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artemether

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Description

Artemether is a semisynthetic antimalarial drug derived from artemisinin, a natural compound extracted from the sweet wormwood plant (Artemisia annua). It is synthesized by reacting artemisinin with sodium borohydride. Artemether exhibits rapid and potent antimalarial activity, particularly against Plasmodium falciparum, the most deadly species of malaria parasite. It is effective in treating both uncomplicated and severe malaria. Artemether's mechanism of action involves generating free radicals that disrupt the parasite's heme detoxification pathway, leading to oxidative stress and cell death. Its rapid action and effectiveness against multidrug-resistant parasites have made it a crucial component of artemisinin-based combination therapies (ACTs), the current gold standard for malaria treatment. Artemether is studied extensively to understand its pharmacokinetic properties, optimize its therapeutic efficacy, and explore its potential applications in other diseases, such as cancer and viral infections.'
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Artemether: An artemisinin derivative that is used in the treatment of MALARIA. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

artemether : An artemisinin derivative that is artemisinin in which the lactone has been converted to the corresponding lactol methyl ether. It is used in combination with lumefantrine as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID68911
CHEMBL ID566534
CHEBI ID195280
SCHEMBL ID1650501
MeSH IDM0102449

Synonyms (70)

Synonym
AB00698368-05
qinghao
artemisininelactol methyl ether
sm-224
artemos
artenam
artimist
paluther
artemetheri
artemether (jan/usan/inn)
D02483
nsc 665970
hsdb 7456
artemetero [inn-spanish]
3,12-epoxy-12h-pyrano(4,3-j)-1,2-benzodioxepin, decahydro-10-methoxy-3,6,9-trimethyl-, (3-alpha,5a-beta,6-beta,8a-beta,9-alpha,12-beta,12ar)-, (+)-
beta-dihydroartemisinin methyl ether
artemetherum [inn-latin]
methyl-dihydroartemisinine
beta-artemether
sm 224
dihydroquinghaosu methyl ether
artemether
methoxy(trimethyl)[?]
3,12-epoxy-12h-pyrano[4,3-j]-1,2-benzodioxepin, decahydro-10-methoxy-3,6,9-trimethyl-, (3r,5as,6r,8as,9r,10s,12r,12ar)-
dihydroartemisinin methyl ether
MLS001424249
smr000469218
cpd000469218
NCGC00164591-01
HMS2052L09
DB06697
10-methoxy-1,5,9-trimethyl-(1r,4s,5r,8s,9r,10s,12r,13r)-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecane
dihydroqinghaosu methyl ether
(1r,4s,5r,8s,9r,10s,12r,13r)-10-methoxy-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0^{4,13}.0^{8,13}]hexadecane
CHEBI:195280 ,
(1r,4s,5r,8s,9r,10s,12r,13r)-10-methoxy-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0;{4,13}.0;{8,13}]hexadecane
(3r,5as,6r,8as,9r,10s,12r,12ar)-10-methoxy-3,6,9-trimethyldecahydro-3,12-epoxypyrano[4,3-j][1,2]benzodioxepine
artemetero
artemetherum
CHEMBL566534
dihydroartemisinin impurity g
unii-c7d6t3h22j
artemether [usan:inn:ban]
dtxcid30819889
dtxsid7040651 ,
cas-71963-77-4
tox21_112217
HMS2232J21
CCG-101180
HY-N0402
NC00430
SCHEMBL1650501
AB00698368_06
AKOS026750084
artemether, >=98% (hplc)
cgp 56696
artemether, united states pharmacopeia (usp) reference standard
(3r,5as,6r,8as,9r,10s,12r,12ar)-10-methoxy-3,6,9-trimethyldecahydro-3h-3,12-epoxy[1,2]dioxepino[4,3-i]isochromene
bdbm50248200
Q416199
2-chloro-3,5-dimethyl-4-methoxypyridinehydrochloride
Z1541759910
SXYIRMFQILZOAM-HVNFFKDJSA-N
beta artemether
AMY25769
gtpl9955
EN300-122380
d8z ,
(3r,5as,6r,8as,9r,10s,12r,12ar)-decahydro-10methoxy-3,6,9-trimethyl-3,12-epoxy-12h-pyrano[4,3-j]-1,2benzodioxepin
artemether 100 microg/ml in acetonitrile

Research Excerpts

Overview

Artemether (ATM) is a natural antimalarial drug that can also regulate glucose and lipid metabolism. Artemether-lumefantrine is a first-line regimen for the treatment of uncomplicated malaria during the second and third trimesters of pregnancy.

ExcerptReferenceRelevance
"Artemether (ART) is a lactone with antitumor properties, demonstrating low bioavailability and water solubility."( Artemether-loaded polymeric lipid-core nanocapsules reduce cell viability and alter the antioxidant status of U-87 MG cells.
Andrade, CMB; Branco, CLB; Costa, SA; Cruz, L; da Conceição, AGB; da Silva, KP; Ferrarini, SR; Pires, J; Reis, ÉM; Sinhorin, AP, 2022
)
2.89
"Artemether (ATM) is a natural antimalarial drug that can also regulate glucose and lipid metabolism. "( Therapeutic role of Artemether in the prevention of hepatic steatosis through miR-34a-5p/PPARα pathway.
Cao, X; Chen, L; Hong, S; Li, Y; Lin, X; Xiao, H; Yu, S; Zhu, X, 2023
)
2.68
"Artemether is a well‑known Chinese herbal medicine, and its pharmacological action is related to the regulation of mitochondrial function and redox status."( Artemether ameliorates adriamycin induced cardiac atrophy in mice.
Dong, Y; Han, P; Shao, M; Sun, H; Wang, T; Weng, W; Yu, X, 2023
)
3.07
"Artemether-lumefantrine is an artemisinin-based combination therapy for the treatment of malaria, which are primarily metabolized by cytochrome P450 3A4. "( Determine the enzymatic kinetic characteristics of CYP3A4 variants utilizing artemether-lumefantrine.
Cai, J; Chen, G; Hu, G; Jin, L; Li, J; Li, Q; Li, S; Li, Y; Qian, J; Zhang, X; Zhou, Q, 2023
)
2.58
"Artemether is a natural compound derived from Artemisia annua L."( Artemether attenuates LPS-induced inflammatory bone loss by inhibiting osteoclastogenesis and bone resorption via suppression of MAPK signaling pathway.
Hu, B; Meng, J; Shi, Z; Wu, H; Yan, S; Yang, Y; Zhao, X; Zhou, C; Zhou, X, 2018
)
2.64
"Artemether-lumefantrine is a first-line regimen for the treatment of uncomplicated malaria during the second and third trimesters of pregnancy. "( Artemether-Lumefantrine Pharmacokinetics and Clinical Response Are Minimally Altered in Pregnant Ugandan Women Treated for Uncomplicated Falciparum Malaria.
Achan, J; Aweeka, F; Huang, L; Kajubi, R; Kiconco, S; Mwebaza, N; Mwima, MW; Nguyen, VK; Nyunt, MM; Parikh, S; Ssebuliba, J, 2015
)
3.3
"β-artemether (ARM) is a widely used anti-malarial drug isolated from the Chinese antimalarial plant, Artemisia annua. "( Solvents effects on crystallinity and dissolution of β-artemether
Gui, S; Guo, T; Singh, P; Singh, V; Sun, L; Wu, L; Xu, J; Xu, X; Yin, X; Zhang, J, 2017
)
1.42
"Artemether (ART) is a well-described antimalarial with efficacy against juvenile schistosomes, with 7-day-old schistosomula being particularly susceptible. "( Artemether treatment of prepatent Schistosoma japonicum induces resistance to reinfection in association with reduced pathology.
Bartley, PB; Duke, M; Glanfield, A; Jones, MK; Li, Y; McManus, DP; Stanisic, DI, 2008
)
3.23
"Artemether is an artemisinin derivative that is used as an antimalarial drug, especially in situations where chloroquine resistance is suspected. "( Artemether shows promising female schistosomicidal and ovicidal effects on the Egyptian strain of Schistosoma mansoni after maturity of infection.
Abdul-Ghani, R; Hassan, A; Loutfy, N; Sheta, M, 2011
)
3.25
"Artemether is an efficacious antimalarial drug that also displays antischistosomal properties. "( Randomized, double-blind, placebo-controlled trial of oral artemether for the prevention of patent Schistosoma haematobium infections.
Chollet, J; Gnaka, HN; Kigbafori, SD; Lengeler, C; N'Goran, EK; N'Guessan, NA; Shuhua, X; Tanner, M; Utzinger, J; Yapi, A, 2003
)
2
"Artemether-Lumefantrine is a newly developed artemisinin-based combination agent for the treatment of uncomplicated multi-drug resistant malaria."( [An imported case of falciparum malaria successfully treated with Artemether-Lumefantrine in Japan].
Hatabu, T; Ishizaki, A; Kano, S; Kikuchi, Y; Oka, S; Yasuoka, A, 2003
)
1.28
"Artemether is a good alternative drug to quinine for P."( A comparative clinical trial of artemether and quinine in children with severe malaria.
Afzal, K; Ali, SM; Huda, SN; Khan, HM; Shahab, T, 2003
)
1.32
"Artemether is an efficacious antimalarial drug that also displays antischistosomal properties. "( Effect of artemether alone and in combination with grapefruit juice on hepatic drug-metabolising enzymes and biochemical aspects in experimental Schistosoma mansoni.
Badawy, AA; Ebeid, FA; El-Lakkany, NM; Seif el-Din, SH, 2004
)
2.17
"Artemether is a derivative of the Chinese traditional remedy ginghaosu, and is chemically unrelated to quinine or other existing antimalarials."( Rapid coma resolution with artemether in Malawian children with cerebral malaria.
Chisale, M; Kazembe, P; Molyneux, ME; Ratsma, EY; Taylor, TE; Wills, BA; Wirima, JJ, 1993
)
1.2
"Artemether is a new antimalarial agent that clears parasites from the circulation more rapidly than quinine, but its effect on mortality is unclear."( A trial of artemether or quinine in children with cerebral malaria.
Bennett, S; Enwere, G; Forck, S; Frenkel, J; Greenwood, B; Jaffar, S; Kwiatkowski, D; Nusmeijer, A; Onyiorah, E; Palmer, A; Schneider, G; van Hensbroek, MB, 1996
)
1.41
"Artemether is a satisfactory alternative to quinine for the treatment of severe malaria in adults."( A controlled trial of artemether or quinine in Vietnamese adults with severe falciparum malaria.
Day, NP; Dinh, XS; Ha, V; Ly, VC; Nguyen, HP; Nguyen, TH; Peto, TE; Pham, PL; Tran, TH; Waller, D; White, NJ, 1996
)
2.05
"Coartemether is a fixed 1:6 ratio of artemether and lumefantrine (benflumetol), a joint development between Novartis Pharma and the Academy of Military Medical Sciences (Beijing, China). "( Positioning, labelling, and medical information control of co-artemether tablets (CPG 56697): a fixed novel combination of artemether and benflumetol. Novartis Co-Artemether International Development Team.
Mull, R; Skelton-Stroud, P, 1998
)
1.26
"Artemether is a new and effective treatment for malaria, although relapse is a problem in monotherapy. "( The effect of grapefruit juice on the time-dependent decline of artemether plasma levels in healthy subjects.
Gupta, V; van Agtmael, MA; van Boxtel, CJ; van der Graaf, CA, 1999
)
1.98
"Artemether-lumefantrine is a new fixed antimalarial combination effective against multidrug-resistant falciparum malaria. "( No evidence of cardiotoxicity during antimalarial treatment with artemether-lumefantrine.
Ezzet, F; Gathmann, I; Looareesuwan, S; Nosten, F; van Vugt, M; White, NJ; Wilairatana, P, 1999
)
1.98
"Co-artemether is an oral tablet of artemether (20 mg) and lumefantrine (120 mg) for the treatment of falciparum malaria. "( Cardiac effects of co-artemether (artemether/lumefantrine) and mefloquine given alone or in combination to healthy volunteers.
Bindschedler, M; Ezzet, F; Lefèvre, G; Meyer, I; Schaeffer, N; Thomsen, MS, 2000
)
1.24
"Artemether is an oil-soluble methyl ether of artemesinin (qinghaosu). "( Comparison of artemether and chloroquine for severe malaria in Gambian children.
Brewster, D; Chapman, D; Crawley, J; Greenwood, BM; Nosten, F; Waller, D; White, NJ, 1992
)
2.09

Effects

Artemether has an active metabolite, dihydroartemisinin. Artemether-lumefantrine has a high cure rate irrespective of whether given under supervision with food or under conditions of routine clinic practice.

Artemether has the potential to be an alternative antimalarial for multiple drug resistant falciparum malaria. Artemether-lumefantrine has a high cure rate irrespective of whether given under supervision with food or under conditions of routine clinic practice.

ExcerptReferenceRelevance
"Artemether has an active metabolite, dihydroartemisinin."( Pharmacokinetic interaction between etravirine or darunavir/ritonavir and artemether/lumefantrine in healthy volunteers: a two-panel, two-way, two-period, randomized trial.
DeMasi, R; Kakuda, TN; Mohammed, P; van Delft, Y, 2013
)
1.34
"Artemether-lumefantrine has a high cure rate irrespective of whether given under supervision with food or under conditions of routine clinic practice. "( Supervised versus unsupervised intake of six-dose artemether-lumefantrine for treatment of acute, uncomplicated Plasmodium falciparum malaria in Mbarara, Uganda: a randomised trial.
Babigumira, J; Bajunirwe, F; Biraro, S; Checchi, F; Ferradini, L; Fogg, C; Grandesso, F; Guthmann, JP; Kigozi, I; Kiguli, J; Kyomuhendo, J; Piola, P; Ruzagira, E; Taylor, W,
)
1.83
"Artemether has biological effects by targeting mitochondria and exhibits potential therapeutic value for kidney disease."( Artemether ameliorates kidney injury by restoring redox imbalance and improving mitochondrial function in Adriamycin nephropathy in mice.
Cai, Y; Chen, Y; Han, P; Shao, M; Sun, H; Wang, M; Wang, T; Wang, Y; Weng, W; Yu, X; Zhan, H, 2021
)
2.79
"Artemether has an active metabolite, dihydroartemisinin."( Pharmacokinetic interaction between etravirine or darunavir/ritonavir and artemether/lumefantrine in healthy volunteers: a two-panel, two-way, two-period, randomized trial.
DeMasi, R; Kakuda, TN; Mohammed, P; van Delft, Y, 2013
)
1.34
"Artemether also has potential therapeutic effects against tumors."( Artemether combined with shRNA interference of vascular cell adhesion molecule-1 significantly inhibited the malignant biological behavior of human glioma cells.
Hu, Y; Li, Z; Liu, YH; Wang, P; Wang, YB; Xue, YX; Yao, YL; Yu, B, 2013
)
2.55
"Artemether has been used for a long time in the treatment of malaria as safe and non expensive drug. "( Preparation and optimization of transferrin-modified-artemether lipid nanospheres based on the orthogonal design of emulsion formulation and physically electrostatic adsorption.
Eltayeb, SE; Li, S; Ping, Q; Shi, Y; Su, Z; Xiao, Y, 2013
)
2.08
"The artemether patch has long-releasing property."( [Studies on pharmacokinetics of artemether patch in mice].
He, C; Li, JS; Liang, BW; Wang, NJ; Yang, HS; Ye, ZG, 2008
)
1.19
"Artemether-lumefantrine has become one of the most widely used antimalarial drugs in the world. "( Population pharmacokinetics of lumefantrine in pregnant women treated with artemether-lumefantrine for uncomplicated Plasmodium falciparum malaria.
Annerberg, A; Ashley, EA; Day, NP; Kamanikom, B; Lindegardh, N; McGready, R; Nosten, F; Pimanpanarak, M; Singhasivanon, P; Stepniewska, K; Tarning, J; White, NJ, 2009
)
2.03
"Artemether has also been developed as an antischistosomal agent, exhibiting highest activity against immature parasites."( Selection and reversal of Plasmodium berghei resistance in the mouse model following repeated high doses of artemether.
Cai, Y; Chollet, J; Tanner, M; Utzinger, J; Xiao, SH; Yao, JM, 2004
)
1.26
"Artemether-lumefantrine has potential advantages over non-artemisinin regimens because of the faster clearance time and gametocyte clearance."( Artemether-lumefantrine for uncomplicated malaria: a systematic review.
Gamble, C; Garner, P; Omari, AA, 2004
)
2.49
"Artemether-lumefantrine has a high cure rate irrespective of whether given under supervision with food or under conditions of routine clinic practice. "( Supervised versus unsupervised intake of six-dose artemether-lumefantrine for treatment of acute, uncomplicated Plasmodium falciparum malaria in Mbarara, Uganda: a randomised trial.
Babigumira, J; Bajunirwe, F; Biraro, S; Checchi, F; Ferradini, L; Fogg, C; Grandesso, F; Guthmann, JP; Kigozi, I; Kiguli, J; Kyomuhendo, J; Piola, P; Ruzagira, E; Taylor, W,
)
1.83
"Artemether has the potential to be an alternative antimalarial for multiple drug resistant falciparum malaria. "( Artemether in the treatment of multiple drug resistant falciparum malaria.
Bunnag, D; Harinasuta, T; Karbwang, J, 1992
)
3.17

Actions

ExcerptReferenceRelevance
"Artemether could increase both DTH reaction and the production of hemagglutinating antibody in normal mice. "( Antitumor and immunomodulatory properties of artemether and its ability to reduce CD4+ CD25+ FoxP3+ T reg cells in vivo.
Farsam, V; Hassan, ZM; Mahdavi, M; Noori, S; Ranjbar, M; Zavaran-Hosseini, A, 2011
)
2.07

Treatment

Artemether treatment markedly aggravated anemia within 24 h. Artemether-treated mice showed lower FBG and HbA1c and reduced urinary albumin excretion.

ExcerptReferenceRelevance
"Artemether-treated mice showed lower FBG and HbA1c and reduced urinary albumin excretion, as well as urinary NAG."( Artemether Alleviates Diabetic Kidney Disease by Modulating Amino Acid Metabolism.
Cai, Y; Chen, Y; Ge, N; Gu, X; Han, P; Huang, J; Rong, G; Shao, M; Sun, H; Weng, W; Wu, X; Yu, X; Yuan, R, 2022
)
2.89
"Artemether treatment markedly aggravated anemia within 24 h."( Whole blood transfusion improves vascular integrity and increases survival in artemether-treated experimental cerebral malaria.
Ackerman, HC; Carvalho, LJM; Conceição, FG; Daniel-Ribeiro, CT; Gul, S; Moreira, AS; Ribeiro-Gomes, FL; Sanches, GS, 2021
)
1.57
"Artemether treatment resulted in total and female worm burden reductions ranging between 71.1% and 85.3%, whereas mefloquine achieved total and female worm burden reductions of 80.4-97.8%."( Activity of artemether and mefloquine against juvenile and adult Schistosoma mansoni in athymic and immunocompetent NMRI mice.
Doenhoff, MJ; Keiser, J; Vargas, M, 2010
)
1.46
"The artemether treatment (5 d intramuscular regimen) was effective and the drug was well tolerated."( The efficacy of artemether in the treatment of Plasmodium falciparum malaria in Sudan.
Abedelrahim, AM; Ali, AE; Elhassan, IM; Elkhalifa, AA; Fadul, I; Ming, C; Satti, GH; Theander, TG,
)
0.96
"artemether treatment: 3.2 mg kg-1 on day 0 and 0.8 mg kg-1 on days 1-4 (treatment R)."( Dose-finding and efficacy study for i.m. artemotil (beta-arteether) and comparison with i.m. artemether in acute uncomplicated P. falciparum malaria.
Krudsood, S; Looareesuwan, S; Lugt, ChB; Oosterhuis, B; Peeters, PA; Peggins, JO; Schilizzi, BM; Sollie, FA; Wilairatana, P, 2002
)
1.26
"Treatment with artemether was started when the parasite density exceeded 70,000/microL."( Laboratory evaluation of the ict malaria P.f./P.v. immunochromatographic test for detecting the panmalarial antigen using a rodent malaria model.
Arai, M; Ishii, A; Matsuoka, H, 2004
)
0.66
"Treatment with artemether resulted in decreased worm body size, expansion of the pharynx and dilation of the gut with marked reduction in pigment."( Effect of artemether on Schistosoma mansoni: dose-efficacy relationship, and changes in worm morphology and histopathology.
Chollet, J; Guo, J; Tanner, M; Utzinger, J; Wu, JT; Xiao, SH, 2004
)
1.07

Toxicity

Artemether-lumefantrine (AL) and dihydroart Artemisinin-piperaquine (DP) No major adverse events were recorded for either treatment group. Five patients on artemether had a transient spike of temperature after clearance of parasitaemia.

ExcerptReferenceRelevance
" No major adverse events were recorded for either treatment group although five patients on artemether had a transient spike of temperature after clearance of parasitaemia."( A comparative study of the schizontocidal efficacy and safety of artemether versus chloroquine in uncomplicated malaria.
Chandiwana, S; Mharakurwa, S; Mutetwa, S; Neill, P; Simooya, O; Stein, M, 1992
)
0.74
" There were no major adverse events with either drug."( Efficacy and safety of CGP 56697 (artemether and benflumetol) compared with chloroquine to treat acute falciparum malaria in Tanzanian children aged 1-5 years.
Abdulla, S; Beck, HP; Gathmann, I; Hatz, C; Kibatala, P; Mull, R; Royce, C; Schellenberg, D; Tanner, M, 1998
)
0.58
" Their toxicity may be due to an interaction of iron with the endoperoxide bridge of the derivative to produce toxic free radicals and/or other toxic metabolites."( The role of iron in neurotoxicity: a study of novel antimalarial drugs.
Edwards, G; Maggs, JL; McLean, WG; Park, BK; Smith, SL; Ward, SA,
)
0.13
" In this assay, dihydroartemisinin is significantly more toxic than artemether or arteether."( In vitro neurotoxicity of artemisinin derivatives.
McLean, WG; Ward, SA, 1998
)
0.54
" There was no difference in the incidence of possible adverse effects between the two drugs, and no evidence that either derivative caused allergic reactions, neurologic or psychiatric reactions, or cardiovascular or dermatologic toxicity."( Adverse effects in patients with acute falciparum malaria treated with artemisinin derivatives.
Chongsuphajaisiddhi, T; Kham, A; Luxemburger, C; McGready, R; Nosten, F; Phaipun, L; Price, R; Simpson, J; ter Kuile, F; van Vugt, M; White, NJ, 1999
)
0.3
" The most commonly reported and possibly related adverse effects following A-L therapy involved the gastro-intestinal (abdominal pain, anorexia, nausea, vomiting, diarrhoea) and central nervous (headache, dizziness) systems."( An integrated assessment of the clinical safety of artemether-lumefantrine: a new oral fixed-dose combination antimalarial drug.
Alteri, E; Bakshi, R; Gathmann, I; Hermeling-Fritz, I,
)
0.38
" Dihydroartemisinin (DQHS), a more toxic and active metabolite of AE, was also analyzed."( Neurotoxicity and efficacy of arteether related to its exposure times and exposure levels in rodents.
Gettayacamin, M; Kyle, DE; Li, QG; Milhous, WK; Mog, SR; Si, YZ, 2002
)
0.31
"Proportion of treatment success and adverse drug effects that required discontinuation of treatment and/or follow-up."( Safety and efficacy of artemether-lumefantrine in the treatment of uncomplicated falciparum malaria in Ethiopia.
Argaw, D; Babaniyi, O; Jima, D; Kebede, A; Medhin, A; Tesfaye, G, 2005
)
0.64
"8) and no adverse effects or complaints related to the drug that required discontinuation of treatment or withdrawal from follow-up was reported."( Safety and efficacy of artemether-lumefantrine in the treatment of uncomplicated falciparum malaria in Ethiopia.
Argaw, D; Babaniyi, O; Jima, D; Kebede, A; Medhin, A; Tesfaye, G, 2005
)
0.64
"1%) clinical and parasitological cure for the treatment of uncomplicated falciparum malaria with no reports of adverse reaction that required withdrawal of treatment or discontinuation of follow-up."( Safety and efficacy of artemether-lumefantrine in the treatment of uncomplicated falciparum malaria in Ethiopia.
Argaw, D; Babaniyi, O; Jima, D; Kebede, A; Medhin, A; Tesfaye, G, 2005
)
0.64
" The main finding of this analysis is that the six-dose regimen of coartemether is safe and more efficacious than the four-dose regimen in children."( Efficacy and safety of the six-dose regimen of artemether-lumefantrine in pediatrics with uncomplicated Plasmodium falciparum malaria: a pooled analysis of individual patient data.
Andriano, K; De Palacios, PI; Falade, C; Hunt, P; Karbwang, J; Makanga, M; Mueller, EA; Premji, Z, 2006
)
0.83
" Artemether was administered orally or intramuscularly; sheep were monitored for 8 h posttreatment and then once daily for adverse events, and drug efficacy was estimated by fecal egg count reductions and worm burden reductions."( Efficacy and safety of artemether against a natural Fasciola hepatica infection in sheep.
Cringoli, G; Keiser, J; Mezzino, L; Rinaldi, L; Tanner, M; Utzinger, J; Veneziano, V, 2008
)
1.57
" Participants were actively monitored for adverse events for 28 days and then passively for up to 63 days after treatment."( Safety and tolerability of artemether-lumefantrine versus dihydroartemisinin-piperaquine for malaria in young HIV-infected and uninfected children.
Arinaitwe, E; Bigira, V; Dorsey, G; Gasasira, A; Homsy, J; Kakuru, A; Kamya, MR; Katrak, S; Sandison, TG; Tappero, JW; Wanzira, H, 2009
)
0.65
" Most adverse events were rare, with only cough, diarrhoea, vomiting, and anaemia occurring in more than 1% of treatments."( Safety and tolerability of artemether-lumefantrine versus dihydroartemisinin-piperaquine for malaria in young HIV-infected and uninfected children.
Arinaitwe, E; Bigira, V; Dorsey, G; Gasasira, A; Homsy, J; Kakuru, A; Kamya, MR; Katrak, S; Sandison, TG; Tappero, JW; Wanzira, H, 2009
)
0.65
"Both AL and DP were safe and well tolerated for the treatment of uncomplicated malaria in young HIV-infected and uninfected children."( Safety and tolerability of artemether-lumefantrine versus dihydroartemisinin-piperaquine for malaria in young HIV-infected and uninfected children.
Arinaitwe, E; Bigira, V; Dorsey, G; Gasasira, A; Homsy, J; Kakuru, A; Kamya, MR; Katrak, S; Sandison, TG; Tappero, JW; Wanzira, H, 2009
)
0.65
" Large clinical studies and meta-analyses did not show serious side effects, although proper monitoring of adverse effects in developing countries might not be a trivial task."( Toxicity of the antimalarial artemisinin and its dervatives.
Efferth, T; Kaina, B, 2010
)
0.36
"0%) adverse events in 849 patients assigned to pyronaridine-artesunate and 241 (57."( Efficacy and safety of a fixed-dose oral combination of pyronaridine-artesunate compared with artemether-lumefantrine in children and adults with uncomplicated Plasmodium falciparum malaria: a randomised non-inferiority trial.
Bedu-Addo, G; Bhatt, KM; Borghini-Fuhrer, I; Bustos, DG; Duparc, S; Fleckenstein, L; Gaye, O; Kayentao, K; Sesay, SS; Shin, CS; Thompson, R; Tjitra, E; Tshefu, AK, 2010
)
0.58
"5 mg/kg for 7-28 days, indicating that the safe dosing duration in monkeys should be longer than 7 days under the exposure."( Toxicokinetic and toxicodynamic (TK/TD) evaluation to determine and predict the neurotoxicity of artemisinins.
Hickman, M; Li, Q, 2011
)
0.37
" The primary end point was parasitological cure on day 28 while the secondary end points included: improvement in haemoglobin levels and occurrence, and severity of adverse events."( Therapeutic efficacy and safety of artemether-lumefantrine for the treatment of uncomplicated falciparum malaria in North-Eastern Tanzania.
Buza, J; Ishengoma, DS; Lemnge, MM; Mandara, CI; Shahada, F; Shayo, A, 2014
)
0.68
" Reported adverse events included cough (49."( Therapeutic efficacy and safety of artemether-lumefantrine for the treatment of uncomplicated falciparum malaria in North-Eastern Tanzania.
Buza, J; Ishengoma, DS; Lemnge, MM; Mandara, CI; Shahada, F; Shayo, A, 2014
)
0.68
" Adverse events though common were similar between treatment arms and mostly related to the disease."( Efficacy and safety of fixed-dose artesunate-amodiaquine vs. artemether-lumefantrine for repeated treatment of uncomplicated malaria in Ugandan children.
Afizi, K; Fredrick, M; Kamya, MR; Lameyre, V; Lukwago, R; Talisuna, AO; Yeka, A, 2014
)
0.64
"Plasmodium falciparum sporozite (PfSPZ) Vaccine is a metabolically active, non-replicating, whole malaria sporozoite vaccine that has been reported to be safe and protective against P falciparum controlled human malaria infection in malaria-naive individuals."( Safety and efficacy of PfSPZ Vaccine against Plasmodium falciparum via direct venous inoculation in healthy malaria-exposed adults in Mali: a randomised, double-blind phase 1 trial.
Abebe, Y; Billingsley, PF; Chakravarty, S; Diallo, H; Ding, K; Dolo, A; Doumbo, O; Duffy, PE; Fay, MP; Gabriel, EE; Guindo, MA; Gunasekera, A; Healy, SA; Hoffman, SL; James, ER; Kamate, B; Katile, A; Li, M; Manoj, A; Murshedkar, T; Niangaly, A; Niaré, K; Nutman, TB; O'Connell, EM; Omaswa, F; Richie, TL; Ruben, AJ; Samake, Y; Sim, BKL; Sissoko, K; Sissoko, MS; Thera, I; Walther, M; Wong-Madden, S; Zaidi, I; Zeguime, A, 2017
)
0.46
" We detected no significant differences in local or systemic adverse events or laboratory abnormalities between the PfSPZ Vaccine and placebo groups, and only grade 1 (mild) local or systemic adverse events occurred in both groups."( Safety and efficacy of PfSPZ Vaccine against Plasmodium falciparum via direct venous inoculation in healthy malaria-exposed adults in Mali: a randomised, double-blind phase 1 trial.
Abebe, Y; Billingsley, PF; Chakravarty, S; Diallo, H; Ding, K; Dolo, A; Doumbo, O; Duffy, PE; Fay, MP; Gabriel, EE; Guindo, MA; Gunasekera, A; Healy, SA; Hoffman, SL; James, ER; Kamate, B; Katile, A; Li, M; Manoj, A; Murshedkar, T; Niangaly, A; Niaré, K; Nutman, TB; O'Connell, EM; Omaswa, F; Richie, TL; Ruben, AJ; Samake, Y; Sim, BKL; Sissoko, K; Sissoko, MS; Thera, I; Walther, M; Wong-Madden, S; Zaidi, I; Zeguime, A, 2017
)
0.46
"0%) patients experienced at least one drug-related adverse event (AE)."( Safety and tolerability of artesunate-amodiaquine, artemether-lumefantrine and quinine plus clindamycin in the treatment of uncomplicated Plasmodium falciparum malaria in Kinshasa, the Democratic Republic of the Congo.
Fungula, B; Inocencio da Luz, R; Kalabuanga, M; Lula Ntamba, Y; Lutumba, P; Muhindo Mavoko, H; Ntamabyaliro Nsengi, PM; Tona Lutete, G; Van Geertruyden, JP, 2019
)
0.77
" Reactive focal mass drug administration (rfMDA) may be safe and more effective."( Effectiveness and safety of reactive focal mass drug administration (rfMDA) using dihydroartemisinin-piperaquine to reduce malaria transmission in the very low-endemic setting of Eswatini: a pragmatic cluster randomised controlled trial.
Baltzell, K; Benjamin-Chung, J; Bhangu, K; Dlamini, B; Dlamini, N; Dufour, MK; Gosling, R; Greenhouse, B; Helb, D; Hsiang, MS; Kalungero, M; Kunene, S; Malambe, C; Maphalala, G; Mngadi, N; Nhlabathi, N; Ntshalintshali, N; Pindolia, D; Prach, LM; Tesfa, G; Vilakati, S; Whittemore, B, 2021
)
0.62
" No serious adverse events occurred."( Effectiveness and safety of reactive focal mass drug administration (rfMDA) using dihydroartemisinin-piperaquine to reduce malaria transmission in the very low-endemic setting of Eswatini: a pragmatic cluster randomised controlled trial.
Baltzell, K; Benjamin-Chung, J; Bhangu, K; Dlamini, B; Dlamini, N; Dufour, MK; Gosling, R; Greenhouse, B; Helb, D; Hsiang, MS; Kalungero, M; Kunene, S; Malambe, C; Maphalala, G; Mngadi, N; Nhlabathi, N; Ntshalintshali, N; Pindolia, D; Prach, LM; Tesfa, G; Vilakati, S; Whittemore, B, 2021
)
0.62
"In drug trials, clinical adverse events (AEs), concomitant medication and laboratory safety outcomes are repeatedly collected to support drug safety evidence."( Joint modelling of multivariate longitudinal clinical laboratory safety outcomes, concomitant medication and clinical adverse events: application to artemisinin-based treatment during pregnancy clinical trial.
Chapotera, G; Chirwa, T; D'Alessandro, U; Kazembe, L; Laufer, MK; Mathanga, D; Mukaka, M; Mwapasa, V; Patson, N, 2021
)
0.62
" Safety was based on assessment of adverse events (AEs) and severe adverse events (SAEs) from day 1 to day 28."( Effectiveness and safety of artesunate-amodiaquine versus artemether-lumefantrine for home-based treatment of uncomplicated Plasmodium falciparum malaria among children 6-120 months in Yaoundé, Cameroon: a randomized trial.
Aboh, PM; Adzemye, LM; Akam, LF; Ali, IM; Alifrangis, M; Ambani, MCE; Ango, Z; Bigoga, JD; Chedjou, JPK; Dinza, G; Dongmo, CH; Douanla, A; Ewane, MS; Fomboh, CT; Fosah, DA; Kotcholi, GB; Ludovic, AJ; Mbacham, WF; Moyeh, MN; Nana, WD; Ndikum, VN; Ngu, JA; Niba, PTN; Nji, AM; Nna, DRA; Oben, OLA; Omgba, PAM; Selly-Ngaloumo, AA; Tatah, FM; Ticha, JT, 2022
)
0.97
" Expected mild to moderate adverse events were reported in both arms [AS-AQ = 83 (84."( Effectiveness and safety of artesunate-amodiaquine versus artemether-lumefantrine for home-based treatment of uncomplicated Plasmodium falciparum malaria among children 6-120 months in Yaoundé, Cameroon: a randomized trial.
Aboh, PM; Adzemye, LM; Akam, LF; Ali, IM; Alifrangis, M; Ambani, MCE; Ango, Z; Bigoga, JD; Chedjou, JPK; Dinza, G; Dongmo, CH; Douanla, A; Ewane, MS; Fomboh, CT; Fosah, DA; Kotcholi, GB; Ludovic, AJ; Mbacham, WF; Moyeh, MN; Nana, WD; Ndikum, VN; Ngu, JA; Niba, PTN; Nji, AM; Nna, DRA; Oben, OLA; Omgba, PAM; Selly-Ngaloumo, AA; Tatah, FM; Ticha, JT, 2022
)
0.97
"This study demonstrated that AS-AQ and AL are effective and safe for home management of malaria in Yaoundé."( Effectiveness and safety of artesunate-amodiaquine versus artemether-lumefantrine for home-based treatment of uncomplicated Plasmodium falciparum malaria among children 6-120 months in Yaoundé, Cameroon: a randomized trial.
Aboh, PM; Adzemye, LM; Akam, LF; Ali, IM; Alifrangis, M; Ambani, MCE; Ango, Z; Bigoga, JD; Chedjou, JPK; Dinza, G; Dongmo, CH; Douanla, A; Ewane, MS; Fomboh, CT; Fosah, DA; Kotcholi, GB; Ludovic, AJ; Mbacham, WF; Moyeh, MN; Nana, WD; Ndikum, VN; Ngu, JA; Niba, PTN; Nji, AM; Nna, DRA; Oben, OLA; Omgba, PAM; Selly-Ngaloumo, AA; Tatah, FM; Ticha, JT, 2022
)
0.97
"25 mg/kg single-dose primaquine is safe and sufficient to reduce transmission of gametocytes in individuals with no, reduced, or increased CYP2D6 enzyme activity."( A single low dose of primaquine is safe and sufficient to reduce transmission of Plasmodium falciparum gametocytes regardless of cytochrome P450 2D6 enzyme activity in Bagamoyo district, Tanzania.
Kweka, E; Mårtensson, A; Mmbando, BP; Msolo, D; Mwaiswelo, RO; Ngasala, B, 2022
)
0.72
" Separate network meta-analyses in the frequentist framework, using a random effects model, with quinine as reference, were conducted for adults and children, and rankings were produced using p-scores to assess mortality, parasite clearance, coma recovery, fever clearance, neurological sequela and adverse events."( Comparative efficacy and safety of the artemisinin derivatives compared to quinine for treating severe malaria in children and adults: A systematic update of literature and network meta-analysis.
Amoh, G; Amuzu, DSY; Andoh, NE; Ansong, M; Hirst, J; Nyaaba, N; Ordóñez-Mena, JM, 2022
)
0.72
" The intervention was generally well tolerated, with two grade 3 adverse events of neutropenia, and no serious adverse events."( Safety, Tolerability, and Parasite Clearance Kinetics in Controlled Human Malaria Infection after Direct Venous Inoculation of Plasmodium falciparum Sporozoites: A Model for Evaluating New Blood-Stage Antimalarial Drugs.
Barnes, KI; Berghmans, PJ; Chalon, S; Chughlay, MF; El Gaaloul, M; Escoffier, E; Flynn, J; Gobeau, N; Izquierdo-Juncàs, D; Jansen, B; Kümmel, A; Marx, MW; Mitov, V; Möhrle, JJ; Rosanas-Urgell, A; Van Geertruyden, JP; Van Leuven, K, 2022
)
0.72
" Besides, no adverse events occurred in both groups."( Evaluation of the efficacy and safety of artemether emulsion on localized senile pruritus: A randomized pilot study.
Fei, JB; He, HQ; Pei, Q; Qin, HH; Shen, WT; Wang, GJ; Yu, Y, 2022
)
0.99
" No serious adverse events were reported during the 28 days follow-up."( Safety and therapeutic efficacy of artemether-lumefantrine in the treatment of uncomplicated Plasmodium falciparum malaria at Shecha health centre, Arba Minch, Ethiopia.
Abay, SM; Assefa, A; Assefa, G; Bekele, W; Gidey, B; Gubae, K; Haile, M; Hailgiorgis, H; Mare, AK; Mohammed, H; Sime, H; Tasew, G, 2023
)
1.19
" Adverse events in both treatment arms were mild and similar to the symptoms of malaria infection."( Efficacy and safety of pyronaridine-artesunate versus artemether-lumefantrine in the treatment of acute uncomplicated malaria in children in South-West Nigeria: an open-labelled randomized controlled trial.
Adedapo, AD; Anjorin, OE; Falade, CO; Funwei, RI; Michael, OS; Mokuolu, OA; Olusanya, AL; Olusola, FI; Orimadegun, AE; Orimadegun, BE, 2023
)
1.16
" Artemisinin-based combination treatments are generally well tolerated, safe and effective; the most used being artemether-lumefantrine (AL) and dihydroartemisinin-piperaquine (DP)."( Efficacy and safety of pyronaridine-artesunate (PYRAMAX) for the treatment of
D'Alessandro, U; Dabira, ED; Diakite, H; Djimde, M; Dorlo, TP; Erhart, A; González, R; Kabore, B; Kayentao, K; Keita, M; Macuacua, S; Menendez, C; Mens, P; Muhindo, HM; Piqueras, M; Sagara, I; Schallig, H; Sevene, E; Tinto, H; Traore, M; Tshiongo, JK; Vala, A, 2023
)
1.12

Pharmacokinetics

There are sparse published data relating to the pharmacokinetic properties of artemether, lumefantrine, an antimalarial described as a substrate (and possible inhibitor) of CYP3A4. This article describes the clinically observedArtemether exposure data in pediatric populations across various age groups and body weights.

