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piperaquine

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Description

Piperaquine is a synthetic antimalarial drug that is used in combination therapy to treat uncomplicated malaria. Its mechanism of action involves inhibiting the formation of hemozoin, a detoxification product of heme, which is crucial for the survival of the malaria parasite Plasmodium falciparum. Piperaquine is effective against both chloroquine-sensitive and chloroquine-resistant strains of P. falciparum. It has a long half-life, allowing for once-weekly or even once-monthly dosing regimens, which enhances treatment adherence and reduces the risk of drug resistance development. Piperaquine is typically used in combination with artemisinin derivatives, such as artemether or artesunate, forming artemisinin-based combination therapies (ACTs) that are considered the gold standard for malaria treatment. Piperaquine is particularly important for the treatment of malaria in areas where resistance to other antimalarial drugs is prevalent. Ongoing research focuses on investigating the optimal dosage regimens, understanding the mechanisms of drug resistance, and exploring potential new drug combinations involving piperaquine for improved malaria control. '

piperaquine : An aminoquinoline that is 1,3-di(piperazin-1-yl)propane in which the nitrogen at position 4 of each of the piperazine moieties is replaced by a 7-chloroquinolin-4-yl group. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID122262
CHEMBL ID303933
CHEBI ID91231
SCHEMBL ID131649
MeSH IDM0106912

Synonyms (40)

Synonym
brn 0905079
quinoline, 4,4'-(trimethylenedi-4,1-piperazinediyl)bis(7-chloro-
piperaquine
piperaquinoline
quinoline, 4,4'-(1,3-propanediyldi-4,1-piperazinediyl)bis(7-chloro-
4,4'-(propane-1,3-diyldipiperazine-4,1-diyl)bis(7-chloroquinoline)
piperaquine phosphate
CHEMBL303933
FT-0650576
7-chloro-4-[4-[3-[4-(7-chloroquinolin-4-yl)piperazin-1-yl]propyl]piperazin-1-yl]quinoline
4085-31-8
7-chloro-4-[4-[3-[4-(7-chloro-4-quinolyl)piperazin-1-yl]propyl]piperazin-1-yl]quinoline;1,3-bis[4-(7-chloro-4-quinolinyl)-1-piperazinyl]propane tetraphosphate tetrahydrate
A825322
7-chloro-4-[4-[3-[4-(7-chloro-4-quinolyl)piperazin-1-yl]propyl]piperazin-1-yl]quinoline
5-23-03-00072 (beilstein handbook reference)
unii-a0hv2q956y
a0hv2q956y ,
NCGC00344515-02
AKOS015896173
SCHEMBL131649
piperaquine [who-dd]
7-chloro-4-(4-{3-[4-(7-chloroquinolin-4-yl)piperazin-1-yl]propyl}piperazin-1-yl)quinoline
1,3-bis[4-(7-chloroquinolin-4-yl)piperazin-1-yl]propane
CHEBI:91231
1,3-bis(4-(7-chloroquinolin-4-yl)piperazin-1-yl)propane
quinoline, 4,4'-(1,3-propanediyldi-4,1-piperazinediyl)bis[7-chloro-
DTXSID00193825
gtpl10025
4,4-(1,3-propanediyldi-4,1-piperazinediyl)bis(7-chloroquinoline)phosphate
DB13941
4,4'-(1,3-propanediydi-4,1-piper-azinediyl)bis[7-chloroquinoline]
BCP09615
Q7197338
SB19150
piperaquine-phosphate
1,3-bis[4-(7-chloroquinoline-4-yl)piperazin-1-yl]propane
bdbm50519563
HY-B1896
CS-0013957
piperaquine-d6

Research Excerpts

Overview

Piperaquine (PQ) is an important partner drug in antimalarial combination treatments. The long half-life of PQ raises concerns about drug resistance. Piperaquine is a highly lipid-soluble drug with a large Vss/F, long t1.

ExcerptReferenceRelevance
"Piperaquine (PQ) is an important partner in antimalarial treatment strategies. "( Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
Andrzejewski, C; Batty, KT; Ilett, KF; Jago, JD; Moore, BR; Page-Sharp, M, 2008
)
2.05
"Piperaquine was found to be a reversible, potent inhibitor of CYP3A with the following parameter estimates (%CV): IC"( Inhibition of CYP3A by Antimalarial Piperaquine and Its Metabolites in Human Liver Microsomes With IVIV Extrapolation.
Ashton, M; Aziz, MY; Hoffmann, KJ, 2018
)
1.48
"Piperaquine is an important partner drug used in artemisinin-based combination therapies (ACTs). "( Photo-Induced Electron Transfer Real-Time PCR for Detection of Plasmodium falciparum plasmepsin 2 Gene Copy Number.
L'Episcopia, M; Lucchi, NW; Severini, C; Souza, SS; Udhayakumar, V, 2018
)
1.92
"Piperaquine (PQ) is an important partner drug in antimalarial combination treatments, but the long half-life of PQ raises concerns about drug resistance. "( Piperaquine pharmacodynamics and parasite viability in a murine malaria model.
Batty, KT; Ilett, KF; Jago, JD; Moore, BR; Page-Sharp, M, 2009
)
3.24
"Piperaquine is a bisquinoline antimalarial drug extensively used as monotherapy in China in the 1980s and subsequently included as one of the components of the artemisinin-based combination therapies (ACTs) in the 1990s. "( Antimalarial efficacy of piperaquine-based antimalarial combination therapies: facts and uncertainties.
Bassat, Q; Cenci, F; Gargano, N, 2011
)
2.12
"Piperaquine is a promising anti-malarial partner drug used in a fixed-dose combination with dihydroartemisinin."( A population pharmacokinetic model of piperaquine in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum malaria in Sudan.
Adam, I; Ashton, M; Day, NP; Hanpithakpong, W; Hoglund, RM; Lindegardh, N; Nosten, F; Tarning, J; White, NJ, 2012
)
1.37
"Piperaquine (PQ) is an antimalarial drug enjoying a resurgence of use in combination with an artemisinin derivative because of parasite resistance to standard treatments. "( Measurement of piperaquine in plasma by liquid chromatography with ultraviolet absorbance detection.
Davis, TM; Hung, TY; Ilett, KF, 2003
)
2.11
"Piperaquine is a highly lipid-soluble drug with a large Vss/F, long t1/2,z and a clearance that is markedly higher in children than in adults."( Population pharmacokinetics of piperaquine in adults and children with uncomplicated falciparum or vivax malaria.
Davis, TM; Denis, MB; Hewitt, S; Hung, TY; Ilett, KF; Karunajeewa, H; Lim, C; Socheat, D, 2004
)
2.05
"Piperaquine is a bisquinoline antimalarial drug that was first synthesised in the 1960s, and used extensively in China and Indochina as prophylaxis and treatment during the next 20 years. "( Piperaquine: a resurgent antimalarial drug.
Davis, TM; Hung, TY; Ilett, KF; Karunajeewa, HA; Sim, IK, 2005
)
3.21
"Piperaquine (PQ) is an antimalarial drug whose high lipid solubility suggests that its absorption can be increased by a high-fat meal. "( Effects of a high-fat meal on the relative oral bioavailability of piperaquine.
Davis, TM; Ilett, KF; Sim, IK, 2005
)
2.01
"Piperaquine phosphate is an orally active bisquinolone antimalarial drug that has been used for the past 3 decades. "( Safety, tolerability, and single- and multiple-dose pharmacokinetics of piperaquine phosphate in healthy subjects.
Ahmed, T; Batra, V; Ganguly, S; Gautam, A; Kothari, M; Moehrle, JJ; Paliwal, J; Saha, N; Sharma, P; Varshney, B, 2008
)
2.02
"Piperaquine is an antimalarial drug that was extensively used in China during the 1980s and has recently received renewed interest as a partner drug in artemisinin-based combination therapy."( Quantification of the antimalarial piperaquine in plasma.
Lindegardh, N; Tarning, J, 2008
)
1.34

Toxicity

DPQ was highly efficacious and safe for the treatment of malaria in HIV-infected patients concurrently taking efavirenz- or nevirapine-based ART. IPTsc with dihydroartemisinin-piperaquine or artesunate-amodiaquine is a safe and effective approach to reducing malaria parasitaemia.

ExcerptReferenceRelevance
"Artekin is safe and effective combination therapy for uncomplicated malaria in children and adults."( Safety evaluation of fixed combination piperaquine plus dihydroartemisinin (Artekin) in Cambodian children and adults with malaria.
Davis, TM; Denis, MB; Hung, TY; Ilett, KF; Karunajeewa, H; Lim, C; Socheat, D, 2004
)
0.59
" Adverse events and clinical and parasitological outcomes were recorded."( Safety and efficacy of dihydroartemisinin/piperaquine (Artekin) for the treatment of uncomplicated Plasmodium falciparum malaria in Rwandan children.
D'Alessandro, U; Fanello, CI; Karema, C; Ngamije, D; van Doren, W; van Geertruyden, JP; van Overmeir, C, 2006
)
0.6
"Dihydroartemisinin-piperaquine, a fixed-dose combination antimalarial, is an inexpensive, safe and highly effective treatment for uncomplicated falciparum or vivax malaria."( Efficacy and safety of dihydroartemisinin-piperaquine.
Ashley, EA; Day, NP; Myint, HY; Nosten, F; White, NJ, 2007
)
0.93
" There were no significant dose-related adverse effects, but leucocytes were mildly elevated (F(1) and F(2) mice) and serum albumin was reduced (F(1) only) in the 300 mg/kg/day group."( Investigation of reproductive toxicity of piperaquine in mice.
Batty, KT; Davis, TM; Ilett, KF; Karunajeewa, HA; Moore, BR; Mueller, I; Page-Sharp, M; Rogerson, SJ; Shilkin, KB; Stirling, V, 2010
)
0.62
" Participants were actively monitored for adverse events for 28 days and then passively for up to 63 days after treatment."( Safety and tolerability of artemether-lumefantrine versus dihydroartemisinin-piperaquine for malaria in young HIV-infected and uninfected children.
Arinaitwe, E; Bigira, V; Dorsey, G; Gasasira, A; Homsy, J; Kakuru, A; Kamya, MR; Katrak, S; Sandison, TG; Tappero, JW; Wanzira, H, 2009
)
0.58
" Most adverse events were rare, with only cough, diarrhoea, vomiting, and anaemia occurring in more than 1% of treatments."( Safety and tolerability of artemether-lumefantrine versus dihydroartemisinin-piperaquine for malaria in young HIV-infected and uninfected children.
Arinaitwe, E; Bigira, V; Dorsey, G; Gasasira, A; Homsy, J; Kakuru, A; Kamya, MR; Katrak, S; Sandison, TG; Tappero, JW; Wanzira, H, 2009
)
0.58
"Both AL and DP were safe and well tolerated for the treatment of uncomplicated malaria in young HIV-infected and uninfected children."( Safety and tolerability of artemether-lumefantrine versus dihydroartemisinin-piperaquine for malaria in young HIV-infected and uninfected children.
Arinaitwe, E; Bigira, V; Dorsey, G; Gasasira, A; Homsy, J; Kakuru, A; Kamya, MR; Katrak, S; Sandison, TG; Tappero, JW; Wanzira, H, 2009
)
0.58
"04), there were no differences between treatment arms in the occurrence of adverse events."( Safety and efficacy of dihydroartemisinin-piperaquine versus artemether-lumefantrine in the treatment of uncomplicated Plasmodium falciparum malaria in Zambian children.
Chaponda, M; D'Alessandro, U; Hachizovu, S; Mukwamataba, D; Mulenga, M; Nambozi, M; Ubben, D; Van Geertruyden, JP, 2011
)
0.63
"DHA/PQP was as efficacious, safe and well tolerated in treatment of uncomplicated malaria as AL, though in the latter group more new infections during the follow up were observed."( Safety and efficacy of dihydroartemisinin-piperaquine versus artemether-lumefantrine in the treatment of uncomplicated Plasmodium falciparum malaria in Zambian children.
Chaponda, M; D'Alessandro, U; Hachizovu, S; Mukwamataba, D; Mulenga, M; Nambozi, M; Ubben, D; Van Geertruyden, JP, 2011
)
0.63
" Few and mild adverse events were reported."( Efficacy and safety of artemisinin-naphthoquine versus dihydroartemisinin-piperaquine in adult patients with uncomplicated malaria: a multi-centre study in Indonesia.
Amansyah, F; Dedang, TA; Driyah, S; Ekowatiningsih, R; Hasugian, AR; Januar, L; Labora, J; Prasetyorini, B; Purnama, A; Purnamasari, T; Salwati, E; Siswantoro, H; Tjitra, E; Wijayanto, B; Yusnita, EA; Yuwarni, E, 2012
)
0.61
"AN and DHP are confirmed very effective, safe and tolerate for treatment of any malaria."( Efficacy and safety of artemisinin-naphthoquine versus dihydroartemisinin-piperaquine in adult patients with uncomplicated malaria: a multi-centre study in Indonesia.
Amansyah, F; Dedang, TA; Driyah, S; Ekowatiningsih, R; Hasugian, AR; Januar, L; Labora, J; Prasetyorini, B; Purnama, A; Purnamasari, T; Salwati, E; Siswantoro, H; Tjitra, E; Wijayanto, B; Yusnita, EA; Yuwarni, E, 2012
)
0.61
" 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
)
0.63
" No serious adverse event was noted during the study period."( Monitoring the efficacy and safety of three artemisinin based-combinations therapies in Senegal: results from two years surveillance.
Abiola, A; Faye, B; Folly, K; Gaye, O; Lo, AC; Ndiaye, JL; Ndiaye, LA; Ndiaye, M; Sow, D; Sylla, K; Tine, RC, 2013
)
0.39
"In the context of scaling up of ACTs in Senegal, ASAQ, AL and DHAPQ are highly effective and safe antimalarial drugs."( Monitoring the efficacy and safety of three artemisinin based-combinations therapies in Senegal: results from two years surveillance.
Abiola, A; Faye, B; Folly, K; Gaye, O; Lo, AC; Ndiaye, JL; Ndiaye, LA; Ndiaye, M; Sow, D; Sylla, K; Tine, RC, 2013
)
0.39
" Incidence of adverse events was related to underlying disease; malaria being reported in both treatment arms."( Efficacy and safety of artemether-lumefantrine and dihydroartemisinin-piperaquine in the treatment of uncomplicated Plasmodium falciparum malaria in Kenyan children aged less than five years: results of an open-label, randomized, single-centre study.
Akhwale, W; Eyase, F; Johnson, JD; Juma, E; Koskei, N; Obonyo, C; Ogutu, BR; Omollo, R; Omondi, EK; Ongecha, JM; Onyango, KO; Otieno, GA; Otieno, L; Perkins, DJ, 2014
)
0.64
" Both ACT regimens were safe and well tolerated."( Artemisinin-based combination therapies are efficacious and safe for treatment of uncomplicated malaria in HIV-infected Ugandan children.
Achan, J; Arinaitwe, E; Charlebois, E; Clark, TD; Dorsey, G; Havlir, D; Ikilezi, G; Kakuru, A; Kamya, MR; Muhindo, MK; Mwangwa, F; Rosenthal, PJ; Ruel, T; Tappero, JW, 2014
)
0.4
"Treatment of uncomplicated malaria with AL or DP was efficacious and safe in HIV-infected children taking ART."( Artemisinin-based combination therapies are efficacious and safe for treatment of uncomplicated malaria in HIV-infected Ugandan children.
Achan, J; Arinaitwe, E; Charlebois, E; Clark, TD; Dorsey, G; Havlir, D; Ikilezi, G; Kakuru, A; Kamya, MR; Muhindo, MK; Mwangwa, F; Rosenthal, PJ; Ruel, T; Tappero, JW, 2014
)
0.4
"9% of side reaction with 7 cases suffering from mild adverse responses among 71 of full-course medication."( [Therapeutic efficacy and safety of compound dihydroartemisinin/piperaquine for uncomplicated Plasmodium falciparum infection in Laiza City of Myanmar bordering on China].
Deng, Y; Lasi, JH; Sun, XD; Sun, XY; Wang, H; Wang, J; Yang, YC; Zhang, ZX, 2011
)
0.61
"DHAPIP is efficacious and safe for the treatment of uncomplicated falciparum malaria in Laiza city of Myanmar in the border area."( [Therapeutic efficacy and safety of compound dihydroartemisinin/piperaquine for uncomplicated Plasmodium falciparum infection in Laiza City of Myanmar bordering on China].
Deng, Y; Lasi, JH; Sun, XD; Sun, XY; Wang, H; Wang, J; Yang, YC; Zhang, ZX, 2011
)
0.61
" There were no differences between the study arms in the incidence of serious adverse events during the intervention and the incidence of malaria during the 1-y period after the intervention was stopped."( Protective efficacy and safety of three antimalarial regimens for the prevention of malaria in young Ugandan children: a randomized controlled trial.
Achan, J; Aweeka, FT; Bigira, V; Clark, TD; Dorsey, G; Havlir, DV; Huang, L; Kamya, MR; Kapisi, J; Kinara, S; Muhindo, MK; Mwangwa, F; Osterbauer, B; Rosenthal, PJ, 2014
)
0.4
" No statistical significant differences were observed in the occurrence of adverse events among treatment groups."( Randomized non-inferiority and safety trial of dihydroartemisin-piperaquine and artesunate-amodiaquine versus artemether-lumefantrine in the treatment of uncomplicated Plasmodium falciparum malaria in Cameroonian children.
Ali, IM; Chedjou, JP; Ekollo, AM; Evehe, MS; Froeschl, G; Heumann, C; Mansmann, U; Mbacham, WF; Moyeh, MN; Ndikum, VN; Ngongang, EO; Nji, AM; Ogundahunsi, O, 2015
)
0.66
" Patients were contacted on day 5 ± 2 to assess adherence and adverse events (AEs)."( Prospective observational study to evaluate the clinical safety of the fixed-dose artemisinin-based combination Eurartesim® (dihydroartemisinin/piperaquine), in public health facilities in Burkina Faso, Mozambique, Ghana, and Tanzania.
Abdulla, S; Adjei, A; Adjuik, M; Akparibo, R; Baiden, R; Binka, F; Compaoré, G; Gyapong, M; Halidou, T; Macete, E; Mulokozi, A; Oduro, A; Ogutu, B; Osei, I; Owusu-Agyei, S; Sevene, E; Sie, A; Smith, P; Upunda, GL; Valea, I; Yawson, A, 2015
)
0.62
" Most patients,95% (10,359/10,925), did not report any adverse event following at least one dose of Eurartesim®."( Prospective observational study to evaluate the clinical safety of the fixed-dose artemisinin-based combination Eurartesim® (dihydroartemisinin/piperaquine), in public health facilities in Burkina Faso, Mozambique, Ghana, and Tanzania.
Abdulla, S; Adjei, A; Adjuik, M; Akparibo, R; Baiden, R; Binka, F; Compaoré, G; Gyapong, M; Halidou, T; Macete, E; Mulokozi, A; Oduro, A; Ogutu, B; Osei, I; Owusu-Agyei, S; Sevene, E; Sie, A; Smith, P; Upunda, GL; Valea, I; Yawson, A, 2015
)
0.62
" Safety was analysed based on adverse events (AE), laboratory abnormalities and abnormalities on electrocardiograph."( Efficacy and safety of fixed dose combination of arterolane maleate and piperaquine phosphate dispersible tablets in paediatric patients with acute uncomplicated Plasmodium falciparum malaria: a phase II, multicentric, open-label study.
Anvikar, AR; Arora, S; Iyer, SS; Jalali, RK; Mishra, P; Rao, BS; Roy, A; Rulisa, S; Saha, N; Sharma, P; Toure, OA; Valecha, N, 2015
)
0.65
" The primary endpoint was the PCR-corrected adequate clinical and parasitological response (ACPR) at day 28 (D28); the secondary endpoints included ACPR at D42, clearance times for parasites, fever, and gametocytes, and the incidence of adverse events."( [Evaluation of the efficacy and safety of three 2-drug combinations for the treatment of uncomplicated Plasmodium falciparum malaria in Senegal: artesunate-amodiaquine, dihydroartemisinin-piperaquine, and artemether-lumefantrine].
Abiola, A; Ba, MS; Dieng, Y; Faye, B; Gaye, O; Lo, AC; Ndiaye, JL; Ndiaye, M; Pene, M; Seck, A; Sow, D; Sylla, K; Tine, RC,
)
0.32
" The combinations were well tolerated, with no serious adverse events reported during the follow-up period."( [Evaluation of the efficacy and safety of three 2-drug combinations for the treatment of uncomplicated Plasmodium falciparum malaria in Senegal: artesunate-amodiaquine, dihydroartemisinin-piperaquine, and artemether-lumefantrine].
Abiola, A; Ba, MS; Dieng, Y; Faye, B; Gaye, O; Lo, AC; Ndiaye, JL; Ndiaye, M; Pene, M; Seck, A; Sow, D; Sylla, K; Tine, RC,
)
0.32
" Safety endpoints were analysis of adverse events, vital signs, laboratory data, and abnormalities on electrocardiograph."( Comparison of the safety and efficacy of fixed-dose combination of arterolane maleate and piperaquine phosphate with chloroquine in acute, uncomplicated Plasmodium vivax malaria: a phase III, multicentric, open-label study.
Anvikar, AR; Arora, S; Gogtay, N; Iyer, SS; Jalali, RK; Kochar, SK; Kumar, NB; Lakhani, JD; Rajadhyaksha, GC; Rao, BH; Roy, A; Saha, N; Savargaonkar, D; Sharma, P; Solanki, BB; Srivastava, B; Tripathi, SK; Valecha, N, 2016
)
0.66
" Incidence of adverse events was 82."( Comparison of the safety and efficacy of fixed-dose combination of arterolane maleate and piperaquine phosphate with chloroquine in acute, uncomplicated Plasmodium vivax malaria: a phase III, multicentric, open-label study.
Anvikar, AR; Arora, S; Gogtay, N; Iyer, SS; Jalali, RK; Kochar, SK; Kumar, NB; Lakhani, JD; Rajadhyaksha, GC; Rao, BH; Roy, A; Saha, N; Savargaonkar, D; Sharma, P; Solanki, BB; Srivastava, B; Tripathi, SK; Valecha, N, 2016
)
0.66
"AZI-PQ appears to be well tolerated and safe in pregnancy."( Safety, tolerability and pharmacokinetic properties of coadministered azithromycin and piperaquine in pregnant Papua New Guinean women.
Auyeung, SO; Batty, KT; Benjamin, JM; Davis, TM; Griffin, S; Moore, BR; Mueller, I; Page-Sharp, M; Rogerson, SJ; Salman, S; Siba, PM; Yadi, G, 2016
)
0.66
" Monthly IPT-DP was associated with fewer serious adverse events than placebo, daily co-trimoxazole, or monthly SP."( Safety, tolerability, and efficacy of repeated doses of dihydroartemisinin-piperaquine for prevention and treatment of malaria: a systematic review and meta-analysis.
Dorsey, G; Gutman, J; Kovacs, S; Stergachis, A; Ter Kuile, FO, 2017
)
0.69
"In endemic areas, malaria and its adverse effects in schoolchildren may be prevented by intermittent preventive treatment (IPTsc)."( Efficacy and safety of intermittent preventive treatment in schoolchildren with sulfadoxine/pyrimethamine (SP) and SP plus piperaquine in Democratic Republic of the Congo: a randomised controlled trial.
da Luz, RI; Doua, JY; Lutumba, P; Matangila, JR; Mitashi, P; Van Geertruyden, JP, 2017
)
0.66
"Uncommon and rare adverse events (AEs), with delayed onset may not be detected before new drugs are licensed and deployed."( Post-licensure safety evaluation of dihydroartemisinin piperaquine in the three major ecological zones across Ghana.
Adjei, A; Adjuik, M; Baiden, R; Binka, F; Gyapong, M; Oduro, AR; Osei, I; Owusu-Agyei, S; Sobe, E; Yawson, A, 2017
)
0.7
" There were nine adverse events of special interest (AESI); itching/pruritus (7), dizziness (1), and skin lesions (1)."( Post-licensure safety evaluation of dihydroartemisinin piperaquine in the three major ecological zones across Ghana.
Adjei, A; Adjuik, M; Baiden, R; Binka, F; Gyapong, M; Oduro, AR; Osei, I; Owusu-Agyei, S; Sobe, E; Yawson, A, 2017
)
0.7
" 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
" For quinine, clindamycin, and mefloquine and the combinations of sulfadoxine+pyrimethamine and artemether+lumefantrine, there are reports (including studies without internal comparison groups) that combined describe 304 to >1100 exposures of women in the first trimester for each drug with no conclusive evidence of adverse effects on pregnancy at therapeutic doses."( Animal Embryotoxicity Studies of Key Non-Artemisinin Antimalarials and Use in Women in the First Trimester.
Clark, RL, 2017
)
0.46
" Both the treatments were found to be safe and well tolerated."( Assessment of Efficacy and Safety of Arterolane Maleate-Piperaquine Phosphate Dispersible Tablets in Comparison With Artemether-Lumefantrine Dispersible Tablets in Pediatric Patients With Acute Uncomplicated Plasmodium falciparum Malaria: A Phase 3, Rando
Anvikar, AR; Behra, N; Das, RR; Gaye, O; Jalali, RK; Maheshwar, AV; Mishra, P; Mwapasa, V; Nasa, A; Roy, A; Sagara, I; Sharma, P; Sharma, SK; Thompson, R; Toure, OA; Tshefu, AK; Valecha, N, 2017
)
0.7
" Its adverse effects are generally tolerable and temporary."( Choreoathetosis - an unusual adverse effect of dihydroartemisinin-piperaquine: a case report.
Kadia, BM; Morfaw, C; Simo, ACG, 2017
)
0.69
"Although dihydroartemisinin-piperaquine is increasingly popular as a well-tolerated/efficacious antimalarial drug, clinicians must note the rare possibility of choreoathetosis as an adverse effect of this medication and educate patients accordingly."( Choreoathetosis - an unusual adverse effect of dihydroartemisinin-piperaquine: a case report.
Kadia, BM; Morfaw, C; Simo, ACG, 2017
)
0.99
" The majority of adverse events affected the gastrointestinal and respiratory tracts and were transient and mild to moderate in severity."( Efficacy and Safety of Fosmidomycin-Piperaquine as Nonartemisinin-Based Combination Therapy for Uncomplicated Falciparum Malaria: A Single-Arm, Age De-escalation Proof-of-Concept Study in Gabon.
Adegnika, AA; Cattaneo, C; Duparc, S; Endamne, L; Flohr, L; Groger, M; Hutchinson, D; Kabwende, L; Kim, J; Kremsner, PG; Lell, B; Lötsch, F; Mischlinger, J; Moehrle, J; Mombo-Ngoma, G; Mordmüller, B; Nguyen, TT; Ramharter, M; Remppis, J; Sievers, M; Velavan, TP; Veletzky, L; Zoleko Manego, R, 2018
)
0.76
" The combination appeared to have high efficacy and be safe and well tolerated despite observed transient changes in electrocardiogram with prolongation of the QT interval."( Efficacy and Safety of Fosmidomycin-Piperaquine as Nonartemisinin-Based Combination Therapy for Uncomplicated Falciparum Malaria: A Single-Arm, Age De-escalation Proof-of-Concept Study in Gabon.
Adegnika, AA; Cattaneo, C; Duparc, S; Endamne, L; Flohr, L; Groger, M; Hutchinson, D; Kabwende, L; Kim, J; Kremsner, PG; Lell, B; Lötsch, F; Mischlinger, J; Moehrle, J; Mombo-Ngoma, G; Mordmüller, B; Nguyen, TT; Ramharter, M; Remppis, J; Sievers, M; Velavan, TP; Veletzky, L; Zoleko Manego, R, 2018
)
0.76
" After exclusion of blue urine, adverse events were similar across all groups (59 [74%] of 80 participants had 162 adverse events overall, 145 [90%] of which were mild)."( Efficacy and safety of primaquine and methylene blue for prevention of Plasmodium falciparum transmission in Mali: a phase 2, single-blind, randomised controlled trial.
Bousema, T; Bradley, J; Brown, JM; Chen, I; Diarra, K; Diawara, H; Dicko, A; Drakeley, C; Gosling, R; Hwang, J; Issiaka, D; Keita, S; Kone, DT; Lanke, K; Mahamar, A; McCulloch, C; Müller, O; Roh, ME; Sanogo, K; Soumare, HM; Srinivasan, V; Stone, WJR; Traore, SF, 2018
)
0.48
" Additional outcomes included intervention coverage, treatment adherence, occurrence of adverse events, and cumulative incidences 3, 12, and 16 months post-MDA."( A cluster randomised controlled trial of two rounds of mass drug administration in Zanzibar, a malaria pre-elimination setting-high coverage and safety, but no significant impact on transmission.
Ali, AS; Ali, SM; Aydin-Schmidt, B; Bennett, A; Björkman, A; Hodzic, L; Islam, A; Jovel, I; Khamis, M; Magnusson, E; Mårtensson, A; Mkali, H; Morris, U; Msellem, MI; Poirot, E; Sachs, MC; Shija, SJ; Tarning, J, 2018
)
0.48
" Adverse events were reported in 11."( A cluster randomised controlled trial of two rounds of mass drug administration in Zanzibar, a malaria pre-elimination setting-high coverage and safety, but no significant impact on transmission.
Ali, AS; Ali, SM; Aydin-Schmidt, B; Bennett, A; Björkman, A; Hodzic, L; Islam, A; Jovel, I; Khamis, M; Magnusson, E; Mårtensson, A; Mkali, H; Morris, U; Msellem, MI; Poirot, E; Sachs, MC; Shija, SJ; Tarning, J, 2018
)
0.48
"Plasmodium falciparum and Plasmodium vivax infections are important causes of adverse pregnancy outcomes in the Asia-Pacific region."( Efficacy and safety of intermittent preventive treatment and intermittent screening and treatment versus single screening and treatment with dihydroartemisinin-piperaquine for the control of malaria in pregnancy in Indonesia: a cluster-randomised, open-la
Adams, ER; Ahmed, R; Asih, PBS; Chen, T; Faragher, B; Khairallah, C; Lukito, T; Maratina, SS; Pace, C; Poespoprodjo, JR; Price, RN; Santana-Morales, MA; Smedley, J; Syafruddin, D; Ter Kuile, FO; Unwin, VT; Wang, D; Williams, CT, 2019
)
0.71
" Conditions related to the pregnancy, the puerperium, and the perinatal period were the most common serious adverse events for the mothers, and infections and infestations for the infants."( Efficacy and safety of intermittent preventive treatment and intermittent screening and treatment versus single screening and treatment with dihydroartemisinin-piperaquine for the control of malaria in pregnancy in Indonesia: a cluster-randomised, open-la
Adams, ER; Ahmed, R; Asih, PBS; Chen, T; Faragher, B; Khairallah, C; Lukito, T; Maratina, SS; Pace, C; Poespoprodjo, JR; Price, RN; Santana-Morales, MA; Smedley, J; Syafruddin, D; Ter Kuile, FO; Unwin, VT; Wang, D; Williams, CT, 2019
)
0.71
" They received a directly-observed 3-day standard treatment of DPQ and were followed up until day 63 for malaria infection and adverse events."( Efficacy and safety of dihydroartemisinin-piperaquine for treatment of Plasmodium falciparum uncomplicated malaria in adult patients on antiretroviral therapy in Malawi and Mozambique: an open label non-randomized interventional trial.
Banda, CG; Kalilani-Phiri, L; Khoo, SH; Lalloo, DG; Macuacua, S; Maculuve, S; Mallewa, J; Mukaka, M; Mwapasa, V; Piqueras, M; Sevene, E; Terlouw, DJ; Vala, A, 2019
)
0.78
"DPQ was highly efficacious and safe for the treatment of malaria in HIV-infected patients concurrently taking efavirenz- or nevirapine-based ART, despite known pharmacokinetic interactions between dihydroartemisinin-piperaquine and efavirenz- or nevirapine-based ART regimens."( Efficacy and safety of dihydroartemisinin-piperaquine for treatment of Plasmodium falciparum uncomplicated malaria in adult patients on antiretroviral therapy in Malawi and Mozambique: an open label non-randomized interventional trial.
Banda, CG; Kalilani-Phiri, L; Khoo, SH; Lalloo, DG; Macuacua, S; Maculuve, S; Mallewa, J; Mukaka, M; Mwapasa, V; Piqueras, M; Sevene, E; Terlouw, DJ; Vala, A, 2019
)
0.96
" Although piperaquine administration resulted in QTc prolongation, no cardiovascular adverse events were found in these patients."( Pooled Multicenter Analysis of Cardiovascular Safety and Population Pharmacokinetic Properties of Piperaquine in African Patients with Uncomplicated Falciparum Malaria.
Abdulla, S; Adjei, A; Adjuik, M; Asante, KP; Baiden, R; Binka, F; Compaore, G; Day, NPJ; Gyapong, M; Kabanywanyi, AM; Macete, E; Oduro, A; Ogutu, B; Osei, I; Owusu-Agyei, S; Sevene, E; Sie, A; Tarning, J; Tinto, H; Valea, I; Wattanakul, T; White, NJ; Winterberg, M, 2020
)
1.18
" Adverse events were assessed within four hours of drugs intake."( Efficacy and safety of praziquantel and dihydroartemisinin piperaquine combination for treatment and control of intestinal schistosomiasis: A randomized, non-inferiority clinical trial.
Aklillu, E; Kamuhabwa, A; Kinung'hi, S; Minzi, O; Mnkugwe, RH, 2020
)
0.8
"4%) of the study participants experienced mild and transient treatment-associated adverse events, post-treatment abdominal pain (27."( Efficacy and safety of praziquantel and dihydroartemisinin piperaquine combination for treatment and control of intestinal schistosomiasis: A randomized, non-inferiority clinical trial.
Aklillu, E; Kamuhabwa, A; Kinung'hi, S; Minzi, O; Mnkugwe, RH, 2020
)
0.8
" The computed tomography (CT) imaging changes within 10 days, corrected QT interval changes, adverse events, and abnormal laboratory parameters were the secondary outcomes."( Safety and efficacy of artemisinin-piperaquine for treatment of COVID-19: an open-label, non-randomised and controlled trial.
Deng, C; Guan, X; Guo, J; Jin, C; Li, G; Li, H; Song, J; Tang, Y; Wang, Q; Xie, F; Xu, Q; Yu, W; Yuan, M; Yuan, Y; Zhang, H; Zou, Y, 2021
)
0.9
" Both groups had mild adverse events."( Safety and efficacy of artemisinin-piperaquine for treatment of COVID-19: an open-label, non-randomised and controlled trial.
Deng, C; Guan, X; Guo, J; Jin, C; Li, G; Li, H; Song, J; Tang, Y; Wang, Q; Xie, F; Xu, Q; Yu, W; Yuan, M; Yuan, Y; Zhang, H; Zou, Y, 2021
)
0.9
" Both treatments were safe and well-tolerated."( Efficacy and safety of dihydroartemisinin-piperaquine versus artemether-lumefantrine for treatment of uncomplicated Plasmodium falciparum malaria in Ugandan children: a systematic review and meta-analysis of randomized control trials.
Assefa, DG; Bekele, D; Getachew, E; Joseph, M; Manyazewal, T; Tesfahunei, HA; Zeleke, ED, 2021
)
0.89
" Adverse events (AE) were collected, with a special focus on cardiovascular safety by including electrocardiogram QT intervals evaluated after correction with either Bazett's (QTcB) or Fridericia's (QTcF) methods, at baseline and after treatment."( Longitudinal study based on a safety registry for malaria patients treated with artenimol-piperaquine in six European countries.
Angheben, A; Bacchieri, A; Bardají, A; Behrens, RH; Bisoffi, Z; Bottieau, E; Bouchaud, O; Bourhis, Y; Calleri, G; Duparc, S; Hatz, C; Iannucelli, M; Jelinek, T; Martin, C; Mattera, GG; Mechain, M; Merlo Pich, E; Nothdurft, HD; Ramos, JM; Rapp, C; Rojo-Marcos, G; Salas-Coronas, J; Tommasini, S; Velasco, M; Vignier, N; Visser, LG, 2021
)
0.84
" Reactive focal mass drug administration (rfMDA) may be safe and more effective."( Effectiveness and safety of reactive focal mass drug administration (rfMDA) using dihydroartemisinin-piperaquine to reduce malaria transmission in the very low-endemic setting of Eswatini: a pragmatic cluster randomised controlled trial.
Baltzell, K; Benjamin-Chung, J; Bhangu, K; Dlamini, B; Dlamini, N; Dufour, MK; Gosling, R; Greenhouse, B; Helb, D; Hsiang, MS; Kalungero, M; Kunene, S; Malambe, C; Maphalala, G; Mngadi, N; Nhlabathi, N; Ntshalintshali, N; Pindolia, D; Prach, LM; Tesfa, G; Vilakati, S; Whittemore, B, 2021
)
0.84
" No serious adverse events occurred."( Effectiveness and safety of reactive focal mass drug administration (rfMDA) using dihydroartemisinin-piperaquine to reduce malaria transmission in the very low-endemic setting of Eswatini: a pragmatic cluster randomised controlled trial.
Baltzell, K; Benjamin-Chung, J; Bhangu, K; Dlamini, B; Dlamini, N; Dufour, MK; Gosling, R; Greenhouse, B; Helb, D; Hsiang, MS; Kalungero, M; Kunene, S; Malambe, C; Maphalala, G; Mngadi, N; Nhlabathi, N; Ntshalintshali, N; Pindolia, D; Prach, LM; Tesfa, G; Vilakati, S; Whittemore, B, 2021
)
0.84
" Imatinib + SOC-treated participants exhibited no increase in number or severity of adverse events, a significantly accelerated decline in parasite density and pyrexia, and no DPC."( Imatinib augments standard malaria combination therapy without added toxicity.
Chien, HD; Kesely, KR; Low, PS; Noomuna, P; Pantaleo, A; Putt, KS; Tuan, TA; Turrini, FM, 2021
)
0.62
" The commonly reported clinical adverse event was vomiting."( Efficacy and safety of fixed dose combination of arterolane maleate and piperaquine phosphate in comparison with chloroquine phosphate in children with acute uncomplicated
Anvikar, AR; Bahl, RK; Baliga, BS; Bhardwaj, AC; Choudhury, R; Das, RR; Ghosh, SK; Goyal, VK; Jalali, RK; Jauhri, N; Khurana, O; Mishra, DN; Nasa, A; Pandey, M; Punj, A; Roy, A; Sharma, SK; Soans, ST; Srivastava, B; Valecha, N,
)
0.36
"Intermittent preventive treatment in pregnancy (IPTp) with sulfadoxine-pyrimethamine (SP) is recommended by the World Health Organization for the prevention of malaria in pregnancy (MIP)-associated adverse outcomes in high burden areas."( Safety and efficacy of intermittent presumptive treatment with sulfadoxine-pyrimethamine using rapid diagnostic test screening and treatment with dihydroartemisinin-piperaquine at the first antenatal care visit (IPTp-SP+): study protocol for a randomized
Champo, D; Chongwe, G; Ippolito, MM; Kabuya, JB; Manyando, C; Mulenga, M; Mwakazanga, D; Sikalima, J; Tende, C; Young, AMP, 2021
)
0.82
" Secondary endpoints include incident MIP at other time points, placental malaria, congenital malaria, hemoglobin trends, birth outcomes, and incidence of adverse events in infants up to the first birthday."( Safety and efficacy of intermittent presumptive treatment with sulfadoxine-pyrimethamine using rapid diagnostic test screening and treatment with dihydroartemisinin-piperaquine at the first antenatal care visit (IPTp-SP+): study protocol for a randomized
Champo, D; Chongwe, G; Ippolito, MM; Kabuya, JB; Manyando, C; Mulenga, M; Mwakazanga, D; Sikalima, J; Tende, C; Young, AMP, 2021
)
0.82
" Intermittent preventive treatment in pregnancy (IPTp) with sulphadoxine-pyrimethamine is recommended for malaria prevention in HIV-uninfected women, but it is contraindicated in those HIV-infected on cotrimoxazole prophylaxis (CTXp) due to potential adverse effects."( Evaluation of the safety and efficacy of dihydroartemisinin-piperaquine for intermittent preventive treatment of malaria in HIV-infected pregnant women: protocol of a multicentre, two-arm, randomised, placebo-controlled, superiority clinical trial (MAMAH
Dimessa, LB; El Gaaloul, M; Esen, M; Garcia-Otero, L; González, R; Lagler, H; Lell, B; Menendez, C; Mischlinger, J; Mombo-Ngoma, G; Nhampossa, T; Piqueras, M; Pons-Duran, C; Ramharter, M; Sanz, S; Saute, F; Sevene, E; Tchouatieu, AM; Zoleko Manego, R, 2021
)
0.86
" Secondary outcomes include prevalence of malaria-related maternal and infant outcomes and proportion of adverse perinatal outcomes."( Evaluation of the safety and efficacy of dihydroartemisinin-piperaquine for intermittent preventive treatment of malaria in HIV-infected pregnant women: protocol of a multicentre, two-arm, randomised, placebo-controlled, superiority clinical trial (MAMAH
Dimessa, LB; El Gaaloul, M; Esen, M; Garcia-Otero, L; González, R; Lagler, H; Lell, B; Menendez, C; Mischlinger, J; Mombo-Ngoma, G; Nhampossa, T; Piqueras, M; Pons-Duran, C; Ramharter, M; Sanz, S; Saute, F; Sevene, E; Tchouatieu, AM; Zoleko Manego, R, 2021
)
0.86
" There were no reported serious adverse events associated with any of the regimens."( Efficacy and safety of artemether-lumefantrine and dihydroartemisinin-piperaquine for the treatment of uncomplicated Plasmodium falciparum malaria and prevalence of molecular markers associated with artemisinin and partner drug resistance in Uganda.
Asua, V; Belay, K; Bosco, A; Bwanika, JB; Ebong, C; Gonahasa, S; Gudoi, S; Halsey, ES; Kamya, MR; Kapisi, J; Kigozi, R; Kyabayinze, D; Lucchi, NW; Moriarty, LF; Mpimbaza, A; Namuganga, JF; Niang, M; Nsobya, SL; Opigo, J; Rubahika, D; Rutazana, D; Sebikaari, G; Souza, SSS; Sserwanga, A; Tibenderana, J; Yeka, A, 2021
)
0.86
"DP remains highly effective and safe for the treatment of uncomplicated malaria in Uganda."( Efficacy and safety of artemether-lumefantrine and dihydroartemisinin-piperaquine for the treatment of uncomplicated Plasmodium falciparum malaria and prevalence of molecular markers associated with artemisinin and partner drug resistance in Uganda.
Asua, V; Belay, K; Bosco, A; Bwanika, JB; Ebong, C; Gonahasa, S; Gudoi, S; Halsey, ES; Kamya, MR; Kapisi, J; Kigozi, R; Kyabayinze, D; Lucchi, NW; Moriarty, LF; Mpimbaza, A; Namuganga, JF; Niang, M; Nsobya, SL; Opigo, J; Rubahika, D; Rutazana, D; Sebikaari, G; Souza, SSS; Sserwanga, A; Tibenderana, J; Yeka, A, 2021
)
0.86
" No delay in parasite clearance nor severe adverse reaction was observed."( Efficacy and safety of dihydroartemisinin-piperaquine for the treatment of uncomplicated Plasmodium falciparum and Plasmodium vivax malaria in Papua and Sumatra, Indonesia.
Anggraeni, ND; Asih, PBS; Basri, HH; Bustos, MDG; Dewayanti, FK; Hutahaean, J; Kusumaningsih, M; Mulyani, PS; Robaha, M; Rozi, IE; Sariwati, E; Syafruddin, D; Wangsamuda, S; Zulfah, S, 2022
)
0.99
" Adverse events over the first 28 days were reported in 27 (54%) of 50 patients treated with dihydroartemisinin-piperaquine alone, 29 (58%) of 50 patients treated with tafenoquine plus dihydroartemisinin-piperaquine, and 22 (44%) of 50 patients treated with primaquine plus dihydroartemisinin-piperaquine."( Tafenoquine co-administered with dihydroartemisinin-piperaquine for the radical cure of Plasmodium vivax malaria (INSPECTOR): a randomised, placebo-controlled, efficacy and safety study.
Baird, JK; Berni, A; Budiman, W; Cedar, E; Chand, K; Crenna-Darusallam, C; Duparc, S; Ekawati, LL; Elyazar, I; Fernando, D; Fletcher, K; Goyal, N; Green, JA; Instiaty, I; Jones, S; Kleim, JP; Lardo, S; Martin, A; Noviyanti, R; Prasetya, CB; Rolfe, K; Santy, YW; Satyagraha, AW; Sharma, H; Soebandrio, A; Subekti, D; Sutanto, I; Tan, LK; Taylor, M, 2023
)
1.37
" 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
)
1.46
"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
)
1.42
" RCTs comparing IPTp DP versus recommended standard treatment for IPTp with these outcome measures were analyzed; change in QTc interval, serious adverse events (SAE), grade 3 or 4 adverse events possibly related to study drug and vomiting within 30 min after study drug administration."( Safety and tolerability of repeated doses of dihydroartemisinin-piperaquine for intermittent preventive treatment of malaria in pregnancy: a systematic review and an aggregated data meta-analysis of randomized controlled trials.
Abebe, A; Ahmedin, M; Atim, MG; Embaye, SM; Kahabuka, M; Kazembe, D; Manyazewal, T; Mesfin, T; Muthoka, EN; Namuganza, S; Usmael, K, 2023
)
1.15

