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. Author manuscript; available in PMC: 2022 Jun 8.
Published in final edited form as: Circulation. 2021 Jun 7;143(23):2293–2309. doi: 10.1161/CIRCULATIONAHA.120.044221

Table 3 –

Drugs affecting HDL Metabolism

Drugs % HDL-C Elevation Mechanism of Action Stage of Development
Niacin 30-50 Multifactorial effects Approved
Fibrates
(Fenofibrate)
5-15 Multifactorial effects by acting as PPAR agonists Approved
CETP- Inhibitors
(Anacetrapib, Dalcetrapib)
25-135 Inhibit transfer of cholesteryl esters away from HDL Phase III
(completed)
BET Inhibitor
(Apabetalone)
5-10 Epigenetic modification altering apoA-I transcription Phase III
(completed)
HDL Infusion Therapy
(CSL-112)
50-200 Direct infusion of exogenous HDL Ongoing Phase III
(AEGIS-II: NCT03473223)
Recombinant LCAT
(MEDI6012)
50-100 Increase esterification of cholesterol on HDL Ongoing Phase II
((REAL-TIMI 63B: NCT03578809))

HDL=high density lipoprotein; PPAR=peroxisome proliferator-activated receptor; CETP=cholesteryl ester transfer protein; BET=bromodomain and extraterminal; apoA-I=apolipoprotein A-I; AEGIS=ApoA-I Event reducing in Ischemic Syndromes; LCAT=lecithin-cholesterol acyltransferase;