Chiesi Reports Successful Completion First-in-Man Phase 1 Study With Novel Inhaled PDE4 Inhibitor

PARMA, Italy, October 16, 2012 /PRNewswire/ --

Chiesi Group announces that it has successfully completed a Phase I trial of its inhaled PDE4 (phosphodiesterase 4) inhibitor, denoted CHF 6001, a new chemical entity developed for the treatment of inflammatory respiratory disorders, such as chronic obstructive pulmonary disease (COPD) and asthma.

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The phase 1 study was conducted to evaluate safety, tolerability and pharmacokinetics after administration of single doses (up to 2000 µg) and repeated doses (up to 2000 µg for 7 days) to healthy volunteers. CHF6001 was well tolerated up to the highest doses administered, both in single and multiple dose parts of the study, particularly with respect to gastrointestinal side effects: an area which has posed significant development hurdles for other PDE4 inhibitors in the past. No relevant safety findings, including cardiac side effects were observed. The long-lasting exposure in the systemic circulation supports once-a-day dosing. Based on these positive results, two phase 2a proof of concept studies are ongoing in patients with asthma and COPD.

About CHF 6001

CHF 6001 is a novel selective PDE4 inhibitor, optimized for inhaled delivery to improve efficacy and tolerability. The anti-inflammatory activity of CHF 6001 has been proven in vitro and in several animal models of airway inflammation, showing higher potency than the marketed oral PDE4 inhibitor (roflumilast) and more targeted anti-inflammatory effects than corticosteroids in COPD models. The compound is characterized by a low oral bioavailability, inactive metabolites, high plasma protein binding, low plasma/lung concentration ratio and low brain exposure. Moreover, CHF 6001 was very well tolerated in extended pre-clinical safety studies and the safety margin between the anti-inflammatory action and side-effects (such as nausea and emesis) is much larger in comparison to oral and inhaled PDE4 inhibitors developed to date.

The doses achievable in humans with most PDE4 inhibitors are limited by side effects, and therefore the optimal therapeutic effects of this class of drug have never been achieved. The profile of CHF 6001 indicates that it will not be under-dosed in humans to achieve an acceptable side effect profile, supporting its high potential for the treatment of COPD and asthma.

About Chiesi Group

Founded in 1935 in Parma (Italy), the Chiesi Group achieved a turnover of 1,056 million Euro in 2011, up by 4.1% on the previous year. The Group, currently has a total of 25 affiliates worldwide and is present in over 60 countries with its drugs, which are produced at plants in Parma, Blois (France) and Santana de Parnaiba (Brazil). In 2011 investment in R&D reached 169.3 million Euro, equivalent to 16% of the turnover. The R&D centres in Parma, Paris, Rockville (USA) and Chippenham (UK) integrate their efforts to work together on the Group's pre-clinical, clinical and registration programmes. At the end of 2011, the Chiesi Group's total staff stood at over 3,800 people, more than 320 of whom are dedicated to R&D.

The main areas of activity are in respiratory therapeutics and specialist medicine areas. A clear shift occurred in the last years towards more innovative molecules. The respiratory pipeline now comprises several classes of novel bronchodilating agents (Long acting muscarinic antagonists, bifunctional muscarinic antagonists-Βeta2 Agonits) and anti-inflammatory agents (PDE4 inhibitors, p38 kinase inhibitors, Neutrophil Elastase Inhibitors) that provide opportunities for future innovative fixed combinations for the treatment of asthma and COPD.

SOURCE Chiesi Farmaceutici S.p.A.