 mg TID | -0.01 |
The change between the value of fasting C-peptide collected at week 20 and fasting C-peptide collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 20.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 0.15 |
| Alogliptin 12.5 mg QD | 0.35 |
| Alogliptin 25 mg QD | 0.28 |
| Alogliptin 50 mg QD | 0.56 |
| Voglibose 0.2 mg TID | -0.16 |
The change between the value of fasting C-peptide collected at week 24 and fasting C-peptide collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 24.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 0.12 |
| Alogliptin 12.5 mg QD | 0.26 |
| Alogliptin 25 mg QD | 0.20 |
| Alogliptin 50 mg QD | 0.23 |
| Voglibose 0.2 mg TID | -0.10 |
The change between the value of fasting C-peptide collected at week 28 and fasting C-peptide collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 28.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 0.11 |
| Alogliptin 12.5 mg QD | 0.21 |
| Alogliptin 25 mg QD | 0.26 |
| Alogliptin 50 mg QD | 0.29 |
| Voglibose 0.2 mg TID | -0.04 |
The change between the value of fasting C-peptide collected at week 32 and fasting C-peptide collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 32.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 0.03 |
| Alogliptin 12.5 mg QD | 0.41 |
| Alogliptin 25 mg QD | 0.45 |
| Alogliptin 50 mg QD | 0.37 |
| Voglibose 0.2 mg TID | -0.01 |
The change between the value of blood glucose collected at week 52 or final visit and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 65.0 |
| Alogliptin 12.5 mg QD | 63.8 |
| Alogliptin 25 mg QD | 60.4 |
| Alogliptin 50 mg QD | 52.6 |
| Voglibose 0.2 mg TID | 52.6 |
The change between the value of blood glucose collected at week 12 and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263496)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | 62.9 |
| Alogliptin 12.5 mg QD | 61.8 |
| Alogliptin 25 mg QD | 56.4 |
| Alogliptin 50 mg QD | 55.8 |
| Voglibose 0.2 mg TID | 64.8 |
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 and glycosylated hemoglobin collected at baseline. (NCT01263496)
Timeframe: Baseline and Week 24.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 6.25 mg QD | -0.47 |
| Alogliptin 12.5 mg QD | -0.61 |
| Alogliptin 25 mg QD | -0.66 |
| Alogliptin 50 mg QD | -0.83 |
| Voglibose 0.2 mg TID | -0.29 |
The change between the value of fasting C-peptide collected at week 36 and fasting C-peptide collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 36.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.33 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.38 |
The change between the value of fasting C-peptide collected at week 40 and fasting C-peptide collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 40.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.30 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.37 |
The change between the value of fasting C-peptide collected at week 44 and fasting C-peptide collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 44.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.08 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.25 |
The change between the value of fasting C-peptide collected at week 48 and fasting C-peptide collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 48.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.45 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.38 |
The change between the value of fasting C-peptide collected at week 52 and fasting C-peptide collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 52.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.80 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.40 |
The change between the value of fasting C-peptide collected at week 8 and fasting C-peptide collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 8.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.05 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.11 |
The change between the value of fasting plasma glucose collected at week 52 or final visit and fasting plasma glucose collected at baseline. (NCT01263509)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -17.5 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -23.3 |
The change between the value of fasting plasma glucose collected at week 12 and fasting plasma glucose collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -17.1 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -18.8 |
The change between the value of fasting plasma glucose collected at week 16 and fasting plasma glucose collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 16.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -16.0 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -15.3 |
The change between the value of fasting plasma glucose collected at week 20 and fasting plasma glucose collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 20.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -15.6 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -15.0 |
The change between the value of fasting plasma glucose collected at week 24 and fasting plasma glucose collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 24.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -13.8 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -15.6 |
The change between the value of fasting plasma glucose collected at week 28 and fasting plasma glucose collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 28.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -14.5 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -21.9 |
The change between the value of fasting plasma glucose collected at week 32 and fasting plasma glucose collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 32.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -17.7 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -20.1 |
The change between the value of fasting plasma glucose collected at week 36 and fasting plasma glucose collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 36.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -17.3 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -22.6 |
The change between the value of fasting plasma glucose collected at week 40 and fasting plasma glucose collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 40.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -19.7 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -22.8 |
The change between the value of fasting plasma glucose collected at week 44 and fasting plasma glucose collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 44.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -21.5 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -24.4 |
The change between the value of fasting plasma glucose collected at week 48 and fasting plasma glucose collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 48.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -20.5 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -23.1 |
The change between the value of fasting plasma glucose collected at week 52 and fasting plasma glucose collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 52.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -20.7 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -24.0 |
The change between the value of fasting plasma glucose collected at week 8 and fasting plasma glucose collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 8.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -18.2 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -20.4 |
The change between the value of glucagons collected at week 52 or final visit and glucagons collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | pg•hr/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -11.7 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -20.9 |
The change between the value of glucagons collected at week 12 and glucagons collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 12.
| Intervention | pg•hr/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -14.3 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -20.0 |
The change between the value of glucagons collected at week 24 and glucagons collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 24.
| Intervention | pg•hr/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -4.6 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -6.8 |
The change between the value of glucagons collected at week 52 and glucagons collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 52.
| Intervention | pg•hr/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -12.0 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -22.2 |
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 52 or final visit and glycosylated hemoglobin collected at baseline. (NCT01263509)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -0.81 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.89 |
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 12 and glycosylated hemoglobin collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 12.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -0.89 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.96 |
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 16 and glycosylated hemoglobin collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 16.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -0.91 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.96 |
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 20 and glycosylated hemoglobin collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 20.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -0.90 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.89 |
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 and glycosylated hemoglobin collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 24.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -0.83 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.88 |
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 28 and glycosylated hemoglobin collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 28.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -0.81 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.89 |
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 32 and glycosylated hemoglobin collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 32.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -0.80 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.85 |
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 36 and glycosylated hemoglobin collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 36.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -0.82 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.90 |
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 40 and glycosylated hemoglobin collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 40.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -0.78 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.92 |
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 44 and glycosylated hemoglobin collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 44.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -0.88 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.94 |
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 48 and glycosylated hemoglobin collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 48.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -0.92 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.94 |
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 52 and glycosylated hemoglobin collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 52.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -0.95 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.95 |
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 8 and glycosylated hemoglobin collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 8.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -0.69 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -0.79 |
The change between the value of insulin collected at week 52 or final visit and insulin collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | μU•hr/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -0.61 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.01 |
The change between the value of insulin collected at week 12 and insulin collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 12.
| Intervention | μU•hr/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 3.05 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 2.95 |
The change between the value of insulin collected at week 24 and insulin collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 24.
| Intervention | μU•hr/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 4.42 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 2.26 |
The change between the value of insulin collected at week 52 and insulin collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 52.
| Intervention | μU•hr/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -1.28 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.18 |
A treatment-emergent adverse event (TEAE) is defined as an adverse event with an onset that occurs after receiving study drug and within 30 days after receiving the last dose of study drug. A TEAE may also be a pre-treatment adverse event or a concurrent medical condition diagnosed prior to the date of first dose of study drug, which increases in intensity after the start of dosing. Adverse events data with onset occurring more than 30 days after last dose of study drug (AE start date - last dose date >30) will be listed, but not included in the summary tables below. (NCT01263509)
Timeframe: 52 Weeks.
| Intervention | participants (Number) | ||
|---|---|---|---|
| Serious Adverse Event | Serious Adverse Event Related to Study Drug | Other Adverse Events (Incidence ≥3%) | |
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 6 | 0 | 85 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 7 | 1 | 73 |
The change between the value of blood glucose collected at week 52 or final visit and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 39.6 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 39.4 |
The change between the value of blood glucose collected at week 12 and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 41.2 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 37.6 |
The change between the value of blood glucose collected at week 24 and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 24.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 38.0 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 37.1 |
The change between the value of blood glucose collected at week 52 and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 52.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 39.0 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 40.8 |
The change between the value of blood glucose collected at week 52 or final visit and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | mg•hr/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -77.5 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -82.2 |
The change between the value of blood glucose collected at week 12 and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 12.
| Intervention | mg•hr/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -73.2 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -76.8 |
The change between the value of blood glucose collected at week 24 and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 24.
| Intervention | mg•hr/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -69.0 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -70.4 |
The change between the value of blood glucose collected at week 52 and blood glucose collected at baseline. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 52.
| Intervention | mg•hr/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | -83.5 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | -83.4 |
The change between the value of C-peptide collected at week 52 or final visit and C-peptide collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | ng•hr/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 1.05 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.80 |
The change between the value of C-peptide collected at week 12 and C-peptide collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 12.
| Intervention | ng•hr/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.71 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.71 |
The change between the value of C-peptide collected at week 24 and C-peptide collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 24.
| Intervention | ng•hr/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 1.38 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 1.12 |
The change between the value of C-peptide collected at week 52 and C-peptide collected at baseline as measured by the meal tolerance test. Meal tolerance test measures blood glucose, insulin, C-peptide and glucagon through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01263509)
Timeframe: Baseline and Week 52.
| Intervention | ng•hr/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.96 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 2.18 |
The change between the value of fasting C-peptide collected at week 52 or final visit and fasting C-peptide collected at baseline. (NCT01263509)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.31 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.29 |
The change between the value of fasting C-peptide collected at week 12 and fasting C-peptide collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 12.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.10 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.13 |
The change between the value of fasting C-peptide collected at week 16 and fasting C-peptide collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 16.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.24 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.21 |
The change between the value of fasting C-peptide collected at week 20 and fasting C-peptide collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 20.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.24 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.15 |
The change between the value of fasting C-peptide collected at week 24 and fasting C-peptide collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 24.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.19 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.14 |
The change between the value of fasting C-peptide collected at week 28 and fasting C-peptide collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 28.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.18 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.25 |
The change between the value of fasting C-peptide collected at week 32 and fasting C-peptide collected at baseline. (NCT01263509)
Timeframe: Baseline and Week 32.
| Intervention | ng/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Voglibose 0.2 mg TID | 0.47 |
| Alogliptin 25 mg QD and Voglibose 0.2 mg TID | 0.31 |
Clinical response was assessed by the percentage of participants with HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) less than or equal to 7.0% at Week 16. (NCT01289119)
Timeframe: Week 16
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 30.0 |
| Alogliptin Monotherapy | 63.3 |
| Metformin | 25.8 |
| Metformin + Alogliptin Add-on Therapy | 55.1 |
| Pioglitazone | 31.7 |
| Pioglitazone + Alogliptin Add-on Therapy | 61.7 |
The change from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) at Weeks 4, 8 and 12. Least squares means are derived from an analysis of covariance (ANCOVA) model with treatment as a fixed effect, and baseline HbA1c as a covariate for the monotherapy, baseline HbA1c with baseline metformin dose as covariates for the metformin therapy, baseline HbA1c with baseline metformin therapy status and baseline pioglitazone dose as covariates for the pioglitazone therapy. (NCT01289119)
Timeframe: Baseline and Weeks 4, 8 and 12.
| Intervention | percentage glycosylated hemoglobin (Least Squares Mean) | ||
|---|---|---|---|
| Week 4 (n=90, 88, 97, 98, 63, 60) | Week 8 (n=90, 90, 97, 98, 63, 60) | Week 12 (n=90, 90, 97, 98, 63, 60) | |
| Alogliptin Monotherapy | -0.56 | -0.86 | -0.99 |
| Metformin | -0.15 | -0.15 | -0.24 |
| Metformin + Alogliptin Add-on Therapy | -0.43 | -0.66 | -0.86 |
| Pioglitazone | -0.09 | -0.31 | -0.25 |
| Pioglitazone + Alogliptin Add-on Therapy | -0.44 | -0.70 | -0.77 |
| Placebo | -0.24 | -0.39 | -0.41 |
The change between body weight measured at Baseline and body weight measured at Weeks 8 and 16. The least squares means are derived from an ANCOVA model with treatment as a fixed effect, and baseline body weight as a covariate for the monotherapy, baseline body weight with baseline metformin dose as covariates for the add-on to metformin therapy, baseline body weight with baseline metformin therapy status and baseline pioglitazone dose as covariates for the add-on to pioglitazone therapy. (NCT01289119)
Timeframe: Baseline and Weeks 8 and 16.
| Intervention | kg (Least Squares Mean) | |
|---|---|---|
| Week 8 (n=87, 86, 94, 96, 63, 59) | Week 16 (n=88, 87, 94, 96, 63, 59) | |
| Alogliptin Monotherapy | -0.71 | -0.89 |
| Metformin | -0.82 | -1.06 |
| Metformin + Alogliptin Add-on Therapy | -0.43 | -0.76 |
| Pioglitazone | -0.74 | -0.68 |
| Pioglitazone + Alogliptin Add-on Therapy | -0.15 | -0.10 |
| Placebo | -1.04 | -1.55 |
Clinical response was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 1.5% at Week 16. (NCT01289119)
Timeframe: Baseline and Week 16.
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 7.8 |
| Alogliptin Monotherapy | 23.3 |
| Metformin | 1.0 |
| Metformin + Alogliptin Add-on Therapy | 22.4 |
| Pioglitazone | 7.9 |
| Pioglitazone + Alogliptin Add-on Therapy | 8.3 |
Clinical response was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 1.0% at Week 16. (NCT01289119)
Timeframe: Baseline and Week 16
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 20.0 |
| Alogliptin Monotherapy | 50.0 |
| Metformin | 9.3 |
| Metformin + Alogliptin Add-on Therapy | 45.9 |
| Pioglitazone | 19.0 |
| Pioglitazone + Alogliptin Add-on Therapy | 46.7 |
Clinical response was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 0.5% at Week 16. (NCT01289119)
Timeframe: Baseline and Week 16
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 41.1 |
| Alogliptin Monotherapy | 84.4 |
| Metformin | 37.1 |
| Metformin + Alogliptin Add-on Therapy | 70.4 |
| Pioglitazone | 42.9 |
| Pioglitazone + Alogliptin Add-on Therapy | 76.7 |
The change from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) collected at Week 16. Least squares means are derived from an analysis of covariance (ANCOVA) model with treatment as a fixed effect, and baseline HbA1c as a covariate for the monotherapy, baseline HbA1c with baseline metformin dose as covariates for the metformin therapy, baseline HbA1c with baseline metformin therapy status and baseline pioglitazone dose as covariates for the pioglitazone therapy. (NCT01289119)
Timeframe: Baseline and Week 16.
| Intervention | percentage glycosylated hemoglobin (Least Squares Mean) |
|---|---|
| Placebo | -0.42 |
| Alogliptin Monotherapy | -0.99 |
| Metformin | -0.22 |
| Metformin + Alogliptin Add-on Therapy | -0.91 |
| Pioglitazone | -0.25 |
| Pioglitazone + Alogliptin Add-on Therapy | -0.76 |
Clinical response was assessed by the percentage of participants with a decrease from Baseline in HbA1c of greater than or equal to 2.0% at Week 16. (NCT01289119)
Timeframe: Baseline and Week 16.
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 2.2 |
| Alogliptin Monotherapy | 8.9 |
| Metformin | 0.0 |
| Metformin + Alogliptin Add-on Therapy | 9.2 |
| Pioglitazone | 1.6 |
| Pioglitazone + Alogliptin Add-on Therapy | 3.3 |
Clinical response was assessed by the percentage of participants with HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) less than or equal to 6.5% at Week 16. (NCT01289119)
Timeframe: Week 16
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 12.2 |
| Alogliptin Monotherapy | 36.7 |
| Metformin | 4.1 |
| Metformin + Alogliptin Add-on Therapy | 21.4 |
| Pioglitazone | 9.5 |
| Pioglitazone + Alogliptin Add-on Therapy | 30.0 |
Clinical response was assessed by the percentage of participants with HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) less than or equal to 7.5% at Week 16. (NCT01289119)
Timeframe: Week 16
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 53.3 |
| Alogliptin Monotherapy | 81.1 |
| Metformin | 50.5 |
| Metformin + Alogliptin Add-on Therapy | 80.6 |
| Pioglitazone | 47.6 |
| Pioglitazone + Alogliptin Add-on Therapy | 85.0 |
Marked Hyperglycemia was defined as fasting plasma glucose greater than or equal to 200 mg/dL (11.1 mmol/L). (NCT01289119)
Timeframe: Randomization to Week 16.
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 16.9 |
| Alogliptin Monotherapy | 4.5 |
| Metformin | 25.8 |
| Metformin + Alogliptin Add-on Therapy | 13.4 |
| Pioglitazone | 23.8 |
| Pioglitazone + Alogliptin Add-on Therapy | 8.3 |
The change from Baseline in fasting plasma glucose (FPG) at Weeks 4, 8, 12 and 16. Least squares means are derived from an ANCOVA model with treatment as a fixed effect, and baseline FPG as a covariate for the monotherapy, baseline FPG with baseline metformin dose as covariates for the metformin therapy, baseline FPG with baseline metformin therapy status and baseline pioglitazone dose as covariates for the pioglitazone therapy. (NCT01289119)
Timeframe: Baseline and Weeks 4, 8, 12 and 16.
| Intervention | mmol/L (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 4 (n=89, 87, 97, 97, 63, 60) | Week 8 (n=89, 89, 97, 97, 63, 60) | Week 12 (n=89, 89, 97, 97, 63, 60) | Week 16 (n=89, 89, 97, 97, 63, 60) | |
| Alogliptin Monotherapy | -0.719 | -1.015 | -1.123 | -1.243 |
| Metformin | -0.251 | -0.235 | -0.335 | -0.512 |
| Metformin + Alogliptin Add-on Therapy | -0.985 | -1.265 | -1.270 | -1.240 |
| Pioglitazone | 0.284 | -0.038 | -0.187 | -0.114 |
| Pioglitazone + Alogliptin Add-on Therapy | -0.985 | -0.924 | -1.177 | -1.070 |
| Placebo | -0.331 | -0.330 | -0.411 | -0.317 |
The change between the value of fasting plasma glucose collected at week 12 or final visit and glycosylated hemoglobin collected at baseline. (NCT01318070)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30mg QD | -14.9 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -18.9 |
| Pioglitazone 15 mg or 30 mg QD | -2.4 |
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 12 and glycosylated hemoglobin collected at baseline. (NCT01318070)
Timeframe: Baseline and Week 12.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30mg QD | -0.91 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.97 |
| Pioglitazone 15 mg or 30 mg QD | -0.19 |
The change between the value of fasting plasma glucose collected at week 8 and glycosylated hemoglobin collected at baseline. (NCT01318070)
Timeframe: Baseline and Week 8.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30mg QD | -17.1 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -21.3 |
| Pioglitazone 15 mg or 30 mg QD | -4.2 |
The change between the value of fasting plasma glucose collected at week 4 and glycosylated hemoglobin collected at baseline. (NCT01318070)
Timeframe: Baseline and Week 4.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30mg QD | -14.4 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -17.9 |
| Pioglitazone 15 mg or 30 mg QD | -3.1 |
The change between the value of blood glucose measured by the meal tolerance test collected at week 12 or final visit and blood glucose measured by the meal tolerance test collected at baseline. Meal tolerance test measures blood glucose through blood samples drawn before a meal and 2 hours after the start of the meal. (NCT01318070)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30mg QD | 58.3 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | 49.4 |
| Pioglitazone 15 mg or 30 mg QD | 70.6 |
The change between the value of fasting plasma glucose collected at week 2 and glycosylated hemoglobin collected at baseline. (NCT01318070)
Timeframe: Baseline and Week 2.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30mg QD | -12.8 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -17.0 |
| Pioglitazone 15 mg or 30 mg QD | -3.9 |
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 8 and glycosylated hemoglobin collected at baseline. (NCT01318070)
Timeframe: Baseline and Week 8.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30mg QD | -0.76 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.81 |
| Pioglitazone 15 mg or 30 mg QD | -0.17 |
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 4 and glycosylated hemoglobin collected at baseline. (NCT01318070)
Timeframe: Baseline and Week 4.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30mg QD | -0.47 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.46 |
| Pioglitazone 15 mg or 30 mg QD | -0.10 |
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 2 and glycosylated hemoglobin collected at baseline. (NCT01318070)
Timeframe: Baseline and Week 2.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30mg QD | -0.22 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.22 |
| Pioglitazone 15 mg or 30 mg QD | -0.04 |
The change between the value of fasting plasma glucose collected at week 8 and baseline. (NCT01318083)
Timeframe: Baseline and Week 8.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride QD or BID | -22.3 |
| Alogliptin 25 mg QD and Glimepiride QD or BID | -17.4 |
| Glimepiride 1, 2, 3 or 4 mg QD or BID | 5.3 |
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 12 or final visit and glycosylated hemoglobin collected at baseline. (NCT01318083)
Timeframe: Baseline and Week 12.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride QD or BID | -0.60 |
| Alogliptin 25 mg QD and Glimepiride QD or BID | -0.66 |
| Glimepiride 1, 2, 3 or 4 mg QD or BID | 0.34 |
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 2 and glycosylated hemoglobin collected at baseline. (NCT01318083)
Timeframe: Baseline and Week 2.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride QD or BID | -0.12 |
| Alogliptin 25 mg QD and Glimepiride QD or BID | -0.13 |
| Glimepiride 1, 2, 3 or 4 mg QD or BID | 0.08 |
The change between the value of blood glucose measured by the meal tolerance test collected at week 12 or final visit and blood glucose measured by the meal tolerance test collected at baseline. Meal tolerance test measures blood glucose through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01318083)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride QD or BID | 76.6 |
| Alogliptin 25 mg QD and Glimepiride QD or BID | 80.9 |
| Glimepiride 1, 2, 3 or 4 mg QD or BID | 100.0 |
The change between the value of fasting plasma glucose collected at week 12 or final visit and baseline. (NCT01318083)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride QD or BID | -22.3 |
| Alogliptin 25 mg QD and Glimepiride QD or BID | -15.9 |
| Glimepiride 1, 2, 3 or 4 mg QD or BID | 6.0 |
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 4 and glycosylated hemoglobin collected at baseline. (NCT01318083)
Timeframe: Baseline and Week 4.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride QD or BID | -0.32 |
| Alogliptin 25 mg QD and Glimepiride QD or BID | -0.36 |
| Glimepiride 1, 2, 3 or 4 mg QD or BID | 0.09 |
The change between the value of fasting plasma glucose collected at week 2 and baseline. (NCT01318083)
Timeframe: Baseline and Week 2.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride QD or BID | -17.5 |
| Alogliptin 25 mg QD and Glimepiride QD or BID | -17.4 |
| Glimepiride 1, 2, 3 or 4 mg QD or BID | 0.2 |
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 8 and glycosylated hemoglobin collected at baseline. (NCT01318083)
Timeframe: Baseline and Week 8.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride QD or BID | -0.52 |
| Alogliptin 25 mg QD and Glimepiride QD or BID | -0.59 |
| Glimepiride 1, 2, 3 or 4 mg QD or BID | 0.18 |
The change between the value of fasting plasma glucose collected at week 4 and baseline. (NCT01318083)
Timeframe: Baseline and Week 4.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride QD or BID | -21.2 |
| Alogliptin 25 mg QD and Glimepiride QD or BID | -22.9 |
| Glimepiride 1, 2, 3 or 4 mg QD or BID | 2.0 |
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 4 and glycosylated hemoglobin collected at baseline. (NCT01318109)
Timeframe: Baseline and Week 4.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Metformin 500mg BID or 750mg TID | -0.29 |
| Alogliptin 25mg QD and Metformin 500mg BID or 750mg TID | -0.31 |
| Metformin 500mg BID or 750mg TID | 0.09 |
The change between the value of fasting plasma glucose collected at week 12 or final visit and baseline. (NCT01318109)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Metformin 500mg BID or 750mg TID | -19.0 |
| Alogliptin 25mg QD and Metformin 500mg BID or 750mg TID | -23.1 |
| Metformin 500mg BID or 750mg TID | -0.8 |
The change between the value of fasting plasma glucose collected at week 2 and baseline. (NCT01318109)
Timeframe: Baseline and Week 2.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Metformin 500mg BID or 750mg TID | -19.2 |
| Alogliptin 25mg QD and Metformin 500mg BID or 750mg TID | -23.2 |
| Metformin 500mg BID or 750mg TID | 0.0 |
The change between the value of fasting plasma glucose collected at week 4 and baseline. (NCT01318109)
Timeframe: Baseline and Week 4.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Metformin 500mg BID or 750mg TID | -19.8 |
| Alogliptin 25mg QD and Metformin 500mg BID or 750mg TID | -23.5 |
| Metformin 500mg BID or 750mg TID | -2.2 |
The change between the value of fasting plasma glucose collected at week 8 and baseline. (NCT01318109)
Timeframe: Baseline and Week 8.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Metformin 500mg BID or 750mg TID | -22.0 |
| Alogliptin 25mg QD and Metformin 500mg BID or 750mg TID | -21.3 |
| Metformin 500mg BID or 750mg TID | -3.1 |
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 8 and glycosylated hemoglobin collected at baseline. (NCT01318109)
Timeframe: Baseline and Week 8.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Metformin 500mg BID or 750mg TID | -0.49 |
| Alogliptin 25mg QD and Metformin 500mg BID or 750mg TID | -0.56 |
| Metformin 500mg BID or 750mg TID | 0.13 |
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 12 or final visit and glycosylated hemoglobin collected at baseline. (NCT01318109)
Timeframe: Baseline and Week 12.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Metformin 500mg BID or 750mg TID | -0.54 |
| Alogliptin 25mg QD and Metformin 500mg BID or 750mg TID | -0.64 |
| Metformin 500mg BID or 750mg TID | 0.21 |
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 2 and glycosylated hemoglobin collected at baseline. (NCT01318109)
Timeframe: Baseline and Week 2.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Metformin 500mg BID or 750mg TID | -0.13 |
| Alogliptin 25mg QD and Metformin 500mg BID or 750mg TID | -0.13 |
| Metformin 500mg BID or 750mg TID | 0.06 |
The change between the value of blood glucose measured by the meal tolerance test collected at week 12 or final visit and blood glucose measured by the meal tolerance test collected at baseline. Meal tolerance test measures blood glucose through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01318109)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Metformin 500mg BID or 750mg TID | 61.7 |
| Alogliptin 25mg QD and Metformin 500mg BID or 750mg TID | 64.2 |
| Metformin 500mg BID or 750mg TID | 70.6 |
The change between the value of fasting blood glucose collected at week 28 and baseline. (NCT01318122)
Timeframe: Baseline and Week 28.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -5.6 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -9.1 |
The change between the value of fasting blood glucose collected at week 44 and baseline. (NCT01318122)
Timeframe: Baseline and Week 44.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -10.4 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -10.4 |
The change between the value of fasting blood glucose collected at week 24 and baseline. (NCT01318122)
Timeframe: Baseline and Week 24.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -10.0 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -10.7 |
The change between the value of fasting blood glucose collected at week 20 and baseline. (NCT01318122)
Timeframe: Baseline and Week 20.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -10.1 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -13.9 |
The change between the value of fasting blood glucose collected at week 6 and baseline. (NCT01318122)
Timeframe: Baseline and Week 16.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -11.9 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -13.4 |
The change between the value of fasting blood glucose collected at week 52 or final visit and baseline. (NCT01318122)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -11.4 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -11.1 |
The change between the value of blood glucose measured by the meal tolerance test collected at week 52 or final visit and blood glucose measured by the meal tolerance test collected at baseline. Meal tolerance test measures blood glucose through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01318122)
Timeframe: Baseline and Week 52.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | 59.1 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | 57.2 |
The change between the value of blood glucose measured by the meal tolerance test collected at week 24 and blood glucose measured by the meal tolerance test collected at baseline. Meal tolerance test measures blood glucose through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01318122)
Timeframe: Baseline and Week 24.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | 55.9 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | 47.9 |
The change between the value of blood glucose measured by the meal tolerance test collected at week 12 and blood glucose measured by the meal tolerance test collected at baseline. Meal tolerance test measures blood glucose through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01318122)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | 58.3 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | 49.5 |
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 36 and glycosylated hemoglobin collected at baseline. (NCT01318122)
Timeframe: Baseline and Week 36.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -0.67 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.69 |
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 40 and glycosylated hemoglobin collected at baseline. (NCT01318122)
Timeframe: Baseline and Week 40.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -0.65 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.66 |
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 44 and glycosylated hemoglobin collected at baseline. (NCT01318122)
Timeframe: Baseline and Week 44.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -0.70 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.74 |
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 48 and glycosylated hemoglobin collected at baseline. (NCT01318122)
Timeframe: Baseline and Week 48.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -0.73 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.76 |
The change between the value of blood glucose measured by the meal tolerance test collected at week 52 or end of study and blood glucose measured by the meal tolerance test collected at baseline. Meal tolerance test measures blood glucose through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01318122)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | 59.8 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | 56.8 |
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 52 and glycosylated hemoglobin collected at baseline. (NCT01318122)
Timeframe: Baseline and Week 52.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -0.77 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.79 |
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 8 and glycosylated hemoglobin collected at baseline. (NCT01318122)
Timeframe: Baseline and Week 8.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -0.68 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.73 |
Treatment-emergent adverse events (TEAE) are adverse events with an onset that occurs after receiving study drug and within 30 days after receiving the last dose of study drug. A TEAE may also be a pre-treatment adverse event or a concurrent medical condition diagnosed prior to the date of first dose of study drug that increases in severity after the start of dosing. (NCT01318122)
Timeframe: 52 Weeks.
| Intervention | participants (Number) | |
|---|---|---|
| Number of Participants with Serious Adverse Event | Number of Participants with Other Adverse Event | |
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | 14 | 143 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | 11 | 146 |
The change between the value of fasting blood glucose collected at week 12 and baseline. (NCT01318122)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -13.4 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -16.3 |
The change between the value of fasting blood glucose collected at week 40 and baseline. (NCT01318122)
Timeframe: Baseline and Week 40.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -9.5 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -10.6 |
The change between the value of fasting blood glucose collected at week 36 and baseline. (NCT01318122)
Timeframe: Baseline and Week 36.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -7.1 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -11.9 |
The change between the value of fasting blood glucose collected at week 32 and baseline. (NCT01318122)
Timeframe: Baseline and Week 32.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -7.9 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -10.4 |
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 32 and glycosylated hemoglobin collected at baseline. (NCT01318122)
Timeframe: Baseline and Week 32.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -0.72 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.72 |
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 28 and glycosylated hemoglobin collected at baseline. (NCT01318122)
Timeframe: Baseline and Week 28.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -0.75 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.76 |
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 and glycosylated hemoglobin collected at baseline. (NCT01318122)
Timeframe: Baseline and Week 24.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -0.78 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.82 |
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 20 and glycosylated hemoglobin collected at baseline. (NCT01318122)
Timeframe: Baseline and Week 20.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -0.84 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.90 |
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 16 and glycosylated hemoglobin collected at baseline. (NCT01318122)
Timeframe: Baseline and Week 16.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -0.86 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.92 |
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 12 and glycosylated hemoglobin collected at baseline. (NCT01318122)
Timeframe: Baseline and Week 12.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -0.81 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.88 |
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 52 or final visit and glycosylated hemoglobin collected at baseline. (NCT01318122)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -0.65 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -0.65 |
The change between the value of fasting blood glucose collected at week 8 and baseline. (NCT01318122)
Timeframe: Baseline and Week 8.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -15.5 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -18.1 |
The change between the value of fasting blood glucose collected at week 52 and baseline. (NCT01318122)
Timeframe: Baseline and Week 52.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -12.8 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -13.6 |
The change between the value of fasting blood glucose collected at week 48 and baseline. (NCT01318122)
Timeframe: Baseline and Week 48.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Pioglitazone 15 or 30 mg QD | -12.2 |
| Alogliptin 25 mg QD and Pioglitazone 15 or 30 mg QD | -14.0 |
The change between the value of fasting blood glucose collected at week 36 and baseline. (NCT01318135)
Timeframe: Baseline and Week 36.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -25.5 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -26.7 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -23.4 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -26.0 |
The change between the value of fasting blood glucose collected at week 40 and baseline. (NCT01318135)
Timeframe: Baseline and Week 40.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -21.3 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -22.7 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -19.8 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -23.2 |
The change between the value of blood glucose measured by the meal tolerance test collected at week 24 and blood glucose measured by the meal tolerance test collected at baseline. Meal tolerance test measures blood glucose through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01318135)
Timeframe: Baseline and Week 24.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | 87.4 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | 77.9 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | 60.7 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | 62.4 |
The change between the value of fasting blood glucose collected at week 44 and baseline. (NCT01318135)
Timeframe: Baseline and Week 44.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -15.4 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -21.9 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -16.3 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -24.0 |
The change between the value of fasting blood glucose collected at week 48 and baseline. (NCT01318135)
Timeframe: Baseline and Week 48.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -13.6 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -16.6 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -14.3 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -23.3 |
The change between the value of fasting blood glucose collected at week 52 and baseline. (NCT01318135)
Timeframe: Baseline and Week 52.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -13.3 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -11.9 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -14.0 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -16.1 |
The change between the value of fasting blood glucose collected at week 8 and baseline. (NCT01318135)
Timeframe: Baseline and Week 8.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -20.7 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -19.6 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -22.0 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -23.4 |
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 final visit and glycosylated hemoglobin collected at baseline. (NCT01318135)
Timeframe: Baseline and Final Visit (up to 52).
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -0.42 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -0.58 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -0.44 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -0.58 |
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 12 and glycosylated hemoglobin collected at baseline. (NCT01318135)
Timeframe: Baseline and Week 12.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -0.63 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -0.72 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -0.61 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -0.71 |
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 16 and glycosylated hemoglobin collected at baseline. (NCT01318135)
Timeframe: Baseline and Week 16.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -0.66 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -0.76 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -0.69 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -0.78 |
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 20 and glycosylated hemoglobin collected at baseline. (NCT01318135)
Timeframe: Baseline and Week 20.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -0.63 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -0.70 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -0.67 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -0.78 |
The change between the value of fasting blood glucose collected at week 32 and baseline. (NCT01318135)
Timeframe: Baseline and Week 32.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -22.4 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -26.1 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -23.2 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -28.2 |
Treatment-emergent adverse events (TEAE) are defined as any unfavorable and unintended sign, symptom or disease temporally associated with the use of a medicinal product reported from first dose of study drug through 30 days after receiving the last dose of study drug. A TEAE may also be a pretreatment adverse event or a concurrent medical condition diagnosed prior to the date of first dose of study drug that increases in severity after the start of dosing. (NCT01318135)
Timeframe: 52 Weeks.
| Intervention | participants (Number) | |
|---|---|---|
| Serious Adverse Event | Other Adverse Event (≥3% Frequency Threshold) | |
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | 16 | 116 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | 7 | 108 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | 3 | 134 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | 5 | 113 |
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 8 and glycosylated hemoglobin collected at baseline. (NCT01318135)
Timeframe: Baseline and Week 8.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -0.53 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -0.65 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -0.53 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -0.59 |
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 52 and glycosylated hemoglobin collected at baseline. (NCT01318135)
Timeframe: Baseline and Week 52.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -0.33 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -0.53 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -0.29 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -0.53 |
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 48 and glycosylated hemoglobin collected at baseline. (NCT01318135)
Timeframe: Baseline and Week 48.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -0.40 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -0.61 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -0.36 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -0.62 |
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 44 and glycosylated hemoglobin collected at baseline. (NCT01318135)
Timeframe: Baseline and Week 44.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -0.48 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -0.71 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -0.47 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -0.70 |
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 40 and glycosylated hemoglobin collected at baseline. (NCT01318135)
Timeframe: Baseline and Week 40.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -0.66 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -0.74 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -0.63 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -0.74 |
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 36 and glycosylated hemoglobin collected at baseline. (NCT01318135)
Timeframe: Baseline and Week 36.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -0.64 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -0.77 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -0.67 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -0.79 |
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 32 and glycosylated hemoglobin collected at baseline. (NCT01318135)
Timeframe: Baseline and Week 32.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -0.63 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -0.77 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -0.67 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -0.81 |
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 and glycosylated hemoglobin collected at baseline. (NCT01318135)
Timeframe: Baseline and Week 24.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -0.59 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -0.70 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -0.68 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -0.78 |
The change between the value of blood glucose measured by the meal tolerance test collected at final visit and blood glucose measured by the meal tolerance test collected at baseline. Meal tolerance test measures blood glucose through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01318135)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | 84.8 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | 84.9 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | 63.5 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | 63.7 |
The change between the value of blood glucose measured by the meal tolerance test collected at week 12 and blood glucose measured by the meal tolerance test collected at baseline. Meal tolerance test measures blood glucose through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01318135)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | 80.2 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | 80.1 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | 61.6 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | 64.0 |
The change between the value of blood glucose measured by the meal tolerance test collected at week 52 and blood glucose measured by the meal tolerance test collected at baseline. Meal tolerance test measures blood glucose through blood samples drawn before a meal and at 2 hours after the start of the meal. (NCT01318135)
Timeframe: Baseline and Week 52.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | 83.8 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | 83.2 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | 62.5 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | 62.7 |
The change between the value of fasting blood glucose collected at final visit and baseline. (NCT01318135)
Timeframe: Baseline and Final Visit (up to Week 52).
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -16.0 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -13.0 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -16.4 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -17.7 |
The change between the value of fasting blood glucose collected at week 12 and baseline. (NCT01318135)
Timeframe: Baseline and Week 12.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -22.0 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -18.1 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -22.9 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -24.2 |
The change between the value of fasting blood glucose collected at week 6 and baseline. (NCT01318135)
Timeframe: Baseline and Week 16.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -22.3 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -17.8 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -21.8 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -26.1 |
The change between the value of fasting blood glucose collected at week 20 and baseline. (NCT01318135)
Timeframe: Baseline and Week 20.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -22.4 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -22.3 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -23.4 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -26.1 |
The change between the value of fasting blood glucose collected at week 24 and baseline. (NCT01318135)
Timeframe: Baseline and Week 24.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -24.0 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -25.0 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -25.6 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -26.3 |
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 28 and glycosylated hemoglobin collected at baseline. (NCT01318135)
Timeframe: Baseline and Week 28.
| Intervention | percentage of Glycosylated Hemoglobin (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -0.62 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -0.76 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -0.70 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -0.84 |
The change between the value of fasting blood glucose collected at week 28 and baseline. (NCT01318135)
Timeframe: Baseline and Week 28.
