HDL mimetic CER-001 targets atherosclerotic plaques in patients

Abstract Background and aims Infusion of high-density lipoprotein (HDL) mimetics aimed at reducing atherosclerotic burden has led to equivocal results, which may relate in part to the inability of HDL mimetics to adequately reach atherosclerotic lesions in humans. This study evaluated delivery of recombinant human apolipoprotein A-I (apoA-I) containing HDL mimetic CER-001 in carotid plaques in patients. Methods CER-001 was radiolabeled with the long-lived positron emitter zirconium-89 (89 Zr) to enable positron emission tomography with computed tomography (PET/CT) imaging. Eight patients with atherosclerotic carotid artery disease (>50% stenosis) received a single infusion of unlabeled CER-001 (3 mg/kg), co-administered with 10 mg of89 Zr-labeled CER-001 (18 MBq). Serial PET/CT imaging and contrast enhanced-magnetic resonance imaging (CE-MRI) were performed to evaluate targeted delivery of CER-001. Results One hour after infusion, mean plasma apoA-I levels increased by 9.9 mg/dL ( p = 0.026), with a concomitant relative increase in the plasma cholesterol efflux capacity of 13.8% ( p