Antimalarial compounds in Phase II clinical development

Bibliography

• WHO. World malaria report, 2013. 2013. Available from: http://www.who.int/iris/bitstream/10665/97008/1/9789241564694_eng.pdf [Last accessed 16 December 2014]
   Google Scholar
• Noedl H, Se Y, Schaecher K, et al. Evidence of artemisinin-resistant malaria in western Cambodia. N Engl J Med 2008;359(24):2619-20
   PubMed Web of Science ®Google Scholar
• WHO Global Malaria Programme (GMP) and Department of Immunization VBIaU. Intermittent preventive treatment for infants using sulfadoxine-pyrimethamine (SP-IPTi) for malaria control in Africa: implementation field guide. 2011. Available from: http://whqlibdoc.who.int/hq/2011/WHO_IVB_11.07_eng.pdf [Last accessed 02 October 2014]
   Google Scholar
• von Seidlein L, Auburn S, Espino F, et al. Review of key knowledge gaps in glucose-6-phosphate dehydrogenase deficiency detection with regard to the safe clinical deployment of 8-aminoquinoline treatment regimens: a workshop report. Malar J 2013;12:112
   PubMed Web of Science ®Google Scholar
• Bennett JW, Pybus BS, Yadava A, et al. Primaquine failure and cytochrome P-450 2D6 in Plasmodium vivax malaria. N Engl J Med 2013;369(14):1381-2
   PubMed Web of Science ®Google Scholar
• Looareesuwan S, Viravan C, Webster HK, et al. Clinical studies of atovaquone, alone or in combination with other antimalarial drugs, for treatment of acute uncomplicated malaria in Thailand. Am J Trop Med Hyg 1996;54(1):62-6
   PubMed Web of Science ®Google Scholar
• Korsinczky M, Chen N, Kotecka B, et al. Mutations in Plasmodium falciparum cytochrome b that are associated with atovaquone resistance are located at a putative drug-binding site. Antimicrob Agents Chemother 2000;44(8):2100-8
   PubMed Web of Science ®Google Scholar
• Gonzalez R, Hellgren U, Greenwood B, Menendez C. Mefloquine safety and tolerability in pregnancy: a systematic literature review. Malar J 2014;13:75
   PubMed Web of Science ®Google Scholar
• Gonzalez R, Mombo-Ngoma G, Ouedraogo S, et al. Intermittent preventive treatment of malaria in pregnancy with mefloquine in HIV-negative women: a multicentre randomized controlled trial. PLoS Med 2014;11(9):e1001733
   PubMed Web of Science ®Google Scholar
• Burrows JN, van Huijsduijnen RH, Mohrle JJ, et al. Designing the next generation of medicines for malaria control and eradication. Malar J 2013;12:187
   PubMed Web of Science ®Google Scholar
• MMV Interactive Research & Development portfolio. Available from: http://www.mmv.org/research-development/rd-portfolio [Last accessed 20 October 2014]
   Google Scholar
• Anthony MP, Burrows JN, Duparc S, et al. The global pipeline of new medicines for the control and elimination of malaria. Malar J 2012;11:316
   PubMed Web of Science ®Google Scholar
• Flannery EL, Chatterjee AK, Winzeler EA. Antimalarial drug discovery - approaches and progress towards new medicines. Nat Rev Microbiol 2013;11(12):849-62
   PubMed Web of Science ®Google Scholar
• Held J, Kreidenweiss A, Mordmuller B. Novel approaches in antimalarial drug discovery. Expert Opin Drug Discov 2013;8(11):1325-37
   PubMed Web of Science ®Google Scholar
• Schrader FC, Barho M, Steiner I, et al. The antimalarial pipeline--an update. Int J Med Microbiol 2012;302(4-5):165-71
   PubMed Web of Science ®Google Scholar
• Kreidenweiss A, Kremsner PG, Dietz K, Mordmuller B. In vitro activity of ferroquine (SAR97193) is independent of chloroquine resistance in Plasmodium falciparum. Am J Trop Med Hyg 2006;75(6):1178-81
   PubMed Web of Science ®Google Scholar
