Investigation of the pharmacokinetics and metabolic fate of Fasiglifam (TAK-875) in male and female rats following oral and intravenous administration

References

• Bradshaw PR, Athersuch TJ, Stachulski AV, Wilson ID. 2020. Acyl glucuronide reactivity in perspective. Drug Discov Today. 25(9):1639–1650.
   PubMed Web of Science ®Google Scholar
• Darnell M, Weidolf L. 2013. Metabolism of xenobiotic carboxylic acids: focus on coenzyme A conjugation, reactivity, and interference with lipid metabolism. Chem Res Toxicol. 26(8):1139–1155.
   PubMed Web of Science ®Google Scholar
• Dickie AP, Wilson CE, Schreiter K, Wehr R, Wilson EM, Bial J, Scheer N, Wilson ID, Riley RJ. 2017. The pharmacokinetics and metabolism of lumiracoxib in chimeric humanized and murinized FRG mice. Biochem Pharmacol. 135:139–150.
   PubMed Web of Science ®Google Scholar
• Ekdahl A, Weidolf L, Baginski M, Morikawa Y, Thompson RA, Wilson ID. 2018. The metabolic fate of fenclozic acid in chimeric mice with a humanized liver. Arch Toxicol. 92(9):2819–2828. 2018,
   PubMed Web of Science ®Google Scholar
• Giles K, Ujma J, Wildgoose J, Pringle S, Richardson K, Langridge D, Green M. 2019. A cyclic ion mobility-mass spectrometry system. Anal. Chem. 91(13):8564–8573.
   PubMed Web of Science ®Google Scholar
• Grillo MP, Ma J, Teffera Y, Waldon DJ. 2008. A novel bioactivation pathway for 2-[2-(2,6-dichlorophenyl)aminophenyl]ethanoic acid (diclofenac) initiated by cytochrome P450-mediated oxidative decarboxylation. Drug Metab Dispos. 36(9):1740–1744.
   PubMed Web of Science ®Google Scholar
• Iwamura A, Nakajima M, Oda S, Yokoi T. 2017. Toxicological potential of acyl glucuronides and its assessment. Drug Metab Pharmacokinetics. 32(1):2–11.
   PubMed Web of Science ®Google Scholar
• Johnson CH, Karlsson E, Sarda S, Iddon L, Iqbal M, Meng X, Harding JR, Stachulski AV, Nicholson JK, Wilson ID, et al. 2010. Integrated HPLC-MS and 1 H-NMR spectroscopic studies on acyl migration reaction kinetics of model drug ester glucuronides. Xenobiotica. 40(1):9–23.
   PubMed Web of Science ®Google Scholar
• Kaku K. 2013. Fasiglifam as a new potential treatment option for patients with type 2 diabetes. Expert Opin Pharmacother. 14(18):2591–2600.
   PubMed Web of Science ®Google Scholar
• Kaku K, Enya K, Nakaya R, Ohira T, Matsuno R. 2015. Efficacy and safety of fasiglifam (TAK-875), a G protein-coupled receptor 40 agonist, in Japanese patients with type 2 diabetes inadequately controlled by diet and exercise: a randomized, double-blind, placebo-controlled, phase III trial. Diabetes Obes Metab. 17(7):675–681.
   PubMed Web of Science ®Google Scholar
• Kaku K, Enya K, Nakaya R, Ohira T, Matsuno R. 2016. Long-term safety and efficacy of fasiglifam (TAK-875), a G-protein-coupled receptor 40 agonist, as monotherapy and combination therapy in Japanese patients with type 2 diabetes: a 52-week open-label phase III study. Diabetes Obes Metab. 18(9):925–929.
   PubMed Web of Science ®Google Scholar
• Kogame A, Lee R, Pan L, Sudo M, Nonaka M, Moriya Y, Higuchi T, Tagawa Y. 2019a. Disposition and metabolism of the G protein coupled receptor 40 agonist TAK-875 (Fasiglifam) in rats, dogs, and humans. Xenobiotica. 49(4):433–445.
   PubMed Web of Science ®Google Scholar
• Kogame A, Moriya Y, Mori I, Pan L, Morohashi A, Ebihara T, Fukui H, Tagawa Y, Benet LZ. 2019b. Characterization of fasiglifam-related liver toxicity in dogs. Drug Metab Dispos. 47(5):525–534.
   PubMed Web of Science ®Google Scholar
• Li X, Zhong K, Guo Z, Zhong D, Chen X. 2015. Fasiglifam (TAK-875) inhibits hepatobiliary transporters: a possible factor contributing to fasiglifam-induced liver injury. Drug Metab Dispos. 43(11):1751–1759.
   PubMed Web of Science ®Google Scholar
• Mortishire-Smith RJ, Castro-Perez JM, Yu K, Shockcor JP, Goshawk J, Hartshorn MJ, Hill A. 2009. Generic dealkylation: a tool for increasing the hit-rate ofmetabolite rationalization, and automatic customizationof mass defect filters. Rapid Commun Mass Spectrom. 23(7):939–948.
   PubMed Web of Science ®Google Scholar
• Naik H, Vakilynejad M, Wu J, Viswanathan P, Dote N, Higuchi T, Leifke E. 2012. Safety, tolerability, pharmacokinetics, and pharmacodynamic properties of the GPR40 agonist TAK-875: results from a double-blind, placebo-controlled single oral dose rising study in healthy volunteers. J Clin Pharmacol. 52(7):1007–1016.
   PubMed Web of Science ®Google Scholar
• Otieno MA, Snoeys J, Lam W, Ghosh A, Player MR, Pocai A, Salter R, Simic D, Skaggs H, Singh B, et al. 2018. Fasiglifam (TAK-875): mechanistic investigation and retrospective identification of hazards for drug induced liver injury. Toxicological Sciences. 163(2):374–384.
   PubMed Web of Science ®Google Scholar
• Sarda S, Page C, Pickup K, Schulz-Utermoehl T, Wilson I. 2012. Diclofenac metabolism in the mouse: novel in vivo metabolites identified by high performance liquid chromatography coupled to linear ion trap mass spectrometry. Xenobiotica. 42(2):179–194.
   PubMed Web of Science ®Google Scholar
• Sawamura R, Okudaira N, Watanabe K, Murai T, Kobayashi Y, Tachibana M, Ohnuki T, Masuda K, Honma H, Kurihara A, et al. 2010. Predictability of idiosyncratic drug toxicity risk for carboxylic acid-containing drugs based on the chemical stability of acyl glucuronide. Drug Metab Dispos. 38(10):1857–1864.
   PubMed Web of Science ®Google Scholar
• Thompson RA, Isin EM, Li Y, Weidolf L, Page K, Wilson I, Swallow S, Middleton B, Stahl S, Foster AJ, et al. 2012. In vitro approach to assess the potential for risk of idiosyncratic adverse reactions caused by candidate drugs. Chem Res Toxicol. 25(8):1616–1632.
   PubMed Web of Science ®Google Scholar
• Wolenski FS, Zhu AZX, Johnson M, Yu S, Moriya Y, Ebihara T, Csizmadia V, Grieves J, Paton M, Liao M, et al. 2017. Fasiglifam (TAK-875) alters bile acid homeostasis in rats and dogs: a potential cause of drug induced liver injury. Toxicol Sci. 157:50–61.
   PubMed Web of Science ®Google Scholar
• Zhang Y, Huo M, Zhou J, Xie S. 2010. PKSolver: An add-in program for pharmacokinetic and pharmacodynamic data analysis in Microsoft Excel. Comput Methods Programs Biomed. 99(3):306–314.
   PubMed Web of Science ®Google Scholar