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD and Glimepiride 1- 6 mg QD or BID | -19.9 |
| Alogliptin 25 mg QD and Glimepiride 1 - 6 mg QD or BID | -25.9 |
| Alogliptin 12.5 mg QD and Metformin 500 mg BID or 750 mg TID | -25.8 |
| Alogliptin 25 mg QD and Metformin 500 mg BID or 750 mg TID | -28.2 |
Area under the plasma concentration-time curve from time 0 to infinity after administration of a single dose of the study drug. (NCT01391663)
Timeframe: Day 1-4
| Intervention | ng·hr/mL (Mean) |
|---|---|
| Alogliptin 12.5 mg QD | 895.28 |
| Alogliptin 25 mg QD | 1674.88 |
| Alogliptin 50 mg QD | 3306.68 |
| Placebo | NA |
Area under the curve from 0 to 24 hours after administrations of a single dose and multiple doses of the study drug. (NCT01391663)
Timeframe: Day 1-4, Day 10.
| Intervention | ng·hr/mL (Mean) | |
|---|---|---|
| Day 1 (n=12; n=12; n=12; n=12) | Day 10 (n=12; n=12; n=11; n=12) | |
| Alogliptin 12.5 mg QD | 601.65 | 842.17 |
| Alogliptin 25 mg QD | 1174.76 | 1625.58 |
| Alogliptin 50 mg QD | 2488.48 | 3389.21 |
| Placebo | NA | NA |
Time required for half of the drug to be eliminated from the plasma after administration of a single dose of the study drug. (NCT01391663)
Timeframe: Day 1-4
| Intervention | hr (Mean) |
|---|---|
| Alogliptin 12.5 mg QD | 20.67 |
| Alogliptin 25 mg QD | 19.45 |
| Alogliptin 50 mg QD | 17.00 |
| Placebo | NA |
CL/F is apparent clearance of the drug from the plasma after administration of a single dose of the study drug. (NCT01391663)
Timeframe: Day 1-4
| Intervention | L/hr (Mean) |
|---|---|
| Alogliptin 12.5 mg QD | 14.06 |
| Alogliptin 25 mg QD | 15.30 |
| Alogliptin 50 mg QD | 15.44 |
| Placebo | NA |
Time to reach the maximum plasma concentration (Tmax) after administrations of a single dose and multiple doses of the study drug (NCT01391663)
Timeframe: Day 1-4, Day 10.
| Intervention | hr (Median) | |
|---|---|---|
| Day 1 (n=12; n=12; n=12; n=12) | Day 10 (n=12; n=12; n=11; n=12) | |
| Alogliptin 12.5 mg QD | 1.49 | 1.02 |
| Alogliptin 25 mg QD | 1.01 | 2.00 |
| Alogliptin 50 mg QD | 3.00 | 1.02 |
| Placebo | NA | NA |
Maximum observed plasma concentration (Cmax) is the peak plasma concentration after administrations of a single dose and multiple doses of the study drug (NCT01391663)
Timeframe: Day 1-4, Day 10
| Intervention | ng/mL (Mean) | |
|---|---|---|
| Day 1 (n=12; n=12; n=12; n=12) | Day 10 (n=12; n=12; n=11; n=12) | |
| Alogliptin 12.5 mg QD | 55.28 | 75.38 |
| Alogliptin 25 mg QD | 114.08 | 154.83 |
| Alogliptin 50 mg QD | 246.00 | 335.36 |
| Placebo | NA | NA |
The change in the value of fasting glucose collected at Week 52 or the final visit relative to Baseline. (NCT01456130)
Timeframe: Baseline and Week 52
| Intervention | mg/dL (Mean) |
|---|---|
| Alogliptin | -10.5 |
An TEAE is any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have a causal relationship with this treatment. A serious TEAE is defined as any untoward medical occurrence that resulted in death, was life threatening, required or prolonged inpatient hospitalization, resulted in persistent or significant disability or incapacity, led to a congenital anomaly/birth defect or was an important medical event that may have required intervention to prevent any of items above. (NCT01456130)
Timeframe: 52 Weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Any adverse event | Adverse event leading to discontinuation | Serious adverse event (SAE) | SAE leading to discontinuation | Death | |
| Alogliptin | 57 | 5 | 6 | 0 | 0 |
The change in the value of glycosylated hemoglobin collected at Week 52 or at the final visit relative to Baseline. (NCT01456130)
Timeframe: Baseline and Week 52
| Intervention | percentage of glycosylated hemoglobin (Mean) |
|---|---|
| Alogliptin | -0.46 |
Clinical response is defined as an HbA1c level less than 5.8% or less than 6.5% at Week 52 or at the final visit. (NCT01456130)
Timeframe: Week 52
| Intervention | percentage of participants (Number) | |
|---|---|---|
| HbA1c of < 5.8% | HbA1c of < 6.5% | |
| Alogliptin | 4.5 | 28.4 |
The concentration of glucagon-like peptide-1 (GLP-1) in blood before and up to 8 hours after eating (postprandial) was plotted and the area under the curve calculated using the linear trapezoidal rule at Baseline and on Day 11. Least squares means of the change from Baseline to Day 11 were obtained using an analysis of covariance (ANCOVA) model with treatment as fixed effect, and Baseline postprandial AUC (0-8) of active GLP-1 as a continuous covariate. (NCT01664624)
Timeframe: Baseline and Day 11; samples were taken at -15 min and -5 min (pre-meal), and 15 min, 30 min, and 1, 2, 3, 4, 6, and 8 hours (post-meal).
| Intervention | pmol/L*hr (Least Squares Mean) |
|---|---|
| Roflumilast + Alogliptin | 26.5 |
| Alogliptin Alone | 31.6 |
| Roflumilast Alone | 3.8 |
| Exenatide | -2.3 |
"Appetite sensations were measured using a visual analog scale (VAS) questionnaire. Participants were asked to indicate their level of fullness, hunger, satiety, and prospective consumption (how much do you think you can eat?) on a 100 mm line ranging from Not at all (0 mm) to extremely (100 mm). Appetite sensation scores before and up to 8 hours after eating were plotted and the area under the curve calculated using the linear trapezoidal rule at Baseline and on Day 11. Least squares means of the change from Baseline to Day 11 were obtained using an ANCOVA model with treatment as fixed effect, and Baseline postprandial AUC (0-8) of appetite sensation VAS score as a continuous covariate." (NCT01664624)
Timeframe: At Baseline and Day 11, every 30 minutes, starting 1 hour before eating until 8 hour after the meal.
| Intervention | mm*hr (Least Squares Mean) | |||
|---|---|---|---|---|
| Fullness | Hunger | Prospective consumption | Satiety | |
| Alogliptin Alone | 62.0 | 3.1 | -14.9 | -3.2 |
| Exenatide | 116.8 | -122.5 | -124.3 | -127.7 |
| Roflumilast + Alogliptin | 70.5 | -103.6 | -97.1 | -82.7 |
| Roflumilast Alone | 136.0 | -132.7 | -169.5 | -139.2 |
Plasma glucose was measured by Continuous Glucose Monitoring System (CGMS). CGMS measures glucose every 5 minutes, starting in the fasting state 8 hour prior to the standardized breakfast (12 AM) until 16 hours after the breakfast. The average 24-hour plasma glucose concentration was calculated. Least squares means were obtained using an ANCOVA model with treatment as fixed effect, and Baseline 24-hour Glucose Measured by CGMS as a continuous covariate. (NCT01664624)
Timeframe: Baseline (Day -1) and Day 11, from 12 AM through 24 hours.
| Intervention | mg/dL (Least Squares Mean) |
|---|---|
| Roflumilast + Alogliptin | -25.4 |
| Alogliptin Alone | -17.5 |
| Roflumilast Alone | -14.5 |
| Exenatide | -34.9 |
The concentration of insulin in blood before and up to 8 hours after eating was plotted and the area under the curve calculated using the linear trapezoidal rule at Baseline and on Day 11. Least squares means of the change from Baseline to Day 11 were obtained using an ANCOVA model with treatment as fixed effect, and Baseline postprandial AUC (0-8) of insulin as a continuous covariate. (NCT01664624)
Timeframe: Baseline and Day 11; samples were taken at -15 min and -5 min (pre-meal), and 15 min, 30 min, and 1, 2, 3, 4, 6, and 8 hours (post-meal).
| Intervention | pmol/L*hr (Least Squares Mean) |
|---|---|
| Roflumilast + Alogliptin | -49.5 |
| Alogliptin Alone | 107.8 |
| Roflumilast Alone | 26.9 |
| Exenatide | -136.4 |
The concentration of C-peptide in blood before and up to 8 hours after eating (postprandial) was plotted and the area under the curve calculated using the linear trapezoidal rule at Baseline and on Day 11. Least squares means of the change from Baseline to Day 11 were obtained using an ANCOVA model with treatment as fixed effect, and Baseline postprandial AUC (0-8) of C-peptide as a continuous covariate. (NCT01664624)
Timeframe: Baseline and Day 11; samples were taken at -15 min and -5 min (pre-meal), and 15 min, 30 min, and 1, 2, 3, 4, 6, and 8 hours (post-meal).
| Intervention | ng/mL*hr (Least Squares Mean) |
|---|---|
| Roflumilast + Alogliptin | 1.0 |
| Alogliptin Alone | 1.4 |
| Roflumilast Alone | -0.7 |
| Exenatide | 0.0 |
The concentration of glucose in blood before and up to 8 hours after eating (postprandial) was plotted and the area under the curve calculated using the linear trapezoidal rule at Baseline and on Day 11. Least squares means of the change from Baseline to Day 11 were obtained using an ANCOVA model with treatment as fixed effect, and baseline postprandial AUC (0-8) of plasma glucose as a continuous covariate. (NCT01664624)
Timeframe: Baseline and Day 11 at -15 min and -5 min (pre-meal), and 15 min, 30 min, and 1, 2, 3, 4, 6, and 8 hours (post-meal).
| Intervention | mmol/L*hr (Least Squares Mean) |
|---|---|
| Roflumilast + Alogliptin | -13.4 |
| Alogliptin Alone | -9.8 |
| Roflumilast Alone | -9.0 |
| Exenatide | -18.5 |
Clinical response at Week 26 will be assessed by the percentage of participants with HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) ≤6.5%. (NCT01890122)
Timeframe: Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Metformin HCl 500 mg | 27.3 |
| Alogliptin 12.5 mg | 21.6 |
| Alogliptin 12.5 mg + Metformin HCl 500 mg FDC | 55.1 |
| Placebo | 11.8 |
Clinical response at Week 26 will be assessed by the percentage of participants with a decrease from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) of ≥2.0%. (NCT01890122)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Metformin HCl 500 mg | 17.4 |
| Alogliptin 12.5 mg | 17.3 |
| Alogliptin 12.5 mg + Metformin HCl 500 mg FDC | 34.8 |
| Placebo | 6.2 |
Clinical response at Week 26 will be assessed by the percentage of participants with a decrease from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) of ≥1.5%. (NCT01890122)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Metformin HCl 500 mg | 37.3 |
| Alogliptin 12.5 mg | 36.4 |
| Alogliptin 12.5 mg + Metformin HCl 500 mg FDC | 62.0 |
| Placebo | 14.9 |
Clinical response at Week 26 will be assessed by the percentage of participants with a decrease from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) of ≥0.5%. (NCT01890122)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Metformin HCl 500 mg | 81.4 |
| Alogliptin 12.5 mg | 74.1 |
| Alogliptin 12.5 mg + Metformin HCl 500 mg FDC | 89.2 |
| Placebo | 42.9 |
Rescue is defined as meeting one of the following criteria, confirmed by a second sample drawn within 7 days of first sample: After >1 week of treatment but prior to Week 4 visit: A single FPG ≥275 mg/dL (≥15.27 mmol/L); From the Week 4 but prior to the Week 8 visit: A single FPG ≥250 mg/dL (≥13.88 mmol/L); From the Week 8 visit but prior to the Week 12 visit: A single FPG ≥225 mg/dL (≥12.49 mmol/L); From the Week 12 visit through the end-of-treatment visit (week 26): HbA1c ≥8.5% and ≤0.5% reduction in HbA1c from baseline. (NCT01890122)
Timeframe: Baseline up to Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Metformin HCl 500 mg | 8.7 |
| Alogliptin 12.5 mg | 14.8 |
| Alogliptin 12.5 mg + Metformin HCl 500 mg FDC | 4.4 |
| Placebo | 25.5 |
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 26 or early termination relative to baseline. Negative change indicates better glycemic control. (NCT01890122)
Timeframe: Baseline and Week 26 (or Early termination)
| Intervention | percentage of glycosylated hemoglobin (Mean) |
|---|---|
| Metformin HCl 500 mg | -0.32 |
| Alogliptin 12.5 mg | -1.23 |
| Alogliptin 12.5 mg + Metformin HCl 500 mg FDC | -1.06 |
| Placebo | -1.72 |
Clinical response at Week 26 will be assessed by the percentage of participants with a decrease from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) of ≥1.0%. (NCT01890122)
Timeframe: Baseline and Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Metformin HCl 500 mg | 63.4 |
| Alogliptin 12.5 mg | 53.7 |
| Alogliptin 12.5 mg + Metformin HCl 500 mg FDC | 83.5 |
| Placebo | 25.5 |
Clinical response at Week 26 will be assessed by the percentage of participants with HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) ≤7%. (NCT01890122)
Timeframe: Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Metformin HCl 500 mg | 55.9 |
| Alogliptin 12.5 mg | 44.4 |
| Alogliptin 12.5 mg + Metformin HCl 500 mg FDC | 77.2 |
| Placebo | 30.4 |
Clinical response at Week 26 will be assessed by the percentage of participants with HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) ≤7.5%. (NCT01890122)
Timeframe: Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Metformin HCl 500 mg | 73.3 |
| Alogliptin 12.5 mg | 60.5 |
| Alogliptin 12.5 mg + Metformin HCl 500 mg FDC | 84.8 |
| Placebo | 46.0 |
Marked hyperglycemia is defined as FPG level ≥200 mg/dL (11.1 mmol/L). (NCT01890122)
Timeframe: Baseline up to Week 26
| Intervention | percentage of participants (Number) |
|---|---|
| Metformin HCl 500 mg | 8.8 |
| Alogliptin 12.5 mg | 12.7 |
| Alogliptin 12.5 mg + Metformin HCl 500 mg FDC | 5.7 |
| Placebo | 15.9 |
Rescue is defined as meeting one of the following criteria, confirmed by a second sample drawn within 7 days of first sample: After >1 week of treatment but prior to Week 4 visit: A single FPG ≥275 mg/dL (≥15.27 mmol/L); From the Week 4 but prior to the Week 8 visit: A single FPG ≥250 mg/dL (≥13.88 mmol/L); From the Week 8 visit but prior to the Week 12 visit: A single FPG ≥225 mg/dL (≥12.49 mmol/L); From the Week 12 visit through the end-of-treatment visit (week 26): HbA1c ≥8.5% and ≤0.5% reduction in HbA1c from baseline. Time to hyperglycemic rescue was censored if the participant did not experience a hyperglycemic rescue event. (NCT01890122)
Timeframe: From the date of randomization through Week 26
| Intervention | days (Median) |
|---|---|
| Metformin HCl 500 mg | NA |
| Alogliptin 12.5 mg | NA |
| Alogliptin 12.5 mg + Metformin HCl 500 mg FDC | NA |
| Placebo | NA |
Change in participant's body weight at Weeks 12 and 26 relative to baseline. (NCT01890122)
Timeframe: Baseline and Weeks 12 and 26
| Intervention | kg (Median) | |
|---|---|---|
| Week 12 (n=153,151,149,145) | Week 26 (n=156,156,156,152) | |
| Alogliptin 12.5 mg | -0.19 | -0.22 |
| Alogliptin 12.5 mg + Metformin HCl 500 mg FDC | -0.14 | -0.57 |
| Metformin HCl 500 mg | -0.71 | -0.93 |
| Placebo | -0.32 | -0.33 |
The change between the FPG value collected at Weeks 4, 8, 12, 16, 20 and 26 relative to baseline. Negative change indicates better glycemic control. (NCT01890122)
Timeframe: Baseline and Weeks 4, 8, 12, 16, 20 and 26
| Intervention | mg/dL (Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 (n=157,154,155,156) | Week 8 (n=160,158,158,157) | Week 12 (n=160,158,158,157) | Week 16 (n=160,158,158,157) | Week 20 (n=160,158,158,157) | Week 26 (n=160,158,158,157) | |
| Alogliptin 12.5 mg | -1.01 | -1.17 | -1.33 | -1.25 | -1.19 | -1.06 |
| Alogliptin 12.5 mg + Metformin HCl 500 mg FDC | -2.01 | -2.13 | -2.14 | -2.17 | -2.26 | -2.06 |
| Metformin HCl 500 mg | -1.42 | -1.50 | -1.48 | -1.62 | -1.57 | -1.45 |
| Placebo | 0.02 | -0.08 | -0.08 | -0.07 | -0.12 | -0.04 |
The change in the value of HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) collected at Weeks 4, 8, 12, 16 and 20 relative to baseline. Negative change indicates better glycemic control. (NCT01890122)
Timeframe: Baseline and Weeks 4, 8, 12, 16 and 20
| Intervention | percentage of glycosylated hemoglobin (Mean) | ||||
|---|---|---|---|---|---|
| Week 4 (n=157,156,154,156) | Week 8 (n=160,160,158,157) | Week 12 (n=160,160,158,157) | Week 16 (n=160,160,158,157) | Week 20 (n=160.160,158,157) | |
| Alogliptin 12.5 mg | -0.41 | -0.78 | -1.01 | -1.06 | -1.11 |
| Alogliptin 12.5 mg + Metformin HCl 500 mg FDC | -0.80 | -1.29 | -1.57 | -1.71 | -1.74 |
| Metformin HCl 500 mg | -0.57 | -0.90 | -1.06 | -1.18 | -1.24 |
| Placebo | -0.18 | -0.29 | -0.27 | -0.33 | -0.33 |
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 month 36 relative to baseline. (NCT01945216)
Timeframe: Baseline, Months 1, 3, 6, 12, 18, 24, 30, 36 and final assessment (up to Month 36)
| Intervention | Percent (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Change at Month 1 | Change at Month 3 | Change at Month 6 | Change at Month 12 | Change at Month 18 | Change at Month 24 | Change at Month 30 | Change at Month 36 | Change at Final Assessment | |
| Alogliptin | -0.45 | -0.79 | -0.84 | -0.83 | -0.81 | -0.82 | -0.83 | -0.84 | -0.81 |
| Alogliptin + α-GI | -0.33 | -0.54 | -0.70 | -0.75 | -0.62 | -0.66 | -0.73 | -0.72 | -0.63 |
The change in the value of fasting blood glucose collected at month 36 relative to baseline. (NCT01945216)
Timeframe: Baseline, Months 1, 3, 6, 12, 18, 24, 30, 36 and final assessment (up to Month 36)
| Intervention | mg/dL (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Change at Month 1 | Change at Month 3 | Change at Month 6 | Change at Month 12 | Change at Month 18 | Change at Month 24 | Change at Month 30 | Change at Month 36 | Change at Final Assessment | |
| Alogliptin | -22.9 | -21.7 | -19.1 | -23.1 | -21.1 | -19.9 | -24.4 | -23.0 | -24.5 |
| Alogliptin + α-GI | -4.9 | -8.3 | -14.5 | -18.4 | -16.0 | -14.0 | -11.7 | -18.6 | -12.2 |
(NCT01945216)
Timeframe: Up to Month 36
| Intervention | Participants (Count of Participants) |
|---|---|
| Alogliptin | 151 |
| Alogliptin + α-GI | 98 |
| Alogliptin + Other | 139 |
The change between the fasting blood glucose value collected at 1 month, 3 months, 6 months, 12 months or final visit (last visit for a participant in the study, up to Month 12) relative to baseline. The efficacy analysis was planned to be assessed in the total alogliptin arm irrespective of the thiazolidinedione treatment. (NCT01945242)
Timeframe: Baseline, Months 1, 3, 6, 12, and final assessment (up to 12 months)
| Intervention | milligram per deciliter (mg/dL) (Mean) | |||||
|---|---|---|---|---|---|---|
| Baseline (n=389) | Change at Month 1 (n=283) | Change at Month 3 (n=301) | Change at Month 6 (n=297) | Change at Month 12 (n=293) | Change at Final assessment (n=398) | |
| Alogliptin | 145.4 | -9.8 | -11.8 | -13.9 | -16.2 | -13.5 |
The change between the fasting insulin value collected at 1 month, 3 months, 6 months, 12 months or final visit (last visit for a participant in the study, up to Month 12) relative to baseline. The efficacy analysis was planned to be assessed in the total alogliptin arm irrespective of the thiazolidinedione treatment. (NCT01945242)
Timeframe: Baseline, Months 1, 3, 6, 12, and final assessment (up to 12 months)
| Intervention | mg/dL (Mean) | |||||
|---|---|---|---|---|---|---|
| Baseline (n=82) | Change at Month 1 (n=54) | Change at Month 3 (n=57) | Change at Month 6 (n=60) | Change at Month 12 (n=68) | Change at Final assessment (n=82) | |
| Alogliptin | 6.32 | 0.19 | -0.02 | 0.29 | -0.32 | -0.25 |
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 1 month, 3 months, 6 months, 12 months or final visit (last visit for a participant in the study, up to Month 12) relative to baseline. The efficacy analysis was planned to be assessed in the total alogliptin arm irrespective of the thiazolidinedione treatment. (NCT01945242)
Timeframe: Baseline, Months 1, 3, 6, 12, and final assessment (up to 12 months)
| Intervention | percentage of glycosylated hemoglobin (Mean) | |||||
|---|---|---|---|---|---|---|
| Baseline (n=1124) | Change at Month 1 (n=879) | Change at Month 3 (n=1005) | Change at Month 6 (n=988) | Change at Month 12 (n=949) | Change at Final assessment (n=1124) | |
| Alogliptin | 7.67 | -0.25 | -0.47 | -0.53 | -0.64 | -0.57 |
Serious adverse drug reactions are defined as serious adverse events (SAEs) which are in the investigator's opinion of causal relationship to the study treatment. 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. The safety analysis was planned to be assessed in alogliptin + thiazolidinedione and alogliptin + other arm separately. (NCT01945242)
Timeframe: Baseline up to 12 months
| Intervention | participants (Number) | |
|---|---|---|
| Hyperglycaemia | Hypoglycaemia | |
| Alogliptin + Other | 0 | 0 |
| Alogliptin + Thiazolidinedione | 1 | 2 |
The rate of achieving objective glycemic control in HbA1c level, was calculated at 1 month, 3 months, 6 months, 12 months or final visit (last visit for a participant in the study, up to Month 12). Glycemic control was measured as <8.0 percent, <7.0 percent, and <6.0 percent of glycosylated hemoglobin. The efficacy analysis was planned to be assessed in the total alogliptin arm irrespective of the thiazolidinedione treatment. (NCT01945242)
Timeframe: Baseline, Months 1, 3, 6, 12, and final assessment (up to 12 months)
| Intervention | percentage of participants (Number) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| <8.0 percent (Baseline) (n=1124) | <8.0 percent (Month 1) (n=879) | <8.0 percent (Month 3) (n=1005) | <8.0 percent (Month 6) (n=988) | <8.0 percent (Month 12) (n=949) | <8.0 percent (Final assessment) (n=1124) | <7.0 percent (Baseline) (n=1124) | <7.0 percent (Month 1) (n=879) | <7.0 percent (Month 3) (n=1005) | <7.0 percent (Month 6) (n=988) | <7.0 percent (Month 12) (n=949) | <7.0 percent (Final assessment) (n=1124) | <6.0 percent (Baseline) (n=1124) | <6.0 percent (Month 1) (n=879) | <6.0 percent (Month 3) (n=1005) | <6.0 percent (Month 6) (n=988) | <6.0 percent (Month 12) (n=949) | <6.0 percent (Final assessment) (n=1124) | |
| Alogliptin | 68.0 | 75.8 | 84.2 | 84.5 | 87.1 | 83.6 | 27.6 | 34.3 | 47.1 | 51.2 | 57.5 | 54.2 | 2.7 | 3.2 | 5.6 | 6.8 | 8.2 | 8.0 |
Adverse drug reactions are defined as adverse events (AEs) which are in the investigator's opinion of causal relationship to the study treatment. AEs are defined as any unfavorable and unintended signs, symptoms or diseases temporally associated with the use of a medicinal product reported from the first dose of study drug to the last dose of study drug. The safety analysis was planned to be assessed in alogliptin + thiazolidinedione and alogliptin + other arm separately. (NCT01945242)
Timeframe: Baseline up to 12 months
| Intervention | participants (Number) | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Hypothyroidism | Hyperglycaemia | Hypoglycaemia | Dyslipidaemia | Dizziness | Photopsia | Hypertension | Abdominal distension | Diarrhoea | Eczema | Pruritus | Arthralgia | Joint swelling | Local swelling | Pyrexia | Blood insulin decreased | Blood insulin increased | Hand fracture | Rib fracture | |
| Alogliptin + Other | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Alogliptin + Thiazolidinedione | 1 | 1 | 5 | 1 | 3 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 |
(NCT01964963)
Timeframe: Up to Month 36
| Intervention | Percentage of Participants (Number) |
|---|---|
| Alogliptin 25 mg | 10.54 |
The change in the value of fasting blood glucose level collected at final assessment point (up to Month 36) relative to baseline. (NCT01964963)
Timeframe: Baseline, and final assessment point (up to Month 36)
| Intervention | Milligram (mg)/ deciliter (dL) (Mean) |
|---|---|
| Alogliptin 25 mg | -5.8 |
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 final assessment point (up to Month 36) relative to baseline. (NCT01964963)
Timeframe: Baseline, and final assessment point (up to Month 36)
| Intervention | Percent HbA1c (Mean) |
|---|---|
| Alogliptin 25 mg | -0.14 |
(NCT01990300)
Timeframe: Up to 12 Months
| Intervention | Participants (Count of Participants) |
|---|---|
| Alogliptin/Pioglitazone | 206 |
Reported data are changes in HbA1c from baseline at Month 1, 3, 6, 12 and final assessment (up to 12 months). (NCT01990300)
Timeframe: Baseline and Month 1, 3, 6, 12 and final assessment (up to 12 Months)
| Intervention | Percent HbA1c (Mean) | ||||
|---|---|---|---|---|---|
| Change in HbA1c at Month 1 | Change in HbA1c at Month 3 | Change in HbA1c at Month 6 | Change in HbA1c at Month 12 | Change in HbA1c at Final Assessment | |
| Alogliptin/Pioglitazone | -0.26 | -0.58 | -0.66 | -0.66 | -0.65 |
Reported data are changes in fasting blood glucose level from baseline at Month 1, 3, 6, 12 and final assessment (up to 12 months). (NCT01990300)
Timeframe: Baseline and Month 1, 3, 6, 12 and final assessment (up to 12 Months)
| Intervention | mg/dL (Mean) | ||||
|---|---|---|---|---|---|
| Change in FBG at Month 1 | Change in FBG at Month 3 | Change in FBG at Month 6 | Change in FBG at Month 12 | Change in FBG at Final Assessment | |
| Alogliptin/Pioglitazone | -14.7 | -18.7 | -18.4 | -19.6 | -19.8 |
The change in the value of HbA1c (NGSP) (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) collected at End of Treatment Period relative to Baseline. A negative change from Baseline indicates improvement. An Analysis of Covariate (ANCOVA) model with change from Baseline as a dependent variable and Baseline and treatment as independent variables was used for main analyses. (NCT02068443)
Timeframe: Baseline and End of Treatment (EOT) (Up to Week 24)
| Intervention | percent (Least Squares Mean) |
|---|---|
| Alogliptin Alone | 0.16 |
| Alogliptin + Metformin Hydrochloride QD | -0.49 |
| Alogliptin + Metformin Hydrochloride BID | -0.60 |
An Adverse Event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (example, a clinically significant abnormal laboratory finding), symptom, or disease temporally associated with the use of a drug, whether or not it is considered related to the drug. A treatment-emergent adverse event (TEAE) is defined as an adverse event with an onset that occurs after receiving study drug. (NCT02068443)
Timeframe: 24 Weeks
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin Alone | 57.7 |
| Alogliptin + Metformin Hydrochloride QD | 50.7 |
| Alogliptin + Metformin Hydrochloride BID | 52.3 |
The change in the value of the fasting plasma glucose collected at Weeks 2, 4, 8, 12, 16, 20 and 24 relative to Baseline. A negative change from Baseline indicates improvement. (NCT02068443)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16, 20, 24 and EOT (Up to Week 24)
| Intervention | mg/dL (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 2 (n=71, 152, 151) | Week 4 (n=70, 150, 150) | Week 8 (n=68, 149, 149) | Week 12 (n=67, 148, 148) | Week 16 (n=66, 148, 148) | Week 20 (n=65, 146, 148) | Week 24 (n=64, 146, 148) | EOT (n=71, 152, 151) | |
| Alogliptin + Metformin Hydrochloride BID | -23.7 | -25.2 | -23.4 | -22.9 | -22.6 | -17.6 | -18.2 | -18.2 |
| Alogliptin + Metformin Hydrochloride QD | -16.6 | -16.4 | -18.4 | -15.2 | -13.0 | -11.3 | -7.2 | -7.6 |
| Alogliptin Alone | 0.4 | -0.9 | -2.1 | 1.5 | 0.4 | 6.6 | 8.0 | 7.4 |
The change in the value of HbA1c (NGSP) (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) collected at Weeks 2, 4, 8, 12, 16, 20, 24, and EOT relative to Baseline. A negative change from Baseline indicates improvement. (NCT02068443)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16, 20, 24 and EOT (Up to Week 24)
| Intervention | percent (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 2 (n=71, 152, 151) | Week 4 (n=70, 150, 150) | Week 8 (n=68, 149, 149) | Week 12 (n=67, 148, 148) | Week 16 (n=66, 148, 147) | Week 20 (n=65, 146, 148) | Week 24 (n=64, 146, 148) | EOT (n=71, 152, 151) | |
| Alogliptin + Metformin Hydrochloride BID | -0.19 | -0.35 | -0.60 | -0.75 | -0.81 | -0.71 | -0.62 | -0.62 |
| Alogliptin + Metformin Hydrochloride QD | -0.14 | -0.28 | -0.50 | -0.61 | -0.64 | -0.58 | -0.49 | -0.49 |
| Alogliptin Alone | 0.01 | 0.01 | -0.01 | -0.02 | 0.01 | 0.11 | 0.17 | 0.17 |
The value of the fasting plasma glucose collected at Baseline and Weeks 2, 4, 8, 12, 16, 20, 24 and EOT. (NCT02068443)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16, 20, 24 and EOT (Up to Week 24)
| Intervention | mg/dL (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Baseline (n=71, 152, 151) | Week 2 (n=71, 152, 151) | Week 4 (n=70, 150, 150) | Week 8 (n=68, 149, 149) | Week 12 (n=67, 148, 148) | Week 16 (n=66, 148, 148) | Week 20 (n=65, 146, 148) | Week 24 (n=64, 146, 148) | EOT (n=71, 152, 151) | |
| Alogliptin + Metformin Hydrochloride BID | 165.9 | 142.3 | 140.7 | 142.0 | 142.5 | 142.9 | 147.8 | 147.3 | 147.7 |
| Alogliptin + Metformin Hydrochloride QD | 164.7 | 148.1 | 148.7 | 146.5 | 149.2 | 151.4 | 153.2 | 157.4 | 157.1 |
| Alogliptin Alone | 162.4 | 162.8 | 161.4 | 158.9 | 161.1 | 158.5 | 164.6 | 165.9 | 169.8 |
"Number of participants who had ECG findings changed from normal or abnormal but not clinically relevant at Baseline to abnormal and clinically relevant." (NCT02068443)
Timeframe: Baseline and Weeks 12 and 24
| Intervention | participants (Number) | |
|---|---|---|
| Week 12 | Week 24 | |
| Alogliptin + Metformin Hydrochloride BID | 0 | 2 |
| Alogliptin + Metformin Hydrochloride QD | 0 | 0 |
| Alogliptin Alone | 0 | 0 |
HbA1c (NGSP) is the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound. The percentage of participants with HbA1c levels of ≥6.0, ≥7.0 and ≥8.0 at the end of Screening (Baseline) with change to target values <6.0, <7.0 and <8.0 respectively at EOT. (NCT02068443)
Timeframe: Baseline and EOT (Up to Week 24)
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| ≥6.0 at Baseline to <6.0 at EOT (n=71, 152, 151) | ≥7.0 at Baseline to <7.0 at EOT ( n=63, 137, 140) | ≥8.0 at Baseline to <8.0 at EOT (n=26, 59, 64) | |
| Alogliptin + Metformin Hydrochloride BID | 1.3 | 34.3 | 60.9 |
| Alogliptin + Metformin Hydrochloride QD | 0.7 | 35.0 | 47.5 |
| Alogliptin Alone | 0.0 | 4.8 | 23.1 |
The percentage of participants with any clinically relevant safety laboratory changes (chemistry, hematology and urinalysis) collected throughout study and recorded as AEs. (NCT02068443)
Timeframe: 24 Weeks
| Intervention | percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Blood Creatine Phosphokinase increased | Blood Lactic Acid increased | Amylase increased | Lipase increased | Blood Albumin decreased | Gamma-glutamyltransferase increased | |
| Alogliptin + Metformin Hydrochloride BID | 0.7 | 0 | 2.0 | 2.0 | 0.7 | 0.7 |
| Alogliptin + Metformin Hydrochloride QD | 2.0 | 1.3 | 0 | 0 | 0 | 0 |
| Alogliptin Alone | 0 | 0 | 0 | 0 | 0 | 0 |
Vital signs included sitting systolic and diastolic blood pressures (mmHg) (measured after resting for ≥ 5 minutes) and pulse rate (beats per minute [bpm]). (NCT02068443)
Timeframe: 24 Weeks
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Hypertension | Blood Pressure increased | |
| Alogliptin + Metformin Hydrochloride BID | 0 | 0.7 |
| Alogliptin + Metformin Hydrochloride QD | 0 | 0 |
| Alogliptin Alone | 1.4 | 0 |
The value of HbA1c (NGSP) (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) collected at Baseline and Weeks 2, 4, 8, 12, 16, 20, 24, and EOT. (NCT02068443)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16, 20, 24 and EOT (Up to Week 24)
| Intervention | percent (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Baseline (n=71, 152, 151) | Week 2 (n=71, 152, 151) | Week 4 (n=70, 150, 150) | Week 8 (n=68, 149, 149) | Week 12 (n=67, 148, 148) | Week 16 (n=66, 148, 147) | Week 20 (n=65, 146, 148) | Week 24 (n=64, 146, 148) | EOT (n=71, 152, 151) | |
| Alogliptin + Metformin Hydrochloride BID | 7.89 | 7.70 | 7.54 | 7.28 | 7.13 | 7.08 | 7.18 | 7.27 | 7.28 |
| Alogliptin + Metformin Hydrochloride QD | 7.82 | 7.67 | 7.55 | 7.32 | 7.19 | 7.16 | 7.23 | 7.32 | 7.33 |
| Alogliptin Alone | 7.77 | 7.78 | 7.78 | 7.72 | 7.70 | 7.70 | 7.81 | 7.86 | 7.95 |
The reported data were change from baseline in fasting insulin level. (NCT02221284)
Timeframe: Baseline, and final assessment point (up to Month 12)
| Intervention | Micro Units per Milliliter (μU/mL) (Mean) |
|---|---|
| Alogliptin + Insulin | -3.08 |
| Alogliptin + Glinide | 2.26 |
| Alogliptin + SGLT-2 Inhibitor | 0.40 |
The reported data were change from baseline in fasting blood glucose level. (NCT02221284)
Timeframe: Baseline, and final assessment point (up to Month 12)
| Intervention | Milligram (mg)/deciliter (dL) (Mean) |
|---|---|
| Alogliptin + Insulin | -16.4 |
| Alogliptin + Glinide | -32.0 |
| Alogliptin + SGLT-2 Inhibitor | -18.7 |
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 final assessment point (up to Month 12) relative to baseline. (NCT02221284)
Timeframe: Baseline, and final assessment point (up to Month 12)
| Intervention | Percent (Mean) |
|---|---|
| Alogliptin + Insulin | -0.66 |
| Alogliptin + Glinide | -0.49 |
| Alogliptin + SGLT-2 Inhibitor | -0.60 |
The reported data were number of participants who achieved specified HbA1c Level (< 7.0% and <6.0%) during this study. (NCT02221284)
Timeframe: Baseline, and final assessment point (up to Month 12)
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| HbA1c Level < 7.0% | HbA1c Level < 6.0% | |
| Alogliptin + Glinide | 87 | 10 |
| Alogliptin + Insulin | 161 | 22 |
| Alogliptin + SGLT-2 Inhibitor | 55 | 7 |
Adverse drug reactions are defined as adverse events (AEs) which are in the investigator's opinion of causal relationship to the study treatment. AEs are defined as any unfavorable and unintended signs, symptoms or diseases temporally associated with the use of a medicinal product reported from the first dose of study drug to the last dose of study drug. (NCT02221284)
Timeframe: Up to Month 12
| Intervention | Percentage of Participants (Number) |
|---|---|
| Alogliptin + Insulin | 5.41 |
| Alogliptin + Glinide | 1.20 |
| Alogliptin + SGLT-2 Inhibitor | 0.98 |
| Alogliptin + Other | 0.00 |
The reported data were change from baseline in HOMA-R. HOMA-R measures insulin resistance, calculated by fasting insulin (μU/mL) multiplied by fasting glucose (mg/dL), and divided by a constant (405). A higher score indicates higher insulin resistance. (NCT02221284)
Timeframe: Baseline, and final assessment point (up to Month 12)
| Intervention | HOMA-R Score (Mean) |
|---|---|
| Alogliptin + Insulin | -2.58 |
| Alogliptin + Glinide | -0.25 |
| Alogliptin + SGLT-2 Inhibitor | 0.00 |
The reported data were change from baseline in HOMA-β. HOMA-β measures as following; HOMA-β = fasting insulin (μU/mL) ×360/{fasting glucose (mg/dL) - 63}. (NCT02221284)
Timeframe: Baseline, and final assessment point (up to Month 12)
| Intervention | Percentage of beta cell function (Mean) |
|---|---|
| Alogliptin + Insulin | 12.32 |
| Alogliptin + Glinide | 33.38 |
| Alogliptin + SGLT-2 Inhibitor | 15.40 |
Mean residence time (MRT) calculated as area under the first moment plasma concentration-time curve (AUMC [0-inf]) divided by AUC (0-inf). (AUMC [0-inf]) is the area under the first moment plasma concentration-time curve from time 0 to infinity. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | hr (Mean) |
|---|---|
| SYR-322-MET Fasted | 18.06 |
| SYR-322-MET Fed | 17.72 |
MRT (0-tlqc) is a measure of the mean residence time from time 0 to time of the last quantifiable concentration (tlqc) calculated as MRT (0-tlqc) =AUMC (0-tlqc)/AUC (0-tlqc). AUMC (0-tlqc) is the area under the first moment plasma concentration-time curve from time 0 to time of the last quantifiable concentration (tlqc), calculated using the linear trapezoidal rule. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, and 48 hours postdose
| Intervention | hr (Mean) |
|---|---|
| SYR-322-MET Fasted | 5.697 |
| SYR-322-MET Fed | 5.697 |
MRT (0-tlqc) is a measure of the mean residence time from time 0 to time of the last quantifiable concentration (tlqc) calculated as MRT (0-tlqc) =AUMC (0-tlqc)/AUC (0-tlqc). AUMC (0-tlqc) is the area under the first moment plasma concentration-time curve from time 0 to time of the last quantifiable concentration (tlqc), calculated using the linear trapezoidal rule. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | hr (Mean) |
|---|---|
| SYR-322-MET Fasted | 14.84 |
| SYR-322-MET Fed | 14.17 |
An Adverse Event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (eg, a clinically significant abnormal laboratory finding), symptom, or disease temporally associated with the use of a drug, whether or not it is considered related to the drug. A treatment-emergent adverse event (TEAE) is defined as an adverse event with an onset that occurs after receiving study drug. (NCT02276274)
Timeframe: Baseline up to the day of discharge (Day 4) in the second intervention period
| Intervention | participants (Number) |
|---|---|
| SYR-322-MET Fasted | 0 |
| SYR-322-MET Fed | 0 |
Clinically significant change participant's body weight observed at any time point are reported. (NCT02276274)
Timeframe: 3 hours prior to administration (predose), 24 and 72 hours postdose
| Intervention | participants (Number) |
|---|---|
| SYR-322-MET Fasted | 0 |
| SYR-322-MET Fed | 0 |
Vital signs included body temperature (infra-axillary), supine blood pressure resting more than 5 minutes (systolic and diastolic [Millimeters of mercury]), respiratory rate and pulse (beats per minute). Clinically significant change in vital signs observed at any time point are reported. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 2, 24 and 72 hours postdose
| Intervention | participants (Number) |
|---|---|
| SYR-322-MET Fasted | 0 |
| SYR-322-MET Fed | 0 |
Laboratory assessments included hematology, serum chemistry and urinalysis. Any laboratory-related TEAE reported at any time point were reported in this measure. (NCT02276274)
Timeframe: 3 hours prior to administration (predose), 24 and 72 hours postdose
| Intervention | participants (Number) |
|---|---|
| SYR-322-MET Fasted | 0 |
| SYR-322-MET Fed | 0 |
Clinically significant change in electrocardiograms observed at any time point are reported. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 2, 24 and 72 hours postdose
| Intervention | participants (Number) |
|---|---|
| SYR-322-MET Fasted | 0 |
| SYR-322-MET Fed | 0 |
Terminal phase elimination half-life (T1/2) is the time required for half of the drug to be eliminated from the plasma. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, and 48 hours postdose
| Intervention | hr (Mean) |
|---|---|
| SYR-322-MET Fasted | 5.290 |
| SYR-322-MET Fed | 4.338 |
Terminal phase elimination half-life (T1/2) is the time required for half of the drug to be eliminated from the plasma. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | hr (Mean) |
|---|---|
| SYR-322-MET Fasted | 17.94 |
| SYR-322-MET Fed | 19.24 |
Time to reach Emax for the first time was determined from the inhibition-time curve. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 24 hours postdose
| Intervention | hour (Median) |
|---|---|
| SYR-322-MET Fasted | 3.000 |
| SYR-322-MET Fed | 1.000 |
Tmax: Time to reach the maximum plasma concentration (Cmax), equal to time (hours) to Cmax. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, and 48 hours postdose
| Intervention | hr (Median) |
|---|---|
| SYR-322-MET Fasted | 3.000 |
| SYR-322-MET Fed | 3.000 |
Tmax: Time to reach the maximum plasma concentration (Cmax), equal to time (hours) to Cmax. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | hour (hr) (Median) |
|---|---|
| SYR-322-MET Fasted | 3.000 |
| SYR-322-MET Fed | 1.00 |
Cumulative urinary excretion ratio of metformin was calculated as the percentage of metformin dose. (NCT02276274)
Timeframe: 0 to 24 hours postdose
| Intervention | percentage of dose (Mean) |
|---|---|
| SYR-322-MET Fasted | 50.078 |
| SYR-322-MET Fed | 49.923 |
Cumulative urinary excretion ratio of metformin was calculated as the percentage of metformin dose. (NCT02276274)
Timeframe: 0 to 48 hours postdose
| Intervention | percentage of dose (Mean) |
|---|---|
| SYR-322-MET Fasted | 50.626 |
| SYR-322-MET Fed | 50.067 |
Cumulative urinary excretion ratio of metformin was calculated as the percentage of metformin dose. (NCT02276274)
Timeframe: 0 to 12 hours postdose
| Intervention | percentage of dose (Mean) |
|---|---|
| SYR-322-MET Fasted | 45.143 |