Pharmacokinetics

Piperaquine-dihydroartemisinin combination therapy has established efficacy for the treatment of malaria. A more comprehensive understanding of the pharmacokinetic properties and factors contributing to inter- and intra-individual variability is critical to optimize clinical use. Co-administration of PPQ and KAF156 had no overall effect on AUC of either compound.

ExcerptReferenceRelevance
"To investigate the pharmacokinetic properties of piperaquine after repeated oral administration of the antimalarial combination CV8 in healthy subjects."( Pharmacokinetics of piperaquine after repeated oral administration of the antimalarial combination CV8 in 12 healthy male subjects.
Ashton, M; Friberg Hietala, S; Hai, TN; Röshammar, D; Van Huong, N, 2006
)
0.91
" Population pharmacokinetic parameter estimates were obtained by nonlinear mixed effects modeling of the observed data using NONMEM."( Pharmacokinetics of piperaquine after repeated oral administration of the antimalarial combination CV8 in 12 healthy male subjects.
Ashton, M; Friberg Hietala, S; Hai, TN; Röshammar, D; Van Huong, N, 2006
)
0.66
" Piperaquine pharmacokinetics were characterized by a large volume of distribution and a terminal half-life of several days."( Pharmacokinetics of piperaquine after repeated oral administration of the antimalarial combination CV8 in 12 healthy male subjects.
Ashton, M; Friberg Hietala, S; Hai, TN; Röshammar, D; Van Huong, N, 2006
)
1.57
"This study aimed to evaluate the pharmacokinetic properties of piperaquine in the rat after intravenous and oral administration, and to identify and characterize the main piperaquine metabolites in rat plasma, urine, faeces and bile after intravenous administration."( Pharmacokinetics and metabolism of the antimalarial piperaquine after intravenous and oral single doses to the rat.
Ashton, M; Day, NJ; Lindegardh, N; Sandberg, S; Tarning, J; White, NJ, 2008
)
0.84
" However, there is a paucity of detailed preclinical and pharmacokinetic data to link PQ serum concentrations and toxicity or efficacy."( Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
Andrzejewski, C; Batty, KT; Ilett, KF; Jago, JD; Moore, BR; Page-Sharp, M, 2008
)
0.61
" Pharmacokinetic analysis for both the rising single- and multiple-dose studies was done using the noncompartmental approach."( Safety, tolerability, and single- and multiple-dose pharmacokinetics of piperaquine phosphate in healthy subjects.
Ahmed, T; Batra, V; Ganguly, S; Gautam, A; Kothari, M; Moehrle, JJ; Paliwal, J; Saha, N; Sharma, P; Varshney, B, 2008
)
0.58
" (iii) Pharmacokinetic parameters determined from mice given 100mg/(kg day) PQP for 5 days."( Toxicology and pharmacokinetics of piperaquine in mice.
Batty, KT; Davis, TM; Ilett, KF; Karunajeewa, HA; Moore, BR; Mueller, I; Page-Sharp, M; Shilkin, KB; Stirling, V, 2008
)
0.62
" The aim of this study was to determine the influence of a standard Vietnamese meal on the single-dose pharmacokinetics of piperaquine when administered in combination with dihydroartemisinin, and to gain extended data on the terminal half-life of piperaquine in healthy Vietnamese volunteers."( The influence of food on the pharmacokinetics of piperaquine in healthy Vietnamese volunteers.
Ashton, M; Hai, TN; Hietala, SF; Van Huong, N, 2008
)
0.81
"0057), and the terminal elimination half-life was significantly shorter (17."( Pharmacokinetics of dihydroartemisinin and piperaquine in pregnant and nonpregnant women with uncomplicated falciparum malaria.
Laochan, N; Lindegardh, N; McGready, R; Mu, O; Nosten, F; Phyo, AP; Rijken, MJ; Singhasivanon, P; Tarning, J; Than, HH; White, N; Win, AK, 2011
)
0.63
" The pharmacokinetic properties of antimalarial drugs are often affected by pregnancy, resulting in lower drug concentrations and a consequently higher risk of treatment failure."( Population pharmacokinetics of dihydroartemisinin and piperaquine in pregnant and nonpregnant women with uncomplicated malaria.
Day, NP; Hanpithakpong, W; Lindegardh, N; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Tarning, J; White, NJ, 2012
)
0.63
" The aim of this study was to describe the pharmacokinetic and pharmacodynamic properties of piperaquine in 236 children with uncomplicated falciparum malaria in Burkina Faso."( Population pharmacokinetics and pharmacodynamics of piperaquine in children with uncomplicated falciparum malaria.
Day, NP; Hanpithakpong, W; Jongrak, N; Lindegardh, N; Nosten, F; Ouedraogo, JB; Parikh, S; Rosenthal, PJ; Rouamba, N; Somé, FA; Tarning, J; White, NJ; Zongo, I, 2012
)
0.85
"The pharmacokinetic properties of piperaquine were investigated in 12 pregnant and 12 well-matched, non-pregnant women receiving a three-day oral fixed dose combination regimen of dihydroartemisinin and piperaquine for treatment of uncomplicated Plasmodium falciparum at New Halfa Hospital in eastern Sudan."( Pharmacokinetics of piperaquine in pregnant women in Sudan with uncomplicated Plasmodium falciparum malaria.
Adam, I; Lindegardh, N; Mahgoub, H; McGready, R; Nosten, F; Tarning, J, 2012
)
0.98
" The pharmacokinetic properties of many anti-malarials are also altered during pregnancy, often resulting in a decreased drug exposure."( A population pharmacokinetic model of piperaquine in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum malaria in Sudan.
Adam, I; Ashton, M; Day, NP; Hanpithakpong, W; Hoglund, RM; Lindegardh, N; Nosten, F; Tarning, J; White, NJ, 2012
)
0.65
" A statistically significant decrease in estimated terminal piperaquine half-life in pregnant compared with non-pregnant women was found, but there were no differences in post-hoc estimates of total piperaquine exposure."( A population pharmacokinetic model of piperaquine in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum malaria in Sudan.
Adam, I; Ashton, M; Day, NP; Hanpithakpong, W; Hoglund, RM; Lindegardh, N; Nosten, F; Tarning, J; White, NJ, 2012
)
0.89
"The population pharmacokinetic properties of piperaquine were well described by a three-compartment disposition model in pregnant and non-pregnant women with uncomplicated malaria."( A population pharmacokinetic model of piperaquine in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum malaria in Sudan.
Adam, I; Ashton, M; Day, NP; Hanpithakpong, W; Hoglund, RM; Lindegardh, N; Nosten, F; Tarning, J; White, NJ, 2012
)
0.91
" Inter- and intra-individual variabilities in the pharmacokinetic parameters were assessed and the contribution of demographic and other covariates was quantified using a nonlinear mixed-effects modelling approach (NONMEM®)."( Population pharmacokinetics of mefloquine, piperaquine and artemether-lumefantrine in Cambodian and Tanzanian malaria patients.
Ariey, F; Beck, HP; Buclin, T; Csajka, C; Decosterd, LA; Duong, S; Genton, B; Guidi, M; Kabanywanyi, AM; Mercier, T; Olliaro, P; Staehli Hodel, EM; Zanolari, B, 2013
)
0.65
" From all the covariates tested, only body weight (for all antimalarials) and concomitant treatment (for artemether only) showed a significant influence on these drugs' pharmacokinetic profiles."( Population pharmacokinetics of mefloquine, piperaquine and artemether-lumefantrine in Cambodian and Tanzanian malaria patients.
Ariey, F; Beck, HP; Buclin, T; Csajka, C; Decosterd, LA; Duong, S; Genton, B; Guidi, M; Kabanywanyi, AM; Mercier, T; Olliaro, P; Staehli Hodel, EM; Zanolari, B, 2013
)
0.65
" Compartmental pharmacokinetic models for PQ and DHA were developed using a population-based approach."( Effect of coadministered fat on the tolerability, safety, and pharmacokinetic properties of dihydroartemisinin-piperaquine in Papua New Guinean children with uncomplicated malaria.
Batty, KT; Benjamin, JM; Davis, TM; Ginny, E; Griffin, S; Moore, BR; Mueller, I; Page-Sharp, M; Robinson, LJ; Salman, S; Siba, P, 2014
)
0.61
" Pharmacokinetic assessment was done with a noncompartmental approach."( Open-label crossover study of primaquine and dihydroartemisinin-piperaquine pharmacokinetics in healthy adult thai subjects.
Ashley, EA; Chotsiri, P; Day, NP; Hanboonkunupakarn, B; Hanpithakpong, W; Jittamala, P; Lee, SJ; Panapipat, S; Pukrittayakamee, S; Tarning, J; Wattanakul, T; White, NJ, 2014
)
0.64
" The polymorphic effects of UGT1A9 (I399C>T) and UGT2B7*2 (802C>T), the major enzymes involved in the metabolism of DHA, on the pharmacokinetic profiles of DHA and its metabolite was also studied."( The effect of UGTs polymorphism on the auto-induction phase II metabolism-mediated pharmacokinetics of dihydroartemisinin in healthy Chinese subjects after oral administration of a fixed combination of dihydroartemisinin-piperaquine.
Li, X; Liu, H; Xing, J; Yang, A; Zang, M; Zhao, L; Zhu, F, 2014
)
0.59
" No polymorphic effect was found for UGT1A9 (I399C>T) and UGT2B7*2 (802C>T) on the pharmacokinetic profiles of DHA and its metabolite DHA-Glu."( The effect of UGTs polymorphism on the auto-induction phase II metabolism-mediated pharmacokinetics of dihydroartemisinin in healthy Chinese subjects after oral administration of a fixed combination of dihydroartemisinin-piperaquine.
Li, X; Liu, H; Xing, J; Yang, A; Zang, M; Zhao, L; Zhu, F, 2014
)
0.59
" Compartmental pharmacokinetic models were developed using a population-based approach."( Population pharmacokinetics, tolerability, and safety of dihydroartemisinin-piperaquine and sulfadoxine-pyrimethamine-piperaquine in pregnant and nonpregnant Papua New Guinean women.
Batty, KT; Benjamin, JM; Davis, TM; Lorry, L; Moore, BR; Mueller, I; Page-Sharp, M; Robinson, LJ; Salman, S; Siba, PM; Tawat, S; Yadi, G, 2015
)
0.65
"Piperaquine-dihydroartemisinin combination therapy has established efficacy for the treatment of malaria; however, a more comprehensive understanding of the pharmacokinetic properties and factors contributing to inter- and intra-individual variability is critical to optimize clinical use."( Effect of food on the pharmacokinetics of piperaquine and dihydroartemisinin.
Bacchieri, A; Evans, AM; Francis, B; Lungershausen, Y; Pace, S; Reuter, SE; Shakib, S; Ubben, D; Valentini, G, 2015
)
2.12
" Blood samples were collected for analysis of plasma piperaquine and dihydroartemisinin concentrations, which were utilized for calculation of pharmacokinetic parameters, using a standard model-independent approach."( Effect of food on the pharmacokinetics of piperaquine and dihydroartemisinin.
Bacchieri, A; Evans, AM; Francis, B; Lungershausen, Y; Pace, S; Reuter, SE; Shakib, S; Ubben, D; Valentini, G, 2015
)
0.93
"The pharmacokinetic compatibility of short-acting CDRI candidate antimalarial trioxane derivative, 99-411, was tested with long-acting prescription antimalarials, lumefantrine and piperaquine."( Assessment of pharmacokinetic compatibility of short acting CDRI candidate trioxane derivative, 99-411, with long acting prescription antimalarials, lumefantrine and piperaquine.
Raju, KS; Singh, SP; Taneja, I; Wahajuddin, M, 2015
)
0.8
" Pharmacokinetic analysis was by population-based compartmental models."( Safety, tolerability and pharmacokinetic properties of coadministered azithromycin and piperaquine in pregnant Papua New Guinean women.
Auyeung, SO; Batty, KT; Benjamin, JM; Davis, TM; Griffin, S; Moore, BR; Mueller, I; Page-Sharp, M; Rogerson, SJ; Salman, S; Siba, PM; Yadi, G, 2016
)
0.66
"Median parasite clearance half-life was prolonged, and clearance half-life was greater than 5 h in 21% of patients."( Parasite clearance rates in Upper Myanmar indicate a distinctive artemisinin resistance phenotype: a therapeutic efficacy study.
Ashley, EA; Aung, SS; Day, NP; Dhorda, M; Dondorp, AM; Hlaing, TM; Imwong, M; Jeeyapant, A; Promnarate, C; Smithuis, FM; Thein, M; Tun, KM; White, NJ; Woodrow, CJ; Yuentrakul, P, 2016
)
0.43
" The pharmacokinetic parameters of tafenoquine, piperaquine, lumefantrine, artemether, and dihydroartemisinin were determined by using noncompartmental methods."( Pharmacokinetic Interactions between Tafenoquine and Dihydroartemisinin-Piperaquine or Artemether-Lumefantrine in Healthy Adult Subjects.
Bouhired, S; Duparc, S; Goyal, N; Green, JA; Hussaini, A; Jones, SW; Koh, GC; Kostov, I; Mohamed, K; Taylor, M; Wolstenholm, A, 2016
)
0.92
" This study utilised a population-based pharmacokinetic approach to optimise the antimalarial treatment regimen for piperaquine."( Population Pharmacokinetic Properties of Piperaquine in Falciparum Malaria: An Individual Participant Data Meta-Analysis.
Ashley, EA; Barnes, KI; Borrmann, S; Dahal, P; Day, NP; Edstein, MD; Guerin, PJ; Hoglund, RM; Lwin, KM; McGready, R; Mwai, L; Nosten, F; Nsanzabana, C; Ouedraogo, JB; Parikh, S; Phyo, AP; Price, RN; Quang, NN; Sambol, NC; Tarning, J; Thanh, NX; White, NJ; Workman, L; Zongo, I, 2017
)
0.93
"Published pharmacokinetic studies on piperaquine were identified through a systematic literature review of articles published between 1 January 1960 and 15 February 2013."( Population Pharmacokinetic Properties of Piperaquine in Falciparum Malaria: An Individual Participant Data Meta-Analysis.
Ashley, EA; Barnes, KI; Borrmann, S; Dahal, P; Day, NP; Edstein, MD; Guerin, PJ; Hoglund, RM; Lwin, KM; McGready, R; Mwai, L; Nosten, F; Nsanzabana, C; Ouedraogo, JB; Parikh, S; Phyo, AP; Price, RN; Quang, NN; Sambol, NC; Tarning, J; Thanh, NX; White, NJ; Workman, L; Zongo, I, 2017
)
0.99
"The derived population pharmacokinetic model was used to develop a revised dose regimen of dihydroartemisinin-piperaquine that is expected to provide equivalent piperaquine exposures safely in all patients, including in small children with malaria."( Population Pharmacokinetic Properties of Piperaquine in Falciparum Malaria: An Individual Participant Data Meta-Analysis.
Ashley, EA; Barnes, KI; Borrmann, S; Dahal, P; Day, NP; Edstein, MD; Guerin, PJ; Hoglund, RM; Lwin, KM; McGready, R; Mwai, L; Nosten, F; Nsanzabana, C; Ouedraogo, JB; Parikh, S; Phyo, AP; Price, RN; Quang, NN; Sambol, NC; Tarning, J; Thanh, NX; White, NJ; Workman, L; Zongo, I, 2017
)
0.93
" A population pharmacokinetic model was developed to compare exposure-response relationships between the 2DP and 3DP regimens while accounting for differences in regimen and sample collection times between studies."( Piperaquine Population Pharmacokinetics and Cardiac Safety in Cambodia.
Buathong, N; Cantilena, L; Chann, S; Haigney, M; Ittiverakul, M; Kodchakorn, C; Kuntawunginn, W; Lanteri, C; Lon, C; Manning, J; Milner, E; Pann, ST; Prom, S; Saunders, D; So, M; Sok, S; Spring, M; Sriwichai, S; Ta-Aksorn, W; Vanachayangkul, P; Wojnarski, M; Youdaline, T, 2017
)
1.9
"The aims of the present study were to evaluate the pharmacokinetic properties of dihydroartemisinin (DHA) and piperaquine, potential drug-drug interactions with concomitant primaquine treatment, and piperaquine effects on the electrocardiogram in healthy volunteers."( Population pharmacokinetics and electrocardiographic effects of dihydroartemisinin-piperaquine in healthy volunteers.
Blessborn, D; Chotsiri, P; Day, NPJ; Hanboonkunupakarn, B; Hoglund, RM; Jittamala, P; Pukrittayakamee, S; Tarning, J; Wattanakul, T; White, NJ, 2017
)
0.89
"The population pharmacokinetic properties of DHA and piperaquine were assessed in 16 healthy Thai adults using an open-label, randomized, crossover study."( Population pharmacokinetics and electrocardiographic effects of dihydroartemisinin-piperaquine in healthy volunteers.
Blessborn, D; Chotsiri, P; Day, NPJ; Hanboonkunupakarn, B; Hoglund, RM; Jittamala, P; Pukrittayakamee, S; Tarning, J; Wattanakul, T; White, NJ, 2017
)
0.93
" Concomitant treatment with primaquine did not affect the pharmacokinetic properties of DHA or piperaquine."( Population pharmacokinetics and electrocardiographic effects of dihydroartemisinin-piperaquine in healthy volunteers.
Blessborn, D; Chotsiri, P; Day, NPJ; Hanboonkunupakarn, B; Hoglund, RM; Jittamala, P; Pukrittayakamee, S; Tarning, J; Wattanakul, T; White, NJ, 2017
)
0.9
"1% and was clearly associated with parasite clearance half-life (PCt1/2)."( A randomised, double-blind clinical phase II trial of the efficacy, safety, tolerability and pharmacokinetics of a single dose combination treatment with artefenomel and piperaquine in adults and children with uncomplicated Plasmodium falciparum malaria.
Adamy, M; Adoke, Y; Bassat, Q; Biguenet, S; Bouyou-Akotet, M; Demarest, H; Duong, TT; Duparc, S; Foster, C; Issifou, S; Kibuuka, A; Kremsner, PG; Laurijssens, BE; Leipoldt, I; Leroy, D; Macintyre, F; Mombo-Ngoma, G; Ouedraogo, A; Phuc, BQ; Ramharter, M; Smith, M; Tinto, H; Tiono, AB; Tshefu, AK, 2017
)
0.65
" Based on in vitro data, a two-way pharmacokinetic interaction was hypothesized for KAF156 use in combination with piperaquine (PPQ) as both drugs are CYP3A4 substrates and inhibitors."( A phase 1 evaluation of the pharmacokinetic/pharmacodynamic interaction of the anti-malarial agents KAF156 and piperaquine.
Feng, Y; Goswami, B; Jain, JP; Leong, FJ; Stein, DS, 2018
)
0.9
" Routine safety and pharmacokinetic assessments were carried out up to 61 days."( A phase 1 evaluation of the pharmacokinetic/pharmacodynamic interaction of the anti-malarial agents KAF156 and piperaquine.
Feng, Y; Goswami, B; Jain, JP; Leong, FJ; Stein, DS, 2018
)
0.69
" Co-administration of PPQ and KAF156 had no overall effect on AUC of either compound, but the Cmax values of both KAF156 (~ 23%) and piperaquine (~ 70%) increased."( A phase 1 evaluation of the pharmacokinetic/pharmacodynamic interaction of the anti-malarial agents KAF156 and piperaquine.
Feng, Y; Goswami, B; Jain, JP; Leong, FJ; Stein, DS, 2018
)
0.9
"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

