Drug ID:Drug103
Drug Name:Rifaximin
CID:6436173
DrugBank ID:DB01220
Modality:Small Molecule
Groups:approved|investigational
US Approved:YES
Other Approved:YES
Identifier: NCT00355602
Molecular Formula:C43H51N3O11
Molecular Weight:785.9 g/mol
Isomeric SMILES:C[C@H]1/C=C/C=C(\\C(=O)NC2=C(C3=C(C4=C(C(=C3O)C)O[C@@](C4=O)(O/C=C/[C@@H]([C@H]([C@H]([C@@H]([C@@H]([C@@H]([C@H]1O)C)O)C)OC(=O)C)C)OC)C)C5=C2N6C=CC(=CC6=N5)C)O)/C
Synonyms:Rifaximin; Rifaxidin; 80621-81-4; Rifacol; Rifamycin L 105; Rifaximine; Fatroximin; Rifamixin; Rifaximina; Normix
Phase 0: 4
Phase 1: 20
Phase 2: 73
Phase 3: 50
Phase 4: 32
Description:Rifaximin is a semisynthetic, rifamycin-based non-systemic antibiotic, meaning that the drug will not pass the gastrointestinal wall into the circulation as is common for other types of orally administered antibiotics. It is used to treat diarrhea caused by E. coli.

Molecular Structure

2D Molecular Structure

Knowledge Graph

dtIDCIDCompound NameGene IDGene NameSpeciesPubMed IDsAction
dt880 6436173 Rifaximin 8856 NR1I2 Homo sapiens (human) None
dt881 6436173 Rifaximin 93777907 rpoB Escherichia coli K-12 Inhibitor
dt882 6436173 Rifaximin 8856 NR1I2 Homo sapiens (human) Agonist
dt883 6436173 Rifaximin 1576 CYP3A4 Homo sapiens (human) Substrate|Inducer
dt884 6436173 Rifaximin 1557 CYP2C19 Homo sapiens (human) Inducer
dt885 6436173 Rifaximin 1558 CYP2C8 Homo sapiens (human) 11996015 Inducer
dt886 6436173 Rifaximin 8856 NR1I2 Homo sapiens (human) 22790967 [NR1I2 results in increased susceptibility to rifaximin] which results in increased expression of CD36 protein|[nr1i2 results in increased susceptibility to rifaximin] which results in increased expression of CFD mrna|[nr1i2 results in increased susceptib
dt887 6436173 Rifaximin 8856 NR1I2 Homo sapiens (human) 21599020 [rifaximin binds to and results in increased activity of NR1I2 protein] inhibits the reaction [trinitrobenzenesulfonic acid results in increased expression of TNF protein]|[rifaximin binds to and results in increased activity of NR1I2 protein] inhibits th
dt888 6436173 Rifaximin 8856 NR1I2 Homo sapiens (human) Rifaximin results in increased activity of NR1I2 protein
dt889 6436173 Rifaximin 8856 NR1I2 Homo sapiens (human) Rifaximin results in increased expression of NR1I2 mRNA

  • No data available

Phase Distribution
Phase Description
  • Phase 0: Exploratory trials to assess drug behavior in humans
  • Phase 1: Safety trials to determine safe dosage range
  • Phase 2: Efficacy trials to evaluate therapeutic effects
  • Phase 3: Large-scale trials to confirm efficacy and safety
  • Phase 4: Post-marketing surveillance for long-term safety and efficacy

