V2 receptor Inhibitors
4 drugsAbout V2 receptor
The V2 receptor (AVPR2) is a G protein-coupled receptor that regulates water reabsorption in the kidneys, maintaining fluid balance. Activation of this receptor by vasopressin increases water permeability in kidney tubules. It plays a crucial role in concentrating urine and preventing dehydration.
Human genetics strongly support AVPR2 as a therapeutic target, with a max score of 0.87 linking loss-of-function variants to nephrogenic diabetes insipidus. Additional genetic associations include nephrogenic syndrome of inappropriate antidiuresis (0.85) and other genetic disorders (0.61). Activation of AVPR2 is likely beneficial based on genetic evidence.
Four FDA-approved small molecule drugs target AVPR2, including DDAVP (desmopressin) and various formulations of vasopressin. These drugs, developed by companies like NORDIC PHARMA, Dr. Reddy's, Baxter and GLAND, are used to treat rare diseases and other conditions related to fluid balance.
V2 receptor Genetic Evidence Strong
Strong genetic evidence supports AVPR2's role in nephrogenic diabetes insipidus (0.87) and related disorders.
Strong genetic support suggests that clinical trials targeting AVPR2 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 2 traits
- • Strong signal in urinary system disease, genetic, familial or congenital disease pathways
Cross-Disease Effects
Trade-off: LowDirection of Effect
100% alignedEvidence Across Diseases
5 totalGWAS and other genetic studies link AVPR2 to 5 diseases.
Loss-of-function causes disease; activation may help
Loss-of-function causes disease; activation may help
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 V2 receptor Drugs
Four companies, including NORDIC PHARMA and Dr. Reddy's, have approved drugs targeting AVPR2.
The presence of established players suggests moderate barriers to entry in this market.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| VASOPRESSIN IN DEXTROSE 5% | GLAND | 2024 | 2 |
V2 receptor Drug Modality Landscape
Modalities
Routes of Administration
V2 receptor is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or peptides could provide a competitive advantage.
V2 receptor Clinical Trials 177 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on V2 receptor. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 19 | 13 | 3 | 3 | 81% |
| Phase 2 | 53 | 30 | 13 | 10 | 70% |
| Phase 3 | 41 | 23 | 4 | 14 | 85% |
| Phase 4 | 64 | 38 | 10 | 15 | 79% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
V2 receptor Drug Approval Timeline (1978 - 2024)
The first drug was approved in 1978, with the most recent approval in 2024, spanning 47 years.
The continued approval of new drugs indicates sustained interest and potential for further innovation.
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Deep insights for drug target analysis
Competitive Landscape
- • 4 companies competing
- • Market share by company
Full Drug Portfolio
- • All 4 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 4-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 141 (16 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 V2 receptor. A trial counts if an approved drug acting on V2 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.