This invention relates to the field of
biomedical technology, and more particularly to the use of a combination of RVX208 and
temozolomide for the treatment of
glioblastoma. It also relates to the use of RVX208 to resensitize
temozolomide-resistant cancers to
temozolomide treatment. The use of at least one of RVX208, a pharmaceutically acceptable salt of RVX208, a solvate of RVX208, a
hydrate of RVX208, a polymorph of RVX208, an isomer of RVX208, a
prodrug form of RVX208, and temozolomide in the preparation of a
glioblastoma therapeutic agent. RVX208 inhibits the
transcriptional activity of various genes related to
cell cycle progression and proliferation maintenance by inhibiting BET family proteins or other target molecules, leading to
cell cycle arrest, inhibition of
cell proliferation, and induction of
programmed cell death. RVX208 also interferes with the
transcriptional expression of genes related to mitochondrial
homeostasis regulation, resulting in a decrease in mitochondrial
membrane potential and reduced
ATP production, thus enabling RVX208 to disrupt mitochondrial function in GBM cells and produce a synergistic antitumor effect with temozolomide.