Pharmacokinetics and Bioequivalence Study of HMPL-523 Acetate Tablets in Humans

NCT07331194 | Completed Phase 1

• 1 other identifier: 2025-523-00CH1
• Study Type: interventional
• Target: 54
• Locations: 1 country
• Sites: 1

Brief Summary

Two formulations containing the same active pharmaceutical ingredient are considered bioequivalent if their relative bioavailability (rate and extent of drug absorption) falls within acceptable predetermined limits after administration at the same molar dose. Formulations with bioequivalence are considered to act comparably in vivo, i.e., similar in terms of safety and efficacy. This study aims to evaluate the pharmacokinetic (PK) profile and bioequivalence of the original and modified formulations of HMPL-523 acetate tablets in healthy participants to bridge the safety and efficacy of the modified formulation of HMPL 523 acetate tablets in humans.

Conditions

Healthy

Keywords

HMPL-523

Outcome Measures

Primary Outcomes (6)

• PK parameters

  area under the plasma concentration-time curve from 0 to the time point t when the last concentration can be accurately measured (AUC0-t)

  up to two months

• PK parameters

  area under the plasma concentration-time curve from 0 to infinity (AUC0-∞)

  up to two months

• PK parameters

  maximum concentration (Cmax)

  up to two months

• PK parameters

  time to maximum concentration (Tmax)

  up to two months

• PK parameters

  terminal elimination half-life (t1/2)

  up to two months

• The bioequivalence of two different drug product formulations of HMPL 523 acetate tablets

  It will be evaluated based on the area under the plasma concentration-time curve (AUC) and Cmax.

  up to two months

Secondary Outcomes (3)

• To compare the relative bioavailability of two different drug product formulations of 300 mg (100 mg/tablet × 3) HMPL-523 acetate tablets

  up to two months

• Adverse events (AEs)

  up to two months

• Laboratory tests

  up to two months

Study Arms (2)

TRTR

OTHER

Total 54 Chinese healthy participants are planned to be enrolled and randomly assigned to 2 dosing sequence groups (TRTR, and RTRT) in a 1:1 ratio and administered once per cycle, with a washout period of at least 7 days, where T is the test formulation (the modified formulation) and R is the reference formulation (the original formulation). the dose is 300mg for each cycle, and there were 4 cycles for each participant.

Drug: HMPL-523 Acetate Tablets (Test Formulation); Drug: HMPL-523 Acetate Tablets (Reference Formulation)

RTRT

OTHER

Total 54 Chinese healthy participants are planned to be enrolled and randomly assigned to 2 dosing sequence groups (TRTR, and RTRT) in a 1:1 ratio and administered once per cycle, with a washout period of at least 7 days, where T is the test formulation (the modified formulation) and R is the reference formulation (the original formulation). the dose is 300mg for each cycle, and there were 4 cycles for each participant.

Drug: HMPL-523 Acetate Tablets (Test Formulation); Drug: HMPL-523 Acetate Tablets (Reference Formulation)

Interventions

HMPL-523 Acetate Tablets (Test Formulation) DRUG

The trial participants were administered the drug on the first day of each cycle. dose 300mg

RTRT; TRTR

HMPL-523 Acetate Tablets (Reference Formulation) DRUG

The trial participants were administered the drug on the first day of each cycle. dose 300mg

RTRT; TRTR

Eligibility Criteria

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

You may qualify if:

• Trial participants must meet all of the following criteria for enrollment:
• Participants can communicate well with the investigator, must voluntarily sign the ICF and agree to comply with the requirements of the study protocol;
• Male and female healthy participants aged 18-45 years (inclusive);
• Body weight ≥ 45 kg (females) or ≥ 50 kg (males), body mass index (BMI) 19-26 kg/m2 (inclusive);
• Study participants must commit to using highly effective contraception for both themselves and their sexual partners during the study, and for 180 days after the end of the last study dose, and must not engage in sperm donation, egg donation, or have birth plan.

You may not qualify if:

• Study participants must be excluded from this study if one of the following conditions is met:
• Abnormal and clinically significant results of vital signs, physical examination, 12-lead ECG, chest X-ray (frontal and lateral), laboratory tests (including hematology, blood chemistry, urinalysis, etc.) or serum creatinine above the upper limit of normal at screening;
• Positive for any of the HBsAg, HCV antibody, HIV antibody, or Treponema pallidum antibody;
• History or current evidence of severe or chronic metabolic/endocrine, hepatic, renal, hematological, pulmonary, immunological, cardiovascular, gastrointestinal, genitourinary, neurological or psychiatric diseases;
• Prior history of hypertension;
• Prior history of severe gastrointestinal diseases such as dysphagia, active gastric ulcers, etc., resulting in inability to take oral medication or disorders in absorption of oral medication
• Prior history of gastrointestinal surgery, renal surgery, cholecystectomy, etc. that, in the judgment of the investigator, may affect drug absorption or excretion;
• Prior history of drug allergy, or acute allergic rhinitis or food allergy within 2 weeks before screening, or allergy to the active ingredients or excipients of the study drug;
• Use of any prescription drugs and Chinese herbal medicines within 30 days prior to the first dose;
• Use of any over-the-counter drugs, vitamins, and health products within 14 days prior to the first dose;
• Consumption of more than 10 cigarettes per day within 3 months before screening, or those who cannot quit smoking during the study;
• Regular alcohol consumption within 6 months before screening, that is, those who drink more than 14 units of alcohol per week (1 unit = 360 mL of beer, or 45 mL of spirits with an alcohol content of 40%, or 150 mL of wine), or those who cannot abstain from alcohol during the study, or those who are positive for alcohol breath test;
• History of drug abuse or recreational use, or positive for urine drug abuse screen;
• Blood donation (including blood component donation) or blood loss ≥ 400 mL within 3 months prior to screening, blood products within 2 months prior to screening, blood donation (including component blood donation) or lost blood ≥ 200 mL within 1 month prior to screening, or a plan to donate blood or blood components during the study or within 1 month after the end of the study;
• Difficulty in blood collection, or a history of needle phobia or blood phobia, or intolerance to blood sampling via venipuncture, or poor evaluation of venous blood collection;

Sponsors & Collaborators

• Hutchmed: lead

Study Sites (1)

The First Affiliated Hospital of Shandong First Medical University

Jinan, Shandong, 250014, China

Location

Study Officials

• Bin Yang

  Hutchmed

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: Two formulations containing the same active pharmaceutical ingredient are considered bioequivalent if their relative bioavailability (rate and extent of drug absorption) falls within acceptable predetermined limits after administration at the same molar dose. Formulations with bioequivalence are considered to act comparably in vivo, i.e., similar in terms of safety and efficacy. This study aims to evaluate the pharmacokinetic (PK) profile and bioequivalence of the original and modified formulations of HMPL-523 acetate tablets in healthy participants to bridge the safety and efficacy of the modified formulation of HMPL 523 acetate tablets in humans.

Study Record Dates

• First Submitted: September 11, 2025
• First Posted: January 9, 2026
• Study Start: October 28, 2025
• Primary Completion: November 28, 2025
• Study Completion: February 2, 2026
• Last Updated: February 12, 2026

Record last verified: 2026-02

Locations

CN (1)