Pfizer Announces Positive Top-Line Results from Pivotal Phase 3 Maintenance Trial of Oral XELJANZ® (Tofacitinib Citrate) in Ulcerative Colitis

NEW YORK–(BUSINESS WIRE)– Pfizer Inc. (NYSE:PFE) announced today top-line results from Oral
Clinical Trials for tofAcitinib in ulceratiVE colitis (OCTAVE) Sustain,
the third Phase 3 study of XELJANZ^® (tofacitinib citrate)
being investigated in patients with moderately to severely active
ulcerative colitis (UC). OCTAVE Sustain is a 52 week study that
evaluated oral tofacitinib 5 mg and 10 mg twice daily (BID) as a
maintenance treatment in adult patients with moderately to severely
active UC who previously completed and achieved clinical response in
either the OCTAVE Induction 1 or OCTAVE Induction 2 studies.

Top-line results from the OCTAVE Sustain study showed that the
proportion of patients in remission at week 52, the primary efficacy
endpoint, was significantly greater in both the tofacitinib 5 and 10 mg
BID groups compared to placebo. In OCTAVE Sustain, remission was defined
as total Mayo score^a ≤2, no subscore >1, and rectal bleeding
subscore of 0. No new or unexpected safety findings for
tofacitinib were observed in the study.

“Ulcerative colitis is a chronic, often debilitating inflammatory
condition that can be difficult to treat. There are a limited number of
therapies available and patients need additional treatment options” said
Michael Corbo, PhD, Chief Development Officer, Inflammation &
Immunology, Pfizer, Inc. “These findings, along with the previously
released positive induction data from the OCTAVE studies, are
encouraging and provide evidence that tofacitinib, if approved, has the
potential to be an effective new oral treatment option that both induces
and maintains remission. We are proud to advance our clinical
development program for tofacitinib as we work to bring a potential new
treatment option to patients living with ulcerative colitis.”

OCTAVE Sustain is a Phase 3, randomized, double-blind,
placebo-controlled, parallel group, multi-center study. A total of 593
patients were randomized to tofacitinib 5 mg BID, tofacitinib 10 mg BID
and placebo BID. Detailed analyses of OCTAVE Sustain, including
additional efficacy and safety data, will be submitted for presentation
at a future scientific meeting.

About the OCTAVE Clinical Development Program

The OCTAVE global clinical development program includes three Phase 3
studies, OCTAVE Induction 1, OCTAVE Induction 2, and OCTAVE Sustain, as
well as a long-term extension trial, OCTAVE Open. We expect that these
four studies will form the submission package to regulatory authorities
for a potential UC indication.

OCTAVE Induction 1 and OCTAVE Induction 2 are two replicate Phase 3
placebo-controlled studies that evaluated induction of remission by oral
tofacitinib 10 mg BID in adult patients with moderately to severely
active UC. Subjects needed to have failed or been intolerant to UC
treatments including corticosteroids, thiopurines or tumor necrosis
factor inhibitors (TNFi).

OCTAVE Sustain is a Phase 3 placebo-controlled study evaluating oral
tofacitinib 5 mg and 10 mg BID as maintenance therapy in adult patients
with moderately to severely active UC.

OCTAVE Open is an ongoing open-label extension study designed to assess
the safety and tolerability of tofacitinib 5 mg and 10 mg BID in
patients who have completed or who have had treatment failure in OCTAVE
Sustain or who were non-responders upon completing OCTAVE Induction 1 or
2.

About Ulcerative Colitis

UC is a chronic, often debilitating inflammatory bowel disease that
affects millions of people worldwide. It is believed that UC
is the result of complex interactions between multiple factors that
include the environment, genetic predisposition, immune response, and
the gut microbiome in the colon or intestines. It can cause abdominal
pain, fever, weight loss and chronic, bloody diarrhea. UC can
have an effect on work, family and social activities. In up to one-third
of patients with UC, treatment is not completely successful or
complications arise. Under these circumstances, surgery to remove the
colon (colectomy) may be considered. Even after surgery, certain
symptoms of UC may still persist.

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.

References available upon request

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
health care providers, governments and local communities to support and
expand access to reliable, affordable health care around the world. For
more than 150 years, Pfizer has worked to make a difference for all who
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DISCLOSURE NOTICE: The information contained in this release is as of
July 28, 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 adult patients with
moderately to severely active UC (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.

^a Mayo score is a measurement index comprised of four
categories (stool frequency, rectal bleeding, findings on endoscopy,
physician global assessment) that are each rated from 0 (normal) to 3
(most severe) for a total score that ranges from 0-12.

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