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GENE:

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

i
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
Dual-Biosensor for Five Drugs Detection in Precision Oncology. (PubMed, Bionanoscience)
In this work, we propose a novel dual-biosensor platform for TDM, designed to simultaneously detect multiple chemotherapeutic agents-cyclophosphamide, ifosfamide, etoposide, methotrexate, and 5-fluorouracil-for precision oncology. By integrating MWCNTs with cytochrome P450 enzymes (CYP3A4 and CYP2B6), our platform achieves enhanced electron transfer and substrate specificity, enabling sensitive and selective detection of the five chemotherapeutic drugs, individually and in combination, within clinically relevant ranges. Designed for portability and rapid analysis, this dual-biosensor platform enables real-time, cost-effective drug monitoring at the point-of-care, advancing personalized cancer treatment with greater precision and accessibility.
Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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5-fluorouracil • cyclophosphamide • ifosfamide • etoposide IV • methotrexate
2d
Simultaneous Determination of Venetoclax and Posaconazole in Human Plasma by UPLC-MS/MS: Application to Therapeutic Drug Monitoring in Acute Myeloid Leukemia Patients. (PubMed, Drug Des Devel Ther)
The trough concentrations of venetoclax were 9326.88 ± 12,169.05 ng/mL in patients treated with venetoclax alone, and 31,623.55 ± 28,453.67 ng/mL in patients treated with venetoclax in combination with posaconazole. A rapid and simple method was established and successfully applied to the simultaneous determination of the concentrations of venetoclax and posaconazole in AML patients, providing a basis for TDM and clinical pharmacokinetic analysis of these drugs in AML patients.
Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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Venclexta (venetoclax) • Noxafil (posaconazole)
9d
Prevalence of actionable pharmacogenomic variants in Brazilian patients with cancer. (PubMed, Front Pharmacol)
Nearly all Brazilian patients with cancer carried at least one actionable PGx variant, highlighting the potential impact of PGx-guided therapy in oncology. These results underscore the value of integrating pharmacogenomic strategies into clinical practice in Brazil.
Clinical • Journal
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HER-2 (Human epidermal growth factor receptor 2) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • 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) • CYP3A5 (Cytochrome P450 Family 3 Subfamily A Member 5) • DPYD (Dihydropyrimidine Dehydrogenase) • NUDT15 (Nudix Hydrolase 15)
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EGFR positive
9d
Pharmacokinetics of Asciminib 200 mg in the Presence of a Strong CYP3A4 Inducer, Phenytoin, in Healthy Participants. (PubMed, Clin Pharmacokinet)
These data support that, considering its large therapeutic window, asciminib 200 mg twice daily can be used without any dose adjustment when co-administered with a strong CYP3A4 inducer drug. Furthermore, asciminib is not an OATP1B inhibitor up to this dose.
PK/PD data • Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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Scemblix (asciminib)
14d
Ifosfamide-Induced Encephalopathy in a Very Young Child With Rhabdomyosarcoma: Case Report and Literature Review. (PubMed, J Pediatr Hematol Oncol)
IIE is a rare but severe side effect of ifosfamide infusion, and clinical manifestations in children may be misunderstood. We speculate that pharmacogenetic testing may be warranted in very young children to prevent severe IIE.
Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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cyclophosphamide • ifosfamide
19d
Integrative metabolomics and network pharmacology reveal the antifibrotic mechanisms of Gurigumu-13 in a rat model of hepatic fibrosis. (PubMed, Clin Transl Oncol)
This study provides the first comprehensive evidence that Gurigumu-13 possesses significant hepatoprotective and antifibrotic properties. Its antifibrotic effects are mediated through the modulation of metabolic pathways and interactions with multiple molecular targets involved in inflammation, lipid metabolism, and oxidative stress. By integrating metabolomics with network pharmacology, this work offers novel insights into the mechanisms of Gurigumu-13 and supports its potential clinical application for treating liver fibrosis.