| SYR-322-MET Fed | 44.809 |
Cumulative urinary excretion ratio of unchanged SYR-322 was calculated as the percentage of SYR-322 dose. (NCT02276274)
Timeframe: 0 to 12 hours postdose
| Intervention | percentage of dose (Mean) |
|---|---|
| SYR-322-MET Fasted | 42.609 |
| SYR-322-MET Fed | 45.028 |
Cumulative urinary excretion ratio of unchanged SYR-322 was calculated as the percentage of SYR-322 dose. (NCT02276274)
Timeframe: 0 to 48 hours postdose
| Intervention | percentage of dose (Mean) |
|---|---|
| SYR-322-MET Fasted | 70.200 |
| SYR-322-MET Fed | 71.148 |
Cumulative urinary excretion ratio of unchanged SYR-322 was calculated as the percentage of SYR-322 dose. (NCT02276274)
Timeframe: 0 to 72 hours postdose
| Intervention | percentage of dose (Mean) |
|---|---|
| SYR-322-MET Fasted | 73.728 |
| SYR-322-MET Fed | 74.547 |
Terminal elimination rate constant, calculated as the negative of the slope of the log-linear regression of the natural logarithm concentration-time curve during the terminal phase. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | hr^-1 (Mean) | |
|---|---|---|
| M-I (n = 9, 9) | M-II (n = 12, 12) | |
| SYR-322-MET Fasted | 0.02711 | 0.06458 |
| SYR-322-MET Fed | 0.02708 | 0.06651 |
AUC (0-72) is measure of area under the curve from time 0 to 72 hours post dose. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | ng*hr/mL (Mean) | |
|---|---|---|
| M-I | M-II | |
| SYR-322-MET Fasted | 9.49 | 39.18 |
| SYR-322-MET Fed | 8.28 | 37.00 |
AUC (0-inf) is a measure of total plasma exposure to the drug from time zero extrapolated to infinity. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | ng*hr/mL (Mean) | |
|---|---|---|
| M-I (n = 9, 9) | M-II (n = 12, 12) | |
| SYR-322-MET Fasted | 15.86 | 40.28 |
| SYR-322-MET Fed | 14.53 | 38.01 |
AUC (0-tlqc) is a measure of total plasma exposure to the drug from Time 0 to Time of the Last Quantifiable Concentration (AUC [0-tlqc]). (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | ng*hr/mL (Mean) | |
|---|---|---|
| M-I | M-II | |
| SYR-322-MET Fasted | 8.93 | 38.48 |
| SYR-322-MET Fed | 7.72 | 36.00 |
Maximum observed plasma concentration (Cmax) is the peak plasma concentration of a drug after administration, obtained directly from the plasma concentration-time curve. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | ng/mL (Mean) | |
|---|---|---|
| M-I | M-II | |
| SYR-322-MET Fasted | 0.42 | 4.18 |
| SYR-322-MET Fed | 0.40 | 3.58 |
DPP-4 activity was assessed from the plasma samples collected from the participants. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 24 hours postdose
| Intervention | nanomole/minute/milliliter (nmoL/min/mL) (Mean) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Predose | 0.25 hour | 0.5 hour | 1 Hour | 1.5 Hour | 2 hours | 3 hours | 4 hours | 6 hours | 8 hours | 24 hours | |
| SYR-322-MET Fasted | 7.8167 | 2.5833 | 1.1944 | 0.7122 | 0.6366 | 0.5003 | 0.3575 | 0.3977 | 0.5423 | 0.6422 | 1.4275 |
| SYR-322-MET Fed | 7.8492 | 3.4518 | 0.7823 | 0.3737 | 0.3312 | 0.3475 | 0.4128 | 0.4873 | 0.6196 | 0.7425 | 1.4550 |
DPP-4 activity and inhibition rate of DPP-4 activity was assessed from the plasma samples collected from the participants. Inhibition of DPP-4 enzyme was used to determine the antihyperglycemic activity of the investigational product. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 24 hours postdose
| Intervention | percentage of inhibition (Mean) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Predose | 0.25 hour | 0.5 hour | 1 hour | 1.5 hour | 2 hour | 3 hour | 4 hour | 6 hour | 8 hour | 24 hour | |
| SYR-322-MET Fasted | 0.00 | 68.00 | 85.65 | 91.05 | 91.85 | 93.63 | 95.52 | 94.88 | 93.04 | 91.78 | 81.74 |
| SYR-322-MET Fed | 0.00 | 57.99 | 90.31 | 95.27 | 95.79 | 95.58 | 94.71 | 93.78 | 92.06 | 90.51 | 81.38 |
Mean residence time (MRT) calculated as area under the first moment plasma concentration-time curve (AUMC [0-inf]) divided by AUC (0-inf). AUMC (0-inf) is the area under the first moment plasma concentration-time curve from time 0 to infinity. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | hr (Mean) | |
|---|---|---|
| M-I (n = 9, 9) | M-II (n = 12, 12) | |
| SYR-322-MET Fasted | 39.87 | 13.93 |
| SYR-322-MET Fed | 49.97 | 13.81 |
MRT (0-tlqc) is a measure of the mean residence time from time 0 to time of the last quantifiable concentration (tlqc) calculated as MRT (0-tlqc) =AUMC (0-tlqc)/AUC (0-tlqc). AUMC (0-tlqc) is the area under the first moment plasma concentration-time curve from time 0 to time of the last quantifiable concentration (tlqc), calculated using the linear trapezoidal rule. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | hr (Mean) | |
|---|---|---|
| M-I (n= 11, 11) | M-II (n=12, 12) | |
| SYR-322-MET Fasted | 17.95 | 10.88 |
| SYR-322-MET Fed | 17.75 | 10.45 |
Terminal phase elimination half-life (T1/2) is the time required for half of the drug to be eliminated from the plasma. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | hr (Mean) | |
|---|---|---|
| M-I (n = 9, 9) | M-II (n = 12, 12) | |
| SYR-322-MET Fasted | 26.09 | 12.43 |
| SYR-322-MET Fed | 31.39 | 11.70 |
Tmax: Time to reach the maximum plasma concentration (Cmax), equal to time (hours) to Cmax. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | hr (Median) | |
|---|---|---|
| M-I (n = 11, 11) | M-II (n = 12, 12) | |
| SYR-322-MET Fasted | 3.000 | 3.000 |
| SYR-322-MET Fed | 1.500 | 2.500 |
Cumulative urinary excretion ratio of SYR-322 metabolites M-I and M-II was calculated as the percentage of SYR-322 dose. (NCT02276274)
Timeframe: 0 to 12 hours postdose
| Intervention | percentage of dose (Mean) | |
|---|---|---|
| M-I | M-II | |
| SYR-322-MET Fasted | 0.235 | 1.202 |
| SYR-322-MET Fed | 0.234 | 1.145 |
Cumulative urinary excretion ratio of SYR-322 metabolites M-I and M-II was calculated as the percentage of SYR-322 dose. (NCT02276274)
Timeframe: 0 to 24 hours post dose
| Intervention | percentage of dose (Mean) | |
|---|---|---|
| M-I | M-II | |
| SYR-322-MET Fasted | 0.394 | 1.562 |
| SYR-322-MET Fed | 0.363 | 1.502 |
Cumulative urinary excretion ratio of SYR-322 metabolites M-I and M-II was calculated as the percentage of SYR-322 dose. (NCT02276274)
Timeframe: 0 to 48 hours postdose
| Intervention | percentage of dose (Mean) | |
|---|---|---|
| M-I | M-II | |
| SYR-322-MET Fasted | 0.535 | 1.788 |
| SYR-322-MET Fed | 0.495 | 1.732 |
Cumulative urinary excretion ratio of SYR-322 metabolites M-I and M-II was calculated as the percentage of SYR-322 dose. (NCT02276274)
Timeframe: 0 to 72 hours postdose
| Intervention | percentage of dose (Mean) | |
|---|---|---|
| M-I | M-II | |
| SYR-322-MET Fasted | 0.588 | 1.853 |
| SYR-322-MET Fed | 0.536 | 1.796 |
Cumulative urinary excretion ratio of unchanged SYR-322 was calculated as the percentage of SYR-322 dose. (NCT02276274)
Timeframe: 0 to 24 hours postdose
| Intervention | percentage of dose (Mean) |
|---|---|
| SYR-322-MET Fasted | 58.618 |
| SYR-322-MET Fed | 59.886 |
CL/F is apparent clearance of the drug from the plasma, calculated as the drug dose divided AUC (0-inf), expressed in L/hr. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, and 48 hours postdose
| Intervention | L/hr (Mean) |
|---|---|
| SYR-322-MET Fasted | 55.84 |
| SYR-322-MET Fed | 56.75 |
CL/F is apparent clearance of the drug from the plasma, calculated as the drug dose divided AUC (0-inf), expressed in liter/hour (L/hr). (NCT02276274)
Timeframe: 3 hours prior to administration, and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 hours after administration
| Intervention | L/hr (Mean) |
|---|---|
| SYR-322-MET Fasted | 16.24 |
| SYR-322-MET Fed | 16.52 |
Terminal elimination rate constant, calculated as the negative of the slope of the log-linear regression of the natural logarithm concentration-time curve during the terminal phase. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, and 48 hours postdose
| Intervention | hr^-1 (Mean) |
|---|---|
| SYR-322-MET Fasted | 0.1366 |
| SYR-322-MET Fed | 0.1638 |
Terminal elimination rate constant, calculated as the negative of the slope of the log-linear regression of the natural logarithm concentration-time curve during the terminal phase. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | hr^-1 (Mean) |
|---|---|
| SYR-322-MET Fasted | 0.03912 |
| SYR-322-MET Fed | 0.03673 |
Area under the inhibition rate of plasma DPP-4 activity-time curve from time 0 to 24 hours was determined from the inhibition-time curve. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 24 hours postdose
| Intervention | percentage of inhibition*hour (Mean) |
|---|---|
| SYR-322-MET Fasted | 2114.62 |
| SYR-322-MET Fed | 2100.74 |
AUC (0-48) is measure of area under the curve from time 0 to 48 hours post dose. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, and 48 hours postdose
| Intervention | ng*hr/mL (Mean) |
|---|---|
| SYR-322-MET Fasted | 9157.3 |
| SYR-322-MET Fed | 8991.8 |
AUC (0-72) is measure of area under the curve from time 0 to 72 hours post dose. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | nanogram*milliliter per hour (ng*hr/mL) (Mean) |
|---|---|
| SYR-322-MET Fasted | 1494.9 |
| SYR-322-MET Fed | 1472.8 |
AUC (0-inf) is a measure of total plasma exposure to the drug from time zero extrapolated to infinity. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, and 48 hours postdose
| Intervention | ng*hr/mL (Mean) |
|---|---|
| SYR-322-MET Fasted | 9195.3 |
| SYR-322-MET Fed | 8997.4 |
AUC (0-inf) is a measure of total plasma exposure to the drug from time zero extrapolated to infinity. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | ng*hr/mL (Mean) |
|---|---|
| SYR-322-MET Fasted | 1555.0 |
| SYR-322-MET Fed | 1536.8 |
AUC (0-tlqc) is a measure of total plasma exposure to the drug from Time 0 to Time of the Last Quantifiable Concentration (AUC [0-tlqc]). (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, and 48 hours postdose
| Intervention | ng*hr/mL (Mean) |
|---|---|
| SYR-322-MET Fasted | 9038.8 |
| SYR-322-MET Fed | 8853.8 |
AUC (0-tlqc) is a measure of total plasma exposure to the drug from Time 0 to Time of the Last Quantifiable Concentration (AUC [0-tlqc]). (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | ng*hr/mL (Mean) |
|---|---|
| SYR-322-MET Fasted | 1494.9 |
| SYR-322-MET Fed | 1472.8 |
CLr is a measure of apparent clearance of the drug from the urine. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, and 48 hours postdose
| Intervention | L/hr (Mean) |
|---|---|
| SYR-322-MET Fasted | 27.88 |
| SYR-322-MET Fed | 28.34 |
CLr is a measure of apparent clearance of the drug from the urine. The clearance is the rate at which waste substances are cleared from the blood. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | L/hr (Mean) |
|---|---|
| SYR-322-MET Fasted | 11.96 |
| SYR-322-MET Fed | 12.33 |
Maximum observed plasma concentration (Cmax) is the peak plasma concentration of a drug after administration, obtained directly from the plasma concentration-time curve. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, and 48 hours postdose
| Intervention | ng/mL (Mean) |
|---|---|
| SYR-322-MET Fasted | 1473.3 |
| SYR-322-MET Fed | 1251.7 |
Maximum observed plasma concentration (Cmax) is the peak plasma concentration of a drug after administration, obtained directly from the plasma concentration-time curve. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, and 72 hours postdose
| Intervention | ng/mL (Mean) |
|---|---|
| SYR-322-MET Fasted | 154.9 |
| SYR-322-MET Fed | 173.4 |
Maximum inhibition rate of plasma DPP-4 activity was determined from the inhibition-time curve. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 24 hours postdose
| Intervention | percentage of inhibition (Mean) |
|---|---|
| SYR-322-MET Fasted | 96.10 |
| SYR-322-MET Fed | 96.33 |
Mean residence time (MRT) calculated as area under the first moment plasma concentration-time curve (AUMC [0-inf]) divided by AUC (0-inf). AUMC (0-inf) is the area under the first moment plasma concentration-time curve from time 0 to infinity. (NCT02276274)
Timeframe: 3 hours prior to administration (predose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, and 48 hours postdose
| Intervention | hr (Mean) |
|---|---|
| SYR-322-MET Fasted | 6.213 |
| SYR-322-MET Fed | 6.097 |
The change between the baseline (pre-prandial (before meal)) and postprandial (after meal) glucose values were collected at Months 3 and 6 relative to baseline. (NCT02756832)
Timeframe: Baseline, Months 3 and 6
| Intervention | mmol/l (Mean) | |||
|---|---|---|---|---|
| Baseline | Change from Baseline to Month 3 | Change from Month 3 to Month 6 | Change from Baseline to Month 6 | |
| Alogliptin Benzoate | 10.4 | -1.9 | -0.5 | -2.4 |
Change in the participant's weight was collected at Months 3 and 6 relative to baseline. (NCT02756832)
Timeframe: Baseline, Months 3 and 6
| Intervention | kg (Mean) | |||
|---|---|---|---|---|
| Baseline | Change from Baseline to Month 3 | Change from Month 3 to Month 6 | Change from Baseline to Month 6 | |
| Alogliptin Benzoate | 90.6 | -1.5 | -1.1 | -2.6 |
Healthcare resources included rate of hospitalization, emergency, emergency room visits, physician office visits, and other type of usage. (NCT02756832)
Timeframe: Baseline up to Month 6
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Rate of Hospitalization | Rate of Emergency | Rate of Physician Office Visits | Rate of Other Type of Usage | |
| Alogliptin Benzoate | 0.6 | 0.1 | 0.6 | 0.1 |
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 Month 6 relative to baseline. Percentage of participants with a decrease of ≥0.3% from baseline in HbA1c were reported. (NCT02756832)
Timeframe: Baseline and Month 6
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin Benzoate | 89.1 |
Marked hyperglycemia is defined as fasting plasma glucose (FPG) higher than or equal to 11 mmol/L. (NCT02756832)
Timeframe: Month 3
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin Benzoate | 0.9 |
The change in the value of fasting plasma glucose value collected at Months 3 and 6 relative to baseline. Target FPG depended on the defined individual targets of glycemic control by HbA1c level ≤6.5 to 8.0 mmol/l. A negative change from Baseline indicates improvement. (NCT02756832)
Timeframe: Baseline, Months 3 and 6
| Intervention | mmol/l (Mean) | |||
|---|---|---|---|---|
| Baseline | Change from Baseline to Month 3 | Change from Month 3 to Month 6 | Change from Baseline to Month 6 | |
| Alogliptin Benzoate | 8.7 | -1.7 | -0.4 | -2.1 |
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 Month 6 relative to baseline. Glycosylated hemoglobin (HbA1c) as a diagnostic criteria of diabetes mellitus is ≥6.5%. A negative change from Baseline indicates improvement. (NCT02756832)
Timeframe: Baseline and Month 6
| Intervention | percentage of glycosylated hemoglobin (Mean) | |
|---|---|---|
| Baseline | Change from Baseline at Month 6 | |
| Alogliptin Benzoate | 8.1 | -1.2 |
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 Month 6 relative to baseline. Glycosylated hemoglobin (HbA1c) as a diagnostic criteria of diabetes mellitus is ≥6.5%. Subgroups included participants with different baseline clinical characteristics with predictors such as prior therapy of diabetes mellitus, sex, age group, cardiovascular risk group, therapy type (monotherapy or combined therapy), baseline body mass index (BMI) and initial glycemic control and T2DM duration. A negative change from Baseline indicates improvement. (NCT02756832)
Timeframe: Baseline and Month 6
| Intervention | percentage of glycosylated hemoglobin (Mean) | ||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Prior Therapy Diabetes Mellitus (DM), No Therapy | Prior Therapy DM, Monotherapy: Biguanides | Prior Therapy DM, Monotherapy: Sulfonylureas | Prior Therapy DM, Monotherapy: Other | Prior Therapy DM, Biguanides+Sulfonylureas | Prior Therapy DM, Biguanides+SGLT2 inhibitors | Prior Therapy DM, Combined therapy: Other | Sex, Male | Sex,Female | Age Group, <58 Years | Age Group, ≥58 Years | Cardiovascular (CV) Risk Group, High CV Risk | CV Risk Group, Very High CV Risk | Therapy Type (TT), Monotherapy: VIPIDIA® | TT, Combined: VIPIDIA®+Biguanides | TT, Combined: VIPIDIA®+Sulfonylureas | TT, Combined: VIPIDIA®+SGLT2 Inhibitors | TT, Combined: VIPIDIA®+Biguanides+Sulfonylureas | TT, Combined: VIPIDIA®+Biguanides+SGLT2 Inhibitors | TT, Combined: VIPIDIA®+Biguanides+Antidiabetics | TT,Combined: VIPIDIA®+Biguanide+Sulfonylurea+SGLT2 | BMI, Normal Weight (<25 kg/m^2) | BMI, Over-Weight (25≤BMI<30 kg/m^2) | BMI, Obesity Class I (30≤BMI<35 kg/m^2) | BMI, Obesity Class II (35≤BMI<40 kg/m^2) | BMI, Obesity Class III (BMI≥40 kg/m^2) | Glycemic Control, HBA1C<7.5% | Glycemic Control, 7.5%≥HBA1C<9% | Glycemic Control, HBA1C≥9% | T2DM Duration, 0-3 Years | T2DM Duration, 3-5 Years | T2DM Duration, 5-10 Years | T2DM Duration, >=10 Years | |
| Alogliptin Benzoate | -1.4 | -1.1 | -1.3 | -1.1 | -1.3 | -1.4 | -1.8 | -1.4 | -1.1 | -1.3 | -1.1 | -1.3 | -1.2 | -1.3 | -1.1 | -1 | 0 | -1.4 | -1.3 | -2.4 | -2.1 | -1.3 | -1.2 | -1.2 | -1.2 | -1.2 | -0.6 | -1.1 | -2.5 | -1.3 | -1.0 | -1.2 | -1.2 |
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 Months 3 and 6 relative to baseline. Glycosylated hemoglobin (HbA1c) as a diagnostic criteria of diabetes mellitus is ≥6.5%. A negative change from Baseline indicates improvement. (NCT02756832)
Timeframe: Baseline, Months 3 and 6
| Intervention | percentage of glycosylated hemoglobin (Mean) | ||
|---|---|---|---|
| Baseline | Change from Baseline to Month 3 | Change from Month 3 to Month 6 | |
| Alogliptin Benzoate | 8.1 | -0.8 | -0.4 |
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 Month 6 relative to baseline. Percentage of participants with a decrease of <7.0% from baseline in HbA1c were reported. (NCT02756832)
Timeframe: Baseline and Month 6
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin Benzoate | 52 |
The change between the total cholesterol triglycerides, low density lipoproteins and high density lipoproteins values were collected at Months 3 and 6 relative to baseline. (NCT02756832)
Timeframe: Baseline, Months 3 and 6
| Intervention | mmol/l (Mean) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Total Cholesterol, Baseline | Total Cholesterol, Change from Baseline to Month 3 | Total Cholesterol, Change from Month 3 to Month 6 | Total Cholesterol, Change from Baseline to Month 6 | Triglycerides, Baseline | Triglycerides, Change from Baseline to Month 3 | Triglycerides, Change from Month 3 to Month 6 | Triglycerides, Change from Baseline to Month 6 | Low Density Lipoproteins (LDL), Baseline | LDL, Change from Baseline to Month 3 | LDL, Change from Month 3 to Month 6 | LDL, Change from Baseline to Month 6 | High Density Lipoproteins (HDL), Baseline | HDL, Change from Baseline to Month 3 | HDL, Change from Month 3 to Month 6 | HDL, Change from Baseline to Month 6 | |
| Alogliptin Benzoate | 5.6 | -0.5 | -0.2 | -0.6 | 2.2 | -0.4 | -0.1 | -0.4 | 3.4 | -0.4 | -0.2 | -0.6 | 1.3 | 0.0 | 0.0 | 0.1 |
Changes in the SD of 24-hour blood glucose values (mg/dL) for each 7-day period between Week 3 and Week 4 (between Day 2 on Week 3 [Day 22] and Day 8 on Week 3 [Day 28]) of the treatment period, calculated from the value at the start of the observation period. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Day(D) 2 Week(W) 3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -13.04 | -15.24 | -12.91 | -13.28 | -11.94 | -10.90 | -11.63 |
| Trelagliptin 100 mg | -7.51 | -11.76 | -11.71 | -9.89 | -12.75 | -9.50 | -7.35 |
Change from baseline in SD of nocturnal blood glucose values at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -2.45 | -9.76 | -7.86 | -5.21 | -8.23 | -8.01 | -6.64 |
| Trelagliptin 100 mg | -0.71 | -3.55 | -4.06 | -2.96 | -5.67 | -5.25 | -2.93 |
Change from baseline in AUC for blood glucose during periods when blood glucose levels reached 110 mg/dL at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg·min/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -4735.1 | -3742.8 | -4576.9 | -4812.0 | -4592.1 | -4169.3 | -4335.7 |
| Trelagliptin 100 mg | -2263.8 | -2479.2 | -3755.3 | -3845.6 | -2581.9 | -2184.1 | -2634.2 |
Change from baseline in SD of daytime blood glucose values at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -13.28 | -13.12 | -10.98 | -12.54 | -10.44 | -9.49 | -10.81 |
| Trelagliptin 100 mg | -9.78 | -12.82 | -11.98 | -10.88 | -11.94 | -8.13 | -6.49 |
(NCT02771093)
Timeframe: Up to 29 days
| Intervention | Participants (Count of Participants) |
|---|---|
| Trelagliptin 100 mg | 1 |
| Alogliptin 25 mg | 2 |
Change from baseline in AUC for blood glucose levels at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg·min/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -4828.9 | -3594.8 | -4565.6 | -5023.4 | -4526.4 | -4097.5 | -4302.9 |
| Trelagliptin 100 mg | -2340.4 | -2348.4 | -3723.2 | -4017.8 | -2408.2 | -1837.6 | -2438.5 |
Change from baseline in AUC for blood glucose during periods when blood glucose levels was less than 70 mg/dL at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg·min/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | 0.4 | 0.0 | 13.4 | 26.9 | 0.0 | 0.0 | 0.0 |
| Trelagliptin 100 mg | -31.2 | -43.0 | -42.3 | -30.5 | -39.8 | -43.0 | -43.0 |
Change from baseline in AUC for blood glucose during periods when blood glucose levels reached 180 mg/dL at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg·min/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -2247.9 | -2086.7 | -2352.2 | -2492.3 | -2109.1 | -1976.3 | -2009.8 |
| Trelagliptin 100 mg | -989.9 | -1332.7 | -1685.1 | -1486.5 | -1449.4 | -1264.2 | -1166.8 |
Change from baseline in AUC for blood glucose during periods when blood glucose levels reached 140 mg/dL at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg·min/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -4021.4 | -3378.3 | -4119.9 | -4230.4 | -3840.0 | -3566.4 | -3667.1 |
| Trelagliptin 100 mg | -1935.9 | -2001.2 | -2978.2 | -2981.5 | -2550.5 | -1946.5 | -2043.5 |
Change from baseline in AUC for blood glucose during periods when blood glucose levels reached 160 mg/dL at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg·min/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -3075.8 | -2767.3 | -3273.0 | -3384.5 | -2990.8 | -2768.9 | -2818.8 |
| Trelagliptin 100 mg | -1458.0 | -1702.0 | -2335.8 | -2171.8 | -2031.0 | -1636.5 | -1603.9 |
Change from baseline in AUC for blood glucose when specific blood glucose levels (110 mg/dL) were observed during the 3 hour time period after breakfast, lunch and evening meal at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg·min/dL (Mean) | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| D2W3 after breakfast | D3W3 after breakfast | D4W3 after breakfast | D5W3 after breakfast | D6W3 after breakfast | D7W3 after breakfast | D8W3 after breakfast | D2W3 after lunch | D3W3 after lunch | D4W3 after lunch | D5W3 after lunch | D6W3 after lunch | D7W3 after lunch | D8W3 after lunch | D2W3 after evening meal | D3W3 after evening meal | D4W3 after evening meal | D5W3 after evening meal | D6W3 after evening meal | D7W3 after evening meal | D8W3 after evening meal | |
| Alogliptin 25 mg | -1052.7 | -1030.9 | -958.9 | -1319.8 | -832.5 | -966.3 | -1024.8 | -1131.4 | -941.9 | -701.1 | -1065.4 | -534.4 | -488.7 | -923.5 | -800.5 | -1023.6 | -1228.5 | -756.1 | -1144.2 | -669.9 | -577.0 |
| Trelagliptin 100 mg | -203.7 | -662.6 | -1024.6 | -97.2 | -696.1 | -573.8 | -399.0 | -669.0 | -500.1 | -468.2 | -793.5 | -798.5 | -320.4 | -521.3 | -1079.4 | -1273.0 | -1359.6 | -1351.4 | -1199.9 | -884.2 | -1142.0 |
Change from baseline in AUC for blood glucose when specific blood glucose levels (140 mg/dL) were observed during the 3 hour time period after breakfast, lunch and evening meal at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg·min/dL (Mean) | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| D2W3 after breakfast | D3W3 after breakfast | D4W3 after breakfast | D5W3 after breakfast | D6W3 after breakfast | D7W3 after breakfast | D8W3 after breakfast | D2W3 after lunch | D3W3 after lunch | D4W3 after lunch | D5W3 after lunch | D6W3 after lunch | D7W3 after lunch | D8W3 after lunch | D2W3 after evening meal | D3W3 after evening meal | D4W3 after evening meal | D5W3 after evening meal | D6W3 after evening meal | D7W3 after evening meal | D8W3 after evening meal | |
| Alogliptin 25 mg | -981.2 | -926.1 | -801.6 | -1178.0 | -791.8 | -910.1 | -951.6 | -1079.1 | -845.4 | -648.1 | -970.0 | -517.0 | -458.3 | -867.4 | -637.6 | -862.0 | -1016.8 | -613.7 | -966.4 | -586.4 | -535.0 |
| Trelagliptin 100 mg | -218.5 | -510.2 | -886.4 | -21.3 | -559.8 | -457.4 | -348.5 | -588.5 | -489.7 | -429.3 | -725.5 | -707.9 | -294.9 | -474.7 | -950.8 | -1077.3 | -1147.1 | -1147.5 | -1030.6 | -822.3 | -964.8 |
Change from baseline in AUC for blood glucose when specific blood glucose levels (160 mg/dL) were observed during the 3 hour time period after breakfast, lunch and evening meal at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg·min/dL (Mean) | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| D2W3 after breakfast | D3W3 after breakfast | D4W3 after breakfast | D5W3 after breakfast | D6W3 after breakfast | D7W3 after breakfast | D8W3 after breakfast | D2W3 after lunch | D3W3 after lunch | D4W3 after lunch | D5W3 after lunch | D6W3 after lunch | D7W3 after lunch | D8W3 after lunch | D2W3 after evening meal | D3W3 after evening meal | D4W3 after evening meal | D5W3 after evening meal | D6W3 after evening meal | D7W3 after evening meal | D8W3 after evening meal | |
| Alogliptin 25 mg | -829.2 | -770.4 | -609.9 | -981.3 | -696.8 | -760.4 | -806.3 | -890.4 | -705.5 | -552.5 | -811.9 | -469.7 | -384.6 | -730.1 | -507.4 | -671.1 | -808.9 | -508.3 | -759.6 | -504.1 | -460.2 |
| Trelagliptin 100 mg | -164.5 | -377.8 | -759.4 | 25.6 | -405.5 | -356.6 | -273.4 | -448.1 | -462.2 | -389.7 | -579.4 | -534.1 | -249.9 | -350.8 | -730.5 | -825.2 | -914.5 | -887.5 | -809.5 | -742.3 | -763.4 |
Change from baseline in AUC for blood glucose when specific blood glucose levels (180 mg/dL) were observed during the 3 hour time period after breakfast, lunch and evening meal at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg·min/dL (Mean) | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| D2W3 after breakfast | D3W3 after breakfast | D4W3 after breakfast | D5W3 after breakfast | D6W3 after breakfast | D7W3 after breakfast | D8W3 after breakfast | D2W3 after lunch | D3W3 after lunch | D4W3 after lunch | D5W3 after lunch | D6W3 after lunch | D7W3 after lunch | D8W3 after lunch | D2W3 after evening meal | D3W3 after evening meal | D4W3 after evening meal | D5W3 after evening meal | D6W3 after evening meal | D7W3 after evening meal | D8W3 after evening meal | |
| Alogliptin 25 mg | -660.1 | -592.9 | -375.6 | -776.3 | -556.5 | -578.2 | -603.6 | -626.6 | -521.1 | -404.1 | -589.9 | -354.6 | -293.6 | -546.4 | -375.9 | -484.4 | -597.2 | -427.8 | -552.4 | -374.5 | -346.5 |
| Trelagliptin 100 mg | -90.7 | -241.2 | -632.2 | 36.5 | -272.2 | -264.2 | -214.8 | -300.3 | -383.8 | -307.0 | -430.4 | -353.5 | -184.2 | -234.0 | -507.6 | -592.4 | -662.4 | -641.9 | -598.8 | -612.6 | -555.4 |
Change from baseline in maximum variation of glucose levels between before and after breakfast, lunch and evening meal at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg/dL (Mean) | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| D2W3 between before/after breakfast | D3W3 between before/after breakfast | D4W3 between before/after breakfast | D5W3 between before/after breakfast | D6W3 between before/after breakfast | D7W3 between before/after breakfast | D8W3 between before/after breakfast | D2W3 between before/after lunch | D3W3 between before/after lunch | D4W3 between before/after lunch | D5W3 between before/after lunch | D6W3 between before/after lunch | D7W3 between before/after lunch | D8W3 between before/after lunch | D2W3 between before/after evening meal | D3W3 between before/after evening meal | D4W3 between before/after evening meal | D5W3 between before/after evening meal | D6W3 between before/after evening meal | D7W3 between before/after evening meal | D8W3 between before/after evening meal | |
| Alogliptin 25 mg | -28.9 | -35.4 | -42.1 | -25.5 | -29.8 | -33.3 | -34.5 | -35.5 | -29.5 | -6.2 | -31.2 | -13.1 | -14.9 | -29.1 | -15.6 | -21.8 | -24.2 | -5.2 | -24.6 | -4.4 | -6.6 |
| Trelagliptin 100 mg | -13.9 | -47.4 | -41.2 | -7.0 | -38.6 | -36.4 | -36.2 | -30.2 | -34.5 | -23.8 | -34.8 | -37.0 | -12.7 | -15.6 | -37.8 | -49.1 | -42.6 | -31.5 | -41.9 | -33.6 | -39.3 |
Change from baseline in mean 24-hour blood glucose levels at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -16.77 | -12.46 | -15.85 | -17.46 | -15.79 | -14.23 | -14.94 |
| Trelagliptin 100 mg | -8.14 | -8.15 | -13.12 | -13.95 | -8.37 | -6.38 | -8.46 |
Change from baseline in MAGE at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -47.25 | -52.75 | -44.67 | -50.22 | -34.82 | -37.18 | -41.38 |
| Trelagliptin 100 mg | -28.42 | -33.72 | -36.08 | -23.12 | -38.05 | -25.74 | -24.26 |
Change from baseline in mean nocturnal blood glucose levels at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -10.69 | -3.38 | -3.76 | -6.43 | -7.98 | -8.59 | -5.96 |
| Trelagliptin 100 mg | -2.65 | 0.52 | -3.17 | -4.09 | 5.55 | 3.86 | 1.06 |
Change from baseline in mean daytime blood glucose levels at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -20.38 | -17.21 | -21.80 | -22.54 | -19.34 | -16.92 | -19.78 |
| Trelagliptin 100 mg | -11.08 | -12.48 | -18.42 | -19.53 | -14.27 | -10.86 | -12.90 |
Change from baseline in peak postprandial glucose levels during the 3 hour time period after breakfast, lunch and evening meal at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg/dL (Mean) | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| D2W3 after breakfast | D3W3 after breakfast | D4W3 after breakfast | D5W3 after breakfast | D6W3 after breakfast | D7W3 after breakfast | D8W3 after breakfast | D2W3 after lunch | D3W3 after lunch | D4W3 after lunch | D5W3 after lunch | D6W3 after lunch | D7W3 after lunch | D8W3 after lunch | D2W3 after evening meal | D3W3 after evening meal | D4W3 after evening meal | D5W3 after evening meal | D6W3 after evening meal | D7W3 after evening meal | D8W3 after evening meal | |
| Alogliptin 25 mg | -35.6 | -29.1 | -29.0 | -41.1 | -24.2 | -29.6 | -31.4 | -40.8 | -35.1 | -16.6 | -41.6 | -18.7 | -18.1 | -33.6 | -21.3 | -21.6 | -32.7 | -15.6 | -33.8 | -13.9 | -15.9 |
| Trelagliptin 100 mg | -11.3 | -35.4 | -39.4 | -4.9 | -28.6 | -23.7 | -16.6 | -26.9 | -25.9 | -21.9 | -34.8 | -32.7 | -11.5 | -17.7 | -40.6 | -44.5 | -45.8 | -40.6 | -41.5 | -32.3 | -42.2 |
Change from baseline in cumulative time during periods when blood glucose levels reached 140 mg/dL at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | min (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -212.5 | -147.1 | -166.1 | -163.2 | -193.2 | -182.1 | -198.6 |
| Trelagliptin 100 mg | -116.9 | -105.0 | -163.8 | -192.3 | -114.2 | -96.9 | -133.8 |
Change from baseline in cumulative time during periods when blood glucose levels reached 160 mg/dL at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | min (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -229.3 | -173.2 | -234.3 | -236.8 | -232.9 | -213.2 | -225.4 |
| Trelagliptin 100 mg | -134.2 | -75.0 | -167.7 | -200.0 | -153.1 | -93.5 | -115.0 |
Change from baseline in cumulative time during periods when blood glucose levels reached 180 mg/dL at each time points was calculated. (NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | min (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | -210.7 | -167.1 | -236.4 | -225.4 | -216.8 | -194.3 | -193.2 |
| Trelagliptin 100 mg | -91.2 | -117.3 | -167.3 | -153.1 | -137.7 | -94.2 | -105.0 |
(NCT02771093)
Timeframe: Baseline, up to 28 days
| Intervention | mg/dL (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline | D2W3 | D3W3 | D4W3 | D5W3 | D6W3 | D7W3 | D8W3 | |
| Alogliptin 25 mg | 40.44 | 27.41 | 25.20 | 27.54 | 27.16 | 28.51 | 29.54 | 28.81 |
| Trelagliptin 100 mg | 38.18 | 30.68 | 26.42 | 26.48 | 28.29 | 25.44 | 28.68 | 30.84 |
Physical examination included examination of the following body systems: (1) respiratory system; (2) cardiovascular system; (3) nervous system (4) dermatologic system; and (5) gastrointestinal system. A summarized data for the above body systems was reported for participants with clinically significant findings. (NCT02856113)
Timeframe: From Day 1 to end of treatment period (up to 52 weeks)
| Intervention | percentage of participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 4 | Week 12 | Week 18 | Week 26 | Week 32 | Week 39 | Week 45 | Week 52 | |
| Placebo | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
Physical examination included examination of the following body systems: (1) respiratory system; (2) cardiovascular system; (3) nervous system (4) dermatologic system; and (5) gastrointestinal system. A summarized data for the above body systems was reported for participants with clinically significant findings. (NCT02856113)
Timeframe: From Day 1 to end of treatment period (up to 52 weeks)
| Intervention | percentage of participants (Number) | ||||
|---|---|---|---|---|---|
| Week 12 | Week 18 | Week 26 | Week 39 | Week 52 | |
| Alogliptin 25 mg | 0 | 0 | 0 | 0 | 0 |
Vital signs included body temperature (oral or tympanic measurement), respiratory rate, blood pressure [systolic blood pressure (SBP) and diastolic blood pressure (DBP)] resting more than 5 minutes, and pulse (beats per minute). Data for participants with abnormal vital signs was reported. The percentage of participants are calculated based on the participants with non-missing data at that time-point. (NCT02856113)
Timeframe: From Day 1 to end of treatment period (up to 52 weeks)
| Intervention | percentage of participants (Number) | ||||
|---|---|---|---|---|---|
| SBP (millimeters of mercury [mmHg]): >150 | DBP (mmHg): >95 | Pulse Rate (beats per minute [bpm]): <50 | Pulse Rate (beats per minute [bpm]): >120 | Temperature (Celsius [C]): <35.6 | |
| Alogliptin 25 mg | 2.8 | 4.2 | 1.4 | 1.4 | 3.1 |
Vital signs included body temperature (oral or tympanic measurement), respiratory rate, blood pressure [systolic blood pressure (SBP) and diastolic blood pressure (DBP)] resting more than 5 minutes, and pulse (beats per minute). Data for participants with abnormal vital signs was reported. The percentage of participants are calculated based on the participants with non-missing data at that time-point. (NCT02856113)
Timeframe: From Day 1 to end of treatment period (up to 52 weeks)
| Intervention | percentage of participants (Number) | |
|---|---|---|
| SBP (millimeters of mercury [mmHg]): >150 | DBP (mmHg): >95 | |
| Placebo | 1.3 | 4.0 |
The percentage of participants with any abnormal standard safety laboratory values (hematology, serum chemistry, and urinalysis) were collected throughout study. Abnormal values for hematology included hematocrit (percentage of hematocrit [%]), hemoglobin (grams per liter [g/L]), erythrocyte mean corpuscular volume (MCV)(femtoliter [fL]), erythrocytes (10^12/L), and leukocytes (10^9/L). Abnormal values for serum chemistry included for alanine aminotransferase (units per liter [U/L]), aspartate aminotransferase (U/L), cholesterol (millimoles per liter [mmol/L]), gamma glutamyl transferase (U/L), glucose (mmol/L): < 2.8 mmol/L, potassium (mmol/L), sodium (mmol/L), and triglycerides (mmol/L). ULN is upper limit of normal and LLN is lower limit of normal. (NCT02856113)
Timeframe: From Day 1 to end of treatment period (up to 52 weeks)
| Intervention | percentage of participants (Number) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Alanine Aminotransferase (U/L): >= 3 x ULN | Cholesterol (mmol/L): >7.72 mmol/L | Gamma Glutamyl Transferase (U/L): >= 3 x ULN | Glucose (mmol/L): < 2.8 mmol/L | Glucose (mmol/L): >19.4 mmol/L | Potassium (mmol/L): <3.0 mmol/L | Phosphate (mmol/L): >2.00 mmol/L | Triglycerides (mmol/L): >2.5x ULN | Hematocrit (%): >1.2 x ULN | Hemoglobin (g/L): < 0.8 x LLN | Hemoglobin (g/L): >1.2 x ULN | Erythrocyte Mean Corpuscular Volume (fL): <70 fL | Erythrocyte Mean Corpuscular Volume (fL): >100 fL | Erythrocytes (10^12/L): >1.2 x ULN | Leukocytes (10^9/L): >1.5 x ULN | |
| Alogliptin 25 mg | 5.6 | 1.4 | 6.9 | 20.5 | 13.7 | 1.4 | 1.4 | 1.4 | 8.3 | 1.4 | 2.8 | 2.8 | 2.8 | 1.4 | 2.8 |
The percentage of participants with any abnormal standard safety laboratory values (hematology, serum chemistry, and urinalysis) were collected throughout study. Abnormal values for hematology included hematocrit (percentage of hematocrit [%]), hemoglobin (grams per liter [g/L]), erythrocyte mean corpuscular volume (MCV)(femtoliter [fL]), erythrocytes (10^12/L), and leukocytes (10^9/L). Abnormal values for serum chemistry included for alanine aminotransferase (units per liter [U/L]), aspartate aminotransferase (U/L), cholesterol (millimoles per liter [mmol/L]), gamma glutamyl transferase (U/L), glucose (mmol/L): < 2.8 mmol/L, potassium (mmol/L), sodium (mmol/L), and triglycerides (mmol/L). ULN is upper limit of normal and LLN is lower limit of normal. (NCT02856113)
Timeframe: From Day 1 to end of treatment period (up to 52 weeks)
| Intervention | percentage of participants (Number) | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Alanine Aminotransferase (U/L): >= 3 x ULN | Aspartate Aminotransferase (U/L): >= 3 x ULN | Cholesterol (mmol/L): >7.72 mmol/L | Gamma Glutamyl Transferase (U/L): >= 3 x ULN | Glucose (mmol/L): < 2.8 mmol/L | Glucose (mmol/L): >19.4 mmol/L | Sodium (mmol/L): <130 mmol/L | Triglycerides (mmol/L): >2.5x ULN | Hematocrit (%): >1.2 x ULN | Hemoglobin (g/L): >1.2 x ULN | Erythrocyte Mean Corpuscular Volume (fL): <70 fL | Erythrocytes (10^12/L): >1.2 x ULN | Leukocytes (10^9/L): >1.5 x ULN | |
| Placebo | 10.7 | 2.7 | 1.3 | 2.7 | 13.3 | 10.7 | 1.3 | 6.7 | 9.5 | 4.1 | 2.7 | 1.4 | 2.7 |
(NCT02856113)
Timeframe: Week 26 and 52
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Week 26: Abnormal, Not Clinically Significant | Week 26: Abnormal, Clinically Significant | Week 52: Abnormal, Not Clinically Significant | Week 52: Abnormal, Clinically Significant | |
| Alogliptin 25 mg | 6 | 0 | 6 | 0 |
| Placebo | 7 | 2 | 7 | 1 |
Change in the value of HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) was collected at Weeks 12, 18, 39 and 52 relative to Baseline. MMRM was used for the analysis. (NCT02856113)
Timeframe: Baseline and Weeks 12, 18, 39 and 52
| Intervention | percentage of HbA1c (Least Squares Mean) | |||
|---|---|---|---|---|
| Change From Baseline at Week 12 | Change From Baseline at Week 18 | Change From Baseline at Week 39 | Change From Baseline at Week 52 | |
| Alogliptin 25 mg | -0.365 | -0.202 | 0.091 | 0.281 |
| Placebo | -0.319 | -0.206 | 0.502 | 0.764 |
(NCT02856113)
Timeframe: Baseline, Weeks 26 and 52
| Intervention | percentage of CD8+ T cells (Mean) | ||
|---|---|---|---|
| Baseline | Change From Baseline at Week 26 | Change From Baseline at Week 52 | |
| Alogliptin 25 mg | 59.6 | 1.7 | -0.3 |
| Placebo | 59.7 | -0.2 | 1.0 |
(NCT02856113)
Timeframe: Baseline, Weeks 26 and 52
| Intervention | percentage of CD4+ T cells (Mean) | ||
|---|---|---|---|
| Baseline | Change From Baseline at Week 26 | Change From Baseline at Week 52 | |
| Alogliptin 25 mg | 77.7 | 1.6 | 0.8 |
| Placebo | 78.2 | 1.2 | 1.0 |
