Pfizer Announces Positive Top-Line Results from Second Phase 3 Trial of Oral XELJANZ® (Tofacitinib Citrate) in Adults with Psoriatic Arthritis

NEW YORK–(BUSINESS WIRE)– Pfizer Inc. (NYSE:PFE) announced today top-line results from Oral
Psoriatic Arthritis triaL (OPAL) Beyond, the second Phase 3 study of
XELJANZ^® (tofacitinib citrate) being investigated in patients
with active psoriatic arthritis (PsA). This study evaluated the efficacy
and safety of tofacitinib 5 mg and 10 mg twice daily (BID) in adult
patients with active PsA who had an inadequate response to at least one
tumor necrosis factor inhibitor (TNFi), making it the first PsA study to
focus exclusively on TNFi-IR patients.¹ OPAL Beyond met its
primary efficacy endpoints demonstrating a statistically significant
(p<0.0001) improvement with tofacitinib 5 mg BID and 10 mg BID compared
to placebo treatment as measured by American College of Rheumatology 20
(ACR20) response and Health Assessment Questionnaire Disability Index
(HAQ-DI) score at 3 months.¹

“There is a significant need for additional PsA treatment options as
many people living with the condition do not respond well to available
therapies,” said Michael Corbo, Category Development Lead, Inflammation
& Immunology, Pfizer Global Innovative Pharmaceuticals Business. “The
positive results of both Phase 3 PsA studies, OPAL Broaden in DMARD-IR
patients and OPAL Beyond in TNFi-IR patients, demonstrate that
tofacitinib, if approved, may have potential to be an important
treatment option to help address unmet needs for patients with PsA.”

Overall safety findings in this study were consistent with those
observed in the broader rheumatology clinical development program for
tofacitinib.

OPAL Beyond is a Phase 3, randomized, double-blind, placebo-controlled,
6-month study investigating the efficacy and safety of tofacitinib 5 mg
and 10 mg twice daily in patients with active PsA who had inadequate
response to at least one TNFi due to lack of efficacy or an adverse
event.¹ A total of 395 subjects enrolled in the study and
were randomized equally to tofacitinib 5 mg BID, tofacitinib 10 mg BID
and placebo. Patients enrolled in the study were required to be on one
conventional synthetic disease modifying antirheumatic drug (csDMARD) as
background therapy and continue that dose for the duration of the study.

About the OPAL Global Clinical Development Program

The OPAL global clinical development program includes two Phase 3
studies, OPAL Broaden and OPAL Beyond, as well as a long-term extension
trial, OPAL Balance. These three studies are expected to form the
potential submission package for possible future regulatory
applications. Positive top-line results for OPAL Broaden were announced
in April 2016. Detailed results for OPAL Broaden and OPAL Beyond are
expected to be submitted for presentation at a future scientific meeting.

About Psoriatic Arthritis

Psoriatic Arthritis (PsA) is a chronic inflammatory multisystem disease.²
PsA causes joint pain and stiffness, skin and nail psoriasis, swollen
toes and fingers, persistent painful tendonitis, and irreversible joint
damage. An estimated 3 million people in the U.S. and Europe combined
have PsA.³ Disease prevalence may even be higher because it
is often misdiagnosed or goes undiagnosed altogether.^4,5,6

About XELJANZ (tofacitinib citrate) and XELJANZ XR (tofacitinib
citrate) extended-release

XELJANZ^®/XELJANZ XR^® (tofacitinib citrate) is a
prescription medicine called a Janus kinase (JAK) inhibitor. In the
United States, XELJANZ XR 11 mg QD is the first and only once-daily oral
JAK inhibitor approved for the treatment of moderate to severe
rheumatoid arthritis (RA).

As the developer of XELJANZ/XELJANZ XR, Pfizer is a leader in JAK
innovation. XELJANZ is approved in more than 45 countries around the
world for the treatment of moderate to severe RA as a second-line
therapy after failure of one or more disease-modifying antirheumatic
drugs (DMARDs).

Pfizer is committed to advancing the science of JAK inhibition and
enhancing understanding of XELJANZ through a robust clinical development
program. The efficacy and safety profile of XELJANZ has been studied in
approximately 6,200 patients with moderate to severe RA, amounting to
more than 19,400 patient-years of drug exposure in the global clinical
development program.

