Cancer chemotherapy: a SN-38 (7-ethyl-10-hydroxycamptothecin) glucuronide prodrug for treatment by a PMT (Prodrug MonoTherapy) strategy.
A glucuronide-based prodrug of SN-38 (7-ethyl-10-hydroxycamptothecin) has been synthesized for use in a Prodrug MonoTherapy Strategy (PMT). Since this prodrug is significantly less cytotoxic than SN-38 itself and efficiently releases the drug in vitro in the presence of beta-D-glucuronidase, it can be considered as an appropriate candidate for cancer treatment by a PMT strategy.
Angenault
Stéphane
S
UMR176 CNRS/Institut Curie, 26, rue d'Ulm, 75248 Paris Cedex 05, France.
Thirot
Sylvie
S
Schmidt
Frédéric
F
Monneret
Claude
C
Pfeiffer
Bruno
B
Renard
Pierre
P
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology*; D005966:Glucuronidase / Q000378:metabolism; D020719:Glucuronides / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D019073:HT29 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D000077146:Irinotecan; D011355:Prodrugs / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*
D000970:Antineoplastic Agents; D020719:Glucuronides; D011355:Prodrugs; D000077146:Irinotecan; D005966:Glucuronidase; D002166:Camptothecin