ARRY-614 is a potent, orally active, inhibitor of p38 and Tie2, which have been shown to block new blood vessel growth, inhibit inflammation and antagonize tumor growth. ARRY-614 has a low side effect profile with prolonged dosing in preclinical models of human cancer and arthritis. By targeting p38 and Tie2, we believe ARRY-614 will have broad therapeutic benefits in a number of cancers and chronic inflammatory diseases.
About p38/Tie2 Inhibition
Increased production of certain cytokines can cause abnormal tissue proliferation that is found in a number of inflammation diseases. ARRY-614 inhibits the activity of p38, a mitogen-activated protein kinase family member, regulating the production of numerous pro-inflammatory and pro-proliferative cytokines, including TNF, IL-6 and IL-1. Tie2, a receptor tyrosine kinase, plays an important role in angiogenesis and blood vessel growth which may lead to uncontrolled cell growth that characterizes a number of cancer and chronic inflammatory diseases. We believe the dual inhibition of p38 and Tie2 may produce additive and / or synergistic effects in multiple myeloma tumor models and cancer therapies.
Phase 1 Clinical Trial
We initiated a Phase 1 study with ARRY-614 in healthy volunteers in early 2008. ARRY-614 has shown good efficacy and a low side effect profile in preclinical models of human cancer and arthritis. The compound will initially be evaluated on safety, tolerability, exposure and inhibition of mechanism-related biomarkers in a single and multiple dose escalation study in normal healthy volunteers.
Future Milestones
During fiscal 2009, we plan to initiate first-in-patient trials in either cancer or inflammatory disease.
Scientific Posters
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