Drugs / Methylnaltrexone
Methylnaltrexone
also known as
MNTX · MOA-728 · Methylnaltrexone bromide · N-methylnaltrexone bromide · N-methylnaltrexone · Relistor · Bromure de methylnaltrexone · Bromuro de metilnaltrexona · +7 more
Other / unclassified targets OPRM1 via inhibition
Regulatory milestones approvals, filings & regulatory actions · 3 recorded
| Milestone | Jurisdiction | Brand | Indication | Date | Sentence it was read from |
|---|---|---|---|---|---|
| Label expansion | US (FDA) | RELISTOR | — | 2014-09-29 | fda.gov ↗ |
| Approved | EU (EMA) | Relistor | — | 2008-07-01 | europa.eu ↗ |
| Approved | US (FDA) | RELISTOR | — | 2008-04-24 | fda.gov ↗ |
Trials 55
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 122 trials | ||||||
| Phase 1 | NCT01889290 | Feb 2014 → Jun 2016 | opioid abuse | University of Zurich | Completed | No outcome recorded |
| Phase 1 | NCT01366326 | Jul → Aug 2010 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT00427258 | Jan 2010 → ? | — | Bausch Health Americas, Inc. | Withdrawn | No outcome recorded |
| Phase 1 | NCT00505583 | Jul → Dec 2007 | — | Bausch Health Americas, Inc. | Withdrawn | No outcome recorded |
| Phase 1 | NCT00464802 | Apr → Jun 2007 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT00444158 | Mar → Jul 2007 | constipation disorder | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT00434395 | Mar → Oct 2007 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT00447811 | Mar → May 2007 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01366378 | Jan → Feb 2007 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT00398502 | Oct → Dec 2006 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01366365 | Oct → Nov 2006 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT00387491 | Jun → Oct 2006 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01367535 | Mar → Aug 2006 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT00311350 | Mar → Aug 2006 | constipation disorder | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01367483 | Jun 2005 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01363323 | Nov 2004 → Jan 2005 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01367509 | Mar 2004 → Jan 2005 | impaired renal function disease | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01367522 | Mar → Jul 2004 | liver disorder | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01366352 | Feb → Mar 2004 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01366339 | Oct → Dec 2003 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01367561 | Oct 2002 → May 2003 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01367496 | Jun → Aug 2002 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 29 trials · 1 missed | ||||||
| Phase 2 | NCT03852524 | Feb 2019 → Apr 2021 | ileus | Ohio State University | Completed | Missed primary |
| Phase 2 | NCT01004393 | Oct 2009 → Dec 2013 | constipation disorder, neoplasm, substance-related disorder | University of Vermont | Completed | No outcome recorded |
| Phase 2 | NCT00605644 | Jan → May 2008 | constipation disorder | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT00640146 | Oct 2007 → Jan 2009 | opioid-induced constipation | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT00547586 | Oct 2007 → Feb 2008 | constipation disorder | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT00366431 | Aug 2006 → Mar 2007 | constipation disorder | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT01367548 | Jul 2003 → Dec 2004 | ileus | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT01367587 | Apr → Jul 2002 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT01367574 | Apr 2002 → May 2003 | bowel dysfunction | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 2/32 trials | ||||||
