2014年7月17日星期四

Antibody-drug conjugates/ADCs Related |medchemexpress


Now, let the specialized technician from famous inhibitors supplier Medchemexpress chemicals will tell people main functions of this kind of inhibitors. 
Conjugation to cytotoxic drugs or radionuclides can expand the utility of mAbs and improve their potency and effectiveness, the antibodies are thus used as a means to target and delivery a toxic payload to the selected diseased tissue. This approach is currently a major focus of therapeutic research. Antibodies have been conjugated to a number of cytotoxic drugs, though various linker chemistries and these antibody drug conjugates (ADCs) have the ability to selectively and potently kill antigen–expressing tumor cells in vitro and in xenograft studies. ADCs have demonstrated success in the clinic, and there are now two such drugs, ado-trastuzumab emtansine (Kadcyla®) and brentuximab vedotin (Adcetris®), marketed in the United States. With over 30 ADCs currently undergoing clinical studies, it is likely that more conjugates will be approved in the future.
ADC development has been an iterative learning process, with ADCs evolving from murine antibodies that were conjugated to standard chemotherapeutic drugs to fully human antibodies conjugated to highly potent cytotoxic drugs. Our understanding of ADCs has improved substantially over the past 10 years and we now understand many of the critical factors required for their successful development, including target antigen selection, antibody, linker, and payload. One area of research that has seen recent advancement is that of conjugation chemistry. The implementation of site-specific conjugation, in which conjugation occurs only at engineered cysteine residues or unnatural amino acids for example, has resulted in homogeneous ADC production and improved ADC pharmacokinetic (PK) properties.
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