Repositioning Candidate Details
| Candidate ID: | R0317 |
| Source ID: | DB00872 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Conivaptan |
| Synonyms: | 4'-((4,5-dihydro-2-methylimidazo(4,5-d)(1)benzazepin-6(1H)-yl)carbonyl)-2-biphenylcarboxanilide; Conivaptan |
| Molecular Formula: | C32H26N4O2 |
| SMILES: | CC1=NC2=C(CCN(C(=O)C3=CC=C(NC(=O)C4=CC=CC=C4C4=CC=CC=C4)C=C3)C3=CC=CC=C23)N1 |
| Structure: |
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| DrugBank Description: | Conivaptan is a non-peptide inhibitor of antidiuretic hormone (vasopressin). It was approved in 2004 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH). Conivaptan inhibits both isotypes of the vasopressin receptor (V1a and V2). |
| CAS Number: | 210101-16-9 |
| Molecular Weight: | 498.5744 |
| DrugBank Indication: | For the treatment of euvolemic or hypervolemic hyponatremia (e.g. the syndrome of inappropriate secretion of antidiuretic hormone, or in the setting of hypothyroidism, adrenal insufficiency, pulmonary disorders, etc.) in hospitalized patients. |
| DrugBank Pharmacology: | Conivaptan is a nonpeptide, dual antagonist of arginine vasopressin (AVP) V<sub>1A</sub> and V<sub>2</sub> receptors. The level of AVP in circulating blood is critical for the regulation of water and electrolyte balance and is usually elevated in both euvolemic and hypervolemic hyponatremia. The AVP effect is mediated through V<sub>2</sub> receptors, which are functionally coupled to aquaporin channels in the apical membrane of the collecting ducts of the kidney. These receptors help to maintain plasma osmolality within the normal range by increasing permeability of the renal collecting ducts to water. Vasopressin also causes vasoconstriction through its actions on vascular <sub>1A</sub> receptors. The predominant pharmacodynamic effect of conivaptan in the treatment of hyponatremia is through its V<sub>2</sub> antagonism of AVP in the renal collecting ducts, an effect that results in aquaresis, or excretion of free water. Conivaptan's antagonist activity on V<sub>1A</sub> receptors may also cause splanchnic vasodilation, resulting in possible hypotension or variceal bleeding in patients with cirrhosis. The pharmacodynamic effects of conivaptan include increased free water excretion (i.e., effective water clearance ) generally accompanied by increased net fluid loss, increased urine output, and decreased urine osmolality. |
| DrugBank MoA: | Conivaptan is a dual AVP antagonist with nanomolar affinity for human arginine vasopressin V<sub>1A</sub> and V<sub>2</sub> receptors <i>in vitro</i>. This antagonism occurs in the renal collecting ducts, resulting in aquaresis, or excretion of free water. |
| Targets: | Vasopressin V1a receptor antagonist; Vasopressin V2 receptor antagonist |
| Inclusion Criteria: | Indication associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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