About PENAO

PENAO is a novel, proprietary anti-cancer compound that contains an active arsenic molecule to disrupt a key molecule in cancer cell growth.

PENAO is a second-generation compound of GSAO. PENAO has been shown to accumulate in cells at a rate 85-fold faster than GSAO, which results in a 44-fold increased anti-proliferative activity and a ~20-fold increased anti-tumour efficacy in mice.

How does PENAO work?

  • PENAO enters tumor cells and accumulates in the mitochondria where it cross-links two amino acids on a transport protein known as adenine nucleotide translocase (ANT). This inactivates the transporter and leads to death of the cell.
  • PENAO has shown pre-clinical activity in a variety of cancers including ovarian, breast, and pancreatic cancer. It is the only ANT inhibitor in clinical development.

PENAO combines well with marketed drugs

mTOR inhibitors (eg. everolimus)

The combination of PENAO and mTOR inhibitors is strongly synergistic, leading to effective deletion of mTOR protein in tumour cells, proliferation arrest, enhanced mitochondrial disruption and rapid induction of cell death – Tsoli et al, Oncotarget, 2018.

epidermal growth factor receptor (EGFR) inhibitors (eg. gefitinib)

Combining gefitinib and PENAO resulted in synergistic inhibition in both a time- and dose-dependent manner in 3 sarcoma cell lines with less prominent monotherapy effects – Wang et al, Oncotarget, 2020.