Stepwise optimization of tumor-targeted dual-action platinum(iv)-gemcitabine prodrugs.

ABSTRACT: While platinum-based chemotherapeutic agents have established themselves as indispensable components of anticancer therapy, they are accompanied by a variety of side effects and the rapid occurrence of drug resistance. A promising strategy to address these challenges is the use of platinum(iv) prodrugs, which remain inert until they reach the tumor tissue, thereby mitigating detrimental effects on healthy cells. Typically, platinum drugs are part of combination therapy settings. Consequently, a very elegant strategy is the development of platinum(iv) prodrugs bearing a second, clinically relevant therapeutic in axial position. In the present study, we focused on gemcitabine as an approved antimetabolite, which is highly synergistic with platinum drugs. In addition, to increase plasma half-

SUBMITTER: Kastner A 

PROVIDER: S-EPMC10790623 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature