Peringatan Keamanan

In single dose studies in CD-1 male mice, Artenimol did not show signs of toxicity up to 1200 mg/kg L1149.

In repeated dose studies in CD-1 mice, the NOAEL for Artenimol was determined to be 200 mg/kg/day L1149. This value was determined to be 90 mg/kg/day in beagle dogs. The maximum tolerable dose in rats was observed to be 270 mg/kg/day. Doses of 540 mg/kg/day resulted in acute toxicity progressing to lethal effects. Toxicity was characterized by infiltration of macrophages and intracytoplasmic deposition of basophilic granular materials in macrophages consistent with phospholipidosis. Toxicity at high doses were accompanied by decreases in reticulocytes, and increases in AST and ALT.

Artenimol

DB11638

small molecule approved experimental investigational

Deskripsi

Artenimol is an artemisinin derivative and antimalarial agent used in the treatment of uncomplicated *Plasmodium falciparum* infections FDA Label. It was first authorized for market by the European Medicines Agency in October 2011 in combination with DB13941 as the product Eurartesim. Artemisinin combination therapy is highly effective against malaria and stongly recommended by the World Health Organization L1156.

Struktur Molekul 2D

Berat 284.352
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Artenimol was reported to have a half life of elimination of approximately 1 h [FDA Label].
Volume Distribusi Artenimol was observed to have a mean apparent volume of distribution of 0.801 L/kg in adult patients and 0.705 L/kg in pediatric patients wit *P. falciparum* malaria [L1149].
Klirens (Clearance) Artenimol was observed to have a mean apparent clearance of 1.340 L/h/kg in adult patients and 1.450 L/h/kg in pediatric patients with *P. falciparum* malaria [L1149].

Absorpsi

The reported oral bioavailability of Artenimol was reported to be 45% in healthy adults L1149. The observed Tmax was 1-2 h This is known to increase in malaria infected patients which could be attributed to reduced metabolism by the liver or the drug's collection in infected erythrocytes. Artenimol was obeserved to have flip-flop kinetics with an overall absorption half-life of 1.04 h. When administered with food the AUC for Artenimol increases by 144%. Cmax was observed to increase by 129% but was not found to be statistically significant. Food was observed to delay Tmax by 1 h.

Metabolisme

The primary metabolite of Artenimol is the glucuronide conjugate, ?-artenimol-?-glucuronide FDA Label. It is largely metabolized by UGT1A9 with some contribution by UGT2B7 L1149.

Rute Eliminasi

Artenimol is eliminated via metabolism to glucuronide conjugates FDA Label. There is little data on elimination of Artenimol but elimination of unchanged artemisinin compounds in feces and urine has been reported to be negligible.

