The Next Fountain-of-Youth Craze? Peptide Injections

As influencers share stories of physiological transformations, more people are seeking out experimental treatments: ‘If I can be a superhero and function at my absolute optimum, why wouldn’t I?’ The Next Fountain-of-Youth Craze? Peptide Injections

After decades of turning to diet pills, steroids and plastic surgery to alter their bodies inside and out, people are increasingly open to an alternative method: injecting themselves with peptides at home.

Proponents say that peptides—a broad category of substances including FDA-approved drugs, supplements and experimental treatments—can help them build lean muscle, shed weight, increase energy and get a dewy glow.

Though the term has appeared on a range of consumer products for years, injectable peptides are getting more attention as celebrity doctors and influencers share stories of physiological transformations that go beyond diet and exercise.

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These substances are being prescribed to patients by doctors as well as paramedical providers such as nurses and naturopaths, even though several in-demand peptides are not approved by regulators.

The lack of oversight has raised concerns about the purity of ingredients, improper dosing and unknown side effects. But advocates say they’re comfortable with any risks.

“I remember filling up my first syringe, and I was thinking, ‘Oh, my God, I can’t believe I’m gonna do this,’” said actor Brian Austin Green. Despite his fear of needles, he started taking peptide injections in 2021, when he was a contestant on “Dancing With the Stars,” under the guidance of William Seeds, an orthopedic surgeon.

Soon, he was taking three injections every morning for several months. He said that even with the show’s physical demands and grueling rehearsal schedule, “I so didn’t feel my age.”

This year, Mr. Green turns 50. He is in talks with Telegenixx, a telehealth startup where Dr. Seeds is a board member and co-founder, to start peptide injections again and promote the treatments on social media.

The startup’s chief executive declined to disclose which peptides it offers.

“People are more interested now in, What can I do to protect myself as I am aging, against disease, against stress?’” Dr. Seeds said.

Mr. Green, a father of five, said it’s important to him to be an active dad. “I don’t necessarily want to feel like I’m aging,” he said.

For years, peptides such as BPC-157, CJC-1295 and ipamorelin have been popular among bodybuilders and athletes who are seeking to speed up healing or build muscle.

The substances are being procured from compounders, a patchwork industry made up of state-licensed and FDA-registered providers, whose quality standards vary. Regulators have cracked down on their sales, and the World Anti-Doping Agency has expressly banned their use.

That hasn’t crimped broader interest. Doctors and medical spas nationwide are listing “peptide therapy” among their services and supplying injections to patients who are paying hundreds of dollars a month to take them at home.

Some consumers are going directly to suppliers of ingredients intended only for research in order to obtain the substances cheaply and without medical consultation, providers said.

In scientific terms, a peptide is a short chain of amino acids. There are thousands in the human body, and lab-produced versions that mimic them—insulin has often been cited as the first—marked great advancements in modern medicine.

Peptide-based drugs have been approved for treating diseases such as multiple sclerosis, Type 2 diabetes and obesity. But as the term “peptides” has entered the consumer vernacular, some providers have come to market them not as drugs but as rejuvenation treatments.

“We’re in this age of hyperfocus on wellness, antiaging, preventive health,” said Abraham Malkin, co-founder of two companies that offer at-home medical care. Both of them have six peptide injections on the menu, some of which Dr. Malkin takes himself. Only two of them have FDA approval, but Dr. Malkin’s website lists them for purposes outside those uses.

“We are very clear with our patients that peptides are generally not FDA-approved at this time, however we do talk to our patients to understand their health needs and enable them to purchase peptides that we feel can allow them to meet their health goals,” Dr. Malkin said.

Bec Donlan, a 36-year-old fitness coach and wellness consultant in Los Angeles, was introduced to peptide injections several years ago, as she sought to address autoimmune symptoms she believes were related to her breast implants.

“I’ve gotten back to normal health, but now I’m like ‘Great, so what else can I do?’” Ms. Donlan said. She is following a peptide regimen that she says has reduced inflammation, boosted her immune system and increased her metabolism.

