ARIAD Presents Preclinical Data on Deforolimus and Bicalutamide in Androgen-Independent...

ARIAD Presents Preclinical Data on Deforolimus and Bicalutamide in Androgen-Independent Prostate Cancer

Phase 2 clinical trial evaluating the same combination now
underway in prostate cancer patients
CAMBRIDGE, Mass.--(Business Wire)--
ARIAD Pharmaceuticals, Inc. (NASDAQ: ARIA) today presented
preclinical data on the investigational mTOR inhibitor, deforolimus,
alone or in combination with the anti-androgen agent, bicalutamide, in
models of prostate cancer. This investigational study shows that the
combination inhibits the growth of prostate cancer cell lines in
various model systems. The data were presented at the EORTC-NCI-AACR
(ENA) symposium on "Molecular Targets and Cancer Therapeutics" held in
Geneva, Switzerland this week and provide the scientific rationale for
an ongoing Phase 2 clinical trial examining the same combination in
patients with advanced prostate cancer.

Preclinical studies showed that the combination of deforolimus and
bicalutamide had anti-tumor activity in an established prostate cancer
model. Together, these agents were also found to inhibit the mTOR and
androgen receptor signaling pathways in prostate cancer cells.
Prostate specific antigen (PSA) levels are controlled by the androgen
receptor pathway and may be used as an indicator of prostate tumor
cell proliferation. In this study, PSA levels decreased following
treatment with deforolimus and bicalutamide.

"These results provide support for the study of deforolimus in
combination with bicalutamide in patients with advanced prostate
cancer," stated Timothy Clackson, Ph.D., senior vice president and
chief scientific officer of ARIAD. "Based partly on these data, we are
working with our partner, Merck & Co., Inc., to advance the ongoing
Phase 2 clinical trial that tests this combination in prostate cancer
patients."

In this preclinical study, deforolimus alone was shown to inhibit
proliferation of multiple prostate cancer cell lines. Deforolimus is a
potent inhibitor of mTOR, a master switch that regulates cell growth
and division. Communication between mTOR and the androgen receptor
pathway has been implicated in progression of prostate cancer from
androgen-dependence to androgen-independence. Consistent with this
hypothesis, the combination of deforolimus and bicalutamide blocked
the growth of prostate cancer cells in both cell culture and mouse
models.

"Androgen-deprivation, or hormone therapy in prostate cancer
patients, is often successful initially, but most patients see their
cancer progress, highlighting the need for alternative or combination
therapies," added Clackson. "The apparent role of the mTOR pathway in
this progression provides a strong, scientific rationale for the
combination of deforolimus and bicalutamide, validated by our new
preclinical data."

Other Data Presented

In addition to this preclinical study, ARIAD also presented data
from its Phase 1 clinical trial evaluating the pharmacodynamic profile
of oral deforolimus when administered in multiple dosing schedules.
These data supported the dosing regimen being evaluated in the Phase 3
SUCCEED clinical trial of deforolimus in patients with metastatic
soft-tissue and bone sarcomas. Additionally, data on the molecular
profiling of blood cells from a Phase 1b study of deforolimus in
patients with advanced solid tumors were presented at the meeting.

About Deforolimus

ARIAD's lead product candidate, deforolimus, is a novel rapamycin
analog that specifically and potently inhibits mTOR, a downstream
activator of the PI3K/Akt and nutrient sensing pathways. The mTOR
protein acts as a "master switch" in cancer cells. Blocking mTOR
creates a starvation-like effect in cancer cells by interfering with
cell growth, division, metabolism, and angiogenesis. Multiple Phase 1
and 2 clinical trials of deforolimus in solid tumors and hematologic
cancers have completed patient enrollment. The global Phase 3 SUCCEED
trial of oral deforolimus in metastatic soft-tissue and bone sarcomas
is based on a Special Protocol Assessment agreed upon by the U.S. Food
and Drug Administration. ARIAD has a global partnership with Merck &
Co., Inc. to develop and commercialize deforolimus, an investigational
mTOR inhibitor, in patients with cancer.

About ARIAD

ARIAD is engaged in the discovery and development of breakthrough
medicines to treat cancer by regulating cell signaling with small
molecules. ARIAD is developing a comprehensive approach to patients
with cancer that addresses the greatest medical need - aggressive and
advanced-stage cancers for which current treatments are inadequate.
ARIAD has a global partnership with Merck & Co., Inc. to develop and
commercialize deforolimus, ARIAD's lead cancer product candidate,
which is in Phase 3 clinical development. ARIAD's second oncology
product candidate, oral AP24534, is a novel multi-targeted kinase
inhibitor in Phase 1 clinical development in hematological cancers.
ARIAD has an exclusive license to pioneering technology and patents
related to certain NF-(kappa)B treatment methods, and the discovery
and development of drugs to regulate NF-(kappa)B cell-signaling
activity, which may be useful in treating certain diseases. Additional
information about ARIAD can be found on the web at
http://www.ariad.com.

This press release contains "forward-looking statements."
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, the costs
associated with our research, development, manufacturing and other
activities, the conduct and results of pre-clinical and clinical
studies of our product candidates, difficulties or delays in obtaining
regulatory approvals to market products resulting from our development
efforts, our reliance on our strategic partners and licensees and
other key parties for the successful development, manufacturing and
commercialization of products, the adequacy of our capital resources
and the availability of additional funding, patent protection and
third-party intellectual property claims relating to our and any
partner's product candidates, the timing, scope, cost and outcome of
legal and patent office proceedings concerning our NF-(kappa)B patent
portfolio, the merger of the Company with its former subsidiary, ARIAD
Gene Therapeutics, Inc., future capital needs, risks related to key
employees, markets, economic conditions, prices, reimbursement rates
and competition, 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.

ARIAD Pharmaceuticals, Inc.
Maria E. Cantor, 617-621-2208

Copyright Business Wire 2008