CGC-11047 + 5-fluorouracil + leucovorin

CGC-11047 + 5-fluorouracil + leucovorin is a combination regimen under investigation for cancer therapy. **CGC-11047** is a second-generation polyamine analog designed to inhibit cell proliferation and induce apoptosis in tumor cells by displacing endogenous polyamines from DNA binding sites, interfering with cell cycle processes, depleting natural polyamines, and disrupting gene and ligand-receptor activities involved in cell growth[1][2][4]. It has shown antitumor activity in preclinical models of lung and prostate cancer[8], as well as non-Hodgkin’s lymphoma[5]. **5-fluorouracil** is an antimetabolite chemotherapeutic agent that inhibits thymidylate synthase, thereby blocking DNA synthesis. **Leucovorin**, also known as folinic acid or Citrovorum factor, is used to enhance the efficacy of fluoropyrimidine drugs like 5-fluorouracil by stabilizing the binding of the drug to its target enzyme or as a rescue agent for normal cells after high-dose methotrexate therapy[7]. The combination aims to maximize antitumor effects through complementary mechanisms: direct cytotoxicity from 5-fluorouracil enhanced by leucovorin’s modulation of nucleotide metabolism, together with disruption of tumor cell proliferation pathways via CGC‑11047.

Other names

polyamine analogue PG11047N1,N12-bis(ethyl)-cis-6,7-dehydrospermine tetrahydrochloride (for CGC-11047)folinic acid (for leucovorin)Citrovorum factor (for leucovorin)5-formyl-tetrahydrofolic acid (for leucovorin)