Regulus Therapeutics Inc announced that it achieved the initial milestone from GlaxoSmithKline (GSK) as part of their ongoing worldwide strategic alliance established to discover, develop and market novel microRNA-based therapeutics to treat inflammatory diseases. The two companies are working to identify drugs directed at four different microRNA targets related to inflammatory disease.

Regulus has now reached an important discovery milestone, which triggered a payment, concurrent with the first demonstration of a pharmacological effect in immune cells by specific microRNA inhibition. Scientists successfully delivered specific microRNA inhibitors, known as anti-miRs, to mice and clearly identified changes in expression of the genes regulated by the microRNA in immune cells.

"This milestone is further evidence that microRNAs represent disease targets whose therapeutic modulation could revolutionize the way we treat immune diseases," said Peter S Linsley, chief scientific officer at Regulus. "We believe that we are the leaders in microRNA and are delighted to have such a good partner as GSK supporting the translation of our groundbreaking research into therapeutic opportunities. We are particularly pleased that this has been achieved in the first year of the collaboration."

The Regulus-GSK alliance, which has a potential value of nearly $600 million, was established in April 2008 to focus on inflammatory diseases. Regulus is responsible for the development of antagonists to four microRNA targets from discovery through completion of clinical proof of concept. GSK has an exclusive license for worldwide development and commercialization of drugs developed by Regulus under each program for the relevant microRNA. The alliance combines Regulus' unique expertise and comprehensive intellectual property estate in the microRNA therapeutics field with GSK's extensive inflammatory disease expertise.

microRNAs are a recently discovered class of genetically encoded endogenous RNAs, approximately 20 nucleotides in length, that are believed to regulate the expression of a large number of human genes.

Regulus Therapeutics is a biopharmaceutical company aiming to discover, develop, and commercialize microRNA-based therapeutics.