IL1R1 Inhibitors
2 drugsAbout IL1R1
Interleukin-1 receptor type 1 (IL1R1), also known as IL-1, is a cell surface receptor that initiates intracellular signaling upon binding the cytokine interleukin-1 (IL-1). This signaling cascade plays a critical role in inflammation.
Human genetic studies provide strong support for IL1R1 as a therapeutic target, with variants linked to antisynthetase syndrome (score 0.74), allergic rhinitis (0.64) and eczematoid dermatitis (0.64). Colocalization analysis reveals 20 strong eQTL/pQTL signals (max H4: 1.00).
IL1R1 is targeted by two FDA-approved drugs, ILARIS and KINERET, spanning immunology and other therapeutic areas. These drugs include one antibody and one biologic (other) modality.
IL1R1 Genetic Evidence Strong
Genetic evidence provides strong support for IL1R1's role in multiple diseases.
Strong genetic support (max score 0.74) may increase clinical trial success probability.
Evidence Across Diseases
10 totalGWAS and other genetic studies link IL1B to 10 diseases.
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for IL1B 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 IL1R1 Drugs
Novartis and BIOVITRUM AB are the companies with approved IL1R1-targeting drugs.
The presence of only two companies suggests a market with potential for new entrants.
IL1R1 Drug Modality Landscape
Modalities
Routes of Administration
IL1R1 is exclusively targeted by antibodies, suggesting it may be a cell-surface or secreted protein.
Consider novel modalities to differentiate from existing IL1R1-targeting drugs.
📈 Modality Evolution
other biologics pioneered IL1R1 targeting (2001), with antibodies entering more recently (2009).
IL1R1 Clinical Trials 207 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on IL1R1. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 45 | 23 | 14 | 8 | 62% |
| Phase 2 | 106 | 64 | 23 | 18 | 74% |
| Phase 3 | 48 | 28 | 11 | 9 | 72% |
| Phase 4 | 8 | 2 | 5 | 1 | 29% |
Top Sponsors
By Modality
IL1R1 Drug Approval Timeline (2001 - 2009)
The first IL1R1-targeting drug was approved in 2001, and the most recent in 2009.
The relatively long gap since the last approval suggests a potential for renewed innovation in this area.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 2 companies competing
- • Market share by company
Full Drug Portfolio
- • All 2 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 2-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 97 (9 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 IL1R1. A trial counts if an approved drug acting on IL1R1 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.