Drug intelligence / Profile preview

facinicline

Development stage
Phase 2
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

Facinicline is a small molecule drug that acts as a selective partial agonist at the nicotinic acetylcholine receptor alpha-7 subunit (α7 nAChR) and as an antagonist at the serotonin 3 (5-HT3) receptor. It was developed for oral administration and investigated primarily for cognitive enhancement in neurological disorders. Facinicline has demonstrated improvement in cognition and sensorimotor gating in preclinical rodent models. Its mechanism involves enhancing dopamine efflux via α7 nAChR stimulation and modulating acetylcholine release through 5-HT3 antagonism. The drug reached phase 2 clinical trials for Alzheimer's disease and schizophrenia but did not progress further[1][2][3][4][5][7].

Other names
facinicline hydrochlorideRG3487 hydrochlorideRG-3487 hydrochlorideRG 3487 hydrochloride
02

Targets

CHRNA7 (α7 nicotinic receptor)HTR3A (5-hydroxytryptamine receptor 3A)

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