NCIt definition : An orally active, small molecule inhibitor of hypoxia inducible factor (HIF)-2alpha,
with potential antineoplastic activity. Upon oral administration, HIF-2alpha inhibitor
PT2385 allosterically binds to HIF-2alpha, thereby preventing HIF-2alpha heterodimerization
and its subsequent binding to DNA. This results in decreased transcription and expression
of HIF-2alpha downstream target genes, many of which regulate tumor cell growth and
survival. Blocking HIF-2alpha reduces the proliferation of HIF-2alpha-expressing tumor
cells. HIF-2alpha, a heterodimeric transcription factor overexpressed in many cancers,
promotes tumorigenesis.;