TABLE 2.
Published studies of remimazolam trials in human volunteers. NA = not available/applicable, PK = pharmacokinetics, PD = pharmacodynamics, iv = intravenous, ECG = electrocardiogram. N = number of subjects. *Note that the doses appear to represent the molecular weight of the salt and not to been corrected to base in these studies (Zhou et al., 2018).
| Trial ID | N | Endpoints | Salt | Dose | Route | Infusion duration | Co-treatment | Comparator | Ref |
|---|---|---|---|---|---|---|---|---|---|
| CNS 7056-001 | 81 | Safety, PK, PD | Besylate | 0.01–0.3 mg/kg | iv | 1 min | NA | Placebo, midazolam | Antonik et al. (2012); Wiltshire et al. (2012) |
| CNS 7056-002 (A) | 6 | Flumazenil reversal | Besylate | 0.25 mg/kg | iv | 1 min | Flumazenil | Placebo | Worthington et al. (2013) |
| CNS 7056-002 (B) | 45 | Colonoscopy: Safety, efficacy | Besylate | 0.04–0.1 mg/kg + top-ups | iv | 1 min | Fentanyl | NA | Worthington et al. (2013) |
| ONO-2745-01 | 42 | Safety, PK, PD | Besylate | 0.05–0.5 mg/kg | iv | 1 min | NA | NA | Doi, (2014) |
| ONO-2745-02 | 10 | Safety, PK, PD | Besylate | 1 mg/kg/h | iv | Up to 60 min | NA | NA | Doi, (2014) |
| ChiCTR 1800015185 | 62 | Safety, PK, PD | Besylate | 0.025–0.4 mg/kg | iv | 1 min | NA | Placebo, midazolam | Sheng et al., (2020) |
| ChiCTR 1800015186 | 12 | Safety, PK, PD | Besylate | 0.2 mg/kg then 1 mg/kg/h | iv | 1 min, 2 h | NA | Midazolam | Sheng et al., (2020) |
| NCT01970072 | 79 | Safety, PK, PD | Tosylate | 0.01–0.45 mg/kg* | iv | 1 min | NA | Placebo, midazolam | Chen et al., (2020b) |
| NCT03444480 | 8 | Flumazenil reversal | Tosylate | 0.4 mg/kg then 1.5 mg/kg/h* | iv | 1 min, 2 h | Flumazenil | NA | Chen et al., (2020b) |
| EudraCT 2017-000455-12 | 20 | PK, PD | Besylate | 5 mg/min, 3 mg/min, 1 mg/min | iv | 5, 15, 15 min | NA | NA | Schüttler et al. (2020) |
| NCT03329014 | 12 | Safety, PK, PD | Besylate | 10–40 mg | Nasal | NA | NA | Placebo, iv remimazolam | Pesic et al., (2020a) |
| NCT04113564 | 14 | Safety, PK, PD | Besylate | 0.14 mg/kg | Oral | NA | NA | iv remimazolam | Pesic et al. (2020b) |
| NCT04113343 Part1 | 21 | Safety, PK, PD | Besylate | 60–480 mg | Oral | NA | NA | NA | Pesic et al. (2020b) |
| NCT04113343 Part2 | 11 | Safety, PK, PD | Besylate | 360 mg | Oral | NA | Alcohol | NA | Pesic et al., (2020b) |
| NCT04110535 | 40 | Abuse potential | Besylate | 5–10 mg | iv | 1 min | NA | Placebo, midazolam | Schippers et al. (2020) |
| CNS 7056-005 | 57 | ECG | Besylate | 10–20 mg | iv | 1 min | NA | Midazolam, moxifloxacin, placebo | Kleiman et al. (2020) |
| EudraCT 2017-000455-12 | 20 | ECG | Besylate | 5 mg/min, 3 mg/min, 1 mg/min | iv | 5, 15, 15 min | NA | Placebo | Kleiman et al. (2020) |