Elomotecan (BN 80927 free base) is a potent inhibitor of topoisomerases I and II. Elomotecan is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan is able to inhibit different types of tumors with better efficacy.

METHODS: Elomotecan (BN 80927 free base) (1, 10, 50, 100 μM, 72 hours) was used to treat human tumor cell lines (HT29, SKOV-3, DU145 and MCF7), and the IC50 values ​​of the cells were detected by WAT method.
RESULTS The IC50 values ​​of Elomotecan against human tumor cancer cells (HT29, SKOV-3, DU145 and MCF7) were (0.0066, 0.013, 0.003, 0.048 μM) respectively. [2]

METHODS: Elomotecan (BN 80927 free base) was administered as a 30-minute intravenous infusion at doses ranging from 1.5 to 75 mg every 3 weeks, and plasma concentration data and adverse effects were modeled using a population approach.
RESULTS Elomotecan showed linear pharmacokinetics, and clearance decreased with age; the model predicted that CL was 47% and 61% lower in 60-year-old and 80-year-old patients, respectively, compared with younger patients (30 years old); neutropenia represented a dose-limiting toxicity, with the maximum tolerated dose and recommended dose (RD) of 75 and 60 mg, respectively; elomotecan caused severe neutropenia, fatigue, nausea, and vomiting in 20%, 5%, 2%, and 2% of patients at the RD, respectively. [1]