(UroToday.com) Dysregulated metabolism is a hallmark of renal cell carcinoma (RCC), driven by overexpression of glutaminase, a key enzyme of glutamine metabolism. Telaglenastat is an investigational, first-in-class, selective, oral glutaminase inhibitor that blocks glutamine utilization and is critical downstream pathways. Pre-clinically, telaglenastat synergized with cabozantinib, a VEGFR2/MET/AXL inhibitor, against RCC tumors utilizing dual inhibition of glucose and glutamine metabolic pathways. In a phase 1 study, telaglenastat + cabozantinib showed encouraging safety/efficacy as >=second-line therapy for mRCC with an objective response rate of 50% and 100% disease control rate. At the 2021 America Society of Clinical Oncology (ASCO) annual program, Dr. Nizar Tannir presented results of the CANTATA trial, comparing telaglenastat + cabozantinib versus placebo + cabozantinib in previously treated patients with clear-cell mRCC.

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