The pharmacological targets of current or potential lipid-lowering agents for dyslipidemia therapy. ACL, ATP-citrate lyase; ANGPTL3, angiopoietin-like protein 3, Apo(a), Apolipoprotein(a); ApoC-III, Apolipoprotein C-III; ASO, antisense oligonucleotides; CM, chylomicrons; HDL, high-density lipoproteins; HMG-CoA, 3-hydroxy-3-methyl-glutaryl-coenzyme A; HMGCR, 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase; IDL, intermediate-density lipoprotein; LDL, low-density lipoproteins; LDLR, low-density lipoprotein receptor; LPL, lipoprotein lipase; Lp(a), lipoprotein (a); NPC1L1, Niemann-Pick C1-like 1 protein; PCSK9, proprotein convertase subtilisin/kexin type 9; VLDL, very-low-density lipoproteins. The approaches for inhibition of targets in lipid/lipoprotein metabolism are highlighted in the boxes (created with BioRender.com, accessed on 2 July 2021).