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Abiraterone Acetate (CB7630)
Abiraterone acetate (CB7630) is an orally administered inhibitor of the steroidal enzyme 17α-hydroxylase/C17,20 lyase, a cytochrome p450 complex that is involved in testosterone production (see Figure below). Scientists believe that testosterone levels in the testes and adrenals stimulate the growth of prostate cancer cells. In preclinical and clinical studies, CB7630 has demonstrated the ability to selectively inhibit the target enzyme, resulting in inhibition of testosterone production in both the adrenals and the testes.
Potential applications of CB7630 include (1) serving as second-line hormonal therapy for patients with hormone refractory prostate cancer who have failed first-line hormone therapy; (2) serving as first-line hormonal therapy for patients with advanced prostate cancer who have not yet undergone traditional LHRH agonist and/or anti-androgen therapy; and (3) serving as second-line chemotherapy for patients with advanced prostate cancer who have failed treatment with docetaxel-based chemotherapy.
CB7630 is currently being tested in Phase I, Phase II and Phase III trials in castration resistant prostate cancer patients at numerous locations in North America, Europe, and Australia. Based on interim clinical trial results to date, patients have experienced confirmed declines in prostate specific antigen (PSA) levels of up to 90+%, partial radiological responses (as measured by the RECIST criteria), regressing bone disease, improvement in pain and reduced opioid use. The compound has been well tolerated at doses as high as 2000 mg/day with minimal toxicity and no dose limiting toxicity has been observed. Further information on clinical trials is available at http://www.clinicaltrials.gov/ct2/results?term=abiraterone.
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