Biomarkers of bone turnover are bone-specific alkaline phosphatase to assess changes in bone formation and C-terminal telopeptide (CTX) to assess changes in bone resorption. (NCT02856113)
Timeframe: Baseline, Weeks 26 and 52
| Intervention | units per liter (U/L) (Mean) | ||
|---|---|---|---|
| Baseline | Change From Baseline at Week 26 | Change From Baseline at Week 52 | |
| Alogliptin 25 mg | 62.62 | -7.47 | -15.43 |
| Placebo | 62.09 | -6.20 | -14.36 |
An AE was defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. (NCT02856113)
Timeframe: From the study start up to end of the study (up to 54 weeks)
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 76.3 |
| Alogliptin 25 mg | 80.0 |
Mild to moderate hypoglycemia (abnormal low blood sugar) was defined as blood glucose less than (<) 60 milligram per deciliter (mg/dL) (3.33 millimole per liter [mmol/L]) in the presence of symptoms, or blood glucose <50 mg/dL (2.78 mmol/L) with or without symptoms. Severe hypoglycemia was defined as any episode requiring the assistance of another person to actively administer carbohydrate, glucagon, or other resuscitative actions, associated with a documented blood glucose <60 mg/dL (3.33 mmol/L) (unless the clinical situation makes obtaining a blood glucose difficult [example, it involves coma or seizure]). (NCT02856113)
Timeframe: From Day 1 to end of treatment period (up to 52 weeks)
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 7.9 |
| Alogliptin 25 mg | 5.3 |
Change in the value of HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) was collected at Week 26 relative to Baseline. Mixed model for repeated measures (MMRM) was used for the analysis. (NCT02856113)
Timeframe: Baseline and Week 26
| Intervention | percentage of HbA1c (Least Squares Mean) |
|---|---|
| Placebo | -0.011 |
| Alogliptin 25 mg | 0.091 |
The percentage of participants are calculated based on the participants with non-missing data at that time-point. (NCT02856113)
Timeframe: From Day 1 to end of treatment period (up to 52 weeks)
| Intervention | percentage of participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Bladder Infection | COVID-19 Infection | Low Urinary Tract Infection | Lower Respiratory Tract Infection | Sinus Infection | Upper Respiratory Infection | Upper Respiratory Tract Infection | Lower Urinary Tract Infection | |
| Alogliptin 25 mg | 11.1 | 0.0 | 11.1 | 11.1 | 11.1 | 44.4 | 0.0 | 0.0 |
| Placebo | 0.0 | 9.1 | 0.0 | 9.1 | 9.1 | 18.2 | 9.1 | 9.1 |
(NCT02989649)
Timeframe: Months 3 and 6
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Month 3 | Month 6 | |
| Alogliptin or Alogliptin Fixed Dose Combinations (FDCs) | 100 | 100 |
An ADR is defined as any response to a medicinal product that is noxious and unintended and that occurs at doses normally used in humans for the prophylaxis, diagnosis, or therapy of diseases or for the restoration, correction, or modification of physiological function. An SAE is defined as any untoward medical occurrence or effect that at any dose results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect or is medically important due to other reasons than the above mentioned criteria. Adverse events such as pancreatitis, hepatic disorders, and hypersensitivity reactions (including angioedema, anaphylaxis, and Stevens-Johnson syndrome) were considered as AESI. (NCT02989649)
Timeframe: Baseline up to Month 6
| Intervention | Participants (Count of Participants) | ||
|---|---|---|---|
| Adverse Drug Reaction (ADR) | Serious Adverse Event (SAE) | Adverse Event of Special Interest (AESI) | |
| Alogliptin or Alogliptin Fixed Dose Combinations (FDCs) | 1 | 0 | 0 |
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 Months 3 and 6 relative to baseline. A negative change from Baseline indicates improvement. (NCT02989649)
Timeframe: Baseline and Months 3 and 6
| Intervention | percentage of glycosylated hemoglobin (Mean) | |
|---|---|---|
| Month 3 | Month 6 | |
| Alogliptin or Alogliptin Fixed Dose Combinations (FDCs) | -1.022 | -1.092 |
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 Month 6 relative to baseline. Glycosylated hemoglobin (HbA1c) as a diagnostic criteria of diabetes mellitus is ≥6.5%. Subgroups included participants with different baseline clinical characteristics with predictors such as prior therapy of diabetes mellitus, sex, age group, cardiovascular risk group, therapy type (monotherapy or combined therapy), baseline body mass index (BMI) and initial glycemic control. A negative change from Baseline indicates improvement. (NCT02989649)
Timeframe: Baseline and Month 6
| Intervention | percentage of glycosylated hemoglobin (Mean) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Prior Therapy of Diabetes Mellitus, Ever Used | Prior Therapy of Diabetes Mellitus, Never Used | Sex, Male | Sex, Female | Age, <45 years | Age, >=45 to <65 years | Age,>=65 years | Cardiovascular Risk Group, Yes | Cardiovascular Risk Group, No | Therapy Type, Monotherapy | Therapy Type, Combined Therapy | Baseline BMI, <25 kg/m^2 | Baseline BMI, 25 to <30 kg/m^2 | Baseline BMI, >=30 kg/m^2 | Initial Glycemic Control, <7% | Initial Glycemic Control, >=7% | |
| Alogliptin or Alogliptin Fixed Dose Combinations (FDCs) | -1.154 | -0.882 | -1.055 | -1.150 | -1.658 | -1.370 | -0.203 | -1.100 | -1.092 | -1.032 | -1.106 | -1.101 | -1.037 | -1.342 | -0.046 | -1.525 |
The change between the fasting plasma glucose value collected at Months 3 and 6 relative to baseline. A negative change from Baseline indicates improvement. (NCT02989649)
Timeframe: Baseline and Months 3 and 6
| Intervention | mg/dL (Mean) | |
|---|---|---|
| Month 3 | Month 6 | |
| Alogliptin or Alogliptin Fixed Dose Combinations (FDCs) | -1.058 | -0.714 |
Percentage of participants with a decrease of >0.3% from baseline in HbA1c along with no tolerability findings were reported. Tolerability findings included hypoglycemic event, or weight gain ≥5%. (NCT02989649)
Timeframe: Baseline and Month 6
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin or Alogliptin Fixed Dose Combinations (FDCs) | 64.3 |
Percentage of participants with a decrease of <7.0% from baseline in HbA1c were reported. (NCT02989649)
Timeframe: Baseline and Month 6
| Intervention | percentage of participants (Number) |
|---|---|
| Alogliptin or Alogliptin Fixed Dose Combinations (FDCs) | 51.0 |
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 Month 6 relative to baseline. Glycosylated hemoglobin (HbA1c) as a diagnostic criteria of diabetes mellitus is ≥6.5%. A negative change from Baseline indicates improvement. (NCT02989649)
Timeframe: Baseline and Month 6
| Intervention | percentage of glycosylated hemoglobin (Mean) |
|---|---|
| Alogliptin or Alogliptin Fixed Dose Combinations (FDCs) | -1.092 |
Participants answered standardized questions about their preference of drug therapy for Type 2 Diabetes Mellitus. Participants selected one choice from the following 4 choices; either once-weekly DPP-4 inhibitor or daily DPP-4 inhibitor, once-weekly DPP-4 inhibitor, daily DPP-4 inhibitor, neither once-weekly DPP-4 inhibitor nor daily DPP-4 inhibitor. Reported data was the number of participants with a choice of either trelagliptin (once-weekly DPP-4 inhibitor) or alogliptin (once-daily DPP-4 inhibitor), trelagliptin, alogliptin, neither trelagliptin nor alogliptin. (NCT03231709)
Timeframe: At Week 16
| Intervention | Participants (Count of Participants) | |||
|---|---|---|---|---|
| Either Trelagliptin or Alogliptin | Trelagliptin | Alogliptin | Neither Trelagliptin nor Alogliptin | |
| Alogliptin 25 mg + Trelagliptin 100 mg | 7 | 10 | 13 | 0 |
| Trelagliptin 100 mg + Alogliptin 25 mg | 4 | 8 | 18 | 0 |
Participants answered standardized questions about their preference of drug therapy for Type 2 Diabetes Mellitus. The preference of drug therapy was categorized by background factors like age (years), gender, height (cm), weight (kg), BMI (kg/m^2), duration of diabetes (years), work status, alcohol intake history, smoking habits, experience of educational hospitalization on DM, presence of cohabiter, percentage of compliance with DPP-4 inhibitors during 4-weeks before the start of treatment period, number of oral drugs per day at the beginning of treatment period (excluding investigational drug), complication of metabolic syndrome, percentage of HbA1c (NGSP is the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) at the time of informed consent. (NCT03231709)
Timeframe: At Week 16
| Intervention | Participants (Count of Participants) | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Age, Min <= - <65 | Age, 65 <= - <75 | Gender, Male | Gender, Female | Height, Min <= - <150 | Height, 150 <= - <160 | Height, 160 <= - <170 | Height, 170 <= - <=Max | Weight, Min <= - <50.0 | Weight, 50.0 <= - <60.0 | Weight, 60.0<= - <70.0 | Weight, 70.0 <= - <80.0 | Weight, 80.0 <= - <=Max | BMI, Min <= - <18.5 | BMI, 18.5 <= - <25.0 | BMI, 25.0 <= - <=Max | Duration of Diabetes, 3 Years or More | Duration of Diabetes, Less than 3 Years | Work Status, Worker | Work Status, Unemployed | Alcohol Intake History, Regular Drinker | Alcohol Intake History, Occasional Drinker | Alcohol Intake History, Non-Drinker | Had Smoking Habits | Had No Smoking Habits | Had Experience of Educational Hospitalization | Had No Experience of Educational Hospitalization | Presence of Cohabiter, Live alone | Presence of Cohabiter, Living together | Compliance with DPP-4 Inhibitors, 90% or More | Number of Oral Drugs per Day, 1 or 2 Tablet(s) | Number of Oral Drugs per Day, 3 - 5 Tablets | Number of Oral Drugs per Day, 6 Tablets or More | Had Complication of Metabolic Syndrome | Had No Complication of Metabolic Syndrome | HbA1c (NGSP), < 7.0% | HbA1c (NGSP), 7.0%<= - <8.0% | HbA1c (NGSP), 8.0%<= | |
| Alogliptin Preference | 16 | 15 | 27 | 4 | 0 | 2 | 14 | 15 | 0 | 5 | 12 | 7 | 7 | 0 | 18 | 13 | 28 | 3 | 22 | 9 | 23 | 0 | 8 | 2 | 29 | 2 | 29 | 4 | 27 | 31 | 13 | 11 | 7 | 14 | 17 | 11 | 14 | 6 |
| Either Trelagliptin or Alogliptin | 9 | 2 | 11 | 0 | 0 | 0 | 1 | 10 | 0 | 0 | 3 | 8 | 0 | 0 | 9 | 2 | 10 | 1 | 9 | 2 | 5 | 2 | 4 | 4 | 7 | 3 | 8 | 1 | 10 | 11 | 1 | 5 | 5 | 4 | 7 | 1 | 7 | 3 |
| Neither Trelagliptin Nor Alogliptin | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Trelagliptin Preference | 13 | 5 | 16 | 2 | 1 | 1 | 9 | 7 | 1 | 5 | 3 | 6 | 3 | 1 | 9 | 8 | 17 | 1 | 16 | 2 | 7 | 3 | 8 | 4 | 14 | 0 | 18 | 3 | 15 | 18 | 7 | 8 | 3 | 4 | 14 | 6 | 8 | 4 |
Participants answered standardized questions about their preference of drug therapy for Type 2 Diabetes Mellitus. The preference of drug therapy was categorized by background factors like age (years), gender, height (cm), weight (kg), BMI (kg/m^2), duration of diabetes (years), work status, alcohol intake history, smoking habits, experience of educational hospitalization on DM, presence of cohabiter, percentage of compliance with DPP-4 inhibitors during 4-weeks before the start of treatment period, number of oral drugs per day at the beginning of treatment period (excluding investigational drug), complication of metabolic syndrome, percentage of HbA1c (NGSP is the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) at the time of informed consent. (NCT03231709)
Timeframe: At Week 16
| Intervention | Participants (Count of Participants) | |||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Age, Min <= - <65 | Age, 65 <= - <75 | Gender, Male | Gender, Female | Height, 150 <= - <160 | Height, 160 <= - <170 | Height, 170 <= - <=Max | Weight, 50.0 <= - <60.0 | Weight, 60.0<= - <70.0 | Weight, 70.0 <= - <80.0 | Weight, 80.0 <= - <=Max | BMI, Min <= - <18.5 | BMI, 18.5 <= - <25.0 | BMI, 25.0 <= - <=Max | Duration of Diabetes, 3 Years or More | Duration of Diabetes, Less than 3 Years | Work Status, Worker | Work Status, Unemployed | Alcohol Intake History, Regular Drinker | Alcohol Intake History, Occasional Drinker | Alcohol Intake History, Non-Drinker | Had Smoking Habits | Had No Smoking Habits | Had Experience of Educational Hospitalization | Had No Experience of Educational Hospitalization | Presence of Cohabiter, Live alone | Presence of Cohabiter, Living together | Compliance with DPP-4 Inhibitors, 90% or More | Number of Oral Drugs per Day, 1 or 2 Tablet(s) | Number of Oral Drugs per Day, 3 - 5 Tablets | Number of Oral Drugs per Day, 6 Tablets or More | Had Complication of Metabolic Syndrome | Had No Complication of Metabolic Syndrome | HbA1c (NGSP), < 7.0% | HbA1c (NGSP), 7.0%<= - <8.0% | HbA1c (NGSP), 8.0%<= | |
| Alogliptin Preference | 7 | 6 | 12 | 1 | 1 | 3 | 9 | 1 | 7 | 2 | 3 | 0 | 8 | 5 | 13 | 0 | 9 | 4 | 11 | 0 | 2 | 1 | 12 | 1 | 12 | 2 | 11 | 13 | 4 | 6 | 3 | 5 | 8 | 8 | 3 | 2 |
| Either Trelagliptin or Alogliptin | 5 | 2 | 7 | 0 | 0 | 1 | 6 | 0 | 2 | 5 | 0 | 0 | 5 | 2 | 6 | 1 | 5 | 2 | 2 | 1 | 4 | 4 | 3 | 1 | 6 | 1 | 6 | 7 | 0 | 2 | 5 | 3 | 4 | 0 | 6 | 1 |
| Neither Trelagliptin Nor Alogliptin | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Trelagliptin Preference | 8 | 2 | 9 | 1 | 1 | 6 | 3 | 5 | 1 | 2 | 2 | 1 | 5 | 4 | 10 | 0 | 9 | 1 | 3 | 3 | 4 | 2 | 8 | 0 | 10 | 1 | 9 | 10 | 5 | 3 | 2 | 3 | 7 | 2 | 4 | 4 |
Participants answered standardized questions about their preference of drug therapy for Type 2 Diabetes Mellitus. The preference of drug therapy was categorized by background factors like age (years), gender, height (cm), weight (kg), BMI (kg/m^2), duration of diabetes (years), work status, alcohol intake history, smoking habits, experience of educational hospitalization on DM, presence of cohabiter, percentage of compliance with DPP-4 inhibitors during 4-weeks before the start of treatment period, number of oral drugs per day at the beginning of treatment period (excluding investigational drug), complication of metabolic syndrome, percentage of HbA1c (NGSP is the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) at the time of informed consent. (NCT03231709)
Timeframe: At Week 16
| Intervention | Participants (Count of Participants) | ||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Age, Min <= - <65 | Age, 65 <= - <75 | Gender, Male | Gender, Female | Height, Min <= - <150 | Height, 150 <= - <160 | Height, 160 <= - <170 | Height, 170 <= - <=Max | Weight, Min <= - <50.0 | Weight, 50.0 <= - <60.0 | Weight, 60.0<= - <70.0 | Weight, 70.0 <= - <80.0 | Weight, 80.0 <= - <=Max | BMI, 18.5 <= - <25.0 | BMI, 25.0 <= - <=Max | Duration of Diabetes, 3 Years or More | Duration of Diabetes, Less than 3 Years | Work Status, Worker | Work Status, Unemployed | Alcohol Intake History, Regular Drinker | Alcohol Intake History, Occasional Drinker | Alcohol Intake History, Non-Drinker | Had Smoking Habits | Had No Smoking Habits | Had Experience of Educational Hospitalization | Had No Experience of Educational Hospitalization | Presence of Cohabiter, Live alone | Presence of Cohabiter, Living together | Compliance with DPP-4 Inhibitors, 90% or More | Number of Oral Drugs per Day, 1 or 2 Tablet(s) | Number of Oral Drugs per Day, 3 - 5 Tablets | Number of Oral Drugs per Day, 6 Tablets or More | Had Complication of Metabolic Syndrome | Had No Complication of Metabolic Syndrome | HbA1c (NGSP), < 7.0% | HbA1c (NGSP), 7.0%<= - <8.0% | HbA1c (NGSP), 8.0%<= | |
| Alogliptin Preference | 9 | 9 | 15 | 3 | 0 | 1 | 11 | 6 | 0 | 4 | 5 | 5 | 4 | 10 | 8 | 15 | 3 | 13 | 5 | 12 | 0 | 6 | 1 | 17 | 1 | 17 | 2 | 16 | 18 | 9 | 5 | 4 | 9 | 9 | 3 | 11 | 4 |
| Either Trelagliptin or Alogliptin | 4 | 0 | 4 | 0 | 0 | 0 | 0 | 4 | 0 | 0 | 1 | 3 | 0 | 4 | 0 | 4 | 0 | 4 | 0 | 3 | 1 | 0 | 0 | 4 | 2 | 2 | 0 | 4 | 4 | 1 | 3 | 0 | 1 | 3 | 1 | 1 | 2 |
| Neither Trelagliptin Nor Alogliptin | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Trelagliptin Preference | 5 | 3 | 7 | 1 | 1 | 0 | 3 | 4 | 1 | 0 | 2 | 4 | 1 | 4 | 4 | 7 | 1 | 7 | 1 | 4 | 0 | 4 | 2 | 6 | 0 | 8 | 2 | 6 | 8 | 2 | 5 | 1 | 1 | 7 | 4 | 4 | 0 |
(NCT03501277)
Timeframe: Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose
| Intervention | nanogram per milliliter (ng/ml) (Geometric Mean) | |
|---|---|---|
| Alogliptin | Pioglitazone | |
| Regimen A | 165.3 | 678.3 |
| Regimen B | 154.9 | 706.5 |
| Regimen C | 162.3 | 1052.1 |
| Regimen D | 157.4 | 1141.5 |
(NCT03501277)
Timeframe: Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose
| Intervention | hour*nanogram per milliliter (h*ng/mL) (Geometric Mean) | |
|---|---|---|
| Alogliptin | Pioglitazone | |
| Regimen A | 2197.3 | 5726.0 |
| Regimen B | 2163.4 | 5471.9 |
| Regimen C | 2194.7 | 10141.6 |
| Regimen D | 2195.0 | 9907.6 |
The change in the value of fasting blood glucose collected at final assessment point (up to Month 12) relative to baseline. (NCT03555565)
Timeframe: Baseline, up to final assessment point (up to Month 12)
| Intervention | milligram/deciliter (mg/dL) (Mean) |
|---|---|
| Alogliptin and Metformin Hydrochloride | -12.08 |
The change in the value of fasting insulin collected at final assessment point (up to Month 12) relative to baseline. (NCT03555565)
Timeframe: Baseline, up to final assessment point (up to Month 12)
| Intervention | microunit/milliliter (mcrU/mL) (Mean) |
|---|---|
| Alogliptin and Metformin Hydrochloride | 1.21 |
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 final assessment point (up to Month 12) relative to baseline. (NCT03555565)
Timeframe: Baseline, up to final assessment point (up to Month 12)
| Intervention | Percent (Mean) |
|---|---|
| Alogliptin and Metformin Hydrochloride | -0.259 |
An adverse event (AE) is defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have a causal relationship with this treatment. (NCT03555565)
Timeframe: Up to 12 months
| Intervention | Percentage of Participants (Number) |
|---|---|
| Alogliptin and Metformin Hydrochloride | 5.93 |
Serious ADRs are defined as SAEs that are, in the investigator's opinion, of causal relationship to the study treatment. An SAE is an adverse event 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. 95% Confidence Interval was calculated using exact method. (NCT04980040)
Timeframe: From first dose of study drug up to 30 days post last dose of study drug (Up to 79.77 weeks)
| Intervention | percentage of participants (Number) |
|---|---|
| Nesina® Tablet | 0.16 |
An SAE is an adverse event 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. 95% Confidence Interval was calculated using exact method. (NCT04980040)
Timeframe: From first dose of study drug up to 30 days post last dose of study drug (Up to 79.77 weeks)
| Intervention | percentage of participants (Number) |
|---|---|
| Nesina® Tablet | 1.18 |
Unexpected ADRs are unexpected AEs that are, in the investigator's opinion, of causal relationship to the study treatment. 95% Confidence Interval was calculated using exact method. (NCT04980040)
Timeframe: From first dose of study drug up to 30 days post last dose of study drug (Up to 79.77 weeks)
| Intervention | percentage of participants (Number) |
|---|---|
| Nesina® Tablet | 2.01 |
Participants were assessed for overall improvement and effectiveness assessments as per the following categories: 'Improved - signs and symptoms are significantly improved'; 'Unchanged - improvement in signs and symptoms is not significant or there is no change in signs and symptoms'. (NCT04980040)
Timeframe: Up to Week 26
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| Improved | Unchanged | Worsened | |
| Nesina® Tablet | 82.57 | 9.64 | 7.79 |
HbA1c are glycated haemoglobin or amount of glucose attached to haemoglobin. (NCT04980040)
Timeframe: Baseline (Before administration of alogliptin), 13 weeks (±2 weeks) and 26 weeks (±2 weeks) after administration
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| Before Administration | 13 weeks After Administration | 26 weeks After Administration | |
| Nesina® Tablet | 17.84 | 60.96 | 63.49 |
HbA1c are glycated haemoglobin or amount of glucose attached to haemoglobin. (NCT04980040)
Timeframe: Baseline (Before administration of alogliptin), 13 weeks (±2 weeks) and 26 weeks (±2 weeks) after administration
| Intervention | percentage of Hb1Ac (Mean) | ||
|---|---|---|---|
| Before Administration | 13 weeks (±2 weeks) After Administration | 26 weeks (±2 weeks) After Administration | |
| Nesina® Tablet | 8.05 | 6.96 | 6.87 |
(NCT04980040)
Timeframe: Baseline (Before administration of alogliptin), 13 weeks (±2 weeks) and 26 weeks (±2 weeks) after administration
| Intervention | g/dL (Mean) | ||
|---|---|---|---|
| Before Administration | 13 weeks (±2 weeks) After Administration | 26 weeks (±2 weeks) After Administration | |
| Nesina® Tablet | 166.22 | 136.84 | 133.09 |
An unexpected AE is an AE with a difference in nature, severity, specificity, or outcome, compared to the product licensure/safety notification of the drug. 95% Confidence Interval was calculated using exact method. (NCT04980040)
Timeframe: From first dose of study drug up to 30 days post last dose of study drug (Up to 79.77 weeks)
| Intervention | percentage of participants (Number) |
|---|---|
| Nesina® Tablet | 8.88 |
| Substance | Relationship Strength | Studies | Trials | Classes | Roles |
|---|---|---|---|---|---|
| aminolevulinic acid Aminolevulinic Acid: A compound produced from succinyl-CoA and GLYCINE as an intermediate in heme synthesis. It is used as a PHOTOCHEMOTHERAPY for actinic KERATOSIS.. 5-aminolevulinic acid : The simplest delta-amino acid in which the hydrogens at the gamma position are replaced by an oxo group. It is metabolised to protoporphyrin IX, a photoactive compound which accumulates in the skin. Used (in the form of the hydrochloride salt)in combination with blue light illumination for the treatment of minimally to moderately thick actinic keratosis of the face or scalp. | 2.6 | 1 | 0 | 4-oxo monocarboxylic acid; amino acid zwitterion; delta-amino acid | antineoplastic agent; dermatologic drug; Escherichia coli metabolite; human metabolite; mouse metabolite; photosensitizing agent; plant metabolite; prodrug; Saccharomyces cerevisiae metabolite |
| benzoic acid Benzoic Acid: A fungistatic compound that is widely used as a food preservative. It is conjugated to GLYCINE in the liver and excreted as hippuric acid.. benzoic acid : A compound comprising a benzene ring core carrying a carboxylic acid substituent.. aromatic carboxylic acid : Any carboxylic acid in which the carboxy group is directly bonded to an aromatic ring. | 2.15 | 1 | 0 | benzoic acids | algal metabolite; antimicrobial food preservative; drug allergen; EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor; EC 3.1.1.3 (triacylglycerol lipase) inhibitor; human xenobiotic metabolite; plant metabolite |
| coumarin 2H-chromen-2-one: coumarin derivative | 2.6 | 1 | 0 | coumarins | fluorescent dye; human metabolite; plant metabolite |
| salicylic acid Scalp: The outer covering of the calvaria. It is composed of several layers: SKIN; subcutaneous connective tissue; the occipitofrontal muscle which includes the tendinous galea aponeurotica; loose connective tissue; and the pericranium (the PERIOSTEUM of the SKULL). | 2.6 | 1 | 0 | monohydroxybenzoic acid | algal metabolite; antifungal agent; antiinfective agent; EC 1.11.1.11 (L-ascorbate peroxidase) inhibitor; keratolytic drug; plant hormone; plant metabolite |
| gallic acid gallate : A trihydroxybenzoate that is the conjugate base of gallic acid. | 3.27 | 1 | 0 | trihydroxybenzoic acid | antineoplastic agent; antioxidant; apoptosis inducer; astringent; cyclooxygenase 2 inhibitor; EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor; geroprotector; human xenobiotic metabolite; plant metabolite |
| dimethyl sulfoxide Dimethyl Sulfoxide: A highly polar organic liquid, that is used widely as a chemical solvent. Because of its ability to penetrate biological membranes, it is used as a vehicle for topical application of pharmaceuticals. It is also used to protect tissue during CRYOPRESERVATION. Dimethyl sulfoxide shows a range of pharmacological activity including analgesia and anti-inflammation.. dimethyl sulfoxide : A 2-carbon sulfoxide in which the sulfur atom has two methyl substituents. | 2.31 | 1 | 0 | sulfoxide; volatile organic compound | alkylating agent; antidote; Escherichia coli metabolite; geroprotector; MRI contrast agent; non-narcotic analgesic; polar aprotic solvent; radical scavenger |
| 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. | 2.6 | 1 | 0 | dithiolanes; heterocyclic fatty acid; thia fatty acid | fundamental metabolite; geroprotector |
| 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. | 7.28 | 6 | 4 | cyclitol; hexol | |
| naringenin [no description available] | 3.27 | 1 | 0 | 4'-hydroxyflavanones; trihydroxyflavanone | |
| 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. | 2.6 | 1 | 0 | pyridinemonocarboxylic acid | human metabolite; MALDI matrix material |
| thiamine thiamine(1+) : A primary alcohol that is 1,3-thiazol-3-ium substituted by (4-amino-2-methylpyrimidin-5-yl)methyl, methyl and 2-hydroxyethyl groups at positions 3, 4 and 5, respectively. | 2.6 | 1 | 0 | primary alcohol; vitamin B1 | Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| uracil 2,4-dihydroxypyrimidine: a urinary biomarker for bipolar disorder | 21.24 | 273 | 80 | pyrimidine nucleobase; pyrimidone | allergen; Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; prodrug; Saccharomyces cerevisiae metabolite |
| 1-(3-chlorophenyl)piperazine 1-(3-chlorophenyl)piperazine: supposed metabolite of TRAZODONE; RN given refers to parent cpd; structure. 1-(3-chlorophenyl)piperazine : A N-arylpiperazine that is piperazine carrying a 3-chlorophenyl substituent at position 1. It is a metabolite of the antidepressant drug trazodone. | 2.11 | 1 | 0 | monochlorobenzenes; N-arylpiperazine | drug metabolite; environmental contaminant; serotonergic agonist; xenobiotic |
| 3-aminobenzamide [no description available] | 2.6 | 1 | 0 | benzamides; substituted aniline | EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor |
| pleconaril WIN 63843: structure given in first source | 2.6 | 1 | 0 | ||
| 4-(2-aminoethyl)benzenesulfonylfluoride [no description available] | 2.6 | 1 | 0 | ||
| phenytoin [no description available] | 2.6 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant; drug allergen; sodium channel blocker; teratogenic agent |
| acetaminophen Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.. paracetamol : A member of the class of phenols that is 4-aminophenol in which one of the hydrogens attached to the amino group has been replaced by an acetyl group. | 2.17 | 1 | 0 | acetamides; phenols | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; cyclooxygenase 3 inhibitor; environmental contaminant; ferroptosis inducer; geroprotector; hepatotoxic agent; human blood serum metabolite; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| acetazolamide Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337) | 2.6 | 1 | 0 | monocarboxylic acid amide; sulfonamide; thiadiazoles | anticonvulsant; diuretic; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
| alprenolol Alprenolol: One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.. alprenolol : A secondary alcohol that is propan-2-ol substituted by a 2-allylphenoxy group at position 1 and an isopropylamino group at position 3. It is a beta-adrenergic antagonist used as a antihypertensive, anti-arrhythmia and a sympatholytic agent. | 2.6 | 1 | 0 | secondary alcohol; secondary amino compound | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent |
| amantadine amant: an antiviral compound consisting of an adamantane derivative chemically linked to a water-solube polyanioic matrix; structure in first source | 2.6 | 1 | 0 | adamantanes; primary aliphatic amine | analgesic; antiparkinson drug; antiviral drug; dopaminergic agent; NMDA receptor antagonist; non-narcotic analgesic |
| theophylline [no description available] | 2.11 | 1 | 0 | dimethylxanthine | adenosine receptor antagonist; anti-asthmatic drug; anti-inflammatory agent; bronchodilator agent; drug metabolite; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; fungal metabolite; human blood serum metabolite; immunomodulator; muscle relaxant; vasodilator agent |
| 2-aminothiazole 2-aminothiazole: RN given refers to parent cpd; structure. 1,3-thiazol-2-amine : A primary amino compound that is 1,3-thiazole substituted by an amino group at position 2. | 2.6 | 1 | 0 | 1,3-thiazoles; primary amino compound | |
| amodiaquine Amodiaquine: A 4-aminoquinoline compound with anti-inflammatory properties.. amodiaquine : A quinoline having a chloro group at the 7-position and an aryl amino group at the 4-position. | 2.6 | 1 | 0 | aminoquinoline; organochlorine compound; phenols; secondary amino compound; tertiary amino compound | anticoronaviral agent; antimalarial; drug allergen; EC 2.1.1.8 (histamine N-methyltransferase) inhibitor; non-steroidal anti-inflammatory drug; prodrug |
| 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. | 10.2 | 2 | 1 | benzoic 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 |
| baclofen [no description available] | 2.6 | 1 | 0 | amino acid zwitterion; gamma-amino acid; monocarboxylic acid; monochlorobenzenes; primary amino compound | central nervous system depressant; GABA agonist; muscle relaxant |
| benzamide benzamide : An aromatic amide that consists of benzene bearing a single carboxamido substituent. The parent of the class of benzamides. | 2.6 | 1 | 0 | benzamides | |
| camostat camostat : A benzoate ester resulting from the formal condensation of the carboxy group of 4-guanidinobenzoic acid with the hydroxy group of 2-(dimethylamino)-2-oxoethyl (4-hydroxyphenyl)acetate. It is a potent inhibitor of the human transmembrane protease serine 2 (TMPRSS2) and its mesylate salt is currently under investigation for its effectiveness in COVID-19 patients. | 2.6 | 1 | 0 | benzoate ester; carboxylic ester; diester; guanidines; tertiary carboxamide | anti-inflammatory agent; anticoronaviral agent; antifibrinolytic drug; antihypertensive agent; antineoplastic agent; antiviral agent; serine protease inhibitor |
| camphor, (+-)-isomer [no description available] | 2.6 | 1 | 0 | bornane monoterpenoid; cyclic monoterpene ketone | plant metabolite |
| candesartan candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension. | 2.6 | 1 | 0 | benzimidazolecarboxylic acid; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| cetylpyridinium Cetylpyridinium: Cationic bactericidal surfactant used as a topical antiseptic for skin, wounds, mucous membranes, instruments, etc.; and also as a component in mouthwash and lozenges. | 2.6 | 1 | 0 | pyridinium ion | |
| chloroxylenol chloroxylenol: topical antiseptic; RN given refers to parent cpd; structure. 4-chloro-3,5-dimethylphenol : A member of the class of phenols that is 3,5-xylenol which is substituted at position 4 by chlorine. It is bactericidal against most Gram-positive bacteria but less effective against Staphylococci and Gram-negative bacteria, and often inactive against Pseudomonas species. It is ineffective against bacterial spores. | 2.6 | 1 | 0 | monochlorobenzenes; phenols | antiseptic drug; disinfectant; molluscicide |
| chlorpromazine Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety. | 2.6 | 1 | 0 | organochlorine compound; phenothiazines; tertiary amine | anticoronaviral agent; antiemetic; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; phenothiazine antipsychotic drug |
| cimetidine Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach. | 8.44 | 1 | 1 | aliphatic sulfide; guanidines; imidazoles; nitrile | adjuvant; analgesic; anti-ulcer drug; H2-receptor antagonist; P450 inhibitor |
| ciprofibrate [no description available] | 2.6 | 1 | 0 | cyclopropanes; monocarboxylic acid; organochlorine compound | antilipemic drug |
| clomipramine Clomipramine: A tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.. clomipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(dimethylamino)propyl group. One of the more sedating tricyclic antidepressants, it is used as the hydrochloride salt for the treatment of depression as well as obsessive-compulsive disorder and phobias. | 2.6 | 1 | 0 | dibenzoazepine | anticoronaviral agent; antidepressant; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; serotonergic antagonist; serotonergic drug; serotonin uptake inhibitor |
| danthron danthron: structure. chrysazin : A dihydroxyanthraquinone that is anthracene-9,10-dione substituted by hydroxy groups at positions 1 and 8. | 2.6 | 1 | 0 | dihydroxyanthraquinone | apoptosis inducer; plant metabolite |
| deferiprone Deferiprone: A pyridone derivative and iron chelator that is used in the treatment of IRON OVERLOAD in patients with THALASSEMIA.. deferiprone : A member of the class of 4-pyridones that is pyridin-4(1H)-one substituted at positions 1 and 2 by methyl groups and at position 3 by a hydroxy group. A lipid-soluble iron-chelator used for treatment of thalassaemia. | 2.6 | 1 | 0 | 4-pyridones | iron chelator; protective agent |
| dipyridamole Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752). dipyridamole : A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots. | 2.6 | 1 | 0 | piperidines; pyrimidopyrimidine; tertiary amino compound; tetrol | adenosine phosphodiesterase inhibitor; EC 3.5.4.4 (adenosine deaminase) inhibitor; platelet aggregation inhibitor; vasodilator agent |
| disulfiram [no description available] | 2.6 | 1 | 0 | organic disulfide; organosulfur acaricide | angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor; EC 3.1.1.1 (carboxylesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 5.99.1.2 (DNA topoisomerase) inhibitor; ferroptosis inducer; fungicide; NF-kappaB inhibitor |
| valproic acid Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem. | 2.6 | 1 | 0 | branched-chain fatty acid; branched-chain saturated fatty acid | anticonvulsant; antimanic drug; EC 3.5.1.98 (histone deacetylase) inhibitor; GABA agent; neuroprotective agent; psychotropic drug; teratogenic agent |
| doxazosin Doxazosin: A prazosin-related compound that is a selective alpha-1-adrenergic blocker.. doxazosin : A member of the class of quinazolines that is quinazoline substituted by an amino group at position 4, methoxy groups at positions 6 and 7 and a piperazin-1-yl group at position 2 which in turn is substituted by a 2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl group at position 4. An antihypertensive agent, it is used in the treatment of high blood pressure. | 2.6 | 1 | 0 | aromatic amine; benzodioxine; monocarboxylic acid amide; N-acylpiperazine; N-arylpiperazine; quinazolines | alpha-adrenergic antagonist; antihyperplasia drug; antihypertensive agent; antineoplastic agent; vasodilator agent |
| ebselen ebselen : A benzoselenazole that is 1,2-benzoselenazol-3-one carrying an additional phenyl substituent at position 2. Acts as a mimic of glutathione peroxidase. | 2.6 | 1 | 0 | benzoselenazole | anti-inflammatory drug; antibacterial agent; anticoronaviral agent; antifungal agent; antineoplastic agent; antioxidant; apoptosis inducer; EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; EC 1.3.1.8 [acyl-CoA dehydrogenase (NADP(+))] inhibitor; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; EC 3.1.3.25 (inositol-phosphate phosphatase) inhibitor; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor; EC 3.5.4.1 (cytosine deaminase) inhibitor; EC 5.1.3.2 (UDP-glucose 4-epimerase) inhibitor; enzyme mimic; ferroptosis inhibitor; genotoxin; hepatoprotective agent; neuroprotective agent; radical scavenger |
| etidronate Etidronic Acid: A diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover.. etidronic acid : A 1,1-bis(phosphonic acid) that is (ethane-1,1-diyl)bis(phosphonic acid) having a hydroxy substituent at the 1-position. It inhibits the formation, growth, and dissolution of hydroxyapatite crystals by chemisorption to calcium phosphate surfaces. | 2.6 | 1 | 0 | 1,1-bis(phosphonic acid) | antineoplastic agent; bone density conservation agent; chelator |
| 2-hexyloxybenzamide 2-hexyloxybenzamide: structure | 2.6 | 1 | 0 | aromatic ether; benzamides | antifungal agent |
| brl 42810 [no description available] | 2.6 | 1 | 0 | 2-aminopurines; acetate ester | antiviral drug; prodrug |
| 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. | 2.31 | 1 | 0 | piperidines; tertiary amine | anti-allergic agent; H1-receptor antagonist |
| fluphenazine [no description available] | 2.6 | 1 | 0 | N-alkylpiperazine; organofluorine compound; phenothiazines | anticoronaviral agent; dopaminergic antagonist; phenothiazine antipsychotic drug |
| fluorouracil Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth. | 2.6 | 1 | 0 | nucleobase analogue; organofluorine compound | antimetabolite; antineoplastic agent; environmental contaminant; immunosuppressive agent; radiosensitizing agent; xenobiotic |
| gabexate Gabexate: A serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin. | 2.6 | 1 | 0 | benzoate ester | |
| gliclazide Gliclazide: An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion. | 8.59 | 1 | 1 | N-sulfonylurea | hypoglycemic agent; insulin secretagogue; radical scavenger |
| glimepiride glimepiride: structure given in first source | 8.98 | 2 | 1 | sulfonamide | |
| 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. | 5.1 | 3 | 3 | aromatic amide; monocarboxylic acid amide; N-sulfonylurea; pyrazines | EC 2.7.1.33 (pantothenate kinase) inhibitor; hypoglycemic agent; insulin secretagogue |
| glutaral Glutaral: One of the protein CROSS-LINKING REAGENTS that is used as a disinfectant for sterilization of heat-sensitive equipment and as a laboratory reagent, especially as a fixative.. glutaraldehyde : A dialdehyde comprised of pentane with aldehyde functions at C-1 and C-5. | 2.6 | 1 | 0 | dialdehyde | cross-linking reagent; disinfectant; fixative |
| 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. | 5.31 | 2 | 2 | monochlorobenzenes; 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 |
| fasudil fasudil: intracellular calcium antagonist; structure in first source. fasudil : An isoquinoline substituted by a (1,4-diazepan-1-yl)sulfonyl group at position 5. It is a Rho-kinase inhibitor and its hydrochloride hydrate form is approved for the treatment of cerebral vasospasm and cerebral ischemia. | 2.6 | 1 | 0 | isoquinolines; N-sulfonyldiazepane | antihypertensive agent; calcium channel blocker; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; geroprotector; neuroprotective agent; nootropic agent; vasodilator agent |
| haloperidol Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety. | 2.6 | 1 | 0 | aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol | antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist |
| miltefosine miltefosine: hexadecyl phosphocholine derivative of cisplatin; did not substantially activate HIV long terminal repeat; less toxic than cisplatin. miltefosine : A phospholipid that is the hexadecyl monoester of phosphocholine. | 2.6 | 1 | 0 | phosphocholines; phospholipid | anti-inflammatory agent; anticoronaviral agent; antifungal agent; antineoplastic agent; antiprotozoal drug; apoptosis inducer; immunomodulator; protein kinase inhibitor |
| hexylresorcinol [no description available] | 2.6 | 1 | 0 | resorcinols | |
| beta-thujaplicin beta-thujaplicin: structure. beta-thujaplicin : A monoterpenoid that is cyclohepta-2,4,6-trien-1-one substituted by a hydroxy group at position 2 and an isopropyl group at position 4. Isolated from Thuja plicata and Chamaecyparis obtusa, it exhibits antimicrobial activities. | 2.6 | 1 | 0 | cyclic ketone; enol; monoterpenoid | antibacterial agent; antifungal agent; antineoplastic agent; antiplasmodial drug; plant metabolite |
