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.
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 |
|---|---|---|---|
| VICTOZA | Novo Nordisk | 2010 | 2 |
| XULTOPHY 100/3.6 | Novo Nordisk | 2016 | 2 |
| SOLIQUA 100/33 | SANOFI-AVENTIS US | 2016 | 2 |
| RYBELSUS | Novo Nordisk | 2019 | 2 |
| MOUNJARO | Eli Lilly | 2022 | 2 |
| MOUNJARO KWIKPEN | Eli Lilly | 2022 | 2 |
| MOUNJARO (AUTOINJECTOR) | Eli Lilly | 2022 | 2 |
| OZEMPIC | Novo Nordisk | 2017 | 2 |
| ZEPBOUND KWIKPEN | Eli Lilly | 2023 | 2 |
| ZEPBOUND (AUTOINJECTOR) | Eli Lilly | 2023 | 2 |
| LIRAGLUTIDE | Novartis | 2024 | 1 |
| BYETTA | AstraZeneca | 2005 | 1 |
| WEGOVY | Novo Nordisk | 2021 | - |
| ADLYXIN | SANOFI-AVENTIS US | 2016 | - |
GLP1R Drug Modality Landscape
Modalities
Routes of Administration
GLP1R is primarily targeted by peptide modalities (88% of approved drugs).
The dominance of peptides suggests an opportunity for novel small molecule or biologic GLP1R modulators.
📈 Modality Evolution
Peptides pioneered GLP1R targeting (2010), with other biologics entering more recently (2016).
GLP1R Clinical Trials 1,659 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on GLP1R. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 350 | 288 | 16 | 46 | 95% |
| Phase 2 | 334 | 182 | 25 | 127 | 88% |
| Phase 3 | 523 | 401 | 23 | 99 | 95% |
| Phase 4 | 452 | 279 | 47 | 125 | 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 (2010 - 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
- • Sponsors: 485 (93 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 GLP1R. A trial counts if an approved drug acting on GLP1R 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.