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Types of Cytotoxic Drugs

author image Dr. Tina M. St. John
Tina M. St. John runs a health communications and consulting firm. She is also an author and editor, and was formerly a senior medical officer with the U.S. Centers for Disease Control and Prevention. St. John holds an M.D. from Emory University School of Medicine.
Types of Cytotoxic Drugs
Chemotherapeutic medications may be used in combination (Ref3, Intro). Photo Credit: Comstock/Stockbyte/Getty Images

Cancer treatment utilizes medications classified as antineoplastic -- anti-cancer -- and cytotoxic -- destructive to cells (Ref1, Pg1). Treatment with these medications is commonly known as chemotherapy, and over 100 medications are in use today (Ref1, Pg2). These medications may damage the DNA of cancer cells, inhibit new DNA from forming, or stop the splitting of one cell into two cells (Ref3, Cancer Chemotherapy). Some medications may act in more than one way as well (Ref1). This article focuses on the various types of cytotoxic medications available.

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Alkylating Agents

These medications directly damage cell DNA, the genetic material required for cells to grow and reproduce (Ref1, Pg5). Alkylating agents include cisplatin (Platinol) and the antibiotics -- daunorubicin (Cerubidine), doxorubicin (Adriamycin, Doxil), and etoposide (Toposar, Etopophos) (Ref3, Categories of Chemotherapy Drugs). These agents are used to treat a variety of cancers including but not limited to leukemia, lymphoma, Hodgkin disease, and lung, ovary, and breast cancers (Ref1Pg5).


DNA and another type of cell material called RNA are made up of molecules that act like genetic building blocks. Antimetabolite medications interfere with these so-called building blocks thus preventing replication of cancer cells (Ref1, Pg5). Examples of antimetabolite medications include methotrexate (Trexall, Otrexup), fluorouracil (Adrucil, Efudex), hydroxyurea (Hydrea, Droxia), and mercaptopurine (Purinethol) (Ref3, Categories of Chemotherapy Drugs).These medications are used to treat leukemias, breast and ovarian cancer, cancers of the intestinal tract, as well as others (Ref1, Pg6).

Inhibitors of Mitosis

Mitosis is the process by which the genetic material of a cell replicates and splits to form two cells from one original cell (Ref2). Medications are available that halt cell replication at this step, leading to cell death (Ref1, Pg7). Examples of medications that stop mitosis are vinblastine, vincristine (Vincasar PFS, Marqibo) and pacitaxel (Abraxane, Onxol) (Ref3, Categories of Chemotherapy Drugs).These drugs are used to treat breast and lung cancers, myelomas, lymphomas, and leukemias (Ref1, Pg7).

Topoisomerase Inhibitors

Topoisomerases are molecules within cells that aid copying of the DNA before a cell can replicate (Ref1, Pg7). Examples of topoisomerase inhibitors include etoposide (Etopophos), teniposide (Vumon), and mitoxantrone (Ref1, Pg7). These medications are used to treat leukemias, lung, ovarian, and intestinal cancers, among others (Ref1, Pg7).

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