Drug intelligence / Profile preview

capecitabine + lapatinib + trastuzumab

Development stage
Unknown
Lead developer
GSK
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

This is a combination therapy consisting of three agents—capecitabine, lapatinib, and trastuzumab—used primarily in the treatment of HER2-positive metastatic breast cancer (MBC), especially after progression on prior trastuzumab-containing regimens. - **Capecitabine** is an oral prodrug that is converted to 5-fluorouracil (5-FU) in the body and acts as an antimetabolite chemotherapeutic agent by inhibiting DNA synthesis. - **Lapatinib** is an orally active small molecule tyrosine kinase inhibitor targeting both epidermal growth factor receptor (EGFR/ErbB1) and human epidermal growth factor receptor 2 (HER2/ErbB2), blocking downstream signaling pathways involved in cell proliferation and survival. - **Trastuzumab** is a monoclonal antibody that binds to the extracellular domain of HER2, inhibiting its signaling and mediating antibody-dependent cellular cytotoxicity. The rationale for this triplet combination lies in maximizing HER2 blockade through dual anti-HER2 targeting with both lapatinib (intracellular inhibition) and trastuzumab (extracellular inhibition), combined with chemotherapy for cytotoxic effect. Clinical studies have shown this regimen to be effective and generally well-tolerated in patients with advanced or metastatic HER2-positive breast cancer who have progressed on previous therapies[5][6]. The most common serious adverse events include neutropenia, leukopenia, diarrhea, palmar–plantar erythrodysesthesia syndrome, and anemia[5].

Other names
CLT regimenTLC regimen
02

Targets

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

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