Safety, Pharmacokinetics, and Pharmacodynamics of Continuous KL0011034 Infusion in Healthy Chinese Adults

NCT07841626 | Not Yet Recruiting Phase 1

• 1 other identifier: KL0011034-103
• Study Type: interventional
• Target: 30
• Locations: 0 countries
• Sites: N/A

Brief Summary

This Phase 1 study will evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of continuous intravenous infusion of KL0011034 Injection in healthy Chinese adults. Approximately 30 participants will be enrolled in three sequential infusion-duration cohorts (1, 2, and 3 hours; 10 participants per cohort). Within each cohort, participants will be randomized in a 4:1 ratio to KL0011034 Injection or active-control propofol for anesthesia maintenance. All participants will receive propofol 2 mg/kg for anesthesia induction. Safety, pharmacokinetic, pharmacodynamic, recovery, and anesthesia-satisfaction assessments will be performed through 24 hours after dosing. Progression to the next infusion-duration cohort will occur only after the preceding cohort is considered safe and tolerable.

Conditions

Healthy Participants Study; General Anesthesia

Keywords

KL0011034; Continuous Intravenous Infusion; General Anesthesia; Pharmacokinetics; Pharmacodynamics; Bispectral Index; Healthy Participants

Outcome Measures

Primary Outcomes (17)

• Adverse Events and Serious Adverse Events

  Incidence, severity, seriousness, relationship, and outcome of adverse events and serious adverse events.

  From informed consent through Day 2 discharge/early termination; unresolved adverse events are followed as specified in the protocol.

• Physical Examination Findings

  Number of participants with clinically significant changes or abnormalities in physical examination findings.

  Screening, Day -2 as applicable, Day -1, Day 2/end-of-study, and early termination.

• Holter Monitoring Findings

  Clinically significant abnormalities detected by protocol-specified Holter monitoring.

  Time-matched baseline on Day -1; Day 1 from infusion start through 24 hours after infusion at protocol-specified time points (infusion start; 30 minutes, 1, 2, 3 hours after start; 2, 10, 30 minutes, 1, 4, 12, 24 hours after completion).

• Plasma Cortisol Concentration

  Plasma cortisol concentration (measured in nmol/L) assessed by protocol-specified laboratory testing.

  Screening (Day -14 to Day -2) at 07:00-08:00, 16:00 , and 00:00; time-matched baseline on Day -1; on Day 1, pre-dose, at 30 minutes, 1 hour, 2 hours, 3 hours, 4 hours, and 8 hours after infusion start, and at 16:00 and 00:00; and on Day 2 at 08:00.

• Plasma Adrenocorticotropic Hormone Concentration

  Plasma adrenocorticotropic hormone (ACTH) concentration (measured in pg/mL) assessed by protocol-specified laboratory testing.

  Screening (Day -14 to Day -2) at 07:00-08:00, 16:00 , and 00:00; time-matched baseline on Day -1; on Day 1, pre-dose, at 30 minutes, 1 hour, 2 hours, 3 hours, 4 hours, and 8 hours after infusion start, and at 16:00 and 00:00; and on Day 2 at 08:00.

• Blood Pressure

  Change from baseline in blood pressure (systolic and diastolic, measured in mmHg) assessed by standard vital sign measurement.

  Day 1: pre-dose; during infusion at 30 minutes, 1, 2, 3 hours; post-infusion at 30 minutes, 1, 2, 4, 8, 12, 24 hours; and at early termination.

• Pulse Rate

  Change from baseline in pulse rate (measured in beats per minute) assessed by standard vital sign measurement.

  Day 1: pre-dose; during infusion at 30 minutes, 1, 2, 3 hours; post-infusion at 30 minutes, 1, 2, 4, 8, 12, 24 hours; and at early termination.

• Respiratory Rate

  Change from baseline in respiratory rate (measured in breaths per minute) assessed by standard vital sign measurement.

  Day 1: pre-dose; during infusion at 30 minutes, 1, 2, 3 hours; post-infusion at 30 minutes, 1, 2, 4, 8, 12, 24 hours; and at early termination.

• Body Temperature

  Change from baseline in tympanic body temperature (measured in degrees Celsius) assessed by standard vital sign measurement.

  Day 1: pre-dose; during infusion at 30 minutes, 1, 2, 3 hours; post-infusion at 30 minutes, 1, 2, 4, 8, 12, 24 hours; and at early termination.

