Pharmacokinetics and pharmacodynamics of clofazimine in a mouse model of tuberculosis

Antimicrobial Agents and Chemotherapy

Volumn 59, Issue 6, 2015, Pages 3042-3051

  Swanson, Rosemary V ^a,b   Adamson, John ^a   Moodley, Chivonne ^a   Ngcobo, Bongani ^a   Ammerman, Nicole C ^a,c   Dorasamy, Afton ^a   Moodley, Sashen ^a   Mgaga, Zinhle ^a   Tapley, Asa ^a,d,e   Bester, Linda A ^f   Singh, Sanil ^f   Grosset, Jacques H ^a,c   Almeida, Deepak V ^a,c  

^a UNIVERSITY OF KWAZULU NATAL   (South Africa)

^b UNIVERSITY OF KWAZULU NATAL   (South Africa)

^c JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE   (United States)

^d UNIVERSITY OF CALIFORNIA   (United States)

^e HOWARD HUGHES MEDICAL INSTITUTE   (United States)

^f UNIVERSITY OF KWAZULU NATAL   (South Africa)

Author keywords

[No Author keywords available]

Indexed keywords

CLOFAZIMINE; PROTEIN BINDING; TUBERCULOSTATIC AGENT;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BACTERICIDAL ACTIVITY; BODY WEIGHT; CONTROLLED STUDY; DRUG SCREENING; MINIMUM INHIBITORY CONCENTRATION; MOUSE; MYCOBACTERIUM TUBERCULOSIS; NONHUMAN; PHARMACODYNAMICS; PHARMACOLOGICAL PARAMETERS; PLASMA PROTEIN BINDING; PRIORITY JOURNAL; TUBERCULOSIS; ANIMAL; BAGG ALBINO MOUSE; BLOOD; FEMALE; LIQUID CHROMATOGRAPHY; MASS SPECTROMETRY;

ANIMALS; ANTITUBERCULAR AGENTS; CHROMATOGRAPHY, LIQUID; CLOFAZIMINE; FEMALE; MASS SPECTROMETRY; MICE; MICE, INBRED BALB C; PROTEIN BINDING; TUBERCULOSIS;

EID: 84929587393     PISSN: 00664804     EISSN: 10986596     Source Type: Journal    
DOI: 10.1128/AAC.00260-15     Document Type: Article

References (37)

