Eribulin mesylate for the treatment of late-stage breast cancer

Gourmelon, Carole; Frenel, Jean-Sébastien; Campone, Mario

doi:10.1517/14656566.2011.637490

Cited by 17 publications

(13 citation statements)

References 23 publications

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“…It acts differently from other tubulin-targeted agents, like taxanes and vinca alkaloids. Eribulin inhibits microtubule growth without shortening them, and aggregates soluble tubulin in a nonproductive form [5]. This mechanism of action leads to irreversible mitosis arrest and finally to apoptosis.…”

Section: Introductionmentioning

confidence: 99%

Predictive Factors of Eribulin Activity in Metastatic Breast Cancer Patients

et al. 2018

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Objectives: Predictive factors of response to eribulin are lacking. We aimed to investigate the activity and safety of eribulin in a real-world population of metastatic breast cancer (MBC) patients and to identify possible predictive factors of progression-free survival (PFS) and objective response. Methods: We retrospectively analyzed 71 eribulin-treated MBC patients. Best response rate, PFS, and adverse events (AEs) were evaluated. The impact of different clinical-pathological factors on PFS was evaluated using the Cox proportional hazards model. Predictive factors of response were identified by discriminant function analysis (DFA). Results: Median PFS was 3.75 months (95% CI, 2.39–4.48); 12 patients (16.90%) achieved partial response (PR), 27 (38.03%) stable disease. The most common AEs were fatigue (25.83%), neutropenia (16.56%), and peripheral neuropathy (13.91%). A worse performance status (p = 0.025) and a higher number of metastatic organ sites (p = 0.011) were associated with a worse PFS under eribulin. Overall, in the DFA-predictive model, neutrophil-to-lymphocyte ratio at baseline, estrogen receptor, Ki67, histology, and age were predictive of PR with 100% accuracy. Conclusions: Activity and safety profiles of eribulin were consistent with literature data. Performance status and number of metastatic sites were predictive factors of PFS. DFA could be a promising tool to discriminate responses to eribulin among MBC patients.

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Section: Introductionmentioning

confidence: 99%

Predictive Factors of Eribulin Activity in Metastatic Breast Cancer Patients

et al. 2018

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“…Among the 5 hit drugs, eribulin is most recently approved with the indication of metastatic breast cancer [12][13][14] and malignant soft tissue sarcoma. 30) Eribulin is now attracting a lot of attention because of its high clinical efficacy against advanced breast cancer.…”

Section: Discussionmentioning

confidence: 99%

“…The fifth one was eribulin, a recently approved drug with the indication of advanced breast cancer. [12][13][14] This is the first study to report that vinorelbine, vindesine and eribulin induces Golgi-disruption. Intriguingly, the primary target of the 5 drugs is tubulin polymerization.…”

Section: Introductionmentioning

confidence: 92%

Discovery of Inhibitors of Membrane Traffic from a Panel of Clinically Effective Anticancer Drugs

Kamata

Sadahiro

Yamori

2019

Biological & Pharmaceutical Bulletin

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In addition to their major targets, clinically effective drugs may have unknown off-targets. By identifying such off-targets it may be possible to repurpose approved drugs for new indications. We are interested in the Golgi apparatus as a novel target for cancer therapy, but there is a paucity of candidate Golgi-disrupting drugs. Here, we aimed to identify Golgi-disrupting compounds from a panel of 34 approved anticancer drugs by using HBC-4 human breast cancer cells and immunofluorescence microscopy to visualize the Golgi apparatus. The screen identified five drugs having Golgi-disrupting activity. Four of them were vinca alkaloids (vinorelbine, vindesine, vincristine and vinblastine), and the fifth drug was eribulin. This is the first study to demonstrate that vinorelbine, vindesine and eribulin possess Golgi-disrupting activity. The 5 drugs are known to inhibit tubulin polymerization and to induce microtubule depolymerization. Interestingly, a microtubule-stabilizer paclitaxel did not induce Golgi-disruption, suggesting that the three-dimensionally preserved microtubules are partly responsible for maintaining the Golgi complex. Concerning eribulin, a noteworthy drug because of its high clinical efficacy against advanced breast cancer, we further confirmed its Golgi-disrupting activity in 3 different human breast cancer cell lines, BSY-1, MDA-MB-231 and MCF-7. Golgi-disruption may contribute to anticancer efficacy of eribulin. In conclusion, the present study revealed that 4 vinca alkaloids and eribulin possessed potential Golgi-disrupting activity among a panel of 34 approved anticancer drugs. Other drugs covering various molecular-targeted drugs and classical DNA-damaging drugs showed no Golgi-disrupting effect. These results suggest that tubulin polymerization-inhibitors might be promising candidate drugs with Golgi-disrupting activity.

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“…It is the third single-agent chemotherapy that has improved OS (after anthracycline and taxane) in advanced breast cancer. [51] The US FDA has approved eribulin mesylate as a third-line for MBC refractory to anthracyclines and taxanes. Its unique mechanism of action enhances its ability to overcome chemo-resistance.…”

Section: Adverse Effectsmentioning

confidence: 99%

Eribulin mesylate: A new therapeutic option for metastatic breast cancer

Aditya

2013

J Basic Clin Reprod Sci

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More than a million women are diagnosed with breast cancer annually worldwide. Death from breast cancer is usually a result of chemotherapy-resistant metastatic disease. Eribulin mesylate is a recent addition to the therapeutic armamentarium for treating locally advanced or metastatic breast cancer (MBC) in patients who have received at least two prior chemotherapy regimens for late-stage disease. This synthetic analog, derived from a marine sponge macrolide halichondrin B, inhibits microtubule stability by blocking microtubule growth without affecting microtubule shortening. The US Food and Drug Administration has approved eribulin mesylate as a third-line treatment for MBC refractory to anthracyclines and taxanes based on a Phase III clinical trial showing significantly increased overall survival compared to treatment of investigator's. Asthenia, fatigue, neutropenia, alopecia, nausea, anorexia, and neuropathy are the most frequent adverse effects associated with this drug. The aim of this review was to highlight the importance of this drug in the management of breast cancer. Medline, Excerpta Medica database, cochrane database, medscape, Elsevier Scopus, and clinicaltrials.gov were searched using terms "eribulin," "E7389," "halichondrin," "metastatic breast cancer." Journal articles published from 2007 to 2012 discussing pharmacology and/or clinical trials were screened. The development of this microtubule inhibitor helps to address the need for additional effective regimens for patients progressing after standard treatment with anthracycline-and taxane-containing regimens.

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Eribulin mesylate for the treatment of late-stage breast cancer

Cited by 17 publications

References 23 publications

Predictive Factors of Eribulin Activity in Metastatic Breast Cancer Patients

Predictive Factors of Eribulin Activity in Metastatic Breast Cancer Patients

Discovery of Inhibitors of Membrane Traffic from a Panel of Clinically Effective Anticancer Drugs

Eribulin mesylate: A new therapeutic option for metastatic breast cancer

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