Drug intelligence / Profile preview

lapatinib + FOLFOX4

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral (lapatinib), Intravenous (oxaliplatin, Fluorouracil, Folinic Acid)
01

Overview

**lapatinib + FOLFOX4** is an investigational combination regimen consisting of lapatinib, a small molecule dual tyrosine kinase inhibitor of ErbB1 (epidermal growth factor receptor, EGFR) and ErbB2 (HER2), administered in combination with the FOLFOX4 chemotherapy regimen. FOLFOX4 includes oxaliplatin (a platinum-based DNA crosslinker), folinic acid (leucovorin, which enhances 5-FU cytotoxicity), and fluorouracil (5-FU, a pyrimidine antimetabolite inhibiting thymidylate synthase). Lapatinib targets tumor cell growth and survival signaling, while FOLFOX4 exerts cytotoxic effects via DNA damage and inhibition of DNA synthesis. The primary clinical indication under investigation is advanced and metastatic gastrointestinal (especially colorectal) cancers, with the regimen evaluated for safety and tolerability in phase I studies for solid tumors[1][3][5].

Brand names
Tykerb (for lapatinib)Eloxatin (for oxaliplatin, a FOLFOX4 component)
Other names
lapatinib + FOLFOX4lapatinib plus oxaliplatin/leucovorin/fluorouracillapatinib with folinic acid, fluorouracil, oxaliplatin
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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