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Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose–Efficacy Modeling


Sergio Wittlin and colleagues report in vivo and in vitro modelling of antimalarial activity and dose-efficacy of a new drug candidate.


Vyšlo v časopise: Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose–Efficacy Modeling. PLoS Med 13(10): e32767. doi:10.1371/journal.pmed.1002138
Kategorie: Research Article
prolekare.web.journal.doi_sk: https://doi.org/10.1371/journal.pmed.1002138

Souhrn

Sergio Wittlin and colleagues report in vivo and in vitro modelling of antimalarial activity and dose-efficacy of a new drug candidate.


Zdroje

1. World Malaria Report 2015. 2015;280.

2. Gamo F-J, Sanz LM, Vidal J, de Cozar C, Alvarez E, Lavandera J-L, et al. Thousands of chemical starting points for antimalarial lead identification. Nature. 2010;465(7296):305–10. doi: 10.1038/nature09107 20485427

3. Wells TNC. New Medicines to Combat Malaria: An Overview of the Global Pipeline of Therapeutics. Treat Prev Malar. 2012;281–307. http://link.springer.com/10.1007/978-3-0346-0480-2

4. Brunner R, Aissaoui H, Boss C, Bozdech Z, Brun R, Corminboeuf O, et al. Identification of a new chemical class of antimalarials. J Infect Dis. 2012;206:735–43. doi: 10.1093/infdis/jis418 22732921

5. Brunner R, Ng CL, Aissaoui H, Akabas MH, Boss C, Brun R, et al. UV-triggered affinity capture identifies interactions between the Plasmodium falciparum multidrug resistance protein 1 (PfMDR1) and antimalarial agents in live parasitized cells. J Biol Chem. 2013;288(31):22576–83. doi: 10.1074/jbc.M113.453159 23754276

6. Ng CL, Siciliano G, Lee MCS, Almeida MJ De, Corey VC, Bopp SE, et al. CRISPR-Cas9-modified pfmdr1 protects Plasmodium falciparum asexual blood stages and gametocytes against a class of piperazine-containing compounds but potentiates artemisinin-based combination therapy partner drugs. Mol Microbiol. 2016;1–35.

7. Burrows JN, van Huijsduijnen RH, Möhrle JJ, Oeuvray C, Wells TNC. Designing the next generation of medicines for malaria control and eradication. Malar J. 2013;12:187. http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=3685552&tool=pmcentrez&rendertype=abstract doi: 10.1186/1475-2875-12-187 23742293

8. Leroy D, Campo B, Ding X, Jeremy, Burrows N, Cherbuin S. Defining the biology component of the drug discovery strategy for malaria eradication. Trends Parasitol. 2014;30(10): 478–90.

9. Snyder C, Chollet J, Santo-Tomas J, Scheurer C, Wittlin S. In vitro and in vivo interaction of synthetic peroxide RBx11160 (OZ277) with piperaquine in Plasmodium models. Exp Parasitol. 2007;115:296–300. 17087929

10. Schleiferböck S, Scheurer C, Ihara M, Itoh I, Bathurst I, Burrows JN, et al. In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models. Drug Des Devel Ther. 2013;7:1377–84. doi: 10.2147/DDDT.S51298 24255594

11. Witkowski B, Amaratunga C, Khim N, Sreng S, Chim P, Kim S, et al. Novel phenotypic assays for the detection of artemisinin-resistant Plasmodium falciparum malaria in Cambodia: In-vitro and ex-vivo drug-response studies. Lancet Infect Dis. 2013;13(13):1043–9. http://dx.doi.org/10.1016/S1473-3099(13)70252-4

12. Straimer J, Gnädig NF, Witkowski B, Amaratunga C, Duru V, Ramadani AP, et al. K13-propeller mutations confer artemisinin resistance in Plasmodium falciparum clinical isolates. Science. 2014;2624(1985):428–31.

