Tafenoquine

(BAN, rINN)
Tafenoquine Chemical formula
Synonyms: Tafenoquina; Tafénoquine; Tafenoquinum; WR-238605. (±)-8[(4-Amino-1-methylbutyl)amino]-2,6-dimethoxy-4-methyl-5[( 4 -[2,6-Dimethoxy4-methyl-5-(3-trifluoromethylphenoxy)quinolin-8-yl]pentane1,4-diamine.
Cyrillic synonym: Тафенохин.

Chemical information

Chemical formula: C24H28F3N3O3 = 463.5.
CAS — 106635-80-7.

Profile

Tafenoquine is an 8-aminoquinoline antimalarial. It acts as a tissue schizontocide and is under investigation as the succinate for the radical cure and prevention of relapse in vivax malaria. It may also have a role in the prophylaxis of falciparum malaria.
1. Walsh DS, et al. Randomized dose-ranging study of the safety and efficacy of WR 238605 (tafenoquine) in the prevention of relapse of Plasmodium vivax malaria in Thailand. J Infect Dis 1999; 180: 1282–7
2. Lell B, et al. Malaria chemoprophylaxis with tafenoquine: a randomised study. Lancet 2000; 355: 2041–5
3. Shanks GD, et al. A new primaquine analogue, tafenoquine (WR 238605), for prophylaxis against Plasmodium falciparum malaria. Clin Infect Dis 2001; 33: 1968–74
4. Nasveld P, et al. Comparison of tafenoquine (WR238605) and primaquine in the post-exposure (terminal) prophylaxis of vivax malaria in Australian Defence Force personnel. Trans R Soc Trop Med Hyg 2002; 96: 683–4
5. Hale BR, et al. A randomized, double-blind, placebo-controlled, dose-ranging trial of tafenoquine for weekly prophylaxis against Plasmodium falciparum. Clin Infect Dis 2003; 36: 541–9
6. Walsh DS, et al. Randomized trial of 3-dose regimens of tafenoquine (WR238605) versus low-dose primaquine for preventing Plasmodium vivax malaria relapse. Clin Infect Dis 2004; 39: 1095–1103
7. Walsh DS, et al. Efficacy of monthly tafenoquine for prophylaxis of Plasmodium vivax and multidrug-resistant P. falciparum malaria. J Infect Dis 2004; 190: 1456–63.
Published October 07, 2018.