Telaglenastat is an orally bioavailable glutaminase inhibitor with potential antineoplastic activity. CB-839 selectively and irreversibly inhibits glutaminase, a mitochondrial enzyme critical for converting glutamine into glutamate. By blocking glutamine utilization, it impairs proliferation in rapidly growing cells. Glutamine-dependent tumors rely on converting exogenous glutamine into glutamate and metabolites for energy and macromolecular building blocks. It functions as an EC 3.5.1.2 (glutaminase) inhibitor.
