pazopanib + palbociclib

Pazopanib + palbociclib is a combination therapy being investigated for the treatment of refractory solid tumors, specifically those with 11q13 chromosomal amplification (including *CCND1*, *FGF3*, *FGF4*, and *FGF19*). Pazopanib is an oral multi-targeted tyrosine kinase inhibitor (TKI) that primarily targets vascular endothelial growth factor receptors (VEGFR-1, -2, and -3), platelet-derived growth factor receptors (PDGFR-α and -β), and the stem cell factor receptor (c-Kit), thereby inhibiting tumor angiogenesis and growth. Palbociclib is an oral, selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which prevents the phosphorylation of the retinoblastoma (Rb) protein and blocks cell cycle progression from the G1 to the S phase. This combination aims to overcome resistance mechanisms in tumors where 11q13 amplification drives both cell cycle dysregulation and pro-angiogenic signaling. It is currently being evaluated in a Phase Ib/II clinical trial led by Tianjin Medical University Second Hospital for indications such as urothelial carcinoma and head and neck squamous cell carcinoma.

Other names

pazopanib combined with palbociclib