Catalog No.S2097 Synonyms: LU-208075,BSF-208075
Molecular Weight(MW): 378.42
Ambrisentan is a highly selective antagonist of the endothelin-1 type A receptor, used in the treatment of pulmonary arterial hypertension (PAH).
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Choose Selective Endothelin Receptor Inhibitors
|Description||Ambrisentan is a highly selective antagonist of the endothelin-1 type A receptor, used in the treatment of pulmonary arterial hypertension (PAH).|
Ambrisentan only increases intracellular calcein fluorescence in P388/dx cells at concentrations above 100 μM and in L-MDR1 cells not at all indicating negligible P-gp inhibition.  Ambrisentan inhibits specific [(125)I]ET-1 binding in these tissues in a concentration-dependent manner.  Ambrisentan undergoes oxidative metabolism mainly by cytochrome P450 (CYP) 3A4 and to a lesser extent by CYP3A5 and CYP2C19. Ambrisentan is not only a strong inducer of CYP3A4, but also of ABCB1 and ABCG2. Ambrisentan also has a concentration-dependent effect on PXR activity, but because plateau effects are not reached, an EC50-value could not be calculated.  Ambrisentan inhibits specific [(125)I]ET-1 binding in a concentration-dependent manner at nanomolar ranges of IC50. Ambrisentan significantly increases the dissociation constant for bladder [(125)I]ET-1 binding without affecting maximal number of binding sites (Bmax). Ambrisentan seem to bind to bladder ET-1 receptor in a competitive and reversible manner.  Ambrisentan is an effective and safe treatment which is a valuable addition to the armamentarium against PAH. Ambrisentan offers a relative lack of drug interactions, once daily dosing and reassuring liver safety, offering safety and convenience advantages over bosentan. 
-  Weiss J, et al. Eur J Pharmacol,?011, 660(2-3), 298-304.
-  Yokoyama Y, et al. Biol Pharm Bull,?014, 37(3), 461-465.
-  Weiss J, et al. Biochem Pharmacol,?013, 85(2), 265-273.
|In vitro||DMSO||76 mg/mL (200.83 mM)|
|Ethanol||22 mg/mL (58.13 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02885012||Recruiting||Pulmonary Arterial Hypertension||Medical University of South Carolina|Ochsner Health System||June 2016||Phase 4|
|NCT02688387||Recruiting||Hypertension, Pulmonary||GlaxoSmithKline|Covance Harrogate|Hammersmith Medicines Research||March 2016||Phase 1|
|NCT02253394||Recruiting||Pulmonary Arterial Hypertension||Brigham and Womens Hospital|Gilead Sciences||September 2015||Phase 4|
|NCT02712346||Recruiting||Sickle Cell Anemia||Augusta University|Gilead Sciences|National Heart, Lung, and Blood Institute (NHLBI)||September 2015||Phase 1|
|NCT02080637||Recruiting||Hypoplastic Left Heart Syndrome|Hypoplastic Right-sided Heart Complex||Kevin Hill|Duke University||July 2015||Phase 2|
|NCT02290613||Unknown status||Systemic Sclerosis|Pulmonary Hypertension||Heidelberg University|GlaxoSmithKline||December 2014||Phase 2|
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