Page last updated: 2024-12-08
artelinic acid
Description
Research Excerpts
Clinical Trials
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Pathways
Study Profile
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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 Source | ID |
|---|---|
| PubMed CID | 10341948 |
| SCHEMBL ID | 18674195 |
| MeSH ID | M0173588 |
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
| Excerpt | Reference | Relevance |
|---|---|---|
| "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
| Excerpt | Reference | Relevance |
|---|---|---|
| " 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
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.
| Excerpt | Relevance | Reference |
|---|---|---|
| "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)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 1 (3.33) | 18.7374 |
| 1990's | 16 (53.33) | 18.2507 |
| 2000's | 5 (16.67) | 29.6817 |
| 2010's | 7 (23.33) | 24.3611 |
| 2020's | 1 (3.33) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (2.94%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 33 (97.06%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||