Cancer remains one of the leading causes of morbidity and mortality worldwide. Conventional chemotherapy often causes severe side effects due to lack of selectivity and damage to healthy tissues. Targeted drug delivery systems have emerged as promising strategies to improve therapeutic efficacy while minimizing systemic toxicity. These systems utilize various nanotechnology-based carriers such as liposomes, nanoparticles, dendrimers, and polymeric micelles to deliver drugs directly to tumor tissues. Targeted drug delivery can be achieved through passive targeting, active targeting, and stimuli-responsive mechanisms. Recent advances in pharmacological research have led to the development of several innovative targeted therapies including antibody-drug conjugates, ligand-based targeting, and nanocarrier-mediated drug delivery systems. These approaches enhance drug accumulation at tumor sites and improve treatment outcomes. This review discusses the principles of targeted drug delivery, recent pharmacological advances, clinical applications, and future perspectives in cancer therapy. Keywords: Targeted drug delivery, cancer therapy, nanoparticles, nanomedicine, pharmacological advances, chemotherapy.