Trial IDTitlePhaseStatusSponsorIndicationsInterventions
NCT05453916 Comparing the Efficacy of Nitazoxanide Versus Rifaximin in Adult Patients With Irritable Bowel Syndrome Without Constipation PHASE1|PHASE2 WITHDRAWN Sadat City University Irritable Bowel Syndrome With Diarrhea DRUG: Nitazoxanide 500Mg Oral Tablet|DRUG: Rifaxi… Details
NCT04841980 Rifaximin Therapy vs Low FODMAP Diet In IBS PHASE4 UNKNOWN University of Malaya Irritable Bowel Syndrome|Small Intestinal Bacteri… DRUG: Rifaximin|OTHER: Low FODMAP diet Details
NCT04557215 Efficacy and Safety of Rifaximin With NAC in IBS-D PHASE1|PHASE2 COMPLETED Cedars-Sinai Medical Center Irritable Bowel Syndrome With Diarrhea DRUG: Rifaximin|DRUG: N-acetylcysteine|DRUG: Plac… Details
NCT04316806 Effect of a Probiotic Formula on Reducing SIBO in IBS Patients NA TERMINATED AB Biotics, SA Irritable Bowel Syndrome|Small Intestinal Bacteri… DIETARY_SUPPLEMENT: Probiotic|DRUG: Rifaximin Details
NCT04254549 Rifaximin in Patients With Diabetic Gastroparesis PHASE2 TERMINATED Mayo Clinic Crohn Disease|Diabetic Gastroparesis DRUG: Rifaximin|DRUG: Placebo Details
NCT04154735 Autologous Transplant Targeted Against Crohn's PHASE2 WITHDRAWN Northwestern University Crohn's Disease DRUG: Fludarabine|DRUG: Cyclophosphamide|DRUG: Me… Details
NCT04074421 Effects of Continuous Treatment With Rifaximin and Probiotics on the Gut Microbiota of Patients With IBS-D PHASE4 UNKNOWN Second Affiliated Hospital, School of Medicine, Zhejiang University IBS - Irritable Bowel Syndrome|Gut Microbiota DRUG: Rifaximin|DRUG: Probiotic Formula|DRUG: Pla… Details
NCT03729271 Hydrogen Breath Test an Instrument to Predict Rifaximin-Response in Irritable Bowel Syndrome Predominant Diarrhea PHASE4 COMPLETED University of Michigan Irritable Bowel Syndrome|Irritable Bowel Syndrome… DRUG: Rifaximin|DEVICE: Glucose and lactulose hyd… Details
NCT03557788 Changes in Microbiota and Metabolomic Profile Between Rifaximin Responders and Non-responders In Diarrhoea-Predominant Irritable Bowel Syndrome PHASE4 COMPLETED National University Hospital, Singapore Irritable Bowel Syndrome With Diarrhea DRUG: Rifaximin Oral Tablet Details
NCT03537157 A Multicentre Study on Rifaximin in Post-operative Endoscopic Crohn's Disease Recurrence Prevention PHASE2 TERMINATED Alfasigma S.p.A. Crohn Disease DRUG: Rifaximin delayed release tablets|OTHER: Pl… Details
NCT03462966 Rifaximin on Visceral Hypersensitivity PHASE2 TERMINATED Cedars-Sinai Medical Center Visceral Hypersensitivity|Irritable Bowel Syndrome DRUG: Rifaximin Details
NCT03219528 A Longitudinal Study to Identify IBS Phenotypes Using Fecal Microbiota and Hydrogen Breath Testing PHASE4 COMPLETED University of Michigan Irritable Bowel Syndrome DRUG: Rifaximin 550 MG|OTHER: Low FODMAP Diet Details
NCT03185624 Effectiveness of Rifaximin on Preventing Postoperative Recurrence in Crohn's Disease PHASE3 UNKNOWN Sixth Affiliated Hospital, Sun Yat-sen University Crohn Disease DRUG: Rifaximin Details
NCT03185611 Effectiveness of Rifaximin Combined With Thiopurine on Preventing Postoperative Recurrence in Crohn's Disease PHASE3 UNKNOWN Sixth Affiliated Hospital, Sun Yat-sen University Crohn Disease DRUG: Rifaximin|DRUG: Azathioprine Details
NCT02651740 Gut Microbiota Reconstruction in the Treatment of Irritable Bowel Syndrome With Predominant Diarrhea PHASE2|PHASE3 UNKNOWN Shanghai Zhongshan Hospital Irritable Bowel Syndrome DRUG: Rifaximin|PROCEDURE: Fecal microbiota trans… Details
NCT02620007 Evaluation of Adherent Invasive E. Coli Eradication in Adult Crohn Disease PHASE2 TERMINATED Assistance Publique - Hôpitaux de Paris Crohn Disease|Adherent-invasive E. Coli DRUG: Ciprofloxacin|DRUG: Rifaximin|DRUG: Ciprofl… Details
NCT02565654 Efficacy of Rifaximin to Treat Diarrhea-predominant Irritable Bowel Syndrome NULL UNKNOWN First Affiliated Hospital, Sun Yat-Sen University Irritable Bowel Syndrome None Details
NCT02272868 Fecal Microbial Transplant in Pediatric Crohn's Disease PHASE1|PHASE2 TERMINATED Seattle Children's Hospital Crohn's Disease BIOLOGICAL: Fecal Microbial transplant|DRUG: Norm… Details
NCT02240121 One Year Study of Rifaximin Delayed Release (DR) Tablets in Crohn's Disease PHASE3 TERMINATED Bausch Health Americas, Inc. Crohn's Disease DRUG: Rifaximin EIR|DRUG: Placebo Details
NCT02240108 One Year Study of Rifaximin Delayed Release (DR) in Crohn's Disease PHASE3 TERMINATED Bausch Health Americas, Inc. Crohn's Disease DRUG: Rifaximin EIR|DRUG: Placebo Details

