Page last updated: 2024-12-07

artesunic acid

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Artesunic acid is a sesquiterpene lactone derived from the plant Artemisia annua. It is the active ingredient in the antimalarial drug artemisinin. Artesunic acid is synthesized from artemisinin through a multi-step process involving oxidation, esterification, and deprotection. Artesunic acid has potent antimalarial activity, particularly against Plasmodium falciparum, the most deadly species of malaria parasite. It acts by producing reactive oxygen species that damage the parasite. Artesunic acid is important because it is highly effective against drug-resistant malaria parasites and is considered a key component in the fight against this deadly disease. Research on artesunic acid is ongoing to improve its efficacy, reduce side effects, and develop new drug formulations. '
```

Cross-References

ID SourceID
PubMed CID105031
CHEMBL ID1967249
SCHEMBL ID12922911
MeSH IDM0289338

Synonyms (11)

Synonym
LS-14742
NCI60_039350
88495-63-0
artesunate ,
dihydroqinghaosusuccinate
nsc712571
182824-33-5
SCHEMBL12922911
CHEMBL1967249
4-oxo-4-[(1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-yl)oxy]butanoic acid
4-oxo-4-[[(1s,4s,5r,8s,9r,10s,12r,13r)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-yl]oxy]butanoic acid

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" 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
" Both regimens were safe and well tolerated and there were no adverse experiences attributed to the combination."( A randomized safety and tolerability trial of artesunate plus sulfadoxine--pyrimethamine versus sulfadoxine-pyrimethamine alone for the treatment of uncomplicated malaria in Gambian children.
Alloueche, A; Bayo, L; Doherty, JF; Milligan, P; Olliaro, P; Pinder, M; Sadiq, AD; von Seidlein, L,
)
0.13
" There were no adverse effects experienced by the patients."( A safety and efficacy trial of artesunate, sulphadoxine-pyrimethamine and primaquine in P falciparum malaria.
Faizal, HM; Fernando, WP; Galappaththy, G; Weerasinghe, KL; Wickremasinghe, AR; Wickremasinghe, DR, 2002
)
0.31
"The combination of artesunate, S + P and primaquine was found to be effective and safe in the treatment of uncomplicated P falciparum malaria."( A safety and efficacy trial of artesunate, sulphadoxine-pyrimethamine and primaquine in P falciparum malaria.
Faizal, HM; Fernando, WP; Galappaththy, G; Weerasinghe, KL; Wickremasinghe, AR; Wickremasinghe, DR, 2002
)
0.31
" Severe malaria in rural areas of Sudan, where facilities for the safe and effective use of parenteral quinine are lacking, is a frequent problem."( Descriptive study on the efficacy and safety of artesunate suppository in combination with other antimalarials in the treatment of severe malaria in Sudan.
Alkadru, AM; Awad, MI; Baraka, OZ; Behrens, RH; Eltayeb, IB, 2003
)
0.32
" There were no adverse events (AEs) reported during the study."( Randomised efficacy and safety study of two 3-day artesunate rectal capsule/mefloquine regimens versus artesunate alone for uncomplicated malaria in Ecuadorian children.
Cambon, N; Gomez, EA; Jurado, MH, 2003
)
0.32
" The no or low adverse effect levels were in the range of 5 to 7 mg/kg/day artesunate."( Developmental toxicity of artesunate and an artesunate combination in the rat and rabbit.
A Clode, S; Clark, RL; Gaunt, I; Ward, SA; White, TE; Winstanley, P, 2004
)
0.32
" There was rapid relief of symptoms the median time of fever clearance was one day and the most common drug related adverse events were headache dizziness and asthenia."( Efficacy and safety of an artesunate/mefloquine combination, (artequin) in the treatment of uncomplicated P. falciparum malaria in Kenya.
Bhatt, KM; Bhatt, SM; Samia, BM; Wasunna, KM, 2006
)
0.33
"Artesunate-mefloquine combination given simultaneously was found to be highly effective and safe in the treatment of uncomplicated malaria."( Efficacy and safety of an artesunate/mefloquine combination, (artequin) in the treatment of uncomplicated P. falciparum malaria in Kenya.
Bhatt, KM; Bhatt, SM; Samia, BM; Wasunna, KM, 2006
)
0.33
"9%) withdrew because of drug-related adverse events; seven had gastrointestinal complaints of whom two were hospitalized for vomiting."( Efficacy and safety of artesunate plus amodiaquine in routine use for the treatment of uncomplicated malaria in Casamance, southern Sénégal.
Agnamey, P; Brasseur, P; Gaye, O; Olliaro, PL; Taylor, WR; Vaillant, M, 2007
)
0.34
" The safety was evaluated by incidence of adverse events."( Randomized, comparative study of the efficacy and safety of artesunate plus amodiaquine, administered as a single daily intake versus two daily intakes in the treatment of uncomplicated falciparum malaria.
Brasseur, P; Cisse, M; Diouf, AM; Faye, B; Gaye, O; Kuété, T; Lameyre, V; Ndiaye, JL; Same-Ekobo, A; Seck, PA, 2008
)
0.35
" The main adverse events were gastrointestinal disorders (2."( Randomized, comparative study of the efficacy and safety of artesunate plus amodiaquine, administered as a single daily intake versus two daily intakes in the treatment of uncomplicated falciparum malaria.
Brasseur, P; Cisse, M; Diouf, AM; Faye, B; Gaye, O; Kuété, T; Lameyre, V; Ndiaye, JL; Same-Ekobo, A; Seck, PA, 2008
)
0.35
" No drug-related serious adverse events and no deaths occurred."( Safety and efficacy of methylene blue combined with artesunate or amodiaquine for uncomplicated falciparum malaria: a randomized controlled trial from Burkina Faso.
Coulibaly, B; Klose, C; Kouyaté, B; Mansmann, U; Meissner, P; Mockenhaupt, FP; Müller, O; Schirmer, RH; Sié, A; Walter-Sack, I; Zoungrana, A, 2008
)
0.35
" No significant adverse event attributable to any of the study drugs was found."( Efficacy, safety, and selection of molecular markers of drug resistance by two ACTs in Mali.
Dama, S; Dembele, D; Dicko, A; Djimdé, AA; Doumbo, OK; Fofana, B; Ouologuem, D; Sagara, I; Sidibe, B; Toure, S, 2008
)
0.35
" Participants were actively monitored for adverse events for the first 14 days after each treatment, and then passively followed until their next study medication treatment, or withdrawal from study."( Safety and tolerability of combination antimalarial therapies for uncomplicated falciparum malaria in Ugandan children.
Clark, TD; Dorsey, G; Jagannathan, P; Kamya, MR; Maiteki-Sebuguzi, C; Njama-Meya, D; Nzarubara, B; Rosenthal, PJ; Staedke, SG; Talisuna, AO; Yau, VM, 2008
)
0.35
" There were no serious adverse events."( Efficacy, safety and tolerability of artesunate-mefloquine in the treatment of uncomplicated Plasmodium falciparum malaria in four geographic zones of Nigeria.
Agomo, PU; Aina, OO; Ezeiru, VI; Meremikwu, MM; Odey, FA; Oguche, S; Omalu, IJ; Watila, IM, 2008
)
0.35
"This co-packaged formulation of artesunate + mefloquine (Artequin) is highly efficacious, safe and well-tolerated."( Efficacy, safety and tolerability of artesunate-mefloquine in the treatment of uncomplicated Plasmodium falciparum malaria in four geographic zones of Nigeria.
Agomo, PU; Aina, OO; Ezeiru, VI; Meremikwu, MM; Odey, FA; Oguche, S; Omalu, IJ; Watila, IM, 2008
)
0.35
" Most common drug-related adverse events were gastrointestinal symptoms (such as vomiting and diarrhea) which were slightly higher in the AS-SMP 24-hour group."( Efficacy and safety of a fixed dose artesunate-sulphamethoxypyrazine-pyrimethamine compared to artemether-lumefantrine for the treatment of uncomplicated falciparum malaria across Africa: a randomized multi-centre trial.
Adam, I; Dara, N; Dicko, A; Dicko, YT; Djimdé, A; Doumbo, OK; Jansen, FH; Maiga, H; Mbacham, W; Rulisa, S; Sagara, I; Sissoko, K; Traore, OB, 2009
)
0.35
" Adverse events were monitored and laboratory parameters on study Days 0, 2, 5, and 7 post drug administrations were analyzed."( Comparative study of dihydroartemisinin and artesunate safety in healthy Thai volunteers.
Atipas, S; Chatsiricharoenkul, S; Kaewkungwal, J; Khuhapinant, A; Kongpatanakul, S, 2009
)
0.35
" All adverse events were mild."( Comparative study of dihydroartemisinin and artesunate safety in healthy Thai volunteers.
Atipas, S; Chatsiricharoenkul, S; Kaewkungwal, J; Khuhapinant, A; Kongpatanakul, S, 2009
)
0.35
" 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
" Abdominal pain was the most frequent adverse event, with a higher incidence among children treated with mefloquine (89%), mefloquine-artesunate (83%), and artesunate (60%) than among children treated with praziquantel (46%)."( Efficacy and safety of mefloquine, artesunate, mefloquine-artesunate, and praziquantel against Schistosoma haematobium: randomized, exploratory open-label trial.
Adoubryn, KD; Hatz, C; Keiser, J; N'Goran, EK; N'Guessan, NA; Silué, KD; Utzinger, J; Vounatsou, P, 2010
)
0.36
" The most frequent adverse events were vomiting (17%), abdominal pain (11%) and headache (17%)."( Efficacy and safety of a new pediatric artesunate-mefloquine drug formulation for the treatment of uncomplicated falciparum malaria in Gabon.
Agnandji, ST; Bélard, S; Bouyou-Akotet, MK; Heidecker, JL; Issifou, S; Kombila, M; Kremsner, PG; Kurth, F; Mamfoumbi, MM; Mihindou, MP; Missinou, MA; Ngoungou, EB; Ramharter, M; Trapp, S, 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
)
0.36
" Clinical laboratory electrocardiogram (ECG), adverse events (AEs), efficacy, and pharmacokinetic parameters were assessed over 28 days."( New fixed-dose artesunate-mefloquine formulation against multidrug-resistant Plasmodium falciparum in adults: a comparative phase IIb safety and pharmacokinetic study with standard-dose nonfixed artesunate plus mefloquine.
Chalermrut, K; Kiechel, JR; Krudsood, S; Leowattana, W; Looareesuwan, S; Navaratnam, V; Olliaro, P; Phumratanaprapin, W; Ramanathan, S; Tangpukdee, N; Taylor, WR; Vaillant, M; Wilairatana, P, 2010
)
0.36
" 50 neurological and neuropsychiatric adverse events occurred in 28 patients."( Artesunate-mefloquine combination therapy in acute Plasmodium falciparum malaria in young children: a field study regarding neurological and neuropsychiatric safety.
Chelo, D; Djoukoue, F; Frey, SG; Hatz, C; Kinkela, MN; Tietche, F; Weber, P, 2010
)
0.36
"African children showed a low percentage of self-limited neurological and neuropsychiatric adverse events, confirming studies on neurological safety in Asian children treated with artesunate and mefloquine."( Artesunate-mefloquine combination therapy in acute Plasmodium falciparum malaria in young children: a field study regarding neurological and neuropsychiatric safety.
Chelo, D; Djoukoue, F; Frey, SG; Hatz, C; Kinkela, MN; Tietche, F; Weber, P, 2010
)
0.36
" Most adverse events were mild or moderate and affected all treatment groups; serious adverse events--vertigo, nausea, vomiting, and anxiety--were reported only by patients taking mefloquine or mefloquine-artesunate."( Efficacy and safety of mefloquine, artesunate, mefloquine-artesunate, tribendimidine, and praziquantel in patients with Opisthorchis viverrini: a randomised, exploratory, open-label, phase 2 trial.
Akkhavong, K; Hatz, C; Keiser, J; Odermatt, P; Sayasone, S; Soukhathammavong, P; Vonghachack, Y; Vounatsou, P, 2011
)
0.37
" The high correlation between embryotoxicity and reticulocytopenia further supports the assertion that therapeutic dosage regimens of artemisinins that cause decreases in reticulocyte count in pregnant women during the putative critical period (approximately postconception wk 3 to 9) are at risk of also causing adverse effects on the embryo."( Artesunate and artelinic acid: association of embryotoxicity, reticulocytopenia, and delayed stimulation of hematopoiesis in pregnant rats.
Brannen, KC; Clark, RL; Hoberman, AM; Sanders, JE, 2011
)
0.37
" The results support the continued safe and efficacious use of artemether-lumefantrine in uncomplicated falciparum malaria."( Randomized, prospective, three-arm study to confirm the auditory safety and efficacy of artemether-lumefantrine in Colombian patients with uncomplicated Plasmodium falciparum malaria.
Barón, C; Carrasquilla, G; Cousin, M; Fisher, LM; Lefèvre, G; Monsell, EM; Sander, O; Walter, V, 2012
)
0.38
" Both DP and A + M were well tolerated, with the majority of adverse events of mild or moderate severity."( Therapeutic efficacy and safety of dihydroartemisinin-piperaquine versus artesunate-mefloquine in uncomplicated Plasmodium falciparum malaria in India.
Bacchieri, A; Bhattacharyya, PC; Corsi, M; Dev, V; Dubashi, N; Gargano, N; Ghosh, SK; Kumar, A; Rao, BH; Srivastava, B; Tommasini, S; Ubben, D; Valecha, N, 2012
)
0.38
" Mefloquine (80 mg/kg bwt/day) was maternally toxic and enhanced fetal variations."( Study on the developmental toxicity of combined artesunate and mefloquine antimalarial drugs on rats.
Boareto, AC; Dalsenter, PR; de Araujo, SL; Gomes, C; Lombardi, N; Lourenço, AC; Lourenço, EL; Minatovicz, B; Müller, JC; Paumgartten, FR, 2012
)
0.38
" Adverse events occurred in 57."( Safety and efficacy of pyronaridine-artesunate in uncomplicated acute malaria: an integrated analysis of individual patient data from six randomized clinical trials.
Arbe-Barnes, S; Borghini-Fuhrer, I; Craft, CJ; Duparc, S; Fleckenstein, L; Miller, RM; Shin, CS, 2013
)
0.39
" No neurological or cardiac toxicity was observed and seven dogs exhibited no adverse effects at all."( Safety and efficacy field study of artesunate for dogs with non-resectable tumours.
Efferth, T; Erich, SA; Fleckenstein, L; Grinwis, GC; London, CA; Mol, JA; Rutteman, GR; Spee, B, 2013
)
0.39
" As secondary endpoint, the proportion of any adverse event was assessed."( Artesunate versus quinine in the treatment of severe imported malaria: comparative analysis of adverse events focussing on delayed haemolysis.
Burchard, GD; Cramer, JP; Kluge, S; Rolling, T; Schmiedel, S; Wichmann, D, 2013
)
0.39
"While adverse events observed in patients treated with artesunate were limited to delayed haemolysis (three patients, 60%) and temporary deterioration in renal function (three patients, 60%), patients treated with quinine showed a more diverse picture of side effects with 22 patients (71%) experiencing at least one adverse event."( Artesunate versus quinine in the treatment of severe imported malaria: comparative analysis of adverse events focussing on delayed haemolysis.
Burchard, GD; Cramer, JP; Kluge, S; Rolling, T; Schmiedel, S; Wichmann, D, 2013
)
0.39
" Artesunate, extracted from the Chinese herb Artemisia annua, has proven to be effective and safe as an anti-malarial drug that possesses anticancer potential."( Synergism of cytotoxicity effects of triptolide and artesunate combination treatment in pancreatic cancer cell lines.
Cui, YF; Liu, Y, 2013
)
0.39
" ASMQ was well-tolerated and no serious adverse events were reported."( Safety, efficacy and population pharmacokinetics of fixed-dose combination of artesunate-mefloquine in the treatment of acute uncomplicated Plasmodium falciparum malaria in India.
Anvikar, AR; Dash, AP; Dubhashi, NG; Ghosh, SK; Jullien, V; Kiechel, JR; Kumar, A; Rao, BH; Sharma, B; Singh, JP; Srivastava, B; Taylor, WR; Valecha, N, 2013
)
0.39
"Methylene blue (MB) has been shown to be safe and effective against falciparum malaria in Africa and to have pronounced gametocytocidal properties."( Efficacy and safety of triple combination therapy with artesunate-amodiaquine-methylene blue for falciparum malaria in children: a randomized controlled trial in Burkina Faso.
Berens-Riha, N; Bountogo, M; Bousema, T; Breitkreutz, J; Coulibaly, B; Drakeley, C; Kieser, M; Klose, C; Meissner, PE; Mockenhaupt, FP; Müller, O; Nebié, E; Pritsch, M; Schirmer, RH; Sié, A; Sirima, SB; Wieser, A, 2015
)
0.42
" No evidence was found that pyronaridine-artesunate re-treatment increased safety risk based on laboratory values, reported adverse event frequencies, or electrocardiograph findings."( Safety and efficacy of re-treatments with pyronaridine-artesunate in African patients with malaria: a substudy of the WANECAM randomised trial.
Beavogui, AH; Bjorkman, A; Borghini-Fuhrer, I; Borrmann, S; Camara, D; Compaore, YD; Coulibaly, AS; Dara, N; Diallo, MS; Dicko, A; Djimdé, AA; Doumbo, OK; Duparc, S; Fofana, B; Gil, JP; Kabore, MJ; Miller, RM; Nikiema, F; Ouedraogo, JB; Sagara, I; Shin, J; Sirima, SB; Somé, AF; Soulama, I; Sylla, MM; Thera, I; Traore, OB; Zongo, I, 2016
)
0.43
" During the test phase, four patients had adverse events (AEs) of the auditory system possibly related to the intake of ART."( Investigation of ototoxicity of artesunate as add-on therapy in patients with metastatic or locally advanced breast cancer: new audiological results from a prospective, open, uncontrolled, monocentric phase I study.
Baumann, I; Edler, L; Hoth, S; König, M; Sertel, S; von Hagens, C; Walter-Sack, I, 2016
)
0.43
" Here we present the side effect profile of MQ for the treatment of uncomplicated malaria on the Thai-Myanmar/Cambodia borders."( Adverse effects of mefloquine for the treatment of uncomplicated malaria in Thailand: A pooled analysis of 19, 850 individual patients.
Lee, SJ; Luxemburger, C; Nosten, F; Price, RN; Ter Kuile, FO, 2017
)
0.46
" However, despite solid evidence that AS is safe and more effective than quinine in endemic areas, its deployment in non-endemic areas has been slow, due in part to the absence of a full good manufacturing practice (GMP) qualification (although prequalification has been granted in 2010)."( Artesunate to treat severe malaria in travellers: review of efficacy and safety and practical implications.
Buffet, PA; Caumes, E; Jauréguiberry, S; Ndour, PA; Roussel, C; Thellier, M, 2017
)
0.46
" Dizziness, nausea, vomiting, headache and asthenia as adverse events (AEs) were more common in MQAS than in AL or DHAPQ (p < 0."( Artemisinin-based combination therapy in pregnant women in Zambia: efficacy, safety and risk of recurrent malaria.
