Peptide-drug conjugates are a new type of conjugated drug, which usually refers to the combination of drug and targeted peptide through appropriate conjugating agent. Once the conjugate enters cancer cells through receptor-mediated endocytosis, it will promote the chemical or enzymatic release of drug. By controlling the peptide chain of about 10 amino acid sequences, it can change its conjugated hydrophobicity and ionize and target tumor cells, which affect the bioavailability in vitro and in vivo, and without causing immune response. PDCs with low molecular weight can be easily purified by HPLC technology. These characteristics of PDCs are essential for optimizing pharmacokinetics.