Antimycobacterial drugs currently in Phase II clinical trials and preclinical phase for tuberculosis treatment

Bibliography

• World Health Organization. Global tuberculosis control. WHO 2011 report. Press Release (2011): 2011
   Google Scholar
• World Health Organization. Multidrug and extensively drug-resistant TB (M/XDR-TB). global report on surveillance and response. Press Release (2010). 2010
   Google Scholar
• Schatz A, Waksman SA. Effect of Streptomycin and Other Antibiotic Substances upon Mycobacterium tuberculosis and Related Organisms. Proc Soc Experiment Biol Med 1944;57(2):244-8
   Google Scholar
• Lehmann J. Para-aminosalicylic acid in the treatment of tuberculosis. Lancet 1946;1(6384):15
   PubMedGoogle Scholar
• Nitti V. Antituberculosis activity of rifampin. Report of studies performed and in progress (1966-1971). Chest 1972;61(6):589-98
   PubMed Web of Science ®Google Scholar
• World Health Organization. Treatment of Tuberculosis. Guidelines for National Programmes. Press Release (2003). 2003
   Google Scholar
• Alangaden GJ, Kreiswirth BN, Aouad A, Mechanism of resistance to amikacin and kanamycin in Mycobacterium tuberculosis. Antimicrob Agents Chemother 1998;42(5):1295-7
   PubMed Web of Science ®Google Scholar
• Kruuner A, Jureen P, Levina K, Discordant resistance to kanamycin and amikacin in drug-resistant Mycobacterium tuberculosis. Antimicrob Agents Chemother 2003;47(9):2971-3
   PubMed Web of Science ®Google Scholar
• Maus CE, Plikaytis BB, Shinnick TM. Molecular analysis of cross-resistance to capreomycin, kanamycin, amikacin, and viomycin in Mycobacterium tuberculosis. Antimicrob Agents Chemother 2005;49(8):3192-7
   PubMed Web of Science ®Google Scholar
• Kass JS, Shandera WX. Nervous system effects of antituberculosis therapy. CNS Drugs 2010;24(8):655-67
   PubMed Web of Science ®Google Scholar
• Berning SE. The role of fluoroquinolones in tuberculosis today. Drugs 2001;61(1):9-18
   PubMed Web of Science ®Google Scholar
• Bryskier A, Lowther J. Fluoroquinolones and tuberculosis. Expert Opin Investig Drugs 2002;11(2):233-58
   PubMed Web of Science ®Google Scholar
• Migliori GB, Lange C, Girardi E, Fluoroquinolones: are they essential to treat multidrug-resistant tuberculosis? Eur Respir J 2008;31(4):904-5
   PubMed Web of Science ®Google Scholar
• Aubry A, Veziris N, Cambau E, Novel gyrase mutations in quinolone-resistant and -hypersusceptible clinical isolates of Mycobacterium tuberculosis: functional analysis of mutant enzymes. Antimicrob Agents Chemother 2006;50(1):104-12
   PubMed Web of Science ®Google Scholar
• , Jr., Takiff HE, Salazar L, Guerrero C, Cloning and nucleotide sequence of Mycobacterium tuberculosis gyrA and gyrB genes and detection of quinolone resistance mutations. Antimicrob Agents Chemother 1994;38(4):773-80
   PubMed Web of Science ®Google Scholar
• Xu C, Kreiswirth BN, Sreevatsan S, Fluoroquinolone resistance associated with specific gyrase mutations in clinical isolates of multidrug-resistant Mycobacterium tuberculosis. J Infect Dis 1996;174(5):1127-30
   PubMed Web of Science ®Google Scholar
• Yamazaki H. In vitro experiments on the tuberculo-bacteriostatic activity of o-aminophenol, p-aminosalicylic acid, streptomycin and tibione in the presence of p-aminobenzoic acid. Jpn Med J (Natl Inst Health Jpn) 1950;3(5):299-307
   PubMedGoogle Scholar
• Caminero JA. Treatment of multidrug-resistant tuberculosis: evidence and controversies. Int J Tuberc Lung Dis 2006;10(8):829-37
   PubMed Web of Science ®Google Scholar
• Falzon D, Jaramillo E, Schunemann HJ, WHO guidelines for the programmatic management of drug-resistant tuberculosis: 2011 update. Eur Respir J 2011;38(3):516-28