Sometimes she posts about her regimen on Instagram, where she has more than 59,000 followers.

“If I can be a superhero and function at my absolute optimum, why wouldn’t I?” Ms. Donlan said.

Jamie Sherrill, a registered nurse who specializes in aesthetics, shared a TikTok last year in which she described “peptide therapy” as the future, holding a syringe in one hand and a vial in the other. She is known on the platform as Nurse Jamie.

Ms. Sherrill said her medical spa in Los Angeles County has a naturopath doctor who writes prescriptions for peptide injections. Speaking of the laser treatments and fillers she offers clients, she said, “I just think it all works so much better if you are taking a peptide.”

Some clients remain squeamish about at-home injections, Ms. Sherrill said. But she has seen interest rise over the past two years, especially as Type 2 diabetes drug Ozempic, which is taken by injection, has gained traction among people looking to lose some weight.

In addition to injections, some peptides are sold and prescribed as nasal sprays or capsules.

“I’ll have influencers or models come in and say, What can I use in addition to my Botox, microneedling or whatever else they are having done,” said Neil Paulvin, a regenerative-medicine doctor in New York City.

Tyler Jean, a 30-year-old naturopathic doctor in Los Angeles, started injecting the peptide BPC-157 daily—and sometimes twice a day—last fall alongside regular exercise and a healthy diet.

“I wanted to see how I could leverage some of these resources to better support my body’s ability to slow aging, optimize metabolism, maintain lean muscle,” said Dr. Jean, who is a patient of Dr. Paulvin. (Ms. Donlan, the fitness coach, is also one of Dr. Paulvin’s patients.)

Dr. Jean said that he stocks up on injections in New York, where they’re easier for him to get. After recently running out, he began taking BPC-157 in pill form.

Regulators have taken action against providers who sell unapproved peptides, including Tailor Made Compounding, which formerly supplied to patients of Dr. Paulvin.

In 2020, the Kentucky-based compounder pleaded guilty to a federal charge for distributing unapproved drugs, including peptides BPC-157, ipamorelin and melanotan II, also known as the Barbie peptide for its purported weight loss and tanning effects. The company was ordered to forfeit $1.7 million and placed on a three-year probation.

Now under new ownership, the company does not dispense the unapproved drugs referenced in the settlement, said Blake McLeod, the chief operating officer. Dr. Paulvin said he now works with multiple other compounders.

Generally speaking, pharmacies are not permitted to compound drug products with unapproved substances, the FDA said. A representative for the agency added that “compounded drugs should only be used to meet the needs of patients whose medical needs cannot be met by an FDA-approved drug.”

Unlike supplements that come in the form of capsules and powders, injections are subject to the agency’s premarket approval process.

While many of the peptides aren’t new, they have found new resonance in an era where influential podcasters are promoting nonconventional treatments to their audiences.

In March 2020, Upgrade Labs CEO and well-known biohacker Dave Asprey self-injected various peptides on his podcast, which included a video component. In an emailed statement, Mr. Asprey said, “You are in charge of your biology. Not your doctor. Not your government. You.”

Joe Rogan, who apologized in 2022 after critics said his popular podcast spread misinformation about Covid-19 vaccines, discussed his use of peptides on the show “Flagrant” the same year. Mr. Rogan did not respond to requests for comment.

Jordan Green, a biomedical engineering professor at Johns Hopkins University, said peptide-based drugs can sometimes be safer than other drugs meant to treat the same conditions. In 2011, he co-founded a startup that researches and develops peptide-based treatments for eye diseases.

“But, as with any drug, it needs to be carefully studied before the government and then physicians feel comfortable prescribing it to patients,” he said. Some of the results patients are describing could simply be placebo effects, he added.

Musician George Clanton, 35, learned about the at-home injections from watching the reality show “90 Day Fiancé,” on which a cast member was self-injecting a peptide called sermorelin.