Buyze, J; D'Alessandro, U; Hachizovu, S; Kabuya, JB; Kasongo, W; Mulenga, J; Mulenga, M; Mwakazanga, D; Nambozi, M; Van Geertruyden, JP, 2017
)
0.46
" In this study, we sought to assess the incidence of common adverse events (AEs) following the intake of Inj AS in real-life settings."( Safety Experience During Real-World Use of Injectable Artesunate in Public Health Facilities in Ghana and Uganda: Outcomes of a Modified Cohort Event Monitoring Study (CEMISA).
Akakpo, S; Ampadu, HH; Asante, KP; Bosomprah, S; Dodoo, ANO; Gardarsdottir, H; Hugo, P; Kajungu, D; Leufkens, HGM, 2018
)
0.48
"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
)
0.51
" A total of 36 adverse events were reported in the pilot study and 277 in the comparative study."( Safety and parasite clearance of artemisinin-resistant Plasmodium falciparum infection: A pilot and a randomised volunteer infection study in Australia.
Abd-Rahman, AN; Cascales, L; Chalon, S; Chen, N; Collins, KA; Marquart, L; McCarthy, JS; Möhrle, JJ; Odedra, A; Pasay, C; Pava, Z; Peatey, CL; Rebelo, M; Watts, RE; Webb, L, 2020
)
0.56
" The proportions of non-clinical hepatic adverse events (AEs) following first and repeated treatments with PA and AL were compared within study arms."( Hepatic safety of repeated treatment with pyronaridine-artesunate versus artemether-lumefantrine in patients with uncomplicated malaria: a secondary analysis of the WANECAM 1 data from Bobo-Dioulasso, Burkina Faso.
Barry, N; Compaoré, YD; Djimdé, A; Kaboré, TN; Kabré, Z; Nikiéma, F; Ouattara, A; Ouédraogo, JB; Sagara, I; Somé, AF; Wermi, K; Yerbanga, RS; Zongo, I; Zongo, M, 2021
)
0.62
" Main reported adverse events (AEs) were anemia (136 cases), cardiac events (24, including 20 episodes of conduction disorders and/or arrhythmia), and liver enzyme elevation (23)."( Intravenous Artesunate for the Treatment of Severe Imported Malaria: Implementation, Efficacy, and Safety in 1391 Patients.
Angoulvant, A; Argy, N; Bouchaud, O; Bruneel, F; Buffet, P; Caumes, E; Chambrion, C; Courtin, D; Danis, M; Delacour, H; Gay, F; Henry, B; Houzé, S; Jauréguiberry, S; Kendjo, E; Larréché, S; Lebrun-Vignes, B; Mouri, O; Ndour, PA; Piarroux, R; Roussel, C; Siriez, JY; Taieb, A; Thellier, M, 2021
)
0.62
" Adverse event frequency was similar between the 3-day (51."( Efficacy, Safety and Tolerability of Pyronaridine-artesunate in Asymptomatic Malaria-infected Individuals: a Randomized Controlled Trial.
Achan, J; Arbe-Barnes, S; Borghini-Fuhrer, I; Conteh, B; D'Alessandro, U; Dabira, ED; Duparc, S; Hachizovu, S; Lawal, B; Manyando, C; Mendy, A; Miller, R; Mulenga, JM; Mwanza, S; Ndiath, MO; Nyang, H; Shin, J, 2022
)
0.72
" Adverse events of any cause occurred in 20."( Pyronaridine-artesunate real-world safety, tolerability, and effectiveness in malaria patients in 5 African countries: A single-arm, open-label, cohort event monitoring study.
Agnandji, ST; Allen, SJ; Arbe-Barnes, S; Assi, SB; Bigoga, JD; Borghini-Fuhrer, I; Duparc, S; Groger, M; Koukouikila-Koussounda, F; Kremsner, PG; Miller, R; Mombo-Ngoma, G; Ntamabyaliro, NY; Ntoumi, F; Ramharter, M; Shin, J; Tona Lutete, G, 2021
)
0.62
" Demographic, clinical, laboratory, adverse event, and outcome information were collected."( Safety and Effectiveness of Intravenous Artesunate for Treatment of Severe Malaria in the United States-April 2019 Through December 2020.
Abanyie, F; Acharya, SD; Bowe, M; Leavy, I; Tan, KR, 2021
)
0.62
"IVAS is a safe and effective drug for the treatment of severe malaria in the United States; timely administration can be lifesaving."( Safety and Effectiveness of Intravenous Artesunate for Treatment of Severe Malaria in the United States-April 2019 Through December 2020.
Abanyie, F; Acharya, SD; Bowe, M; Leavy, I; Tan, KR, 2021
)
0.62
" In this work, we report a stable, safe and potent alternative artemisinin-based injectable nanocomplex consisting of dimeric artesunate-choline conjugate (dACC) micelles coated with hyaluronic acid (HA)."( Dimeric artesunate-choline conjugate micelles coated with hyaluronic acid as a stable, safe and potent alternative anti-malarial injection of artesunate.
Dogovski, C; Du, Y; He, W; Hu, R; Li, C; Li, X; Tao, Z; Wang, J; Wang, Y; Yao, C, 2021
)
0.62
" Adverse events both solicited and unsolicited are recorded all through the study post-randomization."( Efficacy and safety of dual intravenous artesunate plus quinine compared to intravenous artesunate for cerebral malaria in a triple blinded parallel multisite randomized controlled trial in Nigerian children: DUAL PAQ TRIAL Protocol.
Alao, MA; Asinobi, AO; Gbadero, DA; Ibrahim, OR; Nna, EO; Okoye, IJ; Orimadegun, AE; Oyenuga, AO, 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
)
0.72
" 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
)
0.72
"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
)
0.72
" Patients spontaneous reported any clinical adverse events (AEs) occurring within 28 days following the treatment."( Prospective observational study to evaluate the clinical and biological safety profile of pyronaridine-artesunate in a rural health district in Burkina Faso.
Baiden, R; Binka, F; Compaore, A; Diande, NA; Hien, FS; Rouamba, T; Sondo, P; Tahita, MC; Tinto, H; Traore-Coulibaly, M; Valea, I; Yerbanga, IW, 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 real-life safety was assessed by related adverse events (AE) and monitoring of biological blood parameters during the hospital stay and follow-up period."( Use of artesunate in the treatment of severe imported malaria in France: review of the effectiveness and real-life safety in two French university hospitals.
Bertault-Peres, P; Bonsergent, M; Flet, L; Honoré, S; Lepelletier, A; Perez, T; Tching-Sin, M, 2023
)
0.91
"This study aimed at determining whether intravenous artesunate is safe and effective in reducing multiple organ dysfunction syndrome in trauma patients with major hemorrhage."( Safety and efficacy of artesunate treatment in severely injured patients with traumatic hemorrhage. The TOP-ART randomized clinical trial.
Anton, L; Brentnall, AR; Brohi, K; Ross, J; Rourke, C; Shepherd, JM; Tarning, J; Thiemermann, C; White, NJ, 2023
)
0.91
" The safety outcome was the 28-day serious adverse event (SAE) rate."( Safety and efficacy of artesunate treatment in severely injured patients with traumatic hemorrhage. The TOP-ART randomized clinical trial.
Anton, L; Brentnall, AR; Brohi, K; Ross, J; Rourke, C; Shepherd, JM; Tarning, J; Thiemermann, C; White, NJ, 2023
)
0.91
" Dihydroartemisinin-piperaquine and artesunate-amodiaquine were associated with a small number of mild adverse events, and there were no treatment-related serious adverse events or deaths."( Effectiveness and safety of intermittent preventive treatment with dihydroartemisinin-piperaquine or artesunate-amodiaquine for reducing malaria and related morbidities in schoolchildren in Tanzania: a randomised controlled trial.
Baraka, V; Francis, F; Geertruyden, JV; Gesase, S; Kyaruzi, E; Lusingu, JPA; Madebe, R; Makenga, G; Minja, DTR; Mtove, G; Nakato, S, 2023
)
0.91
"IPTsc with dihydroartemisinin-piperaquine or artesunate-amodiaquine is a safe and effective approach to reducing malaria parasitaemia, clinical malaria, and related morbidities, and is feasible to implement through programmes delivered by schoolteachers."( Effectiveness and safety of intermittent preventive treatment with dihydroartemisinin-piperaquine or artesunate-amodiaquine for reducing malaria and related morbidities in schoolchildren in Tanzania: a randomised controlled trial.
Baraka, V; Francis, F; Geertruyden, JV; Gesase, S; Kyaruzi, E; Lusingu, JPA; Madebe, R; Makenga, G; Minja, DTR; Mtove, G; Nakato, S, 2023
)
0.91
" Mild and moderate adverse events, including gastrointestinal and/or nervous disorders, were reported in 11."( Therapeutic efficacy and safety of artesunate + amodiaquine and artemether + lumefantrine in treating uncomplicated Plasmodium falciparum malaria in children on the rainy south-east coast of Madagascar.
Carn, G; Harimanana, AN; Hotahiene, R; Irinantenaina, J; Ralemary, N; Randriamiarinjatovo, DNAL; Randrianarivelojosia, M; Randriarison, M; Razafinjato, C; Razanatsiorimalala, S, 2023
)
0.91
" Clinical assessments were completed prior to each dose cycle and included exam and review of adverse event (AE) diary cards."( Safety and efficacy of topical artesunate for the treatment of vulvar intraepithelial neoplasia 2/3.
AlHilli, M; Beffa, L; Belinson, JL; Brainard, J; Debernardo, R; Michener, CM; Plesa, M; Ricci, S; Trimble, CL; Waggoner, SE, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" However, artesunate was shown to have a very short half-life when given iv in animals as well as in human beings."( [The pharmacokinetics of a transdermal preparation of artesunate in mice and rabbits].
Song, ZY; Xuan, WY; Zhao, KC; Zhao, Y, 1989
)
0.28
"The pharmacokinetic properties of oral artesunate (3 mg/kg) were determined in 10 Vietnamese children, aged from 6 to 15 years, with acute falciparum malaria of moderate severity."( Pharmacokinetics of oral artesunate in children with moderately severe Plasmodium falciparum malaria.
Bethell, DB; Cao, XT; Day, NP; Kyle, D; Nguyen, TT; Pham, TP; Pham, TT; Ta, TT; Teja-Isavadharm, P; Tran, TN; White, NJ,
)
0.13
" Pharmacokinetic parameters were calculated by non-compartmental methods."( A pharmacokinetic and pharmacodynamic study of intravenous vs oral artesunate in uncomplicated falciparum malaria.
Batty, KT; Binh, TQ; Davis, TM; Hung, NC; Ilett, KF; Kim, NV; Mai, TX; Powell, SM; Thien, HV; Thu, LT; Tien, NP, 1998
)
0.3
" bolus, ARTS had a peak concentration of 29."( A pharmacokinetic and pharmacodynamic study of intravenous vs oral artesunate in uncomplicated falciparum malaria.
Batty, KT; Binh, TQ; Davis, TM; Hung, NC; Ilett, KF; Kim, NV; Mai, TX; Powell, SM; Thien, HV; Thu, LT; Tien, NP, 1998
)
0.3
"To investigate the pharmacokinetic and pharmacodynamic properties of artesunate (ARTS) and its active metabolite dihydroartemisinin (DHA) in Plasmodium vivax infections, 12 male Vietnamese adults with slide-positive vivax malaria received either intravenous ARTS (120 mg; group 1) or oral ARTS (100 mg; group 2) with the alternative preparation given 8 hr later in a randomized, open, cross-over study."( A pharmacokinetic and pharmacodynamic study of artesunate for vivax malaria.
Batty, KT; Davis, TM; Huynh, VT; Ilett, KF; Le, AT; Nguyen, CH; Nguyen, PT; Nguyen, VM; Powell, SM; Tran, QB; Truong, XM; Vuong, VC, 1998
)
0.3
"To construct a population pharmacokinetic model for mefloquine in the treatment of falciparum malaria."( Population pharmacokinetics of mefloquine in patients with acute falciparum malaria.
Aarons, L; Chongsuphajaisiddhi, T; Looareesuwan, S; Nosten, F; Price, R; Simpson, JA; Teja-Isavatharm, P; ter Kuile, F; White, NJ, 1999
)
0.3
" The factors that influence the pharmacokinetic properties of mefloquine in acute malaria are not well characterized."( Population pharmacokinetics of mefloquine in patients with acute falciparum malaria.
Aarons, L; Chongsuphajaisiddhi, T; Looareesuwan, S; Nosten, F; Price, R; Simpson, JA; Teja-Isavatharm, P; ter Kuile, F; White, NJ, 1999
)
0.3
"The pharmacokinetic properties of mefloquine were evaluated in 257 patients with acute falciparum malaria by use of nonlinear mixed-effects modeling."( Population pharmacokinetics of mefloquine in patients with acute falciparum malaria.
Aarons, L; Chongsuphajaisiddhi, T; Looareesuwan, S; Nosten, F; Price, R; Simpson, JA; Teja-Isavatharm, P; ter Kuile, F; White, NJ, 1999
)
0.3
"The pharmacokinetic properties of mefloquine in malaria were relatively unaffected by demographic variables (other than body weight) or disease severity."( Population pharmacokinetics of mefloquine in patients with acute falciparum malaria.
Aarons, L; Chongsuphajaisiddhi, T; Looareesuwan, S; Nosten, F; Price, R; Simpson, JA; Teja-Isavatharm, P; ter Kuile, F; White, NJ, 1999
)
0.3
" Population pharmacokinetic modelling was performed using NONMEM."( Population pharmacokinetics of the new antimalarial agent tafenoquine in Thai soldiers.
Brewer, TG; Charles, BG; Eamsila, C; Edstein, MD; Kocisko, DA; Walsh, DS, 2001
)
0.31
"To determine the pharmacokinetic properties of atovaquone, proguanil, and the triazine metabolite cycloguanil in women with recrudescent multi-drug resistant falciparum malaria during the second and third trimesters of pregnancy treated by artesunate-atovaquone-proguanil."( The pharmacokinetics of atovaquone and proguanil in pregnant women with acute falciparum malaria.
Cho, T; Edstein, MD; Gilveray, G; Looareesuwan, S; McGready, R; Nosten, F; Stepniewska, K; White, NJ, 2003
)
0.32
" Using conventional and population pharmacokinetic analyses, Cl/F and Vd/F estimates for both drugs were approximately twice, and plasma concentrations less than half those reported previously in healthy subjects and patients with acute malaria."( The pharmacokinetics of atovaquone and proguanil in pregnant women with acute falciparum malaria.
Cho, T; Edstein, MD; Gilveray, G; Looareesuwan, S; McGready, R; Nosten, F; Stepniewska, K; White, NJ, 2003
)
0.32
"The aims of this study were to determine the pharmacokinetic parameters of a single dose of 200 mg oral and rectal artesunate in healthy volunteers, and to suggest a rational dosage regimen for rectal administration."( Pharmacokinetics of artesunate following oral and rectal administration in healthy Sudanese volunteers.
Alkadru, AM; Awad, MI; Baraka, OZ; Behrens, RH; Eltayeb, IB, 2004
)
0.32
"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
)
0.32
"To determine the pharmacokinetic properties of dihydroartemisinin (DHA) following oral artesunate treatment in women with recrudescent multi-drug resistant falciparum malaria, in the second and third trimesters of pregnancy."( Pharmacokinetics of dihydroartemisinin following oral artesunate treatment of pregnant women with acute uncomplicated falciparum malaria.
Cho, T; Gilveray, G; Looareesuwan, S; McGready, R; Nosten, F; Stepniewska, K; Ward, SA; White, NJ, 2006
)
0.33
" Conventional non-compartmental modelling and a population one-compartment pharmacokinetic model were applied to the data."( Pharmacokinetics of dihydroartemisinin following oral artesunate treatment of pregnant women with acute uncomplicated falciparum malaria.
Cho, T; Gilveray, G; Looareesuwan, S; McGready, R; Nosten, F; Stepniewska, K; Ward, SA; White, NJ, 2006
)
0.33
" The DHART levels are somewhat higher than those of ART (a peak concentration after 6 h starting medication of 151 microg/ml ART as compared to 276 microg/ml DHART)."( Pharmacokinetics/Pharmacodynamics findings after repeated administration of ARTESUNATE thermostable suppositories (RECTOCAPS) in Vietnamese patients with uncomplicated malaria.
Benakis, A; Binh, TQ; Keundjian, A; Scheiwe, MW,
)
0.13
" This study was designed to construct a population pharmacokinetic model describing this new dosage regimen of mefloquine given as loose tablets together with artesunate."( Population pharmacokinetic assessment of a new regimen of mefloquine used in combination treatment of uncomplicated falciparum malaria.
Ashley, EA; Hae, R; Hutagalung, R; Lindegårdh, N; McGready, R; Nosten, F; Singhasivanon, P; Stepniewska, K; White, NJ, 2006
)
0.33
" The pharmacokinetic properties of DHA were determined using nonlinear mixed-effects modelling."( Population pharmacokinetics of artesunate and dihydroartemisinin following intra-rectal dosing of artesunate in malaria patients.
Agbenyega, T; Barnes, KI; Di Perri, G; Folb, P; Gomes, M; Krishna, S; Krudsood, S; Looareesuwan, S; Mansor, S; McIlleron, H; Miller, R; Molyneux, M; Mwenechanya, J; Navaratnam, V; Nosten, F; Olliaro, P; Pang, L; Ribeiro, I; Simpson, JA; Tembo, M; van Vugt, M; Ward, S; Weerasuriya, K; White, NJ; Win, K, 2006
)
0.33
"The pharmacokinetic properties of DHA were affected only by gender and body weight."( Population pharmacokinetics of artesunate and dihydroartemisinin following intra-rectal dosing of artesunate in malaria patients.
Agbenyega, T; Barnes, KI; Di Perri, G; Folb, P; Gomes, M; Krishna, S; Krudsood, S; Looareesuwan, S; Mansor, S; McIlleron, H; Miller, R; Molyneux, M; Mwenechanya, J; Navaratnam, V; Nosten, F; Olliaro, P; Pang, L; Ribeiro, I; Simpson, JA; Tembo, M; van Vugt, M; Ward, S; Weerasuriya, K; White, NJ; Win, K, 2006
)
0.33
"Paediatric drug formulations of artemisinin combination therapies and pharmacokinetic data supporting their use in African children are urgently needed for the effective treatment of young children suffering from falciparum malaria in sub-Saharan Africa."( Pharmacokinetics of two paediatric artesunate mefloquine drug formulations in the treatment of uncomplicated falciparum malaria in Gabon.
Adegnika, AA; Agnandji, ST; Bélard, S; Bouyou-Akotet, MK; Cambon, N; Heidecker, JL; Issifou, S; Kombila, M; Kremsner, PG; Kurth, FM; Mamfoumbi, MM; Missinou, MA; Ramharter, M, 2007
)
0.34
"In this study, the pharmacokinetic characteristics of a novel paediatric granule formulation of artesunate-mefloquine therapy were evaluated in comparison to the standard tablet formulation in the treatment of uncomplicated malaria in paediatric patients."( Pharmacokinetics of two paediatric artesunate mefloquine drug formulations in the treatment of uncomplicated falciparum malaria in Gabon.
