Patent Highlights August–September 2021

Mucke, Hermann Am

doi:10.4155/ppa-2021-0025

Pharm. Pat. Anal.

2022

DOI: 10.4155/ppa-2021-0025

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Patent Highlights August–September 2021

Hermann Am Mucke¹

Abstract: A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.

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2024

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Cited by 2 publications

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Various pharmacological agents in the pipeline against intractable epilepsy

Waris,

Asim,

Ullah

et al. 2024

Archiv der Pharmazie

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Epilepsy is a noncommunicable chronic neurological disorder affecting people of all ages, with the highest prevalence in low and middle‐income countries. Despite the pharmacological armamentarium, the plethora of drugs in the market, and other treatment options, 30%–35% of individuals still show resistance to the current medication, termed intractable epilepsy/drug resistance epilepsy, which contributes to 50% of the mortalities due to epilepsy. Therefore, the development of new drugs and agents is needed to manage this devastating epilepsy. We reviewed the pipeline of drugs in “ClinicalTrials. gov,” which is the federal registry of clinical trials to identify drugs and other treatment options in various phases against intractable epilepsy. A total of 31 clinical trials were found regarding intractable epilepsy. Among them, 48.4% (15) are about pharmacological agents, of which 26.6% are in Phase 1, 60% are in Phase 2, and 13.3% are in Phase 3. The mechanism of action or targets of the majority of these agents are different and are more diversified than those of the approved drugs. In this article, we summarized various pharmacological agents in clinical trials, their backgrounds, targets, and mechanisms of action for the treatment of intractable epilepsy. Treatment options other than pharmacological ones, such as devices for brain stimulation, ketogenic diets, gene therapy, and others, are also summarized.

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Various pharmacological agents in the pipeline against intractable epilepsy

Waris,

Asim,

Ullah

et al. 2024

Archiv der Pharmazie

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Exploring the role of AMPA receptor auxiliary proteins in synaptic functions and diseases

Qneibi,

Bdir,

Bdair

et al. 2024

The FEBS Journal

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α‐Amino‐3‐hydroxy‐5‐methyl‐4‐isoxazolepropionic acid (AMPA) ionotropic glutamate receptors (AMPARs) mediate rapid excitatory synaptic transmission in the mammalian brain, primarily driven by the neurotransmitter glutamate. The modulation of AMPAR activity, particularly calcium‐permeable AMPARs (CP‐AMPARs), is crucially influenced by various auxiliary subunits. These subunits are integral membrane proteins that bind to the receptor's core and modify its functional properties, including ion channel kinetics and receptor trafficking. This review comprehensively catalogs all known AMPAR auxiliary proteins, providing vital insights into the biochemical mechanisms governing synaptic modulation and the specific impact of CP‐AMPARs compared to their calcium‐impermeable AMPA receptor (CI‐AMPARs). Understanding the complex interplay between AMPARs and their auxiliary subunits in different brain regions is essential for elucidating their roles in cognitive functions such as learning and memory. Importantly, alterations in these auxiliary proteins' expression, function or interactions have been implicated in various neurological disorders. Aberrant signaling through CP‐AMPARs, in particular, is associated with severe synaptic dysfunctions across neurodevelopmental, neurodegenerative and psychiatric conditions. Targeting the distinct properties of AMPAR‐auxiliary subunit complexes, especially those involving CP‐AMPARs, could disclose new therapeutic strategies, potentially allowing for more precise interventions in treating complex neuronal disorders.

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Patent Highlights August–September 2021

Abstract: A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.

Cited by 2 publications

References 47 publications

Various pharmacological agents in the pipeline against intractable epilepsy

Various pharmacological agents in the pipeline against intractable epilepsy

Exploring the role of AMPA receptor auxiliary proteins in synaptic functions and diseases

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