Macitentan

Definition

An orally available dual endothelin receptor (ETR) antagonist with potential antihypertensive and antineoplastic activity. Upon administration, macitentan and its metabolites block the binding of endothelin isoform 1 (ET-1) to type-A and type-B ETR on both the tumor cells and the endothelial cells in the tumor vasculature. This prevents ET-1 mediated signaling transduction which may decrease tumor cell proliferation, progression, and angiogenesis in tumor tissue. ET-1, a potent vasoconstrictor that plays an important role in inflammation and tissue repair, is, together with its receptors, overexpressed varyingly in many tumor cell types.

Also known as ACT-064992, Actelion-1, MACITENTAN, N-(5-(4-Bromophenyl)-6-(2-((5-Bromopyrimidin-2-Yl)Oxi)Ethoxy)Pyrimidin-4-Yl)-N'-Propylsulfuric Diamide — per NCIT

Also identified as

• ATC C02KX04 per RXNORM
• NCIT NCIT:C87728 per NCIT
• SCTID 710283008 per RXNORM
• SCTID 715555005 per RXNORM
• UNII Z9K9Y9WMVL per RXNORM

Indications