Tafenoquine treatment of Plasmodium vivax malaria: suggestive evidence that CYP2D6 reduced metabolism is not associated with relapse in the Phase 2b DETECTIVE trial.

St Jean PL, Xue Z, Carter N, Koh GC, Duparc S, Taylor M, Beaumont C, Llanos-Cuentas A, Rueangweerayut R, Krudsood S, Green JA, Rubio JP.Malar J. 2016 Feb 18;15:97. doi: 10.1186/s12936-016-1145-5.PMID: 26888075Free PMC ArticleSimilar articlesSelect item 243603692.

Tafenoquine plus chloroquine for the treatment and relapse prevention of Plasmodium vivax malaria (DETECTIVE): a multicentre, double-blind, randomised, phase 2b dose-selection study.

Llanos-Cuentas A, Lacerda MV, Rueangweerayut R, Krudsood S, Gupta SK, Kochar SK, Arthur P, Chuenchom N, Möhrle JJ, Duparc S, Ugwuegbulam C, Kleim JP, Carter N, Green JA, Kellam L.Lancet. 2014 Mar 22;383(9922):1049-58. doi: 10.1016/S0140-6736(13)62568-4. Epub 2013 Dec 19.PMID: 24360369 Similar articles Select item 154868313.

Randomized trial of 3-dose regimens of tafenoquine (WR238605) versus low-dose primaquine for preventing Plasmodium vivax malaria relapse.

Walsh DS, Wilairatana P, Tang DB, Heppner DG Jr, Brewer TG, Krudsood S, Silachamroon U, Phumratanaprapin W, Siriyanonda D, Looareesuwan S.

Clin Infect Dis. 2004 Oct 15;39(8):1095-103. Epub 2004 Sep 24.

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Primaquine treatment and relapse in Plasmodium vivax malaria.

Rishikesh K, Saravu K.

Pathog Glob Health. 2016;110(1):1-8. doi: 10.1080/20477724.2015.1133033. Epub 2016 Feb 18. Review.

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Single-Dose Tafenoquine to Prevent Relapse of Plasmodium vivax Malaria.

Lacerda MVG, Llanos-Cuentas A, Krudsood S, Lon C, Saunders DL, Mohammed R, Yilma D, Batista Pereira D, Espino FEJ, Mia RZ, Chuquiyauri R, Val F, Casapía M, Monteiro WM, Brito MAM, Costa MRF, Buathong N, Noedl H, Diro E, Getie S, Wubie KM, Abdissa A, Zeynudin A, Abebe C, Tada MS, Brand F, Beck HP, Angus B, Duparc S, Kleim JP, Kellam LM, Rousell VM, Jones SW, Hardaker E, Mohamed K, Clover DD, Fletcher K, Breton JJ, Ugwuegbulam CO, Green JA, Koh GCKW.

N Engl J Med. 2019 Jan 17;380(3):215-228. doi: 10.1056/NEJMoa1710775.

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Cytochrome P450 2D-mediated metabolism is not necessary for tafenoquine and primaquine to eradicate the erythrocytic stages of Plasmodium berghei.

Milner EE, Berman J, Caridha D, Dickson SP, Hickman M, Lee PJ, Marcsisin SR, Read LT, Roncal N, Vesely BA, Xie LH, Zhang J, Zhang P, Li Q.

Malar J. 2016 Dec 7;15(1):588.

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Assessment of the prophylactic activity and pharmacokinetic profile of oral tafenoquine compared to primaquine for inhibition of liver stage malaria infections.

Li Q, O'Neil M, Xie L, Caridha D, Zeng Q, Zhang J, Pybus B, Hickman M, Melendez V.

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Estimation of the Antirelapse Efficacy of Tafenoquine, Using Plasmodium vivax Genotyping.

Beck HP, Wampfler R, Carter N, Koh G, Osorio L, Rueangweerayut R, Krudsood S, Lacerda MV, Llanos-Cuentas A, Duparc S, Rubio JP, Green JA.

J Infect Dis. 2016 Mar 1;213(5):794-9. doi: 10.1093/infdis/jiv508.Epub 2015 Oct 23.

