Tesamorelin consists of the 44-amino acid sequence of human growth hormone-releasing hormone (GHRH) with an added trans-3-hexenoic acid group attached to the N-terminus. This structural modification significantly enhances the compound’s stability and extends its half-life in laboratory models by increasing its resistance to cleavage by the dipeptidyl peptidase-4 (DPP-4) enzyme.

Current research applications focus on its highly specific binding to GHRH receptors located in the anterior pituitary gland. In-vitro and animal studies frequently utilize Tesamorelin to investigate the pulsatile release of endogenous growth hormone and its subsequent downstream regulatory effects on insulin-like growth factor 1 (IGF-1) levels. Furthermore, researchers study its targeted metabolic pathways, particularly how it influences the lipolysis of visceral adipose tissue and hepatic lipid accumulation without significantly altering glucose homeostasis.