PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 32656158-4 2020 To specifically and quickly measure CYP3A activity, we developed method based on gas chromatography interfaced with triple-quadrupole mass spectrometry for the quantification of cortisol, cortisone, 6beta-hydroxycortisol, and 6beta-hydroxycortisone simultaneously in urine and 4beta-hydroxycholesterol in plasma. cholest-5-ene-3,4-diol 277-301 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 36-41 32537715-7 2020 The mean plasma Day 14/Day 1 ratio of 4beta-hydroxycholesterol, an endogenous biomarker of CYP3A4 activity, was 0.59 (90% CI 0.54-0.66), suggesting a net inhibition of CYP3A4 by fedratinib. cholest-5-ene-3,4-diol 38-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 91-97 32537715-7 2020 The mean plasma Day 14/Day 1 ratio of 4beta-hydroxycholesterol, an endogenous biomarker of CYP3A4 activity, was 0.59 (90% CI 0.54-0.66), suggesting a net inhibition of CYP3A4 by fedratinib. cholest-5-ene-3,4-diol 38-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 168-174 31002385-0 2019 Use of 4beta-Hydroxycholesterol Plasma Concentrations as an Endogenous Biomarker of CYP3A Activity: Clinical Validation in Individuals With Type 2 Diabetes. cholest-5-ene-3,4-diol 7-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-89 30058048-3 2019 We describe the utility of 4beta hydroxycholesterol as a marker of CYP3A activity. cholest-5-ene-3,4-diol 27-51 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 67-72 30826567-4 2019 We measured plasma concentrations of the above compounds in stable kidney transplant recipients, and evaluated their relations with phenoconversion of CYP3A evaluated by plasma concentration of 4beta-hydroxycholesterol, a biomarker of CYP3A activity. cholest-5-ene-3,4-diol 194-218 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 151-156 30826567-0 2019 Factors involved in phenoconversion of CYP3A using 4beta-hydroxycholesterol in stable kidney transplant recipients. cholest-5-ene-3,4-diol 51-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-44 30748026-0 2019 4beta-Hydroxycholesterol as an Endogenous Biomarker for CYP3A Activity: Literature Review and Critical Evaluation. cholest-5-ene-3,4-diol 0-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-61 30748026-2 2019 Recently, plasma 4beta-hydroxycholesterol (4beta-OHC), the metabolite of CYP3A-mediated cholesterol metabolism, has been championed as an endogenous biomarker for CYP3A, particularly during chronic conditions where CYP3A activity is altered by disease and in long-term treatment studies where midazolam administration is not optimal. cholest-5-ene-3,4-diol 17-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-78 30748026-2 2019 Recently, plasma 4beta-hydroxycholesterol (4beta-OHC), the metabolite of CYP3A-mediated cholesterol metabolism, has been championed as an endogenous biomarker for CYP3A, particularly during chronic conditions where CYP3A activity is altered by disease and in long-term treatment studies where midazolam administration is not optimal. cholest-5-ene-3,4-diol 17-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 163-168 30748026-2 2019 Recently, plasma 4beta-hydroxycholesterol (4beta-OHC), the metabolite of CYP3A-mediated cholesterol metabolism, has been championed as an endogenous biomarker for CYP3A, particularly during chronic conditions where CYP3A activity is altered by disease and in long-term treatment studies where midazolam administration is not optimal. cholest-5-ene-3,4-diol 17-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 163-168 30858735-0 2019 Modeling and simulation of the endogenous CYP3A induction marker 4beta-hydroxycholesterol during enasidenib treatment. cholest-5-ene-3,4-diol 65-89 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 42-47 29649093-0 2018 Comparison of CYP3A4-Inducing Capacity of Enzyme-Inducing Antiepileptic Drugs Using 4beta-Hydroxycholesterol as Biomarker. cholest-5-ene-3,4-diol 84-108 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-20 29991576-4 2018 CYP3A4 phenotype was measured as serum concentration of 4beta-hydroxycholesterol (4betaOHC) by ultra-performance liquid chromatography-tandem mass spectrometry in samples collected prior to and 3 months after initiation of treatment with TNF-alpha inhibitors. cholest-5-ene-3,4-diol 56-80 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 30340067-0 2018 Quantitative analysis of 4beta- and 4alpha-hydroxycholesterol in human plasma and serum by UHPLC/ESI-HR-MS. Cholesterol oxidation product 4beta-hydroxycholesterol (4beta-OHC) may possibly be used as an endogenous biomarker of CYP3A enzyme activity and as CYP3A4 is involved in the metabolism of approximately 50% of the drugs in clinical use, the monitoring of CYP3A activity by 4beta-OHC plasma or serum levels, may be of clinical significance. cholest-5-ene-3,4-diol 138-162 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 226-231 30340067-0 2018 Quantitative analysis of 4beta- and 4alpha-hydroxycholesterol in human plasma and serum by