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Neratinib (Oral)

Medically reviewed by Last updated on Mar 26, 2022.

Commonly used brand name(s)

In the U.S.

  • Nerlynx

Available Dosage Forms:

  • Tablet

Therapeutic Class: Antineoplastic Agent

Pharmacologic Class: Tyrosine Kinase Inhibitor

Uses for neratinib

Neratinib is used to treat patients with HER2-overexpressed or amplified breast cancer that has been previously treated with trastuzumab. Neratinib is also used in combination with capecitabine to treat advanced or metastatic HER2-positive breast cancer (breast cancer that has already spread) in patients who have received two or more anti-HER2 based regimens. It belongs to the group of medicines, called antineoplastics.

Neratinib interferes with the growth of cancer cells, which are eventually destroyed. Since the growth of normal cells may also be affected by the medicine, other unwanted effects will also occur. Some of these may be serious and must be reported to your doctor.

Neratinib is available only with your doctor's prescription.

Before using neratinib

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 neratinib, the following should be considered:


Tell your doctor if you have ever had any unusual or allergic reaction to neratinib 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 neratinib in the pediatric population. Safety and efficacy have not been established.


Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of neratinib in the elderly. However, elderly patients are more likely to have serious unwanted effects (including kidney problems, vomiting, diarrhea, and dehydration), which may require caution in patients receiving neratinib.


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 neratinib, 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 neratinib 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.

  • Abametapir
  • Aluminum Carbonate, Basic
  • Aluminum Hydroxide
  • Aluminum Phosphate
  • Apalutamide
  • Boceprevir
  • Bosentan
  • Calcium Carbonate
  • Carbamazepine
  • Cenobamate
  • Cimetidine
  • Clarithromycin
  • Cobicistat
  • Conivaptan
  • Cyclosporine
  • Dexlansoprazole
  • Digoxin
  • Dihydroxyaluminum Aminoacetate
  • Dihydroxyaluminum Sodium Carbonate
  • Dronedarone
  • Efavirenz
  • Enzalutamide
  • Erythromycin
  • Esomeprazole
  • Etravirine
  • Famotidine
  • Fedratinib
  • Fexinidazole
  • Fosnetupitant
  • Fosphenytoin
  • Idelalisib
  • Indinavir
  • Itraconazole
  • Ketoconazole
  • Lansoprazole
  • Lopinavir
  • Lorlatinib
  • Lumacaftor
  • Magaldrate
  • Magnesium Carbonate
  • Magnesium Hydroxide
  • Magnesium Oxide
  • Magnesium Trisilicate
  • Mitotane
  • Modafinil
  • Nafcillin
  • Nefazodone
  • Nelfinavir
  • Netupitant
  • Nirmatrelvir
  • Nizatidine
  • Omeprazole
  • Pantoprazole
  • Phenobarbital
  • Phenytoin
  • Posaconazole
  • Primidone
  • Rabeprazole
  • Ranitidine
  • Rifampin
  • Ritonavir
  • Saquinavir
  • Sodium Bicarbonate
  • St John's Wort
  • Telaprevir
  • Telithromycin
  • Verapamil
  • Voriconazole

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. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other medical problems

The presence of other medical problems may affect the use of neratinib. Make sure you tell your doctor if you have any other medical problems, especially:

  • Dehydration or
  • Hypotension (low blood pressure) or
  • Kidney disease—Use with caution. May cause side effects to become worse.
  • Liver disease—Use with caution. May make this condition worse.

Proper use of neratinib

Medicines used to treat cancer are very strong and can have many side effects. Before using neratinib, make sure you understand all the risks and benefits. It is important for you to work closely with your doctor during your treatment.

Take neratinib exactly 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.

Neratinib comes with a patient information insert. Read and follow the instructions carefully. Ask your doctor if you have any questions.

Full Dose: You will be given medicines to help prevent diarrhea (including loperamide) during your first dose of neratinib. Continue taking these medicines for 2 cycles (56 days) of treatment with neratinib. Keep the number of your bowel movements at 1 to 2 per day and take anti-diarrhea medicines only as directed by your doctor.

