A Study to Evaluate the Drug-Drug Interaction Between KL0011034 Injection and Alfentanil Hydrochloride Injection in Participants With Moderate-to-Severe Non-Cancer Chronic Pain

NCT07751094 | Not Yet Recruiting Phase 1

• 1 other identifier: KL0011034-102
• Study Type: interventional
• Target: 27
• Locations: 0 countries
• Sites: N/A

Brief Summary

This study will evaluate the drug-drug interaction between KL0011034 Injection and Alfentanil Hydrochloride Injection in participants with moderate-to-severe non-cancer chronic pain. The study consists of two parts. Part 1 is a single-center, randomized, open-label, parallel-design study to evaluate the safety, tolerability, and pharmacodynamics of the combination. Approximately 9 participants will be enrolled and randomized to one of three dose groups (n=3 per group). Part 2 is a single-center, randomized, open-label, three-sequence, three-period crossover study to evaluate the pharmacokinetic interaction, safety, tolerability, and pharmacodynamic effects. Approximately 18 participants will be enrolled and randomized to one of three sequences (n=6 per sequence), with a 3-day washout period between each period.

Conditions

Chronic Pain

Keywords

Drug-Drug Interaction; KL0011034; Alfentanil; Pharmacokinetics; Non-Cancer Chronic Pain

Outcome Measures

Primary Outcomes (9)

• Maximum Plasma Concentration (Cmax) of KL0011034

  Cmax of KL0011034 in plasma, determined by non-compartmental analysis of concentration-time data.

  Part 2, each of the 3 treatment periods (Day 1, Day 4, Day 7): pre-dose (within 60 minutes before dosing); immediately after infusion completion, and at 2, 5, 10, 15, 20, 30, 40, 50 minutes, and 1, 2, 4, 8, 12, 24 hours

• Maximum Plasma Concentration (Cmax) of KL0011034 Metabolite A644S(A)-Z7

  Cmax of KL0011034 major metabolite A644S(A)-Z7 in plasma, determined by non-compartmental analysis of concentration-time data.

  Part 2, each of the 3 treatment periods (Day 1, Day 4, Day 7): pre-dose (within 60 minutes before dosing); immediately after infusion completion, and at 2, 5, 10, 15, 20, 30, 40, 50 minutes, and 1, 2, 4, 8, 12, 24 hours post-dose.

• Maximum Plasma Concentration (Cmax) of Alfentanil

  Cmax of Alfentanil in plasma, determined by non-compartmental analysis of concentration-time data.

  Part 2, each of the 3 treatment periods (Day 1, Day 4, Day 7): pre-dose (within 60 minutes before dosing); immediately after bolus completion, and at 1, 2, 3, 6, 11, 16, 21, 31, 41, 51, 61 minutes, and 2, 4, 8, 12, 24 hours post-dose.

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

  AUC0-t of KL0011034 in plasma, determined by non-compartmental analysis using linear-log trapezoidal method.

  Part 2, each of the 3 treatment periods (Day 1, Day 4, Day 7): pre-dose (within 60 minutes before dosing); immediately after infusion completion, and at 2, 5, 10, 15, 20, 30, 40, 50 minutes, and 1, 2, 4, 8, 12, 24 hours

• Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUC0-t) of KL0011034 Metabolite A644S(A)-Z7

  AUC0-t of KL0011034 major metabolite A644S(A)-Z7 in plasma, determined by non-compartmental analysis using linear-log trapezoidal method.

  Part 2, each of the 3 treatment periods (Day 1, Day 4, Day 7): pre-dose (within 60 minutes before dosing); immediately after infusion completion, and at 2, 5, 10, 15, 20, 30, 40, 50 minutes, and 1, 2, 4, 8, 12, 24 hours

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

  AUC0-t of Alfentanil in plasma, determined by non-compartmental analysis using linear-log trapezoidal method.

  Part 2, each of the 3 treatment periods (Day 1, Day 4, Day 7): pre-dose (within 60 minutes before dosing); immediately after infusion completion, and at 2, 5, 10, 15, 20, 30, 40, 50 minutes, and 1, 2, 4, 8, 12, 24 hours

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

  AUC0-∞ of KL0011034 in plasma, calculated as AUC0-t + Clast/λz.

