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GSK to Buy Cellzome for $99M as Pharma Interest in Chemical Proteomics Continues to Build

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This article originally ran on May 15 and has been updated to include additional comments from GlaxoSmithKline.

GlaxoSmithKline said today that it has entered an agreement to purchase chemical proteomics firm Cellzome for £61 million ($99 million).

The drugmaker, which already holds a roughly 20 percent equity interest in Cellzome, said it expects to complete the deal on May 21. Simultaneous with the acquisition, Cellzome shareholders including GSK plan to launch a spin-off company that will hold rights to various Cellzome assets and activities that GSK doesn't wish to pursue.

Melinda Stubbee, director of media, global R&D and pipeline news at GSK, told ProteoMonitor that the company has begun discussing what Cellzome assets might be included in the spin-off, but that "at the moment nothing has been decided."

She declined to discuss the particulars of GSK's integration plans for Cellzome, noting that this process would begin when the deal becomes official next week. Cellzome has roughly 110 employees divided between facilities in Heidelberg, Germany and Cambridge, UK.

Cellzome specializes in mass spec-based proteomic screens for measuring drug-protein interactions. The company uses bead-based matrices of inhibitor probes to perform competition binding assays to address questions including drug activity and off-target effects. Its two main products are its Kinobeads platform for kinase research and its Episphere platform for epigenetics work.

Cellzome's technology "really applies across a wide spectrum of the drug discovery chevron," said Bob Hertzberg, vice president of screening and platform profiling at GSK. He cited among its potential uses compound selectivity profiling, mechanistic studies, and identifying potential off-target effects.

While chemical proteomics isn't a new technology, recent advances – particularly in the mass spec portions of workflows – have in recent years contributed to increasing adoption of the approach, Hertzberg told ProteoMonitor. And, indeed, last year, Cellzome added two new cutting-edge mass specs – an Orbitrap Elite and a Q Exactive, both from Thermo Fisher Scientific.

"The ability to do [chemical proteomics] effectively has grown significantly over the past two to three years with the advent of mass spec technology," he said. "The sensitivity of detection, the throughput, and the cost have all improved. The data analysis has improved. Capturing data from experiments on a broad scale is possible now."

Hertzberg added that the move within pharma toward using cell extracts and whole cells as model systems for research has also led to increased interest in technologies like Cellzome's.

There is "the realization that studying [drug] activity in cell-free biochemical systems can only take you so far," he said. "While that's a very valuable way to study compounds, people are realizing that phenotypic assays in whole cells are very important toward developing effective drugs, and this technology enables you to study compounds in a cellular context more effectively."

While Cellzome's Kinobeads and Episphere platforms both use cell extract, Hertzberg said that the company's mass spec capabilities "can be used in the context of whole cells" as well.

"That's the strategic direction that we want to head," he said. "To study compounds in a setting that more closely represents that found in a whole biological system in man."

Cellzome launched in May 2000 in partnership with the European Molecular Biology Laboratory. In 2001, it acquired GSK's Cell Map protein-protein interaction unit, at which time the pharma firm became a minority shareholder.

In 2008, Cellzome signed a £14.4 million deal with GSK to use its Kinobeads platform to discover and develop kinase inhibitors for treating inflammatory disease. Under the agreement, Cellzome was also eligible for up to £118 million in potential development, regulatory, and commercial milestones, as well as double-digit royalties from sales of drugs developed through the partnership. It achieved the first milestone in the collaboration in December 2008, followed by a second and third milestone in March 2009, and a clinical candidate milestone in September 2011.

In 2010 the companies signed another pact, this time to use Cellzome's Episphere platform to research immunoinflammatory disease. Under this deal, Cellzome received a €33 million upfront payment from GSK and was eligible for milestone payments of more than €475 million. It achieved the first milestone in this agreement in December 2010 and a second in February 2011.

While the bulk of the two firms' work thus far has focused on inflammatory disorders, GSK sees potential for "a wide application" of Cellzome's technology across "many therapeutic areas," Hertzberg said, although he said the drugmaker hadn't yet prioritized areas where it might prove most useful.

Other pharmaceutical firms have also shown interest in chemical proteomics approaches like Cellzome's. Last February, German drugmaker Evotec acquired chemical proteomics firm Kinaxo Biotechnologies for €16 million (GWDN 2/9/2011).

Like Cellzome, Kinaxo, which was spun out of the Max Planck Institute by researchers including Matthias Mann, uses mass-spec based competition binding assays to profile small molecule drugs and drug targets. In June of last year, Evotec signed a deal with Roche to use the technology to identify biomarkers for oncology drugs in Roche's pipeline (PM 7/1/2011). Prior to the acquisition, Kinaxo had collaborations ongoing with pharma firms including Takeda and AstraZeneca.

In an interview with ProteoMonitor last year following announcement of the Roche deal, Evotec CEO Werner Lanthaler estimated that its Kinaxo business would grow at around 30 percent year over year.

Last month, University of North Carolina researchers published a paper in Cell on a chemical proteomics method similar to those developed by Cellzome and Kinaxo, which they used to study drug resistance in triple-negative breast cancer (PM 4/20/2012). That platform, UNC researcher Gary Johnson told ProteoMonitor, had drawn interest from a number of pharmaceutical companies including Novartis, Johnson & Johnson, and GSK.

GSK, in fact, "approached me a couple of years ago and wanted me to screen their whole library of kinase inhibitors [using the technique]," Johnson said. However, he noted, no agreement was ever reached for that project.

Cellzome itself has inked deals with a number of pharma firms outside of GSK including Novartis, Pfizer, Johnson & Johnson, and Bayer.

According to Stubbee, any of Cellzome's ongoing pharma collaborations will "be evaluated [by GSK] with the total package of programs to decide which one stay inside and which ones potentially could be spun out."

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