In order to comprehensively address atherosclerotic risk, the need to achieve and maintain very low LDL-cholesterol levels and manage other atherogenic factors has led to the development of new therapeutic options. This review reports the main agents in an advanced status of development that have LDL-cholesterol, triglycerides, lipoprotein(a), inflammation, and body weight as therapeutic targets. We discuss the mechanism of action, biological effects, and safety profile of these new drugs (bempedoic acid, lomitapide, inclisiran, evinacumab, vupanorsen, mipomersen, eicosapent ethyl, volanesorsen, pemafibrate, AKCEA-APO(a)-LRx, colchicine, semaglutide). Lastly, we briefly report therapeutic interventions based on biotechnological methods that could be implemented in the near future.