TheraRadar
Data updated: May 26, 2026

RELISTOR (methylnaltrexone bromide)

Trial Activity: Declining
Gastrointestinal Approved 2008-04-24

RELISTOR is indicated for the treatment of Opioid-Induced Constipation; Chronic Non-Cancer Pain; Active Cancer.

Source: FDA Label • SALIX

How RELISTOR Works

Methylnaltrexone is a selective antagonist of opioid binding at the mu-opioid receptor. As a quaternary amine, its ability to cross the blood-brain barrier is restricted. This allows the medication to function as a peripherally-acting mu-opioid receptor antagonist (PAMORA) in tissues such as the gastrointestinal tract, decreasing the constipating effects of opioids without reversing their analgesic effects in the central nervous system.

Development Insights

Bausch Health Americas, Inc. conducting 3 trials (75%)
6 indications explored (Moderate)
pancreatic cancer (1 trials)
healthy adult subjects (1 trials)
opioid-induced constipation (1 trials)
3
Indications
--
Phase 3 Trials
18
Years on Market

Details

Status
Prescription
First Approved
2008-04-24
Patent Cliff
2031

Pro Metrics

Patent cliff and revenue data

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Routes
ORAL, SUBCUTANEOUS
Dosage Forms
TABLET, SOLUTION

Companies

Active Ingredient: METHYLNALTREXONE BROMIDE

RELISTOR Approval History

2009
2010
2011
2012
2013
2014
2015
2016
2017
2018
2019
2020
2021
2022
2023
2024
2025
2026
Original
New Indication
New Form
Label Update
43 FDA actions from 2008 to 2018 · 1 indication expansions
Mar 2018 SUPPL
Label · Labeling
Aug 2017 SUPPL
Label · Labeling
May 2017 SUPPL
Label · Labeling

What RELISTOR Treats

3 indications

RELISTOR is approved for 3 conditions since its original approval in 2008. These indications span multiple therapeutic areas including oncology, immunology, and more.

  • Opioid-Induced Constipation
  • Chronic Non-Cancer Pain
  • Active Cancer
Source: FDA Label

RELISTOR Competitive Set

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Three rings of competition based on shared molecular targets and treated indications.

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Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.

Drugs Similar to RELISTOR

3 of 4

FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.

MOVANTIK
NALOXEGOL OXALATE
2 shared
AVERITAS
Shared indications:
Opioid-Induced ConstipationChronic Non-Cancer Pain
AMITIZA
LUBIPROSTONE
1 shared
SUCAMPO PHARMA LLC
Shared indications:
Opioid-Induced Constipation
LUBIPROSTONE
LUBIPROSTONE
1 shared
ASCENT PHARMS INC
Shared indications:
Opioid-Induced Constipation
📋

Clinical Trial Registry

4 trials
Trial Sponsor ID Phase Status Title
NCT04083651 SAL-REL-2042 Ph 2, Ph 3 withdrawn A Study of Methylnaltrexone Bromide (MNTX) in Participants With Advanced Pancreatic Cancer
NCT01366326 MNTX 1109 Ph 1 completed Evaluate the Pharmacokinetics (PK) of Methylnaltrexone (MNTX) in Healthy Adult Subjects
NCT00672139 results posted 3200K1-4001 B2541006 Ph 4 completed Safety of Subcutaneous Methylnaltrexone for Opioid-Induced Constipation in Patients With Advanced Illness
NCT01004393 results posted VCC 0911 VCC 0911 Ph 2 completed Methylnaltrexone for Opioid-induced Constipation in Cancer Patients
🔬

Active Pipeline

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Ongoing clinical trials by development phase

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Key Completed Trials

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Completed studies with published results, ranked by significance

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Trial Timeline

Full development history with FDA approval milestones

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Understanding FDA Approval Types
Count Type What it means
- ORIG Original approval - drug first enters market
- SUPPL - Efficacy New indication (new disease/condition approved)
- SUPPL - Labeling Label text changes (warnings, dosing updates)
- SUPPL - Manufacturing Production changes (new facility)
- SUPPL - Chemistry Formulation changes (new dosage strength)

Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.

RELISTOR FDA Label Details

Indications & Usage

FDA Label (PDF)

RELISTOR is indicated for the treatment of Opioid-Induced Constipation; Chronic Non-Cancer Pain; Active Cancer.

View full patent landscape →
12 OB patents · 3 families · 182 international docs across 37 countries

RELISTOR Patents & Exclusivity

Latest Patent: Mar 2031

Patents (12 active)

US8956651 Expires Mar 10, 2031
US9314461 Expires Mar 10, 2031
US10376505 Expires Mar 10, 2031
US8524276 Expires Mar 10, 2031
US10307417 Expires Mar 10, 2031
US8247425 Expires Dec 31, 2030
US9180125 Expires Sep 30, 2029
US9492445 Expires Sep 30, 2029
US9724343 Expires Sep 30, 2029
US8420663 Expires Sep 30, 2029
US8822490 Expires Sep 30, 2029
US12303592 Expires Aug 3, 2027
Source: FDA Orange Book

Pro Intelligence Preview

Deep insights for RELISTOR

Revenue Insights

  • Quarterly revenue tracking
  • Historical trend analysis

Patent Timeline

  • Cliff: 2031
  • 72 active patents

Trial Analysis

  • 4 total trials
  • Stage: Declining

Competitive Landscape

  • 4 similar drugs
  • Same target/indication analysis
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Full approval history • All patents • Revenue trends • Competitor analysis

Data Sources

Data sourced from official FDA and NIH databases. Click links to verify on original sources.

How We Calculate These Metrics

Trial Activity Stage

Measures the current development activity pattern based on trial phases, status, and trends. Important: This measures R&D activity, not commercial lifecycle.

Trial statuses: "Active" means recruiting or ongoing. "Completed" means reached planned endpoint. "Terminated" means stopped early—often due to safety, efficacy, or business reasons.

  • Growth: High proportion of early-phase trials (Phase 1/2), active development
  • Expansion: Significant Phase 3 activity, approaching or pursuing approvals
  • Mature: Substantial Phase 4 post-marketing studies
  • Stable: Mixed phase distribution, steady development
  • Declining: Low active trial ratio, reduced R&D investment