Drug intelligence / Profile preview

PEP-010

Development stage
Unknown
Lead developer
PEP-Therapy
Modality
Modified Peptides → Peptides
Administration
Intravenous
01

Overview

PEP-010 is a first-in-class bifunctional therapeutic peptide developed for the treatment of advanced solid tumors, including metastatic pancreatic ductal adenocarcinoma and platinum-resistant ovarian cancer. It is designed using CP&IP (Cell Penetrating & Interfering Peptides) technology and consists of two functional domains: an optimized cell-penetrating peptide that delivers the active component into the cytosol and a short interfering peptide that specifically disrupts the protein-protein interaction between caspase-9 and protein phosphatase 2A (PP2A). By dissociating this interaction, PEP-010 restores normal apoptosis in cancer cells—a process often dysregulated in malignancies—without affecting physiological mechanisms. The drug has demonstrated good safety and tolerability profiles as well as preliminary antitumor activity in preclinical models and early-phase clinical trials. It is currently being evaluated both as monotherapy and in combination with standard chemotherapies such as paclitaxel or gemcitabine[2][3][5][6][7].

02

Targets

CASP9 (Caspase-9)PP2A (Protein phosphatase 2A)

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