Remimazolam (CNS-7056) is a benzodiazepine derivative drug, developed by PAION, in collaboration with Japanese licensee Ono Pharmaceutical as an alternative to the short-acting imidazobenzodiazepine midazolam, for use in induction of anaesthesia and conscious sedation for minor invasive procedures. Remimazolam was found to be both faster acting and shorter lasting than midazolam, and human clinical trials showed a faster recovery time and predictable, consistent pharmacokinetics, suggesting some advantages over existing drugs for these applications.
Phase I and Ib dose-finding studies for procedural sedation with patients recovering faster from remimazolam than midazolam. Phase II trials comparing remimazolam to the standard anesthesia protocols for cardiac surgery and colonoscopy were presented at major conferences in October 2014.
A phase IIa trial comparing remimazolam to midazolam for upper endoscopy was published in December 2014, finding a similar safety profile. Remimazolam was originally discovered in the late 1990s at Glaxo Wellcome in their labs in Research Triangle Park, NC.
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^Antonik, Laurie J.; Goldwater, D. Ronald; Kilpatrick, Gavin J.; Tilbrook, Gary S.; Borkett, Keith M. (Aug 2012). "A placebo- and midazolam-controlled phase I single ascending-dose study evaluating the safety, pharmacokinetics, and pharmacodynamics of remimazolam (CNS 7056): Part I. Safety, efficacy, and basic pharmacokinetics". Anesth. Analg. 115 (2): 274–83. doi:10.1213/ANE.0b013e31823f0c28. PMID22190555.
^Worthington, Mark T.; Antonik, Laurie J.; Goldwater, D. Ronald; Lees, James P.; Wilhelm-Ogunbiyi, Karin; Borkett, Keith M.; Mitchell, Mack C. (Nov 2013). "A phase Ib, dose-finding study of multiple doses of remimazolam (CNS 7056) in volunteers undergoing colonoscopy". Anesth. Analg. 117 (5): 1093–100. doi:10.1213/ANE.0b013e3182a705ae. PMID24108261.
^Borkett, Keith M.; Riff, Dennis S.; Schwartz, Howard I.; Winkle, Peter J.; Pambianco, Daniel J.; Lees, James P.; Wilhelm-Ogunbiyi, Karin (Dec 11, 2014). "A Phase IIa, Randomized, Double-Blind Study of Remimazolam (CNS 7056) Versus Midazolam for Sedation in Upper Gastrointestinal Endoscopy". Anesthesia. 120 (4): 771–80. doi:10.1213/ANE.0000000000000548. PMID25502841.