Compound-Compound Interactions

Study investigated safety and pharmacokinetics of KAE609 in combination with the long-acting antimalarial piperaquine (PPQ)

ExcerptReferenceRelevance
" Competitive uptake of radiolabeled chloroquine and dihydroartemisinin in combination with other antimalarials was observed."( Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
Adagu, IS; Fivelman, QL; Warhurst, DC, 2007
)
0.73
"A high prevalence of chloroquine-resistant Plasmodium vivax in Indonesia has shifted first-line treatment to artemisinin-based combination therapies, combined with primaquine (PQ) for radical cure."( A randomized comparison of dihydroartemisinin-piperaquine and artesunate-amodiaquine combined with primaquine for radical treatment of vivax malaria in Sumatera, Indonesia.
Chavez, I; Chokejindachai, W; Dondorp, AM; Imwong, M; Pasaribu, AP; Pasaribu, S; Sirivichayakul, C; Tanomsing, N; Tjitra, E; White, NJ, 2013
)
0.65
" This study investigated the safety and pharmacokinetics of KAE609 in combination with the long-acting antimalarial piperaquine (PPQ) in healthy volunteers."( Open-label, single-dose, parallel-group study in healthy volunteers to determine the drug-drug interaction potential between KAE609 (cipargamin) and piperaquine.
Griffin, P; Jain, JP; Kangas, M; Lefèvre, G; Lickliter, J; Machineni, S; Stein, DS, 2015
)
0.83
" This study demonstrated that LC-HRMS(n) in combination with multiple data-mining techniques in tandem can be a valuable analytical strategy for rapid metabolite profiling of drugs."( Metabolite identification of the antimalarial piperaquine in vivo using liquid chromatography-high-resolution mass spectrometry in combination with multiple data-mining tools in tandem.
Fan, P; Liu, H; Xing, J; Yang, A; Zang, M, 2016
)
0.69
"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
)
0.66
" 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
" Furthermore, doxycycline has anti-malarial properties and is already recommended as prophylaxis for travellers and for treatment of falciparum malaria in combination with other anti-malarial drugs."( Has doxycycline, in combination with anti-malarial drugs, a role to play in intermittent preventive treatment of Plasmodium falciparum malaria infection in pregnant women in Africa?
Boxberger, M; Gaillard, T; Madamet, M; Pradines, B, 2018
)
0.48
" We aimed to establish the efficacy and safety of three single low doses of tafenoquine in combination with dihydroartemisinin-piperaquine for reducing gametocyte density and transmission to mosquitoes."( Single low-dose tafenoquine combined with dihydroartemisinin-piperaquine to reduce Plasmodium falciparum transmission in Ouelessebougou, Mali: a phase 2, single-blind, randomised clinical trial.
Attaher, O; Bousema, T; Bradley, J; Diallo, M; Dicko, A; Dicko, OM; Drakeley, C; Issiaka, D; Keita, S; Lanke, K; Maguiraga, SO; Mahamar, A; McCall, MBB; Niambele, SM; Sacko, A; Samake, S; Sanogo, K; Sinaba, Y; Smit, MJ; Stone, W; Ter Heine, R; Traore, SF, 2022
)
1.17
" This study evaluated the efficacy of different dosages of aqueous extract of Strychnos ligustrina combined with dihydroartemisinin and piperaquine phosphate (DHP) against murine Plasmodium berghei infection."( Antimalarial Efficacy of Aqueous Extract of Strychnos ligustrina and Its Combination with Dihydroartemisinin and Piperaquine Phosphate (DHP) against Plasmodium berghei Infection.
Cahyaningsih, U; Maring, AJ; Nugraha, AB; Sa'diah, S; Sari, RK; Syafii, W, 2022
)
1.14

Bioavailability

Piperaquine was best described by a three-compartment disposition model with a 45% higher elimination clearance and a 47% increase in relative bioavailability in pregnant women compared with nonpregnant women. Piperaquine AUC was proportional to the two doses tested and a moderate-fat meal enhanced the bioavailability of piper Aquine by 41%.

ExcerptReferenceRelevance
" The oral bioavailability of PQ relative to the fasting state was 121% greater after the high-fat meal (95% confidence interval, 26 to 216% increase; P=0."( Effects of a high-fat meal on the relative oral bioavailability of piperaquine.
Davis, TM; Ilett, KF; Sim, IK, 2005
)
0.56
" The absolute oral bioavailability was approximately 50%."( Pharmacokinetics and metabolism of the antimalarial piperaquine after intravenous and oral single doses to the rat.
Ashton, M; Day, NJ; Lindegardh, N; Sandberg, S; Tarning, J; White, NJ, 2008
)
0.6
" Piperaquine AUC was proportional to the two doses tested and a moderate-fat meal enhanced the bioavailability of piperaquine by 41%, which should improve the therapeutic efficacy of this drug."( Pharmacokinetics of the antimalarial drug piperaquine in healthy Vietnamese subjects.
Bui, D; Edstein, MD; Nguyen, NQ; Nguyen, TC; Nguyen, XT; Travers, T, 2008
)
1.52
" In addition, the oral bioavailability of piperaquine improves when given with a high-fat meal, though this does not necessarily translate into a higher efficacy."( Progress in the development of piperaquine combinations for the treatment of malaria.
D'alessandro, U, 2009
)
0.9
" The lipophilic characteristic of piperaquine suggests that administration together with fat will increase the oral bioavailability of the drug, and this has been reported for healthy volunteers."( A small amount of fat does not affect piperaquine exposure in patients with malaria.
Annerberg, A; Ashley, E; Day, NP; Khrutsawadchai, S; Lindegardh, N; Lwin, KM; Nosten, F; Singhasivanon, P; Tarning, J; White, NJ, 2011
)
0.92
" Piperaquine was best described by a three-compartment disposition model with a 45% higher elimination clearance and a 47% increase in relative bioavailability in pregnant women compared with nonpregnant women."( Population pharmacokinetics of dihydroartemisinin and piperaquine in pregnant and nonpregnant women with uncomplicated malaria.
Day, NP; Hanpithakpong, W; Lindegardh, N; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Tarning, J; White, NJ, 2012
)
1.54
"Previously published literature reports various impacts of food on the oral bioavailability of piperaquine."( Population pharmacokinetic assessment of the effect of food on piperaquine bioavailability in patients with uncomplicated malaria.
Annerberg, A; Ashley, E; Day, NP; Kiricharoen, L; Lindegardh, N; Lwin, KM; Nosten, F; Tarning, J; White, NJ, 2014
)
0.86
" Based on these results, the alternative common three-day regimen for QHS-PQ could probably lead to lower bioavailability of QHS and higher potential of drug-drug interaction caused by the induction of drug-metabolizing enzymes."( Auto-induction of phase I and phase II metabolism of artemisinin in healthy Chinese subjects after oral administration of a new artemisinin-piperaquine fixed combination.
Li, X; Xing, J; Yang, A; Zang, M; Zhu, F, 2014
)
0.6
"Coadministration of dihydroartemisinin-piperaquine (DHA-PQ) with fat may improve bioavailability and antimalarial efficacy, but it might also increase toxicity."( Effect of coadministered fat on the tolerability, safety, and pharmacokinetic properties of dihydroartemisinin-piperaquine in Papua New Guinean children with uncomplicated malaria.
Batty, KT; Benjamin, JM; Davis, TM; Ginny, E; Griffin, S; Moore, BR; Mueller, I; Page-Sharp, M; Robinson, LJ; Salman, S; Siba, P, 2014
)
0.88
" The metabolic capability could recover after a 12-h dosing interval, which suggested that the alternative common three-day regimen (once daily) for DHA-PQ could probably lead to higher bioavailability of DHA."( The effect of UGTs polymorphism on the auto-induction phase II metabolism-mediated pharmacokinetics of dihydroartemisinin in healthy Chinese subjects after oral administration of a fixed combination of dihydroartemisinin-piperaquine.
Li, X; Liu, H; Xing, J; Yang, A; Zang, M; Zhao, L; Zhu, F, 2014
)
0.59
"001) in association with a greater clearance relative to bioavailability (73."( Population pharmacokinetics, tolerability, and safety of dihydroartemisinin-piperaquine and sulfadoxine-pyrimethamine-piperaquine in pregnant and nonpregnant Papua New Guinean women.
Batty, KT; Benjamin, JM; Davis, TM; Lorry, L; Moore, BR; Mueller, I; Page-Sharp, M; Robinson, LJ; Salman, S; Siba, PM; Tawat, S; Yadi, G, 2015
)
0.65
" This likely reflects an increase in the oral bioavailability of the drug, directly related to the fat content of the meal."( Effect of food on the pharmacokinetics of piperaquine and dihydroartemisinin.
Bacchieri, A; Evans, AM; Francis, B; Lungershausen, Y; Pace, S; Reuter, SE; Shakib, S; Ubben, D; Valentini, G, 2015
)
0.68
" Compared with previous pregnancy studies, the area under the concentration-time curve (AUC0-∞ ) for PQ [38818 (24354-52299) μg h l(-1) ] was similar to published values but there was a 52% increase in relative bioavailability with each dose."( Safety, tolerability and pharmacokinetic properties of coadministered azithromycin and piperaquine in pregnant Papua New Guinean women.
Auyeung, SO; Batty, KT; Benjamin, JM; Davis, TM; Griffin, S; Moore, BR; Mueller, I; Page-Sharp, M; Rogerson, SJ; Salman, S; Siba, PM; Yadi, G, 2016
)
0.66
" Based on the present/other data, total AZI doses higher than 3 g for the treatment and prevention of malaria may be unnecessary in pregnant women, while clearance of parasitaemia could improve the relative bioavailability of PQ."( Safety, tolerability and pharmacokinetic properties of coadministered azithromycin and piperaquine in pregnant Papua New Guinean women.
Auyeung, SO; Batty, KT; Benjamin, JM; Davis, TM; Griffin, S; Moore, BR; Mueller, I; Page-Sharp, M; Rogerson, SJ; Salman, S; Siba, PM; Yadi, G, 2016
)
0.66
"5%) in piperaquine bioavailability between each piperaquine dose occasion."( Population Pharmacokinetic Properties of Piperaquine in Falciparum Malaria: An Individual Participant Data Meta-Analysis.
Ashley, EA; Barnes, KI; Borrmann, S; Dahal, P; Day, NP; Edstein, MD; Guerin, PJ; Hoglund, RM; Lwin, KM; McGready, R; Mwai, L; Nosten, F; Nsanzabana, C; Ouedraogo, JB; Parikh, S; Phyo, AP; Price, RN; Quang, NN; Sambol, NC; Tarning, J; Thanh, NX; White, NJ; Workman, L; Zongo, I, 2017
)
1.18
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" They also showed exceptionally better treatment of malaria owing to their sustained release properties and improved bioavailability and are recommended to Pharmaceutical companies for further studies."( Assessment of the Anti-Malarial Properties of Dihydroartemisinin- Piperaquine Phosphate Solid Lipid-Based Tablets.
Amarachi, CS; Attama, AA; Onunkwo, GC, 2022
)
0.96

Dosage Studied

A three-day course of total 8 tablets compound dihydroartemisinin-piperaquine was administered to an adult. Children tend to have a smaller central volume of distribution, a shorter distribution half-life and a more rapid fall in early piperaquined plasma concentrations.

