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Volumn 157, Issue 1, 2017, Pages 50-61

Fasiglifam (TAK-875) alters bile acid homeostasis in rats and dogs: A potential cause of drug induced liver injury

Author keywords

Bile acid inhibition; Biliary excretion; Biomarkers; Drug induced liver injury

Indexed keywords

ALPHA MURICHOLIC ACID; BETA MURICHOLIC ACID; BILE ACID; CHENODEOXYCHOLIC ACID; CHOLIC ACID; DEOXYCHOLIC ACID; FASIGLIFAM; GLYCOCHENODEOXYCHOLIC ACID; GLYCOCHOLIC ACID; GLYCODEOXYCHOLIC ACID; GLYCOLITHOCHOLIC ACID; GLYCOURSODEOXYCHOLIC ACID; HYODEOXYCHOLIC ACID; LITHOCHOLIC ACID; TAURO ALPHA MURICHOLIC ACID; TAURO BETA MURICHOLIC ACID; TAUROCHENODEOXYCHOLIC ACID; TAUROCHOLIC ACID; TAURODEOXYCHOLIC ACID; TAUROHYODEOXYCHOLIC ACID; TAUROLITHOCHOLIC ACID; TAUROURSODEOXYCHOLIC ACID; UNCLASSIFIED DRUG; URSODEOXYCHOLIC ACID; BENZOFURAN DERIVATIVE; SULFONE; TAK-875;

EID: 85020110686     PISSN: 10966080     EISSN: 10960929     Source Type: Journal    
DOI: 10.1093/toxsci/kfx018     Document Type: Article
Times cited : (48)

References (47)
  • 1
    • 84906937883 scopus 로고    scopus 로고
    • Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump
    • Aleo, M. D., Luo, Y., Swiss, R., Bonin, P. D., Potter, D. M., and Will, Y. (2014). Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. Hepatology 60, 1015-1022
    • (2014) Hepatology , vol.60 , pp. 1015-1022
    • Aleo, M.D.1    Luo, Y.2    Swiss, R.3    Bonin, P.D.4    Potter, D.M.5    Will, Y.6
  • 2
    • 34548572892 scopus 로고    scopus 로고
    • Bile acid transporters: Structure, function, regulation and pathophysiological implications
    • Alrefai, W. A., and Gill, R. K. (2007). Bile acid transporters: Structure, function, regulation and pathophysiological implications. Pharm. Res. 24, 1803-1823
    • (2007) Pharm. Res , vol.24 , pp. 1803-1823
    • Alrefai, W.A.1    Gill, R.K.2
  • 3
    • 0022656312 scopus 로고
    • Bile acid-induced liver toxicity: Relation to the hydrophobic-hydrophilic balance of bile acids
    • Attili, A. F., Angelico, M., Cantafora, A., Alvaro, D., and Capocaccia, L. (1986). Bile acid-induced liver toxicity: Relation to the hydrophobic-hydrophilic balance of bile acids. Med. Hypotheses 19, 57-69
    • (1986) Med. Hypotheses , vol.19 , pp. 57-69
    • Attili, A.F.1    Angelico, M.2    Cantafora, A.3    Alvaro, D.4    Capocaccia, L.5
  • 4
    • 84859625938 scopus 로고    scopus 로고
    • TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: A phase 2, randomised, double-blind, placebo-controlled trial
    • Burant, C. F., Viswanathan, P., Marcinak, J., Cao, C., Vakilynejad, M., Xie, B., and Leifke, E. (2012). TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: A phase 2, randomised, double-blind, placebo-controlled trial. Lancet 379, 1403-1411
    • (2012) Lancet , vol.379 , pp. 1403-1411
    • Burant, C.F.1    Viswanathan, P.2    Marcinak, J.3    Cao, C.4    Vakilynejad, M.5    Xie, B.6    Leifke, E.7
  • 5
    • 70349430938 scopus 로고    scopus 로고
    • Bile acids: Regulation of synthesis
    • Chiang, J. Y. (2009). Bile acids: Regulation of synthesis. J. Lipid Res. 50, 1955-1966
    • (2009) J. Lipid Res , vol.50 , pp. 1955-1966
    • Chiang, J.Y.1
  • 6
    • 84891710536 scopus 로고    scopus 로고
    • Bile acid metabolism and signaling
    • Chiang, J. Y. (2013). Bile acid metabolism and signaling. Compr. Physiol. 3, 1191-1212
    • (2013) Compr. Physiol , vol.3 , pp. 1191-1212
    • Chiang, J.Y.1
  • 7
    • 0027275566 scopus 로고
    • Physiological parameters in laboratory animals and humans
