e-Drug3D

943

cas 58-46-8

CLASS

NERVOUS SYSTEM
CNS
TREATMENT OF CHOREA ASSOCIATED WITH HUNTINGTON DISEASE
INHIBITOR
IS BELIEVED TO BE RELATED TO ITS EFFECT AS A REVERSIBLE DEPLETOR OF MONOAMINES (SUCH AS DOPAMINE, SEROTONIN, NOREPINEPHRINE, AND HISTAMINE) FROM NERVE TERMINALS
VESICULAR MONOAMINE TRANSPORTER TYPE 2 (VMAT2) (KI=100 NANOMOLAR)

ROUTE (list)

ORAL

PK parameters

F 75 PERCENT
PPB 84 PERCENT

TARGET VESICULAR MONOAMINE TRANSPORTER TYPE 2 (VMAT2)

PDB
8THR (STRUCTURE OF THE HUMAN VESICULAR MONOAMINE TRANSPORTER 2 (VMAT2) BOUND TO TETRABENAZINE IN AN OCCLUDED CONFORMATION)

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

Download experimental 3D coordinates of EBZ with added hydrogens

MW 317.42
NB_atoms 23
XLogP 3.24
PSA 43.997
NB_HD 0
NB_HA 4
fsp3 0.63
Lipinski(0=no;1=yes) 1

FDA
NDA 021894 (pdf not found) INN (TETRABENAZINE) XENAZINE (BAUSCH) APPROVAL= AP YEAR= 2008 NEWMOLECULARENTITY
NDA 206129 (pdf not found) INN (TETRABENAZINE) TETRABENAZINE (SUN PHARM) APPROVAL= AP YEAR= 2015 DISCONTINUED
NDA 204574 (pdf not found) INN (TETRABENAZINE) TETRABENAZINE (HETERO LABS LTD V) APPROVAL= AP YEAR= 2016
NDA 206686 (pdf not found) INN (TETRABENAZINE) TETRABENAZINE (ACTAVIS LABS FL INC) APPROVAL= AP YEAR= 2017
NDA 207682 (pdf not found) INN (TETRABENAZINE) TETRABENAZINE (MYLAN) APPROVAL= AP YEAR= 2017
NDA 208826 (pdf not found) INN (TETRABENAZINE) TETRABENAZINE (BIONPHARMA) APPROVAL= AP YEAR= 2017
NDA 209284 (pdf not found) INN (TETRABENAZINE) TETRABENAZINE (DR REDDYS) APPROVAL= AP YEAR= 2018
NDA 210544 (pdf not found) INN (TETRABENAZINE) TETRABENAZINE (CHARTWELL RX) APPROVAL= AP YEAR= 2018
NDA 209739 (pdf not found) INN (TETRABENAZINE) TETRABENAZINE (HIKMA) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 206093 (pdf not found) INN (TETRABENAZINE) TETRABENAZINE (APOTEX) APPROVAL= AP YEAR= 2020
NDA 213316 (pdf not found) INN (TETRABENAZINE) TETRABENAZINE (ADAPTIS) APPROVAL= AP YEAR= 2020
NDA 213621 (pdf not found) INN (TETRABENAZINE) TETRABENAZINE (AJANTA PHARMA LTD) APPROVAL= AP YEAR= 2020 DISCONTINUED