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artemisinin + amodiaquin (ASAQ / Winthrop / Coarsucam)

✓ Approved

DNDi · 小分子 · 小分子

什么是 artemisinin + amodiaquin？

artemisinin + amodiaquin 是一种小分子，由DNDi研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名ASAQ, Winthrop, Coarsucam
公司DNDi
药物类别小分子
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, DNDi

治疗适应症

artemisinin + amodiaquin 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Infections and infestationsPlasmodium malariae infection✓ Approved

相关研究文献

PubMedApoptosis : an international journal on programmed cell death2026-07-27

Artemisinin liposomes regulates breast cancer metastasis and apoptosis through TIGIT/CD155 signal axis.

Feng Yachan Y, Han Zexu Z, Shao Jiangtao J, Caliskan Bilgen B et al.

To investigate the mechanism of artemisinin liposomes regulating breast cancer metastasis and apoptosis through TIGIT/CD155 signal axis. Artemisinin liposomes were synthesized by thin film dispersion method and characterized in morphology, zeta potential, hydrodynamic size, entrapment efficiency as well as thermal stability. Furthermore, the cytotoxic effects of artemisinin liposomes on HC11 and 4T1 cell was evaluated by the MTS test. Scratch, transwell and colony formation experiment were conducted to assess the effect of artemisinin liposomes on cell metastasis. Apoptosis, cell cycle arrest were measured using flowcytometry. Meanwhile, bioinformatics analysis was used to investigate the relationship between TIGIT as a drug target for breast cancer and artemisinin liposomes, TIGIT/CD155 signal axis. Additionally, the mouse tumor model(group(saline, artemisinin, liposomes, artemisinin liposomes), dose(100 mg/kg/d)) was employed to detect the tumor-suppressive efficacy. Finally, the expression levels of Src, Akt, Mtor and Stat3 was further explored by Western Blot and RT-PCR to elucidate the regulatory mechanism of artemisinin liposomes on the TIGIT/CD155 signaling axis. The liposomes and artemisinin liposomes had average sizes of approximately 80 nm and 130 nm respectively, with a polydispersity index (PDI) of 0.225, 0.287. Artemisinin was effectively encapsulated within liposomes, as shown by the high encapsulation efficiency of 90.11% ± 0.88, with a cumulative release rate of 32.8% at pH = 5.5. In vitro studies demonstrated that artemisinin liposomes possessed significantly greater cytotoxicity against 4T1 cells, the IC50 values were approximately 480 µM. In contrast to artemisinin alone, artemisinin liposomes can effectively inhibit 4T1 cell metastasis, with an inhibition rate of 93.02% at 20 µM, and also promote cell apoptosis, with an apoptosis rate of 14.17% at 20 µM. Bioinformatic analysis demonstrated that TIGIT/CD155 signal axis was highly expressed in breast cancer and had poor prognosis. In vivo results revealed that artemisinin liposomes alone produced an anti-tumor effect comparable to the combination of TIGIT/CD155 and IL-15. Ultimately, artemisinin liposomes can regulate breast cancer progression by modulating the TIGIT/CD155 signaling axis and critical factors in the SRC pathway, specifically SRC, AKT, STAT3, and mTOR. The clinical treatment of breast cancer does not rely on the use of chemotherapy drugs alone, but selects the effective ingredients of Chinese medicine with higher safety.

PMID 42507162
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PubMedJournal of functional biomaterials2026-07-27

Enhanced Antibacterial Activity of Artemisia absinthium Extract Containing Artemisinin and Polyphenols Loaded into Mesoporous Silica Calcium- and Cerium-Doped Nanoparticles.

Tsamesidis Ioannis I, Pouroutzidou Georgia K GK, Christodoulou Athanasios A, Gkiliopoulos Dimitrios D et al.

