vildagliptin profile

ID Source	ID
PubMed CID	6918537
CHEMBL ID	142703
CHEBI ID	135285
SCHEMBL ID	16579
MeSH ID	M0486919

Synonym
AC-1273
vildagliptin ,
jalra
equa
nvp-laf-237
laf-237
xiliarx
galvus
equa (tn)
vildagliptin (jan/usan/inn)
galvus (tn)
D07080
nvp-laf237
(2s)-1-{2-[(3-hydroxyadamantan-1-yl)amino]acetyl}pyrrolidine-2-carbonitrile
bdbm11695
chembl142703 ,
CHEBI:135285
laf 237
laf237
nvp-laf 237
vitagliptin
DB04876
(2s)-1-[2-[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile
(2s)-(((3-hydroxyadamantan-1-yl)amino)acetyl)pyrrolidine-2-carbonitrile
2-pyrrolidinecarbonitrile, 1-[2-[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]-, (2s)-
vildagliptin (laf-237)
unii-i6b4b2u96p
vidagliptin (see vildagliptin)
i6b4b2u96p ,
2-pyrrolidinecarbonitrile, 1-(((3-hydroxytricyclo(3.3.1.13,7)dec-1-yl)amino)acetyl)-, (2s)-
(2s)-{((3-hydroxyadamantan-1-yl)amino)acetyl}pyrrolidine-2-carbonitrile
vildagliptin [usan:inn:ban:jan]
vildagliptin [mart.]
vildagliptin [usan]
(-)-(2s)-1-(((3-hydroxytricyclo(3.3.1.1(sup(3,7))dec-1-yl)amino)acetyl)pyrrolidine-2-carbonitrile
vildagliptin [mi]
(2s)-1-(((3-hydroxytricyclo(3.3.1.1(sup 3,7))dec-1-yl)amino)acetyl)pyrrolidine-2-carbonitrile
vildagliptin [who-dd]
2-pyrrolidinecarbonitrile, 1-(((3-hydroxytricyclo(3.3.1.1(sup 3,7))dec-1-yl)amino)acetyl)-, (2s)-
vildagliptin [ema epar]
vildagliptin [inn]
vildagliptin [jan]
AKOS015898120
S3033
gtpl6310
CS-1465
HY-14291
SYOKIDBDQMKNDQ-XWTIBIIYSA-N
AM20090695
SCHEMBL16579
AB01566863_01
NCGC00386200-01
SW220049-1
2s)-1-[[(3-hydroxytricyclo[3.3.1.13,7]decane-1-yl)amino]acetyl]-2-pyrrolidinecarbonitrile
(2s)-1-{[(3-hydroxyadamant-1-yl)amino]acetyl}pyrrolidine-2-carbonitrile
a10bh02
1-[2-[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]-2s-pyrrolidinecarbonitrile
(2s)-1-{[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl}pyrrolidine-2-carbonitrile
a10bd08
(2s)-1-[n-(3-hydroxyadamantan-1-yl)glycyl]pyrrolidine-2-carbonitrile
(2s)-1-{2-[(3-hydroxyadamant-1-yl)amino]acetyl}pyrrolidine-2-carbonitrile
zomelis
Q421042
CCG-267505
NCGC00386200-02
EN300-18527744
BV164521
vildagliptin- bio-x
vildagliptina
(2s)-1-(((3-hydroxytricyclo(3.3.1.13,7)dec-1-yl)amino)acetyl)pyrrolidine-2-carbonitrile
vildagliptin (mart.)
dtxcid201022401
vildagliptinum
vildagliptine

Excerpt	Reference
"Vildagliptin (VDG)is a frontier drug for diabetes mellitus. "	( Luminescence studies of binding affinity of vildagliptin with bovine serum albumin. Aswal, P; Kaur, L; Ojha, H; Pathak, M; Rahman, AJ; Singh, A; Singhal, R; Tiwari, AK; Verma, P, 2023)
"Vildagliptin is a marketed DPP4 inhibitor, used in the management of type 2 diabetes. "	( Vildagliptin-Derived Dipeptidyl Peptidase 9 (DPP9) Inhibitors: Identification of a DPP8/9-Specific Lead. Augustyns, K; Benramdane, S; Beyens, O; De Loose, J; De Meester, I; De Winter, H; Van der Veken, P; Van Rymenant, Y; Vliegen, G, 2022)
"Vildagliptin (VIL) is an antidiabetic drug that inhibits dipeptidyl peptidase-4 (DPP4) through a covalent mechanism. "	( Insight into the Role of Active Site Protonation States and Water Molecules in the Catalytic Inhibition of DPP4 by Vildagliptin. Corredor, JD; Febres-Molina, C; Jaña, GA; Jiménez, VA, 2023)
"Vildagliptin (V) is a dipeptidyl peptidase-4 inhibitor that has a hepatorenal protective effect against models of liver and renal IR."	( Renoprotective effect of vildagliptin following hepatic ischemia/reperfusion injury. Al-Shaalan, NH; Alshaalan, AA; Sherif, IO, 2020)
"Vildagliptin is a representative of Dipeptidyl Peptidase-4 (DPP-4) inhibitors, antihyperglycemic drugs, approved for use as monotherapy and combination therapy in type 2 diabetes mellitus. "	( Vasculoprotective Effects of Vildagliptin. Focus on Atherogenesis. Górski, K; Malinowski, B; Nowaczewska, M; Walczak, M; Wiciński, M; Wódkiewicz, E, 2020)
"Vildagliptin is an antidiabetic agent, belongs to the dipeptidyl peptidase IV (DPP-4) inhibitors."	( Analytical Method Development and Validation of UV-visible Spectrophotometric Method for the Estimation of Vildagliptin in Gastric Medium. Khansili, A; Kumari, B, 2020)
"Vildagliptin is an inhibitor of the enzyme dipeptidyl peptidase 4, indicated for the treatment of type 2 diabetes mellitus, combined or not with metformin. "	( Cost-effectiveness of vildagliptin for people with type 2 diabetes mellitus in Brazil; findings and implications. Acurcio, FA; De Oliveira, GL; Godman, B; Guerra Júnior, AA, 2017)
"Vildagliptin is a dipeptidyl peptidase-4 inhibitor commonly used as a dual oral agent with metformin, thiazolidinediones, or sulfonylurea for the treatment of type 2 diabetes mellitus (T2DM). "	( Effectiveness of vildagliptin as add-on to metformin monotherapy among uncontrolled type 2 diabetes mellitus patients in a real-world setting. Chodick, G; Davis, C; Melzer Cohen, C; Shalev, V, 2018)
"Vildagliptin (VD) is a drug that has addressed these issues successfully with the desired safety portfolio."	( DNA scaffold nanoparticles coated with HPMC/EC for oral delivery. Abbas, M; Ansari, MT; Baig, MMFA; Chunxia, W; Hasnat, M; Khan, GJ; Naveed, M; Shad, A; Sohail, M; Ullah, S, 2019)
"Vildagliptin (VI) is a potent DPP-4 inhibitor with least adverse events compared to other DPP-4 inhibitors."	( Design, synthesis and evaluation of DNA nano-cubes as a core material protected by the alginate coating for oral administration of anti-diabetic drug. Abbas, M; Ansari, MT; Baig, MMFA; Hasnat, M; Kassim, SA; Khan, GJ; Naveed, M; Shah, K; Sohail, M; Ullah, S, 2019)
"Vildagliptin is a novel dipeptidyl peptidase-4 inhibitor that is given either alone or in combination with oral hypoglycemic drugs, including metformin."	( Effects of vildagliptin/metformin therapy on patient-reported outcomes: work productivity, patient satisfaction, and resource utilization. Genovese, S; Tedeschi, D, 2013)
"Vildagliptin is a molecule from the group of DPP 4 inhibitors which is recently used in internal outpatient care."	( [Use of vildagliptin from an internal disease specialists point of view]. Kožnarová, R, 2013)
"Vildagliptin is an oral inhibitor of dipeptidyl peptidase-4, an enzyme mainly responsible for inactivating incretins, and one of the widely used drugs for the treatment of type 2 diabetes. "	( Beneficial effects of vildagliptin on retinal injury in obese type 2 diabetic rats. Ishibashi, Y; Maeda, S; Matsui, T; Nakashima, S; Nishino, Y; Ojima, A; Yamagishi, S; Yamakawa, R; Yoshida, Y, 2013)
"Vildagliptin is a dipeptidyl peptidase-4 inhibitor targeting the incretin system to improve glycemic control in type 2 diabetes."	( Vildagliptin, a dipeptidyl peptidase-4 inhibitor, for the treatment of type 2 diabetes. Davis, SN; Lamos, EM; Stein, SA, 2014)
"Vildagliptin is an effective and well-tolerated oral dipeptidyl peptidase-4 inhibitor. "	( Vildagliptin, a dipeptidyl peptidase-4 inhibitor, for the treatment of type 2 diabetes. Davis, SN; Lamos, EM; Stein, SA, 2014)
"Vildagliptin is a dipeptidyl peptidase IV inhibitor (DPP4i). "	( [Safety and efficacy of Vildagliptin in real life Chilean diabetic patients]. Godoy J, G; Gutiérrez, V; Montecinos, M; Yenes, A, 2015)
"Vildagliptin is a member of a new class of oral anti-diabetic drug. "	( Identification, isolation and characterization of potential process-related impurity and its degradation product in vildagliptin. Devineni, SR; Dubey, SK; Kadirappa, A; Kumar, N; Kumar, P; Singh, G, 2016)
"Vildagliptin is an effective and safe therapeutic option for patients with T2DM, both as monotherapy and as add-on treatment."	( Systematic review and meta-analysis of vildagliptin for treatment of type 2 diabetes. Athanasiadou, E; Bekiari, E; Boura, P; Karagiannis, T; Liakos, A; Mainou, M; Papatheodorou, K; Rika, M; Rizava, C; Tsapas, A, 2016)
"Vildagliptin is an inhibitor of dipeptidyl peptidase-4 that is used for the treatment of type 2 diabetes mellitus. "	( MicroRNA expression in the vildagliptin-treated two- and three-dimensional HepG2 cells. Asakura, M; Atsuda, K; Fujii, H; Fujiwara, R; Itoh, T; Mitsugi, R; Nagai, K; Yamashita, Y, 2016)
"Vildagliptin is a new drug used to treat diabetes mellitus (DM)."	( A case of bullous pemphigoid ınduced by vildagliptin. Ersoy-Evans, S; Gököz, O; Gönül, M; Keseroglu, HO; Taş-Aygar, G, 2017)
"Vildagliptin is a potent, orally active inhibitor of dipeptidyl peptidase-4 (DPP-4) for the treatment of type 2 diabetes mellitus. "	( Vildagliptin and its metabolite M20.7 induce the expression of S100A8 and S100A9 in human hepatoma HepG2 and leukemia HL-60 cells. Asakura, M; Atsuda, K; Fujii, H; Fujiwara, R; Itoh, T; Karaki, F, 2016)
"Vildagliptin is a selective inhibitor of dipeptidyl peptidase IV (DPP-4) that improves glycemic control and pancreatic b-cell function in patients with Type 2 diabetes. "	( Evaluation of pharmacokinetic and pharmacodynamic interaction between the dipeptidyl peptidase IV inhibitor vildagliptin, glyburide and pioglitazone in patients with Type 2 diabetes. Balez, S; Bullock, J; Dole, WP; He, YL; Jarugula, V; Ligueros-Saylan, M; Riviere, GJ; Schwartz, S; Serra, D; Wang, Y, 2008)
"Vildagliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-4), orally active, that improves glycemic control in patients with type 2 diabetes (T2DM) primarily by enhancing pancreatic (alpha and beta) islet function. "	( Combination treatment in the management of type 2 diabetes: focus on vildagliptin and metformin as a single tablet. Dejager, S; Foley, J; Halimi, S; Minic, B; Schweizer, A, 2008)
"Vildagliptin is an orally effective, potent, and selective inhibitor of dipeptidyl peptidase IV (DPP-4) that improves glycemic control in patients with type 2 diabetes. "	( Pharmacokinetics and pharmacodynamics of vildagliptin in healthy Chinese volunteers. Deckert, F; Dole, WP; He, YL; Hu, P; Jiang, J; Kjems, L; Liu, D; Yin, Q, 2009)
"Vildagliptin (Galvus) is an antihyperglycaemic agent that selectively inhibits the dipeptidyl peptidase-4 (DPP-4) enzyme. "	( Vildagliptin: a review of its use in the management of type 2 diabetes mellitus. Croxtall, JD; Keam, SJ, 2008)
"Vildagliptin is a new oral antidiabetic agent that enhances pancreatic islet cell responsiveness to glucose. "	( Vildagliptin: a new oral treatment for type 2 diabetes mellitus. Degrande, E; Mathieu, C, 2008)
"Vildagliptin is an oral incretin enhancer that acts to increase active levels of the incretin hormone glucagon-like peptide-1 (GLP-1) by inhibiting the dipeptidyl peptidase-4 enzyme responsible for the rapid deactivation of GLP-1 in vivo. "	( The scientific evidence: vildagliptin and the benefits of islet enhancement. Mathieu, C, 2009)
"Vildagliptin is a potent and selective oral dipeptidyl peptidase-4 inhibitor that improves glycaemic control in patients with type 2 diabetes mellitus (T2DM) by increasing both alpha- and beta-cell responsiveness to glucose. "	( Translating science into clinical practice: focus on vildagliptin in combination with metformin. Barnett, AH, 2009)
"Vildagliptin (Galvus) is a selective inhibitor of dipeptidylpeptidase-4, an enzyme involved in the metabolism of glucagon-like peptide-1 (GLP-1) secreted by L cells of the intestine. "	( [Vildagliptin (Galvus) and fixed combination vildagliptine-metformin (Eucreas) in the treatment of type 2 diabetes]. Paquot, N; Scheen, AJ, 2009)
"Vildagliptin is an effective and well-tolerated treatment option in elderly patients with type 2 diabetes, demonstrating similar improvement in glycaemic control as metformin, with superior GI tolerability."	( Comparison of vildagliptin and metformin monotherapy in elderly patients with type 2 diabetes: a 24-week, double-blind, randomized trial. Bosi, E; Dejager, S; Schweizer, A, 2009)
"Vildagliptin is an orally active, potent inhibitor of dipeptidyl peptidase IV and was developed for the treatment of type 2 diabetes. "	( Hormonal and metabolic effects of morning or evening dosing of the dipeptidyl peptidase IV inhibitor vildagliptin in patients with type 2 diabetes. Dole, WP; Foley, J; He, YL; Ligueros-Saylan, M; Schwartz, SL; Valencia, J; Zhang, Y, 2010)
"Vildagliptin is a novel dipeptidyl peptidase-4 (DPP-4) inhibitor that improves pancreatic islet function by enhancing both α- and β-cell responsiveness to increased blood glucose."	( A randomized, placebo-controlled, double-blind, prospective trial to evaluate the effect of vildagliptin in new-onset diabetes mellitus after kidney transplantation. Döller, D; Haidinger, M; Hecking, M; Hörl, WH; Pleiner, J; Säemann, MD; Stemer, G; Voigt, HC; Weichhart, T; Werzowa, J, 2010)
"Vildagliptin is a stable inhibitor of dipeptidyl peptidase-IV, a responsible enzyme that mainly inactivates glucagon-like peptide-1, and now one of the widely used agents for the treatment of diabetes. "	( Vildagliptin blocks vascular injury in thoracic aorta of diabetic rats by suppressing advanced glycation end product-receptor axis. Matsui, T; Nishino, Y; Takeuchi, M; Yamagishi, S, 2011)
"Vildagliptin is a new DPP-4 inhibitor approved in many countries for the treatment of T2DM."	( Vildagliptin in the treatment of type 2 diabetes mellitus. Schneider, SH; Stamataros, G, 2011)
"Vildagliptin is a drug from a new class of medications called dipeptidyl peptidase IV (DPP4) inhibitors."	( Emerging role of dipeptidyl peptidase-IV (DPP-4) inhibitor vildagliptin in the management of type 2 diabetes. Kalra, S, 2011)
"Vildagliptin is an oral DPP-4 inhibitor approved in more than 70 countries."	( The efficacy and safety of vildagliptin in patients with type 2 diabetes: a meta-analysis of randomized clinical trials. Cai, L; Cai, Y; Liu, P; Lu, ZJ; Zhang, Y, 2012)
"Vildagliptin is an orally active, potent and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, shown to be effective and well tolerated in patients with type 2 diabetes mellitus (T2DM) as either monotherapy or in combination with other anti-diabetic agents. "	( Clinical pharmacokinetics and pharmacodynamics of vildagliptin. He, YL, 2012)
"Vildagliptin is an inhibitor of oral DPP-4, the most studied of this new class."	( [Characterization of patients with type 2 diabetes treated with vildagliptin]. Carvalho, R; Chambel, P; Domingues, A; Jácome De Castro, J; Lopes, L; Lopes, MS; Marcelino, M; Paradinha, M; Santos, V; Vilar, H, )
"Vildagliptin is an incretin degradation inhibitor that improves beta-cell function in diabetic patients by increasing the insulin secretory tone."	( Vildagliptin, a dipeptidyl peptidase-IV inhibitor, improves model-assessed beta-cell function in patients with type 2 diabetes. Deacon, CF; Dunning, BE; Foley, JE; He, YL; Holst, JJ; Ligueros-Saylan, M; Mari, A; Sallas, WM; Watson, C, 2005)
"Vildagliptin is a competitive and reversible inhibitor of dipeptidyl peptidase-4. "	( Vildagliptin: an inhibitor of dipeptidyl peptidase-4 with antidiabetic properties. Ahrén, B, 2006)
"Vildagliptin is a potent, orally active, highly selective DPP-4 inhibitor that enhances the antidiabetic actions of the incretins."	( Vildagliptin: a novel DPP-4 inhibitor with pancreatic islet enhancement activity for treatment of patients with type 2 diabetes. Bates, PC; Ristic, S, 2006)
"Vildagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that is being evaluated in the treatment of patients with type 2 diabetes mellitus. "	( Vildagliptin. Henness, S; Keam, SJ, 2006)
"Vildagliptin is a selective dipeptidyl peptidase IV inhibitor that augments meal-stimulated levels of biologically active glucagon-like peptide-1. "	( The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients. Baig, MR; Balas, B; Cusi, K; Darland, C; Deacon, CF; DeFronzo, RA; Dunning, BE; Foley, JE; He, YL; Holst, JJ; Ligueros-Saylan, M; Mari, A; Wang, Y; Watson, C, 2007)
"Vildagliptin is an effective and well-tolerated treatment option in patients with type 2 diabetes, demonstrating similar glycemic reductions as rosiglitazone but without weight gain."	( Comparison of vildagliptin and rosiglitazone monotherapy in patients with type 2 diabetes: a 24-week, double-blind, randomized trial. Baron, MA; Dejager, S; Mills, D; Rosenstock, J; Schweizer, A, 2007)
"Vildagliptin is a dipeptidyl peptidase-IV inhibitor, which improves glycaemic control by increasing pancreatic beta cell responsiveness to glucose and suppressing inappropriate glucagon secretion."	( Addition of vildagliptin to insulin improves glycaemic control in type 2 diabetes. Albrecht, D; Baron, MA; Chang, I; Dejager, S; Fonseca, V; Schweizer, A, 2007)
"Vildagliptin is a potent and selective dipeptidyl peptidase-IV (DPP-4) inhibitor that improves glycemic control in patients with type 2 diabetes mellitus by increasing alpha- and beta-cell responsiveness to glucose. "	( The influence of hepatic impairment on the pharmacokinetics of the dipeptidyl peptidase IV (DPP-4) inhibitor vildagliptin. Campestrini, J; Dilzer, SC; Dole, WP; He, YL; Howard, D; Lasseter, KC; Ligueros-Saylan, M; Sabo, R; Wang, Y, 2007)
"Vildagliptin is a potent and selective dipeptidyl peptidase-IV (DPP-4) inhibitor that improves glycemic control in patients with type 2 diabetes by increasing alpha and beta-cell responsiveness to glucose. "	( Effect of the novel oral dipeptidyl peptidase IV inhibitor vildagliptin on the pharmacokinetics and pharmacodynamics of warfarin in healthy subjects. Dole, WP; He, YL; Howard, D; Leon, S; Ligueros-Saylan, M; Riviere, GJ; Rosenberg, M; Sabo, R; Sunkara, G, 2007)
"Vildagliptin is an agent in a new class of medications called dipeptidyl peptidase IV (DPP4) inhibitors. "	( Vildagliptin: a novel oral therapy for type 2 diabetes mellitus. Lauster, CD; McKaveney, TP; Muench, SV, 2007)
"Vildagliptin is a potent and selective oral DPP-4 inhibitor that has been studied both as monotherapy and in combination with other antidiabetic treatments."	( Dipeptidyl peptidase 4 inhibition and vildagliptin therapy for type 2 diabetes. Del Prato, S, 2007)
"Vildagliptin is a dipeptidyl peptidase IV (DPP-4) inhibitor currently under development for the treatment of type 2 diabetes mellitus."	( Pharmacokinetics and pharmacodynamics of vildagliptin in patients with type 2 diabetes mellitus. Campestrini, J; Deacon, CF; He, YL; Holst, JJ; Ligueros-Saylan, M; Nielsen, JC; Riviere, GJ; Schwartz, S; Serra, D; Wang, Y, 2007)
"Vildagliptin is likely to be a useful therapy for patients with type 2 diabetes based on the inhibition of DPP-4 and the subsequent increase in incretin hormones, GLP-1 and GIP, and the decrease in glucose and glucagon levels."	( Pharmacokinetics and pharmacodynamics of vildagliptin in patients with type 2 diabetes mellitus. Campestrini, J; Deacon, CF; He, YL; Holst, JJ; Ligueros-Saylan, M; Nielsen, JC; Riviere, GJ; Schwartz, S; Serra, D; Wang, Y, 2007)
"Vildagliptin is a potent and selective dipeptidyl peptidase IV inhibitor in development for the treatment of type 2 diabetes that improves glycemic control by enhancing alpha- and beta-cell responsiveness to glucose. "	( Dose proportionality and the effect of food on vildagliptin, a novel dipeptidyl peptidase IV inhibitor, in healthy volunteers. Campestrini, J; Dole, WP; He, YL; Howard, D; Rosenberg, M; Sabo, R; Sunkara, G; Wang, Y, 2007)
"Vildagliptin is a novel antidiabetic agent that is an orally active, potent, and selective inhibitor of dipeptidyl peptidase IV, the enzyme responsible for degradation of the incretin hormones. "	( Evaluation of pharmacokinetic interactions between vildagliptin and digoxin in healthy volunteers. Bizot, MN; Dole, WP; He, YL; Howard, D; Leon, S; Ligueros-Saylan, M; Riviere, GJ; Sabo, R; Sunkara, G, 2007)
"Vildagliptin is a potent, selective, orally active inhibitor of dipeptidylpeptidase-IV being developed for the treatment of type 2 diabetes mellitus. "	( The absolute oral bioavailability and population-based pharmacokinetic modelling of a novel dipeptidylpeptidase-IV inhibitor, vildagliptin, in healthy volunteers. Balez, S; Campestrini, J; He, YL; Howard, D; Laurent, A; Ligueros-Saylan, M; Sabo, R; Sadler, BM; Wang, Y, 2007)
"Vildagliptin is a potent selective inhibitor of dipeptidyl peptidase-4 (DPP-4) that improves glycaemic control by increasing islet alpha-cell and beta-cell responsiveness to glucose. "	( The DPP-4 inhibitor vildagliptin: robust glycaemic control in type 2 diabetes and beyond. Panina, G, 2007)
"Vildagliptin is an orally active, potent and selective inhibitor of dipeptidyl peptidase IV (DPP-4), the enzyme responsible for the degradation of incretin hormones. "	( Evaluation of the potential for steady-state pharmacokinetic interaction between vildagliptin and simvastatin in healthy subjects. Ayalasomayajula, SP; Campestrini, J; Dole, K; He, YL; Humbert, H; Ligueros-Saylan, M; Sunkara, G; Wang, Y, 2007)
"Vildagliptin is a new, potent, and selective inhibitor of DPP-4."	( The effect of age, gender, and body mass index on the pharmacokinetics and pharmacodynamics of vildagliptin in healthy volunteers. Campestrini, J; Dole, WP; He, YL; Howard, D; Ligueros-Saylan, M; Nielsen, JC; Riviere, GJ; Rosenberg, M; Sabo, R; Wang, Y, 2008)
"Vildagliptin is a selective inhibitor of dipeptidyl peptidase-4, and prevents the rapid degradation of the incretin hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide. "	( Update: vildagliptin for the treatment of Type 2 diabetes. Garber, AJ; Sharma, MD, 2008)
"Vildagliptin is a potent, selective and reversible inhibitor of dipeptidyl peptidase-4 (DPP-4), the enzyme responsible for rapid inactivation of the incretin hormones glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP). "	( The islet enhancer vildagliptin: mechanisms of improved glucose metabolism. Ahrén, B; Foley, JE, 2008)
"Vildagliptin is an orally active, potent and selective DPP-4 inhibitor that improves glycemic control in patients with type 2 diabetes by increasing alpha- and beta-cell responsiveness to glucose."	( Effect of food on the pharmacokinetics of a vildagliptin/metformin (50/1000 mg) fixed-dose combination tablet in healthy volunteers. Campestrini, J; Flannery, B; He, YL; Jarugula, V; Leon, S; Ligueros-Saylan, M; Zinny, MA, 2008)

Excerpt	Reference
"Vildagliptin has a half-life of about 90 minutes; however, > or = 50% of DPP4 inhibition continues for more than 10 hours, allowing for once- or twice-daily dosing."	( Emerging role of dipeptidyl peptidase-IV (DPP-4) inhibitor vildagliptin in the management of type 2 diabetes. Kalra, S, 2011)
"Vildagliptin has a low potential for drug interactions, as cytochrome P450 (CYP) enzymes are minimally (<1.6%) involved in the overall metabolism."	( Clinical pharmacokinetics and pharmacodynamics of vildagliptin. He, YL, 2012)
"Vildagliptin has a halflife of about 90 minutes; however, > or =50% of DPP4 inhibition continues for more than 10 hours, allowing for once- or twice-daily dosing."	( Vildagliptin: a novel oral therapy for type 2 diabetes mellitus. Lauster, CD; McKaveney, TP; Muench, SV, 2007)
"Vildagliptin has been shown to exert beneficial effects on several organs in cases of obese-insulin resistant condition."	( Dipeptidyl peptidase-4 inhibitor enhances restoration of salivary glands impaired by obese-insulin resistance. Apaijai, N; Chattipakorn, N; Chattipakorn, S; Ittichaicharoen, J; Sa-Nguanmoo, P; Tanajak, P, 2018)
"Thus vildagliptin has been shown both to improve insulin secretion and to suppress the inappropriate glucagon secretion seen in patients with T2DM."	( Combination treatment in the management of type 2 diabetes: focus on vildagliptin and metformin as a single tablet. Dejager, S; Foley, J; Halimi, S; Minic, B; Schweizer, A, 2008)
"As vildagliptin has been used most often at doses of 50 mg once or twice daily, in combination with metformin, this review focuses on these dose regimens."	( Clinical evidence and mechanistic basis for vildagliptin's action when added to metformin. Ahrén, B; Bosi, E; Foley, JE, 2011)
"Vildagliptin has been shown to stimulate insulin secretion and inhibit glucagon secretion in a glucose-dependent manner."	( Mechanisms of action of the dipeptidyl peptidase-4 inhibitor vildagliptin in humans. Ahrén, B; Dejager, S; Dunning, BE; Foley, JE; Schweizer, A; Villhauer, EB, 2011)
"Vildagliptin has been demonstrated to be efficacious, safe and well tolerated in elderly patients with T2DM without dose adjustment."	( Clinical pharmacokinetics and pharmacodynamics of vildagliptin. He, YL, 2012)
"Vildagliptin has been added mostly in patients medicated with metformin."	( [Characterization of patients with type 2 diabetes treated with vildagliptin]. Carvalho, R; Chambel, P; Domingues, A; Jácome De Castro, J; Lopes, L; Lopes, MS; Marcelino, M; Paradinha, M; Santos, V; Vilar, H, )
"Vildagliptin has been evaluated in > 4800 patients in nine Phase III studies in the range of 24 - 52 weeks in duration: four placebo- or active-controlled monotherapy trials that enrolled drug-naive patients; four add-on studies in which vildagliptin was added to a stable regimen of either metformin, a sulfonylurea, a thiazolidinedione or insulin; and a study in which an initial combination of vildagliptin plus pioglitazone in drug-naive patients was evaluated."	( Update: vildagliptin for the treatment of Type 2 diabetes. Garber, AJ; Sharma, MD, 2008)