UHPLC/ESI-HR-MS. Cholesterol oxidation product 4beta-hydroxycholesterol (4beta-OHC) may possibly be used as an endogenous biomarker of CYP3A enzyme activity and as CYP3A4 is involved in the metabolism of approximately 50% of the drugs in clinical use, the monitoring of CYP3A activity by 4beta-OHC plasma or serum levels, may be of clinical significance. cholest-5-ene-3,4-diol 138-162 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 255-261 30340067-0 2018 Quantitative analysis of 4beta- and 4alpha-hydroxycholesterol in human plasma and serum by UHPLC/ESI-HR-MS. Cholesterol oxidation product 4beta-hydroxycholesterol (4beta-OHC) may possibly be used as an endogenous biomarker of CYP3A enzyme activity and as CYP3A4 is involved in the metabolism of approximately 50% of the drugs in clinical use, the monitoring of CYP3A activity by 4beta-OHC plasma or serum levels, may be of clinical significance. cholest-5-ene-3,4-diol 138-162 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 255-260 29649093-3 2018 METHODS: Residual serum samples from patients treated with EIAEDs or levetiracetam were collected from a therapeutic drug monitoring service for analysis of 4beta-hydroxycholesterol (4betaOHC), which is an indicator of CYP3A4 activity. cholest-5-ene-3,4-diol 157-181 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 219-225 29691891-0 2018 Kuypers and Vanhove reply to "Was 4beta-hydroxycholesterol ever going to be a useful marker of CYP3A4 activity?" cholest-5-ene-3,4-diol 34-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-101 29749106-1 2018 reply to "Was 4beta-hydroxycholesterol ever going to be a useful marker of CYP3A4 activity?" cholest-5-ene-3,4-diol 14-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-81 29464732-0 2018 Was 4beta-hydroxycholesterol ever going to be a useful marker of CYP3A4 activity? cholest-5-ene-3,4-diol 4-28 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 65-71 29117990-7 2018 The simulated midazolam area under the curve ratio of 0.54 and an accompanying observed 1.9-fold increase in the CYP3A4 activity of biomarker 4beta-hydroxycholesterol indicated a weak-to-moderate CYP3A4 induction by midostaurin and its metabolites at steady state in patients with advSM. cholest-5-ene-3,4-diol 142-166 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 113-119 29759884-0 2018 Assessment of induced CYP3A activity in pregnant women using 4beta-hydroxycholesterol: Cholesterol ratio as an appropriate metabolic marker. cholest-5-ene-3,4-diol 61-85 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 22-27 29759884-5 2018 RESULTS: An increased 4beta-hydroxycholesterol/cholesterol ratio, consistent with high CYP3A activity, was observed in pregnant women compared with that in non-pregnant women; however, no differences were observed among trimesters. cholest-5-ene-3,4-diol 22-46 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-92 29759884-7 2018 CONCLUSIONS: We observed an increase in the activity of CYP3A following but not during pregnancy when measured using the 4beta-hydroxycholesterol/cholesterol ratio. cholest-5-ene-3,4-diol 121-145 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-61 29279486-2 2018 Methods The level of serum 4beta-hydroxycholesterol (4betaHC), a surrogate marker of CYP3A4 activity, was determined by LC-MS/MS in samples obtained from patients with HCV infection (CHCs) as well as healthy control subjects (CTLs). cholest-5-ene-3,4-diol 27-51 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 85-91 29279486-2 2018 Methods The level of serum 4beta-hydroxycholesterol (4betaHC), a surrogate marker of CYP3A4 activity, was determined by LC-MS/MS in samples obtained from patients with HCV infection (CHCs) as well as healthy control subjects (CTLs). cholest-5-ene-3,4-diol 53-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 85-91 29279486-10 2018 Conclusion The evaluation of CYP3A4 activity by measuring 4betaHC before treatment may provide additional information that can potentially be used to select cost- and efficacy-optimized treatment of HCV. cholest-5-ene-3,4-diol 58-65 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-35 29858698-6 2018 In addition, in vitro studies using human liver microsomes showed that the formation of 4beta-HC was strongly inhibited by a CYP3A inhibitor, while the inhibitory effect of the CYP3A inhibition on the formation of 25-HC was weak. cholest-5-ene-3,4-diol 88-96 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 125-130 29117990-7 2018 The simulated midazolam area under the curve ratio of 0.54 and an accompanying observed 1.9-fold increase in the CYP3A4 activity of biomarker 4beta-hydroxycholesterol indicated a weak-to-moderate CYP3A4 induction by midostaurin and its metabolites at steady state in patients with advSM. cholest-5-ene-3,4-diol 142-166 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 196-202 28585378-0 2017 4beta-Hydroxycholesterol level significantly correlates with steady-state serum concentration of the CYP3A4 substrate quetiapine in psychiatric patients. cholest-5-ene-3,4-diol 