Table 3: Summary of selected strategies to increase HDL/apoA-I and potential compound under development. Numbers in the right hand column refer to Figure 1.

Pharmacotherapeutic StrategyDrugAimFigure 1

Recombinant apoA-I Milano/phospholipidsETC-216Directly augmenting apoA-I/HDL pool1
Purified native apoA-I/phospholipidsCSL-111
CSL-112
Directly augmenting apoA-I/HDL pool2
Upregulators of endogenous apoA-I productionRVX-208Directly augmenting apoA-I/HDL pool3
ApoA-I mimetic peptidesD-4F
L-4F
6F, 5A
ATI-5261
Mimicking apoA-I functionality
4
Autologous Delipidated HDLSelective HDL delipidatedDirectly augmenting apoA-I/HDL pool5
Gene therapymiR-33Modulating HDL levels and cholesterol efflux expression6
Liver X receptor agonistsLXRα/β agonists
LxR-623
T0901317, GW3965
ATI-111
Enhancing RCT & Macrophage cholesterol efflux7
Niacin receptor agonistsARI-3037MOIndirectly augmenting apoA-I and HDL-cholesterol8
Farnesoid X receptorFxR-450Modulate HDL levels9
Cholesteryl ester transfer inhibitorsAnacetrapib MK-0859Evacetrapib LY248595Indirectly augmenting apoA-I and HDL-cholesterol10
Endothelial lipase inhibitionBoronic acid inhibitors
Selective sulfonylfuran urea
Increasing HDL-cholesterol11
LCAT activatorsrLCAT
ETC-642
Enhancing RCT12