lomeguatrib + temozolomide

Lomeguatrib + temozolomide is a combination therapy consisting of lomeguatrib, a potent small molecule inhibitor of O6-methylguanine-DNA methyltransferase (MGMT), and temozolomide, an oral alkylating agent. Lomeguatrib acts as a pseudosubstrate that inactivates MGMT, an enzyme responsible for repairing DNA damage caused by alkylating agents like temozolomide. By inhibiting MGMT, lomeguatrib aims to overcome resistance to temozolomide and enhance its cytotoxic effects against tumor cells. This combination has been investigated primarily in advanced cancers such as glioblastoma, metastatic melanoma, and metastatic colorectal cancer. Clinical studies have shown that while the regimen effectively depletes MGMT activity and increases markers of apoptosis in tumor cells, its efficacy compared to temozolomide alone has been limited in some settings; dose-limiting toxicities are mainly hematologic[1][2][3][6].

Other names

LM + TMZlomeguatrib-temozolomide combination