e-Drug3D

762

RILUZOLE


INN
RILUZOLE

cas 1744-22-5
CLASS

NERVOUS SYSTEM
NEUROPROTECTIVE
INHIBITORY EFFECT ON GLUTAMATE RELEASE
PARTIAL INACTIVATION OF VOLTAGE-DEPENDENT SODIUM CHANNELS (PMID25548669)
SEDATIVES
MYORELAXANT
TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS (ALS)
ACTIVATES SK CHANNELS BUT NOT BK CHANNELS

ROUTE (list)

ORAL

ATC code

N07XX02

PK parameters

F 60 PERCENT
VD 245 LITER
PPB 96 PERCENT
t1/2 12 HOUR

Solubility

VERY SLIGHTLY SOLUBLE IN WATER


Target

TARGET SMALL-CONDUCTANCE CALCIUM-ACTIVATED POTASSIUM (SK) CHANNELS (PMID26311432)

PDB
5V02 (A POSITIVE ALLOSTERIC MODULATOR BINDING POCKET IN SK2 ION CHANNELS IS SHARED BY RILUZOLE AND CYPPA)

Ligand code = 657 (link to the list of PDB complexes)

Download experimental 3D coordinates of 657 with added hydrogens

DrugCentral

Sodium channel protein type 5 subunit alpha UNIPROT Q14524 SCN5A

Download SDF file 6-(trifluoromethoxy)-1,3-benzothiazol-2-amine

Formula:
C8H5F3N2OS

Calculated chemical properties:

MW 234.21
NB_atoms 15
XLogP 2.78
PSA 45.911
NB_HD 2
NB_HA 3
fsp3 0.12
Lipinski(0=no;1=yes) 1

FDA
NDA 020599 (label) INN (RILUZOLE) RILUTEK (COVIS) APPROVAL= AP YEAR= 1995 DISCONTINUED
NDA 076173 (pdf not found) INN (RILUZOLE) RILUZOLE (IMPAX LABS) APPROVAL= AP YEAR= 2003
NDA 091394 (pdf not found) INN (RILUZOLE) RILUZOLE (GLENMARK PHARMS LTD) APPROVAL= AP YEAR= 2013
NDA 091417 (pdf not found) INN (RILUZOLE) RILUZOLE (SUN PHARM INDS LTD) APPROVAL= AP YEAR= 2013 DISCONTINUED
NDA 091300 (pdf not found) INN (RILUZOLE) RILUZOLE (APOTEX CORP) APPROVAL= AP YEAR= 2013 DISCONTINUED
NDA 203042 (pdf not found) INN (RILUZOLE) RILUZOLE (PHARMOBEDIENT) APPROVAL= AP YEAR= 2013 DISCONTINUED
NDA 204048 (pdf not found) INN (RILUZOLE) RILUZOLE (ALKEM LABS LTD) APPROVAL= AP YEAR= 2016
NDA 204430 (pdf not found) INN (RILUZOLE) RILUZOLE (DAITO PHARMS CO LTD) APPROVAL= AP YEAR= 2018 DISCONTINUED
NDA 209080 (label) INN (RILUZOLE) TIGLUTIK KIT (ITALFARMACO SA) APPROVAL= AP YEAR= 2018
NDA 206045 (pdf not found) INN (RILUZOLE) RILUZOLE (KENTON) APPROVAL= AP YEAR= 2019
NDA 212640 (label) INN (RILUZOLE) EXSERVAN (AQUESTIVE) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 216035 (pdf not found) INN (RILUZOLE) RILUZOLE (ALKEM LABS LTD) APPROVAL= AP YEAR= 2024

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL