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2-methoxyestradiol (CASI Pharmaceuticals, Inc.)
- Development stage
- Unknown
- Lead developer
- CASI Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
2-methoxyestradiol is a naturally occurring metabolite of estradiol with potent anti-angiogenic and anti-tumor properties. It acts primarily by inhibiting microtubule polymerization and destabilizing microtubules, which leads to cell cycle arrest in the G2/M phase. Additionally, it inhibits the expression and activity of hypoxia-inducible factor 1-alpha (HIF-1α), thereby reducing the production of vascular endothelial growth factor (VEGF) and suppressing tumor angiogenesis. Developed by CASI Pharmaceuticals (formerly EntreMed), it has been investigated in various formulations, including a nanocrystal colloidal dispersion (Panzem NCD), for the treatment of metastatic renal cell carcinoma, multiple myeloma, and prostate cancer.
- Brand names
- Panzem
- Other names
- 2-ME2-methoxyestradiol nanocrystal colloidal dispersionPanzem NCD
02
Targets
TUBB (Tubulin (alpha and beta subunits))HIF1A (Hypoxia-inducible factor 1-alpha)
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