Pharmacodynamic hormonal effects of anamorelin, a novel oral ghrelin mimetic and growth hormone secretagogue in healthy volunteers.

OBJECTIVE: Activation of ghrelin receptors stimulates GH secretion and appetite, increasing lean body mass and body weight. However, clinical use of ghrelin is limited because it has a short half-life and must be administered parenterally. Anamorelin is a novel, orally active, non-peptidic ghrelin mimetic and growth hormone secretagogue. Our objective was to evaluate its hormonal effects in healthy subjects.

DESIGN: A double-blind, randomized, placebo-controlled study evaluated the short-term effects of anamorelin on GH, insulin-like growth factor-1 (IGF-1), insulin-like growth factor binding protein 3 (IGFBP-3), prolactin, ACTH, LH, FSH, TSH, cortisol, insulin and glucose. Normal healthy volunteers (n=32) recruited from the general population were administered escalating doses of anamorelin (25, 50, and 75 mg daily) vs. placebo.

RESULTS: Anamorelin significantly increased GH levels at all doses (p
CONCLUSIONS: Anamorelin increases GH, IGF-1, IGFBP-3 and body weight with good tolerability and selectivity, without affecting other anterior pituitary axes or fasting glucose levels.