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A Pharmacokinetic Study of the Food Effect on Flonoltinib Maleate Tablets

Not Applicable
Completed
Conditions
Heathly Subjects
Interventions
Drug: flunotinib
Registration Number
NCT07193576
Lead Sponsor
Chengdu Zenitar Biomedical Technology Co., Ltd
Brief Summary

A Randomized, Open-Label, Two-Period, Two-Crossover Study to Evaluate the Effect of Food on the Pharmacokinetics of Flonoltinib Maleate Tablets in Healthy Subjects Under Fed Conditions

Detailed Description

Primary Study Objective. To evaluate the effect of a high-fat diet on the pharmacokinetics of single-dose oral Flonoltinib Maleate tablets in healthy subjects.

Secondary Study Objectives To evaluate the safety of single-dose oral administration of Flonoltinib Maleate Tablets under Fast or Fed condition in healthy subjects.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
24
Inclusion Criteria
  1. 18 to 45 years old (including 18 and 45 years old), gender is not limited;
  2. Male subjects weighing ≥50.0 kg, female subjects ≥45.0 kg, with body mass index (BMI) between 19.0 and 25.0 kg/m2 (including borderline values);
  3. Fully understand the content of the trial, the test drug, the trial process, etc, and be able to communicate well with the researcher, willing to comply with the study regulations, participate in the trial voluntarily and sign an Inform consent.
Exclusion Criteria
  1. Those with a history of severe allergies (e.g, angioedema and anaphylaxis), allergies (Screening Consultation/Admission Consultation) Those with a history of severe allergy (e.g, angioedema and anaphylaxis), allergy (e.g, allergy to pollen, two or more medications/foods), or history of food or drug allergy or other metabolic disorders (e.g, asthma, hives, eczematous dermatitis, etc.) judged by the investigator to be clinically significant, or a known allergy to JAK inhibitors or an allergy to excipient components of the test medication;
  2. Abnormal and clinically significant results of physical examination, vital signs, 12-lead electrocardiogram, laboratory tests (including routine blood, blood biochemistry, urine routine, blood pregnancy (only for women of childbearing age), infectious disease screening, antinuclear antibody, coagulation function, tuberculosis antibody, chest X-ray, abdominal ultrasound) prior to enrolment;
  3. QTcF > 440 ms for males and > 460 ms for females on ECG during the screening period;
  4. Those who have undergone major surgical procedures within 3 months prior to screening or plan to undergo surgery during the trial period;
  5. Acute illness within 2 weeks prior to screening; clinically significant infection (e.g, upper respiratory tract infection, nasopharyngitis, urinary tract infection, etc.) within 3 months prior to screening; evidence of any infection within 7 days prior to screening; history of herpes simplex infection, or recurrent (>once) herpes zoster or disseminated herpes zoster;
  6. History of any clinically serious disease or any disease or condition that, in the opinion of the investigator, may affect the outcome of the trial, including but not limited to a history of circulatory, endocrine, neurological, gastrointestinal, urinary, or haematological, immunological, psychiatric, and metabolic disorders;
  7. Dysphagia or any history of gastrointestinal disorders (or gastrointestinal resection, etc.) affecting drug absorption; 8 . Those with irregular bowel movements and habitual constipation or diarrhoea;

9. Those with a history of lipid metabolism defects, such as: familial hyperlipidaemia, lipoid nephropathy, or patients with acute pancreatitis accompanied by hyperlipidaemia; 10. Those with a positive combined urine multi-drug test (including morphine, methamphetamine, ketamine, methylenedioxyamphetamine, tetrahydrocannabinolic acid); 11. Those with a history of previous drug abuse or drug dependence; 12. Anyone who has been vaccinated within 8 weeks prior to screening or who plan to be vaccinated during the course of the study or within 8 weeks of administration of study drug; 13. Anyone who has donated or lost ≥400 mL of blood or received a blood transfusion within 3 months prior to screening; or anyone who has donated blood or blood components within 1 month of the planned end of the trial; 14. Those with special dietary requirements or those who are unable to comply with the uniform dietary and appropriate regulations of the study center; 15. Those who have smoked more than 3 cigarettes/day or equivalent amount of tobacco in the 3 months prior to screening; or who have consumed ≥14 units of alcohol per week (1 unit equals to 17.5mL or 14g of pure alcohol, which is approximately equal to 35mL of 50° white wine or 350mL of 5° beer); or who do not agree to abstain from smoking or drinking alcohol for the duration of the trial; or those who have a positive result from an alcohol breathalyzer test; 16. Any person who has taken any prescription drug, over-the-counter drug, any vitamin product or herbal medicine (JAK inhibitor, immunosuppressant, etc.) within 14 days prior to screening; 17. Those who have combined strong inducers of liver metabolism enzymes (e.g, omeprazole, barbiturates, carbamazepine, amiloride, pallidomycin, aminoglutethimide, phenytoin, grumet, rifampicin, sulfinpyrazone, roxithromycin, etc.) within the 4 weeks (28 days) prior to Screening, or any other history of medication use that in the judgement of the Investigator has the potential to interfere with in vivo pharmacokinetics of the test drug. Anyone who has taken any drug known to cause prolongation of the QT/QTcF interval or a drug with a risk of causing torsades de pointes (TdP) within 4 weeks (28 days) prior to Screening; or drugs with a long half-life; 18. Anyone who consumed any food or drink containing caffeine (e.g. coffee, strong tea, cola, chocolate, etc.) or food containing grapefruit juice that may have an effect on metabolising enzymes or who consumed food or drink containing alcohol within 48 h prior to the administration of the drug; 19. Those who are participating in other clinical trials and have used an investigational drug, vaccine or device within 3 months prior to the first dose; 20. Pregnant or breastfeeding women or women of childbearing age who have had unprotected sex within 14 days prior to screening; 21. The subject or his/her partner is unwilling to use non-pharmacological contraception (e.g, total abstinence, condom, IUD, ligation, etc.) for contraception during the trial period or the subject and/or his/her partner has a pregnancy plan within 3 months of the administration of the study drug; 22. The subject may not be able to complete the study for other reasons or there are other factors that, in the opinion of the investigator, make participation in the trial unsuitable.

