Artemisinin

Summary

Artemisinin (CHEMBL269671) is a phase-3 clinical-stage small-molecule antimalarial (ATC P01BE01); indicated across 3 conditions including malaria and severe acute respiratory syndrome.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: P01BE01
• Indications: 3 conditions
• Clinical trials: 70
• Chemistry: 282.33 Da · C15H22O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL269671
Name	Artemisinin
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	68827
ChEBI	CHEBI:223316
ATC	P01BE01
Molecular formula	C15H22O5
Molecular weight	282.33
InChIKey	BLUAFEHZUWYNDE-NNWCWBAJSA-N

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

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

ChEBI definition: A sesquiterpene lactone obtained from sweet wormwood, Artemisia annua, which is used as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.

Pharmacological roles (ChEBI): antimalarial.

Other ChEBI roles (chemical / environmental): plant metabolite.

Also known as: (+)-artemisinin, Artemisinin, Artemisinina, Artemisinine, Artemisininum, GNF-PF-5341, Huanghuahaosu, NSC-369397, Qing hau sau, artemisnin, artemisinin, Artemisinin analogue

Patent coverage: 7,139 distinct patent families (15,668 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: 7 (assay-derived). Sample: Ferritin light chain, Cytochrome P450 1A2, Cytochrome P450 3A4, Nuclear receptor subfamily 1 group I member 2, Aldehyde dehydrogenase 1A1, Prostaglandin E synthase 2, Cytochrome P450 2B6.

Bioactivity

ChEMBL activities: 10 potent at pChembl ≥ 5 of 19 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PTGES2	6.28	Kd	530	nM	CHEMBL_ACT_25967691
CYP2B6	6.22	EC50	600	nM	CHEMBL_ACT_15466352
CYP1A2	5.7	IC50	2000	nM	CHEMBL_ACT_7610224
CYP2B6	5.34	Ki	4600	nM	CHEMBL_ACT_15466343
CYP3A4	5.23	EC50	5900	nM	CHEMBL_ACT_15466273
CYP2B6	5.08	IC50	8400	nM	CHEMBL_ACT_15466347
PTGES2	5.06	IC50	8800	nM	CHEMBL_ACT_25967625
PTGES2	5.06	IC50	8800	nM	CHEMBL_ACT_25967674
PTGES2	5.05	IC50	8900	nM	CHEMBL_ACT_25967692
PTGES2	5	IC50	9900	nM	CHEMBL_ACT_25967672

Target pathways

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

Indications & clinical

Indications

3 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
severe acute respiratory syndrome	2	MONDO:0005091	MONDO:0100096

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

Clinical trials

Total trials: 70.

