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50 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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CYP3A4
cytochrome P450 family 3 subfamily A member 4
Chromosome 7 · 7q22.1
NCBI Gene: 1576Ensembl: ENSG00000160868.17HGNC: HGNC:2637UniProt: P08684
965PubMed Papers
21Diseases
3Drugs
2Pathogenic Variants
FUNCTIONAL ROLE
Hub Gene
RESEARCH IMPACT
Highly Studied
CLINICAL
FDA Approved TargetOMIM Disease Gene
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
monooxygenase activityvitamin D metabolic processvitamin D catabolic processretinol metabolic processHIV infectionHIV-1 infectionchronic hepatitis C virus infectionhepatitis C virus infection
✦AI Summary

CYP3A4 is a cytochrome P450 monooxygenase that catalyzes oxidative metabolism of endogenous substrates and xenobiotics through insertion of molecular oxygen into carbon-hydrogen bonds, with electrons provided by NADPH via cytochrome P450 reductase 1. Functionally, CYP3A4 metabolizes approximately 30-50% of marketed drugs, making it the most abundant hepatic and intestinal phase I enzyme 23. Beyond drug metabolism, CYP3A4 catalyzes hydroxylation of estrogens (2-hydroxy and 16α-hydroxylated estrone and estradiol), oxidative deactivation of testosterone to 2β- and 6β-hydroxytestosterones, formation of oxysterols from cholesterol, and hydroxylation of polyunsaturated fatty acids 456. CYP3A4 also metabolizes retinoids, catalyzing the rate-limiting conversion of all-trans-retinol to all-trans-retinal, and inactivates calcitriol (active vitamin D) 78. Genetic polymorphisms cause significant inter-individual variability in enzymatic activity, leading to altered drug efficacy or toxicity requiring personalized dosage adjustments 2. Drug-drug interactions involving CYP3A4 inhibitors (macrolide antibiotics, antiretrovirals) or inducers (rifampin, phenytoin) are clinically important, potentially causing unfavorable or fatal outcomes 3. Rare loss-of-function variants have been documented 9. Clock gene expression (DBP) regulates CYP3A4 activity in response to benzodiazepine exposure 10.

Sources cited
1
CYP3A4 is a cytochrome P450 monooxygenase that catalyzes oxidative metabolism of endogenous substrates and xenobiotics through insertion of molecular oxygen into carbon-hydrogen bonds, with electrons provided by NADPH via cytochrome P450 reductase .
PMID: 21490593
2
Functionally, CYP3A4 metabolizes approximately 30-50% of marketed drugs, making it the most abundant hepatic and intestinal phase I enzyme , .
PMID: 39650550
3
Functionally, CYP3A4 metabolizes approximately 30-50% of marketed drugs, making it the most abundant hepatic and intestinal phase I enzyme , .
PMID: 18473749
4
Beyond drug metabolism, CYP3A4 catalyzes hydroxylation of estrogens (2-hydroxy and 16α-hydroxylated estrone and estradiol), oxidative deactivation of testosterone to 2β- and 6β-hydroxytestosterones, formation of oxysterols from cholesterol, and hydroxylation of polyunsaturated fatty acids , , .
PMID: 12865317
5
Beyond drug metabolism, CYP3A4 catalyzes hydroxylation of estrogens (2-hydroxy and 16α-hydroxylated estrone and estradiol), oxidative deactivation of testosterone to 2β- and 6β-hydroxytestosterones, formation of oxysterols from cholesterol, and hydroxylation of polyunsaturated fatty acids , , .
PMID: 15373842
6
Beyond drug metabolism, CYP3A4 catalyzes hydroxylation of estrogens (2-hydroxy and 16α-hydroxylated estrone and estradiol), oxidative deactivation of testosterone to 2β- and 6β-hydroxytestosterones, formation of oxysterols from cholesterol, and hydroxylation of polyunsaturated fatty acids , , .
PMID: 21576599
7
CYP3A4 also metabolizes retinoids, catalyzing the rate-limiting conversion of all-trans-retinol to all-trans-retinal, and inactivates calcitriol (active vitamin D) , .
