Tesamorelin is a growth hormone releasing hormone (GHRH) analogue approved by the FDA for use in HIV-associated lipodystrophy. Because it increases growth hormone (GH) levels, tesamorelin can increase lean body mass, improve bone strength, burn fat, and even enhance immune function. It is the fat burning properties of tesamorelin, however, that are of greatest interest in the clinical setting. Tesamorelin is also known for its ability to improve peripheral nerve regeneration and is under investigation as a potential treatment for mild cognitive impairment (MCI). Tesamorelin has been in clinical use since 2010. Because of its long production history and relatively simple to produce characteristics, tesamorelin cost is one of the lowest among the GHRH analogues.
As a nearly bioidentical GHRH analogue, tesamorelin binds to the GHRH receptor in the anterior pituitary and stimulates GH release. This leads to increases in levels of IGF-1 and other growth factors that contribute to increased muscle mass, reduced fat mass, improved bone strength, and enhanced immunity. Research shows that tesamorelin has relatively few side effects and that it preserves the normal, physiological release of GH.
One interesting recent finding about tesamorelin is that it changes the quality of fat tissue even if it doesn’t reduce total fat tissue quantity. Research shows that tesamorelin alters existing fat deposits such that they become denser[4]. This may seem counterintuitive, but denser fat depositions are more efficient and therefore result in less distributed fat in muscle and subcutaneous tissues. In other words, tesamorelin alters the quality of fat in the body even in the rare settings where it doesn’t reduce overall fat levels. This seems to result from shifting fat out of muscle where it doesn’t belong and into existing fat depositions.
Though the research is still in its infancy, there is good reason to believe that other chronic diseases also lead to abnormal fat distribution and that correcting this might help to reduce symptoms of the diseases or even push some diseases into remission. The most recent research looked at Crohn’s disease and found that visceral fat quantities were higher in those with Crohn’s compared to normal controls. Additionally, visceral fat deposits correlated with disease severity and risk of adverse outcomes even as subcutaneous fat deposits did not[5]–[7]. Crohn’s and inflammatory bowel disease in general are expensive diseases to treat and place a high burden on the healthcare system. Tesamorelin cost is low, so any impact it might have on disease course or severity in inflammatory bowel disease could have a large impact on healthcare expenses.
Research shows that abnormal fat depositions may be a leading contributor to heart disease. Tesamorelin not only helps to reduce these fatty deposits, it has also been shown to lower triglyceride and cholesterol levels substantially. As discussed above, the net effect of tesamorelin may be to alter fat deposition patterns so that less of it is deposited in arteries where it can cause serious problems. This, combined with the decreased systemic inflammation that results from decreased total fat mass, can substantially impact the risk of heart disease and heart attack.
The bonus in all of this is that tesamorelin cost is a fraction of what many major heart medications cost. A perfect example would be statin drugs which cost patients literally billions of dollars per year and provide very limited benefit. The ability of tesamorelin to fight against ectopic fat deposits, such as epicardial and intravascular fat, means the peptide is targeting one of the major factors associated with increased risk of cardiovascular disease and it is doing so at relatively little expense.
Because it mimics natural physiological control, tesamorelin is safe and simple to use with almost no risk of overdose. Low tesamorelin cost is simply a benefit on top of the peptide’s already impressive properties. The tesamorelin cost to benefit equation tilts heavily in favor of benefit, thereby making it a common choice for research protocols and studies of the effects of growth hormone releasing hormone in many biological settings.
[2]Clinical Review Report: Tesamorelin (Egrifta). Ottawa (ON): Canadian Agency for Drugs and Technologies in Health, 2016. Accessed: Apr. 06, 2022. [Online]. Available: http://www.ncbi.nlm.nih.gov/books/NBK539131/
[3]A. Mangili, J. Falutz, J.-C. Mamputu, M. Stepanians, and B. Hayward, “Predictors of Treatment Response to Tesamorelin, a Growth Hormone-Releasing Factor Analog, in HIV-Infected Patients with Excess Abdominal Fat,” PLoS ONE, vol. 10, no. 10, p. e0140358, Oct. 2015, doi: 10.1371/journal.pone.0140358.
[4]J. E. Lake et al., “Tesamorelin improves fat quality independent of changes in fat quantity,” AIDS Lond. Engl., vol. 35, no. 9, pp. 1395–1402, Jul. 2021, doi: 10.1097/QAD.0000000000002897.
[5]C. R. Rowan, J. McManus, K. Boland, and A. O’Toole, “Visceral adiposity and inflammatory bowel disease,” Int. J. Colorectal Dis., vol. 36, no. 11, pp. 2305–2319, Nov. 2021, doi: 10.1007/s00384-021-03968-w.