Adegnika, AA; Agnandji, ST; Bélard, S; Bouyou-Akotet, MK; Cambon, N; Heidecker, JL; Issifou, S; Kombila, M; Kremsner, PG; Kurth, FM; Mamfoumbi, MM; Missinou, MA; Ramharter, M, 2007
)
0.34
" As no pharmacokinetic data on this combination have been published to date, we investigated its pharmacokinetic interactions and tolerability in healthy volunteers in Africa."( Pharmacokinetics and tolerability of artesunate and amodiaquine alone and in combination in healthy volunteers.
Barnes, KI; Folb, P; Little, F; Olliaro, P; Orrell, C; Smith, P; Taylor, W, 2008
)
0.35
"Thirteen volunteers completed the study, and pharmacokinetic parameters could be determined for twelve volunteers."( Pharmacokinetics and tolerability of artesunate and amodiaquine alone and in combination in healthy volunteers.
Barnes, KI; Folb, P; Little, F; Olliaro, P; Orrell, C; Smith, P; Taylor, W, 2008
)
0.35
"The aim was to study the pharmacokinetic profile of artesunate and its metabolite dihydroartemisinin (DHA) in a pig model."( Pharmacokinetics of artesunate in the domestic pig.
Aglioni, C; Bressolle, FM; Mosnier, J; Parzy, D; Sinou, V; Taudon, N, 2008
)
0.35
"The pharmacokinetic properties of artesunate and DHA in pigs were similar to those reported in humans, suggesting that the swine model is suitable for determining the preclinical pharmacokinetics of artemisinin derivatives."( Pharmacokinetics of artesunate in the domestic pig.
Aglioni, C; Bressolle, FM; Mosnier, J; Parzy, D; Sinou, V; Taudon, N, 2008
)
0.35
"Pharmacokinetic and pharmacodynamic responses were evaluated after intramuscular (i."( Pharmacokinetic and pharmacodynamic evaluation of intramuscular artesunate in healthy beagle dogs.
Bennett, K; Li, Q; Si, Y; Steinbach, T; Zhang, J, 2008
)
0.35
"The pharmacokinetic (PK) parameters of artesunate, recently discovered to possess promising trematocidal activity, and its main metabolite dihydroartemisinin (DHA) were determined in rats infected with hepatic and biliary stages of Fasciola hepatica and compared with uninfected rats after single intragastric and intravenous (iv) doses."( Pharmacokinetic parameters of artesunate and dihydroartemisinin in rats infected with Fasciola hepatica.
Decosterd, L; Gruyer, MS; Keiser, J; Mercier, T; Perrottet, N; Zanolari, B, 2009
)
0.35
" This study examines the in vivo efficacy and pharmacokinetic parameters through Day 56 of three commercial formulations of MQ (Lariam, Mephaquin, and Mefloquina-AC Farma) given in combination with artesunate."( Mefloquine pharmacokinetics and mefloquine-artesunate effectiveness in Peruvian patients with uncomplicated Plasmodium falciparum malaria.
Bacon, DJ; Durand, S; Ganguly, B; Green, M; Gutman, J; Quezada, WM; Rojas, OV; Ruebush, TK; Slutsker, L; Utz, GC, 2009
)
0.35
"Whole blood mefloquine concentrations were determined by high-performance liquid chromatography and pharmacokinetic parameters were determined using non-compartmental analysis of concentration versus time data."( Mefloquine pharmacokinetics and mefloquine-artesunate effectiveness in Peruvian patients with uncomplicated Plasmodium falciparum malaria.
Bacon, DJ; Durand, S; Ganguly, B; Green, M; Gutman, J; Quezada, WM; Rojas, OV; Ruebush, TK; Slutsker, L; Utz, GC, 2009
)
0.35
" All three MQ formulations had a terminal half-life of 14-15 days and time to maximum plasma concentration of 45-52 hours."( Mefloquine pharmacokinetics and mefloquine-artesunate effectiveness in Peruvian patients with uncomplicated Plasmodium falciparum malaria.
Bacon, DJ; Durand, S; Ganguly, B; Green, M; Gutman, J; Quezada, WM; Rojas, OV; Ruebush, TK; Slutsker, L; Utz, GC, 2009
)
0.35
"There is limited pharmacokinetic data available for the combination artesunate + amodiaquine, which is used widely to treat uncomplicated malaria."( Tolerability and pharmacokinetics of non-fixed and fixed combinations of artesunate and amodiaquine in Malaysian healthy normal volunteers.
Kiechel, JR; Mansor, SM; Navaratnam, V; Olliaro, P; Ramanathan, S; Siew Hua, G; Taylor, WR; Vaillant, M; Wahab, MS, 2009
)
0.35
"Both combinations were well tolerated and had comparable pharmacokinetic profiles; differences are unlikely to be clinically relevant."( Tolerability and pharmacokinetics of non-fixed and fixed combinations of artesunate and amodiaquine in Malaysian healthy normal volunteers.
Kiechel, JR; Mansor, SM; Navaratnam, V; Olliaro, P; Ramanathan, S; Siew Hua, G; Taylor, WR; Vaillant, M; Wahab, MS, 2009
)
0.35
" Blood samples for pharmacokinetic analysis were collected up to 24 h post-first dose."( Pharmacokinetics of chlorproguanil, dapsone, artesunate and their major metabolites in patients during treatment of acute uncomplicated Plasmodium falciparum malaria.
Bandyopadhyay, N; Duparc, S; Kirby, PL; Miller, AK; Ward, SA; Winstanley, PA; Wootton, DG, 2009
)
0.35
"The pharmacokinetic analysis included 115 patients."( Pharmacokinetics of chlorproguanil, dapsone, artesunate and their major metabolites in patients during treatment of acute uncomplicated Plasmodium falciparum malaria.
Bandyopadhyay, N; Duparc, S; Kirby, PL; Miller, AK; Ward, SA; Winstanley, PA; Wootton, DG, 2009
)
0.35
"A prospective population pharmacokinetic study of AS and AQ was conducted in children aged six months to five years."( Population pharmacokinetics of artesunate and amodiaquine in African children.
Gansané, A; Kiechel, JR; Morgan, CC; Ouedraogo, A; Ouedraogo, EB; Simpson, JA; Sirima, SB; Stepniewska, K; Taylor, W; White, NJ, 2009
)
0.35
" Amodiaquine was converted rapidly to DeAq, which was then eliminated with an estimated median (range) elimination half-life of 9 (7 to 12) days."( Population pharmacokinetics of artesunate and amodiaquine in African children.
Gansané, A; Kiechel, JR; Morgan, CC; Ouedraogo, A; Ouedraogo, EB; Simpson, JA; Sirima, SB; Stepniewska, K; Taylor, W; White, NJ, 2009
)
0.35
" Pharmacokinetic model-dependent analysis is suitable for AS, whereas DHA fits both model-dependent and -independent methods."( Pharmacokinetic profiles of artesunate after single intravenous doses at 0.5, 1, 2, 4, and 8 mg/kg in healthy volunteers: a phase I study.
Cantilena, LR; Leary, KJ; Li, Q; Melendez, V; Miller, RS; Saviolakis, GA; Weina, PJ, 2009
)
0.35
" 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
)
0.36
" A pharmacokinetic study was also conducted to evaluate the bioavailability of AS following the IM administrations."( Severe embryolethality of artesunate related to pharmacokinetics following intravenous and intramuscular doses in pregnant rats.
Li, Q; Si, Y; Weina, P; Xie, L; Zhang, J, 2009
)
0.35
" Nonlinear mixed-effect modelling was used to obtain the pharmacokinetic and variability (inter-individual and residual variability) parameter estimates."( Population pharmacokinetics of artesunate and dihydroartemisinin following single- and multiple-dosing of oral artesunate in healthy subjects.
Craft, JC; Fleckenstein, L; Jang, IJ; Kirsch, LE; Naik, H; Shin, CS; Tan, B; Yu, KS, 2009
)
0.35
"A novel parent-metabolite pharmacokinetic model consisting of a dosing compartment, a central compartment for AS, a central compartment and a peripheral compartment for DHA was developed."( Population pharmacokinetics of artesunate and dihydroartemisinin following single- and multiple-dosing of oral artesunate in healthy subjects.
Craft, JC; Fleckenstein, L; Jang, IJ; Kirsch, LE; Naik, H; Shin, CS; Tan, B; Yu, KS, 2009
)
0.35
"A novel simultaneous parent-metabolite pharmacokinetic model with good predictive power was developed to study the population pharmacokinetics of AS and DHA in healthy subjects following single- and multiple-dosing of AS with or without the presence of food."( Population pharmacokinetics of artesunate and dihydroartemisinin following single- and multiple-dosing of oral artesunate in healthy subjects.
Craft, JC; Fleckenstein, L; Jang, IJ; Kirsch, LE; Naik, H; Shin, CS; Tan, B; Yu, KS, 2009
)
0.35
" The main disposition parameters to AS+AQ were: for DHA, AUC = 632 +/- 475 ng h/ml and Cmax = 432 +/- 325 ng/ml, and for MdAQ = 14268 +/- 4114 ng h/ml and Cmax = 336 +/- 225 ng/ml (mean +/- standard deviation)."( Pharmacokinetics and pharmacodynamics of a new ACT formulation: Artesunate/Amodiaquine (TRIMALACT) following oral administration in African malaria patients.
Alegre, SS; Benakis, A; Bertaux, L; Lwango, R; Malaika, LT; Parzy, D; Sinou, V; Sugnaux, F; Taudon, N,
)
0.13
" Clinical laboratory electrocardiogram (ECG), adverse events (AEs), efficacy, and pharmacokinetic parameters were assessed over 28 days."( New fixed-dose artesunate-mefloquine formulation against multidrug-resistant Plasmodium falciparum in adults: a comparative phase IIb safety and pharmacokinetic study with standard-dose nonfixed artesunate plus mefloquine.
Chalermrut, K; Kiechel, JR; Krudsood, S; Leowattana, W; Looareesuwan, S; Navaratnam, V; Olliaro, P; Phumratanaprapin, W; Ramanathan, S; Tangpukdee, N; Taylor, WR; Vaillant, M; Wilairatana, P, 2010
)
0.36
" Pharmacokinetic and safety data supporting the use of artemisinin derivatives in pregnancy are urgently needed."( Pharmacokinetics and pharmacodynamics of artesunate and dihydroartemisinin following oral treatment in pregnant women with asymptomatic Plasmodium falciparum infections in Kinshasa DRC.
Atibu, J; Bose, C; Capparelli, EV; Douoguih, M; Fleckenstein, L; Hemingway-Foday, J; Koch, MA; Lokomba, V; Meshnick, SR; Onyamboko, MA; Ryder, RW; Tshefu, AK; Wesche, D; Wright, LL, 2011
)
0.37
" Non-compartmental pharmacokinetic analysis was performed using standard methods."( Pharmacokinetics and pharmacodynamics of artesunate and dihydroartemisinin following oral treatment in pregnant women with asymptomatic Plasmodium falciparum infections in Kinshasa DRC.
Atibu, J; Bose, C; Capparelli, EV; Douoguih, M; Fleckenstein, L; Hemingway-Foday, J; Koch, MA; Lokomba, V; Meshnick, SR; Onyamboko, MA; Ryder, RW; Tshefu, AK; Wesche, D; Wright, LL, 2011
)
0.37
" Estimates for pharmacokinetic and variability parameters were obtained through nonlinear mixed effects modelling."( Population pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant women with malaria.
Atibu, J; Bose, C; Capparelli, E; Douoguih, M; Fleckenstein, L; Hemingway-Foday, J; Koch, MA; Lokomba, V; Meshnick, S; Morris, CA; Onyamboko, MA; Ryder, RW; Tshefu, AK; Wesche, D; Wright, L, 2011
)
0.37
"In this analysis, pharmacokinetic modelling suggests that pregnant women have accelerated DHA clearance compared to non-pregnant women receiving orally administered AS."( Population pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant women with malaria.
Atibu, J; Bose, C; Capparelli, E; Douoguih, M; Fleckenstein, L; Hemingway-Foday, J; Koch, MA; Lokomba, V; Meshnick, S; Morris, CA; Onyamboko, MA; Ryder, RW; Tshefu, AK; Wesche, D; Wright, L, 2011
)
0.37
"Currently, population pharmacokinetic (PK) studies of anti-malarial drugs are designed primarily by the logistical and ethical constraints of taking blood samples from patients, and the statistical models that are fitted to the data are not formally considered."( Optimal designs for population pharmacokinetic studies of oral artesunate in patients with uncomplicated falciparum malaria.
Duffull, SB; Jamsen, KM; Lindegardh, N; Simpson, JA; Tarning, J; White, NJ, 2011
)
0.37
" The pharmacokinetic properties of artesunate-azithromycin given in combination are comparable to those of the drugs given alone."( Pharmacokinetics and ex vivo antimalarial activity of artesunate-azithromycin in healthy volunteers.
Anh, CX; Birrell, GW; Chavchich, M; Chinh, NT; Dai, B; Edstein, MD; Quang, NN; Thanh, NX, 2011
)
0.37
" Intravenous AS is associated with high initial AS concentrations which subsequently decline rapidly, with typical AS half-life estimates of less than 15 minutes."( Review of the clinical pharmacokinetics of artesunate and its active metabolite dihydroartemisinin following intravenous, intramuscular, oral or rectal administration.
Borghini-Fuhrer, I; Duparc, S; Fleckenstein, L; Jung, D; Morris, CA; Shin, CS, 2011
)
0.37
" Yet, limited data is available on pharmacokinetic interactions between these drugs."( Effects of amodiaquine and artesunate on sulphadoxine-pyrimethamine pharmacokinetic parameters in children under five in Mali.
Barnes, KI; Beavogui, AH; Djimde, AA; Doumbo, OK; Evans, A; Fredericks, A; Maiga, H; Sangare, CP; Smith, P; Tekete, MM; Toure, S; Traore, ZI, 2011
)
0.37
" Exactly 100 μl of capillary blood was collected onto filter paper before drug administration at day 0 and at days 1, 3, 7, 14, 21 and 28 after drug administration for analysis of sulphadoxine and pyrimethamine pharmacokinetic parameters."( Effects of amodiaquine and artesunate on sulphadoxine-pyrimethamine pharmacokinetic parameters in children under five in Mali.
Barnes, KI; Beavogui, AH; Djimde, AA; Doumbo, OK; Evans, A; Fredericks, A; Maiga, H; Sangare, CP; Smith, P; Tekete, MM; Toure, S; Traore, ZI, 2011
)
0.37
"001) and thus elimination half-life (3."( Effects of amodiaquine and artesunate on sulphadoxine-pyrimethamine pharmacokinetic parameters in children under five in Mali.
Barnes, KI; Beavogui, AH; Djimde, AA; Doumbo, OK; Evans, A; Fredericks, A; Maiga, H; Sangare, CP; Smith, P; Tekete, MM; Toure, S; Traore, ZI, 2011
)
0.37
"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
)
0.38
" No significant dose-effect or concentration-effect relationships between pharmacokinetic (PK) and parasite clearance parameters were observed, though baseline parasitemia was modestly correlated with increased parasite clearance times."( Pharmacokinetics and pharmacodynamics of oral artesunate monotherapy in patients with uncomplicated Plasmodium falciparum malaria in western Cambodia.
Bethell, D; Chanthap, L; Fukuda, M; Khemawoot, P; Lin, J; Noedl, H; Ringwald, P; Rutvisuttinunt, W; Saunders, D; Se, Y; Siripokasupkul, R; Smith, B; Socheat, D; Sriwichai, S; Teja-Isavadharm, P; Timmermans, A; Tyner, S; Vanachayangkul, P, 2012
)
0.38
"Artemisinin resistance, a long parasite clearance half-life in response to artemisinin, has been described in patients with Plasmodium falciparum malaria in southeast Asia."( Plasmodium falciparum clearance rates in response to artesunate in Malian children with malaria: effect of acquired immunity.
Anderson, JM; Chiang, S; Diakite, M; Diakite, SA; Doumbia, S; Doumbouya, M; Fairhurst, RM; Fay, MP; Keita, AS; Konate, DS; Long, CA; Lopera-Mesa, TM; Ndiaye, D; Sa, JM; Stepniewska, K; Traore, K; Zeituni, AE, 2013
)
0.39
" We estimated half-life by measuring parasite density every 6 hours until undetectable and evaluated the effects of age, sex, ethnicity, and red blood cell (RBC) polymorphisms on half-life."( Plasmodium falciparum clearance rates in response to artesunate in Malian children with malaria: effect of acquired immunity.
Anderson, JM; Chiang, S; Diakite, M; Diakite, SA; Doumbia, S; Doumbouya, M; Fairhurst, RM; Fay, MP; Keita, AS; Konate, DS; Long, CA; Lopera-Mesa, TM; Ndiaye, D; Sa, JM; Stepniewska, K; Traore, K; Zeituni, AE, 2013
)
0.39
" IgG responses to parasitized RBCs shorten half-life and may influence this parameter in areas where age is not an adequate surrogate of immunity and correlates of parasite-clearing immunity have not been identified."( Plasmodium falciparum clearance rates in response to artesunate in Malian children with malaria: effect of acquired immunity.
Anderson, JM; Chiang, S; Diakite, M; Diakite, SA; Doumbia, S; Doumbouya, M; Fairhurst, RM; Fay, MP; Keita, AS; Konate, DS; Long, CA; Lopera-Mesa, TM; Ndiaye, D; Sa, JM; Stepniewska, K; Traore, K; Zeituni, AE, 2013
)
0.39
" A population pharmacokinetic study of ARS and dihydroartemisinin (DHA) was conducted from sparse sampling in 70 Tanzanian children of ages 6 months to 11 years."( Population pharmacokinetics of intramuscular artesunate in African children with severe malaria: implications for a practical dosing regimen.
Day, NP; Dondorp, AM; Gesase, S; Hendriksen, IC; Kent, A; Lemnge, MM; Lindegardh, N; Mtove, G; Reyburn, H; Tarning, J; von Seidlein, L; White, NJ, 2013
)
0.39
" The pharmacokinetic analysis was performed using a population approach."( Population pharmacokinetics of mefloquine, administered as a fixed-dose combination of artesunate-mefloquine in Indian patients for the treatment of acute uncomplicated Plasmodium falciparum malaria.
Jullien, V; Kiechel, JR; Sharma, B; Srivastava, B; Valecha, N, 2014
)
0.4
" These values were consistent with the pharmacokinetic results described in Thai patients."( Population pharmacokinetics of mefloquine, administered as a fixed-dose combination of artesunate-mefloquine in Indian patients for the treatment of acute uncomplicated Plasmodium falciparum malaria.
Jullien, V; Kiechel, JR; Sharma, B; Srivastava, B; Valecha, N, 2014
)
0.4
" However, limited data are available on the effect of pregnancy on its pharmacokinetic properties."( Pharmacokinetics of co-formulated mefloquine and artesunate in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum infection in Burkina Faso.
D'Alessandro, U; Davies, GR; Lindegardh, N; Tarning, J; Tinto, H; Toe, LC; Traore-Coulibaly, M; Valea, I; Van Geertruyden, JP; Ward, SA, 2014
)
0.4
" Frequent blood samples were collected before treatment and at scheduled times post-dose for the drug measurements and pharmacokinetic analyses."( Pharmacokinetics of co-formulated mefloquine and artesunate in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum infection in Burkina Faso.
