MedPath

Methylnaltrexone

Generic Name
Methylnaltrexone
Brand Names
Relistor
Drug Type
Small Molecule
Chemical Formula
C21H26NO4
CAS Number
916055-93-1
Unique Ingredient Identifier
0RK7M7IABE
Background

Methylnaltrexone is a pheriphally-acting μ-opioid antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation without producing analgesic effects or withdrawal symptoms. It is also a weak CYP2D6 inhibitor. FDA approved in 2008.

Indication

Treatment of opioids induced constipation in palliative patients that are inadequately responding to laxative therapy.

Associated Conditions
Opioid Induced Constipation (OIC)

Methylnaltrexone as a Method to Improve Ticagrelor Uptake in Morphine Treated STEMI Patients

Phase 4
Completed
Conditions
STEMI
Morphine
Ticagrelor
Methylnaltrexone
Interventions
First Posted Date
2016-10-24
Last Posted Date
2018-04-09
Lead Sponsor
Karolinska University Hospital
Target Recruit Count
82
Registration Number
NCT02942550
Locations
🇸🇪

Södersjukhuset (Stockholm South General Hospital), Stockholm, Sweden

🇸🇪

Karolinska University Hospital, Stockholm, Sweden

Study of Methylnaltrexone in Opioid-Induced Constipation Patients

Phase 2
Conditions
Opioid-induced Constipation
Interventions
First Posted Date
2015-10-14
Last Posted Date
2015-10-14
Lead Sponsor
Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
Target Recruit Count
198
Registration Number
NCT02574819
Locations
🇨🇳

Henan Provincial Cancer Hospital, Zhengzhou, Henan, China

🇨🇳

The Affiliated Hospital of Xuzhou Medical College, Xuzhou, Jiangsu, China

🇨🇳

Xin Hua Hospital affiliated to Shanghai Jiao Tong University School of Medicine Chongming Branch, Shanghai, Shanghai, China

and more 9 locations

Effect of Methylnaltrexone on the PK/PD Profiles of Ticagrelor in Patients Treated With Morphine

Phase 4
Completed
Conditions
Coronary Artery Disease
Interventions
First Posted Date
2015-03-31
Last Posted Date
2017-05-30
Lead Sponsor
University of Florida
Target Recruit Count
30
Registration Number
NCT02403830
Locations
🇺🇸

University of Florida, Jacksonville, Florida, United States

Methylnaltrexone for Opioid Induced Constipation

Terminated
Conditions
Constipation
Interventions
First Posted Date
2013-10-07
Last Posted Date
2019-08-05
Lead Sponsor
Amsterdam UMC, location VUmc
Target Recruit Count
7
Registration Number
NCT01955213
Locations
🇳🇱

VU University Medical Center, Amsterdam, Netherlands

🇳🇱

Hospice Demeter, De Bilt, Netherlands

🇳🇱

Medical Center Alkmaar, Alkmaar, Netherlands

and more 3 locations

Methylnaltrexone Pharmacokinetics in Neurointensive Care Patients

Phase 1
Completed
Conditions
Opioid Use, Unspecified With Other Opioid-induced Disorder
Interventions
First Posted Date
2013-06-28
Last Posted Date
2016-10-26
Lead Sponsor
University of Zurich
Target Recruit Count
9
Registration Number
NCT01889290
Locations
🇨🇭

Neurointensive Care Unit, Zurich, Switzerland

Methylnaltrexone Use for Opioid-induced Postoperative Constipation

Phase 4
Completed
Conditions
Constipation
Interventions
Drug: Senna, docusate sodium, bisacodyl, magnesium hydroxide, Miralax
First Posted Date
2013-01-23
Last Posted Date
2015-05-19
Lead Sponsor
Shriners Hospitals for Children
Target Recruit Count
60
Registration Number
NCT01773096
Locations
🇺🇸

Shriners Hospitals for Children- Spokane, Spokane, Washington, United States

Effects of Methylnaltrexone in Comparison to Naloxone on Loperamide-induced Delay of the Oro-cecal, Whole-gut and Colon Transit Time.

Phase 1
Completed
Conditions
Intestinal Obstruction
Interventions
First Posted Date
2012-05-11
Last Posted Date
2012-05-11
Lead Sponsor
University Medicine Greifswald
Target Recruit Count
16
Registration Number
NCT01596764
Locations
🇩🇪

Department of Clinical Pharmacology, Ernst-Moritz-Arndt-University Greifswald, Greifswald, Mecklenburg-Vorpommern, Germany

Effects of 500 mg Immediate Release and Extended Release Methylnaltrexone on Loperamide-induced Delay of the Oro-cecal and Whole-gut Transit Time in Healthy Subjects

First Posted Date
2012-05-11
Last Posted Date
2016-10-26
Lead Sponsor
University Medicine Greifswald
Target Recruit Count
15
Registration Number
NCT01596777
Locations
🇩🇪

Department of Clinical Pharmacology, Ernst-Moritz-Arndt-University Greifswald, Greifswald, Mecklenburg-Vorpommern, Germany

Compassionate Use Study of Methylnaltrexone

Not Applicable
Completed
Conditions
Opioid-induced Constipation
Interventions
First Posted Date
2011-06-08
Last Posted Date
2019-09-04
Lead Sponsor
Bausch Health Americas, Inc.
Target Recruit Count
26
Registration Number
NCT01368562
Locations
🇺🇸

Progenics Pharmaceuticals, Inc., Tarrytown, New York, United States

Pharmacokinetics, Safety, and Tolerability of Methylnaltrexone (MNTX) in Subjects With Impaired Renal Function

Phase 1
Completed
Conditions
Renal Impairment
Interventions
First Posted Date
2011-06-07
Last Posted Date
2019-11-27
Lead Sponsor
Bausch Health Americas, Inc.
Target Recruit Count
32
Registration Number
NCT01367509
Locations
🇺🇸

Progenics Pharmaceuticals, Inc., Tarrytown, New York, United States

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