- Guide to PHARMACOLOGY
Synonyms: Champix® | Chantix® | compound 9a [PMID: 16171993] | CP 526555
varenicline is an approved drug (FDA and EMA (2006))
Compound class: Synthetic organic
Comment: Marketed formulations usually contain varenicline tartrate (PubChem CID 9906942). ChEMBL represents this compound without specified stereochemistry (see link above).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: varenicline
|No information available.
|Summary of Clinical Use
|Used as an aid to smoking cessation.
|Mechanism Of Action and Pharmacodynamic Effects
|Inhibits the binding of nicotine to the α4β2 nicotinic acetylcholine receptor, and exerts mild agonistic activity at the receptor, therefore easing nicotine withdrawal symptoms.
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)