Tesamorelin

What is Tesamorelin?

Tesamorelin (TH9507) is a peptide, meaning it is a chain of amino acids linked into a particular configuration. More specifically, tesamorelin is made of 44 amino acids which retain the same sequence as the GHRH.

GHRH is naturally produced in the pituitary gland to stimulate the production of GH. Similar to this hormone, tesamorelin can activate the GHRH receptors and stimulate GH synthesis in the anterior pituitary gland.

Yet, the sequence is additionally enhanced with a trans-3-hexenoic acid group at the C-terminus (end) which leads to an increased affinity towards the receptors, and it also offers greater resistance against degradation.

As a result, the half-life of tesamorelin extends to 30-40 minutes, compared to the 7 minute long half-life of native GHRH.

Developed by Canadian pharmaceutical company Theratechnologies, this peptide targets lipodystrophy in HIV/AIDS patients, a condition marked by irregular fat distribution. Patients may experience noticeable fat loss in areas like the arms, legs, or face, and fat accumulation in the abdomen and around internal organs.

Often linked to specific antiretroviral treatments, this condition can lead to visceral obesity, causing metabolic issues like insulin resistance and type 2 diabetes. Therefore, lipodystrophy presents both aesthetic concerns and significant health implications.

By 2010, the peptide had undergone extensive phase 3 trials for its safety and efficacy, which led to the approval of tesamorelin by the US Food and Drug Administration (FDA). It is currently available as daily subcutaneous injections under the brand names Egrifta and Egrifta SV (“Small Volume”).

How Does Tesamorelin Work?

Tesamorelin works by activating the GHRH receptors in the anterior pituitary gland, which stimulates the production of GH and its release into the bloodstream. As a result, studies report that tesamorelin can significantly increase serum GH levels.

As mentioned, the half-life of tesamorelin extends to 30-40 minutes. Thus, the peptide results in a peak in serum GH levels within 30-60 minutes after administration.

Additionally, a trial in 13 healthy middle-aged men reported that 14 days of tesamorelin injections at 2 mg per day led to a 69% increase in mean 12-hour GH levels. Moreover, GH pulses lasted considerably longer, with a mean 55% more hormone being released during each peak.

At the same time, the total number of GH pulses as well as the amplitude of GH peaks remained within physiological limits.

GH has well-known catabolic effects on fat tissue, especially abdominal and visceral (adiposity around and inside organs) fat. Therefore, tesamorelin is expected to stimulate fat breakdown (lipolysis) and facilitate fat loss.

The increase in GH also stimulates the production of its main anabolic mediator, called insulin-like growth factor-1 (IGF-1). IGF-1 is a potent anabolic hormone that increases lean mass, tissue repairs, and cell proliferation.

The aforementioned trial reported a 2.2-fold increase in mean IGF-1 levels compared to baseline after two weeks of therapy.

The effects appear to be less notable in patients with metabolic conditions such as diabetes and obesity, as one trial in type 2 diabetes patients reported about 60% increase in IGF-1 levels within 12 weeks of tesamorelin at the same dosage.

At our clinic, experienced medical professionals carefully supervise the administration of tesamorelin. They rigorously follow stringent safety procedures, focusing on maximizing treatment effectiveness and vigilantly managing any possible side effects.

Benefits of Tesamorelin

Weight loss and especially visceral fat loss appears to be the main benefit reported in clinical trials involving tesamorelin. In addition, the peptide can also lead to improved muscle mass, cognitive function and metabolic health.

Here are some of the most notable benefits as reported in clinical trials:

• Weight loss and fat reduction: In a study involving healthy but overweight participants, tesamorelin administration (2 mg/day) resulted in an average body fat reduction of approximately 3.7lb from the initial measurements after a 52-week period. These subjects also showed an 8% decrease in visceral fat from the start of the study.
• Reduction in visceral fat: Tesamorelin is notably effective in diminishing visceral fat levels in HIV/AIDS patients. The studies reported reductions in visceral fat by up to 25% from baseline within a 52-week timeframe.
• Muscle and lean mass growth: Administering tesamorelin at a daily dose of 2 mg significantly countered muscle degradation in HIV/AIDS patients. A study observed a marked increase in muscle density and size at various body sites after 26 weeks of treatment.
• Improvement in cognitive function: A trial indicated that a daily dose of 1 mg of tesamorelin for 20 weeks enhanced cognitive function in elderly individuals with mild cognitive impairment and in healthy older adults. The improvement might be attributed to tesamorelin’s positive effects on the inhibitory neurotransmitters γ-aminobutyric acid (GABA) and N-acetylaspartylglutamate (NAAG).

Side Effects of Tesamorelin

Tesamorelin has received FDA approval for the management of AIDS-related lipodystrophy, following positive safety findings from phase 3 trials that included more than 800 HIV-positive participants.

The combined results from these trials documented the following frequencies of adverse reactions:

• Reactions at the injection site (pain, redness, induration) (24.5%)
• Achy joints (13.3%)
• Swollen limbs (6.1%)
• Muscle ache (5.5%)
• Increased insulin resistance (4.5%)
• Allergies (3.6%)
• Carpal tunnel syndrome (1.5%)

Tesamorelin is contraindicated in patients with malignancies as the increase in growth hormone can speed up tumor cell proliferation. Severe pituitary damage, pregnancy and hypersensitivity to the product are also contraindications.

How to Use Tesamorelin

Tesamorelin is typically administered as a daily dose of 1-2 mg, preferably in the evening to align with the body’s natural GH synthesis.

It’s sold as a lyophilized powder that must be reconstituted into a liquid with a suitable solvent before use.

As a powder, the peptide is stable and can be stored for long periods in cool, dark, and dry conditions. Once reconstituted, the shelf-life of the peptide depends on the solvent.

It is generally recommended to use bacteriostatic water as a solvent, since it contains a preservative that extends the shelf-life of the peptide up to 28 days when refrigerated at 36 to 46 °F.

Once reconstituted, tesamorelin can be injected only subcutaneously. Suitable areas for injection include the abdomen (2 inches from the navel), outer upper arms, or front outer thighs.

Here is a summary of all the materials required for successful reconstitution and application of the peptide:

• A vial of tesamorelin
• A vial of bacteriostatic water
• Sterile needles and syringes for reconstitution
• Sterile needles and syringes for subcutaneous injections
• Alcohol pads
• Sharps container

Once the peptide is reconstituted, there are several simple steps to follow for successful injection:

1. Wash your hands, disinfect them with hand sanitizer and put on sterile gloves.
2. Disinfect the top of the peptide vial with an alcohol swab.
3. Use a sterile syringe to draw the peptide solution.
4. Disinfect the injection site with an alcohol swab.
5. Pinch the skin at the desired injection site to form a fold and insert the needle into the skinfold at a 45-degree angle with the bevel up.
6. Inject the solution, wait a few seconds, then withdraw the needle smoothly.
7. Dispose of the needle and syringe in a sharps container.
8. Apply light pressure with an alcohol swab to the injection site.

Avoid shaking or stirring the reconstituted peptide, or tapping the syringe as this can damage the peptide and inactivate it. Rotating injection sites after each application is important to prevent local lipodystrophy.