6.2
Clinical Pharmacology and Biopharmaceutics Individual Study Reviews
6.2.1
PET
STUDY OF DOPAMINE TRANSPORTER OCCUPANCY
AN
OPEN LABEL POSITRON EMISSION TOMOGRAPHY STUDY TO EVALUATE DOPAMINE TRANSPORTER
OCCUPANCY, AS MEASURED BY C-ßCIT-FE FOLLOWING 150 MG WELLBUTRIN SR TWICE DAILY
FOR 8 DAYS IN HEALTHY MALE VOLUNTEERS
Study
Investigators and Site:
[blacked
out]
Protocol
Number: OHB10001
OBJECTIVES:
To
define the relationship between dopamine transporter occupancy and bupropion
(and metabolite(s)) concentration at steady state.
To
determine the time course of occupancy of bupropion (and metabolite(s)) at the
DA transporter using 11C-BCIT-FE at steady-state over 12 and 24
hours.
FORMULATIONS:
The
product used in OHB10001 was WELLBUTRIN SR 150 mg tablets (GlaxoSmithKline,
Inc.).
STUDY
DESIGN:
This
study was a multiple dose, 1 treatment, open-label study. Inclusion criteria included healthy
nonsmoking males, 18 to 55 years of age.
Exclusion criteria included previous participation in a PET study, use
of any prescription medication within four weeks of the Treatment Phase,
ingestion of alcohol or caffeine-containing food or beverage within 72 hours
prior to the first dose of study medication and throughout the treatment
period, and ingestion of OTC medications including vitamins and antacids within
72 hours before the first dose of study medication and continuing through study
completion.
Between
1 and 7 days prior to initial bupropion dosing, a baseline PET study was
performed with 300 MBq of 11C-labeled N-omega-fluoroalkyl-2
beta-carboyx-3-beta-(4-iodophenyl) nortropane ester (11C-ßCIT-FE). According to the Sponsor, 11C- ßCIT-FE
is widely used as a selective ligand for the dopamine transporter, and had
previously been shown to be displaced from the dopamine transporter by
bupropion in a dose-dependent fashion and was therefore
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