“I looked it up and found a whole subculture of thousands of people discussing it every day on Reddit,” Mr. Clanton said. He ordered a few peptides online from a site that sells the substances for research purposes and indicates that they are not for human consumption. “I realize it’s stupid,” he said.

For several months before going on tour, he self-injected.

“It wasn’t like I was getting jacked,” he said, but “slowly, I just started to realize, I was waking up in the morning, ready to talk and think, instead of having to lay in the bed for an hour, and then have coffee and then mope around.”

Aside from some bruising and soreness, he hasn’t seen any downsides.

“People in my line of work, you know, sometimes there’s people injecting black-tar heroin into their bloodstream,” he said. “So I feel like this is so much less risky.”

Updated: 3-31-2023

Peptide Applications

Peptide applications may soon be as varied as peptides themselves. Indeed, cell-penetrating peptides (CPP) have served to deliver various molecules and particles into cells. Biomedical research is vastly improving and gaining ground due to the use of CPPs and synthetic peptides.

Disease diagnostics as well as future drug components show a very bright future via delivery of these therapeutic molecules such as nucleic acids, drugs, and imaging agents, to cells and tissues. From small chemical drugs to large plasmid DNA, these peptides are relatively easy to synthesize. They are also very functional and can be readily characterized.

CPPs can be manipulated in order to obtain large levels of gene expression, gene silencing, and even tumor targeting. Once they are functionalized or chemically altered, they can create effective delivery methods in order to target certain corrupt cells or tissues.

In addition to the medical and pharmaceutical arena, synthetic peptides (throughout we will interchangeably refer to synthetic peptides and cell-penetrating peptides [CPP]) have found their places in biochemistry, molecular biology, and immunology. Synthetic peptides are extremely useful in studies regarding polypeptides, as well as:

* Peptide Hormones
* Hormone Analogues
* Cross-Reacting Antibody Preparation
* Design Of Novel Enzymes

The design of synthetic peptides was begun mainly due to the availability of secondary structure prediction methods, and by the discovery of finding protein fragments that are >100 residues can assume or maintain their native structures as well as activities.

Here it is important to note that, due to the biological activity of peptides, they must take on conformational aspects which mirror their conformational properties. These are all determined by:

* Amino Acid Sequences
* Polarity Of The Medium
* Ligand Interactions, Such As: Nucleic Acids, Receptors, Metal Ions

Taking all of this into account, peptide chemists and the like have been able to perform experimental and computational techniques in order to focus on peptide conformational stability and the accompanying and resulting dynamics of such.

Molecular biologists, on the other hand, perform protein engineering processes at the level of DNA, but this work was initiated by peptide chemists. Peptide chemists were also the first to prepare synthetic peptides (a/k/a peptide libraries) in vast amounts.

Model proteins and synthetic mini-proteins have been used to observe structure-activity relationships. All of this work has catapulted scientists into present-day studies of peptide applications, for which they are varied, including biotech companies who have discovered new peptides that hold valuable pharmacologic properties.

The routine synthesis of large polypeptides or small proteins of 30-100 amino acids has enhanced peptide applications.

Synthetized Bioactive Peptides

Synthetic peptides and proteins also have their place in the market for which they have yielded billions of USDs. New chemical entities (NCE) have remained steady over the last decade, other than peptide and protein NCEs, which have been increasing. Synthetic peptides can positively influence functions and conditions of humans. In fact, several useful properties for human health using bioactive peptides have been realized, such as for these activities:

* Antimicrobial
* Antifungal
* Antiviral
* Antitumor
* Antioxidant
* Antithrombotic

All peptides exist in limited quantities within natural settings or nature. Therefore, researchers have re-produced them in their labs, and these are known as synthesized bioactive peptides.

As we can see, their applications and properties have been applied to various areas. Synthesized peptides are categorized by class and the mechanisms that they serve.

Classes of Biosynthetic Peptides & Peptidomimetics

Delving further into the particular classes of peptides is important. In order to better understand these classes, first we will explore peptidomimetrics, which are known as compounds that contain crucial elements (pharmacophore) which mimic a protein in 3D space, or a natural peptide.

