2-methoxyestradiol

**Description:** 2-methoxyestradiol (also known as 2ME2 or 2-MeOE2) is a naturally occurring endogenous metabolite of estradiol. It functions primarily as an angiogenesis inhibitor by preventing the formation of new blood vessels that tumors require for growth. Mechanistically, it inhibits endothelial cell proliferation and induces apoptosis in these cells[3][4]. Additionally, it disrupts microtubule assembly by inhibiting tubulin polymerization and interfering with mitotic spindle dynamics, leading to cell cycle arrest in cancer cells—even those lacking estrogen receptors[8]. Preclinical studies have shown anti-proliferative activity against various tumor types and potential efficacy in inflammatory diseases such as rheumatoid arthritis[5][6]. Despite promising anticancer properties demonstrated in vitro and early-phase clinical trials (notably for breast cancer), its development has been hampered by low oral bioavailability and high pharmacokinetic variability[5].

Brand names

PulmoLAR

Other names

2-methoxyestradiol2ME22-MeOE2