A rifapentine-containing inhaled triple antibiotic formulation for rapid treatment of tubercular infection

Pharmaceutical Research

Volumn 31, Issue 5, 2014, Pages 1239-1253

  Chan, John Gar Yan ^a   Tyne, Anneliese S ^b   Pang, Angel ^b   Chan, Hak Kim ^b   Young, Paul M ^a   Britton, Warwick J ^b,c   Duke, Colin C ^b   Traini, Daniela ^a  

^a University of Sydney   (Australia)

^b UNIVERSITY OF SYDNEY   (Australia)

^c UNIVERSITY OF SYDNEY   (Australia)

Author keywords

inhaled aerosol; rifapentine; treatment shortening; tuberculosis

Indexed keywords

LEUCINE; MOXIFLOXACIN; PYRAZINAMIDE; RIFAMPICIN; RIFAPENTINE; RIFAPENTINE PLUS MOXIFLOXACIN PLUS PYRAZINAMIDE; TUBERCULOSTATIC AGENT; UNCLASSIFIED DRUG; AEROSOL; POWDER;

AEROSOL; ANTIBACTERIAL ACTIVITY; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; CRYSTALLIZATION; DRUG FORMULATION; DRUG STABILITY; DRY POWDER; IN VITRO STUDY; MINIMUM INHIBITORY CONCENTRATION; MOISTURE; MYCOBACTERIUM TUBERCULOSIS; NONHUMAN; PARTICLE SIZE; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; SPRAY DRYING; ANALOGS AND DERIVATIVES; ANIMAL; HUMAN; INHALATIONAL DRUG ADMINISTRATION; MICROBIAL SENSITIVITY TEST; MOUSE; POWDER; POWDER DIFFRACTION; SCANNING ELECTRON MICROSCOPY; TUBERCULOSIS;

ADMINISTRATION, INHALATION; AEROSOLS; ANIMALS; ANTIBIOTICS, ANTITUBERCULAR; HUMANS; MICE; MICROBIAL SENSITIVITY TESTS; MICROSCOPY, ELECTRON, SCANNING; PARTICLE SIZE; POWDER DIFFRACTION; POWDERS; RIFAMPIN; TUBERCULOSIS;

EID: 84902246417     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-013-1245-7     Document Type: Article

References (76)

