Editorial
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World J Clin Oncol. Feb 10, 2011; 2(2): 80-93
Published online Feb 10, 2011. doi: 10.5306/wjco.v2.i2.80
Tyrosine kinase inhibitors: Multi-targeted or single-targeted?
Fleur Broekman, Elisa Giovannetti, Godefridus J Peters
Fleur Broekman, Elisa Giovannetti, Godefridus J Peters, Department of Medical Oncology, VU University Medical Center, 1007 MB Amsterdam, The Netherlands
Author contributions: Broekman F collected literature and drafted the first version; Giovannetti E revised paper and add the additional literature; Peters GJ revised paper and found out additional literature and add final additions.
Correspondence to: Godefridus J Peters, PhD, Professor, Department of Medical Oncology, VU University Medical Center, PO Box 7057, 1007 MB Amsterdam, The Netherlands. gj.peters@vumc.nl
Telephone: +31-20-4442633 Fax: +31-20-4443844
Received: August 2, 2010
Revised: September 5, 2010
Accepted: September 12, 2010
Published online: February 10, 2011
Abstract

Since in most tumors multiple signaling pathways are involved, many of the inhibitors in clinical development are designed to affect a wide range of targeted kinases. The most important tyrosine kinase families in the development of tyrosine kinase inhibitors are the ABL, SCR, platelet derived growth factor, vascular endothelial growth factor receptor and epidermal growth factor receptor families. Both multi-kinase inhibitors and single-kinase inhibitors have advantages and disadvantages, which are related to potential resistance mechanisms, pharmacokinetics, selectivity and tumor environment. In different malignancies various tyrosine kinases are mutated or overexpressed and several resistance mechanisms exist. Pharmacokinetics is influenced by interindividual differences and differs for two single targeted inhibitors or between patients treated by the same tyrosine kinase inhibitor. Different tyrosine kinase inhibitors have various mechanisms to achieve selectivity, while differences in gene expression exist between tumor and stromal cells. Considering these aspects, one type of inhibitor can generally not be preferred above the other, but will depend on the specific genetic constitution of the patient and the tumor, allowing personalized therapy. The most effective way of cancer treatment by using tyrosine kinase inhibitors is to consider each patient/tumor individually and to determine the strategy that specifically targets the consequences of altered (epi)genetics of the tumor. This strategy might result in treatment by a single multi kinase inhibitor for one patient, but in treatment by a couple of single kinase inhibitors for other patients.

Keywords: Tyrosine kinase inhibitors; Targeted therapy; Epidermal growth factor receptor; Vascular endothelial growth factor receptor; Platelet derived growth factor; Breakpoint cluster region-Abelson murine leukemia oncogene homolog 1; Janus kinase