Kinase Inhibitor

Kinase Inhibitor - What is a Kinase Inhibitor?

A protein kinase inhibitor is a type of enzyme inhibitor that specifically blocks the action of one or more protein kinases. Hence, they can be subdivided or characterised by the amino acids whose phosphorylation is inhibited.

Most kinases act on both serine and threonine, the tyrosine kinases act on tyrosine, and a number (dual-specificity kinases) act on all three. There are also protein kinases that phosphorylate other amino acids, including histidine kinases that phosphorylate histidine residues.

They can interfere with the repair of DNA double-strand breaks.

Kinase inhibitors such as dasatinib are often used in the treatment of cancer and inflammation. The novel kinase inhibitor PLX5568 is currently in clinical trials for treatment of polycystic kidney disease as well as pain.

Some of the kinase inhibitors used in treating cancer are inhibitors of tyrosine kinases. The effectiveness of kinase inhibitors on various cancers can vary from patient to patient.

This article is licensed under the Creative Commons Attribution-ShareAlike License. It uses material from the Wikipedia article on "Protein kinase inhibitor" All material adapted used from Wikipedia is available under the terms of the Creative Commons Attribution-ShareAlike License. Wikipedia® itself is a registered trademark of the Wikimedia Foundation, Inc.

Drugs Targeting Kinase Inhibitors

Currently there are several drugs launched or in development that target protein kinases and the receptors that activate them:

NameTargetCompanyClassFDA Approval
BevacizumabVEGFGenentechMonoclonal antibody2004 Colorectal
BIBW 2992EGFR/Erb2Boehringer IngelheimSmall moleculeNot yet
CetuximabErb1Imclone/BMSMonoclonal antibody2006 Mar (SCCHN)
ImatinibBcr-AblNovartisSmall molecule2001 (CML)
TrastuzumabErb2Genentech/RocheMonoclonal antibody1998
GefitinibEGFRAstraZenecaSmall molecule2003
RanibizumabVEGFGenentechMonoclonal antibody2006 (AMD)
PegaptanibVEGFOSI/PfizerRNA Aptamer2004 (AMD)
Sorafenibmultiple targetsOnyx/BayerSmall molecule2005 Dec (kidney)
Dasatinibmultiple targetsBMSSmall molecule2006
Sunitinibmultiple targetsPfizerSmall molecule2006 Jan (RCC & GIST)
ErlotinibErb1Genentech/RocheSmall molecule2005 Nov ?
NilotinibBcr-AblNovartisSmall molecule2007
LapatinibErb1/Erb2GSKSmall molecule2007 (HER2+ Breast)
PanitumumabEGFRAmgenMonoclonal antibody2006
VandetanibRET/VEGFR/EGFRAstraZenecaSmall moleculeE7080
PazopanibVEGFR2/PDGFR/c-kitGlaxoSmithKlineSmall molecule2009
Mubritinib?TakedaSmall moleculeNot yet

This article is licensed under the Creative Commons Attribution-ShareAlike License. It uses material from the Wikipedia article on "Protein kinase inhibitor" All material adapted used from Wikipedia is available under the terms of the Creative Commons Attribution-ShareAlike License. Wikipedia® itself is a registered trademark of the Wikimedia Foundation, Inc.