ARIAD Presents New Preclinical Data Showing Ponatinib is a Potent Inhibitor of RET and FGFR, Two Oncogenic Drivers of Non-Small

  ARIAD Presents New Preclinical Data Showing Ponatinib is a Potent Inhibitor
  of RET and FGFR, Two Oncogenic Drivers of Non-Small Cell Lung Cancer

Business Wire

CAMBRIDGE, Mass. & WASHINGTON -- April 8, 2013

ARIAD Pharmaceuticals, Inc. (NASDAQ: ARIA) today announced the presentation of
preclinical data on ponatinib (Iclusig™) , at the American Association for
Cancer Research (AACR) Annual Meeting 2013, in Washington. In separate
studies, ponatinib is shown to potently inhibit RET, a clinically proven
oncogenic driver of medullary thyroid cancer (MTC) and non-small cell lung
cancer (NSCLC), and FGFR, which is commonly mutated in endometrial, lung and
other cancers.

The first preclinical study, “Ponatinib is a highly-potent inhibitor of
activated variants of RET found in MTC and NSCLC,” shows that ponatinib
inhibits naturally occurring activating mutants of RET found in MTC and NSCLC
at clinically achievable plasma concentrations. The potency of ponatinib was
found to substantially exceed that of other approved tyrosine kinase
inhibitors with RET activity. These results provide strong support for the
clinical evaluation of ponatinib in patients with RET-driven cancers.

“The unique design features that allow ponatinib to overcome mutation-based
resistance in CML, including the gatekeeper mutation, also apply to its
activity against its other tyrosine kinase targets including RET, FGFR and
KIT,” stated Timothy P. Clackson, Ph.D., president of research and development
and chief scientific officer at ARIAD. “These preclinical data strongly
support moving forward with evaluating ponatinib in RET-positive cancers, and
we look forward to the start of a Phase 2 investigator-sponsored trial in
patients with RET-positive NSCLC in this second quarter of 2013.”

In the second preclinical study, “Ponatinib potently inhibits the activity of
mutant variants of FGFR commonly found in endometrial, lung and other
cancers,” the ability of ponatinib to inhibit a broad panel of naturally
occurring mutant variants of FGFR1, 2, 3, and 4 was evaluated. Ponatinib
potently blocked a variety of mutant variants of FGFR, with particularly
promising activity against mutant variants of FGFR2 that have been observed in
endometrial and squamous cell carcinomas (SCCs) of the lung. Specifically,
ponatinib inhibits the eight mutants that make up more than 90 percent of the
mutations observed in endometrial cancer patients, and six mutants observed in
SCC at clinically achievable plasma concentrations. Ponatinib also shows
encouraging activity against FGFR1/3 fusion proteins found in glioblastoma
multiforme. These data support clinical evaluation of ponatinib in FGFR-driven
cancers, including a Phase 2 investigator-sponsored trial of ponatinib in
patients with SCCs that is currently underway and enrolling patients.

About ARIAD

ARIAD Pharmaceuticals, Inc., headquartered in Cambridge, Massachusetts and
Lausanne, Switzerland, is an integrated global oncology company focused on
transforming the lives of cancer patients with breakthrough medicines. ARIAD
is working on new medicines to advance the treatment of various forms of
chronic and acute leukemia, lung cancer and other difficult-to-treat cancers.
ARIAD utilizes computational and structural approaches to design
small-molecule drugs that overcome resistance to existing cancer medicines.
For additional information, visit http://www.ariad.comor follow ARIAD on
Twitter (@ARIADPharm).

This press release contains “forward-looking statements” including, but not
limited to, updates on preclinical developments for our product candidates.
Forward-looking statements are based on management's expectations and are
subject to certain factors, risks and uncertainties that may cause actual
results, outcome of events, timing and performance to differ materially from
those expressed or implied by such statements. These risks and uncertainties
include, but are not limited to, preclinical data and early-stage clinical
data that may not be replicated in later-stage clinical studies, the costs
associated with our research, development, manufacturing and other activities,
the conduct, timing and results of pre-clinical and clinical studies of our
product candidates, the adequacy of our capital resources and the availability
of additional funding, and other factors detailed in the Company's public
filings with the U.S. Securities and Exchange Commission. The information
contained in this press release is believed to be current as of the date of
original issue. The Company does not intend to update any of the
forward-looking statements after the date of this document to conform these
statements to actual results or to changes in the Company's expectations,
except as required by law.

Contact:

ARIAD Pharmaceuticals, Inc.
Investors:
Kendra Adams, 617-503-7028
Kendra.adams@ariad.com
or
Media:
Liza Heapes, 617-621-2315
Liza.heapes@ariad.com
 
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