Drug intelligence / Profile preview

capecitabine + lapatinib + oxaliplatin

Development stage
Unknown
Lead developer
GSK
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent 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
XELOXTykerb
Other names
capecitabine, lapatinib, oxaliplatinCapeOx plus lapatinib
02

Targets

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

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