simmitecan

Simmitecan is a small molecule ester prodrug of chimmitecan, a 9-alkyl substituted camptothecin derivative with potent antineoplastic activity. Upon intravenous administration, simmitecan is hydrolyzed by carboxylesterase to produce the active metabolite chimmitecan. Chimmitecan acts as a DNA topoisomerase I inhibitor by stabilizing covalent topoisomerase I-DNA complexes and inhibiting the religation of single-strand DNA breaks. This leads to interference with DNA replication machinery and results in potentially lethal double-strand DNA breaks, ultimately inhibiting cell proliferation and inducing apoptosis. The modification at position 9 confers improved cytotoxicity compared to other camptothecin analogues. Simmitecan has demonstrated superior in vitro and in vivo antitumor activity compared to SN38 (the active metabolite of irinotecan) and topotecan against various tumor types including multidrug-resistant cells[1][2][4][5]. It has been developed primarily for solid tumors such as colorectal cancer and neuroendocrine tumors.

Other names

Simmitecan hydrochlorideL-P