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

Healthy Subjects Clinical Trial

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

Clinical Trial Details — Status: Completed

Administrative data

• NCT number: NCT01367496
• Other study ID #: MNTX 103
• Status: Completed
• Phase: Phase 1
• Start date: June 2002
• Est. completion date: August 2002

Study information

• Verified date: November 2019
• Source: Bausch Health Americas, Inc.
• Contact: n/a
• Is FDA regulated: No
• Study type: Interventional

Clinical Trial 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.

Recruitment information / eligibility

• Status: Completed
• Enrollment: 6
• Est. completion date: August 2002
• Est. primary completion date: August 2002
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: Male
• Age group: 18 Years to 45 Years

Eligibility

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.

Related Conditions & MeSH terms

• Healthy Subjects

Intervention

Drug:
• SC Methylnaltrexone (MNTX)
Dose 1
• SC Methylnaltrexone (MNTX)
Dose 2
• SC Methylnaltrexone (MNTX)
Dose 3
• IV Methylnaltrexone (MNTX)

Locations

Country	Name	City	State
United States	Progenics Pharmaceuticals, Inc.	Tarrytown	New York

Sponsors (1)

Lead Sponsor	Collaborator
Bausch Health Americas, Inc.

Country where clinical trial is conducted

United States, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	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.	32 days
Secondary	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.	32 days
Secondary	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.	32 days
Secondary	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.	32 days
Secondary	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.	32 days
Secondary	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.	32 days
Secondary	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.	32 days
Secondary	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.	32 days