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MC-VA-PAB-exatecan
- Development stage
- Preclinical
- Lead developer
- Chongqing Sintaho Pharmaceutical
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
MC-VA-PAB-exatecan is a linker-payload intermediate designed for the construction of antibody-drug conjugates (ADCs). It features exatecan, a potent camptothecin-derived DNA topoisomerase I inhibitor, as the cytotoxic payload. The payload is attached to a maleimidocaproyl-valine-alanine-p-aminobenzyloxycarbonyl (MC-VA-PAB) linker. This specific linker chemistry utilizes a cathepsin B-cleavable valine-alanine dipeptide and a self-immolative PAB group to ensure the selective release of the active drug within the acidic environment of the lysosome following ADC internalization. The maleimide group allows for site-specific conjugation to cysteine residues on a targeting antibody. This construct is a key component of Chongqing Sintaho's ADC technology platform.
- Other names
- MC-Val-Ala-PAB-exatecanMal-Cap-Val-Ala-PAB-exatecan
02
Targets
TOP1 (DNA Topoisomerase I)
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