• Biot C, Glorian G, Maciejewski LA, Brocard JS. Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. J Med Chem 1997;40(23):3715-18
   PubMed Web of Science ®Google Scholar
• Delhaes L, Abessolo H, Biot C, et al. In vitro and in vivo antimalarial activity of ferrochloroquine, a ferrocenyl analogue of chloroquine against chloroquine-resistant malaria parasites. Parasitol Res 2001;87(3):239-44
   PubMed Web of Science ®Google Scholar
• Mombo-Ngoma G, Supan C, Dal-Bianco MP, et al. Phase I randomized dose-ascending placebo-controlled trials of ferroquine – a candidate anti-malarial drug – in adults with asymptomatic Plasmodium falciparum infection. Malar J 2011;10:53
   PubMed Web of Science ®Google Scholar
• Supan C, Mombo-Ngoma G, Dal-Bianco MP, et al. Pharmacokinetics of ferroquine, a novel 4-aminoquinoline, in asymptomatic carriers of Plasmodium falciparum infections. Antimicrob Agents Chemother 2012;56(6):3165-73
   PubMed Web of Science ®Google Scholar
• De D, Krogstad FM, Cogswell FB, Krogstad DJ. Aminoquinolines that circumvent resistance in Plasmodium falciparum in vitro. Am J Trop Med Hyg 1996;55(6):579-83
   PubMed Web of Science ®Google Scholar
• Mzayek F, Deng H, Mather FJ, et al. Randomized dose-ranging controlled trial of AQ-13, a candidate antimalarial, and chloroquine in healthy volunteers. PLoS Clin Trials 2007;2(1):e6
   PubMedGoogle Scholar
• White NJ. Cardiotoxicity of antimalarial drugs. Lancet Infect Dis 2007;7(8):549-58
   PubMed Web of Science ®Google Scholar
• Crockett M, Kain KC. Tafenoquine: a promising new antimalarial agent. Expert Opin Investig Drugs 2007;16(5):705-15
   PubMed Web of Science ®Google Scholar
• Shanks GD, Oloo AJ, Aleman GM, et al. A new primaquine analogue, tafenoquine (WR 238605), for prophylaxis against Plasmodium falciparum malaria. Clin Infect Dis 2001;33(12):1968-74
   PubMed Web of Science ®Google Scholar
• Marcsisin SR, Sousa JC, Reichard GA, et al. Tafenoquine and NPC-1161B require CYP 2D metabolism for anti-malarial activity: implications for the 8-aminoquinoline class of anti-malarial compounds. Malar J 2014;13:2
   PubMed Web of Science ®Google Scholar
• Galappaththy GN, Tharyan P, Kirubakaran R. Primaquine for preventing relapse in people with Plasmodium vivax malaria treated with chloroquine. Cochrane Database Syst Rev 2013;10:CD004389
   PubMedGoogle Scholar
• Baird JK, Hoffman SL. Primaquine therapy for malaria. Clin Infect Dis 2004;39(9):1336-45
   PubMed Web of Science ®Google Scholar
• Brueckner RP, Lasseter KC, Lin ET, Schuster BG. First-time-in-humans safety and pharmacokinetics of WR 238605, a new antimalarial. Am J Trop Med Hyg 1998;58(5):645-9
   PubMed Web of Science ®Google Scholar
• Brueckner RP, Coster T, Wesche DL, et al. Prophylaxis of Plasmodium falciparum infection in a human challenge model with WR 238605, a new 8-aminoquinoline antimalarial. Antimicrob Agents Chemother 1998;42(5):1293-4
   PubMed Web of Science ®Google Scholar
• Brueckner RC, Coster T, Kin-Ahn G, et al. Safety, pharmacokinetics and antimalarial activity of WR 238605 in Man. Am J Trop Med Hyg 1997;57(3 Suppl):522
   Google Scholar
• Nasveld PE, Edstein MD, Reid M, et al. Randomized, double-blind study of the safety, tolerability, and efficacy of tafenoquine versus mefloquine for malaria prophylaxis in nonimmune subjects. Antimicrob Agents Chemother 2010;54(2):792-8
   PubMed Web of Science ®Google Scholar
• Walsh DS, Eamsila C, Sasiprapha T, et al. Efficacy of monthly tafenoquine for prophylaxis of Plasmodium vivax and multidrug-resistant P. falciparum malaria. J Infect Dis 2004;190(8):1456-63
   PubMed Web of Science ®Google Scholar
