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Cabozantinib

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Cabozantinib, sold under the brand names Cometriq and Cabometyx, is a medication used to treat medullary thyroid cancer, renal cell carcinoma, and hepatocellular carcinoma. 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.

Product Description

Basic Characteristics

Product Name Cabozantinib
CAS Number 849217-68-1
Molecular Formula C28H24FN3O5
Molar mass 501.514
Synonyms XL184, BMS907351;

Cabometyx;

Cometriq;

Cabozanix.

Appearance White crystalline powder
Storage and Handling Store it at room temperature and away from excess heat and moisture.

 

CabozantinibDescription

Cabozantinib, sold under the brand names Cometriq and Cabometyx, is a medication used to treat medullary thyroid cancer, renal cell carcinoma, and hepatocellular carcinoma. 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 November 2012, cabozantinib (Cometriq) in its capsule formulation was approved by the U.S. Food and Drug Administration (FDA) under the name Cometriq for treating patients with medullary thyroid cancer. The capsule form was approved in the European Union for the same purpose in 2014.

In April 2016, the FDA granted approval for marketing the tablet formulation (Cabometyx) as a second line treatment for kidney cancer[8][9] and the same was approved in the European Union in September of that year.The brands Cometriq and Cabometyx have different formulations and are not interchangeable.

 

Cabozantinib Mechanism of Action

Cabozantinib inhibits the following receptor tyrosine kinases: MET (hepatocyte growth factor receptor protein) and VEGFR, RET, GAS6 receptor (AXL), KIT), and Fms-like tyrosine kinase-3 (FLT3).

 

CabozantinibApplication

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.

 

CabozantinibSide Effects & Warning

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.

 

Reference

[1] “Cabozantinib Use During Pregnancy”. Drugs.com. 30 March 2020. Retrieved 23 September 2020.

[2] “Cabometyx- cabozantinib tablet”. DailyMed. 21 July 2020. Retrieved 23 September 2020.

[3] “Cometriq- cabozantinib kit Cometriq- cabozantinib capsule”. DailyMed. 11 February 2020. Retrieved 23 September 2020.

[4] “Cometriq EPAR”. European Medicines Agency (EMA). Retrieved 23 September 2020.

[5] “Cabometyx EPAR”. European Medicines Agency. 17 September 2018. Retrieved 23 September 2020.

[6] “FDA approves Cometriq to treat rare type of thyroid cancer” (Press release). U.S. Food and Drug Administration (FDA). 29 November 2012. Archived from the original on July 7, 2014.