Metabolic dysfunction-associated steatotic liver disease (MASLD) affects an ever-increasing part of the global population, affecting millions of individuals worldwide. Despite the progress in the treatment of other liver diseases, there is a scarcity of liver-specific drugs targeting MASLD. In light of that, research has focused both on pipeline drugs targeting multiple different receptors implicated in the pathogenesis of the disease, as well as medications already approved for other indications, that might exert beneficial effects on MASLD. The fact that MASLD is associated with an increased prevalence of obesity and type 2 diabetes mellitus (T2DM) establishes a possible pathway with respect to already available pharmaceutical interventions for this group of patients, such as glucagon-like peptide-1 receptor agonists (GLP-1RAs) and sodium-glucose co-transporter-2 inhibitors (SGLT2-is). Thus, the hitherto at hand, along with the upcoming members of these families, provide much-needed options for our arsenal. This review attempts to explore old and novel dimensions of the pharmaceutical treatment of MASLD in the continuous effort of the medical society to improve patient outcomes.