0-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 101-107 28928137-2 2017 Therefore, the aim of this study was to evaluate the change in CYP3A activity measured as 4beta-hydroxycholesterol (4betaOHC) concentration after kidney transplantation. cholest-5-ene-3,4-diol 90-114 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 63-68 28585378-1 2017 AIM: 4beta-Hydroxycholesterol (4betaOHC) is sensitive towards induction or inhibition of CYP3A4, but its potential usefulness as a dosing biomarker remains to be demonstrated. cholest-5-ene-3,4-diol 5-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 28603840-1 2017 AIMS: The CYP3A metric 4beta-hydroxycholesterol (4betaOHC) has been shown to correlate with tacrolimus steady-state apparent oral clearance (CL/F). cholest-5-ene-3,4-diol 23-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 10-15 27138546-0 2017 An Exposure-Response Modeling Approach to Examine the Relationship Between Potency of CYP3A Inducer and Plasma 4beta-Hydroxycholesterol in Healthy Subjects. cholest-5-ene-3,4-diol 111-135 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 86-91 28146606-3 2017 The aim of this study was to assess the value of the endogenous CYP3A marker 4beta-hydroxycholesterol (4betaOHC) for tacrolimus dose individualization early after kidney transplantation. cholest-5-ene-3,4-diol 77-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 64-69 27975131-1 2017 PURPOSE: Individual variability in the endogenous CYP3A metabolite 4beta-hydroxycholesterol (4betaOHC) is substantial, but to which extent this is determined by genetic and nongenetic factors remains unclear. cholest-5-ene-3,4-diol 67-91 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 50-55 27718639-0 2017 Perspective: 4beta-hydroxycholesterol as an emerging endogenous biomarker of hepatic CYP3A. cholest-5-ene-3,4-diol 13-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 85-90 27718639-3 2017 Plasma 4beta-hydroxycholesterol (4beta-HC) is considered as an emerging endogenous biomarker for cytochrome P450 3A (CYP3A), one of the major drug metabolizing enzymes. cholest-5-ene-3,4-diol 7-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-115 27718639-3 2017 Plasma 4beta-hydroxycholesterol (4beta-HC) is considered as an emerging endogenous biomarker for cytochrome P450 3A (CYP3A), one of the major drug metabolizing enzymes. cholest-5-ene-3,4-diol 7-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 117-122 27718639-3 2017 Plasma 4beta-hydroxycholesterol (4beta-HC) is considered as an emerging endogenous biomarker for cytochrome P450 3A (CYP3A), one of the major drug metabolizing enzymes. cholest-5-ene-3,4-diol 33-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-115 27718639-3 2017 Plasma 4beta-hydroxycholesterol (4beta-HC) is considered as an emerging endogenous biomarker for cytochrome P450 3A (CYP3A), one of the major drug metabolizing enzymes. cholest-5-ene-3,4-diol 33-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 117-122 27718639-5 2017 Herein, we review the biology of 4beta-HC, its response to treatment with CYP3A inducers, inhibitors and mixed inducer/inhibitors in healthy volunteers and patients, the association of 4beta-HC with other probes of CYP3A activity (e.g. midazolam, urinary cortisol ratios), and present predictive pharmacokinetic models. cholest-5-ene-3,4-diol 33-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 74-79 27991741-2 2017 We determined 4beta-hydroxycholesterol (4betaOHC), an endogenous CYP3A4 metabolite, in patients with rheumatoid arthritis (RA) before and after treatment with biological disease-modifying antirheumatic drugs (bDMARDs). cholest-5-ene-3,4-diol 14-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 65-71 27565568-0 2016 Rapid LC-MS/MS method for the determination of 4-hydroxycholesterol/cholesterol ratio in serum as endogenous biomarker for CYP3A activity in human and foals. cholest-5-ene-3,4-diol 47-67 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 123-128 27777246-6 2017 The sensitive CYP3A biomarker 4beta-hydroxycholesterol is built into the early clinical phase I studies for all candidates since rare cases of in vivo induction have been found without any induction alerts from the currently used in vitro methods. cholest-5-ene-3,4-diol 30-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-19 27565568-2 2016 Thus, it was the aim of this study to develop and validate an analytical method allowing estimation of the hepatic CYP3A enzyme activity using the 4-hydroxycholesterol to cholesterol ratio as an endogenous biomarker in serum. cholest-5-ene-3,4-diol 147-167 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-120 27565568-11 2016 Finally, the validated assay was applied to measure 4-hydroxycholesterol and cholesterol in serum samples of clinical studies in humans and foals that could verify induction of hepatic CYP3A4 (human) and CYP3A89 (foals) after premedication with the known enzyme inducer rifampicin. cholest-5-ene-3,4-diol 52-72 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 