AstraZeneca Announces Top-Line Results From OSKIRA-1 Phase 3 Study of Fostamatinib in Rheumatoid Arthritis

    AstraZeneca Announces Top-Line Results From OSKIRA-1 Phase 3 Study of
                     Fostamatinib in Rheumatoid Arthritis

PR Newswire

SOUTH SAN FRANCISCO, Calif., April 5, 2013

SOUTH SAN FRANCISCO, Calif., April 5, 2013 /PRNewswire/ --AstraZeneca today
announced top-line results of OSKIRA-1, a Phase 3 study to assess the efficacy
and safety of fostamatinib, the first oral spleen tyrosine kinase (SYK)
inhibitor in development for rheumatoid arthritis (RA). OSKIRA-1 had two
primary endpoints: assessing signs and symptoms of RA as measured by ACR20
response rates, and an X-ray endpoint known as mTSS (modified Total Sharp

In the OSKIRA-1 study, fostamatinib achieved a statistically significant
improvement in ACR20 response rate at 24 weeks in both the 100 mg twice daily
group and the group that received 100 mg twice daily for four weeks followed
by 150 mg once daily (49%, p<0.001 and 44%, p=0.006 respectively) compared to
placebo (34%). Fostamatinib did not demonstrate a statistically significant
difference in mTSS compared to placebo at 24 weeks for either dose (p=0.252
and p=0.170, respectively).

The safety and tolerability findings for fostamatinib observed in the OSKIRA-1
study were generally consistent with those previously reported for the TASKi
Phase 2 program. The most commonly reported adverse events were typical of
those seen in earlier studies, including hypertension, diarrhea, nausea,
headache and nasopharyngitis (common cold).

Briggs Morrison, MD, executive vice president of Global Medicines Development
and chief medical officer, said: "These top-line results provide important
information on the efficacy and safety of fostamatinib and demonstrate that
the compound has an effect on the signs and symptoms of rheumatoid arthritis.
We will await the results of the remaining Phase 3 studies, OSKIRA-2 and
OSKIRA-3, to further evaluate and characterize the profile of fostamatinib as
a potential treatment for rheumatoid arthritis."

OSKIRA-1 randomized 923 patients who had experienced an inadequate response to
methotrexate (MTX) and, over a 24-week period, evaluated the effectiveness of
two dosing regimens of fostamatinib (100 mg twice daily or fostamatinib 100 mg
twice daily for four weeks followed by 150 mg once daily) in combination with
MTX versus placebo in combination with MTX. Patients on fostamatinib remained
on treatment in OSKIRA-1 for 12 months.

The OSKIRA-2 and OSKIRA-3 results are expected later in the second quarter of

About ACR20 and mTSS

The American College of Rheumatology (ACR) score represents a percentage
improvement in symptoms (tenderness and swelling in the joints). 28 joints are
evaluated for tenderness and swelling respectively (prior to taking any
required analgesic that day if possible). To qualify for an ACR20 score, a
person with RA must have at least 20% fewer tender joints and at least 20%
fewer swollen joints. He or she must also show a 20% improvement in at least
three of the following five areas: 1) the person's overall (global) assessment
of his or her own RA, 2) the physician's global assessment of the person's RA,
3) the person's assessment of his or her own pain, 4) the person's assessment
of his or her own physical functioning, and 5) the results of an erythrocyte
sedimentation rate or C-reactive protein blood test (both of which test for

Radiographic mTSS is measured in the hands and feet using X-rays. mTSS is a
measure of bone erosion and joint space narrowing on X-rays. In each hand, 16
areas are measured for erosions and 15 areas are measured for joint space
narrowing. In each foot, six areas are measured for erosions and six areas are
measured for joint space narrowing. A smaller change in mTSS over a given
time period, given in percentage change of mTSS score, reflects less
progression of joint damage.

About the OSKIRA program

The ongoing (Oral SYK Inhibition in Rheumatoid Arthritis) OSKIRA program, has
been designed to investigate fostamatinib as a potential new oral treatment
option for rheumatoid arthritis and an alternative to injectable therapies for
patients with an inadequate response to conventional Disease Modifying
Anti-Rheumatic Drugs (DMARDs), including methotrexate (OSKIRA-1 and OSKIRA-2)
and those with an inadequate response to TNF-α antagonists (OSKIRA-3).

