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Drug intelligence / Profile preview
capecitabine + lapatinib + oxaliplatin
- Development stage
- Phase 3
- Lead developer
- GSK
- 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, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
Overview
This is a combination regimen consisting of three drugs: - **Capecitabine** is an oral prodrug of 5-fluorouracil (5-FU), a pyrimidine analog that inhibits DNA synthesis by interfering with thymidylate synthase, leading to cell death in rapidly dividing cancer cells. - **Lapatinib** is an oral small molecule tyrosine kinase inhibitor targeting both epidermal growth factor receptor (EGFR/HER1/ERBB1) and human epidermal growth factor receptor 2 (HER2/ERBB2). It blocks the intracellular phosphorylation of these receptors, inhibiting downstream signaling pathways involved in tumor cell proliferation and survival. - **Oxaliplatin** is a platinum-based chemotherapeutic agent that forms DNA crosslinks, inhibiting DNA replication and transcription. The combination has been studied primarily for HER2-positive advanced or metastatic gastroesophageal adenocarcinoma and metastatic colorectal cancer. Clinical trials have shown increased response rates but not significant improvement in overall survival compared to standard regimens. The regimen may be associated with increased toxicity, particularly diarrhea[1][6][8].
- Brand names
- XELOX
- Other names
- capecitabine, lapatinib, oxaliplatinCapeOx plus lapatinib
02
Targets
EGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)TS (Thymidylate synthase)Pt-DNA adduct (DNA-oxaliplatin adduct)
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