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Tesamorelin vs Ipamorelin
Tesamorelin is a GHRH analog that stimulates the pituitary directly, and it has been investigated in adipose-tissue compartment research. Ipamorelin is a ghrelin-mimetic GH secretagogue that produces a discrete GH pulse. Different upstream targets, overlapping downstream GH effects.
Tesamorelin
Tesamorelin is a synthetic analog of human growth hormone-releasing hormone (GHRH, also known as somatocrinin), with a trans-3-hexenoic acid group attached to the N-terminus. That modification makes it resistant to cleavage by dipeptidyl peptidase-4 (DPP-4), the enzyme that normally breaks GHRH down, so it stays active longer than native GHRH(1–44). Tesamorelin binds to and activates the GHRH receptor (GHRHR) on pituitary somatotrophs, the pituitary cells that make growth hormone. This stimulates pulsatile secretion of growth hormone (GH) through Gsα/adenylyl cyclase/cAMP/PKA signaling. GH in turn stimulates hepatic and peripheral production of IGF-1 (insulin-like growth factor 1), which carries out many of the anabolic and metabolic effects. Unlike exogenous GH administration, tesamorelin preserves pulsatile GH release and keeps feedback regulation through somatostatin intact, giving a more physiological GH profile. FDA approved tesamorelin (Egrifta®) in 2010 for reduction of excess abdominal fat in HIV-infected patients with lipodystrophy. It was the first GHRH analog approved in the US. Research interest extends to aging-related GH decline, cognition, and metabolic syndrome.
Ipamorelin
Ipamorelin is a selective growth hormone secretagogue pentapeptide, a five-amino-acid chain that prompts the pituitary to release its own growth hormone. It acts as a partial agonist at the ghrelin receptor (GHS-R1a), stimulating pulsatile GH release from pituitary somatotrophs. Unlike older GH secretagogues, ipamorelin is highly selective, with minimal effects on ACTH, cortisol, aldosterone, or prolactin.
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