Drug intelligence / Profile preview

TC-2216

Development stage
Phase 1
Lead developer
Targacept
Modality
Small Molecules
Administration
Oral
01

Overview

TC-2216 is a small molecule drug developed by Targacept and initially by Catalyst KK as an oral treatment for depression and anxiety disorders. It acts as a partial agonist/antagonist at neural nicotinic acetylcholine receptors (nAChRs), with selectivity for the alpha4beta2 subtype. The compound modulates neurotransmitter release involved in mood regulation and has shown antidepressant effects comparable to selective serotonin reuptake inhibitors and tricyclics in preclinical studies. Although it reached phase I clinical trials for anxiety and depression, development was discontinued due to lack of therapeutic success; however, it remains used in pharmacological research as an alpha4beta2-selective antagonist[1][2][3][4].

Other names
TC 2216TC2216TC-2216TC-2216 trihydrochlorideTC2216 trihydrochlorideTC 2216 trihydrochloride1,7-DIAZASPIRO(4.4)NONANE, 7-(3-PYRIDINYL)-, HYDROCHLORIDE (1:3)
02

Targets

α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)

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