This review comprehensively examines the landscape of antineoplastic agents, delving into their mechanisms of action, clinical applications, and recent advancements. The paper categorizes these agents based on their classes, including chemotherapy, immunotherapy, and targeted therapy. A critical analysis of their efficacy, side effects, and challenges in clinical settings is presented. The review highlights recent breakthroughs and emerging trends, offering insights into the future of antineoplastic research. By exploring historical developments and addressing current challenges, this paper contributes to a deeper understanding of the complexities surrounding antineoplastic treatments. Keywords: Antineoplastic agents, Chemotherapy, Immunotherapy, Targeted therapy, Mechanisms of action, Clinical applications, Efficacy, Resistance, Side effects, Recent developments, Classification, Cancer treatment, Molecularly targeted therapy, Hormonal therapy, Radiation therapy, Combination therapy, Personalized medicine, Biomarkers, Drug discovery, Nanoparticle drug delivery.