donepezil / Generic mfg. - LARVOL DELTA

Saccadic Oscillations After Donepezil Administration in Patients with Dementia: Time Course and Clinical Correlates. (PubMed, J Eye Mov Res) - "On rmcorr, SO without fixation was associated with the VADL (r = 0.59, p = 0.005) but neither measure was associated with the DHI. A transient, fixation-specific increase in SO was observed, peaking at one month and only partially resolved by three months; it correlated with functional disability rather than subjective handicap, suggesting that video-oculography warrants further study as a potential pharmacodynamic correlate of cholinergic drug effect in dementia."

Journal • Alzheimer's Disease • CNS Disorders • Dementia • Otorhinolaryngology

Effect of Donepezil on Speech Recognition in Adult Cochlear Implant Users: A Pilot Randomized Clinical Trial. (PubMed, Ear Hear) - "These findings provide preliminary evidence that cholinergic enhancement with donepezil may improve speech perception and facilitate neuroplasticity in multisensory and cognitive brain regions in CI users. In addition, the neuroimaging analyses support cholinergic-induced neuroplasticity with DPZ treatment. While this pilot study was underpowered to determine the clinical efficacy of donepezil, pharmacological interventions like donepezil represent a promising novel approach to optimizing CI outcomes, and we offer recommendations for future clinical trials in this population."

Clinical • Journal • Fatigue • Otorhinolaryngology

Neuropsychiatric Symptom Changes in Parkinson's Disease Patients Treated with Different Doses of Donepezil: A 24-Week Follow-up Study (MDS Congress 2026) - No abstract available

Clinical • CNS Disorders • Movement Disorders • Parkinson's Disease • Psychiatry

Isatin derivatives as potent cholinesterase inhibitors: recent developments and future challenges. (PubMed, RSC Adv) - "However, the currently approved small molecules, including tacrine, donepezil, rivastigmine, and galantamine, are limited by their modest efficacy, poor selectivity, and adverse effects, necessitating the development of improved therapeutic agents. Structure-activity relationship studies have revealed the critical influence of electronic effects, linker optimization, N-substitution, and molecular hybridization on inhibitory potency and selectivity. This review summarizes the most promising isatin-based cholinesterase inhibitors reported from 2020 to the present, highlighting their biological activities, structure-activity relationships, and potential for the development of next-generation anti-Alzheimer therapeutics."

Journal • Review • Alzheimer's Disease • CNS Disorders • Pain

Crystal structure, intermolecular interactions, Hirshfeld surface analysis, theoretical studies and biological evaluation of (E)-5-(benzyloxy)-2-{[(2,5-dimethoxyphenyl)imino]methyl}phenol, a new Schiff base. (PubMed, Acta Crystallogr C Struct Chem) - "Compared with the corresponding reference inhibitors, BDIMPh showed a slightly higher IC50 value than donepezil for AChE, a slightly lower IC50 value than ethacrynic acid for GST and a higher IC50 value than acarbose for α-glucosidase. These results indicate an enzyme-dependent inhibitory profile rather than uniformly superior activity relative to the reference inhibitors."

Journal • Pain • Tyrosinase

Formoterol attenuates lipopolysaccharide-induced mnemonic impairment in the delayed nonmatch to position task in rats. (PubMed, Behav Pharmacol) - "By means of validation, the effect of treatment with the muscarinic receptor antagonist scopolamine [0.02 mg/kg, subcutaneously (s.c.)], known to disrupt performance in the task, and its reversal by coadministration of the cognitive-enhancing agent and acetylcholinesterase inhibitor donepezil (0.3 mg/kg, s.c.) were confirmed. Coadministration of Formoterol (0.5 mg/kg, s.c.) attenuated LPS-driven mnemonic impairments in males but not females. Overall, the results show the DNMTP task is a paradigm sensitive to acute systemic inflammation and indicate that Formoterol may have useful anti-inflammatory properties in mitigating inflammatory-associated cognitive impairment."

Journal • Preclinical • Cognitive Disorders • Inflammation

Transcriptomic integration reveals immune heterogeneity in vascular dementia and identifies ELF2 as a candidate therapeutic target. (PubMed, Medicine (Baltimore)) - "Molecular docking analysis suggested strong binding affinities between ELF2 and nicergoline (-7.23 kcal/mol), nimodipine (-6.92 kcal/mol), and donepezil (-6.29 kcal/mol). This integrative transcriptomic study reveals disrupted immune balance and neuroglial-vascular cell homeostasis in vascular dementia, and prioritizes ELF2 as a candidate regulator associated with immune heterogeneity in VaD."