ExcerptReferenceRelevance
" In theory, short half-life compounds reduce the selective pressure for resistance, which may be a major determinant of the useful therapeutic life of an antimalarial drug."( Pharmacology and pharmacokinetics of new antimalarials.
Watkins, WM, 1995
)
0.29
" Tmax was also delayed with the combination regimen [14 (5-24) vs 6 (4-16) h]."( Pharmacokinetics of mefloquine, when given alone and in combination with artemether, in patients with uncomplicated falciparum malaria.
Banmairuroi, V; Karbwang, J; Molunto, P; Na-Bangchang, K; Thanavibul, A, 1995
)
0.52
"The relatively short half-life of ARM may be one of the factors responsible for the poor radical cure rate of falciparum malaria with regimens employing daily dosing."( Single dose pharmacokinetics of oral artemether in healthy Malaysian volunteers.
Mansor, SM; Mordi, MN; Navaratnam, V; Wernsdorfer, WH, 1997
)
0.57
" The resulting pharmacokinetic parameter estimates were substantially different not only between drugs but also between routes of administration for the same drug."( The pharmacokinetics and bioavailability of dihydroartemisinin, arteether, artemether, artesunic acid and artelinic acid in rats.
Brewer, TG; Fleckenstein, LL; Heiffer, MH; Li, QG; Masonic, K; Peggins, JO, 1998
)
0.53
" Patients with ARF had significantly higher Cmax [2."( Pharmacokinetics of intramuscular artemether in patients with severe falciparum malaria with or without acute renal failure.
Harinasuta, T; Karbwang, J; Na-Bangchang, K; Rimchala, W; Sukontason, K; Tin, T, 1998
)
0.58
" Elimination of pyrimethamine was however, a relatively slow process compared with artemether, and thus resulted in a long terminal phase elimination half-life (50-106 hours)."( Pharmacokinetic interactions of artemether and pyrimethamine in healthy male Thais.
Karbwang, J; Na-Bangchang, K; Tan-ariya, P; Thanavibul, A; Thipawangkosol, P; Ubalee, R, 1998
)
0.81
"To investigate the pharmacokinetic and pharmacodynamic properties of artemether and benflumetol in a fixed combination tablet (CGP 56697) and to offer an explanation for the lower than expected cure rate in a Thai clinical trial."( Population pharmacokinetics and therapeutic response of CGP 56697 (artemether + benflumetol) in malaria patients.
Ezzet, F; Karbwang, J; Mull, R, 1998
)
0.77
" Parasite clearance time and 28 day cure rate were correlated with the derived pharmacokinetic parameters."( Population pharmacokinetics and therapeutic response of CGP 56697 (artemether + benflumetol) in malaria patients.
Ezzet, F; Karbwang, J; Mull, R, 1998
)
0.54
"Using a population-based approach it was confirmed that the pharmacokinetic and pharmacodynamic properties of benflumetol and artemether differ markedly."( Population pharmacokinetics and therapeutic response of CGP 56697 (artemether + benflumetol) in malaria patients.
Ezzet, F; Karbwang, J; Mull, R, 1998
)
0.74
" The pharmacokinetics of benflumetol were highly variable, with coefficients of variation in pharmacokinetic parameters ranging from 14."( Pharmacokinetics of benflumetol given as a fixed combination artemether-benflumetol (CGP 56697) in Thai patients with uncomplicated falciparum malaria.
Farkad, E; Karbwang, J; Mull, R; Na-Bangchang, K; Tasanor, U; Thanavibul, A, 1999
)
0.54
"The objective of this study was to conduct a prospective population pharmacokinetic and pharmacodynamic evaluation of lumefantrine during blinded comparisons of artemether-lumefantrine treatment regimens in uncomplicated multidrug-resistant falciparum malaria."( Pharmacokinetics and pharmacodynamics of lumefantrine (benflumetol) in acute falciparum malaria.
Ezzet, F; Looareesuwan, S; Nosten, F; van Vugt, M; White, NJ, 2000
)
0.5
"Forty-two healthy subjects were randomized in a parallel three-group design trial to investigate potential electrocardiographic and pharmacokinetic interactions between the new antimalarial co-artemether, a combination of artemether and lumefantrine (both of which are predominantly metabolized through CYP3A4), and mefloquine, another antimalarial described as a substrate (and possible inhibitor) of CYP3A4."( Pharmacokinetic interaction trial between co-artemether and mefloquine.
Bindschedler, M; Ezzet, F; Lefèvre, G; Meyer, I; Schaeffer, N; Thomsen, MS, 2000
)
0.76
"The study was carried out to investigate the pharmacokinetic and pharmacodynamic interactions between artemether (ARTEM) and quinoline antimalarials namely mefloquine (MQ), quinine (QN) and primaquine (PQ) when given concurrently."( Absence of significant pharmacokinetic and pharmacodynamic interactions between artemether and quinoline antimalarials.
Karbwang, J; Na-Bangchang, K; Saenglertsilapachai, S; Thanavibul, A; Ubalee, R,
)
0.57
" The pharmacokinetic curves of artemether and its metabolites dihydroartemisinin and furano acetate of artemether were determined and the results showed that the half-life of artemether under the conditions simulated the pH of plasma or small intestine was more than 150 min and that of stomach acid was 74."( [Pharmacokinetic studies on artemether under conditions simulated in vivo].
Chen, YG; Yu, BY, 2002
)
0.89
"4 (range 5-108) months were recruited into the study and data from 90 of these children (30 with respiratory distress and 60 with no respiratory distress) were used in the population pharmacokinetic analysis."( Population pharmacokinetics of artemether and dihydroartemisinin following single intramuscular dosing of artemether in African children with severe falciparum malaria.
Aarons, L; Edwards, G; Kokwaro, GO; Majid, O; Marsh, K; Mithwani, S; Mohamed, S; Muchohi, S; Watkins, W, 2004
)
0.61
"The first-dose pharmacokinetic properties of intramuscular (i."( Comparative pharmacokinetics of intramuscular artesunate and artemether in patients with severe falciparum malaria.
Agus, C; Chiswell, GM; Chuong, LV; Davis, TM; Farrar, J; Hien, TT; Ilett, KF; Phu, NH; Sinh, DX; White, NJ, 2004
)
0.56
" Since beta-arthemeter is now available, an open-label pharmacodynamic analysis was performed in 73 adults with uncomplicated Plasmodium falciparum malaria."( Pharmacodynamic analysis of antimalarials used in Plasmodium falciparum imported malaria in northern Italy.
Calleri, G; Canta, F; Caramello, P; Cavecchia, I; Di Perri, G; Gobbi, F; Lipani, F; Sergi, G,
)
0.13
" According to the pharmacodynamic parameters measured, no significant differences were recorded among patients with or without prior exposure to malaria."( Pharmacodynamic analysis of antimalarials used in Plasmodium falciparum imported malaria in northern Italy.
Calleri, G; Canta, F; Caramello, P; Cavecchia, I; Di Perri, G; Gobbi, F; Lipani, F; Sergi, G,
)
0.13
" Plasma carbamazepine levels were assayed by high-performance liquid chromatography and pharmacokinetic parameters calculated."( Effects of artemisinin, artemether, arteether on the pharmacokinetics of carbamazepine.
Medhi, B; Pandhi, P; Sukhija, M, 2006
)
0.64
" Plasma phenytoin levels were assayed by HPLC, and pharmacokinetic parameters were calculated."( Effects of artemisinin, artemether, and arteether on the pharmacokinetics of phenytoin.
Medhi, B; Pandhi, P; Sukhija, M, 2006
)
0.64
"A six-dose antimalarial regimen of artemether-lumefantrine (A/L) may soon become one of the most widely used drug combination in Africa, despite possible constraints with adherence and poor absorption due to inadequate nutrition, and a lack of pharmacokinetic and effectiveness data."( Supervised versus unsupervised antimalarial treatment with six-dose artemether-lumefantrine: pharmacokinetic and dosage-related findings from a clinical trial in Uganda.
Babigumira, J; Bajunirwe, F; Biraro, S; Checchi, F; Ferradini, L; Fogg, C; Grandesso, F; Guthmann, JP; Kigozi, I; Kiguli, J; Kyomuhendo, J; Piola, P; Ruzagira, E; Taylor, WR, 2006
)
0.85
"To determine the pharmacokinetic properties of artemether and lumefantrine (AL) in pregnant women with recrudescent uncomplicated multi-drug resistant falciparum malaria."( The pharmacokinetics of artemether and lumefantrine in pregnant women with uncomplicated falciparum malaria.
Ashley, EA; La, Y; Lindegardh, N; McGready, R; Nosten, F; Singhasivanon, P; Stepniewska, K; White, NJ, 2006
)
0.9
" Serial blood samples were taken over a 7-day period, and pharmacokinetic parameters were estimated."( The pharmacokinetics of artemether and lumefantrine in pregnant women with uncomplicated falciparum malaria.
Ashley, EA; La, Y; Lindegardh, N; McGready, R; Nosten, F; Singhasivanon, P; Stepniewska, K; White, NJ, 2006
)
0.64
"To establish a HPLC-MS-MS determination method of artemether (ARM) and active derivatives DHA, and compare the pharmacokinetic parameters of ARM after transdermal and oral administration."( [Studies on pharmacokinetics of artemether patch in mice].
He, C; Li, JS; Liang, BW; Wang, NJ; Yang, HS; Ye, ZG, 2008
)
0.88
" For artemether, trends toward Cmax and AUC decreases (Cmax 14."( Lopinavir/ritonavir affects pharmacokinetic exposure of artemether/lumefantrine in HIV-uninfected healthy volunteers.
Aweeka, FT; Charlebois, E; Dorsey, G; German, P; Hanpithakpong, W; Havlir, D; Lawrence, J; Lindegardh, N; Parikh, S; Rosenthal, PJ, 2009
)
1.11
" The objective of this study was to determine the population pharmacokinetic properties of lumefantrine in pregnant women with uncomplicated multidrug-resistant Plasmodium falciparum malaria on the northwestern border of Thailand."( Population pharmacokinetics of lumefantrine in pregnant women treated with artemether-lumefantrine for uncomplicated Plasmodium falciparum malaria.
Annerberg, A; Ashley, EA; Day, NP; Kamanikom, B; Lindegardh, N; McGready, R; Nosten, F; Pimanpanarak, M; Singhasivanon, P; Stepniewska, K; Tarning, J; White, NJ, 2009
)
0.58
" Pharmacokinetic (PK) data informing the optimum dosing of these drug regimens is limited, especially in children."( Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
Annerberg, A; Aweeka, F; Clark, TD; Dorsey, G; Drysdale, T; German, P; Kalyango, JN; Kamya, MR; Lindegardh, N; McGee, B; Mwesigwa, J; Parikh, S; Rosenthal, PJ, 2010
)
0.68
" The validated method was successfully applied to determine the plasma concentrations of artemether and lumefantrine in healthy volunteers, in a one-dose pharmacokinetic study, over the course of 11 days."( Liquid chromatography-tandem mass spectrometry for the simultaneous quantitation of artemether and lumefantrine in human plasma: application for a pharmacokinetic study.
Bellorio, KB; César, IC; Chellini, PR; de Abreu, FC; Moreira, JM; Pianetti, GA; Ribeiro, JA; Teixeira, Lde S, 2011
)
0.82
"The overall pharmacokinetic properties of artemether and dihydroartemisinin in healthy Pakistani subjects are comparable to healthy subjects and patients from other populations."( Pharmacokinetics of artemether and dihydroartemisinin in healthy Pakistani male volunteers treated with artemether-lumefantrine.
Ali, S; Lindegardh, N; Najmi, MH; Tarning, J, 2010
)
0.95
"The pharmacokinetic and pharmacodynamic properties of a new pediatric formulation of artemether-lumefantrine, dispersible tablet, were determined within the context of a multicenter, randomized, parallel-group study."( Pharmacokinetic and pharmacodynamic characteristics of a new pediatric formulation of artemether-lumefantrine in African children with uncomplicated Plasmodium falciparum malaria.
Abdulla, S; Bassat, Q; Borrmann, S; Djimdé, AA; Lefèvre, G; Lyimo, J; Mandomando, I; Tekete, M, 2011
)
0.82
"There are sparse published data relating to the pharmacokinetic properties of artemether, lumefantrine, and their active metabolites in children, especially desbutyl-lumefantrine."( Population pharmacokinetics of artemether, lumefantrine, and their respective metabolites in Papua New Guinean children with uncomplicated malaria.
Davis, TM; Griffin, S; Ilett, KF; Kose, K; Mueller, I; Page-Sharp, M; Salman, S; Siba, PM, 2011
)
0.88
"The pharmacokinetic (PK) parameters of artesunate, artemether and their metabolites dihydroartemisinin (DHA) and dihydroartemisinin-glucuronide (DHA-glucuronide) were determined in sheep naturally infected with Fasciola hepatica."( Evaluation of the pharmacokinetic profile of artesunate, artemether and their metabolites in sheep naturally infected with Fasciola hepatica.
Cringoli, G; Duthaler, U; Huwyler, J; Keiser, J; Rinaldi, L, 2012
)
0.88
" Pregnancy has been reported to alter the pharmacokinetic properties of many anti-malarial drugs."( Population pharmacokinetics of Artemether and dihydroartemisinin in pregnant women with uncomplicated Plasmodium falciparum malaria in Uganda.
Day, NP; Dhorda, M; Guerin, PJ; Kloprogge, F; Lindegardh, N; Muwanga, S; Nosten, F; Nuengchamnong, N; Piola, P; Tarning, J; Turyakira, E; White, NJ, 2012
)
0.66
" A simultaneous drug-metabolite population pharmacokinetic model for artemether and dihydroartemisinin was developed taking into account different disposition, absorption, error and covariate models."( Population pharmacokinetics of Artemether and dihydroartemisinin in pregnant women with uncomplicated Plasmodium falciparum malaria in Uganda.
Day, NP; Dhorda, M; Guerin, PJ; Kloprogge, F; Lindegardh, N; Muwanga, S; Nosten, F; Nuengchamnong, N; Piola, P; Tarning, J; Turyakira, E; White, NJ, 2012
)
0.9
" The objective was to investigate pharmacokinetic interactions between darunavir/ritonavir or etravirine and arthemether/lumefrantrine."( Pharmacokinetic interaction between etravirine or darunavir/ritonavir and artemether/lumefantrine in healthy volunteers: a two-panel, two-way, two-period, randomized trial.
DeMasi, R; Kakuda, TN; Mohammed, P; van Delft, Y, 2013
)
0.62
"Pregnancy alters the pharmacokinetic properties of many drugs used in the treatment of malaria, usually resulting in lower drug exposures."( Pharmacokinetic properties of artemether, dihydroartemisinin, lumefantrine, and quinine in pregnant women with uncomplicated plasmodium falciparum malaria in Uganda.
Dhorda, M; Guerin, PJ; Jullien, V; Kloprogge, F; Nosten, F; Piola, P; Tarning, J; White, NJ, 2013
)
0.68
" Computed descriptors often used to predict absorption, distribution, metabolism, elimination and toxicity (ADMET) were used to assess the pharmacokinetic profiles of the isolated compounds."( New antimalarial hits from Dacryodes edulis (Burseraceae)--part I: isolation, in vitro activity, in silico "drug-likeness" and pharmacokinetic profiles.
Ngemenya, MN; Ntie-Kang, F; Tane, P; Tematio, EL; Tene, M; Titanji, VP; Zofou, D, 2013
)
0.39
" Plasma artemether and dihydroartemisinin (DHA) levels were measured using liquid chromatography-mass spectrometry, and the data were analyzed using established population compartmental pharmacokinetic models."( Pharmacokinetics of a novel sublingual spray formulation of the antimalarial drug artemether in African children with malaria.
Bendel, D; Davis, TM; Lee, TC; Salman, S; Templeton, D, 2015
)
1.08
" Population compartmental pharmacokinetic models were developed."( Pharmacokinetics of a novel sublingual spray formulation of the antimalarial drug artemether in healthy adults.
Bendel, D; Davis, TM; Lee, TC; Salman, S; Templeton, D, 2015
)
0.64
" The observation of a shorter terminal half-life for lumefantrine may have contributed to a higher frequency of reinfection or a shorter posttreatment prophylactic period in pregnant women than in nonpregnant adults."( Artemether-Lumefantrine Pharmacokinetics and Clinical Response Are Minimally Altered in Pregnant Ugandan Women Treated for Uncomplicated Falciparum Malaria.
Achan, J; Aweeka, F; Huang, L; Kajubi, R; Kiconco, S; Mwebaza, N; Mwima, MW; Nguyen, VK; Nyunt, MM; Parikh, S; Ssebuliba, J, 2015
)
1.86
" In vivo pharmacodynamic properties (parasite clearance time, parasite reduction ratio, dose and regimen determination) against multidrug resistant (MDR) rodent malaria parasite and toxicological parameters (median lethal dose, liver function test, kidney function test) were also investigated."( Pyrrolidine-Acridine hybrid in Artemisinin-based combination: a pharmacodynamic study.
Batra, S; Biswas, S; Chauhan, BS; Gunjan, S; Pandey, SK; Singh, S; Singh, SK; Srivastava, K; Tripathi, R, 2016
)
0.43
" This article describes the clinically observed artemether exposure data in pediatric populations across various age groups (1 month to 12 years) and body weights (<5 or ≥5 kg) using physiologically based pharmacokinetic (PBPK) mechanistic models."( A Physiologically Based Pharmacokinetic Model to Describe Artemether Pharmacokinetics in Adult and Pediatric Patients.
Awasthi, R; Hamed, K; He, H; Heimbach, T; Jain, JP; Lin, W; Sunkara, G, 2016
)
0.93
" Pharmacokinetic parameters (area under the plasma concentration vs."( Concomitant nevirapine impacts pharmacokinetic exposure to the antimalarial artemether-lumefantrine in African children.
Aweeka, FT; Barlow-Mosha, L; Carey, V; Gingrich, D; Graham, B; Huang, L; Kamthunzi, P; Lindsey, JC; Marzan, F; Nachman, S; Parikh, S; Ssemambo, PK, 2017
)
0.68
" Fifteen of the 16 (aged 4 to 11 years) on nevirapine-based ART were included in the pharmacokinetic analysis."( Concomitant nevirapine impacts pharmacokinetic exposure to the antimalarial artemether-lumefantrine in African children.
Aweeka, FT; Barlow-Mosha, L; Carey, V; Gingrich, D; Graham, B; Huang, L; Kamthunzi, P; Lindsey, JC; Marzan, F; Nachman, S; Parikh, S; Ssemambo, PK, 2017
)
0.68
" The pharmacokinetic differences among blood cells and plasma still remain unclear."( Comparison of in vitro/in vivo blood distribution and pharmacokinetics of artemisinin, artemether and dihydroartemisinin in rats.
Dai, R; Dai, T; Guo, Z; Jiang, W; Xie, Y, 2019
)
0.74
"We developed a population pharmacokinetic model of dolutegravir with data from 26 healthy volunteers in two Phase 2 studies with a total of 403 dolutegravir plasma concentrations at steady state."( Dolutegravir pharmacokinetics during co-administration with either artemether/lumefantrine or artesunate/amodiaquine.
Denti, P; Kawuma, AN; Khoo, S; Lamorde, M; Pillai, GC; Walimbwa, SI; Wasmann, RE, 2021
)
0.86
"The aim of this study was to assess the pharmacokinetic properties of artemether, lumefantrine and their active metabolites in Plasmodium knowlesi malaria."( The pharmacokinetic properties of artemether and lumefantrine in Malaysian patients with Plasmodium knowlesi malaria.
Davis, TME; Davis, WA; Hii, KC; Page-Sharp, M; Salman, S; Singh, B; Sugiarto, SR, 2022
)
1.23
" Multi-compartmental population pharmacokinetic models were developed using plasma with or without DBS drug concentrations."( The pharmacokinetic properties of artemether and lumefantrine in Malaysian patients with Plasmodium knowlesi malaria.
Davis, TME; Davis, WA; Hii, KC; Page-Sharp, M; Salman, S; Singh, B; Sugiarto, SR, 2022
)
1
" DBS lumefantrine concentrations can be used in pharmacokinetic studies but DBS technology is currently unreliable for the other analytes."( The pharmacokinetic properties of artemether and lumefantrine in Malaysian patients with Plasmodium knowlesi malaria.
Davis, TME; Davis, WA; Hii, KC; Page-Sharp, M; Salman, S; Singh, B; Sugiarto, SR, 2022
)
1
" The major limitations of the artemisinin combination therapy are erratic absorption from the injection site and high dosing frequency due to a very short elimination half-life of the drug."( Evaluation of Pharmacokinetics, Biodistribution, and Antimalarial Efficacy of Artemether-Loaded Polymeric Nanorods.
Bhide, AR; Dighe, VD; Jindal, AB; Jirwankar, YB; Katnoria, S; Kaur, S; Suri, M, 2023
)
1.14

Compound-Compound Interactions

Artemether combined with primaquine and single artemether showed good therapeutic effects in falciparum malaria cases. All the three compounds showed synergistic effects with Artemether, unlike slight antagonistic interactions of atranorin and 2β,3β,19α-trihydroxy-urs-12-en-28-oic acid in combination with quinine.

ExcerptReferenceRelevance
"To compare the therapeutic efficacy of oral artesunate and artemether in combination with mefloquine for the treatment of multidrug resistant malaria, a trial was conducted in 540 adults and children on the Thai-Myanmar border."( Artesunate versus artemether in combination with mefloquine for the treatment of multidrug-resistant falciparum malaria.
Brockman, A; Chongsuphajaisiddhi, T; Kham, A; Luxemburger, C; Nosten, F; Price, RN; White, NJ,
)
0.71
"To evaluate the efficacy and side effects of artemether combined with primaquine in the treatment of falciparum malaria."( [A study of artemether combined with primaquine in the treatment of falciparum malaria].
Elie, N; Gao, YQ; Huang, JR, 2001
)
0.95
" Sixty-one cases were treated with artemether combined with primaquine (Group A used artemether orally, Group B used artemether intramuscularly)."( [A study of artemether combined with primaquine in the treatment of falciparum malaria].
Elie, N; Gao, YQ; Huang, JR, 2001
)
0.97
"Artemether combined with primaquine and single artemether(via both routes) showed good therapeutic effects in falciparum malaria cases, while artemether combined with primaquine was more effective than single artemether in reducing relapes rate of malaria."( [A study of artemether combined with primaquine in the treatment of falciparum malaria].
Elie, N; Gao, YQ; Huang, JR, 2001
)
2.13
" Competitive uptake of radiolabeled chloroquine and dihydroartemisinin in combination with other antimalarials was observed."( Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
Adagu, IS; Fivelman, QL; Warhurst, DC, 2007
)
0.34
"The purpose of the study is to explore the efficacy of mefloquine administered orally at single, multiple doses, or in combination with artesuante, artemether, or praziquantel in mouse--Schistosoma japonicum model."( Effect of mefloquine administered orally at single, multiple, or combined with artemether, artesunate, or praziquantel in treatment of mice infected with Schistosoma japonicum.
Jiao, PY; Mei, JY; Xiao, SH, 2011
)
0.8
" All the three compounds showed synergistic effects with artemether, unlike the slight antagonistic interactions of atranorin and 2β,3β,19α-trihydroxy-urs-12-en-28-oic acid in combination with quinine."( Antimalarial drug interactions of compounds isolated from Kigelia africana (Bignoniaceae) and their synergism with artemether, against the multidrug-resistant W2mef Plasmodium falciparum strain.
Tane, P; Tene, M; Titanji, VP; Zofou, D, 2012
)
0.83
" This study also demonstrated the effectiveness of high-resolution mass spectrometry in combination with an online H/D exchange LC/HR-MS(n) technique in rapid identification of drug metabolites."( Metabolite identification of artemether by data-dependent accurate mass spectrometric analysis using an LTQ-Orbitrap hybrid mass spectrometer in combination with the online hydrogen/deuterium exchange technique.
Du, F; Liu, T; Xing, J; Zhu, F, 2011
)
0.66
"To investigate the association between vasculopathy and survival during experimental cerebral malaria (ECM), and to determine whether targeting the endothelin-1 (ET-1) pathway alone or in combination with the anti-malaria drug artemether (a semi-synthetic derivative of artemisinin) will improve microvascular hemorrhage and survival."( The novel ETA receptor antagonist HJP-272 prevents cerebral microvascular hemorrhage in cerebral malaria and synergistically improves survival in combination with an artemisinin derivative.
Bruno, FP; Dai, M; Desruisseaux, MS; Freeman, B; Reznik, SE; Shikani, HJ; Stephani, RA; Tanowitz, HB; Weiss, LM, 2012
)
0.56
" In this work, we investigated the role and mechanism of artemether combined with shRNA interference of VCAM-1 (shRNA-VCAM-1) on the migration, invasion and apoptosis of glioma cells."( Artemether combined with shRNA interference of vascular cell adhesion molecule-1 significantly inhibited the malignant biological behavior of human glioma cells.
Hu, Y; Li, Z; Liu, YH; Wang, P; Wang, YB; Xue, YX; Yao, YL; Yu, B, 2013
)
2.08
" We undertook two pharmacokinetic studies in healthy volunteers, using standard adult doses of artemether-lumefantrine or artesunate-amodiaquine given with 50 mg once daily dolutegravir (DTG) to investigate the drug-drug interaction between artemether-lumefantrine or artesunate-amodiaquine and dolutegravir."( Drug Interactions between Dolutegravir and Artemether-Lumefantrine or Artesunate-Amodiaquine.
Amara, A; Byakika-Kibwika, P; Chiong, J; Else, L; Gini, J; Kaboggoza, J; Khoo, SH; Lamorde, M; Tarning, J; Waitt, C; Walimbwa, SI; Winterberg, M, 2019
)
1
" The results highlighted the possibility of using (ω-3) PUFA combined with ART as a novel anti-schistosomal combination therapy."( Effect of omega-3 fatty acids administered as monotherapy or combined with artemether on experimental Schistosoma mansoni infection.
Abd El-Mageed, SA; Abdalla, HA; El-Beshbishi, SN; El-Nemr, HEE; Saleh, NE; Shebl, AM; Taman, A, 2019
)
0.74
" Although the clinical importance remains unclear to date, clinicians should be aware of potential drug-drug interactions and monitor patients on ACT closely."( Drug-Drug Interactions of Artemisinin-Based Combination Therapies in Malaria Treatment: A Narrative Review of the Literature.
Grundmann, O; Hernandez Maldonado, J, 2022
)
0.72

Bioavailability

Grapefruit juice significantly increases the oral bioavailability of artemether without an effect on the elimination half-life. The variability in bioavailability was large both between doses and between patients, but was less pronounced for benflumetol. The mean (95% CI) relative bioavailability compared with oral artem ether in the 6 h following administration AUC (0.01) was 0.02.

ExcerptReferenceRelevance
" The mean (95% CI) relative bioavailability compared with oral artemether in the 6 h following administration AUC (0."( Comparative bioavailability of oral, rectal, and intramuscular artemether in healthy subjects: use of simultaneous measurement by high performance liquid chromatography and bioassay.
Brewer, TG; Kyle, DE; Luxemburger, C; Nosten, F; Peggins, JO; Teja-Isavadharm, P; Ter Kuile, F; White, NJ, 1996
)
0.77
" We conclude that the bioavailability of intramuscular AM in children with severe malaria may be highly variable, particularly in the presence of respiratory distress, and may be associated with an inadequate therapeutic response."( The disposition of intramuscular artemether in children with cerebral malaria; a preliminary study.
Crawley, J; English, M; Lowe, B; Marsh, K; Mberu, E; Muhia, D; Murphy, SA; Newton, CR; Waruiru, C; Watkins, WM; Winstanley, P,
)
0.41
"The pharmacokinetics and bioavailability of artemether and dihydroartemisinin were investigated in eight Thai males following the administration of single oral and intramuscular doses of artemether (300 mg) in a randomized two-way cross-over study."( Pharmacokinetics and bioavailability of oral and intramuscular artemether.
Congpuong, K; Karbwang, J; Molunto, P; Na-Bangchang, K; Thanavibul, A, 1997
)
0.8
" Mean oral bioavailability relative to intramuscular administration was 43."( Pharmacokinetics and bioavailability of oral and intramuscular artemether.
Congpuong, K; Karbwang, J; Molunto, P; Na-Bangchang, K; Thanavibul, A, 1997
)
0.54
"The pharmacokinetics and bioavailability of dihydroartemisinin (DQHS), artemether (AM), arteether (AE), artesunic acid (AS) and artelinic acid (AL) have been investigated in rats after single intravenous, intramuscular and intragastric doses of 10 mg kg(-1)."( The pharmacokinetics and bioavailability of dihydroartemisinin, arteether, artemether, artesunic acid and artelinic acid in rats.
Brewer, TG; Fleckenstein, LL; Heiffer, MH; Li, QG; Masonic, K; Peggins, JO, 1998
)
0.76
" The variability in bioavailability of artemether and dihydroartemisinin was large both between doses and between patients, but was less pronounced for benflumetol."( Population pharmacokinetics and therapeutic response of CGP 56697 (artemether + benflumetol) in malaria patients.
Ezzet, F; Karbwang, J; Mull, R, 1998
)
0.81
"Grapefruit juice significantly increases the oral bioavailability of artemether without an effect on the elimination half-life."( Grapefruit juice increases the bioavailability of artemether.
Gupta, V; Rutten, JP; van Agtmael, MA; van Boxtel, CJ; van der Wösten, TH, 1999
)
0.79
" The aim of this study was to evaluate the effect of grapefruit juice on the decreasing bioavailability over time of artemether."( The effect of grapefruit juice on the time-dependent decline of artemether plasma levels in healthy subjects.
Gupta, V; van Agtmael, MA; van Boxtel, CJ; van der Graaf, CA, 1999
)
0.75
"Grapefruit juice significantly increased the oral bioavailability of artemether but did not prevent the time-dependent reduction in bioavailability."( The effect of grapefruit juice on the time-dependent decline of artemether plasma levels in healthy subjects.
Gupta, V; van Agtmael, MA; van Boxtel, CJ; van der Graaf, CA, 1999
)
0.78
" The aim of this study was to examine the relative oral antimalarial bioavailability and pharmacokinetics of the two derivatives."( A comparison of oral artesunate and artemether antimalarial bioactivities in acute falciparum malaria.
Angus, B; Keeratithakul, D; Newton, PN; Pukrittayakamee, S; Rasameesoraj, M; Suputtamongkol, Y; Teja-Isavadharm, P; White, NJ, 2001
)
0.59
" The mean (95% CI) oral antimalarial bioavailability of artemether, relative to oral artesunate, corrected for molar dose was 58 (40-76)%."( A comparison of oral artesunate and artemether antimalarial bioactivities in acute falciparum malaria.
Angus, B; Keeratithakul, D; Newton, PN; Pukrittayakamee, S; Rasameesoraj, M; Suputtamongkol, Y; Teja-Isavadharm, P; White, NJ, 2001
)
0.83
"The oral antimalarial bioavailability following artemether was significantly lower than that after artesunate."( A comparison of oral artesunate and artemether antimalarial bioactivities in acute falciparum malaria.
Angus, B; Keeratithakul, D; Newton, PN; Pukrittayakamee, S; Rasameesoraj, M; Suputtamongkol, Y; Teja-Isavadharm, P; White, NJ, 2001
)
0.84
"92 microg x h/ml) due to a higher bioavailability of AECM (74."( Neurotoxicity and efficacy of arteether related to its exposure times and exposure levels in rodents.
Gettayacamin, M; Kyle, DE; Li, QG; Milhous, WK; Mog, SR; Si, YZ, 2002
)
0.31
" Further pharmacokinetic studies showed that the bioavailability in rats following oral administration was 25 times greater for 11b than for artemether 1b."( Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin.
Bégué, JP; Bonnet-Delpon, D; Charman, WN; Charneau, S; Chorki, F; Crousse, B; Grellepois, F; Grellier, P; McIntosh, KA; Ourévitch, M; Pradines, B, 2004
)
0.53
" The combination of underdosing, poor-quality drug, and the intrinsic low bioavailability of artemether may have contributed to his poor clinical response."( Impaired clinical response in a patient with uncomplicated falciparum malaria who received poor-quality and underdosed intramuscular artemether.
Fernández, FM; Green, MD; Keoluangkhot, V; Mayxay, M; Newton, PN; Nyadong, L, 2008
)
0.77
"81-fold enhancement in apparent bioavailability compared to artemether."( Artemether/hydroxypropyl-beta-cyclodextrin host-guest system: characterization, phase-solubility and inclusion mode.
Chen, Y; Lin, J; Liu, Y; Yang, B, 2009
)
2.04
" Although artemether bioavailability was variable and its clearance increased by 67."( Population pharmacokinetics of artemether, lumefantrine, and their respective metabolites in Papua New Guinean children with uncomplicated malaria.
Davis, TM; Griffin, S; Ilett, KF; Kose, K; Mueller, I; Page-Sharp, M; Salman, S; Siba, PM, 2011
)
1.06
"The objective of this study was to compare different methods of adjusted indirect comparisons that can be used to investigate the relative bioavailability of different generic products."( Statistical approaches to indirectly compare bioequivalence between generics: a comparison of methodologies employing artemether/lumefantrine 20/120 mg tablets as prequalified by WHO.
García-Arieta, A; Gordon, J; Gwaza, L; Hansson, H; Potthast, H; Stahl, M; Welink, J, 2012
)
0.59
"Data from three bioequivalence studies conducted independently that compared three generics with the same reference product were used to indirectly determine the relative bioavailability between the generics themselves."( Statistical approaches to indirectly compare bioequivalence between generics: a comparison of methodologies employing artemether/lumefantrine 20/120 mg tablets as prequalified by WHO.
García-Arieta, A; Gordon, J; Gwaza, L; Hansson, H; Potthast, H; Stahl, M; Welink, J, 2012
)
0.59
"Existence of anti-malarial generic drugs with low bioavailability marketed on sub-Saharan Africa raises a concern on patients achieving therapeutic concentrations after intake of such products."( Comparison of bioavailability between the most available generic tablet formulation containing artemether and lumefantrine on the Tanzanian market and the innovator's product.
Abdulla, S; Chemba, M; Juma, O; Marealle, IA; Minzi, OM; Ngaimisi, E; Rutaihwa, M; Sasi, P; Shekalaghe, S, 2013
)
0.61
" The most widely available generic (Artefan®, Ajanta Pharma Ltd, Maharashtra, India) was sampled for bioavailability comparison with Coartem® (Novartis Pharma, Basel, Switzerland)--the innovator's product."( Comparison of bioavailability between the most available generic tablet formulation containing artemether and lumefantrine on the Tanzanian market and the innovator's product.
Abdulla, S; Chemba, M; Juma, O; Marealle, IA; Minzi, OM; Ngaimisi, E; Rutaihwa, M; Sasi, P; Shekalaghe, S, 2013
)
0.61
" Of the formulations tested, stability was highest for dry solid forms and bioavailability for hard gelatin capsules; AM release from AMAZ rectodispersible tablet was suboptimal due to a modification of its micro-crystalline structure."( Preliminary pharmaceutical development of antimalarial-antibiotic cotherapy as a pre-referral paediatric treatment of fever in malaria endemic areas.
Ba, BB; Boiron, JM; Fabre, JL; Fawaz, F; Gaubert, A; Gaudin, K; Grislain, L; Kauss, T; Lafarge, X; Lembege, M; Lindegardh, N; Marchivie, M; Millet, P; Olliaro, PL; White, NJ, 2014
)
0.4
" The purpose of the research is to improve the solubility, bioavailability and therapeutic efficacy of lipophilic artemether using homolipid-based microparticles."( Formulation, characterization and anti-malarial activity of homolipid-based artemether microparticles.
Agubata, CO; Attama, AA; Mueller-Goymann, CC; Nzekwe, IT; Onunkwo, GC, 2015
)
0.86
" Relative to the tablets, sublingual artemether had greater bioavailability (≥1."( Pharmacokinetics of a novel sublingual spray formulation of the antimalarial drug artemether in healthy adults.
Bendel, D; Davis, TM; Lee, TC; Salman, S; Templeton, D, 2015
)
0.92
"Oral delivery and bioavailability of artemether and lumefantrine could be improved using SRMS-based SLMs."( Formulation design, in vitro characterizations and anti-malarial investigations of artemether and lumefantrine-entrapped solid lipid microparticles.
Agbo, C; Agubata, O; Attama, A; Chime, S; Kenechukwu, F; Lovelyn, C; Ofokansi, K; Ogbonna, J; Umeyor, C, 2016
)
0.93
" There were no significant difference in area under the curve and bioavailability between DMNs group and intramuscular group (P>0."( Systemic delivery of artemether by dissolving microneedles.
Gao, Y; He, M; Li, C; Qiu, Y; Yang, G; Zhang, S, 2016
)
0.75
" Age had a significant positive correlation with bioavailability in a model that included allometric scaling."( Population Pharmacokinetics and Pharmacodynamics of Lumefantrine in Young Ugandan Children Treated With Artemether-Lumefantrine for Uncomplicated Malaria.
Arinaitwe, E; Aweeka, FT; Bergqvist, Y; Bigira, V; Blessborn, D; Creek, DJ; Kakuru, A; McCormack, SA; Muhindo, M; Parikh, S; Sambol, NC; Sukumar, N; Tappero, JW; Tchaparian, E; Wanzira, H, 2016
)
0.65
"Poor aqueous solubility is often linked with a poor dissolution rate and ultimately, limited bioavailability of pharmaceutical compounds."( Impact of processing methods on the dissolution of artemether from two non-ordered mesoporous silicas.
Hussain, T; Mahmood, T; Shahzad, Y; Sheikh, R; Tahir, H; Waters, LJ; Yousaf, AM, 2018
)
0.73
"Artemether (ATM) cardiotoxicity, its short half-life and low oral bioavailability are the major limiting factors for its use to treat malaria."( Reduced cardiotoxicity and increased oral efficacy of artemether polymeric nanocapsules in Plasmodium berghei-infected mice.
Antunes, LR; Grabe-Guimarães, A; Guimarães, HN; Mosqueira, VCF; Richard, S; Silveira, APA; Souza, ACM, 2018
)
2.17
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" In-vivo pharmacokinetic study revealed better absorption and long circulation of FPS and FAS, which further leads to increased relative bioavailability of drugs(13."( Fabrication and in vivo evaluation of ligand appended paclitaxel and artemether loaded lipid nanoparticulate systems for the treatment of NSCLC: A nanoparticle assisted combination oncotherapy.
Badanthadka, M; Chokshi, N; Khatri, H; Patel, BM; Patel, MM; Rawal, S, 2020
)
0.79
" Artemether (ART) is a lactone with antitumor properties, demonstrating low bioavailability and water solubility."( Artemether-loaded polymeric lipid-core nanocapsules reduce cell viability and alter the antioxidant status of U-87 MG cells.
Andrade, CMB; Branco, CLB; Costa, SA; Cruz, L; da Conceição, AGB; da Silva, KP; Ferrarini, SR; Pires, J; Reis, ÉM; Sinhorin, AP, 2022
)
3.07

