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Xenobiotica
the fate of foreign compounds in biological systems
Volume 49, 2019 - Issue 4
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Clinical Pharmacokinetics and Metabolism

Disposition and metabolism of the G protein-coupled receptor 40 agonist TAK-875 (fasiglifam) in rats, dogs, and humans

Akifumi KogameDrug Metabolism and Pharmacokinetics Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited, Fujisawa, Kanagawa, Japan; Correspondence[email protected]
,
Ronald LeeTakeda Development Center Americas, Inc., Deerfield, IL, USA
,
Liping PanTakeda Development Center Americas, Inc., Deerfield, IL, USA
,
Miyako SudoDrug Metabolism and Pharmacokinetics Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited, Fujisawa, Kanagawa, Japan;
,
Masami NonakaDrug Metabolism and Pharmacokinetics Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited, Fujisawa, Kanagawa, Japan;
,
Yuu MoriyaDrug Metabolism and Pharmacokinetics Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited, Fujisawa, Kanagawa, Japan;
,
Tomoaki HiguchiDrug Metabolism and Pharmacokinetics Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited, Fujisawa, Kanagawa, Japan;
&
Yoshihiko TagawaDrug Metabolism and Pharmacokinetics Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited, Fujisawa, Kanagawa, Japan;
show all
Pages 433-445 | Received 28 Dec 2017, Accepted 13 Mar 2018, Published online: 05 Apr 2018

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Qiang Ren, Yiqing Fan, Lixin Yang, Mayu Shan, Wei Shi & Hai Qian. (2023) An updated patent review of GPR40/ FFAR1 modulators (2020 – present). Expert Opinion on Therapeutic Patents 33:9, pages 565-577.
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Billy J. Molloy, Adam King, Lee A. Gethings, Robert S. Plumb, Russell J. Mortishire-Smith & Ian D. Wilson. (2023) Investigation of the pharmacokinetics and metabolic fate of Fasiglifam (TAK-875) in male and female rats following oral and intravenous administration. Xenobiotica 53:2, pages 93-105.
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Lars Weidolf & Ian Wilson. (2023) Minimizing the DILI potential of carboxylic acid-containing drugs: a perspective. Medicinal Chemistry Research.
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Nikunj Tanna, Robert S. Plumb, Billy J. Molloy, Paul D. Rainville & Ian D. Wilson. (2023) Enhanced chromatographic efficiency obtained with vacuum jacketed columns facilitates the rapid UHPLC/MS/MS-based analysis of fasiglifam in rat plasma. Talanta 254, pages 124089.
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Robert S. Jones, Christian Leung, Jae H. Chang, Suzanne Brown, Ning Liu, Zhengyin Yan, Jane R. Kenny & Fabio Broccatelli. (2022) Application of Empirical Scalars To Enable Early Prediction of Human Hepatic Clearance Using In Vitro-In Vivo Extrapolation in Drug Discovery: An Evaluation of 173 Drugs. Drug Metabolism and Disposition 50:8, pages 1053-1063.
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Erkka Järvinen, Feng Deng, Wilma Kiander, Alli Sinokki, Heidi Kidron & Noora Sjöstedt. (2022) The Role of Uptake and Efflux Transporters in the Disposition of Glucuronide and Sulfate Conjugates. Frontiers in Pharmacology 12.
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Katarzyna Bazydlo-Guzenda, Pawel Buda, Mateusz Mach, Jerzy Pieczykolan, Izabela Kozlowska, Michal Janiszewski, Ewa Drzazga, Jakub Dominowski, Hubert Ziolkowski, Maciej Wieczorek & Shayne Cox Gad. (2021) Evaluation of the hepatotoxicity of the novel GPR40 (FFAR1) agonist CPL207280 in the rat and monkey. PLOS ONE 16:9, pages e0257477.
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Paolo Governa, Maria Cristina Caroleo, Gabriele Carullo, Francesca Aiello, Erika Cione & Fabrizio Manetti. (2021) FFAR1/GPR40: One target, different binding sites, many agonists, no drugs, but a continuous and unprofitable tug-of-war between ligand lipophilicity, activity, and toxicity. Bioorganic & Medicinal Chemistry Letters 41, pages 127969.
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John O. Miners, Andrew Rowland, Jonathan J. Novak, Kimberly Lapham & Theunis C. Goosen. (2021) Evidence-based strategies for the characterisation of human drug and chemical glucuronidation in vitro and UDP-glucuronosyltransferase reaction phenotyping. Pharmacology & Therapeutics 218, pages 107689.
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Amit S. Kalgutkar. (2019) Designing around Structural Alerts in Drug Discovery. Journal of Medicinal Chemistry 63:12, pages 6276-6302.
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Hikaru Ueno, Ryo Ito, Shin-ichi Abe, Mitsugi Ookawara, Hirohisa Miyashita, Hitomi Ogino, Yasufumi Miyamoto, Tomoki Yoshihara, Akihiro Kobayashi, Yoshiyuki Tsujihata, Koji Takeuchi, Masanori Watanabe, Yukio Yamada, Tsuyoshi Maekawa, Nobuhiro Nishigaki & Yusuke Moritoh. (2019) SCO-267, a GPR40 Full Agonist, Improves Glycemic and Body Weight Control in Rat Models of Diabetes and Obesity. Journal of Pharmacology and Experimental Therapeutics 370:2, pages 172-181.
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Timothy Ackerson, Alexander Amberg, Jens Atzrodt, Catherine Arabeyre, Elisabeth Defossa, Martina Dorau, Angela Dudda, Jacquelyn Dwyer, Wolfgang Holla, Thomas Kissner, Markus Kohlmann, Ulrich Kürzel, József Pánczél, Shibani Rajanna, Jens Riedel, Friedemann Schmidt, Kerstin Wäse, Dietmar Weitz & Volker Derdau. (2019) Mechanistic investigations of the liver toxicity of the free fatty acid receptor 1 agonist fasiglifam (TAK875) and its primary metabolites. Journal of Biochemical and Molecular Toxicology 33:8.
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Yutai Li, Raymond Evers, Michael J Hafey, Kyeongmi Cheon, Hong Duong, Donna Lynch, Lisa LaFranco-Scheuch, Stephen Pacchione, Alex M Tamburino, Keith Q Tanis, Kristin Geddes, Daniel Holder, Nanyan Rena Zhang, Wen Kang, Raymond J Gonzalez, Alema Galijatovic-Idrizbegovic, Kara M Pearson, Jose A Lebron, Warren E Glaab & Frank D Sistare. (2019) Use of a Bile Salt Export Pump Knockdown Rat Susceptibility Model to Interrogate Mechanism of Drug-Induced Liver Toxicity. Toxicological Sciences 170:1, pages 180-198.
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Jin-Qi Li, Jie Li, Jia-Feng Wang, Shu-han Zhang, Dan He, Rong-Sheng Yong & Shu-Ya She. (2018) In vitro and in vivo metabolic profiles of fasiglifam using ultrahigh-performance liquid chromatography combined with Q-Exactive Orbitrap tandem mass spectrometry . Rapid Communications in Mass Spectrometry 32:16, pages 1387-1395.
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