Amsacrine

Amsacrine, also known as m-AMSA, is an antineoplastic agent in the acridine class used in chemotherapy. It exerts cytotoxic effects primarily by intercalating into DNA and inhibiting topoisomerase II, leading to DNA strand breaks and disruption of replication and transcription. This mechanism makes it active against rapidly dividing cancer cells.

It has been used in the treatment of hematologic malignancies, including acute myeloid leukemia and acute lymphoblastic leukemia, and has appeared in regimens for certain lymphomas. Over time its use has varied by region and has declined in some settings due to toxicity and the availability of newer therapies; it is typically part of multi-drug combinations rather than a stand-alone treatment.

Administration is intravenous, usually given as a short infusion within a broader chemotherapy protocol. Dosing is protocol-dependent and considerations such as prior therapy, performance status, and organ function influence planned exposure. Pharmacokinetic data indicate hepatic metabolism with renal excretion contributing to clearance; the drug’s half-life can vary with liver impairment.

Adverse effects are dose-related and can be significant. The major toxicity is bone marrow suppression, but patients may also experience nausea, vomiting, mucositis, and alopecia. A characteristic and important safety concern is central nervous system toxicity, including seizures, which can occur during treatment. Other risks include liver function abnormalities and, less commonly, cardiovascular effects. Monitoring and supportive care are integral components of therapy when using amsacrine.