| Phase 2/3 | NCT04083651 | Jan 2020 → Oct 2023 | malignant pancreatic neoplasm | Bausch Health Americas, Inc. | Withdrawn | No outcome recorded |
| Phase 2/3 | NCT02574819 | Apr 2015 → Dec 2016 | opioid-induced constipation | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Unknown | No outcome recorded |
| Phase 312 trials · 5 met primary · 3 missed | ||||||
| Phase 3 | NCT04151719 | Feb 2020 → Feb 2024 | pancreatic adenocarcinoma | Bausch Health Americas, Inc. | Withdrawn | No outcome recorded |
| Phase 3 | NCT01186770 | Sep 2010 → Sep 2011 | opioid-induced constipation | Bausch Health Americas, Inc. | Completed | Met primary |
| Phase 3 | NCT00936884 | Jul 2009 → Nov 2013 | constipation disorder | Bausch Health Americas, Inc. | Completed | Met primary |
| Phase 3 | NCT00804141 | Dec 2008 → Sep 2010 | constipation disorder | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT00528970 | Oct 2007 → Feb 2008 | ileus | Bausch Health Americas, Inc. | Completed | Missed primary |
| Phase 3 | NCT00529087 | Aug 2007 → Dec 2008 | constipation disorder | Bausch Health Americas, Inc. | Completed | Met primary |
| Phase 3 | NCT00387309 | Dec 2006 → Nov 2007 | intestinal dysmotility syndrome | Bausch Health Americas, Inc. | Completed | Missed primary |
| Phase 3 | NCT00401375 | Oct 2006 → Feb 2008 | ileus | Bausch Health Americas, Inc. | Completed | Missed primary |
| Phase 3 | NCT01367613 | Mar 2004 → Jan 2006 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT00402038 | Feb 2004 → Oct 2005 | opioid-induced constipation | Bausch Health Americas, Inc. | Completed | Met primary |
| Phase 3 | NCT00401362 | Feb 2003 → Feb 2005 | opioid-induced constipation | Bausch Health Americas, Inc. | Completed | Met primary |
| Phase 3 | NCT01367600 | Feb 2003 → Feb 2005 | — | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 48 trials · 1 met primary · 2 missed | ||||||
| Phase 4 | NCT06162377 | Jan 2024 → Dec 2026 expected | head and neck squamous cell carcinoma | M.D. Anderson Cancer Center | Recruiting | No outcome recorded |
| Phase 4 | NCT02403830 | Aug 2015 → May 2016 | coronary artery disorder | University of Florida | Completed | Missed primary |
| Phase 4 | NCT01773096 | May 2013 → May 2015 | constipation disorder | Shriners Hospitals for Children | Completed | No outcome recorded |
| Phase 4 | NCT01055704 | Nov 2009 → Feb 2010 | functional gastric disease | Mayo Clinic | Completed | Missed primary |
| Phase 4 | NCT00949377 | Sep 2009 → Dec 2011 | intestinal dysmotility syndrome | Beth Israel Medical Center | Withdrawn | No outcome recorded Stop: Enrollment |
| Phase 4 | NCT00858754 | Mar → Aug 2009 | opioid-induced constipation | Bausch Health Americas, Inc. | Withdrawn | No outcome recorded Stop: Business |
| Phase 4 | NCT00672139 | Jul 2008 → Jan 2013 | opioid-induced constipation | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Phase 4 | NCT00672477 | Jun 2008 → Feb 2013 | opioid-induced constipation | Bausch Health Americas, Inc. | Completed | Met primary |
| Phase not applicable2 trials | ||||||
| — | NCT04787848 | Nov 2021 → May 2027 expected | chronic pain syndrome | Florida International University | Recruiting | No outcome recorded |
| — | NCT01368562 | Jan 2003 → Jun 2008 | opioid-induced constipation | Bausch Health Americas, Inc. | Completed | No outcome recorded |
| Comparator or background therapy12 trials | ||||||
| Phase 1 | NCT01596764 Comparator | May → Jul 2011 | intestinal obstruction | University Medicine Greifswald | Completed | No outcome recorded |
