MTP156

MTP156 is a novel indole-based multitarget small molecule (MSM) designed for the treatment of glioblastoma. It was developed by combining pharmacophoric moieties from the HDAC pan-inhibitor belinostat and the multi-target compound contilisant. MTP156 is engineered to simultaneously inhibit histone deacetylases (HDACs), monoamine oxidases (MAOs), and cholinesterases (ChEs), while also acting as a histamine H3 receptor (H3R) antagonist and a sigma-1 receptor (S1R) agonist. In preclinical studies, MTP156 demonstrated potent cytotoxic activity against glioma cells and impaired glioma stem cell (GSC) activity. Computational models predict that the molecule is capable of crossing the blood-brain barrier, addressing a critical challenge in treating primary brain tumors.