Disease IDDisease NameDefinitionCategoryRelated DrugsMechanism
2.0 ulcerative colitis A colitis that is predominantly confined to the mucosa located_in colon and includes characteristic ulcers, or open sores. disease of anatomical entity, gastrointestinal system disease, autoimmune disease of gastrointestinal tract; intestinal disease, inflammatory bowel disease, colitis; disease, primary immunodeficiency disease, autoimmune disease, autoimmune disease of gastrointestinal tract Mirikizumab; Olsalazine; Balsalazide; Sulfasalazine; Budesonide; Hydrocortisone acetate; Tixocortol; Kappadione; Teicoplanin; Atezolizumab; Gamolenic acid; Upadacitinib No abstract available Details

Strategy IDTherapeutic StrategySynonymsRelated DrugsMechanism
S01 Anti-inflammatory inflammatory 5-Aminosalicylates (5-ASAs); corticosteroids Crohn's disease and ulcerative colitis are the two main com… Details
S02 Immunosuppression Classic immunosuppressive drugs azathioprine; 6-mercaptopurine; methotrexate; ciclosporin-A; tacrolimus Ciclosporin-A and tacrolimus bind to specific intracellular… Details
S03 Anti-TNF agents Tumor necrosis factor infliximab; adalimumab; golimumab; certolizumab pegol TNF is produced by various immune and non-immune cells in t… Details
S04 T-cell homing and retention T-cell trafficking vedolizumab; anti-MAdCAM1 antibodies ; etrolizumab Inhibition of the interaction between α4β7 integrins on T c… Details
S07 Blockade of cytokine Cytokine signalling apremilast; roflumilast; filgotinib; tofacitinib; ABT494; ABT-874; ustekinumab; isankizumab; LY-2525623; AMG139; MEDI2079; guselkumab Various T-cell subsets, their differentiation pathways and … Details
S08 Strengthening barrier function Modulation of barrier function phosphatidylcholine (lecithin); imiquimod; mongersen Escherichia coli Nissle (EcN) is a nonpathogenic Gram-negat… Details
S11 Improveming Intestinal Microecology the intestinal microbiota antibiotics; probiotics; prebiotics; postbiotics; synbiotics; fecal microbiota transplantation (FMT) The imbalance between beneficial bacteria and harmful patho… Details

Rifaximin as a Therapeutic Ally in the Modulation of Dysbiosis: A Narrative Rev…

PMID: 40530108
Year: 2025
Relationship Type: Treatment Score: 6.5

BACKGROUND: The gastrointestinal microbiota is vital for a well-functioning digestive tract, nutrient metabolism, immune support, and protection agai…

Update on the Role of Rifaximin in Digestive Diseases

PMID: 37004222
Year: 2023
Relationship Type: Treatment Score: 6.5

Various environmental factors affecting the human microbiota may lead to gut microbial imbalance and to the development of pathologies. Alterations o…

Does rifaximin offer any promise in Crohn's disease in remission and concurrent…

PMID: 33429768
Year: 2021
Relationship Type: Treatment Score: 6.5

Microbiota plays an important role in many diseases including inflammatory bowel diseases. Inflammatory bowel disease patients can have concurrent ir…

Increased Faecalibacterium abundance is associated with clinical improvement in…

PMID: 32885687
Year: 2020
Relationship Type: Treatment Score: 6.5

Compositional and functional alterations of the gut microbiota are involved in the pathogenesis of several gastrointestinal diseases. Rifaximin is of…

Mechanism of action and therapeutic benefit of rifaximin in patients with irrit…

PMID: 32047534
Year: 2020
Relationship Type: Treatment Score: 6.5

Irritable bowel syndrome (IBS) is a common functional gastrointestinal disorder with a multifactorial pathophysiology. The gut microbiota differs bet…

Rifaximin anti-inflammatory activity on bovine endometrium primary cell culture…

PMID: 29984902
Year: 2018
Relationship Type: Treatment Score: 6.3

Rifaximin is an unabsorbed oral antibiotic showing anti-inflammatory properties in human pathologies like irritable bowel syndrome and inflammatory b…

