Tesamorelin is a synthetic polypeptide comprised of 44 amino acids similar to growth hormone-releasing hormone. The N-terminus of the molecule has been changed compared to growth hormone-releasing hormone (GHRH), which is hypothesized to lead to enhanced stability and pharmacokinetics. Tesamorelin also goes by its commercial (brand) name, Egrifta, or TH9507.
Tesamorelin Peptide Background
Highly active antiretroviral therapy (HAART) was developed for HIV research models in the mid-1990s and is now the standard treatment for HIV. Soon after, specialists speculated that although this option appeared to lower the HIV-related death rate drastically, it led to lipodystrophy in the researched subjects.
Numerous investigations have purported that HIV models with lipodystrophy may have abnormally low growth hormone levels. Experts hypothesized that increasing natural levels of growth hormones might improve fat oxidation and lower cholesterol. This led to research on the growth hormone axis and its regulation of fat storage, ultimately leading to the discovery of Tesamorelin.
What is Lipodystrophy?
Lipodystrophy refers to the abnormal accumulation and distribution of lipids. Acquired lipodystrophy is when it occurs after birth rather than at birth. A prime example of a disease that might trigger this condition is HIV.
Changes in insulin resistance, excessive lipid buildup, and endothelial dysfunction are hallmarks of HIV-induced lipodystrophy, and they may be attributable to antiretroviral treatment.
Tesamorelin Peptide: Mechanism of Action
Studies suggest that Tesamorelin may stimulate growth hormone synthesis and secretion by binding to and activating anterior pituitary growth hormone-releasing hormone (GHRH) receptors. Insulin-like growth factor-1 (IGF-1) production is stimulated by growth hormones when they act on many cells throughout the body, including hepatocytes. Analogous to G.H., IGF-1 is hypothesized to promote growth and inhibit programmed cell death, glucose reduction, and lipolysis.
Low levels of G.H. and IGF-1 are associated with lipodystrophy in HIV subjects. Research suggests this may be adjusted with Tesamorelin presentation, allowing for better control of lipid metabolism and buildup in the body.
As suggested before, the N-terminus of the molecule is changed in Tesamorelin, compared to the native GHRH. Because of this, unlike natural GHRH, the peptide is very stable and resistant to enzyme deactivation.
Tesamorelin Peptide Properties
Investigations purport that Tesamorelin may be commonly utilized in the context of lipodystrophy, notably in reducing excess fat in the abdominal area in HIV-infected research models. Recent research suggests that the peptide may also help treat NAFLD, which is common in HIV models.
Tesamorelin Peptide and Lipodystrophic HIV
The current research included two 26-week-long phase III investigations with 806 test subjects. HIV research models presented with antiretroviral treatment and having significant abdominal obesity were enrolled in this research. Subjects were randomly assigned to receive a placebo or Tesamorelin every other week for 26 weeks. After this length, the Tesamorelin research models were again randomly separated into two groups. Half remained with Tesamorelin's presentation, and professionals gave the other half a placebo for another 26 weeks.
The experiment's findings implied that visceral adipose tissue levels appeared to be reduced by at least 15.4% in Tesamorelin subjects by week 26. In addition, triglyceride and cholesterol levels seemed much lower than they had been after receiving the placebo. In week 52, no change was seen in the subjects who remained to receive peptide presentation.
This research suggested that Tesamorelin presentations may have resulted in visceral fat loss for up to 52 weeks. This suggests that Tesamorelin may otherwise be highly useful and well-tolerated in animal models.
Tesamorelin Peptide and NAFLD
Studies suggest that nearly 40% of HIV research models also suffer from non-alcoholic fatty liver disease (NAFLD), making it one of the most prevalent co-occurring disorders.
Researchers chose sixty-one HIV-positive male and female subjects with a high hepatic fat fraction (HFF) for inclusion in this research. These models were given Tesamorelin or a placebo for a year. Specialists tracked the trial's endpoint HFF rate.
After 12 months, experts theorized that 35% of research models presented with Tesamorelin appeared to exhibit a decrease in HFF rate by less than 5% compared to just 4% in subjects receiving a placebo. There appeared to be no distinction in the glucose levels.
Tesamorelin Peptide and Diabetes
One of the primary goals of this research was to determine whether Tesamorelin had any effect on insulin sensitivity.
Fifty-three research models with Type II diabetes were recruited in this 12-week randomized experiment. Subjects were randomly assigned to receive either a sugar pill (placebo) or Tesamorelin.
After 12 weeks, the concentration of fasting glucose, glycosylated hemoglobin, and diabetes control was assessed. The findings suggested that neither of these measures appeared to decrease noticeably. Researchers speculated that the outcomes seemed similar across all three research groups. Therefore, this research suggested that Tesamorelin may be less effective than other GHRH peptides in modifying insulin sensitivity and managing diabetes.
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