Evaluation of the Pharmacokinetics of NRL972 Following Pre-Administration of Rifampicin and Cyclosporine

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. Identifier: NCT00856752
Recruitment Status : Completed
First Posted : March 6, 2009
Last Update Posted : March 6, 2009
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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.

Condition or disease Intervention/treatment Phase
Pharmacokinetics Drug: NRL972 Phase 1

Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 12 participants
Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: None (Open Label)
Primary Purpose: Diagnostic
Official Title: A Single-Centre, Open, Controlled, Randomised Cross-Over Study in Healthy Male and Female Volunteers to Evaluate the Pharmacokinetics of Cholyl-Lysyl-Fluorescein (NRL972) in the Presence of Medication-Induced Changes in Cytochrome P450 or Biliary Transporter Proteins. Part A: Interaction With Rifampicin and Cyclosporine
Study Start Date : June 2006
Actual Primary Completion Date : July 2006
Actual Study Completion Date : August 2006

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Arm Intervention/treatment
Experimental: T1
Pre-treatment with rifampicin
Drug: NRL972
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

Experimental: T2
Pre-treatment with cyclosporin
Drug: NRL972
Single intravenous administration of 2 mg NRL972 injection after pre-treatment with 100 mg cyclosporine on the evening of Day D-1 and on the morning of Day D01 one hour before administration of NRL972

Experimental: Reference
Administration of NRL001 alone: no pre-treatment
Drug: NRL972
Reference test: Single intravenous administration of 2 mg NRL972

Primary Outcome Measures :
  1. Total clearance by non-compartmental analysis. Apparent terminal disposition half-life t½ by non-compartmental analysis [ Time Frame: Up to 6 hours post dose ]

Secondary Outcome Measures :
  1. 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 [ Time Frame: Up to 6 hours post dose ]

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Ages Eligible for Study:   21 Years to 40 Years   (Adult)
Sexes Eligible for Study:   All
Accepts 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).

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To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its identifier (NCT number): NCT00856752

Dept. Clinical Pharmacology & Therapeutics, MHAPT "Zaritza Johanna" University Hospital
Sofia, Bulgaria, 1527
Sponsors and Collaborators
Study Director: Hans J Gruss, MD Norgine Ltd
Principal Investigator: Emil Gatchev, PD Dr MHAPT "Zaritza Johanna" University Hospital

Responsible Party: Vice President Clinical Development, Norgine Identifier: NCT00856752     History of Changes
Other Study ID Numbers: NRL972-04A/2005 (IN-A)
First Posted: March 6, 2009    Key Record Dates
Last Update Posted: March 6, 2009
Last Verified: March 2009

Additional relevant MeSH terms:
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action
Immunosuppressive Agents
Immunologic Factors
Physiological Effects of Drugs
Antifungal Agents
Anti-Infective Agents
Dermatologic Agents
Antirheumatic Agents
Calcineurin Inhibitors
Antibiotics, Antitubercular
Antitubercular Agents
Anti-Bacterial Agents
Leprostatic Agents
Nucleic Acid Synthesis Inhibitors
Cytochrome P-450 CYP2B6 Inducers
Cytochrome P-450 Enzyme Inducers
Cytochrome P-450 CYP2C8 Inducers
Cytochrome P-450 CYP2C19 Inducers
Cytochrome P-450 CYP2C9 Inducers
Cytochrome P-450 CYP3A Inducers