Tokyo and Woburn, Massachusetts (ots/PRNewswire) -
Daiichi Sankyo Company, Limited (TSE 4568) and ArQule, Inc. today
announced that the first patient has been enrolled in the phase III
trial of ARQ 197, an investigational selective inhibitor of the c-Met
receptor tyrosine kinase, in combination with erlotinib, for patients
diagnosed with non-squamous, non-small cell lung cancer (NSCLC), who
have received one or two prior systemic anti-cancer therapies.
The phase III trial is a randomised, double-blinded, controlled
study of previously treated patients with locally advanced or
metastatic, non-squamous NSCLC who will receive ARQ 197 plus
erlotinib or placebo plus erlotinib.
The primary objective is to evaluate the overall survival (OS) in
the intent-to-treat (ITT) population. Secondary endpoints include OS
in the subpopulation of patients with epidermal growth factor
receptor (EGFR) wild type, progression-free survival (PFS) in the ITT
population, and further assessment of the safety of ARQ 197 in
combination with erlotinib.
According to the International Agency for Research on Cancer,
more than 1.6 million new cases of lung cancer were diagnosed in 2008
globally, and NSCLC accounted for 80 percent of those cases.
According to the American Cancer Society more than 220,000 cases of
lung cancer will have been diagnosed in 2010 in the U.S. Of
patients diagnosed with lung cancer in Europe, almost 90 percent die
of the disease.
"With lung cancer accounting for more deaths than colon, breast
and prostate cancers combined, we are very pleased to begin this
phase III trial to advance the knowledge about the role ARQ 197 might
have in the treatment of patients with non-small cell lung cancer in
combination with erlotinib," said Dr. Kazunori Hirokawa, global head
of R&D Unit, Daiichi Sankyo. "It is our hope and expectation that
this late-stage study will confirm the results we observed in
patients with non-squamous cell histology in phase II, which showed
promise toward extending overall survival and progression-free
survival in this group when ARQ 197 was combined with erlotinib."
"The start of this phase III trial marks a key milestone in the
development of ARQ 197 and our partnership with Daiichi Sankyo," said
Paolo Pucci, chief executive officer of ArQule. "Lung cancer is a
devastating disease, and our hope is that ARQ 197 will prove to be an
effective treatment option that will help patients diagnosed with
In October 2010, agreement was reached with the U.S. Food and
Drug Administration (FDA) on a Special Protocol Assessment (SPA) for
the phase III trial comparing ARQ 197 plus erlotinib against
erlotinib plus placebo. The phase III study of ARQ 197 plus erlotinib
will enroll 988 patients in 150 sites in the U.S., Canada, Eastern
and Western Europe, Australia and Latin America. Additional details
are available on http://www.clinicaltrials.gov.
About ARQ 197 and c-Met
ARQ 197 is an orally available, selective inhibitor of c-Met, a
receptor tyrosine kinase that is currently in phase II and phase III
clinical trials and is not yet approved for use. In healthy adult
cells, c-Met is present in normal levels to support natural cellular
function, but in cancer cells, c-Met is inappropriately and
continuously activated for unknown reasons. When abnormally
activated, c-Met plays multiple roles in aspects of human cancer,
including cancer cell growth, survival, angiogenesis, invasion and
Pre-clinical data have demonstrated that ARQ 197 inhibits c-Met
activation in a range of human tumor cell lines and shows anti-tumor
activity against several human tumor xenografts. In clinical trials
to date, treatment with ARQ 197 has been well-tolerated and has
resulted in tumor responses and prolonged stable disease across a
broad range of tumors.
In December 2008, ArQule and Daiichi Sankyo signed a license,
co-development and co-commercialisation agreement to co-develop ARQ
197 in the U.S., Europe, South America and the rest of the world,
excluding Japan, China (including Hong Kong), South Korea and Taiwan,
where Kyowa Hakko Kirin Co., Ltd. has exclusive rights for
development and commercialisation.
About Daiichi Sankyo
The Daiichi Sankyo Group is dedicated to the creation and supply
of innovative pharmaceutical products to address the diversified,
unmet medical needs of patients in both mature and emerging markets.
