Attention, Enzyme-Cleavable Linker, the most popular application in ADCs
Antibody–drug conjugate (ADC) is typically composed of a monoclonal antibody (mAbs) covalently attached to a cytotoxic drug (payload) via a chemical linker. The linker plays a key role in the therapeutic effectiveness of ADCs, significantly influencing their therapeutic index, pharmacodynamics, and pharmacokinetics.[1]
ADC linkers can be classified as cleavable or non-cleavable. Compared to non-cleavable linkers, cleavable linkers have the ability to exert a bystander effect, thus offering broader applicability and being more commonly used. Cleavable linkers can be further subcategorized as chemically-cleavable or enzyme-cleavable.[2] The typical mechanism of ADC action involves cellular internalization followed by trafficking to the lysosome, where high concentrations of specific hydrolytic enzymes provide an opportunity for enzyme-cleavable linkers to be selectively cleaved inside the cell. Currently, the application of enzyme-cleavable linkers has been the most successful. Of the 15 ADC drugs on the market, 8 utilize enzyme-cleavable linkers.[3-4]
ChemExpress advantages
As one of the earliest CDMO companies engaged in ADC payload & linker manufacturing, ChemExpress provides a variety of enzyme-cleavable linkers. We have a rich inventory of ADC small molecule products, including over 80 payloads and more than 400 linkers. If you have any requirements regarding ADC, in addition to the ADC payloads & linkers in stock, we can also provide you with customized services to meet your needs for ADC projects. Please email us at [email protected] to get more information.
Enzyme-Cleavable Linker List
[1] Chem Soc Rev, 2019, 16, 4361-4374.
[2] Nat. Rev.Drug Discovery, 2017, 16, 315–337.
[3] Cancer Res, 2008, 68, 9280–9290.
[4] Bioconjugate Chem, 2015, 26, 650–659.