CPT-11

CPT-11

An antineoplastic chemotherapeutic agent.

irinotecan

A topoisomerase-1 inhibitor and semisynthetic analogue of the natural alkaloid camptothecin, which is activated by hydrolysis in vivo to an active metabolit, SN-38, and inactivated by glucuronidation with uridine diphosphate glucoronosyltransferase 1A1 (UGT1A1). It was FDA-approved for managing colorectal carcinoma in 1994. 

Adverse effects
Severe diarrhoea, possibly leading to dehydration, requiring aggressive antidiarrhoeal management with loperamide or Lomotil; immunosuppression with severe neutropaenia; functional overdose in patients who under-express UGT1A1 and cannot clear irinotecan as quickly (e.g., those with Gilbert syndrome as normal patients).
References in periodicals archive ?
Irinotecan (camptothecin-11 (CPT-11)) is a topoisomerase I inhibitor that has been used in the treatment of a wide spectrum of cancer, particularly colorectal cancer.
A phase II study of CPT-11, a new derivative of camptothecin, for previously untreated non-small-cell lung cancer.
Two clinically used CPT derivatives irinotecan (CPT-11) and topotecan are widely used to inhibit the growth of lung cancer in combination with cisplatin, paclitaxel [9], and bevacizumab [10].
Initially, the collaboration will concentrate on the development of next-generation product candidate to TheraBiologics' TBX02, which uses an established NSC line engineered to express a modified carboxylesterase enzyme that converts the prodrug, CPT-11 (Irinotecan), to the potent chemotherapy agent, SN-38, which is 1000x more toxic to cancer cells than CPT-11.
Establishment of a camptothecin analog (Cpt-11)-resistant cell-line of human non-small cell lung-cancer--characterization and mechanism of resistance.
Including acetaminophen and the chemotherapy medication CPT-11. The authors propose that the same mechanisms may be at work with environmental chemicals.
Pharmacology of topoisomerase I inhibitors irinotecan (CPT-11) and topotecan.
A retrospective study of bifractionated CPT-11 with LF5FU infusion (FOLFIRI-3) in colorectal cancer patients pretreated with oxaliplatin and CPT-11 containing chemotherapies
Colorectal cancer patients were treated with oxaliplatin plus 5-fluorouracil (5-FU), or weekly CPT-11 or 5-FU and folates (FA).