Information about Neratinib
Neratinib is an orally available tyrosine kinase receptor inhibitor that is used in the extended adjuvant therapy of early stage breast cancer.
Liver safety of Neratinib
Neratinib is associated with a low rate of transient elevations in serum aminotransferase levels during therapy, but has not been convincingly linked to cases of clinically apparent liver injury with jaundice.
Mechanism of action of Neratinib
Neratinib (ne ra' ti nib) is a small molecule tyrosine kinase receptor inhibitor with potent activity against human epidermal growth factor receptor 2 (HER2 or ErbB2). These tyrosine kinase receptors are often mutated and over expressed in tumor tissue and cause unregulated cell growth and proliferation. This mutation is present in 20% of breast cancers and is particularly overexpressed in early stage cancers. Inhibition of the unregulated receptor can lead to reversal of progression of the cancer, although clinical responses are sometimes limited by the development of tumor resistance caused by further mutations in the receptor gene. In several large controlled trials, adjuvant therapy with neratinib was shown to improve progression free survival in patients with early stage, HER2-positive breast cancer.
FDA approval information for Neratinib
Dosage and administration for Neratinib
Neratinib is available in tablets of 40 mg under the brand name Nerlynx. The recommended dose is 240 mg (6 tablets) once daily for one year or until intolerable toxicity occurs.
Side effects of Neratinib
Side effects are common and particularly diarrhea [95%], which can be severe and dose limiting and for which prophylaxis with antidiarrheal agents is recommended. Other frequent side effects include nausea, abdominal pain, anorexia, weight loss, abdominal distension, fatigue, rash, stomatitis, dry skin, paronychia, muscle spasms and urinary treat infections. Uncommon, but potentially severe side effects include severe diarrhea leading to dehydration and renal failure, and embryo-fetal toxicity.