Neratinib
Pronunciation: (neh-RAH-tih-nib).
- Generic name
- neratinib
- Brand names
- Nerabest, Nerlynx, Neratin
- Drug class
- Tyrosine kinase inhibitor (TKI), Antineoplastic agent
Availability and supply rules vary by country
Trade names by country: United States
Australia: · Full directory
What neratinib is and how it works
Uses, formulations, monitoring, and supply rules can differ by patient, product, and country. Follow the exact local product information and professional advice.
Mechanism of action: how neratinib works
Neratinib is an irreversible tyrosine kinase inhibitor that targets the human epidermal growth factor receptors HER1 (EGFR), HER2, and HER4. By binding covalently to these receptors, it blocks autophosphorylation and downstream signaling pathways (including MAPK and PI3K/AKT), inhibiting proliferation of tumor cells that overexpress HER2. (1)
What neratinib is used for
Neratinib is a prescription medicine used to treat adults with early-stage, HER2-positive breast cancer after they have completed treatment with trastuzumab-based therapy. It is also sometimes used for advanced or metastatic HER2-positive breast cancer in combination with other medicines. Neratinib works by blocking the activity of HER2 and other related proteins on cancer cells.
Extracted from the clinician-authored database description field (no separate structured indications list was present in the DB record for this medicine).
Before taking neratinib
Do not take / not appropriate for
- The US prescribing information for NERLYNX states plainly that there are no contraindications ("Section 4 Contraindications: None"). The European product information does list contraindications, which are set out below. (United States)
- Do not take neratinib if you are hypersensitive (allergic) to neratinib or to any of the excipients in the tablets. (European Union)
- Do not take neratinib together with strong inducers of CYP3A4/P-gp: carbamazepine or phenytoin (antiepileptics), St John’s wort (Hypericum perforatum), or rifampicin. These lower neratinib levels substantially. (European Union)
- Do not take neratinib if you have severe liver impairment (Child-Pugh C). (European Union)
- Neratinib should not be used during pregnancy unless your doctor judges that your condition requires it. Based on animal studies it can cause harm to an unborn baby, and it can cause fetal harm when given to a pregnant woman. (all countries)
Tell your clinician about
- Every other medicine, supplement and herbal product you take — including St John’s wort, antiepileptics, rifampicin, antifungals, some antibiotics, and medicines that reduce stomach acid (proton pump inhibitors, H2-blockers and antacids), all of which change neratinib levels.
- That you should avoid grapefruit and pomegranate, and their juices, which can raise neratinib levels.
- Any liver problem or abnormal liver blood tests; hepatotoxicity is a labelled warning and liver function is monitored during treatment.
- If you could become pregnant — highly effective contraception is required during treatment and for 1 month after the last dose, and a barrier method should be added if you use systemic hormonal contraception. Men should use barrier contraception during treatment and for 3 months after stopping.
- If you are breastfeeding — the US labelling advises not to breastfeed during treatment and for at least 1 month after the last dose.
- Diarrhoea, which is very common and can be severe: start the anti-diarrhoeal medicine your team prescribes with the very first dose of neratinib and report dehydration or persistent diarrhoea promptly.
How to take neratinib
- General Instructions: Take Neratinib exactly as prescribed by your doctor, usually once daily with food. Swallow the tablets whole with water.. Adult Dosing: The typical adult dose is 240 mg (six 40 mg tablets) taken orally once daily with food for 12 months.. Pediatric Dosing: Neratinib is not recommended for use in children or adolescents under 18 years of age.. Administration: Take at the same time each day with food. Do not crush, chew, or split the tablets.. When To Stop: Do not stop taking Neratinib without consulting your doctor. Treatment is usually continued for 12 months unless side effects require discontinuation.. Storage: Store at room temperature (20°C to 25°C/68°F to 77°F), away from moisture and heat. Keep out of reach of children.
- This page does not provide a dose calculator. Dosing must follow the prescriber, pharmacist, or product label.
Procedures and treatment changes
Tell the treating team before surgery, procedures, or any medicine change. Do not alter treatment without the responsible clinician.
Missed dose
If you miss a dose, take it as soon as you remember unless it is less than 12 hours until your next dose. If it is less than 12 hours, skip the missed dose and take your next dose at the regular time. Do not take two doses at once.
