Amodiaquine
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Also known as AmodiaquinAmodiaquinaAmodiaquinumGNF-Pf-5648NSC-13453SJ000110703Sunoquine
Summary
Amodiaquine (CHEMBL682) is an approved small-molecule non-steroidal anti-inflammatory drug (ATC P01BA06); indicated across 6 conditions including malaria and plasmodium falciparum malaria.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: P01BA06
- Indications: 6 conditions
- Clinical trials: 41
- Chemistry: 355.9 Da · C20H22ClN3O
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL682 |
| Name | Amodiaquine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 2165 |
| ChEBI | CHEBI:2674 |
| ATC | P01BA06 |
| Molecular formula | C20H22ClN3O |
| Molecular weight | 355.9 |
| InChIKey | OVCDSSHSILBFBN-UHFFFAOYSA-N |
SMILES: CCN(CC)CC1=C(C=CC(=C1)NC2=C3C=CC(=CC3=NC=C2)Cl)O
IUPAC name: 4-[(7-chloroquinolin-4-yl)amino]-2-(diethylaminomethyl)phenol
ChEBI definition: A quinoline having a chloro group at the 7-position and an aryl amino group at the 4-position.
Pharmacological roles (ChEBI): antimalarial, non-steroidal anti-inflammatory drug, drug allergen, prodrug, EC 2.1.1.8 (histamine N-methyltransferase) inhibitor, anticoronaviral agent.
Also known as: Amodiaquin, Amodiaquina, Amodiaquine, Amodiaquinum, GNF-Pf-5648, NSC-13453, SJ000110703, Sunoquine, AMODIAQUINE, amodiaquine
Parent form; salt/anhydrous children: CHEMBL1630, CHEMBL1357648, CHEMBL1707005, CHEMBL3137745, CHEMBL3216010
Patent coverage: 1,992 distinct patent families (7,153 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 7,108 (99%) of the total. 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: 18 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2C adrenergic receptor, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 1A, Muscarinic acetylcholine receptor M1, D(2) dopamine receptor, Sodium-dependent noradrenaline transporter, Prostaglandin G/H synthase 2, Mu-type opioid receptor, Sodium-dependent dopamine transporter.
Bioactivity
ChEMBL activities: 11 potent at pChembl ≥ 5 of 23 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| CYP2D6 | 6.19 | IC50 | 640 | nM | CHEMBL_ACT_15450972 |
| KCNH2 | 6.19 | AC50 | 650 | nM | CHEMBL_ACT_25117900 |
| CYP2J2 | 6 | IC50 | 990 | nM | CHEMBL_ACT_15461599 |
| HTR2B | 5.82 | AC50 | 1500 | nM | CHEMBL_ACT_25227545 |
| APP | 5.4 | IC50 | 4000 | nM | CHEMBL_ACT_18580012 |
| ADRA2C | 5.32 | AC50 | 4800 | nM | CHEMBL_ACT_25147899 |
| APP | 5.27 | IC50 | 5400 | nM | CHEMBL_ACT_18580039 |
| PTGS2 | 5.18 | AC50 | 6600 | nM | CHEMBL_ACT_25166217 |
| SLC6A2 | 5.1 | AC50 | 7900 | nM | CHEMBL_ACT_25145025 |
| DRD2 | 5.05 | AC50 | 8900 | nM | CHEMBL_ACT_25140357 |
| HRH3 | 5.01 | AC50 | 9800 | nM | CHEMBL_ACT_25200615 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
6 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 |
| severe acute respiratory syndrome | 2 | MONDO:0005091 | MONDO:0100096 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 41.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 14 |
| PHASE4 | 9 |
| PHASE2 | 6 |
| Not specified | 5 |
| PHASE1 | 3 |
| PHASE2/PHASE3 | 2 |
| PHASE1/PHASE2 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT07322068 | PHASE4 | NOT_YET_RECRUITING | Perennial Malaria Chemoprevention in the Malaria Vaccine Era |
| NCT00137514 | PHASE4 | COMPLETED | Chloroquine and Amodiaquine for Treatment of Malaria in Children |
| NCT00445796 | PHASE4 | COMPLETED | Arsucam® (Artesunate + Amiodaquine) Efficacy and TOLerance |
| NCT00465257 | PHASE4 | SUSPENDED | Efficacy of Artesunate + Amodiaquine Four Years After Its Introduction in Zanzibar |
| NCT01023399 | PHASE4 | COMPLETED | Artesunate Plus Amodiaquine in Malaria in Cote d’Ivoire |
| NCT03431714 | PHASE4 | COMPLETED | Efficacy and Safety of ASAQ and PD for the Treatment of Uncomplicated Falciparum Malaria in Mainland Tanzania |
| NCT03768908 | PHASE4 | COMPLETED | Efficacy of Artesunate + Amodiaquine Versus Artemether-lumefantrine for Falciparum Malaria in Zanzibar, 2005 |
| NCT05323721 | PHASE4 | UNKNOWN | Effectiveness and Chemoprevention Efficacy of Implementing Seasonal Malaria Chemoprevention in Karamoja Region, Uganda |
| NCT05478954 | PHASE4 | UNKNOWN | Chemoprevention Efficacy Study in Burkina Faso |
