Data on Proprietary BTK Inhibitor, ARQ 531, Demonstrating Inhibition of Wild Type & C481S Mutant BTK & Superiority to Ibrutin...
December 04 2016 - 9:00PM
Business Wire
ARQ 531 demonstrates best-in-class potential as
a reversible, non-covalent BTK inhibitor
ArQule, Inc. (Nasdaq: ARQL) today announced that preclinical
data was presented on Bruton's tyrosine kinase (BTK) inhibitor, ARQ
531, in a poster presentation by The Ohio State University at the
American Society of Hematology (ASH) Annual Meeting. The
presentation highlighted preclinical studies of ARQ 531 in Chronic
Lymphocytic Leukemia (CLL). ARQ 531 is an investigational, orally
bioavailable, potent and reversible BTK inhibitor.
ARQ 531 Poster Presentation Highlights
Title: The Bruton's Tyrosine Kinase (BTK) Inhibitor ARQ 531
Effectively Inhibits Wild Type and C481S Mutant BTK and Is Superior
to Ibrutinib in a Mouse Model of Chronic Lymphocytic Leukemia
- Multi-targeted inhibition of cytokine,
chemokine, and BCR pathways by ARQ 531 decreases activation,
migration, and viability of CLL cells.
- Unlike ibrutinib, ARQ 531 inhibits
activation of C481S mutated BTK variants and maintains cytotoxicity
in ibrutinib resistant clones.
- ARQ 531 demonstrates remarkable
efficacy in an in vivo TCL1 adoptive transfer model, improving
survival to a greater extent than ibrutinib and restoring
granulocyte production.
- The company plans to complete
preclinical studies and file an Investigational New Drug (IND)
application in early 2017 to begin clinical testing later in the
year.
The presentation can be viewed at
https://www.arqule.com/wp-content/uploads/ASH-2016-ARQ-531-in-CLL.pdf.
"Irreversible kinase inhibitors directed at BTK have really
changed the landscape of CLL but at extended follow up, we are
beginning to see a subset of high risk patients who are relapsing,”
said Dr. Jennifer Woyach, M.D., of The Ohio State University
College of Medicine. “Small molecules that target BTK that are
not dependent upon the C481 site represent an exciting option for
future clinical trials. We are excited to be working with ArQule
on this project and look forward to initiating the first in
man study with ARQ 531."
“We began our BTK discovery program in 2011 which ultimately
lead to the selection of ARQ 531, a potent reversible inhibitor of
both wild type and mutant BTK,” said Dr. Giovanni Abbadessa, M.D.,
PhD., Vice President of Clinical Development, Translational
Medicine and Medical Affairs at ArQule. “With the recent emergence
in 2015 of BTK resistance we concentrated our efforts in this
growing CLL patient population. We are pleased to be working with
The Ohio State University to finish preclinical studies on this
exciting program. We remain on track to file an IND application
early next year.”
About BTK and ARQ 531
ARQ 531 is an investigational, orally bioavailable, potent and
reversible Bruton’s tyrosine kinase (BTK) inhibitor. Biochemical
and cellular studies have shown that ARQ 531inhibits both the wild
type and C481S-mutant forms of BTK. The C481S mutation is a known
emerging resistance mechanism for first generation irreversible BTK
inhibitors. ARQ 531 has high oral bioavailability as well as good
ADME, pharmacokinetic and metabolic properties. The company plans
to file an IND for ARQ 531 in early 2017. BTK is a therapeutic
target that has been clinically proven to inhibit B-cell receptor
signaling in blood cancers.
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
preclinical experiments and planned clinical trials with ARQ 531.
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 results does not ensure that clinical trials
will be successful. For example, ARQ 531 may not demonstrate
promising therapeutic effect in man; in addition, and ARQ 531 may
not exhibit an adequate safety profile in ongoing toxicology
testing and may not demonstrate appropriate safety in planned,
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 these compounds that could
lead the Company 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. 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.
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version on businesswire.com: http://www.businesswire.com/news/home/20161204005028/en/
ArQule, Inc.Dawn Schottlandt, 781-994-0300Sr. Director, Investor
Relations/Corp. Communicationswww.arqule.com
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