• Oxygen Saturation (SpO2)

  Change from baseline in oxygen saturation (measured as percentage of oxygen saturation) assessed by pulse oximetry.

  Day 1: pre-dose; during infusion at 30 minutes, 1, 2, 3 hours; post-infusion at 30 minutes, 1, 2, 4, 8, 12, 24 hours; and at early termination.

• Heart Rate

  Change from baseline in heart rate (measured in beats per minute) assessed by 12-lead electrocardiogram.

  Pre-dose (within 1 hour before anesthesia induction); after completion of continuous infusion at 30 minutes (±5 minutes), 2 hours (±10 minutes), 4 hours (±10 minutes), 8 hours (±15 minutes), and 24 hours (±20 minutes); and at early termination.

• PR Interval

  Change from baseline in PR interval (measured in milliseconds) assessed by 12-lead electrocardiogram.

  Pre-dose (within 1 hour before anesthesia induction); after completion of continuous infusion at 30 minutes (±5 minutes), 2 hours (±10 minutes), 4 hours (±10 minutes), 8 hours (±15 minutes), and 24 hours (±20 minutes); and at early termination.

• Change From Time-Matched Baseline in Plasma Cortisol Concentration

  Change from time-matched baseline in plasma cortisol concentration (measured in nmol/L) assessed by protocol-specified laboratory testing.

  Screening (Day -14 to Day -2) at 07:00-08:00, 16:00 , and 00:00; time-matched baseline on Day -1; on Day 1, pre-dose, at 30 minutes, 1 hour, 2 hours, 3 hours, 4 hours, and 8 hours after infusion start, and at 16:00 and 00:00; and on Day 2 at 08:00.

• QRS Interval

  Change from baseline in QRS interval (measured in milliseconds) assessed by 12-lead electrocardiogram.

  Pre-dose (within 1 hour before anesthesia induction); after completion of continuous infusion at 30 minutes (±5 minutes), 2 hours (±10 minutes), 4 hours (±10 minutes), 8 hours (±15 minutes), and 24 hours (±20 minutes); and at early termination.

• QT Interval

  Change from baseline in QT interval (measured in milliseconds) assessed by 12-lead electrocardiogram.

  Pre-dose (within 1 hour before anesthesia induction); after completion of continuous infusion at 30 minutes (±5 minutes), 2 hours (±10 minutes), 4 hours (±10 minutes), 8 hours (±15 minutes), and 24 hours (±20 minutes); and at early termination.

• QTcF Interval

  Change from baseline in QT interval corrected using Fridericia's formula (measured in milliseconds) assessed by 12-lead electrocardiogram.

  Pre-dose (within 1 hour before anesthesia induction); after completion of continuous infusion at 30 minutes (±5 minutes), 2 hours (±10 minutes), 4 hours (±10 minutes), 8 hours (±15 minutes), and 24 hours (±20 minutes); and at early termination.

• Change From Time-Matched Baseline in Plasma Adrenocorticotropic Hormone Concentration

  Change from time-matched baseline in plasma adrenocorticotropic hormone (ACTH) concentration (measured in pg/mL) assessed by protocol-specified laboratory testing.

  Screening (Day -14 to Day -2) at 07:00-08:00, 16:00 , and 00:00; time-matched baseline on Day -1; on Day 1, pre-dose, at 30 minutes, 1 hour, 2 hours, 3 hours, 4 hours, and 8 hours after infusion start, and at 16:00 and 00:00; and on Day 2 at 08:00.

Secondary Outcomes (48)

• Maximum Plasma Concentration (Cmax) of KL0011034

  pre-induction and pre-maintenance; during infusion at 5, 10, 20, 30, and 45 minutes and 1, 2, or 3 hours as applicable; after infusion at 2, 5, 10, 20, 30, and 40 minutes and 1, 2, 4, 8, 12, and 24 hours.

• Time to Maximum Plasma Concentration (Tmax) of KL0011034

  Pre-induction and pre-maintenance; during infusion at 5, 10, 20, 30, and 45 minutes and 1, 2, or 3 hours as applicable; after infusion at 2, 5, 10, 20, 30, and 40 minutes and 1, 2, 4, 8, 12, and 24 hours.

