amonafide l-malate

Amonafide l-malate is the malate salt form of amonafide, a synthetic small molecule and imide derivative of naphthalic acid with antineoplastic activity. It acts as a DNA intercalator and inhibits topoisomerase II. This dual mechanism leads to DNA double-strand breaks and inhibition of both DNA replication and RNA synthesis. Unlike classical topoisomerase II inhibitors that induce apoptosis primarily through extensive DNA damage, amonafide l-malate disrupts chromatin organization independently of ATP and can evade P-glycoprotein-mediated multidrug resistance mechanisms. It was developed for use in oncology—primarily acute myeloid leukemia (AML), especially secondary AML—and has also been studied in solid tumors such as breast cancer, ovarian cancer, and prostate cancer[1][3][6][8]. The drug received orphan drug status in the US and EU for AML but was discontinued after failing to meet primary endpoints in Phase III trials[3].

Brand names

Xanafide

Other names

amonafide L-malate5-Amino-2-(2-(dimethylamino)ethyl)-1H-benz(de)isoquinoline-1,3(2H)-dione (2S)-2-hydroxybutanedioate