Interaksi Obat

378 Data
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Artenimol.
Artemether The risk or severity of QTc prolongation can be increased when Artenimol is combined with Artemether.
Lumefantrine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Lumefantrine.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Artenimol.
Thiethylperazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Thiethylperazine.
Promazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Promazine.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Prochlorperazine.
Chlorpromazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Chlorpromazine.
Triflupromazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Triflupromazine.
Fluphenazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Fluphenazine.
Thioridazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Thioridazine.
Moricizine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Moricizine.
Trifluoperazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Trifluoperazine.
Perphenazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Perphenazine.
Mesoridazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Mesoridazine.
Acetophenazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Acetophenazine.
Promethazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Promethazine.
Alimemazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Alimemazine.
Methotrimeprazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Methotrimeprazine.
Periciazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Periciazine.
Acepromazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Acepromazine.
Aceprometazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Aceprometazine.
Pipotiazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Pipotiazine.
Thioproperazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Thioproperazine.
BL-1020 The risk or severity of QTc prolongation can be increased when Artenimol is combined with BL-1020.
Cyamemazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Cyamemazine.
Methylene blue The risk or severity of QTc prolongation can be increased when Artenimol is combined with Methylene blue.
Propiopromazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Propiopromazine.
Perazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Perazine.
Butaperazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Butaperazine.
Chlorproethazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Chlorproethazine.
Thiazinam The risk or severity of QTc prolongation can be increased when Artenimol is combined with Thiazinam.
Dixyrazine The risk or severity of QTc prolongation can be increased when Artenimol is combined with Dixyrazine.
Perphenazine enanthate The risk or severity of QTc prolongation can be increased when Artenimol is combined with Perphenazine enanthate.
Dapsone The risk or severity of adverse effects can be increased when Artenimol is combined with Dapsone.
Vemurafenib The risk or severity of QTc prolongation can be increased when Vemurafenib is combined with Artenimol.
Aripiprazole The metabolism of Aripiprazole can be decreased when combined with Artenimol.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be decreased when combined with Artenimol.
Pantoprazole The metabolism of Pantoprazole can be decreased when combined with Artenimol.
Pentobarbital The metabolism of Pentobarbital can be decreased when combined with Artenimol.
Methadone The metabolism of Methadone can be decreased when combined with Artenimol.
Omeprazole The metabolism of Omeprazole can be decreased when combined with Artenimol.
Trimethadione The metabolism of Trimethadione can be decreased when combined with Artenimol.
Clobazam The metabolism of Clobazam can be decreased when combined with Artenimol.
Carisoprodol The metabolism of Carisoprodol can be decreased when combined with Artenimol.
Progesterone The metabolism of Progesterone can be decreased when combined with Artenimol.
Zolpidem The metabolism of Zolpidem can be decreased when combined with Artenimol.
Lansoprazole The metabolism of Lansoprazole can be decreased when combined with Artenimol.
Quinine The metabolism of Quinine can be decreased when combined with Artenimol.
Fluoxetine The metabolism of Fluoxetine can be decreased when combined with Artenimol.
Albendazole The metabolism of Albendazole can be decreased when combined with Artenimol.
Voriconazole The metabolism of Voriconazole can be decreased when combined with Artenimol.
Esomeprazole The metabolism of Esomeprazole can be decreased when combined with Artenimol.
Clopidogrel The metabolism of Clopidogrel can be decreased when combined with Artenimol.
Primidone The metabolism of Primidone can be decreased when combined with Artenimol.
Diazepam The metabolism of Diazepam can be decreased when combined with Artenimol.
Methylphenobarbital The metabolism of Methylphenobarbital can be decreased when combined with Artenimol.
Zonisamide The metabolism of Zonisamide can be decreased when combined with Artenimol.
Ramelteon The metabolism of Ramelteon can be decreased when combined with Artenimol.
Praziquantel The metabolism of Praziquantel can be decreased when combined with Artenimol.
Rabeprazole The metabolism of Rabeprazole can be decreased when combined with Artenimol.
Proguanil The metabolism of Proguanil can be decreased when combined with Artenimol.
Escitalopram The metabolism of Escitalopram can be decreased when combined with Artenimol.
Lapatinib The metabolism of Lapatinib can be decreased when combined with Artenimol.
St. John's Wort The metabolism of St. John's Wort can be decreased when combined with Artenimol.
Hexobarbital The metabolism of Hexobarbital can be decreased when combined with Artenimol.
Barbital The metabolism of Barbital can be decreased when combined with Artenimol.
Methsuximide The metabolism of Methsuximide can be decreased when combined with Artenimol.
Dexlansoprazole The metabolism of Dexlansoprazole can be decreased when combined with Artenimol.
Lacosamide The metabolism of Lacosamide can be decreased when combined with Artenimol.
Etravirine The metabolism of Etravirine can be decreased when combined with Artenimol.
Apixaban The metabolism of Apixaban can be decreased when combined with Artenimol.
Seratrodast The metabolism of Seratrodast can be decreased when combined with Artenimol.
(R)-warfarin The metabolism of (R)-warfarin can be decreased when combined with Artenimol.
Vortioxetine The metabolism of Vortioxetine can be decreased when combined with Artenimol.
Etizolam The metabolism of Etizolam can be decreased when combined with Artenimol.
Esketamine The metabolism of Esketamine can be decreased when combined with Artenimol.
Lynestrenol The metabolism of Lynestrenol can be decreased when combined with Artenimol.
Dexrabeprazole The metabolism of Dexrabeprazole can be decreased when combined with Artenimol.
(S)-Warfarin The metabolism of (S)-Warfarin can be decreased when combined with Artenimol.
Fedratinib The metabolism of Fedratinib can be decreased when combined with Artenimol.
Estradiol The metabolism of Estradiol can be decreased when combined with Artenimol.
Voxelotor The metabolism of Voxelotor can be decreased when combined with Artenimol.
Cenobamate The metabolism of Cenobamate can be decreased when combined with Artenimol.
Testosterone The metabolism of Testosterone can be decreased when combined with Artenimol.
Glyburide The metabolism of Glyburide can be decreased when combined with Artenimol.
Selumetinib The metabolism of Selumetinib can be decreased when combined with Artenimol.
Valproic acid The metabolism of Valproic acid can be decreased when combined with Artenimol.
Nilutamide The metabolism of Nilutamide can be decreased when combined with Artenimol.
Gliclazide The metabolism of Gliclazide can be decreased when combined with Artenimol.
Stiripentol The metabolism of Artenimol can be decreased when combined with Stiripentol.
Benzocaine The risk or severity of methemoglobinemia can be increased when Artenimol is combined with Benzocaine.
Rilpivirine The metabolism of Rilpivirine can be decreased when combined with Artenimol.
Cyclophosphamide The metabolism of Cyclophosphamide can be decreased when combined with Artenimol.
Axitinib The metabolism of Axitinib can be decreased when combined with Artenimol.
Phenytoin The metabolism of Phenytoin can be decreased when combined with Artenimol.
Thiopental The metabolism of Thiopental can be decreased when combined with Artenimol.
Phenobarbital The metabolism of Phenobarbital can be decreased when combined with Artenimol.
Fosphenytoin The metabolism of Fosphenytoin can be decreased when combined with Artenimol.
Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Artenimol.