13. Ratcliff A, Siswantoro H, Kenangalem E, Wuwung M, Brockman A, Edstein MD, et al. Therapeutic response of multidrug-resistant Plasmodium falciparum and P. vivax to chloroquine and sulfadoxine-pyrimethamine in southern Papua, Indonesia. Trans R Soc Trop Med Hyg. 2007;101(4):351–9. 17028048

14. Hasugian AR, Purba HLE, Kenangalem E, Wuwung RM, Ebsworth EP, Maristela R, et al. Dihydroartemisinin-piperaquine versus artesunate-amodiaquine: superior efficacy and posttreatment prophylaxis against multidrug-resistant Plasmodium falciparum and Plasmodium vivax malaria. Clin Infect Dis. 2007;44(8):1067–74. http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=2532501&tool=pmcentrez&rendertype=abstract 17366451

15. Hasugian AR, Tjitra E, Ratcliff A, Siswantoro H, Kenangalem E, Wuwung RM, et al. In vivo and in vitro efficacy of amodiaquine monotherapy for treatment of infection by chloroquine-resistant plasmodium vivax. Antimicrob Agents Chemother. 2009;53(3):1094–9. doi: 10.1128/AAC.01511-08 19104023

16. Sanz LM, Crespo B, De-Cózar C, Ding XC, Llergo JL, Burrows JN, et al. P. falciparum in vitro killing rates allow to discriminate between different antimalarial mode-of-action. PLoS ONE. 2012;7(2).

17. Desjardins RE, Canfield CJ, Haynes JD, Chulay JD. Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique. Antimicrob Agents Chemother. 1979;16(6):710–8. 394674

18. Charman S, Arbe-Barnes S, Bathurst IC, Brun R, Campbell M, Charman WN, et al. Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria. Proc Natl Acad Sci U S A. 2011;108:4400–5. doi: 10.1073/pnas.1015762108 21300861

19. Fidock D a, Rosenthal PJ, Croft SL, Brun R, Nwaka S. Antimalarial drug discovery: efficacy models for compound screening. Nat Rev Drug Discov. 2004;3(6):509–20. 15173840

20. Angulo-Barturen I, Jiménez-Díaz MB, Mulet T, Rullas J, Herreros E, Ferrer S, 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. 2008;3(5).

21. Jiménez-Díaz MB, Mulet T, Viera S, Gómez V, Garuti H, Ibáñez J, et al. Improved murine model of malaria using Plasmodium falciparum competent strains and non-myelodepleted NOD-scid IL2Rγnull mice engrafted with human erythrocytes. Antimicrob Agents Chemother. 2009;53(10):4533–6. doi: 10.1128/AAC.00519-09 19596869

22. Ruecker a., Mathias DK, Straschil U, Churcher TS, Dinglasan RR, Leroy D, et al. A Male and Female Gametocyte Functional Viability Assay To Identify Biologically Relevant Malaria Transmission-Blocking Drugs. Antimicrob Agents Chemother. 2014;58(12):7292–302. doi: 10.1128/AAC.03666-14 25267664

23. Baragaña B, Hallyburton I, Lee MCS, Norcross NR, Grimaldi R, Otto TD, et al. A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature. 2015;522(7556):315–20. http://www.nature.com/doifinder/10.1038/nature14451 doi: 10.1038/nature14451 26085270

24. Maerki S, Brun R, Charman S a., Dorn A, Matile H, Wittlin S. In vitro assessment of the pharmacodynamic properties and the partitioning of OZ277/RBx-11160 in cultures of Plasmodium falciparum. J Antimicrob Chemother. 2006;58(1):52–8. 16735432

25. Peatey CL, Leroy D, Gardiner DL, Trenholme KR. Anti-malarial drugs: how effective are they against Plasmodium falciparum gametocytes? Malar J. 2012;11(1):34.

26. Bousema T, Okell L, Shekalaghe S, Griffin JT, Omar S, Sawa P, 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. 2010;9:136. doi: 10.1186/1475-2875-9-136 20497536

27. Delves MJ, Ruecker A, Straschil U, Lelièvre J, Marques S, López-Barragán MJ, et al. Male and female Plasmodium falciparum mature gametocytes show different responses to antimalarial drugs. Antimicrob Agents Chemother. 2013;57(7):3268–74. doi: 10.1128/AAC.00325-13 23629698

28. Kolk MVANDER, Vlas SJDE, Saul A. Evaluation of the standard membrane feeding assay (SMFA) for the determination of malaria transmission-reducing activity using empirical data. Parasitology. 2005;130:13–22. 15700753

29. Churcher TS, Blagborough AM, Delves M, Ramakrishnan C, Kapulu MC, Williams AR, et al. Measuring the blockade of malaria transmission—An analysis of the Standard Membrane Feeding Assay. Int J Parasitol. 2012;42(11):1037–44. doi: 10.1016/j.ijpara.2012.09.002 23023048

30. Bruderer S, Hurst N, de Kanter R, Miraval T, Pfeifer T, Donazzolo Y, et al. First-in-Humans Study of the Safety, Tolerability, and Pharmacokinetics of ACT-451840, a New Chemical Entity with Antimalarial Activity. Antimicrob Agents Chemother. 2015;59(2):935–42. http://aac.asm.org/lookup/doi/10.1128/AAC.04125-14 doi: 10.1128/AAC.04125-14 25421475

31. Rottmann M, McNamara C, Yeung BKS, Lee MCS, Zou B, Russell B, et al. Spiroindolones, a potent compound class for the treatment of malaria. Science. 2010;329 (September):1175–80.

