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sacituzumab govitecan
- Development stage
- Approved
- Lead developer
- Gilead Sciences
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Sacituzumab govitecan is a Trop-2-directed antibody-drug conjugate (ADC) used primarily for the treatment of metastatic triple-negative breast cancer (mTNBC), metastatic hormone receptor-positive/HER2-negative breast cancer, and metastatic urothelial cancer. It consists of a humanized anti-Trop-2 monoclonal antibody chemically linked to SN-38, the active metabolite of irinotecan and a topoisomerase I inhibitor. The drug binds to Trop-2-expressing tumor cells, is internalized, and releases SN-38 intracellularly via hydrolysis of its linker. This results in DNA damage-mediated cell death by inhibiting topoisomerase I activity within the targeted cancer cells.
- Brand names
- Trodelvy
- Other names
- sacituzumab govitecan-hziy
02
Targets
TACSTD2 (Tumor-associated calcium signal transducer 2)TOP1 (DNA Topoisomerase I)
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