Therapeutic peptides: Historical perspectives, current development trends, and future directions
Open accessAbstract
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.
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Peptides and proteins have better selectivity for human specific targets, better biological activity, and lower toxicity than small molecules.
“Peptides (2–50 amino acids) and proteins (more than 50 amino acids) have better selectivity for human specific targets. The larger molecular size and diverse quaternary structure enhance their interaction with specific protein pockets, making peptides and protein drugs have better biological activity and lower toxicity than small molecules.294,295”
From Smart nanoparticles for cancer therapy (2023) · cites this paper as [294]
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- Authors
- Lau, J. L., & Dunn, M. K.
- Affiliations
- Ferring Research Institute (United States) (US)
- Corresponding author
- Dunn, Michael K.
- Venue
- Bioorganic & Medicinal Chemistry
- Publisher
- Elsevier BV
- Published
- 2018-06
- Volume
- 26
- Issue
- 10
- Pages
- 2700-2707
- ISSN
- 0968-0896 (ISSN-L)
- OpenAlex
- W2724823461
- Cited by
- 1,879
- References
- 44
- Citations by year
- 2026: 146 · 2025: 179 · 2024: 205 · 2023: 236 · 2022: 299 · 2021: 275 · 2020: 278 · 2019: 194 · 2018: 59 · 2017: 3 · 2013: 1 · 2012: 1
- FWCI
- 13.65
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Bioorganic & Medicinal Chemistry (publishedVersion, cc-by-nc-nd)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Health Sciences › Medicine › Pharmacology › Microbial Natural Products and Biosynthesis
- Keywords
- peptide therapeutics, peptide drug discovery, clinical development, insulin, therapeutic areas
- MeSH terms
- Animals, Drug Evaluation, Humans, Peptides, Drug Approval, Drug Discovery, Molecular Targeted Therapy
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