Cytarabine, or cytosine arabinoside, is a chemotherapy agent used mainly in the treatment of hematological malignancies such as leukemia and non-Hodgkin lymphoma. It is also known as ara C.

History

Cytarabine was discovered in Europe in the 1960s. It was approved by the United States Food and Drug Administration in June 1969, and was initially marketed in the US by Upjohn under the trade name Cytosar-U.

Mechanism

Cytosine arabinoside is an antimetabolic agent with the chemical name of 1?-arabinofuranosylcytosine. Its mode of action is due to its rapid conversion into cytosine arabinoside triphosphosphate, which damages DNA when the cell cycle holds in the S phase (synthesis of DNA). Rapidly dividing cells, which require DNA replication for mitosis, are therefore most affected. Cytosine arabinoside also inhibits both DNA and RNA polymerases and nucleotide reductase enzymes needed for DNA synthesis. Cytarabine is rapidly deaminated in the body into the inactive uracil derivative and therefore is often given by continuous intravenous infusion.

Clinical uses

Cytarabine is mainly used in the treatment of acute myeloid leukaemia, and in lymphomas,^[1] where it is the backbone of induction chemotherapy. Cytarabine also possesses antiviral activity, and it has been used for the treatment of generalised herpesvirus infection. However, cytarabine is not very selective in this setting and causes bone marrow suppression and other severe side effects, so it is used mainly for the chemotherapy of hematologic cancers.

One of the unique toxicities of cytarabine is cerebellar toxicity when given in high doses.

Toxicity: Leukopenia, Thrombocytopenia, anemia, GI disturbances, stomatitis, conjunctivitis, pneumonitis, fever, and dermatitis.

Cytarabine is also used in the study of the nervous system to control the proliferation of glial cells in cultures, the amount of glial cells having an important impact on neurons.

Brand names

• Cytosar-U
• Tarabine PFS
• Depocyt (longer-lasting liposomal formulation)

External links

• MedlinePlus page on cytarabine
• ADAP drugs page on cytarabine
• BC Cancer network page on cytarabine
• Chembank entry
• Sea to Ara C An essay on the history of cytarabine.

References

1. ↑

• Hobbs J.B. in Comprehensive Medicinal Chemistry Vol. 2: (ed. Sammes, Peter G.) Pergamon Press, 1990
• Männistö P.T., Tuominen R.K. in Farmakologia ja Toksikologia, 5^th edition: (ed. Koulu, Tuomisto, Paasonen) Medicina, 1996
• Rang H.P., Dale M.M., Ritter J.M.: Pharmacology, 3^rd edition. Pearson Professional Ltd, 1995.

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