Excerpt	Reference
"Vildagliptin prevents the increase of fibrosis markers in WAT of HFD-fed mice and reduces blood glucose, serum triglycerides, total cholesterol and leptin levels. "	( Dipeptidyl peptidase IV (DPP-IV) inhibition prevents fibrosis in adipose tissue of obese mice. Cavadas, C; Cunha-Santos, J; Leal, H; Marques, AP; Pereira de Almeida, L; Rosmaninho-Salgado, J; Sousa-Ferreira, L, 2018)
"Vildagliptin showed lower glucose fluctuations than glimepiride as measured by mean amplitude of glycaemic excursions (MAGE, p = 0.1076), standard deviation (s.d., p = 0.1346) of blood glucose rate of change, but did not reach statistical significance attributed to the small sample size."	( Differential effects of vildagliptin and glimepiride on glucose fluctuations in patients with type 2 diabetes mellitus assessed using continuous glucose monitoring. Forst, T; Foteinos, G; He, YL; Kulmatycki, K; Mattapalli, D; Neelakantham, S; Taylor, A, 2013)
"Vildagliptin promotes beta cell survival by inhibiting cell apoptosis. "	( Dipeptidyl peptidase-4 inhibitor, vildagliptin, inhibits pancreatic beta cell apoptosis in association with its effects suppressing endoplasmic reticulum stress in db/db mice. Chen, LM; Guo, H; Guo, X; Kong, Y; Li, CJ; Li, DQ; Liu, DM; Wu, YJ; Yang, Y; Zhang, J, 2015)
"Vildagliptin can suppress temporal lobe epilepsy in rats by up-regulating GLP-1 and GLP-1R expressions."	( [Vildagliptin suppresses temporal lobe epilepsy by up-regulating glucagon-like peptide-1]. Shi, QH; Wen, YT; Wu, KL, 2017)
"Vildagliptin acts to inhibit the breakdown of glucagon-like peptide (GLP)-1, which in turn enhances the beta-cell response to glucose and inhibits glucagon secretion. "	( Vildagliptin in the treatment of type 2 diabetes mellitus. Schneider, SH; Stamataros, G, 2011)
"Vildagliptin did not cause any clinically relevant changes in safety and was well tolerated."	( Vildagliptin: a novel DPP-4 inhibitor with pancreatic islet enhancement activity for treatment of patients with type 2 diabetes. Bates, PC; Ristic, S, 2006)
"Vildagliptin displays approximately dose-proportional pharmacokinetics over the 25- to 200-mg dose range, and administration with food has no clinically relevant effect on vildagliptin pharmacokinetics."	( Dose proportionality and the effect of food on vildagliptin, a novel dipeptidyl peptidase IV inhibitor, in healthy volunteers. Campestrini, J; Dole, WP; He, YL; Howard, D; Rosenberg, M; Sabo, R; Sunkara, G; Wang, Y, 2007)

Excerpt	Reference
"Vildagliptin treatment increased the myocardial homing of circulating CXCR4+ stem cells and angiogenesis. "	( Vildagliptin and G-CSF Improved Angiogenesis and Survival after Acute Myocardial Infarction. Hu, Z; Li, M; Wang, Z; Xia, H; Yu, L, 2019)
"Vildagliptin pretreatment improved neurological deficit score, locomotor activity, and motor coordination in MCAO rats."	( Neuroprotective effect of vildagliptin against cerebral ischemia in rats. Abd-Elsalam, RM; Abdel-Rahman, RF; El-Marasy, SA, 2018)
"Vildagliptin treatment increased levels of butyrylcarnitine and acetylcarnitine."	( Metabolomics Based on MS in Mice with Diet-Induced Obesity and Type 2 Diabetes Mellitus: the Effect of Vildagliptin, Metformin, and Their Combination. Bugáňová, M; Haluzík, M; Holubová, M; Kuneš, J; Kuzma, M; Maletínská, L; Pelantová, H; Šedivá, B; Tomášová, P; Železná, B, 2019)
"Vildagliptin treatment was associated with less fluctuation of glucose levels than glimepiride treatment as assessed by 24-h CGM device, suggesting vildagliptin may have the potential to offer long-term beneficial effects for patients with T2DM in preventing the development of complications of diabetes."	( Differential effects of vildagliptin and glimepiride on glucose fluctuations in patients with type 2 diabetes mellitus assessed using continuous glucose monitoring. Forst, T; Foteinos, G; He, YL; Kulmatycki, K; Mattapalli, D; Neelakantham, S; Taylor, A, 2013)
"Vildagliptin and voglibose treatments, alone or when co-administered, were well tolerated in Japanese patients with Type 2 diabetes."	( Pharmacokinetic and pharmacodynamic interaction of vildagliptin and voglibose in Japanese patients with Type 2 diabetes. Furihata, K; He, YL; Kulmatycki, K; Mita, S; Saji, T; Sekiguchi, K; Yamaguchi, M, 2013)
"Vildagliptin treatment also produced an increase in blood pressure and heart rate likely via increased sympathetic tone."	( Vascular origin of vildagliptin-induced skin effects in Cynomolgus monkeys: pathomechanistic role of peripheral sympathetic system and neuropeptide Y. Bentley, P; Burkey, B; Busch, S; Chibout, SD; Dubost, V; Flavahan, N; Hayes, M; Hoffmann, P; Kaushik, V; Lapadula, D; Longo, L; Martin, L; Moulin, P; Pantano, S; Sahota, P; Schoenfeld, H; Spaet, R; Zhou, W, 2014)
"Vildagliptin-treated patients had significantly (P<0.05) improved compliance (68.3% versus 62.5%, respectively), persistence (61.5% versus 55.1%), and metabolic control (63.3% versus 57.6%)."	( Use of metformin and vildagliptin for treatment of type 2 diabetes in the elderly. Navarro-Artieda, R; Sicras-Mainar, A, 2014)
"Vildagliptin treatment increased the area under the curve for the C peptide reactivity (CPR) (AUCCPR; 26.66±5.15 vs."	( The dipeptidyl peptidase-4 inhibitor vildagliptin has the capacity to repair β-cell dysfunction and insulin resistance. Horie, A; Ide, K; Ishizuka, T; Kanatsuka, A; Marumo, K; Oshikiri, K; Sunaga, M; Suzuki, Y; Tokuyama, Y, 2014)
"Vildagliptin treatment with or without metformin was generally well tolerated."	( Clinical effectiveness and safety of vildagliptin in >19 000 patients with type 2 diabetes: the GUARD study. Abou Jaoude, E; Al-Arouj, M; DiTommaso, S; Fawwad, A; Latif, ZA; Orabi, A; Rosales, R; Shah, P; Vaz, J, 2015)
"Vildagliptin treatment reduced glycosylated hemoglobin by 1.1% and was well tolerated in this group of diabetic patients."	( [Safety and efficacy of Vildagliptin in real life Chilean diabetic patients]. Godoy J, G; Gutiérrez, V; Montecinos, M; Yenes, A, 2015)
"Vildagliptin treatment more than doubled responses of intact GLP-1 and glucose-dependent insulinotropic polypeptide and lowered glucose responses without changing AUCISR/AUCglucose in healthy subjects."	( Quantification of the Contribution of GLP-1 to Mediating Insulinotropic Effects of DPP-4 Inhibition With Vildagliptin in Healthy Subjects and Patients With Type 2 Diabetes Using Exendin [9-39] as a GLP-1 Receptor Antagonist. Broschag, M; Deacon, CF; Foley, J; He, YL; Holst, JJ; Kind, J; Kjems, L; Köthe, LD; Nauck, MA, 2016)
"Vildagliptin treatment significantly increased BMD and trabecular bone volume."	( Protective Effects of Vildagliptin against Pioglitazone-Induced Bone Loss in Type 2 Diabetic Rats. Eom, YS; Gwon, AR; Kim, BJ; Kim, JY; Kim, KW; Kim, YS; Kwak, KM; Lee, K; Lee, S; Park, IB; Yu, SH, 2016)
"With vildagliptin treatment, mean amplitude of glycemic excursions was significantly improved compared with sitagliptin treatment (57.9 ± 22.2 vs."	( Effects of 50 mg vildagliptin twice daily vs. 50 mg sitagliptin once daily on blood glucose fluctuations evaluated by long-term self-monitoring of blood glucose. Atsumi, T; Cho, KY; Kameda, H; Kimachi, K; Kondo, T; Miyoshi, H; Nagai, S; Nakamura, A; Nomoto, H, 2017)
"Vildagliptin treatment improves beta-cell sensitivity to glucose, producing increased insulin secretory rate relative to glucose in both postprandial and fasting states."	( The scientific evidence: vildagliptin and the benefits of islet enhancement. Mathieu, C, 2009)
"Vildagliptin treatment appears to address both these defects."	( Role of vildagliptin in managing type 2 diabetes mellitus in the elderly. Dejager, S; Halimi, S; Raccah, D; Schweizer, A, 2010)
"Vildagliptin treatment led to a dose-dependent increase in plasma active GLP-1 levels; the overall increases (area under the effect-time course from 0 to 8 h, AUE0-8h) after 7 days' treatment were 1.5-, 1.7-, and 1.8-fold with vildagliptin 10 mg, 25 mg and 50 mg twice daily, respectively (all p < 0.0001 vs."	( Pharmacokinetics and pharmacodynamics of vildagliptin in Japanese patients with type 2 diabetes. He, YL; Ito, H; Sekiguchi, K; Terao, S; Yamaguchi, M, 2010)
"Vildagliptin treatment decreased fasting plasma glucose and heart rate in OLETF rats."	( Vildagliptin blocks vascular injury in thoracic aorta of diabetic rats by suppressing advanced glycation end product-receptor axis. Matsui, T; Nishino, Y; Takeuchi, M; Yamagishi, S, 2011)
"No vildagliptin- or placebo-treated volunteer had QTcF > 450 ms."	( Thorough QT study of the effects of vildagliptin, a dipeptidyl peptidase IV inhibitor, on cardiac repolarization and conduction in healthy volunteers. Dole, WP; He, YL; Ligueros-Saylan, M; Serra, D; Wang, Y; Zhang, Y, 2011)
"Vildagliptin pre-treatment to both normal and diabetic rats had shown mild decrease in NO, but significantly increased insulin secretions."	( Relationships between the islets blood flow, nitric oxide, insulin, and cytosolic calcium in rat pancreatic islets: effects of DPP-IV inhibitor vildagliptin. Akarte, AS; Gandhi, S; Srinivasan, BP, 2012)
"Vildagliptin treatment was associated with a stronger decrease in nitrotyrosine (P < 0.01), IL-6 (P < 0.05), and IL-18 (P < 0.05) than sitagliptin treatment."	( Reduction of oxidative stress and inflammation by blunting daily acute glucose fluctuations in patients with type 2 diabetes: role of dipeptidyl peptidase-IV inhibition. Barbieri, M; Marfella, R; Paolisso, G; Rizzo, MR, 2012)
"The vildagliptin + telmisartan treatment group showed no weight gain and controlled blood pressure, renovascular structural and biochemical parameters in diabetic neuropathy rats."	( Dual therapy of vildagliptin and telmisartan on diabetic nephropathy in experimentally induced type 2 diabetes mellitus rats. Dhakad, PK; Joshi, M; Joshi, S; Kanawat, DS; Kurmi, MK; Mishra, A; Raikwar, SK; Sharma, AK; Sharma, P; Srinivasan, BP; Srivastava, V, 2014)
"Vildagliptin treatment reduced the hepatic expression of genes important for cholesterol synthesis and fatty acid oxidation, including phospho-mevalonate kinase (Mvk), acyl-coenzyme dehydrogenase medium chain (Acadm), mevalonate (diphospho)decarboxylase (Mvd), and Acyl-CoA synthetase (Acsl1), in WT but not in DIRKO mice."	( Incretin receptors for glucagon-like peptide 1 and glucose-dependent insulinotropic polypeptide are essential for the sustained metabolic actions of vildagliptin in mice. Baggio, LL; Drucker, DJ; Flock, G; Longuet, C, 2007)
"Vildagliptin treatment did not increase adverse events among older patients with mild renal impairment (62.0%)."	( Management of type 2 diabetes in treatment-naive elderly patients: benefits and risks of vildagliptin monotherapy. Banerji, MA; Couturier, A; Dejager, S; Pi-Sunyer, FX; Pratley, RE; Rosenstock, J; Schweizer, A, 2007)
"Treatment with vildagliptin lowers the level of PAI-1 presenting possible antithrombotic effect."	( Vasculoprotective Effects of Vildagliptin. Focus on Atherogenesis. Górski, K; Malinowski, B; Nowaczewska, M; Walczak, M; Wiciński, M; Wódkiewicz, E, 2020)
"Treatment with vildagliptin improved memory deficits and decreased neuronal apoptosis in the hippocampus."	( Vildagliptin prevents cognitive deficits and neuronal apoptosis in a rat model of Alzheimer's disease. Huang, M; Jiang, LF; Ma, QH; Mao, JL; Xu, WX, 2018)
"Treatment with vildagliptin significantly increased the levels of active glucagon-like peptide-1 by 2.36-fold (p ≤ 0.0001) and suppressed glucagon by 8% (p = 0.01), whereas glimepiride significantly increased the levels of insulin and C-peptide by 21% (p = 0.012) and 12% (p = 0.003), respectively."	( Differential effects of vildagliptin and glimepiride on glucose fluctuations in patients with type 2 diabetes mellitus assessed using continuous glucose monitoring. Forst, T; Foteinos, G; He, YL; Kulmatycki, K; Mattapalli, D; Neelakantham, S; Taylor, A, 2013)
"Mice treated with vildagliptin showed normal cytokine production, immune cell activation and lymphocyte trafficking upon TLR activation."	( The dipeptidylpeptidase-IV inhibitors sitagliptin, vildagliptin and saxagliptin do not impair innate and adaptive immune responses. Anz, D; Bourquin, C; Endres, S; Haubner, S; Kruger, S; Rapp, M, 2014)
"Treatment with vildagliptin enhanced blood flow recovery and capillary density in the ischemic limbs of wild-type mice, with accompanying increases in phosphorylation of Akt and endothelial nitric-oxide synthase (eNOS)."	( Vildagliptin stimulates endothelial cell network formation and ischemia-induced revascularization via an endothelial nitric-oxide synthase-dependent mechanism. Bando, YK; Ishii, M; Kambara, T; Kondo, K; Murohara, T; Nishimura, M; Ouchi, N; Shibata, R; Shimizu, Y; Tanigawa, T, 2014)
"Treatment with vildagliptin increased serum levels of insulin, improved beta cell function and improved the lipid profile."	( Vildagliptin induces β-cell neogenesis and improves the lipid profile in a later phase of type 1 diabetes. Costa, DC; de Amorim Miranda, PH; de Lima, WG; Monteiro, OM; Rossoni, JV; Silva, ME, 2015)
"Treatment with vildagliptin dose-dependently decreased plasma DPP-4 activity, increased plasma glucagon-like peptide 1 (GLP-1) levels and attenuated the development of salt-induced hypertension."	( Effect of dipeptidyl peptidase-4 inhibition on circadian blood pressure during the development of salt-dependent hypertension in rats. Fujisawa, Y; Kobori, H; Kohno, M; Masaki, T; Mori, H; Nakano, D; Nishiyama, A; Ohmori, K; Rafiq, K; Rahman, A; Sufiun, A, 2015)
"Treatment with vildagliptin or enalapril significantly decreased oxidative stress, attenuated cardiac fibrosis and improved HRV and LV function."	( Dipeptidyl peptidase-4 inhibitor improves cardiac function by attenuating adverse cardiac remodelling in rats with chronic myocardial infarction. Apaijai, N; Chattipakorn, N; Chattipakorn, SC; Inthachai, T; Kumfu, S; Lekawanvijit, S; Pongkan, W, 2015)
"The treatment with vildagliptin was associated with fewer hypoglycaemic events compared with SUs and was well tolerated with good glycaemic and weight control in patients with T2DM fasting during Ramadan."	( Comparison of hypoglycaemia episodes in people with type-2 diabetes fasting in Ramazan, treated with vildaglipton or sulphonylurea: results of the Pakistani cohort of the VIRTUE study. Fawwad, A; Hasan, MI; Hussain, S; Khan, MA; Khan, MI; Kumar, K; Mahar, SA; Maheshwary, N; Siddiqi, A, 2014)
"The treatment with Vildagliptin significantly suppressed both, the incidence and growth of lung metastases."	( Suppression of lung metastases by the CD26/DPP4 inhibitor Vildagliptin in mice. Baerts, L; De Meester, I; Gil-Bazo, I; Jang, JH; Jungraithmayr, W; Limani, P; Waumans, Y; Weder, W; Yamada, Y, 2015)
"Treatment with vildagliptin (10 mg/kg/day s.c.), a DPP-4 inhibitor, suppressed Beclin-1-Bcl-2 interaction and increased both LC3-II protein level and autophagosomes in the non-infarcted region in OLETF, though it did not normalize AMPK/ULK-1 or mTOR/S6 signaling."	( Inhibition of DPP-4 reduces acute mortality after myocardial infarction with restoration of autophagic response in type 2 diabetic rats. Ishikawa, S; Kouzu, H; Kuno, A; Miki, T; Miura, T; Murase, H; Nishizawa, K; Ogasawara, M; Tanno, M; Tobisawa, T; Yano, T, 2015)
"Treatment with vildagliptin did not significantly change the vascular responses to sodium nitroprusside."	( Vildagliptin improves endothelium-dependent vasodilatation in type 2 diabetes. Netea, MG; Smits, P; Tack, CJ; van Poppel, PC, 2011)
"Treatment with vildagliptin for 1 year was not associated with changes in markers of bone resorption and calcium homeostasis in drug-naïve patients with T2D and mild hyperglycemia."	( Effects of vildagliptin on postprandial markers of bone resorption and calcium homeostasis in recently diagnosed, well-controlled type 2 diabetes patients. Bunck, MC; Diamant, M; Eekhoff, EM; Foley, JE; Heine, RJ; Nijpels, G; Poelma, M; Schweizer, A, 2012)
"Treatment with vildagliptin showed increase in the number of insulin-positive β-cells in islets and improved the expressions of genes and proteins are responsible for insulin secretions."	( Vildagliptin selectively ameliorates GLP-1, GLUT4, SREBP-1c mRNA levels and stimulates β-cell proliferation resulting in improved glucose homeostasis in rats with streptozotocin-induced diabetes. Akarte, AS; Gandhi, S; Srinivasan, BP, )
"Treatment with vildagliptin for 4 weeks improves postprandial plasma triglyceride and apolipoprotein B-48-containing triglyceride-rich lipoprotein particle metabolism after a fat-rich meal. "	( Vildagliptin therapy reduces postprandial intestinal triglyceride-rich lipoprotein particles in patients with type 2 diabetes. Dunning, BE; Foley, JE; Mänttäri, S; Matikainen, N; Mills, D; Schweizer, A; Taskinen, MR; Ulvestad, A, 2006)
"Treatment with vildagliptin restored the islet topography."	( DPP-4 inhibition improves glucose tolerance and increases insulin and GLP-1 responses to gastric glucose in association with normalized islet topography in mice with beta-cell-specific overexpression of human islet amyloid polypeptide. Ahrén, B; Burkey, B; Hughes, TE; Sundler, F; Wierup, N; Winzell, MS, 2007)
"Treatment with vildagliptin did not alter the MTV of Ensure (1657 +/- 308 vs."	( The effect of dipeptidyl peptidase-4 inhibition on gastric volume, satiation and enteroendocrine secretion in type 2 diabetes: a double-blind, placebo-controlled crossover study. Bock, G; Burton, DB; Camilleri, M; Deacon, CF; Foley, JE; Giesler, PD; Rizza, RA; Saylan, ML; Serra, DB; Vella, A, 2008)

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" Careful postmarketing surveillance for adverse effects, especially among the DPP4 inhibitors, and continued evaluation in longer-term studies and in clinical practice are required to determine the role of this new class among current pharmacotherapies for type 2 diabetes."	( Efficacy and safety of incretin therapy in type 2 diabetes: systematic review and meta-analysis. Amori, RE; Lau, J; Pittas, AG, 2007)
" One or more adverse event (AE) was reported by 82."	( Efficacy and safety of vildagliptin monotherapy during 2-year treatment of drug-naïve patients with type 2 diabetes: comparison with metformin. Calle Pascual, A; Dejager, S; Foley, J; Göke, B; Hershon, K; Kerr, D; Schweizer, A; Shao, Q, 2008)
" The incidence of adverse events (AEs), serious AEs and adjudicated cardiovascular events was 74."	( Fifty-two-week efficacy and safety of vildagliptin vs. glimepiride in patients with type 2 diabetes mellitus inadequately controlled on metformin monotherapy. Ahrén, B; Byiers, S; Dejager, S; Ferrannini, E; Fonseca, V; Matthews, D; Shao, Q; Zinman, B, 2009)
" More serious adverse events (SAEs) occurred in vildagliptin- than rosiglitazone-treated patients (12."	( Long-term 2-year safety and efficacy of vildagliptin compared with rosiglitazone in drug-naïve patients with type 2 diabetes mellitus. Maldonado-Lutomirsky, M; Niggli, M; Rosenstock, J, 2009)
" DPP-4 inhibitors are safe and tolerable with no increased risk of adverse events compared to placebo and have a low risk of hypoglycaemia."	( Clinical results of treating type 2 diabetic patients with sitagliptin, vildagliptin or saxagliptin--diabetes control and potential adverse events. Ahrén, B, 2009)
" The overall incidence of any adverse events was similar in both groups (approximately 61%), but the number of serious adverse events was higher in the gliclazide group (8."	( A comparison of efficacy and safety of vildagliptin and gliclazide in combination with metformin in patients with Type 2 diabetes inadequately controlled with metformin alone: a 52-week, randomized study. Filozof, C; Gautier, JF, 2010)
" Overall adverse events (AEs) were lower in the vildagliptin-treated patients compared with that in the voglibose-treated patients (61."	( Efficacy and safety of vildagliptin and voglibose in Japanese patients with type 2 diabetes: a 12-week, randomized, double-blind, active-controlled study. Iwamoto, Y; Kashiwagi, A; Mimori, N; Suzuki, M; Tachibana, H; Terao, S; Yamada, N, 2010)
" The aim of this paper is therefore to assess the general safety and tolerability, including incidences of the most common adverse events (AEs), of vildagliptin based on a large pooled database of Phase II and III clinical trials."	( Assessing the general safety and tolerability of vildagliptin: value of pooled analyses from a large safety database versus evaluation of individual studies. Dejager, S; Foley, JE; Kothny, W; Schweizer, A, 2011)
" Meta-analyses were conducted for HbA1c, weight, fasting plasma glucose (FPG), hypoglycaemia and other adverse events."	( The efficacy and safety of vildagliptin in patients with type 2 diabetes: a meta-analysis of randomized clinical trials. Cai, L; Cai, Y; Liu, P; Lu, ZJ; Zhang, Y, 2012)
" In addition, compared to comparators, vildagliptin was not associated with an increase in overall risk for any adverse events [RR, 0·97 (95% CI, 0·94-0·99)]."	( The efficacy and safety of vildagliptin in patients with type 2 diabetes: a meta-analysis of randomized clinical trials. Cai, L; Cai, Y; Liu, P; Lu, ZJ; Zhang, Y, 2012)
"Vildagliptin is effective in glycaemic control with a low risk of hypoglycaemia and other adverse reactions."	( The efficacy and safety of vildagliptin in patients with type 2 diabetes: a meta-analysis of randomized clinical trials. Cai, L; Cai, Y; Liu, P; Lu, ZJ; Zhang, Y, 2012)
" In patients with moderate RI, similar proportions of patients experienced any adverse event (AE) (84 vs."	( One-year safety, tolerability and efficacy of vildagliptin in patients with type 2 diabetes and moderate or severe renal impairment. Groop, PH; Kothny, W; Lukashevich, V; Shao, Q, 2012)
"Teneligliptin is a novel DPP-4 inhibitor in development for treating type 2 diabetes mellitus that does not require dose adjustment for diabetic patients with end-stage renal disease; however, it had not been known whether or not teneligliptin is safe or potent in dialysis patients."	( Safety and efficacy of teneligliptin: a novel DPP-4 inhibitor for hemodialysis patients with type 2 diabetes. Kosaka, T; Kuwahara, Y; Nakamura, K; Otsuki, H; Shimomura, F; Tsukamoto, T, 2014)
" Adverse events were generally mild and occurred at similar rates in both groups."	( Efficacy and safety of vildagliptin in new-onset diabetes after kidney transplantation--a randomized, double-blind, placebo-controlled trial. Antlanger, M; Döller, D; Haidinger, M; Hecking, M; Kopecky, C; Kovarik, JJ; Pacini, G; Pleiner, J; Säemann, MD; Stemer, G; Werzowa, J, 2014)
" Open-label design and under reporting of adverse events are limitations of this post hoc analysis."	( Real-life efficacy and safety of vildagliptin compared with sulfonylureas as add-on to metformin in patients with type 2 diabetes mellitus in Germany. Bader, G; Dworak, M; Göke, R; Gruenberger, JB, 2014)
" The rate of adverse events was comparable in both groups."	( [Efficacy and safety of vildagliptin as a second-line therapy vs other oral antidiabetic agents in patients with type 2 diabetes: Czech results within the worldwide prospective cohort EDGE study]. Brada, M; Dohnalová, L; Edelsberger, T; Gerle, J; Haluzík, M; Houdová, J; Veselá, V, 2013)
"This review considers the pharmacokinetic profile, adverse effects and drug interactions of DPP-4 inhibitors."	( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected]. Athyros, VG; Elisaf, MS; Filippatos, TD, 2014)
" However, DPP-4 inhibitors have certain differences in their pharmacokinetic properties that may be associated with different clinical effects and adverse event profiles."	( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected]. Athyros, VG; Elisaf, MS; Filippatos, TD, 2014)
" Glycosylated hemoglobin (HbA1c) values, fasting and postprandial blood glucose (FBG and P2BG), body weight, body mass index (BMI), episodes of hypoglycemia and adverse events were evaluated."	( Efficacy and safety comparison of add-on therapy with liraglutide, saxagliptin and vildagliptin, all in combination with current conventional oral hypoglycemic agents therapy in poorly controlled Chinese type 2 diabetes. Ding, M; Li, CJ; Liu, XJ; Yu, DM; Yu, P; Yu, Q; Zhang, QM, 2014)
" In total, 136 adverse events (AEs) were observed in 71 (10."	( Real-life safety and efficacy of vildagliptin as add-on to metformin in patients with type 2 diabetes in Turkey--GALATA study. Akin, F; Ar, IB; Ayvaz, G; Dokmetas, HS; Keskin, L; Tasan, E; Uren, E, 2015)
" The main outcomes were changes in glycosylated hemoglobin and the occurrence of adverse effects."	( [Safety and efficacy of Vildagliptin in real life Chilean diabetic patients]. Godoy J, G; Gutiérrez, V; Montecinos, M; Yenes, A, 2015)
" The primary endpoint was occurrence of major adverse CV events (MACEs; myocardial infarction, stroke and CV death)."	( Cardiovascular and heart failure safety profile of vildagliptin: a meta-analysis of 17 000 patients. Del Prato, S; Evans, M; Kothny, W; Lukashevich, V; McInnes, G; Schweizer, A; Shao, Q; Stumvoll, M, 2015)
" The key secondary endpoints included percentage of patients achieving target HbA1c without adverse gastrointestinal (GI) events and mean change in fasting plasma glucose (FPG) from baseline to week 24."	( Efficacy and safety of combination therapy with vildagliptin and metformin versus metformin uptitration in Chinese patients with type 2 diabetes inadequately controlled with metformin monotherapy: a randomized, open-label, prospective study (VISION). Ji, LN; Li, H; Li, Q; Li, QF; Lu, JM; Pan, CY; Peng, YD; Tian, HM; Wang, BH; Wang, L; Yao, C; Zhao, ZG; Zhu, DL, 2016)
" Safety was assessed by reporting of adverse events and serious adverse events (SAEs)."	( Effectiveness and safety of vildagliptin and vildagliptin add-on to metformin in real-world settings in Egypt - results from the GUARD study. Rakha, S; Shelbaya, S, 2017)
" The IRRs and their 95% CIs were close to 1, demonstrating no increased risk of adverse CV events, including the risk of CHF, with vildagliptin vs other NIADs in real-world conditions."	( Cardiovascular safety of vildagliptin in patients with type 2 diabetes: A European multi-database, non-interventional post-authorization safety study. Chu, C; de Vries, F; Kothny, W; Lopez-Leon, S; Schlienger, R; Serban, C; Williams, R, 2017)
" In terms of safety, the rate of adverse events in patients with T2D who received empagliflozin plus metformin was relatively lower when compared with saxagliptin plus metformin (OR=0."	( A network meta-analysis for efficacy and safety of seven regimens in the treatment of type II diabetes. Hua, WC; Li, CM; Liu, Q; Wang, H; Wang, LG, 2017)
" Saxagliptin showed higher adverse reactions than acarbose and vildagliptin."	( A comparative study of acarbose, vildagliptin and saxagliptin intended for better efficacy and safety on type 2 diabetes mellitus treatment. Chen, Y; Dong, B; Hu, J; Wang, J; Wang, Y; Wang, Z, 2021)
" The study endpoints were mean changes from baseline (CFB) in HbA1c (primary), fasting plasma glucose (FPG), post-prandial plasma glucose (PPG), body weight (BW) and blood pressure (BP) for efficacy and adverse events (AE) monitoring for safety assessments."	( Efficacy and Safety of a Fixed Dose Combination of Remogliflozin Etabonate and Vildagliptin in Patients with Type-2 Diabetes Mellitus: A Randomized, Active-Controlled, Double-Blind, Phase III Study. Barkatestrong/Strong, H; Khaladkar, K; Mohan, B; Suryawanshi, S, 2022)
" In terms of safety, the vildagliptin plus metformin as combination therapy did not increase risk of total adverse events (AEs) [RR=0."	( Efficacy and safety of combination therapy with vildagliptin and metformin vs. metformin monotherapy for Type 2 Diabetes Mellitus therapy: a meta-analysis. Cao, L; Ding, Y; Dong, F; Li, Y; Lin, M; Lin, S; Liu, Y; Qu, Y, 2022)

