Physicians' Academy for Cardiovascular Education

BET inhibitor downregulates components of complement cascade

Downregulation of the Complement Cascade In Vitro, in Mice and in Patients with Cardiovascular Disease by the BET Protein Inhibitor Apabetalone (RVX-208)

Literature - Wasiak S, Gilham D, Tsujikawa LM, et al. - J. of Cardiovasc. Trans. Res. 2017, In press

Main results

In vitro experiments

In vivo experiments

Patient plasma protein expression


BET inhibitor RVX-208 shows a repressive effect on expression of multiple complement cascade components and regulators. As these effects were also observed with a different BET inhibitor, JQ1, this seems to be BET inhibitor-specific rather than RVX-208-specific. This was also observed when complement was induced upon cytokine treatment. In vitro and in vivo experiments were confirmed with CAD patient analyses, which showed a reduction in circulating levels of multiple complement components and regulators with RVX-208, versus placebo. Thus, in addition to improving the lipoprotein and inflammatory profile, RVX-208 may benefit CVD patients by modulating the complement cascade.


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Find this article online at Journal of Cardiovascular Translational Research

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