National Cancer Institute Thesaurus

Last uploaded: February 23, 2024
Preferred Name

Tolvaptan
Synonyms

N-(4-{[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide

7-Chloro-5-hydroxy-1-(2-methyl-4-(2-methylbenzoylamino)benzoyl)2,3,4,5-tetrahydro-1H-1-benzazepine

OPC-41061

Samsca

TOLVAPTAN

Tolvaptan

Definitions

An orally bioavailable, selective, arginine vasopressin receptor 2 (V2, AVPR2) antagonist that can be used to treat hyponatremia. Upon oral administration, tolvaptan selectively and competitively binds to and blocks the V2 receptor located in the walls of the vasculature and luminal membranes of renal collecting ducts, thereby preventing the binding of vasopressin to the V2 receptor. This prevents water absorption in the kidneys and increases the excretion of electrolyte-free water via the kidneys. This reduces intravascular volume and increases serum sodium concentrations and osmolality.

ID

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C77082

CAS_Registry

150683-30-0

Chemical_Formula

C26H25ClN2O3

code

C77082

Concept_In_Subset

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C176424

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116978

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116977

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C63923

Contributing_Source

CTRP

FDA

DEFINITION

An orally bioavailable, selective, arginine vasopressin receptor 2 (V2, AVPR2) antagonist that can be used to treat hyponatremia. Upon oral administration, tolvaptan selectively and competitively binds to and blocks the V2 receptor located in the walls of the vasculature and luminal membranes of renal collecting ducts, thereby preventing the binding of vasopressin to the V2 receptor. This prevents water absorption in the kidneys and increases the excretion of electrolyte-free water via the kidneys. This reduces intravascular volume and increases serum sodium concentrations and osmolality.

Display_Name

Tolvaptan

FDA_UNII_Code

21G72T1950

FULL_SYN

N-(4-{[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide

7-Chloro-5-hydroxy-1-(2-methyl-4-(2-methylbenzoylamino)benzoyl)2,3,4,5-tetrahydro-1H-1-benzazepine

OPC-41061

Samsca

TOLVAPTAN

Tolvaptan

Has_Target

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C26100

label

Tolvaptan

Legacy Concept Name

Tolvaptan

NCI_Drug_Dictionary_ID

686120

PDQ_Closed_Trial_Search_ID

686120

PDQ_Open_Trial_Search_ID

686120

Preferred_Name

Tolvaptan

prefixIRI

Thesaurus:C77082

Semantic_Type

Pharmacologic Substance

UMLS_CUI

C1176308

subClassOf

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C2180

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