  Part 2, each of the 3 treatment periods (Day 1, Day 4, Day 7): pre-dose (within 60 minutes before dosing); immediately after infusion completion, and at 2, 5, 10, 15, 20, 30, 40, 50 minutes, and 1, 2, 4, 8, 12, 24 hours

• Area Under the Curve From Time Zero Extrapolated to Infinity (AUC0-∞) of KL0011034 Metabolite A644S(A)-Z7

  AUC0-∞ of KL0011034 major metabolite A644S(A)-Z7 in plasma, calculated as AUC0-t + Clast/λz.

  Part 2, each of the 3 treatment periods (Day 1, Day 4, Day 7): pre-dose (within 60 minutes before dosing); immediately after infusion completion, and at 2, 5, 10, 15, 20, 30, 40, 50 minutes, and 1, 2, 4, 8, 12, 24 hours

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

  AUC0-∞ of Alfentanil in plasma, calculated as AUC0-t + Clast/λz.

  Part 2, each of the 3 treatment periods (Day 1, Day 4, Day 7): pre-dose (within 60 minutes before dosing);immediately after infusion completion, and at 2, 5, 10, 15, 20, 30, 40, 50 minutes, and 1, 2, 4, 8, 12, 24 hours

Secondary Outcomes (30)

• Time to Maximum Plasma Concentration (Tmax) of KL0011034

  Part 2, each of the 3 treatment periods (Day 1, Day 4, Day 7): pre-dose (within 60 minutes before dosing); immediately after infusion completion, and at 2, 5, 10, 15, 20, 30, 40, 50 minutes, and 1, 2, 4, 8, 12, 24 hours post-dose.

• Time to Maximum Plasma Concentration (Tmax) of KL0011034 Metabolite A644S(A)-Z7

  Part 2, each of the 3 treatment periods (Day 1, Day 4, Day 7): pre-dose (within 60 minutes before dosing); immediately after infusion completion, and at 2, 5, 10, 15, 20, 30, 40, 50 minutes, and 1, 2, 4, 8, 12, 24 hours post-dose.

• Time to Maximum Plasma Concentration (Tmax) of Alfentanil

  Part 2, each of the 3 treatment periods (Day 1, Day 4, Day 7): pre-dose (within 60 minutes before dosing); immediately after bolus completion, and at 1, 2, 3, 6, 11, 16, 21, 31, 41, 51, 61 minutes, and 2, 4, 8, 12, 24 hours post-dose.

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

  Part 2, each of the 3 treatment periods (Day 1, Day 4, Day 7): pre-dose (within 60 minutes before dosing); immediately after infusion completion, and at 2, 5, 10, 15, 20, 30, 40, 50 minutes, and 1, 2, 4, 8, 12, 24 hours post-dose.

• Area Under the Curve From Time Zero to 24 Hours (AUC0-24h) of KL0011034 Metabolite A644S(A)-Z7

  Part 2, each of the 3 treatment periods (Day 1, Day 4, Day 7): pre-dose (within 60 minutes before dosing); immediately after infusion completion, and at 2, 5, 10, 15, 20, 30, 40, 50 minutes, and 1, 2, 4, 8, 12, 24 hours post-dose.

Study Arms (6)

1.Alfentanil 5 µg/kg + KL0011034 0.3 mg/kg

EXPERIMENTAL

Part 1: Participants receive a single dose of Alfentanil Hydrochloride Injection 5 μg/kg combined with KL0011034 Injection 0.3 mg/kg on Day 1. Safety, tolerability, and pharmacodynamic evaluations are conducted.

Drug: KL0011034 injection; Drug: Alfentanil Hydrochloride Injection

2.Alfentanil 5 µg/kg + KL0011034 0.35 mg/kg

EXPERIMENTAL

Part 1: Participants receive a single dose of Alfentanil Hydrochloride Injection 5 μg/kg combined with KL0011034 Injection 0.35 mg/kg on Day 1. Safety, tolerability, and pharmacodynamic evaluations are conducted.

Drug: KL0011034 injection; Drug: Alfentanil Hydrochloride Injection

3.Alfentanil 5 µg/kg + KL0011034 0.4 mg/kg

EXPERIMENTAL

Part 1: Participants receive a single dose of Alfentanil Hydrochloride Injection 5 μg/kg combined with KL0011034 Injection 0.4 mg/kg on Day 1. Safety, tolerability, and pharmacodynamic evaluations are conducted.

