Research Progress of Small-Format Antibody Drug Conjugates and Analogs
In cancer treatment,the effectiveness of solid tumor treatment has always been a concern in the pharmaceutical industry.Antibodies and antibody-drug conjugates have been clinically used to treat some solid tumors,but their large molecular weights cause limited penetration and thus cannot fully exert the expected efficacy.And because it circulates for a long time in vivo,it can cause toxicity to the liver and other tissues,limit the therapeutic window.Small-format drug conjugates and their analogs,such as antibody fragment drug conjugates,scaffold antibody-drug conjugates,or peptide drug conjugates,can quickly penetrate the tumor and accumulate in the tumor tissue.Compared with traditional antibody-drug conjugates,the renal metabolism rate of small-format drug conjugates increased,enabling rapid metabolism of free drugs in plasma and reducing adverse reactions caused by long-term systemic circulation of drugs.However,its short half-life may reduce the actual amount of drug entering the tumor.Therefore,different half-life extension methods have been derived to adjust the drug half-life,increase the total amount entering the tumor tissue,and improve the therapeutic effect.This review summarizes the preclinical and clinical progress of small-format drug conjugates and their development trend to provide some reference for the development of small-format drug conjugates and their analogs.
antibody-drug conjugatepeptide drug conjugateantibody fragmenthalf-life
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