Chlorambucil, approved by the Food and Drug Administration (FDA) in 1957, is an antineoplastic/alkylating agent with a broad spectrum of antitumor activity used to treat chronic lymphocytic leukemia (CLL), Hodgkin’s and non-Hodgkin’s lymphomas. 

Property

The chemical is of a white to pale slight odorous powder, insoluble in water. It is very slightly dispersible in diethyl ether and acetone. It has a melting point of 69°C, boiling point of 424°C, and 5.75 pKa. The partition coefficient is 4.07 and has a molecular weight of 304.22 g mol-1.

Uses

Chlorambucil is FDA indicated for the treatment of CLL, Hodgkin’s and non-Hodgkin’s lymphomas, and mycosis fungoides. It has also been known to treat other conditions such as polycythemia vera, uveitis, hairy cell leukemia, ovarian carcinoma, and Waldenstrom’s magroglobulinemia.

Mechanism

The mechanism of action of chlorambucil is thought to be an alkylating agent and an aromatic nitrogen mustard derivative; it interferes with DNA replication and RNA transcription by alkylation and cross-linking the strands of DNA.

Side effects

Bone marrow suppression (anemia, neutropenia, thrombocytopenia) is the most commonly occurring side effect of chlorambucil. Withdrawn from the drug, this side effect is typically reversible. Like many alkylating agents, chlorambucil has been associated with the development of other forms of cancer.

Less commonly occurring side effects include:

Gastrointestinal Distress (nausea, vomiting, diarrhea, and oral ulcerations).

Central Nervous System: Seizures, tremors, muscular twitching, confusion, agitation, ataxia, and hallucinations.

Skin reactions;

Hepatotoxicity;

Infertility;

Hair Loss.