Artesunate
drugOn this page
Also known as .alpha.-artesunic acidArsumaxArtesunate amivasArtesunatoArtesunatumArtesunic acidDihydroqinghaosu hemisuccinateLJPC-0118NSC-712571PlasmotrinQinghaozhiSaphnateZysunateDeoxoartemisitene derivativeArtesunateÊArtesunateÂ
Summary
Artesunate (CHEMBL361497) is an approved small-molecule antineoplastic agent (ATC P01BE03); indicated across 17 conditions including malaria and plasmodium falciparum malaria.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: P01BE03
- Indications: 17 conditions
- Clinical trials: 105
- Chemistry: 384.4 Da · C19H28O8
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL361497 |
| Name | Artesunate |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 6917864 |
| ChEBI | CHEBI:63918 |
| ATC | P01BE03 |
| Molecular formula | C19H28O8 |
| Molecular weight | 384.4 |
| InChIKey | FIHJKUPKCHIPAT-AHIGJZGOSA-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(=O)CCC(=O)O)C
IUPAC name: 4-oxo-4-[[(1R,4S,5R,8S,9R,10S,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-yl]oxy]butanoic acid
ChEBI definition: An artemisinin derivative that is the hemisuccinate ester of the lactol resulting from the reduction of the lactone carbonyl group of artemisinin. It is used, generally as the sodium salt, for the treatment of malaria.
Pharmacological roles (ChEBI): antimalarial, ferroptosis inducer, antineoplastic agent.
Also known as: .alpha.-artesunic acid, Arsumax, Artesunate, Artesunate amivas, Artesunato, Artesunatum, Artesunic acid, Dihydroqinghaosu hemisuccinate, LJPC-0118, NSC-712571, Plasmotrin, Qinghaozhi
Parent form; salt/anhydrous children: CHEMBL207675
Patent coverage: 232 distinct patent families (392 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: 1 (assay-derived). Sample: Prostaglandin E synthase 2.
Bioactivity
ChEMBL activities: 1 potent at pChembl ≥ 5 of 1 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| PTGES2 | 5.8 | IC50 | 1600 | nM | CHEMBL_ACT_25967629 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
17 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 |
| cytomegalovirus infection | 3 | MONDO:0005132 | EFO:0001062 |
| urinary schistosomiasis | 3 | MONDO:0006001 | EFO:0007530 |
| schistosomiasis | 3 | MONDO:0015254 | EFO:1001475 |
| severe acute respiratory syndrome | 3 | MONDO:0005091 | MONDO:0100096 |
| Crohn disease | 2 | MONDO:0005011 | EFO:0000384 |
| atopic conjunctivitis | 2 | MONDO:0005642 | EFO:0007141 |
| intestinal cancer | 2 | MONDO:0005814 | EFO:0007330 |
| colorectal neoplasm | 2 | MONDO:0005335 | MONDO:0005575 |
| hepatocellular carcinoma | 1 | MONDO:0007256 | EFO:0000182 |
| neoplasm | 1 | MONDO:0005070 | EFO:0000616 |
| breast neoplasm | 1 | MONDO:0021100 | MONDO:0007254 |
| Friedreich ataxia | 1 | MONDO:0100339 | MONDO:0100339 |
| idiopathic pulmonary fibrosis | 1 | MONDO:0800504 | EFO:0000768 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 105.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 25 |
| PHASE2 | 25 |
| PHASE3 | 20 |
| PHASE1 | 16 |
| Not specified | 14 |
| PHASE2/PHASE3 | 4 |
| PHASE1/PHASE2 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00445796 | PHASE4 | COMPLETED | Arsucam® (Artesunate + Amiodaquine) Efficacy and TOLerance |
| NCT00452907 | PHASE4 | COMPLETED | ACT MALI: Treatment of Malaria Based on Combination Therapies |
| NCT00465257 | PHASE4 | SUSPENDED | Efficacy of Artesunate + Amodiaquine Four Years After Its Introduction in Zanzibar |
| NCT00875030 | PHASE4 | COMPLETED | A Study Comparing Blood Levels After Single-Dose Administration Of Artesunate Sachets (Pfizer) Versus Single-Dose Administration Of Arsuamoon® Tablets (Guilin-China) In Healthy Subjects |
| NCT00978172 | PHASE4 | COMPLETED | Safety and Efficacy Study of Artesunate and Mefloquin in Children With Uncomplicated Malaria |
| NCT01023399 | PHASE4 | COMPLETED | Artesunate Plus Amodiaquine in Malaria in Cote d’Ivoire |
| NCT01082731 | PHASE4 | TERMINATED | Efficacy of Artemisinin Combination Therapies for the Treatment of Uncomplicated P. Falciparum in Pregnancy in Brazil |
