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rifampin

Small moleculeapproved

Approved

May 21, 1971

Rifampin is an antibiotic that inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme. It is bactericidal and has a very broad spectrum of activity against most gram-positive and gram-negative organisms (including Pseudomonas aeruginosa) and specifically Mycobacterium tuberculosis. It is FDA approved for the treatment of tuberculosis, meningococcal carrier state. Healthy subjects who received rifampin 600 mg once daily concomitantly with saquinavir 1000 mg/ritonavir 100 mg twice daily (ritonavir-boosted saquinavir) developed severe hepatocellular toxicity. Rifampin has been reported to substantially decrease the plasma concentrations of the following antiviral drugs: atazanavir, darunavir, fosamprenavir, saquinavir, and tipranavir. These antiviral drugs must not be co-administered with rifampin. Common adverse reactions include heartburn, epigastric distress, anorexia, nausea, vomiting, jaundice, flatulence, cramps. — NCATS

Clinical trial activity

463 trials · 501 clinical orgs · 17 marketing orgs

Phase 1
263
Phase 2
125
Phase 3
60
Phase 4
42

Earliest trial started Jan 1, 1991 (NCT00004689)

Timeline

1970s

  1. May 21, 1971

    Earliest FDA Approval

  2. May 21, 1971

    Oxford Pharmaceuticals — NDA Secondary Org

  3. May 21, 1971

    Sanofi-Aventis — NDA Secondary Org

  4. Jul 11, 1975

    Sanofi-Aventis — Marketing Organization

1990s

  1. Jan 1, 1991

    Earliest Phase 2 Sponsor(trial)

  2. May 28, 1997

    Epic Pharma Llc — Marketing Organization

  3. May 28, 1997

    Sandoz — Marketing Organization

  4. Jan 1, 1999

    Earliest Phase 3 Sponsor(trial)

  5. Oct 29, 1999

    West-Ward Pharmaceutical — Marketing Organization

2000s

  1. Mar 14, 2001

    Akorn, Inc. — Marketing Organization

  2. Jan 1, 2005

    Earliest Phase 1 Sponsor(trial)

  3. Jul 29, 2005

    Hikma — Marketing Organization

  4. Mar 28, 2008

    Chartwell Pharmaceuticals — Marketing Organization

  5. Mar 28, 2008

    Lannett Company, Inc. — Marketing Organization

  6. May 22, 2008

    Mylan — Marketing Organization

2010s

  1. Aug 21, 2013

    Lupin — Marketing Organization

  2. Aug 18, 2014

    Emcure — Marketing Organization

  3. Aug 18, 2014

    Avet Lifesciences — Marketing Organization

  4. Aug 21, 2014

    Fresenius — Marketing Organization

  5. Jan 19, 2016

    Watson Pharmaceuticals — Marketing Organization

  6. Jan 19, 2016

    Allergan PLC (2015) — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Combination products

Approval history

  • approvedMay 21, 1971

Chemistry & pharmacology

Loading structure…

SMILES

CO[C@H]1\C=C\O[C@@]2(C)OC3=C(C2=O)C4=C(O)C(\C=N\N5CCN(C)CC5)=C(NC(=O)C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C)C(O)=C4C(O)=C3C
Mol. weight
822.9402 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Availability
Prescription Only

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • 3-(((4-methyl-1-piperazinyl)imino)methyl)rifamycin sv
  • 3-(((4-methyl-1-piperazinyl)imino)methyl)rifamycin sv
  • ba-411661e
  • ba-411661e
  • ba-41166e
  • ba-41166e
  • dextrosulphenidol
  • dextrosulphenidol
  • eremfat
  • eremfat
  • l-5103
  • l-5103
  • l-5103-lepetit
  • l-5103-lepetit
  • refampicin
  • rfp
  • rfp
  • rifadin
  • rifadin
  • rifadin
  • rifadin
  • rifadin
  • rifadine
  • rifadine
  • rifaldazine
  • rifaldin
  • rifampicin
  • rifampicin
  • rifampicin
  • rifampicin
  • rifampicin
  • rifampicin
  • rifampicin
  • rifampicin
  • rifampicin
  • rifampicina
  • rifampicina
  • rifampicinum
  • rifampicinum
  • rifampin
  • rifampin
  • rifampin
  • rifampin
  • rifampin
  • rifampin
  • rifampin
  • rifaprodin
  • rimactane
  • rimactane
  • thiamphenicol
  • thiamphenicol
  • thiamphenicol
  • thiamphenicol
  • thiamphenicol
  • thiamphenicol
  • thiamphenicol
  • thiamphenicol
  • thiamphenicol aminoacetate hcl
  • thiamphenicol aminoacetate hcl
  • thiamphenicol aminoacetate hydrochloride
  • thiamphenicol glycinate
  • thiamphenicol glycinate
  • thiamphenicol glycinate
  • thiamphenicol glycinate
  • thiamphenicol glycinate
  • thiamphenicol glycine ester
  • thiocymetin
  • thiocymetin
  • thiocymetin
  • thiophenicol
  • thiophenicol
  • thiophenicol
  • thiophenicol glycinate
  • urfamicin
  • win-50632
  • win-50632

