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Diabetes and hyperlipidemia are global epidemics that significantly increase the morbidity and mortality of the affected population. Several medications have been utilized to mitigate the risk of diabetes and hyperlipidemia. Insulin, alpha-glucosidase inhibitors, thiazolidinediones have been used for decades as antidiabetic medications. Statins are a cornerstone in hyperlipidemia management. Omega‐3 fatty acid supplementation has been used to treat hypertriglyceridemia with debatable effects on cardiovascular outcomes. In the past decade, multiple new discoveries have revolutionized the management of these disorders. Sodium–glucose cotransporter 2 (SGLT2) inhibitors are a class of oral anti-diabetic drugs with a unique mechanism of action. SGLT2 was proven to reduce cardiovascular events, including hospitalization for heart failure, with this benefit extending to patients without diabetes. PCSK9 inhibitors are a new class of antihyperlipidemic that significantly lowers plasma LDL-C on top of the conventional treatment. In this book chapter, we review the history of diabetes and hyperlipidemia medications and discuss the new classes of lipid-lowering and anti-diabetic medications and their associated cardioprotective benefits.