Entrectinib

Entrectinib is used in adults to treat non-small cell lung cancer that has spread to other parts of the body (metastatic).

Entrectinib is also used in adults and children at least 1 month old who have cancer that has spread to other parts of the body (metastatic), cannot be removed with surgery, or when other treatments did not work or stopped working.

Your doctor will make sure you have the correct tumor type to be treated with entrectinib.

Entrectinib may also be used for purposes not listed in this medication guide.

Follow all directions on your prescription label and read all medication guides or instruction sheets. Your doctor may change your dose from time to time. Use the medicine exactly as directed.

Your doctor will perform tests to ensure that entrectinib is the right treatment for you.

Entrectinib is usually taken once a day, with or without food. Take it the same way each time.

Do not change your dose or stop taking entrectinib without your doctor's advice.

Swallow the capsule whole with water and do not crush, chew, break, or open it. Do not take a capsule that is damaged in any way.

If you cannot swallow capsules whole, read and carefully follow the Instructions for Use provided with this medicine on how to open the capsules to prepare an oral suspension. Your healthcare provider will show you how many capsules and how much liquid you should use to prepare it correctly.

This oral suspension may also be given through a feeding tube. Make sure to measure a dose with the supplied measuring device (not a kitchen spoon). If you cannot take the oral suspension right away, keep it at room temperature and use it within 2 hours.

To take the oral pellets, open the packet and sprinkle the entire contents and mix with applesauce, yogurt, or pudding. Take the mixture within 20 minutes. Do not crush, chew, or give the oral pellets through a feeding tube.

Drink water right away after taking the oral suspension or oral pellets to ensure you receive a full dose. Ask your doctor or pharmacist if you do not understand these instructions.

If you vomit shortly after taking entrectinib, take another dose right away.

Doses are based on body surface area (height and weight) in children and teenagers. Your child's dose may change if the child gains or loses weight or if they are still growing.

You will need frequent medical tests, and your cancer treatments may change, be delayed, or discontinued based on the results.

Store tightly closed in the original container at room temperature away from moisture and heat.

Use only as directed. Inform your doctor if you are taking other medicines or have other medical conditions or allergies.

Tell your doctor if you have or have ever had:

• gout;
• heart problems, including long QT syndrome (in you or a family member);
• an electrolyte imbalance (such as low blood levels of potassium or magnesium);
• nervous system problems;
• problems with your eyes or vision; or
• liver or kidney disease.

You may be more likely to have a broken bone while using entrectinib. Talk with your doctor about ways to keep your bones healthy.

Entrectinib can harm an unborn baby if the mother or the father is using entrectinib.

• If you are a woman, you will need a pregnancy test to make sure you are not pregnant. Use birth control while using this medicine and for at least 5 weeks after your last dose.
• If you are a man, use birth control if your sex partner is able to get pregnant. Keep using birth control for at least 3 months after your last dose.
• Tell your doctor right away if a pregnancy occurs.

Do not breastfeed while using this medicine, and for at least 7 days after your last dose.

Get emergency medical help if you have signs of an allergic reaction: hives, difficulty breathing, swelling of your face, lips, tongue, or throat.

Entrectinib may cause serious side effects. Call your doctor immediately if you have:

• sudden pain or trouble moving your hip, wrist, or back;
• heart problems--swelling, rapid weight gain, feeling short of breath, fast or pounding heartbeats, fluttering in your chest, or sudden dizziness (like you might pass out);
• nervous system problems--dizziness, mood changes, confusion, hallucinations, problems with speech or concentration, thinking or memory problems, trouble hearing, reading, or sleeping;
• high levels of uric acid in blood--joint problems, stomach pain, little or no urination, nausea, vomiting, pink or brown urine;
• vision problems--blurred vision, vision loss, increased sensitivity to light, seeing flashes of light or "floaters" in your vision; or
• liver problems--loss of appetite, nausea, vomiting, stomach pain (upper right side), tiredness, itching, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).

Your cancer treatments may be delayed or permanently stopped if you experience certain side effects.

Common side effects of entrectinib may include:

• changes in your mental status;
• vision changes;
• nausea, vomiting, diarrhea, constipation;
• fever, cough;
• dizziness, tiredness;
• weight gain, swelling;
• muscle or joint pain;
• confusion, hallucinations, problems with memory;
• shortness of breath; or
• changes in your sense of taste or touch.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Usual Adult Dose for Non-Small Cell Lung Cancer:

600 mg orally once a day until disease progression or unacceptable toxicityUse: For adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are ROS1-positive

Usual Adult Dose for Solid Tumors:

600 mg orally once a day until disease progression or unacceptable toxicityUses: For adult patients with solid tumors that have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion without a known acquired resistance mutation; are metastatic or where surgical resection is likely to result in severe morbidity; and have progressed following treatment or have no satisfactory alternative therapy.

Usual Pediatric Dose for Solid Tumors:

12 years and older:-Body surface area (BSA) greater than 1.5 m2: 600 mg orally once a day-BSA 1.11 to 1.5 m2: 500 mg orally once a day-BSA 0.91 to 1.1 m2: 400 mg orally once a dayUse: For pediatric patients 12 years and older with solid tumors that have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion without a known acquired resistance mutation; are metastatic or where surgical resection is likely to result in severe morbidity; and have progressed following treatment or have no satisfactory alternative therapy.

Take the medicine as soon as possible, but skip the missed dose if your next dose is less than 12 hours away. Do not take two doses at once.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

• Avoid driving or hazardous activity until you know how entrectinib will affect you. Dizziness or drowsiness can cause falls, accidents, or severe injuries.

• Grapefruit may interact with entrectinib and cause side effects. Avoid consuming grapefruit products.

Sometimes it is not safe to use certain medicines at the same time. Some drugs can change the levels of other drugs in your blood, which may increase side effects or make the medicines less effective.

Entrectinib can cause a serious heart problem. Your risk may be higher if you also use certain other medicines for infections, asthma, heart problems, high blood pressure, depression, mental illness, cancer, malaria, or HIV.

Many drugs can affect entrectinib. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed here. Tell your doctor about all other medicines you use.