2. Academic Validation
  3. An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus

An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus

  • ACS Med Chem Lett. 2012 Feb 13;3(4):303-7. doi: 10.1021/ml2002955.
Susanne C Feil 1,  Stephanie Hamilton 2,  Guy Y Krippner 2,  Bo Lin 2,  Angela Luttick 2,  Darryl B McConnell 2,  Roland Nearn 2,  Michael W Parker 3,  Jane Ryan 2,  Pauline C Stanislawski 2,  Simon P Tucker 2,  Keith G Watson 2,  Craig J Morton 4
Affiliations

Affiliations

  • 1 Biota Structural Biology Laboratory, St. Vincent's Institute , 9 Princes Street, Fitzroy, Victoria 3065, Australia.
  • 2 Biota Holdings Ltd. , 10/585 Blackburn Road, Notting Hill, Victoria 3168, Australia.
  • 3 Biota Structural Biology Laboratory, St. Vincent's Institute , 9 Princes Street, Fitzroy, Victoria 3065, Australia ; Department of Biochemistry and Molecular Biology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne , 30 Flemington Road, Parkville, Victoria 3010, Australia.
  • 4 Biota Holdings Ltd. , 10/585 Blackburn Road, Notting Hill, Victoria 3168, Australia ; Biota Structural Biology Laboratory, St. Vincent's Institute , 9 Princes Street, Fitzroy, Victoria 3065, Australia.
PMID: 24900468 DOI: 10.1021/ml2002955
Abstract

Respiratory infections caused by human rhinovirus are responsible for severe exacerbations of underlying clinical conditions such as asthma in addition to their economic cost in terms of lost working days due to illness. While several Antiviral compounds for treating rhinoviral infections have been discovered, none have succeeded, to date, in reaching approval for clinical use. We have developed a potent, orally available rhinovirus inhibitor 6 that has progressed through early clinical trials. The compound shows favorable pharmacokinetic and activity profiles and has a confirmed mechanism of action through crystallographic studies of a rhinovirus-compound complex. The compound has now progressed to phase IIb clinical studies of its effect on natural rhinovirus Infection in humans.

Keywords

antiviral; capsid; inhibitor; rhinovirus.

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