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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › ALKYLATING AGENTS › Nitrosoureas
lomustine
L01AD02
Forms & Strengths
- Capsules: 10 mg
- Capsules: 40 mg
- Capsules: 100 mg
Adult Dosing
- Brain tumors and Hodgkin lymphoma: 130 mg/m² orally as a single dose every 6 weeks
- Repeat doses should not be given until bone marrow recovery is adequate (platelets > 100,000/mcL, leukocytes > 4,000/mcL)
- Adjust subsequent doses based on nadir blood counts from the preceding dose
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been firmly established
- Dosing regimens in pediatric protocols generally mirror adult body surface area calculations (130 mg/m² every 6 weeks)
Indications
- Brain tumors (primary and metastatic) as adjunctive therapy
- Hodgkin lymphoma as secondary therapy in combination with other approved agents
Mechanism of Action
- Alkylating agent (nitrosourea)
- Inhibits synthesis of both DNA and RNA through carbamoylation and alkylation of DNA strands
- Crosses the blood-brain barrier readily due to high lipid solubility
Contraindications
- Hypersensitivity to lomustine or any component of the formulation
- Severe bone marrow suppression
Adverse Reactions
- Delayed myelosuppression (cumulative, dose-limiting, nadir at 4 to 6 weeks)
- Thrombocytopenia and leukopenia
- Nausea and vomiting (acute, usually within 3-6 hours of administration)
- Pulmonary toxicity (fibrosis, infiltrates)
- Hepatotoxicity (transient elevations in liver enzymes, jaundice)
- Stomatitis and alopecia
Drug Interactions
- Myelosuppressive agents: Increased bone marrow toxicity and immunosuppression
- Coadministration with hepatotoxic drugs may increase the risk of liver injury
- Live vaccines: Risk of severe or fatal infections due to immunosuppression
- CYP inhibitors/inducers: Potential pharmacokinetic alterations (lomustine undergoes extensive hepatic metabolism via CYP450 enzymes)
Curated Content: Needs Vetting Before Put to Clinical Use