Orteronel

Orteronel (developmental code names TAK-700) is an experimental drug that was under investigation for the treatment of prostate cancer. It is an enzyme inhibitor, specifically targeting the 17,20-lyase enzyme, a critical enzyme in the production of steroid hormones.

Mechanism of Action

Orteronel works by inhibiting the enzyme 17,20-lyase, which is involved in the biosynthesis of steroidal hormones such as testosterone and estrogen. By inhibiting this enzyme, orteronel reduces the production of testosterone, which is known to fuel the growth of prostate cancer cells. This mechanism of action places orteronel in the class of drugs known as CYP17 inhibitors, which are used in the treatment of prostate cancer that has become resistant to traditional hormone therapy.

Clinical Trials

Orteronel has been evaluated in several clinical trials for its effectiveness and safety in treating patients with metastatic castration-resistant prostate cancer (mCRPC). Early phase trials showed promise, leading to larger, phase III trials to further assess its efficacy. However, despite initial optimism, development was eventually discontinued after phase III trials did not demonstrate a significant improvement in overall survival rates for patients treated with orteronel compared to standard therapies.

Adverse Effects

Like other CYP17 inhibitors, orteronel can cause a range of side effects due to its mechanism of action. Common adverse effects reported in clinical trials include fatigue, hypertension, and liver enzyme abnormalities. As with any cancer therapy, the balance between efficacy and tolerability is crucial in the management of treatment.

Current Status

As of the last update, development of orteronel for the treatment of prostate cancer has been discontinued. The decision was based on the results of phase III clinical trials, which did not meet the primary endpoint of significantly improving overall survival in patients with mCRPC. Despite this, research into CYP17 inhibitors continues, with the hope of finding more effective treatments for hormone-driven cancers.

See Also

• Prostate cancer
• CYP17 inhibitor
• Hormone therapy for prostate cancer

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