Single-Dose Phase 0 Exploratory Pharmacokinetic Clinical Trial Comparing Five Oral Formulations of SR13668, an Orally Active AKT Pathway Inhibitor
PRIMARY OBJECTIVES:
I. Determine which oral formulation of Akt inhibitor SR13668 provides the best
bioavailability in normal, healthy volunteers.
SECONDARY OBJECTIVES:
I. Determine the oral pharmacokinetics of a single, low dose of Akt inhibitor SR13668 in
healthy volunteers.
II. Characterize the metabolism of Akt inhibitor SR13668 in healthy volunteers. III. Collect
preliminary safety data for Akt inhibitor SR13668 in healthy volunteers.
OUTLINE:
STAGE 1 (for the first 6 participants enrolled in the study [closed to accrual as of August,
2009]): Participants are randomized to 1 of 2 arms.
ARM I: Participants complete an overnight fast of ≥ 10 hours, eat a high-fat (approximately
50% of total caloric content of the meal) and high-calorie (approximately 800-1,000
calories), and then receive a single dose of oral SR13668 in a PEG400/Labrasol® liquid
formulation with 8 ounces of water. Participants may not eat for ≥ 4 hours after study drug
administration.
ARM II: Participants complete an overnight fast of ≥ 10 hours and then receive a single dose
of oral SR13668 in a PEG400/Labrasol® liquid formulation with 8 ounces of water.
Participants may not eat for ≥ 4 hours after study drug administration.
STAGE 2 (for the next 12 participants enrolled in the study): The preferred dietary
condition (Arm I) identified in stage 1 is used. Participants are randomized to 1 of 4 arms.
ARM III: Participants receive a single dose of oral Akt inhibitor SR13668 in a Solutol®
self-emulsifying solid dispersion capsule formulation.
ARM IV: Participants receive a single dose of oral Akt inhibitor SR13668 in a
Solutol®/vitamin E TGPS self-emulsifying solid dispersion capsule formulation.
ARM V: Participants receive a single dose of oral Akt inhibitor SR13668 in a vitamin E TGPS
self-emulsifying solid dispersion capsule formulation.
ARM VI: Participants receive a single dose of oral Akt inhibitor SR13668 in a Myrj 53
self-emulsifying solid dispersion capsule formulation.
Blood and urine samples are collected at baseline and periodically during the 24 hours after
study drug administration for pharmacokinetic analysis by high performance liquid
chromatography assay.
After completion of study treatment, participants are followed by telephone at 7-10 days and
at 30 days.
Interventional
Allocation: Randomized, Endpoint Classification: Pharmacokinetics Study, Intervention Model: Parallel Assignment, Masking: Open Label, Primary Purpose: Treatment
Food effect on the bioavailability of SR13668 after oral administration
The first stage will be used to compare fed vs. fasted diet effect on the pharmacokinetics parameters under formulation 1.
Up to 30 days after completion of study treatment
No
Paul Limburg
Principal Investigator
Mayo Clinic
United States: Food and Drug Administration
NCI-2009-01106
NCT00896207
June 2009
Name | Location |
---|---|
Mayo Clinic | Rochester, Minnesota 55905 |