Estrogen associations with human pregnancy related increases in cytochrome P450 3A activity [PDF]
Frontiers in PharmacologyIntroductionIncreased CYP3A-mediated drug clearance during pregnancy can lead to subtherapeutic dosing of CYP3A substrates. Pregnancy-related hormones (PRHs) increase CYP3A4 expression and activity in cultured human hepatocytes.
Muluneh M. Fashe +8 more
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Dynamic phenotype monitoring to prevent genotype–phenotype discrepancies in pharmacogenetic-guided drug therapy [PDF]
Frontiers in PharmacologyBackgroundOne of the limiting factors for the clinical application of pharmacogenomics (PGx) is phenoconversion, i.e., the dynamic discrepancy between genotype-predicted and actual drug-metabolizing phenotypes.
Pálma Porrogi
doaj +2 more sources
CYP3A Activity in End-of-Life Cancer Patients Measured by 4β-Hydroxycholesterol/cholesterol Ratio, in Men and Women. [PDF]
Cancers (Basel), 2021 More than 50% of all drugs are metabolized by the cytochrome P450 3A enzyme (CYP3A). The aim of this study was to investigate if the CYP3A activity, measured by the endogenous marker 4β-hydroxycholesterol/cholesterol ratio (4β-OHC/C), is changed during ...
Bergström H +5 more
europepmc +2 more sources
Plasma 4β-Hydroxycholesterol Predicts Ribociclib CYP3A-Mediated Metabolism, but Not Plasma Exposure, in Patients with Primary Brain Cancer. [PDF]
Cancers (Basel)Background/Objectives: This study aimed to evaluate the potential utility of plasma 4β-hydroxycholesterol (4β-OHC) as an endogenous biomarker of hepatic CYP3A activity for predicting ribociclib metabolism and systemic pharmacokinetics in patients with ...
Wickramasinghe C +6 more
europepmc +2 more sources
Comparative performance of oral midazolam clearance and plasma 4β-hydroxycholesterol to explain interindividual variability in tacrolimus clearance. [PDF]
Br J Clin Pharmacol, 2016 We compared the CYP3A4 metrics weight-corrected midazolam apparent oral clearance (MDZ Cl/F/W) and plasma 4β-hydroxycholesterol/cholesterol (4β-OHC/C) as they relate to tacrolimus (TAC) Cl/F/W in renal transplant recipients.status ...
Vanhove T +5 more
europepmc +2 more sources
PHENOTYPING CYP3A4/5 USING AN ENDOGENOUS BIOMARKER IN CHILDREN WITH DOWN SYNDROME [PDF]
Bulletin of Pharmaceutical Sciences. Assiut University, 2020 Background: Down syndrome (DS); a common chromosomal abnormality in humans can affect multiple organ systems. DS individuals usually use a wide range of medications.
Lateef Khan +5 more
doaj +1 more source
Elevated 4β-hydroxycholesterol/cholesterol ratio in anorexia nervosa patients. [PDF]
Pharmacol Res Perspect, 2018 Recent studies have shown that the cytochrome P450 (CYP) 3A phenotype marker 4β‐hydroxycholesterol/cholesterol (4βOHC/C) ratio is negatively correlated with body weight in healthy volunteers, and that obese patients have lower 4βOHC levels than healthy ...
Hole K +5 more
europepmc +2 more sources
4β-hydroxycholesterol as an endogenous CYP3A marker in cancer patients treated with taxanes. [PDF]
Br J Clin Pharmacol, 2015 Aim Taxanes are anti-cancer agents used to treat several types of solid tumours. They are metabolized by cytochrome P450 (CYP) 3A, displaying a large pharmacokinetic (PK) variability.
de Graan AJ +8 more
europepmc +2 more sources
Journal of Lipid Research, 2022 4β-Hydroxycholesterol (4β-OHC) is formed by Cytochrome P450 (CYP)3A and has drawn attention as an endogenous phenotyping probe for CYP3A activity. However, 4β-OHC is also increased by cholesterol autooxidation occurring in vitro due to dysregulated ...
Yosuke Suzuki +10 more
doaj +1 more source
Correlations between 4β-hydroxycholesterol and hepatic and intestinal CYP3A4: protein expression, microsomal ex vivo activity, and in vivo activity in patients with a wide body weight range. [PDF]
Eur J Clin Pharmacol, 2022 PURPOSE: Variability in cytochrome P450 3A4 (CYP3A4) metabolism is mainly caused by non-genetic factors, hence providing a need for accurate phenotype biomarkers.
Eide Kvitne K +18 more
europepmc +2 more sources