title: Emerging small molecule drugs.
abstract: Dyslipidaemia is a major risk factor for cardiovascular diseases. Pharmacological lowering of LDL-C levels using statins reduces cardiovascular risk. However, a substantial residual risk persists especially in patients with type 2 diabetes mellitus. Because of the inverse association observed in epidemiological studies of HDL-C with the risk for cardiovascular diseases, novel therapeutic strategies to raise HDL-C levels or improve HDL functionality are developed as complementary therapy for cardiovascular diseases. However, until now most therapies targeting HDL-C levels failed in clinical trials because of side effects or absence of clinical benefits. This chapter will highlight the emerging small molecules currently developed and tested in clinical trials to pharmacologically modulate HDL-C and functionality including new CETP inhibitors (anacetrapib, evacetrapib), novel PPAR agonists (K-877, CER-002, DSP-8658, INT131 and GFT505), LXR agonists (ATI-111, LXR-623, XL-652) and RVX-208.
authors.affiliation: Université Lille 2, F-59000, Lille, France.
authors.forename: Sophie
authors.initials: S
authors.lastname: Colin
authors.forename: Giulia
authors.initials: G
authors.lastname: Chinetti-Gbaguidi
authors.forename: Jan A
authors.initials: JA
authors.lastname: Kuivenhoven
authors.forename: Bart
authors.initials: B
authors.lastname: Staels
mesh_terms: D000818:Animals; D002318:Cardiovascular Diseases / Q000209:etiology / Q000378:metabolism / Q000517:prevention & control*; D053480:Cholesterol Ester Transfer Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D015195:Drug Design; D050171:Dyslipidemias / Q000150:complications / Q000188:drug therapy* / Q000378:metabolism; D006801:Humans; D000960:Hypolipidemic Agents / Q000737:chemistry / Q000627:therapeutic use*; D000071518:Liver X Receptors; D058990:Molecular Targeted Therapy; D057093:Orphan Nuclear Receptors / Q000819:agonists / Q000378:metabolism; D047492:Peroxisome Proliferator-Activated Receptors / Q000819:agonists / Q000378:metabolism; D011799:Quinazolines / Q000627:therapeutic use; D052999:Quinazolinones; D015398:Signal Transduction / Q000187:drug effects
chemical_list: C506642:CETP protein, human; D053480:Cholesterol Ester Transfer Proteins; D000960:Hypolipidemic Agents; D000071518:Liver X Receptors; D057093:Orphan Nuclear Receptors; D047492:Peroxisome Proliferator-Activated Receptors; D011799:Quinazolines; D052999:Quinazolinones; C000628794:apabetalone