Beyond Macros: How Tiny Peptides Are Driving a Health Revolution

When it comes to getting in shape, losing weight, building muscle, and staying in shape, “track your macros” is so 2022. Could there be another way, a better way toward optimal health in 2025? In this article we’ll discuss why it may be time to start trending a new health and wellness phrase: “Step up your peptides.”

Peptides?

Perhaps you have never heard of peptides. What are they, and what do they have to do with health and getting into shape? When it comes to our bodies, the most important players are often the smallest. Peptides are small molecules made up of short chains of amino acids, the “building blocks of proteins.” While proteins consist of 51 or more amino acids chained together by peptide bonds, peptides consist of 2-50 amino acids per chain. Though smaller than proteins, peptides play a powerful role in keeping our bodies balanced, healthy, and functioning properly.

One easy way to understand peptides is to think of amino acids like letters of the alphabet. Peptides, then, are single words made up of letters (amino acids), and proteins are full sentences, made up of long and complex chains of more than 50 amino acids, called polypeptides. 

Peptides that you may have heard of include collagen peptides for antiaging and skin health and creatine peptides for building muscle and enhancing athletic performance. But our bodies produce hundreds of different peptides used to send signals between cells, trigger specific actions, and control a variety of systems—like metabolism, mood, growth, and immune response.

What Do Peptides Do in the Body?

Peptides are a type of signaling molecule that transmits information between cells. They may bind to a receptor site on a cell, or they may be able to cross the cell membrane and exert their activity directly inside the cell.

Examples of peptides and their functions:

• Insulin – regulates blood sugar. Insulin has 51 amino acids, but is often considered a peptide, rather than a protein. Without it, blood glucose stays high because it cannot enter into cells, leading to diabetes.

• Endorphins – endogenous morphine. Endorphins are neuropeptides that relieve pain and promote a sense of wellbeing. When we exercise, endorphins and other chemicals are released, contributing to the feeling of wellbeing.

• GLP-1 (glucagon-like peptide-1) – helps control appetite and regulates insulin and glucagon release.

• Growth hormone-releasing peptides (GHRPs) – support tissue repair, metabolism, and potentially, anti-aging. These are often used by bodybuilders to help build muscle.

• Calcitonin – regulates calcium levels and bone strength.

  
  

How Are Peptides Used in Medicine?

The first therapeutic peptide, insulin, was developed in 1921. Since that time, around 100 therapeutic peptide drugs have been approved worldwide, with nearly half of these approvals occurring in the past 20 years. Many more are still being studied in clinical trials. These peptide drugs are employed or being tested in the management of an array of medical conditions including cardiovascular, neurological, infectious, and rare diseases, diabetes, fatty liver disease, cancers, inflammatory bowel conditions, and rare diseases.

An advantage of peptides over other drugs is that they are highly versatile, providing a wide variety of pharmaceutical targets, with high specificity and low toxicity. They act like messengers, or keys, carrying instructions and unlocking specific actions in the cells they target.

Some FDA-approved peptide-based medications include:

• Calcitonin – helps manage bone-related diseases like osteoporosis and Paget’s disease.

  
  

• Insulin – used for managing Type I and Type II diabetes.

• Semaglutide (Ozempic, Wegovy, Rybelsus) – a GLP-1 receptor agonist used for Type II diabetes and weight loss.

• Teriparatide (Forteo) – a synthetic form of parathyroid hormone used to treat osteoporosis.

• Tesamorelin (Egrifta SV) – a growth hormone-releasing hormone (GHRH) receptor agonist used to reduce visceral abdominal fat in people with HIV-related lipodystrophy.

• Tirzepatide (Mounjaro, Zepbound) – a GLP-1 receptor agonist and glucose-dependent insulinotropic polypeptide (GIP) used to treat Type II diabetes, obesity, and sleep apnea.

