A Phase 1 interventional study of Remimazolam Besylate in Chronic Kidney Diseases and Renal Transplantation, sponsored by Qianfoshan Hospital. Recruiting at 1 site in China. Open to participants aged 18 Years to 65 Years. Per ClinicalTrials.gov, last updated 2025-10-01.
Sponsored by Qianfoshan Hospital · Phase 1, Interventional, and Treatment
The goal of this clinical trial is to evaluate the pharmacokinetics (PK) and pharmacodynamics (PD) of remimazolam (CNS 70754) in healthy adult participants. The main questions it aims to answer are:
What are the key pharmacokinetic parameters of remimazolam, including peak concentration (Cmax), time to peak concentration (Tmax), area under the curve (AUC), and elimination half-life (T1/2)? What is the effect of remimazolam on consciousness, as measured by the MOAA/S scale and Narcotrend monitoring during anesthesia? Researchers will compare the pharmacokinetic and pharmacodynamic effects of remimazolam to see if the drug provides consistent and predictable sedation without significant adverse effects.
Participants will:
Receive continuous Infusion of Remimazolam. Have blood samples taken at various time points to measure plasma concentrations and calculate PK parameters.
Be monitored for consciousness and sedation levels using the MOAA/S scale and Narcotrend.
Undergo safety assessments, including laboratory tests, vital signs monitoring, and physical examinations throughout the study.
This study will help determine the drug's behavior in the body and its impact on sedation, providing valuable information for its future clinical use in anesthesia and other medical applications.
Last updated on December 22, 2024
3,144 studies on the registry are indexed under Renal Insufficiency, Chronic; 704 are open to participants now.
This study's planned enrollment of 30 is below the median of 74 across 2,176 interventional studies indexed under Renal Insufficiency, Chronic.
Browse Renal Insufficiency, Chronic studies →Qianfoshan Hospital is the lead sponsor of 140 studies on the registry; 73 are open to participants now.
Counted across the registry records on this site, refreshed daily.
Inclusion Criteria Signed informed consent
Age ≥18 years and \<65 years
Chronic renal failure scheduled for renal transplantation
Body mass index (BMI) 18-30 kg/m² (inclusive)
Weight ≥50 kg (males) or ≥45 kg (females)
ASA physical status classification III or IV
Exclusion Criteria Hepatic, psychiatric, or neurological disorders
Coagulopathy
Heart failure
Respiratory failure
Long-term sedative or antidepressant use
Pregnancy or lactation
Inability to communicate or cooperate
Participation in other drug/device trials within 3 months prior
Positive hepatitis B surface antigen (HBsAg)
Positive hepatitis C antibody (HCV-Ab)
Positive HIV antibody
Positive syphilis antibody
Use of hepatic enzyme inhibitors/inducers within 30 days prior (per Appendix 1)
Known hypersensitivity to ≥2 substances
Alcohol consumption >14 units/week within 6 months prior*
Drug abuse history within 3 months prior
Major infection/trauma within 1 month prior
Gastrointestinal surgery affecting drug absorption within 1 month prior
Vaccination within 1 month prior or planned during study
Blood loss/donation >400 mL within 3 months prior
Blood transfusion within 1 month prior
INR >1.5, PT >ULN+4 seconds, or APTT >15×ULN
Significant bleeding history within 3 months prior
Current anticoagulant therapy
Any condition deemed unsuitable by investigator
All enrolled participants receive a standardized Remimazolam Besylate-based anesthesia protocol for renal transplant surgery, as follows: 1. Intervention Drug: ◦ Remimazolam Besylate (Trade name: Rymazol®), supplied as a lyophilized powder (25 mg/vial) reconstituted with sterile water. 2. Dosing Regimen: * Induction: Continuous IV infusion at 6 mg/kg/h until loss of consciousness (defined as MOAA/S score ≤1). * Maintenance: Titrated IV infusion (0.5-2 mg/kg/h) to maintain target anesthesia depth (Narcotrend Index: 27-60) until end of surgery. 3. Ancillary Medications (per protocol §7.2): * Analgesia: Sufentanil (0.4-0.5 μg/kg induction; 10 μg at peritoneum closure) + Remifentanil infusion intraoperatively. * Muscle Relaxant: Rocuronium (0.6 mg/kg induction; 0.15 mg/kg bolus PRN). * Immunosuppression: Methylprednisolone 750 mg + Furosemide 60 mg pre-reperfusion. * Prohibited Agents: Sevoflurane, propofol, midazolam, dexmedetomidine, or etomidate. 4. Depth Monitoring: * Real-time Narcot
Drug: Remimazolam Besylate
This is the first clinical trial evaluating Remimazolam's pharmacokinetics (PK), pharmacodynamics (PD), and safety in renal transplant recipients-a population with unique physiological alterations due to end-stage renal disease and graft reperfusion. Key differentiators include: Population-Specific Dosing Protocol: Induction: 6 mg/kg/h until MOAA/S ≤1 (vs. 5-12 mg/kg/h in general surgery). Maintenance: Titrated (0.5-2 mg/kg/h) to Narcotrend Index 27-60 (lower than typical BIS 40-60 targets), accounting for altered drug metabolism post-transplant. Transplant-Specific Context: Administered alongside standard immunosuppressants (methylprednisolone 750 mg + furosemide 60 mg at reperfusion) but prohibits common sedatives (midazolam/propofol) to isolate Remimazolam's effects. PK/PD sampling accounts for graft function dynamics (e.g., blood draws during reperfusion and post-op days 1-6). Exploratory Genetic Analysis: First study linking VDR/
Remimazolam Plasma Concentration
Blood concentration (ng/mL) of Remimazolam
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes, hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes.