| hycanthone Hycanthone: Potentially toxic, but effective antischistosomal agent, it is a metabolite of LUCANTHONE.. hycanthone : A thioxanthen-9-one compound having a hydroxymethyl substituent at the 1-position and a 2-[(diethylamino)ethyl]amino substituent at the 4-position. It was formerly used (particularly as the monomethanesulfonic acid salt) as a schistosomicide for individual or mass treatement of infection with Schistosoma haematobium and S. mansoni, but due to its toxicity and concern about possible carcinogenicity, it has been replaced by other drugs such as praziquantel. | 2.6 | 1 | 0 | thioxanthenes | mutagen; schistosomicide drug |
| 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. | 2.6 | 1 | 0 | benzothiadiazine; organochlorine compound; sulfonamide | antihypertensive agent; diuretic; environmental contaminant; xenobiotic |
| hydroxyurea [no description available] | 2.6 | 1 | 0 | one-carbon compound; ureas | antimetabolite; antimitotic; antineoplastic agent; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; genotoxin; immunomodulator; radical scavenger; teratogenic agent |
| ibuprofen Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine | 2.6 | 1 | 0 | monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; environmental contaminant; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug; radical scavenger; xenobiotic |
| indomethacin Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis. | 2.6 | 1 | 0 | aromatic ether; indole-3-acetic acids; monochlorobenzenes; N-acylindole | analgesic; drug metabolite; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; gout suppressant; non-steroidal anti-inflammatory drug; xenobiotic metabolite; xenobiotic |
| 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. | 2.6 | 1 | 0 | azaspiro compound; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| itraconazole [no description available] | 2.6 | 1 | 0 | piperazines | |
| kojic acid [no description available] | 2.6 | 1 | 0 | 4-pyranones; enol; primary alcohol | Aspergillus metabolite; EC 1.10.3.1 (catechol oxidase) inhibitor; EC 1.10.3.2 (laccase) inhibitor; EC 1.13.11.24 (quercetin 2,3-dioxygenase) inhibitor; EC 1.14.18.1 (tyrosinase) inhibitor; EC 1.4.3.3 (D-amino-acid oxidase) inhibitor; NF-kappaB inhibitor; skin lightening agent |
| 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. | 8.48 | 1 | 1 | benzimidazoles; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor |
| lapachol lapachol : A hydroxy-1,4-naphthoquinone that is 1,4-naphthoquinone substituted by hydroxy and 3-methylbut-2-en-1-yl groups at positions 2 and 3, respectively. It is a natural compound that exhibits antibacterial and anticancer properties, first isolated in 1882 from the bark of Tabebuia avellanedae. | 2.6 | 1 | 0 | ||
| loperamide Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.. loperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease. | 2.6 | 1 | 0 | monocarboxylic acid amide; monochlorobenzenes; piperidines; tertiary alcohol | anticoronaviral agent; antidiarrhoeal drug; mu-opioid receptor agonist |
| loratadine Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders. | 2.6 | 1 | 0 | benzocycloheptapyridine; ethyl ester; N-acylpiperidine; organochlorine compound; tertiary carboxamide | anti-allergic agent; cholinergic antagonist; geroprotector; H1-receptor antagonist |
| 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 | 2.6 | 1 | 0 | biphenylyltetrazole; imidazoles | angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor antagonist |
| 4-(dimethylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)benzamide 4-(dimethylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)benzamide: structure in first source. 4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide : A benzamide resulting from the formal condensation of the carboxy group of 4-(dimethylamino)benzoic acid with the amino group of 7-amino-N-hydroxyheptanamide. It is a potent inhibitor of histone deacetylases and induces cell cycle arrest and apoptosis in several human cancer cell lines. | 2.6 | 1 | 0 | benzamides; hydroxamic acid; secondary carboxamide; tertiary amino compound | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor |
| mafenide Mafenide: A sulfonamide that inhibits the enzyme CARBONIC ANHYDRASE and is used as a topical anti-bacterial agent, especially in burn therapy. | 2.6 | 1 | 0 | aromatic amine | |
| 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. | 13.84 | 32 | 17 | guanidines | environmental contaminant; geroprotector; hypoglycemic agent; xenobiotic |
| methazolamide Methazolamide: A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma. | 2.6 | 1 | 0 | sulfonamide; thiadiazoles | |
| methocarbamol Methocarbamol: A centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1206). methocarbamol : A racemate comprising equimolar amounts of (R)- and (S)-methocarbamol. A centrally acting skeletal muscle relaxant, it is used as an adjunct in the short-term symptomatic treatment of painful muscle spasm. The (R)-enantiomer is more active than the (S)-enantiomer.. 2-hydroxy-3-(2-methoxyphenoxy)propyl carbamate : A carbamate ester that is glycerol in which one of the primary alcohol groups has been converted to its 2-methoxyphenyl ether while the other has been converted to the corresponding carbamate ester. | 2.6 | 1 | 0 | aromatic ether; carbamate ester; secondary alcohol | |
| mitoxantrone Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8. | 2.6 | 1 | 0 | dihydroxyanthraquinone | analgesic; antineoplastic agent |
| entinostat [no description available] | 2.6 | 1 | 0 | benzamides; carbamate ester; primary amino compound; pyridines; substituted aniline | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor |
| ethylmaleimide Ethylmaleimide: A sulfhydryl reagent that is widely used in experimental biochemical studies. | 2.6 | 1 | 0 | maleimides | anticoronaviral agent; EC 1.3.1.8 [acyl-CoA dehydrogenase (NADP(+))] inhibitor; EC 2.1.1.122 [(S)-tetrahydroprotoberberine N-methyltransferase] inhibitor; EC 2.7.1.1 (hexokinase) inhibitor |
| nabumetone Nabumetone: A butanone non-steroidal anti-inflammatory drug and cyclooxygenase-2 (COX2) inhibitor that is used in the management of pain associated with OSTEOARTHRITIS and RHEUMATOID ARTHRITIS.. nabumetone : A methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs. | 2.6 | 1 | 0 | methoxynaphthalene; methyl ketone | cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug |
| nafamostat nafamostat: inhibitor of trypsin, plasmin, pancreatic kallikrein, plasma kallikrein & thrombin; strongly inhibits esterolytic activities of C1r & C1 esterase complement-mediated hemolysis; antineoplastic | 2.6 | 1 | 0 | benzoic acids; guanidines | |
| nevirapine Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection. | 2.6 | 1 | 0 | cyclopropanes; dipyridodiazepine | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| 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. | 2.6 | 1 | 0 | aromatic ether; benzimidazoles; pyridines; sulfoxide | |
| osalmide osalmide: structure | 2.6 | 1 | 0 | organic molecular entity | |
| oxethazaine [no description available] | 2.6 | 1 | 0 | amino acid amide | |
| palmidrol palmidrol: a cannabinoid receptor-inactive eCB-related molecule used as prophylactic in helping to prevent respiratory viral infection. palmitoyl ethanolamide : An N-(long-chain-acyl)ethanolamine that is the ethanolamide of palmitic (hexadecanoic) acid. | 2.6 | 1 | 0 | endocannabinoid; N-(long-chain-acyl)ethanolamine; N-(saturated fatty acyl)ethanolamine | anti-inflammatory drug; anticonvulsant; antihypertensive agent; neuroprotective agent |
| papaverine Papaverine: An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.. papaverine : A benzylisoquinoline alkaloid that is isoquinoline substituted by methoxy groups at positions 6 and 7 and a 3,4-dimethoxybenzyl group at position 1. It has been isolated from Papaver somniferum. | 2.6 | 1 | 0 | benzylisoquinoline alkaloid; dimethoxybenzene; isoquinolines | antispasmodic drug; vasodilator agent |
| pd 98059 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one: inhibits MAP kinase kinase (MEK) activity, p42 MAPK and p44 MAPK; structure in first source. 2-(2-amino-3-methoxyphenyl)chromen-4-one : A member of the class of monomethoxyflavones that is 3'-methoxyflavone bearing an additional amino substituent at position 2'. | 2.05 | 1 | 0 | aromatic amine; monomethoxyflavone | EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector |
| pentoxifylline [no description available] | 2.6 | 1 | 0 | oxopurine | |
| perhexiline Perhexiline: 2-(2,2-Dicyclohexylethyl)piperidine. Coronary vasodilator used especially for angina of effort. It may cause neuropathy and hepatitis. | 2.6 | 1 | 0 | piperidines | cardiovascular drug |
| phenazopyridine Phenazopyridine: A local anesthetic that has been used in urinary tract disorders. Its use is limited by problems with toxicity (primarily blood disorders) and potential carcinogenicity.. phenazopyridine : A diaminopyridine that is 2,6-diaminopyridine substituted at position 3 by a phenylazo group. A local anesthetic that has topical analgesic effect on mucosa lining of the urinary tract. Its use is limited by problems with toxicity (primarily blood disorders) and potential carcinogenicity. | 2.6 | 1 | 0 | diaminopyridine; monoazo compound | anticoronaviral agent; carcinogenic agent; local anaesthetic; non-narcotic analgesic |
| 4-phenylbutyric acid 4-phenylbutyric acid: RN refers to the parent cpd. 4-phenylbutyric acid : A monocarboxylic acid the structure of which is that of butyric acid substituted with a phenyl group at C-4. It is a histone deacetylase inhibitor that displays anticancer activity. It inhibits cell proliferation, invasion and migration and induces apoptosis in glioma cells. It also inhibits protein isoprenylation, depletes plasma glutamine, increases production of foetal haemoglobin through transcriptional activation of the gamma-globin gene and affects hPPARgamma activation. | 2.6 | 1 | 0 | monocarboxylic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor; prodrug |
| phenylmethylsulfonyl fluoride Phenylmethylsulfonyl Fluoride: An enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex.. phenylmethanesulfonyl fluoride : An acyl fluoride with phenylmethanesulfonyl as the acyl group. | 2.6 | 1 | 0 | acyl fluoride | serine proteinase inhibitor |
| pimobendan pimobendan: produces arterial & venous dilatation in dogs; structure given in first source | 2.6 | 1 | 0 | benzimidazoles; pyridazinone | cardiotonic drug; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent |
| 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. | 13.32 | 34 | 15 | aromatic 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 |
| pj-34 PJ34 : A member of the class of phenanthridines that is 5,6-dihydrophenanthridine substituted at positions 2 and 6 by (N,N-dimethylglycyl)amino and oxo groups, respectively. It is a potent inhibitor of poly(ADP-ribose) polymerases PARP1 and PARP2 (IC50 of 110 nM and 86 nM, respectively) and exhibits anti-cancer, cardioprotective and neuroprotective properties. | 2.6 | 1 | 0 | phenanthridines; secondary carboxamide; tertiary amino compound | angiogenesis inhibitor; anti-inflammatory agent; antiatherosclerotic agent; antineoplastic agent; apoptosis inducer; cardioprotective agent; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor; neuroprotective agent |
| praziquantel azinox: Russian drug | 2.6 | 1 | 0 | isoquinolines | |
| probenecid Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups. | 2.6 | 1 | 0 | benzoic acids; sulfonamide | uricosuric drug |
| probucol Probucol: A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993).. probucol : A dithioketal that is propane-2,2-dithiol in which the hydrogens attached to both sulfur atoms are replaced by 3,5-di-tert-butyl-4-hydroxyphenyl groups. An anticholesteremic drug with antioxidant and anti-inflammatory properties, it is used to treat high levels of cholesterol in blood. | 2.6 | 1 | 0 | dithioketal; polyphenol | anti-inflammatory drug; anticholesteremic drug; antilipemic drug; antioxidant; cardiovascular drug |
| promazine Promazine: A phenothiazine with actions similar to CHLORPROMAZINE but with less antipsychotic activity. It is primarily used in short-term treatment of disturbed behavior and as an antiemetic.. promazine : A phenothiazine deriative in which the phenothiazine tricycle has a 3-(dimethylaminopropyl) group at the N-10 position. | 2.6 | 1 | 0 | phenothiazines; tertiary amine | antiemetic; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; muscarinic antagonist; phenothiazine antipsychotic drug; serotonergic antagonist |
| promethazine Promethazine: A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.. promethazine : A tertiary amine that is a substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropan-2-amine moiety. | 2.6 | 1 | 0 | phenothiazines; tertiary amine | anti-allergic agent; anticoronaviral agent; antiemetic; antipruritic drug; H1-receptor antagonist; local anaesthetic; sedative |
| propranolol Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3. | 2.6 | 1 | 0 | naphthalenes; propanolamine; secondary amine | anti-arrhythmia drug; antihypertensive agent; anxiolytic drug; beta-adrenergic antagonist; environmental contaminant; human blood serum metabolite; vasodilator agent; xenobiotic |
| rimantadine Rimantadine: An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. | 2.6 | 1 | 0 | alkylamine | |
| rolipram [no description available] | 2.6 | 1 | 0 | pyrrolidin-2-ones | antidepressant; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor |
| scriptaid scriptide: provokes translocation of GLUT4 to increase glucose uptake; structure in first source | 2.6 | 1 | 0 | isoquinolines | |
| sebacic acid sebacic acid : An alpha,omega-dicarboxylic acid that is the 1,8-dicarboxy derivative of octane. | 2.6 | 1 | 0 | alpha,omega-dicarboxylic acid; dicarboxylic fatty acid | human metabolite; plant metabolite |
| fenofibrate [no description available] | 2.6 | 1 | 0 | benzochromenone; delta-lactone; naphtho-alpha-pyrone | platelet aggregation inhibitor; Sir2 inhibitor |
| imatinib [no description available] | 2.6 | 1 | 0 | aromatic amine; benzamides; N-methylpiperazine; pyridines; pyrimidines | antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor |
| suprofen Suprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It inhibits prostaglandin synthesis and has been proposed as an anti-arthritic.. suprofen : An aromatic ketone that is thiophene substituted at C-2 by a 4-(1-carboxyethyl)benzoyl group. | 2.6 | 1 | 0 | aromatic ketone; monocarboxylic acid; thiophenes | antirheumatic drug; drug allergen; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; peripheral nervous system drug |
| 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. | 2.31 | 1 | 0 | diarylmethane | |
| thalidomide Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group. | 2.6 | 1 | 0 | phthalimides; piperidones | |
| ticlopidine Ticlopidine: An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.. ticlopidine : 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. | 2.6 | 1 | 0 | monochlorobenzenes; thienopyridine | anticoagulant; fibrin modulating drug; hematologic agent; P2Y12 receptor antagonist; platelet aggregation inhibitor |
| triamterene Triamterene: A pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.. triamterene : Pteridine substituted at positions 2, 4 and 7 with amino groups and at position 6 with a phenyl group. A sodium channel blocker, it is used as a diuretic in the treatment of hypertension and oedema. | 2.6 | 1 | 0 | pteridines | diuretic; sodium channel blocker |
| trifluoperazine [no description available] | 2.6 | 1 | 0 | N-alkylpiperazine; N-methylpiperazine; organofluorine compound; phenothiazines | antiemetic; calmodulin antagonist; dopaminergic antagonist; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor; phenothiazine antipsychotic drug |
| triflupromazine Triflupromazine: A phenothiazine used as an antipsychotic agent and as an antiemetic.. triflupromazine : A member of the class of phenothiazines that is 10H-phenothiazine having a trifluoromethyl subsitituent at the 2-position and a 3-(dimethylamino)propyl group at the N-10 position. | 2.6 | 1 | 0 | organofluorine compound; phenothiazines; tertiary amine | anticoronaviral agent; antiemetic; dopaminergic antagonist; first generation antipsychotic |
| 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. | 2.6 | 1 | 0 | alkaloid; iminium betaine | food component; human urinary metabolite; plant metabolite |
| trimethobenzamide trimethobenzamide: major descriptor (64-84); on-line search BENZAMIDES (64-84); Index Medicus search TRIMETHOBENZAMIDE (64-84); RN given refers to parent cpd. trimethobenzamide : The amide obtained by formal condensation of 3,4,5-trihydroxybenzoic acid with 4-[2-(N,N-dimethylamino)ethoxy]benzylamine. It is used to prevent nausea and vomitting in humans. | 2.6 | 1 | 0 | benzamides; tertiary amino compound | antiemetic |
| trimethoprim Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge. | 2.6 | 1 | 0 | aminopyrimidine; methoxybenzenes | antibacterial drug; diuretic; drug allergen; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; environmental contaminant; xenobiotic |
| tyrphostin a9 [no description available] | 2.6 | 1 | 0 | alkylbenzene | geroprotector |
| delavirdine Delavirdine: A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.. delavirdine : The amide resulting from the formal condensation of 5-[(methylsulfonyl)amino]-1H-indole-2-carboxylic acid and 4-amino group of 1-[3-(isopropylamino)pyridin-2-yl]piperazine, delavirdine is a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection. | 2.6 | 1 | 0 | aminopyridine; indolecarboxamide; N-acylpiperazine; sulfonamide | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| vesnarinone [no description available] | 2.6 | 1 | 0 | organic molecular entity | |
| idoxuridine [no description available] | 2.6 | 1 | 0 | organoiodine compound; pyrimidine 2'-deoxyribonucleoside | antiviral drug; DNA synthesis inhibitor |
| 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. | 2.31 | 1 | 0 | nitrosamine | carcinogenic 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. | 3.18 | 1 | 0 | guanidines | |
| 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. | 2.08 | 1 | 0 | L-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 |
| chloramphenicol Amphenicol: Chloramphenicol and its derivatives. | 2.6 | 1 | 0 | C-nitro compound; carboxamide; diol; organochlorine compound | antibacterial drug; antimicrobial agent; Escherichia coli metabolite; geroprotector; Mycoplasma genitalium metabolite; protein synthesis inhibitor |
| lysine Lysine: An essential amino acid. It is often added to animal feed.. lysine : A diamino acid that is caproic (hexanoic) acid bearing two amino substituents at positions 2 and 6.. L-lysine : An L-alpha-amino acid; the L-isomer of lysine. | 2.6 | 1 | 0 | aspartate family amino acid; L-alpha-amino acid zwitterion; L-alpha-amino acid; lysine; organic molecular entity; proteinogenic amino acid | algal metabolite; anticonvulsant; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; plant metabolite; Saccharomyces cerevisiae metabolite |
| phenylethyl alcohol Phenylethyl Alcohol: An antimicrobial, antiseptic, and disinfectant that is used also as an aromatic essence and preservative in pharmaceutics and perfumery.. 2-phenylethanol : A primary alcohol that is ethanol substituted by a phenyl group at position 2. | 2.6 | 1 | 0 | benzenes; primary alcohol | Aspergillus metabolite; fragrance; plant growth retardant; plant metabolite; Saccharomyces cerevisiae metabolite |
| zoxazolamine Zoxazolamine: A uricosuric and muscle relaxant. Zoxazolamine acts centrally as a muscle relaxant, but the mechanism of its action is not understood. | 2.6 | 1 | 0 | benzoxazole | |
| cycloheximide Cycloheximide: Antibiotic substance isolated from streptomycin-producing strains of Streptomyces griseus. It acts by inhibiting elongation during protein synthesis.. cycloheximide : A dicarboximide that is 4-(2-hydroxyethyl)piperidine-2,6-dione in which one of the hydrogens attached to the carbon bearing the hydroxy group is replaced by a 3,5-dimethyl-2-oxocyclohexyl group. It is an antibiotic produced by the bacterium Streptomyces griseus. | 2.6 | 1 | 0 | antibiotic fungicide; cyclic ketone; dicarboximide; piperidine antibiotic; piperidones; secondary alcohol | anticoronaviral agent; bacterial metabolite; ferroptosis inhibitor; neuroprotective agent; protein synthesis inhibitor |
| ficusin Ficusin: A naturally occurring furocoumarin, found in PSORALEA. After photoactivation with UV radiation, it binds DNA via single and double-stranded cross-linking.. psoralen : The simplest member of the class of psoralens that is 7H-furo[3,2-g]chromene having a keto group at position 7. It has been found in plants like Psoralea corylifolia and Ficus salicifolia. | 2.6 | 1 | 0 | psoralens | plant metabolite |
| tubercidin Tubercidin: An antibiotic purine ribonucleoside that readily substitutes for adenosine in the biological system, but its incorporation into DNA and RNA has an inhibitory effect on the metabolism of these nucleic acids.. tubercidin : An N-glycosylpyrrolopyrimidine that is adenosine in which the in the 5-membered ring that is not attached to the ribose moiety is replaced by a carbon. Tubercidin is produced in the culture broth of Streptomyces tubericidus. | 2.6 | 1 | 0 | antibiotic antifungal agent; N-glycosylpyrrolopyrimidine; ribonucleoside | antimetabolite; antineoplastic agent; bacterial metabolite |
| mannitol [no description available] | 2.15 | 1 | 0 | mannitol | allergen; antiglaucoma drug; compatible osmolytes; Escherichia coli metabolite; food anticaking agent; food bulking agent; food humectant; food stabiliser; food thickening agent; hapten; metabolite; osmotic diuretic; sweetening agent |
| trifluridine Trifluridine: An antiviral derivative of THYMIDINE used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to HERPES SIMPLEX virus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p557). trifluridine : A pyrimidine 2'-deoxyribonucleoside compound having 5-trifluoromethyluracil as the nucleobase. An antiviral drug used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis. | 2.6 | 1 | 0 | nucleoside analogue; organofluorine compound; pyrimidine 2'-deoxyribonucleoside | antimetabolite; antineoplastic agent; antiviral drug; EC 2.1.1.45 (thymidylate synthase) inhibitor |
| acetonitrile acetonitrile: RN given refers to unlabeled cpd. acetonitrile : A nitrile that is hydrogen cyanide in which the hydrogen has been replaced by a methyl group. | 2.17 | 1 | 0 | aliphatic nitrile; volatile organic compound | EC 3.5.1.4 (amidase) inhibitor; NMR chemical shift reference compound; polar aprotic solvent |
| 9,10-anthraquinone 9,10-anthraquinone : An anthraquinone that is anthracene in which positions 9 and 10 have been oxidised to carbonyls. | 2.6 | 1 | 0 | anthraquinone | |
| salicylanilide salicylanilide: RN given refers to parent cpd. salicylanilide : An amide of salicylic acid and of aniline; it is therefore both a salicylamide and an anilide. | 2.6 | 1 | 0 | benzanilide fungicide; salicylamides; salicylanilides | |
| gramine gramine : An aminoalkylindole that is indole carrying a dimethylaminomethyl substituent at postion 3. | 2.6 | 1 | 0 | aminoalkylindole; indole alkaloid; tertiary amino compound | antibacterial agent; antiviral agent; plant metabolite; serotonergic antagonist |
| aminacrine Aminacrine: A highly fluorescent anti-infective dye used clinically as a topical antiseptic and experimentally as a mutagen, due to its interaction with DNA. It is also used as an intracellular pH indicator.. 9-aminoacridine : An aminoacridine that is acridine in which the hydrogen at position 9 is replaced by an amino group. A fluorescent dyd and topical antiseptic agent, it is used (usually as the hydrochloride salt) in eye drops for the treatment of superficial eye infections. | 2.6 | 1 | 0 | aminoacridines; primary amino compound | acid-base indicator; antiinfective agent; antiseptic drug; fluorescent dye; MALDI matrix material; mutagen |
| methyl gallate methyl gallate: has both immunosuppressive and phytogenic antineoplastic activities; isolated from Acer saccharinum. methyl 3,4,5-trihydroxybenzoate : A gallate ester obtained by the formal condensation of gallic acid with methanol. It exhibits anti-oxidant, anti-tumor, anti-microbial and anti-inflammatory properties. | 2.6 | 1 | 0 | gallate ester | anti-inflammatory agent; antioxidant; plant metabolite |
| monobenzone monobenzone: structure. monobenzone : The monobenzyl ether of hydroquinone. It is used as a topical drug for medical depigmentation. | 2.6 | 1 | 0 | benzyl ether | allergen; dermatologic drug; melanin synthesis inhibitor |
| 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. | 2.06 | 1 | 0 | alkylamine | |
| thiophenes Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring. | 3.51 | 1 | 1 | mancude organic heteromonocyclic parent; monocyclic heteroarene; thiophenes; volatile organic compound | non-polar solvent |
| 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. | 3.18 | 1 | 0 | hexosamine; secondary amino compound | |
| ditiocarb Ditiocarb: A chelating agent that has been used to mobilize toxic metals from the tissues of humans and experimental animals. It is the main metabolite of DISULFIRAM.. diethyldithiocarbamic acid : A member of the class of dithiocarbamic acids that is diethylcarbamic acid in which both of the oxygens are replaced by sulfur. | 2.6 | 1 | 0 | dithiocarbamic acids | chelator; copper chelator |
| catechin Catechin: An antioxidant flavonoid, occurring especially in woody plants as both (+)-catechin and (-)-epicatechin (cis) forms.. catechin : Members of the class of hydroxyflavan that have a flavan-3-ol skeleton and its substituted derivatives.. rac-catechin : A racemate comprising equimolar amounts of (+)- and (-)-catechin. (+)-catechin : The (+)-enantiomer of catechin and a polyphenolic antioxidant plant metabolite. | 2.6 | 1 | 0 | catechin | antioxidant; plant metabolite |
| 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. | 8.05 | 14 | 0 | azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; quinazolines | |
| adamantane Adamantane: A tricyclo bridged hydrocarbon. | 12.6 | 48 | 2 | adamantanes; polycyclic alkane | |
| 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. | 10.94 | 20 | 3 | diazine; pyrazines | Daphnia magna metabolite |
| azacitidine Azacitidine: A pyrimidine analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent.. 5-azacytidine : An N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-ribofuranosyl residue via an N-glycosidic linkage. An antineoplastic agent, it is used in the treatment of myeloid leukaemia. | 2.6 | 1 | 0 | N-glycosyl-1,3,5-triazine; nucleoside analogue | antineoplastic agent |
| lucanthone Lucanthone: One of the SCHISTOSOMICIDES, it has been replaced largely by HYCANTHONE and more recently PRAZIQUANTEL. (From Martindale The Extrapharmacopoeia, 30th ed., p46). lucanthone : A thioxanthen-9-one compound having a methyl substituent at the 1-position and a 2-[(diethylamino)ethyl]amino substituent at the 4-position. Formerly used for the treatment of schistosomiasis. It is a prodrug, being metabolised to hycanthone. | 2.6 | 1 | 0 | thioxanthenes | adjuvant; antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; mutagen; photosensitizing agent; prodrug; schistosomicide drug |
| cepharanthine cepharanthine: isoquinoline alkaloid from tubers of STEPHANIA; stimulates recovery of immunologic function in lymphatic system after administration of antineoplastic agents or x-irradiation. cepharanthine : A bisbenzylisoquinoline alkaloid from tubers of Stephania; stimulates recovery of immunologic function in lymphatic system after administration of antineoplastic agents or x-irradiation. | 2.6 | 1 | 0 | bisbenzylisoquinoline alkaloid; isoquinolines | |
| aloe emodin aloe emodin: structure distinct from emodin; this does not mean emodin from aloe. Aloe emodin : A dihydroxyanthraquinone that is chrysazin carrying a hydroxymethyl group at position 3. It has been isolated from plant species of the genus Aloe. | 2.6 | 1 | 0 | aromatic primary alcohol; dihydroxyanthraquinone | antineoplastic agent; plant metabolite |
| chrysophanic acid chrysophanic acid: RN given refers to parent cpd; structure in Merck, 9th ed, #2260. chrysophanol : A trihydroxyanthraquinone that is chrysazin with a methyl substituent at C-3. It has been isolated from Aloe vera and exhibits antiviral and anti-inflammatory activity. | 2.6 | 1 | 0 | dihydroxyanthraquinone | anti-inflammatory agent; antiviral agent; plant metabolite |
| emetine Emetine: The principal alkaloid of ipecac, from the ground roots of Uragoga (or Cephaelis) ipecacuanha or U. acuminata, of the Rubiaceae. It is used as an amebicide in many different preparations and may cause serious cardiac, hepatic, or renal damage and violent diarrhea and vomiting. Emetine inhibits protein synthesis in EUKARYOTIC CELLS but not PROKARYOTIC CELLS.. emetine : A pyridoisoquinoline comprising emetam having methoxy substituents at the 6'-, 7'-, 10- and 11-positions. It is an antiprotozoal agent and emetic. It inhibits SARS-CoV2, Zika and Ebola virus replication and displays antimalarial, antineoplastic and antiamoebic properties. | 2.6 | 1 | 0 | isoquinoline alkaloid; pyridoisoquinoline | antiamoebic agent; anticoronaviral agent; antiinfective agent; antimalarial; antineoplastic agent; antiprotozoal drug; antiviral agent; autophagy inhibitor; emetic; expectorant; plant metabolite; protein synthesis inhibitor |
| osthol osthol: from Cnidium monnieri and Angelica pubescens (both Apiaceae); structure given in first source | 2.6 | 1 | 0 | botanical anti-fungal agent; coumarins | metabolite |
| flavanone flavanone: RN given refers to cpd with unspecified isomeric designation; structure in first source. flavanone : The simplest member of the class of flavanones that consists of flavan bearing an oxo substituent at position 4. | 2.6 | 1 | 0 | flavanones | |
| phloretic acid phloretic acid: structure. N-hydroxysuccinimide ester : An ester of N-hydroxysuccinimide.. phloretic acid : A hydroxy monocarboxylic acid consisting of propionic acid having a 4-hydroxyphenyl group at the 3-position. | 2.6 | 1 | 0 | hydroxy monocarboxylic acid | plant metabolite |
| thiazolidines Thiazolidines: Reduced (protonated) form of THIAZOLES. They can be oxidized to THIAZOLIDINEDIONES. | 4.14 | 4 | 0 | thiazolidine | |
| oleanolic acid [no description available] | 2.6 | 1 | 0 | hydroxy monocarboxylic acid; pentacyclic triterpenoid | plant metabolite |
| angelicin angelicin: used as tranquillizer; sedative; or anticonvulsant; structure | 2.6 | 1 | 0 | furanocoumarin | |
| flavone flavone: RN given refers to unlabeled cpd; structure given in first source. flavone : The simplest member of the class of flavones that consists of 4H-chromen-4-one bearing a phenyl substituent at position 2. | 3.27 | 1 | 0 | flavones | metabolite; nematicide |
| diperodon diperodon: RN given refers to parent cpd; structure given in first source | 2.6 | 1 | 0 | carbamate ester | |
| eosine yellowish-(ys) Eosine Yellowish-(YS): A versatile red dye used in cosmetics, pharmaceuticals, textiles, etc., and as tissue stain, vital stain, and counterstain with HEMATOXYLIN. It is also used in special culture media.. eosin YS dye : An organic sodium salt that is 2',4',5',7'-tetrabromofluorescein in which the carboxy group and the phenolic hydroxy group have been deprotonated and the resulting charge is neutralised by two sodium ions. | 2.6 | 1 | 0 | organic sodium salt; organobromine compound | fluorochrome; histological dye |
| megestrol acetate [no description available] | 2.6 | 1 | 0 | 20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; steroid ester | antineoplastic agent; appetite enhancer; contraceptive drug; progestin; synthetic oral contraceptive |
| acetylcysteine N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine. | 2.6 | 1 | 0 | acetylcysteine; 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. | 3.19 | 1 | 0 | delta-lactam; piperidones | EC 1.2.1.88 (L-glutamate gamma-semialdehyde dehydrogenase) inhibitor |
| hydroxychloroquine sulfate [no description available] | 2.6 | 1 | 0 | ||
| ethambutol Ethambutol: An antitubercular agent that inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect. (From Smith and Reynard, Textbook of Pharmacology, 1992, p863). ethambutol : An ethylenediamine derivative that is ethane-1,2-diamine in which one hydrogen attached to each of the nitrogens is sutstituted by a 1-hydroxybutan-2-yl group (S,S-configuration). It is a bacteriostatic antimycobacterial drug, effective against Mycobacterium tuberculosis and some other mycobacteria. It is used (as the dihydrochloride salt) in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol is used alone. | 2.6 | 1 | 0 | ethanolamines; ethylenediamine derivative | antitubercular agent; environmental contaminant; xenobiotic |
| metformin hydrochloride metformin hydrochloride : A hydrochloride resulting from the reaction of metformin with one molar equivalent of hydrogen chloride. | 2.6 | 1 | 0 | hydrochloride | environmental contaminant; hypoglycemic agent; xenobiotic |
| sodium hydroxide Sodium Hydroxide: A highly caustic substance that is used to neutralize acids and make sodium salts. (From Merck Index, 11th ed) | 2.13 | 1 | 0 | alkali metal hydroxide | |
| antimycin a [no description available] | 2.6 | 1 | 0 | benzamides; formamides; macrodiolide; phenols | antifungal agent; mitochondrial respiratory-chain inhibitor; piscicide |
| 5,5'-dimethyl-2,2'-bipyridyl 5,5'-dimethyl-2,2'-bipyridyl: structure in first source | 2.6 | 1 | 0 | bipyridines | |
| dichlorobenzyl alcohol 2,4-dichlorobenzyl alcohol : A member of the class of benzyl alcohols that is benzyl alcohol in which the hydrogens at positions 2 and 4 are replaced by chlorines. | 2.6 | 1 | 0 | benzyl alcohols; dichlorobenzene | antiseptic drug |
| stavudine Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase | 2.6 | 1 | 0 | dihydrofuran; nucleoside analogue; organic molecular entity | antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| dideoxyadenosine Dideoxyadenosine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is an inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal side effect is nephrotoxicity. In vivo, dideoxyadenosine is rapidly metabolized to DIDANOSINE (ddI) by enzymatic deamination; ddI is then converted to dideoxyinosine monophosphate and ultimately to dideoxyadenosine triphosphate, the putative active metabolite. | 2.6 | 1 | 0 | adenosines; purine 2',3'-dideoxyribonucleoside | EC 3.5.4.4 (adenosine deaminase) inhibitor; EC 4.6.1.1 (adenylate cyclase) inhibitor |
| fructosamine Fructosamine: An amino sugar formed when glucose non-enzymatically reacts with the N-terminal amino group of proteins. The fructose moiety is derived from glucose by the classical Amadori rearrangement. | 3.43 | 1 | 1 | ||
| vidarabine adenine arabinoside : A purine nucleoside in which adenine is attached to arabinofuranose via a beta-N(9)-glycosidic bond. | 2.6 | 1 | 0 | beta-D-arabinoside; purine nucleoside | antineoplastic agent; bacterial metabolite; nucleoside antibiotic |
| 3-deazaadenosine 3-deazaadenosine: RN given refers to parent cpd. | 2.6 | 1 | 0 | ||
| palladium Palladium: A chemical element having an atomic weight of 106.4, atomic number of 46, and the symbol Pd. It is a white, ductile metal resembling platinum, and following it in abundance and importance of applications. It is used in dentistry in the form of gold, silver, and copper alloys.. palladium : Chemical element (nickel group element atom) with atomic number 46. | 2.17 | 1 | 0 | metal allergen; nickel group element atom; platinum group metal atom | |
| zalcitabine Zalcitabine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.. zalcitabine : A pyrimidine 2',3'-dideoxyribonucleoside compound having cytosine as the nucleobase. | 2.6 | 1 | 0 | pyrimidine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; HIV-1 reverse transcriptase inhibitor |
| 4-chloro-7-nitrobenzofurazan 4-Chloro-7-nitrobenzofurazan: A benzofuran derivative used as a protein reagent since the terminal N-NBD-protein conjugate possesses interesting fluorescence and spectral properties. It has also been used as a covalent inhibitor of both beef heart mitochondrial ATPase and bacterial ATPase.. 4-chloro-7-nitrobenzofurazan : A benzoxadiazole that is 2,1,3-benzoxadiazole which is substituted at position 4 by chlorine and at position 7 by a nitro group. | 7.25 | 1 | 0 | benzoxadiazole; C-nitro compound; organochlorine compound | EC 1.4.3.4 (monoamine oxidase) inhibitor; EC 3.6.1.3 (adenosinetriphosphatase) inhibitor; fluorescent probe; fluorochrome |
| ancitabine Ancitabine: Congener of CYTARABINE that is metabolized to cytarabine and thereby maintains a more constant antineoplastic action.. ancitabine : An organic heterotricyclic compound resulting from the formal condensation of the oxo group of cytidine to the 2' position with loss of water to give the corresponding cyclic ether. A prodrug, it is metabolised to the antineoplastic agent cytarabine, so is used to maintain a more constant antineoplastic action. | 2.6 | 1 | 0 | diol; organic heterotricyclic compound | antimetabolite; antineoplastic agent; prodrug |
| chloropyramine chloropyramine: RN given refers to parent cpd; structure | 2.6 | 1 | 0 | aminopyridine | |
| levamisole Levamisole: An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6). levamisole : A 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole that has S configuration. It is used (generally as the monohydrochloride salt) to treat parasitic worm infections in pigs, sheep and cattle and was formerly used in humans as an adjuvant to chemotherapy for the treatment of various cancers. It is also widely used as an adulterant to coccaine. | 2.6 | 1 | 0 | 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole | antinematodal drug; antirheumatic drug; EC 3.1.3.1 (alkaline phosphatase) inhibitor; immunological adjuvant; immunomodulator |
| n'-nitrosonornicotine N'-nitrosonornicotine: structure; a potent carcinogen in laboratory animals | 2.6 | 1 | 0 | pyridines; pyrrolidines | |
| 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. | 2.6 | 1 | 0 | aminoglycoside antibiotic; anthracycline; p-quinones; tetracenequinones | antineoplastic agent; bacterial metabolite |
| zidovudine Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase. | 2.6 | 1 | 0 | azide; pyrimidine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; HIV-1 reverse transcriptase inhibitor |
| ribavirin Rebetron: Rebetron is tradename | 2.6 | 1 | 0 | 1-ribosyltriazole; aromatic amide; monocarboxylic acid amide; primary carboxamide | anticoronaviral agent; antiinfective agent; antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| fluorescamine Fluorescamine: A nonfluorescent reagent for the detection of primary amines, peptides and proteins. The reaction products are highly fluorescent. | 7.25 | 1 | 0 | ||
| pyridoxal phosphate [no description available] | 2.6 | 1 | 0 | pyridinecarbaldehyde | |
| ng-nitroarginine methyl ester NG-Nitroarginine Methyl Ester: A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension. | 2.11 | 1 | 0 | alpha-amino acid ester; L-arginine derivative; methyl ester; N-nitro compound | EC 1.14.13.39 (nitric oxide synthase) inhibitor |
| nitazoxanide nitazoxanide: a 5-nitrothiazolyl derivative used for a broad range of intestinal parasitic infections including CRYPTOSPORIDIUM and GIARDIA; it is a redox-active nitrothiazolyl-salicylamide prodrug | 2.6 | 1 | 0 | benzamides; carboxylic ester | |
