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SB-T-1213 is a third-generation, semisynthetic taxane (taxoid) designed to overcome multidrug resistance in cancer therapy. It is structurally modified at the C10 and C3' positions to dramatically increase potency—up to 400-fold more active than paclitaxel—against both P-glycoprotein (P-gp) positive (drug-resistant) and negative cancer cells[1][3]. SB-T-1213 binds to β-tubulin on microtubules, inducing rapid and robust microtubule polymerization and stabilizing microtubules, which leads to mitotic arrest at the G2/M phase, apoptosis, and anti-proliferative effects[1][3][5]. Distinct from paclitaxel, SB-T-1213 not only enhances polymerization but also induces morphological changes in microtubules, suggesting a unique interaction contributing to its enhanced cytotoxicity[1]. It also demonstrates the ability to inhibit the P-gp efflux pump, a major mediator of multidrug resistance, and is orally available[3]. SB-T-1213 is in preclinical and early phase clinical development for treatment of various cancers, particularly tumors resistant to conventional taxanes[1][3]. Conjugation of SB-T-1213 to fatty acids (e.g., DHA-SB-T-1213) further improves antitumor activity in resistant tumor xenograft models[8][9].
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