Profile: Targacept, Inc. (TRGT.O)

Targacept, Inc., incorporated in 1997, is a biopharmaceutical company engaged in the design, discovery and development of neuronal nicotinic receptors (NNR) Therapeutics for the treatment of multiple diseases and disorders of the central nervous system. The Company has clinical-stage product candidates for target indications in three therapeutic areas, which includes cognitive impairment, depression and anxiety, and pain. It also has preclinical programs focused in smoking cessation, addiction, obesity, pain, Parkinson’s disease and inflammation. The Company has collaboration with AstraZeneca and an alliance with GlaxoSmithKline. The drug discovery activities utilize computer-based molecular design methodologies and biological data for a library of compounds developed and collected over more than 20 years. The technologies are referred to as Pentad. The Company use Pentad to design or optimize AZD3480 (TC-1734), TC-5619, TC-2216 and TC-6499.

TC-5214

TC-5214 modulates the activity of various NNR subtypes, including multiple forms of the a4ß2 NNR. The Company is conducting an ongoing Phase 2b clinical trial of TC-5214 as an augmentation treatment in subjects with major depressive disorder who do not respond well to first-line treatment with the marketed drug citalopram hydrobromide. The Company may also conduct development of TC-5214 in one or more other indications.

TC-5214 is one of the two enantiomers of mecamylamine hydrochloride. Enantiomers are mirror images of each other that have the same chemical but potentially different biological properties and together form a chemical mixture known as a racemate. It completed a Phase 2 clinical trial of the racemate mecamylamine hydrochloride as an augmentation treatment in subjects with major depressive disorder who did not respond well to first-line treatment with citalopram. In its evaluation in various preclinical models of depression, TC-5214 more often exhibited antidepressant activity, had equal or superior potency and exhibited a more favorable safety profile as compared to mecamylamine. The Company has no current plans to conduct further clinical development of racemic mecamylamine and intend instead to develop TC-5214.

AZD3480 (TC-1734), AZD1446 (TC-6683) and AstraZeneca Collaboration

AZD3480 (TC-1734) is a small molecule that modulates the activity of the a4ß2 NNR. The Company has a collaborative research and license agreement with AstraZeneca AB for the development of AZD3480 as a treatment for various conditions characterized by cognitive impairment, including Alzheimer’s disease and ADHD. It and AstraZeneca are conducting an ongoing exploratory Phase 2 trial of AZD3480 in adults with ADHD. During the year ended December 31, 2008, AstraZeneca completed two Phase 2b clinical trials of AZD3480, one in mild to moderate Alzheimer’s disease and one in cognitive dysfunction in schizophrenia. In December 2008, it and AstraZeneca announced that AZD3480 is not expected to be advanced into Phase 3 clinical development in cognitive dysfunction in schizophrenia.

TC-5619

TC-5619 is a small molecule that it plans to develop for cognitive dysfunction in schizophrenia or potentially one or more other conditions characterized by cognitive impairment. TC-5619 modulates the activity of the a7 NNR. It completed a Phase 1 single rising dose clinical trial and a Phase 1 multiple rising dose clinical trial of TC-5619 in healthy volunteers. In a single rising dose trial, each subject in a dose group receives a single dose of the agent being evaluated, with subjects in each subsequent dose group receiving a pre-determined higher dosage than subjects in the preceding dose group. In a multiple rising dose clinical trial, each subject in a dose group receives a dosage of the agent being evaluated multiple times, with subjects in each subsequent dose group receiving a pre-determined higher dosage than subjects in the preceding dose group.

TC-2216 or enantiomer

TC-2216 is a product candidate for depression and anxiety disorders. TC-2216, which is a racemate, and its enantiomers inhibit the activity of the a4ß2 NNR. It completed a Phase 1 single rising dose clinical trial of TC-2216 in healthy volunteers.

The Company competes with AstraZeneca, Eli Lilly, Sanofi-Aventis, Wyeth, Bristol Myers Squibb, GlaxoSmithKline, Johnson & Johnson, Novartis, NeuroSearch A/S, Solvay, Servier, CoMentis, EnVivo Pharmaceuticals, Xytis and Galantos Pharma.