XELJANZ is the only JAK inhibitor included in the 2015 American
College of Rheumatology Guideline for the Treatment of Rheumatoid
Arthritis.⁷

XELJANZ/XELJANZ XR U.S. Label Information

XELJANZ (tofacitinib citrate)/XELJANZ XR (tofacitinib citrate)
extended-release is a prescription medicine called a Janus kinase (JAK)
inhibitor. XELJANZ/XELJANZ XR is used to treat adults with moderately to
severely active rheumatoid arthritis in which methotrexate did not work
well. XELJANZ/XELJANZ XR may be used as a single agent or in combination
with methotrexate (MTX) or other non-biologic disease-modifying
antirheumatic drugs (DMARDs). Use of XELJANZ/XELJANZ XR in combination
with biologic DMARDs or potent immunosuppressants, such as azathioprine
and cyclosporine, is not recommended.

• It is not known if XELJANZ/XELJANZ XR is safe and effective in people
  with hepatitis B or C.
• XELJANZ/XELJANZ XR is not for people with severe liver problems.
• It is not known if XELJANZ/XELJANZ XR is safe and effective in
  children.

Important Safety Information

• XELJANZ/XELJANZ XR can lower the ability of the immune system to
  fight infections. Some people can have serious infections while taking
  XELJANZ/XELJANZ XR, including tuberculosis (TB), and infections caused
  by bacteria, fungi, or viruses that can spread throughout the body.
  Some people have died from these infections. Healthcare providers
  should test patients for TB before starting XELJANZ/XELJANZ XR, and
  monitor them closely for signs and symptoms of TB and other infections
  during treatment. People should not start taking XELJANZ/XELJANZ XR if
  they have any kind of infection unless their healthcare provider tells
  them it is okay.
• People may be at a higher risk of developing shingles.
• XELJANZ/XELJANZ XR may increase the risk of certain cancers by
  changing the way the immune system works. Lymphoma and other cancers,
  including skin cancers, can happen in patients taking XELJANZ/XELJANZ
  XR.
• The risks and benefits of treatment should be considered prior to
  initiating XELJANZ/XELJANZ XR in patients with chronic or recurrent
  infection; who have been exposed to tuberculosis; with a history of a
  serious or an opportunistic infection; who have resided or traveled in
  areas of endemic tuberculosis or endemic mycoses; or with underlying
  conditions that may predispose them to infection.
• Viral reactivation, including cases of herpes virus reactivation
  (e.g., herpes zoster), was observed in clinical studies with XELJANZ.
• Use of live vaccines should be avoided concurrently with
  XELJANZ/XELJANZ XR. Update immunizations in agreement with current
  immunization guidelines prior to initiating XELJANZ/XELJANZ XR therapy.
• Some people who have taken XELJANZ with certain other medicines to
  prevent kidney transplant rejection have had a problem with certain
  white blood cells growing out of control (Epstein Barr
  virus-associated post-transplant lymphoproliferative disorder).
• Some people taking XELJANZ/XELJANZ XR can get tears in their stomach
  or intestines. This happens most often in people who also take
  nonsteroidal anti-inflammatory drugs (NSAIDs), corticosteroids, or
  methotrexate.
• XELJANZ/XELJANZ XR should be used with caution in patients who may be
  at increased risk for gastrointestinal perforation (e.g., patients
  with a history of diverticulitis), or who have a narrowing within
  their digestive tract. Patients should tell their healthcare provider
  right away if they have fever and stomach-area pain that does not go
  away or a change in bowel habits.
• XELJANZ/XELJANZ XR can cause changes in certain lab test results
  including low blood cell counts, increases in certain liver tests, and
  increases in cholesterol levels. Healthcare providers should do blood
  tests before starting patients on XELJANZ/XELJANZ XR and while they
  are taking XELJANZ/XELJANZ XR, to check for these side effects. Normal
  cholesterol levels are important to good heart health. Healthcare
  providers may stop XELJANZ/XELJANZ XR treatment because of changes in
  blood cell counts or liver test results.
• Use of XELJANZ/XELJANZ XR in patients with severe hepatic impairment
  is not recommended.
• Patients should tell their healthcare providers if they plan to become
  pregnant or are pregnant.

It is not known if XELJANZ/XELJANZ XR will harm an unborn baby. To
monitor the outcomes of pregnant women exposed to XELJANZ/XELJANZ XR, a
registry has been established. Physicians are encouraged to register
patients and pregnant women are encouraged to register themselves by
calling 1-877-311-8972.

