On November 3, 2016 ArQule, Inc. (Nasdaq: ARQL) reported that preclinical data will be presented on two molecules from its proprietary pipeline at the 2016 American Society of Hematology (ASH) (Free ASH Whitepaper) Annual Meeting in San Diego, California, December 3 – 6, 2016 (Press release, ArQule, NOV 3, 2016, View Source [SID1234516206]).
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A poster presentation summarizing preclinical studies of ARQ 531 in Chronic Lymphocytic Leukemia (CLL) will be presented by The Ohio State University investigators. ARQ 531 is an investigational, orally bioavailable, potent and reversible Bruton’s tyrosine kinase (BTK) inhibitor.
An oral presentation of preclinical studies with ARQ 092 in Sickle Cell Disease will be presented by ArQule’s collaborator, the University of Illinois College of Medicine. ARQ 092 is an orally available, selective pan-AKT inhibitor.
The data reinforce the strength and depth of ArQule’s proprietary pipeline while warranting further exploration of both molecules in their respective indications. The company remains on track to submit an Investigational New Drug (IND) application for ARQ 531 in early 2017. ARQ 092 is currently being tested in a phase 1b trial for AKT driven oncology malignancies and in a phase 1 trial in the ultra-rare Proteus syndrome indication in collaboration with the National Institutes of Health (NIH).
Details, including times and locations, of the ASH (Free ASH Whitepaper) Annual Meeting presentations can be found below. Abstracts are available online at View Source
ARQ 092 in Sickle Cell Disease
Title: Specific inhibition of AKT with ARQ 092, an orally-available selective allosteric AKT inhibitor, attenuates acute vaso-occlusive events in sickle cell disease
Presenter: Dr. Jaehyung Cho, University of Illinois College of Medicine
Session Date: Saturday, December 3, 2016
Oral Session Name: Hemoglobinopathies, Excluding Thalassemia – Basic and
Translational Science: Mechanisms of Vaso-Occlusion
Session Time: 2:00 PM – 3:30 p.m. PT
Oral Presentation Time: 2:45 p.m. PT
Location: San Diego Convention Center, Room 7AB
ARQ 531 in Chronic Lymphocytic Leukemia
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
Presenter: Sean Reiff, The Ohio State University
Session: Date: Sunday, December 4, 2016
Poster Session Name: CLL: Therapy, excluding Transplantation: Poster II
Poster Viewing Time: 9:00 a.m. – 8:00 p.m. PT
Poster Presentation Time: 6:00 p.m. – 8:00 p.m. PT
Location: San Diego Convention Center, Hall GH
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 fully enrolled a phase 1b trial including 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. In mid-2016 the company initiated a phase 1 clinical trial with ARQ 751, a next generation AKT inhibitor, in cancers with AKT mutations.
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 hematological cancers.