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Chemical Compound Review

Tolvaptan     N-[4-[(10-chloro-2-hydroxy- 6...

Synonyms: Samsca, CHEMBL344159, SureCN242421, ANW-59865, OPC-41061, ...
 
 
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Disease relevance of Tolvaptan

 

Psychiatry related information on Tolvaptan

  • Experiments were designed to demonstrate the efficacy of tolvaptan reducing mortality in an acute model, and controlling the extent of serum sodium elevation without causing abnormal animal behavior suggesting neurological symptoms in a chronic model [2].
 

High impact information on Tolvaptan

  • Effectiveness of vasopressin V2 receptor antagonists OPC-31260 and OPC-41061 on polycystic kidney disease development in the PCK rat [1].
  • PCK kidneys have increased Ras-GTP and phosphorylated ERK levels and 95-kD/68-kD B-Raf ratios, changes that are corrected by the administration of OPC-31260 or OPC-41061 [1].
  • Renal and neurohumoral effects of tolvaptan and furosemide were assessed in an open-label, randomized, placebo-controlled crossover study in 14 patients with NYHA II-III CHF [7].
  • OPC-41061 inhibited cAMP production induced by AVP with no intrinsic agonist activity [8].
  • In rats, OPC-41061 inhibited [3H]-AVP binding to V1a-receptors (Ki = 325 +/- 41 nM) and V2-receptors (Ki = 1.33 +/- 0. 30 nM), showing higher receptor selectivity (V1a/V2 = 244) than with human receptors [8].
 

Chemical compound and disease context of Tolvaptan

 

Biological context of Tolvaptan

 

Associations of Tolvaptan with other chemical compounds

  • Rationale and design of the multicenter, randomized, double-blind, placebo-controlled study to evaluate the Efficacy of Vasopressin antagonism in Heart Failure: Outcome Study with Tolvaptan (EVEREST) [3].
  • Although tolvaptan and lixivaptan are selective for the vasopressin-2 (V(2)) receptor responsible for the antidiuretic actions of AVP, conivaptan demonstrates activity at both the V(2) receptor and the V(1a) receptor responsible for the vasoconstricting properties of AVP [12].
 

Gene context of Tolvaptan

 

Analytical, diagnostic and therapeutic context of Tolvaptan

  • However, rats treated with repeated oral administrations of tolvaptan (1, 3, and 10 mg/kg) produced dose-dependent aquaresis (i.e. urine volume increased and urine osmolality decreased) that resulted in a gradual increase in plasma sodium concentration [2].
  • Rats receiving dose titrations of tolvaptan (0.25, 0.5, 1, 2, 4, and 8 mg/kg) increased plasma sodium to healthy levels without causing abnormal animal behavior suggesting neurological symptoms or death, improved hyponatremia-driven increases in wet weight and water content in the organs [2].
  • By November 2003, tolvaptan was undergoing phase III clinical trials [15].
  • The composite of cardiovascular death or hospitalization for heart failure occurred in 871 tolvaptan group patients (42.0%) and 829 placebo group patients (40.2%; hazard ratio, 1.04; 95% CI, 0.95-1.14; P = .55) [16].
  • METHODS AND RESULTS: This was a double-blind study investigating the effects of three doses of tolvaptan and placebo in patients with CHF [17].

