“…Peptides, as constituents of proteins, are promising, safe, and effective anti-cancer therapeutics and are engaged in nearly all biological functions. Short peptides do not induce an undesired autoimmune response; they have high selectivity and specificity, are able to cross cell membranes, and penetrate tumors more efficiently [ 16 , 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 , 25 , 26 , 27 ]. Herein, applications of peptide-drug conjugates, their basic components, conjugation chemistry, release action, and different stages of their clinical development, regulatory procedures, and other challenges are presented.…”