Drug Detail

Information about ARQ 092

Generic Name
IND	ARQ 092
Brand Name (US)
Manufacturer	ArQule
Drug Type	Tyrosine Kinase Inhibitor
Delivery
Approval Status	Phase 1
Indications
Overall Strategy	Oncogenic Signal Path Based
Strategy	Block AKT
Drug Category	AKT inhibitor

ARQ 092 is an investigational orally available, selective, pan-AKT inhibitor that potently inhibits AKT1, 2 and 3 isoforms. The drug is currently in phase 1b for oncology and about to enter phase 1 for Proteus syndrome, a rare over-growth disease. Both trials are biomarker-driven and are focused on enrolling patients with the AKT1 mutation.

ARQ 092 has demonstrated inhibition of tumor growth and downstream AKT signaling, in vivo, in tumors whose growth is driven by these targets. Single agent activity with ARQ 092 was observed in phase 1a and phase 1b studies as well as reductions in expression levels of relevant biomarkers. Publications support AKT1 as a viable target in oncology and Proteus syndrome.
Mechanism of Action

ARQ 092 suppresses the AKT pathway via two modes of action. First, by binding to the inactive form of AKT, ARQ 092 prevents membrane localization and full AKT activation. Second, ARQ 092 also directly inhibits the membrane associated active form of AKT.
Precision Medicine

The AKT1 mutation is believed to play a role in certain cancers and over-growth diseases, such as Proteus syndrome.

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. Pre-clinical research has demonstrated that ARQ 092 potently and selectively inhibits both the active and inactive forms of AKT.