Page last updated: 2024-12-08

artelinic acid

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

Description

artelinic acid: RN given refers to parent cpd without isomeric designation; benzyl ether of artemether [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10341948
SCHEMBL ID18674195
MeSH IDM0173588

Synonyms (15)

Synonym
beta-artelinic acid
artelinic acid
unii-08x93406pg
08x93406pg ,
120020-26-0
.beta.-artelinic acid
benzoic acid, 4-((((3r,5as,6r,8as,9r,10s,12r,12ar)-decahydro-3,6,9-trimethyl-3,12-epoxy-12h-pyrano(4,3-j)-1,2-benzodioxepin-10-yl)oxy)methyl)-
SCHEMBL18674195
Q4797402
HY-135578
CS-0113531
4-[[(1r,4s,5r,8s,9r,10s,12r,13r)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-yl]oxymethyl]benzoic acid
MS-27319
DTXSID501316558
AKOS040732471

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"5 mg/kg for 7-28 days, indicating that the safe dosing duration in monkeys should be longer than 7 days under the exposure."( Toxicokinetic and toxicodynamic (TK/TD) evaluation to determine and predict the neurotoxicity of artemisinins.
Hickman, M; Li, Q, 2011
)
0.37
" The high correlation between embryotoxicity and reticulocytopenia further supports the assertion that therapeutic dosage regimens of artemisinins that cause decreases in reticulocyte count in pregnant women during the putative critical period (approximately postconception wk 3 to 9) are at risk of also causing adverse effects on the embryo."( Artesunate and artelinic acid: association of embryotoxicity, reticulocytopenia, and delayed stimulation of hematopoiesis in pregnant rats.
Brannen, KC; Clark, RL; Hoberman, AM; Sanders, JE, 2011
)
0.37

Pharmacokinetics

ExcerptReferenceRelevance
" After intravenous administration, artelinic acid concentrations in blood plasma were high (C0: 76 +/- 15 mg L-1), and the drug was rapidly eliminated from the central compartment, showing linear elimination kinetics with an elimination half-life of 15 +/- 3 min."( Pharmacokinetic and pharmacodynamic aspects of artelinic acid in rodents.
Eling, WM; Titulaer, HA; Zuidema, J, 1993
)
0.29
" The resulting pharmacokinetic parameter estimates were substantially different not only between drugs but also between routes of administration for the same drug."( The pharmacokinetics and bioavailability of dihydroartemisinin, arteether, artemether, artesunic acid and artelinic acid in rats.
Brewer, TG; Fleckenstein, LL; Heiffer, MH; Li, QG; Masonic, K; Peggins, JO, 1998
)
0.3
" Blood samples were obtained after the first dose within 6 h for pharmacokinetic (PK) and ex vivo pharmacodynamic evaluation by simultaneously measuring plasma drug concentration and anti-malarial activity against Plasmodium falciparum in vitro."( Comparative pharmacokinetics and pharmacodynamics of intravenous artelinate versus artesunate in uncomplicated Plasmodium coatneyi-infected rhesus monkey model.
Chanarat, N; Gettayacamin, M; Komcharoen, N; Limsalakpeth, A; Rasameesoraj, M; Saunders, DL; Scott Miller, R; Siriyanonda, D; Teja-Isavadharm, P; Weina, PJ, 2016
)
0.43

Bioavailability

ExcerptReferenceRelevance
" A large inter-subject variation appeared in the absorption rate and the extent of absorption (2-92%) over the 120 min interval after intramuscular administration."( Pharmacokinetic and pharmacodynamic aspects of artelinic acid in rodents.
Eling, WM; Titulaer, HA; Zuidema, J, 1993
)
0.29
"The pharmacokinetics and bioavailability of dihydroartemisinin (DQHS), artemether (AM), arteether (AE), artesunic acid (AS) and artelinic acid (AL) have been investigated in rats after single intravenous, intramuscular and intragastric doses of 10 mg kg(-1)."( The pharmacokinetics and bioavailability of dihydroartemisinin, arteether, artemether, artesunic acid and artelinic acid in rats.
Brewer, TG; Fleckenstein, LL; Heiffer, MH; Li, QG; Masonic, K; Peggins, JO, 1998
)
0.3
" Oral bioavailability of ARTL was 79."( Pharmacology and toxicology of artelinic acid: preclinical investigations on pharmacokinetics, metabolism, protein and red blood cell binding, and acute and anorectic toxicities.
Brewer, TG; Li, QG; Lin, AJ; Masonic, KJ; Peggins, JO; Trotman, KM,
)
0.13

