ArQule Announces Issuance of U.S. Patent Covering Composition of Matter of Proprietary Reversible BTK Inhibitor, ARQ 531
April 26 2017 - 7:00AM
Business Wire
ArQule, Inc. (Nasdaq: ARQL) today announced that the U.S. Patent
and Trademark Office has issued U.S. Patent Number 9,630,968. The
patent claims composition of matter of ARQ 531. ArQule will be
entitled to patent protection through December 2035 in the U.S. for
the allowed claims. ARQ 531 is an investigational, orally
bioavailable, potent and reversible inhibitor of both wild type and
C481S-mutant Bruton’s tyrosine kinase (BTK). The company plans to
begin a phase 1 clinical trial by the third quarter of 2017 with
ARQ 531 in patients with B-cell malignancies who are refractory to
other therapeutic options.
“This patent secures long lasting and foundational intellectual
protection for ARQ 531,” said Peter Lawrence, President, Chief
Operating Officer, and General Counsel at ArQule. “We continue to
work to extend and strengthen all intellectual property related to
chemical equity that has been generated through our multiple years
of investment in the BTK discovery program.”
B-cell malignancies, like chronic lymphocytic leukemia,
Waldenstrom’s macroglobulinemia, diffuse large B-cell lymphoma 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 four 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 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, 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.
This press release contains forward-looking statements regarding
the Company’s patent protection for its BTK inhibitor, ARQ 531,
including its current composition of matter patent and anticipated
future patent filings, and also planned clinical trials regarding
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 different
materially. For example, although the U.S. Patent and Trademark
Office has granted composition of matter protection to ARQ 531 in
the United States, similar foreign patent authorities have yet to
act on the composition of matter patent filings for ARQ 531 and may
not grant such protection. In addition, the U.S. Patent and
Trademark Office and similar foreign patent authorities may not
grant additional patents for ARQ 531. Moreover, third parties may
successfully challenge the validity of our patents. Regarding the
Company’s planned clinical trials with ARQ 531, problems may arise
that could lead to the delays or discontinuation of clinical
development, including safety and regulatory issues. For more
detailed information on the risks and uncertainties associated with
the Company’s patent, 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/20170426005141/en/
ArQule, Inc.Dawn Schottlandt, 781-994-0300Sr. Director, Investor
Relations/Corp. Communicationswww.arqule.com
ArQule (NASDAQ:ARQL)
Historical Stock Chart
From Mar 2024 to Apr 2024
ArQule (NASDAQ:ARQL)
Historical Stock Chart
From Apr 2023 to Apr 2024