Drug intelligence / Profile preview

CPBSN38L

Development stage
Preclinical
Modality
Small Molecules, Liposomes → Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

CPBSN38L is an **ultrasound-activated prodrug-loaded liposomal nanoparticle** developed for cancer therapy, designed to enable tumor-selective activation and release of the cytotoxic agent SN38 (the active metabolite of irinotecan). The formulation incorporates two main components: a sonosensitizer (chlorin e6, Ce6) integrated into the lipid bilayer, and a redox-responsive prodrug, PBSN38 (pinacol boronic ester conjugated 7-ethyl-10-hydroxycamptothecin), encapsulated inside the liposome. Upon intravenous administration, CPBSN38L accumulates in tumors, where exposure to ultrasound (US) irradiation activates Ce6 to generate reactive oxygen species (ROS). The ROS, in turn, trigger cleavage of the prodrug and controlled release of SN38 within the tumor microenvironment, allowing for spatial and temporal control of cytotoxicity and minimizing systemic toxicity. Preclinical studies demonstrated potent anti-tumor efficacy in murine models of colon adenocarcinoma and hepatocellular carcinoma, with significant tumor growth inhibition after US exposure and improved safety compared to conventional camptothecin analogues[1][3].

02

Targets

TOP1 (DNA Topoisomerase I)

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