Cytarabine

Cytarabine (ara-C) is a nucleoside analog and prodrug form of the DNA polymerase inhibitor ara-CTP.¹ It is triphosphorylated to ara-CTP by the successive actions of deoxycytidine kinase, deoxycytidylate kinase, and nucleoside diphosphate kinase.² Ara-C inhibits proliferation of HL-60, ML-1, Raji, and Jurkat human leukemia cell lines with IC₅₀ values of 37, 17, 16, and 72 nM, respectively.³ It induces cell cycle arrest at the G₀/G₁ phase in HL-60 cells when used at concentrations of 2.5 and 15 µM.¹ ara-C (75 mg/kg per day, i.p.) reduces tumor growth and increases tumor caspase-3 activity in an MOLM-13 mouse xenograft model.⁴ It also increases survival and reduces brain herpesvirus titers in infected rats when administered subcutaneously at doses of 80 and 320 mg/kg.⁵ Formulations containing ara-C have been used in the treatment of acute myeloid leukemia.

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1. Li, Z., Guo, J.-R., Chen, Q.-Q., et al. Exploring the antitumor mechanism of high-dose cytarabine through the metabolic perturbations of ribonucleotide and deoxyribonucleotide in human promyelocytic leukemia HL-60 cells. Molecules 22(3), E499 (2017).

2. Emadi, A., and Karp, J.E. The clinically relevant pharmacogenomic changes in acute myelogenous leukemia. Pharmacogenomics 13(11), 1257-1269 (2012).

3. Qin, T., Youssef, E.M., Jelinek, J., et al. Effect of cytarabine and decitabine in combination in human leukemic cell lines. Clin. Cancer Res. 13(14), 4225-4232 (2007).

4. Kelly, K.R., Espitia, C.M., Taverna, P., et al. Targeting PIM kinase activity significantly augments the efficacy of cytarabine. Br. J. Haematol. 156(1), 129-132 (2012).

5. Renis, H.E. Antiviral activity of cytarabine in Herpesvirus–infected rats. Antimicrob. Agents Chemother. 4(4), 439-444 (1973).