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lapatinib + pertuzumab + trastuzumab
- Development stage
- Unknown
- Lead developer
- Roche
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous, Subcutaneous
01
Overview
Lapatinib + pertuzumab + trastuzumab is a combination regimen of three targeted therapies used in the treatment of HER2-positive breast cancer. Lapatinib is an oral small molecule tyrosine kinase inhibitor that blocks the intracellular domains of both HER2 (human epidermal growth factor receptor 2) and EGFR (epidermal growth factor receptor), thereby inhibiting downstream signaling pathways involved in cell proliferation. Trastuzumab and pertuzumab are monoclonal antibodies that bind to different extracellular domains of the HER2 receptor; trastuzumab binds to subdomain IV, while pertuzumab targets subdomain II, preventing dimerization with other HER family receptors. The combination aims for comprehensive blockade of HER2-driven signaling by targeting multiple sites on the receptor and its associated pathways, potentially overcoming resistance mechanisms seen with single-agent therapy. This triplet has been studied primarily in metastatic or advanced settings after progression on prior anti-HER2 regimens[1][5]. Clinical data suggest additive or synergistic effects when these agents are combined.
- Brand names
- HerceptinPerjetaTykerbTyverb
- Other names
- Triple HER2 blockade
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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