185-191 27138133-0 2016 Compelling Relationship of CYP3A Induction to Levels of the Putative Biomarker 4beta-Hydroxycholesterol and Changes in Midazolam Exposure. cholest-5-ene-3,4-diol 79-103 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-32 27350147-0 2016 Recommendations on the Development of a Bioanalytical Assay for 4beta-Hydroxycholesterol, an Emerging Endogenous Biomarker of CYP3A Activity. cholest-5-ene-3,4-diol 64-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 126-131 27350147-1 2016 The availability of reliable assays for measuring 4beta-hydroxycholesterol (4beta-HC), a CYP3A metabolite of cholesterol, is an important step in qualifying this endogenous moiety as a biomarker of CYP3A activity. cholest-5-ene-3,4-diol 50-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-94 27350147-1 2016 The availability of reliable assays for measuring 4beta-hydroxycholesterol (4beta-HC), a CYP3A metabolite of cholesterol, is an important step in qualifying this endogenous moiety as a biomarker of CYP3A activity. cholest-5-ene-3,4-diol 50-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 198-203 27350147-1 2016 The availability of reliable assays for measuring 4beta-hydroxycholesterol (4beta-HC), a CYP3A metabolite of cholesterol, is an important step in qualifying this endogenous moiety as a biomarker of CYP3A activity. cholest-5-ene-3,4-diol 76-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-94 27350147-1 2016 The availability of reliable assays for measuring 4beta-hydroxycholesterol (4beta-HC), a CYP3A metabolite of cholesterol, is an important step in qualifying this endogenous moiety as a biomarker of CYP3A activity. cholest-5-ene-3,4-diol 76-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 198-203 24964282-1 2014 A Bayesian mechanism-based pharmacokinetic/pharmacodynamic model of cytochrome P450 3A4 (CYP3A4) activity was developed based on a clinical study of the effects of ketoconazole and rifampin on midazolam exposure and plasma 4beta-hydroxycholesterol (4betaHC) concentrations. cholest-5-ene-3,4-diol 223-247 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 26399557-2 2016 The biomarkers 4beta-hydroxycholesterol (4betaHC) and 6beta-hydroxycortisol (6betaHCL) are sensitive to CYP3A induction and inhibition. cholest-5-ene-3,4-diol 15-39 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 104-109 26399557-2 2016 The biomarkers 4beta-hydroxycholesterol (4betaHC) and 6beta-hydroxycortisol (6betaHCL) are sensitive to CYP3A induction and inhibition. cholest-5-ene-3,4-diol 41-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 104-109 26399557-4 2016 We investigated whether endogenous plasma biomarkers (4betaHC and 6betaHCL) are associated with basal CYP3A metabolic activity in healthy subjects assessed by a convenient single-time-point oral midazolam (MDZ) phenotyping strategy. cholest-5-ene-3,4-diol 54-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-107 26805594-0 2016 Use of 4beta-hydroxycholesterol in animal and human plasma samples as a biomarker for CYP3A induction. cholest-5-ene-3,4-diol 7-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 86-91 26805594-1 2016 BACKGROUND: 4beta-hydroxycholesterol (4betaHC) has recently been proposed as a potential endogenous biomarker for CYP3A activity. cholest-5-ene-3,4-diol 12-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-119 26805594-1 2016 BACKGROUND: 4beta-hydroxycholesterol (4betaHC) has recently been proposed as a potential endogenous biomarker for CYP3A activity. cholest-5-ene-3,4-diol 38-45 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-119 26805594-4 2016 CONCLUSION: These assays were applied to multiple studies and demonstrated potential applications of 4betaHC as a CYP3A biomarker across preclinical and clinical settings. cholest-5-ene-3,4-diol 101-108 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-119 26654672-0 2015 CYP3A activity based on plasma 4beta-hydroxycholesterol during the early postpartum period has an effect on the plasma disposition of amlodipine. cholest-5-ene-3,4-diol 31-55 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 26654672-1 2015 This study aimed to evaluate plasma 4beta-hydroxycholesterol as an endogenous marker of CYP3A4/5 activity in early postpartum women and its impact on the plasma disposition of amlodipine. cholest-5-ene-3,4-diol 36-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-94 26654672-10 2015 In conclusion, early postpartum women possessed higher CYP3A activity based on plasma 4beta-hydroxycholesterol and had a large pharmacokinetic variability in amlodipine. cholest-5-ene-3,4-diol 86-110 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-60 25096076-0 2014 Pharmacokinetic and pharmacogenomic modelling of the CYP3A activity marker 4beta-hydroxycholesterol during efavirenz treatment and efavirenz/rifampicin co-treatment. cholest-5-ene-3,4-diol 75-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-58 24839948-11 2014 CONCLUSIONS: Both 6betaCR and 4betaHC levels showed a good dynamic response range upon strong