Drug intelligence / Profile preview

palbociclib + cabozantinib

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

**palbociclib + cabozantinib** is a combination of two targeted small molecule inhibitors used (primarily experimentally or off-label) in oncology for their complementary anti-cancer effects. **Palbociclib** is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which prevents cell cycle progression in RB-proficient cancer cells by blocking the G1-S phase transition, leading to cell cycle arrest and reduced proliferation[4]. **Cabozantinib** is a multi-kinase inhibitor that targets receptor tyrosine kinases (RTKs) including VEGF receptors (VEGFR1, VEGFR2, VEGFR3), MET, RET, AXL, TYRO3, c-Kit, ROS1, Tie-2, and TrkB, thereby suppressing angiogenesis, tumor proliferation, invasion, metastasis, and resistance mechanisms[8][12]. This combination is not currently an approved regimen but may be studied preclinically or in experimental clinical trials, given evidence that combinatorial approaches can overcome resistance and exert additive or synergistic anti-tumor effects.

Other names
palbociclibcabozantinib
02

Targets

AXL (AXL receptor tyrosine kinase)NTRK2 (Tropomyosin-related kinase receptor type B)MET (Mesenchymal-epithelial transition factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)CDK6 (Cyclin-dependent kinase 6)TEK (Tie2)CYP3A4 (Cytochrome P450 3A4)VEGFR-1 (Vascular endothelial growth factor receptor 1)CDK4 (Cyclin-dependent kinase 4)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR2 (Vascular endothelial growth factor receptor 2)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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