Pharmacokinetics and tolerability of intravenous busulfan in hematopoietic stem cell transplantation

• Published in: Clinical transplantation 2007-05, Vol.21 (3), p.417-422
• Main Authors: Cho, Yo-Han, Lim, Hyun-Ae, Lee, Mark Hong, Kim, Inho, Lee, Jong Seok, Park, Seong yang, Kim, Byoung Kook, Yoon, Sung-Soo
• Format: Article
• Language: English
• Subjects: Adolescent; Adult; Anesthesia. Intensive care medicine. Transfusions. Cell therapy and gene therapy; Area Under Curve; Biological and medical sciences; Bone marrow, stem cells transplantation. Graft versus host reaction; busulfan; Busulfan - administration & dosage; Busulfan - pharmacokinetics; Female; Fundamental and applied biological sciences. Psychology; Fundamental immunology; Granulocyte Colony-Stimulating Factor - therapeutic use; Hematopoietic Stem Cell Transplantation; Hepatic Veno-Occlusive Disease - etiology; Humans; Infusions, Intravenous; intravenous; Leukemia, Myelogenous, Chronic, BCR-ABL Positive - therapy; Male; Medical sciences; Middle Aged; pharmacokinetics; Precursor Cell Lymphoblastic Leukemia-Lymphoma - therapy; stem cell transplantation; Surgery (general aspects). Transplantations, organ and tissue grafts. Graft diseases; Tissue, organ and graft immunology; Transfusions. Complications. Transfusion reactions. Cell and gene therapy
• ISSN: 0902-0063; 1399-0012
• DOI: 10.1111/j.1399-0012.2007.00664.x

:  Intravenous (IV) busulfan has been developed to overcome variable absorption of oral busulfan and tested in several trials. We tested its pharmacological properties and tolerability in 16 Korean stem cell transplantation (SCT) patients. IV busulfan was administered at 0.8 mg/kg every six h for a total of 16 doses (days −7 to −4), which was followed by cyclophosphamide administration at 60 mg/kg every 24 h for two d (days −3 and −2). The median AUCinf values (at the first dose) and AUCss (at the steady state) were 1060.4 μM·min (range: 511.1–1812.7) and 1092.5 μM·min (range: 539.7–1560.8) respectively. All patients had an AUCinf of