- |||||||||| Review, Journal: Dual bronchodilation for the treatment of COPD - From bench to bedside. (Pubmed Central) - Jul 23, 2022
Consequently, several LAMA/LABA FDCs have been developed and approved for clinical use as treatments for patients with COPD. However, to date, there are unfortunately very few head-to-head studies comparing the safety and efficacy of different LAMA/LABA FDCs making it difficult to choose the most appropriate combination, although the use of meta-analyses has provided some information in this regard.
- |||||||||| Zolinza (vorinostat) / Merck (MSD)
Journal: Epigenetic restoration and activation of ERβ: an inspiring approach for treatment of triple-negative breast cancer. (Pubmed Central) - Jul 20, 2022
However, to date, there are unfortunately very few head-to-head studies comparing the safety and efficacy of different LAMA/LABA FDCs making it difficult to choose the most appropriate combination, although the use of meta-analyses has provided some information in this regard. The antiproliferative effect of ERβ could be retained when co-expressed with Erα using a powerful epigenetic combination of Decitabine and vorinostat with DPN.
- |||||||||| erteberel (LY500307) / Eli Lilly
Journal, Cancer stem cells, PARP Biomarker: Therapeutic Targeting of Ovarian Cancer Stem Cells Using Estrogen Receptor Beta Agonist. (Pubmed Central) - Jul 17, 2022
Importantly, treatment of LY500307 significantly attenuated the tumor-initiating capacity of OCSCs in orthotopic OCa murine xenograft models. Our results demonstrate that ERβ agonist LY500307 is highly efficacious in reducing the stemness and promoting apoptosis of OCSCs and shows significant promise as a novel therapeutic agent in treating OCa.
- |||||||||| epinephrine / Generic mfg.
RGS4 Is Essential For The Sympathetic Regulation of The Short-chain Fatty Acid Receptor FFAR3 In The Heart () - Jul 16, 2022 - Abstract #ENDO2022ENDO_2129;
Also, catecholamines, like epinephrine, can induce RGS4 to block these actions by FFAR3 in the heart. Therefore, drugs that can stimulate RGS4 actions in the heart, including beta-adrenergic agonists like isoproterenol and the anti-asthmatic drug albuterol, may protect against shot chain, saturated fatty acid-promoted myocardial inflammation.
- |||||||||| Retrospective data, Journal, Real-world evidence: Effects of Asthma Medication Type on Asthma Exacerbation in a Real-World Setting. (Pubmed Central) - Jul 1, 2022
Increased awareness among policymakers and healthcare practitioners is needed to ensure implementation of current, evidence-based, treatment recommendations to optimize asthma management in this region. In the real world, asthma medications affect asthma exacerbation variably according to the medication type.
- |||||||||| Trelegy Ellipta (fluticasone furoate/umeclidinium bromide/vilanterol) / GSK, Innoviva, Theravance Biopharma
Observational data, Journal: Characteristics of New Users of Single- and Multiple-Inhaler Triple Therapy for COPD in Primary Care in England. (Pubmed Central) - Jul 1, 2022
In total, 3536 patients initiated fluticasone furoate, umeclidinium, and vilanterol (FF/UMEC/VI) SITT for the first time: 65% had a Medical Research Council (MRC) dyspnea score ≥3, 45% had forced expiratory volume in 1 second (FEV)% predicted <50%, and 64% had a moderate or severe exacerbation in the previous 12 months...First-time triple therapy was frequently initiated in patients with COPD inadequately controlled on maintenance therapy. General practitioners in England generally identify appropriate patients who require initiation of triple therapy.
- |||||||||| Retrospective data, Journal: Evaluation of a pediatric asthma high-risk scoring algorithm. (Pubmed Central) - Jun 30, 2022
Texas Children's Health Plan asthma risk score stratifies risk of asthma hospitalization and ED visits for Medicaid-insured children. The risk score performs better for children aged 3 to less than 18 years than for those aged 1 to less than 3 years.
- |||||||||| Journal: Stereoisomers in sports drug testing: Analytical strategies and applications. (Pubmed Central) - Jun 22, 2022
The immense variability of the substance classes represents however a major challenge, especially because both 'classic' doping agents belonging to the category of lower molecular mass molecules (e.g. stimulants, β-agonists, betablockers, corticoids, etc.) as well as larger molecules from the category of peptides and proteins necessitate consideration. In the present (mini)review, the current status of analytical techniques in the field of doping control analysis of stereoisomers is highlighted and critically reviewed.
