Cancer incidence and mortality are rapidly growing worldwide. In attempts to develop more efficacious therapeutic regimens for patients with cancer, nanomedicines have found increasing applications. Findings reveal that nanomedicines improve the clinical outcomes of cancer treatment by virtue of modified pharmacokinetics (PK) and biodistributions of the bioactive agents while reducing their systemic toxicity and adverse effects. Here, we provide an update on cancer nanomedicines that have been clinically approved and paradigmatic nanomedicines utilized in various therapeutic platforms undergoing Phase II/III clinical trials. We discuss the role of the developed nanomedicines in the improvement of current therapeutic regimens from both therapeutic and PK standpoints. By describing the state-of-the-art of nanomedicine and discussing their clinical advantages and challenges, we provide a perspective on the development of more effective therapeutic regimens to improve the clinical outcomes of cancer treatments.