Repositioning: The fast track to new anti-malarial medicines?

Malaria Journal

Volumn 13, Issue 1, 2014, Pages

  Lotharius, Julie ^a   Gamo Benito, Francisco Javier ^b   Angulo Barturen, Iñigo ^b   Clark, Julie ^c   Connelly, Michele ^c   Ferrer Bazaga, Santiago ^b   Parkinson, Tanya ^d   Viswanath, Pavithra ^e   Bandodkar, Balachandra ^e   Rautela, Nikhil ^e   Bharath, Sowmya ^e   Duffy, Sandra ^f   Avery, Vicky M ^f   Möhrle, Jörg J ^a   Guy, R Kiplin ^c   Wells, Timothy ^a  

^a Medicines for Malaria Venture MMV   (Switzerland)

^b GLAXOSMITHKLINE   (Spain)

^c ST JUDE CHILDREN S RESEARCH HOSPITAL   (United States)

^d Independent Consultant   (United Kingdom)

^e ASTRAZENECA   (United Kingdom)

^f GRIFFITH UNIVERSITY   (Australia)

Author keywords

Anti malarial drugs; Candidate drug re profiling; Drug repositioning; in vitro; in vivo; Malaria; Plasmodium berghei; Plasmodium falciparum

Indexed keywords

AG 024322; AMINOPTERIN; ANTIMALARIAL AGENT; BOSUTINIB; BRADYKININ B2 RECEPTOR ANTAGONIST; CE 245677; CEP 1347; CJ 0231112; CP 631992; CYCLOSPORIN A; CYPROTERONE; DACTINOMYCIN; DIPYRONE; DOXORUBICIN; LAPATINIB; LESTAURTINIB; METHOTREXATE; METHYLENE BLUE; PENTAMIDINE; PIMOZIDE; PIRITREXIM; PRAVASTATIN; PROPAFENONE; PROTEIN TYROSINE KINASE INHIBITOR; SULFAMERAZINE; TIOTIXENE; UK 112214; UNCLASSIFIED DRUG; VALSPODAR; VORINOSTAT;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; CYTOTOXICITY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG REPOSITIONING; DRUG SCREENING; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MALARIA FALCIPARUM; MALE; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; PARASITEMIA; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PLASMODIUM BERGHEI;

ANIMALS; ANTIMALARIALS; DRUG REPOSITIONING; MALARIA; MALARIA, FALCIPARUM; MALE; MICE; MICE, INBRED BALB C; PARASITIC SENSITIVITY TESTS; PLASMODIUM BERGHEI; PLASMODIUM FALCIPARUM;

EID: 84899475908     PISSN: None     EISSN: 14752875     Source Type: Journal    
DOI: 10.1186/1475-2875-13-143     Document Type: Article

References (68)

