Chelsea Therapeutics Begins Patient Dosing in Second Pivotal Phase III Trial of Droxidopa...

Chelsea Therapeutics Begins Patient Dosing in Second Pivotal Phase III Trial of
Droxidopa in Neurogenic Orthostatic Hypotension

CHARLOTTE, N.C., Sept. 2, 2008 (GLOBE NEWSWIRE) -- Chelsea Therapeutics
International, Ltd. (Nasdaq:CHTP) announced that it has initiated patient dosing
in Study 301, the second of two pivotal Phase III trials designed to demonstrate
efficacy and support U.S. marketing approval of Droxidopa in neurogenic
orthostatic hypotension (NOH).

Study 301 is a multinational, randomized, placebo-controlled, induction-design
Phase III trial evaluating up to 118 patients. The trial is approximately 4
weeks in duration and includes an initial open-label dose titration period of up
to two weeks, after which patients undergo a 7-day washout period prior to
randomization into a 7-day double-blind treatment period. During the open label
dose titration period, all patients will be titrated to maximum therapeutic
benefit with up to 600 mg t.i.d. of Droxidopa and must demonstrate both a blood
pressure and symptomatic improvement. Patients not responding to treatment
during the titration period will be excluded from the trial. All patients
demonstrating improvement will then undergo a 7 day washout period prior to
being equally randomized (N=59) to receive either their respective effective
doses of active drug or placebo for 1 week. At the end of the 1 week blinded,
treatment period, patients are evaluated for changes in symptomatic benefit
relative to that recorded at randomization.

The primary endpoint will be the relative symptomatic change, as measured by the
mean score of Item 1 (dizziness or light-headedness) of the Orthostatic
Hypotension Symptom Assessment (OHSA), 7 days following randomization either to
continued therapy with Droxidopa or to placebo. The OHSA scale is a validated
scale designed to rate symptoms occurring specifically as a result of low blood
pressure and uses an 11-point scale (zero to 10), with more severe symptoms
scoring higher.

Study 301 was reviewed by the U.S. Food and Drug Administration (FDA) and
awarded a Special Protocol Assessment (SPA). An SPA provides a binding agreement
that the study design, including trial size, clinical endpoints and/or data
analyses is acceptable to support regulatory approval. In addition to the SPA,
the FDA recently awarded Chelsea Fast Track designation for its pivotal program
in NOH. Fast Track designation is designed to facilitate the review of products
that address serious or potentially life-threatening conditions for which there
is an unmet medical need and allows a company to file a New Drug Application
(NDA) on a rolling basis. This permits the FDA to review the filing as it is
received, expediting the review process.

"I am pleased to report that we now have both of our pivotal trials in
neurogenic orthostatic hypotension actively recruiting and enrolling patients,"
commented Dr. Simon Pedder, President and CEO of Chelsea. "We are confident in
the design and strength of both of our Phase III trials and believe that
together, the results of Studies 301 and 302 should provide a solid basis to
support approval of Droxidopa in this indication."

About Droxidopa and Symptomatic Neurogenic Orthostatic Hypotension (NOH)

Symptomatic NOH is a neurogenic disorder resulting from a deficient release of
norepinephrine, the neurotransmitter used by sympathetic autonomic nerves to
send signals to the blood vessels and the heart. This deficiency results in
decreased blood pressure when a person assumes a standing position and is
characterized by lightheadedness, dizziness, blurred vision and syncope.
Droxidopa, an orally active synthetic precursor of norepinephrine, increases the
supply of norepinephrine available for delivery to its receptors to improve
orthostatic blood pressure and alleviate symptoms of orthostatic hypotension.

Chelsea estimates that nearly 300,000 patients suffer from chronic symptomatic
NOH in the U.S. and EU combined. In addition to creating significant health care
costs, symptomatic NOH has a dramatic impact on the quality of patient life.
Midodrine, currently the only FDA approved treatment for orthostatic
hypotension, not only fails to treat the underlying cause of symptomatic NOH but
is limited in its use by a pronounced side-effect profile and black box warning
for supine hypertension. Given the chronic nature of symptomatic NOH and the
proven safety and tolerability of Droxidopa, Chelsea expects that daily oral
treatment with Droxidopa should provide a significant improvement in the
long-term treatment of symptomatic NOH.

Droxidopa, developed by and licensed from Dainippon Sumitomo Pharma Co., Ltd.
(DSP), initially received Japanese approval in 1989 for the treatment of frozen
gait and dizziness on standing associated with Parkinson's Disease and for the
treatment of orthostatic hypotension, syncope or dizziness on standing
associated with Shy-Drager syndrome and Familial Amyloidotic Polyneuropathy. In
2000, Droxidopa received expanded marketing approval to include prevention of
vertigo, dizziness and weakness associated with orthostatic hypotension in
hemodialysis patients.

About Chelsea Therapeutics

Chelsea Therapeutics is a biopharmaceutical development company that acquires
and develops innovative products for the treatment of a variety of human
diseases. The Company is currently developing a library of metabolically inert
antifolate compounds engineered to have potent anti-inflammatory and anti-tumor
activity to treat a range of immunological disorders. Early clinical data
suggests that Chelsea's lead antifolate compound, CH-1504, is a safe and
effective treatment alternative to methotrexate for RA and may have further
applications for psoriasis, IBD and certain cancers. Chelsea's antifolate
program is complemented by a strategic partnership with Active Biotech AB for
the joint development of a portfolio of therapeutics targeting immune-mediated
inflammatory disorders and transplantation. In addition to its autoimmune
pipeline, Chelsea is developing Droxidopa, an orally active synthetic precursor
of norepinephrine, for the treatment of neurogenic orthostatic hypotension.
Currently approved and marketed in Japan, Droxidopa has accumulated over 15
years of proven safety and efficacy, historically generating annual revenues of
approximately $50 million in Japan.

This press release contains forward-looking statements regarding future events.
These statements are just predictions and are subject to risks and uncertainties
that could cause the actual events or results to differ materially. These risks
and uncertainties include reliance on collaborations and licenses, risks and
costs of drug development, regulatory approvals, intellectual property risks,
our reliance on our lead drug candidate CH-1504, our history of losses and need
to raise more money, competition, market acceptance for our products if any are
approved for marketing, reliance on key personnel including specifically Dr.
Pedder, management of rapid growth, and the need to acquire or develop
additional products.

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CONTACT: Chelsea Therapeutics
Nick Riehle, Chief Financial Officer
704-341-1516 x101
Kathryn McNeil, Investor/Media Relations
718-788-2856