Challenges in antimalarial drug discovery

Future Medicinal Chemistry

Volumn 3, Issue 11, 2011, Pages 1401-1412

  Burrows, Jeremy N ^a   Leroy, Didier ^a   Lotharius, Julie ^a   Waterson, David ^a  

^a Medicines for Malaria Venture   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIMALARIAL AGENT; ARTEMISININ; ARTESUNATE; MEFLOQUINE;

ANTIMALARIAL ACTIVITY; ASEXUAL REPRODUCTION; DISEASE TRANSMISSION; DRUG HALF LIFE; HUMAN; IN VITRO STUDY; IN VIVO STUDY; MALARIA; NONHUMAN; PLASMODIUM FALCIPARUM; PLASMODIUM VIVAX; PRIORITY JOURNAL; REVIEW;

ANIMALS; ANTIMALARIALS; CHEMISTRY, PHARMACEUTICAL; DRUG DISCOVERY; HUMANS; MALARIA; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 80052405122     PISSN: 17568919     EISSN: 17568927     Source Type: Journal    
DOI: 10.4155/fmc.11.91     Document Type: Review

References (43)

1. Wells TNC, Alonso PL, Gutteridge WE. New medicines to improve control and contribute to the eradication of malaria. Nat. Rev. Drug Disc. 8, 879-891 (2009).
2. Olliaro P, Wells TNC. The global portfolio of new antimalarial medicines under development. Clin. Pharm. Ther. 85(6), 584-595 (2009).
3. Bathurst I, Hentschel C. Medicines for Malaria Venture: sustaining antimalarial drug development. Trends Parasit. 22(7), 301-307 (2009). (Pubitemid 43949613)
4. Alonso PL, Brown G, Arevalo-Herrera M et al. A research agenda for malaria eradication: drugs. PLoS medicine. 8(1), e1000406 (2011).
5. Fidock DA, Rosenthal PJ, Croft SA, Brun R, Nwaka S. Antimalarial drug discovery: efficacy models for compound screening. Nat. Rev. Drug Discov. 3, 509-520 (2004). (Pubitemid 38807533)
6. Burrows JN, Waterson D. Discovering new medicines to control and eradicate malaria. In:Diseases of the Developing World . Elliot R (Ed.).Springer, Washington, DC, USA (2011).
7. Gamo FJ, Sanz LM, Vidal J et al. Thousands of chemical starting points for antimalarial lead identification. Nature 465, 305-310 (2010).
8. Plouffe D, Brinker A, McNamara C et al. In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. PNAS 105(26), 9059-9064 (2008).
9. Guiguemde WA, Shelat AA, Bouck D et al. Chemical genetics of Plasmodium falciparum. Nature 465, 311-315 (2010).
10. Lipinski CA, Lombardo F, Dominy BW, Feeney PJ. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Deliv. Rev. 23, 3-25 (1997). (Pubitemid 27046991)
11. Ridgway D, Tuszynski JA, Tam YK. reassessing models of hepatic extraction. J. Biol. Phys. 29(1), 1-21 (2003). (Pubitemid 36356284)
12. Fry JR. The metabolism of drugs by isolated hepatocytes. Q. Rev. Drug Metab. Drug Interact. 4, 99-122 (1982).
13. Peters W, Robinson BL. Malaria In:Handbook of Animal Models of Infection. Zak O, Sande M (Eds).Academic Press, London, UK 757-773 (1999).
14. Angulo-Barturen I, Jimenez-Diaz MB, Mulet T et al. A murine model of falciparum-malaria by in vivo selection of competent strains in non-myelodepleted mice engrafted with human erythrocytes. PloS one. 3(5), e2252 (2008).
15. Lagrutta AA, Trepakova ES, Salata JJ. The hERG channel and risk of drug-acquired cardiac arrhythmia: an overview. Curr. Topics Med. Chem. 8(13), 1102-1112 (2008).
16. Kirkland D, Reeve L, Gatehouse D, Vanparys P. A core in vitro genotoxicity battery comprising the Ames test plus the in vitro micronucleus test is sufficient to detect rodent carcinogens and in vivo genotoxins. Mutat. Res. 721(1), 27-73 (2011).
17. Hamon J, Whitebread S, Techer-Etienne V, Le Coq H, Azzaoui K, Urban L. In vitro safety pharmacology profiling: what else beyond hERG? Future Med. Chem. 1(4), 645-665 (2009).
18. Sinden RE. Malaria, sexual development and transmission: retrospect and prospect. Parasitology 136(12), 1427-1434 (2009).
19. Bousema T, Okell L, Shekalaghe S et al. Revisiting the circulation time of Plasmodium falciparum gametocytes: molecular detection methods to estimate the duration of gametocyte carriage and the effect of gametocytocidal drugs. Malar. J. 9, 136 (2010).
20. Delves M, Sinden RE. A semi-automated method for counting fluorescent malaria oocysts increases the throughput of transmission blocking studies. Malar. J. 9, 35 (2010).
21. Buchholz K, Burke TA, Williamson KC, Wiegand RC, Wirth DF, Marti M. A high-throughput screen targeting malaria transmission stages opens new avenues for drug development. J. Infect. Dis. 203 (10), 1445-1453 (2011).
