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artemisinin + amodiaquin (ASAQ / Winthrop / Coarsucam)

✓ Approved

DNDi · Small Molecule · Small Molecule

What is artemisinin + amodiaquin?

artemisinin + amodiaquin is a small molecule developed by DNDi. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesASAQ, Winthrop, Coarsucam
CompanyDNDi
Drug ClassSmall Molecule
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, DNDi

Therapeutic Indications

artemisinin + amodiaquin is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Infections and infestationsPlasmodium malariae infection✓ Approved

Related Research Articles

PubMedExpert opinion on therapeutic targets2026-08-29

Exploiting ER proteostasis in malaria: protein disulphide isomerases as selective antimalarial targets.

Odugbemi Adeshina I AI, Mthembu Wendy W, Zininga Tawanda T

The emergence of partial resistance to artemisinin-based therapies has intensified the search for antimalarial targets beyond classical kinases and proteases. Protein disulfide isomerases (PDIs) have emerged as attractive candidates due to their roles in endoplasmic reticulum (ER) oxidative folding, redox homeostasis, and survival under proteotoxic stress. Several Plasmodium falciparum PDI family members are essential during asexual blood stages and contribute to parasite transmission. We summarize PfPDI architecture, catalytic and holdase functions, and their integration within the parasite ER folding network, highlighting structural divergence from human PDIs that may enable selective inhibition. We review PDI-directed chemotypes, including covalent active-site binders and non-covalent/allosteric modulators, and highlight the absence of PfPDI-selective probes with validated intracellular mechanisms. We further discuss approaches for target validation, including chemoproteomics, activity-based profiling, and chemical genetics, alongside medicinal chemistry considerations for achieving exposure to an intracellular ER target. Finally, we examine PfPDIs within a proteostasis-stress framework and discuss combination strategies with protein-damaging agents such as artemisinin derivatives. Progress will depend on structure-guided targeting of divergent non-catalytic surfaces, optimization of intracellular and ER exposure, and rigorous in-parasite target-engagement studies. PfPDI inhibitors are most likely to succeed as components of resistance-robust combination therapies.

PMID 42667181
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PubMedFrontiers in immunology2026-08-28

Artemisinin ameliorates rheumatoid arthritis through modulation of the IL-17/PI3K/AKT signaling pathway: integrated network pharmacology, bioinformatics, and experimental validation.

Zhou Zongyuan Z, Wang Le L, Li Yongzuo Y, Yang Yue Y et al.

Artemisinin regulates the immune system and is applied in RA treatment. Nevertheless, the effectiveness and potential mechanisms of artemisinin in the treatment of RA remain unclear, especially in fibroblast-like synoviocytes (FLSs). This study aimed to investigate the mechanism of artemisinin in the treatment of rheumatoid arthritis (RA) through an integrated network pharmacology and bioinformatics approach, supported by experimental validation both in MH7A cells and collagen-induced arthritis (CIA) mice. SwissTargetPrediction database, TCMSP, TargetNet, SuperPred, and PharmMapper were used to identify the targets of artemisinin. RA-related differentially expressed genes (DEGs) were collected by integrating three GEO datasets. DEGs related to artemisinin were utilized to create protein-protein interaction networks and visualize them with STRING and Cytoscape. GO and KEGG functional enrichment analyses were executed. Molecular docking and molecular dynamics (MD) simulations were carried out to analyze core targets using the AutoDock Vina and Desmond software. Furthermore, CIA mouse and MH7A cells were used to validate the results obtained from network pharmacology. There were 73 target genes intersecting between the artemisinin targets and the DEGs. PPI network analysis and its topology indicated that AR, EGFR, JAK2, and PTGS2 had the greatest centrality. GO and KEGG enrichment analyses suggested that the candidate targets were significantly associated with the PI3K/AKT signaling pathway. Molecular docking and an in vivo study were used for further investigation. Artemisinin interacted with the cavities of AR, JAK2, EGFR, and PTGS2 with binding energies of -8.65, -8.61, -7.48, and -8.48 kcal/mol, respectively. MD simulations showed that the AR-artemisinin complex maintained persistent interactions and stable energy profiles over 20 ns. The CIA model and MH7A cell studies confirmed that artemisinin exposure inhibited the proliferation and production of IL-1β, IL-6, and IL-8 triggered by IL-17. Furthermore, artemisinin attenuated IL-17-induced AKT phosphorylation levels. These findings suggest that artemisinin may ameliorate RA partly by suppressing IL-17-induced inflammatory activation and PI3K/AKT signaling. AR, EGFR, JAK2, and PTGS2 were prioritized as candidate hub targets.

