Research paperHepatic and intestinal metabolism of indinavir, an HIV protease inhibitor, in rat and human microsomes: Major role of CYP3A
References (22)
- et al.
Heterogeneity of cytochrome P450IIIA expression in rat gut epithelia
Gastroenterology
(1992) - et al.
The carbon-monoxide binding pigment of liver microsomes
J Biol Chem
(1964) - et al.
Cytochrome P450 of small intestinal epithelial cells: Immunochemical characterization of the increase in cyto chrome P450 caused by phenobarbital
Gastroenterology
(1985) - et al.
Protein measurement with the Polin phenol reagent
J Biol Chem
(1951) - et al.
Time and dose dependence of 3-methylcholanthrene-induced metabolism in rat intestinal mucosal cells and microsomes
Biochem Pharmacol
(1982) - et al.
Physiologically based pharmaco-kinetic modeling: Principles and applications
J Pharma Sci
(1983) - et al.
Prediction of intestinal first-pass effect of phenacetin in the rat from enzyme kinetic data-Correlation with in vivo data using mucosal blood flow
Biochem Pharmacol
(1982) - et al.
Small intestinal cytochrome P450
Crit Rev Toxicol
(1992) - et al.
Characterization of rat small intestinal cytochrome P-450 composition and inducibility
Drug Metab Dispos
(1996) - et al.
Cytochrome P450 isoenzymes, epoxide hydrolase and glutathione transferases in rat and human hepatic and extra hepatic tissues
J Pharmacol Exp Ther
(1990)
Bioavailability of cyclosporine with concomitant rifampin administration is markedly less than predicted by hepatic en zyme induction
Clin Pharmacol Ther
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2023, European Journal of Pharmaceutical SciencesAtypical kinetics of cytochrome P450 enzymes in pharmacology and toxicology
2022, Advances in PharmacologyCitation Excerpt :Currently, limited evidence of atypical kinetics occurring with the use of human intestinal microsomes (HIMs) or other in vitro models of human intestinal metabolism have been reported in contrast to HLMs (Oda & Kharasch, 2001a, 2001b). Substrate inhibition kinetics has been reported for metabolite formation from indinavir oxidation in permeabilized enterocytes (Davies et al., 2020) although it is unknown if this atypical kinetics was correspondingly observed in indinavir oxidation in HLMs as only kinetic parameters Km and Vmax were reported without corresponding graphical representations (Chiba, Hensleigh, & Lin, 1997). With reference to a previous example on wild-type CYP2B6.1 metabolism of S-efavirenz which demonstrates complete substrate inhibition, CYP2B6 is significantly expressed in human intestine (relative P450 expression in jejunum of 4.9–7.8% and highest mean percentage contribution of colon P450 expression to intestinal P450 expression) (Fritz et al., 2019) and contributes significantly to the elimination of efavirenz with an estimated fraction metabolized of 62% (Ke, Barter, Rowland-Yeo, & Almond, 2016).
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