Overdose
If you take too much Neratinib, seek emergency medical attention or call your local poison control center immediately. Symptoms of overdose may include severe diarrhea, vomiting, and dehydration. Supportive care and monitoring are recommended.
Side effects
Side effects and their urgency vary; report severe, persistent, or concerning symptoms to a healthcare professional.
The most common side effect is diarrhea, which can be severe. Other frequent mild side effects include nausea, vomiting, abdominal pain, fatigue, rash, decreased appetite, and mouth sores.
Incidence: Reported in the clinician-authored database; frequency not established
Warning sign
What to notice: Severe or persistent diarrhea Signs of dehydration (dizziness, dry mouth, reduced urination) Yellowing of the skin or eyes (jaundice) Dark urine or pale stools Unusual bruising or bleeding
What to do: Seek immediate medical attention if you experience severe diarrhea with dehydration, signs of liver problems (jaundice, dark urine, upper right abdominal pain), severe allergic reactions (swelling, difficulty breathing), or severe skin reactions. (1)
Serious warnings
Severe diarrhea is common and can lead to dehydration — serious
Symptoms: Severe diarrhea is common and can lead to dehydration. Liver toxicity may occur; monitor liver function regularly. May cause harm to an unborn baby; use effective contraception. Drug interactions are possible, especially with acid-reducing agents. Not recommended for use in children.
Action: Follow the urgency stated and seek prompt or emergency care when indicated.
Contraindications recorded in the clinician database — serious
Symptoms: Contraindications recorded in the clinician database: Contraindicated in patients with known hypersensitivity to neratinib or any excipients. Use with caution in patients with hepatic impairment, as exposure is increased. Not recommended in severe hepatic impairment (Child-Pugh C). Monitor for severe diarrhea and hepatotoxicity. Not recommended in pediatric patients.
Action: Follow the urgency stated and seek prompt or emergency care when indicated.
Interactions
| Medicine or test | Effect | Action |
|---|---|---|
| Recorded interactions | Neratinib interacts with many medicines, especially those that affect stomach acid (such as proton pump inhibitors, H2 blockers, and antacids), as these can reduce its absorption. It is also metabolized by CYP3A4, so strong inhibitors or inducers of this enzyme (such as ketoconazole, rifampin, or certain anticonvulsants) may alter its effectiveness or increase side effects. Always inform your healthcare provider of all medicines and supplements you are taking. | (1) |
Pregnancy, breastfeeding, kidney/liver function, age
Pregnancy
Pregnancy Category D. Neratinib can cause fetal harm; use effective contraception during treatment.
Breastfeeding
It is not known if neratinib is excreted in human milk. Caution should be exercised when administered to a nursing woman.
Children
Frequency: Not applicable. Weight Based: Not recommended for pediatric use. Max Daily Dose: Not applicable. Max Single Dose: Not applicable. Age Restrictions: Safety not established in children
Renal_impairment
Renal impairment: No dosage adjustment is necessary for patients with renal impairment. Hepatic impairment: Reduce dose to 160 mg once daily in patients with moderate hepatic impairment (Child-Pugh B). Not recommended in severe hepatic impairment (Child-Pugh C). Elderly: No specific dosage adjustments are recommended based on age; however, monitor for increased sensitivity in elderly patients.
Hepatic_impairment
Renal impairment: No dosage adjustment is necessary for patients with renal impairment. Hepatic impairment: Reduce dose to 160 mg once daily in patients with moderate hepatic impairment (Child-Pugh B). Not recommended in severe hepatic impairment (Child-Pugh C). Elderly: No specific dosage adjustments are recommended based on age; however, monitor for increased sensitivity in elderly patients.
Monitoring
Storage
The clinician-authored database record does not specify storage conditions for this medicine. As an oral tablet, standard practice (consistent with other oral antineoplastic tablets) is to store at 20-25 degrees C (68-77 degrees F), away from moisture and heat, out of reach of children; follow the specific product's own label for confirmation.
Professional information
Clinician-facing context only. This section does not replace current product labeling.
General
Indication: Extended adjuvant treatment of early-stage HER2-positive breast cancer
Dose summary: 240 mg orally once daily, taken continuously.
