Healthy VolunteersPhase 1NCT07841522
A Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of HW243040 in Healthy Participants
A Phase 1 study testing HW243040 in people with Healthy Volunteers, run by The Third Xiangya Hospital of Central South University.
Trial summary
This is a Phase I, randomized, double-blind, placebo-controlled, single-center, dose-escalation study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of HW243040 in healthy participants. Read more about this study
- Who is it for?
- Ages 18 to 55 yearsHealthy volunteers can take part
- Conditions the study is for
- Healthy Volunteers
- What is being tested?
- HW243040
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- Yes, some participants may receive a placebo
- How many people
- 98 participants
- Where
- No sites listed yet
- Study dates
- 30 Sep 2026to 31 Jul 2027
- Phase
- Phase 1
- Are there results?
- Not yet: the study is under way
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 55 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- Signed informed consent form prior to any study-related procedures, with full understanding of the study content, procedures, and potential adverse reactions, and ability to complete the study as per protocol requirements.
- Healthy male or female, aged ≥ 18 and ≤ 55 years on the day of signing the informed consent form.
- Body weight: males ≥ 50 kg, females ≥ 45 kg; body mass index (BMI) between 19 and 26 kg/m² inclusive (BMI = weight (kg) / height² (m²)).
- Vital signs, physical examination, laboratory tests (hematology, blood biochemistry, urinalysis, coagulation function, and thyroid function), and 12-lead electrocardiogram (ECG) findings are normal or clinically insignificant at screening and baseline.
- Abdominal ultrasound, thyroid ultrasound, and chest X-ray findings are normal or clinically insignificant at screening.
- Willing and able to undergo pain testing procedures and trained qualified.
- Female participants of childbearing potential and male participants with partners of childbearing potential must have adopted contraceptive measures within 2 weeks prior to signing the informed consent form, and must agree to remain abstinent or use highly effective contraceptive methods from the signing of the informed consent form through the end of the follow-up period.
- Female participants of childbearing potential must agree to use highly effective contraceptive methods during the study and for 3 months after the last dose; serum pregnancy test must be negative at screening and baseline, and must not be breastfeeding. Male participants must agree to use highly effective contraceptive methods and refrain from sperm donation during the study and for 3 months after the last dose.
Who cannot join
- -
- 1. Presence of any of the following diseases or treatment history:
- Current or previous history of any clinically significant disease involving the urinary, cardiovascular, endocrine, neurological, digestive, respiratory, hematopoietic, immune, psychiatric, or metabolic systems, or any other condition that, in the investigator's judgment, may interfere with the study results, such as intestinal diseases (including irritable bowel syndrome) and urinary tract infections.
- History of malignancy (except for cancers that have been cured or in remission for ≥ 5 years, radically resected basal cell or squamous cell skin carcinoma, in situ cervical carcinoma, and resected colon polyps).
- Any condition or disease that, in the investigator's judgment, may affect the absorption, metabolism, and/or excretion of the study drug.
- Severe infection, severe trauma, or major surgery within 3 months prior to screening or baseline, or planned surgery during the study period.
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- Use of any medication (including prescription drugs, over-the-counter drugs, herbal medicines, dietary supplements, vitamin A and its derivatives, etc., except for routine vitamins and occasional use of acetaminophen) within 2 weeks prior to screening or baseline, or still within 5 half-lives of the drug at screening or baseline (whichever is longer); or planned use of non-study medications during the study period.
- Participation in any other drug or medical device clinical trial within 3 months prior to screening or baseline, or planned participation during the study period, or still within 5 half-lives of the investigational drug at screening or baseline (whichever is longer).
- 2. Any of the following laboratory findings at screening:
- Sitting systolic blood pressure < 90 mmHg or sitting diastolic blood pressure < 50 mmHg at screening or baseline.
- Orthostatic hypotension confirmed by repeat measurement within 15 minutes at screening or baseline.
- Clinically significant 12-lead ECG abnormalities at screening or baseline; QTcF > 450 ms for males or QTcF > 460 ms for females.
- Positive for hepatitis B surface antigen (HBsAg), human immunodeficiency virus (HIV) antibody, syphilis antibody, or hepatitis C virus (HCV) antibody at screening.
- 3. General conditions:
- Blood donation or significant blood loss (≥ 400 mL) within 8 weeks prior to screening or baseline, or blood transfusion within 4 weeks prior to screening or baseline; or intention to donate blood during the study period.
- Vaccination within 2 weeks prior to screening or baseline, or planned vaccination during the study period.
- Smoking history (average > 5 cigarettes per day) within 4 weeks prior to screening or baseline, or inability to refrain from using any tobacco products during the study period.
- Average daily alcohol intake > 15 g within 4 weeks prior to screening or baseline (15 g alcohol is equivalent to approximately 450 mL beer, 150 mL wine, or 50 mL liquor), or inability to abstain from alcohol during the study period; or positive breath alcohol test at baseline.
- History of drug abuse or dependence prior to screening or baseline; or positive urine drug screen at baseline.
- Excessive consumption of tea, coffee, or caffeinated beverages (average > 8 cups per day, 250 mL per cup) within 6 months prior to screening or baseline.
- Consumption of special foods (such as grapefruit, grapefruit juice, or foods/beverages containing grapefruit juice, chocolate, tobacco, alcohol, caffeinated foods or beverages, etc.) within 48 hours prior to baseline.
- Special dietary requirements or inability to comply with the standardized diet provided by the study center.
- Dysphagia, difficulty in venous blood collection, or physical condition unable to tolerate intensive blood sampling.
- Known allergy to any component of the investigational medicinal product; history of allergic diseases or allergic constitution.
- Use of strong or moderate inhibitors/inducers of CYP2C9, or any inhibitors of P-gp, OATP1B1, OATP1B3, or OAT3 within 30 days prior to screening or planned during the study period.
- Any other condition that, in the investigator's judgment, makes the participant unsuitable for participation in this study, including but not limited to any physiological or psychological condition that may increase the risk of the study, affect the participant's compliance with the protocol, or affect the participant's ability to complete the study.
About this study
Official title: A Phase I, Randomized, Double-Blind, Single-Center, Dose-Escalation, Placebo-Controlled Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of HW243040 in Healthy Participants
This is a Phase I, randomized, double-blind, placebo-controlled, single-center, dose-escalation study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of HW243040 in healthy participants. The study consists of two parts: Part A (Single Ascending Dose, SAD) and food effect study, and Part B (Multiple Ascending Dose, MAD). A total of approximately 98 healthy participants will be enrolled.
