Tesamorelin is a synthetic analogue of human growth hormone releasing hormone (1-44), stabilised by a trans-3-hexenoyl modification at the N-terminus. It is approved by the FDA as Egrifta for the reduction of excess visceral adipose tissue in adults with HIV-associated lipodystrophy, supported by two Phase III randomised placebo-controlled trials that demonstrated a consistent and specific reduction in visceral rather than subcutaneous fat. Later investigator-led work has examined its effect on hepatic fat in non-alcoholic fatty liver disease, with positive findings, and separate work has explored cognitive endpoints. It is therefore among the strongest evidence positions in this range – with the important qualification that the evidence is specific to a defined clinical population, and that use outside that population is off-label.
Active Compound: Tesamorelin (trans-3-hexenoyl-GHRH 1-44 analogue)
Permitted Claim GuidelinesA GHRH analogue approved in the United States for a specific licensed indication. Supplied on prescription for practitioner-directed use.
Mechanism of ActionBinds the GHRH receptor on anterior pituitary somatotrophs, stimulating pulsatile endogenous growth hormone release and consequent hepatic IGF-1 production. Growth hormone promotes lipolysis in visceral adipose tissue preferentially over subcutaneous depots, which accounts for the specificity of the observed effect.
Evidence Grade: A - FDA-approved with Phase III evidence in the licensed population
Clinical Evidence BaseTwo Phase III randomised placebo-controlled trials in HIV-associated lipodystrophy demonstrated significant reduction in visceral adipose tissue, supporting FDA approval. Subsequent randomised trials reported reduction in hepatic fat and slowed fibrosis progression in NAFLD. Evidence in the general population without lipodystrophy is limited.
Literature & ReferencesFalutz J et al. N Engl J Med, 2007 - tesamorelin and visceral adipose tissue in HIV-associated lipodystrophy. | Falutz J et al. J Acquir Immune Defic Syndr, 2010 - Phase III long-term efficacy and safety. | Stanley TL et al. Lancet HIV, 2019 - tesamorelin for hepatic fat in HIV-associated NAFLD. | US FDA prescribing information, Egrifta (tesamorelin for injection).
Safety & PrecautionsAdverse effects reflect growth hormone elevation: arthralgia, peripheral oedema, myalgia, paraesthesia and injection-site reactions. Impaired glucose tolerance and increased blood glucose occur and require monitoring, particularly in patients with diabetes or pre-diabetes. Contraindicated in active malignancy given IGF-1 elevation, in pituitary disease and in pregnancy. Baseline and periodic IGF-1 and glucose monitoring should be standard. Benefit is not maintained after discontinuation.
ContraindicationsActive malignancy; disruption of the hypothalamic-pituitary axis or pituitary tumour; pregnancy; known hypersensitivity to tesamorelin or mannitol.
Storage & HandlingStore lyophilised vial at 2-8 C, protected from light.
Regulatory StatusApproved in the United States (Egrifta) for a specific indication; not authorised in the UK or EU. Prohibited in sport under the WADA Prohibited List (S2). The product supplied here is not the licensed presentation; use is off-label and prescription-medicine advertising restrictions apply.