They maintain a striking ability to interact with designated biological targets. They then create the same biological effect as their natural counterparts. Peptidomimetrics serve to avoid some of the issues that are associated with natural peptides, such as their duration of activity and unavailability.

In addition, properties such as potency or receptor selectivity can be improved, giving mimicking proteins the ability to aid in drug discovery. Now, for the classes of biosynthetic peptides and peptidomimetics:

Gonadorelin Super-agonists: These peptides have been used to treat endocrine cancers, most notably breast and prostate cancers. Many of the pharmaceutical products either being tested in clinical trials or currently being administered to cancer patients have not yet been replaced by gonadorelin antagonists, but this market is expected to grow steadily in the next few years.

Somatostatin Analogues: Product sales in this class are also growing in the market. There are two main products in the market that contain somatostatin agonists. They are expected to be released in generic forms fairly soon, but the formulations that are currently registered will be on the market for several years to come.

Angiotensin Converting Enzyme (ACE) Inhibitors: Many of these have not been categorized as peptides since they are primarily replacement dipeptides that are developed in mass quantities by conventional, organic synthesis. Though, if we look closely at this process, peptide synthesis is, in fact, a specialized branch of organic chemistry.

Nevertheless, the two main drugs in this class are Enalapril and Lysinopril, and new non-peptide angiotensin II receptor antagonists have been introduced as well. This is a larger class than gonadorelin super-agonists, and certainly much bigger than the somatostatin analogues classification. Currently there are over 15 launched products in this class, and counting.

HIV Protease Inhibitors: This sequence was deduced via cDNA sequences, but it was the synthesis by Dan Veber and Steve Kent that permitted the precise determination of its enzymatic activity as well as the design of synthetic vasopressin analogues. The most widely used agent of this family is Desmopressin and its therapeutic usage is for enuresis.

Calcitonins: This class of agents treats osteoporosis. Calcitonins come from three main products, and they are salmon, human and eel calcitonin. Though, some research has indicated that salmon calcitonin was 10 times stronger than human calcitonin, but this turned out to be erroneous as each of these are considered equally potent. This large peptide contains 32 amino acids.

Immunostimulating Peptides: These peptides have been produced since the 1980s. One of the most known of this class was thymopentin, a sequence of one of the Immunostimulating thymic hormones, but it was taken off the market due to reimbursement policies by insurance companies. Another thymic hormone, thymosin &alpha-1 continues to be used in South America, Southern Asia, and the Middle East.

Other peptides that have been around even longer, such as the natural human angiotensins and oxytocins, as well as ACTH-(124) are still being produced and used.

Let it be said once again that the market for peptides and proteins is steadily growing. The triggering of certain receptors or the modulation of enzymatic activities can be accomplished in specific and targeted ways by using these potent tools to guard against, and defeat human diseases.

Peptide-Based Vaccines

Specific tumor antigens have advanced the field of medicine, specifically oncology, to target cancer cells. Cancer vaccines have been developed as a result of heightened knowledge regarding the molecular basis of antigen recognition.

This has resulted in human class I or class II major histocompatibility (MHC) motifs which bind to these human classes. Here, synthetic peptides have been used for these cancer vaccines while presenting the following advantages of their uses:

* Ease Of Construction And Production
* Chemical Stability
* Lack Of Infectious Or Oncogenic Potential
* Improved Manipulation Of Immune Responses Via Epitopes That Stimulate T-Cell Subsets
* Improved Effectiveness For Generating Immune Responses To Self-Proteins

With the primary aim being that of eliciting immune responses to tumor antigens, this is an exciting area for cancer treatment where peptide immunization is playing a huge role.

Evidence largely points to T-cells being tolerant to dominant epitopes of self-proteins, but they might also respond to subdominant epitopes (an epitope is a site on an antigen surface molecule where a single antibody molecule binds).