Dosage Studied

The high adherence to artemether-lumefantrine found in our study suggest that this drug is likely to be very effective in Mbarara provided that patients receive clear dosage explanations. Robust training on appropriate anti-malarial and dosage is needed.

ExcerptRelevanceReference
" However, it has been associated with high recrudescent rates which may be due to incorrect dosage regimens."( Artemether in the treatment of multiple drug resistant falciparum malaria.
Bunnag, D; Harinasuta, T; Karbwang, J, 1992
)
1.73
" The proper dosage regimen remains to be defined."( Comparison of oral artemether and mefloquine in acute uncomplicated falciparum malaria.
Bangchang, KN; Bunnag, D; Chongsuphajaisiddhi, T; Harinasuta, T; Karbwang, J; Thanavibul, A, 1992
)
0.61
" When artemether was given ig or im to mice infected with Schistosoma japonicum for 32-35 d at the dosage of 1/10-1/2 LD50."( [Effect of artemether against Schistosoma japonicum].
Mei, JY; Xiao, SH; You, JQ, 1992
)
1.15
" Further studies of artesunate and artemether should be carried out to find the optimum dosage regimen and to clarify the hematological effects."( Clinical trial of artesunate and artemether on multidrug resistant falciparum malaria in Thailand. A preliminary report.
Bunnag, D; Harinasuta, T; Karbwang, J; Looareesuwan, S; Viravan, C, 1991
)
0.84
" Results showed that after injection of Artemether for 15 successive days, the T, B, and T mu lymphocytes of the 19 and 32 MKD groups were markedly reduced and the T gamma lymphocytes of all 3 dosage groups were decreased to zero."( Effects of artemether on peripheral T, B, T mu and T gamma lymphocytes in beagle dog.
Cui, YF; Gu, YX; Shi, XC; Teng, XH; Wu, BA, 1989
)
0.93
" Artemether fat emulsion was given intravenously at the dosage of 80 mg/kg."( [Assessment of absorption and distribution of artemether in rats using a thin layer chromatography scanning technique].
Jiang, JR; Shu, HL; Zeng, YL; Zou, CD, 1989
)
1.45
" In infected mice treated ig with Art at the same dosage for 24 h, the inhibition rates of alkaline phosphatase (AKP) activity in female and male worms were 30% and 25%, respectively."( [Effect of artemether on glycogen, protein, alkaline phosphatase and acid phosphatase of Schistosoma japonicum].
Feng, J; Guo, H; Jiao, P; Mei, J; Xiao, S; Yao, M; You, J, 1994
)
0.68
" In infected rabbits treated repeatedly with the above-mentioned dosage of Art at 2-wk intervals (i."( [Pathological changes in the livers of rabbits infected with schistosome cercariae and treated with artemether or praziquantel in the early stage of infection].
Xiao, S; Yang, Y; Zhang, C, 1995
)
0.51
" This novel drug delivery system may be an easy and safe way to administer artemisinin-type antimalarials and also a good alternative dosage form for active compounds with solubility problems."( Antimalarial activity of dihydroartemisinin derivatives by transdermal application.
Ager, AL; Klayman, DL; Lin, AJ, 1994
)
0.29
"kg-1 and followed by the repeated dosing at 2-3 wk intervals, the total and female worm reduction rates as compared with the control were evident."( Effect of early treatment of artemether against schistosomiasis in mice.
Jiao, PY; Mei, JY; Xiao, SH; You, JQ, 1994
)
0.58
" We noted a progressive syndrome of clinical neurological defects with cardio-respiratory collapse and death in 5/6 dogs dosed daily for 8 d with intramuscular arteether (AE) at 20 mg/kg/d in a pharmacokinetic study."( Neurotoxicity in animals due to arteether and artemether.
Brewer, TG; Grate, SJ; Heiffer, MH; Levine, BS; Peggins, JO; Petras, JM; Schuster, BG; Swearengen, J; Weina, PJ, 1994
)
0.55
" To reduce the side effects, another test was carried out in 3 monkeys and the dosage regimen was modified to pyronaridine 6 mg/kg-artemether 10 mg/kg-chloroquine 20 mg/kg (PAC-2) once daily for 3 days."( [Studies on the establishment of malarial animal model of short-term relapse. III. Combined therapy with pyronaridine-artemether-chloroquine for parasitemia clearance].
Fang, Y; Lin, BY; Pan, YR; Zhang, JX; Zheng, H, 1993
)
0.7
" When the drug was given at a daily dosage of 200 mg/kg for 4 successive days from 46 days post-infection, a significant reduction in worm recovery was observed."( Studies on chemotherapy of parasitic helminths: efficacy of artemether on Japanese strain of Schistosoma japonicum in mice.
Akyol, CV; Ishih, A; Ito, M; Sano, M; Tungtrongchitr, A, 1993
)
0.53
" In Art group, the first dose of 6 mg/kg was given in late August, followed by repeated dosing every 15 days for 3 times."( [Field studies on preventive effect of artemether against infection with Schistosoma japonicum].
Chen, M; Chu, B; Shi, Z; Wang, C; Xiao, S; Zhang, Z; Zheng, J; Zhuo, S, 1995
)
0.56
" When rabbits were treated ig with artemether 10 mg kg-1 on day 7 after infection, followed by repeated dosing every week for 4 times, some parameters related to acute schistosomiasis, such as temperature, eosinophil count and eggs in the feces were negative, and low specific antigen and antibody levels in serum were seen."( Experimental studies on early treatment of schistosomal infection with artemether.
Wang, CZ; Xiao, SH; Yang, YQ; You, JQ, 1995
)
0.8
" The results showed that in mice a promising effect was obtained when an initial dose of Art 300 mg/kg was given ig on d7 after infection with cercariae, followed by repeated dosing every wk for 4 times."( [Experimental studies on the preventive effect of artemether against schistosomal infection].
Guo, H; Jiao, P; Mei, J; Xiao, S; Yang, Y; You, J, 1995
)
0.54
" There is potential advantage of this combination therapy in reducing the dosage and treatment period of artemisinin derivative, which is therefore likely to improve complaince in clinical practice."( Artemether-pyrimethamine in the treatment of pyrimethamine-resistant falciparum malaria.
Kanda, T; Karbwang, J; Na-Bangchang, K; Suprakob, K; Tan-ariya, P; Thanavibul, A; Tipwangso, P, 1996
)
1.74
" The clinical efficacy of artemether is dependent on the formulation, dosing scheme, duration of treatment, and the severity of the disease [1, 2]."( Pharmacokinetics and bioavailability of oral and intramuscular artemether.
Congpuong, K; Karbwang, J; Molunto, P; Na-Bangchang, K; Thanavibul, A, 1997
)
0.84
" Plasma was separated from blood samples collected at different times after dosing and analysed for parent drug."( The pharmacokinetics and bioavailability of dihydroartemisinin, arteether, artemether, artesunic acid and artelinic acid in rats.
Brewer, TG; Fleckenstein, LL; Heiffer, MH; Li, QG; Masonic, K; Peggins, JO, 1998
)
0.53
"kg-1 on d 21 after infection, followed by the repeated dosing once every 1 or 2 wk for 2-4 times."( Microscopic observations on livers of rabbits and dogs infected with Schistosoma japonicum cercariae and early treatment with artemether or praziquantel.
Xiao, SH; Yang, YQ; You, JQ; Zhang, CW, 1996
)
0.5
" on d 7-15 after infection, followed by repeated dosing once every 7-15 d for a total of 3 doses."( Preventive effect of artemether in rabbits infected with Schistosoma japonicum cercariae.
Feng, Z; Guo, HF; Jiao, PY; Mei, JY; Xiao, SH; You, JQ, 1998
)
0.62
" Characterisation of these pharmacokinetic-pharmacodynamic relationships provided the basis for dosage optimisation, an approach that could be applied to other antimalarial drugs."( Clinical pharmacokinetics and pharmacodynamics and pharmacodynamics of artemether-lumefantrine.
Ezzet, F; van Vugt, M; White, NJ, 1999
)
0.54
"Electrocardiograms (ECGs) were recorded before dosing and repeatedly thereafter."( Cardiac effects of co-artemether (artemether/lumefantrine) and mefloquine given alone or in combination to healthy volunteers.
Bindschedler, M; Ezzet, F; Lefèvre, G; Meyer, I; Schaeffer, N; Thomsen, MS, 2000
)
0.62
"The RNA and DNA contents of female worms recovered from the host 48 h after dosing were markedly decreased by 51."( [Effect of artemether on nucleoside uptake and nucleic acid content in Schistosoma japonicum].
Mei, J; Xiao, S; Yao, M; You, J; Zhai, Z, 1999
)
0.69
" The high adherence to artemether-lumefantrine found in our study suggest that this drug is likely to be very effective in Mbarara provided that patients receive clear dosage explanations."( Adherence to a six-dose regimen of artemether-lumefantrine for treatment of uncomplicated Plasmodium falciparum malaria in Uganda.
Bajunirwe, F; Biraro, S; Checchi, F; Fogg, C; Guthmann, JP; Kiguli, J; Kyomugisha, A; Musabe, J; Namiiro, P; Piola, P, 2004
)
0.91
"The dose-response curves and effective concentration that resulted in a 50% inhibitory of parasitemia (IC50) of chloroquine, artemisinin, artemether and pyronaridine phosphate against Plasmodium falciparum strain FCC1/HN cultured in vitro were tested by microfluorimetric assay (MFA) and compared with those determined by microscopy-based assay."( [The microfluorimetric assay (MFA) in in vitro testing the sensitivity of Plasmodium falciparum to antimalarial drugs].
Hi, YC; Huang, F; Tang, LH; Wang, QM, 2006
)
0.54
" Insufficient numbers of tablets and inadequate package inserts result in sub-optimal dosing and possible treatment failure."( Malaria treatment failures after artemisinin-based therapy in three expatriates: could improved manufacturer information help to decrease the risk of treatment failure?
Chappuis, F; Jackson, Y; Loutan, L; Taylor, W, 2006
)
0.33
" The method has been successfully applied in the analysis of lipid based parenteral formulations and marketed oral solid dosage formulation."( Validated HPTLC method of analysis for artemether and its formulations.
Nagarsenker, MS; Tayade, NG, 2007
)
0.61
"Two HPLC-UV methods are described for the separate determination of artemether (AM) and the combined preservatives, methylparaben and propylparaben in a pharmaceutical dosage form."( Assay of artemether, methylparaben and propylparaben in a formulated paediatric antimalarial dry suspension.
Atemnkeng, MA; Marchand, E; Plaizier-Vercammen, J, 2007
)
0.99
"5 mg/kg artemether-treated group, but was significantly higher in infected rats than in uninfected rats dosed with 25."( Changes in the visceral functions of Plasmodium berghei-infected and -uninfected rats following administration of artemether.
Adeoshun, IO; Akanji, BO; Akomolafe, RO; Ayoka, AO; Fakunle, JB; Iwalewa, EO, 2006
)
0.98
" Mothers/guardians of children were asked about fever in the last 14 days and related treatment actions including the timing, drugs used, dosing and adherence supported by visual aids of commonly available drug products."( The use of artemether-lumefantrine by febrile children following national implementation of a revised drug policy in Kenya.
Ajanga, A; Amin, AA; Gitonga, CW; Kangwana, BB; Noor, AM; Snow, RW, 2008
)
0.74
" However, AL has several limitations, including a twice-daily dosing regimen, recommendation for administration with fatty food, and a high risk of reinfection soon after therapy in high transmission areas."( Artemether-lumefantrine versus dihydroartemisinin-piperaquine for treating uncomplicated malaria: a randomized trial to guide policy in Uganda.
Bukirwa, H; Dorsey, G; Kamya, MR; Lugemwa, M; Rosenthal, PJ; Rwakimari, JB; Staedke, SG; Talisuna, A; Wabwire-Mangen, F; Yeka, A, 2008
)
1.79
"DP is highly efficacious, and operationally preferable to AL because of a less intensive dosing schedule and requirements."( Artemether-lumefantrine versus dihydroartemisinin-piperaquine for treating uncomplicated malaria: a randomized trial to guide policy in Uganda.
Bukirwa, H; Dorsey, G; Kamya, MR; Lugemwa, M; Rosenthal, PJ; Rwakimari, JB; Staedke, SG; Talisuna, A; Wabwire-Mangen, F; Yeka, A, 2008
)
1.79
" PZQ given as a dosage of 60 mg/kg (1 day, 3 x 20 mg/kg doses at 4-5 hour intervals) may be as effective as a dosage of 120 mg/kg (6 days, 20 mg/kg for each day split into 3 doses at 4-5 hour intervals)."( A randomized, double-blind, placebo-controlled trial of safety and efficacy of combined praziquantel and artemether treatment for acute schistosomiasis japonica in China.
Balen, J; Ellis, M; Gray, DJ; He, YK; Hou, XY; Li, YS; Luo, XS; McManus, DP; Williams, GM, 2008
)
0.56
" Whilst administration of tribendimidine at smaller but multiple doses given within 2-3 days at the same total dosage resulted in a slightly higher worm reduction (77."( [Effect of tribendimidine, artesunate, artemether and praziquantel, administered intragastrically at single, multiple or combined doses, to rats infected with Clonorchis sinensis].
Keiser, J; Liu, XY; Qiang, HQ; Tanner, M; Utzinger, J; Xiao, SH; Xue, J; Zhang, YN, 2008
)
0.62
"5 and 7 mg/kg when dosed during organogenesis, the surviving fetuses showed fetal growth retardation without incidence of malformations, treatment during blastogenesis and fetal period had no lethal or teratogenic effect although the mean fetal body weight was significantly lower than control."( Evaluation of the developmental toxicity of artemether during different phases of rat pregnancy.
El-Dakdoky, MH, 2009
)
0.61
" hepatica, dosed orally with artemether at a concentration of 200 mg/kg and flukes recovered at 24, 48 and 72 h post-treatment (p."( Adult triclabendazole-resistant Fasciola hepatica: morphological changes in the tegument and gut following in vivo treatment with artemether in the rat model.
Brennan, GP; Fairweather, I; Halferty, L; Johnston, RC; Keiser, J; O'Neill, JF, 2009
)
0.85
" Data from previous experiments were included, and negative binomial regression analyses were carried out to determine dose-response relationships and to study the effect of drug combination."( Combination chemotherapy against Clonorchis sinensis: experiments with artemether, artesunate, OZ78, praziquantel, and tribendimidine in a rat model.
Keiser, J; Smith, TA; Utzinger, J; Xiao, SH, 2009
)
0.59
" Pharmacokinetic (PK) data informing the optimum dosing of these drug regimens is limited, especially in children."( Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
Annerberg, A; Aweeka, F; Clark, TD; Dorsey, G; Drysdale, T; German, P; Kalyango, JN; Kamya, MR; Lindegardh, N; McGee, B; Mwesigwa, J; Parikh, S; Rosenthal, PJ, 2010
)
0.68
" sinensis, dosed orally with single agents or combination treatments and flukes recovered at 3 or 5 days post-treatment."( Effect of artemether, artesunate, OZ78, praziquantel, and tribendimidine alone or in combination chemotherapy on the tegument of Clonorchis sinensis.
Keiser, J; Vargas, M, 2010
)
0.76
" The optimized spiroindolone NITD609 shows pharmacokinetic properties compatible with once-daily oral dosing and has single-dose efficacy in a rodent malaria model."( Spiroindolones, a potent compound class for the treatment of malaria.
Beck, HP; Brun, R; Cohen, SB; Dartois, V; Dharia, NV; Diagana, TT; Fidock, DA; Goh, A; González-Páez, GE; Jegla, T; Keller, TH; Lakshminarayana, SB; Lee, MC; McNamara, C; Nosten, F; Plouffe, DM; Renia, L; Rottmann, M; Russell, B; Schmitt, EK; Seitz, P; Spencer, KR; Suwanarusk, R; Tan, J; Winzeler, EA; Yeung, BK; Zou, B, 2010
)
0.36
"5 mg/kg for 7-28 days, indicating that the safe dosing duration in monkeys should be longer than 7 days under the exposure."( Toxicokinetic and toxicodynamic (TK/TD) evaluation to determine and predict the neurotoxicity of artemisinins.
Hickman, M; Li, Q, 2011
)
0.37
" Mice were treated on day 46 onwards with three dosing protocols (400 mg/kg/day for 2 days; 200 mg/kg/day for 4 days; 100 mg/kg/day for 6 days) after being infected."( Artemether shows promising female schistosomicidal and ovicidal effects on the Egyptian strain of Schistosoma mansoni after maturity of infection.
Abdul-Ghani, R; Hassan, A; Loutfy, N; Sheta, M, 2011
)
1.81
" Patients were randomized to 3 different dosing groups (weights of 5 to <15 kg, 15 and <25 kg, and 25 to <35 kg)."( Pharmacokinetic and pharmacodynamic characteristics of a new pediatric formulation of artemether-lumefantrine in African children with uncomplicated Plasmodium falciparum malaria.
Abdulla, S; Bassat, Q; Borrmann, S; Djimdé, AA; Lefèvre, G; Lyimo, J; Mandomando, I; Tekete, M, 2011
)
0.59
" Patients who remained Fasciola-positive following artemether dosing were treated with single 10 mg/kg oral triclabendazole."( Efficacy and safety of artemether in the treatment of chronic fascioliasis in Egypt: exploratory phase-2 trials.
Anani, S; Botros, S; el-Din, SS; el-Ghanam, M; el-Maadawy, W; el-Wakeel, A; Hatz, C; Keiser, J; Sabry, H; Sayed, H; Utzinger, J, 2011
)
0.93
" In the three AL body weight dosing groups (5 to < 15 kg, 15 to < 25 kg and 25 to < 35 kg), 80% of patients were aged 10-50 months, 46-100 months and 90-147 months, respectively."( Similar efficacy and safety of artemether-lumefantrine (Coartem®) in African infants and children with uncomplicated falciparum malaria across different body weight ranges.
Bashraheil, M; Bassat, Q; González, R; Kipkeu, C; Lefèvre, G; Lyimo, J; Machevo, S; Maiga, H; Mårtensson, A; Menéndez, C; Nahum, A; Nwaiwu, O; Ogutu, B; Ouma, P; Ubben, D; Walter, V, 2011
)
0.66
"Efficacy of AL in uncomplicated falciparum malaria is similar across body weight dosing groups as currently recommended in the label with no clinically relevant differences in safety or tolerability."( Similar efficacy and safety of artemether-lumefantrine (Coartem®) in African infants and children with uncomplicated falciparum malaria across different body weight ranges.
Bashraheil, M; Bassat, Q; González, R; Kipkeu, C; Lefèvre, G; Lyimo, J; Machevo, S; Maiga, H; Mårtensson, A; Menéndez, C; Nahum, A; Nwaiwu, O; Ogutu, B; Ouma, P; Ubben, D; Walter, V, 2011
)
0.66
" The study clearly demonstrates the effectiveness of this novel alternative to existing artesunate dosage forms."( Intravenous β-artemether formulation (ARM NLC) as a superior alternative to commercial artesunate formulation.
Joshi, M; Pathak, S; Patil, S; Patravale, V; Sharma, S, 2012
)
0.74
"In the first study, the toxicity of artemether was evaluated in juvenile rats dosed with 0, 10, 30, and 100mg/kg/day on postpartum days (ppds) 7 to 21."( Neurotoxicity assessment of artemether in juvenile rats.
Beckman, DA; Butt, MT; Youreneff, M, 2013
)
0.96
" More studies with appropriate control groups in larger series are needed to characterize the degree to which pregnant women are underdosed with current antimalarial dosing regimens."( Pharmacokinetic properties of artemether, dihydroartemisinin, lumefantrine, and quinine in pregnant women with uncomplicated plasmodium falciparum malaria in Uganda.
Dhorda, M; Guerin, PJ; Jullien, V; Kloprogge, F; Nosten, F; Piola, P; Tarning, J; White, NJ, 2013
)
0.68
"05013-14), the absorption of sublingual artemether was biphasic, and multiple dosing was associated with the autoinduction of the metabolism of artemether to DHA (which itself has potent antimalarial activity)."( Pharmacokinetics of a novel sublingual spray formulation of the antimalarial drug artemether in African children with malaria.
Bendel, D; Davis, TM; Lee, TC; Salman, S; Templeton, D, 2015
)
0.91
"Specially created pediatric formulations have the potential to improve the acceptability, effectiveness, and accuracy of dosing of artemisinin-based combination therapy (ACT) in young children, a patient group that is inherently vulnerable to malaria."( Tailoring a Pediatric Formulation of Artemether-Lumefantrine for Treatment of Plasmodium falciparum Malaria.
Bassat, Q; Djimde, A; Hamed, K; Ogutu, B; Stricker, K, 2015
)
0.69
" Rats infected with the triclabendazole (TCBZ)-resistant Sligo isolate were dosed orally with artemether at a concentration of 200mg/kg and flukes recovered at 24, 48 and 72 h post-treatment (pt)."( A comparative study on the impact of two artemisinin derivatives, artemether and artesunate, on the female reproductive system of Fasciola hepatica.
Brennan, GP; Fairweather, I; Halferty, L; Hanna, RE; Johnston, RC; O'Neill, JF, 2015
)
0.87
"Current artemether-lumefantrine dosing recommendations achieve day 7 lumefantrine concentrations ≥200 ng/ml and high cure rates in most uncomplicated malaria patients."( Artemether-lumefantrine treatment of uncomplicated Plasmodium falciparum malaria: a systematic review and meta-analysis of day 7 lumefantrine concentrations and therapeutic response using individual patient data.
, 2015
)
2.29
" Rats infected with the triclabendazole (TCBZ)-resistant Sligo isolate were dosed orally with artemether at a concentration of 200 mg/kg and flukes recovered at 24, 48 and 72 h post treatment (pt)."( Disruption of spermatogenesis in the liver fluke, Fasciola hepatica by two artemisinin derivatives, artemether and artesunate.
Brennan, GP; Fairweather, I; Halferty, L; Hanna, RE; Johnston, RC; O'Neill, JF, 2017
)
0.89
" The safety profiles of artesunate-mefloquine and artemether-lumefantrine were similar, with low rates of early vomiting (71 [15·3%] of 463 patients in the artesunate-mefloquine group vs 79 [16·8%] of 471 patients in the artemether-lumefantrine group in any of the three dosing days), few neurological adverse events (ten [2·1%] of 468 vs five [1·1%] of 465), and no detectable psychiatric adverse events."( Comparison of artesunate-mefloquine and artemether-lumefantrine fixed-dose combinations for treatment of uncomplicated Plasmodium falciparum malaria in children younger than 5 years in sub-Saharan Africa: a randomised, multicentre, phase 4 trial.
Ackermann, I; Aubin, F; Carn, G; Gesase, S; Lusingu, JPA; Mnkande, E; Mrango, Z; Mtoro, A; Ngocho, JS; Ogutu, B; Onyango, KO; Ouedraogo, A; Sirima, SB; Strub, N; Vanraes, J; Yaro, JB, 2016
)
0.95
" Further refinement of artemether-lumefantrine dosing to improve exposure in infants and very young children may be warranted."( Population Pharmacokinetics and Pharmacodynamics of Lumefantrine in Young Ugandan Children Treated With Artemether-Lumefantrine for Uncomplicated Malaria.
Arinaitwe, E; Aweeka, FT; Bergqvist, Y; Bigira, V; Blessborn, D; Creek, DJ; Kakuru, A; McCormack, SA; Muhindo, M; Parikh, S; Sambol, NC; Sukumar, N; Tappero, JW; Tchaparian, E; Wanzira, H, 2016
)
0.96
" However, the reduction in artemisinin exposure may warrant further study, and suggests that dosage adjustment of artemether-lumefantrine with nevirapine-based ART in children is likely warranted."( Concomitant nevirapine impacts pharmacokinetic exposure to the antimalarial artemether-lumefantrine in African children.
Aweeka, FT; Barlow-Mosha, L; Carey, V; Gingrich, D; Graham, B; Huang, L; Kamthunzi, P; Lindsey, JC; Marzan, F; Nachman, S; Parikh, S; Ssemambo, PK, 2017
)
0.9
" These data suggest that malaria and HIV coinfected pregnant women may require adjustments in AL dosage or treatment duration to achieve exposure comparable with HIV-uninfected pregnant women."( Efavirenz-Based Antiretroviral Therapy Reduces Artemether-Lumefantrine Exposure for Malaria Treatment in HIV-Infected Pregnant Women.
Aweeka, F; Huang, L; Hughes, E; Kajubi, R; Mwebaza, N; Mwima, MW; Nguyen, V; Nyunt, MM; Orukan, F; Parikh, S, 2020
)
0.82
"Good powder flow is critical for powders destined for inclusion into tablets - especially when employing direct compression as method of manufacture - in this case, lipid matrix tablets, which have demonstrated huge promise as a prospective dosage form for future use in malarial treatment."( Characterization of solid lipid dispersions prepared by hot fusion containing a double-fixed dose combination of artemether and lumefantrine.
du Plessis, LH; Viljoen, JM; Wilkins, CA, 2020
)
0.77
" This study aimed to develop an intravenous dosage form of artemether using nanotechnology."( Artemether-Loaded Zein Nanoparticles: An Innovative Intravenous Dosage Form for the Management of Severe Malaria.
Boateng-Marfo, Y; Dong, Y; Lin, HS; Ng, WK, 2021
)
2.31
"Industrial implementation of continuous oral solid dosage form manufacturing has been impeded by the poor powder flow properties of many active pharmaceutical ingredients (APIs)."( Control of Drug-Excipient Particle Attributes with Droplet Microfluidic-based Extractive Solidification Enables Improved Powder Rheology.
Doyle, PS; Khan, SA; Lai, D; Nelson, AZ; Ng, DZL; Ward, G, 2022
)
0.72
"Droplet-based extractive solidification is an attractive particle engineering technique for improving powder processing and may aid in the implementation of continuous solid dosage form manufacturing."( Control of Drug-Excipient Particle Attributes with Droplet Microfluidic-based Extractive Solidification Enables Improved Powder Rheology.
Doyle, PS; Khan, SA; Lai, D; Nelson, AZ; Ng, DZL; Ward, G, 2022
)
0.72
" Dosing is suboptimal in young children."( The Impact of Extended Treatment With Artemether-lumefantrine on Antimalarial Exposure and Reinfection Risks in Ugandan Children With Uncomplicated Malaria: A Randomized Controlled Trial.
Aweeka, FT; Colt, M; Goodwin, J; Huang, L; Kajubi, R; Li, F; Mwebaza, N; Orukan, F; Parikh, S; Richards, K; Wang, K; Whalen, ME, 2023
)
1.18
" Participants were randomly allocated 1:1 to antimalarial chemoprophylaxis, a 3-day course of twice-daily artemether-lumefantrine followed by the same daily dosing once a week while travelling in the forest and for a further 4 weeks after leaving the forest (four tablets per dose; 20 mg of artemether and 120 mg of lumefantrine per tablet), or a multivitamin with no antimalarial activity."( Antimalarial chemoprophylaxis for forest goers in southeast Asia: an open-label, individually randomised controlled trial.
Callery, JJ; Chotthanawathit, P; Conradis-Jansen, F; Dondorp, AM; Duanguppama, J; Ean, M; Heng, C; Imwong, M; Jongdeepaisal, M; Khonputsa, P; Madmanee, W; Maude, RJ; Mukaka, M; Peerawaranun, P; Pell, C; Peto, TJ; Pongsoipetch, K; Rekol, H; Sokha, M; Sovannaroth, S; Soviet, U; Tarning, J; Tripura, R; von Seidlein, L; Waithira, N; White, NJ, 2023
)
1.12
" However, the optimal choice of medication and dosing for many potential candidates is not clear."( Modelling the optimal dosing schedule for artemether-lumefantrine chemoprophylaxis against malaria.
Dondorp, AM; Maude, RJ; Tarning, J; von Seidlein, L; White, NJ, 2022
)
0.99
" However, the most favourable exposure profile, and arguably most practical dosing scenario, was an initial 3 day full AL treatment course followed by twice daily dosing given once a week for the duration of chemoprevention."( Modelling the optimal dosing schedule for artemether-lumefantrine chemoprophylaxis against malaria.
Dondorp, AM; Maude, RJ; Tarning, J; von Seidlein, L; White, NJ, 2022
)
0.99
" The major limitations of the artemisinin combination therapy are erratic absorption from the injection site and high dosing frequency due to a very short elimination half-life of the drug."( Evaluation of Pharmacokinetics, Biodistribution, and Antimalarial Efficacy of Artemether-Loaded Polymeric Nanorods.
Bhide, AR; Dighe, VD; Jindal, AB; Jirwankar, YB; Katnoria, S; Kaur, S; Suri, M, 2023
)
1.14
" Participants were randomly assigned (1:1) to receive single low-dose primaquine combined with either artemether-lumefantrine or dihydroartemisinin-piperaquine, dosed by bodyweight."( Safety of age-dosed, single low-dose primaquine in children with glucose-6-phosphate dehydrogenase deficiency who are infected with Plasmodium falciparum in Uganda and the Democratic Republic of the Congo: a randomised, double-blind, placebo-controlled, n
Abongo, G; Basara, BB; Baseke, J; Bongo, GS; Day, NJP; Dhorda, M; Dondorp, AM; Fanello, C; Kayembe, DK; Maitland, K; Muhindo, R; Mukaka, M; Namayanja, C; Ndjowo, PO; Okalebo, CB; Olupot-Olupot, P; Onyamboko, MA; Onyas, P; Peerawaranun, P; Tarning, J; Taya, C; Taylor, WR; Titin, H; Uyoga, S; Waithira, N; Weere, W; Williams, TN, 2023
)
1.13
" Parasite regrowth occurred after dosing with 200 mg (3/3 participants) and 300 mg (3/4 participants) but not after 400 mg or 600 mg."( Characterizing the Blood-Stage Antimalarial Activity of Tafenoquine in Healthy Volunteers Experimentally Infected With Plasmodium falciparum.
Abd-Rahman, AN; Barber, BE; Birrell, GW; Edstein, MD; Leelasena, I; Llewellyn, S; Marquart, L; McCarthy, JS; Moehrle, JJ; Potter, AJ; Sahai, N; Shanks, GD; Webster, R; Wesche, D, 2023
)
0.91
"This retrospective, observational study explored associations between changing malaria service point (health facility or CHW) density per 1000 people and severe malaria admissions or malaria inpatient deaths by district and month in a dose-response approach, using existing routine and programmatic data."( Effectiveness of community case management of malaria on severe malaria and inpatient malaria deaths in Zambia: a dose-response study using routine health information system data.
Ashton, RA; Bennett, A; Burnett, S; Eisele, TP; Hainsworth, M; Hamainza, B; Lungu, C; Miller, JM; Porter, T; Rutagwera, MI; Silumbe, K; Slater, H, 2023
)
0.91
" Robust training on appropriate anti-malarial and dosage is needed, particularly given the recent change in recommendation for artemether-lumefantrine use in the first trimester."( Healthcare provider and drug dispenser knowledge and adherence to guidelines for the case management of malaria in pregnancy in the context of multiple first-line artemisinin-based combination therapy in western Kenya.
Dellicour, S; Gutman, JR; Hill, J; Ochodo, E; Osoro, CB; Ter Kuile, F; Young, T, 2023
)
1.12
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
antimalarialA drug used in the treatment of malaria. Antimalarials are usually classified on the basis of their action against Plasmodia at different stages in their life cycle in the human.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (5)

