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NCI Drug Dictionary


An orally available synthetic mimetic of the growth hormone (GH) secretagogue ghrelin with potential anti-cachexia activity. Upon oral administration, macimorelin mimics endogenous ghrelin by stimulating appetite and binds to the growth hormone secretagogue receptor GHSR in the central nervous system, thereby mimicking the GH-releasing effects of ghrelin from the pituitary gland. Stimulation of GH secretion increases insulin-like growth factor-I (IGF-I) levels which may further stimulate protein synthesis. In addition, ghrelin reduces the production of pro-inflammatory cytokines, which may play a direct role in cancer-related loss of appetite. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
Code names:AEZS-130
EP 1572
JMV 1843
Chemical structure:N-(2-Amino-2-Methylpropanoyl-N1-((1R)-1-Formamido-2-(1H-Indol-3-yl)Ethyl)-D-Tryptophanamide