D'Alessandro, U; Davies, GR; Lindegardh, N; Tarning, J; Tinto, H; Toe, LC; Traore-Coulibaly, M; Valea, I; Van Geertruyden, JP; Ward, SA, 2014
)
0.4
" The objective of this study is to show the pharmacokinetic (PK) profile of intravenous artesunate (AS), which was manufactured under good manufacturing practice (GMP) conditions, in adults with uncomplicated falciparum malaria in Kenya."( Pharmacokinetic evaluation of intravenous artesunate in adults with uncomplicated falciparum malaria in Kenya: a phase II study.
Hickman, MR; Li, Q; Melendez, V; Miller, SR; Ogutu, B; Otieno, W; Polhemus, M; Remich, S; Smith, B; Teja-Isavadharm, P; Weina, PJ, 2014
)
0.4
" Pharmacokinetic data were analysed with a compartmental analysis for AS and DHA."( Pharmacokinetic evaluation of intravenous artesunate in adults with uncomplicated falciparum malaria in Kenya: a phase II study.
Hickman, MR; Li, Q; Melendez, V; Miller, SR; Ogutu, B; Otieno, W; Polhemus, M; Remich, S; Smith, B; Teja-Isavadharm, P; Weina, PJ, 2014
)
0.4
" The high mean peak concentration (Cmax) of AS was shown to be 28,558 ng/mL while the Cmax of DHA was determined to be 2,932 ng/mL."( Pharmacokinetic evaluation of intravenous artesunate in adults with uncomplicated falciparum malaria in Kenya: a phase II study.
Hickman, MR; Li, Q; Melendez, V; Miller, SR; Ogutu, B; Otieno, W; Polhemus, M; Remich, S; Smith, B; Teja-Isavadharm, P; Weina, PJ, 2014
)
0.4
" Given the much longer half-life of DHA compared to the short half-life of AS, DHA also plays a significant role in treatment of severe malaria."( Pharmacokinetic evaluation of intravenous artesunate in adults with uncomplicated falciparum malaria in Kenya: a phase II study.
Hickman, MR; Li, Q; Melendez, V; Miller, SR; Ogutu, B; Otieno, W; Polhemus, M; Remich, S; Smith, B; Teja-Isavadharm, P; Weina, PJ, 2014
)
0.4
" The noncompartmental pharmacokinetic parameters were computed for metoprolol, its metabolite alpha-hydroxymetoprolol, and pyronaridine."( Pharmacokinetic interaction between pyronaridine-artesunate and metoprolol.
Arbe-Barnes, S; Borghini-Fuhrer, I; Duparc, S; Fleckenstein, L; Lopez-Lazaro, L; Miller, RM; Morris, CA; Pokorny, R; Shin, JS, 2014
)
0.4
" A combined drug-metabolite population pharmacokinetic model was developed to describe the plasma pharmacokinetics of ARS and DHA in plasma."( Population pharmacokinetics of artesunate and dihydroartemisinin during long-term oral administration of artesunate to patients with metastatic breast cancer.
Äbelö, A; Ashton, M; Blank, A; Ericsson, T; von Hagens, C, 2014
)
0.4
" Population pharmacokinetic modelling was conducted using NONMEM."( Population pharmacokinetics of orally administered mefloquine in healthy volunteers and patients with uncomplicated Plasmodium falciparum malaria.
Evans, AM; Navaratnam, V; Olliaro, PL; Reuter, SE; Upton, RN, 2015
)
0.42
" Monte Carlo simulations predict that falciparum malaria infection is associated with a shorter elimination half-life (407 versus 566 h) and T>MIC (766 versus 893 h)."( Population pharmacokinetics of orally administered mefloquine in healthy volunteers and patients with uncomplicated Plasmodium falciparum malaria.
Evans, AM; Navaratnam, V; Olliaro, PL; Reuter, SE; Upton, RN, 2015
)
0.42
"This is the first known population pharmacokinetic study to show falciparum malaria to influence mefloquine disposition."( Population pharmacokinetics of orally administered mefloquine in healthy volunteers and patients with uncomplicated Plasmodium falciparum malaria.
Evans, AM; Navaratnam, V; Olliaro, PL; Reuter, SE; Upton, RN, 2015
)
0.42
" A single-dose, randomized, three-sequence crossover study was conducted in healthy Thai volunteers to characterize potential pharmacokinetic interactions between these drugs."( Pharmacokinetic interactions between primaquine and pyronaridine-artesunate in healthy adult Thai subjects.
Ashley, EA; Blessborn, D; Chairat, K; Day, NP; Hanboonkunupakarn, B; Jittamala, P; Lee, SJ; Nosten, F; Panapipat, S; Pukrittayakamee, S; Tarning, J; Thana, P; White, NJ, 2015
)
0.42
" Malaria and pregnancy had no effect on the pharmacokinetic properties of artesunate or dihydroartemisinin after intravenous artesunate administration."( Opposite malaria and pregnancy effect on oral bioavailability of artesunate - a population pharmacokinetic evaluation.
Day, NP; Hanpithakpon, W; Hlaing, N; Kloprogge, F; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Tarning, J; Than, HH; White, NJ; Zin, NT, 2015
)
0.42
"The population pharmacokinetic analysis demonstrated opposite effects of malaria and pregnancy on the bioavailability of orally administered artesunate."( Opposite malaria and pregnancy effect on oral bioavailability of artesunate - a population pharmacokinetic evaluation.
Day, NP; Hanpithakpon, W; Hlaing, N; Kloprogge, F; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Tarning, J; Than, HH; White, NJ; Zin, NT, 2015
)
0.42
" In summary, the LC-MS/MS metho described herein was fully successfully applied to pharmacokinetic studies of artesunate nanoemulsion after intramuscular delivery to sheep."( Determination and pharmacokinetic studies of artesunate and its metabolite in sheep plasma by liquid chromatography-tandem mass spectrometry.
Li, B; Li, JS; Li, JY; Liu, XW; Niu, JR; Wei, XJ; Yang, YJ; Zhang, J; Zhang, JY; Zhou, XZ, 2015
)
0.42
" The aim of the study was to investigate the pharmacokinetic interaction between the anti-malarial drugs, artesunate-mefloquine and the antiretroviral drug, lopinavir boosted with ritonavir (LPV/r)."( Pharmacokinetic interactions between artesunate-mefloquine and ritonavir-boosted lopinavir in healthy Thai adults.
Cressey, TR; Kongjam, P; Na-Bangchang, K; Rattanapunya, S; Rueangweerayut, R; Tawon, Y, 2015
)
0.42
"The study was an open-label, three-way, sequential, cross-over, pharmacokinetic study in healthy Thai adults."( Pharmacokinetic interactions between artesunate-mefloquine and ritonavir-boosted lopinavir in healthy Thai adults.
Cressey, TR; Kongjam, P; Na-Bangchang, K; Rattanapunya, S; Rueangweerayut, R; Tawon, Y, 2015
)
0.42
" Nonlinear mixed-effects modeling using NONMEM software was used to obtain the pharmacokinetic and inter- and intraindividual variability parameter estimates."( Population Pharmacokinetics of Pyronaridine in Pediatric Malaria Patients.
Ayyoub, A; Borghini-Fuhrer, I; Djimde, AA; Duparc, S; Fleckenstein, L; Methaneethorn, J; Ramharter, M; Shin, JS; Tekete, M, 2015
)
0.42
" Blood samples were obtained after the first dose within 6 h for pharmacokinetic (PK) and ex vivo pharmacodynamic evaluation by simultaneously measuring plasma drug concentration and anti-malarial activity against Plasmodium falciparum in vitro."( Comparative pharmacokinetics and pharmacodynamics of intravenous artelinate versus artesunate in uncomplicated Plasmodium coatneyi-infected rhesus monkey model.
Chanarat, N; Gettayacamin, M; Komcharoen, N; Limsalakpeth, A; Rasameesoraj, M; Saunders, DL; Scott Miller, R; Siriyanonda, D; Teja-Isavadharm, P; Weina, PJ, 2016
)
0.43
" This work aimed to evaluate the pharmacokinetic and pharmacodynamic properties of artesunate and its active metabolite, dihydroartemisinin, in patients with sensitive and resistant falciparum infections in Southern Myanmar."( Population pharmacokinetic and pharmacodynamic properties of artesunate in patients with artemisinin sensitive and resistant infections in Southern Myanmar.
Aye, KH; Aye, MM; Bergstrand, M; Chit, K; Karlsson, MO; Kyaw, MP; Lohy Das, JP; Nyunt, MH; Tarning, J, 2018
)
0.48
" The pharmacokinetic studies indicated ARS-TPGS-Lipo had higher AUC, longer circulation time and better liver targeting."( The characterization, pharmacokinetic, and tissue distribution studies of TPGS-modified artesunate liposome in rats.
An, R; Hu, C; Liang, K; Wang, X; You, L, 2018
)
0.48
"Characterization of the pharmacokinetic properties of the enantiomers of primaquine and carboxyprimaquine following administration of racemic primaquine given alone and in combination with commonly used antimalarial drugs."( Enantiospecific pharmacokinetics and drug-drug interactions of primaquine and blood-stage antimalarial drugs.
Blessborn, D; Chairat, K; Day, NPJ; Hanboonkunupakarn, B; Hanpithakpong, W; Jittamala, P; Pukrittayakamee, S; Tarning, J; White, NJ, 2018
)
0.48
"Population pharmacokinetic models characterizing the enantiospecific properties of primaquine were developed successfully."( Enantiospecific pharmacokinetics and drug-drug interactions of primaquine and blood-stage antimalarial drugs.
Blessborn, D; Chairat, K; Day, NPJ; Hanboonkunupakarn, B; Hanpithakpong, W; Jittamala, P; Pukrittayakamee, S; Tarning, J; White, NJ, 2018
)
0.48
" In untreated mice, pRBCs were removed from circulation with a half-life of 15."( Quantification of host-mediated parasite clearance during blood-stage Plasmodium infection and anti-malarial drug treatment in mice.
Akter, J; Aogo, RA; Cromer, D; Davenport, MP; Elliott, T; Fogg, LG; Haque, A; Khoury, DS; Laohamonthonkul, P; Liligeto, UN; Nair, AS; Pernold, CPS; Romanczuk, AS; Soon, MSF; Thomas, BS, 2018
)
0.48
" The present study aimed to develop a population pharmacokinetic model for mefloquine based on whole blood concentration-time profiles of this target population for further dose optimization."( Population pharmacokinetics of mefloquine given as a 3-day artesunate-mefloquine in patients with acute uncomplicated Plasmodium falciparum malaria in a multidrug-resistant area along the Thai-Myanmar border.
Hoglund, RM; Na-Bangchang, K; Ruengweerayut, R, 2018
)
0.48
" A non-linear mixed-effect modelling approach was applied for population pharmacokinetic analysis using the NONMEM v7."( Population pharmacokinetics of mefloquine given as a 3-day artesunate-mefloquine in patients with acute uncomplicated Plasmodium falciparum malaria in a multidrug-resistant area along the Thai-Myanmar border.
Hoglund, RM; Na-Bangchang, K; Ruengweerayut, R, 2018
)
0.48
"Population pharmacokinetic analysis of mefloquine was performed in all patients with a total of 653 samples."( Population pharmacokinetics of mefloquine given as a 3-day artesunate-mefloquine in patients with acute uncomplicated Plasmodium falciparum malaria in a multidrug-resistant area along the Thai-Myanmar border.
Hoglund, RM; Na-Bangchang, K; Ruengweerayut, R, 2018
)
0.48
" Study endpoints were; parasite clearance half-life (the time required for parasitaemia to decrease by 50% based on the linear portion of the parasite clearance slope) and parasite clearance time (time required for complete clearance of initial parasitaemia)."( Assessment of parasite clearance following treatment of severe malaria with intravenous artesunate in Ugandan children enrolled in a randomized controlled clinical trial.
Byakika-Kibwika, P; Kiragga, AN; Lamorde, M; Nyakato, P, 2018
)
0.48
" A comprehensive understanding of the pharmacokinetic characteristics of AS will be conducive to the further development of new pharmacological actions and clinical application of AS."( [Research progress on pharmacokinetics and pharmacological activities of artesunate].
Cen, YY; Li, P; Li, XL; Zao, YB; Zeng, XX; Zhou, H, 2018
)
0.48
"The World Health Organization (WHO) recommends combinations of an artemisinin derivative plus an anti-malarial drug of longer half-life as treatment options for uncomplicated Plasmodium falciparum infections."( Population pharmacokinetics and pharmacodynamics of the artesunate-mefloquine fixed dose combination for the treatment of uncomplicated falciparum malaria in African children.
Aouri, M; Carn, G; Csajka, C; Decosterd, LA; Guidi, M; Kiechel, JR; Mercier, T; Ogutu, B, 2019
)
0.51
"The population pharmacokinetic models developed for both AS/DHA and MQ showed a large variability in drug exposure in the investigated African paediatric population."( Population pharmacokinetics and pharmacodynamics of the artesunate-mefloquine fixed dose combination for the treatment of uncomplicated falciparum malaria in African children.
Aouri, M; Carn, G; Csajka, C; Decosterd, LA; Guidi, M; Kiechel, JR; Mercier, T; Ogutu, B, 2019
)
0.51
" Regression analyses assessed the effects of antibody seropositivity on the parasite clearance half-life (PC½), having a PC½ of ≥5 hours, and having parasitemia 3 days after treatment."( Contribution of Functional Antimalarial Immunity to Measures of Parasite Clearance in Therapeutic Efficacy Studies of Artemisinin Derivatives.
Amaratunga, C; Ashley, EA; Ataíde, R; Beeson, JG; Day, NP; Dhorda, M; Dondorp, AM; Fairhurst, RM; Faiz, MA; Feng, G; Fowkes, FJI; Hien, TT; Htut, Y; Lim, P; Mayxay, M; Nosten, F; O'Flaherty, K; Powell, R; Pukrittayakamee, S; Reiling, L; Simpson, JA; White, NJ; Zaloumis, SG, 2019
)
0.51
" All studies on ART and DHA pharmacokinetic post-administration of artesunate in human patients or volunteers were included."( Systematic review of artesunate pharmacokinetics: Implication for treatment of resistant malaria.
Bienvenu, AL; Bonnot, G; Kouakou, YI; Lavoignat, A; Leboucher, G; Picot, S; Tod, M, 2019
)
0.51
" Parasitemia slope half-life was calculated after microscopy."( Different Plasmodium falciparum clearance times in two Malian villages following artesunate monotherapy.
Beshir, KB; Coulibaly, A; Dembele, D; Diallo, N; Djimde, AA; Doumbo, OK; Fofana, B; Gil, JP; Haidara, AS; Haidara, K; Kone, A; Sagara, I; Sangare, CO; Sanogo, K; Sissoko, S; Toure, S; Traore, A, 2020
)
0.56
" We calculated the parasite clearance (CL) half-life using the Worldwide Antimalarial Resistance Network (WWARN) online parasite clearance estimator (PCE)."( Slow parasite clearance, absent K13-propeller gene polymorphisms and adequate artesunate levels among patients with malaria: A pilot study from southern India.
Bhattacharjee, S; Jayaseelan, V; Kumar, S; Mammen, JJ; Mathew, BS; Miraclin, TA; Prabhakar Abhilash, KP; Ramachandran, SV; Rupali, P; Sathyendra, S; Sudarsanam, TD,
)
0.13
" To optimally apply these drugs, information about their tissue-specific disposition is required, and one approach to predict these pharmacokinetic characteristics is physiologically based pharmacokinetic (PBPK) modeling."( Predicting the Disposition of the Antimalarial Drug Artesunate and Its Active Metabolite Dihydroartemisinin Using Physiologically Based Pharmacokinetic Modeling.
Arey, R; Reisfeld, B, 2021
)
0.62
"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
)
0.62

Compound-Compound Interactions

ExcerptReferenceRelevance
"A randomized comparative trial of the pharmacokinetics and pharmacodynamics of oral doses of mefloquine and of mefloquine in combination with artesunate was carried out on 20 Thai male patients with acute, uncomplicated falciparum malaria."( Pharmacokinetics of mefloquine alone or in combination with artesunate.
Back, DJ; Bunnag, D; Harinasuta, T; Karbwang, J; Na Bangchang, K; Thanavibul, A, 1994
)
0.29
"A randomized comparative trial of the pharmacokinetics and pharmacodynamics of oral doses of mefloquine and of mefloquine in combination with artesunate was carried out on 20 Thai male patients with acute, uncomplicated falciparum malaria."( Pharmacokinetics of mefloquine alone or in combination with artesunate.
Back, DJ; Bunnag, D; Harinasuta, T; Karbwang, J; Na Bangchang, K; Thanavibul, A, 1994
)
0.29
"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,
)
0.13
" Early disappearance of fever and parasitemia, and absence of important side effects suggest that artesunate, isolated or administrated in combination with mefloquine, constitutes an able therapeutical procedure to constitutes and able therapeutical procedure to contribute for disease control in that region."( [An efficacy and tolerance study of oral artesunate alone and in combination with mefloquine in the treatment of uncomplicated falciparum malaria in an endemic area of Pará, Brazil].
Amoras, WW; Baena, J; Cardoso, Bda S; Crescente, JA; Dourado, HV; Pinheiro, Mda C; Saraty, S,
)
0.13
"A randomized pilot study to compare the safety and efficacy of artesunate suppositories (15 mg/kg/day for three days) versus oral artesunate (6 mg/kg/day for three days), both in combination with mefloquine (25 mg/kg), was conducted in 52 Thai children with uncomplicated multidrug-resistant falciparum malaria."( Comparative clinical trial of artesunate suppositories and oral artesunate in combination with mefloquine in the treatment of children with acute falciparum malaria.
Attanath, P; Brewer, TG; Chanthavanich, P; Chongsuphajaisiddhi, T; Heppner, DG; Mookmanee, D; Phanuaksook, P; Poonpanich, Y; Prarinyanupharb, V; Sabchareon, A; Teja-Isavadharm, P, 1998
)
0.3
" In combination with artesunate, mefloquine administration should be delayed until the second or third day after presentation."( Pharmacokinetics of mefloquine combined with artesunate in children with acute falciparum malaria.
Chongsuphajaisiddhi, T; Heppner, DG; Luxemburger, C; Nosten, F; Price, R; Simpson, JA; Teja-Isavatharm, P; Than, MM; White, NJ, 1999
)
0.3
"A cross sectional study was carried out in a rural area of Myanmar to identify malaria patients' acceptance of artesunate plus mefloquine drug combination and to determine the cost borne by patients."( Acceptance of short course artesunate plus mefloquine drug combination by malaria patients in rural Myanmar.
Aung, S; Lwin, M; Mar, KK; Shwe, T; Win, LL; Zaw, AK, 1999
)
0.3
" From September to December 1998, 598 children with uncomplicated malaria were treated; 135 received chloroquine (CQ) alone, 276 received pyrimethamine/sulfadoxine (Fansidar, PSD) alone, 113 received PSD with a single dose of artesunate (PSD + 1ART) and 74 received PSD combined with three doses of artesunate (PSD + 3ART)."( Parasitaemia and gametocytaemia after treatment with chloroquine, pyrimethamine/sulfadoxine, and pyrimethamine/sulfadoxine combined with artesunate in young Gambians with uncomplicated malaria.
