Drug intelligence / Profile preview

bempedoic acid + ezetimibe + rosuvastatin

Development stage
Phase 1
Lead developer
Daiichi Sankyo
Modality
Small Molecules
Administration
Oral
01

Overview

Bempedoic acid/ezetimibe/rosuvastatin is an oral fixed-dose triple combination therapy developed by Daiichi Sankyo for the treatment of hypercholesterolemia and mixed dyslipidemia. This combination leverages three distinct, complementary mechanisms to lower LDL cholesterol: bempedoic acid inhibits ATP citrate lyase upstream of the statin pathway; ezetimibe inhibits the NPC1L1 transporter to reduce intestinal cholesterol absorption; and rosuvastatin inhibits HMG-CoA reductase to decrease hepatic cholesterol synthesis. The formulation is primarily intended for patients with primary hypercholesterolemia or mixed dyslipidemia who require intensive LDL-C lowering beyond what is achievable with dual therapy or standard statin regimens. It is currently being evaluated in Phase 1 bioequivalence studies comparing the fixed-dose combination tablet against the co-administration of its individual reference components.

Other names
bempedoic acid/ezetimibe/rosuvastatin FDCbempedoic acid + ezetimibe + rosuvastatin fixed-dose combination
02

Targets

ACLY (ATP-citrate synthase)OATP1B1 (Organic anion transporting polypeptide 1B1)SLCO1B3 (Organic anion transporting polypeptide 1B3)NPC1L1 (Niemann-pick C1-Like 1 transporter)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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