Characterization of chronic cough patients participating in a phase 2b clinical trial of gefapixant, a P2X3 receptor antagonist
Conclusions: Large proportions of chronic cough patients in this trial were diagnosed with GERD, asthma, or allergic rhinitis. Despite receiving treatment for these conditions, chronic cough for these subjects had persisted for over a decade. (Source: European Respiratory Journal)
Source: European Respiratory Journal - November 20, 2019 Category: Respiratory Medicine Authors: McGarvey, L., Smith, J., Birring, S., Morice, A., Sher, M., Wu, W.-C., Muccino, D. Tags: Clinical Problems Source Type: research
Determination of benzonatate and its metabolite in human plasma by HPLC–MS/MS: A preliminary pharmacokinetic study in healthy Chinese volunteers after oral administration of benzonatate soft capsule
In this study, two sensitive high-performance liquid chromatography-tandem mass spectrometry (HPLC–MS/MS) methods were developed and fully validated for the determination of the original 4-(butylamino)benzoic acid (method B) and total 4-(butylamino)benzoic acid (containing the original 4-(butylamino)benzoic acid and 4-(butylamino)benzoic acid converted from benzonatate after collection, method A). For both methods, one-step protein precipitation by methanol was performed to extract analytes from the plasma samples. Chromatographic separation was done on an InfinityLab Poroshell 120 Phenyl Hexyl column (2.1 mm × 50...
Source: Journal of Pharmaceutical and Biomedical Analysis - May 17, 2019 Category: Drugs & Pharmacology Source Type: research
Genotoxicity assessment of the novel antitussive agent Benzonatate and its major metabolite
In conclusion, Benzonatate and its major metabolite BBA were not mutagenic and did not cause numerical or structural chromosome alterations. While the MPG metabolite was not tested, studies on structural analogues indicated it was also unlikely to be genotoxic. This was supported by oral rodent carcinogenicity assays showing no increase in malignancies. (Source: Mutation Research Genetic Toxicology and Environmental Mutagenesis)
Source: Mutation Research Genetic Toxicology and Environmental Mutagenesis - April 14, 2018 Category: Genetics & Stem Cells Source Type: research
In silico identification of potent small molecule inhibitors targeting epidermal growth factor receptor 1
Conclusions: Our findings suggested that the small molecule ZINC03830276 (Benzonatate) could be a promising EGFR inhibitor candidate and may also provide new ideas for designing more potent EGFR inhibitors for the future study. (Source: Journal of Cancer Research and Therapeutics)
Source: Journal of Cancer Research and Therapeutics - March 8, 2018 Category: Cancer & Oncology Authors: Zheng Shi Jie Chen Xiaolan Guo Lijia Cheng Xiaoheng Guo Tian Yu Source Type: research
Benzonatate Inhibition of Voltage-Gated Sodium Currents.
Abstract
Benzonatate was FDA-approved in 1958 as an antitussive. Its mechanism of action is thought to be anesthesia of vagal sensory nerve fibers that mediate cough. Vagal sensory neurons highly express the Nav1.7 subtype of voltage-gated sodium channels, and inhibition of this channel inhibits the cough reflex. Local anesthetics inhibit voltage-gated sodium channels, but there are no reports of whether benzonatate affects these channels. Our hypothesis is that benzonatate inhibits Nav1.7 voltage-gated sodium channels. We used whole cell voltage clamp recording to test the effects of benzonatate on voltag...
Source: Neuropharmacology - September 16, 2015 Category: Drugs & Pharmacology Authors: Evans MS, Maglinger GB, Fletcher AM, Johnson SR Tags: Neuropharmacology Source Type: research
