apabetalone

Small moleculeexperimental

Apabetalone is an orally available small molecule created by Resverlogix Corp. that is being evaluated in clinical trials for the treatment of atherosclerosis and associated cardiovascular disease (CVD). 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. 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). 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. 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. The trial is designed to determine whether apabetalone in combination with statins can decrease cardiac events compared to treatment with statins alone. — Wikipedia

Chemistry & pharmacology

Loading structure…

SMILES

COc1cc(OC)c2c(=O)[nH]c(-c3cc(C)c(OCCO)c(C)c3)nc2c1
Mol. weight
370.41 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3h)-one
  • apabetalone
  • apabetalone
  • apabetalone
  • rvx000222
  • rvx000222
  • rvx000222
  • rvx 000222
  • rvx-000222
  • rvx-100
  • rvx208
  • rvx 208
  • rvx-208

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06590324Phase 2/Phase 3 (Phase 3)Nov 30, 2024Resverlogix Corp
NCT04915300Phase 2Dec 31, 2021Canadian Institutes of Health Research (CIHR), Laval University, Resverlogix Corp
NCT04894266Phase 2/Phase 3 (Phase 3)Nov 1, 2021Resverlogix Corp
NCT03228940Phase 1/Phase 2 (Phase 2)Jan 31, 2019Queen Elizabeth Hospital NHS Foundation Trust, Resverlogix Corp
NCT03655704Early Phase 1 (Phase 1)Nov 30, 2018Laval University
NCT03160430Phase 1/Phase 2 (Phase 2)Jun 15, 2017Resverlogix Corp
NCT02586155Phase 3Oct 1, 2015ICON, Medidata Solutions, PPD, Resverlogix Corp, University of London
NCT01863225Phase 2May 1, 2013Resverlogix Corp, South Australian Health and Medical Research Institute, University of Adelaide
NCT01728467Phase 2Nov 1, 2012Monash University, Nucleus Network Ltd, Resverlogix Corp
NCT01067820Phase 2Sep 1, 2011Resverlogix Corp, University of Rochester
NCT01423188Phase 2Aug 1, 2011Resverlogix Corp, University of Rochester
NCT01076699Phase 2Mar 1, 2010Metropolitan Gastroenterology Group PC, Chevy Chase Clinical Research, Revogenex, Inc.
NCT01058018Phase 2Dec 1, 2009Resverlogix Corp, University of Rochester
NCT00768274Phase 1/Phase 2 (Phase 2)Sep 1, 2008Resverlogix Corp
Showing 14 of 14 trials
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Organizations

Research & Development (15)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Resverlogix CorpFor profit121122008
University of RochesterAcademic/Hospital3012009
Laval UniversityAcademic/Hospital2222018
Canadian Institutes of Health Research (CIHR)Academic/Hospital1012021
ICONFor profit1012015
Medidata SolutionsFor profit1012015
Metropolitan Gastroenterology Group PC, Chevy Chase Clinical ResearchAcademic/Hospital1012010
Monash UniversityAcademic/Hospital1012012
Nucleus Network LtdFor profit1012012
PPDFor profit1012015
Queen Elizabeth Hospital NHS Foundation TrustAcademic/Hospital1012019
Revogenex, Inc.For profit1112010
South Australian Health and Medical Research InstituteAcademic/Hospital1012013
University of AdelaideAcademic/Hospital1012013
University of LondonAcademic/Hospital1012015
15 organizations
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