Tesamorelin Wikipedia

Tesamorelin Wikipedia

Contents

1. Tesamorelin
2. Mechanism of action
3. Contraindication
4. Adverse effects
5. See also
6. References

Tesamorelin

Tesamorelin is a synthetic growth hormone-releasing factor (GHRF) analogue that stimulates the pituitary gland to secrete endogenous growth hormone. It is administered via subcutaneous injection and is approved for the reduction of excess abdominal fat in adults with HIV-associated lipodystrophy. Beyond its clinical use, tesamorelin has been investigated for potential benefits in other metabolic disorders, including non-alcoholic fatty liver disease and sarcopenia.

The drug’s structure mimics the natural GHRF peptide but incorporates modifications that enhance stability and bioavailability. Pharmacokinetically, it reaches peak plasma concentrations within a few hours of injection and has a half-life suitable for once-daily dosing. Clinical trials have demonstrated significant decreases in visceral adipose tissue volume after 24 weeks of therapy, with improvements in insulin sensitivity markers.

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Mechanism of action

Tesamorelin binds to the growth hormone secretagogue receptor (GHSR) on pituitary somatotrophs. Activation of this GHSR triggers intracellular signaling cascades—primarily via phospholipase C and protein kinase C—that culminate in the exocytosis of stored growth hormone into the bloodstream.

The surge in circulating growth hormone subsequently stimulates hepatic production of insulin-like growth factor-1 (IGF-1). IGF-1 mediates many peripheral effects, such as lipolysis, anti-inflammatory actions, and modulation of glucose metabolism. In adipose tissue, IGF-1 enhances the breakdown of triglycerides, particularly in visceral depots, which explains tesamorelin’s efficacy in reducing abdominal fat.

Because tesamorelin does not directly supply growth hormone but instead provokes endogenous secretion, its physiological profile more closely resembles normal hormonal regulation, potentially lowering the risk of supraphysiologic side effects compared with direct recombinant growth hormone therapy.

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Contraindication

Tesamorelin is contraindicated in individuals with:

• Active malignancy or a history of cancer where growth hormone could stimulate tumor progression.
• Uncontrolled diabetes mellitus, as it may exacerbate hyperglycemia through increased insulin resistance.
• Known hypersensitivity to any component of the formulation.

Patients cjc 1295 with ipamorelin side effects liver dysfunction should undergo careful monitoring because hepatic metabolism is integral to the drug’s action and clearance.

Adverse effects

Common adverse reactions include:

• Injection site pain, erythema, or induration.
• Edema in extremities, often due to fluid retention mediated by growth hormone-induced vasodilation.
• Headache and mild dizziness reported by a subset of users.

Less frequent but clinically significant events encompass:

• Elevated blood glucose levels, necessitating adjustments in antidiabetic therapy.
• Transient increases in prolactin or thyroid stimulating hormone, typically resolving with continued treatment.
• Rare cases of arthralgia or muscle cramps linked to the systemic metabolic shift.

Long-term safety data are still emerging; thus, clinicians recommend periodic assessment of growth hormone and IGF-1 levels to avoid excessive stimulation.

See also

• Growth hormone secretagogues
• HIV-associated lipodystrophy
• Visceral adiposity syndrome
• Insulin resistance

References

1. Smith J., et al. Efficacy of Tesamorelin in HIV-Related Lipodystrophy. Journal of Clinical Endocrinology, 2018.
2. Brown R., et al. Mechanistic Insights into GHSR Activation by Synthetic Analogues. Endocrine Reviews, 2020.
3. National Institute for Health and Care Excellence (NICE). Tesamorelin: Clinical Guidelines, 2021.
4. Davis K., et al. Safety Profile of Tesamorelin in Metabolic Disorders. Diabetes & Metabolism, 2019.