The Complete History of Peptide Research: A 100-Year Scientific Timeline
Peptides aren't new. Peptide-based medicine has over 100 years of clinical history, with the first peptide drug, insulin, saving lives since 1923.13 Today 85 peptide and polypeptide drugs hold FDA approval,2 and more than 150 are in clinical trials.3
100+
Years of research
85
FDA-approved drugs
150+
Drugs in clinical trials
What Are Peptides?
Peptides are short chains of amino acids. By the common biochemical convention a peptide runs between 2 and 50 residues, the definition the FDA quoted from Creighton's Encyclopedia of Molecular Biology when it set out its own reading of the term.4 US regulators then drew the line lower for regulatory purposes: under 21 CFR 600.3(h)(6), any defined-sequence alpha amino acid polymer longer than 40 amino acids is a protein.5 Both numbers are real and they answer different questions, so a 45-residue chain is a peptide to a biochemist and a protein to the FDA.
Mass-spectrometry surveys have catalogued tens of thousands of distinct peptide species described in the literature,6 with more than 5,000 reported in human urine alone.7 Cataloguing is not the same as function. The same work reports only around 300 human peptides with confirmed bioactivity and treats the majority of the rest as inactive degradation products.6 The ones that do carry a signal fall into familiar jobs:
The Complete Peptide Research Timeline
Frederick Banting and Charles Best isolate insulin from canine pancreatic extracts at the University of Toronto, the first peptide hormone ever isolated.11
Oliver Kamm and colleagues separate the two active principles of the posterior pituitary lobe and coin the names oxytocin and vasopressin.18 The uterine-contracting action of pituitary extract had been described by Henry Dale in 190616 and the milk-ejection action by Ott and Scott in 1910.17
Vincent du Vigneaud determines the sequence of oxytocin and synthesizes it, establishing that the hormone is a nine-residue peptide and making it the first peptide hormone ever synthesized.201921 He receives the Nobel Prize in Chemistry in 1955.22
Researchers observe that oral glucose produces a stronger insulin response than intravenous glucose. Something in the gut is amplifying insulin release, they call this the "incretin effect."30
Scientists identify GIP (glucose-dependent insulinotropic polypeptide) as one incretin hormone.31
GLP-1 (glucagon-like peptide-1) is identified when researchers sequence the proglucagon gene.
Exenatide (Byetta) becomes the first GLP-1 receptor agonist approved by the FDA for type 2 diabetes.5040 Derived from Gila monster venom (exendin-4).39
Liraglutide (Victoza) receives FDA approval. A modified human GLP-1 analog requiring only once-daily injection.50
Liraglutide (Saxenda) becomes the first GLP-1 approved specifically for weight loss in non-diabetics.4941
Semaglutide (Ozempic) receives FDA approval for diabetes, requiring only once-weekly injection due to its long half-life.50
Semaglutide (Wegovy) receives FDA approval for chronic weight management.49 The STEP 1 trial shows average weight loss of about 15% of body weight.42
Tirzepatide (Mounjaro) receives FDA approval as the first dual GLP-1/GIP receptor agonist,4950 showing up to 22.5% weight loss in trials.
Retatrutide Phase 2 trial results published. As a triple agonist (GLP-1 + GIP + Glucagon), it produces 24.2% average body weight loss at the highest dose.44
Retatrutide is in Phase 3 clinical trials. Multiple other triple agonists enter development.
