A Phase Ⅰa Study of Remimazolam Tosylate in Healthy Volunteers

NCT01970072 | Completed Phase 1 DMC

• 1 other identifier: RMZL-PIa
• Study Type: interventional
• Target: 79
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to evaluate and compare the Pharmacokinetics/Pharmacodynamics and safety of Remimazolam Tosylate with midazolam in healthy volunteers

Conditions

Healthy

Keywords

Remimazolam Tosylate; Phase Ⅰ study; Health

Outcome Measures

Primary Outcomes (3)

• To study the Pharmacokinetics of Remimazolam Tosylate by assessment of drug concentration through blood sample analysis

  Pre-dose to 8 hours post-dosee

• Bispectral index (BIS) and Modified Observer's Assessment of Alertness/Sedation(MOAA/S) score assessments

  Pre-dose to 2 hours post-dose

• Adverse event；Vital sign；Physical examination；Laboratory examination；ECG；The nervous system function test

  Pre-dose to 24 hours post-dose

Study Arms (11)

1.Remimazolam Tosylate

EXPERIMENTAL

Single IV bolus of Remimazolam Tosylate over 1 minute at 0.01 mg/kg body weight

Drug: Remimazolam Tosylate

2.Remimazolam Tosylate

EXPERIMENTAL

Single IV bolus of Remimazolam Tosylate over 1 minute at 0.02 mg/kg body weight

Drug: Remimazolam Tosylate

3.Remimazolam Tosylate

EXPERIMENTAL

Single IV bolus of Remimazolam Tosylate over 1 minute at 0.05 mg/kg body weight

Drug: Remimazolam Tosylate

4.Remimazolam Tosylate

EXPERIMENTAL

Single IV bolus of Remimazolam Tosylate over 1 minute at 0.075 mg/kg body weight

Drug: Remimazolam Tosylate

5.Remimazolam Tosylate

EXPERIMENTAL

Single IV bolus of Remimazolam Tosylate over 1 minute at 0.1 mg/kg body weight

Drug: Remimazolam Tosylate

6.Remimazolam Tosylate

EXPERIMENTAL

Single IV bolus of Remimazolam Tosylate over 1 minute at 0.15 mg/kg body weight

Drug: Remimazolam Tosylate

7.Remimazolam Tosylate

EXPERIMENTAL

Single IV bolus of Remimazolam Tosylate over 1 minute at 0.2 mg/kg body weight

Drug: Remimazolam Tosylate

8.Remimazolam Tosylate

EXPERIMENTAL

Single IV bolus of Remimazolam Tosylate over 1 minute at 0.25 mg/kg body weight

Drug: Remimazolam Tosylate

9.Remimazolam Tosylate

EXPERIMENTAL

Single IV bolus of Remimazolam Tosylate over 1 minute at 0.3mg/kg body weight

Drug: Remimazolam Tosylate

10.Remimazolam Tosylate

EXPERIMENTAL

Single IV bolus of Remimazolam Tosylate over 1 minute at 0.35 mg/kg body weight

Drug: Remimazolam Tosylate

11.Midazolam

ACTIVE COMPARATOR

Single IV bolus of Midazolam over 1 minute at 0.075 mg/kg body weight

Drug: Midazolam

Interventions

Remimazolam Tosylate DRUG

1.Remimazolam Tosylate; 10.Remimazolam Tosylate; 2.Remimazolam Tosylate; 3.Remimazolam Tosylate; 4.Remimazolam Tosylate; 5.Remimazolam Tosylate; 6.Remimazolam Tosylate; 7.Remimazolam Tosylate; 8.Remimazolam Tosylate; 9.Remimazolam Tosylate

Midazolam DRUG

11.Midazolam

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy males or females
• Weight range 50 to 100 kg inclusive
• Body mass index (BMI) 18 to 26 kg/m2

You may not qualify if:

• Has a known sensitivity to benzodiazepines, flumazenil, or anesthetic agents, or a medical condition such that these agents are contraindicated
• With evidence of uncontrolled renal, hepatic, central nervous system, respiratory, cardiovascular, or metabolic dysfunction, in the opinion of the investigator or medical monitor
• Has known or suspected history of alcoholism or drug abuse or misuse within 6 months of Screening or evidence of tolerance or physical dependence before dosing with study drug
• With a history of laboratory results that show the presence of hepatitis B surface antigen (HBs Ag), hepatitis C antibody (HCV Ab), or human immunodeficiency virus (HIV)
• Pregnant,lactating
• Mallampati score ≥3

Sponsors & Collaborators

• Jiangsu HengRui Medicine Co., Ltd.: lead

Study Sites (1)

Peking Union Medical College Hospital

Beijing, 100032, China

Location

Related Publications (2)

• Chen X, Sang N, Song K, Zhong W, Wang H, Jiang J, Huang Y, Hu P. Psychomotor Recovery Following Remimazolam-induced Sedation and the Effectiveness of Flumazenil as an Antidote. Clin Ther. 2020 Apr;42(4):614-624. doi: 10.1016/j.clinthera.2020.02.006. Epub 2020 Mar 13.

  PMID: 32178858 DERIVED

• Zhou Y, Hu P, Huang Y, Nuoer S, Song K, Wang H, Wen J, Jiang J, Chen X. Population Pharmacokinetic/Pharmacodynamic Model-Guided Dosing Optimization of a Novel Sedative HR7056 in Chinese Healthy Subjects. Front Pharmacol. 2018 Nov 19;9:1316. doi: 10.3389/fphar.2018.01316. eCollection 2018.

  PMID: 30510509 DERIVED

MeSH Terms

Interventions

4-methylbenzenesulfonic acid; Midazolam

Intervention Hierarchy (Ancestors)

Benzodiazepines; Benzazepines; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds

Study Officials

• Bei Hu, Professor

  Peiking Union Medical College Hospital

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Who Masked: PARTICIPANT, INVESTIGATOR
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: October 22, 2013
• First Posted: October 25, 2013
• Study Start: October 14, 2013
• Primary Completion: June 20, 2014
• Study Completion: June 20, 2014
• Last Updated: January 31, 2018

Record last verified: 2018-01

Locations

CN (1)