ArticleBritish journal of clinical pharmacology2013
Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin.
Article in British journal of clinical pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 28 citations in OpenAlex.
- Article
- Article
- Eribulin, Child-Pugh score, and liver-function tests: lessons from pivotal breast cancer studies 301 and 305.Breast cancer research : BCR · 2021Article
- Marine-Derived Anticancer Agents: Clinical Benefits, Innovative Mechanisms, and New Targets.Marine drugs · 2019Review
- Phase I dose-finding study of eribulin and capecitabine for metastatic breast cancer: JBCRG-18 cape study.Breast cancer (Tokyo, Japan) · 2018Article
- Primary Culture of Undifferentiated Pleomorphic Sarcoma: Molecular Characterization and Response to Anticancer Agents.International journal of molecular sciences · 2017Article
- Integrating mechanisms of response and resistance against the tubulin binding agent Eribulin in preclinical models of osteosarcoma.Oncotarget · 2016Article
- Activity of Eribulin in a Primary Culture of Well-Differentiated/Dedifferentiated Adipocytic Sarcoma.Molecules (Basel, Switzerland) · 2016Article
- Eribulin in Cancer Treatment.Marine drugs · 2015Review
- Population pharmacokinetic-pharmacodynamic analysis for eribulin mesilate-associated neutropenia.British journal of clinical pharmacology · 2013Article
- Initial testing (stage 1) of eribulin, a novel tubulin binding agent, by the pediatric preclinical testing program.Pediatric blood & cancer · 2013Article
Corrections and comments
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Authors and funding
13 authors at 7 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimEribulin mesylate is a non-taxane microtubule dynamics inhibitor that was recently approved for treatment of metastatic breast cancer. The aim of this study was to determine the effect of rifampicin, a CYP3A4 inducer, on the plasma pharmacokinetics of eribulin in patients with solid tumours.
methodsAn open-label, non-randomized phase I study was carried out. Patients received intravenous 1.4 mg m(-2) eribulin mesylate on days 1 and 15 and oral rifampicin 600 mg on days 9 to 20 of a 28 day cycle. Pharmacokinetic sampling for determination of eribulin plasma concentrations was performed up to 144 h following administration. AUC(0,∞) and C(max) for eribulin exposure without or with co-administration of rifampicin were subjected to an analysis of variance (anova) and corresponding 90% confidence intervals (CI) were calculated. Subsequently, patients were allowed to continue eribulin mesylate treatment with 1.4 mg m(-2) eribulin mesylate on days 1 and 8 of a 21 day cycle. Also the adverse event profile and anti-tumour activity were assessed.
resultsFourteen patients were included and 11 patients were evaluable for pharmacokinetic analysis. Co-administration of rifampicin had no effect on single dose exposure to eribulin (geometric least square means ratio: AUC(0,∞) = 1.10, 90% CI 0.91, 1.34 and C(max) = 0.97, 90% 0.81, 1.17). The most common treatment-related grade ≥3 adverse events were grade 3 neutropenia (4/14, 29%), leucopenia and fatigue (both 3/14, 21%).
conclusionsThese results indicate that eribulin mesylate may be safely co-administered with compounds that are CYP3A4 inducers.
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