• Area Under the Curve From Time Zero to the Last Quantifiable Concentration (AUC0-t) of KL0011034

  Pre-induction and pre-maintenance; during infusion at 5, 10, 20, 30, and 45 minutes and 1, 2, or 3 hours as applicable; after infusion at 2, 5, 10, 20, 30, and 40 minutes and 1, 2, 4, 8, 12, and 24 hours.

• Area Under the Curve From Time Zero Extrapolated to Infinity (AUC0-∞) of KL0011034

  Pre-induction and pre-maintenance; during infusion at 5, 10, 20, 30, and 45 minutes and 1, 2, or 3 hours as applicable; after infusion at 2, 5, 10, 20, 30, and 40 minutes and 1, 2, 4, 8, 12, and 24 hours.

• Area Under the Curve From Time Zero to 24 Hours (AUC0-24h) of KL0011034

  Pre-induction and pre-maintenance; during infusion at 5, 10, 20, 30, and 45 minutes and 1, 2, or 3 hours as applicable; after infusion at 2, 5, 10, 20, 30, and 40 minutes and 1, 2, 4, 8, 12, and 24 hours.

Study Arms (6)

Cohort 1: KL0011034, 1-Hour Infusion

EXPERIMENTAL

Participants receive propofol injectable emulsion 2 mg/kg IV for induction, followed by KL0011034 Injection at a recommended maintenance rate of 1.1 mg/kg/hour for 1 hour. The rate may be adjusted to maintain BIS 40-60 within protocol limits.

Drug: KL0011034 Injection

Cohort 1: Propofol, 1-Hour Infusion

ACTIVE COMPARATOR

Participants receive propofol injectable emulsion 2 mg/kg IV for induction, followed by propofol injectable emulsion at 4-12 mg/kg/hour for 1 hour. The rate may be adjusted to maintain BIS 40-60.

Drug: Propofol Injectable Emulsion

Cohort 2: KL0011034, 2-Hour Infusion

EXPERIMENTAL

Participants receive propofol injectable emulsion 2 mg/kg IV for induction, followed by KL0011034 Injection at a recommended maintenance rate of 1.1 mg/kg/hour for 2 hours. The rate may be adjusted to maintain BIS 40-60 within protocol limits.

Drug: KL0011034 Injection

Cohort 2: Propofol, 2-Hour Infusion

ACTIVE COMPARATOR

Participants receive propofol injectable emulsion 2 mg/kg IV for induction, followed by propofol injectable emulsion at 4-12 mg/kg/hour for 2 hours. The rate may be adjusted to maintain BIS 40-60.

Drug: Propofol Injectable Emulsion

Cohort 3: KL0011034, 3-Hour Infusion

EXPERIMENTAL

Participants receive propofol injectable emulsion 2 mg/kg IV for induction, followed by KL0011034 Injection at a recommended maintenance rate of 1.1 mg/kg/hour for 3 hours. The rate may be adjusted to maintain BIS 40-60 within protocol limits.

Drug: KL0011034 Injection

Cohort 3: Propofol, 3-Hour Infusion

ACTIVE COMPARATOR

Participants receive propofol injectable emulsion 2 mg/kg IV for induction, followed by propofol injectable emulsion at 4-12 mg/kg/hour for 3 hours. The rate may be adjusted to maintain BIS 40-60.

Drug: Propofol Injectable Emulsion

Interventions

KL0011034 Injection DRUG

Intravenous maintenance infusion at a recommended rate of 1.1 mg/kg/hour for 1, 2, or 3 hours according to assigned cohort. The investigator may adjust the rate to maintain BIS 40-60; any upward adjustment must remain within the protocol-defined maximum rate of 2.5 mg/kg/hour.

Cohort 1: KL0011034, 1-Hour Infusion; Cohort 2: KL0011034, 2-Hour Infusion; Cohort 3: KL0011034, 3-Hour Infusion

Propofol Injectable Emulsion DRUG

All participants receive 2 mg/kg intravenously over 1 minute (±5 seconds) for anesthesia induction. In active-comparator arms, maintenance propofol is infused at a suggested rate of 4-12 mg/kg/hour for 1, 2, or 3 hours according to assigned cohort, adjustable to maintain BIS 40-60.