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Variation in Human Cytochrome P-450 Drug-Metabolism Genes: A Gateway to the Understanding of Plasmodium vivax Relapses.

Silvino AC, Costa GL, Araújo FC, Ascher DB, Pires DE, Fontes CJ, Carvalho LH, Brito CF, Sousa TN.

PLoS o­ne. 2016 Jul 28;11(7):e0160172. doi: 10.1371/journal.pone.0160172. eCollection 2016. Erratum in:PLoS o­ne. 2018 Feb 1;13(2):e0192534.

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Exposure-Response Analyses for Tafenoquine after Administration to Patients with Plasmodium vivax Malaria.

Tenero D, Green JA, Goyal N.

Antimicrob Agents Chemother. 2015 Oct;59(10):6188-94. doi: 10.1128/AAC.00718-15. Epub 2015 Jul 27.

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Therapeutic efficacy of chloroquine and chloroquine plus primaquine for the treatment of Plasmodium vivax in Ethiopia.

Yeshiwondim AK, Tekle AH, Dengela DO, Yohannes AM, Teklehaimanot A.

Acta Trop. 2010 Feb;113(2):105-13. doi: 10.1016/j.actatropica.2009.10.001.Epub 2009 Oct 14.

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Differential cytochrome P450 2D metabolism alters tafenoquine pharmacokinetics.

Vuong C, Xie LH, Potter BM, Zhang J, Zhang P, Duan D, Nolan CK, Sciotti RJ, Zottig VE, Nanayakkara NP, Tekwani BL, Walker LA, Smith PL, Paris RM, Read LT, Li Q, Pybus BS, Sousa JC, Reichard GA, Smith B, Marcsisin SR.

Antimicrob Agents Chemother. 2015 Jul;59(7):3864-9. doi: 10.1128/AAC.00343-15. Epub 2015 Apr 13.

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Tafenoquine for preventing relapse in people with Plasmodium vivax malaria.

Rajapakse S, Rodrigo C, Fernando SD.

Cochrane Database Syst Rev. 2015 Apr 29;(4):CD010458. doi: 10.1002/14651858.CD010458.pub2. Review.

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Tafenoquine for the treatment of recurrent Plasmodium vivax malaria.

Kitchener S, Nasveld P, Edstein MD.

Am J Trop Med Hyg. 2007 Mar;76(3):494-6.

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Chloroquine-Primaquine versus Chloroquine Alone to Treat Vivax Malaria in Afghanistan: An Open Randomized Superiority Trial.

Awab GR, Imwong M, Bancone G, Jeeyapant A, Day NPJ, White NJ, Woodrow CJ.

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Pathway-specific inhibition of primaquine metabolism by chloroquine/quinine.

Fasinu PS, Tekwani BL, Avula B, Chaurasiya ND, Nanayakkara NP, Wang YH, Khan IA, Walker LA.

Malar J. 2016 Sep 13;15:466. doi: 10.1186/s12936-016-1509-x.

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CYP2D6 activity and the risk of recurrence of Plasmodium vivax malaria in the Brazilian Amazon: a prospective cohort study.

Brasil LW, Rodrigues-Soares F, Santoro AB, Almeida ACG, Kühn A, Ramasawmy R, Lacerda MVG, Monteiro WM, Suarez-Kurtz G.

Malar J. 2018 Feb 1;17(1):57. doi: 10.1186/s12936-017-2139-7.

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Comparative ophthalmic assessment of patients receiving tafenoquine or chloroquine/primaquine in a randomized clinical trial for Plasmodium vivax malaria radical cure.

Warrasak S, Euswas A, Fukuda MM, Ittiverakul M, Miller RS, Krudsood S, Ohrt C.

Int Ophthalmol. 2018 Sep 29. doi: 10.1007/s10792-018-1003-2. [Epub ahead of print]

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Tafenoquine versus Primaquine to Prevent Relapse of Plasmodium vivax Malaria.

