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G3.5-Gly-SN38
- Development stage
- Preclinical
- Modality
- Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Oral
01
Overview
G3.5-Gly-SN38 is a research-stage polymeric drug delivery system consisting of a generation 3.5 carboxyl-terminated poly(amidoamine) (PAMAM) dendrimer covalently conjugated to SN38, the active metabolite of irinotecan, via a glycine spacer. SN38 is a potent topoisomerase I inhibitor, but its clinical utility is limited by poor water solubility and systemic toxicity. This dendrimer-based conjugate is designed to improve the bioavailability and efficacy of SN38 while minimizing gastrointestinal toxicity. In preclinical studies, G3.5-Gly-SN38 demonstrated significant antiproliferative activity against human colorectal cancer cell lines (HCT-116 and HT-29), induced G2/M phase cell cycle arrest, and showed potential for oral delivery to treat hepatic colorectal cancer metastases. The compound is primarily an academic research tool and is not currently part of a commercial development program.
- Other names
- G3.5 PAMAM dendrimer-glycine-SN38 conjugateG-3.5 PAMAM dendrimer-glycine-SN38 conjugateG 3.5 PAMAM dendrimer-glycine-SN38 conjugate
02
Targets
TOP1 (DNA Topoisomerase I)
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