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Erschienen in: Drugs 15/2008

01.10.2008 | Adis Drug Profile

Ambrisentan

verfasst von: Jamie D. Croxtall, Susan J. Keam

Erschienen in: Drugs | Ausgabe 15/2008

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Abstract

  • ▴ 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.
  • ▴ 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.
  • ▴ 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.
  • ▴ 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.
  • ▴ 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%.
  • ▴ Treatment with ambrisentan for up to 2.8 years was generally well tolerated in clinical trials.
Fußnoten
1
The use of trade names is for identification purposes only and does not imply endorsement.
 
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Metadaten
Titel
Ambrisentan
verfasst von
Jamie D. Croxtall
Susan J. Keam
Publikationsdatum
01.10.2008
Verlag
Springer International Publishing
Erschienen in
Drugs / Ausgabe 15/2008
Print ISSN: 0012-6667
Elektronische ISSN: 1179-1950
DOI
https://doi.org/10.2165/00003495-200868150-00008

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