• Elmes NJ, Nasveld PE, Kitchener SJ, et al. The efficacy and tolerability of three different regimens of tafenoquine versus primaquine for post-exposure prophylaxis of Plasmodium vivax malaria in the Southwest Pacific. Trans R Soc Trop Med Hyg 2008;102(11):1095-101
   PubMed Web of Science ®Google Scholar
• Nasveld P, Kitchener S, Edstein M, Rieckmann K. Comparison of tafenoquine (WR238605) and primaquine in the post-exposure (terminal) prophylaxis of vivax malaria in Australian Defence Force personnel. Trans R Soc Trop Med Hyg 2002;96(6):683-4
   PubMed Web of Science ®Google Scholar
• Lell B, Faucher JF, Missinou MA, et al. Malaria chemoprophylaxis with tafenoquine: a randomised study. Lancet 2000;355(9220):2041-5
   PubMed Web of Science ®Google Scholar
• Hale BR, Owusu-Agyei S, Fryauff DJ, et al. A randomized, double-blind, placebo-controlled, dose-ranging trial of tafenoquine for weekly prophylaxis against Plasmodium falciparum. Clin Infect Dis 2003;36(5):541-9
   PubMed Web of Science ®Google Scholar
• Leary KJ, Riel MA, Roy MJ, et al. A randomized, double-blind, safety and tolerability study to assess the ophthalmic and renal effects of tafenoquine 200 mg weekly versus placebo for 6 months in healthy volunteers. Am J Trop Med Hyg 2009;81(2):356-62
   PubMed Web of Science ®Google Scholar
• Dow GS, Gettayacamin M, Hansukjariya P, et al. Radical curative efficacy of tafenoquine combination regimens in Plasmodium cynomolgi-infected Rhesus monkeys (Macaca mulatta). Malar J 2011;10:212
   PubMed Web of Science ®Google Scholar
• Miller AK, Harrell E, Ye L, et al. Pharmacokinetic interactions and safety evaluations of coadministered tafenoquine and chloroquine in healthy subjects. Br J Clin Pharmacol 2013;76(6):858-67
   PubMed Web of Science ®Google Scholar
• Walsh DS, Wilairatana P, Tang DB, et al. Randomized trial of 3-dose regimens of tafenoquine (WR238605) versus low-dose primaquine for preventing Plasmodium vivax malaria relapse. Clin Infect Dis 2004;39(8):1095-103
   PubMed Web of Science ®Google Scholar
• Walsh DS, Looareesuwan S, Wilairatana P, et al. Randomized dose-ranging study of the safety and efficacy of WR 238605 (Tafenoquine) in the prevention of relapse of Plasmodium vivax malaria in Thailand. J Infect Dis 1999;180(4):1282-7
   PubMed Web of Science ®Google Scholar
• Llanos-Cuentas A, Lacerda MV, Rueangweerayut R, et al. Tafenoquine plus chloroquine for the treatment and relapse prevention of Plasmodium vivax malaria (DETECTIVE): a multicentre, double-blind, randomised, phase 2b dose-selection study. Lancet 2014;383(9922):1049-58
   PubMed Web of Science ®Google Scholar
• Green JA, Patel AK, Patel BR, et al. Tafenoquine at therapeutic concentrations does not prolong fridericia-corrected QT interval in healthy subjects. J Clin Pharmacol 2014;54(9):995-1005
   PubMed Web of Science ®Google Scholar
• WHO. WHO briefing on malaria treatment guidelines and artemisinin monotherapies. Available from: http://www.who.int/malaria/publications/atoz/meeting_briefing19april/en/ [Last accessed 18 October 2014]
   Google Scholar
• WHO. WHO releases new malaria guidelines for treatment and procurement of medicines. WHO. Available from: http://www.who.int/mediacentre/news/releases/2010/malaria_20100308/en/ [Last accessed 09 October 2014]
   Google Scholar
• Douglas NM, Anstey NM, Angus BJ, et al. Artemisinin combination therapy for vivax malaria. Lancet Infect Dis 2010;10(6):405-16
   PubMed Web of Science ®Google Scholar
• Vennerstrom JL, Arbe-Barnes S, Brun R, et al. Identification of an antimalarial synthetic trioxolane drug development candidate. Nature 2004;430(7002):900-4
