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datopotamab monomethyl auristatin E
- Development stage
- Preclinical
- Lead developer
- AstraZeneca
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Datopotamab monomethyl auristatin E (Dato-MMAE) is an experimental antibody-drug conjugate (ADC) designed to target cells expressing the tumor-associated calcium signal transducer 2 (TROP2). It consists of the humanized monoclonal antibody datopotamab conjugated to the microtubule-disrupting cytotoxic payload monomethyl auristatin E (MMAE). While the more clinically advanced datopotamab deruxtecan (Dato-DXd) utilizes a topoisomerase I inhibitor payload, Dato-MMAE is being investigated in preclinical research as a strategy to overcome resistance to topoisomerase I inhibitors, such as those found in patients previously treated with sacituzumab govitecan. MMAE exerts its therapeutic effect by binding to tubulin and inhibiting its polymerization, which leads to G2/M phase cell cycle arrest and subsequent apoptosis in targeted tumor cells.
- Other names
- datopotamab + monomethyl auristatin Eanti-TROP2-MMAE ADCanti-TROP-2-MMAE ADCanti-TROP 2-MMAE ADC
02
Targets
TACSTD2 (Tumor-associated calcium signal transducer 2)TUBB (Tubulin (alpha and beta subunits))
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