| Item |
Information |
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Drug Groups
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approved |
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Description
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An alkylating agent of value against both hematologic malignancies and solid tumors. [PubChem] |
| Indication |
For the treatment of primary and metastatic brain tumors as a component of combination chemotherapy in addition to appropriate surgical and/or radiotherapeutic procedures. Also used in combination with other agents as secondary therapy for the treatment of refractory or relapsed Hodgkin's disease. |
| Pharmacology |
Lomustine is an alkylating agent of the nitrosourea type. Lomustine and its metabolites interferes with the function of DNA and RNA. It is cell cycle–phase nonspecific. Cancers form when some cells within the body multiply uncontrollably and abnormally. These cells then spread and destroy nearby tissues. Lomustine acts by slowing this process down. It kills cancer cells by damaging the DNA (the genetic material inside the cells) and stops them from dividing. |
| Toxicity |
Oral, rat: LD50 = 70 mg/kg. Pulmonary toxicity has been reported at cumulative doses usually greater than 1,100 mg/m2. There is one report of pulmonary toxicity at a cumulative dose of only 600 mg. The onset of toxicity has varied from 6 months after initiation of therapy, to as late as 15 years after. |
| Affected Organisms |
| • |
Humans and other mammals |
|
| Biotransformation |
Hepatic. Rapid and complete, with active metabolites. |
| Absorption |
Well and rapidly absorbed from the gastrointestinal tract. |
| Half Life |
Approximately 94 minutes, however the metabolites have a serum half-life of 16 to 48 hours. |
| Protein Binding |
50% |
| Elimination |
Following oral administration of radioactive CeeNU at doses ranging from 30 mg/m2 to 100 mg/m2, about half of the radioactivity given was excreted in the urine in the form of degradation products within 24 hours. |
| External Links |
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