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pegirinotecan
- Development stage
- Unknown
- Lead developer
- JenKem Technology
- Modality
- Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous
01
Overview
Pegirinotecan (JK-1201G) is a long-acting, 4-arm polyethylene glycol (PEG) conjugate of irinotecan developed by Tianjin Jiankai Technology (JenKem Technology). As a prodrug, it is designed to release irinotecan, which is subsequently converted into its active metabolite, SN-38. SN-38 acts as a potent inhibitor of topoisomerase I, leading to DNA double-strand breaks and apoptosis in rapidly dividing cancer cells. The PEGylation strategy is intended to improve the solubility and pharmacokinetic profile of irinotecan, extending its half-life and enhancing its accumulation in tumor tissues via the enhanced permeability and retention (EPR) effect. It is primarily being investigated for the treatment of high-grade gliomas, including glioblastoma multiforme, where it aims to overcome the limitations of conventional irinotecan therapy, such as rapid clearance and poor tumor penetration.
- Other names
- PEG-irinotecan4-arm PEG-irinotecan
02
Targets
TOP1 (DNA Topoisomerase I)
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