• Patients should tell their healthcare providers if they plan to
  breastfeed or are breastfeeding. Patients and their healthcare
  provider should decide if they will take XELJANZ/XELJANZ XR or
  breastfeed. They should not do both.
• In carriers of the hepatitis B or C virus (viruses that affect the
  liver), the virus may become active while using XELJANZ/XELJANZ XR.
  Healthcare providers may do blood tests before and during treatment
  with XELJANZ/XELJANZ XR.
• Common side effects include upper respiratory tract infections (common
  cold, sinus infections), headache, diarrhea, and nasal congestion,
  sore throat, and runny nose (nasopharyngitis).

Please click the direct link to the full prescribing information for
XELJANZ/XELJANZ XR, including boxed warning and Medication Guide: http://labeling.pfizer.com/ShowLabeling.aspx?id=959.

Pfizer Inc.: Working together for a healthier world^®

At Pfizer, we apply science and our global resources to bring therapies
to people that extend and significantly improve their lives. We strive
to set the standard for quality, safety and value in the discovery,
development and manufacture of healthcare products. Our global portfolio
includes medicines and vaccines as well as many of the world’s
best-known consumer healthcare products. Every day, Pfizer colleagues
work across developed and emerging markets to advance wellness,
prevention, treatments and cures that challenge the most feared diseases
of our time. Consistent with our responsibility as one of the world’s
premier innovative biopharmaceutical companies, we collaborate with
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DISCLOSURE NOTICE: The information contained in this release is as of
June 7, 2016. Pfizer assumes no obligation to update forward-looking
statements contained in this release as the result of new information or
future events or developments.

This release contains forward-looking information about a potential
new indication for XELJANZ for the treatment of adults with active
psoriatic arthritis (the “potential indication”), including its
potential benefits, that involves substantial risks and uncertainties
that could cause actual results to differ materially from those
expressed or implied by such statements. Risks and uncertainties
include, among other things, the uncertainties inherent in research and
development, including the ability to meet anticipated trial
commencement and completion dates and regulatory submission dates, as
well as the possibility of unfavorable clinical trial results, including
unfavorable new clinical data and additional analyses of existing
clinical data; uncertainties regarding the commercial success of XELJANZ
and XELJANZ XR; whether and when any applications for the potential
indication may be filed with regulatory authorities in any
jurisdictions; whether and when regulatory authorities in any
jurisdictions may approve such applications and/or any other
applications that are pending or may be filed for XELJANZ or XELJANZ XR,
which will depend on the assessment by such regulatory authorities of
the benefit-risk profile suggested by the totality of the efficacy and
safety information submitted; decisions by regulatory authorities
regarding labeling and other matters that could affect the availability
or commercial potential of XELJANZ and XELJANZ XR, including the
potential indication; and competitive developments.

A further description of risks and uncertainties can be found in
Pfizer’s Annual Report on Form 10-K for the fiscal year ended December
31, 2015 and in its subsequent reports on Form 10-Q, including in the
sections thereof captioned “Risk Factors” and “Forward-Looking
Information and Factors That May Affect Future Results”, as well as in
its subsequent reports on Form 8-K, all of which are filed with the U.S.
Securities and Exchange Commission and available at www.sec.gov and www.pfizer.com.

¹ OPAL Beyond (A3921125) Study Protocol.

² Ritchlin CT, Kavanaugh A, Gladman DD, et al. Treatment
recommendations for psoriatic arthritis. Ann Rheum Dis.
2009;68(9):1387-1394.

³ Data on File. Decision Resources Group. Table 1-4: Number
of Total Prevalent Cases of Psoriatic Arthritis in the Major
Pharmaceutical Markets, 2013-2023. United States and Europe, 2016.

⁴ Van de Kerkhof PCM, Reich K, Kavanaugh A, et al. Physician
perspectives in the management of psoriasis and psoriatic arthritis:
results from the population-based Multinational Assessment of Psoriasis
and Psoriatic Arthritis survey. J Eur Acad Dermatol Venereol.
2015.

⁵ Helliwell P, Coates L, Chandran V, et al. Qualifying unmet
needs and improving standards of care in psoriatic arthritis. Arthritis
Care Res (Hoboken). 2014;66(12):1759-1766.

⁶ National Psoriasis Foundation. 2011 Survey Panel Snapshot. http://www.psoriasis.org/document.doc?id=1782.
Accessed July 15, 2015.

⁷ Singh, J. A., Saag, K. G., Bridges, S. L., et al. 2015
American College of Rheumatology Guideline for the Treatment of
Rheumatoid Arthritis. Arthritis & Rheumatology. doi: 10.1002/art.39480.

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