General
Preferred name
ARTEMETHER
Synonyms
SM224 ()
Dihydroartemisinin methyl ether ()
Dihydroqinghaosu methyl ether ()
CGP 56696 ()
SM-224 ()
Artemetheri ()
Paluther ()
Larither ()
Gvither ()
Artemetherum ()
Falcidol ()
NSC-759820 ()
Malartem ()
Dihydroartemisinin impurity g ()
Artesaph ()
NSC-665970 ()
SM 224 ()
.beta.-artemether ()
Artemetero ()
Artemether component of coartem ()
Artemether-d3 ()
P&D ID
PD003141
CAS
159573-83-8
71963-77-4
93787-85-0
Tags
available
prodrug
drug
Approved by
FDA
First approval
2009
Drug indication
Malaria
Neoplasm
Drug Status
approved
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.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.
MOA Involves an interaction with ferriprotoporphyrin IX (“heme”), 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)
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.
DESCRIPTION Artemether is an anti-malarial compound that targets drug-resistant strains of falciparum malaria[1].
PRICE 29
DESCRIPTION Multidrug resistance protein (MRP) 4 inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Artemether is an antimalarial agent used in combination with lumefantrine for the treatment of acute uncomplicated malaria caused by Plasmodium falciparum. (Enamine Bioactive Compounds)
DESCRIPTION Artemether (CGP 56696) is an antimalarial agent used to treat acute uncomplicated malaria. (TargetMol Bioactive Compound Library)
Cell lines
7
Organisms
6
Compound Sets
22
Cayman Chemical Bioactives
CeMM library of unique drugs (CLOUD)
ChEMBL Approved Drugs
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Enamine Bioactive Compounds
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
External IDs
42
Properties
(calculated by RDKit )
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
Custom attributes
(extracted from source data)
MOA
protozoal calcium transporting ATPase inhibitor
Antibiotic
antimalarial agent
Target
Ferriprotoporphyrin IX
antibiotic
Parasite
ATP1A1
Primary Target
Antimalarials
Indication
malaria
Pathway
Microbiology/virology
Anti-infection
Biosynthetic Origin
Terpenoid
Therapeutic Indication
Antiparasitic
Therapeutic Class
Antimicrobial
Source data