Drug intelligence / Profile preview

capecitabine + cyclophosphamide + lapatinib + trastuzumab

Development stage
Unknown
Lead developer
Roche
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

This is a four-drug combination regimen consisting of capecitabine, cyclophosphamide, lapatinib, and trastuzumab. It is primarily used in the treatment of HER2-positive breast cancer, particularly in metastatic or advanced settings. - **Capecitabine** is an oral prodrug that is converted to 5-fluorouracil (5-FU) in the body and acts as an antimetabolite inhibiting DNA synthesis. - **Cyclophosphamide** is an alkylating agent that crosslinks DNA strands, leading to cell death. - **Lapatinib** is a 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 tumor proliferation[8]. - **Trastuzumab** is a monoclonal antibody directed against the extracellular domain of HER2/ErbB2 receptor, inhibiting its signaling and mediating antibody-dependent cellular cytotoxicity[5][6][7]. The rationale for combining these agents lies in their complementary mechanisms—capecitabine and cyclophosphamide provide cytotoxic chemotherapy with non-overlapping toxicities[1][3], while lapatinib and trastuzumab offer dual blockade of HER2 at different sites (intracellular vs extracellular), which has shown synergistic antitumor activity[5][6]. This combination aims to maximize efficacy by targeting multiple pathways critical for tumor survival and progression.

Other names
Metronomic Capecitabine, Cyclophosphamide, Lapatinib, and TrastuzumabMetronomic Capecitabine and Cyclophosphamide With Lapatinib and Trastuzumab
02

Targets

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

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