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Apabetalone (RVX-208) reduces vascular inflammation in vitro and in CVD patients by a BET-dependent epigenetic mechanism.

Laura M TsujikawaLi FuShovon DasChristopher HallidayBrooke D RakaiStephanie C StotzChristopher D SarsonsDean GilhamEmily DazeSylwia WasiakDeborah StuderKristina D RinkerMichael SweeneyJan O JohanssonNorman C W WongEwelina Kulikowski
Published in: Clinical epigenetics (2019)
Apabetalone suppressed gene expression of VI mediators in monocytes and endothelial cells by inhibiting BET-dependent transcription induced by multiple inflammatory stimuli. In CVD patients, apabetalone treatment reduced circulating levels of VI mediators, an outcome conducive with atherosclerotic plaque stabilization and MACE reduction. Inhibition of inflammatory and adhesion molecule gene expression by apabetalone is predicted to contribute to MACE reduction in the phase III BETonMACE trial.
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