Lomeguatrib

Lomeguatrib is an orally bioavailable small molecule that acts as a potent and highly specific inhibitor of O6-methylguanine-DNA methyltransferase (MGMT), a DNA repair enzyme. By serving as a pseudosubstrate, lomeguatrib covalently inactivates MGMT, thereby preventing the repair of O6-alkylguanine lesions in DNA. This mechanism sensitizes tumor cells to the cytotoxic effects of O6-alkylating agents such as temozolomide and BCNU, which are commonly used chemotherapeutics. Lomeguatrib was developed primarily for use in combination with these agents to overcome resistance mediated by MGMT activity in various cancers, including melanoma, colorectal cancer, glioblastoma, prostate cancer, and other solid tumors. The drug was initially developed by AstraZeneca and has been evaluated in phase I and II clinical trials; however, its global development status is discontinued[1][2][3][4][5][8].

Other names

6-(4-bromo-2-thienyl) methoxy purin-2-amine