Heterogeneity • Journal • CNS Disorders • Dementia • Solid Tumor • CD4

Design, Synthesis and Molecular Docking Studies of Some Novel Hydrazone Derivatives Based on Trimetazidine as Selective and Potent AChE Inhibitors. (PubMed, Drug Dev Res) - "The compounds were evaluated for in vitro inhibition of AChE and butyrylcholinesterase (BChE) using donepezil and tacrine as reference inhibitors, respectively. To rationalize the observed activity trends, molecular docking studies were performed, suggesting that the most active ligands adopt donepezil-like binding modes spanning the catalytic and peripheral anionic sites and are further stabilized by π-π/π-cation contacts and hydrogen-bonding interactions within the active gorge. Overall, these findings identify trimetazidine-derived hydrazide-hydrazones as a promising chemotype for the development of selective AChE inhibitors and provide a basis for further optimization and advanced biological validation."

Journal • Alzheimer's Disease • CNS Disorders • Pain

Multi-functional bionic nanoparticles for precise neuronal targeting and synergistic therapy in Alzheimer's disease. (PubMed, Mater Today Bio) - "The nanoparticles (NPs) core was fabricated using safe, biocompatible poly (lactic-co-glycolic acid) (PLGA) to co-deliver natural product genistein and mature marketed donepezil, which act synergistically to enhance therapeutic efficacy. Collectively, BTRN treats AD through multiple mechanisms, including reducing Aβ production, regulating cholinergic function, and inhibiting neuronal apoptosis. This biomimetic system presents a promising therapeutic strategy and offers valuable insights for the clinical translation of combination therapies in AD."

Journal • Alzheimer's Disease • CNS Disorders

Topical Donepezil for Cholinergic Modulation in Chronic Wound Repair. (PubMed, Wound Repair Regen) - "This approach may complement metabolic therapies that support arginine-NO coupling and redox balance. Controlled pilot studies should assess local cutaneous pharmacodynamics, perfusion responses, and wound-closure outcomes."

Journal • Review • Pain • NOS3

Efficacy of donepezil in patients with chronic tinnitus. (PubMed, Clinics (Sao Paulo)) - "In the present double-blind, randomized, placebo-controlled clinical trial, no statistically significant difference was identified between the groups regarding the primary outcome. However, the donepezil-treated group demonstrated better performance than the placebo group, and a possible indication of greater clinical benefit was observed in the treatment group in those using amplification, suggesting a potential therapeutic relevance, but larger, more in-depth studies are needed to confirm our findings."

Clinical • Journal • CNS Disorders • Dementia • Otorhinolaryngology

Bushen-Yizhi formula promotes neurogenesis and ameliorates cognitive impairment by activating ST8Sia Ⅱ/Ⅳ-PSA-NCAM pathway in ibotenic acid induced mice. (PubMed, J Ethnopharmacol) - "Our study demonstrates BSYZ promotes hippocampal neurogenesis to ameliorate cognitive impairment by activating ST8Sia II/IV-PSA-NCAM pathway. These findings provide mechanistic evidence supporting the therapeutic potential of BSYZ for AD treatment."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • NCAM1 • NES

Longitudinal Multi-tracer PET/CT for Monitoring the Progression of Diabetic Cardiac Autonomic Neuropathy: A Preclinical Study. (PubMed, Acad Radiol) - "This multi-tracer longitudinal investigation establishes that parasympathetic denervation precedes sympathetic impairment during DCAN development, with both deficits predating microvascular and metabolic crises. These insights offer a critical, noninvasive diagnostic window for early DCAN detection and clinical monitoring."

Journal • Preclinical • Diabetes • Diabetic Neuropathy • Inflammation • Metabolic Disorders • Pain • Type 2 Diabetes Mellitus

Phase 3 randomized placebo-controlled trial of donepezil for cancer-related cognitive impairment among breast cancer survivors: Results on patient-reported cognitive function from the Wake Forest NCI Community Oncology Research Program (NCORP) Research Base REMEMBER trial (WF97116). (ASCO 2023) - P3 | "There were no differences in PRO-assessed cognitive function domains between donepezil or placebo. The magnitude of improvement in patient-rated cognitive function was comparable across treatment arms. These results underscore the importance of placebo controls for CRCI intervention trials."

Clinical • P3 data • Alzheimer's Disease • Breast Cancer • Cognitive Disorders • Depression • Fatigue • Oncology • Psychiatry • Solid Tumor

Phase III Randomized, Placebo-Controlled Clinical Trial of Donepezil for Treatment of Cognitive Impairment in Breast Cancer Survivors After Adjuvant Chemotherapy (WF-97116). (PubMed, J Clin Oncol) - "BCS 1-5 years after completing chemotherapy with documented memory problems, randomly assigned to 24 weeks of 5-10 mg of donepezil once daily, did not perform differently at the end of treatment on tests of memory, other cognitive functions, or subjective functioning than those randomly assigned to placebo."

