Drug intelligence / Profile preview

5-fluorouracil + folinic acid + levamisole

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination chemotherapy regimen consisting of three drugs: - **5-fluorouracil (5-FU):** A pyrimidine analog antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis and leading to cell death. It is primarily used as an antineoplastic agent in the treatment of various cancers. - **Folinic acid (leucovorin):** A reduced form of folic acid that enhances the binding of 5-FU to thymidylate synthase, thereby increasing its cytotoxic effect on cancer cells. Folinic acid itself does not have significant anticancer activity but acts as a biomodulator. - **Levamisole:** Originally developed as an antihelminthic agent, it has immunomodulatory properties and was historically used in combination with 5-FU for adjuvant treatment of colorectal cancer. This regimen was widely studied and used for adjuvant therapy in colorectal cancer. However, large clinical trials such as QUASAR demonstrated no survival benefit from adding levamisole or using high-dose folinic acid compared to low-dose regimens[1][6]. The use of this specific combination has largely been superseded by other regimens due to lack of additional efficacy and concerns about toxicity[4].

Other names
5FU + folinic acid + levamisolefluorouracil + leucovorin + levamisole5-fluorouracil/leucovorin/levamisole
02

Targets

TS (Thymidylate synthase)

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