Most cancer patients present with advanced disease at diagnosis, and a large percentage of those diagnosed with early-stage disease eventually experience recurrence of metastatic disease. Although chemotherapy has recently produced promising results and some progress has been made in the treatment of locally advanced and advanced disease, treatment outcomes and adverse profiles for advanced cancers are still very disappointing. Thus, clinical research on new treatment strategies is warranted. Traditionally, chemotherapy is given by injection. Oral chemotherapy has been developed as a more convenient method of treatment for patients, without the need for cumbersome and uncomfortable injection devices. As oral chemotherapy is taken in the form of a tablet or capsule, it does not need to be injected into the body like other types of chemotherapy. There are many types of oral chemotherapy available for the treatment of different types of cancers. For many patients who are prescribed oral chemotherapy, taking their medication at home is one of the main advantages, as it allows them to live their daily lives without the disruption by hospital visits. In addition, some oral chemotherapy can be more effective and have fewer side effects than conventional chemotherapy. The growing availability of effective oral chemotherapy, especially the new class of 'targeted biologic therapies', is one of the wonderful recent advances in cancer care, as it has given cancer patients unprecedented convenience compared to intravenous infusion therapy. Here, newly developed oral chemotherapy agents and possible approaches to overcome these challenges are discussed.