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Apabetalone
Chemical compound / From Wikipedia, the free encyclopedia
Apabetalone (development codes RVX 208, RVX-208, and RVX000222)[1] is an orally available small molecule created by Resverlogix Corp.[2] that is being evaluated in clinical trials for the treatment of atherosclerosis and associated cardiovascular disease (CVD).[3][4] In the phase II clinical trial ASSURE in patients with angiographic coronary disease and low high-density lipoprotein cholesterol (HDL-C) levels, apabetalone showed no greater increase in HDL-cholesterol (HDL-c) and apolipoprotein A-I (ApoA-I) levels or incremental regression of atherosclerosis than administration of placebo, while causing a statistically significant greater incidence of elevated liver enzymes.[5] However, pooled analysis of the effect of apabetalone in three phase II clinical trials ASSERT, ASSURE, and SUSTAIN demonstrated increases in HDL-cholesterol (HDL-c) and apolipoprotein A-I (ApoA-I) levels, as well as decreases in the incidence of major adverse cardiac events (MACE).[6] Reduction of MACE was more profound in patients with diabetes mellitus. In a short-term study in prediabetics, favorable changes in glucose metabolism were observed in patients receiving apabetalone.[7] An international, multicenter phase III trial, “Effect of RVX000222 on Time to Major Adverse Cardiovascular Events in High-Risk Type 2 Diabetes Mellitus Subjects with Coronary Artery Disease” (BETonMACE) commenced in October 2015.[8] The trial is designed to determine whether apabetalone in combination with statins can decrease cardiac events compared to treatment with statins alone.
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Names | |
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IUPAC name
2-[4-(2-Hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-4(3H)-quinazolinone | |
Other names
RVX208, RVX-208 | |
Identifiers | |
3D model (JSmol) |
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ChEMBL | |
ChemSpider | |
DrugBank | |
ECHA InfoCard | 100.242.963 ![]() |
EC Number |
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KEGG | |
PubChem CID |
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UNII | |
CompTox Dashboard (EPA) |
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Properties | |
C20H22N2O5 | |
Molar mass | 370.405 g·mol−1 |
Density | 1.3±0.1 g/cm3 |
Hazards | |
GHS labelling: | |
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Warning | |
H371 | |
P260, P264, P270, P309+P311, P405, P501 | |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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