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Drugs Fut 2018, 43(12): 881
ISSN 0377-8282
e-ISSN 2013-0368
Copyright 2018 Clarivate
CCC: 0377-8282
DOI: 10.1358/dof.2018.043.12.2869764
 
 
Telaglenastat. Glutaminase inhibitor, Treatment of advanced solid tumors
Gras, J.
 
 
Cancer cells can be distinguished from most normal cells by metabolic reprogramming, i.e., Warburg effect and glutamine dependency. Glutamine is converted by the mitochondrial enzyme glutaminase to glutamate. Suppression of glutaminase activity has antitumor activity in a wide variety of tumor types. Telaglenastat (CB-839) is a first-in-class, small-molecule, oral, potent and selective allosteric glutaminase inhibitor. In clinical trials it has been safe, and in triple-negative breast cancer (TNBC) patients refractory to taxane the drug showed a disease control rate (DCR) of 55% in combination with paclitaxel, and in renal cell carcinoma (RCC) patients in combination with everolimus it showed a DCR of 92%. Currently, there are three ongoing phase II studies with CB-839 in combination with everolimus or cabozantinib in patients with RCC, and in combination with paclitaxel in patients of African ancestry and non-African ancestry with advanced TNBC. The U.S. Food and Drug Administration has granted fast track designation for CB-839 in combination with everolimus or cabozantinib for the treatment of RCC patients.


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