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Published in: Drugs 7/2016

01-05-2016 | Review Article

Naphthoquine: An Emerging Candidate for Artemisinin Combination Therapy

Authors: Brioni R. Moore, Moses Laman, Sam Salman, Kevin T. Batty, Madhu Page-Sharp, Francis Hombhanje, Laurens Manning, Timothy M. E. Davis

Published in: Drugs | Issue 7/2016

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Abstract

Naphthoquine is a 4-aminoquinoline antimalarial drug first synthesised in China in 1986 but which was not developed for clinical use until the late 1990s. Early in vitro parasite sensitivity and in vivo efficacy data, together with a long terminal elimination half-life (up to 23 days), suggested that it could be used as monotherapy for uncomplicated falciparum and vivax malaria, but is now marketed as a single-dose, fixed co-formulation with artemisinin in a milligram per kilogram ratio of 1:2.5. This form of artemisinin combination therapy (ACT) has also shown high cure rates, especially in two randomised trials in which, consistent with World Health Organization recommendations for all ACTs, it was administered daily for 3 days rather than as single dose for Plasmodium falciparum and P. vivax infections (28-day adequate clinical and parasitological response ≥98.4 %). Although detailed safety monitoring has been performed in a minority of subjects, >4000 healthy volunteers and patients with malaria have been exposed to naphthoquine without any documented significant toxicity. As with other 4-aminoquinolines, naphthoquine is associated with prolongation of the electrocardiographic QT interval but not with cardiac or neurological events. It has been administered to children as young as 4 months of age but, due to a lack of pharmacokinetic, efficacy and toxicity data in young infants and in pregnant/lactating women, it should not be used in these vulnerable patient groups.With the emergence of parasite resistance to other ACTs, naphthoquine partnered with a potent artemisinin derivative may prove a viable alternative treatment for uncomplicated malaria.
Literature
2.
go back to reference Muregi FW. Antimalarial drugs and their useful therapeutic lives: rational drug design lessons from pleiotropic action of quinolines and artemisinins. Curr Drug Discov Technol. 2010;7(4):280–316.CrossRefPubMed Muregi FW. Antimalarial drugs and their useful therapeutic lives: rational drug design lessons from pleiotropic action of quinolines and artemisinins. Curr Drug Discov Technol. 2010;7(4):280–316.CrossRefPubMed
3.
go back to reference Wang JY, Cao WC, Shan CQ, Zhang M, Li GF, Ding DB, et al. Naphthoquine phosphate and its combination with artemisinine. Acta Trop. 2004;89(3):375–81.CrossRefPubMed Wang JY, Cao WC, Shan CQ, Zhang M, Li GF, Ding DB, et al. Naphthoquine phosphate and its combination with artemisinine. Acta Trop. 2004;89(3):375–81.CrossRefPubMed
4.
go back to reference Deng RX. Recent progress in research on antimalarials in China. Chin J Pharm. 1989;20:372–6. Deng RX. Recent progress in research on antimalarials in China. Chin J Pharm. 1989;20:372–6.
5.
go back to reference Law XX. Progress in clinical research on naphthoquine phosphate for treatment of malaria. Shanghai Pharm J. 2004;4(25):160–1. Law XX. Progress in clinical research on naphthoquine phosphate for treatment of malaria. Shanghai Pharm J. 2004;4(25):160–1.
6.
go back to reference Wang JY, Shan CQ, Fu DD, Sun ZW, Ding DB. Efficacy of naphthoquine, artemisinine and a combination of the two drugs in the treatment of falciparum malaria. Chin J Parasitol Parasit Dis. 2003;21(3):131–3. Wang JY, Shan CQ, Fu DD, Sun ZW, Ding DB. Efficacy of naphthoquine, artemisinine and a combination of the two drugs in the treatment of falciparum malaria. Chin J Parasitol Parasit Dis. 2003;21(3):131–3.
7.
go back to reference Shan CQ, Wang JY, Ding DB, Sun ZW. Efficacy of naphthoquine phosphate, artemisinine and a combination of the two drug in the treatment of falciparum malaria. Acta Parasitologica et Medica Entomologica Sinica. 2005;12(2):90–2. Shan CQ, Wang JY, Ding DB, Sun ZW. Efficacy of naphthoquine phosphate, artemisinine and a combination of the two drug in the treatment of falciparum malaria. Acta Parasitologica et Medica Entomologica Sinica. 2005;12(2):90–2.
8.
go back to reference Li CF, Che LG, Yang CZ, Tao DZ. Effect of naphthoquine phosphate against malaria. J Pract Parasit Dis. 1998;6(2):58–9. Li CF, Che LG, Yang CZ, Tao DZ. Effect of naphthoquine phosphate against malaria. J Pract Parasit Dis. 1998;6(2):58–9.
9.
go back to reference Li XL, Che LG, Li CF. Observation on the effectiveness of naphthoquine phosphate tablets on patients with vivax malaria and falciparum malaria. Chin Trop Med. 2003;3(5):608–9. Li XL, Che LG, Li CF. Observation on the effectiveness of naphthoquine phosphate tablets on patients with vivax malaria and falciparum malaria. Chin Trop Med. 2003;3(5):608–9.
10.
go back to reference Li XL, Li CZ, He W, Dao QY. The treating effect of naphthoquine phosphates and artemether compound to P. falciparum. Chin J Pest Control. 2001;17(6):284–5. Li XL, Li CZ, He W, Dao QY. The treating effect of naphthoquine phosphates and artemether compound to P. falciparum. Chin J Pest Control. 2001;17(6):284–5.
11.
go back to reference Shan CQ, Liu GG, Jiao XQ. Primary observation on efficacy of naphthoquine phospate on the treatment of Plasmodium falciparum malaria. Acta Parasitologica et Medica Entomologica Sinica. 2003;10(4):198–201. Shan CQ, Liu GG, Jiao XQ. Primary observation on efficacy of naphthoquine phospate on the treatment of Plasmodium falciparum malaria. Acta Parasitologica et Medica Entomologica Sinica. 2003;10(4):198–201.
