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Anamorelin

Anamorelin ( INN) (developmental code names ONO-7643, RC-1291, ST-1291), also known as anamorelin hydrochloride ( USAN, JAN), is a non-peptide, orally-active, centrally-penetrant, selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) with appetite-enhancing and anabolic effects which is under development by Helsinn Therapeutics for the treatment of cancer cachexia and anorexia.

Anamorelin significantly increases plasma levels of growth hormone (GH), insulin-like growth factor 1 (IGF-1), and insulin-like growth factor-binding protein 3 (IGFBP-3) in humans, without affecting plasma levels of prolactin, cortisol, insulin, glucose, adrenocorticotropic hormone (ACTH), luteinizing hormone (LH), follicle-stimulating hormone (FSH), or thyroid-stimulating hormone (TSH). In addition, anamorelin significantly increases appetite, overall body weight, lean body mass, and muscle strength, with increases in body weight correlating directly with increases in plasma IGF-1 levels.

As of February 2016, anamorelin has completed phase III clinical trials for the treatment of cancer cachexia and anorexia associated with non-small-cell lung carcinoma. Results of the studies were positive, and the drug is now in preregistration with the European Medicines Agency.1