The Future of Peptide Research: Anti-Aging Therapies

Aging is a natural and unavoidable phenomenon characterized by various behavioral, physiological, metabolic and structural changes that occur over time. These changes are manifested in several ways, such as the loss of muscle mass and skin elasticity, compromised immune reactions, and the emergence of fine lines and wrinkles. As aging progresses, susceptibility to disease and other health complications occurs.

Antiaging peptide research is gaining increasing attention with the development of peptides that have the potential to enhance a healthy lifespan and slow or prevent aging-related consequences. One such peptide that can be found in cosmetic creams, Cu-GHK, is a naturally occurring peptide in the body that regenerates tissue and stimulates collagen formation. Argireline, a peptide similar to Botulinum toxin, exerts an anti-wrinkle effect and is also popular in cosmetics. Humanin and MOTSc are peptides derived from mitochondria that are being researched for their use in improving mitochondrial function and biogenesis.

The kidneys are often the first internal organs to exhibit aging symptoms due to their high workload.  High blood pressure exacerbates this decline by placing additional stress on the kidneys. ACE inhibitors are drugs used to improve blood flow to the kidneys and slow the decline of kidney disease, yet they are not without side effects that require regular monitoring. Peptides that mimic ACE-inhibitory activity are being studied for their antihypertensive and antiaging effects while avoiding the undesirable side effects.

Peptides to improve cognition and prevent neurodegenerative disorders like Alzheimer’s and Parkinson's are also being studied, as well as peptides to improve energy and reduce fatigue that may be helpful for Long Covid and autoimmune conditions like Chronic Fatigue. BPC-157 is a peptide with extensive animal research showing benefits for gut healing, inflammation, and muscle and joint injuries. It is currently available over-the-counter as a supplement. Peptides are also being studied as co-therapies in cancer treatment.

Peptide research for medical use has exploded over the last ten years, as is witnessed by increasing numbers of peptide therapies gaining FDA approval. Those sold as supplements and antiaging injections, however, are not approved or regulated by the FDA and caution must be used when considering taking these products.

On September 5, 2025, the FDA issued a warning for consumers and healthcare professionals to be cautious of unapproved versions of GLP-1 weight loss peptide drugs, as they have not been reviewed by the FDA for safety, effectiveness, or quality.

Are Peptide Therapies Safe?

When prescribed by a licensed medical provider, peptide therapies are generally safe and effective.

However, there are risks with unregulated peptide products:

• Some are sold illegally without FDA oversight

• Quality and purity can vary

• Possible side effects or drug interactions

  
  

It’s important to talk to your doctor before using any peptide—whether it’s prescribed, over-the-counter, or online.

The Last Word on Peptides

Peptides may be small, but they play a big role in your health. From managing blood sugar to building strong bones and supporting brain function, these tiny chains of amino acids are at the center of many essential processes—and new medical breakthroughs.

As research continues, peptides are becoming one of the most exciting areas in healthcare. But with that comes the need for caution. Stick with therapies that are medically approved and always consult your healthcare provider before trying anything new.

References

Akbarian, M., Khani, A., Eghbalpour, S., & Uversky, V. N. (2022). Bioactive peptides: Synthesis, sources, applications, and proposed mechanisms of action. International Journal of Molecular Sciences, 23(3), 1445. https://doi.org/10.3390/ijms23031445

Al Musaimi, O., Al Shaer, D., de la Torre, B. G., & Albericio, F. (2018). 2017 FDA peptide harvest. Pharmaceuticals (Basel, Switzerland), 11(2), 42. https://doi.org/10.3390/ph11020042

Berlanga-Acosta, J., Abreu-Cruz, A., Herrera, D. G. B., Mendoza-Marí, Y., Rodríguez-Ulloa, A., García-Ojalvo, A., Falcón-Cama, V., Hernández-Bernal, F., Beichen, Q., & Guillén-Nieto, G. (2017). Synthetic growth hormone-releasing peptides (GHRPs): A historical appraisal of the evidences supporting their cytoprotective effects. Clinical Medicine Insights. Cardiology, 11, 1179546817694558. https://doi.org/10.1177/1179546817694558

