A Clinical Trial to Assess Absorption, Metabolism and Excretion of [14C]-LXI-15028 in Chinese Healthy Male Subjects - Mass Balance and Biotransformation Study of [14C]LXI-15028 in Humans
Overview
- Phase
- Phase 1
- Status
- Completed
- Enrollment
- 6
- Locations
- 1
- Primary Endpoint
- LXI-15028 and metabolite PK:t1/2
Overview
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.
Study Design
- Study Type
- Interventional
- Allocation
- Na
- Intervention Model
- Single Group
- Primary Purpose
- Health Services Research
- Masking
- None
Eligibility Criteria
- Ages
- 18 Years to 45 Years (Adult)
- Sex
- Male
- Accepts Healthy Volunteers
- Yes
Inclusion Criteria
- •Chinese healthy male subjects;
- •18 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.
Exclusion Criteria
- •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;
Arms & Interventions
[14C]LXI-15028(n=6-8)
Subjects will receive a single oral dose of [14C]LXI-15028 suspension under the fasted state .
Intervention: [14C]LXI-15028 (Drug)
Outcomes
Primary Outcomes
LXI-15028 and metabolite PK:t1/2
Time Frame: approximately 11 days
Elimination half-life.
Mass balance
Time Frame: approximately 11 days
Mass balance recovery of total radioactivity in urine and fecal samples
Metabolite Profiling
Time Frame: approximately 11 days
To provide plasma, urine and faecal samples for metabolite profiling and structural identification
Total radioactivity in plasma PK:t1/2
Time Frame: approximately 11 days
Elimination half-life.
LXI-15028 and metabolite PK:Cmax
Time Frame: approximately 11 days
Maximum plasma concentration
LXI-15028 and metabolite PK:Tmax
Time Frame: approximately 11 days
Time for Cmax
Total radioactivity in plasma PK:Tmax
Time Frame: approximately 11 days
Time for Cmax
Total radioactivity in plasma PK:CL/F
Time Frame: approximately 11 days
Drug clearance
Total radioactivity in plasma PK:AUC0-t
Time Frame: approximately 11 days
Area under the plasma concentration time profile from time 0 to time of the last quantifiable concentration.
Total radioactivity in plasma PK:Vd/F
Time Frame: approximately 11 days
Apparent volume of distribution following oral administration
LXI-15028 and metabolite PK:AUC0-t
Time Frame: approximately 11 days
Area under the plasma concentration time profile from time 0 to time of the last quantifiable concentration.
LXI-15028 and metabolite PK:AUC0-inf
Time Frame: approximately 11 days
Area under the plasma concentration time profile from time 0 to infinity.
LXI-15028 and metabolite PK:CL/F
Time Frame: approximately 11 days
Drug clearance
LXI-15028 and metabolite PK:Vd/F
Time Frame: approximately 11 days
Apparent volume of distribution following oral administration
Secondary Outcomes
- Adverse events(approximately 11 days)