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"To assess the pharmacokinetic and pharmacodynamic characteristics and tolerability of vildagliptin at doses of 10 mg, 25 mg and 100 mg twice daily following oral administration in patients with type 2 diabetes."	( Pharmacokinetics and pharmacodynamics of vildagliptin in patients with type 2 diabetes mellitus. Campestrini, J; Deacon, CF; He, YL; Holst, JJ; Ligueros-Saylan, M; Nielsen, JC; Riviere, GJ; Schwartz, S; Serra, D; Wang, Y, 2007)
" This open-label, randomized, 3-period crossover study investigated the potential for pharmacokinetic interactions in 18 healthy subjects during coadministration of vildagliptin and digoxin."	( Evaluation of pharmacokinetic interactions between vildagliptin and digoxin in healthy volunteers. Bizot, MN; Dole, WP; He, YL; Howard, D; Leon, S; Ligueros-Saylan, M; Riviere, GJ; Sabo, R; Sunkara, G, 2007)
" Noncompartmental analysis and population pharmacokinetic modelling were performed."	( The absolute oral bioavailability and population-based pharmacokinetic modelling of a novel dipeptidylpeptidase-IV inhibitor, vildagliptin, in healthy volunteers. Balez, S; Campestrini, J; He, YL; Howard, D; Laurent, A; Ligueros-Saylan, M; Sabo, R; Sadler, BM; Wang, Y, 2007)
"Both noncompartmental analysis and population pharmacokinetic modelling estimated the absolute oral bioavailability of vildagliptin to be 85%."	( The absolute oral bioavailability and population-based pharmacokinetic modelling of a novel dipeptidylpeptidase-IV inhibitor, vildagliptin, in healthy volunteers. Balez, S; Campestrini, J; He, YL; Howard, D; Laurent, A; Ligueros-Saylan, M; Sabo, R; Sadler, BM; Wang, Y, 2007)
" There fore, this study was conducted to determine the potential for pharmacokinetic drug-drug interaction between vildagliptin and simvastatin at steady-state."	( Evaluation of the potential for steady-state pharmacokinetic interaction between vildagliptin and simvastatin in healthy subjects. Ayalasomayajula, SP; Campestrini, J; Dole, K; He, YL; Humbert, H; Ligueros-Saylan, M; Sunkara, G; Wang, Y, 2007)
" Pharmacokinetic and statistical analyses were performed using WinNonlin and SAS, respectively."	( Evaluation of the potential for steady-state pharmacokinetic interaction between vildagliptin and simvastatin in healthy subjects. Ayalasomayajula, SP; Campestrini, J; Dole, K; He, YL; Humbert, H; Ligueros-Saylan, M; Sunkara, G; Wang, Y, 2007)
"We conducted 3 open-label, multiple-dose, 3-period, randomized, crossover studies in healthy subjects to assess the potential pharmacokinetic interaction between vildagliptin, a novel dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes, and representatives of 3 commonly prescribed antihypertensive drug classes: (1) the calcium channel blocker, amlodipine; (2) the angiotensin receptor blocker, valsartan; and (3) the angiotensin-converting enzyme inhibitor, ramipril."	( Vildagliptin, a novel dipeptidyl peptidase IV inhibitor, has no pharmacokinetic interactions with the antihypertensive agents amlodipine, valsartan, and ramipril in healthy subjects. Campestrini, J; Dole, K; Dole, WP; He, YL; Howard, D; Ligueros-Saylan, M; Marion, A; Pommier, F; Sabo, R; Sunkara, G; Wang, Y; Zhao, C, 2008)
" Two studies were performed to determine the potential for pharmacokinetic and pharmacodynamic interactions between vildagliptin and the sulfonylurea, glyburide, or pioglitazone in patients with Type 2 diabetes."	( Evaluation of pharmacokinetic and pharmacodynamic interaction between the dipeptidyl peptidase IV inhibitor vildagliptin, glyburide and pioglitazone in patients with Type 2 diabetes. Balez, S; Bullock, J; Dole, WP; He, YL; Jarugula, V; Ligueros-Saylan, M; Riviere, GJ; Schwartz, S; Serra, D; Wang, Y, 2008)
" Changes in AUC and Cmax during combination treatment were small ( pound 15%), and 90% confidence intervals for the geometric mean ratios (drug coadministration/monotherapy) were generally contained within the acceptance range for bioequivalence (0."	( Evaluation of pharmacokinetic and pharmacodynamic interaction between the dipeptidyl peptidase IV inhibitor vildagliptin, glyburide and pioglitazone in patients with Type 2 diabetes. Balez, S; Bullock, J; Dole, WP; He, YL; Jarugula, V; Ligueros-Saylan, M; Riviere, GJ; Schwartz, S; Serra, D; Wang, Y, 2008)
"0 hours) across the dose range of 25 to 200 mg and was quickly eliminated with a terminal elimination half-life (t1/2) of approximately 2 hours."	( Pharmacokinetics and pharmacodynamics of vildagliptin in healthy Chinese volunteers. Deckert, F; Dole, WP; He, YL; Hu, P; Jiang, J; Kjems, L; Liu, D; Yin, Q, 2009)
" Blood samples for pharmacokinetic sampling were taken frequently on the final day (Day 5) of each treatment period."	( Study of the pharmacokinetic interaction of vildagliptin and metformin in patients with type 2 diabetes. Dole, WP; He, YL; Herron, J; Ligueros-Saylan, M; Picard, F; Sabo, R; Wang, Y, 2009)
" PK/pharmacodynamics characteristics, that is, sufficiently prolonged half-life and sustained DPP-4 enzyme inactivation, generally allow one single oral administration per day for the management of T2DM; the only exception is vildagliptin for which a twice-daily administration is recommended because of a shorter half-life."	( Pharmacokinetics of dipeptidylpeptidase-4 inhibitors. Scheen, AJ, 2010)
"Vildagliptin demonstrated similar pharmacokinetic and pharmacodynamic effects in Japanese patients to those observed previously in non-Japanese patients with Type 2 diabetes."	( Pharmacokinetics and pharmacodynamics of vildagliptin in Japanese patients with type 2 diabetes. He, YL; Ito, H; Sekiguchi, K; Terao, S; Yamaguchi, M, 2010)
" Vildagliptin possesses several desirable pharmacokinetic properties that contribute to its lower variability and low potential for drug interaction."	( Clinical pharmacokinetics and pharmacodynamics of vildagliptin. He, YL, 2012)
" By utilizing the TMDD approach, slow dissociation of vildagliptin from DPP-4 was found in patients and the half-life of hydrolysis by DPP-4 estimated."	( Mechanism-based population pharmacokinetic modelling in diabetes: vildagliptin as a tight binding inhibitor and substrate of dipeptidyl peptidase IV. He, YL; Jusko, WJ; Landersdorfer, CB, 2012)
"Reliable prediction of two fundamental human pharmacokinetic (PK) parameters, systemic clearance (CL) and apparent volume of distribution (Vd), determine the size and frequency of drug dosing and are at the heart of drug discovery and development."	( Quantitative structure-activity relationship models of clinical pharmacokinetics: clearance and volume of distribution. Gombar, VK; Hall, SD, 2013)
"Compared to age-, gender-, BMI-matched subjects with normal renal function, the mean AUC of vildagliptin after 14 days in patients with mild, moderate, and severe RI increased by 40%, 71%, and 100%, respectively, and the Cmax of vildagliptin showed similar and minimal increases of 37%, 32% and 36%, respectively."	( Pharmacokinetics of vildagliptin in patients with varying degrees of renal impairment. He, YL; Kulmatycki, K; Ligueros-Saylan, M; Reynolds, C; Taylor, A; Zhang, Y; Zhou, W, 2013)
"To assess the extent of pharmacokinetic and pharmacodynamic interaction between vildagliptin, a potent and selective inhibitor of dipeptidyl peptidase IV (DPP-4) enzyme, and voglibose, an α-glucosidase inhibitor widely prescribed in Japan, when coadministered in Japanese patients with Type 2 diabetes."	( Pharmacokinetic and pharmacodynamic interaction of vildagliptin and voglibose in Japanese patients with Type 2 diabetes. Furihata, K; He, YL; Kulmatycki, K; Mita, S; Saji, T; Sekiguchi, K; Yamaguchi, M, 2013)
" Co-administration led to significantly better pharmacodynamic response compared with each treatment alone, including higher active GLP-1 and lower glucose levels."	( Pharmacokinetic and pharmacodynamic interaction of vildagliptin and voglibose in Japanese patients with Type 2 diabetes. Furihata, K; He, YL; Kulmatycki, K; Mita, S; Saji, T; Sekiguchi, K; Yamaguchi, M, 2013)
"This review considers the pharmacokinetic profile, adverse effects and drug interactions of DPP-4 inhibitors."	( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected]. Athyros, VG; Elisaf, MS; Filippatos, TD, 2014)
" However, DPP-4 inhibitors have certain differences in their pharmacokinetic properties that may be associated with different clinical effects and adverse event profiles."	( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected]. Athyros, VG; Elisaf, MS; Filippatos, TD, 2014)
"The availability of intravenous and oral pharmacokinetic data in animals enabled the allometry scaling of 6 DPP-IV inhibitors."	( Retrospective and Prospective Human Intravenous and Oral Pharmacokinetic Projection of Dipeptidyl peptidase-IV Inhibitors Using Simple Allometric Principles - Case Studies of ABT-279, ABT-341, Alogliptin, Carmegliptin, Sitagliptin and Vildagliptin. Bhamidipati, RK; Gilibili, RR; Mullangi, R; Srinivas, NR, 2015)
" A population pharmacokinetic (PPK) analysis of pooled metformin concentration-time data was performed to evaluate whether country-sourced metformin is a significant covariate."	( Population pharmacokinetic modeling and noncompartmental analysis demonstrated bioequivalence between metformin component of metformin/vildagliptin fixed-dose combination products and metformin immediate-release tablet sourced from various countries. Chitnis, SD; Han, Y; Kulmatycki, K; Mita, S; Sunkara, G; Yamaguchi, M; Zhao, R, 2016)
" To determine the rate of DPP-4 inhibition induced by these inhibitors, pharmacokinetic and pharmacodynamic parameters were used to theoretically examine the relationship between the rate of DPP-4 inhibition and clinical efficacy following the administration of four different DPP-4 inhibitors (sitagliptin, vildagliptin, alogliptin, linagliptin) by focusing on the increase in the level of glucagon-like peptide-1 (GLP-1) induced by their administration."	( Evaluation of drug efficacy of DPP-4 inhibitors based on theoretical analysis with pharmacokinetics and pharmacodynamics. Kimura, K; Takayanagi, R; Uchida, T; Yamada, Y, 2017)
" With our continuous interest in developing AM2-S31N inhibitors as oral influenza antivirals, we report here the progress of optimizing the in vitro pharmacokinetic (PK) properties of AM2-S31N inhibitors."	( In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses. Hau, RK; Hu, Y; Ma, C; Musharrafieh, R; Wang, J; Wang, Y; Xu, S; Zhang, Y, 2018)
"The 5/6 nephrectomized (5/6 Nx) rat model, to simulate chronic renal failure (CRF) patients, combined with kidney slices and transporter studies in vitro were used to assess this pharmacokinetic differences."	( Mechanistic Study on the Effect of Renal Impairment on the Pharmacokinetics of Vildagliptin and its Carboxylic Acid Metabolite. Chen, X; Chen, Z; Guo, Z; Hu, J; Kong, F; Xie, N, 2022)

Excerpt	Reference
"The purpose of this study was to assess the efficacy and tolerability of the dipeptidyl peptidase-4 inhibitor vildagliptin in combination with the thiazolidinedione (TZD) pioglitazone in patients with type 2 diabetes (T2DM)."	( Vildagliptin in combination with pioglitazone improves glycaemic control in patients with type 2 diabetes failing thiazolidinedione monotherapy: a randomized, placebo-controlled study. Baron, MA; Dejager, S; Garber, AJ; Rochotte, E; Schweizer, A, 2007)
"Patients with type 2 diabetes mellitus (T2DM) are generally treated with many pharmacological compounds and are exposed to a high risk of drug-drug interactions."	( Dipeptidylpeptidase-4 inhibitors (gliptins): focus on drug-drug interactions. Scheen, AJ, 2010)
"73 m(2), 100 randomized to vildagliptin, 78 randomized to placebo), all of whom were receiving insulin therapy (alone or in combination with an oral antidiabetic agent) for longstanding type 2 diabetes (mean approximately 19 years)."	( Efficacy of vildagliptin in combination with insulin in patients with type 2 diabetes and severe renal impairment. Dickinson, S; Foley, JE; Groop, PH; Kothny, W; Lukashevich, V; Schweizer, A, 2013)
"With vildagliptin in combination with insulin, the adjusted mean change (AMΔ) in HbA(1c) from baseline (7."	( Efficacy of vildagliptin in combination with insulin in patients with type 2 diabetes and severe renal impairment. Dickinson, S; Foley, JE; Groop, PH; Kothny, W; Lukashevich, V; Schweizer, A, 2013)
" The data support the use of vildagliptin in combination with insulin in general and, in line with emerging clinical practice, suggest that treating patients with vildagliptin, metformin, and basal insulin could be an attractive therapeutic option."	( Clinical evidence and mechanistic basis for vildagliptin's effect in combination with insulin. Ahrén, B; Foley, JE; Kothny, W; Schweizer, A, 2013)
" We evaluated the effects of long-term treatment with vildagliptin, a DPP-4 inhibitor, on metabolic parameters and β-cell function, in combination with miglitol, an alpha-glucosidase inhibitor, in diet-controlled db/db mice."	( Beneficial effects of vildagliptin combined with miglitol on glucose tolerance and islet morphology in diet-controlled db/db mice. Abe, H; Fujitani, Y; Hara, A; Ishibashi, K; Kanazawa, A; Kawamori, R; Komiya, K; Ogihara, T; Tamaki, M; Uchida, T; Watada, H, 2013)
" We report here that a low-carbohydrate diet combined with an SGLT2 inhibitor was effective and safe to treat refractory hyperglycemia in the perioperative period in a type 2 diabetes patient complicated with a high titer of insulin antibodies."	( Low-carbohydrate diet combined with SGLT2 inhibitor for refractory hyperglycemia caused by insulin antibodies. Abiru, N; Ando, T; Horie, I; Kawakami, A; Shigeno, R, 2016)
"Vildagliptin efficacy in combination with metformin for early treatment of T2DM (VERIFY) is an ongoing, multicentre, randomized controlled trial aiming to demonstrate the clinical benefits of glycaemic durability and glucose control achieved with an early combination therapy in newly-diagnosed type 2 diabetes (T2DM) patients."	( A pre-specified statistical analysis plan for the VERIFY study: Vildagliptin efficacy in combination with metformin for early treatment of T2DM. Bader, G; Chiang, Y; Del Prato, S; Han, J; Matthews, DR; Paldánius, PM; Proot, P; Stumvoll, M, 2019)

Excerpt	Reference
"1-[[(3-Hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties."	( Inhibition of dipeptidyl-peptidase IV catalyzed peptide truncation by Vildagliptin ((2S)-{[(3-hydroxyadamantan-1-yl)amino]acetyl}-pyrrolidine-2-carbonitrile). Brandt, I; Chen, X; De Meester, I; Joossens, J; Lambeir, AM; Maes, MB; Scharpé, S, 2005)
" The objective of this study was to assess the absolute oral bioavailability of vildagliptin by comparing the systemic exposure after oral and intravenous administration in healthy volunteers."	( The absolute oral bioavailability and population-based pharmacokinetic modelling of a novel dipeptidylpeptidase-IV inhibitor, vildagliptin, in healthy volunteers. Balez, S; Campestrini, J; He, YL; Howard, D; Laurent, A; Ligueros-Saylan, M; Sabo, R; Sadler, BM; Wang, Y, 2007)
"Both noncompartmental analysis and population pharmacokinetic modelling estimated the absolute oral bioavailability of vildagliptin to be 85%."	( The absolute oral bioavailability and population-based pharmacokinetic modelling of a novel dipeptidylpeptidase-IV inhibitor, vildagliptin, in healthy volunteers. Balez, S; Campestrini, J; He, YL; Howard, D; Laurent, A; Ligueros-Saylan, M; Sabo, R; Sadler, BM; Wang, Y, 2007)
"Vildagliptin is rapidly and well absorbed with an estimated absolute bioavailability of 85%."	( The absolute oral bioavailability and population-based pharmacokinetic modelling of a novel dipeptidylpeptidase-IV inhibitor, vildagliptin, in healthy volunteers. Balez, S; Campestrini, J; He, YL; Howard, D; Laurent, A; Ligueros-Saylan, M; Sabo, R; Sadler, BM; Wang, Y, 2007)
" The rate of absorption of metformin was decreased when given with food, as reflected by the prolonged t(max) (2-4 h) and reduction in C(max) (by 26%), but the extent of absorption was not changed."	( Effect of food on the pharmacokinetics of a vildagliptin/metformin (50/1000 mg) fixed-dose combination tablet in healthy volunteers. Campestrini, J; Flannery, B; He, YL; Jarugula, V; Leon, S; Ligueros-Saylan, M; Zinny, MA, 2008)
" Moderate to high bioavailability was observed in both species (45-100%)."	( Disposition of vildagliptin, a novel dipeptidyl peptidase 4 inhibitor, in rats and dogs. Filipeck, R; Fischer, V; Flood, D; He, H; Howard, D; Kramp, R; Smith, H; Tran, P; Yin, H, 2009)
"Although considerably less potent than specified DPP-IV inhibitors, the possibility that some of the beneficial actions of nateglinide are indirectly mediated through DPP-IV inhibition and increased bioavailability of GIP and other incretins merits consideration."	( Insulinotropic actions of nateglinide in type 2 diabetic patients and effects on dipeptidyl peptidase-IV activity and glucose-dependent insulinotropic polypeptide degradation. Bell, PM; Duffy, NA; Flatt, PR; Green, BD; Lindsay, JR; McKillop, AM; O'Harte, FP; Patterson, S, 2009)
" All together gliptins have a good oral bioavailability which is not significantly influenced by food intake."	( Pharmacokinetics of dipeptidylpeptidase-4 inhibitors. Scheen, AJ, 2010)
" Lipoyl vildagliptin might have very high CL/F values and V(d)/F values, which indicated that the bioavailability of this drug might be low or lipoyl vildagliptin might distribute extensively or accumulate in tissues in view of its high liposolubility."	( Pharmacokinetics of lipoyl vildagliptin, a novel dipeptidyl peptidase IV inhibitor after oral administration in rats. Liu, H; Wang, W; Wang, X; Xu, W; Zhang, D, 2010)
" We also demonstrated a markedly enhanced oral bioavailability of the prodrugs versus the parent drug in mice."	( Dipeptidyl peptidase IV dependent water-soluble prodrugs of highly lipophilic bicyclic nucleoside analogues. Andrei, G; Balzarini, J; Camarasa, MJ; De Meester, I; Diez-Torrubia, A; Snoeck, R; Velázquez, S, 2011)
" Following oral administration, vildagliptin is rapidly and well absorbed with an absolute bioavailability of 85%."	( Clinical pharmacokinetics and pharmacodynamics of vildagliptin. He, YL, 2012)
"05 μM) and good oral bioavailability (F = 53."	( Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors. Dong, T; Gao, Z; Ji, X; Jiang, H; Li, J; Li, Z; Liu, H; Su, M; Wan, X; Wang, J; Xia, C; Zhang, L; Zhao, L, 2014)
" The rate of absorption of metformin decreased when administered under fed condition, as reflected by a prolonged t(max) (3 hours in fasted state vs."	( Bioequivalence and food effect assessment for vildagliptin/metformin fixed-dose combination tablets relative to free combination of vildagliptin and metformin in Japanese healthy subjects. Chitnis, SD; He, YL; Kulmatycki, K; Mita, S; Salunke, A; Suzuki, H; Zhou, W, 2016)
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)

