Tafenoquine: A 2018 Novel FDA-Approved Prodrug for the Radical Cure of Plasmodium vivax Malaria and Prophylaxis of Malaria

被引：13

作者：

Mayence, Annie ^{[1
]}

Vanden Eynde, Jean Jacques ^{[2
]}

机构：

[1] Haute Ecole Prov Hainaut Condorcet, B-7330 Saint Ghislain, Belgium

[2] Univ Mons UMONS, Dept Organ Chem FS, B-7000 Mons, Belgium

来源：

PHARMACEUTICALS | 2019年 / 12卷 / 03期

基金：

美国国家卫生研究院;

关键词：

aminoquinoline; approved drugs; FDA; hypnozoite; malaria; Plasmodium; PREVENT RELAPSE; SAFETY;

D O I：

10.3390/ph12030115

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Tafenoquine (an 8-aminoquinoline) was approved by the Food and Drug Administration (FDA) in 2018 for the radical cure of Plasmodium vivax malaria and preventive action against malaria. Despite the fact that the mechanism of action of the drug remains unclear, all studies indicated that a metabolite is responsible for its efficacy. Routes for the preparation of the drug are described.

引用

页数：7

共 13 条

[1]

Allgower Andrea, 2016, Rev Med Suisse, V12, P878

[2] First-time-in-humans safety and pharmacokinetics of WR 238605, a new antimalarial [J].

Brueckner, RP ;

Lasseter, KC ;

Lin, ET ;

Schuster, BG .

AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE, 1998, 58 (05) :645-649

[3] Killing the hypnozoite - drug discovery approaches to prevent relapse in Plasmodium vivax [J].

Campo, Brice ;

Vandal, Omar ;

Wesche, David L. ;

Burrows, Jeremy N. .

PATHOGENS AND GLOBAL HEALTH, 2015, 109 (03) :107-122

[4] The Activities of Current Antimalarial Drugs on the Life Cycle Stages of Plasmodium: A Comparative Study with Human and Rodent Parasites [J].

Delves, Michael ;

Plouffe, David ;

Scheurer, Christian ;

Meister, Stephan ;

Wittlin, Sergio ;

Winzeler, Elizabeth A. ;

Sinden, Robert E. ;

Leroy, Didier .

PLOS MEDICINE, 2012, 9 (02)

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

Li, Qigui ;

O'Neil, Michael ;

Xie, Lisa ;

Caridha, Diana ;

Zeng, Qiang ;

Zhang, Jing ;

Pybus, Brandon ;

Hickman, Mark ;

Melendez, Victor .

MALARIA JOURNAL, 2014, 13

[6] Tafenoquine versus Primaquine to Prevent Relapse of Plasmodium vivax Malaria [J].

Llanos-Cuentas, A. ;

Lacerda, M. V. G. ;

Hien, T. T. ;

Velez, I. D. ;

Namaik-Iarp, C. ;

Chu, C. S. ;

Villegas, M. F. ;

Val, F. ;

Monteiro, W. M. ;

Brito, M. A. M. ;

Costa, M. R. F. ;

Chuquiyauri, R. ;

Casapia, M. ;

Nguyen, C. H. ;

Aruachan, S. ;

Papwijitsil, R. ;

Nosten, F. H. ;

Bancone, G. ;

Angus, B. ;

Duparc, S. ;

Craig, G. ;

Rousell, V. M. ;

Jones, S. W. ;

Hardaker, E. ;

Clover, D. D. ;

Kendall, L. ;

Mohamed, K. ;

Koh, G. C. K. W. ;

Wilches, V. M. ;

Breton, J. J. ;

Green, J. A. .

NEW ENGLAND JOURNAL OF MEDICINE, 2019, 380 (03) :229-241

[7] Primaquine pharmacology in the context of CYP 2D6 pharmacogenomics: Current state of the art [J].

Marcsisin, Sean R. ;

Reichard, Gregory ;

Pybus, Brandon S. .

PHARMACOLOGY & THERAPEUTICS, 2016, 161 :1-10

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

Marcsisin, Sean R. ;

Sousa, Jason C. ;

Reichard, Gregory A. ;

Caridha, Diana ;

Zeng, Qiang ;

Roncal, Norma ;

McNulty, Ronan ;

Careagabarja, Julio ;

Sciotti, Richard J. ;

Bennett, Jason W. ;

Zottig, Victor E. ;

Deye, Gregory ;

Li, Qigui ;

Read, Lisa ;

Hickman, Mark ;

Nanayakkara, N. P. Dhammika ;

Walker, Larry A. ;

Smith, Bryan ;

Melendez, Victor ;

Pybus, Brandon S. .

MALARIA JOURNAL, 2014, 13

[9] Pharmacokinetic interactions and safety evaluations of coadministered tafenoquine and chloroquine in healthy subjects [J].

Miller, Ann K. ;

Harrell, Emma ;

Ye, Li ;

Baptiste-Brown, Sharon ;

Kleim, Jorg-Peter ;

Ohrt, Colin ;

Duparc, Stephan ;

Moehrle, Joerg J. ;

Webster, Alison ;

Stinnett, Sandra ;

Hughes, Arlene ;

Griffith, Sandy ;

Beelen, Andrew P. .

BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 2013, 76 (06) :858-867

[10] Tafenoquine for malaria prophylaxis in adults: An integrated safety analysis [J].

Novitt-Moreno, Anne ;

Ransom, Janet ;

Dow, Geoffrey ;

Smith, Bryan ;

Read, Lisa Thomas ;

Toovey, Stephen .

TRAVEL MEDICINE AND INFECTIOUS DISEASE, 2017, 17 :19-27

← 1 2 →