10 Facts About Irinotecan

Irinotecan, sold under the brand name Camptosar among others, is a medication used to treat colon cancer, and small cell lung cancer.

Irinotecan is a topoisomerase inhibitor—it blocks the topoisomerase I enzyme, resulting in DNA damage and cell death.

Irinotecan was approved for medical use in the United States in 1996.

Irinotecan-associated diarrhea is severe and clinically significant, sometimes leading to severe dehydration requiring hospitalization or intensive care unit admission.

Irinotecan is a hydrophilic compound with a large volume of distribution .

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Irinotecan is metabolized by intrahepatic cytochrome P450 enzymes, CYP3A4 and CYP3A5 into inactive metabolites APC and NPC .

Irinotecan is transported to bile by the ATP-binding cassette transporter proteins: ABCB1, ABCC1, ABCC2, and ABCG2.

Irinotecan is converted by an enzyme into its active metabolite SN-38, which is in turn inactivated by the enzyme UGT1A1 by glucuronidation.

Irinotecan is one of the first widely used chemotherapy agents that is dosed according to the recipient's genotype.

Irinotecan received accelerated approval from the U S Food and Drug Administration in 1996, and full approval in 1998.