Medically reviewed by Drugs.com. Last updated on Jan 22, 2024.
Uses for entrectinib
Entrectinib is used to treat metastatic (lung cancer that has already spread) non-small cell lung cancer (NSCLC) that is caused by a gene called ROS1. This medicine is also used to treat solid tumors (cancer) that are caused by certain abnormal NTRK genes and have spread or if surgery to remove the cancer is likely to cause severe complications, and there is no acceptable treatment option or the cancer grew or spread on other treatments. Your doctor will perform a test before you take this medicine.
Entrectinib belongs to the group of medicines called antineoplastics (cancer medicines). It works by interfering with the growth of cancer cells, which are eventually destroyed.
This medicine is available only with your doctor's prescription.
Before using entrectinib
In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:
Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
Appropriate studies have not been performed on the relationship of age to the effects of entrectinib to treat ROS1-positive NSCLC in children. Safety and efficacy have not been established.
Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of entrectinib to treat NTRK gene fusion-positive solid tumors in children 1 month of age and older. However, safety and efficacy have not been established in children younger than 1 month of age.
Appropriate studies on the relationship of age to the effects of entrectinib have not been performed in the geriatric population. However, no geriatric-specific problems have been documented to date.
There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.
Interactions with Medicines
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.
Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- Aripiprazole Lauroxil
- Arsenic Trioxide
- Inotuzumab Ozogamicin
- Sodium Phosphate
- Sodium Phosphate, Dibasic
- Sodium Phosphate, Monobasic
- St John's Wort
Interactions with Food/Tobacco/Alcohol
Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.
- Grapefruit Juice
Other Medical Problems
The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:
- Bone problems or
- Congestive heart failure or
- Electrolyte imbalance or
- Eye or vision problems or
- Heart disease (eg, myocarditis) or
- Heart rhythm problems (eg, QT prolongation, slow heartbeat) or
- Hyperuricemia (high uric acid in the blood) or
- Liver disease—Use with caution. May make these conditions worse.
Related/similar drugsImfinzi, Rybrevant, Opdivo, Keytruda, Tafinlar, methotrexate, hydroxyurea
Proper use of entrectinib
Medicines used to treat cancer are very strong and can have many side effects. Before using this medicine, make sure you understand all the risks and benefits. It is important for you to work closely with your doctor during your treatment.
Take this medicine only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.
This medicine comes with patient information leaflet and patient instructions. Read and follow the instructions carefully and make sure you understand them before taking this medicine. Ask your doctor if you have any questions.
Swallow the capsule whole. Do not crush or chew it. You may take this medicine with or without food.
If you are taking the capsules prepared as a suspension:
- Open the prescribed number of capsules and pour them into room temperature drinking water or milk. Let the suspension sit for 15 minutes before taking it.
- Measure the correct dose of medicine with the provided oral dosing syringe or measuring cup.
- Drink water after taking the suspension to make sure you swallow all the medicine. Store no longer than 2 hours at room temperature.
- If you are using a nasogastric tube or gastric feeding tube, the suspension can be given through the tube. Flush the tube with water or milk after each dose.
To use the oral pellets:
- Tap the packets to make sure that the pellets are on one side of the packet. Make sure you do not cut the pellets with scissors.
- Sprinkle the required number of packets on one or more spoonfuls of soft food (including applesauce, yogurt, or pudding). Take the mixture within 20 minutes. Drink water after taking the mixture to make sure you swallow all the medicine.
- Do not crush or chew the pellets to avoid bitter taste. Use the whole packet. Do not use part of the packet.
- Do not use the pellets to make an oral liquid. Do not give it using a nasogastric tube or gastric feeding tube, the pellets may clog the feeding tube.
Do not eat grapefruit or drink grapefruit juice while you are using this medicine. Grapefruit and grapefruit juice may change the amount of medicine that is absorbed in the body.
The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
- For oral dosage form (capsules or pellets):
- For ROS1-positive non-small cell lung cancer:
- Adults—600 milligrams (mg) once a day. Your doctor may adjust your dose as needed and tolerated.
- Children—Use and dose must be determined by your doctor.
- For NTRK gene fusion-positive solid tumors:
- Adults—600 milligrams (mg) once a day. Your doctor may adjust your dose as needed and tolerated.
- Children older than 6 months of age—Dose is based on body surface area (BSA) and must be determined by your doctor. Your doctor may adjust your dose as needed and tolerated.
