Section 14 · Monograph
Lomustine
Reviewed Nov 2026FDA label
GleostineNitrosourea alkylator
- Forms
- Cap: 5, 40, 100mg
- Dose
- 130mg/m² single oral dose every 6 weeks (reduce if marrow compromised)
- MOA
- Crosslinks DNA/RNA; crosses blood-brain barrier
Black Box Warning
- Delayed myelosuppression (thrombocytopenia and leukopenia) that may contribute to bleeding and infection; do not give more often than every 6 weeks; monitor blood counts weekly for at least 6 weeks after each dose
- Overdosage: dispense only the number of capsules needed for a single dose to avoid fatal overdose
Indications
- Primary and metastatic brain tumors as part of multimodal regimens (after surgery/radiation)FDA-labeled
- Relapsed Hodgkin lymphoma (in combination)FDA-labeled
Mechanism of Action
- Nitrosourea alkylating agent that crosslinks DNA and RNA; lipophilic and crosses the blood-brain barrier
Full Dosing
Adult / usual
- 130mg/m² as a single oral dose every 6 weeks; reduce to 100mg/m² in patients with compromised marrow function; adjust for nadir counts
- Take on an empty stomach; antiemetic premedication
- Single dose per prescription to avoid overdose
Contraindications
- Known hypersensitivity to lomustine
Drug Interactions
- Additive myelosuppression with other myelosuppressive agents and radiation
Adverse Effects
- Delayed myelosuppression
- Nausea and vomiting
- Pulmonary toxicity and fibrosis (risk rises with cumulative dose, especially above about 1,100mg/m²)
- Hepatotoxicity and nephrotoxicity
- Secondary malignancies
Monitoring Parameters
- CBC weekly for at least 6 weeks after each dose
- Liver and renal tests at baseline and periodically
- Baseline and periodic pulmonary function tests; track cumulative dose
Pregnancy & Lactation
- Embryo-fetal toxicity; contraception during and after treatment
- Breastfeeding not recommended