Disclosed is the use of 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione (napabucasin) for treatment of cancer in a subject in need thereof, wherein the medicament is formulated for administration to the subject at a total daily dose in a range of from about 20 mg to about 2000 mg. Also disclosed is treatment where napabucasin is administered at a dose sufficient to achieve a blood concentration of the compound in the subject of at least 1.0 μΜ or above for at least two hours, wherein the blood concentration of the compound in the subject is substantially cleared within at most 24 hours.
