Abstract Cancer is one of the leading causes of death worldwide. Despite there are numerous treatments available for cancer therapy, early detection and efficient treatment with least side effects is still challenging. Covalent organic frameworks (COFs) are emerging crystalline porous polymeric material comprised of light weight atoms like H, B, C, N and O. The Unique characteristics of COFs is its porosity, large surface area and bio‐compatibility which makes them a suitable candidate for potential biomedical applications especially in cancer therapeutics, through targeted drug delivery. This review focused on general introduction of porous materials, history of COFs, an overview on cancer, brief discussion on the various synthetic strategies, dynamic linkages in COFs and potential biomedical application of COFs such as targeted drug delivery, photo thermal therapy (PTT) and photodynamic therapy (PDT). This review aims to provide in‐depth knowledge about COFs and its application in cancer therapeutics.