| Stereochemistry | ABSOLUTE |
| Molecular Formula | C24H25FN4O2 |
| Molecular Weight | 420.4793 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@H]1CC[C@@H](COC2=NC=C(F)C=C2)CN1C(=O)C3=CC(C)=CC=C3C4=NC=CC=N4
InChI
InChIKey=NPFDWHQSDBWQLH-QZTJIDSGSA-N
InChI=1S/C24H25FN4O2/c1-16-4-8-20(23-26-10-3-11-27-23)21(12-16)24(30)29-14-18(6-5-17(29)2)15-31-22-9-7-19(25)13-28-22/h3-4,7-13,17-18H,5-6,14-15H2,1-2H3/t17-,18-/m1/s1
Filorexant (MK-6096) is a novel, structurally distinct dual orexin receptor antagonist, conclusively validates orexin signalling mechanism as a specific and effective target for the treatment of insomnia and potentially other disorders in which sleep/wake dysregulation occurs. Also, it is being investigated as a possible agent against diabetic neuropathies, major depressive disorder and for the a migraine prophylaxis. Detected adverse events are: sleep-onset paralysis, excessive daytime sleepiness. As of May 2015, filorexant is no longer listed on Merck's online development pipeline.
CNS Activity
Originator
Approval Year
Sourcing
Sample Use Guides
2.5 or 5 or 10 or 20mg once daily at bedtime during 4 weeks
Route of Administration:
Oral
MK-6096 showed radioligand displacement to occupy OX2R in transgenic rat brain in a dose-dependent manner. Following peripheral dosing, MK-6096 achieved 90% occupancy at an exposure of 142 nM in plasma, showing 3-14 fold higher potency than DORA-22 (Occ90 = 1139 nM) and almorexant (Occ90 = 1922 nM) .
ACTIVE MOIETY
