Tyrosine kinase receptors, drug

Key Words EGFR Non-small cell lung eaneer Oneogenes Receptor tyrosine kinases Gefitinib Erlotinib Tyrosine kinase inhibitors Drug resistance... 

Minor, L.K. 2003. Assays to measure the activation of membrane tyrosine kinase receptors focus on cellular methods. Curr. Opin. Drug Discov. Devel. 6, 760-765. 

Lipid Domains, Chemistry of Receptor Tyrosine Kinases Receptor-Ligand Interactions Receptors, Chemistry of Signal Transduction Across Membranes Virus-Based Drug Delivery... 

Li Sun and Gerald McMahon, Inhibition of tumor angiogenesis by synthetic receptor tyrosine kinase inhibitors. Drug Discovery Today, 5 (2000), 344—353. 

Semaxanib (SU-5416) was discovered in Sugen (owned by Pharmacia at the time, now Pfizer) as the lead compound in a series of small-molecule inhibitors of the multiple tyrosine kinase receptor for the potential treatment of cancer. In February 2002, Pharmacia made the decision to discontinue the drug based on interim results from phase III trials involving colorectal cancer patients. 

Pharmacodynamic (PD) biomarkers are markers of a certain pharmacological response, which are of special interest in dose optimization studies. Pharmacodynamic modeling is often based on animal studies and known behavior of certain individual drug classes. The models are used to support initial dosing studies. Two examples include cyclooxygenase inhibitors and a new tyrosine kinase receptor inhibitor [35-38]. 

Lankhorst S, Baelde HI, Kappers MH et al (2015) Greater sensitivity of blood pressure than renal toxicity to tyrosine kinase receptor inhibition with sunitinib. Hypertension 66 543-549 Lankhorst S, Kappers MH, van Esch JH et al (2014) Treatment of hypertension and renal injury induced by the angiogenesis inhibitor sunitinib precUnical study. Hypertension 64 1282-1289 Le DL, Cao H, Yang LX (2014) Cardiotoxicity of molecular-targeted drug therapy. Anticancer Res 34 3243-3249... 

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