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The antimalarial MMV688533 provides potential for single-dose cures with a high barrier to Plasmodium falciparum parasite resistance.
Murithi JM, Pascal C, Bath J, Boulenc X, Gnädig NF, Pasaje CFA, Rubiano K, Yeo T, Mok S, Klieber S, Desert P, Jiménez-Díaz MB, Marfurt J, Rouillier M, Cherkaoui-Rbati MH, Gobeau N, Wittlin S, Uhlemann AC, Price RN, Wirjanata G, Noviyanti R, Tumwebaze P, Cooper RA, Rosenthal PJ, Sanz LM, Gamo FJ, Joseph J, Singh S, Bashyam S, Augereau JM, Giraud E, Bozec T, Vermat T, Tuffal G, Guillon JM, Menegotto J, Sallé L, Louit G, Cabanis MJ, Nicolas MF, Doubovetzky M, Merino R, Bessila N, Angulo-Barturen I, Baud D, Bebrevska L, Escudié F, Niles JC, Blasco B, Campbell S, Courtemanche G, Fraisse L, Pellet A, Fidock DA, Leroy D. Murithi JM, et al. Among authors: bebrevska l. Sci Transl Med. 2021 Jul 21;13(603):eabg6013. doi: 10.1126/scitranslmed.abg6013. Sci Transl Med. 2021. PMID: 34290058 Free PMC article.
A novel multiple-stage antimalarial agent that inhibits protein synthesis.
Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Luksch T, Martínez MS, Luksch T, Bolscher JM, Woodland A, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH. Baragaña B, et al. Among authors: bebrevska l. Nature. 2015 Jun 18;522(7556):315-20. doi: 10.1038/nature14451. Nature. 2015. PMID: 26085270 Free PMC article.
Safety, tolerability, pharmacokinetics, and activity of the novel long-acting antimalarial DSM265: a two-part first-in-human phase 1a/1b randomised study.
McCarthy JS, Lotharius J, Rückle T, Chalon S, Phillips MA, Elliott S, Sekuloski S, Griffin P, Ng CL, Fidock DA, Marquart L, Williams NS, Gobeau N, Bebrevska L, Rosario M, Marsh K, Möhrle JJ. McCarthy JS, et al. Among authors: bebrevska l. Lancet Infect Dis. 2017 Jun;17(6):626-635. doi: 10.1016/S1473-3099(17)30171-8. Epub 2017 Mar 28. Lancet Infect Dis. 2017. PMID: 28363636 Free PMC article. Clinical Trial.
Safety, tolerability, pharmacokinetics, and antimalarial efficacy of a novel Plasmodium falciparum ATP4 inhibitor SJ733: a first-in-human and induced blood-stage malaria phase 1a/b trial.
Gaur AH, McCarthy JS, Panetta JC, Dallas RH, Woodford J, Tang L, Smith AM, Stewart TB, Branum KC, Freeman BB 3rd, Patel ND, John E, Chalon S, Ost S, Heine RN, Richardson JL, Christensen R, Flynn PM, Van Gessel Y, Mitasev B, Möhrle JJ, Gusovsky F, Bebrevska L, Guy RK. Gaur AH, et al. Among authors: bebrevska l. Lancet Infect Dis. 2020 Aug;20(8):964-975. doi: 10.1016/S1473-3099(19)30611-5. Epub 2020 Apr 8. Lancet Infect Dis. 2020. PMID: 32275867 Clinical Trial.
Corrigendum: A novel multiple-stage antimalarial agent that inhibits protein synthesis.
Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Martínez MS, Bolscher JM, Woodland A, Luksch T, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH. Baragaña B, et al. Among authors: bebrevska l. Nature. 2016 Sep 1;537(7618):122. doi: 10.1038/nature18280. Epub 2016 May 25. Nature. 2016. PMID: 27281209 Free article. No abstract available.
Combining SJ733, an oral ATP4 inhibitor of Plasmodium falciparum, with the pharmacokinetic enhancer cobicistat: An innovative approach in antimalarial drug development.
Gaur AH, Panetta JC, Smith AM, Dallas RH, Freeman BB 3rd, Stewart TB, Tang L, John E, Branum KC, Patel ND, Ost S, Heine RN, Richardson JL, Hammill JT, Bebrevska L, Gusovsky F, Maki N, Yanagi T, Flynn PM, McCarthy JS, Chalon S, Guy RK. Gaur AH, et al. Among authors: bebrevska l. EBioMedicine. 2022 Jun;80:104065. doi: 10.1016/j.ebiom.2022.104065. Epub 2022 May 19. EBioMedicine. 2022. PMID: 35598441 Free PMC article. Clinical Trial.
An innovative study design with intermittent dosing to generate a GLP-regulatory package in preclinical species for long lasting molecule M5717, inhibitor of Plasmodium eukaryotic translation elongation factor 2.
Hewitt P, Abla N, Lignet F, Oeuvray C, Bagchus W, Bebrevska L. Hewitt P, et al. Among authors: bebrevska l. Toxicol Appl Pharmacol. 2022 May 15;443:116006. doi: 10.1016/j.taap.2022.116006. Epub 2022 Mar 31. Toxicol Appl Pharmacol. 2022. PMID: 35367236 Free article.
13 results