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Tesamorelin, est un analogue d'hormones de libération de l'hormone de croissance (GHRH) utilisé cliniquement pour le traitement de la lipodystrophie associée au VIH (dépôt de graisse dysfonctionnel). Il est également recherché pour sa capacité à améliorer la santé du nerf périphérique, ralentit la progression des troubles cognitifs légers et la réduction de la masse grasse.
Utilisation du produit:Ce produit est conçu uniquement comme un produit chimique de recherche.Cette désignation permet l'utilisation de produits chimiques de recherche strictement pour les tests in vitro et l'expérimentation de laboratoire uniquement. Toutes les informations sur les produits disponibles sur ce site Web sont à des fins éducatives uniquement. L'introduction corporelle de toute nature dans l'homme ou les animaux est strictement interdite par la loi. Ce produit ne doit être géré que par des professionnels agréés et qualifiés. Ce produit n'est pas une drogue, de la nourriture ou un cosmétique et peut ne pas être mal étendu, mal utilisé ou erroné comme drogue, aliment ou cosmétique.
Tesamoreline est un analogue d'hormone libérant des hormone de croissance (GHRH) composé de GHRH standard auquel un groupe d'acide trans-3-hexanoïque supplémentaire a été ajouté. Produit par Theratechnologies du Canada, Tesamorelin est devenu le plus récent médicament à approuver par la FDA pour une utilisation dans la lipodystrophie lipo-associée au VIH en 2010. Le peptide a également été étudié pour sa capacité à améliorer la régénération du nerf périphérique et comme une intervention potentielle pour une légère déficience cognitive (MCI), le précurseur du démentiment.
En tant queCulpabilitéAnalogique, Tesamorelin a tous les mêmes effets que les analogues GHRH et GHRH commesermorelin, Grf (1-29), CJC-1295, etc. L'ajout d'acide trans-3-hexanoïque à la tesamoriéline le rend plus stable dans le plasma humain et augmente ainsi sa demi-vie. Malgré cette augmentation de la demi-vie, Tesamorelin, comme CJC-1295, préserve l'action physiologique de la GHRH et a donc moins d'effets secondaires que les molécules similaires qui effaceront la libération d'hormones de croissance pulsatile normale (GH).
L'utilisation principale de la Tesamoreline réside dans le traitement de la lipodystrophie associée au VIH, qui survient à la fois en conséquence de l'infection par le VIH et comme un effet secondaire du traitement antirétroviral. Dans la lipodystrophie, la graisse s'accumule excessivement à la fois dans l'abdomen et dans d'autres zones du corps. Le mécanisme physiologique responsable de cela n'est pas clairement compris, mais on pense que les inhibiteurs de protéase couramment utilisés jouent un rôle important dans la pathogenèse de la lipodystrophie[1].
Patients suffering from lipodystrophy initially had diet, exercise, and a handful of ineffective medications to rely on for treatment. If those did not work, surgery was a last-ditch, often ineffective, and frequently complicated solution. In 2010, however, the FDA approved tesamorelin specifically for the treatment of HIV-associated lipodystrophy. The drug has been found to reduce adiposity by nearly 20% in this population [1]. Research suggests that tesamorelin is approximately 4 times more effective in reducing adiposity than all of the other available therapies combined [2].
People with HIV are at increased risk of developing cardiovascular disease (CVD), in part due to abnormal fat deposition and in part due to the actions of antiretroviral drugs themselves. Prevention of CVD in HIV-positive individuals is considered to be the most important medical intervention for long-term well-being, after highly active antiretroviral therapy (HAART) of course. Until recently, statins have been the cornerstone of medical management in this population.
Research shows that tesamorelin, in addition to decreasing lipodystrophy, also reduces triglyceride levels, total cholesterol levels, and non-HDL-C levels in HIV-positive patients. A 15% reduction in visceral adipose tissue by tesamorelin correlates with a 50 mg decrease in trigylceride levels[3], [4].
It is worth noting that ectopic fat deposition, as seen in lipodystrophy, is associated with inflammation. Inflammation of any kind is a risk factor for CVD. Visceral adipose tissue, liver fat, and epicardial fat are all independently associated with increased risk of CVD. By reducing ectopic fat deposition, tesamorelin directly decreases inflammation and an individual’s risk for CVD.
Recent evidence suggests that HAART is associated with a number of endocrine and metabolic problems, including growth hormone (GH) deficiency. It appears that the pituitary gland is altered in HIV infection and, as a consequence, approximately one third of patients with HIV who are taking HAART have GH deficiency[5]. This may, to some extent, explain why lipodystrophy is so common in individuals with HIV and also why tesamorelin is such an effective treatment. Tesamorelin is a safer and more effective way to raise GH levels than administration of exogenous GH, particularly in HIV-positive individuals.
Peripheral nerve damage can be a consequence of injury, diabetes, or even surgical interventions. It often results in debilitating problems with both motor and sensory function in the affected area, but there is little that can be done to correct the problem because nerve cells are notoriously difficult to regenerate. Research, however, suggests that therapies based on growth hormone manipulation may improve peripheral nerve injury and increase both rate and extent of healing[6]. Tesamorelin is currently the leading candidate for such intervention, in part because it already has FDA approval.
There is now evidence to suggest that GHRH analogues, like tesamorelin, are effective in enhancing cognition in patients suffering from the early stages of dementia. A large, randomized, double-blind, placebo-controlled study at the University of Washington School of Medicine, carried out over twenty weeks, suggests that tesamorelin and other GHRH analogues may impact dementia by increase gamma-aminobutyric acid (GABA) levels in the brain and by decreasing myo-insoitol (MI) levels[7]. These findings open up a pathway for using tesamorelin in the treatment of dementia, but also suggest new areas for scientists to explore as they look for a cure or a preventative.
Because it is FDA approved for use in humans, tesamorelin is an attractive peptide for ongoing clinical research. It is currently under review for its ability to reduce cardiovascular disease in HIV, improve healing of peripheral nerves following injury, and slow the progression of dementia. Clinical trials are already underway in several different areas.
Tesamorelin exhibits minimal side effects, low oral and excellent subcutaneous bioavailability in mice. Per kg dosage in mice does not scale to humans. Tesamorelin for sale at
The above literature was researched, edited and organized by Dr. Logan, M.D. Dr. Logan holds a doctorate degree from Case Western Reserve University School of Medicine and a B.S. in molecular biology.
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