multikinase

Multikinase is a term used in biochemistry and pharmacology to describe enzymes or drugs that engage multiple kinase activities. In enzymology, it can refer to kinases that can phosphorylate more than one substrate or that contain multiple catalytic kinase domains within a single protein, enabling diverse regulatory and signaling roles. The concept highlights the complexity of cellular signaling networks, where a single molecule can influence several pathways.

In pharmacology, multikinase inhibitors are small molecules designed to block the activity of several kinases simultaneously. This broad activity aims to suppress redundant or compensatory signaling that can drive disease progression, especially in cancer. By targeting multiple kinases involved in proliferation, survival, angiogenesis, and metastasis, these inhibitors seek to produce more durable therapeutic responses than single-target agents. However, the broad activity can also increase the risk of off-target effects and toxicity, requiring careful patient monitoring and management.

Clinically used multikinase inhibitors include several approved cancer drugs that inhibit a range of kinases. Examples commonly cited are sorafenib, sunitinib, pazopanib, regorafenib, and lenvatinib, each with overlapping but distinct target profiles that commonly include vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), fibroblast growth factor receptors (FGFR), and other tyrosine kinases involved in tumor growth and angiogenesis. These agents have been applied across multiple tumor types, including renal cell carcinoma, hepatocellular carcinoma, gastrointestinal stromal tumors, and thyroid cancers.

Research on multikinase strategies focuses on optimizing selectivity, understanding resistance mechanisms, and balancing efficacy with safety. The term remains broad, encompassing both structural multi-domain kinases and pharmacologic multi-target inhibitors used in modern oncology.