   PubMed Web of Science ®Google Scholar
• Quemard A, Laneelle G, Lacave C. Mycolic acid synthesis: a target for ethionamide in mycobacteria? Antimicrob Agents Chemother 1992;36(6):1316-21
   PubMed Web of Science ®Google Scholar
• Protopopova M, Hanrahan C, Nikonenko B, Identification of a new antitubercular drug candidate, SQ109, from a combinatorial library of 1,2-ethylenediamines. J Antimicrob Chemother 2005;56(5):968-74
   PubMed Web of Science ®Google Scholar
• Tahlan K, Wilson R, Kastrinsky DB, 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(4):1797-809
   PubMed Web of Science ®Google Scholar
• Chen P, Gearhart J, Protopopova M, Synergistic interactions of SQ109, a new ethylene diamine, with front-line antitubercular drugs in vitro. J Antimicrob Chemother 2006;58(2):332-7
   PubMed Web of Science ®Google Scholar
• Reddy VM, Einck L, Andries K, Nacy CA. In vitro interactions between new antitubercular drug candidates SQ109 and TMC207. Antimicrob Agents Chemother 2010;54(7):2840-6
   PubMed Web of Science ®Google Scholar
• Jia L, Coward L, Gorman GS, Pharmacoproteomic effects of isoniazid, ethambutol, and N-geranyl-N'-(2-adamantyl)ethane-1,2-diamine (SQ109) on Mycobacterium tuberculosis H37Rv. J Pharmacol Exp Ther 2005;315(2):905-11
   PubMed Web of Science ®Google Scholar
• SQ109. 2012. Avilable from http://www.newtbdrugs.org/project.php?id=144
   Google Scholar
• Andries K, Verhasselt P, Guillemont J, A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis. Science 2005;307(5707):223-7
   PubMed Web of Science ®Google Scholar
• Ibrahim M, Andries K, Lounis N, Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis. Antimicrob Agents Chemother 2007;51(3):1011-15
   PubMed Web of Science ®Google Scholar
• Ibrahim M, Truffot-Pernot C, Andries K, Sterilizing activity of R207910 (TMC207)-containing regimens in the murine model of tuberculosis. Am J Respir Crit Care Med 2009;180(6):553-7
   PubMed Web of Science ®Google Scholar
• Lounis N, Veziris N, Chauffour A, Combinations of R207910 with drugs used to treat multidrug-resistant tuberculosis have the potential to shorten treatment duration. Antimicrob Agents Chemother 2006;50(11):3543-7
   PubMed Web of Science ®Google Scholar
• Veziris N, Ibrahim M, Lounis N, Sterilizing activity of second-line regimens containing TMC207 in a murine model of tuberculosis. PLoS One 2011;6(3):e17556
   PubMed Web of Science ®Google Scholar
• Rustomjee R, Diacon AH, Allen J, Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis. Antimicrob Agents Chemother 2008;52(8):2831-5
   PubMed Web of Science ®Google Scholar
• Diacon AH, Donald PR, Pym A, Randomized Pilot Trial of Eight Weeks of Bedaquiline (TMC207) Treatment for Multidrug-Resistant Tuberculosis: long-Term Outcome, Tolerability, and Effect on Emergence of Drug Resistance. Antimicrob Agents Chemother 2012;56(6):3271-6
   PubMed Web of Science ®Google Scholar
• Stover CK, Warrener P, VanDevanter DR, A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. Nature 2000;405(6789):962-6
   PubMed Web of Science ®Google Scholar
• Manjunatha U, Boshoff HI, Barry CE. The mechanism of action of PA-824: novel insights from transcriptional profiling. Commun Integr Biol 2009;2(3):215-18
   PubMedGoogle Scholar
• Singh R, Manjunatha U, Boshoff HI, PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. Science 2008;322(5906):1392-5
   PubMed Web of Science ®Google Scholar
• Ahmad Z, Peloquin CA, Singh RP, PA-824 exhibits time-dependent activity in a murine model of tuberculosis. Antimicrob Agents Chemother 2011;55(1):239-45
