Remimazolam – anaesthetic/sedative

Remimazolam is an innovative short-acting general anaesthetic/sedative that is being developed by PAION initially for use in minor medical interventions (procedural sedation). Sedatives are used, for example, in endoscopic procedures such as colonoscopies. After intra­venous administration to over 300 human volunteers/patients in the course of the clinical trials performed, Remimazolam has clearly shown a controllable sedative effect with rapid onset and offset. This means that the patient can be selectively sedated for the duration of the intervention and rapidly regains full consciousness after the procedure. The rapid offset of the effect of the substance is due to its metabolism by tissue esterase enzymes that are widely distributed throughout the body.

Remimazolam has additional potential in anaesthesia, which is the initial indication being developed by PAION’s partner Ono Pharmaceutical Co., Ltd. (Ono) for the Japanese market. Furthermore, Remimazolam could also be used as a sedative during artificial respira­tion in the Intensive Care Unit (ICU).

The clinical studies performed with Remimazolam comprise two Phase I and two Phase II studies with single or multiple dose without an intervention or during endoscopy of the upper gastrointestinal tract or the colon.

The generated data indicate a good tolerability of Remimazolam. A rapid onset and offset of the sedative effect was observed during the procedures. It was also shown that it is possible to achieve the same (safety) or better (efficacy) results with single or multiple dosing of Remima­zolam as compared to single or multiple dosing of the gold standard Midazolam. The effect of Remimazolam can be reversed by the benzodiazepine antagonist Flumazenil.

Based on the results of the Phase IIb study, the optimal dose regimens for Phase III studies can now be defined.

The substance was added to PAION's portfolio by acquiring CeNeS who in turn had acquired the substance from GlaxoSmithKline. In 2007 Ono was granted the rights to develop and market Remimazolam for the Japanese market. In this co-operation, data and information are continually shared so that each party benefits from the development progress of the other party.

PAION is currently in discussions with potential licence partners to advance the develop­ment of Remimazolam, preferably for multiple indications, as quickly as possible as well as to prepare for subsequent commercialisation.