Description

Product Summary – Tesamoreln 10 mg

Field	Details
Product Name	Tesamoreln
Category	Synthetic growth hormone–releasing hormone (GHRH/GRF) analog; peptide drug for HIV-associated abdominal lipodystrophy
Length	44 amino acids
Amino Acid Sequence	N-terminal hexenoyl–Tyr-Ala-Asp-Gly-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu-NH₂
Molecular Formula	C₂₂₁H₃₆₆N₇₂O₆₇S (free base; acetate salt in marketed product)
Molecular Weight	≈ 5135.9 Da (free base equivalent)
Form & Purity	Sterile lyophilized powder for injection; preservative-free; supplied in single-use vials (EGRIFTA SV: 2 mg; EGRIFTA WR: 11.6 mg). Reconstitute with sterile water; ≥95% purity (HPLC, vendor spec).
Storage	Store vials refrigerated (2–8 °C); protect from light. Do not store the reconstituted solution; inject immediately after mixing.
Typical Dose	– EGRIFTA SV: 1.4 mg SC once daily (from 2 mg vial) – EGRIFTA WR: 1.28 mg SC once daily (from 11.6 mg vial)
Key Mechanisms	– Stimulates pituitary GHRH receptors → increases endogenous GH secretion – Elevates IGF-1 transiently – Promotes lipolysis and preferential reduction of visceral adipose tissue (VAT) – Improves some lipid and adipokine profiles
Research / Clinical Use Cases	– FDA-approved: reduction of excess abdominal VAT in HIV-infected adults with lipodystrophy – Investigational: hepatic steatosis/NAFLD (trials show reduced liver fat and slower fibrosis progression), metabolic markers, body-composition studies
Common AEs / Safety Signals	– Injection-site reactions (pain, redness, pruritus) – Peripheral edema, arthralgia, carpal tunnel symptoms – Hyperglycemia or worsened glucose tolerance – Hypersensitivity (rash, urticaria) – Elevated IGF-1 (monitor regularly)
Contraindications / Warnings	– Active malignancy – Known hypersensitivity to tesamoreln or components – Pregnancy – Use caution in diabetes, glucose intolerance, and in patients with a disrupted hypothalamic–pituitary axis
Compliance	FDA approved (2010; updated formulations 2019–2023) for – HIV-associated abdominal lipodystrophy – Not approved for general obesity or weight loss – Prescription-only; follow formulation-specific label guidance. But the drug we have can be used for research purposes only

Mechanism of Action of Tesamoreln

Receptor Binding and Signal Transduction

Tesamoreln is a GHRH analog that binds to the GHRH receptor (GHRHR) and causes the release of acute GH secretion and long-term upregulation of GH gene transcription. Some contexts explain further modulation of GH release due to GHRHR signaling effect on nitric oxide synthase and calcium-mediated pathways. [1]

Physiological Modulation of GH Pulsatility

Tesamoreln preserves the physiological rhythm of GH release by inducing the rapid GH pulses, leaving somatostatin-mediated inhibitory control intact. This rhythmic excursion is similar to the endogenous patterns.

Insulin-like growth factor-1 (IGF-1), released due to GH’s effect on the liver, has a negative feedback mechanism to both the hypothalamus and pituitary to maintain the homeostatic regulation of the GH-IGF axis during chronic therapy. [2]

Adipose Tissue Effects and Visceral Fat Reduction

Tesamoreln preferentially reduces the visceral adipose tissue (VAT). GH release because of tesamoreln activates the hormone-sensitive lipase and adipose triglyceride lipase and suppresses the lipoprotein lipase activity to shift the adipocyte metabolism towards the triglyceride mobilization. [3]

VAT deposits are more sensitive to GH because of their depot-specific receptor density, vascular supply, and adipokine signaling. The selective lipolysis of tesamoreln in which reduces the VAT and relatively preserves the subcutaneous fat, improves the body composition and metabolic markers such as triglycerides and non-HDL cholesterol.

Hepatic Lipid Metabolism and NAFLD Improvement

Tesamoreln, through its GH, IGF-1 signaling, increases fatty acid oxidation, suppresses the de novo lipogenesis, and decreases the portal free fatty acid flux due to long-term reduction in VAT. Due to these effects of tesamoreln, it reduces the triglyceride content and improves the non-alcoholic fatty liver disease (NAFLD). [4]

Effects on Muscle and Systemic Substrate Handling

Some studies have observed the anabolic effects of tesamoreln due to its insulin antagonistic properties, which lead to decreased insulin-stimulated glucose uptake in muscles and adipose tissues. Tesamoreln improves the skeletal muscle composition by increasing protein synthesis and reducing intracellular lipid infiltration. [5]

Tolerability and Safety Considerations of Tesamoreln

Generally well tolerated in clinical trials.
The most common adverse events may be the injection site reactions, arthralgia, myalgia, and edema.
Can increase IGF-1 levels.
Contraindicated in patients with active malignancy.
Long-term safety data demonstrate sustained efficacy; however, vigilance is necessary regarding the risk of neoplasia.
FDA-approved for HIV-associated lipodystrophy; use outside this indication is investigational.

Citations

Halmos, G., Szabo, Z., Dobos, N., Juhasz, E., & Schally, A. V. (2025). Growth hormone-releasing hormone receptor (GHRH-R) and its signaling. Reviews in endocrine & metabolic disorders, 26(3), 343–352. https://doi.org/10.1007/s11154-025-09952-x
Olarescu NC, Gunawardane K, Hanson TK, et al. Normal Physiology of Growth Hormone in Normal Adults. [Updated 2025 Apr 18]. In: Feingold KR, Ahmed SF, Anawalt B, et al., editors. Endotext [Internet]. South Dartmouth (MA): MDText.com, Inc.; 2000-. Available from: https://www.ncbi.nlm.nih.gov/books/NBK279056/
Kopchick, J. J., Berryman, D. E., Puri, V., Lee, K. Y., & L Jørgensen, J. O. (2019). The effects of growth hormone on adipose tissue: Old observations, new mechanisms. Nature Reviews. Endocrinology, 16(3), 135. https://doi.org/10.1038/s41574-019-0280-9
Kopchick, J. J., Berryman, D. E., Puri, V., Lee, K. Y., & L Jørgensen, J. O. (2019). The effects of growth hormone on adipose tissue: Old observations, new mechanisms. Nature Reviews. Endocrinology, 16(3), 135. https://doi.org/10.1038/s41574-019-0280-9
Lake, J. E., La, K., Erlandson, K. M., Adrian, S., Yenokyan, G., Scherzinger, A., Dubé, M. P., Stanley, T., Grinspoon, S., Falutz, J., Mamputu, J. C., Marsolais, C., McComsey, G. A., & Brown, T. T. (2021). Tesamoreln improves fat quality independent of changes in fat quantity. AIDS (London, England), 35(9), 1395–1402. https://doi.org/10.1097/QAD.