Drug intelligence / Profile preview

mureletecan

Development stage
Phase 1
Lead developer
Pfizer
Modality
Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

Mureletecan is a water-soluble prodrug consisting of camptothecin covalently linked to a polymeric backbone of methacryloylglycynamide. It is designed to improve the solubility and delivery of camptothecin, an alkaloid with potent antineoplastic activity derived from Camptotheca acuminata. After administration and entry into tumor cells, the active moiety (camptothecin) is slowly released via hydrolysis of the ester linkage. Camptothecin acts by binding to and stabilizing the topoisomerase I-DNA covalent complex, thereby inhibiting religation of single-stranded DNA breaks and leading to potentially lethal double-stranded DNA breaks during DNA replication. This results in inhibition of DNA replication and induction of apoptosis in cancer cells. The prodrug formulation aims to increase drug delivery specifically to tumor sites while reducing systemic toxicity compared to free camptothecin[3][4][5][7]. Mureletecan has been investigated primarily for metastatic solid tumors.

Brand names
Vulcanchem
Other names
mureletecancamptothecin-methacryloylglycynamide conjugate
02

Targets

TOP1 (DNA Topoisomerase I)

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