Read the detailed description
This is a first-in-human, Phase I, randomized, double-blind, placebo-controlled, single-center, dose-escalation clinical trial designed to evaluate the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of HW243040, a novel angiotensin II type 2 receptor (AT2R) antagonist, in healthy participants. Preclinical data have demonstrated that HW243040 exhibits good analgesic efficacy in neuropathic pain models with a favorable safety profile, supporting its further clinical development. This study does not aim to explore the maximum tolerated dose (MTD) but focuses on characterizing the safety and PK profile across a range of doses.
The study is divided into two main parts: Part A (Single Ascending Dose, SAD, combined with a Food Effect evaluation) and Part B (Multiple Ascending Dose, MAD) . A total of approximately 98 healthy participants are planned for enrollment across both parts.
Part A: SAD and Food Effect Study Part A consists of 6 dose cohorts: 50 mg, 150 mg, 300 mg, 600 mg, 900 mg, and 1200 mg. Except for the 600 mg cohort, each cohort enrolls 10 participants (8 receiving active HW243040 and 2 receiving placebo) under fasting conditions. The 600 mg cohort enrolls 18 participants (16 active, 2 placebo) and utilizes a two-period, two-sequence crossover design to evaluate the effect of a high-fat, high-calorie meal on the PK of HW243040. In this cohort, participants receive the study drug under fasting conditions in one period and under fed conditions in the other, with a 7-day washout between periods. Dose escalation proceeds sequentially from the lowest to the highest dose, with dose progression decisions made by a Safety Review Committee (SRC) based on review of safety and available PK data from the preceding cohort. Dose escalation will be halted if predefined stopping criteria are met (e.g., ≥1/2 participants with moderate related AEs, ≥1/3 with severe related AEs, or any related SAE).
Part B: MAD Study Based on the safety and PK results from Part A, Part B evaluates three dose levels of HW243040 administered twice daily (BID). The planned dose levels are 150 mg, 300 mg, and 600 mg BID. Each cohort enrolls 10 participants (8 active, 2 placebo). Participants receive the study drug for 5 consecutive days (morning and evening, approximately 12 hours apart, for a total of 9 administrations, with only the morning dose given on Day 5). The final dosing regimen, duration, and sampling schedule for Part B may be adjusted based on emerging data from Part A.
Study Population:
Healthy male and female participants aged 18 to 55 years, with a body mass index (BMI) between 19 and 26 kg/m², and body weight ≥50 kg for males and ≥45 kg for females. Participants must be willing to undergo pain testing procedures and comply with the study requirements.
Intervention and Blinding:
HW243040 is formulated as oral tablets in 50 mg and 200 mg strengths. Matching placebo tablets are provided. The study is double-blinded; participants, investigators, site staff, and outcome assessors will be blinded to treatment allocation. Randomization is performed using a block randomization method with a 8:2 (active:placebo) ratio for most cohorts (and 8:1 for the 600 mg SAD cohort).
Study Procedures and Assessments:
The study comprises a screening period (Day -7 to Day -1), a treatment/observation period, and a follow-up period (for unresolved AEs).
Safety Assessments: Include monitoring of adverse events (AEs), serious adverse events (SAEs), vital signs, physical examinations, 12-lead electrocardiograms (ECGs), clinical laboratory tests (hematology, biochemistry, urinalysis, coagulation, and thyroid function), and pregnancy tests for females of childbearing potential. A C-QTc sub-study is planned for cohorts at doses ≥300 mg (including the 600 mg cohort, Sequence A only) to explore the relationship between HW243040 plasma concentrations and changes in QTcF interval.
Pharmacokinetic Assessments:
SAD/FE (non-600mg cohorts): Blood samples are collected at 13 time points from pre-dose to 72 hours post-dose.
SAD/FE (600mg cohort): Blood samples are collected at 26 time points across two periods (up to 72 hours post-dose per period).
MAD: Blood samples are collected on Day 1 (pre-dose to 12 hours), pre-dose on Days 3, 4, and 5, and intensively on Day 5 up to 72 hours post final dose (25 time points total).
Urine and Feces (Exploratory): Full urine and fecal samples are collected from participants in Sequence A of the 600 mg cohort during the first period for metabolite profiling and excretion mass balance exploration.
Pharmacodynamic Assessments:
PD evaluations are performed using standardized pain tests, including Pressure Pain Threshold (PPT) measured by a pressure algometer and Pain Tolerance Time (PTT) measured by the cold pressor test (immersion of hand in ice water, maximum 120 seconds). PD assessments are conducted at pre-dose and at 1, 2, 4, 6, 8, and 12 hours post-dose.
Pharmacokinetic Parameters:
Key PK parameters calculated using non-compartmental analysis include: C~max~, T~max~, AUC~0-t~, AUC~0-inf~, t~1/2~, CL/F, and Vz/F (SAD); and additionally C~trough,ss~, AUC~tau,ss~, and accumulation ratios (R~ac~) for MAD.
Statistical Analysis:
Analyses will be performed using SAS (Version 9.4 or higher). The Safety Analysis Set (SS) will be used for all safety summaries. PK parameters will be summarized descriptively by dose group. For the food effect evaluation, a linear mixed-effects model (with sequence, period, and treatment as fixed effects and participant as random effect) will be applied to log-transformed exposure parameters (AUC~0-t~, AUC~0-inf~, C~max~) to calculate geometric mean ratios and 90% confidence intervals. PD endpoints, C-QTc relationship, and dose proportionality will be explored descriptively or via appropriate modeling approaches (e.g., power model, linear mixed-effects model).
Study Duration and Follow-up:
Participants will be confined to the clinical unit from Day -1 through the end of the observation period (Day 4 for most SAD cohorts; Day 11 for the 600 mg cohort; Day 8 for MAD cohorts). All participants with ongoing AEs at discharge will be followed until resolution, return to baseline, stabilization, or loss to follow-up.
The study is being conducted at a single center, The Third Xiangya Hospital of Central South University, Changsha, China, under the sponsorship of Hubei Bio-Pharmaceutical Industrial Technology Research Institute Co., Ltd.
