Non-small cell lung cancer (NSCLC) is the most common cancer type in lung cancers and causes most motality for all the lung cancers. Fortunately, several inhibitors of epidermal growth factor receptor have the clinical application for treating this disease such as Gefitinib and Lapatinib, which were under clinical trial for this disease or had been approved for marketing. In some cases, the resistance of chemotherapy for treating solid tumor can also be overcome by the inhibition of receptor tyrosine kinase (RTK). Angiogenesis, a mechanism for forming blood vessel in tissue, is critical for the growth and metastasis of tumor. Malignant tumor tissue stimulates its own growth of blood vessel by break the balance of pro and anti angiogenic factors. There are three factors regulating angiogenesis including vascular endothelial growth factor (VEGF), platelet-derived growth factor and fibroblast growth factor. BIBF 1120 (Vargatef) is a newly developed compound which could inhibit all of three receptors classes and thus completely block the stimulation mechanism of angiogenesis. Ideally, BIBF1120 could prevent both tumor growth and metastasis. Indeed, BIBF1120 reduced the tumor progression in lab animals for many types of solid tumors. Based on these results, BIBF1120 is now under phase I clinical trial for non-small cell lung cancer in healthy human. Ellis et al (1) selected thirty one patients in this study. Among them, 21 patients complete this study. The most common adverse effect are nausea, vomiting, abdominal pain and diarrhea. Other side effect includes fatigue, nausea, anorexia, rash, diarrhea and vomiting. In conclusion, BIBF 1120 and pemetrexed together is a good choice for further clinical trial. As I mentioned in last several blogs, the inhibitor of receptor tyrosine kinase (RTK) is widely used to treat solid tumor such as non-small cell lung cancer (NSCLC), breast cancer, ovarian cancer etc. Now another inhibitor of receptor tyrosine kinase (RTK) is being developed by two pharmaceutical company Aveo and Astellas to treat solid tumor. Tivozanib is now under phase III clinical trial for the treatment of advanced renal cell carcinoma (RCC) based on its good results from phase II clinical trial. Tivozanib is an inhibitor of vascular endothelial growth factor (VEGF). Blood vessel is critical for cancer progression becuase cancer cells needs oxygen and nutrition to keep growth. VEGF is a receptor tyrosine kinase that mediates the growth of blood vessel especially in cancer tissue. Blocking VEGF is to eliminate the supply of tumor growth and thus inhibit the progression of tumor. Although effective, the inhibitor of VEGF still has its limitations. For example, some tumor resist the effect of VEGF inhibitor treatment. Inhibitors of VEGF, together with other receptor tyrosine kinase, are the first choice for treating advance renal cell carcinoma (RCC)[1]. Tivozanib is a novel orally available small molecule and is found to be an effective inhibitor of VEGF. It potentially inhibits all three types of VEGF, therefore maximize its on-target effect and limit its off-target toxicity. Phase II clinical trial showed that tivozanib is well tolerated and significantly prolonged the life of patients with advance renal cell carcinoma. The phase III clinical trial, aim to examine widely the effectiveness and safety of the drug, is now in progress. Soon after, the drug will marketed in both USA and Europe. (1) Clin Cancer Res.2010 May 15;16(10):2881-9. Epub 2010 May 11 Related Posts: 1. Epidermal Growth Factor, a target for killing cancers 2. Lapatinib, a EGFR inhibitor, is now under phase II clinical trial for head and neck tumor
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