The success obtained employing PI3K isoform‐specific inhibitors in the treatment of relapsed chronic lymphocytic leukemia (CLL) (Furman et al, 2014), relapsed indolent lymphoma (Gopal et al, 2014), and PIK3CA‐mutant breast cancers (Juric et al, 2018a,b) demonstrated the clinical potential of inhibiting specific nodes of PI3K signaling in patients selected based on cancer type and biomarkers. The gene discussed is PIK3CA; the disease is B-cell chronic lymphocytic leukemia.