CB-839 (telaglenastat)

Telaglenastat is a potent and selective reversible inhibitor of glutaminase activity.

In recent decades, cancer research has undergone a profound paradigm shift, recognizing cancer not solely as a genetic disease, but also as a disorder of altered metabolism. This realization has led to the emergence of novel therapeutic strategies targeting the unique metabolic vulnerabilities of cancer cells.

Telaglenastat is a promising small molecule, designed to target glutaminase, a key enzyme involved in the metabolism of glutamine, a non-essential amino acid crucial for cellular growth and proliferation. By inhibiting glutaminase, telaglenastat aims to disrupt the metabolic pathways that cancer cells heavily rely on, thereby impairing their ability to sustain uncontrolled growth and evade therapeutic interventions.

To date, telaglenastat has been well tolerated in patients both in a single agent setting and in combination with SOC.