title: An evaluation of RVX-208 for the treatment of atherosclerosis.
abstract: BACKGROUND
  RVX-208 is a first-in-class, orally active, novel small molecule in development by Resverlogix Corporation (Calgary, AB, Canada). It acts through an epigenetic mechanism by inhibiting the bromodomain and extraterminal (BET) family of proteins, increasing apolipoprotein A-I (apoA-I) and targeting high-density lipoprotein (HDL) metabolism, including generating of nascent HDL and increased larger HDL particles, resulting in the stimulation of reverse cholesterol transport. RVX-208 also has a beneficial effect on inflammatory factors known to be involved in atherosclerosis and plaque stability. New therapeutic strategies are needed for patients with atherosclerosis.
  
  
  METHODS
  In this review, the authors evaluate the use of RVX-208 as an agent for the treatment of atherosclerosis. The article is based on a literature search considering both animal and human studies available on PubMed as well as Media Releases from the Resverlogix Corporation.
  
  
  CONCLUSIONS
  The current evidence suggests promising beneficial effects of this novel drug in the prevention and treatment of atherosclerosis and other metabolic disorders. Its unique mechanism of action is encouraging; it affects several pathways and has a modest effect on HDL levels. There is also a shift in particle size to larger HDL particles, which may have potent atheroprotective effects. Future clinical development is needed, including safety assessment.
authors.affiliation: a 1 University of Palermo, Biomedical Department of Internal Medicine and Medical Specialties , Palermo, Italy.
authors.forename: Dragana
authors.initials: D
authors.lastname: Nikolic
authors.affiliation: a 1 University of Palermo, Biomedical Department of Internal Medicine and Medical Specialties , Palermo, Italy.|b 2 Euro-Mediterranean Institute of Science and Technology , Italy.
authors.forename: Manfredi
authors.initials: M
authors.lastname: Rizzo
authors.affiliation: c 3 University College London (UCL), University College London Medical School, Department of Clinical Biochemistry , Royal Free Campus, London, UK.
authors.forename: Dimitri P
authors.initials: DP
authors.lastname: Mikhailidis
authors.affiliation: d 4 University of Calgary, Department of Medicine, Biochemistry and Molecular Biology , Calgary, Alberta, Canada.
authors.forename: Norman C
authors.initials: NC
authors.lastname: Wong
authors.affiliation: e 5 University of Lodz, Medical University of Lodz, WAM University Hospital in Lodz, Department of Hypertension , Zeromskiego 113; 90-549 Lodz, Poland +48 4 2639 3771 ; +48 4 2639 3771 ; maciejbanach@aol.co.uk.
authors.forename: Maciej
authors.initials: M
authors.lastname: Banach
mesh_terms: D000818:Animals; D050197:Atherosclerosis / Q000188:drug therapy* / Q000503:physiopathology / Q000517:prevention & control; D008076:Cholesterol, HDL / Q000097:blood; D044127:Epigenesis, Genetic; D006801:Humans; D008659:Metabolic Diseases / Q000188:drug therapy / Q000503:physiopathology / Q000517:prevention & control; D058226:Plaque, Atherosclerotic / Q000188:drug therapy* / Q000473:pathology; D011799:Quinazolines / Q000494:pharmacology / Q000627:therapeutic use*; D052999:Quinazolinones
chemical_list: D008076:Cholesterol, HDL; D011799:Quinazolines; D052999:Quinazolinones; C000628794:apabetalone
keywords: RVX-208; apolipoprotein A-I; atherosclerosis; high-density lipoprotein; high-density lipoprotein particles