Cooper GM. The Cell: A Molecular Approach. 2nd edition. Sunderland (MA): Sinauer Associates; 2000. Signaling Molecules and Their Receptors. Available from: https://www.ncbi.nlm.nih.gov/books/NBK9924/

Jastreboff, A., Aronne, L., Ahmad, N., Wharton, S., Connery, L., Alves, B., Kiyosue, A., Zhang, S., Liu, B., Bunck, M., Stefanski, A., for the SURMOUNT-1 Investigators. (2022). Tirzepatide once weekly for the treatment of obesity. NEJM. 387(3), p. 205-216. https://doi.org/10.1056/NEJMoa2206038

Karimi, I., Olfati, P., Mohammed, L., Tarrad, J., Amshawee, A., Hussain, M., Schiöth, H. (2026). The anti-aging potential of antihypertensive peptides of Pariset, a dataset of algal peptides. Frontiers in Aging, 6. https://doi.org/10.3389/fragi.2025.1618082

Kunjulakshmi, K., Kumar, A., Vinod Kumar, K., Sengupta, A., Kundal, K., Sharma, S., Pawar, A., Krishna, P. S., Alfatah, M., Ray, S., Tiwari, B., & Kumar, R. (2024). AagingBase: a comprehensive database of anti-aging peptides. Database : The Journal of Biological Databases and Curation, 2024, baae016. https://doi.org/10.1093/database/baae016

Morales-Brown, P. (2025, May 2). What to know about peptides for health. Medical News Today. https://www.medicalnewstoday.com/articles/326701#about

National Cancer Institute (nd.). NCI Dictionary: Definition of endorphin. https://www.cancer.gov/publications/dictionaries/cancer-terms/def/endorphin

Rosson, E., Lux, F., David, L., Godfrin, Y., Tillement, O., Thomas, E. (2025). Focus on therapeutic peptides and their delivery. International Journal of Pharmaceutics, 675. https://doi.org/10.1016/j.ijpharm.2025.125555

U.S. Food & Drug Administration (5 September 2025). FDA’s concerns with unapproved GLP-1 drugs used for weight loss. https://www.fda.gov/drugs/postmarket-drug-safety-information-patients-and-providers/fdas-concerns-unapproved-glp-1-drugs-used-weight-loss

Usmani, S. S., Bedi, G., Samuel, J. S., Singh, S., Kalra, S., Kumar, P., Ahuja, A. A., Sharma, M., Gautam, A., & Raghava, G. P. S. (2017). THPdb: Database of FDA-approved peptide and protein therapeutics. PloS One, 12(7), e0181748. https://doi.org/10.1371/journal.pone.0181748

Wang, L., Wang, N., Zhang, W., Cheng, X., Yan, Z., Shao, G., Wang, X., Wang, R., & Fu, C. (2022). Therapeutic peptides: current applications and future directions. Signal Transduction and Targeted Therapy, 7(1), 48. https://doi.org/10.1038/s41392-022-00904-4

Wärmländer, S. K. T. S., Lakela, A. L., Berntsson, E., Jarvet, J., & Gräslund, A. (2025). Secondary Structures of human calcitonin at different temperatures and in different membrane-mimicking environments, characterized by circular dichroism (CD) spectroscopy. ACS Omega, 10(17), 17133–17142. https://doi.org/10.1021/acsomega.4c05312

Xiao, W., Jiang, W., Chen, Z. et al. Advance in peptide-based drug development: delivery platforms, therapeutics and vaccines. Signal Transducttion and Targeted Therapy 10, 74 (2025). https://doi.org/10.1038/s41392-024-02107-5

Zheng, B., Wang, X., Guo, M., & Tzeng, C. M. (2025). Therapeutic peptides: Recent advances in discovery, synthesis, and clinical translation. International Journal of Molecular Sciences, 26(11), 5131. https://doi.org/10.3390/ijms26115131

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