miR-122 is a liver-expressed microRNA that has been shown to be a critical endogenous “host factor” for the replication of hepatitis C virus (HCV), and anti-miRs targeting miR-122 have been shown to block HCV infection (Jopling et al. (2005) Science 309, 1577-81). In earlier work, scientists at Alnylam Pharmaceuticals and Isis Pharmaceuticals demonstrated the ability to antagonize miR-122 in vivo using chemically modified single-stranded anti-miR oligonucleotides. Data from multiple preclinical studies have shown a robust HCV antiviral effect following inhibition of miR-122.
Regulus Therapeutics Inc. is developing a microRNA therapeutic targeting miR-122 for the treatment of HCV infection and plans to file an investigational new drug (IND) application in 2011.
Today, Regulus announced that the European Patent Office (EPO) and United States Patent and Trademark Office (USPTO) have recently granted claims for microRNA-122 therapy in hepatitis C viral (HCV) infections. These two new patents will further strengthen the Regulus-controlled patent estate surrounding miR-122 compositions and methods of use, which include:
- The ‘Sarnow’ patent claiming the use of anti-miR-122 to inhibit HCV replication (US Patent No. 7,307,067)
- The ‘Esau’ patent claiming the use of anti-miRs targeting miR-122 as inhibitory agents (US Patent No. 7,683,036)
- The ‘Tuschl III’ patent claiming compositions of matter for miR-122 and complementary oligonucleotides (US Patent No. 7,232,806)
- The ‘Manoharan’ patent claiming antagomirs, including antagomirs targeting miR-122 (US Patent No. 7,582,744)
- A recently granted Regulus-owned European application claiming the use of miR-122 antagonists for reducing cholesterol (EP Application No. 06813949.2)