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zamzetoclax + sacituzumab govitecan
- Development stage
- Unknown
- Lead developer
- Gilead Sciences
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Oral, Intravenous
01
Overview
This combination therapy pairs zamzetoclax, a potent and selective B-cell lymphoma 2 (BCL-2) inhibitor, with sacituzumab govitecan, a TROP-2-directed antibody-drug conjugate (ADC). Zamzetoclax (BGB-11417) is designed to promote apoptosis by inhibiting the BCL-2 protein, which is often overexpressed in various cancers to evade programmed cell death. Sacituzumab govitecan (Trodelvy) consists of a humanized monoclonal antibody targeting TROP-2 linked via a hydrolyzable linker to SN-38, a topoisomerase I inhibitor payload. The combination aims to leverage the cytotoxic effects of the ADC with the pro-apoptotic sensitization provided by the BCL-2 inhibitor, potentially overcoming resistance mechanisms in TROP-2-expressing solid tumors such as triple-negative breast cancer (TNBC), HR+/HER2- breast cancer, and small cell lung cancer (SCLC).
- Brand names
- Trodelvy
- Other names
- zamzetoclax + sacituzumab govitecan-hziyBGB-11417 + sacituzumab govitecan
02
Targets
TACSTD2 (Tumor-associated calcium signal transducer 2)TOP1 (DNA Topoisomerase I)
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