Epigenetic Drug Improves Cholesterol Levels

Results from a Phase II trial for cardiovascular disease with an epigenetic target therapy show promise.

By Edyta Zielinska | August 28, 2012

Nephron" > Atherosclerotic plaqueWikimedia, Nephron

A drug that targets epigenetic proteins, aimed at boosting so-called “good” cholesterol levels, showed positive signs in Phase II clinical trial, its maker Resverlogix Corporation announced yesterday (August 28).

The therapy is intended to improve upon statins, which reduce the levels of “bad” cholesterol, or low density lipoprotein (LDL), but do not increase the levels of the beneficial high density lipoprotein (HDL). Trial results showed that the drug RVX-208 from Resverlogix was able to increase HDL levels in treated patients. Pfizer’s torcetrapib also attempted to increase HDL levels, but that compound failed in Phase III trials, when treated patients died from heart disease more frequently than untreated patients, according to Nature.

Resverlogix’s drug targets bromodomain proteins, which detect epigenetic modifications on histone proteins and recruits additional proteins to the site. As a result, the cells produce more Apo-A1, the main component of HDL, which helps remove atherosclerotic plaques already formed.  “We think our drug will reverse the plaque buildup that causes hundreds of thousands of deaths each year,” Donald McCaffrey, the president of Resverlogix told Nature.

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Avatar of: James Kohl

James Kohl

Posts: 53

August 29, 2012

Isn't the diet-responsive and presumably exercise-responsive
hypothalamic neurogenic niche most likely to be involved in the cause
and effect regulation of HDL via nutrient chemical-dependent epigenetic
effects on gonadotropin releasing hormone? If so, the epigenetic "tweaking" of immense gene networks
that solve problems through the exchange and the selective cancellation
and modification of signals will almost no doubt be accompanied by
unanticipated side effects that could be more important health
considerations than raising HDL.

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