Tesamorelin 10mg

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Form: Lyophilized powder
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SKU: P-TESAMRLN-10
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A Guide to Tesamorelin

Lipodystrophy is the irregular distribution and storage of the lipids throughout the body. When people develop this overtime, rather than from birth, it is called acquired lipodystrophy. HIV is one such disorder, which can lead to this ailment.

HIV induced lipodystrophy is characterized by bodily changes in insulin resistance, excessive lipid accumulation and endothelial dysfunction – all of which may be due to the antiretroviral therapy (1).

Several treatment options are available to treat this morbidity and decrease its rate. One such option is peptide treatment, including peptide called Tesamorelin.

Tesamorelin is a synthetic peptide used in the treatment of HIV induced lipodystrophy, approved by the US FDA in 2010 (2).

Introduction

Tesamorelin is a synthetic polypeptide composed of 44 amino acids and analogous to growth hormone releasing hormone (3).

The N-terminus of the compound has been modified compared to growth hormone releasing hormone (GHRH) which leads to improved stability and pharmacokinetics (3). Tesamorelin also goes by its trade (brand) name, called Egrifta (4,5) or simply called TH9507 (10).

History

In the mid-1990s, the highly active antiretroviral therapy (HAART) for HIV patients was introduced and soon became widely used in HIV treatment. Soon after it was noticed that while this therapy dramatically reduced the HIV associated mortality rate, it led to lipodystrophy in the treated patients(6).

After various studies, it was discovered that HIV patients suffering from lipodystrophy had extremely low levels of growth hormone. It was determined that upon increasing the endogenous volumes of growth hormones it may increase fat oxidation and reduce levels of cholesterol. This led to an investigation of the growth hormone axis and its management of fat accumulation, thereby leading to the discovery of Tesamorelin(6).

US FDA Approval History

Theratechnologies Inc., located at Montreal, Quebec (Canada), submitted a New Drug Application (NDA) to the US FDA in June 2009. Once the US FDA accepted the application, the company progressed with the drug production and development. In November 2010, Egrifta (Tesamorelin for injection) was approved by the US FDA – the first and only approved treatment of HIV induced lipodystrophy at the time (5).

Functioning of Tesamorelin

Tesamorelin activates the growth hormone releasing hormones (GHRH) receptors located at the anterior pituitary gland, which leads to increased production and secretion of growth hormones in the body. The growth hormones then act on several bodily cells, including hepatocytes, which then stimulate the synthesis of insulin like growth factor-1 (IGF-1) (3).

Analogous to GH, IGF-1 also stimulates growth, inhibits programmed cell death, glucose reduction and lipolysis (3).

HIV patients with lipodystrophy have low levels of GH and IGF-1. With Tesamorelin treatment, this can be altered, and lipid metabolism and accumulation in the body can be managed effectively.

As mentioned earlier, the N-terminus of the molecule is altered in Tesamorelin, compared to the natural GHRH. Owing to this, the peptide is highly stable and more resistant to the enzyme deactivation than the natural GHRH (7).

Benefits of Tesamorelin

Tesamorelin is widely used in the treatment of lipodystrophy, mainly in treating the excess fat in the abdominal region (8), in HIV infected patients.

Recent studies (9) have also shown that the peptide may also be used for the treatment of non-alcoholic fatty liver disease (NAFLD) in patients with HIV.

Tesamorelin Clinical studies

Tesamorelin for HIV Patients with Lipodystrophy

In this study (10), two phase III studies were conducted with 806 patients over a period of 26 weeks, followed by another 26-week extension.

806 HIV patients treated with antiretroviral therapy and having excessive abdominal fat were entered in this study. They were divided into two groups, one group with 543 patients were treated with 2mg Tesamorelin and remaining 263 patients were treated with placebo, both given subcutaneously for a period of 26 weeks. After this duration, the Tesamorelin treated patients were again randomly divided into 2 groups, in which half continued with Tesamorelin 2mg treatment and the other half were given placebo, for another period of 26 weeks.

At week 26, it was noticed that there was a significant decrease in visceral adipose tissue level amongst the Tesamorelin treated patients, by at least 15.4%. Additionally, the levels of triglycerides and cholesterol decreased significantly compared to the placebo treatment. Overall body image also improved. The same levels were maintained in week 52 in the patients who were continued with peptide treatment.

This study demonstrated that Tesamorelin led to visceral fat reduction for up to 52 weeks, with no adverse events reported in patients, concluding Tesamorelin is otherwise highly effective and well tolerated in humans.

Tesamorelin for HIV Patients with NAFLD Syndrome

One of the most common comorbidities in HIV patients is liver disorder, where non-alcoholic fatty liver disease (NAFLD) occurs in almost 40% of the HIV patients (11).

