Irinotecan

Irinotecan is a topoisomerase inhibitor used for chemotherapy. It is a water-soluble analogue of [camptothecin], that is extracted from the Chinese tree Camptotheca acuminate. The bis-piperidine side chain in the structure of irinotecan bestows enhanced water solubility. As an anticancer drug, irinotecan was first commercially available in Japan in 1994 to treat various cancers including lung, cervical and ovarian cancer. Approved by the FDA in 1996, irinotecan is used to treat colorectal cancer and pancreatic adenocarcinoma. Irinotecan liposome was approved by the FDA in February 2024. The active metabolite SN-38 is also a potent inhibitor of DNA topoisomerase I. Both irinotecan and SN-38 mediate antitumor activity by forming a complex with topoisomerase I and blocking its enzymatic activity, thereby interfering with DNA synthesis. This leads to the arrest of the cell cycle in the S-G2 phase and cancer cell death. It is grouped under the following drug class(es): Cytotoxics and Topoisomerase inhibitors. Its therapeutic use is listed as anti-cancer agents. The directory classifies it as a commercial API with a semi-synthetic source/manufacturing origin. Other names for this substance include camptothecin-11, Biotecan and Irinotecanum. Its PubChem CID is 60838.