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Aragon Pharmaceuticals Doses First Patient in Phase 1/2 Clinical Trial of ARN-509 for Castration-Resistant Prostate Cancer

ARN-509 to Address Drug Resistance in Tumors Resistant to Anti-Hormonal Therapies


News provided by

Aragon Pharmaceuticals Inc.

Aug 09, 2010, 08:00 ET

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SAN DIEGO, Aug. 9 /PRNewswire/ -- Aragon Pharmaceuticals today 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 U.S. 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).

About Aragon Pharmaceuticals

Aragon Pharmaceuticals is a privately held small-molecule drug discovery company identifying breakthrough medicines for the treatment of hormonally driven cancers.  These cancers are traditionally treated with anti-hormonal therapies but often become resistant, and follow-on therapies are largely ineffective or are toxic and thus patients experience a diminished quality of life.  The company's lead compound, ARN-509, is being developed to treat patients with castration-resistant prostate cancer.  In addition, Aragon has built a research and development team with expertise in oncology, nuclear receptor biology, medicinal chemistry and drug discovery to identify and develop selective androgen receptor degraders (SARDs) for prostate cancer and selective estrogen receptor degraders (SERDs) for estrogen sensitive breast cancer.  SERDs and SARDs not only bind to and block the hormone receptors that drive tumor growth, but also induce a conformational change in these proteins that results in their degradation.

Aragon recently closed a $22 million series B financing with new investor Aisling Capital participating in the financing along with existing investors OrbiMed Advisors and The Column Group.  The financing brings the total amount of capital raised to $30 million since the company's founding.

For more information, visit www.aragonpharm.com.

Media Contact:


Heidi Chokeir, Ph.D., or David Schull

Russo Partners

(619) 528-2217

[email protected]

[email protected]

SOURCE Aragon Pharmaceuticals Inc.

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