Tesamorelin

Tesamorelin acts as an agonist of the GHRH receptor in the anterior pituitary gland.

• GH stimulation: It binds to the GHRH receptor, activating the cAMP signaling pathway, which induces the synthesis and pulsatile release of growth hormone.
• IGF-1 increase: The released GH stimulates hepatic and peripheral production of insulin-like growth factor type 1 (IGF-1), mediating many of its anabolic and lipolytic effects.
• Lipolysis: GH and IGF-1 promote the mobilization of fatty acids from visceral adipose tissue, reducing abdominal fat.
• Metabolic effect: It improves insulin sensitivity and reduces triglycerides, although it may transiently elevate blood glucose.

• HIV-associated lipodystrophy: Reduction of excess visceral fat in HIV patients receiving antiretroviral therapy.
• Obesity and metabolic syndrome: Investigated to decrease abdominal fat and improve metabolic parameters.
• Sarcopenia: Potential to increase muscle mass and strength in elderly or cachectic patients.
• Aging: Studied for its effects on body composition and cognitive function in older adults.

Tesamorelin produces a significant reduction in visceral fat (measured by computed tomography) and an improvement in lipid profile, with decreased triglycerides. It may also increase lean mass and improve quality of life in patients with lipodystrophy. However, it does not reduce peripheral subcutaneous fat and may cause metabolic effects such as transient hyperglycemia.

Contraindicated in patients with active pituitary tumors, active cancer, hypersensitivity to the active substance or any excipients. It should not be used in patients with active bone fractures, uncontrolled proliferative diabetic retinopathy, or intracranial hypertension. The most common adverse effects include pain, erythema, or pruritus at the injection site, arthralgias, myalgias, peripheral edema, and increased blood glucose. Monitoring of IGF-1 and glucose levels is recommended during treatment. It is not approved for use in children or in pregnant or breastfeeding women.

Approved by the FDA in November 2010 for the treatment of HIV-associated lipodystrophy (reduction of excess visceral fat). Also approved by the European Medicines Agency (EMA) in 2011. Not approved for other indications.

The recommended dose is 2 mg administered subcutaneously once daily. It should be injected into the abdomen, rotating injection sites. Treatment duration should not exceed 6 months, although it may be extended based on clinical response and tolerance.

Store under refrigeration between 2°C and 8°C. Do not freeze. Protect from light. Once reconstituted, the solution should be used immediately or may be stored under refrigeration for up to 24 hours. Do not shake vigorously.