ExcerptRelevanceReference
" The total dosage recommended was 2800-3200 mg."( [Comparative study of artemisinin suppositories and piperaquine phosphate in the treatment of falciparum malaria].
Fu, LC; Guo, XB, 1989
)
0.53
"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
)
0.56
" The dosing regimen has been simplified from four doses to once daily over 3 days."( Efficacy and safety of dihydroartemisinin-piperaquine.
Ashley, EA; Day, NP; Myint, HY; Nosten, F; White, NJ, 2007
)
0.6
"The population pharmacokinetics of piperaquine in adults and children with uncomplicated Plasmodium falciparum malaria treated with two different dosage regimens of dihydroartemisinin-piperaquine were characterized."( Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
Ashley, EA; Ashton, M; Day, NP; Lindegardh, N; McGready, R; Nosten, F; Phaiphun, L; Stepniewska, K; Tarning, J; White, NJ, 2008
)
0.91
" However, AL has several limitations, including a twice-daily dosing regimen, recommendation for administration with fatty food, and a high risk of reinfection soon after therapy in high transmission areas."( Artemether-lumefantrine versus dihydroartemisinin-piperaquine for treating uncomplicated malaria: a randomized trial to guide policy in Uganda.
Bukirwa, H; Dorsey, G; Kamya, MR; Lugemwa, M; Rosenthal, PJ; Rwakimari, JB; Staedke, SG; Talisuna, A; Wabwire-Mangen, F; Yeka, A, 2008
)
0.6
"DP is highly efficacious, and operationally preferable to AL because of a less intensive dosing schedule and requirements."( Artemether-lumefantrine versus dihydroartemisinin-piperaquine for treating uncomplicated malaria: a randomized trial to guide policy in Uganda.
Bukirwa, H; Dorsey, G; Kamya, MR; Lugemwa, M; Rosenthal, PJ; Rwakimari, JB; Staedke, SG; Talisuna, A; Wabwire-Mangen, F; Yeka, A, 2008
)
0.6
" However, children, compared to the population mean profile, tend to have a smaller central volume of distribution, a shorter distribution half-life and a more rapid fall in early piperaquine plasma concentrations, suggesting that an increase of the weight-adjusted dosage in children may be required."( Progress in the development of piperaquine combinations for the treatment of malaria.
D'alessandro, U, 2009
)
0.83
"The dosage recommended for children may need to be reviewed and the usefulness of the coadministration with food should be determined."( Progress in the development of piperaquine combinations for the treatment of malaria.
D'alessandro, U, 2009
)
0.64
" falciparum malaria in central Sudan, although treatment with DHA-P (which requires a simpler dosing regimen) might be preferred to treatment with AL."( Dihydroartemisinin-piperaquine versus artemether-lumefantrine, in the treatment of uncomplicated Plasmodium falciparum malaria in central Sudan.
Adam, I; Elhassan, AH; Elmardi, KA; Eltahir, HG; Malik, EM; Salah, MT, 2010
)
0.69
" A three-day course of total 8 tablets compound dihydroartemisinin-piperaquine was administered to an adult (each tablet containing 40 mg of dihydroartemisinin and 320 mg of piperaquine phosphate), dosage for children was based on ages (details in the treatment regimen) ."( [Efficacy of compound dihydroartemisinin/piperaquine in treatment of uncomplicated falciparum malaria in Myanmar].
Li, CF; Liu, H; Nie, RH; Wang, HY; Yang, HL; Zhang, J, 2011
)
0.87
"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
" PQP at the dose of 80 mg/kg, induced prolonged gestation, dystocic delivery and increase perinatal mortality both with interruption of treatment (GD6 to GD17 and LD1-21) and with continuous dosing (GD19-LD21)."( Piperaquine phosphate: reproduction studies.
Brughera, M; Ferraris, L; Longo, M; Mazuè, G; Messina, M; Pace, S; Ubben, D, 2012
)
1.82
" The better safety profile of DP and once-daily dosage improves adherence and its fixed co-formulation ensures that both drugs are taken together."( Efficacy and safety of dihydroartemisinin-piperaquine for treatment of uncomplicated Plasmodium falciparum malaria in endemic countries: meta-analysis of randomised controlled studies.
Aung, K; Mak, JW; Naing, C; Wong, JY, 2013
)
0.65
" Dosing on body weight appears justified."( Population pharmacokinetics of mefloquine, piperaquine and artemether-lumefantrine in Cambodian and Tanzanian malaria patients.
Ariey, F; Beck, HP; Buclin, T; Csajka, C; Decosterd, LA; Duong, S; Genton, B; Guidi, M; Kabanywanyi, AM; Mercier, T; Olliaro, P; Staehli Hodel, EM; Zanolari, B, 2013
)
0.65
"Dihydroartemisinin-piperaquine (DP) is increasingly recommended for antimalarial treatment in many endemic countries; however, concerns have been raised over its potential under dosing in young children."( The effect of dosing regimens on the antimalarial efficacy of dihydroartemisinin-piperaquine: a pooled analysis of individual patient data.
, 2013
)
0.94
" The better safety profile of DHP and the once-daily dosage improves adherence, and its fixed co-formulation ensures that both drugs (dihydroartemisinin and piperaquine) are taken together."( Efficacy and safety of dihydroartemisinin-piperaquine for treatment of Plasmodium vivax malaria in endemic countries: meta-analysis of randomized controlled studies.
Aung, K; Mak, JW; Naing, C; Racloz, V; Reid, SA; Tanner, M; Whittaker, MA, 2013
)
0.85
" The dosing schedule is simpler with the artenimol + piperaquine combination than with artemether + lumefantrine."( Artenimol + piperaquine. Very slow piperaquine elimination: cardiovascular risks and interactions.
, 2014
)
1.03
" However, the optimal drug and dosing regimens for IPT remain to be determined."( Impact of intermittent preventive treatment with dihydroartemisinin-piperaquine on malaria in Ugandan schoolchildren: a randomized, placebo-controlled trial.
Amuge, P; Brooker, SJ; Dorsey, G; Kamya, MR; Kiwanuka, N; Nankabirwa, JI; Rosenthal, PJ; Staedke, SG; Wandera, B, 2014
)
0.64
" The development of appropriate pragmatic dosing regimens for low-resource settings or community-based use is not formally regulated, even though these may alter factors which can substantially affect individual patient and population level outcome, such as drug exposure, patient adherence and the spread of drug resistance and can affect a drug's reputation and its eventual therapeutic lifespan."( Optimizing the programmatic deployment of the anti-malarials artemether-lumefantrine and dihydroartemisinin-piperaquine using pharmacological modelling.
Hastings, IM; Hayes, DJ; Hodel, EM; Kay, K; Terlouw, DJ, 2014
)
0.62
"An in silico pharmacological model of anti-malarial drug treatment with the pharmacokinetic/pharmacodynamic profiles of artemether-lumefantrine (AM-LF, Coartem®) and dihydroartemisinin-piperaquine (DHA-PPQ, Eurartesim®) was constructed to assess the potential impact of programmatic factors, including regionally optimized, age-based dosing regimens, poor patient adherence, food effects and drug resistance on treatment outcome at population level, and compared both drugs' susceptibility to these factors."( Optimizing the programmatic deployment of the anti-malarials artemether-lumefantrine and dihydroartemisinin-piperaquine using pharmacological modelling.
Hastings, IM; Hayes, DJ; Hodel, EM; Kay, K; Terlouw, DJ, 2014
)
0.81
"Compared with DHA-PPQ, therapeutic effectiveness of AM-LF seems more robust to factors affecting drug exposure, such as age- instead of weight-based dosing or poor adherence."( Optimizing the programmatic deployment of the anti-malarials artemether-lumefantrine and dihydroartemisinin-piperaquine using pharmacological modelling.
Hastings, IM; Hayes, DJ; Hodel, EM; Kay, K; Terlouw, DJ, 2014
)
0.62
"This study has developed mechanistic models that describe the parasite-time curve after single, multiple or combination dosing of antimalarials to mice."( Predicting the parasite killing effect of artemisinin combination therapy in a murine malaria model.
Batty, KT; Gibbons, PL; Kirkpatrick, CM; Moore, BR; Patel, K, 2014
)
0.4
" The cases were given a 2-day course with DHAPIP tablets each containing 40 mg of dihydroartemisinin and 320 mg of piperaquine phosphate, and the total dosage varied with the body weight."( [Therapeutic efficacy and safety of compound dihydroartemisinin/piperaquine for uncomplicated Plasmodium falciparum infection in Laiza City of Myanmar bordering on China].
Deng, Y; Lasi, JH; Sun, XD; Sun, XY; Wang, H; Wang, J; Yang, YC; Zhang, ZX, 2011
)
0.82
" The safety and efficacy of a monthly 2-day dosing regimen of dihydroartemisinin-piperaquine were evaluated in a two-arm, randomized, double-blind, placebo-controlled cohort study with 2:1 treatment allocation."( Randomized, double-blind, placebo-controlled clinical trial of a two-day regimen of dihydroartemisinin-piperaquine for malaria prevention halted for concern over prolonged corrected QT interval.
Auayporn, M; Buathong, N; Cantilena, L; Chann, S; Chour, CM; Haigney, M; Kaewkungwal, J; Kuntawunginn, W; Lanteri, C; Lon, C; Manning, J; Mitprasat, M; Phann, ST; Prom, S; Saunders, D; Se, Y; Sea, D; Siripokasupkul, R; So, M; Soh, E; Somethy, S; Spring, M; Sriwichai, S; Tang, D; Teja-Isavadharm, P; Timmermans, A; Vanachayangkul, P, 2014
)
0.84
" However, the optimal chemoprevention drug and dosing strategy is unclear in areas of year-round transmission and resistance to many antimalarial drugs."( Protective efficacy and safety of three antimalarial regimens for the prevention of malaria in young Ugandan children: a randomized controlled trial.
Achan, J; Aweeka, FT; Bigira, V; Clark, TD; Dorsey, G; Havlir, DV; Huang, L; Kamya, MR; Kapisi, J; Kinara, S; Muhindo, MK; Mwangwa, F; Osterbauer, B; Rosenthal, PJ, 2014
)
0.4
" This result relies on the assumption that compliance to treatment with DhP is higher than that with AL due to its relatively simple once-a-day dosage regimen."( Cost-effectiveness of dihydroartemisinin-piperaquine compared with artemether-lumefantrine for treating uncomplicated malaria in children at a district hospital in Tanzania.
Mori, AT; Ngalesoni, F; Norheim, OF; Robberstad, B, 2014
)
0.67
" Simulations of monthly dosing, based on the final model and published pharmacokinetic data, suggested that the incidence of malaria infections over 1 year could be reduced by 70% with a recently suggested dosing regimen compared to the current manufacturer's recommendations for small children (8 to 12 kg)."( Characterization of an in vivo concentration-effect relationship for piperaquine in malaria chemoprevention.
Bergstrand, M; Karlsson, MO; Lwin, KM; Nosten, F; Tarning, J; White, NJ, 2014
)
0.64
" Due to auto-induction metabolism, declining plasma concentrations after the repeated dosing have been reported for artemisinin (Qing-hao-su) and artemether."( The effect of UGTs polymorphism on the auto-induction phase II metabolism-mediated pharmacokinetics of dihydroartemisinin in healthy Chinese subjects after oral administration of a fixed combination of dihydroartemisinin-piperaquine.
Li, X; Liu, H; Xing, J; Yang, A; Zang, M; Zhao, L; Zhu, F, 2014
)
0.59
" The metabolic capability could recover after a 12-h dosing interval, which suggested that the alternative common three-day regimen (once daily) for DHA-PQ could probably lead to higher bioavailability of DHA."( The effect of UGTs polymorphism on the auto-induction phase II metabolism-mediated pharmacokinetics of dihydroartemisinin in healthy Chinese subjects after oral administration of a fixed combination of dihydroartemisinin-piperaquine.
Li, X; Liu, H; Xing, J; Yang, A; Zang, M; Zhao, L; Zhu, F, 2014
)
0.59
"Adherence to anti-malarial dosing schedules is essential to ensure effective treatment."( Perceptions and utilization of the anti-malarials artemether-lumefantrine and dihydroartemisinin-piperaquine in young children in the Chikhwawa District of Malawi: a mixed methods study.
Ewing, VL; Kapinda, A; Lalloo, DG; Pace, C; Richards, E; Terlouw, DJ; Tolhurst, R, 2015
)
0.63
" While the sweet taste of dispersible AL may have reduced conflict between the child and caregiver, sub-optimal dosing due to medication loss remained a problem and overall adherence was greater among those receiving DHA-PPQ, which requires fewer doses."( Perceptions and utilization of the anti-malarials artemether-lumefantrine and dihydroartemisinin-piperaquine in young children in the Chikhwawa District of Malawi: a mixed methods study.
Ewing, VL; Kapinda, A; Lalloo, DG; Pace, C; Richards, E; Terlouw, DJ; Tolhurst, R, 2015
)
0.63
" Current weight-based dosing does not adequately address physiological changes in early childhood."( Population Pharmacokinetics of Piperaquine in Young Ugandan Children Treated With Dihydroartemisinin-Piperaquine for Uncomplicated Malaria.
Arinaitwe, E; Aweeka, FT; Bigira, V; Creek, DJ; Kakuru, A; Lindegardh, N; McCormack, SA; Nosten, F; Parikh, S; Sambol, NC; Tappero, JW; Tarning, J; Wanzira, H; Yan, L, 2015
)
0.7
" Subjects were randomized to four parallel dosing arms with five cohorts (2:2:2:2:1), receiving 75 mg KAE609 plus 320 mg PPQ, 25 mg KAE609 plus 1,280 mg PPQ, 25 mg KAE609 alone, 320 mg PPQ alone, or 1,280 mg PPQ alone."( Open-label, single-dose, parallel-group study in healthy volunteers to determine the drug-drug interaction potential between KAE609 (cipargamin) and piperaquine.
Griffin, P; Jain, JP; Kangas, M; Lefèvre, G; Lickliter, J; Machineni, S; Stein, DS, 2015
)
0.62
" 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
" Children were randomized at 6 months of age to no chemoprevention (n = 89) or monthly DHA/PQ (n = 87) and followed through 24 months of age, with pharmacokinetic sampling performed at variable times following monthly dosing of DHA/PQ."( Variable piperaquine exposure significantly impacts protective efficacy of monthly dihydroartemisinin-piperaquine for the prevention of malaria in Ugandan children.
Aweeka, F; Bigira, V; Dorsey, G; Huang, L; Jagannathan, P; Kakuru, MM; Kamya, MR; Kapisi, J; Savic, R; Sundell, K, 2015
)
0.83
" Strategies to ensure good adherence to monthly dosing and optimize drug exposure are critical to maximize the efficacy of this promising malaria control strategy."( Variable piperaquine exposure significantly impacts protective efficacy of monthly dihydroartemisinin-piperaquine for the prevention of malaria in Ugandan children.
Aweeka, F; Bigira, V; Dorsey, G; Huang, L; Jagannathan, P; Kakuru, MM; Kamya, MR; Kapisi, J; Savic, R; Sundell, K, 2015
)
0.83
" Candidate regimens that were tested included monthly administration of standard therapeutic doses, bimonthly dosing, and weekly dosing (with and without a loading dose)."( Rethinking Dosing Regimen Selection of Piperaquine for Malaria Chemoprevention: A Simulation Study.
Arinaitwe, E; Parikh, S; Sambol, NC; Tappero, JW, 2016
)
0.7
" In contrast, weekly dosing of 320 mg (i."( Rethinking Dosing Regimen Selection of Piperaquine for Malaria Chemoprevention: A Simulation Study.
Arinaitwe, E; Parikh, S; Sambol, NC; Tappero, JW, 2016
)
0.7
" This therapeutic failure with DP by under-dosing highlighted the importance of appropriate dosing guidelines and the need of research data (efficacy, pharmacokinetics and pharmacodynamics) in over-weight patient group."( Failure of dihydroartemisinin plus piperaquine treatment of falciparum malaria by under-dosing in an overweight patient.
Javelle, E; Madamet, M; Paleiron, N; Pradines, B; Roseau, JB; Simon, F; Vedy, S, 2016
)
0.71
" This study explored alternative DHA-PQ adult dosing regimens compared to the monthly adult dosing regimen currently being studied in clinical trials."( Prediction of Improved Antimalarial Chemoprevention with Weekly Dosing of Dihydroartemisinin-Piperaquine.
Bergstrand, M; Karlsson, MO; Nosten, F; Permala, J; Tarning, J; White, NJ, 2017
)
0.67
" This may soon change to recommending artemisinin-based combination therapies (standard duration of dosing = 3 days)."( Animal Embryotoxicity Studies of Key Non-Artemisinin Antimalarials and Use in Women in the First Trimester.
Clark, RL, 2017
)
0.46
"5 mg can make dosing convenient in children."( Assessment of Efficacy and Safety of Arterolane Maleate-Piperaquine Phosphate Dispersible Tablets in Comparison With Artemether-Lumefantrine Dispersible Tablets in Pediatric Patients With Acute Uncomplicated Plasmodium falciparum Malaria: A Phase 3, Rando
Anvikar, AR; Behra, N; Das, RR; Gaye, O; Jalali, RK; Maheshwar, AV; Mishra, P; Mwapasa, V; Nasa, A; Roy, A; Sagara, I; Sharma, P; Sharma, SK; Thompson, R; Toure, OA; Tshefu, AK; Valecha, N, 2017
)
0.7
"For HIV-infected pregnant women receiving efavirenz, low daily DHA-PQ dosing was predicted to improve protection against parasitemia and reduce risk of toxicity compared to monthly dosing."( Predicting Optimal Dihydroartemisinin-Piperaquine Regimens to Prevent Malaria During Pregnancy for Human Immunodeficiency Virus-Infected Women Receiving Efavirenz.
Aweeka, F; Dorsey, G; Havlir, D; Huang, L; Jagannathan, P; Kakuru, A; Kamya, M; Muhindo, M; Nakalembe, M; Natureeba, P; Rosenthal, PJ; Savic, RM; Vucicevic, K; Wallender, E, 2018
)
0.75
" Determining associations between piperaquine (PQ) exposure, malaria risk, and adverse birth outcomes informs optimal dosing strategies."( Intermittent Preventive Treatment for Malaria in Pregnancy: Optimization of Target Concentrations of Dihydroartemisinin-Piperaquine.
Aweeka, FT; Clark, TD; Dorsey, G; Havlir, DV; Huang, L; Jagannathan, P; Kajubi, R; Kakuru, A; Kamya, M; Muhindo, MK; Mwebaza, N; Opira, B; Rosenthal, PJ; Savic, RM; Wallender, E; Were, M; Zhang, N, 2018
)
0.97
" Simulations of new dosing scenarios were performed."( Intermittent Preventive Treatment for Malaria in Pregnancy: Optimization of Target Concentrations of Dihydroartemisinin-Piperaquine.
Aweeka, FT; Clark, TD; Dorsey, G; Havlir, DV; Huang, L; Jagannathan, P; Kajubi, R; Kakuru, A; Kamya, M; Muhindo, MK; Mwebaza, N; Opira, B; Rosenthal, PJ; Savic, RM; Wallender, E; Were, M; Zhang, N, 2018
)
0.69
" Studies of the efficacy and safety of alternative DHA-PQ IPTp dosing strategies are warranted."( Intermittent Preventive Treatment for Malaria in Pregnancy: Optimization of Target Concentrations of Dihydroartemisinin-Piperaquine.
Aweeka, FT; Clark, TD; Dorsey, G; Havlir, DV; Huang, L; Jagannathan, P; Kajubi, R; Kakuru, A; Kamya, M; Muhindo, MK; Mwebaza, N; Opira, B; Rosenthal, PJ; Savic, RM; Wallender, E; Were, M; Zhang, N, 2018
)
0.69
" 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
)
0.74
" Isolates exhibit a bimodal dose-response curve when exposed to PPQ, with the area under the curve quantifying their survival in vitro."( Plasmepsin II-III copy number accounts for bimodal piperaquine resistance among Cambodian Plasmodium falciparum.
Amaratunga, C; Ariey, F; Ashley, EA; Bopp, S; Dhorda, M; Dondorp, AM; Fairhurst, RM; Lim, P; Magistrado, P; Menard, D; Mukherjee, A; Schaffner, SF; Volkman, SK; White, NJ; Wirth, DF; Wong, W; Woodrow, CJ, 2018
)
0.73
" We provide published data supporting the use of a higher dosage regimen of ivermectin in malaria and difficult-to-treat head lice, and announce an ongoing randomized clinical trial in severe scabies."( High-dose ivermectin in malaria and other parasitic diseases: a new step in the development of a neglected drug.
Bernigaud, C; Chosidow, O; Do-Pham, G, 2018
)
0.48
"Nous soulignons l’absence de données probantes de haut niveau sur les études de dosage concernant l’utilisation de l’ivermectine par voie orale dans les maladies parasitaires sensibles."( High-dose ivermectin in malaria and other parasitic diseases: a new step in the development of a neglected drug.
Bernigaud, C; Chosidow, O; Do-Pham, G, 2018
)
0.48
" Future studies are needed to better understand the biological mechanisms of in utero drug exposure on drug metabolism and how this may affect the dosing of antimalarial drugs for treatment and prevention during infancy."( Dihydroartemisinin-piperaquine for intermittent preventive treatment of malaria during pregnancy and risk of malaria in early childhood: A randomized controlled trial.
Aweeka, F; Beeson, J; Charlebois, ED; Clark, TD; Dorsey, G; Drakeley, C; Feeney, ME; Greenhouse, B; Havlir, DV; Jagannathan, P; Kakuru, A; Kamya, MR; Muhindo, MK; Nakalembe, M; Nankya, F; Natureeba, P; Okiring, J; Olwoch, P; Opira, B; Prahl, M; Reiling, L; Rodriguez-Barraquer, I; Ssewanyana, I; Tetteh, K; Wallender, E, 2018
)
0.81
" 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
)
0.97
"Dihydroartemisinin (DHA)-piperaquine is being evaluated as intermittent preventive therapy for malaria, but dosing has not been optimized for children."( Reduced Exposure to Piperaquine, Compared to Adults, in Young Children Receiving Dihydroartemisinin-Piperaquine as Malaria Chemoprevention.
Aweeka, FT; Chamankhah, N; Dorsey, G; Huang, L; Jagannathan, P; Kajubi, R; Kamya, MR; Mwebaza, N; Orukan, F; Rosenthal, PJ; Wallender, E; Whalen, ME, 2019
)
1.14
" However, the optimal dosing strategy is unclear and conflicting evidence exists regarding the risk of malaria after cessation of chemoprevention."( Intermittent preventive treatment with dihydroartemisinin-piperaquine and risk of malaria following cessation in young Ugandan children: a double-blind, randomised, controlled trial.
Charlebois, E; Clark, TD; Dorsey, G; Feeney, ME; Havlir, DV; Jagannathan, P; Kakuru, A; Kamya, MR; Muhindo, MK; Nalugo, N; Okiring, J; Olwoch, P; Opira, B; Ruel, T, 2019
)
0.76
"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
)
2.22
" Nineteen percent of HCPs thought that dihydroartemisinin/piperaquine gave the most satisfactory patient treatment outcomes, while 80% HCPs thought that artemether/lumefantrine gave the least satisfactory patient treatment outcomes, possibly due to dosing schedule and pill burden."( Healthcare professionals' perspective can guide post-marketing surveillance of artemisinin-based combination therapy in Uganda.
D'Hoore, W; Kiguba, R; Kirabira, E; Manirakiza, L; Mukonzo, J; Nabirye, L; Ndagije, HB; Olsson, S; Speybroeck, N; Spinewine, A; Sserwanga, A, 2020
)
0.8
" Participants in the intermittent preventive malaria treatment arm will receive dihydroartemisinin/piperaquine (DP) dosed by weight, 1 month apart, prior to the first immunisation, followed by monthly treatment thereafter."( Effect of intermittent preventive treatment for malaria with dihydroartemisinin-piperaquine on immune responses to vaccines among rural Ugandan adolescents: randomised controlled trial protocol B for the '
Akello, F; Amongi, S; Amongin, R; Cose, S; Elliott, AM; Kabuubi, PN; Kiwanuka, S; Kiwudhu, F; Kizindo, R; Mutebe, A; Nakazibwe, E; Nassuuna, J; Natukunda, A; Nkurunungi, G; Nsubuga, D; Oduru, G; Onen, C; Sewankambo, M; Staedke, SG; Webb, E; Zirimenya, L, 2021
)
1.06
" 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
" Optimal DP dosing regimens will maximize efficacy and reduce toxicity and resistance selection."( Identifying an optimal dihydroartemisinin-piperaquine dosing regimen for malaria prevention in young Ugandan children.
Ali, AM; Aweeka, F; Dorsey, G; Duvalsaint, M; Huang, L; Hughes, E; Jagannathan, P; Kakuru, A; Kamya, MR; Legac, J; Muhindo, MK; Opira, B; Rosenthal, PJ; Savic, RM; Wallender, E; Whalen, M, 2021
)
0.89
" Piperaquine prolongs the corrected QT interval (QTc), and it is possible that repeated monthly dosing could lead to progressive QTc prolongation."( Piperaquine-Induced QTc Prolongation Decreases With Repeated Monthly Dihydroartemisinin-Piperaquine Dosing in Pregnant Ugandan Women.
Aweeka, F; Clark, TD; Dorsey, G; Hughes, E; Jagannathan, P; Kajubi, R; Kakuru, A; Kamya, MR; Ochieng, T; Rosenthal, PJ; Savic, RM; Wallender, E, 2022
)
3.07
"Repeated DHA-PQ dosing did not result in increased risk of QTc prolongation and the postdose QTc intervals progressively decreased."( Piperaquine-Induced QTc Prolongation Decreases With Repeated Monthly Dihydroartemisinin-Piperaquine Dosing in Pregnant Ugandan Women.
Aweeka, F; Clark, TD; Dorsey, G; Hughes, E; Jagannathan, P; Kajubi, R; Kakuru, A; Kamya, MR; Ochieng, T; Rosenthal, PJ; Savic, RM; Wallender, E, 2022
)
2.16
" Drug sensitivity against a panel of antimalarials, the ring-stage survival assay (RSA), the PPQ survival assay (PSA), and bimodal dose-response curves were used to evaluate antimalarial susceptibility."( A single point mutation in the Plasmodium falciparum 3'-5' exonuclease does not alter piperaquine susceptibility.
Boonyalai, N; Griesenbeck, JS; Kirativanich, K; Praditpol, C; Thamnurak, C; Vesely, BA; Waters, NC; Wojnarski, M, 2022
)
0.94
" Participants were randomly assigned (1:1:1:1) to standard treatment with dihydroartemisinin-piperaquine, or dihydroartemisinin-piperaquine plus a single dose of tafenoquine (in solution) at a final dosage of 0·42 mg/kg, 0·83 mg/kg, or 1·66 mg/kg."( Single low-dose tafenoquine combined with dihydroartemisinin-piperaquine to reduce Plasmodium falciparum transmission in Ouelessebougou, Mali: a phase 2, single-blind, randomised clinical trial.
Attaher, O; Bousema, T; Bradley, J; Diallo, M; Dicko, A; Dicko, OM; Drakeley, C; Issiaka, D; Keita, S; Lanke, K; Maguiraga, SO; Mahamar, A; McCall, MBB; Niambele, SM; Sacko, A; Samake, S; Sanogo, K; Sinaba, Y; Smit, MJ; Stone, W; Ter Heine, R; Traore, SF, 2022
)
1.18
" We will also assess toxicity from cumulative DP dosing and the development of resistance."( Dihydroartemisinin-piperaquine or sulphadoxine-pyrimethamine for the chemoprevention of malaria in children with sickle cell anaemia in eastern and southern Africa (CHEMCHA): a protocol for a multi-centre, two-arm, double-blind, randomised, placebo-contro
Akun, P; Galileya, LT; Idro, R; Kalibbala, D; Nambatya, W; Nkosi-Gondwe, T; Opoka, R; Phiri, K; Robberstad, B; Rujumba, J; Ssenkusu, J; TerKuile, F, 2023
)
1.24
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

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

Drug Classes (3)

ClassDescription
N-arylpiperazine
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
aminoquinolineAny member of the class of quinolines in which the quinoline skeleton is substituted by one or more amino or substituted-amino groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 3A4Homo sapiens (human)Ki0.09000.00011.41629.9000AID1579733
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (19)

Processvia Protein(s)Taxonomy
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (277)

