Artemether

Summary

Artemether (CHEMBL566534) is an approved small-molecule antimalarial (ATC P01BE02); indicated across 7 conditions including malaria and plasmodium falciparum malaria.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: P01BE02
• Indications: 7 conditions
• Clinical trials: 36
• Chemistry: 298.37 Da · C16H26O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL566534
Name	Artemether
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	68911
ChEBI	CHEBI:195280
ATC	P01BE02
Molecular formula	C16H26O5
Molecular weight	298.37
InChIKey	SXYIRMFQILZOAM-HVNFFKDJSA-N

SMILES: C[C@@H]1CC[C@H]2[C@H]([C@H](O[C@H]3[C@@]24[C@H]1CC[C@](O3)(OO4)C)OC)C

IUPAC name: (1R,4S,5R,8S,9R,10S,12R,13R)-10-methoxy-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecane

ChEBI definition: An artemisinin derivative that is artemisinin in which the lactone has been converted to the corresponding lactol methyl ether. It is used in combination with lumefantrine as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.

Pharmacological roles (ChEBI): antimalarial.

Also known as: .beta.-artemether, Artemetero, Artemether, Artemether component of coartem, Artemetherum, Artesaph, Artemetheri, Dihydroartemisinin impurity g, Falcidol, Gvither, Larither, Malartem

Patent coverage: 63 distinct patent families (88 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Prelamin-A/C, Prostaglandin E synthase 2.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
LMNA	6.25	Potency	562.3	nM	CHEMBL_ACT_3622827
PTGES2	5.14	IC50	7200	nM	CHEMBL_ACT_25967628

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

7 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
malaria	4	MONDO:0005136	EFO:0001068
Plasmodium falciparum malaria	3	MONDO:0005920	EFO:0007444
Plasmodium vivax malaria	3	MONDO:0005921	EFO:0007445
urinary schistosomiasis	2	MONDO:0006001	EFO:0007530
neoplasm	1	MONDO:0005070	EFO:0000616
HIV infectious disease	1	MONDO:0005109	EFO:0000764

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 36.

