Tesamorelin

Tesamorelin Overview

Tesamorelin is a specialized synthetic analog of growth hormone-releasing hormone (GHRH) designed to mimic the action of the endogenous hormone produced by the hypothalamus. By binding to GHRH receptors in the anterior pituitary gland, it stimulates the natural, pulsatile secretion of growth hormone. Clinical data indicates that Tesamorelin administration can elevate IGF-1 levels by an average of 181 micrograms per liter.

Beyond its primary role in hormonal regulation, Tesamorelin is widely researched for its metabolic benefits, including the reduction of visceral adipose tissue and the lowering of triglyceride levels. It has also shown promise in neuroprotective studies, where it may enhance cognitive function in aging populations or those with mild cognitive impairment. Significantly, research suggests that Tesamorelin does not interfere with the natural regulation of other pituitary hormones, maintaining a focused impact on the growth hormone axis.

Tesamorelin Peptide Structure

The structural integrity of Tesamorelin is enhanced through strategic chemical modifications at both ends of the peptide chain. These adjustments improve its resistance to enzymatic degradation, specifically against dipeptidyl peptidase-4, thereby extending its biological half-life.

Chemical Identification: N-(trans-3-hexenoyl)-[Tyr1]hGHRF(1-44)NH2 acetate

Structure Solution Formula: C221H366N72O67S

Molecular Overview:

• N-Terminal Modification: Inclusion of a trans-3-hexenoyl group.
• C-Terminal Modification: Presence of an acetyl group for stability.
• Peptide Type: 44-amino acid synthetic peptide.

Tesamorelin Research

Lipodystrophy and Visceral Fat Reduction

Tesamorelin is extensively studied for its impact on lipodystrophy, a condition characterized by the abnormal distribution of body fat. In major Phase III trials involving over 800 participants, researchers observed a 15.4 percent reduction in visceral adipose tissue (VAT) over a 26-week period. This reduction in "deep" abdominal fat was accompanied by a notable decrease in circulating triglycerides and cholesterol, suggesting a significant improvement in metabolic health.

Hepatic Health and Liver Fat

Clinical investigations have also targeted non-alcoholic fatty liver disease (NAFLD) in immunodeficient subjects. In a 12-month study, 35 percent of participants receiving Tesamorelin saw a reduction in hepatic fat fraction (HFF) of at least 5 percent, compared to only 4 percent in the placebo group. This indicates that the peptide may play a role in reducing ectopic fat stores in the liver without negatively impacting glucose levels.

Muscle Composition and Density

Research utilizing CT imaging has demonstrated that Tesamorelin significantly influences muscle quality. In various muscle groups, including the paraspinal and psoas major muscles, Tesamorelin was associated with increased muscle density and size. Simultaneously, studies showed a decrease in intramuscular fat, highlighting the peptide's potential to improve overall body composition by shifting the ratio of fat to lean tissue.

Cognitive Enhancement and Neuroprotection

The "nootropic" potential of Tesamorelin is an emerging area of research. Studies on older adults with mild cognitive impairment suggest that by modulating the growth hormone axis, Tesamorelin may support cognitive health. Specifically, researchers are investigating its ability to improve the Global Deficit Score in individuals at high risk for neurodegenerative diseases like Alzheimer’s.

Comparative Research Outcomes

Research Area

Primary Biological Impact

Statistical Significance

Visceral Fat (VAT)

15.4% to 25% Reduction

High

IGF-1 Levels

Mean increase of 122% to 181 mcg/L

Significant

Muscle Density

Notable increase in muscle size

High

Liver Fat (HFF)

31% more effective than placebo

Moderate

Triglycerides

Measurable reduction in lipid levels

Significant

Glucose Levels

Minimal to no alteration

Neutral

Article Author

Scientific Journal Author

Reference Citations

1. 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]. https://www.ncbi.nlm.nih.gov/books/NBK548730/
2. Spooner, L. M., and Olin, J. L. (2012). Tesamorelin: a growth hormone-releasing factor analogue for HIV-associated lipodystrophy. The Annals of pharmacotherapy, 46(2), 240-247.
3. Stanley TL, et al. 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.
4. Ferdinandi ES, et al. Non-clinical pharmacology and safety evaluation of TH9507, a human growth hormone-releasing factor analogue. Basic Clin Pharmacol Toxicol. 2007 Jan;100(1):49-58.
5. Stanley, T. L., et al. (2019). Effects of tesamorelin on non-alcoholic fatty liver disease in HIV: a randomised, double-blind, multicentre trial. The lancet. HIV, 6(12), e821-e830.
6. Falutz J, et al. Effects of tesamorelin (TH9507) in human immunodeficiency virus-infected patients with excess abdominal fat. J Clin Endocrinol Metab. 2010 Sep;95(9):4291-304.
7. Tesamorelin Effects on Liver Fat and Histology in HIV. ClinicalTrials.gov Identifier: NCT02196831.
8. Phase II Trial of Tesamorelin for Cognition in Aging HIV-Infected Persons. ClinicalTrials.gov Identifier: NCT02572323.
9. Clemmons, D. R., et al. (2017). Safety and metabolic effects of tesamorelin in patients with type 2 diabetes. PloS one, 12(6), e0179538.
10. Adrian S, et al. The Growth Hormone Releasing Hormone Analogue, Tesamorelin, Decreases Muscle Fat and Increases Muscle Area. J Frailty Aging. 2019;8(3):154-159.
11. Sivakumar T, et al. Growth hormone axis treatments for HIV-associated lipodystrophy: a systematic review. HIV Med. 2011 Sep;12(8):453-62.

Storage

Storage Instructions

Tesamorelin is produced using a lyophilization (freeze-drying) process that ensures maximum molecular stability. In its lyophilized (powder) form, the product is stable for shipping at room temperature for approximately 3 to 4 months. Once reconstituted with bacteriostatic water, the peptide must be refrigerated at 2 to 8 degrees Celsius (36 to 46 degrees Fahrenheit). Reconstituted solutions should be used within 30 days.

Environmental Precautions

Peptides are sensitive to light and temperature fluctuations. For long-term storage (months to years), keep the lyophilized vials in a freezer at -80 degrees Celsius (-112 degrees Fahrenheit). Avoid frost-free freezers, as the constant temperature cycles can compromise the peptide's structural integrity.

Handling and Reconstitution

To prevent oxidation and contamination, allow the vial to reach room temperature before opening or injecting diluent. This prevents moisture from condensing inside the vial. When mixing, avoid aggressive shaking; instead, gently swirl the vial to ensure the powder is fully dissolved.