12.
go back to reference Shan CQ, Liu GG, Jiao XQ. Observation on efficacy of naphthoquine against vivax malaria. J Pathog Biol. 1998;11(4):275–6. Shan CQ, Liu GG, Jiao XQ. Observation on efficacy of naphthoquine against vivax malaria. J Pathog Biol. 1998;11(4):275–6.
13.
go back to reference Guo WZ, Zheng Q, Li G, Ou FZ, Guo XB. A randomized-controlled study of naphthoquine and artesunate in the treatment of falciparum malaria. J Guangzhou Univ Tradit Chin Med. 2000;17(3):25–7. Guo WZ, Zheng Q, Li G, Ou FZ, Guo XB. A randomized-controlled study of naphthoquine and artesunate in the treatment of falciparum malaria. J Guangzhou Univ Tradit Chin Med. 2000;17(3):25–7.
14.
go back to reference Guo WZ, Guo XB, Zheng QJ, Tan B, Chen RJ, Ou FZ, et al. A randomized comparative study of naphtoquine, mefloquine and artsunate in the treatment of falciparum malaria. Zhonghua Yi Xue Za Zhi. 2003;83(16):1406–8.PubMed Guo WZ, Guo XB, Zheng QJ, Tan B, Chen RJ, Ou FZ, et al. A randomized comparative study of naphtoquine, mefloquine and artsunate in the treatment of falciparum malaria. Zhonghua Yi Xue Za Zhi. 2003;83(16):1406–8.PubMed
15.
go back to reference Deben D, inventor. Research Institute of Microbial Epidemiology, The Academy of Military Medical Science, assignee. Patent: process for preparing synergetic antimalarial-compound naphthoquine phosphate. 1998. Deben D, inventor. Research Institute of Microbial Epidemiology, The Academy of Military Medical Science, assignee. Patent: process for preparing synergetic antimalarial-compound naphthoquine phosphate. 1998.
16.
go back to reference Wang S, Meng F, Shen H, Wen Y, Zhuo K, Zhu Q, et al. Therapeutic effect of dihydroartemisinin combined with naphthoquine phosphate in patients with falciparum malaria. Chin J Parasitol Parasit Dis. 2002;20(3):180–2. Wang S, Meng F, Shen H, Wen Y, Zhuo K, Zhu Q, et al. Therapeutic effect of dihydroartemisinin combined with naphthoquine phosphate in patients with falciparum malaria. Chin J Parasitol Parasit Dis. 2002;20(3):180–2.
17.
go back to reference Yang HL, Gao BH, Yang PF, Li CF, Li XL, Zhang ZY. Study on artesunate combined with naphthoquine delaying resistance of Plasmodium falciparum to artesunate in laboratory. Chin J Schistosomiasis Control. 2003;15(6):426–8. Yang HL, Gao BH, Yang PF, Li CF, Li XL, Zhang ZY. Study on artesunate combined with naphthoquine delaying resistance of Plasmodium falciparum to artesunate in laboratory. Chin J Schistosomiasis Control. 2003;15(6):426–8.
18.
go back to reference Li XL, Yang HL, Yang PF, Li CF, Li L. Efficacy of artesunate-naphthoquine combination against falciparum malaria. Chin J Parasit Dis Control. 2003;16(4):208–9. Li XL, Yang HL, Yang PF, Li CF, Li L. Efficacy of artesunate-naphthoquine combination against falciparum malaria. Chin J Parasit Dis Control. 2003;16(4):208–9.
19.
go back to reference Wang JY, Shan CQ, Fu DD, Pang XJ, Lu YF, Su LF, et al. Clinical trial of co-naphthoquine in the treatment of falciparum malaria. Chin J Parasit Dis Control. 2003;16(3):134–6. Wang JY, Shan CQ, Fu DD, Pang XJ, Lu YF, Su LF, et al. Clinical trial of co-naphthoquine in the treatment of falciparum malaria. Chin J Parasit Dis Control. 2003;16(3):134–6.
20.
go back to reference Shan CQ, Wang JY, Ding DB, Wu BA, Shi YL. Observation on efficacy of complex naphthoquine against Plasmodium vivax malaria. Acta Parasitologica et Medica Entomologica Sinica. 2004;11(1):8–10. Shan CQ, Wang JY, Ding DB, Wu BA, Shi YL. Observation on efficacy of complex naphthoquine against Plasmodium vivax malaria. Acta Parasitologica et Medica Entomologica Sinica. 2004;11(1):8–10.
21.
go back to reference Yan Q, Gong Y, inventors. Guilin Pharmaceutical Corporation Ltd, assignee. Patent: Compound antimalarial three-layered tablets containing artemisinin or its derivatives and its preparing method. China. 2007. Yan Q, Gong Y, inventors. Guilin Pharmaceutical Corporation Ltd, assignee. Patent: Compound antimalarial three-layered tablets containing artemisinin or its derivatives and its preparing method. China. 2007.
22.
go back to reference Zhang GL, Zeng T, Gao XO, inventors; Kunming Pharmaceutical Group Co. Ltd, assignee. Patent: Compound naphthoquine phosphate pellets and preparation method thereof. China. 2012. Zhang GL, Zeng T, Gao XO, inventors; Kunming Pharmaceutical Group Co. Ltd, assignee. Patent: Compound naphthoquine phosphate pellets and preparation method thereof. China. 2012.
23.
go back to reference Li GQ, Song JP, inventors. Li GQ, Song JP, assignee. Patent: Malaria-resisting arteannuin naphthoquine compound composition. China. 2008. Li GQ, Song JP, inventors. Li GQ, Song JP, assignee. Patent: Malaria-resisting arteannuin naphthoquine compound composition. China. 2008.
24.
go back to reference Heng S, inventor. Heng, S, assignee. Patent: Novel compound antimalarial preparation method. China. 2004. Heng S, inventor. Heng, S, assignee. Patent: Novel compound antimalarial preparation method. China. 2004.
26.
go back to reference Yang HL, Li XL, Yang PF, Li CF, Wu C, Zhang ZY, et al. Preventive effect on naphthoquine against vivax malaria and drug resistant falciparum malaria in Yunnan, China. Chin J Parasit Dis Con. 2003;16(3):137–9. Yang HL, Li XL, Yang PF, Li CF, Wu C, Zhang ZY, et al. Preventive effect on naphthoquine against vivax malaria and drug resistant falciparum malaria in Yunnan, China. Chin J Parasit Dis Con. 2003;16(3):137–9.
