Drug intelligence / Profile preview

trastuzumab deruxtecan + pembrolizumab

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 + pembrolizumab** is an investigational combination therapy comprising trastuzumab deruxtecan, an antibody-drug conjugate that targets HER2 (human epidermal growth factor receptor 2), and pembrolizumab, a monoclonal antibody that inhibits PD-1 (programmed death receptor-1). Trastuzumab deruxtecan delivers a cytotoxic topoisomerase I inhibitor to HER2-expressing cancer cells, leading to cell death, while pembrolizumab potentiates antitumor immunity by preventing PD-1/PD-L1-mediated immune evasion. The combination is primarily under investigation for HER2-positive and HER2-low metastatic breast cancer, endometrial cancer, and advanced gastric/esophageal/gastroesophageal junction adenocarcinoma, aiming to produce additive or synergistic antitumor effects by combining targeted cytotoxic and immune checkpoint blockade mechanisms[1][2][4][7][10].

Brand names
Keytruda (for pembrolizumab)Enhertu (for trastuzumab deruxtecan)
Other names
trastuzumab deruxtecanpembrolizumabDS-8201aDS8201aDS 8201aT-DXd
02

Targets

PDCD1 (Programmed cell death protein 1 receptor)TOP1 (DNA Topoisomerase I)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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