22. Tanaka TQ, Williamson KC. A malaria gametocytocidal assay using oxidoreduction indicator, alamarBlue. Mol. Biochem. Parasitol. 177(2), 160-163 (2011).
23. Rodríguez MC, Margos G, Compton H et al. Plasmodium berghei: routine production of pure gametocytes, extracellular gametes, zygotes, and ookinetes. Exp. Parasitol. 101, 73-76 (2002). (Pubitemid 36279306)
24. Peatey CL, Skinner-Adams TS, Dixon MWA, McCarthy JS, Gardiner DL, Trenholme KR. Effect of antimalarial drugs on Plasmodium falciparum gametocytes. J. Infect. Dis. 200(10), 1518-1521 (2009).
25. Mazier D, Beaudoin RL, Mellouk S et al. Complete development of hepatic stages of Plasmodium falciparum in vitro. Science 227(4685), 440-442 (1985). (Pubitemid 15153505)
26. Ploemen IHJ, Prudencio M, Douradinha BG et al. Visualisation and quantitative analysis of the rodent malaria liver stage by real time imaging. PloS one. 4(11), e7881 (2009).
27. Price RN, Tjiltra E, Guerra CA, Yeung S, White NJ, Anstey NM. Vivax malaria: neglected and not benign. Am. J. Trop. Med. Hyg. 77 (Suppl. 6), 79-87 (2007).
28. Wells TNC, Burrows JN, Baird JK. Targeting the hypnozoite reservoir of Plasmodium vivax: the hidden obstacle to malaria elimination. Trends Parasit. 26(3), 145-151 (2010).
29. Mazier D, Landau I, Druilhe P et al. Cultivation of the liver forms of Plasmodium vivax in human hepatocytes. Nature 307(5949), 367-369 (1984). (Pubitemid 14134063)
30. Chattopadhyay R, Velmurugan S, Chakiath C et al. Establishment of an in vitro assay for assessing the effects of drugs on the liver stages of Plasmodium vivax malaria. PLoS One 5(12), e14275 (2010).
31. Carraz M, Jossang A, Rasoanaivo P, Mazier D, Frappier F. Isolation and antimalarial activity of new morphinan alkaloids on Plasmodium yoelii liver stage. Bioorg. Med. Chem. 16(11), 6186-6192 (2008). (Pubitemid 351766715)
32. Mwakingwe A, Ting LM, Hochman S, Chen J, Sinnis P, Kim K. Noninvasive real-time monitoring of liver-stage development of bioluminescent Plasmodium parasites. J. Inf. Dis. 200(9), 1470-1478 (2009).
33. Gego A, Silvie O, Franetich JF et al. New approach for high-throughput screening of drug activity on Plasmodium liver stages. Antimicrob. Agents Ch. 50(4), 1586-1589 (2006).
34. Westenberger SJ, McClean CM, Chattopadhyay R et al. A systems-based analysis of Plasmodium vivax lifecycle transcription from human to mosquito. PLoS Negl. Trop. Dis. 4(4), e653 (2010).
35. Dembele L, Gego A, Zeeman AM. Towards an in vitro model of Plasmodium hypnozoites suitable for drug discovery. PLoS One 6(3), e18162 (2011).
36. Schmidt LH. Relationships between chemical structures of 8-aminoquinolines and their capacities for radical cure of infections with Plasmodium cynomolgi in rhesus monkeys. Antimicrob. Agents Ch. 615-652 (1983). (Pubitemid 14203859)
37. Bass A, Kinter L, Williams P. Origins, practices and future of safety pharmacology. J. Pharmacol. Toxicol. Methods 49(3), 145-151 (2004). (Pubitemid 38686652)
38. Young RD, Rathod PK. Clonal viability measurements on Plasmodium falciparum to assess in vitro schizonticidal activity of leupeptin, chloroquine, and 5-fluoroorotate. Antimicrob. Agents Ch. 37(5), 1102-1107 (1993). (Pubitemid 23141327)
39. Painter HJ, Morrisey JM, Vaidya AB. Mitochondrial electron transport inhibition and viability of intraerythrocytic Plasmodium falciparum. Antimicrob. Agents Chemother. 54(12), 5281-5287 (2010).
40. Barnes KI, Watkins WM, White NJ. Antimalarial dosing regimens and drug resistance. Trends Parasit. 24(3), 127-134 (2008).
41. Ambrose PG, Bhavnani SM, Rubino CM et al. Pharmacokinetics- pharmacodynamics of antimicrobial therapy: it's not just for mice anymore. Clin. Infect. Dis. 44(1), 79-86 (2007). (Pubitemid 44968990)
42. Rathod PK, Mcerlean T, Lee PC. Variations in frequencies of drug resistance in Plasmodium falciparum. PNAS 94(17), 9389-9393 (1997). (Pubitemid 27357839)
43. Simpson JA, Watkins ER, Price RN, Aarons L, Kyle DE, White NJ. Mefloquine pharmacokinetic-pharmacodynamic models: implications for dosing and resistance. Antimicrob. Agents Chemother. 44, 3414-3424 (2000). (Pubitemid 33009503)