Eribulin mesylate pharmacokinetics in patients with hepatic impairment.

Witteveen, P.; Marchetti, Serena; Mergui-Roelvink, Marja; Reyderman, Larisa; Copalu, William; Wanders, J.; Jenner, A.; Edwards, G.; Schellens, Jan H.M.; Voest, Emile E.

doi:10.1200/jco.2010.28.15_suppl.2582

Cited by 16 publications

(12 citation statements)

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“…Therefore, a specific Phase I and pharmacokinetic trial was carried out in patients with normal liver function and in those with mild-to-moderate hepatic impairment (as defined by Child-Pugh criteria). 40 Eribulin could be administered at 1.4 mg/m 2 if hepatic function was normal, and at 1.1 mg/m 2 and 0.7 mg/m 2 if hepatic dysfunction was mild-to-moderate, respectively. Compared with those having normal liver function, exposure to eribulin (as reflected by the area under the concentration-time curve), increased 1.7-fold and 2.8-fold in patients with mild and moderate liver dysfunction, respectively.…”

Section: -39mentioning

confidence: 99%

Eribulin (Halaven): a new, effective treatment for women with heavily pretreated metastatic breast cancer

Menis

Twelves

2011

BCTT

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Although metastatic breast cancer remains essentially incurable, many patients previously treated with an anthracycline, taxane, and capecitabine are relatively fit and keen to receive further therapy. Several drugs are used in this setting, but with little evidence of clinically relevant benefit, and none have previously shown improved survival. Eribulin (Halaven ® ) is a nontaxane tubulin-binding agent with a novel mode of action, and was recently approved by the European Medicines Agency and US Food and Drug Agency as a single agent for patients with heavily pretreated metastatic breast cancer. This review provides an overview of the discovery, and preclinical and clinical development of eribulin, culminating in the recently published EMBRACE metastatic breast cancer study.

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Section: -39mentioning

confidence: 99%

Eribulin (Halaven): a new, effective treatment for women with heavily pretreated metastatic breast cancer

Menis

Twelves

2011

BCTT

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“…In addition, this agent has a long terminal half-life of up to 48 h after administration and shows low renal clearance [18][19][20][21]. Although systemic exposure to eribulin increased in patients with hepatic impairment, it was generally safe and well tolerated [28]. Co-administration of ketoconazole, a CYP3A4 inhibitor, had no statistically significant effect upon eribulin pharmacokinetics following single-dose exposure [29].…”

Section: Phase 1 Clinical Trialsmentioning

confidence: 96%

The Place for Eribulin in the Treatment of Metastatic Breast Cancer

Gradishar

2010

Curr Oncol Rep

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Treatment of metastatic breast cancer (MBC) remains one of the major challenges in cancer care. Chemotherapeutic agents currently approved for the treatment of invasive disease may exhibit initial efficacy; however, the development of resistance to therapy and concerns over tolerability are common and generally limit treatment options available to physicians and patients. Novel chemotherapeutic agents are, therefore, necessary to increase survival, delay disease progression, and improve tolerability. Eribulin mesylate (E7389) is a novel microtubule dynamics inhibitor with a unique mechanism of action that has shown antitumor efficacy and a manageable tolerability profile in clinical trials. Importantly, eribulin is the only single agent to date that has been shown to prolong overall survival in patients with heavily pretreated MBC. This review will discuss eribulin, with focus on the potential it has to address the specific treatment needs of patients with MBC who are refractory to conventional chemotherapies.

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“…Hepatic impairment decreases its clearance and extends its elimination half-life. Yet treatment remains well tolerated [20]. No formal pharmacokinetic trials have been conducted in patients with renal impairment.…”

Section: Pharmacokinetics and Metabolismmentioning

confidence: 99%