ClassDescription
sesquiterpenoidAny terpenoid derived from a sesquiterpene. The term includes compounds in which the C15 skeleton of the parent sesquiterpene has been rearranged or modified by the removal of one or more skeletal atoms (generally methyl groups).
cyclic acetalAn acetal in the molecule of which the acetal carbon and one or both oxygen atoms thereon are members of a ring.
organic peroxideCompounds of structure ROOR' in which R and R' are organic groups.
artemisinin derivativeAny organic peroxide formally obtained from artemisinin.
semisynthetic derivativeAny organic molecular entity derived from a natural product by partial chemical synthesis.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (1)

PathwayProteinsCompounds
Artemether Metabolism Pathway410

Protein Targets (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency2.07860.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency2.11320.000221.22318,912.5098AID743042
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency50.11870.01237.983543.2770AID1645841
pregnane X nuclear receptorHomo sapiens (human)Potency15.84890.005428.02631,258.9301AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency18.99590.000229.305416,493.5996AID743069
GVesicular stomatitis virusPotency39.81070.01238.964839.8107AID1645842
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency16.20110.000323.4451159.6830AID743065; AID743067
Interferon betaHomo sapiens (human)Potency39.81070.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency39.81070.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency39.81070.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency39.81070.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (86)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (40)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (32)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (283)

Assay IDTitleYearJournalArticle
AID1751422Antifungal activity against Candida albicans SC5314 assessed as inhibition of fungal filamentation in Spider medium at 100 uM incubated for 1 hr by microscopic analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID729046Antimalarial activity against Plasmodium berghei ANKA infected in C57BL/6J mouse assessed as suppression of blood parasitemia level at 6 mg/kg, po measured on day 3 relative to vehicle-treated control in presence of lumefantrine2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and antimalarial efficacy of two-carbon-linked, artemisinin-derived trioxane dimers in combination with known antimalarial drugs.
AID247005Effective dose required to reduce the parasitemia in mice when compound administered with SSV after 3 day postinfection2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID497986Cmax in Ugandan children patient with uncomplicated malaria assessed as dihydroartemisin administered twice daily for 3 days as 20/120 mg tablets containing artemether-lumefantrine combination2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID443096Antimalarial activity against Plasmodium berghei ANKA infected NMRI mice (Mus musculus) assessed as reduction of parasitemia treated perorally for 3 days measured on day 42010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Modular synthesis and in vitro and in vivo antimalarial assessment of C-10 pyrrole mannich base derivatives of artemisinin.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID481435Therapeutic index, ratio of TD50 for HFF cells to IC50 for Toxoplasma gondii F22010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Thiazole, oxadiazole, and carboxamide derivatives of artemisinin are highly selective and potent inhibitors of Toxoplasma gondii.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1283271Inhibition of HMGCoA reductase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID1304202Antimalarial activity against multidrug resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I fluorescence based assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities.
AID543627Antimicrobial activity against Echinococcus granulosus protoscoleces assessed as reduction in protoscoleces viability at 40 uM by trypan blue exclusion assay2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro and in vivo treatments of echinococcus protoscoleces and metacestodes with artemisinin and artemisinin derivatives.
AID1751431Antifungal activity against Candida parapsilosis NL001 assessed as fungal growth at 100 uM measured after 24 hrs by absorbance based analysis relative to vehicle-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID158869In vitro antimalarial activity against Plasmodium falciparum W2 Indochina1995Journal of medicinal chemistry, Mar-03, Volume: 38, Issue:5
Antimalarial activity of new dihydroartemisinin derivatives. 6. alpha-Alkylbenzylic ethers.
AID251473Antimalarial activity (100 mg/kg, subcutaneously) given 1 day post infection of mice (Mus musculus) with Plasmodium berghei is its ability to reduce parasitemia on day 3 post infection2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID285476Antimalarial activity against Plasmodium vinckei petteri infected subcutaneously dosed Swiss Albino mice (Mus musculus)2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Trioxaquines are new antimalarial agents active on all erythrocytic forms, including gametocytes.
AID1251274Antimalarial activity against Plasmodium berghei ANKA infected in C57BL/6 mouse experimental cerebral model assessed as mouse survival rate at 25 mg/kg, ip qd for 5 days measured after 24 hrs2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
NO-Donor Dihydroartemisinin Derivatives as Multitarget Agents for the Treatment of Cerebral Malaria.
AID158698In vitro inhibitory concentration against chloroquine-sensitive Plasmodium falciparum HB32002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Mechanism-based design of parasite-targeted artemisinin derivatives: synthesis and antimalarial activity of new diamine containing analogues.
AID1751419Potentiation of micafungin-induced antifungal activity against Candida albicans SC5314 assessed as fungal growth at 100 microM measured after 24 hrs in presence of micafungin by absorbance based analysis relative to micafungin-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID748940Half life in human2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Recent advances in malaria drug discovery.
AID276159Antimalarial activity against Plasmodium falciparum NF542006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine.
AID252957Ratio of concentration that reduced cell viability to inhibitory concentration for ConA-induced T cell proliferation2005Journal of medicinal chemistry, Jul-14, Volume: 48, Issue:14
Synthesis and immunosuppressive activity of new artemisinin derivatives. 1. [12(beta or alpha)-Dihydroartemisininoxy]phen(ox)yl aliphatic acids and esters.
AID317969Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum by [3H]hypoxanthine incorporation2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum.
AID1327393Cytotoxicity against CHO cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID285474Antimalarial activity against Plasmodium vinckei petteri infected intraperitoneally dosed Swiss Albino mice (Mus musculus)2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Trioxaquines are new antimalarial agents active on all erythrocytic forms, including gametocytes.
AID543629Antimicrobial activity against Echinococcus multilocularis metacestode assessed as increase in alkaline phosphatase activity at 40 uM within 4 days2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro and in vivo treatments of echinococcus protoscoleces and metacestodes with artemisinin and artemisinin derivatives.
AID323679Reduction of [3H]chloroquine uptake in chloroquine-sensitive Plasmodium falciparum 3D7 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID383806Cytotoxicity against mouse Ehrlich Ascites carcinoma by trypan blue exclusion assay2008European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
Bioactive peroxides as potential therapeutic agents.
AID1751424Potentiation of fluconazole-induced antifungal activity against Candida albicans SC5314 assessed as inhibition of fungal filamentation by measuring reduction in fungal hyphae growth in Spider medium at 100 uM incubated for 1 hr in presence of fluconazole 2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1175637Antimalarial activity Plasmodium berghei ANKA infected in C57BL/6J mouse assessed as suppression of parasitemia at 6 mg/kg, po administered as single dose combined with 18 mg/kg mefloquine hydrochloride measured on day 3 after innfection2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Antimalarial chemotherapy: orally curative artemisinin-derived trioxane dimer esters.
AID729112Antimalarial activity against Plasmodium berghei ANKA infected in C57BL/6J mouse assessed as average survival time at 6 mg/kg, po in presence of mefloquine (Rvb = 8.8 days)2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and antimalarial efficacy of two-carbon-linked, artemisinin-derived trioxane dimers in combination with known antimalarial drugs.
AID1751429Antifungal activity against Candida auris NL002 assessed as fungal growth at 100 uM measured after 24 hrs by absorbance based analysis relative to vehicle-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID158856Inhibitory concentration against Plasmodium falciparum W2 Indochina1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Arteether, a new antimalarial drug: synthesis and antimalarial properties.
AID497988Cmax in Ugandan children patient with uncomplicated malaria administered twice daily for 3 days as 20/120 mg tablets containing artemether-lumefantrine combination2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID247016Effective dose required to reduce the parasitemia in mice when compound administered with Tween-80 after 3 day postinfection2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID113169In vivo antimalarial activity in mice (Mus musculus) against chloroquine-sensitive Plasmodium berghei N after oral administration2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides.
AID753934Cytotoxicity against human JURKAT-TALL cells after 48 hrs by Alamar Blue assay2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
Artemisinin-derived dimer phosphate esters as potent anti-cytomegalovirus (anti-CMV) and anti-cancer agents: a structure-activity study.
AID1751448Antifungal activity against Saccharomyces cerevisiae harboring pdr10 delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1751443Antifungal activity against Saccharomyces cerevisiae harboring adp1 delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1751461Potentiation of fluconazole-induced antifungal activity against Candida albicans CNL002 harboring cdr1 delta mutant assessed as inhibition of fungal growth at 100 uM measured after 24 hrs by absorbance based analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID247108Effective dose required to reduce the parasitemia in mice when compound administered with SSV after 3 day postinfection2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1304203Antimalarial activity against multidrug resistant Plasmodium falciparum W2 infected in human erythrocytes assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I fluorescence based assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities.
AID323683Reduction of [3H]dihydroartemisinin uptake in chloroquine-resistant Plasmodium falciparum K1 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID1751454Antifungal activity against Saccharomyces cerevisiae harboring ybt1 delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID113177In vivo antimalarial activity against Plasmodium berghei. Activity expressed as ED50.1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Structure-activity relationships of lactone ring-opened analogs of the antimalarial 1,2,4-trioxane artemisinin.
AID444495Anticancer activity against human XF498 cells by sulforhodamine B assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and anticancer activity of novel amide derivatives of non-acetal deoxoartemisinin.
AID236289Volume distribution after intravenous administration of 10 mg/kg2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID248452In vitro inhibition of chloroquine-sensitive Plasmodium falciparum NF542005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID1327394Selectivity index, ratio of IC50 for human WI38 cells to IC50 for chloroquine-sensitive asexual erythrocyte stage form Plasmodium falciparum NF542016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID560761Stability of compound in presence of oxyhemoglobin assessed as pseudo-first order degradation rate constant at 10 uM at 20degC over 24 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Stability of peroxide antimalarials in the presence of human hemoglobin.
AID276164Partition coefficient, logP of the compound2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1751434Potentiation of fluconazole-induced antifungal activity against Candida tropicalis NL001 assessed as fungal growth at 100 uM measured after 24 hrs in presence of fluconazole by absorbance based analysis relative to vehicle treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID13116Volume of distribution following 10 mg/kg intravenous or 50 mg/kg oral dosing in rats was determined2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin.
AID1698017Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 by LDH assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes.
AID511098Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as survival at 10 mg/kg, perorally administered through 7% Tween80/3% Ethanol formulation 24 hrs post infection for 3 days measured 96 hrs post infecti2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID323682Reduction of [3H]dihydroartemisinin uptake in chloroquine-sensitive Plasmodium falciparum FC27 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID1327389Antiplasmodial activity against chloroquine-sensitive asexual erythrocyte stage form Plasmodium falciparum NF54 measured after 48 hrs by pLDH assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID1751442Antifungal activity against Saccharomyces cerevisiae BY4742 assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1698023Selectivity index, ratio of IC50 for CHO cells to IC50 for antileishmanial activity against Leishmania donovani 9515 by resazurin dye based assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes.
AID1751462Inhibition of PDR5 in Saccharomyces cerevisiae BY4742 assessed as inhibition of R6G efflux incubated for 4 hrs followed by R6G addition and measured after 1.5 hrs by fluorescence based analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID248451In vitro concentration of compound required to inhibit ConA-induced T cell proliferation to 50% in BALB/c mice2005Journal of medicinal chemistry, Jul-14, Volume: 48, Issue:14
Synthesis and immunosuppressive activity of new artemisinin derivatives. 1. [12(beta or alpha)-Dihydroartemisininoxy]phen(ox)yl aliphatic acids and esters.
AID1751440Antifungal activity against Cryptococcus neoformans H99 assessed as inhibition of fungal growth at 0.2 uM measured every 15 mins for 24 hrs by absorbance based analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID510649Antimalarial activity against Plasmodium falciparum 3D7 assessed as parasite growth inhibition at 8 nM after 6 hrs by [3H]hypoxanthin incorporation assay2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID21492Solubility in oral formulation was determined after incubation at 25 degree C2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin.
AID19205Partition coefficient between octanol and water (logP)2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin.
AID1163255Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O positive erythrocyte assessed as reduction in parasitemia after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1251266Antiplasmodial activity against Plasmodium berghei ANKA early trophozoite stage by parasite LDH assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
NO-Donor Dihydroartemisinin Derivatives as Multitarget Agents for the Treatment of Cerebral Malaria.
AID323678Reduction of [3H]chloroquine uptake in chloroquine-sensitive Plasmodium falciparum FC27 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID1751456Antifungal activity against Saccharomyces cerevisiae harboring ynr070w delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1251272Antimalarial activity against Plasmodium berghei ANKA infected in C57BL/6 mouse experimental cerebral model with body temperature >32 deg C assessed as mouse survival rate at 25 mg/kg, ip qd for 5 days2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
NO-Donor Dihydroartemisinin Derivatives as Multitarget Agents for the Treatment of Cerebral Malaria.
AID1327387Thermal stability of the compound assessed as onset of decomposition temperature by thermogravimetric analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID481433Antiparasitic activity against Toxoplasma gondii 2F infected in HFF cells assessed as beta galactosidase activity after 5 days2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Thiazole, oxadiazole, and carboxamide derivatives of artemisinin are highly selective and potent inhibitors of Toxoplasma gondii.
AID1751421Antifungal activity against Candida albicans SC5314 assessed as inhibition of fungal filamentation in YEPD containing 10% serum medium at 100 uM incubated for 1 hr by microscopic analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID510909Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as reduction in parasitaemia at 10 mg/kg, perorally administered as single dose 24 hrs post infection for 1 day measured 72 hrs post infection2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID444496Anticancer activity against human SK-MEL-2 cells by sulforhodamine B assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and anticancer activity of novel amide derivatives of non-acetal deoxoartemisinin.
AID510925Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as cure rate at 50 mg/kg, perorally administered through 0.5% MCM/0.1%solutol HS15 formulation 24 hrs post infection for 3 days measured on day 30 post2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID444497Anticancer activity against human A549 cells by sulforhodamine B assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and anticancer activity of novel amide derivatives of non-acetal deoxoartemisinin.
AID1751417Antifungal activity against Candida albicans SC5314 assessed as inhibition of fungal growth by measuring decrease in OD600 at 100 microM measured after 24 hrs by absorbance based analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1751418Potentiation of amphotericin B-induced antifungal activity against Candida albicans SC5314 assessed as fungal growth at 100 microM measured after 24 hrs in presence of amphotericin B by absorbance based analysis relative to amphotericin B-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1751437Potentiation of fluconazole-induced antifungal activity against Candida tropicalis NL001 assessed as fungal growth at 100 uM measured after 24 hrs in presence of fluconazole by absorbance based analysis relative to fluconazole-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID323680Reduction of [3H]chloroquine uptake in chloroquine-resistant Plasmodium falciparum RSA11 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID251256Survival of mice to 30-day postinfection with Plasmodium berghei upon 100 mg/kg upon subcutaneous dose was determined2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID1751455Antifungal activity against Saccharomyces cerevisiae harboring ycf1 delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1327395Selectivity index, ratio of IC50 for CHO cells to IC50 for chloroquine-sensitive asexual erythrocyte stage form Plasmodium falciparum NF542016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID285475Antimalarial activity against Plasmodium vinckei petteri infected orally dosed Swiss Albino mice (Mus musculus)2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Trioxaquines are new antimalarial agents active on all erythrocytic forms, including gametocytes.
AID1751463Inhibition of PDR5 in Saccharomyces cerevisiae BY4742 assessed as inhibition of R6G efflux at 400 uM incubated for 4 hrs followed by R6G addition and measured after 1.5 hrs by fluorescence based analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1751432Antifungal activity against Saccharomyces cerevisiae BY4742 assessed as inhibition of fungal growth at 100 uM measured after 24 hrs by absorbance based analysis relative to vehicle-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1751420Potentiation of fluconazole-induced antifungal activity against Candida albicans SC5314 assessed as fungal growth at 100 microM measured after 24 hrs in presence of fluconazole by absorbance based analysis relative to fluconazole-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID119665Number of mice survived in a group of 18 mice after injecting single intraperitoneal dose of 1000 mg/kg (single dose of 250 mg/kg did not cause mice mortality)2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides.
AID1327390Antiplasmodial activity against chloroquine-resistant asexual erythrocyte stage form Plasmodium falciparum Dd2 measured after 48 hrs by pLDH assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID119666Number of mice survived in a group of 18 mice after injecting single intraperitoneal dose of 500 mg/kg (single dose of 250 mg/kg did not cause mice mortality)2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides.
AID248408In vitro inhibition of chloroquine-resistant Plasmodium falciparum K12005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID510914Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as survival at 100 mg/kg, perorally administered as single dose 24 hrs post infection for 1 day measured 72 hrs post infection2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID1751430Antifungal activity against Candida tropicalis NL001 assessed as fungal growth at 100 uM measured after 24 hrs by absorbance based analysis relative to vehicle-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1327391Resistance index, ratio of IC50 for chloroquine-resistant asexual erythrocyte stage form Plasmodium falciparum Dd2 to IC50 for chloroquine-sensitive asexual erythrocyte stage form Plasmodium falciparum NF542016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID158198In vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum HB32001Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1
Synthesis, antimalarial activity, biomimetic iron(II) chemistry, and in vivo metabolism of novel, potent C-10-phenoxy derivatives of dihydroartemisinin.
AID1751464Inhibition of PDR5 in Saccharomyces cerevisiae BY4741 assessed as intracellular accumulation of fluconazole at 400 uM measured per gm of cells after 4 hrs by HPLC analysis (Rvb = 11.3 nmol)2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID158686In vitro inhibitory activity against the chloroquine-resistant Plasmodium falciparum W2 Indochina2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Alkylation of manganese(II) tetraphenylporphyrin by antimalarial fluorinated artemisinin derivatives.
AID251434Antimalarial activity is its ability to reduce survival days (100 mg/kg, subcutaneously) of mice (Mus musculus) infected with Plasmodium berghei2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID323685Reduction of [3H]dihydroartemisinin uptake in chloroquine-resistant Plasmodium falciparum RSA11 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID158868In vitro antimalarial activity against Plasmodium falciparum D6 (Sierra Leone I)1995Journal of medicinal chemistry, Mar-03, Volume: 38, Issue:5
Antimalarial activity of new dihydroartemisinin derivatives. 6. alpha-Alkylbenzylic ethers.
AID1751445Antifungal activity against Saccharomyces cerevisiae harboring bpt1 delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1698019Cytotoxicity against CHO cells assessed as reduction in cell viability by MTT assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes.
AID1304204Resistance index, ratio of IC50 for multi-drug-resistant Plasmodium falciparum K1 infected in human erythrocytes to IC50 for chloroquine-sensitive asexual Plasmodium falciparum NF54 infected in human erythrocytes2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities.
AID497984Half life in Ugandan children patient with uncomplicated malaria assessed as dihydroartemisin administered twice daily for 3 days as 20/120 mg tablets containing artemether-lumefantrine combination2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID158195In vitro anti-protozoal activity against Plasmodium falciparum Ghana2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
1,4-Dihydroxy-2,3-dioxatricyclo[8.4.0.0(4,9)]tetradecane and derivatives with in vitro activity against Plasmodium falciparum, Trypanasoma b brucei, Trypanasoma cruzi, and Leishmaniasis infantum.
AID1751449Antifungal activity against Saccharomyces cerevisiae harboring pdr11 delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID417432Inhibition of beta-hematin formation at drug to heme molar equivalent ratio of 15 by infrared spectra measured after 18 hrs2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Trioxaquines and heme-artemisinin adducts inhibit the in vitro formation of hemozoin better than chloroquine.
AID1751438Potentiation of fluconazole-induced antifungal activity against Candida parapsilosis NL001 assessed as fungal growth at 100 uM measured after 24 hrs in presence of fluconazole by absorbance based analysis relative to fluconazole-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID510922Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as survival at 50 mg/kg, perorally administered through 0.5% MCM/0.1%solutol HS15 formulation 24 hrs post infection for 3 days measured 96 hrs post inf2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID510912Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as survival at 10 mg/kg, perorally administered as single dose as single dose 24 hrs post infection for 1 day measured 72 hrs post infection2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID1698025Selectivity index, ratio of IC50 for CHO cells to IC50 for antileishmanial activity against Leishmania major IR-173 by resazurin dye based assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes.
AID543630Antimicrobial activity against Echinococcus multilocularis metacestode assessed as increase in alkaline phosphatase activity at 10 uM2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro and in vivo treatments of echinococcus protoscoleces and metacestodes with artemisinin and artemisinin derivatives.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1751436Potentiation of fluconazole-induced antifungal activity against Candida auris NL002 assessed as fungal growth at 100 uM measured after 24 hrs in presence of fluconazole by absorbance based analysis relative to fluconazole-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1175636Antimalarial activity Plasmodium berghei ANKA infected in C57BL/6J mouse assessed as mouse survival at 6 mg/kg, po administered as single dose combined with 18 mg/kg mefloquine hydrochloride2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Antimalarial chemotherapy: orally curative artemisinin-derived trioxane dimer esters.
AID117773Percent survival of mice (Mus musculus) after 20 days post infection of malarial parasite in out of 5 mice (Mus musculus)2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin.
AID323681Reduction of [3H]chloroquine uptake in chloroquine-resistant Plasmodium falciparum RSA11 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID1327392Cytotoxicity against human WI38 cells assessed as reduction in cell viability measured after 48 hrs by SRB assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID520092Induction of heme alkylation of Fe(II) heme assessed as loss of heme at 10 uM in presence of 50% ACN-H2O with excess sodium dithionite under argon at 20 degC by spectrophotometry2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Relationship between antimalarial activity and heme alkylation for spiro- and dispiro-1,2,4-trioxolane antimalarials.
AID276160Antimalarial activity in Plasmodium berghei infected MORO mice (Mus musculus) at 10 mg/kg peroral dose2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine.
AID251470Antimalarial activity (10 mg/kg, subcutaneously) given 1 day post infection of mice (Mus musculus) with Plasmodium berghei is its ability to reduce parasitemia on day 3 post infection2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID418051Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected type A+ human erythrocytes after 24 hrs by [G-3H]hypoxanthine uptake2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates.
AID252956Ratio of concentration that reduced cell viability to inhibitory concentration for LPS-induced B cell proliferation2005Journal of medicinal chemistry, Jul-14, Volume: 48, Issue:14
Synthesis and immunosuppressive activity of new artemisinin derivatives. 1. [12(beta or alpha)-Dihydroartemisininoxy]phen(ox)yl aliphatic acids and esters.
AID1751450Antifungal activity against Saccharomyces cerevisiae harboring pdr12 delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID13323Oral bioavailability in rat (dose 10 mg/kg i.v. and 50 mg/kg p.o.)2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin.
AID560762Stability of compound in presence of methoxyhemoglobin assessed as pseudo-first order degradation rate constant at 10 uM at 20degC over 24 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Stability of peroxide antimalarials in the presence of human hemoglobin.
AID1304206Cytotoxicity against human WI38 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities.
AID403421Antifungal activity against Cryptococcus neoformans ATCC 90113 by modified NCCLS method2005Journal of natural products, Aug, Volume: 68, Issue:8
Antifungal activity of artemisinin derivatives.
AID276162Survival of MORO mice (Mus musculus) infected with Plasmodium berghei at 10 mg/kg, perorally after 30 day post-infection2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine.
AID113170In vivo antimalarial activity in mice (Mus musculus) against chloroquine-sensitive Plasmodium berghei N after subcutaneous administration2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides.
AID1751446Antifungal activity against Saccharomyces cerevisiae harboring nft1 delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID368231Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine uptake2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Synthesis and biological evaluation of extraordinarily potent C-10 carba artemisinin dimers against P. falciparum malaria parasites and HL-60 cancer cells.
AID246938Effective dose required to reduce the parasitemia in mice by suppressive test after 4 day postinfection2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID1751466Antifungal activity against Saccharomyces cerevisiae YNL013 harboring pdr5 delta mutant assessed as inhibition of fungal growth at 100 uM measured after 24 hrs by absorbance based analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID251433Antimalarial activity is its ability to reduce survival days (100 mg/kg, peroral) of mice (Mus musculus) infected with Plasmodium berghei2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID1546521Cytotoxicity against human MCF7 cells at 50 nM in presence of doxorubicin relative to control2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Artemisia: a promising plant for the treatment of cancer.
AID118005In vivo antimalarial activity against Plasmodium berghei NK173 in mice (Mus musculus) by intraperitoneal route at a concentration of 35.5 uM/kg at day 112004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin.
AID1751423Potentiation of fluconazole-induced antifungal activity against Candida albicans SC5314 assessed as inhibition of fungal filamentation by measuring reduction in fungal hyphae growth in YEPD containing 10% serum medium at 100 uM incubated for 1 hr in prese2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID772517Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Using genetic methods to define the targets of compounds with antimalarial activity.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID276161Antimalarial activity in Plasmodium berghei infected MORO mice (Mus musculus) at 10 mg/kg subcutaneous dose2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine.
AID276163Survival of MORO mice (Mus musculus) infected with Plasmodium berghei at 10 mg/kg, subcutaneously after 30 day post-infection2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine.
AID112562In vivo antimalarial activity in mice (Mus musculus) against chloroquine-sensitive Plasmodium berghei N after oral administration2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides.
AID418052Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 infected type A+ human erythrocytes after 24 hrs by [G-3H]hypoxanthine uptake2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates.
AID319193Antimalarial activity against Plasmodium falciparum 3D72008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles.
AID444498Anticancer activity against human SKOV3 cells by sulforhodamine B assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and anticancer activity of novel amide derivatives of non-acetal deoxoartemisinin.
AID118008In vivo antimalarial activity against Plasmodium berghei NK173 in mice (Mus musculus) by intraperitoneal route at a concentration of 35.5 uM/kg at day 42004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID19456Partition coefficient (logP)2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Alkylation of manganese(II) tetraphenylporphyrin by antimalarial fluorinated artemisinin derivatives.
AID314497Antimalarial activity against Plasmodium falciparum 3D72008Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
An efficient route into synthetically challenging bridged achiral 1,2,4,5-tetraoxanes with antimalarial activity.
AID323684Reduction of [3H]dihydroartemisinin uptake in chloroquine-sensitive Plasmodium falciparum 3D7 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID144637Evaluated for the neurotoxicity against NB2a Neuroblastoma cells.2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Synthesis and antimalarial activity of sixteen dispiro-1,2,4, 5-tetraoxanes: alkyl-substituted 7,8,15,16-tetraoxadispiro[5.2.5. 2]hexadecanes.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1304201Antimalarial activity against chloroquine-sensitive asexual Plasmodium falciparum NF54 infected in human erythrocytes assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I fluorescence based assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities.
AID338840Cell cycle arrest in mouse EAC assessed as accumulation at S phase by FACS analysis1993Journal of natural products, Jun, Volume: 56, Issue:6
Cytotoxicity of artemisinin-related endoperoxides to Ehrlich ascites tumor cells.
AID1751435Potentiation of fluconazole-induced antifungal activity against Candida parapsilosis NL001 assessed as fungal growth at 100 uM measured after 24 hrs in presence of fluconazole by absorbance based analysis relative to vehicle-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1698018Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 by LDH assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes.
AID368232Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Synthesis and biological evaluation of extraordinarily potent C-10 carba artemisinin dimers against P. falciparum malaria parasites and HL-60 cancer cells.
AID1751444Antifungal activity against Saccharomyces cerevisiae harboring aus1 delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID414407Antimalarial activity after 48 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Antitumour and antimalarial activity of artemisinin-acridine hybrids.
AID13114Plasma clearance following 10 mg/kg intravenous or 50 mg/kg oral dosing in rats2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin.
AID245962In vitro concentration of compound required to reduced spleen cell viability to 50% in BALB/c mice2005Journal of medicinal chemistry, Jul-14, Volume: 48, Issue:14
Synthesis and immunosuppressive activity of new artemisinin derivatives. 1. [12(beta or alpha)-Dihydroartemisininoxy]phen(ox)yl aliphatic acids and esters.
AID497995AUC (0-infinity) in Ugandan children patient with uncomplicated malaria administered twice daily for 3 days as 20/120 mg tablets containing artemether-lumefantrine combination2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID444500Anticancer activity against human HCT15 cells by sulforhodamine B assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and anticancer activity of novel amide derivatives of non-acetal deoxoartemisinin.
AID251469Antimalarial activity (10 mg/kg, peroral) given 1 day post infection of mice (Mus musculus) with Plasmodium berghei is its ability to reduce parasitaemia on day 3 post infection2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1751465Increase in intracellular fluconazole accumulation in Saccharomyces cerevisiae YNL032 harboring pdr5 deletion mutant at 400 uM measured after 4 hrs by HPLC analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID443013Therapeutic index, ratio of IC50 for human KB cells to IC50 for Plasmodium falciparum 3D72010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Modular synthesis and in vitro and in vivo antimalarial assessment of C-10 pyrrole mannich base derivatives of artemisinin.
AID1751457Antifungal activity against Saccharomyces cerevisiae harboring yol075c delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID158197In vitro antimalarial activity against Plasmodium falciparum FCR32003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Synthesis and antimalarial activity of 2-methoxyprop-2-yl peroxides derivatives.
AID251472Antimalarial activity (100 mg/kg, peroral) given 1 day post infection of mice (Mus musculus) with Plasmodium berghei is its ability to reduce parasitaemia on day 3 post infection2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID510949Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as reduction in parasitaemia at 10 mg/kg, perorally administered through 7% Tween80/3% Ethanol formulation 24 hrs post infection for 3 days measured 962010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID366933Antiplasmodial activity in Plasmodium berghei ANKA infected BALB/c mice (Mus musculus) at 54 mg/kg peroral dose as reduced parasitaemia2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells.
AID338836Cytotoxicity against mouse EAC at >125 uM after 3 days by MTT assay1993Journal of natural products, Jun, Volume: 56, Issue:6
Cytotoxicity of artemisinin-related endoperoxides to Ehrlich ascites tumor cells.
AID403422Antifungal activity against Candida albicans ATCC 90028 at 50 ug/mL by modified NCCLS method2005Journal of natural products, Aug, Volume: 68, Issue:8
Antifungal activity of artemisinin derivatives.
AID1698020Antileishmanial activity against Leishmania donovani 1S promastigotes assessed as inhibition of parasite growth incubated for 72 hrs by resazurin dye based assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes.
AID338835Cytotoxicity against mouse EAC after 3 days by MTT assay1993Journal of natural products, Jun, Volume: 56, Issue:6
Cytotoxicity of artemisinin-related endoperoxides to Ehrlich ascites tumor cells.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID247109Effective dose required to reduce the parasitemia in mice when compound administered with Tween-80 after 3 day postinfection2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID1751458Antifungal activity against Saccharomyces cerevisiae harboring yor1 delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID26470Half-life in plasma2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Alkylation of manganese(II) tetraphenylporphyrin by antimalarial fluorinated artemisinin derivatives.
AID158862Intrinsic equimolar activity against Plasmodium falciparum D6 (Sierra Leone) relative to QHS1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Arteether, a new antimalarial drug: synthesis and antimalarial properties.
AID510911Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as reduction in parasitaemia at 100 mg/kg, perorally administered as single dose 24 hrs post infection for 1 day measured 72 hrs post infection2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID497987Half life in Ugandan children patient with uncomplicated malaria administered twice daily for 3 days as 20/120 mg tablets containing artemether-lumefantrine combination2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID1751426Antifungal activity against fluconazole-resistant Candida albicans CNL012 assessed as fungal growth at 100 uM measured after 24 hrs by absorbance based analysis relative to vehicle-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID753935Antiviral activity against Cytomegalovirus infected in HFF after 72 hrs by luciferase reporter gene assay2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
Artemisinin-derived dimer phosphate esters as potent anti-cytomegalovirus (anti-CMV) and anti-cancer agents: a structure-activity study.
AID1698024Selectivity index, ratio of IC50 for CHO cells to IC50 for antileishmanial activity against Leishmania donovani 1S by resazurin dye based assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes.
AID1251270Antimalarial activity against Plasmodium berghei ANKA infected in C57BL/6 mouse experimental cerebral model assessed as mouse survival rate at 25 mg/kg, ip qd for 5 days2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
NO-Donor Dihydroartemisinin Derivatives as Multitarget Agents for the Treatment of Cerebral Malaria.
AID510913Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as survival at 30 mg/kg, perorally administered as single dose 24 hrs post infection for 1 day measured 72 hrs post infection2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID158709In vitro inhibitory concentration against chloroquine-resistant Plasmodium falciparum FcB12004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin.
AID520093Antimalarial activity against chloroquine-resistant Plasmodium falciparum K12008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Relationship between antimalarial activity and heme alkylation for spiro- and dispiro-1,2,4-trioxolane antimalarials.
AID510918Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as reduction in parasitaemia at 30 mg/kg, perorally administered through 0.5% MCM/0.1%solutol HS15 formulation 24 hrs post infection for 3 days measure2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID10468Half-life following 10 mg/kg intravenous or 50 mg/kg oral dosing in rats was determined2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin.
AID21358Solubility in PBS AT pH 7.4 was determined after incubation at 25 degree C2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin.
AID1751427Recovery of fluconazole susceptibility against fluconazole-resistant Candida albicans CNL011 assessed as inhibition of fungal growth at 100 uM measured every 15 mins for 24 hrs by absorbance based analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID248433In vitro concentration of compound required to inhibit LPS-induced B cell proliferation to 50% in BALB/c mice2005Journal of medicinal chemistry, Jul-14, Volume: 48, Issue:14
Synthesis and immunosuppressive activity of new artemisinin derivatives. 1. [12(beta or alpha)-Dihydroartemisininoxy]phen(ox)yl aliphatic acids and esters.
AID158380In vitro antimalarial activity for Plasmodium falciparum W-21998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Synthesis and antimalarial activities of fluoroalkyl derivatives of dihydroartemisinin.
AID1304207Selectivity index, ratio of IC50 for human WI38 cells to IC50 chloroquine-sensitive asexual Plasmodium falciparum NF54 infected in human erythrocytes2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities.
AID481434Cytotoxicity against HFF after 5 days by Cell titer glo assay2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Thiazole, oxadiazole, and carboxamide derivatives of artemisinin are highly selective and potent inhibitors of Toxoplasma gondii.
AID560760Stability of compound in presence water assessed as pseudo-first order degradation rate constant at 10 uM at 20degC over 24 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Stability of peroxide antimalarials in the presence of human hemoglobin.
AID443094Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 (Thailand) assessed as growth inhibition by [3H]hypoxanthine incorporation assay relative to artemisinin2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Modular synthesis and in vitro and in vivo antimalarial assessment of C-10 pyrrole mannich base derivatives of artemisinin.
AID443011Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as growth inhibition by [3H]hypoxanthine incorporation assay2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Modular synthesis and in vitro and in vivo antimalarial assessment of C-10 pyrrole mannich base derivatives of artemisinin.
AID366935Antiplasmodial activity as reduced parasitaemia in Plasmodium berghei ANKA infected BALB/c mice (Mus musculus) at 144 mg/kg peroral dose2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1348370Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O-positive erythrocytes assessed as decrease in parasitaemia after 72 hrs by NBT dye-based spectrophotometric method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID1751439Potentiation of fluconazole-induced antifungal activity against Saccharomyces cerevisiae BY4742 assessed as inhibition of fungal growth at 100 uM measured after 24 hrs in presence of fluconazole by absorbance based analysis relative to fluconazole-treated2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1751447Antifungal activity against Saccharomyces cerevisiae harboring pdr5 delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1546462Cytotoxicity against human PG100 cells assessed as cell viability at 955.2 ug/mL after 24 hrs by MTT assay relative to control2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Artemisia: a promising plant for the treatment of cancer.
AID21490Solubility in iv formulation was determined after incubation at 25 degree C2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin.
AID663124Antimalarial activity against Plasmodium berghei NS infected in po dosed CD1 mouse assessed as decrease in parasitemia measured on day 42012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification, design and biological evaluation of heterocyclic quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).
AID729111Antimalarial activity against Plasmodium berghei ANKA infected in C57BL/6J mouse assessed as average survival time at 6 mg/kg, po in presence of lumefantrine (Rvb = 8.8 days)2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and antimalarial efficacy of two-carbon-linked, artemisinin-derived trioxane dimers in combination with known antimalarial drugs.
AID276158Antimalarial activity against Plasmodium falciparum K12006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine.
AID158855Inhibitory concentration against Plasmodium falciparum D6 (Sierra Leone)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Arteether, a new antimalarial drug: synthesis and antimalarial properties.
AID772516Antimalarial activity against mature gametocytic stage of Plasmodium falciparum assessed as inhibition of mature gamete exflagellation at 10 uM incubated for 24 hrs prior to exflagellation induction at 21 degC measured after 20 mins by microscopic analysi2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Using genetic methods to define the targets of compounds with antimalarial activity.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID251234Survival of mice to 30-day postinfection with Plasmodium berghei upon 100 mg/kg peroral dose was determined2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID112571In vivo antimalarial activity against Plasmodium berghei. Activity expressed as ED90.1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Structure-activity relationships of lactone ring-opened analogs of the antimalarial 1,2,4-trioxane artemisinin.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1698022Antileishmanial activity against Leishmania major IR-173 promastigotes assessed as inhibition of parasite growth incubated for 72 hrs by resazurin dye based assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes.
AID158700In vitro inhibitory concentration against chloroquine-resistant Plasmodium falciparum K12002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Mechanism-based design of parasite-targeted artemisinin derivatives: synthesis and antimalarial activity of new diamine containing analogues.
AID510921Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as survival at 30 mg/kg, perorally administered through 0.5% MCM/0.1%solutol HS15 formulation 24 hrs post infection for 3 days measured 96 hrs post inf2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID348882Antimalarial activity against Plasmodium falciparum 3D7 infected human erythrocytes after 24 hrs by [3H]hypoxanthine uptake2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Piperidine dispiro-1,2,4-trioxane analogues.
AID729110Antimalarial activity against Plasmodium berghei ANKA infected in C57BL/6J mouse assessed as suppression of blood parasitemia level at 6 mg/kg, po measured on day 3 relative to vehicle-treated control in presence of mef-HCl2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and antimalarial efficacy of two-carbon-linked, artemisinin-derived trioxane dimers in combination with known antimalarial drugs.
AID1751453Antifungal activity against Saccharomyces cerevisiae harboring vmr1 delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID366929Antiplasmodial activity as survival in Plasmodium berghei ANKA infected BALB/c mice (Mus musculus) at 54 mg/kg peroral dose2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells.
AID1751433Potentiation of fluconazole-induced antifungal activity against Candida auris NL002 assessed as fungal growth at 100 uM measured after 24 hrs in presence of fluconazole by absorbance based analysis relative to vehicle-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID132761In vivo antimalarial activity against Plasmodium berghei2001Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1
Synthesis, antimalarial activity, biomimetic iron(II) chemistry, and in vivo metabolism of novel, potent C-10-phenoxy derivatives of dihydroartemisinin.
AID1698021Antileishmanial activity against Leishmania donovani 9515 promastigotes assessed as inhibition of parasite growth incubated for 72 hrs by resazurin dye based assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes.
AID236182Plasma clearance after intravenous administration of 10 mg/kg2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID1751441Potentiation of fluconazole-induced antifungal activity against Cryptococcus neoformans H99 assessed as inhibition of fungal growth at 0.2 uM measured every 15 mins for 24 hrs in presence of fluconazole by absorbance based analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID562277Antiparasitic activity against Schistosoma mansoni assessed as parasite death at 300 ug/ml2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of trioxaquines against Schistosoma mansoni.
AID1327388Thermal stability of the compound assessed as melting point by thermogravimetric analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID11005350% effective dose for antimalarial activity (in vivo) against Plasmodium berghei2002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Mechanism-based design of parasite-targeted artemisinin derivatives: synthesis and antimalarial activity of new diamine containing analogues.
AID1751451Antifungal activity against Saccharomyces cerevisiae harboring pdr15 delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID729109Antimalarial activity against Plasmodium berghei ANKA infected in C57BL/6J mouse assessed as suppression of blood parasitemia level at 6 mg/kg, po measured on day 3 relative to vehicle-treated control in presence of mefloquine2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and antimalarial efficacy of two-carbon-linked, artemisinin-derived trioxane dimers in combination with known antimalarial drugs.
AID510919Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as reduction in parasitaemia at 50 mg/kg, perorally administered through 0.5% MCM/0.1%solutol HS15 formulation 24 hrs post infection for 3 days measure2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID1440393Antibiofilm activity against Candida albicans SC5314 after 24 hrs in presence of miconazole by Cell-Titer Blue assay2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Tackling Fungal Resistance by Biofilm Inhibitors.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID520094Induction of heme alkylation of Fe(II) heme assessed as adduct A472 absorbance change at completion of reaction at 10 uM in presence of 50% ACN-H2O with excess sodium dithionite under argon at 20 degC by spectrophotometry2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Relationship between antimalarial activity and heme alkylation for spiro- and dispiro-1,2,4-trioxolane antimalarials.
AID1751428Recovery of fluconazole susceptibility against fluconazole-resistant Candida albicans CNL012 assessed as inhibition of fungal growth at 100 uM measured every 15 mins for 24 hrs by absorbance based analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID247107Effective dose required to reduce the parasitemia in mice by suppressive test after 4 day postinfection2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1751460Potentiation of fluconazole-induced antifungal activity against Saccharomyces cerevisiae YNL033 overexpressing PDR5 assessed as fungal growth at 100 uM measured after 24 hrs by absorbance based analysis relative to fluconazole-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID443012Cytotoxicity against human KB cells after 72 hrs by alamar blue assay2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Modular synthesis and in vitro and in vivo antimalarial assessment of C-10 pyrrole mannich base derivatives of artemisinin.
AID443095Antimalarial activity against Plasmodium berghei ANKA infected Swiss CD1 mice (Mus musculus) assessed as reduction of parasitemia at 30 mg/kg, perorally administered after 3 hrs of infection for 3 days measured on day 4 relative to control2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Modular synthesis and in vitro and in vivo antimalarial assessment of C-10 pyrrole mannich base derivatives of artemisinin.
AID158199In vitro antimalarial activity against chloroquine-resistant Plasmodium falciparum K12001Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1
Synthesis, antimalarial activity, biomimetic iron(II) chemistry, and in vivo metabolism of novel, potent C-10-phenoxy derivatives of dihydroartemisinin.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID729115Antimalarial activity against Plasmodium berghei ANKA infected in C57BL/6J mouse assessed as average survival time at 6 mg/kg, po in presence of Mef-HCl (Rvb = 7.3 days)2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and antimalarial efficacy of two-carbon-linked, artemisinin-derived trioxane dimers in combination with known antimalarial drugs.
AID237221Plasma half life period after intravenous administration ( 10 mg/kg )2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID366930Antiplasmodial activity as survival in Plasmodium berghei ANKA infected BALB/c mice (Mus musculus) at 72 mg/kg peroral dose2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells.
AID510910Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as reduction in parasitaemia at 30 mg/kg, perorally administered as single dose 24 hrs post infection for 1 day measured 72 hrs post infection2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID443015Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 (Thailand) assessed as growth inhibition by [3H]hypoxanthine incorporation assay2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Modular synthesis and in vitro and in vivo antimalarial assessment of C-10 pyrrole mannich base derivatives of artemisinin.
AID131169Compound was tested in vivo for antimalarial activity against Plasmodium berghei in the mice (Mus musculus) model.1999Journal of medicinal chemistry, Dec-30, Volume: 42, Issue:26
Novel, potent, semisynthetic antimalarial carba analogues of the first-generation 1,2,4-trioxane artemether.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1348371Cytotoxicity against human MRC5 SV2 cells assessed as decrease in cell viability after 72 hrs by resazurin dye-based fluorometric method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID112564In vivo antimalarial activity in mice (Mus musculus) against chloroquine-sensitive Plasmodium berghei N after subcutaneous administration2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides.
AID662967Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by MSF assay2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Coumarin-trioxane hybrids: synthesis and evaluation as a new class of antimalarial scaffolds.
AID1751425Antifungal activity against fluconazole-resistant Candida albicans CNL011 assessed as fungal growth at 100 uM measured after 24 hrs by absorbance based analysis relative to vehicle-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID158699In vitro inhibitory concentration against chloroquine-resistant Plasmodium falciparum K12002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Mechanism-based design of parasite-targeted artemisinin derivatives: synthesis and antimalarial activity of new diamine containing analogues.
AID366931Antiplasmodial activity as survival in Plasmodium berghei ANKA infected BALB/c mice (Mus musculus) at 144 mg/kg peroral dose2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells.
AID1304205Resistance index, ratio of IC50 for multi-drug-resistant Plasmodium falciparum W2 infected in human erythrocytes to IC50 for chloroquine-sensitive asexual Plasmodium falciparum NF54 infected in human erythrocytes2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities.
AID1500572Antiplasmodial activity against Plasmodium yoelii N67 infected in Swiss mouse assessed as parasitaemia in blood at 5 mg/kg, ip qd for 4 consecutive days measured on day 4 post last dose by Giemsa staining based light microscopic method (Rvb = 9.8 to 16.6%
AID158863Intrinsic equimolar activity against Plasmodium falciparum W2 Indochina relative to QHS1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Arteether, a new antimalarial drug: synthesis and antimalarial properties.
AID236027Oral bioavailability (dose 50 mg/kg)2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID366934Antiplasmodial activity as reduced parasitaemia in Plasmodium berghei ANKA infected BALB/c mice (Mus musculus) at 72 mg/kg peroral dose2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells.
AID1751459Potentiation of fluconazole-induced antifungal activity against Saccharomyces cerevisiae BY4741 assessed as fungal growth at 100 uM measured after 24 hrs by absorbance based analysis relative to fluconazole-treated control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID753933Cytotoxicity against PHA-stimulated human PBMC cells after 48 hrs by Alamar Blue assay2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
Artemisinin-derived dimer phosphate esters as potent anti-cytomegalovirus (anti-CMV) and anti-cancer agents: a structure-activity study.
AID497985AUC (0-infinity) in Ugandan children patient with uncomplicated malaria assessed as dihydroartemisin administered twice daily for 3 days as 20/120 mg tablets containing artemether-lumefantrine combination2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID1751452Antifungal activity against Saccharomyces cerevisiae harboring snq2 delta mutant assessed as fungal growth at 1600 uM measured after 24 hrs by absorbance based analysis relative to control2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Evaluation of artemisinin derivative artemether as a fluconazole potentiator through inhibition of Pdr5.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (995)

