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Relative Bioavailability Study of Enzalutamide in Prostate Cancer Patients

Phase 1
Completed
Conditions
Pharmacokinetics of Enzalutamide
Prostate Cancer
Interventions
Registration Number
NCT01902251
Lead Sponsor
Astellas Pharma Europe B.V.
Brief Summary

A multiple dose relative bioavailability study in patients with prostate cancer comparing a capsule and a tablet formulation of enzalutamide.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
27
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.
  • 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.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Enzalutamide capsuleEnzalutamide capsuleMultiple once daily oral doses of enzalutamide formulated as liquid-filled soft gelatin capsule for approximately 8 weeks
Enzalutamide tabletEnzalutamide tabletMultiple once daily oral doses of enzalutamide formulated as a tablet for approximately 8 weeks
Primary Outcome Measures
NameTimeMethod
Pharmacokinetic profile of Enzalutamide under fasted conditions measured by Cmax (Maximum concentration)Day1 through Day 56 (12 samples)

Day 56 (fasted) Cmax under steady state conditions of enzalutamide

Pharmacokinetic profile of Enzalutamide under fasted conditions measured by AUC0-24h (Area under the concentration-time curve 0-24h)Day1 through Day 56 (12 samples)

Day 56 (fasted) AUC0-24h under steady state conditions of enzalutamide

Secondary Outcome Measures
NameTimeMethod
Pharmacokinetic profile of Enzalutamide under fasted and fed conditionsDay 1, 8, 29, 55, 56 and 57 (38 samples)

Measured by: Cmax, tmax (Time to attain Cmax), AUC0-24h, Ctrough (Trough concentration), PTR (Peak-trough ratio), CLss/F (Apparent clearance at steady state)

Pharmacokinetic profile of MDPC0001 alone, MDPC0002 alone and sum of Enzalutamide plus MDPC0002Day 8, 29, 55, 56 and 57 (26 samples)

Measured by: Ctrough, Cmax, tmax, AUC0-24h, Ctrough (24h after dosing), PTR

Evaluation of the safety and tolerability of two oral formulations of Enzalutamide assessed through vital signs, adverse events, electrocardiogram and clinical laboratory assessmentsDay 1 through Day 58

Trial Locations

Locations (4)

University of Pittsburgh Medical Center

🇺🇸

Pittsburgh, Pennsylvania, United States

South Texas Accelerated Research Therapeutics

🇺🇸

San Antonio, Texas, United States

University of Colorado - Anschutz Medical Campus

🇺🇸

Denver, Colorado, United States

University of Chicago Medical Center

🇺🇸

Chicago, Illinois, United States

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