27.
go back to reference Pang XJ, Wang GZ, Xing QL. Hundred one cases of Plasmodium falciparum treated with naphthoquine phosphate. Chin J Parasit Dis. 1999;17(1):20–2. Pang XJ, Wang GZ, Xing QL. Hundred one cases of Plasmodium falciparum treated with naphthoquine phosphate. Chin J Parasit Dis. 1999;17(1):20–2.
28.
go back to reference Kunming Pharmaceutical Company (KPC). ARCO® dosing guidelines. Kunming Pharmaceutical Company. 2010. Kunming Pharmaceutical Company (KPC). ARCO® dosing guidelines. Kunming Pharmaceutical Company. 2010.
29.
go back to reference Wells TN. New medicines to combat malaria: an overview of the global pipeline of therapeutics. In: Staines HM, Krishna S, editors. Treatment and prevention of malaria: antimalarial drug chemistry, action and use. New York: Springer; 2012. p. 227–47. Wells TN. New medicines to combat malaria: an overview of the global pipeline of therapeutics. In: Staines HM, Krishna S, editors. Treatment and prevention of malaria: antimalarial drug chemistry, action and use. New York: Springer; 2012. p. 227–47.
33.
go back to reference World Health OrganizationGlobal Malaria Programme. Guidelines for the treatment of malaria. Report. Geneva: World Health Organization; 2015. World Health OrganizationGlobal Malaria Programme. Guidelines for the treatment of malaria. Report. Geneva: World Health Organization; 2015.
35.
go back to reference Burrows JN, Chibale K, Wells TNC. The state of the art in anti-malarial drug discovery and development. Curr Top Med Chem. 2011;11(10):1226–54.CrossRefPubMed Burrows JN, Chibale K, Wells TNC. The state of the art in anti-malarial drug discovery and development. Curr Top Med Chem. 2011;11(10):1226–54.CrossRefPubMed
36.
go back to reference Crowe A, Ilett KF, Karunajeewa HA, Batty KT, Davis TM. Role of P glycoprotein in absorption of novel antimalarial drugs. Antimicrob Agents Chemother. 2006;50(10):3504–6.CrossRefPubMedPubMedCentral Crowe A, Ilett KF, Karunajeewa HA, Batty KT, Davis TM. Role of P glycoprotein in absorption of novel antimalarial drugs. Antimicrob Agents Chemother. 2006;50(10):3504–6.CrossRefPubMedPubMedCentral
37.
go back to reference Tun T, Tint HS, Lin K, Kyaw TT, Myint MK, Khaing W, et al. Efficacy of oral single dose therapy with artemisinin-naphthoquine phosphate in uncomplicated falciparum malaria. Acta Trop. 2009;111(3):275–8.CrossRefPubMed Tun T, Tint HS, Lin K, Kyaw TT, Myint MK, Khaing W, et al. Efficacy of oral single dose therapy with artemisinin-naphthoquine phosphate in uncomplicated falciparum malaria. Acta Trop. 2009;111(3):275–8.CrossRefPubMed
38.
go back to reference Sullivan DJ Jr, Gluzman IY, Russell DG, Goldberg DE. On the molecular mechanism of chloroquine’s antimalarial action. Proc Natl Acad Sci USA. 1996;93(21):11865–70.CrossRefPubMedPubMedCentral Sullivan DJ Jr, Gluzman IY, Russell DG, Goldberg DE. On the molecular mechanism of chloroquine’s antimalarial action. Proc Natl Acad Sci USA. 1996;93(21):11865–70.CrossRefPubMedPubMedCentral
39.
go back to reference Wei XL, Su RB, Wang JY, Shi YL. Effect of complex naphthoquine on DNA content and pH value of the lysosome in Plasmodium berghei. Bull Acad Mil Med Sci. 2002;26(3):191–6. Wei XL, Su RB, Wang JY, Shi YL. Effect of complex naphthoquine on DNA content and pH value of the lysosome in Plasmodium berghei. Bull Acad Mil Med Sci. 2002;26(3):191–6.
40.
go back to reference Shao P, Shi YL, Chen PH, Wang FY. The effect of naphthoquine phosphate on the DNA content of Plasmodium yoelii yoelii: an analysis by flow cytometry. Chin J Zoonoses. 2000;16(1):51–4. Shao P, Shi YL, Chen PH, Wang FY. The effect of naphthoquine phosphate on the DNA content of Plasmodium yoelii yoelii: an analysis by flow cytometry. Chin J Zoonoses. 2000;16(1):51–4.
41.
go back to reference Yuan J, Chen PQ, Du QY, Li GQ, Chen L, Lei WW, et al. Effect of compound naphthoquine on the ultrastructure of Plasmodium berghei ANKA strain in erythrocytic stage. J Guangzhou Univ Tradit Chin Med. 2000;1:46–50. Yuan J, Chen PQ, Du QY, Li GQ, Chen L, Lei WW, et al. Effect of compound naphthoquine on the ultrastructure of Plasmodium berghei ANKA strain in erythrocytic stage. J Guangzhou Univ Tradit Chin Med. 2000;1:46–50.
42.
go back to reference Wong RP, Lautu D, Tavul L, Hackett SL, Siba P, Karunajeewa HA, et al. In vitro sensitivity of Plasmodium falciparum to conventional and novel antimalarial drugs in Papua New Guinea. Trop Med Int Health. 2010;15(3):342–9.CrossRefPubMed Wong RP, Lautu D, Tavul L, Hackett SL, Siba P, Karunajeewa HA, et al. In vitro sensitivity of Plasmodium falciparum to conventional and novel antimalarial drugs in Papua New Guinea. Trop Med Int Health. 2010;15(3):342–9.CrossRefPubMed
43.
go back to reference Koleala T. In vitro drug susceptibility of Plasmodium falciparum isolates in Madang Province, PNG using an optimized fluorescence assay and investigation of the effect of strain multiplicity on the outcome of in vitro antimalarial drug susceptibility measurements. Madang: University of Papua New Guinea; 2013. Koleala T. In vitro drug susceptibility of Plasmodium falciparum isolates in Madang Province, PNG using an optimized fluorescence assay and investigation of the effect of strain multiplicity on the outcome of in vitro antimalarial drug susceptibility measurements. Madang: University of Papua New Guinea; 2013.
