Determination of DAR in ADC Drugs

Antibody-Drug Conjugate (ADC) is an effective tumor-targeting therapeutic drug, composed of a monoclonal antibody with specific targeting action, a small molecule cytotoxin with powerful cell-killing power, and their linker. The key feature of ADC drugs is the combination of highly selective monoclonal antibodies and toxic drugs through chemical connection. Given the remarkable efficacy and superior safety of ADC drugs, they are currently widely used for the treatment of various cancers. DrugtoAntibody Ratio (DAR) refers to the average number of toxic drug molecules connected to each antibody molecule. DAR is one of the important parameters to evaluate the production process and product quality of ADC drugs. In general, the higher the DAR, the more drug molecules are connected to each antibody molecule, and the stronger the cytotoxicity of the drug. However, a too high DAR may lead to a decrease in the stability of the ADC drug and an increase in the release rate of the drug, thereby affecting its efficacy and safety. Therefore, accurate determination of the DAR value of ADC drugs is crucial for drug development and quality control.

 

The determination of the DAR value is mainly by Mass Spectrometry (MS) and High-Performance Liquid Chromatography (HPLC). MS is to measure the relative abundance of antibody molecules and drug molecules in ADC drugs by a mass spectrometer, and thus calculate the DAR value. MS has the characteristics of high resolution, high sensitivity, and high accuracy, and can accurately measure the relative quantity of drugs and antibodies in ADC drugs. The HPLC method separates the ADC drug sample into different components, and then uses a fluorescence detector or ultraviolet detector to detect and determine the relative content of the drug and antibody, and then calculate the DAR value. The HPLC method is simple to operate, highly sensitive, suitable for large-scale sample analysis, and is widely used in the quality control of ADC drugs. MS and HPLC provide a feasible way to accurately measure the DAR value of ADC drugs.

 

MtoZ Biolabs provides drug quality research services that comply with global drug regulations for customers. Based on the advanced high-quality mass spectrometry platform and professional analysis team, we provide efficient and rapid ADC DAR value determination service packages to help you better understand the pharmacological characteristics of ADC drugs. Free consultation is welcome.