1. World Health Organisation W. Standard treatment regimens. Geneva: WHO Press; 2010.
2. Rosenthal IM, Zhang M, Williams KN, Peloquin CA, Tyagi S, Vernon AA, et al. Daily dosing of rifapentine cures tuberculosis in three months or less in the murine model. PLoS Med. 2007;4(12):e344. Epub 2007/12/21.
3. Trajman A, Lapa ESJR, Dalcolmo M, Golub JE. Pulmonary tuberculosis. Pulm Med. 2013;2013:645747. Epub 2013/05/22.
4. Nuermberger EL, Yoshimatsu T, Tyagi S, O'Brien RJ, Vernon AN, Chaisson RE, et al. Moxifloxacin-containing regimen greatly reduces time to culture conversion in murine tuberculosis. Am J Respir Crit Care Med. 2004;169(3):421-6. Epub 2003/10/28.
5. Nuermberger EL, Yoshimatsu T, Tyagi S, Williams K, Rosenthal I, O'Brien RJ, et al. Moxifloxacin-containing regimens of reduced duration produce a stable cure in murine tuberculosis. Am J Respir Crit Care Med. 2004;170(10):1131-4. Epub 2004/08/13.
6. Rosenthal IM, Zhang M, Almeida D, Grosset JH, Nuermberger EL. Isoniazid or moxifloxacin in rifapentine-based regimens for experimental tuberculosis? Am J Respir Crit Care Med. 2008;178(9):989-93. Epub 2008/08/30.
7. Zhang M, Li SY, Rosenthal IM, Almeida DV, Ahmad Z, Converse PJ, et al. Treatment of tuberculosis with rifamycin-containing regimens in immune-deficient mice. Am J Respir Crit Care Med. 2011;183(9):1254-61. Epub 2011/02/19.
8. Munsiff SS, Kambili C, Ahuja SD. Rifapentine for the treatment of pulmonary tuberculosis. Clin Infect Dis Off Publ Infect Dis Soc Am. 2006;43(11):1468-75.
9. Dorman SE, Johnson JL, Goldberg S, Muzanye G, Padayatchi N, Bozeman L, et al. Substitution of moxifloxacin for isoniazid during intensive phase treatment of pulmonary tuberculosis. Am J Respir Crit Care Med. 2009;180(3):273-80. Epub 2009/05/02.
10. Dorman S, Goldberg S, Feng P, Heilig C, Stout JE, Schluger NW, et al. A Phase II study of a rifapentine-containing regimen for intensive phase treatment of pulmonary tuberculosis: preliminary results for tuberculosis trials consortium study 29. Am J Respir Crit Care Med. 2011;183:A6413.
11. Dutta NK, Illei PB, Peloquin CA, Pinn ML, Mdluli KE, Nuermberger EL, et al. Rifapentine is not more active than rifampin against chronic tuberculosis in guinea pigs. Antimicrob Agents Chemother. 2012;56(7):3726-31. Epub 2012/05/02.
12. Grosset J. Mycobacterium tuberculosis in the extracellular compartment: an underestimated adversary. Antimicrob Agents Chemother. 2003;47(3):833-6.
13. Hoff DR, Ryan GJ, Driver ER, Ssemakulu CC, De Groote MA, Basaraba RJ, et al. Location of intra- and extracellular M. tuberculosis populations in lungs of mice and guinea pigs during disease progression and after drug treatment. PloS One. 2011;6(3):e17550.
14. Rosenthal IM, Tasneen R, Peloquin CA, Zhang M, Almeida D, Mdluli KE, et al. Dose-ranging comparison of rifampin and rifapentine in two pathologically distinct murine models of tuberculosis. Antimicrob Agents Chemother. 2012;56(8):4331-40. Epub 2012/06/06.
15. Burman WJ, Gallicano K, Peloquin C. Comparative pharmacokinetics and pharmacodynamics of the rifamycin antibacterials. Clin Pharm. 2001;40(5):327-41. Epub 2001/07/04.
16. Mitchison DA. Development of rifapentine: the way ahead. Int J Tuberc Lung Dis Off J Int Union Against Tuberc Lung Dis. 1998;2(8):612-5. Epub 1998/08/26.
17. Rosenthal IM, Williams K, Tyagi S, Vernon AA, Peloquin CA, Bishai WR, et al. Weekly moxifloxacin and rifapentine is more active than the denver regimen in murine tuberculosis. Am J Respir Crit Care Med. 2005;172(11):1457-62. Epub 2005/09/06.
18. Sirgel FA, Fourie PB, Donald PR, Padayatchi N, Rustomjee R, Levin J, et al. The early bactericidal activities of rifampin and rifapentine in pulmonary tuberculosis. Am J Respir Crit Care Med. 2005;172(1):128-35.
19. Rosenthal IM, Tasneen R, Peloquin CA, Zhang M, Almeida D, Mdluli KE, et al. Dose-ranging comparison of rifampin and rifapentine in two pathologically distinct murine models of tuberculosis. Antimicrob Agents Chemother. 2012. Epub 2012/06/06.
