Merck licenses PI3K-delta inhibitor from Exelixis

Exelixis, Inc., a biotechnology company focused on developing therapies for cancer, has announced a license agreement with Merck, known as MSD outside of the United States and Canada.

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SOUTH SAN FRANCISCO, Calif.—Exelixis, Inc., a biotechnologycompany focused on developing therapies for cancer, has announced a licenseagreement with Merck, known as MSD outside of the United States and Canada. Theagreement grants Merck an exclusive worldwide license to Exelixis' PI3K-deltaresearch and development program, which includes XL499, the company's mostadvanced PI3K-delta inhibitor, and other related compounds. XL499 is currentlyin the preclinical stage, having been advanced to development candidate statusin January 2010. As a result, Merck will be solely responsible for researching,developing and commercializing compounds originating from the program.
"Exelixis has established a strong reputation for innovationin the development of targeted kinase inhibitors," Don Nicholson, Ph.D., VicePresident and Head of Worldwide Discovery, Respiratory and Immunology Franchiseat Merck Research Laboratories, said in a press release. "Collaborations likethis are an important part of our strategy as we seek new ways to address unmetneeds in inflammatory disease and oncology."
Under the terms of the agreement, Merck will pay Exelixis$12 million upfront, with the potential for development and regulatorymilestone payments for multiple indications of up to $239 million. Exelixiswill be eligible for potential combined sales performance milestones androyalties on net-sales of products that result from the agreement, andmilestones and royalties are payable on compounds that result from Exelixis'PI3K-delta program or from certain compounds that emerge from Merck's internaldiscovery efforts targeting PI3K-delta within a certain period.
PI3K-delta, a member of the Class 1 family ofphosphoinositide-3 kinases, is predominately expressed in the cells of theimmune system. PI3K-delta is activated in response to a variety of stimuli fromthe immune cells, and inappropriate PI3K-delta activation is considered tocontribute to several different inflammatory and allergic disorders, includingallergic asthma and rheumatoid arthritis. Exelixis notes on its site that"targeting PI3K-delta signaling has been sown to significantly reduceinflammation and disease progression in preclinical models of rheumatoid arthritisand allergic asthma." Selective targeting of PI3K-delta has also been shown to"lead to clinically relevant responses in some lymphoma patients."
"PI3K-delta is an interesting target with potential utilityin a number of therapeutic areas, including inflammation and oncology," MichaelM. Morrissey, Ph.D., president and chief executive officer of Exelixis, said ina press release. "Our PI3K-delta program builds on our prior interest in thePI3K family, which led to the advancement of pan-PI3K inhibitors into clinicaldevelopment for cancer. Merck's global presence and significant resources makeit the ideal organization to carry the PI3K-delta program forward. At the sametime, this agreement provides Exelixis with resources for the continueddevelopment and potential commercialization of our lead compound, cabozantinib,which is in late-stage development for medullary thyroid and prostate cancers."
Cabozantinib is a potent dual inhibitor of the MET and VEGFpathways, and is designed to block MET-driven tumor escape. Exelixis notes onits site that the compound has been shown to "kill tumor cells, reducemetastases and inhibit angiogenesis." Cabozantinib is currently being tested inseveral clinical trials for a variety of indications, including ovarian cancer,small cell lung cancer, breast cancer, pancreatic cancer, non-small cell lungcancer, castration-resistant prostate cancer and renal cell carcinoma.
SOURCE: Exelixis press release

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