Molecular Formula: C221H366N72O67S
Molecular Weight: 5135.77 g/mol
PubChem: CID 44147413
CAS Number: 901758-09-6
What Is Tesamorelin?
Tesamorelin is a chemically altered growth hormone-releasing hormone (GHRH) analogue. This peptide is a trans-3-hexanoic acid version of natural GHRH. In 2010, the peptide which was produced by Theratechnologies of Canada became the newest drug to be approved by the FDA for the treatment of 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 analogues 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 analogues which disrupt the physiological rhythm of GH release.
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 compared to the administration of exogenous GH, particularly in HIV-positive individuals.
Adiposity and use of 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 not only lipodystrophy but also triglyceride, total cholesterol and non-HDL-C in HIV-positive patients. Ectopic fat deposition is involved in inflammation which happens to increase the risk of CVD. Adipose tissue deposition in visceral organs, epicardium and liver enhances the risk of CVD. The peptide thus decreases inflammatory response by controlling excess adiposity.
Tesamorelin and Lypodystrophy
It is principally used for the treatment of HIV-associated lipodystrophy caused by the viral infection as well as the adverse effect of antiretroviral therapy.
Patients suffering from lipodystrophy relied on diet, exercise, some ineffective medications and finally on 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 challenges with both motor and sensory function 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 as well as 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 analogues including tesamorelin help to 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 by decreasing myo-insoitol (MI). Thus these findings the potential of tesamorelin use in the treatment of dementia, but also suggest new venues for research for finding 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.
Buy Tesamorelin peptide (10mg) if you are a licensed researcher.