Coleman, R; Doherty, T; Jawara, M; Targett, G; von Seidlein, L; Walraven, G, 2001
)
0.31
" Overall 14,017 (85%) individuals living in the study area were treated with either placebo or sulfadoxine-pyrimethamine (SP) combined with a single dose of artesunate (AS)."( The effect of mass administration of sulfadoxine-pyrimethamine combined with artesunate on malaria incidence: a double-blind, community-randomized, placebo-controlled trial in The Gambia.
Alexander, N; Bennett, S; Coleman, R; De Martin, S; Deen, JL; Doherty, JF; Drakeley, C; Greenwood, BM; Jawara, M; Lindsay, SW; Manneh, F; McAdam, KP; Milligan, PJ; Okunoye, K; Olliaro, P; Pinder, M; Schim van der Loeff, M; Targett, GA; von Seidlein, L; Walraven, G,
)
0.13
"The effectiveness of chloroquine or sulfadoxine-pyrimethamine administered with artesunate for treating uncomplicated falciparum malaria was assessed in 2 Vietnamese provinces where the sensitivity of parasites in vitro to conventional therapies had increased with the removal of drug pressure."( Treatment of uncomplicated falciparum malaria in southern Vietnam: can chloroquine or sulfadoxine-pyrimethamine be reintroduced in combination with artesunate?
Cox-Singh, J; Davis, TM; Doan, HN; Hewitt, S; Le, DC; Nguyen, MH; Nguyen, TH; Tran, BK; Tran, QT; Vo, NP, 2003
)
0.32
"We investigated the safety and efficacy of amodiaquine alone (AQ) and combined with artesunate (AQ + AS) in 308 Rwandan children 6-59 months old with uncomplicated Plasmodium falciparum malaria attending three sentinel sites."( Is amodiaquine failing in Rwanda? Efficacy of amodiaquine alone and combined with artesunate in children with uncomplicated malaria.
D'Alessandro, U; Dujardin, JC; Erhart, A; Karema, C; Mugisha, V; Ringwald, P; Rwagacondo, CE; Van Overmeir, C, 2004
)
0.32
" Further studies are now required to determine whether DDS, CPG or an as-yet unidentified metabolite of CPG interact with ASN, and whether a simple double combination of ASN with one or other of these would be as protective, against the selection of resistance, as CDA."( The chemotherapy of rodent malaria. LXIII. Drug combinations to impede the selection of drug resistance, part 6: the potential value of chlorproguanil and dapsone in combination, and with the addition of artesunate.
Peters, W; Robinson, BL; Stewart, LB, 2005
)
0.33
" We conclude that atovaquone-proguanil shows no evidence of cardiotoxicity either alone or when combined with artesunate."( Short report: no evidence of cardiotoxicity of atovaquone-proguanil alone or in combination with artesunate.
Gupta, RK; Looareesuwan, S; Nosten, F; Paiphun, L; Slight, T; Van Vugt, M; White, NJ, 2005
)
0.33
" We therefore evaluated three-day treatment with artesunate combined with either 2 or 3 days of mefloquine co-administered once a day with artesunate."( An open, randomized trial of three-day treatment with artesunate combined with a standard dose of mefloquine divided over either two or three days, for acute, uncomplicated falciparum malaria.
Chalermrut, K; Krudsood, S; Leowattana, W; Looareesuwan, S; Silachamroon, U; Srivilairit, S; Tangpukdee, N; Thanachartwet, W; Thimasarn, K; Wilaiaratana, P, 2005
)
0.33
" This study was designed to compare the efficacy and toxicity of artesunate combined with NP (a chemotherapy regimen of vinorelbine and cisplatin) and NP alone in the treatment of advanced non-small cell lung cancer (NSCLC)."( [Artesunate combined with vinorelbine plus cisplatin in treatment of advanced non-small cell lung cancer: a randomized controlled trial].
Huang, XY; Li, DQ; Miao, LY; Xia, XH; Yu, SQ; Zhang, XP; Zhang, ZY; Zhu, YP, 2008
)
0.35
" Artesunate combined with NP can elevate the short-term survival rate and prolong the TTP of patients with advanced NSCLC without extra side effects."( [Artesunate combined with vinorelbine plus cisplatin in treatment of advanced non-small cell lung cancer: a randomized controlled trial].
Huang, XY; Li, DQ; Miao, LY; Xia, XH; Yu, SQ; Zhang, XP; Zhang, ZY; Zhu, YP, 2008
)
0.35
"MB-AQ is a promising alternative drug combination against malaria in Africa."( Safety and efficacy of methylene blue combined with artesunate or amodiaquine for uncomplicated falciparum malaria: a randomized controlled trial from Burkina Faso.
Coulibaly, B; Klose, C; Kouyaté, B; Mansmann, U; Meissner, P; Mockenhaupt, FP; Müller, O; Schirmer, RH; Sié, A; Walter-Sack, I; Zoungrana, A, 2008
)
0.35
"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
)
0.37
" In the present study, we firstly found that artesunate in combination with oxacillin was capable of protecting mice challenged with live MRSA WHO-2 (WHO-2) and the protection was related to the reduced TNF-α and IL-6 levels and decreased bacterial load."( Artesunate in combination with oxacillin protect sepsis model mice challenged with lethal live methicillin-resistant Staphylococcus aureus (MRSA) via its inhibition on proinflammatory cytokines release and enhancement on antibacterial activity of oxacilli
Cao, H; Cen, Y; Jiang, W; Li, B; Li, J; Liu, X; Pan, X; Zheng, J; Zheng, X; Zhou, H, 2011
)
0.37
"Forty-six patients in a remote health post of Amazonas, Venezuela, accidentally received artesunate in a dose of 10 mg/kg/day combined with mefloquine."( High dose artesunate in combination with mefloquine: pharmacovigilance in the Venezuelan Amazon.
Brooms, JD; Cruz, L; España, R; Giron, A; Magris, M; Metzger, WG; Peña Pimentel, FN; Perez, L; Villalobos, N; Vivas-Martínez, S, 2012
)
0.38
"A multiple dose, parallel group study was conducted to assess for a drug-drug interaction between the pyronaridine/artesunate (PA) combination antimalarial and ritonavir."( Drug-drug interaction analysis of pyronaridine/artesunate and ritonavir in healthy volunteers.
Borghini-Fuhrer, I; Duparc, S; Fleckenstein, L; Jung, D; Lopez-Lazaro, L; Methaneethorn, J; Morris, CA; Pokorny, R; Shin, CS, 2012
)
0.38
" Participants were randomized to receive chloroquine alone or combined with artesunate, azithromycin or atovaquone-proguanil for all episodes of uncomplicated malaria for one year."( A longitudinal trial comparing chloroquine as monotherapy or in combination with artesunate, azithromycin or atovaquone-proguanil to treat malaria.
Dzinjalamala, FK; Laufer, MK; Laurens, MB; Masonga, R; Nyirenda, OM; Plowe, CV; Stokes-Riner, A; Taylor, TE; Thesing, PC, 2012
)
0.38
" This object of this report was to document synergistic effects of artesunate combined with allicin on osteosarcoma cell lines in vitro and in vivo."( The synergistic anticancer effect of artesunate combined with allicin in osteosarcoma cell line in vitro and in vivo.
Huang, Y; Jiang, W; Wang, JP; Yu, XY; Zhang, LY, 2013
)
0.39
"Artesunate (AS) in combination with sulfadoxine/pyrimethamine (SP) is the first-line therapy for management of uncomplicated Plasmodium falciparum malaria in Sudan."( Pharmacokinetics of artesunate alone and in combination with sulfadoxine/pyrimethamine in healthy Sudanese volunteers.
Awad, AI; Elamin, SB; Matar, KM, 2014
)
0.4
"05) were reduced in mice treated with VACV combined with ART versus VACV alone."( Valacyclovir combined with artesunate or rapamycin improves the outcome of herpes simplex virus encephalitis in mice compared to antiviral therapy alone.
Boivin, G; Canivet, C; Menasria, R; Piret, J; Rhéaume, C, 2015
)
0.42
" alata leaf extracts, administered alone or in combination with Artesunate (ART) in malaria treatment."( Efficacy of Lophira alata Leaf Extract and its Combination with Artesunate in Mice Prior Exposed to Plasmodium berghei.
Falade, MO; Komoni, F; Nwuba, RI, 2018
)
0.48
"Characterization of the pharmacokinetic properties of the enantiomers of primaquine and carboxyprimaquine following administration of racemic primaquine given alone and in combination with commonly used antimalarial drugs."( Enantiospecific pharmacokinetics and drug-drug interactions of primaquine and blood-stage antimalarial drugs.
Blessborn, D; Chairat, K; Day, NPJ; Hanboonkunupakarn, B; Hanpithakpong, W; Jittamala, P; Pukrittayakamee, S; Tarning, J; White, NJ, 2018
)
0.48
"Enantiomeric pharmacokinetics were evaluated in 49 healthy adult volunteers enrolled in three randomized cross-over studies in which a single dose of primaquine was given alone and then, after a suitable washout period, in combination with chloroquine, dihydroartemisinin/piperaquine or pyronaridine/artesunate."( Enantiospecific pharmacokinetics and drug-drug interactions of primaquine and blood-stage antimalarial drugs.
Blessborn, D; Chairat, K; Day, NPJ; Hanboonkunupakarn, B; Hanpithakpong, W; Jittamala, P; Pukrittayakamee, S; Tarning, J; White, NJ, 2018
)
0.48
" No drug-drug interaction effects were seen on the pharmacokinetics of either carboxyprimaquine enantiomer."( Enantiospecific pharmacokinetics and drug-drug interactions of primaquine and blood-stage antimalarial drugs.
Blessborn, D; Chairat, K; Day, NPJ; Hanboonkunupakarn, B; Hanpithakpong, W; Jittamala, P; Pukrittayakamee, S; Tarning, J; White, NJ, 2018
)
0.48
" 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
)
0.51
" Primaquine (PQ) and methylene blue (MB) are gametocytocidal drugs that can be combined with artemisinin-based combination therapy (ACT) to reduce malaria transmission, including resistant strains."( Safety and efficacy of artesunate-amodiaquine combined with either methylene blue or primaquine in children with falciparum malaria in Burkina Faso: A randomized controlled trial.
Compaoré, G; Coulibaly, B; D Alessandro, U; Jahn, A; Kieser, M; Klose, C; Krisam, J; Lu, G; Meissner, P; Mendes Jorge, M; Mockenhaupt, FP; Müller, O; Nebie, E; Ouermi, L; Sié, A, 2019
)
0.51
"Artesunate combined with fractional CO2 laser is effective in hypertrophic scarring in this rabbit model."( Effectiveness of artesunate combined with fractional CO2 laser in a hypertrophic scar model with underlying mechanism.
Cheng, X; Luo, W; Peng, Z; Xia, Z; Yang, R; Zhang, J; Zhou, S, 2022
)
0.72
"Artesunate combined with arsenous acid inhibits proliferation and promotes apoptosis of tumor cells through PI3K/AKT signaling pathway, and is superior to the effect of two drugs alone."( [Effects of Artesunate Combined with Arsenious Acid on Proliferation and Apoptosis of Multiple Myeloma Cells via PI3K/AKT Signaling Pathway].
Dong, JF; Dong, K; Gao, W; Hu, GF; Wang, Y, 2021
)
0.62
" 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
" A revisiting on mefloquine pharmacokinetics-pharmacodynamics (PK/PD) could assist in finding new appropriate dosage regimens in combination with artesunate as a three-day course treatment."( Prediction of improved antimalarial chemotherapy of artesunate-mefloquine in combination with mefloquine sensitive and resistant Plasmodium falciparum malaria.
Na-Bangchang, K; Saeheng, T, 2023
)
0.91
" Therefore, this study investigated the effects of MET combined with ART combination therapy on autophagy and apoptosis in GBM cells."( Lower dose of metformin combined with artesunate induced autophagy-dependent apoptosis of glioblastoma by activating ROS-AMPK-mTOR axis.
Ding, W; Liao, L; Liao, Y; Liu, J; Tang, Q; Zhao, J, 2023
)
0.91
" Ethanolic extracts of Atractylodes lancea (a dose of 400 mg/kg) and Prabchompoothaweep remedy (a dose of 600 mg/kg) were evaluated as monotherapy and adjunctive therapy combined with artesunate at the onset of signs of cerebral malaria and continued for 7 consecutive days."( Efficacy of artesunate combined with Atractylodes lancea or Prabchompoothaweep remedy extracts as adjunctive therapy for the treatment of cerebral malaria.
Chaniad, P; Konyanee, A; Phuwajaroanpong, A; Plirat, W; Punsawad, C; Septama, AW; Viriyavejakul, P, 2023
)
0.91

Bioavailability

ExcerptReferenceRelevance
" Moderate oral bioavailability has been suggested as a possible cause."( Transport of artemisinin and sodium artesunate in Caco-2 intestinal epithelial cells.
Augustijns, P; D'Hulst, A; Kinget, R; Van Daele, J, 1996
)
0.29
" Delaying administration of mefloquine until day 2 was associated with a mean (95% confidence interval) increase in estimated oral bioavailability of 72% (36 to 109%)."( Pharmacokinetics of mefloquine combined with artesunate in children with acute falciparum malaria.
Chongsuphajaisiddhi, T; Heppner, DG; Luxemburger, C; Nosten, F; Price, R; Simpson, JA; Teja-Isavatharm, P; Than, MM; White, NJ, 1999
)
0.3
" If it is assumed that apparent clearance and volume of distribution are unaffected by dose regimen, then splitting the 25 mg/kg mefloquine dose improves oral bioavailability and the therapeutic response in the treatment of acute falciparum malaria."( Population pharmacokinetics of mefloquine in patients with acute falciparum malaria.
Aarons, L; Chongsuphajaisiddhi, T; Looareesuwan, S; Nosten, F; Price, R; Simpson, JA; Teja-Isavatharm, P; ter Kuile, F; White, NJ, 1999
)
0.3
" The mean absolute oral bioavailability of the antimalarial agent in patients with acute malaria was 61% (95% confidence interval [CI], 52 to 70%)."( Antimalarial bioavailability and disposition of artesunate in acute falciparum malaria.
Bates, I; Navaratnam, V; Newton, P; Pukrittayakamee, S; Suputtamongkol, Y; Teja-Isavadharm, P; White, N, 2000
)
0.31
" 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
)
0.31
" 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
)
0.31
"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
)
0.31
"34 hr, and the bioavailability over 12 hr (area under the curve [AUC](0-12)) was 253+/-185 nmol hr/L."( Comparative pharmacokinetics and effect kinetics of orally administered artesunate in healthy volunteers and patients with uncomplicated falciparum malaria.
Brewer, TG; Eamsila, C; Jongsakul, K; Keeratithakul, G; Kyle, DE; Li, Q; Luesutthiviboon, L; Sirisopana, N; Teja-Isavadharm, P; Watt, G, 2001
)
0.31
" The mean antimalarial activity in terms of the bioavailability of DHA relative to that of artesunate did not differ significantly from 1, suggesting that DHA can be formulated to be an acceptable oral alternative to artesunate."( Comparison of oral artesunate and dihydroartemisinin antimalarial bioavailabilities in acute falciparum malaria.
Looareesuwan, S; Newton, PN; Nosten, F; Rasameesoroj, M; Ruangveerayuth, R; Siriyanonda, D; Slight, T; Suputtamongkol, Y; Teerapong, P; Teja-Isavadharm, P; van Vugt, M; White, NJ, 2002
)
0.31
"The aim of this study was to evaluate the bioavailability of artesunate (ARTS) and dihydroartemisinin (DHA)."( Relative bioavailability of artesunate and dihydroartemisinin: investigations in the isolated perfused rat liver and in healthy Caucasian volunteers.
Batty, KT; Davis, TM; Iletr, KE; Martin, J; Powell, SM, 2002
)
0.31
" We studied the pharmacokinetics and bioavailability of ARS given by the intramuscular (i."( Intramuscular bioavailability and clinical efficacy of artesunate in gabonese children with severe malaria.
Dzeing, A; Kombila, M; Kremsner, PG; Krishna, S; Müller-Römer, U; Nealon, C; Parzy, D; Planche, T; Sinou, V, 2002
)
0.31
" The relative bioavailability of rectal artesunate was [mean (coefficient of variation %) 54."( Pharmacokinetics of artesunate following oral and rectal administration in healthy Sudanese volunteers.
Alkadru, AM; Awad, MI; Baraka, OZ; Behrens, RH; Eltayeb, IB, 2004
)
0.32
" The mean common volumes of distribution for ARTS and DHA relative to bioavailability were 42."( Disposition of artesunate and dihydroartemisinin after administration of artesunate suppositories in children from Papua New Guinea with uncomplicated malaria.
Alpers, MP; Barrett, PH; Bockarie, M; Davis, TM; Dufall, K; Ilett, KF; Karunajeewa, HA; Kemiki, A; Vicini, P, 2004
)
0.32
"Food has been reported to increase the bioavailability of mefloquine in healthy volunteers, but its role in increasing blood mefloquine concentrations in malaria patients treated with mefloquine is unclear."( Fatty food does not alter blood mefloquine concentrations in the treatment of falciparum malaria.
Binh, VQ; Dai, B; Dao, NV; Edstein, MD; Ngoa, ND; Quoc, NP; Rieckmann, KH; The, ND; Thuy, le T, 2005
)
0.33
" Splitting the 25 mg/kg dose of mefloquine into three doses of 8 mg/kg each resulted in improved oral bioavailability compared to the conventional split-dose regimen results."( Population pharmacokinetic assessment of a new regimen of mefloquine used in combination treatment of uncomplicated falciparum malaria.
Ashley, EA; Hae, R; Hutagalung, R; Lindegårdh, N; McGready, R; Nosten, F; Singhasivanon, P; Stepniewska, K; White, NJ, 2006
)
0.33
" Patients with the lowest area under the DHA concentration curve did not have slower parasite clearance, suggesting that rectal artesunate is well absorbed in most patients with moderately severe malaria."( Population pharmacokinetics of artesunate and dihydroartemisinin following intra-rectal dosing of artesunate in malaria patients.
Agbenyega, T; Barnes, KI; Di Perri, G; Folb, P; Gomes, M; Krishna, S; Krudsood, S; Looareesuwan, S; Mansor, S; McIlleron, H; Miller, R; Molyneux, M; Mwenechanya, J; Navaratnam, V; Nosten, F; Olliaro, P; Pang, L; Ribeiro, I; Simpson, JA; Tembo, M; van Vugt, M; Ward, S; Weerasuriya, K; White, NJ; Win, K, 2006
)
0.33
" This thermolability coupled with the poor physicochemical properties and relative oral bioavailability of DHA suggests that it is inferior to artesunate in application as an antimalarial drug."( Artesunate and dihydroartemisinin (DHA): unusual decomposition products formed under mild conditions and comments on the fitness of DHA as an antimalarial drug.