    • Davies, B., and Morris, T. (1993). Physiological parameters in laboratory animals and humans. Pharm. Res. 10, 1093-1095
    • (1993) Pharm. Res , vol.10 , pp. 1093-1095
    • Davies, B.1    Morris, T.2
  • 8
    • 70849133150 scopus 로고    scopus 로고
    • Bile acid transporters
    • Dawson, P. A., Lan, T., and Rao, A. (2009). Bile acid transporters. J. Lipid Res. 50, 2340-2357
    • (2009) J. Lipid Res , vol.50 , pp. 2340-2357
    • Dawson, P.A.1    Lan, T.2    Rao, A.3
  • 9
    • 84455171488 scopus 로고    scopus 로고
    • In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans
    • Dawson, S., Stahl, S., Paul, N., Barber, J., and Kenna, J. G. (2012). In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. Drug Metab. Dispos. 40, 130-138
    • (2012) Drug Metab. Dispos , vol.40 , pp. 130-138
    • Dawson, S.1    Stahl, S.2    Paul, N.3    Barber, J.4    Kenna, J.G.5
  • 10
    • 66949163736 scopus 로고    scopus 로고
    • Proteomic analysis of human bile and potential applications for cancer diagnosis
    • Farina, A., Dumonceau, J. M., and Lescuyer, P. (2009). Proteomic analysis of human bile and potential applications for cancer diagnosis. Expert Rev. Proteomics 6, 285-301
    • (2009) Expert Rev. Proteomics , vol.6 , pp. 285-301
    • Farina, A.1    Dumonceau, J.M.2    Lescuyer, P.3
  • 11
    • 0035036050 scopus 로고    scopus 로고
    • The endothelin antagonist bosentan inhibits the canalicular bile salt export pump: A potential mechanism for hepatic adverse reactions
    • Fattinger, K., Funk, C., Pantze, M., Weber, C., Reichen, J., Stieger, B., and Meier, P. J. (2001). The endothelin antagonist bosentan inhibits the canalicular bile salt export pump: A potential mechanism for hepatic adverse reactions. Clin. Pharmacol. Ther. 69, 223-231
    • (2001) Clin. Pharmacol. Ther , vol.69 , pp. 223-231
    • Fattinger, K.1    Funk, C.2    Pantze, M.3    Weber, C.4    Reichen, J.5    Stieger, B.6    Meier, P.J.7
  • 12
    • 84871242500 scopus 로고    scopus 로고
    • Bile acid transporters and regulatory nuclear receptors in the liver and beyond
    • Halilbasic, E., Claudel, T., and Trauner, M. (2013). Bile acid transporters and regulatory nuclear receptors in the liver and beyond. J. Hepatol. 58, 155-168
    • (2013) J. Hepatol , vol.58 , pp. 155-168
    • Halilbasic, E.1    Claudel, T.2    Trauner, M.3
  • 13
    • 63849295015 scopus 로고    scopus 로고
    • The enterohepatic circulation of bile acids in mammals: Form and functions
    • Hofmann, A. F. (2009). The enterohepatic circulation of bile acids in mammals: Form and functions. Front. Biosci. (Landmark Ed.) 14, 2584-2598
    • (2009) Front. Biosci. (Landmark Ed.) , vol.14 , pp. 2584-2598
    • Hofmann, A.F.1
  • 14
    • 79953081372 scopus 로고    scopus 로고
    • Contribution of high basolateral bile salt efflux to the lack of hepatotoxicity in rat in response to drugs inducing cholestasis in human
    • Jemnitz, K., Veres, Z., and Vereczkey, L. (2010). Contribution of high basolateral bile salt efflux to the lack of hepatotoxicity in rat in response to drugs inducing cholestasis in human. Toxicol. Sci. 115, 80-88
    • (2010) Toxicol. Sci , vol.115 , pp. 80-88
    • Jemnitz, K.1    Veres, Z.2    Vereczkey, L.3
  • 15
    • 84873835561 scopus 로고    scopus 로고
    • Randomized, double-blind, dose-ranging study of TAK-875, a novel GPR40 agonist, in Japanese patients with inadequately controlled type 2 diabetes
    • Kaku, K., Araki, T., and Yoshinaka, R. (2013). Randomized, double-blind, dose-ranging study of TAK-875, a novel GPR40 agonist, in Japanese patients with inadequately controlled type 2 diabetes. Diabetes Care 36, 245-250
