Tesamorelin 5mg

Tesamorelin — Synthetic GHRH Analog for Research in Lipodystrophy, Neurology, and Metabolic Health

Overview

Tesamorelin is a synthetic peptide that stimulates the natural secretion of human growth hormone (HGH) — a hormone critical for metabolism, body composition, and overall vitality.
Developed by Theratechnologies (Canada), Tesamorelin is a stabilized analog of growth hormone–releasing hormone (GHRH) with an added trans-3-hexenoic acid group that enhances its half-life and resistance to degradation in plasma.

The peptide received FDA approval in 2010 for the treatment of HIV-associated lipodystrophy — a condition involving abnormal fat distribution caused by both the infection and antiretroviral therapy.
Beyond this, Tesamorelin continues to be studied for its potential effects on nerve regeneration, cognitive decline, and metabolic balance.

Structure and Biochemical Properties

• Amino Acid Sequence: 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: 5195.9 g/mol

• CAS Number: 901758-09-6

• PubChem CID: 44147413

• Peptide Class: Synthetic GHRH analog

Mechanism of Action

Tesamorelin mimics the physiological effects of growth hormone–releasing hormone (GHRH).
By binding to GHRH receptors in the pituitary gland, it promotes natural pulsatile release of growth hormone (GH) — maintaining normal rhythm and minimizing side effects compared to direct GH administration.
The added trans-3-hexenoic acid group significantly improves peptide stability and half-life, extending biological activity.

Tesamorelin and HIV-Associated Lipodystrophy

Lipodystrophy, commonly seen in individuals with HIV, is characterized by excess visceral fat accumulation due to both viral infection and antiretroviral medications.
In clinical studies, Tesamorelin was shown to:

• Reduce visceral adipose tissue (VAT) by approximately 15–20%,

• Improve metabolic profiles and body composition,

• Outperform all other available therapies combined in reducing central adiposity.

FDA approval of Tesamorelin in 2010 marked a significant advancement for managing HIV-related metabolic complications, providing a non-surgical and physiological approach to visceral fat reduction.

Cardiovascular Research

HIV-positive patients face elevated cardiovascular risk due to abnormal fat storage and inflammation.
Clinical research shows that Tesamorelin not only reduces visceral fat but also:

• Lowers triglyceride levels,

• Decreases non-HDL cholesterol,

• Improves overall lipid metabolism.

A 15% reduction in visceral fat was associated with an average 50 mg/dL reduction in triglycerides, indicating a strong metabolic correlation.
By reducing ectopic fat and systemic inflammation, Tesamorelin may contribute to cardiovascular risk reduction in clinical populations under study.

Growth Hormone Deficiency in HIV

Endocrine complications of HIV and antiretroviral therapy (HAART) often include growth hormone deficiency.
Research indicates that approximately one-third of HIV patients on HAART exhibit low GH levels, which contributes to metabolic dysfunction and fat redistribution.
Tesamorelin offers a safer, more natural alternative to exogenous GH by stimulating the body’s own GH release while maintaining physiological secretion patterns.

Peripheral Nerve Regeneration

Nerve damage — whether from trauma, diabetes, or surgery — is notoriously difficult to repair due to poor neuronal regeneration.
Experimental studies suggest that growth hormone axis activation can enhance recovery of peripheral nerves.
Tesamorelin has emerged as a promising candidate for such research due to its established safety profile and neuroregenerative potential in animal and early-stage human studies.

Cognitive Function and Dementia Research

Recent clinical trials have explored Tesamorelin’s potential in mild cognitive impairment (MCI) and early dementia.
A 20-week double-blind, placebo-controlled study at the University of Washington demonstrated that GHRH analogs like Tesamorelin may improve brain GABA levels and reduce myo-inositol, suggesting neuroprotective and memory-supportive effects.
These findings open the door for continued research into Tesamorelin’s role in cognitive health and neurodegeneration.

Current Clinical Studies

Because Tesamorelin is already FDA-approved for human use, it remains an attractive subject for ongoing research in:

• Cardiovascular risk modulation

• Nerve repair and recovery

• Cognitive decline and aging-related metabolic dysfunction

Current trials continue to evaluate Tesamorelin’s broader metabolic and neuroendocrine potential.

References

1. Clinical Review Report: Tesamorelin (Egrifta). Canadian Agency for Drugs and Technologies in Health, 2016.

2. Mangili A., Falutz J., Mamputu J.-C., Stepanians M., Hayward B. Predictors of Treatment Response to Tesamorelin in HIV-Infected Patients with Excess Abdominal Fat. PLoS ONE. 2015;10(10):e0140358. PubMed: 26496650

3. Falutz J. et al. Metabolic effects of a growth hormone–releasing factor in patients with HIV. N Engl J Med. 2007;357(23):2359–2370. PubMed: 18057339

4. Stanley T.L. et al. Reduction in visceral adiposity is associated with an improved metabolic profile in HIV-infected patients receiving Tesamorelin. Clin Infect Dis. 2012;54(11):1642–1651. PubMed: 22474222

5. Rochira V., Guaraldi G. Growth hormone deficiency and human immunodeficiency virus. Best Pract Res Clin Endocrinol Metab. 2017;31(1):91–111. PubMed: 28477763

6. Tuffaha S.H. et al. Therapeutic augmentation of the growth hormone axis to improve outcomes following peripheral nerve injury. Expert Opin Ther Targets. 2016;20(10):1259–1265. PubMed: 27338347

7. Friedman S.D. et al. Growth hormone–releasing hormone effects on brain GABA levels in mild cognitive impairment and healthy aging. JAMA Neurology. 2013;70(7):883–890. PubMed: 23649788

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