Phase distribution

Phase	Trials
Not specified	25
PHASE3	13
PHASE2	11
PHASE4	8
PHASE1	6
PHASE2/PHASE3	3
PHASE1/PHASE2	2
EARLY_PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07322068	PHASE4	NOT_YET_RECRUITING	Perennial Malaria Chemoprevention in the Malaria Vaccine Era
NCT01887821	PHASE4	COMPLETED	Antimalarial Drug Susceptibility and Molecular Characterization of Plasmodium Vivax Isolates in Vietnam
NCT01930331	PHASE4	COMPLETED	Safety, Tolerability, Pharmacokinetics and Efficacy of ARCO
NCT02775929	PHASE4	COMPLETED	Partners Demonstration Project of PrEP and ART
NCT03052010	PHASE4	COMPLETED	The Partners Scale-Up Project
NCT04767191	PHASE4	COMPLETED	Malaria Therapeutic Efficacy Study (TES) Kenya
NCT05004753	PHASE4	COMPLETED	A Study to Evaluate the Safety and Efficacy of Artemisinin- a Herbal Supplement on COVID-19 Subjects
NCT05465135	PHASE4	COMPLETED	The Effect of Dihydroartemisinin in PCOS
NCT05631093	PHASE3	ACTIVE_NOT_RECRUITING	A Switch to Doravirine/Islatravir (DOR/ISL) in Participants With Human Immunodeficiency Virus Type 1 (HIV-1) Who Are Virologically Suppressed on Antiretroviral Therapy (ART) (MK-8591A-051)
NCT06694805	PHASE3	RECRUITING	A Study to Evaluate the Effectiveness of Long-acting (LA) Cabotegravir (CAB) + Rilpivirine (RPV) LA When Given to Participants With Detectable HIV-1
NCT00128388	PHASE2/PHASE3	COMPLETED	Psychodynamic Therapy for Treating Panic Disorder
NCT00682578	PHASE3	COMPLETED	A Comparative Study of Artekin With Standard Malarial Treatment Regimes in Afghanistan
NCT01009671	PHASE3	UNKNOWN	Study to Evaluate the Digestive Tolerability of ART44 Versus ART®50 in Patients With Osteoarthritis of the Knee
NCT01288820	PHASE3	COMPLETED	Study of ACTs Plus Primaquine for Uncomplicated Plasmodium Vivax Malaria
NCT01391403	PHASE3	COMPLETED	Artemisinin With Risperidone for First-Episode and Drug-Naive Schizophrenia
NCT01899820	PHASE3	UNKNOWN	Evaluation of the Efficacy of Artemisinin Combination Therapy in Kenya
NCT02974348	PHASE3	COMPLETED	Antimalaria Drugs Susceptibility Testing for an Effective Management of Infected Patients in Sub-Sahara Africa
NCT03037372	PHASE3	UNKNOWN	Statin Adjunct Therapy Among ART-treated Adults in Sub-Saharan Africa: Atorvastatin and Rosuvastatin Equivalence Trial
NCT04049916	PHASE2/PHASE3	COMPLETED	Pyronaridine-artesunate With Low Dose Primaquine for Preventing P. Falciparum Transmission
NCT04149106	PHASE3	UNKNOWN	Seasonal Malaria Chemoprevention With Dihydroartemisin Piperaquin vs. Sulfadoxine-pyrimethamin+Amodiaquin
NCT04223778	PHASE3	COMPLETED	Safety and Efficacy of a Switch to Doravirine/Islatravir in Participants With HIV-1 (MK-8591A-017)
NCT04654624	PHASE2/PHASE3	COMPLETED	Child Discomfort and Parental Acceptability of Silver Diamine Fluoride and Alternative Restorative Treatment
NCT04844099	PHASE3	COMPLETED	Dihydroartemisinin-Piperaquine or Sulphadoxine-Pyrimethamine for the Chemoprevention of Malaria in Sickle Cell Anaemia
NCT05946642	PHASE3	UNKNOWN	Innovative Intermittent Preventive Treatment Approaches to Reduce Malaria Burden in School-age Children in Burkina Faso
NCT05719441	PHASE2	RECRUITING	A Clinical Trial of Combination HIV-Specific Broadly Neutralizing Monoclonal Antibodies Combined With ART Initiation During Acute HIV Infection to Induce HIV Remission
NCT06842524	PHASE2	RECRUITING	Dihydroartemisinin for the Treatment of Polycystic Ovary Syndrome
NCT07557927	PHASE2	NOT_YET_RECRUITING	A Multicentre, Randomised, Double-blind, Positive-control Clinical Trial Evaluating Dihydroartemisinin Tablets for the Treatment of Discoid Lupus Erythematosus
NCT00000948	PHASE2	COMPLETED	Effects of Giving Interleukin-2 (IL-2) Plus Anti-HIV Therapy to HIV-Positive Patients With CD4 Cell Counts of at Least 350 Cells/mm3
NCT00731991	PHASE1/PHASE2	COMPLETED	Art and Surface Electromyography (EMG)
NCT03396393	PHASE2	UNKNOWN	Exploratory Study of DHA in Systemic Lupus Erythematosus Patients
NCT03707977	PHASE1/PHASE2	COMPLETED	Dual bNAb Treatment in Children
NCT04387240	PHASE2	WITHDRAWN	Evaluating the Efficacy of Artesunate in Adults With Mild Symptoms of COVID-19
NCT04609098	PHASE2	COMPLETED	Single Low Dose Tafenoquine to Reduce P. Falciparum Transmission in Mali (NECTAR2)
NCT04801017	PHASE2	UNKNOWN	A Study to Evaluate the Safety and Efficacy of OT-101+Artemisinin in Hospitalized COVID-19 Subjects
NCT05829187	PHASE2	COMPLETED	Momordica Charantia and Dihydroartemisinin-piperaquined-primaquine for Uncomplicated Plasmodium Falciparum Malaria Patients in Southwest Sumba Regency
NCT06036030	PHASE2	COMPLETED	Combination Momordica Charantia Extract and Primaquine Againts Plasmodium Falciparum Uncomplicated and Plasmodium Vivax Uncomplicated Treatment in Manokwari, West Papua
NCT06417099	PHASE2	COMPLETED	Efficacy of Dihydroartemisinin for Treating PCOS
NCT05890963	PHASE1	ACTIVE_NOT_RECRUITING	10E8.4/iMab Bispecific Antibody and VRC07-523LS Monoclonal Antibody in HIV-infected Adults
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
NCT03060447	PHASE1	COMPLETED	Study to Evaluate the Safety and Efficacy of Vesatolimod in Antiretroviral Treated Human Immunodeficiency Virus (HIV-1) Infected Controllers

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 1 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

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