    • (2013) Diabetes Care , vol.36 , pp. 245-250
    • Kaku, K.1    Araki, T.2    Yoshinaka, R.3
  • 16
    • 84931956659 scopus 로고    scopus 로고
    • Efficacy and safety of fasiglifam (TAK-875), a G proteincoupled 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
    • Kaku, K., Enya, K., Nakaya, R., Ohira, T., and Matsuno, R. (2015). Efficacy and safety of fasiglifam (TAK-875), a G proteincoupled 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, 675-681
    • (2015) Diabetes Obes. Metab , vol.17 , pp. 675-681
    • Kaku, K.1    Enya, K.2    Nakaya, R.3    Ohira, T.4    Matsuno, R.5
  • 17
    • 84978386144 scopus 로고    scopus 로고
    • Long-term safety and efficacy of fasiglifam (TAK-875), a GPR40 agonist, as monotherapy and combination therapy in Japanese patients with type 2 diabetes: A 52-week open-label phase III study
    • Kaku, K., Enya, K., Nakaya, R., Ohira, T., and Matsuno, R. (2016). Long-term safety and efficacy of fasiglifam (TAK-875), a GPR40 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, 925-929
    • (2016) Diabetes Obes. Metab , vol.18 , pp. 925-929
    • Kaku, K.1    Enya, K.2    Nakaya, R.3    Ohira, T.4    Matsuno, R.5
  • 18
    • 48749087514 scopus 로고    scopus 로고
    • Bile acid transporters in health and disease
    • Kosters, A., and Karpen, S. J. (2008). Bile acid transporters in health and disease. Xenobiotica 38, 1043-1071
    • (2008) Xenobiotica , vol.38 , pp. 1043-1071
    • Kosters, A.1    Karpen, S.J.2
  • 20
    • 24944483081 scopus 로고    scopus 로고
    • Bile acid transport in sister of P-glycoprotein (ABCB11) knockout mice
    • Lam, P., Wang, R., and Ling, V. (2005). Bile acid transport in sister of P-glycoprotein (ABCB11) knockout mice. Biochemistry 44, 12598-12605
    • (2005) Biochemistry , vol.44 , pp. 12598-12605
    • Lam, P.1    Wang, R.2    Ling, V.3
  • 21
  • 23
    • 84862589520 scopus 로고    scopus 로고
    • A multiple-ascending-dose study to evaluate safety, pharmacokinetics, and pharmacodynamics of a novel GPR40 agonist, TAK-875, in subjects with type 2 diabetes
    • Leifke, E., Naik, H., Wu, J., Viswanathan, P., Demanno, D., Kipnes, M., and Vakilynejad, M. (2012). A multiple-ascending-dose study to evaluate safety, pharmacokinetics, and pharmacodynamics of a novel GPR40 agonist, TAK-875, in subjects with type 2 diabetes. Clin. Pharmacol. Ther. 92, 29-39
    • (2012) Clin. Pharmacol. Ther , vol.92 , pp. 29-39
    • Leifke, E.1    Naik, H.2    Wu, J.3    Viswanathan, P.4    Demanno, D.5    Kipnes, M.6    Vakilynejad, M.7
  • 24
    • 84946213017 scopus 로고    scopus 로고
    • Fasiglifam (TAK-875) inhibits hepatobiliary transporters: A possible factor contributing to fasiglifam-induced liver injury
    • Li, X., Zhong, K., Guo, Z., Zhong, D., and Chen, X. (2015). Fasiglifam (TAK-875) inhibits hepatobiliary transporters: A possible factor contributing to fasiglifam-induced liver injury. Drug Metab. Dispos. 43, 1751-1759
    • (2015) Drug Metab. Dispos , vol.43 , pp. 1751-1759
    • Li, X.1    Zhong, K.2    Guo, Z.3    Zhong, D.4    Chen, X.5
  • 25
    • 34447577912 scopus 로고    scopus 로고
    • Circumventing the Crabtree effect: Replacing media glucose with galactose increases susceptibility of HepG2 cells to mitochondrial toxicants
    • Marroquin, L. D., Hynes, J., Dykens, J. A., Jamieson, J. D., and Will, Y. (2007). Circumventing the Crabtree effect: Replacing media glucose with galactose increases susceptibility of HepG2 cells to mitochondrial toxicants. Toxicol. Sci. 97, 539-547