   PubMed Web of Science ®Google Scholar
• Nuermberger E, Rosenthal I, Tyagi S, Combination chemotherapy with the nitroimidazopyran PA-824 and first-line drugs in a murine model of tuberculosis. Antimicrob Agents Chemother 2006;50(8):2621-5
   PubMed Web of Science ®Google Scholar
• Nuermberger E, Tyagi S, Tasneen R, 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(4):1522-4
   PubMed Web of Science ®Google Scholar
• Diacon AH, Dawson R, du Bois J, Phase II Dose-Ranging Trial of the Early Bactericidal Activity of PA-824. Antimicrob Agents Chemother 2012;56(6):3027-31
   PubMed Web of Science ®Google Scholar
• Matsumoto M, Hashizume H, Tomishige T, OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. PLoS Med 2006;3(11):e466
   PubMed Web of Science ®Google Scholar
• Gler MT, Skripconoka V, Sanchez-Garavito E, Delamanid for multidrug-resistant pulmonary tuberculosis. N Engl J Med 2012;366(23):2151-60
   PubMed Web of Science ®Google Scholar
• Safety and Efficacy Trial of Delamanid for 6 Months in Patients With Multidrug Resistant Tuberculosis. 2012. Available from: http://www.newtbdrugs.org/project.php?id=136
   Google Scholar
• Alcala L, Ruiz-Serrano MJ, Perez-Fernandez Turegano C, In vitro activities of linezolid against clinical isolates of Mycobacterium tuberculosis that are susceptible or resistant to first-line antituberculous drugs. Antimicrob Agents Chemother 2003;47(1):416-17
   PubMed Web of Science ®Google Scholar
• Shinabarger DL, Marotti KR, Murray RW, Mechanism of action of oxazolidinones: effects of linezolid and eperezolid on translation reactions. Antimicrob Agents Chemother 1997;41(10):2132-6
   PubMed Web of Science ®Google Scholar
• Williams KN, Stover CK, Zhu T, Promising antituberculosis activity of the oxazolidinone PNU-100480 relative to that of linezolid in a murine model. Antimicrob Agents Chemother 2009;53(4):1314-19
   PubMed Web of Science ®Google Scholar
• Dietze R, Hadad DJ, McGee B, Early and extended early bactericidal activity of linezolid in pulmonary tuberculosis. Am J Respir Crit Care Med 2008;178(11):1180-5
   PubMed Web of Science ®Google Scholar
• Condos R, Hadgiangelis N, Leibert E, Case series report of a linezolid-containing regimen for extensively drug-resistant tuberculosis. Chest 2008;134(1):187-92
   PubMedGoogle Scholar
• von der Lippe B, Sandven P, Brubakk O. Efficacy and safety of linezolid in multidrug resistant tuberculosis (MDR-TB)–a report of ten cases. J Infect 2006;52(2):92-6
   PubMed Web of Science ®Google Scholar
• Singla R, Caminero JA, Jaiswal A, Linezolid: an effective, safe and cheap drug for patients failing multidrug-resistant tuberculosis treatment in India. Eur Respir J 2012;39(4):956-62
   PubMed Web of Science ®Google Scholar
• Alffenaar JW, van der Laan T, Simons S, Susceptibility of clinical Mycobacterium tuberculosis isolates to a potentially less toxic derivate of linezolid, PNU-100480. Antimicrob Agents Chemother 2011;55(3):1287-9
   PubMed Web of Science ®Google Scholar
• Williams K, Minkowski A, Amoabeng O, Sterilizing activities of novel combinations lacking first- and second-line drugs in a murine model of tuberculosis. Antimicrob Agents Chemother 2012;56(6):3114-20
   PubMed Web of Science ®Google Scholar
• Arbex MA, Varella Mde C, Siqueira HR, Mello FA. Antituberculosis drugs: drug interactions, adverse effects, and use in special situations. Part 2: second line drugs. J Bras Pneumol 2010;36(5):641-56
   PubMed Web of Science ®Google Scholar
• Baulard AR, Betts JC, Engohang-Ndong J, Activation of the pro-drug ethionamide is regulated in mycobacteria. J Biol Chem 2000;275(36):28326-31
   PubMed Web of Science ®Google Scholar