Drug: KL0011034 injection; Drug: Alfentanil Hydrochloride Injection

4.Sequence A: KL0011034 → Alfentanil → Alfentanil + KL0011034

EXPERIMENTAL

Part 2, Sequence A: Participants receive three interventions across three periods (Day 1, Day 4, Day 7) with a 3-day washout between periods: Period 1: KL0011034 Injection (selected dose from Part 1); Period 2: Alfentanil Hydrochloride Injection 5 μg/kg; Period 3: Alfentanil Hydrochloride Injection 5 μg/kg + KL0011034 Injection (selected dose from Part 1). Pharmacokinetic, pharmacodynamic, and safety evaluations are conducted.

Drug: KL0011034 injection; Drug: Alfentanil Hydrochloride Injection

5. Sequence B: Alfentanil → Alfentanil + KL0011034 → KL0011034

EXPERIMENTAL

Part 2, Sequence B: Participants receive three interventions across three periods (Day 1, Day 4, Day 7) with a 3-day washout between periods: Period 1: Alfentanil Hydrochloride Injection 5 μg/kg; Period 2: Alfentanil Hydrochloride Injection 5 μg/kg + KL0011034 Injection (selected dose from Part 1); Period 3: KL0011034 Injection (selected dose from Part 1). Pharmacokinetic, pharmacodynamic, and safety evaluations are conducted.

Drug: KL0011034 injection; Drug: Alfentanil Hydrochloride Injection

6. Sequence C: Alfentanil + KL0011034 → KL0011034 → Alfentanil

EXPERIMENTAL

Part 2, Sequence C: Participants receive three interventions across three periods (Day 1, Day 4, Day 7) with a 3-day washout between periods: Period 1: Alfentanil Hydrochloride Injection 5 μg/kg + KL0011034 Injection (selected dose from Part 1); Period 2: KL0011034 Injection (selected dose from Part 1); Period 3: Alfentanil Hydrochloride Injection 5 μg/kg. Pharmacokinetic, pharmacodynamic, and safety evaluations are conducted.

Drug: KL0011034 injection; Drug: Alfentanil Hydrochloride Injection

Interventions

KL0011034 injection DRUG

KL0011034 Injection is an investigational drug being studied for its analgesic properties in combination with alfentanil. It is administered via intravenous infusion. The dose levels evaluated are 0.3 mg/kg, 0.35 mg/kg, and 0.4 mg/kg in Part 1; the selected dose from Part 1 is used in Part 2.

1.Alfentanil 5 µg/kg + KL0011034 0.3 mg/kg; 2.Alfentanil 5 µg/kg + KL0011034 0.35 mg/kg; 3.Alfentanil 5 µg/kg + KL0011034 0.4 mg/kg; 4.Sequence A: KL0011034 → Alfentanil → Alfentanil + KL0011034; 5. Sequence B: Alfentanil → Alfentanil + KL0011034 → KL0011034; 6. Sequence C: Alfentanil + KL0011034 → KL0011034 → Alfentanil

Alfentanil Hydrochloride Injection DRUG

Alfentanil Hydrochloride Injection is an opioid analgesic administered via intravenous bolus at a fixed dose of 5 μg/kg. It is used alone and in combination with KL0011034 Injection to evaluate drug-drug interaction.

1.Alfentanil 5 µg/kg + KL0011034 0.3 mg/kg; 2.Alfentanil 5 µg/kg + KL0011034 0.35 mg/kg; 3.Alfentanil 5 µg/kg + KL0011034 0.4 mg/kg; 4.Sequence A: KL0011034 → Alfentanil → Alfentanil + KL0011034; 5. Sequence B: Alfentanil → Alfentanil + KL0011034 → KL0011034; 6. Sequence C: Alfentanil + KL0011034 → KL0011034 → Alfentanil

Eligibility Criteria

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

You may qualify if:

• Those who fully understand the purpose, content, process and possible risks of the trial, and voluntarily participate and sign the informed consent form;
• Male and female patients with moderate to severe non-cancerous chronic pain (such as patients with shoulder inflammation, chronic back pain, myofascial pain syndrome) aged between 18 and 55 years (inclusive of the boundary values), with a NRS score of \>= 4;
• Male weight not less than 50.0 kg, female weight not less than 45.0 kg; Body Mass Index (BMI) within the range of 19.0 to 26.0 kg/m2 (including the critical value);
• From the date of signing the informed consent form to the last administration of the trial medication within 3 months, the trial participants (and their partners) have no plans for conception, and the trial participants have no plans for sperm donation/egg donation; From the date of signing the informed consent form to the completion of the exit examination, the participants voluntarily adopt non-pharmacological contraceptive measures; After the exit examination to the last 3 months after the last administration of the trial medication, the participants voluntarily adopt effective contraceptive measures;
• Able to communicate well with the researchers, willing and able to comply with the lifestyle restrictions stipulated in the protocol, and cooperate to complete the trial process.

You may not qualify if:

• Known to be allergic to alfentanil or other opioid analgesics, etomidate or other anesthetic drugs, or to be of allergic constitution (such as allergy to two or more drugs, food or pollen), or prone to develop rashes, urticaria, etc., or having a history of allergic diseases, or known to be allergic to the excipients or raw materials of this product;
• Having a history of head trauma, possible intracranial hypertension, cerebral aneurysm, cerebrovascular accident, or mental illness such as schizophrenia, mania, bipolar disorder, mental confusion, long-term use of psychotropic drugs or cognitive dysfunction;
• Having a history of serious cardiovascular diseases (such as hypertension, heart failure, severe arrhythmia, etc.) and/or heart diseases, family history of heart disease and/or unstable angina pectoris, or having had a myocardial infarction in the past 6 months;
• Having a history of other cardiovascular, endocrine, respiratory, digestive, urinary, nervous, hematological and/or lymphatic system diseases, and the investigator considers that it still has clinical significance during the screening;
• Having a history of anesthesia accidents, severe adverse reactions during anesthesia or family history of anesthesia accidents, or having contraindications for general anesthesia;
• Having difficulty breathing or suspected difficult airway or estimated difficulty in tracheal intubation (such as modified Mallampati score grade III-IV, congenital small tongue, maldevelopment of mandible, etc.);
• Having a history of airway diseases such as bronchial asthma, chronic obstructive pulmonary disease, sleep apnea syndrome, etc.;
• Having a history of adrenal insufficiency, adrenal tumor or hereditary hemoglobin biosynthesis disorder or hereditary acute porphyria;
• Having a surgical history within 3 months before screening, or not recovering from surgery, or having planned surgery during the trial;
• Having conditions, surgical history, diseases related to the use of the test drug, or any other special circumstances that may significantly affect drug absorption, distribution, metabolism and excretion;
• Abnormal results of physical examination, vital signs, full thoracic radiograph, abdominal B-ultrasound, laboratory tests (blood routine, urine routine, blood biochemistry, coagulation function) have clinical significance;
• Having clinically significant electrocardiogram abnormalities found during screening, such as QTcF \>=450 ms (male) or \>=460 ms (female), etc.;
• Positive for hepatitis B surface antigen (HBsAg), hepatitis C antibody (HCV-Ab), human immunodeficiency virus antibody (HIV-Ab), and syphilis spirochete antibody (TP-Ab);
• Having unprotected sexual behavior within 2 weeks before the first administration of the test drug;
• Female subjects during the screening period are in pregnancy or lactation, or have a positive pregnancy result;

Sponsors & Collaborators

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

MeSH Terms

Conditions

Chronic Pain

Interventions

Alfentanil

Condition Hierarchy (Ancestors)

Pain; Neurologic Manifestations; Signs and Symptoms; Pathological Conditions, Signs and Symptoms

Intervention Hierarchy (Ancestors)

Fentanyl; Piperidines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Central Study Contacts

Huang Jie

CONTACT

+86 731 8991 8665; cellahuang1988@163.com

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: OTHER
• Responsible Party: PRINCIPAL INVESTIGATOR
• PI Title: Professor of Clinical Pharmacology

Study Record Dates

• First Submitted: July 6, 2026
• First Posted: August 7, 2026
• Study Start: July 30, 2026
• Primary Completion (Estimated): July 31, 2027
• Study Completion (Estimated): July 31, 2027
• Last Updated: August 7, 2026

Record last verified: 2026-08

Data Sharing

• IPD Sharing: Will not share