   PubMed Web of Science ®Google Scholar
• Kreidenweiss A, Mordmuller B, Krishna S, Kremsner PG. Antimalarial activity of a synthetic endoperoxide (RBx-11160/OZ277) against Plasmodium falciparum isolates from Gabon. Antimicrob Agents Chemother 2006;50(4):1535-7
   PubMed Web of Science ®Google Scholar
• Valecha N, Looareesuwan S, Martensson A, et al. Arterolane, a new synthetic trioxolane for treatment of uncomplicated Plasmodium falciparum malaria: a phase II, multicenter, randomized, dose-finding clinical trial. Clin Infect Dis 2010;51(6):684-91
   PubMed Web of Science ®Google Scholar
• Valecha N, Krudsood S, Tangpukdee N, et al. Arterolane maleate plus piperaquine phosphate for treatment of uncomplicated Plasmodium falciparum malaria: a comparative, multicenter, randomized clinical trial. Clin Infect Dis 2012;55(5):663-71
   PubMed Web of Science ®Google Scholar
• Charman SA, Arbe-Barnes S, Bathurst IC, et al. Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria. Proc Natl Acad Sci USA 2011;108(11):4400-5
   PubMed Web of Science ®Google Scholar
• Moehrle JJ, Duparc S, Siethoff C, et al. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials. Br J Clin Pharmacol 2013;75(2):524-37
   PubMed Web of Science ®Google Scholar
• James S, McCarthy PG, Suzanne E, et al. A dose ranging study in the human induced blood stage malaria model to define the antiparasitic activity and pharmacokinetic-pharmacodynamic relationship of the synthetic peroxide antimalarial OZ439. Abstract book Am J Trop Med Hyg 2013;89:1-78
   Google Scholar
• Medhi B, Patyar S, Rao RS, et al. Pharmacokinetic and toxicological profile of artemisinin compounds: an update. Pharmacology 2009;84(6):323-32
   PubMed Web of Science ®Google Scholar
• Genovese RF, Newman DB. Understanding artemisinin-induced brainstem neurotoxicity. Arch Toxicol 2008;82(6):379-85
   PubMed Web of Science ®Google Scholar
• Ramharter M, Burkhardt D, Nemeth J, et al. In vitro activity of artemisone compared with artesunate against Plasmodium falciparum. Am J Trop Med Hyg 2006;75(4):637-9
   PubMed Web of Science ®Google Scholar
• Vivas L, Rattray L, Stewart LB, et al. Antimalarial efficacy and drug interactions of the novel semi-synthetic endoperoxide artemisone in vitro and in vivo. J Antimicrob Chemother 2007;59(4):658-65
   PubMed Web of Science ®Google Scholar
• Obaldia NIII, Kotecka BM, Edstein MD, et al. Evaluation of artemisone combinations in Aotus monkeys infected with Plasmodium falciparum. Antimicrob Agents Chemother 2009;53(8):3592-4
   PubMed Web of Science ®Google Scholar
• Nagelschmitz J, Voith B, Wensing G, et al. First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. Antimicrob Agents Chemother 2008;52(9):3085-91
   PubMed Web of Science ®Google Scholar
• Leitgeb AM, Blomqvist K, Cho-Ngwa F, et al. Low anticoagulant heparin disrupts Plasmodium falciparum rosettes in fresh clinical isolates. Am J Trop Med Hyg 2011;84(3):390-6
   PubMed Web of Science ®Google Scholar
• Press Release. Available from: www.dilaforette.se [Last accessed 09 December 2014]
   Google Scholar
• Charunwatthana P, Leitgeb AM, Rueangveerayuth R, et al. Sevuparin: adjunct therapy in P. falciparum malaria shows anti-adhesive and anti-merozoite effects - potential to improve outcome of severe malaria. Poster presented at ASTMH 2014. Available from: http://www.dilaforette.se/wp-content/uploads/2014/11/ASTMH_LB-3278.pdf [Last accessed 09 December 2014]
   Google Scholar
• Saiwaew S, Udomsangpetch R, Charunwatthana P, et al. Effects of sevuparin on rosette formation and cytoadherence of Plasmodium falciparum - infected erythrocyte. Available from: http://www.dilaforette.se/wp-content/uploads/2014/11/ASTMH_LB-220.pdf [Last accessed 09 December 2014]
