Mass Balance and Biotransformation Study of [14C]LXI-15028 in Humans

NCT05883306 | Completed Phase 1

• 1 other identifier: NE822201
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

To assess absorption, metabolism and excretion of \[14C\]-LXI-15028 in Chinese healthy male Subjects following a single oral dose of \[14C\]LXI-15028 suspension.

Conditions

Healthy Subjects; Pharmacokinetics of 14C-labeled of LXI-15028

Outcome Measures

Primary Outcomes (14)

• Mass balance

  Mass balance recovery of total radioactivity in urine and fecal samples

  approximately 11 days

• Metabolite Profiling

  To provide plasma, urine and faecal samples for metabolite profiling and structural identification

  approximately 11 days

• Total radioactivity in plasma PK:Tmax

  Time for Cmax

  approximately 11 days

• Total radioactivity in plasma PK:AUC0-t

  Area under the plasma concentration time profile from time 0 to time of the last quantifiable concentration.

  approximately 11 days

• Total radioactivity in plasma PK:t1/2

  Elimination half-life.

  approximately 11 days

• Total radioactivity in plasma PK:CL/F

  Drug clearance

  approximately 11 days

• Total radioactivity in plasma PK:Vd/F

  Apparent volume of distribution following oral administration

  approximately 11 days

• LXI-15028 and metabolite PK:Cmax

  Maximum plasma concentration

  approximately 11 days

• LXI-15028 and metabolite PK:Tmax

  Time for Cmax

  approximately 11 days

• LXI-15028 and metabolite PK:AUC0-t

  Area under the plasma concentration time profile from time 0 to time of the last quantifiable concentration.

  approximately 11 days

• LXI-15028 and metabolite PK:AUC0-inf

  Area under the plasma concentration time profile from time 0 to infinity.

  approximately 11 days

• LXI-15028 and metabolite PK:t1/2

  Elimination half-life.

  approximately 11 days

• LXI-15028 and metabolite PK:CL/F

  Drug clearance

  approximately 11 days

• LXI-15028 and metabolite PK:Vd/F

  Apparent volume of distribution following oral administration

  approximately 11 days

Secondary Outcomes (1)

• Adverse events

  approximately 11 days

Study Arms (1)

[14C]LXI-15028(n=6-8)

EXPERIMENTAL

Subjects will receive a single oral dose of \[14C\]LXI-15028 suspension under the fasted state .

Drug: [14C]LXI-15028

Interventions

[14C]LXI-15028 DRUG

\[14C\]LXI-15028

[14C]LXI-15028(n=6-8)

Eligibility Criteria

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

You may qualify if:

• Chinese healthy male subjects;
• to 45 years of age (inclusive)
• Body mass index (BMI) of 19-26 kg/m2 (inclusive), and body weight not less than 50 kg (inclusive)
• Voluntarily signing the ICF
• Ability to communicate well with the investigator and compliance to complete the trial according to the protocol.

You may not qualify if:

• Clinically significant abnormality of physical examination, vital signs, routine laboratory tests (hematology, blood chemistry, coagulation, urinalysis, stool routine + occult blood, and thyroid function), 12-lead ECG, chest CT, and abdomen ultrasound (liver, gallbladder, pancreas, spleen, and kidneys), etc.
• Resting QT interval (QTcF) ≥ 450 ms by 12-lead electrocardiogram (ECG)
• Hepatitis B surface antigen or hepatitis B e antigen test, hepatitis C virus antibody IgG test, human immunodeficiency virus antigen/antibody combination test, or Treponema pallidum antibody test is positive
• Novel coronavirus infection screening shows C-reactive protein is clinically significant abnormality, or COVID-19 nucleic acid test is positive
• Use of any drugs inhibiting or inducing hepatic drug metabolizing enzymes within 30 days before screening;
• Use of any prescription drugs, over-the-counter drugs, Chinese herbal medicines, or dietary supplements such as vitamins and calcium supplements within 14 days before screening;
• History of any clinical critical illness or presence of diseases or conditions that the investigator considers may affect the trial results, including but not limited to diseases of cardiovascular system, circulatory system, respiratory system, endocrine system, nervous system, digestive system, urinary system or blood, immune system, and psychiatric system, especially metabolism and nutrition diseases and gastrointestinal diseases;
• Major surgery within 6 months before screening or incomplete healing of surgical incision, the major surgeries including but not limited to any procedures that have significant risk of hemorrhage, prolonged general anesthesia, open biopsy, or marked traumatic invasive injury;
• Subjects with an allergic constitution (e.g., history of bronchial asthma, allergy to food and pollen, allergy to two or more drugs, or history of allergy), including any previous serious adverse reaction to proton pump inhibitors or potassium-competitive acid blockers (e.g., omeprazole, rabeprazole, lansoprazole, and vonoprazan), or known hypersensitivity to penicillin or cephalosporin antibiotics; or those who may be hypersensitive to the investigational drug or its excipients, as judged by the investigator;
• Hemorrhoids or perianal diseases with regular/current hematochezia, irritable bowel syndrome, and inflammatory bowel disease;
• Habitual constipation or diarrhea;
• Alcoholism or frequent alcohol use within 6 months before screening, i.e., weekly alcohol consumption \> 14 units (1 unit = 360 mL of beer or 45 mL of ABV 40% spirit or 150 mL of wine); or positive alcohol breath test result at Screening;
• Daily smoking exceeding 5 cigarettes (≥ 5 cigarettes) within 3 months before Screening, or habitual use of nicotine-containing products and inability to withdraw during the trial period;
• Drug abuse, use of soft drug (e.g., marijuana) within 3 months before screening, or use of hard drug (e.g., cocaine, amphetamines, phencyclidine, etc.) within 1 year before screening; or positive urine drug test at screening;
• Drinking excessive tea, coffee and/or caffeine-containing beverages (over 8 cups, 1 cup = 250 mL) on a daily basis within 3 months prior to screening;

Sponsors & Collaborators

• Shandong Luoxin Pharmaceutical Group Stock Co., Ltd.: lead

Study Sites (1)

The First Affiliated Hospital of Soochow University

Suzhou, Jiangsu, 215006, China

Location

Related Publications (1)

• Bian Y, Yuan J, Ma S, Nan J, Gu Z, Feng H, Yu Z, Liu Z, Xie F, Wang Y, Liu C, Zhang H, Miao L. Mass balance and metabolite profiles in humans of tegoprazan, a novel potassium-competitive acid blocker, using 14C-radiolabelled techniques. Expert Opin Drug Metab Toxicol. 2025 Jul;21(7):897-907. doi: 10.1080/17425255.2025.2505637. Epub 2025 May 13.

  PMID: 40349123 DERIVED

Study Officials

• Liyan Miu

  The First Affiliated Hospital of Soochow University

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: HEALTH SERVICES RESEARCH
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: May 10, 2023
• First Posted: May 31, 2023
• Study Start: June 30, 2022
• Primary Completion: July 21, 2022
• Study Completion: December 23, 2022
• Last Updated: May 31, 2023

Record last verified: 2023-05

Locations

CN (1)