SAN DIEGO, Oct. 30 /PRNewswire-FirstCall/ -- Metabasis Therapeutics, Inc. , a biopharmaceutical company focused on the discovery, development and commercialization of novel drugs to address some of the world’s most widespread and costly chronic diseases, announced today that it has initiated a Phase 1 clinical trial of MB07811, a novel, orally active product candidate for the management of hyperlipidemia, or elevated cholesterol. MB07811, Metabasis’ fifth internally discovered product candidate to enter human clinical trials, uses the Company’s proprietary HepDirect(R) prodrug technology to target a beta-subtype-selective thyroid hormone receptor (TRB) agonist to the liver to reduce serum cholesterol (LDL) and triglycerides (TGs). The Company believes that this drug class has the potential to be additive to the class of hyperlipidemia drugs known as “statins”, and preclinical data suggests that MB07811 could be as effective at lowering serum cholesterol as this important drug class. Statins represent a drug class commonly used to treat hyperlipidemia and at present comprise the single largest pharmaceutical market in the world, growing by over 15% per year.
The study initiated today will evaluate the safety and tolerability of MB07811 in a rising single dose study in healthy volunteers. Assuming the successful completion of additional preclinical trials and the recently initiated Phase 1 single dose trial, the Company expects to pursue further clinical studies, including a multiple dose Phase 1 study in healthy volunteers.
Thyroid hormone receptor agonists are known to reduce cholesterol in animal models, but typically at doses similar to those associated with potential safety concerns, including cardiac and other non-hepatic toxicities. MB07811 is a HepDirect prodrug of a novel TRB receptor agonist discovered at Metabasis that is designed to deliver the agonist to the site where cholesterol is produced, i.e. the liver, while reducing the exposure of the agonist to other tissues. The Company believes that liver-targeting may avoid the safety concerns previously seen with non-liver targeted TRB agonists and thus unlock the therapeutic potential of this approach.
Cardiovascular disease is the leading cause of death worldwide, and in the U.S. alone claims more lives than cancer, chronic respiratory diseases, accidents and diabetes combined. Patients with hyperlipidemia, a clinical condition characterized by an elevation of cholesterol and/or triglycerides in the bloodstream, are at greater risk of cardiovascular disease and of experiencing a heart attack or stroke. Even though many patients take medications designed to lower serum cholesterol, such as statins, over 80% of patients with hyperlipidemia remain above the targeted levels set by the National Cholesterol Education Program. Although effective for treating many patients with elevated LDL cholesterol, statins have little affect on TGs, and can cause side effects, especially at doses that are often required to achieve target LDL levels.
In preclinical studies, Metabasis demonstrated that MB07811 lowers LDL cholesterol with a significantly improved safety profile relative to non-liver targeted TRB agonists. In addition, studies in rabbits and primates showed that MB07811 resulted in significant cholesterol lowering either alone or in combination with a statin. Preclinical studies have also shown that MB07811 results in decreased triglycerides which in certain animal models can result in reduced liver fat. High levels of triglycerides are also associated with increased risk of cardiac disease, and fatty liver is associated with increased risk of diabetes and chronic liver disease.
“We have extensively evaluated the potential of MB07811 in numerous animal models including primates and we are encouraged by the results seen to date,” commented Dr. Mark Erion, executive vice president of research and development and chief scientific officer. “We are excited to begin human clinical trials as we believe that MB07811 could prove to be the first in an important new class of hyperlipidemia therapies. MB07811 was designed using our knowledge in targeting drugs to the liver and our proprietary HepDirect technology. The HepDirect technology is currently used in pradefovir and MB07133, two product candidates that are currently in clinical trials for the treatment of hepatitis B and primary liver cancer, respectively. Clinical data to date on both of these promising product candidates have provided evidence that the HepDirect technology is targeting drugs to the liver, as expected. If liver targeting can unlock the efficacy of the TRB agonists by avoiding the safety concerns that have prevented them from advancing in the clinic in the past, we may be able to provide physicians and patients with an important new approach to controlling hyperlipidemia.”
“Hyperlipidemia and cardiovascular disease remain inadequately treated despite the availability of statins,” said Dr. Paul Laikind, president and chief executive officer. “MB07811 represents an exciting new strategy for treating this disease. In addition, MB07811 expands our pipeline of product candidates for metabolic disease, namely CS-917 and MB07803, both currently in clinical trials for the treatment of type 2 diabetes. Lastly, we are proud of the fact that MB07811 is the fifth product candidate discovered by Metabasis’ talented research team to enter clinical trials since the Company was founded. We expect to continue that record of accomplishment by recommending additional clinical candidates targeting metabolic diseases possibly over the next few years.”
About Metabasis (www.mbasis.com):
Metabasis Therapeutics is a biopharmaceutical company focused on the discovery, development and commercialization of novel drugs to address some of the world’s most widespread and costly chronic diseases involving pathways in the liver. The Company has established a pipeline that includes clinical stage and preclinical product candidates targeting major diseases with significant unmet medical needs. Targeted diseases include metabolic diseases such as diabetes, hyperlipidemia and obesity as well as liver diseases such as hepatitis and primary liver cancer. Metabasis has developed several proprietary technologies for use in discovering and optimizing drugs, including the NuMimetic(TM) and HepDirect(R) technologies. Metabasis is continuing to identify and develop new product candidates using its proprietary technologies and expertise.
Forward-Looking Statements:
Statements in this press release that are not strictly historical in nature constitute “forward-looking statements.” Such statements include, but are not limited to, references to the potential safety, efficacy and market potential of MB07811, the benefits of Metabasis’ HepDirect technology, and the Company’s ability to recommend additional clinical candidates targeting metabolic diseases. Such forward-looking statements involve known and unknown risks, uncertainties and other factors which may cause Metabasis’ actual results to be materially different from historical results or from any results expressed or implied by such forward-looking statements. These factors include, but are not limited to, the progress and timing of clinical trials for Metabasis’ product candidates; the fact that positive results from clinical trials does not necessarily mean later clinical trials will succeed; difficulties or delays in development, testing, obtaining regulatory approval, producing and marketing Metabasis’ product candidates; the potential and progress of preclinical compounds and programs; and risks and uncertainties discussed in the “Risk Factors” section of Metabasis’ Quarterly Report on Form 10-Q for the quarter ended June 30, 2006 and in Metabasis’ other filings with the Securities and Exchange Commission. All forward-looking statements are qualified in their entirety by this cautionary statement. Metabasis is providing this information as of this date of this release and does not undertake any obligation to update any forward-looking statements contained in this release as a result of new information, future events or otherwise.
Metabasis Therapeutics, Inc.
CONTACT: Constance C. Bienfait, Vice President, Investor Relations &Corporate Communications of Metabasis Therapeutics, Inc., +1-858-622-5575
Web site: http://www.mbasis.com/
