The volume is dedicated to novel anticancer strategies. Our aim was to identify and cover novel, emerging anticancer approaches that will form the backbone of future, more efficient anticancer therapies. Beside classical “small molecule” pharmacologic approaches, or radiotherapy, the review introduces cancer stem cell, their markers involved in metastasizing, it covers various immunotherapeutic experimental treatment, inclusive anticancer cellular vaccines, as well as computational strategies aimed at modeling of cancer therapy or at least the intermolecular interactions between drug and the cellular target. Large portion of the volume is dedicated to various targeted anticancer approaches that involve either novel targets within cancer cells (i.e. endoplasmic reticulum and protein folding, or cell–cell adherence), or novel molecules like TRAIL and another human cytokine mda-7/IL-24, Brevinin-2R, viral proteins R4orf4, NS1, and apoptin, HAMLET, onconase, and other molecules. Significant part of the review is also dedicated towards targeting of receptor-initiated and intracellular kinase cascades that are often upregulated in various malignancies. We hope that the variety of topics highlighted in this volume will foster cross-discipline collaborations, so necessary for the development of novel therapeutics.