The Immune-Mediated Inflammatory Disease Forum on LinkedIn: #rhematoidarthritis (2024)

Until recently, drug carcinogenicity assessment required two different in vivo studies, one of which was typically a two-year lifetime study in rats. The new addendum to the S1B guidelines allows certain drugs to forego the two-year rat study and utilize only one species (mice) for #carcinogenicity testing.This Drug Discovery World article describes how the use of #transgenic rasH2 mice can condense the in-vivo portion of testing to six months, significantly decreasing the time to New Drug Application (NDA) filing. Learn more: https://bit.ly/3QsCyMI

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Profiling oncogenic KRAS mutant drugs with a cell-based Lumit p-ERK immunoassay. No fuss Lumit immunoassay for detection of phosphorylated ERK. See paper in link -https://lnkd.in/edh22Hhg#KRAS #Lumit #immumoassay #phospho-ERK

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Sharing recent coverage of Insilico's novel, potentially first-in-class AI-designed inhibitor for inflammatory bowel disease (IBD) from Drug Discovery World. ◾ IBD is a widespread condition with limited therapeutic options. ◾ The current standard of treatment for IBD consists of anti-inflammatory drugs which offer limited improvement in mucosal healing, which is closely correlated to positive prognosis according to genetic and clinical evidence. ◾ Insilico's drug, ISM5411, now in Phase 1 trials, targets mucosal healing with the unique mechanism of barrier protection enhancement. ◾ Analysts GlobalData predict that the totalsales of IBD drugs will reach approximately $10.2 billionin the US in 2023.*Link to article in comments*

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Phenylglycine and its derivatives, arylglycines, form structural fragments in many drug molecules. From antibiotic Vancomycin approved for medical use in 1958 to recent drugs: Pasireotide (Cushing’s disease, 2012), Oritavancin (skin infections, 2014), Ivosidenib (acute myeloid leukemia, 2022), arylglycines have been reliably serving to medicinal chemistry. Enamine stock offers over 250 arylglycines with various substitution patterns. We offer𝑁-Fmoc,𝑁-Boc and free amino acid forms:https://bit.ly/40YlSjvTry our arylglycines in your research!

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Encouraging results from a recent head-to-headclinical trial demonstrates that a TYK2/JAK1 dual inhibitor has superior efficacy in rheumatoid arthritis patients compared to the approved JAK1/JAK3 dual inhibitor Xeljanz (tofacitinib), and was well tolerated and had no unexpected safety concerns.At Sareum we are developing SDC-1801, a potent and selective TYK2/JAK1 kinase inhibitor designed to address autoimmune diseases. SDC-1801 is currentlyin aPhase 1a clinical trialinvestigatingthe safety, tolerability, pharmaco*kinetics and pharmacodynamics of an oral formulation of the drug in healthy subjects.More here:https://lnkd.in/eJ36EkEA#JAKInhibitor

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There are various oral treatments available for psoriatic arthritis, a chronic and inflammatory form of arthritis. Although psoriatic arthritis is a lifelong disease requiring ongoing treatment, with the right treatment plan in place, remission is possible.The oral treatments that are currently available are:- Nonsteroidal anti-inflammatory drugs (NSAIDs)- Apremilast (Otezla)- Conventional disease-modifying antirheumatic drugs (DMARDs) such as sulfasalazine, methotrexate, leflunomide, hydroxychloroquine- Targeted synthetic DMARDs known as Janus kinase (JAK) inhibitors, such as tofacitinib (Xeljanz) and upadacitinib (Rinvoq)To read about the differences between these medications, you can click here: https://bit.ly/43xeriW

A complete tale on the unprecedented medicinal chemistry feat and inspiring insights behind the discovery of cysteine protease inhibitors: Nnirmatrelvir, Ensitrelvir, Leritrelvir, Simnotrelvir and many more such as EDP-235, FB-2001 and STI-1558/Olgotrelvir or five undisclosed compounds (CDI-988, ASC11, ALG-097558, QLS1128 and H-10517) undergoing clinical trials for COVID-19 treatment.

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Delighted to announce the publication of our latest paper in Journal of Biomolecular Structure and Dynamics: The binding mechanism of failed, in processing and succeed inhibitors target SARS-CoV-2 main protease.💡 Leveraging MindRank's Molecule Dance platform, the research team employed the Motion Based Drug Discovery module to conduct a comparative analysis of the interactions between the #SARS-CoV-2 Main Protease (SCM) and five prevalent #COVID-19 inhibitors (ritonavir, lopinavir, N3, ensitrelvir and nirmatrelvir). The results show that the binding site is highly flexible to fit those five different inhibitors and each compound has its unique binding mode at the same binding site. Moreover, the binding affinities of positive and negative inhibitors to SCM exhibit significant differences. 👉 Read more here: https://lnkd.in/eNtgdyHA #covid19 #artificialintelligence #drugdiscovery #research #healthcare

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#HighlyCitedPapers 💡🔬 Multiplex Patient-Based Drug Response Assay in Pancreatic Ductal Adenocarcinoma, by Armstrong and colleagues.In this study, the authors developed a multiplex #drug screening assay to assess ex vivo drug response to conventional and investigational drugs in pancreatic ductal #adenocarcinoma and identify #gene signature and pathways that may influence response to #therapy.Full text ➡️ https://lnkd.in/dUx-8Dxs

Cardiosight®-S Use CaseAssessment of the proarrhythmic effects of repurposed antimalarials for COVID-19 treatment using a comprehensive in vitro proarrhythmia assay (CiPA)1. Cell type : CHO cell (for hERG assay), hiPSC-derived Cardiomyocytes2. Test Drug : Pyronaridine, Artesunate, Dihydroartemisinin (DHA)3. Measuring Method : revised CiPA assay1) hERG assay2) hiPSC-CMs model3) in-silico model (ORd model)4. Parameters : ion Channel Inhibition (%), AP (Action Potential), Torsade Metric ScoreIn summary, pyronaridine, artesunate, and a combination of both drugs have been confirmed to pose a low proarrhythmogenic risk at therapeutic and supratherapeutic (up to 4 times) free Cmax.This experiment applied the revised CiPA assay, and may provide novel insights for evaluating drug-induced cardiotoxicity.For detailed information :https://lnkd.in/gTRUMN4Q#Cardiotoxicity#CiPA#TdP#Arrhythmia#ActionPotential#iPSC#Cardiomyocytes#hERG

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