CB-839

CB-839

CB-839, also known as Telaglenastat, is a small molecule inhibitor of glutaminase, an enzyme that plays a critical role in the metabolism of glutamine. Glutaminase catalyzes the conversion of glutamine to glutamate, which is a key step in the utilization of glutamine as a carbon and nitrogen source for rapidly proliferating cancer cells. By inhibiting glutaminase, CB-839 aims to starve cancer cells of the nutrients they need to grow and survive.

Mechanism of Action

CB-839 targets the enzyme glutaminase, which is overexpressed in many types of cancer cells. Glutaminase is responsible for converting glutamine into glutamate, which is then used in various biosynthetic pathways, including the production of nucleotides, amino acids, and lipids. By inhibiting glutaminase, CB-839 reduces the availability of glutamate, thereby disrupting these biosynthetic processes and inhibiting cancer cell growth.

Clinical Development

CB-839 is currently being investigated in clinical trials for its efficacy in treating various types of cancer, including renal cell carcinoma, triple-negative breast cancer, and non-small cell lung cancer. Early-phase clinical trials have shown promising results, with CB-839 demonstrating the ability to inhibit tumor growth and, in some cases, shrink tumors.

Pharmacokinetics

CB-839 is administered orally and has been shown to have a favorable pharmacokinetic profile. It is rapidly absorbed and achieves therapeutic concentrations in the plasma. The drug is metabolized primarily in the liver and excreted in the urine.

Side Effects

The most common side effects of CB-839 include fatigue, nausea, vomiting, and diarrhea. These side effects are generally mild to moderate in severity. In clinical trials, CB-839 has been well-tolerated, with a manageable safety profile.

Research and Future Directions

Ongoing research is focused on identifying biomarkers that predict response to CB-839, as well as exploring combination therapies that may enhance its efficacy. There is also interest in investigating the role of CB-839 in other metabolic pathways and its potential use in other types of cancer.

Also see

• Glutaminase
• Cancer metabolism
• Targeted cancer therapy
• Renal cell carcinoma
• Triple-negative breast cancer

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