PMID 42661803
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PubMedThe Pan African medical journal2026-08-28

[Impact of introducing a fifth monthly cycle of seasonal malaria chemoprevention among children aged 3 to 59 months: a quasi-experimental difference-in-differences study in the Zinder Region, Niger].

Wazodan Almoustapha Mahamane AM, Lamine Mahaman Moustapha MM, Alkassoum Ibrahim I, Doutchi Mahamadou M et al.

The addition of a fifth monthly cycle to seasonal malaria chemoprevention (SMC) has been proposed to extend protection during prolonged transmission seasons in the Sahel. This study evaluated the effect of introducing a fifth SMC cycle on malaria incidence and on the utilization of malaria diagnostic and treatment services in the Takieta health district, Niger. We conducted a quasi-experimental, non-randomized, before-and-after study with a comparison group ("here-elsewhere" design), using routine health data from 19 integrated health centers across two health districts between 2020 and 2023. Nine health centers implemented five monthly SMC cycles (SMC5), while ten continued the standard four-cycle strategy. Data were extracted from the national health information system. A fixed-effects difference-in-differences (DiD) model was applied to estimate the impact of the fifth SMC cycle on malaria incidence, rapid diagnostic test (RDT) utilization, RDT positivity rates, and artemisinin-based combination therapy (ACT) consumption. The introduction of a fifth SMC cycle was associated with a significant reduction in malaria incidence, corresponding to a decrease of 2.44 cases per 1,000 population during the intervention period. This reduction was accompanied by a 2.99% improvement in health service performance and a significant decline in RDT positivity rates (p = 0.003). However, the difference-in-differences coefficients for RDT use (158.59) and ACT use (153.05) were not statistically significant, indicating that SMC5 had no measurable impact on reducing the use of diagnostic tests or antimalarial treatments. The addition of a fifth monthly cycle of seasonal malaria chemoprevention was associated with a reduction in malaria incidence in the study districts during the intervention period. However, no corresponding reduction in RDT or ACT consumption was observed. These findings suggest that extending SMC coverage by one additional month may reduce malaria burden without significantly altering the use of diagnostic or treatment services in health facilities.

PMID 42662648
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PubMedMolecules (Basel, Switzerland)2026-08-27

Artemisia annua and A. afra Teas, Artemisinin, and Dihydroartemisinin Differentially Regulate ROS and Fibrosis-Associated Phenotypes in Human Dermal Fibroblasts.

Isife Samuel S, Bush Trevor T, Medasani Isha I, Towler Melissa M et al.

Fibrosis is driven by persistent fibroblast activation, oxidative stress, myofibroblast differentiation, and extracellular matrix remodeling, yet available antifibrotic therapies remain limited. This study evaluated whether artemisinin (ART), dihydroartemisinin (DHA), and traditional tea infusions of Artemisia annua and A. afra differentially regulate fibrosis-associated responses in human dermal fibroblasts. Neonatal and adult human dermal fibroblasts were cultured under pre-fibrotic or TGF-β/ascorbic acid-stimulated pro-fibrotic conditions and assessed for intracellular ROS, scratch-wound closure, collagen gel contraction, fibrosis-associated gene expression, and α-SMA protein abundance. Artemisia teas produced greater ROS reduction than purified ART or DHA, with A. afra showing the strongest antioxidant effect despite lacking detectable artemisinin. DHA and A. annua most consistently suppressed scratch closure, while A. afra produced intermediate inhibition and ART was comparable to vehicle control. Collagen gel contraction was most strongly reduced by A. annua, with DHA and A. afra producing intermediate suppression. Under pro-fibrotic conditions, DHA and A. annua downregulated ACTA2, A. annua suppressed COL1A1, and DHA and A. annua increased matrix-remodeling MMP expression. Reduced levels of α-SMA confirmed the antifibrotic effects. These findings indicate that antifibrotic activity differs among artemisinin-related compounds and whole-plant Artemisia preparations, with DHA and A. annua showing the strongest overall activity.

