How did lomustine become standard of care in recurrent glioblastoma?

Lomustine, also known as CCNU (chloroethyl-cyclohexyl-nitrosourea), is an alkylating agent of the nitrosourea family [1,2,3] (Fig. 1). It is a monofunctional alkylating agent which alkylates DNA and RNA and can cross-link DNA and thus acts in a cell cycle-dependent and -independent manner. One of the most relevant lesions induced by lomustine, the formation of O6-chloroethylguanine, can be reverted by O6-methylguanine DNA methyltransferase (MGMT). Lomustine may also inhibit enzymatic functions by carbamoylation of amino acids but the contribution of this activity to clinical activity remains unknown.
Source: Cancer Treatment Reviews - Category: Cancer & Oncology Authors: Tags: Anti-tumour Treatment Source Type: research