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donepezil + memantine ER (ADS8703 / Arimenda / ADS8704)

✓ Approved

Forest Laboratories Inc. · ACHE · 小分子

什么是 donepezil + memantine ER?

donepezil + memantine ER 是一种小分子,由Forest Laboratories Inc.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ADS8703, Arimenda, ADS8704
公司Forest Laboratories Inc.
药物类别小分子
分子靶点ACHE, GRIN1
给药途径Oral (PO)
状态Approved

作用机制

分子靶点

donepezil + memantine ER 作用于 2 个分子靶点:

ACHEacetylcholinesterase (Cartwright blood group) (N-ACHE, ACEE)
GRIN1glutamate ionotropic receptor NMDA type subunit 1 (NMD-R1, NMDA1)
需要更深入的分析?Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

donepezil + memantine ER 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
Nervous system disordersDementia Alzheimer's type✓ Approved

相关研究文献

PubMedTraffic (Copenhagen, Denmark)2026-09-10

Investigating Translocation Mechanisms of TDP-43 Into the Endoplasmic Reticulum Using Budding Yeast Models.

Saito Miku M, Tsuzuki Hana H, Hosomi Akira A

Signal peptides direct secretory and membrane proteins to the endoplasmic reticulum (ER), but proteins lacking classical signal peptides can occasionally engage the ER translocation machinery. TDP-43 is a nuclear RNA-binding protein implicated in amyotrophic lateral sclerosis and frontotemporal lobar degeneration. TDP-43 pathology has been linked to extracellular TDP-43 species, association with the ER luminal oxidoreductase PDI, and ER stress-related phenotypes, yet whether TDP-43 fragments can directly access the ER lumen remains unclear. Here, we used budding yeast to examine signal peptide-independent ER entry of TDP-43. C-terminal fragments of TDP-43 acquired N-glycans in ste24Δ cells, whereas full-length TDP-43 showed little detectable ER entry. Endo H digestion confirmed N-glycosylation of the fragments, and a protease protection assay supported ER luminal localization of TDP-43(Δ2-89). ER entry was reduced by sec61-41 and sec66Δ, indicating engagement of a Sec61/Sec66-dependent translocation pathway. Deletion analyses identified opposing sequence elements: residues 320-343 facilitated ER entry, whereas an N-terminal region upstream of the nuclear localization signal suppressed it. TDP-43(Δ2-89) also accessed the secretory pathway, and selected disease-associated variants caused Ire1-dependent growth vulnerability without increasing detectable ER translocation. These findings reveal a Ste24-suppressed route for noncanonical ER entry of TDP-43 fragments.

PMID 42719958
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PubMedAAPS PharmSciTech2026-09-10

Correlative Spectroscopic and Structural Imaging for Resin-Embedded Extended-Release Morphine Sulfate Pellets.

Zaker Yeakub Y, Ahmed Snober S, Tian Li L, Yilmaz Huzeyfe H et al.

Correlative spectroscopic and structural imaging provides a powerful approach for characterizing the microstructure of complex pharmaceutical formulations. Laser direct infrared (LDIR) spectroscopy is an emerging, rapid spectroscopic imaging technique that complements traditional approaches by enabling non-destructive chemical and morphological analysis over large sample surfaces within minutes. In this study, the capabilities of LDIR imaging were evaluated alongside Raman mapping, SEM-EDS, laser microscopy, and micro-CT as part of a correlative workflow to characterize the microstructure and chemical composition of pharmaceutical pellets. Resin embedding enabled consistent handling and structural preservation of extended-release pharmaceutical pellets across all imaging modalities. Two commercially available morphine sulfate ER pellets (ER-1 and ER-2) with different excipient compositions were used as model systems. Laser microscopy revealed distinct differences in surface topography, while micro-CT performed before milling confirmed inherent structural features. ER-1 displayed a smooth, intact core, whereas ER-2 exhibited internal cracks and cavities. Hyperspectral LDIR imaging successfully identified major components in both formulations (hit-quality index, HQI ≥ 0.83) with strong concordance to Raman mapping (HQI ≥ 0.85). The spatial distribution of the active pharmaceutical ingredient (API) revealed a layered structure in ER-1 and a homogeneous core in ER-2. This correlative workflow, combining resin embedding with multiple imaging modalities, underscores the value of LDIR and complementary techniques for comprehensive physicochemical characterization of complex drug products. These findings highlight the utility of correlative imaging for regulatory assessment and quality control of complex extended-release formulations.

PMID 42717169
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PubMedFrontiers in cell and developmental biology2026-09-10

Faf2 is required for neural differentiation in embryonic neural progenitor cells.

Kakebeen Anneke Dixie AD, Dunphy Leon L, Hazen Heather K HK, Niswander Lee A LA

Neural progenitor cell differentiation is a complex process requiring the proper integration of instructive and permissive factors. Instructive cues including signaling molecules and transcription factor networks have been well studied in this context, but permissive factors such as cell homeostasis have not. Cell homeostasis is critical to support the health and stability of a cell and enable the cell to act on instructive differentiation cues. Our study investigates a homeostasis protein, FAF2, and its function in neural progenitor cells. FAF2 is an adaptor protein involved in endoplasmic reticulum (ER) associated degradation to remove misfolded proteins and restore ER homeostasis. Here we show that knocking out Faf2 in neural progenitor cells results in increased ER stress signature at the protein and transcription level, indicating a conserved functional role in neural progenitor cells. Induced neural differentiation of FAF2 deletion cells shows a failure of neurite development but RNA-seq indicates genes that support neural differentiation are induced. Reducing ER stress in FAF2 knockout cells with a small molecule inhibitor can rescue neural differentiation, providing evidence that excess ER stress contributes to the inhibited differentiation. Taken together, these results reveal that FAF2 is a critical protein in neural progenitor cells for the maintenance of ER homeostasis and execution of neural differentiation.