1. World Health Organization, World Malaria Report 2011 http://www.who.int/ malaria/world-malaria-report-2011/en/
2. World Health Organization, Global Malaria Control and Elimination: report of a technical review http://whqlibdoc.who.int/publications/2008/9789241596756- eng.pdf
3. Malaria. Did they really say eradication? Roberts L, Enserink M, Science 2007 318 1544 1545 10.1126/science.318.5856.1544 18063766
4. New medicines to improve control and contribute to the eradication of malaria. Wells TN, Alonso PL, Gutteridge WE, Nat Rev Drug Discov 2009 8 879 891 10.1038/nrd2972 19834482
5. A research agenda for malaria eradication: drugs. malERA Consultative Group on Drugs, PLoS Med 2011 8 1000402 21311580
6. World Health Organization, Global report on antimalarial drug efficacy and drug resistance: 2000-2010 http://whqlibdoc.who.int/publications/2010/ 9789241500470-eng.pdf
7. Artemisinin resistance-the clock is ticking. White NJ, Lancet 2010 376 2051 2052 10.1016/S0140-6736(10)61963-0 21168039
8. Global phenotypic screening for antimalarials. Guiguemde WA, Shelat AA, Garcia-Bustos JF, Diagana TT, Gamo FJ, Guy RK, Chem Biol 2012 19 116 129 10.1016/j.chembiol.2012.01.004 22284359
9. Thousands of chemical starting points for antimalarial lead identification. Gamo FJ, Sanz LM, Vidal J, de Cozar C, Alvarez E, Lavandera JL, Vanderwall DE, Green DV, Kumar V, Hasan S, Brown JR, Peishoff CE, Cardon LR, Garcia-Bustos JF, Nature 2010 465 305 310 10.1038/nature09107 20485427
10. Chemical genetics of Plasmodium falciparum. Guiguemde WA, Shelat AA, Bouck D, Duffy S, Crowther GJ, Davis PH, Smithson DC, Connelly M, Clark J, Zhu F, Jimenez-Diaz MB, Martinez MS, Wilson EB, Tripathi AK, Gut J, Sharlow ER, Bathurst I, El Mazouni F, Fowble JW, Forquer I, McGinley PL, Castro S, Angulo-Barturen I, Ferrer S, Rosenthal PJ, Derisi JL, Sullivan DJ, Lazo JS, Roos DS, Riscoe MK, et al. Nature 2010 465 311 315 10.1038/nature09099 20485428
11. The European Bioinformatics Institute http://www.ebi.ac.uk/
12. The global pipeline of new medicines for the control and elimination of malaria. Anthony MP, Burrows JN, Duparc S, Moehrle J, Wells TN, Malar J 2012 11 316 10.1186/1475-2875-11-316 22958514
13. Spiroindolones, a potent compound class for the treatment of malaria. Rottmann M, McNamara C, Yeung BK, Lee MC, Zou B, Russell B, Seitz P, Plouffe DM, Dharia NV, Tan J, Cohen SB, Spencer KR, Gonzalez-Paez GE, Lakshminarayana SB, Goh A, Suwanarusk R, Jegla T, Schmitt EK, Beck HP, Brun R, Nosten F, Renia L, Dartois V, Keller TH, Fidock DA, Winzeler EA, Diagana TT, Science 2010 329 1175 1180 10.1126/science.1193225 20813948
14. APT drug R&D: the right active ingredient in the right presentation for the right therapeutic use. Cavalla D, Nat Rev Drug Discov 2009 8 849 853 19713959
15. A novel method of transcriptional response analysis to facilitate drug repositioning for cancer therapy. Jin G, Fu C, Zhao H, Cui K, Chang J, Wong ST, Cancer Res 2012 72 33 44 10.1158/0008-5472.CAN-11-2333 22108825
16. Drug repositioning for orphan diseases. Sardana D, Zhu C, Zhang M, Gudivada RC, Yang L, Jegga AG, Brief Bioinform 2011 12 346 356 10.1093/bib/bbr021 21504985
17. New anti-tuberculosis agents amongst known drugs. Lougheed KE, Taylor DL, Osborne SA, Bryans JS, Buxton RS, Tuberculosis (Edinb) 2009 89 364 370 10.1016/j.tube.2009.07.002 19699151
18. Drug discovery for schistosomiasis: hit and lead compounds identified in a library of known drugs by medium-throughput phenotypic screening. Abdulla MH, Ruelas DS, Wolff B, Snedecor J, Lim KC, Xu F, Renslo AR, Williams J, McKerrow JH, Caffrey CR, PLoS Negl Trop Dis 2009 3 478 10.1371/journal.pntd.0000478 19597541
19. Repositioning of an existing drug for the neglected tropical disease onchocerciasis. Gloeckner C, Garner AL, Mersha F, Oksov Y, Tricoche N, Eubanks LM, Lustigman S, Kaufmann GF, Janda KD, Proc Natl Acad Sci U S A 2010 107 3424 3429 10.1073/pnas.0915125107 20142509
