Pharmacokinetics and Bioavailability of Single Subcutaneous Doses of Methylnaltrexone Versus Intravenous Dose
- Conditions
- Healthy Subjects
- Interventions
- Registration Number
- NCT01367496
- Lead Sponsor
- Bausch Health Americas, Inc.
- Brief Summary
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.
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- Male
- Target Recruitment
- 6
- 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.
- 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.
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- CROSSOVER
- Arm && Interventions
Group Intervention Description Arm 4 IV Methylnaltrexone (MNTX) - Arm 3 SC Methylnaltrexone (MNTX) - Arm 1 SC Methylnaltrexone (MNTX) - Arm 2 SC Methylnaltrexone (MNTX) -
- Primary Outcome Measures
Name Time Method Peak Plasma Concentration of MNTX 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 Outcome Measures
Name Time Method Half-live of MNTX 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.
Volume of Distribution of MNTX 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.
Time to Maximum Plasma Concentration (Tmax) of MNTX 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.
Clearance of MNTX 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.
Area Under the Plasma Concentration versus Time Curve (AUC) of MNTX 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.
Urinary Clearance of MNTX 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.
Percentage of MNTX Excreted in Urine 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.
Trial Locations
- Locations (1)
Progenics Pharmaceuticals, Inc.
🇺🇸Tarrytown, New York, United States