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20-September-2008 09:55:50 - Sitaxsentan Sitaxsentan Systematic IUPAC name N-4-chloro-3-methyl-oxazol-5-yl-2-2-6-methylbenzo 1,3dioxol-5-ylacetylthiophene-3-sulfonamide Identifiers CAS number 210421-64-0 ATC code C02KX03 PubChem 216235 Chemical data Formula C18H15ClN2O6S2 Mol. mass 454.906 g/mol SMILES eMolecules PubChem Pharmacokinetic data Bioavailability 70 to 100% Protein binding 99% Metabolism Hepatic CYP2C9- and CYP3A4-mediated Half life 10 hours Excretion Renal 50 to 60% Fecal 40 to 50% Therapeutic considerations Licence data EU Pregnancy cat. ? Legal status Prescription Only S4AU POMUK Routes Oral Sitaxsentan or sitaxsentan sodium actual INN: sitaxentan marketed as Thelin by Encysive Pharmaceuticals is a small molecule sodium salt that blocks the action of endothelin ET on the endothelin-A ETA receptor selectively by a factor of 6000 compared to the ETB. It is a sulfonamide class endothelin receptor antagonist ERA and is undergoing Food and Drug Administration FDA review for treating pulmonary hypertension. The rationale for benefit compared to bosentan, a nonselective ET blocker, is negligible inhibition of the beneficial effects of ETB stimulation, such as nitric oxide production and clearance of ET from circulation. However, in clinical trials, the efficacy of sitaxsentan has been much the same as bosentan, but the liver toxicity has been better. Therefore sitaxsentan is expected to be marketed as a safer drug than bosentan, but not necessarily more effective. Contents 1 Regulatory status 2 Adverse effects 3 External links 4 References Regulatory status Thelin has been approved for marketing in both the European Union on 10 August 2006, in Canada1 and in Australia on 7 March 2007. By February 2008 it had been launched commercially in Germany, Austria, The Netherlands, the United Kingdom, Ireland, France, Spain and Italy. On the Prescription Drug User Fee Act PDUFA target action date of 24 March 2006 the United States' FDA recommended an approvable status to Thelin but said it would not yet approve the product. On July 24, 2006 Thelin received a second approvable letter stating that efficacy outcome issues raised in the context of the STRIDE-2 study were still unresolved. In July 2007, Encysive commenced a formal dispute resolution process in a preliminary meeting with the FDA. However, in September 2007 the company announced that it was making preparations for another phase III clinical trial STRIDE-5 to overcome the FDA's deficiency claims concerning the New Drug Application, and that it would not pursue the dispute resolution process 2. Adverse effects Adverse effects observed with Thelin are class effects of endothelin receptor antagonists, and include : liver enzyme abnormalities increased ALT and AST headache oedema constipation nasal congestion upper respiratory tract infection dizziness insomnia flushing. Because Thelin inhibits metabolism of warfarin, a decreased dose of warfarin is needed when co-administered with thelin. This is because warfarin acts to prevent blood from clotting, and if it remains unmetabolized, it can continue to thin the blood. External links http://www.drugs.com/nda/thelin_050714.html References ^ UPDATE 1-Encysive gets Canadian approval for hypertension drug. Reuters May 30, 2007. Retrieved on 2007-07-08. ^ Encysive Pharmaceuticals to Conduct Phase III Study With Thelin Sitaxsentan Sodium in Pulmonary Arterial Hypertension. PrimeNewswire via COMTEX News Network September 29, 2007. Retrieved on 2007-12-12. Girgis RE, Frost AE, Hill NS, Horn EM, Langleben D, Mc Laughlin VV, Oudiz RJ, Robbins IM, Seibold JR, Shapiro S, Tapson VF, Barst RJ. 'Selective endothelinA receptor antagonism with sitaxsentan for pulmonary arterial hypertension associated with connective tissue disease' ARD 2007 0: ard.2007.069609v2 ATS 2005. The International Conference of the American Thoracic Society. 20 May - 25 May 2005. San Diego, CA. American Heart Association. Primary or Unexplained Pulmonary Hypertension Barst RJ, Langleben D, Frost A et al. Sitaxsentan therapy for pulmonary arterial hypertension. American Journal of Respiratory Critical Care Medicine 2004 15 February 2004 ;1694:441-7. Electronic publication 20 November 2003. Robyn J. Barst, MD; Stuart Rich, MD, FCCP; Allison Widlitz, MS, PA; Evelyn M. Horn, MD; Vallerie McLaughlin, MD and Joyce McFarlin, RN : Clinical Efficacy of Sitaxsentan, an Endothelin-A Receptor Antagonist, in Patients With Pulmonary Arterial Hypertension Chest. 2002;121:1860-1868. 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 Centrally acting/antiadrenergics α2 agonist Clonidine, Guanfacine, Methyldopa imidazoline receptor agonist Moxonidine, Rilmenidine adrenergic uptake inhibitor Rescinnamine, Reserpine Ganglion-blocking/nicotinic antagonist Mecamylamine, Trimethaphan Peripherally acting/antiadrenergics α1 blockers: Prazosin Indoramin Trimazosin Doxazosin Urapidil Guanidine derivatives: Betanidine Guanethidine Guanoxan Debrisoquine Guanoclor Guanazodine Guanoxabenz Vasodilators Diazoxide hydrazinophthalazine Hydralazine, Dihydralazine, Endralazine, Cadralazine Minoxidil Nitroprusside Phentolamine Other antihypertensives serotonin antagonist Ketanserin endothelin receptor antagonist Bosentan, Ambrisentan, Sitaxsentan MAOI Pargyline THI Metirosine Diuretics Low ceiling Thiazides at DCT Bendroflumethiazide Hydroflumethiazide Hydrochlorothiazide Chlorothiazide Polythiazide Trichlormethiazide Cyclopenthiazide Methyclothiazide Cyclothiazide Mebutizide Sulfonamides Quinethazone Clopamide Chlortalidone Mefruside Clofenamide Metolazone Meticrane Xipamide Indapamide Clorexolone Fenquizone Other Mersalyl Theobromine Cicletanine osmotic Mannitol, Urea carbonic anhydrase inhibitor at PT Acetazolamide High ceiling Loop diuretic at AL Bumetanide, Furosemide, Torasemide, Ethacrynic acid Potassium-sparing at CD ESC blockers Amiloride, Triamterene aldosterone antagonists Spironolactone, Eplerenone, Potassium canrenoate, Canrenone Retrieved from http://en..org/wiki/Sitaxsentan Categories: Endothelin receptor antagonists | Thiophenes | Isoxazoles Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Deutsch This page was last modified on 28 May 2008, at 15:29
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