Excerpt	Reference
" This study examined acute (single dose) and chronic (once-a-day dosing for 21 days) effects of the DPP-4 inhibitor vildagliptin (0."	( Acute and chronic effects of the incretin enhancer vildagliptin in insulin-resistant rats. Balkan, B; Bolognese, L; Burkey, BF; Hughes, TE; Li, X; Mone, M; Russell, M; Wang, PR, 2005)
" There was no apparent dose-response in the overall population; however, in patients with high baseline HbA1c, there were greater reductions with either 100 mg dose regimen (Delta=-1."	( Vildagliptin in drug-naïve patients with type 2 diabetes: a 24-week, double-blind, randomized, placebo-controlled, multiple-dose study. Dejager, S; Foley, JE; Razac, S; Schweizer, A, 2007)
"This randomized, open-label, placebo-controlled, 7-period crossover study assessed dose-response relationships following single oral doses (10-400 mg) of vildagliptin in 16 patients with type 2 diabetes mellitus."	( Pharmacodynamics of vildagliptin in patients with type 2 diabetes during OGTT. Bullock, JM; Deacon, CF; Dunning, BE; Foley, JE; He, YL; Holst, JJ; Ligueros-Saylan, M; Wang, Y, 2007)
" No dosage adjustment of either warfarin or vildagliptin is necessary when these drugs are co-medicated."	( Effect of the novel oral dipeptidyl peptidase IV inhibitor vildagliptin on the pharmacokinetics and pharmacodynamics of warfarin in healthy subjects. Dole, WP; He, YL; Howard, D; Leon, S; Ligueros-Saylan, M; Riviere, GJ; Rosenberg, M; Sabo, R; Sunkara, G, 2007)
" No adjustment in dosage based on pharmacokinetic considerations is required should vildagliptin be coadministered with amlodipine, valsartan, or ramipril in patients with type 2 diabetes and hypertension."	( Vildagliptin, a novel dipeptidyl peptidase IV inhibitor, has no pharmacokinetic interactions with the antihypertensive agents amlodipine, valsartan, and ramipril in healthy subjects. Campestrini, J; Dole, K; Dole, WP; He, YL; Howard, D; Ligueros-Saylan, M; Marion, A; Pommier, F; Sabo, R; Sunkara, G; Wang, Y; Zhao, C, 2008)
" The mean plasma concentration 24 h after dose after 12-week daily dosing with 1500 mg/kg/day in mice was 2279 nM."	( Adverse effects of dipeptidyl peptidases 8 and 9 inhibition in rodents revisited. Burkey, BF; Foley, JE; Hassiepen, U; Hoffmann, PK; Juedes, M; Trappe, J, 2008)
" Vildagliptin 25 to 200 mg qd exhibits approximately dose-proportional pharmacokinetics with no evidence of accumulation after multiple dosing in healthy Chinese participants."	( Pharmacokinetics and pharmacodynamics of vildagliptin in healthy Chinese volunteers. Deckert, F; Dole, WP; He, YL; Hu, P; Jiang, J; Kjems, L; Liu, D; Yin, Q, 2009)
" The primary objective was to demonstrate that HbA(1c) reduction with once-daily vildagliptin 100 mg AM dosing is superior to placebo."	( Efficacy and tolerability of vildagliptin in patients with type 2 diabetes inadequately controlled with metformin monotherapy. Goodman, M; Penman, J; Thurston, H, 2009)
" In clinical trials, once or twice daily dosing with vildagliptin (up to 100 mg day(-1)) has been shown to reduce endogenous glucose production and fasting plasma glucose in patients with type 2 diabetes."	( Hormonal and metabolic effects of morning or evening dosing of the dipeptidyl peptidase IV inhibitor vildagliptin in patients with type 2 diabetes. Dole, WP; Foley, J; He, YL; Ligueros-Saylan, M; Schwartz, SL; Valencia, J; Zhang, Y, 2010)
"Once daily dosing with vildagliptin 100 mg for 28 days improved glycaemic control in patients with type 2 diabetes independent of whether vildagliptin was administered in the morning or evening."	( Hormonal and metabolic effects of morning or evening dosing of the dipeptidyl peptidase IV inhibitor vildagliptin in patients with type 2 diabetes. Dole, WP; Foley, J; He, YL; Ligueros-Saylan, M; Schwartz, SL; Valencia, J; Zhang, Y, 2010)
"Forty-eight patients were randomized to once daily vildagliptin 100 mg administered before breakfast or before dinner for 28 days then crossed over to the other dosing regimen."	( Hormonal and metabolic effects of morning or evening dosing of the dipeptidyl peptidase IV inhibitor vildagliptin in patients with type 2 diabetes. Dole, WP; Foley, J; He, YL; Ligueros-Saylan, M; Schwartz, SL; Valencia, J; Zhang, Y, 2010)
"5,24 h) was greater with evening than morning dosing (-336 vs."	( Hormonal and metabolic effects of morning or evening dosing of the dipeptidyl peptidase IV inhibitor vildagliptin in patients with type 2 diabetes. Dole, WP; Foley, J; He, YL; Ligueros-Saylan, M; Schwartz, SL; Valencia, J; Zhang, Y, 2010)
"Both morning and evening dosing of once daily vildagliptin 100 mg significantly reduced post-prandial glucose in patients with type 2 diabetes; only evening dosing significantly decreased fasting plasma glucose."	( Hormonal and metabolic effects of morning or evening dosing of the dipeptidyl peptidase IV inhibitor vildagliptin in patients with type 2 diabetes. Dole, WP; Foley, J; He, YL; Ligueros-Saylan, M; Schwartz, SL; Valencia, J; Zhang, Y, 2010)
" There are important differences in the kinetics of the interaction of different gliptins with the catalytic site of DPP-4, which may lead to varying pharmacokinetics, pharmacodynamics and dosing regimens."	( Clinical evidence and mechanistic basis for vildagliptin's action when added to metformin. Ahrén, B; Bosi, E; Foley, JE, 2011)
" Placebo-adjusted mean change from baseline in QT interval, heart-rate-corrected QT intervals by Fridericia's (QTcF) or Bazett's (QTcB) formula, and PR and QRS intervals were compared at each time-point (time-matched analysis) and for values averaged across the dosing period (time-averaged analysis)."	( Thorough QT study of the effects of vildagliptin, a dipeptidyl peptidase IV inhibitor, on cardiac repolarization and conduction in healthy volunteers. Dole, WP; He, YL; Ligueros-Saylan, M; Serra, D; Wang, Y; Zhang, Y, 2011)
" Furthermore, in patients with higher baseline GA levels, a higher vildagliptin dosage was required to produce a noticeable effect."	( The dipeptidyl peptidase-4 (DPP-4) inhibitor vildagliptin improves glycemic control in type 2 diabetic patients undergoing hemodialysis. Abe, M; Higuchi, T; Ito, M; Kikuchi, F; Maruyama, N; Okada, K; Sasaki, H; Soma, M; Tsuchida, M, 2011)
" The objective of this model-based meta-analysis was to describe the time course of HbA1c response after dosing with alogliptin (ALOG), saxagliptin (SAXA), sitagliptin (SITA), or vildagliptin (VILD)."	( Quantitative model of the relationship between dipeptidyl peptidase-4 (DPP-4) inhibition and response: meta-analysis of alogliptin, saxagliptin, sitagliptin, and vildagliptin efficacy results. Barbee, T; Correa, I; Fredrickson, J; Gibbs, JP; Gibbs, MA; Lin, SL; Smith, B, 2012)
" The present model can be used to predict the effects of other dosage regimens of vildagliptin on DPP-4 inhibition, active GLP-1, glucose and insulin concentrations, or can be modified and applied to other incretin-related anti-diabetes therapies."	( Mechanism-based population modelling of the effects of vildagliptin on GLP-1, glucose and insulin in patients with type 2 diabetes. He, YL; Jusko, WJ; Landersdorfer, CB, 2012)
" This model can be used to predict DPP-4 inhibition effects of other dosage regimens and be modified for other DPP-4 inhibitors to differentiate their properties."	( Mechanism-based population pharmacokinetic modelling in diabetes: vildagliptin as a tight binding inhibitor and substrate of dipeptidyl peptidase IV. He, YL; Jusko, WJ; Landersdorfer, CB, 2012)
"A simple, precise and stability-indicating reversed-phase liquid chromatography method was developed and validated for the determination of vildagliptin (VLG) in pharmaceutical dosage form."	( Stability-indicating RP-LC method for the determination of vildagliptin and mass spectrometry detection for a main degradation product. Barden, AT; Salamon, B; Schapoval, EE; Steppe, M, 2012)
"One hundred seventy-one type 2 diabetes patients, naive to antidiabetes therapy and with poor glycemic control, were instructed to take metformin for 8±2 months up to a mean dosage of 2,500±500 mg/day; then they were randomly assigned to add vildaglipin 50 mg twice a day or placebo for 12 months."	( Vildagliptin added to metformin on β-cell function after a euglycemic hyperinsulinemic and hyperglycemic clamp in type 2 diabetes patients. Bianchi, L; Bonaventura, A; Carbone, A; Cicero, AF; Derosa, G; Fogari, E; Maffioli, P; Ragonesi, PD; Romano, D, 2012)
" Finally, the rationale for vildagliptin dosing frequency in monotherapy is discussed."	( Evidence to support the use of vildagliptin monotherapy in the treatment of type 2 diabetes mellitus. Dejager, S; Foley, JE; Schweizer, A, 2012)
"Reliable prediction of two fundamental human pharmacokinetic (PK) parameters, systemic clearance (CL) and apparent volume of distribution (Vd), determine the size and frequency of drug dosing and are at the heart of drug discovery and development."	( Quantitative structure-activity relationship models of clinical pharmacokinetics: clearance and volume of distribution. Gombar, VK; Hall, SD, 2013)
"A total of 96 subjects were enrolled, and each subject received vildagliptin 50 mg dosed orally once daily for 14 days."	( Pharmacokinetics of vildagliptin in patients with varying degrees of renal impairment. He, YL; Kulmatycki, K; Ligueros-Saylan, M; Reynolds, C; Taylor, A; Zhang, Y; Zhou, W, 2013)
" The differences in the reductions achieved in FPG and HbA1c with the two dosing regimens were significant."	( Glycemic effects of vildagliptin and metformin combination therapy in Indian patients with type 2 diabetes: an observational study. Chatterjee, S, 2014)
"A simple, precise and stability-indicating HPLC method was developed and validated for the simultaneous determination of metformin hydrochloride (MET) and vildagliptin (VLG) in pharmaceutical dosage forms."	( Development of validated stability indicating assay method for simultaneous estimation of metformin hydrochloride and vildagliptin by RP-HPLC. Pradeepkumar, M; Rao, VJ; Satheeshkumar, N; Shanthikumar, S, 2014)
" It is dosed orally and can be used safely as monotherapy or in combination with other oral anti-hyperglycemic agents and insulin."	( Vildagliptin, a dipeptidyl peptidase-4 inhibitor, for the treatment of type 2 diabetes. Davis, SN; Lamos, EM; Stein, SA, 2014)
" The developed methods were satisfactorily applied to analysis of the investigated drugs and proved to be specific and accurate for quality control of them in pharmaceutical dosage forms."	( Validation of different spectrophotometric methods for determination of vildagliptin and metformin in binary mixture. Abdel-Aziz, O; Abdel-Ghany, MF; Ayad, MF; Tadros, MM, 2014)
"A stability-indicating capillary zone electrophoresis (CZE) method was validated for the determination of vildagliptin (VLG) in pharmaceutical dosage forms using ranitidine hydrochloride (RH) as internal standard."	( Capillary zone electrophoresis for determination of vildagliptin (a DPP-4 inhibitor) in pharmaceutical formulation and comparative study with HPLC. Barden, AT; Piccoli, BL; Schapoval, EE; Steppe, M; Volpato, NM, 2014)
" This is the first report on the tissue pharmacokinetics of a DPP-4 inhibitor and could contribute to drug dosage optimization in the future."	( Validation of LC-MS/MS method applied to evaluation of free tissue concentrations of vildagliptin in diabetic rats by microdialysis. Costa, TD; de Andrade, C; de Araújo Lock, G; de Araújo, BV; Haas, SE; Pigatto, MC, 2014)
"Simple, selective and reproducible spectrofluorimetric and spectrophotometric methods have been developed for the determination of vildagliptin and saxagliptin in bulk and their pharmaceutical dosage forms."	( Compatible validated spectrofluorimetric and spectrophotometric methods for determination of vildagliptin and saxagliptin by factorial design experiments. Abdel-Aziz, O; Ayad, MF; Tadros, MM, 2015)
"0%) with a stable dosage of metformin plus gliclazide for more than 3 months were randomized to receive either vildagliptin 50 mg twice daily (BID, n = 37) or saxagliptin 5 mg once daily (QD, n = 36)."	( Effects of vildagliptin versus saxagliptin on daily acute glucose fluctuations in Chinese patients with T2DM inadequately controlled with a combination of metformin and sulfonylurea. Jing, W; Shunyou, D; Xiaochun, H; Xiaoyan, C; Yingyu, F; Yuyu, T, 2016)
" This prescribing could have been due to the complexity of different dosing requirements, or a lack of awareness of the need for dose adjustment of most DPP-4 inhibitors in patients with renal impairment."	( Demographic and Clinical Characteristics of Patients With Type 2 Diabetes Mellitus Initiating Dipeptidyl Peptidase 4 Inhibitors: A Retrospective Study of UK General Practice. Bingham-Gardiner, P; Bolodeoku, J; Hassan, SW; Lee, S; Scowcroft, A; Spencer, W; Tebboth, A, 2016)
" On the basis of the relationship shown, changes in clinical efficacy in association with dose change were examined in order to discuss clinical dosage from the standpoint of proper usage."	( Evaluation of drug efficacy of DPP-4 inhibitors based on theoretical analysis with pharmacokinetics and pharmacodynamics. Kimura, K; Takayanagi, R; Uchida, T; Yamada, Y, 2017)
" The high-fat (HF) diet-induced obese insulin-resistant rats were divided into 4 groups and received the following treatments for 28 days: vehicle (HFV); vildagliptin at a dosage of 3 mg/kg/day (HFVil); dapagliflozin at a dosage of 1 mg/kg/day (HFDa) and combination drugs (HFDaVil)."	( Cardioprotection of dapagliflozin and vildagliptin in rats with cardiac ischemia-reperfusion injury. Chattipakorn, N; Chattipakorn, SC; Sa-Nguanmoo, P; Siri-Angkul, N; Sivasinprasasn, S; Tanajak, P; Thummasorn, S, 2018)
"0%, change in body weight at 12 and 24 weeks, change in HbA1c by sub-groups (baseline HbA1c, age, body mass index [BMI], dosage strength, co-morbidities) from baseline to week 24, and safety."	( Initial combination therapy with vildagliptin plus metformin in drug-naïve patients with T2DM: a 24-week real-life study from Asia. Chawla, M; Cooke, K; Faruque, P; Hours-Zesiger, P; Kim, TH; Mirasol, RC; Shete, A, 2018)
" The formulated nanospheres attained size uniformity and better therapeutic outcomes in terms of reduced adverse events and better control of glycemic levels than previously reported methods with decreased dosage frequency tested in Db/Db mice."	( Design, synthesis and evaluation of DNA nano-cubes as a core material protected by the alginate coating for oral administration of anti-diabetic drug. Abbas, M; Ansari, MT; Baig, MMFA; Hasnat, M; Kassim, SA; Khan, GJ; Naveed, M; Shah, K; Sohail, M; Ullah, S, 2019)
" Secondary endpoints included mean change in body weight, insulin dosage and safety after 12 weeks."	( Effectiveness, safety, and tolerability of vildagliptin or vildagliptin/metformin combination in patients with type 2 diabetes uncontrolled on insulin therapy in a real-world setting in Egypt: The OMEGA study. El Ebrashy, I; El Kafrawy, N; Raouf, R; Yousry, D, 2020)
" Blood samples were collected up to 36 hours after dosing in each period with a 7-day washout."	( Pharmacokinetics and Bioequivalence of a Generic Fixed-Dose Combination Tablet of Metformin Hydrochloride/Vildagliptin Versus a Branded Product in Healthy Chinese Subjects Under Fed and Fasting Conditions. Cai, S; Chen, S; Gao, Y; Li, B; Ling, N; Tao, X; Wang, F; Wang, Y; Ye, L, 2022)
"We aimed to investigate the effect of dosage reduction of four hypoglycemic multidrug regimens on the incidences of acute glycemic complications in people with type 2 diabetes who fast during Ramaḍān."	( Effect of Dosage Reduction of Hypoglycemic Multidrug Regimens on the Incidences of Acute Glycemic Complications in People With Type 2 Diabetes Who Fast During Ramaḍān: A Randomized Controlled Trial. Amarin, JZ; Beirat, AF; Hasan, YY; Hassoun Al Najar, AM; Qtaishat, A; Tierney, ME; Zaghlol, LY; Zaghlol, RY; Zayed, AA, 2021)
" Application of the method for assay of drugs in their combined pharmaceutical dosage forms."	( Chemometric-Based AQbD and Green Chemistry Approaches to Chromatographic Analysis of Remogliflozin Etabonate and Vildagliptin. Ahir, H; Prajapati, B; Prajapati, P; Shah, S, 2022)

Class	Description
amino acid amide	An amide of an amino acid formed formally by conversion of the carboxy group to a carboxamido 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)
Dipeptidyl peptidase 9	Bos taurus (cattle)	IC50 (µMol)	0.6800	0.6800	0.6800	0.6800	AID1501063
ATP-binding cassette sub-family C member 3	Homo sapiens (human)	IC50 (µMol)	133.0000	0.6315	4.4531	9.3000	AID1473740
Multidrug resistance-associated protein 4	Homo sapiens (human)	IC50 (µMol)	133.0000	0.2000	5.6774	10.0000	AID1473741
Dipeptidyl peptidase IV	Porphyromonas gingivalis	IC50 (µMol)	1.3000	1.3000	1.3000	1.3000	AID1501058
Dipeptidyl peptidase IV	Porphyromonas gingivalis	Ki	0.0170	0.0170	0.0170	0.0170	AID1501065
Kynurenine 3-monooxygenase	Rattus norvegicus (Norway rat)	IC50 (µMol)	52.0000	0.0220	1.3749	8.0000	AID659183
Bile salt export pump	Homo sapiens (human)	IC50 (µMol)	133.0000	0.1100	7.1903	10.0000	AID1473738
Heat shock protein HSP 90-beta	Homo sapiens (human)	IC50 (µMol)	14.2190	0.0010	0.6836	10.0000	AID258960
Dipeptidyl peptidase 4	Rattus norvegicus (Norway rat)	IC50 (µMol)	14.2190	0.0023	1.2155	5.0000	AID258960
Dipeptidyl peptidase 4	Homo sapiens (human)	IC50 (µMol)	8.5618	0.0001	0.4444	10.0000	AID1057361; AID1069459; AID1127772; AID1161870; AID1501061; AID1631905; AID1662183; AID1796783; AID1796864; AID1796870; AID1896135; AID1917944; AID240687; AID240861; AID241330; AID258959; AID343974; AID393561; AID393688; AID419062; AID427677; AID429379; AID429380; AID484489; AID484498; AID484499; AID484836; AID509568; AID56215; AID611365; AID659183; AID685045; AID749996; AID767523
Dipeptidyl peptidase 4	Homo sapiens (human)	Ki	3.6836	0.0000	0.3414	2.2000	AID1796928; AID273290; AID343974
Dipeptidyl peptidase 4	Mus musculus (house mouse)	IC50 (µMol)	0.0510	0.0460	0.0500	0.0530	AID258959
Prolyl endopeptidase	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0011	1.9896	9.7500	AID659184
Prolyl endopeptidase FAP	Mus musculus (house mouse)	IC50 (µMol)	52.0000	0.0660	0.1884	0.3700	AID659183
Prolyl endopeptidase FAP	Homo sapiens (human)	IC50 (µMol)	36.1225	0.0120	1.1589	5.8300	AID1057357; AID1161874; AID1663821; AID1796864; AID1896134; AID393564; AID484493; AID509564
Dipeptidyl peptidase 8	Homo sapiens (human)	IC50 (µMol)	15.7617	0.0019	2.6532	10.0000	AID1057359; AID1161872; AID1501062; AID1570156; AID1614274; AID1781442; AID1796783; AID1796864; AID1796870; AID240546; AID241294; AID258960; AID343972; AID393562; AID419063; AID484490; AID484837; AID509565; AID611363; AID767526
Dipeptidyl peptidase 8	Homo sapiens (human)	Ki	0.7132	0.0015	0.4624	1.3420	AID1796928; AID273291; AID688693
Dipeptidyl peptidase 9	Homo sapiens (human)	IC50 (µMol)	0.4224	0.0001	1.4207	10.0000	AID1057358; AID1161873; AID1570157; AID1614275; AID1781440; AID343973; AID484491; AID484838; AID509566; AID611364; AID767525
Dipeptidyl peptidase 9	Homo sapiens (human)	Ki	0.3154	0.0005	0.2062	1.3420	AID1796928; AID273292; AID688690
Canalicular multispecific organic anion transporter 1	Homo sapiens (human)	IC50 (µMol)	133.0000	2.4100	6.3433	10.0000	AID1473739
Dipeptidyl peptidase 2	Homo sapiens (human)	IC50 (µMol)	197.7124	0.0002	0.9316	6.6000	AID1161871; AID1501064; AID163294; AID1796783; AID1796864; AID1796870; AID241293; AID241356; AID258961; AID343975; AID393563; AID419064; AID484492; AID509567; AID611366; AID688688; AID767524
[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	0.0066	0.0000	0.0080	0.0285	AID1631907; AID1631913
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
xenobiotic metabolic process	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
bile acid and bile salt transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
leukotriene transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
monoatomic anion transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transport across blood-brain barrier	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
prostaglandin secretion	Multidrug resistance-associated protein 4	Homo sapiens (human)
cilium assembly	Multidrug resistance-associated protein 4	Homo sapiens (human)
platelet degranulation	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic metabolic process	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
bile acid and bile salt transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
prostaglandin transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
urate transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
glutathione transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
cAMP transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
leukotriene transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
monoatomic anion transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
export across plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
transport across blood-brain barrier	Multidrug resistance-associated protein 4	Homo sapiens (human)
guanine nucleotide transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
fatty acid metabolic process	Bile salt export pump	Homo sapiens (human)
bile acid biosynthetic process	Bile salt export pump	Homo sapiens (human)
xenobiotic metabolic process	Bile salt export pump	Homo sapiens (human)
xenobiotic transmembrane transport	Bile salt export pump	Homo sapiens (human)
response to oxidative stress	Bile salt export pump	Homo sapiens (human)
bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
response to organic cyclic compound	Bile salt export pump	Homo sapiens (human)
bile acid and bile salt transport	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transport	Bile salt export pump	Homo sapiens (human)
protein ubiquitination	Bile salt export pump	Homo sapiens (human)
regulation of fatty acid beta-oxidation	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transport	Bile salt export pump	Homo sapiens (human)
bile acid signaling pathway	Bile salt export pump	Homo sapiens (human)
cholesterol homeostasis	Bile salt export pump	Homo sapiens (human)
response to estrogen	Bile salt export pump	Homo sapiens (human)
response to ethanol	Bile salt export pump	Homo sapiens (human)
xenobiotic export from cell	Bile salt export pump	Homo sapiens (human)
lipid homeostasis	Bile salt export pump	Homo sapiens (human)
phospholipid homeostasis	Bile salt export pump	Homo sapiens (human)
positive regulation of bile acid secretion	Bile salt export pump	Homo sapiens (human)
regulation of bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
transmembrane transport	Bile salt export pump	Homo sapiens (human)
telomere maintenance via telomerase	Heat shock protein HSP 90-beta	Homo sapiens (human)
placenta development	Heat shock protein HSP 90-beta	Homo sapiens (human)
response to unfolded protein	Heat shock protein HSP 90-beta	Homo sapiens (human)
virion attachment to host cell	Heat shock protein HSP 90-beta	Homo sapiens (human)
positive regulation of transforming growth factor beta receptor signaling pathway	Heat shock protein HSP 90-beta	Homo sapiens (human)
regulation of protein ubiquitination	Heat shock protein HSP 90-beta	Homo sapiens (human)
negative regulation of proteasomal ubiquitin-dependent protein catabolic process	Heat shock protein HSP 90-beta	Homo sapiens (human)
positive regulation of phosphoprotein phosphatase activity	Heat shock protein HSP 90-beta	Homo sapiens (human)
regulation of protein localization	Heat shock protein HSP 90-beta	Homo sapiens (human)
negative regulation of apoptotic process	Heat shock protein HSP 90-beta	Homo sapiens (human)
positive regulation of nitric oxide biosynthetic process	Heat shock protein HSP 90-beta	Homo sapiens (human)
positive regulation of cell differentiation	Heat shock protein HSP 90-beta	Homo sapiens (human)
chaperone-mediated protein complex assembly	Heat shock protein HSP 90-beta	Homo sapiens (human)
regulation of cell cycle	Heat shock protein HSP 90-beta	Homo sapiens (human)
chaperone-mediated protein folding	Heat shock protein HSP 90-beta	Homo sapiens (human)
cellular response to interleukin-4	Heat shock protein HSP 90-beta	Homo sapiens (human)
supramolecular fiber organization	Heat shock protein HSP 90-beta	Homo sapiens (human)
negative regulation of proteasomal protein catabolic process	Heat shock protein HSP 90-beta	Homo sapiens (human)
telomerase holoenzyme complex assembly	Heat shock protein HSP 90-beta	Homo sapiens (human)
positive regulation of protein localization to cell surface	Heat shock protein HSP 90-beta	Homo sapiens (human)
cellular response to heat	Heat shock protein HSP 90-beta	Homo sapiens (human)
protein folding	Heat shock protein HSP 90-beta	Homo sapiens (human)
protein stabilization	Heat shock protein HSP 90-beta	Homo sapiens (human)
behavioral fear response	Dipeptidyl peptidase 4	Homo sapiens (human)
response to hypoxia	Dipeptidyl peptidase 4	Homo sapiens (human)
proteolysis	Dipeptidyl peptidase 4	Homo sapiens (human)
cell adhesion	Dipeptidyl peptidase 4	Homo sapiens (human)
positive regulation of cell population proliferation	Dipeptidyl peptidase 4	Homo sapiens (human)
negative regulation of extracellular matrix disassembly	Dipeptidyl peptidase 4	Homo sapiens (human)
peptide hormone processing	Dipeptidyl peptidase 4	Homo sapiens (human)
receptor-mediated endocytosis of virus by host cell	Dipeptidyl peptidase 4	Homo sapiens (human)
T cell costimulation	Dipeptidyl peptidase 4	Homo sapiens (human)
regulation of cell-cell adhesion mediated by integrin	Dipeptidyl peptidase 4	Homo sapiens (human)
locomotory exploration behavior	Dipeptidyl peptidase 4	Homo sapiens (human)
psychomotor behavior	Dipeptidyl peptidase 4	Homo sapiens (human)
T cell activation	Dipeptidyl peptidase 4	Homo sapiens (human)
endothelial cell migration	Dipeptidyl peptidase 4	Homo sapiens (human)
symbiont entry into host cell	Dipeptidyl peptidase 4	Homo sapiens (human)
receptor-mediated virion attachment to host cell	Dipeptidyl peptidase 4	Homo sapiens (human)
negative chemotaxis	Dipeptidyl peptidase 4	Homo sapiens (human)
membrane fusion	Dipeptidyl peptidase 4	Homo sapiens (human)
negative regulation of neutrophil chemotaxis	Dipeptidyl peptidase 4	Homo sapiens (human)
glucagon processing	Dipeptidyl peptidase 4	Homo sapiens (human)
proteolysis	Prolyl endopeptidase	Homo sapiens (human)
angiogenesis	Prolyl endopeptidase FAP	Homo sapiens (human)
proteolysis	Prolyl endopeptidase FAP	Homo sapiens (human)
cell adhesion	Prolyl endopeptidase FAP	Homo sapiens (human)
regulation of collagen catabolic process	Prolyl endopeptidase FAP	Homo sapiens (human)
negative regulation of extracellular matrix disassembly	Prolyl endopeptidase FAP	Homo sapiens (human)
endothelial cell migration	Prolyl endopeptidase FAP	Homo sapiens (human)
proteolysis involved in protein catabolic process	Prolyl endopeptidase FAP	Homo sapiens (human)
regulation of cell cycle	Prolyl endopeptidase FAP	Homo sapiens (human)
regulation of fibrinolysis	Prolyl endopeptidase FAP	Homo sapiens (human)
negative regulation of cell proliferation involved in contact inhibition	Prolyl endopeptidase FAP	Homo sapiens (human)
melanocyte proliferation	Prolyl endopeptidase FAP	Homo sapiens (human)
positive regulation of execution phase of apoptosis	Prolyl endopeptidase FAP	Homo sapiens (human)
melanocyte apoptotic process	Prolyl endopeptidase FAP	Homo sapiens (human)
negative regulation of extracellular matrix organization	Prolyl endopeptidase FAP	Homo sapiens (human)
proteolysis	Dipeptidyl peptidase 8	Homo sapiens (human)
apoptotic process	Dipeptidyl peptidase 8	Homo sapiens (human)
immune response	Dipeptidyl peptidase 8	Homo sapiens (human)
negative regulation of programmed cell death	Dipeptidyl peptidase 8	Homo sapiens (human)
pyroptosis	Dipeptidyl peptidase 9	Homo sapiens (human)
negative regulation of programmed cell death	Dipeptidyl peptidase 9	Homo sapiens (human)
proteolysis	Dipeptidyl peptidase 9	Homo sapiens (human)
xenobiotic metabolic process	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
negative regulation of gene expression	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bile acid and bile salt transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bilirubin transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
heme catabolic process	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic export from cell	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transepithelial transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
leukotriene transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
monoatomic anion transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transport across blood-brain barrier	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
proteolysis	Dipeptidyl peptidase 2	Homo sapiens (human)
lysosomal protein catabolic process	Dipeptidyl peptidase 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
serine-type peptidase activity	Dipeptidyl peptidase 9	Bos taurus (cattle)
ATP binding	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type xenobiotic transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type bile acid transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATP hydrolysis activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
icosanoid transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
guanine nucleotide transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
protein binding	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATP binding	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
urate transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
purine nucleotide transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type bile acid transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
efflux transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATP hydrolysis activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
glutathione transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
protein binding	Bile salt export pump	Homo sapiens (human)
ATP binding	Bile salt export pump	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Bile salt export pump	Homo sapiens (human)
bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
ABC-type bile acid transporter activity	Bile salt export pump	Homo sapiens (human)
ATP hydrolysis activity	Bile salt export pump	Homo sapiens (human)
RNA binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
double-stranded RNA binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
protein binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
ATP binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
ATP hydrolysis activity	Heat shock protein HSP 90-beta	Homo sapiens (human)
protein kinase regulator activity	Heat shock protein HSP 90-beta	Homo sapiens (human)
kinase binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
protein kinase binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
MHC class II protein complex binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
nitric-oxide synthase regulator activity	Heat shock protein HSP 90-beta	Homo sapiens (human)
TPR domain binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
heat shock protein binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
ubiquitin protein ligase binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
peptide binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
identical protein binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
protein homodimerization activity	Heat shock protein HSP 90-beta	Homo sapiens (human)
histone deacetylase binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
ATP-dependent protein binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
protein folding chaperone	Heat shock protein HSP 90-beta	Homo sapiens (human)
cadherin binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
protein dimerization activity	Heat shock protein HSP 90-beta	Homo sapiens (human)
tau protein binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
DNA polymerase binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
disordered domain specific binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
ATP-dependent protein folding chaperone	Heat shock protein HSP 90-beta	Homo sapiens (human)
receptor ligand inhibitor activity	Heat shock protein HSP 90-beta	Homo sapiens (human)
histone methyltransferase binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
unfolded protein binding	Heat shock protein HSP 90-beta	Homo sapiens (human)
virus receptor activity	Dipeptidyl peptidase 4	Homo sapiens (human)
protease binding	Dipeptidyl peptidase 4	Homo sapiens (human)
aminopeptidase activity	Dipeptidyl peptidase 4	Homo sapiens (human)
serine-type endopeptidase activity	Dipeptidyl peptidase 4	Homo sapiens (human)
signaling receptor binding	Dipeptidyl peptidase 4	Homo sapiens (human)
protein binding	Dipeptidyl peptidase 4	Homo sapiens (human)
serine-type peptidase activity	Dipeptidyl peptidase 4	Homo sapiens (human)
dipeptidyl-peptidase activity	Dipeptidyl peptidase 4	Homo sapiens (human)
identical protein binding	Dipeptidyl peptidase 4	Homo sapiens (human)
protein homodimerization activity	Dipeptidyl peptidase 4	Homo sapiens (human)
chemorepellent activity	Dipeptidyl peptidase 4	Homo sapiens (human)
serine-type endopeptidase activity	Prolyl endopeptidase	Homo sapiens (human)
protein binding	Prolyl endopeptidase	Homo sapiens (human)
serine-type peptidase activity	Prolyl endopeptidase	Homo sapiens (human)
oligopeptidase activity	Prolyl endopeptidase	Homo sapiens (human)
protease binding	Prolyl endopeptidase FAP	Homo sapiens (human)
endopeptidase activity	Prolyl endopeptidase FAP	Homo sapiens (human)
serine-type endopeptidase activity	Prolyl endopeptidase FAP	Homo sapiens (human)
integrin binding	Prolyl endopeptidase FAP	Homo sapiens (human)
protein binding	Prolyl endopeptidase FAP	Homo sapiens (human)
peptidase activity	Prolyl endopeptidase FAP	Homo sapiens (human)
serine-type peptidase activity	Prolyl endopeptidase FAP	Homo sapiens (human)
dipeptidyl-peptidase activity	Prolyl endopeptidase FAP	Homo sapiens (human)
identical protein binding	Prolyl endopeptidase FAP	Homo sapiens (human)
protein homodimerization activity	Prolyl endopeptidase FAP	Homo sapiens (human)
aminopeptidase activity	Dipeptidyl peptidase 8	Homo sapiens (human)
protein binding	Dipeptidyl peptidase 8	Homo sapiens (human)
serine-type peptidase activity	Dipeptidyl peptidase 8	Homo sapiens (human)
dipeptidyl-peptidase activity	Dipeptidyl peptidase 8	Homo sapiens (human)
aminopeptidase activity	Dipeptidyl peptidase 9	Homo sapiens (human)
protein binding	Dipeptidyl peptidase 9	Homo sapiens (human)
serine-type peptidase activity	Dipeptidyl peptidase 9	Homo sapiens (human)
dipeptidyl-peptidase activity	Dipeptidyl peptidase 9	Homo sapiens (human)
identical protein binding	Dipeptidyl peptidase 9	Homo sapiens (human)
protein binding	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATP binding	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
organic anion transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bilirubin transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATP hydrolysis activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
aminopeptidase activity	Dipeptidyl peptidase 2	Homo sapiens (human)
serine-type peptidase activity	Dipeptidyl peptidase 2	Homo sapiens (human)
serine-type exopeptidase activity	Dipeptidyl peptidase 2	Homo sapiens (human)
dipeptidyl-peptidase activity	Dipeptidyl peptidase 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Dipeptidyl peptidase 9	Bos taurus (cattle)
plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basal plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basolateral plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
nucleolus	Multidrug resistance-associated protein 4	Homo sapiens (human)
Golgi apparatus	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
basolateral plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
apical plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
platelet dense granule membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
external side of apical plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
basolateral plasma membrane	Bile salt export pump	Homo sapiens (human)
Golgi membrane	Bile salt export pump	Homo sapiens (human)
endosome	Bile salt export pump	Homo sapiens (human)
plasma membrane	Bile salt export pump	Homo sapiens (human)
cell surface	Bile salt export pump	Homo sapiens (human)
apical plasma membrane	Bile salt export pump	Homo sapiens (human)
intercellular canaliculus	Bile salt export pump	Homo sapiens (human)
intracellular canaliculus	Bile salt export pump	Homo sapiens (human)
recycling endosome	Bile salt export pump	Homo sapiens (human)
recycling endosome membrane	Bile salt export pump	Homo sapiens (human)
extracellular exosome	Bile salt export pump	Homo sapiens (human)
membrane	Bile salt export pump	Homo sapiens (human)
COP9 signalosome	Heat shock protein HSP 90-beta	Homo sapiens (human)
protein folding chaperone complex	Heat shock protein HSP 90-beta	Homo sapiens (human)
extracellular region	Heat shock protein HSP 90-beta	Homo sapiens (human)
nucleus	Heat shock protein HSP 90-beta	Homo sapiens (human)
nucleoplasm	Heat shock protein HSP 90-beta	Homo sapiens (human)
cytoplasm	Heat shock protein HSP 90-beta	Homo sapiens (human)
mitochondrion	Heat shock protein HSP 90-beta	Homo sapiens (human)
cytosol	Heat shock protein HSP 90-beta	Homo sapiens (human)
cell surface	Heat shock protein HSP 90-beta	Homo sapiens (human)
membrane	Heat shock protein HSP 90-beta	Homo sapiens (human)
secretory granule lumen	Heat shock protein HSP 90-beta	Homo sapiens (human)
melanosome	Heat shock protein HSP 90-beta	Homo sapiens (human)
neuronal cell body	Heat shock protein HSP 90-beta	Homo sapiens (human)
dendritic growth cone	Heat shock protein HSP 90-beta	Homo sapiens (human)
axonal growth cone	Heat shock protein HSP 90-beta	Homo sapiens (human)
perinuclear region of cytoplasm	Heat shock protein HSP 90-beta	Homo sapiens (human)
extracellular exosome	Heat shock protein HSP 90-beta	Homo sapiens (human)
dynein axonemal particle	Heat shock protein HSP 90-beta	Homo sapiens (human)
ficolin-1-rich granule lumen	Heat shock protein HSP 90-beta	Homo sapiens (human)
protein-containing complex	Heat shock protein HSP 90-beta	Homo sapiens (human)
aryl hydrocarbon receptor complex	Heat shock protein HSP 90-beta	Homo sapiens (human)
HSP90-CDC37 chaperone complex	Heat shock protein HSP 90-beta	Homo sapiens (human)
perinuclear region of cytoplasm	Heat shock protein HSP 90-beta	Homo sapiens (human)
plasma membrane	Heat shock protein HSP 90-beta	Homo sapiens (human)
cytosol	Heat shock protein HSP 90-beta	Homo sapiens (human)
extracellular region	Dipeptidyl peptidase 4	Homo sapiens (human)
lysosomal membrane	Dipeptidyl peptidase 4	Homo sapiens (human)
plasma membrane	Dipeptidyl peptidase 4	Homo sapiens (human)
focal adhesion	Dipeptidyl peptidase 4	Homo sapiens (human)
cell surface	Dipeptidyl peptidase 4	Homo sapiens (human)
membrane	Dipeptidyl peptidase 4	Homo sapiens (human)
apical plasma membrane	Dipeptidyl peptidase 4	Homo sapiens (human)
lamellipodium	Dipeptidyl peptidase 4	Homo sapiens (human)
endocytic vesicle	Dipeptidyl peptidase 4	Homo sapiens (human)
lamellipodium membrane	Dipeptidyl peptidase 4	Homo sapiens (human)
membrane raft	Dipeptidyl peptidase 4	Homo sapiens (human)
intercellular canaliculus	Dipeptidyl peptidase 4	Homo sapiens (human)
extracellular exosome	Dipeptidyl peptidase 4	Homo sapiens (human)
plasma membrane	Dipeptidyl peptidase 4	Homo sapiens (human)
nucleus	Prolyl endopeptidase	Homo sapiens (human)
cytoplasm	Prolyl endopeptidase	Homo sapiens (human)
cytosol	Prolyl endopeptidase	Homo sapiens (human)
membrane	Prolyl endopeptidase	Homo sapiens (human)
cytosol	Prolyl endopeptidase	Homo sapiens (human)
extracellular space	Prolyl endopeptidase FAP	Homo sapiens (human)
cytoplasm	Prolyl endopeptidase FAP	Homo sapiens (human)
plasma membrane	Prolyl endopeptidase FAP	Homo sapiens (human)
focal adhesion	Prolyl endopeptidase FAP	Homo sapiens (human)
cell surface	Prolyl endopeptidase FAP	Homo sapiens (human)
membrane	Prolyl endopeptidase FAP	Homo sapiens (human)
lamellipodium	Prolyl endopeptidase FAP	Homo sapiens (human)
lamellipodium membrane	Prolyl endopeptidase FAP	Homo sapiens (human)
ruffle membrane	Prolyl endopeptidase FAP	Homo sapiens (human)
apical part of cell	Prolyl endopeptidase FAP	Homo sapiens (human)
basal part of cell	Prolyl endopeptidase FAP	Homo sapiens (human)
peptidase complex	Prolyl endopeptidase FAP	Homo sapiens (human)
plasma membrane	Prolyl endopeptidase FAP	Homo sapiens (human)
cytoplasm	Dipeptidyl peptidase 8	Homo sapiens (human)
cytoplasm	Dipeptidyl peptidase 8	Homo sapiens (human)
cytosol	Dipeptidyl peptidase 8	Homo sapiens (human)
cytosol	Dipeptidyl peptidase 9	Homo sapiens (human)
nucleus	Dipeptidyl peptidase 9	Homo sapiens (human)
cytosol	Dipeptidyl peptidase 9	Homo sapiens (human)
microtubule	Dipeptidyl peptidase 9	Homo sapiens (human)
cell leading edge	Dipeptidyl peptidase 9	Homo sapiens (human)
plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
cell surface	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apical plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
intercellular canaliculus	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apical plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
extracellular region	Dipeptidyl peptidase 2	Homo sapiens (human)
Golgi apparatus	Dipeptidyl peptidase 2	Homo sapiens (human)
azurophil granule lumen	Dipeptidyl peptidase 2	Homo sapiens (human)
intracellular membrane-bounded organelle	Dipeptidyl peptidase 2	Homo sapiens (human)
extracellular exosome	Dipeptidyl peptidase 2	Homo sapiens (human)
vesicle	Dipeptidyl peptidase 2	Homo sapiens (human)
vesicle	Dipeptidyl peptidase 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (217)

