Tesamorelin | Reviews, Clinical Trials, and Safety

Tesamorelin | Reviews, Clinical Trials, and Safety

Tesamorelin is a research peptide being studied for its fat reduction, cognitive, and regenerative effects.

Compound Overview

Class of Compound:

Peptide

Mechanism of Action:

As an analogue of growth hormone-releasing hormone, tesamorelin binds with the growth hormone-releasing hormone receptors of the anterior pituitary gland, thus stimulating the secretion of growth hormone.

Notable Studies:

Tesamorelin: a review of its use in the management of HIV-associated lipodystrophy

Tesamorelin: A hope for ART-induced lipodystrophy

Growth hormone–releasing hormone effects on brain γ-aminobutyric acid levels in mild cognitive impairment and healthy aging

Also Known As:

Egrifta, Tesamorelin Acetate, LGW5H38VE3, TH9507, UNII-LGW5H38VE3

Research Applications:

Fat reduction

Peripheral nerve health

Cognitive health

Risks:

Injection site pain

FDA approval limited to HIV patients

Prohibited by WADA

Chemical Structure

What is Tesamorelin?

Tesamorelin is a synthetic analogue of human growth hormone-releasing hormone (GHRH) that is used to stimulate the manufacture and release of growth hormone (GH) in the human body. Tesamorelin was first developed by Canadian firm Theratechnologies Inc. to treat lipodystrophy, a condition that is common in HIV patients who receive long-term antiretroviral therapy [1]. Lipodystrophy sufferers experience, among other things, increased amounts of abdominal fat—a condition that tesamorelin helps to improve.

In 2010, the United States Food & Drug Administration (FDA) first approved tesamorelin as a treatment for HIV-related lipodystrophy, and the prescription drug became available for sale under brand name Egrifta [2].

The peptide is now being researched for applications beyond body fat redistribution syndrome, including to facilitate fat loss, aid in recovery following nerve injury, and as a potential treatment of mild cognitive impairment.

Keep reading for more details on how tesamorelin works, as well as our overview of its benefits, side effects, dosage conventions, and where to buy research-grade tesamorelin online.

What Does Tesamorelin Do?

Tesamorelin is similar to GHRH (also known as growth hormone-releasing factor) in structure and effects, but it is actually a peptide, composed of 44 amino acids as well as a trans-3-hexenoic acid group [3]. The latter helps to make tesamorelin more stable and longer-lasting than natural GHRH.

As an analogue of GHRH, tesamorelin binds to the growth hormone-releasing hormone receptors (GHRHr) located in the anterior pituitary gland, thereby prompting the somatotropic cells therein to synthesize and release growth hormone (GH) in the body [4].

Growth hormone is a powerful anabolic hormone, one of the most important chemical signals for the body to build and repair tissue. It is involved in many processes, from creating new muscle to repairing torn tissue and even breaking down fat. GH is plentiful in the body during childhood and adolescence, but decreases with age. This process of decline can affect athletic performance, mobility, and the length of time it takes to recover from an injury [4].

Given the above, a GHRH analogue like tesamorelin can be successfully used to stimulate the production of GH to address a variety of conditions like growth hormone deficiency, fat accumulation, cognitive decline, and nerve injury.

Tesamorelin Benefits | Clinical Trials

As tesamorelin has been approved by the FDA, there has been extensive research on the peptide and we know quite a lot about it. Here is what the research says about how tesamorelin might benefit subjects and how it can be used.

Reduction of adipose tissue: The primary and approved use of tesamorelin is to treat HIV-afflicted individuals who suffer from lipodystrophy, a condition that causes the accumulation of fat in the upper back and around the stomach [5]. This increase in adipose tissue can cause body image issues as well as increase the risk of heart attack and other cardiovascular diseases.

Tesamorelin has been shown to trigger lipolysis (fat loss) in individuals with this condition. In HIV-infected patients with lipodystrophy and excess body fat around the abdomen, tesamorelin was found to significantly decrease subcutaneous adipose tissue (body fat) by 15 percent [6]. In contrast, the control group participants experienced a five percent increase in body fat. In this same study, tesamorelin was also found to improve insulin resistance and cholesterol.

More importantly, patients’ scores on body image improved significantly in the tesamorelin group, with subjects perceiving their bodies as more attractive following treatment [6].

These results are not isolated, having been confirmed by a review of four randomized controlled trials [7]. The research suggests that tesamorelin is actually four times more effective in reducing adipose tissue (body fat) than all other treatments combined [8].

Recovery from peripheral nerve damage: Injury, surgery, and even diabetes can cause peripheral nerve damage and result in the loss of motor and sensory function in various parts of the body. Typically, there is very little that can be done about this, as nerve cells are difficult to regenerate.

However, promising research has shown that tesamorelin and other GHRH secretagogues can improve the extent to which nerves can regenerate themselves, with tesamorelin being investigated as one of the more promising treatment options [9].

Improved cognitive function: There is also research about the role that GHRH analogues, including tesamorelin, may play in improving cognitive function in subjects with mild cognitive impairment.

