What is the connection between Tesamorelin and diabetes is the subject of today’s article. If you are interested in finding out the answer, then keep reading.
Tesamorelin is a synthetic polypeptide comprised of 44 amino acids similar to growth hormone-releasing hormone.
The N-terminus of the molecule has changed compared to growth hormone-releasing hormone (GHRH), which leads to enhanced stability and pharmacokinetics. Tesamorelin also goes by its commercial (brand) name, Egrifta, or TH9507.
History
Highly active antiretroviral therapy (HAART) was developed for HIV patients in the mid-1990s and is now the standard treatment for HIV. Soon after, specialists found that although this medication drastically lowered the HIV-related death rate, it led to lipodystrophy in the treated subjects.
Numerous investigations have shown that HIV models with lipodystrophy have abnormally low growth hormone levels. Also, Experts showed that increasing natural levels of growth hormones might improve fat oxidation and lower cholesterol. However, This led to research on the growth hormone axis and its regulation of fat storage, ultimately leading to the discovery of Tesamorelin.
Tesamorelin: A User’s Manual
Lipodystrophy refers to the abnormal accumulation and distribution of lipids. Acquired lipodystrophy describes 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.
The good news is that one may treat this illness and its prevalence reduced using various approaches. One such possibility is peptide therapy, including a peptide called Tesamorelin. The FDA authorized the synthetic peptide Tesamorelin in 2010 to treat HIV-related lipodystrophy.
Timeline of FDA Approval in the United States
A New Drug Application (NDA) was filed with the U.S. Food and Drug Administration (FDA) by Theratechnologies Inc. of Montreal, Quebec (Canada) in June 2009. Once the US FDA approved the application, the business continued with the medication manufacture and development. U.S. regulators gave the green light to Egrifta in November 2010, making it the first and sole therapy for HIV-related lipodystrophy.
How Does Tesamorelin Work?
Tesamorelin stimulates 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 stimulated by growth hormones when they act on many cells throughout the body, including hepatocytes.
Analogous to G.H., IGF-1 promotes growth and inhibits programmed cell death, glucose reduction, and lipolysis.
Low levels of G.H. and IGF-1 are associated with lipodystrophy in HIV subjects. This may adjusted with Tesamorelin therapy, allowing for better control of lipid metabolism and buildup in the body.
As indicated before, the N-terminus of the molecule changed in Tesamorelin, compared to the native GHRH. Because of this, unlike natural GHRH, the peptide is very stable and resistant to enzyme deactivation.
What’s Good About Tesamorelin?
Tesamorelin commonly utilized in treating lipodystrophy, notably in reducing the excess fat in the abdominal area in HIV-infected subjects. Recent research suggests that the peptide may also help treat NAFLD, which is common in HIV models.
Research
Lipodystrophy HIV Subjects
The current research included two 26-week-long phases III investigations with 806 test subjects.
806 HIV research models treated with antiretroviral treatment and having significant abdominal obesity enrolled in this research. Patients randomly assigned to receive Tesamorelin every other week for 26 weeks or a placebo. After this length, the Tesamorelin-treated patients again randomly separated into 2 groups. Half remained with Tesamorelin medication, and professionals gave the other half a placebo for another 26 weeks.
Visceral adipose tissue levels shown to reduced by at least 15.4% in Tesamorelin-treated subjects by week 26. In addition, triglyceride and cholesterol levels much lower than they had after receiving the placebo. Overall, body image also improved. In week 52, no change seen in the patients who remained to receive peptide therapy.
This research indicated that Tesamorelin resulted in visceral fat loss for up to 52 weeks, with no side effects identified in subjects. This suggests Tesamorelin is otherwise highly effective and well tolerated in animal models.
HIV Subjects And NAFLD
Nearly 40% of HIV patients 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. For a year, these models took Tesamorelin or a placebo with the same appearance. Specialists tracked the trial’s endpoint HFF rate.
After 12 months, experts noted that 35% of patients treated with Tesamorelin exhibited a decrease in HFF rate by less than 5% vs. just 4% of participants getting a placebo showed HFF reduction. There was no distinction in the glucose levels.
Tesamorelin might be a promising therapeutic medication for treating NAFLD in test subjects with HIV syndrome.
Tesamorelin for Diabetes
One of the primary goals of this research was to determine whether Tesamorelin had any effect on insulin sensitivity and if one may use it to aid in treating and controlling diabetes.
Fifty-three participants who had Type II diabetes participated in this 12-week randomized experiment. Subjects randomly assigned to receive either a sugar pill (placebo), or Tesamorelin.
After 12 weeks, the concentration of fasting glucose, glycosylated hemoglobin, and diabetes control assessed. Both of these measures didn’t decrease noticeably. The outcomes were similar across all three therapy groups. Therefore, this research showed that Tesamorelin is not as effective as other GHRH peptides in modifying insulin sensitivity and managing diabetes.
Results to Expect
Following some of the peptide’s documented adverse effects. Normal adverse reactions include:
- Muscle soreness and stiffness
- Hurtful limbs and aching joints
Some less prevalent adverse effects include:
- Headache
- Discomfort, burning, and tingling in all fingers
- Discomfort in the chest
- Weakness and dizziness
- Arrhythmia
- Nervousness, awkwardness, irritability
- Blurred eyesight and hammering in the ears
- Discomfort, nausea, and vomiting
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