&lt;p&gt;Pitolisant to Treat Excessive Daytime Sleepiness and Cataplexy in Adults with Narcolepsy: Rationale and Clinical Utility&lt;/p&gt;

Guevarra, Jay T; Hiensch, Robert; Varga, Andrew W.; Rapoport, David M.

doi:10.2147/nss.s264140

Cited by 15 publications

(10 citation statements)

References 47 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Thus, the H 3 receptor blocking ligands are promising agents for the treatment of CNS disorders, obesity, sleep disorders, Alzheimer's disease, and schizophrenia 43–47 Pitolisant. is a first‐in‐class FDA‐approved agent for the treatment of daytime sleepiness in adults with narcolepsy by acting as an antagonist/inverse agonist at the H 3 receptor 34,35,48 …”

Section: Histamine Receptorsmentioning

confidence: 99%

Histamine in cancer immunology and immunotherapy. Current status and new perspectives

Sarasola

Delgado

Nicoud

et al. 2021

Pharmacology Res & Perspec

View full text Add to dashboard Cite

Cancer is the second leading cause of death globally and its incidence and mortality are rapidly increasing worldwide. The dynamic interaction of immune cells and tumor cells determines the clinical outcome of cancer. Immunotherapy comes to the forefront of cancer treatments, resulting in impressive and durable responses but only in a fraction of patients. Thus, understanding the characteristics and profiles of immune cells in the tumor microenvironment (TME) is a necessary step to move forward in the design of new immunomodulatory strategies that can boost the immune system to fight cancer. Histamine produces a complex and fine‐tuned regulation of the phenotype and functions of the different immune cells, participating in multiple regulatory responses of the innate and adaptive immunity. Considering the important actions of histamine‐producing immune cells in the TME, in this review we first address the most important immunomodulatory roles of histamine and histamine receptors in the context of cancer development and progression. In addition, this review highlights the current progress and foundational developments in the field of cancer immunotherapy in combination with histamine and pharmacological compounds targeting histamine receptors.

show abstract

Section: Histamine Receptorsmentioning

confidence: 99%

Histamine in cancer immunology and immunotherapy. Current status and new perspectives

Sarasola

Delgado

Nicoud

et al. 2021

Pharmacology Res & Perspec

View full text Add to dashboard Cite

show abstract

“…5 Treatment of narcolepsy involves pharmacologic and non-pharmacologic interventions, with the primary aim of increasing wakefulness and reducing cataplexy attacks. 6 Non-pharmacologic interventions include scheduled napping, proper sleep hygiene, and avoidance of drugs that induce daytime sleepiness. 6 Wake-promoting agents, such as Modafinil and Armodafinil, are first-line pharmacotherapies for EDS in narcolepsy.…”

Section: Introductionmentioning

confidence: 99%

“…6 Non-pharmacologic interventions include scheduled napping, proper sleep hygiene, and avoidance of drugs that induce daytime sleepiness. 6 Wake-promoting agents, such as Modafinil and Armodafinil, are first-line pharmacotherapies for EDS in narcolepsy. 6 The exact mechanism of action in promoting wakefulness is elusive, but there appears to be an increase in dopaminergic signaling via blocking dopamine reuptake.…”

Section: Introductionmentioning

confidence: 99%

“…6 Wake-promoting agents, such as Modafinil and Armodafinil, are first-line pharmacotherapies for EDS in narcolepsy. 6 The exact mechanism of action in promoting wakefulness is elusive, but there appears to be an increase in dopaminergic signaling via blocking dopamine reuptake. 6 Solriamfetol, norepinephrine, and dopamine reuptake inhibitor are indicated to improve wakefulness in EDS among individuals with narcolepsy or OSA.…”

Section: Introductionmentioning

confidence: 99%

“…6 The exact mechanism of action in promoting wakefulness is elusive, but there appears to be an increase in dopaminergic signaling via blocking dopamine reuptake. 6 Solriamfetol, norepinephrine, and dopamine reuptake inhibitor are indicated to improve wakefulness in EDS among individuals with narcolepsy or OSA. 7 Pitolisant is a novel noncontrolled drug approved by the Food and Drug Administration (FDA) in August 2019 to treat EDS in adults with narcolepsy.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

pitolisant, a novel histamine-3 receptor competitive antagonist, and inverse agonist, in the treatment of excessive daytime sleepiness in adult patients with narcolepsy

