Looking for clinical data related to tesamorelin for weight loss?
Researchers around the world are turning to tesamorelin to tackle obesity and the associated risks of serious, life limiting conditions, including cardiovascular disease, stroke, and diabetes.
While numerous treatment solutions for the obesity epidemic have been proposed, many are ineffective or difficult to carry out successfully.
Current, cutting-edge research has identified properties of tesamorelin that may be able to reduce weight and the cardiovascular and diabetic risks associated with obesity.
Tesamorelin is a peptide that stimulates the release of growth hormone in a physiological manner and has been shown to reduce visceral fat mass and improve cardiovascular risk metrics without the usual risks of direct treatment with synthetic growth hormone.
In this guide, researchers will find a summary of research supporting the potential benefits of tesamorelin for the management of obesity and its related risks, including the current knowledge about its clinical use, dosages, and safety.
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What is Tesamorelin?
Peptides like tesamorelin are small proteins that perform a myriad of important tasks in the body. Many components of cell and tissue structure, regulatory substances, enzymes, and hormones are peptides. They also serve as the building blocks for larger proteins.
Essential types of peptides include hormones such as growth hormone (GH) and insulin-like growth factor 1 (IGF-1). GH was named as such because it was initially thought to primarily regulate growth in children. It is now known that GH is a powerful and pleiotropic substance with many tissue growth and healing properties affecting nearly every cell in the body [1].
GH also stimulates the release of IGF-1, which itself has numerous properties that include regulating tissue metabolism and growth, fat metabolism, and cellular health [2]
There are several mechanisms that regulate the release of growth hormone from the anterior pituitary gland in the brain. A peptide known as growth hormone-releasing hormone (GHRH) is one of the principal means to increase GH, and consequently IGF-1, levels.
Tesamorelin is a 44 amino acid synthetic form of GHRH (GHRH analog) and its structure and properties are identical to natural GHRH [3]. In addition to stimulating the release of GH, GHRH itself has direct beneficial effects on wound healing, inflammation, immune and reproductive health, and cardioprotection [4].
A potentially important distinction between the use of synthetic GH and tesamorelin is the level of GH achieved in the circulation. The efficient breakdown of lipids to generate energy appears to require the release of GH in a pulsatile manner. This pulsatile GH pattern is not achieved with continuous administration of GH but is seen following tesamorelin administration [5].
Benefits of Tesamorelin for Weight Loss
Now that we have covered the basics of tesamorelin, let’s go over why the research community is excited about the potential use of tesamorelin for weight loss.
Growth Hormone and Body Fat
To understand the potential benefits of tesamorelin treatment for abdominal obesity it is important to understand a bit about body fat metabolism and growth hormone [6, 7].
It is inarguable that excess body fat, especially visceral adipose tissue (VAT), has numerous adverse effects on the body and quality of life.
Among its multifunctional properties, GH stimulates lipolysis and the uptake of triglycerides into muscle. It is generally accepted that growth hormone deficiency is highly associated with increased body fat, abnormal lipid metabolism, and associated health risks. As such, most of the early research and clinical investigations of tesamorelin were done in HIV-infected individuals on earlier forms of combined antiretroviral therapy (cART) [3].
An adverse effect associated with cART was lipid dysmetabolism production, in particular abdominal VAT. Fat is not merely a passive tissue but actively secretes a number of hormones and other peptides, many of which are inflammatogenic. VAT is highly associated with insulin resistance, hepatic steatosis, metabolic syndrome, cardiovascular disease, hypertension, and early mortality. By contrast, subcutaneous adipose tissue (SAT) has ameliorating effects on these risks [8].
The exogenous administration of growth hormone reduces abdominal fat mass in patients with excess VAT although it is associated with abnormally elevated IGF-1 levels and increased insulin resistance [6].
Researchers should note that IGF-I itself is a multifunctional peptide that can have somewhat paradoxical effects. While normal levels of IGF enable normal fat and carbohydrate metabolism, elevated levels are associated with insulin deficiency, growth hormone suppression, and dyslipidemia.
Tesamorelin Reduces Visceral Adipose Tissue
Tesamorelin was approved by the United States Food and Drug Administration (FDA) in 2010 for the treatment of obesity-associated diabetes and cardiovascular disease in HIV patients [9].
Both GH and adiponectin levels are decreased in obese patients and improve with weight loss. Adiponectin is a peptide secreted by fat cells with properties that include reduction of inflammation and atherogenesis, and increased insulin sensitivity [8].
However, contrary to findings with endogenous pulsatile GH, increased exogenous pulsatile GH levels from tesamorelin treatment was not shown to increase adiponectin levels in either normal or obese human subjects [10].
A double-blind study in HIV-infected patients treated with tesamorelin showed a significant reduction of VAT compared to controls (-24 ± 41 versus 2 ± 35 cm²) while SAT remained unchanged. Body weight and BMI did not change after six months but waist circumference significantly decreased, lean body mass increased, and patient self-image improved. Also noted was a significant reduction in serum triglycerides (-37 ± 139 versus 6 ± 112 mg/dL) [11].
Two pooled analyses of randomized, controlled studies of HIV-infected patients with acquired lipodystrophy have examined the potential benefits of tesamorelin in overweight and obese individuals [12, 13].
Both studies showed significant absolute reductions of visceral fat. The effect was more pronounced in patients with baseline elevations of triglyceride levels >1.7 mmol/L (151 mg/dL) and in white versus nonwhite patients [12]. Mean reductions of VAT after six months ranged from -11.7% to -19.6% with waist circumference reductions from 1.32-1.8cm.
