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Regulus Therapeutics Secures Additional Patents on microRNA Therapeutics for the Treatment of Hepatitis C Virus (HCV) Infection

Thursday, September 23, 2010

La Jolla, CA -- Regulus Therapeutics Inc. announced today 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. The EPO issued a Notice of Intent to Grant for an application in the ‘Sarnow’ patent series (European Patent Application No. 05749437.9) for claims covering the use of an antisense inhibitor of miR-122 for the treatment of HCV infection and related conditions, either alone or in combination with other HCV therapeutic agents. Additionally, the USPTO has recently allowed claims in a continuation application in the Sarnow patent series (US Serial No. 11/953,705), directed to methods of reducing HCV viral genome amount with an antisense inhibitor of miR-122 in combination with other HCV therapeutic agents. The Sarnow patent series, owned by Stanford University and licensed to Regulus, relates to the discovery and development of therapeutic products for HCV infection by inhibiting the liver-specific microRNA known as miR-122.

“We are very pleased that the Sarnow patent estate continues to generate patents worldwide. Notably, the claims capture uses of anti-miR-122 in combination with the therapeutic agents, such as interferon and ribavirin, which comprise the current standard of care for the treatment of HCV infection,” said Garry E. Menzel, Ph.D., Executive Vice President Corporate Development and Finance of Regulus.

Regulus controls a broad and dominant patent estate related to microRNA therapeutics, including miR-122 therapeutic agents. These two new patents will further strengthen the Regulus-controlled patent estate surrounding miR-122 compositions and methods of use, which includes but is not limited to:

  • 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)

miR-122 is a liver-expressed microRNA that has been shown to be a critical endogenous “host factor” for the replication of 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 (Regulus’ co-founders) 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. Through a collaboration with GlaxoSmithKline, Regulus is developing a microRNA therapeutic targeting miR-122 for the treatment of HCV infection as its most advanced therapeutic program. Regulus plans to identify a clinical development candidate in the fourth quarter of 2010 and file an investigational new drug (IND) application in 2011.

About microRNAs

The discovery of microRNA in humans is one of the most exciting scientific breakthroughs in the last decade. microRNAs are small RNA molecules, typically 20 to 25 nucleotides in length that do not encode proteins but instead regulate gene expression. Nearly 700 microRNAs have been identified in the human genome, and more than one-third of all human genes are believed to be regulated by microRNAs. As a single microRNA can regulate entire networks of genes, these new molecules are considered the master regulators of the genome. microRNAs have been shown to play an integral role in numerous biological processes including the immune response, cell-cycle control, metabolism, viral replication, stem cell differentiation and human development. Most microRNAs are conserved across multiple species indicating the evolutionary importance of these molecules as modulators of critical biological pathways. Indeed, microRNA expression or function has been shown to be significantly altered in many disease states, including cancer, heart failure and viral infections. Targeting microRNAs with anti-miRs, antisense oligonucleotide inhibitors of microRNAs, or miR-mimics, double-stranded oligonucleotides to replace microRNA function, opens the possibility of a novel class of therapeutics and a unique approach to treating disease by modulating entire biological pathways. To learn more about microRNAs please visit

About Regulus Therapeutics Inc.

Regulus Therapeutics is a biopharmaceutical company leading the discovery and development of innovative new medicines based on microRNAs. Regulus is targeting microRNAs as a new class of therapeutics by working with a broad network of academic collaborators and leveraging oligonucleotide drug discovery and development expertise from its founding companies Alnylam Pharmaceuticals (Nasdaq:ALNY) and Isis Pharmaceuticals (Nasdaq:ISIS). Regulus is advancing microRNA therapeutics towards the clinic in several areas including hepatitis C infection, cardiovascular disease, fibrosis, oncology, immuno-inflammatory diseases, and metabolic diseases. Regulus’ intellectual property estate contains both the fundamental and core patents in the field and includes over 600 patents and more than 300 pending patent applications pertaining primarily to chemical modifications of oligonucleotides targeting microRNAs for therapeutic applications. In April 2008, Regulus entered into a major alliance with GlaxoSmithKline to discover and develop microRNA therapeutics for immuno-inflammatory diseases. In February 2010, Regulus entered into a new collaboration with GlaxoSmithKline to develop and commercialize microRNA therapeutics targeting microRNA-122 for the treatment of Hepatitis C Viral infection. In June 2010, sanofi-aventis and Regulus entered into the largest-to-date strategic alliance on microRNA therapeutics focused initially on fibrosis. For more information, visit

Forward-Looking Statements

This press release includes forward-looking statements regarding the future therapeutic and commercial potential of Regulus’ business plans, technologies and intellectual property related to microRNA therapeutics being discovered and developed by Regulus, including the therapeutic potential of targeting microRNA-122. Any statement describing Regulus’ goals, expectations, financial or other projections, intentions or beliefs is a forward-looking statement and should be considered an at-risk statement. Such statements are subject to certain risks and uncertainties, particularly those inherent in the process of discovering, developing and commercializing drugs that are safe and effective for use as human therapeutics, and in the endeavor of building a business around such products. Such party’s forward-looking statements also involve assumptions that, if they never materialize or prove correct, could cause their results to differ materially from those expressed or implied by such forward-looking statements. Although these forward-looking statements reflect the good faith judgment of the management of Regulus, these statements are based only on facts and factors currently known by Regulus. As a result, you are cautioned not to rely on these forward-looking statements. These and other risks concerning Regulus’ programs are described in additional detail in each of Isis’ and Alnylam’s annual report on Form 10-K for the year ended December 31, 2009 and their most recent quarterly report on Form 10-Q, which are on file with the SEC. Copies of these and other documents are available from either Isis or Alnylam.

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