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epofolate
- Development stage
- Discontinued
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
Epofolate is a folate receptor-targeting antimitotic agent developed as a conjugate of folic acid and the epothilone analog BMS-748285. It was designed to selectively target cancer cells that overexpress the folate receptor, facilitating targeted drug delivery. Once bound to the folate receptor, epofolate is internalized by cancer cells via receptor-mediated endocytosis. Inside the cell, it disrupts microtubule dynamics by stabilizing tubulin polymers, leading to cell cycle arrest and apoptosis—mechanisms characteristic of the epothilone class of microtubule-stabilizing agents. Epofolate underwent Phase I/IIa clinical trials for advanced solid tumors but did not demonstrate significant antitumor activity; its development has since been discontinued[2][3][4][5].
- Other names
- epofolateQ3XAW4B1DPQ-3XAW4B1DPQ 3XAW4B1DPUNII-Q3XAW4B1DPUNII-Q-3XAW4B1DPUNII-Q 3XAW4B1DP
02
Targets
TUBB (Tubulin (alpha and beta subunits))FOLR1 (FRα)
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