Eribulin Mesylate

Abstract

Eribulin mesylate, a nontaxane, completely synthetic microtubule inhibitor, has recently been approved by the U.S. Food and Drug Administration as third-line treatment of metastatic breast cancer refractory to anthracyclines and taxanes. Eribulin is a synthetic analogue of halichondrin B, which inhibits microtubule polymerization by a mechanism distinct from other available antitubulin agents. Eribulin significantly increased overall survival (OS; median OS for the eribulin-treated group was 13.1 months versus 10.6 months for the group treated by investigator's choice) in a heavily pretreated metastatic breast cancer population. Eribulin has a manageable side-effect profile, notably neutropenia and fatigue, and a relatively low incidence of peripheral neuropathy. The mechanism of action, pharmacokinetics, preclinical antitumor activity, and clinical trials of eribulin in the metastatic breast cancer setting are reviewed here. Clin Cancer Res; 17(21); 6615-22. Ó2011 AACR.

Advances in emerging drugs for osteosarcoma

“…Eribulin mesylate proved to inhibit cancer cell proliferation at nanomolar concentrations and showed a favorable pharmacokinetic and pharmacodynamic profile in comparison to other microtubule inhibitors, such as vinca alkaloids and taxanes [106]. Eribulin mesylate showed activity in human OS xenograft models [107], and it is presently under clinical evaluation in patients with recurrent or refractory OS inside a Phase II trial ( Table 1).…”

Eribulin as a Feasible and Safe Monotherapy in a Dialytic Pretreated Woman with Metastatic Breast Cancer: A Case Report

“…Renal excretion is minimal, with 5-11% of the administered dose eliminated in the urine. To our knowledge, no literature data are available on the use of eribulin in dialytic patient settings [11]. This case report is emblematic because of the use of eribulin in the second-line setting in a dialytic and cardiopathic patient with both anthracycline and capecitabine contraindications.…”

Selected hybrid natural products as tubulin modulators

“…Moreover, it also promotes the centromere spindle relaxation without affecting the rate of stretching [49]. Several biochemical apoptosis-related studies, like cytochrome c release from mitochondria, activation of caspase-3 and -9 cleavage of PARP, including phosphorylation of Bcl-2 in eribulin treated human lymphoma and prostate cancer cell were also undertaken [50].…”