Llanos-Cuentas A, Lacerda MVG, Hien TT, Vélez ID, Namaik-Larp C, Chu CS, Villegas MF, Val F, Monteiro WM, Brito MAM, Costa MRF, Chuquiyauri R, Casapía M, Nguyen CH, Aruachan S, Papwijitsil R, Nosten FH, Bancone G, Angus B, Duparc S, Craig G, Rousell VM, Jones SW, Hardaker E, Clover DD, Kendall L, Mohamed K, Koh GCKW, Wilches VM, Breton JJ, Green JA.

N Engl J Med. 2019 Jan 17;380(3):229-241. doi: 10.1056/NEJMoa1802537.

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Enantioselective metabolism of primaquine by human CYP2D6.

Fasinu PS, Tekwani BL, Nanayakkara NP, Avula B, Herath HM, Wang YH, Adelli VR, Elsohly MA, Khan SI, Khan IA, Pybus BS, Marcsisin SR, Reichard GA, McChesney JD, Walker LA.

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The chemotherapy of rodent malaria. LXI. Drug combinations to impede the selection of drug resistance, part 4: the potential role of 8-aminoquinolines.

Peters W, Stewart LB, Robinson BL.

Ann Trop Med Parasitol. 2003 Apr;97(3):221-36.

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Primaquine ineligibility in anti-relapse therapy of Plasmodium vivax malaria: the problem of G6PD deficiency and cytochrome P-450 2D6 polymorphisms.

Baird JK, Battle KE, Howes RE.

Malar J. 2018 Jan 22;17(1):42. doi: 10.1186/s12936-018-2190-z.

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A randomized, double-blind, active-control trial to evaluate the efficacy and safety of a three day course of tafenoquine monotherapy for the treatment of Plasmodium vivax malaria.

Fukuda MM, Krudsood S, Mohamed K, Green JA, Warrasak S, Noedl H, Euswas A, Ittiverakul M, Buathong N, Sriwichai S, Miller RS, Ohrt C.

PLoS o­ne. 2017 Nov 9;12(11):e0187376. doi: 10.1371/journal.pone.0187376. eCollection 2017.

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Randomized trial of primaquine hypnozoitocidal efficacy when administered with artemisinin-combined blood schizontocides for radical cure of Plasmodium vivax in Indonesia.

Nelwan EJ, Ekawati LL, Tjahjono B, Setiabudy R, Sutanto I, Chand K, Ekasari T, Djoko D, Basri H, Taylor WR, Duparc S, Subekti D, Elyazar I, Noviyanti R, Sudoyo H, Baird JK.

BMC Med. 2015 Dec 11;13:294. doi: 10.1186/s129 16-015-0535-9.

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Efficacy and safety of chloroquine for treatment in patients with uncomplicated Plasmodium vivax infections in endemic countries.

Naing C, Aung K, Win DK, Wah MJ.

Trans R Soc Trop Med Hyg. 2010 Nov;104(11):695-705. doi: 10.1016/j.trstmh.2010.08.009.Epub 2010 Sep 20. Review.

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Tafenoquine and NPC-1161B require CYP 2D metabolism for anti-malarial activity: implications for the 8-aminoquinoline class of anti-malarial compounds.

Marcsisin SR, Sousa JC, Reichard GA, Caridha D, Zeng Q, Roncal N, McNulty R, Careagabarja J, Sciotti RJ, Bennett JW, Zottig VE, Deye G, Li Q, Read L, Hickman M, Dhammika Nanayakkara NP, Walker LA, Smith B, Melendez V, Pybus BS.

Malar J. 2014 Jan 3;13:2. doi: 10.1186/1475-2875-13-2.

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Implications of current therapeutic restrictions for primaquine and tafenoquine in the radical cure of vivax malaria.

Watson J, Taylor WRJ, Bancone G, Chu CS, Jittamala P, White NJ.

PLoS Negl Trop Dis. 2018 Apr 20;12(4):e0006440. doi: 10.1371/journal.pntd.0006440. eCollection 2018 Apr.

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A randomised trial of an eight-week, o­nce weekly primaquine regimen to prevent relapse of plasmodium vivax in Northwest Frontier Province, Pakistan.

Leslie T, Mayan I, Mohammed N, Erasmus P, Kolaczinski J, Whitty CJ, Rowland M.

