Nilotinib
Nilotinib is approved to treat chronic or accelerated phase Philadelphia chromosomeA long DNA molecule containing genetic information (genes). Humans have 46 chromosomes. One set of 23 is inherited from each parent. A full set of chromosomes is present in the nucleus of each human cell.-positive chronic myelogenous 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) that is resistant to prior therapy with imatinib.1
Nilotinib (Tasigna®) 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 inhibitor that binds to the inactive form of the 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. to inhibit Bcr-Abl kinase activity.1
The diagram below shows the 3D molecular structure of Nilotinib.
Side Effects include: myelosuppressionThe decreased activity of the blood cell precursors located in the bone marrow. Both red and white blood cells in the bloodstream originate from these cells which are often short-lived and are replaced constantly by rapidly dividing precursor stem cells. Chemotherapy agents, radiation and many other cancer treatments are designed to attack rapidly dividing cells and inhibit the activity of these normal bone marrow cells. Several side effects of cancer treatment, such as anemia and a decreased ability to fight infections (immunosuppression) are due to the effects of these treatments on bone marrow cells., elevations in serum lipase, electrolyte abnormalities, and fatigue.1
The most common toxicities produced by nilotinib are myelosuppressionThe decreased activity of the blood cell precursors located in the bone marrow. Both red and white blood cells in the bloodstream originate from these cells which are often short-lived and are replaced constantly by rapidly dividing precursor stem cells. Chemotherapy agents, radiation and many other cancer treatments are designed to attack rapidly dividing cells and inhibit the activity of these normal bone marrow cells. Several side effects of cancer treatment, such as anemia and a decreased ability to fight infections (immunosuppression) are due to the effects of these treatments on bone marrow cells. (low blood counts), QT prolongation (increased duration of cardiac ventricular repolarization), elevated serum lipase, liver toxicity and electrolyte abnormalities (irregular levels of phosphate, potassium, calcium and sodium). Nilotinib is not recommended for patients with low potassium levels, low magnesium levels or long QT syndrome. Additionally, nilotinib contains lactose so patients with galactose intolerance, severe lactase deficiency or problems with glucose-galactose absorption should be treated with caution. Due to potential harm to the fetus, prospective mothers should be warned before beginning treatment and women should avoid becoming pregnant while receiving nilotinib. Mothers should not breast feed infants while undergoing nilotinib treatment. Due to the possibility of drug interaction, administration of nilotinib along with CYP3A4 inhibitors or drugs that prolong QT interval is not advised.1
Top