TimeframeStudies, This Drug (%)All Drugs %
pre-199050 (5.03)18.7374
1990's160 (16.08)18.2507
2000's299 (30.05)29.6817
2010's309 (31.06)24.3611
2020's177 (17.79)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 73.71

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index73.71 (24.57)
Research Supply Index7.16 (2.92)
Research Growth Index5.06 (4.65)
Search Engine Demand Index129.85 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (73.71)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials237 (22.57%)5.53%
Reviews88 (8.38%)6.00%
Case Studies49 (4.67%)4.05%
Observational4 (0.38%)0.25%
Other672 (64.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (163)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Multicentre Randomised Comparative Clinical Trial of the Efficacy of Artesunate + Amodiaquine Versus Artemether-lumefantrine (Coartem®) for the Treatment of Uncomplicated Childhood Plasmodium Falciparum Malaria in Zanzibar [NCT03768908]Phase 4359 participants (Actual)Interventional2005-01-05Completed
Surveillance for the Effectiveness and Safety of Artemether-lumefantrine in Pediatric and Adult Patients With Malaria [NCT01228344]324 participants (Actual)Observational2010-05-01Completed
Effectiveness and Safety Evaluation of the Riamet® Versus Malarone® in the Treatment of Uncomplicated Malaria : a Multicentric Study [NCT01150344]Phase 4317 participants (Actual)Interventional2010-07-31Completed
A Phase 2, Multi-center, Randomized, Open-label, Dose-escalation Study to Determine Safety of Single (QD) and Multiple (3 QD) Doses of KAE609, Given to Adults With Uncomplicated Plasmodium Falciparum Malaria. [NCT03334747]Phase 2188 participants (Actual)Interventional2017-11-16Completed
Artemether-lumefantrine vs Chloroquine in Patients With Acute Non-severe P. Vivax Malaria in Sabah, Malaysia [NCT02348788]Phase 398 participants (Anticipated)Interventional2015-01-31Recruiting
Efficacy and Safety of a Single Low-dose Primaquine Added to Standard Artemether-lumefantrine Treatment for the Clearance of Plasmodium Falciparum Gametocytes. [NCT02090036]Phase 4220 participants (Actual)Interventional2014-07-31Completed
A Four-arm Trial Comparing Artemether-lumefantrine With or Without Single-dose Primaquine and Sulphadoxine-pyrimethamine/Amodiaquine With or Without Single-dose Tafenoquine to Reduce P. Falciparum Transmission in Mali [NCT05081089]Phase 280 participants (Actual)Interventional2021-10-12Completed
Host and Parasites Factors Contributing to Risk of Plasmodium Re-infection and Morbidity in Elementary School Children in Maprik, East Sepik Province [NCT02143934]Phase 4524 participants (Actual)Interventional2009-08-31Completed
A Randomized Clinical Trial to Measure the Impact of Retreatment With an Artemisinin-based Combination on Malaria Incidence and Its Potential Selection of Resistant Strains [NCT01374581]Phase 32,117 participants (Actual)Interventional2012-05-31Completed
Efficacy and Safety of Artemether-lumefantrine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in the Philippines in 2017-2018 [NCT05958810]80 participants (Actual)Observational2017-01-02Completed
Optimizing the Dose of Tafenoquine for the Radical Cure of Plasmodium Vivax Malaria in Southeast Asia [NCT04704999]Phase 4700 participants (Anticipated)Interventional2023-09-18Not yet recruiting
Evaluation of the Safety of Primaquine in Combination With Artemether-lumefantrine in Glucose-6-phosphate Dehydrogynase Deficient Males With an Asymptomatic Malaria Infection in Burkina Faso (SAFEPRIM) [NCT02174900]Phase 2/Phase 370 participants (Actual)Interventional2014-10-31Completed
Clinical Efficacy of Artemisinin-based Combination Therapy for Treatment of Uncomplicated Plasmodium Falciparum Malaria in North Sumatera, Indonesia and the Association of Molecular Markers With Treatment Outcomes [NCT02325180]Phase 4338 participants (Actual)Interventional2015-01-31Completed
An Open-label Randomised Trial to Assess the Therapeutic Efficacy and Tolerability of Arterolane-piperaquine Plus Single Low Dose Primaquine Versus Arterolane-piperaquine Plus Mefloquine and Single Low Dose Primaquine Versus Artemether-lumefantrine Plus S [NCT03452475]Phase 3219 participants (Actual)Interventional2018-03-07Completed
A Randomised, Open-label Non-inferiority Trial of Artemether-lumefantrine Versus Quinine for the Treatment of Uncomplicated Falciparum Malaria During Pregnancy, Mbarara, Uganda (2006-2007) [NCT00495508]Phase 4300 participants (Actual)Interventional2006-10-31Completed
Efficacy of Antimalarial Drugs Used for the Treatment of Uncomplicated Malaria, Plasmodium Falciparum, at the Agadez, Gaya and Tessaoua Sentinel Sites [NCT05070520]Phase 4259 participants (Actual)Interventional2020-09-01Completed
Treatment Outcomes for Non-malarial Febrile Illness in Children Aged 6-59 Months in Areas of Perennial Malaria Transmission [NCT01043744]1,000 participants (Actual)Interventional2010-01-31Completed
Evaluation of the Efficacy of Artemether-lumefantrine and Dihydroartemisinin-piperaquine in Children With Uncomplicated Clinical Malaria in Rural Rwanda [NCT04767217]Phase 4528 participants (Anticipated)Interventional2021-06-14Recruiting
Safety and Feasibility of a Malaria Transmission Model in Semi-immune Kenyan Adults Using Plasmodium Falciparum Sporozoites [NCT04280692]Phase 1/Phase 244 participants (Actual)Interventional2022-08-22Active, not recruiting
A Phase 1/2a Study of LON002 (Sublingual Artemether Spray) in Subjects With Advanced Solid Tumours. [NCT02263950]Phase 1/Phase 287 participants (Anticipated)Interventional2014-10-31Recruiting
A Double Blind Randomized Controlled Trial of Artemether-Lumefantrine Alone and in Combination With Ivermectin to Reduce Post-Treatment Malaria Transmission [NCT01603251]Phase 1/Phase 2120 participants (Actual)Interventional2013-01-31Completed
Phase I, Randomized, Parallel Group Study to Evaluate the Effect of Multiple Oral Doses of Eurartesim on the QT/QTc Interval Compared to Riamet, Placebo and Moxifloxacin in Healthy Male and Female Volunteers [NCT01103830]Phase 1287 participants (Actual)Interventional2010-02-28Completed
Phase 2/3, Open-Label, Comparative Trial Of Azithromycin Plus Chloroquine Versus Artemether-Lumefantrine For The Treatment Of Uncomplicated Plasmodium Falciparum Malaria In Children In Africa [NCT00677833]Phase 2/Phase 3361 participants (Actual)Interventional2008-06-30Completed
Impact Tanzania in Vivo Efficacy 2010: Assessing the Efficacy of Artemisinin Combination Therapies for Treatment of Uncomplicated Malaria Infection in Children Aged 6-59 Months [NCT01082705]Phase 3323 participants (Actual)Interventional2010-04-30Completed
A Multi-center, Open-label, Randomized Trial of Chloroquine, Artemether-Lumefantrine, and Mefloquine-Artesunate for the Treatment of Uncomplicated P. Vivax Malaria in Pregnant Women in Brazil [NCT01107145]Phase 416 participants (Actual)Interventional2011-02-28Terminated(stopped due to Extremely slow enrollment)
An Adaptive, Randomized, Active-controlled, Open-label, Sequential Cohort, Multicenter Study to Evaluate the Efficacy, Safety, Tolerability and Pharmacokinetics of Intravenous Cipargamin (KAE609) in Adult and Pediatric Participants With Severe Plasmodium [NCT04675931]Phase 2252 participants (Anticipated)Interventional2022-03-07Recruiting
Antioxidant Micronutrients in Malaria:a Randomised Clinical Trial [NCT01152931]Phase 310 participants (Actual)Interventional2010-08-31Completed
Randomized Study of the Tolerability and Efficacy of Artemether-Lumefantrine Versus Artesunate Plus Amodiaquine Coadministered for the Treatment of Uncomplicated Falciparum Malaria in Zanzibar [NCT03764527]Phase 4408 participants (Actual)Interventional2002-11-01Completed
Assessing the Effectiveness of Targeted Active Case Detection Among High Risk Populations in Southern Lao PDR [NCT03783299]Phase 439,968 participants (Actual)Interventional2017-11-28Completed
A Cluster Randomized, Single-centre, Controlled, Parallel,12-month Prospective Study and Additional 12-month Follow-up in Africa of Malaria Incidence in a Community Setting Following Systematic Treatment of P. Falciparum Asymptomatic Carriers With Artemet [NCT01256658]Phase 414,075 participants (Actual)Interventional2010-11-30Completed
Open Label, Multicenter Study for Evaluation of Safety and Efficacy of Artemether-Lumefantrine Tablets (6-Dose Regimen) in African Infants and Children in the Treatment of Acute Uncomplicated Falciparum Malaria [NCT00709969]Phase 3310 participants (Actual)Interventional2002-07-31Completed
Efficacy and Safety of Artemether-Lumefantrine and Dihydroartemisinin-Piperaquine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria Among Children in the North Region of Cameroon [NCT05340153]Phase 4184 participants (Anticipated)Interventional2022-04-11Not yet recruiting
Assessment of Use of Rapid Diagnostic Testing in the Context of Home Management With ACTs [NCT00720811]6,456 participants (Actual)Interventional2009-10-31Completed
Evaluation of the Effect of Artemisinin-based Combination Therapies on Urinary Schistosoma Haematobium When Administered for the Treatment of Malaria Co-infection [NCT04264130]Phase 254 participants (Actual)Interventional2018-07-31Completed
In Vivo and in Vitro Efficacy of the Recommended First Line Antimalarial Treatments (Artemether-Lumefantrine and Amodiaquine-Artesunate) in Children With Uncomplicated Malaria in Burkina Faso [NCT00808951]Phase 4440 participants (Actual)Interventional2008-12-31Completed
Safety and Protective Efficacy of Chemoprophylaxis and Sporozoite Immunization With Plasmodium Falciparum NF135 Against Homologous and Heterologous Challenge Infection in Healthy Volunteers in the Netherlands [NCT03813108]43 participants (Actual)Interventional2019-04-01Terminated(stopped due to Subject withdrawals after temporal suspension of the trial (for personal, logistic reasons). At time of reinitiation the number of enrolled subjects did not meet the predefined threshold for continuation of the trial.)
[NCT00868465]600 participants (Anticipated)Interventional2009-04-30Completed
Efficacy and Safety of Artesunate-amodiaquine and Artemether-lumefantrine in the Treatment of Uncomplicated Plasmodium Falciparum Malaria in the Democratic Republic of the Congo: a Randomized Controlled Trial (TES2022) [NCT06076213]Phase 41,408 participants (Anticipated)Interventional2023-05-01Recruiting
Pharmacokinetics of Drugs Used to Treat Uncomplicated Malaria in Breastfeeding Mother-infant Pairs: An Observational Pharmacokinetic Study [NCT05676645]30 participants (Anticipated)Observational2023-03-20Recruiting
A Five-arm Trial Comparing Artesunate-amodiaquine and Artemether-lumefantrine-amodiaquine With or Without Single-dose Primaquine to Reduce P. Falciparum Transmission in Mali [NCT05550909]Phase 2100 participants (Actual)Interventional2022-10-17Completed
Open Label Randomized Study Evaluating the in Vivo Efficacies of Artemether-lumefantrine and Dihydroartemisinin-piperaquine in the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Children Under Five Years of Age in Western Kenya [NCT05060198]340 participants (Actual)Interventional2016-06-17Completed
Improving Neonatal Health Through Rapid Malaria Testing in Early Pregnancy With High-Sensitivity [NCT05757167]Phase 42,500 participants (Anticipated)Interventional2023-11-06Recruiting
Evaluation of Dolutegravir Interactions With Artemether-Lumefantrine and Amodiaquine-Artesunate [NCT02242799]Phase 146 participants (Actual)Interventional2015-06-30Completed
Efficacy of Artemether/Lumefantrine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Children Five Years After Wide Scale Use of the Drug in Tanzania. [NCT02089841]Phase 4140 participants (Actual)Interventional2012-05-31Completed
In Vivo Efficacy of Artemether-lumefantrine and Amodiaquine-artesunate for the Treatment of Uncomplicated Falciparum Malaria in Children: A Multisite, Open-label, Two-cohort Clinical Trial in Mozambique. [NCT02168569]Phase 4700 participants (Actual)Interventional2011-06-30Completed
A Five-cohort, Randomized, Open-label, Parallel-group Study to Evaluate the Pharmacokinetics of a Single Dose of Tafenoquine (SB252263) 300mg When Co-administered With the Artemisinin-based Combination Therapies (ACT) Artemether + Lumefantrine (AL) and Di [NCT02184637]Phase 1120 participants (Actual)Interventional2014-07-31Completed
Efficacy and Safety of Artemether Lumefantrine Combination Therapy for the Treatment of Malaria Due to Plasmodium Ovale, Plasmodium Malariae, and Mixed Plasmodium Infections in Gabon [NCT00725777]40 participants (Actual)Interventional2008-07-31Completed
A Multi-center, Open-label, Randomized, Phase 4, Trial of Artemether-Lumefantrine and Mefloquine-Artesunate for the Treatment of Uncomplicated P. Falciparum Malaria Parasitemia in Pregnant Women in Brazil [NCT01082731]Phase 46 participants (Actual)Interventional2010-11-30Terminated(stopped due to Extremely slow enrollment)
An Open-label, Randomized, Single-center, Parallel Group Study of the Effects of Artemether-lumefantrine (Coartem®) Atovaquone-proguanil (Malarone®) and Artesunate-mefloquine on Auditory Function Following the Treatment of Acute Uncomplicated Plasmodium F [NCT00444106]Phase 4265 participants (Actual)Interventional2007-05-31Completed
Extended Duration Artemether-lumefantrine Treatment for Malaria in Children [NCT03453840]Phase 4305 participants (Actual)Interventional2018-02-19Completed
Ethiopia In-vivo Efficacy Study 2009: Evaluating the Efficacy of Artemether-lumefantrine for the Treatment of Uncomplicated Plasmodium Falciparum Infection and Either Artemether-lumefantrine or Chloroquine for P. Vivax Infection [NCT01052584]354 participants (Actual)Interventional2009-10-31Completed
A Multi-site Cohort Observational Study for Molecular Assessment of Artemisinin Resistance Falciparum Malaria in Myanmar [NCT02792816]550 participants (Actual)Observational2009-06-30Completed
Targeting Malaria High-risk Populations With Tailored Intervention Packages: A Study to Assess Feasibility and Effectiveness in Northern Namibia [NCT04094727]Phase 43,302 participants (Actual)Interventional2019-10-31Completed
A Randomized, Open-Label Study to Evaluate Potential Pharmacokinetic Interactions of Orally Administered Artemether-lumefantrine, Amodiaquine and Primaquine in Healthy Adult Subjects [NCT02696954]Phase 1/Phase 217 participants (Actual)Interventional2016-11-18Terminated
In Vivo Efficacy of Artesunate-amodiaquine and Artemether-lumefantrine for the Treatment of Uncomplicated Falciparum Malaria: an Open-randomised, Non-inferiority Clinical Trial in South Kivu, DR Congo [NCT02741024]Phase 4288 participants (Actual)Interventional2013-10-31Completed
Pharmacokinetic Interaction Between Coartem® and Either Nevirapine, Efavirenz or Rifampicin in HIV Positive Ugandan Patients [NCT00620438]Phase 490 participants (Anticipated)Interventional2008-02-29Active, not recruiting
Evaluation of the Effect of Targeted Mass Drug Administration and Reactive Case Detection on Malaria Transmission and Elimination in East Hararghe Zone, Oromia, Ethiopia [NCT04241705]48,960 participants (Anticipated)Interventional2020-01-20Recruiting
Study of Therapeutic Efficacy, Safety and Pharmacokinetic Interactions Between Artemether-lumefantrine and Nevirapine-based Antiretrovirals in HIV-infected Patients With Uncomplicated Falciparum-malaria in Muheza, Northeastern Tanzania [NCT00885287]Phase 4830 participants (Actual)Interventional2009-07-31Completed
A Pilot, Double-blind, Randomized, Parallel-group, Placebo-controlled, Exploratory Study to Assess the Safety and Efficacy of 5-aminolevulinic Acid Hydrochloride (5-ALA HCl) and Sodium Ferrous Citrate (SFC) Added on Artemisinin-based Combination Therapy ( [NCT04020653]Phase 20 participants (Actual)Interventional2019-09-06Withdrawn(stopped due to Considering the Thai FDA requirement, changes of Malaria cases in Thailand and EC recommendation, the decision to withdrawal the study was made.)
Programmatic Implementation of ACTs in Malawi: Safety and Effectiveness of Combination Therapies With Repeated Treatments for Uncomplicated P. Falciparum Malaria Over a Three-year Period [NCT01038063]Phase 41,200 participants (Anticipated)Interventional2010-10-31Recruiting
Artemether-lumefantrine Vs Co-formulated Amodiaquine + Artesunate for the Treatment of Uncomplicated Falciparum Malaria: a Randomized Open-label Trial to Evaluate the Effectiveness of the Burkina Faso New Drug Policy [NCT01017770]Phase 4340 participants (Anticipated)Interventional2008-09-30Completed
Effectiveness and Safety of Artemether + Lumefantrine and Dihydroartemisinin + Piperaquine for the Treatment of Uncomplicated Malaria in Guinea-Bissau [NCT04897919]Phase 4474 participants (Actual)Interventional2015-08-01Completed
A Randomized Trial of Azithromycin + Artesunate v Artemether-lumefantrine in Uncomplicated Malaria in Tanzanian Children. [NCT00694694]Phase 3261 participants (Actual)Interventional2008-06-30Completed
Pharmacokinetic Interactions Between Antiretroviral Agents, Lopinavir/Ritonavir and Efavirenz and Antimalarial Drug Combinations, Artesunate/Amodiaquine and Artemether/Lumefantrine. [NCT00697892]Phase 138 participants (Actual)Interventional2005-07-31Completed
Efficacy and Safety of Artemether-lumefantrine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in the Philippines in 2015 [NCT05958693]82 participants (Actual)Observational2015-01-05Completed
An Open-label, Randomised, Controlled, Non-inferiority Trial to Compare the Efficacy, Safety and Tolerability of a Fixed Dose Triple Artemisinin-based Combination Therapy (TACT) Artemether-lumefantrine-amodiaquine Versus First-line Artemisinin-based Combi [NCT05951595]Phase 31,440 participants (Anticipated)Interventional2024-01-01Not yet recruiting
Pharmacokinetic Interaction Between the Antimalarial Combination Artemether/Lumefantrine and Combination Antiretroviral Therapy Including Nevirapine in HIV-infected Adults [NCT00790881]Phase 436 participants (Anticipated)Interventional2008-10-31Completed
Safe and Efficacious Artemisinin-based Combination Treatments for African Pregnant Women With Malaria [NCT00852423]Phase 33,428 participants (Actual)Interventional2010-06-30Completed
A Multi-centre Randomised Controlled Non-inferiority Trial to Compare the Efficacy, Safety and Tolerability of Triple Artemisinin-based Combination Therapies Versus First-line ACTs + Placebo for the Treatment of Uncomplicated Plasmodium Falciparum Malaria [NCT03939104]Phase 31,368 participants (Anticipated)Interventional2021-06-30Recruiting
A Multi-centre Randomised Controlled Non-inferiority Trial to Compare the Efficacy, Safety and Tolerability of Triple Artemisinin-based Combination Therapies Versus First-line ACTs + Placebo for the Treatment of Uncomplicated Plasmodium Falciparum Malaria [NCT03923725]Phase 33,240 participants (Anticipated)Interventional2020-09-01Recruiting
Evaluation of 4 Artemisinin-based Combinations for Treating Uncomplicated Malaria in African Children [NCT00393679]Phase 34,112 participants (Actual)Interventional2007-07-31Completed
[NCT01075945]Phase 4140 participants (Anticipated)Interventional2010-02-28Recruiting
A Phase 1 Clinical Trial To Evaluate The Safety and Infectivity Of Direct Venus Inoculation of Aseptic, Purified, Cryopreserved Plasmodium Falciparum 7G8 And NF54 Challenge Strains (PfSPZ) in a Head-To-Head Comparative Study [NCT04203186]0 participants (Actual)Interventional2020-03-31Withdrawn(stopped due to Funding was lost due to the COVID19 Pandemic)
A Study to Assess Safety of Current Standard Malaria Treatment and an Assessment of Glucose-6-dehydrogenase Status in South-east Bangladesh [NCT02389374]Phase 4181 participants (Actual)Interventional2014-08-31Completed
Comparison of Lumefantrine Concentrations Measured in Venous Plasma Versus in Dried Capillary Blood Spot Samples in Healthy Volunteers. [NCT02742285]Phase 416 participants (Actual)Interventional2016-05-31Completed
In-vivo Efficacy and Safety of Artemether/Lumefantrine Vs Dihydroartemisinin-piperaquine for Treatment of Uncomplicated Malaria and Assessment of Parasite Genetic Factors Associated With Parasite Clearance or Treatment Failure [NCT02590627]Phase 4509 participants (Actual)Interventional2014-05-31Completed
An Open-label, Single-center Study of the Effects of Co-artemether, Atovaquone-proguanil, and Artesunate-mefloquine on Auditory Function Following the Treatment of Acute Uncomplicated Plasmodium Falciparum Malaria in Patients 12 Years of Age or Older. [NCT00386750]Phase 4265 participants Interventional2005-06-30Terminated
A Randomized Open-Label Trial of the Efficacy of Artemether-Lumefantrine Suspension Compared With Artemether-Lumefantrine Tablets for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Children Less Than Five Years in Western Kenya [NCT00529867]Phase 4267 participants (Actual)Interventional2007-05-31Completed
Interactions Between HIV and Malaria in African Children [NCT00527800]Phase 3351 participants (Actual)Interventional2007-08-31Completed
Optimizing Malaria Treatment for HIV-Malaria Co-Infected Individuals by Addressing Drug Interactions Between Artemether-Lumefantrine and Efavirenz; a Randomized Controlled Trial [NCT04708496]Phase 4888 participants (Anticipated)Interventional2021-01-18Recruiting
Effectiveness of Oral Quinine and Artemether-Lumefantrine in the Treatment of Uncomplicated Malaria in Ugandan Children [NCT00540202]Phase 4302 participants (Anticipated)Interventional2007-09-30Recruiting
A Phase III Comparative (Double-blind, Double-dummy) Randomised, Multi-centre Study to Assess the Efficacy of Pyronaridine Artesunate (180:60mg) Versus Coartem® (Artemether Lumefantrine) in Children & Adult Patients With Falciparum Malaria [NCT00422084]Phase 31,272 participants (Actual)Interventional2007-01-31Completed
Phase III Clinical Trials of Artemisinin-based Combination Therapy in Cameroon [NCT00297882]Phase 3816 participants (Actual)Interventional2006-07-31Completed
Efficacy and Safety of the Dispersible Formulation of Artemether-lumefantrine, Co-formulated Artesunate-amodiaquine and Co-formulated Dihydroartemisinin-piperaquine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Machinga District, Mal [NCT01326754]498 participants (Actual)Interventional2011-08-31Completed
A Phase I, Partially Randomized, Open Label, Two-way, Two Period Cross-over Study to Investigate the Pharmacokinetic Interaction Between Etravirine or Darunavir/Rtv and Artemether/Lumefantrine at Steady-state in Healthy HIV-negative Subjects [NCT01876966]Phase 133 participants (Actual)Interventional2011-03-31Completed
THE OPTIMAL TIMING OF PRIMAQUINE TO PREVENT MALARIA TRANSMISSION AFTER ARTEMISININ-COMBINATION THERAPY [NCT01906788]Phase 4250 participants (Anticipated)Interventional2013-05-31Recruiting
Comparison of Two Regimens of Artemether-lumefantrine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Pregnant Women in the Democratic Republic of Congo [NCT01916954]Phase 396 participants (Actual)Interventional2013-07-31Completed
A Double Blind Randomized Controlled Trial to Assess the Efficacy and Safety of Low Dose Primaquine for Clearance of Gametocytes in Asymptomatic Individuals Infected With P. Falciparum in Burkina Faso [NCT01935882]Phase 2/Phase 3360 participants (Actual)Interventional2013-09-30Completed
Treatment Efficacy and Malaria TRANSmission After Artemisinin Combination Therapy 2 (TRANSACT2) [NCT01939886]Phase 3219 participants (Actual)Interventional2013-04-30Completed
Community-based Scheduled Screening and Treatment of Malaria in Pregnancy for Improved Maternal and Infant Health: a Cluster-randomized Trial in The Gambia, Burkina Faso and Benin [NCT01941264]4,265 participants (Actual)Interventional2013-10-31Completed
Open-label, Multi-center, Non-comparative Efficacy, Safety, and Tolerability Study of Co-artemether in the Treatment of Acute Uncomplicated Malaria in Non-immune Patients [NCT00233337]Phase 40 participants Interventional2001-05-31Completed
Efficacy and Bio-availability of Artemether-Lumefantrine Fixed Combination in Severely Malnourished Children Compared to Non-severely Malnourished Children [NCT01958905]399 participants (Actual)Interventional2013-11-30Completed
Adherence to Artemisinin-Based Combination Therapy (ACT) for the Treatment of Malaria in Sierra Leone [NCT01967472]1,145 participants (Actual)Interventional2013-09-16Completed
In Vivo and In Vitro Efficacy of Artemisinin Combination Therapy in Kisumu County, Western Kenya [NCT01976780]Phase 4118 participants (Actual)Interventional2013-06-30Completed
Parasite Clearance Time and Time to Recurrent Infection Following Treatment With Artemether/Lumefantrine Among Children With Uncomplicated P. Falciparum Malaria Five Years After Wide Scale Use of the Drug in Tanzania [NCT01998295]Phase 445 participants (Actual)Interventional2012-05-31Completed
Artemether-lumefantrine vs Chloroquine in Patients With Acute Uncomplicated P. Knowlesi Malaria: a Randomized Open Label Trial in Sabah, Malaysia (CAN KNOW Trial) [NCT02001012]Phase 3123 participants (Actual)Interventional2014-01-31Completed
An Open-label Randomized Controlled Trial to Evaluate the Effectiveness and Safety of a 3 Day Versus 5 Day Course of Artemether-lumefantrine for the Treatment of Uncomplicated Falciparum Malaria in Myanmar [NCT02020330]Phase 3150 participants (Actual)Interventional2013-11-25Completed
A Randomized, Investigator-Blinded, Multicenter, Parallel-Group Study to Compare Efficacy, Safety and Tolerability of Arthemeter/ Lumefantrine Dispersible Tablet Formulation vs. Artemether/ Lumefantrine 6-Dose Crushed Tablet in the Treatment of Acute Unco [NCT00386763]Phase 3890 participants Interventional2006-08-31Completed
Monitoring the Effectiveness and Safety of Artesunate-Amodiaquine and Artemether-Lumefantrine During the Treatment of Uncomplicated Plasmodium Falciparum Malaria Among Children in Yaounde, Cameroon [NCT04565184]Phase 4242 participants (Actual)Interventional2019-05-09Completed
Impact of a School-based Programme of Malaria Diagnosis and Treatment on School Attendance in Southern Malawi [NCT02213211]3,667 participants (Actual)Interventional2014-04-30Completed
Efficacy of Chloroquine + Sulfadoxine Pyrimethamine Versus Artemether + Lumefantrine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in the Philippines [NCT00229775]560 participants (Actual)Interventional2003-07-31Completed
Pharmacokinetic Interaction Between the Antimalarial Combination Artemether/Lumefantrine and Combination Antiretroviral Therapy Including Lopinavir/Ritonavir in HIV-infected Adults [NCT00869700]Phase 418 participants (Actual)Interventional2009-06-30Completed
In Vivo Efficacy of Artemether-Lumefantrine and Artesunate-Amodiaquine for Uncomplicated Plasmodium Falciparum Malaria in Malawi, 2014 [NCT02637128]Phase 4452 participants (Actual)Interventional2014-03-31Completed
Multicenter, Open-label, Single-arm Study to Evaluate the PK, Safety, Tolerability and Efficacy of a New Artemether:Lumefantrine (2.5 mg:30 mg) Dispersible Tablet in the Treatment of Infants and Neonates <5 kg Body Weight With Acute Uncomplicated Plasmodi [NCT04300309]Phase 2/Phase 328 participants (Actual)Interventional2020-12-21Active, not recruiting
A Multi-centre, Randomised, Double-blind, Double Dummy Study Comparing the Efficacy and Safety of Chlorproguanil-dapsone-artesunate Versus Artemether-lumefantrine in the Treatment of Acute Uncomplicated Plasmodium Falciparum Malaria in Children and Adoles [NCT00344006]Phase 31,395 participants (Actual)Interventional2006-06-30Completed
Effectiveness of Artemether-Lumefantrine Treatment Provided by Community Health Worker Against Uncomplicated Malaria in Children Under 5 Years of Age in Tanzania [NCT00454961]Phase 4200 participants (Anticipated)Interventional2007-04-30Completed
Malaria as a Risk Factor for COVID-19 in Western Kenya and Burkina Faso [NCT04695197]Phase 3142 participants (Anticipated)Interventional2021-01-08Recruiting
An Individually Randomised Trial of Seasonal Malaria Chemoprevention Versus a Long-acting Artemisinin Combination Therapy for the Prevention of Malaria and Anaemia in Children Living in an Area of Extended Seasonal Transmission in Ghana. [NCT01651416]Phase 42,400 participants (Actual)Interventional2012-07-31Completed
Longitudinal Comparison of Combination Antimalarial Therapies in Ugandan Children: Evaluation of Safety, Tolerability, and Efficacy [NCT00123552]Phase 3601 participants (Actual)Interventional2004-11-30Completed
Characterization of Novel Molecular Tools for the Epidemiological Surveillance of Antimalarial Drug Resistance in Mali [NCT00127998]1,011 participants Interventional2005-07-31Completed
Chloroquine and Coartem for Treatment of Symptomatic Children With Plasmodium Falciparum in Guinea Bissau. [NCT00426439]Phase 4300 participants (Anticipated)Interventional2006-12-31Completed
Sulfadoxine-Pyrimethamine Versus Artemether-Lumefantrine Versus Amodiaquine-Artesunate Coformulation in Uncomplicated Plasmodium Falciparum Malaria : an Open Randomized Study [NCT00460369]240 participants (Actual)Interventional2007-04-30Completed
Randomized Trial of the Safety and Effectiveness of Lapdap and Coartemether for Uncomplicated Malaria in Operational Settings [NCT00118794]Phase 31,200 participants Interventional2004-09-30Completed
Assessing and Monitoring the Efficacy of Sulfadoxine/ Pyrimethamine (SP) and the Combination of SP Plus Artesunate for Uncomplicated Malaria Infections Among Children [NCT00140361]Phase 4390 participants (Actual)Interventional2000-01-31Completed
[NCT00406146]Phase 30 participants Interventional2004-10-31Active, not recruiting