PLoS o­ne. 2008 Aug 6;3(8):e2861. doi: 10.1371/journal.pone.0002861.

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Artemisinin-naphthoquine combination versus chloroquine-primaquine to treat vivax malaria: an open-label randomized and non-inferiority trial in Yunnan Province, China.

Liu H, Yang HL, Xu JW, Wang JZ, Nie RH, Li CF.

Malar J. 2013 Nov 11;12:409. doi: 10.1186/1475-2875-12-409.

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Strategies for understanding and reducing the Plasmodium vivax and Plasmodium ovale hypnozoite reservoir in Papua New Guinean children: A randomised placebo-controlled trial and mathematical model.

Robinson LJ, Wampfler R, Betuela I, Karl S, White MT, Li Wai Suen CS, Hofmann NE, Kinboro B, Waltmann A, Brewster J, Lorry L, Tarongka N, Samol L, Silkey M, Bassat Q, Siba PM, Schofield L, Felger I, Mueller I.

PLoS Med. 2015 Oct 27;12(10):e1001891. doi: 10.1371/journal.pmed.1001891. eCollection 2015 Oct.

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The blood schizonticidal activity of tafenoquine makes an essential contribution to its prophylactic efficacy in nonimmune subjects at the intended dose (200 mg).

Dow G, Smith B.

Malar J. 2017 May 19;16(1):209. doi: 10.1186/s12936-017-1862-4. Review.

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Blood stage of Plasmodium vivax in central China is still susceptible to chloroquine plus primaquine combination therapy.

Zhu G, Lu F, Cao J, Zhou H, Liu Y, Han ET, Gao Q.

Am J Trop Med Hyg. 2013 Jul;89(1):184-7. doi: 10.4269/ajtmh.12-0683. Epub 2013 May 13.

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Primaquine in vivax malaria: an update and review o­n management issues.

Fernando D, Rodrigo C, Rajapakse S.

Malar J. 2011 Dec 12;10:351. doi: 10.1186/1475-2875-10-351. Review.

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Association of Impaired Cytochrome P450 2D6 Activity Genotype and Phenotype With Therapeutic Efficacy of Primaquine Treatment for Latent Plasmodium vivax Malaria.

Baird JK, Louisa M, Noviyanti R, Ekawati L, Elyazar I, Subekti D, Chand K, Gayatri A, Instiaty, Soebianto S, Crenna-Darusallam C, Djoko D, Hasto BD, Meriyenes D, Wesche D, Nelwan EJ, Sutanto I, Sudoyo H, Setiabudy R.

JAMA Netw Open. 2018 Aug 3;1(4):e181449. doi: 10.1001/jamanetworkopen.2018.1449.

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Randomized dose-ranging study of the safety and efficacy of WR 238605 (Tafenoquine) in the prevention of relapse of Plasmodium vivax malaria in Thailand.

Walsh DS, Looareesuwan S, Wilairatana P, Heppner DG Jr, Tang DB, Brewer TG, Chokejindachai W, Viriyavejakul P, Kyle DE, Milhous WK, Schuster BG, Horton J, Braitman DJ, Brueckner RP.

J Infect Dis. 1999 Oct;180(4):1282-7.

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Tafenoquine and its potential in the treatment and relapse prevention of Plasmodium vivax malaria: the evidence to date.

Ebstie YA, Abay SM, Tadesse WT, Ejigu DA.

Drug Des Devel Ther. 2016 Jul 26;10:2387-99. doi: 10.2147/DDDT.S61443. eCollection 2016. Review.

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Efficacy of three chloroquine-primaquine regimens for treatment of Plasmodium vivax malaria in Colombia.

Alvarez G, Piñeros JG, Tobón A, Ríos A, Maestre A, Blair S, Carmona-Fonseca J.

Am J Trop Med Hyg. 2006 Oct;75(4):605-9.Erratum in: Am J Trop Med Hyg. 2006 Dec;75(6):1238.

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In vivo therapeutic efficacy of chloroquine alone or in combination with primaquine against vivax malaria in Kolkata, West Bengal, India, and polymorphism in pvmdr1 and pvcrt-o genes.