20. Dooley KE, Bliven-Sizemore EE, Weiner M, Lu Y, Nuermberger EL, Hubbard WC, et al. Safety and pharmacokinetics of escalating daily doses of the antituberculosis drug rifapentine in healthy volunteers. Clin Pharm Ther. 2012;91(5):881-8.
21. Burman WJ, Goldberg S, Johnson JL, Muzanye G, Engle M, Mosher AW, et al. Moxifloxacin versus ethambutol in the first 2 months of treatment for pulmonary tuberculosis. Am J Respir Crit Care Med. 2006;174(3):331-8. Epub 2006/05/06.
22. Conde MB, Efron A, Loredo C, De Souza GR, Graca NP, Cezar MC, et al. Moxifloxacin versus ethambutol in the initial treatment of tuberculosis: a double-blind, randomised, controlled phase II trial. Lancet. 2009;373(9670):1183-9. Epub 2009/04/07.
23. Rustomjee R, Lienhardt C, Kanyok T, Davies GR, Levin J, Mthiyane T, et al. A Phase II study of the sterilising activities of ofloxacin, gatifloxacin and moxifloxacin in pulmonary tuberculosis. Int J Tuberc Lung Dis Off J Int Union Against Tuberc Lung Dis. 2008;12(2):128-38. Epub 2008/01/31.
24. Pletz MW, De Roux A, Roth A, Neumann KH, Mauch H, Lode H. Early bactericidal activity of moxifloxacin in treatment of pulmonary tuberculosis: a prospective, randomized study. Antimicrob Agents Chemother. 2004;48(3):780-2. Epub 2004/02/26.
25. Gosling RD, Uiso LO, Sam NE, Bongard E, Kanduma EG, Nyindo M, et al. The bactericidal activity of moxifloxacin in patients with pulmonary tuberculosis. Am J Respir Crit Care Med. 2003;168(11):1342-5. Epub 2003/08/15.
26. Fouad M, Gallagher JC. Moxifloxacin as an alternative or additive therapy for treatment of pulmonary tuberculosis. Annals Pharm. 2011;45(11):1439-44. Epub 2011/10/13.
27. Miyazaki E, Miyazaki M, Chen JM, Chaisson RE, Bishai WR. Moxifloxacin (BAY12-8039), a new 8-methoxyquinolone, is active in a mouse model of tuberculosis. Antimicrob Agents Chemother. 1999;43(1):85-9. Epub 1998/12/31.
28. Chan CY, Au-Yeang C, Yew WW, Leung CC, Cheng AF. In vitro postantibiotic effects of rifapentine, isoniazid, and moxifloxacin against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2004;48(1):340-3. Epub 2003/12/25.
29. Drusano GL, Sgambati N, Eichas A, Brown DL, Kulawy R, Louie A. The combination of rifampin plus moxifloxacin is synergistic for suppression of resistance but antagonistic for cell kill of Mycobacterium tuberculosis as determined in a hollow-fiber infection model. MBio. 2010;1(3). Epub 2010/08/31.
30. Balasubramanian V, Solapure S, Gaonkar S, Mahesh Kumar KN, Shandil RK, Deshpande A, et al. Effect of coadministration of moxifloxacin and rifampin on Mycobacterium tuberculosis in a murine aerosol infection model. Antimicrob Agents Chemother. 2012;56(6):3054-7. Epub 2012/04/04.
31. Almeida D, Nuermberger E, Tasneen R, Rosenthal I, Tyagi S, Williams K, et al. Paradoxical effect of isoniazid on the activity of rifampin-pyrazinamide combination in a mouse model of tuberculosis. Antimicrob Agents Chemother. 2009;53(10):4178-84. Epub 2009/07/22.
32. Grosset J, Truffot-Pernot C, Lacroix C, Ji B. Antagonism between isoniazid and the combination pyrazinamide-rifampin against tuberculosis infection in mice. Antimicrob Agents Chemother. 1992;36(3):548-51. Epub 1992/03/01.
33. Zvada SP, Denti P, Geldenhuys H, Meredith S, van As D, Hatherill M, et al. Moxifloxacin population pharmacokinetics in patients with pulmonary tuberculosis and the effect of intermittent high-dose rifapentine. Antimicrob Agents Chemother. 2012;56(8):4471-3. Epub 2012/05/16.
34. Gumbo T, Louie A, Deziel MR, Parsons LM, Salfinger M, Drusano GL. Selection of a moxifloxacin dose that suppresses drug resistance in Mycobacterium tuberculosis, by use of an in vitro pharmacodynamic infection model and mathematical modeling. J Infect Dis. 2004;190(9):1642-51. Epub 2004/10/13.
35. Chang K-C, Dheda K. Rationalizing use of fluoroquinolones and pyrazinamide in the battle against multidrug-resistant tuberculosis. Am J Respir Crit Care Med. 2013;188(1):10-1.
36. Ahmad Z, Fraig MM, Bisson GP, Nuermberger EL, Grosset JH, Karakousis PC. Dose-dependent activity of pyrazinamide in animal models of intracellular and extracellular tuberculosis infections. Antimicrob Agents Chemother. 2011;55(4):1527-32.
