Abstract

Peptide–drug conjugates (PDCs) are an emerging targeted therapeutic drug following on from the relative success of antibody–drug conjugates (ADCs). In this class, peptides are used to target payload molecules at the disease sites, thereby reducing toxicity and improving the physicochemical properties of the payload. A PDC is composed of three parts: peptide, linker and toxin molecule, and in this structure, the selection of the target in addition to the affinity and stability of the peptide are the keys to the success of PDCs. Since the development of ADCs, drugs have undergone several updates – can PDCs leverage the experience and lessons learned from the development of ADCs over the years to achieve new success? This review presents a systematic introduction of each component of PDCs, as well as the characteristics of PDCs under investigation, with the prospect of PDC development to deepen understanding of their mechanism of action.

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