Drug reference

Neratinib

Tyrosine Kinase Inhibitor · Targeted therapy responsive malignancy

Tyrosine Kinase InhibitorTargeted therapy responsive malignancy

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

AmprenavirSevereDatabaseDDInter
ApalutamideSevereDatabaseDDInter
AprepitantSevereDatabaseDDInter
AtazanavirSevereDatabaseDDInter

Mechanism

Neratinib is a tyrosine kinase inhibitor. It is a small molecule inhibitor of tyrosine kinases associated with EGFR, HER2, and HER4, resulting in inhibition of intracellular ErbB signaling.

Indications

HER2-overexpressed/amplified breast cancer (specialist use only)Breast cancerearly-stage HER2-positive breast cancer following trastuzumab–based therapy (as single agent)advanced or metastatic HER2-positive breast cancer after two or more anti-HER2–based regimens (in combination with capecitabine)Approved for use in early-stage breast cancerHigh-risk individuals who have completed a year of anti-HER2 therapy can consider addition of oral neratinib for another year (benefits are incremental)For metastatic HER2-positive breast cancer, small-molecule inhibitors may offer disease control as they cross into the central nervous system

Dosing

Adult: 240 mg once daily for 1 year, to be taken with food, preferably in the morning. If concurrent use of potent CYP3A4 inhibitors is unavoidable, reduce dose to 40 mg once daily.
Geriatric: Increased risk of complications of diarrhoea.

Pharmacokinetics

Half-life

7 to 17 h

Metabolism

Metabolized by CYP3A4

Contraindications

Cardiac risk factors or conditions which may affect left ventricular ejection fraction
Elderly (increased risk of complications of diarrhoea)
Significant, chronic gastro-intestinal disorder with diarrhoea as a major symptom (no clinical experience)

Side effects

Common

Appetite decreasedDehydrationDiarrhoeaDry mouthEpistaxisFatigueGastrointestinal discomfortIncreased risk of infectionMucositisMuscle spasmsNail discolourationNail disordersNauseaOral disordersSkin reactionsVomitingWeight decreaseddiarrhea (most common and frequent, grade 3 or 4 in over one-third of patients)

Serious