The CYP3A4 gene encodes an enzyme from the cytochrome P450 superfamily which is involved in metabolism of steroids (hormones and lipids) and various drugs.
CYP3A4 inhibitors
Antiarrhythmics Dronedaron
Antibiotics Erythromycin, Clarithromycin, Telithromycin
Antidepressants Nefazodon
Antimycotic drugs Itraconazol, Ketoconazol, Voriconazol
Protease inhibitors Indinavir, Nelfinavir, Ritonavir
Cytostatics Idelalisib, Ribocuclib
Other Grapefruitesaft
CYP3A4 inducer
Antibiotics Rifampicin
Antidiabetics Pioglitazon
Anticonvulsants Carbamazepin, Oxcarbazepin, Phenytoin
Antiretroviral drugs Efavirenz, Nevirapin
Glucocorticoids
Cytostatics Brigatinib, Enzalutamid
Tranquillizers Barbiturate, Phenobarbital
Other Hypericum, Modafinil
Clinic | Method | Carrier testing |
Turnaround | 5 days | |
Specimen type | genomic DNA |
Clinic | Method | Massive parallel sequencing |
Turnaround | 25 days | |
Specimen type | genomic DNA |
Clinic | Method | Genomic sequencing of the entire coding region |
Turnaround | 25 days | |
Specimen type | genomic DNA |
Clinic | Method | Multiplex Ligation-Dependent Probe Amplification |
Turnaround | 25 days | |
Specimen type | genomic DNA |
Disturbances of cytochrome p450 system | ||||
CYP1A2 | ||||
CYP2A6 | ||||
CYP2C9 | ||||
CYP2D6 | ||||
CYP3A4 | ||||
CYP4F2 | ||||
Siponimod intolerance | ||||
CYP2C9 | ||||
1. |
Dimaraki EV et al. (2003) Troglitazone induces CYP3A4 activity leading to falsely abnormal dexamethasone suppression test. |
2. |
Lehmann JM et al. (1998) The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions. |
3. |
Felix CA et al. (1998) Association of CYP3A4 genotype with treatment-related leukemia. |
4. |
Paris PL et al. (1999) Association between a CYP3A4 genetic variant and clinical presentation in African-American prostate cancer patients. |
5. |
Goodwin B et al. (1999) The orphan human pregnane X receptor mediates the transcriptional activation of CYP3A4 by rifampicin through a distal enhancer module. |
7. |
Xie W et al. (2000) Humanized xenobiotic response in mice expressing nuclear receptor SXR. |
8. |
Kittles RA et al. (2002) CYP3A4-V and prostate cancer in African Americans: causal or confounding association because of population stratification? |
9. |
Goodwin B et al. (2002) Transcriptional regulation of the human CYP3A4 gene by the constitutive androstane receptor. |
10. |
Zeigler-Johnson CM et al. (2002) Ethnic differences in the frequency of prostate cancer susceptibility alleles at SRD5A2 and CYP3A4. |
11. |
Tirona RG et al. (2003) The orphan nuclear receptor HNF4alpha determines PXR- and CAR-mediated xenobiotic induction of CYP3A4. |
12. |
Nebert DW et al. (1987) P450 genes: structure, evolution, and regulation. |
13. |
Masuyama H et al. (2003) Expression and potential roles of pregnane X receptor in endometrial cancer. |
14. |
Markowitz JS et al. (2003) Effect of St John's wort on drug metabolism by induction of cytochrome P450 3A4 enzyme. |
15. |
Loukola A et al. (2004) Comprehensive evaluation of the association between prostate cancer and genotypes/haplotypes in CYP17A1, CYP3A4, and SRD5A2. |
16. |
Gupta RP et al. (2004) CYP3A4 is a human microsomal vitamin D 25-hydroxylase. |
17. |
Williams PA et al. (2004) Crystal structures of human cytochrome P450 3A4 bound to metyrapone and progesterone. |
18. |
Hirota T et al. (2004) Allelic expression imbalance of the human CYP3A4 gene and individual phenotypic status. |
19. |
