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Institute of Cancer Research scientists proposed that the malignant growth of certain prostate cancers was driven by bodily production of male sex hormones (androgens). This highlighted the androgen biosynthetic pathway as a target for drug intervention. In the early 1990s, the ICR undertook a drug discovery research programme to identify compounds that could inhibit the synthesis of testosterone and identified and patented compound CB7598 which was named abiraterone.

Abiraterone 3D ModelThe team went on to carry out in vivo pharmacokinetic and biochemical research, which established that abiraterone blocked the synthesis of testosterone and reduced the size of androgen-dependent tumours. From 1996, a phase I trial conducted at the ICR and The Royal Marsden NHS Foundation Trust, established that abiraterone acetate, the prodrug form of abiraterone, resulted in sustained suppression of testosterone generation in patients with prostate cancer.

Following ICR-led phase II and III clinical trials, which demonstrated prolonged survival and improved quality of life for patients with certain types of aggressive prostate cancer, abiraterone (now under the trade name Zytiga) was granted approval by the FDA, EMA and NICE. In 2011–2012, abiraterone worldwide sales reached $2.755 billion and an estimated 25,000 patients per year are receiving treatment with abiraterone.

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