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.
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.
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.
Females who are pregnant, lactating, or have plans to become pregnant during the study
Parallel
HYR-PB21， 100 mg
DrugHYR-PB21， 100 mg, administered as a single subcutaneous injection.
HYR-PB21， 200 mg
DrugHYR-PB21 200 mg, administered as a single subcutaneous injection.
HYR-PB21， 400 mg
DrugHYR-PB21 400 mg, administered as a single subcutaneous injection.
Bupivacaine hydrochloride， 100 mg (as base)
DrugBupivacaine Hydrochloric acid injection 100 mg (expressed as bupivacaine base), administered as a single subcutaneous injection. Active comparator.
Maximum observed plasma concentration(Cmax) of bupivacaine
The maximum observed plasma concentrations of bupivacaine was directly obtained from the observed concentration-time curves. Units: ng/mL. The PK parameters will be analyzed using the non-partial model. For ease of statistical comparison, the Cmax values will be log-transformed.
Maximum observed plasma concentration(Cmax) of pamoic acid
The maximum observed plasma concentrations of pamoic acid was directly obtained from the observed concentration-time curves. Units: ng/mL. The PK parameters will be analyzed using the non-partial model. For ease of statistical comparison, the Cmax values will be log-transformed.
Area Under the Curve(AUC0-t) of bupivacaine
During the period from time zero (the administration time) to Tlast (the last time point when the concentration reaches or exceeds the quantitative lower limit), the area under the plasma concentration-time curve of bupivacaine was calculated according to the mixed logarithmic linear trapezoidal rule. Unit: ng·hour/mL.
Area Under the Curve(AUC0-t) of pamoic acid
During the period from time zero (the administration time) to Tlast (the last time point when the concentration reaches or exceeds the quantitative lower limit), the area under the plasma concentration-time curve of pamoic acid was calculated according to the mixed logarithmic linear trapezoidal rule. Unit: ng·hour/mL.
Number of participants with abnormal laboratory tests results, abnormal vital signs,abnormal ECG readings, abnormal physical examination findings
Laboratory tests include hematology (e.g., hemoglobin, white blood cell count, platelet count), blood chemistry (e.g., Alanine Aminotransferase, Aspartate Aminotransferase, total bilirubin, creatinine, glucose), urinalysis, and coagulation (e.g., Prothrombin Time, Activated Partial Thromboplastin Time). Vital signs include sitting systolic/diastolic blood pressure, pulse rate, respiratory rate, and body temperature. Abnormal is defined as a value outside the institutional reference range. Clinically significant abnormal values will also be summarized separately, defined as CTCAE Grade ≥1 . Values are summarized as number (%) of participants.
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Fruithy Holdings Limited
Lead sponsor
Frontage Clinical Services
Collaborator
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