Gupta RP et al. (2005) CYP3A4 is a vitamin D-24- and 25-hydroxylase: analysis of structure function by site-directed mutagenesis. |
20. |
Schirmer M et al. (2006) Genetic signature consistent with selection against the CYP3A4*1B allele in non-African populations. |
21. |
Ekroos M et al. (2006) Structural basis for ligand promiscuity in cytochrome P450 3A4. |
22. |
van Herwaarden AE et al. (2007) Knockout of cytochrome P450 3A yields new mouse models for understanding xenobiotic metabolism. |
23. |
Thummel KE et al. (1998) In vitro and in vivo drug interactions involving human CYP3A. |
24. |
Paolini M et al. (1999) Co-carcinogenic effect of beta-carotene. |
25. |
Daly AK et al. (1992) Deficient nifedipine oxidation: a rare inherited trait associated with cystic fibrosis kindreds. |
26. |
Inoue K et al. (1992) Assignment of the human cytochrome P-450 nifedipine oxidase gene (CYP3A4) to chromosome 7 at band q22.1 by fluorescence in situ hybridization. |
27. |
Wolf CR et al. (1992) Relationship between the debrisoquine hydroxylase polymorphism and cancer susceptibility. |
28. |
Wrighton SA et al. (1992) The human hepatic cytochromes P450 involved in drug metabolism. |
29. |
Forrester LM et al. (1990) Evidence for involvement of multiple forms of cytochrome P-450 in aflatoxin B1 metabolism in human liver. |
30. |
Shimada T et al. (1989) Evidence for cytochrome P-450NF, the nifedipine oxidase, being the principal enzyme involved in the bioactivation of aflatoxins in human liver. |
31. |
Wrighton SA et al. (1989) Isolation and characterization of human fetal liver cytochrome P450HLp2: a third member of the P450III gene family. |
32. |
Spurr NK et al. (1989) The human cytochrome P450 CYP3 locus: assignment to chromosome 7q22-qter. |
33. |
Brooks BA et al. (1988) The gene CYP3 encoding P450pcn1 (nifedipine oxidase) is tightly linked to the gene COL1A2 encoding collagen type 1 alpha on 7q21-q22.1. |
34. |
Renwick AG et al. (1988) The pharmacokinetics of oral nifedipine--a population study. |
35. |
Gonzalez FJ et al. (1988) Human P450PCN1: sequence, chromosome localization, and direct evidence through cDNA expression that P450PCN1 is nifedipine oxidase. |
36. |
Schellens JH et al. (1988) Lack of bimodality in nifedipine plasma kinetics in a large population of healthy subjects. |
37. |
Molowa DT et al. (1986) Complete cDNA sequence of a cytochrome P-450 inducible by glucocorticoids in human liver. |
38. |
Watkins PB et al. (1985) Identification of an inducible form of cytochrome P-450 in human liver. |
39. |
Kleinbloesem CH et al. (1984) Variability in nifedipine pharmacokinetics and dynamics: a new oxidation polymorphism in man. |
40. |
Elshourbagy NA et al. (1980) Separation, purification, and characterization of a novel form of hepatic cytochrome P-450 from rats treated with pregnenolone-16 alpha-carbonitrile. |
41. |
Shet MS et al. (1993) Human cytochrome P450 3A4: enzymatic properties of a purified recombinant fusion protein containing NADPH-P450 reductase. |
42. |
Chen H et al. (1996) Increased risk for myelodysplastic syndromes in individuals with glutathione transferase theta 1 (GSTT1) gene defect. |
43. |
Lown KS et al. (1997) Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression. |
44. |
Rebbeck TR et al. (1998) Modification of clinical presentation of prostate tumors by a novel genetic variant in CYP3A4. |
45. |
Orphanet article Orphanet ID 423802 |
46. |
NCBI article NCBI 1576 |
47. |
OMIM.ORG article Omim 124010 |
48. |
Wikipedia article Wikipedia EN (CYP3A4) |