20. The use of the 2 substituted 5-nitroimidazole, Fexinidazole (Hoe 239) in the treatment of chronic T. brucei infections in mice. Jennings FW, Urquhart GM, Z Parasitenkd 1983 69 577 581 10.1007/BF00926669 6636983
21. Fexinidazole - a new oral nitroimidazole drug candidate entering clinical development for the treatment of sleeping sickness. Torreele E, Bourdin Trunz B, Tweats D, Kaiser M, Brun R, Mazue G, Bray MA, Pecoul B, PLoS Negl Trop Dis 4 923 http://www.ncbi.nlm.nih.gov/pubmed/21200426
22. A clinical drug library screen identifies astemizole as an antimalarial agent. Chong CR, Chen X, Shi L, Liu JO, Sullivan DJ Jr, Nat Chem Biol 2006 2 415 416 10.1038/nchembio806 16816845
23. A high-throughput screen targeting malaria transmission stages opens new avenues for drug development. Buchholz K, Burke TA, Williamson KC, Wiegand RC, Wirth DF, Marti M, J Infect Dis 2011 203 1445 1453 10.1093/infdis/jir037 21502082
24. Drug screen targeted at Plasmodium liver stages identifies a potent multistage antimalarial drug. da Cruz FP, Martin C, Buchholz K, Lafuente-Monasterio MJ, Rodrigues T, Sonnichsen B, Moreira R, Gamo FJ, Marti M, Mota MM, Hannus M, Prudencio M, J Infect Dis 2012 205 1278 1286 10.1093/infdis/jis184 22396598
25. Medicines for Malaria Venture: Target Product Proposal 1 Available at: http://www.mmv.org/sites/default/files/uploads/docs/essential-info-for- scientists/TCPs-and-TPPs/TPP1-with-figures.pdf
26. Medicines for Malaria Venture: Target Product Proposal 2 Available at: http://www.mmv.org/sites/default/files/uploads/docs/essential-info-for- scientists/TCPs-and-TPPs/TPP2.pdf
27. Novel, rapid, and inexpensive cell-based quantification of antimalarial drug efficacy. Bennett TN, Paguio M, Gligorijevic B, Seudieu C, Kosar AD, Davidson E, Roepe PD, Antimicrob Agents Chemother 2004 48 1807 1810 10.1128/AAC.48.5.1807-1810.2004 15105139
28. Human malaria parasites in continuous culture. Trager W, Jensen JB, Science 1976 193 673 675 10.1126/science.781840 781840
29. Simple and inexpensive fluorescence-based technique for high-throughput antimalarial drug screening. Smilkstein M, Sriwilaijaroen N, Kelly JX, Wilairat P, Riscoe M, Antimicrob Agents Chemother 2004 48 1803 1806 10.1128/AAC.48.5. 1803-1806.2004 15105138
30. Plasmodium falciparum: assessment of in vitro growth by [3H] hypoxanthine incorporation. Chulay JD, Haynes JD, Diggs CL, Exp Parasitol 1983 55 138 146 10.1016/0014-4894(83)90007-3 6337059
31. Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique. Desjardins RE, Canfield CJ, Haynes JD, Chulay JD, Antimicrob Agents Chemother 1979 16 710 718 10.1128/AAC.16.6.710 394674
32. Malaria Research and Reference Reagent Resource Center (MR4) http://www.mr4.org
33. Development and optimization of a novel 384-well anti-malarial imaging assay validated for high-throughput screening. Duffy S, Avery VM, Am J Trop Med Hyg 2012 86 84 92 10.4269/ajtmh.2012.11-0302 22232455
34. Peters W, Chemotherapy and drug resistance in malaria (vol. 1) London: Academic Press 1987
35. Fast mouse PK (Fast PK): a rapid screening method to increase pharmacokinetic throughput in pre-clinical drug discovery. Reddy J, Madishetti S, Vachaspati PR, Eur J Pharm Sci 2012 47 444 450 10.1016/j.ejps.2012.07.001 22789493
36. A murine model of falciparum-malaria by in vivo selection of competent strains in non-myelodepleted mice engrafted with human erythrocytes. Angulo-Barturen I, Jimenez-Diaz MB, Mulet T, Rullas J, Herreros E, Ferrer S, Jimenez E, Mendoza A, Regadera J, Rosenthal PJ, Bathurst I, Pompliano DL, Gomez De Las Heras F, Gargallo-Viola D, PLoS One 2008 3 2252 10.1371/journal.pone. 0002252 18493601
