N-Desmethylenzalutamide Explained

N-Desmethylenzalutamide is a nonsteroidal antiandrogen (NSAA) and the major metabolite of enzalutamide, an NSAA which is used as a hormonal antineoplastic agent in the treatment of metastatic prostate cancer.[1] [2] [3] It has similar activity to that of enzalutamide and, with enzalutamide therapy, circulates at similar concentrations to those of enzalutamide at steady state. N-Desmethylenzalutamide is formed from enzalutamide in the liver by the cytochrome P450 enzymes CYP2C8 and CYP3A4. It has a longer terminal half-life than enzalutamide (7.8 days versus 5.8 days).

Notes and References

  1. Keating GM . Enzalutamide: a review of its use in chemotherapy-naïve metastatic castration-resistant prostate cancer . Drugs Aging . 32 . 3 . 243–9 . 2015 . 25711765 . 10.1007/s40266-015-0248-y . 29563345 .
  2. El-Amm J, Patel N, Freeman A, Aragon-Ching JB . Metastatic castration-resistant prostate cancer: critical review of enzalutamide . Clin Med Insights Oncol . 7 . 235–45 . 2013 . 24179414 . 3813614 . 10.4137/CMO.S11670 .
  3. Benoist GE, Hendriks RJ, Mulders PF, Gerritsen WR, Somford DM, Schalken JA, van Oort IM, Burger DM, van Erp NP . Pharmacokinetic Aspects of the Two Novel Oral Drugs Used for Metastatic Castration-Resistant Prostate Cancer: Abiraterone Acetate and Enzalutamide . Clin Pharmacokinet . 55 . 11 . 1369–1380 . 2016 . 27106175 . 5069300 . 10.1007/s40262-016-0403-6 .

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