Researchers have identified a novel compound that can block testosterone from fuelling the tumours in mice and act as a new generation therapy for prostate cancer.
“Prostate cancer is the most prevalent form of cancer in men, and the principal driver of tumour growth is the androgen receptor,” said John D. Norris, Associate Professor at Duke University in North Carolina, US.
The new compound, called tetraaryl cyclobutane, or CB, is being studied as an option for prostate tumours that have grown resistant to current anti-androgen drugs, notably enzalutamide.
“Suppression of androgen receptor function by anti-endocrine therapies is initially effective, but most tumours develop resistance, resulting in a more aggressive cancer,” Norris added.
The new compound act as competitive inhibitors of androgen receptors, but are structurally different from current anti-androgens such as enzalutamide.
One of the CB compounds, inhibits mutant forms of the androgen receptors that promote resistance to enzalutamide.
It functions by preventing the androgen receptor from entering the nucleus of the cell where it can promote tumour growth.
“It’s encouraging that this compound has a different mechanism of action when compared to current therapies, which gives it a good chance of having efficacy in resistant disease,” Norris said.
Animal models have showed that the compound is active against prostate tumours where enzalutamide fails, the researchers concluded in the paper published online in the journal Nature Chemical Biology.
Aug 9, 2016