dexmecamylamine

Dexmecamylamine (TC-5214) is the S-enantiomer of mecamylamine, a non-selective and non-competitive antagonist of neuronal nicotinic acetylcholine receptors (nAChRs). It was developed as a nicotinic channel modulator intended to treat various neuropsychiatric and autonomic disorders. The drug was most notably investigated in a large-scale Phase III clinical program (the RENAISSANCE program) by AstraZeneca and Targacept as an adjunct therapy for patients with major depressive disorder (MDD) who had an inadequate response to SSRI or SNRI antidepressants. The therapeutic hypothesis was based on the role of cholinergic signaling in mood regulation. However, dexmecamylamine failed to meet its primary efficacy endpoints in these trials, leading to the discontinuation of its development for depression. Subsequently, the compound was explored by Atacama Therapeutics for the treatment of primary palmar hyperhidrosis (excessive sweating of the palms) and has also been studied for overactive bladder.

Other names

S-mecamylamine(S)-mecamylamine(S)-(+)-mecamylamine