elomotecan

Elomotecan (BN80927) is a synthetic small molecule belonging to the homocamptothecin family of camptothecin analogs. It functions as a dual inhibitor of topoisomerase I and topoisomerase II, with potent antiproliferative activity against a broad range of human tumor cell lines in vitro and demonstrated efficacy in vivo in xenograft models. Elomotecan stabilizes the DNA-topoisomerase I complex (poisoning activity), leading to DNA damage and cell death, while also catalytically inhibiting topoisomerase II-mediated DNA relaxation without cleavable-complex stabilization. Notably, it retains activity against some tumor cells resistant to other topoisomerase I inhibitors such as SN38, suggesting additional mechanisms beyond Topo I inhibition. Elomotecan was developed for intravenous administration in patients with advanced solid tumors and has undergone phase I clinical trials[1][2][3][4][5][7].

Other names

elomotecan hydrochloride