Clinical trial NCT04476394: Open-label Study to Assess the Absorption, Metabolism, Excretion, and Mass Balance of a Single Oral Dose of [14C]-20 mg/100 μCi Anaprazole Sodium Enteric-coated Capsule in Healthy Adult Male Subjects
Official title: A Single-center, Open, Single Dose Mass Balance Study to Assess the Absorption, Metabolism, Excretion of [14C]-20 mg/100 μCi Anaprazole Sodium Enteric-coated Capsule in Chinese Health Adult Male Subjects
Study type: INTERVENTIONAL
Overall status: UNKNOWN
Phase: PHASE1
Conditions: Healthy Male Volunteers
Lead sponsor: Sihuan Pharmaceutical Holdings Group Ltd.
Sponsor class: INDUSTRY
First posted: 2020-07-20
Enrollment: 6
Sex: MALE
Minimum age (years): 18
Maximum age (years): 45
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: NA
Intervention model: SINGLE_GROUP
Primary purpose: TREATMENT

Brief summary: This is an open-label, single-dose, absorption, metabolism, excretion, and mass balance study following a single oral dose of \[14C\]-20 mg/100 μCi Anaprazole Sodium enteric-coated capsule in healthy adult male subjects. Whole blood, plasma samples will be collected at hour 0 pre-dose and 1，2，3，4，5，6，8，12，24，48，72，96，120，144，168 hours post-dose (tentative, adjusted according to plasma drug concentration); urine samples will be collected at hour 24 pre-dose and 0-4，4-8，8-12，12-24，24-48，48-72，72-96，96-120，120-144，144-168，168-192，192-216，216-240 hours post-dose (tentative, adjusted according to sample recovery rate) ; fecal samples will be collected at hour 24 pre-dose and 0-24，24-48，48-72，72-96，96-120，120-144，144-168，168-192，192-216，216-240 hours post-dose (tentative, adjusted according to sample recovery rate) following the start of administration to measure total radioactivity and plasma drug concentrations.


Eligibility criteria: Inclusion Criteria:

* 1.The subject is a Chinese adult male, aged 18 to 45 years, inclusive.
* 2.The subject weighed at least 50.0 kg and had a body mass index (BMI) between 19.0 kg/m\^2 and 26.0 kg/m\^2, inclusive.
* 3. Participants with evaluations of vital signs, physicial examination results,clinical laboratory and ECG testing outside the reference range that are deemed not clinically significant at investigator discretion at screening.
* 4.The subject with childbearing potential agrees that the subject and his sexual partner use adequate contraception from signing of informed consent throughout the duration of the study and for 6 months after study completion.
* 5.The subject is capable of understanding and complying with protocol requirements, and signed and dated a written informed consent form voluntarily

Exclusion Criteria:

* 1.Has clinical significant drug allergy or allergic disease history(Such as asthma, urticaria, eczema dermatitis, etc), or has hypersensitivity or allergy to investigatory drugs or related supplements；
* 2.Has clinical significant ECG abnormal history or family history of long QT syndrome(Grandparents, parents and siblings)
* 3.Any disease or medical history that may significantly affect the absorption, distribution, metabolism, and excretion of drugs, or any condition that may pose a hazard to the subject. Such as:

