Description
Lomeguatrib is an anticancer chemotherapeutic compound that is used as a pseudosubstrate for O6-methylguanine-DNA methyltransferase (MGMT), inactivating the enzyme and inhibiting DNA repair across many cancer cell lines. Lomeguatrib is currently in clinical trials as a co-administered compound that increases the efficacy of chemotherapeutics such as temozolomide and dacarbazine in the treatment of melanoma and other solid tumors. In glioblastoma cells, lomeguatrib decreases activity of MGMT and increases expression of p53, inducing DNA fragmentation and apoptosis.