Target Protein

Actin, cytoplasmic 2 ACTG1
Alpha-aminoadipic semialdehyde dehydrogenase ALDH7A1
Annexin A2 ANXA2
ATP synthase subunit alpha, mitochondrial ATP5F1A
ATP synthase subunit g, mitochondrial ATP5MG
ATP synthase subunit O, mitochondrial ATP5PO
Calpastatin CAST
T-complex protein 1 subunit gamma CCT3
Cofilin-1 CFL1
Chloride intracellular channel protein 1 CLIC1
Cysteine and glycine-rich protein 1 CSRP1
Dihydropyrimidinase-related protein 2 DPYSL2
Desmoplakin DSP
Elongation factor 1-alpha 1 EEF1A1
Alpha-enolase ENO1
Filamin-A FLNA
Alpha-ketoglutarate-dependent dioxygenase FTO FTO
Glucose-6-phosphate 1-dehydrogenase G6PD
Glyceraldehyde-3-phosphate dehydrogenase, testis-specific GAPDHS
Glucose-6-phosphate isomerase GPI
Heterogeneous nuclear ribonucleoproteins A2/B1 HNRNPA2B1
Heterogeneous nuclear ribonucleoprotein D0 HNRNPD
Heterogeneous nuclear ribonucleoprotein K HNRNPK
Heterochromatin protein 1-binding protein 3 HP1BP3
Heat shock protein beta-1 HSPB1
Ras GTPase-activating-like protein IQGAP1 IQGAP1
Far upstream element-binding protein 2 KHSRP
L-lactate dehydrogenase A chain LDHA
L-lactate dehydrogenase B chain LDHB
Galectin-1 LGALS1
Microtubule-associated protein 4 MAP4
Malate dehydrogenase, cytoplasmic MDH1
Puromycin-sensitive aminopeptidase NPEPPS
Profilin-1 PFN1
Phosphoglycerate kinase 1 PGK1
Pyruvate kinase PKM PKM
Peptidyl-prolyl cis-trans isomerase A PPIA
Peroxiredoxin-1 PRDX1
Large ribosomal subunit protein uL16 RPL10
Large ribosomal subunit protein eL14 RPL14
Large ribosomal subunit protein eL18 RPL18
Large ribosomal subunit protein uL23 RPL23A
Large ribosomal subunit protein uL29 RPL35
Large ribosomal subunit protein uL4 RPL4
Small ribosomal subunit protein uS15 RPS13
Small ribosomal subunit protein eS17 RPS17
Small ribosomal subunit protein uS13 RPS18
Small ribosomal subunit protein eS19 RPS19
Small ribosomal subunit protein eS28 RPS28
Small ribosomal subunit protein uS7 RPS5
Small ribosomal subunit protein eS6 RPS6
Small ribosomal subunit protein eS8 RPS8
Small ribosomal subunit protein uS4 RPS9
Splicing factor 1 SF1
Splicing factor, proline- and glutamine-rich SFPQ
Small nuclear ribonucleoprotein Sm D2 SNRPD2
Signal recognition particle 14 kDa protein SRP14
Serine/arginine-rich splicing factor 4 SRSF4
Transgelin TAGLN
Transgelin-2 TAGLN2
Triosephosphate isomerase TPI1
Tropomyosin alpha-1 chain TPM1
Tubulin alpha-1A chain TUBA1A
Vimentin VIM
Zyxin ZYX
Heat shock cognate 71 kDa protein HSPA8
Tubulin beta-6 chain TUBB6
Tubulin beta-4A chain TUBB4A
Tubulin beta chain TUBB
Fructose-bisphosphate aldolase A ALDOA
Glyceraldehyde-3-phosphate dehydrogenase GAPDH
Cytochrome c CYCS
Phosphoglycerate mutase 1 PGAM1
Myosin-9 MYH9
Protein disulfide-isomerase P4HB
Probable ATP-dependent RNA helicase DDX5 DDX5
Serine hydroxymethyltransferase, mitochondrial SHMT2
Spliceosome RNA helicase DDX39B DDX39B
Nucleophosmin NPM1
Translationally-controlled tumor protein homolog TCTP
P-type Ca2+-transporting ATPase serca
Ornithine aminotransferase OAT
Elongation factor 1-alpha MEF-1
Multidrug resistance protein MDR1
Elongation factor 2
Actin-1
Glyceraldehyde-3-phosphate dehydrogenase GAPDH
Fructose-bisphosphate aldolase
