This systematic review further analyzes the pharmacological actions of novel lipid-lowering agents such as adenosine triphosphate-citrate lyase inhibitors (ACLi), selective peroxisome proliferator-activated receptor alpha (PPARα) modulators, cholesteryl ester transfer protein inhibitors (CETPi), antisense oligonucleotides (ASO), and angiopoietin-like protein 3 inhibitors (ANGPTL3i) as well as their efficacy in treating dyslipidemia while sparing the user of potentially severe side effects. Here, CETP is linked to metabolic syndrome.