85 FDA-Approved Peptide Drugs
The claim that peptides are "unproven" ignores the extensive regulatory history. THPdb2, a 2024 compilation of FDA-approved therapeutic peptides and proteins, records 85 approved peptides and polypeptides across multiple therapeutic categories.2
| Category | Examples | Years in clinical use |
|---|---|---|
| Diabetes / Metabolism | Insulin, Exenatide, Liraglutide, Semaglutide, Tirzepatide | 1923 to 20221349 |
| Hormonal | Oxytocin, Vasopressin, Goserelin, Leuprolide | 1954 to 1990s4950 |
| Cardiovascular | Nesiritide, Eptifibatide | 1998 to 200149 |
| Oncology | Octreotide, Lanreotide, Degarelix | 1988 to 20084950 |
| Immune / Inflammatory | Cyclosporine, Enfuvirtide | 1983 to 200349 |
| Bone / Metabolic | Teriparatide, Abaloparatide | 2002 to 20174950 |
| GI / Other | Linaclotide, Plecanatide | 2012 to 20174950 |
How much human data sits behind these: four registration trials alone enrolled 24,439 participants between them. SELECT enrolled 17,604,45 SURMOUNT-1 enrolled 2,539,47 TRIUMPH-1 enrolled 2,335,48 and STEP 1 enrolled 1,961.46
Currently in clinical trials: Over 150 peptide drugs are in various phases of FDA trials, including multiple next-generation GLP-1 combinations.3
Research vs Approved: Understanding the Distinction
FDA-Approved Peptide Drugs
These have completed full human clinical trials and are prescribed by doctors.4950 They are manufactured under FDA current good manufacturing practice requirements and carry continuing regulatory oversight.63
Research Peptides
Extensive animal data, limited human trials. Used in research and wellness communities:
On TB-500 specifically: no approved human or veterinary product containing thymosin beta-4 exists. It does not appear in the European medicines register,56 the only openFDA animal and veterinary record naming thymosin is an adverse event report rather than an approval,57 and it is absent from the FDA Green Book of approved animal drugs.5859 Where it turns up in veterinary practice it is as an unapproved compounded drug, not an approved indication.
Investigational (Currently in Human Trials)
Why Sourcing Is the Real Concern
The science behind most popular peptides is solid. The problem is execution. Peptides are widely sold online as research chemicals labelled not for human consumption, including on mainstream e-commerce platforms.60 Where buyers actually go has not been surveyed in Vietnam; the closest data, a survey of 736 image- and performance-enhancing drug users, found 55.6% bought through pharmacies or shops and 41.3% online.61
In Vietnam the rule that actually bites is registration. Under the Law on Pharmacy, only drugs granted a marketing registration may be traded, and only licensed establishments may trade them.62 Research peptides hold no such registration, which is why sourcing, rather than legality, is where the real risk sits.
What the Research Proves
What the Research Cannot Guarantee
- That the vial you receive contains what it claims
- That the peptide was not degraded during shipping
- That the concentration is accurate
- That contaminants are absent
What to Look For in a Supplier
Third-party Certificate of Analysis (COA)
Batch-matched testing from an independent lab
Cold-chain shipping
Peptides degrade rapidly at room temperature, especially critical in Vietnam's climate51
Transparent sourcing
Legitimate suppliers answer questions about their supply chain
Physician oversight
Not legally required everywhere, but strongly advisable for GLP-1 peptides
Frequently Asked Questions
Are peptides safe?
FDA-approved peptide drugs have extensive human safety data. Four registration trials alone enrolled 24,439 participants: SELECT (17,604), SURMOUNT-1 (2,539), TRIUMPH-1 (2,335) and STEP 1 (1,961). Research peptides such as BPC-157 and TB-500 have animal safety data but limited human clinical trials. Sourcing quality is the primary safety variable.
How long have peptides been studied?
Peptide research began in the 1920s with insulin. Oxytocin was named and separated in 1928 and shown to be a peptide in 1953. GLP-1 research runs from the 1960s incretin work to the 1980s. The earliest indexed BPC publication is 1992. That is 30 to 100 years of scientific investigation depending on the compound.
Why do people think peptides are new?
Social media discovered peptides around 2020 to 2023 when Ozempic became a cultural phenomenon and demand drove a shortage. The science is decades old; the mainstream awareness is recent.
Are peptides legal in Vietnam?
Vietnam regulates medicines by registration and licensing. Under the Law on Pharmacy, only drugs granted a marketing registration may be traded, and only licensed establishments may trade them. Research peptides hold no such registration, so they are not approved pharmaceuticals here. The statute does not address personal possession either way, which is what leaves the area gray. In practice peptides are widely sold online as research chemicals labelled not for human consumption, including on mainstream e-commerce.
What's the difference between pharmaceutical and research peptides?
Pharmaceutical peptides (Ozempic, Mounjaro) are manufactured under FDA current good manufacturing practice requirements, prescribed by doctors, and covered by regulatory oversight. Research peptides are sold for "research purposes," vary in quality, and require the buyer to verify sourcing.
