General Information of Drug (ID: DM48QOT)

Drug Name
Artemether Drug Info
Synonyms
Artemetero; Artemether[inn]; Artemetheri; Artemetherum; Artemos; Artenam; Artesaph; Artesian; Artimist; Artmether; Falcidol; Gvither; Malartem; Paluther; Rither; Arteannuin ether; Artemether [INN]; Artemisininelactol methyl ether; Dihydroartemisinin methyl ether; Dihydroquinghaosu methyl ether; SM 224; SM 229; Alpha-Artemether; Alpha-Dihydroartemisinin methyl ether; Artemetero [INN-Spanish]; Artemether (INN); Artemetherum [INN-Latin]; Beta-Artemether; Beta-Dihydroartemisinin methyl ether; Methyl-dihydroartemisinine; O-Methyldihydroartemisinine; SM-224; Beta-Methylether of 11-epi-dihydroartemisinin; Artemether, (3R-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,12aR*))-isomer; (3R,5aS,6R,8aS,9R,10S,12R,12aR)-10-methoxy-3,6,9-trimethyldecahydro-3,12-epoxypyrano[4,3-j][1,2]benzodioxepine; (3R,5aS,6R,8aS,9R,10S,12R,12aR)-Decahydro-10-methoxy-3,6,9-trimethyl-3,12-epoxy-12H-pyrano(4,3-j)-1,2-benzodioxepin; (3alpha,5abeta,6beta,8abeta,9alpha,10beta,12beta,12aR*)-isomer of artemether; (3r,5as,6r,8as,9r,10r,12r,12ar)-10-methoxy-3,6,9-trimethyldecahydro-3,12-epoxy[1,2]dioxepino[4,3-i]isochromene; (5aS,6R,8aS,9R,10S,12R,12aR)-10-methoxy-3,6,9-trimethyldecahydro-3,12-epoxy[1,2]dioxepino[4,3-i]isochromene; 10-methoxy-1,5,9-trimethyl-(1R,4S,5R,8S,9R,10S,12R,13R)-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecane; 3,12-Epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin, decahydro-10-methoxy-3,6,9-tri
Indication
Disease Entry ICD 11 Status REF
Malaria 1F40-1F45 Approved [1]
Cross-matching ID
PubChem CID
68911
ChEBI ID
CHEBI:195280
CAS Number
CAS 71963-77-4
TTD Drug ID
DM48QOT
INTEDE Drug ID
DR0140

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Sodium pump subunit alpha-1 (ATP1A1) TTWK8D0 AT1A1_HUMAN Binder [1]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [2]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Approved [3]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Approved [4]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Approved [3]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Approved [5]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Approved [6]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Sodium pump subunit alpha-1 (ATP1A1) DTT ATP1A1 7.891 11.257 11.348 10.906
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.867 5.142 5.52 7.08
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 3.307 5.005 3.921 5.327
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 11.76 5.931 6.164 9.423
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Malaria
ICD Disease Classification 1F40-1F45
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Sodium pump subunit alpha-1 (ATP1A1) DTT ATP1A1 4.66E-01 1.00E-02 0.06
Sodium pump subunit alpha-1 (ATP1A1) DTT ATP1A1 3.31E-01 -0.03 -0.19
Cytochrome P450 2B6 (CYP2B6) DME CYP2B6 2.10E-02 9.95E-02 3.65E-01
Cytochrome P450 2B6 (CYP2B6) DME CYP2B6 2.07E-03 -2.31E-01 -5.10E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 6.74E-01 5.99E-02 7.30E-02
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 3.51E-01 1.59E-01 2.09E-01
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 4.79E-03 1.32E-01 7.85E-01
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 1.82E-01 -1.71E-02 -9.86E-02
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 8.01E-02 6.73E-02 3.36E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 2.91E-04 1.41E-01 6.14E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 7.33E-02 5.59E-02 2.99E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 5.65E-03 -7.28E-02 -1.24E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 2.13E-01 4.03E-02 2.50E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 8.21E-02 8.17E-02 4.35E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 The fight against drug-resistant malaria: novel plasmodial targets and antimalarial drugs. Curr Med Chem. 2008;15(2):161-71.
2 The effect of grapefruit juice on the time-dependent decline of artemether plasma levels in healthy subjects. Clin Pharmacol Ther. 1999 Oct;66(4):408-14.
3 The contribution of the enzymes CYP2D6 and CYP2C19 in the demethylation of artemether in healthy subjects. Eur J Drug Metab Pharmacokinet. 1998 Jul-Sep;23(3):429-36.
4 Pharmacokinetic interaction between etravirine or darunavir/ritonavir and artemether/lumefantrine in healthy volunteers: a two-panel, two-way, two-period, randomized trial. HIV Med. 2013 Aug;14(7):421-9.
5 Effect of pharmacogenetics on plasma lumefantrine pharmacokinetics and malaria treatment outcome in pregnant women. Malar J. 2017 Jul 3;16(1):267.
6 Insights into CYP2B6-mediated drug-drug interactions. Acta Pharm Sin B. 2016 Sep;6(5):413-425.