[6]Y. Li et al., “Visceral fat area is associated with a high risk for early postoperative recurrence in Crohn’s disease,” Colorectal Dis. Off. J. Assoc. Coloproctology G. B. Irel., vol. 17, no. 3, pp. 225–234, Mar. 2015, doi: 10.1111/codi.12798.
[7]D. Q. Holt, G. T. Moore, B. J. G. Strauss, A. L. Hamilton, P. De Cruz, and M. A. Kamm, “Visceral adiposity predicts post-operative Crohn’s disease recurrence,” Aliment. Pharmacol. Ther., vol. 45, no. 9, pp. 1255–1264, May 2017, doi: 10.1111/apt.14018.
Purification Steps Determine Tesamorelin Cost
The cost of producing peptides generally comes from the purification and lyophilization steps of the process and not from the actual peptide synthesis. This was not always the case and producing larger peptides like tesamorelin cost quite a lot in the past. With advances in scalable synthesis, however, the production costs of many peptides have come down dramatically. This is particularly true for peptides, like tesamorelin, that require some degree of modification from their “normal” or standard counterpart[1]. In short, tesamorelin cost has declined significantly as manufacturing processes have advanced. While the purification step currently represents the bulk of the cost to manufacture tesamorelin, that is only because the cost of all of the other steps has been reduced so dramatically.Tesamorelin Function
As a GHRH analogue, tesamorelin ultimately has effects similar to growth hormone. In fact, tesamorelin is nothing more than GHRH to which an additional trans-3-hexanoic acid has been added. This addition makes the peptide more stable in human plasma. As a result of this extended half-life, tesamorelin is both more affordable and easier to work with than many other GHRH analogues.As a nearly bioidentical GHRH analogue, tesamorelin binds to the GHRH receptor in the anterior pituitary and stimulates GH release. This leads to increases in levels of IGF-1 and other growth factors that contribute to increased muscle mass, reduced fat mass, improved bone strength, and enhanced immunity. Research shows that tesamorelin has relatively few side effects and that it preserves the normal, physiological release of GH.
Tesamorelin and Lipodystrophy
The primary use of tesamorelin is in the treatment of HIV-associated lipodystrophy. Because of its GHRH characteristics, tesamorelin is highly effective in stimulating thermogenesis in adipose tissue while increasing basal metabolism and shifting biochemical pathways toward muscle building. In other words, tesamorelin burns fat and builds muscle. For people suffering from the abnormal fat deposition seen in HIV and other chronic diseases, tesamorelin can reduce adiposity by as much as 20% and is 4 times more effective in burning fat that all other available anti-obesity drugs with FDA approval[2], [3].One interesting recent finding about tesamorelin is that it changes the quality of fat tissue even if it doesn’t reduce total fat tissue quantity. Research shows that tesamorelin alters existing fat deposits such that they become denser[4]. This may seem counterintuitive, but denser fat depositions are more efficient and therefore result in less distributed fat in muscle and subcutaneous tissues. In other words, tesamorelin alters the quality of fat in the body even in the rare settings where it doesn’t reduce overall fat levels. This seems to result from shifting fat out of muscle where it doesn’t belong and into existing fat depositions.
Though the research is still in its infancy, there is good reason to believe that other chronic diseases also lead to abnormal fat distribution and that correcting this might help to reduce symptoms of the diseases or even push some diseases into remission. The most recent research looked at Crohn’s disease and found that visceral fat quantities were higher in those with Crohn’s compared to normal controls. Additionally, visceral fat deposits correlated with disease severity and risk of adverse outcomes even as subcutaneous fat deposits did not[5]–[7]. Crohn’s and inflammatory bowel disease in general are expensive diseases to treat and place a high burden on the healthcare system. Tesamorelin cost is low, so any impact it might have on disease course or severity in inflammatory bowel disease could have a large impact on healthcare expenses.
Tesamorelin and Heart Disease
Heart disease is the leading cause of death in most developed nations and a major target of public health programs worldwide. In 2011, heart disease and stroke cost an estimated $316 billion in health care expenditures in the United States alone and accounted for fully one third of all deaths.Research shows that abnormal fat depositions may be a leading contributor to heart disease. Tesamorelin not only helps to reduce these fatty deposits, it has also been shown to lower triglyceride and cholesterol levels substantially. As discussed above, the net effect of tesamorelin may be to alter fat deposition patterns so that less of it is deposited in arteries where it can cause serious problems. This, combined with the decreased systemic inflammation that results from decreased total fat mass, can substantially impact the risk of heart disease and heart attack.
