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trastuzumab deruxtecan + teraplizumab
- Development stage
- Unknown
- Lead developer
- Daiichi Sankyo
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
trastuzumab deruxtecan + teraplizumab is a combination therapy consisting of the antibody-drug conjugate (ADC) trastuzumab deruxtecan and the immune checkpoint inhibitor teraplizumab. Trastuzumab deruxtecan (marketed as Enhertu) is composed of a humanized anti-HER2 monoclonal antibody (trastuzumab) covalently linked to a topoisomerase I inhibitor payload (deruxtecan) via a cleavable tetrapeptide-based linker. It targets HER2-expressing cells, delivering the cytotoxic payload directly to the tumor to induce DNA damage and apoptosis. Teraplizumab is a monoclonal antibody that targets the Programmed Cell Death Protein 1 (PD-1) receptor, blocking its interaction with ligands PD-L1 and PD-L2 to restore and enhance the anti-tumor activity of T cells. This combination is currently being evaluated in a Phase II clinical trial sponsored by Guangzhou Women and Children's Medical Center as a neoadjuvant treatment for Chinese patients with intermediate- to high-risk, HR-positive, HER2-low early-stage breast cancer.
- Brand names
- Enhertu + teraplizumab
- Other names
- trastuzumab deruxtecan + teraplizumab
02
Targets
PDCD1 (Programmed cell death protein 1 receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)TOP1 (DNA Topoisomerase I)
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