Conivaptan

Conivaptan

Clinical data
Trade names	Vaprisol
Other names	YM 087
AHFS/Drugs.com	Monograph
License data	US DailyMed: Conivaptan
Routes of administration	Intravenous
ATC code	C03XA02 (WHO)
Legal status
Legal status	US: ℞-only
Pharmacokinetic data
Bioavailability	N/A
Identifiers
IUPAC name N-(4-((4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin- 6(1H)-yl)carbonyl)phenyl)- (1,1'-biphenyl)-2-carboxamide
CAS Number	210101-16-9 Y
PubChem CID	151171
IUPHAR/BPS	2203
DrugBank	DB00872 Y
ChemSpider	133239 Y
UNII	0NJ98Y462X
KEGG	D01236 N
ChEBI	CHEBI:681850 Y
ChEMBL	ChEMBL1755 Y
CompTox Dashboard (EPA)	DTXSID80175220
Chemical and physical data
Formula	C32H26N4O2
Molar mass	498.586 g·mol−1
3D model (JSmol)	Interactive image
SMILES c1ccccc1-c2ccccc2C(=O)Nc3ccc(cc3)C(=O)N4c5ccccc5-c6[nH]c(C)nc6CC4
InChI InChI=1S/C32H26N4O2/c1-21-33-28-19-20-36(29-14-8-7-13-27(29)30(28)34-21)32(38)23-15-17-24(18-16-23)35-31(37)26-12-6-5-11-25(26)22-9-3-2-4-10-22/h2-18H,19-20H2,1H3,(H,33,34)(H,35,37) Y Key:IKENVDNFQMCRTR-UHFFFAOYSA-N Y
NY (what is this?)  (verify)

Conivaptan, sold under the brand name Vaprisol, is a non-peptide inhibitor of the receptor for anti-diuretic hormone, also called vasopressin. It was approved in 2004 for hyponatremia (low blood sodium levels). The compound was discovered by Astellas and marked in 2006. The drug is now marketed by Cumberland Pharmaceuticals, Inc.

Conivaptan inhibits two of the three subtypes of the vasopressin receptor (V1a and V2). Effectively, it causes iatrogenic nephrogenic diabetes insipidus.

Conivaptan has not been approved by the American Food and Drug Administration for the treatment of decompensated congestive heart failure. However, in theory, vasopressin receptor antagonism would be particularly useful in this setting, and an initial study shows that it has some promise.^[1]