Tesamorelin
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Product Description
Tesamorelin is a synthetic peptide analog of the hypothalamic peptide Growth Hormone-Releasing Hormone (GHRH), specifically designed to reduce excess abdominal fat in HIV-infected patients with lipodystrophy. This condition is characterized by metabolic abnormalities such as insulin resistance, fat redistribution, and hyperlipidemia, often associated with antiretroviral therapy. Tesamorelin, consisting of the first 44 amino acids of human GHRH with modifications to enhance stability, stimulates the release of growth hormone, which in turn promotes lipolysis and reduces visceral adipose tissue. Studies have shown its efficacy in reducing liver fat in HIV patients with non-alcoholic fatty liver disease (NAFLD), potentially slowing fibrosis progression. Additionally, tesamorelin has demonstrated cognitive benefits in older adults with mild cognitive impairment (MCI) and healthy aging, improving executive function and verbal memory.
Primary Clinical Use
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Treatment of Excess Abdominal Fat (Lipodystrophy) in HIV-Patients: Approved to reduce excess visceral abdominal fat in HIV-infected patients with lipodystrophy.
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Mechanism of Action:
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Binds to GHRH receptors in the pituitary gland.
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Stimulates pulsatile release of endogenous Growth Hormone (GH).
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GH acts on fat cells, promoting lipolysis and reducing visceral fat tissue.
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Mechanism of Action
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Binds to GHRH receptors in the anterior pituitary gland.
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Stimulates the natural release of growth hormone (GH), which elevates IGF-1 (insulin-like growth factor 1) levels.
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Enhances lipolysis and reduces visceral fat, particularly in the abdomen.
Clinical Use
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Indication: Reduction of excess abdominal fat in HIV-infected patients with lipodystrophy.
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Administration: Subcutaneous injection, 2 mg once daily.
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Brand Name: Egrifta®.
Side Effects / Considerations
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Common Side Effects: Injection-site reactions, arthralgia, edema, myalgia.
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IGF-1 Increase: May raise theoretical risk of neoplasia in susceptible individuals.
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Contraindications: Active malignancy.
Structural and Functional Interpretation of the Formula
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Carbon (C₂₂₁) & Hydrogen (H₃₆₆): Indicate a large, complex organic molecule with a backbone and side chains of amino acids.
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Nitrogen (N₇₂): High nitrogen count is characteristic of peptides, indicating the presence of amino groups and peptide bonds.
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Oxygen (O₆₇): Found in carboxyl groups, peptide bonds, and side chains of specific amino acids.
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Sulfur (S): Indicates the presence of at least one amino acid with a sulfur-containing side chain, such as Methionine.
What is Tesamorelin?
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Synthetic Peptide: Tesamorelin is a synthetic peptide designed in a laboratory, modified from the first 44 amino acids of the human Growth Hormone-Releasing Hormone (GHRH).
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Natural GHRH (1-44): Produced by the hypothalamus, stimulates the pituitary gland to produce and release Growth Hormone (GH).
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Tesamorelin (Modification): Replaces the first amino acid (L-Alanine) with L-Tyrosine and adds a trans-3-hexenoic acid group to the N-terminus to enhance stability and potency.
Key Characteristics Summary
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Chemical Nature: Synthetic 44-amino acid peptide analog of GHRH.
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Mechanism: GHRH receptor agonist.
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Primary Effect: Stimulates endogenous pulsatile release of Growth Hormone.
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Clinical Use: Reduction of excess visceral abdominal fat in HIV-associated lipodystrophy.
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Trade Name: Egrifta SV® (subcutaneous injection).
Detailed Information
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Molecular Weight: Approximately 5135.86 g/mol.
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Structure: Consists of the entire 44-amino-acid sequence of human GHRH with a trans-3-hexenoic acid group added to the N-terminal tyrosine residue.
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Administration: Daily subcutaneous injection.
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Brand Name: Egrifta® (by Theratechnologies / EMD Serono).
Safety Information
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Regulation:
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Pharmaceutical-Grade: FDA-approved and manufactured under cGMP.
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Research-Grade: Unregulated for human use; intended for laboratory study.
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Quality Control:
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Pharmaceutical-Grade: Extensive testing for purity, potency, and contaminants, including microbial and other impurities.
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Research-Grade: Varies by supplier; may include HPLC purity verification, but lacks rigorous checks for contaminants.
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Intended Use:
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Pharmaceutical-Grade: Therapeutic use in humans under medical supervision.
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Research-Grade: Non-clinical laboratory applications only.
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Storage:
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Pharmaceutical-Grade: Specific storage instructions for the lyophilized powder and diluent are provided to maintain stability.
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Research-Grade: Proper storage is still required, but stability testing is less rigorous.
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