Product Spotlight: Historical and Current Perspectives of Peptide Therapeutics

As a follow up to our most recent Product Spotlight on Research Exemption Peptides, we thought it would be appropriate to survey the dozens of peptide drugs (peptide therapeutics) that have been approved and the many currently in the clinical pipeline. 

A comprehensive list of the peptide active pharmaceutical ingredients (APIs) would be prohibitively lengthy for this article. Since are there numerous therapeutic proteins and peptides approved for clinical use by the US FDA and an even larger amount worldwide,1 we will just address some of the commonly known or interesting ones. 

Early History
Since the epochal discovery of insulin by Sir Frederick G. Banting and John J.R. Macleod, peptide therapeutics was born.2-4  This resulted in them jointly being awarded the Nobel Prize in Physiology or Medicine 1923. For approximately the next forty years only ACTH and Calcitonin were added.5

Then in 1962, both Oxytocin and Vasopressin - albeit naturally occurring (native or endogenous) - were the first synthetically produced and clinically introduced peptide therapeutics.5  However, going forward, with the issues of a short half-life, proteolytic degradation and low solubility, future viability was seen as limited.5,6

Growth of Peptide Therapeutics
With the advent of analogous and heterologous versions, these limitations have been somewhat circumvented and peptide and protein therapeutics has grown since then.  As of an article written in 2017, there were 269 approved for clinical use since the 1980s.7 Here is a small sample:

Potential Peptides Therapeutics
As to be expected, among the ongoing items being assessed a large number are SARS-CoV-2 related.8 With their relative safety, tolerance, and efficacy and along with advances in drug delivery systems, peptide therapeutics such as neoantigen vaccines, radiolabeled peptides, and self-assembling peptides are showing exciting potential for wide applications.9

Impurity Profiles
Along with peptide therapeutics, there is a need for impurities of these peptides, for characterization and safety profiling, particularly as a part of the new drug application (NDA) and abbreviated new drug application (ANDA) process.10 In solid-phase peptide synthesis (SPPS), common impurities can include truncation or deletion sequences, pyroglutamate formation, mis-folded or unfolded peptides, degradation products, and other undesirable synthetic byproducts.  Should you need help synthesizing peptide impurities for your peptide therapeutic, we are happy to offer a quote for these custom synthesis services.

References

  1. https://www.sciencedirect.com/science/article/pii/S0968089617310222
  2. https://www.nobelprize.org/prizes/medicine/1923/summary/
  3. https://www.frontiersin.org/articles/10.3389/fendo.2018.00613/full#h5
  4. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5292515/
  5. https://www.sciencedirect.com/science/article/pii/S0968089617310222
  6. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5536290/
  7. https://www.sciencedirect.com/science/article/pii/S1359644614003997
  8. https://www.pharmaceutical-technology.com/comment/synthetic-peptides-covid-19-candidates/
  9. https://pubmed.ncbi.nlm.nih.gov/16918365/
  10. https://www.fda.gov/regulatory-information/search-fda-guidance-documents/ndas-impurities-drug-substances

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