Long acting muscarinic antagonists for the treatment of chronic obstructive pulmonary disease: a review of current and developing drugs

Mastrodicasa, M; Droege, Christopher; Mulhall, Aaron M.; Ernst, Neil; Panos, Ralph J.; Zafar, Muhammad Ahsan

doi:10.1080/13543784.2017.1276167

Cited by 14 publications

(4 citation statements)

References 43 publications

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“…The efficacy and safety of LAMA monotherapies are well established in patients with moderate-to-severe COPD (Table 1) [1,13,14]. Clinical studies have shown that treatment with the LAMA, tiotropium (TIO), reduces the risk of exacerbations compared with no treatment or with LABAs [15,16].…”

Section: Lamasmentioning

confidence: 99%

An overview of glycopyrrolate/eFlow® CS in COPD

Kerwin

Ferguson²

2018

Expert Review of Respiratory Medicine

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COPD is highly prevalent in the US and globally, requiring new treatment strategies due to the high disease burden and increase in the aging population. Here, we profile the newly FDA-approved LONHALA MAGNAIR (glycopyrrolate [GLY]/eFlow® Closed System [CS]; 25 mcg twice daily), a nebulized long-acting muscarinic antagonist (LAMA) for the long-term maintenance treatment of COPD, including chronic bronchitis and/or emphysema. Areas covered: An overview of COPD and treatment landscape, focusing on GLY/eFlow CS, reviewing the published literature pertinent to the drug/device combination is reported. Expert commentary: GLY/eFlow CS consists of glycopyrrolate delivered via a novel electronic nebulizer and is the first nebulized LAMA to be approved by the FDA. GLY/eFlow CS has been studied in an extensive clinical development program, including phase II dose-ranging studies, two 12-week phase III studies demonstrating statistically significant and clinically important improvements in pulmonary function and patient-reported outcomes with a well-tolerated safety profile, and a 48-week phase III study highlighting the long-term safety of GLY/eFlow CS, along with long-term improvements in lung function and patient-reported outcomes. Additional studies are required to assess the impact of GLY/eFlow CS on COPD exacerbations, identify alternative uses of the eFlow CS nebulizer, and direct comparisons to other LAMAs.

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Section: Lamasmentioning

confidence: 99%

An overview of glycopyrrolate/eFlow® CS in COPD

Kerwin

Ferguson²

2018

Expert Review of Respiratory Medicine

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“…The GOLDEN phase 3 trials demonstrated clinically important efficacy outcomes and that nebulized GLY is well tolerated among patients with COPD. 36,37 Whereas the efficacy and safety of LAMA monotherapies are well established in patients with moderate to severe COPD, 39 the drug-device combination of GLY/eFlow CS provides a portable, patient-friendly, efficient, and rapid drug delivery system. 26,33,35-37…”

Section: Discussionmentioning

confidence: 99%

Glycopyrrolate/eFlow CS: The First Nebulized Long-Acting Muscarinic Antagonist Approved to Treat Chronic Obstructive Pulmonary Disease

Pleasants

2018

Ann Pharmacother

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“…COPD is an independent risk factor for NSCLC (Durham & Adcock, 2015; Takiguchi, Sekine, Iwasawa, Kurimoto, & Tatsumi, 2014). Muscarinic receptors play a crucial role in the pathophysiology and airway remodeling associated with COPD (Gosens, Zaagsma, Meurs, & Halayko, 2006;Mastrodicasa, et al, 2017). This led to extensive research on the status of muscarinic receptors in NSCLC Spindel, 2012Spindel, , 2016.…”

Section: Muscarinic Receptorsmentioning

confidence: 99%

Acetylcholine signaling system in progression of lung cancers

Friedman

Richbart

Merritt

et al. 2019

Pharmacology & Therapeutics

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The neurotransmitter acetylcholine (ACh) acts as an autocrine growth factor for human lung cancer. Several lines of evidence show that lung cancer cells express all of the proteins required for the uptake of choline (choline transporter 1, choline transporter-like proteins) synthesis of ACh (choline acetyltransferase, carnitine acetyltransferase), transport of ACh (vesicular acetylcholine transport, OCTs, OCTNs) and degradation of ACh (acetylcholinesterase, butyrylcholinesterase). The released ACh binds back to nicotinic (nAChRs) and muscarinic receptors on lung cancer cells to accelerate their proliferation, migration and invasion. Out of all components of the cholinergic pathway, the nAChR-signaling has been studied the most intensely. The reason for this trend is due to genome-wide data studies showing that nicotinic receptor subtypes are involved in lung cancer risk, the relationship between cigarette smoke and lung cancer risk as well as the rising popularity of electronic cigarettes considered by many as a "safe" alternative to smoking. There are a small number of review articles which review the contribution of the other cholinergic proteins in the pathophysiology of lung cancer. The primary objective of this review article is to discuss the function of the acetylcholine-signaling proteins in the progression of lung cancer. The investigation of the role of cholinergic network in lung cancer will pave the way to novel molecular targets and drugs in this lethal malignancy.

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Long acting muscarinic antagonists for the treatment of chronic obstructive pulmonary disease: a review of current and developing drugs

Cited by 14 publications

References 43 publications

An overview of glycopyrrolate/eFlow® CS in COPD

An overview of glycopyrrolate/eFlow® CS in COPD

Glycopyrrolate/eFlow CS: The First Nebulized Long-Acting Muscarinic Antagonist Approved to Treat Chronic Obstructive Pulmonary Disease

Acetylcholine signaling system in progression of lung cancers

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