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   Articles with "cyp3a" as a keyword



Evaluation of the Cytochrome P450 3A and P-glycoprotein Drug-Drug Interaction Potential of Futibatinib.

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recommendations! Published in 2023 at "Clinical pharmacology in drug development"

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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recommendations! Published in 2018 at "Clinical Pharmacology in Drug Development"

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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recommendations! Published in 2022 at "Clinical Pharmacology and Therapeutics"

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
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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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recommendations! Published in 2023 at "Journal of clinical pharmacology"

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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recommendations! Published in 2017 at "Pharmaceutical Research"

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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recommendations! Published in 2017 at "Biochemical Pharmacology"

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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recommendations! Published in 2019 at "Chemico-biological interactions"

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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recommendations! Published in 2020 at "Chemico-biological interactions"

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

High-throughput assay to simultaneously evaluate activation of CYP3A and the direct and time-dependent inhibition of CYP3A, CYP2C9, and CYP2D6 using liquid chromatography-tandem mass spectrometry

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recommendations! Published in 2024 at "Xenobiotica"

DOI: 10.1080/00498254.2024.2308818

Abstract: Abstract In the early stages of drug discovery, adequate evaluation of the potential drug–drug interactions (DDIs) of drug candidates is important. Several CYP3A activators are known to lead to underestimation of DDIs. These compounds affect… read more here.

Keywords: inhibition; activation; drug; cyp3a ... 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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recommendations! Published in 2022 at "British journal of clinical pharmacology"

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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recommendations! Published in 2023 at "British journal of clinical pharmacology"

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