A Phase Ⅰb Study of Remimazolam Tosylate in Healthy Volunteers

NCT03444480 | Completed Phase 1

• 1 other identifier: RMZL-PIb
• Study Type: interventional
• Target: 8
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to evaluate the Pharmacokinetics/Pharmacodynamics and safety of Remimazolam Tosylate in healthy volunteers after loading/maintenance dose regimen.

Conditions

Anesthesia

Outcome Measures

Primary Outcomes (4)

• Peak Plasma Concentration (Cmax) of Remimazolam in human plasma.

  From prior to study drug injection until 4 hours post-dose

• Area under the plasma concentration versus time curve (AUC) of Remimazolam in human plasma.

  From prior to study drug injection until 4 hours post-dose

• Peak Plasma Concentration (Cmax) of M01 in human plasma.

  M01 is the main metabolite of Remimazolam

  From prior to study drug injection until 4 hours post-dose

• Area under the plasma concentration versus time curve (AUC) of M01 in human plasma.

  M01 is the main metabolite of Remimazolam

  From prior to study drug injection until 4 hours post-dose

Secondary Outcomes (1)

• Safety by measurement of Adverse Events.

  From start of study drug injection to patient discharge (approx. 2 days)

Study Arms (2)

Remimazolam Tosylate 1

EXPERIMENTAL

IV bolus of Remimazolam Tosylate with a loading dose of 0.4mg/kg body weight over 1 minute followed by a maintenance dose of 1.5mg/kg/h over 2 hours.1 h 55 min after dosing start， 0.5 mg Flumazenil is administered

Drug: Remimazolam Tosylate

Remimazolam Tosylate 2

EXPERIMENTAL

IV bolus of Remimazolam Tosylate with a loading dose of 0.4mg/kg body weight over 1 minute followed by a maintenance dose of 1.5mg/kg/h over 2 hours.1 h 55 min after dosing start time,0.5ml placebo is administered

Drug: Remimazolam Tosylate

Interventions

Remimazolam Tosylate DRUG

Initial dose plus supplemental doses

Also known as: HR7056

Remimazolam Tosylate 1; Remimazolam Tosylate 2

Eligibility Criteria

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

You may qualify if:

• Aged ≥18 and ≤55 years.
• Weight range 50 to 100 kg and body mass index (BMI) 18 to 26 kg/m2.
• Willing and able to comply with the requirements of the protocol.
• Provide written informed consent to participate in the study.

You may not qualify if:

• Abnormal results of physical or laboratory examination with clinical significance
• 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).
• With evidence of uncontrolled renal, hepatic, central nervous system, respiratory, cardiovascular, or metabolic dysfunction, in the opinion of the investigator or medical monitor.
• Subject with clinically significant abnormalities in baseline 12-lead electrocardiogram (ECG) or vital signs（SBP \<90 mmHg or \>140 mmHg，DBP \<50 mmHg or \>90 mmHg；Hr \<50 bpm or \>100 bpm；SpO2 \<95%）.
• Has a known sensitivity to benzodiazepines, flumazenil, or anesthetic agents, or a medical condition such that these agents are contraindicated.
• Receipt of other medication within 14 days of the first study day.
• Blood donation greater than 200 ml or participation in a clinical study of an unlicensed drug in the previous 3 months.
• History of smoking or alcohol abuse within 6 months of screening.
• History of grapefruit juice or any other foods affect the activity of cytochrome P450 3A4（CYP3A4） within 7 days of screening.
• Pregnant,lactating.
• Mallampati score ≥3.
• Patients who in the opinion of the investigator may not be able to comply with the requirements of the study are not eligible

Sponsors & Collaborators

• Jiangsu HengRui Medicine Co., Ltd.: lead

Study Sites (1)

Peking Union Medical College Hospital

Beijing, Beijing Municipality, 100032, China

Location

Related Publications (1)

• 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

MeSH Terms

Interventions

4-methylbenzenesulfonic acid

Study Officials

• Pei Hu

  Peking Union Medical College

  PRINCIPAL INVESTIGATOR

Study Design

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

Study Record Dates

• First Submitted: August 4, 2015
• First Posted: February 23, 2018
• Study Start: July 23, 2014
• Primary Completion: August 16, 2014
• Study Completion: August 16, 2014
• Last Updated: February 23, 2018

Record last verified: 2018-02

Locations

CN (1)