Irinotecan Hcl Trihydrate(Campto) /

生物活性

Irinotecan hydrochloride trihydrate is a hydrochloride trihydrate of irinotecan (Camptosar, Campto, CPT-11) which is a topoisomerase I inhibitor with IC50 of 15.8 and 5.17 μM for LoVo cells and HT-29 cells, respectively. As a Topo I inhibitor, Irinotecan (Camptosar, Campto, CPT-11) inhibits the religation step of the enzyme’s normal action, inducing single stranded DNA breaks. These single stranded breaks are then converted to double-stranded breaks within the course of DNA replication which is reported to induce apoptosis or repair mechanisms as a result. Irinotecan is activated by esterases to produce the activated metabolite and has been reported to be associated with cleavage of poly (ADP-ribose) polymerase (PARP) in colon carcinoma cells. Irinotecan’s active metabolite is additionally noted to activate p53 in the Huh7 cell line.

参考文献

[1] http://en.wikipedia.org/wiki/Irinotecan

[2] Pavillard V et al. Cancer Chemother Pharmacol. 2002 Apr;49(4):329-35.