Many cancer type-specific anticancer agents have been developed and significant
advances have been made toward precision medicine in cancer treatment. However …

Covalent modification of therapeutic compounds is a clinically proven strategy to devise
prodrugs with enhanced treatment efficacies. This prodrug strategy relies on the modified …

Background The combination of fluorouracil and leucovorin has until recently been standard
therapy for metastatic colorectal cancer. Irinotecan prolongs survival in patients with …

CPT-11 belongs to the class of topoisomerase I inhibitors, and it acts as a prodrug of SN-38,
which is approximately 100–1000-fold more cytotoxic than the parent drug. CPT-11 has …

Purpose Severe toxicity is commonly observed in cancer patients receiving irinotecan. UDP-
glucuronosyltransferase 1A1 (UGT1A1) catalyzes the glucuronidation of the active …

The size of anticancer agent‐incorporating micelles can be controlled within the diameter
range of 20–100 nm to ensure that they do not penetrate normal vessel walls. With this …

The camptothecins are a maturing class of anticancer agents. In this article, we review the
pharmacology and antitumor activity of the camptothecin analogues that are approved for …

Supported by detailed understanding of their mechanism of action, and facilitated by
chemical manipulations that have amplified their solubility, the camptothecins have …

Camptothecin analogues and derivatives appear to exert their antitumour activity by binding
to topoisomerase I and have shown significant activity against a broad range of tumours. In …

The prodrug irinotecan is an active agent for the treatment of advanced colorectal cancer
and a number of other solid tumors. Irinotecan is converted in vivo to SN-38 (7-ethyl-10 …