Tesamorelin Mechanism of Action

How Tesamorelin behaves at the molecular and cellular level, based on current research literature.

Tesamorelin binds to GHRH receptors on somatotroph cells in the anterior pituitary, triggering GH synthesis and secretion. Unlike exogenous GH administration, tesamorelin preserves the natural pulsatile pattern of GH release . In clinical studies, tesamorelin increased mean overnight GH by 0.5 µg/L and IGF-1 by 181 µg/L after 2 weeks of administration . The peptide's DPP-4 resistance ensures sustained receptor activation compared to native GHRH, which degrades within minutes.

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