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01.10.2008 | Adis Drug Profile
Ambrisentan
Erschienen in: Drugs | Ausgabe 15/2008
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▴ Elevated endothelin (ET)-1 levels are strongly correlated with the pathogenesis and prognosis of pulmonary arterial hypertension (PAH). Ambrisentan is an orally active, highly selective ETa receptor antagonist with >4000-fold higher selectivity over the ETb receptor.
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▴ In two large, well designed, 12-week, placebo-controlled, phase III trials (ARIES-1, n = 202 and ARIES-2, n = 192) in patients with PAH (WHO group I), ambrisentan 2.5–10 mg once daily significantly increased 6-minute walk distance by 31–59 m from baseline (primary outcome measure) versus placebo.
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▴ The incidence of clinical worsening (secondary outcome measure) was significantly delayed for the combined ambrisentan 5 mg once daily groups versus the combined placebo groups from ARIES-1 and -2.
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▴ At week 12, WHO functional class distribution was significantly improved with once-daily ambrisentan 5 mg, and Borg dyspnoea scores were significantly improved with ambrisentan 2.5–10 mg versus placebo in combined data from the ARIES-1 and -2 trials.
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▴ The beneficial effects of ambrisentan on exercise capacity, WHO functional class and Borg dyspnoea scores seen at 12 weeks were maintained at 48 weeks in the ARIES-E phase III extension trial (n = 361). One-year survival rates with ambrisentan were 95–97%.
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▴ Treatment with ambrisentan for up to 2.8 years was generally well tolerated in clinical trials.