temozolomide + O6-benzylguanine + irinotecan

This is a combination regimen of three small molecule drugs: temozolomide, an oral alkylating agent; O6-benzylguanine, an inhibitor of the DNA repair enzyme methylguanine-DNA methyltransferase (MGMT); and irinotecan, a topoisomerase I inhibitor. Temozolomide induces cytotoxicity by methylating DNA at several sites, most notably the O6 position of guanine. MGMT repairs this lesion and confers resistance to temozolomide; thus, inhibition by O6-benzylguanine enhances the efficacy of temozolomide. Irinotecan inhibits topoisomerase I, leading to DNA damage during replication. The combination has been investigated in preclinical models and early-phase clinical trials for recurrent or progressive malignant glioma and neuroblastoma due to potential synergistic anti-tumor effects[1][2][3][4].

Brand names

TemodarCamptosar

Other names

TMZO6-BGO-6-BGO 6-BGCPT-11CPT11CPT 11