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- | Trelegy Ellipta (fluticasone furoate/umeclidinium bromide/vilanterol) / GSK, Innoviva, Theravance Biopharma, Anoro Ellipta (umeclidinium/vilanterol) / Innoviva, GSK, Veramyst (fluticasone furoate nasal spray) / GSK
Journal: Baseline characteristics and ICS/LAMA/LABA response in asthma: analyses from the CAPTAIN study. (Pubmed Central) - May 9, 2024
P3
Unlike previous findings with type 2 biomarkers, lung function, bronchodilator reversibility, age and age at asthma onset do not appear to predict response to inhaled therapy.
- || Rezdiffra (resmetirom) / Madrigal Pharma
Review, Journal: Intrahepatic hypothyroidism in MASLD: Role of liver-specific thyromimetics including resmetirom. (Pubmed Central) - May 7, 2024
In euthyroid individuals with MASH, development of intrahepatic hypothyroidism results in further progression of the disease. In clinical trials, resmetirom treatment results in a significant improvement in steatosis, inflammation and fibrosis and is the first drug approved by the US Food and Drug Administration (FDA) for the treatment of noncirrhotic MASH with moderate to advanced fibrosis.
- HSK31679 / Haisco
Efficacy and safety of HSK31679, a thyroid hormone receptor ? agonist, for the treatment of asian nonalcoholic fatty liver disease: a multicenter randomized, double-blind, placebo-controlled, phase 2a trial () - Apr 29, 2024 - Abstract #EASLILC2024EASL_ILC_2703;
- THR-? Agonists and Other Disease-specific Therapies Poised to Change the Paradigm (Brown 3) - Apr 29, 2024 - Abstract #EASLILC2024EASL_ILC_2503;
In clinical trials, resmetirom treatment results in a significant improvement in steatosis, inflammation and fibrosis and is the first drug approved by the US Food and Drug Administration (FDA) for the treatment of noncirrhotic MASH with moderate to advanced fibrosis. Sponsored By AKH.
- AKH: Entering a New Era in Metabolic Associated Steatohepatitis: Examining the Clinical Implications of Emerging Disease-Specific Therapies (Brown 3) - Apr 29, 2024 - Abstract #EASLILC2024EASL_ILC_2501;
Sponsored By AKH. At the end of the program, learners will be able to:
- | Journal: Risks of maternal cardiopulmonary events associated with ritodrine for tocolysis: A national database linkage study in 1?831?564 pregnant women. (Pubmed Central) - Apr 26, 2024
Pregnant women receiving intravenous ritodrine therapy had higher cardiopulmonary risks and should be intensively monitored. While the relative risk associated with oral ritodrine is not pronounced, it should be used judiciously among pregnant women as well.
- || Review, Journal: Molecular insights into the potential effects of selective estrogen receptor ? agonists in Alzheimer's and Parkinson's diseases. (Pubmed Central) - Apr 19, 2024
Ultimately, we established a correlation between the importance of ER? activation and the process underlying ER?'s neuroprotective mechanisms in AD and PD.
- | Xolair (omalizumab) / Roche, Novartis
Biomarker, Journal: Biomarker Predictors of Clinical Efficacy of the Anti-IgE Biologic, Omalizumab, in Severe Asthma in Adults: Results of the SoMOSA Study. (Pubmed Central) - Apr 18, 2024
Conclusions This is the first discovery of omics biomarkers that predict improvement to a biologic for asthma. Their prospective validation and development for clinical use is justified.
- | Journal: Pectolinarigenin ameliorates osteoporosis via enhancing Wnt signaling cascade in PPAR?-dependent manner. (Pubmed Central) - Apr 13, 2024
Their prospective validation and development for clinical use is justified. PEC significantly promotes bone formation and reduces bone loss in both BMSCs and ovariectomy-induced osteoporosis mice via enhancing the Wnt signaling cascade in a PPAR?-dependent manner, providing a new alternative therapy for preventing estrogen deficiency-induced osteoporotic diseases.
- | budesonide/formoterol / Generic mfg.
