fluorouracil + leucovorin + rofecoxib

This is a combination regimen consisting of three drugs: - **Fluorouracil (5-FU):** A pyrimidine analog antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis and leading to cell death, primarily used as an antineoplastic agent in various cancers. - **Leucovorin (folinic acid):** A reduced form of folic acid that enhances the binding of 5-FU to thymidylate synthase, thereby increasing its cytotoxic effect. Leucovorin itself does not have significant anticancer activity but potentiates the efficacy of fluorouracil. - **Rofecoxib:** A selective cyclooxygenase-2 (COX-2) inhibitor previously used as an anti-inflammatory and analgesic agent. In oncology research, COX-2 inhibitors were investigated for their potential to enhance chemotherapy efficacy by targeting tumor-promoting inflammation. This specific combination was studied in metastatic colorectal cancer based on preclinical evidence suggesting possible additive or synergistic effects when combining 5-FU with COX-2 inhibitors like rofecoxib. However, clinical studies found that adding rofecoxib did not improve antitumor activity and led to increased gastrointestinal toxicity without additional benefit[1]. The study was terminated early due to lack of efficacy and unacceptable toxicity.

Other names

5-fluorouracil + folinic acid + rofecoxib