- Conditions
- Healthy Volunteers
- Being tested
- HW243040, HW243040 Matching Placebo
- Keywords
- HW243040, Angiotensin II Type 2 Receptor Antagonist, AT2R Antagonist, Healthy Volunteers, Pharmacokinetics, Single Ascending Dose, Multiple Ascending Dose, Food Effect
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
HW243040Drug
HW243040 tablets, 50mg and 200mg规格, administered orally. Doses range from 50mg to 1200mg as a single dose in Part A, or 150mg to 600mg twice daily for 5 days in Part B. Administered with 240mL water under fasting or fed (high-fat, high-calorie meal) conditions as specified per arm.
HW243040 Matching PlaceboDrug
HW243040 matching placebo tablets, 50mg and 200mg规格, identical in appearance to HW243040 active tablets. Administered orally with 240mL water under the same conditions as the corresponding active dose arm.
| Study group | Role | What they receive |
|---|---|---|
| HW243040 50mg Single Dose | Experimental | Participants receive a single oral dose of HW243040 50mg (one 50mg tablet) under fasting conditions on Day 1. Receives: Drug: HW243040 |
| HW243040 150mg Single Dose | Experimental | Participants receive a single oral dose of HW243040 150mg (three 50mg tablets) under fasting conditions on Day 1. Receives: Drug: HW243040 |
| HW243040 300mg Single Dose | Experimental | Participants receive a single oral dose of HW243040 300mg (six 50mg tablets or one 200mg + two 50mg tablets) under fasting conditions on Day 1. Receives: Drug: HW243040 |
| HW243040 600mg Single Dose (Fasting and Fed) | Experimental | Participants receive a single oral dose of HW243040 600mg (three 200mg tablets) in a two-period crossover design: one dose under fasting conditions and one dose under fed (high-fat, high-calorie meal) conditions, with a 7-day washout period between doses. Receives: Drug: HW243040 |
| HW243040 900mg Single Dose | Experimental | Participants receive a single oral dose of HW243040 900mg (one 200mg + one 50mg tablets, total 4.5 tablets) under fasting conditions on Day 1. Receives: Drug: HW243040 |
| HW243040 1200mg Single Dose | Experimental | Participants receive a single oral dose of HW243040 1200mg (six 200mg tablets) under fasting conditions on Day 1. Receives: Drug: HW243040 |
| Placebo Single Dose | Placebo comparator | Participants receive a single oral dose of HW243040 matching placebo tablets (number of tablets matching the corresponding active dose group) under fasting conditions on Day 1. Receives: Drug: HW243040 Matching Placebo |
| HW243040 150mg BID Multiple Doses | Experimental | Participants receive HW243040 150mg (three 50mg tablets) orally twice daily (every 12 hours) for 5 days (9 doses total, Day 1 to Day 5 morning) under fasting conditions. Receives: Drug: HW243040 |
| HW243040 300mg BID Multiple Doses | Experimental | Participants receive HW243040 300mg (six 50mg tablets or one 200mg + two 50mg tablets) orally twice daily (every 12 hours) for 5 days (9 doses total, Day 1 to Day 5 morning) under fasting conditions. Receives: Drug: HW243040 |
| HW243040 600mg BID Multiple Doses | Experimental | Participants receive HW243040 600mg (three 200mg tablets) orally twice daily (every 12 hours) for 5 days (9 doses total, Day 1 to Day 5 morning) under fasting conditions. Receives: Drug: HW243040 |
| Placebo BID Multiple Doses | Placebo comparator | Participants receive HW243040 matching placebo tablets orally twice daily (every 12 hours) for 5 days (9 doses total, Day 1 to Day 5 morning) under fasting conditions. Receives: Drug: HW243040 Matching Placebo |
What is being measured
The primary outcome is the main question the study is designed to answer.
Incidence of Treatment-Emergent Adverse Events (TEAEs)
Number of participants with TEAEs, including serious adverse events (SAEs), assessed by CTCAE v5.0.
Measured: From signing of informed consent form through follow-up period (until AE resolution; up to Day 4 for SAD 50/150/300/900/1200 mg, Day 11 for 600 mg FE, Day 8 for MAD cohorts).
Number of Participants with Clinically Significant Vital Signs Changes
Measured: Baseline (Day -1) to End of Study; measured at screening, Day -1, pre-dose and 1, 2, 4, 8, 12, 24, 48, 72 hours post-dose (schedule varies per cohort).
Number of Participants with Clinically Significant Laboratory Abnormalities
Measured: Baseline (Screening) to End of Study (Day 4 for SAD 50/150/300/900/1200 mg; Day 11 for 600 mg FE; Day 8 for MAD).
Number of Participants with Clinically Significant 12-lead ECG Abnormalities
Measured: Baseline (Day -1) to End of Study; measured at screening, Day -1, pre-dose and 1, 2, 4, 8, 12, 24, 48, 72 hours post-dose (schedule varies per cohort).
Secondary outcomes (37)
Maximum Observed Plasma Concentration (Cmax) Following Single Ascending Dose Administration
Cmax of HW243040 in plasma following single ascending dose administration, measured by validated LC-MS/MS method.
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose.
Time to Maximum Observed Plasma Concentration (Tmax) of HW243040 Following Single Ascending Dose Administration
Tmax of HW243040 in plasma following single ascending dose administration, determined directly from concentration-time data.
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose.
Apparent Terminal Elimination Half-life (t1/2) of HW243040 Following Single Ascending Dose Administration
Terminal elimination half-life of HW243040 in plasma following single ascending dose administration, calculated as ln(2)/λz.
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose.
Area Under the Plasma Concentration-Time Curve from Time Zero to Last Measurable Concentration (AUC0-t) of HW243040 Following Single Ascending Dose Administration
AUC0-t of HW243040 in plasma following single ascending dose administration, calculated using the linear-up/log-down trapezoidal method. Unit: h*ng/mL.
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose.
Area Under the Plasma Concentration-Time Curve from Time Zero Extrapolated to Infinity (AUC0-inf) of HW243040 Following Single Ascending Dose Administration
AUC0-inf of HW243040 in plasma following single ascending dose administration, calculated as AUC0-t + Clast/λz.
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose.
Apparent Total Clearance (CL/F) of HW243040 Following Single Ascending Dose Administration
Apparent total clearance of HW243040 from plasma following single ascending dose administration, calculated as Dose/AUC0-inf.
