RP10107

RP10107 is a potent and selective small molecule inhibitor of glutaminase-1 (GLS-1), an enzyme that catalyzes the conversion of glutamine to glutamate. Developed by Rhizen Pharmaceuticals in collaboration with Incozen Therapeutics, RP10107 targets the metabolic dependency of cancer cells on glutaminolysis, a process critical for tumor progression and survival. Preclinical data presented at AACR 2018 demonstrated that RP10107 has nanomolar potency against human, mouse, and rat GLS-1 with over 380-fold selectivity over GLS-2. In multiple myeloma models, RP10107 has shown synergistic activity when combined with the proteasome inhibitor carfilzomib, leading to increased apoptosis, G0/G1 cell cycle arrest, and enhanced expression of cleaved caspase-8 and cleaved PARP.