The most recent successful example of combining allosteric and orthosteric drugs to circumvent drug resistance is the treatment of chronic myeloid leukemia (CML) by targeting Breakpoint Cluster Region-Abelson1 (BCR-ABL1) kinase (Heisterkamp et al., 1985). The gene discussed is BCR; the disease is chronic myelogenous leukemia, BCR-ABL1 positive.