Drug intelligence / Profile preview

edotecarin

Development stage
Phase 3
Lead developer
MS K.K.
Modality
Small Molecules
Administration
Intravenous
01

Overview

Edotecarin is a novel small molecule antineoplastic agent belonging to the indolocarbazole class. It acts as a non-camptothecin DNA topoisomerase I inhibitor by stabilizing the DNA-topoisomerase I complex and enhancing single-strand DNA cleavage. This results in inhibition of DNA replication and decreased tumor cell proliferation. Edotecarin is structurally related to staurosporine but lacks protein kinase inhibitory activity. It has demonstrated antitumor activity in vitro and in vivo across multiple cancer models including breast, cervix, pharynx, lung, prostate, colon, gastric and hepatic cancers. The drug was developed for use primarily as an anticancer agent; however its development has been discontinued[1][2][4][5].

Other names
12-(beta-D-glucopyranosyl)-2,10-dihydroxy-6-[2-hydroxy-1-(hydroxymethyl)ethylamino]-6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-dione
02

Targets

TOP1 (DNA Topoisomerase I)

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