NRX-1074

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NRX-1074
NRX-1074 structure.png
Systematic (IUPAC) name
(2S,3R)-2-{[(2S)-1-[(2R)-1-[(2S,3R)-2-amino-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]-2-benzylpyrrolidin-2-yl]formamido}-3-hydroxybutanamide
Clinical data
Legal status
  • Investigational New Drug
Identifiers
UNII TTT1F11FZB YesY
Synonyms threonyl-prolyl-2R-(2-benzyl)-prolyl-threonine amide
Chemical data
Formula C25H37N5O6
Molecular mass 503.60 g·mol−1
  • N[C@H](C(=O)N1CCC[C@@H]1C(=O)N2CCC[C@]2(CC3=CC=CC=C3)C(=O)N[C@H](C(=O)N)[C@@H](C)O)[C@@H](C)O
  • InChI=1S/C25H37N5O6/c1-15(31)19(26)23(35)29-12-6-10-18(29)22(34)30-13-7-11-25(30,14-17-8-4-3-5-9-17)24(36)28-20(16(2)32)21(27)33/h3-5,8-9,15-16,18-20,31-32H,6-7,10-14,26H2,1-2H3,(H2,27,33)(H,28,36)/t15-,16-,18-,19+,20+,25+/m1/s1
  • Key:DVBUEXCIEIAXPM-ZQKMVPBFSA-N

NRX-1074 (also known as AGN-241660) is a novel antidepressant, acting as a selective partial agonist of an allosteric site of the glycine site of the NMDA receptor complex, which is under investigation by Naurex (recently acquired by Allergan) for the treatment of major depressive disorder.[1][2][3][4] Its mechanism of action and effects are similar to those of rapastinel (GLYX-13), which is under development as an adjunctive therapy for treatment-resistant depression also by Naurex; however, NRX-1074 is 100-fold more potent by weight and, unlike GLYX-13 (which must be administered via intravenous injection), is orally-active.[3] NRX-1074 is intended by Naurex as an improved, follow-up drug to GLYX-13. The drug has shown rapid antidepressant effects in pre-clinical models of depression.[3] In addition, similarly to GLYX-13, it is well-tolerated and lacks the schizophrenia-like psychotomimetic effects of other NMDA receptor antagonists such as ketamine.[3] As of 2015, an intravenous formulation of NRX-1074 is in a phase II clinical trial for MDD,[3][5] and an oral formulation is concurrently in phase I trials for MDD.

See also

References

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External links



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