References

  1. Effectiveness of vasopressin V2 receptor antagonists OPC-31260 and OPC-41061 on polycystic kidney disease development in the PCK rat. Wang, X., Gattone, V., Harris, P.C., Torres, V.E. J. Am. Soc. Nephrol. (2005) [Pubmed]
  2. Therapeutic effects of tolvaptan, a potent, selective nonpeptide vasopressin V2 receptor antagonist, in rats with acute and chronic severe hyponatremia. Miyazaki, T., Yamamura, Y., Onogawa, T., Nakamura, S., Kinoshita, S., Nakayama, S., Fujiki, H., Mori, T. Endocrinology (2005) [Pubmed]
  3. Rationale and design of the multicenter, randomized, double-blind, placebo-controlled study to evaluate the Efficacy of Vasopressin antagonism in Heart Failure: Outcome Study with Tolvaptan (EVEREST). Gheorghiade, M., Orlandi, C., Burnett, J.C., Demets, D., Grinfeld, L., Maggioni, A., Swedberg, K., Udelson, J.E., Zannad, F., Zimmer, C., Konstam, M.A. J. Card. Fail. (2005) [Pubmed]
  4. Comparison of 60-day mortality in hospitalized heart failure patients with versus without hypothermia. Payvar, S., Orlandi, C., Stough, W.G., Elkayam, U., Ouyang, J., Casscells, S.W., Gheorghiade, M. Am. J. Cardiol. (2006) [Pubmed]
  5. Short-term clinical effects of tolvaptan, an oral vasopressin antagonist, in patients hospitalized for heart failure: the EVEREST Clinical Status Trials. Gheorghiade, M., Konstam, M.A., Burnett, J.C., Grinfeld, L., Maggioni, A.P., Swedberg, K., Udelson, J.E., Zannad, F., Cook, T., Ouyang, J., Zimmer, C., Orlandi, C. JAMA (2007) [Pubmed]
  6. Tolvaptan, an oral vasopressin antagonist, in the treatment of hyponatremia in cirrhosis. Cárdenas, A., Ginès, P., Marotta, P., Czerwiec, F., Oyuang, J., Guevara, M., Afdhal, N.H. J. Hepatology (2011) [Pubmed]
  7. Vasopressin-2-receptor antagonism augments water excretion without changes in renal hemodynamics or sodium and potassium excretion in human heart failure. Costello-Boerrigter, L.C., Smith, W.B., Boerrigter, G., Ouyang, J., Zimmer, C.A., Orlandi, C., Burnett, J.C. Am. J. Physiol. Renal Physiol. (2006) [Pubmed]
  8. OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats. Yamamura, Y., Nakamura, S., Itoh, S., Hirano, T., Onogawa, T., Yamashita, T., Yamada, Y., Tsujimae, K., Aoyama, M., Kotosai, K., Ogawa, H., Yamashita, H., Kondo, K., Tominaga, M., Tsujimoto, G., Mori, T. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  9. Vasopressin v(2) receptor blockade with tolvaptan versus fluid restriction in the treatment of hyponatremia. Gheorghiade, M., Gottlieb, S.S., Udelson, J.E., Konstam, M.A., Czerwiec, F., Ouyang, J., Orlandi, C. Am. J. Cardiol. (2006) [Pubmed]
  10. Tolvaptan: a selective vasopressin type 2 receptor antagonist in congestive heart failure. Rangasetty, U.C., Gheorghiade, M., Uretsky, B.F., Orlandi, C., Barbagelata, A. Expert opinion on investigational drugs. (2006) [Pubmed]
  11. Effects of tolvaptan, a vasopressin antagonist, in patients hospitalized with worsening heart failure: a randomized controlled trial. Gheorghiade, M., Gattis, W.A., O'Connor, C.M., Adams, K.F., Elkayam, U., Barbagelata, A., Ghali, J.K., Benza, R.L., McGrew, F.A., Klapholz, M., Ouyang, J., Orlandi, C. JAMA (2004) [Pubmed]
  12. Current treatments and novel pharmacologic treatments for hyponatremia in congestive heart failure. Goldsmith, S.R. Am. J. Cardiol. (2005) [Pubmed]
  13. New agents for managing hyponatremia in hospitalized patients. Munger, M.A. American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists (2007) [Pubmed]
  14. Tolvaptan administration does not affect steady state amiodarone concentrations in patients with cardiac arrhythmias. Shoaf, S.E., Elizari, M.V., Wang, Z., Sekar, K., Grinfeld, L.R., Barbagelata, N.A., Lerman, J., Bramer, S.L., Trongé, J., Orlandi, C. J. Cardiovasc. Pharmacol. Ther. (2005) [Pubmed]
  15. Tolvaptan (Otsuka). Doggrell, S.A. Current opinion in investigational drugs (London, England : 2000) (2004) [Pubmed]
  16. Effects of oral tolvaptan in patients hospitalized for worsening heart failure: the EVEREST Outcome Trial. Konstam, M.A., Gheorghiade, M., Burnett, J.C., Grinfeld, L., Maggioni, A.P., Swedberg, K., Udelson, J.E., Zannad, F., Cook, T., Ouyang, J., Zimmer, C., Orlandi, C. JAMA (2007) [Pubmed]
  17. Vasopressin V2-receptor blockade with tolvaptan in patients with chronic heart failure: results from a double-blind, randomized trial. Gheorghiade, M., Niazi, I., Ouyang, J., Czerwiec, F., Kambayashi, J., Zampino, M., Orlandi, C. Circulation (2003) [Pubmed]
 
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