Assay ID	Title	Year	Journal	Article
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1896134	Inhibition of FAP (unknown origin)	2022	European journal of medicinal chemistry, Oct-05, Volume: 240	Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications.
AID1057337	Antidiabetic activity in KKAy mouse assessed as reduction in glucose excursion at 10 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured after 30 mins by oral glucose tolerance test (Rvb = 22.74 +/- 2.62 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID685045	Inhibition of human DPP4 expressed in baculovirus expression system using Gly-Pro-AMC substrate incubated or 30 mins by fluorescence based assay	2012	Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10	Long-acting peptidomimetics based DPP-IV inhibitors.
AID1662183	Inhibition of DPP4 (unknown origin)	2020	Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5	Anti-diabetic drugs recent approaches and advancements.
AID1057360	Inhibition of 6xHis-tagged recombinant DPP7 (unknown origin) expressed in baculovirus expression system assessed as hydrolysis of Nle-Pro-aminomethylcoumarin after 20 mins by fluorometric assay	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1057320	Antidiabetic activity in ICR mouse assessed as reduction in glucose excursion at 10 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured after 120 mins by oral glucose tolerance test (Rvb = 8.04 +/- 0.79 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1057329	Antidiabetic activity in ICR mouse assessed as reduction in glucose excursion at 3 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured after 30 mins by oral glucose tolerance test (Rvb = 13.42 +/- 1.12 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1057350	Antidiabetic activity in ICR mouse assessed as reduction in glucose excursion at 10 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured immediately by oral glucose tolerance test (Rvb = 6.84 +/- 1.12 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID429380	Inhibition of DPP4	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.
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.
AID509568	Inhibition of human recombinant His-tagged DPP4 expressed in insect cells	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18	Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.
AID1161884	Increase in basal plasma insulin content in C57BKS db/db mouse at 15 mg/kg/day, po relative to control	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID484489	Inhibition of DPP4	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
AID240546	Inhibitory concentration against Dipeptidylpeptidase 8	2005	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13	Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.
AID709521	Antihyperglycemic activity in Wistar rat assessed as glucose excursion curve at 10 mg/kg, po by glucose tolerance test	2012	Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24	Discovery of 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines as orally available G protein-coupled receptor 119 agonists.
AID1487390	Inhibition of membrane-bound DPP-4 (unknown origin) assessed as dissociation rate constant	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID611364	Inhibition of DPP9	2011	Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16	Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?
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.
AID1161873	Inhibition of DPP9 (unknown origin) expressed in baculovirus expression system using Ala-Pro-AMC as substrate by continuous fluorometric assay	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID611365	Inhibition of DPP4	2011	Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16	Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?
AID1519405	Anti-glycation activity assessed as inhibition of AGE formation by measuring decrease in glycated BSA protein level at 1000 uM incubated for 24 hrs in presence of glucose by fluorescence based assay relative to control
AID56215	Inhibitory activity against dipeptidylpeptidase IV.	2004	Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1	4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.
AID484836	Inhibition of DPP4	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
AID1487349	Inhibition of human seminal fluid DPP-4 expressed in Sf9 cell membranes assessed as residence time using Gly-Pro-AMC as substrate preincubated for 60 mins followed by substrate addition measured up to 40 mins by spectrophotometric method	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID1161881	Reduction in fasting blood glucose level in C57BKS db/db mouse at 15 mg/kg/day, po (Rvb =23.0 +/- 1.0 mM)	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID1501062	Inhibition of DPP8 (unknown origin)	2017	European journal of medicinal chemistry, Oct-20, Volume: 139	Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.
AID241294	Inhibitory concentration against dipeptidylpeptidase 8	2005	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3	Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.
AID343973	Inhibition of DPP9	2008	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14	Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.
AID1057361	Inhibition of 6xHis-tagged recombinant human DPP4 expressed in baculovirus expression system assessed as hydrolysis of Ala-Pro-aminomethylcoumarin by fluorometric assay	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID393564	Inhibition of human FAP	2009	Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6	Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors.
AID1487389	Inhibition of membrane-bound DPP-4 (unknown origin) assessed as association rate constant	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID688684	Selectivity ratio of Ki for DPP9 to Ki 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.
AID1519406	Anti-glycation activity assessed as inhibition of AGE formation by measuring decrease in glycated BSA protein level at 100 uM incubated for 24 hrs in presence of glucose by fluorescence based assay relative to control
AID1057335	Antidiabetic activity in KKAy mouse assessed as reduction in glucose excursion at 10 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured after 60 mins by oral glucose tolerance test (Rvb = 19.64 +/- 2.35 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1057322	Antidiabetic activity in ICR mouse assessed as reduction in glucose excursion at 1 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured after 120 mins by oral glucose tolerance test (Rvb = 8.04 +/- 0.79 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
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.
AID419498	Volume of distribution at steady state in human	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	In silico prediction of volume of distribution in human using linear and nonlinear models on a 669 compound data set.
AID1896135	Inhibition of DPP4 (unknown origin)	2022	European journal of medicinal chemistry, Oct-05, Volume: 240	Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications.
AID484494	Ex vivo inhibition of DPP4 in rat plasma at 3 mg/kg, po after 30 mins	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
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.
AID1161876	Selectivity ratio of IC50 for DPP9 (unknown origin) expressed in baculovirus expression system to IC50 for human recombinant DPP4 expressed in baculovirus expression system	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID1076230	Antidiabetic activity in C57BKS db/db mouse assessed as blood glucose level at 15 mg/kg/day administered for 5 weeks followed by glucose challenge at 6 hrs starvation of post last dose measured immediately by OGTT (Rvb = 25 +/- 1.2 mmol/L)	2014	European journal of medicinal chemistry, Mar-21, Volume: 75	Design, synthesis and biological evaluation of hetero-aromatic moieties substituted pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID484838	Inhibition of DPP9	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
AID484496	Ex vivo inhibition of DPP4 in rat plasma at 3 mg/kg, po after 8 hrs	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
AID1161883	Reduction in free fatty acid in C57BKS db/db mouse at 15 mg/kg/day, po (Rvb = 1.46 +/- 0.10 mM)	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID1501061	Inhibition of human DPP4	2017	European journal of medicinal chemistry, Oct-20, Volume: 139	Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.
AID1161870	Inhibition of human recombinant DPP4 expressed in baculovirus expression system using Ala-Pro-AMC as substrate by continuous fluorometric assay	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
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.
AID1487347	Inhibition of human seminal fluid DPP-4 expressed in Sf9 cell membranes assessed as association rate constant using Gly-Pro-AMC as substrate preincubated for 60 mins followed by substrate addition measured up to 40 mins by spectrophotometric method	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
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.
AID767525	Inhibition of human purified His-tagged DPP-9 assessed as cleavage of substrate using Gly-Pro-AMC chromogenic substrate after 60 mins by fluorescence spectrophotometry	2013	Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18	Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors.
AID393561	Inhibition of human DPP4	2009	Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6	Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors.
AID1057348	Antidiabetic activity in ICR mouse assessed as decrease in blood glucose AUC (0 to 120 mins) at 1 mg/kg, po administered 0.5 hrs prior to glucose-challenge by oral glucose tolerance test (Rvb = 20.74 +/- 1.25 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID484492	Inhibition of DPP2	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
AID484845	Antidiabetic activity in ICR mouse assessed as reduction in glucose AUC (0 to 120) at 10 mg/kg, po pretreated 30 mins before glucose challenge measured after 120 mins by oral glucose tolerance test relative to control	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
AID659187	Inhibition of bovine testes DPP9 assessed as pNA release from Ala-Pro-p-nitroanilide substrate pre-incubated with enzyme for 15 min prior to substrate addition by fluorescence technique	2012	Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10	Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity.
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?
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.
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.
AID1057321	Antidiabetic activity in ICR mouse assessed as reduction in glucose excursion at 3 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured after 120 mins by oral glucose tolerance test (Rvb = 8.04 +/- 0.79 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1501064	Inhibition of DPP2 (unknown origin)	2017	European journal of medicinal chemistry, Oct-20, Volume: 139	Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.
AID484493	Inhibition of FAP	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
AID273292	Inhibition of DPP9	2006	Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21	Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the tr
AID1057325	Antidiabetic activity in ICR mouse assessed as reduction in glucose excursion at 3 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured after 60 mins by oral glucose tolerance test (Rvb = 11.07 +/- 1.09 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID419062	Inhibition of DPP4	2009	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7	Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors.
AID163294	Inhibitory activity against quiescent cell prolyl peptidase (QPP).	2004	Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1	4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.
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.
AID393688	Inhibition of DPP4	2009	Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5	Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes.
AID1501058	Inhibition of Porphyromonas gingivalis N-terminal His-tagged DPP4 expressed in Escherichia coli using Gly-Pro-p-nitroanilide as substrate	2017	European journal of medicinal chemistry, Oct-20, Volume: 139	Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.
AID1057356	Selectivity ratio of IC50 for recombinant DPP8 (unknown origin) to IC50 for recombinant human DPP4	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1057359	Inhibition of 6xHis-tagged recombinant DPP8 (unknown origin) expressed in baculovirus expression system assessed as hydrolysis of Ala-Pro-aminomethylcoumarin preincubated for 20 mins followed by Gly-PropNA3 Tos addition measured after 90 mins by fluoromet	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID258962	Inhibition of plasma DPP4 in BALB/c mice 30 min after administration of 18 mg/kg, po	2006	Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1	2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
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.
AID1069459	Inhibition of DPP4 (unknown origin)	2014	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3	Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV.
AID1057328	Antidiabetic activity in ICR mouse assessed as reduction in glucose excursion at 10 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured after 30 mins by oral glucose tolerance test (Rvb = 13.42 +/- 1.12 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1161878	Reduction in glucose excursion in ICR mouse assessed as glucose AUC (0 to 120 mins) at 15 mg/kg administered as single dose by oral glucose tolerance test (Rvb = 1175.5 +/- 216.4 mmol/L/min)	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID484490	Inhibition of DPP8	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
AID659184	Inhibition of human recombinant PREP expressed in Escherichia coli assessed as pNA release from Z-Gly-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique	2012	Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10	Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity.
AID509567	Inhibition of human recombinant His-tagged DPP2 expressed in insect cells	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18	Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.
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.
AID1057347	Antidiabetic activity in ICR mouse assessed as decrease in blood glucose AUC (0 to 120 mins) at 3 mg/kg, po administered 0.5 hrs prior to glucose-challenge by oral glucose tolerance test (Rvb = 20.74 +/- 1.25 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1161871	Inhibition of DPP7 (unknown origin) expressed in baculovirus expression system using Nle-Pro-AMC as substrate by continuous fluorometric assay	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID1076227	Antidiabetic activity in C57BKS db/db mouse assessed as blood glucose level at 15 mg/kg/day administered for 5 weeks followed by glucose challenge at 6 hrs starvation of post last dose measured at 60 mins by OGTT (Rvb = 30.2 +/- 1.5 mmol/L)	2014	European journal of medicinal chemistry, Mar-21, Volume: 75	Design, synthesis and biological evaluation of hetero-aromatic moieties substituted pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID1487351	Inhibition of rat DPP-4 assessed as association rate constant using Gly-Pro-AMC as substrate measured after 20 mins by fluorescence assay	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
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.
AID1594248	Antidiabetic activity in HDF/STZ-induced obese type-2 diabetes Wistar rat model assessed as reduction in blood glucose level at 10 mg/kg, ip pretreated for 30 mins followed by glucose challenge and measured up to 120 mins by OGTT	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9	Synthesis and biological evaluation of 3-substituted 2-oxindole derivatives as new glycogen synthase kinase 3β inhibitors.
AID343975	Inhibition of DPP2	2008	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14	Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.
AID1057333	Antidiabetic activity in KKAy mouse assessed as reduction in glucose excursion at 10 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured after 120 mins by oral glucose tolerance test (Rvb = 11.2 +/- 2.94 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
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.
AID659186	Inhibition of human seminal plasma DPP4 assessed as pNA release from Gly-Pro-p-nitroanilide substrate pre-incubated with enzyme for 15 min prior to substrate addition by fluorescence technique	2012	Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10	Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity.
AID688683	Selectivity ratio of Ki for DPP8 to Ki 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.
AID509565	Inhibition of human recombinant His-tagged DPP8 expressed in insect cells	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18	Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.
AID611363	Inhibition of DPP8	2011	Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16	Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?
AID273291	Inhibition of DPP8	2006	Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21	Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the tr
AID241330	Inhibitory concentration against dipeptidylpeptidase IV	2005	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3	Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.
AID1473410	Half life in human administered as single oral dose	2018	Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3	In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.
AID484498	Inhibition of DPP4 in presence of 50% human serum	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
AID767523	Inhibition of human purified His-tagged DPP-4 assessed as cleavage of substrate using Gly-Pro-AMC chromogenic substrate after 60 mins by fluorescence spectrophotometry	2013	Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18	Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors.
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.
AID1161886	Reduction in total cholesterol content in C57BKS db/db mouse at 15 mg/kg/day, po	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID393562	Inhibition of human DPP8	2009	Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6	Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors.
AID1161880	Reduction in glucose AUC (0 to 120 mins) in C57BKS db/db mouse at 15 mg/kg/day, po for 5 weeks by oral glucose tolerance test (Rvb = 3649.5 +/- 91.5mmol/L/min)	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID1057357	Inhibition of 6xHis-tagged recombinant FAP (unknown origin) expressed in baculovirus expression system assessed as hydrolysis of Nle-Pro-aminomethylcoumarin after 20 mins by fluorometric assay	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID484491	Inhibition of DPP9	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
AID343972	Inhibition of DPP8	2008	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14	Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.
AID1161872	Inhibition of DPP8 (unknown origin) expressed in baculovirus expression system using Ala-Pro-AMC as substrate by continuous fluorometric assay	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID611366	Inhibition of DPP2	2011	Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16	Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?
AID1057345	Antidiabetic activity in ICR mouse assessed as decrease in blood glucose AUC (0 to 120 mins) at 10 mg/kg, po administered 0.5 hrs prior to glucose-challenge by oral glucose tolerance test (Rvb = 20.74 +/- 1.25 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1398540	Hypoglycemic activity in albino CD-1 mouse assessed as reduction in blood glucose level at 10 mg/kg, po pretreated for 0.5 hrs followed by glucose challenge and measured after 30 to 90 mins by OGTT	2018	Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15	Synthesis and evaluation of camphor and cytisine-based cyanopyrrolidines as DPP-IV inhibitors for the treatment of type 2 diabetes mellitus.
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.
AID1501063	Inhibition of bovine DPP9	2017	European journal of medicinal chemistry, Oct-20, Volume: 139	Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.
AID767524	Inhibition of human purified His-tagged DPP-7 assessed as cleavage of substrate using Gly-Pro-AMC chromogenic substrate after 60 mins by fluorescence spectrophotometry	2013	Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18	Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors.
AID1473741	Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID509564	Inhibition of human recombinant FAP expressed in Hi5 insect cells	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18	Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.
AID1519408	Metal chelating activity assessed as inhibition of Cu2+ ion-induced oxidation of ascorbic acid compound treated with CuSO4.5H2O for 5 mins followed by ascorbate addition and measured immediately by spectrophotometric analysis
AID1487352	Inhibition of rat DPP-4 assessed as residence time using Gly-Pro-AMC as substrate measured after 20 mins by fluorescence assay	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID1631911	Inhibition of DPP4 in human CaCo2 cells assessed as dissociation rate constant using Ala-Pro-AFC as substrate preincubated for 1 hr followed by substrate addition 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.
AID1057331	Antidiabetic activity in KKAy mouse assessed as decrease in blood glucose AUC (0 to 120 mins) at 10 mg/kg, po administered 0.5 hrs prior to glucose-challenge by oral glucose tolerance test (Rvb = 34.78 +/- 3.62 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1519401	Inhibition of DPP4 in human serum assessed as decrease in p-nitroaniline formation using Gly-Pro-p-nitroanilide as substrate at 100 uM preincubated for 5 mins followed by incubation with substrate for 15 mins by microplate reader analysis relative to cont
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.
AID1487355	Inhibition of human DPP-4 assessed as residence time using H-Ala-Pro-pNA as substrate measured every 10 s for 600 s	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID1127772	Inhibition of DPP4 (unknown origin)	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?
AID419530	Clearance in human at 25 mg, iv administered 30 mins infusion	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	In silico prediction of volume of distribution in human using linear and nonlinear models on a 669 compound data set.
AID419063	Inhibition of DPP8	2009	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7	Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors.
AID1501060	Inhibition of Porphyromonas gingivalis N-terminal His-tagged DPP4 expressed in Escherichia coli using Gly-Pro-p-nitroanilide as substrate after 1 hr	2017	European journal of medicinal chemistry, Oct-20, Volume: 139	Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.
AID419070	Inhibition of plasma DPP4 in Wistar rat at 3 mg/kg, po measured after 8 hrs	2009	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7	Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors.
AID1487348	Inhibition of human seminal fluid DPP-4 expressed in Sf9 cell membranes assessed as dissociation rate constant using Gly-Pro-AMC as substrate preincubated for 60 mins followed by substrate addition measured up to 40 mins by spectrophotometric method	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID1057351	Antidiabetic activity in ICR mouse assessed as reduction in glucose excursion at 3 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured immediately by oral glucose tolerance test (Rvb = 6.84 +/- 1.12 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1161882	Reduction in plasma triglyceride content in C57BKS db/db mouse at 15 mg/kg/day, po (Rvb = 1.01 +/- 0.09 mM)	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID1473738	Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID484499	Inhibition of DPP4 in presence of 50% rat serum	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
AID1057346	Antidiabetic activity in ICR mouse assessed as reduction in glucose excursion at 1 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured after 30 mins by oral glucose tolerance test (Rvb = 13.42 +/- 1.12 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1888485	Anti-hyperglycemic activity in Wistar rat assessed as reduction in plasma glucose AUC (0 to 120 mins) at 10 mg/kg, po followed by sucrose load by oral sucrose tolerance test	2022	Bioorganic & medicinal chemistry letters, 01-01, Volume: 55	Towards multi-target antidiabetic agents: In vitro and in vivo evaluation of 3,5-disubstituted indolin-2-one derivatives as novel α-glucosidase inhibitors.
AID484856	Antidiabetic activity in KKAy mouse assessed as reduction of blood glucose AUC (0 to 120 mins) level at 10 mg/kg, po administered 30 mins before oral glucose challenge by oral glucose tolerance test	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	Synthesis and biological evaluation of bicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
AID1161874	Inhibition of FAP (unknown origin) expressed in baculovirus expression system using Nle-Pro-AMC as substrate by continuous fluorometric assay	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID427676	Selectivity index, ratio of IC50 for human recombinant DPP7 to IC50 for human recombinant DDP9	2009	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15	Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors.
AID1076225	Antidiabetic activity in C57BKS db/db mouse assessed as blood glucose level at 15 mg/kg/day administered for 5 weeks followed by glucose challenge at 6 hrs starvation of post last dose measured at 120 mins by OGTT (Rvb = 28.1 +/- 1.3 mmol/L)	2014	European journal of medicinal chemistry, Mar-21, Volume: 75	Design, synthesis and biological evaluation of hetero-aromatic moieties substituted pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID1662184	Toxicity in mouse	2020	Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5	Anti-diabetic drugs recent approaches and advancements.
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
AID1487354	Inhibition of human DPP-4 assessed as dissociation rate constant using H-Ala-Pro-pNA as substrate measured every 10 s for 600 s	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID258963	Decrease in blood glucose level in Wistar rat 2 hrs after administration of 10 mg/kg, po	2006	Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1	2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
AID1057352	Antidiabetic activity in ICR mouse assessed as reduction in glucose excursion at 1 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured immediately by oral glucose tolerance test (Rvb = 6.84 +/- 1.12 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1501056	Inhibition of Porphyromonas gingivalis N-terminal His-tagged DPP4 expressed in Escherichia coli at 10 uM using Gly-Pro-p-nitroanilide as substrate relative to control	2017	European journal of medicinal chemistry, Oct-20, Volume: 139	Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.
AID393563	Inhibition of human DPP2	2009	Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6	Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors.
AID427677	Inhibition of human recombinant DPP4 by fluorescence assay	2009	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15	Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors.
AID1161875	Selectivity ratio of IC50 for DPP8 (unknown origin) expressed in baculovirus expression system to IC50 for human recombinant DPP4 expressed in baculovirus expression system	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID659183	Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique	2012	Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10	Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity.
AID258960	Inhibitory activity against DPP8	2006	Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1	2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
AID1057326	Antidiabetic activity in ICR mouse assessed as reduction in glucose excursion at 1 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured after 60 mins by oral glucose tolerance test (Rvb = 11.07 +/- 1.09 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1473740	Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID258959	Inhibitory activity against DPP4	2006	Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1	2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
AID1519404	Ex vivo inhibition of DPP4 in Wistar rat serum assessed as decrease in p-nitroaniline formation at 10 mg/kg, po by incubating 0 to 4 hrs compound-treated serum with Gly-Pro-p-nitroanilide substrate and measured for 30 mins by microplate reader analysis
AID427679	Selectivity index, ratio of IC50 for human recombinant DPP7 to IC50 for human recombinant DDP8	2009	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15	Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors.
AID340643	Antiproliferative activity against T cells	2008	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14	Discovery of conformationally rigid 3-azabicyclo[3.1.0]hexane-derived dipeptidyl peptidase-IV inhibitors.
AID343974	Inhibition of DPP4	2008	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14	Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.
AID1057341	Antidiabetic activity in KKAy mouse assessed as reduction in glucose excursion at 10 mg/kg, po after 30 mins by oral glucose tolerance test in absence of glucose-challenge (Rvb = 9.52 +/- 2.06 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID484849	Selectivity ratio of IC50 for DPP8 to IC50 for DPP4	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
AID1057339	Antidiabetic activity in KKAy mouse assessed as reduction in glucose excursion at 10 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured immediately by oral glucose tolerance test (Rvb = 12.26 +/- 3.52 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-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.
AID1501065	Inhibition of Porphyromonas gingivalis N-terminal His-tagged DPP4 expressed in Escherichia coli using Gly-Pro-p-nitroanilide as substrate preincubated for 15 mins	2017	European journal of medicinal chemistry, Oct-20, Volume: 139	Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.
AID427678	Selectivity index, ratio of IC50 for human recombinant DPP7 to IC50 for human recombinant DDP4	2009	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15	Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors.
