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To evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of single intravenous doses of KL0011034 injection in healthy volunteers.
This trial is a randomized, double-blind, placebo- and active-controlled, single-dose escalation study in healthy volunteers. A total of 76 volunteers will be enrolled. Healthy volunteers will be randomly assigned to receive KL0011034 injection, placebo, or Etomidate Injectable Emulsion. Each volunteer is allowed to participate in only one dose cohort; intra-volunteer dose escalation is not permitted. Enrollment into the next cohort will begin only after safety and tolerability data from the previous cohort have been reviewed and deemed acceptable by the investigator(s) and sponsor. If the highest dose is well tolerated, the investigator(s) and sponsor will evaluate the accumulated data and decide whether to terminate dose escalation or continue to higher dose levels.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| KL0011034 injection group | Experimental | Volunteers will receive KL0011034 injection in different doses. |
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| KL0011034 injection placebo group | Placebo Comparator | Volunteers will receive KL0011034 injection placebo. |
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| Etomidate Injectable Emulsion group | Active Comparator | Volunteers will receive Etomidate Injectable Emulsion. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| KL0011034 injection | Drug | Intravenous injection, single dose |
| |
| Measure | Description | Time Frame |
|---|---|---|
| Number of reported Adverse Events | Safety and tolerability was assessed by the number of volunteers with adverse events. | From first dose of drug until day 2 |
| Measure | Description | Time Frame |
|---|---|---|
| PK parameter Cmax in plasma | Maximum peak plasma concentration (Cmax) after single dose. | From first dose of drug until day 2 |
| PK parameter Tmax in plasma | Time of Cmax (Tmax) after single dose. PK parameters will be assessed for plasma KL0011034 and its metabolite(s) . |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Role | Phone | Extension | |
|---|---|---|---|---|
| Wei Qi | Contact | 028-82339360 | qiw@kelun.com |
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| The Third XIANGYA Hospital of Central South University | Recruiting | Changsha | Hunan | 410205 | China |
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| Placebo |
| Drug |
Intravenous injection, single dose |
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| Etomidate Injectable Emulsion | Drug | Intravenous injection, single dose |
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| From first dose of drug until day 2 |
| PK parameter AUC0-t in plasma | Area under the concentration-time curve (AUC0-t) from time zero to time "t" after single dose. PK parameters will be assessed for plasma KL0011034 and its metabolite(s) . | From first dose of drug until day 2 |
| PK parameter AUC0-∞ in plasma | AUC from time zero to infinity (AUC0-∞) after single dose. PK parameters will be assessed for plasma KL0011034 and its metabolite(s) . | From first dose of drug until day 2 |
| PK parameter t1/2 in plasma | Terminal-phase elimination half-life (t1/2) after single dose. PK parameters will be assessed for plasma KL0011034 and its metabolite(s) . | From first dose of drug until day 2 |
| Modified Observer's Assessment of Alertness Sedation (MOAA/S) scale | MOAA/S is a commonly used clinical sedation assessment scale, ranging from 0 to 5, which helps clinicians determine the level of sedation in patients. A score of 5 indicates full consciousness, whereas a score of 0 indicates deep coma. Lower scores correspond to deeper levels of sedation. | From first dose of drug until 10 minutes after fully alert on day 1. |
| Electroencephalogram bispectrality index (BIS) monitoring | BIS is the most widely used method for the continuous monitoring of sedation depth in clinical anesthesia. BIS values range from 0 to 100, where 100 represents complete wakefulness and 0 indicates complete cortical electrical inhibition. | From first dose of drug until 10 minutes after fully alert on day 1. |
| Loss of eyelash reflex | The eyelash reflex is a commonly used clinical method to assess the level of consciousness in patients. Gentle stimulation of the eyelashes with a cotton swab normally elicits a blink; absence of this response indicates loss of the eyelash reflex. | From first dose of drug until the reflex was fully restored on day 1. |
| Modified Aldrete Scoring (Aldrete) Scale | The Modified Aldrete Score is the most widely used standardized tool for assessing discharge readiness from post-anesthesia care unit (PACU). It evaluates five parameters: activity, respiration, blood pressure consciousness, and SpO2. Ranging from 0 to 10, the higher the score, the better the quality of recovery. | From being fully alert until meeting the discharge criteria to leave the unit on day 1. |