Advances in preclinical small molecules for the treatment of NSCLC

BACKGROUND: NSCLC accounts for 85% of all lung cancer cases and is the leading cause of cancer mortality. Advances in the knowledge of molecular events governing oncogenesis have led to a number of novel therapeutic agents targeting specific pathways critical for tumor growth. OBJECTIVE: To summarize the recent preclinical developments of small molecules for NSCLC therapy. METHODS: This review primarily consists of patents and publications between 1997 and 2008. RESULTS/CONCLUSION: Small molecules with known targets, such as inhibitors for EGFR, VEGF, RAS-RAF-MAP kinase pathway, phosphoinositide 3-kinase pathway, histone deacetylase, protein phosphatase, topoisomerase, cyclin dependent kinases, heat-shock protein, tubulin, DNA and MET are reviewed. Other novel small molecules with potent efficacy without target information are also discussed.