A large study has found evidence that tesamorelin may increase levels of certain neurotransmitters in the brain that are associated with the prevention and treatment of cognitive decline [10]. More research is needed to confirm these findings.

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Tesamorelin Side Effects

Based on human clinical trials, tesamorelin is not associated with any severe side effects. However, as with most peptides, there are a number of mild side effects associated with tesamorelin administration, including:

Swelling and itching at or around the injection site

Muscular aches and pain

Diarrhea

Sweating

Less common but more serious side effects include:

Diarrhea with fever and dehydration

Shortness of breath

Muscle or joint pain

Numbness, tingling, swelling in arms or legs

Another notable risk of tesamorelin is that it may cause glucose intolerance and increase the risk of type 2 diabetes mellitus. It is contraindicated during pregnancy [5].

Is Tesamorelin Safe?

As noted above, the FDA has approved injectable tesamorelin to treat HIV-associated lipodystrophy. To gain that approval, the peptide underwent two Phase 3 clinical trials and was determined by the FDA to meet the requirements of safety and efficacy for the specific purpose of reducing excess abdominal fat in in HIV-infected patients with lipodystrophy [2].

That said, it falls upon researchers to weigh the risks against the benefits of administering non-prescription tesamorelin for any other purpose, including general weight loss management. Non-prescription tesamorelin should only be handled by a qualified researcher or laboratory professional, and under no circumstances should it be self-administered for a non-research purpose.

Tesamorelin Dosage Calculator

For reference, in the treatment of HIV-associated lipodystrophy, patients are typically directed to subcutaneously inject 2 mg of tesamorelin, at least 90 minutes after eating, preferably before bedtime, in a single injection, a total of five nights per week [3].

For research purposes, a typical tesamorelin dose is 1 mg per dose, injected subcutaneously late at night, at least 90 minutes after eating. For testing on a first-time tesamorelin subject, it is important to begin with the lowest dose possible and increasing as needed.

Tesamorelin should not be administered indefinitely or continuously—regardless of the research application. It is commonly administered in cycles, whose lengths vary based on the research purpose.

Where to Buy Tesamorelin Online? | 2024 Edition

Peptide investigators and laboratory professionals looking to source tesamorelin online for a research study are well-advised to visit our preferred vendors.

Here they are:

Xcel Peptides

Xcel Peptides is an accredited US-based vendor that offers research-grade tesamorelin for $79 per 10mg vial, with discounts available.

We fully endorse this vendor for the following reasons:

Quality Assurance: Xcel Peptides has a rigorous quality control program in place to ensure that all of their peptides are up to standard. They source their peptides from clean, certified American facilities.

Pure Peptides: Xcel Peptides sells peptides that exceed 99% purity to ensure quality and consistent results in research. Purity is assessed via high performance liquid chromatography and mass spectrometry (HPLC-MS) testing.

Fast Shipping: Xcel Peptides offers secure online shopping with affordable shipping. Domestic orders over $200 get free shipping.

High-Quality Information: The vendor’s website includes detailed research summaries of each peptide up for sale, as well as peptide research-related tips.

Limitless Life

Limitless Life is another one of our preferred peptide vendors. We highly recommend this company because of their quality control practices, commitment to safety, and dedication to customer services.

Here are a few things that really make Limitless Life stand out:

Exceptional Quality Control: Limitless Life demonstrates their commitment to exceptional quality control practices by ensuring that each batch of peptides is tested and verified by a third-party laboratory.

Outstanding Reputation: Thanks to their dedication to customer satisfaction, product quality, and safety, Limitless LIfe has earned high reviews and has an exceptionally low rate of credit card charge-backs.

Responsive Service Team: For those based in the US, Limitless Life’s service team is available Monday through Friday during normal business hours. In addition, they keep weekend hours, so they’re available seven days per week.

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FAQ

Tesamorelin typically comes in the form of powder and must be reconstituted using bacteriostatic or sterile water.

After being reconstituted, tesamorelin is administered subcutaneously.

Tesamorelin needs to be reconstituted with bacteriostatic or sterile water. Follow all standard safety precautions during reconstitution, including wiping the tops of the vials with alcohol wipes and avoiding all contact with the syringe used to pull the bacteriostatic or sterile water. To properly reconstitute the peptide solution, take care to drip the reconstituting liquid down the side of the peptide vial. Let the solution dissolve on its own.

In the United States, tesamorelin is available as a prescription medication for patients with HIV-associated lipodystrophy, and may be purchased as Egrifta at a pharmacy.

For all other uses, qualified researchers may buy tesamorelin as a reference material from a vendor.

In the domain of competitive sport, it is important to note that tesamorelin and other growth hormone-releasing hormone analogues are banned by the World Anti-Doping Agency, meaning that they cannot be used by athletes competing under any of the over 650 sports organizations that have adopted the World Anti-Doping Code [11].

Only qualified researchers or laboratory professionals are generally advised to purchase and possess tesamorelin.

While tesamorelin is FDA-approved as a treatment for HIV-associated lipodystrophy and has exhibited minimal side effects in published research to date, researchers should note the lack of long-term clinical studies involving tesamorelin as a risk of administration.