Assay IDTitleYearJournalArticle
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID748935Antimalarial activity against multidrug-resistant Plasmodium falciparum W2 infected in ip dosed mouse assessed as reduction in parasitemia administered on day 64 post-infection2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Recent advances in malaria drug discovery.
AID561061Half life in Plasmodium falciparum-infected patient at 320 mg/kg, po2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID547315Antimalarial activity against Plasmodium falciparum2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro activities of quinine and other antimalarials and pfnhe polymorphisms in Plasmodium isolates from Kenya.
AID561064Antiplasmodial activity against Plasmodium falciparum D62009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID428119Terminal half life in human children2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID428115Antiparasitic activity as parasitaemia against Plasmodium berghei ANKA infected Swiss mice (Mus musculus) at 30 mg/kg intraperitoneal dose 64 hrs post infection2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID519196Antimicrobial activity against Plasmodium vivax at the ring stage measured after 30 hrs by microscopy2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Determinants of in vitro drug susceptibility testing of Plasmodium vivax.
AID563112Antimalarial activity against Plasmodium falciparum 3D7 harboring Ppcrt I371R mutant gene and Pfnhe-1 ms4760 microsatellite mutant assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID545363Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum C3 harboring Dd2 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID521748Terminal half-life in healthy human at 25 mg/kg, po after 29 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID521760Apparent oral clearance in human with uncomplicated malaria at 35 mg/kg, perorally after 35 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID545381Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum TM6 infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of dihydroartimisinin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID586608Antimalarial activity against trophozoites stage of Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID423738Apparent clearance with respect to bioavailability in human after fasting using non-compartmental analysis2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID521745Plasma concentration in human with uncomplicated malaria at 31 mg/kg, perorally at day 282008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID576573Antimalarial activity against Plasmodium vivax at the ring stage infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax.
AID1638537Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human RBC assessed as reduction in parasite growth after 35 to 56 hrs by nucleic acid staining based flow cytometry2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
3,3'-Disubstituted 5,5'-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity.
AID423743Volume of distribution at steady state with respect to bioavailability in Vietnamese human2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID423741Absorption half life in Vietnamese human by three-compartmental analysis2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID564300Antimalarial activity against Plasmodium falciparum IMT 10500 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID545384Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum C2 infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of dihydroartimisinin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID323678Reduction of [3H]chloroquine uptake in chloroquine-sensitive Plasmodium falciparum FC27 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID564295Antimalarial activity against Plasmodium falciparum IMT 31 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1649452Ratio of AUC (0 to infinity) in ICR mouse liver to plasma at 80 mg/kg, po administered as single dose2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials.
AID563102Antimalarial activity against Plasmodium falciparum IMT 9881 harboring Ppcrt I371R mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID323683Reduction of [3H]dihydroartemisinin uptake in chloroquine-resistant Plasmodium falciparum K1 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID323682Reduction of [3H]dihydroartemisinin uptake in chloroquine-sensitive Plasmodium falciparum FC27 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID323684Reduction of [3H]dihydroartemisinin uptake in chloroquine-sensitive Plasmodium falciparum 3D7 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID423714Tlag in Paua New Guinean children with uncomplicated malaria at 20 mg/kg daily for 3 days2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID423713Distribution half life in Paua New Guinean children with uncomplicated malaria at 20 mg/kg daily for 3 days2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID564316Antimalarial activity against Plasmodium falciparum IMT A4 harboring Ppcrt M74I, N75E, K76T, A220H, Q271E, N326S and I356T mutant gene, Pmdr1 Y184F, N1042D, D1246Y mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation co2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1593289Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring M133I mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
AID423712Elimination half life in Paua New Guinean children with uncomplicated malaria at 20 mg/kg daily for 3 days2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID545389Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 harboring parental pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of dihydroartimisinin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID564302Antimalarial activity against Plasmodium falciparum IMT K14 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID564313Antimalarial activity against Plasmodium falciparum 106/1 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID521762Terminal half-life in human with uncomplicated malaria at 31 mg/kg, perorally2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID521764Apparent steady-state volume of distribution with respect to bioavailability in human with uncomplicated malaria at 31 mg/kg, perorally2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID428111Plasma concentration in Swiss mice (Mus musculus) infected with Plasmodium berghei ANKA at 90 mg/kg, intraperitoneally administered 64 hrs after infection measured after 30 days2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID521746Plasma concentration in human with uncomplicated malaria at 31 mg/kg, perorally four-dose treatment regimen measured at day 202008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID521755Apparent steady-state volume of distribution with respect to bioavailability in human with uncomplicated malaria at 35 mg/kg, perorally after 35 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID564231Antiplasmodial activity against multidrug-sensitive Plasmodium falciparum 3D7 after 18 hrs by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1.
AID561065Antiplasmodial activity against Plasmodium falciparum K1 isolated from po dosed patient with malaria after 7 days2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID428093Apparent clearance in Swiss mice (Mus musculus) infected with Plasmodium berghei ANKA at 90 mg/kg, intraperitoneally administered 64 hrs after infection2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID521770AUC (3 to 20 days) in children with uncomplicated malaria at 31 mg/kg, perorally2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID563108Antimalarial activity against Plasmodium falciparum IMT K2 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S mutant gene, Pmdr1 S1034C, N1042D mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hr2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1688325Antimalarial activity against Plasmodium falciparum infected in human erythrocytes assessed as inhibition of [G-3H]hypoxanthine uptake incubated for 42 hrs by liquid scintillation spectrometry2020European journal of medicinal chemistry, Feb-15, Volume: 188Current progress in antimalarial pharmacotherapy and multi-target drug discovery.
AID423716Apparent clearance with respect to bioavailability in Paua New Guinean children with uncomplicated malaria at 20 mg/kg daily for 3 days2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID564293Antimalarial activity against Plasmodium falciparum IMT Guy assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID564298Antimalarial activity against Plasmodium falciparum IMT 10336 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID564307Antimalarial activity against Plasmodium falciparum W2 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID423732Volume of distribution at steady state with respect to bioavailability in Cambodian children with malaria2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID423731Elimination half life in Cambodian children with malaria2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID428121Antiparasitic activity as survival at day 30 against Plasmodium berghei ANKA infected Swiss mice (Mus musculus) at 10 mg/kg intraperitoneal dose 64 hrs post infection2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID586610Antimalarial activity against Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID496886Antimalarial activity against chloroquine-resistant Plasmodium falciparum2010European journal of medicinal chemistry, Aug, Volume: 45, Issue:8
Quinolines and structurally related heterocycles as antimalarials.
AID563103Antimalarial activity against Plasmodium falciparum IMT 10336 harboring Pfcrt Q271E mutant gene and Ppcrt I371R mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID562110Antiplasmodial activity against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID545361Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID545390Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 harboring D10 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of dihydroartimisinin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID323672Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D72007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID423717AUC (0 to 42 days) in Paua New Guinean children with uncomplicated malaria at 20 mg/kg daily for 3 days2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID545388Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 harboring 7G8 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of dihydroartimisinin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID545391Selectivity ratio of IC50 for chloroquine-resistant Plasmodium falciparum C3 harboring Dd2 pfcrt allele to IC50 for chloroquine-sensitive Plasmodium falciparum C22009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID323674Antimalarial activity against chloroquine-resistant Plasmodium falciparum K12007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID521769Apparent oral clearance in human with uncomplicated malaria at 31 mg/kg, perorally2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID576574Antimalarial activity against Plasmodium vivax trophozoites infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax.
AID576571Antimalarial activity against Plasmodium falciparum at the ring stage infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax.
AID423739Apparent clearance with respect to bioavailability in human after fat meal using non-compartmental analysis2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID564314Antimalarial activity against Plasmodium falciparum IMT Bres harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1593296Inhibition of Plasmodium falciparum cytochrome b-c12019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
AID561052Cmax in Plasmodium falciparum-infected patient at 320 mg/kg, po2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID564296Antimalarial activity against Plasmodium falciparum IMT 8425 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID521768AUC (3 to 20 days) in human adult with uncomplicated malaria at 31 mg/kg, perorally2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID428090Terminal half life in healthy Swiss mouse at 90 mg/kg, ip by two compartment model assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID428089Initial half life in healthy Swiss mouse at 90 mg/kg, ip by two compartment model assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID1579733Inhibition of CYP3A4 (unknown origin)2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
The Development Process for Discovery and Clinical Advancement of Modern Antimalarials.
AID576576Antimalarial activity against Plasmodium vivax infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax.
AID1593287Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring V259L mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
AID555962Antimalarial activity against chloroquine-resistant Plasmodium vivax by Giemsa staining2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
In vivo and in vitro efficacy of amodiaquine monotherapy for treatment of infection by chloroquine-resistant Plasmodium vivax.
AID428122Antimalarial activity against chloroquine-resistant Plasmodium falciparum by Peters 4 day test2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID1579735Cardiotoxicity in human assessed as effect on QT parameters at 1280 mg2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
The Development Process for Discovery and Clinical Advancement of Modern Antimalarials.
AID519198Antimicrobial activity against Plasmodium vivax at the ring stage measured within 30 hrs by microscopy2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Determinants of in vitro drug susceptibility testing of Plasmodium vivax.
AID561071Antiplasmodial activity against Plasmodium falciparum D6 isolated from patient with malaria at 25 ng/ml after 28 days2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID519197Antimicrobial activity against Plasmodium vivax trophozoites measured within 30 hrs by microscopy2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Determinants of in vitro drug susceptibility testing of Plasmodium vivax.
AID748940Half life in human2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Recent advances in malaria drug discovery.
AID586613Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as inhibition of [3H]hypoxanthine incorporation2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID772515Antimalarial activity against gametocytic stage of Plasmodium berghei infected in blood assessed as inhibition of ookinete formation at 10 uM after 24 hrs by Giemsa staining-based microscopic analysis relative to control2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Using genetic methods to define the targets of compounds with antimalarial activity.
AID428087Apparent clearance in healthy Swiss mouse at 90 mg/kg, ip2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID545366Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 harboring 7G8 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID545368Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 harboring D10 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID428094Apparent volume of distribution in Swiss mice (Mus musculus) infected with Plasmodium berghei ANKA at 90 mg/kg, intraperitoneally administered 64 hrs after infection2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID545360Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID564308Antimalarial activity against Plasmodium falciparum D6 harboring Ppcrt I371R mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID564285Antimalarial activity against Plasmodium falciparum W2 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID511256Antimicrobial activity against Plasmodium falciparum harboring mdr1 N86Y/D1246Y/Y184F mutant gene by ELISA2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda.
AID423718AUC (0 to infinity) in Paua New Guinean children with uncomplicated malaria at 20 mg/kg daily for 3 days2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID545365Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID428123Toxicity in mouse2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID151200In vitro activity against Plasmodium falciparum D61992Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
Bisquinolines. 1. N,N-bis(7-chloroquinolin-4-yl)alkanediamines with potential against chloroquine-resistant malaria.
AID586606Antimalarial activity against trophozoites stage of Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID521763Apparent oral clearance in human with uncomplicated malaria at 31 mg/kg, perorally after 63 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID521771AUC (0 to 60 days) in children with uncomplicated malaria at 31 mg/kg, perorally2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID428086AUC in healthy Swiss mouse at 90 mg/kg, ip2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID423737Volume of distribution at steady state with respect to bioavailability in human after fat meal using non-compartmental analysis2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID561070Antiplasmodial activity against Plasmodium falciparum D6 isolated from po dosed patient with malaria after 7 days2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID561072Antiplasmodial activity against Plasmodium falciparum K1 isolated from patient with malaria at 25 ng/ml after 28 days2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID1638536Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FC27 infected in human RBC assessed as reduction in parasite growth after 35 to 56 hrs by nucleic acid staining based flow cytometry2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
3,3'-Disubstituted 5,5'-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity.
AID561073Plasma concentration in Plasmodium falciparum-infected patient at 320 mg/kg, po after 28 days2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID1638539Antimalarial activity against multidrug-resistant Plasmodium vivax clinical isolates assessed as reduction in parasite growth after 35 to 56 hrs by nucleic acid staining based flow cytometry2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
3,3'-Disubstituted 5,5'-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity.
AID521766Apparent intercompartmental clearance with respect to bioavailability in human with uncomplicated malaria at 31 mg/kg, perorally2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID428118Terminal half life in adult human2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID1593253Antimalarial activity against multidrug-resistant Plasmodium falciparum Dd2 infected in human erythrocytes by SYBR green 1-based fluorescence assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
AID521776Apparent oral clearance in high-fat fed healthy human at 4.2 mg/kg, po after 42 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID563111Antimalarial activity against Plasmodium falciparum IMT Vol harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scin2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID748942Antiplasmodial activity against multidrug-resistant Plasmodium falciparum W2 infected in human erythrocytes after 72 hrs by ELISA2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Recent advances in malaria drug discovery.
AID521744AUC (0 to 63 days) in human with uncomplicated malaria at 31 mg/kg, perorally once daily for 3 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID1593288Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring M133I/A138T double mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
AID561055Tmax in Plasmodium falciparum-infected patient at 320 mg/kg, po2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID423748Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID323673Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 106/12007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID428091Half life in Swiss mice (Mus musculus) infected with Plasmodium berghei ANKA at 90 mg/kg, intraperitoneally administered 64 hrs after infection2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID521754Apparent steady-state volume of distribution with respect to bioavailability in healthy human at 4.2 mg/kg, po after 42 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID564290Antimalarial activity against Plasmodium falciparum HB3 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID511251Antimicrobial activity against Plasmodium falciparum by ELISA2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda.
AID564230Antiplasmodial activity against multidrug-resistant Plasmodium falciparum VS/1 after 18 hrs by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1.
AID586612Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of [3H]hypoxanthine incorporation2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID564294Antimalarial activity against Plasmodium falciparum IMT A4 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID423715Volume of distribution at steady state with respect to bioavailability in Paua New Guinean children with uncomplicated malaria at 20 mg/kg daily for 3 days2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID563105Antimalarial activity against Plasmodium falciparum IMT 10500 harboring Pfcrt Q271E mutant gene and Ppcrt I371R mutant gene and Pfnhe-1 ms4760 microsatellite mutant assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID564286Antimalarial activity against Plasmodium falciparum D6 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID521778Terminal half-life in high-fat fed healthy human at 4.2 mg/kg, po after 42 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID545386Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum C6harboring 7G8 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of dihydroartimisinin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID521757Apparent steady-state volume of distribution with respect to bioavailability in human with uncomplicated malaria at 31 mg/kg, perorally after 63 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID323680Reduction of [3H]chloroquine uptake in chloroquine-resistant Plasmodium falciparum RSA11 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID561066Antiplasmodial activity against Plasmodium falciparum K12009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID423742Apparent clearance with respect to bioavailability in Vietnamese human2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID564311Antimalarial activity against Plasmodium falciparum PA harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID323677Antimalarial activity against chloroquine-resistant Plasmodium falciparum 34-1/E2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID564304Antimalarial activity against Plasmodium falciparum IMT K4 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID423733Apparent clearance with respect to bioavailability in Cambodian children with malaria2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID564312Antimalarial activity against Plasmodium falciparum HB3 harboring Ppcrt I371R mutant gene and Pfmdr1 Y184F mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID428125Antiparasitic activity as survival at day 30 against Plasmodium berghei ANKA infected Swiss mice (Mus musculus) at 20-30 mg/kg intraperitoneal dose 64 hrs post infection2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID323675Antimalarial activity against chloroquine-resistant Plasmodium falciparum RSA112007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID564235Antiplasmodial activity against Plasmodium falciparum harboring mutant pfcrt-76 gene after 18 hrs by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1.
AID564301Antimalarial activity against Plasmodium falciparum IMT 16332 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID428095Initial half life in Swiss mice (Mus musculus) infected with Plasmodium berghei ANKA at 90 mg/kg, intraperitoneally by two compartment model assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID564284Antimalarial activity against Plasmodium falciparum 3D7 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID545380Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of dihydroartimisinin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID423740Absorption half life in Vietnamese human by two-compartmental analysis2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID521774AUC (3 to 20 days) in uncomplicated malaria patient at 31 mg/kg, perorally once daily for 3 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID586609Antimalarial activity against ring stage of Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID323685Reduction of [3H]dihydroartemisinin uptake in chloroquine-resistant Plasmodium falciparum RSA11 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID585012Antimalarial activity against Plasmodium ovale ring stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
In vivo and in vitro efficacy of chloroquine against Plasmodium malariae and P. ovale in Papua, Indonesia.
AID563110Antimalarial activity against Plasmodium falciparum IMT L1 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillatio2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID561057AUC in Plasmodium falciparum-infected patient at 320 mg/kg, po2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID564288Antimalarial activity against Plasmodium falciparum FCR3 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID511255Antimicrobial activity against chloroquine-resistant Plasmodium falciparum K1 by ELISA2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda.
AID423735Absorption half life in human after fat meal using non-compartmental analysis2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID545359Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum TM6 infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID521765Apparent peripheral volume of distribution with respect to bioavailability in human with uncomplicated malaria at 31 mg/kg, perorally2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID317969Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum by [3H]hypoxanthine incorporation2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum.
AID521772AUC (0 to 60 days) in human adult with uncomplicated malaria at 31 mg/kg, perorally2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID521759Apparent oral clearance in healthy human at 4.2 mg/kg, po after 42 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID521749Terminal half-life in healthy human at 4.2 mg/kg, po after 42 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID545382Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of dihydroartimisinin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID521747Plasma concentration in human with uncomplicated malaria at 31 mg/kg, perorally once daily for 3 days measured at day 202008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID428124Plasma concentration in Swiss mouse at 90 mg/kg, ip administered 64 hrs after infection measured after 60 days2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID576575Antimalarial activity against Plasmodium falciparum infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax.
AID521753Apparent steady-state volume of distribution with respect to bioavailability in healthy human at 25 mg/kg, po after 29 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID428088Apparent volume of distribution in healthy Swiss mouse at 90 mg/kg, ip2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID521756Apparent steady-state volume of distribution with respect to bioavailability in human with uncomplicated malaria at 32 mg/kg, perorally after 35 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID585009Antimalarial activity against Plasmodium malariae trophozoite stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
In vivo and in vitro efficacy of chloroquine against Plasmodium malariae and P. ovale in Papua, Indonesia.
AID423734Absorption half life in human after fasting using non-compartmental analysis2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID511254Antimicrobial activity against chloroquine-resistant Plasmodium falciparum HB3 by ELISA2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda.
AID323670Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FC272007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID521775AUC (0 to 63 days) in uncomplicated malaria patient at 31 mg/kg, perorally four-dose treatment regimen2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID586611Antimalarial activity against Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID521773AUC (3 to 20 days) in uncomplicated malaria patient at 31 mg/kg, perorally four-dose treatment regimen2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID564292Antimalarial activity against Plasmodium falciparum IMT Bres assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID563109Antimalarial activity against Plasmodium falciparum IMT K4 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S mutant gene, Pmdr1 S1034C, N1042D mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hr2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID585011Antimalarial activity against Plasmodium ovale trophozoite stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
In vivo and in vitro efficacy of chloroquine against Plasmodium malariae and P. ovale in Papua, Indonesia.
AID496885Antimalarial activity against chloroquine-sensitive Plasmodium falciparum2010European journal of medicinal chemistry, Aug, Volume: 45, Issue:8
Quinolines and structurally related heterocycles as antimalarials.
AID564297Antimalarial activity against Plasmodium falciparum IMT 9881 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID564287Antimalarial activity against Plasmodium falciparum FCM29 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID521761Apparent oral clearance in human with uncomplicated malaria at 32 mg/kg, perorally after 35 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID511253Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum D6 by ELISA2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda.
AID323681Reduction of [3H]chloroquine uptake in chloroquine-resistant Plasmodium falciparum RSA11 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID1593291Antimalarial activity against drug-resistant Plasmodium falciparum 3D7 harboring A82T/V259L double mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
AID428112Plasma concentration in Swiss mice (Mus musculus) infected with Plasmodium berghei ANKA at 90 mg/kg, intraperitoneally administered 64 hrs after infection measured after 60 days2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID564305Antimalarial activity against Plasmodium falciparum IMT L1 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID564232Antiplasmodial activity against Plasmodium falciparum clinical isolate after 18 hrs by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1.
AID428109Plasma concentration in Swiss mice (Mus musculus) infected with Plasmodium berghei ANKA at 90 mg/kg, intraperitoneally administered 64 hrs after infection measured after 2 to 7 days2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID576572Antimalarial activity against Plasmodium falciparum trophozoites infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax.
AID423711Absorption half life in Papua New Guinean children with uncomplicated malaria at 20 mg/kg daily for 3 days2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID428092AUC in Swiss mice (Mus musculus) infected with Plasmodium berghei ANKA at 90 mg/kg, intraperitoneally administered 64 hrs after infection2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID564317Antimalarial activity against Plasmodium falciparum IMT 31 harboring Ppcrt I371R mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID521767Apparent volume of distribution with respect to bioavailability in human with uncomplicated malaria at 31 mg/kg, perorally2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID564318Antimalarial activity against Plasmodium falciparum IMT 8425 harboring Ppcrt I371R mutant gene and Pfnhe-1 ms4760 microsatellite mutant assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID561067Antiplasmodial activity against Plasmodium falciparum K1 assessed as inhibition of [3H]hypoxanthine incorporation by beta counting2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID545364Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum C6harboring 7G8 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID561059AUC (0 to infinity) in Plasmodium falciparum-infected patient at 320 mg/kg, po2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID511252Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum W2 by ELISA2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda.
AID563106Antimalarial activity against Plasmodium falciparum IMT 16332 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E mutant gene, Pmdr1 N86Y mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID323679Reduction of [3H]chloroquine uptake in chloroquine-sensitive Plasmodium falciparum 3D7 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID545383Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of dihydroartimisinin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID1593290Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
AID323671Antimalarial activity against chloroquine-sensitive Plasmodium falciparum T9962007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID428084Plasma concentration in Swiss mice (Mus musculus) infected with Plasmodium berghei ANKA at 90 mg/kg, intraperitoneally administered 64 hrs after infection measured after 36 hrs2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID428096Terminal half life in Swiss mice (Mus musculus) infected with Plasmodium berghei ANKA at 90 mg/kg, intraperitoneally by two compartment model assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID564303Antimalarial activity against Plasmodium falciparum IMT K2 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID521750Terminal half-life in human with uncomplicated malaria at 35 mg/kg, perorally after 35 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID1638538Antimalarial activity against multidrug-resistant Plasmodium falciparum clinical isolates infected assessed as reduction in parasite growth after 35 to 56 hrs by nucleic acid staining based flow cytometry2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
3,3'-Disubstituted 5,5'-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity.
AID545367Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 harboring parental pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID586607Antimalarial activity against ring stage of Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID423730Absorption half life in Cambodian children with malaria2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID564233Antiplasmodial activity against Plasmodium falciparum harboring wild type pfcrt-76 gene after 18 hrs by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1.
AID423736Volume of distribution at steady state with respect to bioavailability in human after fasting using non-compartmental analysis2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID521752Terminal half-life in human with uncomplicated malaria at 32 mg/kg, perorally after 35 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID545385Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum C3 harboring Dd2 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of dihydroartimisinin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID545387Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of dihydroartimisinin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID521777Apparent steady-state volume of distribution with respect to bioavailability in high-fat fed healthy human at 4.2 mg/kg, po after 42 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID563107Antimalarial activity against Plasmodium falciparum IMT K14 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S mutant gene, Pmdr1 Y184F, S1034C, N1042D, D1246Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxant2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID428083Plasma concentration in Swiss mice (Mus musculus) infected with Plasmodium berghei ANKA at 90 mg/kg, intraperitoneally administered 64 hrs after infection measured after 2 hrs2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID576577Antimalarial activity against Plasmodium vivax with >50% parasites at ring stage infected in human erythrocytes assessed as growth inhibition after 30 to 50 hrs by microscopic analysis using giemsa staining2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax.
AID519195Antimicrobial activity against Plasmodium vivax trophozoites measured after 30 hrs by microscopy2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Determinants of in vitro drug susceptibility testing of Plasmodium vivax.
AID564299Antimalarial activity against Plasmodium falciparum IMT 10354 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID585010Antimalarial activity against Plasmodium malariae ring stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
In vivo and in vitro efficacy of chloroquine against Plasmodium malariae and P. ovale in Papua, Indonesia.
AID564289Antimalarial activity against Plasmodium falciparum PA assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID521758Apparent oral clearance in healthy human at 25 mg/kg, po after 29 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID564309Antimalarial activity against Plasmodium falciparum FCM29 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID428110Antiparasitic activity as parasitaemia after 36 hrs against Plasmodium berghei ANKA infected Swiss mice (Mus musculus) at 90 mg/kg intraperitoneal dose 64 hrs post infection2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID564291Antimalarial activity against Plasmodium falciparum 106/1 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID545362Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum C2 infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID564306Antimalarial activity against Plasmodium falciparum IMT Vol assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID235122Resistance index was measured as the ratio of IC50 of Plasmodium falciparum W-2 clone / IC50 of P. falciparum D-6 clone1992Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
Bisquinolines. 1. N,N-bis(7-chloroquinolin-4-yl)alkanediamines with potential against chloroquine-resistant malaria.
AID423747Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
AID323676Antimalarial activity against chloroquine-resistant Plasmodium falciparum 7G8-mdr7G82007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID1649432Antimalarial activity against Plasmodium falciparum clinical isolates measured after 72 hrs by SYBR green dye based fluorescence assay2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials.
AID564315Antimalarial activity against Plasmodium falciparum IMT Guy harboring Ppcrt K76T, A220S, N326D and I371R mutant gene, Pmdr1 T184FN, 1042D and D1246Y, mutant gene and Pfmrp H191Y and S437A mutant gene and Pfnhe-1 ms4760 microsatellite mutant assessed as in2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID521751Terminal half-life in human with uncomplicated malaria at 31 mg/kg, perorally after 63 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
AID151201In vitro activity against Plasmodium falciparum W-21992Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
Bisquinolines. 1. N,N-bis(7-chloroquinolin-4-yl)alkanediamines with potential against chloroquine-resistant malaria.
AID428085Half life in healthy Swiss mouse at 90 mg/kg, ip2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID564310Antimalarial activity against Plasmodium falciparum FCR3 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs 2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID563104Antimalarial activity against Plasmodium falciparum IMT 10354 harboring Ppcrt M74I, N75E, K76T, A220S mutant gene, Pmdr1 D1246Y mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID428120Antiparasitic activity as survival at day 30 against Plasmodium berghei ANKA infected Swiss mice (Mus musculus) at 30 mg/kg intraperitoneal dose 64 hrs post infection2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID549354Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (635)

TimeframeStudies, This Drug (%)All Drugs %
pre-199023 (3.62)18.7374
1990's8 (1.26)18.2507
2000's88 (13.86)29.6817
2010's371 (58.43)24.3611
2020's145 (22.83)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 56.93

