e-Drug3D

946

VARENICLINE


INN
VARENICLINE

cas 249296-44-4
CLASS

NERVOUS SYSTEM
NICOTINIC AGONISTS
USE AS AN AID TO SMOKING CESSATION TREATMENT

ROUTE (list)

ORAL NASAL

ATC code

N07BA03
S01XA28

PK parameters

F 90 PERCENT
Tmax 3.5 HOUR
VD 415 LITER
PPB 20 PERCENT
t1/2 24 HOUR

Solubility

HIGHLY SOLUBLE IN WATER


Target

TARGET NEURONAL ACETYLCHOLINE RECEPTOR SUBUNIT ALPHA-4 BETA-2
5-HT3 RECEPTOR (KI=350 NANOMOLAR)

PDB
5AIN (VARENICLINE INTERACTIONS AT THE 5HT3 RECEPTOR LIGAND BINDING SITE ARE REVEALED BY 5HTBP)

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

Download experimental 3D coordinates of QMR with added hydrogens

DrugCentral

Neuronal acetylcholine receptor

Download SDF file 6,10-Methano-6H-pyrazino[2,3-h][3]benzazepine, 7,8,9,10-tetrahydro-

Formula:
C13H13N3

Calculated chemical properties:

MW 211.26
NB_atoms 16
XLogP 1.80
PSA 34.076
NB_HD 1
NB_HA 3
fsp3 0.38
Lipinski(0=no;1=yes) 1

FDA
NDA 021928 (pdf not found) INN (VARENICLINE TARTRATE) CHANTIX (PF PRISM CV) APPROVAL= AP YEAR= 2006 DISCONTINUED
NDA 201920 (pdf not found) INN (VARENICLINE) VARENICLINE (TEVA PHARMS USA) APPROVAL= TA YEAR= 2013
NDA 201808 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (WATSON LABS INC) APPROVAL= TA YEAR= 2016
NDA 201785 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (PH HEALTH) APPROVAL= AP YEAR= 2021
NDA 213978 (pdf not found) INN (VARENICLINE TARTRATE) TYRVAYA (OYSTER POINT PHARMA) APPROVAL= AP YEAR= 2021
NDA 201962 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (APOTEX) APPROVAL= AP YEAR= 2023
NDA 216723 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (ZYDUS) APPROVAL= AP YEAR= 2023
NDA 211862 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (LUPIN LTD) APPROVAL= AP YEAR= 2023
NDA 214255 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (MANKIND PHARMA) APPROVAL= AP YEAR= 2023
NDA 214557 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (ALKEM LABS LTD) APPROVAL= AP YEAR= 2023
NDA 214571 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (HETERO LABS LTD III) APPROVAL= AP YEAR= 2023
NDA 217151 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (MEDLEY PHARMS) APPROVAL= AP YEAR= 2023
NDA 202019 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (PHARMOBEDIENT) APPROVAL= AP YEAR= 2024
NDA 213019 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (AJANTA PHARMA LTD) APPROVAL= AP YEAR= 2024
NDA 217283 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (NE RX PHARMA) APPROVAL= AP YEAR= 2024
NDA 215048 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (MACLEODS PHARMS LTD) APPROVAL= AP YEAR= 2024
NDA 215931 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (DR REDDYS) APPROVAL= AP YEAR= 2024
NDA 217115 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (PIRAMAL) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 219106 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (INDOCO) APPROVAL= AP YEAR= 2024
NDA 212879 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (VIWIT PHARM) APPROVAL= AP YEAR= 2025
NDA 213268 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (RHODES PHARMS) APPROVAL= AP YEAR= 2025
NDA 214595 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (AUROBINDO PHARMA) APPROVAL= AP YEAR= 2025
NDA 216615 (pdf not found) INN (VARENICLINE TARTRATE) VARENICLINE TARTRATE (SHILPA) APPROVAL= AP YEAR= 2025

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL