Regular ArticlePrediction of the Intestinal First-pass Metabolism of CYP3A and UGT Substrates in Humans from in vitro Data
References (41)
Kinetic impact of presystemic intestinal metabolism on drug absorption: experiment and data analysis for the prediction of in vivo absorption from in vitro data
Drug Metab. Pharmacokinet.
(2002)Pharmacokinetics of raloxifene and its clinical application
Eur. J. Obstet. Gynecol. Reprod. Biol.
(1999)- et al.
Caco-2 permeability of weakly basic drugs predicted with the double-sink PAMPA pKa(flux) method
Eur. J. Pharm. Sci.
(2005) - et al.
The intestinal first-pass metabolism of substrates of CYP3A4 and P-glycoprotein – quantitative analysis based on information from the literature
Drug Metab. Pharmacokinet.
(2003) Troglitazone: the discovery and development of a novel therapy for the treatment of Type 2 diabetes mellitus
Adv. Drug Deliv. Rev.
(2002)- et al.
Utility of 96 well Caco-2 cell system for increased throughput of P-gp screening in drug discovery
Eur. J. Pharm. Biopharm.
(2004) - et al.
Species differences in in vitro and in vivo small intestinal metabolism of CYP3A substrates
J. Pharm. Sci.
(2008) - et al.
UDPglucuronosyltransferases and clinical drug-drug interactions
Pharmacol. Ther.
(2005) Intestinal glucuronidation metabolism may have a greater impact on oral bioavailability than hepatic glucuronidation metabolism in humans: A study with raloxifene, substrate for UGT1A1, 1A8, 1A9, and 1A10
Int. J. Pharm.
(2009)- et al.
Presystemic and systemic intestinal metabolism of fenoterol in the conscious rat
Drug Metab. Dispos.
(1985)
Quantitation of extrahepatic metabolism
Pulmonary and intestinal conjugation of naphthol. Drug Metab. Dispos.
(1985)
Prediction of intestinal first-pass drug metabolism
Curr. Drug Metab.
(2007)
Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data
Drug Metab. Dispos.
(2010)
Prediction of the intestinal first-pass metabolism of CYP3A substrates in humans using cynomolgus monkeys
Drug Metab. Dispos.
(2010)
The rise of PAMPA
Expert Opin. Drug Metab. Toxicol.
(2005)
Cytochromes P450 and experimental models of drug metabolism
J. Cell. Mol. Med.
(2002)
The human intestinal cytochrome P450 “PIE”
Drug Metab. Dispos.
(2006)
Drugdrug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios
Drug Metab. Dispos.
(2004)
Human UDP-glucuronosyltransferases: metabolism, expression, and disease
Annu. Rev. Pharmacol. Toxicol.
(2000)
In vitro glucuronidation using human liver microsomes and the pore-forming peptide alamethicin
Drug Metab. Dispos.
(2000)
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