{"entity":{"id":"neratinib","kind":"drug","name":"Neratinib","aka":[],"tldr":"A pill taken for a year after trastuzumab to further reduce recurrence in HER2-positive, hormone-positive breast cancer, limited by severe diarrhoea.","summary":"ExteNET: extended adjuvant neratinib for 1 year after trastuzumab improved 5-year iDFS (90.2% vs 87.7%, HR 0.73), with benefit concentrated in HR+ disease that started within a year of trastuzumab. NALA (with capecitabine, metastatic): PFS HR 0.76 and fewer CNS interventions. Grade 3 diarrhoea ~40% without prophylaxis; loperamide prophylaxis or dose escalation (CONTROL) mitigates it.","status":"approved","asOf":"2026-09-07","wikipedia":"https://en.wikipedia.org/wiki/Neratinib","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Neratinib"}],"tags":[],"related":[],"cancers":["breast-her2-positive","her2-positive-breast-brain-metastases"],"sections":[],"technologies":["kinase-inhibitors","her2-tyrosine-kinase-inhibitors"],"targets":["her2","egfr"],"drugs":[],"companies":["puma-biotechnology"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Nerlynx","modality":"Small-molecule irreversible pan-HER kinase inhibitor","mechanism":"Irreversible covalent inhibitor of HER1/HER2/HER4 kinases.","approvals":[{"region":"US","year":2017,"indication":"Extended adjuvant HER2+ early breast cancer after trastuzumab"},{"region":"US","year":2020,"indication":"HER2+ metastatic breast cancer with capecitabine after ≥2 anti-HER2 regimens"}],"mechanismSteps":[],"dosing":{"route":"Oral","schedule":"240 mg once daily with food for 1 year (adjuvant); with capecitabine in metastatic","modifications":"Dose escalation (120→160→240 mg) over 2 weeks; loperamide prophylaxis","monitoring":"Diarrhoea, liver enzymes"},"toxicity":[{"event":"Diarrhoea","anyGradePct":95,"grade3PlusPct":40,"note":"without prophylaxis; ~15% grade 3 with escalation"},{"event":"Nausea","anyGradePct":43},{"event":"Fatigue","anyGradePct":27}],"access":[],"regulatoryEvents":[]},"route":"/drugs/neratinib/","neighbours":{"cancer":[{"id":"her2-mutant-nsclc","kind":"cancer","name":"HER2-mutant non-small-cell lung cancer","route":"/cancers/her2-mutant-nsclc/"},{"id":"breast-her2-positive","kind":"cancer","name":"HER2-positive breast cancer","route":"/cancers/breast-her2-positive/"},{"id":"her2-positive-breast-brain-metastases","kind":"cancer","name":"HER2-positive breast cancer with brain metastases","route":"/cancers/her2-positive-breast-brain-metastases/"}],"technology":[{"id":"her2-tyrosine-kinase-inhibitors","kind":"technology","name":"HER2 tyrosine kinase inhibitors","route":"/technologies/her2-tyrosine-kinase-inhibitors/"},{"id":"kinase-inhibitors","kind":"technology","name":"Small-molecule kinase inhibitors","route":"/technologies/kinase-inhibitors/"}],"target":[{"id":"egfr","kind":"target","name":"EGFR","route":"/targets/egfr/"},{"id":"her2","kind":"target","name":"HER2","route":"/targets/her2/"},{"id":"erbb4","kind":"target","name":"HER4 (ERBB4)","route":"/targets/erbb4/"}],"company":[{"id":"puma-biotechnology","kind":"company","name":"Puma Biotechnology","route":"/companies/puma-biotechnology/"}],"term":[{"id":"her2-brain-metastases","kind":"term","name":"HER2-positive brain metastases","route":"/terms/her2-brain-metastases/"}],"trial":[{"id":"i-spy-2","kind":"trial","name":"I-SPY 2","route":"/trials/i-spy-2/"},{"id":"intuitt-nf2","kind":"trial","name":"INTUITT-NF2","route":"/trials/intuitt-nf2/"},{"id":"nala","kind":"trial","name":"NALA","route":"/trials/nala/"},{"id":"plasmamatch","kind":"trial","name":"plasmaMATCH","route":"/trials/plasmamatch/"},{"id":"safir-abc10","kind":"trial","name":"SAFIR-ABC10","route":"/trials/safir-abc10/"},{"id":"nct06813079","kind":"trial","name":"Using Tumor Models to Determine Treatments","route":"/trials/nct06813079/"}],"biomarker":[{"id":"her2-ihc-3-plus","kind":"biomarker","name":"HER2 IHC 3+ (HER2-positive by immunohistochemistry)","route":"/biomarkers/her2-ihc-3-plus/"}],"pathway":[{"id":"breast-cancer-signalling","kind":"pathway","name":"Breast cancer (KEGG map)","route":"/pathways/breast-cancer-signalling/"}]}}