Titanium is one of the most abundantly utilized nanomaterials for human consumption. Biomedical applications of nano titania include sunscreens, drug delivery, prosthetic implants, bioimaging probes, and antimicrobial and antirheumatic agents for various treatment of diseases, including autoimmune disease, neurogenerative diseases, cardiovascular, musculoskeletal, and cancer. Its applications as a drug delivery vehicle and photosensitizer in cancer therapy and diagnosis are highly appreciated, especially for skin and natural cavities applications. The reactive oxygen species (i.e., H2O2, OH., OH2, 1O2, etc.) generation properties of nano titania after activation with light or ultrasound make it ideal for apoptosis induction in neoplastic cells. In addition, the singlet oxygen (1O2) generating properties make it suitable for bioimaging deep-seated and superficial tumors after activation. Nano titania is highly biocompatible with negligible adverse effects. In this chapter, we will focus on the anticancer effects of nano titania on various types of cancers by employing it as a drug delivery vehicle and sensitizer for external source-activated modalities viz. photodynamic and sonodynamic therapy.