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What is chlorambucil used for?

What is chlorambucil used for?

Chlorambucil is used treat a certain type of chronic lymphocytic leukemia (CLL; a type of cancer of the white blood cells). Chlorambucil is also used to treat non-Hodgkin’s lymphoma (NHL) and Hodgkin’s disease (types of cancer that begin in certain white blood cells that normally fight infection).

What is the mechanism of action of chlorambucil?

Chlorambucil produces its anti-cancer effects by interfering with DNA replication and damaging the DNA in a cell. The DNA damage induces cell cycle arrest and cellular apoptosis via the accumulation of cytosolic p53 and subsequent activation of Bcl-2-associated X protein, an apoptosis promoter.

What is chlorambucil made of?

It is a bifunctional alkylating agent of the nitrogen mustard type that has been found active against selected human neoplastic diseases. Chlorambucil is known chemically as 4-[bis(2-chlorethyl)amino]benzenebutanoic acid and has the following structural formula: Chlorambucil hydrolyzes in water and has a pKa of 5.8.

Is chlorambucil an alkylating agent?

Chlorambucil is an antineoplastic in the class of alkylating agents that is used to treat various forms of cancer. Alkylating agents are so named because of their ability to add alkyl groups to many electronegative groups under conditions present in cells.

What is the generic name for chlorambucil?

Trade name: Leukeran Leukeran is the trade name for chlorambucil. In some cases, health care professionals may use the trade name leukeran when referring to the generic drug name chlorambucil. Drug Type: Chlorambucil is an anti-cancer (“antineoplastic” or “cytotoxic”) chemotherapy drug.

Where can chlorambucil be found?

Chlorambucil belongs to the nitrogen mustard group of alkylating agents. It is well absorbed from the gastrointestinal tract of rats and humans and is mainly distributed to liver, kidney and plasma in the rat.

Is chlorambucil a prodrug?

A Prodrug of Two Approved Drugs, Cisplatin and Chlorambucil, for Chemo War Against Cancer. Mol Cancer Ther. 2017 Apr;16(4):625-636. doi: 10.1158/1535-7163.

How does nitrogen mustard work?

The discovery of nitrogen mustard as an alkylating agent in 1942, opened a new era in the cancer chemotherapy. This valuable class of alkylating agent exerts its biological activity by binding to DNA, cross linking two strands, preventing DNA replication and ultimate cell death.

How is chlorambucil excreted?

It is extensively metabolized in the liver to its major metabolite, phenylacetic acid mustard (PAAM), which also has bifunctional alkylating activity. The half-lives of chlorambucil and PAAM are 1.5 and 2.5 hours, respectively; less than 1% of either chlorambucil or PAAM is excreted in the urine.

Is chlorambucil a chemotherapy?

Chlorambucil is a chemotherapy drug and is also known by its brand name Leukeran. It is used mainly to treat: chronic lymphocytic leukaemia (CLL) Non-Hodgkin lymphoma.

Is chlorambucil still used?

The major uses are in the treatment of Waldenström macroglobulinemia, low-grade lymphomas, chronic lymphocytic leukemia (CLL), and Hodgkin lymphoma. Except for CLL, chlorambucil has been supplanted by newer agents.

What is the half life of chlorambucil?

The terminal phase elimination half life ranges from 1.3-1.5 hours for chlorambucil and is approximately 1.8 hours for PAAM.