Tesamorelin
Tesamorelin (Egrifta)
Tesamorelin is a synthetic analogue of growth hormone-releasing hormone (GHRH) consisting of the full 44-amino acid sequence of endogenous GHRH with a trans-3-hexenoic acid modification at the N-terminus that enhances stability. It is FDA-approved (brand name Egrifta) specifically for the reduction of excess abdominal fat (lipodystrophy) in HIV-infected patients on antiretroviral therapy, and is also investigated off-label for cognitive enhancement and body composition improvement in aging adults.
Mechanism of Action
Tesamorelin binds to and activates GHRH receptors on somatotroph cells in the anterior pituitary, stimulating the pulsatile release of endogenous growth hormone (GH) in a physiologically regulated manner. The resultant increase in GH and downstream IGF-1 promotes lipolysis in visceral adipose tissue, reduces lipogenesis, and may exert neuroprotective effects by enhancing insulin-like growth factor signaling in the brain. Unlike exogenous GH administration, tesamorelin preserves the natural feedback mechanisms of the hypothalamic-pituitary axis, reducing the risk of GH-axis suppression.
Evidence by Health Goal(14 goals)
Dosing Protocols
Morning, on an empty stomach or at least 30 minutes before eating, administered subcutaneously into the abdomen
Cycle: Continuous use assessed at 26 weeks per FDA labeling; off-label users often cycle 3-6 months on, 1-2 months off
Reconstitute lyophilized powder with supplied sterile water; rotate injection sites within the abdominal region; do not inject into scar tissue, bruises, or the navel. Some off-label protocols use 1mg/day to reduce cost and side effect burden while maintaining partial efficacy.
Safety & Side Effects
Tesamorelin is an FDA-approved prescription peptide with a well-characterized safety profile from randomized controlled trials, but it requires monitoring of IGF-1 levels, fasting glucose, and HbA1c due to its glucose-elevating potential; it is contraindicated in active malignancy, pituitary pathology, pregnancy, and in patients with hypersensitivity to GHRH. Off-label use outside supervised medical care carries risks of unsupervised IGF-1 elevation and metabolic dysregulation.
Possible Side Effects
- !Injection site reactions including erythema, pruritus, pain, and induration (most common, reported in up to 25% of users)
- !Peripheral edema and fluid retention, particularly in the extremities
- !Arthralgia and joint stiffness, especially in the hands and wrists
- !Myalgia and musculoskeletal discomfort
- !Elevated fasting blood glucose and insulin resistance (clinically significant in pre-diabetic individuals)
- !Carpal tunnel syndrome with prolonged use
- !Nausea, vomiting, or upper abdominal discomfort
- !Potential stimulation of IGF-1-dependent tissue growth; theoretical concern for promotion of pre-existing malignancies
Interactions
- -May antagonize the glucose-lowering effects of insulin and oral antidiabetic agents, requiring dose adjustments in diabetic patients
- -Glucocorticoids (e.g., prednisone, dexamethasone) attenuate GHRH signaling and may significantly reduce tesamorelin efficacy
- -May alter the clearance of drugs metabolized by CYP450 enzymes as GH and IGF-1 modulate hepatic enzyme activity
- -Concurrent use with other GH secretagogues (e.g., ipamorelin, MK-677) may produce additive IGF-1 elevation and amplify side effect risk
- -Estrogen replacement therapy may reduce hepatic GH sensitivity, potentially blunting IGF-1 response to tesamorelin
Cost & Where to Buy
FDA-approved Egrifta brand can exceed $3,000/month through US pharmacies before insurance; research-grade tesamorelin from peptide vendors ranges $80-$400/month at 2mg/day dosing depending on vendor quality and quantity purchased. Prescription coverage for HIV-associated lipodystrophy may reduce out-of-pocket costs substantially through manufacturer assistance programs.
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