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GENE:

CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)

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Other names: Cytochrome P450 Family 3 Subfamily A Member 4, Cytochrome P450, Subfamily IIIA (Niphedipine Oxidase), Polypeptide 4, Cytochrome P450, Family 3, Subfamily A, Polypeptide 4, Albendazole Monooxygenase (Sulfoxide-Forming), 1,4-Cineole 2-Exo-Monooxygenase, 1,8-Cineole 2-Exo-Monooxygenase, Cholesterol 25-Hydroxylase, Albendazole Sulfoxidase, Quinine 3-Monooxygenase, Cytochrome P450 NF-25, Cytochrome P450-PCN1, Cytochrome P450 3A4, Cytochrome P450 3A3, Cytochrome P450 HLp, Nifedipine Oxidase, CYPIIIA3, CYPIIIA4, CYP3A3, Cytochrome P450, Subfamily IIIA (Niphedipine Oxidase), Polypeptide 3, Taurochenodeoxycholate 6-Alpha-Hydroxylase, Glucocorticoid-Inducible P450, P450-III, Steroid Inducible, P450PCN1, P450C3, CYP3A4, CYP3A, NF-25, VDDR3, CP33, CP34, HLP
2d
Trial completion • Enrollment change
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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midazolam hydrochloride
3d
Evaluation of in Vitro Cytotoxicity and Induction Potential of Açaí (Euterpe oleracea) Extracts in Human Hepatocytes. (PubMed, J Diet Suppl)
Preliminary functional assays also showed minimal impact on P-gp and OATP activity. While preliminary, this study provides a comprehensive evaluation of açaí-mediated modulation of key pharmacokinetic pathways and underscores the need for rigorous assessment of botanical extracts to better predict potential botanical-drug interactions.
Preclinical • Journal
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CYP1A2 (Cytochrome P450, family 1, subfamily A, polypeptide 2) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
5d
Etoposide dosing challenges in a testicular cancer patient with hepatic impairment and drug-drug interactions-a case report. (PubMed, Cancer Chemother Pharmacol)
This case shows that monitoring of etoposide plasma concentrations can be beneficial in complex clinical scenarios involving organ dysfunction and/or potential drug-drug interactions. This is especially important in curative treatment to avoid under dosing. This case report highlights the challenges of dosing etoposide in a patient with cystic fibrosis and liver cirrhosis who is taking multiple drugs that may interact with etoposide. The patient should be monitored closely on how the treatment is tolerated and the dose should be adjusted accordingly.
Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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cisplatin • etoposide IV
6d
Pharmacotherapeutic considerations of selective estrogen receptor modulators for vascular protection. (PubMed, Front Pharmacol)
Among the most studied SERMs are Tamoxifen and Raloxifene. The pharmacological profile of SERMs therefore reflects a delicate equilibrium between receptor-mediated vascular protection and thrombotic liability. Indeed, their raison d'être increasingly extends beyond oncology into cardiovascular endocrine pharmacology, where they serve as prototypes for designing next-generation agents with optimized receptor selectivity and safer vascular outcomes.
Review • Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • NOS3 (Nitric oxide synthase 3)
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tamoxifen • raloxifene hydrochloride
9d
Effect of apatinib on albendazole metabolism in vitro and in vivo. (PubMed, Bioorg Chem)
For the metabolites albendazole sulfoxide and hydroxyalbendazole, apatinib caused significant increases in AUC(0-t), AUC(0-∞), and Tmax, while a significant decrease in CLz/F. In summary, apatinib could inhibit the metabolism of albendazole in vitro and in vivo, so albendazole should be closely monitored for adverse effects when used in combination with apatinib and discontinued if necessary.
Preclinical • Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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AiTan (rivoceranib)
11d
A New Histology-Based Prognostic Index for Acute Lymphoblastic Leukemia: Preliminary Results of the "ALL Urayasu Classification". (PubMed, J Clin Med)
n = 2. The Urayasu classification for ALL is considered reliable for predicting the prognosis of patients with ALL after the initial Hyper CVAD/MA remission induction therapy.
Journal
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SLC29A1 (Solute Carrier Family 29 Member 1) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • AKR1B10 (Aldo-Keto Reductase Family 1 Member B10)
12d
Comparative Proteomics Of Hepatocytes And Hepatic Cell Lines Using Swath-MS Reveals Significant Variations In Proteins Involved In Energy, Lipid, And Xenobiotic Metabolism. (PubMed, Curr Drug Metab)
This study highlights the potential of untargeted global proteomics in detecting differences in protein expression among various hepatic cell lines and provides a comprehensive database to inform the choice of the cell line in future studies.