| 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. | 2.6 | 1 | 0 | alkanethiol; L-proline derivative; N-acylpyrrolidine; pyrrolidinemonocarboxylic acid | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| oltipraz oltipraz : A 1,2-dithiole that is 3H-1,2-dithiole-3-thione substituted at positions 4 and 5 by methyl and pyrazin-2-yl groups respectively. | 2.6 | 1 | 0 | 1,2-dithiole; pyrazines | angiogenesis modulating agent; antimutagen; antineoplastic agent; antioxidant; EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor; neurotoxin; protective agent; schistosomicide drug |
| fiacitabine fiacitabine: anti-herpes virus agent which also inhibits growth of certain human tumor cell lines in vitro. | 2.6 | 1 | 0 | ||
| 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. | 2.6 | 1 | 0 | aromatic amide; monocarboxylic acid amide; monomethoxybenzene; N-alkylpiperazine; secondary alcohol | |
| brequinar brequinar : A quinolinemonocarboxylic acid that is quinoline substituted by 2'-fluoro[1,1'-biphenyl]-4-yl, methyl, carboxy and fluoro groups at positions 2, 3, 4, and 6, respectively. It is an inhibitor of dihydroorotate dehydrogenase, an enzyme that is required for de novo pyrimidine biosynthesis. The compound exhibits antineoplastic and antiviral properties. | 2.6 | 1 | 0 | biphenyls; monocarboxylic acid; monofluorobenzenes; quinolinemonocarboxylic acid | anticoronaviral agent; antimetabolite; antineoplastic agent; antiviral agent; EC 1.3.5.2 [dihydroorotate dehydrogenase (quinone)] inhibitor; immunosuppressive agent; pyrimidine synthesis inhibitor |
| imiquimod Imiquimod: A topically-applied aminoquinoline immune modulator that induces interferon production. It is used in the treatment of external genital and perianal warts, superficial CARCINOMA, BASAL CELL; and ACTINIC KERATOSIS.. imiquimod : An imidazoquinoline fused [4,5-c] carrying isobutyl and amino substituents at N-1 and C-4 respectively. A prescription medication, it acts as an immune response modifier and is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis. | 2.6 | 1 | 0 | imidazoquinoline | antineoplastic agent; interferon inducer |
| adefovir adefovir: inhibitor of African swine fever virus. adefovir(1-) : A organophosphonate oxoanion obtained by removal of a proton from the phosphonate group of adefovir, a nucleoside reverse transcriptase inhibitor. It is the major microspecies at pH 7.3 (according to Marvin v 6.2.0.).. adefovir : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens has been replaced by a 2-(6-amino-9H-purin-9-yl)ethoxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(t-butoxycarbonyloxymethyl) ester (dipivoxil ester) prodrug is used to treat chronic hepatitis B viral infection. | 2.6 | 1 | 0 | 6-aminopurines; ether; phosphonic acids | antiviral drug; DNA synthesis inhibitor; drug metabolite; HIV-1 reverse transcriptase inhibitor; nephrotoxic agent |
| cidofovir anhydrous Cidofovir: An acyclic nucleoside phosphonate that acts as a competitive inhibitor of viral DNA polymerases. It is used in the treatment of RETINITIS caused by CYTOMEGALOVIRUS INFECTIONS and may also be useful for treating HERPESVIRUS INFECTIONS.. cidofovir anhydrous : Cytosine substituted at the 1 position by a 3-hydroxy-2-(phosphonomethoxy)propyl group (S configuration). A nucleoside analogue, it is an injectable antiviral used for the treatment of cytomegalovirus (CMV) retinitis in AIDS patients. | 2.6 | 1 | 0 | phosphonic acids; pyrimidone | anti-HIV agent; antineoplastic agent; antiviral drug; photosensitizing agent |
| celgosivir celgosivir: inhibits glycoprotein processing & the growth of HIVs | 2.6 | 1 | 0 | ||
| gemcitabine gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer. | 2.6 | 1 | 0 | organofluorine compound; pyrimidine 2'-deoxyribonucleoside | antimetabolite; antineoplastic agent; antiviral drug; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; environmental contaminant; immunosuppressive agent; photosensitizing agent; prodrug; radiosensitizing agent; xenobiotic |
| atorvastatin [no description available] | 7.41 | 1 | 0 | aromatic amide; dihydroxy monocarboxylic acid; monofluorobenzenes; pyrroles; statin (synthetic) | environmental contaminant; xenobiotic |
| lamivudine [no description available] | 2.6 | 1 | 0 | monothioacetal; nucleoside analogue; oxacycle; primary alcohol | allergen; anti-HBV agent; antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor; HIV-1 reverse transcriptase inhibitor; prodrug |
| 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. | 2.6 | 1 | 0 | biphenylyltetrazole; monocarboxylic acid amide; monocarboxylic acid | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| zanamivir Zanamivir: A guanido-neuraminic acid that is used to inhibit NEURAMINIDASE. | 2.6 | 1 | 0 | guanidines | antiviral agent; EC 3.2.1.18 (exo-alpha-sialidase) inhibitor |
| adefovir dipivoxil bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine: structure given in first source. adefovir pivoxil : An organic phosphonate that is the dipivoxil ester of adefovir. A prodrug for adefovir, an HIV-1 reverse transcriptase inhibitor, adefovir pivoxil is used to treat chronic hepatitis B viral infection. | 2.6 | 1 | 0 | 6-aminopurines; carbonate ester; ether; organic phosphonate | antiviral drug; DNA synthesis inhibitor; HIV-1 reverse transcriptase inhibitor; nephrotoxic agent; prodrug |
| emtricitabine Emtricitabine: A deoxycytidine analog and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B viruses. It is used to treat HIV INFECTIONS.. emtricitabine : An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infection. | 2.6 | 1 | 0 | monothioacetal; nucleoside analogue; organofluorine compound; pyrimidone | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| adenosine quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit | 2.11 | 1 | 0 | adenosines; purines D-ribonucleoside | analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent |
| octyl gallate [no description available] | 2.6 | 1 | 0 | gallate ester | food antioxidant; hypoglycemic agent; plant metabolite |
| efavirenz efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection. | 2.6 | 1 | 0 | acetylenic compound; benzoxazine; cyclopropanes; organochlorine compound; organofluorine compound | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| nelfinavir Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.. nelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties. | 2.6 | 1 | 0 | aryl sulfide; benzamides; organic heterobicyclic compound; phenols; secondary alcohol; tertiary amino compound | antineoplastic agent; HIV protease inhibitor |
| 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. | 6.48 | 4 | 1 | D-glucopyranose | epitope; mouse metabolite |
| betulinic acid [no description available] | 2.6 | 1 | 0 | hydroxy 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 |
| arctigenin arctigenin: precursor to catechols; in many plants | 2.6 | 1 | 0 | lignan | |
| baicalin [no description available] | 2.6 | 1 | 0 | dihydroxyflavone; glucosiduronic acid; glycosyloxyflavone; monosaccharide derivative | antiatherosclerotic agent; antibacterial agent; anticoronaviral agent; antineoplastic agent; antioxidant; cardioprotective agent; EC 2.7.7.48 (RNA-directed RNA polymerase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; ferroptosis inhibitor; neuroprotective agent; non-steroidal anti-inflammatory drug; plant metabolite; prodrug |
| 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. | 2.6 | 1 | 0 | azacycloalkane; 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 |
| amprenavir [no description available] | 2.6 | 1 | 0 | carbamate ester; sulfonamide; tetrahydrofuryl ester | antiviral drug; HIV protease inhibitor |
| oseltamivir Oseltamivir: An acetamido cyclohexene that is a structural homolog of SIALIC ACID and inhibits NEURAMINIDASE.. oseltamivir : A cyclohexenecarboxylate ester that is the ethyl ester of oseltamivir acid. An antiviral prodrug (it is hydrolysed to the active free carboxylic acid in the liver), it is used to slow the spread of influenza. | 2.6 | 1 | 0 | acetamides; amino acid ester; cyclohexenecarboxylate ester; primary amino compound | antiviral drug; EC 3.2.1.18 (exo-alpha-sialidase) inhibitor; environmental contaminant; prodrug; xenobiotic |
| epigallocatechin gallate epigallocatechin gallate: a steroid 5alpha-reductase inhibitor and antimutagen in green tea (Camellia sinensis). (-)-epigallocatechin 3-gallate : A gallate ester obtained by the formal condensation of gallic acid with the (3R)-hydroxy group of (-)-epigallocatechin. | 3.78 | 2 | 0 | flavans; gallate ester; polyphenol | antineoplastic agent; antioxidant; apoptosis inducer; geroprotector; Hsp90 inhibitor; neuroprotective agent; plant metabolite |
| 1,2,3,4,6-pentakis-O-galloyl-beta-D-glucose pentagalloylglucose: pentahydroxy gallic acid ester of glucose; a phytogenic antineoplastic agent and antibacterial agent. 1,2,3,4,6-pentakis-O-galloyl-beta-D-glucose : A galloyl-beta-D-glucose compound having five galloyl groups in the 1-, 2-, 3-, 4- and 6-positions. | 2.6 | 1 | 0 | gallate ester; galloyl beta-D-glucose | anti-inflammatory agent; antineoplastic agent; geroprotector; hepatoprotective agent; plant metabolite; radiation protective agent; radical scavenger |
| cephalotaxine [no description available] | 2.6 | 1 | 0 | benzazepine alkaloid fundamental parent; benzazepine alkaloid; cyclic acetal; enol ether; organic heteropentacyclic compound; secondary alcohol; tertiary amino compound | |
| desipramine hydrochloride desipramine hydrochloride : The hydrochloride salt of desipramine. | 2.6 | 1 | 0 | hydrochloride | drug allergen |
| mefloquine hydrochloride [no description available] | 2.6 | 1 | 0 | hydrochloride | |
| aloxistatin aloxistatin: a membrane-permeable cysteine protease inhibitor. aloxistatin : An L-leucine derivative that is the amide obtained by formal condensation of the carboxy group of (2S,3S)-3-(ethoxycarbonyl)oxirane-2-carboxylic acid with the amino group of N-(3-methylbutyl)-L-leucinamide. | 2.6 | 1 | 0 | epoxide; ethyl ester; L-leucine derivative; monocarboxylic acid amide | anticoronaviral agent; cathepsin B inhibitor |
| propazole propazole: RN given refers to parent cpd; structure | 2.6 | 1 | 0 | benzimidazoles | |
| prulifloxacin prulifloxacin: structure given in first source | 2.6 | 1 | 0 | fluoroquinolone antibiotic; quinolone antibiotic | |
| 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. | 2.6 | 1 | 0 | benzimidazoles; biphenyls; carboxybiphenyl | angiotensin receptor antagonist; antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; environmental contaminant; xenobiotic |
| bergenin bergenin: RN refers to (2R-(2alpha,3beta,4alpha,4aalpha,10bbeta))-isomer; structure | 2.6 | 1 | 0 | trihydroxybenzoic acid | metabolite |
| 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. | 10.98 | 21 | 3 | 1,2,3-triazole | |
| zoledronic acid Zoledronic Acid: An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS.. zoledronic acid : An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position. | 2.6 | 1 | 0 | 1,1-bis(phosphonic acid); imidazoles | bone density conservation agent |
| artemisinin (+)-artemisinin : A sesquiterpene lactone obtained from sweet wormwood, Artemisia annua, which is used as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria. | 2.6 | 1 | 0 | organic peroxide; sesquiterpene lactone | antimalarial; plant metabolite |
| brinzolamide brinzolamide: an antiglaucoma agent | 2.6 | 1 | 0 | sulfonamide; thienothiazine | antiglaucoma drug; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
| malvidin chloride [no description available] | 3.27 | 1 | 0 | ||
| dipropylacetamide dipropylacetamide: structure. valpromide : A fatty amide derived from valproic acid. | 2.6 | 1 | 0 | fatty amide | geroprotector; metabolite; teratogenic agent |
| oxprenolol hydrochloride [no description available] | 2.6 | 1 | 0 | ||
| opipramol hydrochloride [no description available] | 2.6 | 1 | 0 | ||
| moroxydine [no description available] | 2.6 | 1 | 0 | biguanides | |
| thioxolone tioxolone : A 1,3-benzoxathiole having a hydroxy substituent at the 6-position. | 2.6 | 1 | 0 | benzoxathiole | antiseborrheic |
| hesperetin [no description available] | 3.27 | 1 | 0 | 3'-hydroxyflavanones; 4'-methoxyflavanones; monomethoxyflavanone; trihydroxyflavanone | antineoplastic agent; antioxidant; plant metabolite |
| honokiol [no description available] | 2.6 | 1 | 0 | biphenyls | |
| nobiletin nobiletin : A methoxyflavone that is flavone substituted by methoxy groups at positions 5, 6, 7, 8, 3' and 4' respectively. | 2.6 | 1 | 0 | methoxyflavone | antineoplastic agent; plant metabolite |
| lycorine lycorine: from bulbs of LYCORIS & other plants; RN given refers to (1 alpha,2 beta)-isomer; structure in Merck Index, 9th ed, #5444. lycorine : An indolizidine alkaloid that is 3,12-didehydrogalanthan substituted by hydroxy groups at positions and 2 and a methylenedioxy group across positions 9 and 10. Isolated from Crinum asiaticum, it has been shown to exhibit antimalarial activity. | 2.6 | 1 | 0 | indolizidine alkaloid | anticoronaviral agent; antimalarial; plant metabolite; protein synthesis inhibitor |
| leupeptin [no description available] | 2.6 | 1 | 0 | aldehyde; tripeptide | bacterial metabolite; calpain inhibitor; cathepsin B inhibitor; EC 3.4.21.4 (trypsin) inhibitor; serine protease inhibitor |
| tetrandrine tetrandrine: a bisbenzylisoquinoline that exhibits antifibrogenic activity | 2.6 | 1 | 0 | bisbenzylisoquinoline alkaloid; isoquinolines | |
| calpeptin [no description available] | 2.6 | 1 | 0 | amino acid amide | |
| fangchinoline [no description available] | 2.6 | 1 | 0 | aromatic ether; bisbenzylisoquinoline alkaloid; macrocycle | anti-HIV-1 agent; anti-inflammatory agent; antineoplastic agent; antioxidant; neuroprotective agent; plant metabolite |
| maslinic acid (2Alpha,3beta)-2,3-dihydroxyolean-12-en-28-oic acid: from Luehea divaricata and Agrimonia eupatoria | 2.6 | 1 | 0 | dihydroxy monocarboxylic acid; pentacyclic triterpenoid | anti-inflammatory agent; antineoplastic agent; antioxidant; plant metabolite |
| atovaquone Atovaquone: A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.. atovaquone : A naphthoquinone compound having a 4-(4-chlorophenyl)cyclohexyl group at the 2-position and a hydroxy substituent at the 3-position. | 2.6 | 1 | 0 | hydroxy-1,2-naphthoquinone | |
| eriocitrin eriocitrin: structure in first source. eriocitrin : A disaccharide derivative that consists of eriodictyol substituted by a 6-O-(alpha-L-rhamnopyranosyl)-beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage. | 3.27 | 1 | 0 | 3'-hydroxyflavanones; 4'-hydroxyflavanones; disaccharide derivative; flavanone glycoside; rutinoside; trihydroxyflavanone | antioxidant |
| loganin [no description available] | 2.6 | 1 | 0 | beta-D-glucoside; cyclopentapyran; enoate ester; iridoid monoterpenoid; methyl ester; monosaccharide derivative; secondary alcohol | anti-inflammatory agent; EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.2.1.20 (alpha-glucosidase) inhibitor; EC 3.4.23.46 (memapsin 2) inhibitor; neuroprotective agent; plant metabolite |
| moexipril [no description available] | 2.6 | 1 | 0 | peptide | |
| aucubin [no description available] | 2.6 | 1 | 0 | organic molecular entity | metabolite |
| catalpol [no description available] | 2.6 | 1 | 0 | organic molecular entity | metabolite |
| lekoptin (S)-verapamil : A 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile that has S configuration. | 2.6 | 1 | 0 | 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile | |
| diprotin a [no description available] | 3.62 | 2 | 0 | peptide | |
| n-methyladenosine N-methyladenosine: is a inhibitor of cell differentiation. N(6)-methyladenosine : A methyladenosine compound with one methyl group attached to N(6) of the adenine nucleobase. | 2.6 | 1 | 0 | methyladenosine | |
| sivelestat sivelestat: inhibitor of neutrophil elastase; structure given in first source | 2.6 | 1 | 0 | N-acylglycine; pivalate ester | |
| pyronaridine [no description available] | 2.6 | 1 | 0 | aminoquinoline | |
| geniposide [no description available] | 2.6 | 1 | 0 | terpene glycoside | |
| procyanidin Proanthocyanidins: Dimers and oligomers of flavan-3-ol units (CATECHIN analogs) linked mainly through C4 to C8 bonds to leucoanthocyanidins. They are structurally similar to ANTHOCYANINS but are the result of a different fork in biosynthetic pathways. | 2.1 | 1 | 0 | proanthocyanidin | |
| daidzin daidzin: a potent, selective, and reversible inhibitor of human mitochondrial aldehyde dehydrogenase. daidzein 7-O-beta-D-glucoside : A glycosyloxyisoflavone that is daidzein attached to a beta-D-glucopyranosyl residue at position 7 via a glycosidic linkage. It is used in the treatment of alcohol dependency (antidipsotropic). | 2.6 | 1 | 0 | 7-hydroxyisoflavones 7-O-beta-D-glucoside; hydroxyisoflavone; monosaccharide derivative | plant metabolite |
| sophocarpine [no description available] | 2.6 | 1 | 0 | ||
| marimastat marimastat: a matrix metalloproteinase inhibitor active in patients with advanced carcinoma of the pancreas, prostate, or ovary. marimastat : A secondary carboxamide resulting from the foraml condensation of the carboxy group of (2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoic acid with the alpha-amino group of N,3-dimethyl-L-valinamide. | 2.6 | 1 | 0 | hydroxamic acid; secondary carboxamide | antineoplastic agent; matrix metalloproteinase inhibitor |
| elacridar Elacridar: inhibitor of MDR1 PROTEIN; structure given in first source | 2.6 | 1 | 0 | ||
| mosapride 4-amino-5-chloro-2-ethoxy-N-({4-[(4-fluorophenyl)methyl]morpholin-2-yl}methyl)benzamide : A benzamide resulting from the formal condensation of the carboxy group of 4-amino-5-chloro-2-ethoxybenzoic acid with the amino group of 1-[4-(4-fluorobenzyl)morpholin-2-yl]methanamine. | 7.11 | 1 | 0 | aromatic ether; benzamides; monochlorobenzenes; monofluorobenzenes; morpholines; secondary carboxamide; substituted aniline; tertiary amino compound | |
| 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 | 2.11 | 1 | 0 | benzenes; monocarboxylic acid | |
| celastrol [no description available] | 2.6 | 1 | 0 | monocarboxylic acid; pentacyclic triterpenoid | anti-inflammatory drug; antineoplastic agent; antioxidant; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; Hsp90 inhibitor; metabolite |
| n-(n-(3-carboxyoxirane-2-carbonyl)leucyl)isoamylamine N-(N-(3-carboxyoxirane-2-carbonyl)leucyl)isoamylamine: inhibits calcium-activated neutral protease; see also record for E-64; RN given refers to (2-S-(2alpha,3beta)(R*)-isomer) | 2.6 | 1 | 0 | leucine derivative | |
| vadimezan vadimezan : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by a 5,6-dimethyl-9-oxoxanthen-4-yl group. | 2.6 | 1 | 0 | monocarboxylic acid; xanthones | antineoplastic agent |
| e 64 E 64: cysteine protease inhibitor of microbial origin, which inhibits cathepsin B (EC 3.4.22.1) and cathepsin L (EC 3.4.22.-) | 2.6 | 1 | 0 | dicarboxylic acid monoamide; epoxy monocarboxylic acid; guanidines; L-leucine derivative; zwitterion | antimalarial; antiparasitic agent; protease inhibitor |
| umifenovir umifenovir: an antiviral agent | 2.6 | 1 | 0 | indolyl carboxylic acid | |
| safinamide safinamide: short-acting inhibitor of MOA-B; FCE 26743 is (S)-isomer, FCE 28073 is (R)-isomer; structure in first source | 2.6 | 1 | 0 | amino acid amide | |
| ilomastat CS 610: matrix metalloproteinase inhibitor; structure in first source. ilomastat : An N-acyl-amino acid obtained by formal condensation of the carboxy group of (2R)-2-[2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoic acid with the amino group of N-methyl-L-tryptophanamide. A cell permeable broad-spectrum matrix metalloproteinase (MMP) inhibitor | 2.6 | 1 | 0 | hydroxamic acid; L-tryptophan derivative; N-acyl-amino acid | anti-inflammatory agent; antibacterial agent; antineoplastic agent; EC 3.4.24.24 (gelatinase A) inhibitor; neuroprotective agent |
| atazanavir atazanavir : A heavily substituted carbohydrazide that is an antiretroviral drug of the protease inhibitor (PI) class used to treat infection of human immunodeficiency virus (HIV). | 2.6 | 1 | 0 | carbohydrazide | antiviral drug; HIV protease inhibitor |
| vx 497 N-3-(3-(3-methoxy-4-oxazol-5-ylphenyl)ureido)benzylcarbamic acid tetrahydrofuran-3-yl ester: structure in first source | 2.6 | 1 | 0 | ||
| bcx 1812 [no description available] | 2.6 | 1 | 0 | 3-hydroxy monocarboxylic acid; acetamides; cyclopentanols; guanidines | antiviral drug; EC 3.2.1.18 (exo-alpha-sialidase) inhibitor |
| naproxen Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes. | 2.6 | 1 | 0 | methoxynaphthalene; monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; environmental contaminant; gout suppressant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| olmesartan olmesartan: an active metabolite of CS 866 | 2.6 | 1 | 0 | biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent |
| telbivudine [no description available] | 2.6 | 1 | 0 | pyrimidine 2'-deoxyribonucleoside | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| celastrol methyl ester celastrol methyl ester: isolated from Tripterygium wilfordii; potent inhibitory activity on both Kir2.1 and ERG1 potassium channels, leading to LONG QT SYNDROME | 2.6 | 1 | 0 | carboxylic ester | |
| resiquimod S 28463: structure given in first source | 2.6 | 1 | 0 | imidazoquinoline | |
| tanshinone ii a tashinone IIA: a cardiovascular agent with antineoplastic activity; isolated from Salvia miltiorrhiza; structure in first source | 2.6 | 1 | 0 | abietane diterpenoid | |
| anacardic acid anacardic acid: isolated from Anacardium occidentale; monophenol monooxygenase inhibitor. anacardic acid : A hydroxybenzoic acid that is salicylic acid substituted by a pentadecyl group at position 6. It is a major component of cashew nut shell liquid and exhibits an extensive range of bioactivities. | 2.6 | 1 | 0 | hydroxy monocarboxylic acid; hydroxybenzoic acid | anti-inflammatory agent; antibacterial agent; anticoronaviral agent; apoptosis inducer; EC 2.3.1.48 (histone acetyltransferase) inhibitor; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor; neuroprotective agent; plant metabolite |
| n-valyltryptophan N-valyltryptophan: RN given refers to (L)-isomer | 3.27 | 1 | 0 | peptide | |
| 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). | 2.31 | 1 | 0 | amino acid zwitterion; angiotensin II | human metabolite |
| migalastat migalastat: a potent inhibitor of glycolipid biosynthesis | 2.6 | 1 | 0 | piperidines | |
| erlotinib [no description available] | 2.6 | 1 | 0 | aromatic ether; quinazolines; secondary amino compound; terminal acetylenic compound | antineoplastic agent; epidermal growth factor receptor antagonist; protein kinase inhibitor |
| limonin [no description available] | 2.6 | 1 | 0 | epoxide; furans; hexacyclic triterpenoid; lactone; limonoid; organic heterohexacyclic compound | inhibitor; metabolite; volatile oil component |
| scutellarin scutellarin: see scutellarein for aglycone. scutellarin : The glycosyloxyflavone which is the 7-O-glucuronide of scutellarein. | 2.6 | 1 | 0 | glucosiduronic acid; glycosyloxyflavone; monosaccharide derivative; trihydroxyflavone | antineoplastic agent; proteasome inhibitor |
| cirsimaritin cirsimaritin: has antagonist or partial agonist activity on benzodiazepine receptors. cirsimaritin : A dimethoxyflavone that is flavone substituted by methoxy groups at positions 6 and 7 and hydroxy groups at positions 5 and 4' respectively. | 3.27 | 1 | 0 | dihydroxyflavone; dimethoxyflavone | |
| etravirine [no description available] | 2.6 | 1 | 0 | aminopyrimidine; aromatic ether; dinitrile; organobromine compound | antiviral agent; HIV-1 reverse transcriptase inhibitor |
| chelidonine chelidonine: benzophenanthridine derived from scoulerine from Chelidonium majus; RN given refers to parent cpd (chelidonine, (5bR-(5balpha,6beta,12alpha))-isomer) | 2.6 | 1 | 0 | alkaloid antibiotic; alkaloid fundamental parent; benzophenanthridine alkaloid | |
| 4-n-butylresorcinol 4-n-butylresorcinol: structure in first source | 2.6 | 1 | 0 | resorcinols | |
| darunavir Darunavir: An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.. darunavir : An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors. | 2.6 | 1 | 0 | carbamate ester; furofuran; sulfonamide | antiviral drug; HIV protease inhibitor |
| dapivirine Dapivirine: effectively prevented human immunodeficiency virus (HIV) infection in cocultures of monocyte-derived dendritic cells and T cells, representing primary targets in sexual transmission | 2.6 | 1 | 0 | ||
| nsc 74859 NSC 74859: inhibits Stat3 binding activity; structure in first source. S3I-201 : An amidobenzoic acid obtained by formal condensation of the carboxy group of [(4-methylbenzene-1-sulfonyl)oxy]acetic acid with the amino group of 4-amino-2-hydroxybenzoic acid. | 2.6 | 1 | 0 | amidobenzoic acid; monohydroxybenzoic acid; tosylate ester | STAT3 inhibitor |
| berbamine [no description available] | 2.6 | 1 | 0 | bisbenzylisoquinoline alkaloid; isoquinolines | |
| u-104 SLC-0111: a carbonic anhydrase inhibitor; structure in first source | 2.6 | 1 | 0 | ||
| 7-hydroxy-5-methyl-2-(2-oxopropyl)-8-[3,4,5-trihydroxy-6-(hydroxymethyl)-2-oxanyl]-1-benzopyran-4-one [no description available] | 2.6 | 1 | 0 | glycoside | |
| bortezomib [no description available] | 2.6 | 1 | 0 | amino acid amide; L-phenylalanine derivative; pyrazines | antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor |
| ritonavir Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver. | 2.6 | 1 | 0 | 1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas | antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic |
| tizoxanide tizoxanide: major metabolite of nitazoxanide; structure in first source | 2.6 | 1 | 0 | salicylamides | |
| naringenin (S)-naringenin : The (S)-enantiomer of naringenin. | 3.27 | 1 | 0 | (2S)-flavan-4-one; naringenin | expectorant; plant metabolite |
| taxifolin (+)-taxifolin : A taxifolin that has (2R,3R)-configuration. | 7.31 | 1 | 0 | taxifolin | metabolite |
| arbutin hydroquinone O-beta-D-glucopyranoside : A monosaccharide derivative that is hydroquinone attached to a beta-D-glucopyranosyl residue at position 4 via a glycosidic linkage. | 2.6 | 1 | 0 | beta-D-glucoside; monosaccharide derivative | Escherichia coli metabolite; plant metabolite |
| quinidine Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy. | 2.6 | 1 | 0 | cinchona alkaloid | alpha-adrenergic antagonist; anti-arrhythmia drug; antimalarial; drug allergen; EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor; EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; muscarinic antagonist; P450 inhibitor; potassium channel blocker; sodium channel blocker |
| conessine conessine : A steroid alkaloid that is con-5-enine substituted by a N,N-dimethylamino group at position 3. It has been isolated from the plant species of the family Apocynaceae. | 2.6 | 1 | 0 | steroid alkaloid; tertiary amino compound | antibacterial agent; antimalarial; H3-receptor antagonist; plant metabolite |
| saquinavir Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease. | 2.6 | 1 | 0 | L-asparagine derivative; quinolines | antiviral drug; HIV protease inhibitor |
| abacavir abacavir: a carbocyclic nucleoside with potent selective anti-HIV activity. abacavir : A 2,6-diaminopurine that is (1S)-cyclopent-2-en-1-ylmethanol in which the pro-R hydrogen at the 4-position is substituted by a 2-amino-6-(cyclopropylamino)-9H-purin-9-yl group. A nucleoside analogue reverse transcriptase inhibitor (NRTI) with antiretroviral activity against HIV, it is used (particularly as the sulfate) with other antiretrovirals in combination therapy of HIV infection. | 2.6 | 1 | 0 | 2,6-diaminopurines | antiviral drug; drug allergen; HIV-1 reverse transcriptase inhibitor |
| linezolid [no description available] | 2.6 | 1 | 0 | acetamides; morpholines; organofluorine compound; oxazolidinone | antibacterial drug; protein synthesis inhibitor |
| cyanidin 3-o-beta-d-glucopyranoside cyanidin 3-O-beta-D-glucoside : An anthocyanin cation that is a cyanidin cation linked to a beta-D-glucosyl moiety at position 3. | 3.27 | 1 | 0 | anthocyanin cation; beta-D-glucoside; monosaccharide derivative | metabolite |
| cephaelin cephaelin: do not confuse with cephalin of brain; after emetine this is the most important alkaloid of ipecac; protein synthesis inhibitor. cephaeline : A pyridoisoquinoline comprising emetam having a hydroxy group at the 6'-position and methoxy substituents at the 7'-, 10- and 11-positions. | 2.6 | 1 | 0 | pyridoisoquinoline | |
| (-)-usnic acid (-)-usnic acid : The (-)-enantiomer of usnic acid. | 2.6 | 1 | 0 | usnic acid | EC 1.13.11.27 (4-hydroxyphenylpyruvate dioxygenase) inhibitor |
| acetylleucyl-leucyl-norleucinal acetylleucyl-leucyl-norleucinal: a proteasome inhibitor. acetylleucyl-leucyl-norleucinal : A tripeptide composed of N-acetylleucyl, leucyl and norleucinal residues joined in sequence. | 2.6 | 1 | 0 | aldehyde; tripeptide | cysteine protease inhibitor |
| ao 128 AO 128: alpha-glucosidase inhibitor; structure given in first source | 7.28 | 6 | 4 | organic molecular entity | |
| resveratrol trans-resveratrol : A resveratrol in which the double bond has E configuration. | 3.78 | 2 | 0 | resveratrol | antioxidant; 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. | 2.58 | 2 | 0 | macrolide lactam | bacterial metabolite; immunosuppressive agent |
| lycopene [no description available] | 2.6 | 1 | 0 | acyclic carotene | antioxidant; plant metabolite |
| 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. | 2.6 | 1 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; xenobiotic |
| roflumilast [no description available] | 2.6 | 1 | 0 | aromatic ether; benzamides; chloropyridine; cyclopropanes; organofluorine compound | anti-asthmatic drug; phosphodiesterase IV inhibitor |
| L-cycloserine L-cycloserine : A 4-amino-1,2-oxazolidin-3-one that has S configuration. An antibiotic isolated from Erwinia uredovora. | 2.6 | 1 | 0 | 4-amino-1,2-oxazolidin-3-one | anti-HIV agent; anticonvulsant; EC 2.3.1.50 (serine C-palmitoyltransferase) inhibitor |
| 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. | 2.6 | 1 | 0 | N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide | |
| bevirimat bevirimat: an HIV inhibitor; disrupts late step in processing HIV Major Core Protein p24, preventing the capsid precursor p25 from being converted to mature capsid p24. bevirimat : A pentacyclic triterpenoid obtained by the formal condensation of 2,2-dimethylsuccinic acid with the 3-hydroxy group of betulinic acid. It is isolated from the Chinese herb Syzygium claviflorum. The first in the class of HIV-1 maturation inhibitors to be studied in humans, bevirimat was identified as a potent HIV drug candidate and several clinical trials were conducted, but development into a new drug was plagued by numerous resistance-related problems. | 2.6 | 1 | 0 | dicarboxylic acid monoester; monocarboxylic acid; pentacyclic triterpenoid | HIV-1 maturation inhibitor; metabolite |
| benzyloxycarbonylleucyl-leucyl-leucine aldehyde benzyloxycarbonylleucyl-leucyl-leucine aldehyde: proteasome inhibitor. N-benzyloxycarbonyl-L-leucyl-L-leucyl-L-leucinal : A tripeptide that is L-leucyl-L-leucyl-L-leucine in which the C-terminal carboxy group has been reduced to the corresponding aldehyde and the N-terminal amino group is protected as its benzyloxycarbonyl derivative. | 2.6 | 1 | 0 | amino aldehyde; carbamate ester; tripeptide | proteasome inhibitor |
| tenofovir tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection. | 2.6 | 1 | 0 | nucleoside analogue; phosphonic acids | antiviral drug; drug metabolite; HIV-1 reverse transcriptase inhibitor |
| posaconazole [no description available] | 2.6 | 1 | 0 | aromatic ether; conazole antifungal drug; N-arylpiperazine; organofluorine compound; oxolanes; triazole antifungal drug; triazoles | trypanocidal drug |
| gw 257406x maribavir: has antiviral activity against human cytomegalovirus | 2.6 | 1 | 0 | ||
| shikonin shikonin: a naphthazarin; has antineoplastic and angiogenesis inhibiting activities | 2.6 | 1 | 0 | hydroxy-1,4-naphthoquinone | |
| 4,4-difluoro-N-[(1S)-3-[3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]-1-cyclohexanecarboxamide [no description available] | 2.6 | 1 | 0 | tropane alkaloid | |
| cmx 001 [no description available] | 2.6 | 1 | 0 | ||
| amd 8664 [no description available] | 2.6 | 1 | 0 | ||
| bay 41-4109 BAY 41-4109: structure in first source | 2.6 | 1 | 0 | ||
| bay 57-1293 pritelivir: herpes simplex virus 1 helicase-primase inhibitor | 2.6 | 1 | 0 | ||
| 2'-c-methylcytidine 2'-C-methylcytidine: structure in first source | 2.6 | 1 | 0 | ||
| isoxanthohumol isoxanthohumol: structure in first source | 2.6 | 1 | 0 | flavanones | |
| 4-(4-chloro-2-methylphenoxy)-n-hydroxybutanamide 4-(4-chloro-2-methylphenoxy)-N-hydroxybutanamide: a c-FLIP inhibitor; structure in first source | 2.6 | 1 | 0 | aromatic ether | |
| mecarbinate [no description available] | 2.6 | 1 | 0 | ||
| dimethyl fumarate [no description available] | 2.1 | 1 | 0 | diester; enoate ester; methyl ester | antipsoriatic; immunomodulator |
| acetyl-aspartyl-glutamyl-valyl-aspartal acetyl-aspartyl-glutamyl-valyl-aspartal: a capase inhibitor. Ac-Asp-Glu-Val-Asp-H : A tetrapeptide consisting of two L-aspartic acid residues, an L-glutamyl residue and an L-valine residue with an acetyl group at the N-terminal and with the C-terminal carboxy group reduced to an aldehyde. It is an inhibitor of caspase-3/7. | 2.6 | 1 | 0 | tetrapeptide | protease inhibitor |
| octotropine methylbromide octotropine methylbromide: minor descriptor (65-86); on line & INDEX MEDICUS search TROPANES (69-86); RN given refers to endo-isomer. anisotropine methylbromide : A quaternary ammonium salt resulting from the reaction of the amino group of anisotropine with methyl bromide. | 2.6 | 1 | 0 | ||
| mercaptopurine Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.. purine-6-thiol : A thiol that is the tautomer of mercaptopurine.. mercaptopurine : A member of the class of purines that is 6,7-dihydro-1H-purine carrying a thione group at position 6. An adenine analogue, it is used in the treatment of acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML), Crohn's disease, and ulcerative colitis. | 2.6 | 1 | 0 | aryl thiol; purines; thiocarbonyl compound | anticoronaviral agent; antimetabolite; antineoplastic agent |
| jrf 12 N2,N4-dibenzylquinazoline-2,4-diamine: a selective, potent, reversible, and ATP-competitive p97 inhibitor | 2.6 | 1 | 0 | ||
| 3,4'-dihydroxyflavone 3,4'-dihydroxyflavone: an antioxidant; structure in first source | 2.6 | 1 | 0 | ||
| caffeic acid trans-caffeic acid : The trans-isomer of caffeic acid. | 3.27 | 1 | 0 | caffeic acid | geroprotector; mouse metabolite |
| 3-(3,4-dimethoxyphenyl)propenoic acid 3-(3,4-dimethoxyphenyl)propenoic acid: structure given in first source; RN given refers to parent cpd. 3,4-dimethoxycinnamic acid : A methoxycinnamic acid that is trans-cinnamic acid substituted by methoxy groups at positions 3' and 4' respectively. | 2.6 | 1 | 0 | methoxycinnamic acid | |
| isoferulic acid isoferulic acid: isomer of ferulic acid; structure. isoferulic acid : A ferulic acid consisting of trans-cinnamic acid bearing methoxy and hydroxy substituents at positions 4 and 3 respectively on the phenyl ring. | 2.6 | 1 | 0 | ferulic acids | antioxidant; biomarker; metabolite |
| cyclouridine cyclouridine: structure given in third source | 2.6 | 1 | 0 | ||
| 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. | 2.6 | 1 | 0 | aromatic 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 |
| zucapsaicin [no description available] | 2.6 | 1 | 0 | methoxybenzenes; phenols | |
| nbd 556 [no description available] | 2.6 | 1 | 0 | ||
| thioguanine anhydrous Thioguanine: An antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.. tioguanine : A 2-aminopurine that is the 6-thiono derivative of 2-amino-1,9-dihydro-6H-purine. Incorporates into DNA and inhibits synthesis. Used in the treatment of leukaemia. | 2.6 | 1 | 0 | 2-aminopurines | anticoronaviral agent; antimetabolite; antineoplastic agent |
| 4,5,6,7-tetrachloroindan-1,3-dione 4,5,6,7-tetrachloroindan-1,3-dione: inhibits ubiquitin C-terminal hydrolase L1 | 2.6 | 1 | 0 | ||
| tamoxifen [no description available] | 2.1 | 1 | 0 | stilbenoid; tertiary amino compound | angiogenesis inhibitor; antineoplastic agent; bone density conservation agent; EC 1.2.3.1 (aldehyde oxidase) inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; estrogen antagonist; estrogen receptor antagonist; estrogen receptor modulator |
| srpin340 SRPIN340: Serine-Arginine-Rich Protein Kinase Inhibitor | 2.6 | 1 | 0 | ||
| pr-619 [no description available] | 2.6 | 1 | 0 | ||
| p5091 P5091: inhibits ubiquitin-specific protease 7; structure in first source | 2.6 | 1 | 0 | ||
| 4,6-dimorpholino-n-(4-nitrophenyl)-1,3,5-triazin-2-amine 4,6-dimorpholino-N-(4-nitrophenyl)-1,3,5-triazin-2-amine: an mTOR activator; structure in first source | 2.31 | 1 | 0 | ||
| trovirdine trovirdine: HIV-1 reverse transcriptase inhibitor | 2.6 | 1 | 0 | ||
| fti 277 [no description available] | 2.6 | 1 | 0 | ||
| u 0126 U 0126: protein kinase kinase inhibitor; structure in first source | 2.6 | 1 | 0 | aryl sulfide; dinitrile; enamine; substituted aniline | antineoplastic agent; antioxidant; apoptosis inducer; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; osteogenesis regulator; vasoconstrictor agent |
| vicriviroc vicriviroc: structure in first source | 2.6 | 1 | 0 | (trifluoromethyl)benzenes | |
| telaprevir [no description available] | 2.6 | 1 | 0 | cyclopentapyrrole; cyclopropanes; oligopeptide; pyrazines | antiviral drug; hepatitis C protease inhibitor; peptidomimetic |
| 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. | 2.6 | 1 | 0 | beta-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 |
| ospemifene Ospemifene: structure in first source. ospemifene : An organochlorine compound that is a selective estrogen receptor modulator; used for treatment of dyspareunia. | 2.1 | 1 | 0 | aromatic ether; organochlorine compound; primary alcohol | anti-inflammatory agent; antineoplastic agent; estrogen receptor modulator |
| 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). | 2.6 | 1 | 0 | 1,3-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 |
| yya-021 YYA-021: an HIV entry inhibitor; structure in first source | 2.6 | 1 | 0 | ||
| cp 94253 [no description available] | 2.11 | 1 | 0 | pyrrolopyridine | |
| sb 415286 3-(3-chloro-4-hydroxyphenylamino)-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione: a glycogen synthase kinase-3 inhibitor; structure in first source | 2.6 | 1 | 0 | C-nitro compound; maleimides; monochlorobenzenes; phenols; secondary amino compound; substituted aniline | antioxidant; apoptosis inducer; EC 2.7.11.26 (tau-protein kinase) inhibitor; neuroprotective agent |
| sitagliptin sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity. | 5.85 | 11 | 0 | triazolopyrazine; trifluorobenzene | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; environmental contaminant; hypoglycemic agent; serine proteinase inhibitor; xenobiotic |
| tak-220 TAK-220: structure in first source | 2.6 | 1 | 0 | ||
| jtk-303 [no description available] | 2.6 | 1 | 0 | aromatic ether; monochlorobenzenes; organofluorine compound; quinolinemonocarboxylic acid; quinolone | HIV-1 integrase inhibitor |
