What are Peptides? - Sports Med Review

The very first peptide that was made for clinical practice was insulin in 1921 (1). Therapeutic peptides are amino acids (1). Clinical research has rapidly increased the number of peptide drugs due to advancements in protein synthesis and gene sequencing (1). These peptides are now able to mimic the action of hormones, growth factors, and neurotransmitters (1). They can act like biologic antibodies without the immunogenic effects (1). Peptides have the potential to either enter cells or bind to cell-surface receptors (4).  Peptides have short half lives and have not been found to accumulate in the body (3). Most peptides are rapidly excreted by either heptic or renal clearance (3).

Some of the more well known peptides are the glucagon-like peptide-1 agonists, like Tirzepatide (Mounjaro) (4). One of the advantages of peptides is that they can be delivered either via oral, transdermal, or injectable routes (8).

One of the most talked about peptides in the field of orthopedics is BPC-157, also known as body protective compound-157, which is a peptide found in gastric juices that acts to promote gastric mucosal integrity (2). There is interest in BPC-157 because of its proposed anti-inflammatory effects (2). As it stands now, there is little evidence to support the use of BPC-157 for treatment of musculoskeletal injury (2). There is no FDA approved indication for its use and the peptides are not DEA scheduled (2). As a result, there is no quality and safety requirement for BPC-157 (2). The exact mechanism of BPC-157 is unknown, but the image below shows the many potential pathway mediators and downstream effects (2).

Potential mechanisms of action of BPC-157 (2)

Another frequently used peptide is collagen (5). Collagen hydrolysate is a type of collagen derivative that has been used for osteoarthritis (5). Collagen hydrolysate is comprised of varying lengths of peptides (5). Studies have shown that the peptides from collagen hydrolysate can accumulate in cartilage tissue (5). Side effects from collagen peptides include GI upset and migraines (6). There is little human data, but a study done by Dressler did show that daily collagen peptide intake could have positive effects on chronic ankle instability (9). The table listed below shows other peptides that are being looked at to aid in sports performance (8).

Peptides in sports performance (8)

Overall, peptides are groups of amino acids that can mimic naturally occurring hormones and neurotransmitters. They have been used over the last decade as medications and most recently in the treatment of Diabetes and weight loss. This review looked primarily at BPC-157, a commonly asked about peptide that has the potential to be used for musculoskeletal injuries. However, there is no current research or data to support its use in humans. Further studies are needed looking at the safety and indication for BPC-157.

By Gregory Rubin, DO

rubinsportsmed.com

References

1)      Wang L, Wang N, Zhang W, et al. Therapeutic peptides: current applications and future directions. Signal Transduct Target Ther. 2022;7:48. doi:10.1038/s41392-022-00904-4.

2)      Vasireddi N. Emerging use of BPC-157 in orthopedic sports medicine. J Orthop Surg Res. 2025; (Epub ahead of print). A review of 36 studies (1993–2024) showing that BPC-157 promotes healing by enhancing growth factors and reducing inflammation in musculoskeletal injury models, with limited human data including one injection case series of chronic knee pain. No clinical safety data are available, and the compound is not FDA-approved

3)      Józwiak M, et al. Multifunctionality and possible medical application of the widely studied but still elusive BPC-157. Pharmaceutics. 2025;18(2):185. A comprehensive preclinical review: BPC-157, a pentadecapeptide from human gastric juice, shows pleiotropic therapeutic effects in tissue injury, inflammation, GI disease, and CNS disorders. Despite a seemingly favorable safety profile in animal studies, there are no human clinical trials; it remains unapproved by regulatory authorities.

4)      Fetse JP, Varela CL, Fernandes IP, Ferreira‐Silva B, Santos HA, Costa PF. Recent advances in the development of therapeutic peptides. Trends Pharmacol Sci. 2023;44(7):425-441. doi:10.1016/j.tips.2023.04.003.

5)      Courties A, Calvet JH, Chevalier X. Efficacy and safety of collagen derivatives for osteoarthritis: a systematic review and meta-analysis of randomized controlled trials. Osteoarthritis Cartilage. 2024;32(10):1284-1298. doi:10.1016/j.joca.2024.06.011.

6)      Lin CR, Hsu YC, Chen CM, et al. Analgesic efficacy of collagen peptide in knee osteoarthritis: a systematic review and meta-analysis of randomized controlled trials. J Orthop Surg Res. 2023;18:729. doi:10.1186/s13018-023-04336-9

7)      Ghosh S, Chaudhuri B, Saha P, et al. Peptide-based biomaterials for bone and cartilage regeneration. Biomedicines. 2024;12(1):63. doi:10.3390/biomedicines12010063

8)      DeFoor MT, Dekker TJ. Injectable Therapeutic Peptides—An Adjunct to Regenerative Medicine and Sports Performance? Arthroscopy. 2025;41(2):150–152. doi:10.1016/j.arthro.2024.09.005.

9)      Dressler, P. ∙ Gehring, D. ∙ Zdzieblik, D. Improvement of functional ankle properties following supplementation with specific collagen peptides in athletes with chronic ankle instability, J Sports Sci Med. 2018; 17:298-30