First-in-class dimerisation inhibitors of the androgen receptor as a new treatment for prostate cancer

Eva Estébanez


    Eva Estébanez


    Fundació Bosch i Gimpera, Universitat de Barcelona, Spain


    Prostate cancer (PCa) is the most common cancer in men, affecting one in six men worldwide, and one of the leading causes of cancer death. Male hormones (androgens) such as testosterone and its specific receptor, the androgen receptor (AR), play a central role in the emergence, growth and ultimately metastasis of PCa. For this reason, AR has been the primary target of drug development for the treatment of this cancer. The strategy followed so far to create the so-called antiandrogens is based on compounds capable of competing with the hormone for their specific binding site within the AR. However, tumor cells stop responding to these drugs in 2-3 years, which can even exacerbate tumor growth.

    This project aims to take advantage of the recent results on the 3D structure of the active form of AR to develop drugs against PCa with a novel mode of action (MoA), capable of avoiding this ‘resistance’ to classic antiandrogens. The main beneficiaries of the new generation of antiandrogens to be developed will be PCa patients, especially those who are already resistant to the antiandrogens used in the clinic.