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Ambrisentan is an oral, once-daily endothelin receptor antagonist that is selective for the endothelin type A receptor. Ambrisentan is indicated for the treatment of pulmonary arterial hypertension (PAH). Once daily oral ambrisentan 2.5 to 10 mg/day significantly improved exercise capacity (6-minute walk distance) compared with placebo in two double-blind, multicenter trials (ARIES-1 & ARIES-2). A decrease in dyspnea and a delay in clinical worsening were among the improvements in secondary outcomes generally observed with ambrisentan versus placebo. In ARIES-E, a 2-year extension of ARIES-1 and -2, approved dosages of ambrisentan (5 and 10 mg/day) were associated with a sustained improvement in 6MWD, a generally sustained improvement in dyspnea, and a low risk of clinical worsening and of death. Six months' treatment with ambrisentan 5 mg/day significantly improved 6MWD (primary outcome measure) and dyspnea relative to baseline in an open-label, non-comparative, multicenter study in a diverse population of patients with PAH or non-PAH forms of pulmonary hypertension (ARIES-3 [n = 224]).
| Molecular Weight | 378.42 |
| Formula | C22H22N2O4 |
| CAS Number | 177036-94-1 |
| Solubility (25°C) | DMSO 60 mg/mL Ethanol 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Vatter H, et al. Cardiovasc Drug Rev. Ambrisentan, a non-peptide endothelin receptor antagonist.
| Related Endothelin Receptor Products |
|---|
| Zibotentan
Zibotentan (ZD4054) is a more selective and specific endothelin-A receptor (ETAR) antagonist with an IC50 value of 21 nM. |
| Sitaxsentan sodium
Sitaxsentan (TBC-11251) is an orally active, highly selective antagonist of endothelin A receptors. |
| Macitentan
Macitentan is an orally-active, tissue-targeting dual ET receptor antagonist. |
| Bosentan Hydrate
Bosentan is an endothelin (ET) receptors antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. |
| Bosentan
Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. |
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