    • (2007) Toxicol. Sci , vol.97 , pp. 539-547
    • Marroquin, L.D.1    Hynes, J.2    Dykens, J.A.3    Jamieson, J.D.4    Will, Y.5
  • 26
    • 84919462540 scopus 로고    scopus 로고
    • Evaluation of the pharmacokinetics and safety of a single oral dose of fasiglifam in subjects with normal or varying degrees of impaired renal function
    • Mayer, M., Nudurupati, S., Peng, X., and Marcinak, J. (2014). Evaluation of the pharmacokinetics and safety of a single oral dose of fasiglifam in subjects with normal or varying degrees of impaired renal function. Drugs R D 14, 273-282
    • (2014) Drugs R D , vol.14 , pp. 273-282
    • Mayer, M.1    Nudurupati, S.2    Peng, X.3    Marcinak, J.4
  • 29
    • 84887898959 scopus 로고    scopus 로고
    • A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development
    • Morgan, R. E., van Staden, C. J., Chen, Y., Kalyanaraman, N., Kalanzi, J., Dunn, R. T., 2nd, Afshari, C. A., and Hamadeh, H. K. (2013). A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol. Sci. 136, 216-241
    • (2013) Toxicol. Sci , vol.136 , pp. 216-241
    • Morgan, R.E.1    van Staden, C.J.2    Chen, Y.3    Kalyanaraman, N.4    Kalanzi, J.5    Dunn, R.T.6    Afshari, C.A.7    Hamadeh, H.K.8
  • 30
    • 84863208301 scopus 로고    scopus 로고
    • 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
    • Naik, H., Vakilynejad, M., Wu, J., Viswanathan, P., Dote, N., Higuchi, T., and 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, 1007-1016
    • (2012) J. Clin. Pharmacol , vol.52 , pp. 1007-1016
    • Naik, H.1    Vakilynejad, M.2    Wu, J.3    Viswanathan, P.4    Dote, N.5    Higuchi, T.6    Leifke, E.7
  • 33
    • 21844468483 scopus 로고    scopus 로고
    • Impaired expression and function of the bile salt export pump due to three novel ABCB11 mutations in intrahepatic cholestasis
    • Noe, J., Kullak-Ublick, G. A., Jochum, W., Stieger, B., Kerb, R., Haberl, M., Mullhaupt, B., Meier, P. J., and Pauli-Magnus, C. (2005). Impaired expression and function of the bile salt export pump due to three novel ABCB11 mutations in intrahepatic cholestasis. J. Hepatol. 43, 536-543
    • (2005) J. Hepatol , vol.43 , pp. 536-543
    • Noe, J.1    Kullak-Ublick, G.A.2    Jochum, W.3    Stieger, B.4    Kerb, R.5    Haberl, M.6    Mullhaupt, B.7    Meier, P.J.8    Pauli-Magnus, C.9
  • 35
    • 33244467651 scopus 로고    scopus 로고
    • Bile salt biotransformations by human intestinal bacteria
    • Ridlon, J. M., Kang, D. J., and Hylemon, P. B. (2006). Bile salt biotransformations by human intestinal bacteria. J. Lipid Res. 47, 241-259
    • (2006) J. Lipid Res , vol.47 , pp. 241-259
    • Ridlon, J.M.1    Kang, D.J.2    Hylemon, P.B.3
  • 36
    • 84896108804 scopus 로고    scopus 로고
    • Drug-induced perturbations of the bile acid pool, cholestasis, and hepatotoxicity: Mechanistic considerations beyond the direct inhibition of the bile salt export pump
    • Rodrigues, A. D., Lai, Y., Cvijic, M. E., Elkin, L. L., Zvyaga, T., and Soars, M. G. (2014). Drug-induced perturbations of the bile acid pool, cholestasis, and hepatotoxicity: Mechanistic considerations beyond the direct inhibition of the bile salt export pump. Drug Metab. Dispos. 42, 566-574
    • (2014) Drug Metab. Dispos , vol.42 , pp. 566-574
    • Rodrigues, A.D.1    Lai, Y.2    Cvijic, M.E.3    Elkin, L.L.4    Zvyaga, T.5    Soars, M.G.6
  • 37
    • 0037790917 scopus 로고    scopus 로고
    • The enzymes, regulation, and genetics of bile acid synthesis
