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Verona Pharma's lead drug compound, RPL554, is a novel long acting inhibitor of both phosphodiesterase 3 and phosphodiesterase 4 enzymes, two enzymes known to be of importance in the development and progression of immunological respiratory diseases, particularly rhinitis (hay fever) and asthma. As a PDE 3 inhibitor, the drug is expected to result in bronchodilator actions, whilst the PDE 4 component is expected to be anti-inflammatory.
RPL554 was selected from a class of compounds co-invented by Sir David Jack, the former Director of Research at Glaxo who led the team that discovered many of the commercially successful drugs in the respiratory market.
The competitive advantages of RPL554 include the following:
- combining bronchodilator (PDE 3) and anti-inflammatory actions (PDE 4) in a single drug, something that is currently only achieved with a combination LABA and glucocorticosteroid inhaler,
- unique in not using steroids or beta agonists, which have known side effects,
- planned to be administered by nasal inhalation, thereby reducing the unwanted gastrointestinal side effects of many orally administered drugs, and
- expected to be long acting, thereby allowing once a day treatment which is likely to increase medication compliance.
During the first half of 2007, the synthetic pathway for the production of scaleable quantities of the RPL554 compound was formulated and a sufficient quantity to complete planned preclinical and clinical studies was manufactured. In May 2008, Verona Pharma completed toxicological studies of RPL554 according to Good Laboratory Practices (GLP) with LAB Research Inc. of Hungary, successfully establishing that the compound is safe to give to man in clinical trials. In February 2009, a Phase I/IIa clinical trial of RPL554 was commenced at the Centre for Human Drug Research (CHDR) at Leiden in the Netherlands. In September 2009, the Company announced that it had successfully completed the trial, demonstrating that the drug had a good safety profile and had beneficial effects in terms of bronchodilation and bronchoprotection in asthmatics and a reduction in the numbers of inflammatory cells in the nasal passages of allergic rhinitis patients. The Company is currently seeking licensing agreements or partnerships for the further development and commercialisation of RPL554.
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