BET bromodomain inhibition is an epigenetic mechanism that can turn disease-causing genes off, returning them to a healthier state. BET inhibitors selective for BRD4-BD2 are currently tested in clinical trials with potentially important benefits for patients with diseases such as cardiovascular disease, diabetes mellitus, chronic kidney disease, peripheral artery disease.
AHA 2016 The orally active epigenetic drug RVX-208 or apabetalone that alters gene activity by modifying chromatin structure, lowered the incidence of MACE in a phase 2b study. This effect could not entirely be attributed to an effect on HDL, explains dr. Norman Wong.
A Meeting Impression from a EBAC accredited satellite symposium held at ESC 2016 in Rome that explored a novel approach to reduce residual CV risk, namely BET inhibition
At the 'A novel approach for high cv risk patients with diabetes: the potential of epigenetics' symposium, held at the ESC Congress 2016 in Rome, Kausik Ray spoke about therapeutic targets to further lower CV risk.
At the 'A novel approach for high cv risk patients with diabetes: the potential of epigenetics' symposium, held at the ESC Congress 2016 in Rome, Jorge Plutzky spoke about BET inhibition as a nover pathway for CV risk reduction.
RVX-208 affected HDL lipid composition and HDL particle size distribution and modulated glucose metabolism in prediabetic individuals.
RVX-208 is an investigational BET bromodomain inhibitor that upregulates apoA-I gene transcription, leading to increased HDL-levels and larger HDL particles. This review summarises currently available data.