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sacituzumab tirumotecan + paclitaxel
- Development stage
- Unknown
- Lead developer
- Merck
- Modality
- DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
**Sacituzumab tirumotecan + paclitaxel** is a combination investigational therapy being studied primarily for advanced and metastatic solid tumors, such as HER2-negative gastric/gastroesophageal junction/esophageal adenocarcinoma. The combination consists of an antibody-drug conjugate (ADC), sacituzumab tirumotecan, and the chemotherapeutic agent paclitaxel. Sacituzumab tirumotecan targets TROP2 (trophoblast cell surface antigen 2) with a humanized anti-TROP2 monoclonal antibody linked by a novel hydrolyzable, pH-sensitive linker to a belotecan-derivative topoisomerase I inhibitor (payload), aiming to deliver cytotoxic agents specifically to cells overexpressing TROP2 and induce DNA damage and apoptosis. Paclitaxel stabilizes microtubules, inhibiting cell division. The combination is designed to increase anti-tumor efficacy via complementary mechanisms: targeted DNA damage and mitotic inhibition[1][7].
- Other names
- sacituzumab tirumotecan plus paclitaxel
02
Targets
TOP1 (DNA Topoisomerase I)TUBB (Tubulin (alpha and beta subunits))TACSTD2 (Tumor-associated calcium signal transducer 2)
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