Targeted cancer therapy (TCT) is gaining increased interest because it reduces the risks of adverse side effects by specifically treating tumor cells. TCT testing has traditionally been performed using two‐dimensional (2D) cell culture and animal studies. Organ‐on‐a‐chip (OoC) platforms have been developed to recapitulate cancer in vitro, as cancer‐on‐a‐chip (CoC), and used for chemotherapeutics development and testing. This review explores the use of CoCs to both develop and test TCTs, with a focus on three main aspects, the use of CoCs to identify target biomarkers for TCT development, the use of CoCs to test free, un‐encapsulated TCTs, and the use of CoCs to test encapsulated TCTs. Despite current challenges such as system scaling, and testing externally triggered TCTs, TCToC shows a promising future to serve as a supportive, pre‐clinical platform to expedite TCT development and bench‐to‐bedside translation.