In this study, we will investigate how quickly and to what extent etrumadenant is absorbed, transported, and eliminated from the body. For this study, etrumadenant is radioactively labelled with carbon 14 (14C). In this way, etrumadenant can be…
ID
Source
Brief title
Condition
- Other condition
Synonym
Health condition
Cancer, tumors
Research involving
Sponsors and support
Intervention
Outcome measures
Primary outcome
- To determine the time course of excretion of total radioactivity in urine and
feces after a single oral dose of 150 mg [14C] etrumadenant containing 3.7 MBq
of radioactivity.
- To determine the recovery of total radioactivity (mass balance) as a
percentage of the administered dose after a single oral dose of 150 mg
[14C]-etrumadenant containing 3.7 MBq of radioactivity.
- To determine the percentage of total radioactivity present as [14C]
etrumadenant in urine and feces at selected time points after a single oral
dose of 150 mg [14C] etrumadenant containing 3.7 MBq of radioactivity.
- To assess the safety and tolerability of a single oral dose of 150 mg [14C]
etrumadenant containing 3.7 MBq of radioactivity.
Secondary outcome
- To assess the pharmacokinetics (PK) of total radioactivity etrumadenant and
selected metabolites in plasma after a single oral dose of 150 mg
[14C]-etrumadenant containing 3.7 MBq of radioactivity.
- To determine the percentage of total radioactivity associated with
erythrocytes in whole blood over time after a single oral dose of 150 mg
[14C]-etrumadenant containing 3.7 MBq of radioactivity.
Background summary
Etrumadenant is a compound that may potentially be used for the treatment of
cancer. Etrumadenant inhibits the functioning of adenosine. Adenosine is a
substance produced inside tumors and has a powerful suppressive effect on the
immune system. The immune system is a complex system of cells and proteins that
defends the body against infection and cancer. By suppressing the immune
system, adenosine creates an environment inside tumors in which cancer cells
can easily grow. By inhibiting the functioning of adenosine, functioning of
immune cells may be restored resulting in tumor cell death.
Study objective
In this study, we will investigate how quickly and to what extent etrumadenant
is absorbed, transported, and eliminated from the body. For this study,
etrumadenant is radioactively labelled with carbon 14 (14C). In this way,
etrumadenant can be traced in blood, urine, and feces.
We will also investigate how safe etrumadenant is and how well it is tolerated.
Etrumadenant has been given to humans before in medical-scientific studies. In
addition, it has been extensively tested in the laboratory and on animals.
Study design
For the study, it is necessary that the volunteers stays in the research center
for 1 period of 13 to 16 days (12 to 15 nights), and possibly 2 additional
24-hour visits.
Day 1 is the day when the volunteer receive the study compound.
During the stay, the urine and feces will be collected and the blood will be
sampled each day to measure the amount of radioactivity. The volunteer should
be aware that leaving the research center will be dependent on the amount of
radioactivity in their blood, urine, and feces.
If the amount of radioactivity is still above predefined levels on Day 12 the
volunteer will stay in the research center for a maximum of 3 additional days
(up to Day 15). From Day 12 onwards, we will determine if he can leave the
research center on a daily basis.
If the amount of radioactivity is still above predefined levels on Day 14, the
volunteer will get milk of magnesia (magnesium hydroxide) to promote defecation.
The volunteer will be given 150 mg of 14C-labeled etrumadenant with an oral
syringe (without needle) on Day 1. This amount contains 3.7 MBq radioactivity
(this corresponds to a radiation exposure of 0.40 mSv, which is comparable with
2 months of background radiation. See Section 7.0 for more information). After
intake of the study compound, the volunteer is required to drink 240 mL of
water to rinse the mouth. The study compound may taste bad. If that is still
the case after drinking the water and completing the palatability
questionnaire, the volunteer will receive apple sauce to remove the taste. All
participants will receive the same study compound.
Intervention
The volunteer will be given 150 mg of 14C-labeled etrumadenant with an oral
syringe (without needle) on Day 1. This amount contains 3.7 MBq radioactivity
(this corresponds to a radiation exposure of 0.40 mSv, which is comparable with
2 months of background radiation. See Section 7.0 for more information). After
intake of the study compound, the volunteer is required to drink 240 mL of
water to rinse the mouth. The study compound may taste bad. If that is still
the case after drinking the water and completing the palatability
questionnaire, the volunteer will receive apple sauce to remove the taste. All
participants will receive the same study compound.
During this study, the volunteer might also receive milk of magnesia (magnesium
hydroxide), a compound registered for use as a laxative.
Study burden and risks
Blood draw
Drawing blood may be painful or cause some bruising. The use of the indwelling
cannula can sometimes lead to inflammation, swelling, hardening of the vein,
blood clotting, and bleeding in the environment of the puncture site. In some
individuals, a blood draw can sometimes cause pallor, nausea, seating, low
heart rate, or drop in blood pressure with dizziness or fainting.
In total, we will take about 482 milliliters of blood from the volunteer from
screening to follow-up. This amount does not cause any problems in adults. To
compare: a blood donation involves 500 mL of blood being taken at once each
time. If the investigator thinks it is necessary for the safety of a
participant, extra samples might be taken for possible additional testing. If
this happens, the total amount of blood drawn may be more than the amount
indicated above.
Heart tracing
To make a heart tracing, electrodes will be placed on the arms, chest and legs.
Prolonged use of these electrodes can cause skin irritation.
Fasting
If the volunteer has to fast for a prolonged time during the study, this may
lead to symptoms such as dizziness, headache, stomach upset, or fainting.
Coronavirus test
Samples for the coronavirus test will be taken from the back of the nose and
throat using swabs. Taking the samples only takes a few seconds, but can cause
discomfort and can give an unpleasant feeling. Taking a sample from the back of
the throat may cause the volunteer to gag. When the sample is taken from the
back of the nose, the volunteer may experience a stinging sensation and the
eyes may become watery.
Point Eden Way 3928
Hayward CA 94545
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Point Eden Way 3928
Hayward CA 94545
US
Listed location countries
Age
Inclusion criteria
1. Sex at birth : male.
2. Age : 18 to 55 years, inclusive, at screening.
3. Body mass index (BMI) : 18.0 to 32.0 kg/m2, inclusive, at screening.
4. Body weight : >=50 kg, inclusive, at screening.
5. Status : healthy subjects.
Further criteria apply, see protocol.
Exclusion criteria
1. Employee of PRA or the Sponsor.
2. History of relevant drug and/or food allergies.
3. Using tobacco products within 2 months prior to drug administration.
4. History of alcohol abuse or drug addiction (including soft drugs like
cannabis products) over the past 2 years.
5. Positive drug and alcohol screen (opiates, methadone, cocaine, amphetamines
[including ecstasy], cannabinoids, barbiturates, benzodiazepines, tricyclic
antidepressants, and alcohol) at screening or (first) admission to the clinical
research center.
Further criteria apply, see protocol.
Design
Recruitment
Medical products/devices used
Followed up by the following (possibly more current) registration
No registrations found.
Other (possibly less up-to-date) registrations in this register
No registrations found.
In other registers
| Register | ID |
|---|---|
| EudraCT | EUCTR2022-000822-50-NL |
| CCMO | NL81099.056.22 |