Therapeutic peptides: Historical perspectives, current development trends, and future directions

Bioorg Med Chem. 2018 Jun 1;26(10):2700-2707. doi: 10.1016/j.bmc.2017.06.052. Epub 2017 Jul 1.


Peptide therapeutics have played a notable role in medical practice since the advent of insulin therapy in the 1920s. Over 60 peptide drugs are approved in the United States and other major markets, and peptides continue to enter clinical development at a steady pace. Peptide drug discovery has diversified beyond its traditional focus on endogenous human peptides to include a broader range of structures identified from other natural sources or through medicinal chemistry efforts. We maintain a comprehensive dataset on peptides that have entered human clinical studies that includes over 150 peptides in active development today. Here we provide an overview of the peptide therapeutic landscape, including historical perspectives, molecular characteristics, regulatory benchmarks, and a therapeutic area breakdown.

Keywords: Clinical development; Drug discovery; Drugs; G protein-coupled receptors; Peptides.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Approval
  • Drug Discovery / methods*
  • Drug Evaluation
  • Humans
  • Molecular Targeted Therapy / methods
  • Peptides / chemistry
  • Peptides / pharmacology
  • Peptides / therapeutic use*


  • Peptides