References
- Nagle A, Wu T, Kuhen K, et al. Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. J Med Chem. 2012;55(9):4244–4273.
- Diagana TT. Supporting malaria elimination with 21st century antimalarial agent drug discovery. Drug Discov Today. 2015;20(10):1265–1270.
- Held J, Jeyaraj S, Kreidenweiss A, et al. Antimalarial compounds in phase II clinical development. Expert Opion Investigational Drugs. 2015;24(3):363–382.
- Mischlinger J, Agnandji ST, Ramharter A. Single dose treatment of malaria - current status and perspectives. Expert Rev Anti Infect Ther. 2016;14(7):669–678.
- Bhagavathula AS, Elnour AA, Shehab A. Alternatives to currently used antimalarial drugs: in search of a magic bullet. Infect Dis Poverty. 2016;5(103).
- World Malaria Report 2017. Geneva: World Health Organization; 2017. License: CC BY-NC-SA 3.0 IGO
- WHO 2015. WHO guidelines for the treatment of malaria. 3rd ed. Geneva: World Health Organization; 2015.
- Ménard D, Khim N, Beghain J, et al. A worldwide map of Plasmodium falciparum K13-propeller polymorphisms. N Engl J Med. 2016;374:2453–2464.
- Ouji M, Augereau JM, Paloque L, et al. Plasmodium falciparum resistance to artemisinin-based combination therapies: a sword of Damocles in the path toward malaria elimination. Parasite. 2018;25:24.
- Thu AM, Phyo AP, Landier J, et al. Combating multidrug-resistant Plasmodium falciparum malaria. FEBS J. 2017;284:2569–2578.
- Kuhen K, Chatterjee A, 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):5060–5067.
- Burrows JN, Duparc S, Gutteridge WE, et al. New developments in anti-malarial target candidate and product profiles. Malar J. 2017;16:1.
- Magistrado P, Corey V, Lukens A, et al. Plasmodium falciparum cyclic amine resistance locus (PfCARL), a resistance mechanism for two distinct compound classes. ACS Infect Dis. 2016;2(11):816–826.
- Dembele L, Gupta DK, Lim MYX, et al. Imidazolopiperazines kill both rings and dormant rings in wild-type and K13 artemisin-resistant Plasmodium falciparum in vitro. Antimicr Agents Chemother. 2018;62:e02235–17.
- Huskey S, Forseth R, Li H, et al. Utilization of stable isotope labeling to facilitate the identification of polar metabolites of KAF156, an antimalarial agent. Drug Metabolism and Disposition. 2016;44(10):1697–1708.
- Leong F, 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):6437–6443.
- Leong F, Jain J, Feng Y, et al. A phase 1 evaluation of the pharmacokinetic/pharmacodynamic interaction of the anti-malarial agents KAF156 and piperaquine. Malar J. 2018;17:1.
- White N, Duong T, Uthaisin C, et al. Antimalarial activity of KAF156 in falciparum and vivax malaria. New England J Med. 2016;375(12):1152–1160.
- Nsanzabana C, Djalle D, Guérin PJ, et al. Tools for surveillance of anti-malarial drug resistance: an assessment of the current landscape. Malar J. 2018;17:1.
- Ross LS, Dhingra SK, Mok S, et al. Emerging Southeast Asian pfcrt mutations confer Plasmodium falciparum resistance to the first-line antimalarial piperaquine. Nat Commun. 2018;17:3314.
- EMA. Summary of Eurartesim® product characteristics. [cited 2018 Jul 5]. Available from:http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/001199/WC500118113.pdf
- Jain J, Leong F, Chen L, et al. Bioavailability of lumefantrine is significantly enhanced with a novel formulation approach, an outcome from a randomized, open-label pharmacokinetic study in healthy volunteers. Antimicrob Agents Chemother. 2017;61:9.
- Clinicaltrials.gov. Efficacy and safety of KAF156 in combination with LUM-SDF in adults and children with uncomplicated Plasmodium falciparum malaria; [ Updated 2018 May 8; cited 2018 Apr 4]. Available from: https://clinicaltrials.gov/ct2/show/NCT03167242
- Lim M, LaMonte G, Lee M, et al. UDP-galactose and acetyl-CoA transporters as Plasmodium multidrug resistance genes. Nat Microbiol. 2016;1. doi:10.1038/nmicrobiol.2016.166 [Epub ahead of print]
- [cited 2018 Sept 8]. Available from: https://www.mmv.org/research-development/project-portfolio/kaf156-lumefantrine