e-Drug3D

1171

MEXILETINE


INN
MEXILETINE

cas 31828-71-4
CLASS

CARDIOVASCULAR
LOCAL ANESTHETIC
ANTIARRYTHMIC
SODIUM CHANNEL BLOCKER

ROUTE (list)

ORAL

ATC code

C01BB02

PK parameters

F 90 PERCENT
VD 360 LITER
Cl 30 LITER / HOUR
PPB 55 PERCENT
t1/2 11 HOUR

Solubility

FREELY SOLUBLE IN WATER


Target

TARGET SODIUM CHANNEL

PDB
2VIN (FRAGMENT-BASED DISCOVERY OF MEXILETINE DERIVATIVES AS ORALLY BIOAVAILABLE INHIBITORS OF UROKINASE-TYPE PLASMINOGEN ACTIVATOR)

Ligand code = 505 (link to the list of PDB complexes)

Download experimental 3D coordinates of 505 with added hydrogens

DrugCentral

Sodium channel protein type 5 subunit alpha UNIPROT Q14524 SCN5A

Sodium channel protein type 2 subunit alpha UNIPROT Q99250 SCN2A

Download SDF file 1-(2,6-dimethylphenoxy)propan-2-amine

Formula:
C11H17NO

Calculated chemical properties:

MW 179.26
NB_atoms 13
XLogP 2.03
PSA 34.025
NB_HD 2
NB_HA 2
fsp3 0.45
Lipinski(0=no;1=yes) 1

FDA
NDA 018873 (pdf not found) INN (MEXILETINE HYDROCHLORIDE) MEXITIL (BOEHRINGER INGELHEIM) APPROVAL= AP YEAR= 1985 NEWMOLECULARENTITY DISCONTINUED
NDA 074377 (pdf not found) INN (MEXILETINE HYDROCHLORIDE) MEXILETINE HYDROCHLORIDE (TEVA) APPROVAL= AP YEAR= 1995
NDA 074450 (pdf not found) INN (MEXILETINE HYDROCHLORIDE) MEXILETINE HYDROCHLORIDE (ANI PHARMS) APPROVAL= AP YEAR= 1996
NDA 074711 (pdf not found) INN (MEXILETINE HYDROCHLORIDE) MEXILETINE HYDROCHLORIDE (WATSON LABS) APPROVAL= AP YEAR= 1997 DISCONTINUED
NDA 074865 (label) INN (MEXILETINE HYDROCHLORIDE) MEXILETINE HYDROCHLORIDE (WATSON LABS) APPROVAL= AP YEAR= 1998 DISCONTINUED
NDA 213500 (pdf not found) INN (MEXILETINE HYDROCHLORIDE) MEXILETINE HYDROCHLORIDE (CROSSMEDIKA SA) APPROVAL= AP YEAR= 2020
NDA 214352 (pdf not found) INN (MEXILETINE HYDROCHLORIDE) MEXILETINE HYDROCHLORIDE (NOVAST LABS) APPROVAL= AP YEAR= 2021
NDA 214089 (pdf not found) INN (MEXILETINE HYDROCHLORIDE) MEXILETINE HYDROCHLORIDE (SENORES PHARMS) APPROVAL= AP YEAR= 2021
NDA 215315 (pdf not found) INN (MEXILETINE HYDROCHLORIDE) MEXILETINE HYDROCHLORIDE (RISING) APPROVAL= AP YEAR= 2022
NDA 216463 (pdf not found) INN (MEXILETINE HYDROCHLORIDE) MEXILETINE HYDROCHLORIDE (ANNORA PHARMA) APPROVAL= AP YEAR= 2022
NDA 215876 (pdf not found) INN (MEXILETINE HYDROCHLORIDE) MEXILETINE HYDROCHLORIDE (LEADING) APPROVAL= AP YEAR= 2023

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL