tesamorelin

Action and Spectrum

Actions and spectrum: 

tesamorelin is a synthetic analog of the human growth hormone-releasing hormone (GHRH) used to treat human immunodeficiency virus (HIV)-associated lipodystrophy. tesamorelin stimulates the release of growth hormone from the pituitary gland, increasing insulin-like growth factor-1 (IGF-1) levels.

The resulting increase in IGF-1 levels can improve body composition, mainly by reducing visceral adipose tissue (VAT) in individuals with HIV-associated lipodystrophy. tesamorelin is administered by subcutaneous injection. 

Drug Interaction

Adverse Reaction

Frequency defined:  

>10% 

Arthralgia (13.3%)  

1-10% 

Injection site reactions (up to 8.5%) 

Myalgia (5.5%) 

Nausea (4.4%) 

Rash (3.7%) 

Pruritus (2.4%) 

Dyspepsia (1.7%) 

Increased CPK (1.5%) 

Joint stiffness/swelling (1.1-1.5%) 

Muscle spasms (1.1%) 

Extremity pain (6.1%) 

Paresthesia (4.8%) 

Hypoesthesia (4.2%) 

Vomiting (2.6%) 

Depression (2%) 

Musculoskeletal pain and stiffness (1.7-1.8%) 

Carpal tunnel syndrome (1.5%) 

Hypertension (1.3%) 

<1% 

Anemia 

Mental status changes 

Trigeminal neuralgia 

Upper respiratory tract infection 

Abdominal abscess 

Sepsis 

Cerebellar syndrome 

Viral bronchitis 

Black Box Warning

Black Box Warning  

tesamorelin is used to reduce excess abdominal fat in HIV-infected patients with lipodystrophy. It is not indicated for weight loss management, and its safety and efficacy in patients with liver, kidney, or cardiac disease have not been established. 

Contraindication / Caution

Contraindication/Caution 

Contraindication 

tesamorelin is contraindicated in patients with a known hypersensitivity to tesamorelin or any of its components. It is also contraindicated for patients with active malignancy (cancer).  

Caution 

• Hypersensitivity: tesamorelin should not be used in patients who are hypersensitive to the medication. 
• Increased risk of cancer: There have been reports of malignancies in animals treated with tesamorelin. Therefore, tesamorelin should be used cautiously in patients with a history of cancer. 
• Hyperglycemia: tesamorelin may cause hyperglycemia, and therefore, in patients with a history of diabetes mellitus, it should be used with caution. 
• Fluid retention: tesamorelin may cause fluid retention, and therefore, in patients with a history of heart failure or other conditions, it should be used with caution that it can cause fluid retention. 
• Increased risk of cardiovascular events: tesamorelin may increase the risk of heart attack or stroke. Therefore, in patients with a history of cardiovascular disease, it should be used with caution.

Comorbidities 

• Diabetes mellitus 
• Increased risk of cardiovascular disease 
• Hypersensitivity to tesamorelin or any of its components 
• Increased risk of malignancy, particularly growth hormone-sensitive cancers 
• History of pituitary or hypothalamic disease or surgery 
• Pregnant or breastfeeding women should not use tesamorelin 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category X 

Lactation: not recommeded as it is excreted in milk  

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology 

tesamorelin is a synthetic analog of the human growth hormone-releasing hormone (GHRH). It stimulates the release of growth hormone (GH) from the pituitary gland by binding to the GHRH receptor on the somatotroph cells in the anterior pituitary gland. tesamorelin has a similar structure to naturally occurring GHRH, but it is more potent and has a longer half-life. 

tesamorelin is rapidly absorbed after subcutaneous injection and has a peak plasma concentration at approximately 30 minutes. The drug gets metabolized in the liver and eliminated mainly in the urine. The pharmacological effects of tesamorelin are primarily due to the release of GH, which stimulates insulin-like growth factor-1 (IGF-1) production in the liver and other tissues.

The increased levels of IGF-1 are responsible for the anabolic effects of GH, such as increased muscle mass and bone density. tesamorelin has also been shown to improve cognitive function and reduce abdominal fat in patients with HIV-associated lipodystrophy.  

Pharmacodynamics 

tesamorelin is a synthetic analog of growth hormone-releasing hormone (GHRH) that stimulates the release of growth hormone (GH) from the pituitary gland. It does this by binding to the GHRH receptor on somatotroph cells in the anterior pituitary gland, which stimulates the production and release of GH. 

Unlike other GHRH analogs, tesamorelin is selective for growth hormone release and does not affect other hormones, such as prolactin or cortisol. The exact mechanism by which tesamorelin improves this condition has yet to be fully understood. But it is related to increased insulin-like growth factor-1 (IGF-1), a hormone that regulates metabolism and body composition.  

Pharmacokinetics 

tesamorelin is administered by subcutaneous injection. After administration, it is rapidly absorbed with a bioavailability of approximately 92%. The maximum plasma concentration is achieved within 30 minutes to 3 hours after injection. The elimination half-life is about 30 minutes. The drug is mainly cleared from the body by the kidneys, and less than 2% is excreted in the feces. There are no known active metabolites of tesamorelin. 

Adminstartion

Administration 

tesamorelin is given as a subcutaneous injection (under the skin) once daily, preferably at the same time each day. It is available as a lyophilized powder that should be diluted with sterile water for injection before use.

The injection site should be rotated to different body areas to avoid local irritation. The medication should be used as directed by a healthcare provider with experience treating HIV-associated lipodystrophy. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: tesamorelin 

Pronounced: [tes-a-moe-rel-in]  

Why do we use tesamorelin? 

tesamorelin is a synthetic peptide used as a prescription medicine to reduce excess abdominal fat in HIV-infected patients with lipodystrophy. Lipodystrophy is a condition in which a person experiences changes in the distribution of body fat, which can lead to the accumulation of abdominal fat.

tesamorelin is administered by subcutaneous injection once daily and is typically used as a part of a comprehensive treatment plan that includes regular exercise and a healthy diet. It is not intended for weight loss in individuals who do not have lipodystrophy associated with HIV.