ADC (antibody-drug conjugate) drugs consist of a monoclonal antibody, a linker and an active drug (payload). By binding monoclonal antibodies to specific antigens on the surface of tumor cells, cytotoxic drugs are delivered to tumor lesions in a targeted manner, significantly improving safety and efficacy compared to traditional chemotherapeutic and biological drugs.
The linker is a crucial part of the ADC, which determines the drug release mechanism, PK, therapeutic index and safety of the ADC. Linkers can be divided into two categories: cleavable and non-cleavable. Cleavable linkers are sensitive to the intracellular environment and release free effector molecules and antibodies, such as acid cleavage linkers and protease cleavage linkers, through a combination of catabolism and dissociation in the cell. They are usually stable in blood, but rapidly cleave in low pH and protease-rich lysosomal environments, releasing effector molecules. Non-cleavable linkers are a new generation of linkers that have better plasma stability and tolerance than cleavable linkers, thus reducing off-target toxicity and providing a larger therapeutic window.
Polyethylene glycol (PEG) is one of the most widely used linkers in targeted therapies.
Role of PEG Linker in ADC
1. Increase water solubility. Sacituzumab-govitecan (IMMU-132) improves water solubility by coupling a cleavable maleimide linker with a short PEG unit to SN-38.
2. Increase the DAR (drug-to-antibody ratio) to improve the efficacy of ADC drugs based on low toxicity.
3. Increase the circulating half-life of ADC drugs.
Huateng Pharma is dedicated to being your most reliable partner to provide high-quality PEG linkers to promote the progress of your ADC R&D. PEG Linker is one of the most widely used linkers in ADCs, which can increase the water solubility, improve the DAR value and increase the cycle half-life of ADCs.
PEG Linkers for ADC Drugs
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