artemisone: second-generation semi-synthetic artemisinin derivative for antimalarial therapy devoid of neurotoxicity [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 11531457 |
| CHEMBL ID | 516268 |
| SCHEMBL ID | 22863299 |
| MeSH ID | M0503556 |
| Synonym |
|---|
| artemisone |
| artemifone |
| bay-449585 |
| CHEMBL516268 |
| bay 44-9585 |
| 255730-18-8 |
| 4-((3r,5as,6r,8as,9r,10r,12r,12ar)-3,6,9-trimethyldecahydro-12h-3,12-epoxypyrano(4,3-j)(1,2)benzodioxepin-10-yl)thiomorpholine-1,1-dione |
| CS-0015600 |
| HY-19502 |
| Q27266724 |
| MS-26839 |
| SCHEMBL22863299 |
| 4-[(1r,4s,5r,8s,9r,10r,12r,13r)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-yl]-1,4-thiazinane 1,1-dioxide |
| AKOS040741166 |
Artemisone is a 10-amino-artemisinin derivative that is markedly superior in vitro and in vivo to current artemisinins against malaria. It also possesses antitumor activity.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Artemisone is a 10-amino-artemisinin derivative that is markedly superior in vitro and in vivo to current artemisinins against malaria and also possesses antitumor activity. " | ( In vitro anti-cancer effects of artemisone nano-vesicular formulations on melanoma cells. du Plessis, J; du Plessis, L; du Preez, JL; Dwivedi, A; Haynes, RK; Mazumder, A, 2015) | 2.14 |
| "Artemisone is a new semi-synthetic 10-alkylamino artemisinin that is superior to other artemisinin derivatives in terms of its significantly higher antimalarial activity, its tolerance in vivo, lack of detectable neurotoxic potential, improved in vivo pharmacokinetics and metabolic stability." | ( Neospora caninum: in vivo and in vitro treatment with artemisone. Fish, L; Golenser, J; Haynes, R; Leibovich, B; Mazuz, ML; Molad, T; Savitsky, I; Shkap, V; Wollkomirsky, R, 2012) | 1.35 |
| "Artemisone is a leading candidate of second-generation semi-synthetic artemisinin derivatives for antimalarial therapy devoid of neurotoxicity." | ( In vitro activity of artemisone compared with artesunate against Plasmodium falciparum. Adegnika, AA; Burkhardt, D; Kremsner, PG; Nemeth, J; Ramharter, M, 2006) | 1.37 |
| "Artemisone is a novel 10-alkylamino derivative which is not metabolised to dihydroartemisinin." | ( Differential effects on angiogenesis of two antimalarial compounds, dihydroartemisinin and artemisone: implications for embryotoxicity. Basilico, N; D'Alessandro, S; Gelati, M; Haynes, RK; Parati, EA; Taramelli, D, 2007) | 1.28 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Treatment with artemisone may be useful as an alternative drug for preventing the pathology that results from babesiosis, without interfering with acquired immune protection following recovery from an acute babesiosis infection or vaccination." | ( Artemisone inhibits in vitro and in vivo propagation of Babesia bovis and B. bigemina parasites. Fish, L; Golenser, J; Haynes, RK; Leibovich, B; Mazuz, ML; Shkap, V; Wollkomirsky, R, 2013) | 2.17 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Artemisone was well tolerated, with no serious adverse events and no clinically relevant changes in laboratory and vital parameters." | ( First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. Edstein, MD; Fugmann, B; Haynes, RK; Kotecka, BM; Nagelschmitz, J; Rieckmann, KH; Roemer, A; Voith, B; Wensing, G, 2008) | 1.45 |
| " However, no effect on reproductive and developmental parameters below severe toxic dosages could be observed." | ( Developmental and reproductive toxicity studies on artemisone. Klaus, AM; Krötlinger, F; Langewische, FW; Schmuck, G, 2009) | 0.6 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " In a phase I program with double-blind, randomized, placebo-controlled, single and multiple ascending oral-dose studies, we evaluated the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of artemisone." | ( First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. Edstein, MD; Fugmann, B; Haynes, RK; Kotecka, BM; Nagelschmitz, J; Rieckmann, KH; Roemer, A; Voith, B; Wensing, G, 2008) | 0.73 |
Artemisone (ATM) is a novel derivative of artemisinin (ART) It can be used to treat cancer alone and in combination with chemotherapeutic agents.
