Daily dosing of rifapentine cures tuberculosis in three months or less in the murine model

PLoS Med. 2007 Dec;4(12):e344. doi: 10.1371/journal.pmed.0040344.

Abstract

Background: Availability of an ultra-short-course drug regimen capable of curing patients with tuberculosis in 2 to 3 mo would significantly improve global control efforts. Because immediate prospects for novel treatment-shortening drugs remain uncertain, we examined whether better use of existing drugs could shorten the duration of treatment. Rifapentine is a long-lived rifamycin derivative currently recommended only in once-weekly continuation-phase regimens. Moxifloxacin is an 8-methoxyfluoroquinolone currently used in second-line regimens.

Methods and findings: Using a well-established mouse model with a high bacterial burden and human-equivalent drug dosing, we compared the efficacy of rifapentine- and moxifloxacin-containing regimens with that of the standard daily short-course regimen based on rifampin, isoniazid, and pyrazinamide. Bactericidal activity was assessed by lung colony-forming unit counts, and sterilizing activity was assessed by the proportion of mice with culture-positive relapse after 2, 3, 4, and 6 mo of treatment. Here, we demonstrate that replacing rifampin with rifapentine and isoniazid with moxifloxacin dramatically increased the activity of the standard daily regimen. After just 2 mo of treatment, mice receiving rifapentine- and moxifloxacin-containing regimens were found to have negative lung cultures, while those given the standard regimen still harbored 3.17 log10 colony-forming units in the lungs (p < 0.01). No relapse was observed after just 3 mo of treatment with daily and thrice-weekly administered rifapentine- and moxifloxacin-containing regimens, whereas the standard daily regimen required 6 mo to prevent relapse in all mice.

Conclusions: Rifapentine should no longer be viewed solely as a rifamycin for once-weekly administration. Our results suggest that treatment regimens based on daily and thrice-weekly administration of rifapentine and moxifloxacin may permit shortening the current 6 mo duration of treatment to 3 mo or less. Such regimens warrant urgent clinical investigation.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Antibiotics, Antitubercular / administration & dosage*
  • Antitubercular Agents / administration & dosage*
  • Aza Compounds / administration & dosage*
  • Colony Count, Microbial
  • Disease Models, Animal
  • Drug Administration Schedule
  • Drug Therapy, Combination
  • Fluoroquinolones
  • Isoniazid / administration & dosage
  • Lung / drug effects*
  • Lung / microbiology
  • Mice
  • Mice, Inbred BALB C
  • Moxifloxacin
  • Mycobacterium tuberculosis / drug effects*
  • Mycobacterium tuberculosis / growth & development
  • Pyrazinamide / administration & dosage
  • Quinolines / administration & dosage*
  • Rifampin / administration & dosage
  • Rifampin / analogs & derivatives*
  • Secondary Prevention
  • Time Factors
  • Tuberculosis / drug therapy*
  • Tuberculosis / microbiology

Substances

  • Antibiotics, Antitubercular
  • Antitubercular Agents
  • Aza Compounds
  • Fluoroquinolones
  • Quinolines
  • Pyrazinamide
  • Moxifloxacin
  • Isoniazid
  • Rifampin
  • rifapentine