- |||||||||| Myrbetriq (mirabegron) / Astellas
Preclinical, Journal: Mirabegron attenuates porcine ureteral contractility via α1-adrenoceptor antagonism. (Pubmed Central) - Jun 19, 2022
The present results show that mirabegron suppresses ureteral contractile responses in the porcine ureter via α-adrenoceptor antagonism, since their effects were not present when the tissues were contracted with 5-HT. Furthermore, the inhibitory effects by mirabegron were not affected by β-adrenoceptor antagonists.
- |||||||||| IRS Mediated Recruitment Of PI3Kgamma By Insulin Inhibits Beta-adrenergic Receptor Function (Salon B, Lower Level) - Jun 18, 2022 - Abstract #BCVS2022BCVS_90;
Consistently, CRISPR ablation of I2PP2A relieves this inhibition on PP2A leading to increased PP2A activity. This reduces accumulation of phosphorylated βARs despite the presence of PI3Kγ showing an underappreciated regulation of PP2A by insulin through non-canonical recruitment of PI3Kγ that impairs β2AR function.
- |||||||||| Journal: Clinical characteristics of irritant-induced occupational asthma. (Pubmed Central) - Jun 15, 2022
Six months after the OA diagnosis, a significant proportion of the patients with IIA remain symptomatic and the majority of these patients use asthma medications extensively suggesting uncontrolled asthma. The short-term outcomes of IIA appear poorer than that of sensitizer-induced OA.
- |||||||||| Journal: Estrogen receptor α activation modulates the gut microbiome and type 2 diabetes risk factors. (Pubmed Central) - Jun 15, 2022
As obesity increases the abundance of Firmicutes and decreases the abundance of Bacteroidetes, our study shows that ERα activation can restore the gut microbiome to non-obese abundances. This study further provides novel insights into ERα's role in hepatic fat metabolism via regulation of ACC, FAS, LPL, PPARα, and PPARγ.
- |||||||||| budesonide/salbutamol (PT027) / AstraZeneca, Avillion
Journal: Albuterol-Budesonide Fixed-Dose Combination Rescue Inhaler for Asthma. (Pubmed Central) - Jun 8, 2022
P3
The risk of severe asthma exacerbation was significantly lower with as-needed use of a fixed-dose combination of 180 μg of albuterol and 160 μg of budesonide than with as-needed use of albuterol alone among patients with uncontrolled moderate-to-severe asthma who were receiving a wide range of inhaled glucocorticoid-containing maintenance therapies. (Funded by Avillion; MANDALA ClinicalTrials.gov number, NCT03769090.).
- |||||||||| Observational data, Journal: Severe asthma treatment patterns: A multicenter observational study in the Gulf region. (Pubmed Central) - Jun 8, 2022
Despite recommended ICS/LABA therapy being prescribed to most patients for their severe disease, the majority experienced uncontrolled asthma and exhibited elevated BECs. These findings indicate the need for enhanced treatment strategies to improve and sustain asthma control in the Gulf region.
- |||||||||| Journal: Lipolysis defect in people with obesity who undergo metabolic surgery. (Pubmed Central) - Jun 8, 2022
Patients with obesity requiring metabolic surgery have impaired ability of catecholamines to stimulate lipolysis, which remains despite long-term normalization of body weight by RYGB. Furthermore, preoperative variations in the ability of catecholamines to activate lipolysis may predict the long-term reduction in body weight and fat mass.
- |||||||||| Clinical, Journal: Efficacy and safety of add-on tiotropium in the management of uncontrolled asthma: a patient case series. (Pubmed Central) - Jun 4, 2022
Furthermore, preoperative variations in the ability of catecholamines to activate lipolysis may predict the long-term reduction in body weight and fat mass. Hence, the results from these case reports highlight that tiotropium could be an effective and safe add-on treatment option for patients across a range of age groups with uncontrolled or fixed obstructive asthma receiving prior ICS or ICS + LABA and/or LTRA therapy.
- |||||||||| fluticasone / Generic mfg.
