Peptide Research Timeline: 1953 to 2026

The modern era of peptide science begins with a single landmark achievement — the first total chemical synthesis of a biologically active peptide hormone.

• 1953 — Oxytocin synthesized: Vincent du Vigneaud and his team at Cornell University Medical College achieved the first total synthesis of oxytocin, a 9-amino-acid neuropeptide hormone. This proved that peptides could be constructed entirely in the laboratory and retain full biological activity.
• 1955 — Nobel Prize: Du Vigneaud was awarded the Nobel Prize in Chemistry for this work, establishing peptide synthesis as a legitimate and transformative field of chemistry.
• 1955 — Insulin sequencing: Frederick Sanger completed the amino acid sequence of insulin (51 amino acids), demonstrating that proteins and peptides have defined, reproducible structures. This work earned Sanger his first Nobel Prize.
• 1958 — First synthetic ACTH fragments: Researchers began synthesizing fragments of adrenocorticotropic hormone (ACTH), demonstrating that specific segments of larger peptides could retain biological activity — a concept central to later peptide drug design.

The invention of solid-phase peptide synthesis (SPPS) removed the primary bottleneck in peptide research: the laborious, low-yield process of synthesizing peptides in solution. Simultaneously, neuroendocrine research began identifying the hypothalamic hormones that would later inspire therapeutic peptides.

• 1963 — Solid-phase peptide synthesis: R. Bruce Merrifield at Rockefeller University developed SPPS, a method for building peptides on an insoluble solid support. This reduced synthesis time from months to days and made longer peptides accessible. Merrifield received the Nobel Prize in Chemistry in 1984 for this contribution.
• 1969 — First total synthesis of insulin: Teams in the US and China independently achieved the total chemical synthesis of insulin, confirming that complex peptide hormones could be manufactured.
• 1971 — GHRH characterization begins: Andrew Schally and Roger Guillemin independently characterized hypothalamic releasing hormones (including GHRH and GnRH), earning the 1977 Nobel Prize in Physiology or Medicine. Their work revealed the signaling peptides that control pituitary hormone release — the foundation for compounds like sermorelin and gonadorelin.
• 1977 — Somatostatin synthesized: The synthesis of somatostatin (a growth hormone-inhibiting peptide) demonstrated the therapeutic potential of peptide analogs, leading to the development of octreotide and other clinically used somatostatin analogs.

The 1980s brought a shift from pure chemistry toward therapeutic application. Growth hormone-releasing peptides (GHRPs) were developed, BPC-157 was first characterized, and the pharmaceutical industry began investing seriously in peptide drugs.

• 1980 — Bowers' GHRPs: Cyril Bowers at Tulane University synthesized the first growth hormone-releasing peptides (GHRPs), including GHRP-6 and its successors. These synthetic hexapeptides stimulated GH release through a then-unknown receptor — later identified as the ghrelin receptor. Bowers' work directly led to modern GH secretagogues like ipamorelin, hexarelin, GHRP-2, and GHRP-6.
• 1983 — BPC-157 first described: Croatian researcher Predrag Sikiric and colleagues first characterized Body Protection Compound from human gastric juice. Over the following decades, BPC-157 would become one of the most studied research peptides, with over 100 animal studies demonstrating tissue-protective properties.
• 1984 — Merrifield Nobel Prize: Bruce Merrifield received the Nobel Prize in Chemistry for SPPS, cementing peptide synthesis as an essential technology in biochemistry and drug development.
• 1985 — Recombinant human GH: The FDA approved recombinant human growth hormone (Protropin), produced via recombinant DNA technology. This marked a shift from extraction-based to biotechnology-based peptide and protein production.
• 1986 — Thymosin research expands: Allan Goldstein's laboratory continued research on thymosin peptides, including thymosin beta-4, establishing their roles in immune regulation and wound healing.

The 1990s saw the identification of the ghrelin receptor (connecting Bowers' GHRPs to endogenous physiology), the FDA approval of sermorelin, and the emergence of melanocortin peptides for skin and sexual function research.

• 1992 — Sermorelin FDA approval: Sermorelin (Geref), a GHRH analog, received FDA approval for diagnostic evaluation of pituitary GH secretion and later for GH deficiency in children. It became the first GHRH-based peptide to reach clinical use.
• 1996 — Melanotan peptides developed: Researchers at the University of Arizona developed Melanotan II, a synthetic melanocortin agonist designed to stimulate skin tanning without UV exposure. Side effects including sexual arousal led to the development of PT-141 (bremelanotide) for sexual dysfunction.
• 1999 — Ghrelin discovered: Masayasu Kojima and colleagues discovered ghrelin, the endogenous ligand for the GH secretagogue receptor that Bowers' GHRPs had been activating for nearly two decades. This discovery connected synthetic GHRPs to a major physiological appetite and GH regulation system.
• Late 1990s — GHK-Cu research: Loren Pickart expanded research on GHK-Cu (copper peptide), demonstrating its effects on skin remodeling, wound healing, and gene expression modulation. His work established GHK-Cu as the most-studied cosmetic peptide.

The 2000s represented a turning point for peptide therapeutics. The first GLP-1 agonists reached the market, BPC-157 mechanism research accelerated, and peptide drugs began treating mainstream conditions like diabetes.

