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Apabetalone - BET protein inhibition in cardiovascular disease and Type 2 diabetes

Julia Brandts1,2, Kausik K Ray2

  • 1Department of Medicine I, University Hospital RWTH Aachen, Aachen, Germany.

Future Cardiology
|May 8, 2020
PubMed

Insights

Apabetalone, a BET protein inhibitor, showed potential in cardiovascular diseases (CVD) by modulating risk factors. However, the BET-on-MACE trial did not confirm a significant reduction in major adverse cardiac events (MACE) for Type 2 diabetes patients post-acute coronary syndrome.

Area of Science:

  • Pharmacology
  • Epigenetics
  • Cardiovascular Medicine

Background:

  • BET proteins are epigenetic regulators crucial for gene expression.
  • Apabetalone is a selective BET protein inhibitor targeting cardiovascular diseases (CVD).
  • Previous analyses suggested apabetalone may reduce CVD risk markers and plaque vulnerability.

Purpose of the Study:

  • To evaluate the efficacy of apabetalone in reducing major adverse cardiac events (MACE) in patients with Type 2 diabetes (T2D) and stable CVD.
  • To investigate the impact of apabetalone on cardiovascular outcomes in T2D patients following an acute coronary syndrome.

Main Methods:

  • Apabetalone's effects on reverse cholesterol transport, coagulation, inflammation, and vascular calcification were studied.
  • Post-hoc pooled analyses of existing data were conducted.
  • The BET-on-MACE cardiovascular outcomes trial assessed MACE reduction in T2D patients post-acute coronary syndrome.

Main Results:

  • Apabetalone demonstrated modulation of key CVD pathways including cholesterol transport and inflammation.
  • Circulating markers of CVD risk and plaque vulnerability were reduced by apabetalone.
  • The BET-on-MACE trial did not meet its primary endpoint, failing to show a 30% reduction in MACE.

Conclusions:

  • While apabetalone influences CVD-related biological processes, the BET-on-MACE trial did not confirm its efficacy in reducing MACE in T2D patients after acute coronary syndrome.
  • Further research may be needed to clarify apabetalone's role in specific cardiovascular patient populations.
Keywords:
BET protein inhibitionHDL-cholesterolMACEapabetaloneatherosclerosiscardiovascular diseaseepigenetic regulationmixed dyslipidemiatype 2 diabetes

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