Cancer poses a major health problem, not only due to cancer-related deaths but also because of treatment toxicities. This review discusses early diagnosis and strategies to overcome treatment difficulties, to facilitate recovery, and prevent deaths. Generally, noninvasive techniques such as computed tomography (CT), magnetic resonance imaging (MRI), single photon emission computed tomography (SPECT) and positron emission computed tomography (PET), and their hybrid systems, including SPECT/CT, PET/CT, and PET/MRI, are used in diagnosis of cancer. Cancer treatment in clinics still comprises conventional methods such as chemotherapy, radiotherapy, and surgery. However, these techniques and methods are often inadequate. Therefore, new approaches, including the formulation of actively and/or passively targeted nanosized drug delivery systems and combined treatment protocols, are being investigated. In this article, conventional cancer imaging and treatment are reviewed. In addition, the formulation of nanosized systems and their use in cancer treatment are discussed and combined diagnostic and therapeutic (theranostic) approach are proposed as additional cancer therapies.