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A Study to Explore the Routes of Elimination of MDV3100

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ClinicalTrials.gov Identifier: NCT01911715
Recruitment Status : Completed
First Posted : July 30, 2013
Last Update Posted : July 30, 2013
Sponsor:
Collaborator:
Medivation, Inc.
Information provided by (Responsible Party):
Astellas Pharma Inc ( Astellas Pharma Europe B.V. )

Brief Summary:
A study to investigate the excretion routes of radio-labelled MDV3100.

Condition or disease Intervention/treatment Phase
Healthy Subjects Pharmacokinetics of MDV3100 Drug: MDV3100 Phase 1

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Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 6 participants
Allocation: N/A
Intervention Model: Single Group Assignment
Masking: None (Open Label)
Primary Purpose: Basic Science
Official Title: A Phase I Open-label Study to Investigate the Mass Balance and Biotransformation of a Single Oral 160 mg (100 µCi) Dose of 14C-MDV3100 (ASP9785) in Healthy Male Subjects
Study Start Date : April 2011
Actual Primary Completion Date : July 2011
Actual Study Completion Date : July 2011

Resource links provided by the National Library of Medicine


Arm Intervention/treatment
Experimental: Single Oral MDV3100 dose Drug: MDV3100
Oral
Other Names:
  • Xtandi
  • enzalutamide




Primary Outcome Measures :
  1. Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Maximum concentration (Cmax) [ Time Frame: Day 1 through Day 78 (21 times) ]
  2. Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Time to attain Cmax (tmax) [ Time Frame: Day 1 through Day 78 (21 times) ]
    Time to attain Cmax (tmax)

  3. Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Time to reach quantifiable concentrations (tlag) [ Time Frame: Day 1 through Day 78 (21 times) ]
  4. Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by AUC from the time of dosing to the last measurable concentration (AUC0-t) [ Time Frame: Day 1 through Day 78 (21 times) ]
  5. Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by AUC extrapolated to infinity (AUC0-inf) [ Time Frame: Day 1 through Day 78 (21 times) ]
  6. Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Terminal Disposition Rate Constant (λz) [ Time Frame: Day 1 through Day 78 (21 times) ]
  7. Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Apparent terminal elimination half life (t1/2) [ Time Frame: Day 1 through Day 78 (21 times) ]
  8. Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Apparent total body clearance after extra vascular dosing (CL/F) [ Time Frame: Day 1 through Day 78 (21 times) ]
  9. Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Apparent volume of distribution during the terminal phase after extra vascular dosing (Vz/F) [ Time Frame: Day 1 through Day 78 (21 times) ]
  10. Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by blood-to-plasma ratio (Ratio Cb/p) [ Time Frame: Day 1 through Day 78 (21 times) ]
  11. Assessment of 14C recovery in urine [ Time Frame: Day 1 through Day 78 (17 times) ]
  12. Assessment of 14C recovery in feces [ Time Frame: Day 1 through Day 78 (16 times) ]
  13. Assessment of total 14C recovery (urine and feces combined) within 24 hours [ Time Frame: Day 1 through Day 78 (17 times for urine and 16 times for feces) ]
  14. Assessment of total 14C recovery (urine and feces combined) after Time of last quantifiable concentration (tlast) [ Time Frame: Day 1 through Day 78 (17 times for urine and 16 times for feces) ]
  15. Assessment of Pharmacokinetic profile of MDV3100 and metabolites in plasma [ Time Frame: Day 1 through Day 78 (21 times) ]

    PK of MDV3100, MDPC0001, and MDPC0002 in plasma based on validated LC-MS/MS methods:

    • In plasma: Cmax, tmax, tlag, AUC0-t, AUC0-inf, λz, t1/2, CL/F (parent only), and Vz/F (parent only)

    The ratios of AUCMDV3100/AUC14C , AUCMDPC0001/AUCMDV3100 and AUCMDPC0001/AUC14C (and the same for MDPC0002) will be calculated


  16. Assessment of Pharmacokinetic profile of MDV3100 and metabolites in urine [ Time Frame: Day 1 through Day 78 (17 times) ]

