artemether

Small moleculeapprovedOrphan Drug ^FDAFast Track ^FDA

Approved

Apr 7, 2009

Artemether is an antimalarial agent used to treat acute uncomplicated malaria. It is administered in combination with lumefantrine for improved efficacy against malaria. Artemether is rapidly metabolized into an active metabolite dihydroartemisinin (DHA). The antimalarial activity of artemether and DHA has been attributed to endoperoxide moiety. Artemethe 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. Other mechanisms of action for artemether include their ability to reduce fever by production of signals to hypothalamus thermoregulatory center. Now, recent research has shown the presence of a new, previously unknown cyclooxygenase enzyme COX-3, found in the brain and spinal cord, which is selectively inhibited by artemether, and is distinct from the two already known cyclooxygenase enzymes COX-1 and COX-2. It is now believed that this selective inhibition of the enzyme COX-3 in the brain and spinal cord explains the ability of artemether in relieving pain and reducing fever which is produced by malaria. The most common adverse reactions in adults (>30%) are headache, anorexia, dizziness, asthenia, arthralgia and myalgia. — NCATS

Clinical trial activity

187 trials · 210 clinical orgs · 1 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Jan 1, 2000 (NCT00140361)

Timeline

2000s

Jan 1, 2002
Novartis — Earliest Phase 3 Sponsor(trial)
Jan 1, 2005
Earliest Phase 1 Sponsor(trial)
Aug 31, 2007
Orphan Drug Designation
Jan 1, 2008
Earliest Phase 2 Sponsor(trial)
Apr 7, 2009
Earliest FDA Approval
Apr 7, 2009
Novartis — NDA Secondary Org
Apr 8, 2009
Novartis — First NDA Organization
Apr 8, 2009
Novartis — NDA Organization

Indications

Approved for

Studied for

Mechanism of action

Ferriprotoporphyrin IXINHIBITOR
Ferriprotoporphyrin IX inhibitor
prevents crystallisation
Plasmodium malariaeINHIBITOR
Plasmodium malariae inhibitor

Combination products

coartem
with lumefantrine
Also known as artemether/ lumefantrine

Approval history

approvedPriority reviewFast trackApr 7, 2009

Chemistry & pharmacology

Loading structure…

SMILES

CO[C@H]1O[C@@H]2O[C@]3(C)CC[C@H]4[C@H](C)CC[C@@H]([C@H]1C)[C@@]24OO3

Mol. weight: 298.3746 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Single Stereoisomer
Inorganic: No
Polymer: No
Delivery: Oral
Availability: Prescription Only

Oral

Yes

Parenteral

Topical

First in classProdrug

Sources

Also known as

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
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
(1r,4s,5r,8s,9r,10s,12r,13r)-10-methoxy-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0^{4,13}.0^{8,13}]hexadecane
(1r,4s,5r,8s,9r,10s,12r,13r)-10-methoxy-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0^{4,13}.0^{8,13}]hexadecane
(3r-(3.alpha.,5a.beta.,6.beta.,8a.beta.,9.alpha.,10.alpha.,12.beta.,12ar*))-decahydro-10-methoxy-3,6,9-trimethyl-3,12-epoxy-12h-pyrano(4.3-j)-1,2-benzodioxepin
alpha-artemether
artemetero
artemetero
artemether
artemether
artemether
artemether
artemether
artemether
artemether
artemether
artemether
artemether, (3r-(3alpha,5abeta,6alpha,8abeta,9alpha,10beta,12beta,12ar*))-isomer
artemether, (3r-(3alpha,5abeta,6beta,8aalpha,9alpha,10beta,12beta,12ar*))-isomer
artemether, (3r-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,12ar*))-isomer
artemether - benflumetol
artemether-benflumetol combination
artemether, benflumetol drug combination
artemetheri
artemetheri
artemether-lumefantrine combination
artemetherum
artemetherum
artemisininelactol methyl ether
artemisininelactol methyl ether
artemos
artenam
artenam
artesaph
arthemeter
arthemeter
beta-artemether
beta-artemether
beta-artemether
beta-arthemeter
beta-dihydroartemisinin methyl ether
beta-dihydroartemisinin methyl ether
cgp 56697
cgp-56697
coartem
coartem
coartem
coartemether
co-artemether
co-artemether
dihydroartemisinin methyl ether
dihydroartemisinin methyl ether
dihydroartemisinin methyl ether
dihydroqinghaosu methyl ether
dihydroqinghaosu methyl ether
falcidol
gvither
malartem
methyl-dihydroartemisinine
methyl-dihydroartemisinine
o-methyldihydroartemisinine
sm-224
sm-224

