Chemistry:Macimorelin
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| Trade names | Macrilen |
| Other names | Aib-Trp-gTrp-CHO; AEZS-130; JMV 1843; Macimorelin acetate |
| AHFS/Drugs.com | Professional Drug Facts |
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| Routes of administration | By mouth |
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| Metabolism | Hepatic (CYP3A4-mediated) |
| Elimination half-life | 4.1 hours |
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| Formula | C26H30N6O3 |
| Molar mass | 474.565 g·mol−1 |
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Macimorelin (INN) – or Macrilen (trade name) – is a drug that was developed by Æterna Zentaris for use in the diagnosis of adult growth hormone deficiency.[2] Macimorelin acetate, the salt formulation, is a synthetic growth hormone secretagogue receptor agonist.[3] It is a growth hormone secretagogue receptor (ghrelin receptor) agonist, causing release of growth hormone from the pituitary gland.[4][5][6] Macimorelin acetate is described chemically as D-Tryptophanamide, 2-methylalanyl-N-[(1R)-1-(formylamino)-2-(1H-indol-3-yl)ethyl]-acetate.
Macimorelin (Macrilen™) was invented and first synthesized by the research group of Professor Martinez at University of Montpellier, Centre National de la Recherche Scientitifique (CNRS), France.[7][8][9] This transpired from a long-lasting research collaboration with Aeterna Zentaris. Aeterna Zentaris later in-licensed macimorelin as a development candidate from the CNRS and proceeded with the pre-clinical and clinical development of the compound.
As of January 2014, it was in Phase III clinical trials.[10] The phase III trial for growth hormone deficiency is expected to be complete in December 2016.[11]
As of December 2017, it became FDA-approved as a method to diagnose growth hormone deficiency.[12][13] Traditionally, growth hormone deficiency was diagnosed via means of insulin tolerance test (IST) or glucagon stimulation test (GST). These two means are done parenterally, whereas Macrilen boasts an oral formulation for ease of administration for patients and providers.
The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.[14]
See also
- List of growth hormone secretagogues
References
- ↑ "Macimorelin Aeterna Zentaris". 13 November 2018. https://www.ema.europa.eu/en/medicines/human/EPAR/macimorelin-aeterna-zentaris.
- ↑ "Macimorelin Aeterna Zentaris". 13 November 2018. https://www.ema.europa.eu/en/medicines/human/EPAR/macimorelin-aeterna-zentaris.
- ↑ "Macrilen Prescribing Information". http://www.strongbridgebio.com/wp-content/uploads/macrilen-prescribing-information.pdf.
- ↑ "Macimorelin". NCI Drug Dictionary. National Cancer Institute. http://www.cancer.gov/drugdictionary?cdrid=735530.
- ↑ "Growth hormone in health and disease: Novel ghrelin mimetic is safe and effective as a GH stimulation test". Nature Reviews. Endocrinology 9 (6): 315. June 2013. doi:10.1038/nrendo.2013.89. PMID 23591367.
- ↑ "Macimorelin (AEZS-130)-stimulated growth hormone (GH) test: validation of a novel oral stimulation test for the diagnosis of adult GH deficiency". The Journal of Clinical Endocrinology and Metabolism 98 (6): 2422–2429. June 2013. doi:10.1210/jc.2013-1157. PMID 23559086.
- ↑ Martinez J, Fehrentz JA, Guerlavais V, "Growth hormone secretagogues", WO patent 2001096300, published 20 December 2001
- ↑ "EP1572: a novel peptido-mimetic GH secretagogue with potent and selective GH-releasing activity in man". Journal of Endocrinological Investigation 25 (8): RC26–RC28. September 2002. doi:10.1007/BF03345096. PMID 12240910.
- ↑ "New active series of growth hormone secretagogues". Journal of Medicinal Chemistry 46 (7): 1191–1203. March 2003. doi:10.1021/jm020985q. PMID 12646029.
- ↑ "Aeterna Zentaris NDA for Macimorelin Acetate in AGHD Accepted for Filing by the FDA". Wall Street Journal. January 6, 2014. https://online.wsj.com/article/PR-CO-20140106-907640.html.
- ↑ Clinical trial number NCT02558829 for "Validation of Macimorelin as a Test for Adult Growth Hormone Deficiency" at ClinicalTrials.gov
- ↑ Center for Drug Evaluation and Research. "Drug Approvals and Databases - Drug Trials Snapshots: Marcrilen" (in en). https://www.fda.gov/Drugs/InformationOnDrugs/ucm590519.htm.
- ↑ "FDA Approves Aeterna Zentaris' Macimorelin Growth Hormone Deficiency Test". 21 December 2017. https://www.hcplive.com/view/fda-approves-aeterna-zentaris-macimorelin-growth-hormone-deficiency-test.
- ↑ (PDF) New Drug Therapy Approvals 2017 (Report). January 2018. https://www.fda.gov/media/110526/download. Retrieved 16 September 2020.
External links
- "Macimorelin". Drug Information Portal. U.S. National Library of Medicine. https://druginfo.nlm.nih.gov/drugportal/name/macimorelin.
- "Macimorelin acetate". Drug Information Portal. U.S. National Library of Medicine. https://druginfo.nlm.nih.gov/drugportal/name/macimorelin%20acetate.
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