Pipeline of drugs for related diseases: Tuberculosis

Current Opinion in HIV and AIDS

Volumn 8, Issue 6, 2013, Pages 579-585

  Dooley, Kelly E ^a   Nuermberger, Eric L ^a   Diacon, Andreas H ^b  

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

^b STELLENBOSCH UNIVERSITY   (South Africa)

Author keywords

bedaquiline; fluoroquinolone; HIV; investigational drugs; multidrug resistant tuberculosis; nitroimidazole; oxazolidinone; rifamycin; tuberculosis

Indexed keywords

6,7 DIHYDRO 2 NITRO 6 (4 TRIFLUOROMETHOXYBENZYLOXY) 5H IMIDAZO[2,1 B][1,3]OXAZINE; AZD 5847; BEDAQUILINE; CLOFAZIMINE; DELAMANID; ETHAMBUTOL; ISONIAZID; LINEZOLID; MOXIFLOXACIN; N (2 ADAMANTYL) N' GERANYLETHYLENEDIAMINE; NITROIMIDAZOLE; NITROIMIDAZOLE DERIVATIVE; OXAZOLIDINONE DERIVATIVE; PLACEBO; QUINOLONE DERIVATIVE; RIFAMPICIN; RIFAPENTINE; SUTEZOLID; UNCLASSIFIED DRUG;

ANTIBIOTIC SENSITIVITY; CLINICAL TRIAL; HUMAN; MULTIDRUG RESISTANCE; NONHUMAN; PRIORITY JOURNAL; REVIEW; SPUTUM CULTURE; TREATMENT DURATION; TUBERCULOSIS;

ANTITUBERCULAR AGENTS; CLINICAL TRIALS AS TOPIC; DRUG DISCOVERY; DRUG THERAPY, COMBINATION; HUMANS; TUBERCULOSIS;

EID: 84886095875     PISSN: 1746630X     EISSN: 17466318     Source Type: Journal    
DOI: 10.1097/COH.0000000000000009     Document Type: Review

References (65)