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose.
Apparent Volume of Distribution (Vz/F) of HW243040 Following Single Ascending Dose Administration
Apparent volume of distribution of HW243040 during the terminal phase following single ascending dose administration, calculated as Dose/(AUC0-inf × λz).
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose.
Maximum Observed Plasma Concentration (Cmax) of HW243040 Following Single Dose in Fed and Fasted States
Cmax of HW243040 in plasma following single dose in fed and fasted states, measured by validated LC-MS/MS method.
Measured: Period 1 (Day 1) and Period 2 (Day 8): pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose in each period (two-way crossover, fasted vs fed).
Time to Maximum Observed Plasma Concentration (Tmax) of HW243040 Following Single Dose in Fed and Fasted States
Tmax of HW243040 in plasma following single dose in fed and fasted states.
Measured: Period 1 (Day 1) and Period 2 (Day 8): pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose in each period (two-way crossover, fasted vs fed).
Apparent Terminal Elimination Half-life (t1/2) of HW243040 Following Single Dose in Fed and Fasted States
Terminal elimination half-life of HW243040 in plasma following single dose in fed and fasted states, calculated as ln(2)/λz.
Measured: Period 1 (Day 1) and Period 2 (Day 8): pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose in each period (two-way crossover, fasted vs fed).
Area Under the Plasma Concentration-Time Curve from Time Zero to Last Measurable Concentration (AUC0-t) of HW243040 Following Single Dose in Fed and Fasted States
AUC0-t of HW243040 in plasma following single dose in fed and fasted states, calculated by linear-up/log-down trapezoidal method.
Measured: Period 1 (Day 1) and Period 2 (Day 8): pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose in each period (two-way crossover, fasted vs fed).
Area Under the Plasma Concentration-Time Curve from Time Zero Extrapolated to Infinity (AUC0-inf) of HW243040 Following Single Dose in Fed and Fasted States
AUC0-inf of HW243040 in plasma following single dose in fed and fasted states, calculated as AUC0-t + Clast/λz.
Measured: Period 1 (Day 1) and Period 2 (Day 8): pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose in each period (two-way crossover, fasted vs fed).
Apparent Total Clearance (CL/F) of HW243040 Following Single Dose in Fed and Fasted States
Apparent total clearance of HW243040 in plasma following single dose in fed and fasted states, calculated as Dose/AUC0-inf.
Measured: Period 1 (Day 1) and Period 2 (Day 8): pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose in each period (two-way crossover, fasted vs fed).
Apparent Volume of Distribution (Vz/F) of HW243040 Following Single Dose in Fed and Fasted States
Apparent volume of distribution of HW243040 in plasma following single dose in fed and fasted states, calculated as Dose/(AUC0-inf × λz).
Measured: Period 1 (Day 1) and Period 2 (Day 8): pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose in each period (two-way crossover, fasted vs fed).
Maximum Observed Plasma Concentration (Cmax) of HW243040 on Day 1 of Multiple Ascending Dose Administration
Cmax of HW243040 in plasma on Day 1 after the first dose of multiple ascending dose administration, measured by validated LC-MS/MS method.
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Time to Maximum Observed Plasma Concentration (Tmax) of HW243040 on Day 1 of Multiple Ascending Dose Administration
Tmax of HW243040 in plasma on Day 1 after the first dose of multiple ascending dose administration.
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Area Under the Plasma Concentration-Time Curve from Time Zero to 12 Hours (AUC0-12h) of HW243040 on Day 1 of Multiple Ascending Dose Administration
AUC0-12h of HW243040 in plasma on Day 1, calculated by linear-up/log-down trapezoidal method.
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Area Under the Plasma Concentration-Time Curve from Time Zero Extrapolated to Infinity (AUC0-inf) of HW243040 on Day 1 of Multiple Ascending Dose Administration
AUC0-inf of HW243040 in plasma on Day 1, calculated as AUC0-t + Clast/λz.
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Apparent Total Clearance (CL/F) of HW243040 on Day 1 of Multiple Ascending Dose Administration
Apparent total clearance of HW243040 on Day 1, calculated as Dose/AUC0-inf.
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Apparent Volume of Distribution (Vz/F) of HW243040 on Day 1 of Multiple Ascending Dose Administration
Apparent volume of distribution of HW243040 on Day 1, calculated as Dose/(AUC0-inf × λz).
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Apparent Terminal Elimination Half-life (t1/2) of HW243040 on Day 1 of Multiple Ascending Dose Administration
Terminal elimination half-life of HW243040 on Day 1, calculated as ln(2)/λz.
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Area Under the Plasma Concentration-Time Curve over One Dosing Interval (AUC0-tau) of HW243040 on Day 1 of Multiple Ascending Dose Administration
AUC0-tau of HW243040 in plasma on Day 1, covering the 12-hour dosing interval, calculated by linear-up/log-down trapezoidal method.
Measured: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Area Under the Plasma Concentration-Time Curve over a Dosing Interval at Steady State (AUCtau,ss) of HW243040
AUC over one dosing interval at steady state on Day 5 of multiple ascending dose administration, calculated by linear-up/log-down trapezoidal method.
Measured: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Area Under the Plasma Concentration-Time Curve from Time Zero to Last Measurable Concentration at Steady State (AUC0-t,ss) of HW243040
AUC0-t at steady state on Day 5 of multiple ascending dose administration, calculated by linear-up/log-down trapezoidal method.
Measured: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Area Under the Plasma Concentration-Time Curve from Time Zero Extrapolated to Infinity at Steady State (AUC0-inf,ss) of HW243040
AUC0-inf at steady state on Day 5 of multiple ascending dose administration, calculated as AUC0-t + Clast/λz.
Measured: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Time to Maximum Observed Plasma Concentration at Steady State (Tmax,ss) of HW243040
Tmax at steady state on Day 5 of multiple ascending dose administration.
Measured: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Apparent Terminal Elimination Half-life (t1/2) of HW243040 at Steady State
Terminal elimination half-life at steady state on Day 5 of multiple ascending dose administration, calculated as ln(2)/λz.
Measured: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Apparent Clearance at Steady State (CLss/F) of HW243040
Apparent clearance at steady state on Day 5 of multiple ascending dose administration, calculated as Dose/AUCtau,ss.
