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LE-SN38
- Development stage
- Phase 2
- Lead developer
- Neopharm
- Modality
- Small Molecules, Liposomes → Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous
01
Overview
LE-SN38 is a liposome-encapsulated formulation of SN-38, the active metabolite of irinotecan. It was developed to overcome the poor solubility and delivery limitations of free SN-38, enabling intravenous administration and improved pharmacokinetics. As a topoisomerase I inhibitor, LE-SN38 interferes with DNA replication in cancer cells by stabilizing the DNA-topoisomerase I complex, leading to DNA damage and cell death. Preclinical studies demonstrated antitumor efficacy in murine leukemia and human pancreatic tumor models, while clinical trials evaluated its use primarily in metastatic colorectal cancer after progression on standard therapies[4][5][6]. The formulation aimed to improve therapeutic index compared to irinotecan by reducing toxicities such as diarrhea and myelosuppression[6][8].
- Other names
- Liposome encapsulated SN38SN-38 liposomalSN38 liposomalSN 38 liposomal
02
Targets
TOP1 (DNA Topoisomerase I)
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