Drug intelligence / Profile preview

abemaciclib + cabozantinib

Development stage
Phase 2
Lead developer
Exelixis
Modality
Small Molecules
Administration
Oral
01

Overview

Abemaciclib + cabozantinib is an investigational **combination therapy** under evaluation for treating metastatic clear cell renal cell carcinoma (ccRCC). **Abemaciclib** is a selective small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), disrupting cancer cell cycle progression and proliferation. **Cabozantinib** is a small molecule tyrosine kinase inhibitor that targets multiple kinases involved in tumor cell growth and angiogenesis, including MET, VEGFR, and AXL. The rationale for combining these agents is to simultaneously inhibit cell cycle progression (abemaciclib) and tumor growth/angiogenesis pathways (cabozantinib), thus potentially providing enhanced anti-tumor activity over single-agent approaches. This combination is currently in phase 1b/2 trials, sponsored in part by Memorial Sloan Kettering Cancer Center and has not yet received regulatory approval for any indication[1][2][4][7][8][9][10].

02

Targets

AXL (AXL receptor tyrosine kinase)CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)DYRK1A (Dual-specificity tyrosine-phosphorylation-regulated kinase 1A)FLT3 (Fms related receptor tyrosine kinase 3)HIPK2 (Homeodomain-interacting protein kinase 2)HIPK3KIT (c-KIT proto-oncogene receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)RET (Rearranged during transfection receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)

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