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. Hexarelin is a research peptide that is still being investigated. It is not for human consumption.
What is Hexarelin used for?
Hexarelin is a synthetic analogue of ghrelin that shows benefit in heart disease and cardiac ischemia, protecting the heart following a heart attack. Research has shown that Hexarelin also protects skeletal muscle against wasting and improves cholesterol and triglyceride levels. A recently completed phase II human trial in heart failure patients revealed that Hexarelin protected the heart following a heart attack and the results from this trial are promising.
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In 2011, a multi-center randomized double-blinded, placebo-controlled, dose-escalating study of 30 healthy adult volunteers showed that Hexarelin reduces markers of the aging process (e.g., telomere length, interleukin-6, and C-reactive protein). These effects were dose-dependent.
Is hexarelin a GHRH?
Hexarelin has been shown to reduce insulin resistance, reduce blood pressure, lower cholesterol and triglycerides, reduce adipose tissue inflammation, increase energy expenditure, and reduce the risk of obesity in clinical trials. It has been shown to produce weight loss in clinical trials.
Hexarelin is being developed by Gensign Health in collaboration with Pronos Group (Moss, England) as a potential treatment for cardiovascular disease and other conditions where a sustained release formulation would be advantageous.
What are Hexarelin Benefits?
Cardiovascular disease is a major health problem in the western world. Chronic cardiovascular disease, often seen in combination with diabetes, is the major cause of death in patients with Type 2 Diabetes (T2D).
Ghrelin is a peptide that is predominantly secreted by the stomach and is implicated in metabolic regulation. In its active form, ghrelin has been shown to increase appetite and food intake in a number of animal studies. In humans, plasma levels of ghrelin are elevated following meal ingestion. Ghrelin also has effects on cardiovascular function. In experimental animals, ghrelin is shown to reduce cardiac contractility and blood pressure and to stimulate vasodilation. Chronic administration of ghrelin in rats, induces a decrease in blood pressure and increases endothelium-dependent vasodilation.
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Clinical data have shown that ghrelin and its analogues are associated with favourable effects on body weight and weight gain, in obese and overweight subjects. This clinical benefit is independent of the food that the individual consumes. Studies have also shown that ghrelin may protect the heart following a heart attack and may promote cardiac recovery.
In the setting of ischemia, ghrelin has been shown to reduce infarct size, limit remodeling and improve ejection fraction. This ability to protect the heart during an episode of acute ischemia has implications for the treatment of ischaemic heart disease. Ghrelin also has beneficial effects on the cardiovascular system in individuals with Type 2 Diabetes (T2D). For example, chronic administration of ghrelin increases insulin sensitivity in healthy volunteers, animal models, and patients with T2D. Ghrelin is also shown to increase fat oxidation and reduce systemic lipid levels in patients with T2D.
Development of Hexarelin
A synthetic analog of ghrelin, Hexarelin (hexarelin and \[D-Lys-6\]-GHRP-6), has been shown to be an effective and safe weight loss agent in obese adults. Two-phase III randomized, double-blind, placebo-controlled, multi-center trials have been completed which demonstrated the efficacy of Hexarelin for the treatment of overweight and obese adults.
The phase III trials met their primary endpoints demonstrating that Hexarelin causes greater weight loss than placebo at 12 and 24 weeks. These results were obtained after approximately 11 and 17 days of treatment. These trials also demonstrated a reduction in total fat mass and fat mass in the legs. Although there was no difference between groups in body weight after 12 weeks, patients treated with Hexarelin at the lower doses were less likely to gain weight and remained in a normal weight range.
The primary results of these studies were presented at the 54th Annual Meeting of the European Association for the Study of Diabetes in Munich, Germany.
The safety of Hexarelin was also demonstrated in these trials. These trials showed that Hexarelin did not produce any adverse effects that would lead to discontinuation of the treatment. The most commonly reported side effect in both trials was dizziness (a decrease in blood pressure) that occurred more frequently in the Hexarelin treated groups. Other reported side effects included nausea, abdominal discomfort, headache, and gastroenteritis.
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Results from a recently completed randomized, double-blind, placebo-controlled, dose-escalating trial in a heart failure patient population (NCT00976562) indicated that Hexarelin improved lipid and glucose parameters, reduced the risk of death and hospitalization for heart failure, and reduced the risk of dying or needing a transplant.
The study enrolled 102 patients, of whom 26 were included in the per protocol analysis.
A total of 22 patients (85%) received the higher Hexarelin dose of 1.25 mcg/kg/min and 4 patients (15%) received the lower dose of 0.625 mcg/kg/min. The primary endpoint was changed in insulin resistance. Hexarelin had a positive effect on fasting blood glucose (mean reduction from baseline in Hexarelin treated patients was 0.45 mmol/L), insulin resistance (the homeostasis model assessment insulin resistance, HOMA-IR), and the fasting plasma triglycerides (the mean change from baseline for this parameter was -6.5%). Furthermore, Hexarelin improved the metabolic parameters of the cholesterol fraction and low density lipoprotein (LDL).
The most common side effects in this trial were nausea and dizziness (which occurred in the majority of patients).
Gensign Health is now planning to begin phase III clinical trials in patients with T2D.
Safety and quality research peptides for sale
Hexarelin is manufactured in-house by Gensign Health and all products are manufactured with GMP standards in place.
Hexarelin has been approved by the FDA as an investigational new drug (IND) for the treatment of over weight/obese patients. It is the only synthetic derivative of ghrelin which has been approved for the treatment of obesity and is in the final stages of testing for the treatment of heart disease.
Hexarelin has been marketed in Japan, Germany and the UK for the treatment of obesity.
Hexarelin has been manufactured in GMP conditions by Gensign Health, UK and is packaged in foil pouches and glass vials.