| Phase 1 | NCT01596777 Comparator | Jan → Mar 2010 | intestinal obstruction | University Medicine Greifswald | Completed | No outcome recorded |
| Phase 2 | NCT01117376 Comparator | May 2010 → Jun 2011 | gastroparesis | Shiraz University of Medical Sciences | Terminated | No outcome recorded |
| Phase 2/3 | NCT04743570 Comparator | May 2021 → Apr 2023 | acute pancreatitis | Asbjørn Mohr Drewes | Completed | No outcome recorded |
| Phase 3 | NCT01360372 Comparator | Oct 2010 → May 2012 | — | Drexel University | Withdrawn | No outcome recorded |
| Phase 3 | NCT01050595 Comparator | Dec 2009 → Oct 2010 | opioid-induced constipation | St. John Health System, Michigan | Unknown | No outcome recorded |
| Phase 4 | NCT03523520 Comparator | Dec 2020 → Mar 2023 | opioid-induced constipation | University of Missouri-Columbia | Completed | No outcome recorded |
| Phase 4 | NCT03283020 Comparator | Nov 2017 → Apr 2018 | disorder of pharynx | Region Örebro County | Unknown | No outcome recorded |
| Phase 4 | NCT02977286 Background | Jan 2017 → Oct 2019 | constipation disorder | Tufts Medical Center | Terminated | No outcome recorded Stop: Enrollment |
| Phase 4 | NCT02942550 Comparator | Nov 2016 → Dec 2017 | ST-elevation myocardial infarction | Karolinska University Hospital | Completed | No outcome recorded |
| Phase 4 | NCT01012960 Comparator | Nov 2009 → Jan 2010 | disorder of pharynx, esophageal disorder | Region Örebro County | Completed | No outcome recorded |
| — | NCT03014843 Comparator | Oct 2013 → Jan 2014 | — | Universitaire Ziekenhuizen KU Leuven | Completed | No outcome recorded |
Press releases naming this drug 1 release
| Date | Issuer | Release |
|---|---|---|
| 2023-08-03 | Lantheus Medical Imaging | Lantheus Announces Agreement to Sell RELISTOR® Royalties to HealthCare Royalty lantheus.com ↗ |
Evidence & citations 20 cited values
Every value below carries the sentence it was read from. 72 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | Methylnaltrexone | “A Phase II Double-Blind, Randomized, Parallel Group, Dose Ranging Study of Subcutaneous Methylnaltrexone in Patients With Opioid-Induced Bowel Dysfunction” NCT01367574 ↗ |
| Known as | Bromure de methylnaltrexone | ChEMBL registry synonym — accepted as the source's own label CHEMBL1186579 ↗ |
| Known as | Bromuro de metilnaltrexona | ChEMBL registry synonym — accepted as the source's own label CHEMBL1186579 ↗ |
| Known as | Methylnaltrexone bromide | “Methylnaltrexone bromide (Relistor®). Single intravenous injection of 8 mg (0.4 ml solution) for patients weighing 38-61 kg or 12 mg (0.6 ml solution) patients weighing 62-114 kg).” NCT02942550 ↗8“Methylnaltrexone bromide 150 mg extended release capsule equivalent to 122 mg methylnaltrexone (hard gelatine capsule containing multiple MNTX-ER micro tablets)” NCT01596764 ↗ “Methylnaltrexone bromide will be administered per dose and schedule specified in the respective arm.” NCT04151719 ↗ “Methylnaltrexone bromide 500 mg IR capsule” NCT01596777 ↗ “Intravenous Methylnaltrexone Bromide” NCT01366365 ↗ “Drug: Methylnaltrexone bromide” NCT00672139 ↗ “Drug: Methylnaltrexone bromide” NCT00640146 ↗ |
| Known as | Methylnaltrexone cation | ChEMBL registry synonym — accepted as the source's own label CHEMBL1186579 ↗ |
| Known as | Methylnaltrexone ion | ChEMBL registry synonym — accepted as the source's own label CHEMBL1186579 ↗ |
