Products
Neratinib was approved in the form of film-coated tablets in the United States in 2017, in the EU in 2018, and in many countries in 2020 (Nerlynx).
Structure and properties
Neratinib (C30H29ClN6O3, Mr = 557.1 g/mol) is present in the drug as neratinib maleate, a white to yellow powder that is water soluble, especially at an acidic pH. It is a 4-anilinoquinolide that was developed starting from the structurally closely related pelitinib.
Effects
Neratinib (ATC L01XE45) has antitumor and antiproliferative properties. Neratinib is a kinase inhibitor. Its effects are due to irreversible (noncompetitive) inhibition of epidermal growth factor receptor (EGFR, HER1), human epidermal growth factor receptor 2 (HER2), and HER4.
Indications
For extended adjuvant treatment of adult patients with hormone receptor-positive, HER2-overexpressed/amplified early-stage breast cancer whose prior trastuzumab-based adjuvant therapy has been completed for less than one year.
Dosage
According to the SmPC. Tablets are taken in the morning with breakfast for one year.
Contraindications
- Hypersensitivity
- Concurrent administration of strong inducers of CYP3A4 and P-glycoprotein.
- Concurrent administration of weak CYP3A4 and P-gp inhibitors.
- Severe hepatic insufficiency
- Pregnancy
Full precautions can be found in the drug label.
Interactions
Neratinib is a substrate of CYP3A4 and of FMO, and it is transported by P-glycoprotein.
Adverse effects
The most common potential adverse effects include diarrhea, nausea, fatigue, vomiting, abdominal pain, rash, loss of appetite, upper abdominal pain, stomatitis, and muscle cramps.
