Belotecan hydrochloride (CKD-602)

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)