chlorambucil

Chlorambucil was synthesized in 1953. It is an aromatic derivative of mechlorethamine and is closely related in structure to melphalan. It is the slowest acting and generally least toxic of the alkylating agents.

Alkylation of DNA results in breaks in the DNA molecule as well as cross-linking of the twin strands, thus interfering with DNA replication and transcription of RNA. Like other alkylators, chlorambucil is cell cycle phase-nonspecific.

Chlorambucil (marketed as Leukeran) is a chemotherapy drug that has been mainly used in the treatment of chronic lymphocytic leukemia. It is a nitrogen mustard alkylating agent and can be given orally.

In the past, it has been used for treating some types of non-Hodgkin lymphoma, Waldenström macroglobulinemia, polycythemia vera, trophoblastic neoplasms, ovarian carcinoma. It also has been used as an immunosuppressive drug for various autoimmune and inflammatory conditions, e.g. nephrotic syndrome. Its current use is mainly for CLL as it is well tolerated by most patients, though this has been primarily replaced by fludarabine.

Side effects include myelosuppression (anemia, neutropenia, thrombocytopenia).

See also

 alkylating agents (alkylators)