Uses
Macimorelin (EP-1572) acetate, a GH secretagogue, is an orally active GHSR agonist. Macimorelin acetate stimulates GH release. Macimorelin acetate can be used in the research of adult growth hormone deficiency (AGHD), and Cancer anorexia-cachexia syndrome (CACS)[1][2][3].
Biological Activity
Macimorelin (AEZS-130; ARD-07; EP1572; UMV1843; Aib-DTrp-DgTrp-CHO) is an orally active peptido-mimetic growth hormone (GH) secretagogue (GHS) th at targets human and animal GHS-receptor (IC50 in nM = 10.2/ghrelin, 12.3/hexaghrelin, 15.6/macimorelin against ghrelin binding to human GHS-R) with potent and selective GH-releasing activity in vivo (GH level = 158.8 μg/L 15 min post 300 μg/kg s.c. in neonatal rats; 11.3 μg/L without treatment).
in vivo
Macimorelin (5 mg/kg, i.p. twice daily for 2 weeks) acetate decreased the number and duration of seizures in IHKA mouse model[2].
| Animal Model: | Intrahippocampal kainic acid (IHKA) mouse model[2] |
| Dosage: | 5 mg/kg |
| Administration: | Intraperitoneal injection (i.p.), twice daily for 2 weeks. |
| Result: | Significantly decreased the number and duration of seizures during the treatment period, but had no antiepileptogenic or disease-modifying effect. |
References
[1] Jose M Garcia, et al. Macimorelin as a Diagnostic Test for Adult GH Deficiency. J Clin Endocrinol Metab. 2018 Aug 1;103(8):3083-3093. DOI:
10.1210/jc.2018-00665[2] An Buckinx, et al. Translational potential of the ghrelin receptor agonist macimorelin for seizure suppression in pharmacoresistant epilepsy. Eur J Neurol. 2021 Sep;28(9):3100-3112. DOI:
10.1111/ene.14992[3] Ali SA, Garcia JM. Randomized clinical trial of the novel oral ghrelin mimetic macimorelin in the treatment of cancer cachexia: study design and preliminary results. Endocr Rev. 2013;34:
