Tesamorelin

Tesamorelin is a synthetic analog of growth hormone-releasing hormone (GHRH 1-44) with an N-terminal trans-3-hexenoic acid modification that stabilizes the peptide against dipeptidyl peptidase-4 cleavage and extends biological activity.

The compound binds the GHRH receptor on pituitary somatotrophs, activating adenylyl cyclase via Gs and increasing cAMP-driven synthesis and pulsatile release of endogenous growth hormone. Because the mechanism is upstream of the pituitary, GH secretion remains under normal hypothalamic feedback control — a pharmacological distinction from exogenous recombinant GH administration.

Tesamorelin holds FDA approval for HIV-associated lipodystrophy, and the clinical-trial record in that indication forms the bulk of human pharmacology data on the compound.

Research Applications

• Visceral adipose tissue research in HIV-associated lipodystrophy models.
• GHRH receptor pharmacology and pulsatile GH-IGF-1 axis studies.
• Cognitive and metabolic research in age-related GH decline contexts.