44.
go back to reference Wirjanata G, Sebayang BF, Chalfein F, Prayoga Handayuni I, Trianty L, et al. Potent ex vivo activity of naphthoquine and methylene blue against drug-resistant clinical isolates of Plasmodium falciparum and Plasmodium vivax. Antimicrob Agents Chemother. 2015;59(10):6117–24.CrossRefPubMedPubMedCentral Wirjanata G, Sebayang BF, Chalfein F, Prayoga Handayuni I, Trianty L, et al. Potent ex vivo activity of naphthoquine and methylene blue against drug-resistant clinical isolates of Plasmodium falciparum and Plasmodium vivax. Antimicrob Agents Chemother. 2015;59(10):6117–24.CrossRefPubMedPubMedCentral
45.
go back to reference Yang HL, Li XL, Gao BH, Yang PF, Zhang ZY. Surveillance of Plasmodium falciparum susceptibility to seven antimalarials, including artemether, in the western part of the Sino-Myanmar border area. J Pathog Biol. 2009;11:831–43. Yang HL, Li XL, Gao BH, Yang PF, Zhang ZY. Surveillance of Plasmodium falciparum susceptibility to seven antimalarials, including artemether, in the western part of the Sino-Myanmar border area. J Pathog Biol. 2009;11:831–43.
46.
go back to reference Yang HL, Gao BH, Huang KG. Comparison of naphthoquine, metronidazole and norfloxacine to artesunate sensitive and resistant P. falciparum strains. J Pract Parasit Dis. 1999;2:52–3. Yang HL, Gao BH, Huang KG. Comparison of naphthoquine, metronidazole and norfloxacine to artesunate sensitive and resistant P. falciparum strains. J Pract Parasit Dis. 1999;2:52–3.
47.
go back to reference Koleala T, Karl S, Laman M, Moore BR, Benjamin J, Barnadas C, et al. Temporal changes in Plasmodium falciparum anti-malarial drug sensitivity in vitro and resistance-associated genetic mutations in isolates from Papua New Guinea. Malar J. 2015;14(1):37.CrossRefPubMedPubMedCentral Koleala T, Karl S, Laman M, Moore BR, Benjamin J, Barnadas C, et al. Temporal changes in Plasmodium falciparum anti-malarial drug sensitivity in vitro and resistance-associated genetic mutations in isolates from Papua New Guinea. Malar J. 2015;14(1):37.CrossRefPubMedPubMedCentral
49.
go back to reference Li FL, Wang LH, Ding DB, Yang JD, Gao XS. Studies on antimalarials synthesis of 4-arylamino-tert-butylaminomethyl phenols. Acta Pharmaceutica Sinica. 1982;1:77–9. Li FL, Wang LH, Ding DB, Yang JD, Gao XS. Studies on antimalarials synthesis of 4-arylamino-tert-butylaminomethyl phenols. Acta Pharmaceutica Sinica. 1982;1:77–9.
50.
go back to reference Basco LK, Ringwald P. In vitro activities of piperaquine and other 4-aminoquinolines against clinical isolates of Plasmodium falciparum in Cameroon. Antimicrob Agents Chemother. 2003;47(4):1391–4.CrossRefPubMedPubMedCentral Basco LK, Ringwald P. In vitro activities of piperaquine and other 4-aminoquinolines against clinical isolates of Plasmodium falciparum in Cameroon. Antimicrob Agents Chemother. 2003;47(4):1391–4.CrossRefPubMedPubMedCentral
51.
go back to reference Davis TM, Hamzah J, Ilett KF, Karunajeewa HA, Reeder JC, Batty KT, et al. In vitro interactions between piperaquine, dihydroartemisinin, and other conventional and novel antimalarial drugs. Antimicrob Agents Chemother. 2006;50(8):2883–5.CrossRefPubMedPubMedCentral Davis TM, Hamzah J, Ilett KF, Karunajeewa HA, Reeder JC, Batty KT, et al. In vitro interactions between piperaquine, dihydroartemisinin, and other conventional and novel antimalarial drugs. Antimicrob Agents Chemother. 2006;50(8):2883–5.CrossRefPubMedPubMedCentral
52.
go back to reference Cabrera M, Cui L. In vitro activities of primaquine-schizonticide combinations on asexual blood stages and gametocytes of Plasmodium falciparum. Antimicrob Agents Chemother. 2015;59(12):7650–6.CrossRefPubMed Cabrera M, Cui L. In vitro activities of primaquine-schizonticide combinations on asexual blood stages and gametocytes of Plasmodium falciparum. Antimicrob Agents Chemother. 2015;59(12):7650–6.CrossRefPubMed
53.
go back to reference Wang JY, Ding DB, Li GF, Zhao JH. Therapeutic efficacy of naphthoquine phosphate combined with artemisinine against Plasmodium knowlesi. Chin J Parasitol Parasit Dis. 2008;26(6):442–4. Wang JY, Ding DB, Li GF, Zhao JH. Therapeutic efficacy of naphthoquine phosphate combined with artemisinine against Plasmodium knowlesi. Chin J Parasitol Parasit Dis. 2008;26(6):442–4.
54.
go back to reference Wang JY, Li GF, Zhao JH, Zhang M, Ji XG. Study of synergetic effect of naphthoquine phosphate and its combination with artemisinin and its delaying effect on drug-resistace of Plasmodium berghei. Acta Parasitologica et Medica Entomologica Sinica. 2008;15(3):133–6. Wang JY, Li GF, Zhao JH, Zhang M, Ji XG. Study of synergetic effect of naphthoquine phosphate and its combination with artemisinin and its delaying effect on drug-resistace of Plasmodium berghei. Acta Parasitologica et Medica Entomologica Sinica. 2008;15(3):133–6.
55.
go back to reference Sunday OS, George AO. The antimalarial effect of differnt dosage regimen of artemisinin-naphthoquine on Plasmodium berghei infected mice. Int J Pharmacol Ther. 2013;3(1):67–77. Sunday OS, George AO. The antimalarial effect of differnt dosage regimen of artemisinin-naphthoquine on Plasmodium berghei infected mice. Int J Pharmacol Ther. 2013;3(1):67–77.