Ganguly S, Saha P, Guha SK, Das S, Bera DK, Biswas A, Kundu PK, Saha B, Ray K, Maji AK.

Antimicrob Agents Chemother. 2013 Mar;57(3):1246-51. doi: 10.1128/AAC.02050-12. Epub 2012 Dec 21.

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The metabolism of primaquine to its active metabolite is dependent o­n CYP 2D6.

Pybus BS, Marcsisin SR, Jin X, Deye G, Sousa JC, Li Q, Caridha D, Zeng Q, Reichard GA, Ockenhouse C, Bennett J, Walker LA, Ohrt C, Melendez V.

Malar J. 2013 Jun 20;12:212. doi: 10.1186/1475-2875-12-212.

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A pilot randomized controlled trial to compare the effectiveness of two 14-day primaquine regimens for the radical cure of vivax malaria in South India.

Saravu K, Tellapragada C, Kulavalli S, Xavier W, Umakanth S, Brahmarouphu G, Srinivas NK, Channabasavaiah JP, Bava A, Saadi AV, Guddattu V, Satyamoorthy K, Bhat K.

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[Plasmodium vivax malaria: treatment of primary attacks with primaquine, in three different doses, and a fixed dose of chloroquine, Antioquia, Colombia, 2003-2004].

Carmona-Fonseca J, Alvarez G.

Biomedica. 2006 Sep;26(3):353-65. Spanish.

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Defining Plasmodium falciparum treatment in South West Asia: a randomized trial comparing artesunate or primaquine combined with chloroquine or SP.

Kolaczinski K, Leslie T, Ali I, Durrani N, Lee S, Barends M, Beshir K, Ord R, Hallett R, Rowland M.

PLoS o­ne. 2012;7(1):e28957. doi: 10.1371/journal.pone.0028957. Epub 2012 Jan 31.

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Monitoring of clinical efficacy and in vitro sensitivity of Plasmodium vivax to chloroquine in area along Thai Myanmar border during 2009-2010.

Muhamad P, Ruengweerayut R, Chacharoenkul W, Rungsihirunrat K, Na-Bangchang K.

Malar J. 2011 Feb 16;10:44. doi: 10.1186/1475-2875-10-44.

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Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.

Karunajeewa HA, Ilett KF, Mueller I, Siba P, Law I, Page-Sharp M, Lin E, Lammey J, Batty KT, Davis TM.

Antimicrob Agents Chemother. 2008 Jan;52(1):237-43. Epub 2007 Oct 29.

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[Plasmodium vivax malaria recurrence according to the use of primaquine: analysis of longitudinal descriptive studies].

Carmona-Fonseca J.

Rev Bras Epidemiol.2012 Sep;15(3):488-503. Review. Spanish.

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Evaluation of antimalarial activity and toxicity of a new primaquine prodrug.

Davanço MG, Aguiar AC, Dos Santos LA, Padilha EC, Campos ML, de Andrade CR, da Fonseca LM, Dos Santos JL, Chin CM, Krettli AU, Peccinini RG.

PLoS o­ne. 2014 Aug 18;9(8):e105217. doi: 10.1371/journal.pone.0105217. eCollection 2014.

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The efficacy and tolerability of three different regimens of tafenoquine versus primaquine for post-exposure prophylaxis of Plasmodium vivax malaria in the Southwest Pacific.

Elmes NJ, Nasveld PE, Kitchener SJ, Kocisko DA, Edstein MD.

Trans R Soc Trop Med Hyg. 2008 Nov;102(11):1095-101. doi: 10.1016/j.trstmh.2008.04.024.Epub 2008 Jun 9.

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CYP450 phenotyping and accurate mass identification of metabolites of the 8-aminoquinoline, anti-malarial drug primaquine.

Pybus BS, Sousa JC, Jin X, Ferguson JA, Christian RE, Barnhart R, Vuong C, Sciotti RJ, Reichard GA, Kozar MP, Walker LA, Ohrt C, Melendez V.

Malar J. 2012 Aug 2;11:259. doi: 10.1186/1475-2875-11-259.

