Acute and chronic pain. Study to be conducted in healthy volunteers Not Applicable
Conditions
Interventions
In Part 1 participants will receive a single oral dose of ODM-111 as a tablet, and a single 5 ml IV dose of [14C]ODM-111.
In Part 2 participants will receive a single oral dose of [14C]ODM-111 as an
Sponsors
Orion Corporation (Finland)
Eligibility
Sex/Gender
Male
Inclusion criteria
Inclusion criteria: 1. Must provide written informed consent. 2. Must be willing and able to communicate and participate in the whole study. 3. Aged 30 to 65 years inclusive at the time of signing informed consent. 4. Must agree to and adhere to the contraception requirements defined in the clinical protocol. 5. Males who are healthy as determined by medical evaluation including medical history, physical or neurological examination, vital signs, 12-lead ECG, screening clinical laboratory profiles (haematology, biochemistry, coagulation, and urinalysis), as deemed by the Investigator or designee. 6. Body mass index (BMI) of 18.5 to 32.0 kg/m2 as measured at screening. 7. Weight 55 to 100 kg at screening. 8. Must have regular bowel movements (i.e. average stool production of =1 and =3 stools per day).
Exclusion criteria
Exclusion criteria: 1. Serious adverse reaction or serious hypersensitivity to any drug or formulation excipients. 2. Presence or history of clinically significant allergy requiring treatment, as judged by the investigator. Hay fever is allowed unless it is active. 3. History of clinically significant cardiovascular, renal, hepatic, dermatological, chronic respiratory or GI disease, neurological or psychiatric disorder, as judged by the investigator. 4. Subjects who do not have suitable veins for multiple venepunctures/cannulation as assessed by the investigator or delegate at screening. 5. Any clinically significant physical examination finding, as judged by the investigator. 6. Clinically significant abnormal clinical chemistry, haematology or urinalysis as judged by the investigator. Subjects with Gilbert’s Syndrome are not allowed. 7. Subjects who exhibit any first, second or third degree atrioventricular (AV) block at screening. 8. Subjects who have systolic BP 140 mmHg or diastolic BP 90 mmHg after 5 min in a supine position at screening. 9. Abnormal 12-lead ECG finding of clinical relevance at the screening visit or at pre-dose, (after 5 min rest in supine position), confirmed by a repeat measurement. 10. Positive hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV Ab) or human immunodeficiency virus (HIV) 1 and 2 antibody results. 11. Evidence of renal impairment at screening, as indicated by an estimated glomerular filtration rate (eGFR) of 21 units per week (1 unit = ½ pint beer, or a 25 mL shot of 40% spirit, 1.5 to 2 units = 125 mL glass of wine, depending on type). 21. A confirmed positive alcohol breath test at screening or admission. 22. Current smokers and those who have smoked within the last 12 mon
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Part 1: Absolute bioavailability (F) of ODM-111 based on AUC(0-inf) of oral administration of ODM-111 compared to radiolabelled IV microtracer dose of ODM-111, adjusted for dose. Part 2: Mass balance recovery of total radioactivity in all excreta (urine and faeces) and in urine and faeces separately: Ae, %Ae, CumAe and Cum%Ae and by interval. Part 1: Plasma samples for ODM-111 will be taken from pre-dose on Day 1 until 72 h post oral dose on Day 4. Part 2: Mass balance recovery will be measured in urine and faecal samples collected from pre-dose on Day 1 until discharge (up to Day 10), and potentially also including additional home collections if required. | — |
Secondary
| Measure | Time frame |
|---|---|
| Part 1: 1. PK parameters for ODM-111, [14C]ODM-111 and metabolites, and total radioactivity in plasma after a single IV microtracer dose of [14C]ODM-111. Including, but not limited to the following as applicable: Tmax, Cmax, AUC(0-last), AUC(0-inf), T1/2 and metabolite ratios. Plasma samples for ODM-111 taken from pre-dose (Day 1) until 72 h post oral dose (Day 4) 2. Adverse events (AEs), physical examinations, vital signs, ECGs, and laboratory safety tests. Monitoring for AEs occurs from signing the informed consent form until discharge (prior to Day -1 to Day 4). Results from physical examinations, vital sign measurements, ECGs and safety tests at screening and from pre-dose (Day 1) until 75 h post oral dose (Day 4) Part 2: 1. Collection of plasma, urine and faecal samples for metabolite profiling, structural identification, and quantification analysis. Analysis of blood, urine and faecal samples for ODM-111 taken from pre-dose (Day 1) until discharge (up to Day 10) 2. Identification of the chemical structure of each metabolite accounting for more than 10% by AUC of circulating total radioactivity or accounting for 10% or more of the dose in excreta. Performed by analysing blood, urine and faecal samples for ODM-111 taken from pre-dose (Day 1) until discharge (up to Day 10). Urine and faecal home collections may also be required. 3. Evaluation of whole blood:plasma concentration ratios for total radioactivity. Performed by analysing blood, urine and faecal samples for ODM-111 taken from pre-dose (Day 1) until discharge (up to Day 10). Urine and faecal home collections may also be required. 4. PK parameters for ODM-111, metabolites, and total radioactivity in plasma after a single oral dose of [14C]ODM-111. Including, but not limited to the following as applicable: Tmax, Cmax, AUC(0-last), AUC(0-inf), T1/2 and metabolite ratios. Performed by analysing plasma samples for ODM-111, metabolites and total radioactivity taken from pre-dose (Day 1) until discharge (up to | — |
Countries
England, United Kingdom
Outcome results
None listed