| Excerpt | Reference | Relevance |
|---|---|---|
| " Artemisone represents an important addition to the repertoire of artemisinin combination therapies currently in use, as it has enhanced antimalarial activity, improved bioavailability and stability over current endoperoxides." | ( Antimalarial efficacy and drug interactions of the novel semi-synthetic endoperoxide artemisone in vitro and in vivo. Croft, SL; Fugmann, B; Haynes, RK; Peters, W; Rattray, L; Robinson, BL; Stewart, LB; Vivas, L, 2007) | 1.47 |
| " Nonetheless, its low water solubility and bioavailability has limited its clinical use." | ( In vitro anti-cancer effects of artemisone nano-vesicular formulations on melanoma cells. du Plessis, J; du Plessis, L; du Preez, JL; Dwivedi, A; Haynes, RK; Mazumder, A, 2015) | 0.7 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Plasma samples taken after multiple dosing showed marked ex vivo pharmacodynamic antimalarial activities against two multidrug-resistant Plasmodium falciparum lines." | ( First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. Edstein, MD; Fugmann, B; Haynes, RK; Kotecka, BM; Nagelschmitz, J; Rieckmann, KH; Roemer, A; Voith, B; Wensing, G, 2008) | 0.54 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID570711 | AUC (normalized) in healthy human plasma at 40 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570713 | Half life in healthy human plasma at 40 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574244 | Apparent oral clearance in healthy human at 30 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570937 | AUC in healthy human plasma at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574232 | Tmax in healthy human plasma at 20 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570767 | Ratio of Cmax in in healthy human plasma at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day to Cmax in healthy human plasma at 40 mg, po administered as two 20 mg im | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570763 | Apparent oral clearance in healthy human at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570716 | Apparent volume of distribution with respect to the bioavailability in healthy human at 40 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID563207 | Antiparasitic activity against Toxoplasma gondii PRU-Luc-GFP type 2 infected in 400 mg/kg sulfadiazine-pretreated INFgamma-deficient C57BL/6 mouse reactivated toxoplasmosis model assessed as mouse survival at 10 mg/kg, sc at once daily for 8 days administ | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Artemisone and artemiside control acute and reactivated toxoplasmosis in a murine model. |
| AID574246 | Cmax in healthy human plasma at 40 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574236 | Apparent volume of distribution with respect to the bioavailability in healthy human at 20 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570710 | AUC in healthy human plasma at 40 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570756 | AUC (normalized) in healthy human plasma at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574221 | AUC in healthy human plasma at 10 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574223 | Tmax in healthy human plasma at 10 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570718 | Normalized Cmax in healthy human plasma at 80 mg, po administered as single immediate release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574233 | Half life in healthy human plasma at 20 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574226 | Apparent oral clearance in healthy human at 10 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574208 | Toxicity in healthy human assessed as occurrence of adverse event at 80 mg, po administered daily for 3 days as four 20-mg immediate-release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID563203 | Antiparasitic activity against Toxoplasma gondii RH infected in human foreskin fibroblasts monolayer after 72 hrs by bacterial beta-galactosidase reporter gene assay | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Artemisone and artemiside control acute and reactivated toxoplasmosis in a murine model. |
| AID574218 | Toxicity in healthy human assessed as decrease in glutamate dehydrogenase level at 80 mg, po administered daily for 3 days as four 20-mg immediate-release tablets during 10 hrs overnight fasting state measured after 2 days last post treatment | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570753 | AUC in healthy human plasma at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID325357 | Growth inhibition of Leishmania donovani promastigotes after 72 hrs by Alamar blue assay | 2007 | Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5 | Artemisinins inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense in vitro growth. |
| AID748918 | Antimalarial activity against Plasmodium berghei infected in Swiss albino mouse assessed as reduction in parasitemia after 4 days by microscopic analysis relative to artesunate | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Recent advances in malaria drug discovery. |
| AID325355 | Growth inhibition of Trypanosoma cruzi epimastigotes after 72 hrs by Alamar blue assay | 2007 | Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5 | Artemisinins inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense in vitro growth. |
| AID570933 | Cmax in healthy human plasma at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570940 | AUC (normalized) in healthy human plasma at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574207 | Toxicity in healthy human assessed as occurrence of adverse event at 40 mg, po administered daily for 3 days as two 20-mg immediate-release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID571171 | Cmax in healthy human plasma infected with Plasmodium falciparum K1 at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 days | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570749 | Cmax in healthy human plasma at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570755 | AUC (normalized) in healthy human plasma at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574242 | Half life in healthy human plasma at 30 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570715 | Apparent oral clearance in healthy human at 40 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574219 | Cmax in healthy human plasma at 10 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID571167 | Apparent oral clearance in healthy human at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570752 | Normalized Cmax in healthy human plasma 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570768 | Ratio of Ratio of AUC (0 to infinity) in healthy human plasma at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day to Ratio of AUC (0 to infinity) in healthy human pla | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570762 | Mean residence time in healthy human at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570757 | Tmax in healthy human plasma at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574237 | Cmax in healthy human plasma at 30 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID563201 | Antiparasitic activity against Toxoplasma gondii PRU-Luc-GFP type 2 infected in CD1 mouse acute toxoplasmosis model assessed as mouse survival at 10 mg/kg, sc administered once daily for 8 days measured after 25 days post-infection | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Artemisone and artemiside control acute and reactivated toxoplasmosis in a murine model. |
