OVERVIEW

Tesamorelin is a synthetic peptide composed of 44 amino acids, designed as a growth-hormone-releasing hormone (GHRH) analogue. It is FDA-approved for the treatment of HIV-associated lipodystrophy, a condition characterized by abnormal fat accumulation. Beyond this application, research suggests Tesamorelin may offer additional therapeutic benefits, including:

• Reducing visceral fat and cardiovascular disease risk in HIV patients.
• Enhancing peripheral nerve regeneration, potentially aiding in nerve injury recovery.
• Improving cognitive function and slowing the progression of mild cognitive impairment (MCI), a precursor to dementia.
• Addressing growth hormone (GH) deficiency in HIV patients, supporting hormonal balance without the risks of direct GH administration.

These potential benefits have made Tesamorelin a subject of ongoing research in metabolic, neurological, and regenerative medicine.

RESEARCH

Tesamorelin and HIV-Associated Lipodystrophy

• Tesamorelin was FDA-approved in 2010 for the treatment of HIV-associated lipodystrophy.
• It reduces visceral adiposity by nearly 20%, making it four times more effective than alternative treatments.
• Potential application: Managing abnormal fat accumulation in HIV patients.

Tesamorelin and Cardiovascular Health

• HIV patients face an increased risk of cardiovascular disease (CVD) due to fat accumulation and side effects of antiretroviral therapy.
• Tesamorelin has been shown to:
  • Lower triglycerides, total cholesterol, and non-HDL cholesterol levels.
  • Reduce visceral adipose tissue, improving overall metabolic health.
  • Decrease systemic inflammation, a major risk factor for CVD.
• Potential application: Metabolic health support and cardiovascular disease prevention.

Tesamorelin and Growth Hormone Deficiency in HIV

• One-third of HIV patients receiving Highly Active Antiretroviral Therapy (HAART) develop growth hormone deficiency, contributing to fat accumulation and metabolic dysfunction.
• Tesamorelin safely increases GH levels, avoiding the risks of direct GH administration, such as edema and GH desensitization.
• Potential application: Hormonal balance and metabolic support in HIV patients.

Tesamorelin and Peripheral Nerve Regeneration

• Nerve damage due to injury, diabetes, or surgery is often difficult to treat.
• Studies suggest GH-based therapies, including Tesamorelin, may accelerate nerve repair and enhance sensory and motor function.
• Potential application: Neurological recovery and nerve regeneration therapy.

Tesamorelin and Cognitive Function

• A large randomized controlled study at the University of Washington found that Tesamorelin enhances cognition in early-stage dementia.
• Key findings include:
  • Increased GABA (gamma-aminobutyric acid) levels, supporting brain function and neuroprotection.
  • Reduction of myo-inositol, a compound linked to brain aging and cognitive decline.
• Potential application: Neuroprotection and dementia prevention.

STRUCTURE

• Molecular Formula: C₂₂₃H₃₇₀N₇₂O₆₉S
• Molecular Weight: 5195.908 g/mol
• Amino Acid Sequence:
  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
• CAS Registry Number: 901758-09-6

CITATIONS

1. Clinical Review Report: Tesamorelin (Egrifta). Canadian Agency for Drugs and Technologies in Health(2016).
2. A. Mangili, J. Falutz, J.-C. Mamputu, M. Stepanians, and B. Hayward. Predictors of Treatment Response to Tesamorelin, a Growth Hormone-Releasing Factor Analog, in HIV-Infected Patients with Excess Abdominal Fat.PLOS One (2015).
3. J. Falutz et al. Metabolic effects of a growth hormone-releasing factor in patients with HIV. N. Engl. J. Med. (2007).
4. T. L. Stanley et al. Reduction in visceral adiposity is associated with an improved metabolic profile in HIV-infected patients receiving tesamorelin. Clin. Infect. Dis. Off. Publ. Infect. Dis. Soc. Am. (2012).
5. V. Rochira and G. Guaraldi. Growth hormone deficiency and human immunodeficiency virus. Best Pract. Res. Clin. Endocrinol. Metab. (2017).
6. S. H. Tuffaha et al. Therapeutic augmentation of the growth hormone axis to improve outcomes following peripheral nerve injury. Expert Opin. Ther. Targets (2016).
7. S. D. Friedman et al. Growth hormone-releasing hormone effects on brain γ-aminobutyric acid levels in mild cognitive impairment and healthy aging. JAMA Neurol. (2013).