Beloranib is a potent inhibitor of methionine aminopeptidase 2 (MetAP2), an enzyme involved in protein processing and cellular growth regulation. Its primary therapeutic application has been investigated in the treatment of obesity and type 2 diabetes due to its ability to reduce appetite, improve insulin sensitivity, and promote weight loss. By inhibiting MetAP2, beloranib modulates key metabolic pathways, leading to decreased food intake and increased energy expenditure.

It has shown promise in clinical trials for patients with severe obesity, including those with genetic disorders such as Prader-Willi syndrome, where uncontrolled hunger and obesity are major challenges. Beloranib was observed to induce significant weight loss and improve metabolic markers such as triglycerides and glucose levels.

Additionally, due to its anti-angiogenic properties—resulting from MetAP2 inhibition—beloranib has been explored for potential use in cancer therapy, where it may help suppress tumor growth by limiting blood vessel formation.

Despite its potential, development has faced setbacks due to safety concerns, including serious adverse events in some trials. As a result, further research is needed to fully assess its risk-benefit profile and determine viable clinical applications.