What Is Tesamorelin?
Tesamorelin is a chemically altered growth hormone-releasing hormone (GHRH) analog. This peptide is a trans-3-hexanoic acid version of natural GHRH. In 2010, the peptide that Theratechnologies of Canada produced became the newest drug to be approved by the FDA to treat HIV-associated lipodystrophy. It has the potential to enhance peripheral nerve regeneration and improve mild cognitive impairment (MCI), the precursor to dementia.
Tesamorelin mediates the positive influence of GHRH and other GHRH analogs such as GRF (1-29), CJC-1295, and sermorelin. The trans-3-hexanoic acid modification increases its blood plasma stability and half-life. Both tesamorelin and CJC-1295 maintain the physiological effects of GHRH and show limited side effects compared to other analogs, which disrupt the physiological rhythm of GH release.
Molecular Formula: C221H366N72O67S
Molecular Weight: 5135.77 g/mol
PubChem: CID 44147413
CAS Number: 901758-09-6
Growth Hormone Deficiency and HIV
Highly active antiretroviral therapy (HAART) triggers endocrine and metabolic disorders, including growth hormone (GH) deficiency. HIV infection alters the pituitary gland function and causes GH deficiency in one-third of HAART patients. Tesamorelin is a safer and more effective treatment for improving GH levels than the administration of exogenous GH, particularly in HIV-positive individuals.
Adiposity and antiretroviral drugs put HIV-positive individuals at increased risk of developing cardiovascular disease (CVD). Hence prevention of CVD is of crucial concern in such patients, and statins have been the drug of choice.
Tesamorelin reduces lipodystrophy and triglyceride, total cholesterol, and non-HDL-C in HIV-positive patients. Ectopic fat deposition is involved in inflammation, which increases the risk of CVD. Adipose tissue deposition in visceral organs, epicardium, and liver enhance CVD risk. The peptide thus decreases inflammatory response by controlling excess adiposity.
Tesamorelin and Lypodystrophy
It is principally used to treat HIV-associated lipodystrophy caused by a viral infection and the adverse effect of antiretroviral therapy.
Patients suffering from lipodystrophy relied on diet, exercise, some ineffective medications, and surgery as a last measure. US FDA approved the drug in 2010 exclusively for lipodystrophy treatment. It reduces adiposity by about 20% in the patients and is 4 times more effective than other treatment regimens combined.
Peripheral Nerve Damage
Peripheral nerve damage can be caused by injury, diabetes, or surgical interventions. It triggers debilitating motor and sensory function challenges in the affected parts. There is very limited intervention as nerve cells are tough to regenerate. Studies show that growth hormone manipulation can improve peripheral nerve injury and increase both rate and extent of healing. Tesamorelin is being considered for such intervention, partially due to the existing FDA approval.
Tesamorelin Investigated in Dementia
GHRH analogs, including tesamorelin, help improve cognitive ability in patients suffering from the early stages of dementia. A randomized, double-blind, placebo-controlled study was conducted with a large cohort over a period of twenty weeks at the University of Washington School of Medicine. The study highlights that tesamorelin and other GHRH analogs can influence dementia by increasing gamma-aminobutyric acid (GABA) in the brain and decreasing myo-insoitol (MI). Thus these findings on the potential of tesamorelin use in the treatment of dementia also suggest new avenues for research to find a cure.
The peptide is a sort after molecule for clinical trials as it has been FDA approved for human use. It is presently being evaluated for its ability to regulate cardiovascular disease in HIV, enhance healing of peripheral nerves following injury, and slow the progression of dementia. Clinical trials are being conducted in several different areas.
Tesamorelin shows minimal side effects, low oral bioavailability, and excellent subcutaneous bioavailability in mice. The dosage for use in mice (per kg) does not scale to humans. Tesamorelin is sold at Biotech Peptides mainly for educational and scientific research and not for human use.