In this study (9), 61 men and women suffering from HIV and with a high hepatic fat fraction (HFF) were selected as per the protocol. These subjects were then treated with a daily dose of 2mg Tesamorelin and identical placebo for a duration of 12 months. The rate of HFF was monitored at the end of the trial.

After 12 months, it was noticed that 35% of subjects treated with Tesamorelin showed reduction in HFF rate by less than 5% vs. only 4% of subjects receiving placebo showed HFF reduction. There was no alteration in the glucose levels. The only side effects reported by the subjects were pain or discomfort at the injection site.

This demonstrated that Tesamorelin may be a potential therapeutic agent in treating NAFLD in patients living with HIV syndrome.

Tesamorelin for HIV Patients with Cognition Issues

In this study (12), aged HIV patients suffering from mild cognitive impairment were selected. The main motto of this study was to determine whether Tesamorelin, in conjunction with a text messaging app, would help improve memory functions in HIV patients.

100 subjects, aged more than 40 years, participated in this trial and underwent Tesamorelin treatment where 1.4mg peptide dose was administered daily for a period of 6 months, followed by no treatment for the next 6 months, and then again 1.4 mg dose of Tesamorelin was administered once a day for another 6 months.

The primary outcome of this study was that there was a change in neurocognitive performance measured by the Global Deficit Score (GDS) after the period of 6 and 12 months. This study is underway and final results are yet to be posted.

There is some potential scope for Tesamorelin to be used as a therapeutic agent in treating HIV induced cognitive impairment.

Tesamorelin for Diabetes

The main aim of this study (13) was to find if Tesamorelin would alter insulin sensitivity and assist in the management and control of diabetes.

53 patients suffering from Type II diabetes were enrolled in this 12-week randomized trial. The patients were divided into three treatment groups of placebo, 1 mg, and 2 mg doses of Tesamorelin.

After the period of 12 weeks, the concentration of fasting glucose, glycosylated hemoglobin and diabetes control was measured. There was no significant reduction in either of these parameters. The results of all three treatment groups were indifferent. Thus, this study demonstrated that unlike other GHRH peptides, Tesamorelin is not as efficacious in altering insulin sensitivity and controlling diabetes.

Tesamorelin Side Effects

The reported side effects of the peptide are as follows (8).

Common side effects are:

  • Muscle pain and stiffness
  • Pain in arms, legs, and joints
  • Pain or discomfort at the injection site

Relatively less common side effects are:

  • Headache
  • Burning, tingling pain in all fingers except the smallest one
  • Chest pain
  • Headache and dizziness
  • Arrhythmia
  • Nervousness, awkwardness, irritability
  • Blurred vision and pounding in the ears
  • Nausea, vomiting

Contraindications

Tesamorelin is contraindicated in patients suffering from the following (14):

  • Patients who underwent surgery that caused disruption in hypothalamic pituitary axis
  • Malignant tumors
  • Hypersensitivity toward either Tesamorelin or any of the ingredients in the medication
  • Pregnancy and breastfeeding
  • Precautions must be taken while considering Tesamorelin treatment on patients with benign (non-malignant) neoplasms

Adverse Effects with Tesamorelin

Below listed are potential adverse effects reported in some patients on treatment with Tesamorelin (14):

  • High levels of IGF-1
  • Excessive fluid retention or swelling
  • Glucose intolerance
  • Hypersensitivity reactions such as erythema, flushing, and rashes
  • Drug interactions
  • Simvastatin

Simvastatin is metabolized in the body by CYP450 cytochrome. It is reported that growth hormones alter the CYP50 mediated clearance in humans. Since Tesamorelin induces secretion of growth hormones, it may affect the metabolism of Simvastatin. It is hence recommended to avoid co-administration of the two, or atleast continuously monitor the metabolism of Simvastatin (14).

Cortisone Acetate and Prednisone

Growth hormone inhibits the enzyme called 11beta-hydroxysteroid dehydrogenase type I. This enzyme is responsible for the conversion of cortisone into its active metabolite, cortisol. Since Tesamorelin induces a release of growth hormones, it may interfere in the functioning of cortisone acetate and prednisone medications. Hence, it is recommended to avoid co-administering these medications at the same time (14).

Recommended Dosage and Administration

The recommended dose of Tesamorelin is 2mg per day via subcutaneous route of administration (14).

Tesamorelin is available in powder for reconstitution form, where 1mg powder of the peptide is to be reconstituted with the diluent namely sterile water for injection (14).

Peptide Storage and Handling

Tesamorelin peptide is available in sterile, lyophilized powder form, which must be administered immediately after reconstitution with sterile water (15).

The powder must be stored away from light, in the refrigerator, in its original container. Whereas, the other container with the sterile water, needles and syringes can be stored at room temperature, away from heat and moisture (15).

Conclusion

Tesamorelin is a highly potent growth polypeptide, composed of 44 amino acids and is analogous to the naturally occurring growth hormone releasing hormone (GHRH).

