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Carmustine + O6-benzylguanine is a combination therapy consisting of the alkylnitrosourea carmustine (BCNU) and the O6-alkylguanine-DNA alkyltransferase (AGT) inhibitor O6-benzylguanine. O6-benzylguanine works by inhibiting AGT through suicide inactivation, thereby preventing the repair of DNA damage caused by carmustine. This combination was developed to overcome resistance to nitrosourea therapy in malignant gliomas and other cancers. The maximum tolerated dose of carmustine when combined with O6-benzylguanine at 100 mg/m² was determined to be 40 mg/m² administered at 6-week intervals.
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