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Busulfan

    Brands

    DEA Class; Rx

    Common Brand Names; Myleran, Busulfex

    • Antineoplastics, Alkylating; 
    • Immunosuppressives, PHD

    A bifunctional alkylating agent
    IV formulation used in combination with cyclophosphamide as a conditioning regimen prior to allogeneic hematopoietic stem-cell transplantation in patients with chronic myelogenous leukemia (CML); oral tablet formulation used for palliative treatment of CML
    Black box warning for myelosuppression

    Indicated for the palliative treatment of chronic myelogenous leukemia (CML).

    For stem cell transplant preparation.

    Hypersensitivity, resistance to busulfan

    Patients without definitive diagnosis of CML

    • Neutropenia (nearly 100%)
    • Myelosuppression (nearly 100%)
    • Thrombocytopenia (98%)
    • Nausea (97%)
    • Stomatitis (96%)
    • Anorexia (80%)
    • Diarrhea (80%)
    • Fever (80%)
    • Insomnia (80%)
    • Lymphopenia (79%)
    • Hypomagnesemia (77%)
    • Headache (69%)
    • Hyperglycemia (66%)
    • Hypokalemia (64%)
    • Abdominal pain (62%)
    • Anemia (62%)
    • Asthenia (52%)
    • Hypocalcemia (49%)
    • Chills (47%)
    • Dyspepsia (44%)
    • Tachycardia (44%)
    • Pain (41%)
    • Constipation (38%)
    • Hypertension (36%)
    • Hypersensitivity (32%)
    • Edema (27%)
    • Thrombosis (27%)
    • Dry mouth (26%)
    • Vasodilation (25%)

    Bone marrow depression may occur

    Seizures reported with use; initiate anticonvulsant prophylactic therapy prior to treatment with busulfan; monitor patients with history of seizure disorder, head trauma or receiving epileptogenic drugs

    Cardiac temponade reported in children with thalassemia in combination with cyclophosphamide

    Ovarian failure may occur

    Secondary malignancies reported

    Antiemetics may be recommended to prevent nausea and vomiting

    Increased risk of developing hepatic veno-occlusive disease (HVOD) at AUC greater than 1,500 μM•min; monitor serum transaminases, alkaline phosphatase and bilirubin daily

    Bronchopulmonary dysplasia with pulmonary fibrosis reported and can be fatal; toxicity may be additive if used with other agents that cause pulmonary toxicity; discontinue therapy if busulfan toxicity develops

    Avoid pregnancy; can cause fetal harm; advise of potential risk to a fetus and use of effective contraception

    Can cause fetal harm when administered to a pregnant woman based on animal data

    Advise females of reproductive potential to use effective contraception during treatment and for 6 months following cessation of therapy

    Adults

    8 mg/day PO; 1 mg/kg PO every 6 hours for 16 doses has been studied as part of a conditioning regimen prior to stem-cell transplantation.
    0.8 mg/kg IV every 6 hours for 16 doses; 1 mg/kg IV every 6 hours for 16 doses has been studied as part of a conditioning regimen prior to stem-cell transplantation.

    Geriatric

    8 mg/day PO; 1 mg/kg PO every 6 hours for 16 doses has been studied as part of a conditioning regimen prior to stem-cell transplantation.
    0.8 mg/kg IV every 6 hours for 16 doses; 1 mg/kg IV every 6 hours for 16 doses has been studied as part of a conditioning regimen prior to stem-cell transplantation.

    Adolescents

    60 mcg/kg or 1.8 mg/m2 PO per day.

    Children

    60 mcg/kg or 1.8 mg/m2 PO per day.

    Infants

    60 mcg/kg or 1.8 mg/m2 PO per day.

    Neonates

    60 mcg/kg or 1.8 mg/m2 PO per day.

    Busulfan 

    injectable solution

    • 6mg/mL

    tablet

    • 2mg