Lomustine

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Lomustine
Lomustine Structural Formulae V.1.svg
Lomustine ball-and-stick.png
Systematic (IUPAC) name
N-(2-chloroethyl)-N'-cyclohexyl-N-nitrosourea
Clinical data
Trade names CeeNU
AHFS/Drugs.com monograph
MedlinePlus a682207
Pregnancy cat. D
Legal status Rx only
Routes Oral
Pharmacokinetic data
Bioavailability ~100%
Protein binding 50%
Metabolism hepatic
Half-life 16–48 hours
Identifiers
CAS number 13010-47-4 YesY
ATC code L01AD02
PubChem CID 3950
DrugBank DB01206
ChemSpider 3813 YesY
UNII 7BRF0Z81KG YesY
KEGG D00363 YesY
ChEBI CHEBI:6520
ChEMBL CHEMBL514 YesY
Synonyms 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea
Chemical data
Formula C9H16ClN3O2 
Mol. mass 233.695 g/mol
 YesY (what is this?)  (verify)

Lomustine (or CCNU; marketed under the name CeeNU in U.S.) is an alkylating nitrosourea compound used in chemotherapy. It is in the same family as streptozotocin. This is a highly lipid soluble drug, and thus crosses the blood-brain barrier. This property makes it ideal for treating brain tumors, and is its primary use. Lomustine has a long time to nadir (the time when white blood cells reach their lowest number).

Dose[edit]

  • Adults: 100–150 mg/m2 PO every 6 weeks (subsequent dose based on WBC)[1]
  • Cats (7,5 kg): 15 mg every 6 weeks
  • Dogs: 60–90 mg/m2 every 3 weeks

Dosage Form[edit]

10 mg, 15 mg, 40 mg, 100 mg capsules

Other[edit]

It is the "C" in the "PCV" chemotherapy regimen.

Synthesis[edit]

Lomustine synthesis:[2]

References[edit]

  1. ^ Lexi-Comp Drug Information Handbook
  2. ^ Johnston, Thomas P. (1963). "The Synthesis of Antineoplastic Agents. XXXII. N-Nitrosoureas. 1 I.". Journal of Medicinal Chemistry 6 (6): 669–681. doi:10.1021/jm00342a010.  edit

External links[edit]