The class
Clinician's overview names CETP inhibitors the most potent HDL-raising drugs, but torcetrapib fell to excess cardiovascular harm (Angiology 2009)
Original title: High-density lipoprotein cholesterol: current perspective for clinicians
This clinician-focused overview of HDL cholesterol discusses situations where high HDL is not necessarily protective and reviews available medications. Nicotinic acid is described as the best available agent for raising HDL cholesterol, with cardiovascular benefit, though flushing intolerance limits its use, a problem laropiprant reduces and for which it had European but not US approval. The review identifies CETP inhibitors as the most potent HDL-raising medications available, noting that the first in class, torcetrapib, was eliminated from development due to excess cardiovascular problems, while two newer CETP inhibitors, R1658 (dalcetrapib) and anacetrapib, initially appeared promising, with HDL cholesterol potentially playing an important role in improving cardiovascular risk for the roughly 60% of patients who see no cardiovascular mortality or morbidity benefit from LDL-lowering statin therapy alone.
Original abstract
High-density lipoproteins are regarded as ''good guys'' but not always. Situations involving high-density lipoproteins are discussed and medication results are considered. Clinicians usually consider high-density lipoprotein cholesterol. Nicotinic acid is the best available medication to elevate high-density lipoprotein cholesterol and this appears beneficial for cardiovascular risk. The major problem with nicotinic acid is that many patients do not tolerate the associated flushing. Laropiprant decreases this flushing and has an approval in Europe but not in the United States. The most potent medications for increasing high-density lipoprotein cholesterol are cholesteryl ester transfer protein inhibitors. The initial drug in this class, torcetrapib, was eliminated by excess cardiovascular problems. Two newer cholesteryl ester transfer protein inhibitors, R1658 and anacetrapib, initially appear promising. High-density lipoprotein cholesterol may play an important role in improving cardiovascular risk in the 60% of patients who do not receive cardiovascular mortality/morbidity benefit from low-density lipoproteins reduction by statins.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.