Cell division cycle protein 48 homologue,putative
Heat shock protein 90
Eukaryotic initiation factor 4A H45
Pyruvate kinase
L-lactate dehydrogenase
Protein disulfide-isomerase
Thioredoxin-related protein, putative
Spermidine synthase
Probable ATP-dependent 6-phosphofructokinase
Glutamate dehydrogenase
Endoplasmin homolog, putative
Hypoxanthine-guanine-xanthine phosphoribosyltransferase LACZ
Enolase ENO
40S ribosomal protein S3
Non-SERCA-type Ca2+-transporting P-ATPase
Tubulin alpha chain
Knob-associated histidine-rich protein
S-adenosylmethionine synthase
V-type H(+)-translocating pyrophosphatase, putative
60S ribosomal protein L4
Phosphoethanolamine N-methyltransferase
40S ribosomal protein S3a
Conserved Plasmodium membrane protein
60S ribosomal protein L3
High molecular weight rhoptry protein 2
Serine repeat antigen 5 SERA5
40S ribosomal protein S19
Glycophorin-binding protein GBP
Calcium-transporting ATPase ATP6
V-type proton ATPase catalytic subunit A vapA
60S ribosomal protein L2
Acyl-CoA synthetase ACS3
Plasmepsin IV
Plasmepsin-1
Chloroquine resistance transporter CRT
14-3-3 protein
Isoleucine--tRNA ligase, putative
Plasmodium exported protein
Tubulin beta chain
60S ribosomal protein L27
Sec62, putative
Autophagy-related protein 18, putative
Mature parasite-infected erythrocyte surface antigen
Importin-7, putative
Importin subunit alpha
Peptidyl-prolyl cis-trans isomerase
DnaJ protein, putative
Merozoite surface protein 1 MSP-1
Glutamate--tRNA ligase
T-complex protein 1 subunit eta
Plasmepsin-2
Chaperone, putative
Rhoptry neck protein 3
40S ribosomal protein S5, putative
Skeleton-binding protein 1
Purine nucleotide phosphorylase, putative
Adenosylhomocysteinase
Adenosine deaminase
Methionine--tRNA ligase
Carbamoyl phosphate synthetase
Aspartate carbamoyltransferase
Signal recognition particle receptor, beta subunit
Parasite-infected erythrocyte surface protein
Coatomer alpha subunit, putative
Hexokinase HK
Proteasome subunit alpha type
Haloacid dehalogenase-like hydrolase
Insulinase, putative
40S ribosomal protein S21
Ubiquitin-conjugating enzyme E2
Eukaryotic translation initiation factor 3 subunit C
60S ribosomal protein L24, putative
60S ribosomal protein L23
60S ribosomal protein L17, putative
HAP protein
Heat shock protein 110, putative
60S ribosomal protein L10, putative
Lysophospholipase, putative
Polyadenylate-binding protein
Ubiquitin-60S ribosomal protein L40
Phosphoribosylpyrophosphate synthetase
Thioredoxin peroxidase 1 TPx1
Protein transport protein SEC31 Sec31p
Dipeptidyl aminopeptidase 1
Ring-infected erythrocyte surface antigen RESA
ATP-dependent RNA helicase UAP56 UAP56
Calcium-dependent protein kinase 4 CPK4
GTP-binding nuclear protein Ran
Nucleoside transporter 2
Anamorsin homolog
Glutamine synthetase, putative
60S ribosomal protein L30e, putative
Casein kinase 2, alpha subunit
Threonine--tRNA ligase
cAMP-dependent protein kinase regulatory subunit PKAr
Elongation factor 1-gamma, putative
Thioredoxin-like protein tlp1
60S ribosomal protein L21
60S ribosomal protein L14, putative
Inner membrane complex sub-compartment protein 3
HSP40, subfamily A, putative
Pyridoxal 5'-phosphate synthase subunit Pdx1 pdx1
Albumin ALB

