An update on molecularly targeted therapies in second- and third-line treatment in non-small cell lung cancer: focus on EGFR inhibitors and anti-angiogenic agents.
Docetaxel, pemetrexed and epidermal growth factor receptor tyrosine kinase inhibitors (gefitinib and erlotinib) are recommended second-line therapy for advanced non-small cell lung cancer (NSCLC) patients with disease progression. Although erlotinib is the only recommended third-line therapy, several drugs are being used in the clinic. Recent studies have focused on combining targeted agents with approved therapies, including broad-spectrum multikinase inhibitors targeting multiple ErbB Family receptors and multitargeted anti-angiogenic agents targeting the vascular endothelial growth factor receptor, platelet-derived growth factor receptor and fibroblast growth factor receptor pathways. Here, we review targeted therapies that are being evaluated in second- and third-line settings in NSCLC, including the ErbB Family Blocker afatinib (BIBW 2992), multityrosine kinase inhibitors (pelitinib [EKB-56]), neratinib [HKI-272], canertinib [CI-1033], lapatinib [GW-572016], dacomitinib [PF-299804]) and multitargeted anti-angiogenic agents (vandetanib [ZD6474], sunitinib [SU11248], sorafenib [BAY43-9006], nintedanib [BIBF1120], axitinib [AG-013736], cediranib [AZD2171], motesanib [AMG 706], linifanib [ABT869] and pazopanib [GW786034]).
Medical Oncology Service, Hospital de la Santa Creu i Sant Pau, c/Sant Antoni Maria Claret 167, 08025, Barcelona, Spain. mmajem@santpau.cat
M
M
Majem
C
C
Pallarès
D000077716:Afatinib; D000634:Aminoquinolines / Q000627:therapeutic use; D020533:Angiogenesis Inhibitors / Q000627:therapeutic use*; D000814:Aniline Compounds / Q000627:therapeutic use; D002289:Carcinoma, Non-Small-Cell Lung / Q000098:blood supply / Q000188:drug therapy*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D006801:Humans; D000077341:Lapatinib; D008175:Lung Neoplasms / Q000098:blood supply / Q000188:drug therapy*; D058990:Molecular Targeted Therapy; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D011799:Quinazolines / Q000627:therapeutic use; D011804:Quinolines / Q000627:therapeutic use
D000634:Aminoquinolines; D020533:Angiogenesis Inhibitors; D000814:Aniline Compounds; D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D011804:Quinolines; D000077341:Lapatinib; D000077716:Afatinib; D066246:ErbB Receptors; C487932:neratinib; C413879:EKB 569