Journal, Real-world evidence: Tiotropium Add-On and Treatable Traits in Asthma-COPD Overlap: A Real-World Pilot Study. (Pubmed Central) - Jun 4, 2022
A 12-week open-label cross-over pilot study was conducted in patients with ACO to investigate the effect of tiotropium bromide (TIO) 5 µg/day add-on therapy to fluticasone propionate/formoterol fumarate (FP/FM) 500/20 µg/day compared with FP/FM 500/20 µg/day alone...FEV values after the TIO add-on therapy FP/FM period were significantly higher than those after the run-in period (p < 0.01). TIO add-on therapy to FP/FM in patients with ACO, considered difficult to treat because of the presence of both asthma and COPD, resulted in improvements in lung function parameters in this real-world pilot study, indicating the potential value of TIO add-on therapy as a "treatable traits" option for standard treatment for ACO.
- |||||||||| Clinical, Review, Journal: Combination fixed-dose β agonist and steroid inhaler as required for adults or children with mild asthma: a Cochrane systematic review. (Pubmed Central) - May 29, 2022
FABA/ICS as required is clinically effective in adults and adolescents with mild asthma and reduced exacerbations, hospital admissions or unscheduled healthcare visits and exposure to systemic corticosteroids and probably reduces adverse events compared with FABA as required alone. FABA/ICS as required is as effective as regular ICS and reduced asthma-related hospital admissions or unscheduled healthcare visits, and average exposure to ICS, and is unlikely associated with increased adverse events.
- |||||||||| Trelegy Ellipta (fluticasone furoate/umeclidinium bromide/vilanterol) / GSK, Innoviva, Theravance Biopharma, Anoro Ellipta (umeclidinium/vilanterol) / Innoviva, GSK, Veramyst (fluticasone furoate nasal spray) / GSK
Journal: A single inhaler triple therapy fluticasone furoate/umeclidinium/vilanterol for the treatment of COPD. (Pubmed Central) - May 29, 2022
Only direct head-to-head comparisons will be able to establish whether FF/UMEC/VI may be preferable to the other SITTs approved for COPD due to its pharmacokinetic and pharmacodynamic characteristics and especially the fact that it is the only one that can be taken once-daily. In addition, there is a need for further studies, especially in the real world, to optimize the positioning of FF/UMEC/VI in the treatment of COPD, also considering the availability of FF/VI and UMEC/VI and the need for better differentiation between the three treatments.
- |||||||||| Journal: Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. (Pubmed Central) - May 29, 2022
16g also showed excellent lipid metabolism, safety, metabolic stability, and pharmacokinetic properties. Collectively, 16g is a well-characterized selective and mutation-sensitive TRβ agonist for further investigating its function in treating dyslipidemia, nonalcoholic steatohepatitis (NASH), and resistance to thyroid hormone (RTH).
- |||||||||| Review, Journal: Assessing adherence to inhaled therapies in asthma and the emergence of electronic monitoring devices. (Pubmed Central) - May 26, 2022
This information assists clinicians in distinguishing difficult-to-control from severe asthma. Although additional evidence is required to assess the impact of EMDs on clinical outcome measures such as exacerbation rate, the introduction of EMDs into the asthma armoury is a significant step forward in asthma care with the potential to improve asthma-related outcomes.
- |||||||||| Review, Journal: Assessing the Role of High-Dose β-Agonists Use in Triggering Takotsubo Syndrome During Asthma Exacerbation. (Pubmed Central) - May 25, 2022
We encountered 45 articles, of which 21 were case reports that were reviewed separately for age, sex, diagnosis, recurrence, electrocardiogram findings, echo results, and mortality.Based on our review, it appears as if the use of high doses of β-agonists may predispose patients with asthma to cardiac events that might be preventable if physicians are aware of this association and become more judicious in their use of β-agonists. A standardized identification and treatment protocol would certainly be most helpful.
- |||||||||| Review, Journal: The new era of add-on asthma treatments: where do we stand? (Pubmed Central) - May 22, 2022
In the future, both biologics and small molecules will continue to play key roles in the individualized treatment of severe asthma. However, as targeted therapies, their application will continue to be focused on patients with certain phenotypes who meet the specific criteria for use as identified in pivotal clinical trials.
- |||||||||| Clinical, Journal: Evaluation of choroidal thickness in children with acute asthma attack by optical coherence tomography. (Pubmed Central) - May 19, 2022
The mean choroidal thickness of the control group was 303.0 ± 7.3 μm and compared to the pre-treatment and post-treatment values, it was more similar to the post-treatment values, although there was no statistically difference. In our study, it was shown that choroidal thickness was significantly reduced in children with asthma who received attack treatment with β agonists, and it was similar to the control group after the treatment.
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