1. Barry VC, Conalty ML, Gaffney EE. 1956. Antituberculosis activity in the phenazine series; isomeric pigments obtained by oxidation of o-phenylenediamine derivatives. J Pharm Pharmacol 8:1089-1096. http://dx.doi.org/10.1111/j.2042-7158.1956.tb12238.x.
2. Barry VC, Belton JG, Conalty ML, Denneny JM, Edward DW, O'Sullivan JF, Twomey D, Winder F. 1957. A new series of phenazines (rimino-compounds) with high antituberculosis activity. Nature 179: 1013-1015. http://dx.doi.org/10.1038/1791013a0.
3. World Health Organization. 2004. Multidrug therapy against leprosy: development and implementation over the past 25 years. WHO, Geneva, Switzerland.
4. World Health Organization. 2012. WHO Expert Committee on Leprosy. World Health Organ Tech Rep Ser 968:1-61.
5. Van Deun A, Maug AK, Salim MA, Das PK, Sarker MR, Daru P, Rieder HL. 2010. Short, highly effective, and inexpensive standardized treatment of multidrug-resistant tuberculosis. Am J Respir Crit Care Med 182:684-692. http://dx.doi.org/10.1164/rccm.201001-0077OC.
6. World Health Organization. 2013. Shorter treatment regimens for multidrug-resistant tuberculosis (MDR-TB). WHO, Geneva, Switzerland.
7. World Health Organization. 2011. Guidelines for the programmatic management of drug-resistant tuberculosis. 2011 update. WHO, Geneva, Switzerland.
8. Grosset JH, Tyagi S, Almeida DV, Converse PJ, Li SY, Ammerman NC, Bishai WR, Enarson D, Trébucq A. 2013. Assessment of clofazimine activity in a second-line regimen for tuberculosis in mice. Am J Respir Crit Care Med 188:608-612. http://dx.doi.org/10.1164/rccm.201304-0753OC.
9. Tyagi S, Ammerman NC, Li SY, Adamson J, Converse PJ, Swanson RV, Almeida DV, Grosset JH. 2015. Clofazimine shortens the duration of the first-line treatment regimen for experimental chemotherapy of tuberculosis. Proc Natl Acad Sci U S A 112:869-874. http://dx.doi.org/10.1073/pnas.1416951112.
10. Chang YT. 1955. Chemotherapy of murine leprosy. IV. The effects of amithiozone (TB1/698), p-aminosalicylic acid (PAS), B 283 (a phenazine pigment), five antibiotics and three diphenylthiourea compounds on mouse leprosy. Int J Lepr 23:167-180.
11. Levy L. 1974. Pharmacologic studies of clofazimine. Am J Trop Med Hyg 23:1097-1109.
12. Mansfield RE. 1974. Tissue concentrations of clofazimine (B663) in man. Am J Trop Med Hyg 23:1116-1119.
13. Grosset J, Ji B. 1998. Experimental chemotherapy of mycobacterial diseases, p 51-97. In Gangadharam PRJ, Jenkins PA (ed), Mycobacteria, vol II: chemotherapy. Chapman & Hall, New York, NY.
14. Grosset J, Almeida D, Converse PJ, Tyagi S, Li SY, Ammerman NC, Pym AS, Wallengren K, Hafner R, Lalloo U, Swindells S, Bishai WR. 2012. Modeling early bactericidal activity in murine tuberculosis provides insights into the activity of isoniazid and pyrazinamide. Proc Natl Acad Sci USA109:15001-15005. http://dx.doi.org/10.1073/pnas.1203636109.
15. Herrera AM, Scott DO, Lunte CE. 1990. Microdialysis sampling for determination of plasma protein binding of drugs. Pharm Res 7:1077-1081. http://dx.doi.org/10.1023/A:1015955503708.
16. Burman WJ, Gallicano K, Peloquin C. 2001. Comparative pharmacokinetics and pharmacodynamics of the rifamycin antibacterials. Clin Pharmacokinet 40:327-341. http://dx.doi.org/10.2165/00003088-200140050-00002.
17. Banerjee DK, Ellard GA, Gammon PT, Waters MF. 1974. Some observations on the pharmacology of clofazimine (B663). Am J Trop Med Hyg 23:1110-1115.
18. Williams K, Minkowski A, Amoabeng O, Peloquin CA, Taylor D, Andries K, Wallis RS, Mdluli KE, Nuermberger EL. 2012. Sterilizing activities of novel combinations lacking first- and second-line drugs in a murine model of tuberculosis. Antimicrob Agents Chemother 56:3114-3120. http://dx.doi.org/10.1128/AAC.00384-12.
19. Irwin SM, Gruppo V, Brooks E, Gilliland J, Scherman M, Reichlen MJ, Leistikow R, Kramnik I, Nuermberger EL, Voskuil MI, Lenaerts AJ. 2014. Limited activity of clofazimine as a single drug in a mouse model of tuberculosis exhibiting caseous necrotic granulomas. Antimicrob Agents Chemother 58:4026-4034. http://dx.doi.org/10.1128/AAC.02565-14.
20. Baik J, Rosania GR. 2012. Macrophages sequester clofazimine in an intracellular liquid crystal-like supramolecular organization. PLoS One 7:e47494. http://dx.doi.org/10.1371/journal.pone.0047494.
21. McDougall AC. 1974. Electron microscope studies of the antileprosy drug B663 (clofazimine; Lamprene). Int J Lepr Other Mycobact Dis 42:1-12.
