Information about Pleconaril

Pleconaril is an antiviral drug being developed by Schering-Plough for prevention of asthma exacerbations and common cold symptoms in asthmatic subjects exposed to picornavirus respiratory infections.Although the formulation used by Schering-Plough is a nasal spray, pleconaril is orally bioavailable, and is active against viruses in the Picornaviridae family, including Enterovirus and Rhinovirus.
Pleconaril was originally developed by Sanofi-Aventis, and licensed to ViroPharma in 1997. ViroPharma developed it further, and submitted a New Drug Application to the United States Food and Drug Administration (FDA) in 2001. The application was rejected, citing safety concerns; and ViroPharma re-licensed it to Schering-Plough in 2003. The Phase II clinical trial was completed in 2007. A pleconaril intranasal spray had reached phase II clinical trial for the treatment of the common cold symptoms and asthma complications. However, the results have yet to be reported.
Pleconaril in enteroviruses, prevents the virus from exposing its RNA, and in rhinoviruses prevents the virus from attaching itself to the host cell. Human rhinoviruses (HRVs) contain four structural proteins labeled VP1-VP4. Proteins VP1,VP2 and VP3 are eight stranded anti-parallel β-barrels. VP4 is an extended polypeptide chain on the viral capsid inner surface. Pleconaril binds to a hydrophobic pocket in the VP1 protein. Pleconaril has been shown in viral assembly to associate with viral particles. Through noncovalent, hydrophobic interactions compounds can bind to the hydrophobic pocket. Amino acids in positions Tyr152 and Val191 are a part of the VP1 drug binding pocket.
CAS No.:153168-05-9
Molecular Formula:  C18H18F3N3O3
Molecular Weight:  381.35 g/mol