CYP3A4 induction with rifampicin. cholest-5-ene-3,4-diol 30-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 94-100 24839948-12 2014 Because of lower inter- and intrasubject variability, 4betaHC appeared more reliable and better predictive of CYP3A4 activity compared with 6betaCR. cholest-5-ene-3,4-diol 54-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-116 24964282-0 2014 Evaluation of 4beta-Hydroxycholesterol as a Clinical Biomarker of CYP3A4 Drug Interactions Using a Bayesian Mechanism-Based Pharmacometric Model. cholest-5-ene-3,4-diol 14-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-72 24964282-1 2014 A Bayesian mechanism-based pharmacokinetic/pharmacodynamic model of cytochrome P450 3A4 (CYP3A4) activity was developed based on a clinical study of the effects of ketoconazole and rifampin on midazolam exposure and plasma 4beta-hydroxycholesterol (4betaHC) concentrations. cholest-5-ene-3,4-diol 223-247 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-87 26574235-0 2016 4beta-hydroxycholesterol correlates with dose but not steady-state concentration of carbamazepine: indication of intestinal CYP3A in biomarker formation? cholest-5-ene-3,4-diol 0-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 124-129 26574235-1 2016 AIM: 4beta-hydroxycholesterol (4betaOHC) is an endogenous CYP3A(4) biomarker, which is elevated by use of the CYP3A4 inducer carbamazepine. cholest-5-ene-3,4-diol 5-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 58-63 26574235-1 2016 AIM: 4beta-hydroxycholesterol (4betaOHC) is an endogenous CYP3A(4) biomarker, which is elevated by use of the CYP3A4 inducer carbamazepine. cholest-5-ene-3,4-diol 5-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-116 26773964-2 2015 The aim of this study was to evaluate the influence of CYP3A5 polymorphism on the increase in CYP3A activity after living kidney transplantation, by measuring the plasma concentration of 4beta-hydroxycholesterol. cholest-5-ene-3,4-diol 187-211 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-60 26119961-0 2015 4beta-hydroxycholesterol as an endogenous CYP3A marker in cancer patients treated with taxanes. cholest-5-ene-3,4-diol 0-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 42-47 26119961-3 2015 In this study, we evaluated the endogenous CYP3A4 marker 4beta-hydroxycholesterol (4beta-OHC) as a potential individual taxane PK predictor. cholest-5-ene-3,4-diol 57-81 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-49 24837659-0 2014 Validation of 4beta-hydroxycholesterol and evaluation of other endogenous biomarkers for the assessment of CYP3A activity in healthy subjects. cholest-5-ene-3,4-diol 14-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 107-112 24837659-12 2014 CONCLUSIONS: Changes in plasma 4betaHC can be utilized as a surrogate for MDZ PK after multiple doses of potent CYP3A inducers. cholest-5-ene-3,4-diol 31-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 112-117 24837659-13 2014 There is a more limited dynamic range for 4betaHC for assessment of potential CYP3A inhibitors. cholest-5-ene-3,4-diol 42-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 78-83 24964282-1 2014 A Bayesian mechanism-based pharmacokinetic/pharmacodynamic model of cytochrome P450 3A4 (CYP3A4) activity was developed based on a clinical study of the effects of ketoconazole and rifampin on midazolam exposure and plasma 4beta-hydroxycholesterol (4betaHC) concentrations. cholest-5-ene-3,4-diol 249-256 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-87 24964282-1 2014 A Bayesian mechanism-based pharmacokinetic/pharmacodynamic model of cytochrome P450 3A4 (CYP3A4) activity was developed based on a clinical study of the effects of ketoconazole and rifampin on midazolam exposure and plasma 4beta-hydroxycholesterol (4betaHC) concentrations. cholest-5-ene-3,4-diol 249-256 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 24964282-2 2014 Simulations from the model demonstrated that the dynamic range of 4betaHC as a biomarker of CYP3A4 induction or inhibition was narrower than that of midazolam; an inhibitor that increases midazolam area under the curve by 20-fold may only result in a 20% decrease in 4betaHC after 14 days of dosing. cholest-5-ene-3,4-diol 66-73 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 92-98 24964282-3 2014 Likewise, an inducer that elevates CYP3A4 activity by 1.2-fold would reduce the area under the curve of midazolam by 50% but would only increase 4betaHC levels by 20% after 14 days of dosing. cholest-5-ene-3,4-diol 145-152 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 35-41 24861746-1 2014 4beta-Hydroxycholesterol (4beta-HC) has been proposed as a new endogenous biomarker for cytochrome P450 3A4/5 activity. cholest-5-ene-3,4-diol 0-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-107 24861746-1 2014 4beta-Hydroxycholesterol (4beta-HC) has been proposed as a new endogenous biomarker for cytochrome P450 3A4/5 activity. cholest-5-ene-3,4-diol 26-34 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-107 24595680-11 