polyglutamate camptothecin

Polyglutamate camptothecin is a polymer-drug conjugate consisting of the anticancer agent camptothecin covalently linked to a poly-L-glutamic acid (polyglutamate) backbone. This formulation, also known as CT-2106, was developed to address the poor solubility and high toxicity of native camptothecin by stabilizing its active lactone form and enhancing aqueous solubility. The polyglutamate carrier is designed to exploit the enhanced permeability and retention (EPR) effect in tumors, thereby increasing tumor-specific delivery and reducing systemic toxicity. Polyglutamate camptothecin acts as a prodrug that releases active unconjugated camptothecin over time. Its mechanism of action is inhibition of DNA topoisomerase I, leading to DNA damage and cancer cell death. Clinical studies showed improved tolerability compared with unconjugated camptothecin but development was discontinued after early-phase trials for advanced solid tumors[1][4][6][8].

Other names

poly-L-glutamate camptothecin20(S)-camptothecin poly-L-glutamate conjugate