Cartwright, A; Chan, HW; Gomes, MF; Haynes, RK; Lung, CM; Ng, NC; Shek, LY; Williams, ID; Wong, HN, 2007
)
0.34
" Improvement can be made in terms of rectal bioavailability and stability of current formulations."( In vitro release and stability of an artesunate rectal gel suitable for pediatric use.
Barbaud, A; Boyer, C; Dubost, JP; Fawaz, F; Gaudin, K; Lagueny, AM; Langlois, MH; Millet, P, 2008
)
0.35
"79 L/kg); the bioavailability was 100%."( Pharmacokinetics of artesunate in the domestic pig.
Aglioni, C; Bressolle, FM; Mosnier, J; Parzy, D; Sinou, V; Taudon, N, 2008
)
0.35
" Pharmacokinetic analysis revealed a dose-dependent increase in the maximum plasma/blood concentration and the area under the curve, as well as comparable relative bioavailability for the granule coformulation."( Fixed-dose pyronaridine-artesunate combination for treatment of uncomplicated falciparum malaria in pediatric patients in Gabon.
Bélard, S; Cisse, B; Fleckenstein, L; Glasenapp, Iv; Issifou, S; Kammer, J; Koumba, PK; Kremsner, PG; Kurth, F; Lell, B; Mordmüller, B; Nemeth, J; Oeuvray, C; Ramharter, M; Schlie, M; Schreier, AC, 2008
)
0.35
" The method is sensitive, selective, accurate, reproducible and suited particularly for pharmacokinetic study of AS-AQ drug combination and can also be used to compare the bioavailability of different formulations, including a fixed-dose AS-AQ co-formulation."( Validation of high performance liquid chromatography-electrochemical detection methods with simultaneous extraction procedure for the determination of artesunate, dihydroartemisinin, amodiaquine and desethylamodiaquine in human plasma for application in c
Lai, CS; Mansor, SM; Muniandy, A; Nair, NK; Navaratnam, V; Olliaro, PL, 2009
)
0.35
" This study examines the bioavailability and tolerability of a fixed (200 mg artesunate + 540 mg amodiaquine) and loose (200 mg + 612 mg) combination with a 2x2 cross-over design in 24 healthy volunteers."( Tolerability and pharmacokinetics of non-fixed and fixed combinations of artesunate and amodiaquine in Malaysian healthy normal volunteers.
Kiechel, JR; Mansor, SM; Navaratnam, V; Olliaro, P; Ramanathan, S; Siew Hua, G; Taylor, WR; Vaillant, M; Wahab, MS, 2009
)
0.35
" Relative bioavailability between products was compared by estimating the ratios (and 95% CI) between the areas under the plasma concentration-time curves (AUC)."( Population pharmacokinetics of artesunate and amodiaquine in African children.
Gansané, A; Kiechel, JR; Morgan, CC; Ouedraogo, A; Ouedraogo, EB; Simpson, JA; Sirima, SB; Stepniewska, K; Taylor, W; White, NJ, 2009
)
0.35
"The bioavailability of the co-formulated AS-AQ FDC was similar to that of the separate tablets for desethylamodiaquine, DHA and the total anti-malarial activity."( Population pharmacokinetics of artesunate and amodiaquine in African children.
Gansané, A; Kiechel, JR; Morgan, CC; Ouedraogo, A; Ouedraogo, EB; Simpson, JA; Sirima, SB; Stepniewska, K; Taylor, W; White, NJ, 2009
)
0.35
" A pharmacokinetic study was also conducted to evaluate the bioavailability of AS following the IM administrations."( Severe embryolethality of artesunate related to pharmacokinetics following intravenous and intramuscular doses in pregnant rats.
Li, Q; Si, Y; Weina, P; Xie, L; Zhang, J, 2009
)
0.35
"The aim of the present study was to compare the pharmacokinetic properties, bioavailability and tolerability of artesunate (AS) and amodiaquine (AQ) administered as a fixed-dose combination (Amonate FDC tablets; Dafra Pharma, Turnhout, Belgium) or as a non-fixed dose combination of separate AS tablets (Arsuamoon; Guilin Pharmaceutical Co, Shanghai, China) and AQ tablets (Flavoquine; Sanofi-Aventis, Paris, France)."( Comparative oral bioavailability of non-fixed and fixed combinations of artesunate and amodiaquine in healthy Indian male volunteers.
Fortin, A; Jansen, FH; Verbeeck, RK, 2011
)
0.37
" The proposed method provides a new route to prepare monodisperse nanocapsules to increase bioavailability of hydrophobic solutes."( Firstborn microcrystallization method to prepare nanocapsules containing artesunate.
Hong, ZG; Xiao, XC, 2010
)
0.36
"The efficacy of anti-malarial drugs is determined by the level of parasite susceptibility, anti-malarial drug bioavailability and pharmacokinetics, and host factors including immunity."( Modulating effects of plasma containing anti-malarial antibodies on in vitro anti-malarial drug susceptibility in Plasmodium falciparum.
Chotivanich, K; Dondorp, AM; Krudsood, S; Monatrakul, P; Mungthin, M; Udomsangpetch, R; White, NJ; Wilairatana, P, 2010
)
0.36
" Similarly high bioavailability of DHA (> 80%) is associated with oral administration."( Review of the clinical pharmacokinetics of artesunate and its active metabolite dihydroartemisinin following intravenous, intramuscular, oral or rectal administration.
Borghini-Fuhrer, I; Duparc, S; Fleckenstein, L; Jung, D; Morris, CA; Shin, CS, 2011
)
0.37
" The corresponding median absolute oral bioavailability (F%) was 21."( Artesunate/dihydroartemisinin pharmacokinetics in acute falciparum malaria in pregnancy: absorption, bioavailability, disposition and disease effects.
Hanpithakpon, W; Hlaing, N; Lindegardh, N; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Singhasivanon, P; Tarning, J; Than, HH; White, NJ; Zin, NT, 2012
)
0.38
"Artesunate (AST), the most widely used artemisnin derivative, has poor aqueous solubility and suffers from low oral bioavailability (~40%)."( Artesunate-loaded chitosan/lecithin nanoparticles: preparation, characterization, and in vivo studies.
Chadha, R; Gupta, S; Pathak, N, 2012
)
0.38
" The model incorporated population parameter variability for clearance (CL/F), central volume of distribution (VC/F) and absorption rate constant (KA) and identified, in addition to body weight, malaria infection as a covariate for VC/F (but not CL/F)."( Population pharmacokinetics of orally administered mefloquine in healthy volunteers and patients with uncomplicated Plasmodium falciparum malaria.
Evans, AM; Navaratnam, V; Olliaro, PL; Reuter, SE; Upton, RN, 2015
)
0.42
" Malaria increased the absolute oral bioavailability of artesunate by 87%, presumably by inhibiting first pass effect, whereas pregnancy decreased oral bioavailability by 23%."( Opposite malaria and pregnancy effect on oral bioavailability of artesunate - a population pharmacokinetic evaluation.
Day, NP; Hanpithakpon, W; Hlaing, N; Kloprogge, F; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Tarning, J; Than, HH; White, NJ; Zin, NT, 2015
)
0.42
"The population pharmacokinetic analysis demonstrated opposite effects of malaria and pregnancy on the bioavailability of orally administered artesunate."( Opposite malaria and pregnancy effect on oral bioavailability of artesunate - a population pharmacokinetic evaluation.
Day, NP; Hanpithakpon, W; Hlaing, N; Kloprogge, F; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Tarning, J; Than, HH; White, NJ; Zin, NT, 2015
)
0.42
" The broad antiinfective drug artesunate (ART) offers additional therapeutic options such as oral bioavailability and low levels of toxic side-effects."( The broad-spectrum antiinfective drug artesunate interferes with the canonical nuclear factor kappa B (NF-κB) pathway by targeting RelA/p65.
Bahsi, H; Efferth, T; Einsiedel, J; Fröhlich, T; Gmeiner, P; Godl, K; Hutterer, C; Kadioglu, O; Marschall, M; Milbradt, J; Niemann, I; Reiter, C; Stamminger, T; Tsogoeva, SB; Vogel, N; Wagner, S; Wandinger, S; Zeitträger, I, 2015
)
0.42
" The final parameter estimates of PYR apparent clearance (CL/F), central volume of distribution (V2/F), peripheral volume of distribution (V3/F), intercompartmental clearance (Q/F), and absorption rate constant (Ka) were 377 liters/day, 2,230 liters, 3,230 liters, 804 liters/day and 17."( Population Pharmacokinetics of Pyronaridine in Pediatric Malaria Patients.
Ayyoub, A; Borghini-Fuhrer, I; Djimde, AA; Duparc, S; Fleckenstein, L; Methaneethorn, J; Ramharter, M; Shin, JS; Tekete, M, 2015
)
0.42
" Herein, we report that among the artimisinins, artesunate (ARTS), an orally bioavailable compound has the most potent antileukemic activity in AML models and primary patients' blasts."( Antileukemic activity and cellular effects of the antimalarial agent artesunate in acute myeloid leukemia.
Chen, CC; Chu, S; Forman, SJ; Kalvala, A; Kumar, B; Marcucci, G; Pullarkat, V; Rosen, S, 2017
)
0.46
" However, their clinical applications face challenges because of short half-life, poor bioavailability and growing drug resistance."( Liposomes of dimeric artesunate phospholipid: A combination of dimerization and self-assembly to combat malaria.
Du, Y; Ismail, M; Li, X; Ling, L; Yao, C, 2018
)
0.48
"Artesunate is one of artemisinin derivatives with anti-malarial and anti-inflammatory activities though its water solubility and bioavailability are low."( [Preparation of liposomal artesunate dry powder inhalers and the effect on the acute lung injury of rats].
Hu, YZ; Jin, YG; Li, M; Zhang, TT, 2016
)
0.43
" Artesunate (ART), one of the classical antimalarial drugs, has recently been shown to exert significant cytotoxicity in various cancers, but its bioavailability is low."( Mitochondria-targeted artesunate conjugated cyclometalated iridium(iii) complexes as potent anti-HepG2 hepatocellular carcinoma agents.
Chen, BC; Chen, XQ; Jiang, N; Li, RT; Mao, ZW; Peng, W; Ye, RR, 2020
)
0.56
"Artesunate (ART) has potent anticancer activity but it suffers from poor stability and low bioavailability in vivo due to the special endoperoxide moiety in the molecules."( Artesunate carriers induced ferroptosis to overcome biological barriers for anti-cancer.
Chen, XL; Huang, QF; Huang, ZJ; Jun, M; Li, YH; Wang, GH; Wang, W, 2023
)
0.91

Dosage Studied

ExcerptRelevanceReference
" 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
)
0.28
"5 micrograms/ml of DHA was reached at about 3 minutes after dosing and the AUC was 82 mg/L."( [Pharmacokinetics and metabolism of artesunate in cows].
Huo, JZ; Xia, WJ; Xue, M; Zhou, ZT, 1991
)
0.28
" If some azone was added in the artesunate transdermal preparation at the dosage of 5 mg/kg, bid, for 3 days, the parasitemia of Plasmodium cynomolgi could be cleared and recrudescence prevented, thus, the antimalarial effects was enhanced."( [Effect of artesunate transdermal preparation on Plasmodium cynomolgi].
Li, AY; Liu, X; Xie, PS; Xuan, WY; Zhao, Y, 1990
)
0.28
" A transdermal dosage form of artesunic acid had been prepared and was reported to have reliable suppressing and killing effects on plasmobium berghei in mice."( [The pharmacokinetics of a transdermal preparation of artesunate in mice and rabbits].
Song, ZY; Xuan, WY; Zhao, KC; Zhao, Y, 1989
)
0.57
" The rapidity of effect, availability of an intravenous and intramuscular formulation and convenient dosage regimen make artesunate an ideal candidate for the treatment of severe malaria, including cerebral disease."( Artesunate. A review of its pharmacology and therapeutic efficacy in the treatment of malaria.
Barradell, LB; Fitton, A, 1995
)
0.29
" A significant therapeutic problem is a high, late recrudescence rate, probably due to short half-lives of both artesunate and its active metabolite dihydroartemisinin relative to conventional dosing intervals."( Chemical stability of artesunate injection and proposal for its administration by intravenous infusion.
Batty, KT; Davis, ME; Davis, T; Ilett, KF, 1996
)
0.29
" The rapidity of effect, availability and convenient dosage regimen make artesunate in suppository form a promising treatment for severe falciparum malaria, particularly in rural areas where parenteral formulations are unavailable."( Artesunate suppositories: an effective treatment for severe falciparum malaria in rural areas.
Chongsuphajaisiddhi, T; Looareesuwan, S; Viriyavejakul, P; Wilairatana, P, 1997
)
0.3
" Reasons for compliance included the desire to be cured and to follow the advice of malaria staff/employer, and the simple dosing regimen."( Compliance with artesunate and quinine + tetracycline treatment of uncomplicated falciparum malaria in Thailand.
Fungladda, W; Honrado, ER; Kamolratanakul, P; Karbwang, J; Kitayaporn, D; Masngammueng, R; Thimasarn, K, 1998
)
0.3
" Due to its fast efficacy, its absence of undesirable effects, its presentation in tablets, its quite simple dosage (one box for a treatment), Arsumax positioned itself as an accurate second line antimalaric treatment."( Positioning, labelling and control of medical information: artesunate strategy and Arsumax development story.
Ducret, JP; Moneton, P, 1998
)
0.3
"Single doses (250, 500, 1,000, or 2,000 units/kg) of an ovine polyclonal-specific Fab fragment directed against tumor necrosis factor-alpha (TNF-alpha) were given to 17 adult patients with severe falciparum malaria immediately before treatment with artesunate in a pilot study to assess safety and optimal dosage with a view to future studies."( Polyclonal anti-tumor necrosis factor-alpha Fab used as an ancillary treatment for severe malaria.
Hills, F; Krudsood, S; Looareesuwan, S; Porter, RS; Sjostrom, L; Warrell, DA; Wilairatana, P, 1999
)
0.3
" While most patients with tertian malaria were cured with the standard chloroquine and primaquine regimen, a higher dosage was required for one case acquired in Papua New Guinea."( Imported malaria: successful treatment of 31 patients in the era of chloroquine resistance.
Chang, HL; Chang, SC; Chen, YC; Fang, CT; Hsieh, WC; Hsueh, PR; Hung, CC, 1999
)
0.3
" At this stage, the parasite cycle is halted, making them unsusceptible to further dosing until wakening."( Mathematical modelling of the chemotherapy of Plasmodium falciparum malaria with artesunate: postulation of 'dormancy', a partial cytostatic effect of the drug, and its implication for treatment regimens.
Ginsburg, H; Hoshen, MB; Na-Bangchang, K; Stein, WD, 2000
)
0.31
" In order to characterize the in vivo dose-response relationship for artesunate and thus rationalize dosing, 47 adult patients with acute uncomplicated falciparum malaria and parasitemia > or = 1% were randomized to receive a single oral dose of artesunate varying between 0 and 250 mg together with a curative dose of oral mefloquine."( Oral artesunate dose-response relationship in acute falciparum malaria.
Angus, BJ; Chanthapadith, K; Suputtamongkol, Y; Thaiaporn, I; White, NJ, 2002
)
0.31
" Thus, the use of conventional oral dosage regimens of ARTS appears preferable to oral administration of DHA."( Relative bioavailability of artesunate and dihydroartemisinin: investigations in the isolated perfused rat liver and in healthy Caucasian volunteers.
Batty, KT; Davis, TM; Iletr, KE; Martin, J; Powell, SM, 2002
)
0.31
" Group II received the same dosage of placebo at the corresponding times."( [Field application of oral artesunate for preventing Schistosoma japonicum infection].
Chen, J; Fang, G; Li, J; Li, S; Ou, N; Wang, Q; Wang, T; Xu, M; Zhang, S; Zhang, X, 1999
)
0.3
" Patients were randomized to receive simultaneous dosing (artesunate 200 mg/d plus mefloquine 250 mg/d from the first to the third day [investigational group]) or sequential dosing (artesunate 200 mg/d for 3 d plus mefloquine 250 mg on the second and 500 mg on the third day [reference group])."( A randomized, double-blind study on the efficacy and safety of a practical three-day regimen with artesunate and mefloquine for the treatment of uncomplicated Plasmodium falciparum malaria in Africa.
Cambon, N; Kinde-Gazard, D; Kone, M; Massougbodji, A; Mueller, EA; Same-Ekobo, A,
)
0.13
" The dosage schedule led to a rapid clinical response and reduced parasite clearance and fever subsidence times of (31."( Descriptive study on the efficacy and safety of artesunate suppository in combination with other antimalarials in the treatment of severe malaria in Sudan.
Alkadru, AM; Awad, MI; Baraka, OZ; Behrens, RH; Eltayeb, IB, 2003
)
0.32
" When the cultures were exposed to serial dilutions of anti-malarial drugs, a distinct inhibition of HRP2 production was seen with increasing concentrations of drugs, resulting in sigmoid dose-response curves, similar to those obtained from conventional drug sensitivity assays."( Plasmodium falciparum: effect of anti-malarial drugs on the production and secretion characteristics of histidine-rich protein II.
Kollaritsch, H; Looareesuwan, S; Miller, RS; Myint, KS; Noedl, H; Sukthana, Y; Wernsdorfer, WH; Wiedermann, G; Wongchotigul, V; Wongsrichanalai, C,
)
0.13
" Three NAC dosage regimens were used: an intravenous loading dose of 140 mg/kg followed by 70 mg/kg every four hours intravenously for up to 18 doses (Group 1); a single intravenous loading dose followed by oral NAC in the same amount as for Group 1 (Group 2); a regimen identical to Group 1 except that oral NAC was administered after the first 24 hours (Group 3)."( N-acetylcysteine in severe falciparum malaria in Thailand.
Brittenham, G; Carroll, J; Krudsood, S; Kuhn, WF; Looareesuwan, S; Maek-A-Nantawat, W; Saengnetswang, T; Tosukhowong, T; Treeprasertsuk, S; Vannaphan, S, 2003
)
0.32
" In the naphtoquine group, thirty patients were prescribed single daily dosage of 1,000 mg for one day."( [A randomized comparative study of naphtoquine, mefloquine and artsunate in the treatment of falciparum malaria].
Chen, RJ; Fu, LC; Guo, WZ; Guo, XB; Ou, FZ; Tan, B; Zheng, QJ, 2003
)
0.32
"Although the average fever-subsidence time and the parasite-clearance time of naphtoquine at single 24-hour dosage of 1,000 mg were longer than those of mefloquine and artesunate, the 28-day curative ratio of naphtoquine was higher than that of mefloquine and artesunate."( [A randomized comparative study of naphtoquine, mefloquine and artsunate in the treatment of falciparum malaria].
Chen, RJ; Fu, LC; Guo, WZ; Guo, XB; Ou, FZ; Tan, B; Zheng, QJ, 2003
)
0.32
" Dose-response curves for a Plasmodium falciparum clone (clone W2) and DHA were used as a standard for each assay."( Plasmodium falciparum-based bioassay for measurement of artemisinin derivatives in plasma or serum.
