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trastuzumab rezetecan + pertuzumab
- Development stage
- Phase 3
- Lead developer
- Hengrui Therapeutics
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Trastuzumab rezetecan + pertuzumab is an investigational combination therapy consisting of trastuzumab rezetecan (SHR-A1811), a human epidermal growth factor receptor 2 (HER2)-directed antibody-drug conjugate (ADC), and pertuzumab, a recombinant humanized monoclonal antibody targeting HER2. Trastuzumab rezetecan consists of a humanized anti-HER2 IgG1 monoclonal antibody conjugated via a cleavable tetrapeptide-based linker to a topoisomerase I inhibitor payload (rezetecan). Pertuzumab binds to subdomain II of the extracellular domain of HER2, preventing HER2 from pairing (dimerizing) with other HER receptors. By combining these two agents, the regimen achieves dual HER2 blockade, enhancing tumor cell internalization of the ADC and maximizing direct cytotoxicity and inhibition of downstream signaling pathways. This combination is primarily being developed for the treatment of HER2-positive breast cancer, including in the first-line metastatic and neoadjuvant settings.
- Other names
- Aivida + pertuzumabSHR-A1811 + pertuzumabtrastuzumab rezetecan + pertuzumab
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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