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Lomustine is an oral chemotherapy drug classified as a nitrosourea alkylating agent. It is used alone or in combination with other medicines to treat brain tumors, Hodgkin's lymphoma, and other types of cancer. Lomustine works by undergoing hydrolysis in the body to form reactive metabolites that cause alkylation and cross-linking of DNA (primarily at the O6 position of guanine bases) and RNA, leading to cytotoxicity and inhibition of cell division. Its high lipid solubility allows it to cross the blood-brain barrier effectively, making it particularly useful for treating central nervous system malignancies. Lomustine also inhibits DNA synthesis and can affect various cellular processes including protein modification through carbamoylation.
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