CGRP receptor Inhibitors
5 drugsAbout CGRP receptor
The CGRP receptor, a heterodimeric GPCR composed of CLR and RAMP1, is activated by the neuropeptide CGRP. This activation is implicated in physiological processes, notably migraine pathophysiology. It has emerged as a critical drug target, especially for CNS disorders.
Human genetic studies provide strong validation for CALCRL (score 0.74), a subunit of the CGRP receptor, as a therapeutic target. Genetic associations include hypertension (score 0.74) and obesity (score 0.69). Activation of the receptor is likely beneficial based on genetic evidence.
The CGRP receptor is targeted by 5 FDA-approved drugs, including AIMOVIG, ZAVZPRET, UBRELVY, QULIPTA, and NURTEC ODT, all for CNS indications. These drugs are primarily small molecules (4 drugs) and biologics (1 drug).
Strategic Insights
ℹ️ How we calculate- White space opportunity in Menstrual Migraine (MM) with only 1 trials.
CGRP receptor Genetic Evidence Strong
Genetic evidence strongly supports the CGRP receptor as a target, with a max score of 0.74.
Strong genetic support suggests a higher probability of clinical success for CGRP-targeting therapies.
💡 Why activation?
- • Gain-of-function variants reduce disease risk — enhancing activity may help
- • 100% directional consistency across 1 traits
- • Strong signal in nutritional or metabolic disease, phenotype pathways
Cross-Disease Effects
Trade-off: LowDirection of Effect
100% alignedEvidence Across Diseases
20 totalGWAS and other genetic studies link CALCRL to 39 diseases.
Activating this target may be therapeutic
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for CALCRL 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 CGRP receptor Drugs
Amgen, Pfizer, and AbbVie are the key players in the CGRP receptor drug market.
High market concentration suggests significant barriers to entry for new companies.
CGRP receptor Drug Modality Landscape
Modalities
Routes of Administration
CGRP receptor is druggable by both biologics (4) and small molecules (4), indicating broad therapeutic accessibility.
Consider exploring novel biologic modalities to differentiate from existing small molecule therapies.
📈 Modality Evolution
other biologics pioneered CGRP receptor targeting (2018), with small molecules entering more recently (2019).
CGRP receptor Clinical Trials 108 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 14 | 11 | 2 | 1 | 85% |
| Phase 2 | 25 | 15 | 4 | 6 | 79% |
| Phase 3 | 44 | 28 | 3 | 11 | 90% |
| Phase 4 | 25 | 16 | 4 | 5 | 80% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Phase 3 Readout Calendar Pro
5 Phase 3 trials testing approved CGRP receptor drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting CGRP receptor. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
CGRP receptor Drug Approval Timeline (2018 - 2023)
The first CGRP receptor drug was approved in 2018, with the most recent in 2023.
The recent approval suggests continued interest and potential for further development in this area.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 3 companies competing
- • Market share by company
Full Drug Portfolio
- • All 5 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 5-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Competition: High (15 sponsors)
- • White space: 10 underexplored indications
- • Success rates by condition
Full summary • All drugs • Genetic evidence • Trials • Timeline
How We Calculate These Metrics
Target Attractiveness Score
A 0-100 score based on trial activity, sponsor diversity, and completion rates. Calculated from 118 clinical trials targeting CGRP receptor.
Completion rate: Percentage of trials that reached their planned endpoint. Trials terminated early, withdrawn, or suspended are not counted—these often indicate safety issues, lack of efficacy, or strategic pivots.
- Highly Attractive (80+): High trial activity, many sponsors, strong completion rates
- Attractive (60-79): Good trial activity and validation
- Moderate (40-59): Moderate interest from sponsors
- Low (under 40): Limited trial activity or validation concerns
Strategic Insights
Auto-generated insights based on trial analytics including competition intensity, white space opportunities, modality shifts, and failure patterns. We analyze trial sponsors, phases, indications, and outcomes.
Risk Signals
- High Competition: Many sponsors competing for this target (may reduce market opportunity)
- High Failure Risk: Low trial completion rates suggest development challenges
- Low Validation: Limited trial activity or poor outcomes indicate uncertain viability
- White Space Available: Underexplored indications present opportunities