| NCT01107145 | PHASE4 | TERMINATED | Efficacy of Artemisinin Combination Therapies for the Treatment of Uncomplicated P. Vivax in Pregnancy in Brazil (PAACT-PV) |
| NCT01190371 | PHASE4 | UNKNOWN | Have Malaria Infections in Kenya Become Less Responsive to Artemisinin Treatment? |
| NCT01350856 | PHASE4 | COMPLETED | Tracking Resistance to Artemisinin (TRAC) |
| NCT01662700 | PHASE4 | UNKNOWN | Comparison of Two Antimalarial Drugs Regimens in Patient With Plasmodium Vivax Malaria in Thailand |
| NCT01805232 | PHASE4 | UNKNOWN | Intravenous Artesunate and Malaria |
| NCT01976780 | PHASE4 | COMPLETED | In Vivo and In Vitro Efficacy of Artemisinin Combination Therapy |
| NCT02052323 | PHASE4 | COMPLETED | Harmonized AS/MQ Efficacy Study - Thailand |
| NCT02084602 | PHASE4 | COMPLETED | Assessment of Artesunate/Mefloquine in the Peruvian Amazon |
| NCT02092766 | PHASE4 | COMPLETED | Parenteral Artesunate Compared to Quinine as a Cause of Late Anaemia in African Children With Malaria |
| NCT02653898 | PHASE4 | UNKNOWN | Malaria Elimination Pilot Study in Military Forces in Cambodia |
| NCT03201770 | PHASE4 | COMPLETED | Cohort Event Monitoring Study of Pyramax® |
| NCT03214731 | PHASE4 | UNKNOWN | Efficacy and Safety of Artesunate Plus Standard of Care in Active Lupus Nephritis |
| NCT03431714 | PHASE4 | COMPLETED | Efficacy and Safety of ASAQ and PD for the Treatment of Uncomplicated Falciparum Malaria in Mainland Tanzania |
| NCT03726593 | PHASE4 | UNKNOWN | Drug Combinations of Atovaquone-Proguanil (AP) With ACT |
| NCT03768908 | PHASE4 | COMPLETED | Efficacy of Artesunate + Amodiaquine Versus Artemether-lumefantrine for Falciparum Malaria in Zanzibar, 2005 |
| NCT04706130 | PHASE4 | COMPLETED | Rigorous Assessment of P. Vivax Relapses and Primaquine Efficacy for Radical Cure |
| NCT05273242 | PHASE4 | UNKNOWN | Add-on Study on WHO Solidarity Trial Plus for COVID-19 in Nepal |
| NCT05750459 | PHASE4 | COMPLETED | Pharmacokinetic Study of IV Artesunate to Treat Children With Severe Malaria |
| NCT00123552 | PHASE3 | COMPLETED | Longitudinal Antimalarial Combinations in Uganda |
| NCT00132548 | PHASE3 | COMPLETED | A Trial of Four Drug Regimens for the Prevention of Malaria in Senegalese Children |
| NCT00158548 | PHASE3 | COMPLETED | ACT With Chloroquine, Amodiaquine & Sulphadoxine-pyrimethamine in Pakistan |
| NCT00284687 | PHASE3 | COMPLETED | Artesunate in Preemptive Treatment of Human Cytomegalovirus (CMV) in Stem Cell Transplant Recipients |
| NCT00316329 | PHASE3 | COMPLETED | ATAQ EASY: Artesunate + Amodiaquine Fixed Dose Combination in the Treatment of Uncomplicated Plasmodium Falciparum Malaria |
| NCT00373607 | PHASE3 | COMPLETED | Efficacy and Safety of Dihydroartemisinin/Piperaquine (Artekin®) for the Treatment of Uncomplicated Malaria in Peru |
| NCT00378625 | PHASE3 | COMPLETED | Efficacy, Effect on Gametocytes and Tolerability of the Addition of Artesunate to Amodiaquine in Colombia |
| NCT00379821 | PHASE3 | COMPLETED | Chloroquine Alone or in Combination for Malaria in Children in Malawi |
| NCT00422084 | PHASE3 | COMPLETED | Pyronaridine Artesunate (3:1) Versus Coartem® in P Falciparum Malaria Patients |
| NCT00440999 | PHASE3 | COMPLETED | Pyronaridine Artesunate (3:1) in Children and Adults With Acute Plasmodium Vivax Malaria |
| NCT00541385 | PHASE3 | COMPLETED | Pyronaridine Artesunate 3:1 Granule Formulation vs. Coartem© Crushed Tablets in P. Falciparum Malaria Pediatric Patients |
| NCT00694694 | PHASE3 | COMPLETED | Azithromycin + Artesunate v Artemether-lumefantrine in Uncomplicated Malaria. |
| NCT00936767 | PHASE2/PHASE3 | WITHDRAWN | Artemisone for the Treatment of Uncomplicated Falciparum Malaria in Western Cambodia |
| NCT01074905 | PHASE3 | COMPLETED | Study on the Treatment of Vivax Malaria |
| NCT01082718 | PHASE2/PHASE3 | WITHDRAWN | Pharmacokinetics of Mefloquine-Artesunate in Pregnant Women With Uncomplicated Plasmodium Falciparum Infection |
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).