Amonafide (AS-1413) is a reversible, benzoisoquinolinedione-based DNA intercalator that produces protein-associated DNA cleaveage and single- and double-strand cleavage by mechanisms suggesting an interaction with topoisomerase II. [1]

Amonafide has demonstrated significant activity against P388 leukemia and L1210 cell lines as well as B16 melanoma and M5076 sarcoma cell lines. [2] In phase II studies with cytarabine, overall CR rates of 42% were observed and produced a high complete remission rate and durable responses in patients with acute myeloid leukemia. [3]

Amonafide is easily metabolized and is a substrate of N-acetyl transferase-2 (NAT2); the acetylation adduct is roughly equipotent to amonafide, but has been attributed to the toxicity observed in the clinic. [4]