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Enzalutamide: A Review of Its Use in Metastatic, Castration-Resistant Prostate Cancer

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Abstract

Enzalutamide (MDV3100, XTANDI®) is an androgen receptor inhibitor that is indicated for the treatment of metastatic, castration-resistant, prostate cancer (mCRPC) that has progressed despite treatment with docetaxel. This article reviews the pharmacology, efficacy and tolerability of enzalutamide relevant to this indication. In a randomized, double-blind, placebo-controlled, multinational, phase III trial in patients with mCRPC progressing after docetaxel therapy, enzalutamide significantly prolonged overall survival (OS), delayed prostate specific antigen progression and prolonged radiographic progression-free survival and time to the first skeletal event. The median OS was 18.4 months in the enzalutamide group and 13.6 months in the placebo group, which represents a 37 % reduction in the mortality risk in the enzalutamide group. Enzalutamide was also associated with significant benefits in health-related quality of life and in pain palliation. Enzalutamide was generally as well tolerated as placebo during the trial, with most adverse events at a mild or moderate level of severity. Enzalutamide carries a small increased risk of seizures that appears to be dose-dependent. Enzalutamide is an efficacious and well tolerated treatment for this severe, rapidly progressive disease.

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Disclosure

The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on this article. Changes resulting from comments received were made by the author on the basis of scientific and editorial merit.

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    Mark Sanford

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Correspondence to Mark Sanford.

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The manuscript was reviewed by: N. Agarwal, Department of Medicine, University of Utah Huntsman Cancer Institute, Salt Lake City, UT, USA; U. Emmenegger, Medical Oncology, Sunnybrook Odette Cancer Centre, Toronto, Canada; M. Namiki, Department of Integrative Cancer Therapy and Urology, Kanazawa University Graduate School of Medical Science, Kanazawa, Japan; J.B. Nelson, Department of Urology, University of Pittsburgh School of Medicine, Pittsburgh, PA, USA.

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Sanford, M. Enzalutamide: A Review of Its Use in Metastatic, Castration-Resistant Prostate Cancer. Drugs 73, 1723–1732 (2013). https://doi.org/10.1007/s40265-013-0129-9

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