Phase distribution

Phase	Trials
PHASE4	17
PHASE3	5
Not specified	5
PHASE1	4
PHASE2	3
PHASE1/PHASE2	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04704999	PHASE4	RECRUITING	Southeast Asia Dose Optimization of Tafenoquine
NCT07403643	PHASE4	NOT_YET_RECRUITING	Investigating the Pharmacology of Tafenoquine in Papua New Guinean Children With Uncomplicated Malaria
NCT00451139	PHASE4	COMPLETED	Ototoxicity of Artemether / Lumefantrine (Coartem) and Other Antimalarials
NCT00495508	PHASE4	COMPLETED	Quinine vs. Artemether/Lumefantrine in Uncomplicated Malaria During Pregnancy
NCT00529867	PHASE4	COMPLETED	Randomised Efficacy Study of Two Artemether-Lumefantrine Oral Formulations for the Treatment of Uncomplicated P. Falciparum Malaria
NCT00790881	PHASE4	COMPLETED	Artemether/Lumefantrine and Nevirapine Interaction Study in HIV-infected Adults
NCT00869700	PHASE4	COMPLETED	Pharmacokinetic Interaction Between the Antimalarial Combination Artemether/Lumefantrine and Combination Antiretroviral Therapy Including Lopinavir/Ritonavir in HIV-infected Adults
NCT01728961	PHASE4	TERMINATED	Pharmacology of Antimalarial Therapy With or Without Antiretroviral Therapy
NCT01906788	PHASE4	UNKNOWN	The Optimal Timing Of Primaquine To Prevent Malaria Transmission After Artemisinin-Combination Therapy
NCT01976780	PHASE4	COMPLETED	In Vivo and In Vitro Efficacy of Artemisinin Combination Therapy
NCT01998295	PHASE4	COMPLETED	Parasite Clearance Time and Time to Recurrent Infection Following Treatment With Artemether/Lumefantrine
NCT02143934	PHASE4	COMPLETED	Effect of Liver and Blood-stage Treatment on Subsequent Plasmodium Reinfection and Morbidity
NCT02742285	PHASE4	COMPLETED	Lumefantrine in Venous Plasma Versus Dried Capillary Blood Spot
NCT04565184	PHASE4	COMPLETED	Effectiveness and Safety of Artesunate-Amodiaquine and Artemether-Lumefantrine for the Treatment of Malaria in Yaounde
NCT04767191	PHASE4	COMPLETED	Malaria Therapeutic Efficacy Study (TES) Kenya
NCT05605925	PHASE4	UNKNOWN	Ivermectin-artemisinin Combination Therapy for Eradication of Malaria
NCT06300970	PHASE4	COMPLETED	Efficacy of Artesunate-amodiaquine and Artemether-lumefantrine for Treatment of Plasmodium Falciparum Malaria in Liberia
NCT00123552	PHASE3	COMPLETED	Longitudinal Antimalarial Combinations in Uganda
NCT01152931	PHASE3	COMPLETED	Antioxidant Micronutrients in Malaria
NCT01374581	PHASE3	COMPLETED	Impact of Artemisinin-based Combination Therapy and Quinine on Treatment Failure and Resistance in Uncomplicated Malaria
NCT01625871	PHASE3	COMPLETED	Artemether/Lumefantrine and Vivax Malaria
NCT01899820	PHASE3	UNKNOWN	Evaluation of the Efficacy of Artemisinin Combination Therapy in Kenya
NCT07559370	PHASE2	RECRUITING	Safety and Efficacy of Imatinib in Combination With Artemether-Lumefantrine for Uncomplicated Malaria
NCT01047436	PHASE2	COMPLETED	Efficacy of ArTiMist™ in Children
NCT02263950	PHASE1/PHASE2	UNKNOWN	A Phase 1/2a Study of LON002 in Subjects With Advanced Solid Tumours
NCT04280692	PHASE1/PHASE2	SUSPENDED	Controlled Human Malaria Infection Transmission Model - Phase A
NCT04661579	PHASE2	COMPLETED	Study of Malaria Vaccine RTS,S/AS01E in Plasmodium Falciparum-infected and Uninfected Adults Pre-treated With Anti-malarial Therapy
NCT00697892	PHASE1	COMPLETED	Pharmacokinetic Interactions Between Antiretroviral Agents and Antimalarial Drug Combinations
NCT01876966	PHASE1	COMPLETED	Interaction Between Etravirine or Darunavir/Ritonavir and Artemether / Lumefantrine
NCT02184637	PHASE1	COMPLETED	A Study to Evaluate the Pharmacokinetics of a Single Dose of Tafenoquine Co-administered With Either Artemether + Lumefantrine or Dihydroartemisinin + Piperaquine Tetraphosphate
NCT06294912	PHASE1	COMPLETED	A Study to Evaluate Antimalarial Activity and Safety of MK-7602 in Healthy Adults (MK-7602-003)
NCT00229775	Not specified	COMPLETED	Efficacy of Chloroquine + Sulfadoxine Pyrimethamine Versus Artemether + Lumefantrine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in the Philippines
NCT00304980	Not specified	TERMINATED	Comparative Evaluation of the Safety and the Efficacy of 2 Antimalarials Depending on HIV Status
NCT02213211	Not specified	COMPLETED	School-based Programme of Malaria Diagnosis and Treatment in Southern Malawi
NCT04666350	Not specified	COMPLETED	Clinical Investigation Study to Evaluate the Consistency and Reproducibility of Two Consecutive Mosquito Feeding Assays
NCT07362498	Not specified	COMPLETED	Health Systems Implementation and Molecular Surveillance of Multiple First-Line Treatments for Uncomplicated Malaria in Western Kenya

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).