Drug-Drug Interaction Potential of Remimazolam: CYP 450, Transporters, and Protein Binding

Title:Drug-Drug Interaction Potential of Remimazolam: CYP 450, Transporters, and Protein Binding

Volume: 25 Issue: 4

Author(s): Karl-Uwe Petersen*, Wolfgang Schmalix, Marija Pesic and Thomas Stöhr

Affiliation:

• Department Pharmacology, RWTH Aachen University, Aachen, Germany

Abstract:

Background: The ultra-short-acting benzodiazepine, remimazolam, is a new treatment modality for procedural sedation and general anesthesia. Its activity is terminated by carboxylesterase 1 (CES1).

Objective: The objective of this study was to determine the drug-drug interaction (DDI) potential of remi-mazolam through mechanisms unrelated to its metabolizing enzyme, CES1.

Methods: Conventional in vitro co-exposure experiments were conducted to study possible interactions of remimazolam and its primary metabolite, CNS7054, mediated by competitive binding to plasma protein or reactions with cytochrome P450 isoforms or drug transporters

Results: No relevant interactions of remimazolam or its metabolite with cytochrome P450 (CYP) isoforms at clinically relevant concentrations were identified. Likewise, standard experiments revealed no clinically relevant interactions with drug transporters and plasma proteins.

Conclusion: The present data and analyses suggest a very low potential of remimazolam for pharmacokinetic DDIs mediated by CYP isoforms, drug transporters, and protein binding.

Cite this article as:

Petersen Karl-Uwe*, Schmalix Wolfgang, Pesic Marija and Stöhr Thomas, Drug-Drug Interaction Potential of Remimazolam: CYP 450, Transporters, and Protein Binding, Current Drug Metabolism 2024; 25 (4) . https://dx.doi.org/10.2174/0113892002300657240521094732