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]).
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 60 mg/mL
Ethanol 20 mg/mL
Long-term ambrisentan therapy for the treatment of pulmonary arterial hypertension.
Oudiz RJ, et al. J Am Coll Cardiol. 2009 Nov 17;54(21):1971-81. PMID: 19909879.
Ambrisentan, a non-peptide endothelin receptor antagonist.
Vatter H, et al. Cardiovasc Drug Rev. 2006 Spring;24(1):63-76. PMID: 16939634.
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