   Google Scholar
• Gamo FJ, Sanz LM, Vidal J, et al. Thousands of chemical starting points for antimalarial lead identification. Nature 2010;465(7296):305-10
   PubMed Web of Science ®Google Scholar
• Guiguemde WA, Shelat AA, Bouck D, et al. Chemical genetics of Plasmodium falciparum. Nature 2010;465(7296):311-15
   PubMed Web of Science ®Google Scholar
• Lucantoni L, Avery V. Whole-cell in vitro screening for gametocytocidal compounds. Future Med Chem 2012;4(18):2337-60
   PubMed Web of Science ®Google Scholar
• Meister S, Plouffe DM, Kuhen KL, et al. Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery. Science 2011;334(6061):1372-7
   PubMed Web of Science ®Google Scholar
• Rottmann M, McNamara C, Yeung BK, et al. Spiroindolones, a potent compound class for the treatment of malaria. Science 2010;329(5996):1175-80
   PubMed Web of Science ®Google Scholar
• Smith PW, Diagana TT, Yeung BK. Progressing the global antimalarial portfolio: finding drugs which target multiple Plasmodium life stages. Parasitology 2014;141(1):66-76
   PubMed Web of Science ®Google Scholar
• van Pelt-Koops JC, Pett HE, Graumans W, et al. The spiroindolone drug candidate NITD609 potently inhibits gametocytogenesis and blocks Plasmodium falciparum transmission to anopheles mosquito vector. Antimicrob Agents Chemother 2012;56(7):3544-8
   PubMed Web of Science ®Google Scholar
• Spillman NJ, Allen RJ, McNamara CW, et al. Na(+) regulation in the malaria parasite Plasmodium falciparum involves the cation ATPase PfATP4 and is a target of the spiroindolone antimalarials. Cell Host Microbe 2013;13(2):227-37
   PubMed Web of Science ®Google Scholar
• Leong FJ, Li R, Jain JP, et al. A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel antimalarial spiroindolone KAE609 (cipargamin) to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers. Antimicrob Agents Chemother 2014;58(10):6209-14
   PubMed Web of Science ®Google Scholar
• White NJ, Pukrittayakamee S, Phyo AP, et al. Spiroindolone KAE609 for falciparum and vivax malaria. N Engl J Med 2014;371(5):403-10
   PubMed Web of Science ®Google Scholar
• Derbyshire ER, Prudencio M, Mota MM, Clardy J. Liver-stage malaria parasites vulnerable to diverse chemical scaffolds. Proc Natl Acad Sci USA 2012;109(22):8511-16
   PubMed Web of Science ®Google Scholar
• Wu T, Nagle A, Kuhen K, et al. Imidazolopiperazines: hit to lead optimization of new antimalarial agents. J Med Chem 2011;54(14):5116-30
   PubMed Web of Science ®Google Scholar
• Nagle A, Wu T, Kuhen K, et al. Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. J Med Chem 2012;55(9):4244-73
   PubMed Web of Science ®Google Scholar
• Kuhen KL, Chatterjee AK, Rottmann M, et al. KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission. Antimicrob Agents Chemother 2014;58(9):5060-7
   PubMed Web of Science ®Google Scholar
• Leong FJ, Zhao R, Zeng S, et al. A First-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel imidazolopiperazine KAF156 to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers. Antimicrob Agents Chemother 2014;58(11):6437-43
   PubMed Web of Science ®Google Scholar
• Ehrlich P, Guttmann P. Ueber die Wirkung des Methylenblau bei Malaria. Berl Klin Wochenschr 1891;28:953-6
   Google Scholar
• Vennerstrom JL, Makler MT, Angerhofer CK, Williams JA. Antimalarial dyes revisited: xanthenes, azines, oxazines, and thiazines. Antimicrob Agents Chemother 1995;39(12):2671-7
   PubMed Web of Science ®Google Scholar
