Lurtotecan (OSI221; NX211) is a semi-synthetic camptothecin derivative with anticancer activity. Liposomal lurtotecan (a liposome-encapsulated formulation of lurtotecan) was in clinical trials as a treatment for topotecan-resistant ovarian cancer, but was discontinued. It selectively stabilizes the topoisomerase I-DNA covalent complex and forms an enzyme-drug-DNA ternary complex during S phase of the cell cycle, thereby inhibiting religation of topoisomerase I-mediated single-stranded DNA breaks. This ultimately results in an inhibition of DNA replication, inducing double-stranded DNA breakages, obstruction of RNA and protein synthesis and triggering apoptosis. Furthermore, this agent also stimulates degradation of topoisomerase I, likely mediated through ubiquitin-proteasomal pathway. Liposomal delivery of lurtotecan improves its penetration and delivery into tumors while lowering systemic side effects.

纯度：≥98%

CAS：149882-10-0