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val-ala-pabc-exatecan
- Development stage
- Preclinical
- Lead developer
- Chongqing Sintaho Pharmaceutical
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Val-ala-pabc-exatecan is a cleavable linker-payload intermediate designed for the construction of antibody-drug conjugates (ADCs). It consists of the cytotoxic payload exatecan, a potent DNA topoisomerase I inhibitor, conjugated to a cathepsin-cleavable dipeptide linker (Valine-Alanine) via a self-immolative para-aminobenzyloxycarbonyl (PABC) spacer. This specific configuration is engineered to remain stable in systemic circulation while allowing for the efficient intracellular release of the active exatecan payload upon internalization into target tumor cells and subsequent enzymatic cleavage by lysosomal proteases. It is developed by Chongqing Sintaho as part of their XDC toxin-linker platform to support the development of next-generation targeted cancer therapies.
- Other names
- Val-Ala-PAB-ExatecanVal-Ala-PABC-Exatecan
02
Targets
TOP1 (DNA Topoisomerase I)
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