Tesamorelin

Tesamorelin is a synthetic analog of growth hormone-releasing hormone (GHRH) that consists of all 44 amino acids of human GHRH with the addition of a trans-3-hexenoic acid group at the tyrosine residue. This modification increases stability against enzymatic degradation while maintaining full biological activity at the GHRH receptor.

It stimulates pulsatile growth hormone release through the GHRH receptor and is studied in growth-hormone axis and adipose tissue research.

Tesamorelin acts through the GHRH receptor on pituitary somatotrophs:

GHRH Receptor Activation Tesamorelin binds to GHRH receptors on pituitary somatotroph cells, activating adenylyl cyclase and increasing intracellular cAMP. This triggers GH gene transcription and GH release.

Pulsatile GH Release Unlike exogenous GH, tesamorelin stimulates pulsatile GH release, which better maintains GH receptor sensitivity and mimics natural GH secretion patterns.

IGF-1 Increase The GH released in response to tesamorelin stimulates hepatic IGF-1 production, which mediates many of GH's metabolic effects including effects on body composition.

Visceral Adipose Tissue Published studies have examined its effect on visceral adipose tissue (VAT) in lipodystrophy, through GH's lipolytic effects on lipid metabolism.