Imatinib Mesylate
Imatinib was designed to treat chronic myeloid leukemiaA cancer affecting the cells that develop into white or red blood cells. Both of these cell types originate from stem cells in bone marrow. Red blood cells function to carry oxygen to our tissues and the white cells (leukocytes) are part of our immune system. The cancerous cells often accumulate in the blood. (CML). In CML, a chromosomal rearrangement in white blood cells fuses two genes together. Imatinib is also used in the treatment MDS/MPD, which are associated with rearrangement of the PDGFR geneA stretch of DNA that leads to the production of an RNA. The RNA is produced during the process of transcription. This RNA can be used to guide the formation of a protein via translation or can be used directly in the cell.. It should be noted that Imatinib has a vast range of different doses, so you should talk to your doctor to figure out the best dose for you. Imatinib is taken through an oral tablet.1
Imatinib mesylate (Gleevec®) is a tyrosine kinaseAn enzyme that adds phosphate groups to target molecules. Often the targets of these enzymes are proteins that control the cell division process, so the enzymes play a key role in cell division. See also, kinase. inhibitor that works to prevent the growth-inducing signals sent by enzymes found in some cancerous cells. The product of the BCR-ABL geneA stretch of DNA that leads to the production of an RNA. The RNA is produced during the process of transcription. This RNA can be used to guide the formation of a protein via translation or can be used directly in the cell. is a kinaseAn enzyme that adds phosphate groups to another molecule. Many key proteins controlling gene expression are kinase targets. Addition of a phosphate group to a protein can alter the activity of the protein and are often used as molecular on/off switches. For example, the retinoblastoma tumor suppressor gene is 'off' when phosphate groups are added to the protein at specific locations. Removal of the phosphate groups turns the protein 'on'. Enzymes that remove phosphate groups are known as phosphatases. Note that all enzymes, regardless of function, end in ASE that adds phosphate groups onto target molecules (substrates). Imatinib binds to the the ATP binding site of the enzymeA protein that speeds up the process of chemical reactions in the body without becoming altered in the process. Almost every biological process is driven by the activity of enzymes. Without enzyme catalysts, the complex reactions that build and break down cell parts would not happen at a rate compatible with life. Enzyme names usually describe the reaction that is being catalyzed and all of them end in -ase.. If it is unable to bind ATP, the BCR-ABL proteinOne of the four basic types of biomolecule. Proteins are polymers made up of strings of amino acids. Proteins serve many functions in organisms including transport of molecules, structure, cell adhesion and as signaling molecules such as hormones. Many transcription factors, including p53 and Rb are proteins. cannot carry out its kinase activity. The signals sent by the enzyme would act to stimulate cell division so Imatinib inhibits tumor growth of cancerous cells.1
The diagram above shows the 3D molecular structure of Imatinib Mesylate.
Common side effects include frequent nausea and vomiting, diarrhea, leg aches or cramps, swelling of the face, altered bone marrow function and fluid retention. These side effects are usually mild or moderate and frequently occur during the first month of treatment and may get better after initial treatments.1
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