Tesamorelin

Tesamorelin is a 44-amino acid synthetic GHRH analogue with a trans-3-hexenoic acid modification at the N-terminus, which improves stability and bioavailability. It binds to GHRH receptors on pituitary somatotroph cells, stimulating synthesis and pulsatile release of endogenous growth hormone. The resulting GH pulse promotes lipolysis (particularly of visceral adipose tissue), hepatic IGF-1 production, and improved body composition. Because it works through the physiological GHRH-GH-IGF-1 axis, negative feedback mechanisms remain intact, reducing the risk of supraphysiological GH levels.

Two pivotal Phase 3 RCTs demonstrated significant reductions in visceral adipose tissue (VAT) vs. placebo in HIV-associated lipodystrophy: approximately 15-18% reduction in trunk fat at 26 weeks. FDA approval was based on these trials. Post-marketing studies have confirmed durability of effect. Additional research has explored potential benefits in NAFLD/NASH (investigational), showing reductions in hepatic fat fraction. Tesamorelin has been studied in cognitive function in older adults with mild cognitive impairment, with some positive signals.

Tesamorelin (Egrifta SV) is FDA-approved for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy. Original approval: 2010. Egrifta SV (preservative-free formulation): 2019. It is a prescription medication available through specialty pharmacies. Off-label use for anti-aging or body composition optimization is not supported by the approved labeling but is practiced.

Label-directed monitoring includes: IGF-1 levels (maintain within age-appropriate normal range), fasting glucose and HbA1c (particularly in patients with diabetes or pre-diabetes), assessment of fluid retention symptoms, and periodic evaluation of treatment benefit (VAT reduction). Discontinue if IGF-1 consistently exceeds 3 SDS.

These are general considerations for clinical awareness and do not constitute prescriptive monitoring recommendations for any individual patient.

Per the approved label, Egrifta SV should be stored refrigerated (2-8C). The reconstituted solution should be used immediately. Do not freeze. Protect from light.

1. 1

   RCT

   Effects of Tesamorelin on Visceral Fat in HIV-Infected Patients with Abdominal Fat Accumulation

   Falutz J, Allas S, Blot K, et al. (2007). Journal of Acquired Immune Deficiency Syndromes

   Key findings: Tesamorelin reduced trunk fat by 15.2% vs increase of 5.0% with placebo at 26 weeks in HIV-associated lipodystrophy.

   Limitations: 26-week duration. HIV-specific population.

2. 2

   FDA label

   EGRIFTA SV (tesamorelin for injection) Prescribing Information

   Theratechnologies Inc. (2019). FDA

   Key findings: Full prescribing information including indication, dosing, contraindications, warnings, and clinical trial data.

   Limitations: Label information; not primary research.

   View source
3. 3

   RCT

   Tesamorelin and Hepatic Fat in HIV-Associated NAFLD

   Stanley TL, Fourman LT, Zheng I, et al. (2014). Journal of Clinical Endocrinology & Metabolism

   Key findings: Tesamorelin reduced hepatic fat fraction in HIV-infected patients with NAFLD.

   Limitations: Small study. HIV population may not generalize.