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Entrectinib

Why is it prescribed?

Entrectinib is used to treat locally advanced (not amenable to curative-intent therapy) or metastatic, non-squamous, ROS1-positive non-small cell lung cancer (NSCLC) as a first-line treatment in patients who have stable brain metastases (if present).

Products that have this ingredient include •Rozlytrek® capsules •

See other drugs used in the treatment of •non-small cell lung cancer •

The following side effects are the most common:

  • Swelling of legs 
  • Fatigue
  • Dizziness
  • Constipation
  • Diarrhea
  • Liver toxicity
  • Decreased kidney function
  • Low blood counts. Your white and red blood cells and platelets may temporarily decrease. This can put you at increased risk for infection, anemia and/or bleeding.
  • Electrolyte abnormalities
  • Nausea and vomiting
  • Change in taste
  • Shortness of breath

These are less common side effects: 

  • Fever
  • Low blood pressure
  • Memory impairment
  • Difficulty sleeping
  • Headache
  • Cough
  • Skin rash
  • Tingling/numbness in hands or feet (peripheral neuropathy)
  • Urinary tract infection
  • Abdominal pain
  • Loss of appetite
  • Bone pain
  • Muscle weakness
  • Muscle or joint pain
  • Vision changes
  • Weight gain

Contact your health care provider if you develop:

  • Nausea (interferes with ability to eat and unrelieved with prescribed medication)
  • Vomiting (vomiting more than 4-5 times in a 24-hour period)
  • Diarrhea (4-6 episodes in a 24-hour period)
  • Abnormal or fast heartbeat
  • Unusual bleeding or bruising
  • Black of tarry stools, or blood in your stools
  • Blood in the urine
  • Pain or burning with urination
  • Yellowing of the skin or eyes
  • Swelling of the feet or ankles. Sudden weight gain.
  • Extreme fatigue (unable to carry on self-care activities)
  • Changes in mental status including confusion, dizziness, mood, or balance
  • Mouth sores (painful redness, swelling or ulcers)

Entrectinib is a tyrosine kinase inhibitor in the signal transduction inhibitor category of targeted therapies. It may slow down or stop the cancer from growing. It may also help to shrink the cancer.
 


Do not use if allergic to any ingredients in this medication.

Let your health care provider know if you have:

  • Congestive heart failure
  • Long QT syndrome - a heart rhythm condition
  • high uric acid levels
  • liver or kidney problems
  • bone fractures
  • nervous system or cognitive problems
  • problems like fainting or passing out
  • eye or vision problems

Drug Interactions:

  • St. John’s Wort 
  • Ritonavir, saquinavir 
  • Itraconazole, ketoconazole, posaconazole and voriconazole 
  • Phenytoin, carbamazepine, phenobarbital 
  • Rifampin, rifabutin

Safety in pregnancy: Entrectinib may harm the fetus. Birth control must be used when on this medication and for 5 weeks after the last dose.

Safety in breastfeeding:  It is not known if entrectinib passes into breast milk. Breastfeeding not recommended during treatment and for 14 days after the final dose.