Peptide Tesamorelin is a synthetic form of Growth-hormone-releasing hormone (GHRH), consisting of all 44 amino acids of human GHRH with the addition of a trans-3-hexenoic acid group (the N-terminally modified compound based on GHRH). This modified synthetic form is more potent and stable than the natural endogenous peptide Growth-hormone-releasing hormone. Tesamorelin is also more resistant to cleavage by the dipeptidyl aminopeptidase than human GHRH.
Growth hormone–releasing hormone (GHRH)
Growth hormone–releasing hormone (GHRH; somatocrinin) is a 44-amino acid endogenous peptide hormone, released from neurosecretory nerve terminals of these arcuate neurons in a pulsatile manner. Then is GHRH carried by the hypothalamo-hypophyseal portal system to the anterior pituitary gland, where binds to the growth hormone-releasing hormone receptors and stimulates growth hormone secretion by the pituitary gland.
Mechanism of action of Tesamorelin
Tesamorelin acts similarly if its natural analogue GHRH: In the anterior pituitary gland it binds to the growth hormone-releasing hormone receptors (GHRHR), what triggers the production of Growth hormone (GH) by the pituitary gland. Growth hormone then brings some of its effects by binding to the receptors on target cells on various body organs in the body, however major target organ of Growth hormone is liver where GH stimulates production of IGF-1 (insulin-like growth factor 1).
Growth hormone production is associated with the regulation of many important processes and functions in the body, especially with the regulation of anabolic and lipolytic mechanisms. However, it has been found that the main mechanisms by which Tesamorelin reduces body fat mass are lipolysis followed by reduction in triglycerides level. Lipolysis is the process by which fats are broken down in the body, the metabolic pathway through which lipid triglycerides are hydrolyzed into a glycerol and three fatty acids.
Clinical trials and Tesamorelin use
Tesamorelin is used in the treatment of HIV-associated lipodystrophy, to reduce excess fat around the stomach, that is caused by taking HIV medications. (HIV-associated lipodystrophy is a syndrome that occurs in HIV-infected patients who are being treated with antiretroviral medications.) Performed clinical studies have demostrated that Tesamorelin significantly reduces abdominal fat with less side effects than HGH, although abdominal fat may return (depending on the individual) after discontinuation of Tesamorelin. Tesamorelin may cause harm to the unborn baby or cause birth defects, therefore it cannot be given to pregnant women.
Scientifically investigated possible benefits of Tesamorelin
- Significantly reduces abdominal fat
- Increases the secretion of growth hormone
- And it can also provide multiple and other positive effects associated with increased GH levels
Tesamorelin possible side-effects
- Pain, redness, itching, swelling or other irritation at the injection site
- Numbness or tingling in your hands or fingers
- Swelling in hands, ankles, or feet
- Pain or stiffness in your muscles or joints
- Tesaremolin is contraindicated in pregnancy (category X), it may cause harm to fetus
- May cause glucose intolerance, high blood sugar or may increase the risk of type 2-diabetes
Clinical use for the treatment of excess abdominal fat is 2 mg of Tesamorelin via subcutaneous injection once daily into the abdomen.