On November 8, 2018 ArQule, Inc. (Nasdaq: ARQL) reported that it will be presenting clinical and preclinical data on the company’s next generation AKT inhibitor, ARQ 751, in three poster presentations at the 30th EORTC/AACR/NCI Symposium to be held from November 13 to 16, 2018 in Dublin, Ireland (Press release, ArQule, NOV 8, 2018, View Source [SID1234530928]).
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Presentation Details
Title: A Phase 1 Dose Escalation Study of ARQ 751 in Adult Patients with Advanced Solid Tumors with AKT1, 2, 3 Genetic Alterations, Activating PI3K Mutations, PTEN-null, or Other Known Actionable PTEN Mutations
Abstract #:
395
Session:
Molecular Targeted Agents – PART II
Date:
Friday, November 16, 2018
Time:
10:00-14:00 PM CET
Location:
Exhibition Hall
Title:
Combination of the AKT inhibitor ARQ 751 with Immune Checkpoint Inhibitor and Other Therapeutic Agents
Abstract #:
371
Session:
Molecular Targeted Agents – PART II
Date:
Friday, November 16, 2018
Time:
10:00-14:00 PM CET
Location:
Exhibition Hall
Title:
Miransertib and ARQ 751 exhibit superior cell-death-inducing properties compared to other AKT inhibitors and can overcome resistance to other allosteric AKT inhibitors
Abstract #:
442
Session:
Molecular Targeted Agents – PART II
Date:
Friday, November 16, 2018
Time:
10:00-14:00 PM CET
Location:
Exhibition Hall
About ARQ 751
ARQ 751 is an orally bioavailable, selective small molecule inhibitor of the AKT serine/threonine 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 751 is currently in a Phase 1 study in adult patients with refractory and/or metastatic tumors that harbor genetic alterations along the AKT pathway.
About Miransertib
Miransertib (ARQ 092) is an orally available, selective, pan-AKT (protein kinase B) inhibitor that potently inhibits AKT1, 2 and 3 isoforms. Dysregulation of AKT has been implicated in a variety of rare overgrowth diseases and cancers; however, there are currently no approved inhibitors of AKT. AKT inhibitors, either as single agent or combination therapy, show significant promise in molecularly defined patient populations. Miransertib is currently in a Phase 1/2 company-sponsored study for PIK3CA-Related Overgrowth Spectrum (PROS), a Phase 1 study for ultra-rare Proteus syndrome conducted by the National Institutes of Health (NIH/NHGRI), and a Phase 1b study in combination with the hormonal therapy, anastrozole, in patients with advanced endometrial cancer with AKT and PI3K mutations. Miransertib has been granted Rare Pediatric Disease Designation and Fast Track Designation by the U.S. Food and Drug Administration (FDA), as well as Orphan Designation by the FDA and European Medicines Agency in the rare overgrowth disease, Proteus syndrome.