Tesamorelin

Characteristics

How does Tesamorelin work?

Tesamorelin is a synthetic growth hormone-releasing hormone (GHRH) analog that has been the subject of extensive research in the field of endocrinology and metabolism. This peptide’s primary mechanism of action involves binding to and activating the growth hormone-releasing hormone receptor (GHRHR) in the anterior pituitary gland. This activation stimulates the synthesis and pulsatile release of endogenous growth hormone (GH), which in turn promotes the production of insulin-like growth factor-1 (IGF-1) in the liver and other tissues.

Research

• Visceral Adipose Tissue (VAT) Reduction: Clinical studies have shown that tesamorelin can significantly reduce VAT in individuals with HIV-associated lipodystrophy and in obese individuals without HIV. This reduction in VAT has been associated with improvements in metabolic health markers.
• Insulin Sensitivity: Investigations have indicated that tesamorelin treatment may improve insulin sensitivity in certain populations, including individuals with HIV-associated lipodystrophy and obese individuals without HIV.
• Cognitive Function: Some studies have explored tesamorelin’s potential effects on cognitive function in older adults with mild cognitive impairment (MCI). Preliminary findings suggest possible improvements in executive function, attention, and memory.
• Muscle Mass and Strength: Research has indicated that tesamorelin may increase muscle mass and strength in older adults and individuals with HIV-associated lipodystrophy.
• Bone Health: Studies have observed increases in bone mineral density (BMD) in individuals with HIV-associated lipodystrophy following tesamorelin treatment.

Side Effects

• Injection site reactions
• Edema
• Arthralgia
• Hypersensitivity reactions

Less frequent side effects may include headache, dizziness, and gastrointestinal disturbances. In rare cases, tesamorelin may cause carpal tunnel syndrome or increase the risk of malignancy.

Summary

References

1. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012.
2. Dhillon S. Tesamorelin: a review of its use in the management of HIV-associated lipodystrophy. Drugs. 2011.
3. Fourman LT, Billingsley JM, Agyapong G, Ho Sui SJ, Feldpausch MN, Purdy J, Zheng I, Pan CS, Corey KE, Torriani M, Kleiner DE, Hadigan CM, Stanley TL, Chung RT, Grinspoon SK. Effects of tesamorelin on hepatic transcriptomic signatures in HIV-associated NAFLD. JCI Insight. 2020.
4. Spooner LM, Olin JL. Tesamorelin: a growth hormone-releasing factor analogue for HIV-associated lipodystrophy. Ann Pharmacother. 2012.
5. Clinical Review Report: Tesamorelin (Egrifta) [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2016.
6. Lake JE, La K, Erlandson KM, Adrian S, Yenokyan G, Scherzinger A, Dubé MP, Stanley T, Grinspoon S, Falutz J, Mamputu JC, Marsolais C, McComsey GA, Brown TT. Tesamorelin improves fat quality independent of changes in fat quantity. AIDS. 2021.
7. Pharmacoeconomic Review Report: Tesamorelin (Egrifta) [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2016.
8. Grunfeld C, Dritselis A, Kirkpatrick P. Tesamorelin. Nat Rev Drug Discov. 2011.
9. Wang Y, Tomlinson B. Tesamorelin, a human growth hormone releasing factor analogue. Expert Opin Investig Drugs. 2009.
10. Tomlinson B. Drug evaluation: tesamorelin, a synthetic human growth hormone releasing factor. Curr Opin Investig Drugs. 2006.

Certificate of Analysis (COA)

Resource

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