Thus, tesamorelin decreases VAT, and results in a significant proportion of both overweight and obese patients reaching target reductions of visceral fat. Serum triglyceride, LDL, and non-HDL cholesterol levels also decrease following tesamorelin treatment of type 2 diabetics [14].
The administration of recombinant GH (rGH) also demonstrates effectiveness in the reduction of VAT in HIV-infected obese subjects. Unlike tesamorelin, however, the use of rGH may cause significant decreases in insulin sensitivity, glucose intolerance, and supraphysiologic levels of IGF [15]. By contrast, tesamorelin does not.
Tesamorelin Reduces Liver Fat
Fat accumulation in the liver is common in patients with visceral adipose tissue.
In a double-blind, randomized, placebo-controlled trial conducted over 26 weeks in HIV-infected patients, tesamorelin administration resulted in small but significant reductions of fat content in the liver [16].
Moreover, obese, HIV-infected patients with nonalcoholic fatty liver disease treated with tesamorelin in a similar fashion had reduction of hepatic inflammation as evidenced by reduced elevations of liver transaminases that correlated with reductions of VAT [12].
Tesamorelin Side Effects
In general, few and usually transient side effects have been reported, albeit frequently, in studies of tesamorelin treatment.
In a long-term safety study in HIV patients, treatment with tesamorelin for 52 weeks had no associated persistent or substantial adverse effects (AE) [17].
Other reported symptoms of tesamorelin include nausea, diarrhea, fatigue, headache, upper respiratory infection, and lightheadedness.
Overall, across three randomized studies the overall frequency of any AE was 82.1% in subjects receiving tesamorelin compared to 80.4% for placebo subjects. No attributable serious AE have been observed in placebo controlled studies [18].
Tesamorelin rarely has adverse effects on insulin metabolism or diabetic glycemic control.
Since tesamorelin is most often administered as a subcutaneous injection, researchers should be aware of the possibility of injection-related side effects, including redness, inflammation, burning, or itching at the site of injection. Researchers are advised to rotate sites of injection with each administration.
Apart from these considerations, readers should note that tesamorelin that is sold as a reference material is strictly intended for handling by qualified researchers and laboratory professionals.
How Long is a Tesamorelin Cycle?
Most studies to date have used initial treatment cycles of 26 weeks of daily treatment; some shorter-term studies have not observed significant changes of VAT or waist circumference. Sustained improvement in study extensions up to 52 weeks are well-described [11, 13, 16, 17].
With discontinuation of treatment, phenotypic and laboratory studies (viz lipids) typically return to baseline values.
Despite the relatively long-term duration of these studies, most independent researchers opt to administer tesamorelin in cycles of six to eight weeks, followed by a break from administration of at least equal duration.
Tesamorelin Dosage and Administration for Weight Loss
Clinical studies of tesamorelin have generally used doses of 1mg or 2mg tesamorelin given subcutaneously once daily. As noted above, a common tesamorelin protocol for weight loss typically ranges from six to eight weeks.
In clinical studies, the 2mg daily dose was generally found to have a greater favorable effect on VAT and waist circumference reductions and lowering of elevated lipid levels. Dose adjustments may be built into the protocol to account for out-of-range increases of blood sugar, HB1Ac, supranormal IGF-1 levels, increases of serum creatinine or liver transaminases.
In light of these considerations, here is a sample tesamorelin dosing protocol for weight loss research:
- Dose: 1mg or 2mg tesamorelin
- Frequency: The peptide should be administered subcutaneously once daily. Rotate injection sites to minimize local inflammation and bruising.
- Study Duration: 6-8 weeks
- Notes: Tesamorelin is commonly available as a sterile lyophilized powder containing 5mg of tesamorelin peptide per vial. At the 1mg tesamorelin dose, a researcher would require 12 5mg tesamorelin vials to conduct an eight week study.
Where to Buy Tesamorelin Online? | 2024 Edition
For approved research purposes, tesamorelin can be purchased by investigators without a prescription. However, researchers should be extra careful when determining where to buy peptides online, given the high amount of substandard peptides in the global marketplace.
To secure research-grade tesamorelin for research purposes, visit our go-to provider:
Xcel Peptides
Purchasing tesamorelin and other available peptides from Xcel Peptides promises:
- Top-Quality Peptides: Xcel Peptides consistently supplies superior products of at least 99% purity based on HPLC-MS testing. Laboratory reports are available through their user-friendly website or upon request.
- Fair Prices: As of writing, Xcel Peptides' tesamorelin 10mg retails for $79, with discounts available. Plus, shipping is waived on U.S. orders over $200.
- Outstanding Support: Xcel Peptides' service representatives are always on hand to address any questions or concerns. Response times generally range from 1-2 business days.
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Bacteriostatic Water and Tesamorelin
Additional items are necessary for the proper handling of tesamorelin. These include bacteriostatic water, sterile vials, and more. It is essential that all preparations be handled in a sterile manner.
Efficient acquisition of these supplies can be done through our approved research materials supplier.
Tesamorelin and Weight Loss | Overall
Current evidence is clear that tesamorelin treatment provides tremendous weight loss benefits.
This is seen through evidence that it reduces the volume of VAT, decreases waist circumference, and diminishes elevated triglyceride and cholesterol levels in HIV-infected patients. Notably, similar reductions of VAT have yet to be shown in non-obese individuals.
Two major as yet unanswered questions are whether these observations can be applied to non-HIV patients with excess VAT and, importantly, whether these effects translate to diminished long-term morbidity and mortality associated with cardiovascular disease, diabetes, and other metabolic syndrome-associated disturbances.
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