Tesamorelin

The Fat Reducer

Trim Fat Effectively: Achieve a Leaner Body with Tesamorelin

Tesamorelin is a synthetic peptide that mimics the natural hormone-releasing factor that stimulates the production of growth hormone (GH) from the pituitary gland. It’s structured as a short chain of amino acids and is used primarily for medical purposes, specifically to reduce excess abdominal fat in HIV-infected patients with lipodystrophy, a condition characterized by abnormal fat distribution.

Tesamorelin works by binding to receptors on pituitary cells in the brain, which leads to the release of growth hormone. This release can help regulate body composition by promoting the breakdown of fat and inhibiting its accumulation, particularly in the abdominal area. Unlike growth hormone itself, tesamorelin specifically targets GH secretion without significantly affecting other hormones, which helps to limit side effects related to off-target hormonal imbalances.

Potential Benefits Under Research

• Reduction of Visceral Fat: Tesamorelin has been shown to significantly reduce visceral adipose tissue (VAT), which is the fat stored within the abdominal cavity. Reducing VAT is associated with a lower risk of cardiovascular diseases and diabetes.
• Improvement in Lipid Profiles: Studies suggest that Tesamorelin may help improve lipid profiles, reducing levels of total cholesterol, LDL cholesterol (often referred to as “bad” cholesterol), and triglycerides, which could help decrease cardiovascular risk.
• Cognitive Function: There is emerging evidence that Tesamorelin may improve cognitive function, particularly in older adults or those affected by cognitive decline. The hypothesis is that growth hormone-releasing factors like Tesamorelin might have neuroprotective effects.
• Liver Health: Research indicates that Tesamorelin may reduce liver fat and potentially improve markers of liver function, which is beneficial for patients with non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH).

Dosing Protocol for Research Purposes

• 1 mg injected subcutaneously at night before bed (but at least 90 minutes after your last meal), and 1 mg injected subcutaneously upon waking up in the morning (ideally before fasted cardio or exercising). 
• If you’re going to inject Tesamorelin only once per day, inject it at night as recommended above.
• For Female, a once-a-day injection of 1 mg of Tesamorelin works wonders for improving polyphasic sleep and night-time growth hormone production.
• Tesamorelin on a “five day on, two days off” cycle and injects 1 mg subcutaneously in the morning while fasted before cardio.

Overview

Tesamorelin is a growth hormone-releasing hormone (GHRH) analogue consisting of standard GHRH to which an additional trans-3-hexanoic acid group has been added. Produced by Theratechnologies of Canada, Tesamorelin became the newest drug to be approved by the FDA for use in HIV-associated lipodystrophy in 2010. The peptide has also been investigated for its ability to improve peripheral nerve regeneration and as a potential intervention for mild cognitive impairment (MCI), the precursor to dementia.

Structure

Tesamorelin Research

As a GHRH analogue, Tesamorelin has all of the same effects as GHRH and GHRH analogues like sermorelin, GRF (1-29), CJC-1295, etc. The addition of trans-3-hexanoic acid to Tesamorelin makes it more stable in human plasma and thus increases its half-life. Despite this increase in half-life, Tesamorelin, like CJC-1295, preserves the physiological action of GHRH and thus has fewer side effects than similar molecules that obliterate normal pulsatile growth hormone (GH) release.

Tesamorelin and Lypodystrophy

The primary use for Tesamorelin is in the treatment of HIV-associated lipodystrophy, which arises both as a consequence of HIV infection and as a side effect of antiretroviral therapy. In lipodystrophy, fat accumulates excessively both in the abdomen and in other areas of the body. The physiologic mechanism responsible for

this is not clearly understood, but it is thought that commonly used protease inhibitors play a large role in the pathogenesis of lipodystrophy.

Patients suffering from lipodystrophy initially had diet, exercise, and a handful of ineffective medications to rely on for treatment. If those did not work, surgery was a last-ditch, often ineffective, and frequently complicated solution. In 2010, however, the FDA approved Tesamorelin specifically for the treatment of HIV-associated lipodystrophy. The drug has been found to reduce adiposity by nearly 20% in this population. Research suggests that Tesamorelin is approximately 4 times more effective in reducing adiposity than all of the other available therapies combined.

Tesamorelin Investigated in Cardiac Disease

People with HIV are at increased risk of developing cardiovascular disease (CVD), in part due to abnormal fat deposition and in part due to the actions of antiretroviral drugs themselves. Prevention of CVD in HIV-positive individuals is considered to be the most important medical intervention for long-term well-being, after highly active antiretroviral therapy (HAART) of course. Until recently, statins have been the cornerstone of medical management in this population.

Research shows that Tesamorelin, in addition to decreasing lipodystrophy, also reduces triglyceride levels, total cholesterol levels, and non-HDL-C levels in HIV-positive patients. A 15% reduction in visceral adipose tissue by Tesamorelin correlates with a 50 mg decrease in triglyceride levels.