Brewer, TG; Kyle, DE; Peggins, JO; Teja-Isavadharm, P; Webster, HK; White, NJ, 2004
)
0.32
" Forty patients demonstrated RI type of response, 37 were cured after being retreated with the same dosage and another 3 patients were cured after the third course of treatment."( Six-years monitoring the efficacy of the combination of artesunate and mefloquine for the treatment of uncomplicated falciparum malaria.
Bunnag, D; Chittamas, S; Kanda, T; Looareesuwan, S; Pornkulprasit, V; Rojanawatsirivej, C; Thimasarn, K; Wattanakoon, Y, 2003
)
0.32
"The aims of this study were to determine the pharmacokinetic parameters of a single dose of 200 mg oral and rectal artesunate in healthy volunteers, and to suggest a rational dosage regimen for rectal administration."( Pharmacokinetics of artesunate following oral and rectal administration in healthy Sudanese volunteers.
Alkadru, AM; Awad, MI; Baraka, OZ; Behrens, RH; Eltayeb, IB, 2004
)
0.32
"The optimal dosage of artesunate to prevent murine schistosomiasis was 300 mg/kg."( [Prophylactic effect of artesunate against experimental infection of Schistosoma mansoni].
Kumagai, T; Li, SW; Liu, X; Lou, LJ; Lu, SH; Ohta, N; Shi, JF; Wen, LY; Wu, LJ; Yan, XH; Yan, XL; Yang, MJ, 2004
)
0.32
"The current dosage of DP (6."( Randomized, controlled dose-optimization studies of dihydroartemisinin-piperaquine for the treatment of uncomplicated multidrug-resistant falciparum malaria in Thailand.
Ashley, EA; Brockman, A; Hutagalung, R; Krudsood, S; Leowattana, W; Looareesuwan, S; McGready, R; Nosten, F; Phaiphun, L; Srivilairit, S; White, NJ; Wilairatana, P, 2004
)
0.32
" Using the '4-day test', a low level of synergism or a simple additional action between CPG and DDS was observed with multiple dosing of these two compounds in a combination."( The chemotherapy of rodent malaria. LXIII. Drug combinations to impede the selection of drug resistance, part 6: the potential value of chlorproguanil and dapsone in combination, and with the addition of artesunate.
Peters, W; Robinson, BL; Stewart, LB, 2005
)
0.33
" All dosing regimens were well tolerated."( Short-course regimens of artesunate-fosmidomycin in treatment of uncomplicated Plasmodium falciparum malaria.
Adegnika, AA; Borrmann, S; Esser, G; Hutchinson, D; Issifou, S; Jomaa, H; Kombila, M; Kremsner, PG; Lundgren, I; Matsiegui, PB; Moussavou, F; Oyakhirome, S; Ramharter, M; Wiesner, J, 2005
)
0.33
" The doses and dosing regimens of artesunate and mefloquine varied across trials."( Artesunate plus mefloquine versus mefloquine for treating uncomplicated malaria.
Bukirwa, H; Orton, L, 2005
)
0.33
" mansoni experimentally infected mice were treated at 9th week of infection with ART, PZQ or OX at an oral dosage of 300 mg kg(-1), 600 mg kg(-1) and 100 mg kg(-1), respectively."( Comparative studies on the pathological findings and mortality in Schistosoma mansoni infected mice after treatment with artesunate and the current antischistosomal drugs.
Chaiworaporn, R; Janecharut, T; Kitikoon, V; Maneerat, Y; Matsuda, H; Ramasoota, P; Rojekittikhun, W, 2005
)
0.33
" Comparative studies to assess the therapeutic indices of PQD-A4, PQD-BE, and PQD were conducted in Plasmodium berghei-infected rats following daily intragastric dosing for three consecutive days."( New potential antimalarial agents: therapeutic-index evaluation of pyrroloquinazolinediamine and its prodrugs in a rat model of severe malaria.
Li, Q; Lin, AJ; Skillman, DS; Smith, K; Xie, LH; Zhang, J, 2006
)
0.33
" The fever clearance and the parasitemia reduction rates were found to be effective according to this dosing regimen."( Pharmacokinetics/Pharmacodynamics findings after repeated administration of ARTESUNATE thermostable suppositories (RECTOCAPS) in Vietnamese patients with uncomplicated malaria.
Benakis, A; Binh, TQ; Keundjian, A; Scheiwe, MW,
)
0.13
" This study was designed to construct a population pharmacokinetic model describing this new dosage regimen of mefloquine given as loose tablets together with artesunate."( Population pharmacokinetic assessment of a new regimen of mefloquine used in combination treatment of uncomplicated falciparum malaria.
Ashley, EA; Hae, R; Hutagalung, R; Lindegårdh, N; McGready, R; Nosten, F; Singhasivanon, P; Stepniewska, K; White, NJ, 2006
)
0.33
" 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
" To inform dosage recommendations we assessed the pharmacokinetics of intravenous artesunate after the first dose."( The pharmacokinetics of intravenous artesunate in adults with severe falciparum malaria.
Barnes, KI; Chierakul, W; Evans, AC; Newton, PN; Ruangveerayuth, R; Smith, PJ; White, NJ, 2006
)
0.33
" There are no clear data on whether a higher dosage of rectal artesunate results in a better clinical response."( Comparative study of the effectiveness and pharmacokinetics of two rectal artesunate/oral mefloquine combination regimens for the treatment of uncomplicated childhood falciparum malaria.
Chaivisuth, A; Chanthavanich, P; Na-Bangchang, K; Pengsaa, K; Pojjaroen-Anant, C; Sabchareon, A; Sirivichayakul, C; Thaiarporn, I; Wisetsing, P, 2007
)
0.34
" There was no definite benefit from increasing the dosage of rectal artesunate from 10 to 20 mg/kg/day."( Comparative study of the effectiveness and pharmacokinetics of two rectal artesunate/oral mefloquine combination regimens for the treatment of uncomplicated childhood falciparum malaria.
Chaivisuth, A; Chanthavanich, P; Na-Bangchang, K; Pengsaa, K; Pojjaroen-Anant, C; Sabchareon, A; Sirivichayakul, C; Thaiarporn, I; Wisetsing, P, 2007
)
0.34
" A weight-based dosing regimen was used for the loose tablets during 2000-2003 (n = 731) and a commercially available co-blister was used during 2004-2005 (n = 235)."( Efficacy and safety of artesunate plus amodiaquine in routine use for the treatment of uncomplicated malaria in Casamance, southern Sénégal.
Agnamey, P; Brasseur, P; Gaye, O; Olliaro, PL; Taylor, WR; Vaillant, M, 2007
)
0.34
" Patients were randomly allocated into one of the two regimens, with dosage according to bodyweight range."( Randomized, comparative study of the efficacy and safety of artesunate plus amodiaquine, administered as a single daily intake versus two daily intakes in the treatment of uncomplicated falciparum malaria.
Brasseur, P; Cisse, M; Diouf, AM; Faye, B; Gaye, O; Kuété, T; Lameyre, V; Ndiaye, JL; Same-Ekobo, A; Seck, PA, 2008
)
0.35
" Single oral doses produced embryolethality and similar cardiovascular and skeletal malformations as previously reported in longer term dosing experiments."( Sensitive periods for developmental toxicity of orally administered artesunate in the rat.
Clark, RL; White, TE, 2008
)
0.35
"Groups of up to 15 pregnant females were dosed on Gestation Days (GD) 20-50 or for 3-7-day intervals."( Artesunate: developmental toxicity and toxicokinetics in monkeys.
Arima, A; Bernard, F; Clark, RL; Gristwood, W; Harrell, A; Makori, N; Nakata, Y; White, TE; Wier, PJ, 2008
)
0.35
"Artesunate was embryolethal at > or =12 mg/kg/day when dosed for at least 12 days at the beginning of organogenesis, but not when dosed for 3 or 7 days, indicating that developmental toxicity of artesunate is dependent upon duration of dosing in cynomologus monkeys."( Artesunate: developmental toxicity and toxicokinetics in monkeys.
Arima, A; Bernard, F; Clark, RL; Gristwood, W; Harrell, A; Makori, N; Nakata, Y; White, TE; Wier, PJ, 2008
)
0.35
" The nonlinear clearance of DEAQ and the wide variability in kinetic parameters have safety implications for weight-based dosing of higher-body-weight children with AQ."( Effect of concomitant artesunate administration and cytochrome P4502C8 polymorphisms on the pharmacokinetics of amodiaquine in Ghanaian children with uncomplicated malaria.
Adjei, GO; Alifrangis, M; Goka, BQ; Hoegberg, LC; Kristensen, K; Kurtzhals, JA; Rodrigues, OP, 2008
)
0.35
"Several products of artesunate plus amodiaquine (AS + AQ) are being deployed in malaria-endemic countries for treating uncomplicated falciparum malaria but dosing accuracy and consequential effects on efficacy and tolerability have not been examined."( Dosing accuracy of artesunate and amodiaquine as treatment for falciparum malaria in Casamance, Senegal.
Agnamey, P; Badiane, M; Brasseur, P; Cisse, M; Gaye, O; Olliaro, P; Taylor, WR; Vaillant, M, 2009
)
0.35
" AS + AQ was given as: (i) loose combination (AS 50 mg, AQ 200 mg), dosed on body weight, or (ii) co-blistered product (AS 50 mg, AQ 153 mg) dosed by weight or age."( Dosing accuracy of artesunate and amodiaquine as treatment for falciparum malaria in Casamance, Senegal.
Agnamey, P; Badiane, M; Brasseur, P; Cisse, M; Gaye, O; Olliaro, P; Taylor, WR; Vaillant, M, 2009
)
0.35
" AS was dosed correctly in >99% with all regimens."( Dosing accuracy of artesunate and amodiaquine as treatment for falciparum malaria in Casamance, Senegal.
Agnamey, P; Badiane, M; Brasseur, P; Cisse, M; Gaye, O; Olliaro, P; Taylor, WR; Vaillant, M, 2009
)
0.35
"Oral administration of artesunate with a total dosage of 1000 mg in 6 days inhibits the infectivity of PFG."( [Artesunate in interrupting the transmission of Plasmodium falciparum].
Chen, D; Chen, PQ; Fu, CW; Fu, LC; He, KR; Li, GQ; Ou, FZ; Xu, Y, 2008
)
0.35
" 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
)
0.35
" C(max) and AUC of artesunate and DHA following iv dosing were 5784 +/- 3718 and 140 938 +/- 128 783 ng."( Pharmacokinetic parameters of artesunate and dihydroartemisinin in rats infected with Fasciola hepatica.
Decosterd, L; Gruyer, MS; Keiser, J; Mercier, T; Perrottet, N; Zanolari, B, 2009
)
0.35
" For CCG and MADDS, small to moderate increases in exposure with artesunate dosing were observed."( Pharmacokinetics of chlorproguanil, dapsone, artesunate and their major metabolites in patients during treatment of acute uncomplicated Plasmodium falciparum malaria.
Bandyopadhyay, N; Duparc, S; Kirby, PL; Miller, AK; Ward, SA; Winstanley, PA; Wootton, DG, 2009
)
0.35
" 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
)
0.35
"A single-center, randomized, single-blind, cross-over clinical study was conducted in 18 healthy volunteers with a dosage of 300 mg daily for 2 days."( Comparative study of dihydroartemisinin and artesunate safety in healthy Thai volunteers.
Atipas, S; Chatsiricharoenkul, S; Kaewkungwal, J; Khuhapinant, A; Kongpatanakul, S, 2009
)
0.35
" 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
)
0.36
" In the present study, pregnant rats were selected and dosed with AS (GMP product) intravenously (IV) and intramuscularly (IM) at varied doses daily for 13 days from gestation day (GD) 6 to 18."( Severe embryolethality of artesunate related to pharmacokinetics following intravenous and intramuscular doses in pregnant rats.
Li, Q; Si, Y; Weina, P; Xie, L; Zhang, J, 2009
)
0.35
"A novel parent-metabolite pharmacokinetic model consisting of a dosing compartment, a central compartment for AS, a central compartment and a peripheral compartment for DHA was developed."( Population pharmacokinetics of artesunate and dihydroartemisinin following single- and multiple-dosing of oral artesunate in healthy subjects.
Craft, JC; Fleckenstein, L; Jang, IJ; Kirsch, LE; Naik, H; Shin, CS; Tan, B; Yu, KS, 2009
)
0.35
" 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
)
0.36
" The patients (n = 25/arm) were treated with (i) two fixed-dose tablets (AS-MQ arm; 100 mg AS-200 mg MQ/tablet) daily for 3 days (days 0, 1, and 2) or (ii) nonfixed AS (AS-plus-MQ arm; 4 mg/kg of body weight/day for 3 days) plus MQ (15 mg/kg on day 1 and 10 mg/kg on day 2), dosed by weight."( New fixed-dose artesunate-mefloquine formulation against multidrug-resistant Plasmodium falciparum in adults: a comparative phase IIb safety and pharmacokinetic study with standard-dose nonfixed artesunate plus mefloquine.
Chalermrut, K; Kiechel, JR; Krudsood, S; Leowattana, W; Looareesuwan, S; Navaratnam, V; Olliaro, P; Phumratanaprapin, W; Ramanathan, S; Tangpukdee, N; Taylor, WR; Vaillant, M; Wilairatana, P, 2010
)
0.36
"5% in the Administration I group, whose dosage schedule was identical to schedules used in previous studies."( The sensitivity of artesunate against Schistosoma japonicum decreased after 10 years of use in China.
Guo, HX; Hua, HY; Liang, YS; Wei, JF; Zhang, Y, 2010
)
0.36
"Rats were dosed orally with chlorproguanil/dapsone/artesunate (including 11."( Localization of artesunate and its derivatives in the pregnant rat and fetus following oral administration and relationship to developmental toxicity.
Clark, RL; Gristwood, WE; Harrell, AW; Lewsley, R; Wilson, R, 2010
)
0.36
" Negative binomial regressions of worm and egg counts were used to analyze dose-response relationships and whether the effects of drug combinations were synergistic or antagonistic."( In vivo and in vitro sensitivity of Fasciola hepatica to triclabendazole combined with artesunate, artemether, or OZ78.
Duthaler, U; Keiser, J; Smith, TA, 2010
)
0.36
" Recipients of the 6 mg/kg/day dosage had significantly lower geometric mean absolute neutrophil counts than did recipients of the 2 and 4 mg/kg/day dosages at 6 and 14 days (P < ."( Dose-dependent risk of neutropenia after 7-day courses of artesunate monotherapy in Cambodian patients with acute Plasmodium falciparum malaria.
Bethell, D; Darapiseth, S; Fukuda, MM; Khemawoot, P; Kuntawungin, W; Lee, SJ; Lin, J; Lon, C; Sarim, S; Saunders, D; Se, Y; Smith, B; Socheat, D; Sriwichai, S; Surasri, S; Teja-Isavadharm, P; Tyner, S, 2010
)
0.36
"Artesunate remains a crucial drug for the treatment of malaria, and determining optimal dosing regimens is vital to overcome emerging resistant parasite strains along the Thai-Cambodian border."( Dose-dependent risk of neutropenia after 7-day courses of artesunate monotherapy in Cambodian patients with acute Plasmodium falciparum malaria.
Bethell, D; Darapiseth, S; Fukuda, MM; Khemawoot, P; Kuntawungin, W; Lee, SJ; Lin, J; Lon, C; Sarim, S; Saunders, D; Se, Y; Smith, B; Socheat, D; Sriwichai, S; Surasri, S; Teja-Isavadharm, P; Tyner, S, 2010
)
0.36
" This result supports the hypothesis that artemisinin resistance mainly reflects reduced ring-stage susceptibility and predicts that doubling the frequency of dosing will accelerate clearance of artemisinin-resistant parasites."( Intrahost modeling of artemisinin resistance in Plasmodium falciparum.
Chotivanich, K; Day, NP; Dondorp, AM; Lee, SJ; Lindegårdh, N; Maude, RJ; Nosten, F; Pan-Ngum, W; Saralamba, S; Socheat, D; Tarning, J; White, LJ; White, NJ, 2011
)
0.37
" The high correlation between embryotoxicity and reticulocytopenia further supports the assertion that therapeutic dosage regimens of artemisinins that cause decreases in reticulocyte count in pregnant women during the putative critical period (approximately postconception wk 3 to 9) are at risk of also causing adverse effects on the embryo."( Artesunate and artelinic acid: association of embryotoxicity, reticulocytopenia, and delayed stimulation of hematopoiesis in pregnant rats.
Brannen, KC; Clark, RL; Hoberman, AM; Sanders, JE, 2011
)
0.37
"The study objectives to investigate the distribution of the antimalarial drug mefloquine (MQ) in cellular and fluid blood compartments when given at therapeutic dosage with artesunate and to investigate an eventual association with the occurrence of treatment-related adverse events in Thai patients with acute uncomplicated falciparum malaria."( Distribution of mefloquine in the blood of Thai patients with acute uncomplicated falciparum malaria following administration of therapeutic doses of artesunate.
Na-Bangchang, K; Ruengweerayut, R; Wernsdorfer, WH, 2011
)
0.37
" No electroactive interferences from the excipients and endogenous substance could be observed in the pharmaceutical dosage forms and in biological samples."( Voltammetric behaviour of antimalarial drug artesunate in solubilized systems.
Jain, R, 2011
)
0.37
" Simultaneously, the feared development of parasite drug resistance might drive dosing increases."( The pharmacogenetics of antimalaria artemisinin combination therapy.
Gil, JP; Piedade, R, 2011
)
0.37
" The data are reassuring regarding current dosing recommendations."( Artesunate/dihydroartemisinin pharmacokinetics in acute falciparum malaria in pregnancy: absorption, bioavailability, disposition and disease effects.
Hanpithakpon, W; Hlaing, N; Lindegardh, N; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Singhasivanon, P; Tarning, J; Than, HH; White, NJ; Zin, NT, 2012
)
0.38
" From the day of arthritis onset, rats were treated daily by gavage with leflunomide (Lef) or ART at a dosage of 10 mg/kg/d or 5 mg/kg/d, respectively, for 16 days."( Inhibitory effect of the antimalarial agent artesunate on collagen-induced arthritis in rats through nuclear factor kappa B and mitogen-activated protein kinase signaling pathway.
Chen, G; Huang, H; Li, C; Li, Y; Lin, S; Lin, W; Liu, P; Shen, W; Shen, X; Wang, S; Wang, Y; Zhou, C, 2013
)
0.39
" 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
)
0.38
" Other interventions such as measures to increase nitric oxide, manage acute renal failure or optimize artesunate dosing are discussed."( Adjunctive management of malaria.
Krishna, S, 2012
)
0.38
"Mechanistic within-host models relating blood anti-malarial drug concentrations with the parasite-time profile help in assessing dosing schedules and partner drugs for new anti-malarial treatments."( Assessing the utility of an anti-malarial pharmacokinetic-pharmacodynamic model for aiding drug clinical development.
Charman, SA; Gamo-Benito, J; Humberstone, A; Jamsen, KM; McCaw, J; Moehrle, J; Price, RN; Simpson, JA; Smith, K; Zaloumis, S, 2012
)
0.38
" Patients were randomized (2:1) to pyronaridine-artesunate granules (60/20 mg) once daily or artemether-lumefantrine crushed tablets (20/120 mg) twice daily, both dosed by bodyweight, orally (liquid suspension) for three days."( Pyronaridine-artesunate granules versus artemether-lumefantrine crushed tablets in children with Plasmodium falciparum malaria: a randomized controlled trial.
