Galapagos patents high-stakes Alzheimer's breakthrough

Study finds GPR3 a promising drug target for the disease

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MECHELEN, Belgium—With estimates of the number of individuals affected running as high as 27 million patients worldwide in 2006—and the expectation that this number will quadruple by 2050—Galapagos NV has patented a human drug target that researchers believe plays a key role in Alzheimer's disease. Patent protection has been granted Galapagos in the U.S. and is expected in Europe and elsewhere, says company CEO Onno van de Stolpe.

Work at Galapagos to identify a number of targets in Alzheimer's disease began in 2005, when Dr. Bart De Strooper at the Flanders Institute for Biotechnology (VIB) and the KU Leuven in Belgium was brought aboard as an adviser. De Strooper is one of the leading international experts in the Alzheimer's field and was accorded the $200,000 MetLife prize in 2008 for his pioneering research. Supporting data recently published in Science are a result of the collaboration between Galapagos and Strooper's academic group.

According to Stolpe, the data "prove the key role of GPR3 in Alzheimer's." Galapagos is now starting drug discovery with the aim of delivering a candidate drug to treat the disease.

Using its proprietary adenoviral-based discovery platform, Galapagos has developed a collection of adenoviruses that have human short hairpin RNA (shRNA) cloned into the viral background. These produce double-stranded RNA that are cleaved by a dicer to miRNA. GPR3 was identified in human cells using the Galapagos platform, which was developed between 1999 and 2003 and is patented here and in Europe. Inhibition of GPR3 prevents the accumulation of beta-amyloid, a protein that exists at higher levels in the brains of Alzheimer's patients. GPR3 levels are higher in the areas of the brain that are affected in Alzheimer's patients. Galapagos believes the activity of GPR3 can likely be inhibited with a small molecule drug, which makes GPR3 a promising drug target for development of a treatment for Alzheimer's disease.

Citing the fact that his company has a number of targets running in parallel, Stolpe says that Galapagos is concentrating its resources on the development of first-in-class medicines against bone and joint diseases, while Strooper's academic group continues work in the GRR3-Alzheimer's area. He is confident the results will be breakthroughs in treatment that stop disease rather than just treating the symptoms.

Preclinical development has started on the first rheumatoid arthritis candidate compound—a completely novel kinase, Stolpe says—with the aim of initiating a Phase I clinical trial within two months. Galapagos plans to enter into discussions with potential pharmaceutical partners as GPR3 progresses into drug discovery. The company has already established risk-sharing alliances with GSK, Janssen Pharmaceutica, Eli Lilly and Merck, CEO Stolpe notes. Through an alliance with MorphoSys, Galapagos is also developing new antibody therapies in bone and joint diseases.

Overall, in 2009, Galapagos expects to have three compounds in clinical development, revenues of €100 million, and a year-end cash balance of €20 million. The company currently employs 470 people and operates facilities in six countries.

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