silatecan

Silatecan is a synthetic, highly lipophilic third-generation camptothecin analog with potential antineoplastic and radiosensitizing activities. It acts as a DNA topoisomerase I inhibitor by binding to and stabilizing the topoisomerase I-DNA covalent complex, thereby inhibiting religation of single-stranded DNA breaks. This leads to lethal double-stranded DNA breaks during replication, resulting in inhibition of DNA replication and induction of apoptosis. The tert-butyldimethylsilyl modification increases its lipophilicity and blood stability compared to earlier camptothecins, enhancing the stability of its active lactone form and prolonging activity in vivo. Silatecan has been investigated primarily for glioblastoma multiforme (GBM), gliosarcoma, solid malignancies, and other tumors[1][2][3][4][5].

Brand names

silatecan

Other names

silatecan7-tert-butyldimethylsilyl-10-hydroxycamptothecin(20S)-7-t-butyldimethylsilyl-10-hydroxycamptothecin