Targacept Initiates Phase I Clinical Trial Of TC-2216

Targacept, Inc.
(Nasdaq: TRGT), a clinical-stage biopharmaceutical company developing a new
class of drugs known as NNR Therapeutics(TM), today announced that it has
initiated a 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.



TC-2216 is a novel compound discovered using Targacept's proprietary
drug design platform known as Pentad(TM). 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(TM), 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."



About Targacept



Targacept is a clinical-stage biopharmaceutical company that discovers
and develops NNR Therapeutics(TM), 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. For more information
about Targacept, please visit targacept.

















Forward-Looking Statements



Any statements in this press release about expectations, plans and
prospects for Targacept, Inc., including, without limitation, statements
regarding the progress, timing and scope of research and development of TC-
2216 and related regulatory filings and clinical trials, and all other
statements that are not purely historical in nature, constitute "forward-
looking statements" within the meaning of the Private Securities Litigation
Reform Act of 1995. Without limiting the foregoing, the words "may,"
"will," "could," "would," "should," "expect," "intend," "plan,"
"anticipate," "believe," "estimate," "predict," "project," "potential,"
"promise," "continue," "ongoing" and similar expressions are intended to
identify forward-looking statements. Actual results may differ materially
from those expressed or implied by forward-looking statements as a result
of various important factors, including our critical accounting policies
and risks and uncertainties relating to: the results of non-clinical
studies and assessments and clinical trials with respect to TC-2216 or our
other current and future product candidates in development; the conduct of
clinical trials, including the performance of third parties that we engage
to execute the trials and difficulties or delays in the completion of
patient enrollment or data analysis; and the timing and success of
submission, acceptance and approval of regulatory filings. These and other
risks and uncertainties are described in greater detail under the heading
"Risk Factors" in our most recent Quarterly Report on Form 10-Q and in
other filings that we make with the Securities and Exchange Commission. As
a result of the risks and uncertainties, the results or events indicated by
the forward-looking statements may not occur. We caution you not to place
undue reliance on any forward-looking statement.



In addition, any forward-looking statements in this release represent
our views only as of the date of this release and should not be relied upon
as representing our views as of any subsequent date. We anticipate that
subsequent events and developments may cause our views to change. Although
we may elect to update these forward-looking statements publicly at some
point in the future, whether as a result of new information, future events
or otherwise, we specifically disclaim any obligation to do so, except as
required by applicable law. Our forward-looking statements do not reflect
the potential impact of any future acquisitions, mergers, dispositions,
joint ventures or investments we may make.


Targacept, Inc.

targacept