Artemisia absinthium (A. absinthium) is a perennial plant valued for its antibacterial, antioxidant, and anti-inflammatory properties, exhibiting broader therapeutic potential. Given the need to deliver low doses of A. absinthium extract, mesoporous silica nanoparticles have attracted considerable attention as promising nanocarriers due to their distinctive physical and chemical properties. Physicochemical characterization of the materials was performed and biological assays were conducted to investigate the ROS, antibacterial and antioxidant activity of A. absinthium extract encapsulated within cerium- and calcium-doped mesoporous silica nanoparticles (MNSiCaCe) against both aerobic and anaerobic bacteria. FTIR, SEM, and BET analysis confirmed successful synthesis of the MNSiCaCe. Phytochemical profiling of Artemisia absinthium extract using HPLC revealed the presence of artemisinin and a rich composition of phenolic and flavonoid constituents, with a total phenolic content of 182 ± 3.6 mg GAE/100 g dry plant material and a total flavonoid content of 42.5 ± 0.6 mg QE/100 g. Quantitative drug loading profiling demonstrated that while plain MNSi nanocarriers achieved a loading capacity of 16.96%, the MNSiCaCe enhanced this threshold to 43.11%. The in vitro controlled-release kinetics exhibited a highly prolonged and slow-release profile of the MNSiCaCe. The materials demonstrated excellent hemocompatibility and high mitochondrial activity with human periodontal ligament cells (hPDLCs). Elevated ROS generation was observed under conditions where antibacterial activity was most pronounced. While the artemisinin-doped nanoparticles showed notable antibacterial effects, the complete Artemisia absinthium-loaded nanoparticles achieved a significantly greater reduction in bacterial viability probably due to the synergistic interaction between artemisinin and the extract's rich polyphenol profile. These findings highlight MNSiCaCe as a promising and safe nanocarrier system for drug delivery, with strong antibacterial potential, offering valuable applications in antibacterial therapies.

PMID 42506552
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PubMedTropical medicine and infectious disease2026-07-27

Malaria Epidemiology and Plasmodium Species-Specific Antimalarial Treatment Patterns Among RDT-Confirmed Cases in Northwestern Pakistan.

Mansoor Aqsa A, Narjis Ghulam G, Abdelmalek Imen Ben IB, Firasat Sabika S et al.

Malaria remains a major public health challenge in Pakistan, where persistent transmission, heterogeneous risk patterns, and evolving treatment practices continue to impede control and elimination efforts. A community-based cross-sectional study was conducted among 9211 symptomatic individuals in District Dera Ismail Khan, northwestern Pakistan, from January 2024 to December 2025. Malaria was diagnosed using rapid immunochromatographic assays for Plasmodium vivax (P. vivax) and Plasmodium falciparum (P. falciparum), and associated risk factors were assessed using multivariable logistic regression. Overall malaria prevalence was 36.27% (3341/9211). P. vivax predominated, accounting for 93.8% (3133/3341) of infections, while P. falciparum represented 5.8% (195/3341) and mixed infections 0.4% (13/3341). Infection risk was significantly associated based on multivariate analysis with male sex, younger age, pregnancy (AOR = 4.69), and absence of mosquito net use (AOR = 6.17), whereas indoor residual spraying (AOR = 0.08) showed a strong protective effect. Malaria transmission showed two peaks: October-December (AOR = 3.78-4.97) and February-March (AOR = 2.25-2.31) and declined significantly based on unadjusted analysis from 39.5% in 2024 to 32.8% in 2025 (OR = 0.74; p < 0.001). Blood groups B+ (AOR = 0.77), B- (AOR = 0.78), and AB- (AOR = 0.86) were significantly associated with reduced odds of malaria infection. A notable shift toward artemisinin-based combination therapy was observed, with artemether-lumefantrine largely replacing chloroquine for malaria treatment. The persistence of P. vivax-dominated transmission alongside ongoing P. falciparum circulation highlights the need for targeted vector control, enhanced surveillance, and evidence-based treatment strategies to accelerate malaria elimination in Pakistan.