Cohort 1: Propofol, 1-Hour Infusion; Cohort 2: Propofol, 2-Hour Infusion; Cohort 3: Propofol, 3-Hour Infusion

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Participants who fully understand the purpose, content, procedures, and possible risks of the study, voluntarily agree to participate, and sign the informed consent form.
• Healthy male or female participants aged 18 to 45 years, inclusive, at the time of informed consent.
• Body weight ≥50.0 kg for males and ≥45.0 kg for females; body mass index 19.0 to 26.0 kg/m², inclusive.
• From informed consent through 3 months after completion of study-drug infusion, the participant and partner have no reproductive plans and the participant has no sperm or egg donation plans; the participant agrees to use at least one non-pharmacologic contraceptive method through the last pharmacokinetic sample and effective contraception through 3 months after infusion.
• Able to communicate well with the investigator and willing and able to comply with protocol-specified lifestyle restrictions and complete study procedures.

You may not qualify if:

• Known allergy to etomidate, propofol, or other anesthetic drugs; allergic constitution (for example, allergy to two or more drugs, foods, or pollen); tendency to rash or urticaria; history of allergic disease; or known allergy to the active ingredient or excipients of KL0011034 Injection.
• History of clinically significant cardiovascular, endocrine, respiratory, gastrointestinal, urinary, neurologic, hematologic, lymphatic, or psychiatric disease that remains clinically significant at screening in the investigator's judgment.
• History of anesthesia accident, serious anesthesia-related adverse reaction, or family history of anesthesia accident.
• Difficult ventilation, suspected difficult airway, or anticipated difficult tracheal intubation, including Modified Mallampati Class III-IV, congenital small mouth with macroglossia, mandibular hypoplasia, or similar findings.
• History of airway disease before or at screening, including bronchial asthma, chronic obstructive pulmonary disease, or sleep apnea syndrome.
• History of adrenocortical insufficiency, adrenal tumor, hereditary disorder of heme biosynthesis, or hereditary acute porphyria.
• Clinically significant abnormal findings in physical examination, vital signs, posteroanterior chest radiograph, abdominal ultrasonography, hematology, urinalysis, blood chemistry, coagulation, or infectious-disease screening; or clinically significant abnormal overall circadian pattern of cortisol and/or ACTH at screening in the investigator's judgment.
• Clinically significant electrocardiogram abnormality at screening, including QTcF ≥450 ms in males or ≥460 ms in females.
• Pregnant or breastfeeding female, or a woman of childbearing potential with a positive pregnancy test during screening.
• Unprotected sexual intercourse within 2 weeks before dosing.
• History of drug abuse or drug dependence within 1 year before screening, or positive urine drug screen at screening.
• History of alcohol abuse within 6 months before screening, defined as more than 14 standard units per week (1 unit = 360 mL beer, 45 mL of 40% spirits, or 150 mL wine); positive breath alcohol test; or unwillingness to abstain from alcohol and alcohol-containing products during the study.
• Smoking ≥5 cigarettes per day within 6 months before screening; unwillingness to stop using tobacco products during the study; or positive smoking test at screening.
• Habitual consumption of more than 8 cups per day (1 cup = 250 mL) of tea, coffee, or caffeine-containing beverages, or unwillingness to abstain from these beverages during the study.
• Consumption of grapefruit-rich foods or beverages within 48 hours before first dosing.

Sponsors & Collaborators

• Hunan Kelun Pharmaceutical Co., Ltd.: collaborator
• Sichuan Kelun Pharmaceutical Research Institute Co., Ltd.: collaborator
• The Third Xiangya Hospital of Central South University: lead

Central Study Contacts

Jie Huang

CONTACT

+86 731 8991 8665; cellahuang1988@163.com

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: TRIPLE
• Who Masked: PARTICIPANT, INVESTIGATOR, OUTCOMES ASSESSOR
• Purpose: OTHER
• Intervention Model: PARALLEL
• Sponsor Type: OTHER
• Responsible Party: PRINCIPAL INVESTIGATOR
• PI Title: Professor of Clinical Pharmacology

Study Record Dates

• First Submitted: August 31, 2026
• First Posted: September 25, 2026
• Study Start (Estimated): November 6, 2026
• Primary Completion (Estimated): September 5, 2027
• Study Completion (Estimated): September 5, 2027
• Last Updated: September 25, 2026

Record last verified: 2026-09

Data Sharing

• IPD Sharing: Will not share