Journal: START CARE: a protocol for a randomised controlled trial of step-wise budesonide-formoterol reliever-based treatment in children. (Pubmed Central) - Apr 9, 2024
This will be the first RCT to compare the efficacy and safety of a step-wise budesonide-formoterol reliever alone or MART regimen with conventional inhaled ICS or ICS-long-acting ?-agonist maintenance plus SABA reliever in children. The results will provide a much-needed evidence base for the treatment of asthma in children.
- | Rituxan (rituximab) / Roche
Journal: Generalized myasthenia gravis with acetylcholine receptor antibodies: A guidance for treatment. (Pubmed Central) - Apr 9, 2024
Most patients do reasonably well but there is room for further improvement. Novel treatments are promising, though subject to restricted access due to costs.
- ASC41 / Ascletis
ASC41, a selective THR? agonist significantly reduces liver fat and ALT in biopsy-confirmed MASH patients after 12-week treatment: an interim analysis of a 52-week serial liver biopsy study (Poster Area) - Apr 2, 2024 - Abstract #EASLILC2024EASL_ILC_2135;
- TERN-501 / Terns Pharma
Sex hormone binding globulin as an effective predictor of treatment response to TERN-501, a potent, highly selective thyroid hormone receptor ? agonist: post-hoc analyses from a 12-week phase 2a trial (Poster Area) - Apr 2, 2024 - Abstract #EASLILC2024EASL_ILC_2119;
- TERN-501 / Terns Pharma
TERN-501, a highly selective thyroid hormone receptor ? agonist, significantly improved MRI-PDFF, cT1, and liver volume in clinically relevant patient populations with presumed MASH: subgroup analyses from a 12-week phase 2a trial (Poster Area) - Apr 2, 2024 - Abstract #EASLILC2024EASL_ILC_2102;
- | Preclinical, Journal: Protecting the Brain: Novel Strategies for Preventing Breast Cancer Brain Metastases through Selective Estrogen Receptor ? Agonists and In Vitro Blood-Brain Barrier Models. (Pubmed Central) - Apr 1, 2024
Our results support ER? as a potential target for the prevention and treatment of BCBM and suggest that targeted vector-based approaches may be effective for future preventive and therapeutic implications.
- | Observational data, Journal, Adherence: Impact of treatment adherence and inhalation technique on asthma outcomes of pediatric patients: a longitudinal study. (Pubmed Central) - Mar 29, 2024
P=N/A
Our results confirm longitudinal associations at the within-person level of the two indicators of quality use of inhalers: for adherence to maintenance treatment with symptom control and HRQoL, and for the inhalation technique with HRQoL. Although treatment adherence was shown to be excellent, a third of the participants reported a suboptimal inhalation technique, highlighting the need for actions for improving asthma management of the pediatric population.
- | Journal: Impact of Asthma Medications During Pregnancy on Asthma Exacerbation, Maternal, and Neonatal Outcomes. (Pubmed Central) - Mar 26, 2024
Our study shows the importance of continuing asthma maintenance medication during pregnancy to improve outcomes. Future research should study the postpartum and long-term outcomes with asthma medication during pregnancy.
- | erteberel (LY500307) / Eli Lilly
Journal, PARP Biomarker: Activation of ER? hijacks the splicing machinery to trigger R-loop formation in triple-negative breast cancer. (Pubmed Central) - Mar 25, 2024
activation in TNBC, which provides rationale for ER? activation-based single or combined therapy for patients with TNBC.
- ||| Journal, Adverse events: A singleton pregnancy with placental chorioangioma and hydrops fetalis complicated with mirror syndrome and ritodrine-induced side effects: a case report. (Pubmed Central) - Mar 25, 2024
Our case demonstrates mirror syndrome induced by chorioangioma, which is rare, and ritodrine-induced side effects. The cessation of intravenous ritodrine and delivery are the best methods to treat maternal critical status due to fluid overload.
