Drug intelligence / Profile preview

gefitinib + tegafur + uracil

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Gefitinib + tegafur + uracil is a combination therapy used primarily in the treatment of advanced non-small cell lung cancer (NSCLC), particularly in patients with activating EGFR mutations. Gefitinib is an oral small molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, blocking downstream signaling pathways that promote tumor cell proliferation and survival. Tegafur is a prodrug of 5-fluorouracil (5-FU), which acts as an antimetabolite inhibiting thymidylate synthase and thus DNA synthesis; uracil inhibits dihydropyrimidine dehydrogenase to increase 5-FU bioavailability. The addition of oral UFT to gefitinib has been shown to improve progression-free survival compared to gefitinib alone in patients with EGFR-mutant NSCLC[1][2][4]. This regimen leverages both targeted therapy and metronomic chemotherapy for enhanced anti-tumor efficacy.

Other names
gefitinib + UFTgefitinib plus tegafur/uracil
02

Targets

TS (Thymidylate synthase)DPYD (Dihydropyrimidine dehydrogenase)EGFR (Epidermal growth factor receptor)

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