About Fostamatinib

Fostamatinib (previously referred to as R788) is the first oral spleen
tyrosine kinase (SYK) inhibitor in development for rheumatoid arthritis. In
February 2010, AstraZeneca and Rigel Pharmaceuticals announced a worldwide
license agreement whereby AstraZeneca would develop and commercialize

About Rheumatoid Arthritis (RA)

Rheumatoid arthritis is a systemic autoimmune disease whereby the immune
system attacks the joints, causing pain, swelling to the surrounding tissue
and damage to the cartilage and bone. The disease affects approximately one in
100 people worldwide.

If not adequately treated, RA can destroy cartilage and bone within joints,
leading to serious disability and can be associated with reduced life
expectancy. Not all RA patients have a satisfactory response to existing
therapies because the disease pathology may differ from one individual to
another and a considerable unmet need remains.

In the US alone the total annual societal cost of RA is estimated to amount to
$39.2 billion, with even greater indirect costs to individuals and society
including costs from diminished work capacity, loss of productivity, loss in
earnings and loss in tax contributions.

About Rigel

Rigel Pharmaceuticals, Inc. (Nasdaq: RIGL) is a clinical-stage drug
development company that discovers and develops novel, small-molecule drugs
for the treatment of inflammatory and autoimmune diseases, as well as muscle
disorders. Rigel's pioneering research focuses on intracellular signalling
pathways and related targets that are critical to disease mechanisms. Rigel's
productivity has resulted in strategic collaborations with large
pharmaceutical partners to develop and market its product candidates. Current
product development programs include fostamatinib, an oral SYK inhibitor that
is in Phase 3 clinical trials for RA with its partner AstraZeneca; R343, an
inhaled SYK inhibitor for asthma and R333, a topical JAK/SYK inhibitor for
discoid lupus – both of which have commenced Phase 2 clinical trials; and,
R348, a topical JAK/SYK inhibitor in a Phase 1 clinical trial for the
treatment of chronic dry eye. For more information, visit

About AstraZeneca

AstraZeneca is a global, innovation-driven biopharmaceutical business that
focuses on the discovery, development and commercialisation of prescription
medicines, primarily for the treatment of cardiovascular, metabolic,
respiratory, inflammation, autoimmune, oncology, infection and neuroscience
diseases. AstraZeneca operates in over 100 countries and its innovative
medicines are used by millions of patients worldwide. For more information
please visit:

This press release contains "forward-looking" statements, including, without
limitation, statements related to the further development of, and the
therapeutic and commercial potential of, fostamatinib, partnered with
AstraZeneca, the results of the ongoing OSKIRA-2 and OSKIRA-3 Phase 3 studies
and the timing of completion of those studies, and the timing for potential
regulatory filings and publications of clinical data. Any statements contained
in this press release that are not statements of historical fact may be deemed
to be forward-looking statements. Words such as "planned," "will," "may,"
"expect," and similar expressions are intended to identify these
forward-looking statements. These forward-looking statements are based on
Rigel's current expectations and inherently involve significant risks and
uncertainties. Actual results and the timing of events could differ materially
from those anticipated in such forward looking statements as a result of these
risks and uncertainties, which include, without limitation, the uncertain
timing of completion of and the success of clinical trials and the potential
problems that may arise in the clinical development process, the uncertain and
time-consuming regulatory filing and approval process, the availability of
resources to develop Rigel's product candidates, the uncertain therapeutic and
commercial value of fostamatinib, market competition, risks associated with
and Rigel's dependence on Rigel's corporate partnerships, as well as other
risks detailed from time to time in Rigel's reports filed with the Securities
and Exchange Commission, including its Annual Report on Form 10-K for the year
ended December 31, 2012. Rigel does not undertake any obligation to update
forward-looking statements and expressly disclaims any obligation or
undertaking to release publicly any updates or revisions to any
forward-looking statements contained herein.

Rigel Investor Enquiries
Raul Rodriguez
Phone: 650.624.1302
Rigel Media Enquiries
Media Contact: Susan C. Rogers, Alchemy Consulting, Inc.
Phone: 650.430.3777
AstraZeneca Media Enquiries
Esra Erkal-Paler              +44 20 7604 8030 (UK/Global)
Vanessa Rhodes                +44 20 7604 8037 (UK/Global)
Ayesha Bharmal                +44 20 7604 8034 (UK/Global)
Jacob Lund                    +46 8 553 260 20 (Sweden)
AstraZeneca Investor Enquiries
James Ward-Lilley             +44 20 7604 8122 mob: +44 7785 432613
Karl Hard                     +44 20 7604 8123 mob: +44 7789 654364
Colleen Proctor               +1 302 886 1842  mob: +1 302 357 4882
Ed Seage                      +1 302 886 4065  mob: +1 302 373 1361

SOURCE Rigel Pharmaceuticals, Inc.

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