HALAVEN™ (eribulin mesylate) Injection

Mechanism of Action Exerts its effects via a tubulin-based antimitotic mechanism leading to G2/M cell-cycle block, disruption of mitotic spindles, and, ultimately, apoptotic cell death after prolonged mitotic blockage.
Pharmacodynamics (PD) Effect of HALAVEN on the QTc interval was assessed in patients with solid tumors received 1.4 mg/m2 of HALAVEN on Days 1 and 8 of a 21-day cycle. A delayed QTc prolongation was observed on Day 8, with no prolongation observed on Day 1. The maximum mean QTcF change from baseline (95% upper confidence interval) was 11.4 (19.5) ms.
Pharmacokinetics (PK) Linear PK with a mean elimination half-life of approximately 40 hours, a mean volume of distribution of 43 L/m2 to 114 L/m2 and mean clearance of 1.16 L/hr/m2 to 2.42 L/hr/m2 over the dose range of 0.25 mg/m2 to 4.0 mg/m2

 Eribulin eliminates primarily in feces as unchanged drug

 Human plasma protein binding ranged from 49% to 65%

 No accumulation observed with weekly administration

PK-PD Analysis Not evaluated
Population PK Gender, race, and age do not have a clinically meaningful effect on the PK of eribulin
Special Populations Lower starting dose of 1.1 mg/m2 is recommended for patients with moderate renal impairment
Drug Interactions No drug-drug interactions are expected with CYP system or P-gp

Source : http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/201532lbl.pdf


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