Last reviewed 2026-04-20 · How we verify

Gleostine (LOMUSTINE)

Gleostine works by attaching an alkyl group to the DNA of cancer cells, interfering with their ability to replicate and ultimately leading to cell death.

Gleostine (Lomustine) is a small molecule alkylating drug originally developed by CORDEN PHARMA and currently owned by Azurity. It was FDA approved in 1976 for the treatment of Hodgkin's disease and brain neoplasms. As an off-patent medication, Gleostine is available as a generic formulation. Key safety considerations include its potential for myelosuppression and hepatotoxicity. Gleostine is a well-established treatment option for certain types of cancer.

At a glance

Mechanism of action

Lomustine alkylates DNA and RNA. As with other nitrosoureas, it may also inhibit several key enzymatic processes by carbamoylation of amino acids in proteins.

Approved indications

• Hodgkin's disease
• Neoplasm of brain

Boxed warnings

• WARNING: DELAYED MYELOSUPPRESSION AND RISK OF OVERDOSAGE DELAYED MYELOSUPPRESSION Gleostine causes myelosuppression including fatal myelosuppression. Myelosuppression is delayed, dose-related, and cumulative; occurring 4 to 6 weeks after drug administration and persisting for 1 to 2 weeks. Thrombocytopenia is generally more severe than leukopenia. Cumulative myelosuppression from Gleostine is manifested by greater severity and longer duration of cytopenias. Monitor blood counts for at least 6 weeks after each dose. Do not give Gleostine more frequently than every 6 weeks [see Warnings and Precautions ( 5.1 ), Dosage and Administration ( 2.2 , 2.3 )] . RISK OF OVERDOSAGE PRESCRIBE, DISPENSE, AND ADMINISTER ONLY ENOUGH CAPSULES FOR ONE DOSE. Fatal toxicity occurs with overdosage of Gleostine. Both physician and pharmacist should emphasize to the patient that only one dose of Gleostine is taken every 6 weeks [see Dosage and Administration ( 2.1 ), Warnings and Precautions ( 5.2 ), Overdosage ( 10 )] . WARNING: DELAYED MYELOSUPPRESSION and RISK OF OVERDOSAGE See full prescribing information for complete boxed warning. Delayed Myelosuppression Gleostine causes myelosuppression including fatal myelosuppression. Myelosuppression is delayed, dose-related, and cumulative. Thrombocytopenia is generally more severe than leukopenia. Monitor blood counts and do not give Gleostine more frequently than every 6 weeks. ( 2.2 , 2.3 , 5.1 ) Risk of Overdosage PRESCRIBE, DISPENSE, AND ADMINISTER ONLY ENOUGH CAPSULES FOR ONE DOSE. Fatal toxicity occurs with overdosage of Gleostine. Both physician and pharmacist should emphasize to patient that only one dose of Gleostine is taken every 6 weeks. ( 2.1 , 5.2 , 10 )

Common side effects

• Nausea
• Vomiting
• Stomatitis
• Alopecia
• Delayed myelosuppression
• Nephrotoxicity
• Hepatotoxicity
• Pulmonary toxicity
• Secondary malignancies
• Risks of overdosage
• Optic atrophy
• Visual disturbances

Key clinical trials

• A Single-arm, Prospective Study of a Cladribine-Bridged LABU Conditioning Regimen in Allogeneic Hematopoietic Stem Cell Transplantation for Relapsed/Refractory MDS/AML in Elderly Patients (NA)
• Anti-Lag-3 (Relatlimab) and Anti-PD-1 Blockade (Nivolumab) Versus Standard of Care (Lomustine) for the Treatment of Patients With Recurrent Glioblastoma (PHASE2)
• Study on the Efficacy and Safety of the TmBU Conditioning Regimen in High-risk or Relapsed/Refractory Acute Leukemia (PHASE2)
• Study of TLX101-Tx Plus Standard of Care (SoC) Versus SoC Alone for the Treatment of Patients With Recurrent Glioblastoma (PHASE3)
• Comprehensive Analysis of Chemotherapy and Targeted Therapy Outcomes in Recurrent Malignant Gliomas
• A Study of Treatment for Medulloblastoma Using Sodium Thiosulfate to Reduce Hearing Loss (PHASE3)
• Reduced Craniospinal Radiation Therapy and Chemotherapy in Treating Younger Patients With Newly Diagnosed WNT-Driven Medulloblastoma (PHASE2)
• Lomustine With and Without Reirradiation for First Progression of Glioblastoma: a Randomized Phase III Study (PHASE3)

Primary sources

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