Phortress - CYP-activated DNA-interactive agent

Phortress is the lead compound from work by our group on CYP-activated DNA-interactive anti-cancer agents. Phortress is a water-soluble pro-drug that is synthetically accessible and has been formulated for intravenous administration. It has a distinctive mechanism of action whereby in tumour cells sensitive to the drug the active moiety binds to aryl hydrocarbon receptors in the cytoplasm and is subsequently translocated into the cell nucleus, where it induces its own activation via cytochrome P450 1A1. The resulting electrophilic intermediate species form DNA adducts leading to highly selective cell death.

In preclinical studies (in vitro and in vivo) by both Cancer Research UK and NCI in the US, Phortress has demonstrated potent anti-tumour activity, particularly in breast, ovarian, renal and lung cancer.

Cancer Research UK is currently sponsoring and conducting a Phase I clinical study to establish the safety, pharmacokinetic, pharmacodynamic and early clinical profiles of Phortress in cancer patients. Interim results from the study, which were presented at an international cancer conference in October 2008, showed that the drug had been well tolerated at the doses tested so far, and that three out of nine patients had had stable disease for periods of at least six months whilst on the study.

Pharminox has an exclusive option from Cancer Research UK to license worldwide rights to Phortress and related compounds for cancer.

Phortress is synthetically accessible and has been formulated for intravenous administration.

Preclinical studies (in vitro and in vivo) by both Cancer Research UK and NCI in the US have shown Phortress to be a potent anti-cancer agent, particularly against breast, ovarian, renal and lung cancer.