Remimazolam PK Parameters
Maximum Plasma Concentration
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes, hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes.
Remimazolam PK Parameters
Area Under the Curve (0 to last measurable t)
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes , hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes
Remimazolam PK Parameters
Area Under the Curve (0 to infinity)
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes , hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes
Remimazolam PK Parameters
Time to Cmax
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes , hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes
Remimazolam PK Parameters
Terminal Elimination Half-Life
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes , hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes
Remimazolam PK Parameters
Total Body Clearance
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes , hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes
Remimazolam PK Parameters
Renal Clearance
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes , hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes
Remimazolam PK Parameters
Apparent Volume of Distribution (Terminal)
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes , hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes
Remimazolam PK Parameters
Mean Residence Time
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes , hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes
Remimazolam PK Parameters
Percentage of AUC Extrapolated
Time frame: Pre-infusion, 2/5/10/20/30/45/60/120 minutes , hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes
CNS 7054 (Metabolite) PK Parameters
Maximum Plasma Concentration
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes, hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes.
CNS 7054 (Metabolite) PK Parameters
Area Under the Curve (0 to last measurable t)
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes, hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes.
CNS 7054 (Metabolite) PK Parameters
Area Under the Curve (0 to infinity)
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes, hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes.
CNS 7054 (Metabolite) PK Parameters
Time to Cmax
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes, hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes.
CNS 7054 (Metabolite) PK Parameters
Terminal Elimination Half-Life
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes, hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes.
CNS 7054 (Metabolite) PK Parameters
Mean Residence Time
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes, hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes.
CNS 7054 (Metabolite) PK Parameters
Percentage of AUC Extrapolated
Time frame: During surgery: Pre-infusion, 2/5/10/20/30/45/60/120 minutes, hourly until infusion stop; Post-infusion: 0/5/15/30/60/90/120/240 minutes.
Sedation Depth (PD)
MOAA/S score (0 to 5) + Narcotrend Index (NCI 0 to 100)
Time frame: Induction: every 1minutes until MOAA/S≤1; Maintenance: every 10 minutes; Recovery: every 2 minutes until 3 consecutive MOAA/S=5.
Time to Loss of Consciousness (MOAA/S ≤1)
Time from infusion start to first MOAA/S score ≤1
Time frame: 0 to 10 minutes after infusion start
Time to Full Alertness (3 consecutive MOAA/S=5)
Time from infusion stop to sustained alertness
Time frame: Time from infusion stop to sustained alertness
Narcotrend Index (NCI) Values
Anesthesia depth index (0-100 scale)
Time frame: Continuous monitoring during infusion + 30 min post-stop
Postoperative Urine Output
24-hour urine volume
Time frame: Postoperation Days 1 to 6
Serum Creatinine Level
Blood creatinine concentration
Time frame: Preoperation, Postoperation Days 1 to 6
Estimated Glomerular Filtration Rate
Kidney filtration rate
Time frame: Preoperation, Postoperation Days 1 to 6
Intraoperative Hypotension Incidence
MAP \<65 mmHg for \>1 minute
Time frame: Intra-operative period
Intraoperative Bradycardia Incidence
HR \<45 bpm for \>1 min
Time frame: Intra-operative period
Injection Pain Incidence
Participant-reported pain during drug administration
Time frame: During induction (0 to 10 minutes)
Postoperative Nausea/Vomiting Incidence
Postoperative Nausea/Vomiting occurrence
Time frame: PACU admission to Postoperation Day 6
Postoperative Agitation Incidence
RASS score ≥2
Time frame: PACU stay (0 to 2 hours)
Delayed Recovery Incidence
Extubation time \>30 min post-surgery
Time frame: End of surgery to PACU discharge
Intraoperative Awareness Incidence
Positive Brice questionnaire response
Time frame: Upon PACU discharge (Day 1)
VDR Genotype Effect on Remimazolam Maximum Plasma Concentration
Correlation of VDR polymorphisms with peak concentration
Time frame: Pre-dose (Day 1)
CYP3A Genotype Effect on Remimazolam Area Under the Curve (0 to last measurable t)
Correlation of CYP3A polymorphisms with total exposure
Time frame: Pre-dose (Day 1)
POR Genotype Effect on Remimazolam Clearance
Correlation of POR polymorphisms with systemic clearance
Time frame: Pre-dose (Day 1)
VDR Genotype Effect on CNS 7054 Terminal Elimination Half-Life
Correlation of VDR polymorphisms with metabolite half-life
Time frame: Pre-dose (Day 1)
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Qianfoshan Hospital