GSK525762 + trametinib

GSK525762 + trametinib is an experimental **combination therapy** composed of: - **GSK525762 (molibresib):** a selective small molecule inhibitor of BET (bromodomain and extra-terminal domain) proteins, which play a role in epigenetic regulation of gene expression, including oncogenes such as MYC. It is under development for various solid and hematologic malignancies as an epigenetic modulator[4][6]. - **trametinib:** an oral, selective, allosteric small molecule inhibitor of MEK1 and MEK2, kinases in the MAPK/ERK signaling pathway, approved for use in BRAF V600-mutant cancers (notably in melanoma, often combined with a BRAF inhibitor). Trametinib blocks MEK catalytic activity, preventing cell proliferation and survival signaling[5]. Preclinical research and xenograft studies have shown that this combination can have synergistic anti-tumor effects and overcome resistance to single-agent BET or MEK inhibitors, resulting in enhanced down-regulation of cell-cycle and survival pathways (MYC, KRAS, E2F), more potent cancer cell growth inhibition, and increased apoptosis compared to monotherapy[3]. The combination has been investigated in models of colorectal cancer, triple-negative breast cancer, multiple myeloma, and pancreatic cancer[3].

Brand names

Mekinist

Other names

molibresibGSK525762AGSK-525762AGSK 525762A