Objective: To review the chemistry, pharmacology, pharmacokinetics, safety, and efficacy of eribulin (Halaven).
Data sources: A literature search (up to December 2011) using the terms eribulin, Halaven, ER-086526, and E7389 was performed with PubMed, Google Scholar, selected Ovid bibliography searches, and the abstract search tool from the American Society of Clinical Oncology Annual Meetings and the San Antonio Breast Cancer Symposia. Additional references from the bibliographies of these articles were also assessed.
Data extraction: English-language preclinical and clinical studies on the chemistry, pharmacology, pharmacokinetics, safety, and efficacy of eribulin were reviewed.
Data synthesis: Eribulin is a novel microtubule inhibitor with a unique mechanism of action, which involves interaction with a distinct binding site on β-tubulin leading to G(2)/M phase cell-cycle arrest and apoptosis. Eribulin has been approved by the Food and Drug Administration for the treatment of metastatic breast cancer in patients who have been previously treated with an anthracycline and a taxane. In a pivotal Phase 3 study conducted in patients with metastatic breast cancer, eribulin 1.4 mg/m(2), administered over 2-5 minutes as an intravenous infusion on days 1 and 8 of 21-day cycles, was associated with a significantly increased median overall survival of 13.1 months compared to the median overall survival of 10.6 months in the therapy of physician's choice. Eribulin has also shown activity in Phase 2 studies in other types of cancers, such as non-small cell lung cancer, prostate cancer, urothelial cancer, soft tissue sarcomas, and platinum-susceptible ovarian, fallopian tube, or peritoneal cancers. The most severe (grade 3/4) adverse effects associated with eribulin include neutropenia, leukopenia, and peripheral neuropathy. Common toxicities include fatigue, neutropenia, alopecia, anemia, and peripheral neuropathy.
Conclusions: Eribulin is a promising new cytotoxic chemotherapy agent due to its ability to treat cancers that are refractory or resistant to other drugs as well as its manageable toxicity profile.