tolvaptan (samsca) Report issue

Small molecule Approved FDA
AACT ChEMBL DrugBank Drug Central Drugs@FDA KEGG MeSH PubChem repoDB

Active Ingredient History

NOW
  • Now
Tolvaptan is a selective and competitive arginine vasopressin receptor 2 antagonist. Vasopressin acts on the V2 receptors found in the walls of the vasculature and luminal membranes of renal collecting ducts. By blocking V2 receptors in the renal collecting ducts, aquaporins do not insert themselves into the walls thus preventing water absorption. This action ultimately results in an increase in urine volume, decrease urine osmolality, and increase electrolyte-free water clearance to reduce intravascular volume and an increase serum sodium levels. Tolvaptan is especially useful for heart failure patients as they have higher serum levels of vasopressin. Tolvaptan is used to treat low blood sodium levels (hyponatremia) associated with various conditions like congestive heart failure, cirrhosis, and syndrome of inappropriate antidiuretic hormones (SIADH). FDA approved on May 19, 2009. Tolvaptan is sold under the trade names Samsca and Jinarc.   NCATS

Chemistry

  • SMILES: CC1=CC=CC=C1C(=O)NC2=CC=C(C(=O)N3CCCC(O)C4=CC(Cl)=CC=C34)C(C)=C2
  • InChIKey: GYHCTFXIZSNGJT-UHFFFAOYSA-N
  • Mol. Mass: 448.941
  • ALogP: 5.68
  • ChEMBL Molecule:
    tolvaptan  
More Chemistry

Pharmacology

  • Mechanism of Action:
  • Multi-specific: Missing data
  • Black Box: Yes
  • Availability: Prescription Only
  • Delivery Methods: Oral
  • Pro Drug: No

Drug Pricing (per unit)

United States

$195.2283 - $513.9460
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

Alternative names

7-chloro-5-hydroxy-1-(2-methyl-4-(2-methylbenzoylamino)benzoyl)2,3,4,5-tetrahydro-1h-1-benzazepine | jinarc | opc 41061 | opc-41061 | samsca | tolvaptan | vasopressin v2 receptor antagonist

Organizations (68)

Research & Development (62)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (7)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (27)

Approved Indications (1)


 

Hyponatremia

Experimental Indications - Clinical Trial Phases 1-4 (27)


 

Ascites (Phase 4)

Body Fluids (Phase 4)

Carcinoma (Phase 2)

Cardiomyopathies (Phase 1)

Cardiovascular Diseases (Phase 4)

Dyspnea (Phase 3)

Edema (Phase 2)

Edema, Cardiac (Phase 3)

Fibrosis (Phase 4)

Healthy Volunteers (Phase 4)

Heart Diseases (Phase 4)

Heart Failure (Phase 4)

Hepatic Encephalopathy (Phase 3)

Hormones (Phase 1/Phase 2)

Hyponatremia ()

Inappropriate ADH Syndrome (Phase 3)

Kidney Diseases (Phase 2)

Kidney Failure, Chronic (Phase 2)

Liver Cirrhosis (Phase 3)

Neoplasms (Phase 4)

Nephrolithiasis (Phase 1)

Polycystic Kidney, Autosomal Dominant (Phase 4)

Polycystic Kidney, Autosomal Recessive (Phase 3)

Renal Insufficiency, Chronic (Phase 3)

Tricuspid Valve Insufficiency (Phase 4)

Water-Electrolyte Imbalance (Phase 3)

Water Intoxication (Phase 3)

Overview

  • Highest Phase: Phase 4
  • # of Trials: 97
  • # of Trial Organizations: 62

Trials by Phase

Trial Phase Start Date Organizations Indications

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