Antibody–drug conjugates (ADCs) consist of a desirable monoclonal antibody, a potent cytotoxic drug and an appropriate linker. They have gain popularity as an innovative therapeutic approach for targeted cancer treatments. ADC linkers play key roles in determining the pharmacokinetic properties, therapeutic index, selectivity and the overall success of the ADC.
A properly selected linker helps the antibody to selectively deliver the cytotoxic drug to tumor cells and accurately releases the cytotoxic drug at tumor sites. In addition to conjugation, the linkers play critical roles in ADCs’ stability during the preparation, storage and ADC systemic circulation. The design of linkers for ADCs is challenging as it has to meet stringent criteria of extracellular stability and intracellular release. Intracellular acid and reducing environment, cathepsin enzymatic hydrolysis environment can catalyze or activate the cleavage and release of the payload.
AxisPharm develops a broad range of Linkers and provide custom linker synthesis. Our current product catalog covers click chemistry tools such as DBCO, tetrazine, TCO, BCN and cycloprpene etc., biotin linkers, PEG linkers, peptide linkers, glucuronide linkers, photo cleavable linkers, dye probe linkers and folic acid peg linkers.
As a customer-oriented contract research company, we offer flexible ADC Linker product kits and Bioconjugation services with competitive price.
ref: “Linkers Having a Crucial Role in Antibody–Drug Conjugates”, Int J Mol Sci. 2016 Apr; 17(4): 561.