rilapladib (SB-659032) / GSK - LARVOL DELTA

An AI-Driven Chemogenomics Knowledgebase for Human-Transmissible Pathogens: A Platform for Antimicrobial Drug Discovery. (PubMed, J Chem Inf Model) - "In wet-lab validations, four approved drugs (cefixime, ceftazidime, saquinavir, and rilapladib) identified via virtual screening show binding activity to SARS-CoV-2 nucleoprotein in affinity assays and inhibit SARS-CoV-2 replication in Vero E6 cells, demonstrating HPM-CKB's potential in drug repurposing. Meanwhile, two anti-Staphylococcus aureus lead compounds with novel scaffolds (CYC-HXL-9124 and CYC-HXL-9126) are identified via deep learning, and the potential target protein, cell division protein FtsZ, is subsequently prioritized using HPM-CKB (http://cgai.asia/g/pathogenDB) and experimentally validated by affinity assays. Collectively, these findings establish HPM-CKB as both a chemogenomic knowledgebase and a systematic drug development platform against EIDs."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases • CKB

A novel approach to combat Pseudomonas aeruginosa: repurposing pharmaceuticals for inhibition of phospholipase A. (PubMed, Microbiol Spectr) - "Experimental screening identified that compounds GW4869, darapladib, and rilapladib significantly inhibit Pseudomonas aeruginosa growth by more than 50%. One standout compound, a preclinically studied drug called GW4869, both slows bacterial growth and boosts the effectiveness of the last-resort antibiotic imipenem, suggesting better outcomes with combination treatments. Overall, this research points to the exciting possibility of repurposing human-focused medicines as new antimicrobial agents to help combat the escalating crisis of antibiotic resistance while deepening our insight into how these drugs can influence microbes."

Journal • Infectious Disease

Quinolines-Based SARS-CoV-2 3CLpro and RdRp Inhibitors and Spike-RBD-ACE2 Inhibitor for Drug-Repurposing Against COVID-19: An in silico Analysis. (PubMed, Front Microbiol) - "The result shows rilapladib is the only quinoline that can interrupt the Spike-RBD-ACE2 complex. In conclusion, owing to their ability to target functional macromolecules of SARS-CoV-2, along with positive ADMET properties, quinoline,1,2,3,4-tetrahydro-1-[(2-phenylcyclopropyl)sulfonyl]-trans-(8CI), saquinavir, elvitegravir, oxolinic acid, and rilapladib are suggested for the treatment of COVID-19."

Journal • Infectious Disease • Novel Coronavirus Disease

Study to Determine the Effect of Itraconazole on the Pharmacokinetics of Rilapladib (SB659032) in Healthy Volunteers (clinicaltrials.gov) - P1; N=30; Not yet recruiting; Sponsor: GlaxoSmithKline; Initiation date: May 2014 ->Jun 2014

Trial initiation date • Acute Coronary Syndrome • Alzheimer's Disease • Biosimilar • Chronic Kidney Disease • Dyslipidemia • Heart Failure • Immunology • Myositis