ARIAD Announces Results of Preclinical Studies on AP32788 at the Annual Meeting of the American Association for Cancer Research
April 19 2016 - 7:35AM
Business Wire
First Presentation of Preclinical Data
Supports Upcoming Clinical Testing in Non-Small Cell Lung Cancer
Patients with EGFR and HER2 Exon 20 Mutations
ARIAD Pharmaceuticals, Inc. (NASDAQ: ARIA) today announced the
results of comprehensive preclinical studies on its investigational
tyrosine kinase inhibitor (TKI), AP32788, at the American
Association for Cancer Research (AACR) Annual Meeting 2016. AP32788
is a TKI designed to target specific mutations in EGFR or HER2
present in a subset of patients with non-small cell lung cancer
(NSCLC), for whom there are currently no targeted therapies
available. The Phase 1/2 clinical trial of AP32788 is expected to
begin patient enrollment in the second quarter of 2016.
The data presented were included in an oral presentation
entitled, “AP32788, a potent, selective inhibitor of EGFR and HER2
oncogenic mutants, including exon 20 insertions, in preclinical
models.” The research conducted by ARIAD scientists showed that in
a matched set of engineered cell lines, AP32788 inhibited all
tested EGFR and HER2 mutants, including exon 20 insertion mutants,
with selectivity over wild-type (WT) EGFR. Inhibition of WT EGFR in
non-tumor cells has been associated with dose-limiting toxicities
of EGFR inhibitors in patients. Enzymatic analysis confirmed that
AP32788 irreversibly inactivated EGFR exon 20 with 20-fold
selectivity over WT EGFR, in contrast to other tested EGFR TKIs.
AP32788 also induced tumor regressions in a mouse EGFR exon 20
model at doses that were well tolerated.
“These preclinical data on AP32788 demonstrate its potential to
potently inhibit exon 20 mutant forms of EGFR and HER2, that are
not addressed by currently available TKI treatments,” said Timothy
P. Clackson, Ph.D., president of research and development and chief
scientific officer at ARIAD. “The selectivity data suggest that
efficacious levels of exposure to AP32788 may be achievable in
patients with these challenging mutations —a hypothesis we will be
testing in the Phase 1/2 trial. We believe AP32788 is the first TKI
that has been designed and optimized to inhibit the underlying
mutation present in these orphan oncology disease subsets.”
About Non-Small Cell Lung Cancer, EGFR and HER2
Non-small cell lung cancer (NSCLC) is the most common form of
lung cancer, accounting for approximately 85 percent of the
estimated 221,200 new cases of lung cancer diagnosed in 2015 in the
United States, according to the American Cancer Society. EGFR
mutations represent the largest known, targetable subset of NSCLC.
While the most common types of EGFR mutation are addressed by
approved TKI therapies, there are no targeted treatment options
available for the approximately 4 to 9 percent of EGFR-mutated lung
tumors with exon 20 insertion mutations1. In addition, patients
with HER2 mutations, mostly exon 20 insertion mutations, comprise
approximately 2 percent of NSCLC patients2 and also have no current
treatment options. ARIAD estimates that there are approximately
6,000 patients in the United States living with EGFR exon 20 or
HER2 point mutations, based on available data from 2014 on the
number of Stage IIIB or IV NSCLC and the estimated percentage of
patients with these mutations.
About AP32788
AP32788 is an investigational oral tyrosine kinase inhibitor
(TKI) of activating mutations in EGFR and HER2. The molecule was
designed to address the unmet need in patients with non-small cell
lung cancer (NSCLC) driven by exon 20 insertion mutations in EGFR
and HER2, and is ARIAD’s fourth internally discovered oncology IND
to be cleared for clinical development.
About ARIAD
ARIAD Pharmaceuticals, Inc., headquartered in Cambridge,
Massachusetts and Lausanne, Switzerland, is an orphan 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 orphan 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.com or follow ARIAD on Twitter
(@ARIADPharm).
Forward-Looking Statements
This press release contains forward-looking statements, each of
which are qualified in their entirety by this cautionary statement.
Any statements contained herein which do not describe historical
facts, including, but not limited to our statements about the
timing of expected patient enrollment in the Phase 1/2 clinical
trial of AP32788 and the statements made by Dr. Clackson, are
forward-looking statements that 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 factors, risks and uncertainties
include, but are not limited to, our ongoing strategic review, our
ability to successfully commercialize and generate profits from
sales of Iclusig and our product candidates, if approved;
competition from alternative therapies; our ability to meet
anticipated clinical trial commencement, enrollment and completion
dates and regulatory filing dates for our products and product
candidates and to move new development candidates into the clinic;
our ability to execute on our key corporate initiatives; regulatory
developments and safety issues, including difficulties or delays in
obtaining regulatory and pricing and reimbursement approvals to
market our products; our reliance on the performance of third-party
manufacturers and specialty pharmacies for the supply and
distribution of our products and product candidates; the occurrence
of adverse safety events with our products and product candidates;
the costs associated with our research, development, manufacturing,
commercialization and other activities; the conduct, timing and
results of preclinical and clinical studies of our products and
product candidates, including that preclinical data and early-stage
clinical data may not be replicated in later-stage clinical
studies; the adequacy of our capital resources and the availability
of additional funding; the ability to satisfy our contractual
obligations, including under our leases, convertible debt and
royalty financing agreements; patent protection and third-party
intellectual property claims; litigation; our operations in foreign
countries; risks related to key employees, markets, economic
conditions, health care reform, prices and reimbursement rates; and
other risk factors detailed in our public filings with the U.S.
Securities and Exchange Commission, including our most recent
Annual Report on Form 10-K and subsequent Quarterly Reports on Form
10-Q. Except as otherwise noted, these forward-looking statements
speak only as of the date of this press release and we undertake no
obligation to update or revise any of these statements to reflect
events or circumstances occurring after this press release. We
caution investors not to place considerable reliance on the
forward-looking statements contained in this press release.
1 Costa, D. 2015. EGFR Exon 20 Insertion in Non-Small Cell Lung
Cancer. My Cancer Genome
http://www.mycancergenome.org/content/disease/lung-cancer/egfr/64/http://www.mycancergenome.org/content/disease/lung-cancer/egfr/64/
(Updated November 5, 2015).
2 JCO April 22, 2013 JCO.2012.45.6095
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version on businesswire.com: http://www.businesswire.com/news/home/20160419005162/en/
ARIAD Pharmaceuticals, Inc.For InvestorsMaria Cantor,
617-621-2208Maria.cantor@ariad.comorFor MediaLiza Heapes,
617-621-2315Liza.heapes@ariad.com
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