Tumor angiogenesis inhibitor

Bevacizumab (Avastin), a humanized monoclonal antibody against VEGF-A, has been shown to be effective on colorectal, renal and non-small cell lung cancers. Although it has already established a firm clinical positioning in treatment of such cancers, some side effects such as hypertension have been also concerned, and a balance of cost and relatively short survival period (several months to a couple of years) results in low penetration rates and seems to be a subject of discussion in a health economic field.

A number of pharmaceutical companies have launched and are developing receptor tyrosine kinase inhibitors (TKIs), a part of which are selective for VEGF receptors and the others have more broad spectrums. Although TKIs have also established a certain positioning in treatment of cancers (mainly renal cell carcinoma), relatively high adverse event rates and incidence of serious adverse events is likely to restrict expansion of combination therapies with current chemotherapeutics.

Interprotein is conducting a drug discovery research of small molecule tumor angiogenesis inhibitors that inhibit VEGF-stimulated proliferation of endothelial cells, show no kinase inhibitory activity, and are orally available for therapy of many kinds of advanced cancers, adjuvant therapies and prevention of metastasis. We believe that such a small molecule tumor angiogenesis inhibitor would be leading to the acquisition of broad indications and deep penetration in cancer therapies.