Lower starting dose: Your doctor may also give you a lower starting dose for the first 2 weeks of treatment and then increase you to a full dose to help prevent diarrhea.

Swallow the tablet whole. Do not crush, break, or chew it. Take the medicine with food and at the same time each day.

If you are also using an antacid, take it 3 hours before using neratinib.

Take neratinib at least 2 hours before or 10 hours after an H2 blocker (eg, ranitidine).

Do not eat grapefruit or drink grapefruit juice while you are using neratinib.


The dose of neratinib 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 neratinib. 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 (tablets):
    • For treatment of early stage of breast cancer:
      • Adults—At first, 240 milligrams (mg) (6 tablets) taken once a day for at least 1 year. Some patients may start at 120 mg (3 tablets) once a day on Week 1 (Days 1 to 7), followed by 160 mg (4 tablets) once a day on Week 2 (Days 8 to 14), and then 240 mg (6 tablets) once a day on Week 3 and onwards. Your doctor may adjust your dose as needed and tolerated.
      • Children—Use and dose must be determined by your doctor.
    • For treatment of advanced or metastatic breast cancer:
      • Adults—At first, 240 milligrams (mg) (6 tablets) taken once a day on Days 1 to 21 of a 21-day cycle taken together with capecitabine 750 milligrams per square meter (mg/m[2]) taken twice a day on Days 1 to 14 of a 21-day cycle. Some patients may start at 120 mg (3 tablets) once a day on Week 1 (Days 1 to 7), followed by 160 mg (4 tablets) once a day on Week 2 (Days 8 to 14), and then 240 mg (6 tablets) once a day on Week 3 and onwards. Your doctor may adjust your dose as needed and tolerated.
      • Children—Use and dose must be determined by your doctor.

Missed dose

If you miss a dose of neratinib, skip the missed dose and go back to your regular dosing schedule. Do not double doses.


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 neratinib

It is very important that your doctor check your progress at regular visits to make sure neratinib is working properly. Blood tests may be needed to check for unwanted effects.

Using neratinib while you are pregnant can harm your unborn baby. If you are a woman who can get pregnant, your doctor may do tests to make sure you are not pregnant before starting treatment. Use an effective form of birth control to keep from getting pregnant during treatment with neratinib and for at least 1 month after your last dose. Male patients who have female partners should use effective birth control during treatment with neratinib and for 3 months after the last dose. If you think you have become pregnant while using neratinib, tell your doctor right away.

Check with your doctor right away if you 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.

Neratinib may cause severe diarrhea, which may lead to serious complications, including dehydration, low blood pressure (hypotension), or kidney failure. Your doctor will give you medicines to help prevent diarrhea during treatment with neratinib. If you have any questions about this or if diarrhea continues, or gets worse, check with your doctor.

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 (eg, St. John's wort) or vitamin supplements.

Neratinib side effects

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:

More common

  • Diarrhea

Less common

  • Confusion
  • decreased urination
  • dizziness
  • dry mouth
  • fainting
  • increase in heart rate
  • lightheadedness
  • rapid breathing
  • sunken eyes
  • thirst
  • unusual tiredness or weakness
  • wrinkled skin


  • Bloody urine
  • increased blood pressure
  • increased thirst
  • itching, pain, redness, swelling, tenderness, or warmth on the skin
  • loss of appetite
  • lower back or side pain
  • nausea
  • raised, firm, bright red patches of skin on the arm or leg
  • stomach pain
  • swelling of the face, fingers, or lower legs
  • trouble breathing
  • vomiting
  • 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:

More common

  • Belching
  • bladder pain
  • bloody nose
  • bloody or cloudy urine
  • decreased appetite
  • decreased weight
  • difficult, burning, or painful urination
  • discoloration of the fingernails or toenails
  • dry skin
  • frequent urge to urinate
  • heartburn
  • indigestion
  • muscle spasms
  • stomach discomfort, upset, or pain
  • swelling or inflammation of the mouth

Less common

  • Deep cracks, grooves, or lines in the skin
  • dry mouth

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.

Frequently asked questions

View more FAQ

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.