PF-4191834 / Pfizer - LARVOL DELTA

A quality by design strategy for cocrystal design based on novel computational and experimental screening strategies: part A. (PubMed, Drug Deliv Transl Res) - "This strategy is presented herein as a Quality by Design (QbD) crystal engineering approach, combined with experimental screening methods to produce cocrystals of a novel 5-Lipoxygenase (5-LO) inhibitor, PF-04191834 (PF4). Through this methodology, three new cocrystals were indicated for PF4, confirmed via DSC and XRPD, from less than 50 mg of original testing material. Part B of this study will demonstrate the scalability of this technique continuous extrusion."

Journal

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

Electrophilic fluoroalkylthiolation induced diastereoselective and stereospecific 1,2-metalate migration of alkenylboronate complexes. (PubMed, Chem Sci) - "A transition metal free process for conjunctive functionalization of alkenylboron ate-complexes with electrophilic fluoroalkylthiolating reagents is described, affording β-trifluoroalkylthiolated and difluoroalkylthiolated boronic esters in good yield and excellent diastereoselectivity. The potential applicability of the method was demonstrated by the preparation of a difluoromethylthiolated mimic 12 of a potential drug molecule PF-4191834 for the treatment of asthma."

Journal • Asthma • Immunology • Pulmonary Disease • Respiratory Diseases