cholinergic receptor Inhibitors
7 drugsAbout cholinergic receptor
Cholinergic receptors are proteins essential for nerve impulse transmission. They bind acetylcholine, a neurotransmitter, and mediate diverse physiological processes. As drug targets, they modulate pathways relevant to multiple disease states.
Genetic evidence weakly supports cholinergic receptors as therapeutic targets, with CHRM1 linked to insomnia (score 0.22) and corneal ulcer (score 0.19). Colocalization analysis reveals two strong eQTL/pQTL signals (max H4: 0.97).
Seven FDA-approved drugs target cholinergic receptors, including CLOZAPINE, ROCURONIUM BROMIDE and CISATRACURIUM BESYLATE. All are small molecules, with applications spanning CNS disorders and other therapeutic areas.
cholinergic receptor Genetic Evidence
Genetic evidence offers weak support, with a max score of 0.22 for insomnia.
Further research is needed to validate cholinergic receptors as drug targets for genetically supported indications.
Evidence Across Diseases
2 totalGWAS and other genetic studies link CHRM1 to 2 diseases.
🔗 Colocalization Evidence 2 strong
max H4: 0.97eQTL/pQTL signals for CHRM1 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 cholinergic receptor Drugs
Six companies have approved drugs, including Fresenius Kabi and Teva.
The presence of multiple players suggests a moderately competitive market with potential for new entrants.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| SUCCINYLCHOLINE CHLORIDE | INTL MEDICATION | 1972 | 3 |
| CISATRACURIUM BESYLATE PRESERVATIVE FREE | Fresenius Kabi | 2012 | 3 |
| CLOZAPINE | ACCORD HLTHCARE | 1996 | 2 |
| VERSACLOZ | DOUGLAS PHARMS | 2013 | 2 |
cholinergic receptor Drug Modality Landscape
Modalities
Routes of Administration
cholinergic receptor is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or peptides could provide differentiation in this space.
cholinergic receptor Clinical Trials 105 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on cholinergic receptor. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 3 | 2 | 1 | 0 | 67% |
| Phase 2 | 8 | 8 | 0 | 0 | 100% |
| Phase 3 | 16 | 12 | 2 | 2 | 86% |
| Phase 4 | 78 | 58 | 7 | 13 | 89% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
cholinergic receptor Drug Approval Timeline (1953 - 2013)
The first drug was approved in 1953, and the most recent in 2013.
The long approval span suggests a mature target, but opportunities may exist for novel therapies.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 6 companies competing
- • Market share by company
Full Drug Portfolio
- • All 7 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 7-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 85 (6 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 cholinergic receptor. A trial counts if an approved drug acting on cholinergic receptor 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.