enzastaurin + temozolomide

Enzastaurin + temozolomide is a combination therapy under investigation primarily for the treatment of newly diagnosed glioblastoma multiforme (GBM) and other high-grade gliomas. Enzastaurin is an oral, first-in-class small molecule inhibitor targeting protein kinase C beta (PKCβ), as well as the PI3K and AKT pathways, exerting anti-angiogenic and antineoplastic effects. Temozolomide is an oral alkylating agent that induces DNA damage in tumor cells, leading to cell death. The combination aims to enhance antitumor efficacy by simultaneously inhibiting key signaling pathways involved in tumor growth and survival while inducing direct cytotoxicity through DNA alkylation. This regimen has been evaluated in multiple phase 1–3 clinical trials for safety and efficacy, particularly in patients with newly diagnosed or recurrent glioblastoma who are not candidates for standard chemoradiotherapy[1][2][5][6][7].