Samsca(tolvaptan)
Jinarc, Jynarque, Samsca (tolvaptan) is a small molecule pharmaceutical. Tolvaptan was first approved as Samsca on 2009-05-19. It is used to treat hyponatremia in the USA. It has been approved in Europe to treat autosomal dominant polycystic kidney and inappropriate adh syndrome. The pharmaceutical is active against vasopressin V2 receptor. In addition, it is known to target vasopressin V1a receptor.
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Therapeutic Areas
Therapeutic Area | MeSH |
|---|---|
| nervous system diseases | D009422 |
| urogenital diseases | D000091642 |
| hereditary congenital and neonatal diseases and abnormalities | D009358 |
| nutritional and metabolic diseases | D009750 |
| endocrine system diseases | D004700 |
Trade Name
FDA
EMA
Jynarque, Samsca (generic drugs available since 2020-05-19)
Drug Products
FDA
EMA
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| hyponatremia | HP_0002902 | D007010 | E87.1 |
Agency Specific
FDA
EMA
Expiration | Code | ||
|---|---|---|---|
TOLVAPTAN, JYNARQUE, OTSUKA | |||
| 2025-04-23 | ODE-178 | ||
HCPCS
No data
Clinical
Clinical Trials
102 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Heart failure | D006333 | EFO_0003144 | I50 | 1 | 4 | 6 | 10 | 3 | 24 |
| Hyponatremia | D007010 | HP_0002902 | E87.1 | — | 3 | 10 | 5 | 6 | 23 |
| Autosomal dominant polycystic kidney | D016891 | EFO_1001496 | Q61.2 | — | 7 | 9 | 2 | 2 | 20 |
| Liver cirrhosis | D008103 | EFO_0001422 | K74.0 | 1 | 3 | 6 | 1 | 2 | 12 |
| Healthy volunteers/patients | — | 3 | 1 | — | 1 | 1 | 6 | ||
| Ascites | D001201 | HP_0001541 | R18 | 1 | 1 | 1 | 2 | — | 5 |
| Cardiovascular diseases | D002318 | EFO_0000319 | I98 | — | 1 | — | 1 | — | 2 |
| Tricuspid valve insufficiency | D014262 | HP_0005180 | — | — | — | 1 | — | 1 | |
| Heart diseases | D006331 | EFO_0003777 | I51.9 | — | — | — | 1 | — | 1 |
| Neoplasms | D009369 | C80 | — | — | — | 1 | — | 1 |
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Inappropriate adh syndrome | D007177 | EFO_1000982 | E22.2 | 1 | 1 | 3 | — | 4 | 8 |
| Cardiac edema | D004489 | EFO_1001771 | — | — | 4 | — | — | 4 | |
| Autosomal recessive polycystic kidney | D017044 | Q61.1 | — | — | 2 | — | — | 2 | |
| Water intoxication | D014869 | — | — | 2 | — | — | 2 | ||
| Water-electrolyte imbalance | D014883 | — | — | 2 | — | — | 2 | ||
| Hepatic encephalopathy | D006501 | K72.91 | — | — | 1 | — | — | 1 | |
| Cri-du-chat syndrome | D003410 | Q93.4 | — | — | 1 | — | — | 1 | |
| Chronic renal insufficiency | D051436 | N18 | — | — | 1 | — | — | 1 | |
| Dyspnea | D004417 | HP_0002094 | R06.0 | — | — | 1 | — | — | 1 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Chronic kidney failure | D007676 | EFO_0003884 | N18.6 | — | 3 | — | — | — | 3 |
| Edema | D004487 | R60.9 | — | 1 | — | — | — | 1 |
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Nephrolithiasis | D053040 | N20.0 | 1 | — | — | — | — | 1 | |
| Cardiomyopathies | D009202 | EFO_0000318 | I42 | 1 | — | — | — | — | 1 |
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | TOLVAPTAN |
| INN | tolvaptan |
| Description | Tolvaptan is a benzazepine derivative incorporating a benzenedicarboxamide function whch is a selective vasopressin V2 receptor antagonist used to treat euvolemic and hypervolemic hyponatremia. It is also used in the treatment of rapidly progressing autosomal dominant polycystic kidney disease to slow the rate of cyst development and renal insufficiency. Tolvaptan is a racemate consisting of a 1:1 mixture of 5R and 5S stereomers. It has a role as a vasopressin receptor antagonist and an aquaretic. It is a benzazepine and a benzenedicarboxamide. |
| Classification | Small molecule |
| Drug class | aptamers, classical and mirror; vasopressin receptor antagonists |
| Image (chem structure or protein) | |
| Structure (InChI/SMILES or Protein Sequence) | Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3cc(Cl)ccc32)c(C)c1 |
Identifiers
| PDB | — |
| CAS-ID | 150683-30-0 |
| RxCUI | 358257 |
| ChEMBL ID | CHEMBL344159 |
| ChEBI ID | — |
| PubChem CID | 216237 |
| DrugBank | DB06212 |
| UNII ID | 21G72T1950 (ChemIDplus, GSRS) |
Target
Agency Approved
Alternate
AVPR1A
AVPR1A
Organism
Homo sapiens
Gene name
AVPR1A
Gene synonyms
AVPR1
NCBI Gene ID
Protein name
vasopressin V1a receptor
Protein synonyms
Antidiuretic hormone receptor 1a, AVPR V1a, SCCL vasopressin subtype 1a receptor, V1-vascular vasopressin receptor AVPR1A, V1a vasopressin receptor, Vascular/hepatic-type arginine vasopressin receptor
Uniprot ID
Mouse ortholog
Avpr1a (54140)
vasopressin V1a receptor (Q9QYH2)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 3,071 documents
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Safety
Black-box Warning
Black-box warning for: Jynarque, Samsca, Tolvaptan
Adverse Events
Top Adverse Reactions
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6 adverse events reported
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