Skip to main content
OpenTrials
Completed

NCT Number: NCT01911715

A Study to Explore the Routes of Elimination of MDV3100

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

Completed

Looking for future studies?

Notify Me

Key information

Age range

18 year–55 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

Primary location

PRA International

Zuidlaren, 9471GP, Netherlands

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

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.

Treatment and study plan

MDV3100

Drug

Oral

Other names: Xtandi, enzalutamide

Primary outcomes

  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 outcomes

  1. Safety as assessed by recording adverse events, laboratory assessments, vital signs and electrocardiograms (ECGs)

    Time frame: Day 1 through Day 78

Sponsors and collaborators

Lead sponsor

Astellas Pharma Europe B.V.

Industry

Collaborators

  • Medivation, Inc.

Registry information

Official study 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

Important dates

Study start
2011
Primary completion
2011
Study completion
2011
First posted
Jul 30, 2013
Registry last updated
Jul 30, 2013

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

Published trials that share one or more normalized conditions with this study.