Chemotherapy Drugs 101: Alkylating Antineoplastic Agents


The word instills terror, invokes images of hair loss, weakness, sickness. It can be an extraordinarily trying time, for patients and their caregivers. The literally hundreds of different drugs used in chemotherapy treatment can be daunting. In order to try and remove some of the terror and mystery of chemo, I'm going to use this blog to take an occasional look at the various groups of drugs used in chemo—their names, what they are, and what they do—to cancer cells and to our bodies.

In this entry I'll be looking at a couple of the so-called alkylating antineoplastic agents. These drugs represent some of the first drugs ever used in anticancer chemotherapy treatments. Many if not all of them are known human carcinogens themselves, and have a variety of side effects.

Now, cancer cells have an Achilles heel: they're more susceptible to DNA damage than healthy cells. Generally speaking, in chemo, alkylating antineoplastic agents damage the DNA of cancer cells by 'alkylating' them, or adding a chemical group called an alkyl group to the cancer cell. The end result is a cancerous cell that can't replicate, or divide.

These are some of the primary alkylating antineoplastic drugs used in lymphomas such as Hodgkin's Lymphoma and non-Hodgkin's Lymphoma. Click on the drug to be taken to the American Cancer Society's patient page for that drug, which contains general information as well as potential side effects.

Cyclophosphamide (marketed as Endoxan, Cytoxan, Neosar, Procytox, and Revimmune).

Mechlorethamine (Mustargen, Nitrogen Mustard). This is the first drug used in anticancer chemotherapy treatments

Uramustine (uracil mustard). Effective in non-Hodgkin's lymphoma because cancer cells need a chemical called uracil to divide. In the body, uracil is turned into thymine, which protects the DNA and improves its effectiveness. When cancer cells have it, they perform well. Uracil mustard damages the DNA and makes it impossible for the cancer cell to use the uracil.

Chlorambucil (marketed as Leukeran). Chlorambucil can cause sterility. It is generally used to treat chronic lymphatic (lymphocytic) leukemia, malignant lymphomas including lymphosarcoma, giant follicular lymphoma, and Hodgkin’s disease.

Ifosfamide (marketed as Mitoxana, Ifex). Ifosfamide is used to treat both Hodgkin's lymphoma and non-Hodgkin's lymphoma.

Carmustine (marketed as BCNU, BiCNU, Gliadelv). Carmustine is used to treat both Hodgkin's lymphoma and non-Hodgkin's lymphoma.

Streptozotocin (marketed as Streptozocin, STZ, Zanosar). Streptozotocin is used to treat some cancers but not specifically used to treat lymphomas.

Note: The World Health Organization's Anatomical Therapeutic Chemical Classification System (ATC) classifies alkylating agents as L01A.

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