37. Mitchison DA, Fourie PB. The near future: improving the activity of rifamycins and pyrazinamide. Tuberculosis (Edinb). 2010;90(3):177-81.
38. Gumbo T, Dona CS, Meek C, Leff R. Pharmacokinetics-pharmacodynamics of pyrazinamide in a novel in vitro model of tuberculosis for sterilizing effect: a paradigm for faster assessment of new antituberculosis drugs. Antimicrob Agents Chemother. 2009;53(8):3197-204.
39. Pasipanodya JG, Gumbo T. Clinical and toxicodynamic evidence that high-dose pyrazinamide is not more hepatotoxic than the low doses currently used. Antimicrob Agents Chemother. 2010;54(7):2847-54. Epub 2010/05/05.
40. Pham DD, Fattal E, Ghermani N, Guiblin N, Tsapis N. Formulation of pyrazinamide-loaded large porous particles for the pulmonary route: avoiding crystal growth using excipients. Int J Pharm. 2013;454(2):668-77. Epub 2013/04/23.
41. Sosnik A, Carcaboso AM, Glisoni RJ, Moretton MA, Chiappetta DA. New old challenges in tuberculosis: potentially effective nanotechnologies in drug delivery. Adv Drug Deliv Rev. 2010;62(4-5):547-59. Epub 2009/11/17.
42. Xie Y, Zeng P, Wiedmann TS. Disease guided optimization of the respiratory delivery of microparticulate formulations. Expert Opin Drug Deliv. 2008;5(3):269-89. Epub 2008/03/06.
43. Yadav AB, Sharma R, Muttil P, Singh AK, Verma RK, Mohan M, et al. Inhalable microparticles containing isoniazid and rifabutin target macrophages and 'stimulate the phagocyte' to achieve high efficacy. Indian J Exp Biol. 2009;47(6):469-74. Epub 2009/07/29.
44. Sharma R, Saxena D, Dwivedi AK, Misra A. Inhalable microparticles containing drug combinations to target alveolar macrophages for treatment of pulmonary tuberculosis. Pharm Res. 2001;18(10):1405-10. Epub 2001/11/08.
45. Son YJ, McConville JT. A new respirable form of rifampicin. Eur J Pharm Biopharm Off J Arb Pharm Verfahr eV. 2011;78(3):366-76. Epub 2011/02/18.
46. Sung JC, Garcia-Contreras L, Verberkmoes JL, Peloquin CA, Elbert KJ, Hickey AJ, et al. Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. Antimicrob Agents Chemother. 2009;53(4):1338-43. Epub 2009/01/14.
47. Coowanitwong I, Arya V, Kulvanich P, Hochhaus G. Slow release formulations of inhaled rifampin. AAPS J. 2008;10(2):342-8. Epub 2008/06/28.
48. Kumar Verma R, Mukker JK, Singh RS, Kumar K, Verma PR, Misra A. Partial biodistribution and pharmacokinetics of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to rhesus macaques. Mol Pharm. 2012;9(4):1011-6. Epub 2012/03/09.
49. Muttil P, Kaur J, Kumar K, Yadav AB, Sharma R, Misra A. Inhalable microparticles containing large payload of anti-tuberculosis drugs. Eur J Pharm Sci. 2007;32(2):140-50. Epub 2007/08/08.
50. Son YJ, McConville JT. Preparation of sustained release rifampicin microparticles for inhalation. J Pharm Pharmacol. 2012;64(9):1291-302.
51. Suarez S, O'Hara P, Kazantseva M, Newcomer CE, Hopfer R, McMurray DN, et al. Respirable PLGA microspheres containing rifampicin for the treatment of tuberculosis: screening in an infectious disease model. Pharm Res. 2001;18(9):1315-9. Epub 2001/10/31.
52. Verma RK, Kaur J, Kumar K, Yadav AB, Misra A. Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice. Antimicrob Agents Chemother. 2008;52(9):3195-201. Epub 2008/07/02.
53. Fiegel J, Garcia-Contreras L, Thomas M, VerBerkmoes J, Elbert K, Hickey A, et al. Preparation and in vivo evaluation of a dry powder for inhalation of capreomycin. Pharm Res. 2008;25(4):805-11. Epub 2007/07/28.
54. Garcia-Contreras L, Fiegel J, Telko MJ, Elbert K, Hawi A, Thomas M, et al. Inhaled large porous particles of capreomycin for treatment of tuberculosis in a guinea pig model. Antimicrob Agents Chemother. 2007;51(8):2830-6. Epub 2007/05/23.
55. Tsapis N, Bennett D, O'Driscoll K, Shea K, Lipp MM, Fu K, et al. Direct lung delivery of para-aminosalicylic acid by aerosol particles. Tuberculosis (Edinb). 2003;83(6):379-85. Epub 2003/11/19.
56. Chan JG, Chan HK, Prestidge CA, Denman JA, Young PM, Traini D. A novel dry powder inhalable formulation incorporating three first-line anti-tubercular antibiotics. Eur J Pharm Biopharm Off J Arb Pharm Verfahr eV. 2012;83(2):285-92. Epub 2012/09/18.