| AID574213 | Toxicity in healthy human assessed as occurrence of changes in electrocardiogram parameters at 40 mg, po administered daily for 3 days as two 20-mg immediate-release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570723 | Mean residence time in healthy human at 80 mg, po administered as single immediate release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570758 | Tmax in healthy human plasma at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID372372 | Antiparasitic activity against Toxoplasma gondii ATCC 50839 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Artemisinin-resistant mutants of Toxoplasma gondii have altered calcium homeostasis. |
| AID570936 | Normalized Cmax in healthy human plasma 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570720 | AUC (normalized) in healthy human plasma at 80 mg, po administered as single immediate release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574239 | AUC in healthy human plasma at 30 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574243 | Mean residence time in healthy human at 30 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID563202 | Cytotoxicity against HFF | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Artemisone and artemiside control acute and reactivated toxoplasmosis in a murine model. |
| AID570941 | Tmax in healthy human plasma at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570722 | Half life in healthy human plasma at 80 mg, po administered as single immediate release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570942 | Tmax in healthy human plasma at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570944 | Half life in healthy human plasma at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574217 | Toxicity in healthy human assessed as decrease in alanine aminotransferase level at 80 mg, po administered daily for 3 days as four 20-mg immediate-release tablets during 10 hrs overnight fasting state measured after 2 days last post treatment | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570724 | Apparent oral clearance in healthy human at 80 mg, po administered as single immediate release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID571170 | Cmax in healthy human plasma infected with Plasmodium falciparum K1 at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574222 | AUC (normalized) in healthy human plasma at 10 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570951 | Ratio of Cmax in in healthy human plasma at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day to Cmax in healthy human plasma at 80 mg, po administered as four 20 mg | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574247 | Normalized Cmax in healthy human plasma at 40 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570764 | Apparent oral clearance in healthy human at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID748929 | Antiplasmodial activity against drug-sensitive Plasmodium falciparum 3D7 after 24 hrs by [3H]-hypoxanthine incorporation assay | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Recent advances in malaria drug discovery. |
| AID570754 | AUC in healthy human plasma at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID571168 | Cmax in healthy human plasma infected with Plasmodium falciparum K1 at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574234 | Mean residence time in healthy human at 20 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570943 | Half life in healthy human plasma at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570947 | Apparent oral clearance in healthy human at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570714 | Mean residence time in healthy human at 40 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574235 | Apparent oral clearance in healthy human at 20 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574211 | Toxicity in healthy human assessed as occurrence of clinically relevant changes in vital signs at 80 mg, po administered daily for 3 days as four 20-mg immediate-release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570721 | Tmax in healthy human plasma at 80 mg, po administered as single immediate release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570952 | Ratio of AUC (0 to infinity) in healthy human plasma at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day to AUC (0 to infinity) in healthy human plasma at 80 mg, po | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570760 | Half life in healthy human plasma at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570747 | Antimalarial activity against Plasmodium falciparum K1 in human plasma assessed as inhibition of hypoxanthine uptake by intraerythrocytic malaria parasites by hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570948 | Apparent oral clearance in healthy human at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570750 | Cmax in healthy human plasma at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574225 | Mean residence time in healthy human at 10 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574227 | Apparent volume of distribution with respect to the bioavailability in healthy human at 10 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574241 | Tmax in healthy human plasma at 30 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID1274389 | Antimalarial activity against sporozoite stage of Plasmodium berghei yoelii infected in human HepG2 cells | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials? |
| AID574212 | Toxicity in healthy human assessed as occurrence of changes in electrocardiogram parameters at 10 to 80 mg, po administered as single ascending doses during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574215 | Toxicity in healthy human assessed as increase in alanine aminotransferase level at 80 mg, po administered daily for 3 days as four 20-mg immediate-release tablets during 10 hrs overnight fasting state measured after 24 hrs last post treatment | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574245 | Apparent volume of distribution with respect to the bioavailability in healthy human at 30 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID563206 | Antiparasitic activity against Toxoplasma gondii PRU-Luc-GFP type 2 infected in 400 mg/kg sulfadiazine-pretreated INFgamma-deficient C57BL/6 mouse reactivated toxoplasmosis model assessed as mouse survival at 10 mg/kg, sc at once daily for 8 days administ | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Artemisone and artemiside control acute and reactivated toxoplasmosis in a murine model. |
