apabetalone
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
Clinical trial activity
14 trials · 15 clinical orgs · 0 marketing orgs
Earliest trial started Sep 1, 2008 (NCT00768274)
Timeline
Indications
Studied for
- Acute Coronary Syndrome · Phase 1/Phase 2
- Atherosclerosis · Phase 2
- Cardiovascular Diseases · Phase 1/Phase 2
- Coronary Artery Disease · Phase 3
- COVID-19 · Phase 2/Phase 3
- Diabetes Mellitus · Phase 2
- Diabetes Mellitus, Type 2 · Phase 3
- Dyslipidemias · Phase 2
- Fabry Disease · Phase 1/Phase 2
- Irritable Bowel Syndrome · Phase 2
- Kidney Failure, Chronic · Phase 1/Phase 2
- Pulmonary Arterial Hypertension · Phase 2
Mechanism of action
- Bromodomain-containing protein 7INHIBITOR
BRD7 inhibitor
Bromodomain and extra-terminal motif (BET) inhibitor
Chemistry & pharmacology
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
- ChEMBLCHEMBL2393130 ↗
- WikipediaApabetalone ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06590324 | Phase 2/Phase 3 (Phase 3) | Nov 30, 2024 | Resverlogix Corp |
| NCT04915300 | Phase 2 | Dec 31, 2021 | Canadian Institutes of Health Research (CIHR), Laval University, Resverlogix Corp |
| NCT04894266 | Phase 2/Phase 3 (Phase 3) | Nov 1, 2021 | Resverlogix Corp |
| NCT03228940 | Phase 1/Phase 2 (Phase 2) | Jan 31, 2019 | Queen Elizabeth Hospital NHS Foundation Trust, Resverlogix Corp |
| NCT03655704 | Early Phase 1 (Phase 1) | Nov 30, 2018 | Laval University |
| NCT03160430 | Phase 1/Phase 2 (Phase 2) | Jun 15, 2017 | Resverlogix Corp |
| NCT02586155 | Phase 3 | Oct 1, 2015 | ICON, Medidata Solutions, PPD, Resverlogix Corp, University of London |
| NCT01863225 | Phase 2 | May 1, 2013 | Resverlogix Corp, South Australian Health and Medical Research Institute, University of Adelaide |
| NCT01728467 | Phase 2 | Nov 1, 2012 | Monash University, Nucleus Network Ltd, Resverlogix Corp |
| NCT01067820 | Phase 2 | Sep 1, 2011 | Resverlogix Corp, University of Rochester |
| NCT01423188 | Phase 2 | Aug 1, 2011 | Resverlogix Corp, University of Rochester |
| NCT01076699 | Phase 2 | Mar 1, 2010 | Metropolitan Gastroenterology Group PC, Chevy Chase Clinical Research, Revogenex, Inc. |
| NCT01058018 | Phase 2 | Dec 1, 2009 | Resverlogix Corp, University of Rochester |
| NCT00768274 | Phase 1/Phase 2 (Phase 2) | Sep 1, 2008 | Resverlogix Corp |
Organizations
Research & Development (15)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Resverlogix Corp | For profit | 12 | 11 | 2 | 2008 |
| University of Rochester | Academic/Hospital | 3 | 0 | 1 | 2009 |
| Laval University | Academic/Hospital | 2 | 2 | 2 | 2018 |
| Canadian Institutes of Health Research (CIHR) | Academic/Hospital | 1 | 0 | 1 | 2021 |
| ICON | For profit | 1 | 0 | 1 | 2015 |
| Medidata Solutions | For profit | 1 | 0 | 1 | 2015 |
| Metropolitan Gastroenterology Group PC, Chevy Chase Clinical Research | Academic/Hospital | 1 | 0 | 1 | 2010 |
| Monash University | Academic/Hospital | 1 | 0 | 1 | 2012 |
| Nucleus Network Ltd | For profit | 1 | 0 | 1 | 2012 |
| PPD | For profit | 1 | 0 | 1 | 2015 |
| Queen Elizabeth Hospital NHS Foundation Trust | Academic/Hospital | 1 | 0 | 1 | 2019 |
| Revogenex, Inc. | For profit | 1 | 1 | 1 | 2010 |
| South Australian Health and Medical Research Institute | Academic/Hospital | 1 | 0 | 1 | 2013 |
| University of Adelaide | Academic/Hospital | 1 | 0 | 1 | 2013 |
| University of London | Academic/Hospital | 1 | 0 | 1 | 2015 |