General
Preferred name
ARTEMETHER
Synonyms
Dihydroartemisinin methyl ether ()
SM224 ()
Dihydroqinghaosu methyl ether ()
CGP 56696 ()
SM-224 ()
Artemetheri ()
.beta.-artemether ()
Dihydroartemisinin impurity g ()
NSC-759820 ()
Artemetherum ()
Artesaph ()
Larither ()
Malartem ()
Paluther ()
Gvither ()
SM 224 ()
NSC-665970 ()
Falcidol ()
Artemether-d3 ()
P&D ID
PD003141
CAS
159573-83-8
71963-77-4
93787-85-0
Tags
prodrug
natural product
drug
available
Approved by
FDA
First approval
2009
Drug Status
approved
Drug indication
Malaria
Max Phase
Phase 4
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Artemether is a semisynthetic derivative of , a natural product isolated from the quinghaosu or sweet wormwood plant (Artemisia annua).
Artemether is a prodrug that is converted to the active metabolite (dihydroartemisinin). It has potent antimalarial activity against the asexual blood stage of P. falciparum (including chloroquine-resistant strains) and is characterised by an extremely rapid parasitemia clearance.
Artemether is listed in the WHO 20th Essential Medicines List (2017) as an antimalarial for use in the management of severe malaria. It is also listed as a curative treatment for uncomplicated malaria in combination with . This is one of the artemisinin-based combination therapies (ACTs) recommended in the WHO Guidelines for the treatment of malaria .
Potential Target/Mechanism Of Action: As the precise mechanism of action of artemether is not yet known, we do not have a molecular target for this compound.
Artemether is a prodrug that is converted to the active metabolite (dihydroartemisinin). It has potent antimalarial activity against the asexual blood stage of P. falciparum (including chloroquine-resistant strains) and is characterised by an extremely rapid parasitemia clearance.
Artemether is listed in the WHO 20th Essential Medicines List (2017) as an antimalarial for use in the management of severe malaria. It is also listed as a curative treatment for uncomplicated malaria in combination with . This is one of the artemisinin-based combination therapies (ACTs) recommended in the WHO Guidelines for the treatment of malaria .
Potential Target/Mechanism Of Action: As the precise mechanism of action of artemether is not yet known, we do not have a molecular target for this compound.
MOA
Involves an interaction with ferriprotoporphyrin IX (âhemeâ), or ferrous ions, in the acidic parasite food vacuole, which results in the generation of cytotoxic radical species. ; ; The generally accepted mechanism of action of peroxide antimalarials involves interaction of the peroxide-containing drug with heme, a hemoglobin degradation byproduct, derived from proteolysis of hemoglobin. This interaction is believed to result in the formation of a range of potentially toxic oxygen and carbon-centered radicals.
DESCRIPTION
Artemether is a semisynthetic derivative of , a natural product isolated from the qinghao or sweet wormwood plant (Artemisia annua). Synthesis yields two crystalline anomers, α- and β-artemether, the latter predominates and is marginally more active .
Artemether is a prodrug that is converted to the active metabolite (dihydroartemisinin).
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY. (GtoPdb)
Artemether is a prodrug that is converted to the active metabolite (dihydroartemisinin).
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY. (GtoPdb)
DESCRIPTION
Artemether is a semisynthetic derivative of , a natural product isolated from the quinghaosu or sweet wormwood plant (Artemisia annua). Synthesis yields two crystalline anomers, α- and β-artemether, the latter predominates and is marginally more active .
Artemether is a prodrug that is converted to the active metabolite (dihydroartemisinin). It has potent antimalarial activity against the asexual blood stage of P. falciparum (including chloroquine-resistant strains) and is characterised by an extremely rapid parasitemia clearance.
Artemether is listed in the WHO 20th Essential Medicines List (2017) as an antimalarial for use in the management of severe malaria. It is also listed as a curative treatment for uncomplicated P. falciparum malaria in combination with . This is one of the artemisinin-based combination therapies (ACTs) recommended in the WHO Guidelines for the treatment of malaria .
Potential Target/Mechanism Of Action: As the precise mechanism of action of artemether is not yet known, we do not have a molecular target for this compound.
Artemether is a prodrug that is converted to the active metabolite (dihydroartemisinin). It has potent antimalarial activity against the asexual blood stage of P. falciparum (including chloroquine-resistant strains) and is characterised by an extremely rapid parasitemia clearance.
Artemether is listed in the WHO 20th Essential Medicines List (2017) as an antimalarial for use in the management of severe malaria. It is also listed as a curative treatment for uncomplicated P. falciparum malaria in combination with . This is one of the artemisinin-based combination therapies (ACTs) recommended in the WHO Guidelines for the treatment of malaria .
Potential Target/Mechanism Of Action: As the precise mechanism of action of artemether is not yet known, we do not have a molecular target for this compound.
DESCRIPTION
Multidrug resistance protein (MRP) 4 inhibitor
(Tocris Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
6
Organisms
8
Compound Sets
20
CeMM library of unique drugs (CLOUD)
ChEMBL Approved Drugs
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Enamine BioReference Compounds
Guide to Pharmacology
MedChem Express Bioactive Compound Library
Natural product-based probes and drugs
NCATS Inxight Approved Drugs
NIH Clinical Collections (NCC)
NPC Screening Collection
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
37
Molecular Weight
298.18
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
0
Rotatable Bonds
1
Ring Count
5
Aromatic Ring Count
0
cLogP
2.84
TPSA
46.15
Fraction CSP3
1.0
Chiral centers
8.0
Largest ring
7.0
QED
0.7
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
MOA
protozoal calcium transporting ATPase inhibitor
Antibiotic
antimalarial agent
Target
Ferriprotoporphyrin IX
antibiotic
ATP1A1
Parasite
Pathway
Microbiology&virology
Anti-infection
Primary Target
Antimalarials
Indication
malaria
Biosynthetic Origin
Terpenoid
Therapeutic Indication
Antiparasitic
Therapeutic Class
Antimicrobial
Source data