Preclinical • Journal • Metabolomic study
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PTGS2 (Prostaglandin-Endoperoxide Synthase 2) • PPARG (Peroxisome Proliferator Activated Receptor Gamma) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • PACERR (PTGS2 Antisense NFKB1 Complex-Mediated Expression Regulator RNA) • PPARA (Peroxisome Proliferator Activated Receptor Alpha)
21d
Gene expression-based machine learning model for diagnosis, prognosis, and treatment response prediction in hepatocellular carcinoma: a retrospective study. (PubMed, J Yeungnam Med Sci)
Our gene expression-based machine learning model provides a robust tool for HCC diagnosis, prognosis, and treatment response prediction, with potential as a supportive system for personalized clinical decision-making.
Retrospective data • Journal
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TOP2A (DNA topoisomerase 2-alpha) • CDK1 (Cyclin-dependent kinase 1) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • ADH1B (Alcohol Dehydrogenase 1B (Class I), Beta Polypeptide) • RACGAP1 (Rac GTPase activating protein 1)
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sorafenib
28d
Sustained Drug-Drug Interaction Between Cyclosporine and Apalutamide in a Patient With Metastatic Hormone-Sensitive Prostate Cancer: A Case Report and Evaluation of CYP3A4 Induction via Pregnane X Receptor Activation by Apalutamide. (PubMed, Case Rep Oncol Med)
A 75-year-old man with mHSPC was treated with Apa and leuprorelin. Apa induced CYP3A4 via the PXR pathway, leading to a sustained DDI with CsA. Careful monitoring is necessary when Apa is coadministered with CYP3A4 substrates.
Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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apalutamide • cyclosporine • leuprolide acetate for depot suspension
1m
Differential gene regulation by SR12813 and rifampicin: Insights into PXR and PPARγ activation and metabolic pathway modulation in LS180 colon cancer cells. (PubMed, Drug Metab Dispos)
SIGNIFICANCE STATEMENT: SR12813 activates both pregnane X receptor and peroxisome proliferator-activated receptor gamma, demonstrating dual nuclear receptor modulation in colon cancer cells. By linking xenobiotic metabolism with lipid and mitochondrial pathways, this work uncovers previously unreported receptor crosstalk and provides a mechanistic framework for how diverse ligands can differentially shape transcriptional programs relevant to drug metabolism and tumor biology.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • UGT1A1 (UDP glucuronosyltransferase family 1 member A1) • PPARG (Peroxisome Proliferator Activated Receptor Gamma) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • NR1I2 (Nuclear Receptor Subfamily 1 Group I Member 2)
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rifampicin
1m
Drug Interactions Between Direct Oral Anticoagulants and Nonsteroidal Anti-inflammatory Drugs: A Clinical Risk-Benefit Analysis With Focus on Special Populations. (PubMed, Am J Ther)
However, the clinical message should not be a blanket prohibition of NSAID use in anticoagulated patients. However, careful and judicious use, at the lowest effective dose and for the shortest necessary duration, should be considered in select clinical situations.
Journal • Benefit-risk assessment
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
1m
Phytochemical study of Homalanthus giganteus: isolation, antiproliferative activity, and computational mechanistic insights of tigliane diterpenes against colorectal cancer. (PubMed, Pharm Biol)
Six compounds were isolated from H. giganteus, with 4 exhibiting antiproliferative activity through PRKCA and GSK3β modulation. These findings provide the first phytochemical and mechanistic evidence that support H. giganteus as a promising source of active anti-colon cancer leads.
Journal
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STAT3 (Signal Transducer And Activator Of Transcription 3) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • PRKCA (Protein Kinase C Alpha)
1m
Effect of carbamazepine on the pharmacokinetics of vepdegestrant, a PROteolysis TArgeting Chimera estrogen receptor degrader, in healthy adults. (PubMed, Br J Clin Pharmacol)
Coadministration of multiple doses of carbamazepine 200 mg, a strong CYP3A4 inducer, with a single dose of vepdegestrant 200 mg resulted in a modest (36%) decrease in plasma vepdegestrant exposure. A single dose of vepdegestrant 200 mg was well tolerated in healthy adult participants.
PK/PD data • Journal
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ER (Estrogen receptor) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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vepdegestrant (ARV-471)