Dosage Studied

9 mg of artelinic acid was administered twice a day, beginning on day 3 after infection, for three days (total dosage of 270 mg/kg) berghei (with 3/8 cured) superior to that of artelinic acid (1-8 cured), whereas p-fluorophenyl and p-methoxyphenyl analogs demonstrated activity only comparable (1/8 cure) at the same dosage level.

ExcerptRelevanceReference
"9 mg of artelinic acid that was administered twice a day, beginning on day 3 after infection, for three days (total dosage of 270 mg/kg)."( Transdermal artelinic acid: an effective treatment for Plasmodium berghei-infected mice.
Ager, AL; Fleckenstein, L; Klayman, DL; Lin, AJ, 1991
)
0.28
" This novel drug delivery system may be an easy and safe way to administer artemisinin-type antimalarials and also a good alternative dosage form for active compounds with solubility problems."( Antimalarial activity of dihydroartemisinin derivatives by transdermal application.
Ager, AL; Klayman, DL; Lin, AJ, 1994
)
0.29
" berghei (with 3/8 cured) superior to that of artelinic acid (1/8 cured), whereas p-fluorophenyl and p-methoxyphenyl analogs demonstrated activity only comparable (1/8 cured) to that of artelinic acid at the same dosage level (64 mg/kg twice a day)."( Antimalarial activity of new dihydroartemisinin derivatives. 7. 4-(p-substituted phenyl)-4(R or S)-[10(alpha or beta)-dihydroartemisininoxy]butyric acids.
Kyle, DE; Lin, AJ; Zikry, AB, 1997
)
0.3
" Plasma was separated from blood samples collected at different times after dosing and analysed for parent drug."( The pharmacokinetics and bioavailability of dihydroartemisinin, arteether, artemether, artesunic acid and artelinic acid in rats.
Brewer, TG; Fleckenstein, LL; Heiffer, MH; Li, QG; Masonic, K; Peggins, JO, 1998
)
0.3
" In rats dosed with [14C]ARTL, unchanged ARTL accounted for less than 13% of the total radioactivity after all 3 administration routes, suggesting that ARTL was extensively biotransformed."( Pharmacology and toxicology of artelinic acid: preclinical investigations on pharmacokinetics, metabolism, protein and red blood cell binding, and acute and anorectic toxicities.
Brewer, TG; Li, QG; Lin, AJ; Masonic, KJ; Peggins, JO; Trotman, KM,
)
0.13
" After dose range study, rats were dosed at either 160 mg/kg daily for 9 consecutive days or at 288 mg/kg once every other day for five doses, so that the total dose (1440 mg/kg) and duration (9 days) were identical."( Neurotoxicity and toxicokinetics of artelinic acid following repeated oral administration in rats.
Bennett, K; Johnson, TO; Li, Q; Mog, S; Si, Y; Weina, PJ; Xie, L,
)
0.13
"5 mg/kg for 7-28 days, indicating that the safe dosing duration in monkeys should be longer than 7 days under the exposure."( Toxicokinetic and toxicodynamic (TK/TD) evaluation to determine and predict the neurotoxicity of artemisinins.
Hickman, M; Li, Q, 2011
)
0.37
" The high correlation between embryotoxicity and reticulocytopenia further supports the assertion that therapeutic dosage regimens of artemisinins that cause decreases in reticulocyte count in pregnant women during the putative critical period (approximately postconception wk 3 to 9) are at risk of also causing adverse effects on the embryo."( Artesunate and artelinic acid: association of embryotoxicity, reticulocytopenia, and delayed stimulation of hematopoiesis in pregnant rats.
Brannen, KC; Clark, RL; Hoberman, AM; Sanders, JE, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (30)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (3.33)18.7374
1990's16 (53.33)18.2507
2000's5 (16.67)29.6817
2010's7 (23.33)24.3611
2020's1 (3.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (2.94%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other33 (97.06%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]