Drug intelligence / Profile preview

Capecitabine + lapatinib

Development stage
Unknown
Lead developer
GSK
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Capecitabine + lapatinib is a combination therapy used primarily for the treatment of advanced or metastatic HER2-positive breast cancer, particularly in patients who have previously received treatments such as anthracyclines, taxanes, and trastuzumab that were not effective[1][8]. Capecitabine is an oral prodrug of 5-fluorouracil (5-FU), an antimetabolite that interferes with DNA synthesis. Lapatinib is a small molecule tyrosine kinase inhibitor that targets both epidermal growth factor receptor (EGFR/ERBB1) and human epidermal growth factor receptor type 2 (HER2/ERBB2), inhibiting their intracellular kinase domains and blocking downstream signaling pathways involved in tumor cell proliferation and survival[3][6]. The combination has demonstrated superiority over capecitabine alone in prolonging time to progression in HER2-positive metastatic breast cancer after failure of prior therapies[8].

Brand names
TykerbXeloda
Other names
capecitabine + lapatinib
02

Targets

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

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