For research use only.
Catalog No.S1760 Synonyms: MDL473
CAS No. 61379-65-5
Rifapentine (MDL473) is an antibiotic, which inhibits DNA-dependent RNA polymerase activity, used to treat tuberculosis.
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|Description||Rifapentine (MDL473) is an antibiotic, which inhibits DNA-dependent RNA polymerase activity, used to treat tuberculosis.|
Rifapentine inhibits the function of DNA-dependent RNA polymerase in strains of M. tuberculosis, while inducing no effect on mammalian cells. Both Rifapentine and its active metabolite, 25-desacetylrifapentine, localize within monocyte-derived macrophages, thus allowing for intracellular inhibition of M. tuberculosis at a greater kill rate as compared with that of the parent or metabolite alone. Rifapentine is deacetylated in the liver and induces cytochrome P450 much less than rifampin.  Rifapentine has shown higher bacteriostatic and bactericidal activities (MICs and MBCs) than RMP, especially against intracellular bacteria growing in human monocyte-derived macrophages. 
|In vivo||Rifapentine inhibits bacterial RNA synthesis by binding to the β-subunit of DNA-dependent RNA polymerase in susceptible species. Rifapentine is generally more active than rifampicin against sensitive strains of M. tuberculosis.  Rifapentine significantly increases the rate of antipyrine and pentobarbital metabolism in vivo. Rifapentine also increases liver weight, the content of liver microsomal protein and cytochrome P-450, the activity of NADPH-cytochrome C reductase and NADPH oxidase.  Rifapentine combined with isoniazid (INH) and pyrazinamide (PZA) administered daily results in an apparent clearance of M.tuberculosis organisms in the lungs and spleens of infected mice after 10 weeks of treatment. |
-  Temple ME, et al. Ann Pharmacother, 1999, 33(11), 1203-1210.
-  Mor N, et al. Antimicrob Agents Chemother, 1995, 39(9), 2073-2077.
-  Jarvis B, et al. Drugs, 1998, 56(4), 607-616.
|In vitro||DMSO||100 mg/mL (114.02 mM)|
|Ethanol||17 mg/mL (19.38 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03730181||Active not recruiting||Drug: Rifapentine|Drug: Isoniazid||Latent Tuberculosis||Centers for Disease Control and Prevention|University of Stellenbosch|Johns Hopkins University|Sanofi|University of Cape Town|Chris Hani Baragwanath Academic Hospital|Washington D.C. Veterans Affairs Medical Center||October 12 2019||Phase 1|Phase 2|
|NCT04094012||Recruiting||Drug: isoniazid and rifapentine||Latent Tuberculosis Infection||National Taiwan University Hospital||September 24 2019||Phase 3|
|NCT01690403||Completed||Drug: rifapentine (M000473)|Drug: EFZ EMT TDF||Tuberculosis||Sanofi||December 2012||Phase 1|
|NCT01574638||Completed||Drug: Rifapentine (RPT)||Tuberculosis||National Institute of Allergy and Infectious Diseases (NIAID)||June 2012||Phase 1|
|NCT00814671||Completed||Drug: Rifapentine 450|Drug: Rifapentine 600|Drug: Rifampin||Tuberculosis||Johns Hopkins University|University of Cape Town Lung Institute|University of Cape Town||April 2010||Phase 2|
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