[Clinical and pharmacokinetic studies of high dose N4-behenoyl-1-beta-D-arabinofuranosylcytosine].
Effect of high dose of N4-behenoyl-1-beta-D-arabinofuranosylcytosine (BH-AC) was studied clinically and pharmacologically in non-Hodgkin's lymphoma and acute leukemia. The schedule of drug administration consisted of daily i.v. infusion for 5 consecutive days. The daily close was initiated with 500 mg/m2 which was escalated up to 1300 mg/m2. Eruption was found to be dose-limiting toxicity and there was no myelosuppression. The plasma concentration curve of BH-AC showed a biphasic curve. The half-lives of the initial phase (t1/2 alpha) and the second phase (t1/2 beta) by the administration (1 hr iv infusion) of 700 mg/m2 were 1.08 and 3.65 h respectively. The plasma 1-beta-D-arabinofuranosylcytosine was detected for 12-24 hr after infusion (Cmax: 0.26 microgram/ml).
D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000378:metabolism*; D003561:Cytarabine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D007938:Leukemia / Q000188:drug therapy* / Q000378:metabolism; D008228:Lymphoma, Non-Hodgkin / Q000188:drug therapy* / Q000378:metabolism
D000970:Antineoplastic Agents; D003561:Cytarabine; C015019:enocitabine