Drug intelligence / Profile preview

varenicline + extended duration varenicline

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination therapy involving standard-duration varenicline and an extended duration of varenicline treatment. Varenicline is a small molecule partial agonist at neuronal nicotinic acetylcholine receptors, primarily the α4β2 subtype, used as a pharmacotherapy for smoking cessation. The mechanism involves partial agonism at these receptors, leading to moderate dopamine release (less than nicotine), which helps reduce cravings and withdrawal symptoms while also blocking nicotine’s rewarding effects by preventing its binding. Extended duration refers to continuing varenicline beyond the standard 12-week course—often up to 24 weeks or longer—to help maintain abstinence in individuals who have recently quit smoking[4]. This approach has been shown to further improve long-term cessation rates compared with standard treatment durations.

02

Targets

α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)α4β4 nAChR (α4β4 nicotinic receptor)α6β2 nAChR (α6β2 nicotinic receptor)CHRNA7 (α7 nicotinic receptor)

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