GSK’s kinase connection

GSK signs potential $1.5B inflammatory disease deal with Cellzome

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LONDON—Furthering its stated commitment to discover novel therapeutics for inflammatory diseases through external collaborations, GlaxoSmithKline last month signed a research deal worth up to $1.5 billion with Anglo-German drug discovery company Cellzome Inc. for the development of kinase inhibitors in the treatment of inflammatory diseases.

The deal gives Cellzome an up-front payment of $25.31 million in cash and equity and milestone payments up to $207.47 million per program for the discovery and development of inhibitors against seven different targets. GSK will have an exclusive option to license all product candidates and will pay Cellzome double-digit royalties on net sales of products resulting from the alliance.

GSK declined to comment on the deal, but in a statement announcing the alliance, Dr. Jose Carlos Gutierrez-Ramos, senior vice president and head of the Immuno-Inflammation Centre of Excellence for Drug Discovery at GSK, said it is in line with GSK's commitment "to becoming a world leader in immuno-inflammation drug discovery by finding transformative medicines through internal efforts and external collaborations."

For Cellzome, partnering with GSK is "a major event in Cellzome's development," says CEO Tim Edwards.

"The collaboration is, we believe, one of the larger small molecule preclinical transactions published in the past two years in Europe, validating our Kinobeads product engine and our expertise in identifying a new generation of kinase-targeted drugs to treat inflammatory diseases," Edwards says.

Kinases are key molecular switches in cellular signaling events with a central role in many inflammatory responses, and selective inhibitors offer a different approach to therapeutic intervention in diseases such as rheumatoid arthritis or multiple sclerosis. Kinobeads screens compounds in a physiological setting and is designed to improve the predictability of these drug candidates' performance in clinical testing.

"The kinase is studied in an environment that is as close as possible to its true biological context, and is thus more predictive of clinical outcome," Edwards says. "Cellzome is applying Kinobeads to all aspects of the drug discovery process, from library screening to the analysis of drug effects in patients. Kinases represent a large target class whose members are all closely related, with similar structural homology around the ATP-binding site, so it has proved difficult to identify selective, potent inhibitors. Drugs which cross-react with multiple kinases are more likely to have unwanted side effects."

The collaboration will focus on diseases with a high unmet medical need where an orally available, small molecule therapeutic would bring significant benefits, such as rheumatoid arthritis, Crohn's disease or systemic lupus erythematosus, Edwards says.

"Both companies have a strong interest in inflammatory diseases, where GSK aspires to become a world leader in the discovery of novel anti-inflammatory drugs," he says. "Since kinases are attractive targets in numerous inflammatory diseases, and many patients do not respond to current therapies, both Cellzome and GSK believe that this is an important area of drug discovery." DDN


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