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Taltobulin is a fully synthetic tripeptide analog of the marine natural product hemiasterlin that functions as a potent antimicrotubule cytotoxin and experimental antineoplastic agent. It binds tubulin and inhibits tubulin polymerization, disrupting microtubule organization, inducing mitotic arrest, and triggering apoptosis in tumor cells, while demonstrating reduced susceptibility to P-glycoprotein–mediated efflux compared with taxanes and vinca alkaloids.[3][5][6][11][12] Initially developed by Pfizer, taltobulin has been evaluated preclinically and in early clinical studies for solid tumors and is also used as a cytotoxic payload component in antibody-drug conjugate research.[1][6][8][9][12][13]
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