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Tesamorelin is a synthetic growth hormone-releasing hormone (GHRH) analog. It was based on the 44 amino acids sequence of GHRH and contains a trans-3 hexenoic group to protect it from enzymatic degradation. These modifications allow it to be more stable and have a longer half-life.
Just like Sermorelin, Ipamorelin or GHRP-2, Tesamorelin is considered a growth hormone secretagogue (GHS) which stimulates the secretion of GH and increases the level of insulin-like growth factor (IGF-1). The importance of IGF-1 is it tends to be lower in patients with obesity, diabetes and especially in those with lipodystrophy.
References:
- Sinha DK, Balasubramanian A, Tatem AJ, Rivera-Mirabal J, Yu J, Kovac J, Pastuszak AW, Lipshultz LI. Beyond the androgen receptor: the role of growth hormone secretagogues in the modern management of body composition in hypogonadal males. Transl Androl Urol. 2020 Mar;9(Suppl 2):S149-S159. doi: 10.21037/tau.2019.11.30. PMID: 32257855; PMCID: PMC7108996.
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What Is Tesamorelin?
Tesamorelin is a synthetic peptide used in medicine for a specific purpose. It is classified as a growth hormone-releasing hormone (GHRH) analog and is primarily used to stimulate the production and release of growth hormone (GH) from the pituitary gland. This hormone is crucial in various physiological processes, including growth, metabolism, and tissue repair.
This peptide is often used with HIV-associated lipodystrophy. According to some animal studies, it helps reduce excess abdominal fat, improving body composition and potentially enhancing insulin sensitivity.
Tesamorelin Structure
- Sequence (Single Letter): Unk-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu
- Molecular Formula: C223H370N72O69S
- Molecular Weight: 5195.908 g/mol
- PubChem CID: 44147413
- CAS Number: 901758-09-6
Tesamorelin and Lypodystrophy
Tesamorelin is a synthetic growth hormone-releasing factor that has shown promise in the treatment of lipodystrophy, particularly with HIV-associated lipodystrophy. Lipodystrophy refers to changes in body fat distribution and metabolism that can occur as a side effect of antiretroviral therapy for HIV.
Several animal studies have demonstrated the efficacy of tesamorelin in reducing central fat accumulation and improving visceral adiposity with HIV-associated lipodystrophy. Clinical trials have shown that tesamorelin injections can significantly decrease visceral abdominal fat.
Furthermore, tesamorelin has been found to have minimal effects on CYP3A, an enzyme involved in drug metabolism. This suggests that tesamorelin may not interfere with or be affected by medications metabolized by CYP3A.
The U.S. Food and Drug Administration (FDA) has approved tesamorelin for the treatment of lipodystrophy in patients with HIV. This approval was based on the positive results from clinical trials showcasing the effectiveness of tesamorelin in reducing visceral fat and improving lipid profiles.
Tesamorelin Investigated in Cardiac Disease
While tesamorelin has primarily been studied in treating lipodystrophy, there are also investigations into its potential effects on cardiac disease. However, it is important to note that long-term cardiovascular benefits have not been extensively studied.
One animal study found that lower visceral adipose tissue (VAT) and subcutaneous adipose tissue (SAT) density, which can be improved by tesamorelin, were associated with lower levels of adiponectin (a protein involved in regulating glucose and fatty acid metabolism) and increased cardiovascular disease risk.
Growth Hormone Deficiency and HIV
Growth hormone deficiency (GHD) can be a common complication in individuals with HIV infection. HIV-associated lipodystrophy often includes GHD as one of its components.
Based on the animal studies, GHRT can help increase lean body mass, decrease fat mass, and improve lipid profiles. It has also been associated with improvements in bone mineral density and quality of life.
However, it's important to note that the use of GHRT in HIV should be carefully evaluated and monitored, as there may be potential interactions with antiretroviral medications and other comorbidities.
Tesamorelin for Peripheral Nerve Damage
Tesamorelin has been investigated for its potential use in peripheral nerve damage. Several studies and clinical trials on animals have assessed its efficacy in enhancing axonal regeneration and improving functional outcomes following peripheral nerve injuries.
These studies suggest that GH-based therapies, such as tesamorelin, hold promise in the treatment of peripheral nerve injuries due to their multi-modal mechanism of action.
