Drug intelligence / Profile preview

EPIC-1042

Development stage
Preclinical
Lead developer
Tianjin Medical University General Hospital
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

EPIC-1042 is a small molecule inhibitor of Polymerase I and transcript release factor (PTRF/Cavin1) developed for the treatment of glioblastoma (GBM). Identified through computer-aided drug design (CADD), EPIC-1042 specifically disrupts the interaction between PTRF and caveolin-1. This disruption reduces the secretion of small extracellular vesicles (sEVs) and the efflux of temozolomide (TMZ), thereby overcoming chemoresistance. Additionally, EPIC-1042 promotes the autophagic degradation of PARP1 by enhancing p62 binding and facilitating its translocation into autolysosomes. In preclinical studies, EPIC-1042 has demonstrated the ability to suppress tumor growth and sensitize GBM cells to TMZ treatment.

02

Targets

PTRF (Polymerase I and transcript release factor)CAV1 (Caveolin-1)

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