Peptide therapy for heart health explained—covering safety, effectiveness, and what patients can expect from this innovative treatment.
Peptide therapy is rapidly advancing in medicine. In just six years, the FDA approved 26 peptide-based drugs, with more than 200 currently in clinical trials and about 600 still in early development.
With this momentum, many are curious about how peptides might affect heart health. Below are some of the most common questions on the topic.
Peptide therapy uses short chains of amino acids, called peptides, as treatment. These peptides can come from many sources. Some occur naturally in the human body, in plants, or in animals, such as peptide hormones. Others are created in the lab through chemical synthesis, genetic engineering, or computer-based design.
The idea itself isn’t new. In fact, one of the earliest and most successful peptide therapies is insulin, first introduced in the 1920s to help people with diabetes.
When it comes to heart and metabolic health, the only peptide treatments that consistently show real benefits are those in the glucagon-like peptide-1 receptor agonist (GLP-1RA) class. These include:
Other peptides often advertised in wellness settings, such as BPC-157, TB-500 (a thymosin-β4 fragment), or MOTS-c, don’t have strong human evidence to support heart benefits. None of these are approved by the FDA for medical use.
Currently, there isn’t a peptide that the FDA has approved to regenerate the human heart. The most promising candidates focus on supporting the heart’s own repair processes, such as:
But so far, these findings are mostly from animal studies or very early human trials.
One of the first peptides investigated for heart repair was Thymosin beta-4 (Tβ4), a naturally occurring peptide known for its role in wound healing and tissue repair.
In a 2014 mouse study of heart attacks, treatment with Tβ4 led to better survival, less inflammation, healthier blood vessels, reduced scar formation, and improved heart function overall.
A newer line of research has focused on peptide Lv, another naturally occurring peptide. This compound activates VEGFR-2, a receptor critical for forming and widening blood vessels. In both lab experiments and animal studies, peptide Lv promoted the growth of new vessel networks, pointing to potential use in restoring blood flow after heart damage.
Mitochondrial peptides are small proteins made inside your mitochondria, which are the energy-making structures in your cells. They’re being studied as possible therapies since they seem to enhance the natural protective functions of mitochondria.
One example is elamipretide (SS-31). This lab-made peptide is designed to target and bind to cardiolipin, a special fat molecule in the inner mitochondrial membrane. This helps stabilize the mitochondria, improve their energy production, and reduce harmful oxidative stress.
However, in May 2025, the FDA rejected Stealth BioTherapeutics’ application for elamipretide in Barth syndrome (a rare genetic heart condition) after a lengthy review, citing insufficient evidence.
Another candidate is MOTS-c, a naturally occurring peptide. During stress or after exercise, cells release more MOTS-c, which then enters the cell nucleus to activate protective genes.
In the heart, experimental studies suggest that MOTS-c helps the muscle work more efficiently. It improves how strongly the heart pumps (systolic function), how well it relaxes between beats (diastolic function), and it protects the heart’s structure from the harmful effects of type 2 diabetes.
That said, MOTS-c remains strictly experimental. The FDA has warned that no human safety data exists, and it cannot be prescribed or compounded as a medication. The US Anti-Doping Agency (USADA) also confirms that MOTS-c is not approved for therapeutic use and is banned in sports due to its experimental nature.
Another peptide drug once used in cardiology was nesiritide, marketed as Natrecor. The FDA approved it in 2001 to treat acute decompensated heart failure (ADHF), a condition where patients are hospitalized with sudden worsening of heart failure symptoms. However, its use declined over time, and the manufacturer, Janssen Pharmaceuticals, officially discontinued it in 2018.
Natriuretic peptides are hormones made by your heart and blood vessels that help control blood pressure, blood volume, and fluid balance. The word “natriuretic” means “causing sodium to be excreted in urine.” By making your kidneys release more sodium (and water), they reduce blood volume and ease the workload on your heart.
Currently being studied is ularitide, a lab-made version of a natural natriuretic peptide, which could improve survival and heart outcomes in patients hospitalized with sudden worsening heart failure. However, results suggest that ularitide does not offer a clinical benefit over standard therapy for acute decompensated heart failure.
More natriuretic peptides are still being studied for heart health.
Drugs that act on the GLP-1 pathway have shown meaningful heart benefits in large clinical trials.
At present, these benefits apply mainly to people with type 2 diabetes. An exception is semaglutide 2.4 mg (Wegovy), which may be used in adults who have both established cardiovascular disease and overweight/obesity, even if they do not have diabetes.
