Our study pharmacologically indicates that Benz, GBR-12935 (a selective DAT inhibitor), and Amitriptyline (a non-selective MAT inhibitor) targeted SLC6A3/DAT, inasmuch as these drugs significantly suppressed tumorigenesis and cancer cell viability, whereas neither muscarinic antagonists, the NET inhibitor nisoxetine, the dopamine receptor antagonist sulpiride, nor dopamine did. This evidence concerns the gene SLC6A2 and cancer.