• Atamna H, Krugliak M, Shalmiev G, et al. Mode of antimalarial effect of methylene blue and some of its analogues on Plasmodium falciparum in culture and their inhibition of P. vinckei petteri and P. yoelii nigeriensis in vivo. Biochem Pharmacol 1996;51(5):693-700
   PubMed Web of Science ®Google Scholar
• Rengelshausen J, Burhenne J, Frohlich M, et al. Pharmacokinetic interaction of chloroquine and methylene blue combination against malaria. Eur J Clin Pharmacol 2004;60(10):709-15
   PubMed Web of Science ®Google Scholar
• Walter-Sack I, Rengelshausen J, Oberwittler H, et al. High absolute bioavailability of methylene blue given as an aqueous oral formulation. Eur J Clin Pharmacol 2009;65(2):179-89
   PubMed Web of Science ®Google Scholar
• Meissner PE, Mandi G, Witte S, et al. Safety of the methylene blue plus chloroquine combination in the treatment of uncomplicated falciparum malaria in young children of Burkina Faso [ISRCTN27290841]. Malar J 2005;4:45
   PubMed Web of Science ®Google Scholar
• Meissner PE, Mandi G, Coulibaly B, et al. Methylene blue for malaria in Africa: results from a dose-finding study in combination with chloroquine. Malar J 2006;5:84
   PubMedGoogle Scholar
• Bountogo M, Zoungrana A, Coulibaly B, et al. Efficacy of methylene blue monotherapy in semi-immune adults with uncomplicated falciparum malaria: a controlled trial in Burkina Faso. Trop Med Int Health 2010;15(6):713-17
   PubMed Web of Science ®Google Scholar
• Zoungrana A, Coulibaly B, Sie A, et al. Safety and efficacy of methylene blue combined with artesunate or amodiaquine for uncomplicated falciparum malaria: a randomized controlled trial from Burkina Faso. PLoS One 2008;3(2):e1630
   PubMed Web of Science ®Google Scholar
• Coulibaly B, Zoungrana A, Mockenhaupt FP, et al. Strong gametocytocidal effect of methylene blue-based combination therapy against falciparum malaria: a randomised controlled trial. PLoS One 2009;4(5):e5318
   PubMed Web of Science ®Google Scholar
• Coulibaly B, Pritsch M, Bountogo M, et al. Efficacy and safety of triple combination therapy with artesunate-amodiaquine-methylene blue for falciparum malaria in children: a randomised controlled trial in Burkina Faso. J Infect Dis 2014. [ Epub ahead of print]
   Web of Science ®Google Scholar
• Murakawa T, Sakamoto H, Fukada S, et al. Pharmacokinetics of fosmidomycin, a new phosphonic acid antibiotic. Antimicrob Agents Chemother 1982;21(2):224-30
   PubMed Web of Science ®Google Scholar
• Kuemmerle HP, Murakawa T, De Santis F. Pharmacokinetic evaluation of fosmidomycin, a new phosphonic acid antibiotic. Chemioterapia 1987;6(2):113-19
   PubMedGoogle Scholar
• Missinou MA, Borrmann S, Schindler A, et al. Fosmidomycin for malaria. Lancet 2002;360(9349):1941-2
   PubMed Web of Science ®Google Scholar
• Lell B, Ruangweerayut R, Wiesner J, et al. Fosmidomycin, a novel chemotherapeutic agent for malaria. Antimicrob Agents Chemother 2003;47(2):735-8
   PubMed Web of Science ®Google Scholar
• Held J, Zanger P, Issifou S, et al. In vitro activity of tigecycline in Plasmodium falciparum culture-adapted strains and clinical isolates from Gabon. Int J Antimicrob Agents 2010;35(6):587-9
   PubMed Web of Science ®Google Scholar
• Borrmann S, Adegnika AA, Matsiegui PB, et al. Fosmidomycin-clindamycin for Plasmodium falciparum infections in African children. J Infect Dis 2004;189(5):901-8
   PubMed Web of Science ®Google Scholar
• Lell B, Kremsner PG. Clindamycin as an antimalarial drug: review of clinical trials. Antimicrob Agents Chemother 2002;46(8):2315-20
   PubMed Web of Science ®Google Scholar