- | selonsertib (GS-4997) / Gilead, Rezdiffra (resmetirom) / Madrigal Pharma
Preclinical, Journal: Co-targeting ASK1 and THR? synergistically improves steatohepatitis and fibrosis in a MASH animal model. (Pubmed Central) - Mar 19, 2024
The cessation of intravenous ritodrine and delivery are the best methods to treat maternal critical status due to fluid overload. GS4997 and MGL3196, when used in combination, have been shown to have a comprehensive effect on MASH by synergistically regulating lipid, inflammation, and fibrosis-related gene expression through co-targeting ASK1 and THR?.
- | prinaberel (ERB-041) / Pfizer
Journal, IO biomarker, Tumor cell: Synergistic Anti-Cancer Effects of ERB-041 and Genistein through Estrogen Receptor Suppression-Mediated PI3K/AKT Pathway Downregulation in Canine Mammary Gland Tumor Cells. (Pubmed Central) - Mar 17, 2024
We also found a synergistic decrease in the expression of ER?, and the expression of proteins involved in the PI3K/AKT pathway, including p-PI3K, phosphatase and tensin homolog (PTEN), AKT, and mechanistic target of rapamycin (mTOR). In conclusion, ERB-041 and genistein exhibited a synergistic anticancer effect on CMTs, suggesting that cotreatment with ERB-041 and genistein is a promising treatment for CMTs.
- A Review of Asthma Treatment Plans for Single Maintenance and Reliever Therapy (SMART) in a Primary Care Clinic (Convention Center Exhibit Hall) - Mar 16, 2024 - Abstract #PAS2024PAS_2814;
In conclusion, ERB-041 and genistein exhibited a synergistic anticancer effect on CMTs, suggesting that cotreatment with ERB-041 and genistein is a promising treatment for CMTs. Thirty two SMART ATPs were provided to children who were on average 10 years (
- ||| Journal, Adverse events: Safety of Biological Therapies for Severe Asthma: An Analysis of Suspected Adverse Reactions Reported in the WHO Pharmacovigilance Database. (Pubmed Central) - Mar 15, 2024
The most frequently reported suspected ADRs of asthma biologics in VigiBase confirmed the presence of well-known adverse effects such as general disorders, injection-site reactions, nasopharyngitis, headache and hypersensitivity, while some others (e.g. asthma reactivation or therapeutic failure) could be ascribed to the indication of use. Moreover, the analysis of signals of disproportionate reporting suggests the presence of malignancies, effects on the cardiovascular system, alopecia and autoimmune conditions, requiring further assessment and investigation.
- | Journal: Layer-by-Layer Biopolymer Assembly for the In Situ Fabrication of AuNP Plasmonic Paper-A SERS Substrate for Food Adulteration Detection. (Pubmed Central) - Mar 11, 2024
Additionally, we demonstrate a simultaneous detection of ?-agonists, including ractopamine (RAC) and salbutamol (SAL), exhibiting the multiplexing capability and versatility of the plasmonic paper in food contaminant analysis. The development of this simple plasmonic paper through the LbL biopolymer assembly not only paves the way for novel SERS substrate fabrication but also broadens the application of SERS technology in food contaminant monitoring.
- Crosstalk of estrogen receptor ? with tumor microenvironment signaling explains tumor suppressor actions in TNBC (Section 12) - Mar 5, 2024 - Abstract #AACR2024AACR_8655;
The results of these studies help lay the groundwork for further research on the clinical potential of ER? especially in the realm of immunotherapy and treatment of TNBC.
- MMP14 and MKLN1 as colorectal cancer susceptibility genes and a drug repurposing candidate from genome-wide association study in South Korea (Section 33) - Mar 5, 2024 - Abstract #AACR2024AACR_8524;
agonist (GW0742) as a drug-repurposing candidate for the treatment of CRC. These findings can promote the understanding of CRC development and provide a novel therapeutic candidate for CRC patients in the future.
- | Journal: Effects of protein concentration and beta-adrenergic agonists on ruminal bacterial communities in finishing beef heifers. (Pubmed Central) - Mar 4, 2024
These results suggest possible effects on microbial communities with different concentrations of protein but limited impact with RAC. However, both may potentially act synergistically to improve performance in finishing beef cattle.