1. World Health Organization. Global tuberculosis report 2012 WHO/ HTM/TB/2012. 6. http://apps.who.int/iris/bitstream/10665/75938/1/ 9789241564502-eng.pdf [Accessed 26 March 2013]
2. World Health Organization. Global tuberculosis control: WHO report 2011. WHO/HTM/TB/2011.16. 2011. http://www.who.int/tb/publications/global- report/2011/gtbr11-full.pdf
3. UNAIDS. Global report fact sheet 2010, the global AIDS epidemic. http:// www.unaids.org/en/media/unaids/contentassets/documents/factsheet/ 2010/20101123-FS-Global-em-en.pdf [Accessed 20 January 2012]
4. American Thoracic Society. Targeted tuberculin testing and treatment of latent tuberculosis infection. MMWR Recomm Rep 2000; 49 (RR-6): 1-51.
5. Sterling TR, Villarino ME, Borisov AS, et al. Three months of rifapentine and isoniazid for latent tuberculosis infection. N Engl J Med 2011; 365:2155-2166.
6. Klopper M, Warren RM, Hayes C, et al. Emergence and spread of extensively and totally drug-resistant tuberculosis, South Africa. Emerg Infect Dis 2013; 19:449-455.
7. Slomski A. South Africa warns of emergence of totally drug-resistant tuberculosis. JAMA 2013; 309:1097-1098.
8. Loewenberg S. India reports cases of totally drug-resistant tuberculosis. Lancet 2012; 379:205.
9. Udwadia ZF, Amale RA, Ajbani KK, Rodrigues C. Totally drug-resistant tuberculosis in India. Clin Infect Dis 2012; 54:579-581.
10. World Health Organization. Multidrug-resistant tuberculosis (MDR-TB) [Update]. 2013; http://www.who.int/tb/challenges/mdr/MDR-TB-Fact- Sheet.pdf [accessed 28 June 2013] 11.
11. World Health Organization. Guidelines for the programmatic management of drug-resistant tuberculosis [Update]. Geneva: WHO 2011 http://www.who.int/tb/ challenges/mdr/programmatic-guidelines-for-mdrtb/en/index. html [Accessed 29 July 2013]
12. Andries K, Verhasselt P, Guillemont J, et al. A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis. Science 2005 307 223-227.
13. Nunn AJ, Phillips PP, Mitchison DA. Timing of relapse in short-course chemotherapy trials for tuberculosis. Int J Tuberc Lung Dis 2010; 14:241-242.
14. Jayaram R, Gaonkar S, Kaur P, et al. Pharmacokinetics-pharmacodynamics of rifampin in an aerosol infection model of tuberculosis. Antimicrob Agents Chemother 2003; 47:2118-2124.
15. Diacon AH, Patientia RF, Venter A, et al. Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears. Antimicrob Agents Chemother 2007; 51:2994-2996.
16. Boeree MJ, Plemper van Balen G, Aarnoutse RA. High-dose rifampicin: how do we proceed? Int J Tuberc Lung Dis 2011; 15:1133.
17. Boeree M, Diacon A, Dawson R, et al. What is the right dose of rifampin? 20th Conference on Retroviruses and Opportunistic Infections [Paper 148LB, Abstract 128]. Atlanta, Georgia. 2013.
18. Rosenthal IM, Zhang M, Williams KN, et al. Daily dosing of rifapentine cures tuberculosis in three months or less in the murine model. PLoS Med 2007; 4:e344.
19. Dorman SE, Goldberg S, Stout JE, et al. Substitution of rifapentine for rifampin during intensive phase treatment of pulmonary tuberculosis: study 29 of the tuberculosis trials consortium. J Infect Dis 2012; 206:1030-1040.
20. Dorman SE and the CDC TB Trials Consortium. Antimicrobial activity and safety of high-dose rifapentine-containing regimens for treatment of pulmonary TB: study 29X of the CDC Tuberculosis Trials Consortium. In: Annual Meeting of the American Thoracic Society; 18 May 2013; Philadelphia, PA.
21. Nuermberger EL, Yoshimatsu T, Tyagi S, et al. Moxifloxacin-containing regimen greatly reduces time to culture conversion in murine tuberculosis. Am J Respir Crit Care Med 2004; 169:421-426.
22. Dorman SE, Johnson JL, Goldberg S, et al. Substitution of moxifloxacin for isoniazid during intensive phase treatment of pulmonary tuberculosis. Am J Respir Crit Care Med 2009; 180:273-280.
23. Conde MB, Efron A, Loredo C, et al. Moxifloxacin versus ethambutol in the initial treatment of tuberculosis: a double-blind, randomised, controlled phase II trial. Lancet 2009; 373:1183-1189.
24. Rustomjee R, Lienhardt C, Kanyok T, et al. A Phase II study of the sterilising activities of ofloxacin, gatifloxacin and moxifloxacin in pulmonary tuberculosis. Int J Tuberc Lung Dis 2008; 12:128-138.