Clinical • Journal • P3 data • Alzheimer's Disease • Breast Cancer • Cognitive Disorders • Oncology • Solid Tumor

Integrated computational and automated flow synthesis platform for the rapid discovery of N-benzylpiperidine acetylcholinesterase inhibitors. (PubMed, Eur J Med Chem) - "Single-point screening at 5 μM identified ten compounds with ≥70% AChE inhibition, and dose-response determination against electric eel AChE (eeAChE) gave three sub-200 nM inhibitors: 69 (91 nM), 8 (93 nM) and 12 (117 nM), each exceeding galantamine (237 nM) and approaching donepezil (1, 42 nM) under identical assay conditions. The complete cycle was executed in under three months by a three-person team. We report this as a measured platform capability rather than as accelerated drug discovery allowing the rapid generation of first-round leads."

Journal • Alzheimer's Disease • CNS Disorders • Pain

Targeting the protein tyrosine phosphatase 1B signaling axis in Alzheimer's disease: Emerging therapeutic potential of ivermectin. (PubMed, Biochem Biophys Res Commun) - "The in vivo study of IVM (10 mg/kg) in the mouse model showed improvement in cognitive deficits on behavioral assays and was comparable to donepezil and DPM1001...The IHC showed a reduction in the Aβ plaque load and activated microglia cell count. These preliminary data demonstrate that IVM exhibits considerable PTP1B inhibitory potential and require further exploration in a robust, statistically powered preclinical study, followed by clinical trials, to repurpose it in AD and related conditions."

Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Inflammation • Metabolic Disorders • PTPN1

Synthesis, Characterization, and Multifunctional Bioactivity of ZnO/CuO@Amoxicillin Nanocomposites: A Synergistic Nano-Platform With Potent Antioxidant, Anti-Inflammatory, Antidiabetic, and Anti-Cholinesterase Activities. (PubMed, Chem Biodivers) - "In antidiabetic assays, the nanocomposite showed strong inhibitory effects on alpha-amylase (IC50 = 21.57 ± 1.68 mg/mL) and alpha-glucosidase (IC50 = 13.95 ± 0.76 mg/mL), with activities comparable to acarbose, while anti-inflammatory tests yielded low IC50 values of 0.22 ± 0.03 mg/mL for egg albumin denaturation and 0.34 ± 0.07 mg/mL for human serum albumin, approaching the performance of diclofenac. Antioxidant performance was outstanding, with total antioxidant capacity of 298.27 ± 4.70 mg ascorbic acid equivalents per gram and ferric reducing antioxidant power of 311.67 ± 2.53 mM Fe2 +/g, both higher than ascorbic acid, alongside efficient hydrogen peroxide scavenging (IC50 = 0.16 ± 0.04 mg/mL) and protection against H2O2/FeCl3-induced hemolysis at an IC50 of 0.007 ± 0.00 mg/mL; together with moderate but significant acetylcholinesterase inhibition (IC50 = 33.16 ± 3.02 mg/mL vs...."

Journal • Hematological Disorders • Inflammation • Metabolic Disorders

Design of a spermine-β-cyclodextrin functionalized gelatin nanoaggregate hydrogel for nose-to-brain delivery of donepezil. (PubMed, RSC Adv) - "Collectively, these findings establish a clear structure-property-function relationship, demonstrating that chemically engineered SPM-β-CD nanoaggregates function as molecular regulators of gelatin hydrogel architecture. To the best of our knowledge, this study is the first to report a chemically engineered SPM-β-CD nanoaggregate gelatin hydrogel that utilizes supramolecular nanoaggregate engineering for sustained intranasal delivery of donepezil."

Journal

Computational identification of novel acetylcholinesterase inhibitors as potential treatments for Alzheimer's disease. (PubMed, J Alzheimers Dis) - "Although symptomatic treatments are available, they neither prevent nor halt disease progression; therefore, it is necessary to develop new therapeutic alternatives.ObjectiveTo identify acetylcholinesterase inhibitors with potential biological activity through a computational protocol.MethodsIn this study, a computational approach based on virtual screening, molecular docking, and molecular dynamics simulations was applied to identify new potential acetylcholinesterase inhibitors.ResultsThe results allowed the identification of three compounds with higher binding affinities than donepezil, which was used as a reference. Among them, ligand code 24771824 stood out for establishing hydrophobic and aromatic interactions that maximize dispersive contributions and promote a rigid and stable conformation within the active site. In contrast, ligand codes 151171 and 21081761 were favored by more directional polar contacts, which increased specificity but limited the overall..."

