LEVELS OF 2'-DEOXYCOFORMYCIN, ADENOSINE, AND DEOXYADENOSINE IN PATIENTS WITH ACUTE LYMPHOBLASTIC-LEUKEMIA

  • 1 January 1981
    • journal article
    • research article
    • Vol. 41  (11) , 4508-4511
Abstract
2''-Deoxycoformycin (dCF), a potent inhibitor of adenosine deaminase, has recently undergone phase I clinical trials and was found to be therapeutically active in acute lymphoblastic leukemia. In this report, levels of dCF in plasma, plasma concentrations of adenosine and deoxyadenosine and urine levels of deoxyadenosine were measured in leukemic patients undergoing treatment with dCF during a phase I clinical trial. dCF was administered i.v. at a dose of 0.25-1.0 mg/kg (7.5-30 mg/sq m) for 3 consecutive days. Plasma drug levels of 2 to 6 .mu.M were observed following the 3rd dose of dCF, and drug accumulation occurred only at the 1-mg/kg dosage. In this limited series of patients the plasma concentrations of adenosine and deoxyadenosine and the urine concentration of deoxyadenosine did not show an obvious correlation with dCF dose, therapeutic response or toxicity.