telaglenastat + talazoparib

**Telaglenastat + talazoparib** is an investigational combination therapy composed of telaglenastat (CB-839), an oral glutaminase inhibitor, and talazoparib, an oral poly(ADP-ribose) polymerase (PARP) inhibitor. Telaglenastat selectively inhibits glutaminase, a key enzyme enabling glutamine metabolism critical for tumor cell survival and proliferation; this blockade disrupts tumor cell metabolic pathways. Talazoparib inhibits PARP1 and PARP2 enzymatic activity, preventing DNA single-strand break repair and trapping PARP on damaged DNA, leading to increased double-strand breaks and synthetic lethality—particularly in cells with homologous recombination repair (HRR) deficiencies such as BRCA mutations. The combination was explored for enhanced antitumor effect by targeting both cancer metabolism and DNA repair mechanisms[1][2][3][4][6][7][8].

Other names

telaglenastat and talazoparibglutaminase inhibitor and PARP inhibitor combination