  * Inflammatory bowel disease, gastric ulcer, duodenal ulcer, gastrointestinal / rectal bleeding, persistent nausea, or other clinically significant gastrointestinal abnormalities;
  * Has suffered from gastrointestinal diseases or complications that may affect the absorption of drugs (ie: malabsorption, gastroesophageal reflux, peptic ulcer, erosive esophagitis, frequent heartburn) within 6 months before screening or had history of gastrointestinal surgery (for example: gastrectomy, gastrointestinal anastomosis, intestinal resection, gastric bypass, gastric segmentation or gastric banding, cholecystectomy, except for appendicitis surgery and proctectomy);
  * Evidence of liver disease or clinically impaired liver function at the time of screening (eg AST, ALT or total bilirubin\> 1.5 times ULN);
  * A history or evidence of nephropathy or renal insufficiency at the time of screening, showing clinically significant abnormality of creatinine or abnormal urine composition (such as proteinuria, creatinine\> 176.8 umol / L, etc.)
  * Has difficulty swallowing oral preparations.
* 4.Thyroid stimulating hormone (TSH)\> ULN; or serum free triiodothyronine (FT3)\> ULN; or serum free thyroxine (FT4)\> ULN at the time of screening;
* 5. Frequent smokers and alcoholics within 3 months before screening (smoke more than 5 cigarettes / day, drink more than 21 units of alcohol per week, 1 unit = 360 mL beer or 45 mL liquor or 150 mL wine), or can't stop using any tobacco products, and alcohol intake during the study period ; or those who have a positive alcohol breath test before enrollment;
* 6. Has received any investigational compound (including post-marketing investigational drugs) or participated in clinical trials of any drugs /devices within 3 months before screening;
* 7. A history of drug abuse within 12 months before screening or a positive urine test result at screening;
* 8. Has used any prescription drugs, non-prescription drugs (including chemical drugs, vitamin drugs, Chinese herbal medicines, etc.) within 4 weeks before administration of investigational drugs;
* 9. Has taken foods that affect CYP3A4 (such as grapefruit or beverages containing grapefruit) within 2 weeks before administration of investigational drugs;
* 10. Human immunodeficiency virus antibody, hepatitis B surface antigen, hepatitis C antibody, and Treponema pallidum specific antibody test results were positive at screening;
* 11. Has difficulty in venous blood collection or halo acupuncture;
* 12.Blood donation / blood loss ≥200 mL within 1 month, or ≥400 mL within 3 months before screening; or has blood donation plan during the period of medication of investigational drugs and within 3 months after drug withdrawal;
* 13. Has special dietary requirements and cannot follow the unified dietary arrangements;
* 14. Has particpated in another clinical study with radioactive labeling within 1 year before administration.
* 15. Has significant radiation exposure (Radiation exposure from chest X-ray, CT scan or barium meal examination more than once, or be engaged in radiation related occupations) within 1 year before administration.
* 16. Any conditions in which considered by investigator not be appropriate to participate in this trial.

Primary outcomes:
measure: Cmax of Anaprazole according to total radioactivity concentration equivalents in whole blood and plasma
timeFrame: Hour 0 pre-dose and 1，2，3，4，5，6，8，12，24，48，72，96，120，144，168 hours post-dose (tentative, adjusted according to plasma drug concentration)
measure: Tmax of Anaprazole according to total radioactivity concentration equivalents in whole blood and plasma
timeFrame: Hour 0 pre-dose and 1，2，3，4，5，6，8，12，24，48，72，96，120，144，168 hours post-dose (tentative, adjusted according to plasma drug concentration)
measure: AUC of Anaprazole according to total radioactivity concentration equivalents in whole blood and plasma
timeFrame: Hour 0 pre-dose and 1，2，3，4，5，6，8，12，24，48，72，96，120，144，168 hours post-dose (tentative, adjusted according to plasma drug concentration)
measure: Cumulative excretion and cumulative excretion rate in urine
timeFrame: Hour 24 pre-dose and 0-4，4-8，8-12，12-24，24-48，48-72，72-96，96-120，120-144，144-168，168-192，192-216，216-240 hours post-dose (tentative, adjusted according to sample recovery rate)
measure: Cumulative excretion and cumulative excretion rate in feces
timeFrame: Hour 24 pre-dose and 0-24，24-48，48-72，72-96，96-120，120-144，144-168，168-192，192-216，216-240 hours post-dose (tentative, adjusted according to sample recovery rate)
measure: Radioactivity spectrum indentification of metabolites in plasma
timeFrame: Hour 0 pre-dose and 1，2，3，4，5，6，8，12，24，48，72，96，120，144，168 hours post-dose (tentative, adjusted according to plasma drug concentration)
measure: Radioactivity spectrum indentification of metabolites in urine
timeFrame: Hour 24 pre-dose and 0-4，4-8，8-12，12-24，24-48，48-72，72-96，96-120，120-144，144-168，168-192，192-216，216-240 hours post-dose (tentative, adjusted according to sample recovery rate)
measure: Concentration of metabolites in feces
timeFrame: Hour 24 pre-dose and 0-24，24-48，48-72，72-96，96-120，120-144，144-168，168-192，192-216，216-240 hours post-dose (tentative, adjusted according to sample recovery rate)
Secondary outcomes:
Other outcomes:
Locations:
Study officials:
References: