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Lomustine

Alkylating Agent · Antineoplastic

Also known as CCNU

Alkylating AgentAntineoplastic
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 12
  • AdalimumabSevereDatabaseDDInter
  • BaricitinibSevereDatabaseDDInter
  • CertolizumabSevereDatabaseDDInter
  • CimetidineSevereDatabaseDDInter

Mechanism

Lomustine, a nitrosourea, exerts its cytotoxicity through spontaneous breakdown to the 2-chloroethyl diazonium ion, an alkylating intermediate. This strong electrophile alkylates guanine, cytidine, and adenine bases, leading to interstrand or intrastrand cross-linking of DNA. It also causes carbamylation of DNA, thereby inhibiting DNA synthesis.

Indications

CNS tumorslymphomaHodgkin diseasebrain tumorsgliomas (as part of PVC regimen)Meningeal leukaemiasBrain cancer

Dosing

Adult
counts must be checked before each treatment, and doses should be reduced or therapy delayed if bone-marrow has not recovered. Cytotoxic drugs may be contra-indicated in patients with acute infection; any infection should be treated before, or when starting, cytotoxic drugs.…

Pharmacokinetics

Onset
not specified
Peak effect
not specified
Bioavailability
orally bioavailable
Protein binding
not specified
Metabolism
Undergoes spontaneous breakdown to an alkylating intermediate, the 2-chloroethyl diazonium ion.

Contraindications

  • Acute infection

Side effects

Common
Bone-marrow suppressionAlopeciaStomatitisprofound and delayed myelosuppression (recovery 4-6 weeks after single dose)NauseaVomitingCNS effects
Serious
  • Pulmonary fibrosis
  • Carcinogenic effects
  • renal failure (especially semustine, with long-term treatment courses)
  • pulmonary dysfunction (with repeated treatment courses)
  • prolonged bone marrow toxicity (with repeated treatment courses)
  • highly carcinogenic
  • mutagenic
  • Delayed bone marrow depression
  • Visceral fibrosis
  • Renal damage

Drug interactions

Adalimumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Baricitinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Certolizumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cimetidine
Severe
Database

Drug interaction classified as: synergy, metabolism

Source: DDInter

Cladribine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Clozapine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Deferiprone
Severe
Database

Clinical effect not specified

Source: DDInter

Etanercept
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Fingolimod
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Golimumab
Severe
Database

Clinical effect not specified

Source: DDInter

Infliximab
Severe
Database

Clinical effect not specified

Source: DDInter

Leflunomide
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

Other Alkylating Agent drugs

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Sources: KD Tripathi 7e, Goodman & Gilman 14e, BNF·Verified: 2026-05-13 · House clinical team