🔴Tesamorelin | 5mg

Tesamorelin is a synthetic peptide analog of human growth-hormone-releasing hormone (GHRH), engineered to enhance growth hormone (GH) secretion with high specificity and efficacy. Structurally, Tesamorelin comprises a 44-amino acid sequence with an additional trans-3-hexenoyl group at the N-terminus, which augments its binding affinity and biological activity towards the GHRH receptor located on the pituitary gland’s somatotroph cells.

It binds to the GHRH receptor, triggering a conformational change that activates the receptor-associated G-protein (Gs). This activation leads to the stimulation of adenylate cyclase, catalyzing the conversion of ATP to cyclic AMP (cAMP). Elevated levels of cAMP activate protein kinase A (PKA), which then phosphorylates specific transcription factors and other proteins within the cell.

One of the critical targets of PKA in this pathway is the transcription factor CREB (cAMP response element-binding protein). Phosphorylated CREB binds to the cAMP response elements in the promoter regions of the GH gene, enhancing its transcription. This process results in the synthesis of prepro-GH, which is subsequently cleaved to form mature GH that is stored in secretory vesicles.

The release of GH from the pituitary gland is pulsatile, governed by the complex interplay of signals within the hypothalamic-pituitary axis. Tesamorelin’s efficacy stems from its ability to mimic the natural pulsatile release pattern of GHRH, thereby maintaining physiological cycles of GH peaks that are critical for its metabolic effects, such as lipolysis and fatty acid oxidation in peripheral tissues.

The targeted action of Tesamorelin on visceral adipose tissue is particularly noteworthy. GH induces the expression of lipolytic enzymes and suppresses lipogenesis in adipocytes by modulating the activity of enzymes like hormone-sensitive lipase and lipoprotein lipase. The result is a reduction in visceral fat, which is a significant therapeutic goal in the treatment of HIV-associated lipodystrophy. This specific lipolytic action is mediated by GH-induced signaling pathways involving STAT5b and the insulin-like growth factor 1 (IGF-1) axis, which further influences metabolic processes in liver and muscle tissues, promoting an overall healthier metabolic profile.

Tesamorelin’s development and application, thus, represent a refined approach to modulating the GH axis, offering a therapeutic option that combines high receptor specificity, potent GH-stimulating capacity, and a favorable safety profile, making it an effective treatment for conditions associated with GH deficiency and excess abdominal fat.