Drug intelligence / Profile preview

MTP150

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

MTP150 is a novel indole-based multitarget small molecule (MSM) designed for the treatment of glioblastoma. It was developed by integrating pharmacophoric elements from the HDAC inhibitor belinostat and the multi-target compound contilisant. MTP150 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. Preclinical studies indicate that MTP150 can cross the blood-brain barrier and effectively impair glioma stem cell (GSC) activity. In vivo models have demonstrated significant tumor growth inhibition when used as a monotherapy or in combination with temozolomide (TMZ), primarily through the disruption of cell cycle regulation pathways.

02

Targets

HTR6 (5-hydroxytryptamine receptor 6)AcetylcholinesteraseButyrylcholinesteraseHDAC1 (Histone Deacetylase 1)HDAC6 (Histone deacetylase 6)HRH3 (Histamine Receptor H3)MAOA (Monoamine oxidase A)SIGMAR1 (Sigma non-opioid intracellular receptor 1)

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