Tesamorelin mainly acts by stimulating the GHRH receptors located in the pituitary gland. Once stimulated, these receptors produce and release growth hormones (GH) which then also lead to the synthesis of IGF-1. Both GH and IGF-1 stimulate lipolysis and metabolism of lipids in the body, especially the abdominal region.

Tesamorelin is the first and only peptide treatment for HIV induced lipodystrophy and is the potential therapeutic agent in the treatment of HIV induced liver disorder (namely NAFLD liver disease) and mild cognitive impairment.

This peptide has been approved by the US FDA since 2010 and has been widely used ever since. Tesamorelin, a sterile medication, is available for various platforms and is available for prescription use only.

While many studies and research data are available to demonstrate peptide efficacy, trials continue to be conducted to explore the full utilization of this peptide as a therapeutic agent.

References:

1.Guzman N, Vijayan V. HIV-associated Lipodystrophy. [Updated 2021 May 12]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2021 Jan. https://www.ncbi.nlm.nih.gov/books/NBK493183/

2.Chemistry review(s), application number: 22-505. Center for Drug evaluation and research. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022505Orig1s000ChemR.pdf

3.Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Tesamorelin. [Updated 2018 Oct 20]. https://www.ncbi.nlm.nih.gov/books/NBK548730/

4.National Center for Biotechnology Information. "PubChem Compound Summary for CID 16137828, Egrifta" PubChem, https://pubchem.ncbi.nlm.nih.gov/compound/Egrifta

5.Egrifta FDA Approval History. https://www.drugs.com/history/egrifta.html

6.Bedimo, Roger. “Growth hormone and tesamorelin in the management of HIV-associated lipodystrophy.” HIV/AIDS (Auckland, N.Z.) vol. 3 (2011): 69-79. doi:10.2147/HIV.S14561. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3218714/

7.Ferdinandi ES, Brazeau P, High K, Procter B, Fennell S, Dubreuil P. Non-clinical pharmacology and safety evaluation of TH9507, a human growth hormone-releasing factor analogue. Basic Clin Pharmacol Toxicol. 2007 Jan;100(1):49-58. doi: 10.1111/j.1742-7843.2007.00008.x. PMID: 17214611. https://pubmed.ncbi.nlm.nih.gov/17214611/

8.Tesamorelin (Subcutaneous Route). https://www.mayoclinic.org/drugs-supplements/tesamorelin-subcutaneous-route/

9.Stanley, T. L., Fourman, L. T., Feldpausch, M. N., Purdy, J., Zheng, I., Pan, C. S., Aepfelbacher, J., Buckless, C., Tsao, A., Kellogg, A., Branch, K., Lee, H., Liu, C. Y., Corey, K. E., Chung, R. T., Torriani, M., Kleiner, D. E., Hadigan, C. M., & Grinspoon, S. K. (2019). Effects of tesamorelin on non-alcoholic fatty liver disease in HIV: a randomised, double-blind, multicentre trial. The lancet. HIV, 6(12), e821–e830. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6981288/

10.Falutz J, Mamputu JC, Potvin D, Moyle G, Soulban G, Loughrey H, Marsolais C, Turner R, Grinspoon S. Effects of tesamorelin (TH9507), a growth hormone-releasing factor analog, in human immunodeficiency virus-infected patients with excess abdominal fat: a pooled analysis of two multicenter, double-blind placebo-controlled phase 3 trials with safety extension data. J Clin Endocrinol Metab. 2010 Sep;95(9):4291-304. doi: 10.1210/jc.2010-0490. Epub 2010 Jun 16. PMID: 20554713. https://pubmed.ncbi.nlm.nih.gov/20554713/

11.Tesamorelin Effects on Liver Fat and Histology in HIV. https://clinicaltrials.gov/ct2/show/NCT02196831

12.Phase II Trial of Tesamorelin for Cognition in Aging HIV-Infected Persons. https://clinicaltrials.gov/ct2/show/record/NCT02572323

13.Clemmons, D. R., Miller, S., & Mamputu, J. C. (2017). Safety and metabolic effects of tesamorelin, a growth hormone-releasing factor analogue, in patients with type 2 diabetes: A randomized, placebo-controlled trial. PloS one, 12(6), e0179538. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5472315/

14.Tesamorelin label and prescribing information. https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022505s000lbl.pdf

15.Tesamorelin injection. https://medlineplus.gov/druginfo/meds/a611035.html


 

Tesamorelin Peptide in the News

According to the paper published in Nature.com in Oct 2020, a number of studies demonstrated that GHRH exerts a variety of bioactivities due to its wide distribution and autocrine/paracrine mechanisms. And they concluded that GHRH and its analogs, including Tesamorelin, have been developed as potential therapeutic agents to treat diabetes, cancers, and cardiovascular diseases.
https://www.nature.com/articles/s41467-020-18945-0

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