56.
go back to reference Zhang ZX. Current situation of clinical treatment of falciparum malaria in Yunnan. J Kunming Med Univ. 2009;8:26–34. Zhang ZX. Current situation of clinical treatment of falciparum malaria in Yunnan. J Kunming Med Univ. 2009;8:26–34.
57.
go back to reference World Health Organization. Assessment and monitoring of antimalarial drug efficacy for the treatment of uncomplicated falciparum malaria. Geneva: World Health Organization; 2003. World Health Organization. Assessment and monitoring of antimalarial drug efficacy for the treatment of uncomplicated falciparum malaria. Geneva: World Health Organization; 2003.
58.
go back to reference Yang HL, Yang PF, Li CF, Li XL, Li L, Yang CJ. Curative effect on artesunate-naphthoquine combination in treatment of malaria. Chin J Parasit Dis Control. 2004;17(2):87–9. Yang HL, Yang PF, Li CF, Li XL, Li L, Yang CJ. Curative effect on artesunate-naphthoquine combination in treatment of malaria. Chin J Parasit Dis Control. 2004;17(2):87–9.
59.
go back to reference Liu H, Li CF, Nie RH, Sun YH, Li GS, Shen X. Treatment of malariae malaria with artesunate and naphthoquine phosphate: a report of two cases. Chin J Schistosomiasis Control. 2009;21(2):135. Liu H, Li CF, Nie RH, Sun YH, Li GS, Shen X. Treatment of malariae malaria with artesunate and naphthoquine phosphate: a report of two cases. Chin J Schistosomiasis Control. 2009;21(2):135.
60.
go back to reference Krudsood S, Chalermrut K, Pengruksa C, Srivilairit S, Silachamroon U, Treeprasertsuk S, et al. Comparative clinical trial of two-fixed combinations dihydroartemisinin-napthoquine-trimethoprim (DNP®) and artemether-lumefantrine (Coartem®/Riamet®) in the treatment of acute uncomplicated falciparum malaria in Thailand. Southeast Asian J Trop Med Public Health. 2003;34(2):316.PubMedPubMedCentral Krudsood S, Chalermrut K, Pengruksa C, Srivilairit S, Silachamroon U, Treeprasertsuk S, et al. Comparative clinical trial of two-fixed combinations dihydroartemisinin-napthoquine-trimethoprim (DNP®) and artemether-lumefantrine (Coartem®/Riamet®) in the treatment of acute uncomplicated falciparum malaria in Thailand. Southeast Asian J Trop Med Public Health. 2003;34(2):316.PubMedPubMedCentral
61.
go back to reference Song JP, Xu Y, Ou FZ, Peng NZ, Li GQ, Jin TS. Dosage verification of compound naphthoquine for falciparum malaria. J Guangzhou Univ Tradit Chin Med. 2001;18(1):19–24. Song JP, Xu Y, Ou FZ, Peng NZ, Li GQ, Jin TS. Dosage verification of compound naphthoquine for falciparum malaria. J Guangzhou Univ Tradit Chin Med. 2001;18(1):19–24.
62.
go back to reference Hu AH, Li XM, Wang JH. Cost-minimization analysis on 3 kinds of medicines in the treatment of falciparum malaria. Strait Pharm J. 2011;4:199–201. Hu AH, Li XM, Wang JH. Cost-minimization analysis on 3 kinds of medicines in the treatment of falciparum malaria. Strait Pharm J. 2011;4:199–201.
63.
go back to reference Meremikwu MM, Odey F, Oringanje C, Oyo-Ita A, Effa E, Esu EB, et al. Open-label trial of three dosage regimens of fixed-dose combination of artemisinin and naphthoquine for treating uncomplicated falciparum malaria in Calabar, Nigeria. Malar J. 2012;11:413.CrossRefPubMedPubMedCentral Meremikwu MM, Odey F, Oringanje C, Oyo-Ita A, Effa E, Esu EB, et al. Open-label trial of three dosage regimens of fixed-dose combination of artemisinin and naphthoquine for treating uncomplicated falciparum malaria in Calabar, Nigeria. Malar J. 2012;11:413.CrossRefPubMedPubMedCentral
64.
go back to reference Udoh E, Meremikwu M, Odey F, Oringanje C, Oduwole O, Oyo-ita A. Artemisinin-naphthoquine versus artemether-lumefantrine for treating uncomplicated plasmodium falciparum malaria in children: A randomized controlled trial of efficacy and safety. Niger J Paediatr. 2014;41(3):170–4.CrossRef Udoh E, Meremikwu M, Odey F, Oringanje C, Oduwole O, Oyo-ita A. Artemisinin-naphthoquine versus artemether-lumefantrine for treating uncomplicated plasmodium falciparum malaria in children: A randomized controlled trial of efficacy and safety. Niger J Paediatr. 2014;41(3):170–4.CrossRef
65.
go back to reference Liu H, Yang HL, Xu JW, Wang JZ, Nie RH, Li CF. Artemisinin-naphthoquine combination versus chloroquine-primaquine to treat vivax malaria: an open-label randomized and non-inferiority trial in Yunnan Province, China. Malar J. 2013;12:409.CrossRefPubMedPubMedCentral Liu H, Yang HL, Xu JW, Wang JZ, Nie RH, Li CF. Artemisinin-naphthoquine combination versus chloroquine-primaquine to treat vivax malaria: an open-label randomized and non-inferiority trial in Yunnan Province, China. Malar J. 2013;12:409.CrossRefPubMedPubMedCentral
66.
go back to reference Laman M, Moore BR, Benjamin JM, Yadi G, Bona C, Warrel J, et al. Artemisinin-naphthoquine versus artemether-lumefantrine for uncomplicated malaria in Papua New Guinean children: an open-label randomized trial. PLoS Med. 2014;11(12):e1001773.CrossRefPubMedPubMedCentral Laman M, Moore BR, Benjamin JM, Yadi G, Bona C, Warrel J, et al. Artemisinin-naphthoquine versus artemether-lumefantrine for uncomplicated malaria in Papua New Guinean children: an open-label randomized trial. PLoS Med. 2014;11(12):e1001773.CrossRefPubMedPubMedCentral
67.
