Conivaptan

Conivaptan
Clinical data
Trade namesVaprisol
Other namesYM 087
AHFS/Drugs.comMonograph
License data
Routes of
administration
Intravenous
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityN/A
Elimination half-life5 hours
Identifiers
  • N-(4-((4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin- 6(1H)-yl)carbonyl)phenyl)- (1,1'-biphenyl)-2-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC32H26N4O2
Molar mass498.586 g·mol−1
3D model (JSmol)
  • c1ccccc1-c2ccccc2C(=O)Nc3ccc(cc3)C(=O)N4c5ccccc5-c6[nH]c(C)nc6CC4
  • 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). Additionally, conivaptan is used for the treatment of syndrome of inappropriate antidiuretic hormone secretion.

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 US Food and Drug Administration (FDA) 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.