|Drug class||Growth-hormone-releasing hormone (GHRH)|
|Main uses||HIV-associated lipodystrophy|
|Side effects||Joint pain, redness at the site of injection, leg swelling|
|Typical dose||2mg OD|
|Elimination half-life||26–38 min|
|Chemical and physical data|
|Molar mass||5135.86 g·mol−1|
|3D model (JSmol)|
Tesamorelin, sold under the brand name Egrifta, is a medication used to treat HIV-associated lipodystrophy. Specifically it is used for excess abdominal fat. It is given by injection under the skin.
Common side effects include joint pain, redness at the site of injection, and leg swelling. Other side effects may include allergic reactions and cancer. Use in pregnancy may harm the baby. It is a manufactured form of growth-hormone-releasing hormone (GHRH).
It is given at a dose of 2 mg once per day.
Tesamorelin therapy may cause glucose intolerance and increase the risk of type 2-diabetes, so it is contraindicated in pregnancy. It is also contraindicated in pregnancy (category X) because it may cause harm to fetus. It is also contraindicated in patients affected by hypothalamic-pituitary axis disruption due to pituitary gland tumor, head irradiation and hypopituitarism.
Mechanism of action
Tesamorelin is the N-terminally modified compound based on 44 amino acids sequence of human GHRH. This modified synthetic form is more potent and stable than the natural peptide. It is also more resistant to cleavage by the dipeptidyl aminopeptidase than human GHRH. It stimulates the synthesis and release of endogenous GH, with an increase in level of insulin-like growth factor (IGF-1). The released GH then binds with the receptors present on various body organs and regulates the body composition. This regulation is mainly because of the combination 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.
It is produced and developed by Theratechnologies, Inc. of Canada. The drug is a synthetic peptide consisting of all 44 amino acids of human GHRH with the addition of a trans-3-hexenoic acid group.
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