Clinical Programs with Riociguat in Pulmonary Hypertension Well on Track

Encouraging top-line data from the first Phase II study in pulmonary hypertension owing to interstitial lung disease (PH-ILD) / First Phase II study in pulmonary hypertension owing to chronic obstructive pulmonary disease (PH-COPD) successfully completed
Berlin, Germany, December 10, 2009 – A first Phase II trial with Bayer Schering Pharma’s oral agent riociguat (BAY 63-2521) in pulmonary hypertension owing to interstitial lung disease (PH-ILD) has successfully been completed. PH-ILD is a form of pulmonary hypertension for which no approved treatment options are currently available. The primary objectives of the study – to investigate safety and tolerability of riociguat in this subgroup of PH-patients – were achieved. The study demonstrated a reduction in pulmonary vascular resistance (PVR), together with a considerable increase in cardiac output and slight improvement of exercise capacity as measured by a six-minute walk test (6-MWT). Riociguat is the first member of a novel class of therapeutics called soluble guanylate cyclase (sGC) stimulators and is being investigated as a new approach to treat different forms of pulmonary hypertension (PH).

“These preliminary results from this initial investigation of riociguat in patients with PH-ILD are very promising in this difficult-to-treat indication where therapies are urgently needed,” said lead investigator Professor Marius Hoeper, Hannover Medical School, Hannover, Germany. “The reduction in pulmonary vascular resistance was remarkable and in the same range we have seen in previous studies with riociguat in pulmonary arterial hypertension. These positive results will pave the way for further studies on riociguat in PH-ILD and may offer physicians an opportunity to provide their patients a treatment in the future.”

It is planned to present the data at an international scientific meeting in 2010.

“Based on the encouraging data on riociguat in PH-ILD, Bayer will consider initiating the next step in the clinical PH-ILD program in 2010,” said Frank Misselwitz, MD, Vice President of Global Clinical Development and Head of the Cardiovascular and Coagulation Therapeutic Area, Bayer Schering Pharma AG. “We are making good progress in all our study programs with riociguat. We are well on track in our work on pulmonary hypertension owing to chronic obstructive pulmonary disease, having completed a first Phase II study in this field. Detailed data analyses are ongoing and will be presented in 2010.”

Bayer Schering Pharma is exploring the potential of riociguat as an innovative therapy for patients suffering from pulmonary hypertension, including forms for which there are currently no drug therapies.


About the Phase II studies
PH-ILD
A multicenter, open-label, uncontrolled Phase II study in patients with pulmonary hypertension owing to interstitial lung disease (PH-ILD): Patients received a dose of up to 2.5 mg riociguat three times daily for 12 weeks. The objective of the study was to investigate the safety and tolerability of riociguat. In addition, pulmonary hemodynamics, blood gases and exercise capacity measured by a six-minute walk test (6-MWT) as well as other parameters were assessed after 12 weeks of drug treatment and compared to baseline values. Within PH, PH-ILD has a global prevalence of approximately 110.000 patients* of the PH.

PH-COPD
A multicenter, open-label, uncontrolled Phase II study in patients with pulmonary hypertension owing to chronic obstructive pulmonary disease (PH-COPD): The objective of the study was to investigate the safety, tolerability and clinical effects of a single dose riociguat on the parameters of pulmonary hemodynamics, gas exchange and lung function in this subgroup of PH-patients. Within PH, PH-COPD has a global prevalence of approximately 1.1 million patients* of the PH population.

* current estimate by Bayer Schering Pharma


About Pulmonary Hypertension
Pulmonary Hypertension (PH) is a disorder in which the pressure in the pulmonary arteries is above normal. People with PH develop a markedly decreased exercise tolerance and reduced quality of life. Early PH is often asymptomatic. By the time symptoms appear, disease progression is usually well advanced. The most common symptoms of PH include shortness of breath with physical exercise (exertional dyspnea), fatigue, dizziness and fainting, all of which are worsened by exertion. PH is a severe and life-threatening disease that can lead to heart failure and death. According to the WHO classification, there are five different types of PH based on the underlying causes of pulmonary hypertension.