AID484837	Inhibition of DPP8	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
AID240687	Inhibitory concentration against Dipeptidylpeptidase IV [DPP-IV]	2005	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13	Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.
AID484844	Antidiabetic activity in ICR mouse assessed as reduction in glucose AUC (0 to 120) at 3 mg/kg, po pretreated 30 mins before glucose challenge measured after 120 mins by oral glucose tolerance test relative to control	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
AID1888486	Anti-hyperglycemic activity in Wistar rat assessed as reduction in plasma glucose AUC (0 to 120 mins) at 10 mg/kg, po followed by glucose load by oral glucose tolerance test	2022	Bioorganic & medicinal chemistry letters, 01-01, Volume: 55	Towards multi-target antidiabetic agents: In vitro and in vivo evaluation of 3,5-disubstituted indolin-2-one derivatives as novel α-glucosidase inhibitors.
AID1519407	Anti-glycation activity assessed as inhibition of AGE formation by measuring decrease in glycated BSA protein level incubated for 24 hrs in presence of glucose by fluorescence based assay
AID258961	Inhibitory activity against DPP2	2006	Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1	2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
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.
AID1487386	Inhibition of solubilized DPP-4 (unknown origin) assessed as association rate constant	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID1076228	Antidiabetic activity in C57BKS db/db mouse assessed as blood glucose level at 15 mg/kg/day administered for 5 weeks followed by glucose challenge at 6 hrs starvation of post last dose measured at 30 mins by OGTT (Rvb = 46.6 +/- 2.2 mmol/L)	2014	European journal of medicinal chemistry, Mar-21, Volume: 75	Design, synthesis and biological evaluation of hetero-aromatic moieties substituted pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
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.
AID273290	Inhibition of human DPP4 expressed in Caco-2 cells	2006	Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21	Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the tr
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.
AID1487388	Inhibition of solubilized DPP-4 (unknown origin) assessed as residence time	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID484843	Antidiabetic activity in ICR mouse assessed as reduction in glucose AUC (0 to 120) at 1 mg/kg, po pretreated 30 mins before glucose challenge measured after 120 mins by oral glucose tolerance test relative to control	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of 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.
AID1161885	Reduction in random blood glucose level in C57BKS db/db mouse at 15 mg/kg/day, po (Rvb =23.3 +/- 1.0 mM)	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID241356	Inhibitory concentration against DPP-II [Quiescent cell proline dipeptidase] or DPP-VII	2005	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13	Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.
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.
AID767526	Inhibition of human purified His-tagged DPP-8 assessed as cleavage of substrate using Gly-Pro-AMC chromogenic substrate after 60 mins by fluorescence spectrophotometry	2013	Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18	Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors.
AID1473739	Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID509566	Inhibition of human recombinant His-tagged DPP9 expressed in insect cells	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18	Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.
AID419069	Inhibition of plasma DPP4 in Wistar rat at 3 mg/kg, po measured 30 mins to 4 hrs	2009	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7	Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors.
AID419064	Inhibition of DPP2	2009	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7	Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors.
AID1487391	Inhibition of membrane-bound DPP-4 (unknown origin) assessed as residence time	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID1487353	Inhibition of human DPP-4 assessed as association rate constant using H-Ala-Pro-pNA as substrate measured every 10 s for 600 s	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID1057358	Inhibition of 6xHis-tagged recombinant DPP9 (unknown origin) expressed in baculovirus expression system assessed as hydrolysis of Ala-Pro-aminomethylcoumarin preincubated for 20 mins followed by Gly-PropNA3 Tos addition measured after 90 mins by fluoromet	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID1487350	Inhibition of rat DPP-4 assessed as dissociation rate constant using Gly-Pro-AMC as substrate measured after 20 mins by fluorescence assay	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
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.
AID419068	Reduction in glucose excursion in C57BL/6 mouse at 3 mg/kg, po measured up to 120 mins by oral glucose tolerance test	2009	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7	Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors.
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.
AID241293	Inhibitory concentration against dipeptidylpeptidase 2	2005	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3	Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.
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.
AID1896133	Inhibition of POP (unknown origin)	2022	European journal of medicinal chemistry, Oct-05, Volume: 240	Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications.
AID1076238	Antidiabetic activity in ICR mouse assessed as decrease in blood glucose AUC (0 to 120 mins) at 30 mg/kg administered for 30 mins prior to glucose challenge measured after 4 hrs by OGTT relative to vehicle-treated control	2014	European journal of medicinal chemistry, Mar-21, Volume: 75	Design, synthesis and biological evaluation of hetero-aromatic moieties substituted pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID1057355	Selectivity ratio of IC50 for recombinant DPP9 (unknown origin) to IC50 for recombinant human DPP4	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID240861	Inhibitory concentration against dipeptidylpeptidase IV	2004	Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17	Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
AID773604	Antidiabetic activity in high fat-fed Zucker diabetic fatty rat assessed as decrease in blood glucose AUC at 50 mg/kg, po qd administered 21 days measured for 2 hrs post last dose by OGTT relative to control	2013	Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19	Identification of a new class of glucokinase activators through structure-based design.
AID1057324	Antidiabetic activity in ICR mouse assessed as reduction in glucose excursion at 10 mg/kg, po administered 0.5 hrs prior to glucose-challenge measured after 60 mins by oral glucose tolerance test (Rvb = 11.07 +/- 1.09 mmol/L)	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23	Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
AID393693	Oral bioavailability in cynomolgus monkey	2009	Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5	Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes.
AID1076226	Antidiabetic activity in C57BKS db/db mouse assessed as blood glucose level at 15 mg/kg/day administered for 5 weeks followed by glucose challenge at 6 hrs starvation of post last dose measured at 90 mins by OGTT (Rvb = 27.2 +/- 1.3 mmol/L)	2014	European journal of medicinal chemistry, Mar-21, Volume: 75	Design, synthesis and biological evaluation of hetero-aromatic moieties substituted pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
AID1487387	Inhibition of solubilized DPP-4 (unknown origin) assessed as dissociation rate constant	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID659185	Inhibition of human seminal plasma DPP2 assessed as pNA release from Lys-Ala-p-nitroanilide substrate pre-incubated with enzyme for 15 min prior to substrate addition by fluorescence technique	2012	Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10	Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity.
AID419065	Inhibition of FAP	2009	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7	Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors.
AID1519402	Inhibition of DPP4 in human serum assessed as decrease in p-nitroaniline formation using Gly-Pro-p-nitroanilide as substrate preincubated for 5 mins followed by incubation with substrate for 15 mins by microplate reader analysis
AID1796864	Enzyme Inhibition Assay from Article 10.1016/j.bmcl.2006.03.037: \\Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.\\	2006	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 16, Issue:12	Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.
AID1796783	Dipeptidyl Peptidase Inhibition Assay from Article 10.1021/jm0507781: \\2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of	2006	Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1	2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
AID1796870	Enzyme Inhibition Assay from Article 10.1016/j.bmcl.2004.11.023: \\Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.\\	2005	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3	Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.
AID1796928	DPPIV Inhibition Assay from Article 10.1021/jm060777o: \\Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]-4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated	2006	Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21	Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the tr
AID1345443	Human dipeptidyl peptidase 4 (S9: Prolyl oligopeptidase)	2009	Current drug targets, Jan, Volume: 10, Issue:1	Emerging drug candidates of dipeptidyl peptidase IV (DPP IV) inhibitor class for the treatment of Type 2 Diabetes.
[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	169 (21.83)	29.6817
2010's	476 (61.50)	24.3611
2020's	129 (16.67)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	186 (23.46%)	5.53%
Reviews	136 (17.15%)	6.00%
Case Studies	34 (4.29%)	4.05%
Observational	21 (2.65%)	0.25%
Other	416 (52.46%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (170)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Study of the Effect of Vildagliptin on Glucagon Counterregulation Response During Hypoglycemia in Insulin-treated Patients With Type 2 Diabetes[NCT01219400]	Phase 4	28 participants (Actual)	Interventional	2012-01-31	Completed
A Multicenter, Prospective, Randomized, Open-label, Parallel Group Study to Investigate the Clinical Benefit on Hypoglycemia Frequency of 24 Weeks Treatment With Galvus Versus Usual Care (Any OAD of Another Class Added to Metformin Within SmPc) in Older P[NCT01238978]	Phase 4	46 participants (Actual)	Interventional	2010-10-31	Completed
Multi-center, Open-label, 24-week Study to Demonstrate the Efficacy and Safety of Combination Therapy of Vildagliptin/Metformin 50/500 or 50/1000 mg Twice Daily in Patients With T2DM Inadequately Controlled With Metformin[NCT01196546]	Phase 4	161 participants (Actual)	Interventional	2010-03-31	Completed
Glucose Control in Pre-Diabetic Renal Transplant Patients: Efficacy and Safety of Vildagliptin and Pioglitazone[NCT01346254]	Phase 2	51 participants (Actual)	Interventional	2009-12-31	Completed
A Multicenter, Double-blind, Randomized, Parallel-group Study to Compare the Effect of 24 Weeks Treatment With Vildagliptin 50mg qd to Placebo as add-on Therapy to Glimepiride in Patients With Type 2 Diabetes Inadequately Controlled With Sulfonylurea Mono[NCT01357252]	Phase 3	279 participants (Actual)	Interventional	2011-04-30	Completed
A 24-week, Multi-center, Double-blind, Randomized, Placebo-controlled, Parallel-group Study to Assess the Efficacy and Safety of Vildagliptin 50mg Bid as an add-on Therapy to Insulin, With or Without Metformin, in Patients With Type 2 Diabetes Mellitus.[NCT01224366]	Phase 3	448 participants (Actual)	Interventional	2010-09-30	Completed
Pilot Study to Assess the Difference in Glycemic Profiles Between Vildagliptin and Glimepiride Using Continuous Glucose Monitoring Device[NCT01262586]	Phase 3	24 participants (Actual)	Interventional	2010-11-30	Completed
An Open-label, Randomized and Crossover Study to Assess the Effect of Co-administration of Vildagliptin and Voglibose on the Steady-state Pharmacokinetics / Pharmacodynamics in Japanese Patients With Type 2 Diabetes[NCT01309698]	Phase 4	24 participants (Actual)	Interventional	2011-02-28	Completed
The Study About Glucose Lowering Effect of Vildagliptin in Type 2 Diabetes Patients Who Are Uncontrolled With Metformin and a Sulphonylurea[NCT01099137]	Phase 4	344 participants (Actual)	Interventional	2010-01-31	Completed
Clinical Study Evaluating the Effectiveness of Vildagliptin Versus Vildagliptin/Metformin on NAFLD With DM[NCT03925701]	Phase 3	120 participants (Anticipated)	Interventional	2019-04-01	Recruiting
Efficacy and Safety of Vildagliptin Added to Continuous Subcutaneous Insulin Infusion in Uncontrolled Type 2 Diabetes[NCT03563794]	Phase 4	400 participants (Anticipated)	Interventional	2018-06-10	Recruiting
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
An Open-label, Randomized, Active-controlled Study to Compare the Effect of DPP-IV Inhibitor and TZD as add-on Therapy to Metformin on Glycemic Variability and Oxidative Stress in Patients With Type 2 Diabetes Inadequately Controlled With Metformin Monoth[NCT01339143]	Phase 4	80 participants (Anticipated)	Interventional	2010-04-30	Recruiting
Incretin-based Drugs and the Risk of Heart Failure: A Multi-center Network Observational Study[NCT02456428]		1,499,650 participants (Actual)	Observational	2014-03-31	Completed
A Single-center,Double-blind,Randomised,Placebo-controlled,Parallel-group Study to Assess the Effect of 24 Weeks of Treatment With Vildagliptin on Insulin Sensitivity and Its Underlying Mechanism in Patients With T2DM Treated With Metformin[NCT01356381]	Phase 4	43 participants (Actual)	Interventional	2011-04-30	Completed
Effect of Vildagliptin & Metformin Combination on Glycemic Control and Hypoglycemic Episodes. An Observational Real Life Trial[NCT03577184]		0 participants (Actual)	Observational	2018-07-31	Withdrawn(stopped due to Institutions issue)
Comparison of Three DPP-4 Inhibitors on 24 Hour Blood Glucose, Incretin Hormones and Islet Function in Patients With Type 2 Diabetes[NCT02089438]	Phase 4	24 participants (Actual)	Interventional	2014-05-31	Completed
Efficacy of Vildagliptin, Liraglutide and Empagliflozin in the Management of Fatty Liver Disease Among Patients With Type 2 Diabetes[NCT05041673]		120 participants (Anticipated)	Interventional	2021-02-23	Active, not recruiting
Vildagliptin Compared to Glimepiride in Combination With Metformin in Patients With Type 2 Diabetes[NCT00106340]	Phase 3	3,118 participants (Actual)	Interventional	2005-03-31	Completed
Study of the Effect of Vildagliptin on Glucagon Counterregulation Response During Hypoglycemia in Patients With Type 1 Diabetes[NCT01147276]	Phase 4	28 participants (Actual)	Interventional	2010-09-30	Completed
Prospective, Randomized, Open-label Study With Blinded Endpoint (PROBE Design) to Compare the 72 hr Glycemic Profiles Obtained by Continuous Subcutaneous Glucose Monitoring (CSGM) in Type 2 Diabetic Patients at Baseline With Metformin Monotherapy and Afte[NCT01193296]	Phase 4	36 participants (Actual)	Interventional	2010-06-30	Completed
Role of Vitagliptin and Vitamin D in the Treatment of Non Alcoholic Fatty Liver Disease (NAFLD)[NCT01083992]		60 participants (Anticipated)	Interventional	2012-04-30	Not yet recruiting
The Use of Incretin-based Drugs and the Risk of Acute Pancreatitis in Patients With Type 2 Diabetes[NCT02476760]		1,417,914 participants (Actual)	Observational	2014-03-31	Completed
An Open-label, Parallel Group Study to Determine the PK of 25 and 50 mg OD Single and Multiple Dose Over 14 Days, of Vildagliptin and Its Metabolites in Renal Impaired Patients Compared to Matching Healthy Volunteers[NCT00818571]	Phase 1/Phase 2	96 participants (Actual)	Interventional	2008-12-31	Completed
Comparative Efficacy and Safety of Vildagliptin Versus Metformin in Reduction of Cardiovascular Complications in Type 2 Diabetic Patients With Hypertension[NCT03253562]	Phase 4	120 participants (Actual)	Interventional	2017-02-01	Completed
A Multicenter, Open-label Sub-study to LMF237A2302 to Assess the Effect of 24 Weeks Treatment With Initial Combination of Vildagliptin 100mg qd Plus Metformin 1000mg Bid in Drug Naive Patients With Type 2 Diabetes With Very Poor Glycemic Control[NCT00468039]	Phase 3	94 participants (Actual)	Interventional	2007-03-06	Completed
A Multicenter, Double-blind, Randomized Parallel-group, Study to Demonstrate the Effect of 24 Weeks Treatment With Vildagliptin 100 mg qd as add-on to Metformin 500 mg Bid Compared to Metformin 1000 mg Bid in Patients With Type 2 Diabetes Inadequately Con[NCT00396357]	Phase 3	914 participants (Actual)	Interventional	2006-10-31	Completed
A Multicentre, National, Randomized, Parallel-group, Phase 3 Study to Compare the Efficacy and Safety of Gemigliptin and Vildagliptin as Add-on Therapy to Metformin in People With Type 2 Diabetes Inadequately Controlled With Metformin[NCT02343926]	Phase 3	443 participants (Actual)	Interventional	2014-12-31	Completed
[NCT00860288]	Phase 2/Phase 3	1,988 participants (Actual)	Interventional	2009-02-28	Completed
A 28 Week Extension to a 24 Week Multi-center, Randomized, Double-blind Clinical Trial to Evaluate the Safety and Tolerability of Vildagliptin (50 mg qd) Versus Placebo in Patients With Type 2 Diabetes and Moderate or Severe Renal Insufficiency[NCT00765830]	Phase 3	349 participants (Actual)	Interventional	2008-09-30	Completed
A Clinical Study to Assess the Effect of Vildagliptin on Beta Cell Function in Drug Naive Patients With Type 2 Diabetes[NCT00260156]	Phase 3	59 participants (Actual)	Interventional	2005-11-30	Completed
Effect of the DPP-4 Inhibitor, Vildagliptin, on Gastric Accommodation and Food Intake in Humans[NCT03500900]		20 participants (Actual)	Interventional	2016-03-01	Completed
Efficacy of Vildagliptin Versus Metformin in Poly Cystic Ovary Syndrome: A Randomized Clinical Trial[NCT06142656]	Phase 2/Phase 3	60 participants (Anticipated)	Interventional	2023-11-25	Recruiting
A Multi-center, Randomized, Double-blind Clinical Trial to Evaluate the Safety and Tolerability of 24 Weeks Treatment With (50 mg qd) Versus Placebo in Patients With Type 2 Diabetes and Moderate or Severe Renal Insufficiency[NCT00646542]	Phase 3	525 participants (Actual)	Interventional	2005-03-31	Completed
Effect of Glimepiride, Vildagliptin, Pioglitazone and Canagliflozin on Durability of Glycemic Control After Metformin Failure in Type 2 Diabetes[NCT02142309]	Phase 4	450 participants (Anticipated)	Interventional	2005-10-31	Recruiting
A Multi-center, Randomized, Double-blind Placebo Controlled Study to Evaluate the Efficacy and Safety of 24 Weeks Treatment With Vildagliptin 50 mg Bid as add-on Therapy to Metformin Plus Glimepiride in Patients With Type 2 Diabetes[NCT01233622]	Phase 3	317 participants (Actual)	Interventional	2010-10-31	Completed
Vildagliptin Compared to Gliclazide in Combination With Metformin in Patients With Type 2 Diabetes[NCT00102466]	Phase 3	1,007 participants (Actual)	Interventional	2005-01-31	Completed
A Multi-center, Randomized, Double-blind, Placebo-controlled Clinical Trial to Evaluate the Effect of 52 Weeks Treatment With Vildagliptin on Left Ventricular Function in Patients With Type 2 Diabetes and Congestive Heart Failure[NCT00894868]	Phase 4	798 participants (Actual)	Interventional	2009-05-31	Completed
A Multicenter, Randomized, Double-Blind, Active Controlled Study to Compare the Effect of 24 Weeks Treatment With Vildagliptin 100 mg qd or Metformin 1500 mg Daily in Elderly Drug Naive Patients With Type 2 Diabetes[NCT00383578]	Phase 3	335 participants (Actual)	Interventional	2006-09-30	Completed
A Randomized, Double-blind, Active-controlled, Multicenter Study to Compare the Effect of 24 Weeks Treatment With a Fixed Combination Therapy of Vildagliptin and Metformin to the Individual Monotherapy Components in Drug Naive Patients With Type 2 Diabete[NCT00382096]	Phase 3	1,179 participants (Actual)	Interventional	2006-09-30	Completed
A Multi-center, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Efficacy and Safety of 24 Weeks Treatment With Vildagliptin in Type 2 Diabetes Mellitus Patients ≥ 70 Years (Drug-naive or Inadequately Controlled on Oral Agents)[NCT01257451]	Phase 3	431 participants (Actual)	Interventional	2010-12-31	Completed
Does Modulating the Gut Hormones, Incretins, Modify Vascular Function, Thereby Reducing the Risk of Vascular Complications in Insulin Resistant Individuals?[NCT01122641]	Phase 3	15 participants (Actual)	Interventional	2010-05-31	Completed
Effects of Vildagliptin, a DPP-4 Inhibitor, in Elderly Diabetic Patients With Mild Cognitive Impairment[NCT03819127]	Phase 4	60 participants (Actual)	Interventional	2015-01-31	Completed
Randomized, Open Label, Two-sequence, Two-treatment, Two-period, Crossover, Single Dose Bioequivalence Study of Vildagliptin Tablets 50 mg of AET Laboratories Pvt. Ltd., India With Galvus 50 mg Tablets of Novartis Europharm Ltd., United Kingdom in Normal [NCT05329844]		66 participants (Actual)	Interventional	2014-02-28	Completed
A Multicenter, Double-Blind, Randomized, Parallel-Group Study to Compare the Effect of 24 Weeks Treatment With Vildagliptin 50 mg Bid to Placebo as Add-On Therapy in Patients With Type 2 Diabetes Inadequately Controlled With Metformin Monotherapy[NCT00822211]	Phase 3	404 participants (Actual)	Interventional	2008-12-31	Completed
Open Label, Randomized, Single Dose, Two-way Crossover Bioequivalence Study of Vildagliptin From Gliptus 50 mg Tablet (EVA Pharma, Egypt) and Galvus 50 mg Tablet (NOVARTIS PHARMA, GERMANY)[NCT02816970]	Phase 1	24 participants (Actual)	Interventional	2014-02-28	Completed
12-week Randomized Study to Compare the Effect of Vildagliptin vs. Glibenclamide Associated to Metformin in Endothelial Function in Patients With Type 2 Diabetes and Hypertension[NCT02145611]	Phase 4	50 participants (Actual)	Interventional	2013-07-31	Completed
Vildagliptin Compared to Pioglitazone in Combination With Metformin in Patients With Type 2 Diabetes[NCT00237237]	Phase 3	588 participants	Interventional	2005-10-31	Completed
A Multicenter, Open Label, Long-Term Safety Study of 52 Weeks Treatment With Vildagliptin in Patients With Type 2 Diabetes[NCT01159249]	Phase 3	245 participants (Actual)	Interventional	2010-06-30	Completed
[NCT00821977]	Phase 2/Phase 3	338 participants (Actual)	Interventional	2008-11-30	Completed
Efficacy and Safety of Vildagliptin in Combination With Pioglitazone in Patients With Type 2 Diabetes[NCT00099853]	Phase 3	362 participants (Actual)	Interventional	2004-05-31	Completed
Randomized, Two-way, Two-period, Single Oral Dose, Open-label, Crossover, Bioequivalence Study to Compare Metformin / Vildagliptin Film Coated Tablets (1000 mg/50 mg) Versus Galvumet® Film Coated Tablets (1000 mg/50 mg)[NCT06073600]	Phase 1	18 participants (Actual)	Interventional	2022-05-20	Completed
A Prospective, Multicenter, Randomized, Open-label Study of 12 Week Duration to Evaluate the Effect of VILDagliptin Added to Insulin on Glycaemic Control in haemoDIALyzed Patients With Type 2 Diabetes: Probe Analysis of CGM[NCT02176681]	Phase 4	70 participants (Actual)	Interventional	2014-06-30	Completed
Feed-Back Suppression of Meal-Induced GLP-1 Secretion Mediated Through Elevations in Intact GLP-1 Caused by Dipeptidyl Peptidase 4 (DPP-4) Inhibition: A Randomized, Prospective Comparison of Sitagliptin and Vildagliptin Treatment[NCT02749032]	Phase 1	24 participants (Actual)	Interventional	2011-11-30	Completed
Evaluation of the Efficacy of Rapamycin and a Dipeptidyl Peptidase-4 Inhibitor (Vildagliptin) in Improving Beta Cell Function in Type 1 Diabetes of Long Duration, a Perspective Randomized Study[NCT02803892]	Phase 2	55 participants (Actual)	Interventional	2016-05-31	Completed
A Double-blind, Placebo-controlled, Randomized, Cross-over Study to Evaluate the GLP-1-mediated and Non-GLP-1-mediated Effects of LAF237 on Glucagon Secretion in Patients With Type 2 Diabetes and in Healthy Subjects[NCT00651105]	Phase 3	63 participants (Actual)	Interventional	2008-02-29	Completed
Effect of Dosage Reduction of Glucose-Lowering Multidrug Regimens on the Incidence of Acute Glycemic Complications in People With Type 2 Diabetes Who Fast During Ramadan: An Open-Label, Parallel-Group, Randomized, Controlled Trial[NCT04237493]	Phase 4	687 participants (Actual)	Interventional	2017-02-14	Completed
The Effect of Vildagliptin on Endothelium-dependent Vasodilatation. A Double Blind Cross-over Study in Type 2 Diabetes Mellitus.[NCT01000688]	Phase 3	16 participants (Anticipated)	Interventional	2010-01-31	Completed
Effect of Adding Vildagliptin on Beta Cell Function and Cardiovascular Risk Markers in Patients With Moderate Metabolic Control During Metformin Monotherapy[NCT01565096]	Phase 4	44 participants (Anticipated)	Interventional	2011-11-30	Recruiting
A Phase II, Randomized, Double-blind, 2-arm Controlled Study to Evaluate Efficacy of the DPPIV-inhibitor Vildagliptin for Prevention of Type 2 Diabetes in Women With a Recent History of Insulin-requiring Gestational Diabetes[NCT01018602]	Phase 2	140 participants (Anticipated)	Interventional	2008-01-31	Recruiting
A Double Blind, Cross Over, Placebo Controlled, Multiple-dose Study to Evaluate the Effects of LAF237 on Gastric Emptying, Gastric Volume and Satiety in Patients With Type 2 Diabetes.[NCT00952991]	Phase 3	18 participants	Interventional	2005-05-31	Completed
A 24-week, Open-label, Randomized, Multi-center, Parallel-group Study to Evaluate the Efficacy and Safety of Early Combination of Vildagliptin and Metformin in Patients With Type 2 Diabetes Mellitus Who Are Inadequately Controlled With Prior Metformin Mon[NCT00975065]	Phase 4	266 participants (Actual)	Interventional	2009-08-31	Completed
A Double-blind, Crossover, Placebo-Controlled, Multiple-dose Study to Evaluate the Effects of Vildagliptin on Gastric Emptying, Gastric Volume and Satiety in Patients With Type 2 Diabetes[NCT00351507]	Phase 3	10 participants (Actual)	Interventional	2005-05-31	Completed
The Impact of Metformin and Dipeptidyl Peptidase- 4 Inhibitors on Cognitive Function and Cardiovascular Protection in Type 2 Diabetic Patients[NCT05429554]		60 participants (Anticipated)	Observational	2022-06-30	Recruiting
Randomized, Open Label, Two-sequence, Two-treatment, Two-period, Crossover, Single Dose Bioequivalence Study Fixed-dose Combination of Metformin and Vildagliptin Tablets 1000/50 mg Manufactured by Oman Pharmaceuticals Products Co. LLC, Sultanate of Oman, [NCT05329857]		60 participants (Actual)	Interventional	2015-12-31	Completed
Randomized, Two-way, Two-period, Single Oral Dose, Open-label, Crossover, Bioequivalence Study to Compare Metformin/Vildagliptin (850 mg/50 mg) Film-coated Tablets Versus Galvumet®, in Healthy Subjects Under Fed Conditions.[NCT06103747]	Phase 1	18 participants (Actual)	Interventional	2023-02-21	Completed
Cross-over Study to Assess the Difference in Fasting Plasma Glucose (FPG) Between Vildagliptin (Galvus®/Eucreas®) and Sitagliptin (Januvia®/Janumet®) After Two Weeks[NCT01398592]	Phase 4	187 participants (Actual)	Interventional	2011-06-30	Completed
A Randomized, Open-label, Cross-over Study to Evaluate Patient Preferences for Eucreas® Versus Victoza® as add-on to Metformin in Type 2 Diabetes Mellitus Patients Who Did Not Have Adequate Glycaemic Control With Metformin.[NCT01518101]	Phase 4	62 participants (Actual)	Interventional	2012-01-31	Completed
Vildagliptin in New Onset Diabetes After Transplantation - A Double-blind, Randomized, Placebo-controlled Trial[NCT00980356]	Phase 2	32 participants (Actual)	Interventional	2009-09-30	Completed
Functional Improvement of Progenitor Cells and Endothelial Function by Vildagliptin in Diabetes Mellitus (FINNjA-DM).[NCT00936234]	Phase 2/Phase 3	0 participants (Actual)	Interventional	2009-07-31	Withdrawn(stopped due to insufficient recruitment)
Short Term Effect of Liraglutide Versus Vildagliptine on Insulin Secretion and Insulin Sensitivity in a Sub Saharan African Population With Type 2 Diabetes[NCT02832999]	Phase 4	14 participants (Actual)	Interventional	2016-01-31	Completed
Comparison of Empaglifozin and Vildagliptin in Efficacy and Safety in Type 2 Diabetes Mellitus[NCT05359432]	Phase 4	120 participants (Actual)	Interventional	2020-07-01	Completed
Efficacy and Safety of Vildagliptin in Subjects With Impaired Glucose Tolerance[NCT00237250]	Phase 3	171 participants (Actual)	Interventional	2005-10-31	Completed
A 12-week Study to Compare the Effects of Vildagliptin Versus Glibenclamide on Glycemic Variability After a Sub Maximal Exercise Test in Patients With Type 2 Diabetes Inadequately Controlled With Metformin.[NCT01867502]	Phase 4	20 participants (Anticipated)	Interventional	2014-04-30	Recruiting
A Single-center, Double-blind, Randomized, Placebo-controlled, Cross-over Study to Assess the Effect of Vildagliptin on Glucagon Counterregulatory Response During Hypoglycemia in Patients With Type 2 Diabetes.[NCT00390520]	Phase 3	28 participants (Anticipated)	Interventional	2006-09-30	Completed
A Multicenter, Open, Long Term Safety Study of 52 Weeks Treatment With Vildagliptin (100 mg qd) In Patients With Type 2 Diabetes (Extension Study of Study CLAF237A1303)[NCT00389415]	Phase 3	150 participants	Interventional	2006-10-31	Completed
A 24-week, Multi-center, Double-blind, Randomized, Placebo-controlled, Parallel-group Study to Assess the Efficacy and Safety of Vildagliptin 50mg Bid as an add-on Therapy to Insulin, With or Without Metformin, in Patients With Type 2 Diabetes Mellitus[NCT01582230]	Phase 3	293 participants (Actual)	Interventional	2012-04-30	Completed
An Open-Label, Parallel-Group Study to Determine the Single and Multiple Dose Pharmacokinetics of Vildagliptin and Its Metabolites in Mild, Moderate or Severe Renal Impaired Patients Compared to Age, Sex and Weight-Matched Healthy Volunteers Following Dai[NCT00567047]	Phase 1	96 participants (Anticipated)	Interventional	2007-07-31	Completed
A Multicentric, Randomized, Open Label Study on Comparison of Pancreatic Beta Cell Recovery and Preservation in Type 2 Diabetic Patients Treated With DPP-4 Inhibitor (Vildagliptin) and Metformin[NCT02853630]	Phase 4	203 participants (Actual)	Interventional	2013-12-31	Completed
The Effect of Vildagliptin Based Treatment Versus Sulfonylurea on Glycemic Variability, Oxidative Stress, GLP-1, and Endothelial Function in Patients With Type 2 Diabetes[NCT01404676]	Phase 4	34 participants (Actual)	Interventional	2010-06-30	Completed
