Drug intelligence / Profile preview

5-fluorouracil + folinic acid + rhGM-CSF

Development stage
Unknown
Modality
Cytokines & Interferons → Recombinant Proteins and Enzymes, Small Molecules
Administration
Intravenous, Subcutaneous
01

Overview

This is a combination regimen consisting of three agents: - **5-fluorouracil (5-FU)**, a pyrimidine analog antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis and leading to cell death in rapidly dividing cells. - **Folinic acid (leucovorin)**, a reduced form of folic acid that enhances the binding of 5-FU to thymidylate synthase, thereby increasing its cytotoxic effect. Folinic acid itself is not cytotoxic but potentiates the action of fluorouracil[9][7][1]. - **Recombinant human granulocyte-macrophage colony-stimulating factor (rhGM-CSF)**, a cytokine that stimulates proliferation and differentiation of hematopoietic progenitor cells into granulocytes and macrophages. In this regimen, it is used to support bone marrow recovery after chemotherapy-induced myelosuppression[1]. The combination has been investigated primarily for use in advanced or metastatic colorectal cancer and other gastrointestinal malignancies. The addition of rhGM-CSF aims to allow higher dosing or improved tolerance by stimulating white blood cell recovery; however, studies have shown dose-limiting toxicities such as mucositis may still occur[1].

Other names
5-FU + leucovorin + recombinant human granulocyte-macrophage colony-stimulating factor5-fluorouracil + leucovorin + rhGM-CSF5-fluorouracil + folinic acid + recombinant human GM-CSF
02

Targets

CSF2R (Granulocyte-macrophage colony-stimulating factor receptor)TS (Thymidylate synthase)

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