Tolvaptan
Tolvaptan is a selective vasopressin V2 receptor antagonist (vaptans class) that blocks the antidiuretic action of arginine vasopressin (AVP) in the renal collecting duct, preventing water reabsorption and promoting free water excretion (aquaresis) without significant sodium or potassium loss. It is approved for hyponatremia in syndrome of inappropriate ADH secretion (SIADH), congestive heart failure, and cirrhosis, and for slowing kidney cyst growth in autosomal dominant polycystic kidney disease (ADPKD). Its aquaretic mechanism corrects hyponatremia and reduces cyst expansion without the electrolyte disturbances of conventional diuretics.
Peso Molecular
448,9000 g/mol
LogP
4,80
TPSA
69,60 Ų
Regra dos 5 de Lipinski
Aprovado
Áreas Terapêuticas
Mecanismo de Ação
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Estrutura 2D
Cite this structure
Embed this structure
SMILES
Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3cc(Cl)ccc32)c(C)c1
InChI
InChI=1S/C26H25ClN2O3/c1-16-6-3-4-7-20(16)25(31)28-19-10-11-21(17(2)14-19)26(32)29-13-5-8-24(30)22-15-18(27)9-12-23(22)29/h3-4,6-7,9-12,14-15,24,30H,5,8,13H2,1-2H3,(H,28,31)
Molecular Formula
C26H25ClN2O3
HBD / HBA
2 / 3
Ligações Rotacionáveis
3
Átomos Pesados
32
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Perguntas frequentes
Tolvaptan is a selective vasopressin V2 receptor antagonist (vaptans class) that blocks the antidiuretic action of arginine vasopressin (AVP) in the renal collecting duct, preventing water reabsorption and promoting free water excretion (aquaresis) without significant sodium or potassium loss. It is approved for hyponatremia in syndrome of inappropriate ADH secretion (SIADH), congestive heart failure, and cirrhosis, and for slowing kidney cyst growth in autosomal dominant polycystic kidney disease (ADPKD). Its aquaretic mechanism corrects hyponatremia and reduces cyst expansion without the …
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Yes, Tolvaptan is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL344159. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 216237. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
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