2014 The results suggest that 4beta-hydroxycholesterol can be used as an endogenous biomarker to identify strong CYP3A inducers in cynomolgus monkeys, which may help to evaluate drug-drug interaction potential of drug candidates in preclinical settings. cholest-5-ene-3,4-diol 25-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 108-113 23386704-1 2013 The primary aim was to study the relationship between individual serum levels of 25-hydroxyvitamin D and 4beta-hydroxycholesterol, which is an endogenous biomarker of the drug-metabolizing CYP3A enzymes. cholest-5-ene-3,4-diol 105-129 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 189-194 23833241-3 2013 In this study, we evaluated the effect of renal function on CYP3A activity after kidney transplantation in patients with end-stage renal disease (ESRD) by measuring the change in CYP3A activity using plasma concentration of 4beta-hydroxycholesterol as a biomarker. cholest-5-ene-3,4-diol 224-248 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-65 23674608-0 2013 Comparison of endogenous 4beta-hydroxycholesterol with midazolam as markers for CYP3A4 induction by rifampicin. cholest-5-ene-3,4-diol 25-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-86 23386704-0 2013 Serum levels of 25-hydroxyvitamin D and the CYP3A biomarker 4beta-hydroxycholesterol in a high-dose vitamin D supplementation study. cholest-5-ene-3,4-diol 60-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 44-49 24595680-0 2014 4beta-Hydroxycholesterol as an endogenous biomarker of CYP3A activity in cynomolgus monkeys. cholest-5-ene-3,4-diol 0-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-60 24595680-1 2014 It has been proposed that in humans 4beta-hydroxycholesterol is formed mainly by CYP3A-catalyzed metabolism of cholesterol and thus may serve as an endogenous marker for CYP3A activity. cholest-5-ene-3,4-diol 36-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-86 24595680-1 2014 It has been proposed that in humans 4beta-hydroxycholesterol is formed mainly by CYP3A-catalyzed metabolism of cholesterol and thus may serve as an endogenous marker for CYP3A activity. cholest-5-ene-3,4-diol 36-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 170-175 24595680-3 2014 In the current study, the potential application of 4beta-hydroxycholesterol as an endogenous biomarker of CYP3A in response to drug treatment was evaluated in cynomolgus monkeys. cholest-5-ene-3,4-diol 51-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 106-111 24595680-4 2014 Following multiple oral administration of rifampicin (a known CYP3A inducer) at 15 mg/kg/d in cynomolgus monkeys, the mean serum 4beta-hydroxycholesterol levels increased 4-fold from the baseline of 55.3 +- 21.7 to 221 +- 53.4 ng/ml. cholest-5-ene-3,4-diol 129-153 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-67 23089673-1 2013 We investigated the effects of pharmacogenetic variations and efavirenz pharmacokinetics on inter-individual differences in the extent of CYP3A induction by efavirenz using 4beta-hydroxycholesterol/cholesterol (4beta-OHC/Chol) as a marker for CYP3A induction. cholest-5-ene-3,4-diol 173-197 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 138-143 23386704-11 2013 However, the negative correlation between CRP and 4beta-hydroxycholesterol supports earlier experimental results that inflammation may suppress hepatic CYP3A activity, a finding of potentially high clinical relevance that warrants further exploration. cholest-5-ene-3,4-diol 50-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 152-157 21507593-1 2011 A novel liquid chromatography-tandem mass spectrometry method is described for the quantitative determination of the endogenous CYP 3A4/5 marker 4beta-hydroxycholesterol in human K(2)-EDTA plasma. cholest-5-ene-3,4-diol 145-169 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 128-135 21728364-1 2011 It has recently been proposed that plasma levels of 4beta-hydroxycholesterol (4betaHC) may be indicative of cytochrome P450 3A4 (P450 3A) activity and therefore could be used to probe for P450 3A-mediated drug-drug interactions. cholest-5-ene-3,4-diol 52-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 108-127 21728364-1 2011 It has recently been proposed that plasma levels of 4beta-hydroxycholesterol (4betaHC) may be indicative of cytochrome P450 3A4 (P450 3A) activity and therefore could be used to probe for P450 3A-mediated drug-drug interactions. cholest-5-ene-3,4-diol 78-85 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 108-127 19954708-0 2009 4beta-hydroxycholesterol as a marker of CYP3A4 inhibition in vivo - effects of itraconazole in man. cholest-5-ene-3,4-diol 0-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-46 21219398-0 2011 4beta-Hydroxycholesterol, an endogenous marker of CYP3A4/5 activity in humans. cholest-5-ene-3,4-diol 0-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 50-56 21219398-1 2011 We have proposed that 4beta-hydroxycholesterol (4beta-OHC) may be used as an endogenous marker of CYP3A activity. cholest-5-ene-3,4-diol 