Drug intelligence / Profile preview

cabozantinib + CB-839

Development stage
Unknown
Lead developer
Calithera Biosciences, Inc
Modality
Small Molecules
Administration
Oral
01

Overview

Cabozantinib + CB-839 is a combination of two small molecule drugs under investigation for cancer treatment, primarily in metastatic renal cell carcinoma (RCC) and neuroendocrine tumors (NETs). **Cabozantinib** is a tyrosine kinase inhibitor that targets multiple kinases, notably **VEGFR2, MET, and AXL**, which are key drivers of tumor growth, metastasis, and angiogenesis. **CB-839** (also known as **telaglenastat**) is an oral, selective inhibitor of **glutaminase**, an enzyme crucial for cancer cell metabolism, particularly in tumors that are dependent on glutamine for proliferation and survival. By combining these agents, the regimen aims to disrupt complementary oncogenic pathways: inhibiting both key tyrosine kinases and tumor cell metabolism. Preclinical and early clinical studies have shown that this combination can be synergistic in renal cell and neuroendocrine tumor models. However, large clinical trials to date have not shown a significant improvement in progression-free survival over cabozantinib monotherapy in metastatic RCC, though the combination is generally well tolerated.

Brand names
CabometyxCometriq
Other names
cabozantinibCB-839CB839CB 839telaglenastat
02

Targets

AXL (AXL receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)TEK (Tie2)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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