Renal context: No dosage adjustment is necessary for patients with renal impairment. (1)
Frequently asked questions
What is Neratinib used for?
Neratinib is used to reduce the risk of breast cancer returning in adults with early-stage, HER2-positive breast cancer after completing trastuzumab-based therapy. It may also be used for advanced or metastatic HER2-positive breast cancer in combination with other medicines.
How should I take Neratinib?
Take Neratinib once daily with food, at the same time each day. Swallow the tablets whole with water. Do not crush, chew, or split the tablets.
What are the most common side effects?
The most common side effect is diarrhea, which can be severe. Other common side effects include nausea, vomiting, abdominal pain, fatigue, rash, and decreased appetite.
How can I manage diarrhea caused by Neratinib?
Your doctor may prescribe anti-diarrheal medicines such as loperamide to help prevent or manage diarrhea. It is important to start these medicines at the beginning of treatment and follow your doctor's instructions closely.
Can I take other medicines with Neratinib?
Some medicines can interact with Neratinib, especially those that affect stomach acid or are metabolized by CYP3A4. Always tell your doctor about all medicines and supplements you are taking.
Is Neratinib safe during pregnancy or breastfeeding?
Neratinib can harm an unborn baby and should not be used during pregnancy. Effective contraception is recommended during treatment and for at least 1 month after the last dose. Do not breastfeed while taking Neratinib and for at least 1 month after the last dose.
What should I do if I miss a dose?
If you miss a dose, take it as soon as you remember unless it is less than 12 hours until your next dose. If it is less than 12 hours, skip the missed dose and take your next dose at the regular time. Do not double up doses.
What happens if I take too much Neratinib?
Taking too much Neratinib can lead to an exacerbation of side effects, particularly severe diarrhea, nausea, vomiting, and fatigue. In cases of suspected overdose, it is crucial to seek immediate emergency medical attention. Do not attempt to induce vomiting or self-treat. Prompt medical evaluation is necessary to manage symptoms and provide supportive care.
Can I drink alcohol while taking Neratinib?
It is generally advisable to limit or avoid alcohol consumption while taking Neratinib. Alcohol can increase the risk of certain side effects, such as liver problems and gastrointestinal upset, which are also potential side effects of Neratinib. Discuss your alcohol intake with your healthcare provider to understand the specific risks and recommendations for your individual situation.
Is Neratinib safe during pregnancy?
Neratinib is generally not recommended during pregnancy due to potential risks to the fetus. It falls under a pregnancy category that indicates potential harm. If you are pregnant, planning to become pregnant, or breastfeeding, it is imperative to consult your healthcare provider immediately. They can discuss the risks and benefits and explore alternative treatment options or management strategies.
What is the mechanism of action of neratinib?
Neratinib is an irreversible tyrosine kinase inhibitor that targets the human epidermal growth factor receptors HER1 (EGFR), HER2, and HER4. By binding covalently to these receptors, it blocks autophosphorylation and downstream signaling pathways (including MAPK and PI3K/AKT), inhibiting proliferation of tumor cells that overexpress HER2. (1)
What is the generic name of Neratinib?
The generic name is neratinib. It is sold under brand names including Nerabest, Nerlynx, Neratin.
What class of drug is neratinib?
Neratinib is classed as: Tyrosine kinase inhibitor (TKI), Antineoplastic agent.
References
- MedGuideGlobal Clinician-Authored Medicine Record — Neratinib (internal Supabase medicines table)MedGuideGlobal · null · accessed 2026-08-07 · source 1
- NERLYNX (NERATINIB) TABLET [PUMA BIOTECHNOLOGY, INC.] — US prescribing information (DailyMed SPL)U.S. National Library of Medicine (DailyMed) · US · accessed 2026-08-14 · source 2
- Nerlynx — FDA approval record (Drugs@FDA NDA208051)U.S. Food and Drug Administration · US · accessed 2026-08-14 · source 3
- neratinib — RxNorm normalized drug concept (RXCUI 1940642)U.S. National Library of Medicine (RxNorm) · US · accessed 2026-08-14 · source 4
Brand names by country
Single-ingredient neratinib names are shown separately by country. Product availability, strengths, and supply rules can change; combination products are not included here.
Priority countries
United States
- Nerlynx40 mg · puma biotechnology, inc.