22-46 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-103 20197489-0 2010 Does the long plasma half-life of 4beta-hydroxycholesterol impact its utility as a cytochrome P450 3A (CYP3A) metric? cholest-5-ene-3,4-diol 34-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-101 20197489-0 2010 Does the long plasma half-life of 4beta-hydroxycholesterol impact its utility as a cytochrome P450 3A (CYP3A) metric? cholest-5-ene-3,4-diol 34-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 103-108 20197489-1 2010 Plasma 4beta-hydroxycholesterol (4betaHC) has been proposed as an endogenous marker of cytochrome P450 3A (CYP3A). cholest-5-ene-3,4-diol 7-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-105 20197489-1 2010 Plasma 4beta-hydroxycholesterol (4betaHC) has been proposed as an endogenous marker of cytochrome P450 3A (CYP3A). cholest-5-ene-3,4-diol 7-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 107-112 20197489-1 2010 Plasma 4beta-hydroxycholesterol (4betaHC) has been proposed as an endogenous marker of cytochrome P450 3A (CYP3A). cholest-5-ene-3,4-diol 33-40 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-105 20197489-1 2010 Plasma 4beta-hydroxycholesterol (4betaHC) has been proposed as an endogenous marker of cytochrome P450 3A (CYP3A). cholest-5-ene-3,4-diol 33-40 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 107-112 20197489-2 2010 To assess its utility as a CYP3A metric, a pharmacokinetic model, assuming no alteration in cholesterol plasma concentrations, was developed to simulate the effect of CYP3A induction and inhibition on 4betaHC plasma levels under different treatment durations. cholest-5-ene-3,4-diol 201-208 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 167-172 20197489-5 2010 On the other hand, simulations indicated that at least 2 weeks of dosing would be needed to detect the potent inhibition of CYP3A (maximal ~40% decrease in 4betaHC plasma levels). cholest-5-ene-3,4-diol 156-163 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 124-129 20231858-10 2011 A clear gene-dose effect implies plasma 4beta-hydroxycholesterol level as a useful endogenous biomarker for total CYP3A activity (CYP3A5 plus CYP3A4) whereas the omeprazole/omeprazole sulfone ratio reflects mainly CYP3A4 activity. cholest-5-ene-3,4-diol 40-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-119 20231858-10 2011 A clear gene-dose effect implies plasma 4beta-hydroxycholesterol level as a useful endogenous biomarker for total CYP3A activity (CYP3A5 plus CYP3A4) whereas the omeprazole/omeprazole sulfone ratio reflects mainly CYP3A4 activity. cholest-5-ene-3,4-diol 40-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 142-148 20231858-10 2011 A clear gene-dose effect implies plasma 4beta-hydroxycholesterol level as a useful endogenous biomarker for total CYP3A activity (CYP3A5 plus CYP3A4) whereas the omeprazole/omeprazole sulfone ratio reflects mainly CYP3A4 activity. cholest-5-ene-3,4-diol 40-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 214-220 19954708-2 2009 Here, we study the potential endogenous serum marker of CYP3A4 activity, 4beta-hydroxycholesterol, during therapy with itraconazole. cholest-5-ene-3,4-diol 73-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 19954708-9 2009 Absolute and cholesterol-corrected concentrations of 4beta-hydroxycholesterol, formed by CYP3A4-mediated oxidation, decreased significantly during both cycles, on average by 29.1% (p = 0.0006) and 20.8% (p = 0.0062), respectively. cholest-5-ene-3,4-diol 53-77 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 19954708-11 2009 CONCLUSIONS: In conclusion, 4beta-hydroxycholesterol appears to be a sensitive endogenous surrogate marker in human serum for inhibition of CYP3A4 by itraconazole. cholest-5-ene-3,4-diol 28-52 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 140-146 19006545-0 2009 4beta-hydroxycholesterol as an endogenous marker for CYP3A4/5 activity. cholest-5-ene-3,4-diol 0-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-59 19458613-0 2009 Plasma 4beta-hydroxycholesterol: an endogenous CYP3A metric? cholest-5-ene-3,4-diol 7-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 47-52 19006545-3 2009 We have previously shown that plasma 4beta-hydroxycholesterol continues to increase for several weeks after maximal induction of CYP3A4/5 by carbamazepine at the dose given. cholest-5-ene-3,4-diol 37-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 129-135 19006545-4 2009 In the present study we aimed to determine the time course of the decrease in plasma 4beta-hydroxycholesterol after termination of induction of CYP3A4/5 by rifampicin. cholest-5-ene-3,4-diol 85-109 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 144-150 19006545-14 2009 CONCLUSIONS: After termination of induction of CYP3A4/5, plasma 4beta-hydroxycholesterol levels decreased slowly during 8 weeks. cholest-5-ene-3,4-diol 64-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 47-53 11514559-0 2001 Antiepileptic drugs increase plasma levels of 4beta-hydroxycholesterol