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07118696Phase 3Feb 1, 2026Hamilton Health Sciences Corporation, McMaster University, University of London
NCT07303699Phase 2Jan 3, 2026Obafemi Awolowo University, Open Philanthropy Project
NCT07242781Phase 1Dec 8, 2025Bristol-Myers Squibb, Celgene
NCT07253688Phase 3Nov 30, 2025Canadian Institutes of Health Research (CIHR), McGill University, The Peter Doherty Institute, University of Melbourne
NCT07163143Phase 3Nov 30, 2025Aurum Institute, Foundation for Innovative New Diagnostics, Switzerland, KTH Royal Institute of Technology, University of London, Wits Health Consortium (Pty) Ltd
NCT07313215N/ANov 13, 2025Fujian Medical University
NCT07073638Phase 2Oct 6, 202530 Technology
NCT07069582Phase 1Oct 1, 2025McGill University, Padjadjaran University
NCT07129629Phase 2Aug 20, 2025Fudan University, Huazhong University of Science and Technology
NCT07058090Phase 1Jul 31, 2025Liaquat University of Medical & Health Sciences
NCT07076225Phase 3Jul 25, 2025Capital Medical University, Fudan University, Huazhong University of Science and Technology, Shenzhen Third People's Hospital, Sichuan University, Tsinghua University
NCT07084402Phase 4Jul 24, 2025Capital Medical University, MicuRx, Peking University
NCT07213765Phase 4Jul 24, 2025Anhui Medical University, Capital Medical University, Guangzhou Chest Hospital., Huazhong University of Science and Technology, Jiangxi Chest Hospital, MicuRx, Peking University
NCT07056842Phase 1Jul 20, 2025Government of China
NCT07018635Phase 1Jul 16, 2025Incyte
NCT07014488Phase 1Jun 20, 2025Hengrui Therapeutics, Inc.
NCT07196449Phase 1May 14, 2025Seoul National University
NCT06909162Phase 1May 5, 2025Incyte
NCT06905522Phase 3Apr 15, 2025Shenyang Tenth People's Hospital, Shenzhen Third People's Hospital, Zhejiang University
NCT06917495Phase 2Apr 5, 2025Shandong University
Showing 20 of 463 trials
Page 1 / 24

Organizations

Research & Development (501)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Institute of Allergy and Infectious Diseases (NIAID)Government262051999
Johns Hopkins UniversityAcademic/Hospital18842002
University of Cape TownAcademic/Hospital17532008
PfizerFor profit161331994
Radboud UniversityAcademic/Hospital13552010
Bristol-Myers SquibbFor profit12912005
Centers for Disease Control and Prevention (CDC)Government111042000
University of California, San FranciscoAcademic/Hospital11752004
University of LondonAcademic/Hospital11422008
AstraZenecaFor profit10922010
Boehringer IngelheimFor profit101012009
GlaxoSmithKlineFor profit10622006
Global Alliance for TB Drug DevelopmentAcademic/Hospital10732006
TASK Applied ScienceFor profit10312010
Fudan UniversityAcademic/Hospital9452009
Government of ChinaGovernment9432015
Johnson and JohnsonFor profit9812007
CelgeneFor profit8812011
European and Developing Countries Clinical Trials Partnership (EDCTP)Academic/Hospital8022008
Hengrui Therapeutics, Inc.For profit8812016
501 organizations
Page 1 / 26

Marketing (21)

OrganizationOrg typeRelationshipDate
Akorn, Inc.For profitMKTGMar 14, 2001
Allergan PLC (2015)For profitMKTGJan 19, 2016
Avet LifesciencesFor profitMKTGAug 18, 2014
Chartwell PharmaceuticalsFor profitMKTGMar 28, 2008
EmcureFor profitMKTGAug 18, 2014
Epic Pharma LlcFor profitSYNMay 28, 1997
Epic Pharma LlcFor profitMKTGMay 28, 1997
FreseniusFor profitMKTGAug 21, 2014
HikmaFor profitMKTGJul 29, 2005
HikmaFor profitSYNMar 3, 2016
HikmaFor profitSYNOct 29, 1999
Lannett Company, Inc.For profitMKTGMar 28, 2008
LupinFor profitMKTGAug 21, 2013
MylanFor profitMKTGMay 22, 2008
Oxford PharmaceuticalsFor profitNDA2May 21, 1971
Richardson Vicks IncFor profitNDA—
SandozFor profitMKTGMay 28, 1997
Sanofi-AventisFor profitNDA2May 21, 1971
Sanofi-AventisFor profitMKTGJul 11, 1975
Watson PharmaceuticalsFor profitMKTGJan 19, 2016
West-Ward PharmaceuticalFor profitMKTGOct 29, 1999