Changing the channel

Milestone-driver collaboration between Essen BioScience and Nycomed boosts ion-channel drug discovery

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ANN ARBOR, Mich.—Essen BioScience Inc., a specialty provider of cell-based assay solutions and contract research services, and Nycomed, a privately owned global pharmaceutical company headquartered in Zurich, Switzerland, have agreed to cooperate in research aimed at identifying novel small-molecule ion channel modulators as pain therapeutics.

Ion channels are complex, multi-subunit proteins that govern the movement of ions across the cell membrane, which the two companies are betting offer unique opportunities for drug discovery.

"As inventors of two paradigm-shifting ion channel assay technologies, IonWorks and FLIPR, we have a deep understanding of the biological and technical requirements for constructing relevant ion channel assays," says Dr. Derek Trezise, European Discovery Services, who will head the Essen team from its recently opened European office at the BioPark in Welwyn Garden City, U.K.

In April 2010, the company changed its name from Essen Instruments to Essen BioScience to better reflect its current business model.

Under the terms of the agreement, the two companies will collaborate to screen, optimize and develop modulators of voltage-gated ion channels. Essen BioScience will provide core expertise in ion channel drug discovery, planar array electrophysiology and in vitro profiling. Nycomed will contribute capabilities in medicinal chemistry, drug discovery and development.

IonWorks and FLIPR—the two technical platforms that anchor the joint program—are Essen developments the company believes may revolutionize ion channel-directed research. The process involves a high-throughput cell-based assay (FLIPR) and high-throughput planar electrophysiology (IonWorks). Generically referred to as patch clamp electrophysiology, the method positions a glass microelectrode on the surface of a single cell and uses low-noise amplifier circuitry to measure ionic currents with high sensitivity and temporal resolution.

While extremely powerful, the conventional patch clamp method is technically demanding and slow, and this has hindered the application of this method for drug screening and other types of experiments. The Essen IonWorks platform provides a quantal increase in the throughput of patch clamp electrophysiology. The system uses machined apertures (1-2μm) in a planar, kapton substrate as the recording sites and is formatted as a 384-well microtiter plate to increase the number of possible recordings from five to 10 or in excess of 3,000 per day, enabling new approaches to ion channel science.

Financial terms of the agreement were not disclosed, but Trezise was specific about the importance of its milestone-driven context.  

"The milestone-driven aspect of this collaboration recognizes our team's experience in ion channel drug discovery as well as ion channel technology," he says. Any other arrangement "would have made less sense," he adds.

Trezise notes that while Essen is a hybrid instruments and service company, its senior staff have more than 100 years of drug discovery experience and regard themselves as drug discovery solution providers.

Nycomed's strategy, on the other hand, is to build partnerships to develop new, innovative products. Its R&D effort is structured around partnerships, and in-licensing is a cornerstone of the company's growth strategy.

In that regard, Sham Nikam, head of global discovery, refers to the Essen collaboration as "a real win-win situation" and notes that it significantly strengthens Nycomed's development pipeline.

A privately owned global pharmaceutical company with a differentiated portfolio focused on branded medicines in gastroenterology, respiratory and inflammatory diseases, pain, osteoporosis and tissue management, Nycomed employs 12,000 associates worldwide. The company generated total sales of $4.2 billion in 2009 and an adjusted EBITDA of $1.4 billion.

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