- | Journal: Identification of estrogen receptor agonists among hydroxylated polychlorinated biphenyls using classification-based quantitative structure-activity relationship models. (Pubmed Central) - Mar 4, 2024
However, both may potentially act synergistically to improve performance in finishing beef cattle. Predictions made by models I and II correctly classified 84.0
- | Journal: Muscle-building supplement ?-hydroxy ?-methylbutyrate stimulates the maturation of oligodendroglial progenitor cells to oligodendrocytes. (Pubmed Central) - Feb 29, 2024
These results suggest that HMB stimulates the maturation of OPCs via PPAR? and that HMB may have therapeutic prospects in remyelination.
- | Journal: BitterDB database analysis plus cell stiffness screening identify flufenamic acid as the most potent TAS2R14-based relaxant of airway smooth muscle cells for therapeutic bronchodilation. (Pubmed Central) - Feb 27, 2024
FFA also attenuated lipopolysaccharide-induced inflammatory response in cultured ASMCs. FFA as a potent TAS2R14 agonist to relax ASMCs while suppressing cytokine release might be a favorite drug agent for further development of TAS2R-based novel dual functional medication for bronchodilation and anti-inflammation in asthma therapy.
- | Journal: Phosphorylation of RyR2 simultaneously expands the dyad and rearranges the tetramers. (Pubmed Central) - Feb 22, 2024
Lastly, the correlation of structural with functional changes suggests that tetramer-tetramer contacts play an important functional role. We thus conclude that both the size of the dyad and the arrangement of the tetramers are linked to the state of the channel tetramer and can be dynamically altered by a ?-adrenergic receptor agonist.
- | Trelegy Ellipta (fluticasone furoate/umeclidinium bromide/vilanterol) / GSK, Innoviva, Theravance Biopharma
Journal: Outcomes of Patients with COPD Treated with ICS/LABA Before and After Initiation of Single-Inhaler Triple Therapy with Fluticasone Furoate/Umeclidinium/Vilanterol (FF/UMEC/VI). (Pubmed Central) - Feb 22, 2024
We thus conclude that both the size of the dyad and the arrangement of the tetramers are linked to the state of the channel tetramer and can be dynamically altered by a ?-adrenergic receptor agonist. Patients with COPD treated with ICS/LABA during baseline, including patients specifically treated with BUD/FORM and those with a history of ??1 exacerbation, had fewer COPD exacerbations and lower COPD-related HCRU after initiating FF/UMEC/VI.
- | Journal: Risk assessment in patients with symptomatic and asymptomatic pre-excitation. (Pubmed Central) - Feb 20, 2024
P=N/A
Sudden loss of pre-excitation during EST has a low NPV in excluding high-risk APs. The EPS with the use of isoproterenol should be considered to accurately assess the risk of patients with pre-excitation regardless of symptoms (ClinicalTrials.gov Identifier: NCT03301935).
- Cholesterol Accumulation in Alveolar Macrophages Drives Pulmonary Fibrosis (San Diego Convention Center, Room 30C-E (Upper Level)) - Feb 20, 2024 - Abstract #ATS2024ATS_5531;
Foam cell formation is a result of increased AT2 cell secretion and reduced recycling of cholesterol. Elimination of cholesterol in macrophages through improved macrophage efflux pathways and AT2 recycling is a promising strategy for therapeutic lung fibrosis.
- treprostinil / Generic mfg.
Treprostinil Inhibits Human Lung Fibroblast Matrix Production Via the IP Receptor Independently of cAMP (San Diego Convention Center, Area E (Hall A-B2, Ground Level)) - Feb 20, 2024 - Abstract #ATS2024ATS_2035;
Recent clinical trials show that inhaled Treprostinil (Tre), a stable analogue of prostacyclin, mitigated the decline of pulmonary function in patients with IPF. These findings suggest the antifibrotic effects of Treprostinil are mediated through the IP receptor in a cAMP independent manner since both Isoproterenol and PGE2 induce more cAMPi but have less effect on extracellular matrix production as measure by COL1A1 and PAI-1.
