NAMPT and cancer: In an attempt to broaden the therapeutic index, a second generation of NAMPTi (such as OT-82), as well as dual-function enzymatic inhibitors (i.e., inhibiting NAMPT enzymatic activity plus another target overexpressed in tumors, e.g., KPT-9274, which also blocks P21-activated kinase 4), were generated and are currently being evaluated in phase I clinical trials in cancer (250).