Class I Peptide-Based Vaccines: Cancer patients can be administered (be vaccinated with) class I peptide-based vaccines. Several clinical trials have involved vaccinating patients who’ve been diagnosed with certain cancers.

This originated from various tumor antigens which resulted in patients being immunized so as to boost their immunities to self-tumor antigens. Peptide-based vaccines have offered a thorough and superior model for assessing the ability of these immunizations by measuring immunity that is generated with assays. These assays measure class I, T-cell responses.

Class II Peptide-Based Vaccines: Patients with cancer can also be immunized with class II peptide-based vaccines. Cancers that are treated with interferon to upregulate class I vaccines were found to not always respond to the vaccines. In these instances, GM-CSF was used as an adjuvant for immunizing patients.

GM-CSF is a maturation factor for skin dendritic cells as well as Langerhans cells, and may allow for more effective peptide epitope presentation than standard adjuvants used in Class I peptide-based vaccinations. Hence, they are characterized as Class II peptide-based vaccinations.

Continued clinical trials using multiple tumor antigen specific peptides for both Class I and Class II-derived epitopes are showing much promise for the treatment of cancers. Clinical trials of single peptides have shown that cancer patients can be vaccinated against self-tumor antigens, with some studies showing positive early results.

On the horizon are continuing efforts for multiple peptide vaccinations for the prevention and treatment of malignant human cancers. Other efforts include the focus on improving the immunogenicity of individual MHC-binding peptides.

Peptide Nanotubes

Nanotechnology is known as molecular manufacturing. Nanotubes are grown in laboratories and they hold thermal and electrical properties that are used in chips, for instance. Nanotubes also have the ability to be used as semiconductors with the possibility of replacing silicon. Peptide nanotubes (PNTs) are surfacing as one of the most compelling nanostructures within the field of nanotechnology. These smart self-assemblies have various applications such as:

* Sensors
* Catalysis
* Electronics
* Stimulus-Response Materials
* Nanoreactor Designs

PNT synthesis and production are extremely up and coming as they are under extensive study. Novel biomedical applications also include smart nanodevices and innovative drug delivery systems.

By controlling peptide-nanoparticle interactions, it will be possible to produce more sophisticated bio-functionalized materials with even more enhanced properties and nanostructures.

More research, however, needs to be done in determining peptide-nanoparticle interactions, and designing more precise computer modeling to help predict and guide peptide-nanomaterial binding, among other crucial nano-processes.

Antimicrobial Peptides For Food Safety

Antimicrobial peptides have also found their place as a beneficial application in the area of biomedical devices, food processing equipment, and food preservation. In the latter, peptides can be incorporated into materials that create an antimicrobial packaging (Appendini and Hotchkiss, 2002).

This type of packaging serves to sustain food safety and quality by reducing bacterial growth on product surfaces (Soares, et al., 2009). It works to inhibit, reduce, or retard the growth of unhealthy microorganisms within the food.

Specific food preservation is enacted via peptide synthesis and peptide bioproperties, making food safer for public consumption.

Advantages And Disadvantages of Peptides As Drugs

For all their usefulness and varied applications, synthesized peptides and CPPs, when used as drugs, do have disadvantages. For instance, they have to be injected, or they must consist of specific formulations due to their low bioavailability.

As well, synthesis is very costly, but this could change with increased production of necessary products such as protected amino acids, coupling reagents, and resins.

However, their advantages far outweigh any disadvantages, which include the fact that, to be effective, only small doses of peptide are needed, and the total amount to be produced is small. They also have low systemic toxicity since they do not accumulate within body tissues, organs and blood due to short half-lives.

New non-injectable peptide (and protein) formulations are being developed such as non-degradable implants, liposomes, inhalation, oral administration and more. While dozens of companies are supporting new formulations, not all are focusing on peptides and proteins.

It is considered this will change as more and more research reveals the steady benefits of synthesized peptides for human therapeutics, diagnostics, and treatments, as well as nanotechnology, food safety and food quality.

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