Tesamorelin Investigated in Dementia
Exciting new evidence has emerged regarding the potential benefits of GHRH analogues, including tesamorelin, in enhancing cognition in the early stages of dementia. A groundbreaking study conducted at the University of Washington School of Medicine shed light on the positive influence of tesamorelin and similar analogues on dementia by modulating specific brain chemicals.
In this comprehensive twenty-week-long study, researchers employed a rigorous methodology with randomized, double-blind, placebo-controlled design. The results pointed towards the intriguing role of tesamorelin in increasing levels of gamma-aminobutyric acid (GABA) while simultaneously lowering (MI) myo-inositol levels in the brain.
Please note that all the articles and product information provided on this website are intended for informational and educational purposes only.
The products offered on this platform are specifically designed for in-vitro studies, meaning they are conducted outside the body.
References:
- Bedimo R. Growth hormone and tesamorelin in the management of HIV-associated lipodystrophy. HIV AIDS (Auckl). 2011;3:69-79. doi: 10.2147/HIV.S14561. Epub 2011 Jul 10. PMID: 22096409; PMCID: PMC3218714.
- Bedimo R. Growth hormone and tesamorelin in the management of HIV-associated lipodystrophy. HIV AIDS (Auckl). 2011;3:69-79. doi: 10.2147/HIV.S14561. Epub 2011 Jul 10. PMID: 22096409; PMCID: PMC3218714.
- Patel A, Gandhi H, Upaganlawar A. Tesamorelin: A hope for ART-induced lipodystrophy. J Pharm Bioallied Sci. 2011 Apr;3(2):319-20. doi: 10.4103/0975-7406.80763. PMID: 21687371; PMCID: PMC3103937.
- Linda M Spooner, PharmD BCPS; Jacqueline L Olin, MS PharmD BCPS CPP CDE, “Tesamorelin A Growth Hormone-releasing Factor Analogue for HIV-associated Lipodystrophy”
- 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 Jul 15;35(9):1395-1402. doi: 10.1097/QAD.0000000000002897. PMID: 33756511; PMCID: PMC8243807.
- Stanley TL, Falutz J, Mamputu JC, Soulban G, Potvin D, Grinspoon SK. Effects of tesamorelin on inflammatory markers in HIV patients with excess abdominal fat: relationship with visceral adipose reduction. AIDS. 2011 Jun 19;25(10):1281-8. doi: 10.1097/QAD.0b013e328347f3f1. PMID: 21516030; PMCID: PMC3673013.
- Gilbreath KR, Nawaratna GI, Wickersham TA, Satterfield MC, Bazer FW, Wu G. Ruminal microbes of adult steers do not degrade extracellular L-citrulline and have a limited ability to metabolize extracellular L-glutamate1,2. J Anim Sci. 2019 Sep 3;97(9):3611-3616. doi: 10.1093/jas/skz227. PMID: 31269197; PMCID: PMC6735895.
- Lin J, Yang H, Kelly WK. Prostate cancer biomarker: a key field to explore. Asian J Androl. 2013 May;15(3):358-9. doi: 10.1038/aja.2013.1. Epub 2013 Feb 25. PMID: 23435472; PMCID: PMC3739636.
- Blavier L, Lazaryev A, Shi XH, Dorey FJ, Shackleford GM, DeClerck YA. Stromelysin-1 (MMP-3) is a target and a regulator of Wnt1-induced epithelial-mesenchymal transition (EMT). Cancer Biol Ther. 2010 Jul 15;10(2):198-208. doi: 10.4161/cbt.10.2.12193. Epub 2010 Jul 29. PMID: 20534975; PMCID: PMC3040898.
- Carvalho CR, Oliveira JM, Reis RL. Modern Trends for Peripheral Nerve Repair and Regeneration: Beyond the Hollow Nerve Guidance Conduit. Front Bioeng Biotechnol. 2019 Nov 22;7:337. doi: 10.3389/fbioe.2019.00337. PMID: 31824934; PMCID: PMC6882937.
- Jaimie T. Shores, MD, “Tesamorelin Therapy to Enhance Axonal Regeneration, Minimize Muscle Atrophy and Improve Functional Outcomes Following Peripheral Nerve Injury and Repair”
- “Phase II Trial of Tesamorelin for Cognition in Aging HIV-Infected Persons” - https://ichgcp.net/clinical-trials-registry/NCT02572323
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