Safety, Tolerability, and Pharmacokinetics of Single, Escalating Oral Doses of RTI-336 in Healthy, Male Subjects
This is the first study to be conducted in humans for RTI-336, a new chemical entity, with evaluations focusing on the safety, tolerability, and pharmacokinetics of RTI-336 following administration of single, oral doses. RTI-336 is a novel dopamine transporter inhibitor of the 3-phenyltropane class, and is currently being developed by RTI International as a potential pharmacotherapy to treat cocaine dependence. Data from this study will be used to plan and define dose ranges for subsequent studies.
|Study Design:||Allocation: Randomized
Endpoint Classification: Pharmacokinetics Study
Intervention Model: Single Group Assignment
Masking: Double Blind (Subject, Caregiver, Investigator, Outcomes Assessor)
Primary Purpose: Basic Science
|Official Title:||A Double-Blind, Placebo-Controlled Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single, Escalating Oral Doses of RTI-336 in Healthy, Male Subjects|
- Safety and tolerability of RTI-336; clinical signs and symptoms, adverse events (AEs), vital signs, electrocardiographic (ECG) parameters, clinical laboratory test results [ Time Frame: Days 0 (Baseline), 1-3, and 8 ] [ Designated as safety issue: Yes ]
- Pharmacokinetic parameters of RTI-336 and metabolites [ Time Frame: 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, and 48 hours after dosing ] [ Designated as safety issue: Yes ]
|Study Start Date:||October 2008|
|Study Completion Date:||March 2009|
|Primary Completion Date:||March 2009 (Final data collection date for primary outcome measure)|
Drug: RTI-336 (CTDP 31862)
Cocaine abuse has been an epidemic in the United States since the mid- to late-1970s. It is hypothesized that a medication to treat cocaine addiction should have some, but not all, of the behavioral pharmacological properties of cocaine. Substantial evidence links the euphoric highs and addictive properties of cocaine to the inhibition of the dopamine transporter (DAT) in the brain. Cocaine binds quickly and potently to this transporter and blocks the presynaptic uptake of dopamine, resulting in subjective highs and reinforcing effects in both preclinical studies and humans. Compounds that mimic the DAT-binding properties of cocaine that are less stimulating and act with a slower receptor onset and offset may prove useful as treatment for cocaine dependence. The 3-phenyltropane analog, RTI-336, is a potent and selective DAT inhibitor that has demonstrated desirable pharmacological properties in preclinical species and is an appropriate compound to test for its potential as a medication to treat cocaine dependence.
This is the first study to be conducted in humans for RTI-336, a new chemical entity, with evaluations focusing on the safety, tolerability, and pharmacokinetics of RTI-336 following administration of single, oral doses, with the possibility of identifying the maximum tolerated dose in humans. Data from this study will be used to plan for and define dose ranges for subsequent studies.
|United States, Florida|
|Comprehensive Phase One|
|Miramar, Florida, United States, 33025|
|Principal Investigator:||William A. Gerson, DO, CPI||Comprehensive Phase One|