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CompletedNCT01367496Updated Nov 27, 2019

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

A Phase 1 interventional study of SC Methylnaltrexone (MNTX) and SC Methylnaltrexone (MNTX) in Healthy Subjects, sponsored by Bausch Health Americas, Inc.. Completed at 1 site in United States. Open to male participants aged 18 Years to 45 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2019-11-27.

Sponsored by Bausch Health Americas, Inc. · Phase 1, Interventional, and Treatment

Phase
Phase 1
Study type
Interventional
Enrollment
6
Allocation
Non-randomized
Ages
18 Years to 45 Years
Sex
Male
01

Study 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.

02

Conditions studied

  • Healthy Subjects
03

In context

Lead sponsor

Bausch Health Americas, Inc. is the lead sponsor of 209 studies on the registry; 9 are open to participants now.

Of its 23 completed or terminated interventional studies of FDA-regulated products, 16 (70%) have results posted.

Counted across the registry records on this site, refreshed daily.

04

Who can participate

Ages eligible
18 Years to 45 Years
Sexes eligible
Male
Accepts healthy volunteers
Yes

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

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.
05

Study design

Phase
Phase 1
Primary purpose
Treatment
Allocation
Non-randomized
Intervention model
Crossover assignment
Masking
None (open label)
Enrollment
6 participants (actual)

Study arms

  • Experimental
    Arm 1

    Drug: SC Methylnaltrexone (MNTX)

  • Experimental
    Arm 2

    Drug: SC Methylnaltrexone (MNTX)

  • Experimental
    Arm 3

    Drug: SC Methylnaltrexone (MNTX)

  • Experimental
    Arm 4

    Drug: IV Methylnaltrexone (MNTX)

Interventions

  • DrugSC Methylnaltrexone (MNTX)

    Dose 1

  • DrugSC Methylnaltrexone (MNTX)

    Dose 2

  • DrugSC Methylnaltrexone (MNTX)

    Dose 3

  • DrugIV Methylnaltrexone (MNTX)
06

What researchers measure

Primary outcomes

  1. Peak Plasma Concentration of MNTX

    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 frame: 32 days

Secondary outcomes

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

    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 frame: 32 days

  2. Clearance of MNTX

    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 frame: 32 days

  3. Half-live of MNTX

    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 frame: 32 days

  4. Volume of Distribution of MNTX

    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 frame: 32 days

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

    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 frame: 32 days

  6. Urinary Clearance of MNTX

    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 frame: 32 days

  7. Percentage of MNTX Excreted in Urine

    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 frame: 32 days

07

Study locations

1 site
  • Progenics Pharmaceuticals, Inc.
    Tarrytown, New York 10591, United States
08

Updates

Tracking since Sep 25, 2026
No changes since tracking began. The registry record was last updated on Nov 27, 2019, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
09

Registry details

Key details

Study ID
NCT01367496
Lead sponsor
Bausch Health Americas, Inc.
First posted
Jun 7, 2011
Start date
Jun 2002
Primary completion
Aug 2002
Completion
Aug 2002
Last update
Nov 27, 2019

Study contacts

Tage Ramakrishna, MD
study director · Progenics Pharmaceuticals, Inc.

Oversight

Data monitoring committee
No
View the source record on ClinicalTrials.gov ↗

Not currently enrolling

This study is completed, as verified in Nov 2019. You cannot join it, but the record below documents what was studied.

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