Drug information of Lomustine


Drug group:

An alkylating agent of value against both hematologic malignancies and solid tumors.
For the treatment of primary and metastatic brain tumors as a component of combination chemotherapy in addition to appropriate surgical and/or radiotherapeutic procedures. Also used in combination with other agents as secondary therapy for the treatment of refractory or relapsed Hodgkin's disease.

Mechanism of effect

Inhibition of DNA & RNA synthesis resulting from carbamylation of DNA polymerase, alkylation of DNA, and alteration of RNA proteins


Lomustine is an alkylating agent of the nitrosourea type. Lomustine and its metabolites interferes with the function of DNA and RNA. It is cell cycle–phase nonspecific. Cancers form when some cells within the body multiply uncontrollably and abnormally. These cells then spread and destroy nearby tissues. Lomustine acts by slowing this process down. It kills cancer cells by damaging the DNA (the genetic material inside the cells) and stops them from dividing.


Half-Life Elimination (biphasic): 16-24 hr (parent drug); 16-48 hr (active metabolite)

Peak plasma time: ~3 hr

Metabolism: Liver

Duration: 5-6 weeks (bone marrow recovery)

Excretion: Urine (50%); feces (<5%)


130 mg/m² PO once q6week

Drug contraindications

Hypersensitivity to this drug

Side effects

Alopecia , nausea , vomiting , Rhinitis


Myelosuppression is delayed, dose-related, and cumulative; thrombocytopenia is generally more severe than leukopenia; may occur 4-6 weeks after drug administration and persist for 1- 2 weeks; thrombocytopenia and leucopenia may contribute to bleeding and overwhelming infections in an already compromised patient; monitor blood counts weekly for 6 or more weeks after a dose; do not give therapy more frequently than every 6 weeks; bone marrow toxicity is cumulative; adjust dose based on nadir blood counts from prior dosage

Therapy should be administered by experienced cancer physician; prescribe, dispense, and administer enough capsules for one dose; fatal toxicity occurs with overdosage; prescribe, dispense, and administer only enough capsules for one dose;

Causes myelosuppression that can result in fatal infections and bleeding; monitor blood counts for at least 6 weeks after each dose; do not give more frequently than q6wk due to delayed myelosuppression

Avoid pregnancy; can cause fetal harm; advise males and females of reproductive potential of potential risk to fetus and to use effective contraception; advise males with female partners of reproductive potential to use effective contraception during treatment and for 3.5 months after the final dose; therapy may result in reduced fertility in males and females of reproductive potential

Hepatotoxicity reported; increased levels of transaminases, alkaline phosphatase and bilirubin can occur; monitor liver function

Can cause renal failure; monitor renal function

Delayed pulmonary toxicity may occur; pulmonary infiltrates and/or fibrosis may occur; perform pulmonary function tests prior to treatment and repeat frequently; permanently discontinue therapy in patients diagnosed with pulmonary fibrosis

Secondary malignancies reported; acute leukemia and myelodysplasia can occur with long-term use

Points of recommendation

 both physician and pharmacist should emphasize to patient that only one dose of the drug is taken every 6 weeks

Pregnancy level


Breast feeding warning

Unknown if metabolites present in breast milk; avoid nursing during treatment and for 2 weeks after final dose

Drug forms

Gleostine, CCNU

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