    PK of MDV3100, MDPC0001, and MDPC0002 in urine based on validated LC-MS/MS methods:

    • In urine: Cumulative amount excreted in urine from time zero to the last measurable concentration after dosing (Ae0-t), Renal clearance (CLR), Percent of dose excreted in urine from time zero to the last measurable concentration after dosing (Ae0-t%), Cumulative amount excreted in urine from time zero extrapolated to infinity (Ae0-inf), Percent of dose excreted in urine from time zero extrapolated to infinity (Ae0-inf%)

    The ratios of AUCMDV3100/AUC14C , AUCMDPC0001/AUCMDV3100 and AUCMDPC0001/AUC14C (and the same for MDPC0002) will be calculated


  17. Metabolic Profile: Profiling of possible metabolites of MDV3100 in plasma, urine, and feces [ Time Frame: Day 1 through Day 78 (14 times) ]
    Identification and possible quantification of metabolites in plasma, and if applicable, in urine and feces


Secondary Outcome Measures :
  1. Safety as assessed by recording adverse events, laboratory assessments, vital signs and electrocardiograms (ECGs) [ Time Frame: Day 1 through Day 78 ]


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Ages Eligible for Study:   18 Years to 55 Years   (Adult)
Sexes Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  • Body Mass Index within 18.5 to 30.0kg/m2
  • Regular defecation pattern (minimum once per 2 days).
  • Subject must be non-fertile, i.e., surgically sterilized or must practice an adequate contraceptive method to prevent pregnancies as defined in the protocol.

Exclusion Criteria:

  • Known or suspected hypersensitivity to MDV3100, or any components of the formulation used.
  • Any of the liver function tests above the upper limit of normal. A retest to confirm the result may be performed once.
  • Any clinically significant history of asthma, eczema, any other allergic condition or previous severe hypersensitivity to any drug (excluding non-active hay fever).
  • Abnormal pulse and/or blood pressure measurements at the pre-study visit as follows: Pulse <40 or >90 bpm; mean systolic blood pressure >140 mmHg ; mean diastolic blood pressure >90 mmHg (blood pressure measurements taken in triplicate after subject has been resting in supine position for 5 min; pulse will be measured automatically).
  • A QTc interval of > 430 ms after repeated measurements (consistently after duplicate measurements), a history of unexplained syncope, cardiac arrest, unexplained cardiac arrhythmias or torsades de pointes, structural heart disease, or a family history of Long QT Syndrome (LQTS).
  • Use of any prescribed or OTC (over-the-counter) drugs (including vitamins, natural and herbal remedies, e.g. St. John's wort) in the 2 weeks prior to admission to the Clinical Unit, except for occasional use of paracetamol (up to 3 g/day).
  • Regular use of any inducer of metabolism (e.g., barbiturates, rifampin) in the 3 months prior to admission to the Clinical Unit.
  • Positive serology test for HBsAg, anti HAV (IgM), anti-HCV or anti-HIV 1+2.
  • Exposure to radiation for diagnostic reasons (except dental X-rays and plain X-rays of thorax and bony skeleton (excluding spinal column)), during work or during participation in a clinical study in the previous year.

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT01911715


Locations
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Netherlands
PRA International
Zuidlaren, Netherlands, 9471GP
Sponsors and Collaborators
Astellas Pharma Europe B.V.
Medivation, Inc.
Investigators
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Study Chair: Operation Senior Research Manager Astellas Pharma Europe B.V.
Publications automatically indexed to this study by ClinicalTrials.gov Identifier (NCT Number):
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Responsible Party: Astellas Pharma Europe B.V.
ClinicalTrials.gov Identifier: NCT01911715    
Other Study ID Numbers: 9785-CL-0001
2011-000089-37 ( EudraCT Number )
First Posted: July 30, 2013    Key Record Dates
Last Update Posted: July 30, 2013
Last Verified: July 2013
Keywords provided by Astellas Pharma Inc ( Astellas Pharma Europe B.V. ):
Phase 1
Mass Balance
MDV3100
Xtandi
Enzalutamide
Metabolism
Excretion