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
A groupflunotinibSubjects received Flonoltinib Maleate: under fast condition → washout → under fed condition
B groupflunotinibSubjects received Flonoltinib Maleate: under fed condition → washout → under fast condition
Primary Outcome Measures
NameTimeMethod
CmaxDay1 and Day11 Within 2hours before administration and 0.5 hours, 1 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 12hours, 24hours, 48 hours, 72 hours, 96 hours, 120hours, 144 hours after administration

maximum concentration

AUC0-tDay1 and Day11 Within 2 hours before administration and 0.5 hours, 1 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 12hours, 24hours, 48 hours, 72 hours, 96 hours, 120hours, 144 hours after administration

Area under the blood concentration-time curve from 0 o 'clock to the last measurable concentration at collection time t

AUC0-∞Day1 and Day11 Within 2 hours before administration and 0.5 hours, 1 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 12hours, 24hours, 48 hours, 72 hours, 96 hours, 120hours, 144 hours after administration

The area under the blood drug concentration-time curve from 0 to infinity time

TmaxDay1 and Day11 Within 2 hours before administration and 0.5 hours, 1 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 12hours, 24hours, 48 hours, 72 hours, 96 hours, 120hours, 144 hours after administration

time to peak

t1/2Day1 and Day11 Within 2 hours before administration and 0.5 hours, 1 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 12hours, 24hours, 48 hours, 72 hours, 96 hours, 120hours, 144 hours after administration

Terminal phase elimination half-life

tlagDay1 and Day11 Within 2 hours before administration and 0.5 hours, 1 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 12hours, 24hours, 48 hours, 72 hours, 96 hours, 120hours, 144 hours after administration

retardation time

CL/FDay1 and Day11 Within 2 hours before administration and 0.5 hours, 1 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 12hours, 24hours, 48 hours, 72 hours, 96 hours, 120hours, 144 hours after administration

apparent clearance

Vd/FDay1 and Day11 Within 2 hours before administration and 0.5 hours, 1 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 12hours, 24hours, 48 hours, 72 hours, 96 hours, 120hours, 144 hours after administration

apparent volume of distribution

λzDay1 and Day11 Within 2 hours before administration and 0.5 hours, 1 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 12hours, 24hours, 48 hours, 72 hours, 96 hours, 120hours, 144 hours after administration

Terminal elimination rate constant

%AUCexDay1 and Day11 Within 2 hours before administration and 0.5 hours, 1 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 12hours, 24hours, 48 hours, 72 hours, 96 hours, 120hours, 144 hours after administration

The extrapolation percentage of AUC0--∞

Secondary Outcome Measures
NameTimeMethod
health checkupScreening period, day 17 or early withdrawal

General examination

participants with abnormal vital signsScreening period,Day1to day7 and day11 to day17

blood pressure

participants with abnormal laboratory tests resultsScreening period, Day-1 (examination results within 7 days are acceptable), Day17, or early withdrawal

total cholesterol

Urinary albumin creatinine ratioD-1, D17 or early termination

Urinary albumin creatinine ratio

ECG QT IntervScreening period, Day-1 ,Day1, Day10, Day11, Day17 or early termination

12-lead electrocardiogram

adverse eventFrom date of randomization until the date of completion of data collection, assessed up to 17 days or early termination

Adverse events, serious adverse events, suspected and unexpected serious adverse reactions (SUSAR), priority adverse reactions, incidence of adverse reactions

participants with abnormal urinalysisScreening period, Day-1 , Day17, or early withdrawal

Glucose

Trial Locations

Locations (1)

Chengdu Xinhua Hospital

🇨🇳

Chengdu, Sichuan, China

Chengdu Xinhua Hospital
🇨🇳Chengdu, Sichuan, China

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