37. Improved murine model of malaria using Plasmodium falciparum competent strains and non-myelodepleted NOD-scid IL2Rgnull mice engrafted with human erythrocytes. Jimenez-Diaz MB, Mulet T, Viera S, Gomez V, Garuti H, Ibanez J, Alvarez-Doval A, Shultz LD, Martinez A, Gargallo-Viola D, Angulo-Barturen I, Antimicrob Agents Chemother 2009 53 4533 4536 10.1128/AAC.00519-09 19596869
38. Quantitative measurement of Plasmodium-infected erythrocytes in murine models of malaria by flow cytometry using bidimensional assessment of SYTO-16 fluorescence. Jimenez-Diaz MB, Mulet T, Gomez V, Viera S, Alvarez A, Garuti H, Vazquez Y, Fernandez A, Ibanez J, Jimenez M, Gargallo-Viola D, Angulo-Barturen I, Cytometry A 2009 75 225 235 18785271
39. Quinolone-3-diarylethers: a new class of antimalarial drug. Nilsen A, LaCrue AN, White KL, Forquer IP, Cross RM, Marfurt J, Mather MW, Delves MJ, Shackleford DM, Saenz FE, Morrisey JM, Steuten J, Mutka T, Li Y, Wirjanata G, Ryan E, Duffy S, Kelly JX, Sebayang BF, Zeeman AM, Noviyanti R, Sinden RE, Kocken CH, Price RN, Avery VM, Angulo-Barturen I, Jimenez-Diaz MB, Ferrer S, Herreros E, Sanz LM, et al. Sci Transl Med 2013 5 177 137
40. Protein kinases as targets for anti-parasitic chemotherapy. Doerig C, Biochim Biophys Acta 2004 1697 155 168 10.1016/j.bbapap.2003.11.021 15023358
41. Targeting protein kinases in the malaria parasite: update of an antimalarial drug target. Zhang VM, Chavchich M, Waters NC, Curr Top Med Chem 2012 12 456 472 10.2174/156802612799362922 22242850
42. Searching for new antimalarial therapeutics amongst known drugs. Weisman JL, Liou AP, Shelat AA, Cohen FE, Guy RK, DeRisi JL, Chem Biol Drug Des 2006 67 409 416 10.1111/j.1747-0285.2006.00391.x 16882315
43. Mammalian interphase Cdks. Dispensable master regulators of the cell cycle. Enders GH, Genes Cancer 2012 3 11 12
44. Subhashchandra Brahmkshatriya P, Lepsik M, Hajduch M: Aurora kinase inhibitors: Progress towards the clinic. Kollareddy M, Zheleva D, Dzubak P, Invest New Drugs 2012 30 2411 2432 10.1007/s10637-012-9798-6 22350019
45. Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders. Hexner EO, Serdikoff C, Jan M, Swider CR, Robinson C, Yang S, Angeles T, Emerson SG, Carroll M, Ruggeri B, Dobrzanski P, Blood 2008 111 5663 5671 10.1182/blood-2007-04-083402 17984313
46. Antiretrovirals as antimalarial agents. Skinner-Adams TS, McCarthy JS, Gardiner DL, Hilton PM, Andrews KT, J Infect Dis 2004 190 1998 2000 10.1086/425584 15529265
47. The frequency of malaria is similar among women receiving either lopinavir/ritonavir or nevirapine-based antiretroviral treatment. Skinner-Adams TS, Butterworth AS, Porter KA, D'Amico R, Sawe F, Shaffer D, Siika A, Hosseinipour MC, Stringer E, Currier JS, Chipato T, Salata R, Lockman S, Eron JJ, Meshnick SR, McCarthy JS, PLoS One 7 34399
48. Methotrexate and aminopterin lack in vivo antimalarial activity against murine malaria species. Irungu B, Kiboi D, Langat B, Rukunga G, Wittlin S, Nzila A, Exp Parasitol 2009 123 118 121 10.1016/j.exppara.2009.06.007 19527714
49. Methotrexate is highly potent against pyrimethamine-resistant Plasmodium vivax. Imwong M, Russell B, Suwanarusk R, Nzila A, Leimanis ML, Sriprawat K, Kaewpongsri S, Phyo AP, Snounou G, Nosten F, Renia L, J Infect Dis 2011 203 207 210 10.1093/infdis/jiq024 21288820
50. The potential use of methotrexate in the treatment of falciparum malaria: in vitro assays against sensitive and multidrug-resistant falciparum strains. Dar O, Khan MS, Adagu I, Jpn J Infect Dis 2008 61 210 211 18503171
51. Anticancer agents against malaria: time to revisit? Nzila A, Okombo J, Becker RP, Chilengi R, Lang T, Niehues T, Trends Parasitol 2010 26 125 129 10.1016/j.pt.2009.12.002 20056487
52. A phase I trial to evaluate the safety and pharmacokinetics of low-dose methotrexate as an anti-malarial drug in Kenyan adult healthy volunteers. Chilengi R, Juma R, Abdallah AM, Bashraheil M, Lodenyo H, Nyakundi P, Anabwani E, Salim A, Mwambingu G, Wenwa E, Jemutai J, Kipkeu C, Oyoo GO, Muchohi SN, Kokwaro G, Niehues T, Lang T, Nzila A, Malar J 2011 10 63 10.1186/1475-2875-10- 63 21410944
