Chemical Name: CERC-301
CAS Number: 808732-98-1
Mechanism: NMDA receptor (NR2B-selective) antagonist
Status: Phase II
Developer: Cerecor
In 2013, the FDA granted Fast Track Designation to CERC-301 as a potential adjunctive therapy for depression and suicidal ideation. Pharmacodynamic studies have shown that CERC-301 has a highly selective antagonistic effect on the NR2B subunit of the NMDA receptor. Its selective affinity for the NR2B subunit of the NMDA receptor is thought to minimize the likelihood of psychotomimetic effects (e.g., drug-induced psychosis) occurring in conjunction with other non-selective NMDA receptor antagonists.
Cerecor, the developer of CERC-301, was shown to have rapid antidepressant activity, resulting in relief of depressive symptoms within minutes or hours of administration, rather than days or weeks. Preliminary data from the CERC-301 trial suggest that the drug is well tolerated and safe. Many believe that CERC-301 is the most promising of the NMDA antagonists being developed for the treatment of depression.
