ArQule Presents Preclinical Data for BTK Inhibitor, ARQ 531, at the 22nd Annual Congress of the European Hematology Associati...
June 23 2017 - 7:00AM
Business Wire
In preclinical models ARQ 531 demonstrates
potent anti-tumor activity in DLBCL
ArQule, Inc. (Nasdaq: ARQL) today announced that preclinical
data for ARQ 531 in diffuse large B-cell lymphoma (DLBCL) in vitro
and in vivo tumor models was presented at EHA Congress in Madrid,
Spain. ARQ 531 is an investigational, orally bioavailable, potent
and reversible inhibitor of both wild type and C481S-mutant
Bruton’s tyrosine kinase (BTK).
The presentation titled “ARQ 531, A Reversible BTK Inhibitor,
Demonstrates Potent Anti-Tumor Activity in ABC-DLBCL and GCB-DLBCL”
can be viewed at
https://www.arqule.com/wp-content/uploads/ARQ531_EHA_2017.pdf.
ARQ 531 Poster Presentation Highlights
- Preclinical data suggests ARQ 531 has
the potential for broad clinical utility in a wide range of
hematological malignancies and lymphomas.
- The signaling pathways evaluated show a
distinct kinase inhibition profile that could be advantageous in
treating lymphomas.
- ARQ 531, unlike other BTK inhibitors,
has activity in both ABC-DLBCL and GCB-DLBCL preclinical
models.
- A phase 1 trial with ARQ 531 in
patients with B-cell malignancies refractory to other therapeutic
options, including ibrutinib, is planned to commence by the third
quarter of 2017.
"This data further strengthens a very comprehensive preclinical
package for ARQ 531," said Dr. Brian Schwartz, M.D., Head of
Research and Development and Chief Medical Officer at ArQule.
"While targeting ibrutinib resistant patients will be an initial,
fast-to-market strategy for the clinical development of ARQ 531,
the data presented at EHA clearly demonstrate the potential
clinical utility of the drug beyond ibrutinib refractory
cancers."
B-cell malignancies, like chronic lymphocytic leukemia,
Waldenstrom’s macroglobulinemia, DLBCL and mantle cell lymphoma are
driven by BTK. The only approved BTK inhibitor, ibrutinib, is
irreversible and makes a covalent bond with the C481 residue of the
targeted protein. Although ibrutinib has demonstrated excellent
responses in patients with elevated B-cell receptor signaling,
clinical resistance has been observed, and the BTK C481S mutation
is emerging as a predominant mechanism of resistance. As a
reversible inhibitor, ARQ 531 does not require interaction with the
C481 residue, a binding site essential for irreversible ibrutinib
binding to BTK, thus positioning ARQ 531 as a targeted therapy for
patients harboring C481S-mutant BTK who have developed resistance
to irreversible BTK inhibitors.
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 531 inhibits 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. In preclinical studies ARQ 531 has demonstrated high
oral bioavailability as well as good ADME, pharmacokinetic and
metabolic properties. The company plans to initiate a phase 1 trial
by the third quarter of 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. ArQule’s 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 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 a phase
1/2 company sponsored study for Overgrowth Diseases, in a phase 1
study for ultra-rare Proteus syndrome conducted by the National
Institutes of Health (NIH), as well as in multiple oncology
indications; 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, through
toxicology testing and plan to initiate a phase 1 trial by the
third quarter of 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.
Forward Looking Statements
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, it may not
exhibit an adequate safety profile in planned 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 ARQ 531 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. 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/20170623005026/en/
ArQule, Inc.Dawn Schottlandt, 781-994-0300Vice President,
Investor Relations/Corp. Communicationswww.ArQule.com
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