Pharmacodynamics

 

The PET studies evaluated specific binding of ¹¹C-CIT-FE in the striatum after administration of bupropion.  The mean dopamine transporter occupancy remained at approximately 26% at the 3 hour, 12 hour, and 24 hour time points after the last dose of bupropion, as shown in the figure below (provided by Sponsor).

 

 

 

 

The comparison between occupancy and plasma concentrations of bupropion or the CCV, shown below, demonstrate that although the plasma concentrations change over the 24 hour period, the occupancy remains relatively constant.

 

 

Pharmacogenetics

 

According to the Sponsor, no apparent relationships were observed between DAT and NET variants and dopamine transporter occupancy, and no apparent relationships were observed between bupropion and hydroxybupropion exposure and variants in the [blacked out] genes.  The Sponsor notes that the conclusions are limited by the small number of subjects in the study.

 

 

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