Journal • Alzheimer's Disease • CNS Disorders

L-theanine attenuates AlCl3-induced cognitive dysfunction and neurotoxicity in rats: a behavioral and biochemical study. (PubMed, Turk J Med Sci) - "A total of 32 male Wistar rats were allocated into four groups: control, AlCl3-induced AD-like group, LTN-treated AD-like group, and donepezil-treated AD-like group...The increases in lipid peroxidation and nitric oxide observed in the AlCl3 group were suppressed by LTN treatment, while decreased antioxidant defenses, namely reduced glutathione levels and catalase activity, were restored. The findings demonstrate that AlCl3 exposure impairs cholinergic function, induces oxidative damage, and leads to cognitive dysfunction, whereas LTN treatment effectively mitigates these effects, suggesting potential neuroprotective benefits against aluminum-induced neurotoxicity."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • CAT • MPO

Ficus deltoidea preserves neuronal-glial ultrastructure and attenuates neuroinflammation in an Alzheimer's disease-like rat model. (PubMed, Nutr Neurosci) - "Histopathological analysis demonstrated dose-dependent preservation of pyramidal neurons in prefrontal cortex and hippocampal layers II (p < 0.0001), III (p < 0.0001), and V (p < 0.0001), with the highest dose of FD producing neuronal viability comparable to donepezil...Collectively, this study provides the first integrated ultrastructural and molecular evidence that FD confers multi-level neuroprotection across the cortical-hippocampal axis by preserving neuronal-glial architecture and attenuating neuroinflammation. These findings highlight FD as a promising multi-target natural candidate for mitigating neurodegenerative processes associated with AD."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders • Inflammation • IL1B • IL6 • TNFA

AMBMP Hydrochloride Reverses STZ-Induced Alzheimer-Type Dementia Associated with Wnt/β-catenin/TLR4 Signaling. (PubMed, Neuromolecular Med) - "Mice received bilateral intracerebroventricular (i.c.v.) injections of STZ (3 mg/kg) on Day 1 and Day 3, followed by administration of Donepezil (3 mg/kg)/ AMBMP Hydrochloride (5 mg/kg and 10 mg/kg)/Palmitic acid (TLR4 agonist, 20 mg/kg) via the intraperitoneal (i.p.) route from Day 4 to Day 22...In summary, we confirmed that AMBMP Hydrochloride exhibits potent neuroprotective effects associated with modulating Wnt/β-catenin/TLR4 signaling, offering a promising therapeutic approach against Alzheimer-Type Dementia. Future studies should delve deeper into the molecular mechanisms and translational promise of AMBMP hydrochloride, paving the way for its development as a potential candidate for AD management."

Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Dementia • Inflammation • Oncology • Pain • IL1B • IL6 • TNFA

Design and synthesis of quinoline-derived thioureas as potential antihyperglycemic, anti-Alzheimer, and antioxidant agents. (PubMed, RSC Adv) - "Among forty-one compounds, 27-31 and 33-37 showed excellent inhibition against α-amylase (IC50 = 18.36-28.21 µM) and α-glucosidase (IC50 = 17.77-29.31 µM) compared to the standard acarbose (IC50 = 16.98 ± 0.12, 14.19 ± 0.06 µM). Moreover, compounds 27, 28, 30, 31, 34, 35, and 37 inhibited AChE (IC50 = 5.60-14.97 µM) and BChE (IC50 = 6.99-15.70 µM) with greater potency than the standard donepezil chloride (IC50 = 1.49 ± 0.13, 2.39 ± 0.06 µM)...Among this library, compound 31, with a difluoro group on the phenyl ring, was identified as the most potent inhibitor against all enzymes. Thus, this study suggests that the reported compounds hold the potential to be further advanced as lead anti-Alzheimer and anti-diabetic agents."

Journal • Alzheimer's Disease • CNS Disorders • Diabetes • Pain

Acupuncture for Alzheimer's disease: A systematic review and meta-analysis integrating traditional insights and scientific evidence. (PubMed, J Integr Med) - "This review highlights acupuncture as a holistic, multi-targeted therapy with promising potential for managing AD. Future research should aim to standardize acupuncture protocols, integrate TCM syndrome differentiation, and adopt neurobiological and imaging techniques to explore mechanisms. Please cite this article as: Huang WL, Wang LL, Shi JR, Liu Q. Acupuncture for Alzheimer's disease: A systematic review and meta-analysis integrating traditional insights and scientific evidence. J Integr Med. 2026; Epub ahead of print."

Journal • Retrospective data • Review • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Dementia