Regular ArticlePrediction of Inter-individual Variability in the Pharmacokinetics of CYP2C19 Substrates in Humans
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Cited by (18)
Prediction of inter-individual variability on the pharmacokinetics of CYP2C8 substrates in human
2017, Drug Metabolism and PharmacokineticsCitation Excerpt :Our group has previously proposed a method that uses the Monte Carlo simulation to predict the inter-individual variability in pharmacokinetics from the mean value and standard deviation (SD) of physiological and pharmacokinetic parameters collected from the literature. This method was successfully applied to predict the inter-individual variability in the pharmacokinetics of CYP1A2 [16], CYP2C9 [17], CYP2C19 [18], CYP2D6 [19,20], and CYP3A4 [21] substrates in healthy volunteers. In the case of CYP1A2, CV of CLint,h,1A2 was estimated from the clinical pharmacokinetic data of caffeine, which is a CYP1A2 substrate with high fmCYP1A2 and low hepatic first-pass effect.
Estimation of Interindividual Variability of Pharmacokinetics of CYP2C9 Substrates in Humans
2017, Journal of Pharmaceutical SciencesCitation Excerpt :They collected the CVs reported for CYP3A4 content in human liver microsomes (33%-99%); based on a dispersion model for the in vivo variability of the area under the blood concentration curve (AUC) for the substrates and other physiological parameters (i.e., blood flow rate, plasma protein binding, liver volume, and body weight), they determined a CV of 33% for CLint,h of CYP3A4 substrates by Monte Carlo simulation. Using the reported variability of the AUC of omeprazole, we previously used this method to estimate the variability of the hepatic intrinsic clearance of CYP2C19 substrates (CLint,h,cyp2C19) as 66% and 56% for subjects with CYP2C19*1/*1 and CYP2C19*1/*2 or CYP2C19*1/*3, respectively.15 Using these CV values, the AUC variabilities of other CYP2C19 substrates have been successfully estimated.15
Influence of different proton pump inhibitors on the pharmacokinetics of voriconazole
2017, International Journal of Antimicrobial AgentsIdentifying populations sensitive to environmental chemicals by simulating toxicokinetic variability
2017, Environment InternationalCitation Excerpt :CV of abundance has been estimated at 31% for CYP3A4 and 36% for CYP2E1 (Lipscomb et al., 2003). CV of isozyme-specific CLint has been estimated at 33% for CYP3A4 (Kato et al., 2010); 60–70% for CYP2D6 (Chiba et al., 2012); 66% in extensive CYP2C19 metabolizers, and 26% in poor CYP2C19 metabolizers (Chiba et al., 2014). HTTK-Pop's assumption of 30% CV in overall CLint may therefore be reasonable for compounds primarily metabolized by CYP3A4 or 2E1, but may be an underestimate for compounds primarily metabolized by CYP2D6 or 2C19.
Prediction of inter-individual variability on the pharmacokinetics of CYP1A2 substrates in non-smoking healthy volunteers
2016, Drug Metabolism and PharmacokineticsCitation Excerpt :Because drugs with a low hepatic first-pass effect minimize the variability of that effect, they can be considered to estimate the CV of CLint,h,1A2 more accurately. The inter-individual variability of other CYPs that have been reported by our group are 33% CV for CYP3A4 [6], 60% CV for CYP2D6 in EM [7], 66% CV for CYP2C19 in EM [59], and 18.1% CV for CYP2C9 in EM. The inter-individual variability of CYP1A2 (55%) was similar to that of CYP2D6 but otherwise relatively high among CYPs.
Effects of 31 recombinant CYP2C19 variants on clomipramine metabolism in vitro
2021, Journal of Psychopharmacology
Software supported in part by KAKENHI (grant no. 24590210) was used in the present analysis.