| AID570939 | AUC (normalized) in healthy human plasma at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574210 | Toxicity in healthy human assessed as occurrence of clinically relevant changes in vital signs at 40 mg, po administered daily for 3 days as two 20-mg immediate-release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID325356 | Growth inhibition of Trypanosoma brucei rhodesiense trypomastigotes after 72 hrs by Alamar blue assay | 2007 | Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5 | Artemisinins inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense in vitro growth. |
| AID574216 | Toxicity in healthy human assessed as increase in glutamate dehydrogenase level at 80 mg, po administered daily for 3 days as four 20-mg immediate-release tablets during 10 hrs overnight fasting state measured after 24 hrs last post treatment | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570765 | Apparent volume of distribution with respect to the bioavailability in healthy human at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID563384 | Antiparasitic activity against Toxoplasma gondii PRU-Luc-GFP type 2 infected in 400 mg/kg sulfadiazine-pretreated INFgamma-deficient C57BL/6 mouse reactivated toxoplasmosis model assessed as mouse survival at 10 mg/kg, sc at once daily for 8 days administ | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Artemisone and artemiside control acute and reactivated toxoplasmosis in a murine model. |
| AID570748 | Antimalarial activity against Plasmodium falciparum TM90-C2A in human plasma assessed as inhibition of hypoxanthine uptake by intraerythrocytic malaria parasites by hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID563385 | Partition coefficient, log P of the compound | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Artemisone and artemiside control acute and reactivated toxoplasmosis in a murine model. |
| AID574209 | Toxicity in healthy human assessed as occurrence of clinically relevant changes in vital signs at 10 to 80 mg, po administered as single ascending doses during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570717 | Cmax in healthy human plasma at 80 mg, po administered as single immediate release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570949 | Apparent volume of distribution with respect to the bioavailability in healthy human at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570761 | Mean residence time in healthy human at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID563204 | Antiparasitic activity against Toxoplasma gondii PRU-Luc-GFP type 2 infected in CD1 mouse acute toxoplasmosis model assessed as decrease in parasite burden at 10 mg/kg, sc administered once daily for 8 days measured after 25 days post-infection by lucifer | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Artemisone and artemiside control acute and reactivated toxoplasmosis in a murine model. |
| AID570766 | Apparent volume of distribution with respect to the bioavailability in healthy human at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570945 | Mean residence time in healthy human at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574228 | Cmax in healthy human plasma at 20 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570719 | AUC in healthy human plasma at 80 mg, po administered as single immediate release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID748919 | Antiplasmodial activity against Plasmodium falciparum relative to artesunate | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Recent advances in malaria drug discovery. |
| AID570725 | Apparent volume of distribution with respect to the bioavailability in healthy human at 80 mg, po administered as single immediate release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570934 | Cmax in healthy human plasma at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570935 | Normalized Cmax in healthy human plasma 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574229 | Normalized Cmax in healthy human plasma at 20 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574231 | AUC (normalized) in healthy human plasma at 20 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570938 | AUC in healthy human plasma at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574214 | Toxicity in healthy human assessed as occurrence of changes in electrocardiogram parameters at 80 mg, po administered daily for 3 days as four 20-mg immediate-release tablets during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574224 | Half life in healthy human plasma at 10 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574240 | AUC (normalized) in healthy human plasma at 30 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574230 | AUC in healthy human plasma at 20 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570946 | Mean residence time in healthy human at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID748932 | Antimalarial activity against Plasmodium berghei infected in Swiss albino mouse assessed as reduction in parasitemia after 4 days by microscopic analysis | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Recent advances in malaria drug discovery. |
| AID570712 | Tmax in healthy human plasma at 40 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574238 | Normalized Cmax in healthy human plasma at 30 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID571169 | Cmax in healthy human plasma infected with Plasmodium falciparum K1 at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 days | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570759 | Half life in healthy human plasma at 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID574220 | Normalized Cmax in healthy human plasma at 10 mg, po administered as single ascending doses as solution during 10 hrs overnight fasting state | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570950 | Apparent volume of distribution with respect to the bioavailability in healthy human at 80 mg, po administered as four 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 3 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| AID570751 | Normalized Cmax in healthy human plasma 40 mg, po administered as two 20 mg immediate release tablets daily for 3 days during 10 hrs overnight fasting state measured after 1 day | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 10 (25.64) | 29.6817 |
| 2010's | 27 (69.23) | 24.3611 |
| 2020's | 2 (5.13) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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 strong demand-to-supply ratio for research on this compound.
| This Compound (44.09) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (2.56%) | 5.53% |
| Reviews | 1 (2.56%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 37 (94.87%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||