Clinical development of SRC tyrosine kinase inhibitors in lung cancer.
Src tyrosine kinases regulate a large number of important mechanisms in normal and cancerous cells, are overexpressed in a broad range of tumors including lung cancer, and thus represent a potential target for cancer therapy. Preclinical experiments indicate that small-molecule inhibitors of Src block tumor growth, metastasis, and angiogenesis. Phase I data from healthy volunteers also suggest that inhibitors of Src prevent bone resorption. Several phase II trials with small-molecule inhibitors of Src are under way or have been initiated in lung cancer and in other malignancies, as discussed herein.
Lee
David
D
CIG Media Group, LP, Dallas, TX, USA.
Gautschi
Oliver
O
D052117:Benzodioxoles / Q000008:administration & dosage / Q000627:therapeutic use; D017321:Clinical Trials, Phase I as Topic; D000069439:Dasatinib; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000008:administration & dosage / Q000627:therapeutic use*; D011743:Pyrimidines / Q000008:administration & dosage / Q000627:therapeutic use; D011799:Quinazolines / Q000008:administration & dosage / Q000627:therapeutic use; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D013844:Thiazoles / Q000008:administration & dosage / Q000627:therapeutic use; D019061:src-Family Kinases / Q000378:metabolism
D052117:Benzodioxoles; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D011799:Quinazolines; D013844:Thiazoles; C515233:saracatinib; D020794:Receptor Protein-Tyrosine Kinases; D019061:src-Family Kinases; D000069439:Dasatinib