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Busulfan parenteral

Updated 2 Feb 2023 | Alkylating agents


Parenteral formulations of busulfan.

Drugs List

  • busulfan 60mg/10ml concentrate for solution for infusion
  • Therapeutic Indications


    Conditioning for HPCT following fludarabine, in RIC suitable patients
    Conditioning for HPCT in children prior to receiving melphalan
    Conditioning for HPCT, prior to receiving cyclophosphamide

    Busulfan followed by cyclophosphamide is indicated as conditioning treatment prior to conventional haematopoietic progenitor cell transplantation (HPCT) in adult patients when the combination is considered the best available option.

    Busulfan following fludarabine is indicated as conditioning treatment prior to HPCT in adult patients who are candidates for a reduced-intensity conditioning (RIC) regimen.

    Busulfan followed by cyclophosphamide or melphalan is indicated as conditioning treatment prior to conventional HPCT in paediatric patients.


    Whilst the doses stated below are those recommended by the manufacturer, local cancer network protocols for the relevant indication should be consulted.

    Obese patients, dosing based on adjusted ideal body weight should be considered.


    Busulfan in combination with cyclophosphamide
    Recommended dose is 0.8mg/kg body weight of busulfan every 6 hours over 4 consecutive days for a total of 16 doses.

    Followed by treatment with cyclophosphamide (60mg/kg per day over 2 days), at least 24 hours after the last busulfan dose.

    Busulfan in combination with fludarabine
    3.2mg/kg of busulfan as a single daily dose for 2 to 3 consecutive days, immediately after treatment with fludarabine.

    Prior treatment with fludarabine (30mg/metre squared for 5 consecutive days or 40mg/metre squared for 4 days).


    Busulfan is administered every 6 hours over 4 consecutive days for a total of 16 doses.

    Busulfan in combination with cyclophosphamide or melphalan
    Children aged up to 17 years
    Above 34kg body weight: 0.8mg/kg body weight
    More than 23kg to 34kg body weight: 0.95mg/kg body weight
    16kg to 23kg body weight: 1.1mg/kg body weight
    9kg to less than 16kg body weight: 1.2mg/kg body weight
    Below 9kg body weight: 1mg/kg body weight

    Followed by 4 cycles of 50mg/kg body weight cyclophosphamide, or by one administration of 140mg/metre squared melphalan.

    Busulfan in combination with fludarabine
    No dose recommendation can be made. Safety and efficacy has not been established in children under 17 years.


    Busulfan must be diluted prior to use and administered by intravenous infusion via central venous catheter.

    Busulfan in combination with cyclophosphamide or melphalan: Busulfan should be administered as a two hour infusion.

    Busulfan in combination with fludarabine: Busulfan should be administered as a three hour infusion.


    Children under 18 years with BMI greater than 30kg/m2

    Precautions and Warnings

    Children under 17 years
    History of progenitor cell transplantation
    History of radiotherapy
    Fanconi's anaemia
    Hepatic impairment
    History of seizures
    Renal impairment

    Administration of live vaccines is not recommended
    Consider use of anti-infective prophylaxis during neutropenic phase
    Give pre-treatment counselling and consideration of sperm cryopreservation
    Give prophylactic anti-convulsant 12hrs prior to 24hrs after last dose
    Paracetamol should be avoided for 72 hours before and during administration
    Pre-medicate with antiemetics & continue according to local protocol
    Treatment to be prescribed under the supervision of a specialist
    Consult local policy on the safe use of anti-cancer drugs
    Staff: Not to be handled by pregnant staff
    Monitor cardiac function
    Monitor haematological parameters regularly throughout treatment
    Monitor hepatic function
    Monitor patient for signs and symptoms of respiratory distress
    Monitor patients with a history of mediastinal or pulmonary radiation
    Monitor renal function
    Advise patient to report symptoms of thrombotic microangiopathy
    Advise patient to report unexplained fever, sore throat, bruising, bleeding
    Consider hepatic veno-occlusive disease if hepatic impairment occurs
    Consider treatment with blood growth factors if severe cytopenias develop
    Immunosuppressive drugs may increase risk of malignancy
    Monitor for signs of hepatotoxicity post transplant
    Potentially leukaemogenic
    Potentially mutagenic and carcinogenic
    Risk of developing opportunistic infections
    In obese patients dosing should be based on ideal weight
    Not licensed for all indications in all age groups
    Male & female: May cause infertility
    Male & female: Contraception required during & for 6 months after treatment

    Thrombotic microangiopathy and fatalities have been reported after hematopoietic cell transplantation in which high doses of busulfan was administered in combination with another conditioning treatment.

    Pregnancy and Lactation


    Busulfan is contraindicated in pregnancy.

    At the time of writing there is limited published information regarding the use of busulfan during pregnancy. Congenital abnormalities have been reported with low-dose oral busulfan, though it is unclear if this is attributable to busulfan. Briggs considers busulfan to be teratogenic.

    Animal studies on busulfan have shown potential teratogenic effects and impaired fertility in the offspring.

    The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( ) or if this is unavailable at the backup site ( ).


    Busulfan is contraindicated in breastfeeding.

    It is not known whether busulfan or its metabolites are excreted in human breast milk. However, due to the potential for serious toxicity in the nursing infant it is recommended that breastfeeding is discontinued during treatment.

    The effect of concurrent therapies must also be considered.

    LactMed suggests that it may be possible to breastfeed safely during intermittent therapy by using an appropriate period of breastfeeding abstinence, and cautiously suggests 24 hours or more may be sufficient.

    Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
    Specialist advice is available from the UK Drugs in Lactation Advisory Service at

    Side Effects

    Abnormal breath sounds
    Allergic reaction
    Atrial fibrillation
    Capillary leak syndrome
    Cerebral haemorrhage
    Decreased ejection fraction
    Electrolyte disturbances
    Enamel hypoplasia
    Exacerbation of myasthenia gravis
    Eye disorder
    Febrile neutropenia
    Gastro-intestinal haemorrhage
    Gastro-intestinal symptoms
    Graft versus host disease
    Haemorrhagic cystitis
    Hepatic veno-occlusive disease
    Increase in alkaline phosphatase
    Increase in blood urea nitrogen
    Increase in creatinine
    Increases in hepatic enzymes
    Interstitial lung disease
    Local pain (injection site)
    Ovarian failure
    Pericardial effusion
    Pleural effusion
    Premature menopause
    Pulmonary fibrosis
    Pulmonary haemorrhage
    Renal impairment
    Respiratory distress syndrome
    Respiratory failure
    Serum bilirubin increased
    Skin pigmentation changes
    Thrombotic microangiopathy
    Ventricular extrasystoles
    Weight gain


    It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

    The following number will direct the caller to the relevant local centre (0844) 892 0111

    Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( ) or if this is unavailable at the backup site ( ).

    Further Information

    Last Full Review Date: October 2018

    Reference Sources

    Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 2nd edition (2007) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.

    Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 9th edition (2011) ed. Briggs, G., Freeman, R. and Yaffe, S. Lippincott Williams & Wilkins, Philadelphia.

    NICE Evidence Services Available at: Last accessed: 17 October 2018

    Summary of Product Characteristics: Busilvex 6mg per ml concentrate for solution for infusion. Pierre Fabre Limited. Revised May 2017.

    Summary of Product Characteristics: Busulfan 6mg/ml concentrate for solution for infusion. Accord Healthcare Limited. Revised April 2018.

    US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
    Available at:
    Busulfan. Last revised: 1 October 2018
    Last accessed: 17 October 2018

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