rifapentine

Trade name: priftin

Small moleculeapprovedOrphan Drug FDA

Approved

Jun 22, 1998

PRIFTIN® (rifapentine) is indicated in adults and children 12 years and older for the treatment of active pulmonary tuberculosis (TB) caused by Mycobacterium tuberculosis. PRIFTIN must always be used in combination with one or more antituberculosis (anti-TB) drugs to which the isolate is susceptible. Rifapentine 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. And it acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death. 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. Because of rapid emergence of resistant bacteria, use is restricted to treatment of mycobacterial infections and a few other indications. Rifampin is well absorbed when taken orally and is distributed widely in body tissues and fluids, including the CSF. It is metabolized in the liver and eliminated in bile and, to a much lesser extent, in urine, but dose adjustments are unnecessary with renal insufficiency. Rifapentine has shown higher bacteriostatic and bactericidal activities especially against intracellular bacteria growing in human monocyte-derived macrophages. — NCATS

Clinical trial activity

65 trials · 95 clinical orgs · 2 marketing orgs

Phase 1
17
Phase 2
36
Phase 3
25
Phase 4
9

Earliest trial started Apr 1, 1995 (NCT00023335)

Timeline

1990s

  1. Jan 1, 1995

    Earliest Phase 3 Sponsor(trial)

  2. Jun 9, 1995

    Orphan Drug Designation

  3. Jun 22, 1998

    Hoechst Marion Roussel — Earliest FDA Approval

  4. Jun 22, 1998

    Sanofi-Aventis — NDA Secondary Org

  5. Jun 22, 1998

    Hoechst Marion Roussel — NDA Organization

  6. Jan 1, 1999

    Earliest Phase 2 Sponsor(trial)

2000s

  1. Jan 1, 2007

    Earliest Phase 1 Sponsor(trial)

Indications

Mechanism of action

Approval history

  • approvedPriority reviewAcceleratedJun 22, 1998

Chemistry & pharmacology

Loading structure…

SMILES

CO[C@H]1\C=C\O[C@@]2(C)OC3=C(C)C(O)=C4C(O)=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(\C=N\N5CCN(CC5)C6CCCC6)=C(O)C4=C3C2=O
Mol. weight
877.0307 g/mol
Lipinski Ro5
4 violation(s)
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • 25-desacetyl rifapentin
  • 25-desacetyl rifapentine
  • 25-desacetyl rifapentine
  • 3-(((4-cyclopentyl-1-piperazinyl)imino)methyl)rifamycin
  • 3-(((4-cyclopentyl-1-piperazinyl)imino)methyl)rifamycin
  • 3-(((4-cyclopentyl-1-piperazinyl)imino)methyl)rifamycin
  • 3-(((4-cyclopentyl-1-piperazinyl)imino)methyl)rifamycin sv
  • cyclopentylrifampicin
  • cyclopentylrifampicin
  • dl473
  • dl 473
  • dl-4-73
  • dl 473-it
  • mdl 473
  • mdl-473
  • mdl-473
  • priftin
  • priftin
  • priftin
  • priftin
  • priftin (tn)
  • priftin (tn)
  • rifapentene
  • rifapentine
  • rifapentine
  • rifapentine
  • rifapentine
  • rifapentine
  • rifapentine
  • rifapentine
  • rifapentine
  • rifapentine
  • rifapentine
  • rifapentine
  • rifapex

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07124559Phase 1/Phase 2 (Phase 2)Dec 15, 2025National Institute of Allergy and Infectious Diseases (NIAID), National Institute of Mental Health (NIMH), National Institutes of Health (NIH)
NCT07086820N/AOct 31, 2025Pontificia Universidad Catolica de Chile
NCT07069582Phase 1Oct 1, 2025McGill University, Padjadjaran University
NCT06917495Phase 2Apr 5, 2025Shandong University
NCT06498414Phase 2/Phase 3 (Phase 3)Feb 1, 2025Canadian Institutes of Health Research (CIHR), McGill University
NCT06568484Phase 3Nov 30, 2024Elizabeth Glaser Pediatric AIDS Foundation, Johns Hopkins University, United States Agency for International Development
NCT06253715Phase 3Nov 27, 2024Johns Hopkins University, United States Agency for International Development
NCT06281834Phase 1Sep 30, 2024APIN Public Health Initiatives, Harvard University, University of Cape Town
NCT06191692Phase 3Apr 1, 2024Freundeskreis Für Internationale Tuberkulosehilfe e.V
NCT06022146Phase 3Sep 1, 2023Fudan University
NCT05630872Phase 2Feb 6, 2023Mylan, National Institute of Allergy and Infectious Diseases (NIAID), ViiV Healthcare
NCT05401071Phase 3Nov 1, 2022Fudan University
NCT05122767Phase 1/Phase 2 (Phase 2)Oct 30, 2022Aurum Institute, Johns Hopkins University
NCT05118490Phase 4Oct 30, 2022Aurum Institute, Johns Hopkins University
NCT05122026Phase 1/Phase 2 (Phase 2)Oct 30, 2022Aurum Institute, Cornell University, Johns Hopkins University, University of Washington
NCT05454345Phase 3Oct 1, 2022Zhejiang University
NCT05411744Phase 4Jul 1, 2022Rutgers University
NCT05021731Phase 4Apr 1, 2022Hospital Universitari de Bellvitge, Universidad Carlos III Madrid, University of Barcelona
NCT04703075Phase 4Dec 31, 2021Johns Hopkins University, National Institute of Allergy and Infectious Diseases (NIAID)
NCT04856644Phase 3May 1, 2021Chang Gung University, Government of Taiwan, Kaohsiung Medical University, National Taiwan University, Taipei Veteran General hospital
Showing 20 of 65 trials
Page 1 / 4

Organizations

Research & Development (95)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Johns Hopkins UniversityAcademic/Hospital16742002
Centers for Disease Control and Prevention (CDC)Government141241995
National Institute of Allergy and Infectious Diseases (NIAID)Government9842002
Department of Veteran AffairsGovernment8041995
Aurum InstituteAcademic/Hospital5332016
Fudan UniversityAcademic/Hospital5522015
University of LondonAcademic/Hospital5112016
SanofiFor profit4122008
University of Cape TownAcademic/Hospital4132010
National Institutes of Health (NIH)Government3222016
National Taiwan UniversityAcademic/Hospital3212014
University of Texas, San AntonioAcademic/Hospital3132005
AIDS Clinical Trials GroupAcademic/Hospital2012016
Cornell UniversityAcademic/Hospital2012017
McGill UniversityAcademic/Hospital2222025
MerckFor profit2012009
Stellenbosch UniversityAcademic/Hospital2022016
United States Agency for International DevelopmentGovernment2012024
University of California, San FranciscoAcademic/Hospital2022016
University of NebraskaAcademic/Hospital2022012
95 organizations
Page 1 / 5

Marketing (2)

OrganizationOrg typeRelationshipDate
Hoechst Marion RousselFor profitNDAJun 22, 1998
Sanofi-AventisFor profitNDA2Jun 22, 1998