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

MetricThis Compound (vs All)
Research Demand Index56.93 (24.57)
Research Supply Index6.76 (2.92)
Research Growth Index5.83 (4.65)
Search Engine Demand Index93.50 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (56.93)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials227 (35.58%)5.53%
Reviews43 (6.74%)6.00%
Case Studies16 (2.51%)4.05%
Observational9 (1.41%)0.25%
Other343 (53.76%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (132)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
School-based Malaria Control: Impact of Intermittent Preventive Treatment on Malaria Morbidity and Cognitive Function in Ugandan School Children [NCT01231880]Phase 3740 participants (Actual)Interventional2011-02-28Completed
An Active Malaria Epidemiology Cohort Study With Evaluation of a 2 Day Versus 3 Day Treatment Regimen of Dihydroartemisinin (DHA)-Piperaquine for Patients With Uncomplicated Malaria [NCT01280162]222 participants (Actual)Interventional2010-09-30Completed
Comparison of the Efficacy and Safety of Two ACTs Plus Primaquine for Uncomplicated Plasmodium Vivax Malaria in North Sumatera, Indonesia: 1 Year Followup [NCT01288820]Phase 3331 participants (Actual)Interventional2011-01-31Completed
Efficacy, Safety and Tolerability of Dihydroartemisinin-Piperaquine for Treatment of Uncomplicated Falciparum Malaria in Pregnancy: an Open-label, Randomised Controlled, Non-inferiority Trial [NCT01231113]Phase 3417 participants (Actual)Interventional2011-07-31Completed
A Randomised, Double-blind, Placebo Controlled, Parallel Group Study in Healthy Adult Volunteers to Determine the Tolerability and Safety of Pyronaridine (PYR) Co-administered With Piperaquine (PQP) Under Fasted Conditions [NCT05160363]Phase 137 participants (Actual)Interventional2022-02-18Active, not recruiting
An Open-label Randomized Trial to Assess the Therapeutic Efficacy of Arterolane-piperaquine Versus Dihydroartemisinin-piperaquine for the Treatment of Uncomplicated Falciparum Malaria in Eastern Myanmar, an Area of Emerging Artemisinin-resistant Falciparu [NCT02461186]Phase 2/Phase 30 participants (Actual)Interventional2015-06-30Withdrawn(stopped due to Change of the study site due to the current political climate in Myanmar.)
Triple Antimalarial Combination (Imatinib-DHA-PPQ) to Accelerate the Parasite Clearance and to Prevent the Selection of Resistant Parasites [NCT03697668]Phase 250 participants (Anticipated)Interventional2017-09-17Recruiting
Prevention of Malaria in HIV-uninfected Pregnant Women and Infants [NCT02793622]Phase 3782 participants (Actual)Interventional2016-09-30Completed
Proof of Concept Study of Eurartesim® in Patients With Imported Uncomplicated Plasmodium Vivax Malaria [NCT02110784]Phase 227 participants (Actual)Interventional2014-06-18Terminated(stopped due to Low recruitment)
Clinical Trial to Evaluate Intermittent Screening and Treatment and Intermittent Preventive Treatment of Malaria in Asymptomatic Schoolchildren to Decrease P. Falciparum Infection and Transmission: Phase 2 Comparing Drug Regimens [NCT05980156]Phase 4646 participants (Actual)Interventional2023-02-13Completed
Clinical Investigation of In-vivo Susceptibility of P. Falciparum to Artesunate in Phuoc Long Hospital, Binh Phuoc Province, Vietnam [NCT01165372]Phase 2166 participants (Actual)Interventional2010-08-31Completed
Evaluation of the Safety of Primaquine in Combination With Dihydroartemisinin-piperaquine in G6PD Deficient Males in The Gambia [NCT02654730]Phase 2/Phase 361 participants (Actual)Interventional2015-12-31Terminated(stopped due to Enrollment took longer than anticipated; it was financially and logistically impossible to recruit the final cohort (G6PDd 0.4mg/kg PQ).)
Defining Effective, Appropriate, Implementable Strategies for Malaria Elimination in Military Forces in Cambodia as a Model for Mobile Populations [NCT02653898]Phase 41,050 participants (Actual)Interventional2016-01-31Active, not recruiting
Effects of Metronidazole Plus Intermittent Preventive Treatment of Malaria in Pregnancy on Birth Outcomes: a Randomised Controlled Trial in Zambia [NCT04189744]Phase 35,436 participants (Actual)Interventional2019-12-15Completed
Clinical Efficacy of Artemisinin-based Combination Therapy for Treatment of Uncomplicated Plasmodium Falciparum Malaria in North Sumatera, Indonesia and the Association of Molecular Markers With Treatment Outcomes [NCT02325180]Phase 4338 participants (Actual)Interventional2015-01-31Completed
Combination Momordica Charantia Extract and Primaquine Againts Plasmodium Falciparum Uncomplicated and Plasmodium Vivax Uncomplicated Treatment in Manokwari, West Papua [NCT06036030]Phase 250 participants (Actual)Interventional2019-01-11Completed
Dihydroartemisinin-Piperaquine or Sulphadoxine-Pyrimethamine for the Chemoprevention of Malaria in Children With Sickle Cell Anaemia in Eastern and Southern Africa: a Double Blind Randomised Trial (CHEMCHA) [NCT04844099]Phase 3723 participants (Actual)Interventional2021-04-09Completed
Observational Study to Evaluate the Clinical Safety After Introduction of the Fixed Dose Artemisinin-based Combination Therapy Eurartesim® (Dihydroartemisinin/Piperaquine [Dha/Pqp]) in Public Health Districts in Sub-Saharan Africa. [NCT02199951]10,000 participants (Anticipated)Observational2013-09-30Recruiting
Clinical Trial to Evaluate Efficacy and Safety of Sulfadoxine/Pyrimethamine-Amodiaquine and Dihydroartemsinin-Piperaquine Plus Ivermectin Administered Monthly as Intermittent Preventive Treatment in School-aged Children in Burkina Faso [NCT05946642]Phase 313,000 participants (Anticipated)Interventional2023-07-15Recruiting
A Randomised, Single-blinded Controlled Treatment Trial of Subclinical Vivax Infections With Primaquine in Nong Province, Laos [NCT02802813]Phase 1/Phase 241 participants (Actual)Interventional2016-06-14Completed
DPART Study: Dihydroartemisinin-Piperaquine in the Context of Antiretroviral Therapy [NCT04487145]Phase 4190 participants (Actual)Interventional2020-11-23Completed
The Tolerability and Safety of Low Dose Primaquine for Transmission Blocking in Symptomatic Falciparum Infected Cambodians [NCT02434952]Phase 4109 participants (Actual)Interventional2014-10-31Completed
An Open-label Randomised Trial to Assess the Therapeutic Efficacy and Tolerability of Arterolane-piperaquine Plus Single Low Dose Primaquine Versus Arterolane-piperaquine Plus Mefloquine and Single Low Dose Primaquine Versus Artemether-lumefantrine Plus S [NCT03452475]Phase 3219 participants (Actual)Interventional2018-03-07Completed
Effectiveness and Safety of Intermittent Preventive Treatment for Malaria Using Either Dihydroartemisinin-piperaquine or Artesunate-amodiaquine in Reducing Malaria Related Morbidities and Improving Cognitive Ability in School-aged Children in Tanzania: A [NCT03640403]Phase 31,555 participants (Actual)Interventional2019-03-26Active, not recruiting
Optimal Chemopreventive Regimens to Prevent Malaria and Improve Birth Outcomes in Uganda [NCT04336189]Phase 32,757 participants (Anticipated)Interventional2020-12-28Recruiting
Evaluating the Effectiveness and Feasibility of Reactive Focal Mass Drug Administration vs. Reactive Case Detection as a Community Level Intervention in Response to a Passively Identified Index Malaria Case in Swaziland [NCT02315690]Phase 34,000 participants (Actual)Interventional2015-09-30Completed
Open-Label Study to Evaluate Potential Pharmacokinetic and Pharmacodynamic Interactions of Orally Administered Mefloquine and Dihydroartemisinin-Piperaquine in Healthy Adult Subjects [NCT02324738]Phase 416 participants (Actual)Interventional2015-01-31Completed
Evaluation of the Efficacy of Artemether-lumefantrine and Dihydroartemisinin-piperaquine in Children With Uncomplicated Clinical Malaria in Rural Rwanda [NCT04767217]Phase 4528 participants (Anticipated)Interventional2021-06-14Recruiting
A Double Blind Randomized Controlled Trial of Dihydroartemisinin-piperaquine Alone and in Combination With Single Dose Primaquine to Reduce Post-treatment Malaria Transmission. [NCT02259426]Phase 3120 participants (Actual)Interventional2014-10-31Completed
Safety and Feasibility of a Malaria Transmission Model in Semi-immune Kenyan Adults Using Plasmodium Falciparum Sporozoites [NCT04280692]Phase 1/Phase 244 participants (Actual)Interventional2022-08-22Active, not recruiting
Efficacy and Safety of Artesunate-amodiaquine and Dihydroartemisinin-piperaquine for the Treatment of Uncomplicated Falciparum Malaria in Mainland Tanzania [NCT03431714]Phase 4333 participants (Actual)Interventional2017-07-14Completed
Phase I, Randomized, Parallel Group Study to Evaluate the Effect of Multiple Oral Doses of Eurartesim on the QT/QTc Interval Compared to Riamet, Placebo and Moxifloxacin in Healthy Male and Female Volunteers [NCT01103830]Phase 1287 participants (Actual)Interventional2010-02-28Completed
Comparison of the Electrocardiographic Effects in Relation to Pharmacokinetic Profile of Chloroquine and Piperaquine in Healthy Thai Subjects [NCT02192944]Phase 416 participants (Actual)Interventional2014-07-31Completed
Impact Tanzania in Vivo Efficacy 2010: Assessing the Efficacy of Artemisinin Combination Therapies for Treatment of Uncomplicated Malaria Infection in Children Aged 6-59 Months [NCT01082705]Phase 3323 participants (Actual)Interventional2010-04-30Completed
Mass Drug Administration of Ivermectin and Dihydroartemisinin-piperaquine as an Additional Intervention for Malaria Elimination [NCT03576313]Phase 34,939 participants (Actual)Interventional2018-08-11Completed
Effectiveness of Mass Drug Administration (MDA) for Reducing Seasonal Malaria Transmission Towards Its Elimination in Hotspot Areas in Zanzibar - a Cluster-randomised Controlled Trial [NCT02721186]22,500 participants (Actual)Interventional2016-04-30Completed
A Randomized Controlled Trial of Monthly Dihydroartemisinin-piperaquine Versus Monthly Sulfadoxine-pyrimethamine Versus Daily Trimethoprim-sulfamethoxazole Versus No Therapy for the Prevention of Malaria [NCT00948896]Phase 3600 participants (Actual)Interventional2010-06-30Completed
'Controlled Human Malaria Infection Study to Assess Gametocytaemia and Mosquito Transmissibility in Participants Challenged With Plasmodium Falciparum by Sporozoite Challenge to Establish a Model for the Evaluation of Transmission-blocking Interventions' [NCT02836002]Phase 1/Phase 229 participants (Actual)Interventional2016-06-30Completed
[NCT00845533]Phase 40 participants Interventional2007-08-31Completed
[NCT00868465]600 participants (Anticipated)Interventional2009-04-30Completed
A Phase II, Open-label, Multicentre, Pharmacokinetic, Pharmacodynamics and Safety Study of a New Paediatric Eurartesim Dispersible Formulation and Crushed Film Coated Eurartesim Tablet, in Infant Patients With P. Falciparum Malaria [NCT01992900]Phase 2300 participants (Actual)Interventional2013-11-30Completed
Open Label Randomized Study Evaluating the in Vivo Efficacies of Artemether-lumefantrine and Dihydroartemisinin-piperaquine in the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Children Under Five Years of Age in Western Kenya [NCT05060198]340 participants (Actual)Interventional2016-06-17Completed
Phase 1b to Assess Safety, Tolerability, Pharmacokinetic Profile, and Antimalarial Activity of Single Doses of Co-administered OZ439and PQP Against Early Plasmodium Falciparum Blood Stage Infection in Healthy Adult Volunteers [NCT03542149]Phase 124 participants (Actual)Interventional2018-04-23Completed
Adaptation of Blood-stage Controlled Human Malaria Infection for Evaluation of Transmission Blocking Malaria Interventions in Malaria Endemic Countries [NCT06172686]Phase 124 participants (Anticipated)Interventional2024-01-09Not yet recruiting
A Five-cohort, Randomized, Open-label, Parallel-group Study to Evaluate the Pharmacokinetics of a Single Dose of Tafenoquine (SB252263) 300mg When Co-administered With the Artemisinin-based Combination Therapies (ACT) Artemether + Lumefantrine (AL) and Di [NCT02184637]Phase 1120 participants (Actual)Interventional2014-07-31Completed
Malaria Chemoprevention With Monthly Treatment With Dihydroartemisinin-Piperaquine for the Post-discharge Management of Severe Anaemia in Children Less Than 5 Years in Malawi [NCT02721420]Phase 3375 participants (Anticipated)Interventional2016-03-24Recruiting
A Multi-site Cohort Observational Study for Molecular Assessment of Artemisinin Resistance Falciparum Malaria in Myanmar [NCT02792816]550 participants (Actual)Observational2009-06-30Completed
Chemoprevention With Monthly IPTp With Dihydroartemisinin-piperaquine for Malaria in HIV-infected Pregnant Participants on Daily Cotrimoxazole in Kenya and Malawi: a Multi-centre Placebo-controlled Trial [NCT04158713]Phase 3898 participants (Actual)Interventional2019-11-11Completed
Intermittent Preventive Treatment in Pregnancy With Sulfadoxine-pyrimethamine Plus Dihydroartemisinin-piperaquine to Prevent Malaria Infection and Reduce Adverse Pregnancy Outcomes in Papua New Guinea - a Randomised Controlled Trial [NCT05426434]Phase 31,172 participants (Anticipated)Interventional2022-08-31Recruiting
Randomized Clinical Trial of the Efficacy and Safety of Dihydroartimisinine+Papiraquine (Artekin) Compared With First Line Drugs for Treatment of Vivax and Uncomplicated Falciparum Malaria in Afghanistan [NCT00682578]Phase 31,086 participants (Actual)Interventional2007-07-31Completed
IPT in Schoolchildren: Comparison of the Efficacy, Safety, and Tolerability of Antimalarial Regimens in Uganda [NCT00852371]Phase 3760 participants (Actual)Interventional2008-02-29Completed
Effectiveness and Safety of Artemether + Lumefantrine and Dihydroartemisinin + Piperaquine for the Treatment of Uncomplicated Malaria in Guinea-Bissau [NCT04897919]Phase 4474 participants (Actual)Interventional2015-08-01Completed
Malaria Chemoprevention With Monthly Treatment With Dihydroartemisinin-piperaquine for the Post-discharge Management of Severe Anaemia in Children Aged Less Than 5 Years in Uganda and Kenya: A Two-arm Randomised Placebo Controlled Trial [NCT02671175]Phase 31,049 participants (Actual)Interventional2016-05-20Completed
A Safety, Tolerability, Pharmacokinetic and Efficacy Study of Azithromycin Plus Piperaquine as Presumptive Treatment in Pregnant Papua New Guinean Women [NCT02575755]Phase 4150 participants (Anticipated)Interventional2012-10-31Recruiting
Enhancing Immunity to Malaria in Young Children With Effective Chemoprevention [NCT04978272]Phase 3924 participants (Actual)Interventional2022-02-08Active, not recruiting
A Phase1 Interventional Sequential Single Site Study to Characterize the Effectiveness of Oral KAE609 in Reducing Asexual & Sexual Blood-stage P. Falciparum Following Inoculation in Healthy-volunteers & Subsequent Infectivity to Mosquitoes [NCT02543086]Phase 18 participants (Actual)Interventional2015-07-31Terminated
A Randomized, Placebo-controlled, Double-blind Trial Using Dihydroartemisinine+Piperaquine (DP) to Protect Forest Workers From Malaria in Bu Gia Map National Park [NCT02788864]Phase 4150 participants (Actual)Interventional2016-05-20Completed
A Multi-Site, Open-Label, Randomized Trial to Assess the Efficacy, Safety, and Tolerability of Dihydroartemisinin-Piperaquine Plus Mefloquine Compared to Dihydroartemisinin-Piperaquine or Artesunate-Mefloquine in Patients With Uncomplicated Falciparum Mal [NCT02612545]Phase 1216 participants (Actual)Interventional2015-11-20Completed
Safe and Efficacious Artemisinin-based Combination Treatments for African Pregnant Women With Malaria [NCT00852423]Phase 33,428 participants (Actual)Interventional2010-06-30Completed
The Efficacy and Safety of Pyronaridine-artesunate Combined With Low Dose Primaquine for Preventing Transmission of P. Falciparum Gametocytes in Sub-Saharan Africa [NCT04049916]Phase 2/Phase 3100 participants (Actual)Interventional2019-09-12Completed
A Multi-centre Randomised Controlled Non-inferiority Trial to Compare the Efficacy, Safety and Tolerability of Triple Artemisinin-based Combination Therapies Versus First-line ACTs + Placebo for the Treatment of Uncomplicated Plasmodium Falciparum Malaria [NCT03939104]Phase 31,368 participants (Anticipated)Interventional2021-06-30Recruiting
A Multi-centre Randomised Controlled Non-inferiority Trial to Compare the Efficacy, Safety and Tolerability of Triple Artemisinin-based Combination Therapies Versus First-line ACTs + Placebo for the Treatment of Uncomplicated Plasmodium Falciparum Malaria [NCT03923725]Phase 33,240 participants (Anticipated)Interventional2020-09-01Recruiting
Evaluation of 4 Artemisinin-based Combinations for Treating Uncomplicated Malaria in African Children [NCT00393679]Phase 34,112 participants (Actual)Interventional2007-07-31Completed
[NCT01075945]Phase 4140 participants (Anticipated)Interventional2010-02-28Recruiting
Efficacy and Safety of Artemether-Lumefantrine and Dihydroartemisinin-Piperaquine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria Among Children in the North Region of Cameroon [NCT05340153]Phase 4184 participants (Anticipated)Interventional2022-04-11Not yet recruiting
Electrocardiographic Safety Evaluation of Monthly Dihydroartemisinin-Piperaquine for the Use in Mass Treatment Campaigns to Block Malaria Transmission [NCT02605720]Phase 378 participants (Actual)Interventional2015-09-30Completed
In-vivo Efficacy and Safety of Artemether/Lumefantrine Vs Dihydroartemisinin-piperaquine for Treatment of Uncomplicated Malaria and Assessment of Parasite Genetic Factors Associated With Parasite Clearance or Treatment Failure [NCT02590627]Phase 4509 participants (Actual)Interventional2014-05-31Completed
Targeted Chemo-elimination (TCE) to Eradicate Malaria in Areas of Suspected or Proven Artemisinin Resistance in Southeast Asia and South Asia [NCT01872702]8,000 participants (Actual)Interventional2013-04-30Completed
Impact of Mass Screening and Selective Treatment With Dihydroartemisinin-piperaquine Plus Primaquine on Malaria Transmission in High Endemic Area, Belu Regency, Nusa Tenggara Timur Province, Indonesia: a Randomized Cluster Trial [NCT01878357]Phase 41,488 participants (Actual)Interventional2013-06-30Completed
Safety, Tolerability, Pharmacokinetics and Efficacy, Phase Iv, Open Label Study of Fixed Arco® and Eurartesim® Therapies in Adults and Children With Uncomplicated P. Falciparum Malaria in Tanzania [NCT01930331]Phase 460 participants (Actual)Interventional2014-01-07Completed
Interactions Between HIV and Malaria in African Children [NCT00527800]Phase 3351 participants (Actual)Interventional2007-08-31Completed
Efficacy and Safety of the Dispersible Formulation of Artemether-lumefantrine, Co-formulated Artesunate-amodiaquine and Co-formulated Dihydroartemisinin-piperaquine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Machinga District, Mal [NCT01326754]498 participants (Actual)Interventional2011-08-31Completed
A Phase IIa Proof of Concept Study to Explore the Efficacy, Tolerability and Safety of Fosmidomycin Sodium When Administered With Piperaquine Tetraphosphate to Adults and Older Children With Acute Uncomplicated Plasmodium Falciparum Malaria [NCT02198807]Phase 2100 participants (Actual)Interventional2014-03-31Active, not recruiting
A Randomised Controlled Trial to Assess the Antimalarial Drug Susceptibility and Molecular Characterization of Plasmodium Vivax Isolates in Vietnam [NCT01887821]Phase 4330 participants (Actual)Interventional2013-02-28Completed
Single Low Dose Tafenoquine to Reduce P. Falciparum Transmission in Mali (NECTAR2) [NCT04609098]Phase 280 participants (Actual)Interventional2020-10-29Completed
Effectiveness of Dihydroartemisinin-piperaquine as Seasonal Malaria Chemoprophylaxis in Extended High Transmission Settings of Tanzania: an Open Cluster Randomized Clinical Trial. [NCT05874869]13,800 participants (Actual)Interventional2020-07-01Completed
A Randomized, Open Label, Two-part, Parallel-group, Phase I Study to Evaluate the Pharmacokinetics of Piperaquine Oral Dispersible Granules Formulation Compared to Piperaquine Hard Tablets Administered as a Single Dose in Fasting Condition (Part 1) and of [NCT05930782]Phase 160 participants (Anticipated)Interventional2023-07-24Active, not recruiting
Intermittent Screening and Treatment for the Control of Malaria in the First Year of Life in Papua, Indonesia: A Cluster Randomized Controlled Trial [NCT02001428]757 participants (Actual)Interventional2014-07-21Completed
'SCHOOL-BASED TREATMENT WITH ACT TO REDUCE TRANSMISSION' (START-IPT): Evaluation of the Community Impact of Intermittent Preventive Treatment for Malaria in Ugandan Children: a Cluster Randomised Trial [NCT02009215]Phase 410,746 participants (Actual)Interventional2014-02-28Completed
Comparison of Safety, Tolerability and Efficacy of Three Drug Combinations for Intermittent Preventive Treatment in Children Aged 1-5 Years in an Area of Seasonal Malaria Transmission in Upper River Division, The Gambia [NCT00561899]Phase 2/Phase 31,295 participants (Actual)Interventional2007-08-31Completed
Randomised Parallel Open Label Comparison Between 7 and 14 Day Primaquine Combined With 3-day Dihydroartemisinin-piperaquine or 3-day Chloroquine Regimens for Radical Cure of Plasmodium Vivax [NCT01640574]Phase 3680 participants (Actual)Interventional2012-02-29Completed
Effect of Imatinib on Suppression of Malaria Parasites in Patients With Uncomplicated Plasmodium Falciparum Malaria [NCT02614404]Phase 115 participants (Actual)Interventional2015-11-30Completed
Reactive Household-based Self-administered Treatment Against Residual Malaria Transmission: a Cluster Randomized Trial [NCT02878200]2,236 participants (Actual)Interventional2016-11-04Completed
Acceptability and Feasibility of IPTp With Dihydroartemisinin-piperaquine With or Without Azithromycin to Prevent Malaria, Sexually Transmitted and Reproductive Tract Infections in HIV-uninfected Pregnant Women (IMPROVE) in Kenya. [NCT04160026]Phase 41,600 participants (Actual)Interventional2019-11-11Completed
Efficacy, Safety, and Pharmacokinetics of Sulphadoxine-pyrimethamine-amodiaquine (SP-AQ), SP-AQ Plus Primaquine, Dihydroartemisinin-piperaquine (DP), DP Plus Methylene Blue for Preventing Transmission of P. Falciparum Gametocytes in Mali [NCT02831023]Phase 280 participants (Actual)Interventional2016-07-31Completed
Evaluation of the Household-level Impact of a Single Round of Intermittent Preventive Treatment of Malaria in Schoolchildren: A Randomized Study [NCT04660110]Phase 31,500 participants (Anticipated)Interventional2021-01-28Recruiting
Evaluation of Impact Dihydroartemisinin-piperaquine Plus Primaquine on Malaria Transmission in Lempasing Village, Lampung Province, Southern Sumatra [NCT01389557]Phase 477 participants (Actual)Interventional2011-02-28Completed
Effectiveness of Dihydroartemisinin-piperaquine With or Without Primaquine on Gametocytes Plasmodium Falciparum in Mesoendemic Area of Indonesia [NCT01392014]Phase 4374 participants (Actual)Interventional2008-12-31Completed
Evaluation of the Implementation and Effectiveness of Intermittent Preventive Treatment for Malaria Using Dihydroartemisinin-piperaquine on Reducing Malaria Burden in School Aged Children in Tanzania [NCT04245033]Phase 44,100 participants (Actual)Interventional2020-07-20Active, not recruiting
A Randomised Open Label Trial Comparing Standard Dose of Dihydroartemisinin-piperaquine, Standard Fixed Artesunate-mefloquine Regimen and a Longer Regimen of Artemether-lumefantrine in the Treatment of Uncomplicated Malaria in Pregnancy [NCT01054248]Phase 3511 participants (Actual)Interventional2010-02-16Completed
Effectiveness of Momordica Charantia Extract Compared to the Standard Antimalarial Drug Combination Dihydroartemisinin Piperaquine-primaquine in Patients With Uncomplicated Falciparum Malaria, in Sumba Barat Daya District of Indonesia [NCT05829187]Phase 236 participants (Actual)Interventional2022-11-01Completed
Active Surveillance for P. Falciparum Drug Resistance With Assessment of Transmission Blocking Activity of Single Dose Primaquine in Cambodia [NCT01849640]150 participants (Anticipated)Interventional2012-12-31Suspended(stopped due to Poor efficacy of DHA-piperaquine due to likely drug resistance.)
Does Artemisinin Combination Treatment Reduce the Radical Curative Efficacy of High Dose Tafenoquine for Plasmodium Vivax Malaria? [NCT05788094]Phase 4388 participants (Anticipated)Interventional2023-06-26Recruiting
Mass Drug Administration of Monthly DHA-PQP to Accelerate Towards Malaria Elimination in Magude District, Southern Mozambique [NCT02914145]240,502 participants (Actual)Interventional2015-11-30Completed
Randomized Trial of Effectiveness and Acceptability of Three Alternative Regimens for Malaria Seasonal Intermittent Preventive Treatment in Senegal [NCT00529620]Phase 31,833 participants (Actual)Interventional2007-09-30Completed
Cardiac Safety of Dihydroartemisinin-Piperaquine Amongst Pregnant Women in Tanzania [NCT02909712]Phase 2201 participants (Actual)Interventional2016-09-30Completed
Evaluation of a Pilot Implementation of Intermittent Preventive Treatment With Dihydroartemisinin-piperaquine to Prevent Adverse Birth Outcomes in Papua, Indonesia [NCT05294406]Phase 41,420 participants (Anticipated)Interventional2022-02-07Active, not recruiting
Evaluation of the Safety and Efficacy of Dihydroartemisinin-piperaquine for Intermittent Preventive Treatment of Malaria in HIV-infected Pregnant Women [NCT03671109]Phase 3666 participants (Actual)Interventional2019-09-18Completed
Randomised Phase IIb Study of Efficacy, Safety, Tolerability & Pharmacokinetics of a Single Dose Regimen of Artefenomel (OZ439) in Loose Combination With Piperaquine in Adults and Children With Uncomplicated Plasmodium Falciparum Malaria. [NCT02083380]Phase 2/Phase 3448 participants (Actual)Interventional2014-07-31Completed
A Cluster-randomised, Open-label Trial to Compare the Impact of Combined Mass Vaccine and Drug Administrations, Mass Drug Administration, Mass Vaccinations, or no Intervention on Plasmodium Falciparum Malaria Transmission [NCT06068530]Phase 410,000 participants (Anticipated)Interventional2023-11-01Not yet recruiting
Efficacy and Safety of Artesunate-amodiaquine, Artemether-lumefantrine and Dihydroartemisinine-piperaquine in the Treatment of Uncomplicated Plasmodium Falciparum Malaria in the Democratic Republic of Congo: a Randomized Controlled Trial [NCT02940756]Phase 41,615 participants (Actual)Interventional2017-03-15Completed
IPTp With Dihydroartemisinin-piperaquine and Azithromycin for Malaria, Sexually Transmitted and Reproductive Tract Infections in Pregnancy in High Sulphadoxine-pyrimethamine Resistance Areas in Kenya, Malawi and Tanzania [NCT03208179]Phase 34,680 participants (Actual)Interventional2018-03-29Completed
Preventing Malaria in School Children to Protect the Whole Community in Rural Blantyre District, Malawi [NCT06083688]Phase 41,000 participants (Anticipated)Interventional2024-10-31Not yet recruiting
A Randomized, Double Blind, Placebo-controlled Clinical Trial of Monthly DHA-piperaquine for Malaria Prevention in Cambodia. [NCT01624337]231 participants (Anticipated)Interventional2012-05-31Terminated(stopped due to Medication safety concern)
An Individually Randomised Trial of Seasonal Malaria Chemoprevention Versus a Long-acting Artemisinin Combination Therapy for the Prevention of Malaria and Anaemia in Children Living in an Area of Extended Seasonal Transmission in Ghana. [NCT01651416]Phase 42,400 participants (Actual)Interventional2012-07-31Completed
Efficacy and Safety of Artemether + Lumefantrine and Dihydroartemisinin + Piperaquine for the Treatment of Uncomplicated Malaria in Guinea-Bissau. [NCT01704508]Phase 4346 participants (Actual)Interventional2012-11-30Completed
Phase 2a Dose Escalation Study of the Efficacy, Safety, and Pharmacokinetics of Low Dose Primaquine for Gametocytocidal Activity Against P. Falciparum in Sub-Saharan Africa and South East Asia [NCT01743820]Phase 281 participants (Actual)Interventional2013-09-30Completed
Efficacy of Artesunate-amodiaquine, Dihydroartemisinin-piperaquine and Artemether-lumefantrine Combination Therapies for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Children Aged 6 to 59 Months in Maradi, Niger 2012-13 [NCT01755559]Phase 4663 participants (Actual)Interventional2013-06-30Completed
Phase III Study to Study the Clinical Response to ACT Fixed Dose Combination in 42 Days in Uncomplicated Malaria in Cameroon [NCT01845701]Phase 3720 participants (Actual)Interventional2010-03-31Completed
Study 200894: A Double-blind, Double-dummy, Randomized, Parallel Group, Placebo-controlled Superiority Study to Evaluate the Efficacy and Safety of Tafenoquine (SB-252263, WR238605) Co-administered With Dihydroartemisinin-piperaquine (DHA-PQP) for the Rad [NCT02802501]Phase 3150 participants (Actual)Interventional2018-04-08Completed
Evaluation of Community-based Screening and Treatment for Malaria in the KEMRI/CDC Health and Demographic Surveillance System (HDSS) in Western Kenya [NCT02987270]Phase 390,000 participants (Actual)Interventional2013-04-30Completed
Controlled Human Malaria Infection Study to Assess Gametocytemia and Mosquito Transmissibility in Participants Challenged With Plasmodium Falciparum by Sporozoite or Blood Stage Challenge to Establish a Model for the Evaluation of Transmission-blocking In [NCT03454048]24 participants (Actual)Interventional2018-05-07Completed
Adjunctive Ivermectin Mass Drug Administration for Malaria Control on the Bijagos Archipelago of Guinea Bissau: A Cluster-randomized Placebo-controlled Trial [NCT04844905]Phase 324,000 participants (Anticipated)Interventional2021-05-03Recruiting
Assessment of Antimalaria Drugs Susceptibility Testing for an Effective Management of Infected Patients in Sub-Sahara Africa [NCT02974348]Phase 3300 participants (Actual)Interventional2013-01-31Completed
Randomized Open-label Trial of Comparison Between DHA-Piperaquine and Mefloquine Artesunate Combinations 3 Day-regimens for the Treatment of Uncomplicated Plasmodium Falciparum Malaria on the Thai-Myanmar Border (RDM) [NCT01640587]76 participants (Actual)Interventional2013-11-30Terminated(stopped due to No adequate malaria patient)
Efficacy and Safety of Sulfadoxine-pyrimethamine or Sulfadoxine-pyrimethamine Plus Piperaquine Regimens Delivered Through Intermittent Preventive Treatment in Schoolchildren of Democratic Republic of Congo: A Randomised Control Trial [NCT01722539]Phase 3616 participants (Actual)Interventional2012-11-30Completed
Clinical Trial to Evaluate Intermittent Screening and Treatment and Intermittent Preventive Treatment of Malaria in Asymptomatic Schoolchildren to Decrease P. Falciparum Infection and Transmission [NCT05244954]Phase 4746 participants (Actual)Interventional2022-02-01Completed
A Prospective Randomized Open-Label Study on the Efficacy and Safety of Intermittent Preventive Treatment in Pregnancy (IPTp) With Dihydroartemisinin-Piperaquine (DP) Versus IPTp With Sulfadoxine-Pyrimethamine (SP) in Malawi [NCT03009526]Phase 3602 participants (Actual)Interventional2017-01-17Completed
Reducing the Burden of Malaria in HIV-uninfected Pregnant Women and Infants (PROMOTE Birth Cohort 1) [NCT02163447]Phase 3300 participants (Actual)Interventional2014-06-23Completed
Reducing the Burden of Malaria in HIV-Infected Pregnant Women and Their HIV-Exposed Children (PROMOTE Birth Cohort 2) [NCT02282293]Phase 3200 participants (Actual)Interventional2014-12-09Completed
Blood Stage Challenge Study to Asses Mosquito Transmissibility in Participants Inoculated With Plasmodium Falciparum [NCT02431637]Phase 16 participants (Actual)Interventional2015-04-30Completed
Phase 3a: Efficacy, Safety, and Tolerability of Dihydroartemisinin/Piperaquine (Artekin®) for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in the Peruvian Amazon Region [NCT00373607]Phase 3522 participants (Actual)Interventional2003-07-31Completed
Mass Drug Administration With Dihydroartemisinin-piperaquine and Primaquine to Reduce Malaria in a Moderate-low Transmission Setting in Senegal: A Cluster Randomized Controlled Trial [NCT04864444]10,715 participants (Actual)Interventional2021-06-19Completed
Efficacy and Safety of Dihydroartemisinin-piperaquine for the Treatment of Uncomplicated Plasmodium Falciparum and Plasmodium Vivax Malaria in Timika, Indonesia [NCT02353494]130 participants (Actual)Observational2015-03-31Completed
Boosting the Impact of Seasonal Malaria Chemoprevention (SMC) Through Simultaneous Screening and Treatment of SMC-Children's Roommates in Burkina Faso [NCT04816461]Phase 4789 participants (Anticipated)Interventional2021-07-31Not yet recruiting
Enhancing Preventive Therapy of Malaria In Children With Sickle Cell Anemia in East Africa (EPiTOMISE) [NCT03178643]Phase 4246 participants (Actual)Interventional2018-01-23Completed
Evaluation of the Efficacy of Artemisinin Combination Therapy in Kenya [NCT01899820]Phase 32,100 participants (Anticipated)Interventional2013-04-30Active, not recruiting
A Hybrid Effectiveness-implementation Study to Assess the Effectiveness and Chemoprevention Efficacy of Implementing Seasonal Malaria Chemoprevention in Five Districts in Karamoja Region, Uganda [NCT05323721]Phase 46,805 participants (Actual)Interventional2022-06-01Active, not recruiting
Efficacy of Artemether Lumefantrine (AL) and Dihydroartemisinin-Piperaquine (DHP) for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Siaya and Bungoma Counties, Kenya [NCT04767191]Phase 4400 participants (Actual)Interventional2021-03-15Completed
A Phase I Study to Investigate the Safety, Tolerability & Pharmacokinetics of Co-administered Single Doses of OZ439 and Piperaquine to Healthy Subjects [NCT01660022]Phase 159 participants (Actual)Interventional2012-09-30Completed
Field Study of the Pharmacokinetics and Pharmacodynamics of Artemisinin-based Combination Therapy for Gametocyte Clearance and Post-treatment Chemoprotection in Zambian Children With Uncomplicated Falciparum Malaria [NCT04009343]Phase 2/Phase 3182 participants (Anticipated)Interventional2019-06-19Active, not recruiting
Efficacy and Safety of High-dose Ivermectin for Reducing Malaria Transmission: A Dose Finding Study (IVERMAL) [NCT02511353]Phase 2141 participants (Actual)Interventional2015-07-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00948896 (4) [back to overview]Incident Malaria Cases Per Person Year at Risk in HIV-unexposed Participants
NCT00948896 (4) [back to overview]Incident Malaria Cases Per Person Year at Risk in HIV-exposed Participants
NCT00948896 (4) [back to overview]Rebound Incidence of Malaria Defined as the Number of Treatments for New Episodes of Malaria Per Time at Risk
NCT00948896 (4) [back to overview]Incidence of Any Adverse Events Defined as Severity Grade 3-4 That Are Possibly, Probably, or Definitely Related to Study Drugs
NCT01660022 (6) [back to overview]OZ439 AUC(0-168)
NCT01660022 (6) [back to overview]OZ439 t1/2
NCT01660022 (6) [back to overview]Piperaquine t1/2
NCT01660022 (6) [back to overview]OZ439 Cmax
NCT01660022 (6) [back to overview]Piperaquine AUC(0-168)
NCT01660022 (6) [back to overview]Piperaquine Cmax
NCT02083380 (32) [back to overview]PCR-adjusted ACPR at Day 42 in the ITT Population
NCT02083380 (32) [back to overview]PCR-adjusted ACPR at Day 63 in the ITT Population
NCT02083380 (32) [back to overview]PCR-adjusted ACPR at Day 63 in the PP Population
NCT02083380 (32) [back to overview]Piperaquine: Cday7 Africa (> 5 Years)
NCT02083380 (32) [back to overview]Piperaquine: Cday7 Africa (>=0.5 to <= 2 Years)
NCT02083380 (32) [back to overview]Crude ACPR at Day 63 in the ITT Population
NCT02083380 (32) [back to overview]Piperaquine: Cday7 Asia (All Ages)
NCT02083380 (32) [back to overview]PRR48
NCT02083380 (32) [back to overview]Piperaquine: Cday7 Africa (>2 to <= 5 Years)
NCT02083380 (32) [back to overview]Artefenomel Cday7 African Patients (> 5 Years)
NCT02083380 (32) [back to overview]Artefenomel Cday7 African Patients (>=0.5 to <= 2 Years)
NCT02083380 (32) [back to overview]Artefenomel Cday7 African Patients (>2 to <= 5 Years)
NCT02083380 (32) [back to overview]Artefenomel Cday7 Asian Patients (All Ages)
NCT02083380 (32) [back to overview]Crude ACPR at Day 28 in the ITT Population
NCT02083380 (32) [back to overview]Crude ACPR at Day 28 in the PP Population
NCT02083380 (32) [back to overview]Crude ACPR at Day 42 in the ITT Population
NCT02083380 (32) [back to overview]Crude ACPR at Day 42 in the PP Population
NCT02083380 (32) [back to overview]Crude ACPR at Day 63 in the PP Population
NCT02083380 (32) [back to overview]Fever Clearance Time
NCT02083380 (32) [back to overview]Kaplan-Meier Estimate of New Infection Rate
NCT02083380 (32) [back to overview]Kaplan-Meier Estimate of Recrudescence
NCT02083380 (32) [back to overview]Kaplan-Meier Estimate of Recurrence
NCT02083380 (32) [back to overview]Parasite Clearance Time
NCT02083380 (32) [back to overview]PCR - Adjusted ACPR at Day 42 in the PP Population
NCT02083380 (32) [back to overview]PCR-adjusted ACPR at Day 28 in the ITT Population
NCT02083380 (32) [back to overview]PCR-adjusted ACPR at Day 28 in the PP Population (All Patients)
NCT02083380 (32) [back to overview]PCR-adjusted ACPR at Day 28 in the PP Population: Africa (< = 5 Years)
NCT02083380 (32) [back to overview]PCR-adjusted ACPR at Day 28 in the PP Population: Africa (> Than 5 Years)
NCT02083380 (32) [back to overview]PCR-adjusted ACPR at Day 28 in the PP Population: Africa (>= 0.5 to <= 2 Years)
NCT02083380 (32) [back to overview]PCR-adjusted ACPR at Day 28 in the PP Population: Africa (>2 to <= 5 Years)
NCT02083380 (32) [back to overview]PCR-adjusted ACPR at Day 28 in the PP Population: Africa (All Ages)
NCT02083380 (32) [back to overview]PCR-adjusted ACPR at Day 28 in the PP Population: Asia (All Ages)
NCT02163447 (14) [back to overview]Number of Participants With One or More Birth Outcomes: Congenital Malformations, Spontaneous Abortion, LBW (<2500g), Still Birth, Pre-term Delivery
NCT02163447 (14) [back to overview]Prevalence of Anemia in Pregnant Women
NCT02163447 (14) [back to overview]Prevalence of Gametocytemia in Infants
NCT02163447 (14) [back to overview]Prevalence of Gametocytemia in Pregnant Women
NCT02163447 (14) [back to overview]Prevalence of Parasitemia at the Time of Monthly Routine Visits During Pregnancy
NCT02163447 (14) [back to overview]Prevalence of Parasitemia in Infants
NCT02163447 (14) [back to overview]Prevalence of Placental Malaria
NCT02163447 (14) [back to overview]Number of Participants With Blood Samples Positive for Parasites by Microscopy or LAMP
NCT02163447 (14) [back to overview]Number of Participants With Maternal Blood Samples Positive for Parasites by Microscopy and LAMP at Delivery
NCT02163447 (14) [back to overview]Incidence of Complicated Malaria in Infants
NCT02163447 (14) [back to overview]Incidence of Hospital Admissions in Infants
NCT02163447 (14) [back to overview]Incidence of Malaria in Infants
NCT02163447 (14) [back to overview]Incidence of Malaria in Infants
NCT02163447 (14) [back to overview]Incidence of Malaria in Pregnant Women
NCT02282293 (7) [back to overview]Incidence of Malaria, Pregnant Women
NCT02282293 (7) [back to overview]Number of Monthly Routine Visits With Positive Blood Samples for Parasites
NCT02282293 (7) [back to overview]Number of Participants With Placental Malaria
NCT02282293 (7) [back to overview]Number of Routine Visits Measured Every 8 Weeks During Pregnancy for Which the Participants Had Anemia
NCT02282293 (7) [back to overview]Maternal Parasitemia at Delivery by Microscopy and LAMP
NCT02282293 (7) [back to overview]Placental Parasitemia (Number of Women With Placental Blood Samples Positive for Malaria by Microscopy or PCR)
NCT02282293 (7) [back to overview]Composite Adverse Birth Outcome (Proportion With Low Birth Weight (<2500 gm), Spontaneous Abortion (<28 Weeks), Stillbirth (Fetal Demise ≥28 Weeks), Congenital Anomaly, or Preterm Delivery (<37 Weeks)
NCT02431637 (1) [back to overview]Safety: Number of AEs
NCT02793622 (14) [back to overview]Prevalence of Maternal Malaria
NCT02793622 (14) [back to overview]Prevalence of Placental Malaria by Histology
NCT02793622 (14) [back to overview]Prevalence of Placental Parasitemia
NCT02793622 (14) [back to overview]Incidence of Complicated Malaria in Infants
NCT02793622 (14) [back to overview]Incidence of Hospital Admissions in Infants
NCT02793622 (14) [back to overview]Incidence of Malaria in Infants
NCT02793622 (14) [back to overview]Infant Mortality Rate
NCT02793622 (14) [back to overview]Mean Gestational Age in Weeks at Birth
NCT02793622 (14) [back to overview]Number of Participants Who Deliver With a Composite Adverse Birth Outcome
NCT02793622 (14) [back to overview]Number of Participants With Adverse Events
NCT02793622 (14) [back to overview]Prevalence of Anemia in Infants
NCT02793622 (14) [back to overview]Prevalence of Anemia in Pregnant Women
NCT02793622 (14) [back to overview]Prevalence of Asymptomatic Parasitemia in Infants
NCT02793622 (14) [back to overview]Prevalence of Asymptomatic Parasitemia in Pregnant Women
NCT02802501 (20) [back to overview]Percentage of Participants With Relapse-free Efficacy at Four Months After Administration of Tafenoquine With DHA-PQP and DHA-PQP Alone
NCT02802501 (20) [back to overview]Number of Participants With Recrudescence
NCT02802501 (20) [back to overview]Number of Participants With Electrocardiogram (ECG) Values Outside Clinical Concern Range-QT Interval Corrected Using Fredericia's Formula (QTcF)
NCT02802501 (20) [back to overview]Percentage of Participants With Relapse-free Efficacy at Six Months After Administration of Tafenoquine With DHA-PQP and DHA-PQP Alone
NCT02802501 (20) [back to overview]Percentage of Participants With Relapse-free Efficacy at Six Months After Administration of Tafenoquine With DHA-PQP and Primaquine+DHA-PQP
NCT02802501 (20) [back to overview]Time to Fever Clearance
NCT02802501 (20) [back to overview]Time to Parasite Clearance
NCT02802501 (20) [back to overview]Time to Relapse of P. Vivax Malaria
NCT02802501 (20) [back to overview]Change From Baseline in Methemoglobin/ Total Hemoglobin
NCT02802501 (20) [back to overview]Change From Baseline in QT Interval Corrected by Fridericia's Formula (QTcF)
NCT02802501 (20) [back to overview]Number of Participants With Any Adverse Events (AEs) and Serious Adverse Events (SAEs) During the Double-blind Treatment Phase
NCT02802501 (20) [back to overview]Number of Participants With Chemistry Values Outside Clinical Concern Range
NCT02802501 (20) [back to overview]Number of Participants With Gastrointestinal AEs
NCT02802501 (20) [back to overview]Number of Participants With Hematology Values Outside Clinical Concern Range
NCT02802501 (20) [back to overview]Percentage of Participants With Relapse-free Efficacy at Six Months After Administration of Primaquine With DHA-PQP and DHA-PQP Alone
NCT02802501 (20) [back to overview]Number of Participants With Protocol-defined SAE (Hemoglobin Drop)
NCT02802501 (20) [back to overview]Number of Participants With Worst Case Body Temperature Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT02802501 (20) [back to overview]Number of Participants With Worst Case Pulse Rate Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT02802501 (20) [back to overview]Number of Participants With Worst Case Respiratory Rate Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT02802501 (20) [back to overview]Number of Participants With Worst Case Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT03454048 (8) [back to overview]AUC Gametocytes
NCT03454048 (8) [back to overview]Frequency of Adverse Events in the CHMI-trans Model
NCT03454048 (8) [back to overview]Gametocyte Commitment
NCT03454048 (8) [back to overview]Gametocyte Prevalence
NCT03454048 (8) [back to overview]Gametocyte Sex-ratio
NCT03454048 (8) [back to overview]Number of Participants Infectious for Mosquitoes Through DFA
NCT03454048 (8) [back to overview]Peak Density Gametocytes
NCT03454048 (8) [back to overview]Magnitude of Adverse Events in the CHMI-trans Model