The bonus in all of this is that tesamorelin cost is a fraction of what many major heart medications cost. A perfect example would be statin drugs which cost patients literally billions of dollars per year and provide very limited benefit. The ability of tesamorelin to fight against ectopic fat deposits, such as epicardial and intravascular fat, means the peptide is targeting one of the major factors associated with increased risk of cardiovascular disease and it is doing so at relatively little expense.
Tesamorelin and Peripheral Nerve Damage
Another area in which tesamorelin cost may prove beneficial is in the treatment of peripheral nerve disease. Conditions like diabetes, injury, and even surgery can lead to nearly untreatable nerve damage that costs the economy billions in lost productivity and healthcare costs every year. Research shows that tesamorelin and other growth hormone analogues may improve peripheral nerve damage by stimulating neurons to regrow. Studies in mice show an improvement in both the rate and extent of healing of damaged nerves in individuals treated with growth hormone analogues[8]. Because it is already FDA approved, tesamorelin cost parameters are more favorable than many other growth hormone analogues. As such, it is likely to see expanded use in this setting and a larger market can only help to drive tesamorelin cost down further.Tesamorelin and Dementia
Given its benefits in nerve regrowth, it should come as no surprise that tesamorelin has been investigated in the treatment of neurodegenerative diseases of the brain. Research in dementia indicates that tesamorelin can benefit both executive function and verbal memory, particularly in the early stages of the disease. It seems that tesamorelin increases levels of gamma-aminobutyric acid (GABA) and decreases levels of myoinositol in the central nervous system[9]. Because tesamorelin cost is substantially less than that of leading Alzheimer’s medications and its benefits appear to be equivalent or even superior, it may become a mainstay of treatment if additional research is fruitful.Tesamorelin Cost and Benefit
Tesamorelin cost is not the only benefit the peptide provides. In fact, it is generally considered functionally superior in treating growth hormone deficiency, even over recombinant growth hormone itself. As a treatment for HIV-associated lipodystrophy, tesamorelin is a game changer for many patients.Because it mimics natural physiological control, tesamorelin is safe and simple to use with almost no risk of overdose. Low tesamorelin cost is simply a benefit on top of the peptide’s already impressive properties. The tesamorelin cost to benefit equation tilts heavily in favor of benefit, thereby making it a common choice for research protocols and studies of the effects of growth hormone releasing hormone in many biological settings.
Resources
[1]V. Glaser, “Reducing the Cost of Peptide Synthesis,” GEN - Genetic Engineering and Biotechnology News, Jul. 01, 2013. https://www.genengnews.com/magazine/206/reducing-t... (accessed Apr. 07, 2022).[2]Clinical Review Report: Tesamorelin (Egrifta). Ottawa (ON): Canadian Agency for Drugs and Technologies in Health, 2016. Accessed: Apr. 06, 2022. [Online]. Available: http://www.ncbi.nlm.nih.gov/books/NBK539131/
[3]A. Mangili, J. Falutz, J.-C. Mamputu, M. Stepanians, and B. Hayward, “Predictors of Treatment Response to Tesamorelin, a Growth Hormone-Releasing Factor Analog, in HIV-Infected Patients with Excess Abdominal Fat,” PLoS ONE, vol. 10, no. 10, p. e0140358, Oct. 2015, doi: 10.1371/journal.pone.0140358.
[4]J. E. Lake et al., “Tesamorelin improves fat quality independent of changes in fat quantity,” AIDS Lond. Engl., vol. 35, no. 9, pp. 1395–1402, Jul. 2021, doi: 10.1097/QAD.0000000000002897.
[5]C. R. Rowan, J. McManus, K. Boland, and A. O’Toole, “Visceral adiposity and inflammatory bowel disease,” Int. J. Colorectal Dis., vol. 36, no. 11, pp. 2305–2319, Nov. 2021, doi: 10.1007/s00384-021-03968-w.
[6]Y. Li et al., “Visceral fat area is associated with a high risk for early postoperative recurrence in Crohn’s disease,” Colorectal Dis. Off. J. Assoc. Coloproctology G. B. Irel., vol. 17, no. 3, pp. 225–234, Mar. 2015, doi: 10.1111/codi.12798.
[7]D. Q. Holt, G. T. Moore, B. J. G. Strauss, A. L. Hamilton, P. De Cruz, and M. A. Kamm, “Visceral adiposity predicts post-operative Crohn’s disease recurrence,” Aliment. Pharmacol. Ther., vol. 45, no. 9, pp. 1255–1264, May 2017, doi: 10.1111/apt.14018.
