A PET Study to Determine PDE4 Occupancy of Roflumilast

• Research type

  Research Study

• Full title

  An Open-Label, [11C](R)-Rolipram, Positron Emission Tomography (PET) Study to Determine PDE4 Occupancy of Roflumilast after Oral Doses in Human Volunteers

• IRAS ID

  111444

• Contact name

  Darren Wilbraham

• Sponsor organisation

  Nycomed a Takeda Company

• Eudract number

  2012-002063-98

• ISRCTN Number

  n/a

• Clinicaltrials.gov Identifier

  n/a

• Research summary

  fluilast (trade names Daxas©, Daliresp©) is an anti-inflammatory drug that is currently licensed for severe COPD (chronic obstructive pulmonary disease) in the UK, a breathing disease. More than 14000 healthy volunteers and patients have received this drug in over 100 clinical trials worldwide. Because of the way that fluilast works in the body (it inhibits a type of protein called phospodiesterase 4 or PDE4) it may have a beneficial effect on cognition. Cognition processes are mental processes such as attention, concentration, learning, thinking, and problem solving. Some brain disorders, like Alzheimer??s disease (AD), are associated with significant difficulties in cognition. AD is the most common cause of dementia. There is no cure for this disease. Drugs such as donepezil (Aricept?½) are available but provide only modest and short-lived symptomatic treatment to a portion of patients. This purpose of this trial is to investigate the relationship between the repeated oral (by mouth) doses of fluilast and PDE4 inhibition in brain. The information obtained from this clinical trial will be used to select appropriate dose of fluilast for use in future clinical trials. The inhibition of PDE4 in brain will be detected by special x-ray technique called Positron Emission Tomography (PET). This will involve the intravenous injection of a small amount of radioactive chemical, [11C]R-rolipram which attach to PDE4 receptors in brain. Up to 12 healthy male volunteers will undergo 3 PET scans with [11C] (R)-rolipram at Baseline, following the first single oral dose (by mouth) of fluilast, and after 8 days of daily administration of fluilast. Each participant will also have an MRI (Magnetic Resonance Imaging) scan of the brain following screening to picture different parts of brain and provide information to help in the analysis of PET scan images. The study will also explore the safety and tolerability of fluilast.

• REC name

  London - Riverside Research Ethics Committee

• REC reference

  12/LO/1309

• Date of REC Opinion

  19 Oct 2012

• REC opinion

  Further Information Favourable Opinion