HDL, Atherosclerosis, and Emerging Therapies

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 Strategy	Drug	Aim	Figure 1
Recombinant apoA-I Milano/phospholipids	ETC-216	Directly augmenting apoA-I/HDL pool	1
Purified native apoA-I/phospholipids	CSL-111; CSL-112	Directly augmenting apoA-I/HDL pool	2
Upregulators of endogenous apoA-I production	RVX-208	Directly augmenting apoA-I/HDL pool	3
ApoA-I mimetic peptides	D-4F; L-4F; 6F, 5A; ATI-5261	Mimicking apoA-I functionality	4
Autologous Delipidated HDL	Selective HDL delipidated	Directly augmenting apoA-I/HDL pool	5
Gene therapy	miR-33	Modulating HDL levels and cholesterol efflux expression	6
Liver X receptor agonists	LXRα/β agonists; LxR-623; T0901317, GW3965; ATI-111	Enhancing RCT & Macrophage cholesterol efflux	7
Niacin receptor agonists	ARI-3037MO	Indirectly augmenting apoA-I and HDL-cholesterol	8
Farnesoid X receptor	FxR-450	Modulate HDL levels	9
Cholesteryl ester transfer inhibitors	Anacetrapib MK-0859Evacetrapib LY248595	Indirectly augmenting apoA-I and HDL-cholesterol	10
Endothelial lipase inhibition	Boronic acid inhibitors; Selective sulfonylfuran urea	Increasing HDL-cholesterol	11
LCAT activators	rLCAT; ETC-642	Enhancing RCT	12