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
NL-OMON25521 Microbiota targeted therapy as alternative for prednisolone and biologicals in IBD patients during the current COVID-19 threat: a prospective study addressing the safety of Budesonide in combination with rifaximin or the Crohns Disease Exclusion Diet (CDED) Not Available No Nestlé 23/08/2021 None The results of this prospective study may result … Details
NCT00355602 Antibiotics for the Treatment of Ulcerative Colitis None COMPLETED University of Dundee Colitis, Ulcerative DRUG: Cefuroxime|DRUG: Ciprofloxacin|DRUG: Clarit… 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