Currently, there are only two peptide-based drugs used in routine cardiology:
Both are FDA-approved and used in hospital settings for acute coronary syndrome (ACS) or during percutaneous coronary intervention (PCI), such as angioplasty and stent placement.
These aren’t long-term “heart health” medications for home use. Instead, they are given through an IV in the hospital during emergencies or procedures, where preventing dangerous clots is critical.
BPC-157 is a synthetic peptide modeled after one naturally found in human stomach fluid. It is still experimental, has no FDA approval, and so far, no human studies have shown heart benefits. Most of the information available comes from animal research or lab experiments.
In preclinical studies, BPC-157 appeared to protect the inner lining of blood vessels (endothelium) and organ surfaces (epithelium). Researchers described this as a “cytoprotective” effect, suggesting possible heart-protective properties.
Another claim is that it helps small blood vessels grow or adapt so they can take over the function of a blocked major vessel. This is like the body making a natural bypass when a main artery is clogged.
Only one very small pilot study has involved people. Two adults received BPC-157 infusions that seemed well-tolerated, but the study did not evaluate any heart outcomes.
The FDA has since warned that compounded BPC-157 products may carry safety risks, such as contamination or immune reactions, and has emphasized that no human safety data exists.
There isn’t one peptide that can be called the “safest” for heart health. Safety depends on the individual, the reason for treatment, the dose, and whether the drug is FDA-approved and used as studied.
Right now, the peptide medicines with the strongest evidence for protecting the heart are GLP-1 receptor agonists, especially semaglutide.
In the large SELECT trial, semaglutide 2.4 mg (Wegovy) reduced the risk of cardiovascular death, heart attack, or stroke by 20% in adults with established heart disease and overweight or obesity. This drug is FDA-approved, and while side effects are common, its overall safety profile is well-documented when used as directed.
As a rule, it’s best to rely on approved, guideline-supported therapies instead of compounded or off-label peptide products, which lack proven safety and effectiveness.
For GLP-1 medicines (e.g., semaglutide), do not use if you or a family member has had medullary thyroid carcinoma (MTC) or MEN2, or if you’ve had a serious allergy to the active ingredient.
For peptides used in prevention, mainly GLP-1 drugs, the main risks to be aware of include:
For peptides used in the hospital during a heart attack or stent procedure (like bivalirudin and eptifibatide):
“Research peptides” marketed online carry serious uncertainties. They may contain impurities, trigger immune reactions, or be poorly studied, making their safety highly questionable.
GLP-1 medicines are designed for long-term use. In large trials lasting more than three years, patients who stayed on treatment had fewer heart attacks and strokes. Once the medication is stopped, however, those benefits often fade.
In contrast, peptides used in emergency or procedural settings are strictly short-term.
For unapproved peptides, the safest duration is not to use them at all. Sticking with proven, FDA-approved options is the best way to balance benefit and safety.
When treatment is stopped, much of the progress tends to fade. With semaglutide, patients saw improvements in several cardiovascular risk factors, such as:
But these improvements did not last once therapy was discontinued. In the STEP 1 trial extension, blood pressure returned to baseline, and most cholesterol and triglyceride levels worsened after stopping semaglutide.
The FDA has flagged several widely marketed peptides as bulk substances that should not be compounded under section 503A because of safety concerns. These include:
Purchasing so-called “research-use” vials online is especially risky. These products may contain the wrong dose, lack sterility, or carry harmful impurities, making them unsafe for human use.
Yes, some peptides can be taken by mouth, but most are not absorbed well. The problem is that peptides don’t pass easily through the digestive tract. For a drug to be absorbed, it usually needs to be small, somewhat fatty (lipophilic), and able to cross cell membranes. Peptides are the opposite. They’re large, water-loving molecules that struggle to get through.
Even if peptides make it to the gut wall, they often get broken down by stomach acid, cut apart by digestive enzymes, or degraded by gut bacteria.
This is why most peptide medicines today still need to be injected rather than swallowed.
Currently, only a few peptides truly help heart health. GLP-1 drugs like semaglutide, liraglutide, and dulaglutide have solid proof that they lower heart attack, stroke, and death risks in large trials. Other peptides often promoted online, like BPC-157, MOTS-c, or thymosin fragments, lack human evidence and aren’t FDA-approved.
In hospitals, bivalirudin and eptifibatide are used during heart attacks or stent procedures, but they aren’t long-term “heart health” medications. Most experimental peptides for heart repair or mitochondrial protection are still in early research.
Stick with FDA-approved peptide drugs backed by trials. They’re proven, safer, and effective. Unregulated or “research” peptides carry unknown risks and no guaranteed benefit.