Sarfraz

Okuampa

Hansen

et al. 2022

Health Psychology Research

View full text Add to dashboard Cite

Narcolepsy is a debilitating sleep disorder that presents with excessive daytime sleepiness (EDS) and cataplexy, which is a sudden paralysis of muscle tone triggered by strong emotions such as laughing. It is also associated with many other disorders, including psychiatric disorders, neurologic illnesses, and medication side effects. Common causes of delayed and incorrect diagnoses of these conditions include lack of physician familiarity with narcolepsy symptoms and comorbidities which mask narcolepsy signs and symptoms. Current pharmacologic therapies include Modafinil and Armodafinil for EDS and sodium oxybate for cataplexy. This review discusses the epidemiology, pathophysiology, risk factors, presentation, treatment of narcolepsy, and the role of a novel drug, Pitolisant, in the treatment of EDS in adults with narcolepsy. Pitolisant is a histamine-3 receptor (H3R), competitive antagonist, and inverse agonist, acting through the histamine system to regulate wakefulness. It is a novel drug approved in August 2019 by the FDA, is not classified as a controlled substance, and is approved for use in Europe and the United States to treat EDS and cataplexy in narcolepsy. Recent phase II and III trials have shown that Pitolisant helps reduce the ESS score and cataplexy. In summary, based on comparative studies, recent evidence has shown that Pitolisant is non-inferior to Modafinil in the treatment of EDS but superior to Modafinil in reducing cataplexy.

show abstract

Histaminergic neurotransmission in aging and Alzheimer's disease: A review of therapeutic opportunities and gaps

Satpati

Neylan

Grinberg

2023

A&D Transl Res & Clin Interv

View full text Add to dashboard Cite

Introduction Alzheimer's disease (AD) is a progressive neurodegenerative disorderfeaturing a brain accumulation of extracellular β‐amyloidplaques (Aβ) and intracellular neurofibrillary tautangles (NFTs). Although cognitive decline is a disease‐defining symptom of AD, sleep dysfunction, a common symptom often preceding cognitive decline, hasrecently gained more attention as a core AD symptom. Polysomnography and othersleep measures show sleep fragmentation with shortening of N3 sleep togetherwith excessive daytime sleepiness (EDS) and sundowning as the main findings in AD patients. The latter reflects dysfunction of the wake‐promoting neurons (WPNs), including histaminergic neurons (HAN) located in thetuberomammillary nucleus (TMN) of the posterior hypothalamus, which projectunmyelinated axons to various parts of the brain. Histamine's role in cognitionand arousal is broadly recognized. Selective targeting of histaminergic subtype‐3 and 4 receptors show therapeutic potential in rodent models of AD andaging. Method Based on PubMed, Scopus, and google scholar databases search, this review summarizes the current knowledge on the histaminergic system in AD and aging, its therapeutic potential in AD, and highlight areas where moreresearch is needed. Results Animal studies have demonstrated that pharmacological manipulation of histaminergic receptors or histamine supplementation improves cognition in AD models. However, measurements of HA or HA metabolite levels in the human brainand CSF present contradictory reports due to either lack of power or controls for known confounders. Discussion Systemic studies including broad age, sex, neuropathological diagnosis, and disease stage are warranted to fill the gap in our current understanding of the histaminergic neurotransmitter/neuromodulator system in humans, especially age‐related changes, and therapeuticpotential of histamine in AD‐related dysfunction.

show abstract

<p>Pitolisant to Treat Excessive Daytime Sleepiness and Cataplexy in Adults with Narcolepsy: Rationale and Clinical Utility</p>

Cited by 15 publications

References 47 publications

Histamine in cancer immunology and immunotherapy. Current status and new perspectives

Histamine in cancer immunology and immunotherapy. Current status and new perspectives

pitolisant, a novel histamine-3 receptor competitive antagonist, and inverse agonist, in the treatment of excessive daytime sleepiness in adult patients with narcolepsy

Histaminergic neurotransmission in aging and Alzheimer's disease: A review of therapeutic opportunities and gaps

Contact Info

Product

Resources

About