CEN-209 is selectively activated in areas of low oxygen often found within solid tumors.
Auckland Cancer Society Research Centre (ACSRC) professor William Wilson and associate professor Michael Hay, along with other researchers identified and characterized CEN-209 under the name SN30000.
According to Wilson, CEN-209 was created by improving upon tirapazamine (TPZ), another substance which attacked hypoxic cells but did not improve patient outcomes, in part because TPZ does not penetrate deeply enough into solid tumors to be effective.
Hay said the computer models of drug transport developed in-house at ACSRC allowed the synthetic chemists to test their design theories through computer simulations, which considerably shortened the discovery process.
Centella Therapeutics president Thorsten Melcher said radiotherapy works by damaging tumor cells’ DNA, but only in well-oxygenated areas, whereas CEN-209 is designed to ‘switch on’ and damage the DNA only of hypoxic cells, leaving other cells alone.
"Thus, the two treatment approaches have the potential to complement each other, and CEN-209 is specifically designed to be preferentially used in combination with radiotherapy," Melcher said.
Centella plans to develop CEN-109, an investigational positron emission tomography (PET) imaging agent that is designed to identify tumors with hypoxic areas.