PMID 42653828
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PubMedGenes2026-08-27

Breaking the Growth-Defense Trade-Off: bHLH Transcription Factors as Integrators of Development, Metabolism, and Yield in Artemisia annua.

Yuan Mingyuan M, Zhou Fei F

Artemisinin, a sesquiterpene lactone produced by Artemisia annua, is synthesized and stored predominantly in glandular secretory trichomes (GSTs). Despite substantial advances in elucidating its biosynthetic pathway and transcriptional regulation, a key challenge remains: how developmental processes, hormone signaling, and metabolic pathways are coordinately integrated to overcome the trade-off between trichome density, metabolic flux, and vegetative biomass, which ultimately limits whole-plant yield. Recent studies have identified basic helix-loop-helix (bHLH) transcription factors (TFs) as central integrative hubs in this network. AabHLH113 functions as a convergence node linking jasmonic acid (JA) and abscisic acid (ABA) signaling to activate core biosynthetic genes. AaMYC3 bridges development and metabolism by promoting GST initiation via AaHD1 while enhancing pathway flux and cooperating with other bHLH factors to amplify amorpha-4,11-diene synthase (ADS) and artemisinic aldehyde delta-11(13) reductase (DBR2) expression. Extending this regulation to the whole-plant level, AaSPATULA coordinates GST formation with photosynthetic capacity, carbon assimilation, and biomass accumulation. Here, we propose a unified framework in which bHLH TFs integrate hormone signaling, trichome development, metabolic flux, and carbon allocation into a coherent regulatory system. We further discuss implications for next-generation metabolic engineering and highlight future directions, including multi-omics-guided, multi-target editing of regulatory hubs. This developmental-metabolic integration framework provides a conceptual basis for optimizing artemisinin production and improving high-value metabolite biosynthesis in other trichome-bearing plants.

PMID 42650076
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PubMedAdvances in pharmacological and pharmaceutical sciences2026-08-27

Annona muricata Polyphenols Induce Cytoskeletal Alterations and Predicted Aldose Reductase Binding in Giardia lamblia.

Govea-Flores Diana Valeria DV, Garza-Ontiveros Mariana M, Gutiérrez-Gutiérrez Filiberto F, Gómez-Ibarra Ana Gabriela AG et al.

Giardiasis has been classified as a neglected disease by the World Health Organization since 2004. Despite ongoing efforts, challenges such as drug resistance and treatment failures continue to hinder effective management. In recent years, the exploration of plant-derived compounds as antiparasitic agents has emerged as a promising strategy. This is supported by the discovery of plant-derived compounds such as quinine and artemisinin in antiparasitic pharmacology. The identification of specific molecular targets in Giardia lamblia, a protozoan with unique cytoskeletal and metabolic features, has further advanced drug discovery efforts. In this study, we evaluated the in vitro and in silico effects of a polyphenol-enriched extract from Annona muricata (soursop) leaves against G. lamblia trophozoites. The extract had a noticeable impact on parasite growth, cell adhesion, and morphology. Ultrastructural analyses revealed elongation, flagellar abnormalities, and damage to the ventral disk. Western blot and immunofluorescence assays demonstrated reduced α-tubulin expression and altered localization, indicating cytoskeletal alterations in treated trophozoites. Molecular docking analyses predicted favorable interactions between soursop polyphenols and Giardia aldose reductase, particularly involving the catalytic residues Y40 and K71. Collectively, these findings suggest that A. muricata polyphenols exert antigiardial effects through multiple cellular alterations and support the hypothesis that metabolic and cytoskeletal processes may both contribute to the observed biological effects. Further studies are required to experimentally validate the role of aldose reductase and its relationship with cytoskeletal disruption.

PMID 42656692
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