GIPR Agonists
6 drugsAbout GIPR
GIPR (Glucose-dependent Insulinotropic Polypeptide Receptor) mediates the effects of GIP, stimulating insulin release from pancreatic beta cells in a glucose-dependent manner. As a drug target, GIPR modulates glucose homeostasis and is primarily targeted in metabolic therapeutic areas.
Human genetic studies provide strong validation for GIPR as a therapeutic target, with variants linked to obesity (score 0.70), morbid obesity (0.65), and skeletal abnormalities (0.63). Gain-of-function variants are protective, suggesting activation-based therapies may be beneficial.
GIPR is targeted by 6 FDA-approved peptide drugs, including Zepbound and Mounjaro, all developed by Eli Lilly. The target spans metabolic disease indications.
Strategic Insights
ℹ️ How we calculate- Validated target with strong trial activity and 89% attractiveness score.
- White space opportunity in Cannabis Use Disorder with only 2 trials.
Human Genetic Evidence Strong
GIPR has strong genetic support with a max score of 0.70 linked to 31 diseases.
Strong genetic support increases clinical success probability, making GIPR a promising target.
💡 Why activation?
- • Gain-of-function variants reduce disease risk — enhancing activity may help
- • 100% directional consistency across 2 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 GIPR to 31 diseases.
Activating this target may be therapeutic
Activating this target may be therapeutic
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for GIPR 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 Drugs
Eli Lilly is the only company with approved GIPR-targeting drugs.
High market concentration with Eli Lilly indicates high entry barriers or first-mover advantage.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| MOUNJARO (AUTOINJECTOR) | Eli Lilly | 2022 | 2 |
| ZEPBOUND KWIKPEN | Eli Lilly | 2023 | 2 |
| ZEPBOUND (AUTOINJECTOR) | Eli Lilly | 2023 | 2 |
Drug Modality Landscape
Modalities
Routes of Administration
GIPR is primarily targeted by peptide modalities (100% of approved drugs).
The modality landscape is entirely peptides, suggesting an opportunity for small molecule or antibody development.
Clinical Trials 180 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 42 | 32 | 1 | 9 | 97% |
| Phase 2 | 60 | 11 | 2 | 46 | 85% |
| Phase 3 | 44 | 26 | 1 | 17 | 96% |
| Phase 4 | 34 | 4 | 2 | 27 | 67% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Phase 3 Readout Calendar Pro
8 Phase 3 trials testing approved GIPR drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting GIPR. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
Drug Approval Timeline (2022 - 2023)
The first GIPR drug was approved in 2022, with the most recent in 2023.
Recent approvals suggest a growing interest in GIPR, but the market may be approaching saturation.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 1 companies competing
- • Market share by company
Full Drug Portfolio
- • All 6 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 6-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 164 clinical trials targeting GIPR.
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