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

This study has been completed.
Sponsor:
Information provided by:
Salix Pharmaceuticals
ClinicalTrials.gov Identifier:
NCT01367496
First received: May 27, 2011
Last updated: July 17, 2011
Last verified: July 2011
  Purpose

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.


Condition Intervention Phase
Healthy Subjects
Drug: SC Methylnaltrexone (MNTX)
Drug: IV Methylnaltrexone (MNTX)
Phase 1

Study Type: Interventional
Study Design: Allocation: Non-Randomized
Endpoint Classification: Pharmacokinetics Study
Intervention Model: Crossover Assignment
Masking: Open Label
Primary Purpose: Treatment
Official 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

Resource links provided by NLM:


Further study details as provided by Salix Pharmaceuticals:

Primary Outcome Measures:
  • Peak Plasma Concentration of MNTX [ Time Frame: 32 days ] [ Designated as safety issue: No ]
    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:
  • Time to Maximum Plasma Concentration (Tmax) of MNTX [ Time Frame: 32 days ] [ Designated as safety issue: No ]
    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 [ Time Frame: 32 days ] [ Designated as safety issue: No ]
    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.

  • Half-live of MNTX [ Time Frame: 32 days ] [ Designated as safety issue: No ]
    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 [ Time Frame: 32 days ] [ Designated as safety issue: No ]
    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 [ Time Frame: 32 days ] [ Designated as safety issue: No ]
    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 [ Time Frame: 32 days ] [ Designated as safety issue: No ]
    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 [ Time Frame: 32 days ] [ Designated as safety issue: No ]
    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.


Enrollment: 6
Study Start Date: June 2002
Study Completion Date: August 2002
Primary Completion Date: August 2002 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: Arm 1 Drug: SC Methylnaltrexone (MNTX)
Dose 1
Experimental: Arm 2 Drug: SC Methylnaltrexone (MNTX)
Dose 2
Experimental: Arm 3 Drug: SC Methylnaltrexone (MNTX)
Dose 3
Experimental: Arm 4 Drug: IV Methylnaltrexone (MNTX)

  Eligibility

Ages Eligible for Study:   18 Years to 45 Years
Genders Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  1. Subject weight between 60 and 80 kg
  2. Subject a non-smoker
  3. 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:

  1. Subject with known hypersensitivity to methylnaltrexone, naltrexon or other opioids
  2. 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
  3. Subject consuming barbiturates or other inducers or inhibitors of CYP450 within 3 months of screening
  4. Subject with history or evidence of cardiovascular, gastrointestinal, hepatic, neurological, pulmonary, and renal or other significant chronic illness.
  Contacts and Locations
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

Please refer to this study by its ClinicalTrials.gov identifier: NCT01367496

Locations
United States, New York
Progenics Pharmaceuticals, Inc.
Tarrytown, New York, United States, 10591
Sponsors and Collaborators
Salix Pharmaceuticals
Investigators
Study Director: Tage Ramakrishna, MD Progenics Pharmaceuticals, Inc.
  More Information

No publications provided

Responsible Party: Tage Ramakrishna, M.D., Progenics Pharmaceuticals, Inc.
ClinicalTrials.gov Identifier: NCT01367496     History of Changes
Other Study ID Numbers: MNTX 103
Study First Received: May 27, 2011
Last Updated: July 17, 2011
Health Authority: United States: Food and Drug Administration

Additional relevant MeSH terms:
Methylnaltrexone
Naltrexone
Central Nervous System Agents
Narcotic Antagonists
Peripheral Nervous System Agents
Pharmacologic Actions
Physiological Effects of Drugs
Sensory System Agents
Therapeutic Uses

ClinicalTrials.gov processed this record on November 27, 2014