Cognex (tacrine) / Shionogi 
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  • ||||||||||  donepezil / Generic mfg., galantamine hydrobromide / Generic mfg., memantine / Generic mfg.
    Review, Journal:  Potential therapeutic natural products against Alzheimer's disease with Reference of Acetylcholinesterase. (Pubmed Central) -  Aug 13, 2021   
    In this review we summarize the studies reporting phytocompounds and extracts from medicinal plants that show AChE inhibitory activities and could be of potential benefit in AD. Future research directions are suggested and recommendations made to expand the use of medicinal plants and their formulations to prevent, mitigate and treat AD.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal:  Dimeric Tacrine(10)-hupyridone as a Multitarget-Directed Ligand To Treat Alzheimer's Disease. (Pubmed Central) -  Aug 4, 2021   
    Our results indicated that A10E could produce anti-AD neuroprotective effects via the inhibition of Aβ aggregation, the activation of the BDNF/TrkB pathway, the alleviation of neuroinflammation, and the decrease of AChE activity. As MTDLs could produce additional benefits, such as overcoming the deficits of drug combination and enhancing the compliance of AD patients, our results also suggested that A10E might be developed as a promising MTDL lead for the treatment of AD.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal:  Accuracy and precision of binding free energy prediction for a tacrine related lead inhibitor of acetylcholinesterase with an arsenal of supercomputerized molecular modelling methods: a comparative study. (Pubmed Central) -  Jul 30, 2021   
    The binding free energies were estimated using flexible molecular docking, molecular mechanics/generalized Born surface area/Poisson-Boltzmann surface area (MM/GBSA/PBSA), transmutation REST/FEP with 12 x 5 ns/λ windows, annihilation FEP with 20 x 5 ns/λ steps, PMF with weight histogram analysis method (WHAM) and 40 x 5 ns samples, and PMF/AWH with 10 x 100 ns replicas. Confrontation of the classical approaches such as canonical molecular dynamics and molecular docking with alchemical calculations and steered molecular dynamics enabled us to show how large errors in ΔG predictions can be expected if these in silico methods are employed in the elucidation of a common case of enzyme inhibition.Communicated by Ramaswamy H. Sarma.
  • ||||||||||  donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
    Review, Journal:  The State of The Art on Acetylcholinesterase Inhibitors in the Treatment of Alzheimer's Disease. (Pubmed Central) -  Jul 22, 2021   
    The purpose of this review is to provide an overview of what has been published over the last decade on the effectiveness of AChEIs in AD, analysing the most relevant issues under the clinical and methodological profiles and the consequent possible welfare effects for the whole world. Furthermore, novel drugs and possible therapeutic approaches are also discussed.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal:  Tacrine-sugar mimetic conjugates as enhanced cholinesterase inhibitors. (Pubmed Central) -  Jul 21, 2021   
    Two of the heterodimers were significantly stronger acetylcholinesterase inhibitors than the monomeric tacrine. Molecular modelling indicated that the longer heterodimers fitted better into the active gorge of acetylcholinesterase than the shorter counterparts and the former provided more efficient simultaneous interaction with the tryptophan residues in the catalytic anionic binding site (CAS) and the peripheral anionic binding site (PAS).
  • ||||||||||  donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
    Journal:  Natural products and their derivatives as multifunctional ligands against Alzheimer's disease. (Pubmed Central) -  Jul 11, 2021   
    Therefore, natural products and their derivatives with proven efficacy could be used in the management of the neurodegenerative disorders. This review focuses on the natural product based multitarget directed ligands like tacrine-coumarin, tacrine-huperzine A, harmine-isoxazoline, berberine-thiophenyl, galantamine-indole, pyridoxine-resveratrol, donepezil-curcumin and their mode of action.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Review, Journal:  Tacrines as Therapeutic Agents for Alzheimer's Disease. V. Recent Developments. (Pubmed Central) -  Jul 7, 2021   
    Herein we have reviewed our recent developments for the identification of new tacrine analogues for Alzheimer's disease (AD) therapy...Thus, the drug was withdrawn from the clinics administration. Since then, many publications have described non-hepatotoxic tacrines, and in addition, important efforts have been made to design multitarget tacrines by combining their cholinesterase inhibition profile with the modulation of other biological targets involved in AD.
  • ||||||||||  Cognex (tacrine) / Shionogi
    [VIRTUAL] Synthesis of isatin-thiazolidine-2-thione hybrids for acetylcholinesterase inhibition () -  Jun 27, 2021 - Abstract #ACSMARM2021ACS_MARM_45;    
    The current AChE inhibitors (AChEi) are both incapable of halting or reversing disease progression and potentially damaging to other organs, such as liver toxicity from tacrine...In addition, molecular modeling images of selected hybrids docked with AChE will show the predicted binding energies and conformations. Isatin-based inhibitors could be the key in discovering new treatments to low AD progression.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Clinical, Journal:  EXPRESS: Cerebrovascular events and outcomes in hospitalized patients with COVID-19: The SVIN COVID-19 Multinational Registry. (Pubmed Central) -  Jun 22, 2021   
    The validation parameters such as LOD, LOQ and recovery (%) were calculated in the range of 2.87 mM, 9.58 mM and 85-96%, respectively. Of the 14,483 patients with laboratory-confirmed SARS-CoV-2, 172 were diagnosed with an acute cerebrovascular event (1.13% of cohort; 1130/100,000 patients, 95%CI 970-1320/100,000), 68/171 (40.5%) were female and 96/172 (55.8%) were between the ages 60 and 79 years...No abstract available
  • ||||||||||  midazolam hydrochloride / Generic mfg., ritonavir / Generic mfg., dextromethorphan / Generic mfg.
