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ArQule Announces Publication of Manuscript Highlighting Activity of AKT Inhibitor ARQ 092 and Next Generation AKT Inhibitor ARQ 751 in Oncology

Pre-Clinical Data Supports the Use of AKT1 and PI3K Mutations as Biomarkers for the Company’s AKT Inhibitors

BURLINGTON, Mass., Oct. 15, 2015 (GLOBE NEWSWIRE) -- ArQule, Inc. (NASDAQ:ARQL) today announced the publication of a paper detailing the pre-clinical profile of ARQ 092 and ARQ 751, orally available selective pan-AKT inhibitors. The findings, published on-line by PLOS ONE, http://dx.plos.org/10.1371/journal.pone.0140479, demonstrate that ARQ 092 and ARQ 751 potently and selectively inhibit both the active and inactive forms of AKT.

Both ARQ 092 and ARQ 751 demonstrated signal abrogation and efficacy in pre-clinical in vitro and in vivo models harboring AKT1 and PI3K mutations. These data support the clinical advancement of ARQ 092 in a biomarker enriched population, and the filing of an investigational new drug (IND) application for ARQ 751 as a next generation AKT inhibitor.

“These data strongly support the current phase 1b biomarker-driven trial we are conducting with ARQ 092 in oncology,” said Brian Schwartz, M.D., Head of Research and Development and Chief Medical Officer at ArQule. “Preliminary evidence of clinical efficacy was recently presented at ESMO, where we highlighted four partial responses out of 25 patients from our on-going phase 1b trial, in follicular lymphoma (AKT1 E17K mutation), breast cancer (AKT1 E17K mutation) and endometrial cancer (PIK3CA H1047R mutation), validating the pre-clinical hypothesis generated in this publication.”

ArQule continues to enroll patients in the phase 1b study for ARQ 092 in oncology and expects to file an IND application for ARQ 751 by the end of 2015.

About ARQ 092 and the AKT Pathway

ARQ 092 is an orally available, selective small molecule inhibitor of the AKT kinase. 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, lymphoma and tumors harboring either AKT or PI3K mutations. A number of next-generation compounds in the Company’s AKT program are in early to late stages of pre-clinical development.

About ArQule

ArQule is a biotechnology company engaged in the research and development of next-generation, small-molecule cancer therapeutics. The Company’s targeted, broad-spectrum products and research programs are focused on key biological processes that are central to human cancers. ArQule’s lead product, in Phase 2 and Phase 3 clinical development, is tivantinib (ARQ 197), an oral, selective inhibitor of the c-MET receptor tyrosine kinase. The Company’s pipeline includes: ARQ 092, designed to inhibit the AKT serine/threonine kinase, and ARQ 087, a multi-kinase inhibitor designed to preferentially inhibit the fibroblast growth factor receptor (FGFR) family. ArQule’s current discovery efforts are focused on the identification of novel kinase inhibitors, leveraging the Company’s proprietary library of compounds.

This press release contains forward-looking statements regarding 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 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, it 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 these compounds 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.

Contacts: Dawn Schottlandt Sr. Director, Investor Relations/ Corp. Communications (781) 994-0300 www.ArQule.com

Source:ArQule, Inc.