Measured: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Apparent Volume of Distribution at Steady State (Vz/F) of HW243040
Apparent volume of distribution at steady state on Day 5 of multiple ascending dose administration, calculated as Dose/(AUCtau,ss × λz).
Measured: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Trough Concentration at Steady State (Ctrough,ss) of HW243040
Trough plasma concentration at steady state on Day 5 of multiple ascending dose administration.
Measured: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Peak Concentration at Steady State (Cmax,ss) of HW243040
Peak plasma concentration at steady state on Day 5 of multiple ascending dose administration.
Measured: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Accumulation Ratio (Rac) of HW243040 at Steady State
Accumulation ratio based on AUC (Rac,AUC) and Cmax (Rac,Cmax) at steady state on Day 5 of multiple ascending dose administration.
Measured: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Cumulative Amount of Unchanged HW243040 Excreted in Urine (Ae)
Cumulative amount of unchanged HW243040 excreted in urine, measured by validated LC-MS/MS method.
Measured: Period 1 (Day 1): pre-dose (within 12 hours) and 0-4, 4-8, 8-12, 12-24, 24-48, 48-72 hours post-dose.
Cumulative Amount of Unchanged HW243040 Excreted in Feces (Ae)
Cumulative amount of unchanged HW243040 excreted in feces, measured by validated LC-MS/MS method.
Measured: Period 1 (Day 1): pre-dose (within 12 hours) and 0-4, 4-8, 8-12, 12-24, 24-48, 48-72 hours post-dose.
Fraction of Unchanged HW243040 Excreted in Urine (fe)
Fraction of unchanged HW243040 excreted in urine, calculated as Ae/dose.
Measured: Period 1 (Day 1): pre-dose (within 12 hours) and 0-4, 4-8, 8-12, 12-24, 24-48, 48-72 hours post-dose.
Fraction of Unchanged HW243040 Excreted in Feces (fe)
Fraction of unchanged HW243040 excreted in feces, calculated as Ae/dose.
Measured: Period 1 (Day 1): pre-dose (within 12 hours) and 0-4, 4-8, 8-12, 12-24, 24-48, 48-72 hours post-dose.
Renal Clearance (CLR) of HW243040
Renal clearance of HW243040, calculated as cumulative amount excreted in urine divided by AUC.
Measured: Period 1 (Day 1): pre-dose (within 12 hours) and 0-4, 4-8, 8-12, 12-24, 24-48, 48-72 hours post-dose.
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted25 Sep 2026
- Study start30 Sep 2026 (estimated)
- Primary completion31 Jul 2027 (estimated)
- Study completion31 Jul 2027 (estimated)
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Other trials for Healthy VolunteersStudies of the same condition, open and under way.
- More trials run by The Third Xiangya Hospital of Central South UniversityThe sponsor's other registered studies.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Other
- Allocation
- Randomised
- Intervention model
- Sequential
- Masking
- Triple blind
- Who is masked
- Participant, Investigator, Outcomes assessor
- Enrolment
- 98 participants (estimated)
Sponsor and investigators
- Sponsor type
- University, hospital or other
- Responsible party
- Principal investigator, Guoping Yang, The Third Xiangya Hospital of Central South University
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT07841522
- Sponsor's protocol ID
- HW243040-101
- Status last verified
- Sep 2026
- First submitted
- 31 Aug 2026
- Last updated
- 25 Sep 2026
- Results posted
- No
- Data monitoring committee
- No
- FDA-regulated drug
- No
- FDA-regulated device
- No
- Individual data sharing
- No: Individual participant data (IPD) will not be shared because this is a first-in-human or early-stage clinical trial involving a novel investigational drug. The data contain proprietary and confidential information that could compromise ongoing patent applications and future commercial development. Public data sharing at this stage may also violate our confidentiality agreements with the contract research organization (CRO) and regulatory authorities. Therefore, IPD sharing is not feasible until the drug receives market approval or the primary study results are fully published.
Study at a glance
From the registry record, last updated by the sponsor on 25 Sep 2026. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A Phase I, Randomized, Double-Blind, Single-Center, Dose-Escalation, Placebo-Controlled Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of HW243040 in Healthy Participants
- ClinicalTrials.gov ID
- NCT07841522
- Acronym / sponsor ID
- HW243040-101
- Conditions
- Healthy Volunteers
- Keywords
- HW243040, Angiotensin II Type 2 Receptor Antagonist, AT2R Antagonist, Healthy Volunteers, Pharmacokinetics, Single Ascending Dose, Multiple Ascending Dose, Food Effect
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Not yet recruiting
- Enrolment
- 98 participants (estimated)
- Lead sponsor
- The Third Xiangya Hospital of Central South UniversityUniversity, hospital or other
- Study start
- 30 Sep 2026 (estimated)
- Primary completion
- 31 Jul 2027 (estimated)
- Study completion
- 31 Jul 2027 (estimated)
- First posted
- 25 Sep 2026 (actual)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
This is a Phase I, randomized, double-blind, placebo-controlled, single-center, dose-escalation study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of HW243040 in healthy participants. The study consists of two parts: Part A (Single Ascending Dose, SAD) and food effect study, and Part B (Multiple Ascending Dose, MAD). A total of approximately 98 healthy participants will be enrolled.
Detailed description
This is a first-in-human, Phase I, randomized, double-blind, placebo-controlled, single-center, dose-escalation clinical trial designed to evaluate the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of HW243040, a novel angiotensin II type 2 receptor (AT2R) antagonist, in healthy participants. Preclinical data have demonstrated that HW243040 exhibits good analgesic efficacy in neuropathic pain models with a favorable safety profile, supporting its further clinical development. This study does not aim to explore the maximum tolerated dose (MTD) but focuses on characterizing the safety and PK profile across a range of doses.
The study is divided into two main parts: Part A (Single Ascending Dose, SAD, combined with a Food Effect evaluation) and Part B (Multiple Ascending Dose, MAD) . A total of approximately 98 healthy participants are planned for enrollment across both parts.