| NCT00123552 | PHASE3 | COMPLETED | Longitudinal Antimalarial Combinations in Uganda |
| NCT00131703 | PHASE3 | COMPLETED | Efficacy and Safety of Sulphadoxine-pyrimethamine and Amodiaquine in Ghanaian Pregnant Women |
| NCT00132548 | PHASE3 | COMPLETED | A Trial of Four Drug Regimens for the Prevention of Malaria in Senegalese Children |
| NCT00146783 | PHASE2/PHASE3 | COMPLETED | Navrongo Drug Options for IPT in Pregnancy Trial |
| NCT00158548 | PHASE3 | COMPLETED | ACT With Chloroquine, Amodiaquine & Sulphadoxine-pyrimethamine in Pakistan |
| NCT00316329 | PHASE3 | COMPLETED | ATAQ EASY: Artesunate + Amodiaquine Fixed Dose Combination in the Treatment of Uncomplicated Plasmodium Falciparum Malaria |
| NCT00561899 | PHASE2/PHASE3 | COMPLETED | Comparison of Three Drug Combinations for Intermittent Treatment of Malaria in Children |
| NCT00852371 | PHASE3 | COMPLETED | Intermittent Preventive Treatment of Malaria in Schoolchildren |
| 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 |
| NCT01378286 | PHASE3 | COMPLETED | Efficacy and Tolerability of Artesunate Amodiaquine Versus Chloroquine in the Treatment of Uncomplicated Plasmodium Vivax Malaria |
| NCT02211729 | PHASE3 | COMPLETED | A Trial of Seasonal Malaria Chemoprevention Plus Azithromycin in African Children |
| NCT03939104 | PHASE3 | COMPLETED | A Trial to Compare the Efficacy, Safety and Tolerability of Combinations of 3 Anti-malarial Drugs Against Combinations of 2 Anti-malarial Drugs (Asia) |
| NCT04149106 | PHASE3 | UNKNOWN | Seasonal Malaria Chemoprevention With Dihydroartemisin Piperaquin vs. Sulfadoxine-pyrimethamin+Amodiaquin |
| NCT05471544 | PHASE3 | UNKNOWN | Effectiveness, Feasibility and Acceptability of Seasonal Malaria Chemoprevention in Aweil South County in South Sudan |
| NCT05946642 | PHASE3 | UNKNOWN | Innovative Intermittent Preventive Treatment Approaches to Reduce Malaria Burden in School-age Children in Burkina Faso |
| NCT00261222 | PHASE2 | COMPLETED | Efficacy of Amodiaquine in the Treatment of Uncomplicated Falciparum Malaria in Young Children of Burkina Faso |
| NCT00323622 | PHASE2 | COMPLETED | Long-Term Follow-up of Children for a 2-Year Period to Confirm the Safety and Immunogenicity of GSK 257049 Vaccine |
| NCT00354380 | PHASE2 | COMPLETED | Safety and Efficacy of Methylene Blue Combined With Artesunate or Amodiaquine for Malaria Treatment in Children of Burkina Faso: a Pilot Study |
| NCT00563914 | PHASE1/PHASE2 | COMPLETED | A Comparative Safety and Activity Study With Ferroquine Associated With Artesunate Versus Amodiaquine Associated With Artesunate in African Adult Patients With Uncomplicated Malaria |
| NCT01955382 | PHASE2 | COMPLETED | Evaluation of Oral Activated Charcoal on Antimalarial Drug’s Ability to Kill Parasites in Malian Children With Malaria |
| NCT02696954 | PHASE1/PHASE2 | TERMINATED | Study of Artemether-lumefantrine, Amodiaquine and Primaquine in Healthy Subjects |
| NCT02831023 | PHASE2 | COMPLETED | Phase 2 Efficacy Study of Primaquine and Methylene Blue |
| NCT05550909 | PHASE2 | COMPLETED | Gametocytocidal and Transmission-blocking Efficacy of ASAQ and ALAQ With or Without PQ in Mali |
| NCT00386503 | PHASE1 | COMPLETED | Bioavailability of the Fixed Combination of Amodiaquine and Artesunate Under Fed & Fasted Conditions |
| NCT00894660 | PHASE1 | COMPLETED | A Bioequivalence Study Comparing Amodiaquine Tablet (Pfizer) To Amodiaquine Tablets (Arsuamoon-Guilin China) In Healthy Subjects |
| NCT04080895 | PHASE1 | TERMINATED | Pharmacokinetic Study of Artemether-lumefantrine and Amodiaquine in Healthy Subjects |
| NCT00127998 | Not specified | COMPLETED | Antimalarial Drug Resistance in Mali |
| NCT00285662 | Not specified | COMPLETED | Intermittent Preventive Treatment (IPTi) for the Prevention of Malaria and Anaemia in PNG Infants |
| NCT00356824 | Not specified | COMPLETED | Relationship Between HIV and Malaria in Ugandan Children |
| NCT05354258 | Not specified | UNKNOWN | Feasibility and Safety of Combining Anti-malarial With Deworming Drugs in African Children |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 3 clinical and 6 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).