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The role of neratinib in HER2-driven breast cancer

Mathew A Cherian1, Cynthia X Ma1

  • 1Division of Oncology, Department of Medicine, Washington University in Saint Louis, St Louis, MO 63110, USA.

Future Oncology (London, England)
|July 1, 2017
PubMed

Insights

Neratinib shows promise for treating early-stage and metastatic HER2+ breast cancer, including HER2-mutated cases resistant to current therapies. This irreversible HER kinase inhibitor offers new hope for patients with limited treatment options.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • A significant percentage of early-stage HER2-positive breast cancer patients relapse despite trastuzumab therapy.
  • Most patients with metastatic HER2-positive breast cancer develop treatment resistance.
  • Activating HER2 mutations in HER2-negative breast cancer are not currently targeted by HER2-directed therapies.

Purpose of the Study:

  • To evaluate the potential role of neratinib in treating various HER2-related breast cancer scenarios.
  • To explore neratinib's efficacy in trastuzumab-resistant metastatic HER2+ breast cancer.
  • To assess neratinib's activity in HER2-mutated breast cancers.

Main Methods:

  • Phase III trial of neratinib as extended adjuvant therapy post-trastuzumab.
  • Phase II trials investigating neratinib in combination with cytotoxic agents for metastatic HER2+ breast cancer.
  • Phase II trials assessing neratinib monotherapy or in combination with fulvestrant for HER2-mutated breast cancers.

Main Results:

  • Neratinib demonstrated activity in extended adjuvant therapy in a Phase III trial.
  • Phase II trials showed promising activity of neratinib in trastuzumab-resistant metastatic HER2+ breast cancer.
  • Neratinib exhibited activity as monotherapy or with fulvestrant in HER2-mutated breast cancers.

Conclusions:

  • Neratinib is an irreversible HER kinase inhibitor with demonstrated efficacy in multiple HER2-related breast cancer settings.
  • Neratinib offers a potential therapeutic option for patients with early-stage disease, metastatic disease resistant to trastuzumab, and HER2-mutated breast cancers.
  • Further investigation and application of neratinib are anticipated for these challenging patient populations.
Keywords:
HER2adjuvant therapybreast cancerneratinibtyrosine kinase inhibitor

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