Part A: SAD and Food Effect Study Part A consists of 6 dose cohorts: 50 mg, 150 mg, 300 mg, 600 mg, 900 mg, and 1200 mg. Except for the 600 mg cohort, each cohort enrolls 10 participants (8 receiving active HW243040 and 2 receiving placebo) under fasting conditions. The 600 mg cohort enrolls 18 participants (16 active, 2 placebo) and utilizes a two-period, two-sequence crossover design to evaluate the effect of a high-fat, high-calorie meal on the PK of HW243040. In this cohort, participants receive the study drug under fasting conditions in one period and under fed conditions in the other, with a 7-day washout between periods. Dose escalation proceeds sequentially from the lowest to the highest dose, with dose progression decisions made by a Safety Review Committee (SRC) based on review of safety and available PK data from the preceding cohort. Dose escalation will be halted if predefined stopping criteria are met (e.g., ≥1/2 participants with moderate related AEs, ≥1/3 with severe related AEs, or any related SAE).
Part B: MAD Study Based on the safety and PK results from Part A, Part B evaluates three dose levels of HW243040 administered twice daily (BID). The planned dose levels are 150 mg, 300 mg, and 600 mg BID. Each cohort enrolls 10 participants (8 active, 2 placebo). Participants receive the study drug for 5 consecutive days (morning and evening, approximately 12 hours apart, for a total of 9 administrations, with only the morning dose given on Day 5). The final dosing regimen, duration, and sampling schedule for Part B may be adjusted based on emerging data from Part A.
Study Population:
Healthy male and female participants aged 18 to 55 years, with a body mass index (BMI) between 19 and 26 kg/m², and body weight ≥50 kg for males and ≥45 kg for females. Participants must be willing to undergo pain testing procedures and comply with the study requirements.
Intervention and Blinding:
HW243040 is formulated as oral tablets in 50 mg and 200 mg strengths. Matching placebo tablets are provided. The study is double-blinded; participants, investigators, site staff, and outcome assessors will be blinded to treatment allocation. Randomization is performed using a block randomization method with a 8:2 (active:placebo) ratio for most cohorts (and 8:1 for the 600 mg SAD cohort).
Study Procedures and Assessments:
The study comprises a screening period (Day -7 to Day -1), a treatment/observation period, and a follow-up period (for unresolved AEs).
Safety Assessments: Include monitoring of adverse events (AEs), serious adverse events (SAEs), vital signs, physical examinations, 12-lead electrocardiograms (ECGs), clinical laboratory tests (hematology, biochemistry, urinalysis, coagulation, and thyroid function), and pregnancy tests for females of childbearing potential. A C-QTc sub-study is planned for cohorts at doses ≥300 mg (including the 600 mg cohort, Sequence A only) to explore the relationship between HW243040 plasma concentrations and changes in QTcF interval.
Pharmacokinetic Assessments:
SAD/FE (non-600mg cohorts): Blood samples are collected at 13 time points from pre-dose to 72 hours post-dose.
SAD/FE (600mg cohort): Blood samples are collected at 26 time points across two periods (up to 72 hours post-dose per period).
MAD: Blood samples are collected on Day 1 (pre-dose to 12 hours), pre-dose on Days 3, 4, and 5, and intensively on Day 5 up to 72 hours post final dose (25 time points total).
Urine and Feces (Exploratory): Full urine and fecal samples are collected from participants in Sequence A of the 600 mg cohort during the first period for metabolite profiling and excretion mass balance exploration.
Pharmacodynamic Assessments:
PD evaluations are performed using standardized pain tests, including Pressure Pain Threshold (PPT) measured by a pressure algometer and Pain Tolerance Time (PTT) measured by the cold pressor test (immersion of hand in ice water, maximum 120 seconds). PD assessments are conducted at pre-dose and at 1, 2, 4, 6, 8, and 12 hours post-dose.
Pharmacokinetic Parameters:
Key PK parameters calculated using non-compartmental analysis include: C~max~, T~max~, AUC~0-t~, AUC~0-inf~, t~1/2~, CL/F, and Vz/F (SAD); and additionally C~trough,ss~, AUC~tau,ss~, and accumulation ratios (R~ac~) for MAD.
Statistical Analysis:
Analyses will be performed using SAS (Version 9.4 or higher). The Safety Analysis Set (SS) will be used for all safety summaries. PK parameters will be summarized descriptively by dose group. For the food effect evaluation, a linear mixed-effects model (with sequence, period, and treatment as fixed effects and participant as random effect) will be applied to log-transformed exposure parameters (AUC~0-t~, AUC~0-inf~, C~max~) to calculate geometric mean ratios and 90% confidence intervals. PD endpoints, C-QTc relationship, and dose proportionality will be explored descriptively or via appropriate modeling approaches (e.g., power model, linear mixed-effects model).
Study Duration and Follow-up:
Participants will be confined to the clinical unit from Day -1 through the end of the observation period (Day 4 for most SAD cohorts; Day 11 for the 600 mg cohort; Day 8 for MAD cohorts). All participants with ongoing AEs at discharge will be followed until resolution, return to baseline, stabilization, or loss to follow-up.
The study is being conducted at a single center, The Third Xiangya Hospital of Central South University, Changsha, China, under the sponsorship of Hubei Bio-Pharmaceutical Industrial Technology Research Institute Co., Ltd.
