Table 1.

Notable features of eribulin mesylate (E7389).

Anti-cancer mechanism

Synthetic macrocyclic ketone analog of the marine natural product halichondrin B

Binds to tubulin and microtubules inducing mitotic arrest

Regulatory clearance

Approved by the Japanese authority in May 2010, the US FDA in November 2010, and the EMA in March 2011, and reimbursed by the Taiwan National Health Insurance since December 2014 Recommended dose for eribulin mesylate is 1.4 mg/m2 (equivalent to 1.23 mg/m2 eribulin) intravenously over 2–5 min on days 1 and 8 of a 3-week cycle

Pharmacokinetic and pharmacodynamic characteristics

Reduced doses of 1.1 and 0.7 mg/m2 are recommended for patients with Child–Pugh grades A and B, respectively10 Eliminated in feces with limited chemical modification; renal clearance represents <10% of clearance Grade 3 peripheral neuropathy 5% (no grade 4 toxicity)

Higher rates of neutropenia in Korean (88.5%; grade 3/4: 86.5%)14 and Japanese patients (grade 3/4: 95.1%);13 these rates may apply to all East Asian patients

No clinical concerns regarding minor prolongation of cardiac repolarization (QTc)11