Drug Metabolism and Pharmacokinetics 
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This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.Analysis of the interplay of physiological response to food intake and drug properties in food-drug interactions
This study aimed to identify key drug properties that influence food effect (FE) using supervised machine learning approaches. The analysis showed that drugs with high logP, dose number, and extraction ratio have a higher probability of positive FE, while drugs with low permeability and high efflux saturation index have a greater likelihood of negative FE. Weakly acidic drugs also showed a greater probability of positive FE, particularly at pKa >4.3. The importance of drug properties in predicting FE was ranked as logP, dose number, extraction ratio, pKa, and permeability. The accuracy of FE prediction using the models ...
Source: Drug Metabolism and Pharmacokinetics - October 19, 2023 Category: Drugs & Pharmacology Authors: Sheena Sharma Clark Kogan Manthena V S Varma Bhagwat Prasad Source Type: research
Simple confirmation methods for rare but impaired variants of human flavin-containing monooxygenase 3 (FMO3) found in an updated genome resource databank
Drug Metab Pharmacokinet. 2023 Aug 23;53:100528. doi: 10.1016/j.dmpk.2023.100528. Online ahead of print.ABSTRACTForty-seven new nonsense or missense human flavin-containing monooxygenase 3 (FMO3) variants were recently identified in an updated Japanese population reference panel. Of these, 20 rare single-nucleotide substitutions resulted in moderately or severely impaired FMO3 activity. To easily identify these 20 FMO3 variants (2 stop codon mutations, 2 frameshifts, and 16 amino-acid substitutions) in the clinical setting, simple confirmation methods for impaired FMO3 variants are proposed using polymerase chain reaction ...
Source: Drug Metabolism and Pharmacokinetics - October 19, 2023 Category: Drugs & Pharmacology Authors: Makiko Shimizu Miaki Makiguchi Yuka Yokota Erika Shimamura Moegi Matsuta Yuria Nakamura Mizuki Harano Hiroshi Yamazaki Source Type: research
Involvement of multiple cytochrome P450 isoenzymes in drug interactions between ritonavir and direct oral anticoagulants
Drug Metab Pharmacokinet. 2023 Feb 18;53:100498. doi: 10.1016/j.dmpk.2023.100498. Online ahead of print.ABSTRACTHerein, we aimed to determine the significance of drug interactions (DIs) between ritonavir and direct oral anticoagulants (DOACs) and identify the involved cytochrome P450 (CYP) isoenzymes. Using an in vitro cocktail method with human liver microsomes (HLM), we observed that ritonavir strongly inhibited CYPs in the following order: CYP3A, CYP2C8, CYP2D6, CYP2C9, CYP2C19, CYP2B6, and CYP2J2 (IC50: 0.023-6.79 μM). The degree of CYP2J2 inhibition was inconclusive, given the substantial discrepancy between the HLM ...
Source: Drug Metabolism and Pharmacokinetics - October 1, 2023 Category: Drugs & Pharmacology Authors: Yuta Tamemoto Yukihiro Shibata Natsumi Hashimoto Hiromi Sato Akihiro Hisaka Source Type: research
