setileuton (MK-0633) / Merck (MSD) - LARVOL DELTA

Unveiling the Anti-cancer Potential of Oxadiazole Derivatives: A Comprehensive Exploration of Structure-Activity Relationships and Chemico-Biological Insights. (PubMed, Med Chem) - "Overall, these results will prove to be a helpful and vital tool for medicinal chemists investigating and working with oxadiazoles for anti-cancer action."

Journal • Review • Oncology

The role and transformative potential of IL-19 in atherosclerosis. (PubMed, Cytokine Growth Factor Rev) - "Most antiatherosclerotic drugs in current clinical use, including atorvastatin and alirocumab, target hyperlipidemia. Several other drugs have also been investigated in clinical trials as anti-inflammatory agents; the development of some of these agents has been terminated (canakinumab, darapladib, varespladib, losmapimod, atreleuton, setileuton, PF-04191834, veliflapon, and methotrexate), but others remain in development (ziltivekimab, tocilizumab, Somalix, IFM-2427, anakinra, mesenchymal stem cells (MSCs), colchicine, everolimus, allopurinol, and montelukast)...We propose that IL-19 is a promising biomarker and target for the diagnosis and treatment of atherosclerosis. This review considers the role and mechanism of action of IL-19 in atherosclerosis and discusses whether IL-19 is a potential therapeutic target for this condition."

Journal • Review • Atherosclerosis • Cardiovascular • CNS Disorders • Dyslipidemia • Immunology • Inflammation • Multiple Sclerosis • Orthopedics

1,3,4-Oxadiazole Containing Compounds As Therapeutic Targets For Cancer Therapy. (PubMed, Mini Rev Med Chem) - "The discussion outlined herein will proved to be a helpful and vital tool for medicinal chemists investigating and working with 1,3,4-oxadiazoles and anticancer research programs."

Journal • Oncology

SARS-CoV-2 M inhibitors: identification of anti-SARS-CoV-2 M compounds from FDA approved drugs. (PubMed, J Biomol Struct Dyn) - "Based on comparative molecular simulation and interaction profiling of the screened drugs with SARS-CoV-2 M revealed R428 (-10.5 kcal/mol), Teniposide (-9.8 kcal/mol), VS-5584 (-9.4 kcal/mol), and Setileuton (-8.5 kcal/mol) with stronger stability and affinity than other drugs and N3 inhibitor; and hence, these drugs are advocated for further validation using in vitro enzyme inhibition and in vivo studies against SARS-CoV-2 infection."

FDA event • Journal • Infectious Disease • Novel Coronavirus Disease

5-Lipoxygenase as a drug target: A review on trends in inhibitors structural design, SAR and mechanism based approach. (PubMed, Bioorg Med Chem) - "Currently, the only drug against 5-LOX which is available is Zileuton, while a few inhibitors are in clinical trial stages such as Atreleuton and Setileuton. So, there is a dire requirement in the area of progress of novel 5-LOX inhibitors which necessitates an understanding of their structure activity relationship and mode of action. In this review, novel 5-LOX inhibitors reported so far, their structural design, SAR and developmental strategies along with clinical updates are discussed over the last two decades."

Journal • Review • Allergy • Asthma • Atherosclerosis • Cardiovascular • Dyslipidemia • Immunology • Inflammation • Respiratory Diseases