• Engohang-Ndong J, Baillat D, Aumercier M, EthR, a repressor of the TetR/CamR family implicated in ethionamide resistance in mycobacteria, octamerizes cooperatively on its operator. Mol Microbiol 2004;51(1):175-88
   PubMed Web of Science ®Google Scholar
• Schumacher MA, Miller MC, Grkovic S, Structural mechanisms of QacR induction and multidrug recognition. Science 2001;294(5549):2158-63
   PubMed Web of Science ®Google Scholar
• Frenois F, Engohang-Ndong J, Locht C, Structure of EthR in a ligand bound conformation reveals therapeutic perspectives against tuberculosis. Mol Cell 2004;16(2):301-7
   PubMed Web of Science ®Google Scholar
• Willand N, Dirie B, Carette X, Synthetic EthR inhibitors boost antituberculous activity of ethionamide. Nat Med 2009;15(5):537-44
   PubMed Web of Science ®Google Scholar
• Flipo M, Desroses M, Lecat-Guillet N, Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors. J Med Chem 2011;54(8):2994-3010
   PubMed Web of Science ®Google Scholar
• Flipo M, Desroses M, Lecat-Guillet N, Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors. J Med Chem 2012;55(1):68-83
   PubMed Web of Science ®Google Scholar
• SQ609. 2011. Avilable from http://www.sequella.com/docs/Sequella_1sheet_SQ609_v1.pdf
   Google Scholar
• Bogatcheva E, Dubuisson T, Protopopova M, Chemical modification of capuramycins to enhance antibacterial activity. J Antimicrob Chemother 2011;66(3):578-87
   PubMed Web of Science ®Google Scholar
• Muramatsu Y, Muramatsu A, Ohnuki T, Studies on novel bacterial translocase I inhibitors, A-500359s. I. Taxonomy, fermentation, isolation, physico-chemical properties and structure elucidation of A-500359 A, C, D and G. J Antibiot (Tokyo) 2003;56(3):243-52
   PubMed Web of Science ®Google Scholar
• Reddy VM, Einck L, Nacy CA. In vitro antimycobacterial activities of capuramycin analogues. Antimicrob Agents Chemother 2008;52(2):719-21
   PubMed Web of Science ®Google Scholar
• Koga T, Fukuoka T, Doi N, Activity of capuramycin analogues against Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium intracellulare in vitro and in vivo. J Antimicrob Chemother 2004;54(4):755-60
   PubMed Web of Science ®Google Scholar
• Nikonenko BV, Reddy VM, Protopopova M, Activity of SQ641, a capuramycin analog, in a murine model of tuberculosis. Antimicrob Agents Chemother 2009;53(7):3138-9
   PubMed Web of Science ®Google Scholar
• CPZEN-45. 2011. Avilable from http://www.newtbdrugs.org/project.php?id=92
   Google Scholar
• Sood R, Rao M, Singhal S, Rattan A. Activity of RBx 7644 and RBx 8700, new investigational oxazolidinones, against Mycobacterium tuberculosis infected murine macrophages. Int J Antimicrob Agents 2005;25(6):464-8
   PubMed Web of Science ®Google Scholar
• Ahmad Z, Minkowski A, Peloquin CA, Activity of the fluoroquinolone DC-159a in the initial and continuation phases of treatment of murine tuberculosis. Antimicrob Agents Chemother 2011;55(4):1781-3
   PubMed Web of Science ®Google Scholar
• Sekiguchi J, Disratthakit A, Maeda S, Doi N. Characteristic resistance mechanism of Mycobacterium tuberculosis to DC-159a, a new respiratory quinolone. Antimicrob Agents Chemother 2011;55(8):3958-60
   PubMed Web of Science ®Google Scholar
• Makarov V, Manina G, Mikusova K, Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis. Science 2009;324(5928):801-4
   PubMed Web of Science ®Google Scholar
• Manina G, Bellinzoni M, Pasca MR, Biological and structural characterization of the Mycobacterium smegmatis nitroreductase NfnB, and its role in benzothiazinone resistance. Mol Microbiol 2010;77(5):1172-85
   PubMed Web of Science ®Google Scholar