September 9 2015
Discovery and preclinical development of pan-serotype small molecule inhibitors against dengue virus NS5 RNA-dependent RNA polymerase (RdRp) using fragment screening
Dengue is the most important mosquito-borne disease of humans and an important tropical infectious disease. The National Institute of Allergy and Infectious Diseases in the US lists the causative agent, dengue virus (DENV) ― of which there are four serotypes: 1 to 4 ― as a “category A” priority bio-threat pathogen. Approximately one third of the world’s population is at risk of infection ― which occurs most frequently in children less than 15 years of age. The spread of DENV in sub-tropical and tropical regions of the world has occurred over just a few decades due to globalisation and a failure to control the primary vector Aedes aegyptii. As Ae. Albopictus, a secondary DENV vector, is spreading to cooler climates the disease is spreading further. A recent 2014 outbreak in Portugal underlines this concern. There are currently no marketed treatments for DENV infection; thus, there is a real need for an effective and safe treatment.
The ultimate aim of Effecta’s dengue drug discovery programme is to identify pan-serotype inhibitors of the DENV NS5 polymerase protein for the treatment of dengue fever that bind to allosteric pockets of this critical viral protein, inhibiting viral replication and producing an antiviral effect. The Pathfinder award will allow Effecta Pharma to develop the first step in this programme: the technology to target the NS5 conserved region and identify the first chemical starting points for drug discovery. Beyond the Pathfinder award these chemical starting points will be used for lead identification and optimisation, ultimately resulting in preclinical candidate drugs to be tested in a clinical PoC study.
About Effecta Pharma Limited
Effecta Pharma Limited (http://effectapharma.com) is a UK-based biotechnology company dedicated to the discovery and development of novel medicines to treat viral diseases. Effecta‘s pipeline consists of a range of early stage programmes, initially focussing on small molecule antivirals for dengue virus. Effecta currently operates semi-virtually and has an experienced management team and a seasoned team of industry and academic advisors and collaborators. These include Dr Geoff Lawton, ex-Roche, board Antabio, Dr Ronald van Rij at the University of Nijmegen, Dr Andrew Davidson, at Bristol University. Charles River Laboratories (Biofocus/Argenta) is currently its drug discovery CRO partner. Effecta Pharma was founded by Paul Edwards (BI, Galapagos, Pfizer) and Helmuth van Es (co-founder Galapagos, Audion, Antabio and Citryll).
Effecta Pharma contact:
Potential partners and investors interested in talking to Effecta can contact us through the contact page on our website.