- | tetracycline / Generic mfg.
Journal: Comparison of filter membranes in the analysis of 183 veterinary and other drugs by liquid chromatography-tandem mass spectrometry. (Pubmed Central) - Feb 19, 2024
Drug classes represented among the analytes included ?-agonists, ?-lactams, anthelmintics, macrolides, tetracyclines, sulfonamides, tranquilizers, (fluoro)quinolones, anti-inflammatories, nitroimidazoles, coccidiostats, phenicols, and others...In testing by flow-injection analysis, all of the membrane filters were also observed to leach interfering components. Ultimately, filtration was avoided altogether in the final sample preparation approach known as the quick, easy, cheap, effective, rugged, safe, efficient, and robust (QuEChERSER) mega-method, and ultracentrifugation was chosen as an alternative.
- | Journal: The Association Between Short-Acting ?-Agonist Over-Prescription, and Patient-Reported Acquisition and Use on Asthma Control and Exacerbations: Data from Australia. (Pubmed Central) - Feb 4, 2024
Both self-reported SABA overuse and zero SABA prescriptions were associated with poor asthma outcomes. The disconnect between prescribing authorisation, OTC availability and actual use, make it difficult for clinicians to quantify SABA use.
- | fluticasone propionate/salmeterol xinafoate inhalation powder / Generic mfg.
Journal, HEOR: Comparative effectiveness and safety of inhaled corticosteroid plus long-acting ?-agonist fixed-dose combinations vs. long-acting muscarinic antagonist in bronchiectasis. (Pubmed Central) - Jan 31, 2024
Beclomethasone/formoterol (BEC/FOR) or budesonide/formoterol (BUD/FOR) led to a lower risk of acute exacerbation compared to fluticasone/salmeterol (FLU/SAL) (BEC/FOR HR 0.59, 95% CI 0.43-0.81; BUD/FOR HR 0.68, 95% CI 0.50-0.93)...Our findings provide important evidence on the effectiveness and safety of ICS/LABA FDC compared with LAMA for bronchiectasis. BEC/FOR and BUD/FOR were associated with better outcomes than FLU/SAL.
- | Retrospective data, Journal: Predictors of excessive short-acting ?-agonist use and asthma exacerbations: a retrospective analysis of a Polish prescription database. (Pubmed Central) - Jan 29, 2024
1 exacerbation (1.60, 1.50-1.71). Excessive SABA use is highly prevalent in asthma management, is associated with lack of prescriptions for inhaled corticosteroids, and substantially increases the exacerbation risk.
- ||| Retrospective data, Journal, Adverse events: Assessing adverse pregnancy outcomes in women with uncontrolled asthma vs. mild asthma: a retrospective comparative analysis. (Pubmed Central) - Jan 26, 2024
Excessive SABA use is highly prevalent in asthma management, is associated with lack of prescriptions for inhaled corticosteroids, and substantially increases the exacerbation risk. Uncontrolled asthma during pregnancy is associated with higher adverse maternal-fetal and neonatal outcomes compared to mild asthma.
- || Trelegy Ellipta (fluticasone furoate/umeclidinium bromide/vilanterol) / GSK, Innoviva, Theravance Biopharma
Clinical, Journal, Real-world evidence, Real-world effectiveness, Real-world: Real-World Effectiveness of Fluticasone Furoate/Umeclidinium/Vilanterol Once-Daily Single-Inhaler Triple Therapy for Symptomatic COPD: The ELLITHE Non-Interventional Trial. (Pubmed Central) - Jan 26, 2024
In usual care, treatment with odSITT resulted in significant and clinically relevant improvements of CAT score and FEV in COPD patients, regardless of the occurrence of exacerbations. These findings challenge the current guideline recommendations for SITT only in patients experiencing exacerbations.
