Tezosentan - Misplaced Pages

Chemical compound Pharmaceutical compound

Tezosentan
Clinical data


ATC code	none
Identifiers
IUPAC name N-pyrimidin-4-yl]-5-propan-2-ylpyridine-2-sulfonamide
CAS Number	180384-57-0
PubChem CID	151174
ChemSpider	133242
UNII	64J9J55263
ChEMBL	ChEMBL61780
CompTox Dashboard (EPA)	DTXSID20170956
Chemical and physical data
Formula	C₂₇H₂₇N₉O₆S
Molar mass	605.63 g·mol
3D model (JSmol)	Interactive image
SMILES O=S(=O)(c1ncc(cc1)C(C)C)Nc3nc(nc(OCCO)c3Oc2ccccc2OC)c5ccnc(c4nnn4)c5
InChI InChI=1S/C27H27N9O6S/c1-16(2)18-8-9-22(29-15-18)43(38,39)34-26-23(42-21-7-5-4-6-20(21)40-3)27(41-13-12-37)31-24(30-26)17-10-11-28-19(14-17)25-32-35-36-33-25/h4-11,14-16,37H,12-13H2,1-3H3,(H,30,31,34)(H,32,33,35,36) Key:TUYWTLTWNJOZNY-UHFFFAOYSA-N
(verify)

Tezosentan is a non-selective ET_A and ET_B receptor antagonist. It acts as a vasodilator and was designed by Actelion as a therapy for patients with acute heart failure. However, studies showed that tezosentan did not improve dyspnea or reduce the risk of fatal or nonfatal cardiovascular events.

References

Urbanowicz W, Sogni P, Moreau R, Tazi KA, Barriere E, Poirel O, et al. (December 2004). "Tezosentan, an endothelin receptor antagonist, limits liver injury in endotoxin challenged cirrhotic rats". Gut. 53 (12). BMJ Publishing Group Ltd & British Society of Gastroenterology: 1844–9. doi:10.1136/gut.2003.036517. PMC 1774327. PMID 15542526.
"Tezosentan does not appear to improve symptoms for patients with acute heart failure". Medical Studies/Trials. news-medical.net. 7 Nov 2007. Retrieved 2007-11-24.

Sympatholytic (and closely related) antihypertensives (C02)

Sympatholytics
(antagonize α-adrenergic
vasoconstriction)

Central

α₂-Adrenergic receptor agonists	Clonidine Guanabenz Guanfacine Guanoxabenz Methyldopa Tiamenidine
Adrenergic release inhibitors	Bethanidine Bretylium Debrisoquine Guanadrel Guanazodine Guancydine Guanethidine Guanoclor Guanoxan
Imidazoline receptor agonists	Moxonidine Rilmenidine Tolonidine
Ganglion-blocking/nicotinic antagonists	Hexamethonium Mecamylamine Pentolinium Trimethaphan

Peripheral

Indirect

Monoamine oxidase inhibitors	Pargyline
VMAT inhibitors	Bietaserpine Deserpidine Methoserpidine Reserpine Syrosingopine
Tyrosine hydroxylase inhibitors	Metirosine

Direct

α₁-Adrenergic receptor blockers	Doxazosin Ketanserin Indoramin Prazosin Trimazosin Urapidil
Non-selective α-adrenergic receptor blockers	Phentolamine

Other antagonists

Serotonin receptor antagonists	Ketanserin Lidanserin
Endothelin receptor antagonists (for PHTooltip Pulmonary hypertension)	dual (Aprocitentan, Bosentan, Macitentan (+tadalafil), Riociguat) selective (Ambrisentan (+tadalafil), Sitaxentan, Sotatercept)

WHO-EM
Withdrawn from market
Clinical trials:
- Phase III
- Never to phase III

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