JPO to grant patent from the Tuschl III patent series

Regulus Therapeutics Inc., Alnylam Pharmaceuticals, Inc. (Nasdaq: ALNY), and Isis Pharmaceuticals, Inc. (Nasdaq: ISIS), announced today that the Japan Patent Office (JPO) has notified the Max Planck Society of its intent to grant a patent from the Tuschl III patent series (JP Application Number 2003-532675). This patent series pertains to the discovery of over 120 novel mammalian microRNAs, including miR-122, which is a leading pre-clinical program at Regulus. The grant of this first Tuschl III patent in Japan extends the scope of this patent estate, which has already yielded patents in the U.S. (U.S. Patent No. 7,232,806) and in Australia (Australian Patent No. 2002 347 035).

The Tuschl III patent series stems from groundbreaking research (Lagos-Quintana et al., (2001) Science 294, 853-858) performed by Alnylam founder and Regulus scientific advisory board member Dr. Thomas Tuschl, Associate Professor of RNA Molecular Biology at The Rockefeller University, while at the Max Planck Society. The Tuschl III patent series is exclusively held by Regulus for microRNA therapeutics through license agreements amongst Max Planck, Alnylam, and Isis.

“Regulus is advancing a whole new frontier of pharmaceutical research through the discovery of microRNA therapeutics, which have the potential to affect broad disease pathways as opposed to single gene targets,” said Kleanthis G. Xanthopoulos, Ph.D., President and Chief Executive Officer of Regulus Therapeutics. “Through our partnerships with Alnylam, Isis, and our relationships with leading academic institutions such as the Max Planck, we have built a dominant intellectual property estate for the development of microRNA therapeutics. This is first in the Tuschl III series to grant in Japan, and we expect more to come from this important and early patent series.”

“We are pleased with the continued recognition of the pioneering contributions of Professor Tuschl’s work performed at the Max Planck,” said Dr. Joern Erselius, Managing Director, Max Planck-Innovation GmbH. “The Tuschl III patent series describes an important set of discoveries for the advancement of microRNA therapeutics. With Regulus, we have an ideal partner for the development of this seminal research into a promising new approach for medicine.”

The newly granted claims of the Tuschl III patent cover miR-122, a liver-specific microRNA that has subsequently been shown to facilitate replication of hepatitis C virus (HCV) infection. The claims cover single-stranded and double-stranded antisense compounds complementary to mir-122, as well as precursors and analogs of mir-122.

Regulus is advancing microRNA therapeutics targeting miR-122, among others. Pre-clinical studies suggest that miR-122 is essential for the replication of HCV (Jopling et al. (2005) Science 309, 1577-81) and that creating an inhibitor to miR-122 may define a novel therapeutic strategy for the treatment of HCV infection.