The last 100 years have seen a dramatic alteration in the treatment of cancer. Aside from small molecule inhibitors of protein tyrosine kinases, monoclonal antibodies have also been found to provide valuable therapeutic approaches for modulating tumour pathophysiology. As our knowledge of cancer biology improves, the specificity of this new generation of drugs is generally delivering an improved therapeutic ratio compared to traditional cytotoxic agents. However, patient selection through the use of biomarkers is key in optimising efficacy and improving cost-effectiveness. The most recent wave of revolutionary new systemic therapy approaches to cancer has arrived in recent years in the form of immune checkpoint inhibitors, now clinically validated as modulators of immune-regulatory pathways. The future of oncology therapeutics includes a combination of cytotoxic agents, targeted therapies and immunotherapy.