Table 1.

Pre-clinical studies of the main ACAT inhibitors for atherosclerosis.

Name	Animal	Plasma Cholesterol	Atherosclerotic Lesion Effect	Other Effects	Reference
F-1394	Rats	↓	N.D.	↓ cholesterol absorption	[31]
	Apoe−/− ldlr−/− mice	N.S.	↓		[32]
	Rabbits (balloon injury)	N.S.	N.D.	↓ neointimal thickening	[33]
	Apoe−/− mice	↓	↓		[34]
	Apoe−/− mice	N.S.	↓ progression	↓ lesion tissue factor	[35]
	Apoe−/− mice	N.S.	N.S.		[36]
	Apoe−/− and human APO A1-transgenic mice	N.S.	N.S.		[36]
CI-1011 (avasimibe)	Male monkeys	↓	N.D.	↓ Lp(a)	[37]
	Miniature pigs	↓	N.D.		[38]
	Male rabbits	N.S.	↓ progression	↓ lesion MMP expression	[39]
	Beagle dogs	N.D.	N.D.	↑ Emesis, saliva, hepatic toxicity,	[40]
	ApoE *3-Leiden mice	↓	↓		[41]
	Miniature pigs	↓	N.D.		[42]
	Apoe−/− mice	↓	↓ progression		[43]
	Rabbits	N.D.	↓ progression		[44]
CS-505 (pactimibe sulfate)	Apoe−/− mice	↓	↓ progression	↓ MMP expression	[43]
	Rabbits	N.S.	N.S.	↑ lesion fibers and smooth muscle cells	[45]
	Hamsters	↓	↓		[46]
	Hamsters	↓	N.D.	↓ hepatic lipids; ↓ lipid absorption; ↑ fecal lipid excretion	[47]
	Monkeys	↓	N.D.		[47]
	Diabetic rats	N.D.	N.D.	↓ postprandial fat loading	[47]
	Apoe−/− mice	↓	↓		[48]
CI-976	Rabbits	N.S.	↓ progression		[49]
	Hamsters	↓	N.D.		[50]
	Rats	↓	N.D.	↓ liver CE	[51]
	Micropigs	N.S.	N.D.	↓ liver CE	[52]
	Endogenous hypercholesterolemia rabbits	↓	N.D.		[53]
	Rabbits	↓	↓		[54]
	Nephrotic syndrome (NS) rats	↓	N.D.	restore LDL and HDL receptors	[55]
K-604 (ACAT-1 selective)	Hamsters	↓ (at high dose)	↓		[56]
	Apoe−/− mice	↓ (at high dose)	N.S.	↑ lesion collagen	[48]
PD 132301-2	Rats	↓	N.D.		[57]
	Guinea pigs	↓	N.D.		[57]
	Rabbits	↓	N.D.		[57]
CL 277,082	Rats	↓	N.D.		[57]
	Guinea pigs	↓ (at high dose)	N.D.		[57]
	Rabbits	↓	N.D.		[57]
	Rats	↓	N.D.		[51]

N.D., not determined; N.S., not significantly different; MMP, matrix metalloproteinases.