22. Conalty ML, Barry VC, Jina A. 1971. The antileprosy agent B.663 (Clofazimine) and the reticuloendothelial system. Int J Lepr Other Mycobact Dis 39:479-492.
23. Tasneen R, Li SY, Peloquin CA, Taylor D, Williams KN, Andries K, Mdluli KE, Nuermberger EL. 2011. Sterilizing activity of novel TMC207-and PA-824-containing regimens in a murine model of tuberculosis. Antimicrob Agents Chemother 55:5485-5492. http://dx.doi.org/10.1128/AAC.05293-11.
24. Yano T, Kassovska-Bratinova S, Teh JS, Winkler J, Sullivan K, Isaacs A, Schechter NM, Rubin H. 2011. Reduction of clofazimine by mycobacterial type 2 NADH:quinone oxidoreductase: a pathway for the generation of bactericidal levels of reactive oxygen species. J Biol Chem 286:10276-10287. http://dx.doi.org/10.1074/jbc.M110.200501.
25. Baik J, Stringer KA, Mane G, Rosania GR. 2013. Multiscale distribution and bioaccumulation analysis of clofazimine reveals a massive immune system-mediated xenobiotic sequestration response. Antimicrob Agents Chemother 57:1218-1230. http://dx.doi.org/10.1128/AAC.01731-12.
26. Diacon AH, Dawson R, von Groote-Bidlingmaier F, Symons G, Venter A, Donald PR, van Niekerk C, Everitt D, Hutchings J, Burger DA, Schall R, Mendel CM. 26 January 2015. Bactericidal activity of pyrazinamide and clofazimine alone and in combinations with pretomanid and bedaquiline. Am J Respir Crit Care Med http://dx.doi.org/10.1164/rccm.201410-1801OC.
27. Barry VC. 1969. Synthetic phenazine derivatives and mycobacterial disease: a twenty year investigation. Boyle Medal Lecture no. 16. Sci Proc R Dublin Soc Ser A 3:153-170.
28. Harper J, Skerry C, Davis SL, Tasneen R, Weir M, Kramnik I, Bishai WR, Pomper MG, Nuermberger EL, Jain SK. 2012. Mouse model of necrotic tuberculosis granulomas develops hypoxic lesions. J Infect Dis 205:595-602. http://dx.doi.org/10.1093/infdis/jir786.
29. Pan H, Yan BS, Rojas M, Shebzukhov YV, Zhou H, Kobzik L, Higgins DE, Daly MJ, Bloom BR, Kramnik I. 2005. Ipr1 gene mediates innate immunity to tuberculosis. Nature 434:767-772. http://dx.doi.org/10.1038/nature03419.
30. Janssen Therapeutics Division, Janssen Products LP. 2013. Sirturo (bedaquiline) 100 mg tablets full prescribing information. Reference ID 3644668. Revised 2014. Janssen Therapeutics, Titusville, NJ.
31. Rouan MC, Lounis N, Gevers T, Dillen L, Gilissen R, Raoof A, Andries K. 2012. Pharmacokinetics and pharmacodynamics of TMC207 and its N-desmethyl metabolite in a murine model of tuberculosis. Antimicrob Agents Chemother 56:1444-1451. http://dx.doi.org/10.1128/AAC.00720-11.
32. Rustomjee R, Diacon AH, Allen J, Venter A, Reddy C, Patientia RF, Mthiyane TC, De Marez T, van Heeswijk R, Kerstens R, Koul A, De Beule K, Donald PR, McNeeley DF. 2008. Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis. Antimicrob Agents Chemother 52:2831-2835. http: //dx.doi.org/10.1128/AAC.01204-07.
33. Koul A, Vranckx L, Dhar N, Göhlmann HWH, Özdemir E, Neefs JM, Schulz M, Lu P, Mørtz E, McKinney JD, Andries K, Bald D. 2014. Delayed bactericidal response of Mycobacterium tuberculosis to bedaquiline involves remodelling of bacterial metabolism. Nat Commun 5:3369. http://dx.doi.org/10.1038/ncomms4369.
34. Dhillon J, Andries K, Phillips PP, Mitchison DA. 2010. Bactericidal activity of the diarylquinoline TMC207 against Mycobacterium tuberculosis outside and within cells. Tuberculosis 90:301-305. http://dx.doi.org/10.1016/j.tube.2010.07.004.
35. Diacon AH, Dawson R, Von Groote-Bidlingmaier F, Symons G, Venter A, Donald PR, Conradie A, Erondu N, Ginsberg AM, Egizi E, Winter H, Becker P, Mendel CM. 2013. Randomized dose-ranging study of the 14-day early bactericidal activity of bedaquiline (TMC207) in patients with sputum microscopy smear-positive pulmonary tuberculosis. Antimicrob Agents Chemother 57:2199-2203. http://dx.doi.org/10.1128/AAC.02243-12.
36. Andries K, Verhasselt P, Guillemont J, Gohlmann HW, Neefs JM, Winkler H, Van Gestel J, Timmerman P, Zhu M, Lee E, Williams P, de Chaffoy D, Huitric E, Hoffner S, Cambau E, Truffot-Pernot C, Lounis N, Jarlier V. 2005. A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis. Science 307:223-227. http://dx.doi.org/10.1126/science.1106753.
37. Hartkoorn RC, Uplekar S, Cole ST. 2014. Cross-resistance between clofazimine and bedaquiline through upregulation of MmpL5 in Mycobacterium tuberculosis. Antimicrob Agents Chemother 58:2979-2981. http://dx.doi.org/10.1128/AAC.00037-14.