Extension to a Study to Assess the Efficacy and Safety of Three Doses of Vildagliptin in Patients With Type 2 Diabetes[NCT00138541]	Phase 3	440 participants (Actual)	Interventional	2004-10-31	Completed
The Swiss Glucose Variability Study[NCT01426737]	Phase 4	50 participants (Anticipated)	Interventional	2011-04-30	Recruiting
A 12 Week Multi Center, Open Label, Single Arm Study to Assess the Safety and Efficacy of Vildagliptin 50 mg Twice Daily in Patients With Type 2 Diabetes Mellitus Inadequately Controlled With Metformin[NCT01426802]	Phase 4	150 participants (Actual)	Interventional	2010-10-31	Completed
Vildagliptin for Treatment of Antipsychotic-induced Dyslipidemia: a Randomized, Double-blind, Placebo-controlled Study[NCT04761861]	Phase 2	150 participants (Anticipated)	Interventional	2021-02-16	Recruiting
Randomized, Open Label, Two-sequence, Two-treatment, Two-period, Crossover, Single Dose Bioequivalence Study Fixed-dose Combination of Metformin and Vildagliptin Tablets 850/ 50 mg Manufactured by Oman Pharmaceuticals Products Co. LLC, Sultanate of Oman, [NCT05337969]		60 participants (Actual)	Interventional	2015-12-31	Completed
A Multicenter, Double-Blind, Randomized, Parallel-Group Placebo-Controlled Study to Compare the Effect of 13-Week Treatment With Vildagliptin as Add-On Therapy to Improve Glucose Variability in Type 2 Diabetes Mellitus Patients Inadequately Controlled Wit[NCT01862263]	Phase 4	191 participants (Actual)	Interventional	2013-05-31	Terminated
A Multicenter, Double-blind, Randomized, Parallel-Group Study to Compare the Effect of 24 Weeks Treatment With Vildagliptin 100 MG QD to Placebo as Add-on Therapy in Patients With Type 2 Diabetes Inadequately Controlled With Metformin Monotherapy[NCT00351884]	Phase 3	370 participants (Actual)	Interventional	2006-05-31	Completed
Evaluation of Vildagliptin (Galvus®) as add-on to Insulin in Residual β-cell Function and Inflammatory Markers in New-onset Type 1 Diabetes Mellitus.[NCT01559025]	Phase 3	44 participants (Anticipated)	Interventional	2014-03-31	Recruiting
The Effect of DPP4 Inhibitor on Glycemic Variability in Patients With Type 2 Diabetes Treated With Twice Daily Premixed Human Insulin[NCT04654676]	Phase 4	12 participants (Actual)	Interventional	2018-09-15	Completed
A Double-Blind, Placebo-Controlled, Randomized, Crossover Study to Explore the Acute Effects of LAF 237 on the Rate of Appearance and Disappearance of Glucose During the Overnight Post-Absorptive Period in Type 2 Diabetics[NCT00230464]	Phase 3	16 participants	Interventional	2004-11-30	Completed
A Clinical Study to Assess the Efficacy and Safety of Vildagliptin in Patients With Type 2 Diabetes[NCT00238498]	Phase 2	291 participants (Actual)	Interventional	2004-07-31	Completed
Efficacy and Safety of Vildagliptin Compared to Rosiglitazone in Drug Naive Patients With Type 2 Diabetes[NCT00099918]	Phase 3	717 participants (Actual)	Interventional	2004-05-31	Completed
A Clinical Study to Assess the Effect of Vildagliptin on Postprandial Lipid Parameters in Patients With Type 2 Diabetes[NCT00099957]	Phase 2	38 participants	Interventional	2003-09-30	Completed
Efficacy and Safety of Vildagliptin in Patients With Type 2 Diabetes With HbA1c 9-11%[NCT00101673]	Phase 3	251 participants (Actual)	Interventional	2004-03-31	Completed
Efficacy and Safety of Vildagliptin Compared to Placebo in Patients With Type 2 Diabetes and Mild Hyperglycemia[NCT00101712]	Phase 3	274 participants (Actual)	Interventional	2004-10-31	Completed
A Single-blind, Single-treatment Study to Evaluate the Effects of Vildagliptin on Response to an Intravenous Glucose Load in Pre-diabetic Subjects With Impaired Fasting Glucose[NCT00312130]	Phase 3	20 participants	Interventional	2005-04-30	Completed
A Randomized, Double-Blind, Placebo-Controlled, Time-Lagged, Parallel-Group, Ascending Single and Multiple Oral Dose Study of the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of LAF237 in Chinese Healthy Subjects[NCT00419887]	Phase 1	60 participants	Interventional	2006-09-30	Completed
A Multicenter, Double-Blind, Randomized, Parallel-Group Study to Compare the Effect of 12 Weeks Treatment With Vildagliptin to Placebo as Add-on Therapy to Sulfonylurea in Patients With Type 2 Diabetes Inadequately Controlled With Sulfonylurea Monotherapy[NCT00325117]	Phase 3	200 participants	Interventional	2006-04-30	Completed
A Multicenter, Open, Long Term Safety Study of 52 Weeks Treatment With Vildagliptin in Patients With Type 2 Diabetes[NCT00325429]	Phase 3	150 participants	Interventional	2006-04-30	Completed
Efficacy and Safety of Vildagliptin Compared to Metformin in Drug Naive Patients With Type 2 Diabetes[NCT00099866]	Phase 3	570 participants (Actual)	Interventional	2004-01-31	Completed
A Clinical Study to Assess the Efficacy and Safety of Three Doses of Vildagliptin in Patients With Type 2 Diabetes[NCT00099905]	Phase 3	639 participants (Actual)	Interventional	2004-04-30	Completed
Efficacy and Safety of Vildagliptin in Combination With Glimepiride in Patients With Type 2 Diabetes[NCT00099944]	Phase 3	515 participants (Actual)	Interventional	2004-05-31	Completed
Extension to a Study on the Efficacy and Safety of Vildagliptin Compared to Metformin in Drug Naive Patients With Type 2 Diabetes[NCT00138567]	Phase 3	530 participants	Interventional	2005-01-31	Completed
Extension to a Study on the Efficacy and Safety of Vildagliptin in Combination With Insulin in Patients With Type 2 Diabetes[NCT00138606]	Phase 3	179 participants (Actual)	Interventional	2005-01-31	Completed
Efficacy and Safety of Vildagliptin Compared to Acarbose in Drug Naive Patients With Type 2 Diabetes[NCT00110240]	Phase 3	594 participants (Actual)	Interventional	2005-04-30	Completed
A Multicenter, Double-Blind, Randomized, Parallel-Group Study to Compare the Effect of 12 Weeks Treatment With Vildagliptin (50mg qd, 50mg Bid, 100mg qd) to Placebo in Patients With Type 2 Diabetes[NCT00351832]	Phase 3	236 participants	Interventional	2006-06-30	Completed
Efficacy and Safety of Three Doses of Vildagliptin in Drug Naive Patients With Type 2 Diabetes[NCT00120536]	Phase 3	288 participants (Actual)	Interventional	2005-06-30	Completed
A Multicenter, Randomized, Double-blind, Parallel-group Study to Investigate the Glucose Lowering Effect, Safety and Tolerability of 24 Weeks Treatment With Vildagliptin 100 mg o.d. Versus Placebo Followed by a 12 Weeks Treatment Period With Open-label Vi[NCT00494884]	Phase 3	0 participants	Interventional	2007-06-30	Completed
Extension to a Study on the Efficacy and Safety of Vildagliptin in Combination With Metformin in Patients With Type 2 Diabetes[NCT00138515]	Phase 3	418 participants (Actual)	Interventional	2004-11-30	Completed
Extension to a Study on the Efficacy and Safety of Vildagliptin in Combination With Pioglitazone in Patients With Type 2 Diabetes[NCT00138554]	Phase 3	318 participants (Actual)	Interventional	2004-11-30	Completed
Extension to a Study of the Efficacy and Safety of Vildagliptin in Patients With Type 2 Diabetes With HbA1c 9-11%[NCT00138593]	Phase 3	180 participants	Interventional	2004-07-31	Completed
Dipeptidyl Peptidase (DPP) IV Inhibition Facilitates Healing of Chronic Foot Ulcers in Patients With Type 2 Diabetes[NCT01472432]	Phase 4	106 participants (Actual)	Interventional	2011-05-31	Completed
An Open-label, Parallel-group Study to Determine the Single and Multiple Dose Pharmacokinetics of LAF237 and Its Metabolites in Mild Renal Impaired Patients Compared to Age, Sex and Weight-matched Healthy Volunteers Following Daily Doses of 100 mg LAF237 [NCT00572650]	Phase 1	29 participants (Actual)	Interventional	2007-10-31	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
An Open-labeled, Randomized, Multicenter, Prospective, Parallel Group, Interventional Study to Demonstrate the Effectiveness of 24 Weeks Treatment With Vildagliptin 50mg Bid as Add on to Metformin 500 mg Bid Compared to Metformin up to 1000 mg Bid in Chin[NCT01541956]	Phase 4	3,091 participants (Actual)	Interventional	2012-02-29	Completed
Efficacy and Safety of Vildagliptin in Combination With Metformin in Patients With Type 2 Diabetes[NCT00099892]	Phase 3	544 participants (Actual)	Interventional	2004-05-31	Completed
Efficacy and Safety of Vildagliptin in Combination With Insulin in Patients With Type 2 Diabetes[NCT00099931]	Phase 3	254 participants (Actual)	Interventional	2004-05-31	Completed
Efficacy and Safety of Vildagliptin in Combination With Pioglitazone in Drug Naive Patients With Type 2 Diabetes[NCT00101803]	Phase 3	527 participants (Actual)	Interventional	2005-01-31	Completed
Efficacy and Safety of Vildagliptin Compared to Gliclazide in Drug Naive Patients With Type 2 Diabetes[NCT00102388]	Phase 3	1,092 participants (Actual)	Interventional	2005-01-31	Completed
Extension to a Study on the Efficacy and Safety of Vildagliptin in Combination With Glimepiride in Patients With Type 2 Diabetes[NCT00138580]	Phase 3	345 participants	Interventional	2004-11-30	Completed
Extension to a Study on the Efficacy and Safety of Vildagliptin Compared to Rosiglitazone in Drug Naive Patients With Type 2 Diabetes[NCT00138619]	Phase 3	478 participants (Actual)	Interventional	2004-11-30	Completed
A Single-center, Double-blind, Randomized, Placebo-controlled, Cross-over Study to Assess the Effect of Vildagliptin on the Incretin Effect in Patients With Type 2 Diabetes Treated With Metformin[NCT00396071]	Phase 3	22 participants (Actual)	Interventional	2006-10-31	Completed
A Multi-center, Randomized, Open-label, Active Controlled, Parallel Arm Study to Compare the Efficacy of 12 Weeks of Treatment With Vildagliptin 100 mg, qd to Thiazolidinedione (TZD) as add-on Therapy in Patients With Type 2 Diabetes Inadequately Controll[NCT00396227]	Phase 3	2,665 participants (Actual)	Interventional	2006-10-31	Completed
Effects of DPP4 Inhibitor Versus SGLT2 Inhibitor on Ischemic Burden in Stable Ischemic Heart Disease Patients[NCT03178591]	Phase 4	43 participants (Actual)	Interventional	2014-10-31	Completed
Effect of Vildagliptin Versus Glimepiride on Copeptin and Fetuin-A in Type 2 Diabetic Patients[NCT06068686]		70 participants (Anticipated)	Interventional	2022-10-01	Recruiting
Evaluate Efficacy and Safety of Gosogliptin as Monotherapy and in Combination With Metformin vs. Vildagliptin as Monotherapy and in Combination With Metformin in Drug-naive Type 2 Diabetic Patients.[NCT03088670]	Phase 3	299 participants (Actual)	Interventional	2013-04-23	Completed
A Multicenter, Randomized, Double-Blind, Active-Controlled Study to Compare the Effects of 12 Weeks Treatment With Vildagliptin 50 mg Bid to Voglibose 0.2 mg Tid in Patients With Type 2 Diabetes[NCT00368134]	Phase 3	370 participants	Interventional	2006-08-31	Completed
Study of the Effect of Vildagliptin Versus Dapagliflozin on Glucagon Response to Mixed Meal in Metformin-treated Subjects With Type 2 Diabetes[NCT02475070]	Phase 4	28 participants (Actual)	Interventional	2016-01-31	Completed
Randomized, Open Label, Two Parallel Arms, Intervention Trial Comparing the Effect of DPP-IV Inhibitor Vildagliptin vs. Glibenclamide on Circulating Endothelial Progenitor Cell Number in Patients With Type 2 Diabetes in Metformin Failure[NCT01822548]	Phase 3	64 participants (Actual)	Interventional	2010-10-31	Completed
A Single Center, Randomized, Open-Label, Crossover, Single Oral Dose Study to Assess the Bioequivalence of LAF237 Tablet Manufactured by Beijing Novartis Pharma Ltd. to Imported LAF237 Tablet in Chinese Healthy Subjects[NCT00414947]	Phase 1	30 participants	Interventional	2006-12-31	Completed
A 56-Week Extension to a Clinical Study to Assess the Efficacy and Safety of Vildagliptin Compared to Placebo in Drug Naive Patients With Type 2 Diabetes and Mild Hyperglycemia[NCT00300287]	Phase 3	150 participants	Interventional	2006-02-20	Completed
A Multicenter, Double-Blind, Randomized, Parallel-Group Study to Compare the Effect of 12 Weeks Treatment With LAF237 50 mg Bid to Placebo as Add-On Therapy in Patients With Type 2 Diabetes Inadequately Controlled With Metformin Monotherapy[NCT01497522]	Phase 3	183 participants (Actual)	Interventional	2011-12-31	Completed
A Multicenter, Randomized, Double-Blind Comparative Study of Efficacy，Tolerance and Safety Between Sitagliptin ,Vildagliptin and Saxagliptin After 12-week Monotherapy in Drug-naive Adult Patients With Type 2 Diabetes Mellitus[NCT01703637]		300 participants (Anticipated)	Interventional	2012-10-31	Recruiting
Evaluation of Galvus (Vildagliptin) Efficacy Versus Placebo in Patients With Type 2 Diabetes, Inadequately Controlled by Metformin and Basal Insulin, This One Having Been Properly Titrated.[NCT01757587]	Phase 4	39 participants (Actual)	Interventional	2011-12-31	Completed
A Double Blind, Double Dummy, Randomised, Multi-centre Study to Assess the Tolerability and Efficacy Profile of Vildagliptin Compared to Gliclazide as Dual Therapy With Metformin in Muslim Patients With Type 2 Diabetes Fasting During Ramadan[NCT01758380]	Phase 4	557 participants (Actual)	Interventional	2013-01-31	Completed
The Use of Incretin-based Drugs and the Risk of Pancreatic Cancer in Patients With Type 2 Diabetes[NCT02475499]		886,172 participants (Actual)	Observational	2014-03-31	Completed
Effects of Vildagliptine and Glimepiride on Glycemic Variability and Cardiovascular Parameters in Patients With Type 2 Diabetes by CGMS[NCT01812122]	Phase 4	16 participants (Actual)	Interventional	2013-03-31	Completed
Acute and Short-term Chronic Effects of Galvus (Vildagliptin) on Endothelial Function and Oxidative Stress on Recently Diagnosed Type 2 Diabetic Obese Women: the Role of Intestinal Peptides During Lipid Overload[NCT01827280]	Phase 4	40 participants (Actual)	Interventional	2013-04-30	Completed
Effect of Vildagliptin on Adipose Tissue and Skeletal Muscle Metabolism in Obese Patients With Type 2 Diabetes[NCT00380445]	Phase 3	21 participants (Actual)	Interventional	2006-01-31	Completed
A Randomized, Single-blind, Placebo Controlled, Cross-over Study to Evaluate the Acute Effects of Vildagliptin on Gastric Emptying in Patients With Type 2 Diabetes.[NCT00380380]	Phase 3	18 participants	Interventional	2006-01-31	Completed
The DPP-4 Inhibitor Vildagliptin as Adjunct in Major Depressive Disorder Patients: A Proof-of-Concept, Randomized, Double-Blind, Placebo-Controlled Trial[NCT04410341]	Phase 1/Phase 2	100 participants (Anticipated)	Interventional	2020-05-01	Recruiting
An Open-label, Multiple Dose Study to Assess the Steady-state Skin Concentrations and Pharmacokinetics of Vildagliptin 50 mg BID for 10 Days in Healthy Subjects and Patients With Type 2 Diabetes[NCT00633997]	Phase 1/Phase 2	22 participants (Actual)	Interventional	2008-02-29	Terminated(stopped due to After analysis of the existing data, it was determined that additional skin biopsy samples would not be required to determine study outcome.)
Prevention of New Onset Diabetes After Transplantation by a Short Term Treatment of Vildagliptin in the Early Post-transplant Period[NCT02849899]	Phase 3	186 participants (Anticipated)	Interventional	2018-10-26	Recruiting
Effect of a DPP-IV Inhibitor Treatment on the Secretion of Glucagon in Patients Presenting With Type 1 Diabetes Mellitus With or Without Autonomic Neuropathy[NCT01452113]	Phase 2	21 participants (Actual)	Interventional	2010-10-31	Completed
Effect of Acarbose and Vildagliptin on Visceral Fat Distribution in Overweight and Obesity Patients With Newly Diagnosed Type 2 Diabetes Mellitus: A Randomized Control Study[NCT02999841]	Phase 4	100 participants (Anticipated)	Interventional	2016-03-31	Recruiting
Investigating the Protective Effect of Newer Antidiabetic Drugs on Cognitive Decline in Diabetic Patients[NCT05347459]		100 participants (Anticipated)	Observational	2022-03-02	Recruiting
Effects of Vildagliptin/Metformin Combination on Markers of Atherosclerosis, Thrombosis, and Inflammation in Diabetic Patients With Coronary Artery Disease[NCT01604213]	Phase 4	60 participants (Actual)	Interventional	2012-09-30	Completed
A Study to Assess the Effects of DPP-4 Inhibition on Insulin Sensitivity in Type 2 Diabetes[NCT00351546]	Phase 3	12 participants (Actual)	Interventional	2005-02-28	Completed
A Double-blind, Placebo-controlled, Randomized, Parallel-group Study to Evaluate the Effects of Vildagliptin on the Maximum Insulin Secretion in Patients With Type 2 Diabetes Mellitus[NCT00351585]	Phase 3	39 participants (Actual)	Interventional	2004-07-31	Completed
A Prospective, Open-label, Interventional Study to Assess the HbA1c Change an 24-hr Glucose Fluctuation After Vildagliptin Plus Metformain (SPC) Treatment in Metformin Monotherapy Uncontrolled Type 2 Diabetes Mellitus Patients[NCT01582243]	Phase 4	40 participants (Actual)	Interventional	2013-04-30	Completed
Multicentric Cross-over Trial to Assess the Glycemic Profiles on 8 Weeks of Vildagliptin and Sitagliptin Treatment, Each, in Type-2 Diabetic Patients With a Pre-existing Cardiovascular Disease Pre-treated With Insulin, Using a PROBE-design[NCT01686932]	Phase 4	51 participants (Actual)	Interventional	2012-11-30	Completed
Comparative Effecacy of Metformin and Vildagliptin on Cardiometabolic Risk Factors, Metabolic Syndrome, and Diabetic Nephropathy Progression[NCT04485845]	Phase 4	39 participants (Anticipated)	Interventional	2019-11-01	Recruiting
A 5-year Study to Compare the Durability of Glycemic Control of a Combination Regimen With Vildagliptin & Metformin Versus Standard-of-care Monotherapy With Metformin, Initiated in Treatment-naïve Patients With Type 2 Diabetes Mellitus[NCT01528254]	Phase 4	2,004 participants (Actual)	Interventional	2012-03-30	Completed
The Effect of Adding Vildagliptin Versus Glimepiride to Metformin on Markers of Inflammation, Thrombosis, and Atherosclerosis in Diabetic Patients With Symptomatic Coronary Artery Diseases[NCT03693560]	Phase 4	80 participants (Actual)	Interventional	2018-10-08	Completed
Randomized, Open-label, SU-controlled Study of 24-week Duration to Compare Metformin/Vildagliptin + Basal Insulin Versus Metformin/SU + Basal Insulin in T2DM Patients Starting Basal Insulin After Failing Metformin/SU[NCT01871558]	Phase 3	42 participants (Actual)	Interventional	2013-06-30	Completed
A Comparative Study to Assess the Effect of Vildagliptin Versus Glimepiride on Glucose Variability in Type 2 Diabetic Patients Uncontrolled on Metformin Alone[NCT01910441]	Phase 4	95 participants (Actual)	Interventional	2013-07-31	Terminated(stopped due to The study was terminated due to the unavailability of Continuous Glucose Monitoring sensors (CGMS) which were required to assess the primary end-point.)
An Open-label, Randomized, Active-controlled Study to Compare the Effect of 16 Weeks Treatment With Vildagliptin to Pioglitazone as add-on Therapy to Metformin in Type 2 Diabetic Patients Inadequately Controlled With Metformin Monotherapy[NCT01882907]	Phase 4	287 participants (Actual)	Interventional	2009-12-31	Completed
A Multi-center, Randomized, Double-Blinded, Parallel, Vildagliptin and Placebo-Controlled Phase III Clinical Study to Evaluate the Efficacy and Safety of PB-201 in Treatment-naive Patients With Type 2 Diabetes Mellitus[NCT05102149]	Phase 3	672 participants (Anticipated)	Interventional	2021-09-30	Recruiting
Safety and Efficacy of Sitagliptin, Vildagliptin, and Metformin in Recently Diagnosed Drug-naïve Patients With Type 2 Diabetes[NCT04916093]	Phase 4	60 participants (Actual)	Interventional	2019-12-20	Completed
Durable Effect of Imeglimin on the Glycemic Control in Patients With Type 2 Diabetes Mellitus: a Multicenter, Open-label, Randomized, Controlled Trial (DIGNITY Trial)[NCT05366868]	Phase 4	567 participants (Anticipated)	Interventional	2022-05-26	Recruiting
Efficacy and Safety of the Oral Combined Therapy Glimepiride / Vildagliptin / Metformin in Patients With Type 2 Diabetes With Dual Treatment Failure[NCT04841096]	Phase 3	172 participants (Anticipated)	Interventional	2023-03-21	Recruiting
A Local Phase IV, Multicenter, Open-label Study to Evaluate Early add-on Vildagliptin in Patients With Type 2 Diabetes Inadequately Controlled by Metformin[NCT01766778]	Phase 4	117 participants (Actual)	Interventional	2013-05-13	Completed
A Study to Assess and Compare the Pharmacokinetic and Pharmacodynamic Profiles for Sitagliptin, Saxagliptin and Vildagliptin in Patients With Type 2 Diabetes Mellitus[NCT01582308]	Phase 1	22 participants (Actual)	Interventional	2012-06-21	Completed
A 28-week Extension to a 24-week Multicenter, Randomized, Double-blind, Active-controlled Clinical Trial to Evaluate the Safety and Tolerability of Vildagliptin (50 mg qd) Versus Sitagliptin (25 mg qd) in Patients With Type 2 Diabetes and Severe Renal Ins[NCT00770081]	Phase 3	75 participants (Actual)	Interventional	2008-09-30	Completed
A Multicenter, Double-blind, Randomized Study to Compare the Efficacy of 24 Weeks Treatment With Fixed Combination Therapy of Vildagliptin and Metformin (25/1000 mg Bid) Versus Metformin Monotherapy (1000 mg Bid) in Patients With Type 2 Diabetes Inadequat[NCT00728351]	Phase 3	317 participants (Actual)	Interventional	2008-06-30	Completed
A Multi-center, Randomized, Double-blind, Active-controlled Clinical Trial to Evaluate the Safety and Tolerability of 24 Weeks Treatment With Vildagliptin (50 mg qd) Versus Sitagliptin (25 mg qd) in Patients With Type 2 Diabetes and Severe Renal Insuffici[NCT00616811]	Phase 3	148 participants (Actual)	Interventional	2008-01-31	Completed
Effect of Anti-diabetic Drugs on Bone Metabolism and Glycemic Variability.A Comparison Between Vildagliptin and Gliclazide MR[NCT01679899]	Phase 4	56 participants (Actual)	Interventional	2012-12-31	Completed
Glycemic Excursions in Type 2 Diabetic Patients Treated With Vildagliptin and Metformin (GalvusMet) Versus Glimepiride and Metformin[NCT02007278]	Phase 4	40 participants (Actual)	Interventional	2014-01-03	Completed
A 12-week, Multi-center, Double-blind, Randomized, Placebo-controlled, Parallel-group Study to Assess the Efficacy and Safety of Equa (Vildagliptin) 50 mg Bid as an add-on Therapy to Insulin, With or Without Metformin, in Patients With Type 2 Diabetes Mel[NCT02002221]	Phase 4	156 participants (Actual)	Interventional	2013-12-31	Completed
Evaluation of Continuous Glucose Monitoring as a Tool to Measure Glucoregulatory Effects of a Twice Daily Oral Insulin Secretagogue[NCT01537120]	Phase 1	25 participants (Actual)	Interventional	2011-12-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT01472432 (4) [back to overview]	Full Epithelialization of the Wound
NCT01472432 (4) [back to overview]	Capillary Density
NCT01472432 (4) [back to overview]	HIF-1α
NCT01472432 (4) [back to overview]	VEGF
NCT01528254 (8) [back to overview]	Time to Initial Treatment Failure
NCT01528254 (8) [back to overview]	Rate of Loss in Glycemic Control During Period 1
NCT01528254 (8) [back to overview]	Rate of Loss in Glycemic Control in Fasting Plasma Glucose (FPG) During Period 1
NCT01528254 (8) [back to overview]	Rate of Loss in Glycemic Control in Fasting Plasma Glucose (FPG) Over Time During Period 2
NCT01528254 (8) [back to overview]	Rate of Loss in Glycemic Control in HbA1c Over Time During Period 2
NCT01528254 (8) [back to overview]	Percentage of Participants With Adverse Events, Serious Adverse Events and Death
NCT01528254 (8) [back to overview]	Rate of Change in Insulin Sensitivity From Baseline to End of Study
NCT01528254 (8) [back to overview]	Rate of Loss of Beta Cell Function From Baseline to End of Study
NCT01537120 (3) [back to overview]	HbA1C At 12 Weeks
NCT01537120 (3) [back to overview]	24 Hour Weighted Mean Glucose (WMG) At 2 Weeks
NCT01537120 (3) [back to overview]	Hemoglobin A1C (HbA1C) At 2 Weeks
NCT01582243 (6) [back to overview]	Mean Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 12
NCT01582243 (6) [back to overview]	Mean Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 24
NCT01582243 (6) [back to overview]	Mean Change From Baseline in Mean Amplitude of Glycemic Excursions (MAGE) Detected by Continuous Glucose Monitoring System (CGMS) After 24-week
NCT01582243 (6) [back to overview]	Mean Change From Baseline in Fasting Plasma Glucose(FPG) at Week 12 and 24
NCT01582243 (6) [back to overview]	Mean Change From Baseline in Postprandial Plasma Glucose(PPG) at Week 12 and 24
NCT01582243 (6) [back to overview]	The Percentage of Patients Achieving the Two Glycemic Goals After 12- and 24-week Treatment
NCT01582308 (5) [back to overview]	Pharmacokinetic Analysis: Area Under the Curve 0-24 Hours (AUC 0-24hr)
NCT01582308 (5) [back to overview]	Percent Inhibition of Dipeptidyl Peptidase IV (DPP-4) Activity at Trough
NCT01582308 (5) [back to overview]	Pharmacokinetic Analysis: Area Under the Curve 0-12 Hours (AUC 0-12hr) for Vildagliptin 50 mg BID
NCT01582308 (5) [back to overview]	Pharmacokinetic Analysis: Peak Plasma Drug Concentration (Cmax)
NCT01582308 (5) [back to overview]	Pharmacokinetic Analysis: Time to the Peak Plasma Drug Concentration (Tmax)
NCT01686932 (11) [back to overview]	Change From Baseline of Inflammatory Biomarkers Interleukin 6 (IL-6) After 8 Weeks of Treatment in Period 1 & Period 2
NCT01686932 (11) [back to overview]	Change From Baseline of Inflammatory Biomarkers High Sensitivity C-reactive Protein (hsCRP) After 8 Weeks of Treatment in Period 1 & Period 2
NCT01686932 (11) [back to overview]	Number of Severe Hypoglycemic Events During Vildagliptin Treatment Compared to Sitagliptin Treatment After 8 Weeks of Treatment in Period 1 and Period 2
NCT01686932 (11) [back to overview]	Glucose Fluctuations During the Day Under Vildagliptin Treatment Compared to Sitagliptin Treatment on Day 2 After 8 Weeks of Treatment Period 1 & Period 2
NCT01686932 (11) [back to overview]	Hypoglycemic Profile of Vildagliptin Compared to Sitagliptin Over 4 Days After 8 Weeks of Treatment in Period 1 & 2
NCT01686932 (11) [back to overview]	Mean Amplitudes of Hypoglycemic Events (mmol/L) Measured With Continuous Glucose Monitoring (CGM) Over 4 Days After 8 Weeks of Treatment for Period 1 & Period 2
NCT01686932 (11) [back to overview]	Mean Duration of Hypoglycemic Events (Min.) Measured With Continuous Glucose Monitoring (CGM) Over 4 Days After 8 Weeks of Treatment for Period 1 & Period 2
NCT01686932 (11) [back to overview]	Percentage Change From Baseline of Pro-insulin/C-peptide Ratios After 8 Weeks of Treatment Period 1 & Period 2
NCT01686932 (11) [back to overview]	Number of Hypoglycemic Events During Vildagliptin Treatment Compared to Sitagliptin Treatment.
NCT01686932 (11) [back to overview]	Number of Occurrence of Pre-defined ECG Findings During 4 Days of Continuous ECG Monitoring at Baseline and in the 8th Week of Periods 1 and 2
NCT01686932 (11) [back to overview]	Number of Participants With ECG Abnormalities Depending on Hypoglycemic Events After 8 Weeks of Treatment Period 1 & Period 2
NCT01766778 (6) [back to overview]	Number of Patients With Adverse Events, Serious Adverse Events and Death as an Assessment of Overall Safety and Tolerability
NCT01766778 (6) [back to overview]	Change of Glycosylated Hemoglobin A1c (HbA1c) From Baseline to Month 12
NCT01766778 (6) [back to overview]	Percentage of Overall Drug Compliance in 12 Months
NCT01766778 (6) [back to overview]	Change in Fasting Plasma Glucose (FPG) From Baseline to Month 3, 6, 9 and 12 (Based on MMRM Analysis)
NCT01766778 (6) [back to overview]	Percentage of Patients Achieving Good Glycemic Control
NCT01766778 (6) [back to overview]	Change of Glycosylated Hemoglobin A1c (HbA1c) From Baseline to Month 3, 6, 9 and 12 (Based on MMRM Analysis)
NCT01822548 (2) [back to overview]	Absolute Change in HbA1C Compared to Baseline
NCT01822548 (2) [back to overview]	Absolute Change in the Endothelial Progenitor Cell (EPC) Number
NCT01871558 (7) [back to overview]	Change From Baseline in HbA1c to Week 24 in Both Treatment Arms
NCT01871558 (7) [back to overview]	Percentage of Patients Reaching Their Glycemic Target Without Hypoglycemic Events
NCT01871558 (7) [back to overview]	Mean Daily Insulin Dose at Week 24
NCT01871558 (7) [back to overview]	Change From Baseline in Body Weight in Both Treatment Arms
NCT01871558 (7) [back to overview]	Percent of Participants That Reach Therapeutic Goal (HbA1c ≤ 7%) at Week 24 Without Any Hypoglycaemic Episode (Symptomatic or Not) and Without Any Weight Gain (Variation ≥3% Compared to Baseline)
NCT01871558 (7) [back to overview]	Percentage of Patients Who Reported at Least One Symptomatic Hypoglycemic Event During the 24 Week Randomized Period in Both Treatment Arms
NCT01871558 (7) [back to overview]	Percentage of Patients With Severe and Confirmed Hypoglycemic Events
NCT01882907 (6) [back to overview]	the Mean Changes of Body Weight From Baseline Between Vildagliptin + Metformin and Pioglitazone + Metformin Groups
NCT01882907 (6) [back to overview]	the Mean Changes of FPG and PPG From Baseline Between Vildagliptin + Metformin and Pioglitazone + Metformin Groups
NCT01882907 (6) [back to overview]	Non-inferiority of HbA1C Change From Baseline in Vildagliptin + Metformin Group Compared With Pioglitazone + Metformin Group
NCT01882907 (6) [back to overview]	the Mean Changes of Insulin, C-peptide, HOMA-IR, HOMA-beta From Baseline Between Vildagliptin + Metformin and Pioglitazone + Metformin Groups
NCT01882907 (6) [back to overview]	the Mean Changes of Lipid Profiles From Baseline Between Vildagliptin + Metformin and Pioglitazone + Metformin Groups
NCT01882907 (6) [back to overview]	the Numbers of Participants With Adverse Events Between Vildagliptin + Metformin and Pioglitazone + Metformin Groups
NCT02002221 (5) [back to overview]	Number of Participants With Adverse Events, Serious Adverse Events and Death
NCT02002221 (5) [back to overview]	Change From Baseline in Fasting Plasma Glucose (FPG) at 12 Weeks
NCT02002221 (5) [back to overview]	Change From Baseline in Glycosylated Hemoglobin (HbA1c) at 12 Weeks Between Treatment Groups
NCT02002221 (5) [back to overview]	Number of Participants With Incidence of Hypoglycemia and Severe Hypoglycemia
NCT02002221 (5) [back to overview]	Percentage of Patients Meeting Responder Rates in HbA1c
NCT02007278 (8) [back to overview]	Change in HbA1c at Week 12 of Treatment in Comparison to HbA1c at Baseline
NCT02007278 (8) [back to overview]	Glycemic Variability Measured by Continuous Overlapping Net Glycemic Action (CONGA)
NCT02007278 (8) [back to overview]	Glycemic Variability Measured by Mean Amplitude of Glucose Excursions (MAGE)
NCT02007278 (8) [back to overview]	Glycemic Variability Measured by Total Standard Deviation (TSD)
NCT02007278 (8) [back to overview]	Mean Amplitude of Glycemic Excursions (MAGE) for Patients With Hypoglycemia Incidence After 12 Weeks of Treatment
NCT02007278 (8) [back to overview]	Number of Patients With Any Adverse Events, Serious Adverse Events and Death
NCT02007278 (8) [back to overview]	Number of Patients With Incidence of Hypoglycemia
NCT02007278 (8) [back to overview]	Percentage of Patients Who Achieved a Decrease Equal to or Greater Than 0.3% in Value of HbA1c at Week 12
NCT02475070 (2) [back to overview]	Incretin Hormones
NCT02475070 (2) [back to overview]	Glucagon Response to Meal

