Entrectinib is used to treat a certain type of non-small cell lung cancer (NSCLC) in adults that has spread to other parts of the body. It is also used to treat certain types of solid tumors in adults and children 12 years of age and older that cannot be treated by surgery or that has spread to other parts of the body and that worsened after treatment with other chemotherapy medications. Entrectinib is in a class of medications called kinase inhibitors.

It works by blocking the action of the abnormal protein that signals cancer cells to multiply. This helps to stop or slow the spread of cancer cells.

Side Effects Of Entrectinib

Entrectinib may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • tiredness
  • constipation
  • diarrhea
  • taste changes
  • headache
  • cough, fever, or other signs of infection
  • muscle or joint pain
  • back pain
  • weight changes
  • rash
  • difficulty falling or staying asleep

Some side effects can be serious. If you experience any of these symptoms, call your doctor immediately or get emergency medical treatment:

  • difficulty with learning, memory, attention, or problem solving
  • mood changes such as anxiety, depression, confusion, or agitation
  • bone pain or difficulty moving
  • vision problems or changes in vision
  • joint pain, stiffness, redness, or swelling
  • pain in the upper right part of the stomach, yellowing of skin or eyes, loss of appetite, or bleeding or bruising easily
  • shortness of breath; difficulty breathing when lying down; or swelling of the arms, legs, hands, or feet

Entrectinib may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.

Warnings & Precautions

Before taking entrectinib:

  • tell your doctor and pharmacist if you are allergic to entrectinib, any other medications, or any of the ingredients in entrectinib capsules. Ask your pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention the following: aprepitant (Emend), certain antifungal medications such as fluconazole (Diflucan), itraconazole (Omel, Sporanox), or ketoconazole; certain medications for arrhythmias such as amiodarone (Nexterone, Pacerone), procainamide, quinidine (in Nuedexta), and sotalol (Betapace, Sorine, Sotylize); azithromycin (Zithromax); clarithromycin (Biaxin, in Prevpac); diltiazem (Cardizem, Tiazac, others); erythromycin (E.E.S., Erythrocin, others); enzalutamide (Xtandi); certain HIV medications such as efavirenz (Sustiva, in Atripla), indinavir (Crixivan), nelfinavir (Viracept), nevirapine (Viramune), ritonavir (Norvir, in Kaletra, others), or saquinavir (Invirase); lithium (Lithobid); modafinil (Provigil); nefazodone; oxcarbazepine (Trileptal); phenobarbital; phenytoin (Dilantin, Phenytek); pioglitazone (Actos, in Actoplus, Duetact, Oseni); rifabutin (Mycobutin); rifampin (Rifadin, Rimactane, in Rifater); oral steroids such as dexamethasone, methylprednisolone (Medrol), and prednisone (Rayos); and verapamil (Calan). Your doctor may need to change the doses of your medications or monitor you carefully for side effects. Many other medications may also interact with entrectinib, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list.
  • tell your doctor what herbal products you are taking, especially St. John’s Wort.
  • tell your doctor if you have or have ever had a nervous system condition, a prolonged QT interval (a rare heart problem that may cause irregular heartbeat, fainting, or sudden death), a slow or irregular heartbeat, a heart attack, heart failure, or heart or liver disease.
  • tell your doctor if you are pregnant, plan to become pregnant, or if you plan on fathering a child. If you are female, you will need to take a pregnancy test before you start treatment and use birth control to prevent pregnancy during your treatment and for at least 5 weeks after your final dose. If you are a male, you and your partner should use birth control during your treatment with entrectinib and for 3 months after your final dose. Talk to your doctor about birth control methods that you can use during your treatment. If you or your partner become pregnant while taking entrectinib, call your doctor immediately. Entrectinib may harm the fetus.
  • tell your doctor if you are breastfeeding. You should not breastfeed while you are taking entrectinib and for 7 days after the final dose.
  • you should know that entrectinib may make cause dizziness or confusion. Do not drive a car or operate machinery until you know how this medication affects you.

Dosage Of Entrectinib

Entrectinib comes as a capsule to take by mouth. It is usually taken with or without food once daily. Take entrectinib at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take entrectinib exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Swallow the capsules whole; do not open, chew, or crush them.

If you vomit immediately after you take entrectinib, take another dose as soon as possible.

Ask your pharmacist or doctor for a copy of the manufacturer’s information for the patient.


Keep all appointments with your doctor and the laboratory. Your doctor will order a lab test before you begin your treatment to see whether your cancer can be treated with entrectinib. Your doctor may order certain lab tests before and during your treatment to check your body’s response to entrectinib.

Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.


All information has been provided courtesy of MedLinePlus from the National Library of Medicine and from the FDA.