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33 News |  |
- || ladostigil hemitartrate (TV-3326) / Avraham
Review, Journal: Therapeutic agents for Alzheimer's disease: a critical appraisal. (Pubmed Central) - Dec 24, 2024
Chronic oral administration to aging rats prevented the decline in memory and suppressed overexpression of genes adversely affecting synaptic function in relevant brain regions. In a phase 2 trial, ladostigil reduced the decline in short-term memory and in whole brain and hippocampal volumes in human subjects with mild cognitive impairment and had no more adverse effects than placebo.
- | ladostigil hemitartrate (TV-3326) / Avraham
Journal: Ladostigil Reduces the Adenoside Triphosphate/Lipopolysaccharide-Induced Secretion of Pro-Inflammatory Cytokines from Microglia and Modulate-Immune Regulators, TNFAIP3, and EGR1. (Pubmed Central) - Jan 27, 2024
Ladostigil significantly decreased Egr1 gene expression and levels of the protein in the nucleus and increased TNF alpha-induced protein 3 (TNFaIP3), which suppresses cytokine release, in the microglial cytoplasm. Restoration of the aberrant signaling of these proteins in ATP/LPS-activated microglia in vivo might explain the prevention by ladostigil of the morphological and inflammatory changes in the brain of aging rats.
- donepezil / Generic mfg.
Donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer (In-Person) - Jul 6, 2023 - Abstract #AAIC2023AAIC_2473;
protein fragments that accumulate in the brain. The pharmacological profile of compound 11, as well as the fact that it is a readily available compound in a short synthetic sequence, in good chemical yields, prompts us to select it as a lead-compound for further optimization in our current research programme targeted to the preparation of new molecules for the potential treatment of AD.
- | ladostigil hemitartrate (TV-3326) / Avraham
Journal: Oxidative Stress and Its Modulation by Ladostigil Alter the Expression of Abundant Long Non-Coding RNAs in SH-SY5Y Cells. (Pubmed Central) - Nov 23, 2022
We found that the induction of abundant lncRNAs, such as MALAT1, NEAT-1, MIAT, and SHNG12, by the Sin1 oxidative stress paradigm specifies only the undifferentiated cell state. We conclude that a global alteration in the lncRNA profiles upon stress in SH-SY5Y may shift cell homeostasis and is an attractive in vitro system to characterize drugs that impact the redox state of the cells and their viability.
- |||| ladostigil hemitartrate (TV-3326) / Avraham
Clinical: Well for dogs there’s deprenyl. For humans there could be ladostigil — MAO-B inhibitor that increases critical brain volumes. But all you people just want to lambast drugs that decrease volumes 🐶 ruff. (Twitter) - Nov 17, 2022
- || ladostigil hemitartrate (TV-3326) / Avraham
Submitting ladostigil for accelerated approval then?! (Twitter) - Nov 2, 2022
- ||||| ladostigil hemitartrate (TV-3326) / Avraham, donanemab (LY3002813) / Eli Lilly
Licensing / partnership: If concerned #donanemab is assoc with atrophy/neuron/synapse loss, then be super impressed with low dose MAOB-I ladostigil substantially increasing brain & hippocampus volumes, no doubt gaining neurons & synapses. Good stuff? @Lillypad in-licensing opportunity u shouldn't pass up (Twitter) - Nov 2, 2022
- ||| ladostigil hemitartrate (TV-3326) / Avraham, donanemab (LY3002813) / Eli Lilly
Clinical, FDA event: Only one of these Rx is going to come up for FDA approval next year #Donanemab. Unless of course you can convince the FDA that these ladostigil induced changes are “reasonably likely” to result in clinical benefit! (Twitter) - Oct 1, 2022
- || ladostigil hemitartrate (TV-3326) / Avraham, donepezil / Generic mfg.
Right, are you going to 'buy' ladostigil as volumes are going in the 'right' direction and 'sell' donepezil? (What donepezil study is this, Dubois?) (Twitter) - Oct 1, 2022
- |||| ladostigil hemitartrate (TV-3326) / Avraham, donanemab (LY3002813) / Eli Lilly
I see your ladostigil and raise you a #donanemab. Look at the decline in brain volume and ventricular expansion. I am only a neurologist but don’t think that can be a good thing in a progressive neurodegenerative disease. (Twitter) - Oct 1, 2022
- |||| ladostigil hemitartrate (TV-3326) / Avraham
Clinical: Want to help with Series B $$$ for this neuroprotective drug? Not much clinically but look at those brain volumes! Knocks your socks off, no? Schneider LS, Geffen Y, Rabinowitz J, Thomas RG, Schmidt R, Ropele S, Weinstock M: Low-dose ladostigil for MCI Neurology 2019, 93:e1474 (Twitter) - Oct 1, 2022
- | ladostigil hemitartrate (TV-3326) / Avraham
Journal: Ladostigil Attenuates Induced Oxidative Stress in Human Neuroblast-like SH-SY5Y Cells. (Pubmed Central) - Sep 29, 2021
We postulate that ladostigil alleviated cell damage induced by oxidation. Therefore, under conditions of chronic stress that are observed in the aging brain, ladostigil may block oxidative stress processes and consequently reduce neurotoxicity.
- | donepezil / Generic mfg., rasagiline / Generic mfg.
