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Probucol has a long history of clinical application with established efficacy and
safety profiles. Probucol is a potent anti-oxidant drug that has been in clinical
use during the past few decades for the treatment and prevention of cardiovascular
diseases. Here we review the current status of knowledge on the pharmacology, clinical
benefits, and the mechanism of actions of this unique drug. Probucol has diverse pharmacological
properties with therapeutic effects on the cardiovascular systems. Its mechanism of
pharmacologic actions at the molecular level has recently been elucidated with the
new concept of HDL metabolism associated with cholesteryl ester transfer protein (CETP)
or scavenger receptor class B type I (SR-BI). HDL-C reduction may not be a "side effect"
but it most likely might reflect a mechanism of action of probucol. Probucol could
be reconsidered as an option at least in case statins, which are known to be effective
in lowering low-density lipoproteins (LDL) and coronary artery disease (CAD) risk,
are not effective. In particular, a marked CAD risk reduction has been recently reported
in long-term probucol treatment of patients with heterozygous familial hypercholesterolemia
(FH) in Japan. Therefore, probucol could be a more common therapeutic drug for the
treatment of patients with FH as well. There is more than enough reason to believe
that this old drug has much more to offer than hitherto known.