Tezosentan

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Structural formula
Structural formula tezosentan
General
Non-proprietary name Tezosentan
other names
  • N - {6- (2-hydroxyethoxy) -5- (2-methoxyphenoxy) -2- [2- (1 H -tetrazol-5-yl) -4-pyridyl] pyrimidin-4-yl} -5-isopropylpyridin- 2-sulfonamide ( IUPAC )
  • RITZ 1 (Actelion / Genentech)
Molecular formula C 27 H 27 N 9 O 6 S
External identifiers / databases
CAS number 180384-57-0
PubChem 151174
ChemSpider 133242
DrugBank DB06558
Wikidata Q426203
Drug information
Mechanism of action

Endothelin - antagonist

properties
Molar mass 605.63 g · mol -1
safety instructions
GHS hazard labeling
no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Tezosentan is a potential drug from the group of endothelin receptor antagonists that was developed by the Swiss pharmaceutical company Actelion . He should for treatment of acute heart failure are used.

However, recent studies have shown that tezosentan does not improve dyspnoea or reduce the risk of cardiovascular events.

pharmacology

Tezosentan is a competitive antagonist of endothelin - receptors A and B. By inhibition of binding of endothelin-1 , endothelin-3 and sarafotoxin to the endothelin receptors A and B, tezosentan prevents constriction of the smooth muscle .

The plasma half-life is 3–5  min and the plasma protein binding 0.2–60  μg / ml .

The disodium salt is used medicinally.

literature

  • M. Clozel, H. Ramuz, V. Breu, P. Hess, B. Löffler, P. Coassolo, S. Roux: Journal of pharmacology and experimental therapeutics . 290 (2), pp. 840-842 (1999)
  • A. Driver, PLM VanGiersbergen, J. Dingemanse: Xenobiotica . 33 (4), pp. 399-414 (2001)
  • J. Bergler-Klein, R. Pacher: Journal for Cardiology 9 (5), pp. 169–175 (2002)

Individual evidence

  1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
  2. ↑ McMurray JJ, Teerlink JR, Cotter G, et al. : Effects of tezosentan on symptoms and clinical outcomes in patients with acute heart failure: the VERITAS randomized controlled trials . In: JAMA: The Journal of the American Medical Association . 298, No. 17, November 2007, pp. 2009-2019. PMID 17986694 .
  3. ↑ JJV McMurray, JR Teerlink, G. Cotter et al .: Outcomes in Patients With Acute Heart Failure . In: The Journal of the American Medical Association . tape 17 , no. 298 , 2007, doi : 10.1001 / jama.298.17.2009 .
  4. ↑ Urbanowicz W, Sogni P, Moreau R, et al. : Tezosentan, an endothelin receptor antagonist, limits liver injury in endotoxin challenged cirrhotic rats . In: Good . 53, No. 12, December 2004, pp. 1844-1849. PMID 15542526 . PMC 1774327 (free full text).

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