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. Author manuscript; available in PMC: 2014 Nov 14.
Published in final edited form as: Circulation. 2013 Jul 2;128(1):72–78. doi: 10.1161/CIRCULATIONAHA.112.000443

Table. Emerging Therapeutic Approaches for Treating Low HDL-C.

Therapeutic Strategy Rationale
CETP inhibition Increase HDL-C by inhibiting transfer of cholesteryl esters from HDL-C to Apo-B–containing particles.
Apo A-I/reconstituted HDL infusion Promote reverse cholesterol transport and stabilize atherosclerotic plaque
Apo A-I mimetic peptides/ upregulators of Apo A-I production Seek to mimic pleiotropic beneficial effects of Apo A-I
LXR agonism/ inhibition of microRNA MiR-33 Upregulate transporters involved in efflux of cholesterol from macrophages, promoting reverse cholesterol transport
Dual PPARα/PPARγ agonism Combines PPARα effect of fibrates on lipid metabolism with PPARγ effect on improved insulin resistance

Examples of strategies for increasing levels of HDL or its components, and the rationale for these approaches are provided.

Apo indicates apolipoprotein; CETP, cholesteryl ester transfer protein; HDL, highdensity lipoprotein; HDL-C, high-density lipoprotein cholesterol; LXR, liver X receptor; PPARα, peroxisome proliferator-activated receptor alpha; and PPARγ, peroxisome proliferator-activated receptor gamma.