Rislenemdaz

Rislenemdaz
Clinical data
Other namesCERC-301; MK-0657
Routes of
administration		By mouth
Drug classSelective NMDA receptor antagonist
Identifiers
  • 4-Methylbenzyl (3S,4R)-3-fluoro-4-[(2-pyrimidinylamino)methyl]-1-piperidinecarboxylate
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H23FN4O2
Molar mass358.417 g·mol−1
3D model (JSmol)
  • CC1=CC=C(C=C1)COC(=O)N2CC[C@@H]([C@@H](C2)F)CNC3=NC=CC=N3
  • InChI=1S/C19H23FN4O2/c1-14-3-5-15(6-4-14)13-26-19(25)24-10-7-16(17(20)12-24)11-23-18-21-8-2-9-22-18/h2-6,8-9,16-17H,7,10-13H2,1H3,(H,21,22,23)/t16-,17-/m1/s1
  • Key:RECBFDWSXWAXHY-IAGOWNOFSA-N

Rislenemdaz (developmental code names CERC-301, MK-0657) is an orally active, selective NMDA receptor subunit 2B (NR2B) antagonist which is under development by Cerecor in the United States as an adjunctive therapy for treatment-resistant depression (TRD).[1] In November 2013, phase II clinical trials were initiated,[2] and in the same month, rislenemdaz received Fast Track Designation from the Food and Drug Administration for TRD.[3]

A pilot study was published in 2012,[1] and a phase II trial was completed in 2014, but was deemed insufficient.[4] A second attempt at a phase II trial in 2016 also found that the drug failed to demonstrate efficacy against depression.[5]

  1. ^ a b Ibrahim L, Diaz Granados N, Jolkovsky L, Brutsche N, Luckenbaugh DA, Herring WJ, et al. (August 2012). "A Randomized, placebo-controlled, crossover pilot trial of the oral selective NR2B antagonist MK-0657 in patients with treatment-resistant major depressive disorder". Journal of Clinical Psychopharmacology. 32 (4): 551–557. doi:10.1097/JCP.0b013e31825d70d6. PMC 3438886. PMID 22722512.
  2. ^ "Cerecor Announces Initiation of Phase 2 Study for CERC-301, an Oral Rapid-acting Antidepressant Candidate". Yahoo! Finance. 2013. Archived from the original on 14 July 2014.
  3. ^ "Cerecor Receives Fast Track Designation for CERC-301 for the Treatment of Major Depressive Disorder". Yahoo! Finance. 2013. Archived from the original on 14 July 2014.
  4. ^ Clinical trial number NCT01941043 for "A Randomized, Double-Blind, Placebo-Controlled, Sequential Parallel Study of CERC-301 in the Adjunctive Treatment of Subjects With Severe Depression and Recent Active Suicidal Ideation Despite Antidepressant Treatment" at ClinicalTrials.gov
  5. ^ "Cerecor (CERC) Announces CERC-301 Phase 2 Missed Primary Endpoint in MDD". streetinsider.com.