Can Triple Artemisinin-based Combination Therapy for Treatment of Uncomplicated Plasmodium Falciparum Malaria, Delay Drug Resistance Development of Plasmodium Falciparum in Tanzania: a Randomized Three Arm Clinical Trial [NCT05764746]Phase 2/Phase 3384 participants (Anticipated)Interventional2023-04-01Not yet recruiting
Assessment of Adherence to a 6-Dose Regimen of Coartem for Treatment of Uncomplicated Malaria in Children Under 5 Years in Tanzania [NCT00153491]300 participants Observational2002-08-31Completed
Open Label Study to Evaluate Combination Anti-malarial Therapy,in Terms of Efficacy, Prevalence of Gametocyte Carriage and Molecular Markers Associated With Sulfadoxine Pyrimethamine Resistance in Uncomplicated Plasmodium Falciparum [NCT00203801]700 participants Interventional2002-01-31Completed
Efficacy and Safety of Artesunate-amodiaquine, Artemether-lumefantrine and Dihydroartemisinine-piperaquine in the Treatment of Uncomplicated Plasmodium Falciparum Malaria in the Democratic Republic of Congo: a Randomized Controlled Trial [NCT02940756]Phase 41,615 participants (Actual)Interventional2017-03-15Completed
Efficacy and Safety of Artesunate-amodiaquine (ASAQ) and Artemether-lumefantrine (AL) for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in the Center Region of Cameroon [NCT04829695]Phase 4184 participants (Anticipated)Interventional2021-04-05Not yet recruiting
An Open Randomised Trial of the Efficacy of Sulfadoxine-Pyrimethamine (SP), Amodiaquine + SP (AQ-SP), AQ + Artesunate (AQ-Art), Chlorproguanil-Dapsone + Art (CD-Art), and Lumefantrine-Artemether (LA) for Uncomplicated Malaria in Malawi [NCT00164710]Phase 4365 participants Interventional2005-04-30Completed
Pharmacology of Artemisinin-Based Antimalarial Therapy Within the Context of Antiretroviral Therapy [NCT01728961]Phase 419 participants (Anticipated)Interventional2012-02-29Terminated(stopped due to Slow accrual and funding limitations.)
Pharmacokinetic Interactions Between Antiretroviral Agents, Lopinavir/Ritonavir and Efavirenz and Antimalarial Drug Combination, Artemether/Lumefantrine [NCT00266058]Phase 133 participants (Actual)Interventional2005-12-31Completed
Effect of Atazanavir-ritonavir on the Pharmacokinetics and Toxicity of Lumefantrine in People Living With HIV Attending Lagos University Teaching Hospital [NCT04531072]Phase 420 participants (Actual)Interventional2018-09-18Completed
Ethiopia Antimalarial in Vivo Efficacy Study 2012: Evaluating the Efficacy of Artemether-lumefantrine Alone Compared to Artemether-lumefantrine Plus Primaquine and Chloroquine Alone Compared to Chloroquine Plus Primaquine for Plasmodium Vivax Infection [NCT01680406]Phase 4398 participants (Actual)Interventional2012-10-31Completed
Comparative Evaluation of the Safety and the Efficacy of Artemether + Lumefantrine (Coartem™) vs. Sulfadoxine + Pyrimethamine (SP) in Both HIV+ and HIV- Adults With Uncomplicated P. Falciparum Malaria in Zambia [NCT00304980]3,000 participants Interventional2003-03-31Terminated
[NCT00451139]Phase 40 participants InterventionalCompleted
Treatment of Uncomplicated Childhood Malaria by an Artemisinin Derivative in Combination With Lumefantrine. Efficacy, Safety and Genotyping. [NCT00336375]Phase 450 participants (Actual)Interventional2006-06-30Completed
Artemether/Lumefantrine in the Treatment of Plasmodium Vivax Malaria in Eastern Sudan [NCT01625871]Phase 338 participants (Actual)Interventional2011-09-30Completed
Efficacy of Amodiaquine-Artesunate (ASAQ) and Artemether-Lumefantrine (AL) for the Treatment of Uncomplicated Falciparum Malaria in Nanoro, Burkina Faso [NCT01697787]Phase 4150 participants (Actual)Interventional2012-10-31Completed
Efficacy and Safety of Artemether + Lumefantrine and Dihydroartemisinin + Piperaquine for the Treatment of Uncomplicated Malaria in Guinea-Bissau. [NCT01704508]Phase 4346 participants (Actual)Interventional2012-11-30Completed
Efficacy of Artesunate-amodiaquine, Dihydroartemisinin-piperaquine and Artemether-lumefantrine Combination Therapies for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Children Aged 6 to 59 Months in Maradi, Niger 2012-13 [NCT01755559]Phase 4663 participants (Actual)Interventional2013-06-30Completed
Field Study of the Pharmacokinetics and Pharmacodynamics of Artemisinin-based Combination Therapy for Gametocyte Clearance and Post-treatment Chemoprotection in Zambian Children With Uncomplicated Falciparum Malaria [NCT04009343]Phase 2/Phase 3182 participants (Anticipated)Interventional2019-06-19Active, not recruiting
Phase III Study to Study the Clinical Response to ACT Fixed Dose Combination in 42 Days in Uncomplicated Malaria in Cameroon [NCT01845701]Phase 3720 participants (Actual)Interventional2010-03-31Completed
A Comparative Assessment of the Effectiveness of Artemether Plus Lumefantrine Versus Artesunate Plus Amodiaquine for the Treatment of Children With Uncomplicated Plasmodium Falciparum Malaria [NCT00374205]Phase 4245 participants (Actual)Interventional2006-09-30Terminated(stopped due to Interim analysis showed more LCFs in one of the treatment arms)
A Single Centre, Open Label, Pilot Phase Ib Study to Investigate Blood Stage Malaria Infection After Direct Venous Inoculation of Cryopreserved P. Falciparum (NF54 Strain) Sporozoites (PfSPZ-DVI) in Malaria naïve Healthy Adult Volunteers [NCT04310085]Phase 116 participants (Actual)Interventional2020-02-19Completed
A Proof-of-concept Study to Assess the Effect of ACT-451840 Against Early Plasmodium Falciparum Blood Stage Infection in Healthy Subjects [NCT02223871]Phase 18 participants (Actual)Interventional2014-06-30Completed
Cluster Randomized Trial of Malaria Seasonal IPTc Combined With Community Case Management in Saraya District, SE Senegal [NCT01449045]Phase 34,554 participants (Actual)Interventional2011-07-31Completed
Efficacy of Dried Leaf Artemisia (DLA) Versus Coartem (ACT): A Randomized Controlled Clinical Trial for Comparing DLA vs. ACT to Treat Malaria [NCT03199755]Phase 20 participants (Actual)Interventional2018-08-20Withdrawn(stopped due to Withdrawn in 2018 because clinicians did not follow protocols, issues with communication and also with tablet processing, nearby Ebola outbreak in 2018 (in the N Kivu area) confounded efforts.)
Evaluation of Safety and Efficacy of Maytenus Senegalensis for the Treatment of Uncomplicated Malaria Episodes in Adult Patients as Compared to Artemether-lumefantrine [NCT04944966]Phase 212 participants (Actual)Interventional2021-06-02Completed
Evaluation of Three Artemisinin-based Combinations for the Treatment of Uncomplicated Malaria in Childreen in Burkina Faso (CHIMIO2) [NCT04778813]Phase 41,050 participants (Anticipated)Interventional2021-06-01Not yet recruiting
Ivermectin-artemisinin Combination Therapy for Eradication of Malaria [NCT05605925]Phase 4138 participants (Anticipated)Interventional2022-08-04Recruiting
Comparative Efficacy and Safety of Pyronaridine-Artesunate Versus Artemether-Lumefantrine in The Treatment of Acute Uncomplicated Malaria Among Children In South-West Nigeria [NCT05192265]Phase 2/Phase 3172 participants (Actual)Interventional2019-05-20Completed
Pyronaridine-artesunate and Artemether-lumefantrine for the Treatment of Paediatric Uncomplicated Falciparum Malaria in Western Kenya [NCT02411994]Phase 3197 participants (Actual)Interventional2015-10-31Completed
Epidemiology of Malaria in Malawi: Human Hosts and Parasites in Three Districts Part 2: Cross-sectional Surveillance (School-based Cohorts) [NCT04858087]786 participants (Actual)Observational2015-03-24Completed
A Randomized, Open-Label Study to Evaluate Potential Pharmacokinetic Interactions of Orally Administered Artemether-lumefantrine and Amodiaquine in Healthy Adult Subjects [NCT04080895]Phase 116 participants (Anticipated)Interventional2022-11-01Recruiting
In Vivo Efficacy of Artemether-lumefantrine and Amodiaquine-artesunate for the Treatment of Uncomplicated Falciparum Malaria in Children: A Multisite Open Label, Two-cohort Clinical Trial in Mozambique [NCT04370977]Phase 4630 participants (Actual)Interventional2018-03-21Completed
Reducing the Burden of Malaria by Targeting Hotspots of Transmission and Improving Malaria Control Measures in the Highlands of Western Kenya: Simultaneous Rollout of Four Malaria Control Interventions and Evaluation by Cross-sectional Surveys [NCT01575613]17,506 participants (Actual)Interventional2012-04-30Completed
Artemether-Lumefantrine Clinical Effectiveness Study [NCT01599000]Phase 4159 participants (Actual)Interventional2011-03-31Completed
Phase 2 Proof of Concept Study of a Candidate Aminoquinoline Antimalarial (AQ-13) [NCT01614964]Phase 266 participants (Actual)Interventional2013-08-31Completed
The Impact of Intermittent Preventive Malaria Treatment With Artemisinin Combination Therapy (ACT) on Hemoglobin, Malaria, Schistosomiasis, and School Attention Among Primary Schoolchildren in the Kassena-Nankana Districts, Ghana [NCT01459146]Phase 4345 participants (Anticipated)Interventional2010-12-31Recruiting
Evaluating the Efficacy of Artemether-lumefantrine for Treatment of Plasmodium Falciparum Malaria in Cruzeiro do Sul, Acre, Brazil [NCT02600767]79 participants (Actual)Interventional2015-12-31Completed
A Randomised, Single Blind, Placebo Controlled, Phase 1 Trial to Evaluate the Safety, Tolerability, Pharmacokinetic and Pharmacodynamic Activity of Ruxolitinib When Co-administered With Artemether-lumefantrine in Healthy Participants [NCT04456634]Phase 18 participants (Actual)Interventional2020-09-10Completed
Randomized, Placebo-Controlled, Double-Blind Study to Assess Safety, Immunogenicity, and Protective Efficacy of Two Regimens of Radiation Attenuated Plasmodium Falciparum NF54 Sporozoites (PfSPZ Vaccine) During Natural Transmission Season in Healthy Afric [NCT03510481]Phase 1478 participants (Actual)Interventional2018-05-14Completed
Efficacy and Safety of Artesunate-amodiaquine and Artemether-lumefantrine in the Treatment of Uncomplicated Plasmodium Falciparum Malaria in the Democratic Republic of the Congo: a Randomized Controlled Trial [NCT04618523]Phase 41,117 participants (Actual)Interventional2020-10-26Completed
"Aiming at Prolonging the Therapeutic Life Span of Artemisinin-based Combination Therapies (ACT) in an Era of Imminent Plasmodium Falciparum Resistance in Bagamoyo District, Tanzania - New Strategies With Old Tools" [NCT03241901]Phase 4280 participants (Actual)Interventional2017-07-27Completed
An Open-label, Single-arm Study to Evaluate the Efficacy, Safety and PK of Artemether-lumefantrine Dispersible Tablet in the Treatment of Acute Uncomplicated Plasmodium Falciparum Malaria in Infants <5 kg Body Weight [NCT01619878]Phase 2/Phase 320 participants (Actual)Interventional2012-10-31Completed
An Open-label Individually Randomised Controlled Trial to Assess the Efficacy of Artemether-lumefantrine Prophylaxis for Malaria Among Forest Goers in Cambodia [NCT04041973]1,480 participants (Actual)Interventional2020-03-11Completed
Evaluation of the Efficacy of Artemisinin Combination Therapy in Kenya [NCT01899820]Phase 32,100 participants (Anticipated)Interventional2013-04-30Active, not recruiting
An Open Label Randomised Comparative Trial to Establish the Efficacy of 3 mg/kg ArTiMist™ When Compared to Intravenous Quinine in Children With Severe or Complicated Falciparum Malaria, or Uncomplicated Falciparum Malaria With Gastrointestinal Complicatio [NCT01047436]Phase 231 participants (Actual)Interventional2009-12-31Completed
A Phase III, Randomised, Open Labelled, Active Controlled, Multi Centre, Superiority Trial of ArTiMist™ Versus Intravenous Quinine in Children With Severe or Complicated Falciparum Malaria, or Uncomplicated Falciparum Malaria With Gastrointestinal Complic [NCT01258049]Phase 3151 participants (Actual)Interventional2010-12-31Completed
Efficacy of Artemether Lumefantrine (AL) and Dihydroartemisinin-Piperaquine (DHP) for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Siaya and Bungoma Counties, Kenya [NCT04767191]Phase 4400 participants (Actual)Interventional2021-03-15Completed
Efficacy and Safety of Artemether Lumefantrine for the Treatment of Uncomplicated Malaria in Tanzania [NCT03387631]344 participants (Actual)Observational [Patient Registry]2016-04-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00297882 (2) [back to overview]Cure Rate Day 14
NCT00297882 (2) [back to overview]Cure Rate on Day 28
NCT00422084 (8) [back to overview]PCR-corrected Adequate Clinical and Parasitological Response (ACPR) on Day 14
NCT00422084 (8) [back to overview]Crude ACPR (Non-PCR Corrected ACPR) on Day 14 and Day 28
NCT00422084 (8) [back to overview]Adverse Events and Clinically Significant Laboratory Results
NCT00422084 (8) [back to overview]PCR-Corrected Adequate Clinical and Parasitological Response (ACPR) Rate on Day 28
NCT00422084 (8) [back to overview]Parasite Clearance Time
NCT00422084 (8) [back to overview]Fever Clearance Time
NCT00422084 (8) [back to overview]Percentage of Patients With Fever Clearance at Day 1, 2 and 3
NCT00422084 (8) [back to overview]Proportion of Patients With Parasite Clearance at Day 1, 2 and 3
NCT00444106 (4) [back to overview]Auditory Changes Following 3 Days of Treatment at Days 3, 7, 28, and 42 Days as Assessed by Pure Tone Thresholds Assessments (a Type of Hearing Test)
NCT00444106 (4) [back to overview]Efficacy of Polymerase Chain Reaction (PCR) Adjusted Malaria Cure Rates of the Three Treatment Regimens at Days 14, 28 and 42
NCT00444106 (4) [back to overview]Relationship Between Changes in Auditory Function and Treatment Groups
NCT00444106 (4) [back to overview]Percentage of Participants With Auditory Abnormalities at Day 7 Assessed by Auditory Brainstem Response (ABR) Wave III Latency Changes on Day 7(a Type of Hearing Test)
NCT00677833 (19) [back to overview]Percentage of Participants With Early Treatment Failure (ETF) in the mITT Population (PCR-corrected)
NCT00677833 (19) [back to overview]Asexual Plasmodium Falciparum Parasite Clearance Time
NCT00677833 (19) [back to overview]Fever Clearance Time
NCT00677833 (19) [back to overview]Nadir Hemoglobin Level
NCT00677833 (19) [back to overview]Percentage of Participants With ETF in PP Population (PCR-corrected)
NCT00677833 (19) [back to overview]Percentage of Participants With PCR-corrected ACPR at Day 28 in Per-Protocol (PP) Population
NCT00677833 (19) [back to overview]Percentage of Participants With Polymerase Chain Reaction (PCR)-Corrected Adequate Clinical and Parasitologic Response (ACPR) at Day 28 in the Modified Intent-to-treat (mITT) Population
NCT00677833 (19) [back to overview]Time to Recurrence of Parasitemia
NCT00677833 (19) [back to overview]Change From Nadir Hemoglobin Level at Days 14, 28, and 42
NCT00677833 (19) [back to overview]Percentage of Participants With Asexual Parasitologic Response (PCR-corrected)
NCT00677833 (19) [back to overview]Percentage of Participants With Gametocytologic Response
NCT00677833 (19) [back to overview]Percentage of Participants With Late Clinical Failure (LCF) in the mITT Population (PCR-corrected)
NCT00677833 (19) [back to overview]Percentage of Participants With Late Parasitologic Failure (LPF) in the mITT Population (PCR-corrected)
NCT00677833 (19) [back to overview]Percentage of Participants With LCF in PP Population (PCR-corrected)
NCT00677833 (19) [back to overview]Percentage of Participants With LPF in PP Population (PCR-corrected)
NCT00677833 (19) [back to overview]Percentage of Participants With PCR-corrected ACPR in PP Population
NCT00677833 (19) [back to overview]Percentage of Participants With PCR-corrected ACPR in the mITT Population
NCT00677833 (19) [back to overview]Percentage of Participants With PCR-uncorrected ACPR in PP Population
NCT00677833 (19) [back to overview]Percentage of Participants With PCR-uncorrected ACPR in the mITT Population
NCT01047436 (6) [back to overview]Parasite Clearance Time
NCT01047436 (6) [back to overview]Time for Parasite Count to Fall by 50% PCT(50)
NCT01047436 (6) [back to overview]Parasite Reduction Ratio (PRR) at 12 Hours After the First Dose
NCT01047436 (6) [back to overview]Parasite Reduction Ratio (PRR) at 24 h (Hours) After the First Dose
NCT01047436 (6) [back to overview]Parasitological Success Defined as a Reduction in Parasite Count of ≥ 90% of Baseline at 24 Hours After the First Dose
NCT01047436 (6) [back to overview]Time for Parasite Count to Fall by 90% PCT(90)
NCT01256658 (22) [back to overview]Microscopy Confirmed Asymptomatic Carriers of P. Falciparum at Community Screening Campaign 4 (CSC4) (Per Cluster)
NCT01256658 (22) [back to overview]Number of Asymptomatic Carriers With Increase in Hemoglobin Levels by at Least 0.5 g/dL From Community Screening Campaign 1 (CSC1) Infants and Children (>6 Months and <5 Years)- Individual Data
NCT01256658 (22) [back to overview]Number of Asymptomatic Carriers With Increase in Hemoglobin Levels by at Least 0.5 g/dL From Day 1 to Day 28 of Community Screening Campaign 1 (CSC1) in Infants and Children (>6 Months and <5 Years)- Cluster Data
NCT01256658 (22) [back to overview]Number of Symptomatic Malaria Episode, RDT-confirmed, With Parasitemia ≥5000/μL (SMRC5000s) Per Person-year in Infants and Children (<5 Years) in Post Community Screening Campaign (CSC) at Month 12 (Per Cluster)
NCT01256658 (22) [back to overview]Number of Symptomatic Malaria Episode, RDT-confirmed, With Parasitemia ≥5000/μL (SMRC5000s) Per Person-year in Post Community Screening Campaign (CSC)
NCT01256658 (22) [back to overview]Anemia Status Based on Community Screening Campaign 1 (CSC1)/Day 1 in Infants and Children (>6 Months and <5 Years)
NCT01256658 (22) [back to overview]Anemia Status Based on Community Screening Campaign 4 (CSC4)/Day 1 in Infants and Children (>6 Months and <5 Years)
NCT01256658 (22) [back to overview]Change in Hemoglobin Level (g/dL) From Community Screening Campaign 1 (CSC1)/Day 1 to CSC1/Day 28 in Infants and Children (>6 Months and <5 Years) for Asymptomatic Carriers at CSC1
NCT01256658 (22) [back to overview]Change in Hemoglobin Level (g/dL) From Community Screening Campaign 1(CSC1)/Day 1 to Community Screening Campaign 4 (CSC4)/Day 1 (Per Cluster)
NCT01256658 (22) [back to overview]Change in Hemoglobin Level (g/dL) in Asymptomatic Carriers >6 Months of Age (Per Cluster)
NCT01256658 (22) [back to overview]Cumulative Number of Subjects With Symptomatic Malaria Episode, RDT-confirmed, With Parasitemia ≥5000/μL From Week 1 to Week 50
NCT01256658 (22) [back to overview]Hemoglobin Level (g/dL) in Community Screening Campaign 1 (CSC1)/Day 1 and CSC4/Day 1 by Study Arm and Age Group (Per Cluster)
NCT01256658 (22) [back to overview]Microscopy-confirmed Gametocyte Carriers at Community Screening Campaign 4 (CSC4) (Per Cluster)
NCT01256658 (22) [back to overview]Mean of Microscopy-confirmed Asymptomatic Carriers From Community Screening Campaigns 1, 2, 3 and 4 (CSC1, CSC2, CSC3 and CSC4) (Per Cluster)
NCT01256658 (22) [back to overview]Number of Asymptomatic Carriers With Complicated and Uncomplicated Episodes Combined
NCT01256658 (22) [back to overview]Number of Microscopy and qRT-PCR-confirmed Gametocyte Carriers at Community Screening Campaign 4 (CSC4)
NCT01256658 (22) [back to overview]Number of Participants (Infants and Children (> 6 Months and < 5 Years)) With Hospitalizations, Severe Malaria Episodes or Death Post Community Screening Campaign (CSC)
NCT01256658 (22) [back to overview]Number of Participants With Hospitalizations, Severe Malaria Episodes or Death Post Community Screening Campaign (CSC)
NCT01256658 (22) [back to overview]Number of Symptomatic Malaria Episode, RDT-confirmed, With Parasitemia ≥5000/μL (SMRC5000) in Asymptomatic Carriers at Any Time of Diagnosis (Per Cluster)
NCT01256658 (22) [back to overview]Mean Number of Microscopy-confirmed Gametocyte Carriers at Day 1 of Community Screening Campaign 1,2,3,4 (CSC1, CSC2, CSC3 and CSC4) (Per Cluster)
NCT01256658 (22) [back to overview]Percentage of Microscopy-confirmed Gametocyte Carriers Treated With COA566 for Asymptomatic Carriers
NCT01256658 (22) [back to overview]Percentage of COA566-treated Microscopy-confirmed Asymptomatic Carriers at Community Screening Campaign 1, 2 and 3 (CSC1, CSC2 and CSC3) With Parasitological Cure Rate at Day 7
NCT01258049 (16) [back to overview]Parasite Clearance Time (PCT) [MITT Population]
NCT01258049 (16) [back to overview]PCT 50 [MITT Population]
NCT01258049 (16) [back to overview]PCT 90 [MITT Population]
NCT01258049 (16) [back to overview]PRR 12 [MITT Population]
NCT01258049 (16) [back to overview]PRR 24 [MITT Population]
NCT01258049 (16) [back to overview]Time to Return to Full Consciousness
NCT01258049 (16) [back to overview]Time to Return to Normal Per os Status
NCT01258049 (16) [back to overview]Complete Cure Rate
NCT01258049 (16) [back to overview]Parasitological Success (MITT)
NCT01258049 (16) [back to overview]Parasitological Success (PP)
NCT01258049 (16) [back to overview]Early Treatment Failure
NCT01258049 (16) [back to overview]Fever Clearance Time (FCT)
NCT01258049 (16) [back to overview]Late Clinical Failure
NCT01258049 (16) [back to overview]Late Parasitological Failure
NCT01258049 (16) [back to overview]Number of Deaths or Neurological Sequelae at Day 28
NCT01258049 (16) [back to overview]Number of Participants With Treatment Emergent Adverse Events and Serious Adverse Events, of Possible, Probably and Definite Causalities
NCT01619878 (9) [back to overview]Time to Parasite Clearance (PCT)
NCT01619878 (9) [back to overview]Time to Gametocyte Clearance (GCT)
NCT01619878 (9) [back to overview]Time to Fever Clearance (FCT)
NCT01619878 (9) [back to overview]Polymerase Chain Reaction (PCR) Corrected 28 Day Parasitological Cure Rate
NCT01619878 (9) [back to overview]Percent Change of Parasite Count From Baseline at 24 Hours
NCT01619878 (9) [back to overview]Number of Participants With Parasitaemia at 72 Hours After Treatment Initiation Greater Than or Equal to 25 Percent of Count at Baseline
NCT01619878 (9) [back to overview]Number of Participants With Parasitaemia at 48 Hours After Treatment Initiation Greater Than at Baseline
NCT01619878 (9) [back to overview]Polymerase Chain Reaction (PCR) Corrected Parasitological Cure Rate at Day 14 and 42
NCT01619878 (9) [back to overview]Number of Participants With Parasitological Uncorrected Cure Rate at Day 3, 7, 14, 28 and 42
NCT02223871 (9) [back to overview]Change From Baseline in Respiratory Rate to End of Study (EOS)
NCT02223871 (9) [back to overview]Drug-specific Parasite Reduction Ratio (PRR48) of ACT-451840 Over 48 Hours Using a New Approach
NCT02223871 (9) [back to overview]Drug-specific Parasite Reduction Ratio (PRR48) of ACT-451840 Over 48 Hours Using a Standardized Approach
NCT02223871 (9) [back to overview]Maximum Plasma Concentration (Cmax) of ACT-451840
NCT02223871 (9) [back to overview]Terminal Half-life [t(1/2)]
NCT02223871 (9) [back to overview]Time to Reach Maximum Plasma Concentration (Tmax) of ACT-451840
NCT02223871 (9) [back to overview]Areas Under the Plasma Concentration-time Curve of ACT-451840
NCT02223871 (9) [back to overview]Change From Baseline in Blood Pressure to End of Study (EOS)
NCT02223871 (9) [back to overview]Change From Baseline in Body Temperature up to End of Study (EOS)
NCT02389374 (9) [back to overview]Recurrence of Parasitaemia Within 16 Days of Follow up
NCT02389374 (9) [back to overview]Fractional Change in Hb Between Baseline and Day 9 and 16
NCT02389374 (9) [back to overview]The Proportion of Adverse and Serious Adverse Events Following Unsupervised Primaquine Treatment
NCT02389374 (9) [back to overview]The Distribution of G6PD Activity Measured in U/gHb Among All Malaria Patients
NCT02389374 (9) [back to overview]Proportion of Patients With Fever on Day 2 After Treatment
NCT02389374 (9) [back to overview]Proportion of Patients With Any Parasitemia on Day 3 After Treatment
NCT02389374 (9) [back to overview]Proportion of Patients With Anaemia Less Than 8g/dl on Day 2
NCT02389374 (9) [back to overview]Proportion of Patients Receiving Blood Transfusion and With Severe Anaemia (Hb<7g/dl)
NCT02389374 (9) [back to overview]Proportion of Patients Adhering to 14 Days of Primaquine Treatment in the Vivax Cohort as Measured by Pill Count
NCT02600767 (1) [back to overview]Absence of Malaria Parasites in Blood.
NCT03334747 (14) [back to overview]Half-life (T^1/2)
NCT03334747 (14) [back to overview]Maximum Peak Observed Concentration (Cmax)
NCT03334747 (14) [back to overview]Percentage of Participants With Polymerase Chain Reaction (PCR)-Corrected and Uncorrected Adequate Clinical and Parasitological Response (ACPR) at Day 15 and Day 29
NCT03334747 (14) [back to overview]Maximum Peak Observed Concentration (Cmax)
NCT03334747 (14) [back to overview]Fever Clearance Time (FCT)
NCT03334747 (14) [back to overview]Tmax
NCT03334747 (14) [back to overview]Tmax
NCT03334747 (14) [back to overview]Time to Recrudescence and Reinfection at Study Day 29
NCT03334747 (14) [back to overview]Time to Recrudescence and Reinfection at Study Day 29
NCT03334747 (14) [back to overview]Number of Participants With at Least 2 CTCAE Grades Increase From Baseline in Alanine Aminotransferase (ALT) or Aspartate Aminotransferase (AST)
NCT03334747 (14) [back to overview]Parasite Clearance Time (PCT)
NCT03334747 (14) [back to overview]AUC0-24
NCT03334747 (14) [back to overview]AUC0-24
NCT03334747 (14) [back to overview]Half-life (T^1/2)
NCT03510481 (2) [back to overview]Number of Participants With Local and Systemic Adverse Events in Year Two
NCT03510481 (2) [back to overview]Number of Participants With Local and Systemic Adverse Events in Year One
NCT03813108 (5) [back to overview]Frequency of Adverse Events After NF135.C10 CPS Immunization
NCT03813108 (5) [back to overview]Magnitude of Adverse Events After NF135.C10 CPS Immunization
NCT03813108 (5) [back to overview]Break Through Infections
NCT03813108 (5) [back to overview]Break Through Infections
NCT03813108 (5) [back to overview]Time to Parasitemia
NCT04310085 (9) [back to overview]Time to First PCR Positivity.
NCT04310085 (9) [back to overview]Time to First Dose of Treatment With Artemether-lumefantrine (Riamet®) (Cohorts 1 and 2)
NCT04310085 (9) [back to overview]Parasitaemia at the Time Parasitaemia ≥5000 Parasites Per mL Blood (Cohorts 1 and 2)
NCT04310085 (9) [back to overview]Parasitaemia at First PCR Positivity
NCT04310085 (9) [back to overview]Incidence and Severity of Observed or Self-reported Adverse Events (AEs) Considered PfSPZ-DVI Challenge Inoculum-related.
NCT04310085 (9) [back to overview]Time to Parasitaemia of ≥5000 Parasites Per mL Blood (Cohorts 1 and 2)
NCT04310085 (9) [back to overview]Change in Malaria Clinical Score From PfSPZ-DVI Challenge Until Parasite Clearance.
NCT04310085 (9) [back to overview]Incidence of Positive PCR and Parasitaemia of ≥5000 Parasites Per mL Blood.
NCT04310085 (9) [back to overview]Parasitaemia at First Dose of Treatment With Riamet® (Cohorts 1 and 2)
NCT04456634 (5) [back to overview]Number of Participants With ECG Changes
NCT04456634 (5) [back to overview]Number of Participants With Changes in Heart Rate
NCT04456634 (5) [back to overview]Number of Participant With Treatment-Related Adverse Events as Assessed by CTCAE V4.03, All of Observed and Self-reported AEs Affected, by Treatment Regimen.
NCT04456634 (5) [back to overview]AUECt of pSTAT3 Inhibition
NCT04456634 (5) [back to overview]Number of Participants With Changes of Systolic and Diastolic Blood Pressure

Cure Rate Day 14

To evaluate antimalarial efficacy of AL and AQ-AS on day 14 post-treatment (NCT00297882)
Timeframe: Day 0-14

InterventionParticipants (Count of Participants)
1 Artemether-Lumefantrine192
2 Amodiaquine-Artesunate563

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Cure Rate on Day 28

To evaluate the safety and antimalarial efficacy of two drug combinations: Artemether-Lumefantrine (AL) and Amodiaquine-Artesunate (AQ - AS) in Camaroonian patients in Mutengene, Bangolan and Garoua (NCT00297882)
Timeframe: Day 0 - 28

InterventionParticipants (Count of Participants)
1 Artemether-Lumefantrine AL197
2 Amodiaquine-Artesunate AQ-AS603

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PCR-corrected Adequate Clinical and Parasitological Response (ACPR) on Day 14

Percentage of subjects with PCR-corrected adequate clinical and parasitological response (ACPR) on Day 14, defined as absence of parasitaemia on Day 14 without the subject's meeting any of the criteria of early treatment failure, late clinical failure, or late parasitological failure. (NCT00422084)
Timeframe: Day 14

Interventionpercentage of subjects (Number)
PA Group99.9
AL Group100

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Crude ACPR (Non-PCR Corrected ACPR) on Day 14 and Day 28

Percentage of subjects with adequate clinical and parasitological response (ACPR) on Day 28, without correction by PCR, defined as absence of parasitaemia on Day 28 without the subject's meeting any of the criteria of early treatment failure, late clinical failure, or late parasitological failure. (NCT00422084)
Timeframe: Day 14 and 28

,
Interventionpercentage of subjects (Number)
Cure rate (%) at Day 14Cure rate (%) at Day 28
AL Group10097.2
PA Group10098.9

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Adverse Events and Clinically Significant Laboratory Results

Incidence of adverse events and of clinically significant laboratory results, ECG, vital signs or physical examination abnormalities. (NCT00422084)
Timeframe: Day 0 to 42. Subjects experiencing AEs at Day 42 were followed for up to 30 days after the end of study or resolution of the event, whichever was earlier

