PF-03715455 / Pfizer - LARVOL DELTA

Targeting SARS-CoV-2 nsp13 Helicase and Assessment of Druggability Pockets: Identification of Two Potent Inhibitors by a Multi-Site In Silico Drug Repurposing Approach. (PubMed, Molecules) - "Finally, by means of visual inspection analysis and based on their commercial availability, five promising compounds were submitted to in vitro assays. Among them, PF-03715455 was able to block both the unwinding and NTPase activities of nsp13 in a micromolar range."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Screening of drug databank against WT and mutant main protease of SARS-CoV-2: Towards finding potential compound for repurposing against COVID-19. (PubMed, Saudi J Biol Sci) - "While PF-03715455 (Y54C), Salvianolic acid A (N142S and T190I), and Montelukast (A191V) were found to be most active against the other selected mutants. It was also found that some other compounds such as Acteoside, 4-Amino-N- {4-[2-(2,6-Dimethyl-Phenoxy)-Acetylamino]-3-Hydroxy-1-Isobutyl-5-Phenyl-Pentyl}-Benzamide, PF-00610355, 4-Amino-N-4-[2-(2,6-Dimethyl-Phenoxy)-Acetylamino]-3-Hydroxy-1-Isobutyl-5-Phenyl-Pentyl}-Benzamide and Atorvastatin were showing high efficacy against the WT as well as other selected mutants. We believe that these molecules will provide a better and effective option for the treatment of COVID-19 clinical manifestations."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

An Evaluation Of PF-03715455 In Moderate To Severe Chronic Obstructive Pulmonary Disease (clinicaltrials.gov) - P2; N=17; Terminated; Sponsor: Pfizer; N=100 -> 17 ; Recruiting -> Terminated ; Trial primary completion date: Mar 2017 ->May 2015

Enrollment change • Trial primary completion date • Trial termination • Biosimilar • Chronic Obstructive Pulmonary Disease

Pulmonary delivery of a p38 α/β MAP kinase inhibitor: bioanalytical method validation and biodistribution in rat plasma and respiratory tissues. (PubMed, Eur J Pharm Sci) - "In conclusion, a linear, accurate, precise and reproducible method has been developed and validated according to FDA and EMA guidelines to quantify plasmatic and tissue-associated concentrations of PF-03715455 in order to investigate this compound in pharmacokinetics pre-clinical studies in rats. The administration of drug solution evidenced a prolonged permanence of the drug in the lungs that could be related to a slow absorption/poor permeability of the drug across airways epithelia."

Journal • Preclinical • Asthma • Chronic Obstructive Pulmonary Disease • Immunology • Pulmonary Disease • Respiratory Diseases