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.