Pharmacokinetics
Conditions
Brief summary
A study in healthy volunteers to determine whether different drugs metabolised by the liver have any effects on how NRL972 is processed within the body.
Interventions
DRUGNRL972
Single intravenous administration of 2 mg NRL972 after pre-treatment with 600 mg p.o. rifampicin once daily from the evening of Day D-7 until the evening of Day D-1
Sponsors
Norgine
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
DIAGNOSTIC
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
21 Years to 40 Years
Healthy volunteers
Yes
Inclusion criteria
1. Males or females (females of non-childbearing potential or of childbearing potential while taking medically appropriate contraception) 2. Caucasian 3. Age: 21 - 40 years 4. BW 50 - 100 kg 5. BMI 20 - 26 kg.m-2 6. healthy based on the pre-study examination 7. willing and able to provide informed consent
Exclusion criteria
General - all subjects 1. Previous participation in the trial 2. Participant in any other trial during the last 90 days 3. Donation of blood during the last 60 days or a history of blood loss exceeding 300 mL within the last 3 months 4. History of any clinically relevant allergy (including hypersensitivity to the trial medications) 5. Presence of acute or chronic infection 6. Presence or history of any relevant co-morbidity 7. Resting systolic blood pressure \> 160 or \< 90 mmHg, diastolic blood pressure \> 95 or \< 50 mmHg 8. Clinically relevant ECG-abnormalities, prolonged QTc with \> 450 msec in males and \> 460 msec in females in particular 9. Presence of any relevant abnormality in the laboratory safety tests, especially low haemoglobin, increased liver enzymes 10. Positive serology for HBsAg, anti HBc and anti HCV 11. Positive HIV test 12. Positive alcohol or urine drug test on recruitment (and upon admission) 13. History of alcohol and/or drug abuse and/or daily use of \> 30 gr alcohol 14. Smoking more than 15 cigarettes/day or equivalent of other tobacco products 15. Use of prohibited medication 16. Suspicion or evidence that the subject is not trustworthy and reliable 17. Suspicion or evidence that the subject is not able to make a free consent or to understand the information in this regard General - all females 18. Positive pregnancy test 19. Lactating 20. Not using appropriate contraception in pre-menopausal women (note: under the conditions of the present study, women using hormonal contraceptives will be informed that this method is not sufficient during the study and that further i.e. mechanical methods \[condom, diaphragm with spermacide gel\] should be used in addition).
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Total clearance by non-compartmental analysis. Apparent terminal disposition half-life t½ by non-compartmental analysis | Up to 6 hours post dose |
Secondary
| Measure | Time frame |
|---|---|
| Non-compartmental PK-analysis based on the extensive profile (up to last quantifiable data point), the 'short' profile (over the first hour after injection), and the two-point profile based on selected data-pairs over the 1st hour after dosing | Up to 6 hours post dose |
Countries
Bulgaria
Outcome results
None listed