Yes, tesamorelin has been evaluated by the FDA and is an approved treatment for HIV-related lipodystrophy. Numerous studies have been undertaken to prove the effectiveness of tesamorelin as a treatment of this condition, and it is being researched for a variety of other purposes.

Tesamorelin’s research-backed benefits include its ability to increase lean muscle area and decrease muscle fat in adults with HIV [12] and its ability to lower levels of visceral adipose tissue (VAT) in patients with HIV-related lipodystrophy [1]. Research has also shown that tesamorelin is able to trigger lipolysis (fat burning) in lipohypertrophy patients [7].

No, tesamorelin is not an anabolic-androgenic steroid. It is a polypeptide analogue of growth hormone-releasing hormone.

No, tesamorelin does not act to boost testosterone production.

Although World Anti-Doping Agency (WADA) regulations prohibit the use of growth hormone-releasing hormones (GHRHs) such as tesamorelin in sports, we do not have conclusive evidence that tesamorelin can build muscle, or enhance athletic performance, in healthy individuals [13].

No, in published studies to date, tesamorelin has not been found to cause weight gain. In fact, a primary benefit of tesamorelin is its ability to prompt the reduction of adipose tissue, and consequently to produce weight loss.

Tesamorelin | Reviews

Peptide researchers are excited about the diverse range of benefits offered by tesamorelin.

It is now an FDA-approved lipodystrophy treatment that has been proven to help HIV patients reduce stubborn belly fat. Several high-quality, randomized, placebo-controlled studies have shown that subjects lose significant amounts of fat when they take this peptide.

While studies into tesamorelin’s effect in healthy individuals are lacking, the pepide’s clear impact on lipid metabolism and cognitive health makes it an ideal candidate for further research.

To purchase tesamorelin online, we recommend the vendor with the purest peptides and most secure buying experience on the market.

References

Dhillon S. Tesamorelin: a review of its use in the management of HIV-associated lipodystrophy. Drugs. 2011 May 28;71(8):1071-91. doi: 10.2165/11202240-000000000-00000. PMID: 21668043.

Egrifta FDA Approval History - Drugs.com. (2022). Retrieved May 6, 2022, from https://www.drugs.com/history/egrifta.html

Food and Drug Administration (2010). Chemistry Reviews: Application 22-505. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022505Orig1s0 00ChemR.pdf

Macintyre JG. Growth hormone and athletes. Sports Med. 1987 Mar-Apr;4(2):129-42. doi: 10.2165/00007256-198704020-00004. PMID: 3299611.

Patel, Akash et al. “Tesamorelin: A hope for ART-induced lipodystrophy.” Journal of pharmacy & bioallied sciences vol. 3,2 (2011): 319-20. doi:10.4103/0975-7406.80763

Falutz J, Allas S, Blot K, Potvin D, Kotler D, Somero M, Berger D, Brown S, Richmond G, Fessel J, Turner R, Grinspoon S. Metabolic effects of a growth hormone-releasing factor in patients with HIV. N Engl J Med. 2007 Dec 6;357(23):2359-70. doi: 10.1056/NEJMoa072375. PMID: 18057338.

Canadian Agency for Drugs and Technologies in Health (2016). Clinical review report: Tesamorelin (Egrifta). https://www.ncbi.nlm.nih.gov/books/NBK539124/

Mangili, A., Falutz, J., Mamputu, J. C., Stepanians, M., & Hayward, B. (2015). Predictors of treatment response to tesamorelin, a growth hormone-releasing factor analog, in HIV-infected patients with excess abdominal fat. PloS one, 10(10).

Tuffaha, S. H., Singh, P., Budihardjo, J. D., Means, K. R., Higgins, J. P., Shores, J. T., … & Brandacher, G. (2016). Therapeutic augmentation of the growth hormone axis to improve outcomes following peripheral nerve injury. Expert opinion on therapeutic targets, 20(10), 1259-1265.

Friedman SD, Baker LD, Borson S, et al. Growth Hormone–Releasing Hormone Effects on Brain γ-Aminobutyric Acid Levels in Mild Cognitive Impairment and Healthy Aging. JAMA Neurol. 2013;70(7):883–890. doi:10.1001/jamaneurol.2013.1425

World Anti-Doping Agency. World Anti-Doping Code International Standard Prohibited List 2022. WADA website. January 1, 2022. Accessed Mar 2022. https://www.wada-ama.org/sites/default/files/resources/files/2022list_final_en.pdf

Adrian, S., Scherzinger, A., Sanyal, A. et al. The Growth Hormone Releasing Hormone Analogue, Tesamorelin, Decreases Muscle Fat and Increases Muscle Area in Adults with HIV. J Frailty Aging 8, 154–159 (2019). https://doi.org/10.14283/jfa.2018.45

Knoop A, Thomas A, Fichant E, Delahaut P, Schänzer W, Thevis M. Qualitative identification of growth hormone-releasing hormones in human plasma by means of immunoaffinity purification and LC-HRMS/MS. Anal Bioanal Chem. 2016 May;408(12):3145-53. doi: 10.1007/s00216-016-9377-3. Epub 2016 Feb 15. PMID: 26879649; PMCID: PMC4830873.