Neratinib

Neratinib (INN; trade name Nerlynx; development code HKI-272) is a tyrosine kinase inhibitor anticancer drug.RET inhibitors: Vandetanib (also VEGFR and EGFR). Entrectinib (ALK, ROS1, NTRK).c-MET inhibitor: Cabozantinib (also VEGFR2). Neratinib (INN; trade name Nerlynx; development code HKI-272) is a tyrosine kinase inhibitor anticancer drug. Neratinib is used as an adjuvant therapy in people with early stage breast cancer in which HER2 is overexpressed, after the person receives treatment with trastuzumab. People should be given drugs to prevent diarrhea when they are given neratinib. Women who are pregnant should not take it, and women should not become pregnant while taking it, and women who are breast-feeding should not use it, as it causes fetal harm. A clinical trial demonstrated that Neratinib and Temsirolimus in combination produced responses in 19% of patients ranging from 2 to 18+ months in patients with HER2-mutant lung cancers. A common toxicity, diarrhea was well-managed with loperamide prophylaxis. Neratinib can cause life-threatening diarrhea in some people and mild to moderate diarrhea in almost everyone; people who take it are also at risk for complications of diarrhea like dehydration and electrolyte imbalance. Similarly there is a risk of severe liver damage and many patients have some level of it; symptoms of liver damage include fatigue, nausea, vomiting, right upper quadrant pain or tenderness, fever, rash, and high levels of eosinophils. In addition to the above, more than 10% of people taking it have nausea, abdominal pain, vomiting, sores on their lips, stomach upset, decreased appetite, rashes, and muscle spasms. People taking neratinib should not also take gastric acid reducing agents including proton pump inhibitors and H2-receptor antagonists; antacids may be used three hours before of after taking it. Drugs that inhibit CYP3A4 increase the activity of neratinib and can make adverse effects worse, and drugs that induce CYP3A4 make neratinib less active and can reduce its efficacy. Neratinib also inhibits p-glycoprotein and effectively raises the dose of drugs like digoxin that depend on it for elimination.