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gefitinib + 5-fluorouracil + leucovorin

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral (gefitinib), Intravenous (5-fluorouracil, Leucovorin)
01

Overview

Gefitinib + 5-fluorouracil + leucovorin is an investigational combination regimen comprising: - **Gefitinib**: a small molecule oral inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, used primarily to treat cancers with EGFR-activating mutations. - **5-Fluorouracil (5-FU)**: a pyrimidine antimetabolite, which interferes with thymidylate synthase, inhibiting DNA synthesis, and has broad use in gastrointestinal and other solid tumors. - **Leucovorin (folinic acid)**: a vitamin B derivative used to enhance the efficacy and reduce the toxicity of 5-fluorouracil by stabilizing its bond with thymidylate synthase. This combination, while not standard and lacking a distinct brand name or clinical approval as a three-drug set, has been studied in phase I/II clinical trials for **advanced or metastatic colorectal cancer** and **other solid tumors**. The intended mechanism is to synergistically inhibit tumor growth: gefitinib targets EGFR-mediated signaling, while 5-FU (with leucovorin) disrupts DNA synthesis in rapidly dividing tumor cells[1][3][5].

Brand names
AdrucilCaracEfudexXeloda
Other names
gefitinib + 5-FU + LV
02

Targets

TS (Thymidylate synthase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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