• Na-Bangchang K, Ruengweerayut R, Karbwang J, et al. Pharmacokinetics and pharmacodynamics of fosmidomycin monotherapy and combination therapy with clindamycin in the treatment of multidrug resistant falciparum malaria. Malar J 2007;6:70
   PubMed Web of Science ®Google Scholar
• Ruangweerayut R, Looareesuwan S, Hutchinson D, et al. Assessment of the pharmacokinetics and dynamics of two combination regimens of fosmidomycin-clindamycin in patients with acute uncomplicated falciparum malaria. Malar J 2008;7:225
   PubMed Web of Science ®Google Scholar
• Oyakhirome S, Issifou S, Pongratz P, et al. Randomized controlled trial of fosmidomycin-clindamycin versus sulfadoxine-pyrimethamine in the treatment of Plasmodium falciparum malaria. Antimicrob Agents Chemother 2007;51(5):1869-71
   PubMed Web of Science ®Google Scholar
• Borrmann S, Lundgren I, Oyakhirome S, et al. Fosmidomycin plus clindamycin for treatment of pediatric patients aged 1 to 14 years with Plasmodium falciparum malaria. Antimicrob Agents Chemother 2006;50(8):2713-18
   PubMed Web of Science ®Google Scholar
• Lanaspa M, Moraleda C, Machevo S, et al. Inadequate efficacy of a new formulation of fosmidomycin-clindamycin combination in Mozambican children less than three years old with uncomplicated Plasmodium falciparum malaria. Antimicrob Agents Chemother 2012;56(6):2923-8
   PubMed Web of Science ®Google Scholar
• Borrmann S, Adegnika AA, Moussavou F, et al. Short-course regimens of artesunate-fosmidomycin in treatment of uncomplicated Plasmodium falciparum malaria. Antimicrob Agents Chemother 2005;49(9):3749-54
   PubMed Web of Science ®Google Scholar
• D’Alessandro U. Progress in the development of piperaquine combinations for the treatment of malaria. Curr Opin Infect Dis 2009;22(6):588-92
   PubMed Web of Science ®Google Scholar
• Phillips MA, Rathod PK. Plasmodium dihydroorotate dehydrogenase: a promising target for novel anti-malarial chemotherapy. Infect Disord Drug Targets 2010;10(3):226-39
   PubMedGoogle Scholar
• Baldwin J, Michnoff CH, Malmquist NA, et al. High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase. J Biol Chem 2005;280(23):21847-53
   PubMed Web of Science ®Google Scholar
• Phillips MA, Gujjar R, Malmquist NA, et al. Triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors with potent and selective activity against the malaria parasite Plasmodium falciparum. J Med Chem 2008;51(12):3649-53
   PubMed Web of Science ®Google Scholar
• Coteron JM, Marco M, Esquivias J, et al. Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential. J Med Chem 2011;54(15):5540-61
   PubMed Web of Science ®Google Scholar
• Hamze A, Rubi E, Arnal P, et al. Mono- and bis-thiazolium salts have potent antimalarial activity. J Med Chem 2005;48(10):3639-43
   PubMed Web of Science ®Google Scholar
• Vial HJ, Wein S, Farenc C, et al. Prodrugs of bisthiazolium salts are orally potent antimalarials. Proc Natl Acad Sci USA 2004;101(43):15458-63
   PubMed Web of Science ®Google Scholar
• Wein S, Maynadier M, Bordat Y, et al. Transport and pharmacodynamics of albitiazolium, an antimalarial drug candidate. Br J Pharmacol 2012;166(8):2263-76
   PubMed Web of Science ®Google Scholar
• Biagini GA, Richier E, Bray PG, et al. Heme binding contributes to antimalarial activity of bis-quaternary ammoniums. Antimicrob Agents Chemother 2003;47(8):2584-9
   PubMed Web of Science ®Google Scholar
• Nicolas O, Margout D, Taudon N, et al. Pharmacological properties of a new antimalarial bisthiazolium salt, T3, and a corresponding prodrug, TE3. Antimicrob Agents Chemother 2005;49(9):3631-9
   PubMed Web of Science ®Google Scholar