Pixantrone is an anticancer chemotherapeutic and immunosuppressive aza-anthracenedione that acts as a DNA intercalator and topoisomerase II inhibitor; this compound intercalates via the major or minor grooves of DNA, binding to CpG or CpA motifs. In cellular models, pixantrone inhibits proliferation of T cells, but does not affect differentiation of dendritic cells or B cells. In clinical trials, pixantrone increases survival times of patients with relapsed or refractory aggressive non-Hodgkin’s B-cell lymphoma. Pixantrone also shows potential benefit in the treatment of several other diseases. In cellular models, this compound decreases or prevents amyloid-β (Aβ) oligomerization, indicating a potential use in the treatment of Alzheimer’s disease. Additionally, it decreases acetylcholine receptor (AChR)-specific immune responses and prevents and treats experimental autoimmune encephalitis (EAE) in animal models, suggesting potential benefit in the treatment of myasthenia gravis and multiple sclerosis.