Multi-targeted receptor tyrosine kinase (RTK) and non-receptor tyrosine kinase (nRTK) panel (Multi-TKI Profile)

This entry represents a broad profile of tyrosine kinases rather than a single molecular target. It encompasses several families of receptor tyrosine kinases (RTKs) such as the Vascular Endothelial Growth Factor Receptors (VEGFR1/3), Platelet-Derived Growth Factor Receptors (PDGFRα/β), Fibroblast Growth Factor Receptors (FGFR1/2/3), and others like MET, RET, and EGFR, alongside non-receptor kinases like ABL. These proteins are critical mediators of cellular signaling pathways that regulate angiogenesis, cell growth, and tissue repair. In many cancers, these kinases are overexpressed or mutated, driving tumor progression, metastasis, and resistance to conventional therapies. Drugs targeting this specific combination of kinases, often referred to as multi-targeted tyrosine kinase inhibitors (TKIs), are designed to simultaneously disrupt multiple pathways—such as blocking the blood supply to the tumor (via VEGFR) while also inhibiting direct tumor cell proliferation (via FGFR or MET). This multi-pronged approach is particularly effective in complex, heterogeneous tumors but is often associated with a distinct profile of systemic toxicities due to the inhibition of these kinases in healthy tissues.

Other names

Multi-kinase target profileTyrosine kinase inhibitor (TKI) target setPan-kinase target group

Competitive inhibition of the ATP-binding site within the intracellular kinase domain of multiple receptor and non-receptor tyrosine kinases, preventing downstream phosphorylation and signaling cascades.