Incident Malaria Cases Per Person Year at Risk in HIV-unexposed Participants

The incidence of malaria, defined as the number of incident episodes per time at risk, during the period the intervention was given (6-24 mo of age). Treatments within 14d of a prior episode were not considered incident events. Time at risk was from the day following the initiation of study drugs to the last day of observation, minus 14 d after each treatment for malaria. (NCT00948896)
Timeframe: 6 to 24 months of age

,,,
InterventionEpisode per person year at risk (Number)
6-24 mo. of Age6-11 mo. of Age12-24 mo. of Age
HIV-unexposed & Daily TS5.213.276.32
HIV-unexposed & Monthly DP3.021.493.88
HIV-unexposed & Monthly SP6.735.517.41
HIV-unexposed & no Chemoprevention6.956.417.24

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Incident Malaria Cases Per Person Year at Risk in HIV-exposed Participants

The primary outcome was the incidence of malaria, defined as the number of incident episodes per time at risk, during the period the intervention was given. Treatments within 14 days of a prior episode were not considered incident events. Time at risk was from the day following the initiation of study drugs to the last day of observation, minus 14 days after each treatment for malaria. (NCT00948896)
Timeframe: Randomization to 24 months of age

,,,
InterventionEpisodes per person year at risk (Number)
Randomization - 24 mo. of AgeRandomization -16 mo. of Age17-24 mo. of Age
HIV-exposed & Daily TS2.861.703.79
HIV-exposed & Monthly DP1.830.902.67
HIV-exposed & Monthly SP4.503.725.22
HIV-exposed & no Chemoprevention6.285.427.04

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Rebound Incidence of Malaria Defined as the Number of Treatments for New Episodes of Malaria Per Time at Risk

(NCT00948896)
Timeframe: 24 months to 36 months of age

,,,,,,,
InterventionIncidence per person year at risk (Number)
All incident episodes of malariaComplicated malariaAll-cause hospital admissions
HIV-exposed & Daily TS8.130.1160.186
HIV-exposed & Monthly DP6.780.0440.089
HIV-exposed & Monthly SP6.750.1470.318
HIV-exposed & no Chemoprevention9.080.1610.459
HIV-unexposed & Daily TS10.900.0460.091
HIV-unexposed & Monthly DP10.7700.023
HIV-unexposed & Monthly SP11.980.1320.452
HIV-unexposed & no Chemoprevention10.850.0460.046

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OZ439 AUC(0-168)

Area under the plasma concentration versus time curve to 168 hours post-dose. (NCT01660022)
Timeframe: Up to 168 hours post-dose

Interventionng.h/mL (Geometric Mean)
Cohort 1 - OZ439 100mg862
Cohort 1 - OZ439 100mg / PQP 160mg920
Cohort 2 - OZ439 100mg1130
Cohort 2 - OZ439 100mg / PQP 480mg1390
Cohort 3 - OZ439 100mg909
Cohort 3 - OZ439 100mg / PQP 1440mg1520
Cohort 4 - OZ439 300mg5740
Cohort 4 - OZ439 300mg / PQP 1440mg7410
Cohort 5 - OZ439 800mg15300
Cohort 5 - OZ439 800mg / PQP 1440mg18600

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OZ439 t1/2

OZ439 Elimination half-life (NCT01660022)
Timeframe: Up to 168 hours post-dose

Interventionhour (Geometric Mean)
Cohort 1 - OZ439 100mgNA
Cohort 1 - OZ439 100mg / PQP 160mgNA
Cohort 2 - OZ439 100mgNA
Cohort 2 - OZ439 100mg / PQP 480mgNA
Cohort 3 - OZ439 100mgNA
Cohort 3 - OZ439 100mg / PQP 1440mgNA
Cohort 4 - OZ439 300mg90.6
Cohort 4 - OZ439 300mg / PQP 1440mg112
Cohort 5 - OZ439 800mg65.4
Cohort 5 - OZ439 800mg / PQP 1440mg135

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Piperaquine t1/2

Piperaquine Elimination half-life (t1/2). (NCT01660022)
Timeframe: Up to 1008 hours post-dose (Day 43)

Interventionhour (Geometric Mean)
OZ439 100mg / PQP 160mg294
OZ439 100mg / PQP 480mg283
OZ439 100mg / PQP 1440mg515
OZ439 300mg / PQP 1440mg632
OZ439 800mg / PQP 1440mg509

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OZ439 Cmax

OZ439 Maximum concentration level (NCT01660022)
Timeframe: Up to 168 hours post-dose

Interventionng/mL (Geometric Mean)
Cohort 1 - OZ439 100mg142
Cohort 1 - OZ439 100mg / PQP 160mg139
Cohort 2 - OZ439 100mg146
Cohort 2 - OZ439 100mg / PQP 480mg198
Cohort 3 - OZ439 100mg127
Cohort 3 - OZ439 100mg / PQP 1440mg199
Cohort 4 - OZ439 300mg590
Cohort 4 - OZ439 300mg / PQP 1440mg778
Cohort 5 - OZ439 800mg1500
Cohort 5 - OZ439 800mg / PQP 1440mg1650

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Piperaquine AUC(0-168)

Piperaquine area under the plasma concentration versus time curve to 168 hours post-dose (NCT01660022)
Timeframe: Up to 1008 hours post-dose (Day 43)

Interventionng.h/mL (Geometric Mean)
OZ439 100mg / PQP 160mg1340
OZ439 100mg / PQP 480mg3420
OZ439 100mg / PQP 1440mg17500
OZ439 300mg / PQP 1440mg17200
OZ439 800mg / PQP 1440mg13200

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Piperaquine Cmax

Piperaquine Maximum concentration level (NCT01660022)
Timeframe: Up to 1008 hours post-dose (Day 43)

Interventionng/mL (Geometric Mean)
OZ439 100mg / PQP 160mg8.59
OZ439 100mg / PQP 480mg46.6
OZ439 100mg / PQP 1440mg393
OZ439 300mg / PQP 1440mg271
OZ439 800mg / PQP 1440mg356

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PCR-adjusted ACPR at Day 42 in the ITT Population

PCR-adjusted adequate clinical and parasitological response at Day 42 in the ITT population (NCT02083380)
Timeframe: Day 42

Intervention% ACPR PCR-adjusted (Number)
A) Artefenomel 800mg: Piperaquine 640mg46.9
B) Artefenomel 800mg: Piperaquine 960mg48.6
C) Artefenomel 800mg: Piperaquine 1440mg50.0

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PCR-adjusted ACPR at Day 63 in the ITT Population

PCR-adjusted adequate clinical and parasitological response at Day 63 in the ITT population (NCT02083380)
Timeframe: Day 63

Intervention% ACPR PCR-adjusted (Number)
A) Artefenomel 800mg: Piperaquine 640mg36.8
B) Artefenomel 800mg: Piperaquine 960mg38.6
C) Artefenomel 800mg: Piperaquine 1440mg43.7

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PCR-adjusted ACPR at Day 63 in the PP Population

PCR-adjusted adequate clinical and parasitological response at Day 63 (NCT02083380)
Timeframe: Day 63

Intervention% ACPR PCR-adjusted (Number)
A) Artefenomel 800mg: Piperaquine 640mg57.8
B) Artefenomel 800mg: Piperaquine 960mg58.9
C) Artefenomel 800mg: Piperaquine 1440mg69.0

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Piperaquine: Cday7 Africa (> 5 Years)

Piperaquine concentration at Day7 in African patients > 5 years (NCT02083380)
Timeframe: Day 7

Interventionng/mL (Geometric Mean)
A) Artefenomel 800mg: Piperaquine 640mg5.6
B) Artefenomel 800mg: Piperaquine 960mg8.8
C) Artefenomel 800mg: Piperaquine 1440mg12.1

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Piperaquine: Cday7 Africa (>=0.5 to <= 2 Years)

Piperaquine concentration at Day7 in African patients >= 0.5 and <= 2 years (NCT02083380)
Timeframe: Day 7

Interventionng/mL (Geometric Mean)
A) Artefenomel 800mg: Piperaquine 640mg5.0
B) Artefenomel 800mg: Piperaquine 960mg5.9
C) Artefenomel 800mg: Piperaquine 1440mg9.0

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Crude ACPR at Day 63 in the ITT Population

Crude adequate clinical and parasitological response at Day 63 in the ITT population (NCT02083380)
Timeframe: Day 63

Intervention% ACPR unadjusted (crude) (Number)
A) Artefenomel 800mg: Piperaquine 640mg36.8
B) Artefenomel 800mg: Piperaquine 960mg35.0
C) Artefenomel 800mg: Piperaquine 1440mg43.0

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Piperaquine: Cday7 Asia (All Ages)

Piperaquine concentration at Day7 in Asian patients all ages (NCT02083380)
Timeframe: Day 7

Interventionng/mL (Geometric Mean)
A) Artefenomel 800mg: Piperaquine 640mg4.2
B) Artefenomel 800mg: Piperaquine 960mg6.9
C) Artefenomel 800mg: Piperaquine 1440mg9.3

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PRR48

Parasite reduction ratio at 48 hours post dose (NCT02083380)
Timeframe: 0, 6, 12, 18, 24, 30, 36 and 48 hours post dose

Interventionratio (Median)
A) Artefenomel 800mg: Piperaquine 640mg9.120
B) Artefenomel 800mg: Piperaquine 960mg9.300
C) Artefenomel 800mg: Piperaquine 1440mg8.690

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Piperaquine: Cday7 Africa (>2 to <= 5 Years)

Piperaquine concentration at Day7 in African patients > 2 and <= 5years (NCT02083380)
Timeframe: Day 7

Interventionng/mL (Geometric Mean)
A) Artefenomel 800mg: Piperaquine 640mg6.3
B) Artefenomel 800mg: Piperaquine 960mg9.2
C) Artefenomel 800mg: Piperaquine 1440mg10.9

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Artefenomel Cday7 African Patients (> 5 Years)

Artefenomel concentration on Day 7 in African Patients > 5 years. All Treatment arms. (NCT02083380)
Timeframe: Day 7

Interventionng/mL (Geometric Mean)
A) Artefenomel 800mg: PQP 640mg, 960mg & 1440mg3.3

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Artefenomel Cday7 African Patients (>=0.5 to <= 2 Years)

Artefenomel concentration on Day 7 in African Patients >= 0.5 to <=2 years. All Treatment arms. (NCT02083380)
Timeframe: Day 7

Interventionng/mL (Geometric Mean)
A) Artefenomel 800mg: PQP 640mg, 960mg & 1440mg2.0

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Artefenomel Cday7 African Patients (>2 to <= 5 Years)

Artefenomel concentration on Day 7 in African Patients >2 to <= 5 years. All Treatment arms. (NCT02083380)
Timeframe: Day 7

Interventionng/mL (Geometric Mean)
A) Artefenomel 800mg: PQP 640mg, 960mg & 1440mg3.3

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Artefenomel Cday7 Asian Patients (All Ages)

Artefenomel concentration on Day 7 in Asian Patients (all ages). All Treatment arms. (NCT02083380)
Timeframe: Day 7

Interventionng/mL (Geometric Mean)
A) Artefenomel 800mg: PQP 640mg, 960mg & 1440mg5.1

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Crude ACPR at Day 28 in the ITT Population

Crude adequate clinical and parasitological response at Day 28 in the ITT population (NCT02083380)
Timeframe: Day 28

Intervention% ACPR unadjusted (crude) (Number)
A) Artefenomel 800mg: Piperaquine 640mg53.1
B) Artefenomel 800mg: Piperaquine 960mg53.4
C) Artefenomel 800mg: Piperaquine 1440mg63.0

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Crude ACPR at Day 28 in the PP Population

Crude adequate clinical and parasitological response at Day 28 (NCT02083380)
Timeframe: Day 28

Intervention% ACPR unadjusted (crude) (Number)
A) Artefenomel 800mg: Piperaquine 640mg57.4
B) Artefenomel 800mg: Piperaquine 960mg56.6
C) Artefenomel 800mg: Piperaquine 1440mg66.9

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Crude ACPR at Day 42 in the ITT Population

Crude adequate clinical and parasitological response at Day 42 in the ITT population (NCT02083380)
Timeframe: Day 42

Intervention% ACPR unadjusted (crude) (Number)
A) Artefenomel 800mg: Piperaquine 640mg44.1
B) Artefenomel 800mg: Piperaquine 960mg44.6
C) Artefenomel 800mg: Piperaquine 1440mg46.6

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Crude ACPR at Day 42 in the PP Population

Crude adequate clinical and parasitological response at Day 42 (NCT02083380)
Timeframe: Day 42

Intervention% ACPR unajusted (crude) (Number)
A) Artefenomel 800mg: Piperaquine 640mg48.0
B) Artefenomel 800mg: Piperaquine 960mg48.5
C) Artefenomel 800mg: Piperaquine 1440mg51.5

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Crude ACPR at Day 63 in the PP Population

Crude adequate clinical and parasitological response at Day 63 (NCT02083380)
Timeframe: Day 63

Intervention% ACPR unadjusted (crude) (Number)
A) Artefenomel 800mg: Piperaquine 640mg42.1
B) Artefenomel 800mg: Piperaquine 960mg39.3
C) Artefenomel 800mg: Piperaquine 1440mg49.1

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Fever Clearance Time

Time to fever clearance (hours) (NCT02083380)
Timeframe: Day 42

Interventionhours (Median)
A) Artefenomel 800mg: Piperaquine 640mg1.0
B) Artefenomel 800mg: Piperaquine 960mg1.2
C) Artefenomel 800mg: Piperaquine 1440mg1.1

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Kaplan-Meier Estimate of New Infection Rate

Kaplan-Meier estimate of number of patients with new infections (NCT02083380)
Timeframe: Day 63

Intervention% population with new infection (Number)
A) Artefenomel 800mg: Piperaquine 640mg11.3
B) Artefenomel 800mg: Piperaquine 960mg16.3
C) Artefenomel 800mg: Piperaquine 1440mg13.6

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Kaplan-Meier Estimate of Recrudescence

Kaplan-Meier estimate of number of patients with recrudescence (NCT02083380)
Timeframe: Day 63

Intervention% patients with recrudescence (Number)
A) Arttefenomel 800mg: Piperaquine 640mg22.7
B) Artefenomel 800mg: Piperaquine 960mg29.1
C) Artefenomel 800mg: Piperaquine 1440mg18.6

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Kaplan-Meier Estimate of Recurrence

Kaplan-Meier estimate of number of recurrent infections (either recrudescence or new infection) (NCT02083380)
Timeframe: Day 63

Intervention% population recurring (Number)
A) Artefenomel 800mg: Piperaquine 640mg44.7
B) Artefenomel 800mg: Piperaquine 960mg54.6
C) Artefenomel 800mg: Piperaquine 1440mg43.6

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Parasite Clearance Time

Time post dose to parasite clearance (NCT02083380)
Timeframe: 0, 6, 12, 18, 24, 30, 36, 48 and 72 hours post dose

Interventionhours (Median)
A) Artefenomel 800mg: Piperaquine 640mg36.1
B) Artefenomel 800mg: Piperaquine 960mg36.0
C) Artefenomel 800mg: Piperaquine 1440mg36.1

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PCR - Adjusted ACPR at Day 42 in the PP Population

PCR - adjusted adequate clinical and parasitological response at Day 42 (NCT02083380)
Timeframe: Days 42

Intervention% ACPR PCR-adjusted (Number)
A) Artefenomel 800mg: Piperaquine 640mg65.0
B) Artefenomel 800mg: Piperaquine 960mg65.7
C) Artefenomel 800mg: Piperaquine 1440mg72.0

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PCR-adjusted ACPR at Day 28 in the ITT Population

PCR-adjusted adequate clinical and parasitological response at Day 28. Intent to Treat ( ITT) population. (NCT02083380)
Timeframe: Day 28

Intervention% ACPR PCR-adjusted (Number)
A) Artefenomel 800mg: Piperaquine 640mg53.8
B) Artefenomel 800mg: Piperaquine 960mg55.4
C) Artefenomel 800mg: Piperaquine 1440mg65.1

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PCR-adjusted ACPR at Day 28 in the PP Population (All Patients)

"Polymerase chain reaction (PCR)-adjusted adequate clinical and parasitological response (ACPR) at Day 28: defined as: absence of parasitaemia on Day 28, irrespective of axillary temperature, in patients who did not previously meet any of the criteria of early treatment failure (ETF), late clinical failure (LCF) or late parasitological failure (LPF). Definition of ETF, LCF and LPF according to a modified standard WHO classification. Per protocol population (PP).~95% Clopper-Pearson 2-sided Confidence Interval (CI) constructed around the single binomial proportion per treatment arm and total." (NCT02083380)
Timeframe: Day 28

Intervention% ACPR PCR-adjusted (Number)
A) Artefenomel 800mg: Piperaquine 640mg70.8
B) Artefenomel 800mg: Piperaquine 960mg68.4
C) Artefenomel 800mg: Piperaquine 1440mg78.6

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PCR-adjusted ACPR at Day 28 in the PP Population: Africa (< = 5 Years)

"PCR-adjusted adequate clinical and parasitological response (ACPR) at Day 28: defined as: absence of parasitaemia on Day 28, irrespective of axillary temperature, in patients who did not previously meet any of the criteria of early treatment failure (ETF), late clinical failure (LCF) or late parasitological failure (LPF). Definition of ETF, LCF and LPF according to a modified standard WHO classification.~95% Clopper-Pearson 2-sided CI constructed around the single binomial proportion per treatment arm and total." (NCT02083380)
Timeframe: Day 28

Intervention% ACPR PCR-adjusted (Number)
A) Artefenomel 800mg: Piperaquine 640mg71.4
B) Artefenomel 800mg: Piperaquine 960mg63.4
C) Artefenomel 800mg: Piperaquine 1440mg78.9

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PCR-adjusted ACPR at Day 28 in the PP Population: Africa (> Than 5 Years)

"PCR-adjusted adequate clinical and parasitological response (ACPR) at Day 28: defined as: absence of parasitaemia on Day 28, irrespective of axillary temperature, in patients who did not previously meet any of the criteria of early treatment failure (ETF), late clinical failure (LCF) or late parasitological failure (LPF). Definition of ETF, LCF and LPF according to a modified standard WHO classification.~95% Clopper-Pearson 2-sided CI constructed around the single binomial proportion per treatment arm and total." (NCT02083380)
Timeframe: Day 28

Intervention% ACPR PCR-adjusted (Number)
A) Artefenomel 800mg: Piperaquine 640mg77.8
B) Artefenomel 800mg: Piperaquine 960mg90.5
C) Artefenomel 800mg: Piperaquine 1440mg89.5

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PCR-adjusted ACPR at Day 28 in the PP Population: Africa (>= 0.5 to <= 2 Years)

"PCR-adjusted adequate clinical and parasitological response (ACPR) at Day 28: defined as: absence of parasitaemia on Day 28, irrespective of axillary temperature, in patients who did not previously meet any of the criteria of early treatment failure (ETF), late clinical failure (LCF) or late parasitological failure (LPF). Definition of ETF, LCF and LPF according to a modified standard WHO classification.~95% Clopper-Pearson 2-sided CI constructed around the single binomial proportion per treatment arm and total." (NCT02083380)
Timeframe: Day 28

Intervention% ACPR PCR-adjusted (Number)
A) Artefenomel 800mg: Piperaquine 640mg61.1
B) Artefenomel 800mg: Piperaquine 960mg38.1
C) Artefenomel 800mg: Piperaquine 1440mg62.5

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PCR-adjusted ACPR at Day 28 in the PP Population: Africa (>2 to <= 5 Years)

"PCR-adjusted adequate clinical and parasitological response (ACPR) at Day 28: defined as: absence of parasitaemia on Day 28, irrespective of axillary temperature, in patients who did not previously meet any of the criteria of early treatment failure (ETF), late clinical failure (LCF) or late parasitological failure (LPF). Definition of ETF, LCF and LPF according to a modified standard WHO classification.~95% Clopper-Pearson 2-sided CI constructed around the single binomial proportion per treatment arm and total." (NCT02083380)
Timeframe: Day 28

Intervention% ACPR PCR-adjusted (Number)
A) Artefenomel 800mg: Piperaquine 640mg75.6
B) Artefenomel 800mg: Piperaquine 960mg74.0
C) Artefenomel 800mg: Piperaquine 1440mg83.6

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PCR-adjusted ACPR at Day 28 in the PP Population: Africa (All Ages)

"PCR-adjusted adequate clinical and parasitological response (ACPR) at Day 28: defined as: absence of parasitaemia on Day 28, irrespective of axillary temperature, in patients who did not previously meet any of the criteria of early treatment failure (ETF), late clinical failure (LCF) or late parasitological failure (LPF). Definition of ETF, LCF and LPF according to a modified standard WHO classification.~95% Clopper-Pearson 2-sided CI constructed around the single binomial proportion per treatment arm and total." (NCT02083380)
Timeframe: Day 28

Intervention% ACPR PCR-adjusted (Number)
A) Artefenomel 800mg: Piperaquine 640mg72.8
B) Artefenomel 800mg: Piperaquine 960mg69.6
C) Artefenomel 800mg: Piperaquine 1440mg81.1

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PCR-adjusted ACPR at Day 28 in the PP Population: Asia (All Ages)

"PCR-adjusted adequate clinical and parasitological response (ACPR) at Day 28: defined as: absence of parasitaemia on Day 28, irrespective of axillary temperature, in patients who did not previously meet any of the criteria of early treatment failure (ETF), late clinical failure (LCF) or late parasitological failure (LPF). Definition of ETF, LCF and LPF according to a modified standard WHO classification.~95% Clopper-Pearson 2-sided CI constructed around the single binomial proportion per treatment arm and total." (NCT02083380)
Timeframe: Day 28

Intervention% ACPR PCR-adjusted (Number)
A) Artefenomel 800mg: Piperaquine 640mg64
B) Artefenomel 800mg: Piperaquine 960mg64
C) Artefenomel 800mg: Piperaquine 1440mg70.4

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Number of Participants With One or More Birth Outcomes: Congenital Malformations, Spontaneous Abortion, LBW (<2500g), Still Birth, Pre-term Delivery

Congenital malformations, spontaneous abortion, LBW (<2500g), still birth, pre-term delivery (NCT02163447)
Timeframe: Delivery

InterventionParticipants (Count of Participants)
Mothers - 3 Dose SP19
Mothers - 3 Dose DP19
Mothers - Monthly DP9

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Prevalence of Anemia in Pregnant Women

Prevalence of routine hemoglobin measurements < 11 g/dL (NCT02163447)
Timeframe: After first dose of study drugs up to delivery or early termination

Interventionhemoglobin measurements taken every 12wk (Number)
Mothers - 3 Dose SP94
Mothers - 3 Dose DP72
Mothers - Monthly DP61

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Prevalence of Gametocytemia in Infants

Proportion of routine blood smears positive for gametocytes (NCT02163447)
Timeframe: Birth up to 24 months of age or early study termination

InterventionPositive blood smears (Number)
3 Dose SP Pregnancy / 3 Monthly DP Infancy7
3 Dose DP Pregnancy / 3 Monthly DP Infancy1
3 Dose DP Pregnancy / Monthly DP Infancy0
Monthly DP Pregnancy / 3 Monthly DP Infancy4
Monthly DP Pregnancy / Monthly DP Infancy0

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Prevalence of Gametocytemia in Pregnant Women

Proportion of urgent blood smears positive for gametocytes (NCT02163447)
Timeframe: Gestational age between 12-20 weeks (at study entry) up to delivery

InterventionPositive blood smears (Number)
Mothers - 3 Dose SP4
Mothers - 3 Dose DP1
Mothers - Monthly DP3

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Prevalence of Parasitemia at the Time of Monthly Routine Visits During Pregnancy

Detection of malaria parasites by LAMP during pregnancy (NCT02163447)
Timeframe: After first dose of study drug through delivery or early termination

InterventionPositive specimens (Number)
Mothers - 3 Dose SP206
Mothers - 3 Dose DP74
Mothers - Monthly DP26

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Prevalence of Parasitemia in Infants

Proportion of routine monthly samples positive for parasites by LAMP. Proportion of routine samples (LAMP or blood smears) positive for asexual parasites. (NCT02163447)
Timeframe: Birth up to 24 months of age or early study termination

InterventionPositive blood smears (Number)
3 Dose SP Pregnancy / 3 Monthly DP Infancy59
3 Dose DP Pregnancy / 3 Monthly DP Infancy25
3 Dose DP Pregnancy / Monthly DP Infancy7
Monthly DP Pregnancy / 3 Monthly DP Infancy52
Monthly DP Pregnancy / Monthly DP Infancy4

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Prevalence of Placental Malaria

Prevalence of placental malaria based on placental histopathology dichotomized into any evidence of placental infection (parasites or pigment) vs. no evidence and by histopathology as a categorical variable based on Rogerson et al criteria. (NCT02163447)
Timeframe: Delivery

InterventionParticipants (Count of Participants)
Mothers - 3 Dose SP49
Mothers - 3 Dose DP30
Mothers - Monthly DP26

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Number of Participants With Blood Samples Positive for Parasites by Microscopy or LAMP

Prevalence of placental blood samples positive for parasites by microscopy or LAMP (NCT02163447)
Timeframe: Delivery

,,
InterventionParticipants (Count of Participants)
Micropscopic assessment of placental bloodLAMP assessment of placental blood
Mothers - 3 Dose DP33
Mothers - 3 Dose SP519
Mothers - Monthly DP02

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Number of Participants With Maternal Blood Samples Positive for Parasites by Microscopy and LAMP at Delivery

Prevalence of maternal parasitemia at delivery by microscopy and LAMP (NCT02163447)
Timeframe: At delivery

,,
Interventionparticipants (Number)
MicroscopyLAMP
Mothers - 3 Dose DP13
Mothers - 3 Dose SP525
Mothers - Monthly DP01

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Incidence of Complicated Malaria in Infants

Any treatment for malaria meeting criteria for severe malaria or danger signs (NCT02163447)
Timeframe: Birth up to 24 months of age or early study termination

InterventionEvents per person years (Number)
3 Dose SP Pregnancy / 3 Monthly DP Infancy0.022
3 Dose DP Pregnancy / 3 Monthly DP Infancy0.024
3 Dose DP Pregnancy / Monthly DP Infancy0.000
Monthly DP Pregnancy / 3 Monthly DP Infancy0.035
Monthly DP Pregnancy / Monthly DP Infancy0.000

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Incidence of Hospital Admissions in Infants

Admission to a hospital for pediatric inpatient care for any reason (NCT02163447)
Timeframe: Birth up to 24 months of age or early study termination

InterventionEvents per person years (Number)
3 Dose SP Pregnancy / 3 Monthly DP Infancy0.043
3 Dose DP Pregnancy / 3 Monthly DP Infancy0.036
3 Dose DP Pregnancy / Monthly DP Infancy0.089
Monthly DP Pregnancy / 3 Monthly DP Infancy0.082
Monthly DP Pregnancy / Monthly DP Infancy0.043

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Incidence of Malaria in Infants

Incident cases will include all treatments for malaria not proceeded by another treatment in the previous 14 days. The study investigators will test the hypotheses that A) infants born to mothers randomized to receive IPTp with 3 dose DP or monthly DP will have a lower incidence of malaria during the first 24 months of life compared to infants born to mothers who were randomized to receive IPTp with 3 doses of SP, and, B) infants randomized to receive monthly DP between 2-24 months of age will have a lower incidence of malaria between 24-36 months of age after the intervention is stopped compared to infants randomized q 3 monthly DP between 2-24 months of age. (NCT02163447)
Timeframe: Time at risk will begin at 24 months of age and will end when study participants reaches 36 months of age or termination