Full Epithelialization of the Wound

"Biopsy is performed from the periphery of the ulcer, before and after treatment with vildagliptin, in order to evaluate the above referred outcome.~Optic microscopy is used to evaluate the epithelialization of the wound." (NCT01472432)
Timeframe: 3 months of treatment with vildagliptin

Intervention	participants (Number)
Placebo	16
Vildagliptin	8

Intervention	Rate (%) (Number)
	Weeks 13-52	Year 2	Year 3	Year 4	Year 5	> Year 5
Placebo + Metformin	19.97	34.67	48.31	59.29	66.57	74.39
Vilda 50mg Bid + Metformin	7.81	17.79	31.24	39.84	46.41	52.67

Intervention	Percentage of Participants (Number)
	On-treatment Adverse Event (AEs)	On-treatment Serious Adverse Event (SAEs)	On-treatment Deaths
Placebo + Metformin	83.2	18.3	0.9
Vilda 50mg Bid + Metformin	83.5	16.6	1.3

Intervention	Rate (%) (Mean)
	From Week 13 to end of Period 1	From Week 13 to end of Period 2	From Week 13 to end of study
Placebo + Metformin	0.41	-0.99	-1.01
Vilda 50mg Bid + Metformin	-4.61	-6.07	-6.39

Intervention	percentage of participants (Number)
	HbA1c ≤ 6.5% Week 12	HbA1c ≤ 6.5% Week 24	HbA1c ≤ 7.0% Week 12	HbA1c ≤ 7.0% Week 24
Vildagliptin Plus Metformin (SPC)	64.1	66.7	92.3	87.2

Intervention	nM*hr (Geometric Mean)
Sitagliptin 100 mg	7070
Saxagliptin 5 mg	370
Vildagliptin 50 mg	3100
Vildagliptin 50 mg BID	6600

Intervention	Percent inhibition (Least Squares Mean)
Sitagliptin 100 mg	91.73
Saxagliptin 5 mg	73.50
Vildagliptin 50 mg	28.88
Vildagliptin 50 mg BID	90.63
Placebo	3.49

Intervention	nM (Geometric Mean)
Sitagliptin 100 mg	724
Saxagliptin 5 mg	88.8
Vildagliptin 50 mg	586
Vildagliptin 50 mg BID	759

Intervention	number of hypoglycemic events (Number)
	continuous glucose monitoring (CGM)	self-monitored blood glucose (SMBG)
Sitagliptin	37	13
Vitagliptin	69	29

Intervention	number of occurrence (Mean)
	# any VES Per.1 n=23, 25	# any VES Per.2 n=25, 23	# couplets VES Per.1 n=23, 25	# couplets VES Per.2 n=25, 23	# salves VES Per.1 n=23, 25	# salves VES Per.2 n=25, 23
Sitagliptin	2786.7	1060.2	115.0	2.4	15.8	0.9
Vitagliptin	879.7	4389.9	12.8	6.7	1.0	0.8

Intervention	participants (Number)
	Patients with hypoglycemia (n=21,17)	Patients without hypoglycemia (n=28,32)
Sitagliptin	10	24
Vitagliptin	14	19

Intervention	Patients (Number)
	Any adverse events	Serious adverse events	Death	Patients discontinued due to any AE/SAE
LAF237 (Vildagliptin) 50mg Once Daily (QD)	15	2	0	4
LAF237 (Vildagliptin) 50mg Twice Daily (BID)	14	2	0	4

Intervention	percentage of Glycosylated Hemoglobin (Mean)
LAF237 (Vildagliptin) 50mg Once Daily (QD)	-0.8
LAF237 (Vildagliptin) 50mg Twice Daily (BID)	-1.0

Intervention	Percentage of overall drug compliance (Mean)
LAF237 (Vildagliptin) 50mg Once Daily (QD)	96.90
LAF237 (Vildagliptin) 50mg Twice Daily (BID)	97.48

Intervention	mmol/L (Least Squares Mean)
	3 month from baseline	6 month from baseline	9 month from baseline	12 month from baseline
LAF237 (Vildagliptin) 50mg Once Daily (QD)	-0.9	-1.2	-1.1	-0.9
LAF237 (Vildagliptin) 50mg Twice Daily (BID)	-1.3	-0.9	-1.0	-0.8

Intervention	Percentage of patients (Number)
	At Month 3	At Month 6	At Month 9	At Month 12
LAF237 (Vildagliptin) 50mg Once Daily (QD)	33.3	39.2	45.1	49.0
LAF237 (Vildagliptin) 50mg Twice Daily (BID)	47.5	45.6	47.4	40.0

Intervention	percentage (Median)
	V2 (4 month)	V4 (12 month)
Glibenclamide & Metformin	6.8	7.1
Vildagliptin & Metformin	6.8	7.0

Intervention	HbA1c percent (Mean)
	baseline	week 24
Metformin/Vildagliptin + Basal Insulin	8.2	7.2
SU+Metformin + Basal Insulin	8.2	7.4

Intervention	percent of participants (Number)
Metformin/Vildagliptin + Basal Insulin	44.4
SU+Metformin + Basal Insulin	47.4

Intervention	(U/d) (Mean)
Metformin/Vildagliptin + Basal Insulin	33.0
SU+Metformin + Basal Insulin	19.8

Intervention	kg (Mean)
Metformin/Vildagliptin + Basal Insulin	-0.3
SU+Metformin + Basal Insulin	1.4

vildagliptin

Cross-References

Synonyms (74)

Research Excerpts

Overview

Effects

Actions

Treatment

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (17)

Inhibition Measurements

Activation Measurements

Biological Processes (98)

Molecular Functions (62)

Ceullar Components (52)

Bioassays (217)

Research

Studies (774)

Study Types

Clinical Trials (170)

Trial Overview

Trial Outcomes

Full Epithelialization of the Wound

Capillary Density

HIF-1α

VEGF

Time to Initial Treatment Failure

Rate of Loss in Glycemic Control During Period 1

Rate of Loss in Glycemic Control in Fasting Plasma Glucose (FPG) During Period 1

Rate of Loss in Glycemic Control in Fasting Plasma Glucose (FPG) Over Time During Period 2

Rate of Loss in Glycemic Control in HbA1c Over Time During Period 2

Percentage of Participants With Adverse Events, Serious Adverse Events and Death

Rate of Change in Insulin Sensitivity From Baseline to End of Study

Rate of Loss of Beta Cell Function From Baseline to End of Study

HbA1C At 12 Weeks

24 Hour Weighted Mean Glucose (WMG) At 2 Weeks

Hemoglobin A1C (HbA1C) At 2 Weeks

Mean Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 12

Mean Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 24

Mean Change From Baseline in Mean Amplitude of Glycemic Excursions (MAGE) Detected by Continuous Glucose Monitoring System (CGMS) After 24-week

Mean Change From Baseline in Fasting Plasma Glucose(FPG) at Week 12 and 24

Mean Change From Baseline in Postprandial Plasma Glucose(PPG) at Week 12 and 24

The Percentage of Patients Achieving the Two Glycemic Goals After 12- and 24-week Treatment

Pharmacokinetic Analysis: Area Under the Curve 0-24 Hours (AUC 0-24hr)

Percent Inhibition of Dipeptidyl Peptidase IV (DPP-4) Activity at Trough

Pharmacokinetic Analysis: Area Under the Curve 0-12 Hours (AUC 0-12hr) for Vildagliptin 50 mg BID

Pharmacokinetic Analysis: Peak Plasma Drug Concentration (Cmax)

Pharmacokinetic Analysis: Time to the Peak Plasma Drug Concentration (Tmax)

Change From Baseline of Inflammatory Biomarkers Interleukin 6 (IL-6) After 8 Weeks of Treatment in Period 1 & Period 2

Change From Baseline of Inflammatory Biomarkers High Sensitivity C-reactive Protein (hsCRP) After 8 Weeks of Treatment in Period 1 & Period 2

Number of Severe Hypoglycemic Events During Vildagliptin Treatment Compared to Sitagliptin Treatment After 8 Weeks of Treatment in Period 1 and Period 2

Glucose Fluctuations During the Day Under Vildagliptin Treatment Compared to Sitagliptin Treatment on Day 2 After 8 Weeks of Treatment Period 1 & Period 2

Hypoglycemic Profile of Vildagliptin Compared to Sitagliptin Over 4 Days After 8 Weeks of Treatment in Period 1 & 2

Mean Amplitudes of Hypoglycemic Events (mmol/L) Measured With Continuous Glucose Monitoring (CGM) Over 4 Days After 8 Weeks of Treatment for Period 1 & Period 2

Mean Duration of Hypoglycemic Events (Min.) Measured With Continuous Glucose Monitoring (CGM) Over 4 Days After 8 Weeks of Treatment for Period 1 & Period 2

Percentage Change From Baseline of Pro-insulin/C-peptide Ratios After 8 Weeks of Treatment Period 1 & Period 2

Number of Hypoglycemic Events During Vildagliptin Treatment Compared to Sitagliptin Treatment.

Number of Occurrence of Pre-defined ECG Findings During 4 Days of Continuous ECG Monitoring at Baseline and in the 8th Week of Periods 1 and 2

Number of Participants With ECG Abnormalities Depending on Hypoglycemic Events After 8 Weeks of Treatment Period 1 & Period 2

Number of Patients With Adverse Events, Serious Adverse Events and Death as an Assessment of Overall Safety and Tolerability

Change of Glycosylated Hemoglobin A1c (HbA1c) From Baseline to Month 12

Percentage of Overall Drug Compliance in 12 Months

Change in Fasting Plasma Glucose (FPG) From Baseline to Month 3, 6, 9 and 12 (Based on MMRM Analysis)

Percentage of Patients Achieving Good Glycemic Control

Change of Glycosylated Hemoglobin A1c (HbA1c) From Baseline to Month 3, 6, 9 and 12 (Based on MMRM Analysis)

Absolute Change in HbA1C Compared to Baseline

Absolute Change in the Endothelial Progenitor Cell (EPC) Number

Change From Baseline in HbA1c to Week 24 in Both Treatment Arms

Percentage of Patients Reaching Their Glycemic Target Without Hypoglycemic Events

Mean Daily Insulin Dose at Week 24

Change From Baseline in Body Weight in Both Treatment Arms

Percent of Participants That Reach Therapeutic Goal (HbA1c ≤ 7%) at Week 24 Without Any Hypoglycaemic Episode (Symptomatic or Not) and Without Any Weight Gain (Variation ≥3% Compared to Baseline)

Percentage of Patients Who Reported at Least One Symptomatic Hypoglycemic Event During the 24 Week Randomized Period in Both Treatment Arms

Percentage of Patients With Severe and Confirmed Hypoglycemic Events

the Mean Changes of Body Weight From Baseline Between Vildagliptin + Metformin and Pioglitazone + Metformin Groups

Intervention	percent of participants (Number)
Metformin/Vildagliptin + Basal Insulin	27.8
SU+Metformin + Basal Insulin	21.1

Intervention	percent of participants (Number)
Metformin/Vildagliptin + Basal Insulin	22.2
SU+Metformin + Basal Insulin	45.0

Intervention	mg/dL (Mean)
	FBG levels difference	PPG levels difference
Pioglitazone	-15.04	-38.19
Vildagliptin	-20.41	-60.23

Intervention	mcU/mL*mmol/L (Mean)
	Insulin difference	C-peptide difference	HOMA-IR difference	HOMA-beta difference
Pioglitazone	-8.21	-0.24	-3.33	-24.26
Vildagliptin	0.36	0.07	-0.06	9.77

Intervention	mg/dL (Mean)
	Triglyceride	Total cholesterol	LDL	HDL	Non-HDL cholesterol
Pioglitazone	-4.79	9.60	5.38	3.69	5.79
Vildagliptin	-9.22	-6.45	-6.03	-0.34	-8.39

Intervention	participants (Number)
	Number of incidence	Number of adverse events
Pioglitazone	25	37
Vildagliptin	27	48

Intervention	Participants (Number)
	at least one hypoglycemic event	grade 2 hypoglycemic events	suspected grade 2 hypoglycemic events
Placebo	1	0	0
Vildagliptin (LAF237)	5	0	0

Intervention	percentage of patients (Number)
	At least one criterion met (n = 78, 78)	Criterion 1 (n= 77, 78)	Criterion 2 (n= 76, 77)	Criterion 3 (n= 42, 37)	Criterion 4 (n=78, 78)	Criterion 5 (n= 78, 78)
Placebo	21	2	3	3	5	20
Vildagliptin (LAF237)	67	23	38	33	38	62

Intervention	Patients (Number)
	Any adverse events (serious and non-serious)	Serious Adverse Events	Death
Glimepiride and Metformin	13	1	0
Vildagliptin and Metformin	9	0	0

Intervention	percentage of patients (Number)
Vildagliptin and Metformin	100.0
Glimepiride and Metformin	100.0