Cladribine

Cladribine is a nucleoside analog of deoxyadenosine and prodrug form of 2-chlorodeoxyadenosine triphosphate (2-CdATP).¹ It is triphosphorylated to Cd-ATP by the successive actions of deoxycytidine kinase, nucleoside monophosphate kinase, and nucleoside diphosphate kinase. Cladribine is cytotoxic to resting or proliferating lymphocytes.² It inhibits RNA synthesis and induces DNA strand breaks in resting human peripheral blood lymphocytes when used at concentrations of 1 and 10 µM.³ Cladribine induces cell cycle arrest at the G₁ phase and apoptosis in U266, RPMI-8226, and MM.1S multiple myeloma cells in a concentration-dependent manner.⁴ It reduces tumor growth in HT-29 colon cancer, RL lymphoma, and RPMI-8226 multiple myeloma mouse xenograft models when administered at a dose of 12 mg/kg.⁵ Formulations containing cladribine have been used in the treatment of hairy cell leukemia.

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1. Hermann, R., Krajcsi, P., Fluck, M., et al. Cladribine as a potential object of nucleoside transporter‑based drug interactions. Clin. Pharmacokinet. (2021).

2. Carson, D.A., Wasson, D.B., Taetle, R., et al. Specific toxicity of 2-chlorodeoxyadenosine toward resting and proliferating human lymphocytes. Blood 62(4), 737-743 (1983).

3. Seto, S., Carrera, C.J., Kubota, M., et al. Mechanism of deoxyadenosine and 2-chlorodeoxyadenosine toxicity to nondividing human lymphocytes. J. Clin. Invest. 75(2), 377-383 (1985).

4. Ma, J., Wang, S., Zhao, M., et al. Therapeutic potential of cladribine in combination with STAT3 inhibitor against multiple myeloma. BMC Cancer 11, 255 (2011).

5. Bagley, R.G., Roth, S., Kurtzberg, L.S., et al. Bone marrow CFU-GM and human tumor xenograft efficacy of three antitumor nucleoside analogs. Int. J. Oncol. 34(5), 1329-1340 (2009).