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BNZ-111 is a benzimidazole derivative and small molecule tubulin inhibitor developed as an oral anti-cancer drug. It demonstrates strong cytotoxic activity against both chemo-sensitive and chemo-resistant ovarian cancer cells, including those resistant to paclitaxel, by inducing apoptosis and causing G2/M cell cycle arrest. Preclinical studies indicate BNZ-111 is not a substrate for P-glycoprotein (P-gp) and exerts its effects by binding specifically to the β subunit of curved tubulin, thereby modulating β-3 tubulin expression and disrupting microtubule dynamics. BNZ-111 has shown significant in vivo tumor growth inhibition in platinum- and paclitaxel-resistant ovarian cancer models, with good oral exposure, bioavailability, and minimal general toxicity.
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