GLP1R Agonists
17 drugsAbout GLP1R
GLP1R (glucagon-like peptide-1 receptor) regulates blood glucose and appetite, making it a key target for metabolic drug development. Activation of GLP1R is crucial for treating type 2 diabetes and obesity.
Human genetics strongly support GLP1R as a therapeutic target, with variants linked to diabetes mellitus (score 0.78), type 2 diabetes (0.76), and obesity (0.70). Activation of GLP1R is likely beneficial based on genetic evidence.
GLP1R is targeted by 17 FDA-approved drugs, including TRULICITY, RYBELSUS, and WEGOVY. Peptide-based therapies dominate (14 drugs), with biologics and small molecules also represented, spanning metabolic and other therapeutic areas.
Strategic Insights
ℹ️ How we calculate- Validated target with strong trial activity and 81% attractiveness score.
- Emerging modalities (Small molecule) signal innovation opportunity.
GLP1R Genetic Evidence Strong
GLP1R has strong genetic support with a max score of 0.78 across 24 diseases.
Strong genetic support suggests a higher probability of clinical success for GLP1R-targeting drugs.
💡 Why activation?
- • Gain-of-function variants reduce disease risk — enhancing activity may help
- • 100% directional consistency across 3 traits
- • Strong signal in endocrine system disease, 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 GLP1R to 24 diseases.
Activating this target may be therapeutic
Activating this target may be therapeutic
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for GLP1R 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 GLP1R Drugs
Five companies have approved GLP1R-targeting drugs, with Eli Lilly and Novo Nordisk leading the market.
The concentrated market indicates high barriers to entry, requiring differentiated products for new entrants.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| OZEMPIC | Novo Nordisk | 2017 | 2 |
| RYBELSUS | Novo Nordisk | 2019 | 2 |
| MOUNJARO | Eli Lilly | 2022 | 2 |
| MOUNJARO KWIKPEN | Eli Lilly | 2022 | 2 |
| MOUNJARO (AUTOINJECTOR) | Eli Lilly | 2022 | 2 |
| XULTOPHY 100/3.6 | Novo Nordisk | 2016 | 2 |
| SOLIQUA 100/33 | SANOFI-AVENTIS US | 2016 | 2 |
| VICTOZA | Novo Nordisk | 2010 | 2 |
| ADLYXIN | SANOFI-AVENTIS US | 2016 | 2 |
| ZEPBOUND KWIKPEN | Eli Lilly | 2023 | 2 |
| ZEPBOUND (AUTOINJECTOR) | Eli Lilly | 2023 | 2 |
| LIRAGLUTIDE | Lupin | 2024 | 1 |
| BYETTA | AMYLIN | 2005 | 1 |
| WEGOVY | Novo Nordisk | 2021 | - |
GLP1R Drug Modality Landscape
Modalities
Routes of Administration
GLP1R is druggable by both biologics (4) and small molecules (1), indicating broad therapeutic accessibility.
The dominance of peptides suggests an opportunity for novel small molecule or biologic GLP1R modulators.
📈 Modality Evolution
Small molecules pioneered GLP1R targeting (2005), with other biologics entering more recently (2016).
GLP1R Clinical Trials 1,559 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 335 | 285 | 16 | 33 | 95% |
| Phase 2 | 305 | 165 | 25 | 112 | 87% |
| Phase 3 | 497 | 390 | 23 | 84 | 94% |
| Phase 4 | 422 | 272 | 46 | 98 | 86% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Phase 3 Readout Calendar Pro
8 Phase 3 trials testing approved GLP1R drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting GLP1R. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
GLP1R Drug Approval Timeline (2005 - 2024)
The first GLP1R drug was approved in 2005, with the most recent approval in 2024.
The continued approvals suggest sustained interest and potential for further innovation in GLP1R-targeted therapies.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 5 companies competing
- • Market share by company
Full Drug Portfolio
- • All 17 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 17-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Competition: High (15 sponsors)
- • 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 1015 clinical trials targeting GLP1R.
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