Aragon Pharmaceuticals announced the dosing of the first patient in a phase 1/2 clinical trial of the company's lead compound, ARN-509, in patients with castration-resistant prostate cancer (CRPC).

The phase 1 portion of the study, being conducted at the Memorial Sloan-Kettering Cancer Center in New York City, is an open-label, dose-escalating trial evaluating the safety and tolerability of ARN-509 in patients with progressive metastatic castration-resistant prostate cancer. Other endpoints of the study include pharmacokinetics, the effect of ARN-509 on serum prostate-specific antigen levels and disease progression following treatment with ARN-509. The focus of the phase 2 portion of the study is to determine ARN-509 activity in distinct CRPC patient populations and to define dosing for optimal therapeutic activity and safety to be used in subsequent clinical trials.

"There is a huge medical need for novel therapies that address the problem of drug resistance in hormone refractory cancers, such as breast and prostate cancer, as more than 90,000 people die from these cancers in the US every year," said Richard A. Heyman, Ph.D., President and CEO of Aragon. "With its novel mechanism of action, ARN-509 has the potential to be a best-in-class therapeutic that offers a new alternative for patients who currently have limited treatment options."

ARN-509 is an androgen receptor antagonist that inhibits nuclear translocation and DNA binding of the receptor, thereby modulating expression of genes that drive prostate cancer growth.

Aragon Pharmaceuticals was founded in May 2009 in San Diego based on the convergence of the work of co-founders Charles Sawyers, M.D., Howard Hughes Medical Institute investigator at Memorial Sloan-Kettering Cancer Center, and Michael E. Jung, Ph.D., professor of chemistry and biochemistry at University of California, Los Angeles (UCLA).

Aragon Pharmaceuticals is a privately held small-molecule drug discovery company identifying breakthrough medicines for the treatment of hormonally driven cancers.