floxuridine + irinotecan

Floxuridine + irinotecan is a combination of two chemotherapeutic agents used primarily in oncology research and clinical trials. Floxuridine is an antimetabolite that acts as a pyrimidine analog, disrupting DNA synthesis by being metabolized to fluorouracil and inhibiting thymidylate synthase. Irinotecan is a topoisomerase I inhibitor that prevents DNA unwinding necessary for replication and transcription. The combination has shown synergistic cytotoxicity in preclinical models when administered at specific ratios—most notably a 1:1 molar ratio—leading to enhanced antitumor efficacy compared to either agent alone. Liposomal formulations such as CPX-1 or LY01616 have been developed to maintain this synergistic ratio in vivo, improving pharmacokinetics and reducing toxicity. This combination is under investigation for advanced solid tumors including colorectal cancer[1][2][3][4].

Brand names

LY01616 (for the liposomal formulation)

Other names

Irinotecan/floxuridine liposomalCPX-1 (for the 1:1 molar ratio liposomal formulation)