Lomeguatrib is primarily used in research settings as an inhibitor of the DNA repair protein O6-alkylguanine-DNA alkyltransferase (AGT). By inhibiting AGT, it enhances the effectiveness of alkylating chemotherapeutic agents, which are commonly used in cancer treatment. This makes Lomeguatrib a potential candidate for combination therapy in tumors that are resistant to chemotherapy due to high AGT activity. It helps sensitize cancer cells to drugs like temozolomide and BCNU, improving their cytotoxic effects. Most applications remain experimental, with ongoing studies exploring its role in overcoming drug resistance in gliomas and other malignancies.