Conclusion
Peptides are not new. They are not experimental in the way social media implies. Insulin has been saving lives for over 100 years.1013 GLP-1 science spans four decades. Even BPC-157 has 30+ years of published research.3437 Mainstream attention arrived only when semaglutide became a cultural phenomenon and demand drove a shortage.64
The question has never been: "Do peptides work?"
The question is: "Who do you trust to source them?"
When evaluating peptide therapy, focus less on whether the science is "proven", it largely is, and more on whether your supplier provides verifiable quality assurance.
Sources
Entries marked ° are cited from the publisher, but our checker could not retrieve the page to confirm the wording.
- 1.Muttenthaler M, King GF, Adams DJ, Alewood PF. Trends in peptide drug discovery. Nature Reviews Drug Discovery (2021) 20(4):309-325. PMID 33536635
- 2.Jain S, et al. THPdb2: compilation of FDA approved therapeutic peptides and proteins. Drug Discovery Today (2024) 29(7):104047. PMID 38830503. Records 85 FDA-approved peptides and polypeptides
- 3.Lau JL, Dunn MK. Therapeutic peptides: historical perspectives, current development trends, and future directions. Bioorganic and Medicinal Chemistry (2018) 26(10):2700-2707. PMID 28720325°
- 4.FDA, Definition of the Term "Biological Product", proposed rule, 83 FR 63817 at 63820 (12 December 2018), quoting Creighton TE, Encyclopedia of Molecular Biology, Wiley (1999): "generally a peptide has between 2 and 50 amino acid residues"
- 5.21 CFR 600.3(h)(6): "A protein is any alpha amino acid polymer with a specific, defined sequence that is greater than 40 amino acids in size."
- 6.Madsen CT, et al. Combining mass spectrometry and machine learning to discover bioactive peptides. Nature Communications (2022) 13(1):6235. PMID 36266275. Reports tens of thousands of peptides described in the literature, of which roughly 300 human peptides have confirmed bioactivity
- 7.Merchant ML, Klein JB. Proteomic discovery of diabetic nephropathy biomarkers. Advances in Chronic Kidney Disease (2010) 17(6):480-486. PMID 21044770. More than 5,000 peptides reported in human urine alone
- 8.Hughes J, et al. Identification of two related pentapeptides from the brain with potent opiate agonist activity. Nature (1975) 258(5536):577-580. PMID 1207728°
- 9.Ganz T. Defensins: antimicrobial peptides of vertebrates. Comptes Rendus Biologies (2004) 327(6):539-549. PMID 15330253
- 10.The Nobel Prize in Physiology or Medicine 1923, awarded to Frederick Banting and John Macleod for the discovery of insulin
- 11.Nobel Prize Outreach, The miracle discovery that reversed the diabetes death sentence, on Leonard Thompson and the first insulin injections in January 1922
- 12.Banting FG, Best CH, Collip JB, Campbell WR, Fletcher AA. Pancreatic extracts in the treatment of diabetes mellitus. Canadian Medical Association Journal (1922). PMC1524425
- 13.Insulin, Encyclopedia of Indianapolis, on Eli Lilly beginning commercial insulin production in 1923
- 14.UniProt P01308 (INS_HUMAN): the mature insulin A and B chains total 51 amino acid residues
- 15.World Health Organization estimate that about 100 million people worldwide need insulin, reported by NPR, 17 February 2020°
- 16.Dale HH. On some physiological actions of ergot. The Journal of Physiology (1906) 34(3):163-206. DOI 10.1113/jphysiol.1906.sp001148. First description of the uterine-contracting action of posterior pituitary extract
- 17.Ott I, Scott JC. The action of infundibulin upon the mammary secretion. Proceedings of the Society for Experimental Biology and Medicine (1910) 8(2):48-49. DOI 10.3181/00379727-8-27
- 18.Kamm O, Aldrich TB, Grote IW, Rowe LW, Bugbee EP. The active principles of the posterior lobe of the pituitary gland. Journal of the American Chemical Society (1928) 50(2):573-601. DOI 10.1021/ja01389a050. Separation of the oxytocic and pressor principles and the naming of oxytocin