| Known as | MNTX | “Participants will receive methylnaltrexone (MNTX) 12 milligrams (mg) subcutaneously (SC) once daily for up to 4 or 7 days, depending upon the protocol version under which each...” NCT00640146 ↗20“Subjects received subcutaneous methylnaltrexone (also referred to as MOA-728 or MNTX) or placebo every other day beginning on Day 1 up to a maximum of 7 doses during the 2-week...” NCT00936884 ↗ “This is an open label compassionate use study of subcutaneously administered methylnaltrexone (MNTX) in participants with advance medical illness and opioid-induced constipation.” NCT01368562 ↗ “Methylnaltrexone (MNTX) has been used to prevent the effects of opioids on the bowel and could reduce the incidence of POI when administered preoperatively.” PMID 34798295 ↗ Nov 2021 “Methylnaltrexone (MNTX), a peripherally acting μ-opioid receptor (MOR) antagonist, is FDA-approved for treatment of opioid-induced constipation (OIC).” PMID 27573565 ↗ Aug 2016 “Participants will receive methylnaltrexone bromide (MNTX) 450 milligrams (mg) (3 tablets of 150 mg each) once daily (QD) orally.” NCT04151719 ↗ “This study evaluates the safety of multiple doses of IV MNTX in normal healthy adults.” NCT01367587 ↗ “Methylnaltrexone (MNTX) nearly 0.15mg/kg administered every other day for 2 weeks.” NCT02574819 ↗ “Intravenous (IV) Methylnaltrexone (MNTX)” NCT01367548 ↗ “Methylnaltrexone Bromide (MNTX)” NCT00949377 ↗ “SC Methylnaltrexone (MNTX)” NCT01367600 ↗ |
| Known as | MOA-728 | “The primary purpose of this study is to evaluate the safety and dose-response relationship of N-methylnaltrexone bromide (MOA-728) by observing spontaneous bowel movements in...” NCT00605644 ↗15“Subjects received subcutaneous methylnaltrexone (also referred to as MOA-728 or MNTX) or placebo every other day beginning on Day 1 up to a maximum of 7 doses during the 2-week...” NCT00936884 ↗ “N-methylnaltrexone bromide (MOA-728)” NCT00547586 ↗ “N-methylnaltrexone bromide (MOA-728)” NCT00804141 ↗ “Methylnaltrexone (MOA-728)” NCT00387309 ↗ |
| Known as | MRZ 2663BR | ChEMBL registry synonym — accepted as the source's own label CHEMBL1186579 ↗ |
| Known as | MRZ-2663 | ChEMBL registry synonym — accepted as the source's own label CHEMBL1186579 ↗ |
| Known as | N-methylnaltrexone | “The primary purpose of this study is to evaluate the safety and dose-response relationship of N-methylnaltrexone bromide (MOA-728) by observing spontaneous bowel movements in...” NCT00605644 ↗ |
| Known as | N-methylnaltrexone bromide | “The primary purpose of this study is to evaluate the safety and dose-response relationship of N-methylnaltrexone bromide (MOA-728) by observing spontaneous bowel movements in...” NCT00605644 ↗2“N-methylnaltrexone bromide (MOA-728)” NCT00804141 ↗ “N-methylnaltrexone bromide (MOA-728)” NCT00547586 ↗ |
| Known as | NALTREXONE METHIODIDE | ChEMBL registry synonym — accepted as the source's own label CHEMBL1186579 ↗ |
| Known as | Naltrexone methobromide | ChEMBL registry synonym — accepted as the source's own label CHEMBL1186579 ↗ |
| Known as | Naltrexone methylbromide | ChEMBL registry synonym — accepted as the source's own label CHEMBL1186579 ↗ |
| Known as | Relistor | “Methylnaltrexone bromide (Relistor®). Single intravenous injection of 8 mg (0.4 ml solution) for patients weighing 38-61 kg or 12 mg (0.6 ml solution) patients weighing 62-114 kg).” NCT02942550 ↗1“Patients with AP will be administered Methylnaltrexone (Relistor®) intravenously.” NCT04743570 ↗ |
| Action | Inhibit | “the peripherally acting μ-opioid receptor antagonist methylnaltrexone” PMID 21471758 ↗ May 20111“Mu opioid receptor antagonist” CHEMBL1186579 ↗ |
| Modality | Other / unclassified | “Methylnaltrexone is a peripheral opioid receptor antagonist” PMID 31377269 ↗ Jul 2019 |
| Route | Oral | “MOA-728 Administered Orally” NCT00311350 ↗ |
| Target | OPRM1 | “Mu opioid receptor antagonist” CHEMBL1186579 ↗ |