Lomustine is an alkylating drug from the nitrosourea type. It is indicated in the treatment of primary and metastatic brain tumors and brain neoplasm. This drug can also be used in the treatment of refractory or relapsed Hodgkin's disease, as a secondary therapy. Lomustine goes through many reactions in the cell, its metabolites alkylate the DNA (transfers the chloroethyl group of lomustine to the O6 methyl of guanine) and cause interstrand and intrastrand cross-linkings at the O6 position of the guanine bases. This results in the inhibition of DNA synthesis. Furthermore, this blocks the proliferation of the cancerous cell, thus the cell goes through apoptosis. The drug is also metabolized to carbamyolating compounds, which will exhibit a certain cytotoxicity through their actions on proteins. It is believed that, in general, nitrosoureas are metabolized to beta-chloroethanol (alkylating agent) and alkylisocyanate (carbamoylating agent). This drug is administered as an oral tablet/capsule.

Lomustine Pathway References