Irinotecan

Description	Its action is terminated by glucuronidation by UDP glucuronosyl transferase. As a Topo I inhibitor, Irinotecan 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. Irinotecan is active against colorectal cancer in patients whose disease is refractory to fluorouracil.
Pathways	Cell Cycle/DNA Damage
Targets	Topoisomerase

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