Cabozantinib

Cabozantinib, sold under the brand-name Cabometyx and Cometriq, is a medication used to treat medullary thyroid cancer and a second line treatment for renal cell carcinoma among others. It is a small molecule inhibitor of the tyrosine kinases c-Met and VEGFR2, and also inhibits AXL and RET. It was discovered and developed by Exelixis Inc.RET inhibitors: Vandetanib (also VEGFR and EGFR). Entrectinib (ALK, ROS1, NTRK).c-MET inhibitor: Cabozantinib (also VEGFR2). Cabozantinib, sold under the brand-name Cabometyx and Cometriq, is a medication used to treat medullary thyroid cancer and a second line treatment for renal cell carcinoma among others. It is a small molecule inhibitor of the tyrosine kinases c-Met and VEGFR2, and also inhibits AXL and RET. It was discovered and developed by Exelixis Inc. In 2012 cabozantinib in its capsule formulation was approved by the U.S. FDA under the name Cometriq for treating patients with medullary thyroid cancer. The capsule form was approved in Europe for the same purpose in 2014. In April 2016 the US FDA granted approval for marketing the tablet formulation as a second line treatment for kidney cancer and the same was approved in Europe in October of that year. Cabozantinib is used in two forms. A capsule form is used since 2012 to treat medullary thyroid cancer and a tablet form is used since 2016 as a second line treatment for renal cell carcinoma. Cabozantinib has not been tested in pregnant women; it causes harm to fetuses in rodents. Pregnant women should not take this drug, and women should not become pregnant while taking it. It is not known if cabozantinib is excreted in breast milk. The drug should be used with caution in people with a history of heart rhythm problems, including long QT interval. In the US, the capsule formulation (Cometriq) carries a black box warning of the risk of holes forming in the stomach or intestines as well as formation of fistulas (tunnels between the GI tract and the skin). The black box also warns against the risk of uncontrolled bleeding. The tablet formulation (Cabometyx) warns of these effects as well. The labels also warn of the risk of clots forming and causing heart attacks or strokes, high blood pressure including hypertensive crisis, osteonecrosis of the jaw, severe diarrhea, skin sloughing off the palms and soles, a syndrome with headaches, confusion, loss of vision, and seizures, and protein appearing in urine. Very common adverse effects (greater than 10% of people) include decreased appetite; low calcium, potassium, phosphate, and magnesium levels; high bilirubin levels; distorted sense of taste, headache, and dizziness; high blood pressure; distorted sense of hearing, earaches and sore throat; diarrhea, nausea, constipation, vomiting, stomach pain and upset stomach, and inflammation of the mouth and lips and a burning sensation in the mouth; skin sloughing off the palms and soles, hair color changes and hair loss, rash, dry skin, and red skin; joint pain and muscle spasms; fatigue and weakness; weight loss, elevated transaminases, higher cholesterol levels, and loss of red and white blood cells.