- BSA of 1.51 meter squared (m2) or more—600 milligrams (mg) once a day.
- BSA of 1.11 to 1.50 m2—400 mg once a day.
- BSA of 0.81 to 1.10 m2—300 mg once a day.
- BSA of 0.51 to 0.80 m2—200 mg once a day.
- BSA of 0.50 m2 or less—300 milligrams per square meter (mg/m) once a day.
- Children older than 1 month to 6 months of age—Dose is based on body surface area (BSA) and must be determined by your doctor. The dose is usually 250 milligrams per square meter (mg/m) once a day. Your doctor may adjust your dose as needed and tolerated.
- Children younger than 1 month of age—Use and dose must be determined by your doctor.
- For ROS1-positive non-small cell lung cancer:
If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
If your next dose is within 12 hours, skip the missed dose and return to your regular dosing schedule.
If you vomit after taking a dose, take another dose as soon as possible.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Precautions while using entrectinib
It is very important that your doctor check your or your child's progress at regular visits to make sure this medicine is working properly. Blood tests may be needed to check for unwanted effects.
Using this medicine while you are pregnant can harm your unborn baby. If you are a woman who can bear children, your doctor may give you a pregnancy test before you start using this medicine to make sure you are not pregnant. Use an effective form of birth control during treatment and for at least 5 weeks after your final dose. Males with female partners who are able to become pregnant should use an effective form of birth control during treatment and for 3 months after the last dose. If you think you have become pregnant, tell your doctor right away.
Check with your doctor right away if you or your child have a chest pain that is worse than usual, trouble breathing, nausea or vomiting, pain or discomfort in your arms, jaw, back, or neck, feel faint, or you are sweating. This medicine may worsen the symptoms of an existing heart problem.
This medicine may cause dizziness, fainting, tiredness, blurred vision, memory loss, changes in mental status, confusion, or hallucinations. Make sure you know how you react to this medicine before you drive, use machines, or do other jobs that require you to be alert.
This medicine may increase your risk of bone fractures. Ask your doctor about ways to keep your bones strong to help prevent fractures.
Check with your doctor right away if you or your child have pain or tenderness in the upper stomach, pale stools, dark urine, loss of appetite, nausea, vomiting, or yellow eyes or skin. These could be symptoms of a serious liver problem.
Contact your doctor right away if you or your child have any changes to your heart rhythm. You might feel dizzy or faint, or you might have a fast, pounding, or uneven heartbeat. Make sure your doctor knows if you or anyone in your family has ever had a heart rhythm problem such as QT prolongation.
Check with your doctor immediately if blurred vision, difficulty in reading, or any other change in vision occurs during or after treatment. Your doctor may want you or your child to have your eyes checked by an ophthalmologist (eye doctor).
Cancer medicines can cause constipation, diarrhea, nausea, or vomiting in most people, sometimes even after receiving medicines to prevent it. Ask your doctor or nurse about other ways to control these side effects.
Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.
Side Effects of entrectinib
Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor immediately if any of the following side effects occur:
- Blurred vision
- burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings
- change in color vision
- clay colored stools
- dark urine
- decreased appetite
- defects in intelligence, short-term memory, learning ability, and attention
- difficulty seeing at night
- increased sensitivity of the eyes to sunlight
- itching or skin rash
- joint pain, stiffness, or swelling
- loss of appetite
- lower back, side, or stomach pain
- nausea and vomiting
- problems with balance
- sleepiness or unusual drowsiness
- stomach pain or tenderness
- swelling of the feet or lower legs
- trouble sleeping
- unusual tiredness or weakness
- yellow eyes or skin
- Chest pain or tightness
- decreased urine output
- dilated neck veins
- double vision
- extreme fatigue
- irregular breathing
- irregular heartbeat recurrent
- loss of memory
- problems with memory
- problems with speech or speaking
- seeing double
- seeing, hearing, or feeling things that are not there
- swelling of the face, fingers, feet, or lower legs
- trouble remembering
- trouble breathing
- weight gain
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
- Change or loss of taste
- difficulty having a bowel movement (stool)
Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.
Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
Commonly used brand name(s)
In the U.S.
Available Dosage Forms:
Therapeutic Class: Antineoplastic Agent
Pharmacologic Class: Tyrosine Kinase Inhibitor
More about entrectinib
- Check interactions
- Compare alternatives
- Side effects
- Dosage information
- During pregnancy
- Drug class: multikinase inhibitors
- En español
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