go back to reference Laman M, Benjamin JM, Moore BR, Salib M, Tawat S, Davis WA, et al. Artemether-lumefantrine versus artemisinin-naphthoquine in Papua New Guinean children with uncomplicated malaria: a six months post-treatment follow-up study. Malar J. 2015;14:121.CrossRefPubMedPubMedCentral Laman M, Benjamin JM, Moore BR, Salib M, Tawat S, Davis WA, et al. Artemether-lumefantrine versus artemisinin-naphthoquine in Papua New Guinean children with uncomplicated malaria: a six months post-treatment follow-up study. Malar J. 2015;14:121.CrossRefPubMedPubMedCentral
68.
go back to reference Hombhanje FW, Huang Q. Artemisinin–naphthoquine Combination (ARCO®): an overview of the progress. Pharmaceuticals. 2010;3(12):3581–93.CrossRefPubMedCentral Hombhanje FW, Huang Q. Artemisinin–naphthoquine Combination (ARCO®): an overview of the progress. Pharmaceuticals. 2010;3(12):3581–93.CrossRefPubMedCentral
69.
go back to reference Wu DL, Wang GX, Tang DH. Observation on the effect of naphthoquine phosphate on the control of malaria in Qiongzhong County, Hainan Province. China Trop Med. 2001;1(3):216–7. Wu DL, Wang GX, Tang DH. Observation on the effect of naphthoquine phosphate on the control of malaria in Qiongzhong County, Hainan Province. China Trop Med. 2001;1(3):216–7.
70.
go back to reference Wang H, Bei ZC, Wang JY, Cao WC. Plasmodium berghei K173: selection of resistance to naphthoquine in a mouse model. Exp Parasitol. 2011;127(2):436–9.CrossRefPubMed Wang H, Bei ZC, Wang JY, Cao WC. Plasmodium berghei K173: selection of resistance to naphthoquine in a mouse model. Exp Parasitol. 2011;127(2):436–9.CrossRefPubMed
71.
go back to reference Sun YH, Zhou JL, Liu H, Wang HY, Yang HL. In vitro culture of naphthoquione-resistant Plasmodium falciparum strains in Yunnan Province. J Pathog Biol. 2010;2(124–6):33. Sun YH, Zhou JL, Liu H, Wang HY, Yang HL. In vitro culture of naphthoquione-resistant Plasmodium falciparum strains in Yunnan Province. J Pathog Biol. 2010;2(124–6):33.
72.
go back to reference Qu HY, Gao HZ, Hao GT, Li YY, Li HY, Hu JC, et al. Single-dose safety, pharmacokinetics, and food effects studies of compound naphthoquine phosphate tablets in healthy volunteers. J Clin Pharmacol. 2010;50(11):1310–8.CrossRefPubMed Qu HY, Gao HZ, Hao GT, Li YY, Li HY, Hu JC, et al. Single-dose safety, pharmacokinetics, and food effects studies of compound naphthoquine phosphate tablets in healthy volunteers. J Clin Pharmacol. 2010;50(11):1310–8.CrossRefPubMed
73.
go back to reference Batty KT, Salman S, Moore BR, Benjamin J, Lee ST, Page-Sharp M, et al. Artemisinin-naphthoquine combination therapy for uncomplicated pediatric malaria: a pharmacokinetic study. Antimicrob Agents Chemother. 2012;56(5):2472–84.CrossRefPubMedPubMedCentral Batty KT, Salman S, Moore BR, Benjamin J, Lee ST, Page-Sharp M, et al. Artemisinin-naphthoquine combination therapy for uncomplicated pediatric malaria: a pharmacokinetic study. Antimicrob Agents Chemother. 2012;56(5):2472–84.CrossRefPubMedPubMedCentral
74.
go back to reference Li PF. Study on the determination of artemisinin/naphthoquine phosphate in human and pharmacokinetics [masters thesis, Jilin University, China]. 2006. Li PF. Study on the determination of artemisinin/naphthoquine phosphate in human and pharmacokinetics [masters thesis, Jilin University, China]. 2006.
75.
go back to reference Wang JY, Zuo B, Xu ZH, Sun GZ, Zhang M, Wang C, et al. Long-term toxicity of co-naphthoquine in beagle dogs. Bull Acad Mil Med Sci. 2003;27(3):196–8. Wang JY, Zuo B, Xu ZH, Sun GZ, Zhang M, Wang C, et al. Long-term toxicity of co-naphthoquine in beagle dogs. Bull Acad Mil Med Sci. 2003;27(3):196–8.
76.
go back to reference Sunday OS, George AO. Effect of dosage regimen of Artemisinin-naphthoquine combination on biochemical parameters in Plasmodium berghei infected mice. J Med Res Pract. 2013;2(5):129–33. Sunday OS, George AO. Effect of dosage regimen of Artemisinin-naphthoquine combination on biochemical parameters in Plasmodium berghei infected mice. J Med Res Pract. 2013;2(5):129–33.
77.
go back to reference Fowler JSL. Data interpretation. In: Duffus JG, Worth HGJ, editors. Fundamental toxicology. Cambridge: The Royal Society of Chemistry; 2006. p. 53. Fowler JSL. Data interpretation. In: Duffus JG, Worth HGJ, editors. Fundamental toxicology. Cambridge: The Royal Society of Chemistry; 2006. p. 53.