- | Journal: Therapeutic drug monitoring of corticosteroids/?-agonists in the hair of patients with asthma: an open-label feasibility study. (Pubmed Central) - Jan 25, 2024
P=N/A
Segmental hair analysis of inhaled medications was feasible, with low intrapatient variability. This innovative, non-invasive means of assessing monthly drug exposure might help physicians to personalize drug regimens for patients with difficult-to-treat asthma.
- | Journal: Analysis of 14 ?-agonists in pork using an automated wooden tip-based solid-phase microextraction device and ultra-high-performance liquid chromatography-tandem mass spectrometry. (Pubmed Central) - Jan 22, 2024
This innovative, non-invasive means of assessing monthly drug exposure might help physicians to personalize drug regimens for patients with difficult-to-treat asthma. Limits of detection and limits of quantification ranged from 0.09 to 0.39 and 0.27 to 0.99
- HSK31679 / Haisco
Hsk31679 (A Thyroid Hormone Receptor ? Agonist) in Asian NAFLD with Hypercholesterolemia (Room 12, B-1) - Jan 20, 2024 - Abstract #APASL2024APASL_2615;
This study will show the safety and efficacy of THR-? agonist in the Asian NAFLD population.
- | lansoprazole / Generic mfg., indomethacin / Generic mfg.
Journal: Protective effect of Amauroderma rugosum ethanol extract and its primary bioactive compound, ergosterol, against acute gastric ulcers based on LXR-mediated gastric mucus secretions. (Pubmed Central) - Jan 17, 2024
agonist in the Asian NAFLD population. EEA and its primary bioactive compound, ergosterol, exert anti-ulcer effects by promoting gastric mucus secretion through the LXR?/C-fos/COX-1/PGE2 pathway.
- || Review, Journal: Overuse of long-acting ?-agonist/inhaled corticosteroids in patients with chronic obstructive pulmonary disease: time to rethink prescribing patterns. (Pubmed Central) - Jan 11, 2024
We describe practical recommendations for primary care physicians to optimize therapy for their patients and prevent overuse of ICS-based regimens. We advocate adherence to current recommendations and a greater focus on effective treatments to successfully control symptoms, minimize exacerbation risk, preserve lung function, maximize patient outcomes, and reduce the burden of drug-related adverse events.
- | Journal: Aerosol Plumes of Inhalers Used in COPD. (Pubmed Central) - Jan 9, 2024
Plume velocity was lower and spray duration longer for the SMI compared with pMDIs and DPIs. Increasing experimental flow rate was associated with faster plume velocity for DPIs and the SMI, with no or variable impact on plume duration, whereas pMDI aerosol velocity and duration were unaffected by increasing flow rate.
- || Review, Journal: Systematic literature review of traits and outcomes reported in randomised controlled trials of asthma with regular dosing of inhaled corticosteroids with short-acting ?-agonist reliever, as-needed ICS/formoterol, or ICS/formoterol maintenance and reliever therapy. (Pubmed Central) - Jan 8, 2024
Conversely, many other traits and outcomes, although being potentially relevant, were inconsistently reported and limited subgroup reporting meant analyses of treatment response for subgroups of traits was not possible. We recommend more consistent measurement and reporting of clinically relevant patient traits and outcomes in respiratory RCTs.
- ALG-055009 / Aligos Therap
Pharmacodynamics of multiple oral doses of ALG-055009, a THR? agonist, in hyperlipidemic subjects (New Hall) - Jan 6, 2024 - Abstract #APASL2024APASL_2134;
P1
We recommend more consistent measurement and reporting of clinically relevant patient traits and outcomes in respiratory RCTs. Favorable, dose-dependent pharmacodynamic effects on atherogenic lipids and SHBG were observed with multiple dosing of ALG-055009 in HL subjects.
- | Preclinical, Journal: Transcriptional changes during isoproterenol-induced cardiac fibrosis in mice. (Pubmed Central) - Jan 5, 2024
A number of known long non-coding RNAs (lncRNAs) and putative novel lncRNAs exhibited differential regulation. In conclusion, our study shows that isoproterenol administration leads to the dysregulation of genes relevant to ECM deposition and cardiac contraction, and serves as an excellent alternate model to the surgical models of heart failure.