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2-methoxyestradiol + sunitinib
- Development stage
- Discontinued
- Lead developer
- CASI Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
**2-methoxyestradiol + sunitinib** is an experimental oral combination therapy investigated primarily for the treatment of metastatic renal cell carcinoma (RCC) in patients who have progressed on sunitinib monotherapy. 2-methoxyestradiol (2ME2) is a natural estradiol metabolite with anti-angiogenic and anti-tumor properties, mainly acting by disrupting microtubule function via the colchicine binding site on tubulin and downregulating hypoxia-inducible factor 1-alpha (HIF-1α). Sunitinib is an FDA-approved small molecule multi-targeted receptor tyrosine kinase inhibitor that blocks signaling through several cancer-relevant pathways including VEGFR, PDGFR, KIT, FLT3, RET, and CSF-1R. The combination aimed to provide antiangiogenic and antiproliferative effects via complementary mechanisms. However, clinical studies showed limited anti-tumor activity and high toxicity, leading to early termination of trials.
- Other names
- 2ME2 NCD + sunitinib malate
02
Targets
HIF1A (Hypoxia-inducible factor 1-alpha)Microtubule
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