25. Jindani A, Hatherall M, Charalambous S, et al. A multicentre randomized clinical trial to evaluate high-dose rifapentine with a quinolone for treatment of pulmonary TB: The RIFAQUIN Trial. In: 20th Conference on Retroviruses and Opportunistic Infections; 3-6 March 2013; Atlanta, GA. [Oral abstract and paper 147LB].
26. Jawahar MS, Banurekha VV, Paramasivan CN, et al. Randomized clinical trial of thrice-weekly 4-month moxifloxacin or gatifloxacin containing regimens in the treatment of new sputum positive pulmonary tuberculosis patients. PLoS One 2013; 8:e67030.
27. Koul A, Dendouga N, Vergauwen K, et al. Diarylquinolines target subunit c of mycobacterial ATP synthase. Nat Chem Biol 2007; 3:323-324.
28. Tasneen R, Li SY, Peloquin CA, et al. Sterilizing activity of novel TMC207- and PA-824-containing regimens in a murine model of tuberculosis. Antimicrob Agents Chemother 2011; 55:5485-5492.
29. Williams K, Minkowski A, Amoabeng O, et al. Sterilizing activities of novel combinations lacking first- and second-line drugs in a murine model of tuberculosis. Antimicrob Agents Chemother 2012; 56:3114-3120.
30. Diacon AH, Pym A, Grobusch M, et al. The diarylquinoline TMC207 for multidrug-resistant tuberculosis. N Engl J Med 2009; 360:2397-2405. Currently available clinical trial results of Bedaquiline, the first novel anti-TB drug licensed in over 40 years.
31. Diacon AH, Donald PR, Pym A, et al. Randomized pilot trial of eight weeks of bedaquiline (TMC207) treatment for multidrug-resistant tuberculosis: longterm outcome, tolerability, and effect on emergence of drug resistance. Antimicrob Agents Chemother 2012; 56:3271-3276.
32. Sirturo package insert. Janssen Products, LP. http://www.who.int/tb/ challenges/ mdr/Package-insert-bedaquiline.pdf. [accessed 28 June 2013]
33. World Health Organization. The use of bedaquiline in the treatment of multidrugresistant tuberculosis: Interim policy guidance. WHO/HTM/TB/2013.6. 2013. http://apps.who.int/iris/bitstream/10665/84879/1/9789241505482-eng. pdf. [accessed 28 June 2013]
34. Stover CK, Warrener P, VanDevanter DR, et al. A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. Nature 2000; 405:962-966.
35. Singh R, Manjunatha U, Boshoff HI, et al. PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. Science 2008; 322:1392-1395.
36. Dutta NK, Alsultan A, Gniadek TJ, et al. Potent rifamycin-sparing regimen cures Guinea pig tuberculosis as rapidly as the standard regimen. Antimicrob Agents Chemother 2013; 57:3910-3916.
37. Nuermberger E, Tyagi S, Tasneen R, et al. Powerful bactericidal and sterilizing activity of a regimen containing PA-824, moxifloxacin, and pyrazinamide in a murine model of tuberculosis. Antimicrob Agents Chemother 2008; 52:1522-1524.
38. Matsumoto M, Hashizume H, Tomishige T, et al. OPC-67683, a nitro-dihydroimidazooxazole derivative with promising action against tuberculosis in vitro and in mice. PLoS Med 2006; 3:e466.
39. Gler MT, Skripconoka V, Sanchez-Garavito E, et al. Delamanid for multidrug-resistant pulmonary tuberculosis. N Engl J Med 2012; 366:2151-2160.
40. Skripconoka V, Danilovits M, Pehme L, et al. Delamanid improves outcomes and reduces mortality for multidrug-resistant tuberculosis. Eur Respir J 2013; 41:1393-1400.
41. European Medicines Agency. Delamanid. http://www.ema.europa.eu/ema/ index.jsp?curlpages/medicines/human/medicines/002552/smops/Nega tive/human-smop-000572.jsp&midWC0b01ac058001d127 [Accessed 3 August 2013].
42. Diacon AH, Dawson R, Hanekom M, et al. Early bactericidal activity and pharmacokinetics of PA-824 in smear-positive tuberculosis patients. Antimicrob Agents Chemother 2010; 54:3402-3407.
43. Diacon AH, Dawson R, du Bois J, et al. Phase II dose-ranging trial of the early bactericidal activity of PA-824. Antimicrob Agents Chemother 2012; 56:3027-3031.
44. Diacon AH, Dawson R, von Groote-Bidlingmaier F, et al. 14-day bactericidal activity of PA-824, bedaquiline, pyrazinamide, and moxifloxacin combinations: a randomised trial. Lancet 2012; 380:986-993.