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Differential CYP 2D6 metabolism alters primaquine pharmacokinetics.

Potter BM, Xie LH, Vuong C, Zhang J, Zhang P, Duan D, Luong TL, Bandara Herath HM, Dhammika Nanayakkara NP, Tekwani BL, Walker LA, Nolan CK, Sciotti RJ, Zottig VE, Smith PL, Paris RM, Read LT, Li Q, Pybus BS, Sousa JC, Reichard GA, Marcsisin SR.

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Triangular test design to evaluate tinidazole in the prevention of Plasmodium vivax relapse.

Macareo L, Lwin KM, Cheah PY, Yuentrakul P, Miller RS, Nosten F.

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Metabolism of primaquine in normal human volunteers: investigation of phase I and phase II metabolites from plasma and urine using ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry.

Avula B, Tekwani BL, Chaurasiya ND, Fasinu P, Dhammika Nanayakkara NP, Bhandara Herath HMT, Wang YH, Bae JY, Khan SI, Elsohly MA, McChesney JD, Zimmerman PA, Khan IA, Walker LA.

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Short report: primaquine-tolerant Plasmodium vivax in an Italian traveler from Guatemala.

Signorini L, Matteelli A, Castelnuovo F, Castelli F, Oladeji O, Carosi G.

Am J Trop Med Hyg. 1996 Nov;55(5):472-3.

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Malaria prophylaxis/radical cure: recent experiences of the Australian Defence Force.

Edstein MD, Walsh DS, Eamsila C, Sasiprapha T, Nasveld PE, Kitchener S, Rieckmann KH.

Med Trop (Mars). 2001;61(1):56-8. Review.

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Therapeutic efficacy of alternative primaquine regimens to standard treatment in preventing relapses by Plasmodium vivax: A systematic review and meta-analysis.

Zuluaga-Idarraga LM, Tamayo Perez ME, Aguirre-Acevedo DC.

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The clinical and public health problem of relapse despite primaquine therapy: case review of repeated relapses of Plasmodium vivax acquired in Papua New Guinea.

Ingram RJ, Crenna-Darusallam C, Soebianto S, Noviyanti R, Baird JK.

Malar J. 2014 Dec 12;13:488. doi: 10.1186/1475-2875-13-488.

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Validation of a method for the simultaneous quantification of chloroquine, desethylchloroquine and primaquine in plasma by HPLC-DAD.

Zuluaga-Idárraga L, Yepes-Jiménez N, López-Córdoba C, Blair-Trujillo S.

J Pharm Biomed Anal. 2014 Jul;95:200-6. doi: 10.1016/j.jpba.2014.03.006. Epub 2014 Mar 12.

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Studies o­n Plasmodium vivax relapse pattern in Kheda district, Gujarat.

Srivastava HC, Sharma SK, Bhatt RM, Sharma VP.

Indian J Malariol. 1996 Dec;33(4):173-9.

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Resistance of infection by Plasmodium vivax to chloroquine in Bolivia.

Añez A, Moscoso M, Laguna Á, Garnica C, Melgar V, Cuba M, Gutierrez S, Ascaso C.

Malar J. 2015 Jul 1;14:261. doi: 10.1186/s12936-015-0774-4.

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Compliance with 14-day primaquine therapy for radical cure of vivax malaria--a randomized placebo-controlled trial comparing unsupervised with supervised treatment.

Leslie T, Rab MA, Ahmadzai H, Durrani N, Fayaz M, Kolaczinski J, Rowland M.

Trans R Soc Trop Med Hyg. 2004 Mar;98(3):168-73.

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Pharmacokinetics and pharmacodynamics of (+)-primaquine and (-)-primaquine enantiomers in rhesus macaques (Macaca mulatta).

Saunders D, Vanachayangkul P, Imerbsin R, Khemawoot P, Siripokasupkul R, Tekwani BL, Sampath A, Nanayakkara NP, Ohrt C, Lanteri C, Gettyacamin M, Teja-Isavadharm P, Walker L.

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Kaewpruk N, Tan-ariya P, Ward SA, Sitthichot N, Suwandittakul N, Mungthin M.

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