Evaluation of the Cytochrome P450 3A and P-glycoprotein Drug-Drug Interaction Potential of Futibatinib.
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DOI: 10.1002/cpdd.1259
Abstract: Futibatinib, a selective, irreversible fibroblast growth factor receptor 1-4 inhibitor, is being investigated for tumors harboring FGFR aberrations and was recently approved for the treatment of FGFR2 fusion/rearrangement-positive intrahepatic cholangiocarcinoma. In vitro studies identified cytochrome… read more here.
Keywords: cyp3a; plasma concentration; drug drug; cytochrome p450 ... See more keywords
Amenamevir: Studies of Potential CYP3A‐Mediated Pharmacokinetic Interactions With Midazolam, Cyclosporine, and Ritonavir in Healthy Volunteers
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DOI: 10.1002/cpdd.586
Abstract: Amenamevir (formerly ASP2151) is a helicase‐primase inhibitor being developed for the treatment of herpesvirus infection. Amenamevir is both a substrate and inducer of cytochrome P450 (CYP) 3A4. Three studies were done in healthy volunteers to… read more here.
Keywords: cyp3a mediated; cyp3a; healthy volunteers; geometric mean ... See more keywords
Impact of Inflammation on Midazolam Metabolism in Severe COVID‐19 Patients
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DOI: 10.1002/cpt.2698
Abstract: Midazolam is a benzodiazepine frequently used for sedation in patients hospitalized in the intensive care unit (ICU) for coronavirus disease 2019 (COVID‐19). This drug is primarily metabolized by cytochrome P450 3A (CYP3A) isoenzymes. Several studies… read more here.
Keywords: cyp3a; inflammation; metabolism; inflammation midazolam ... See more keywords
Pooled Population Pharmacokinetic Analyses of Venetoclax in Patients Across Indications and Healthy Subjects from Phase 1, 2 and 3 Clinical Trials.
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DOI: 10.1002/jcph.2248
Abstract: Following the decade long clinical investigation, venetoclax has accrued PK data across multiple populations and widely-ranging demographics, intrinsic, and extrinsic factors. We leveraged these rich data to systematically characterize venetoclax PK and assess covariate effects… read more here.
Keywords: indications healthy; cyp3a; pooled population; inhibitor ... See more keywords
A Clinical Cassette Dosing Study for Evaluating the Contribution of Hepatic OATPs and CYP3A to Drug-Drug Interactions
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DOI: 10.1007/s11095-017-2168-5
Abstract: PurposeTo demonstrate the relative importance of organic anion-transporting polypeptides (OATPs) and cytochrome P450 3A (CYP3A) in the hepatic elimination of substrate drugs.MethodsA cocktail of subtherapeutic doses of bosentan, repaglinide, clarithromycin, darunavir, simeprevir, and midazolam (CYP3A… read more here.
Keywords: drug interactions; cyp3a; clinical cassette; study ... See more keywords
Parathyroid hormone contributes to the down‐regulation of cytochrome P450 3A through the cAMP/PI3K/PKC/PKA/NF‐&kgr;B signaling pathway in secondary hyperparathyroidism
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DOI: 10.1016/j.bcp.2017.08.016
Abstract: ABSTRACT Chronic kidney disease (CKD), which affects, not only renal clearance, but also non‐renal clearance, is accompanied by a decline in renal function. Although it has been suggested that humoral factors, such as uremic toxins… read more here.
Keywords: pth; camp; cyp3a; pkc pka ... See more keywords
CYP3A suppression during diet-induced nonalcoholic fatty liver disease is independent of PXR regulation.
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DOI: 10.1016/j.cbi.2019.05.038
Abstract: Cytochrome P450 3A (CYP3A) activity is inhibited, and its expression is suppressed during many diseases, including nonalcoholic fatty liver disease (NAFLD). However, the mechanism is controversial. Here, we report that PXR may not take part… read more here.
Keywords: fatty liver; cyp3a; pxr; nonalcoholic fatty ... See more keywords
Effect of CYP3A inducer/inhibitor on pharmacokinetics of five alkaloids in Evodiae Fructus.
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DOI: 10.1016/j.cbi.2020.109146
Abstract: Evodiae Fructus (EF), the dried nearly mature scented fruit of Tetradium ruticarpum (A.Juss.) T.G.Hartley, was typically used to treat headache, abdominal pain, hernias, and menorrhagia for thousands of years. It had been reported to be… read more here.
Keywords: inhibitor; cyp3a; evodiae fructus; five alkaloids ... See more keywords
Acalabrutinib CYP3A mediated Drug-Drug Interactions: Clinical Evaluations and Physiologically-Based Pharmacokinetic Modeling to inform dose adjustment strategy.
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DOI: 10.1111/bcp.15278
Abstract: AIMS Clinical drug interaction studies with itraconazole and rifampicin demonstrated acalabrutinib is a sensitive substrate of CYP3A. A PBPK model was developed based on the data of these studies. One of the active CYP3A metabolite… read more here.
Keywords: study; drug; cyp3a; acp 5862 ... See more keywords
Time course of CYP3A activity during and after metamizole (dipyrone) in healthy volunteers.
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DOI: 10.1111/bcp.15720
Abstract: BACKGROUND AND PURPOSE In patients of all ages, metamizole is a frequently used analgesic. Recently, metamizole has been identified as an inducer of, among others, cytochrome P450 (CYP) 3A activity, but the time course of… read more here.
Keywords: cyp3a; time; discontinuation metamizole; activity ... See more keywords
Alternatives to rifampicin: A review and perspectives on the choice of strong CYP3A inducers for clinical drug–drug interaction studies
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DOI: 10.1111/cts.13357
Abstract: N‐Nitrosamine (NA) impurities are considered genotoxic and have gained attention due to the recall of several marketed drug products associated with higher‐than‐permitted limits of these impurities. Rifampicin is an index inducer of multiple cytochrome P450s… read more here.
Keywords: cyp3a; strong cyp3a; drug drug; alternatives rifampicin ... See more keywords