Ferring's degarelix set for Phase III trials

Degarelix, a novel GnRH receptor blocker from Ferring, has shown immediate onset of action and sustained activity in men with prostate cancer, thereby paving the way for Phase III studies.

The results of the Phase II dose-escalating study were presented at the XXth congress of the European Association of Urologists (EAU) in Istanbul, Turkey. The multi-centre, randomised trial in 172 men, aged 48-89, tested the efficacy of degarelix by monitoring levels of testosterone and prostate-specific antigen (PSA) in patients treated with doses between 120mg and 320mg at concentrations between 20 to 60 mg/mL. The effects were found to be dependent on dose and concentration, with the best response achieved by an initial dose of 240 mg (40mg/mL), such that 96% of the patients had T levels less than or equal to 0.5 ng/mL at day three and at day 28.

Blocking the body's production of testosterone with degarelix may represent benefits for patients. It appears to avoid problems traditionally associated with hormonal treatment, such as symptoms associated with the initial testosterone surge and severe flare of disease.

'The results of this trial play a key role for planning the late-stage full development of degarelix,' explained Dr Bo-Eric Persson, director of medical sciences, urology/oncology, Ferring.

The majority of tumours found in newly diagnosed prostate cancer patients are dependent on testosterone for their continued growth and are linked to raised levels of PSA. Currently used hormonal treatments for prostate cancer include GnRH agonists, which, unlike degarelix, stimulate the GnRH receptor on the pituitary gland. These agents eventually have a desired clinical effect, but they stimulate testosterone production before shutting it down, thereby encouraging hormone-dependent tumour growth, rather than inhibiting it, and potentially leading to a temporary worsening of cancer symptoms or flare.

Degarelix is a synthetic peptide GnRH blocker modeled on the body's own gonadotrophin-releasing hormone. This creates a fast, profound and sustained suppression of testosterone production without surge, thus avoiding the risk of flare. With GnRH blockers there is no need to administer a second hormonal agent, called an anti-androgen, normally used to combat the flare responses that often accompany GnRH agonists.

Prostate cancer is the second leading cause of cancer death in men in industrialised societies, accounting for around one in six male cancer-related deaths. It is currently only exceeded by lung cancer but, with the ageing population, is expected to overtake it within the next ten years.