53. Safety and efficacy of methylene blue combined with artesunate or amodiaquine for uncomplicated falciparum malaria: a randomized controlled trial from Burkina Faso. Zoungrana A, Coulibaly B, Sie A, Walter-Sack I, Mockenhaupt FP, Kouyate B, Schirmer RH, Klose C, Mansmann U, Meissner P, Muller O, PLoS One 2008 3 1630 10.1371/journal.pone.0001630 18286187
54. Efficacy of methylene blue monotherapy in semi-immune adults with uncomplicated falciparum malaria: a controlled trial in Burkina Faso. Bountogo M, Zoungrana A, Coulibaly B, Klose C, Mansmann U, Mockenhaupt FP, Burhenne J, Mikus G, Walter-Sack I, Schirmer RH, Sie A, Meissner P, Muller O, Trop Med Int Health 2010 15 713 717 10.1111/j.1365-3156.2010.02526.x 20374561
55. Methylene blue for malaria in Africa: results from a dose-finding study in combination with chloroquine. Meissner PE, Mandi G, Coulibaly B, Witte S, Tapsoba T, Mansmann U, Rengelshausen J, Schiek W, Jahn A, Walter-Sack I, Mikus G, Burhenne J, Riedel KD, Schirmer RH, Kouyate B, Muller O, Malar J 2006 5 84 10.1186/1475-2875-5-84 17026773
56. Haemolysis risk in methylene blue treatment of G6PD-sufficient and G6PD-deficient West-African children with uncomplicated falciparum malaria: a synopsis of four RCTs. Muller O, Mockenhaupt FP, Marks B, Meissner P, Coulibaly B, Kuhnert R, Buchner H, Schirmer RH, Walter-Sack I, Sie A, Mansmann U, Pharmacoepidemiol Drug Saf 2012 22 376 385 23135803
57. Antimalarial activity of the anticancer and proteasome inhibitor bortezomib and its analog ZL3B. Reynolds JM, El Bissati K, Brandenburg J, Gunzl A, Mamoun CB, BMC Clin Pharmacol 2007 7 13 10.1186/1471-2210-7-S1-P13 17956613
58. Effect of cyclosporine on parasitemia and survival of Plasmodium berghei infected mice. Bobbala D, Koka S, Lang C, Boini KM, Huber SM, Lang F, Biochem Biophys Res Commun 2008 376 494 498 10.1016/j.bbrc.2008.09.005 18789889
59. The metabolism of platelet-activating factor in severe and cerebral malaria. Davis TM, Binh TQ, van Phuong N, Sturm M, St John A, Dyer JR, Anh TK, J Infect 1995 31 181 188 10.1016/S0163-4453(95)80024-7 8586836
60. Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole. Zhou Z, Vorperian VR, Gong Q, Zhang S, January CT, J Cardiovasc Electrophysiol 1999 10 836 843 10.1111/j.1540-8167.1999.tb00264.x 10376921
61. The role of antimalarial agents in the treatment of SLE and lupus nephritis. Lee SJ, Silverman E, Bargman JM, Nat Rev Nephrol 2011 7 718 729 10.1038/nrneph.2011.150 22009248
62. Hydroxychloroquine: from malaria to autoimmunity. Ben-Zvi I, Kivity S, Langevitz P, Shoenfeld Y, Clin Rev Allergy Immunol 2012 42 145 153 10.1007/s12016-010-8243-x 21221847
63. Chloroquine and its analogs: a new promise of an old drug for effective and safe cancer therapies. Solomon VR, Lee H, Eur J Pharmacol 2009 625 220 233 10.1016/j.ejphar.2009.06.063 19836374
64. Antitumor activity of artemisinin and its derivatives: from a well-known antimalarial agent to a potential anticancer drug. Crespo-Ortiz MP, Wei MQ, J Biomed Biotechnol 2012 2012 247597 22174561
65. Antimalarials in the treatment of schistosomiasis. Keiser J, Utzinger J, Curr Pharm Des 2012 18 3531 3538 22607145
66. Artemisinin derivatives: a patent review (2006-present). Njuguna NM, Ongarora DS, Chibale K, Expert Opin Ther Pat 2012 22 1179 1203 10.1517/13543776.2012.724063 22971128
67. Drug repositioning in the treatment of malaria and TB. Nzila A, Ma Z, Chibale K, Future Med Chem 2011 3 1413 1426 10.4155/fmc.11.95 21879845
68. Road towards new antimalarials-overview of the strategies and their chemical progress. Wu T, Nagle AS, Chatterjee AK, Curr Med Chem 2011 18 853 871 10.2174/092986711794927748 21182479