Drug intelligence / Profile preview

PPC-001 + galunisertib

Development stage
Preclinical
Lead developer
Propanc Biopharma
Modality
Small Molecules, Recombinant Proteins and Enzymes
Administration
Intravenous, Oral
01

Overview

PPC-001 + galunisertib is an investigational combination therapy being evaluated by Propanc Biopharma for the treatment of pancreatic ductal adenocarcinoma (PDAC). PPC-001 (formerly PRP) is a proprietary fixed-ratio combination of two naturally derived pancreatic proenzymes, trypsinogen and chymotrypsinogen A (1:6 ratio), which are activated upon administration to induce differentiation of cancer stem cells, reverse epithelial-mesenchymal transition (EMT), and inhibit angiogenesis. Galunisertib (LY2157299) is an oral small-molecule inhibitor of transforming growth factor-beta receptor type I (TGF-βRI) kinase, originally developed by Eli Lilly, which blocks downstream SMAD2/3 phosphorylation to suppress tumor progression and immune evasion. Preclinical studies have demonstrated that combining PPC-001 with galunisertib synergistically enhances the suppression of cancer-associated fibroblast (CAF) markers, reduces tumor cell and CAF invasion, and inhibits cell proliferation in both wild-type and gemcitabine-resistant pancreatic cancer models.

Other names
PPC-001 + GALPPC-001 + galunisertibPRP + GALPRP + galunisertibPropanc Proenzyme Combination + galunisertibtrypsinogen + chymotrypsinogen + galunisertib
02

Targets

F2R (Protease-activated receptor 1)PAR2 (Protease-activated receptor 2)SMAD2 (Mothers against decapentaplegic homolog 2)TGFB1 (Transforming growth factor Beta-1 proprotein)TGFBR1

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