Antibody-drug conjugates (ADCs) are expected as next therapeutic antibodies, and the number of administrated ADCs has been increased. Antibodies are conjugated by potent toxic low-molecular weight compounds via linkers. The conjugated toxins are delivered to targeted region and released. ADCs expands safety-margin of low molecular compounds. For developing efficient ADCs, contribution from both synthetic organic chemistry and analytical chemistry are essential. By traditional protein conjugation methodology, numerous numbers of ADCs are generated. Now, second-generation ADCs with wider safety-margin is highly required. For the purpose, methodology of homogeneous ADC preparation is highly required. In order to develop efficient ADCs, variation of linker has been increased. In addition, the synthesized ADCs must be characterized for quality evaluation. Especially, high resolution MS and Ultra-Performance Liquid Chromatography (UPLC) analyses are useful for ADC characterization.
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