As the primary enzyme responsible for the activatable conversion of Irinotecan (CPT-11) to
SN-38, carboxylesterase 2 (CES2) is a significant predictive biomarker toward CPT-11 …

Carboxylesterases play a critical role in the bioactivation of the anticancer prodrug
irinotecan {7-ethyl-10-[4-(1-piperidino)-1-piperidino] carbonyloxy-camptothecin; CPT-11} …

CPT-11 is an antitumor prodrug that is hydrolyzed by carboxylesterases (CE) to yield SN-38,
a potent topoisomerase I poison. However, the dose limiting toxicity delays diarrhea that is …

The dose-limiting toxicity of the highly effective anticancer agent 7-ethyl-10-[4-(1-piperidino)-
1-piperidino] carbonyloxy-camptothecin (irinotecan; CPT-11) is delayed diarrhea. This is …

CPT-11 [7-ethyl-10-[4-(1-piperidino)-1-piperidino] carbonyloxycamptothecin or Irinotecan] is
a carbamate prodrug that is activated in vivo by carboxylesterase (CES)-2 to SN-38 (7-ethyl …

Ethyl-10-[4-(1-piperidino)-1-piperidino] carbonyloxy-camptothecin (irinotecan; CPT-11) is a
prodrug activated by carboxylesterase enzymes. We characterized the hydrolysis of CPT-11 …

Irinotecan (CPT-11) is an important anticancer agent activated by carboxylesterase (CE).
Treatment with CPT-11 may be associated with severe adverse effects, however, so …

Enzyme activation of prodrugs to improve the therapeutic index of specific anticancer agents
is an attractive alternative to current chemotherapy regimens. This study addresses the …

CPT-11 is a potent antitumor agent that is activated by carboxylesterases (CE) and
intracellular expression of CEs that can activate the drug results in increased cytotoxicity to …

Abstract Irinotecan (CPT-11) is an anticancer agent for the treatment of colon cancer. CPT-
11 can be considered as a prodrug, since it needs to be activated into the toxic drug SN-38 …