Magnetic mesoporous silica nanoparticles (MMS NPs) stand out as excellent options for targeted chemotherapy owing to their remarkable features, such as extensive surface area, substantial pore volume, adjustable and uniform pore size, facile scalability, and versatile surface chemistry. This review comprehensively explores the latest developments in MMS NPs, emphasizing their design, functionalization, and application in cancer therapy. Initially, we discuss the critical need for targeted and controlled drug delivery (DD) in oncology, highlighting the role of magnetic and MMs in addressing some challenges. Subsequently, the key features of MMS NPs, such as their high surface area, pore structure, and functionalization strategies, are examined for their impact on their DD performance for efficient cancer chemotherapy. The integration of chemotherapy methods such as photothermal therapy and photodynamic therapy with MMS NPs is also explored, showcasing multifunctional platforms that combine imaging and therapeutic capabilities. Finally, we identify the current challenges and provide future perspectives for the development and clinical translation of MMS NPs, underscoring their potential to reshape CT paradigms.