Tolvaptan

(USAN, rINN)
Tolvaptan Chemical formula
Synonyms: OPC-41061; Tolvaptán; Tolvaptanum. (±)-4′-[(7-Chloro-2,3,4,5tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]o-tolum-toluidide.
Cyrillic synonym: Толваптан.

Chemical information

Chemical formula: C26H25ClN2O3 = 448.9.
CAS — 150683-30-0.

Profile

Tolvaptan is a selective vasopressin V2-receptor antagonist under investigation for the treatment of hyponatraemia, including that in heart failure.
1. Schrier RW, et al. SALT Investigators. Tolvaptan, a selective oral vasopressin V -receptor antagonist, for hyponatremia. N Engl J Med 2006; 355: 2099–2112
2. Konstam MA, et al. Effects of oral tolvaptan in patients hospitalized for worsening heart failure: the EVEREST outcome trial. JAMA 2007; 297: 1319–31
3. Gheorghiade M, et al. Short-term clinical effects of tolvaptan, an oral vasopressin antagonist, in patients hospitalized for heart failure: the EVEREST clinical status trials. JAMA 2007; 297: 1332–43
4. Udelson JE, et al. Multicenter, randomized, double-blind, placebo-controlled study on the effect of oral tolvaptan on left ventricular dilation and function in patients with heart failure and systolic dysfunction. J Am Coll Cardiol 2007; 49: 2151–9
5. Shoaf SE, et al. Pharmacokinetics, pharmacodynamics, and safety of tolvaptan, a nonpeptide AVP antagonist, during ascending single-dose studies in healthy subjects. J Clin Pharmacol 2007; 47: 1498–1507.
Published May 08, 2019.