Tesamorelin (

INN Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...

) (trade name Egrifta SV) is a

synthetic Synthetic things are composed of multiple parts, often with the implication that they are artificial. In particular, 'synthetic' may refer to: Science * Synthetic chemical or compound, produced by the process of chemical synthesis * Synthetic o ...

form of growth-hormone-releasing hormone (GHRH) which is used in the treatment of

HIV-associated lipodystrophy HIV-associated lipodystrophy is a condition characterized by loss of subcutaneous fat associated with infection with HIV. Presentation HIV-associated lipodystrophy commonly presents with fat loss in face, buttocks, arms and legs. There is also ...

, approved initially in 2010. It is produced and developed by Theratechnologies, Inc. of Canada. The drug is a synthetic

peptide Peptides (, ) are short chains of amino acids linked by peptide bonds. Long chains of amino acids are called proteins. Chains of fewer than twenty amino acids are called oligopeptides, and include dipeptides, tripeptides, and tetrapeptides. A ...

consisting of all 44

amino acid Amino acids are organic compounds that contain both amino and carboxylic acid functional groups. Although hundreds of amino acids exist in nature, by far the most important are the alpha-amino acids, which comprise proteins. Only 22 alpha am ...

s of human GHRH with the addition of a ''trans''-3-hexenoic acid group.

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 Dipeptidyl peptidase is a type of enzyme classified under EC 3.4.14. Types include: * Cathepsin C, dipeptidyl peptidase-1 * Dipeptidyl-peptidase II * DPP3, dipeptidyl peptidase-3 * DPP4, Dipeptidyl peptidase-4 * DPP6, dipeptidyl peptidase-6 * DPP ...

than human GHRH. It stimulates the synthesis and release of endogenous GH, with an increase in level of insulin-like growth factor (

IGF-1 Insulin-like growth factor 1 (IGF-1), also called somatomedin C, is a hormone similar in molecular structure to insulin which plays an important role in childhood growth, and has anabolic effects in adults. IGF-1 is a protein that in humans is ...

). 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 Lipolysis is the metabolic pathway through which lipid triglycerides are hydrolyzed into a glycerol and free fatty acids. It is used to mobilize stored energy during fasting or exercise, and usually occurs in fat adipocytes. The most important ...

followed by reduction in triglycerides level.

Contraindication

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 Hypopituitarism is the decreased (''hypo'') secretion of one or more of the eight hormones normally produced by the pituitary gland at the base of the brain. If there is decreased secretion of one specific pituitary hormone, the condition is know ...

Adverse effects

Injection site

erythema Erythema (from the Greek , meaning red) is redness of the skin or mucous membranes, caused by hyperemia (increased blood flow) in superficial capillaries. It occurs with any skin injury, infection, or inflammation. Examples of erythema not assoc ...

, peripheral edema, injection site

pruritus Itch (also known as pruritus) is a sensation that causes the desire or reflex to scratch. Itch has resisted many attempts to be classified as any one type of sensory experience. Itch has many similarities to pain, and while both are unpleasant ...

and diarrhea.

References

Growth hormone secretagogues Growth hormone-releasing hormone receptor agonists HIV/AIDS Merck brands Peptides Recombinant proteins World Anti-Doping Agency prohibited substances {{systemic-hormonal-drug-stub

Mechanism of action

Contraindication

Adverse effects

See also

References