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Phosphodiesterase (PDE) research by Prof. David Adams of Heriot-Watt University (HWU) has discovered compounds with potent combined anti-inflammatory and bronchorelaxant activity, relevant to asthma and chronic obstructive pulmonary disease (COPD). This fuelled a major therapeutic development programme by the Japanese company, Kyorin Pharmaceutical Co. Ltd, resulting in 22 patents (18 published since 2008) with a direct link to the foundational work at HWU. The work was a key factor in Kyorin's continued commissioning of projects with Scottish Biomedical (SB) up to £14.9M, a technology management company founded by Scottish Universities, enabling SB's transition into a fully independent drug-discovery services company, [text removed for publication].
Psoriasis is a chronic inflammatory skin disorder affecting up to 2.5% of the world's population, approximately 30% of whom eventually develop psoriatic arthritis, which can lead to debilitating long-term health problems. Current therapies are limited owing to side effects or reductions in efficacy. Prof Miles Houslay, University of Glasgow has performed internationally recognised research on drug targets to alleviate the symptoms of inflammatory skin conditions. Working with Celgene, Houslay identified lead compounds and assays to screen promising early compounds for the treatment of psoriasis and psoriatic arthritis for clinical development. This identified the lead compound (apremilast), which was subsequently developed by Celgene. Between 2010 and 2013, phase III trials on apremilast have validated it as a safe, clinically effective oral drug, on the basis of which apremilast was submitted for regulatory approval of its use in patients with psoriatic arthritis to the health authorities of the USA and Canada in March 2013.
The discovery of a novel, inhaled dual phosphodiesterase 3 and 4 inhibitor, RPL554 — first developed in the Sackler Institute of Pulmonary Pharmacology, King's College London — led to the creation of a SME, Verona Pharma plc, which then successfully demonstrated clinical benefit in Phase II clinical trials. This is a major breakthrough as a "first in class" drug with both bronchodilator and anti-inflammatory activity in a single medicine for the treatment of important respiratory diseases, asthma and chronic obstructive pulmonary disease.
A new anti-inflammatory molecule FX125L was developed by David Fox at Warwick, in collaboration with David Grainger (Department of Medicine, Cambridge) and Funxional Therapeutics Ltd (FXT). Research in lead optimization, mechanistic preclinical chemistry, synthetic route development (for scale-up), and CMC (chemistry, manufacturing and controls) was conducted at Warwick. As a result FX125L completed Phase 1 and entered Phase 2 clinical trials in humans for the treatment of asthma or other inflammatory diseases. Its sale to Boehringer Ingelheim generated a multi-million pound return for FXT and its investors.