Bhatt, KM; Borghini-Fuhrer, I; Bustos, MD; de Salazar, PM; Doumbo, OK; Duparc, S; Fleckenstein, L; Kayentao, K; Kimani, J; Kokolomami, JH; Offianan, AT; Ouédraogo, A; Pénali, LK; Quicho, F; Ramharter, M; Shin, CS; Tiono, AB; Tshefu, AK, 2012
)
0.38
" An adapted dosing regimen including a practical dosing table per weight band is proposed for young children based on the pharmacokinetic model."( Population pharmacokinetics of intramuscular artesunate in African children with severe malaria: implications for a practical dosing regimen.
Day, NP; Dondorp, AM; Gesase, S; Hendriksen, IC; Kent, A; Lemnge, MM; Lindegardh, N; Mtove, G; Reyburn, H; Tarning, J; von Seidlein, L; White, NJ, 2013
)
0.39
" The procedure was applied to the assay of the drug in dosage form, human serum, plasma and urine without matrix interference."( Graphene-polyaniline nanocomposite based biosensor for detection of antimalarial drug artesunate in pharmaceutical formulation and biological fluids.
Das, MR; Khan, R; Kotoky, P; Radhapyari, K, 2013
)
0.39
" Pre-clinical studies in dogs indicated morbidity at high dosage levels."( Safety and efficacy field study of artesunate for dogs with non-resectable tumours.
Efferth, T; Erich, SA; Fleckenstein, L; Grinwis, GC; London, CA; Mol, JA; Rutteman, GR; Spee, B, 2013
)
0.39
" Daily administered FDC ASMQ for three days was dosed by age."( Therapeutic efficacy of fixed dose artesunate-mefloquine for the treatment of acute, uncomplicated Plasmodium falciparum malaria in Kampong Speu, Cambodia.
Ariey, F; Duong, S; Kiechel, JR; Leang, R; Lim, P; Ménard, D; Navaratnam, V; Ros, S; Taylor, WR, 2013
)
0.39
" However, they have short half life, low solubility, and poor oral bioavailability, hence the need to formulate sustained release lipid particulate dosage form of these drugs."( Formulation development and evaluation of the anti-malaria properties of sustained release artesunate-loaded solid lipid microparticles based on phytolipids.
Attama, AA; Chime, SA; Chinaeke, EE; Okore, VC; Onyishi, VI, 2015
)
0.42
" Following dosing with PA, some subjects experienced rises in liver function tests above the upper limit of normal during the first few days following PA administration."( Pharmacokinetic interaction between pyronaridine-artesunate and metoprolol.
Arbe-Barnes, S; Borghini-Fuhrer, I; Duparc, S; Fleckenstein, L; Lopez-Lazaro, L; Miller, RM; Morris, CA; Pokorny, R; Shin, JS, 2014
)
0.4
"The determination of dosing regimens for the treatment of malaria is largely empirical and thus a better understanding of the pharmacokinetic/pharmacodynamic properties of antimalarial agents is required to assess the adequacy of current treatment regimens and identify sources of suboptimal dosing that could select for drug-resistant parasites."( Population pharmacokinetics of orally administered mefloquine in healthy volunteers and patients with uncomplicated Plasmodium falciparum malaria.
Evans, AM; Navaratnam, V; Olliaro, PL; Reuter, SE; Upton, RN, 2015
)
0.42
" Rats infected with the triclabendazole-resistant Oberon isolate were dosed orally with artesunate at a concentration of 200 mg/kg and flukes recovered 24, 48, 72 and 96 h post-treatment (pt)."( Ultrastructural changes in the tegument and gut of adult Fasciola hepatica following in vivo treatment with artesunate.
Brennan, GP; Fairweather, I; Halferty, L; Johnston, RC; O'Neill, JF, 2015
)
0.42
" 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
)
0.42
" In particular, the malaria community may be missing the opportunity to dramatically increase ACT effectiveness through regimen changes, particularly through a switch to twice-daily regimens and/or increases in artemisinin dosing levels."( How Robust Are Malaria Parasite Clearance Rates as Indicators of Drug Effectiveness and Resistance?
Hastings, IM; Hodel, EM; Kay, K, 2015
)
0.42
" The aims of this study were to describe the pharmacokinetics of PYR using a total of 1,085 blood PYR concentrations available from 349 malaria patients younger than 16 years of age with mild to moderate uncomplicated malaria and to confirm the dosing regimen for the pediatric granule formulation."( Population Pharmacokinetics of Pyronaridine in Pediatric Malaria Patients.
Ayyoub, A; Borghini-Fuhrer, I; Djimde, AA; Duparc, S; Fleckenstein, L; Methaneethorn, J; Ramharter, M; Shin, JS; Tekete, M, 2015
)
0.42
" Patients received pyronaridine-artesunate once daily for 3 days, dosed according to body weight."( Efficacy and Safety of Pyronaridine-Artesunate for Treatment of Uncomplicated Plasmodium falciparum Malaria in Western Cambodia.
Borghini Fuhrer, I; Canavati, SE; Denis, MB; Dondorp, AM; Duparc, S; Heng, P; Huy, R; Khim, N; Kim, S; Leang, R; Menard, D; Ringwald, P; Tol, B; Vestergaard, LS, 2016
)
0.43
" 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
)
0.46
" 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
)
0.43
" The proposed formulation design can significantly help in reduction of dose and dosing frequency, which ultimately enhance patient compliance with decreased drug toxicity."( Artesunate-quercetin/luteolin dual drug nanofacilitated synergistic treatment for malaria: A plausible approach to overcome artemisinin combination therapy resistance.
Kumar, RS; Puttappa, N; Yamjala, K, 2017
)
0.46
"As part of its development, the new synthetic trioxolane antimalarial artefenomel (OZ439) was tested in rat whole embryo culture and in rat embryo-fetal toxicity studies with dosing throughout organogenesis or with a single dose on Gestational Day (GD) 12."( Improved safety margin for embryotoxicity in rats for the new endoperoxide artefenomel (OZ439) as compared to artesunate.
Andenmatten, N; Clark, RL; Clode, SA; Edwards, TL; Huber, AC; Kinney, J; Longo, M; Rhodes, J; Rückle, T; Walker, DK; Wells, T, 2018
)
0.48
" Its tissue distribution in rats may change with different dosage forms, which therefore shall be studied after ARS-TPGS-Lipo was injected."( [Tissue distribution of TPGS modified artesunate liposome and its metabolites in rats].
An, R; Hu, C; Liang, K; Wang, XH; You, LS, 2018
)
0.48
" All treatments were once-daily or twice-daily tablets or granules given orally and dosed by bodyweight over 3 days at the study centre."( Pyronaridine-artesunate or dihydroartemisinin-piperaquine versus current first-line therapies for repeated treatment of uncomplicated malaria: a randomised, multicentre, open-label, longitudinal, controlled, phase 3b/4 trial.
, 2018
)
0.48
" falciparum malaria were randomly assigned in a 1:1 ratio to orally receive pyronaridine-artesunate or artemether-lumefantrine, dosed according to bodyweight, for 3 days."( Pyronaridine-artesunate and artemether-lumefantrine for the treatment of uncomplicated Plasmodium falciparum malaria in Kenyan children: a randomized controlled non-inferiority trial.
Choy, F; Makio, N; Mens, P; Okach, S; Omweri, G; Osoti, V; Roth, JM; Sawa, P; Schallig, HDFH, 2018
)
0.48
" The beneficial effects associated with artemisinin treatment include improving symptoms, reducing level of antibodies and proteinuria, ameliorating renal damage, and diminishing the dosage of prednisone use."( Artemisinins-a Promising New Treatment for Systemic Lupus Erythematosus: a Descriptive Review.
Mu, X; Wang, C, 2018
)
0.48
" falciparum to artemisinin, chloroquine and piperaquine by both a standard dose-response analysis and a piperaquine survival assay."( Overexpression of plasmepsin II and plasmepsin III does not directly cause reduction in Plasmodium falciparum sensitivity to artesunate, chloroquine and piperaquine.
Ansbro, MR; Chookajorn, T; Chotivanich, K; de Cozar, C; Gamo, FJ; Kochakarn, T; Kotanan, N; Kümpornsin, K; Lee, MCS; Loesbanluechai, D; Sanz, LM; White, NJ; Wilairat, P, 2019
)
0.51
" In this large clinical study, the pharmacokinetics (PK) of a fixed dose combination of ASMQ was investigated in an African paediatric population to support dosing recommendations used in Southeast Asia and South America."( Population pharmacokinetics and pharmacodynamics of the artesunate-mefloquine fixed dose combination for the treatment of uncomplicated falciparum malaria in African children.
Aouri, M; Carn, G; Csajka, C; Decosterd, LA; Guidi, M; Kiechel, JR; Mercier, T; Ogutu, B, 2019
)
0.51
" The largest contributor to this variability was body weight, which is accommodated for by the ASMQ fixed dose combination (FDC) dosing recommendation."( Population pharmacokinetics and pharmacodynamics of the artesunate-mefloquine fixed dose combination for the treatment of uncomplicated falciparum malaria in African children.
Aouri, M; Carn, G; Csajka, C; Decosterd, LA; Guidi, M; Kiechel, JR; Mercier, T; Ogutu, B, 2019
)
0.51
" The relationship between mg/kg dosage and treatment failures will be assessed using a Cox regression model with study sites considered as a shared frailty term."( The effect of dose on the antimalarial efficacy of artesunate-mefloquine against
Ashley, EA; Dahal, P; Guerin, P; Humphreys, GS; Mansoor, R; Stepniewska, K, 2019
)
0.51
" The positive synergy of Art on inhibiting HCC growth contributes 48% dosage of Sor to reduce tumor cell viability in vitro and tumor size in vivo."( Artesunate promotes sensitivity to sorafenib in hepatocellular carcinoma.
Dong, H; Jing, W; Jun, X; Min, M; Runpeng, Z; Shuo, L; Yingru, X, 2019
)
0.51
"Considering the low day 7 concentrations of piperaquine reported in the patients studied here, we suggest to adopt the recently recommended higher dose of DP in young children or a prolonged 5-day dosing in children living in malaria endemic areas who have suffered an initial episode of severe malaria in order to achieve adequate drug exposures for effective post-treatment prophylactic effects."( Piperaquine concentration and malaria treatment outcomes in Ugandan children treated for severe malaria with intravenous Artesunate or quinine plus Dihydroartemisinin-Piperaquine.
Blessborn, D; Byakika-Kibwika, P; Lamorde, M; Ssenyonga, R; Tarning, J, 2019
)
0.51
" Tolerability was assessed as the percentage of subjects able to complete their designated dosing regimen."( A first-in-human proof-of-concept trial of intravaginal artesunate to treat cervical intraepithelial neoplasia 2/3 (CIN2/3).
Clark, KT; Donovan, MJ; Frantz, PS; Fu, J; Levinson, K; Maldonado, L; Plesa, M; Sanders, SA; Sauter, ME; Shay, ME; Trimble, CL, 2020
)
0.56
"9%), a third knew all dosing intervals (33."( Predictors of health workers' knowledge about artesunate-based severe malaria treatment recommendations in government and faith-based hospitals in Kenya.
Achia, TNO; Amboko, B; Kipruto, H; Machini, B; Malla, L; Snow, RW; Zurovac, D, 2020
)
0.56
" It is expected that such a tool will be useful in characterizing the disposition of these chemicals and ultimately improve dosing regimens by enabling a quantitative assessment of the tissue-specific drug levels critical in the evaluation of efficacy and toxicity."( Predicting the Disposition of the Antimalarial Drug Artesunate and Its Active Metabolite Dihydroartemisinin Using Physiologically Based Pharmacokinetic Modeling.
Arey, R; Reisfeld, B, 2021
)
0.62
" An 80 mg/kg dosage was optimal."( Artesunate Provides Neuroprotection against Cerebral Ischemia-Reperfusion Injury via the TLR-4/NF-κB Pathway in Rats.
Chen, Y; Tian, J; Wang, Y; Wu, J; Yang, G; Zhao, Y; Zhu, J, 2021
)
0.62
" Additionally, these models are able to identify patient characteristics that cause alterations in the expected PK/PD profiles and through simulations can recommend changes to dosing which compensate for the differences."( Malaria PK/PD and the Role Pharmacometrics Can Play in the Global Health Arena: Malaria Treatment Regimens for Vulnerable Populations.
Hughes, E; Jagannathan, P; Mohamed Ali, A; Savic, RM; Wallender, E, 2021
)
0.62
" falciparum infection were randomly assigned (1:1:1) to receive a 3-day, 2-day, or 1-day treatment regimen of PA (180:60 mg), dosed according to bodyweight."( Efficacy, Safety and Tolerability of Pyronaridine-artesunate in Asymptomatic Malaria-infected Individuals: a Randomized Controlled Trial.
Achan, J; Arbe-Barnes, S; Borghini-Fuhrer, I; Conteh, B; D'Alessandro, U; Dabira, ED; Duparc, S; Hachizovu, S; Lawal, B; Manyando, C; Mendy, A; Miller, R; Mulenga, JM; Mwanza, S; Ndiath, MO; Nyang, H; Shin, J, 2022
)
0.72
" Patients received fixed-dose pyronaridine-artesunate once daily for 3 days, dosed by body weight, without regard to food intake."( Pyronaridine-artesunate real-world safety, tolerability, and effectiveness in malaria patients in 5 African countries: A single-arm, open-label, cohort event monitoring study.
Agnandji, ST; Allen, SJ; Arbe-Barnes, S; Assi, SB; Bigoga, JD; Borghini-Fuhrer, I; Duparc, S; Groger, M; Koukouikila-Koussounda, F; Kremsner, PG; Miller, R; Mombo-Ngoma, G; Ntamabyaliro, NY; Ntoumi, F; Ramharter, M; Shin, J; Tona Lutete, G, 2021
)
0.62
"A third of the health workers had high knowledge levels on artesunate treatment policy; almost three-quarters had high knowledge levels on artesunate dosing and preparation."( Cross-sectional study to predict subnational levels of health workers' knowledge about severe malaria treatment in Kenya.
Achia, TN; Amboko, B; Chesang, J; Kipruto, H; Machini, B; Mwaniki, P, 2022
)
0.72
" For the quantitative test, we established a standard curve that resulted from a dose-response curve and evaluated its performances using controls samples."( Assessment of quantitative and semi-quantitative biological test methods of artesunate in vitro.
Bienvenu, AL; Bonnot, G; Kouakou, YI; Lavoignat, A; Omorou, R; Picot, S; Said, IB, 2022
)
0.72
" Nous avons ainsi développé un test biologique quantitatif et un test semi-quantitatif pour le dosage de l’artésunate dans des échantillons liquides."( Assessment of quantitative and semi-quantitative biological test methods of artesunate in vitro.
Bienvenu, AL; Bonnot, G; Kouakou, YI; Lavoignat, A; Omorou, R; Picot, S; Said, IB, 2022
)
0.72
" Additionally, by lowering the effective dosage of TMZ, the combination liposomes reduced systemic TMZ-induced toxicity, highlighting the preclinical potential of this novel integrative strategy to deliver combination therapies to brain tumors."( Targeted liposomes for combined delivery of artesunate and temozolomide to resistant glioblastoma.
Chai, T; Du, Q; Hanif, S; Ismail, M; Li, Y; Muhammad, P; Shi, B; Yang, W; Zhang, D; Zheng, M, 2022
)
0.72
"4% at equivalent artesunate dosage in breast cancer orthotopic implanted mice."( Development of artesunate intelligent prodrug liposomes based on mitochondrial targeting strategy.
Chen, J; Du, M; Gu, L; Liu, D; Liu, S; Peng, Q; Shen, S; Tian, Y; Wang, J; Xiao, W; Zhang, J, 2022
)
0.72
" Then, after 12 hours, mice in the five other groups received intraperitoneal injection of the assigned drugs and dosage once a day."( [Therapeutic Effect of Artesunate on Influenza A Viral Pneumonia].
Bie, MJ; Li, Z; Wu, B; Wu, J; Zhang, J; Zhou, YJ, 2022
)
0.72
" RHF data of 7,983 children was analysed for appropriateness of antimalarials; a subsample of 3,449 children was assessed additionally for dosage and method of ACT provision (treatment compliance)."( Health worker compliance with severe malaria treatment guidelines in the context of implementing pre-referral rectal artesunate in the Democratic Republic of the Congo, Nigeria, and Uganda: An operational study.
Akano, BK; Angiro, I; Athieno, P; Awor, P; Ayodeji, K; Brunner, NC; Buj, V; Burri, C; Cereghetti, N; Delvento, G; Hetzel, MW; Kalenga, JC; Kimera, J; Lambiris, MJ; Lee, TT; Lengeler, C; Napier, HG; Okitawutshu, J; Okon, C; Okuma, J; Omoluabi, E; Signorell, A; Tshefu, A; Tumukunde, G; Visser, T; Yusuf, O, 2023
)
0.91
" A revisiting on mefloquine pharmacokinetics-pharmacodynamics (PK/PD) could assist in finding new appropriate dosage regimens in combination with artesunate as a three-day course treatment."( Prediction of improved antimalarial chemotherapy of artesunate-mefloquine in combination with mefloquine sensitive and resistant Plasmodium falciparum malaria.
Na-Bangchang, K; Saeheng, T, 2023
)
0.91
" A simple concentration-effect pharmacometric model does not explain why dosing more frequently than once daily fails to augment parasite clearance and improve therapeutic responses in vivo."( An artesunate pharmacometric model to explain therapeutic responses in falciparum malaria.
Choosri, N; Dondorp, AM; Pan-Ngum, W; Saralamba, S; Simpson, JA; White, L; White, NJ, 2023
)
0.91
"To propose a revised model of antimalarial pharmacodynamics that incorporates reversible asexual parasite injury and temporary drug refractoriness in order to explain the failure of frequent dosing to augment therapeutic efficacy in falciparum malaria."( An artesunate pharmacometric model to explain therapeutic responses in falciparum malaria.
Choosri, N; Dondorp, AM; Pan-Ngum, W; Saralamba, S; Simpson, JA; White, L; White, NJ, 2023
)
0.91
"AML cell lines resistant to AraC were first constructed by repeated dosing for 5 months."( Artesunate reverses cytarabine resistance in acute myeloid leukemia by blocking the JAK/STAT3 signaling.
Chen, Y; Huang, P; Li, H; Luo, X; Su, Q; Zhang, P, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,997)

TimeframeStudies, This Drug (%)All Drugs %
pre-199038 (1.90)18.7374
1990's124 (6.21)18.2507
2000's562 (28.14)29.6817
2010's903 (45.22)24.3611
2020's370 (18.53)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.78

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index16.78 (24.57)
Research Supply Index7.84 (2.92)
Research Growth Index5.32 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.78)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials443 (21.21%)5.53%
Reviews130 (6.22%)6.00%
Case Studies144 (6.89%)4.05%
Observational15 (0.72%)0.25%
Other1,357 (64.96%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]