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT06967519	Phase 4	Dec 31, 2025	National Institutes of Health (NIH), Yale University
NCT07192900	Phase 1	Oct 31, 2025	Allegheny Health Network, Iovance, Miltenyi Biotec, Inc., University of Pittsburgh
NCT06962319	Phase 3	Sep 30, 2025	Medicines for Malaria Venture, University of Liverpool
NCT06424002	Phase 4	Jun 1, 2024	Boston University, Government of Malawi, Kamuzu University of Health Sciences, Michigan State University
NCT06347471	Phase 4	May 28, 2024	Infectious Disease Institute, Kampala, Uganda, Radboud University, University of London
NCT06294912	Phase 1	Apr 18, 2024	Merck
NCT07235033	Phase 2	Jan 23, 2024	Novartis
NCT05951595	Phase 3	Jan 1, 2024	Mahidol University, University of Oxford
NCT05750628	Phase 2	Dec 26, 2023	Novartis
NCT05842954	Phase 3	Dec 11, 2023	Novartis
NCT05757167	Phase 4	Nov 6, 2023	Duke University, National Institute of Allergy and Infectious Diseases (NIAID)
NCT06076213	Phase 4	May 1, 2023	Centers for Disease Control and Prevention (CDC), Global Health Innovative Technology Fund, Government of the Democratic Republic of the Congo
NCT05567016	Phase 3	Apr 30, 2023	Chan Zuckerberg Initiative, Ifakara Health Institute, National Institute of Allergy and Infectious Diseases (NIAID), Stanford University, University of Basel, University of California, San Francisco
NCT05764746	Phase 2/Phase 3 (Phase 3)	Apr 1, 2023	Muhimbili University, The Swedish Research Council, Uppsala University
NCT06154018	N/A	Mar 18, 2023	University of Ioannina
NCT05550909	Phase 2	Oct 17, 2022	Malaria Research and Training Center, Bamako, Mali, University of London
NCT06300970	Phase 4	Aug 9, 2022	Centers for Disease Control and Prevention (CDC), Government of Liberia
NCT05605925	Phase 4	Aug 4, 2022	Makerere University
NCT05340153	Phase 4	Apr 11, 2022	Association Camerounaise pour le Marketing Social (ACMS), Cameroon, Government of Cameroon, Impact Malaria, Cameroon, University of Yaounde
NCT05343312	Phase 4	Mar 16, 2022	United States Agency for International Development

Showing 20 of 187 trials

Page 1 / 10

Organizations

Research & Development (210)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
University of London	Academic/Hospital	26	12	4	2004
Centers for Disease Control and Prevention (CDC)	Government	21	14	3	2000
University of Oxford	Academic/Hospital	16	15	5	2008
Novartis	For profit	14	13	3	2001
University of California, San Francisco	Academic/Hospital	10	9	3	2004
Karolinska Institute	Academic/Hospital	9	4	1	2002
Mahidol University	Academic/Hospital	9	0	5	2006
Makerere University	Academic/Hospital	9	4	4	2007
Medicines for Malaria Venture	Academic/Hospital	9	4	2	2007
United States Agency for International Development	Government	9	0	2	2000
Institute of Tropical Medicine, Belgium	Academic/Hospital	8	3	4	2003
Kenya Medical Research Institute	Academic/Hospital	7	1	4	2007
Radboud University	Academic/Hospital	7	2	4	2009
World Health Organization	Government	7	0	3	2002
Centre Muraz	Academic/Hospital	6	3	2	2007
Muhimbili University	Academic/Hospital	6	5	2	2006
University of Liverpool	Academic/Hospital	6	4	3	2007
Wellcome Trust	Academic/Hospital	6	0	3	2004
Menzies School of Health Research	Academic/Hospital	5	4	3	2004
National Institute of Allergy and Infectious Diseases (NIAID)	Government	5	1	3	2004

210 organizations

Page 1 / 11

Marketing (2)

Organization	Org type	Relationship	Date
Novartis	For profit	NDA2	Apr 7, 2009
Novartis	For profit	NDA	Apr 8, 2009