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 ?
TBX02 utilizes 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.
Activity of CPT-11 (irinotecan hydrochloride), a topoisomerase I inhibitor, against human tumor colony-forming units.
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).
CPT-11 has shown anticancer activity against a variety of solid tumors in clinical trials, including colorectal cancer, gynecologic cancers, non-small cell and small cell lung cancers, and refractory cervical cancer (5-11).
In 1994 AIDS Treatment News reported on a class of drugs being developed for cancer, but not for HIV, though some experts believed they should be tested as antiretrovirals (see Topotecan, CPT-11 (Irinotecan), Camptothecin, and Other Topoisomerase I Inhibitors, AIDS Treatment News #197, April 15, 1994).
The roles of Taxol-like drugs, CPT-11, gemcitabine, and vinorelbine are still being sorted out in clinical trials, Dr.
One example is the use of an enzyme attached to the fusion protein to activate the cancer drug, camptothecin, or CPT-11 (Camptosar), which is being sold by Pharmacia & Upjohn (Branchburg, NJ) as a therapeutic for colorectal cancers, at the tumor sites.
Such a study has been performed by the UK Fluorouracil, Oxaliplatin and CPT-11 (irinotecan), Use and Sequencing (FOCUS) II investigators for a fluoropyrimidine [+ or -] oxaliplatin and demonstrated a limited advantage of oxaliplatin-based combination therapy in elderly patients [19].
The cells produced an enzyme that activated the chemotherapy drug CPT-11 (irinotecan) at the site of the tumors.
These properties allow EZN-2208 to outperform CPT-11 in a variety of animal models of human cancers, including tumors that develop resistance to CPT-11.