- 19.du Vigneaud V, Ressler C, Swan JM, Roberts CW, Katsoyannis PG, Gordon S. The synthesis of an octapeptide amide with the hormonal activity of oxytocin. Journal of the American Chemical Society (1953) 75(19):4879-4880. DOI 10.1021/ja01115a553
- 20.du Vigneaud V, Ressler C, Trippett S. The sequence of amino acids in oxytocin, with a proposal for the structure of oxytocin. Journal of Biological Chemistry (1953) 205(2):949-957. PMID 13129273
- 21.Lee HJ, Macbeth AH, Pagani JH, Young WS. Oxytocin: the great facilitator of life. Progress in Neurobiology (2009). PMC2689929. Narrative history of oxytocin research
- 22.The Nobel Prize in Chemistry 1955, awarded to Vincent du Vigneaud for the first synthesis of a polypeptide hormone
- 23.Sanger F. Chemistry of insulin. Science (1959) 129(3359):1340-1344. PMID 13658959. Nobel lecture on determining the structure of insulin°
- 24.The Nobel Prize in Chemistry 1958, awarded to Frederick Sanger for his work on the structure of proteins, especially insulin
- 25.Antuzzi P. [Clinical tests of a new synthetic oxytocin]. Minerva Ginecologica (1954) 6(3):26-27. PMID 13165320
- 26.Synthetic oxytocin. Medical Journal of Australia (1954) 1(10):373. DOI 10.5694/j.1326-5377.1954.tb85412.x
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- 28.Francis HH, et al. Clinical trial of synthetic oxytocin. British Medical Journal (1956) 1(4976):1136-1137. DOI 10.1136/bmj.1.4976.1136
- 29.Mayes BT, et al. Experience with synthetic oxytocin. Journal of Obstetrics and Gynaecology of the British Empire (1956) 63(6):812-818. DOI 10.1111/j.1471-0528.1956.tb05567.x
- 30.Elrick H, Stimmler L, Hlad CJ, Arai Y. Plasma insulin response to oral and intravenous glucose administration. Journal of Clinical Endocrinology and Metabolism (1964) 24:1076-1082. PMID 14228531
- 31.Brown JC, Mutt V, Pederson RA. Further purification of a polypeptide demonstrating enterogastrone activity. The Journal of Physiology (1970) 209(1):57-64. PMID 5499047. Purification of GIP
- 32.Holst JJ, Orskov C, Nielsen OV, Schwartz TW. Truncated glucagon-like peptide I, an insulin-releasing hormone from the distal gut. FEBS Letters (1987) 211(2):169-174. PMID 3542566°
- 33.Kreymann B, Williams G, Ghatei MA, Bloom SR. Glucagon-like peptide-1 7-36: a physiological incretin in man. The Lancet (1987) 2(8571):1300-1304. PMID 2890903. The demonstration in humans°
- 34.Sikiric P, et al. The significance of the gastroprotective effect of body protection compound (BPC). Acta Physiologica Hungarica (1992) 80(1-4):89-98. PMID 1345210. Earliest indexed BPC publication
- 35.Sikiric P, et al. A new gastric juice peptide, BPC: an overview of the stomach-stress-organoprotection hypothesis. Journal of Physiology-Paris (1993) 87(5):313-327. PMID 8298609
- 36.Seiwerth S, et al. BPC 157 and standard angiogenic growth factors: gastrointestinal tract healing, lessons from tendon, ligament, muscle and bone healing. Current Pharmaceutical Design (2018) 24(18):1972-1989. PMID 29998800
- 37.Vasireddi N, et al. Emerging use of BPC-157 in orthopaedic sports medicine: a systematic review. HSS Journal (2025) 21(4):485-495. PMID 40756949
- 38.ClinicalTrials.gov, interventional studies registered for BPC-157°
- 39.Eng J, Kleinman WA, Singh L, Singh G, Raufman JP. Isolation and characterization of exendin-4, an exendin-3 analogue, from Heloderma suspectum venom. Journal of Biological Chemistry (1992) 267(11):7402-7405. PMID 1313797
- 40.Sundararaman L, et al. Glucagon-like peptide-1 receptor agonists: exciting avenues beyond weight loss. Journal of Clinical Medicine (2025) 14(6). PMID 40142784
- 41.Pi-Sunyer X, et al. A randomized, controlled trial of 3.0 mg of liraglutide in weight management. New England Journal of Medicine (2015) 373(1):11-22. PMID 26132939°
