The Sound of Evolution
Lomustine
Mechanism of action:
Lomustine is an alkylating agent and a nitrosourea derivative. Lomustine undergoes spontaneous decomposition in the body to generate highly reactive alkylating intermediates. These reactive molecules bind to guanine bases in DNA, causing DNA base modification and structural abnormalities. Lomustine can induce cross-linking between two DNA strands (interstrand) or within the same strand (intrastrand), thereby preventing normal DNA unwinding, replication, and transcription and ultimately triggering cell death.
Reference(s):
1. Larkin JM et al. (2007). A phase I/II study of lomustine and temozolomide in patients with cerebral metastases from malignant melanoma. Br J Cancer.
2. Spiro T et al. (2000). New cytotoxic agents for the treatment of metastatic malignant melanoma: temozolomide and related alkylating agents in combination with guanine analogues to abrogate drug resistance. Forum (Genova).