| nbd 557 [no description available] | 2.6 | 1 | 0 | ||
| quercetin [no description available] | 3.73 | 2 | 0 | 7-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 |
| apigenin Chamomile: Common name for several daisy-like plants (MATRICARIA; TRIPLEUROSPERMUM; ANTHEMIS; CHAMAEMELUM) native to Europe and Western Asia, now naturalized in the United States and Australia. | 3.27 | 1 | 0 | trihydroxyflavone | antineoplastic agent; metabolite |
| luteolin [no description available] | 3.27 | 1 | 0 | 3'-hydroxyflavonoid; tetrahydroxyflavone | angiogenesis inhibitor; anti-inflammatory agent; antineoplastic agent; apoptosis inducer; c-Jun N-terminal kinase inhibitor; EC 2.3.1.85 (fatty acid synthase) inhibitor; immunomodulator; nephroprotective agent; plant metabolite; radical scavenger; vascular endothelial growth factor receptor antagonist |
| 5'-o-caffeoylquinic acid trans-5-O-caffeoyl-D-quinic acid : A cinnamate ester obtained by formal condensation of the carboxy group of trans-caffeic acid with the 5-hydroxy group of quinic acid. | 2.6 | 1 | 0 | cinnamate ester; cyclitol carboxylic acid | plant metabolite |
| luteolin-7-glucoside luteolin-7-glucoside: has both antiasthmatic and antineoplastic activities; has 3C protease inhibitory activity; isolated from Ligustrum lucidum. luteolin 7-O-beta-D-glucoside : A glycosyloxyflavone that is luteolin substituted by a beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage. | 2.6 | 1 | 0 | beta-D-glucoside; glycosyloxyflavone; monosaccharide derivative; trihydroxyflavone | antioxidant; plant metabolite |
| cyclosporine [no description available] | 2.6 | 1 | 0 | ||
| rutin Hydroxyethylrutoside: Monohydroxyethyl derivative of rutin. Peripheral circulation stimulant used in treatment of venous disorders. | 2.17 | 1 | 0 | disaccharide derivative; quercetin O-glucoside; rutinoside; tetrahydroxyflavone | antioxidant; metabolite |
| kaempferol [no description available] | 3.27 | 1 | 0 | 7-hydroxyflavonol; flavonols; tetrahydroxyflavone | antibacterial agent; geroprotector; human blood serum metabolite; human urinary metabolite; human xenobiotic metabolite; plant metabolite |
| harmine Harmine: Alkaloid isolated from seeds of PEGANUM HARMALA; ZYGOPHYLLACEAE. It is identical to banisterine, or telepathine, from Banisteria caapi and is one of the active ingredients of hallucinogenic drinks made in the western Amazon region from related plants. It has no therapeutic use, but (as banisterine) was hailed as a cure for postencephalitic PARKINSON DISEASE in the 1920's.. harmine : A harmala alkaloid in which the harman skeleton is methoxy-substituted at C-7. | 2.6 | 1 | 0 | harmala alkaloid | anti-HIV agent; EC 1.4.3.4 (monoamine oxidase) inhibitor; metabolite |
| genistein [no description available] | 3.27 | 1 | 0 | 7-hydroxyisoflavones | antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; geroprotector; human urinary metabolite; phytoestrogen; plant metabolite; tyrosine kinase inhibitor |
| eprosartan eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure. | 2.6 | 1 | 0 | dicarboxylic acid; imidazoles; thiophenes | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| mycophenolate mofetil mycophenolate mofetil : A carboxylic ester resulting from the formal condensation between the carboxylic acid group of mycophenolic acid and the hydroxy group of 2-(morpholin-4-yl)ethanol. In the liver, it is metabolised to mycophenolic acid, an immunosuppressant for which it is a prodrug. It is widely used to prevent tissue rejection following organ transplants as well as for the treatment of certain autoimmune diseases. | 2.6 | 1 | 0 | carboxylic ester; ether; gamma-lactone; phenols; tertiary amino compound | anticoronaviral agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; immunosuppressive agent; prodrug |
| entacapone entacapone: structure given in first source. entacapone : A monocarboxylic acid amide that is N,N-diethylprop-2-enamide in which the hydrogen at position 2 is substituted by a cyano group and the hydrogen at the 3E position is substituted by a 3,4-dihydroxy-5-nitrophenyl group. | 2.6 | 1 | 0 | 2-nitrophenols; catechols; monocarboxylic acid amide; nitrile | antidyskinesia agent; antiparkinson drug; central nervous system drug; EC 2.1.1.6 (catechol O-methyltransferase) inhibitor |
| amentoflavone [no description available] | 2.6 | 1 | 0 | biflavonoid; hydroxyflavone; ring assembly | angiogenesis inhibitor; antiviral agent; cathepsin B inhibitor; P450 inhibitor; plant metabolite |
| baicalein [no description available] | 2.6 | 1 | 0 | trihydroxyflavone | angiogenesis inhibitor; anti-inflammatory agent; antibacterial agent; anticoronaviral agent; antifungal agent; antineoplastic agent; antioxidant; apoptosis inducer; EC 1.13.11.31 (arachidonate 12-lipoxygenase) inhibitor; EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor; EC 4.1.1.17 (ornithine decarboxylase) inhibitor; ferroptosis inhibitor; geroprotector; hormone antagonist; plant metabolite; prostaglandin antagonist; radical scavenger |
| genkwanin genkwanin: structure. genkwanin : A monomethoxyflavone that is apigenin in which the hydroxy group at position 7 is methylated. | 2.6 | 1 | 0 | dihydroxyflavone; monomethoxyflavone | metabolite |
| hispidulin hispidulin : A monomethoxyflavone that is scutellarein methylated at position 6. | 3.27 | 1 | 0 | monomethoxyflavone; trihydroxyflavone | anti-inflammatory agent; anticonvulsant; antineoplastic agent; antioxidant; apoptosis inducer; plant metabolite |
| hyperoside quercetin 3-O-beta-D-galactopyranoside : A quercetin O-glycoside that is quercetin with a beta-D-galactosyl residue attached at position 3. Isolated from Artemisia capillaris, it exhibits hepatoprotective activity. | 2.6 | 1 | 0 | beta-D-galactoside; monosaccharide derivative; quercetin O-glycoside; tetrahydroxyflavone | hepatoprotective agent; plant metabolite |
| mangostin mangostin: xanthone from rind of Garcinia mangostana Linn. fruit. alpha-mangostin : A member of the class of xanthones that is 9H-xanthene substituted by hydroxy group at positions 1, 3 and 6, a methoxy group at position 7, an oxo group at position 9 and prenyl groups at positions 2 and 8. Isolated from the stems of Cratoxylum cochinchinense, it exhibits antioxidant, antimicrobial and antitumour activities. | 2.6 | 1 | 0 | aromatic ether; phenols; xanthones | antimicrobial agent; antineoplastic agent; antioxidant; plant metabolite |
| 3-methylquercetin isorhamnetin : A monomethoxyflavone that is quercetin in which the hydroxy group at position 3' is replaced by a methoxy group. | 2.6 | 1 | 0 | 7-hydroxyflavonol; monomethoxyflavone; tetrahydroxyflavone | anticoagulant; EC 1.14.18.1 (tyrosinase) inhibitor; metabolite |
| kaempferide kaempferide: structure in first source. kaempferide : A monomethoxyflavone that is the 4'-O-methyl derivative of kaempferol. | 2.6 | 1 | 0 | 7-hydroxyflavonol; monomethoxyflavone; trihydroxyflavone | antihypertensive agent; metabolite |
| orientin orientin: structure given in first source; RN given refers to the (D-glucopyranosyl)-isomer. orientin : A C-glycosyl compound that is luteolin substituted by a beta-D-glucopyranosyl moiety at position 8. | 2.6 | 1 | 0 | 3'-hydroxyflavonoid; C-glycosyl compound; tetrahydroxyflavone | antioxidant; metabolite |
| scutellarein scutellarein: aglycone of scutellarin from Scutellaria baicalensis; carthamidin is 2S isomer of scutellarein; do not confuse with isoscutellarein and/or isocarthamidin which are respective regioisomers, or with the scutelarin protein. scutellarein : Flavone substituted with hydroxy groups at C-4', -5, -6 and -7. | 2.6 | 1 | 0 | tetrahydroxyflavone | metabolite |
| trans-2,3',4,5'-tetrahydroxystilbene trans-2,3',4,5'-tetrahydroxystilbene: hydroxystilbene oxyresveratrol | 2.6 | 1 | 0 | stilbenoid | |
| polydatin trans-piceid : A stilbenoid that is trans-resveratrol substituted at position 3 by a beta-D-glucosyl residue. | 2.6 | 1 | 0 | beta-D-glucoside; monosaccharide derivative; polyphenol; stilbenoid | anti-arrhythmia drug; antioxidant; geroprotector; hepatoprotective agent; metabolite; nephroprotective agent; potassium channel modulator |
| chicoric acid chicoric acid: inhibits HIV-1 integrase | 2.6 | 1 | 0 | organooxygen compound | geroprotector; HIV-1 integrase inhibitor |
| acteoside acteoside: a protein kinase C inhibitor with hepatoprotective, anti-asthmatic, and analgesic activities; a phenylethanoid glycoside related to isoacteoside; from leaves of Lippia multiflora (Verbenaceae). acteoside : A glycoside that is the alpha-L-rhamnosyl-(1->3)-beta-D-glucoside of hydroxytyrosol in which the hydroxy group at position 4 of the glucopyranosyl moiety has undergone esterification by formal condensation with trans-caffeic acid. | 2.6 | 1 | 0 | catechols; cinnamate ester; disaccharide derivative; glycoside; polyphenol | anti-inflammatory agent; antibacterial agent; antileishmanial agent; neuroprotective agent; plant metabolite |
| dorzolamide dorzolamide: topically effective ocular hypotensive carbonic anhydrase inhibitor; RN refers to mono-HCl (4S-trans)-isomer. dorzolamide : 5,6-Dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide in which hydrogens at the 4 and 6 positions are substituted by ethylamino and methyl groups, respectively (4S, trans-configuration). A carbonic anhydrase inhibitor, it is used as the hydrochloride in ophthalmic solutions to lower increased intraocular pressure in the treatment of open-angle glaucoma and ocular hypertension. | 2.6 | 1 | 0 | sulfonamide; thiophenes | antiglaucoma drug; antihypertensive agent; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
| 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. | 2.08 | 1 | 0 | antibiotic 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 |
| topiramate Topiramate: A sulfamate-substituted fructose analog that was originally identified as a hypoglycemic agent. It is used for the treatment of EPILEPSY and MIGRAINE DISORDERS, and may also promote weight loss.. topiramate : A hexose derivative that is 2,3:4,5-di-O-isopropylidene-beta-D-fructopyranose in which the hydroxy group has been converted to the corresponding sulfamate ester. It blocks voltage-dependent sodium channels and is used as an antiepileptic and for the prevention of migraine. | 2.6 | 1 | 0 | cyclic ketal; ketohexose derivative; sulfamate ester | anticonvulsant; sodium channel blocker |
| benzyloxycarbonyl-phe-ala-fluormethylketone cathepsin B inhibitor : A cysteine protease inhibitor which inhibits cathepsin B (EC 3.4.22.1). | 2.6 | 1 | 0 | ||
| n-(n-(3,5-difluorophenacetyl)alanyl)phenylglycine tert-butyl ester DAPT : A dipeptide consisting of alanylphenylglycine derivatised as a 3,5-difluorophenylacetamide at the amino terminal and a tert-butyl ester at the carboxy terminal. A gamma-secretase inhibitor. | 2.6 | 1 | 0 | carboxylic ester; difluorobenzene; dipeptide; tert-butyl ester | EC 3.4.23.46 (memapsin 2) inhibitor |
| casticin casticin: from fruit of Vitex rotundifolia; structure in second source. casticin : A tetramethoxyflavone that consists of quercetagetin in which the hydroxy groups at positions 3, 6, 7 and 4' have been replaced by methoxy groups. It has been isolated from Eremophila mitchellii. | 2.6 | 1 | 0 | dihydroxyflavone; tetramethoxyflavone | apoptosis inducer; plant metabolite |
| 5,7-dihydroxy-6-methoxy-2-phenylchromen-4-one 5,7-dihydroxy-6-methoxy-2-phenylchromen-4-one: isolated from the Chinese herb Scutellariae radix. oroxylin A : A dihydroxy- and monomethoxy-flavone in which the hydroxy groups are positioned at C-5 and C-7 and the methoxy group is at C-6. | 2.6 | 1 | 0 | dihydroxyflavone; monomethoxyflavone | antineoplastic agent; EC 1.14.13.39 (nitric oxide synthase) inhibitor |
| (E)-2,3,5,4'-tetrahydroxystilbene-2-O-beta-D-glucoside 2,3,5,4'-tetrahydroxystilbene-2-O-beta-D-glucopyranoside: Tyrosinase inhibitor from Polygonum multiflorum; structure in first source. (E)-2,3,5,4'-tetrahydroxystilbene-2-O-beta-D-glucoside : A stilbenoid that is trans-stilbene which has been substituted by hydroxy groups at positions 2, 3, 5, and 4', and in which the hydroxy group at positon 2 has then been converted to the corresponding the beta-D-glucoside. | 2.6 | 1 | 0 | beta-D-glucoside; resorcinols; stilbenoid | anti-inflammatory agent; antioxidant; apoptosis inhibitor; cardioprotective agent; cyclooxygenase 2 inhibitor; platelet aggregation inhibitor |
| tyrphostin ag 555 [no description available] | 2.6 | 1 | 0 | ||
| pd 151746 [no description available] | 2.6 | 1 | 0 | ||
| 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. | 2.6 | 1 | 0 | dipeptide | EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| verteporfin (2R,2(1)S)-8-ethenyl-2(1),2(2)-bis(methoxycarbonyl)-17-(3-methoxy-3-oxopropyl)-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13-propanoic acid : The 2(1),2(2),17-trimethyl ester of (2R,2(1)S)-2(1),2(2)-dicarboxy-8-ethenyl-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13,17-dipropanoic acid. | 2.6 | 1 | 0 | ||
| batimastat batimastat: structure given in first source; a synthetic matrix metalloproteinase inhibitor. batimastat : A secondary carboxamide resulting from the formal condensation of the carboxy group of (2S,3R)-5-methyl-3-{[(2S)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl]carbamoyl}-2-[(thiophen-2-ylsulfanyl)methyl]hexanoic acid with the amino group of hydroxylamine. It a broad-spectrum matrix metalloprotease inhibitor. | 2.6 | 1 | 0 | hydroxamic acid; L-phenylalanine derivative; organic sulfide; secondary carboxamide; thiophenes; triamide | angiogenesis inhibitor; antineoplastic agent; matrix metalloproteinase inhibitor |
| indinavir sulfate Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability. | 2.6 | 1 | 0 | dicarboxylic acid diamide; N-(2-hydroxyethyl)piperazine; piperazinecarboxamide | HIV protease inhibitor |
| phosphorus Phosphorus: A non-metal element that has the atomic symbol P, atomic number 15, and atomic weight 31. It is an essential element that takes part in a broad variety of biochemical reactions. | 8.8 | 1 | 1 | monoatomic phosphorus; nonmetal atom; pnictogen | macronutrient |
| solanesol solanesol : A nonaprenol that is hexatriaconta-2,6,10,14,18,22,26,30,34-nonaen-1-ol substituted by 9 methyl groups at positions 3, 7, 11, 15, 19, 23, 27, 31 and 35 (the all-trans0stereoisomer). | 2.6 | 1 | 0 | nonaprenol; primary alcohol | plant metabolite |
| pepstatin pepstatin: inhibits the aspartic protease endothiapepsin | 2.6 | 1 | 0 | pentapeptide; secondary carboxamide | bacterial metabolite; EC 3.4.23.* (aspartic endopeptidase) inhibitor |
| l 685458 L 685458: a gamma-secretase inhibitor; structure in first source. L-685,458 : A peptide and carboxamide that is L-leucyl-L-phenylalaninamide, L-Leu-L-Phe-NH2, which has been acylated on the N-terminus by a Phe-Phe hydroxyethylene dipeptide isotere, 2R-benzyl-5S-tert-butoxycarbonylamino-4R-hydroxy-6-phenylhexanoic acid. Compounds based on the structure of L-685,458 are potent inhibitors of gamma-secretase, which mediates the final catalytic step that generates the amyloid beta-peptide (Abeta), which assembles into the neurotoxic aggregates in the brains of sufferers of Alzheimer's disease. | 2.6 | 1 | 0 | carbamate ester; monocarboxylic acid amide; peptide; secondary alcohol | EC 3.4.23.46 (memapsin 2) inhibitor; peptidomimetic |
| bms 806 BMS 806: prevents entry of HIV into cells by binding HIV envelope protein gp120; no further info available 4/2002 | 2.6 | 1 | 0 | ||
| benzyloxycarbonylvalyl-alanyl-aspartyl fluoromethyl ketone [no description available] | 2.6 | 1 | 0 | ||
| tulobuterol hydrochloride [no description available] | 2.6 | 1 | 0 | organic molecular entity | |
| salubrinal salubrinal: prevents dephosphorylation of eIF2alpha; structure in first source. salubrinal : A member of the class of quinolines that is a mixed aminal resulting from the formal condensation oftrichloroacetaldehyde with the amide nitrogen of trans-cinnamamide and the primary amino group of 1-quinolin-8-ylthiourea. It is a selective inhibitor of cellular complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit alpha (eIF2alpha). | 2.6 | 1 | 0 | aminal; organochlorine compound; quinolines; secondary carboxamide; thioureas | |
| 4,4'-diisothiocyanostilbene-2,2'-disulfonic acid 4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid: An inhibitor of anion conductance including band 3-mediated anion transport. | 2.31 | 1 | 0 | ||
| germacrone germacrone: isolated from Curcuma wenyujin | 2.6 | 1 | 0 | germacrane sesquiterpenoid; olefinic compound | androgen antagonist; anti-inflammatory agent; antifeedant; antifungal agent; antimicrobial agent; antineoplastic agent; antioxidant; antitussive; antiviral agent; apoptosis inducer; autophagy inducer; hepatoprotective agent; insecticide; neuroprotective agent; plant metabolite; volatile oil component |
| (2e,4e,6e,10e)-3,7,11,15-tetramethyl-2,4,6,10,14-hexadecapentaenoic acid (2E,4E,6E,10E)-3,7,11,15-tetramethyl-2,4,6,10,14-hexadecapentaenoic acid: an acyclic retinoid that suppresses hepatocellular carcinoma recurrence; structure in first source | 2.6 | 1 | 0 | ||
| lithospermic acid [no description available] | 2.6 | 1 | 0 | ||
| laq824 LAQ824: Histone deacetylase inhibitor | 2.6 | 1 | 0 | ||
| ekb 569 EKB 569: an EGF receptor kinase inhibitor | 2.6 | 1 | 0 | aminoquinoline; monocarboxylic acid amide; monochlorobenzenes; nitrile | protein kinase inhibitor |
| rilpivirine [no description available] | 2.6 | 1 | 0 | aminopyrimidine; nitrile | EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor; HIV-1 reverse transcriptase inhibitor |
| (1Ar,7aS,10aS,10bS)-1a,5-dimethyl-8-methylidene-2,3,6,7,7a,8,10a,10b-octahydrooxireno[9,10]cyclodeca[1,2-b]furan-9(1aH)-one [no description available] | 2.6 | 1 | 0 | germacranolide | |
| 4,5-di-O-caffeoylquinic acid [no description available] | 2.6 | 1 | 0 | quinic acid | |
| indigo carmine 3,5-di-O-(E)-caffeoylquinic acid: from roots of Lychnophora ericoides; structure in first source. 3,5-di-O-caffeoyl quinic acid : A carboxylic ester that is the diester obtained by the condensation of the hydroxy groups at positions 3 and 5 of (-)-quinic acid with the carboxy group of trans-caffeic acid. Isolated from Brazilian propolis and Suaeda glauca, it exhibits hepatoprotective and cytotoxic activities. | 2.6 | 1 | 0 | ||
| artesunate artesunic acid: RN given for (3R-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,(2aR*))-isomer; succinic ester of artemether | 2.6 | 1 | 0 | artemisinin derivative; cyclic acetal; dicarboxylic acid monoester; hemisuccinate; semisynthetic derivative; sesquiterpenoid | antimalarial; antineoplastic agent; ferroptosis inducer |
| (3S,6S,9S,12R)-3-[(2S)-Butan-2-yl]-6-[(1-methoxyindol-3-yl)methyl]-9-(6-oxooctyl)-1,4,7,10-tetrazabicyclo[10.4.0]hexadecane-2,5,8,11-tetrone [no description available] | 2.6 | 1 | 0 | oligopeptide | |
| vildagliptin [no description available] | 11.49 | 40 | 2 | amino acid amide | |
| talabostat talabostat: an antineoplastic agent; structure in first source | 2.25 | 1 | 0 | ||
| belinostat [no description available] | 2.6 | 1 | 0 | hydroxamic acid; olefinic compound; sulfonamide | antineoplastic agent; EC 3.5.1.98 (histone deacetylase) inhibitor |
| hdac-42 HDAC-42: structure in first source | 2.6 | 1 | 0 | amidobenzoic acid | |
| chlorhexidine Chlorhexidine: A disinfectant and topical anti-infective agent used also as mouthwash to prevent oral plaque.. chlorhexidine : A bisbiguanide compound with a structure consisting of two (p-chlorophenyl)guanide units linked by a hexamethylene bridge. | 2.6 | 1 | 0 | biguanides; monochlorobenzenes | antibacterial agent; antiinfective agent |
| gs-7340 tenofovir alafenamide: component of Biktarvy. tenofovir alafenamide : An L-alanine derivative that is isopropyl L-alaninate in which one of the amino hydrogens is replaced by an (S)-({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)(phenoxy)phosphoryl group. A prodrug for tenofovir, it is used (as the fumarate salt) in combination therapy for the treatment of HIV-1 infection. | 2.6 | 1 | 0 | 6-aminopurines; ether; isopropyl ester; L-alanine derivative; phosphoramidate ester | antiviral drug; HIV-1 reverse transcriptase inhibitor; prodrug |
| iniparib [no description available] | 2.6 | 1 | 0 | carbonyl compound; organohalogen compound | |
| nvp-dpp728 [no description available] | 3.19 | 1 | 0 | ||
| n-(2-amino-5-fluorobenzyl)-4-(n-(pyridine-3-acrylyl)aminomethyl)benzamide [no description available] | 2.6 | 1 | 0 | ||
| pri-2205 [no description available] | 2.6 | 1 | 0 | ||
| mk 0752 [no description available] | 2.6 | 1 | 0 | ||
| givinostat [no description available] | 2.6 | 1 | 0 | carbamate ester | |
| pd 144418 [no description available] | 2.6 | 1 | 0 | ||
| bicyclol bicyclol: an antihepatitis drug, on the metabolism and hepatotoxicity of aflatoxin B1 (AFB1) in rats. | 2.6 | 1 | 0 | ||
| midostaurin midostaurin : An organic heterooctacyclic compound that is the N-benzoyl derivative of staurosporine. | 2.6 | 1 | 0 | benzamides; gamma-lactam; indolocarbazole; organic heterooctacyclic compound | antineoplastic agent; EC 2.7.11.13 (protein kinase C) inhibitor |
| ly 450139 [no description available] | 2.6 | 1 | 0 | peptide | |
| 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). | 2.6 | 1 | 0 | aminopyrimidine; 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 |
| rivaroxaban Rivaroxaban: A morpholine and thiophene derivative that functions as a FACTOR XA INHIBITOR and is used in the treatment and prevention of DEEP-VEIN THROMBOSIS and PULMONARY EMBOLISM. It is also used for the prevention of STROKE and systemic embolization in patients with non-valvular ATRIAL FIBRILLATION, and for the prevention of atherothrombotic events in patients after an ACUTE CORONARY SYNDROME.. rivaroxaban : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-chlorothiophene-2-carboxylic acid with the amino group of 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one. An anticoagulant used for prophylaxis of venous thromboembolism in patients with knee or hip replacement surgery. | 2.6 | 1 | 0 | aromatic amide; lactam; monocarboxylic acid amide; morpholines; organochlorine compound; oxazolidinone; thiophenes | anticoagulant; EC 3.4.21.6 (coagulation factor Xa) inhibitor |
| sb 3ct compound SB 3CT compound: a matrix metalloproteinase-2 inhibitor; structure in first source | 2.6 | 1 | 0 | aromatic ether | |
| dapagliflozin [no description available] | 4.16 | 1 | 0 | aromatic ether; C-glycosyl compound; monochlorobenzenes | hypoglycemic agent; sodium-glucose transport protein subtype 2 inhibitor |
| ginsenoside rb1 [no description available] | 2.6 | 1 | 0 | ginsenoside; glycoside; tetracyclic triterpenoid | anti-inflammatory drug; anti-obesity agent; apoptosis inhibitor; neuroprotective agent; plant metabolite; radical scavenger |
| perampanel perampanel : A member of the class of bipyridines that is 2,3'-bipyridin-6'-one substituted at positions 1' and 5' by phenyl and 2-cyanophenyl groups respectively. Used as an adjunctive therapy for the treatment of partial-onset seizures in patients with epilepsy. | 2.17 | 1 | 0 | bipyridines; nitrile; pyridone | AMPA receptor antagonist; anticonvulsant |
| rucaparib AG14447: Poly(ADP-ribose) polymerase inhibitor; structure in first source | 2.6 | 1 | 0 | azepinoindole; caprolactams; organofluorine compound; secondary amino compound | antineoplastic agent; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor |
| 6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-n-(4-hydroxyphenyl)-2,3,9-trimethyl-, (6s)- [no description available] | 2.6 | 1 | 0 | organonitrogen heterocyclic compound; organosulfur heterocyclic compound | |
| cetilistat cetilistat: lipase inhibitor in randomized, placebo-controlled study of weight reduction in obese patients (3/2007) | 2.6 | 1 | 0 | benzoxazine | |
| ym 201636 6-amino-N-(3-(4-(4-morpholinyl)pyrido(3',2'-4,5)furo(3,2-d)pyrimidin-2-yl)phenyl)-3-pyridinecarboxamide: an antiviral agent; structure in first source | 2.6 | 1 | 0 | aromatic amide | |
| 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. | 14.82 | 35 | 0 | aminopiperidine; quinazolines | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; hypoglycemic agent |
| azd 6244 AZD 6244: a MEK inhibitor | 2.6 | 1 | 0 | benzimidazoles; bromobenzenes; hydroxamic acid ester; monochlorobenzenes; organofluorine compound; secondary amino compound | anticoronaviral agent; antineoplastic agent; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor |
| odanacatib odanacatib: a selective inhibitor of cathepsin K for the treatment of post-menopausal osteoporosis; structure in first source | 2.6 | 1 | 0 | ||
| apilimod [no description available] | 2.6 | 1 | 0 | ||
| apixaban [no description available] | 2.6 | 1 | 0 | aromatic ether; lactam; piperidones; pyrazolopyridine | anticoagulant; EC 3.4.21.6 (coagulation factor Xa) inhibitor |
| betrixaban betrixaban: a highly potent, selective, and orally efficacious factor Xa inhibitor; structure in first source. betrixaban : A secondary carboxamide obtained by formal condensation of the carboxy group of 4-(N,N-dimethylcarbamimidoyl)benzoic acid with the amino group of 2-amino-N-(5-chloropyridin-2-yl)-5-methoxybenzamide. A synthetic anticoagulant compound that targets activated factor Xa in the coagulation cascade. | 2.6 | 1 | 0 | benzamides; guanidines; monochloropyridine; monomethoxybenzene; secondary carboxamide | anticoagulant; EC 3.4.21.6 (coagulation factor Xa) inhibitor |
| edoxaban edoxaban : A monocarboxylic acid amide that is used (as its tosylate monohydrate) for the treatment of deep vein thrombosis and pulmonary embolism. | 2.6 | 1 | 0 | chloropyridine; monocarboxylic acid amide; tertiary amino compound; thiazolopyridine | anticoagulant; EC 3.4.21.6 (coagulation factor Xa) inhibitor; platelet aggregation inhibitor |
| saracatinib [no description available] | 2.6 | 1 | 0 | aromatic ether; benzodioxoles; diether; N-methylpiperazine; organochlorine compound; oxanes; quinazolines; secondary amino compound | anticoronaviral agent; antineoplastic agent; apoptosis inducer; autophagy inducer; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; radiosensitizing agent |
| n-(3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl)-3-(2-((((1,1-dimethylethyl)amino)carbonyl)amino)-3,3-dimethyl-1-oxobutyl)-6,6-dimethyl-3-azabicyclo(3.1.0)hexan-2-carboxamide boceprevir : A synthetic tripeptide consisting of N-(tert-butylcarbamoyl)-3-methyl-L-valyl, a cyclopropyl-fused prolyl and 3-amino-4-cyclobutyl-2-oxobutanamide residues joined in sequence. Used for treatment of chronic hepatitis C virus genotype 1 infection. | 2.6 | 1 | 0 | tripeptide; ureas | antiviral drug; hepatitis C protease inhibitor; peptidomimetic |
| ly 411575 [no description available] | 2.6 | 1 | 0 | dibenzoazepine; difluorobenzene; lactam; secondary alcohol | EC 3.4.23.46 (memapsin 2) inhibitor |
| galidesivir [no description available] | 2.6 | 1 | 0 | ||
| ipragliflozin [no description available] | 3.51 | 1 | 1 | glycoside | |
| PB28 PB28 : A member of the class of tetralins that is tetralin that is substituted by 3-(4-cyclohexylpiperazin-1-yl)propyl and methoxy groups at positions 1 and 5, respectively. It is a sigma 2 (sigma2) receptor agonist (Ki = 0.68 nM) and exhibits antineoplastic and anti SARS-CoV-2 activities. | 2.6 | 1 | 0 | aromatic ether; piperazines; tetralins | anticoronaviral agent; antineoplastic agent; apoptosis inducer; sigma-2 receptor agonist |
| cariprazine cariprazine: Structure in first source. cariprazine : An N-alkylpiperazine that is N,N-dimethyl-N'-{trans-4-[2-(piperazin-1-yl)ethyl]cyclohexyl}urea substituted at position 4 on the piperazine ring by a 2,3-dichlorophenyl group. Used (as the hydrochloride salt) for treatment of schizophrenia and bipolar disorder. | 3.25 | 1 | 0 | ||
| degrasyn degrasyn: a JAK2 kinase inhibitor that induces rapid degradation of c-Myc protein in MM-1 multiple myeloma and other tumor cell lines; structure in first source | 2.6 | 1 | 0 | ||
| epoxomicin [no description available] | 2.6 | 1 | 0 | morpholines; tripeptide | proteasome inhibitor |
| bms 477118 [no description available] | 5.24 | 8 | 0 | adamantanes; azabicycloalkane; monocarboxylic acid amide; nitrile; tertiary alcohol | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; hypoglycemic agent |
| pha 680632 PHA 680632: Aurora kinase inhibitor with potent antitumoral activity; structure in first source | 2.6 | 1 | 0 | ||
| tmc 353121 [no description available] | 2.6 | 1 | 0 | ||
| dutogliptin [no description available] | 3.16 | 1 | 0 | ||
| amd 070 mavorixafor: a derivative of AMD3100; a CXCR4 blocker | 2.6 | 1 | 0 | aminoquinoline | |
| danoprevir [no description available] | 2.6 | 1 | 0 | ||
| bms-626529 [no description available] | 2.6 | 1 | 0 | ||
| bms-663068 fostemsavir: an HIV-1 attachment inhibitor; structure in first source | 2.6 | 1 | 0 | ||
| amenamevir ASP2151: a herpesvirus helicase-primase inhibitor, in a guinea pig model of genital herpes; structure in first source | 2.6 | 1 | 0 | ||
| vx 765 belnacasan: a NSAID | 2.6 | 1 | 0 | dipeptide | |
| Dihydrotanshinone I dihydrotanshinone I: extracted from Radix Salviae | 2.6 | 1 | 0 | abietane diterpenoid | anticoronaviral agent |
| fr 180204 FR 180204: structure in first source | 2.6 | 1 | 0 | pyrazoles; ring assembly | |
| gosogliptin [no description available] | 3.27 | 1 | 0 | amino acid amide | |
| quisinostat [no description available] | 2.6 | 1 | 0 | indoles | |
| carfilzomib [no description available] | 2.6 | 1 | 0 | epoxide; morpholines; tetrapeptide | antineoplastic agent; proteasome inhibitor |
| hcv 796 HCV 796: inhibits HCV RdRp; structure in first source | 2.6 | 1 | 0 | ||
| sitagliptin phosphate 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. | 13.17 | 49 | 4 | ||
| resminostat resminostat: a histone deacetylase inhibitor; structure in first source | 2.6 | 1 | 0 | ||
| lorcaserin lorcaserin: orally active, small-molecule 5-hydroxytryptamine 2C agonist for the potential treatment of obesity and diabetes. lorcaserin : A benzazepine that is 2,3,4,5-tetrahydro-3-benzazepine substituted at position 1 by a methyl group and a t position 6 by a chloro group. | 2.1 | 1 | 0 | benzazepine; organochlorine compound | anti-obesity agent; appetite depressant |
| zk 756326 2-(2-(4-(3-phenoxybenzyl)piperazin-1-yl)ethoxy)ethanol: a CC chemokine receptor CCR8 agonist; structure in first source | 2.6 | 1 | 0 | aromatic ether | |
| balapiravir balapiravir: a prodrug of R1479; structure in first source | 2.6 | 1 | 0 | ||
| trametinib [no description available] | 2.6 | 1 | 0 | acetamides; aromatic amine; cyclopropanes; organofluorine compound; organoiodine compound; pyridopyrimidine; ring assembly | anticoronaviral agent; antineoplastic agent; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector |
| deoxyarbutin 4-((tetrahydro-2H-pyran-2-yl)oxy)phenol: has antineoplastic activity; structure in first source | 2.6 | 1 | 0 | ||
| abexinostat abexinostat: structure in first source | 2.6 | 1 | 0 | benzofurans | |
| silvestrol silvestrol: isolated from the fruit and twig of Aglaia silvestris. silvestrol : An organic heterotricyclic compound that consists of a 2,3,3a,8b-tetrahydro-H-benzo[b]cyclopenta[d]furan framework substituted by hydroxy groups at positions C-1 and C-8b, a methoxycarbonyl group at C-2, a phenyl group at C-3, a 4-methoxyphenyl group at C-3a, a methoxy group at C-8 and a 1,4-dioxan-2-yloxy group at position C-6 which in turn is substituted by a methoxy group at position 3 and a 1,2-dihydroxyethyl group at position 6. Isolated from Aglaia silvestris, it exhibits antineoplastic activity. | 2.6 | 1 | 0 | dioxanes; ether; methyl ester; organic heterotricyclic compound | antineoplastic agent; metabolite |
| td-5108 TD-5108: a selective 5-HT(4) receptor agonist with high intrinsic activity; structure in first source | 2.11 | 1 | 0 | ||
| narlaprevir narlaprevir: an antiviral agent that inhibits hepatitis C virus NS3 protease. narlaprevir : An azabicyclohexane that is (1R,5S)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane substituted by [(3S)-1-(cyclopropylamino)-1,2-dioxoheptan-3-yl]aminoacyl and N-({1-[(tert-butylsulfonyl)methyl]cyclohexyl}carbamoyl)-3-methyl-L-valyl groups at positions 2S and 3, respectively. It is a hepatitis C virus (HCV) NS3/4A serine protease inhibitor (Ki = 6 nM) that is used for the treatment of chronic hepatitis C. | 2.6 | 1 | 0 | azabicyclohexane; cyclopropanes; pyrrolidinecarboxamide; secondary carboxamide; sulfone; tertiary carboxamide; ureas | anticoronaviral agent; antiviral drug; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor; hepatitis C protease inhibitor |
| empagliflozin [no description available] | 9.89 | 3 | 0 | aromatic ether; C-glycosyl compound; monochlorobenzenes; tetrahydrofuryl ether | hypoglycemic agent; sodium-glucose transport protein subtype 2 inhibitor |
| teneligliptin [no description available] | 4 | 3 | 0 | amino acid amide | |
| lc15-0444 LC15-0444: Dipeptidyl Peptidase IV Inhibitors; orally active small molecule for the treatment of type II diabetes | 3.19 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| dextrothyroxine [no description available] | 2.6 | 1 | 0 | ||
| veliparib [no description available] | 2.6 | 1 | 0 | benzimidazoles | EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor |
| pf 03491390 [no description available] | 2.6 | 1 | 0 | ||
| alloin [no description available] | 2.6 | 1 | 0 | anthracenes; C-glycosyl compound; cyclic ketone; phenols | laxative; metabolite |
| thienopyrimidine thienopyrimidine: structure in first source. thienopyrimidine : A class of aromatic heterobicyclic compounds each of which contains a pyrimidine ring ortho fused to a 5-membered thiophene ring. | 2.06 | 1 | 0 | ||
| mdv 3100 [no description available] | 2.6 | 1 | 0 | (trifluoromethyl)benzenes; benzamides; imidazolidinone; monofluorobenzenes; nitrile; thiocarbonyl compound | androgen antagonist; antineoplastic agent |
| trelagliptin trelagliptin: a dipeptidyl peptidase IV inhibitor | 9.95 | 9 | 3 | benzenes; nitrile | |
| bms-650032 asunaprevir: an NS3 protease inhibitor against hepatitis C virus | 2.6 | 1 | 0 | oligopeptide | |
| rg 7128 2'-fluoro-2'-methyl-3',5'-diisobutyryldeoxycytidine: inhibits HCV polymerase; structure in first source | 2.6 | 1 | 0 | ||
| 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. | 7.75 | 3 | 0 | peptide hormone | |
| angiotensinogen Angiotensinogen: An alpha-globulin of about 453 amino acids, depending on the species. It is produced by the liver in response to lowered blood pressure and secreted into blood circulation. Angiotensinogen is the inactive precursor of the ANGIOTENSINS produced in the body by successive enzyme cleavages. Cleavage of angiotensinogen by RENIN yields the decapeptide ANGIOTENSIN I. Further cleavage of angiotensin I (by ANGIOTENSIN CONVERTING ENZYME) yields the potent vasoconstrictor octapeptide ANGIOTENSIN II; and then, via other enzymes, other angiotensins also involved in the hemodynamic-regulating RENIN-ANGIOTENSIN SYSTEM. | 7.11 | 1 | 0 | ||
| oligonucleotides [no description available] | 2.1 | 1 | 0 | ||
| liraglutide [no description available] | 5.66 | 9 | 0 | lipopeptide; 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. | 11.36 | 36 | 3 | ||
| oritavancin oritavancin : A semisynthetic glycopeptide used (as its bisphosphate salt) for the treatment of acute bacterial skin and skin structure infections caused or suspected to be caused by susceptible isolates of designated Gram-positive microorganisms including MRSA. | 2.6 | 1 | 0 | disaccharide derivative; glycopeptide; semisynthetic derivative | antibacterial drug; antimicrobial agent |
| incretins Incretins: Peptides which stimulate INSULIN release from the PANCREATIC BETA CELLS following oral nutrient ingestion, or postprandially. | 6.99 | 12 | 0 | ||
| 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. | 4.45 | 2 | 2 | ||
| 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 | 2.13 | 1 | 0 | ||
| pevonedistat pevonedistat: a potent and selective inhibitor of NAE (NEDD8-activating enzyme). pevonedistat : A pyrrolopyrimidine that is 7H-pyrrolo[2,3-d]pyrimidine which is substituted by a (1S)-2,3-dihydro-1H-inden-1-ylnitrilo group at position 4 and by a (1S,3S,4S)-3-hydroxy-4-[(sulfamoyloxy)methyl]cyclopentyl group at position 7. It is a potent and selective NEDD8-activating enzyme inhibitor with an IC50 of 4.7 nM, and currently under clinical investigation for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndromes. | 2.6 | 1 | 0 | cyclopentanols; indanes; pyrrolopyrimidine; secondary amino compound; sulfamidate | antineoplastic agent; apoptosis inducer |
| uk 453,061 UK 453,061: a reverse transcriptase inhibitor/anti-HIV agent; structure in first source | 2.6 | 1 | 0 | aromatic ether | |
| N-(2-aminophenyl)-2-pyrazinecarboxamide [no description available] | 2.6 | 1 | 0 | aromatic amide | |
| tegobuvir tegobuvir: a non-structural protein 5B polymerase inhibitor | 2.6 | 1 | 0 | ||
| pf-429242 PF-429242: a subtilisin kexin isozyme-1/site-1 protease inhibitor | 2.6 | 1 | 0 | ||
| olaparib [no description available] | 2.6 | 1 | 0 | cyclopropanes; monofluorobenzenes; N-acylpiperazine; phthalazines | antineoplastic agent; apoptosis inducer; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor |
| cx 4945 [no description available] | 2.6 | 1 | 0 | ||
| pci 34051 PCI 34051: an HDAC8 inhibitor | 2.6 | 1 | 0 | indolecarboxamide | |
| lomibuvir lomibuvir: an antiviral agent with polymerase NS5 inhibitory activity | 2.6 | 1 | 0 | thiophenecarboxylic acid | |
| delanzomib [no description available] | 2.6 | 1 | 0 | C-terminal boronic acid peptide; phenylpyridine; secondary alcohol; threonine derivative | antineoplastic agent; apoptosis inducer; proteasome inhibitor |
| 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. | 4.54 | 2 | 0 | C-glycosyl compound; organofluorine compound; thiophenes | hypoglycemic agent; sodium-glucose transport protein subtype 2 inhibitor |
| pitavastatin(1-) pitavastatin(1-) : A hydroxy monocarboxylic acid anion that is the conjugate base of pitavastatin, obtained by deprotonation of the carboxy group. | 2.6 | 1 | 0 | hydroxy monocarboxylic acid anion | |
| GRL-0617 GRL-0617 : A benzamide resulting from the formal condensation of the carboxy group of 5-amino-2-methylbenzoic acid with the amino group of (1R)-1-(naphthalen-1-yl)ethan-1-amine. It is a potent noncovalent inhibitor (IC50 = 600 nM) of severe acute respiratory syndrome-coronavirus papain-like protease (SARS-CoV PLpro). | 2.6 | 1 | 0 | benzamides; naphthalenes; secondary carboxamide; substituted aniline | anticoronaviral agent; protease inhibitor |
| N-[4-[3-[[[7-(hydroxyamino)-7-oxoheptyl]amino]-oxomethyl]-5-isoxazolyl]phenyl]carbamic acid tert-butyl ester CAY10603: a HDAC6 inhibitor | 2.6 | 1 | 0 | carbamate ester | |
| niraparib niraparib: structure in first source. niraparib : A 2-[4-(piperidin-3-yl)phenyl]-2H-indazole-7-carboxamide that has S-configuration. It is a potent inhibitor of PARP1 and PARP2 (IC50 of 3.8 and 2.1 nM, respectively) and approved as a first-line maintenance treatment for women with advanced ovarian cancer after responding to platinum-based chemotherapy. | 2.6 | 1 | 0 | 2-[4-(piperidin-3-yl)phenyl]-2H-indazole-7-carboxamide | antineoplastic agent; apoptosis inducer; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor; radiosensitizing agent |
| jzl 184 JZL 184: inhibits monoacylglycerol lipase; structure in first source | 2.6 | 1 | 0 | benzodioxoles | |
| gsk 650394 [no description available] | 2.6 | 1 | 0 | phenylpyridine | |