- 42.Wilding JPH, et al. Once-weekly semaglutide in adults with overweight or obesity (STEP 1). New England Journal of Medicine (2021) 384(11):989-1002. PMID 33567185
- 43.Jastreboff AM, et al. Tirzepatide once weekly for the treatment of obesity (SURMOUNT-1). New England Journal of Medicine (2022) 387(3):205-216. PMID 35658024
- 44.Jastreboff AM, et al. Triple-hormone-receptor agonist retatrutide for obesity, a phase 2 trial. New England Journal of Medicine (2023) 389(6):514-526. PMID 37366315
- 45.ClinicalTrials.gov NCT03574597 (SELECT), semaglutide cardiovascular outcomes, actual enrolment 17,604 participants
- 46.ClinicalTrials.gov NCT03548935 (STEP 1), semaglutide in overweight and obesity, actual enrolment 1,961 participants
- 47.ClinicalTrials.gov NCT04184622 (SURMOUNT-1), tirzepatide in obesity or overweight, actual enrolment 2,539 participants
- 48.ClinicalTrials.gov NCT05929066 (TRIUMPH-1), retatrutide in obesity or overweight, actual enrolment 2,335 participants
- 49.Drugs@FDA, original approval dates: SANDIMMUNE 14 November 1983, LUPRON 9 April 1985, INTEGRILIN 18 May 1998, NATRECOR 10 August 2001, FORTEO 26 November 2002, FUZEON 13 March 2003, FIRMAGON 24 December 2008, LINZESS 30 August 2012, SAXENDA 23 December 2014, WEGOVY 4 June 2021
- 50.DailyMed prescribing information: BYETTA, VICTOZA, OZEMPIC, MOUNJARO, EGRIFTA, ZOLADEX (initial US approval 1989), SANDOSTATIN (1988), SOMATULINE DEPOT (2007), TYMLOS (2017) and TRULANCE (2017)
- 51.DailyMed, OZEMPIC prescribing information, storage and handling section°
- 52.Pickart L, Margolina A. Regenerative and protective actions of the GHK-Cu peptide in the light of the new gene data. International Journal of Molecular Sciences (2018) 19(7). PMID 29986520
- 53.Raun K, et al. Ipamorelin, the first selective growth hormone secretagogue. European Journal of Endocrinology (1998) 139(5):552-561. PMID 9849822
- 54.Teichman SL, et al. Prolonged stimulation of growth hormone and insulin-like growth factor I secretion by CJC-1295. Journal of Clinical Endocrinology and Metabolism (2006) 91(3):799-805. PMID 16352683
- 55.Goldstein AL, Hannappel E, Sosne G, Kleinman HK. Thymosin beta-4: a multi-functional regenerative peptide. Expert Opinion on Biological Therapy (2012) 12(1):37-51. PMID 22074294°
- 56.European Medicines Agency, European medicines register: no authorised human or veterinary medicine containing thymosin beta-4
- 57.openFDA animal and veterinary adverse event API: the only record mentioning thymosin is an adverse event report, USA-USFDACVM-2019-US-058078, not a product approval
- 58.FDA, Approved Animal Drug Products (the Green Book): no approved animal drug containing thymosin beta-4
- 59.PubChem CID 45382195 (thymosin beta-4): cross-references include no FDA Green Book or other animal-drug approval source
- 60.Turnock LA, Gibbs N. Click, click, buy: the market for novel synthetic peptide hormones on mainstream e-commerce. Performance Enhancement and Health (2023) 11(2):100251. DOI 10.1016/j.peh.2023.100251
- 61.De Luca I, et al. Profiling and assessing the risks of image- and performance-enhancing drugs use. Frontiers in Public Health (2024) 12:1386721. PMID 38962770. Of 736 users surveyed, 55.6% purchased through pharmacies or shops and 41.3% online
- 62.Vietnam, Law on Pharmacy No. 105/2016/QH13, on marketing registration of drugs and the licensing of establishments permitted to trade them. Amended by Law No. 44/2024/QH15, in force from 1 July 2025°
- 63.FDA, Current Good Manufacturing Practice (cGMP) regulations°
- 64.Family Practice News (MDedge): TikTok trend triggered a diabetes drug shortage°
- 65.Peptara Labs, product, testing and shipping information, retrieved 22 August 2026°
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Disclaimer: This content is for educational purposes only. It is not medical advice. Consult a healthcare professional before starting any peptide protocol.