Treatment of acute myelogenous leukemia in adults with N4-behenoyl-1-β-D-arabinofuranosylcytosine

Abstract

Forty-five previously-untreated adult patients with acute myelogenous leukemia (AML) were treated with N'-behenoyl-l-B-Darabinofuranosyl-cytosine (BHAC) in a multi-institutional cooperative study. Among 41 evaluable patients, 15 (36.6%) achieved complete remission (CR) and 10 (24.4%) achieved partial remission by daily administration of 3 to 8 mg/kg of BHAC. Higher daily doses (5 mg/kg or more) produced higher CR rates, and all of the CR were observed among the patients receiving a top1 BHAC dosage of 50 mg/kg or more in a period of 10 days or more. The side effects were mild and acceptable: nausea-anorexia was observed in 27% of the patients and vomiting in 17%. The results of this study thus indicate BHAC to be effective for remission induction of AML, and to deserve further clinical trials in combination with other anti-leukemic drugs.

Symptomatic intracranial haemorrhage in acute nonlymphoblastic leukaemia: analysis of CT and autopsy findings

“…Intracerebral haemorrhage occurred in 30 patients. Twenty-four patients with subcortical haemorrhage were classified into three types: a single haematoma (7), clustered multifocal haematomas (11), and separated multifocal haematomas (6). Subarachnoid haemorrhage (SAH) occurred in 22 patients; 15 with subcortical haemorrhage, 1 with subdural haemorrhage (SDH) and 6 without any other ICH.…”

“…As shown in Table 1, 194 patients with ANLL were classified according to the FAB criteria [2]: 67 had myeloblastic leukaemia without maturation (M1), 33 myeloblastic leukaemia with some maturation to promyelocytes (M2), 33 promyelocytic leukaemia (M3), 26 myelomonocytic leukaemia (M4), 14 monocytic leukaemia (M5), and 13 had erythroleukaemia (M5). Remission induction chemotherapy was given which consisted of either daunorubicin, 1-β-D-arabinofuranosyl cytosine (Ara-C) or N 4 -behenoyl Ara-C, 6-mercaptopurine and prednisolone or a regimen using aclarubicin instead of daunorubicin [11]. Patients with meningeal infiltration received intrathecal chemotherapy consisting of methotrexate, Ara-C and prednisolone.…”

Monitoring of Intracellular l‐βD‐Arabinofuranosylcytosine 5′‐Triphosphate in 1‐β‐D‐Arabinofuranosylcytosine Therapy at Low and Conventional Doses

“…2,3) N 4 -Behenoyl-1-β-D-arabinofuranosylcytosine (BHAC), one of the N 4 -acyl derivatives of ara-C, is frequently used instead of conventional-dose ara-C in Japan. 4) While ara-C is rapidly inactivated by cytidine deaminase in the plasma, BHAC is resistant to deamination 5) and its plasma level is well maintained, resulting in continuous release of ara-C. 6) Low-dose ara-C (3-10 mg/m 2 ) is administered subcutaneously or by continuous infusion to elderly patients with leukemia or myelodysplastic syndrome in the expectation of a mild cytotoxic effect. [7][8][9] Patients with refractory leukemia receive ara-C at high doses (1000-3000 mg/m 2 ) to overcome the drug resistance.…”

Idarubicin Plus Behenoyl Cytarabine and 6-thioguanine Compares Favorably with Idarubicin Plus Cytarabine-based Regimen for Children with Previously Untreated Acute Myeloid Leukemia: 10-Year Retrospective, Multicenter Study in Korea

“…In a phase II study, BHAC monotherapy for adult AML produced a 36% CR rate and adverse events such as nausea and vomiting were less than for cytarabine (17). In a comparative study between BHAC and cytarabine in combination induction and consolidation therapy for adults with de novo AML, the efficacy of BHAC given with daunorubicin was found to be inferior to that of cytarabine in combination with daunorubicin (14).…”