,
InterventionParticipants (Count of Participants)
Nr subj. with ≥1 AENr subj. with ≥1 treatment-related AENr subj. with ≥1 SAENr pat with ≥1 treatment-related SAENr subj. with ≥1 severe or life-threatening AENr subj. with ≥1 AE leading to deathNr subj. ≥1 AE leading to drug discontinuationNr subj. with ≥1 AE leading to study withdrawal
AL Group241123205056
PA Group509275301001619

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PCR-Corrected Adequate Clinical and Parasitological Response (ACPR) Rate on Day 28

Percentage of subjects with PCR-corrected adequate clinical and parasitological response (ACPR) on Day 28, defined as absence of parasitaemia on Day 28 without the subject's meeting any of the criteria of early treatment failure, late clinical failure, or late parasitological failure. (NCT00422084)
Timeframe: Day 28

Interventionpercentage of subjects (Number)
PA Group99.5
AL Group99.2

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Parasite Clearance Time

Parasite clearance time is defined as the time from first dosing to the time of first blood draw with parasite clearance. Parasite clearance is defined as zero presence of asexual parasites for 2 consecutive negative readings taken between 7 and 25 hours apart. (NCT00422084)
Timeframe: Days 0, 3, 7, 14, 21, 28, 35, and 42 (or on any other day if the subject spontaneously returned)

Interventionhours (Median)
PA Group23.9
AL Group24.0

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Fever Clearance Time

Fever clearance time is defined as the time from first dosing to first normal reading of temperature for 2 consecutive normal temperature readings taken between 7 and 25 hours apart (NCT00422084)
Timeframe: Day 0 and every 8 hours over ≥72 hours following first study drug administration or temperature normalization for ≥2 readings between 7 and 25 hours apart, then at each visit and as clinically indicated

Interventionhours (Median)
PA Group7.9
AL Group8.0

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Percentage of Patients With Fever Clearance at Day 1, 2 and 3

Fever clearance time is defined as the time from first dosing to first normal reading of temperature for 2 consecutive normal temperature readings taken between 7 and 25 hours apart. (NCT00422084)
Timeframe: Days 1, 2, 3

,
Interventionpercentage of subjects (Number)
Clearance rate (%) at Day 1 (24h after first dose)Clearance rate (%) at Day 2 (48h after first dose)Clearance rate (%) at Day 3 (72h after first dose)
AL Group87.098.799.3
PA Group88.799.099.5

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Proportion of Patients With Parasite Clearance at Day 1, 2 and 3

Parasite clearance time is defined as the time from first dosing to the time of first blood draw with parasite clearance. Parasite clearance was defined as zero presence of asexual parasites for 2 consecutive negative readings taken between 7 and 25 hours apart. (NCT00422084)
Timeframe: Days 1, 2, 3

,
Interventionpercentage of subjects (Number)
Clearance rate (%) at Day 1 (24h after first dose)Clearance rate (%) at Day 2 (48h after first dose)Clearance rate (%) at Day 3 (72h after first dose)
AL Group52.897.299.7
PA Group68.198.199.5

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Auditory Changes Following 3 Days of Treatment at Days 3, 7, 28, and 42 Days as Assessed by Pure Tone Thresholds Assessments (a Type of Hearing Test)

Audiometric measurements such as pure-tone threshold (air conduction tested at 250 to 8000 HZ) day 3, 7, 28 and 42 following initiation of treatment, including changes from baseline. Pure-tone average (PTA) calculated for each ear by averaging the pure-tone threshold values at 500, 1000, 2000 and 3000 HZ. (NCT00444106)
Timeframe: Baseline (Day 1), 3, 7, 28 and Day 42

,,
InterventiondB (Mean)
Baseline Right EarChange from baseline to Day 3 Right EarChange from baseline to Day 7 Right EarChange from baseline to Day 28 Right EarChange from baseline to Day 42 Right EarBaseline Left EarChange from baseline to Day 3 Left EarChange from baseline to Day 7 Left EarChange from baseline to Day 28 Left EarChange from baseline to Day 42 Left Ear
Artemether-lumefantrine12.2-2.5-2.2-2.7-3.011.4-1.2-1.7-2.0-1.5
Artesunate-mefloquine12.7-1.9-2.6-3.6-3.112.5-1.2-1.4-2.5-3.0
Atovaquone-proguanil (Malarone)12.0-2.4-2.6-2.6-3.311.3-1.5-1.3-1.8-2.1

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Efficacy of Polymerase Chain Reaction (PCR) Adjusted Malaria Cure Rates of the Three Treatment Regimens at Days 14, 28 and 42

Percentage of patients with clearance of asexual parasitemia (observed by optical microscopy) within 7 days of initiation of trial treatment without recrudescence within 14, 28 and 42 days respectively after initiation of treatment. Patients with recurrent parasitemia and paired PCR results were classified as either a new infection (different paired genotypes) or a recrudescence (matching paired genotypes). Patients without paired PCR results or ambiguous results were classified as treatment failures. (NCT00444106)
Timeframe: Days 14, 28 and 42

,,
InterventionPercentage of Participants (Number)
Day 14Day 28Day 42
Artemether-lumefantrine (Coartem)99.498.797.5
Artesunate-mefloquine98.198.198.1
Atovaquone-proguanil (Malarone)100.098.198.1

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Relationship Between Changes in Auditory Function and Treatment Groups

ABR Wave III latency (ms) changes from baseline to Day 7 in the three drug exposure groups. (NCT00444106)
Timeframe: From Baseline to Day 7

,,
Interventionms (Mean)
Baseline Right EarChange from baseline to Day 7 Right EarBaseline Left EarChange from baseline to Day 7 Left Ear
Artemether-lumefantrine (Coartem)3.860.013.850.01
Artesunate-mefloquine3.86-0.043.82-0.03
Atovaquone-proguanil (Malarone)3.89-0.013.88-0.01

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Percentage of Participants With Auditory Abnormalities at Day 7 Assessed by Auditory Brainstem Response (ABR) Wave III Latency Changes on Day 7(a Type of Hearing Test)

"To demonstrate the safety of artemether-lumefantrine after 3 days of treatment in patients with acute, uncomplicated falciparum malaria by testing the null hypothesis that the rate of auditory abnormalities is ≥ 15% in the population treated with artemether-lumefantrine as assessed by ABR at Day 7 following initiation of treatment compared with their baseline values. An auditory nerve abnormality is here defined as a greater than 0.30 ms change in Wave III latency from baseline to Day 7. Exact Pearson-Clopper two-sided 95% confidence limits were constructed for all three treatment groups." (NCT00444106)
Timeframe: 7 days

InterventionPercentage of Participants (Number)
Artemether-lumefantrine (Coartem)2.6

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Percentage of Participants With Early Treatment Failure (ETF) in the mITT Population (PCR-corrected)

"ETF defined as participants who met the following criteria:~Developed signs of severe malaria or clinical deterioration that required rescue medication on Days 0, 1, 2 or 3, in the presence of P. falciparum parasitemia~Last available asexual P. falciparum parasite count on Day 2 greater than the first available parasite count on Day 0 (Baseline), irrespective of axillary, oral or rectal temperature.~Parasitemia (P. falciparum) on Day 3 with fever or~Last available P. falciparum parasite count on Day 3 >=25% of the first available parasite count on Day 0 (Baseline).~PCR-corrected refers to the use of molecular testing to differentiate recrudescence from reinfection in the context of an efficacy evaluation." (NCT00677833)
Timeframe: Day 0 up to Day 3

InterventionPercentage of participants (Number)
Cohort 2: Azithromycin + Chloroquine5.83
Cohort 2: Artemether + Lumefantrine0.79

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Asexual Plasmodium Falciparum Parasite Clearance Time

Defined as time to first of two consecutive zero asexual P. falciparum parasite (PCR-corrected) counts, regardless of recurrence of parasitemia later. PCR-corrected refers to the use of molecular testing to differentiate recrudescence from reinfection in the context of an efficacy evaluation. (NCT00677833)
Timeframe: Baseline to Day 42

InterventionHours (Median)
Cohort 2: Azithromycin + Chloroquine48.000
Cohort 2: Artemether + Lumefantrine24.000

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Fever Clearance Time

Calculated as time of first occurrence of two consecutive time points with temperature less than (<) 38.0 degrees C/100.4 degrees Fahrenheit (F) (rectal), 37.2 degrees C/99.0 degrees F (axillary), or <37.5 degrees C/99.5 degrees F (oral). (NCT00677833)
Timeframe: Baseline to Day 42

InterventionHours (Median)
Cohort 2: Azithromycin + Chloroquine24.000
Cohort 2: Artemether + Lumefantrine24.000

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Nadir Hemoglobin Level

Nadir hemoglobin for each participant was defined as the minimum hemoglobin values obtained from Day 0 through Day 3. (NCT00677833)
Timeframe: Day 0 through Day 3

Interventiongrams per deciliter (g/dL) (Mean)
Cohort 2: Azithromycin + Chloroquine9.63
Cohort 2: Artemether + Lumefantrine9.82

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Percentage of Participants With ETF in PP Population (PCR-corrected)

"ETF defined as participants who met the following criteria:~Developed signs of severe malaria or clinical deterioration that required rescue medication on Days 0, 1, 2 or 3, in the presence of P.falciparum parasitemia~Last available asexual P.falciparum parasite count on Day 2 greater than the first available parasite count on Day 0 (Baseline), irrespective of axillary, oral or rectal temperature.~Parasitemia (P.falciparum) on Day 3 with fever or~Last available P.falciparum parasite count on Day 3 >=25% of the first available parasite count on Day 0 (Baseline).~PCR-corrected refers to the use of molecular testing to differentiate recrudescence from reinfection in the context of an efficacy evaluation." (NCT00677833)
Timeframe: Day 0 up to Day 3

InterventionPercentage of participants (Number)
Cohort 2: Azithromycin + Chloroquine1.75
Cohort 2: Artemether + Lumefantrine0

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Percentage of Participants With PCR-corrected ACPR at Day 28 in Per-Protocol (PP) Population

ACPR (PCR-corrected) was defined as asexual P.falciparum parasitologic clearance at Day 28 irrespective of axillary, oral, rectal, or tympanic temperature, without previously meeting the criteria of ETF (see measure description in secondary outcome measures 7 and 8) or PCR-corrected LTF (which includes PCR-corrected LCF - see measure description in secondary outcome measure 9 and 10, and PCR-corrected LPF - see measure description in secondary outcome measure 11 and 12). PCR-corrected refers to the use of molecular testing to differentiate recrudescence from reinfection in the context of an efficacy evaluation. (NCT00677833)
Timeframe: Day 28

InterventionPercentage of participants (Number)
Cohort 2: Azithromycin + Chloroquine93.08
Cohort 2: Artemether + Lumefantrine99.16

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Percentage of Participants With Polymerase Chain Reaction (PCR)-Corrected Adequate Clinical and Parasitologic Response (ACPR) at Day 28 in the Modified Intent-to-treat (mITT) Population

ACPR (PCR-corrected) was defined as asexual Plasmodium falciparum (P.falciparum) parasitologic clearance at Day 28 irrespective of axillary, oral, rectal, or tympanic temperature, without previously meeting the criteria of Early Treatment Failure (ETF) (see measure description in secondary outcome measures 7 and 8) or PCR-corrected Late Treatment Failure (LTF) (which includes PCR-corrected Late Clinical Failures [LCF] - see measure description in secondary outcome measure 9 and 10, and PCR-corrected Late Parasitologic Failures (LPF)- see measure description in secondary outcome measure 11 and 12). PCR-corrected refers to the use of molecular testing to differentiate recrudescence from reinfection in the context of an efficacy evaluation. (NCT00677833)
Timeframe: Day 28

InterventionPercentage of participants (Number)
Cohort 2: Azithromycin + Chloroquine89.27
Cohort 2: Artemether + Lumefantrine98.37

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Time to Recurrence of Parasitemia

Time from the day of clearance to the time of recurrence of asexual P.falciparum parasitemia (PCR-uncorrected). (NCT00677833)
Timeframe: Baseline (Day 0) to Day 42

InterventionDays (Median)
Cohort 2: Azithromycin + Chloroquine34
Cohort 2: Artemether + LumefantrineNA

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Change From Nadir Hemoglobin Level at Days 14, 28, and 42

Change from nadir = observation minus nadir. Nadir defined as the minimum value for each participant on Days 0-3. (NCT00677833)
Timeframe: Day 14, 28, 42

,
Interventiong/dL (Mean)
Change at Day 14 (n=122, 127)Change at Day 28 (n=122, 127)Change at Day 42 (n=122, 128)
Cohort 2: Artemether + Lumefantrine0.440.961.14
Cohort 2: Azithromycin + Chloroquine0.521.151.29

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Percentage of Participants With Asexual Parasitologic Response (PCR-corrected)

Percentage of participants who were cleared of asexual parasites. Asexual parasite clearance - clearance of asexual P.falciparum parasitemia within 7 days of initiation of treatment without subsequent recurrence (PCR-corrected) through the day of consideration. PCR-corrected refers to the use of molecular testing to differentiate recrudescence from reinfection in the context of an efficacy evaluation. (NCT00677833)
Timeframe: Day 7, 14, 21, 28, 35, 42

,
InterventionPercentage of participants (Number)
Day 7 (n=120, 128)Day 14 (n=120, 127)Day 21 (n=120, 128)Day 28 (n=120, 127)Day 35 (n=120, 128)Day 42 (n=120, 127)
Cohort 2: Artemether + Lumefantrine99.2299.2198.4498.4396.8896.85
Cohort 2: Azithromycin + Chloroquine93.3391.6790.8389.1789.1788.33

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Percentage of Participants With Gametocytologic Response

Gametocyte response/absence/clearance: Clearance of P.falciparum gametocytemia (PCR-uncorrected) (attainment of 2 consecutive zero gametocyte counts) without subsequent recurrence through the day of consideration. PCR-uncorrected: not adjusted for molecular testing which determined recrudescence or true failures from reinfection. (NCT00677833)
Timeframe: Days 7, 14, 21, 28, 35, 42

,
InterventionPercentage of participants (Number)
Day 7 (n=122, 129)Day 14 (n=122, 130)Day 21 (n=122, 130)Day 28 (n=122, 130)Day 35 (n=122, 130)Day 42 (n=122, 130)
Cohort 2: Artemether + Lumefantrine91.4791.5493.0893.0892.3191.54
Cohort 2: Azithromycin + Chloroquine81.9781.1580.3381.9781.9780.33

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Percentage of Participants With Late Clinical Failure (LCF) in the mITT Population (PCR-corrected)

"LCF included participants who met any of the following criteria:~Development of signs of severe malaria or clinical deterioration requiring rescue medication after Day 3 in the presence of P.falciparum parasitemia, without previously meeting any of the criteria of ETF (see measure description in secondary outcome measures 7 and 8)~Presence of P.falciparum parasitemia and fever on any day from Day 4 onward, without previously meeting any of the criteria of ETF (see measure description in secondary outcome measures 7 and 8). PCR-corrected refers to the use of molecular testing to differentiate recrudescence from reinfection in the context of an efficacy evaluation." (NCT00677833)
Timeframe: Days 7, 14, 21, 28, 35, 42

,
InterventionPercentage of participants (Number)
Day 7Day 14Day 21Day 28Day 35Day 42
Cohort 2: Artemether + Lumefantrine000000
Cohort 2: Azithromycin + Chloroquine000000

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Percentage of Participants With Late Parasitologic Failure (LPF) in the mITT Population (PCR-corrected)

LPF: Presence of P. falciparum parasitemia in the mITT population on any day from Day 7 onward and the absence of fever without previously meeting any of the criteria of ETF (see measure description in secondary outcome measures 7 and 8) or LCF (see measure description in secondary outcome measure 9 and 10). PCR-corrected refers to the use of molecular testing to differentiate recrudescence from reinfection in the context of an efficacy evaluation. (NCT00677833)
Timeframe: Days 7, 14, 21, 28, 35, 42

,
InterventionPercentage of participants (Number)
Day 7Day 14Day 21Day 28Day 35Day 42
Cohort 2: Artemether + Lumefantrine000.790.792.382.38
Cohort 2: Azithromycin + Chloroquine01.672.504.174.175.00

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Percentage of Participants With LCF in PP Population (PCR-corrected)

"LCF included participants who met any of the following criteria:~Development of signs of severe malaria or clinical deterioration requiring rescue medication after Day 3 in the presence of P.falciparum parasitemia, without previously meeting any of the criteria of ETF (see measure description in secondary outcome measures 7 and 8)~Presence of P.falciparum parasitemia and fever on any day from Day 4 onward, without previously meeting any of the criteria of ETF (see measure description in secondary outcome measures 7 and 8). PCR-corrected refers to the use of molecular testing to differentiate recrudescence from reinfection in the context of an efficacy evaluation." (NCT00677833)
Timeframe: Days 7, 14, 21, 28, 35, 42

,
InterventionPercentage of participants (Number)
Day 7Day 14Day 21Day 28Day 35Day 42
Cohort 2: Artemether + Lumefantrine000000
Cohort 2: Azithromycin + Chloroquine000000

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Percentage of Participants With LPF in PP Population (PCR-corrected)

LPF: Presence of P.falciparum parasitemia in the PP population on any day from Day 7 onward and the absence of fever without previously meeting any of the criteria of ETF (see measure description in secondary outcome measures 7 and 8) or LCF (see measure description in secondary outcome measure 9 and 10). PCR-corrected refers to the use of molecular testing to differentiate recrudescence from reinfection in the context of an efficacy evaluation. (NCT00677833)
Timeframe: Days 7, 14, 21, 28, 35, 42

,
InterventionPercentage of participants (Number)
Day 7Day 14Day 21Day 28Day 35Day 42
Cohort 2: Artemether + Lumefantrine000.810.812.422.42
Cohort 2: Azithromycin + Chloroquine01.752.634.394.395.26

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Percentage of Participants With PCR-corrected ACPR in PP Population

ACPR (PCR-corrected) was defined as asexual P.falciparum parasitologic clearance on Days 7, 14, 21, 35, 42 irrespective of axillary, oral, rectal, or tympanic temperature, without previously meeting the criteria of ETF (see measure description in secondary outcome measures 7 and 8) or PCR-corrected LTF (which includes PCR-corrected LCF - see measure description in secondary outcome measure 9 and 10, and PCR-corrected LPF - see measure description in secondary outcome measure 11 and 12). PCR-corrected refers to the use of molecular testing to differentiate recrudescence from reinfection in the context of an efficacy evaluation. (NCT00677833)
Timeframe: Days 7, 14, 21, 35, 42

,
InterventionPercentage of participants (Number)
Day 7Day 14Day 21Day 35Day 42
Cohort 2: Artemether + Lumefantrine100.00100.0099.1696.9696.96
Cohort 2: Azithromycin + Chloroquine98.2596.4695.5393.0891.29

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Percentage of Participants With PCR-corrected ACPR in the mITT Population

ACPR (PCR-corrected) was defined as asexual P.falciparum parasitologic clearance on Days 7, 14, 21, 35, 42 irrespective of axillary, oral, rectal, or tympanic temperature, without previously meeting the criteria of ETF (see measure description in secondary outcome measures 7 and 8) or PCR-corrected LTF (which includes PCR-Corrected LCF- see measure description in secondary outcome measure 9 and 10, and PCR-corrected LPF - see measure description in secondary outcome measure 11 and 12). PCR-corrected refers to the use of molecular testing to differentiate recrudescence from reinfection in the context of an efficacy evaluation. (NCT00677833)
Timeframe: Days 7, 14, 21, 35, 42

,
InterventionPercentage of participants (Number)
Day 7Day 14Day 21Day 35Day 42
Cohort 2: Artemether + Lumefantrine99.2199.2198.3796.1996.19
Cohort 2: Azithromycin + Chloroquine94.1792.4791.5989.2787.55

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Percentage of Participants With PCR-uncorrected ACPR in PP Population

ACPR (PCR-uncorrected) was defined as asexual P.falciparum parasitologic clearance on Days 7, 14, 21, 28, 35, 42 irrespective of axillary, oral, rectal, or tympanic temperature, without previously meeting the criteria of ETF (see measure description in secondary outcome measures 7 and 8) or PCR-uncorrected LTF (which includes PCR-uncorrected LCF - see measure description in secondary outcome measure 9 and 10, and PCR-uncorrected LPF - see measure description in secondary outcome measure 11 and 12). PCR-uncorrected: not adjusted for molecular testing which determined recrudescence or true failures from reinfection. (NCT00677833)
Timeframe: Days 7, 14, 21, 28, 35, 42

,
InterventionPercentage of participants (Number)
Day 7Day 14Day 21Day 28Day 35Day 42
Cohort 2: Artemether + Lumefantrine100.0097.5683.6273.9063.4156.74
Cohort 2: Azithromycin + Chloroquine98.2592.8970.5654.2847.0439.80

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Percentage of Participants With PCR-uncorrected ACPR in the mITT Population

ACPR (PCR-uncorrected) was defined as asexual P.falciparum parasitologic clearance on Days 7, 14, 21, 28, 35, 42 irrespective of axillary, oral, rectal, or tympanic temperature, without previously meeting the criteria of ETF (see measure description in secondary outcome measures 7 and 8) or PCR-uncorrected LTF (which includes PCR-uncorrected LCF - see measure description in secondary outcome measure 9 and 10, and PCR-uncorrected LPF - see measure description in secondary outcome measure 11 and 12). PCR-uncorrected: not adjusted for molecular testing which determined recrudescence or true failures from reinfection. (NCT00677833)
Timeframe: Days 7, 14, 21, 28, 35, 42

,
InterventionPercentage of participants (Number)
Day 7Day 14Day 21Day 28Day 35Day 42
Cohort 2: Artemether + Lumefantrine99.2196.7982.9673.3162.9156.29
Cohort 2: Azithromycin + Chloroquine94.1789.0867.8751.5544.6737.80

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Parasite Clearance Time

Time in hours from the initiation of therapy until the first of two successive parasite-negative smears were obtained (NCT01047436)
Timeframe: 3h (hours), 6h, 12h, 18h, 24h, 30h, 36h, 48h, 54h, 60h

InterventionHours (Mean)
ArTiMist35.7
Intravenous Quinine51.2

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Time for Parasite Count to Fall by 50% PCT(50)

The time taken for the parasite count to fall 50% from baseline (NCT01047436)
Timeframe: 3 h (hours) , 6h, 12h, 18h, 24h, 30h, 36h, 48h, 54h, 60h

Interventionhours (Mean)
ArTiMist12.0
Intravenous Quinine10.8

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Parasite Reduction Ratio (PRR) at 12 Hours After the First Dose

Reduction in parasitaemia from baseline at 12 hours after the first dose of study medication (NCT01047436)
Timeframe: 12 h (hours) after first dose

InterventionPercent reduction (Median)
ArTiMist79.6
Intravenous Quinine75.9

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Parasite Reduction Ratio (PRR) at 24 h (Hours) After the First Dose

Reduction in parasitaemia from baseline at 24 h after the first dose of study medication (NCT01047436)
Timeframe: 24 hours after first dose

InterventionPercent reduction (Median)
ArTiMist100.0
Intravenous Quinine96.9

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Parasitological Success Defined as a Reduction in Parasite Count of ≥ 90% of Baseline at 24 Hours After the First Dose

(NCT01047436)
Timeframe: 24 hours after first dose

Interventionparticipants (Number)
ArTiMist14
Intravenous Quinine10

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Time for Parasite Count to Fall by 90% PCT(90)

The time taken for the parasite count to fall 90% from baseline (NCT01047436)
Timeframe: 3h (hours), 6h, 12h, 18h, 24h, 30h, 36h, 48h, 54h, 60h

Interventionhours (Mean)
ArTiMist17.6
Intravenous Quinine19.8

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Microscopy Confirmed Asymptomatic Carriers of P. Falciparum at Community Screening Campaign 4 (CSC4) (Per Cluster)

"Data is presented per cluster. Microscopy confirmation of asymptomatic carriers of P. falciparum at Community Screening Campaign 4 (CSC4) was conducted at month 12. Blood films were histologically treated and examined microscopically. When it was ascertained that P. falciparum was present, a count of the asexual forms against leukocytes was made using a tally counter." (NCT01256658)
Timeframe: Month 12 - period 1

Interventionparticipants (Mean)
Intervention34.6
Control37.6

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Number of Asymptomatic Carriers With Increase in Hemoglobin Levels by at Least 0.5 g/dL From Community Screening Campaign 1 (CSC1) Infants and Children (>6 Months and <5 Years)- Individual Data

Individual data of number of asymptomatic carriers with increase in hemoglobin levels by at least 0.5 g/dL from Day 1 to Day 28 from Community Screening Campaign 1 (CSC1) infants and children (>6 months and <5 years). Hemoglobin levels were measured using the HemoCue® rapid test. This test was performed with a drop of blood collected from the fingertip at Day 1 and at Day 28. (NCT01256658)
Timeframe: Day 1 to Day 28- period 1

Interventionparticipants (Number)
Intervention288
Control79

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Number of Asymptomatic Carriers With Increase in Hemoglobin Levels by at Least 0.5 g/dL From Day 1 to Day 28 of Community Screening Campaign 1 (CSC1) in Infants and Children (>6 Months and <5 Years)- Cluster Data

"Data is presented per cluster. Cluster data of number of asymptomatic carriers with increase in hemoglobin levels by at least 0.5 g/dL from Day 1 to Day 28 of Community Screening Campaign 1 (CSC1) in infants and children (>6 months and <5 years) was measured by Hemoglobin levels based on microscopy reading.~Mean and Standard Deviation (SD) percent were measured indicating the mean and SD of percentages of cluster frequencies under the study arm for that particular category." (NCT01256658)
Timeframe: Day 1 to day 28 - period 1

Interventionparticipants (Mean)
Intervention66.1
Control43.2

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Number of Symptomatic Malaria Episode, RDT-confirmed, With Parasitemia ≥5000/μL (SMRC5000s) Per Person-year in Infants and Children (<5 Years) in Post Community Screening Campaign (CSC) at Month 12 (Per Cluster)

"Data is presented per cluster. Number of Symptomatic malaria episode, RDT-confirmed, with parasitemia ≥5000/μL (SMRC5000s) per person-year in infants and children (<5 years) in post Community Screening Campaign (CSC) at month 12 was detected by Rapid Diagnostic Test (RDT) (using a blood sample from each participant) and later confirmed to have a parasite density ≥5000/uL by microscopy.~Number of SMRC5000: sum of all SMRC5000 for all infants and children (<5 years) in post CSC.~Person-year observed: sum of duration (in days) for all infants and children (<5 years) in post CSC present in study /365.25.~Number of SMRC5000 per person-year = number of SMRC5000/person-year observed." (NCT01256658)
Timeframe: Month 12 of period 1

InterventionSMRC5000 per person-year (Mean)
Intervention1.69
Control1.60

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Number of Symptomatic Malaria Episode, RDT-confirmed, With Parasitemia ≥5000/μL (SMRC5000s) Per Person-year in Post Community Screening Campaign (CSC)

"Number of Symptomatic malaria episode, RDT-confirmed, with parasitemia ≥5000/μL (SMRC5000s) per person-year in post Community Screening Campaign (CSC), by study arm (individual level data) was detected by Rapid Diagnostic Test (RDT) (using a blood sample from each participant) and later confirmed to have a parasite density ≥5000/uL by microscopy.~Number of SMRC5000: sum of all SMRC5000 for all subjects in post CSC. Person-year observed: sum of duration (in days) in post CSC for all subjects present in study /365.25.~Number of SMRC5000 per person-year = number of SMRC5000/person-year observed." (NCT01256658)
Timeframe: 12 months - period 1

InterventionSMRC5000 per person-year (Number)
Intervention0.45
Control0.39

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Anemia Status Based on Community Screening Campaign 1 (CSC1)/Day 1 in Infants and Children (>6 Months and <5 Years)

Anemia status based on Community Screening Campaign 1 (CSC1)/Day 1 in infants and children (>6 months and <5 years) was measured via hemoglobin levels using the HemoCue® rapid test. This test was performed using a drop of blood collected from the fingertip of each participant. The anemic status is defined as follows: hemoglobin (Hb) <5 g/dL = severe anemia, Hb 5 to <8 g/dL = moderate anemia, Hb 8 to <11 g/dL = mild anemia, Hb ≥11 g/dL = no anemia). (NCT01256658)
Timeframe: Day 1 (CSC1/day 1) - period 1

,
Interventionparticipants (Number)
CSC1/Day 1 SevereCSC1/Day 1 ModerateCSC1/Day 1 MildCSC1/Day 1 No symptoms
Control136195116
Intervention380458278

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Anemia Status Based on Community Screening Campaign 4 (CSC4)/Day 1 in Infants and Children (>6 Months and <5 Years)

Anemia status based on Community Screening Campaign 4 (CSC4/Day 1) in infants and children (>6 months and <5 years) was measured via hemoglobin levels using the HemoCue® rapid test. This test was performed using a drop of blood collected from the fingertip of each participant. The anemic status is defined as follows: hemoglobin (Hb) <5 g/dL = severe anemia, Hb 5 to <8 g/dL = moderate anemia, Hb 8 to <11 g/dL = mild anemia, Hb ≥11 g/dL = no anemia). (NCT01256658)
Timeframe: Month 12 (CSC4/day 1) - period 1

,
Interventionparticipants (Number)
CSC4/Day 1 SevereCSC4/Day 1 ModerateCSC4/Day 1 MildCSC4/Day 1 No
Control19117194
Intervention129349448

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Change in Hemoglobin Level (g/dL) From Community Screening Campaign 1 (CSC1)/Day 1 to CSC1/Day 28 in Infants and Children (>6 Months and <5 Years) for Asymptomatic Carriers at CSC1

Change in hemoglobin level (g/dL) from Community Screening Campaign 1 (CSC1)/Day 1 to CSC1/Day 28 in infants and children (>6 Months and <5 Years) for asymptomatic carriers at CSC1 was measured via hemoglobin levels using the HemoCue® rapid test. This test was performed using a drop of blood collected from the fingertip of each participant. The anemic status is defined as follows: hemoglobin (Hb) <5 g/dL = severe anemia, Hb 5 to <8 g/dL = moderate anemia, Hb 8 to <11 g/dL = mild anemia, Hb ≥11 g/dL = no anemia). (NCT01256658)
Timeframe: Day 1 and day 28 - period 1

,
Interventiong/dL (Mean)
CSC1/Day 1 (n=432 ; 179 )CSC1/Day 28 (n=406 ; 174 )
Control9.6710.17
Intervention9.7810.95

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Change in Hemoglobin Level (g/dL) From Community Screening Campaign 1(CSC1)/Day 1 to Community Screening Campaign 4 (CSC4)/Day 1 (Per Cluster)

"Data is presented per cluster. Comparison of hemoglobin level (g/dL) from Community Screening Campaign 1 (CSC1)/Day 1 to Community Screening Campaign 4 (CSC4)/Day 1 in infants and children (>6 months and <5 years) by study arm was measured using the HemoCue® rapid test. This test was performed using a drop of blood collected from the fingertip of each participant." (NCT01256658)
Timeframe: Day 1 (CSC1/day 1) and month 12 (CSC4/day 1) - period 1

,
Interventiong/dL (Mean)
CSC1/Day 1 (n= 819, 827)CSC4/Day 1 (n= 348,321)
Control10.0411.13
Intervention10.2410.99

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Change in Hemoglobin Level (g/dL) in Asymptomatic Carriers >6 Months of Age (Per Cluster)

"Data is presented per cluster. Change in hemoglobin levels from day 1 to day 28 was measured using the HemoCue® rapid test. This test was performed using a drop of blood collected from the fingertip of each asymptomatic carrier from Community Screening Campaign 1 (CSC1), > 6 months of age, at day 1 and at day 28." (NCT01256658)
Timeframe: Day 1 and day 28 of period 1

,
Interventiong/dL (Mean)
Day 1 (n = 2387, 2116)Day 28 (n = 1136, 1091)
Control12.0611.86
Intervention11.8112.33

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Cumulative Number of Subjects With Symptomatic Malaria Episode, RDT-confirmed, With Parasitemia ≥5000/μL From Week 1 to Week 50

"Cumulative number of asymptomatic carriers having Symptomatic malaria episode, RDT-confirmed, with parasitemia ≥5000/μL (SMRC5000) from Week 1 to Week 50, was measured from group of participants diagnosed as asymptomatic carriers at Community Screening Campaign (CSC1)/Day1. Number of participants affected before and after diagnosed with ≥1 symptomatic malaria episode, RDT-confirmed, with parasitemia ≥5000/μL (SMRC5000) (complicated and uncomplicated episodes combined). Number of SMRC5000s was detected by Rapid Diagnostic Test (RDT) using a blood sample from each participant and later confirmed to have a parasite density > or = 5000/uL by microscopy.~Week (1-2) indicates day1 to day14, week (3-4) indicates day 15 to day 28, week (5-6) indicates day 29 to day 42, etc. After first diagnosis of asymptomatic carriers at CSC1/Day1." (NCT01256658)
Timeframe: Week 1 to Week 50

,
Interventionparticipants (Number)
Week (1-2) n at risk= 2397, 1138Week (3-4) n at risk= 2396, 1133Week (5-6) n at risk= 2391, 1129Week (7-8) n at risk= 2390, 1124Week (9-10) n at risk= 2390, 1123Week (11-12) n at risk= 2390, 1121Week (13-14) n at risk= 2390, 1103Week (15-16) n at risk= 2390, 1102Week (17-18) n at risk= 2390, 1102Week (19-20) n at risk= 2390, 1102Week (21-22) n at risk= 2337, 1083Week (23-24) n at risk= 2311, 1077Week (25-26) n at risk= 2246, 1063Week (27-28) n at risk= 2148, 1041Week (29-30) n at risk= 2047, 1020Week (31-32) n at risk= 1979, 996Week (33-34) n at risk= 1931, 979Week (35-36) n at risk= 1894, 968Week (37-38) n at risk= 1868, 956Week (39-40) n at risk= 1837, 935Week (41-42) n at risk= 1816, 927Week (43-44) n at risk= 1805, 920Week (45-46) n at risk= 1785, 913Week (47-48) n at risk= 1773, 910Week (49-50) n at risk= 1758, 904
Control4812131517181818202438597998114121130144149154158159161161
Intervention13444444473092188287347391421440460477483486490492493

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Hemoglobin Level (g/dL) in Community Screening Campaign 1 (CSC1)/Day 1 and CSC4/Day 1 by Study Arm and Age Group (Per Cluster)

"Data is presented per cluster. Hemoglobin levels at Community Screening Campaign 1 and 4 (CSC1 and CSC4) on day 1 per age group (5-9 years, 10-14 years, and ≥15 years) in the intervention versus the control arm was measured using the HemoCue® rapid test. This test was performed using a drop of blood collected from the fingertip of each participant." (NCT01256658)
Timeframe: Day 1 (CSC1/day 1) and month 12 (CSC4/day 1) - period 1

,
Interventiong/dL (Mean)
CSC1 5- 9 years (n= 899, 431)CSC4 5 - 9 years (n= 900, 396)CSC1 10 - 14 years (n= 873, 380)CSC4 10 - 14 years (n= 837, 359)CSC1 >= 15 years (n= 2904, 1279)CSC4 >= 15 years (n= 2760, 1136)
Control11.5912.1312.7112.7213.4913.42
Intervention11.6311.9712.3212.5813.1313.25

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Microscopy-confirmed Gametocyte Carriers at Community Screening Campaign 4 (CSC4) (Per Cluster)

"Data is presented per cluster. Microscopy confirmed gametocyte carriers at Community Screening Campaign 4(CSC4) were assessed via microscopy at month 12 of period 1. Blood films were histologically treated and examined microscopically." (NCT01256658)
Timeframe: Month 12 - period 1

Interventionparticipants (Mean)
Intervention4.9
Control5.1

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Mean of Microscopy-confirmed Asymptomatic Carriers From Community Screening Campaigns 1, 2, 3 and 4 (CSC1, CSC2, CSC3 and CSC4) (Per Cluster)

"Data is presented per cluster. Mean number of asymptomatic carriers from Community Screening Campaigns 1, 2, 3 and 4 (CSC1, CSC2, CSC3 and CSC4) was measured by confirmed positive microscopy for P. falciparum asexual forms in participants with absence of clinical signs and symptoms of malaria.~Mean measured in this analysis is the mean percent indicting the mean of percentages of cluster frequencies under the study arm for that particular category." (NCT01256658)
Timeframe: 12 months - period 1

,
Interventionparticipants (Mean)
CSC1/ day 1 (n= 2428, 1153)CSC2/ day 1 (n= 237, 833)CSC3/ day 1 (n= 171, 741)CSC4/ day 1 (n= 2023, 815)
Control47.535.732.237.8
Intervention42.84.12.834.4

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Number of Asymptomatic Carriers With Complicated and Uncomplicated Episodes Combined

