Eribulin: rediscovering tubulin as an anticancer target.
Eribulin mesylate (E7389) is a synthetic analog of the marine macrolide halichondrin B, which acts as a novel microtubule modulator with a distinct mechanism of action. Two eribulin mesylate phase 1 studies exploring weekly and 3-weekly schedules are reported in this issue. These trials show linear pharmacokinetics, a toxicity profile consisting in neutropenia and fatigue, and early hints of antitumor activity. In this commentary we give a brief historical perspective of the halichondrins and put into context eribulin mesylate as a novel tubulin modulator.
Jimeno
Antonio
A
D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D017321:Clinical Trials, Phase I as Topic; D005663:Furans / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D006801:Humans; D007659:Ketones / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D014404:Tubulin / Q000378:metabolism*; D050257:Tubulin Modulators / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D000095662:Polyether Polyketides
D000970:Antineoplastic Agents; D005663:Furans; D007659:Ketones; D014404:Tubulin; D050257:Tubulin Modulators; C490954:eribulin; D000095662:Polyether Polyketides