Effect of Cimetidine on the Single-Dose PK of IV- Administered MNTX

A Phase 1, Open-Label, Study of the Effect of Cimetidine, a Known Inhibitor of Active Renal Secretion, on the Single-Dose Pharmacokinetics of Intravenously-Administered Methylnaltrexone in Healthy Adults

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01366378

Enrollment

Registered

2011-06-06

Start date

2007-01-31

Completion date

2007-02-28

Last updated

2019-11-27

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy Adult Subjects

Brief summary

This open-label study assesses the single-dose pharmacokinetics of intravenously-administered MNTX in healthy adult male and female subjects in the absence of, and in the presence of, orally-administered cimetidine.

Interventions

DRUGmethylnaltrexone

Study design

Allocation

NON_RANDOMIZED

Intervention model

SINGLE_GROUP

Primary purpose

TREATMENT

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to 45 Years

Healthy volunteers

Yes

Inclusion criteria

1. Healthy males and females between the ages of 18 and 45 2. Subjects who are non-smokers 3. Subjects with body weights with range of 154-220 lbs.

Exclusion criteria

1. Females who are pregnant or lactating 2. Subjects with a history of any clinically significant disease or condition affecting a major organ system 3. Subjects with ECG abnormalities 4. Subjects who have tested positive for hepatitis B, hepatitis C or HIV 5. Subjects who have had a diagnosis of alcohol or substance dependence with the past 12 months 6. Subjects with positive urine results for drugs of abuse.

Design outcomes

Primary

Measure	Time frame	Description
Peak plasma concentration (Cmax) of MNTX prior to and following multi-dose cimetidine regimen	7 days	To assess the potential effects of cimetidine on the pharmacokinetics of MNTX

Secondary

Measure	Time frame	Description
Area under the plasma concentration (AUC) of MNTX prior to and following a multi-dose cimetidine regimen	7 days	To assess the potential effects of cimetidine on the pharmacokinetics of MNTX
Half-life of MNTX prior to and following a multi-dose cimetidine regimen	7 days	To assess the potential effects of cimetidine on the pharmacokinetics of MNTX
Clearance (both total and renal)of MNTX prior to and following a multi-dose cimetidine regimen	7 days	To assess the potential effects of cimetidine on the pharmacokinetics of MNTX
Volume of distribution of MNTX prior to and following a multi-dose cimetidine regimen	7 days	To assess the potential effects of cimetidine on the pharmacokinetics of MNTX
Number of subject with adverse events as measured before, during, and after administration of cimetidine	7 days	To assess the potential effects of cimetidine on safety, and tolerability of MNTX

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026