78.
go back to reference Benjamin J, Moore B, Lee ST, Senn M, Griffin S, Lautu D, et al. Artemisinin-naphthoquine combination therapy for uncomplicated pediatric malaria: a tolerability, safety, and preliminary efficacy study. Antimicrob Agents Chemother. 2012;56(5):2465–71.CrossRefPubMedPubMedCentral Benjamin J, Moore B, Lee ST, Senn M, Griffin S, Lautu D, et al. Artemisinin-naphthoquine combination therapy for uncomplicated pediatric malaria: a tolerability, safety, and preliminary efficacy study. Antimicrob Agents Chemother. 2012;56(5):2465–71.CrossRefPubMedPubMedCentral
80.
go back to reference El-Beshbishi SN, Taman A, El-Malky M, Azab MS, El-Hawary AK, El-Tantawy DA. First insight into the effect of single oral dose therapy with artemisinin-naphthoquine phosphate combination in a mouse model of Schistosoma mansoni infection. Int J Parasitol. 2013;43(7):521–30.CrossRefPubMed El-Beshbishi SN, Taman A, El-Malky M, Azab MS, El-Hawary AK, El-Tantawy DA. First insight into the effect of single oral dose therapy with artemisinin-naphthoquine phosphate combination in a mouse model of Schistosoma mansoni infection. Int J Parasitol. 2013;43(7):521–30.CrossRefPubMed
81.
go back to reference del Villar Perez. L, Burguillo FJ, Lopez-Aban J, Muro A. Systematic review and meta-analysis of artemisinin based therapies for the treatment and prevention of schistosomiasis. PLoS One. 2012;7(9):e45867.CrossRef del Villar Perez. L, Burguillo FJ, Lopez-Aban J, Muro A. Systematic review and meta-analysis of artemisinin based therapies for the treatment and prevention of schistosomiasis. PLoS One. 2012;7(9):e45867.CrossRef
82.
go back to reference Utzinger J, Xiao SH, Tanner M, Keiser J. Artemisinins for schistosomiasis and beyond. Curr Opin Investig Drugs. 2007;8(2):105–16.PubMed Utzinger J, Xiao SH, Tanner M, Keiser J. Artemisinins for schistosomiasis and beyond. Curr Opin Investig Drugs. 2007;8(2):105–16.PubMed
83.
go back to reference El-Beshbishi SN, El Bardicy S, Tadros M, Ayoub M, Taman A. Spotlight on the in vitro effect of artemisinin-naphthoquine phosphate on Schistosoma mansoni and its snail host Biomphalaria alexandrina. Acta Trop. 2015;141(Pt A):37–45.CrossRefPubMed El-Beshbishi SN, El Bardicy S, Tadros M, Ayoub M, Taman A. Spotlight on the in vitro effect of artemisinin-naphthoquine phosphate on Schistosoma mansoni and its snail host Biomphalaria alexandrina. Acta Trop. 2015;141(Pt A):37–45.CrossRefPubMed
84.
go back to reference World Health Organization. Guidelines for the treatment of malaria. Geneva: World Health Organization; 2006. World Health Organization. Guidelines for the treatment of malaria. Geneva: World Health Organization; 2006.
85.
go back to reference Naing C, Whittaker MA, Mak JW, Aung K. A systematic review of the efficacy of a single dose artemisinin-naphthoquine in treating uncomplicated malaria. Malar J. 2015;14(1):392.CrossRefPubMedPubMedCentral Naing C, Whittaker MA, Mak JW, Aung K. A systematic review of the efficacy of a single dose artemisinin-naphthoquine in treating uncomplicated malaria. Malar J. 2015;14(1):392.CrossRefPubMedPubMedCentral
86.
go back to reference Isba R, Zani B, Gathu M, Sinclair D. Artemisinin-naphthoquine for treating uncomplicated Plasmodium falciparum malaria. Cochrane Database Syst Rev. 2015;2:CD011547.PubMed Isba R, Zani B, Gathu M, Sinclair D. Artemisinin-naphthoquine for treating uncomplicated Plasmodium falciparum malaria. Cochrane Database Syst Rev. 2015;2:CD011547.PubMed
87.
go back to reference Price RN, Uhlemann AC, van Vugt M, Brockman A, Hutagalung R, Nair S, et al. Molecular and pharmacological determinants of the therapeutic response to artemether-lumefantrine in multidrug-resistant Plasmodium falciparum malaria. Clin Infect Dis. 2006;42(11):1570–7.CrossRefPubMedPubMedCentral Price RN, Uhlemann AC, van Vugt M, Brockman A, Hutagalung R, Nair S, et al. Molecular and pharmacological determinants of the therapeutic response to artemether-lumefantrine in multidrug-resistant Plasmodium falciparum malaria. Clin Infect Dis. 2006;42(11):1570–7.CrossRefPubMedPubMedCentral
88.
go back to reference Amaratunga C, Lim P, Suon S, Sreng S, Mao S, Sopha C, et al. Dihydroartemisinin-piperaquine resistance in Plasmodium falciparum malaria in Cambodia: a multisite prospective cohort study. Lancet Infect Dis. 2016;16:357–65.CrossRefPubMed Amaratunga C, Lim P, Suon S, Sreng S, Mao S, Sopha C, et al. Dihydroartemisinin-piperaquine resistance in Plasmodium falciparum malaria in Cambodia: a multisite prospective cohort study. Lancet Infect Dis. 2016;16:357–65.CrossRefPubMed
89.
go back to reference Basco LK. Field application of in vitro assays for the sensitivity of human malaria parasites to antimalarial drugs. Geneva: World Health Organization; 2007. Basco LK. Field application of in vitro assays for the sensitivity of human malaria parasites to antimalarial drugs. Geneva: World Health Organization; 2007.
90.
go back to reference Rujumba J, Mworozi EA, Manganda AK, Kiguba R, Rwakimali B, Nsobya S. A comparative study of Arco and Coartem in the treatment of uncomplicated malaria in patients aged 4 months to 16 years attending Mulago hospital, Kapala, Uganda [abstract]. Int J Infect Dis. 2010;14(Suppl 1):e332.CrossRef Rujumba J, Mworozi EA, Manganda AK, Kiguba R, Rwakimali B, Nsobya S. A comparative study of Arco and Coartem in the treatment of uncomplicated malaria in patients aged 4 months to 16 years attending Mulago hospital, Kapala, Uganda [abstract]. Int J Infect Dis. 2010;14(Suppl 1):e332.CrossRef
91.
go back to reference D’Alessandro U, Ubben D, Hamed K, Ceesay SJ, Okebe J, Taal M, et al. Malaria in infants aged less than six months—is it an area of unmet medical need? Malar J. 2012;11:400.CrossRefPubMedPubMedCentral D’Alessandro U, Ubben D, Hamed K, Ceesay SJ, Okebe J, Taal M, et al. Malaria in infants aged less than six months—is it an area of unmet medical need? Malar J. 2012;11:400.CrossRefPubMedPubMedCentral
92.
