Neratinib

(Nerlynx®)

Neratinib

Drug updated on 12/11/2024

Dosage FormTablets (oral; 40 mg)
Drug ClassKinase inhibitors
Ongoing and
Completed Studies
ClinicalTrials.gov

Indication

  • Indicated as a single agent, for the extended adjuvant treatment of adult patients with early-stage HER2-positive breast cancer, to follow adjuvant trastuzumabbased therapy
  • Indicated in combination with capecitabine, for the treatment of adult patients with advanced or metastatic HER2-positive breast cancer who have received two or more prior anti-HER2 based regimens in the metastatic setting.

Latest News

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Summary
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  • This summary is based on the review of seven systematic review(s)/meta-analysis(es). [1-7]
  • Tucatinib combined with trastuzumab and capecitabine (TTC) demonstrated an ORR of 47.3% in patients with human epidermal growth factor receptor 2-positive (HER2+) metastatic breast cancer and brain metastases. Trastuzumab deruxtecan (T-DXd) achieved a pooled overall response rate (ORR) of 64% (95% confidence interval (CI): 43-85%) in heavily pretreated patients with asymptomatic brain metastases, outperforming other therapies like lapatinib and capecitabine, which had a higher risk of bias.
  • For progression-free survival (PFS) and overall survival (OS), tucatinib plus trastuzumab with capecitabine ranked highest, showing superior outcomes compared to other HER2-directed therapies in unresectable or metastatic HER2+ breast cancer. T-DXd ranked first for PFS (hazard ratio (HR) 0.17; 95% credible interval (CrI) 0.03-0.82), while ado-trastuzumab emtansine (T-DM1) ranked first for OS in patients with HER2+ breast cancer brain metastases.
  • In early HER2+ breast cancer, trastuzumab-based dual anti-HER2 therapy, especially when combined with pertuzumab, significantly improved event-free survival (EFS) and OS, with pronounced benefits seen in lymph node-positive subgroups.
  • Trastuzumab-based dual anti-HER2 therapy was associated with a higher risk of cardiotoxicity, particularly when combined with pertuzumab (the surface under the cumulative ranking (SUCRA) of 92%), whereas lapatinib-containing regimens showed more general toxicity but no significant increase in cardiotoxicity.
  • Neratinib-containing regimens were generally well-tolerated but showed no significant safety concerns compared to other HER2-targeted therapies, particularly in the management of CNS disease progression.
  • There is no population types or subgroups information available in the reviewed studies.

Product Monograph / Prescribing Information

Document TitleYearSource
Nerlynx (neratinib) Prescribing Information.2022Puma Biotechnology, Inc., Los Angeles, CA

Systematic Reviews / Meta-Analyses

Clinical Practice Guidelines