General Information of Drug (ID: DM1V329)

Drug Name
Conivaptan Drug Info
Synonyms
Conivaptan [INN]; YM 087; YM087; Conivaptan (INN); Vaprisol (TN); YM-087; N-[4-(2-methyl-4,5-dihydro-3H-imidazo[4,5-d][1]benzazepine-6-carbonyl)phenyl]-2-phenylbenzamide; N-{4-[(2-methyl-4,5-dihydroimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl}biphenyl-2-carboxamide; 4'-((4,5-dihydro-2-methylimidazo(4,5-d)(1)benzazepin-6(1H)-yl)carbonyl)-2-biphenylcarboxanilide
Indication
Disease Entry ICD 11 Status REF
Euvolemic hyponatremia 5C72 Approved [1] , [2]
Cross-matching ID
PubChem CID
151171
ChEBI ID
CHEBI:681850
CAS Number
CAS 210101-16-9
TTD Drug ID
DM1V329
INTEDE Drug ID
DR0376

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Vasopressin V1a receptor (V1AR) TT4TFGN V1AR_HUMAN Modulator [3] , [4]
Vasopressin V2 receptor (V2R) TTK8R02 V2R_HUMAN Modulator [3] , [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [5]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Vasopressin V1a receptor (V1AR) DTT AVPR1A 4.689 3.609 4.591 3.878
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Euvolemic hyponatremia
ICD Disease Classification 5C72
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Vasopressin V1a receptor (V1AR) DTT AVPR1A 8.89E-04 -0.12 -0.34
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 5.10E-04 6.44E-02 2.85E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2203).
2 Emerging diuretics for the treatment of heart failure. Expert Opin Emerg Drugs. 2009 Mar;14(1):195-204.
3 Acute hemodynamic effects of conivaptan, a dual V(1A) and V(2) vasopressin receptor antagonist, in patients with advanced heart failure. Circulation. 2001 Nov 13;104(20):2417-23.
4 Conivaptan: a dual vasopressin receptor v1a/v2 antagonist [corrected]. Cardiovasc Drug Rev. 2007 Fall;25(3):261-79.
5 Conivaptan: a dual vasopressin receptor v1a/v2 antagonist [corrected]. Cardiovasc Drug Rev. 2007 Fall;25(3):261-79.