Preclinical • Journal
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UGT1A1 (UDP glucuronosyltransferase family 1 member A1) • CYP2C9 (Cytochrome P450 Family 2 Subfamily C Member 9) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • UGT1A6 (UDP Glucuronosyltransferase Family 1 Member A6) • UGT2B15 (UDP Glucuronosyltransferase Family 2 Member B15) • UGT1A3 (UDP Glucuronosyltransferase Family 1 Member A3)
15d
Humanized liver mouse models in preclinical drug development: current status, translation challenges and emerging technologies. (PubMed, Drug Discov Today)
These models have been widely applied to MASLD/MASH, fibrosis, hepatocellular carcinoma and viral hepatitis research but remain constrained by the absence of intestinal CYP3A4 expression and functional immune compartments. Emerging approaches, including dual humanization, non-parenchymal cell supplementation, vascularized 3D bioprinting and application of patient-derived hepatocytes, combined with advanced in vitro and computational platforms, further strengthen translational fidelity, reduce R&D attrition and expand the scope for modeling complex metabolism-related diseases.
Preclinical • Review • Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
19d
Retrospection of the USFDA-Approved Halogenated Drugs and Their Implication in Medicinal Chemistry and Drug Discovery: A Perspective of Approved Drugs Between 2019 and 2024. (PubMed, Arch Pharm (Weinheim))
CYP3A4 is a major contributor in the metabolism of 6 drugs, followed by CYP3A (3), CYP1A2 (2), CYP3A4/5 (2), and one each by CYP2C9, UGT1A9, CYP2C8, aldehyde oxidase, and other non-CYP enzymes. The present medicinal chemistry perspective is thus expected to be a valuable read for the medicinal and allied sciences community.
FDA event • Review • Journal
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CYP1A2 (Cytochrome P450, family 1, subfamily A, polypeptide 2) • CYP2C9 (Cytochrome P450 Family 2 Subfamily C Member 9) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • UGT1A9 (UDP Glucuronosyltransferase Family 1 Member A9)
20d
Influence of pharmacokinetics-related polymorphisms on asciminib exposure in patients with Japanese chronic myeloid leukemia. (PubMed, Eur J Clin Pharmacol)
Overall, our findings showed that an adjustment of the initial asciminib dose may be needed based on genotyping information for the NR1I2 -25385C > T polymorphism and the body weight of the patient; however, further prospective studies are necessary.
PK/PD data • Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • ABCC2 (ATP Binding Cassette Subfamily C Member 2) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • NR1I2 (Nuclear Receptor Subfamily 1 Group I Member 2)
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Scemblix (asciminib)
21d
Aesculetin (6,7-dihydroxycoumarin) enhances the differentiation of human bone marrow-derived mesenchymal stem cells into functional hepatocyte-like cells. (PubMed, Sci Rep)
Importantly, further analysis revealed that the differentiation process promoted by aesculetin was associated with the activation of the STAT3 and STAT5 signaling pathways. Collectively, these findings underscore the pivotal role of aesculetin in promoting the hepatic differentiation of hBM-MSCs and demonstrate its potential as a key component for regenerative medicine applications in liver tissue engineering or stem cell-based therapies.
Journal
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CYP1A2 (Cytochrome P450, family 1, subfamily A, polypeptide 2) • SOX17 (SRY-Box Transcription Factor 17) • KRT19 (Keratin 19) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • FOXA2 (Forkhead Box A2) • CYP1A1 (Cytochrome P450 Family 1 Subfamily A Member 1)
24d
Effects of Oxygen-Permeable Plates on Cytochrome P450 and Flavin-Containing Monooxygenase in HepaRG Spheroid Cultures. (PubMed, Biol Pharm Bull)
Using clozapine, a low-clearance antipsychotic drug with limited metabolic elimination that is metabolized by monooxygenases, including CYP3A4 and flavin-containing monooxygenase (FMO), we observed an enhanced decline in clozapine levels in PMP plates compared with the clozapine levels seen in the conventional polystyrene plates...These results suggest that improved oxygenation enhances hepatic functionality in 3D cultures by maintaining cell viability and promoting the expression of drug-metabolizing enzymes. Therefore, the PMP plate-based spheroid model offers a practical and physiologically relevant platform for investigating drug metabolism and hepatotoxicity.
Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)