Tesamorelin

Summary

Tesamorelin (Egrifta) is an FDA-approved GHRH analogue indicated for the reduction of excess abdominal fat (lipodystrophy) in HIV-infected adults on antiretroviral therapy. It works by stimulating endogenous GH secretion rather than directly replacing GH, preserving physiological pulsatility. It has also been investigated for cognitive benefits in older adults and non-alcoholic fatty liver disease (NAFLD).

Mechanism of Action

Tesamorelin is a synthetic analogue of endogenous GHRH that binds to GHRH receptors in the anterior pituitary, stimulating the synthesis and pulsatile release of endogenous growth hormone (GH), which in turn increases IGF-1 levels and promotes lipolysis.

Routes of Administration

Goals & Uses

• Improvement of lipid profileCardiovascular / MetabolicModerate
• Reduction of non-alcoholic fatty liver disease (NAFLD/NASH)Hepatic / MetabolicLow
• General anti-aging / GH optimizationWellness / Off LabelLow
• Lean body mass preservationBody CompositionModerate
• Reduction of HIV-associated lipodystrophy (visceral adiposity)Metabolic / Body CompositionHigh
• Cognitive function improvement in older adultsNeurocognitiveModerate

Contraindications

• Active malignancyOncologyHighUse caution or avoid depending on agent and context
• Disruption of hypothalamic-pituitary axis (e.g., pituitary tumor, head trauma, cranial irradiation)EndocrineHigh
• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• Diabetic retinopathyOphthalmologyModerate
• Hypersensitivity to tesamorelin or mannitolAllergic / ImmunologicHigh

Adverse Effects

• Fluid retention / peripheral edemaCardiovascularCommon
• Carpal tunnel syndromeMusculoskeletalUncommon
• Hypersensitivity reactions (rash, urticaria)ImmunologicUncommon
• Hyperglycemia / glucose intoleranceMetabolic / EndocrineUncommon
• Arthralgia / myalgiaMusculoskeletalCommon
• Injection site reactions (erythema, pruritus, pain, induration)Dermatologic / LocalCommon

Drug Interactions

• Glucocorticoids (systemic)Moderate
• Cytochrome P450-metabolized drugs (e.g., cortisol, sex steroids, anticonvulsants)Low
• Somatostatin analogues (octreotide, lanreotide)High
• Antidiabetic medications (insulin, oral hypoglycemics)Moderate

Population Constraints

• Pediatric patientsAgeAbsolute
• Elderly patients (>65 years)AgeRelative
• Patients with diabetes mellitusMetabolicRelative
• Pregnant womenReproductiveAbsolute
• Patients with renal or hepatic impairmentOrgan FunctionRelative

Regulatory Status

• European UnionUnapprovedNot approved by EMA as of last review; regulatory pathway not pursued in the EU.
• United StatesApprovedApproved: Reduction of excess abdominal fat in HIV-infected patients with lipodystrophyFDA approved November 2010 (Egrifta); reformulated version Egrifta SV approved 2019. Prescription-only.
• United KingdomUnapprovedNot approved by MHRA; available only through named-patient or special access schemes if at all.

FDA-approved in 2010 for HIV-associated lipodystrophy. Not approved for general obesity, anti-aging, or bodybuilding purposes. Classified as a prescription drug in the US. Schedule status varies; not a controlled substance but subject to REMS considerations in some contexts.

Evidence & Sources

No sources recorded yet.