Rifaximin decreases virulence of Crohn's disease-associated Escherichia coli an…

PMID: 29410518
Year: 2018
Relationship Type: Association Score: 6.3

Escherichia coli with an adherent and invasive pathotype (AIEC) is implicated in the pathogenesis of Crohn's disease (CD). Rifaximin improves symptom…

The effect of cyclic rifaximin therapy on symptoms of diverticular disease from…

PMID: 28702105
Year: 2017
Relationship Type: Treatment Score: 6.3

INTRODUCTION: Symptomatic uncomplicated diverticular disease of the colon (SUDD) is one of the most common diseases with which patients present to a …

Use of rifaximin in gastrointestinal and liver diseases

PMID: 27547007
Year: 2016
Relationship Type: Treatment Score: 6.3

Rifaximin is a broad spectrum oral antibiotic with antimicrobial activity against Gram-positive and Gram-negative aerobic and anaerobic bacteria. It …

Synergic Interaction of Rifaximin and Mutaflor (Escherichia coli Nissle 1917) i…

PMID: 27433160
Year: 2016
Relationship Type: Treatment Score: 6.3

Background. Inflammatory bowel disease results from the dysregulation of immune response to environmental and microbial agents in genetically suscept…

Introduction: understanding mechanisms of the actions of rifaximin in selected …

PMID: 26618920
Year: 2016
Relationship Type: Mechanism Score: 6.3

BACKGROUND: Historically, the beneficial effects of the nonsystemic oral agent rifaximin on various gastrointestinal (GI) disorders have been attribu…

Role of Rifaximin in Inflammatory Bowel Disease Treatment

PMID: 26202194
Year: 2015
Relationship Type: Treatment Score: 6.3

Inflammatory bowel diseases are characterised by an altered composition of the intestinal microbiota, which may contribute to their development and m…

Therapeutic Effects and Mechanisms of Action of Rifaximin in Gastrointestinal D…

PMID: 26162610
Year: 2015
Relationship Type: Treatment Score: 6.3

Emerging preclinical and clinic evidence described herein suggests that the mechanism of action of rifaximin is not restricted to direct antibacteria…

EFFECT OF PREGNANE XENOBIOTIC RECEPTOR ACTIVATION ON INFLAMMATORY BOWEL DISEASE…

PMID: 26122229
Year: 2015
Relationship Type: Association Score: 6.3

The causes and pathogenesis of Inflammatory Bowel Disease (IBD) are still not clearly understood. This study aims to prove the important role of rifa…

Rifaximin, gut microbes and mucosal inflammation: unraveling a complex relation…

PMID: 25244596
Year: 2014
Relationship Type: Treatment Score: 6.3

Rifaximin is a non-systemic, broad-spectrum antibiotic that acts against gram-positive, gram-negative, and anaerobic bacteria. Clinical studies indic…

Rifaximin and Crohn's disease

PMID: 24259983
Year: 2013
Relationship Type: Clinical Trial Score: 6.1

In a recent article, Longman and Swaminath analyzed our paper on the use of rifaximin in patients with moderately active Crohn's disease (CD). Here w…

[Rifaximin for hepatic encephalopathy in children. Case report]

PMID: 22231877
Year: 2011
Relationship Type: Treatment Score: 6.1

Rifaximin is an antibiotic recently approved for the treatment of hepatic encephalopathy in adults. In children more than 12 year-old, it has been ap…

Rifaximin-extended intestinal release induces remission in patients with modera…

PMID: 22155172
Year: 2012
Relationship Type: Treatment Score: 6.1

BACKGROUND & AIMS: Bacteria might be involved in the development and persistence of inflammation in patients with Crohn's disease (CD), and antibioti…

Inhibition of NF-κB by a PXR-dependent pathway mediates counter-regulatory acti…

PMID: 21806984
Year: 2011
Relationship Type: Treatment Score: 6.1

A dysregulated interaction between intestinal epithelial cells (IEC) and components of innate immunity is a hallmark of inflammatory bowel diseases. …

Rifaximin modulates the colonic microbiota of patients with Crohn's disease: an…

PMID: 20852272
Year: 2010
Relationship Type: Adverse Effect Score: 6.1

OBJECTIVES: Rifaximin, a rifamycin derivative, has been reported to induce clinical remission of active Crohn's disease (CD), a chronic inflammatory …

Showing 1-20 of 22 articles