Study design
- Primary purpose
- Other
- Allocation
- Randomised
- Intervention model
- Sequential
- Masking
- Triple blind (participant, investigator, outcomes assessor)
- Number of arms
- 11
| Arm | Type | Receives |
|---|---|---|
| HW243040 50mg Single Dose | Experimental | Drug: HW243040Participants receive a single oral dose of HW243040 50mg (one 50mg tablet) under fasting conditions on Day 1. |
| HW243040 150mg Single Dose | Experimental | Drug: HW243040Participants receive a single oral dose of HW243040 150mg (three 50mg tablets) under fasting conditions on Day 1. |
| HW243040 300mg Single Dose | Experimental | Drug: HW243040Participants receive a single oral dose of HW243040 300mg (six 50mg tablets or one 200mg + two 50mg tablets) under fasting conditions on Day 1. |
| HW243040 600mg Single Dose (Fasting and Fed) | Experimental | Drug: HW243040Participants receive a single oral dose of HW243040 600mg (three 200mg tablets) in a two-period crossover design: one dose under fasting conditions and one dose under fed (high-fat, high-calorie meal) conditions, with a 7-day washout period between doses. |
| HW243040 900mg Single Dose | Experimental | Drug: HW243040Participants receive a single oral dose of HW243040 900mg (one 200mg + one 50mg tablets, total 4.5 tablets) under fasting conditions on Day 1. |
| HW243040 1200mg Single Dose | Experimental | Drug: HW243040Participants receive a single oral dose of HW243040 1200mg (six 200mg tablets) under fasting conditions on Day 1. |
| Placebo Single Dose | Placebo comparator | Drug: HW243040 Matching PlaceboParticipants receive a single oral dose of HW243040 matching placebo tablets (number of tablets matching the corresponding active dose group) under fasting conditions on Day 1. |
| HW243040 150mg BID Multiple Doses | Experimental | Drug: HW243040Participants receive HW243040 150mg (three 50mg tablets) orally twice daily (every 12 hours) for 5 days (9 doses total, Day 1 to Day 5 morning) under fasting conditions. |
| HW243040 300mg BID Multiple Doses | Experimental | Drug: HW243040Participants receive HW243040 300mg (six 50mg tablets or one 200mg + two 50mg tablets) orally twice daily (every 12 hours) for 5 days (9 doses total, Day 1 to Day 5 morning) under fasting conditions. |
| HW243040 600mg BID Multiple Doses | Experimental | Drug: HW243040Participants receive HW243040 600mg (three 200mg tablets) orally twice daily (every 12 hours) for 5 days (9 doses total, Day 1 to Day 5 morning) under fasting conditions. |
| Placebo BID Multiple Doses | Placebo comparator | Drug: HW243040 Matching PlaceboParticipants receive HW243040 matching placebo tablets orally twice daily (every 12 hours) for 5 days (9 doses total, Day 1 to Day 5 morning) under fasting conditions. |
Who may qualify
- Ages
- 18 to 55 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (8 listed)
- Signed informed consent form prior to any study-related procedures, with full understanding of the study content, procedures, and potential adverse reactions, and ability to complete the study as per protocol requirements.
- Healthy male or female, aged ≥ 18 and ≤ 55 years on the day of signing the informed consent form.
- Body weight: males ≥ 50 kg, females ≥ 45 kg; body mass index (BMI) between 19 and 26 kg/m² inclusive (BMI = weight (kg) / height² (m²)).
- Vital signs, physical examination, laboratory tests (hematology, blood biochemistry, urinalysis, coagulation function, and thyroid function), and 12-lead electrocardiogram (ECG) findings are normal or clinically insignificant at screening and baseline.
- Abdominal ultrasound, thyroid ultrasound, and chest X-ray findings are normal or clinically insignificant at screening.
Key exclusion criteria (26 listed)
- -
- Current or previous history of any clinically significant disease involving the urinary, cardiovascular, endocrine, neurological, digestive, respiratory, hematopoietic, immune, psychiatric, or metabolic systems, or any other condition that, in the investigator's judgment, may interfere with the study results, such as intestinal diseases (including irritable bowel syndrome) and urinary tract infections.
- History of malignancy (except for cancers that have been cured or in remission for ≥ 5 years, radically resected basal cell or squamous cell skin carcinoma, in situ cervical carcinoma, and resected colon polyps).
- Any condition or disease that, in the investigator's judgment, may affect the absorption, metabolism, and/or excretion of the study drug.
- Severe infection, severe trauma, or major surgery within 3 months prior to screening or baseline, or planned surgery during the study period.
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| HW243040HW243040 tablets, 50mg and 200mg规格, administered orally. Doses range from 50mg to 1200mg as a single dose in Part A, or 150mg to 600mg twice daily for 5 days in Part B. Administered with 240mL water under fasting or fed (high-fat, high-calorie meal) conditions as specified per arm. | Drug | HW243040 1200mg Single Dose, HW243040 150mg BID Multiple Doses, HW243040 150mg Single Dose, HW243040 300mg BID Multiple Doses, HW243040 300mg Single Dose, HW243040 50mg Single Dose, HW243040 600mg BID Multiple Doses, HW243040 600mg Single Dose (Fasting and Fed), HW243040 900mg Single Dose |
| HW243040 Matching PlaceboHW243040 matching placebo tablets, 50mg and 200mg规格, identical in appearance to HW243040 active tablets. Administered orally with 240mL water under the same conditions as the corresponding active dose arm. | Drug | Placebo BID Multiple Doses, Placebo Single Dose |
Primary outcome
Incidence of Treatment-Emergent Adverse Events (TEAEs)
Time frame: From signing of informed consent form through follow-up period (until AE resolution; up to Day 4 for SAD 50/150/300/900/1200 mg, Day 11 for 600 mg FE, Day 8 for MAD cohorts).
Number of participants with TEAEs, including serious adverse events (SAEs), assessed by CTCAE v5.0.
Number of Participants with Clinically Significant Vital Signs Changes
Time frame: Baseline (Day -1) to End of Study; measured at screening, Day -1, pre-dose and 1, 2, 4, 8, 12, 24, 48, 72 hours post-dose (schedule varies per cohort).
Number of Participants with Clinically Significant Laboratory Abnormalities
Time frame: Baseline (Screening) to End of Study (Day 4 for SAD 50/150/300/900/1200 mg; Day 11 for 600 mg FE; Day 8 for MAD).
Number of Participants with Clinically Significant 12-lead ECG Abnormalities
Time frame: Baseline (Day -1) to End of Study; measured at screening, Day -1, pre-dose and 1, 2, 4, 8, 12, 24, 48, 72 hours post-dose (schedule varies per cohort).
37 secondary outcomes
Maximum Observed Plasma Concentration (Cmax) Following Single Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose.
Time to Maximum Observed Plasma Concentration (Tmax) of HW243040 Following Single Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose.
Apparent Terminal Elimination Half-life (t1/2) of HW243040 Following Single Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose.
Area Under the Plasma Concentration-Time Curve from Time Zero to Last Measurable Concentration (AUC0-t) of HW243040 Following Single Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose.
Area Under the Plasma Concentration-Time Curve from Time Zero Extrapolated to Infinity (AUC0-inf) of HW243040 Following Single Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose.
Apparent Total Clearance (CL/F) of HW243040 Following Single Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose.
Apparent Volume of Distribution (Vz/F) of HW243040 Following Single Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose.
Maximum Observed Plasma Concentration (Cmax) of HW243040 Following Single Dose in Fed and Fasted States
Time frame: Period 1 (Day 1) and Period 2 (Day 8): pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose in each period (two-way crossover, fasted vs fed).
