Drug intelligence / Profile preview

delimotecan

Development stage
Unknown
Lead developer
Menarini
Modality
Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

Delimotecan is a polymer-based prodrug of the camptothecin analog T-2513, chemically described as T-2513 bound to carboxymethyl dextran via a triglycine linker[1][4]. It is designed to selectively deliver cytotoxic camptothecin-derived metabolites to tumors. Once internalized, delimotecan is metabolized to release active compounds (T-2513, SN-38, and T-0055), which inhibit DNA topoisomerase I, causing DNA damage and apoptosis in tumor cells[1][4]. Preclinical and early clinical data show activity in solid tumors, particularly metastatic melanoma, where its efficacy is attributed to selective tumor accumulation, phagocytosis by tumor cells, and local enzymatic conversion to active cytotoxic agents[1][2][4].

Other names
delimotecan
02

Targets

TOP1 (DNA Topoisomerase I)

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