Metal-based drugs have emerged as pivotal therapeutics in cancer therapy, enlightening a path toward innovative and effective treatment strategies. Platinum-based therapeutics, notably cisplatin, carboplatin, and oxaliplatin, have transformed the landscape of cancer treatment, setting the stage for the development of next-generation metal-based compounds. Delving into the principles governing the design of metal-based drugs, this article navigates through their intricate coordination chemistry, targeted delivery approaches, and mechanisms of action. Notably, metal-based compounds form covalent bonds with DNA, disrupting vital cellular processes and inducing apoptosis in cancerous tissues. Even though contemporary chemotherapy as well as radiotherapeutic methods have greatly increased patient survival rates, disease recurrence still represents a fatal danger. The probability of metastasis and the drug resistance are increased by the incomplete clearance of neoplastic tissues from the body. This review explores the compelling journey of metal-based compounds, from their historical significance in ancient remedies to their pivotal role in modern oncology, and also discusses the recent advancements and emerging trends that promise to shape the future of metallodrugs. The shining promise of metal-based drugs in cancer remedies holds the potential to revolutionize treatment paradigms, offering hope and resilience in the ongoing battle against one of humanity's most relentless adversaries.