A Phase I, Open Label Study to Assess the Effects of PQ912 on the Pharmacokinetics of Midazolam and Omeprazole in Healthy Male Subjects

NCT02190708 Phase 1 COMPLETED

Midazolam is a rapid-acting benzodiazepine, with a short half-life (approximately 1.9 hours) and is primarily metabolised by CYP3A. Omeprazole is a selective proton pump inhibitor substrate used to reduce gastric acid secretion. Omeprazole is primarily metabolised by CYP2C19. Midazolam and omeprazole are both used as probe drugs in clinical pharmacology studies to evaluate clinical CYP3A and CYP2C19 drug interactions, respectively. Furthermore the EMA and the FDA guidance on drug interactions recommend the use of these drugs for such evaluations. The aim of this study is to assess the effect of PQ912 on the PK of midazolam and omeprazole. In vitro studies have demonstrated that PQ912 inhibits several CYP enzymes, including CYP3A4 and CYP2C19 and at the expected exposure levels in patients, has the potential to inhibit these enzymes in-vivo. This study is therefore planned to investigate the potential changes in the PK of midazolam and omeprazole due to the effect of PQ912 at steady-state. In clinical practice it is likely that co-administration of PQ912 with other drugs that are metabolised via the CYP3A and/or CYP2C19 enzymes will occur. This study will provide important information for the requirement of dose adjustments or contraindications in these circumstances.

Details

Lead sponsor	Vivoryon Therapeutics N.V.
Phase	Phase 1
Status	COMPLETED
Enrolment	18
Start date	2014-06
Completion	2014-08

Conditions

• Healthy Volunteers
• Pharmacologic Action

Interventions

• PQ912
• Midazolam
• Omeprazole

Primary outcomes

• Effect of PQ912 at steady state on pharmacokinetic profile of Omeprazole and Midazolam — from day 1 up to day 6
  Serial blood samples on day 1 and day 6 from predose up to 24 hours postdose

Countries

United Kingdom