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Synonyms: HKI 272 | HKI-272 | Nerlynx®
neratinib is an approved drug (FDA (2017), EMA (2018))
Compound class: Synthetic organic
Comment: Neratinib is an irreversible inhibitor of the receptor tyrosine kinase (RTK), ErbB2 . It also inhibits the related RTK, EGFR.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|No information available.|
|Summary of Clinical Use|
|In July 2017 the FDA granted marketing approval for neratinib's use as an extended adjuvant treatment of early-stage, HER2-positive breast cancer, in patients previously treated with drugs including trastuzumab. Neratinib therapy lowers the risk of cancer recurrence in this patient group. EMA approval followed in August 2018. Visit ClinicalTrials.gov to view currently registered neratinib trials.
Neratinib is one of the drugs being assessed in a new type of clinical trial, called adaptive trials being performed as part of the public/private partnership I-SPY trials which aim to streamline drug testing by targeting drugs to patients by assessing their cancer-specific genetic markers, so that the most useful drugs are used in those patients most likely to respond to them. The I-SPY trials are 'adaptive' in the sense that early data from current patients is used to guide treatment regimens for the next patients entering the trial. It is hoped that this more thoughtful and flexible trial framework will expedite identification of drugs and drug combinations with the most positive outcome in those patients in most need. Positive results from an I-SPY 2 trial (Phase 2) of neratinib in HER2-positive, hormone-receptor-negative breast cancer were reported in 2016 .
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT01808573||A Study of Neratinib Plus Capecitabine Versus Lapatinib Plus Capecitabine in Patients With HER2+ Metastatic Breast Cancer Who Have Received Two or More Prior HER2 Directed Regimens in the Metastatic Setting||Phase 3 Interventional||Puma Biotechnology, Inc.||Neratinib + capecitabine was FDA approved in February 2020 for patients indicated by results from this trial. This drug combination has emerged as an effective regimen for the management of HER2+ve metastatic breast cancer patients with brain metastasis.||2|
For extended ADME data see the following:
European Medicines Agency (EMA)