InterventionEvents per person years (Number)
3 Dose SP Pregnancy / 3 Monthly DP Infancy0.87
3 Dose DP Pregnancy / 3 Monthly DP Infancy0.88
3 Dose DP Pregnancy / Monthly DP Infancy0.83
Monthly DP Pregnancy / 3 Monthly DP Infancy1.24
Monthly DP Pregnancy / Monthly DP Infancy0.64

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Incidence of Malaria in Infants

Incident cases will include all treatments for malaria not proceeded by another treatment in the previous 14 days. The study investigators will test the hypotheses that A) infants born to mothers randomized to receive IPTp with 3 dose DP or monthly DP will have a lower incidence of malaria during the first 24 months of life compared to infants born to mothers who were randomized to receive IPTp with 3 doses of SP, and, B) infants randomized to receive monthly DP between 2-24 months of age will have a lower incidence of malaria between 24-36 months of age after the intervention is stopped compared to infants randomized q 3 monthly DP between 2-24 months of age. (NCT02163447)
Timeframe: Time at risk will begin at birth and will end when study participants reaches 24 months of age or early study termination (if prior to 24 months of age)

InterventionEvents per person years (Number)
3 Dose SP Pregnancy / 3 Monthly DP Infancy0.26
3 Dose DP Pregnancy / 3 Monthly DP Infancy0.30
3 Dose DP Pregnancy / Monthly DP Infancy0.00
Monthly DP Pregnancy / 3 Monthly DP Infancy0.43
Monthly DP Pregnancy / Monthly DP Infancy0.03

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Incidence of Malaria in Pregnant Women

Incidence of malaria, defined as the number of incident episodes per time at risk. Incident cases will include all treatments for malaria not proceeded by another treatment in the previous 14 days. (NCT02163447)
Timeframe: Time at risk will begin after first dose of study drug and will end when study participants deliver or early study termination

Interventionevents per person years (Number)
Mothers - 3 Dose SP0.95
Mothers - 3 Dose DP0.31
Mothers - Monthly DP0

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Incidence of Malaria, Pregnant Women

The primary outcome will be the incidence of malaria, defined as the number of incident episodes per time at risk. Incident cases will include all treatments for malaria not proceeded by another treatment in the previous 14 days. (NCT02282293)
Timeframe: Time at risk will begin following administration of first dose of study drug to delivery

InterventionEvents per person-year (Number)
TS + DP Placebo Pregnancy0.03
Daily TS + Monthly DP Pregnancy0.00

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Number of Monthly Routine Visits With Positive Blood Samples for Parasites

Proportion of monthly routine blood samples positive by LAMP for parasites (NCT02282293)
Timeframe: Following administration of first dose of study drug to delivery

Interventionvisits with positive blood sample (Count of Units)
TS + DP Placebo Pregnancy12
Daily TS + Monthly DP Pregnancy5

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Number of Participants With Placental Malaria

The primary outcome will be the prevalence of placental malaria based on placental histopathology and dichotomized into any evidence of placental infection (parasites or pigment) vs. no evidence of placental infection. (NCT02282293)
Timeframe: at delivery estimated to be within 10 to 30 weeks of study entry

InterventionParticipants (Count of Participants)
TS + DP Placebo Pregnancy3
Daily TS + Monthly DP Pregnancy6

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Number of Routine Visits Measured Every 8 Weeks During Pregnancy for Which the Participants Had Anemia

Anemia (hemoglobin less than 11g/dL) measured every 8 weeks during pregnancy (NCT02282293)
Timeframe: Following administration of first dose of study drugs to delivery

InterventionRoutine visit done every 8 weeks (Count of Units)
TS + DP Placebo Pregnancy65
Daily TS + Monthly DP Pregnancy51

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Maternal Parasitemia at Delivery by Microscopy and LAMP

Proportion of women with parasitemia detected by microscopy or LAMP at delivery (NCT02282293)
Timeframe: At delivery

,
InterventionParticipants (Count of Participants)
MicroscopyLAMP
Daily TS + Monthly DP Pregnancy14
TS + DP Placebo Pregnancy02

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Placental Parasitemia (Number of Women With Placental Blood Samples Positive for Malaria by Microscopy or PCR)

Proportion of placental blood samples positive for malaria by microscopy or PCR (NCT02282293)
Timeframe: At delivery

,
InterventionParticipants (Count of Participants)
Microscopy of placental bloodLAMP analysis of placental blood
Daily TS + Monthly DP Pregnancy13
TS + DP Placebo Pregnancy01

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Composite Adverse Birth Outcome (Proportion With Low Birth Weight (<2500 gm), Spontaneous Abortion (<28 Weeks), Stillbirth (Fetal Demise ≥28 Weeks), Congenital Anomaly, or Preterm Delivery (<37 Weeks)

Proportion with low birth weight (<2500 gm), spontaneous abortion (<28 weeks), stillbirth (fetal demise ≥28 weeks), congenital anomaly, or preterm delivery (<37 weeks) (NCT02282293)
Timeframe: At delivery

InterventionParticipants (Count of Participants)
TS + DP Placebo Pregnancy15
Daily TS + Monthly DP Pregnancy20

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Safety: Number of AEs

Adverse events incidence (NCT02431637)
Timeframe: Blood stage Plasmodium falciparum Challenge Inoculum up to Day 31

InterventionNumber of adverse events (Number)
Piperaquine Phosphate After Infected Blood Malaria Challenge40

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Prevalence of Maternal Malaria

Maternal blood positive for malaria parasites by microscopy. (NCT02793622)
Timeframe: Gestational age between 12-20 weeks (at study entry) up to delivery

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy28
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy1

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Prevalence of Placental Malaria by Histology

Any evidence of placental infection (parasites or pigment). Number of participants with placental tissue positive for malaria parasites or pigment. (NCT02793622)
Timeframe: Delivery

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy197
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy94

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Prevalence of Placental Parasitemia

Proportion of placental blood samples positive for parasites by Loop-mediated isothermal amplification (LAMP) or microscopy (NCT02793622)
Timeframe: Delivery

,
InterventionParticipants (Count of Participants)
LAMPMicroscopy
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy71
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy7129

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Incidence of Complicated Malaria in Infants

Complicated malaria defined as an episode of malaria with danger signs (any of the following: less than 3 convulsions over 24 h, inability to sit or stand, vomiting everything, unable to breastfeed or drink) or the meeting standardized criteria for severe malaria. (NCT02793622)
Timeframe: Birth up to 12 months of age or early termination

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy44
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy24

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Incidence of Hospital Admissions in Infants

Admission to the pediatric ward for any cause (NCT02793622)
Timeframe: Birth up to 12 months of age or early termination

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy19
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy8

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Incidence of Malaria in Infants

episodes per person year (NCT02793622)
Timeframe: Time at risk will begin at birth and end when study participants reaches 12 months of age or early study termination

Interventionepisodes per person year (Number)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy1.98
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy1.71

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Infant Mortality Rate

Any deaths occurring after birth (NCT02793622)
Timeframe: Birth up to 12 months of age

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy9
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy7

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Mean Gestational Age in Weeks at Birth

Gestational age in weeks determined by ultrasound dating (gold standard) and by the metabolic profiling outcome from biological specimens including placental tissue and placental blood. (NCT02793622)
Timeframe: At the time of delivery

Interventionweeks (Mean)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy39.4
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy39.6

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Number of Participants Who Deliver With a Composite Adverse Birth Outcome

Composite adverse birth outcome defined as any one of the following: 1) Low birth weight (< 2500 gm); 2) Preterm delivery (< 37 weeks gestational age); 3) Small for gestational age (< 10th percentile relative to an external growth reference) (NCT02793622)
Timeframe: Delivery

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy60
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy54

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Number of Participants With Adverse Events

All grade 3 and 4 adverse events (NCT02793622)
Timeframe: Starting at the time of their first study drug administration, approximately gestational age between 12-20 weeks, up to one month post-delivery

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy54
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy43

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Prevalence of Anemia in Infants

"Defined as the proportion with hemoglobin < 10 g/dL measure routinely at 12, 28, and 52 weeks of age. Number of cases per person year (PPY).~This is a prevalence measure but are repeated measures during infancy. In other words we measured this outcome up to 3 times for each participant during infancy (at 12, 28 and 52 weeks of age)." (NCT02793622)
Timeframe: Birth up to 12 months of age or early termination

Interventionroutine hemoglobin measurement (Count of Units)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy222
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy216

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Prevalence of Anemia in Pregnant Women

hemoglobin < 11 g/dL (NCT02793622)
Timeframe: Starting at the time of their first study drug administration, approximately gestational age between 12-20 weeks, up to one month post-delivery

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy28
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy8

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Prevalence of Asymptomatic Parasitemia in Infants

Proportion of routine monthly samples positive for parasites by microscopy and LAMP (NCT02793622)
Timeframe: Birth up to 12 months of age or early termination

Interventionblood smears (Count of Units)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy344
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy357

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Prevalence of Asymptomatic Parasitemia in Pregnant Women

Proportion of routine monthly samples positive for parasites by microscopy and LAMP (NCT02793622)
Timeframe: Starting at the time of their first study drug administration, approximately gestational age between 12-20 weeks, up to one month post-delivery

Interventionblood smears (Count of Units)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy519
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy9

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Percentage of Participants With Relapse-free Efficacy at Four Months After Administration of Tafenoquine With DHA-PQP and DHA-PQP Alone

A participant was considered to have demonstrated recurrence-free efficacy at 4 months if: a) Participant had non-zero P. vivax asexual parasite count at Baseline, b) Participant demonstrated initial clearance of P.vivax parasitemia, c) Participant had no positive asexual P.vivax parasite count at any assessment prior to or on Study Day 135 following initial parasite clearance, d) Participants did not take a concomitant medication with anti-malarial activity (excluding study treatment) at any point between Study Day 1 and their first parasite assessment after Study Day 105 (up to and including Study Day 135), e) Participant was parasite-free at 4 months. The rate of relapse-free efficacy was estimated by Kaplan-Meier methodology. The percentage of participants who were relapse-free at 4 months post dose has been presented. (NCT02802501)
Timeframe: 4 months post-dose

InterventionPercentage of participants (Number)
DHA-PQP Only16
Tafenoquine+ DHA-PQP28

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Number of Participants With Recrudescence

Recrudescence was defined as blood stage treatment failure. A participant was considered to have had a recrudescence if both of the following were true: 1) if participant had a positive P. vivax asexual parasite count at Baseline and demonstrated clearance (i.e. two negative asexual P. vivax parasite counts, with at least 6 hours between the counts, and no positive counts in the interval); 2) Participant had a positive genetically homologous asexual P. vivax parasite count on or before Study Day 14, after their zero count in days 1 to 5. (NCT02802501)
Timeframe: Up to Day 14

InterventionParticipants (Count of Participants)
DHA-PQP Only0
Tafenoquine+ DHA-PQP0
Primaquine+DHA-PQP0

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Number of Participants With Electrocardiogram (ECG) Values Outside Clinical Concern Range-QT Interval Corrected Using Fredericia's Formula (QTcF)

12-lead ECG was obtained at indicated time points using an automated ECG machine that measured QTcF. Clinical concern range included:absolute QTcF interval (upper: >480 milliseconds) and increase from Baseline in QTcF (upper: >=60 milliseconds). Data for maximum post-Baseline increase >=60 and >480 milliseconds has been presented. (NCT02802501)
Timeframe: Up to Day 28

InterventionParticipants (Count of Participants)
DHA-PQP Only2
Tafenoquine+ DHA-PQP3
Primaquine+DHA-PQP1

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Percentage of Participants With Relapse-free Efficacy at Six Months After Administration of Tafenoquine With DHA-PQP and DHA-PQP Alone

A participant was considered to have demonstrated relapse-free efficacy at 6 months if: a) Participant had non-zero Plasmodium vivax (P.vivax) asexual parasite count at Baseline (Day 1), b) Participant demonstrated initial clearance of P.vivax parasitemia, c) Participant had no positive asexual P.vivax parasite count at any assessment prior to or on study Day 180 following initial parasite clearance, d) Participants did not take a concomitant medication with anti-malarial activity (excluding study treatment) at any point between Study Day 1 and their last parasite assessment, e) Participant was parasite-free at 6 months. The percentage of participants who were relapse-free at 6 months post dose has been presented. (NCT02802501)
Timeframe: 6 months post-dose

InterventionPercentage of participants (Number)
DHA-PQP Only12
Tafenoquine+ DHA-PQP22

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Percentage of Participants With Relapse-free Efficacy at Six Months After Administration of Tafenoquine With DHA-PQP and Primaquine+DHA-PQP

A participant was considered to have demonstrated relapse-free efficacy at 6 months if: a) Participant had non-zero P. vivax asexual parasite count at Baseline (Day 1), b) Participant demonstrated initial clearance of P.vivax parasitemia, c) Participant had no positive asexual P.vivax parasite count at any assessment prior to or on study Day 180 following initial parasite clearance, d) Participants did not take a concomitant medication with anti-malarial activity (excluding study treatment) at any point between Study Day 1 and their last parasite assessment, e) Participant was parasite-free at 6 months. The percentage of participants who were relapse-free at 6 months post dose has been presented. (NCT02802501)
Timeframe: 6 months post-dose

InterventionPercentage of participants (Number)
Tafenoquine+ DHA-PQP22
Primaquine+DHA-PQP52

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Time to Fever Clearance

Time to fever clearance is defined as time from first dose of treatment to the time when body temperature falls to normal and remains normal for at least 48 hours up to the Day 7 visit. Fever clearance is considered to have been achieved once an initial temperature of greater than 37.4 degree Celsius is reduced to a value less than or equal to 37.4 degree Celsius, in the absence of value greater than 37.4 degree Celsius in the following 48 hours up to Day 7 visit. The time taken to achieve fever clearance was analyzed by Kaplan-Meier method. (NCT02802501)
Timeframe: Up to Day 7

InterventionHours (Median)
DHA-PQP Only16.5
Tafenoquine+ DHA-PQP15.8
Primaquine+DHA-PQP16.8

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Time to Parasite Clearance

Parasite clearance time is defined as time needed to clear asexual parasite from the blood that is, parasite numbers falling below the limit of detection in the thick blood smear and remaining undetectable after >= 6 hours later. The time to achieve parasite clearance was analyzed by Kaplan-Meier method. (NCT02802501)
Timeframe: Up to Day 8

InterventionHours (Median)
DHA-PQP Only18.1
Tafenoquine+ DHA-PQP18.1
Primaquine+DHA-PQP18.0

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Time to Relapse of P. Vivax Malaria

Relapse is defined by a positive blood smear with or without vivax symptoms. Relapse is described as any recurrence of P. vivax malaria after clearance of the initial infection. The time to relapse (number of days between the date of first positive count and date of Study Day 1) was analyzed by the Kaplan-Meier method. The median number of days to relapse along with 95 percent (%) confidence interval (CI) has been presented for each treatment group. (NCT02802501)
Timeframe: Up to Day 180

InterventionDays (Median)
DHA-PQP Only81.5
Tafenoquine+ DHA-PQP96.0
Primaquine+DHA-PQPNA

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Change From Baseline in Methemoglobin/ Total Hemoglobin

Blood samples were collected for the assessment of methemoglobin/Total Hemoglobin (Hb). Methemoglobin is a type of Hb in the form of metalloprotein that cannot bind with oxygen, measured as percentage of methemoglobin in total hemoglobin. Change from Baseline is calculated as Post-Dose Visit Value minus Baseline value. Day 1 was considered as Baseline. (NCT02802501)
Timeframe: Baseline (Day 1) and Days 2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,18,20,21,22,24,26,28 and 60

,,
InterventionPercentage of Methemoglobin in total Hb (Mean)
Day 2, n=48, 50, 50Day 3, n=48, 50, 50Day 4, n=48, 50, 50Day 5, n=48, 50, 50Day 6, n=46, 49, 50Day 7, n=48, 50, 50Day 8, n=46, 48, 48Day 9, n=46, 47, 47Day 10, n=47, 45, 49Day 11, n=47, 44, 49Day 12, n=47, 47, 50Day 13, n=48, 48, 48Day 14, n=48, 50, 50Day 15, n=17, 22, 14Day 16, n=43, 48, 47Day 18, n=46, 48, 49Day 20, n=42, 49, 48Day 21, n=43, 48, 48Day 22, n=45, 49, 48Day 24, n=41, 46, 47Day 26, n=44, 45, 47Day 28, n=47, 50, 50Day 60, n=47, 50, 49
DHA-PQP Only-0.13-0.16-0.16-0.18-0.15-0.19-0.12-0.13-0.16-0.13-0.13-0.14-0.18-0.08-0.12-0.12-0.09-0.07-0.13-0.11-0.17-0.15-0.11
Primaquine+DHA-PQP-0.060.010.280.620.911.201.411.531.691.821.922.022.012.131.841.290.800.690.490.410.190.08-0.01
Tafenoquine+ DHA-PQP-0.07-0.040.060.120.160.190.230.240.240.180.180.180.120.000.120.110.060.030.010.030.030.01-0.07

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Change From Baseline in QT Interval Corrected by Fridericia's Formula (QTcF)

12-lead ECG was obtained at indicated time points using an automated ECG machine that measured QTcF interval. Change from Baseline is calculated as Post-Dose Visit Value minus Baseline value. Day 1 was considered as Baseline. (NCT02802501)
Timeframe: Baseline (Day 1), Day 3: 4 hours post DHA-PQP dose, Days 7 and 28

,,
InterventionMilliseconds (Mean)
Day 3: 4 hours post DHA-PQP doseDay 7Day 28
DHA-PQP Only35.311.52.4
Primaquine+DHA-PQP40.816.510.2
Tafenoquine+ DHA-PQP44.512.27.5

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Number of Participants With Any Adverse Events (AEs) and Serious Adverse Events (SAEs) During the Double-blind Treatment Phase

An AE is any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. A SAE is defined as as any untoward medical occurrence that, at any dose results in death, is life-threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, is a congenital anomaly/birth defect, is associated with liver injury and impaired liver function, other important medical events that may jeopardize the participant or may require medical or surgical intervention to prevent one of the other outcomes listed before. (NCT02802501)
Timeframe: Up to Day 180

,,
InterventionParticipants (Count of Participants)
Any AEsAny SAEs
DHA-PQP Only411
Primaquine+DHA-PQP342
Tafenoquine+ DHA-PQP412

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Number of Participants With Chemistry Values Outside Clinical Concern Range

Blood samples were collected at indicated time points to analyze following chemistry parameters: alanine aminotransferase (ALT), Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST), Bilirubin, Creatine Kinase, Creatinine, Indirect Bilirubin and Urea. Clinical concern range for the parameters included ALT and AST (high: >3 times Upper Limit of Normal [ULN]), ALP (high: >2.5 times ULN), bilirubin and indirect bilirubin (high: >1.5 times ULN), creatine kinase (high: >5 times ULN), creatinine (high: >3 times ULN) and urea (high: >11.067 millimoles per Liter [mmol/L]. Data for any time on treatment has been presented. (NCT02802501)
Timeframe: Up to Day 120

,,
InterventionParticipants (Count of Participants)
ALT, HighALP, HighAST, HighBilirubin, HighCreatine Kinase, HighCreatinine, HighIndirect bilirubin, HighUrea, High
DHA-PQP Only11047010
Primaquine+DHA-PQP00046010
Tafenoquine+ DHA-PQP30166010

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Number of Participants With Gastrointestinal AEs

The number of participants with gastrointestinal AEs: nausea, vomiting, diarrhea, dyspepsia, abdominal distension, abdominal discomfort and constipation has been presented. (NCT02802501)
Timeframe: Up to Day 180

,,
InterventionParticipants (Count of Participants)
NauseaVomitingDiarrheaDyspepsiaAbdominal distensionAbdominal discomfortConstipation
DHA-PQP Only5652100
Primaquine+DHA-PQP3124120
Tafenoquine+ DHA-PQP4523101

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Number of Participants With Hematology Values Outside Clinical Concern Range

Blood samples were collected to analyze the following hematology parameters: Hemoglobin, lymphocytes and Platelet count. The clinical concern ranges for the parameters included: hemoglobin (low: <7 grams per deciliter), lymphocytes: (low: <0.5x10^9 cells per liter and high: >4x10^9 cells per liter),and platelets (low: <50x10^9 cells per liter). Data for any time on treatment has been presented. (NCT02802501)
Timeframe: Up to Day 120

,,
InterventionParticipants (Count of Participants)
Hemoglobin, LowLymphocytes, HighLymphocytes, LowPlatelets, Low
DHA-PQP Only0300
Primaquine+DHA-PQP0210
Tafenoquine+ DHA-PQP0401

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Percentage of Participants With Relapse-free Efficacy at Six Months After Administration of Primaquine With DHA-PQP and DHA-PQP Alone

A participant was considered to have demonstrated relapse-free efficacy at 6 months if: a) Participant had non-zero P. vivax asexual parasite count at Baseline (Day 1), b) Participant demonstrated initial clearance of P.vivax parasitemia, c) Participant had no positive asexual P.vivax parasite count at any assessment prior to or on study Day 180 following initial parasite clearance, d) Participants did not take a concomitant medication with anti-malarial activity (excluding study treatment) at any point between Study Day 1 and their last parasite assessment, e) Participant was parasite-free at 6 months. The percentage of participants who were relapse-free at 6 months post dose has been presented. (NCT02802501)
Timeframe: 6 months post-dose

InterventionPercentage of participants (Number)
DHA-PQP Only12
Primaquine+DHA-PQP52

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Number of Participants With Protocol-defined SAE (Hemoglobin Drop)

Blood samples were collected at indicated time points to analyze the hemoglobin level. Hemoglobin drop is defined as any one of the following occurring in the first 15 days of the study: a relative hemoglobin decrease of >=30% from Baseline, or an absolute hemoglobin decrease of >3 grams per liter from Baseline, or a drop in absolute hemoglobin to <7.0 grams per decilter (g/dL). Number of participants with a protocol-defined hemoglobin SAEs has been presented. (NCT02802501)
Timeframe: Days 3, 5, 7, and 14

,,
InterventionParticipants (Count of Participants)
Day 3Day 5Day 7Day 14
DHA-PQP Only0000
Primaquine+DHA-PQP0000
Tafenoquine+ DHA-PQP0000

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Number of Participants With Worst Case Body Temperature Results Relative to Normal Range Post-Baseline Relative to Baseline

"Body temperature was measured with participants in semi-supine position after 5 minutes of rest. Data was categorized as: body temperature 'low: <36.5 degrees celsius', 'high: >37.3 degrees celsius' and 'To Normal or No change'. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose vital sign value category was unchanged (e.g.,High to High), or whose value became normal, are recorded in the To Normal or No Change category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Day 1 was considered as Baseline." (NCT02802501)
Timeframe: Baseline (Day 1) and up to Day 180

,,
InterventionParticipants (Count of Participants)
To LowTo Normal or No changeTo High
DHA-PQP Only42310
Primaquine+DHA-PQP4256
Tafenoquine+ DHA-PQP38714

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Number of Participants With Worst Case Pulse Rate Results Relative to Normal Range Post-Baseline Relative to Baseline

"Pulse rate was measured with participants in semi-supine position after 5 minutes of rest. Data was categorized as: pulse rate low: <60 beats per minute [bpm], high: >100 bpm and 'To normal or No change'. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose vital sign value category was unchanged (e.g.,High to High), or whose value became normal, are recorded in the To Normal or No Change category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Day 1 was considered as Baseline." (NCT02802501)
Timeframe: Baseline (Day 1) and up to Day 180

,,
InterventionParticipants (Count of Participants)
To LowTo Normal or No changeTo High
DHA-PQP Only19257
Primaquine+DHA-PQP23263
Tafenoquine+ DHA-PQP26236

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Number of Participants With Worst Case Respiratory Rate Results Relative to Normal Range Post-Baseline Relative to Baseline

"Respiratory rate was measured with participants in semi-supine position after 5 minutes of rest. Data was categorized as: respiratory rate low: <12 breaths per minute', high: >18 breaths per minute and 'To normal or No change'. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose vital sign value category was unchanged (e.g.,High to High), or whose value became normal, are recorded in the To Normal or No Change category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%.Day 1 was considered as Baseline. Day 1 was considered as Baseline." (NCT02802501)
Timeframe: Baseline (Day 1) and up to Day 180

,,
InterventionParticipants (Count of Participants)
To LowTo Normal or No changeTo High
DHA-PQP Only0419
Primaquine+DHA-PQP04010
Tafenoquine+ DHA-PQP0419

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Number of Participants With Worst Case Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) Results Relative to Normal Range Post-Baseline Relative to Baseline

"SBP and DBP were measured with participants in semi-supine position after 5 minutes of rest. Data was categorized as: systolic blood pressure (SBP) (low: <90 and high: >120 millimeters of mercury [mmHg]); diastolic blood pressure (DBP) (low: <60 and high: >80 mmHg); and 'To Normal or No change'. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose vital sign value category was unchanged (e.g.,High to High), or whose value became normal, are recorded in the To Normal or No Change category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Day 1 was considered as Baseline." (NCT02802501)
Timeframe: Baseline (Day 1) and up to Day 180

,,
InterventionParticipants (Count of Participants)
SBP, To LowSBP, To Normal or No changeSBP, To HighDBP, To LowDBP, To Normal or No changeDBP, To High
DHA-PQP Only01931111628
Primaquine+DHA-PQP02525151628
Tafenoquine+ DHA-PQP1212992025

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AUC Gametocytes

The area under the curve of gametocyte density versus time. The median AUC was calculated for both cohorts. Since onset of gametocytaemia differs depending on method of infection a window of 15 days was used to calculate AUC, from the time-point where a minimum of 50% of participants within a cohort had detectable gametocytemia. (NCT03454048)
Timeframe: up to day 51 after challenge infection

Intervention(gametocytes*days)/mL (Median)
Cohort A99
Cohort B11043

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Frequency of Adverse Events in the CHMI-trans Model

Frequency of adverse events in the CHMI-trans model. (NCT03454048)
Timeframe: up to day 51 after challenge infection

InterventionAdverse events (Number)
Group 1 (Cohort A) LD-PIP/LD-PIP2/PIP95
Group 2 (Cohort A) LD-PIP/LD-PIP2/SP95
Group 3 (Cohort B) LD-PIP/LD-PIP2/PIP107
Group 4 (Cohort B) LD-PIP/LD-PIP2/SP52

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Gametocyte Commitment

The gametocyte commitment rate is estimated by dividing the peak gametocyte by the peak of asexual parasites. (NCT03454048)
Timeframe: up to day 51 after challenge infection

Interventiongametocytes/asexual parasite (Median)
Cohort A0.0011
Cohort B0.0323

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Gametocyte Prevalence

Number of individuals in each study arm that show prevalence of gametocytes as defined by quantitative reverse-transcriptase PCR (qRT-PCR) for CCp4 (female) and PfMGET (male) mRNA with a threshold of 5 gametocytes/mL for positivity. (NCT03454048)
Timeframe: up to day 51 after challenge infection

InterventionParticipants (Count of Participants)
Group 1 (Cohort A) LD-PIP/LD-PIP2/PIP5
Group 2 (Cohort A) LD-PIP/LD-PIP2/SP6
Group 3 (Cohort B) LD-PIP/LD-PIP2/PIP6
Group 4 (Cohort B) LD-PIP/LD-PIP2/SP6

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Gametocyte Sex-ratio

Proportion of male gametocytes (NCT03454048)
Timeframe: up to day 51 after challenge infection

InterventionProportion of male gametocytes (Median)
Cohort A0.20
Cohort B0.31

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Number of Participants Infectious for Mosquitoes Through DFA

Prevalence of gametocyte infectiousness for Anopheles mosquitoes through Direct Feeding Assays (Direct Skin Feeding Assay, DFA). (NCT03454048)
Timeframe: up to day 51 after challenge infection

InterventionParticipants (Count of Participants)
Cohort A0
Cohort B9

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Peak Density Gametocytes

Peak density of gametocytes by qRT-PCR. (NCT03454048)
Timeframe: up to day 51 after challenge infection

InterventionGametocytes/mL (Median)
Group 1 (Cohort A) LD-PIP/LD-PIP2/PIP13.9
Group 2 (Cohort A) LD-PIP/LD-PIP2/SP21.4
Group 3 (Cohort B) LD-PIP/LD-PIP2/PIP1442.2
Group 4 (Cohort B) LD-PIP/LD-PIP2/SP813.2

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Magnitude of Adverse Events in the CHMI-trans Model

"symptoms will be ranked as (1) mild, (2) moderate, or (3) severe, depending on their intensity according to the following scale:~Mild (grade 1): awareness of symptoms that are easily tolerated and do not interfere with usual daily activity~Moderate (grade 2): discomfort that interferes with or limits usual daily activity~Severe (grade 3): disabling, with subsequent inability to perform usual daily activity, resulting in absence or required bed rest" (NCT03454048)
Timeframe: up to day 51 after challenge infection

,,,
InterventionAdverse events (Number)
Mild (grade I)Moderate (grade II)Severe (grade III)
Group 1 (Cohort A) LD-PIP/LD-PIP2/PIP64229
Group 2 (Cohort A) LD-PIP/LD-PIP2/SP562217
Group 3 (Cohort B) LD-PIP/LD-PIP2/PIP86174
Group 4 (Cohort B) LD-PIP/LD-PIP2/SP4183

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