Drug information of Treosulfan


Treosulfan belongs to the family of Methanesulfonates.
Treosulfan in combination with fludarabine is indicated as part of conditioning treatment prior to allogeneic haematopoietic stem cell transplantation (alloHSCT) in adult patients with malignant and non malignant diseases, and in paediatric patients older than one month with malignant diseases.

Mechanism of effect

The anti-tumour drug treosulfan (L-threitol 1,4-bismethanesulphonate, Ovastat) is a prodrug for epoxy compounds by converting non-enzymatically to L-diepoxybutane via the corresponding monoepoxide under physiological conditions.
 DNA alkylation and interstrand cross-linking of plasmid DNA is observed after treosulfan treatment, but this is again produced via the epoxide species


Alkylating agent; interferes with DNA replication and RNA transcription; cross-links DNA strands; has little immunosuppressive activity; affects myeloid cells more than lymphoid cells; very toxic to hematopoietic stem cells


bioavailability: 0.97
AUC oral: 39.4 ug/ml hr
AUC iv: 85.4 ug/ml hr
cmax oral: 29 ug/ml
cmax iv: 65 ug/ml
tmax oral: 1.5 hr
half life: 1.8 hr
The mean urinary excretion of the parent compound was about 15% of the administered total dose over 24 hr 


vial 1g
vial 5g
capsule 250mg

Drug contraindications

Hypersensitivity to this drug


Bone marrow suppression is a common occurrence; reduce dose or discontinue oral administration for unusual suppression (bond marrow biopsy may be necessary); hematopoietic progenitor cell transplantation is required to prevent potentially fatal complications of prolonged myelosuppression

Monitoring is very important after administering these doses

This drug should be administered under the supervision of an experienced cancer chemotherapy physician
Acute non-lymphocytic leukemia occurred in eight women following long-term treatment with Treosulfan (= dihydroxybusulfan) for ovarian carcinoma

Points of recommendation

Do not increase your dose or take this medication more often than prescribed
administer as intravenous infusion

Pregnancy level


Drug forms


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