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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

PubMedJournal of controlled release : official journal of the Controlled Release Society2026-08-04

Self-exploding tumor microenvironment-responsive nanomedicine as "ROS Bomb" ignites STING pathway for triple-negative breast cancer immunotherapy.

Lu Keqiang K, Su Yaoquan Y, Zhou Xingchen X, Zhang Fang F et al.

Conventional reactive oxygen species (ROS)-mediated tumor therapies such as photo-, sono-, and chemodynamic therapies are often limited by inadequate penetration depth of external stimuli and insufficient endogenous ROS substrates (e.g., O₂ and H₂O₂). Here, we report that horseradish peroxidase (HRP) can catalyze artemisinin to generate ROS. Based on this, a "ROS bomb" nanomedicine was designed for antitumor immunotherapy. The nanocarrier consists of silica cross-linked micelles incorporating ROS-cleavable thioketal bonds and encapsulated artemisinin as the payload, with surface-immobilized HRP serving as the trigger. Within the tumor microenvironment with elevated H₂O₂, the thioketal linkers are cleaved to release artemisinin, initiating an HRP-catalyzed ROS cascade. The ROS burst induces immunogenic cell death and activates the STING pathway in dendritic cells assisted by the co-released drug SN38, effectively suppressing the growth of immunosuppressive triple-negative breast tumors. This exogenous ROS delivery strategy overcomes the restrictions of conventional ROS therapies, offering a potent approach for treating deep-seated tumors.

PMID 42546818
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PubMedMolecular and biochemical parasitology2026-08-04

Why not now? Targeting Plasmodium falciparum histone methyltransferases for next-generation antimalarial strategies.

Parthiban Ezhumalai E, Ramanibai Ravichandran R, Ramachandran Maduraiveeran M

Plasmodium falciparum is the major human malaria parasite and its treatment remains challenging, with current artemisinin-based combination therapies increasingly compromised by emerging resistance in several regions. Although the pre-erythrocytic vaccines, Mosquirix and R21, are recommended only for children under five years of age in highly endemic African regions, their protective efficacy is moderate and wanes over time, underscoring the continued need for effective antimalarial drugs. Epigenetic mechanisms play a central role in regulating the parasite genome in response to diverse host environments, with methyltransferases acting as key components that dynamically modulate chromatin structure to control stage-specific gene expression. These epigenetic factors critically shape parasite fate by governing the expression of surface antigens, including var, RIFINs and STEVORs, thereby enabling immune evasion and the establishment of chronic infections. To date, no therapeutics specifically targeting histone lysine methyltransferases (HKMTs) have reached clinical use, although BIX-01294 has been explored as a candidate antimalarial in preclinical studies. This review synthesizes current knowledge on Plasmodium HKMTs, highlighting their biochemical activities, regulatory roles, and contributions to virulence. While evaluating emerging epigenetic inhibitors as potential antimalarial agents. We further discuss the main challenges in developing such therapies, emphasizing the necessity of detailed structural characterization, optimized pharmacological properties and rigorous validation of candidate compounds across Plasmodium species to enable successful translation.

PMID 42546906
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PubMedThe Journal of the Association of Physicians of India2026-08-03

Artesunate-resistant Plasmodium falciparum at a Tertiary Care Hospital in North India.

Taneja Vinus V, Khosla Pooja P, Narula Shubhank S, Sachdeva Munish M

The emergence of artemisinin resistance poses a serious global challenge to malaria elimination programs. Artemisinin and its derivatives, especially artesunate, are highly effective against Plasmodium falciparum, particularly in severe and uncomplicated cases. However, increasing reports of treatment failure, particularly with artesunate monotherapy, raise concerns regarding emerging resistance. We present a clinically significant case of suspected artesunate-resistant P. falciparum in an Indian male residing in Nigeria. Despite standard therapy, parasite clearance was delayed, necessitating therapeutic modification. While this case report demonstrates clinical resistance, the lack of confirmatory genetic testing (such as Pfkelch13 mutation screening) remains a limitation.

PMID 42543976
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PubMedPhytochemistry2026-07-31

Naturally occurring triterpenoids from plants as potential agents against malaria: a review from 1994 to 2025.

Sikam Klev Gaïtan KG, Happi Gervais Mouthé GM, Mbock Mbamba Ange Lucie AL, Kemayou Guy-Paulin Mouthé GM et al.

Malaria continues to pose a significant global health challenge, with the World Health Organization reporting an estimated 282 million cases and 610,000 deaths in 2024. The rapid spread of resistance to both chloroquine and artemisinin-based combination therapies by Plasmodium falciparum, confirmed in at least eight sub-Saharan African countries, highlights the urgent need for new antimalarial treatments. Triterpenoids derived from medicinal plants represent one of the most structurally diverse and pharmacologically promising classes of natural products for antimalarial drug discovery. These compounds are biosynthesized through the polymerization of six isoprene units, a process regulated by various enzymes. This document provides a comprehensive summary of data on antiplasmodial triterpenoids, compiled from primary literature spanning the last three decades, from 1994 to September 2025. It covers 279 structurally characterized compounds across 18 skeletal classes. The document includes an in-depth discussion on activity trends, structure-activity relationships (SAR), mechanistic findings, and multi-criteria evaluations for drug discovery. It also critically assesses key gaps and future research priorities. This work aims to offer valuable insights for researchers interested in exploring triterpenoid scaffolds for antimalarial drug development.