Referensi & Sumber

Artikel (PubMed)
  • PMID: 26694030
    Wang J, Zhang CJ, Chia WN, Loh CC, Li Z, Lee YM, He Y, Yuan LX, Lim TK, Liu M, Liew CX, Lee YQ, Zhang J, Lu N, Lim CT, Hua ZC, Liu B, Shen HM, Tan KS, Lin Q: Haem-activated promiscuous targeting of artemisinin in Plasmodium falciparum. Nat Commun. 2015 Dec 22;6:10111. doi: 10.1038/ncomms10111.
  • PMID: -
    Haynes RK and Vonwiller SC: The behaviour of qinghaosu (artemisinin) in the presence of heme iron(II) and (III) Tetrahedron Lett. 1996 January 8;37(2):253-256.
  • PMID: 9057849
    Paitayatat S, Tarnchompoo B, Thebtaranonth Y, Yuthavong Y: Correlation of antimalarial activity of artemisinin derivatives with binding affinity with ferroprotoporphyrin IX. J Med Chem. 1997 Feb 28;40(5):633-8. doi: 10.1021/jm960767v.
  • PMID: 8053024
    White NJ: Clinical pharmacokinetics and pharmacodynamics of artemisinin and derivatives. Trans R Soc Trop Med Hyg. 1994 Jun;88 Suppl 1:S41-3.
  • PMID: 26340163
    Ravindra KC, Ho WE, Cheng C, Godoy LC, Wishnok JS, Ong CN, Wong WS, Wogan GN, Tannenbaum SR: Untargeted Proteomics and Systems-Based Mechanistic Investigation of Artesunate in Human Bronchial Epithelial Cells. Chem Res Toxicol. 2015 Oct 19;28(10):1903-13. doi: 10.1021/acs.chemrestox.5b00105. Epub 2015 Sep 21.
  • PMID: 7986020
    Asawamahasakda W, Ittarat I, Pu YM, Ziffer H, Meshnick SR: Reaction of antimalarial endoperoxides with specific parasite proteins. Antimicrob Agents Chemother. 1994 Aug;38(8):1854-8.
  • PMID: 12931192
    Eckstein-Ludwig U, Webb RJ, Van Goethem ID, East JM, Lee AG, Kimura M, O'Neill PM, Bray PG, Ward SA, Krishna S: Artemisinins target the SERCA of Plasmodium falciparum. Nature. 2003 Aug 21;424(6951):957-61. doi: 10.1038/nature01813.
  • PMID: 9632675
    Bhisutthibhan J, Pan XQ, Hossler PA, Walker DJ, Yowell CA, Carlton J, Dame JB, Meshnick SR: The Plasmodium falciparum translationally controlled tumor protein homolog and its reaction with the antimalarial drug artemisinin. J Biol Chem. 1998 Jun 26;273(26):16192-8.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

Produk: 5 • International brands: 0
Produk
  • Eurartesim
    Tablet, film coated • - • Oral • EU • Approved
  • Eurartesim
    Tablet, film coated • - • Oral • EU • Approved
  • Eurartesim
    Tablet, film coated • - • Oral • EU • Approved
  • Eurartesim
    Tablet, film coated • - • Oral • EU • Approved
  • Eurartesim
    Tablet, film coated • - • Oral • EU • Approved

Sekuens Gen/Protein (FASTA)

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