NCIt 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.;
UNII : Z9K9Y9WMVL;
InChIKey : JGCMEBMXRHSZKX-UHFFFAOYSA-N;
CAS number : 441798-33-0; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 441798-33-0
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