Product Pipeline  |   Cancer  |   Inflammation & Pain
Overview  |   Filanesib (ARRY-520) KSP  |   ARRY-614 / p38/Tie2

Novartis – MEK for Cancer Program / ARRY-162 and ARRY-300
In April 2010, Array partnered with Novartis for the worldwide development of the small-molecule MEK inhibitors ARRY-162, currently in a Phase 1 cancer trial, its back-up, ARRY-300, and other MEK inhibitors. Array received $45 million comprising an upfront and milestone payment and is eligible to receive an additional $422 million if certain clinical, regulatory and commercial milestones are achieved. In addition, Array plans to co-develop ARRY-162 in one or more specific indications and fund a portion of development costs. The agreement provides Array with double-digit royalties on sales of approved drugs outside of the U.S., with a significantly higher royalty rate for U.S. sales provided that Array meets its co-funding obligations. Array also has a co-detailing right in the U.S. for approved drugs.

ARRY-162 is an anti-cancer drug in Phase 1 development. It is a small molecule inhibitor that targets a key position in the Ras/Raf/MEK/ERK signaling pathway. Recent research confirms that the MEK pathway acts as a central axis in the proliferation of different tumors including melanoma, non-small cell lung, head/neck and pancreatic cancers.  And MEK inhibition, either alone or in combination with other agents, is an important therapeutic strategy in treating cancer.  ARRY-162 is a novel, orally active, potent, selective, non-ATP-competitive inhibitor of MEK 1 / 2 that has the potential to treat a range of malignant diseases.

Novartis – MEK for Cancer Program / ARRY-162 and ARRY-300
The Phase 1 cancer trial is an open-label, multiple dose study will determine the maximum tolerated dose and evaluate safety, pharmacokinetics and pharmacodynamics of ARRY-162 following daily oral administration to advanced cancer patients with solid tumors.  ARRY-162 is currently in an expansion phase of the Phase 1 trial at the maximum tolerated dose in biliary tract cancer patients at ten clinical sites in North America. The expansion study is designed to evaluate safety, pharmacokinetics and pharmacodynamics of ARRY-162 in patients with biliary tract cancer.

About MEK
MEK is a key protein kinase in the RAS/RAF/MEK/ERK pathway, which signals for cancer cell proliferation and survival.  MEK is frequently activated in cancer, in particular in tumors that have mutations in the RAS and RAF oncogenes.  MEK also regulates the biosynthesis of the inflammatory cytokines TNF, IL-6 and IL-1, which can act as growth and survival factors in cancer.  Preclinical data show that MEK inhibitors are additive or synergistic in combination with other agents.  In particular, the PI-3K/AKT/mTOR pathway interacts with the RAS/RAF/MEK/ERK pathway in response to growth factor signaling.  Simultaneous inhibition of both these pathways has significantly greater preclinical anti-tumor activity compared to inhibition of either pathway alone.  Because these pathways are commonly activated in many tumors, we believe that dual MEK and PI3K/AKT/mTOR inhibition could have broad anti-tumor activity.

Scientific Posters

Please click here to view posters on MEK Inhibitors
presented at Scientific Conferences.

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