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Relamorelin (RM-131), a modified ghrelin peptide, was studied in phase 2 trials for diabetic gastroparesis, and macimorelin, a non-peptidyl GHS-R1a agonist, received FDA approval in December 2017 under the brand name Macrilen for the diagnosis of adult growth hormone deficiency, marking the first FDA-approved compound in the ghrelin receptor agonist class
doi: 10.1016/J.ARCMED.2005.02.006 79 RomieuISienra-MongeJJRamrez-AguilarMTllez-RojoMMMoreno-MacasHReyes-RuizNIet al
Cancer Cell 23 , 450463 (2013)
in 1998, it is distinguished from other GHRPs by releasing GH without meaningfully elevating cortisol, prolactin, or ACTH at therapeutic dosesa selectivity profile unique among its class
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