Tesamorelin

Tesamorelin is a synthetic growth hormone releasing hormone (GHRH) analogue that incorporates standard GHRH with an added trans-3-hexanoic acid group. Developed by Theratechnologies in Canada, Tesamorelin gained FDA approval as the latest drug for managing HIV-associated lipodystrophy in 2010. Additionally, this peptide has been under investigation for its potential to enhance peripheral nerve regeneration and as a potential intervention for mild cognitive impairment (MCI), which is considered a precursor to dementia.

Tesamorelin, being a GHRH analogue, shares all the effects of GHRH and other analogues like sermorelin, GRF (1-29), CJC-1295, and so on. The incorporation of trans-3-hexanoic acid into tesamorelin enhances its stability in human plasma, leading to a prolonged half-life. Despite this extended half-life, tesamorelin, much like CJC-1295, retains the physiological action of GHRH, resulting in fewer side effects compared to similar molecules that disrupt the normal pulsatile release of growth hormone (GH).

Tesamorelin and Lypodystrophy

Tesamorelin finds its primary use in treating HIV-associated lipodystrophy, a condition that arises from HIV infection and as a side effect of antiretroviral therapy. Lipodystrophy leads to excessive fat accumulation in both the abdomen and other areas of the body. While the precise physiological mechanism behind it remains unclear, commonly used protease inhibitors are believed to play a significant role in its development[1].

Previously, patients dealing with lipodystrophy had limited treatment options, relying on diet, exercise, and ineffective medications. Surgery was a last-resort option, often with limited success and potential complications. However, in 2010, the FDA approved tesamorelin specifically for HIV-associated lipodystrophy. This drug has been shown to reduce adiposity by nearly 20% in affected individuals[1]. Remarkably, research suggests that tesamorelin is approximately four times more effective in reducing adiposity compared to all other available therapies combined[2].

Tesamorelin Investigated in Cardiac Disease

Individuals living with HIV face an increased risk of cardiovascular disease (CVD) due to abnormal fat distribution and the effects of antiretroviral drugs. As a crucial step in maintaining long-term well-being after highly active antiretroviral therapy (HAART), preventing CVD is paramount for HIV-positive individuals. Traditionally, statins have been the primary medical approach for managing this risk.

However, recent research has shed light on tesamorelin’s potential benefits beyond reducing lipodystrophy. Studies have revealed that tesamorelin not only decreases lipodystrophy but also leads to notable reductions in triglyceride levels, total cholesterol levels, and non-HDL-C levels in HIV-positive patients. In fact, a 15% reduction in visceral adipose tissue achieved through tesamorelin treatment is associated with a significant 50 mg decrease in triglyceride levels[3], [4]. These findings highlight the promising role of tesamorelin in managing CVD risk and improving the overall health of people living with HIV.

Changes in triglyceride levels of HIV-positive patients who respond to tesamorelin.
Source: PubMed

It’s worth to emphasize that the accumulation of ectopic fat, as observed in lipodystrophy, is linked to inflammation, which is a known risk factor for cardiovascular disease (CVD). Various types of fat deposits, such as visceral adipose tissue, liver fat, and epicardial fat, are each independently associated with an elevated risk of CVD. Through its ability to reduce ectopic fat deposition, tesamorelin directly mitigates inflammation and lowers an individual’s risk for cardiovascular disease (CVD).

Growth Hormone Deficiency and HIV

New evidence indicates that Highly Active Antiretroviral Therapy (HAART) is associated with various endocrine and metabolic issues, including growth hormone (GH) deficiency. HIV infection seems to alter the pituitary gland, leading to approximately one third of HAART-treated patients with HIV experiencing GH deficiency[5]. This deficiency may partly explain the prevalence of lipodystrophy in HIV-positive individuals and underscores the effectiveness of tesamorelin as a treatment. Tesamorelin is a safer and more efficient approach to elevate GH levels compared to administering exogenous GH, especially in those with HIV.

Tesamorelin for Peripheral Nerve Damage

Peripheral nerve damage can arise from various causes, such as injury, diabetes, or surgical procedures. Unfortunately, nerve cell regeneration is notoriously challenging, leading to debilitating issues with motor and sensory functions in the affected region. As a result, effective treatments for peripheral nerve injury have been limited.

However, recent research offers hope, indicating that growth hormone manipulation therapies might hold the key to improving peripheral nerve injury and enhancing the speed and extent of healing[6]. Among the potential interventions, tesamorelin stands out as the leading candidate, benefiting from its existing FDA approval and demonstrating promise in addressing this critical medical challenge.

Tesamorelin Investigated in Dementia

New evidence indicates that GHRH analogues, such as tesamorelin, show promise in improving cognition among patients in the early stages of dementia. A significant, twenty-week-long, randomized, double-blind, placebo-controlled study conducted at the University of Washington School of Medicine suggests that tesamorelin and other GHRH analogues may influence dementia by increasing gamma-aminobutyric acid (GABA) levels in the brain while simultaneously decreasing myo-inositol (MI) levels[7]. These findings not only pave the way for using tesamorelin in dementia treatment but also offer fresh avenues for scientific exploration in the search for a cure or preventive measures.

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

Tesamorelin holds significant appeal for ongoing clinical research due to its FDA approval for human use. It is currently being investigated for its potential in reducing cardiovascular disease in HIV patients, enhancing healing of peripheral nerves after injuries, and slowing the progression of dementia. Numerous clinical trials are already in progress across different areas.

Moreover, Tesamorelin has demonstrated minimal side effects and excellent subcutaneous bioavailability in mice, making it an attractive option for further investigation. However, it is essential to note that the dosage in mice does not directly scale to humans. At Peptide Shop, Tesamorelin is exclusively available for educational and scientific research purposes and is not intended for human consumption. Only licensed researchers should acquire Tesamorelin.

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.

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. [NEJM]
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]

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