go back to reference Davis TM, Mueller I, Rogerson SJ. Prevention and treatment of malaria in pregnancy. Future Microbiol. 2010;5(10):1599–613.CrossRefPubMed Davis TM, Mueller I, Rogerson SJ. Prevention and treatment of malaria in pregnancy. Future Microbiol. 2010;5(10):1599–613.CrossRefPubMed
93.
go back to reference Skinner TS, Manning LS, Johnston WA, Davis TM. In vitro stage-specific sensitivity of Plasmodium falciparum to quinine and artemisinin drugs. Int J Parasitol. 1996;26(5):519–25.CrossRefPubMed Skinner TS, Manning LS, Johnston WA, Davis TM. In vitro stage-specific sensitivity of Plasmodium falciparum to quinine and artemisinin drugs. Int J Parasitol. 1996;26(5):519–25.CrossRefPubMed
94.
go back to reference Shanks GD, Edstein MD, Jacobus D. Evolution from double to triple-antimalarial drug combinations. Trans R Soc Trop Med Hyg. 2015;109(3):182–8.CrossRefPubMed Shanks GD, Edstein MD, Jacobus D. Evolution from double to triple-antimalarial drug combinations. Trans R Soc Trop Med Hyg. 2015;109(3):182–8.CrossRefPubMed
95.
go back to reference Delves M, Plouffe D, Scheurer C, Meister S, Wittlin S, Winzeler EA, et al. The activities of current antimalarial drugs on the life cycle stages of Plasmodium: a comparative study with human and rodent parasites. PLoS Med. 2012;9(2):e1001169.CrossRefPubMedPubMedCentral Delves M, Plouffe D, Scheurer C, Meister S, Wittlin S, Winzeler EA, et al. The activities of current antimalarial drugs on the life cycle stages of Plasmodium: a comparative study with human and rodent parasites. PLoS Med. 2012;9(2):e1001169.CrossRefPubMedPubMedCentral
96.
go back to reference Hombhanje FW, Linge D, Saweri A, Kuanch C, Jones R, Toraso S, et al. Artemisinin-naphthoquine combination (ARCO) therapy for uncomplicated falciparum malaria in adults of Papua New Guinea: a preliminary report on safety and efficacy. Malar J. 2009;8:196.CrossRefPubMedPubMedCentral Hombhanje FW, Linge D, Saweri A, Kuanch C, Jones R, Toraso S, et al. Artemisinin-naphthoquine combination (ARCO) therapy for uncomplicated falciparum malaria in adults of Papua New Guinea: a preliminary report on safety and efficacy. Malar J. 2009;8:196.CrossRefPubMedPubMedCentral
97.
go back to reference Toure OA, Penali LK, Yapi JD, Ako BA, Toure W, Djerea K, et al. A comparative, randomized clinical trial of artemisinin/naphtoquine twice daily one day versus artemether/lumefantrine six doses regimen in children and adults with uncomplicated falciparum malaria in Cote d’Ivoire. Malar J. 2009;8:148.CrossRefPubMedPubMedCentral Toure OA, Penali LK, Yapi JD, Ako BA, Toure W, Djerea K, et al. A comparative, randomized clinical trial of artemisinin/naphtoquine twice daily one day versus artemether/lumefantrine six doses regimen in children and adults with uncomplicated falciparum malaria in Cote d’Ivoire. Malar J. 2009;8:148.CrossRefPubMedPubMedCentral
98.
go back to reference Nour BYM, Hamed NMM, Habour AB, Elkariem AAA, Mohamadani AA, Saeed OK. Efficacy and safety of artemisinin–naphthoquine (ARCO®) in the treatment of uncomplicated Plasmodium falciparum among Sudanese adults. Glob Adv Res J Med Med Sci. 2014;3(1):1–7. Nour BYM, Hamed NMM, Habour AB, Elkariem AAA, Mohamadani AA, Saeed OK. Efficacy and safety of artemisinin–naphthoquine (ARCO®) in the treatment of uncomplicated Plasmodium falciparum among Sudanese adults. Glob Adv Res J Med Med Sci. 2014;3(1):1–7.
99.
go back to reference Tjitra E, Hasugian AR, Siswantoro H, Prasetyorini B, Ekowatiningsih R, Yusnita EA, et al. Efficacy and safety of artemisinin-naphthoquine versus dihydroartemisinin-piperaquine in adult patients with uncomplicated malaria: a multi-centre study in Indonesia. Malar J. 2012;11:153.CrossRefPubMedPubMedCentral Tjitra E, Hasugian AR, Siswantoro H, Prasetyorini B, Ekowatiningsih R, Yusnita EA, et al. Efficacy and safety of artemisinin-naphthoquine versus dihydroartemisinin-piperaquine in adult patients with uncomplicated malaria: a multi-centre study in Indonesia. Malar J. 2012;11:153.CrossRefPubMedPubMedCentral
100.
go back to reference Kinde-Gazard D, Ogouyemi-Hounto A, Capo-Chichi L, Gbaguidi J, Massougbodji A. A randomized clinical trial comparing the effectiveness and tolerability of artemisinine-naphthoquine (Arco®) and artemether-lumefantrine (Coartem®) in the treatment of uncomplicated malaria in Benin. Bull Soc Pathol Exot. 2012;105(3):208–14.CrossRefPubMed Kinde-Gazard D, Ogouyemi-Hounto A, Capo-Chichi L, Gbaguidi J, Massougbodji A. A randomized clinical trial comparing the effectiveness and tolerability of artemisinine-naphthoquine (Arco®) and artemether-lumefantrine (Coartem®) in the treatment of uncomplicated malaria in Benin. Bull Soc Pathol Exot. 2012;105(3):208–14.CrossRefPubMed
Metadata
Title
Naphthoquine: An Emerging Candidate for Artemisinin Combination Therapy
Authors
Brioni R. Moore
Moses Laman
Sam Salman
Kevin T. Batty
Madhu Page-Sharp
Francis Hombhanje
Laurens Manning
Timothy M. E. Davis
Publication date
01-05-2016
Publisher
Springer International Publishing
Published in
Drugs / Issue 7/2016
Print ISSN: 0012-6667
Electronic ISSN: 1179-1950
DOI
https://doi.org/10.1007/s40265-016-0572-5

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