US Food and Drug Administration (FDA) approvals of oral small–molecule anticancer agents have substantially increased over the past 6 years. From 2013 to 2018, 35 new molecular entities received introductory indications, with 9 new drugs approved in 2018.1 These approvals bring progressively increasing prices, prompting greater scrutiny and evaluation of alternative treatment strategies using pharmacology and other data to improve value. Examples include reduced-dose abiraterone, 250 mg (with food), which demonstrated pharmacodynamic noninferiority when compared with 1000 mg (fasting).2 A trial of reduced-dose ibrutinib showed greater than 95% receptor occupancy across doses with commensurate chemokine reductions, prompting calls for larger trials to reduce costs and improve tolerability.3 Clinical pharmacology-based studies add value to cancer care, and there are additional opportunities to use other approaches to treatment such as changes in prescribing and dispensing.