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2-methoxyestradiol (CASI Pharmaceuticals, Inc., 043ca6)
- Development stage
- Unknown
- Lead developer
- CASI Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
2-methoxyestradiol (2-ME) is an endogenous metabolite of 17β-estradiol that possesses potent antiangiogenic and antiproliferative activities. It functions primarily by disrupting microtubule dynamics and inhibiting the expression of hypoxia-inducible factor-1α (HIF-1α), which leads to cell cycle arrest and the induction of apoptosis. Developed by CASI Pharmaceuticals (formerly EntreMed), it has been evaluated in clinical trials for various malignancies, including metastatic hormone-refractory prostate cancer, multiple myeloma, and glioblastoma multiforme. To overcome its poor oral bioavailability, a nanocrystal colloidal dispersion formulation known as Panzem NCD was developed for clinical use.
- Brand names
- Panzem
- Other names
- 2-methoxyestradiol nanocrystal colloidal dispersionPanzem NCD
02
Targets
CFLAR (CASP8 and FADD-like apoptosis regulator)ESR1 (ERα)ESR2 (ERβ)GPER1 (G protein-coupled estrogen receptor 1)HIF1A (Hypoxia-inducible factor 1-alpha)MST1R (Recepteur d'origine nantais)TUBB (Tubulin (alpha and beta subunits))VEGFA (Vascular endothelial growth factor A)
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