Anacetrapib as a potential cardioprotective strategy

Figures & data

Table 1 Properties of CETP inhibitors that have proceeded to advanced stages of clinical development

Parameter	Torcetrapib	Dalcetrapib	Evacetrapib	Anacetrapib	TA-8995
Molecular weight (Da)	600.4	389.6	638.6	673.5	722.6
Adipose tissue accumulation	None	None	None	Demonstrated with terminal half-life >1 year	None
HDL-C	+70%	+30%	+125%	+130%	>+76%
LDL-C	−20%	0%	−25%	−25%	>−27%
Cholesterol efflux	Increase	Increase	Increase	Increase	Increase
Blood pressure	3–6 mmHg increase	No effect	No effect	No effect	No effect
Clinical outcomes	Adverse effects on mortality and CV events	Clinical futility	Clinical futility	9% reduction in CV events	Unknown

Abbreviations: CETP, cholesteryl ester transfer protein; HDL-C, high-density lipoprotein cholesterol; LDL-C, low-density lipoprotein cholesterol; CV, cardiovascular.