While maintaining its portfolio of marketed pharmaceuticals for
hypertension, hyperlipidemia, and bacterial infections, the Group is
engaged in the development of treatments for thrombotic disorders and
focused on the discovery of novel oncology and
cardiovascular-metabolic therapies. Furthermore, the Daiichi Sankyo
Group has created a "Hybrid Business Model," which will respond to
market and customer diversity and optimise growth opportunities
across the value chain. For more information, please visit
The company's world headquarters are in Tokyo. Its European base
is located in Munich. DAIICHI SANKYO EUROPE has affiliates in 12
European countries in addition to a global manufacturing site located
in Pfaffenhofen, Germany.
ArQule is a biotechnology company engaged in the research and
development of next-generation, small-molecule cancer therapeutics.
The Company's targeted, broad-spectrum products and research programs
are focused on key biological processes that are central to human
cancers. ArQule's lead product, in phase II and phase III clinical
development, is ARQ 197, an inhibitor of the c-Met receptor tyrosine
kinase. The Company has also initiated phase I clinical testing with
ARQ 621, designed to inhibit the Eg5 kinesin motor protein, and with
ARQ 736, designed to inhibit the RAF kinases. ArQule's current
discovery efforts, which are based on the ArQule Kinase Inhibitor
Platform (AKIP(TM)), are focused on the identification of novel
kinase inhibitors that are potent, selective and do not compete with
ATP (adenosine triphosphate) for binding to the kinase.
This press release contains forward-looking statements regarding
the progress of the Companies' phase II and phase III clinical trials
with ARQ 197. These statements are based on the Companies' current
beliefs and expectations, and are subject to risks and uncertainties
that could cause actual results to differ materially. Positive
information about early stage clinical trial results is not
necessarily indicative of clinical efficacy and does not ensure that
later stage or larger scale clinical trials will be successful. The
results achieved in later stage trials may not be sufficient to meet
applicable regulatory standards. Problems or delays may arise during
clinical trials or in the course of developing, testing or
manufacturing these compounds that could lead the Companies or their
collaborators to discontinue development. Even if later stage
clinical trials are successful, the risk exists that unexpected
concerns may arise from analysis of data or from additional data or
that obstacles may arise or issues be identified in connection with
review of clinical data with regulatory authorities or that
regulatory authorities may disagree with the Companies' views of the
data or require additional data, information or studies. For example,
ARQ 197 may not demonstrate promising therapeutic effect; in
addition, this compound may not demonstrate an appropriate safety
profile in further pre-clinical testing and in current, later stage
or larger scale clinical trials as a result of known or as yet
unanticipated side effects. In addition, the planned timing of
initiation and completion of clinical trials for ARQ 197 is subject
to the ability of the Companies to enroll patients, enter into
agreements with clinical trial sites and investigators, and other
technical hurdles and issues that may not be resolved. Drug
development involves a high degree of risk. Only a small number of
research and development programs result in the commercialisation of
a product. Furthermore, ArQule may not have the financial or human
resources to pursue drug discovery successfully in the future. For
more detailed information on the risks and uncertainties associated
with the Company's drug development and other activities see the
Company's periodic reports filed with the Securities and Exchange
Commission. The Company does not undertake any obligation to publicly
update any forward-looking statements.
 International Agency for Cancer Research, URL:
http://globocan.iarc.fr/factsheets/cancers/lung.asp. Last accessed
November 10, 2010.
 American Cancer Society. Lung Cancer. URL: http://www.cancer.
ll-cell-overview-non-small-cell-lung-cancer Last accessed November
 American Cancer Society. Lung Cancer. URL: http://www.cancer
all-cell-overview-key-statistics Last accessed November 9, 2010.
(GLOBOCAN 2008) International Agency for Research on Cancer:
 American Cancer Society. Lung Cancer. URL: http://www.cancer.
-cancer-key-statistics Last accessed November 9, 2010.
(Due to the length of these URLs, it may be necessary to copy and
paste the hyperlinks into your Internet browser's URL address field.
Remove the space if one exists.)
For more information, please contact:
William B. Boni
Daiichi Sankyo, Co., Ltd. (Japan)
Daiichi Sankyo, Inc. (US)
Daiichi Sankyo Europe
ots Originaltext: Daiichi Sankyo
Im Internet recherchierbar: http://www.presseportal.ch
CONTACT: William B. Boni, ArQule, Inc., +1(781)994-0300; Toshiaki
Sai,Daiichi Sankyo, Co., Ltd. (Japan), +81-3-6225-1126; Kimberly Wix,
DaiichiSankyo, Inc. (US), +1(973)944-2338, Tetsuya Ohira, Daiichi