in humans: evidence for involvement of cytochrome p450 3A4. cholest-5-ene-3,4-diol 46-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-129 18279471-1 2008 WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT: CYP3A4 converts cholesterol into 4beta-hydroxycholesterol. cholest-5-ene-3,4-diol 75-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 42-48 18279471-2 2008 We have suggested that 4beta-hydroxycholesterol could be used as a clinical marker for CYP3A4 activity aiding in dose adjustments. cholest-5-ene-3,4-diol 23-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-93 18279471-4 2008 WHAT THIS STUDY ADDS: The concentration of 4beta-hydroxycholesterol increases very slowly during CYP3A4/5 induction in paediatric patients. cholest-5-ene-3,4-diol 43-67 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-103 18300941-12 2008 Both 4beta-hydroxycholesterol and quinine/3-hydroxyquinine metabolic ratio showed a higher CYP3A activity in women than in men. cholest-5-ene-3,4-diol 5-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 91-96 18300941-13 2008 The results give strong evidence that the plasma concentration of 4beta-hydroxycholesterol may be used as an endogenous marker of CYP3A activity (CYP3A4+5). cholest-5-ene-3,4-diol 66-90 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 130-135 18300941-13 2008 The results give strong evidence that the plasma concentration of 4beta-hydroxycholesterol may be used as an endogenous marker of CYP3A activity (CYP3A4+5). cholest-5-ene-3,4-diol 66-90 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 146-152 18458892-0 2008 CYP3A induction and inhibition by different antiretroviral regimens reflected by changes in plasma 4beta-hydroxycholesterol levels. cholest-5-ene-3,4-diol 99-123 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 18458892-1 2008 OBJECTIVE AND METHODS: A member of the major human cytochrome P450 superfamily of hemoproteins, CYP3A4/5, converts cholesterol into 4beta-hydroxycholesterol. cholest-5-ene-3,4-diol 132-156 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 96-102 18458892-7 2008 CONCLUSION: Changes in plasma 4beta-hydroxycholesterol following the initiation of efavirenz- or atazanavir/ritonavir-based antiretroviral therapy reflected the respective net increase and decrease of CYP3A activity of these regimens. cholest-5-ene-3,4-diol 30-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 201-206 18300941-0 2008 4Beta-hydroxycholesterol is a new endogenous CYP3A marker: relationship to CYP3A5 genotype, quinine 3-hydroxylation and sex in Koreans, Swedes and Tanzanians. cholest-5-ene-3,4-diol 0-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-50 11514559-7 2001 Recombinant CYP3A4 was shown to convert cholesterol to 4beta-hydroxycholesterol, whereas no conversion was observed with CYP1A2, CYP2C9, or CYP2B6. cholest-5-ene-3,4-diol 55-79 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 12-18 34572915-0 2021 CYP3A Activity in End-of-Life Cancer Patients Measured by 4beta-Hydroxycholesterol/cholesterol Ratio, in Men and Women. cholest-5-ene-3,4-diol 58-82 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 33822485-4 2021 The in vivo CYP3A4 induction effect of ivosidenib was quantified using 4beta-hydroxycholesterol and was subsequently verified with the PK data from an ivosidenib and venetoclax combination study. cholest-5-ene-3,4-diol 71-95 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 12-18 16847425-5 2006 The plasma concentration of 4beta-hydroxycholesterol, an endogenous marker of CYP3A4 activity, was measured before and after administration of 600 mg rifampicin once daily for 9-11 days. cholest-5-ene-3,4-diol 28-52 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 78-84 34580385-6 2021 We measured CYP3A4 activity using 4beta-hydroxycholesterol, an endogenous metabolite. cholest-5-ene-3,4-diol 34-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 12-18 34572915-2 2021 The aim of this study was to investigate if the CYP3A activity, measured by the endogenous marker 4beta-hydroxycholesterol/cholesterol ratio (4beta-OHC/C), is changed during the last weeks and days of life in men and women. cholest-5-ene-3,4-diol 98-122 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 48-53 35181316-1 2022 4beta-Hydroxycholesterol (4beta-OHC) is formed by CYP3A4 and CYP3A5 and has drawn attention as an endogenous phenotyping probe for CYP3A activity. cholest-5-ene-3,4-diol 0-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 50-56 35181316-1 2022 4beta-Hydroxycholesterol (4beta-OHC) is formed by CYP3A4 and CYP3A5 and has drawn attention as an endogenous phenotyping probe for CYP3A activity. cholest-5-ene-3,4-diol 0-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 131-136 33201347-1 2021 PURPOSE: The antifungal drugs ketoconazole and itraconazole reduce serum concentrations of 4beta-hydroxycholesterol, which is a validated marker for hepatic cytochrome P450 (CYP) 3A4 activity. cholest-5-ene-3,4-diol 91-115 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 157-182