Drug intelligence / Profile preview

FOLFIRI + erlotinib

Development stage
Phase 1
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

FOLFIRI + erlotinib is a combination regimen consisting of the chemotherapy protocol FOLFIRI (folinic acid [leucovorin], fluorouracil [5-FU], and irinotecan) administered together with erlotinib, an oral epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. FOLFIRI targets rapidly dividing cancer cells through inhibition of DNA synthesis and topoisomerase I activity, while erlotinib blocks EGFR signaling pathways involved in tumor cell proliferation and survival. This combination has been investigated primarily for the treatment of metastatic colorectal cancer, particularly as a second-line therapy after progression on first-line regimens. Clinical studies have shown that this combination can result in excessive toxicity, including high rates of severe neutropenia and gastrointestinal side effects, which has limited its feasibility for routine use[1][2][3]. The rationale for combining these agents is based on preclinical data suggesting potential synergistic effects when chemotherapy is sequenced with EGFR inhibition; however, clinical trials have demonstrated significant safety concerns.

Other names
FOLFIRI + erlotinib
02

Targets

TS (Thymidylate synthase)TOP1 (DNA Topoisomerase I)EGFR (Epidermal growth factor receptor)

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