Pleconaril

Pleconaril (Picovir[1]) is an antiviral drug that was being developed by Schering-Plough for prevention of asthma exacerbations and common cold symptoms in patients exposed to picornavirus respiratory infections.

[2] Pleconaril, administered either orally or intranasally, is active against viruses in the Picornaviridae family, including Enterovirus[3] and Rhinovirus.

[2] A pleconaril intranasal spray had reached phase II clinical trial for the treatment of the common cold symptoms and asthma complications.

[8] In Coxsackievirus, pleconaril efficiency correlates to the susceptibility of CVB3 with the amino acid at position 1092 in the hydrophobic pocket.

[6] The results of two randomized, double blind, placebo studies found Pleconaril treatment could benefit patients with colds due to picornaviruses.

[14] Participants in the studies were healthy adults from Canada and the United States, with self-diagnosed colds that had occurred within 24 hours of trial enrollment.

Pleconaril treatment showed a reduction in nose blowing, sleep disturbance, and less cold medication used.

[9] A Phase II study that used an intranasal formulation of pleconaril failed to show a statistically significant result for either of its two primary efficacy endpoints, percentage of participants with rhinovirus PCR-positive colds and percentage of participants with asthma exacerbations together with rhinovirus-positive PCR.

Methyl and bromine substitutions created an increase of pleconaril activity towards sensitive and resistant strains.

[14] In the clinical trial two women became pregnant due to the drug interfering with hormonal birth control by activation of cytochrome P-450 3A enzymes.

This image was created in JMOL showing the beta sheets and alpha helices of the Human Rhinovirus. The molecule embedded in the hydrophobic pocket of the VP1 protein is pleconaril.