It is worth noting that ectopic fat deposition, as seen in lipodystrophy, is associated with inflammation. Inflammation of any kind is a risk factor for CVD. Visceral adipose tissue, liver fat, and epicardial fat are all independently associated with an increased risk of CVD. By reducing ectopic fat deposition, Tesamorelin directly decreases inflammation and an individual’s risk for CVD.

Growth Hormone Deficiency and HIV

Recent evidence suggests that HAART is associated with a number of endocrine and metabolic problems, including growth hormone (GH) deficiency. It appears that the pituitary gland is altered in HIV infection and, as a consequence, approximately one-third of patients with HIV who are taking HAART have GH deficiency.

This may, to some extent, explain why lipodystrophy is so common in individuals with HIV and also why Tesamorelin is such an effective treatment. Tesamorelin is a safer and more effective way to raise GH levels than the administration of exogenous GH, particularly in HIV-positive individuals.

Tesamorelin for Peripheral Nerve Damage

Peripheral nerve damage can be a consequence of injury, diabetes, or even surgical interventions. It often results in debilitating problems with both motor and sensory function in the affected area, but there is little that can be done to correct the problem because nerve cells are notoriously difficult to regenerate. Research, however, suggests that therapies based on growth hormone manipulation may improve peripheral nerve injury and increase both the rate and extent of healing. Tesamorelin is currently the leading candidate for such intervention, in part because it already has FDA approval.

Tesamorelin Investigated in Dementia

There is no evidence to suggest that GHRH analogues, like Tesamorelin, are effective in enhancing cognition in patients suffering from the early stages of dementia. A large, randomized, double-blind, placebo-controlled study at the University of Washington School of Medicine, carried out over twenty weeks, suggests that Tesamorelin and other GHRH analogues may impact dementia by increasing gamma-aminobutyric acid(GABA) levels in the brain and by decreasing myo-inositol (MI) levels. These findings open up a pathway for using Tesamorelin in the treatment of dementia, but also suggest new areas for scientists to explore as they look for a cure or a preventative.

Tesamorelin improves both executive function and verbal memory in patients suffering from mild cognitive impairment. Source: PubMed

Tesamorelin Research

Because it is FDA approved for use in humans, Tesamorelin is an attractive peptide for ongoing clinical research. It is currently under review for its ability to reduce cardiovascular disease in HIV, improve healing of peripheral nerves following injury, and slow the progression of dementia. Clinical trials are already underway in several different areas.

Tesamorelin exhibits minimal side effects, low oral and excellent subcutaneous bioavailability in mice. Per kg dosage in mice does not scale to humans. 

“Tesamorelin cycle”: Use the peptide for no longer than 60 days in a row before taking a week-long break to cycle off.

And with respect to expectations, it takes roughly 4-6 weeks for noticeable changes in body composition (i.e. increase in lean muscle mass, decrease in visceral body fat, etc.).

About The Author

The above literature was researched, edited and organized by Dr. Logan, M.D. Dr. Logan holds a doctorate degree from Case Western Reserve University School of Medicine and a B.S. in molecular biology.

Referenced Citations

1. Clinical Review Report: Tesamorelin (Egrifta). Ottawa (ON): Canadian Agency for Drugs and Technologies in Health, 2016. 
2. A. Mangili, J. Falutz, J.-C. Mamputu, M. Stepanians, and B. Hayward, “Predictors of Treatment Response to Tesamorelin, a Growth Hormone-Releasing Factor Analog, in HIV-Infected Patients with Excess Abdominal Fat,” PloS One, vol. 10, no. 10, p. e0140358, 2015. [PubMed] 
3. J. Falutz et al., “Metabolic effects of a growth hormone-releasing factor in patients with HIV,” N. Engl.J. Med., vol. 357, no. 23, pp. 2359–2370, Dec. 2007. 
4. T. L. Stanley et al., “Reduction in visceral adiposity is associated with an improved metabolic profile in HIV-infected patients receiving Tesamorelin,” Clin. Infect. Dis. Off. Publ. Infect. Dis. Soc. Am., vol. 54,no. 11, pp. 1642–1651, Jun. 2012. [PubMed] 
5. V. Rochira and G. Guaraldi, “Growth hormone deficiency and human immunodeficiency virus,” Best Pract. Res. Clin. Endocrinol. Metab., vol. 31, no. 1, pp. 91–111, 2017. [PubMed] 
6. S. H. Tuffaha et al., “Therapeutic augmentation of the growth hormone axis to improve outcomes following peripheral nerve injury,” Expert Opin. Ther. Targets, vol. 20, no. 10, pp. 1259–1265, Oct. 2016. [PubMed]
7. S. D. Friedman et al., “Growth hormone-releasing hormone effects on brain γ-aminobutyric acid levels in mild cognitive impairment and healthy aging,” JAMA Neurol., vol. 70, no. 7, pp. 883–890, Jul. 2013.[PubMed]