NCIt definition : An orally bioavailable liquid formulation containing the small molecule 2-methoxyestradiol
with potential antineoplastic activity. 2-Methoxyestradiol, a naturally occurring
estradiol metabolite, exerts its antitumor effect by inhibiting endothelial cells
as well as tumor cells through multiple mechanisms. This agent binds to tubulin and
disrupts microtubule formation, thereby preventing mitosis and subsequent cellular
proliferation. In addition, 2-methoxyestradiol induces caspase activation, resulting
in cell cycle arrest in G2 phase and apoptosis in due course. This agent also down-regulates
hypoxia inducible factor-one alpha (HIF-1a). The nanocrystal colloidal dispersion
increases the absorption of 2-methoxyestradiol, thereby improving its bioavailability,
which results in enhanced drug plasma levels.;
Semantic type(s)