Small molecule tyrosine kinase inhibitors: clinical development of anticancer agents.

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Laird AD, Cherrington JM

Small molecule tyrosine kinase inhibitors: clinical development of anticancer agents.

Expert Opin Investig Drugs. 2003 Jan;12(1):51-64.

PubMed ID

12517254 [ View in PubMed

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Abstract

Numerous small molecule synthetic tyrosine kinase inhibitors are in clinical development for the treatment of human cancers. These fall into three broad categories: inhibitors of the epidermal growth factor receptor tyrosine kinase family (e.g., Iressa trade mark and Tarceva trade mark ), inhibitors of the split kinase domain receptor tyrosine kinase subgroup (e.g., PTK787/ZK 222584 and SU11248) and inhibitors of tyrosine kinases from multiple subgroups (e.g., Gleevec trade mark ). In addition, agents targeting other tyrosine kinases implicated in cancer, such as Met, Tie-2 and Src, are in preclinical development. As experience is gained in the clinic, it has become clear that unleashing the full therapeutic potential of tyrosine kinase inhibitors will require patient preselection, better assays to guide dose selection, knowledge of mechanism-based side effects and ways to predict and overcome drug resistance.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Erlotinib	Epidermal growth factor receptor	Protein	Humans	Yes	Antagonist	Details