Pharmacokinetic and Safety Study of HYR-PB21 vs Bupivacaine Hydrochloric Acid in Healthy Participants

Starting soon · Phase 1

Conditions studied: Postoperative Analgesia

In brief

This is a Phase I, randomized, single-blind, active-controlled, single-dose, parallel-group study to evaluate the safety and pharmacokinetic (PK) profile of HYR-PB21, a pamoate-formulated bupivacaine injectable, in healthy adult participants. Participants are randomized to receive a single subcutaneous dose of HYR-PB21 at one of three dose levels (100 mg, 200 mg, or 400 mg) or a single 100 mg dose of Bupivacaine hydrochloride injection (as base) as active control. The primary objectives are to characterize the PK profile of HYR-PB21 at the three dose levels compared with Bupivacaine hydrochloride, and to determine the Pharmacokinetics characteristics of the pamoic acid moiety following HYR-PB21 administration. Secondary objectives are to extend cumulative safety and tolerability observations of single subcutaneous doses of HYR-PB21 in healthy adults.

Key facts

Study ID

NCT07717086

Run by

Fruithy Holdings Limited

People needed

28

Starts

2026-07-01

Expected to finish

2026-10-01

Last updated by the study team

2026-07-21

Who can join

Age: 18 and older, up to 50. Sex: any. Healthy volunteers: accepted.

You may qualify if…

• Healthy male or female adult participants
• Age 18 to 50 years old (inclusive)
• Body mass index (BMI) of 18.0 to 32.0 kg/m2 and weight ≥50 kg.
• Participant is generally healthy, as determined by the Investigator based on medical history, physical examination, clinical laboratory test results, vital signs, and 12-lead electrocardiogram (ECG) at screening.
• Additional Detailed Inclusion Criteria Include:
• Female participants who engage in heterosexual intercourse must be non-pregnant or non-lactating. Female participants of childbearing potential must agree to use 2 acceptable methods of contraception with their male partner from screening until 6 months after the last dose of the study drug and refrain from donating ovum for this same period. (Refer to contraception section).Females of non-childbearing potential must either be :
• Post menopausal as defined by at least 12 months of consecutive Amenorrhea and Follicle-Stimulating Hormone(FSH) and estradiol confirming Post menopausal status at screening. See Appendix Section 13 for additional details.
• Surgically sterile at least 6 months prior to screening with documentation.
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• Bilateral tubal ligation
• Hysterectomy (partial or total)
• Bilateral salpingectomy
• Bilateral oophorectomy
• Male participants, if sexually active with a female partner of child-bearing potential, must be vasectomized or agree to take appropriate precautions to prevent conception, including practicing an effective method of contraception, and must not donate sperm from screening through 12 weeks following administration of the last dose of study medication.
• Only non-smokers are eligible. For a period of at least six months prior to Screening, all participants must have been free from excessive alcohol intake or regular use of illegal recreational drugs. Participants with any past or current history of marijuana use are not eligible for the study.
• Ability to understand and willingness to sign a written informed consent form (The consent form must be signed by the participant prior to any study-specific procedures.)
• Willingness and able to comply with catheter placement and blood draws throughout the course of study and comply with study procedures and follow-up examination.

You may not qualify if…

• Participants will be excluded if they have
• A history of hypersensitivity or idiosyncratic reactions to amide-type local anesthetics;
• Have a personal or family history of clotting disorder or hematologic abnormality, such as excessive bleeding, joint hematoma, thrombovascular disease, thrombocytopenia, or any chronic condition requiring treatment with transfusions; have a history of recurrent bleeding episodes (eg, epistaxis, bruising or gingival bleeding) within 1 month prior to Screening, or a longstanding history of such bleeding.
• Participants who were detected to have Glucose-6-phosphate dehydrogenase(G6PD) deficiency during the screening period.
• Additional detailed exclusion criteria include:
• Females who are pregnant, lactating, or have plans to become pregnant during the study
• History and/or recent evidence within six months prior to Screening of alcohol or drug/substance abuse disorder
• History of clinically significant allergies, including drug allergies, or allergic bronchial asthma, or related bronchospastic conditions
• Participants who have a history of unexplained syncope or fainting or a condition that predisposes them to syncope, such as hypotension, orthostatic hypotension, bradycardia, or dehydration.
• Participants who have used P-gp and/or Cytochrome P450 hepatic microsomal enzyme-inducing or inhibiting drugs (e.g., propafenone, voriconazole, fluconazole, cimetidine) within 30 days of first dosing, refer to Appendix 15-16 for detailed list
• Participants with a history or presence of significant cardiovascular, pulmonary, hepatic, gallbladder or biliary tract, renal, hematologic, gastrointestinal, endocrine, immunologic, dermatologic, neurologic, psychiatric disease, or active sexually transmitted disease to include:
• Current or history of thrombosis or thromboembolic disorders
• Any history of malignancy, especially breast cancer or other hormone-sensitive cancers
• Undiagnosed abnormal vaginal bleeding unrelated to pregnancy
• Cholestatic jaundice of pregnancy
• Liver tumors, benign or malignant, or active liver disease
• Uncontrolled hypertension
• History or evidence of acute or chronic respiratory disorders, including but not limited to chronic obstructive pulmonary disease (COPD) or asthma
• History or presence of significant cardiovascular abnormalities, including, without limitation, severe bradycardia, sick sinus syndrome, second- or third-degree atrial ventricular block, long QT syndrome, cardiogenic shock, and decompensated heart failure
• Participant family history of sudden cardiac death or long QT syndrome and baseline QT prolongation >450 for males and >470 for females at screening
• Participants with estimated glomerular filtration rate (eGFR - utilizing Chronic Kidney Disease Epidemiology Collaboration formula) < 80 mL/min/1.73 m2; participants with slightly lower values may be included upon agreement between the sponsor medical representative and the Principal Investigator at screening
• Participants meeting any of the following laboratory criteria will be excluded:
• Screening total bilirubin > 1.3 mg/dL; participants with a documented history of Gilbert's syndrome can be enrolled if the direct bilirubin is < 0.4 mg/dL
• Screening alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP) > upper limits of normal (ULN)
• Screening platelets < 140,000/microliter

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