Halaven Drug Interactions

No drug-drug interactions are expected with CYP3A4 inhibitors, CYP3A4 inducers or P-gp inhibitors. The effect of ketoconazole, a strong inhibitor of CYP3A4 and a P-gp inhibitor, on the pharmacokinetics of eribulin was studied in an open-label, two-treatment, two-sequence, two-way crossover trial in 12 patients with advanced solid tumours. The mean dose-normalized AUC values were similar when eribulin was administered with or without ketoconazole (ratio of the mean AUC: 0.97; 90% CI: 0.83, 1.12). Eribulin exposure (AUC and C_max) was also unaffected by rifampicin, a CYP3A4 inducer.
Eribulin does not inhibit CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 or CYP3A4 enzymes or induce CYP1A2, CYP2C9, CYP2C19 or CYP3A4 enzymes at relevant concentrations. Eribulin is not expected to alter the plasma concentrations of drugs that are substrates of these enzymes.
At relevant clinical concentrations, eribulin did not inhibit BCRP, OCT1, OCT2, OAT1, OAT3, OATP1B1 and OATP1B3 transporter-mediated activity.