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• W2055553642 abstract "The induction of cytochrome P450 enzymes (CYPs) is an important source of drug–drug interaction (DDI) and can result in pronounced changes in pharmacokinetics (PK). Rifampicin (RIF) is a potent inducer of CYP3A4 and also acts as a competitive inhibitor which can partially mask the induction. The objective of this study was to determine a clinical DDI study design for RIF resulting in maximum CYP3A4 induction. A physiologically based pharmacokinetic (PBPK) model was developed to project the dynamics and magnitude of CYP3A4 induction in vivo from in vitro data generated with primary human hepatocytes. The interaction model included both inductive and inhibitory effects of RIF on CYP3A4 in gut and liver and accounting for the observed RIF auto-induction. The model has been verified for 4 CYP3A4 substrates: midazolam, triazolam, alfentanil and nifedipine using plasma concentration data from 20 clinical study designs with intravenous (n = 7) and oral (n = 13) administrations. Finally, the influence of the time between RIF and substrate administration was explored for the interaction between midazolam and RIF. The model integrating in vitro induction parameters correctly predicted intravenous induction but underestimated oral induction with 30% of simulated concentrations more than 2-fold higher than of observed data. The use of a 1.6-fold higher value for the maximum induction effect (Emax) improved significantly the accuracy and precision of oral induction with 82% of simulated concentrations and all predicted PK parameters within 2-fold of observed data. Our simulations suggested that a concomitant administration of RIF and midazolam resulted in significant competitive inhibition limited to intestinal enzyme. Accordingly, a maximum induction effect could be achieved with a RIF pretreatment of 600 mg/day during 5 days and a substrate administration at least 2 h after the last RIF dose. A period of 2 weeks after RIF removal was found sufficient to allow return to baseline levels of enzyme." @default.
• W2055553642 created "2016-06-24" @default.
• W2055553642 creator A5001378539 @default.
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• W2055553642 creator A5055401474 @default.
• W2055553642 creator A5077835854 @default.
• W2055553642 date "2014-06-01" @default.
• W2055553642 modified "2023-10-10" @default.
• W2055553642 title "Physiologically based pharmacokinetic modeling of CYP3A4 induction by rifampicin in human: Influence of time between substrate and inducer administration" @default.
• W2055553642 cites W1581117673 @default.
• W2055553642 cites W1593274271 @default.
• W2055553642 cites W1847561584 @default.
• W2055553642 cites W1964026490 @default.
• W2055553642 cites W1964411950 @default.
• W2055553642 cites W1965941545 @default.
• W2055553642 cites W1972097392 @default.
• W2055553642 cites W1975065437 @default.
• W2055553642 cites W1976696095 @default.
• W2055553642 cites W1978116407 @default.
• W2055553642 cites W1985731196 @default.
• W2055553642 cites W1987952101 @default.
• W2055553642 cites W1991992414 @default.
• W2055553642 cites W1992857384 @default.
• W2055553642 cites W1996949498 @default.
• W2055553642 cites W1997271604 @default.
• W2055553642 cites W2005966874 @default.
• W2055553642 cites W2007761738 @default.
• W2055553642 cites W2013822904 @default.
• W2055553642 cites W2014164434 @default.
• W2055553642 cites W2018429921 @default.
• W2055553642 cites W2018986030 @default.
• W2055553642 cites W2019540147 @default.
• W2055553642 cites W2024179174 @default.
• W2055553642 cites W2024587809 @default.
• W2055553642 cites W2027410033 @default.
• W2055553642 cites W2030021013 @default.
• W2055553642 cites W2031652509 @default.
• W2055553642 cites W2034388219 @default.
• W2055553642 cites W2035168432 @default.
• W2055553642 cites W2035848106 @default.
• W2055553642 cites W2038014794 @default.
• W2055553642 cites W2040233060 @default.
• W2055553642 cites W2041777107 @default.
• W2055553642 cites W2044906812 @default.
• W2055553642 cites W2046948630 @default.
• W2055553642 cites W2056565974 @default.
• W2055553642 cites W2058387955 @default.
• W2055553642 cites W2064641577 @default.
• W2055553642 cites W2067195248 @default.
• W2055553642 cites W2069390464 @default.
• W2055553642 cites W2070177020 @default.
• W2055553642 cites W2079436617 @default.
• W2055553642 cites W2092456450 @default.
• W2055553642 cites W2094738707 @default.
• W2055553642 cites W2098293164 @default.
• W2055553642 cites W2104925243 @default.
• W2055553642 cites W2111070729 @default.
• W2055553642 cites W2113830209 @default.
• W2055553642 cites W2114089215 @default.
• W2055553642 cites W2115722806 @default.
• W2055553642 cites W2118070545 @default.
• W2055553642 cites W2119482262 @default.
• W2055553642 cites W2121460361 @default.
• W2055553642 cites W2124945212 @default.
• W2055553642 cites W2125021132 @default.
• W2055553642 cites W2125270482 @default.
• W2055553642 cites W2131138924 @default.
• W2055553642 cites W2137442330 @default.
• W2055553642 cites W2142573506 @default.
• W2055553642 cites W2144815258 @default.
• W2055553642 cites W2145484821 @default.
• W2055553642 cites W2146393360 @default.
• W2055553642 cites W2146591007 @default.
• W2055553642 cites W2149429360 @default.
• W2055553642 cites W2153179877 @default.
• W2055553642 cites W2156445661 @default.
• W2055553642 cites W2157349792 @default.
• W2055553642 cites W2161894198 @default.
• W2055553642 cites W2165334931 @default.
• W2055553642 cites W2169830276 @default.
• W2055553642 cites W2312400319 @default.
• W2055553642 cites W2466547779 @default.
• W2055553642 cites W39606323 @default.
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• W2055553642 doi "https://doi.org/10.1016/j.ejps.2014.02.002" @default.
• W2055553642 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24530864" @default.
• W2055553642 hasPublicationYear "2014" @default.
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