Edotecarin is a potent topoisomerase I inhibitor. It can decrease single-strand DNA cleavage (IC50: 50 nM).

Topo I:50 nM, PKC:160 μM

Edotecarin (0.6 μmol/L) increases the formation of DNA-protein complexes in a time-dependent manner, in the presence of human colon cancer cells labeled with 3Hthymidine [1].

Edotecarin causes tumor growth delays ranging from 10.45 days at the lowest dose (3 mg/kg) to 24.83 days at the highest (100 mg/kg). Edotecarin produces an 83% increase in survival in mice bearing intracranial D-456MG glioma and shows a strong antimetastatic effect [1]. Combination treatment of edotecarin plus irinotecan improves the antitumor activity in vivo compared with either agent alone [2].