Drug intelligence / Profile preview

erlotinib + tegafur + gimeracil + oteracil

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

Overview

This is a combination of four small molecule drugs: erlotinib, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, and the fixed-dose oral fluoropyrimidine formulation tegafur/gimeracil/oteracil. Erlotinib inhibits EGFR signaling by reversibly binding to its ATP-binding site, blocking downstream pathways involved in cell proliferation and survival. Tegafur is a prodrug of 5-fluorouracil (5-FU), which inhibits thymidylate synthase, disrupting DNA synthesis in rapidly dividing cells. Gimeracil inhibits dihydropyrimidine dehydrogenase (DPD), increasing 5-FU bioavailability by preventing its breakdown. Oteracil reduces gastrointestinal toxicity by inhibiting phosphorylation of 5-FU in the gut[1][2][3][4][5]. This multi-agent regimen would be expected to provide dual antitumor activity through both targeted inhibition of EGFR signaling and cytotoxic effects on DNA synthesis.

02

Targets

DPYD (Dihydropyrimidine dehydrogenase)TS (Thymidylate synthase)OPRT (Orotidine 5'-phosphate decarboxylase)EGFR (Epidermal growth factor receptor)

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