Mass Balance of [14C] TQ05105 in Healthy Chinese Subjects
Conditions
Brief summary
To analyze radioactivity excretion and pharmacokinetics in healthy subjects after a single oral dose of \[¹⁴C\]TQ05105, identifying excretion routes, major metabolites, and biotransformation pathways. Secondary: To determine pharmacokinetics of TQ05105 and metabolites (e.g., TQ12550) via Liquid Chromatography-Tandem Mass Spectrometry (LC-MS/MS) and assess treatment safety.
Interventions
DRUGTQ05105
Janus Kinase 2 (JAK2) inhibitor
Sponsors
Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
Study design
Allocation
NON_RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy adult male; * Age: 18-45 years (inclusive); * Body weight: Body mass index (BMI) between 19-26 kg/m² (inclusive), with a minimum body weight of 50 kg; * Voluntarily signs the informed consent form; * The subject is able to communicate well with the investigator and able to complete the trial in accordance with the protocol requirements.
Exclusion criteria
* Abnormalities with clinical significance detected in comprehensive physical examination, routine laboratory tests (complete blood count, blood biochemistry, coagulation function, urinalysis, fecal routine), thyroid function, 12-lead electrocardiogram, chest CT, abdominal ultrasound (liver, gallbladder, pancreas, spleen, kidneys), etc.; * Abnormal vital signs that remain abnormal upon retesting; * Abnormalities with clinical significance in ophthalmic examinations (slit-lamp, intraocular pressure, and fundus photography); * Positive results for Hepatitis B surface antigen (HBsAg), Hepatitis C virus antibody IgG (Anti-HCV IgG), human immunodeficiency virus antibody (HIV-Ag/Ab), or syphilis antibody; * Positive nucleic acid test result for Coronavirus Disease 2019 (COVID-19); * Use of any drugs known to inhibit or induce hepatic drug-metabolizing enzymes within 30 days prior to screening (see Appendix 1 for details); * Use of any prescription drugs, over-the-counter medications, Chinese herbal health products, or dietary supplements (e.g., vitamins, calcium supplements) within 14 days prior to screening; * History or presence of clinically significant diseases affecting the musculoskeletal, neuropsychiatric, endocrine, circulatory, respiratory, digestive, urinary, or reproductive systems, as judged by the investigator; * Any medical condition that increases the risk of elevated blood glucose, such as a history of primary diabetes, steroid-induced diabetes, other secondary diabetes, acute or chronic pancreatitis, deemed clinically significant by the investigator; * History of organic heart disease, heart failure, myocardial infarction, angina, unexplained arrhythmia, torsades de pointes, ventricular tachycardia, atrioventricular block, or long QT syndrome (or related symptoms/family history), deemed clinically significant by the investigator; * History of interstitial lung disease, severely impaired lung function, severe pulmonary fibrosis, radiation pneumonitis, drug-induced lung disease, or evidence of active pulmonary inflammation on screening chest CT, deemed clinically significant by the investigator; * Major surgery within 6 months prior to screening or incomplete wound healing; major surgery includes procedures with significant bleeding risk, prolonged general anesthesia, open biopsy, major traumatic injury, or surgery affecting drug absorption, distribution, metabolism, or excretion; or planned surgery during the study; * History of drug, environmental, or food allergies, allergic constitution, or potential allergy to the investigational drug or its excipients, as judged by the investigator; * Hemorrhoids or perianal diseases with regular/active bleeding, irritable bowel syndrome, or inflammatory bowel disease; * Factors affecting oral administration or drug absorption (e.g., swallowing difficulties, gastrointestinal resection, ulcerative colitis, symptomatic/inflammatory bowel disease, intestinal obstruction, etc.); * Habitual constipation or diarrhea; * Lactose intolerance (history of diarrhea after consuming milk); * Alcohol abuse or regular alcohol consumption within 6 months prior to screening (\>14 units per week; 1 unit = 360 mL beer, 45 mL 40% spirits, or 150 mL wine); inability to abstain during the trial, or positive alcohol breath test (\>0 mg/100 mL) at screening; * Smoking \>5 cigarettes daily within 3 months prior to screening or habitual use of nicotine products, and inability to abstain during the trial; * Drug abuse or use of soft drugs (e.g., marijuana) within 3 months prior to screening, or hard drugs (e.g., cocaine, amphetamines, phencyclidine) within 1 year prior to screening; or positive urine drug screen at screening; * Habitual consumption of grapefruit juice or excessive tea, coffee, and/or caffeine-containing beverages, and inability to abstain during the trial; * Occupation involving long-term exposure to radiation conditions; or significant radiation exposure within 1 year prior to the trial (≥2 chest/abdominal CT scans or ≥3 other X-ray examinations); or prior participation in radioactive drug-labeled trials; * History of needle or blood phobia, difficulty with blood collection, or inability to tolerate venipuncture; * Participation in other clinical trials involving investigational drugs or devices within 3 months prior to or during screening, or planned participation during this study; or non-personal participation in clinical trials; * Vaccination within 1 month prior to screening or planned vaccination during the trial; * Plans for reproduction or sperm donation during the trial or within 1 year after completion, or unwillingness to use strict contraception during and within 1 year after the trial (see Appendix 3 for details); * Blood loss or donation ≥400 mL within 3 months prior to screening, or blood transfusion within 1 month prior to screening; * Other reasons deemed by the investigator to make the subject unsuitable for participation, or voluntary withdrawal by the subject.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| loss rate | From 24 hours prior to administration to 504 hours post-administration | Total radioactive recovery rate and cumulative total radioactive recovery rate in excreta (urine and feces) for each time interval. |
| Peak concentration (Cmax) | Before administration, 0.16, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 216, 264, 336 hours after administration | Maximum plasma drug concentration |
| Area under drug time curve (AUC0-∞) | Before administration, 0.16, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 216, 264, 336 hours after administration | Area under the plasma concentration-time curve from time 0 extrapolated to infinite time |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Adverse event rate | From before the first administration to 7 days after the administration | Incidence and severity of adverse events and serious adverse events, and abnormal laboratory examination indicators. |
Countries
China
Outcome results
None listed