The study supports further exploration of ARQ 092 in sickle cell
disease
Company Website:
http://www.arqule.com
BURLINGTON, Mass. -- (Business Wire)
ArQule, Inc. (Nasdaq: ARQL) today announced that preclinical data was
presented on its proprietary AKT inhibitor, ARQ 092, in an oral
presentation by the University of Illinois College of Medicine at the
American Society of Hematology (ASH) Annual Meeting. The presentation
highlighted preclinical studies of ARQ 092 in sickle cell disease (SCD).
ARQ 092 is an orally available, selective pan-AKT inhibitor.
ARQ 092 Oral Presentation Highlights
Title: Specific inhibition of AKT with ARQ 092, an
orally-available selective allosteric AKT inhibitor, attenuates acute
vaso-occlusive events in sickle cell disease
-
ARQ 092 inhibits activation, and effectively blocks heterotypic
aggregation, of neutrophils and platelets in SCD patients in vitro.
- Ex vivo studies indicate that ARQ 092 inhibits activation of
neutrophils and platelets isolated from SCD mice after oral
administration.
- In vivo studies with SCD mice demonstrate that
co-administration of hydroxyurea and ARQ 092 effectively attenuates
acute vaso-occlusive events and improves survival.
-
This study provides proof of concept in an established preclinical
model and enables a clinical pathway for ARQ 092 in the treatment of
SCD with or without hydroxyurea.
The presentation can be viewed at https://www.arqule.com/wp-content/uploads/ASH-2016-ARQ-092-in-Sickle-Cell-Disease-.pdf.
“SCD is a debilitating lifetime disease with a worldwide presence. A
report from the American Society of Hematology shows that approximately
100,000 people suffer from this disease in the U.S.” said Dr. Jaehyung
Cho, PhD., of the University of Illinois College of Medicine. “Our
research has been focused on identifying novel therapeutic targets to
prevent and treat vaso-occlusive diseases. The work done at the
University of Illinois, in collaboration with ArQule, shows the
importance of the AKT pathway in inducing vaso-occlusive events during
SCD and the beneficial effect of ARQ 092 in attenuating adhesive
function of neutrophils and platelets in SCD mice. This work warrants
further exploration of ARQ 092 in patients with SCD.”
“Our AKT program, specifically ARQ 092, continues to progress with the
phase 1 trial in Proteus syndrome sponsored by the National Institutes
of Health (NIH) and with the recently approved Investigational New Drug
(IND) application for expansion into the PROS family of rare over-growth
diseases,” said Dr. Brian Schwartz, M.D., Head of Research and
Development and Chief Medical Officer at ArQule. “The PI3K/AKT pathway
has been implicated in multiple diseases including SCD. We would like to
thank the University of Illinois College of Medicine for lending its
expertise and helping to establish valuable proof of concept for ARQ 092
in this disease setting.”
About the AKT Pathway and ARQ 092
ARQ 092 is an orally bioavailable, selective small molecule inhibitor of
the AKT kinases. The AKT pathway when abnormally activated is implicated
in multiple oncogenic processes such as cell proliferation and
apoptosis. This pathway has emerged as a target of potential therapeutic
relevance for compounds that inhibit its activity, which has been linked
to a variety of cancers as well as to select non-oncology indications.
ARQ 092, the lead compound in ArQule’s AKT program, has completed phase
1a clinical testing and has advanced into phase 1b expansion testing in
cohorts of patients with endometrial cancer, lymphomas and tumors
harboring either AKT or PI3K mutations. It is also in a phase 1 trial
being conducted by the NIH for Proteus syndrome, a rare over-growth
disease from the PROS family. Collaborators are exploring, in
preclinical testing, other indications for ARQ 092 including sickle cell
disease.
About ArQule
ArQule
is a biopharmaceutical company engaged in the research and development
of targeted therapeutics to treat cancers and rare diseases. Our mission
is to discover, develop and commercialize novel small molecule drugs in
areas of high unmet need that will dramatically extend and improve the
lives of our patients. Our clinical-stage pipeline consists of five drug
candidates, all of which are in targeted, biomarker-defined patient
populations, making ArQule
a leader among companies our size in precision medicine. ArQule’s lead
product, in phase 3 clinical development, is tivantinib (ARQ 197), an
oral, selective inhibitor of the c-MET receptor tyrosine kinase, for
second-line treatment of hepatocellular carcinoma in partnership with
Daiichi Sankyo in the West and Kyowa Hakko Kirin in Asia. ArQule’s
proprietary pipeline includes: ARQ 087, a multi-kinase inhibitor
designed to preferentially inhibit the fibroblast growth factor receptor
(FGFR) family, in phase 2 for iCCA and in phase 1b for multiple oncology
indications; ARQ 092, a selective inhibitor of the AKT serine/threonine
kinase, in phase 1 for multiple oncology indications as well as
ultra-rare Proteus syndrome, in partnership with the National Institutes
of Health (NIH); ARQ 751, a next generation AKT inhibitor, in phase 1
for patients with AKT1 and PI3K mutations; and ARQ 761, a β-lapachone
analog being evaluated as a promoter of NQO1-mediated programmed cancer
cell necrosis, in phase 1/2 in multiple oncology indications in
partnership with the University of Texas Southwestern Medical Center. In
addition, we have advanced ARQ 531, an investigational, orally
bioavailable, potent and reversible inhibitor of both wild type and
C481S-mutant BTK, into toxicology testing and plan to file an
Investigational New Drug Application in early 2017. ArQule’s current
discovery efforts are focused on the identification and development of
novel kinase inhibitors, leveraging the Company’s proprietary library of
compounds. You can follow us on Twitter
and LinkedIn.
This press release contains forward-looking statements regarding
certain pre-clinical experiments conducted by the Company’s
collaborators and the Company’s clinical trials with ARQ 092. These
statements are based on the Company’s current beliefs and expectations,
and are subject to risks and uncertainties that could cause actual
results to differ materially.Positive information about
pre-clinical, and early stage clinical trial, results, including in SCD
and Proteus syndrome, does not ensure that later stage or larger scale
clinical trials will be successful. For example, ARQ 092 may not
demonstrate promising therapeutic effect; in addition, the drug
candidate may not demonstrate appropriate safety profiles in current or
later stage or larger scale clinical trials as a result of known or as
yet unanticipated side effects. The results achieved in later stage
trials may not be sufficient to meet applicable regulatory standards or
to justify further development. Problems or delays may arise during
clinical trials or in the course of developing, testing or manufacturing
the compound that could lead the Company or its partners, including the
National Institutes of Health, to discontinue development. Even if later
stage clinical trials are successful, unexpected concerns may arise from
subsequent analysis of data or from additional data. Obstacles may arise
or issues may be identified in connection with review of clinical data
with regulatory authorities. Regulatory authorities may disagree with
the Company’s view of the data or require additional data or information
or additional studies.Drug development involves a high degree of
risk. Only a small number of research and development programs result in
the commercialization of a product. Positive pre-clinical data may not
be supported in later stages of development.Furthermore, ArQule
may not have the financial or human resources to successfully pursue
drug discovery 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.
View source version on businesswire.com: http://www.businesswire.com/news/home/20161203005009/en/
Contacts:
ArQule
Dawn Schottlandt, 781-994-0300
Sr. Director, Investor
Relations/Corp. Communications
www.arqule.com
Source: ArQule, Inc.
© 2024 Canjex Publishing Ltd. All rights reserved.