    Preclinical, Journal:  An Automated Cocktail Method for In Vitro Assessment of Direct and Time-Dependent Inhibition of Nine Major Cytochrome P450 Enzymes - Application to Establishing CYP2C8 Inhibitor Selectivity. (Pubmed Central) -  Jun 22, 2021   
    Time-dependent inhibitors (furafylline/CYP1A2, selegiline/CYP2A6, clopidogrel/CYP2B6, gemfibrozil 1-O-β-glucuronide/CYP2C8, tienilic acid/CYP2C9, ticlopidine/CYP2C19, paroxetine/CYP2D6 and ritonavir/CYP3A) and direct inhibitor (terfenadine/CYP2J2) showed similar inhibition with single substrate and cocktail methods...In conclusion, a reliable cocktail method including the nine most important drug-metabolizing CYP enzymes was developed, optimized and validated for detecting time-dependent inhibition. Moreover, gemfibrozil 1-O-β-glucuronide was established as a selective inhibitor of CYP2C8 for use as a diagnostic inhibitor in in vitro studies.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal:  Integration of Mass Spectrometry Imaging and Machine Learning Visualizes Region-Specific Age-Induced and Drug-Target Metabolic Perturbations in the Brain. (Pubmed Central) -  Jun 22, 2021   
    We examined the interplay between aging and the response to tacrine-induced acetylcholinesterase inhibition, a well-characterized therapeutic treatment against dementia...An age-induced increase of endogenous antioxidants, such as α-tocopherol, in the hippocampus was detected, suggesting an augmentation of neuroprotective mechanisms in early aging. Our comprehensive imaging approach visualized heterogeneous age-induced metabolic perturbations in mitochondrial function, neurotransmission, and lipid signaling, not always attenuated by acetylcholinesterase inhibition.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal:  Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease. (Pubmed Central) -  Jun 16, 2021   
    We applied a framework combination of functionalized CNSL components and well-established acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) tacrine templates...The X-ray crystal structure of 5 complexed with BChE allowed rationalizing the observed activity (0.0352 nM). Investigation in BV-2 microglial cells revealed antineuroinflammatory and neuroprotective activities for 5 and 6 (already at 0.01 μM), confirming the design rationale.
  • ||||||||||  Legalon (silibinin) / Mylan, Cognex (tacrine) / Shionogi
    Journal:  Binding studies of known molecules with acetylcholinesterase and bovine serum albumin: A comparative view. (Pubmed Central) -  Jun 4, 2021   
    Further, the protein-ligand complexes are subjected to molecular dynamics and binding free energy calculation to confirm the stability of the molecule in the active site of BSA and AChE. The NCI (non-covalent interaction) approach supports to visualize the iso-surface of the reduced density gradient of such interactions between protein and ligands.
  • ||||||||||  Review, Journal:  Alzheimer's disease treatment: The share of herbal medicines. (Pubmed Central) -  May 7, 2021   
    Lavandula angustifolia, Ginkgo biloba, Melissa officinalis, Crocus sativus, Ginseng, Salvia miltiorrhiza, and Magnolia officinalis have been widely used for relief of symptoms of some neurological disorders. This paper reviews the therapeutic effects of phytomedicines with prominent effects against various factors implicated in the emergence and progression of AD.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal:  Tacrine modulates Kv2.1 channel gene expression and cell proliferation. (Pubmed Central) -  May 5, 2021   
    These lines of evidence indicate that application of tacrine downregulates the expression of Kv2.1 channels and increase cell proliferation. The effect of tacrine on Kv2.1 channels may provide an alternative explanation for its neuroprotective action.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal:  Deep learning based detection of intracranial aneurysms on digital subtraction angiography: A feasibility study. (Pubmed Central) -  May 1, 2021   
    The effect of tacrine on Kv2.1 channels may provide an alternative explanation for its neuroprotective action. The commercial-grade deep learning software allows for detection of intracranial aneurysms on whole-brain, 2D anteroposterior and lateral digital subtraction angiography images, with results being comparable to more specifically engineered deep learning techniques.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal:  Late-Stage Modification of Medicine: Pd-Catalyzed Direct Synthesis and Biological Evaluation of N-Aryltacrine Derivatives. (Pubmed Central) -  Apr 20, 2021   
    Cell-based assays against HepG2 and SH-SY5Y cell lines revealed that 3o had significantly lower hepatotoxicity compared to tacrine, with additional neuroprotective activity against HO-induced damage in SH-SY5Y cells. The advantages including synthetic accessibility, high potency, low toxicity, and adjunctive neuroprotective activity make compound 3o a new promising multifunctional candidate for the treatment of Alzheimer's disease.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal:  Model Amphipathic Peptide Coupled with Tacrine to Improve Its Antiproliferative Activity. (Pubmed Central) -  Mar 30, 2021   
    In turn, BBB-permeability studies were inconclusive, and conjugation to the CPP led to a considerable loss of Tacrine function as an AChE inhibitor. Nonetheless, this work reinforces the potential of repurposing Tacrine for cancer and enhances the antiproliferative activity of this drug through its conjugation to a CPP.