NCIt definition : An orally active small molecule with potential antineoplastic activity. Although its
mechanism of action has yet to be fully elucidated, HIF1-alpha inhibitor PX-478 appears
to inhibit hypoxia-inducible factor 1-alpha (HIF1A) expression, which may result in
decreased expression of HIF1A downstream target genes important to tumor growth and
survival, a reduction in tumor cell proliferation, and the induction of tumor cell
apoptosis. The inhibitory effect of this agent is independent of the tumor suppressor
genes VHL and p53 and may be related to derangements in glucose uptake and metabolism
due to inhibition of glucose transporter-1 (Glut-1).;