Drug intelligence / Profile preview

lurtotecan

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Intravenous
01

Overview

Lurtotecan is a synthetic analog of camptothecin and functions as an inhibitor of DNA topoisomerase I. By stabilizing the complex between topoisomerase I and DNA during replication, it prevents religation of single-strand breaks, leading to double-stranded DNA damage and apoptosis in rapidly dividing cells. Lurtotecan was developed primarily for the treatment of various solid tumors, including ovarian cancer and small cell lung cancer. It has been investigated in both intravenous and liposomal formulations. The drug was originally developed by NeoRx (later acquired by Progenics Pharmaceuticals), but clinical development was discontinued due to limited efficacy and toxicity concerns.

Other names
lurtotecan dihydrochlorideOSI-211OSI211OSI 211
02

Targets

TOP1 (DNA Topoisomerase I)

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