buparlisib + temozolomide

Buparlisib (BKM120) is an orally bioavailable, selective pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor. Temozolomide is an oral alkylating agent used primarily in the treatment of glioblastoma and other high-grade gliomas. The combination of buparlisib and temozolomide has been investigated for synergistic cytotoxicity in glioma cells and newly diagnosed glioblastoma patients. Buparlisib inhibits the PI3K pathway, which is frequently dysregulated in glioblastoma, leading to abnormal cell growth and proliferation. In preclinical studies, BKM120 sensitizes tumor cells to temozolomide by promoting apoptosis and reversing drug resistance mechanisms such as MGMT overexpression via inhibition of NF-κB p65[1]. Clinical trials have evaluated this combination with or without radiotherapy for safety, tolerability, maximum tolerated dose (MTD), and preliminary antitumor activity[2][3][7]. The primary indication under investigation is newly diagnosed or recurrent glioblastoma.

Brand names

TemodarTemodal

Other names

BKM120 + temozolomideBKM120 + TMZbuparlisib + temozolomide