Metabolism and disposition of the dipeptidyl peptidase IV inhibitor teneligliptin in humans

Xenobiotica

Volumn 44, Issue 3, 2014, Pages 242-253

  Nakamaru, Yoshinobu ^a   Hayashi, Yoshiharu ^a   Ikegawa, Ruriko ^a   Kinoshita, Shuji ^a   Madera, Begonya Perez ^b   Gunput, Dave ^b   Kawaguchi, Atsuhiro ^b   Davies, Martin ^b   Mair, Stuart ^c   Yamazaki, Hiroshi ^d   Kume, Toshiyuki ^a   Suzuki, Masayuki ^a  

^a MITSUBISHI TANABE PHARMA CORPORATION   (Japan)

^b Mitsubishi Pharma Europe Ltd   (United Kingdom)

^c Quotient Clinical Limited   (United Kingdom)

^d SHOWA PHARMACEUTICAL UNIVERSITY   (Japan)

Author keywords

DPP 4 inhibitor; Excretion; Human; Mass balance; Metabolism; Teneligliptin

Indexed keywords

AMINE OXIDASE (FLAVIN CONTAINING) ISOENZYME B; CARBON 14; CYTOCHROME P450 3A4; DIPEPTIDYL PEPTIDASE IV INHIBITOR; DRUG METABOLITE; PROTEIN FMO3; TENELIGLIPTIN; THIAZOLIDINE DERIVATIVE; UNCLASSIFIED DRUG;

AREA UNDER THE CURVE; ARTICLE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG DISPOSITION; DRUG ELIMINATION; DRUG EXCRETION; DRUG HALF LIFE; DRUG METABOLISM; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; PHASE 1 CLINICAL TRIAL; RADIOACTIVITY; URINARY EXCRETION;

ABSORPTION; ADULT; AREA UNDER CURVE; CARBON RADIOISOTOPES; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CYTOCHROME P-450 CYP3A; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; FECES; HUMANS; MALE; MASS SPECTROMETRY; MIDDLE AGED; MODELS, BIOLOGICAL; MOLECULAR STRUCTURE; OXYGENASES; PYRAZOLES; SCINTILLATION COUNTING; THIAZOLIDINES; TIME FACTORS;

EID: 84893632010     PISSN: 00498254     EISSN: 13665928     Source Type: Journal    
DOI: 10.3109/00498254.2013.816891     Document Type: Article

References (20)

1. Bergman AJ, Cote J, Yi B, et al. (2007). Effect of renal insufficiency on the pharmacokinetics of sitagliptin, a dipeptidyl peptidase-4 inhibitor. Diabetes Care 30:1862-4.
2. Boulton DW, Li L, Frevert EU, et al. (2011). Influence of renal or hepatic impairment on the pharmacokinetics of saxagliptin. Clin Pharmacokinet 50:253-65.
3. Buteau J, Foisy S, Rhodes CJ, et al. (2001). Protein kinase Czeta activation mediates glucagon-like peptide-1-induced pancreatic betacell proliferation. Diabetes 50:2237-43.
4. Deacon CF, Nauck MA, Toft-Nielsen M, et al. (1995). Both subcutaneously and intravenously administered glucagon-like peptide I are rapidly degraded from the NH2-terminus in type II diabetic patients and in healthy subjects. Diabetes 44:1126-31.
5. Edwards CM, Todd JF, Mahmoudi M, et al. (1999). Glucagon-like peptide 1 has a physiological role in the control of postprandial glucose in humans: studies with the antagonist exendin 9-39. Diabetes 48:86-93.
6. Eto T, Inoue S, Kadowaki T. (2012). Effects of once-daily teneligliptin on 24-h blood glucose control and safety in Japanese patients with type 2 diabetes mellitus: a 4-week, randomized, double-blind, placebo-controlled trial. Diabetes Obes Metab 14:1040-6.
7. Flint A, Raben A, Astrup A, Holst JJ. (1998). Glucagon-like peptide-1 promotes satiety and suppresses energy intake in humans. J Clin Invest 101:515-20.
8. Guo Z, Raeissi S, White RB, Stevens JC. (1997). Orphenadrine and methimazole inhibit multiple cytochrome P450 enzymes in human liver microsomes. Drug Metab Dispos 25:390-3.
9. Halabi A, Maatouk H, Siegler KE, et al. (2013). Pharmacokinetics of teneligliptin in subjects with renal impairment. Clin Pharmacol Drug Develop. [Epub ahead of print]. DOI:10.1002/cpdd.29. Published online: 14 May 2013.
10. Holst JJ, Deacon CF. (1998). Inhibition of the activity of dipeptidylpeptidase IV as a treatment for type 2 diabetes. Diabetes 47:1663-70.
11. Hop CE, Wang Z, Chen Q, Kwei G. (1998). Plasma-pooling methods to increase throughput for in vivo pharmacokinetic screening. J Pharm Sci 87:901-3.
12. Krause RJ, Lash LH, Elfarra AA. (2003). Human kidney flavincontaining monooxygenases and their potential roles in cysteine S-conjugate metabolism and nephrotoxicity. J Pharmacol Exp Ther 304:185-91.
13. Kreymann B, Williams G, Ghatei MA, Bloom SR. (1987). Glucagon-like peptide-1 7-36: a physiological incretin in man. Lancet 2:1300-4.
14. Miyaoka T, Isono Y, Setani K, et al. (2007). Bioanalysis works in the IAA AMS facility: comparison of AMS analytical method with LSC method in human mass balance study. Nuclear Inst Methods Phys Res 259:779-85.
15. Overby LH, Carver GC, Philpot RM. (1997). Quantitation and kinetic properties of hepatic microsomal and recombinant flavin-containing monooxygenases 3 and 5 from humans. Chem Biol Interact 106: 29-45.
16. Scheen AJ. (2010). Dipeptidylpeptitase-4 inhibitors (gliptins). Focus on drug-drug interactions. Clin Pharmacokinet 49:573-88.
17. Vincent SH, Reed JR, Bergman AJ, et al. (2007). Metabolism and excretion of the dipeptidyl peptidase 4 inhibitor [14C]sitagliptin in humans. Drug Metab Dispos 35:533-8.
18. Wettergren A, Schjoldager B, Mortensen PE, et al. (1993). Truncated GLP-1 (proglucagon 78-107-amide) inhibits gastric and pancreatic functions in man. Dig Dis Sci 38:665-73.
19. Xu G, Stoffers DA, Habener JF, Bonner-Weir S. (1999). Exendin-4 stimulates both beta-cell replication and neogenesis, resulting in increased beta-cell mass and improved glucose tolerance in diabetic rats. Diabetes 48:2270-6.
20. Zhou D, Zhang M, Ye X, et al. (2011). In vitro metabolism of a7 neuronal nicotinic receptor agonist AZD0328 and enzyme identification for its N-oxide metabolite. Xenobiotica 41:232-42.