Journal: First Synthesis of Racemic Trans Propargylamino-Donepezil, a Pleiotrope Agent Able to Both Inhibit AChE and MAO-B, with Potential Interest against Alzheimer's Disease. (Pubmed Central) - Sep 12, 2021
Considering these results, we wanted to take benefit of the structural analogy lying in donepezil (DPZ) and rasagiline, two indane derivatives marketed as AChE and MAO-B inhibitors, respectively, and to propose the synthesis and the preliminary in vitro biological characterization of a structural compromise between these two compounds, we called propargylaminodonepezil (PADPZ). The synthesis of racemic trans PADPZ was achieved and its biological evaluation established its inhibitory activities towards both (h)AChE (IC = 0.4 µM) and (h)MAO-B (IC = 6.4 µM).
- | ladostigil hemitartrate (TV-3326) / Avraham
Preclinical, Journal: Effect of ladostigil treatment of aging rats on gene expression in four brain areas associated with regulation of memory. (Pubmed Central) - Aug 14, 2021
Ladostigil also decreased the expression of axonal growth inhibitors and those impairing mitochondrial function. Together, these actions could explain the protection by ladostigil against age-related memory decline.
- || 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.
- || ladostigil hemitartrate (TV-3326) / Avraham
Review, Journal: TV 3326 for Alzheimer's dementia: a novel multimodal ChE and MAO inhibitors to mitigate Alzheimer's-like neuropathology. (Pubmed Central) - Apr 14, 2021
It has also been confirmed that TV 3326 contains neuroprotective and anti-apoptotic properties. Therefore, this distinctive combined inhibition of ChE and MAO along with its neuroprotective property makes TV 3326 a useful drug in the treatment of AD.
- | rasagiline / Generic mfg.
Journal: Exploring the Multifunctional Neuroprotective Promise of Rasagiline Derivatives for Multi-Dysfunctional Alzheimer's Disease. (Pubmed Central) - Mar 20, 2021
It has been revealed that both the compounds possess anti-AD effects and therefore, the clinical development is directed to the treatment of this type of neurodegenerative diseases (NDs). In this article, we have reviewed the neuroprotective molecular mechanisms and multimodal actions of TV-3326 and M-30.
- || memantine / Generic mfg.
Review, Journal, IO biomarker: Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy. (Pubmed Central) - Jan 29, 2021
Apart from acting as inhibitors of both cholinesterases and monoamine oxidases, they show improvement of cognitive impairment, antioxidant activities, enhancement of iron-chelating activities, protect against tau hyperphosphorylation, block metal-associated oxidative stress, regulate APP and Aβ expression processing by the non-amyloidogenic α-secretase pathway, suppress mitochondrial permeability transition pore opening, and coordinate protein kinase C signaling and Bcl-2 family proteins. Other hybrid propargylamine derivatives are also reported.
- | rasagiline / Generic mfg.
Journal: Rasagiline derivatives combined with histamine H receptor properties. (Pubmed Central) - Sep 23, 2020
Surprisingly, the 5-substituted 3-piperidinopropyloxy rasagiline derivative 1 was more potent on both targets than its 6-substituted isomer. It showed nanomolar affinities at the desired targets (MAO B IC = 256 nM; hHR K = 2.6 nM) with a high preference over monoamine oxidase A (MAO A) and negligible affinity at histamine H, H, dopamine D, D receptors or acetyl-/butyrylcholinesterases.
- | ladostigil hemitartrate (TV-3326) / Avraham
Journal: Age-Induced Spatial Memory Deficits in Rats Are Correlated with Specific Brain Region Alterations in Microglial Morphology and Gene Expression. (Pubmed Central) - Sep 13, 2020
The data show brain region-specific relations induced by age in spatial learning, microglial morphology and associated genes and their response to ladostigil treatment. Graphical Abstract.
- || ladostigil hemitartrate (TV-3326) / Avraham
Biomarker, Clinical, P2 data, Journal: Low-dose ladostigil for mild cognitive impairment: A phase 2 placebo-controlled clinical trial. (Pubmed Central) - Feb 15, 2020
P2
Ladostigil was safe and well tolerated but did not delay progression to dementia. Its association with reduced brain and hippocampus volume loss suggests a potential effect on atrophy.
- || ladostigil hemitartrate (TV-3326) / Avraham
Trial primary completion date: A 3 Year Study to Evaluate the Safety and Efficacy of Low Dose Ladostigil in Patients With Mild Cognitive Impairment (clinicaltrials.gov) - Jun 15, 2017
P2, N=210, Completed, Sponsor: Avraham Pharmaceuticals Ltd
Its association with reduced brain and hippocampus volume loss suggests a potential effect on atrophy. Trial primary completion date: Dec 2015 --> Jul 2016
- ||| ladostigil hemitartrate (TV-3326) / Avraham
Enrollment closed: A 3 Year Study to Evaluate the Safety and Efficacy of Low Dose Ladostigil in Patients With Mild Cognitive Impairment (clinicaltrials.gov) - Jul 21, 2013
P2, N=200, Active, not recruiting, Sponsor: Avraham Pharmaceuticals Ltd
Trial primary completion date: Dec 2015 --> Jul 2016 Recruiting --> Active, not recruiting
- |||| ladostigil hemitartrate (TV-3326) / Avraham
Trial completion: Safety and Efficacy Study of Ladostigil in Mild to Moderate Probable Alzheimer's Disease (clinicaltrials.gov) - Jul 21, 2013
P2, N=201, Completed, Sponsor: Avraham Pharmaceuticals Ltd
Recruiting --> Active, not recruiting Active, not recruiting --> Completed
- ||||| ladostigil hemitartrate (TV-3326) / Avraham
New P2 trial: A 3 Year Study to Evaluate the Safety and Efficacy of Low Dose Ladostigil in Patients With Mild Cognitive Impairment (clinicaltrials.gov) - Sep 5, 2011
P2, N=200, Active, not recruiting, Sponsor: Avraham Pharmaceuticals Ltd