Glucagon receptor Agonists
5 drugsAbout Glucagon receptor
The Glucagon receptor (GCGR) is a G protein-coupled receptor primarily in the liver that binds glucagon, counteracting insulin's effects. By stimulating glycogen breakdown and glucose release, GCGR raises blood sugar levels, making it crucial for glucose homeostasis.
Human genetic studies provide strong validation for GCGR as a therapeutic target, with variants linked to GCGR-related hyperglucagonemia (score 0.84). Loss-of-function variants are associated with increased disease risk, suggesting activation may be beneficial.
GCGR is targeted by 5 FDA-approved small molecule drugs, including ZEGALOGUE, BAQSIMI and GLUCAGON. These drugs, developed by companies like Viatris and Zealand Pharma, are used in metabolic conditions and other therapeutic areas.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Alcohol Use Disorder with only 1 trials.
Glucagon receptor Genetic Evidence Strong
Genetic evidence strongly supports GCGR's role in disease, with a max score of 0.84 for GCGR-related hyperglucagonemia.
Strong genetic support suggests that clinical trials targeting GCGR have a higher likelihood of success.
💡 Why activation?
- • Loss-of-function variants increase disease risk (OR > 1) — restoring function may help
- • 100% directional consistency across 1 traits
- • Strong signal in genetic, familial or congenital disease, endocrine system disease, cancer or benign tumor pathways
Cross-Disease Effects
Trade-off: LowDirection of Effect
100% alignedEvidence Across Diseases
2 totalGWAS and other genetic studies link GCGR to 2 diseases.
Loss-of-function causes disease; activation may help
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for GCGR 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 Glucagon receptor Drugs
Four companies, including Viatris and Zealand Pharma, have approved drugs targeting GCGR.
The presence of established players suggests moderate barriers to entry in the GCGR-targeted drug market.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| GVOKE KIT | XERIS | 2019 | 1 |
| GVOKE HYPOPEN | XERIS | 2019 | 1 |
Glucagon receptor Drug Modality Landscape
Modalities
Routes of Administration
Glucagon receptor is druggable by small molecules, though no oral formulations are currently approved.
Exploring alternative modalities like antibodies or peptides could offer a competitive advantage in the GCGR space.
Glucagon receptor Clinical Trials 105 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 43 | 32 | 5 | 6 | 86% |
| Phase 2 | 33 | 24 | 7 | 2 | 77% |
| Phase 3 | 17 | 16 | 0 | 1 | 100% |
| Phase 4 | 12 | 7 | 1 | 4 | 88% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Glucagon receptor Drug Approval Timeline (1960 - 2019)
The first GCGR-targeting drug was approved in 1960, with the most recent in 2021.
The 62-year span indicates a mature market, but recent approvals suggest continued innovation potential.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 4 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 89 clinical trials targeting Glucagon 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