PMID- 17385944 OWN - NLM STAT- MEDLINE DCOM- 20070705 LR - 20181113 IS - 0012-6667 (Print) IS - 0012-6667 (Linking) VI - 67 IP - 5 DP - 2007 TI - Sitaxentan: in pulmonary arterial hypertension. PG - 761-70; discussion 771-2 AB - Sitaxentan is a highly selective endothelin (ET)(A) receptor antagonist, with an approximately 6500 higher affinity for ET(A) than ET(B) receptors. In pulmonary arterial hypertension (PAH), elevated ET-1 levels are strongly correlated with disease severity and prognosis. Sitaxentan 100 mg once daily was efficacious in the management of moderate to severe PAH in the pivotal, 12-18 week, large (n > or = 98), well designed, placebo-controlled STRIDE-1, -2 and -4 trials. In the STRIDE-1 and -2 trials (the majority of patients had New York Heart Association [NYHA]/WHO functional class III PAH), sitaxentan-treated patients experienced significantly greater improvements from baseline in distance walked over 6 minutes (6MWD; primary endpoint in STRIDE-2) and in NYHA/WHO functional class than placebo recipients. In STRIDE-4, although there was no between-group difference in terms of improvements in 6MWD in the primary analysis of patients across all WHO functional classes (61% were functional class II) [primary endpoint], improvements in 6MWD significantly favoured sitaxentan versus placebo-treated patients in a post hoc subgroup analysis of those with WHO functional class III or IV disease. The beneficial effects of sitaxentan therapy on exercise capacity and NYHA/WHO functional class were maintained after up to 2 years' treatment. Treatment with sitaxentan for up to 2 years was generally well tolerated in clinical trials. FAU - Scott, Lesley J AU - Scott LJ AD - Wolters Kluwer Health/ Adis, Auckland, New Zealand. demail@adis.co.nz LA - eng PT - Journal Article PT - Review PL - New Zealand TA - Drugs JT - Drugs JID - 7600076 RN - 0 (Endothelin A Receptor Antagonists) RN - 0 (Isoxazoles) RN - 0 (Receptor, Endothelin A) RN - 0 (Thiophenes) RN - J9QH779MEM (sitaxsentan) SB - IM MH - *Endothelin A Receptor Antagonists MH - Humans MH - Hypertension, Pulmonary/*drug therapy/metabolism MH - Isoxazoles/administration & dosage/*therapeutic use MH - Randomized Controlled Trials as Topic MH - Receptor, Endothelin A/metabolism MH - Thiophenes/administration & dosage/*therapeutic use MH - Treatment Outcome RF - 34 EDAT- 2007/03/28 09:00 MHDA- 2007/07/06 09:00 CRDT- 2007/03/28 09:00 PHST- 2007/03/28 09:00 [pubmed] PHST- 2007/07/06 09:00 [medline] PHST- 2007/03/28 09:00 [entrez] AID - 6757 [pii] AID - 10.2165/00003495-200767050-00007 [doi] PST - ppublish SO - Drugs. 2007;67(5):761-70; discussion 771-2. doi: 10.2165/00003495-200767050-00007.