GMX1778 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), an enzyme involved in the biosynthesis of nicotinamide adenine dinucleotide (NAD+). By targeting NAMPT, GMX1778 effectively depletes cellular NAD+ levels, which disrupts energy metabolism and leads to cancer cell death, particularly in tumor cells with high metabolic demands. It has been investigated primarily for its antitumor activity in preclinical studies, showing promise in models of melanoma, leukemia, and other solid tumors. Due to its mechanism, GMX1778 is studied as a potential agent in oncology, especially in cancers dependent on the NAMPT-mediated NAD+ salvage pathway. Research has also explored its use in combination with other chemotherapeutic agents to enhance cytotoxic effects.