A single-center, open-label study to investigate the mass balance, excretion pathways, and metabolites after a single oral dose of 500 mg, 3.7 MBq, [14C]BTZ-043 in healthy male volunteers
- Conditions
- Tuberculosis
- Registration Number
- NL-OMON50849
- Lead Sponsor
- niversity Hospital LMU Klinikum
- Brief Summary
Not available
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- Completed
- Sex
- Not specified
- Target Recruitment
- 4
1. Sex : male
2. Age : 18 years to 55 years, inclusive, at screening.
3. Body mass index (BMI) : 18.0 to 29.0 kg/m2, inclusive, at screening.
4. Weight : 55 to 90 kg, inclusive, at screening.
5. Status : healthy subjects.
6. Male subjects, if not surgically sterilized, must agree to use adequate
contraception and not donate sperm from admission to the clinical research
center until 90 days after the follow-up visit. Adequate contraception for the
male subject (and his female partner, if she is of childbearing potential) is
defined as using hormonal contraceptives or an intrauterine device combined
with at least 1 of the following forms of contraception: a diaphragm, a
cervical cap, or a condom. Total abstinence, in accordance with the lifestyle
of the subject, is also acceptable.
7. All prescribed medication must have been stopped at least 30 days prior to
admission to the clinical research center.
8. All over-the-counter medications, vitamin preparations (especially vitamin
C), other food supplements, and herbal medications (eg, St. John*s wort) must
have been stopped at least 14 days prior to admission to the clinical research
center. An exception is made for paracetamol, which is allowed up to 48 hours
prior to study drug administration.
9. No vaccination within 14 days prior to study drug administration.
10. Ability and willingness to abstain from alcohol from 48 hours (2 days)
prior to screening and admission to the clinical research center.
11. Ability and willingness to abstain from methylxanthine-containing beverages
or food (coffee, tea, cola, chocolate, and energy drinks), grapefruit (juice),
corn (whole corn kernels and popcorn), cruciferous vegetables, and bitter
oranges from 48 hours (2 days) prior to admission to the clinical research
center.
12. Good physical and mental health on the basis of medical history, physical
examination, clinical laboratory, ECG, and vital signs, as judged by the
Investigator.
13. Willing and able to sign the ICF.
1. Participation in another study with a radiation burden of >0.1 mSv and <=1
mSv in the period of 1 year prior to screening; a radiation burden of >1.1
mSv and <=2 mSv in the period of 2 years prior to screening; a radiation burden
of >2.1 mSv and <=3 mSv in the period of 3 years prior to screening, etc.
2. Exposure to radiation for diagnostic reasons (except dental X-rays and plain
X-rays of thorax and bony skeleton [excluding spinal column]), or during work
within 1 year prior to drug administration.
3. Irregular defecation pattern (less than once per day on average).
4. Employee of PRA, Nuvisan, or the Sponsor.
5. History of relevant drug and/or food allergies.
6. Using tobacco products within 60 days prior to drug administration.
7. History of alcohol abuse or drug addiction (including soft drugs like
cannabis products).
8. Positive drug and alcohol screen (opiates, methadone, cocaine, amphetamines
[including ecstasy], cannabinoids, barbiturates, benzodiazepines,
gamma-hydroxybutyric acid, tricyclic antidepressants, and alcohol) at screening
or admission to the clinical research center.
9. Average intake of more than 24 grams of alcohol per day.
10. Positive screen for hepatitis B surface antigen (HBsAg), hepatitis C virus
(HCV) antibodies, or HIV 1 and 2 antibodies.
11. Participation in a drug study within 30 days prior to drug administration
in the current study. Participation in more than 4 drug studies in the 12
months prior to drug administration in the current study.
12. Donation or loss of more than 450 mL of blood within 60 days prior to drug
administration. Donation or loss of more than 1.5 liters of blood in the 10
months prior to drug administration in the current study.
13. Significant and/or acute illness within 5 days prior to drug administration
that may impact safety assessments, in the opinion of the Investigator.
14. Unwillingness to consume the Food and Drug Administration (FDA)-recommended
high-fat breakfast.
15. Unsuitable veins for infusion or blood sampling.
16. Positive nasopharyngeal PCR test for SARS-CoV-2 on Day -1.
Study & Design
- Study Type
- Interventional
- Study Design
- Not specified
- Primary Outcome Measures
Name Time Method <p>- To determine the rates and routes of excretion of [14C]BTZ-043-related<br /><br>radioactivity, including mass balance of total drug-related radioactivity in<br /><br>urine and feces (and vomit, if applicable), following the oral administration<br /><br>of a single 500 mg dose of [14C]BTZ-043 in healthy male volunteers.<br /><br><br /><br>- To determine the PK of total radioactivity in whole blood and in plasma.<br /><br><br /><br>- To characterize the plasma PK of BTZ-043 and main metabolites by liquid<br /><br>chromatography-mass spectrometry (LC-MS), if applicable.<br /><br><br /><br>- To characterize the urine concentrations of BTZ-043 and main metabolites by<br /><br>LC-MS, if applicable.</p><br>
- Secondary Outcome Measures
Name Time Method <p>- To assess the safety and tolerability of a single 500 mg oral dose of BTZ-043<br /><br>administered to healthy male volunteers.</p><br>