Drug updated on 3/28/2024
| Dosage Form | Tablet (oral: 40 mg) |
| Drug Class | Kinase inhibitors |
| Ongoing and Completed Studies | ClinicalTrials.gov |
Indication
- For the extended adjuvant treatment of adult patients with early-stage HER2-positive breast cancer, to follow adjuvant trastuzumab-based 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.
Summary
- Neratinib maleate (Nerlynx) is indicated for the extended adjuvant treatment of adult patients with early-stage HER2-positive breast cancer, following adjuvant trastuzumab-based therapy. It's also used in combination with capecitabine for treating advanced or metastatic HER2-positive breast cancer in adults who have received two or more prior anti-HER2 based regimens.
- According to a systematic review/meta-analysis, neratinib combined with trastuzumab showed an objective response rate (ORR) of 26% and when combined with fulvestrant it had an ORR of 25%. However, as monotherapy neratinib only achieved an ORR of 16%, indicating that its efficacy may be enhanced when used in combination therapies.
- In terms of safety profile, diarrhea was identified as the most common adverse event associated with neratinib use across multiple studies; however this can be mitigated by prophylactic loperamide according to one study.
- A meta-analysis revealed that while neratinib demonstrated promising clinical activity as monotherapy against HER2-positive breast cancer, its effect was less significant among those patients having HER-mutated breast cancers suggesting potential limitations on patient population type.
- The information provided is derived from seven systematic reviews/meta-analyses which included data from both single-arm clinical studies and randomized controlled trials involving heavily pretreated patients who had received multiple lines of therapy previously.
- One analysis suggested that despite being associated with higher frequency adverse events such as diarrhea which are mostly tolerable; survival outcomes were generally improved under Nerlynx treatments especially when combined other anticancer agents making it potentially beneficial for treating central nervous system metastases related to breast cancer.
Product Monograph / Prescribing Information
| Document Title | Year | Source |
|---|---|---|
| Nerlynx (neratinib maleate) Prescribing Information | 2022 | Puma Biotechnology, Inc., Los Angeles, CA |
Systematic Reviews / Meta-Analyses
Clinical Practice Guidelines
| Document Title | Year | Source |
|---|---|---|
| Systemic therapy for advanced human epidermal growth factor receptor 2–positive breast cancer: ASCO guideline update. | 2022 | Journal of Clinical Oncology |
| Selection of optimal adjuvant chemotherapy and targeted therapy for early breast cancer: ASCO clinical practice guideline focused update. | 2018 | Journal of Clinical Oncology |