Drug intelligence / Profile preview

sacituzumab govitecan + trastuzumab deruxtecan

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

**Sacituzumab govitecan + trastuzumab deruxtecan** is a combination of two antibody–drug conjugates (ADCs) used primarily in advanced breast cancer research, particularly HER2-low or triple-negative metastatic breast cancer. Sacituzumab govitecan targets TROP2 and delivers the cytotoxic topoisomerase I inhibitor SN-38, while trastuzumab deruxtecan targets HER2 and delivers the topoisomerase I inhibitor deruxtecan. Both drugs are designed to exploit tumor antigen expression to deliver cytotoxic payloads specifically to tumor cells, and are given sequentially or in alternation to address tumor heterogeneity and resistance arising from single-agent treatment. Each agent is FDA-approved as a monotherapy, but the combination regimen (alternating or sequential administration) is currently under clinical investigation for its potential to improve survival outcomes in HER2-low metastatic breast cancer[1][3][5][11].

Brand names
EnhertuTrodelvy
Other names
sacituzumab govitecantrastuzumab deruxtecanT-DXdSG
02

Targets

TOP1 (DNA Topoisomerase I)TACSTD2 (Tumor-associated calcium signal transducer 2)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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