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 accomm ...
; trade name Egrifta SV) is a
synthetic
Synthetic may refer to:
Science
* Synthetic biology
* Synthetic chemical or compound, produced by the process of chemical synthesis
* Synthetic elements, chemical elements that are not naturally found on Earth and therefore have to be created in ...
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 f ...
, 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. A polypeptide is a longer, continuous, unbranched peptide chain. Polypeptides that have a molecular mass of 10,000 Da or more are called proteins. Chains of fewer than twenty am ...
consisting of all 44
amino acid
Amino acids are organic compounds that contain both amino and carboxylic acid functional groups. Although over 500 amino acids exist in nature, by far the most important are the 22 α-amino acids incorporated into proteins. Only these 22 a ...
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 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. In the 1950s IGF-1 was called " sulfa ...
). 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 hydrolysis, hydrolyzed into a glycerol and free fatty acids. It is used to mobilize stored energy during fasting or exercise, and usually occurs in Adipose tissue, fat adip ...
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 (, ) 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 associated with pathology inc ...
, peripheral edema, injection site
pruritus
An itch (also known as pruritus) is a sensation that causes a strong desire or reflex to scratch. Itches have resisted many attempts to be classified as any one type of sensory experience. Itches have many similarities to pain, and while both ...
and diarrhea.
See also
*
List of growth hormone secretagogues
References
{{GH/IGF-1 axis signaling modulators
Growth hormone secretagogues
Growth hormone-releasing hormone receptor agonists
HIV/AIDS
Drugs developed by Merck
Peptides
Recombinant proteins
World Anti-Doping Agency prohibited substances