AbstractCancer remains a major global health threat necessitating the multipronged approaches for its prevention and management. Traditional approaches in the form of chemotherapy, surgery, and radiotherapy are often encountered with poor patient outcomes evidenced by high mortality and morbidity, compelling the need for precision medicine for cancer patients to enable personalized and targeted cancer treatment. There has been an emergence of smart multimodal theranostic nanoformulation for triple combination cancer therapy in the last few years, which dramatically enhances the overall safety of the nanoformulation for in vivo and potential clinical applications with minimal toxicity. However, it is imperative to gain insight into the limitations of this system in terms of clinical translation, cost‐effectiveness, accessibility, and multidisciplinary collaboration. This review paper aims to highlight and compare the impact of the recent theranostic nanoformulations of triple therapeutics in a single nanocarrier for effective management of cancer and provide a new dimension for diagnostic and treatment simultaneously.