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.
GIPR 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 GIPR 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 |
GIPR 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.
GIPR Clinical Trials 196 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on GIPR. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 37 | 24 | 0 | 13 | 100% |
| Phase 2 | 66 | 13 | 2 | 51 | 87% |
| Phase 3 | 51 | 30 | 0 | 21 | 100% |
| Phase 4 | 42 | 3 | 1 | 38 | 75% |
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.
GIPR 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
- • Sponsors: 92 (21 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 GIPR. A trial counts if an approved drug acting on GIPR 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.