REVIEW Carmustine is a mustard gas-related compound used in the treatment of many cancers, including brain cancer, multiple myeloma and lymphoma. It causes cross-links in DNA and RNA in all cell cycle phases, resulting in disruption of DNA function, cell cycle arrest, and apoptosis. Carmustine also binds to and modifies glutathione reductase. Carmustine is highly lipophilic and readily crosses the blood-brain barrier.
Carmustine is sometimes used in conjunction with alkyl guanine transferase (AGT) inhibitors, such as O6-benzylguanine. The AGT inhibitors increase the efficacy of carmustine by inhibiting the direct reversal pathway of DNA repair, which will prevent formation of the interstrand crosslink between the N1 of guanine and the N3 of cytosine.
Johnston, Thomas P.; McCaleb, George S.; Montgomery, John A. The synthesis of antineoplastic agents. XXXlI. N-Nitrosoureas. 1 Journal of Medicinal Chemistry (1963), 6(6), 669-81.
Wheeler, Glynn P.; Bowdon, Bonnie J. Some effects of 1,3-bis(2-chloroethyl)-1-nitrosourea on the synthesis of protein and nucleic acids in vivo and in vitro Cancer Research (1965), 25(10), 1770-8.
Yanko, W. H.; et al. 1,3-Bis(2-chloroethyl)-1-nitrosourea U. S. Pat. Appl. (1974), US 523334 19741113.
Carter, Stephen K.; Schabel, Frank M., Jr.; Broder, Lawrence; Johnston, Thomas P. 1,3-Bis(2-chloroethyl)-1-nitrosourea (BCNU) and other nitrosoureas in cancer treatment. Review Advances in Cancer Research (1972), 16, 273-332.