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OpenTrials
Completed

NCT Number: NCT01367496

Pharmacokinetics and Bioavailability of Single Subcutaneous Doses of Methylnaltrexone Versus Intravenous Dose

This is an open-label, Phase I study. Study treatments will entail a four-way crossover among three single, ascending, subcutaneous doses and one intravenous dose of MNTX in six healthy normal male volunteers. Blood samples will be obtained to determine plasma pharmacokinetics, dose proportionality for subcutaneous doses, and absolute bioavailability versus an intravenous dose.

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Key information

Conditions

Healthy Subjects

Age range

18 year–45 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

Primary location

Progenics Pharmaceuticals, Inc.

Tarrytown, New York, 10591, United States

Who can participate

Healthy volunteers accepted: Yes

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

Inclusion criteria

  • Subject weight between 60 and 80 kg
  • Subject a non-smoker
  • Subject in good physical health, based on history, physical exam, appropriate laboratory and diagnostics tests at screening with no evidence of clinically significant chronic medical condition.

Exclusion criteria

  • Subject with known hypersensitivity to methylnaltrexone, naltrexon or other opioids
  • Subject consuming any prescription medication within the past two weeks, over-the-counter (OTC) products within seven days, any experimental medication within 30 days prior to study screening, or of any drug with a half-life longer then three days within 10 half-lives (>30 days) of screening
  • Subject consuming barbiturates or other inducers or inhibitors of CYP450 within 3 months of screening
  • Subject with history or evidence of cardiovascular, gastrointestinal, hepatic, neurological, pulmonary, and renal or other significant chronic illness.

Treatment and study plan

SC Methylnaltrexone (MNTX)

Drug

Dose 1

IV Methylnaltrexone (MNTX)

Drug

Primary outcomes

  1. Peak Plasma Concentration of MNTX

    Time frame: 32 days

    The objective of this study is to determine the plasma pharmacokinetic of single, ascending, subcutaneous doses and a single intravenous dose of methylnaltrexone (MNTX) in normal healthy male subjects.

Secondary outcomes

  1. Time to Maximum Plasma Concentration (Tmax) of MNTX

    Time frame: 32 days

    The objective of this study is to determine the plasma pharmacokinetic of single, ascending, subcutaneous doses and a single intravenous dose of methylnaltrexone (MNTX) in normal healthy male subjects.

  2. Clearance of MNTX

    Time frame: 32 days

    The objective of this study is to determine the plasma pharmacokinetic of single, ascending, subcutaneous doses and a single intravenous dose of methylnaltrexone (MNTX) in normal healthy male subjects.

  3. Half-live of MNTX

    Time frame: 32 days

    The objective of this study is to determine the plasma pharmacokinetic of single, ascending, subcutaneous doses and a single intravenous dose of methylnaltrexone (MNTX) in normal healthy male subjects.

  4. Volume of Distribution of MNTX

    Time frame: 32 days

    The objective of this study is to determine the plasma pharmacokinetic of single, ascending, subcutaneous doses and a single intravenous dose of methylnaltrexone (MNTX) in normal healthy male subjects.

  5. Area Under the Plasma Concentration versus Time Curve (AUC) of MNTX

    Time frame: 32 days

    The objective of this study is to determine the plasma pharmacokinetic of single, ascending, subcutaneous doses and a single intravenous dose of methylnaltrexone (MNTX) in normal healthy male subjects.

  6. Urinary Clearance of MNTX

    Time frame: 32 days

    The objective of this study is to determine the plasma pharmacokinetic of single, ascending, subcutaneous doses and a single intravenous dose of methylnaltrexone (MNTX) in normal healthy male subjects.

  7. Percentage of MNTX Excreted in Urine

    Time frame: 32 days

    The objective of this study is to determine the plasma pharmacokinetic of single, ascending, subcutaneous doses and a single intravenous dose of methylnaltrexone (MNTX) in normal healthy male subjects.

Sponsors and collaborators

Lead sponsor

Bausch Health Americas, Inc.

Industry

Registry information

Official study title

An Open-Label, Phase I Study of the Pharmacokinetics and Bioavailability of Single, Ascending Subcutaneous Doses of Methylnaltrexone Versus Intravenous Dose in Normal, Healthy Male Volunteers

Important dates

Study start
2002
Primary completion
2002
Study completion
2002
First posted
Jun 7, 2011
Registry last updated
Nov 27, 2019

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.

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