Physiologically based pharmacokinetic modelling to determine the impact of CYP2B6 genotype on efavirenz exposure in children, mothers and breastfeeding infants.
Sign Up to like & getrecommendations! Published in 2023 at "Clinical pharmacology and therapeutics"
DOI: 10.1002/cpt.2912
Abstract: The antiretroviral drug efavirenz remains widely used in children and mothers during breastfeeding in tuberculosis-endemic areas. Evaluating the safety of efavirenz during breastfeeding requires an understanding of its pharmacokinetics in breast milk, its exposure in… read more here.
Keywords: efavirenz; mothers breastfeeding; breastfeeding infants; cyp2b6 ... See more keywords
Human CYP2A6, CYP2B6, AND CYP2E1 Atropselectively Metabolize Polychlorinated Biphenyls to Hydroxylated Metabolites.
Sign Up to like & getrecommendations! Published in 2019 at "Environmental science & technology"
DOI: 10.1021/acs.est.8b05250
Abstract: Exposure to chiral polychlorinated biphenyls (PCBs) has been associated with neurodevelopmental disorders. Their hydroxylated metabolites (OH-PCBs) are also potentially toxic to the developing human brain; however, the formation of OH-PCBs by human cytochrome P450 (P450)… read more here.
Keywords: hydroxylated metabolites; cyp2a6 cyp2b6; polychlorinated biphenyls; cyp2e1 ... See more keywords
Human cytochrome P450 2B6 genetic variability in Botswana: a case of haplotype diversity and convergent phenotypes
Sign Up to like & getrecommendations! Published in 2018 at "Scientific Reports"
DOI: 10.1038/s41598-018-23350-1
Abstract: Identification of inter-individual variability for drug metabolism through cytochrome P450 2B6 (CYP2B6) enzyme is important for understanding the differences in clinical responses to malaria and HIV. This study evaluates the distribution of CYP2B6 alleles, haplotypes… read more here.
Keywords: p450 2b6; cyp2b6; botswana; variability ... See more keywords
CYP2B6 allelic variants and non-genetic factors influence CYP2B6 enzyme function
Sign Up to like & getrecommendations! Published in 2022 at "Scientific Reports"
DOI: 10.1038/s41598-022-07022-9
Abstract: Human CYP2B6 enzyme although constitutes relatively low proportion (1–4%) of hepatic cytochrome P450 content, it is the major catalyst of metabolism of several clinically important drugs (efavirenz, cyclophosphamide, bupropion, methadone). High interindividual variability in CYP2B6… read more here.
Keywords: function; cyp2b6; genetic factors; cyp2b6 enzyme ... See more keywords
Bulbine natalensis (currently Bulbine latifolia) and select bulbine knipholones modulate the activity of AhR, CYP1A2, CYP2B6, and P-gp.
Sign Up to like & getrecommendations! Published in 2021 at "Planta medica"
DOI: 10.1055/a-1557-2113
Abstract: Bulbine natalensis, an emerging medicinal herb on the global market with androgenic properties, is often formulated in dietary supplements that promote perceived sexual enhancement. However, to date, comprehensive safety studies of B. natalensis are lacking,… read more here.
Keywords: bulbine natalensis; cyp2b6; activity; bulbine ... See more keywords
Newly identified tree shrew cytochrome P450 2B6 (CYP2B6) and pig CYP2B6b are functional drug-metabolising enzymes
Sign Up to like & getrecommendations! Published in 2022 at "Xenobiotica"
DOI: 10.1080/00498254.2022.2141153
Abstract: Abstract Tree shrews have high phylogenetic affinity to humans and are used in various fields of biomedical research, especially hepatitis virus infection; however, cytochromes P450 (P450s or CYPs) have not been investigated in this species.… read more here.
Keywords: tree shrew; pig cyp2b6b; cyp2b6; cyp2b6 pig ... See more keywords
Effect of diurnal variation, CYP2B6 genotype and age on the pharmacokinetics of nevirapine in African children
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Antimicrobial Chemotherapy"
DOI: 10.1093/jac/dkw388
Abstract: Objectives To characterize the effects of CYP2B6 polymorphisms, diurnal variation and demographic factors on nevirapine pharmacokinetics in African children. Methods Non-linear mixed-effects modelling conducted in NONMEM 7.3 described nevirapine plasma concentration–time data from 414 children… read more here.
Keywords: cyp2b6; effect; metabolizer; diurnal variation ... See more keywords
Polymorphisms of cytochrome P450 2B6 (CYP2B6) in cynomolgus and rhesus macaques
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Medical Primatology"
DOI: 10.1111/jmp.12336
Abstract: Cytochrome P450 2B6 (CYP2B6) is an important drug‐metabolizing enzyme and is expressed in liver. Although human CYP2B6 variants account for variable enzyme properties among individuals and populations, CYP2B6 genetic variants have not been investigated in… read more here.
Keywords: p450 2b6; cyp2b6 cynomolgus; cyp2b6; 2b6 cyp2b6 ... See more keywords
Efavirenz Metabolism: Influence of Polymorphic CYP2B6 Variants and Stereochemistry
Sign Up to like & getrecommendations! Published in 2019 at "Drug Metabolism and Disposition"
DOI: 10.1124/dmd.119.086348
Abstract: Efavirenz (more specifically the S-enantiomer) is a cornerstone antiretroviral therapy for treatment of HIV infection. The major primary metabolite is S-8-hydroxyefavirenz, which does not have antiretroviral activity but is neurotoxic. Cytochrome P450 2B6 (CYP2B6) is… read more here.
Keywords: cyp2b6; efavirenz hydroxylation; cyp2b6 variants; efavirenz metabolism ... See more keywords
Stereoselective Bupropion Hydroxylation by Cytochrome P450 CYP2B6 and Cytochrome P450 Oxidoreductase Genetic Variants
Sign Up to like & getrecommendations! Published in 2020 at "Drug Metabolism and Disposition"
DOI: 10.1124/dmd.119.090407
Abstract: Bioactivation of the antidepressant and smoking cessation drug bupropion is catalyzed predominantly by CYP2B6. The metabolite hydroxybupropion derived from t-butylhydroxylation is considered to contribute to the antidepressant and smoking-cessation effects of the parent drug. Bupropion… read more here.
Keywords: bupropion hydroxylation; cyp2b6; p450; cyp2b6 cyp2b6 ... See more keywords
NADPH-Independent Inactivation of CYP2B6 and NADPH-Dependent Inactivation of CYP3A4/5 by PBD: Potential Implication for Assessing Covalent Modulators for Time-Dependent Inhibition
Sign Up to like & getrecommendations! Published in 2020 at "Drug Metabolism and Disposition"
DOI: 10.1124/dmd.120.090878
Abstract: Pyrrolo[2,1-c][1,4]benzodiazepine dimer (PBD) has shown broad antitumor properties and potential as a therapeutic agent for cancers. During a routine drug-drug interaction assessment, it was found that PBD is a reversible inhibitor of CYP2C8 (IC50 =… read more here.
Keywords: cyp2b6; inhibition; nadph independent; inactivation ... See more keywords