Time to Maximum Observed Plasma Concentration (Tmax) of HW243040 Following Single Dose in Fed and Fasted States
Time frame: Period 1 (Day 1) and Period 2 (Day 8): pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose in each period (two-way crossover, fasted vs fed).
Apparent Terminal Elimination Half-life (t1/2) of HW243040 Following Single Dose in Fed and Fasted States
Time frame: Period 1 (Day 1) and Period 2 (Day 8): pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose in each period (two-way crossover, fasted vs fed).
Area Under the Plasma Concentration-Time Curve from Time Zero to Last Measurable Concentration (AUC0-t) of HW243040 Following Single Dose in Fed and Fasted States
Time frame: Period 1 (Day 1) and Period 2 (Day 8): pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose in each period (two-way crossover, fasted vs fed).
Area Under the Plasma Concentration-Time Curve from Time Zero Extrapolated to Infinity (AUC0-inf) of HW243040 Following Single Dose in Fed and Fasted States
Time frame: Period 1 (Day 1) and Period 2 (Day 8): pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose in each period (two-way crossover, fasted vs fed).
Apparent Total Clearance (CL/F) of HW243040 Following Single Dose in Fed and Fasted States
Time frame: Period 1 (Day 1) and Period 2 (Day 8): pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose in each period (two-way crossover, fasted vs fed).
Apparent Volume of Distribution (Vz/F) of HW243040 Following Single Dose in Fed and Fasted States
Time frame: Period 1 (Day 1) and Period 2 (Day 8): pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose in each period (two-way crossover, fasted vs fed).
Maximum Observed Plasma Concentration (Cmax) of HW243040 on Day 1 of Multiple Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Time to Maximum Observed Plasma Concentration (Tmax) of HW243040 on Day 1 of Multiple Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Area Under the Plasma Concentration-Time Curve from Time Zero to 12 Hours (AUC0-12h) of HW243040 on Day 1 of Multiple Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Area Under the Plasma Concentration-Time Curve from Time Zero Extrapolated to Infinity (AUC0-inf) of HW243040 on Day 1 of Multiple Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Apparent Total Clearance (CL/F) of HW243040 on Day 1 of Multiple Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Apparent Volume of Distribution (Vz/F) of HW243040 on Day 1 of Multiple Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Apparent Terminal Elimination Half-life (t1/2) of HW243040 on Day 1 of Multiple Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Area Under the Plasma Concentration-Time Curve over One Dosing Interval (AUC0-tau) of HW243040 on Day 1 of Multiple Ascending Dose Administration
Time frame: Day 1: pre-dose (within 30 minutes) and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose (12-hour sample is pre-dose for second administration).
Area Under the Plasma Concentration-Time Curve over a Dosing Interval at Steady State (AUCtau,ss) of HW243040
Time frame: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Area Under the Plasma Concentration-Time Curve from Time Zero to Last Measurable Concentration at Steady State (AUC0-t,ss) of HW243040
Time frame: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Area Under the Plasma Concentration-Time Curve from Time Zero Extrapolated to Infinity at Steady State (AUC0-inf,ss) of HW243040
Time frame: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Time to Maximum Observed Plasma Concentration at Steady State (Tmax,ss) of HW243040
Time frame: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Apparent Terminal Elimination Half-life (t1/2) of HW243040 at Steady State
Time frame: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Apparent Clearance at Steady State (CLss/F) of HW243040
Time frame: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Apparent Volume of Distribution at Steady State (Vz/F) of HW243040
Time frame: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Trough Concentration at Steady State (Ctrough,ss) of HW243040
Time frame: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Peak Concentration at Steady State (Cmax,ss) of HW243040
Time frame: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Accumulation Ratio (Rac) of HW243040 at Steady State
Time frame: Day 3, Day 4, and Day 5: pre-dose (morning troughs); Day 5: pre-dose and 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-morning dose; plus 24 hours (Day 6), 48 hours (Day 7), and 72 hours (Day 8) post-morning dose on Day 5.
Cumulative Amount of Unchanged HW243040 Excreted in Urine (Ae)
Time frame: Period 1 (Day 1): pre-dose (within 12 hours) and 0-4, 4-8, 8-12, 12-24, 24-48, 48-72 hours post-dose.
Cumulative Amount of Unchanged HW243040 Excreted in Feces (Ae)
Time frame: Period 1 (Day 1): pre-dose (within 12 hours) and 0-4, 4-8, 8-12, 12-24, 24-48, 48-72 hours post-dose.
Fraction of Unchanged HW243040 Excreted in Urine (fe)
Time frame: Period 1 (Day 1): pre-dose (within 12 hours) and 0-4, 4-8, 8-12, 12-24, 24-48, 48-72 hours post-dose.
Fraction of Unchanged HW243040 Excreted in Feces (fe)
Time frame: Period 1 (Day 1): pre-dose (within 12 hours) and 0-4, 4-8, 8-12, 12-24, 24-48, 48-72 hours post-dose.
Renal Clearance (CLR) of HW243040
Time frame: Period 1 (Day 1): pre-dose (within 12 hours) and 0-4, 4-8, 8-12, 12-24, 24-48, 48-72 hours post-dose.
Results and safety
This study is still under way. Results are not available in the source record yet.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 25 Sep 2026.
- Individual participant dataSharing planned: No. Individual participant data (IPD) will not be shared because this is a first-in-human or early-stage clinical trial involving a novel investigational drug. The data contain proprietary and confidential information that could compromise ongoing patent applications and future commercial development. Public data sharing at this stage may also violate our confidentiality agreements with the contract research organization (CRO) and regulatory authorities. Therefore, IPD sharing is not feasible until the drug receives market approval or the primary study results are fully published.
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part.
The record lists no contact. Use the official record to reach the sponsor.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing HW243040 in people with Healthy Volunteers, run by The Third Xiangya Hospital of Central South University.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 8 inclusion and 26 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: opening soon, as of the sponsor's last update on 25 Sep 2026. Status can change between updates, so confirm with the study contact before making plans.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. Some participants in this study may receive a placebo. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
This study is still under way. Results are not available in the source record yet.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Incidence of Treatment-Emergent Adverse Events (TEAEs) (time frame: From signing of informed consent form through follow-up period (until AE resolution; up to Day 4 for SAD 50/150/300/900/1200 mg, Day 11 for 600 mg FE, Day 8 for MAD cohorts).). The study lists 4 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 25 Sep 2026.