Molecularly targeted anticancer therapies are now available that have been rationally designed to interact with specific proteins associated with tumour development or progression. The main purpose of this article is to review the rationale and phase II/III clinical data for approved and emerging multitargeted agents used in the treatment of solid tumours. Imatinib, sunitinib, sorafenib, and dasatinib have all produced advances in the treatment of the indications for which they are licensed and show promising activity in other tumour types. Newer multitargeted agents in development appear, from preliminary phase I and II data, to be active in a broad range of tumour types, although the clinical relevance of this activity is as yet unproven. The challenge for the future is to ensure that the potential of multitargeted agents is maximised by selecting the patient populations most likely to derive clinical benefit, by optimising the dose schedules used, and by investigating multitargeted therapies combined with other agents of the same type or with conventional chemotherapy and/or other treatment modalities.