Relative Bioavailability Study of Enzalutamide in Prostate Cancer Patients

Inclusion Criteria:

- Histologically confirmed prostate cancer (all stages) for whom androgen deprivation
therapy is indicated (except when indicated in a neoadjuvant/adjuvant setting).
Subjects may be on ongoing androgen deprivation therapy with a gonadotropin releasing
hormone (GnRH) analogue or orchiectomy (i.e., medical or surgical castration) at
study entry.

- Progressive disease by Prostate-specific antigen (PSA) or imaging. Disease
progression for study entry is defined as one or more of the following 3 criteria:

- PSA progression defined by a minimum of 2 rising PSA levels with an interval of
≥1 week between each determination. The PSA value during the pre-investigational
period should be ≥2 μg/L (2 ng/mL);

- Soft tissue disease progression defined by the Response Evaluation Criteria in
Solid Tumors, version 1.1 (RECIST 1.1) for soft tissue disease

- Bone disease progression defined by two or more new lesions on bone scan

Exclusion Criteria:

- Treatment with chemotherapy within 4 weeks prior to enrollment (Day 1 visit) or plans
to initiate treatment with chemotherapy during the study.

- Prior use of ketoconazole for the treatment of prostate cancer.

- History of seizure or any condition that may predispose to seizure. Also, history of
loss of consciousness, or transient ischemic attack within 12 months prior to
enrollment (Day 1 visit).

- Patients who previously received treatment with Enzalutamide.

- Concomitant use of drugs that are potent inducers and/or inhibitors of CYP3A4 and
CYP2C8.

- Confirmed CYP2C8 poor metabolizer status based on genotyping analysis.