An international team of researchers, led by Pfizer in collaboration with Monash University and the Australian-based Cancer Therapeutics Cooperative Research Centre, have discovered a pre-clinical drug candidate demonstrating anti-tumour activity in Estrogen Receptor (ER) positive breast cancer models.

The study describes the identification of a highly potent, selective and orally bioavailable ‘KAT6A/B’ inhibitor called ‘CTx-648’ which led to promising tumour growth inhibition in ER-positive breast cancer models in mice.

The team of researchers also found CTx-648 treatment led to anti-tumour activity in tumours resistant to hormone therapy, a common line of treatment for ER-positive breast cancer patients. As such, the discovery of CTx-648 presents a new opportunity to target KAT6A in patients with ER-positive breast cancer.

“There is an urgent need for new safe and effective treatments for ER-positive breast cancer and the team is excited that a KAT6A inhibitor is currently in Phase I clinical trials,” said Professor Paul Stupple, Director of Medicinal Chemistry at the Monash Institute of Pharmaceutical Sciences (MIPS).