• 2005 — Exenatide (Byetta) approved: The FDA approved exenatide, a synthetic version of exendin-4 (a peptide found in Gila monster venom), as the first GLP-1 receptor agonist for type 2 diabetes. This launched the GLP-1 drug class that would eventually transform obesity treatment.
• 2008 — Tesamorelin studies: Clinical trials demonstrated that tesamorelin (a GHRH analog) significantly reduced visceral adipose tissue in HIV-associated lipodystrophy, leading to FDA approval in 2010 as Egrifta.
• 2009 — BPC-157 mechanism studies: Sikiric's group published key research on BPC-157's interaction with the nitric oxide system and its effects on blood vessel formation (angiogenesis), establishing proposed mechanisms for its tissue-protective effects.
• 2010 — Liraglutide (Victoza) approved: Novo Nordisk's liraglutide received FDA approval for type 2 diabetes, becoming the first once-daily GLP-1 agonist. Liraglutide was later approved as Saxenda (2014) for chronic weight management at a higher dose.
• 2010 — Tesamorelin (Egrifta) approved: The FDA approved tesamorelin for HIV-associated lipodystrophy, making it the only FDA-approved GHRH analog for therapeutic use.

The 2010s saw GLP-1 agonists evolve from diabetes treatments to blockbuster obesity drugs, while longevity-focused peptide research expanded with epitalon, MOTS-c, and senolytic peptides.

• 2012 — Epitalon longevity research: Vladimir Khavinson's team published research on epitalon (epithalon), a synthetic tetrapeptide that activates telomerase, the enzyme that maintains chromosome-protecting telomere length. The research suggested potential anti-aging effects at the cellular level.
• 2015 — MOTS-c discovered: Changhan David Lee at USC identified MOTS-c, a mitochondrial-derived peptide that regulates metabolic homeostasis. Exercise was shown to increase circulating MOTS-c levels, and exogenous MOTS-c improved insulin sensitivity and fat metabolism in animal models.
• 2017 — Semaglutide (Ozempic) approved: The FDA approved semaglutide for type 2 diabetes under the brand name Ozempic. With a 7-day half-life enabling once-weekly dosing and superior efficacy to liraglutide, semaglutide set a new standard for GLP-1 therapy.
• 2017 — FOXO4-DRI senolytic peptide: Dutch researchers published preclinical data on FOXO4-DRI, a peptide that selectively induces apoptosis in senescent cells while sparing healthy cells. This sparked intense interest in peptide-based senolytics for aging.
• 2019 — PT-141 (Vyleesi) approved: The FDA approved bremelanotide (PT-141) as Vyleesi for hypoactive sexual desire disorder in premenopausal women — the first melanocortin-based peptide drug approved for sexual dysfunction.
• 2019 — Oral semaglutide (Rybelsus) approved: The FDA approved oral semaglutide as Rybelsus for type 2 diabetes — the first oral GLP-1 agonist, using SNAC technology to protect the peptide from gastric degradation.

The 2020s have been defined by the explosion of GLP-1-based therapies, next-generation multi-receptor agonists, and a rapidly evolving regulatory landscape that reshaped peptide access.

• 2021 — Wegovy approved: The FDA approved semaglutide 2.4 mg (Wegovy) for chronic weight management, marking the first GLP-1 agonist specifically approved for obesity. The STEP 1 trial demonstrated 14.9% mean body weight loss over 68 weeks.
• 2022 — Tirzepatide (Mounjaro) approved: The FDA approved tirzepatide, the first dual GLP-1/GIP agonist, for type 2 diabetes. The SURMOUNT trials showed up to 22.5% weight loss, surpassing all existing anti-obesity medications.
• 2023 — Retatrutide Phase 2 results: Eli Lilly published Phase 2 results for retatrutide, the first triple agonist (GLP-1/GIP/glucagon), showing 24.2% weight loss — the highest ever recorded for an anti-obesity drug. Phase 3 trials began.
• 2023 — SELECT cardiovascular trial: The SELECT trial demonstrated that semaglutide reduced major adverse cardiovascular events by 20% in obese patients without diabetes, establishing GLP-1 agonists as cardiovascular protective agents beyond their metabolic effects.
• 2024 — FDA Category 2 peptide decision: The FDA classified several popular research peptides (including BPC-157 and AOD-9604) as Category 2 bulk drug substances, restricting compounding pharmacies from creating preparations of these compounds. See Are Peptides Legal? for full details.
• 2024 — Zepbound approved: Tirzepatide received FDA approval as Zepbound for chronic weight management, becoming the most effective FDA-approved weight loss medication.
• 2024 — Survodutide MASH results: Phase 2 results for survodutide (a dual GLP-1/glucagon agonist) showed significant histological improvement in MASH patients, with 62% achieving MASH improvement at the highest dose. It received FDA Breakthrough Therapy designation.
• 2025 — Oral Wegovy approved: The FDA approved oral semaglutide 25 mg (Wegovy pill) for chronic weight management, eliminating the injection requirement for GLP-1-based obesity treatment. The oral formulation launched at $149/month.
• 2026 — Compounded peptide landscape evolves: The regulatory environment continues to shift. Research peptide suppliers adapt to new quality standards, while next-generation compounds (retatrutide, survodutide, CagriSema) advance through Phase 3 trials with FDA decisions expected in 2026-2027.