Singapore, April 21, 2008:  GlaxoSmithKline (GSK) and Regulus Therapeutics LLC (Regulus) announced a worldwide strategic alliance to discover, develop and market novel microRNA-targeted therapeutics to treat inflammatory diseases such as rheumatoid arthritis and inflammatory bowel disease. Regulus is a joint venture between Alnylam Pharmaceuticals and Isis Pharmaceuticals.

 

The alliance leverages Regulus’ unique expertise and intellectual property position in the discovery and development of microRNA-targeted therapeutics and provides GSK with an option to license product candidates directed at four different microRNA targets with relevance in inflammatory disease. Regulus will be responsible for the discovery and development of the microRNA antagonists through completion of clinical proof of concept, unless GSK chooses to exercise its option earlier.

 

After exercise of the option, GSK will have an exclusive license to drugs developed under each program by Regulus for the relevant microRNA target for further development and commercialization on a worldwide basis. Regulus will have the right to further develop and commercialize any microRNA therapeutics which GSK chooses not to develop or commercialize.

 

Regulus will receive $20 million in upfront payments from GSK, including a $15 million option fee and a $5 million note (guaranteed by Isis and Alnylam) that will convert into Regulus common stock in the future under certain specified circumstances. Regulus could also be eligible to receive up to $144.5 million in development, regulatory and sales milestone payments for each of the four microRNA-targeted therapeutics discovered and developed as part of the alliance. In addition to the potential of nearly $600 million Regulus could receive in option, license and milestone payments, Regulus would also receive tiered royalties up to double digits on worldwide sales of products resulting from the alliance.

 

“We are focused on finding innovative medicines through both internal efforts and by 'virtualizing' a portion of the inflammatory diseases pipeline. We are very excited to be working with Regulus and exploring the therapeutic opportunities in inflammation offered by targeting microRNAs, an exciting new area of biology,” said Dr Jose Carlos Gutierrez-Ramos, Senior Vice President and head of the Immuno-Inflammation Center of Excellence for Drug Discovery of GSK.

 

Dr Kleanthis G. Xanthopoulos, President and Chief Executive Officer of Regulus said, “We look forward to expanding our efforts in inflammation where a new class of therapeutics could offer novel options to treat disease. microRNA therapeutics represents an exciting new frontier for pharmaceutical research, opening many opportunities including those present in inflammation and immune diseases. Regulus has the expertise and access to proprietary antisense technologies, which provide the tools and potential to quickly move therapeutic programs toward the clinic.”