It is an oral multi-targeted tyrosine kinase enzymes inhibitor, authorized in Italy as second-line treatment for gastrointestinal Stromal Tumor (GIST) and as first and second line for advanced renal cell carcinoma and / or metastatic (MRCC). Sunitinib is a drug with low molecular weight (small) able to selectively inhibit certain proteins essential in growth cells trasphormed phenotype. These molecular motors are known as Tyrosine kinases (TK), or enzymes that send signals of growth and division to cell.
As part of the genetic study of the causes of malignant hyperproliferation, biologists have discovered a gene mutation that leads to the expression of the Tyrosine kinase that involces the synthesis by the cell of enzymes that have an activity higher than normal, hence the formation of malignant masses.
Moreover these changed entities hamper the activation of the defense mechanism of programmed cell death. The molecule presented below, is a competitive inhibitor for TK, or by interacting with them it prevents the body sends chemical signals that are translated into a proliferative response, preventing tumor growth (by inhibiting the action of FLT3 proliferative factor) and starving the masses going to block neoangiogenesis (VEGF inhibition factor pro neo vascularizing ) by preventing cancer cells are supplied with nutrients.
In a time where are all the rage gene therapy with viral vectors or monoclonal antibodies or other very interesting biotechnological strategies , the dear old molecoline totally chemical synthesis will never disappoint, even if their effectiveness is short-lived.