Belotecan is an inhibitor of DNA topoisomerase I (IC50 = 0.119 ?g/ml) and a derivative of the DNA topoisomerase I inhibitor camptothecin .1 It inhibits the proliferation of various cancer cell lines, including KATO III stomach, HT-29 colon, A549 lung, MDA-MB-231 breast, and SKOV3 ovarian cancer cells (IC50s = 160, 10.9, 9, 345, and 31 ng/ml, respectively). Belotecan (150 ng/ml) induces apoptosis and cell cycle arrest at the G2/M phase in, and inhibits invasion of, SiHa cervical cancer cells.2 It reduces tumor growth in a Ca Ski cervical cancer mouse xenograft model when administered at a dose of 25 mg/kg. Belotecan (80 ?g/kg) reduces food intake and body weight in pregnant dams and increases fetal deaths and decreases litter size.3 Formulations containing belotecan have been used in the treatment of ovarian and small cell lung cancer.
1.Lee, J.H., Lee, J.M., Kim, J.K., et al.Antitumor activity of 7-[2-(N-isopropylamino)ethyl]-(20S)-camptothecin, CKD602, as a potent DNA topoisomerase I inhibitorArch. Pharm. Res.21(5)581-590(1998) 2.Lee, S., Ho, J.Y., Liu, J.J., et al.CKD-602, a topoisomerase I inhibitor, induces apoptosis and cell-cycle arrest and inhibits invasion in cervical cancerMol. Med.25(1)23(2019) 3.Chung, M.-K., Kim, J.-C., and Han, S.-S.Embryotoxic effects of CKD-602, a new camptothecin anticancer agent, in ratsReprod. Toxicol.20(1)165-173(2005)