Apabetalone

Apabetalone is the world leader in a new class of drugs designed to regulate disease-associated proteins.

Traditional therapeutics target a single, disease-causing factor, hoping for a single outcome. By inhibiting the action of bromodomain and extraterminal domain (BET) proteins, apabetalone positively affects multiple disease-causing biological processes – leading a new paradigm shift in the treatment of chronic disease.

Apabetalone has a unique mechanism of action, working at the level of “transcription” as shown in the illustration below. As a selective inhibitor of the BET family of proteins, apabetalone has the ability to normalize dysregulated epigenetics that lie at the heart of many chronic diseases.

When you are sick, BET proteins may act on DNA to turn up gene expression instructing the cell to make proteins that contribute to disease. Apabetalone blocks the action of BET proteins, bringing the increased production of dysregulated proteins back down to healthier levels.

It is important to think about how changes in cell activity add up to broader effects in a whole person. Cells communicate with nearby neighbours and with distant cells of various types. When disease perpetuating messages between cells, cell networks, pathways and organs are blocked with apabetalone, it results in greater overall health and well-being.

Proof in the Data

From data collected in our clinical trials, we now know that apabetalone – through its effects on epigenetics – benefits multiple processes which contribute to the onset and worsening of disease. This is consistent with observed reductions in major adverse cardiac events (MACE) in study participants. Patients who take apabetalone have fewer heart attacks, strokes and cardiac-related deaths. Our data has also shown that a whole host of proteins associated with chronic kidney disease are normalized after treatment with apabetalone.

The following diagram describes the overlapping, biological processes underlying the development of cardiovascular disease and how apabetalone and the inhibition of BET proteins can reduce the incidence of MACE.

A Bright Future

As apabetalone can be administered as a twice daily tablet, it will be affordable and easy to take for all our patients. Most importantly, apabetalone has proven to be safe. Due to its unique epigenetic mechanism, we continue to discover more ways that apabetalone can benefit patients across a broader range of chronic diseases, including neurodegenerative diseases, peripheral artery disease and a number of rare diseases.