    • Russell, D. W. (2003). The enzymes, regulation, and genetics of bile acid synthesis. Annu. Rev. Biochem. 72, 137-174
    • (2003) Annu. Rev. Biochem , vol.72 , pp. 137-174
    • Russell, D.W.1
  • 39
    • 84897863552 scopus 로고    scopus 로고
    • Simple and rapid quantitation of 21 bile acids in rat serum and liver by UPLC-MS-MS: Effect of high fat diet on glycine conjugates of rat bile acids
    • Suzuki, Y., Kaneko, R., Nomura, M., Naito, H., Kitamori, K., Nakajima, T., Ogawa, T., Hattori, H., Seno, H., and Ishii, A. (2013). Simple and rapid quantitation of 21 bile acids in rat serum and liver by UPLC-MS-MS: Effect of high fat diet on glycine conjugates of rat bile acids. Nagoya J. Med. Sci. 75, 57-71
    • (2013) Nagoya J. Med. Sci , vol.75 , pp. 57-71
    • Suzuki, Y.1    Kaneko, R.2    Nomura, M.3    Naito, H.4    Kitamori, K.5    Nakajima, T.6    Ogawa, T.7    Hattori, H.8    Seno, H.9    Ishii, A.10
  • 40
    • 77954362516 scopus 로고    scopus 로고
    • Sandwich-cultured hepatocytes: An in vitro model to evaluate hepatobiliary transporter-based drug interactions and hepatotoxicity
    • Swift, B., Pfeifer, N. D., and Brouwer, K. L. (2010). Sandwich-cultured hepatocytes: An in vitro model to evaluate hepatobiliary transporter-based drug interactions and hepatotoxicity. Drug Metab. Rev. 42, 446-471
    • (2010) Drug Metab. Rev , vol.42 , pp. 446-471
    • Swift, B.1    Pfeifer, N.D.2    Brouwer, K.L.3
  • 41
    • 84879353352 scopus 로고    scopus 로고
    • Validation of a HTS-amenable assay to detect drug-induced mitochondrial toxicity in the absence and presence of cell death
    • Swiss, R., Niles, A., Cali, J. J., Nadanaciva, S., and Will, Y. (2013). Validation of a HTS-amenable assay to detect drug-induced mitochondrial toxicity in the absence and presence of cell death. Toxicol. In Vitro 27, 1789-1797
    • (2013) Toxicol. In Vitro , vol.27 , pp. 1789-1797
    • Swiss, R.1    Niles, A.2    Cali, J.J.3    Nadanaciva, S.4    Will, Y.5
  • 43
    • 70349233968 scopus 로고    scopus 로고
    • Compensatory role of P-glycoproteins in knockout mice lacking the bile salt export pump
    • Wang, R., Chen, H. L., Liu, L., Sheps, J. A., Phillips, M. J., and Ling, V. (2009). Compensatory role of P-glycoproteins in knockout mice lacking the bile salt export pump. Hepatology 50, 948-956
    • (2009) Hepatology , vol.50 , pp. 948-956
    • Wang, R.1    Chen, H.L.2    Liu, L.3    Sheps, J.A.4    Phillips, M.J.5    Ling, V.6
  • 46
    • 84881616816 scopus 로고    scopus 로고
    • An updated review on drug-induced cholestasis: Mechanisms and investigation of physicochemical properties and pharmacokinetic parameters
    • Yang, K., Kock, K., Sedykh, A., Tropsha, A., and Brouwer, K. L. (2013). An updated review on drug-induced cholestasis: Mechanisms and investigation of physicochemical properties and pharmacokinetic parameters. J. Pharm. Sci. 102, 3037-3057
    • (2013) J. Pharm. Sci , vol.102 , pp. 3037-3057
    • Yang, K.1    Kock, K.2    Sedykh, A.3    Tropsha, A.4    Brouwer, K.L.5
  • 47
    • 79951571030 scopus 로고    scopus 로고
    • Diurnal variations of mouse plasma and hepatic bile acid concentrations as well as expression of biosynthetic enzymes and transporters
    • Zhang, Y. K., Guo, G. L., and Klaassen, C. D. (2011). Diurnal variations of mouse plasma and hepatic bile acid concentrations as well as expression of biosynthetic enzymes and transporters. PLoS One 6, e16683
    • (2011) PLoS One , vol.6
    • Zhang, Y.K.1    Guo, G.L.2    Klaassen, C.D.3


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