Resverlogix' RVX-208 increases plasma levels of Apolipoprotein A-I and HDL-cholesterol

Jun 9 2010

Resverlogix ("Resverlogix" or the "Company") (TSX:RVX) is pleased to announce that it has collaborated with the Division of Cardiology at the Research Institute of the McGill University Health Centre (RI of the MUHC), to publish today in the Journal of American College of Cardiology (JACC), a report entitled 'RVX-208 A Small Molecule that Increases Apolipoprotein A-I and High Density Lipoprotein Cholesterol In Vitro and In Vivo'. This peer reviewed manuscript contains important data that describes the successful results of many studies detailing the actions of RVX-208, an orally active novel small molecule for the treatment of atherosclerosis. Dr. Norman Wong, MD, FRCPC, Chief Scientific Officer of Resverlogix stated, "The scientific information contained in this seminal work provides key evidence that RVX-208 is positively impacting critical components of reverse cholesterol transport (RCT). These actions of RVX-208 to enhance RCT and thereby facilitate the removal of cholesterol from atherosclerotic lesions are believed to underlie the protective role of high density lipoprotein cholesterol (HDL) against cardiovascular disease (CVD)."

The manuscript in JACC concludes that RVX-208 successfully increases plasma Apolipoprotein A-I (ApoA-I) and HDL-cholesterol (HDL-C) in addition to altering the biochemical properties, metabolism, and function of HDL. For more than three decades members of the cardiovascular research community have searched for ways to raise plasma levels of ApoA-I/HDL-C. One of the more desirable approaches is to use an orally active small molecule therapeutic. CVD is the leading cause of death in developed nations. In the USA alone, the annual cost in 2009 to the American health care system totaled $475.3 billion, according to the American Heart Association. The underlying cause of CVD is atherosclerosis or so called 'hardening of the arteries' due to the build up of cholesterol inside the plaques that line the wall of the arteries. While statin therapies are the current standard of care for CVD, their effects only prevent progression of the disease. In contrast, a novel therapy that targets ApoA-I/HDL-C to augment RCT has the potential to not only stabilize but possibly reverse atherosclerosis and thus reduce CVD risk beyond the actions of statins.

"The ability of RVX-208 to enhance cholesterol efflux is the first and most important step in reverse cholesterol transport, the process by which cholesterol is removed from the wall of the arteries. Our data show that RVX-208 stimulates the production Apolipoprotein A-I, the major protein component of HDL to trigger the formation of early HDL particles, (so called pre-beta HDL particles) which play the key role in removing cholesterol from cells; this, in turn raise the total mass of HDL-C. This change in HDL profile towards the early, or 'nascent' HDL particles is believed to be an important factor in promoting RCT," said Dr. Jacques Genest, MD, Professor, Faculty of Medicine at McGill University and Director of the Division of Cardiology at the Royal Victoria Hospital of the RI of the MUHC.

The first author in the JACC article is Ms. Dana Bailey who leads a team comprised of many scientific members of Resverlogix. This article is also available online through the electronic edition of the Journal of American College of Cardiology (www.onlinejacc.org). JACC is considered by many as the premiere journal in the field of clinical cardiology.

Resverlogix is also pleased to announce the publication of an additional peer reviewed journal article entitled "Stilbene Analogs as Inducers of ApoA-l Transcription." It appeared in the European Journal of Medicinal Chemistry 2010, 45, 2018-2023, a leading publication devoted to topics in chemistry. The topic of this manuscript details the ability of novel compounds to stimulate ApoA-I gene transcription.