57. Prasad B, Bhutani H, Singh S. Study of the interaction between rifapentine and isoniazid under acid conditions. J Pharm Biomed Anal. 2006;41(4):1438-41. Epub 2006/04/20.
58. Bhutani H, Singh S, Jindal KC, Chakraborti AK. Mechanistic explanation to the catalysis by pyrazinamide and ethambutol of reaction between rifampicin and isoniazid in anti-TB FDCs. J Pharm Biomed Anal. 2005;39(5):892-9. Epub 2005/06/28.
59. Chew NY, Chan HK. In vitro aerosol performance and dose uniformity between the Foradile Aerolizer and the Oxis Turbuhaler. J Aerosol Med Off J Inter Soc Aerosols Med. 2001;14(4):495-501.
60. Taneja NK, Tyagi JS. Resazurin reduction assays for screening of anti-tubercular compounds against dormant and actively growing Mycobacterium tuberculosis, Mycobacterium bovis BCG and Mycobacterium smegmatis. J Antimicrob Chemother. 2007;60(2):288-93.
61. Collins L, Franzblau SG. Microplate alamar blue assay versus BACTEC 460 system for high-throughput screening of compounds against Mycobacterium tuberculosis and Mycobacterium avium. Antimicrob Agents Chemother. 1997;41(5):1004-9.
62. Cherukuvada S, Thakuria R, Nangia A. Pyrazinamide polymorphs: relative stability and vibrational spectroscopy. Cryst Growth Des. 2010;10(9):3931-41.
63. Gervelas C, Serandour AL, Geiger S, Grillon G, Fritsch P, Taulelle C, et al. Direct lung delivery of a dry powder formulation of DTPA with improved aerosolization properties: effect on lung and systemic decorporation of plutonium. J Control Release Off J Control Release Soc. 2007;118(1):78-86.
64. Boraey MA, Hoe S, Sharif H, Miller DP, Lechuga-Ballesteros D, Vehring R. Improvement of the dispersibility of spray-dried budesonide powders using leucine in an ethanol-water cosolvent system. Powder Technol. 2013;236:171-8.
65. Dharmadhikari AS, Kabadi M, Gerety B, Hickey AJ, Fourie PB, Nardell E. Phase I, single-dose, dose-escalating study of inhaled dry powder capreomycin: a new approach to therapy of drug-resistant tuberculosis. Antimicrob Agents Chemother. 2013;57(6):2613-9.
66. Learoyd TP, Burrows JL, French E, Seville PC. Sustained delivery by leucine-modified chitosan spray-dried respirable powders. Int J Pharm. 2009;372(1-2):97-104.
67. Nuermberger EL, Rosenthal IM, Tasneen R, Peloquin CA, Mdluli KE, Karakousis PC, et al. Reply to "Contradictory results with high-dosage rifamycin in mice and humans". Antimicrob Agents Chemother. 2013;57(2):1104-5.
68. van Ingen J, Aarnoutse RE, Donald PR, Diacon AH, Dawson R, van Balen Plemper G, et al. Why do we use 600 mg of rifampicin in tuberculosis treatment? Clin Infect Dis Off Publ Infect Dis Soc Am. 2011;52(9):e194-9.
69. Burhan E, Ruesen C, Ruslami R, Ginanjar A, Mangunnegoro H, Ascobat P, et al. Isoniazid, rifampin, and pyrazinamide plasma concentrations in relation to treatment response in indonesian pulmonary tuberculosis patients. Antimicrob Agents Chemother. 2013;57(8):3614-9.
70. Management of MDR-TB: A field guide. Geneva: WHO Press; 2009.
71. Mendel C, Springsklee M. Moxifloxacin for tuberculosis. Lancet Infect Dis. 2012;12(3):176-7. author reply 7-8. Epub 2012/03/01.
72. Zhang Y, Permar S, Sun Z. Conditions that may affect the results of susceptibility testing of Mycobacterium tuberculosis to pyrazinamide. J Med Microbiol. 2002;51(1):42-9.
73. Drlica K, Zhao X, Kreiswirth B. Minimising moxifloxacin resistance with tuberculosis. Lancet Infect Dis. 2008;8(5):273-5. Epub 2008/05/13.
74. Mitnick CD, McGee B, Peloquin CA. Tuberculosis pharmacotherapy: strategies to optimize patient care. Expert Opin Pharmacother. 2009;10(3):381-401. Epub 2009/02/05.
75. Arbex MA, Varella Mde C, Siqueira HR, Mello FA. Antituberculosis drugs: drug interactions, adverse effects, and use in special situations. Part 1: first-line drugs. J Bras Pneumol Publ Off Soc Bras Pneumol Tisil. 2010;36(5):626-40.
76. Ohtake S, Shalaev E. Effect of water on the chemical stability of amorphous pharmaceuticals: I. Small molecules. J Pharm Sci. 2013;102(4):1139-54. Epub 2013/02/02.