Sanofi-Aventis (France) (SASY.PA) Completes $10 Million Equity Investment in Regulus Therapeutics, Inc.

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LA JOLLA, Calif.--(BUSINESS WIRE)-- Regulus Therapeutics Inc. announced today that the Company has received a $10 million equity investment from sanofi-aventis in connection with the landmark alliance the two companies entered into on June 21, 2010. The equity investment by sanofi-aventis further strengthens the balance sheet of Regulus, and with this investment sanofi-aventis becomes the third investor in Regulus, along with its founding companies Alnylam Pharmaceuticals, Inc. (Nasdaq:ALNY - News) and Isis Pharmaceuticals, Inc. (Nasdaq:ISIS - News).

"The alliance with Regulus underscores the commitment to innovation by sanofi-aventis as microRNAs represent a new therapeutic approach for developing medicines for treating serious diseases," said Philippe Goupit, Vice President of Corporate Licenses of sanofi-aventis. "Regulus has created a microRNA innovation engine that uniquely combines a deep understanding of microRNA biology with a mature oligonucleotide drug platform to effectively modulate microRNAs."

The alliance between Regulus and sanofi-aventis, valued at potentially over $750 million, is for the discovery, development and commercialization of microRNA therapeutics toward four targets including Regulus' leading fibrosis program targeting microRNA-21. The investment of $10 million in Regulus by sanofi-aventis represents less than 10% ownership of the preferred outstanding shares. The remaining preferred outstanding shares are owned equally by Alnylam and Isis.

"We are very pleased to be working in a partnership with sanofi-aventis for the development of microRNA therapeutics that could potentially open a new paradigm in the treatment of major diseases. Sanofi-aventis has an excellent track record for innovation and bringing value to patients," said Garry E. Menzel, Ph.D., Executive Vice President Corporate Development and Finance of Regulus. "With the addition of $10 million from the sanofi-aventis equity investment, Regulus has to date raised $40 million from equity financings and over $58 million from strategic pharmaceutical alliances."

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 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 http://www.regulusrx.com/microrna/microrna-explained.php.

About Regulus Therapeutics Inc.

Regulus Therapeutics is a biopharmaceutical company leading the discovery and development of innovative new medicines targeting microRNAs. Regulus is using a mature therapeutic platform based on technology that has been developed over 20 years and tested in greater than 5,000 human subjects. In addition, Regulus works with a broad network of academic collaborators and leverages 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, immuno-inflammatory diseases, fibrosis, oncology, and cardiovascular/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 for the development of microRNA therapeutics. This alliance is focused initially on fibrosis. For more information, visit http://www.regulusrx.com.