Cancer is a multifaceted disorder with serious threat across the globe. The vision for accomplishing an effective treatment strategy for cancer has always been a major concern worldwide. Although conventional drug therapy, esp. the chemotherapeutics provide benefits upto certain extent for treatment and management of cancers, yet it possesses umpteen challenges in terms of the associated side effects and adverse effects, lack of targeting ability, multi-drug resistance, poor patient acceptance and compliance, etc. at the desired site. To overcome these problems, the nanomedicines have been evolved as an effective and cost-effectual alternative for treatment of cancer. Inspiring from the concept of magic bullet, the world is moving towards developing the surface modified nanocarriers, which not only provide effective drug delivery but also allows site-specific monitoring of the cancer cells through in vivo diagnostic imaging. The present review endeavors to provide an explicit account on various drug targeting strategies employed for nanomedicines like active targeting, passive targeting, magnetic targeting, physical targeting and ultrasound targeting, etc, followed by their utility in the treatment of a particular type of cancer. According to the recent market survey, many nanocarrier-based drug delivery systems have been approved by USFDA, EMEA, MHRA and other global regulatory agencies, testify the high degrees of acceptance of the nanomedicines for treatment of cancer, while many products are under the preclinical and clinical development phases. Thus, for the translation of such technologies into the clinic, the pharma industry needs to be metamorphosing for a change in its culture of developing the traditional therapeutics.