| oprozomib ONX 0912: antineoplastic; an orally active proteasome inhibitor; structure in first source | 2.6 | 1 | 0 | ||
| az 960 [no description available] | 2.6 | 1 | 0 | ||
| golgicide a golgicide A: inhibits the cis-golgi ArfGEF GBF1; structure in first source. golgicide A : A diastereoisomeric mixture comprising racemic cis- and racemic trans-goglioside A in a 10:1 ratio. It is a potent and rapidly reversible GBF1 (Golgi-specific brefeldin A-resistance guanine nucleotide exchange factor 1) inhibitor. The (3aS,4R,9bR) isomer is the most active (see Bioorg. Med. Chem. Lett., 2012, 22, 5177-5181). | 2.6 | 1 | 0 | diastereoisomeric mixture | cis-Golgi ArfGEF GBF inhibitor |
| cobicistat [no description available] | 2.6 | 1 | 0 | 1,3-thiazoles; carbamate ester; monocarboxylic acid amide; morpholines; ureas | P450 inhibitor |
| bms-790052 daclatasvir: an HCV NS5A inhibitor. daclatasvir : A member of the class of biphenyls that is a potent inhibitor of nonstructural protein 5A and is used (as its hydrochloride salt) for treatment of hepatitis C. | 2.6 | 1 | 0 | biphenyls; carbamate ester; carboxamide; imidazoles; valine derivative | antiviral drug; nonstructural protein 5A inhibitor |
| ixazomib ixazomib: a proteasome inhibitor with antineoplastic activity; MLN2238 is the biologically active form of MLN9708; structure in first source. ixazomib : A glycine derivative that is the amide obtained by formal condensation of the carboxy group of N-(2,5-dichlorobenzoyl)glycine with the amino group of [(1R)-1-amino-3-methylbutyl]boronic acid. The active metabolite of ixazomib citrate, it is used in combination therapy for treatment of multiple myeloma. | 2.6 | 1 | 0 | benzamides; boronic acids; dichlorobenzene; glycine derivative | antineoplastic agent; apoptosis inducer; drug metabolite; orphan drug; proteasome inhibitor |
| ucph 101 2-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile: structure in first source | 2.6 | 1 | 0 | ||
| plx4032 [no description available] | 3.18 | 1 | 0 | aromatic ketone; difluorobenzene; monochlorobenzenes; pyrrolopyridine; sulfonamide | antineoplastic agent; B-Raf inhibitor |
| 5-(3-methylsulfonylphenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidine [no description available] | 2.6 | 1 | 0 | aryl sulfide; thienopyrimidine | |
| baricitinib [no description available] | 2.6 | 1 | 0 | azetidines; nitrile; pyrazoles; pyrrolopyrimidine; sulfonamide | anti-inflammatory agent; antirheumatic drug; antiviral agent; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; immunosuppressive agent |
| KOM70144 KOM70144 : A benzamide that is GRL-0617 in which one of the hydrogen's of the primary amino group is replaced by an acetyl group. It an inhibitor of SARS-CoV and SARS-CoV-2 papain-like protease (PLpro) with an IC50 of 2.6 muM and 5.0 muM, respectively. It also inhibits SARS-CoV and SARS-CoV-2 infection of Vero E6 cells in vitro (EC50 values are 13.1 and 21 muM, respectively). | 2.6 | 1 | 0 | acetamides; benzamides; naphthalenes; secondary carboxamide | anticoronaviral agent; protease inhibitor |
| piperidines Piperidines: A family of hexahydropyridines. | 21.24 | 272 | 80 | ||
| e-52862 [no description available] | 2.6 | 1 | 0 | ||
| ly2811376 [no description available] | 2.6 | 1 | 0 | ||
| anagliptin anagliptin: anagliptin hydrochloride salt is the active compound | 11.26 | 5 | 1 | amino acid amide | |
| gardiquimod [no description available] | 2.6 | 1 | 0 | ||
| grazoprevir grazoprevir: has antiviral activity; component of Zepatier. grazoprevir : An azamacrocyclic compound that is a hepatitis C protease inhibitor used in combination with elbasvir (under the brand name Zepatier) for treatment of chronic HCV genotypes 1 or 4 infection in adults. | 2.6 | 1 | 0 | aromatic ether; azamacrocycle; carbamate ester; cyclopropanes; lactam; N-sulfonylcarboxamide; quinoxaline derivative | antiviral drug; hepatitis C protease inhibitor; hepatoprotective agent |
| abt-450 paritaprevir: inhibits HCV NS3 protease. paritaprevir : An azamacrocycle which is used which is in combination with dasabuvir sodium hydrate, ombitasvir and ritonavir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver. | 2.6 | 1 | 0 | ||
| letermovir letermovir: has antiviral activity; structure in first source | 2.6 | 1 | 0 | ||
| 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. | 2.6 | 1 | 0 | isopropyl ester; L-alanyl ester; nucleotide conjugate; organofluorine compound; phosphoramidate ester | antiviral drug; hepatitis C protease inhibitor; prodrug |
| 5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine sapanisertib: an mTOR inhibitor | 2.6 | 1 | 0 | benzoxazole | |
| 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. | 6.55 | 9 | 0 | ||
| blz 945 [no description available] | 2.6 | 1 | 0 | ||
| azd3839 AZD3839: a BACE1 inhibitor; structure in first source | 2.6 | 1 | 0 | ||
| mk-3102 [no description available] | 3.27 | 1 | 0 | pyrrolopyrazole | |
| pf 3084014 nirogacestat: an antineoplastic agent. nirogacestat : A member of the class of imidazoles that is 1H-imidazole substituted by a 1-[(2,2-dimethylpropyl)amino]-2-methylpropan-2-yl group at position 1 and a {N-[(2S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]-L-norvalyl}amino group at position 4. It is a gamma-secretase inhibitor whose hydrobromide salt is indicated for adult patients with progressing desmoid tumours who require systemic treatment. | 2.6 | 1 | 0 | ||
| unc 0638 UNC 0638: inhibits lysine methyltransferases G9a and GLP; structure in first source | 2.6 | 1 | 0 | quinazolines | |
| gs-9620 [no description available] | 2.6 | 1 | 0 | ||
| n-((5-(methanesulfonyl)pyridin-2-yl)methyl)-6-methyl-5-(1-methyl-1h-pyrazol-5-yl)-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamide N-((5-(methanesulfonyl)pyridin-2-yl)methyl)-6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamide: structure in first source | 2.6 | 1 | 0 | ||
| bms 708163 BMS 708163: structure in first source | 2.6 | 1 | 0 | oxadiazole; ring assembly | |
| jq1 compound [no description available] | 2.6 | 1 | 0 | carboxylic ester; organochlorine compound; tert-butyl ester; thienotriazolodiazepine | angiogenesis inhibitor; anti-inflammatory agent; antineoplastic agent; apoptosis inducer; bromodomain-containing protein 4 inhibitor; cardioprotective agent; ferroptosis inducer |
| 1-(5-((2,4-difluorophenyl)thio)-4-nitrothiophen-2-yl)ethanone 1-(5-((2,4-difluorophenyl)thio)-4-nitrothiophen-2-yl)ethanone: a USP7 inhibitor; structure in first source | 2.6 | 1 | 0 | ||
| gsk525762a molibresib: mimicks acetylated histones; structure in first source | 2.6 | 1 | 0 | benzodiazepine | |
| ML240 ML240 : A member of the class of quinazolines that is quinazoline which is substituted at positions 2, 5 and 8 by 2-amino-1H-benzimidazol-1-yl, benzylnitrilo and methoxy groups, respectively. It is a ATP-competetive inhibitor of AAA ATPase p97, also known as valosin-containing protein (VCP). | 2.6 | 1 | 0 | aromatic amine; aromatic ether; benzimidazoles; primary amino compound; quinazolines; secondary amino compound | antineoplastic agent |
| birinapant birinapant: a Smac mimetic with antineoplastic activity | 2.6 | 1 | 0 | dipeptide | |
| ly2886721 [no description available] | 2.6 | 1 | 0 | ||
| nms-p118 NMS-P118: a PARP-1 inhibitor; structure in first source | 2.6 | 1 | 0 | ||
| tubastatin a [no description available] | 2.6 | 1 | 0 | hydroxamic acid; pyridoindole; tertiary amino compound | EC 3.5.1.98 (histone deacetylase) inhibitor |
| pracinostat pracinostat : A hydroxamic acid that is N-hydroxyacrylamide which is substituted at position 3 by a 2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl group (the E isomer). An orally available pan-histone deacetylase inhibitor with demonstrated activity in the treatment of advanced solid tumours. | 2.6 | 1 | 0 | benzimidazole; hydroxamic acid; olefinic compound; tertiary amino compound | antimalarial; antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor |
| spautin-1 [no description available] | 2.6 | 1 | 0 | ||
| ldn 57444 LDN 57444: inhibitor of ubiquitin C-terminal hydrolase-L1; structure in first source | 2.6 | 1 | 0 | ||
| gsk1210151a GSK1210151A: inhibitor of the BET family of proteins; structure in first source | 2.6 | 1 | 0 | imidazoquinoline | |
| i-bet726 [no description available] | 2.6 | 1 | 0 | ||
| 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. | 6.75 | 4 | 3 | polypeptide | |
| acy-1215 ricolinostat: an HDAC6 inhibitor; structure in first source | 2.6 | 1 | 0 | pyrimidinecarboxylic acid | |
| cudc-907 [no description available] | 2.6 | 1 | 0 | ||
| mobic Meloxicam: A benzothiazine and thiazole derivative that acts as a NSAID and cyclooxygenase-2 (COX-2) inhibitor. It is used in the treatment of RHEUMATOID ARTHRITIS; OSTEOARTHRITIS; and ANKYLOSING SPONDYLITIS.. meloxicam : A benzothiazine that is piroxicam in which the pyridin-2-yl group is replaced by a 5-methyl-1,3-thiazol-2-yl group. A non-steroidal anti-inflammatory drug and selective inhibitor of COX-2, it is used particularly for the management of rheumatoid arthritis. | 2.6 | 1 | 0 | 1,3-thiazoles; benzothiazine; monocarboxylic acid amide | analgesic; antirheumatic drug; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| tipranavir tipranavir: inhibits HIV-1 protease. tipranavir : A pyridine-2-sulfonamide substituted at C-5 by a trifluoromethyl group and at the sulfonamide nitrogen by a dihydropyrone-containing m-tolyl substituent. It is an HIV-1 protease inhibitor. | 2.6 | 1 | 0 | sulfonamide | antiviral drug; HIV protease inhibitor |
| tasquinimod tasquinimod: a lead second generation quinoline-3-carboxamide anti-angiogenic agent for the treatment of prostate cancer; structure in first source | 2.6 | 1 | 0 | ||
| gsk1265744 [no description available] | 2.6 | 1 | 0 | difluorobenzene; monocarboxylic acid amide; organic heterotricyclic compound; secondary carboxamide | HIV-1 integrase inhibitor |
| abt-267 ombitasvir: inhibits HCV NS5A protein, component of Viekirax. ombitasvir : A dipeptide derivative which is used which is in combination with dasabuvir sodium hydrate, paritaprevir and ritonavir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver. | 2.6 | 1 | 0 | aromatic amide; carbamate ester; dipeptide; pyrrolidines | antiviral drug; hepatitis C virus nonstructural protein 5A inhibitor |
| abt-333 dasabuvir: an antiviral agent. dasabuvir : A member of the class of pyrimidone, which is (as the monohydrate of its sodium salt) in combination with ombitasvir, paritaprevir and ritonavir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver. | 2.6 | 1 | 0 | aromatic ether; naphthalenes; pyrimidone; sulfonamide | antiviral drug; nonnucleoside hepatitis C virus polymerase inhibitor |
| rgfp966 [no description available] | 2.6 | 1 | 0 | ||
| rg2833 RG2833: a histone deacetylase inhibitor; structure in first source | 2.6 | 1 | 0 | ||
| 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. | 2.58 | 2 | 0 | ||
| pi-1840 PI-1840: has both antineoplastic and proteasome inhibitory activities; structure in first source | 2.6 | 1 | 0 | ||
| acy-738 [no description available] | 2.6 | 1 | 0 | ||
| pelabresib CPI-0610: a bromodomain and extra-terminal protein inhibitor with antineoplastic activity; structure in first source | 2.6 | 1 | 0 | monochlorobenzenes; organic heterotricyclic compound; primary carboxamide | antineoplastic agent; bromodomain-containing protein 4 inhibitor |
| gs-5806 presatovir: a respiratory syncytial virus entry inhibitor | 2.6 | 1 | 0 | ||
| doravirine [no description available] | 2.6 | 1 | 0 | ||
| gn6958 GN6958: inhibits SUMO-sentrin specific protease 1 (SENP1); structure in first source | 2.6 | 1 | 0 | ||
| vx-787 pimodivir: non‐nucleotide inhibitor of the polymerase basic protein 2 (PB2) subunit of the influenza A that is active against H1N1, H7N9 and H5N1, as well as influenza A strains with reduced susceptibility to NAIs | 2.6 | 1 | 0 | ||
| ledipasvir ledipasvir : A benzimidazole derivative that is used in combination with sofosbuvir (under the trade name Harvoni) for the treatment of chronic hepatitis C genotype 1 infection. | 2.6 | 1 | 0 | azaspiro compound; benzimidazole; bridged compound; carbamate ester; carboxamide; fluorenes; imidazoles; L-valine derivative; N-acylpyrrolidine; organofluorine compound | antiviral drug; hepatitis C protease inhibitor |
| gs-5816 velpatasvir: an NS5A inhibitor used for treating hepatitis C infections. velpatasvir : A complex organic heteropentacyclic compound that is a hepatitis C virus nonstructural protein 5A inhibitor used in combination with sofosbuvir (under the brand name Epclusa) for treatment of patients with chronic hepatitis C of all six major genotypes. | 2.6 | 1 | 0 | carbamate ester; ether; imidazoles; L-valine derivative; N-acylpyrrolidine; organic heteropentacyclic compound; ring assembly | antiviral drug; hepatitis C virus nonstructural protein 5A inhibitor |
| g007-lk G007-LK: potent and specific small-molecule tankyrase inhibitor; structure in first source | 2.6 | 1 | 0 | ||
| 4-((1-butyl-3-phenylureido)methyl)-n-hydroxybenzamide 4-((1-butyl-3-phenylureido)methyl)-N-hydroxybenzamide: inhibits HDAC6; structure in first source | 2.6 | 1 | 0 | ||
| selinexor selinexor: inhibits karyopherin XPO1 | 2.6 | 1 | 0 | ||
| verdinexor verdinexor: a selective inhibitor of nuclear export | 2.6 | 1 | 0 | ||
| cb-839 [no description available] | 2.6 | 1 | 0 | ||
| mk-8742 elbasvir: inhibits NS5A protein of hepatitis C virus. elbasvir : A complex organic heterotetracyclic compound that is a hepatitis C virus nonstructural protein 5A inhibitor used in combination with grazoprevir (under the brand name Zepatier) for treatment of chronic HCV genotypes 1 or 4 infection in adults. | 2.6 | 1 | 0 | carbamate ester; imidazoles; L-valine derivative; N-acylpyrrolidine; organic heterotetracyclic compound; ring assembly | antiviral drug; hepatitis C virus nonstructural protein 5A inhibitor; hepatoprotective agent |
| atglistatin atglistatin: inhibits adipose triglyceride lipase; structure in first source. atglistatin : A biphenyl that is 1,1'-biphenyl substituted by (dimethylcarbamoyl)amino and dimethylamino groups at positions 3 and 4', respectively. It is a potent inhibitor of adipose triglyceride lipase activity (IC50 = 700nM). | 2.6 | 1 | 0 | ||
| xen445 [no description available] | 2.6 | 1 | 0 | ||
| santacruzamate a santacruzamate A: HDAC2 inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp.; structure in first source | 2.6 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| ldc4297 LDC4297: a CDK7 inhibitor with antineoplastic activity; structure in first source. LDC4297 : A pyrazolotriazine that is pyrazolo[1,5-a][1,3,5]triazine substituted by a piperidin-3-yloxy group, [2-(1H-pyrazol-1-yl)benzyl]nitrilo group and an isopropyl group at positions 2, 4 and 8 respectively. It is a potent and selective CDK7 inhibitor and exhibits antiviral activity. | 2.6 | 1 | 0 | aromatic ether; piperidines; pyrazoles; pyrazolotriazine; secondary amino compound | antineoplastic agent; antiviral agent; apoptosis inducer; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor |
| enasidenib [no description available] | 2.6 | 1 | 0 | 1,3,5-triazines; aminopyridine; aromatic amine; organofluorine compound; secondary amino compound; tertiary alcohol | antineoplastic agent; EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor |
| insulin glargine Insulin Glargine: A recombinant LONG ACTING INSULIN and HYPOGLYCEMIC AGENT that is used to manage BLOOD GLUCOSE in patients with DIABETES MELLITUS. | 2.06 | 1 | 0 | ||
| s 8932 [no description available] | 2.6 | 1 | 0 | aromatic amine; C-nucleoside; carboxylic ester; nitrile; phosphoramidate ester; pyrrolotriazine | anticoronaviral agent; antiviral drug; prodrug |
| 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. | 3.18 | 1 | 0 | ||
| entecavir entecavir (anhydrous) : Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus. Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it has no activity against HIV. It is used for the treatment of chronic hepatitis B. | 2.6 | 1 | 0 | 2-aminopurines; oxopurine; primary alcohol; secondary alcohol | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| acyclovir Acyclovir: A GUANOSINE analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes.. acyclovir : An oxopurine that is guanine substituted by a (2-hydroxyethoxy)methyl substituent at position 9. Used in the treatment of viral infections. | 2.6 | 1 | 0 | 2-aminopurines; oxopurine | antimetabolite; antiviral drug |
| nu 1025 NU 1064: structure in first source | 2.6 | 1 | 0 | phenols; quinazolines | EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor |
| deoxyguanosine [no description available] | 4.16 | 3 | 1 | purine 2'-deoxyribonucleoside; purines 2'-deoxy-D-ribonucleoside | Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| didanosine Didanosine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite.. didanosine : A purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen. An antiviral drug, it is used as a medication to treat HIV/AIDS. | 2.6 | 1 | 0 | purine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor; geroprotector; HIV-1 reverse transcriptase inhibitor |
| ganciclovir [no description available] | 2.6 | 1 | 0 | 2-aminopurines; oxopurine | antiinfective agent; antiviral drug |
| valacyclovir Valacyclovir: A prodrug of acyclovir that is used in the treatment of HERPES ZOSTER and HERPES SIMPLEX VIRUS INFECTION of the skin and mucous membranes, including GENITAL HERPES. | 2.6 | 1 | 0 | L-valyl ester | antiviral drug |
| penciclovir penciclovir : A member of the class of 2-aminopurines that is guanine in which the hydrogen at position 9 is substituted by a 4-hydroxy-3-(hydroxymethyl)but-1-yl group. An antiviral drug, it is administered topically for treatment of herpes labialis. A prodrug, famciclovir, is used for oral administration. | 2.6 | 1 | 0 | 2-aminopurines; propane-1,3-diols | antiviral drug |
| 4-hydroxyquinazoline 4-oxo-3,4-dihydroquinazoline: structure in first source | 2.6 | 1 | 0 | quinazolines | |
| tegaserod tegaserod: a nonbenzamide 5-hydroxytryptamine(4) agonist; used in treatment of irritable bowel syndrome; marketing suspended 2007 in US due to higher incidence of MI, stroke, and unstable angina; structure given in first source | 2.6 | 1 | 0 | carboxamidine; guanidines; hydrazines; indoles | gastrointestinal drug; serotonergic agonist |
| norclozapine norclozapine: structure given in first source. N-desmethylclozapine : A dibenzodoazepine substituted with chloro and piperazino groups which is a major metabolite of clozapine; a potent and selective 5-HT2C serotonin receptor antagonist. | 2.6 | 1 | 0 | dibenzodiazepine; organochlorine compound; piperazines | delta-opioid receptor agonist; metabolite; serotonergic antagonist |
| pemetrexed pemetrexed disodium : An organic sodium salt that is the disodium salt of N-{4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L-glutamic acid. Inhibits thymidylate synthase (TS), 421 dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT). | 2.6 | 1 | 0 | N-acyl-L-glutamic acid; pyrrolopyrimidine | antimetabolite; antineoplastic agent; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; EC 2.1.1.45 (thymidylate synthase) inhibitor; EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor |
| 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. | 2.6 | 1 | 0 | (trifluoromethyl)benzenes; cyclic acetal; morpholines; triazoles | antidepressant; antiemetic; neurokinin-1 receptor antagonist; peripheral nervous system drug; substance P receptor antagonist |
| azilsartan azilsartan: an angiotensin type 1 receptor blocker; receptor blocker. azilsartan : A benzimidazolecarboxylic acid that is benzimidazole-7-carboxylic acid substituted at position 2 by a methoxy group and at position 1 by a 2'-[(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl group. Used (as the prodrug, azilsartan medoxomil) for treatment of hypertension. | 2.6 | 1 | 0 | 1,2,4-oxadiazole; aromatic ether; benzimidazolecarboxylic acid | angiotensin receptor antagonist; antihypertensive agent |
| hesperadin [no description available] | 2.6 | 1 | 0 | ||
| 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. | 4.16 | 3 | 1 | guanosines | biomarker |
| 6-bromoindirubin-3'-acetoxime 6-bromoindirubin-3'-acetoxime: a synthetic derivative of a compound from the Mediterranean mollusk Hexaplex trunculus, protects cells from varicella infection | 2.6 | 1 | 0 | ||
| n'-(3,4-dihydroxybenzylidene)-3-hydroxy-2-naphthahydrazide [no description available] | 2.6 | 1 | 0 | catechols; hydrazide; hydrazone; naphthols | EC 3.6.5.5 (dynamin GTPase) inhibitor |
| XL413 XL413 : A benzofuropyrimidine that is 3,4-dihydro[1]benzofuro[3,2-d]pyrimidine substituted by (2S)-pyrrolidin-2-yl, oxo and chloro groups at positions 2, 4, and 8, respectively. It is a potent ATP competitive inhibitor of Cdc7 kinase (IC50 = 3.4 nM) and exhibits anticancer properties. | 2.6 | 1 | 0 | benzofuropyrimidine; organochlorine compound; pyrrolidines | antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor |
| me0328 ME0328: inhibits ARTD3; structure in first source | 2.6 | 1 | 0 | ||
| nvp-tnks656 [no description available] | 2.6 | 1 | 0 | ||
| pyrimidinones Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O. | 2.03 | 1 | 0 |
| Condition | Indicated | Relationship Strength | Studies | Trials |
|---|---|---|---|---|
| Alloxan Diabetes [description not available] | 0 | 4.3 | 17 | 0 |
| Diabetes Mellitus, Adult-Onset [description not available] | 0 | 21.29 | 220 | 78 |
| 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. | 1 | 23.29 | 220 | 78 |
| Weight Reduction [description not available] | 0 | 5.12 | 3 | 1 |
| Weight Gain Increase in BODY WEIGHT over existing weight. | 0 | 8.99 | 8 | 5 |
| Weight Loss Decrease in existing BODY WEIGHT. | 0 | 5.12 | 3 | 1 |
| Acute Coronary Syndrome An episode of MYOCARDIAL ISCHEMIA that generally lasts longer than a transient anginal episode that ultimately may lead to MYOCARDIAL INFARCTION. | 0 | 10.3 | 14 | 13 |
| Autosomal Dominant Juvenile Parkinson Disease [description not available] | 0 | 2.31 | 1 | 0 |
| 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. | 0 | 2.31 | 1 | 0 |
| Cirrhosis [description not available] | 0 | 3.27 | 5 | 0 |
| Fibrosis Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury. | 0 | 3.27 | 5 | 0 |
| Coronary Heart Disease [description not available] | 0 | 9.72 | 1 | 1 |
| 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. | 0 | 4.72 | 1 | 1 |
| Autoimmune Disease [description not available] | 0 | 3.8 | 1 | 1 |
| 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. | 0 | 3.8 | 1 | 1 |
| Diabetic Glomerulosclerosis [description not available] | 0 | 6.37 | 4 | 2 |
| Diabetes Mellitus A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE. | 1 | 6.63 | 5 | 1 |
| 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. | 0 | 6.37 | 4 | 2 |
| Mucositis, Oral [description not available] | 0 | 2.6 | 1 | 0 |
| Stomatitis INFLAMMATION of the soft tissues of the MOUTH, such as MUCOSA; PALATE; GINGIVA; and LIP. | 0 | 7.6 | 1 | 0 |
| Insulin Sensitivity [description not available] | 0 | 13.29 | 11 | 4 |
| 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. | 0 | 8.29 | 11 | 4 |
| Fasting Hypoglycemia HYPOGLYCEMIA expressed in the postabsorptive state, after prolonged FASTING, or an overnight fast. | 0 | 12.25 | 19 | 14 |
| 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. | 0 | 12.25 | 19 | 14 |
| 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) | 0 | 2.58 | 2 | 0 |
| Pemphigoid [description not available] | 0 | 3.13 | 4 | 0 |
| Pemphigoid, Bullous A chronic and relatively benign subepidermal blistering disease usually of the elderly and without histopathologic acantholysis. | 0 | 3.13 | 4 | 0 |
| Cardiac Failure [description not available] | 0 | 11.27 | 15 | 5 |
| 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. | 0 | 11.27 | 15 | 5 |
| Benign Neoplasms [description not available] | 0 | 3.17 | 1 | 0 |
| 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. | 0 | 3.17 | 1 | 0 |
| Cancer of Colon [description not available] | 0 | 2.25 | 1 | 0 |
| Allodynia [description not available] | 0 | 2.25 | 1 | 0 |
| Peripheral Nerve Diseases [description not available] | 0 | 2.25 | 1 | 0 |
| Colonic Neoplasms Tumors or cancer of the COLON. | 0 | 2.25 | 1 | 0 |
| Peripheral Nervous System Diseases Diseases of the peripheral nerves external to the brain and spinal cord, which includes diseases of the nerve roots, ganglia, plexi, autonomic nerves, sensory nerves, and motor nerves. | 0 | 2.25 | 1 | 0 |
| Cardiovascular Stroke [description not available] | 0 | 10.04 | 10 | 9 |
| Myocardial Infarction NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION). | 0 | 10.04 | 10 | 9 |
| Acute Confusional Senile Dementia [description not available] | 0 | 2.58 | 2 | 0 |
| Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases. | 0 | 6.25 | 19 | 0 |
| 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) | 0 | 2.58 | 2 | 0 |
| Innate Inflammatory Response [description not available] | 0 | 3.74 | 3 | 0 |
| 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. | 0 | 3.74 | 3 | 0 |
| Pulmonary Arterial Remodeling [description not available] | 0 | 2.25 | 1 | 0 |
| Blood Pressure, High [description not available] | 0 | 5.45 | 4 | 1 |
| 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. | 0 | 5.45 | 4 | 1 |
| Apoplexy [description not available] | 0 | 7.58 | 6 | 5 |
| 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) | 0 | 7.58 | 6 | 5 |
| Cognitive Decline [description not available] | 0 | 2.31 | 1 | 0 |
| Cognitive Dysfunction Diminished or impaired mental and/or intellectual function. | 0 | 2.31 | 1 | 0 |
| Hepatocellular Carcinoma [description not available] | 0 | 7.31 | 1 | 0 |
| Cancer of Liver [description not available] | 0 | 2.31 | 1 | 0 |
| 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. | 0 | 2.31 | 1 | 0 |
| Liver Neoplasms Tumors or cancer of the LIVER. | 0 | 2.31 | 1 | 0 |
| 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. | 0 | 2.31 | 1 | 0 |
| 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. | 0 | 2.31 | 1 | 0 |
| Polycystic Ovarian Syndrome [description not available] | 0 | 3.53 | 1 | 1 |
| Prediabetes [description not available] | 0 | 4.39 | 4 | 1 |
| 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). | 0 | 5.66 | 6 | 1 |
| 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. | 0 | 3.53 | 1 | 1 |
| 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). | 0 | 4.39 | 4 | 1 |
| Atrial Remodeling Long-term changes in the electrophysiological parameters and/or anatomical structures of the HEART ATRIA that result from prolonged changes in atrial rate, often associated with ATRIAL FIBRILLATION or long periods of intense EXERCISE. | 0 | 7.15 | 1 | 0 |
| Auricular Fibrillation [description not available] | 0 | 2.53 | 2 | 0 |
| 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. | 0 | 2.53 | 2 | 0 |
| Injury, Myocardial Reperfusion [description not available] | 0 | 2.53 | 2 | 0 |
| Diabetic Angiopathies VASCULAR DISEASES that are associated with DIABETES MELLITUS. | 0 | 8.56 | 7 | 5 |
| Hyperglycemia, Postprandial Abnormally high BLOOD GLUCOSE level after a meal. | 0 | 9.99 | 13 | 7 |
| Hyperglycemia Abnormally high BLOOD GLUCOSE level. | 0 | 9.99 | 13 | 7 |
| Fatty Liver, Nonalcoholic [description not available] | 0 | 2.58 | 2 | 0 |
| Cirrhosis, Liver [description not available] | 0 | 2.59 | 2 | 0 |
| 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. | 0 | 2.59 | 2 | 0 |
| Non-alcoholic Fatty Liver Disease Fatty liver finding without excessive ALCOHOL CONSUMPTION. | 0 | 7.58 | 2 | 0 |
| Recrudescence [description not available] | 0 | 4.84 | 2 | 1 |
| Cardiovascular Diseases Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM. | 0 | 11.34 | 19 | 7 |
| Heart Disease, Ischemic [description not available] | 0 | 4.48 | 1 | 1 |
| 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). | 0 | 4.48 | 1 | 1 |
| 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. | 0 | 7.55 | 6 | 5 |
| Acute Liver Injury, Drug-Induced [description not available] | 0 | 2.17 | 1 | 0 |
| Encephalopathy, Hepatic [description not available] | 0 | 2.17 | 1 | 0 |
| Age-Related Memory Disorders [description not available] | 0 | 2.17 | 1 | 0 |
| Hepatic Encephalopathy A syndrome characterized by central nervous system dysfunction in association with LIVER FAILURE, including portal-systemic shunts. Clinical features include lethargy and CONFUSION (frequently progressing to COMA); ASTERIXIS; NYSTAGMUS, PATHOLOGIC; brisk oculovestibular reflexes; decorticate and decerebrate posturing; MUSCLE SPASTICITY; and bilateral extensor plantar reflexes (see REFLEX, BABINSKI). ELECTROENCEPHALOGRAPHY may demonstrate triphasic waves. (From Adams et al., Principles of Neurology, 6th ed, pp1117-20; Plum & Posner, Diagnosis of Stupor and Coma, 3rd ed, p222-5) | 0 | 7.17 | 1 | 0 |
| 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. | 0 | 2.17 | 1 | 0 |
| 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. | 0 | 2.17 | 1 | 0 |
| Cerebral Infarction, Middle Cerebral Artery [description not available] | 0 | 2.21 | 1 | 0 |
| Cerebral Ischemia [description not available] | 0 | 7.53 | 2 | 0 |
| 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. | 0 | 2.53 | 2 | 0 |
| Infarction, Middle Cerebral Artery NECROSIS occurring in the MIDDLE CEREBRAL ARTERY distribution system which brings blood to the entire lateral aspects of each CEREBRAL HEMISPHERE. Clinical signs include impaired cognition; APHASIA; AGRAPHIA; weak and numbness in the face and arms, contralaterally or bilaterally depending on the infarction. | 0 | 2.21 | 1 | 0 |
| Left Ventricular Hypertrophy [description not available] | 0 | 2.17 | 1 | 0 |
| Left Ventricular Dysfunction [description not available] | 0 | 2.17 | 1 | 0 |
| Cardiac Remodeling, Ventricular [description not available] | 0 | 2.55 | 2 | 0 |
| 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. | 0 | 2.17 | 1 | 0 |
| 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. | 0 | 2.17 | 1 | 0 |
| Dizzyness [description not available] | 0 | 3.47 | 1 | 1 |
| Bilateral Headache [description not available] | 0 | 3.47 | 1 | 1 |
| Dizziness An imprecise term which may refer to a sense of spatial disorientation, motion of the environment, or lightheadedness. | 0 | 3.47 | 1 | 1 |
| 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. | 0 | 3.47 | 1 | 1 |
| Anterior Cerebral Circulation Infarction [description not available] | 0 | 2.08 | 1 | 0 |
| Brain Swelling [description not available] | 0 | 2.08 | 1 | 0 |
| Nervous System Disorders [description not available] | 0 | 2.08 | 1 | 0 |
| Brain Edema Increased intracellular or extracellular fluid in brain tissue. Cytotoxic brain edema (swelling due to increased intracellular fluid) is indicative of a disturbance in cell metabolism, and is commonly associated with hypoxic or ischemic injuries (see HYPOXIA, BRAIN). An increase in extracellular fluid may be caused by increased brain capillary permeability (vasogenic edema), an osmotic gradient, local blockages in interstitial fluid pathways, or by obstruction of CSF flow (e.g., obstructive HYDROCEPHALUS). (From Childs Nerv Syst 1992 Sep; 8(6):301-6) | 0 | 2.08 | 1 | 0 |
| 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. | 0 | 2.08 | 1 | 0 |
| Brain Infarction Tissue NECROSIS in any area of the brain, including the CEREBRAL HEMISPHERES, the CEREBELLUM, and the BRAIN STEM. Brain infarction is the result of a cascade of events initiated by inadequate blood flow through the brain that is followed by HYPOXIA and HYPOGLYCEMIA in brain tissue. Damage may be temporary, permanent, selective or pan-necrosis. | 0 | 2.08 | 1 | 0 |
| Disease Exacerbation [description not available] | 0 | 6.27 | 5 | 1 |
| Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms. | 0 | 10.79 | 15 | 6 |
| Complications of Diabetes Mellitus [description not available] | 0 | 5.08 | 3 | 1 |
| Chronic Kidney Diseases [description not available] | 0 | 6.12 | 6 | 1 |
| 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) | 0 | 6.12 | 6 | 1 |
| Adverse Drug Event [description not available] | 0 | 3.47 | 1 | 1 |
| 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. | 0 | 3.47 | 1 | 1 |
| Abdominal Aortic Aneurysm [description not available] | 0 | 7.1 | 1 | 0 |
| Dilatation, Pathologic The condition of an anatomical structure's being dilated beyond normal dimensions. | 0 | 2.1 | 1 | 0 |
| 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. | 0 | 2.1 | 1 | 0 |
| Atherogenesis [description not available] | 0 | 6.56 | 6 | 3 |
| Atherosclerosis A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA. | 0 | 6.56 | 6 | 3 |
| 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. | 0 | 2.08 | 1 | 0 |
| Injuries, Spinal Cord [description not available] | 0 | 2.08 | 1 | 0 |
| Cicatrix The fibrous tissue that replaces normal tissue during the process of WOUND HEALING. | 0 | 2.08 | 1 | 0 |
| Spinal Cord Injuries Penetrating and non-penetrating injuries to the spinal cord resulting from traumatic external forces (e.g., WOUNDS, GUNSHOT; WHIPLASH INJURIES; etc.). | 0 | 2.08 | 1 | 0 |
| Angina at Rest [description not available] | 0 | 6.48 | 3 | 3 |
| Angina, Unstable Precordial pain at rest, which may precede a MYOCARDIAL INFARCTION. | 0 | 6.48 | 3 | 3 |
| Acute Kidney Failure [description not available] | 0 | 3 | 1 | 0 |
| Injury, Ischemia-Reperfusion [description not available] | 0 | 3 | 1 | 0 |
| Reperfusion Injury Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA. | 0 | 3 | 1 | 0 |
| 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. | 0 | 3 | 1 | 0 |
| Albuminuria The presence of albumin in the urine, an indicator of KIDNEY DISEASES. | 0 | 8.48 | 1 | 1 |
| MS (Multiple Sclerosis) [description not available] | 0 | 2.1 | 1 | 0 |
| Dyspareunia Recurrent genital pain occurring during, before, or after SEXUAL INTERCOURSE in either the male or the female. | 0 | 2.1 | 1 | 0 |
| 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) | 0 | 2.1 | 1 | 0 |
| 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. | 0 | 3.01 | 1 | 0 |
| 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. | 0 | 3.01 | 1 | 0 |
| Acute Edematous Pancreatitis [description not available] | 0 | 5.68 | 3 | 2 |
| 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. | 0 | 5.68 | 3 | 2 |
| Bright Disease A historical classification which is no longer used. It described acute glomerulonephritis, acute nephritic syndrome, or acute nephritis. Named for Richard Bright. | 0 | 2.11 | 1 | 0 |
| Glomerulonephritis Inflammation of the renal glomeruli (KIDNEY GLOMERULUS) that can be classified by the type of glomerular injuries including antibody deposition, complement activation, cellular proliferation, and glomerulosclerosis. These structural and functional abnormalities usually lead to HEMATURIA; PROTEINURIA; HYPERTENSION; and RENAL INSUFFICIENCY. | 0 | 2.11 | 1 | 0 |
| Proteinuria The presence of proteins in the urine, an indicator of KIDNEY DISEASES. | 0 | 2.11 | 1 | 0 |
| Atrioventricular Nodal Re-Entrant Tachycardia [description not available] | 0 | 2.11 | 1 | 0 |
| Tachycardia, Ventricular An abnormally rapid ventricular rhythm usually in excess of 150 beats per minute. It is generated within the ventricle below the BUNDLE OF HIS, either as autonomic impulse formation or reentrant impulse conduction. Depending on the etiology, onset of ventricular tachycardia can be paroxysmal (sudden) or nonparoxysmal, its wide QRS complexes can be uniform or polymorphic, and the ventricular beating may be independent of the atrial beating (AV dissociation). | 0 | 2.11 | 1 | 0 |
| Vascular Injuries [description not available] | 0 | 2.11 | 1 | 0 |
| Neointima The new and thickened layer of scar tissue that forms on a PROSTHESIS, or as a result of vessel injury especially following ANGIOPLASTY or stent placement. | 0 | 7.11 | 1 | 0 |
| Arterial Inflammation [description not available] | 0 | 7.11 | 1 | 0 |
| Impaired Glucose Tolerance [description not available] | 0 | 2.11 | 1 | 0 |
| 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. | 0 | 2.11 | 1 | 0 |
| Kidney Diseases Pathological processes of the KIDNEY or its component tissues. | 0 | 2.11 | 1 | 0 |
| Arterial Diseases, Carotid [description not available] | 0 | 3.51 | 1 | 1 |
| 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. | 0 | 3.51 | 1 | 1 |
| Coronary Artery Stenosis [description not available] | 0 | 2.15 | 1 | 0 |
| Atheroma [description not available] | 0 | 2.15 | 1 | 0 |
| Coronary Stenosis Narrowing or constriction of a coronary artery. | 0 | 2.15 | 1 | 0 |
| Hypercoagulability [description not available] | 0 | 2.13 | 1 | 0 |
| Thrombophilia A disorder of HEMOSTASIS in which there is a tendency for the occurrence of THROMBOSIS. | 0 | 2.13 | 1 | 0 |
| Arteriosclerosis, Coronary [description not available] | 0 | 3.51 | 1 | 1 |
| Coronary Artery Disease Pathological processes of CORONARY ARTERIES that may derive from a congenital abnormality, atherosclerotic, or non-atherosclerotic cause. | 0 | 8.51 | 1 | 1 |
| Acute Disease Disease having a short and relatively severe course. | 0 | 4.86 | 2 | 1 |
| Nasopharyngitis Inflammation of the NASOPHARYNX, usually including its mucosa, related lymphoid structure, and glands. | 0 | 3.53 | 1 | 1 |
| Infections, Respiratory [description not available] | 0 | 3.53 | 1 | 1 |
| Respiratory Tract Infections Invasion of the host RESPIRATORY SYSTEM by microorganisms, usually leading to pathological processes or diseases. | 0 | 3.53 | 1 | 1 |
| Ureteral Obstruction Blockage in any part of the URETER causing obstruction of urine flow from the kidney to the URINARY BLADDER. The obstruction may be congenital, acquired, unilateral, bilateral, complete, partial, acute, or chronic. Depending on the degree and duration of the obstruction, clinical features vary greatly such as HYDRONEPHROSIS and obstructive nephropathy. | 0 | 2.15 | 1 | 0 |
| Glucose Metabolic Disorder [description not available] | 0 | 2.04 | 1 | 0 |
| Compensatory Hyperinsulinemia A GLUCOSE-induced HYPERINSULINEMIA, a marker of insulin-resistant state. It is a mechanism to compensate for reduced sensitivity to insulin. | 0 | 2.05 | 1 | 0 |
| 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. | 0 | 2.05 | 1 | 0 |
| Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time. | 0 | 2.98 | 1 | 0 |
| Autoimmune Diabetes [description not available] | 0 | 2.06 | 1 | 0 |
| Asymmetric Diabetic Proximal Motor Neuropathy [description not available] | 0 | 2.06 | 1 | 0 |
| 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. | 0 | 2.06 | 1 | 0 |
| 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) | 0 | 2.06 | 1 | 0 |
| Chronic Kidney Failure [description not available] | 0 | 2.06 | 1 | 0 |
| Cardiomyopathies, Primary [description not available] | 0 | 2.06 | 1 | 0 |
| 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. | 0 | 2.06 | 1 | 0 |
| 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). | 0 | 2.06 | 1 | 0 |
| 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. | 0 | 2.06 | 1 | 0 |
| Hyperlipemia [description not available] | 0 | 4.43 | 2 | 2 |
| Hyperlipidemias Conditions with excess LIPIDS in the blood. | 0 | 4.43 | 2 | 2 |
| 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. | 0 | 3.47 | 1 | 1 |
| Angioneurotic Edema [description not available] | 0 | 2.08 | 1 | 0 |
| Angioedema Swelling involving the deep DERMIS, subcutaneous, or submucosal tissues, representing localized EDEMA. Angioedema often occurs in the face, lips, tongue, and larynx. | 0 | 2.08 | 1 | 0 |