pleconaril
Pleconaril (Picovir) 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. Pleconaril, administered either orally or intranasally, is active against viruses in the Picornaviridae family, including Enterovirus and Rhinovirus. It has shown useful activity against the dangerous enterovirus D68. — Wikipedia
Clinical trial activity
3 trials · 3 clinical orgs · 0 marketing orgs
Earliest trial started Jun 1, 2001 (NCT00031512)
Timeline
2000s
- Jan 1, 2001
Earliest Phase 2 Sponsor(trial)
Indications
Mechanism of action
- VP1 capsid proteinDISRUPTING AGENT
VP1 capsid protein disrupting agent
It binds to a hydrophobic pocket in the VP1 protein in the viral capsid inducing conformational changes, which lead to altered receptor binding, viral uncoating preventing the virus from replicating.
Pleconaril inhibits the replication in cell culture of all 75 human rhinovirus (HRV) species A serotypes and 18 of the 25 species B viruses. The seven resistant serotypes are HRV-4, -5, -42, -84, -93, -97 and -99.
It binds to a hydrophobic pocket in the VP1 protein in the viral capsid.
Chemistry & pharmacology
SMILES
Cc1cc(CCCOc2c(C)cc(-c3noc(C(F)(F)F)n3)cc2C)on1- Mol. weight
- 381.35 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaPleconaril ↗
- ChEMBLCHEMBL29609 ↗
Also known as
- 3-(3,5-dimethyl-4-(3-(3-methyl-5-isoxazolyl)propoxy)phenyl)-5-(trifluoromethyl)-1,2,4-oxadiazole
- 3-(3,5-dimethyl-4((3-(3-methyl-5-isoxazolyl)propyl)phenyl)-5-trifluoromethyl)-1,2,4-oxadiazole
- picovir
- picovir
- pleconaril
- pleconaril
- pleconaril
- pleconaril
- pleconaril
- pleconaril
- pleconaril
- pleconaril
- vp-63843
- vp-63843
- win 63843
- win-63843
- win-63843
- win-63843
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04838145 | Phase 2 | Aug 30, 2018 | University of Oslo |
| NCT00394914 | Phase 2 | Aug 1, 2006 | Merck |
| NCT00031512 | Phase 2 | Jun 1, 2001 | National Institute of Allergy and Infectious Diseases (NIAID) |
Organizations
Research & Development (3)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Merck | For profit | 1 | 1 | 1 | 2006 |
| National Institute of Allergy and Infectious Diseases (NIAID) | Government | 1 | 1 | 1 | 2001 |
| University of Oslo | Academic/Hospital | 1 | 1 | 1 | 2018 |