PMID: 10681376
8
CYP3A4 also metabolizes retinoids, catalyzing the rate-limiting conversion of all-trans-retinol to all-trans-retinal, and inactivates calcitriol (active vitamin D) , .
PMID: 29461981
9
Rare loss-of-function variants have been documented .
PMID: 24926778
10
Clock gene expression (DBP) regulates CYP3A4 activity in response to benzodiazepine exposure .
PMID: 37072025
Disease Associationsⓘ21
HIV infectionOpen Targets
0.61Moderate
HIV-1 infectionOpen Targets
0.59Moderate
chronic hepatitis C virus infectionOpen Targets
0.57Moderate
hepatitis C virus infectionOpen Targets
0.55Moderate
infectionOpen Targets
0.52Moderate
COVID-19Open Targets
0.42Moderate
AIDSOpen Targets
0.41Moderate
Hypocalcemic vitamin D-resistant ricketsOpen Targets
0.40Weak
viral diseaseOpen Targets
0.37Weak
neurodegenerative diseaseOpen Targets
0.37Weak
hepatitis D virus infectionOpen Targets
0.34Weak
coronavirus infectious diseaseOpen Targets
0.27Weak
pneumocystosisOpen Targets
0.26Weak
Kaposi's sarcomaOpen Targets
0.20Weak
Middle East respiratory syndromeOpen Targets
0.18Weak
cancerOpen Targets
0.11Weak
hepatocellular carcinomaOpen Targets
0.11Weak
chronic kidney diseaseOpen Targets
0.10Suggestive
long COVID-19Open Targets
0.09Suggestive
breast cancerOpen Targets
0.09Suggestive
Vitamin D-dependent rickets 3UniProt
Pathogenic Variants2
NM_017460.6(CYP3A4):c.902T>C (p.Ile301Thr)Pathogenic
Vitamin D-dependent rickets, type 3
★☆☆☆2022→ Residue 301
NM_017460.6(CYP3A4):c.1095ATT[1] (p.Leu366del)Pathogenic
Familial hypercholesterolemia
☆☆☆☆2022→ Residue 366
View on ClinVar ↗
Drug Targets3
COBICISTATApproved
Cytochrome P450 3A inhibitor
HIV-1 infection
RITONAVIRApproved
Cytochrome P450 3A inhibitor
HIV infection
TABIMORELINPhase II
Cytochrome P450 3A4 inhibitor
Related Genes
FMO1Protein interaction98%FMO4Protein interaction98%UGT1A4Protein interaction98%UGT1A8Protein interaction98%CBR1Protein interaction98%CBR3Protein interaction98%
Tissue Expression6 tissues
Liver
100%
Ovary
0%
Lung
0%
Heart
0%
Brain
0%
Bone Marrow
0%
Gene Interaction Network
Click a node to explore
CYP3A4FMO1FMO4UGT1A4UGT1A8CBR1CBR3
PROTEIN STRUCTURE
Preparing viewer…
PDB5VCC · 1.70 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.82LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF0.61 [0.46–0.82]
RankingsWhere CYP3A4 stands among ~20K protein-coding genes
  • #172of 20,598
    Most Researched965 · top 1%
  • #496of 1,025
    FDA-Approved Drug Targets2
  • #4,186of 5,498
    Most Pathogenic Variants2
  • #6,919of 17,882
    Most Constrained (LOEUF)0.82
Genes detectedCYP3A4
Sources retrieved50 papers
Response time—
📄 Sources
50▼
1
CYP3A4 and CYP3A5: the crucial roles in clinical drug metabolism and the significant implications of genetic polymorphisms.
PMID: 39650550
PeerJ · 2024
1.00
2
Drugs behave as substrates, inhibitors and inducers of human cytochrome P450 3A4.
PMID: 18473749
Curr Drug Metab · 2008
0.90
3
Midazolam Intoxication in a Premature Neonate.
PMID: 32354497
Clin Ther · 2020
0.82
4
Grapefruit-medication interactions: forbidden fruit or avoidable consequences?
PMID: 23184849
CMAJ · 2013
0.80
5
Interplay of Vitamin D and CYP3A4 Polymorphisms in Endocrine Disorders and Cancer.
PMID: 35654576
Endocrinol Metab (Seoul) · 2022
0.78