Number of asymptomatic carriers diagnosed with 1 Symptomatic malaria episode, RDT-confirmed, with parasitemia ≥5000/μL (SMRC5000), 2 SMRC5000, 3 SMRC5000 and >3 SMRC5000 (complicated and uncomplicated episodes combined). Number of SMRC5000s is measured by Rapid diagnostic test (RDT) and later confirmed to have a parasite density ≥ 5000/uL by microscopy. (NCT01256658)
Timeframe: 12 months - period 1

,
Interventionparticipants (Number)
1 SMRC50002 SMRC50003 SMRC5000>3 SMRC5000
Control13638125
Intervention413963417

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Number of Microscopy and qRT-PCR-confirmed Gametocyte Carriers at Community Screening Campaign 4 (CSC4)

Number of gametocyte carriers at Community Screening Campaign 4 (CSC4) was measured via microscopy and confirmed using Quantitative Reverse Transcription PCR (qRT-PCR) at day 1 of CSC4. (NCT01256658)
Timeframe: Month 12 (CSC4/day 1) - period 1

,
Interventionparticipants (Number)
PositiveNegativeNot evaluable
Control4625113
Intervention5085141

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Number of Participants (Infants and Children (> 6 Months and < 5 Years)) With Hospitalizations, Severe Malaria Episodes or Death Post Community Screening Campaign (CSC)

Total number of participants (infants and children (> 6 months and < 5 years)) with hospitalizations, severe malaria episodes or death after Community Screening Campaign (CSC) was assessed. (NCT01256658)
Timeframe: 12 months - period 1

,
Interventionparticipants (Number)
HospitalizationsSevere malaria episodesDeath
Control2152
Intervention2042

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Number of Participants With Hospitalizations, Severe Malaria Episodes or Death Post Community Screening Campaign (CSC)

Total number of participants (all ages) with hospitalizations, severe malaria episodes or death after Community Screening Campaign (CSC) was assessed. (NCT01256658)
Timeframe: 12 months - period 1

,
Interventionparticipants (Number)
HospitalizationsSevere malaria episodesDeath
Control57931
Intervention681031

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Number of Symptomatic Malaria Episode, RDT-confirmed, With Parasitemia ≥5000/μL (SMRC5000) in Asymptomatic Carriers at Any Time of Diagnosis (Per Cluster)

"Data is presented per cluster. Number of Symptomatic malaria episode, RDT-confirmed, with parasitemia ≥5000/μL (SMRC5000) in asymptomatic carriers by study arm from all inhabitants diagnosed at any time for asymptomatic carriers. Number of SMRC5000s is measured by Rapid diagnostic test (RDT) and later confirmed to have a parasite density ≥ 5000/uL by microscopy." (NCT01256658)
Timeframe: 12 months - period 1

,
Interventionpercentage of participants (Mean)
1 SMRC50002 SMRC50003 SMRC5000>3 SMRC5000
Control9.492.780.970.31
Intervention15.253.561.280.67

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Mean Number of Microscopy-confirmed Gametocyte Carriers at Day 1 of Community Screening Campaign 1,2,3,4 (CSC1, CSC2, CSC3 and CSC4) (Per Cluster)

"Data is presented per cluster. Mean number of gametocyte carriers at Day 1 for Community Screening Campaign 1,2,3,4 (CSC1, CSC2, CSC3 and CSC4) was measured using gametocyte assessments (prevalence and density) via microscopy.~Mean measured in this analysis is the mean percent indicating the mean of percentages of cluster frequencies under the study arm for that particular category." (NCT01256658)
Timeframe: 12 months - period 1

,
Interventionparticipants (Mean)
CSC1/Day 1 (n= 543, 246)CSC2/Day 1 (n= 33, 130)CSC3/Day 1 (n= 23, 144)CSC4/Day 1 (n= 279, 113)
Control10.25.55.85.1
Intervention9.50.60.44.8

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Percentage of Microscopy-confirmed Gametocyte Carriers Treated With COA566 for Asymptomatic Carriers

Percentage of microscopy-confirmed gametocyte asymptomatic carriers treated with COA566 for asymptomatic carriers in Community Screening Campaign 1, 2 and 3 (CSC1, CSC2 and CSC3). (NCT01256658)
Timeframe: Day 1, day 7 and day 28 - period 1

Interventionpercentage of participants (Number)
CSC1 Day 1 (n= 3045)CSC 1 Day 7 (n= 3045)CSC 1 Day 28 (n= 3045)CSC2 Day 1 (n= 850)CSC2 Day 7 (n= 850)CSC3 Day 1 (n= 75)CSC3 Day 7 (n= 75)
Intervention15.71.40.12.60.14.00

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Percentage of COA566-treated Microscopy-confirmed Asymptomatic Carriers at Community Screening Campaign 1, 2 and 3 (CSC1, CSC2 and CSC3) With Parasitological Cure Rate at Day 7

Percentage of participants with parasitological cure confirmed via microscopy at day 7 after treatment with COA566. This assessment was done on asymptomatic carriers from Community Screening Campaigns 1, 2 and 3 (CSC1, CSC2 and CSC3) from the intervention group only. (NCT01256658)
Timeframe: Day 7 of CSC1, CSC2 and CSC3 - period 1

Interventionpercentage of participants (Number)
CSC1 (n= 2151)CSC2 (n=182)CSC3 (n=117)
Intervention99.510096.7

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Parasite Clearance Time (PCT) [MITT Population]

Parasite clearance time (PCT). Time in hours from the initiation of therapy until the first of two successive parasite negative smears (zero parasite counts) are obtained (NCT01258049)
Timeframe: 28 days after start of treatment

Interventionhours (Mean)
ArTiMist30.29
Quinine68.30

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PCT 50 [MITT Population]

Time for parasite counts to fall by 50% (NCT01258049)
Timeframe: 28 days after start of treatment

Interventionhours (Mean)
ArTiMist9.42
Quinine18.58

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PCT 90 [MITT Population]

Time for parasite counts to fall by 90% (NCT01258049)
Timeframe: 28 days after start of treatment

Interventionhours (Mean)
ArTiMist15.02
Quinine27.93

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PRR 12 [MITT Population]

The percentage reduction in parasite counts 12 hours after first dose (NCT01258049)
Timeframe: 28 days after start of treatment

Interventionpercentage of baseline (Mean)
ArTiMist47.6
Quinine-132.2

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PRR 24 [MITT Population]

The percentage reduction in parasite counts 24 hours after first dose (NCT01258049)
Timeframe: 28 days after start of treatment

Interventionpercentage of baseline (Mean)
ArTiMist98.2
Quinine44.5

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Time to Return to Full Consciousness

"Time in hours to return to full consciousness (Blantyre Coma Scale = 5), if level of consciousness is reduced (Blantyre Coma Scale <5) prior to dosing or within 24hours of first dosing.~For the Blantyre Coma Scale~Total - maximum 5, eye movement - maximum 1, best motor response - maximum 2, best verbal response - maximum 2" (NCT01258049)
Timeframe: 28 days after start of treatment

Interventionhours (Mean)
ArTiMist20.8
Quinine23.0

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Time to Return to Normal Per os Status

Time in hours to return to normal per os status. Normal per os was when the investigator considered the patient to be able to eat and drink normally. (NCT01258049)
Timeframe: 28 days after start of treatment

Interventionhours (Mean)
ArTiMist22.1
Quinine25.3

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Complete Cure Rate

The complete resolution of clinical signs and symptoms, malaria-related laboratory abnormalities, and elimination of asexual parasites by Day 7, with no recurrence up to Day 28 (+/- 2 days), and the 48h parasite count to be < 25% of baseline with no clinical deterioration (NCT01258049)
Timeframe: 28 days after the start of treatment

,
Interventionparticipants (Number)
CureNo Cure
ArTiMist4114
Quinine4617

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Parasitological Success (MITT)

Parasitological success defined as a reduction in parasite count of ≥ 90% of baseline at 24 hours after the first dose (NCT01258049)
Timeframe: 24 hours after start of treatment

,
Interventionparticipants (Number)
SuccessNot Success
ArTiMist664
Quinine2843

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Parasitological Success (PP)

Parasitological success defined as a reduction in parasite count of ≥ 90% of baseline at 24 hours after the first dose (NCT01258049)
Timeframe: 24 hours after start of treatment

,
Interventionparticipants (Number)
SuccessNot Success
ArTiMist653
Quinine2841

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Early Treatment Failure

"Early treatment failure is indicated by one or more of the following:~Parasite count on Day 2 > Day 0, irrespective of temperature~Parasite count on Day 3 > 0 with tympanic temperature ≥ 38.0°C~Parasite count on Day 3 ≥ 25% of baseline~Administration of rescue antimalarial treatment" (NCT01258049)
Timeframe: Three days after the start of treatment

Interventionparticipants (Number)
ArTiMist0
Quinine14

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Fever Clearance Time (FCT)

Time in hours from the initiation of therapy until the disappearance of fever (tympanic temperature < 38.0) that lasted at least 24 hours. (NCT01258049)
Timeframe: 28 days after start of treatment

Interventionhours (Mean)
ArTiMist42.6
Quinine41.6

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Late Clinical Failure

"Signs of severe malaria on any day between Day 4 and Day 28 in the presence of parasitaemia, without previously meeting any of the criteria of early treatment failure~Presence of parasitaemia and tympanic temperature ≥ 38.0°C (or history of fever), on any day between Day 4 and Day 28, without previously meeting any of the criteria of early treatment failure" (NCT01258049)
Timeframe: 28 days after the start of treatment

Interventionparticipants (Number)
ArTiMist3
Quinine1

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Late Parasitological Failure

o Parasitaemia on any day from Day 7 to Day 28 and tympanic temperature ≤ 38.0°C (NCT01258049)
Timeframe: 28 days after the start of treatment

Interventionparticipants (Number)
ArTiMist12
Quinine14

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Number of Deaths or Neurological Sequelae at Day 28

(NCT01258049)
Timeframe: 28 days after start of treatment

Interventionparticipants (Number)
ArTiMist0
Quinine0

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Number of Participants With Treatment Emergent Adverse Events and Serious Adverse Events, of Possible, Probably and Definite Causalities

(NCT01258049)
Timeframe: 28 days after start of treatment

Interventionparticipants (Number)
ArTiMist5
Quinine6

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Time to Parasite Clearance (PCT)

Time from first dose until first total and continued disappearance of asexual parasite forms which remains at least a further 48 hours. (NCT01619878)
Timeframe: Up to 7 days

Interventionhours (Mean)
Cohort 129.1

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Time to Gametocyte Clearance (GCT)

Time from first dose until first total and continued disappearance of gametocytes which remains at least a further 48 hours. (NCT01619878)
Timeframe: Up to 7 days

Interventionhours (Mean)
Cohort 136.32

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Time to Fever Clearance (FCT)

Time from first dose to the first time the axillary body temperature decreased below and remained below 37.5° C for at least 48 hours. (NCT01619878)
Timeframe: Up to 7 days

Interventionhours (Mean)
Cohort 14.02

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Polymerase Chain Reaction (PCR) Corrected 28 Day Parasitological Cure Rate

Number of participants with clearance of asexual parasites by day 7 after initiating study treatment without recrudescence at day 28, corrected for re-infection by Polymerase Chain Reaction (PCR) assay. (NCT01619878)
Timeframe: 28 days

Interventionnumber of participants (Number)
Cohort 116

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Percent Change of Parasite Count From Baseline at 24 Hours

Percent change of parasite count from baseline at 24 hours (NCT01619878)
Timeframe: baseline, 24 hours

InterventionPercent Change (Mean)
Cohort 1-99.4

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Number of Participants With Parasitaemia at 72 Hours After Treatment Initiation Greater Than or Equal to 25 Percent of Count at Baseline

Number of participants with parasite density at 72 hours after treatment initiation greater than or equal to 25 percent of parasite density at baseline. (NCT01619878)
Timeframe: 72 hours

Interventionparticipants (Number)
Cohort 10

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Number of Participants With Parasitaemia at 48 Hours After Treatment Initiation Greater Than at Baseline

Number of participants with parasite density at 48 hours after treatment initiation greater than parasite density at baseline. (NCT01619878)
Timeframe: 48 hours

Interventionparticipants (Number)
Cohort 10

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Polymerase Chain Reaction (PCR) Corrected Parasitological Cure Rate at Day 14 and 42

Number of participants with clearance of asexual parasites by day 7 after initiating study treatment without recrudescence at day 14 and day 42, corrected for re-infection by Polymerase Chain Reaction (PCR) assay. (NCT01619878)
Timeframe: Day 14 and 42

InterventionNumber of participants (Number)
Day 14Day 42
Cohort 11616

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Number of Participants With Parasitological Uncorrected Cure Rate at Day 3, 7, 14, 28 and 42

Number of patients with clearance of asexual parasites at day 3, 7, 14, 28 and 42 after initiating study treatment. (NCT01619878)
Timeframe: Day 3, 7, 14, 28 and 42

Interventionparticipants (Number)
Day 3Day 7Day 14Day 28Day 42
Cohort 1201616107

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Change From Baseline in Respiratory Rate to End of Study (EOS)

(NCT02223871)
Timeframe: Day 28 (EOS)

InterventionBreaths/min (Median)
Respiratory rate at baseline (Day 0)Respiratory rate at EOS (Day 28)Change from Day 0 to Day 28 in respiratory rate
ACT-451840 500 mg14161.5

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Drug-specific Parasite Reduction Ratio (PRR48) of ACT-451840 Over 48 Hours Using a New Approach

"After the blood stage Plasmodium falciparum challenge (BSPC), malaria parasitemia was measured by polymerase chain reaction (PCR) in regularly collected blood samples.~The subject-specific and drug-specific parasite reduction rates over a 48 h period (PRR48) were calculated following the data-driven method by Marquart et al. (2015), removing potential lag and tail phases prior to log-linear regression modeling." (NCT02223871)
Timeframe: 48 hours after study drug administration

InterventionRatio (Mean)
ACT-451840 500 mg73.6

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Drug-specific Parasite Reduction Ratio (PRR48) of ACT-451840 Over 48 Hours Using a Standardized Approach

"After the blood stage Plasmodium falciparum challenge (BSPC), malaria parasitemia was measured by polymerase chain reaction (PCR) in regularly collected blood samples.~The subject-specific and drug-specific parasite reduction rates over a 48 h period (PRR48) were calculated using an objective standardized approach (observed data over 48 h)" (NCT02223871)
Timeframe: 48 hours after study drug administration

InterventionRatio (Mean)
ACT-451840 500 mg234.5

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Maximum Plasma Concentration (Cmax) of ACT-451840

Cmax was directly derived from the plasma concentrations-time curves of ACT-451840. Blood samples for pharmacokinetic characterization were drawn at pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 48, 72, 96, and 144 hours post-dose. (NCT02223871)
Timeframe: From pre-dose to 144 hours after study drug adminsitration

Interventionng/mL (Geometric Mean)
ACT-451840 500 mg121.7

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Terminal Half-life [t(1/2)]

Blood samples for pharmacokinetic characterization were drawn at pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 48, 72, 96, and 144 hours post-dose (NCT02223871)
Timeframe: From pre-dose to144 hours after study drug adminsitration

InterventionHours (Geometric Mean)
ACT-451840 500 mg36.4

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Time to Reach Maximum Plasma Concentration (Tmax) of ACT-451840

tmax was directly derived from the plasma concentration-time curves of ACT-451840. Blood samples for pharmacokinetic characterization were drawn at pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 48, 72, 96, and 144 hours post-dose. (NCT02223871)
Timeframe: From pre-dose to144 hours after study drug administration

InterventionHours (Median)
ACT-451840 500 mg4.0

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Areas Under the Plasma Concentration-time Curve of ACT-451840

"Two AUCs were calculated using non-compartmental analysis: AUC(0-t) from pre-dose to last time-point of measure and AUC(0-inf) from pre-dose and extrapolated to infinity.~Blood samples for pharmacokinetic characterization were drawn at pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 48, 72, 96, and 144 hours post-dose" (NCT02223871)
Timeframe: From pre-dose to144 hours after study drug administration

Interventionng*h/mL (Geometric Mean)
AUC(0-t)AUC(0-inf)
ACT-451840 500 mg1254.81284.4

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Change From Baseline in Blood Pressure to End of Study (EOS)

Vital signs, including diastolic and systolic blood pressure (DBP/SBP), were measured at each outpatient visit up to 7 days after ACT-451840 administration, every day during confinement or when malaria symptoms were presented and at the end of study visit (EOS). Other measures were performed if required. (NCT02223871)
Timeframe: Day 28 (EOS)

InterventionmmHg (Median)
SBP at baseline (Day 0)SBP at EOS (Day 28)Change from Day 0 to Day 28 in SBPDBP at baseline (Day 0)DBP at EOS (Day 28)Change from Day 0 to Day 28 in DBP
ACT-451840 500 mg121.0125.52.566.070.50.5

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Change From Baseline in Body Temperature up to End of Study (EOS)

Body temperature was measured orally (NCT02223871)
Timeframe: Day 28 (EOS)

InterventionDegree Celsius (Median)
Temperature at baseline (Day 0)Temperature at EOS (Day 28)Change from Day 0 to Day 28 in temperature
ACT-451840 500 mg36.335.9-0.2

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Recurrence of Parasitaemia Within 16 Days of Follow up

(NCT02389374)
Timeframe: day 16

InterventionRecurrences of Parsitaemia (Number)
Chloroquine Primaquine 14days0
Artemether-lumefantrine Primaquine 1day0
Artemether-lumefantrine Primaquine 14days0

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Fractional Change in Hb Between Baseline and Day 9 and 16

(NCT02389374)
Timeframe: day 0 and 16

,,
Interventionpercent change Hb (Mean)
baseline to day 9baseline to day 16
Artemether-lumefantrine Primaquine 14days-13.8-8.3
Artemether-lumefantrine Primaquine 1day-7.7NA
Chloroquine Primaquine 14days-2.3-0.5

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The Proportion of Adverse and Serious Adverse Events Following Unsupervised Primaquine Treatment

The proportion of adverse and serious adverse events following unsupervised primaquine treatment until day 28 (NCT02389374)
Timeframe: during follow up (day 28)

Interventionevents (Number)
Chloroquine Primaquine 14days0
Artemether-lumefantrine Primaquine 1day0
Artemether-lumefantrine Primaquine 14days0

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The Distribution of G6PD Activity Measured in U/gHb Among All Malaria Patients

(NCT02389374)
Timeframe: day 0

InterventionU/gHb (Median)
All Malaria Patients7.82

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Proportion of Patients With Fever on Day 2 After Treatment

(NCT02389374)
Timeframe: day 2

InterventionParticipants (Count of Participants)
Chloroquine Primaquine 14days0
Artemether-lumefantrine Primaquine 1day0
Artemether-lumefantrine Primaquine 14days0

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Proportion of Patients With Any Parasitemia on Day 3 After Treatment

(NCT02389374)
Timeframe: day 3

Interventionparticipants (Number)
Chloroquine Primaquine 14days0
Artemether-lumefantrine Primaquine 1day2
Artemether-lumefantrine Primaquine 14days0

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Proportion of Patients With Anaemia Less Than 8g/dl on Day 2

(NCT02389374)
Timeframe: on day 2

Interventionparticipants with Hb under 8g/dl (Number)
Chloroquine Primaquine 14days0
Artemether-lumefantrine Primaquine 1day2
Artemether-lumefantrine Primaquine 14days0

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Proportion of Patients Receiving Blood Transfusion and With Severe Anaemia (Hb<7g/dl)

(NCT02389374)
Timeframe: day 28

Interventionparticipants (Number)
Chloroquine Primaquine 14days0
Artemether-lumefantrine Primaquine 1day0
Artemether-lumefantrine Primaquine 14days0

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Proportion of Patients Adhering to 14 Days of Primaquine Treatment in the Vivax Cohort as Measured by Pill Count

(NCT02389374)
Timeframe: day 16

InterventionParticipants (Count of Participants)
Chloroquine Primaquine 14days34
Artemether-lumefantrine Primaquine 1dayNA
Artemether-lumefantrine Primaquine 14days7

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Absence of Malaria Parasites in Blood.

Investigators will evaluate the percentage of patients who remain free of malaria parasites in the blood during the 28-day follow-up period. (NCT02600767)
Timeframe: 28 days

InterventionParticipants (Count of Participants)
Artemether-Lumefantrine73

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Half-life (T^1/2)

Half-life (T^1/2) (NCT03334747)
Timeframe: Upto day 15 post dose

,,
InterventionHour (Mean)
Day 1Day 3
KAE609 10 mg QD 3 Days18.532.4
KAE609 25 mg QD 3 Days17.430.1
KAE609 50 mg QD 3 Days32.829.9

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Maximum Peak Observed Concentration (Cmax)

Maximum Peak Observed Concentration (Cmax) (NCT03334747)
Timeframe: Day 1, Day 3

,,,,
Interventionng/mL (Geometric Mean)
Day 1
KAE609 75 mg SD1270
KAE609 10 mg SD179
KAE609 150 mg SD2360
KAE609 50 mg SD773
KAE609 25 mg SD379

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Percentage of Participants With Polymerase Chain Reaction (PCR)-Corrected and Uncorrected Adequate Clinical and Parasitological Response (ACPR) at Day 15 and Day 29

PCR-corrected and PCR-uncorrected were evaluated at Days 15 and 29 (i.e., 14 and 28 days post-dose). The presence of parasitaemia after 7 days due to reinfection was considered as PCR-corrected ACPR. Missing blood smear data at Day 15 visit and thereafter were not considered as responder for the visit unless there was a later blood smear test indicating no parasitaemia. (NCT03334747)
Timeframe: Day 15, Day 29

,,,,,,,,
InterventionPercentage of Participants (Number)
Day 15: PCR correctedDay 15: PCR uncorrectedDay 29: PCR correctedDay 29: PCR uncorrected
KAE609 10 mg QD 3 Days90.090.090.090.0
KAE609 10 mg SD90.090.080.080.0
KAE609 150 mg SD77.377.368.259.1
KAE609 25 mg QD 3 Days95.095.090.080.0
KAE609 25 mg SD83.383.383.366.7
KAE609 50 mg QD 3 Days84.284.273.768.4
KAE609 50 mg SD95.295.285.781.0
KAE609 75 mg SD90.585.781.071.4
Pooled Coartem Control96.196.194.192.2

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Maximum Peak Observed Concentration (Cmax)

Maximum Peak Observed Concentration (Cmax) (NCT03334747)
Timeframe: Day 1, Day 3

,,
Interventionng/mL (Geometric Mean)
Day 1Day 3
KAE609 25 mg QD 3 Days503655
KAE609 50 mg QD 3 Days8281210
KAE609 10 mg QD 3 Days185235

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Fever Clearance Time (FCT)

Fever Clearance Time (FCT) is defined as the time from the first dose until the first time the axillary body temperature decreased below and remained below 37.5°C axillary or 38.0°C oral/tympanic/rectal for at least a further 24 hours. In case a patient received rescue medication before (fever) clearance, the time to event was censored at the first use of rescue medication. (NCT03334747)
Timeframe: Day 29

InterventionHours (Mean)
KAE609 10 mg SD3.9
KAE609 10 mg QD 3 Days2.0
KAE609 25 mg SDNA
KAE609 25 mg QD 3 Days22.0
KAE609 50 mg SD2.4
KAE609 50 mg QD 3 Days7.2
KAE609 75 mg SD5.7
KAE609 150 mg SD9.9
Pooled Coartem Control13.0

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Tmax

Tmax (NCT03334747)
Timeframe: Day 1, Day 3

,,
InterventionHour (Median)
Day 1Day 3
KAE609 10 mg QD 3 Days3.9252.7
KAE609 25 mg QD 3 Days4.2552.1
KAE609 50 mg QD 3 Days4.1252.0

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Tmax

Tmax (NCT03334747)
Timeframe: Day 1, Day 3

,,,,
InterventionHour (Median)
Day 1
KAE609 10 mg SD4.00
KAE609 150 mg SD8.07
KAE609 25 mg SD4.01
KAE609 50 mg SD4.12
KAE609 75 mg SD6.01

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Time to Recrudescence and Reinfection at Study Day 29

Time to recrudescence is calculated from the date of first study medication to the date of first event. Participants without recrudescence/reinfection after Day 7 are censored at the time of treatment failure or at the time of last parasite assessment if no treatment failure occured. (NCT03334747)
Timeframe: Day 29

,,,,,,
InterventionEvent probability (Number)
RecrudescenceReinfection
KAE609 150 mg SD32.513.3
KAE609 25 mg QD 3 Days10.014.3
KAE609 25 mg SD16.725.0
KAE609 50 mg QD 3 Days26.310.0
KAE609 50 mg SD16.05.0
KAE609 75 mg SD15.910.3
Pooled Coartem Control2.42.4

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Time to Recrudescence and Reinfection at Study Day 29

Time to recrudescence is calculated from the date of first study medication to the date of first event. Participants without recrudescence/reinfection after Day 7 are censored at the time of treatment failure or at the time of last parasite assessment if no treatment failure occured. (NCT03334747)
Timeframe: Day 29

,
InterventionEvent probability (Number)
Recrudescence
KAE609 10 mg QD 3 Days10.0
KAE609 10 mg SD12.5

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Number of Participants With at Least 2 CTCAE Grades Increase From Baseline in Alanine Aminotransferase (ALT) or Aspartate Aminotransferase (AST)

The occurrence of at least 2 CTCAE grades increase from baseline in ALT or AST during the 4 weeks study period was evaluated to characterize hepatic safety aspects of single and multiple ascending doses of KAE609 in adult malaria subjects for treatment of uncomplicated malaria caused by plasmodium falciparum. If 2 patients in a 10 patient cohort (Cohorts 1 and 2) or 3 patients in a 20 patient cohort (Cohorts 3, 4 and 5) had at least 2 CTCAE grades increase from Baseline in ALT or AST, recruitment was suspended and a review of liver safety (and any other relevant data) by safety review committee was initiated. Any further progression of the study was based on the decision by the safety review committee. (NCT03334747)
Timeframe: Day 29

InterventionPercentage of Participants (Number)
KAE609 10 mg SD11.1
KAE609 10 mg QD 3 Days0
KAE609 25 mg SD0
KAE609 25 mg QD 3 Days0
KAE609 50 mg SD0
KAE609 50 mg QD 3 Days0
KAE609 75 mg SD0
KAE609 150 mg SD4.5
Pooled Coartem Control3.9

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Parasite Clearance Time (PCT)

Parasite Clearance Time (PCT) is defined as the time from the first dose until the first total and continued disappearance of asexual parasite forms which remained at least a further 48 hours. In case a patient received rescue medication before (parasite) clearance, the time to event was censored at the first use of rescue medication. (NCT03334747)
Timeframe: Day 29

InterventionHours (Mean)
KAE609 10 mg SD26.8
KAE609 10 mg QD 3 Days27.7
KAE609 25 mg SD14.0
KAE609 25 mg QD 3 Days11.4
KAE609 50 mg SD11.1
KAE609 50 mg QD 3 Days9.8
KAE609 75 mg SD8.7
KAE609 150 mg SD8.0
Pooled Coartem Control36.2

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AUC0-24

AUC0-24 (NCT03334747)
Timeframe: Day 1, Day 3

,,,,
Interventionh*ug/mL (Geometric Mean)
Day 1
KAE609 10 mg SD2.77
KAE609 150 mg SD40.4
KAE609 25 mg SD5.14
KAE609 50 mg SD11.6
KAE609 75 mg SD21.4

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AUC0-24

AUC0-24 (NCT03334747)
Timeframe: Day 1, Day 3

,,
Interventionh*ug/mL (Geometric Mean)
Day 1Day 3
KAE609 10 mg QD 3 Days2.593.90
KAE609 25 mg QD 3 Days8.3910.9
KAE609 50 mg QD 3 Days15.621.6

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Half-life (T^1/2)

Half-life (T^1/2) (NCT03334747)
Timeframe: Upto day 15 post dose

,,,,
InterventionHour (Mean)
Day 1
KAE609 10 mg SD24.4
KAE609 150 mg SD29.9
KAE609 25 mg SD35.1
KAE609 50 mg SD31.5
KAE609 75 mg SD25.3

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Number of Participants With Local and Systemic Adverse Events in Year Two

Incidence of local and systemic adverse events (AEs) graded by severity occurring within 7 days after vaccine administration during year two (booster dose) (NCT03510481)
Timeframe: Within 7 days after each vaccination in year two

InterventionParticipants (Count of Participants)
Experimental Arm 1: Dosing Interval 0, 8, 16, and 54 Weeks5
Experimental Arm 2: Dosing Interval 0, 1, 4, and 42 Weeks12
Placebo Comparator 3a: Dosing Interval 0, 8, 16, and 54 Weeks3
Placebo Comparator 3b: Dosing Interval 0, 1, 4, and 42 Weeks2

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Number of Participants With Local and Systemic Adverse Events in Year One

Incidence of local and systemic adverse events (AEs) graded by severity occurring within 7 days after each vaccine administration in year one (NCT03510481)
Timeframe: Within 7 days after each vaccination in year one

InterventionParticipants (Count of Participants)
Experimental Arm 1: Dosing Interval 0, 8, 16, and 54 Weeks39
Experimental Arm 2: Dosing Interval 0, 1, 4, and 42 Weeks27
Placebo Comparator 3a: Dosing Interval 0, 8, 16, and 54 Weeks19
Placebo Comparator 3b: Dosing Interval 0, 1, 4, and 42 Weeks11

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Frequency of Adverse Events After NF135.C10 CPS Immunization

The number of adverse events will be recorded by the trial clinicians for all participants. (NCT03813108)
Timeframe: Cohort A: Inclusion until 35 days after challenge infection (35 weeks) Cohort B: Inclusion - premature end of study (22 weeks)

InterventionAdverse events (Number)
1: NF135 CPS-immunization Challenged by NF135139
2: Low Dose NF135 CPS-immunization Challenged by NF135173
3: NF135 CPS-immunization (A/L) Cohort B172

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Magnitude of Adverse Events After NF135.C10 CPS Immunization

The severity of adverse events will be recorded (mild/moderate/severe) for each adverse event (NCT03813108)
Timeframe: Cohort A: Inclusion until 35 days after challenge infection (35 weeks) Cohort B: Inclusion - premature end of study (22 weeks)

,,
InterventionAdverse events (Number)
Mild adverse events (grade 1)Moderate adverse events (grade 2)Severe adverse events (grade 3)Serious adverse events (grade 4)
1: NF135 CPS-immunization Challenged by NF13510820110
2: Low Dose NF135 CPS-immunization Challenged by NF13512835100
3: NF135 CPS-immunization (A/L) Cohort B12131191

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Break Through Infections

Number of subjects that required rescue treatment with atovaquone/proguanil due to a positive thick smear in combination with symptoms following NF135.C10 immunizations despite mefloquine prophylaxis (Cohort A) or presumptive artemether/lumefantrine treatment (Cohort B). (NCT03813108)
Timeframe: From day 0 until 28 days after each immunization (28 days)

,
Interventionparticipants (Number)
Break through following immunization 1Break through following immunization 2Break through following immunization 3
1: NF135 CPS-immunization Challenged by NF1351034
2: Low Dose NF135 CPS-immunization Challenged by NF1351035

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Break Through Infections

Number of subjects that required rescue treatment with atovaquone/proguanil due to a positive thick smear in combination with symptoms following NF135.C10 immunizations despite mefloquine prophylaxis (Cohort A) or presumptive artemether/lumefantrine treatment (Cohort B). (NCT03813108)
Timeframe: From day 0 until 28 days after each immunization (28 days)

Interventionparticipants (Number)
Break through following immunization 1
3: NF135 CPS-immunization (A/L) Cohort B2

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Time to Parasitemia

The effectiveness of CPS-immunization with NF135 sporozoites to protect against malaria challenge infection with homologous N135.C10 or heterologous NF54 sporozoites will be determined by the time to parasitemia in immunized versus non-immunized volunteers after the challenge infection. (NCT03813108)
Timeframe: Day 1 - 28 after malaria challenge infection (28 days)

Interventiondays to parasitaemia (Median)
1: NF135 CPS-immunization Challenged by NF1359
2: Low Dose NF135 CPS-immunization Challenged by NF1357
5: Control Group Challenged by NF135.C10 Cohort A7

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Time to First PCR Positivity.

For the purpose of this study, 'PCR positivity' is used for the 'protocol-defined PCR positivity' (NCT04310085)
Timeframe: Day 1 to day 21

InterventionDays (Geometric Mean)
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 19.76
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 29.60

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Time to First Dose of Treatment With Artemether-lumefantrine (Riamet®) (Cohorts 1 and 2)

(NCT04310085)
Timeframe: Day 1 to day 21

InterventionDays (Geometric Mean)
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 112.09
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 212.04

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Parasitaemia at the Time Parasitaemia ≥5000 Parasites Per mL Blood (Cohorts 1 and 2)

(NCT04310085)
Timeframe: Day 1 to day 21

InterventionPARASITES/mL (Geometric Mean)
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 112807.4
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 218831.7

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Parasitaemia at First PCR Positivity

POSITIVE PARASITAEMIA IS DEFINED AS qPCR OUTCOME >=250 PARASITES per mL BLOOD. (NCT04310085)
Timeframe: Day 1 to day 21

InterventionPARASITES/mL (Geometric Mean)
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 1367.2
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 2711.7

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Incidence and Severity of Observed or Self-reported Adverse Events (AEs) Considered PfSPZ-DVI Challenge Inoculum-related.

Based on their start date(time), AEs will be allocated to the phase during which they started (Screening, Challenge, Rescue). Each AE will therefore be reported in only one phase. (NCT04310085)
Timeframe: Screening until end of study, day 28.

,
InterventionIncidence (Number)
Adverse eventsAny grade 3 or more adverse eventScreening Adverse eventsChallenge adverse eventsChallenge adverse events grade 3 or aboveRescue adverse eventsRescue adverse events grade 3 or above
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 113107061
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 212205072

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Time to Parasitaemia of ≥5000 Parasites Per mL Blood (Cohorts 1 and 2)

(NCT04310085)
Timeframe: Day 1 to day 21

InterventionDays (Median)
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 111.19
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 211.46

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Change in Malaria Clinical Score From PfSPZ-DVI Challenge Until Parasite Clearance.

"Malaria Clinical Score~14 signs/symptoms frequently associated with malaria will be graded using a 4-point scale (absent: 0; mild: 1; moderate: 2; severe: 3): headache, myalgia (muscle ache), arthralgia (joint ache), fatigue/lethargy, malaise (general discomfort/uneasiness), chills/shivering/rigors, sweating/hot spells, anorexia, nausea, vomiting, abdominal discomfort, fever, tachycardia and hypotension.~Malaria clinical score is calculated as the sum of all (14) malaria sign and symptoms scores (maximum score is 42)." (NCT04310085)
Timeframe: Day 1 until end of study, day 28.

Interventionscore on a scale (Mean)
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 19.63
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 213.0

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Incidence of Positive PCR and Parasitaemia of ≥5000 Parasites Per mL Blood.

(NCT04310085)
Timeframe: Day 1 with PfSPZ-DVI Challenge and Day 28 (per cohort).

InterventionParticipants (Count of Participants)
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 18
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 28

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Parasitaemia at First Dose of Treatment With Riamet® (Cohorts 1 and 2)

(NCT04310085)
Timeframe: Day 1 to day 21

InterventionPARASITES/mL (Geometric Mean)
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 13936.7
PfSPZ-DVI Challenge and Artemether Lumefantrine Cohort 29454.3

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Number of Participants With ECG Changes

Safety signals, trends or significant differences in QT, QTcB and QTcF, QRS between treatment groups were were reported during the study up to 28 days after AL+Rux and AL+Placebo administration in all participants by treatment regimens. (NCT04456634)
Timeframe: up to 28 days after AL+Rux and AL+placebo administration

InterventionParticipants (Count of Participants)
AL&RUX2
AL& Placebo0

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Number of Participants With Changes in Heart Rate

Safety signals, trends or significant differences in heart rate ( beats / min)between treatment groups were were reported during the study up to 28 days after AL+Rux and AL+Placebo administration in all participants by treatment regimens. (NCT04456634)
Timeframe: up to 28 days after AL+Rux and AL+placebo administration

InterventionParticipants (Count of Participants)
AL&RUX1
AL& Placebo0

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AUECt of pSTAT3 Inhibition

Area under the effect curve (AUECt) of pSTAT3 inhibition levels (NCT04456634)
Timeframe: up to 28 days after AL+Rux and AL+placebo administration

Interventionng.hr/mL (Mean)
AL&RUX551
AL& Placebo186

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Number of Participants With Changes of Systolic and Diastolic Blood Pressure

Safety signals, trends or significant differences in blood pressure between treatment groups were were reported during the study up to 28 days after AL+Rux and AL+Placebo administration in all participants by treatment regimens. (NCT04456634)
Timeframe: up to 28 days after AL+Rux and AL+placebo administration

InterventionParticipants (Count of Participants)
AL&RUX2
AL& Placebo0

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