In this article, we will do our best to provide an in-depth understanding of what Tesamorelin is, its functions, and its primary properties.
What Is Tesamorelin Peptide?
A growth hormone-releasing hormone (GHRH) is secreted by a brain region known as the hypothalamus. The hypothalamus creates a connection between the endocrine and neurological systems. This hormone stimulates the anterior pituitary gland to secrete growth hormone (GH), which in turn causes cell growth. [i]
Tesamorelin acetate is a synthetic peptide consisting of 44 amino acids and is similar to the growth hormone-releasing hormone (GHRH) in its structural makeup and may exhibit similar physiological effects. [ii]
Tesamorelin has a slightly changed N-terminal section of the amino acids responsible for the peptide's signature qualities compared to growth hormone-releasing hormone (GHRH). This change is intended to enhance the substance's stability and pharmacodynamics.
Tesamorelin Peptide: Mechanism of Action
In imitating the action of a naturally existing endogenous hormone, studies suggest Tesamorelin may also exert its influence on certain target areas. As a consequence of this, the action mechanism that Tesamorelin employs is rather particular.
Research suggests Tesamorelin may bind to and activate growth hormone-releasing hormone receptors (GHRHr) in the anterior pituitary gland. This binding may cause the somatotrophic cells in the pituitary gland to become stimulated and begin producing and secreting growth hormone (GH).
Adipocytes (cells that store fat), hepatocytes (cells that store liver), myocytes (cells that store muscle), and osteoblasts (cells that store bone) are the primary targets of the growth hormone (GH). [iii]
A negative feedback mechanism may be activated to prevent an excessive increase in serum growth hormone (GH) levels, which is considered to be done to keep the Tesamorelin-induced release of growth hormone (GH) within the parameters that have been established.
Findings imply Tesamorelin may maintain homeostatic coordination between the hypothalamus and pituitary gland because it may naturally cause the production of growth hormone (GH).
Tesamorelin Peptide Potential
Researchers speculate the basic objective of Tesamorelin may be to augment the growth hormone (GH) amounts in the blood. The other possible properties of Tesamorelin may occur as a natural byproduct.
Lipodystrophy is one of the most significant impacts of HIV mitigation practices and antiretroviral compounds. [iv] Either an abnormally large accumulation of fat, most notably the abdominal region or a reduction of the typical amount of body fat is meant by this term.
In clinical studies, subjects with HIV-associated lipodystrophy have been suggested to exhibit a significant decrease in their visceral adipose tissue levels (VAT) levels. Scientists hypothesize Tesamorelin may successfully reduce trunk fat, waist circumference, and waist-to-hip ratio, improving body composition measurements. In addition, Tesamorelin appeared to enhance body composition measures. Studies are still ongoing, and further research is necessary to validate any hypotheses. [v]
Tesamorelin has also been suggested to reduce the size of the carotid-intima media thickness (cIMT). As a result, studies suggest it may slow the development of atherosclerotic vascular disease in the carotid artery.
These potential properties might contribute to establishing a connection between Tesamorelin and a lower risk of developing cardiovascular issues.
Insulin-like growth factor 1 (IGF-1) levels in the blood of test subjects with lipodystrophy are significantly reduced. Research suggests Tesamorelin may kickstart the hepatocytes' insulin-like growth factor 1 (IGF-1) synthesis [vi]. IGF-7 is responsible for the growth process and suppresses the mechanism responsible for programmed cell death. It does this reportedly without affecting the levels of glucose in the blood.
Findings imply that Tesamorelin may accomplish the process of lipolysis, which may result in a decrease in the levels of cholesterol and triglycerides. Therefore, an improvement was suggested in lipid profiles in those subjects that were given Tesamorelin.
Researchers suggest further that Tesamorelin may possibly improve cognitive abilities in aging test models, which contributes to mitigating natural declination in brain functioning. Scientists hypothesize that Tesamorelin may reduce the amount of myoinositol (MI), an osmolyte responsible for the early start of Alzheimer's disease. [vii]
Tesamorelin vs. Ipamorelin
The peptides may be differentiated from one another based on the results of research studies. Studies suggest that even though both peptides may produce results that are, more or less, comparable, there are still variances in the structures and proposed mechanisms of action of the peptides.
Ipamorelin is constructed from five different amino acids. In addition to this, research suggests it may inhibit somatostatin, ending the negative feedback loop that was previously mentioned.
Tesamorelin vs. Sermorelin
Researchers speculate Tesamorelin may be superior to Sermorelin because it has a reported longer half-life and may increase the pulsatile release of growth hormone (GH) from somatotrophic cells. Sermorelin does not appear to possess these properties.
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References
[i] Shahid Z, Asuka E, Singh G. Physiology, Hypothalamus. [Updated 2023 May 1]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2023 Jan-. Available from: https://www.ncbi.nlm.nih.gov/books/NBK535380/
[ii] LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Tesamorelin. [Updated 2018 Oct 20]. Available from: https://www.ncbi.nlm.nih.gov/books/NBK548730/
[iii] Dehkhoda F, Lee CMM, Medina J, Brooks AJ. The Growth Hormone Receptor: Mechanism of Receptor Activation, Cell Signaling, and Physiological Aspects. Front Endocrinol (Lausanne). 2018 Feb 13;9:35. doi: 10.3389/fendo.2018.00035. PMID: 29487568; PMCID: PMC5816795.
[iv] Bedimo R. Growth hormone and tesamorelin in the management of HIV-associated lipodystrophy. HIV AIDS (Auckl). 2011;3:69-79. doi: 10.2147/HIV.S14561. Epub 2011 Jul 10. PMID: 22096409; PMCID: PMC3218714.
[v] 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.
[vi] Stanley TL, Chen CY, Branch KL, Makimura H, Grinspoon SK. Effects of a growth hormone-releasing hormone analog on endogenous GH pulsatility and insulin sensitivity in healthy men. J Clin Endocrinol Metab. 2011 Jan;96(1):150-8. doi: 10.1210/jc.2010-1587. Epub 2010 Oct 13. PMID: 20943777; PMCID: PMC3038486.
[vii] Friedman SD, Baker LD, Borson S, Jensen JE, Barsness SM, Craft S, Merriam GR, Otto RK, Novotny EJ, Vitiello MV. Growth hormone-releasing hormone effects on brain γ-aminobutyric acid levels in mild cognitive impairment and healthy aging. JAMA Neurol. 2013 Jul;70(7):883-90. doi: 10.1001/jamaneurol.2013.1425. PMID: 23689947; PMCID: PMC3764915.