45. Carroll MW, Jeon D, Mountz JM, et al. Efficacy and safety of metronidazole for pulmonary multidrug-resistant tuberculosis. Antimicrob Agents Chemother 2013; 57:3903-3909.
46. Barbachyn MR, Hutchinson DK, Brickner SJ, et al. Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity. J Med Chem 1996; 39:680-685.
47. Wallis RS, Jakubiec W, Kumar V, et al. Biomarker-assisted dose selection for safety and efficacy in early development of PNU-100480 for tuberculosis. Antimicrob Agents Chemother 2011; 55:567-574.
48. Williams KN, Stover CK, Zhu T, et al. Promising antituberculosis activity of the oxazolidinone PNU-100480 relative to that of linezolid in a murine model. Antimicrob Agents Chemother 2009; 53:1314-1319.
49. Wallis RS, Jakubiec WM, Kumar V, et al. Pharmacokinetics and wholeblood bactericidal activity against Mycobacterium tuberculosis of single doses of PNU-100480 in healthy volunteers. J Infect Dis 2010; 202:745-751.
50. Wallis RS, Diacon AH, Dawson R, et al. Safety, tolerability and early bactericidal activity in sputum of PNU-100480 (sutezolid) in patients with pulmonary tuberculosis. In: XIX International AIDS Conference; 22-27 July 2012, Washington, DC; 2012. [Abstract THLBB02].
51. Sequella Incorporated. Sequella acquires exclusive worldwide rights to Pfizers sutezolid, currently in clinical development for tuberculosis. Press release 17 July 2013. http://www.sequella.com/docs/Sutezolid%20press% 20release.pdf [Accessed 3 August 2013]
52. Lee M, Lee J, Carroll MW, et al. Linezolid for treatment of chronic extensively drug-resistant tuberculosis. N Engl J Med 2012; 367:1508-1518.
53. Tahlan K, Wilson R, Kastrinsky DB, et al. SQ109 targets MmpL3, a membrane transporter of trehalose monomycolate involved in mycolic acid donation to the cell wall core of Mycobacterium tuberculosis. Antimicrob Agents Chemother 2012; 56:1797-1809.
54. Chen P, Gearhart J, Protopopova M, et al. Synergistic interactions of SQ109, a new ethylene diamine, with front-line antitubercular drugs in vitro. J Antimicrob Chemother 2006; 58:332-337.
55. Wallis RS, Jakubiec W, Mitton-Fry M, et al. Rapid evaluation in whole blood culture of regimens for XDR-TB containing PNU-100480 (sutezolid), TMC207, PA-824, SQ109, and pyrazinamide. PLoS One 2012; 7:e30479.
56. Reddy VM, Einck L, Andries K, Nacy CA. In vitro interactions between new antitubercular drug candidates SQ109 and TMC207. Antimicrob Agents Chemother 2010; 54:2840-2846.
57. Nikonenko BV, Protopopova M, Samala R, et al. Drug therapy of experimental tuberculosis (TB): improved outcome by combining SQ109, a new diamine antibiotic, with existing TB drugs. Antimicrob Agents Chemother 2007; 51:1563-1565.
58. Abdool Karim SS, Naidoo K, Grobler A, et al. Timing of initiation of antiretroviral drugs during tuberculosis therapy. N Engl J Med 2010; 362:697-706.
59. Abdool Karim SS, Naidoo K, Grobler A, et al. Integration of antiretroviral therapy with tuberculosis. N Engl J Med 2011; 365:1492-1501.
60. Havlir DV, Kendall MA, Ive P, et al. Timing of antiretroviral therapy for HIV-1 infection and tuberculosis. N Engl J Med 2011; 365:1482-1491.
61. Blanc F, Sok T, Laureillard D, et al. Earlier versus later start of antiretroviral therapy in HIV-infected adults with tuberculosis. N Engl J Med 2011; 365:1471-1481.
62. Svensson EM, Aweeka F, Park JG, et al. Model-based estimates of the effects of efavirenz on bedaquiline pharmacokinetics and suggested dose adjustments for patients coinfected with HIV and tuberculosis. Antimicrob Agents Chemother 2013; 57:2780-2787.
63. Dooley KE, Bliven-Sizemore EE, Weiner M, et al. Safety and pharmacokinetics of escalating daily doses of the antituberculosis drug rifapentine in healthy volunteers. Clin Pharmacol Ther 2012; 91:881-888.
64. Burman W, Benator D, Vernon A, et al. Acquired rifamycin resistance with twice-weekly treatment of HIV-related tuberculosis. Am J Respir Crit Care Med 2006; 173:350-356.
65. Weiner M, Benator D, Burman W, et al. Association between acquired rifamycin resistance and the pharmacokinetics of rifabutin and isoniazid among patients with HIV and tuberculosis. Clin Infect Dis 2005; 40:1481-1491.