Apimostinel
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| Other names | NRX-1074; AGN-241660; Threonyl-prolyl-2R-(2-benzyl)-prolyl-threonine amide |
| Routes of administration | By mouth |
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| Formula | C25H37N5O6 |
| Molar mass | 503.600 g·mol−1 |
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Apimostinel (GATE-202, formerly NRX-1074) is an investigational antidepressant, acting as a novel and selective modulator of the NMDA receptor.[1][2][3][4]. It is currently under development for the treatment of major depressive disorder (MDD) by Gate Neurosciences, and previously by Naurex and Allergan.[5][6][7] As of February 2015, an intravenous formulation of apimostinel has completed a phase IIa clinical trial for MDD[5][8].
Its mechanism of action and effects are similar to those of rapastinel (GLYX-13), which was previously under development as an adjunctive therapy for treatment-resistant depression by Naurex and Allergan. However, apimostinel is 1000-fold more potent in vitro and is intended as an improved, follow-up drug to rapastinel.[2][5] Similar to rapastinel, apimostinel is an amidated tetrapeptide, but has been structurally modified via the addition of a benzyl group. The drug has shown rapid and potent antidepressant effects in pre-clinical models of depression.[5] In addition, similarly to rapastinel, it is well tolerated and lacks the schizophrenia-like psychotomimetic effects of NMDA receptor antagonists such as ketamine.[5]
See also
References
- ^ PR Newswire (2010). "Naurex's Novel Antidepressant GLYX-13 Recognized as One of Windhover's Top 10 Neuroscience Projects to Watch".
- ^ a b Henter, Ioline D.; Park, Lawrence T.; Zarate, Carlos A. (2021-05). "Novel Glutamatergic Modulators for the Treatment of Mood Disorders: Current Status". CNS drugs. 35 (5): 527–543. doi:10.1007/s40263-021-00816-x. ISSN 1179-1934. PMC 8201267. PMID 33904154.
{{cite journal}}: Check date values in:|date=(help) - ^ Donello, John E.; Banerjee, Pradeep; Li, Yong-Xin; Guo, Yuan-Xing; Yoshitake, Takashi; Zhang, Xiao-Lei; Miry, Omid; Kehr, Jan; Stanton, Patric K.; Gross, Amanda L.; Burgdorf, Jeffery S. (2019-03-01). "Positive N-Methyl-D-Aspartate Receptor Modulation by Rapastinel Promotes Rapid and Sustained Antidepressant-Like Effects". The International Journal of Neuropsychopharmacology. 22 (3): 247–259. doi:10.1093/ijnp/pyy101. ISSN 1469-5111. PMC 6403082. PMID 30544218.
- ^ Hayley S, Litteljohn D (2013). "Neuroplasticity and the next wave of antidepressant strategies". Front Cell Neurosci. 7: 218. doi:10.3389/fncel.2013.00218. PMC 3834236. PMID 24312008.
- ^ a b c d e PR Newswire (2014). "Naurex Reports Positive Top-Line Phase 2b Results for Novel Antidepressant GLYX-13 and Advances NRX-1074 into Phase 2 Depression Study".
- ^ plc, Allergan. "Allergan Successfully Completes Naurex Acquisition". www.prnewswire.com. Retrieved 2016-11-20.
- ^ "Home - Gate Neurosciences". Retrieved 2022-05-12.
- ^ "Study of Intravenous NRX-1074 in Patients With Major Depressive Disorder". Clinicaltrials.gov. US National Institutes of Health. Retrieved 10 December 2014.