PMID 42506764
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PubMedDose-response : a publication of International Hormesis Society2026-07-25

Mechanistic Insights Into Dose-Dependent Alleviation of Colorectal Cancer Through Artemisinin-Loaded Mesoporous Silica Nanoparticles in 1,2-Dimethylhydrazine-Induced Albino Wistar Rats.

Zahid Fatima F, Ilyas Umair U, Zahid Sara S, Gulzar Faisal F et al.

The current study investigates the suitability of encapsulating the Artemisinin-plant-originated lipophilic drug molecule into polyethylene glycol-coated mesoporous silica nanoparticles in a suitable dose regimen for the specific targeting of the drug in colorectal cancer. Mesoporous silica nanoparticles (MSNPs) were synthesized through the sol-gel method, and Artemisinin was loaded. Then characterization of Artemisinin-loaded mesoporous silica nanoparticles coated with polyethylene glycol (MSN-PEG@Artemisinin) was performed by Fourier transform infrared spectroscopy (FTIR), Zeta analysis, Polydispersity index (PDI) and X-Ray diffraction (XRD) techniques and compared with the standard drug Gemcitabine. The in vivo analysis of 1,2-dimethylhydrazine (DMH) was used to induce colorectal tumors in the colon of inbred male Wistar rats. The treatment group of rats was administered MSN-PEG@Artemisinin through intraperitoneal injection. Hematoxylin and eosin staining were performed to the histopathological examination of tumors. The average size of MSN-PEG@Artemisinin was 203.6 ± 64.78 nm with a zeta potential of -10.9mV. PDI was measured at 0.106. FTIR analysis also supported the successful loading of Artemisinin in mesoporous silica nanoparticles with PEG coating without showing interactions. The encapsulation efficiency (EE) and Drug loading (DL) percentages were 82.75% and 33.10%, respectively. XRD indicated a uniform mesoporous structure with a proper hexagonal symmetry. The in-vitro release was carried out in phosphate buffer with 7.4 pH following biphasic system with 26% drug release during the first 2.5 hours and 57% in 24 hours, indicating a good controlled release rate. In-vivo study revealed DMH-induced colorectal rats showed the increased tumor weight (34.8±0.75mg) tumor length (8.2±0.6) and tumor width (6.0±0.5) at a dose level of 0.5 ml/kg. Artemisinin loaded MSNPs significantly (p < .005) suppressed tumor weight (15.6±1.56), tumor length (5.7±0.23) and tumor width (2.3±0.8) at a dose level of 100 mg/kg body weight. Overexpression of 8-OHdG, MMP-7, CA-19-9, KRAS, IL-8, Caspase-8, PD-1 and PDL-1 in CRC, which were successfully treated with MSN-PEG@Artemisinin and standard Gemicitabine ((p≥0.056). MSNPs-PEG@Artemisinin suppressed DMH-induced colorectal carcinogenesis by targeting oxidative stress, KRAS/MMP-7/IL-8 inflammatory signaling, PD-1/PD-L1-mediated immune evasion, and Caspase-8-associated apoptotic dysregulation. These results highlight the potential of modified MSNPs as a versatile drug delivery system for colorectal cancer, providing a viable approach to enhance the therapeutic window of Artemisinin by controlling the dose while reducing the adverse effects of cancer therapies. This research contributes to advancements in pre-clinical studies and to improvements in targeted colorectal cancer therapies by providing insights into the development and use of mesoporous silica nanoparticles as a promising drug delivery system.

PMID 42500304
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PubMedFree radical biology & medicine2026-07-25

Physiologically relevant oxygen tensions reshape anticancer responses under oxidative stress-permissive culture conditions.

Mielczarek-Puta Magdalena M, Otto-Ślusarczyk Dagmara D, Żyżyńska-Granica Barbara B, Graboń Wojciech W et al.