PMID 42532326
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PubMedMolecular immunology2026-07-31

Dihydroartemisinin promotes neurological rehabilitation after ischemic stroke by targeting TAK1-CREB1 signaling pathway to inhibit ferroptosis.

Ye Suhong S, Bao Ling L, Xu Qiaolu Q, Ding Zihan Z et al.

Ischemic stroke accounts for 87% of all stroke cases, and remains a leading cause of mortality and disability worldwide. Current reperfusion therapies are limited by narrow therapeutic windows, and cerebral ischemia-reperfusion injury (CIRI) remains a major clinical challenge. Ferroptosis, an iron-dependent form of regulated cell death characterized by lethal lipid peroxidation, has been identified as a key pathological driver of CIRI. Dihydroartemisinin (DHA), a semi-synthetic derivative of artemisinin, has shown neuroprotective effects in ischemic stroke, but its underlying mechanism, especially the regulatory effect on ferroptosis via the TAK1-CREB1 signaling axis, remains unclear. To investigate the neuroprotective effect of DHA in ischemic stroke and its molecular mechanism related to the TAK1-CREB1 signaling pathway and ferroptosis regulation. Wild-type (WT) C57BL/6 J mice and astrocyte-specific CREB1 conditional knockout (CREB1 CKO) mice were used to establish a photothrombotic stroke (PTs) model. Neurological function was evaluated by modified neurological severity score (mNSS), Bederson score, Garcia scale and hanging test. Cerebral infarct volume was measured by TTC staining. Cerebral blood flow (CBF) was detected by laser speckle contrast imaging. Histopathological changes were observed by HE and Nissl staining. Mitochondrial ultrastructure was examined by transmission electron microscopy (TEM). The levels of malondialdehyde (MDA), glutathione (GSH), NADPH/NADP+ ratio, ferrous iron (Fe2+) and total iron in brain tissue were detected by biochemical kits. The expression of ferroptosis-related proteins and CREB1 was detected by Western blot and immunofluorescence staining. DHA treatment dose-dependently improved neurological function, reduced infarct volume, restored CBF, and ameliorated histopathological damage in PTs mice. TEM revealed that DHA reversed ferroptosis-typical mitochondrial changes in ischemic brain tissue. Biochemically, DHA decreased MDA, Fe²⁺, and total iron, while increasing GSH and NADPH/NADP⁺ ratio. Mechanistically, DHA dose-dependently upregulated GPX4, xCT, and FTH1, and downregulated ACSL4. Notably, astrocyte-specific CREB1 knockout nearly completely abolished DHA's neuroprotective and anti-ferroptosis effects. DHA promotes neurological rehabilitation after ischemic stroke by targeting the astrocytic TAK1-CREB1 signaling pathway to inhibit ferroptosis. This study provides a novel theoretical basis and promising candidate drug for the clinical treatment of ischemic stroke.

PMID 42531938
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PubMedTransactions of the Royal Society of Tropical Medicine and Hygiene2026-07-30

Efficacy of artemisinin derivatives and kelch13 mutations in Plasmodium falciparum: a systematic review and meta-analysis.

Ulusan Bağcı Özlem Ö, Elhan Atilla Halil AH, Akarsu Gülay Aral GA

Artemisinin-based combination therapies (ACTs) remain the cornerstone of treatment for uncomplicated Plasmodium falciparum malaria; however, the spread of artemisinin resistance linked to kelch13 (pfk13) mutations poses a major global concern. This study aimed to systematically evaluate ACT efficacy in parallel with the global distribution of pfk13 mutations and to explore the relationship between molecular markers and clinical outcomes. A systematic review and meta-analysis were conducted using PubMed, Web of Science, and Scopus. Studies reporting 28-day adequate clinical and parasitological response (ACPR) following ACTs and assessing pfk13 mutations were included. Thirty studies from Asia, Africa, and the Americas were analyzed. ACTs maintained high efficacy, with pooled ACPR rates exceeding 95% and no significant regional differences (P = .99). By contrast, pfk13 mutation prevalence was significantly higher in Asia (P = .001). Notably, high treatment success rates were maintained despite the increasing prevalence of pfk13 mutations, indicating that the relationship between molecular resistance markers and clinical outcomes remains complex and may be modulated by partner-drug efficacy, host immunity, and local transmission dynamics. While ACTs remain highly effective, the marked geographical variation and persistence of resistance-associated mutations underscore the need for integrated molecular surveillance and therapeutic efficacy monitoring.

PMID 42529832
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