MPT0L145

MPT0L145 is a **first-in-class, dual inhibitor** of **phosphatidylinositol 3-kinase catalytic subunit type 3** (PIK3C3, also known as Vps34) and **fibroblast growth factor receptors** (FGFR, with selectivity for FGFR1, FGFR2, and FGFR3). It acts by blocking autophagy via PIK3C3 inhibition and simultaneously inducing autophagosome formation through FGFR inhibition, thereby perturbing autophagic flux and promoting cancer cell death. It also induces G1 cell cycle arrest, production of reactive oxygen species (ROS), and DNA damage in cancer cells. In preclinical models, MPT0L145 has shown potential to overcome drug resistance, sensitize cancer cells to other anticancer agents (e.g., gefitinib, gemcitabine, abemaciclib), and has demonstrated blood-brain barrier permeability comparable to temozolomide. It is under investigation primarily for **bladder cancer**, **glioblastoma multiforme (GBM)**, and other solid tumors[1][2][3][4][6][8].