Delamanid, a new 6-nitro-2,3-dihydroimidazo[2,1-b]oxazole for the management of tuberculosis resistant to at least isoniazid and rifampicin

Expert Opinion on Orphan Drugs

Volumn 2, Issue 1, 2014, Pages 87-94

  Diacon, Andreas H ^a   Von Groote Bidlingmaier, Florian ^b   Donald, Peter R ^a  

^a UNIVERSITY OF STELLENBOSCH   (South Africa)

^b Brooklyn Chest Hospital Task Applied Science   (South Africa)

Author keywords

Antituberculosis treatment; Delamanid; Multidrug resistant tuberculosis; Treatment shortening

Indexed keywords

ANTIRETROVIRUS AGENT; DELAMANID; ISONIAZID; RIFAMPICIN;

ARTICLE; BACTERICIDAL ACTIVITY; CONTROLLED CLINICAL TRIAL (TOPIC); DRUG EFFICACY; DRUG SAFETY; DRUG SCREENING; HUMAN; MULTIDRUG RESISTANT TUBERCULOSIS; QT PROLONGATION; SPUTUM CULTURE; TREATMENT DURATION;

EID: 84896710089     PISSN: None     EISSN: 21678707     Source Type: Journal    
DOI: 10.1517/21678707.2014.863729     Document Type: Article

References (32)

1. World Health Organization. Global tuberculosis report. 2012. Available from: http://www.who.int/tb/publications/2012/en/index.html [Last accessed 30 October 2013]
2. Matsumoto M, Hashizume H, Tsubouchi H, et al. Screening for novel antituberculosis agents that are effective against multidrug resistant tuberculosis. Curr Top Med Chem 2007;7:499-507
3. Diacon AH, Dawson R, Hanekom M, et al. Early bactericidal activity of delamanid (OPC-67683) in smearpositive pulmonary tuberculosis patients. Int J Tuberc Lung Dis 2011;15:949-54
4. Gler MT, Skripconoka V, Sanchez-Garavito E, et al. Delamanid for multidrug-resistant pulmonary tuberculosis. N Engl J Med 2012;366:2151-60
5. Skripconoka V, Danilovits M, Pehme L, et al. Delamanid improves outcomes and reduces mortality for multidrug-resistant tuberculosis. Eur Respir J 2012;41(6):1393-400
6. Wayne LG, Sramek HA. Metronidazole is bactericidal to dormant cells of Mycobacterium tuberculosis. Antimicrob Agents Chemother 1994;38:2054-8
7. Dhillon J, Allen BW, Hu YM, et al. Metronidazole has no antibacterial effect in Cornell model murine tuberculosis. Int J Tuberc Lung Dis 1998;2:736-42
8. Brooks JV, Furney SK, Orme IM. Metronidazole therapy in mice infected with tuberculosis. Antimicrob Agents Chemother 1999;43:1285-8
9. Desai CR, Heera S, Patel A, et al. Role of metronidazole in improving response and specific drug sensitivity in advanced pulmonary tuberculosis. J Assoc Physicians India 1989;37:694-7
10. Nagarajan K, Shankar RG, Rajappa S, et al. Nitroimidazoles XXI 2,3-dihydro-6-nitroimidazo [2,1-b] oxazoles with antitubercular activity. Eur J Med Chem 1989;24:631-3
11. Ashtekar DR, Costa-Perira R, Nagrajan K, et al. In vitro and in vivo activities of the nitroimidazole CGI 17341 against Mycobacterium tuberculosis. Antimicrob Agents Chemother 1993;37:183-6
12. Stover CK, Warrener P, VanDevanter DR, et al. A smallmolecule nitroimidazopyran drug candidate for the treatment of tuberculosis. Nature 2000;405:962-6
13. 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;56:3027-31
14. Diacon AH, Dawson R, Hanekom M, et al. Early bactericidal activity and pharmacokinetics of PA-824 in smearpositive tuberculosis patients. Antimicrob Agents Chemother 2010;54:3402-7
15. 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;380:986-93
16. Thalhammer F, Horl WH. Pharmacokinetics of meropenem in patients with renal failure and patients receiving renal replacement therapy. Clin Pharmacokinet 2000;39:271-9
17. Sasaki H, Haraguchi Y, Itotani M, et al. Synthesis and antituberculosis activity of a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b] oxazoles. J Med Chem 2006;49:7854-60
18. Matsumoto M, Hashizume H, Tomishige T, et al. OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. PLoS Med 2006;3:e466
19. Saliu OY, Crismale C, Schwander SK, et al. Bactericidal activity of OPC-67683 against drug-tolerant Mycobacterium tuberculosis. J Antimicrob Chemother 2007;60:994-8
20. Saito H, Sato K, Tomioka H, et al. In vitro antimycobacterial activity of a new quinolone, levofloxacin (DR-3355). Tuber Lung Dis 1995;76:377-80
21. Sato K, Akaki T, Tomioka H. Antimicrobial activities of benzoxazinorifamycin KRM-1648, clarithromycin and levofloxacin against intracellular Mycobacterium avium complex phagocytosed by murine peritoneal macrophages. J Antimicrob Chemother 1998;41:77-83
22. Botha FJ, Sirgel FA, Parkin DP, et al. Early bactericidal activity of ethambutol, pyrazinamide and the fixed combination of isoniazid, rifampicin and pyrazinamide (Rifater) in patients with pulmonary tuberculosis. S Afr Med J 1996;86:155-8
23. Jindani A, Aber VR, Edwards EA, et al. The early bactericidal activity of drugs in patients with pulmonary tuberculosis. Am Rev Respir Dis 1980;121:939-49
24. Rustomjee R, Diacon AH, Allen J, et al. Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis. Antimicrob Agents Chemother 2008;52:2831-5
25. World Health Organization. Guidelines for the programmatic management of drug-resistant tuberculosis. Available from: http://www.who.int/tb/publications/ 2011/en/index.html [Last accessed 30 October 2013]
26. Paccaly A, Petersen C, Patil S, et al. Absence of clinically relevant drug interaction between delamanid, a new drug for multidrug-resistant tuberculosis (MDR-TB) and tenofovir or lopinavir/ritonavir in healthy subjects [abstract WEPE043]. AIDS. 19th International AIDS Conference; Washington DC; 2012
27. Peloquin CA, MacPhee AA, Berning SE. Malabsorption of antimycobacterial medications. N Engl J Med 1993;329:1122-3
28. Gurumurthy P, Ramachandran G, Hemanth Kumar AK, et al. Malabsorption of rifampin and isoniazid in HIV-infected patients with and without tuberculosis. Clin Infect Dis 2004;38:280-3
29. Otsuka Pharmaceutical Development & Commercialization. Inc. NCT01424670: safety and efficacy trial of delamanid for 6 months in patients with multidrug resistant tuberculosis. Available from: http://www. clinicaltrials.gov [Last accessed 13 September 2013]
30. Mitchison DA. Role of individual drugs in the chemotherapy of tuberculosis. Int J Tuberc Lung Dis 2000;4:796-806
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;56:3271-6
32. Otsuka Pharmaceutical Development & Commercialization. Inc. NCT01859923: A 6-month safety, efficacy, and pharmacokinetic trial of delamanid in pediatric patients with multidrug resistant tuberculosis. Available from: http://www.clinicaltrials.gov [Last accessed 14 September 2013]