CE-224535 / Pfizer - LARVOL DELTA

P2X receptors: Insights from the study of the domestic dog. (PubMed, Neuropharmacology) - "The article will also discuss the characterization of single nucleotide polymorphisms in the canine P2RX7 gene, and contrast this variation to the canine P2RX4 gene, which is largely conserved between dogs. Finally, this article will outline published examples of the use of dogs to study the pharmacokinetics of P2X7 and P2X3 antagonists, and how they have contributed to the preclinical testing of antagonists to human P2X7, CE-224,535, and human P2X3, Gefapixant (AF-219, MK-7264) and Eliapixant (BAY, 1817080), with Gefapixant gaining recent approval for use in the treatment of refractory chronic cough in humans."

Journal • Review • Cardiovascular • Chronic Cough • Cough • Oncology • Pulmonary Disease • Respiratory Diseases

Study of CE-224,535 A Twice Daily Pill To Control Rheumatoid Arthritis In Patients Who Have Not Totally Improved With Methotrexate (clinicaltrials.gov) - P2a | N=100 | Completed | Sponsor: Pfizer | Phase classification: P2/3 ➔ P2a

Phase classification • Immunology • Inflammatory Arthritis • Rheumatoid Arthritis • Rheumatology • CRP

Antagonism of the ATP-gated P2X7 receptor: a potential therapeutic strategy for cancer. (PubMed, Purinergic Signal) - "It also describes in detail a number of key P2X7R antagonists currently in pre-clinical and clinical development, including oxidised ATP, Brilliant Blue G (BBG), KN-62, KN-04, A740003, A438079, GSK1482160, CE-224535, JNJ-54175446, JNJ-55308942, and AZ10606120. Lastly, it summarises the in vivo studies and clinical trials associated with the use and development of these P2X7R antagonists in different disease contexts."

Journal • Review • Immunology • Inflammation • Oncology