NCT03457597

Study in Healthy Subjects to Determine the Effect of Relacorilant on Exposure to Probe Substrates for Cytochrome P450s

A Phase 1, Open-Label, Single-Sequence Crossover Study in Healthy Subjects to Determine the Effect of Relacorilant on Exposure to Probe Substrates for Cytochrome P450s 3A4, 2C8, 2C9, 2C19, and 2D6

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 27 (actual)
• Sponsor: Corcept Therapeutics · Industry
• Sex: All
• Age: 18 Years – 65 Years
• Healthy volunteers: Accepted

Summary

This is an open-label, single-sequence, 3-period crossover study conducted in healthy subjects. Eligible subjects will participate in a single treatment period, in which they will receive the following treatments: Day 1, single doses of midazolam and metoprolol; Day 2, single doses of pioglitazone, tolbutamide, and omeprazole; Days 5 to 17, daily doses of relacorilant; Day 14, single doses of midazolam and metoprolol (with relacorilant); and, Day 15, single doses of pioglitazone, tolbutamide, and omeprazole (with relacorilant).

Detailed description

This is an open-label, single-sequence, 3-period crossover study conducted in healthy subjects. Subjects will be screened for eligibility for the study within 21 days before the first dose of study drug based on entrance criteria specified in Section 4. Eligible subjects will participate in a single treatment period, in which they will receive the following treatments: * Day 1: single doses of midazolam and metoprolol * Day 2: single doses of pioglitazone, tolbutamide, and omeprazole * Days 5 to 17: daily doses of relacorilant * Day 14: single doses of midazolam and metoprolol (with relacorilant) * Day 15: single doses of pioglitazone, tolbutamide, and omeprazole (with relacorilant) Blood samples will be collected before dosing and at intervals up to 24 hours after each midazolam dose, up to 48 hours after each metoprolol, tolbutamide, and omeprazole dose, and up to 72 hours after each pioglitazone dose for assay of the respective probe substrates and relevant metabolites. Additional samples will be collected during the relacorilant dosing period for assay of relacorilant and metabolites to confirm exposure and at the beginning (before dosing on Day 5) and near the end (Day 14) of the relacorilant dosing period for assay for 4β-OH cholesterol, a biomarker for CYP induction. Safety and tolerability will be monitored using AEs, clinical laboratory evaluations, 12-lead ECG recordings, vital sign and pulse oximetry measurements, and physical examinations. Subjects will be admitted to the Clinical Research Unit (CRU) on the morning of Day -1 following an 8-hour fast for baseline assessments and will remain confined until completion of procedures, 72 hours after the last dose of probe substrate and 24 hours after the last dose of relacorilant. Subjects may leave the CRU after safety review on the morning of Day 18. Each subject will have a follow-up (FU) visit 14 ± 2 days after the last dose of study drug.

Conditions

• Healthy

Interventions

Type	Name	Description
DRUG	Midazolam hydrochloride	Midazolam hydrochloride 2.5 mg
DRUG	Metoprolol tartrate	Metoprolol tartrate 100 mg
DRUG	Pioglitazone hydrochloride	Pioglitazone hydrochloride 15 mg
DRUG	Tolbutamide	Tolbutamide 500 mg
DRUG	Omeprazole	Omeprazole 20 mg
DRUG	Relacorilant	Relacorilant 350mg

Timeline

• Start date: 2018-03-06
• Primary completion: 2018-04-15
• Completion: 2018-04-28
• First posted: 2018-03-07
• Last updated: 2018-05-17

Locations

1 site across 1 country: United States

Regulatory

• FDA-regulated drug study