Tesamorelin, 5 vial kit, 10mg

Tesamorelin, 5 vial kit, 10mg

Brand: Full Catalog
Product Code: TS20
Availability:
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Price: $89.00
Description

Tesamorelin 5 vials, 2mg / vial, 10mg total weight

 

Tesamorelin Information

Tesamorelin (Egrifta) is a synthetic growth-hormone releasing-hormone (GHRH) peptide analog, FDA-approved for visceral fat related to lipodystrophy in HIV patients[1]. As a growth hormone (GH) secretagogue, tesamorelin induces GH release through pituitary cells called somatotrophs. Tesamorelin was selected for development as an HIV drug because it is not a ghrelin analog and avoids the drawbacks of GHRPs on appetite and other effects of partial ghrelin agonism, but is more robust than many GHRH analogs. Tesamorelin has also shown the potential for lowering serum triglycerides, improving the metabolic profile of certain patient populations, and restoring GH pulsatility in physiologically deficient states.

The pharmacokinetic properties of tesamorelin allow for infrequent dosing; weekly and daily dosing are commonly used in studies[2]. Unlike hypothalamic GHRH and some analogs, tesamorelin is resistant to physiological degradation and is commonly administered subcutaneously in studies without an accompanying GHRP[2].

Tesamorelin has the full 44 amino acids of it endogenous counterpart, unlike most GRF (growth hormone releasing factor) analogs, as well as an added trans-3-hexenoic acid group. The structure, properties, and durability of tesamorelin and other robust GRF analogs make them attractive for HIV lipodystrophy: “Growth hormone-releasing factor (GRF) analogs with greater stability than the natural hormone can induce growth hormone secretion in a physiological manner, and appear to be promising candidate therapies.”[3]

Unlike synthetic rHGH, tesamorelin does not appear to impair glucose tolerance[4][5]. The main therapeutic effect of tesamorelin can be described as “reduc[ing] the cardiovascular risk associated with lipodystrophy-related [or other] metabolic complications and help to maintain a more normal distribution of body fat”[3].

In mammals the amount and distribution of body fat reflects energy expenditure, health or disease state, genetic factors, and dietary habits, and is also closely linked with the prospective risk and health outcomes of many health conditions. In a randomized multicenter trial of over 800 HIV-positive patients who also had markers of unhealthy body-fat levels and distribution (based primarily on hip and waist circumference, hip-to-waist ratio, and BMI), favorable effects on body composition were observed:

At Week 26, treatment with EGRIFTA™ resulted in a reduction from baseline in mean trunk fat of 1.0 kg in Study 1 and 0.8 kg in Study 2, respectively (compared with an increase of 0.4 kg in Study 1 and of 0.2 kg in Study 2, respectively, in patients receiving placebo). Treatment with EGRIFTA™ resulted in an increase from baseline in mean lean body mass of 1.3 kg in Study 1 and of 1.2 kg in Study 2, respectively (compared with a decrease of 0.2 kg in Study 1 and of 0.03 kg in Study 2, respectively, in patients receiving placebo). On average, there were no adverse effects of EGRIFTA™ on lipids or subcutaneous adipose tissue (SAT)[6]

Visceral adipose tissue strongly appears to be causative in poor health outcomes in other populations, as well:

Visceral fat (VF) accretion is a hallmark of aging in humans. Epidemiologic studies have implicated abdominal obesity as a major risk factor for insulin resistance, type 2 diabetes, cardiovascular disease, stroke, metabolic syndrome and death. Utilizing novel rodent models of visceral obesity, studies have demonstrated a causal relationship between VF and age-related diseases. In contrast, surgically removing large quantities of subcutaneous (SC) abdominal fat does not consistently improve metabolic parameters in humans or rodents, suggesting that SC fat accrual is not an important contributor to metabolic decline. There is also compelling evidence in humans that abdominal obesity is a stronger risk factor for mortality risk than general obesity. Likewise, we have shown that surgical removal of VF improves mean and maximum lifespan in rats, providing the first causal evidence that VF depletion may be an important underlying cause of improved lifespan with CR. Given the hazards of VF accumulation on health, treatment strategies aimed at selectively depleting VF should be considered as a viable tool to effectively reduce disease risk in humans[7]

While robust enough to administer standalone, tesamorelin is not a GHRP (growth-hormone releasing peptide) or ghrelin analog; as a GRF analog, it does not affect eating behavior, or glucose tolerance. Among relevant patient populations, many with visceral adipose tissue (VAT) and abnormal metabolic profiles and/or growth hormone deficiency, this comparative safety advantage is a key factor in viability.

Citations
[1] Falutz J, Allas S, Mamputu JC, et al.  Long-term safety and effects of tesamorelin, a growth hormone-releasing factor analogue, in HIV patients with abdominal fat accumulation.  AIDS.  Sep 2008 12:22(14):1719-28.
[2] Patel A, Gandhi H, Upaganlawar A, Tesamorelin: A hope for ART-induced lipodystrophy.  Journal of Pharmacy and Bioallied Sciences.
[3]Hu M, Tomlinson B. Growth hormone-releasing factor agonists for the treatment of HIV-associated lipodystrophy.  Curr Opin Investig Drugs. 2010 Oct;11(10):1143-50.
[4] Liang L et al.  [Effect of recombinant human growth hormone on glucose metabolism in children with growth hormone deficiency – trans. Chinese]. Zhonghua Er Ke Za Zhi. 2006
[5] Stanley TL, Chen CY, Branch KL, et al.  Effects of a growth hormone-releasing analog on endogenous GH pulsatility and insulin sensitivity in healthy men.  J Clin Endocrinol Metab. 2011 Jan; 96(1):150-8.
[6]Egrifta. Highlights of Prescribing Information. <http://www.egrifta.com/Pdfs/Prescribing_Information.pdf> Accessed 05-18-2016.
[7] Huffman DM, Barzilai N, Role of Visceral Adipose Tissue in Aging. Oct 2009; 1790(10):1117-23.
Sep;44(9):657-61.
[8]Butler G, Carel JC.  Safety of recombinant human growth hormone.  Endocr. Dev. 2010;18:40-54.

 

 

 

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