Wnt signalling pathway constitutes an important and highly conserved cellular pathway in humans that is involved in the regulation of several fundamental cellular processes including cellular proliferation, invasion and differentiation, cellular migration, and stem cell renewal besides genetic stability and apoptosis. It has two main branches through which it mediates its biological functions—canonical and non-canonical. Canonical is dependent upon the mediation of β-catenin, while non-canonical is not. Wnt signalling has been directly implicated in various cancers, especially colorectal, breast, lung and haematopoietic ones. Wnt signalling pathway is also involved in cellular signalling crosstalk with several other important cellular pathways like Notch, Sonic Hedgehog, BMP/TGF-β and Hippo pathways and all this underscores its importance as therapeutic targets for the viable treatment of malignancies. Here in this chapter, we have attempted to exhaustively shed light on the intricate working of the Wnt pathway and how various molecules of this pathway are being used as a target for the novel and effective therapeutics for better management of various cancers.