Clinical trial NCT00829907: A PET Study With ORM-12741
Official title: Effect of ORM-12741 on Receptor Occupancy Studied by Positron Emission Tomography; an Open, Single Dose, Dose Ranging Study in Healthy Males
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Keywords: Healthy volunteer study
Lead sponsor: Orion Corporation, Orion Pharma
Sponsor class: INDUSTRY
First posted: 2009-01-27
Enrollment: 26
Sex: MALE
Minimum age (years): 18
Maximum age (years): 45
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: NON_RANDOMIZED
Intervention model: PARALLEL

Brief summary: The purpose of the study is to evaluate the effect of ORM-12741 on receptor occupancy by positron emission tomography with different doses and plasma concentrations. The pharmacokinetic profile and safety will also be evaluated.


Eligibility criteria: Inclusion Criteria:

* Good general health ascertained by detailed medical history and physical examination
* Males between 18 and 45 years
* Body mass index (BMI; weight/height2) between 18-30 kg/m2
* Weight 55-95 kg

Exclusion Criteria:

* Evidence of clinically significant cardiovascular, renal, hepatic, haematological, gastro-intestinal, pulmonary, metabolic-endocrine, neurological, urogenital or psychiatric disease as judged by the investigator
* Any condition requiring regular concomitant medication including herbal products or likely to need any concomitant medication during the study
* Regular consumption of more than 21 units of alcohol per week (1 unit = 4 cl spirits, about 13 g of alcohol).
* Current use of nicotine-containing products more than 5 cigarettes or equivalent/day
* Inability to refrain from using nicotine-containing products during the stay at the study centre
* Inability to refrain from consuming caffeine-containing beverages during the stay at the study centre e.g. propensity for headache when refraining from caffeine-containing beverages
* Blood donation or loss of significant amount of blood within 3 months prior to the screening visit
* Abnormal 12-lead electrocardiogram (ECG) finding of clinical relevance
* Any abnormal value of laboratory, vital signs, or physical examination, which may in the opinion of the investigator interfere with the interpretation of the test results or cause a health risk for the subject if he takes part into the study
* Anatomical abnormality in brain MRI which may in the opinion of the investigator interfere with the interpretation of the PET results
* Participation in another clinical drug study within 3 months prior to the start of this study or earlier participation in a clinical study with ORM-12741
* Participation in a prior PET study
* Any contraindication to MRI of the brain

Primary outcomes:
measure: Receptor occupancy
timeFrame: 1 day
Secondary outcomes:
measure: Pharmacokinetic variables including peak concentration in plasma, time to peak concentration, area under the plasma concentration-time curve
timeFrame: 1 day
measure: Safety variables including blood pressure, heart rate, electrocardiogram, physical examination, laboratory safety variables (haematology, chemistry, serology, urinanalysis) and adverse events.
timeFrame: During the study
Other outcomes:
Locations:
city: Turku
country: Finland
facility: Turku PET centre
Study officials:
affiliation: Turku PET Centre
name: Juha Rinne, MD, PhD
role: PRINCIPAL_INVESTIGATOR
References:
citation: Shahid M, Rinne JO, Scheinin M, Virta J, Marjamaki P, Solin O, Arponen E, Sallinen J, Kuokkanen K, Rouru J. Application of the PET ligand [11C]ORM-13070 to examine receptor occupancy by the alpha2C-adrenoceptor antagonist ORM-12741: translational validation of target engagement in rat and human brain. EJNMMI Res. 2020 Dec 9;10(1):152. doi: 10.1186/s13550-020-00741-y.