Regulus' Kleanthis G. Xanthopoulos, Ph.D., to Step Down as President and Chief Executive Officer

LA JOLLA, Calif. -- Regulus Therapeutics Inc. (NASDAQ: RGLS), a biopharmaceutical company leading the discovery and development of innovative medicines targeting microRNAs, announced today that Kleanthis G. Xanthopoulos, Ph.D. has resigned as President and Chief Executive Officer and as a member of Regulus' Board of Directors, effective today, to pursue investment opportunities in the biotechnology industry.  Paul Grint, M.D., who previously served as Chief Medical Officer of Regulus, has been appointed as President and Chief Executive Officer and as a member of Regulus' Board of Directors effective today.  In addition, Neil W. Gibson, Ph.D., who has served as Chief Scientific Officer, will continue through June 30, 2015 at the company as President's Fellow to assist Dr. Grint in assembling a new leadership team. 

"I am extremely proud of our achievements at Regulus and am excited about the future of the company and microRNA therapeutics as they become a new and major class of drugs.  RG-101, our GalNAc-conjugated anti-miR-122, is moving rapidly into Phase II and our 'Clinical Map Initiative' strategy is on track to create multiple clinical programs," said Kleanthis G. Xanthopoulos, Ph.D. "Paul shares a common vision to continue to build a leading biopharmaceutical company based on our innovative microRNA platform across multiple therapeutic areas.  I am truly honored to have been a part of building this great company." 

"Under Kleanthis' leadership, Regulus has grown from a small, private company to a rapidly maturing, publicly traded biopharmaceutical company with an exciting technology platform, multiple strategic alliances and collaborations with leading large pharmaceutical companies, and a robust microRNA therapeutics pipeline," said Stelios Papadopoulos, Ph.D., Chairman of the Board of Directors of Regulus.  "We thank Kleanthis for his contributions over the last seven years - his passion for building the company and dedication to discovering and developing therapeutics for patients in need have benefited Regulus greatly." 

Dr. Papadopoulos continued, "We are pleased to appoint Paul as President and Chief Executive Officer and believe that he is perfectly positioned to lead the company.  He has over two decades of executive level experience in drug development and is a recognized leader in our industry.  In particular, his appointment is important at this time as the company increases its investment and focus on RG-101." 

Dr. Grint also commented, "I am honored for the opportunity to lead this great company and particularly excited about entering into multiple Phase II studies for RG-101, with critical four-week combination data coming by year-end.  In addition, we remain focused on the advancement of the overall portfolio and have many key catalysts on the horizon.  In the near term, we expect to initiate our first-in-human clinical study of RG-012, our anti-miR-21 for the treatment of Alport syndrome, and we are aggressively pursuing additional attractive microRNA targets to expand our leadership in the field." 

About Regulus

Regulus Therapeutics Inc. (NASDAQ: RGLS) is a biopharmaceutical company leading the discovery and development of innovative medicines targeting microRNAs.  Regulus has leveraged its oligonucleotide drug discovery and development expertise to develop a well-balanced microRNA therapeutics pipeline complemented by a maturing microMarkersSM biomarkers platform and a rich intellectual property estate to retain its domain dominant leadership in the microRNA field.  Under its 'Clinical Map Initiative', Regulus is developing RG-101, a GalNAc-conjugated anti-miR targeting microRNA-122 for the treatment of chronic hepatitis C virus infection, and RG-012, an anti-miR targeting microRNA-21 for the treatment of Alport syndrome, a life-threatening kidney disease driven by genetic mutations with no approved therapy. In addition, RG-125, a GalNAc-conjugated anti-miR targeting microRNA-103/107 for the treatment of NASH in patients with type 2 diabetes/pre-diabetes, has been selected for clinical development.  Regulus is also advancing several programs toward clinical development in orphan disease indications, oncology and fibrosis.  Regulus' commitment to innovation has resulted in multiple peer-reviewed publications in notable scientific journals and has resulted in the formation of strategic alliances with AstraZeneca and Sanofi and a research collaboration with Biogen focused on microRNA biomarkers.  Regulus maintains its corporate headquarters in La Jolla, CA.  For more information, please visit http://www.regulusrx.com

Forward-Looking Statements

Statements contained in this press release regarding matters that are not historical facts are "forward-looking statements" within the meaning of the Private Securities Litigation Reform Act of 1995, including statements associated with the duration of Dr. Gibson's services as President's Fellow, the expected ability of Regulus to undertake certain activities and accomplish certain goals, the projected timeline of clinical development activities, and expectations regarding future therapeutic and commercial potential of Regulus' business plans, technologies and intellectual property related to microRNA therapeutics and biomarkers being discovered and developed by Regulus.  Because such statements are subject to risks and uncertainties, actual results may differ materially from those expressed or implied by such forward-looking statements. Words such as "believes," "anticipates," "plans," "expects," "intends," "will," "goal," "potential" and similar expressions are intended to identify forward-looking statements. These forward-looking statements are based upon Regulus' current expectations and involve assumptions that may never materialize or may prove to be incorrect.  Actual results and the timing of events could differ materially from those anticipated in such forward-looking statements as a result of various risks and uncertainties, which include, without limitation, risks associated with 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 drugs.  These and other risks concerning Regulus' financial position and programs are described in additional detail in Regulus filings with the Securities and Exchange Commission.  All forward-looking statements contained in this press release speak only as of the date on which they were made. Regulus undertakes no obligation to update such statements to reflect events that occur or circumstances that exist after the date on which they were made.