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CompletedNCT01193621Updated Jul 11, 2013

Early Clinical Evaluation of the Pharmacokinetics and Mechanism Based Pharmacodynamics of Haloperidol Using Positron Emission Tomography in Healthy Volunteers

A Phase 1 interventional study of haloperidol, PET in Healthy, sponsored by Asan Medical Center. Completed at 1 site in Korea, Republic of. Open to male participants aged 19 Years to 45 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2013-07-11.

Sponsored by Asan Medical Center · Phase 1 and Interventional

Phase
Phase 1
Study type
Interventional
Enrollment
12
Allocation
Randomized
Ages
19 Years to 45 Years
Sex
Male
01

Study summary

In the present study, the investigators will establish the clinical trial technology for early evaluation of drug characteristics in terms of pharmacokinetics and pharmacodynamics for haloperidol as a model drug, using positron emission tomography.

Read the detailed description

  1. Study Design

    This study will consist of two parts. One is "biodistribution study of haloperidol" in 12 subjects, and the other is "receptor occupancy study of haloperidol" in 12 subjects. In the biodistribution study, 18F-haloperidol (10 mCi) will be injected intravenously two times into each of the 12 subjects (cross-over design). Whole body PET will be conducted after the first haloperidol injection and local brain PET after the 2nd haloperidol injection after the 7 day washout period.

    1.1 D2-receptor occupancy study Group Doses No. of subjects 1 0.5 mg 4 2 1 mg 4 3 3 mg 4

  2. Measurement 2.1 The D2 receptor Occupancy of haloperidol.

  3. Test schedule 3.1 Biodistribution study

    • Whole body PET (day 1)
    • Brain local PET (day 8) 3.2 Receptor occupancy study
    • Baseline PET before drug administration (day 1 0h), 6h (day 1 6h), 24h (day 2 0h), after the first haloperidol administration (day 1 0h), and 24 h (day 8), 72 h (day 10), and 168 h (day 14) after the last dosing of haloperidol (day 7 0h).
    • Drug administration from day 1 through day 7 every 24 hours PK blood sampling (6 ml, each) prior to the first haloperidol administration (day 1 0h) and 6h (1 day 6h), 24h (2 day 0h), 48 h (3 day 0h), 96 h (5 day 0h), 144 h (7 day 0h) and, 0.5, 1, 2, 4, 6, 8, 12, 24 h (8day 0h), 48h (9day 0h), 72h (10 day 0h) after taking the last oral dose of haloperidol
  4. Analytic Methods 4.1 Pharmacokinetics: Noncompartmental Analysis Using Winnonlin Compartment model using NONMEM VII 4.2 Pharmacodynamics in the brain: Emax or linear model using NONMEM VII
02

Conditions studied

  • Healthy

Keywords

  • early evaluation
  • pharmacokinetics
  • pharmacodynamics
  • Biodistribution
  • D2-receptor occupancy
03

In context

Lead sponsor

Asan Medical Center is the lead sponsor of 562 studies on the registry; 71 are open to participants now.

Counted across the registry records on this site, refreshed daily.

04

Who can participate

Ages eligible
19 Years to 45 Years
Sexes eligible
Male
Accepts healthy volunteers
Yes

Inclusion criteria

  • Overtly healthy males as determined by medical history and physical examination
  • Age from 19 to 45 years
  • Weight ≥ 45 kg and within ± 20% of IBW
  • Clinical laboratory test results within normal reference range for the National Cancer Center, Hospital or results with minor deviations which are judged to be not clinically significant by the investigator
  • Normal blood pressure and heart rate (supine and standing) as determined by the investigator
  • Are reliable and willing to make themselves available for the duration of the study, and who will abide by the study restrictions
  • Have given written informed consent

Exclusion criteria

Exclusion Criteria:

  • History or presence of cardiovascular, respiratory, hepatic, renal, gastrointestinal, neurological disorders capable of altering the absorption, metabolism or elimination of drugs, or of constituting a risk factor when taking the study medication
  • An episode of febrile disease or infectious disease within the past 2 weeks
  • Evidence of significant active hematologic disease and/or blood donation in the last 2 months
  • Evidence of significant active neuropsychiatric disease
  • Regular use of drugs or abuse
  • History of drug hypersensitivity or clinically significant allergic reactions of any origin
  • Participation in a study involving administration of an investigational compound within the past 30 days
  • Have a regular alcohol intake greater than 21 units/week or subjects unwilling to stop alcohol for the duration of the study periods
  • Intend to use concomitant drug therapy, including non prescription medication on a regular basis apart from vitamin/mineral supplements
  • Smoking history for recent 3 months
  • Use of medication within 7 days prior to the study. If this situation arises inclusion of an otherwise suitable volunteer may be at the discretion of the investigator
05

Study design

Phase
Phase 1
Allocation
Randomized
Intervention model
Parallel assignment
Masking
None (open label)
Enrollment
12 participants (actual)

Study arms

  • Active comparator
    haloperidol

    0.5, 1, 3 mg of haloperidol will be administered orally every 24 hours for 7 days to 4 healthy subjects in each dose level (a total of 12 subjects). Dose groups are as follows; D2-receptor occupancy study Group Single Oral Dose No. of subjects 1. 0.5 mg 4 2. 1 mg 4 3. 5 mg 4

    Drug: haloperidol, PET

Interventions

  • Drughaloperidol, PET

    1. Biodistribution study Intravenous 18F haloperidol(10 mCi) Dose injection two times before whole body PET scan 2. D2-receptor occupancy study Group Doses No. of subjects 1 0.5 mg 4 2 1 mg 4 3 3 mg 4 above doses will be administrated orally every 24 hours for 7 days.

06

What researchers measure

Primary outcomes

  1. plasma haloperidol concentration

    Time frame: day 1 0h (predose), day 1 6h, day 2 0h, day 3 0h (predose), day 5 0h (predose), and day 7 0h (predose), 0.5, 1, 2, 4, 6, 8, 12, 24(day 8 0h), 48(day 9 0h), 72h (day 10h)

07

Study locations

1 site
  • Asan Medical Center
    Seoul, 138-736, Korea, Republic of
08

Updates

Tracking since Sep 25, 2026
No changes since tracking began. The registry record was last updated on Jul 11, 2013, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
09

Registry details

Key details

Study ID
NCT01193621
Lead sponsor
Asan Medical Center
Collaborators
Seoul National University Hospital
Responsible party
Kyun-Seop Bae (Associate Professor, Asan Medical Center) — Principal investigator
First posted
Sep 2, 2010
Start date
Jan 2008
Primary completion
Jul 2010
Completion
Jan 2012
Last update
Jul 11, 2013

Oversight

Data monitoring committee
No
View the source record on ClinicalTrials.gov ↗

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This study is completed, as verified in Jul 2013. You cannot join it, but the record below documents what was studied.

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