Drug intelligence / Profile preview

erlotinib + mFOLFOX6

Development stage
Phase 2
Lead developer
Astellas Pharma
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Erlotinib + mFOLFOX6 is a combination regimen used in oncology clinical trials, primarily for the treatment of advanced or metastatic gastrointestinal cancers such as esophageal/gastroesophageal junction (Eso/GEJ) adenocarcinoma and metastatic colorectal cancer. Erlotinib is an oral small molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, which blocks EGFR signaling pathways involved in tumor cell proliferation and survival. mFOLFOX6 is a modified version of the FOLFOX chemotherapy regimen, consisting of oxaliplatin (a platinum-based DNA crosslinker), leucovorin (folinic acid, which enhances 5-fluorouracil activity), and 5-fluorouracil (an antimetabolite that inhibits thymidylate synthase). The combination aims to leverage both targeted therapy against EGFR and cytotoxic chemotherapy to improve response rates in patients with certain gastrointestinal malignancies[1][2][7].

02

Targets

TS (Thymidylate synthase)Pt-DNA adduct (DNA-oxaliplatin adduct)EGFR (Epidermal growth factor receptor)

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