rifapentine
Trade name: priftin
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
Earliest trial started Apr 1, 1995 (NCT00023335)
Timeline
1990s
- Jan 1, 1995
Earliest Phase 3 Sponsor(trial)
- Jun 9, 1995
Orphan Drug Designation
- Jun 22, 1998
Hoechst Marion Roussel — Earliest FDA Approval
- Jun 22, 1998
Sanofi-Aventis — NDA Secondary Org
- Jun 22, 1998
Hoechst Marion Roussel — NDA Organization
- Jan 1, 1999
Earliest Phase 2 Sponsor(trial)
2000s
- Jan 1, 2007
Earliest Phase 1 Sponsor(trial)
Indications
Studied for
- Behavior, Addictive · Phase 4
- Brain Injuries, Traumatic · Phase 2
- Breast Feeding · Phase 1
- Diabetes Mellitus · Phase 3
- Drug Interactions · Phase 1
- Drug-Related Side Effects and Adverse Reactions · Phase 1
- Healthy Volunteers · Phase 1
- Hepatitis · Phase 4
- HIV · Phase 4
- HIV Infections · Phase 4
- HIV Seropositivity · Phase 4
- Infertility, Female · Phase 3
- Kidney Failure, Chronic · Phase 4
- Kidney Neoplasms · Phase 4
- Kidney Transplantation · Phase 4
- Latent Tuberculosis · Phase 4
- Mycobacterium avium-intracellulare Infection · Phase 2
- Mycobacterium tuberculosis · Phase 3
- Opioid-Related Disorders · Phase 4
- Patient Compliance · Phase 4
- Pregnancy · Phase 1/Phase 2
- Prostheses and Implants · Phase 3
- Renal Insufficiency · Phase 4
- Silicosis · Phase 3
- Tuberculosis · Phase 4
- Tuberculosis, Female Genital · Phase 3
- Tuberculosis, Lymph Node · Phase 3
- Tuberculosis, Pulmonary · Phase 3
Mechanism of action
Bacterial DNA-directed RNA polymerase inhibitor
Beta subunit is binding site
Approval history
- approvedPriority reviewAcceleratedJun 22, 1998
Chemistry & pharmacology
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
- WikipediaRifapentine ↗
- NCATSXJM390A33U ↗
- ChEMBLCHEMBL1660 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07124559 | Phase 1/Phase 2 (Phase 2) | Dec 15, 2025 | National Institute of Allergy and Infectious Diseases (NIAID), National Institute of Mental Health (NIMH), National Institutes of Health (NIH) |
| NCT07086820 | N/A | Oct 31, 2025 | Pontificia Universidad Catolica de Chile |
| NCT07069582 | Phase 1 | Oct 1, 2025 | McGill University, Padjadjaran University |
| NCT06917495 | Phase 2 | Apr 5, 2025 | Shandong University |
| NCT06498414 | Phase 2/Phase 3 (Phase 3) | Feb 1, 2025 | Canadian Institutes of Health Research (CIHR), McGill University |
| NCT06568484 | Phase 3 | Nov 30, 2024 | Elizabeth Glaser Pediatric AIDS Foundation, Johns Hopkins University, United States Agency for International Development |
| NCT06253715 | Phase 3 | Nov 27, 2024 | Johns Hopkins University, United States Agency for International Development |
| NCT06281834 | Phase 1 | Sep 30, 2024 | APIN Public Health Initiatives, Harvard University, University of Cape Town |
| NCT06191692 | Phase 3 | Apr 1, 2024 | Freundeskreis Für Internationale Tuberkulosehilfe e.V |
| NCT06022146 | Phase 3 | Sep 1, 2023 | Fudan University |
| NCT05630872 | Phase 2 | Feb 6, 2023 | Mylan, National Institute of Allergy and Infectious Diseases (NIAID), ViiV Healthcare |
| NCT05401071 | Phase 3 | Nov 1, 2022 | Fudan University |
| NCT05122767 | Phase 1/Phase 2 (Phase 2) | Oct 30, 2022 | Aurum Institute, Johns Hopkins University |
| NCT05118490 | Phase 4 | Oct 30, 2022 | Aurum Institute, Johns Hopkins University |
| NCT05122026 | Phase 1/Phase 2 (Phase 2) | Oct 30, 2022 | Aurum Institute, Cornell University, Johns Hopkins University, University of Washington |
| NCT05454345 | Phase 3 | Oct 1, 2022 | Zhejiang University |
| NCT05411744 | Phase 4 | Jul 1, 2022 | Rutgers University |
| NCT05021731 | Phase 4 | Apr 1, 2022 | Hospital Universitari de Bellvitge, Universidad Carlos III Madrid, University of Barcelona |
| NCT04703075 | Phase 4 | Dec 31, 2021 | Johns Hopkins University, National Institute of Allergy and Infectious Diseases (NIAID) |
| NCT04856644 | Phase 3 | May 1, 2021 | Chang Gung University, Government of Taiwan, Kaohsiung Medical University, National Taiwan University, Taipei Veteran General hospital |
Organizations
Research & Development (95)
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Hoechst Marion Roussel | For profit | NDA | Jun 22, 1998 |
| Sanofi-Aventis | For profit | NDA2 | Jun 22, 1998 |