ENMD-1198

ENMD-1198 is an orally active small molecule antimitotic agent developed as an analogue of 2-methoxyestradiol (2ME2) with modifications to improve metabolic stability while retaining and enhancing its multiple mechanisms of action. It acts primarily by disrupting microtubules through binding to the colchicine-binding site of β-tubulin, leading to cell cycle arrest and apoptosis in tumor cells. Additionally, ENMD-1198 inhibits hypoxia-inducible factor 1-alpha (HIF-1α) and signal transducer and activator of transcription 3 (STAT3), contributing to its antiangiogenic and antiproliferative effects. Preclinical studies have demonstrated potent antitumor activity across various cancer models, including leukemia, multiple myeloma, hormone-refractory prostate cancer, breast cancer, and hepatocellular carcinoma. The drug has advanced into phase I clinical trials for advanced cancers but development appears discontinued[1][5][6][7].

Other names

2-methoxyestra-1,3,5(10),16-tetraene-3-carboxamide