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polyglutamate camptothecin

A therapeutic formulation consisting of camptothecin, an alkaloid isolated from the Chinese tree Camptotheca acuminata, conjugated with polyglutamate. During the S phase of the cell cycle, camptothecin selectively stabilizes topoisomerase I-DNA covalent complexes, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery. Conjugation with polyglutamate renders this agent more water soluble and less toxic than the parent molecule.

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Abbreviation:	PG-CPT
Code name:	CT-2106

polyglutamate camptothecin

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