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

On October 15, 2015 ArQule, Inc. (NASDAQ:ARQL) reported the publication of a paper detailing the pre-clinical profile of ARQ 092 and ARQ 751, orally available selective pan-AKT inhibitors (Press release, ArQule, OCT 15, 2015, View Source [SID:1234507724]). The findings, published on-line by PLOS ONE, View Source, 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 (Free ESMO Whitepaper), 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.