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Antimalarial Activity of KAF156 in Falciparum and Vivax Malaria.

White NJ, Duong TT, Uthaisin C, Nosten F, Phyo AP, Hanboonkunupakarn B, Pukrittayakamee S, Jittamala P, Chuthasmit K, Cheung MS, Feng Y, Li R, Magnusson B, Sultan M, Wieser D, Xun X, Zhao R, Diagana TT, Pertel P, Leong FJ.

N Engl J Med. 2016 Sep 22;375(12):1152-60. doi: 10.1056/NEJMoa1602250.


Safety and clinical pharmacokinetics of nemonoxacin, a novel non-fluorinated quinolone, in healthy Chinese volunteers following single and multiple oral doses.

Guo B, Wu X, Zhang Y, Shi Y, Yu J, Cao G, Zhang J.

Clin Drug Investig. 2012 Jul 1;32(7):475-86. doi: 10.2165/11632780-000000000-00000.


Differential pharmacokinetics of diclofenac potassium for oral solution vs immediate-release tablets from a randomized trial: effect of fed and fasting conditions.

Chen C, Bujanover S, Kareht S, Rapoport AM.

Headache. 2015 Feb;55(2):265-75. doi: 10.1111/head.12483. Epub 2014 Dec 24.


Pharmacokinetics, safety, and tolerability of GLPG0259, a mitogen-activated protein kinase-activated protein kinase 5 (MAPKAPK5) inhibitor, given as single and multiple doses to healthy male subjects.

Namour F, Vanhoutte FP, Beetens J, Blockhuys S, De Weer M, Wigerinck P.

Drugs R D. 2012 Sep 1;12(3):141-63. doi: 10.2165/11633120-000000000-00000.


Pharmacokinetics and safety of escalating single and repeat oral doses of GW420867X, a novel non-nucleoside reverse transcriptase inhibitor.

Moore KH, Cass LM, Dallow N, Hardman TC, Jones A, Boyce M, Prince WT.

Eur J Clin Pharmacol. 2001 Jan-Feb;56(11):805-11.


Tolerability, pharmacokinetics and concentration-dependent hemodynamic effects of oral CF101, an A3 adenosine receptor agonist, in healthy young men.

van Troostenburg AR, Clark EV, Carey WD, Warrington SJ, Kerns WD, Cohn I, Silverman MH, Bar-Yehuda S, Fong KL, Fishman P.

Int J Clin Pharmacol Ther. 2004 Oct;42(10):534-42.


A first-in-human, randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study to assess the safety and tolerability of LFF571 in healthy volunteers.

Ting LS, Praestgaard J, Grunenberg N, Yang JC, Leeds JA, Pertel P.

Antimicrob Agents Chemother. 2012 Nov;56(11):5946-51. doi: 10.1128/AAC.00867-12. Epub 2012 Sep 10.


Safety, tolerability and pharmacokinetics of trimebutine 3-thiocarbamoylbenzenesulfonate (GIC-1001) in a randomized phase I integrated design study: single and multiple ascending doses and effect of food in healthy volunteers.

Paquette JM, Rufiange M, Iovu Niculita M, Massicotte J, Lefebvre M, Colin P, Telmat A, Ranger M.

Clin Ther. 2014 Nov 1;36(11):1650-64. doi: 10.1016/j.clinthera.2014.08.005. Epub 2014 Sep 15.


Single- and multiple-ascending dose studies to evaluate the safety, tolerability, and pharmacokinetics of daclatasvir and asunaprevir in healthy male Japanese subjects.

Shiozaki T, Ueno T, Nagashima H, Yamahira N, Hiraoka M, Eley T, Bifano M, Bertz RJ.

Int J Clin Pharmacol Ther. 2015 Apr;53(4):292-302. doi: 10.5414/CP202186.


Safety, tolerability and pharmacokinetics of dalcetrapib following single and multiple ascending doses in healthy subjects: a randomized, double-blind, placebo-controlled, phase I study.

Derks M, Anzures-Cabrera J, Turnbull L, Phelan M.

Clin Drug Investig. 2011;31(5):325-35. doi: 10.2165/11533550-000000000-00000.


Antimalarial activity of artefenomel (OZ439), a novel synthetic antimalarial endoperoxide, in patients with Plasmodium falciparum and Plasmodium vivax malaria: an open-label phase 2 trial.

Phyo AP, Jittamala P, Nosten FH, Pukrittayakamee S, Imwong M, White NJ, Duparc S, Macintyre F, Baker M, Möhrle JJ.

Lancet Infect Dis. 2016 Jan;16(1):61-9. doi: 10.1016/S1473-3099(15)00320-5. Epub 2015 Oct 5.


Phase I clinical studies of the advanced glycation end-product (AGE)-breaker TRC4186: safety, tolerability and pharmacokinetics in healthy subjects.

Chandra KP, Shiwalkar A, Kotecha J, Thakkar P, Srivastava A, Chauthaiwale V, Sharma SK, Cross MR, Dutt C.

Clin Drug Investig. 2009;29(9):559-75. doi: 10.2165/11315260-000000000-00000.


Single and Multiple Ascending-dose Studies of Oral Delafloxacin: Effects of Food, Sex, and Age.

Hoover R, Hunt T, Benedict M, Paulson SK, Lawrence L, Cammarata S, Sun E.

Clin Ther. 2016 Jan 1;38(1):39-52. doi: 10.1016/j.clinthera.2015.10.016. Epub 2015 Nov 12.


KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission.

Kuhen KL, Chatterjee AK, Rottmann M, Gagaring K, Borboa R, Buenviaje J, Chen Z, Francek C, Wu T, Nagle A, Barnes SW, Plouffe D, Lee MC, Fidock DA, Graumans W, van de Vegte-Bolmer M, van Gemert GJ, Wirjanata G, Sebayang B, Marfurt J, Russell B, Suwanarusk R, Price RN, Nosten F, Tungtaeng A, Gettayacamin M, Sattabongkot J, Taylor J, Walker JR, Tully D, Patra KP, Flannery EL, Vinetz JM, Renia L, Sauerwein RW, Winzeler EA, Glynne RJ, Diagana TT.

Antimicrob Agents Chemother. 2014 Sep;58(9):5060-7. doi: 10.1128/AAC.02727-13. Epub 2014 Jun 9.


Clinical pharmacology of DP-b99 in healthy volunteers: first administration to humans.

Rosenberg G, Angel I, Kozak A.

Br J Clin Pharmacol. 2005 Jul;60(1):7-16.

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