32. Meister S, Plouffe DM, Kuhen KL, Bonamy GMC, Wu T, Barnes SW, et al. Imaging of Plasmodium Liver Stages to Drive Next-Generation Antimalarial Drug Discovery. Science. 2011;334:1372–7.

33. Phillips MA, Lotharius J, Marsh K, White J, Dayan A, White KL, et al. A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria. Sci Transl Med. 2015;7(296):296ra111. http://stm.sciencemag.org/content/7/296/296ra111 doi: 10.1126/scitranslmed.aaa6645 26180101

34. Krause A, Dingemanse J, Mathis A, Marquart L, Möhrle JJ, McCarthy JS. Pharmacokinetic/pharmacodynamic modelling of the antimalarial effect of Actelion-451840 in an induced blood stage malaria study in healthy subjects. Br J Clin Pharmacol. 2016;9. Available from: http://doi.wiley.com/10.1111/bcp.12962

35. Lakshminarayana SB, Freymond C, Fischli C, Yu J, Weber S, Goh A, et al. Pharmacokinetic-Pharmacodynamic Analysis of Spiroindolone Analogs and KAE609 in a Murine Malaria Model. Antimicrob Agents Chemother. 2015;59(2):1200–10. http://aac.asm.org/lookup/doi/10.1128/AAC.03274-14 doi: 10.1128/AAC.03274-14 25487807

36. Kuhen KL, Chatterjee AK, Rottmann M, Gagaring K, Borboa R, Buenviaje J, 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. doi: 10.1128/AAC.02727-13 24913172

37. Medhi B, Patyar S, Rao RS, Byrav Ds P, Prakash A. Pharmacokinetic and toxicological profile of artemisinin compounds: An update. Pharmacology. 2009;84(6):323–32. doi: 10.1159/000252658 19851082

38. Moehrle JJ, Duparc S, Siethoff C, van Giersbergen PLM, Craft JC, Arbe-Barnes S, 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):535–48.

39. Price R, Van Vugt M, Nosten F, Luxemburger C, Brockman A, Phaipun L, et al. Artesunate versus artemether for the treatment of recrudescent multidrug-resistant falciparum malaria. Am J Trop Med Hyg. 1998;59(6):883–8. 9886194

40. Price R, Luxemburger C, van Vugt M, Nosten F, Kham a, Simpson J, et al. Artesunate and mefloquine in the treatment of uncomplicated multidrug- resistant hyperparasitaemic falciparum malaria. Trans R Soc Trop Med Hyg. 1998;92:207–11. http://www.ncbi.nlm.nih.gov/htbin-post/Entrez/query?db=m&form=6&dopt=r&uid=0009764335 9764335

41. White N. Antimalarial drug resistance and combination chemotherapy. Philos Trans R Soc Lond B Biol Sci. 1999;354(1384):739–49. 10365399

42. Van Vugt M, Wilairatana P, Gemperli B, Gathmann I, Phaipun L, Brockman a., et al. Efficacy of six doses of artemether-lumefantrine (benflumetol) in multidrug-resistant Plasmodium falciparum malaria. Am J Trop Med Hyg. 1999;60(6):936–42. 10403324

43. Lefèvre G, Looareesuwan S, Treeprasertsuk S, Krudsood S, Silachamroon U, Gathmann I, et al. A clinical and pharmacokinetic trial of six doses of artemether-lumefantrine for multidrug-resistant Plasmodium falciparum malaria in Thailand. Am J Trop Med Hyg. 2001;64(5):247–56.

44. Djimdé A, Lefèvre G. Understanding the pharmacokinetics of Coartem. Malar J. 2009;8 Suppl 1:S4. doi: 10.1186/1475-2875-8-S1-S4 19818171

45. McCarthy JS, Sekuloski S, Griffin PM, Elliott S, Douglas N, Peatey C, et al. A pilot randomised trial of induced blood-stage Plasmodium falciparum infections in healthy volunteers for testing efficacy of new antimalarial drugs. PLoS ONE. 2011;6(8):6–13.

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