CYP3A Inhibitors
8 drugsAbout CYP3A
CYP3A is a key member of the cytochrome P450 superfamily, crucial for drug metabolism. These enzymes break down many medications, influencing their efficacy and safety profiles in patients.
CYP3A is a therapeutic target with moderate genetic support (max score 0.65), linked to hypocalcemic vitamin D-resistant rickets. Targeting CYP3A can be a strategic approach in various therapeutic areas.
CYP3A is targeted by eight FDA-approved drugs, including LOPINAVIR AND RITONAVIR, PREZCOBIX, GENVOYA and SYMTUZA. All drugs are small molecules, addressing infectious diseases and other therapeutic areas.
CYP3A Genetic Evidence Moderate
CYP3A has moderate genetic support with a max score of 0.65 for hypocalcemic vitamin D-resistant rickets.
Further investigation of the genetic link to hypocalcemic vitamin D-resistant rickets may reveal novel therapeutic opportunities.
Evidence Across Diseases
2 totalGWAS and other genetic studies link CYP3A4 to 2 diseases.
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for CYP3A4 colocalize with these GWAS traits, providing causal evidence that gene expression changes drive disease risk.
Understanding these scores
Association Score (0-1): Combines all evidence types (genetic, literature, drugs, animal models). Higher = more evidence linking target to disease. This is a ranking heuristic, not a confidence score.
L2G Score: Open Targets uses a machine learning model (Locus-to-Gene) to predict which gene is causal at each GWAS locus. L2G=0.5 means ~50% probability of being the causal gene. Only associations with L2G > 0.05 are included.
Odds Ratio (OR): From gene burden studies (UK Biobank, AstraZeneca PheWAS). Measures how loss-of-function variants affect disease risk. OR<1 = protective (inhibiting target may help), OR>1 = risk (losing function causes disease).
Beta (β): Effect size for continuous traits. β<0 = protective, β>0 = risk.
Clinical Translation (~1.8x): Based on Nelson et al. 2015: drug targets with genetic evidence have ~2x higher success rates in clinical trials. We estimate: Strong support (score ≥0.7) → ~1.8x, Moderate (0.3-0.7) → ~1.3x, Weak → baseline.
Colocalization (H4): Tests whether a GWAS signal and an eQTL/pQTL signal share the same causal variant. H4 is the posterior probability that both traits are associated AND share a causal variant. H4 > 0.8 = strong evidence that gene expression/protein levels drive disease risk. This links genetic variation → gene expression → disease, supporting the target-disease connection.
Top CYP3A Drugs
Six companies have approved drugs targeting CYP3A, including MACLEODS PHARMS LTD, AbbVie, and Johnson & Johnson.
The presence of multiple established players suggests a moderately competitive landscape with potential entry barriers.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| LOPINAVIR AND RITONAVIR | Cipla | 2016 | 1 |
| EVOTAZ | Bristol-Myers Squibb | 2015 | 1 |
| SYMTUZA | Johnson & Johnson | 2018 | 1 |
| PAXLOVID (COPACKAGED) | Pfizer | 2023 | 1 |
| PREZCOBIX | Johnson & Johnson | 2015 | 1 |
CYP3A Drug Modality Landscape
Modalities
Routes of Administration
CYP3A is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or fusion proteins could provide a competitive advantage.
CYP3A Clinical Trials 400 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on CYP3A. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 155 | 131 | 15 | 8 | 90% |
| Phase 2 | 95 | 74 | 14 | 7 | 84% |
| Phase 3 | 64 | 46 | 10 | 8 | 82% |
| Phase 4 | 86 | 62 | 16 | 8 | 79% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
CYP3A Drug Approval Timeline (2000 - 2023)
The first CYP3A-targeting drug was approved in 2000 (KALETRA), with the most recent approval in 2023 (PAXLOVID).
The continued approval of new drugs indicates sustained interest and potential for further innovation in this area.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 6 companies competing
- • Market share by company
Full Drug Portfolio
- • All 8 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 8-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 183 (51 companies)
- • Completion rates by condition
Full summary • All drugs • Genetic evidence • Trials • Timeline
How We Count Trials
- Trials: phase 1-4 interventional trials on ClinicalTrials.gov that started in 2008 or later and test an FDA-approved drug acting on CYP3A. A trial counts if an approved drug acting on CYP3A is in any arm, including as a comparator, and a trial that tests two such drugs counts once. Trials that test only unapproved drugs are not counted. A trial listed as phase 1/2 counts as phase 1, and phase 2/3 as phase 2.
- Active: recruiting, not yet recruiting, enrolling by invitation, or active and no longer recruiting.
- Completion rate: of the trials that have ended, the share marked Completed rather than Terminated or Withdrawn. Completed means the trial ended as planned; it does not mean the drug worked. Suspended trials are not counted as ended.
- Stopped: terminated or withdrawn. Trials stop for many reasons, including slow enrolment and business decisions, not only safety or efficacy.
- Sponsors: the lead sponsor of each trial. Companies are the sponsors ClinicalTrials.gov classes as industry; the rest are universities, hospitals, cooperative groups, government bodies and individuals.