Chlorambucil (Leukeran)

General information

Class/mechanism: Nitrogen mustard, alkylating agent. Interferes with DNA replication and induces apoptosis through accumulation of p53 in the cytosol and downstream activation of the apoptosis promoter Bax.
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.

Diseases for which it is established

• Follicular lymphoma

Diseases for which it is used

• B-cell lymphoma of mucosa-associated lymphoid tissue
• Chronic lymphocytic leukemia
• Classical Hodgkin lymphoma
• Mantle cell lymphoma
• Marginal zone lymphoma
• Waldenström macroglobulinemia

Diseases for which is was used

• Breast cancer
• Ovarian cancer
• Testicular cancer

Patient drug information

• Chlorambucil (Leukeran) package insert
• Chlorambucil (Leukeran) patient drug information (Chemocare)
• Chlorambucil (Leukeran) patient drug information (UpToDate)

History of changes in FDA indication

• 1957-03-18: Initial FDA approval
• 2003-11-13 (oldest label available at Drugs @ FDA): indicated in the treatment of chronic lymphatic (lymphocytic) leukemia, malignant lymphomas including lymphosarcoma, giant follicular lymphoma, and Hodgkin's disease. It is not curative in any of these disorders but may produce clinically useful palliation. (No supporting studies are cited)

Also known as

• Brand names: Chloraminophene, Chlorambusil, Chlorobutin, Chlorbutin, Leukeran, Linfoxan