Tumor hypoxia is a hallmark of solid malignancies and an important determinant of therapeutic response; however, most in vitro studies are still performed under atmospheric oxygen conditions that poorly reflect physiological tissue oxygenation. Conventional culture systems also rarely account for iron availability and polyunsaturated fatty acids (PUFAs), two important modulators of oxidative stress-associated cytotoxicity. This study investigated how physiologically relevant oxygen tension influences anticancer responses to oxidative stress-modulating compounds under iron- and PUFA-enriched conditions. Human colorectal, lung, and pancreatic cancer cell lines, together with non-tumorigenic HaCaT cells, were cultured under physioxic (10% O2) and hypoxic (1% O2) conditions in the presence of transferrin-bound iron and linoleic acid and exposed to artemisinin (ART), dihydroartemisinin (DHA), honokiol (HNK), and doxycycline (DOXY). The anticancer responses were strongly oxygen- and cell line-dependent. DHA exerted the strongest antiproliferative activity, inducing marked G0/G1 arrest and pronounced apoptosis, particularly under hypoxia. ART and HNK also displayed oxygen-dependent apoptotic and oxidative stress-associated effects, whereas DOXY primarily induced caspase activation accompanied by comparatively weak apoptosis. All compounds increased mitochondrial reactive oxygen species generation, while DHA and ART most consistently enhanced lipid peroxidation. In contrast, GPX4 protein expression remained largely unchanged in most cell lines, suggesting functional rather than expression-level modulation of ferroptosis-associated pathways. Collectively, these findings demonstrate that physiologically relevant oxygen tension profoundly reshapes anticancer responses to redox-active compounds and highlight the importance of incorporating physiologically relevant oxygen conditions into experimental cancer models.

PMID 42497949
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PubMedMedical oncology (Northwood, London, England)2026-07-24

A combination of artemisinin, moxidectin, and doxorubicin drugs can selectively and efficiently induce apoptosis in acute lymphoblastic and chronic myeloid leukemia cells in vitro and ex vivo.

Soto-Mercado Viviana V, Mendivil-Perez Miguel M, Jimenez-Del-Rio Marlene M, Velez-Pardo Carlos C

Acute lymphoblastic (ALL) and chronic myeloid (CML) leukemias are blood cancers that often resist traditional chemotherapy and other treatments. This is likely due to their ability to evade apoptosis. Therefore, inducing apoptosis in leukemia cells using innovative drug combinations may be the most effective therapeutic approach. Methods for multidrug combinations involving three or more drugs are scarce and much more complex to analyze. To address this issue, we propose an effective concentration 50 (EC50)-based, three-step method. The first step determines the lowest EC50 for each drug (e.g., artemisinin, chloroquine, primaquine, mefloquine, ivermectin, moxidectin, doxorubicin, and minocycline) by analyzing four cell endpoints (e.g., cell cycle, sub-G1, mitochondrial membrane potential (ΔΨm), autophagy (lysosomes), and cleaved caspase 3 (CC3)) on K562 cells. Step two involves establishing the deleterious effect of the EC50-based drug combination at concentrations of single drugs at 1-, ½-, and ¼-EC50, respectively, on K562 leukemia cells. Step three involves using the optimal combined drugs to evaluate the same cellular endpoints in other non-leukemic and leukemic cells. We found that the combination of AM (1 µM), MD (10 µM), and DR (1.5 µM), i.e., at ½ EC50, induced cell cycle arrest in the S (25% ± 13, N = 4) and G2/M (55% ± 18, N = 4) phases, a drastic loss of ΔΨm (81% ± 6, N = 4), high lysosome accumulation (82% ± 10, N = 4), and CC3 (83% ± 13, N = 4), as evidence of apoptosis in K562 and Jurkat cells and ex vivo ALL and CML cells. The combined drugs were innocuous to peripheral blood lymphocytes (PBLs) (S phase = 40%; G2/M = 26%; ΔΨm = 4%; lysosomes = 3%; CC3 = 4%; n = 3). Our approach to combining drugs has the potential to provide a new pharmacological treatment for leukemias.

PMID 42496777
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