Cabometyx (Cabozantinib-S-Malate)


Cabometyx, sold under the brand names Cometriq and also Cabozantinib among others. Experts use it to treat medullary thyroid cancer, renal cell carcinoma and hepatocellular carcinoma that is getting worse and that has spread to other parts of the body. Cabometyx is a little molecule inhibitor of the tyrosine kinases c-Met and VEGFR2, and also inhibits AXL and RET. Exelixis Inc haves discovered and also developed it. In fact, it works by blocking the action of an abnormal protein that signals cancer cells to multiply. Also, this helps slow or stop the spread of cancer cells.

In November 2012, the US had approved the cabozantinib in its capsule formulation by the U.S. Food and Drug Administration (FDA). In fact, in April 2016, the FDA granted approval for marketing the tablet formulation (Cabometyx) as a second-line treatment for kidney cancer, and the same was approved in the European Union in September of that year. In January 2019, the FDA approved cabozantinib (Cabometyx, Exelixis, Inc.) for people with hepatoma (HCC) who are previously treated with sorafenib.

Cabozantinib is used in two forms. A capsule form is employed since 2012, to treat medullary thyroid cancer and a tablet form is employed since 2016, as a second-line treatment for renal cell carcinoma.

The formula is C28H24FN3O5·C4H6O5 and therefore the relative molecular mass is 635.6 Daltons as malate salt. The chemical structure of cabozantinib (S)-malate salt is:

Cabozantinib (S)-malate salt is a white to off-white solid that is practically insoluble in aqueous media. CABOMETYX (cabozantinib) tablets for oral use are supplied as film-coated tablets. The film coating contains hypromellose, titanium oxide, triacetin, and iron oxide yellow. Cabozantinib is eliminated mostly by the faeces (54%) and also by the urine (27%). Cabozantinib features a long half-life of 55 hours.

Side effects:

  • Constipation
  • Haemorrhoids
  • Nausea
  • Vomiting
  • Heartburn
  • change inability to taste food
  • difficulty swallowing
  • redness, swelling, sores, or pain in your mouth or throat
  • loss of appetite
  • weight loss
  • tiredness or weakness
  • pain in joints
  • muscle pain or spasms
  • Anxiety
  • numbness, burning or tingling within the hands, arms, feet, or legs
  • dry skin
  • patchy thickening of the skin
  • hair loss
  • hair colour turning lighter or grey
  • voice changes or hoarseness

Some side effects can be serious. In fact, if you experience any of those symptoms call your doctor immediately or get emergency medical treatment:

  • coughing up blood or blood clots
  • vomiting material that’s bloody or seems like dregs 
  • menstrual bleeding that is heavier than usual
  • red or black, tarry stool
  • any unusual or heavy bleeding or bruising
  • Diarrhoea
  • tender or painful stomach area
  • swelling or pain within the arms or legs
  • shortness of breath
  • lightheadedness or fainting
  • Sweating
  • numbness or weakness of the face, arm, or leg on one side of your body
  • Dizziness
  • sudden difficulty with balance or coordination
  • swollen or painful gums
  • sudden, severe headache
  • jaw pain
  • Toothache
  • Seizures
  • sudden trouble walking
  • sudden vision problems
  • Confusion
  • sudden difficulty thinking or speaking clearly
  • Rash
  • redness, pain, swelling or blistering on the palms or the soles
  • difficulty eating or drinking thanks to mouth sores or nausea and vomiting