Sitaxentan

Structural formula
General
Non-proprietary name	Sitaxentan
other names	N - (4-chloro-3-methylisoxazol-5-yl) -2 - [(4,5-methylenedioxy-2-methylphenyl) acetyl] thiophene-3-sulfonamide; Sitaxentanum ( Latin );
Molecular formula	C 18 H 15 ClN 2 O 6 S 2
External identifiers / databases
PubChem	216235
ChemSpider	187436
DrugBank	DB06268
Wikidata	Q905664
Drug information
ATC code	C02 KX03
Drug class	Antihypertensive drugs
Mechanism of action	Endothelin receptor antagonist
properties
Molar mass	454,90 g · mol -1
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
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 .

Sitaxentan (trade name: Thelin ^® , manufacturer: Encysive , a subsidiary of the Pfizer group) is an endothelin receptor antagonist and was used as an alternative to ambrisentan and bosentan as an orphan drug for the treatment of rare pulmonary hypertension ( pulmonary hypertension , NYHA stage III ) authorized.

pharmacology

In clinical studies, sitaxentan has been shown to improve exercise capacity in patients with pulmonary hypertension and slow the progression of symptoms. At the same time, the blood flow to the lungs improves as the pulmonary arteries expand.

Other Information

Sitaxentan had been on the market in Germany since December 2006 and was sold in the form of tablets. The daily therapy costs were around 117 euros. Patients who take the drug (1 tablet daily) have to have their liver values measured monthly, as the class of endothelin receptor antagonists can impair liver function. After two deaths from liver failure associated with taking the drug, the drug was withdrawn from the market in Germany in December 2010.

Individual evidence

↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
↑ Robyn J. Barst, Stuart Rich, Allison Widlitz, Evelyn M. Horn, Vallerie McLaughlin, Joyce McFarlin: Clinical Efficacy of Sitaxsentan, an Endothelin-A Receptor Antagonist, in Patients With Pulmonary Arterial Hypertension . In: Chest . tape 121 , no. 6 , 2002, pp. 1860–1868 , doi : 10.1378 / chest.121.6.1860 , PMID 12065350 (free full text).
↑ Online edition Deutsches Ärzteblatt, December 10, 2010: Fatal Liver Damage: Thelin's withdrawal from the market ( Memento of December 16, 2010 in the Internet Archive ).

[NV-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] Robyn J. Barst, Stuart Rich, Allison Widlitz, Evelyn M. Horn, Vallerie McLaughlin, Joyce McFarlin: Clinical Efficacy of Sitaxsentan, an Endothelin-A Receptor Antagonist, in Patients With Pulmonary Arterial Hypertension . In: Chest . tape 121 , no. 6 , 2002, pp. 1860–1868 , doi : 10.1378 / chest.121.6.1860 , PMID 12065350 (free full text).

[3] Online edition Deutsches Ärzteblatt, December 10, 2010: Fatal Liver Damage: Thelin's withdrawal from the market ( Memento of December 16, 2010 in the Internet Archive ).