PMID 42719004
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PubMedJournal of pineal research2026-09-10

Melatonin Inhibits Metastasis of Sunitinib-Resistant Renal Cell Carcinoma Cells Via the GRP78/p38/CTSD Expression.

Huang Po-Yu PY, Hsieh Yi-Hsien YH, Chen Yong-Syuan YS, Hung Tung-Wei TW et al.

Sunitinib resistance contributes to poor outcomes in advanced renal cell carcinoma (RCC). This study investigated the anti-metastatic effects and underlying mechanisms of melatonin in sunitinib-resistant (SR)-RCC. Melatonin significantly inhibited the migration and invasion of A498-SR and Caki-1-SR cells. SR-RCC cells exhibited elevated CTSD expression, impaired endoplasmic reticulum (ER) stress signaling with reduced GRP78 and IRE1α, and enhanced p38 MAPK activation, all of which were reversed by melatonin. Silencing p38 MAPK further potentiated the inhibitory effects of melatonin on cell migration and invasion. Mechanistically, CTSD expression was regulated through both GRP78/p38 MAPK-mediated ER stress. In vivo, melatonin markedly reduced lung metastasis of Caki-1-SR cells without causing significant toxicity to major organs. Collectively, these findings demonstrate that melatonin inhibited the metastatic potential of SR-RCC by decreasing CTSD expression, restoring ER stress response, and decreasing p38 MAPK expression, supporting its potential as an anti-metastatic therapeutic agent for SR-RCC.

PMID 42720349
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PubMedFrontiers in veterinary science2026-09-10

Role of endoplasmic reticulum stress-mediated autophagy in cadmium-induced apoptosis in BRL-3A cells.

Mao Junbing J, Ling Hao H, Xu Bing B, Shi Yaning Y et al.

Cadmium (Cd), a widely present environmental toxicant, can cause liver damage following chronic exposure. Although endoplasmic reticulum stress (ERS) and autophagy are known to be involved in Cd-induced liver injury, their molecular mechanisms remain incompletely understood. In this study, using an in vitro Cd exposure model and pharmacological interventions, we investigated the mechanisms through which Cd induces autophagy via ERS and its interplay with apoptosis. We found that Cd-induced autophagosome accumulation was linked to the activation of ERS pathways (PERK/eIF2α/ATF4, IRE1α/JNK/Beclin1, and ATF6). Furthermore, this accumulation was also attributable to Cd-induced impairment of autophagic degradation, as evidenced by p62 accumulation. In addition, Cd exposure activates FAM134B-dependent ER-phagy, which requires ERS regulation. Finally, the autophagy activator rapamycin alleviated apoptosis, whereas the inhibitor chloroquine exacerbated it. In summary, our findings reveal a mechanism through which Cd coordinately regulates hepatocyte fate via ER stress-mediated, FAM134B-dependent ER-phagy and canonical autophagy, offering novel therapeutic targets and theoretical foundations for mitigating Cd toxicity.

PMID 42718678
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PubMedFrontiers in cell and developmental biology2026-09-10

Advanced maternal age as a risk factor for endometrial receptivity in repeated implantation failure: intersectional transcriptomic analysis and gene validation.

Guo Yaping Y, Zhang Mianqiu M, Wu Zhenggang Z, Hou Xiaojing X et al.

Repeated implantation failure (RIF) remains a significant challenge in assisted reproductive technology. Endometrial receptivity (ER) plays a critical role in embryo implantation. However, the impact of advanced maternal age (AMA) on ER in this population remains unclear. The study aimed to evaluate whether maternal age is associated with displacement of the window of implantation (WOI) and explore potential endometrial transcriptomic characteristics. This retrospective observational study included 254 women with RIF who underwent evaluation of ER between January 2020 and March 2024. ER status and WOI timing were determined using a transcriptome-based receptivity assessment. Clinical characteristics were compared between women with normal receptivity and those with a 2-day pre-receptive endometrium. Endometrial biopsies were analyzed by RNA sequencing to identify differential gene expression associated with age and receptivity status. An independent small validation cohort was used for qRT-PCR validation. Women in the impaired receptivity group (2-day pre-receptive) were significantly older than those in the normal receptivity group (34.3 ± 3.1 vs. 33.0 ± 4.1, p = 0.016). Multivariate logistic regression further demonstrated maternal age as an independent risk factor for ER displacement (OR = 1.118, 95% CI: 1.013-1.234, p = 0.027). Transcriptomic analysis identified age- and receptivity-associated transcriptomic changes, with 10 overlapping differentially expressed genes (DEGs) between the two comparisons, which were further examined by qRT-PCR in a small independent cohort (n = 10). As a result, four genes, including activating transcription factor 3 (ATF3), C-X-C motif chemokine ligand 1 (CXCL1), parathyroid hormone-like hormone (PTHLH), and non-specific cytotoxic cell receptor protein 1 (NCCRP1), were significantly downregulated in the AMA-RIF group compared with controls. AMA was independently associated with an increased likelihood of WOI displacement in women with RIF, suggesting that aberrant endometrial timing may be associated with implantation failure in this population. These findings provide a rationale for further investigation of personalized embryo transfer strategies in older patients, while the identified candidate genes should be regarded as preliminary molecular associations requiring further functional validation.

PMID 42718970
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