Targacept, Inc., a clinical-stage biopharmaceutical company, has initiated phase I clinical trial of TC-2216, its product candidate for the treatment of depression and anxiety disorders.

The trial is designed to evaluate the safety and tolerability of TC-2216 and to assess its pharmacokinetic profile. The trial is a double-blind, placebo-controlled crossover study, with sequential ascending single oral doses administered to healthy male volunteers, a Targacept press release stated.

TC-2216 is a novel compound discovered using Targacept's proprietary drug design platform known as Pentad. The compound targets specific neuronal nicotinic receptors (NNRs), a class of receptors found in the central nervous system that play a critical role in regulating nervous system activity. TC-2216 selectively inhibits the alpha4beta2 NNR to modulate the release of neurotransmitters that are involved in mood regulation. In preclinical studies, TC-2216 showed greater potency than and anti-depressant effects comparable to selective serotonin reuptake inhibitors and tricyclics, which are commonly used treatments for depression, as well as anxiety-relieving effects.

Targacept currently plans to develop TC-2216 as an oral monotherapy. In November, the company announced positive top line results from a Phase II clinical trial of Tridmac, a treatment combination comprised of mecamylamine hydrochloride as an augmentation therapy to citalopram hydrobromide, in patients who did not respond adequately to citalopram alone. Mecamylamine hydrochloride binds non-selectively to various NNR subtypes, but there is a body of scientific evidence that suggests that its anti-depressant activity is derived through its antagonism at the alpha4beta2 NNR.

"Depression is a highly debilitating illness, and millions of people who suffer with it are not gaining adequate relief from existing therapies," said J. Donald deBethizy, Ph.D., Targacept's president and chief executive officer. "The results of our Tridmac trial not only substantiate the promise of the NNR mechanism in the treatment of depression and other mood disorders, but also further bolster our enthusiasm for the potential of TC-2216."

Targacept is a clinical-stage biopharmaceutical company that discovers and develops NNR Therapeutics, a new class of drugs for the treatment of central nervous system diseases and disorders. Targacept's product candidates selectively modulate neuronal nicotinic receptors that serve as key regulators of the nervous system activity to promote therapeutic effects and limit adverse side effects.

Targacept has product candidates in development for Alzheimer's disease and cognitive deficits in schizophrenia, pain and depression, and multiple preclinical programs. Targacept is located in Winston-Salem, North Carolina.