Bosentan

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Bosentan
Systematic (IUPAC) name
N-[6-(2-hydroxyethoxy)-5- (2-methoxyphenoxy) -2-pyrimidin-2-yl-pyrimidin-4-yl] -4-tert- butyl-benzenesulfonamide
Identifiers
CAS number	147536-97-8
ATC code	C02KX01
PubChem	104865
DrugBank	APRD00829
Chemical data
Formula	C27H29N5O6S
Mol. mass	551.615 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	50%
Protein binding	>98%
Metabolism	Hepatic
Half life	5 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	X
Legal status	℞ Prescription only
Routes	Oral

Bosentan (BOZENTAN) is a dual endothelin receptor antagonist important in the treatment of pulmonary artery hypertension (PAH). It is licensed in the United States, the European Union and other countries by Actelion Pharmaceuticals for the management of PAH under the trade name Tracleer.

Contents 1 Mechanism of Action 2 Clinical uses 3 External links 4 See also

[edit] Mechanism of Action

Bosentan is a competitive antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors. When endothelin-1 binds to these receptors, pulmonary artery pressure is elevated. By blocking this interaction, bosentan in able to lower pulmonary artery pressure. Bosentan has a slightly higher affinity for ET-A than ET-B.

[edit] Clinical uses

Bosentan is indicated for the treatment of pulmonary hypertension.

[edit] External links

• Tracleer official website
• Tracleer prescribing information

[edit] See also

• Sitaxsentan
• Ambrisentan

v • d • e Medications used in the management of pulmonary arterial hypertension (B01, C02) Prostacyclin analogues Beraprost, Epoprostenol, Iloprost, Treprostinil Endothelin receptor antagonists Ambrisentan, Bosentan, Sitaxsentan PDE5 inhibitors Sildenafil, Tadalafil Adjunctive therapy Calcium channel blockers, Diuretics, Digoxin, Oxygen therapy, Warfarin

v • d • e Antihypertensives (C02) and diuretics (C03) Sympatholytic agents (including alpha) centrally acting/antiadrenergics: Clonidine • Guanfacine • Methyldopa • Moxonidine • Rilmenidine • adrenergic uptake inhibitor (Rescinnamine, Reserpine) ganglion-blocking/nicotinic antagonist (Mecamylamine, Trimethaphan) peripherally acting/antiadrenergics (Prazosin, Guanethidine, Indoramin, Doxazosin) Vasodilators Diazoxide • Hydralazine • Minoxidil • Nitroprusside • Phentolamine Other antihypertensives serotonin antagonist (Ketanserin) • endothelin receptor antagonist (Bosentan, Ambrisentan, Sitaxsentan) Low ceiling diuretics Thiazide (Bendroflumethiazide, Chlorothiazide, Hydrochlorothiazide) • Chlortalidone • Indapamide • Quinethazone • Mersalyl • Metolazone • Theobromine • Cicletanine High ceiling diuretics Loop diuretic (Bumetanide, Furosemide, Torasemide) Potassium-sparing diuretics ESC blockers (Amiloride, Triamterene) • aldosterone antagonists (Spironolactone, Eplerenone, Potassium canrenoate, Canrenone)